EA200300017A1 - Ингибиторы серинпротеазы - Google Patents

Ингибиторы серинпротеазы

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Publication number
EA200300017A1
EA200300017A1 EA200300017A EA200300017A EA200300017A1 EA 200300017 A1 EA200300017 A1 EA 200300017A1 EA 200300017 A EA200300017 A EA 200300017A EA 200300017 A EA200300017 A EA 200300017A EA 200300017 A1 EA200300017 A1 EA 200300017A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
serinprotease inhibitors
serinprotease
factor
compounds
Prior art date
Application number
EA200300017A
Other languages
English (en)
Other versions
EA005943B1 (ru
Inventor
Джон Вальтер Либешютц
Кристофер Вилльям Мюррей
Стивен Клинтон Янг
Николас Пол Кэмп
Стюарт Дональд Джоунз
Вилльям Александер Уайли
Джон Джозеф Мастерз
Майкл Роберт Уилли
Скотт Мартин Шихан
Дэвид Биренбаум Энгел
Брайан Морган Уотсон
Питер Роберт Гуццо
Майкл Джон Мейер
Original Assignee
Эли Лилли Энд Компани
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
Priority claimed from PCT/GB2000/002302 external-priority patent/WO2000076971A2/en
Application filed by Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA200300017A1 publication Critical patent/EA200300017A1/ru
Publication of EA005943B1 publication Critical patent/EA005943B1/ru

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/16Heterocyclic 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 acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic 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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/185Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61P9/10Drugs 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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    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/04Heterocyclic 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
    • C07D207/10Heterocyclic 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
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    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
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    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
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    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/04Heterocyclic 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
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    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
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    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

Соединения формулы (I), в которой R, X, Y, Cy, L и L(D)имеют значения, указанные в описании, являются ингибиторами сериновой протеазы фактора Xa и полезны при лечении сердечно-сосудистых расстройств.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200300017A 2000-06-13 2001-06-12 Ингибиторы серинпротеазы EA005943B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PCT/GB2000/002302 WO2000076971A2 (en) 1999-06-14 2000-06-13 Serine protease inhibitors
GBGB0030304.0A GB0030304D0 (en) 2000-12-13 2000-12-13 Compounds
PCT/GB2001/002553 WO2001096323A1 (en) 2000-06-13 2001-06-12 Serine protease inhibitors

Publications (2)

Publication Number Publication Date
EA200300017A1 true EA200300017A1 (ru) 2003-10-30
EA005943B1 EA005943B1 (ru) 2005-08-25

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EA200300017A EA005943B1 (ru) 2000-06-13 2001-06-12 Ингибиторы серинпротеазы

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US (3) US6946467B2 (ru)
EP (2) EP1289972B1 (ru)
JP (1) JP4175885B2 (ru)
KR (1) KR100634936B1 (ru)
CN (1) CN1213040C (ru)
AT (1) ATE275554T1 (ru)
AU (2) AU2001262553B2 (ru)
BR (1) BR0111451A (ru)
CA (1) CA2411805A1 (ru)
DE (1) DE60105419T2 (ru)
DK (1) DK1289972T3 (ru)
EA (1) EA005943B1 (ru)
EC (1) ECSP024382A (ru)
ES (1) ES2228869T3 (ru)
GB (1) GB0030304D0 (ru)
HK (1) HK1054379B (ru)
HR (1) HRP20020997B1 (ru)
HU (1) HUP0300720A3 (ru)
IL (1) IL152586A0 (ru)
MX (1) MXPA02011411A (ru)
NO (1) NO324696B1 (ru)
NZ (1) NZ521896A (ru)
PL (1) PL201525B1 (ru)
PT (1) PT1289972E (ru)
SI (1) SI1289972T1 (ru)
SK (1) SK17222002A3 (ru)
TR (1) TR200402535T4 (ru)
UA (1) UA74372C2 (ru)
WO (1) WO2001096323A1 (ru)

Families Citing this family (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU6407701A (en) * 2000-06-13 2001-12-24 Tularik Ltd Serine protease inhibitors
GB0030304D0 (en) * 2000-12-13 2001-01-24 Lilly Co Eli Compounds
DE10059864A1 (de) 2000-11-30 2002-06-13 Gruenenthal Gmbh Substituierte Amino-furan-2-yl-essigsäure- und Amino-thien-2-yl-essigsäure-Derivate
TWI257389B (en) * 2001-06-12 2006-07-01 Lilly Co Eli Pharmaceutical compound
JP2005502623A (ja) * 2001-07-02 2005-01-27 ノボ ノルディスク アクティーゼルスカブ 置換ピペラジンおよびジアゼパン
AU2002322396A1 (en) * 2001-07-26 2003-02-17 Eli Lilly And Company 1-glycinyl-4 (methylpiperidin-4-yl) piperazines and -piperridines as factor xa antagonists
EP1455787B1 (en) 2001-12-12 2005-06-22 Eli Lilly And Company Certain glycine derivatives as factor xa inhibitors for use in the treatment of thrombotic disorders
AU2002359458A1 (en) 2001-12-12 2003-06-23 Eli Lilly And Company Alanyl-piperidine heterocyclic derivatives useful against cardiovascular diseases
PL373066A1 (en) 2002-04-01 2005-08-08 Eli Lilly And Company Certain 1-(d-cyclopropylglycinyl)-4-(piperidin-4-yl)piperazine compounds as inhibitors of the serine protease factor xa
AU2003267201B2 (en) * 2002-09-14 2009-04-23 The Gov't Of The U.S.A. As Represented By The Secretary Of The Department Of Health And Human Services Structurally rigid dopamine D3 receptor selective ligands and process for making them
PE20040804A1 (es) 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma DERIVADOS DE CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa
US7371743B2 (en) 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
MXPA06013213A (es) * 2004-05-13 2007-02-08 Boehringer Ingelheim Int Nuevas amidas sustituidas del acido tiofencarboxilico, su obtencion y su uso como medicamentos.
CN1984903A (zh) * 2004-06-30 2007-06-20 伊莱利利公司 1-(吲哚-6-羰基-d-苯基甘氨酰基)-4-(1-甲基哌啶-4-基)哌嗪d-酒石酸盐
KR100849242B1 (ko) * 2004-06-30 2008-07-29 일라이 릴리 앤드 캄파니 1(인돌-6-카르보닐-d-페닐글리시닐)-4-(1-메틸피페리딘-4-일) 피페라진 d-타르트레이트
AR051202A1 (es) 2004-09-20 2006-12-27 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa
AU2005329423A1 (en) 2004-09-20 2006-09-28 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
US7951805B2 (en) 2004-09-20 2011-05-31 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase
WO2006034315A2 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-coa desaturase enzymes
CN101083994A (zh) 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其用作硬脂酰CoA去饱和酶抑制剂的用途
CA2580845A1 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
MX2007003321A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
US7674822B2 (en) 2004-11-24 2010-03-09 Wyeth PTP1b inhibitors
BRPI0611187A2 (pt) 2005-06-03 2010-08-24 Xenon Pharmaceuticals Inc derivados aminotiazàis como inibidores da estearoil-coa desaturase humana
US20070270806A1 (en) * 2006-04-07 2007-11-22 Foley Kevin T Devices and methods for receiving elongated connecting elements in spinal surgical procedures
WO2009134666A1 (en) 2008-04-29 2009-11-05 Boehringer Ingelheim International Gmbh Indazole compounds as ccr1 receptor antagonists
WO2009137338A1 (en) * 2008-05-06 2009-11-12 Boehringer Ingelheim International Gmbh Pyrazole compounds as ccr1 antagonists
US20120028024A1 (en) 2008-07-18 2012-02-02 Dow Global Technologies Inc. Cellular structures and viscoelastic polyurethane foams
JP5507567B2 (ja) 2008-09-26 2014-05-28 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ccr1受容体拮抗薬としてのアザインダゾール化合物
KR20120087923A (ko) 2009-10-21 2012-08-07 베링거 인겔하임 인터내셔날 게엠베하 Ccr1 수용체 길항제로서의 인다졸 및 피라졸로피리딘 화합물
US8927550B2 (en) 2009-10-27 2015-01-06 Boehringer Ingelheim International Gmbh Heterocyclic compounds as CCR1 receptor antagonists
BR112012013582A2 (pt) * 2009-12-08 2016-07-05 Boehringer Ingelheim Int processo para síntese de intermediários úteis para a produção de compostos de indazol e azaindazol substituídos
US8871786B2 (en) 2010-04-30 2014-10-28 Boehringer Ingelheim International Gmbh Azaindazole amide compounds as CCR1 receptor antagonists
EP2632464B1 (en) * 2010-10-29 2015-04-29 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
JP5684406B2 (ja) 2010-12-23 2015-03-11 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ccr1受容体アンタゴニストとしてのピラゾロピペリジン化合物
WO2014174102A1 (en) * 2013-04-26 2014-10-30 Sanofi Tartrate salt of 5-chloro-thiophene-2-carboxylic acid [(s)-2-[methyl-3-(2-oxo-pyrrolidin-1-yl)-benzenesulfonylamino]-3-(4-methyl piperazin-1 -yl)-3-oxo-propryl]amide

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3268513A (en) 1964-03-20 1966-08-23 American Home Prod Process for producing 6-(alpha-amino-acylamino-acylamino)-penicillanic acids
US5346907A (en) 1988-04-05 1994-09-13 Abbott Laboratories Amino acid analog CCK antagonists
IE902295A1 (en) 1989-07-07 1991-01-16 Abbott Lab Amino acid analog cck antagonists
CA2200163A1 (en) 1996-03-22 1997-09-22 Michael Robert Wiley Antithrombotic diamides
AU3496297A (en) 1996-06-25 1998-01-14 Eli Lilly And Company Anticoagulant agents
IL123986A (en) 1997-04-24 2011-10-31 Organon Nv Medicinal compounds
US6417200B1 (en) 1997-06-26 2002-07-09 Eli Lilly And Company Antithrombotic agents
IL133621A0 (en) 1997-06-26 2001-04-30 Lilly Co Eli Antithrombotic agents
DE69830504T2 (de) 1997-06-26 2006-03-16 Eli Lilly And Co., Indianapolis Antithrombotische mitteln
AU8269398A (en) 1997-06-26 1999-01-19 Eli Lilly And Company Antithrombotic agents
TW460478B (en) 1997-08-15 2001-10-21 Chugai Pharmaceutical Co Ltd Phenethylamine derivatives
EP1009758B1 (en) 1997-08-29 2005-06-01 Tularik Limited Meta-benzamidine derivatives as serine protease inhibitors
WO2000077027A2 (en) 1999-06-14 2000-12-21 Tularik Limited Serine protease inhibitors
JP2002533453A (ja) 1998-12-23 2002-10-08 イーライ・リリー・アンド・カンパニー Xa因子のインヒビターとしてのヘテロ芳香族アミド
ATE272633T1 (de) 1998-12-23 2004-08-15 Lilly Co Eli Aromatische amiden
EP1140881B1 (en) 1998-12-23 2006-05-17 Eli Lilly And Company Antithrombotic amides
ES2217879T3 (es) 1998-12-24 2004-11-01 Eli Lilly And Company Amidas heterociclicas.
AU5723500A (en) 1999-05-24 2000-12-12 Cor Therapeutics, Inc. Inhibitors of factor xa
WO2000071507A2 (en) 1999-05-24 2000-11-30 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa
ES2248084T3 (es) * 1999-06-14 2006-03-16 Eli Lilly And Company Inhibidores de serinproteasa.
GB0030304D0 (en) * 2000-12-13 2001-01-24 Lilly Co Eli Compounds

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