ZA200402849B - Himbacine analogues as thrombin receptor antagonists. - Google Patents
Himbacine analogues as thrombin receptor antagonists.Info
- Publication number
- ZA200402849B ZA200402849B ZA200402849A ZA200402849A ZA200402849B ZA 200402849 B ZA200402849 B ZA 200402849B ZA 200402849 A ZA200402849 A ZA 200402849A ZA 200402849 A ZA200402849 A ZA 200402849A ZA 200402849 B ZA200402849 B ZA 200402849B
- Authority
- ZA
- South Africa
- Prior art keywords
- himbacine
- analogues
- receptor antagonists
- thrombin receptor
- thrombin
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- 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
- A61P19/00—Drugs for skeletal disorders
-
- 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
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US33035901P | 2001-10-18 | 2001-10-18 |
Publications (1)
Publication Number | Publication Date |
---|---|
ZA200402849B true ZA200402849B (en) | 2005-01-14 |
Family
ID=23289411
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ZA200402849A ZA200402849B (en) | 2001-10-18 | 2004-04-15 | Himbacine analogues as thrombin receptor antagonists. |
Country Status (23)
Country | Link |
---|---|
US (2) | US7037920B2 (ja) |
EP (1) | EP1436298B1 (ja) |
JP (2) | JP4307260B2 (ja) |
KR (1) | KR100960170B1 (ja) |
CN (1) | CN100369917C (ja) |
AR (1) | AR036832A1 (ja) |
AT (1) | ATE525378T1 (ja) |
AU (1) | AU2002335031C1 (ja) |
BR (1) | BR0213967A (ja) |
CA (1) | CA2463628A1 (ja) |
CO (1) | CO5570668A2 (ja) |
EC (1) | ECSP045064A (ja) |
HU (1) | HUP0500443A3 (ja) |
IL (1) | IL160918A0 (ja) |
MX (1) | MXPA04003610A (ja) |
MY (1) | MY139335A (ja) |
NO (1) | NO329349B1 (ja) |
NZ (1) | NZ531869A (ja) |
PE (1) | PE20030808A1 (ja) |
PL (1) | PL371948A1 (ja) |
RU (1) | RU2319704C9 (ja) |
WO (1) | WO2003033501A1 (ja) |
ZA (1) | ZA200402849B (ja) |
Families Citing this family (46)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6346510B1 (en) | 1995-10-23 | 2002-02-12 | The Children's Medical Center Corporation | Therapeutic antiangiogenic endostatin compositions |
US7488742B2 (en) * | 2000-06-15 | 2009-02-10 | Schering Corporation | Thrombin receptor antagonists |
US7235567B2 (en) * | 2000-06-15 | 2007-06-26 | Schering Corporation | Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist |
SG164279A1 (en) * | 2002-04-16 | 2010-09-29 | Schering Corp | Tricyclic thrombin receptor antagonists |
ATE536889T1 (de) * | 2003-07-08 | 2011-12-15 | Accumetrics Inc | Kontrollierte thrombozyten-aktivierung zur überwachung der behandlung von adp-antagonisten |
US20070243632A1 (en) * | 2003-07-08 | 2007-10-18 | Coller Barry S | Methods for measuring platelet reactivity of patients that have received drug eluting stents |
DE602005009355D1 (de) * | 2004-05-28 | 2008-10-09 | Schering Corp | Gehinderte himbacinanaloga als thrombinrezeptorantagonisten |
US20060063930A1 (en) * | 2004-08-20 | 2006-03-23 | Agoston Gregory E | Compositions and methods comprising proteinase activated receptor antagonists |
US8563511B2 (en) * | 2004-10-06 | 2013-10-22 | University Of Rochester | Treatment of pulmonary hypertension using an agent that inhibits a tissue factor pathway |
EP2075250B1 (en) * | 2004-10-08 | 2015-03-04 | Merck Sharp & Dohme Corp. | Thrombin receptor antagonists |
SI1848705T1 (sl) * | 2005-01-14 | 2010-06-30 | Schering Corp | Eksoselektivne in diastereoselektivne sinteze himbacinskih analogov |
WO2006076564A1 (en) * | 2005-01-14 | 2006-07-20 | Schering Corporation | Synthesis of himbacine analogs |
EP2399912B1 (en) * | 2005-01-14 | 2015-02-25 | Merck Sharp & Dohme Corp. | An exo-selective synthesis of himbacine analogs |
TWI316937B (en) * | 2005-03-31 | 2009-11-11 | Schering Corp | Spirocyclic thrombin receptor antagonists |
US7595169B2 (en) * | 2005-04-27 | 2009-09-29 | Accumetrics, Inc. | Method for determining percent platelet aggregation |
US20070219154A1 (en) * | 2005-12-20 | 2007-09-20 | Suxing Liu | Methods for preventing and/or treating a cell proliferative disorder |
CN101384590A (zh) * | 2005-12-22 | 2009-03-11 | 先灵公司 | 作为凝血酶受体拮抗剂的唑并异喹啉 |
US20070202140A1 (en) * | 2005-12-22 | 2007-08-30 | Veltri Enrico P | Thrombin receptor antagonists as prophylaxis to complications from cardiopulmonary surgery |
US7888377B2 (en) * | 2006-03-29 | 2011-02-15 | Schering Corporation | Monocyclic and bicyclic himbacine derivatives useful as thrombin receptor antagonists |
US8003803B2 (en) * | 2006-04-13 | 2011-08-23 | Schering Corporation | Fused ring thrombin receptor antagonists |
CN101506198A (zh) | 2006-06-29 | 2009-08-12 | 先灵公司 | 取代的双环和三环凝血酶受体拮抗剂 |
AR061727A1 (es) * | 2006-06-30 | 2008-09-17 | Schering Corp | Sintesis de dietil [[ 5- ( 3-fluorofenil) -piridin -2il] metil] fosfonato |
TWI367112B (en) * | 2006-06-30 | 2012-07-01 | Schering Corp | Immediate-release tablet formulations of a thrombin receptor antagonist |
TWI343262B (en) * | 2006-09-26 | 2011-06-11 | Schering Corp | Rapidly disintegrating lyophilized oral formulations of a thrombin receptor antagonist |
CA2667082A1 (en) * | 2006-10-04 | 2008-04-10 | Schering Corporation | Bicyclic and tricyclic derivatives as thrombin receptor antagonists |
WO2008060372A2 (en) * | 2006-10-04 | 2008-05-22 | Schering Corporation | Thrombin receptor antagonists based on the modified tricyclic unit of himbacine |
US20080194560A1 (en) * | 2006-12-22 | 2008-08-14 | Zhi Yun Wang | Disintegration promoters in solid dose wet granulation formulations |
BRPI0809095A2 (pt) * | 2007-03-23 | 2014-09-09 | Schering Corp | Redução de eventos adversos após intervenção percutânea através de uso de um antagonista de receptor de trombina |
EP2153235B1 (en) * | 2007-05-03 | 2012-05-16 | Accumetrics, Inc. | Methods of measuring inhibition of platelet aggregation by thrombin receptor antagonists |
JP5526040B2 (ja) | 2008-02-05 | 2014-06-18 | サノフイ | Par1阻害剤としてのトリアゾロピリダジン類、その製造法および薬剤としての使用 |
AR071823A1 (es) | 2008-05-19 | 2010-07-14 | Schering Corp | Derivados heterociclicos de imidazol y pirazol, inhibidores del factor ixa de coagulacion, composiciones farmaceuticas que los contienen y uso de los mismos para tratar diversos trastornos tromboembolicos. |
DK2438060T3 (da) | 2009-06-04 | 2014-01-13 | Merck Sharp & Dohme | Aktiv metabolit af en trombin-receptor-antagonist |
MX2011013091A (es) | 2009-06-08 | 2012-01-12 | Schering Corp | Un antagonista del receptor de trombina y tableta con dosificacion fija de clopidogrel. |
EP2462123B1 (en) | 2009-08-04 | 2013-10-02 | Merck Sharp & Dohme Corp. | 4,5,6-trisubstituted pyrimidine derivatives as factor ixa inhibitors |
US9340530B2 (en) | 2012-03-06 | 2016-05-17 | Merck Sharp & Dohme Corp. | Preparation and use of bicyclic himbacine derivatives as PAR-1 receptor antagonists |
EP3035928B1 (en) | 2013-08-22 | 2023-10-18 | Merck Sharp & Dohme LLC | 3'-pyridyl substituted- 6,6-difluoro bicyclic himbacine derivatives |
WO2015026685A1 (en) | 2013-08-22 | 2015-02-26 | Merck Sharp & Dohme Corp. | 7a-heterocycle substituted- 6, 6-difluoro bicyclic himbacine derivatives |
WO2015026693A1 (en) | 2013-08-22 | 2015-02-26 | Merck Sharp & Dohme Corp. | 7a-amide substituted-6,6-difluoro bicyclic himbacine derivatives |
WO2015160636A1 (en) | 2014-04-16 | 2015-10-22 | Merck Sharp & Dohme Corp. | Factor ixa inhibitors |
CN104610330A (zh) * | 2015-02-25 | 2015-05-13 | 成都安斯利生物医药有限公司 | 一种制备(e)-3-丙烯酸乙酯频呐硼酸酯的方法 |
US20230312560A1 (en) | 2020-07-22 | 2023-10-05 | Janssen Pharmaceutica Nv | Compounds useful as factor xia inhibitors |
US11845748B2 (en) | 2021-03-18 | 2023-12-19 | Janssen Pharmaceutica Nv | Bicyclic pyridine N-oxide derivatives useful as a factor XIa inhibitors |
US11814364B2 (en) | 2021-03-18 | 2023-11-14 | Janssen Pharmaceutica Nv | Pyridine N-oxide derivatives useful as factor XIa inhibitors |
US11919881B2 (en) | 2021-03-18 | 2024-03-05 | Janssen Pharmaceutica Nv | Substituted pyridine N-oxide derivatives useful as a factor XIa inhibitors |
US11897880B2 (en) | 2021-04-30 | 2024-02-13 | Janssen Pharmaceutica Nv | 7,8-dihydrobenzo[e]pyrido[3,4-c]azocine-2,5(3H,6H)-dione derivatives useful as a factor XIa inhibitors |
US11958856B2 (en) | 2021-07-22 | 2024-04-16 | Janssen Pharmaceutica Nv | Substituted 1,2,3,8,9,9a-hexahydro-5H-pyrrolo[1,2-a]azepin-5-ones as factor XIa inhibitors |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5716952A (en) * | 1992-03-18 | 1998-02-10 | Allergan | Method for reducing intraocular pressure in the mammalian eye by administration of muscarinic antagonists |
IL106197A (en) | 1992-07-30 | 1999-11-30 | Cor Therapeutics Inc | Agagonists for the rhombin receptors and pharmaceutical preparations containing them |
JP2000229961A (ja) | 1998-12-11 | 2000-08-22 | Sagami Chem Res Center | ヒドロナフト[2,3−c]フラン誘導体およびその製造方法 |
US6063847A (en) * | 1997-11-25 | 2000-05-16 | Schering Corporation | Thrombin receptor antagonists |
DE19801636A1 (de) * | 1998-01-17 | 1999-07-22 | Bayer Ag | Substituierte bicyclische Lactone |
PL359822A1 (en) | 2000-06-15 | 2004-09-06 | Schering Corporation | Thrombin receptor antagonists |
-
2002
- 2002-10-16 IL IL16091802A patent/IL160918A0/xx not_active IP Right Cessation
- 2002-10-16 NZ NZ531869A patent/NZ531869A/en not_active IP Right Cessation
- 2002-10-16 AU AU2002335031A patent/AU2002335031C1/en not_active Ceased
- 2002-10-16 KR KR1020047005435A patent/KR100960170B1/ko not_active IP Right Cessation
- 2002-10-16 AT AT02801732T patent/ATE525378T1/de not_active IP Right Cessation
- 2002-10-16 CA CA002463628A patent/CA2463628A1/en not_active Abandoned
- 2002-10-16 MY MYPI20023859A patent/MY139335A/en unknown
- 2002-10-16 AR ARP020103876A patent/AR036832A1/es unknown
- 2002-10-16 JP JP2003536240A patent/JP4307260B2/ja not_active Expired - Fee Related
- 2002-10-16 US US10/271,715 patent/US7037920B2/en not_active Expired - Fee Related
- 2002-10-16 CN CNB028206665A patent/CN100369917C/zh not_active Expired - Fee Related
- 2002-10-16 WO PCT/US2002/032936 patent/WO2003033501A1/en active IP Right Grant
- 2002-10-16 PE PE2002001022A patent/PE20030808A1/es not_active Application Discontinuation
- 2002-10-16 MX MXPA04003610A patent/MXPA04003610A/es active IP Right Grant
- 2002-10-16 HU HU0500443A patent/HUP0500443A3/hu unknown
- 2002-10-16 PL PL02371948A patent/PL371948A1/xx not_active Application Discontinuation
- 2002-10-16 EP EP02801732A patent/EP1436298B1/en not_active Expired - Lifetime
- 2002-10-16 RU RU2004115114/04A patent/RU2319704C9/ru not_active IP Right Cessation
- 2002-10-16 BR BR0213967-7A patent/BR0213967A/pt not_active IP Right Cessation
-
2004
- 2004-04-15 EC EC2004005064A patent/ECSP045064A/es unknown
- 2004-04-15 ZA ZA200402849A patent/ZA200402849B/xx unknown
- 2004-04-16 CO CO04034781A patent/CO5570668A2/es not_active Application Discontinuation
- 2004-05-14 NO NO20042021A patent/NO329349B1/no not_active IP Right Cessation
-
2005
- 2005-12-19 US US11/311,083 patent/US20060106050A1/en not_active Abandoned
-
2008
- 2008-09-17 JP JP2008238716A patent/JP2009029820A/ja not_active Withdrawn
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