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)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Virology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Communicable Diseases (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (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 (https=) |
| EP (1) | EP2237793A4 (https=) |
| JP (2) | JP5718647B2 (https=) |
| CN (1) | CN101969973B (https=) |
| BR (1) | BRPI0907729A2 (https=) |
| CA (1) | CA2713108A1 (https=) |
| EA (1) | EA201001262A1 (https=) |
| MX (1) | MX2010008371A (https=) |
| WO (1) | WO2009100225A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010526834A (ja) | 2007-05-10 | 2010-08-05 | インターミューン・インコーポレーテッド | Ｃ型肝炎ウイルス複製の新規ペプチド阻害剤 |
| WO2009142842A2 (en) | 2008-04-15 | 2009-11-26 | Intermune, Inc. | Novel macrocyclic inhibitors of hepatitis c virus replication |
| 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. |
| EP2782903B1 (en) | 2011-11-25 | 2016-04-06 | F.Hoffmann-La Roche Ag | Novel pyrrolidine derivatives as inhibitors of cathepsin |
| US20140256698A1 (en) * | 2013-03-11 | 2014-09-11 | Virobay, Inc. | Cathepsin inhibitors |
| JP7114076B2 (ja) | 2015-12-22 | 2022-08-08 | シャイ・セラピューティクス・エルエルシー | がん及び炎症性疾患の処置のための化合物 |
| HUE064412T2 (hu) | 2016-06-21 | 2024-03-28 | Orion Ophthalmology LLC | Heterociklusos prolinamid-származékok |
| 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 |
| JP2019526563A (ja) * | 2016-08-23 | 2019-09-19 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｈｔｒａ１阻害剤としての新規ジフルオロケタミド誘導体 |
| US10834908B2 (en) * | 2017-04-26 | 2020-11-17 | InfiCure Bio AB | Model animal for fibrosis |
| JP7514005B2 (ja) | 2017-06-21 | 2024-07-10 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ラソパシー、及び線維性疾患の治療のためのｒａｓスーパーファミリーと相互作用する化合物 |
| US11452709B2 (en) * | 2017-07-17 | 2022-09-27 | The Regents Of The University Of Colorado, A Body Corporate | Compositions and methods for preventing and treating radiation-induced bystander effects caused by radiation or radiotherapy |
| JP7407461B2 (ja) | 2018-12-19 | 2024-01-04 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ｒａｓ病、及び線維性疾患の処置のためのｒａｓスーパーファミリーと相互作用する化合物 |
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 |
|---|---|---|---|---|
| CA2309690A1 (en) * | 1997-11-11 | 1999-05-20 | Pfizer Products 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 |
| EP1254901A4 (en) * | 2000-01-26 | 2003-03-05 | Ono Pharmaceutical Co | 5-CHAIN CYCLIC COMPOUNDS, CONTAINING NITROGEN, AND MEDICINAL PRODUCTS CONTAINING THE SAME AS ACTIVE INGREDIENTS |
| CA2369970A1 (en) * | 2002-02-01 | 2003-08-01 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis c inhibitor tri-peptides |
| RS20060197A (sr) | 2003-09-22 | 2008-09-29 | Boehringer Ingelheim International Gmbh., | Makrociklični peptidi koji su aktivni protiv hepatitisa c virusa |
| WO2006113942A2 (en) | 2005-04-20 | 2006-10-26 | Schering Corporation | Method of inhibiting cathepsin activity |
| WO2006130552A2 (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 |
| US20060287248A1 (en) | 2005-06-02 | 2006-12-21 | Schering Corporation | Asymmetric dosing methods |
| RU2008152171A (ru) * | 2006-07-05 | 2010-08-10 | Интермьюн, Инк. (Us) | Новые ингибиторы вирусной репликации гепатита с |
| US20080161254A1 (en) | 2007-01-03 | 2008-07-03 | Virobay, Inc. | Hcv inhibitors |
-
2009
- 2009-02-05 US US12/366,504 patent/US8211897B2/en not_active Expired - Fee Related
- 2009-02-05 EP EP09709414.8A patent/EP2237793A4/en not_active Withdrawn
- 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 BR BRPI0907729-4A patent/BRPI0907729A2/pt not_active IP Right Cessation
- 2009-02-05 EA EA201001262A patent/EA201001262A1/ru unknown
- 2009-02-05 JP JP2010545997A patent/JP5718647B2/ja active Active
- 2009-02-05 CN CN200980109079.9A patent/CN101969973B/zh not_active Expired - Fee Related
- 2009-02-05 MX MX2010008371A patent/MX2010008371A/es active IP Right Grant
-
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 |
|---|---|
| US8211897B2 (en) | 2012-07-03 |
| JP2011511089A (ja) | 2011-04-07 |
| EA201001262A1 (ru) | 2011-04-29 |
| JP2015051985A (ja) | 2015-03-19 |
| CA2713108A1 (en) | 2009-08-13 |
| BRPI0907729A2 (pt) | 2015-07-14 |
| CN101969973A (zh) | 2011-02-09 |
| MX2010008371A (es) | 2010-10-04 |
| WO2009100225A1 (en) | 2009-08-13 |
| US20090203629A1 (en) | 2009-08-13 |
| EP2237793A4 (en) | 2013-07-31 |
| EP2237793A1 (en) | 2010-10-13 |
| JP5718647B2 (ja) | 2015-05-13 |
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| 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 |