CN1065438C - 环状粘着抑制剂 - Google Patents
环状粘着抑制剂 Download PDFInfo
- Publication number
- CN1065438C CN1065438C CN93108015A CN93108015A CN1065438C CN 1065438 C CN1065438 C CN 1065438C CN 93108015 A CN93108015 A CN 93108015A CN 93108015 A CN93108015 A CN 93108015A CN 1065438 C CN1065438 C CN 1065438C
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- phe
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- Expired - Lifetime
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/745—Blood coagulation or fibrinolysis factors
- C07K14/75—Fibrinogen
-
- 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
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
-
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/78—Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin or cold insoluble globulin [CIG]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- Physical Education & Sports Medicine (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Rheumatology (AREA)
- Toxicology (AREA)
- Zoology (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90936792A | 1992-07-06 | 1992-07-06 | |
| US07/909,367 | 1992-07-06 | ||
| US2202493A | 1993-02-24 | 1993-02-24 | |
| US08/022,024 | 1993-02-24 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1084408A CN1084408A (zh) | 1994-03-30 |
| CN1065438C true CN1065438C (zh) | 2001-05-09 |
Family
ID=26695386
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN93108015A Expired - Lifetime CN1065438C (zh) | 1992-07-06 | 1993-07-06 | 环状粘着抑制剂 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US5866540A (enExample) |
| EP (1) | EP0578083B1 (enExample) |
| JP (2) | JP3803392B2 (enExample) |
| KR (1) | KR100261898B1 (enExample) |
| CN (1) | CN1065438C (enExample) |
| AT (1) | ATE178491T1 (enExample) |
| AU (2) | AU675946B2 (enExample) |
| CA (1) | CA2099541C (enExample) |
| CZ (1) | CZ283744B6 (enExample) |
| DE (1) | DE69324305T2 (enExample) |
| DK (1) | DK0578083T3 (enExample) |
| ES (1) | ES2131542T3 (enExample) |
| HU (1) | HU212572B (enExample) |
| MX (1) | MX9304035A (enExample) |
| NO (1) | NO307985B1 (enExample) |
| PL (1) | PL173785B1 (enExample) |
| SK (1) | SK282024B6 (enExample) |
| TW (1) | TW393319B (enExample) |
| UA (1) | UA43823C2 (enExample) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5654267A (en) * | 1988-12-20 | 1997-08-05 | La Jolla Cancer Research Center | Cooperative combinations of ligands contained within a matrix |
| DE4310643A1 (de) | 1993-04-01 | 1994-10-06 | Merck Patent Gmbh | Cyclische Adhäsionsinhibitoren |
| US5753230A (en) * | 1994-03-18 | 1998-05-19 | The Scripps Research Institute | Methods and compositions useful for inhibition of angiogenesis |
| US5770565A (en) * | 1994-04-13 | 1998-06-23 | La Jolla Cancer Research Center | Peptides for reducing or inhibiting bone resorption |
| DE4415310A1 (de) * | 1994-04-30 | 1995-11-02 | Merck Patent Gmbh | Cyclopeptide |
| US6056958A (en) * | 1994-12-09 | 2000-05-02 | Dupont Pharmaceuticals | Method of treatment of arterial and venous thromboembolic disorders |
| US6492332B1 (en) | 1995-12-12 | 2002-12-10 | Omeros Corporation | Irrigation solution and methods for inhibition of tumor cell adhesion, pain and inflammation |
| DE4444260A1 (de) * | 1994-12-13 | 1996-06-20 | Hoechst Ag | Cyclohexapeptide und deren Mischungen, Verfahren zur Herstellung sowie deren Verwendung |
| US5780426A (en) * | 1995-06-07 | 1998-07-14 | Ixsys, Incorporated | Fivemer cyclic peptide inhibitors of diseases involving αv β3 |
| US5767071A (en) * | 1995-06-07 | 1998-06-16 | Ixsys Incorporated | Sevenmer cyclic peptide inhibitors of diseases involving αv β3 |
| US7053041B1 (en) * | 1996-05-31 | 2006-05-30 | The Scripps Research Institute | Methods and compositions useful for inhibition of αvβ5mediated angiogenesis |
| ATE308981T1 (de) * | 1995-08-14 | 2005-11-15 | Scripps Research Inst | Verfahren und mittel zur hemmung der durch alpha v beta 5 vermittelten angiogenese |
| US5817750A (en) * | 1995-08-28 | 1998-10-06 | La Jolla Cancer Research Foundation | Structural mimics of RGD-binding sites |
| US6080719A (en) * | 1996-02-23 | 2000-06-27 | Hoechst Aktiengesellschaft | Cyclohexapeptides and their mixtures, a process for preparing them, and their use |
| DE19613933A1 (de) * | 1996-04-06 | 1997-10-09 | Merck Patent Gmbh | Cyclische Adhäsionsinhibitoren |
| SK163598A3 (en) | 1996-05-31 | 1999-06-11 | Scripps Research Inst | Methods and compositions useful for inhibition of angiogenesis |
| US6245809B1 (en) | 1996-12-09 | 2001-06-12 | Cor Therapeutics Inc. | Integrin antagonists |
| DE19728524A1 (de) * | 1997-07-04 | 1999-01-07 | Merck Patent Gmbh | Cyclische Azapeptide |
| DE19736772A1 (de) * | 1997-08-23 | 1999-02-25 | Merck Patent Gmbh | Cyclopeptidderivate |
| US6852318B1 (en) * | 1998-05-08 | 2005-02-08 | The Regents Of The University Of California | Methods for detecting and inhibiting angiogenesis |
| WO1999065944A1 (en) * | 1998-06-15 | 1999-12-23 | Ixsys Incorporated | PEPTIDE INHIBITORS OF αVβ3 AND αVβ¿5? |
| AU756916B2 (en) * | 1998-11-12 | 2003-01-23 | Jcr Pharmaceuticals Co., Ltd. | Modulation of cell proliferative disorders by cyclic RGD |
| UA71608C2 (en) * | 1999-03-11 | 2004-12-15 | Merck Patent Gmbh | A method for producing the cyclic pentapeptide |
| CA2405469C (en) | 2000-04-12 | 2012-03-20 | Amersham Health As | Integrin binding peptide derivatives |
| NO20004795D0 (no) | 2000-09-26 | 2000-09-26 | Nycomed Imaging As | Peptidbaserte forbindelser |
| US20030129223A1 (en) * | 2000-10-11 | 2003-07-10 | Targesome, Inc. | Targeted multivalent macromolecules |
| US20030133972A1 (en) * | 2000-10-11 | 2003-07-17 | Targesome, Inc. | Targeted multivalent macromolecules |
| US20030082103A1 (en) * | 2000-10-11 | 2003-05-01 | Targesome, Inc. | Targeted therapeutic lipid constructs having cell surface targets |
| US20040029788A1 (en) * | 2000-11-01 | 2004-02-12 | Hans-Markus Bender | Methods and compositions for the treatment of diseases of the eye |
| ATE415163T1 (de) | 2000-11-01 | 2008-12-15 | Merck Patent Gmbh | Verfahren und zusammensetzungen zur behandlung von augenerkrankungen |
| BRPI0210886B8 (pt) | 2001-07-10 | 2021-05-25 | Amersham Health As | composto, composição farmacêutica, uso de um composto, e, métodos de geração de imagens, de monitoração do efeito do tratamento de um corpo humano ou animal com uma droga para combater uma condição associada com câncer e de tratamento de câncer ou de uma doença relacionada em um corpo humano ou animal |
| RU2214416C2 (ru) * | 2001-12-10 | 2003-10-20 | Государственный научный центр вирусологии и биотехнологии "Вектор" | Rgd-содержащие пептиды |
| US7597907B2 (en) * | 2004-11-05 | 2009-10-06 | Trustees Of The University Of Pennsylvania | Antioxidant polymer nanocarriers for use in preventing oxidative injury |
| US7605056B2 (en) | 2005-05-31 | 2009-10-20 | Semiconductor Energy Laboratory Co., Ltd. | Method of manufacturing a semiconductor device including separation by physical force |
| US8568786B2 (en) * | 2007-10-27 | 2013-10-29 | The Trustees Of The Universtiy Of Pennsylvania | Method and compositions for polymer nanocarriers containing therapeutic molecules |
| US7927629B2 (en) * | 2007-10-27 | 2011-04-19 | The Trustees Of The University Of Pennsylvania | Method and compositions for polymer nanocarriers containing therapeutic molecules |
| CN101990425B (zh) * | 2008-04-08 | 2016-01-20 | 默克专利股份有限公司 | 包含环肽的组合物和使用方法 |
| US20110256055A1 (en) | 2008-12-23 | 2011-10-20 | Ge Healthcare Limited | Application of 99mtc peptide-based compound as a bone marrow imaging agent |
| CN103153328A (zh) * | 2010-07-16 | 2013-06-12 | 默克专利股份有限公司 | 肽在乳腺癌和/或骨转移灶的治疗中的用途 |
| DK2892540T3 (en) * | 2012-09-06 | 2018-11-19 | Mcpharma Biotech Inc | TREATMENT OF DIARRES AND DRAWN DIARRES WITH RESISTANT POTATO STARCH |
| US11001609B2 (en) | 2017-04-24 | 2021-05-11 | The Regents Of The University Of California | Cell permeable cyclic peptide scaffolds |
| WO2019058374A1 (en) * | 2017-09-19 | 2019-03-28 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | N-METHYLATED CYCLIC PEPTIDES AND PRODRUGS THEREOF |
| KR102213196B1 (ko) * | 2018-05-08 | 2021-02-05 | 주식회사 메디폴리머 | 클릭화학 반응을 통해 필러 또는 약물전달체로 사용하기 위한 주사제형 조성물 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2945680B2 (ja) * | 1988-09-09 | 1999-09-06 | 旭硝子株式会社 | ペプチド誘導体およびその用途 |
| EP0410537A1 (en) * | 1989-07-28 | 1991-01-30 | Merck & Co. Inc. | Fibrinogen receptor antagonists |
| DK0527798T3 (da) * | 1990-04-06 | 1997-12-15 | Jolla Cancer Res Found | Fremgangsmåde og sammensætning til behandling af thrombose |
| US5192746A (en) * | 1990-07-09 | 1993-03-09 | Tanabe Seiyaku Co., Ltd. | Cyclic cell adhesion modulation compounds |
-
1993
- 1993-06-18 UA UA93002630A patent/UA43823C2/uk unknown
- 1993-06-24 JP JP15346293A patent/JP3803392B2/ja not_active Expired - Lifetime
- 1993-06-26 DK DK93110232T patent/DK0578083T3/da active
- 1993-06-26 DE DE69324305T patent/DE69324305T2/de not_active Expired - Lifetime
- 1993-06-26 ES ES93110232T patent/ES2131542T3/es not_active Expired - Lifetime
- 1993-06-26 AT AT93110232T patent/ATE178491T1/de active
- 1993-06-26 EP EP93110232A patent/EP0578083B1/en not_active Expired - Lifetime
- 1993-06-30 CZ CZ931315A patent/CZ283744B6/cs not_active IP Right Cessation
- 1993-07-02 CA CA002099541A patent/CA2099541C/en not_active Expired - Lifetime
- 1993-07-05 MX MX9304035A patent/MX9304035A/es unknown
- 1993-07-05 HU HU9301950A patent/HU212572B/hu unknown
- 1993-07-05 NO NO932439A patent/NO307985B1/no not_active IP Right Cessation
- 1993-07-05 KR KR1019930012550A patent/KR100261898B1/ko not_active Expired - Lifetime
- 1993-07-05 PL PL93299559A patent/PL173785B1/pl unknown
- 1993-07-06 CN CN93108015A patent/CN1065438C/zh not_active Expired - Lifetime
- 1993-07-06 AU AU41796/93A patent/AU675946B2/en not_active Expired
- 1993-07-06 SK SK706-93A patent/SK282024B6/sk not_active IP Right Cessation
- 1993-08-18 TW TW082106697A patent/TW393319B/zh not_active IP Right Cessation
-
1995
- 1995-01-04 US US08/368,760 patent/US5866540A/en not_active Expired - Lifetime
-
1997
- 1997-02-13 AU AU12687/97A patent/AU1268797A/en not_active Abandoned
-
2004
- 2004-05-06 JP JP2004137652A patent/JP4192114B2/ja not_active Expired - Lifetime
Non-Patent Citations (3)
| Title |
|---|
| ANGEWANDATE CHEMIE IN TERNARIONAL EDITION VOL.31,NO.3 1992.3.1 G.NUUER等"DYNAMIC FORCING ,A METHOD FOR EVALUATING ACTIVITY AND SELECTIBIT * |
| ANGEWANDATE CHEMIE IN TERNARIONAL EDITION VOL.31,NO.3 1992.3.1 G.NUUER等"DYNAMIC FORCING ,A METHOD FOR EVALUATING ACTIVITY AND SELECTIBIT;FEBS LETTERS VOL,291,NO.1 1991.10.1 M.AUMAILLEY等,"ARG-GLY-ASP"COMSTRAINED WOTHIN CYCLIC PEPTIDES STRONG AND SELECTIVE IN HIBITORS OF CE * |
| FEBS LETTERS VOL,291,NO.1 1991.10.1 M.AUMAILLEY等,"ARG-GLY-ASP"COMSTRAINED WOTHIN CYCLIC PEPTIDES STRONG AND SELECTIVE IN HIBITORS OF CE * |
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