MXPA04003610A - Analogos de himbacina como antagonistas del receptor de trombina. - Google Patents

Analogos de himbacina como antagonistas del receptor de trombina.

Info

Publication number
MXPA04003610A
MXPA04003610A MXPA04003610A MXPA04003610A MXPA04003610A MX PA04003610 A MXPA04003610 A MX PA04003610A MX PA04003610 A MXPA04003610 A MX PA04003610A MX PA04003610 A MXPA04003610 A MX PA04003610A MX PA04003610 A MXPA04003610 A MX PA04003610A
Authority
MX
Mexico
Prior art keywords
alkyl
optionally substituted
himbacine
analogues
alkenyl
Prior art date
Application number
MXPA04003610A
Other languages
English (en)
Inventor
Martin C Clasby
Original Assignee
Schering Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Schering Corp filed Critical Schering Corp
Publication of MXPA04003610A publication Critical patent/MXPA04003610A/es

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

Abstract

Se describen triciclitos heterociclicos sustituidos que tienen la formula.Ver formula (I)O sales farmaceuticamente aceptables de los mismos, donde n1 y n2 son independientemente 0-2; Het es un grupo heteroaromatico mono-, bi- o triciclito opcionalmente sustituido; B es alquilo opcionalmente sustituido; R22 es -COR23 o un derivado carboxi, sulfinilo, sulfonilo, sulfonaida o aminoacido; R23 es haloalquilo, alquenilo, haloaluqenilo, alquinilo; cicloalquilo opcionalmente sustituido; cicloal-alquilo SO3H sustituido; R1, R2, R3, R9, R10, R11 son tal como se han definido en la memoria, asi como tambien composiciones farmaceuticas que los contienen y un metodo para tratar enfermedades asociadas con trombosis, ateroesclerosis, restenosis, hipertension, angina, pectoris, arritmia, insuficiencia cardiaca y cancer mediante la administracion de dichos compuestos.
MXPA04003610A 2001-10-18 2002-10-16 Analogos de himbacina como antagonistas del receptor de trombina. MXPA04003610A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33035901P 2001-10-18 2001-10-18
PCT/US2002/032936 WO2003033501A1 (en) 2001-10-18 2002-10-16 Himbacine analogues as thrombin receptor antagonists

Publications (1)

Publication Number Publication Date
MXPA04003610A true MXPA04003610A (es) 2004-07-27

Family

ID=23289411

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA04003610A MXPA04003610A (es) 2001-10-18 2002-10-16 Analogos de himbacina como antagonistas del receptor de trombina.

Country Status (23)

Country Link
US (2) US7037920B2 (es)
EP (1) EP1436298B1 (es)
JP (2) JP4307260B2 (es)
KR (1) KR100960170B1 (es)
CN (1) CN100369917C (es)
AR (1) AR036832A1 (es)
AT (1) ATE525378T1 (es)
AU (1) AU2002335031C1 (es)
BR (1) BR0213967A (es)
CA (1) CA2463628A1 (es)
CO (1) CO5570668A2 (es)
EC (1) ECSP045064A (es)
HU (1) HUP0500443A3 (es)
IL (1) IL160918A0 (es)
MX (1) MXPA04003610A (es)
MY (1) MY139335A (es)
NO (1) NO329349B1 (es)
NZ (1) NZ531869A (es)
PE (1) PE20030808A1 (es)
PL (1) PL371948A1 (es)
RU (1) RU2319704C9 (es)
WO (1) WO2003033501A1 (es)
ZA (1) ZA200402849B (es)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
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
US7235567B2 (en) * 2000-06-15 2007-06-26 Schering Corporation Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist
US7488742B2 (en) * 2000-06-15 2009-02-10 Schering Corporation Thrombin receptor antagonists
ATE494284T1 (de) 2002-04-16 2011-01-15 Schering Corp Tricyclischer thrombinrezeptorantagonist
US20070243632A1 (en) * 2003-07-08 2007-10-18 Coller Barry S Methods for measuring platelet reactivity of patients that have received drug eluting stents
ATE536889T1 (de) 2003-07-08 2011-12-15 Accumetrics Inc Kontrollierte thrombozyten-aktivierung zur überwachung der behandlung von adp-antagonisten
DE602005009355D1 (de) * 2004-05-28 2008-10-09 Schering Corp Gehinderte himbacinanaloga als thrombinrezeptorantagonisten
EP1778652A2 (en) * 2004-08-20 2007-05-02 EntreMed, Inc. Compositions and methods comprising proteinase activated receptor antagonists
AU2005294265A1 (en) * 2004-10-06 2006-04-20 University Of Rochester Treatment of pulmonary hypertension using an agent that inhibits a tissue factor pathway
CA2582639A1 (en) * 2004-10-08 2006-04-20 Schering Corporation Thrombin receptor antagonists
DK1848705T3 (da) * 2005-01-14 2010-06-14 Schering Corp EXO- og diastereoselektive synteser af himbacin-analoger
CN101137636A (zh) * 2005-01-14 2008-03-05 先灵公司 Himbacine类似物的外型选择性合成
CN101137647A (zh) * 2005-01-14 2008-03-05 先灵公司 Himbacine类似物的合成
CA2601575A1 (en) * 2005-03-31 2006-10-05 Schering Corporation Spirocyclic thrombin receptor antagonists
US7595169B2 (en) * 2005-04-27 2009-09-29 Accumetrics, Inc. Method for determining percent platelet aggregation
WO2007075808A2 (en) * 2005-12-20 2007-07-05 Schering Corporation 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
JP2009521472A (ja) * 2005-12-22 2009-06-04 シェーリング コーポレイション 心肺手術の合併症の予防としてのトロンビンレセプターアンタゴニスト
CN101460463A (zh) * 2006-03-29 2009-06-17 先灵公司 可作为凝血酶受体拮抗剂的单环和双环喜巴辛衍生物
EP2266976B1 (en) * 2006-04-13 2013-07-31 Merck Sharp & Dohme Corp. Fused ring thrombin receptor antagonists
KR20090031544A (ko) 2006-06-29 2009-03-26 쉐링 코포레이션 치환된 비사이클릭 및 트리사이클릭 트롬빈 수용체 길항제
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
JP2010505842A (ja) 2006-10-04 2010-02-25 シェーリング コーポレイション トロンビン受容体拮抗薬としての二環式誘導体および三環式誘導体
EP2078012A2 (en) * 2006-10-04 2009-07-15 Schering Corporation Thrombin receptor antagonists based on the modified tricyclic unit of himbacine
CA2673228A1 (en) * 2006-12-22 2008-07-03 Schering Corporation Disintegration promoters in solid dose wet granulation formulations
JP2010522169A (ja) * 2007-03-23 2010-07-01 シェーリング コーポレイション トロンビン受容体アンタゴニストの使用による、経皮的インターベンション後の有害事象の低減
US20080299587A1 (en) * 2007-05-03 2008-12-04 Dennis Durbin Methods of measuring inhibition of platelet aggregation by thrombin receptor antagonists
MX2010008490A (es) 2008-02-05 2010-08-18 Sanofi Aventis Triazolopiridazinas como inhibidores de par1, su produccion y su uso como medicamentos.
US8148363B2 (en) 2008-05-19 2012-04-03 Schering Corporation Heterocyclic compounds as factor IXA inhibitors
JP5789256B2 (ja) 2009-06-04 2015-10-07 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． トロンビン受容体アンタゴニストの活性代謝物
AU2010259003A1 (en) 2009-06-08 2011-11-10 Merck Sharp & Dohme Corp. A thrombin receptor antagonist and clopidogrel fixed dose tablet
TWI393716B (zh) 2009-08-04 2013-04-21 Merck Sharp & Dohme 作為ｉｘａ因子抑制劑之雜環化合物
EP2822557B1 (en) 2012-03-06 2017-08-23 Merck Sharp & Dohme Corp. Preparation and use of bicyclic himbacine derivatives as par-receptor antagonists
US9808473B2 (en) 2013-08-22 2017-11-07 Merck Sharp & Dohme Corp. Preparation and use of 3-pyridyl substituted-6,6-difluoro bicyclic himbacine derivatives as par-1 receptor antagonists
EP3035930A4 (en) 2013-08-22 2017-03-08 Merck Sharp & Dohme Corp. 7a-heterocycle substituted- 6, 6-difluoro bicyclic himbacine derivatives
EP3035929A4 (en) 2013-08-22 2017-03-15 Merck Sharp & Dohme Corp. 7a-amide substituted-6,6-difluoro bicyclic himbacine derivatives
US9969724B2 (en) 2014-04-16 2018-05-15 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
EP4185587A1 (en) 2020-07-22 2023-05-31 JANSSEN Pharmaceutica NV Compounds useful as factor xia inhibitors
US11814364B2 (en) 2021-03-18 2023-11-14 Janssen Pharmaceutica Nv Pyridine N-oxide derivatives 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
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)

* Cited by examiner, † Cited by third party
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
KR100604742B1 (ko) 2000-06-15 2006-07-26 쉐링 코포레이션 트롬빈 수용체 길항제

Also Published As

Publication number Publication date
NZ531869A (en) 2006-11-30
IL160918A0 (en) 2004-08-31
EP1436298A1 (en) 2004-07-14
NO329349B1 (no) 2010-10-04
KR100960170B1 (ko) 2010-05-26
US7037920B2 (en) 2006-05-02
AU2002335031C1 (en) 2006-11-16
RU2319704C2 (ru) 2008-03-20
JP2009029820A (ja) 2009-02-12
HUP0500443A3 (en) 2009-12-28
CO5570668A2 (es) 2005-10-31
MY139335A (en) 2009-09-30
US20030203927A1 (en) 2003-10-30
PL371948A1 (en) 2005-07-11
ZA200402849B (en) 2005-01-14
RU2319704C9 (ru) 2008-08-20
AU2002335031B2 (en) 2005-06-30
NO20042021L (no) 2004-05-14
ECSP045064A (es) 2004-05-28
JP4307260B2 (ja) 2009-08-05
JP2005529841A (ja) 2005-10-06
EP1436298B1 (en) 2011-09-21
CN100369917C (zh) 2008-02-20
KR20050036845A (ko) 2005-04-20
AR036832A1 (es) 2004-10-06
CA2463628A1 (en) 2003-04-24
WO2003033501A1 (en) 2003-04-24
BR0213967A (pt) 2005-08-30
CN1571789A (zh) 2005-01-26
RU2004115114A (ru) 2005-10-27
HUP0500443A2 (hu) 2005-08-29
ATE525378T1 (de) 2011-10-15
PE20030808A1 (es) 2003-09-22
US20060106050A1 (en) 2006-05-18

Similar Documents

Publication Publication Date Title
MXPA04003610A (es) Analogos de himbacina como antagonistas del receptor de trombina.
SG164279A1 (en) Tricyclic thrombin receptor antagonists
WO2006041872A3 (en) Thrombin receptor antagonists
MX2009003761A (es) Derivados biciclicos y triciclicos como antagonistas del receptor de trombina.
TW200640900A (en) 1-(2h)-isoquinolone derivative
NO20060195L (no) Kinolylamidderivater som CCR-5-antagonister
NO20051826L (no) Heterosyklisk substituerte piperaziner for behandling av schizofreni
AR053405A1 (es) Derivados de urea sustituidas, composiciones farmaceuticas y metodos para el tratamiento de cardiopatias
NO20052493L (no) Selekterte CGRP antagonister, fremgangsmater for fremstilling derav og deres anvendelse som farmasoytiske sammensetninger.
EA200801909A1 (ru) Соединения пиридина для лечения заболеваний, опосредованных действием простагландина
NO20052496L (no) Selekterte CGRP antagonister, fremgangsmater for fremstilling derav og anvendelse derav som medikamenter.
TW200734322A (en) Indole derivatives exhibiting PGD2 receptor antagonism
WO2006105217A3 (en) Spirocyclic thrombin receptor antagonists
NO20062021L (no) Omleirede pentanoler, fremgangsmpte for fremstilling av dette, og deres anvendelse som antiflogistika
WO2007126771A3 (en) Monocyclic and bicyclic himbacine derivatives useful as thrombin receptor antagonists
NO20072753L (no) 3-Etylidenhydrazinosubstituerte heterocykliske forbindelser som trombopoietinreseptoraktivatorer
ATE476431T1 (de) Piperidin- und azetidinderivate als glyt1- inhibitoren
WO2007075809A3 (en) Oxazoloisoquinoline derivatives as thrombin receptor antagonists
NO20023161L (no) Substituerte piperidiner, legemidler inneholdende disse forbindelser og fremgangsmåter for fremstilling av dem
MY140887A (en) Thrombin receptor antagonists
NO20000722L (no) 2-(4-aryl eller heteroaryl-piperazin-1-ylmetyl)-1H- indolderivater
NO20070157L (no) Substituerte diketopiperaziner som oksytocinantagonister
NO20063111L (no) Fremgangsmate for fremstilling av tiazolpyrimidiner
MXPA04005426A (es) Derivados de pirazol de anillos fuisionados.
ATE499366T1 (de) 1-ä(6-substituiertes alkoxychinoxalinyl)

Legal Events

Date Code Title Description
FG Grant or registration