UA76088C2 - N-cyanomethyl amides as cysteine protease inhibitors - Google Patents

N-cyanomethyl amides as cysteine protease inhibitors Download PDF

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Publication number
UA76088C2
UA76088C2 UA2001096333A UA2001096333A UA76088C2 UA 76088 C2 UA76088 C2 UA 76088C2 UA 2001096333 A UA2001096333 A UA 2001096333A UA 2001096333 A UA2001096333 A UA 2001096333A UA 76088 C2 UA76088 C2 UA 76088C2
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Ukraine
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alkyl
compound
substituted
hydrogen
halo
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UA2001096333A
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English (en)
Ukrainian (uk)
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Axys Pharm Inc
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Families Citing this family (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9723407D0 (en) * 1997-11-05 1998-01-07 Ciba Geigy Ag Organic compounds
IL145430A0 (en) * 1999-03-15 2002-06-30 Axys Pharm Inc N-cyanomethyl amides, processes for the preparation thereof and pharmaceutical compositions containing the same
US6420364B1 (en) 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
PL364045A1 (en) * 1999-09-13 2004-12-13 Boehringer Ingelheim Pharmaceuticals, Inc. Novel spiroheterocyclic compounds useful as reversible inhibitors of cysteine proteases
AU7490900A (en) * 1999-09-16 2001-04-17 Axys Pharmaceuticals, Inc. Chemical compounds and compositions and their use as cathepsin s inhibitors
GB9928330D0 (en) 1999-11-30 2000-01-26 Ferring Bv Novel antidiabetic agents
AU783145B2 (en) 1999-12-24 2005-09-29 F. Hoffmann-La Roche Ag Nitrile derivatives as cathepsin K inhibitors
CA2396257A1 (en) * 2000-01-06 2001-07-12 Merck Frosst Canada & Co./Merck Frosst Canada & Cie Novel compounds and compositions as protease inhibitors
GB0003111D0 (en) * 2000-02-10 2000-03-29 Novartis Ag Organic compounds
WO2001068645A2 (en) * 2000-03-15 2001-09-20 Axys Pharmaceuticals, Inc. N-cyanomethylcarboxamides and their use as protease inhibitors
UA74362C2 (uk) * 2000-03-27 2005-12-15 Еплайд Рісьорч Системз Ерс Холдінг Н.В. Фармацевтично активні похідні піролідину
SI1268418T1 (sl) * 2000-03-27 2006-10-31 Applied Research Systems Farmacevtsko aktivni pirolidinski derivati kot bax-inhibitorji
CA2407463C (en) * 2000-05-15 2010-01-12 Scott Douglas Cowen N-substituted peptidyl nitriles as cysteine cathepsin inhibitors
DE60139639D1 (de) * 2000-12-08 2009-10-01 Takeda Pharmaceutical Substituierte thiazolderivate mit 3-pyridylgruppen, verfahren zu deren herstellung und deren verwendung
US7030116B2 (en) * 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
WO2002051983A2 (en) 2000-12-22 2002-07-04 Axys Pharmaceuticals, Inc. Novel compounds and compositions as cathepsin inhibitors
EP1372655B1 (en) 2001-03-02 2008-10-01 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
CN1512983A (zh) * 2001-06-01 2004-07-14 AXYSҩ�﹫˾ 作为组织蛋白酶s抑制剂的化合物和组合物
US20040147503A1 (en) * 2002-06-04 2004-07-29 Sheila Zipfeil Novel compounds and compositions as cathepsin inhibitors
WO2003024924A1 (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
JP2005508979A (ja) 2001-10-29 2005-04-07 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド システインプロテアーゼの可逆性インヒビターとして有用な化合物
WO2003039534A1 (en) * 2001-11-08 2003-05-15 Merck & Co., Inc. Compositions and methods for treating osteoporosis
JP4343690B2 (ja) * 2001-11-13 2009-10-14 メルク フロスト カナダ リミテツド プロテアーゼ阻害薬としてのシアノアルキルアミノ誘導体
MXPA04004450A (es) * 2001-11-14 2004-08-11 Aventis Pharma Inc Nuevos compuestos y composiciones como inhibidores de catepsina s.
US7727964B2 (en) * 2001-11-26 2010-06-01 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
US20060009423A1 (en) * 2002-02-19 2006-01-12 Eric Joseph Niesor Phosphonate-phosphate and diphosphonate apolipoprotein e modulators
PT1482924E (pt) 2002-03-05 2008-08-27 Axys Pharm Inc Inibidores de proteases da cisteína catepsina
WO2003075853A2 (en) 2002-03-08 2003-09-18 Bristol-Myers Squibb Company Cyclic derivatives as modulators of chemokine receptor activity
SE0201980D0 (sv) * 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
SE0201977D0 (sv) * 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
SE0201976D0 (sv) * 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
US7279478B2 (en) 2002-09-04 2007-10-09 Merck Frosst Canada & Co. Cathepsin cysteine protease inhibitors
US20060122184A1 (en) * 2002-12-05 2006-06-08 Axys Pharmaceuticals, Inc. Cyanomethyl derivatives as cysteine protease inhibitors
US7109243B2 (en) * 2003-03-24 2006-09-19 Irm Llc Inhibitors of cathepsin S
US7384970B2 (en) * 2003-03-24 2008-06-10 Irm Llc Inhibitors of cathepsin S
JP2006526657A (ja) * 2003-06-04 2006-11-24 アクシス ファーマシューティカルズ システインプロテアーゼ阻害剤としてのアミジノ化合物
US7173051B2 (en) * 2003-06-13 2007-02-06 Irm, Llc Inhibitors of cathepsin S
WO2005005456A2 (en) * 2003-07-08 2005-01-20 Glaxo Group Limited Peptide deformylase inhibitors
US7256207B2 (en) 2003-08-20 2007-08-14 Irm Llc Inhibitors of cathepsin S
CA2535359A1 (en) 2003-08-21 2005-03-03 Merck Frosst Canada Ltd. Cathepsin cysteine protease inhibitors
PT1663958E (pt) 2003-09-18 2015-06-01 Virobay Inc Compostos contendo haloalquilo como inibidores de protease de cisteína
KR100793095B1 (ko) * 2003-10-01 2008-01-10 주식회사 프로메디텍 Ｂａｃｅ 저해효능을 가진 신규한 술폰 아미드 유도체
US7297714B2 (en) * 2003-10-21 2007-11-20 Irm Llc Inhibitors of cathepsin S
EP1682524A1 (en) * 2003-10-24 2006-07-26 Aventis Pharmaceuticals, Inc. Novel keto-oxadiazole derivatives as cathepsin inhibitors
US7935698B2 (en) * 2003-11-10 2011-05-03 Synta Pharmaceuticals Corporation Heteroaryl-hydrazone compounds
WO2006042103A2 (en) * 2004-10-05 2006-04-20 Axys Pharmaceuticals, Inc. Reversible inhibitors of cathepsin b
WO2006060810A1 (en) 2004-12-02 2006-06-08 Schering Aktiengesellschaft Sulfonamide compounds as cysteine protease inhibitors
WO2006062876A2 (en) 2004-12-09 2006-06-15 Merck & Co., Inc. Estrogen receptor modulators
AU2006227254B2 (en) 2005-03-21 2011-09-01 Quest Diagnostics Investments Llc 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
ES2477868T3 (es) * 2005-04-22 2014-07-18 Alantos Pharmaceuticals Holding, Inc. Inhibidores de dipeptidil peptidasa-IV
EP1760076A1 (en) 2005-09-02 2007-03-07 Ferring B.V. FAP Inhibitors
CN102417480B (zh) 2006-06-01 2015-08-26 塞诺菲-安万特股份有限公司 作为蛋白酶抑制剂的螺环腈类
EA022130B1 (ru) 2006-10-04 2015-11-30 Вайробей, Инк. Дифторосодержащие соединения в качестве ингибиторов цистеиновых протеаз
US7893112B2 (en) 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
AU2007338689A1 (en) * 2006-12-22 2008-07-03 Encysive Pharmaceuticals, Inc. Modulators of C3a receptor and methods of use thereof
US7638541B2 (en) * 2006-12-28 2009-12-29 Metabolex Inc. 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine
PL2134704T3 (pl) * 2007-03-08 2011-03-31 Irm Llc Związki i kompozycje pełniące rolę modulatorów aktywności GPR119
AU2008279447A1 (en) 2007-07-19 2009-01-29 Metabolex, Inc. N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the RUP3 or GPR119 receptor for the treatment of diabetes and metabolic disorders
EP2240491B1 (en) 2008-01-09 2015-07-15 Amura Therapeutics Limited TETRAHYDROFURO(2,3-b)PYRROL-3-ONE DERIVATIVES AS INHIBITORS OF CYSTEINE PROTEINASES
EP2344480A1 (en) 2008-10-15 2011-07-20 Boehringer Ingelheim International GmbH Fused heteroaryl diamide compounds useful as mmp-13 inhibitors
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
PL2421826T3 (pl) * 2009-04-20 2014-03-31 Hoffmann La Roche Pochodne proliny jako inhibitory katepsyn
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
CA2775840C (en) 2009-10-01 2018-02-06 Metabolex, Inc. Substituted tetrazol-1-yl-phenoxymethyl-thiazol-2-yl-piperidinyl-pyrimidine salts
AR079022A1 (es) * 2009-11-02 2011-12-21 Sanofi Aventis Derivados de acido carboxilico ciclico sustituidos con acilamino, su uso como productos farmaceuticos, composicion farmaceutica y metodo de preparacion
CN103339265B (zh) 2010-10-06 2018-03-30 生物医学研究机构私人基金会 用于乳腺癌转移的诊断、预后和治疗的方法
MX2013013281A (es) 2011-05-16 2013-12-06 Bayer Ip Gmbh Uso de la inhibicion de la catepsina k para el tratamiento y/o profilaxis de hipertension pulmonar y/o insuficiencia cardiaca.
EP2650682A1 (en) 2012-04-09 2013-10-16 Fundació Privada Institut de Recerca Biomèdica Method for the prognosis and treatment of cancer metastasis
CN104603288B (zh) 2012-06-06 2018-12-14 生物医学研究机构基金会 用于肺癌转移的诊断、预后和治疗的方法
AR091857A1 (es) * 2012-07-25 2015-03-04 Sova Pharmaceuticals Inc INHIBIDORES DE CISTATIONIN-g-LIASA (CSE)
MX365421B (es) 2012-10-12 2019-06-03 Inbiomotion Sl Método in-vitro para diagnóstico, pronóstico y tratamiento de metástasis de cáncer de próstata usando c-maf.
US10119171B2 (en) 2012-10-12 2018-11-06 Inbiomotion S.L. Method for the diagnosis, prognosis and treatment of prostate cancer metastasis
WO2014184679A2 (en) 2013-03-15 2014-11-20 Inbiomotion S.L. Method for the prognosis and treatment of renal cell carcinoma metastasis
KR20150122731A (ko) 2013-03-15 2015-11-02 펀다시오 인스티튜트 드 르세르카 바이오메디카 (아이알비 바르셀로나) 암 전이의 예후 및 치료 방법
WO2015052583A2 (en) 2013-10-09 2015-04-16 Fundacio Institut De Recerca Biomedica (Irb Barcelona) Method for the prognosis and treatment of cancer metastasis
US10035760B2 (en) * 2013-10-24 2018-07-31 Viiv Healthcare Uk (No. 5) Limited Inhibitors of human immunodeficiency virus replication
DE102014116405B4 (de) * 2014-11-10 2018-10-25 Khs Gmbh Druckvorrichtung sowie Verfahren zur Bedruckung von Behältern
MX2017007381A (es) 2014-12-11 2017-11-06 Inbiomotion Sl Miembros de union para homologo del oncogen de fibrosarcoma musculoadoneurotico (c-maf) humano.
JP6929792B2 (ja) 2015-02-16 2021-09-01 ザ ユニバーシティ オブ クィーンズランド スルホニル尿素及び関連化合物並びにその使用
WO2017156071A1 (en) 2016-03-09 2017-09-14 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
ES2877757T3 (es) 2016-05-25 2021-11-17 Inbiomotion Sl Tratamiento terapéutico de cáncer de mama basado en el estado de c-MAF
WO2018009417A1 (en) 2016-07-05 2018-01-11 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
US10292983B2 (en) 2016-08-03 2019-05-21 Cymabay Therapeutics, Inc. Oxymethylene aryl compounds for treating inflammatory gastrointestinal diseases or gastrointestinal conditions
PE20191153A1 (es) * 2016-09-28 2019-09-05 Blade Therapeutics Inc Moduladores de calpainas y usos terapeuticos de los mismos
JP7235742B2 (ja) 2017-07-07 2023-03-08 インフレイゾーム リミテッド 新規なスルホンアミドカルボキサミド化合物
WO2019008029A1 (en) 2017-07-07 2019-01-10 Inflazome Limited SULFONYLURATES AND SULFONYLTHIOURES AS INHIBITORS OF NLRP3
MA49903A (fr) 2017-08-15 2020-06-24 Inflazome Ltd Sulfonylureés et sulfonylthioureés en tant qu'inhibiteurs de nlrp3
WO2019034692A1 (en) 2017-08-15 2019-02-21 Inflazome Limited SULFONYLURATES AND SULFONYLTHIOURES AS INHIBITORS OF NLRP3
TW201910314A (zh) * 2017-08-15 2019-03-16 愛爾蘭商英弗雷佐姆有限公司 新穎化合物
US11926600B2 (en) 2017-08-15 2024-03-12 Inflazome Limited Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors
SG11202003984UA (en) 2017-11-09 2020-05-28 Inflazome Ltd Novel sulfonamide carboxamide compounds
KR20200104298A (ko) 2017-11-22 2020-09-03 인바이오모션 에스.엘. c-MAF 상태에 기반한 유방암의 요법 치료
EP3759077A1 (en) 2018-03-02 2021-01-06 Inflazome Limited Novel compounds
IL309732A (en) 2021-07-09 2024-02-01 Aligos Therapeutics Inc Antiviral compounds
JP2024529062A (ja) * 2021-08-02 2024-08-01 北京華益健康薬物研究中心 コロナウイルス感染症の治療又は予防のための３ｃｌプロテア－ゼ小分子阻害剤及びその用途
CN113563293B (zh) * 2021-08-24 2022-12-30 苏州大学 基于n-氧化物的前药复合物及其制备方法和应用
WO2023043816A1 (en) 2021-09-17 2023-03-23 Aligos Therapeutics, Inc. Anti-viral compounds for treating coronavirus, picornavirus, and norovirus infections
CN115466225A (zh) * 2022-08-16 2022-12-13 中国科学院上海药物研究所 一种酰胺类化合物及其制备方法、药物组合物和用途

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US119788A (en) * 1871-10-10 Improvement in wheels for vehicles
DE3606480A1 (de) * 1986-02-28 1987-09-03 Behringwerke Ag Oligopeptidylnitrilderivate, diese enthaltende mittel, verfahren zu ihrer herstellung und ihre verwendung
JPS63301868A (ja) 1987-06-01 1988-12-08 Nippon Kayaku Co Ltd Ｎ−（２−クロロイソニコチノイル）アミノ酸誘導体およびそれを有効成分とする農園芸用殺菌剤
DE3827415A1 (de) 1988-08-12 1990-02-15 Behringwerke Ag Peptidderivate, verfahren zu ihrer herstellung und ihre verwendung
EP0419683A4 (en) 1989-04-13 1992-03-11 Japan Tobacco Inc. New amino acid derivatives having prolylendopeptidase inhibitor activity
GB8909836D0 (en) 1989-04-28 1989-06-14 Boots Co Plc Therapeutic agent
WO1991018877A1 (fr) * 1990-06-07 1991-12-12 Zeria Pharmaceutical Co., Ltd. Nouveau derive d'arylalcanoylamine et medicament contenant ce derive
HUT74733A (en) 1993-11-09 1997-02-28 Merck & Co Inc Piperidines, pyrrolidines and hexahydro-1h-azepines promote release of growth hormone
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
JPH07228529A (ja) 1994-02-17 1995-08-29 Zeria Pharmaceut Co Ltd コリンエステラーゼ賦活剤
ATE195933T1 (de) 1994-03-10 2000-09-15 Searle & Co L-n6-(1-iminoethyl)lysin - derivate und ihre verwendung als no-synthase - inhibitoren
WO1998001133A1 (fr) * 1996-07-08 1998-01-15 Yamanouchi Pharmaceutical Co., Ltd. Inhibiteurs de la resorption osseuse
DK0933379T3 (da) 1996-08-28 2006-06-26 Shionogi & Co Nye peptidderivater med thiazolyl-alanin-rest
GB9723407D0 (en) * 1997-11-05 1998-01-07 Ciba Geigy Ag Organic compounds
ID24931A (id) * 1997-11-05 2000-08-31 Novartis Ag Dipeptida nitril
US6456502B1 (en) 1998-09-21 2002-09-24 Compaq Computer Corporation Integrated circuit device/circuit board connection apparatus
GB9903861D0 (en) 1999-02-20 1999-04-14 Zeneca Ltd Chemical compounds
WO2000049008A1 (en) 1999-02-20 2000-08-24 Astrazeneca Ab Di- and tripeptide nitrile derivatives as inhibitors of cathepsin l and cathepsin s
AU2560300A (en) 1999-02-20 2000-09-04 Astrazeneca Ab Acetamido acetonitrile derivatives as inhibitors of cathepsin l and/or cathepsins
WO2000051998A1 (en) 1999-03-02 2000-09-08 Boehringer Ingelheim Pharmaceuticals, Inc. Compounds useful as reversible inhibitors of cathepsin s
CA2367348A1 (en) * 1999-03-15 2000-09-21 Axys Pharmaceuticals, Inc. Novel compounds and compositions as protease inhibitors
IL145430A0 (en) * 1999-03-15 2002-06-30 Axys Pharm Inc N-cyanomethyl amides, processes for the preparation thereof and pharmaceutical compositions containing the same
ATE326454T1 (de) 1999-07-30 2006-06-15 Boehringer Ingelheim Pharma Neue bernsteinsäure derivative als cysteine- protease-inhibitoren
PL364045A1 (en) 1999-09-13 2004-12-13 Boehringer Ingelheim Pharmaceuticals, Inc. Novel spiroheterocyclic compounds useful as reversible inhibitors of cysteine proteases
AU7490900A (en) * 1999-09-16 2001-04-17 Axys Pharmaceuticals, Inc. Chemical compounds and compositions and their use as cathepsin s inhibitors
GB9925264D0 (en) 1999-10-26 1999-12-29 Zeneca Ltd Chemical compounds
HU227039B1 (en) 2000-01-25 2010-05-28 Egis Gyogyszergyar Nyilvanosan New process for the production of quetiapine and intermediates therefor
GB0003111D0 (en) 2000-02-10 2000-03-29 Novartis Ag Organic compounds

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