BG101647A - Low molecular weight bicyclic thrombin inhibitors - Google Patents
Low molecular weight bicyclic thrombin inhibitorsInfo
- Publication number
- BG101647A BG101647A BG101647A BG10164797A BG101647A BG 101647 A BG101647 A BG 101647A BG 101647 A BG101647 A BG 101647A BG 10164797 A BG10164797 A BG 10164797A BG 101647 A BG101647 A BG 101647A
- Authority
- BG
- Bulgaria
- Prior art keywords
- molecular weight
- low molecular
- treatment
- thrombin inhibitors
- relates
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D487/04—Ortho-condensed systems
-
- 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
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06139—Dipeptides with the first amino acid being heterocyclic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biophysics (AREA)
- Pharmacology & Pharmacy (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Animal Behavior & Ethology (AREA)
- Molecular Biology (AREA)
- Public Health (AREA)
- Biochemistry (AREA)
- Genetics & Genomics (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Crystallography & Structural Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to competitive heterocyclic inhibitorsof the enzyme thrombin with the formulauntil their preparation and to the pharmaceutical compositionscontaining them. The invention also relates to the application ofthese compounds and compositions in vitro as anticoagulants and invivo as agents for the treatment and prophylaxy of thrombosediseases such as venous thrombosis, lung artery embolism andarterial thromosis occuring in acute ischemic cases, such asinfarction of the myocardium or cerebral infarction. The compoundsand the compositions containing them are useful for the preventionand treatment of coagulapathies related to coronary bypassoperations as well as in other cases appearing as a result oftransluminal angioplasty.57 claims
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB9426038.7A GB9426038D0 (en) | 1994-12-22 | 1994-12-22 | Low molecular weight bicyclic thrombin inhibitors |
GBGB9503136.5A GB9503136D0 (en) | 1994-12-22 | 1995-02-17 | Low molecular weight bicyclic thrombin inhibitors |
GBGB9510267.9A GB9510267D0 (en) | 1995-05-22 | 1995-05-22 | Low molecular weight thiobicyclic thrombin inhibitors |
GBGB9510265.3A GB9510265D0 (en) | 1995-05-22 | 1995-05-22 | Low molecular weight diaminobicyclic thrombin inhibitors |
GBGB9510266.1A GB9510266D0 (en) | 1995-05-22 | 1995-05-22 | Low molecular weight bicyclic thrombin inhibitors |
PCT/CA1995/000708 WO1996019483A1 (en) | 1994-12-22 | 1995-12-21 | Low molecular weight bicyclic thrombin inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
BG101647A true BG101647A (en) | 1998-03-31 |
Family
ID=27517273
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BG101647A BG101647A (en) | 1994-12-22 | 1997-06-20 | Low molecular weight bicyclic thrombin inhibitors |
Country Status (22)
Country | Link |
---|---|
EP (1) | EP0802916A1 (en) |
JP (1) | JPH11508535A (en) |
CN (1) | CN1175259A (en) |
AP (1) | AP9701004A0 (en) |
AU (2) | AU4250596A (en) |
BG (1) | BG101647A (en) |
CA (1) | CA2208772A1 (en) |
CZ (1) | CZ189997A3 (en) |
EE (1) | EE9700113A (en) |
FI (1) | FI972466A (en) |
HU (1) | HUT77651A (en) |
IL (1) | IL116503A0 (en) |
IS (1) | IS4504A (en) |
LV (1) | LV12019B (en) |
MD (1) | MD970253A (en) |
MX (1) | MX9704718A (en) |
NO (1) | NO972892L (en) |
NZ (1) | NZ297360A (en) |
OA (1) | OA10493A (en) |
PL (1) | PL320965A1 (en) |
SK (1) | SK83897A3 (en) |
WO (1) | WO1996019483A1 (en) |
Families Citing this family (46)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6699869B1 (en) | 1995-03-24 | 2004-03-02 | Myriad Genetics Inc. | β-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins |
US6020331A (en) * | 1995-03-24 | 2000-02-01 | Molecumetics, Ltd. | β-sheet mimetics and use thereof as protease inhibitors |
US6245764B1 (en) | 1995-03-24 | 2001-06-12 | Molecumetics Ltd. | β-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins |
IT1277405B1 (en) * | 1995-08-01 | 1997-11-10 | Menarini Farma Ind | BICYCLIC LACTAM DERIVATIVES AS THROMBIN INHIBITORS |
IL119466A (en) | 1995-11-03 | 2001-08-26 | Akzo Nobel Nv | Thrombin inhibitors, their preparation and pharmaceutical compositions containing them |
US6034067A (en) * | 1996-02-13 | 2000-03-07 | Akzo Nobel, N.V. | Serine protease inhibitors |
IL120310A (en) * | 1996-03-01 | 2002-02-10 | Akzo Nobel Nv | Serine protease inhibitors and pharmaceutical compositions containing them |
TW523513B (en) * | 1996-03-01 | 2003-03-11 | Akzo Nobel Nv | Serine protease inhibitors |
US6124291A (en) * | 1996-06-18 | 2000-09-26 | Warner-Lambert Company | Pyrrolo[1,2-a]pyrazine-1,4-dione serine protease inhibitors |
EP1661566A3 (en) * | 1996-08-05 | 2008-04-16 | Myriad Genetics, Inc. | Use of beta-sheet mimetics as protease and kinase inhibitors and as inhibitors of transcription factors |
CA2262900A1 (en) * | 1996-08-05 | 1998-02-12 | Molecumetics Ltd. | Use of beta-sheet mimetics as protease and kinase inhibitors and as inhibitors of transcription factors |
US6117896A (en) | 1997-02-10 | 2000-09-12 | Molecumetics Ltd. | Methods for regulating transcription factors |
AU4172397A (en) * | 1996-09-06 | 1998-03-26 | Biochem Pharma Inc. | Lactam inhibitors of thrombin |
US6369080B2 (en) | 1996-10-11 | 2002-04-09 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
US6194435B1 (en) | 1996-10-11 | 2001-02-27 | Cor Therapeutics, Inc. | Lactams as selective factor Xa inhibitors |
US6262047B1 (en) | 1996-10-11 | 2001-07-17 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
US6063794A (en) | 1996-10-11 | 2000-05-16 | Cor Therapeutics Inc. | Selective factor Xa inhibitors |
WO1998028326A1 (en) * | 1996-12-23 | 1998-07-02 | Biochem Pharma Inc. | Bicyclic thrombin inhibitors |
EP0975659A1 (en) * | 1997-04-14 | 2000-02-02 | Cor Therapeutics, Inc. | SELECTIVE FACTOR Xa INHIBITORS |
AU6896298A (en) | 1997-04-14 | 1998-11-11 | Cor Therapeutics, Inc. | Selective factor xa inhibitors |
NZ500352A (en) | 1997-04-14 | 2001-10-26 | Cor Therapeutics Inc | Cyclic diaza selective factor Xa inhibitors |
US6333321B1 (en) | 1997-08-11 | 2001-12-25 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
US6228854B1 (en) | 1997-08-11 | 2001-05-08 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
US6218382B1 (en) | 1997-08-11 | 2001-04-17 | Cor Therapeutics, Inc | Selective factor Xa inhibitors |
AU740447B2 (en) * | 1997-09-23 | 2001-11-01 | Merck & Co., Inc. | Thrombin inhibitors |
ES2192764T3 (en) * | 1998-02-12 | 2003-10-16 | Molecumetics Ltd | MIMETICS OF LAMINA BETA AND METHODS RELATED TO THE USE OF THE SAME. |
US6323219B1 (en) | 1998-04-02 | 2001-11-27 | Ortho-Mcneil Pharmaceutical, Inc. | Methods for treating immunomediated inflammatory disorders |
US8093293B2 (en) | 1998-07-06 | 2012-01-10 | Johnson & Johnson Consumer Companies, Inc. | Methods for treating skin conditions |
US8106094B2 (en) | 1998-07-06 | 2012-01-31 | Johnson & Johnson Consumer Companies, Inc. | Compositions and methods for treating skin conditions |
EP1140862A4 (en) | 1998-12-23 | 2004-07-28 | Bristol Myers Squibb Pharma Co | THROMBIN OR FACTOR Xa INHIBITORS |
EA200100815A1 (en) | 1999-01-27 | 2002-08-29 | Орто-Макнейл Фармасьютикал, Инк. | PEPTIDILE HETEROCYCLIC KETONES USED AS TRIPTASE INHIBITORS |
FR2795072B1 (en) * | 1999-06-15 | 2001-07-27 | Adir | NOVEL BICYCLIC DERIVATIVES OF AMINO-PYRAZINONES, PROCESS FOR THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
CA2401749A1 (en) * | 2000-03-23 | 2001-09-27 | Elan Pharmaceuticals, Inc. | Compounds and methods to treat alzheimer's disease |
US6586418B2 (en) | 2000-06-29 | 2003-07-01 | Bristol-Myers Squibb Company | Thrombin or factor Xa inhibitors |
US8431550B2 (en) | 2000-10-27 | 2013-04-30 | Johnson & Johnson Consumer Companies, Inc. | Topical anti-cancer compositions and methods of use thereof |
FR2818277B1 (en) * | 2000-12-14 | 2003-01-24 | Servier Lab | NOVEL BICYCLIC DERIVATIVES OF AMINO-PYRAZINONES, PROCESS FOR PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME |
US7192615B2 (en) | 2001-02-28 | 2007-03-20 | J&J Consumer Companies, Inc. | Compositions containing legume products |
CN1642550A (en) | 2002-02-14 | 2005-07-20 | 美瑞德生物工程公司 | Beta-sheet mimetics and composition and methods relating thereto |
WO2003082197A2 (en) | 2002-03-22 | 2003-10-09 | Gpc Biotech Ag | Immunosuppressant compounds, methods and uses related thereto |
BR112017006920A8 (en) | 2014-10-06 | 2023-03-07 | Quince Therapeutics Inc | GINGIPAINE LYSINE INHIBITORS |
JO3637B1 (en) | 2015-04-28 | 2020-08-27 | Janssen Sciences Ireland Uc | Rsv antiviral pyrazolo- and triazolo-pyrimidine compounds |
CA3004095A1 (en) | 2015-11-09 | 2017-05-18 | Cortexyme, Inc. | Inhibitors of arginine gingipain |
TWI787202B (en) | 2016-09-16 | 2022-12-21 | 美商昆斯治療公司 | Ketone inhibitors of lysine gingipain |
TW201932470A (en) | 2017-11-29 | 2019-08-16 | 愛爾蘭商健生科學愛爾蘭無限公司 | Pyrazolopyrimidines having activity against RSV |
EA202091835A1 (en) | 2018-01-31 | 2020-10-20 | Янссен Сайенсиз Айрлэнд Анлимитед Компани | CYCLOALKYL SUBSTITUTED PYRAZOLOPYRIMIDINES WITH AN ACTIVITY AGAINST RSV |
AU2019260109B2 (en) | 2018-04-23 | 2023-07-13 | Janssen Sciences Ireland Unlimited Company | Heteroaromatic compounds having activity against RSV |
-
1995
- 1995-12-21 WO PCT/CA1995/000708 patent/WO1996019483A1/en not_active Application Discontinuation
- 1995-12-21 PL PL95320965A patent/PL320965A1/en unknown
- 1995-12-21 EE EE9700113A patent/EE9700113A/en unknown
- 1995-12-21 JP JP8519383A patent/JPH11508535A/en active Pending
- 1995-12-21 NZ NZ297360A patent/NZ297360A/en unknown
- 1995-12-21 CZ CZ971899A patent/CZ189997A3/en unknown
- 1995-12-21 EP EP95940923A patent/EP0802916A1/en not_active Ceased
- 1995-12-21 HU HU9800216A patent/HUT77651A/en unknown
- 1995-12-21 AU AU42505/96A patent/AU4250596A/en not_active Abandoned
- 1995-12-21 CN CN95197614A patent/CN1175259A/en active Pending
- 1995-12-21 CA CA002208772A patent/CA2208772A1/en not_active Abandoned
- 1995-12-21 AP APAP/P/1997/001004A patent/AP9701004A0/en unknown
- 1995-12-21 MD MD97-0253A patent/MD970253A/en unknown
- 1995-12-21 SK SK838-97A patent/SK83897A3/en unknown
- 1995-12-22 AU AU40628/95A patent/AU715378B2/en not_active Ceased
- 1995-12-22 IL IL11650395D patent/IL116503A0/en unknown
-
1997
- 1997-06-11 IS IS4504A patent/IS4504A/en unknown
- 1997-06-11 FI FI972466A patent/FI972466A/en unknown
- 1997-06-18 OA OA70029A patent/OA10493A/en unknown
- 1997-06-20 BG BG101647A patent/BG101647A/en unknown
- 1997-06-20 NO NO972892A patent/NO972892L/en unknown
- 1997-06-23 MX MX9704718A patent/MX9704718A/en unknown
- 1997-07-15 LV LVP-97-141A patent/LV12019B/en unknown
Also Published As
Publication number | Publication date |
---|---|
IL116503A0 (en) | 1996-03-31 |
NO972892L (en) | 1997-08-20 |
AU4062895A (en) | 1996-07-04 |
CN1175259A (en) | 1998-03-04 |
CA2208772A1 (en) | 1996-06-27 |
WO1996019483A1 (en) | 1996-06-27 |
MD970253A (en) | 1999-05-31 |
AP9701004A0 (en) | 1997-07-31 |
AU715378B2 (en) | 2000-02-03 |
EE9700113A (en) | 1997-12-15 |
HUT77651A (en) | 1998-07-28 |
IS4504A (en) | 1997-06-11 |
SK83897A3 (en) | 1998-05-06 |
MX9704718A (en) | 1998-06-28 |
PL320965A1 (en) | 1997-11-24 |
LV12019B (en) | 1998-07-20 |
AU4250596A (en) | 1996-07-10 |
FI972466A (en) | 1997-08-19 |
EP0802916A1 (en) | 1997-10-29 |
FI972466A0 (en) | 1997-06-11 |
NZ297360A (en) | 2000-03-27 |
JPH11508535A (en) | 1999-07-27 |
NO972892D0 (en) | 1997-06-20 |
LV12019A (en) | 1998-04-20 |
OA10493A (en) | 2002-04-10 |
CZ189997A3 (en) | 1998-09-16 |
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