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DK1259485T3 - Benzamider og beslægtede inhibitorer for faktor Xa - Google Patents

Benzamider og beslægtede inhibitorer for faktor Xa

Info

Publication number
DK1259485T3
DK1259485T3 DK01918257T DK01918257T DK1259485T3 DK 1259485 T3 DK1259485 T3 DK 1259485T3 DK 01918257 T DK01918257 T DK 01918257T DK 01918257 T DK01918257 T DK 01918257T DK 1259485 T3 DK1259485 T3 DK 1259485T3
Authority
DK
Denmark
Prior art keywords
factor
benzamides
compounds
related inhibitors
compositions
Prior art date
Application number
DK01918257T
Other languages
English (en)
Inventor
Penglie Zhang
Lingyan Wang
Wenrong Huang
Wenhao Li
Yonghong Song
Robert Scarborough
Bing-Yan Zhu
Erick Goldman
Jingmei Zuckett
Original Assignee
Millennium Pharm Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26881428&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DK1259485(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US09/663,420 external-priority patent/US6844367B1/en
Application filed by Millennium Pharm Inc filed Critical Millennium Pharm Inc
Application granted granted Critical
Publication of DK1259485T3 publication Critical patent/DK1259485T3/da

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
    • A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/12—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines
    • C07C259/18—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxamidine groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
    • C07C317/38—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atom of at least one amino group being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfones
    • C07C317/40—Y being a hydrogen or a carbon atom
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D213/82—Amides; Imides in position 3
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    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
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    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
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    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)
DK01918257T 2000-02-29 2001-02-28 Benzamider og beslægtede inhibitorer for faktor Xa DK1259485T3 (da)

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Families Citing this family (229)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6822267B1 (en) * 1997-08-20 2004-11-23 Advantest Corporation Signal transmission circuit, CMOS semiconductor device, and circuit board
ATE311366T1 (de) 2000-02-29 2005-12-15 Millennium Pharm Inc Benzamide und ähnliche inhibitoren vom faktor xa
AU776053B2 (en) 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
TWI288745B (en) 2000-04-05 2007-10-21 Daiichi Seiyaku Co Ethylenediamine derivatives
DE60130771T2 (de) 2000-07-27 2008-07-17 Eli Lilly And Co., Indianapolis Substituierte heterocyclische amide
DE60118774T2 (de) 2000-11-22 2007-03-15 Astellas Pharma Inc. Substituierte phenolderivate und deren salze als hemmstoffe von koagulations faktor x
EP1379506A2 (en) * 2000-11-28 2004-01-14 Eli Lilly And Company Substituted carboxamides
US7067539B2 (en) 2001-02-08 2006-06-27 Schering Corporation Cannabinoid receptor ligands
US7507767B2 (en) 2001-02-08 2009-03-24 Schering Corporation Cannabinoid receptor ligands
US7312235B2 (en) * 2001-03-30 2007-12-25 Millennium Pharmaceuticals, Inc. Benzamide inhibitors of factor Xa
WO2003000657A1 (en) 2001-06-20 2003-01-03 Daiichi Pharmaceutical Co., Ltd. Diamine derivatives
SE0102764D0 (sv) * 2001-08-17 2001-08-17 Astrazeneca Ab Compounds
AUPR738301A0 (en) * 2001-08-30 2001-09-20 Starpharma Limited Chemotherapeutic agents
US7868204B2 (en) 2001-09-14 2011-01-11 Methylgene Inc. Inhibitors of histone deacetylase
US6897220B2 (en) * 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
KR20100107509A (ko) 2001-09-14 2010-10-05 9222-9129 퀘벡 인코포레이티드 히스톤 데아세틸라아제의 억제제
HUP0401924A3 (en) 2001-11-14 2009-07-28 Schering Corp Cannabinoid receptor ligands, their use and pharmaceutical compositions containing them
EP1314733A1 (en) 2001-11-22 2003-05-28 Aventis Pharma Deutschland GmbH Indole-2-carboxamides as factor Xa inhibitors
US7030141B2 (en) * 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
US7449457B2 (en) 2001-12-07 2008-11-11 Eli Lilly And Company Substituted heterocyclic carboxamides with antithrombotic activity
WO2003090680A2 (en) * 2002-04-23 2003-11-06 Axys Pharmaceuticals, Inc. Novel phenyl derivatives as inducers of apoptosis
JP2005533809A (ja) 2002-06-19 2005-11-10 シェーリング　コーポレイション カンナビノイドレセプタアゴニスト
AR040336A1 (es) 2002-06-26 2005-03-30 Glaxo Group Ltd Compuesto de piperidina, uso del mismo para la fabricacion de un medicamento, composicion farmaceutica que lo comprende y procedimiento para preparar dicho compuesto
GB0215293D0 (en) 2002-07-03 2002-08-14 Rega Foundation Viral inhibitors
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
CN1309384C (zh) 2002-10-18 2007-04-11 弗·哈夫曼-拉罗切有限公司 具有5－ht6受体亲和性的4－哌嗪基苯磺酰基吲哚
GB0226930D0 (en) 2002-11-19 2002-12-24 Astrazeneca Ab Chemical compounds
PT1569912E (pt) 2002-12-03 2015-09-15 Pharmacyclics Llc Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia
TWI299664B (en) 2003-01-06 2008-08-11 Osi Pharm Inc (2-carboxamido)(3-amino)thiophene compounds
US7696225B2 (en) * 2003-01-06 2010-04-13 Osi Pharmaceuticals, Inc. (2-carboxamido)(3-Amino) thiophene compounds
KR20050096956A (ko) 2003-02-07 2005-10-06 다이이찌 세이야꾸 가부시기가이샤 피라졸 유도체
AR043633A1 (es) 2003-03-20 2005-08-03 Schering Corp Ligandos de receptores de canabinoides
WO2004087696A1 (de) * 2003-04-03 2004-10-14 Merck Patent Gmbh Pirazolidin-1,2-dicarbonsaüre-1-((phenyl)-amid)-2-((phenyl)-amid) derivate als koagulationsfaktor xa inhibitoren zur behandlung von thrombosen
KR20050118708A (ko) * 2003-04-03 2005-12-19 메르크 파텐트 게엠베하 혈전-색전 질환의 치료에서 응고 인자 ｘａ의 저해제로서사용하기 위한피롤리디노-１,２-디카르복시-１-(페닐아미드)-２-(４-(３-옥소-모르폴리노-４-일)-페닐아미드) 유도체 및 관련화합물
TWI372050B (en) 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
NZ544756A (en) 2003-07-22 2009-09-25 Astex Therapeutics Ltd 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
PL1667992T3 (pl) 2003-09-19 2007-05-31 Astrazeneca Ab Pochodne chinazoliny
EP1663953A1 (en) * 2003-09-24 2006-06-07 Methylgene, Inc. Inhibitors of histone deacetylase
SE0302573D0 (sv) * 2003-09-26 2003-09-26 Astrazeneca Ab Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
US7511066B2 (en) * 2003-09-30 2009-03-31 Eli Lilly And Company Antithrombotic aromatic ethers
EP1680109A4 (en) 2003-10-07 2009-05-06 Renovis Inc AMIDE DERIVATIVES AS ION CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE DERIVATIVES
ES2338881T3 (es) * 2003-10-09 2010-05-13 Millennium Pharmaceuticals, Inc. Benzamidas sustituidas con tioeter como inhibidores del factor xa.
ATE544765T1 (de) * 2003-12-22 2012-02-15 Leuven K U Res & Dev Imidazoä4,5-cüpyridinverbindungen und verfahren zur antiviralen behandlung
HRP20100675T1 (hr) 2003-12-23 2011-01-31 Astex Therapeutics Limited Derivati pirazola kao modulatori protein kinaze
US20050165015A1 (en) * 2004-01-23 2005-07-28 Ncube Mghele V. Vanilloid receptor ligands and their use in treatments
AU2005214132B9 (en) * 2004-02-18 2009-06-25 Astrazeneca Ab Benzamide derivatives and their use as glucokinae activating agents
CA2554686A1 (en) * 2004-02-18 2005-09-01 Astrazeneca Ab Compounds
US7253204B2 (en) * 2004-03-26 2007-08-07 Methylgene Inc. Inhibitors of histone deacetylase
US7625949B2 (en) 2004-04-23 2009-12-01 Roche Palo Alto Llc Methods for treating retroviral infections
US7166738B2 (en) 2004-04-23 2007-01-23 Roche Palo Alto Llc Non-nucleoside reverse transcriptase inhibitors
TW200600086A (en) * 2004-06-05 2006-01-01 Astrazeneca Ab Chemical compound
CA2565437A1 (en) * 2004-06-18 2006-01-05 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
US7696352B2 (en) * 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
GT200500208A (es) 2004-08-03 2006-03-02 Indazoles ùtiles para tratar enfermedades cardiovasculares
ES2380709T3 (es) * 2004-09-24 2012-05-17 Astrazeneca Ab Derivados de bencimidazol, composiciones que los contienen, su preparación y usos
GB0422556D0 (en) * 2004-10-11 2004-11-10 Syngenta Participations Ag Novel insecticides
MX2007004560A (es) 2004-10-16 2007-06-08 Astrazeneca Ab Proceso para hacer compuestos de fenoxi benzamida.
GB0423044D0 (en) * 2004-10-16 2004-11-17 Astrazeneca Ab Compounds
GB0423043D0 (en) * 2004-10-16 2004-11-17 Astrazeneca Ab Compounds
AU2005299771A1 (en) 2004-10-21 2006-05-04 High Point Pharmaceuticals, Llc Bissulfonamide compounds as agonists of GalR1, compositions, and methods of use
KR100884146B1 (ko) 2004-11-03 2009-02-17 에프. 호프만-라 로슈 아게 다이카복스아마이드 유도체 및 인자 Ｘａ 억제제로서의이의 용도
ATE457302T1 (de) 2004-11-24 2010-02-15 Lilly Co Eli Aromatische etherderivate als thrombin-hemmer
WO2006057868A1 (en) * 2004-11-29 2006-06-01 Eli Lilly And Company Antithrombotic diamides
EP1824831A2 (en) 2004-12-16 2007-08-29 Takeda San Diego, Inc. Histone deacetylase inhibitors
JP2008524335A (ja) * 2004-12-21 2008-07-10 ギリアド サイエンシズ， インコーポレイテッド イミダゾ［４，５−ｃ］ピリジン化合物および抗ウイルス処置法
EP1833819A1 (en) 2004-12-30 2007-09-19 Astex Therapeutics Limited Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases
NZ556546A (en) 2005-01-07 2011-02-25 Synta Pharmaceuticals Corp Compounds for inflammation and immune-related uses
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
JP5475235B2 (ja) 2005-01-21 2014-04-16 アステックス・セラピューティクス・リミテッド 医薬化合物
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
CN101146532B (zh) 2005-01-21 2012-05-09 阿斯泰克斯治疗有限公司 药物化合物
EP1847527A4 (en) * 2005-02-02 2009-04-08 Ajinomoto Kk NEW BENZAMIDINE DERIVATIVE
US7576099B2 (en) 2005-02-28 2009-08-18 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
DE602006009231D1 (de) 2005-03-10 2009-10-29 Pfizer Substituierte n-sulfonylaminophenylethyl-2-phenoxyacetamidverbindungen
US7264402B2 (en) * 2005-03-10 2007-09-04 Corning Cable Systems Llc Multi-fiber optic receptacle and plug assembly
US7642253B2 (en) 2005-05-11 2010-01-05 Takeda San Diego, Inc. Histone deacetylase inhibitors
EP1891069A1 (en) * 2005-05-24 2008-02-27 AstraZeneca AB 2-phenyl substituted imidazol [4,5b]pyridine/ pyrazine and purine derivatives as glucokinase modulators
TW200714597A (en) * 2005-05-27 2007-04-16 Astrazeneca Ab Chemical compounds
JP2008546751A (ja) 2005-06-22 2008-12-25 アステックス・セラピューティクス・リミテッド 医薬組成物
EP1933832A2 (en) 2005-06-23 2008-06-25 Astex Therapeutics Limited Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators
JP2009500442A (ja) * 2005-07-09 2009-01-08 アストラゼネカ アクチボラグ ２型糖尿病を処置するためのグルコキナーゼのモジュレーターとしての２−ヘテロシクリルオキシベンゾイルアミノヘテロシクリル化合物
KR20110084339A (ko) 2005-07-09 2011-07-21 아스트라제네카 아베 당뇨병 치료에 있어 ｇｌｋ 활성화제로서 사용하기 위한 헤테로아릴 벤즈아미드 유도체
EP2027113A1 (en) * 2005-07-09 2009-02-25 AstraZeneca AB Heteroaryl benzamide derivatives for use as glk activators in the treatment of diabetes
AU2006270322A1 (en) * 2005-07-14 2007-01-25 Takeda San Diego, Inc. Histone deacetylase inhibitors
US9202182B2 (en) * 2005-08-11 2015-12-01 International Business Machines Corporation Method and system for analyzing business architecture
AU2006290442B2 (en) 2005-09-16 2010-07-29 Arrow Therapeutics Limited Biphenyl derivatives and their use in treating hepatitis C
AU2006303368B2 (en) 2005-10-19 2011-05-26 F. Hoffmann-La Roche Ag Non-Nucleoside Reverse Transcriptase Inhibitors
RU2440986C2 (ru) * 2005-11-08 2012-01-27 Милленниум Фамэсьютикэлс, Инк. СОЛЬ ИНГИБИТОРА ФАКТОРА Ха, СПОСОБ ЕЕ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ЕЕ ОСНОВЕ, СОСТОЯЩИЕ ИЗ НАЗВАННОЙ КОМПОЗИЦИИ ТАБЛЕТКА, КАПСУЛА И ЛЕПЕШКА, СПОСОБ ЛЕЧЕНИЯ ТРОМБОЗА И СПОСОБ ИНГИБИРОВАНИЯ КОАГУЛЯЦИИ ОБРАЗЦОВ КРОВИ
TW200738621A (en) * 2005-11-28 2007-10-16 Astrazeneca Ab Chemical process
US8399442B2 (en) 2005-12-30 2013-03-19 Astex Therapeutics Limited Pharmaceutical compounds
JP2009525955A (ja) * 2006-01-13 2009-07-16 タケダ サン ディエゴ インコーポレイテッド ヒストンデアセチラーゼ阻害剤
JP2009528354A (ja) 2006-02-28 2009-08-06 メルク エンド カムパニー インコーポレーテッド ヒストン脱アセチル化酵素のインヒビター
TW200745049A (en) * 2006-03-23 2007-12-16 Astrazeneca Ab New crystalline forms
WO2007112367A2 (en) * 2006-03-27 2007-10-04 Portola Pharmaceuticals, Inc. Potassium channel modulators and platelet procoagulant activity
TW200808709A (en) 2006-03-31 2008-02-16 Glaxo Group Ltd Novel compounds
CN101466670B (zh) * 2006-04-07 2013-04-17 梅特希尔基因公司 组蛋白脱乙酰酶抑制剂
TW200808769A (en) * 2006-04-18 2008-02-16 Astrazeneca Ab Therapeutic compounds
EA015942B1 (ru) 2006-05-05 2011-12-30 Милленниум Фамэсьютикэлс, Инк. Замещенные имидазолы, композиция на их основе, способ профилактики или лечения нежелательного тромбообразования с их помощью и способ ингибирования коагуляции образцов крови
WO2008001101A2 (en) * 2006-06-29 2008-01-03 Astex Therapeutics Limited Pharmaceutical combinations
WO2008001115A2 (en) 2006-06-29 2008-01-03 Astex Therapeutics Limited Pharmaceutical combinations of 1-cyclopropyl-3- [3- (5-m0rphoolin-4-ylmethyl-1h-benzoimidazol-2-yl) -lh-1-pyrazol- 4-yl] -urea
ES2339298T3 (es) * 2006-07-07 2010-05-18 Gilead Sciences, Inc. Compuesto de piridazina novedoso y uso del mismo.
TW200825063A (en) * 2006-10-23 2008-06-16 Astrazeneca Ab Chemical compounds
CL2007003061A1 (es) * 2006-10-26 2008-08-01 Astrazeneca Ab Compuestos derivados de 3,5-dioxi-benzamida; proceso de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar una enfermedad mediada a traves de glk, tal como la diabetes tipo 2.
ES2550057T3 (es) 2006-11-02 2015-11-04 Millennium Pharmaceuticals, Inc. Métodos para sintetizar sales farmacéuticas de un inhibidor del Factor Xa
MX2009004314A (es) * 2006-11-13 2009-05-05 Pfizer Prod Inc Diaril, dipiridinil y arilpiridinilderivados y usos de los mismos.
RU2452484C2 (ru) * 2006-12-08 2012-06-10 Милленниум Фармасьютикалз, Инк. Стандартные лекарственные препараты и способы лечения тромбоза пероральным введением ингибитора фактора ха
WO2008075073A1 (en) * 2006-12-21 2008-06-26 Astrazeneca Ab Novel crystalline compound useful as glk activator
WO2008086226A2 (en) * 2007-01-05 2008-07-17 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
US7816324B2 (en) 2007-03-13 2010-10-19 Board Of Regents, The University Of Texas System Composition and method for the treatment of diseases affected by a peptide receptor
GB0704932D0 (en) 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
KR101473207B1 (ko) * 2007-04-13 2014-12-16 밀레니엄 파머슈티컬스 인코퍼레이티드 Ｘａ 인자 억제제로서 작용하는 화합물과의 병용 항응고 요법
NZ581324A (en) * 2007-05-02 2012-05-25 Portola Pharm Inc Combination therapy with a compound acting as a platelet adp receptor inhibitor
UA99466C2 (en) 2007-07-06 2012-08-27 Гилиад Сайенсиз, Инк. Crystalline pyridazine compound
PL3078743T3 (pl) 2007-09-28 2020-11-02 Portola Pharmaceuticals, Inc. Antidotum dla inhibitorów czynnika XA i sposoby ich stosowania
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
EP2324028A2 (en) 2008-08-04 2011-05-25 AstraZeneca AB Therapeutic agents 414
NZ592837A (en) 2008-11-14 2012-10-26 Portola Pharm Inc Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents
UA106740C2 (uk) * 2009-01-30 2014-10-10 Глаксосмітклайн Ллс Кристалічний гідрохлорид n-{(1s)-2-аміно-1-[(3-фторфеніл)метил]етил}-5-хлор-4-(4-хлор-1-метил-1h-піразол-5-іл)-2-тіофенкарбоксаміду
GB0902434D0 (en) * 2009-02-13 2009-04-01 Astrazeneca Ab Chemical process
GB0902406D0 (en) * 2009-02-13 2009-04-01 Astrazeneca Ab Crystalline polymorphic form
MX346801B (es) 2009-03-13 2017-03-31 Agios Pharmaceuticals Inc Métodos y composiciones para trastornos relacionados con la proliferación celular.
ES2607935T3 (es) 2009-03-30 2017-04-04 Portola Pharmaceuticals, Inc. Antídotos para inhibidores del factor Xa y procedimientos de uso de los mismos
JP5756457B2 (ja) 2009-04-06 2015-07-29 アジオス ファーマシューティカルズ， インコーポレイテッド ピルビン酸キナーゼｍ２調節剤、治療組成物および関連する使用方法
AR076221A1 (es) * 2009-04-09 2011-05-26 Astrazeneca Ab Derivado de pirazol [4,5-e] pirimidina y su uso para tratar diabetes y obesidad
WO2010116177A1 (en) 2009-04-09 2010-10-14 Astrazeneca Ab A pyrazolo [4,5-e] pyrimidine derivative and its use to treat diabetes and obesity
SG177434A1 (en) 2009-06-29 2012-02-28 Agios Pharmaceuticals Inc Therapeutic compounds and compositions
ES2605801T3 (es) 2009-07-15 2017-03-16 Portola Pharmaceuticals, Inc. Formulación de dosis unitaria de antídoto para inhibidores del factor Xa para su uso en la prevención de la hemorragia
US20110086853A1 (en) * 2009-10-08 2011-04-14 William Brown Therapeutic Compounds
WO2011050210A1 (en) 2009-10-21 2011-04-28 Agios Pharmaceuticals, Inc. Methods and compositions for cell-proliferation-related disorders
US8742120B2 (en) * 2009-12-17 2014-06-03 Millennium Pharmaceuticals, Inc. Methods of preparing factor xa inhibitors and salts thereof
WO2011084519A1 (en) 2009-12-17 2011-07-14 Millennium Pharmaceuticals, Inc. Methods of synthesizing factor xa inhibitors
WO2011084652A2 (en) 2009-12-17 2011-07-14 Millennium Pharmaceuticals, Inc. Salts and crystalline forms of a factor xa inhibitor
EA015918B1 (ru) * 2010-03-03 2011-12-30 Дмитрий Геннадьевич ТОВБИН УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА Xa
MX2012013855A (es) 2010-05-28 2013-04-08 Univ Texas Compuestos de oligobenzamida y su uso.
EP2590656B1 (en) 2010-07-07 2017-11-15 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
EP2590965B1 (en) 2010-07-07 2016-04-20 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
EP2590655B1 (en) 2010-07-07 2015-06-24 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
WO2012006477A1 (en) 2010-07-07 2012-01-12 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
TW201221128A (en) 2010-09-01 2012-06-01 Portola Pharm Inc Crystalline forms of a factor Xa inhibitor
TW201240664A (en) 2010-09-01 2012-10-16 Portola Pharm Inc Methods and formulations of treating thrombosis with betrixaban and a P-glycoprotein inhibitor
WO2012083246A1 (en) 2010-12-17 2012-06-21 Agios Pharmaceuticals, Inc. Novel n- (4- (azetidine - 1 - carbonyl) phenyl) - (hetero - ) arylsulfonamide derivatives as pyruvate kinase m2 (pmk2) modulators
MX336022B (es) 2010-12-21 2016-01-06 Agios Pharmaceuticals Inc Activadores de pkm2 bicíclicos.
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
CN103619883A (zh) 2011-01-19 2014-03-05 拜耳知识产权有限责任公司 凝血因子抑制剂的结合蛋白
GB201104267D0 (en) 2011-03-14 2011-04-27 Cancer Rec Tech Ltd Pyrrolopyridineamino derivatives
PT2704721T (pt) 2011-05-03 2018-06-14 Agios Pharmaceuticals Inc Ativadores da piruvato-cinase para utilização em terapia
CA2834692A1 (en) 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy
CN103619170B (zh) 2011-05-04 2016-07-06 默沙东公司 含有氨基-吡啶的脾酪氨酸激酶(syk)抑制剂
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
CN102827170A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
WO2013033370A1 (en) 2011-08-31 2013-03-07 Portola Pharmaceuticals, Inc. Prevention and treatment of thrombosis in medically ill patients
EP2578582A1 (en) 2011-10-03 2013-04-10 Respivert Limited 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors
EP2763984B1 (en) 2011-10-03 2016-04-20 Respivert Limited 1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 map kinase inhibitors
WO2013078277A1 (en) 2011-11-23 2013-05-30 The Board Of Regents Of The University Of Texas System Oligo-benzamide compounds and their use in treating cancers
WO2013078288A1 (en) 2011-11-23 2013-05-30 The Board Of Regents Of The University Of Texas System Oligo-benzamide compounds for use in treating cancers
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
US9296701B2 (en) 2012-04-24 2016-03-29 Vertex Pharmaceuticals Incorporated DNA-PK inhibitors
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
GB201216018D0 (en) 2012-09-07 2012-10-24 Cancer Rec Tech Ltd Pharmacologically active compounds
CA2885259A1 (en) 2012-10-04 2014-04-10 Pfizer Limited Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors
US20140346397A1 (en) 2012-12-27 2014-11-27 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
US9200268B2 (en) 2012-12-27 2015-12-01 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
FR3000895B1 (fr) 2013-01-11 2017-02-24 Laboratoire Francais Du Fractionnement Et Des Biotechnologies Sa Utilisation d'antidotes d'inhibiteurs de la coagulation indiques dans la prevention ou le traitement de pathologies thromboemboliques
JP6360878B2 (ja) 2013-03-12 2018-07-18 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ｄｎａ−ｐｋ阻害剤
US20160016934A1 (en) 2013-03-14 2016-01-21 Respivert Limited Kinase inhibitors
WO2015003360A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
WO2015006591A1 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. 2,4- or 4,6-diaminopyrimidine compounds as idh2 mutants inhibitors for the treatment of cancer
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
EA201300843A1 (ru) * 2013-08-01 2015-04-30 Арсений Валерьевич Айбушев Карбамоилфенильные производные для остановки, предотвращения и профилактики кровотечений или усиления системы гемостаза
GB201314452D0 (en) 2013-08-13 2013-09-25 Ostara Biomedical Ltd Embryo implantation
DK3054936T5 (da) 2013-10-10 2024-03-18 Eastern Virginia Medical School 4-((2-hydroxy-3-methoxybenzyl)amino) benzensulfonamid derivater som 12-lipoxygenase inhibitorer
SI3057953T1 (sl) 2013-10-17 2018-12-31 Vertex Pharmaceuticals Incorporated Ko-kristali(s)-n-metil-8-(1-((2'-metil-(4,5'-bipimiridin)-6-il)amino) propan-2-il)kinolin-4-karboksamida in njegovi devterirani derivati kot inhibitorji dna-pk
US9636298B2 (en) 2014-01-17 2017-05-02 Methylgene Inc. Prodrugs of compounds that enhance antifungal activity and compositions of said prodrugs
TWI664967B (zh) 2014-02-14 2019-07-11 英商瑞斯比維特有限公司 新穎化合物（一）
UA121211C2 (uk) 2014-03-14 2020-04-27 Аджіос Фармасьютикалз, Інк. Фармацевтична композиція, що містить тверду дисперсію, та спосіб лікування гострої мієлогенної/мієлоїдної лейкемії (гмл)
DE102014108210A1 (de) 2014-06-11 2015-12-17 Dietrich Gulba Rodentizid
CN107073082B (zh) 2014-08-20 2021-04-30 博尔托拉制药公司 Xa因子解毒剂的冻干制剂
GB201501302D0 (en) 2015-01-27 2015-03-11 Ostara Biomedical Ltd Embryo implantation
SI3307271T1 (sl) 2015-06-11 2023-11-30 Agios Pharmaceuticals, Inc. Postopki za uporabo aktivatorjev piruvat kinaze
AU2016295693B2 (en) 2015-07-17 2020-05-21 Sunshine Lake Pharma Co., Ltd. Substituted quinazoline compounds and preparation and uses thereof
GB201514021D0 (en) 2015-08-07 2015-09-23 Arner Elias Set Jeno Novel Pyridines and their use in the treatment of cancer
GB201517523D0 (en) 2015-10-05 2015-11-18 Ostara Biomedical Ltd Methods and compositions for managing reproduction
DK3362066T3 (da) 2015-10-15 2021-11-22 Les Laboratoires Servier Sas Kombinationsterapi til behandling af maligniteter
MD3362065T2 (ro) 2015-10-15 2024-08-31 Servier Lab Terapie combinată care conține ivosidenib, citarabină și daunorubicina sau idarubicina pentru tratarea leucemiei acute mielogene
WO2017091757A1 (en) 2015-11-24 2017-06-01 Portola Pharmaceuticals, Inc. Isotopically enriched betrixaban
TWI739783B (zh) 2016-01-22 2021-09-21 比利時商健生藥品公司 作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物
US11001569B2 (en) 2016-01-22 2021-05-11 Janssen Pharmaceutica Nv 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors
WO2017147522A1 (en) 2016-02-24 2017-08-31 Portola Pharmaceuticals, Inc. Lyophilized formulations for factor xa antidote
RU2698202C2 (ru) * 2016-06-01 2019-08-23 Закрытое акционерное общество "ФАРМА ВАМ" СПОСОБ ПОЛУЧЕНИЯ ПРЯМОГО ИНГИБИТОРА ФАКТОРА Ха
EP3472314B1 (en) 2016-06-17 2021-05-05 Alexion Pharmaceuticals, Inc. Preparation of factor xa derivatives
KR102587619B1 (ko) 2016-06-30 2023-10-11 잔센파마슈티카엔.브이. Nik 억제제로서의 시아노인돌린 유도체
CN109641882B (zh) 2016-06-30 2022-10-28 杨森制药有限公司 作为nik抑制剂的杂芳族衍生物
PE20190607A1 (es) 2016-09-02 2019-04-23 Ironwood Pharmaceuticals Inc Estimuladores de sgc
AU2017335648B2 (en) 2016-09-27 2022-02-17 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA-damaging agents and DNA-PK inhibitors
WO2018069936A1 (en) 2016-10-13 2018-04-19 Mylan Laboratories Limited Polymorphs and solid dispersion of betrixaban and methods for the preparation thereof
AU2018218518B2 (en) 2017-02-07 2022-03-17 Oblique Therapeutics Ab Sulfinylpyridines and their use in the treatment of cancer
US11168069B2 (en) 2017-02-07 2021-11-09 Oblique Therapeutics Ab Heterocyclylsulfonyl-substituted pyridines and their use in the treatment of cancer
EP3580215A1 (en) 2017-02-07 2019-12-18 Oblique Therapeutics AB Heteroarylsulfonyl-substituted pyridines and their use in the treatment of cancer
MX392900B (es) 2017-02-07 2025-03-24 Oblique Therapeutics Ab Piridinas sustituidas con hidrocarbilsulfonilo y su uso en el tratamiento del cancer
WO2018229796A2 (en) 2017-06-14 2018-12-20 Mylan Laboratories Limited A process for betrixaban hydrochloride and betrixaban maleate salt
CN111065383A (zh) 2017-07-11 2020-04-24 沃泰克斯药物股份有限公司 用作钠通道调节剂的羧酰胺
KR102717600B1 (ko) 2017-10-06 2024-10-15 포르마 세라퓨틱스 인크. 유비퀴틴 특이적 펩티다제 30의 억제
MX387232B (es) 2017-10-27 2025-03-18 Boehringer Ingelheim Int Derivados de piridincarbonilo y usos terapéuticos de los mismos como inhibidores de trpc6.
CA3098283C (en) 2018-04-26 2023-05-23 Pfizer Inc. 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors
GB201807014D0 (en) 2018-04-30 2018-06-13 Univ Leeds Innovations Ltd Factor xlla inhibitors
CN112513036B (zh) 2018-05-17 2024-05-24 福马治疗有限公司 用作泛素特异性肽酶30抑制剂的稠合双环化合物
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
GB201810092D0 (en) 2018-06-20 2018-08-08 Ctxt Pty Ltd Compounds
GB201810581D0 (en) 2018-06-28 2018-08-15 Ctxt Pty Ltd Compounds
ES2945834T3 (es) 2018-10-05 2023-07-07 Forma Therapeutics Inc Pirrolinas fusionadas que actúan como inhibidores de la proteasa 30 específica de ubiquitina (USP30)
WO2020146682A1 (en) 2019-01-10 2020-07-16 Vertex Pharmaceuticals Incorporated Carboxamides as modulators of sodium channels
US12440481B2 (en) 2019-01-10 2025-10-14 Vertex Pharmaceuticals Incorporated Esters and carbamates as modulators of sodium channels
IL288802B2 (en) 2019-06-18 2025-08-01 Pfizer Benzisoxazole sulfonamide derivatives
LT4069691T (lt) 2019-12-06 2024-12-10 Vertex Pharmaceuticals Incorporated Pakeistieji tetrahidrofuranai kaip natrio kanalų moduliatoriai
TWI775313B (zh) 2020-02-18 2022-08-21 美商基利科學股份有限公司 抗病毒化合物
TWI883391B (zh) 2020-02-18 2025-05-11 美商基利科學股份有限公司 抗病毒化合物
CN115135383B (zh) 2020-02-18 2024-06-11 吉利德科学公司 抗病毒化合物
WO2022211680A1 (ru) * 2021-03-30 2022-10-06 Общество С Ограниченной Ответственностью "Фармадиол" Способ получения антикоагулянта n-(5-хлорпиридин-2-ил)-2-({4-[этан-имидоил(метил)амино]бензоил}амино)-5-метилбензамид гидрохлорида
EP4070658A1 (de) 2021-04-06 2022-10-12 BIORoxx GmbH Verwendung von blutgerinnungshemmenden verbindungen als rodentizide
JP7688152B2 (ja) 2021-04-16 2025-06-03 ギリアード サイエンシーズ， インコーポレイテッド アミドを使用してカルバヌクレオシドを調製する方法
GB202107722D0 (en) 2021-05-28 2021-07-14 Lunac Therapeutics Ltd Factor XIIA Inhibitors
DK4347031T3 (da) 2021-06-04 2025-12-01 Vertex Pharma N-(hydroxyalkyl-(hetero)aryl)-tetrahydrofuran-carboxamider som modulatorer af natriumkanaler
KR20240049311A (ko) 2021-08-18 2024-04-16 길리애드 사이언시즈, 인코포레이티드 인지질 화합물 및 이의 제조 및 사용 방법
WO2024127350A1 (en) 2022-12-16 2024-06-20 Astrazeneca Ab 2,6,9-trisubstituted purines
NL2036011B1 (en) 2023-10-12 2025-04-30 Synapse Res Institute Molecules for reversing anti-coagulant activity of direct oral anticoagulants

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2095619A (en) 1937-10-12 Aryl oxides
CH428747A (de) * 1961-09-11 1967-01-31 Wander Ag Dr A Verfahren zur Herstellung neuer Harnstoff- und Thioharnstoffderivate
GB1047245A (da) * 1963-02-15
JPS6033389B2 (ja) * 1979-02-22 1985-08-02 日産化学工業株式会社 複素環エ−テル系フェノシキ脂肪酸誘導体、その製造法および該誘導体を含有する除草剤
DE3207033C2 (de) 1981-02-27 1984-09-13 Torii & Co., Ltd., Tokyo Amidinverbindungen, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Mittel
US4500714A (en) * 1981-10-15 1985-02-19 Chugai Seiyaku Kabushiki Kaisha 3-Substituted-ureido-N-pyridyl benzamides
US4588587A (en) 1983-03-01 1986-05-13 Pennsylvania Hospital Method of treatment to inhibit metastasis
JPS59181257A (ja) 1983-03-31 1984-10-15 Chugai Pharmaceut Co Ltd ウレイドベンズアミド誘導体
JPS648675A (en) 1987-06-30 1989-01-12 Mitsubishi Electric Corp Formation of schottky gate
JP2668231B2 (ja) 1987-12-29 1997-10-27 大日精化工業株式会社 電子写真感光体
AU606808B2 (en) * 1988-06-29 1991-02-14 Otsuka Pharmaceutical Factory, Inc. Arylcarboxamide substituted by alkylphosphonates, process for preparing the same and a pharmaceutical composition containing the same
JPH0418675A (ja) 1990-05-11 1992-01-22 Ricoh Co Ltd 回路図入力装置
GB9816837D0 (en) * 1998-08-04 1998-09-30 Zeneca Ltd Amide derivatives
ZA928276B (en) 1991-10-31 1993-05-06 Daiichi Seiyaku Co Aromatic amidine derivates and salts thereof.
US5612360A (en) 1992-06-03 1997-03-18 Eli Lilly And Company Angiotensin II antagonists
US5883077A (en) 1992-12-15 1999-03-16 Corvas International, Inc. Inhibitors of factor Xa
US5610335A (en) 1993-05-26 1997-03-11 Cornell Research Foundation Microelectromechanical lateral accelerometer
PT798295E (pt) 1994-12-02 2003-07-31 Yamanouchi Pharma Co Ltd Novo derivado de amidinonaftilo ou sal deste
ES2208737T3 (es) 1995-03-10 2004-06-16 Berlex Laboratories, Inc. Derivados de benzamidina, su preparacion y su utilizacion como anticoagulantes.
EP0742208A1 (en) 1995-05-05 1996-11-13 Grelan Pharmaceutical Co., Ltd. 2-Ureido-benzamide derivatives
US5849759A (en) 1995-12-08 1998-12-15 Berlex Laboratories, Inc. Naphthyl-substituted benzimidazole derivatives as anti-coagulants
US5994375A (en) 1996-02-12 1999-11-30 Berlex Laboratories, Inc. Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants
WO1998006694A1 (en) 1996-08-16 1998-02-19 Du Pont Pharmaceuticals Company Amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof
EP0934068A1 (en) 1996-09-09 1999-08-11 Smithkline Beecham Corporation Compounds and methods
ES2331860T3 (es) 1996-12-23 2010-01-18 Bristol-Myers Squibb Pharma Company Compuestos heteroaromaticos que contienen nitrogeno como inhibidores del factor xa.
EP0946528B1 (en) * 1996-12-23 2003-04-09 Bristol-Myers Squibb Pharma Company OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS
EP0993448A1 (en) 1997-06-19 2000-04-19 The Du Pont Merck Pharmaceutical Company (AMIDINO)6-MEMBERED AROMATICS AS FACTOR Xa INHIBITORS
IL133625A0 (en) * 1997-06-26 2001-04-30 Lilly Co Eli Antithrombotic agents
ES2241151T3 (es) 1997-06-26 2005-10-16 Eli Lilly And Company Agentes antitromboticos.
ES2248911T3 (es) 1997-06-26 2006-03-16 Eli Lilly And Company Agentes antitromboticos.
CA2294042A1 (en) 1997-06-26 1999-01-07 David Kent Herron Antithrombotic agents
WO1999007379A1 (en) 1997-08-11 1999-02-18 Boehringer Ingelheim Pharmaceuticals, Inc. 5,6-HETEROARYL-DIPYRIDO[2,3-b:3',2'-f]AZEPINES AND THEIR USE IN THE PREVENTION OR TREATMENT OF HIV INFECTION
WO1999010316A1 (en) 1997-08-27 1999-03-04 Kissei Pharmaceutical Co., Ltd. 3-amidinoaniline derivatives, activated blood coagulation factor x inhibitors, and intermediates for producing both
US6140351A (en) 1997-12-19 2000-10-31 Berlex Laboratories, Inc. Ortho-anthranilamide derivatives as anti-coagulants
DK1040108T3 (da) 1997-12-19 2004-05-24 Schering Ag Orthoanthranilamidderivater som antikoagulanter
EP0937711A1 (de) 1998-02-18 1999-08-25 Roche Diagnostics GmbH Neue Thiobenzamide, Verfahren zu ihrer Herstellung sowie diese enthaltende Arzneimittel
JPH11302177A (ja) 1998-04-27 1999-11-02 Otsuka Pharmaceut Factory Inc 腎炎治療剤
EP1137633A2 (en) 1998-12-09 2001-10-04 American Home Products Corporation Acetamide and substituted acetamide-containing thiourea inhibitors of herpes viruses
ATE272052T1 (de) 1998-12-09 2004-08-15 Wyeth Corp Thioharnstoff-inhibitoren von herpes-virus
WO2000034269A1 (en) 1998-12-09 2000-06-15 American Home Products Corporation Thiourea inhibitors of herpes viruses
KR20010086090A (ko) 1998-12-09 2001-09-07 이곤 이 버그 헤르페스 바이러스의 티오우레아 억제제
ATE267824T1 (de) 1998-12-09 2004-06-15 Wyeth Corp Alpha-methylbenzyl-enthaltende thioharnstoffe als inhibitoren von herpes-viren mit einer phenylenediamingruppe
CZ20012063A3 (cs) 1998-12-09 2001-10-17 American Home Products Corporation Thiomočovinové sloučeniny obsahující heterocyklický karboxamid a substituovanou fenylendiaminovou skupinu jako inhibitory herpes virů
BR9916046A (pt) 1998-12-09 2001-10-02 American Home Prod Composto, composição farmacêutica, e, processos para inibir a replicação de um vìrus herpes e para tratamento de um paciente que sofra de uma infecção do vìrus herpes
WO2000039118A1 (en) 1998-12-23 2000-07-06 Eli Lilly And Company Aromatic amides
US6844367B1 (en) 1999-09-17 2005-01-18 Millennium Pharmaceuticals, Inc. Benzamides and related inhibitors of factor Xa
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
US6720317B1 (en) 1999-09-17 2004-04-13 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
CA2385592C (en) 1999-09-17 2011-01-11 Bing-Yan Zhu Benzamides and related inhibitors of factor xa
ATE311366T1 (de) * 2000-02-29 2005-12-15 Millennium Pharm Inc Benzamide und ähnliche inhibitoren vom faktor xa
AU776053B2 (en) * 2000-03-31 2004-08-26 Astellas Pharma Inc. Diazepan derivatives or salts thereof
US6373515B1 (en) * 2000-08-09 2002-04-16 Hewlett-Packard Company Variable resolution transition placement device
US7312235B2 (en) 2001-03-30 2007-12-25 Millennium Pharmaceuticals, Inc. Benzamide inhibitors of factor Xa
UA75691C2 (en) * 2001-07-31 2006-05-15 Univ Wayne State Quinoline derivatives, use thereof as antitumor drugs, composition based thereon and therapeutical method for treatment of cancer
ES2338881T3 (es) 2003-10-09 2010-05-13 Millennium Pharmaceuticals, Inc. Benzamidas sustituidas con tioeter como inhibidores del factor xa.
CA2565437A1 (en) 2004-06-18 2006-01-05 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
US7696352B2 (en) 2004-06-18 2010-04-13 Millennium Pharmaceuticals, Inc. Factor Xa inhibitors
RU2440986C2 (ru) 2005-11-08 2012-01-27 Милленниум Фамэсьютикэлс, Инк. СОЛЬ ИНГИБИТОРА ФАКТОРА Ха, СПОСОБ ЕЕ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ЕЕ ОСНОВЕ, СОСТОЯЩИЕ ИЗ НАЗВАННОЙ КОМПОЗИЦИИ ТАБЛЕТКА, КАПСУЛА И ЛЕПЕШКА, СПОСОБ ЛЕЧЕНИЯ ТРОМБОЗА И СПОСОБ ИНГИБИРОВАНИЯ КОАГУЛЯЦИИ ОБРАЗЦОВ КРОВИ
WO2007112367A2 (en) 2006-03-27 2007-10-04 Portola Pharmaceuticals, Inc. Potassium channel modulators and platelet procoagulant activity
EA015942B1 (ru) 2006-05-05 2011-12-30 Милленниум Фамэсьютикэлс, Инк. Замещенные имидазолы, композиция на их основе, способ профилактики или лечения нежелательного тромбообразования с их помощью и способ ингибирования коагуляции образцов крови
RU2452484C2 (ru) 2006-12-08 2012-06-10 Милленниум Фармасьютикалз, Инк. Стандартные лекарственные препараты и способы лечения тромбоза пероральным введением ингибитора фактора ха
WO2008086226A2 (en) 2007-01-05 2008-07-17 Millennium Pharmaceuticals, Inc. Factor xa inhibitors
KR101473207B1 (ko) 2007-04-13 2014-12-16 밀레니엄 파머슈티컬스 인코퍼레이티드 Ｘａ 인자 억제제로서 작용하는 화합물과의 병용 항응고 요법
NZ581324A (en) 2007-05-02 2012-05-25 Portola Pharm Inc Combination therapy with a compound acting as a platelet adp receptor inhibitor

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