PE20081775A1 - Compuestos macrociclicos como inhibidores del factor viia - Google Patents
Compuestos macrociclicos como inhibidores del factor viiaInfo
- Publication number
- PE20081775A1 PE20081775A1 PE2007001814A PE2007001814A PE20081775A1 PE 20081775 A1 PE20081775 A1 PE 20081775A1 PE 2007001814 A PE2007001814 A PE 2007001814A PE 2007001814 A PE2007001814 A PE 2007001814A PE 20081775 A1 PE20081775 A1 PE 20081775A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- phenyl
- ring
- compounds
- factor viia
- Prior art date
Links
- 229940012414 factor viia Drugs 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 150000002678 macrocyclic compounds Chemical class 0.000 title 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- VUWZPRWSIVNGKG-UHFFFAOYSA-N fluoromethane Chemical compound F[CH2] VUWZPRWSIVNGKG-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/12—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
- C07D255/04—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 condensed with carbocyclic rings or ring systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
SE REFIERE A COMPUESTOS MACROCICLICOS DE FORMULA (I) DONDE EL ANILLO A ES FENILO O PIRIDILO; EL ANILLO B ES FENILO O PIRIDILO; Z1 Y Z2 SON CADA UNO C O N; Z3 ES -C(=O)-, -C(=NH)-, -SO2-, ENTRE OTROS; Z4 ES C(O), CR20R20 O SO2, DONDE R20 ES H, CF3, HALOALQUILO(C1-C4), ENTRE OTROS; EL ANILLO D ES FENILO O UN HETEROARILO DE 5 A 6 MIEMBROS; M ES -CONH-, -SO2NH-, -NHCO- O -NHSO2-; L ES -XC(R12R13)-, C(R12R13)Y-, -XC(R12R13)Y-, ENTRE OTROS, DONDE X ES O, S(O)p O NR16; Y ES O U NR16a, EN DONDE R16 Y R16a SON CADA UNO H, ALQUILO(C1-C6), CICLOALQUILO(C3-C6), FENILO, ENTRE OTROS; p ES DE 0 A 2; R12 Y R13 SON CADA UNO H, F, CF3, CN, NO2, ENTRE OTROS; R1 ES H, F, Br, ALQUENILO(C2-C4), ENTRE OTROS; R2 ES H, F, I, FLUOROALQUILO(C1-C4), ENTRE OTROS; R3 ES H, F, ALQUILO(C1-C6), ALQUINILO(C2-C4), ENTRE OTROS; R4 ES H, F, Cl, Br, I O ALQUILO(C1-C4); R5 ES H, ALQUILO(C1-C6), ALQUENILO(C2-C4), ENTRE OTROS; R6 ES H, ALQUILO(C1-C6), ALQUINILO(C2-C4), ENTRE OTROS; R7 ES H O ALQUILO(C1-C6); R8 ES H, F, CN, CH2F, ENTRE OTROS; R9, R10 Y R11 SON CADA UNO H, F, Cl, Br, I, ALQUILO(C1-C4) O ALCOXI(C1-C4); W ES O, S O NRh, DONDE Rh ES H O ALQUILO(C1-C3). SON COMPUESTOS PREFERIDOS: SAL DEL ACIDO (R)-4-METIL-2-(3-OXO-2,3-DIHIDRO-1H-ISOINDOL-5-ILAMINO)-7-(PROPANO-2-SULFONIL)-4,11-DIAZA-TRICICLO[14.2.2.16,10]HENICOSA-1(19),6,8,10(21),16(20),17-HEXAENO-3,12-DIONA TRIFLUOROACETICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES SELECTIVOS DEL FACTOR VIIa
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87086406P | 2006-12-20 | 2006-12-20 | |
| US98446007P | 2007-11-01 | 2007-11-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20081775A1 true PE20081775A1 (es) | 2008-12-18 |
Family
ID=39430763
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007001814A PE20081775A1 (es) | 2006-12-20 | 2007-12-14 | Compuestos macrociclicos como inhibidores del factor viia |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8420830B2 (es) |
| EP (1) | EP2102176A2 (es) |
| JP (1) | JP2010514681A (es) |
| AR (1) | AR064471A1 (es) |
| AU (1) | AU2007337025A1 (es) |
| CA (1) | CA2673598A1 (es) |
| CL (1) | CL2007003718A1 (es) |
| MX (1) | MX2009006689A (es) |
| NO (1) | NO20092279L (es) |
| PE (1) | PE20081775A1 (es) |
| TW (1) | TW200836735A (es) |
| WO (1) | WO2008079836A2 (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101631784A (zh) | 2006-12-20 | 2010-01-20 | 百时美施贵宝公司 | 用作抗凝血药的二环内酰胺凝血因子viia抑制剂 |
| US20110137042A1 (en) * | 2009-12-08 | 2011-06-09 | Boehringer Ingelheim International Gmbh | Process for Synthesis of Intermediates Useful for Making Substituted Indazole and Azaindazole Compounds |
| WO2011100401A1 (en) | 2010-02-11 | 2011-08-18 | Bristol-Myers Squibb Company | Macrocycles as factor xia inhibitors |
| CN102993065B (zh) * | 2011-09-13 | 2015-07-29 | 中国科学院上海药物研究所 | 含手性叔丁基亚磺酰基的α-芳基氨基酸酯类化合物、其制备方法及用途 |
| EP2766346B1 (en) | 2011-10-14 | 2017-03-29 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2797879B1 (en) * | 2011-12-27 | 2018-12-26 | Bio-Pharm Solutions Co., Ltd. | Phenyl carbamate compounds for use in alleviating or treating pain and neuropathic pain |
| EP2858977A1 (en) | 2012-06-08 | 2015-04-15 | Bristol-Myers Squibb Company | Macrocyclic factor viia inhibitors |
| BR112015002081A2 (pt) * | 2012-08-03 | 2017-07-04 | Bristol Myers Squibb Co | di-hidropiridona p1 como inibidores de fator xia |
| SMT201700003T1 (it) * | 2012-08-03 | 2017-03-08 | Bristol Myers Squibb Co | DlIDROPIRIDONI COME INIBITORI DEL FATTORE XIA |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| US9920034B2 (en) | 2012-10-12 | 2018-03-20 | Bristol-Myers Squibb Company | Crystalline forms of a factor XIa inhibitor |
| US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| ES2712699T3 (es) | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
| US9657006B2 (en) | 2013-06-13 | 2017-05-23 | Bristol-Myers Squibb Company | Macrocyclic factor VIIa inhibitors |
| WO2015116885A1 (en) | 2014-01-31 | 2015-08-06 | Bristol-Myers Squibb Company | Macrocycles with aromatic p2' groups as factor xia inhibitors |
| NO2760821T3 (es) | 2014-01-31 | 2018-03-10 | ||
| ES2714283T3 (es) | 2014-09-04 | 2019-05-28 | Bristol Myers Squibb Co | Macrociclos de diamida que son inhibidores de FXIa |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| EP3072943B1 (en) | 2015-03-26 | 2018-05-02 | Idemitsu Kosan Co., Ltd. | Dibenzofuran/carbazole-substituted benzonitriles |
| JP6816103B2 (ja) * | 2015-07-29 | 2021-01-20 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 非芳香族性P2’基を担持する新規大員環の第XIa因子阻害剤 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0028489B1 (en) | 1979-11-05 | 1983-10-05 | Beecham Group Plc | Enzyme derivatives, and their preparation |
| US5023236A (en) | 1988-04-07 | 1991-06-11 | Corvas, Inc. | Factor VII/VIIA active site inhibitors |
| US5843442A (en) | 1990-10-22 | 1998-12-01 | Corvas International, Inc. | Blood coagulation protein antagonists and uses therefor |
| US5866542A (en) | 1994-10-18 | 1999-02-02 | Corvas International, Inc. | Nematode-extracted anticoagulant protein |
| PE121699A1 (es) | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | Heterociclos biciclicos disustituidos como inhibidores de la trombina |
| ZA985247B (en) | 1997-06-19 | 1999-12-17 | Du Pont Merck Pharma | Guanidine mimics as factor Xa inhibitors. |
| CA2383008A1 (en) | 1999-06-14 | 2000-12-21 | Amanda Jane Lyons | Compounds |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| HUP0400651A2 (hu) * | 2000-11-07 | 2004-06-28 | Bristol-Myers Squibb Company | Szerin proteáz inhibitorokként alkalmazható savszármazékok és ezeket tartalmazó gyógyszerkészítmények |
| AR035216A1 (es) | 2000-12-01 | 2004-05-05 | Astrazeneca Ab | Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios |
| AU2002322802A1 (en) * | 2001-07-27 | 2003-02-17 | Merck And Co., Inc. | Thrombin inhibitors |
| EP1427415B1 (en) | 2001-09-21 | 2009-08-12 | Brystol-Myers Squibb Company | Lactam-containing compounds and derivatives thereof as factor xa inhibitors |
| WO2004072101A2 (en) * | 2003-02-11 | 2004-08-26 | Bristol-Myers Squibb Company | Phenylglycine derivatives useful as serine protease inhibitors |
| JP2006517589A (ja) * | 2003-02-11 | 2006-07-27 | ブリストル−マイヤーズ スクイブ カンパニー | セリンプロテアーゼ・インヒビターとして有用なベンゼンアセトアミド化合物 |
| EP1856096B1 (en) * | 2005-01-10 | 2010-09-01 | Bristol-Myers Squibb Company | Phenylglycinamide derivatives useful as anticoagulants |
| EP1866822A4 (en) * | 2005-03-03 | 2010-09-01 | Burnham Inst Medical Research | SCREENING PROCEDURE FOR PROTEIN KINASE B INHIBITORS USING VIRTUAL DOCKING APPARATUS AND COMPOSITIONS AND COMPOSITIONS DISCOVERED THEREFOR |
| US7456195B2 (en) * | 2005-06-24 | 2008-11-25 | Bristol-Myers Squibb Company | Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants |
| AR058380A1 (es) * | 2005-12-23 | 2008-01-30 | Bristol Myers Squibb Co | Inhibidores del factor viia macrociclicos utiles como anticoagulantes |
| US8044242B2 (en) | 2006-03-09 | 2011-10-25 | Bristol-Myers Squibb Company | 2-(aryloxy) acetamide factor VIIa inhibitors useful as anticoagulants |
| CN101631784A (zh) | 2006-12-20 | 2010-01-20 | 百时美施贵宝公司 | 用作抗凝血药的二环内酰胺凝血因子viia抑制剂 |
-
2007
- 2007-12-14 PE PE2007001814A patent/PE20081775A1/es not_active Application Discontinuation
- 2007-12-19 CA CA002673598A patent/CA2673598A1/en not_active Abandoned
- 2007-12-19 EP EP07869479A patent/EP2102176A2/en not_active Withdrawn
- 2007-12-19 US US12/519,376 patent/US8420830B2/en active Active
- 2007-12-19 AU AU2007337025A patent/AU2007337025A1/en not_active Abandoned
- 2007-12-19 WO PCT/US2007/088032 patent/WO2008079836A2/en active Application Filing
- 2007-12-19 CL CL200703718A patent/CL2007003718A1/es unknown
- 2007-12-19 AR ARP070105750A patent/AR064471A1/es not_active Application Discontinuation
- 2007-12-19 MX MX2009006689A patent/MX2009006689A/es not_active Application Discontinuation
- 2007-12-19 TW TW096148731A patent/TW200836735A/zh unknown
- 2007-12-19 JP JP2009543158A patent/JP2010514681A/ja not_active Withdrawn
-
2009
- 2009-06-12 NO NO20092279A patent/NO20092279L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AR064471A1 (es) | 2009-04-01 |
| WO2008079836A4 (en) | 2009-03-12 |
| US8420830B2 (en) | 2013-04-16 |
| US20100113488A1 (en) | 2010-05-06 |
| EP2102176A2 (en) | 2009-09-23 |
| NO20092279L (no) | 2009-08-31 |
| WO2008079836A2 (en) | 2008-07-03 |
| JP2010514681A (ja) | 2010-05-06 |
| MX2009006689A (es) | 2009-06-30 |
| AU2007337025A1 (en) | 2008-07-03 |
| CA2673598A1 (en) | 2008-07-03 |
| CL2007003718A1 (es) | 2008-07-11 |
| TW200836735A (en) | 2008-09-16 |
| WO2008079836A3 (en) | 2009-01-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |