AR032136A1 - Compuestos espiroheterociclicos utiles como inhibidores reversibles de cisteina-proteasas - Google Patents

Compuestos espiroheterociclicos utiles como inhibidores reversibles de cisteina-proteasas

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Publication number
AR032136A1
AR032136A1 ARP000104795A ARP000104795A AR032136A1 AR 032136 A1 AR032136 A1 AR 032136A1 AR P000104795 A ARP000104795 A AR P000104795A AR P000104795 A ARP000104795 A AR P000104795A AR 032136 A1 AR032136 A1 AR 032136A1
Authority
AR
Argentina
Prior art keywords
compounds
reversible
useful
espiroheterociclic
cisteine
Prior art date
Application number
ARP000104795A
Other languages
English (en)
Inventor
Leah Lynn Frye
Eugene Richard Hickey
Weimin Liu
Tina Marie Morwick
Denice Mary Spero
Sanxing Sun
Yancey David Ward
Michel Jose Emmanuel
David S Thomson
Young Erick Richard Rouch
Original Assignee
Boehringer Ingelheim Pharma
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.)
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Publication date
Application filed by Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of AR032136A1 publication Critical patent/AR032136A1/es

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Abstract

Se describen compuestos inhibidores reversibles de cathepsina S, de formulas (1), (2), (3) y (4), en donde los substituyentes R1, R2, R3, R4, R5, R6, R8, Het, X e Y tienen los significados indicados en la memoria descriptiva. Estos compuestos son inhibidores reversibles de la cisteína-proteasa cathepsina S, K, F, L, B, y son utiles, por lo tanto, en el tratamiento de enfermedades autoinmunes y otras enfermedades relacionadas. También se describen procedimientos para preparar tales compuestos, las composiciones farmacéuticas que los contienen y el uso de los mismos para preparar un medicamento destinado a tratar las enfermedades mencionadas más arriba.
ARP000104795A 1999-09-13 2000-09-13 Compuestos espiroheterociclicos utiles como inhibidores reversibles de cisteina-proteasas AR032136A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15373899P 1999-09-13 1999-09-13
US22290000P 2000-08-03 2000-08-03

Publications (1)

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AR032136A1 true AR032136A1 (es) 2003-10-29

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ARP000104795A AR032136A1 (es) 1999-09-13 2000-09-13 Compuestos espiroheterociclicos utiles como inhibidores reversibles de cisteina-proteasas

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EP (1) EP1218372B1 (es)
JP (1) JP2003529546A (es)
KR (1) KR20030024651A (es)
CN (1) CN100410250C (es)
AR (1) AR032136A1 (es)
AT (1) ATE244235T1 (es)
AU (1) AU782246B2 (es)
BG (1) BG106483A (es)
BR (1) BR0013966A (es)
CA (1) CA2385130C (es)
CZ (1) CZ2002844A3 (es)
DE (1) DE60003702T2 (es)
DK (1) DK1218372T3 (es)
EE (1) EE200200132A (es)
ES (1) ES2199856T3 (es)
HK (1) HK1048807A1 (es)
HR (1) HRP20020221A2 (es)
HU (1) HUP0302380A2 (es)
IL (2) IL148184A0 (es)
MY (1) MY122696A (es)
NO (1) NO323354B1 (es)
NZ (1) NZ518255A (es)
PL (1) PL364045A1 (es)
PT (1) PT1218372E (es)
RU (1) RU2255937C2 (es)
SA (1) SA00210456B1 (es)
SK (1) SK286463B6 (es)
TW (1) TWI230159B (es)
WO (1) WO2001019816A1 (es)
YU (1) YU17402A (es)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1161415B1 (en) 1999-03-15 2005-07-13 Axys Pharmaceuticals, Inc. N-cyanomethylamides as protease inhibitors
US6420364B1 (en) * 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
US7030116B2 (en) 2000-12-22 2006-04-18 Aventis Pharmaceuticals Inc. Compounds and compositions as cathepsin inhibitors
AR036375A1 (es) 2001-08-30 2004-09-01 Novartis Ag Compuestos pirrolo [2,3-d] pirimidina -2- carbonitrilo, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos compuestos para la preparacion de medicamentos
WO2003024924A1 (en) 2001-09-14 2003-03-27 Aventis Pharmaceuticals Inc. Novel compounds and compositions as cathepsin inhibitors
EP1434769A2 (en) * 2001-10-02 2004-07-07 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
RU2004117877A (ru) 2001-11-14 2006-01-10 Авентис Фармасьютикалз Инк. (Us) Олигопептиды и композиции, содержащие их, в качестве ингибиторов катепсина s
US7087604B2 (en) 2002-03-08 2006-08-08 Bristol-Myers Squibb Company Cyclic derivatives as modulators of chemokine receptor activity
WO2004000838A1 (en) * 2002-06-24 2003-12-31 Axys Pharmaceuticals, Inc. Peptidic compounds as cysteine protease inhibitors
CA2507501C (en) 2002-11-27 2011-10-04 Incyte Corporation 3-aminopyrrolidine derivatives as modulators of chemokine receptors
CA2506114A1 (en) * 2002-12-05 2004-06-24 Axys Pharmaceuticals, Inc. Cyanomethyl derivatives as cysteine protease inhibitors
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
US7662849B2 (en) 2003-06-04 2010-02-16 Virobay, Inc. Amidino compounds as cysteine protease inhibitors
US7173051B2 (en) 2003-06-13 2007-02-06 Irm, Llc Inhibitors of cathepsin S
US7256207B2 (en) 2003-08-20 2007-08-14 Irm Llc Inhibitors of cathepsin S
PT1663958E (pt) * 2003-09-18 2015-06-01 Virobay Inc Compostos contendo haloalquilo como inibidores de protease de cisteína
US7297714B2 (en) * 2003-10-21 2007-11-20 Irm Llc Inhibitors of cathepsin S
JP5154944B2 (ja) 2004-12-02 2013-02-27 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インヒビターとしてのスルホンアミド含有化合物
DK1865940T3 (da) 2005-03-21 2013-03-04 Virobay Inc Alfaketoamidforbindelser som cysteinproteasehæmmere
CA2602112A1 (en) 2005-03-22 2006-09-28 Celera Genomics Sulfonyl containing compounds as cysteine protease inhibitors
EP1896032B1 (en) * 2005-06-14 2012-10-31 Merck Sharp & Dohme Corp. The preparation and use of compounds as protease inhibitors
WO2007053499A2 (en) 2005-11-01 2007-05-10 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of ccr2
US8067457B2 (en) 2005-11-01 2011-11-29 Millennium Pharmaceuticals, Inc. Compounds useful as antagonists of CCR2
AR059035A1 (es) * 2006-01-16 2008-03-12 Syngenta Participations Ag Insecticidas derivados de antranilamida
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
DK2079683T3 (en) 2006-10-04 2015-04-27 Virobay Inc Difluoro-containing compounds as cysteine protease inhibitors
DE102006057036A1 (de) * 2006-12-04 2008-06-05 Bayer Cropscience Ag Biphenylsubstituierte spirocyclische Ketoenole
WO2009087379A2 (en) 2008-01-09 2009-07-16 Amura Therapeutics Limited Tetrahydrofuro (3, 2 -b) pyrrol- 3 -one derivatives as inhibitors of cysteine proteinases
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
WO2012151319A1 (en) 2011-05-02 2012-11-08 Virobay, Inc. Cathepsin inhibitors for the treatment of bone cancer and bone cancer pain
CN104744315A (zh) 2011-06-07 2015-07-01 株式会社吴羽 氧杂环丁烷化合物的制造方法、唑甲基环戊醇化合物的制造方法、以及中间体化合物
EP2537532A1 (en) 2011-06-22 2012-12-26 J. Stefan Institute Cathepsin-binding compounds bound to a nanodevice and their diagnostic and therapeutic use
JP6083818B2 (ja) 2011-11-18 2017-02-22 ヘプタレス セラピューティクス リミテッドHeptares Therapeutics Limited ムスカリンm1受容体アゴニスト
GB201404922D0 (en) 2014-03-19 2014-04-30 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201513743D0 (en) 2015-08-03 2015-09-16 Heptares Therapeutics Ltd Muscarinic agonists
GB201519352D0 (en) 2015-11-02 2015-12-16 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201617454D0 (en) * 2016-10-14 2016-11-30 Heptares Therapeutics Limited Pharmaceutical compounds
GB201810239D0 (en) 2018-06-22 2018-08-08 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819960D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB201819961D0 (en) 2018-12-07 2019-01-23 Heptares Therapeutics Ltd Pharmaceutical compounds
GB202020191D0 (en) 2020-12-18 2021-02-03 Heptares Therapeutics Ltd Pharmaceutical compounds
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
KR20230040386A (ko) * 2020-06-09 2023-03-22 파르데스 바이오사이언시스, 인크. 시스테인 프로테아제의 억제제 및 이의 사용 방법
WO2022192562A1 (en) * 2021-03-10 2022-09-15 Vincere Biosciences, Inc. Usp30 inhibitors and uses thereof
WO2023044171A1 (en) * 2021-09-20 2023-03-23 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9208383D0 (en) * 1992-04-16 1992-06-03 Ici Plc Substituted ketones
US5776718A (en) * 1995-03-24 1998-07-07 Arris Pharmaceutical Corporation Reversible protease inhibitors
JPH11503417A (ja) * 1995-03-24 1999-03-26 アリス・ファーマシューティカル・コーポレイション 可逆的プロテアーゼインヒビター
TW438591B (en) * 1995-06-07 2001-06-07 Arris Pharm Corp Reversible cysteine protease inhibitors
EP1161415B1 (en) * 1999-03-15 2005-07-13 Axys Pharmaceuticals, Inc. N-cyanomethylamides as protease inhibitors

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