DE60335679D1 - Tricyclischer Thrombinrezeptorantagonist - Google Patents

Tricyclischer Thrombinrezeptorantagonist

Info

Publication number
DE60335679D1
DE60335679D1 DE60335679T DE60335679T DE60335679D1 DE 60335679 D1 DE60335679 D1 DE 60335679D1 DE 60335679 T DE60335679 T DE 60335679T DE 60335679 T DE60335679 T DE 60335679T DE 60335679 D1 DE60335679 D1 DE 60335679D1
Authority
DE
Germany
Prior art keywords
receptor antagonist
thrombin receptor
tricyclic thrombin
tricyclic
antagonist
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 - Lifetime
Application number
DE60335679T
Other languages
English (en)
Inventor
Samuel Chackalamannil
William J Greenlee
Yuguang Wang
Yan Xia
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=29250954&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=DE60335679(D1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Application granted granted Critical
Publication of DE60335679D1 publication Critical patent/DE60335679D1/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
DE60335679T 2002-04-16 2003-04-14 Tricyclischer Thrombinrezeptorantagonist Expired - Lifetime DE60335679D1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US37307202P 2002-04-16 2002-04-16

Publications (1)

Publication Number Publication Date
DE60335679D1 true DE60335679D1 (de) 2011-02-17

Family

ID=29250954

Family Applications (3)

Application Number Title Priority Date Filing Date
DE60317493.0T Expired - Lifetime DE60317493T3 (de) 2002-04-16 2003-04-14 Trizyklische thrombin rezeptor antagonisten
DE60331114T Expired - Lifetime DE60331114D1 (de) 2002-04-16 2003-04-14 Trizyklische Thrombinrezeptorantagonisten
DE60335679T Expired - Lifetime DE60335679D1 (de) 2002-04-16 2003-04-14 Tricyclischer Thrombinrezeptorantagonist

Family Applications Before (2)

Application Number Title Priority Date Filing Date
DE60317493.0T Expired - Lifetime DE60317493T3 (de) 2002-04-16 2003-04-14 Trizyklische thrombin rezeptor antagonisten
DE60331114T Expired - Lifetime DE60331114D1 (de) 2002-04-16 2003-04-14 Trizyklische Thrombinrezeptorantagonisten

Country Status (34)

Country Link
US (3) US7304078B2 (de)
EP (5) EP1495018B3 (de)
JP (2) JP4558331B2 (de)
KR (1) KR101026929B1 (de)
CN (1) CN1659162B (de)
AR (1) AR039570A1 (de)
AT (3) ATE455774T1 (de)
AU (1) AU2003221932B2 (de)
BR (1) BRPI0309309B8 (de)
CA (1) CA2482858C (de)
CY (3) CY1107184T1 (de)
DE (3) DE60317493T3 (de)
DK (2) DK2065384T3 (de)
EC (1) ECSP045368A (de)
ES (3) ES2357876T3 (de)
FR (1) FR15C0047I2 (de)
HK (3) HK1070887A1 (de)
IL (1) IL164585A (de)
LT (1) LTC1495018I2 (de)
LU (1) LU92759I2 (de)
MX (1) MXPA04010308A (de)
MY (1) MY144040A (de)
NL (1) NL300746I1 (de)
NO (2) NO330500B1 (de)
NZ (2) NZ575139A (de)
PE (1) PE20040412A1 (de)
PL (1) PL214718B1 (de)
PT (2) PT2065384E (de)
RU (2) RU2329264C9 (de)
SG (1) SG164279A1 (de)
SI (2) SI1495018T1 (de)
TW (1) TWI343919B (de)
WO (1) WO2003089428A1 (de)
ZA (1) ZA200408342B (de)

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US20040192753A1 (en) * 2000-06-15 2004-09-30 Samuel Chackalamannil Methods of use of thrombin receptor antagonists
US7442712B2 (en) * 2004-05-28 2008-10-28 Schering Corporation Constrained himbacine analogs as thrombin receptor antagonists
WO2006042017A2 (en) * 2004-10-06 2006-04-20 University Of Rochester Treatment of pulmonary hypertension using an agent that inhibits a tissue factor pathway
US7541471B2 (en) * 2005-01-14 2009-06-02 Schering Corporation Synthesis of himbacine analogs
US20060172397A1 (en) * 2005-01-14 2006-08-03 Schering Corporation Preparation of chiral propargylic alcohol and ester intermediates of himbacine analogs
WO2006076452A2 (en) * 2005-01-14 2006-07-20 Schering Corporation An exo-selective synthesis of himbacine analogs
DE602006020414D1 (en) * 2005-01-14 2011-04-14 Schering Corp Synthese von himbacinanaloga
ATE458726T1 (de) * 2005-01-14 2010-03-15 Schering Corp Exo- und diastereoselektive synthese von himbacin-analoga
WO2006105217A2 (en) 2005-03-31 2006-10-05 Schering Corporation Spirocyclic thrombin receptor antagonists
WO2007075808A2 (en) * 2005-12-20 2007-07-05 Schering Corporation Methods for preventing and/or treating a cell proliferative disorder
CN101384259A (zh) * 2005-12-22 2009-03-11 先灵公司 作为预防来自心肺外科手术的并发症的凝血酶受体拮抗剂
PE20080183A1 (es) * 2006-04-06 2008-03-10 Schering Corp Terapias de combinacion de tra
WO2007120730A2 (en) 2006-04-13 2007-10-25 Schering Corporation Fused ring thrombin receptor antagonists
WO2008005262A1 (en) * 2006-06-29 2008-01-10 Schering Corporation Substituted bicyclic and tricyclic thrombin receptor antagonists
TWI367112B (en) * 2006-06-30 2012-07-01 Schering Corp Immediate-release tablet formulations of a thrombin receptor antagonist
AR061727A1 (es) * 2006-06-30 2008-09-17 Schering Corp Sintesis de dietil [[ 5- ( 3-fluorofenil) -piridin -2il] metil] fosfonato
DE102006036023A1 (de) 2006-08-02 2008-02-07 Sanofi-Aventis Imino-imidazo-pyridinderivate mit antithrombotischer Aktivität
TWI343262B (en) * 2006-09-26 2011-06-11 Schering Corp Rapidly disintegrating lyophilized oral formulations of a thrombin receptor antagonist
AR063095A1 (es) * 2006-10-04 2008-12-30 Schering Corp Antagonistas del receptor de trombina basados en la unidad triciclica modificada de himbacina
CN101541782A (zh) 2006-10-04 2009-09-23 先灵公司 作为凝血酶受体拮抗剂的二环和三环衍生物
EP2120879A2 (de) * 2006-12-22 2009-11-25 Schering Corporation Desintegrationspromoter in nassgranulat-formulierungen mit fester dosierung
US20080234236A1 (en) * 2007-03-23 2008-09-25 Veltri Enrico P Reduction of adverse events after percutaneous intervention by use of a thrombin receptor antagonist
AU2009211888B2 (en) 2008-02-05 2013-06-20 Sanofi Triazolium salts as PAR1 inhibitors, production thereof, and use as medicaments
DK2240487T3 (da) 2008-02-05 2012-04-02 Sanofi Sa Triazolopyridaziner som para-inhibitorer, fremstilling og anvendelse heraf som lægemiddel
WO2009124103A2 (en) * 2008-04-02 2009-10-08 Schering Corporation Combination therapies comprising par1 antagonists with par4 antagonists
CA2724430A1 (en) 2008-05-19 2009-11-26 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
CA2764172A1 (en) 2009-06-08 2010-12-16 Schering Corporation A thrombin receptor antagonist and clopidogrel fixed dose tablet
EP2462123B1 (de) 2009-08-04 2013-10-02 Merck Sharp & Dohme Corp. 4,5,6-trisubstituierte pyrimidin- derivate als factor ixa inhibitoren
PL2558462T3 (pl) 2010-04-16 2015-03-31 Sanofi Sa Pirydylo-winylo-pirazolo-chinoliny jako inhibitory PAR1
PL2558465T3 (pl) 2010-04-16 2015-05-29 Sanofi Sa Trycykliczne pirydylo-winylo-pirole jako inhibitory receptora aktywowanego proteazą 1 (PAR1)
KR101303348B1 (ko) 2010-06-25 2013-09-03 한국화학연구원 트롬빈 수용체 길항제인 [6+5]접합 바이사이클, 그의 제조방법 및 그를 포함하는 약제학적 조성물
WO2013134012A1 (en) 2012-03-06 2013-09-12 Merck Sharp & Dohme Corp. Preparation and use of bicyclic himbacine derivatives as par-receptor antagonists
WO2015013083A1 (en) * 2013-07-22 2015-01-29 Merck Sharp & Dohme Corp. Co-crystal of the par-1 receptor antagonist vorapaxar and aspirin
US9701669B2 (en) 2013-08-22 2017-07-11 Merck Sharp & Dohme Corp. Preparation and use of 7a-amide substituted- 6,6-difluoro bicyclic himbacine derivatives as PAR-1 receptor antagonists
WO2015026686A1 (en) * 2013-08-22 2015-02-26 Merck Sharp & Dohme Corp. 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
FR3014693B1 (fr) 2013-12-16 2016-01-08 Pf Medicament Utilisation de la 3-(2-chloro-phenyl)-1-[4-(4-fluoro-benzyl)-piperazin-1-yl]-propenone pour la prevention et/ou le traitement des pathologies fonctionnelles pelvi-perineales
EP3131897B8 (de) 2014-04-16 2022-08-03 Merck Sharp & Dohme LLC Faktor-ixa-hemmer
DE102014108210A1 (de) 2014-06-11 2015-12-17 Dietrich Gulba Rodentizid
CN105985303B (zh) * 2015-02-13 2020-08-14 上海彩迩文生化科技有限公司 抗凝血剂的制备方法、中间体及其制备方法
CN106478608A (zh) * 2015-09-01 2017-03-08 博瑞生物医药(苏州)股份有限公司 沃拉帕沙的硫酸盐的结晶多晶型物
CN106749201A (zh) * 2015-11-25 2017-05-31 博瑞生物医药(苏州)股份有限公司 一种沃拉帕沙及其中间体的制备方法
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CN106236779A (zh) * 2016-08-22 2016-12-21 孔五 一种脐带血富血小板血浆prp的制备方法
FR3090317B1 (fr) 2018-12-19 2021-05-07 Cvasthera Utilisation d’un antagoniste de par-1 pour le traitement d’une maladie inflammatoire chronique intestinale
CN110407819B (zh) * 2019-08-02 2020-06-26 牡丹江医学院 一种作为预防外科手术并发症的凝血酶受体拮抗剂
US20210113536A1 (en) * 2019-10-21 2021-04-22 United States Government as Represented by the Department of Veteran Affairs Methods and compositions for detecting and treating venous thromboembolism
FR3109089B1 (fr) 2020-04-08 2023-04-14 Cvasthera Composition pharmaceutique pour le traitement des maladies inflammatoires intestinales
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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
US11845748B2 (en) 2021-03-18 2023-12-19 Janssen Pharmaceutica Nv Bicyclic pyridine N-oxide derivatives useful as a factor XIa inhibitors
EP4070658A1 (de) 2021-04-06 2022-10-12 BIORoxx GmbH Verwendung von blutgerinnungshemmenden verbindungen als rodentizide
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
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Also Published As

Publication number Publication date
SI1495018T1 (sl) 2008-04-30
MXPA04010308A (es) 2005-02-03
NO20044963L (no) 2004-11-15
ECSP045368A (es) 2005-01-03
KR101026929B1 (ko) 2011-04-04
ATE455774T1 (de) 2010-02-15
CA2482858A1 (en) 2003-10-30
BR0309309A (pt) 2005-02-15
NL300746I2 (de) 2016-01-21
DK1495018T3 (da) 2008-02-18
ES2297150T3 (es) 2008-05-01
FR15C0047I2 (fr) 2016-05-06
HK1123302A1 (en) 2009-06-12
RU2004133375A (ru) 2005-07-10
JP4558331B2 (ja) 2010-10-06
IL164585A (en) 2010-11-30
ES2357876T3 (es) 2011-05-03
PT1495018E (pt) 2008-02-19
CY1107184T1 (el) 2012-10-24
AU2003221932B2 (en) 2007-11-22
EP1495018A1 (de) 2005-01-12
NL300746I1 (de) 2016-01-21
RU2329264C2 (ru) 2008-07-20
ATE494284T1 (de) 2011-01-15
KR20040099441A (ko) 2004-11-26
NZ535880A (en) 2007-11-30
CN1659162A (zh) 2005-08-24
SI2065384T1 (sl) 2011-05-31
US7304078B2 (en) 2007-12-04
DE60317493T2 (de) 2008-09-18
EP1982984A2 (de) 2008-10-22
EP1860106B1 (de) 2010-01-20
BRPI0309309B1 (pt) 2018-09-04
EP1495018B1 (de) 2007-11-14
CY2015029I2 (el) 2016-04-13
RU2329264C9 (ru) 2009-04-20
JP2005528406A (ja) 2005-09-22
NO2015016I2 (no) 2015-07-09
US20070179187A1 (en) 2007-08-02
NZ575139A (en) 2010-08-27
EP1982984A3 (de) 2008-10-29
CA2482858C (en) 2010-11-30
SG164279A1 (en) 2010-09-29
ES2297150T7 (es) 2012-03-16
EP2065384A1 (de) 2009-06-03
DE60331114D1 (de) 2010-03-11
AU2003221932A1 (en) 2003-11-03
IL164585A0 (en) 2005-12-18
CN1659162B (zh) 2011-08-31
ATE378330T1 (de) 2007-11-15
DK2065384T3 (da) 2011-05-02
PL214718B1 (pl) 2013-09-30
PE20040412A1 (es) 2004-07-12
LU92759I2 (en) 2015-08-31
AR039570A1 (es) 2005-02-23
CY1111363T1 (el) 2015-08-05
US7713999B2 (en) 2010-05-11
JP2010132710A (ja) 2010-06-17
EP2062890A1 (de) 2009-05-27
WO2003089428A1 (en) 2003-10-30
NO2015016I1 (no) 2015-07-20
US20070270439A1 (en) 2007-11-22
ES2338171T3 (es) 2010-05-04
TW200404068A (en) 2004-03-16
PL373332A1 (en) 2005-08-22
DE60317493D1 (en) 2011-01-13
BRPI0309309B8 (pt) 2021-05-25
CY2015029I1 (el) 2016-04-13
RU2008106401A (ru) 2009-08-27
US20030216437A1 (en) 2003-11-20
EP2062890B1 (de) 2011-01-05
FR15C0047I1 (de) 2015-08-28
EP1495018B3 (de) 2011-03-16
ZA200408342B (en) 2006-05-31
DE60317493T3 (de) 2018-07-12
PT2065384E (pt) 2011-03-16
EP1860106A1 (de) 2007-11-28
EP2065384B1 (de) 2011-01-05
HK1070887A1 (en) 2005-06-30
EP1982984B1 (de) 2013-02-13
TWI343919B (en) 2011-06-21
HK1129893A1 (en) 2009-12-11
NO330500B1 (no) 2011-05-02
LTC1495018I2 (lt) 2017-04-10
MY144040A (en) 2011-07-29

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