ZA200107494B - N-cyanomethylamides as protease inhibitors. - Google Patents

N-cyanomethylamides as protease inhibitors. Download PDF

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Publication number
ZA200107494B
ZA200107494B ZA200107494A ZA200107494A ZA200107494B ZA 200107494 B ZA200107494 B ZA 200107494B ZA 200107494 A ZA200107494 A ZA 200107494A ZA 200107494 A ZA200107494 A ZA 200107494A ZA 200107494 B ZA200107494 B ZA 200107494B
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South Africa
Prior art keywords
alkyl
substituted
hydrogen
halo
hetero
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ZA200107494A
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English (en)
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Clifford M Bryant
James T Palmer
Robert M Rydzewski
Eduardo L Setti
Zong-Qiang Tian
Shankar Venkatraman
Dan-Xiong Wang
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Axys Pharm Inc
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Publication of ZA200107494B publication Critical patent/ZA200107494B/en

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ZA200107494A 1999-03-15 2001-09-11 N-cyanomethylamides as protease inhibitors. ZA200107494B (en)

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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
JP2002539192A (ja) * 1999-03-15 2002-11-19 アクシス・ファーマシューティカルズ・インコーポレイテッド プロテアーゼ阻害剤としての新規な化合物及び組成物
EP1218372B1 (fr) * 1999-09-13 2003-07-02 Boehringer Ingelheim Pharmaceuticals, Inc. Composes heterocycliques utiles comme inhibiteurs reversibles des cysteine proteases
US6420364B1 (en) 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
US6492362B1 (en) * 1999-09-16 2002-12-10 Axys Pharmaceuticals, Inc. Compounds and compositions as cathepsin S inhibitors
GB9928330D0 (en) * 1999-11-30 2000-01-26 Ferring Bv Novel antidiabetic agents
WO2001047886A1 (fr) 1999-12-24 2001-07-05 F. Hoffmann-La Roche Ag Derives du nitrile en tant qu'inhibiteurs de la cathepsine k
AU779855B2 (en) * 2000-01-06 2005-02-17 Axys Pharmaceuticals, Inc. Novel compounds and compositions as protease inhibitors
GB0003111D0 (en) * 2000-02-10 2000-03-29 Novartis Ag Organic compounds
WO2001068645A2 (fr) * 2000-03-15 2001-09-20 Axys Pharmaceuticals, Inc. Composes et compositions agissant comme inhibiteurs de proteines
MXPA02009382A (es) * 2000-03-27 2003-01-28 Applied Research Systems Derivados de pirrolidina farmaceuticamente activos.
WO2001074769A1 (fr) * 2000-03-27 2001-10-11 Applied Research Systems Ars Holding N.V. Derives de la pyrrolidine pharmaceutiquement actifs comme inhibiteurs de bax
AU9521401A (en) * 2000-05-15 2001-11-26 Novartis Ag N-substituted peptidyl nitriles as cysteine cathepsin inhibitors
ATE440096T1 (de) 2000-12-08 2009-09-15 Takeda Pharmaceutical Substituierte thiazolderivate mit 3- pyridylgruppen, verfahren zu deren herstellung und deren verwendung
MXPA03005601A (es) * 2000-12-22 2004-12-02 Axys Pharm Inc Nuevos compuestos y composiciones como inhibidores de catepsina.
US7030116B2 (en) * 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
AU2002254099B2 (en) 2001-03-02 2006-07-06 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
NZ528944A (en) * 2001-06-01 2007-09-28 Axys Pharm Inc Chemical compounds and pharmaceutical compositions as cathepsin S inhibitors
US20040147503A1 (en) * 2002-06-04 2004-07-29 Sheila Zipfeil Novel compounds and compositions as cathepsin inhibitors
CN1324008C (zh) * 2001-09-14 2007-07-04 安万特药物公司 作为组织蛋白酶抑制剂的新化合物和组合物
EP1434769A2 (fr) 2001-10-02 2004-07-07 Boehringer Ingelheim Pharmaceuticals Inc. Composes utiles comme inhibiteurs reversibles de cysteine protease
WO2003037892A1 (fr) 2001-10-29 2003-05-08 Boehringer Ingelheim Pharmaceuticals, Inc. Composes convenant comme inhibiteurs reversibles de proteases de la cysteine
JP2005511593A (ja) * 2001-11-08 2005-04-28 メルク　エンド　カムパニー　インコーポレーテッド 骨粗鬆症を治療するための組成物及び方法
WO2003041649A2 (fr) 2001-11-13 2003-05-22 Merck Frosst Canada & Co. Derives cyanoalkylamino utilises comme inhibiteurs de la protease
WO2003042197A1 (fr) * 2001-11-14 2003-05-22 Aventis Pharmaceuticals Inc. Nouveaux composes et compositions jouant le role d'inhibiteurs de cathepsine s
US7727964B2 (en) 2001-11-26 2010-06-01 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
EP1485106A2 (fr) * 2002-02-19 2004-12-15 Ilex Products, Inc. Phosphonate-phosphate et modulateurs d'apolipoproteine e diphosphonate
PT1482924E (pt) * 2002-03-05 2008-08-27 Axys Pharm Inc Inibidores de proteases da cisteína catepsina
WO2003075853A2 (fr) 2002-03-08 2003-09-18 Bristol-Myers Squibb Company Derives cycliques servant de modulateurs de l'activite du recepteur de la chimiokine
SE0201977D0 (sv) * 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
SE0201976D0 (sv) * 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
SE0201980D0 (sv) 2002-06-24 2002-06-24 Astrazeneca Ab Novel compounds
EP1537074B1 (fr) * 2002-09-04 2019-02-27 Merck Canada Inc. Inhibiteurs de proteases a cysteine de type cathepsine
WO2004052921A1 (fr) * 2002-12-05 2004-06-24 Axys Pharmaceuticals, Inc. Derives de cyanomethyle en tant qu'inhibiteurs de la protease a cysteine
US7384970B2 (en) * 2003-03-24 2008-06-10 Irm Llc Inhibitors of cathepsin S
US7109243B2 (en) * 2003-03-24 2006-09-19 Irm Llc Inhibitors of cathepsin S
CA2526694A1 (fr) * 2003-06-04 2004-12-16 John W. Patterson Composes amidino servant d'inhibiteurs de proteases a cysteine
US7173051B2 (en) * 2003-06-13 2007-02-06 Irm, Llc Inhibitors of cathepsin S
US7332485B2 (en) * 2003-07-08 2008-02-19 Smithkline Beecham Corp Peptide deformylase inhibitors
US7256207B2 (en) 2003-08-20 2007-08-14 Irm Llc Inhibitors of cathepsin S
EP1673336B1 (fr) * 2003-08-21 2014-06-04 Merck Canada Inc. Inhibiteurs de cathepsine et de cysteine protease
SG146658A1 (en) 2003-09-18 2008-10-30 Schering Ag Haloalkyl containing compounds as cysteine protease inhibitors
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
RU2346943C2 (ru) 2003-10-24 2009-02-20 Авентис Фармасьютикалз Инк. Новые соединения и композиции в качестве ингибиторов катепсина
EP1689403A4 (fr) * 2003-11-10 2007-09-05 Synta Pharmaceuticals Corp Composes heteroaryle-hydrazone
WO2006042103A2 (fr) * 2004-10-05 2006-04-20 Axys Pharmaceuticals, Inc. Inhibiteurs reversibles de la cathepsine b
US8163735B2 (en) 2004-12-02 2012-04-24 Virobay, Inc. Sulfonamide compounds as cysteine protease inhibitors
WO2006062876A2 (fr) 2004-12-09 2006-06-15 Merck & Co., Inc. Modulateurs du recepteur de l'oestrogene
BRPI0609695A2 (pt) 2005-03-21 2011-10-18 Applera Corp composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, método para tratar uma doença e uma paciente sofrendo uma terapia
WO2006102535A2 (fr) 2005-03-22 2006-09-28 Celera Genomics Composes contenant du sulfonyle en tant qu'inhibiteurs de cysteine proteases
AU2006239929B2 (en) 2005-04-22 2011-11-03 Alantos Pharmaceuticals Holding, Inc. Dipeptidyl peptidase-IV inhibitors
EP1760076A1 (fr) 2005-09-02 2007-03-07 Ferring B.V. Inhibiteur de FAP
WO2007137738A1 (fr) 2006-06-01 2007-12-06 Sanofi-Aventis Nitriles spirocycliques en tant qu'inhibiteurs de protéase
CA2664878A1 (fr) 2006-10-04 2008-04-10 Virobay, Inc. Composes contenant un di-fluoro en tant qu'inhibiteurs de cysteine-protease
US7893112B2 (en) 2006-10-04 2011-02-22 Virobay, Inc. Di-fluoro containing compounds as cysteine protease inhibitors
WO2008079371A1 (fr) * 2006-12-22 2008-07-03 Encysive Pharmaceuticals, Inc. Modulateurs du récepteur du c3a et leurs procédés d'utilisation
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
AU2008222812B2 (en) * 2007-03-08 2012-03-22 Irm Llc Compounds and compositions as modulators of GPR119 activity
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 (fr) 2008-01-09 2015-07-15 Amura Therapeutics Limited DÉRIVÉS DE TÉTRAHYDROFURO(2,3-b)PYRROL-3-ONE COMME INHIBITEURS DE CYSTÉINE PROTÉINASES
WO2010045190A1 (fr) * 2008-10-15 2010-04-22 Boehringer Ingelheim International Gmbh Composés de diamide d’hétéroaryle fusionnés utilisés comme inhibiteurs de mmp-13
EP2198879A1 (fr) 2008-12-11 2010-06-23 Institut Curie Agent modulateur de CD74 pour la régulation de la migration de cellules dendritiques et dispositif pour l'étude de la capacité de motilité d'une cellule
UA106748C2 (uk) * 2009-04-20 2014-10-10 Ф. Хоффманн-Ля Рош Аг Похідні проліну як інгібітори катепсину
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
US8410127B2 (en) 2009-10-01 2013-04-02 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
US10047398B2 (en) 2010-10-06 2018-08-14 Fundacio Institut De Recerca Biomedica (Irb Barcelona) Method for the diagnosis, prognosis and treatment of breast cancer metastasis
US9943522B2 (en) 2011-05-16 2018-04-17 Bayer Intellectual Property Gmbh Use of cathepsin K inhibition for the treatment and/or prophylaxis of pulmonary hypertension and/or heart failure
EP2650682A1 (fr) 2012-04-09 2013-10-16 Fundació Privada Institut de Recerca Biomèdica Esters asymétriques d'acides gras utiles en tant que lubrifiants
JP6386450B2 (ja) 2012-06-06 2018-09-05 フンダシオ、インスティトゥト、デ、レセルカ、ビオメディカ（イエレベ、バルセロナ）Ｆｕｎｄａｃｉｏ Ｉｎｓｔｉｔｕｔ Ｄｅ Ｒｅｃｅｒｃａ Ｂｉｏｍｅｄｉｃａ （Ｉｒｂ Ｂａｒｃｅｌｏｎａ） 肺がん転移の診断、予後診断および処置のための方法
AR091857A1 (es) * 2012-07-25 2015-03-04 Sova Pharmaceuticals Inc INHIBIDORES DE CISTATIONIN-g-LIASA (CSE)
US10119171B2 (en) 2012-10-12 2018-11-06 Inbiomotion S.L. Method for the diagnosis, prognosis and treatment of prostate cancer metastasis
DK2906718T3 (da) 2012-10-12 2019-07-01 Inbiomotion Sl Fremgangsmåde til diagnose, prognose og behandling af prostatakræftmetastase under anvendelse af c-maf
US20160032399A1 (en) 2013-03-15 2016-02-04 Inbiomotion S.L. Method for the Prognosis and Treatment of Renal Cell Carcinoma Metastasis
JP6577873B2 (ja) 2013-03-15 2019-09-18 フンダシオ、インスティトゥト、デ、レセルカ、ビオメディカ（イエレベ、バルセロナ）Ｆｕｎｄａｃｉｏ Ｉｎｓｔｉｔｕｔ Ｄｅ Ｒｅｃｅｒｃａ Ｂｉｏｍｅｄｉｃａ （Ｉｒｂ Ｂａｒｃｅｌｏｎａ） がんの転移の予後診断および処置のための方法
CA2926894A1 (fr) 2013-10-09 2015-04-16 Fundacio Institut De Recerca Biomedica (Irb Barcelona) Methode de pronostic et de traitement d'une metastase cancereuse
WO2015061518A1 (fr) * 2013-10-24 2015-04-30 Bristol-Myers Squibb Company Inhibiteurs de réplication du virus de l'immunodéficience humaine
DE102014116405B4 (de) * 2014-11-10 2018-10-25 Khs Gmbh Druckvorrichtung sowie Verfahren zur Bedruckung von Behältern
KR20170093182A (ko) 2014-12-11 2017-08-14 인바이오모션 에스.엘. 인간 c-maf에 대한 결합 구성원
US10538487B2 (en) 2015-02-16 2020-01-21 The University Of Queensland Sulfonylureas and related compounds and use of same
US10590084B2 (en) 2016-03-09 2020-03-17 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
KR102571924B1 (ko) 2016-05-25 2023-08-28 인바이오모션 에스.엘. c-MAF 상태에 기초한 유방암의 치료
WO2018009417A1 (fr) 2016-07-05 2018-01-11 Blade Therapeutics, Inc. Modulateurs de calpain et leurs utilisations thérapeutiques
WO2018026890A1 (fr) 2016-08-03 2018-02-08 Cymabay Therapeutics Composés d'aryle d'oxyméthylène pour le traitement de maladies gastro-intestinales inflammatoires ou de troubles gastro-intestinaux
KR20190063473A (ko) 2016-09-28 2019-06-07 블레이드 테라퓨틱스, 인크. 칼페인 조정자 및 그 치료학적 용도
US11370776B2 (en) 2017-07-07 2022-06-28 Inflazome Limited Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors
HRP20220195T1 (hr) 2017-07-07 2022-04-15 Inflazome Limited Novi spojevi sulfonamid karboksamida
WO2019034692A1 (fr) 2017-08-15 2019-02-21 Inflazome Limited Sulfonylurées et sulfonylthiourées en tant qu'inhibiteurs de nlrp3
JP2020531453A (ja) 2017-08-15 2020-11-05 インフレイゾーム リミテッド Ｎｌｒｐ３阻害剤としてのスルホニルウレアおよびスルホニルチオウレア
RU2020110366A (ru) * 2017-08-15 2021-09-16 Инфлазоум Лимитед Новые соединения сульфонамидкарбоксамидов
US11926600B2 (en) 2017-08-15 2024-03-12 Inflazome Limited Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors
EP3707134A1 (fr) 2017-11-09 2020-09-16 Inflazome Limited Nouveaux composés de sulfonamide carboxamide
EP3713581A1 (fr) 2017-11-22 2020-09-30 Inbiomotion S.L. Traitement thérapeutique du cancer du sein basé sur le c-maf
WO2019166619A1 (fr) 2018-03-02 2019-09-06 Inflazome Limited Nouveaux composés
AU2022306289A1 (en) 2021-07-09 2024-01-18 Aligos Therapeutics, Inc. Anti-viral compounds
CN117836272A (zh) * 2021-08-02 2024-04-05 北京华益健康药物研究中心 用于治疗或预防冠状病毒感染的3cl蛋白酶小分子抑制剂及其用途
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
US12065428B2 (en) 2021-09-17 2024-08-20 Aligos Therapeutics, Inc. Anti-viral compounds
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
AU643300B2 (en) 1990-06-07 1993-11-11 Zeria Pharmaceutical Co., Ltd. Novel arylalkanoylamine derivative and drug containing the same
CZ134296A3 (en) 1993-11-09 1996-12-11 Merck & Co Inc Piperidine, pyrrolidine and hexahydro-1h-azepine derivatives, process of their preparation and pharmaceutical compositions containing thereof
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
DE69518631T2 (de) 1994-03-10 2001-01-11 G.D. Searle & Co., Chicago L-n6-(1-iminoethyl)lysin - derivate und ihre verwendung als no-synthase - inhibitoren
AU3359697A (en) * 1996-07-08 1998-02-02 Yamanouchi Pharmaceutical Co., Ltd. Bone resorption inhibitors
AU713133B2 (en) 1996-08-28 1999-11-25 Shionogi & Co., Ltd. Novel peptide derivatives having thiazolyl-alanine residue
GB9723407D0 (en) * 1997-11-05 1998-01-07 Ciba Geigy Ag Organic compounds
PL202226B1 (pl) * 1997-11-05 2009-06-30 Novartis Ag Nitryl dipeptydowy, jego zastosowanie lecznicze i zawierająca go kompozycja farmaceutyczna
US6456502B1 (en) 1998-09-21 2002-09-24 Compaq Computer Corporation Integrated circuit device/circuit board connection apparatus
EP1155010A1 (fr) 1999-02-20 2001-11-21 AstraZeneca AB Derives acetamido acetonitriles en tant qu'inhibiteurs de la cathepsine l et/ou s
WO2000049008A1 (fr) 1999-02-20 2000-08-24 Astrazeneca Ab Derives nitriles di- et tripeptidiques, utiles en tant qu'inhibiteurs des cathepsines l et s
GB9903861D0 (en) 1999-02-20 1999-04-14 Zeneca Ltd Chemical compounds
US6395897B1 (en) * 1999-03-02 2002-05-28 Boehringer Ingelheim Pharmaceuticals, Inc. Nitrile compounds useful as reversible inhibitors of #9 cathepsin 5
AU779177B2 (en) 1999-03-15 2005-01-13 Axys Pharmaceuticals, Inc. Novel compounds and compositions as protease inhibitors
JP2002539192A (ja) * 1999-03-15 2002-11-19 アクシス・ファーマシューティカルズ・インコーポレイテッド プロテアーゼ阻害剤としての新規な化合物及び組成物
WO2001009110A1 (fr) 1999-07-30 2001-02-08 Boehringer Ingelheim Pharmaceuticals, Inc. Nouveaux composes de derives de succinate utilises comme inhibiteurs des cysteine proteases
EP1218372B1 (fr) 1999-09-13 2003-07-02 Boehringer Ingelheim Pharmaceuticals, Inc. Composes heterocycliques utiles comme inhibiteurs reversibles des cysteine proteases
US6492362B1 (en) * 1999-09-16 2002-12-10 Axys Pharmaceuticals, Inc. Compounds and compositions 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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