KR100518690B1 - 디펩타이드 니트릴 - Google Patents

디펩타이드 니트릴 Download PDF

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KR100518690B1
KR100518690B1 KR10-2000-7004868A KR20007004868A KR100518690B1 KR 100518690 B1 KR100518690 B1 KR 100518690B1 KR 20007004868 A KR20007004868 A KR 20007004868A KR 100518690 B1 KR100518690 B1 KR 100518690B1
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South Korea
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aryl
lower alkyl
formula
substituted
mmol
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Korean (ko)
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KR20010031800A (ko
Inventor
에바 알트만
클라우디아 베챠르트
게이꼬 고다
미유끼 호리우찌
렌 래트만
마틴 미쓰바흐
쥰이찌 사까끼
미찌히로 다까이
나오끼 데노
스코트 더글라스 코웬
폴 데이비드 그린스판
레슬리 위그톤 맥과이어
루벤 앨버토 토마시
존 헨리 밴두저
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노파르티스 아게
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    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—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 two 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
    • C07D207/325—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 two 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 with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • C07D207/327—Radicals substituted by 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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    • C07C323/62—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
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Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2560000A (en) * 1999-02-20 2000-09-04 Astrazeneca Ab Di- and tripeptide nitrile derivatives as inhibitors of cathepsin l and cathepsin
CA2360740A1 (en) * 1999-03-02 2000-09-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cathepsin s
EP1452522A3 (en) * 1999-03-15 2005-02-09 Axys Pharmaceuticals, Inc. Novel compounds and compositions as protease inhibitors
HRP20010738B1 (en) * 1999-03-15 2005-02-28 Axys Pharmaceuticals N-cyanomethyl amides as protease inhibitors
DE60028045T2 (de) 1999-07-30 2007-02-15 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Neue bernsteinsäure derivative als cysteine-protease-inhibitoren
US6420364B1 (en) 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
GB9925264D0 (en) * 1999-10-26 1999-12-29 Zeneca Ltd Chemical compounds
KR100468254B1 (ko) 1999-12-24 2005-01-27 에프. 호프만-라 로슈 아게 카텝신 ｋ 억제제로서의 니트릴 유도체
GB0003111D0 (en) * 2000-02-10 2000-03-29 Novartis Ag Organic compounds
US6653304B2 (en) * 2000-02-11 2003-11-25 Bristol-Myers Squibb Co. Cannabinoid receptor modulators, their processes of preparation, and use of cannabinoid receptor modulators for treating respiratory and non-respiratory diseases
AU2001245764A1 (en) * 2000-03-15 2001-09-24 Axys Pharmaceuticals, Inc. Novel compounds and compositions as protease inhibitors
AU9521401A (en) * 2000-05-15 2001-11-26 Novartis Ag N-substituted peptidyl nitriles as cysteine cathepsin inhibitors
US6812237B2 (en) 2000-05-15 2004-11-02 Novartis Ag N-substituted peptidyl nitriles as cysteine cathepsin inhibitors
US6462076B2 (en) 2000-06-14 2002-10-08 Hoffmann-La Roche Inc. Beta-amino acid nitrile derivatives as cathepsin K inhibitors
EP1309591B1 (en) 2000-08-14 2007-01-24 Ortho-McNeil Pharmaceutical, Inc. Substituted pyrazoles
US7332494B2 (en) 2000-08-14 2008-02-19 Janssen Pharmaceutica, N.V. Method for treating allergies using substituted pyrazoles
KR100837193B1 (ko) 2000-08-14 2008-06-13 오르토-맥네일 파마슈티칼, 인코퍼레이티드 치환된 피라졸
ES2262674T3 (es) 2000-08-14 2006-12-01 Ortho-Mcneil Pharmaceutical, Inc. Pirazoles sustituidos.
US7199102B2 (en) 2000-08-24 2007-04-03 The Regents Of The University Of California Orally administered peptides synergize statin activity
EP1315741A2 (en) * 2000-09-06 2003-06-04 Ortho-McNeil Pharmaceutical, Inc. A method for treating allergies
EP1383748A2 (en) 2000-12-22 2004-01-28 Axys Pharmaceuticals, Inc. Novel compounds and compositions as cathepsin inhibitors
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
EP1372655B1 (en) 2001-03-02 2008-10-01 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
US6982263B2 (en) 2001-06-08 2006-01-03 Boehringer Ingelheim Pharmaceuticals, Inc. Nitriles useful as reversible inhibitors of cysteine proteases
CA2460125A1 (en) 2001-09-14 2003-03-27 Aventis Pharmaceuticals Inc. Novel compounds and compositions as cathepsin inhibitors
AU2002340031A1 (en) 2001-10-02 2003-04-14 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
US6841571B2 (en) 2001-10-29 2005-01-11 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cysteine proteases
US6784288B2 (en) 2001-11-08 2004-08-31 Ortho-Mcneil Pharmaceutical, Inc. Polynucleotide and polypeptide sequences of monkey cathepsin S
US6780985B2 (en) 2001-11-08 2004-08-24 Ortho-Mcneil Pharmaceutical, Inc. Polynucleotide and polypeptide sequences of Canine Cathepsin S
KR20050044497A (ko) 2001-11-14 2005-05-12 아벤티스 파마슈티칼스 인크. 올리고펩티드 및 카텝신 ｓ 억제제로서 이를 포함하는조성물
AU2002352126A1 (en) 2001-12-04 2003-06-17 F. Hoffmann-La Roche Ag Substituted 2-amino-cycloalkanecarboxamides and their use as cysteine protease inhibitors
US6759428B2 (en) 2001-12-04 2004-07-06 Roche Palo Alto Llc Indole nitriles
US7282512B2 (en) 2002-01-17 2007-10-16 Smithkline Beecham Corporation Cycloalkyl ketoamides derivatives useful as cathepsin K inhibitors
WO2003075836A2 (en) * 2002-03-05 2003-09-18 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors
AU2003298740A1 (en) * 2002-12-05 2004-06-30 Axys Pharmaceuticals, Inc. Cyanomethyl derivatives as cysteine protease inhibitors
US7465745B2 (en) 2003-03-13 2008-12-16 Boehringer Ingelheim Pharmaceuticals, Inc. Cathepsin S inhibitors
US7326719B2 (en) 2003-03-13 2008-02-05 Boehringer Ingelheim Pharmaceuticals, Inc. Cathepsin S inhibitors
JP2006527704A (ja) * 2003-06-18 2006-12-07 プロザイメックス・アクティーゼルスカブ プロテアーゼ阻害剤
KR100738230B1 (ko) * 2003-06-30 2007-07-12 주식회사 오스코텍 메톡시아크릴레이트계 화합물을 포함하는, 골다공증 예방 또는 치료용 조성물
US7317019B2 (en) 2003-08-21 2008-01-08 Bristol Myers Squibb Co. N-alkylated diaminopropane derivatives as modulators of chemokine receptor activity
BRPI0410979A (pt) 2003-09-18 2006-07-04 Axys Pharm Inc composto, composição farmacêutica, e, métodos para tratar uma doença em um animal mediada pela catepsina s e para tratar um paciente submetido a uma terapia
CA2543884A1 (en) 2003-10-30 2005-05-19 Boehringer Ingelheim Pharmaceuticals, Inc. Dipeptide-analogue synthesis
WO2005049028A1 (en) * 2003-11-19 2005-06-02 Novartis Ag Use of cathepsin k inhibitors in severe bone loss diseases
CN100548986C (zh) 2003-12-12 2009-10-14 默克弗罗斯特加拿大有限公司 组织蛋白酶半胱氨酸蛋白酶抑制剂
EP1716120A1 (de) * 2003-12-19 2006-11-02 Basf Aktiengesellschaft Herbizide heteroaroyl-substituierte phenylalanin-amide
US7737300B2 (en) * 2004-09-17 2010-06-15 Virobay, Inc. Processes and intermediates preparing cysteine protease inhibitors
AR055283A1 (es) * 2004-11-23 2007-08-15 Merck Frosst Canada Ltd Inhibidores de cisteinproteasa de catepsina
EP1819667B1 (en) 2004-12-02 2012-10-17 ViroBay, Inc. Sulfonamide compounds as cysteine protease inhibitors
RU2414236C2 (ru) 2004-12-06 2011-03-20 Зе Риджентс Оф Зи Юнивесити Оф Кэлифонье Способ улучшения структуры и/или функций артериол
GB0427380D0 (en) * 2004-12-14 2005-01-19 Novartis Ag Organic compounds
WO2006076797A1 (en) * 2005-01-19 2006-07-27 Merck Frosst Canada Ltd. Cathepsin k inhibitors and atherosclerosis
WO2006076796A1 (en) * 2005-01-19 2006-07-27 Merck Frosst Canada Ltd. Cathepsin k inhibitors and obesity
EP1865940B1 (en) 2005-03-21 2013-02-13 Virobay, Inc. Alpha ketoamide compounds as cysteine protease inhibitors
JP5215167B2 (ja) 2005-03-22 2013-06-19 ビロベイ，インコーポレイティド システインプロテアーゼ阻害剤としてのスルホニル基含有化合物
JP5311822B2 (ja) * 2005-07-19 2013-10-09 第一三共株式会社 置換プロパンアミド誘導体及びそれを含む医薬組成物
WO2007081530A2 (en) * 2006-01-03 2007-07-19 Med Institute, Inc. Endoluminal medical device for local delivery of cathepsin inhibitors
WO2007137738A1 (de) 2006-06-01 2007-12-06 Sanofi-Aventis Spiro-cyclische nitrile als protease-inhibitoren
US7893112B2 (en) 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
CA2664878A1 (en) 2006-10-04 2008-04-10 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
EP2719700A1 (en) 2008-01-09 2014-04-16 Amura Therapeutics Limited Tetrahydrofuro(3,2-b)pyrrol-3-one derivatives as inhibitors of cysteine proteinases
WO2009103432A2 (en) * 2008-02-21 2009-08-27 Sanofi-Aventis Covalently binding imaging probes
EP2198879A1 (en) 2008-12-11 2010-06-23 Institut Curie CD74 modulator agent for regulating dendritic cell migration and device for studying the motility capacity of a cell
US8324417B2 (en) 2009-08-19 2012-12-04 Virobay, Inc. Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof
US9365612B2 (en) * 2010-01-29 2016-06-14 United States Of America As Represented By The Secretary, Department Of Health And Human Services Caspase inhibitors
US9330026B2 (en) * 2013-03-05 2016-05-03 Qualcomm Incorporated Method and apparatus for preventing unauthorized access to contents of a register under certain conditions when performing a hardware table walk (HWTW)
EP3342765B1 (en) * 2015-08-29 2021-09-15 Sunshine Lake Pharma Co., Ltd. Cathepsin k inhibitor and application thereof
CN106478564B (zh) * 2015-08-29 2021-11-12 广东东阳光药业有限公司 组织蛋白酶k抑制剂及其用途
CN108368056A (zh) * 2015-11-26 2018-08-03 豪夫迈·罗氏有限公司 锥虫抑制剂
WO2020095983A1 (ja) 2018-11-07 2020-05-14 中外製薬株式会社 Ｏ－置換セリン誘導体の製造方法
US11124497B1 (en) 2020-04-17 2021-09-21 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof
US11174231B1 (en) 2020-06-09 2021-11-16 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof
JP2023530627A (ja) * 2020-06-09 2023-07-19 パルデス バイオサイエンシーズ， インコーポレイテッド システインプロテアーゼの阻害剤及びその使用方法
US20240083845A1 (en) * 2020-12-18 2024-03-14 Heptares Therapeutics Limited Sars-cov-2 mpro inhibitor compounds
GB202107385D0 (en) * 2021-05-24 2021-07-07 Heptares Therapeutics Ltd Sars-cov-2 mpro inhibitor compounds
KR20220115062A (ko) 2021-02-09 2022-08-17 (주)오스티오뉴로젠 크로몬 구조의 화합물을 포함하는 골다공증의 예방 및 치료용 약학적 조성물
CN116589425A (zh) * 2022-12-29 2023-08-15 百放英库医药科技(北京)有限公司 组织蛋白酶l抑制剂

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3697577A (en) * 1964-04-22 1972-10-10 Kyorin Seiyaku Kk Derivatives of n(n-acyl amino acyl) aminoacetonitrile

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2848232B2 (ja) * 1993-02-19 1999-01-20 武田薬品工業株式会社 アルデヒド誘導体
WO1997027200A1 (en) * 1996-01-26 1997-07-31 Smithkline Beecham Plc Thienoxazinone derivatives useful as antiviral agents
IL129504A0 (en) * 1996-11-22 2000-02-29 Elan Pharm Inc N-(aryl/heteroaryl/alkylacetyl) amino acid amides pharmaceutical compositions comprising same and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3697577A (en) * 1964-04-22 1972-10-10 Kyorin Seiyaku Kk Derivatives of n(n-acyl amino acyl) aminoacetonitrile

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Biochemistry, 34, 9136-9143(1995.7) *

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