CN101969973B - 组织蛋白酶b抑制剂 - Google Patents
组织蛋白酶b抑制剂 Download PDFInfo
- Publication number
- CN101969973B CN101969973B CN200980109079.9A CN200980109079A CN101969973B CN 101969973 B CN101969973 B CN 101969973B CN 200980109079 A CN200980109079 A CN 200980109079A CN 101969973 B CN101969973 B CN 101969973B
- Authority
- CN
- China
- Prior art keywords
- tert
- base
- pyrrolidine
- cyclopropylamino
- formula
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Fee Related
Links
- 0 CC*[C@@](*)NC([C@](C[C@@](*CC*)C1)N1C(C1(**)CC1)=O)=O Chemical compound CC*[C@@](*)NC([C@](C[C@@](*CC*)C1)N1C(C1(**)CC1)=O)=O 0.000 description 5
- QIFVYIVGMIOTJC-DOMZBBRYSA-N CC(C)(C)OC(N(C[C@@H](C1)Oc2nc(-c3ncccc3)nc3c2cc[s]3)[C@@H]1C(O)=O)=O Chemical compound CC(C)(C)OC(N(C[C@@H](C1)Oc2nc(-c3ncccc3)nc3c2cc[s]3)[C@@H]1C(O)=O)=O QIFVYIVGMIOTJC-DOMZBBRYSA-N 0.000 description 1
- MZMNEDXVUJLQAF-YUMQZZPRSA-N CC(C)(C)OC(N(C[C@H](C1)O)[C@@H]1C(OC)=O)=O Chemical compound CC(C)(C)OC(N(C[C@H](C1)O)[C@@H]1C(OC)=O)=O MZMNEDXVUJLQAF-YUMQZZPRSA-N 0.000 description 1
- FBGKHCCKXVRREA-QTZVNIFKSA-N CC(C)(C)[C@@H](C(N(C[C@@H](C1)Oc(cc2)ncc2Cl)[C@@H]1C(N[C@@H](CC1CCC1)C(C(NC1CC1)=O)=O)=O)=O)NC(OC(C)(C)C)=O Chemical compound CC(C)(C)[C@@H](C(N(C[C@@H](C1)Oc(cc2)ncc2Cl)[C@@H]1C(N[C@@H](CC1CCC1)C(C(NC1CC1)=O)=O)=O)=O)NC(OC(C)(C)C)=O FBGKHCCKXVRREA-QTZVNIFKSA-N 0.000 description 1
- PKBCCOYLTICKIY-SRGWINKKSA-N CCC[C@@H](C(C(NC1CC1)=O)=O)NC([C@H](C[C@H](C1)Oc2c(ccc(OCC)c3)c3ccn2)N1C([C@H](C(C)(C)C)NC(NC(C)(C)C)=O)=O)=O Chemical compound CCC[C@@H](C(C(NC1CC1)=O)=O)NC([C@H](C[C@H](C1)Oc2c(ccc(OCC)c3)c3ccn2)N1C([C@H](C(C)(C)C)NC(NC(C)(C)C)=O)=O)=O PKBCCOYLTICKIY-SRGWINKKSA-N 0.000 description 1
- DGGJQLCAYQCPDD-UHFFFAOYSA-N COC(c1c(N)[s]cc1)=O Chemical compound COC(c1c(N)[s]cc1)=O DGGJQLCAYQCPDD-UHFFFAOYSA-N 0.000 description 1
- CBIDWCOAELWUSK-UHFFFAOYSA-N Oc1nc(-c2cccc[n]2)nc2c1cc[s]2 Chemical compound Oc1nc(-c2cccc[n]2)nc2c1cc[s]2 CBIDWCOAELWUSK-UHFFFAOYSA-N 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
-
- 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
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- 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]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Virology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Pulmonology (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2700708P | 2008-02-07 | 2008-02-07 | |
| US61/027,007 | 2008-02-07 | ||
| PCT/US2009/033229 WO2009100225A1 (en) | 2008-02-07 | 2009-02-05 | Inhibitors of cathepsin b |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101969973A CN101969973A (zh) | 2011-02-09 |
| CN101969973B true CN101969973B (zh) | 2015-07-22 |
Family
ID=40939419
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200980109079.9A Expired - Fee Related CN101969973B (zh) | 2008-02-07 | 2009-02-05 | 组织蛋白酶b抑制剂 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US8211897B2 (enExample) |
| EP (1) | EP2237793A4 (enExample) |
| JP (2) | JP5718647B2 (enExample) |
| CN (1) | CN101969973B (enExample) |
| BR (1) | BRPI0907729A2 (enExample) |
| CA (1) | CA2713108A1 (enExample) |
| EA (1) | EA201001262A1 (enExample) |
| MX (1) | MX2010008371A (enExample) |
| WO (1) | WO2009100225A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AP2009005057A0 (en) | 2007-05-10 | 2009-12-31 | Array Biopharma Inc | Novel peptide inhibitors of hepatitis c virus replication |
| KR20110005869A (ko) | 2008-04-15 | 2011-01-19 | 인터뮨, 인크. | Ｃ형 간염 바이러스 복제의 신규한 마크로사이클릭 억제제 |
| AR075584A1 (es) | 2009-02-27 | 2011-04-20 | Intermune Inc | COMPOSICIONES TERAPEUTICAS QUE COMPRENDEN beta-D-2'-DESOXI-2'-FLUORO-2'-C-METILCITIDINA Y UN DERIVADO DE ACIDO ISOINDOL CARBOXILICO Y SUS USOS. COMPUESTO. |
| CN103946213A (zh) * | 2011-11-25 | 2014-07-23 | 霍夫曼-拉罗奇有限公司 | 作为组织蛋白酶抑制剂的新吡咯烷衍生物 |
| US20140256698A1 (en) * | 2013-03-11 | 2014-09-11 | Virobay, Inc. | Cathepsin inhibitors |
| AU2016378723B2 (en) | 2015-12-22 | 2021-09-30 | SHY Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
| JP7164521B2 (ja) | 2016-06-21 | 2022-11-01 | オリオン・オフサルモロジー・エルエルシー | 炭素環式プロリンアミド誘導体 |
| MX392422B (es) | 2016-06-21 | 2025-03-24 | Orion Ophthalmology LLC | Derivados de prolinamida heterociclica |
| CN109661389A (zh) * | 2016-08-23 | 2019-04-19 | 豪夫迈·罗氏有限公司 | 作为htra1抑制剂的新型二氟酮酰胺衍生物 |
| US10834908B2 (en) * | 2017-04-26 | 2020-11-17 | InfiCure Bio AB | Model animal for fibrosis |
| MA49458A (fr) | 2017-06-21 | 2020-04-29 | SHY Therapeutics LLC | Composés interagissant avec la superfamille ras destinés à être utilisés dans le traitement de cancers, de maladies inflammatoires, de rasopathies et de maladies fibrotiques |
| WO2019018451A2 (en) * | 2017-07-17 | 2019-01-24 | The Regents Of The University Of Colorado | COMPOSITIONS AND METHODS FOR PREVENTING AND TREATING RADIATION-INDUCED PROXIMITY EFFECTS CAUSED BY RADIATION OR RADIATION THERAPY |
| EP3898609A1 (en) | 2018-12-19 | 2021-10-27 | Shy Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070054864A1 (en) * | 2005-06-30 | 2007-03-08 | Michael Graupe | HCV Inhibitors |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0100287A3 (en) | 1997-11-11 | 2003-04-28 | Pfizer Prod Inc | Thienopyrimidine and thienopyridine derivatives useful as anticancer agents |
| US6404397B1 (en) | 1998-08-10 | 2002-06-11 | Raytheon Company | Compact all-weather electromagnetic imaging system |
| US6323180B1 (en) * | 1998-08-10 | 2001-11-27 | Boehringer Ingelheim (Canada) Ltd | Hepatitis C inhibitor tri-peptides |
| US6608027B1 (en) | 1999-04-06 | 2003-08-19 | Boehringer Ingelheim (Canada) Ltd | Macrocyclic peptides active against the hepatitis C virus |
| WO2001055123A1 (en) | 2000-01-26 | 2001-08-02 | Ono Pharmaceutical Co., Ltd. | Nitrogen-containing 5-membered cyclic compounds and drugs containing these compounds as the active ingredient |
| CA2369970A1 (en) * | 2002-02-01 | 2003-08-01 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis c inhibitor tri-peptides |
| AU2004274051A1 (en) | 2003-09-22 | 2005-03-31 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis C virus |
| WO2006113942A2 (en) | 2005-04-20 | 2006-10-26 | Schering Corporation | Method of inhibiting cathepsin activity |
| US20060276406A1 (en) | 2005-06-02 | 2006-12-07 | Schering Corporation | Methods of treating hepatitis C virus |
| WO2006130554A2 (en) | 2005-06-02 | 2006-12-07 | Schering Corporation | Methods of treating hepatitis c virus |
| WO2006130688A2 (en) | 2005-06-02 | 2006-12-07 | Schering Corporation | Compounds for inhibiting cathepsin activity |
| KR20090024834A (ko) * | 2006-07-05 | 2009-03-09 | 인터뮨, 인크. | Ｃ형 간염 바이러스 복제의 신규 억제제 |
| US20080161254A1 (en) | 2007-01-03 | 2008-07-03 | Virobay, Inc. | Hcv inhibitors |
-
2009
- 2009-02-05 EA EA201001262A patent/EA201001262A1/ru unknown
- 2009-02-05 CA CA2713108A patent/CA2713108A1/en not_active Abandoned
- 2009-02-05 WO PCT/US2009/033229 patent/WO2009100225A1/en not_active Ceased
- 2009-02-05 US US12/366,504 patent/US8211897B2/en not_active Expired - Fee Related
- 2009-02-05 JP JP2010545997A patent/JP5718647B2/ja active Active
- 2009-02-05 BR BRPI0907729-4A patent/BRPI0907729A2/pt not_active IP Right Cessation
- 2009-02-05 MX MX2010008371A patent/MX2010008371A/es active IP Right Grant
- 2009-02-05 CN CN200980109079.9A patent/CN101969973B/zh not_active Expired - Fee Related
- 2009-02-05 EP EP09709414.8A patent/EP2237793A4/en not_active Withdrawn
-
2014
- 2014-10-10 JP JP2014209108A patent/JP2015051985A/ja not_active Withdrawn
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070054864A1 (en) * | 2005-06-30 | 2007-03-08 | Michael Graupe | HCV Inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| EA201001262A1 (ru) | 2011-04-29 |
| MX2010008371A (es) | 2010-10-04 |
| JP2011511089A (ja) | 2011-04-07 |
| BRPI0907729A2 (pt) | 2015-07-14 |
| EP2237793A4 (en) | 2013-07-31 |
| JP5718647B2 (ja) | 2015-05-13 |
| CA2713108A1 (en) | 2009-08-13 |
| JP2015051985A (ja) | 2015-03-19 |
| WO2009100225A1 (en) | 2009-08-13 |
| US20090203629A1 (en) | 2009-08-13 |
| EP2237793A1 (en) | 2010-10-13 |
| CN101969973A (zh) | 2011-02-09 |
| US8211897B2 (en) | 2012-07-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20150722 Termination date: 20160205 |