ATE409482T1 - Cathepsincystein-proteasehemmer - Google Patents
Cathepsincystein-proteasehemmerInfo
- Publication number
- ATE409482T1 ATE409482T1 AT02723314T AT02723314T ATE409482T1 AT E409482 T1 ATE409482 T1 AT E409482T1 AT 02723314 T AT02723314 T AT 02723314T AT 02723314 T AT02723314 T AT 02723314T AT E409482 T1 ATE409482 T1 AT E409482T1
- Authority
- AT
- Austria
- Prior art keywords
- protease inhibitors
- cathepsincystein
- compounds
- inhibitors
- cathepsins
- Prior art date
Links
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 102000005600 Cathepsins Human genes 0.000 abstract 1
- 108010084457 Cathepsins Proteins 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- -1 but not limited to Substances 0.000 abstract 1
- 239000002852 cysteine proteinase inhibitor Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000030991 negative regulation of bone resorption Effects 0.000 abstract 1
Classifications
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C07C255/00—Carboxylic acid nitriles
- C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
- C07C255/24—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same saturated acyclic carbon skeleton
- C07C255/29—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the same saturated acyclic carbon skeleton containing cyano groups and acylated amino groups bound to the carbon skeleton
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- C07C323/60—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 atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
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- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
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- C07D211/06—Heterocyclic 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
- C07D211/08—Heterocyclic 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
- C07D211/18—Heterocyclic 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
- C07D211/20—Heterocyclic 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 singly bound oxygen or sulphur atoms
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- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
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- C07D239/32—One oxygen, sulfur or nitrogen atom
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- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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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- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
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- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three 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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- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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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- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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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- C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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- C07D417/00—Heterocyclic 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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- C07D417/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/10—Heterocyclic 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 carbon chain containing aromatic rings
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
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- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
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- C07C2601/00—Systems containing only non-condensed rings
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- C—CHEMISTRY; METALLURGY
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- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Indole Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Furan Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
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Applications Claiming Priority (1)
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| US27279901P | 2001-03-02 | 2001-03-02 |
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| DE (1) | DE60229114D1 (de) |
| WO (1) | WO2002069901A2 (de) |
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| NZ534583A (en) * | 2002-03-05 | 2006-11-30 | Axys Pharm Inc | Leucinamide derivatives suitable as cathepsin cysteine protease inhibitors |
| AU2003266052B2 (en) * | 2002-09-04 | 2009-04-23 | Merck Frosst Canada Ltd | Cathepsin cysteine protease inhibitors |
| SE0203712D0 (sv) * | 2002-12-13 | 2002-12-13 | Astrazeneca Ab | Novel compounds |
| 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 |
| CA2526694A1 (en) | 2003-06-04 | 2004-12-16 | John W. Patterson | Amidino compounds as cysteine protease inhibitors |
| US7173051B2 (en) | 2003-06-13 | 2007-02-06 | Irm, Llc | Inhibitors of cathepsin S |
| JP4690319B2 (ja) * | 2003-06-30 | 2011-06-01 | メルク フロスト カナダ リミテツド | カテプシンシステインプロテアーゼ阻害剤 |
| JP4692281B2 (ja) | 2003-08-05 | 2011-06-01 | 味の素株式会社 | 新規アゾール化合物 |
| US7256207B2 (en) | 2003-08-20 | 2007-08-14 | Irm Llc | Inhibitors of cathepsin S |
| JP4553899B2 (ja) * | 2003-08-21 | 2010-09-29 | メルク フロスト カナダ リミテツド | カテプシンシステインプロテアーゼ阻害剤 |
| EP1660436A4 (de) * | 2003-08-27 | 2006-11-22 | Merck Frosst Canada Ltd | Cathepsininhibitoren |
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| EP1939181A1 (de) * | 2006-12-27 | 2008-07-02 | sanofi-aventis | Heteroaryl-substituierte Carboxamide und deren Verwendung für die Stimulierung der NO Synthase Expression |
| BRPI0807477A2 (pt) * | 2007-02-14 | 2014-05-13 | Karolinska Innovations Ab | Uso de um polipeptídeo isolado, polipeptídeo isolado, composição farmacêutica, e, métdo de tratamento de um mamífero |
| CA2689945A1 (en) | 2007-06-26 | 2008-12-31 | Astrazeneca Ab | 1-cyanocyclopropyl-derivatives as cathepsin k inhibitors |
| EP2489656A1 (de) | 2007-12-21 | 2012-08-22 | Ligand Pharmaceuticals Inc. | Selektive Androgenrezeptormodulatoren (SARMS) und ihre Verwendung |
| JP5185697B2 (ja) | 2008-05-28 | 2013-04-17 | ルネサスエレクトロニクス株式会社 | 表示装置、表示パネルドライバ、表示パネルの駆動方法、及び表示パネルドライバへの画像データ供給方法 |
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| US8999975B2 (en) * | 2011-09-19 | 2015-04-07 | Boehringer Ingelheim International Gmbh | Substituted N- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin C |
| MY176004A (en) | 2013-02-22 | 2020-07-21 | Samumed Llc | Gamma-diketones as wnt/beta-catenin signaling pathway activators |
| JP6527851B2 (ja) | 2013-03-12 | 2019-06-05 | セルタクシス,インコーポレイテッド | ロイコトリエンa4加水分解酵素を阻害する方法 |
| AU2014230814B2 (en) * | 2013-03-14 | 2017-12-21 | Boehringer Ingelheim International Gmbh | Substituted 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of Cathepsin C |
| US8877775B2 (en) | 2013-03-14 | 2014-11-04 | Boehringer Ingelheim International Gmbh | Substituted 2-aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C |
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| EP2970309A4 (de) | 2013-03-14 | 2016-11-09 | Celtaxsys Inc | Inhibitoren der leukotrien-a4-hydrolase |
| EP2970230B1 (de) | 2013-03-14 | 2019-05-22 | Boehringer Ingelheim International GmbH | Substituierte bicyclische 1-carbonsäure (benzyl-cyano-methyl)amid-inhibitoren von cathepsin c |
| EP2970228B1 (de) * | 2013-03-14 | 2017-05-10 | Boehringer Ingelheim International GmbH | Substituierte 2-aza-bicyclo[2.2.1]heptan-3-carboxylsäure (cyan-methyl)-amid-hemmstoffen von cathepsin c |
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| JP6529575B2 (ja) | 2014-08-01 | 2019-06-12 | 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 | 置換オキセタンおよびそれらのカテプシンcの阻害薬としての使用 |
| EP3206686B1 (de) | 2014-08-20 | 2019-10-09 | Samumed, LLC | Gamma-diketone zur behandlung und vorbeugung von hautalterung und hautfalten |
| KR102510588B1 (ko) | 2014-09-12 | 2023-03-17 | 베링거 인겔하임 인터내셔날 게엠베하 | 카텝신 c의 스피로사이클릭 억제제 |
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| US10494364B2 (en) | 2015-08-29 | 2019-12-03 | Sunshin Lake Pharma Co., Ltd | Cathepsin K inhibitors and application thereof |
| RS64006B1 (sr) * | 2017-05-23 | 2023-03-31 | H Lundbeck As | Pirazol magl inhibitori |
| US10927105B1 (en) | 2017-05-23 | 2021-02-23 | Lundbeck La Jolla Research Center, Inc. | Pyrazole MAGL inhibitors |
| AU2019278935B2 (en) | 2018-05-31 | 2025-02-13 | Celltaxis, Llc | Method of reducing pulmonary exacerbations in respiratory disease patients |
| CA3133929A1 (en) | 2019-04-19 | 2020-10-22 | Lin Zhi | Crystalline forms and methods of producing crystalline forms of a compound |
| UY39276A (es) | 2020-06-19 | 2022-01-31 | Bayer Ag | Uso de compuestos de 1,3,4–oxadiazol–2–ilpirimidina para controlar microorganismos fitopatógenos, métodos de uso y composiciones. |
| CN115466225B (zh) * | 2022-08-16 | 2025-03-07 | 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 |
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| BR9813197A (pt) | 1997-11-05 | 2000-08-29 | Novartis Ag | Dipeptìdeo nitrilas |
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| AU2560000A (en) | 1999-02-20 | 2000-09-04 | Astrazeneca Ab | Di- and tripeptide nitrile derivatives as inhibitors of cathepsin l and cathepsin |
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| US6849605B1 (en) * | 1999-03-05 | 2005-02-01 | The Trustees Of University Technology Corporation | Inhibitors of serine protease activity, methods and compositions for treatment of viral infections |
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| AU4213500A (en) * | 1999-04-09 | 2000-11-14 | Cytovia, Inc. | Caspase inhibitors and the use thereof |
| US6617426B1 (en) * | 1999-06-22 | 2003-09-09 | Merck & Co Inc | Cysteinyl protease inhibitors |
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| GB9917909D0 (en) * | 1999-07-31 | 1999-09-29 | Synphar Lab Inc | Cysteine protease inhibitors |
| US6420364B1 (en) * | 1999-09-13 | 2002-07-16 | Boehringer Ingelheim Pharmaceuticals, Inc. | Compound useful as reversible inhibitors of cysteine proteases |
| WO2001068645A2 (en) | 2000-03-15 | 2001-09-20 | Axys Pharmaceuticals, Inc. | N-cyanomethylcarboxamides and their use as protease inhibitors |
| AU2001256981A1 (en) * | 2000-04-06 | 2001-10-23 | Axys Pharmaceuticals, Inc. | Cathepsin cysteine protease inhibitors |
| AU9521401A (en) | 2000-05-15 | 2001-11-26 | Novartis Ag | N-substituted peptidyl nitriles as cysteine cathepsin inhibitors |
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| US6878706B1 (en) * | 2002-04-05 | 2005-04-12 | Boehringer Ingelheim Pharmaceuticals Inc. | Cyanamides useful as reversible inhibitors of cysteine proteases |
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| WO2002069901A3 (en) | 2003-10-30 |
| US7012075B2 (en) | 2006-03-14 |
| CA2439415A1 (en) | 2002-09-12 |
| WO2002069901A2 (en) | 2002-09-12 |
| JP2004531486A (ja) | 2004-10-14 |
| US20040198982A1 (en) | 2004-10-07 |
| EP1372655A2 (de) | 2004-01-02 |
| JP4365094B2 (ja) | 2009-11-18 |
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