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AR037676A1 - Inhibidores del factor xa y de otras proteasas de serina implicadas en la cascada de la coagulacion; composicion farmaceutica que los comprende y procedimiento para preparar compuestos de formula (i) - Google Patents

Inhibidores del factor xa y de otras proteasas de serina implicadas en la cascada de la coagulacion; composicion farmaceutica que los comprende y procedimiento para preparar compuestos de formula (i)

Info

Publication number
AR037676A1
AR037676A1 ARP020104557A ARP020104557A AR037676A1 AR 037676 A1 AR037676 A1 AR 037676A1 AR P020104557 A ARP020104557 A AR P020104557A AR P020104557 A ARP020104557 A AR P020104557A AR 037676 A1 AR037676 A1 AR 037676A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
formula
heteroaryl
haloalkyl
Prior art date
Application number
ARP020104557A
Other languages
English (en)
Original Assignee
Warner Lambert Co
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
Application filed by Warner Lambert Co filed Critical Warner Lambert Co
Publication of AR037676A1 publication Critical patent/AR037676A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D207/16—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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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/20—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
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    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
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    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
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    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
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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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
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    • C07D233/54—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
    • 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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    • C07—ORGANIC CHEMISTRY
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    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D237/14—Oxygen atoms
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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
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Pyrrole Compounds (AREA)
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  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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  • Hydrogenated Pyridines (AREA)
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Abstract

Composición farmacéutica que los comprende y procedimiento para preparar compuestos de fórmula (1), y sales farmacéuticamente aceptables de los mismos, que son útiles para tratar trastornos trombóticos: También se describen composiciones farmacéuticas que comprenden uno o más compuestos de fórmula (1), procedimientos para la preparación de compuestos de fórmula (1), e intermedios útiles para la preparación de compuestos de fórmula (1). Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable del mismo caracterizado porque: A es arilo o arilo sustituido o heteroarilo monocíclico o heteroarilo monocíclico sustituido; B es -HNCO-alquilo C1-6, -HNCO-cicloalquilo C3-7, HN-COO(alquilo C1-6), -CO-R1, cicloalquilo C3-7, heterociclilo C3-7, cicloalquenilo C4-7, heterociclilo C4-7 insaturado, arilo o heteroarilo, pudiendo estar cualquiera de ellos opcionalmente sustituidos con halo, alquilo C1-6 o haloalquilo C1-6, O-(C1-6), -CN, haloalquilo, amino, alquilamino, amidino, amido o sulfonamido; C es fenilo o heteroarilo, estando fenilo o heteroarilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre halógeno, hidroxi, -CO2R2, -COR2, -CONR2R2', alcoxi, alquilo, -CN, haloalquilo, amino, alquilamino, amidino, amido o sulfonamido; G es H, halo, alquilo C1-6, haloalquilo C1-6, hidroxialquilo C1-6, -CH2O-alquilo C1-6, -CH2-CO2-alquilo C1-6, -CH2-NR2R2' o -CH2-CONH-alquilo C1-6; W1 es una cadena de hidrocarburo saturado o insaturado, sustituido o no sustituido o una cadena de hidrocarburo-heteroátomo que tiene de 2 a 6 átomos, en la que W1 conecta el átomo de nitrógeno en la posición 1 con el átomo de carbono en la posición 2, formando un anillo de 4 a 8 miembros; R1 es alcoxi C1-6, cicloalquilo C3-7, heterocicloalquilo C3-7, cicloalquenilo C4-7, heterocicloalquenilo C4-7, arilo, heteroarilo monocíclico o -NR3R4; cada uno de R2 y R2' es independientemente H o alquilo C1-6, y R3 y R4 son independientemente H, alquilo C1-6, aralquilo, arilo, heteroarilo monocíclico, alcoxicarbonilo, aralcoxicarbonilo, -SO2-alquilo o se toman conjuntamente para formar un anillo saturado o insaturado de 3 a 7 miembros.
ARP020104557A 2001-11-29 2002-11-27 Inhibidores del factor xa y de otras proteasas de serina implicadas en la cascada de la coagulacion; composicion farmaceutica que los comprende y procedimiento para preparar compuestos de formula (i) AR037676A1 (es)

Applications Claiming Priority (2)

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US33416801P 2001-11-29 2001-11-29
US38489502P 2002-05-31 2002-05-31

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AR037676A1 true AR037676A1 (es) 2004-12-01

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ARP020104557A AR037676A1 (es) 2001-11-29 2002-11-27 Inhibidores del factor xa y de otras proteasas de serina implicadas en la cascada de la coagulacion; composicion farmaceutica que los comprende y procedimiento para preparar compuestos de formula (i)

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Families Citing this family (97)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI290136B (en) 2000-04-05 2007-11-21 Daiichi Seiyaku Co Ethylenediamine derivatives
DE10113379B4 (de) * 2001-03-20 2006-08-24 Karl Eugen Fischer Gmbh Maschinenfabrik Vorschubeinrichtung, insbesondere für Cordbänder
US7365205B2 (en) 2001-06-20 2008-04-29 Daiichi Sankyo Company, Limited Diamine derivatives
US7030141B2 (en) * 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
KR20030080810A (ko) * 2002-04-11 2003-10-17 주식회사 엘지생명과학 아미노피리도아릴 그룹을 가진 선택적 트롬빈 억제제
US20040138269A1 (en) * 2002-10-11 2004-07-15 Sugen, Inc. Substituted pyrroles as kinase inhibitors
US7205318B2 (en) 2003-03-18 2007-04-17 Bristol-Myers Squibb Company Lactam-containing cyclic diamines and derivatives as a factor Xa inhibitors
DE502004009440D1 (de) 2003-04-03 2009-06-10 Merck Patent Gmbh Pyrrolidin-1,2-dicarbonsäure-1-(phenylamid)-2-(4-(3-oxo-morpholin-4-yl)-phenylamid) derivate und verwandte verbindungen als inhibitoren des koagulationsfaktors xa zur behandlung von thromboembolischen erkrankungen
DE10329457A1 (de) * 2003-04-03 2005-01-20 Merck Patent Gmbh Ethinylprolinderivate
CN1809346A (zh) * 2003-06-18 2006-07-26 默克专利股份公司 作为凝血因子xa和viia的抑制剂用于治疗形成血栓的1－[(4－乙炔基苯基) ]－2－[(苯基)]－吡咯烷－1,2－二酰胺衍生物
WO2005032490A2 (en) 2003-10-08 2005-04-14 Bristol-Myers Squibb Company Cyclic diamines and derivatives as factor xa inhibitors
DE10358814A1 (de) * 2003-12-16 2005-07-21 Merck Patent Gmbh Prolinylarylacetamide
JPWO2005085200A1 (ja) 2004-03-05 2008-01-17 萬有製薬株式会社 ピリドン誘導体
US7550487B2 (en) * 2004-03-26 2009-06-23 Hoffmann-La Roche Inc. Pyrrolidine-3,4-dicarboxamide derivatives
DE102004014945A1 (de) * 2004-03-26 2005-10-13 Merck Patent Gmbh Prolinylderivate
DE102004016605A1 (de) * 2004-04-03 2005-10-20 Merck Patent Gmbh Thiocarbamoylproline
TWI350168B (en) 2004-05-07 2011-10-11 Incyte Corp Amido compounds and their use as pharmaceuticals
EP1768954A4 (en) 2004-06-24 2008-05-28 Incyte Corp 2-METHYLPROPANAMIDES AND THEIR USE AS PHARMACEUTICALS
DE102004045796A1 (de) * 2004-09-22 2006-03-23 Merck Patent Gmbh Arzneimittel enthaltend Carbonylverbindungen sowie deren Verwendung
DE102004047254A1 (de) * 2004-09-29 2006-04-13 Merck Patent Gmbh Carbonylverbindungen
DE102004047255A1 (de) * 2004-09-29 2006-04-13 Merck Patent Gmbh Prolinderivate
WO2006038119A1 (en) * 2004-10-08 2006-04-13 Warner-Lambert Company Llc Stereoselective synthesis of n-protected alkoxy prolines
BRPI0517964A (pt) * 2004-11-03 2008-10-28 Hoffmann La Roche derivados de dicarboxamida
WO2006055184A2 (en) * 2004-11-16 2006-05-26 Janssen Pharmaceutica N.V. Novel heterocycle derivatives useful as selective androgen receptor modulators (sarms)
RU2368610C2 (ru) 2005-03-24 2009-09-27 УОРНЕР-ЛАМБЕРТ КОМПАНИ Эл-Эл-Си Кристаллические формы известного пирролидинового ингибитора фактора xa
DE102005017116A1 (de) * 2005-04-13 2006-10-26 Novartis Ag Hemmstoffe für Inhibitoren von Apoptose Proteinen (IAP)
PT1928454E (pt) 2005-05-10 2014-12-04 Intermune Inc Derivativos da piridona para modulação do sistema de proteína quinase ativada pelo stress
WO2007009883A1 (en) 2005-07-15 2007-01-25 F. Hoffmann-La Roche Ag Novel heteroaryl fused cyclic amines
US7678917B2 (en) 2005-09-01 2010-03-16 Hoffman-La Roche Inc. Factor Xa inhibitors
WO2007053610A2 (en) * 2005-11-01 2007-05-10 The Regents Of The University Of California Methods of treating atrial fibrillation wtih pirfenidone
JP2009515925A (ja) * 2005-11-16 2009-04-16 エフ．ホフマン−ラ ロシュ アーゲー 凝固第Ｘａ因子のインヒビターとしての新規なピロリジン誘導体
TW200730478A (en) * 2005-12-12 2007-08-16 Genelabs Tech Inc N-(6-membered aromatic ring)-amido anti-viral compounds
WO2007084314A2 (en) * 2006-01-12 2007-07-26 Incyte Corporation MODULATORS OF 11-ß HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME
EP1847537A1 (en) 2006-04-21 2007-10-24 F. Hoffmann-La Roche Ag Dicarboxamide derivatives
MX2008014499A (es) 2006-05-16 2008-11-27 Boehringer Ingelheim Int Prolinamidas sustituidas, su perparacion y su uso como medicamentos.
WO2008044700A1 (en) * 2006-10-11 2008-04-17 Takeda Pharmaceutical Company Limited GSK-3β INHIBITOR
EP2099778A2 (en) * 2006-11-21 2009-09-16 Smithkline Beecham Corporation Amido anti-viral compounds
WO2008065503A1 (en) * 2006-11-29 2008-06-05 Pfizer Products Inc. (r) -5-methyl-4, 5-dihydro- pyrazole-1, 5-dicarboxylic acid 1- [ ( 4 -chlorophenyl) amide 5-{ [2-fluoro-4- (2-oxo-2h-pyridin-1-yl) -phenyl]amide) as a factor xa inhibitor
CA2672373C (en) 2006-12-19 2011-08-30 Pfizer Products Inc. Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases
WO2008127682A2 (en) 2007-04-13 2008-10-23 Millennium Pharmaceuticals, Inc. Combination anticoagulant therapy with a compound that acts as a factor xa inhibitor
TW200911787A (en) * 2007-07-03 2009-03-16 Astrazeneca Ab New aza-bicyclohexane compounds useful as inhibitors of thrombin
ATE506359T1 (de) * 2007-11-30 2011-05-15 Bayer Schering Pharma Ag Heteroaryl-substituierte piperidine
US8304413B2 (en) 2008-06-03 2012-11-06 Intermune, Inc. Compounds and methods for treating inflammatory and fibrotic disorders
TW201006832A (en) * 2008-07-15 2010-02-16 Novartis Ag Organic compounds
IN2012DN02580A (es) 2009-09-04 2015-08-28 Univ Vanderbilt
US8377970B2 (en) * 2009-10-08 2013-02-19 Rhizen Pharmaceuticals Sa Modulators of calcium release-activated calcium channel
US8993612B2 (en) 2009-10-08 2015-03-31 Rhizen Pharmaceuticals Sa Modulators of calcium release-activated calcium channel and methods for treatment of non-small cell lung cancer
WO2012093101A1 (en) 2011-01-04 2012-07-12 Novartis Ag Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd)
PT2800738T (pt) * 2012-01-06 2020-06-23 Novartis Ag Compostos heterocíclicos e métodos para a utilização dos mesmos
KR102438072B1 (ko) * 2012-01-12 2022-08-31 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
JP6155332B2 (ja) 2012-06-28 2017-06-28 ノバルティス アーゲー ピロリジン誘導体、および補体経路調節因子としてのその使用
JP6209605B2 (ja) 2012-06-28 2017-10-04 ノバルティス アーゲー ピロリジン誘導体、および補体経路調節因子としてのその使用
WO2014002052A1 (en) 2012-06-28 2014-01-03 Novartis Ag Pyrrolidine derivatives and their use as complement pathway modulators
ES2712190T3 (es) 2012-06-28 2019-05-09 Novartis Ag Moduladores de la vía del complemento y sus usos
JP6273274B2 (ja) 2012-06-28 2018-01-31 ノバルティス アーゲー 補体経路モジュレーターおよびその使用
EA201590200A1 (ru) 2012-07-12 2015-08-31 Новартис Аг Модуляторы пути активации комплемента и их применение
MX2015000830A (es) 2012-07-18 2015-10-26 Sunshine Lake Pharma Co Ltd Derivados heterociclicos nitrogenosos y su aplicacion en farmacos.
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
EA201300843A1 (ru) * 2013-08-01 2015-04-30 Арсений Валерьевич Айбушев Карбамоилфенильные производные для остановки, предотвращения и профилактики кровотечений или усиления системы гемостаза
CN103570699A (zh) * 2013-09-29 2014-02-12 北京万全德众医药生物技术有限公司 一种制备普卡必利的方法
DK3113772T3 (da) 2014-03-07 2020-12-07 Biocryst Pharm Inc Trifluormethylsubstituerede pyrazoler som inhibitorer af kallikrein fra humant plasma
KR102373700B1 (ko) 2014-04-02 2022-03-11 인터뮨, 인크. 항섬유성 피리디논
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
HK1249058A1 (zh) 2015-03-18 2018-10-26 Arvinas, Inc. 用於增强靶向蛋白质降解的化合物和方法
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
PL3355890T3 (pl) * 2015-10-01 2022-02-21 Biocryst Pharmaceuticals, Inc. Inhibitory ludzkiej kalikreiny osoczowej
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
HUE070289T2 (hu) 2016-10-11 2025-05-28 Arvinas Operations Inc Vegyületek és módszerek az androgénreceptor célzott lebontására
KR20230127371A (ko) 2016-11-01 2023-08-31 아비나스 오퍼레이션스, 인코포레이티드 타우(Tau)-단백질 표적화 프로탁(PROTAC) 및 관련 사용 방법
IL297717A (en) 2016-12-01 2022-12-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
MX2019007649A (es) 2016-12-23 2019-09-10 Arvinas Operations Inc Compuestos y metodos para la degradacion dirigida de polipeptidos de fibrosarcoma acelerado rapidamente.
WO2018119441A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Egfr proteolysis targeting chimeric molecules and associated methods of use
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
IL300417A (en) 2017-01-26 2023-04-01 Arvinas Operations Inc Bifunctional benzothiophene compounds, preparations containing them and their use in therapy
EP3577109A4 (en) 2017-01-31 2020-11-18 Arvinas Operations, Inc. CEREMONY LIGANDS AND BIFUNCTIONAL COMPOUNDS CONTAINING THEM
CN111132673A (zh) 2017-05-03 2020-05-08 维瓦斯治疗公司 非稠合三环化合物
US11192865B2 (en) 2017-08-21 2021-12-07 Vivace Therapeutics, Inc. Benzosulfonyl compounds
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
WO2019113236A1 (en) * 2017-12-06 2019-06-13 Vivace Therapeutics, Inc. Benzocarbonyl compounds
CN110240591A (zh) * 2018-03-08 2019-09-17 天津药物研究院有限公司 脯氨酸衍生物及其制备方法和用途
IL277602B2 (en) * 2018-03-29 2024-06-01 Centre Nat Rech Scient P2RX7 modulators in therapy
JP7720698B2 (ja) 2018-04-04 2025-08-08 アルビナス・オペレーションズ・インコーポレイテッド タンパク質分解の調節因子および関連する使用方法
CA3100503A1 (en) 2018-05-16 2019-11-21 Vivace Therapeutics, Inc. Oxadiazole compounds
CN112912376A (zh) 2018-08-20 2021-06-04 阿尔维纳斯运营股份有限公司 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated
EP4021450B1 (en) 2019-08-26 2025-11-05 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
AU2020405129A1 (en) 2019-12-19 2022-06-23 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
MX2022014071A (es) 2020-05-09 2023-01-30 Arvinas Operations Inc Metodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificacion que comprenden el mismo.
EP4204418A1 (en) 2020-08-28 2023-07-05 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
EP4211128A1 (en) 2020-09-14 2023-07-19 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
TW202432544A (zh) 2022-09-07 2024-08-16 美商亞文納營運公司 快速加速纖維肉瘤降解化合物及相關使用方法
TW202444727A (zh) 2023-01-26 2024-11-16 美商艾維納斯手術有限公司 基於cereblon之kras降解protac及其相關用途
WO2024214038A1 (en) * 2023-04-14 2024-10-17 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof
WO2025163561A1 (en) * 2024-02-01 2025-08-07 Pfizer Inc. Glucose-dependent insulinotropic polypeptide receptor antagonists and uses thereof

Family Cites Families (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US91116A (en) * 1869-06-08 Improvement in guard for door-knobs
US2947755A (en) * 1959-02-05 1960-08-02 Wallace & Tiernan Inc Substituted 1-m-aminophenyl-2-pyridones
US4559157A (en) * 1983-04-21 1985-12-17 Creative Products Resource Associates, Ltd. Cosmetic applicator useful for skin moisturizing
LU84979A1 (fr) * 1983-08-30 1985-04-24 Oreal Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux
US4820508A (en) * 1987-06-23 1989-04-11 Neutrogena Corporation Skin protective composition
US4992478A (en) * 1988-04-04 1991-02-12 Warner-Lambert Company Antiinflammatory skin moisturizing composition and method of preparing same
US4938949A (en) * 1988-09-12 1990-07-03 University Of New York Treatment of damaged bone marrow and dosage units therefor
US5118691A (en) * 1990-09-20 1992-06-02 Warner-Lambert Co. Substituted tetrahydropyridines as central nervous system agents
DE4326465A1 (de) * 1993-01-20 1995-02-09 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
US5681844A (en) 1994-04-18 1997-10-28 Corvas International, Inc. Methionine sulfone and s-substituted cysteine sulfone derivatives as enzyme inhibitors
GB9515489D0 (en) 1995-07-28 1995-09-27 Sandoz Ltd Organic compounds
DE19544687A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
HU224315B1 (hu) 1996-06-05 2005-07-28 Gyógyszerkutató Intézet Kft. Véralvadásgátló hatású peptidil-arginin-aldehid-származékok és a vegyületeket tartalmazó gyógyszerkészítmények
WO1998050031A1 (en) 1997-05-07 1998-11-12 University Of Pittsburgh Inhibitors of protein isoprenyl transferases
DE1019040T1 (de) * 1997-05-23 2001-02-08 Bayer Corp., West Haven Hemmung von p38 kinase aktivität durch arylharnstoff
ZA985247B (en) * 1997-06-19 1999-12-17 Du Pont Merck Pharma Guanidine mimics as factor Xa inhibitors.
CA2308428A1 (en) * 1997-11-03 1999-05-14 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
US6632815B2 (en) * 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
DE60040676D1 (de) 1999-09-17 2008-12-11 Millennium Pharm Inc BENZAMIDE UND ÄHNLICHE INHIBITOREN VON FAKTOR Xa
NZ517828A (en) 1999-09-17 2003-10-31 Millennium Pharm Inc Inhibitors having activity against mammalian factor Xa
DE10008329A1 (de) 2000-02-23 2001-08-30 Merck Patent Gmbh Aminosulfonylbiphenylderivate
CA2401778C (en) 2000-02-29 2010-12-21 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
HRP20020705A2 (en) * 2000-03-27 2004-12-31 Applied Research Systems Pharmaceutically active pyrrolidine derivatives
PT1268418E (pt) * 2000-03-27 2006-08-31 Applied Research Systems Derivados da pirrolidina farmacologicamente activos com inibidores bax
GB0030303D0 (en) 2000-12-13 2001-01-24 Lilly Co Eli Compounds
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
DE10036121A1 (de) 2000-07-25 2002-02-07 Merck Patent Gmbh N-Substituierte-1-amino-1,1-dialkyl-carbonsäurederivate
DE10046272A1 (de) 2000-09-19 2002-03-28 Merck Patent Gmbh Aminoheterocyclen (Faktor Xa Inhibitoren 14)
DE10050723A1 (de) 2000-10-13 2002-04-25 Merck Patent Gmbh N-Substituierte Aminosäurederivate (Faktor Xa Inhibitoren 12)
DE10063008A1 (de) 2000-12-16 2002-06-20 Merck Patent Gmbh Carbonsäureamidderivate
DE10102322A1 (de) 2001-01-19 2002-07-25 Merck Patent Gmbh Phenylderivate
US7030141B2 (en) * 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
WO2005044785A1 (en) * 2003-10-30 2005-05-19 Merck & Co., Inc. Aralkyl amines as cannabinoid receptor modulators
FR2864958B1 (fr) * 2004-01-12 2006-02-24 Sanofi Synthelabo Derive de n-[(1,5-diphenyl-1h-pyrazol-3-yl)methyl] sulfonamide, leur preparation et leur application en therapeutique.
DE102005038537A1 (de) * 2005-08-16 2007-02-22 Merck Patent Gmbh 1-Acyldihydropyrazolderivate
EP2096111A1 (en) * 2006-11-20 2009-09-02 Japan Tobacco Inc. Pyrazoles and use thereof as drugs
DE102007037017A1 (de) * 2007-08-06 2009-02-19 Clariant International Ltd. 1-Alkyl-5-oxo-pyrrolidin-3-carbonsäureester mit verbesserter biologischer Abbaubarkeit

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