[go: up one dir, main page]

BR0309309A - Antagonistas de receptor de trombina tricìclicos - Google Patents

Antagonistas de receptor de trombina tricìclicos

Info

Publication number
BR0309309A
BR0309309A BR0309309-3A BR0309309A BR0309309A BR 0309309 A BR0309309 A BR 0309309A BR 0309309 A BR0309309 A BR 0309309A BR 0309309 A BR0309309 A BR 0309309A
Authority
BR
Brazil
Prior art keywords
nhc
nhs0
nhso
alkyl
optionally substituted
Prior art date
Application number
BR0309309-3A
Other languages
English (en)
Other versions
BRPI0309309B8 (pt
BRPI0309309B1 (pt
Inventor
Samuel Chackalamannil
Martin C Clasby
William J Greenlee
Yuguang Wang
Yan Xia
Enrico P Veltri
Mariappan V Chelliah
Wenxue Wu
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=BR0309309(A) "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
Publication of BR0309309A publication Critical patent/BR0309309A/pt
Publication of BRPI0309309B1 publication Critical patent/BRPI0309309B1/pt
Publication of BRPI0309309B8 publication Critical patent/BRPI0309309B8/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/06—Heterocyclic 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

"ANTAGONISTAS DE RECEPTOR DE TROMBINA TRICìCLICOS". Tricíclicos substituídos por heterocíclicos da Fórmula (I) ou um seu sal farmaceuticamente aceitável onde: a linha pontilhada simples representa uma ligação simples opcional; (a) representa uma ligação dupla opcional; n é 0-2; Q é cicloalquila, opcionalmente substituída por R^ 13^ e R^ 14^, cada R^ 13^ é independentemente selecionado de H~ 1~ (C~ 1~-C~ 6~)alquila, (C~ 3~-C~ 8~)cicloalquila, -(CH~ 2~)~ n6~NHC(O)OR^ 16b^, -(CH~ 2~)~ n6~NHC(O)R^ 16b^, -(CH~ 2~)~ n6~NHC(O)NR^ 4^R^ 5^, (CH~ 2~)~ n6~NHS0~ 2~R^ 16^, -(CH~ 2~)~ n6~NHSO~ 2NR^ 4~R^ 5^ e -(CH~ 2~)~ n6~ C(O)NR^ 28^R^ 29^ onde n~ 6~ é 0-4, haloalquila e halogênio; cada R^ 14^ é independentemente selecionado de H, (C~ 1~-C~ 6~)alquila, -OH, (C~ 1~-C~ 6~)alcóxi, R^ 27^-arila, (C~ 1~-C~ 6~)alquila, heteroarila, heteroarilalquila, heterociclila, heterociclilalquila, -(CH~ 2~)~ n6~NHC(O)OR^ 16b^, -(CH~ 2~)~ n6~NHC(O)R^ 16b^, -(CH~ 2~)~ n6~NHC(O)NR^ 4^R^ 5^, -(CH~ 2~)~ n6~NHSO~ 2~R^ 16^, -(CH~ 2~)~ n6~NHS0~ 2~NR^ 4^R^ 5^ e -(CH~ 2~)~ n6~C(O)NR^ 28^R^ 29^ onde n~ 6~ é 0-4, halogênio e haloalquila; ou R^ 13^ e R^ 14^ tomados juntos formam um anel espirocíclico ou heteroespirocíclico de 3-6 átomos; onde pelo menos um de R^ 13^ ou R^ 14^ é selecionado do grupo consistindo em -(CH~ 2~)~ n6~NHC(O)OR^ 16b^, -(CH~ 2~)~ n6~NHC(O)R^ 16b^, -(CH~ 2~)~ n6~NHC(O)NR^ 4^R^ 5^, -(CH~ 2~)~ n6~NHS0~ 2~R^ 16^, -(CH~ 2~)~ n6~NHSO~ 2~NR^ 4^R^ 5^ e -(CH~ 2~)~ n6~C(O)NR^ 28^R^ 29^ onde n~ 6~ é 0-4; Het é um grupo heteroarila mono- ou bicíclico opcionalmente substituído; e B é uma ligação, alquileno, ou alquenileno ou alquinileno opcionalmente substituído, onde os substituintes restantes são conforme definido no relatório, são descritos, bem como composições farmaceuticamente aceitáveis contendo-os e um método de tratamento de doenças associadas com trombose, aterosclerose, restenose, hipertensão, angina peitoral, arritmia, falência cardíaca e câncer através da administração dos ditos compostos. Terapia de combinação com outros agentes cardiovasculares é também reivindicada.
BRPI0309309A 2002-04-16 2003-04-14 antagonistas de receptor de trombina tricíclicos BRPI0309309B8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37307202P 2002-04-16 2002-04-16
PCT/US2003/011510 WO2003089428A1 (en) 2002-04-16 2003-04-14 Tricyclic thrombin receptor antagonists

Publications (3)

Publication Number Publication Date
BR0309309A true BR0309309A (pt) 2005-02-15
BRPI0309309B1 BRPI0309309B1 (pt) 2018-09-04
BRPI0309309B8 BRPI0309309B8 (pt) 2021-05-25

Family

ID=29250954

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0309309A BRPI0309309B8 (pt) 2002-04-16 2003-04-14 antagonistas de receptor de trombina tricíclicos

Country Status (34)

Country Link
US (3) US7304078B2 (pt)
EP (5) EP2062890B1 (pt)
JP (2) JP4558331B2 (pt)
KR (1) KR101026929B1 (pt)
CN (1) CN1659162B (pt)
AR (1) AR039570A1 (pt)
AT (3) ATE494284T1 (pt)
AU (1) AU2003221932B2 (pt)
BR (1) BRPI0309309B8 (pt)
CA (1) CA2482858C (pt)
CY (3) CY1107184T1 (pt)
DE (3) DE60317493T3 (pt)
DK (2) DK2065384T3 (pt)
EC (1) ECSP045368A (pt)
ES (3) ES2357876T3 (pt)
FR (1) FR15C0047I2 (pt)
HK (3) HK1070887A1 (pt)
IL (1) IL164585A (pt)
LT (1) LTC1495018I2 (pt)
LU (1) LU92759I2 (pt)
MX (1) MXPA04010308A (pt)
MY (1) MY144040A (pt)
NL (1) NL300746I2 (pt)
NO (2) NO330500B1 (pt)
NZ (2) NZ575139A (pt)
PE (1) PE20040412A1 (pt)
PL (1) PL214718B1 (pt)
PT (2) PT1495018E (pt)
RU (2) RU2329264C9 (pt)
SG (1) SG164279A1 (pt)
SI (2) SI1495018T1 (pt)
TW (1) TWI343919B (pt)
WO (1) WO2003089428A1 (pt)
ZA (1) ZA200408342B (pt)

Families Citing this family (62)

* 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
US20040192753A1 (en) * 2000-06-15 2004-09-30 Samuel Chackalamannil Methods of use of thrombin receptor antagonists
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
CA2567981C (en) * 2004-05-28 2010-08-31 Schering Corporation Constrained himbacine analogs as thrombin receptor antagonists
JP2008515908A (ja) * 2004-10-06 2008-05-15 ユニバーシティー オブ ロチェスター 組織因子経路を阻害する薬剤を使用する、肺高血圧症の治療
AR056262A1 (es) * 2005-01-14 2007-10-03 Schering Corp Preparacion de alcoholes propargilicos y esteres intermediarios de analogos de himbacina
JP4775971B2 (ja) 2005-01-14 2011-09-21 シェーリング コーポレイション ヒンバシンアナログのエキソ−選択的合成
ATE458726T1 (de) * 2005-01-14 2010-03-15 Schering Corp Exo- und diastereoselektive synthese von himbacin-analoga
WO2006076564A1 (en) * 2005-01-14 2006-07-20 Schering Corporation Synthesis of himbacine analogs
US7541471B2 (en) * 2005-01-14 2009-06-02 Schering Corporation Synthesis of himbacine analogs
KR20070116066A (ko) * 2005-03-31 2007-12-06 쉐링 코포레이션 스피로사이클릭 트롬빈 수용체 길항제
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
TW200812619A (en) * 2006-04-06 2008-03-16 Schering Corp TRA combination therapies
CN101466704A (zh) * 2006-04-13 2009-06-24 先灵公司 稠合环凝血酶受体拮抗剂
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
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
EP2069326B1 (en) * 2006-10-04 2015-03-18 Merck Sharp & Dohme Corp. 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
WO2008079260A2 (en) * 2006-12-22 2008-07-03 Schering Corporation Disintegration promoters in solid dose wet granulation formulations
AU2008230116A1 (en) * 2007-03-23 2008-10-02 Schering Corporation Reduction of adverse events.after percutaneous intervention by use of a thrombin receptor antagonist
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
MY148732A (en) 2008-02-05 2013-05-31 Sanofi Aventis Triazolium salts as par1 inhibitors, production thereof, and use as medicaments
WO2009124103A2 (en) * 2008-04-02 2009-10-08 Schering Corporation Combination therapies comprising par1 antagonists with par4 antagonists
WO2009143039A2 (en) 2008-05-19 2009-11-26 Schering Corporation Heterocyclic compounds as factor ixa inhibitors
DK2438060T3 (da) * 2009-06-04 2014-01-13 Merck Sharp & Dohme Aktiv metabolit af en trombin-receptor-antagonist
CA2764172A1 (en) 2009-06-08 2010-12-16 Schering Corporation A thrombin receptor antagonist and clopidogrel fixed dose tablet
AR077695A1 (es) 2009-08-04 2011-09-14 Schering Corp Derivados de pirimidina como inhibidores del factor ixa
EP2558465B1 (de) 2010-04-16 2014-12-17 Sanofi Trizyklische pyridyl-vinyl-pyrrole als par1-inhibitoren
EP2558462B1 (de) 2010-04-16 2014-10-22 Sanofi Pyridyl-vinyl-pyrazolo-chinoline als par1-inhibitoren
KR101303348B1 (ko) 2010-06-25 2013-09-03 한국화학연구원 트롬빈 수용체 길항제인 ［6＋5］접합 바이사이클, 그의 제조방법 및 그를 포함하는 약제학적 조성물
US9340530B2 (en) 2012-03-06 2016-05-17 Merck Sharp & Dohme Corp. Preparation and use of bicyclic himbacine derivatives as PAR-1 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
WO2015026685A1 (en) 2013-08-22 2015-02-26 Merck Sharp & Dohme Corp. 7a-heterocycle substituted- 6, 6-difluoro bicyclic himbacine derivatives
EP3035928B1 (en) * 2013-08-22 2023-10-18 Merck Sharp & Dohme LLC 3'-pyridyl 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
WO2015160636A1 (en) 2014-04-16 2015-10-22 Merck Sharp & Dohme Corp. Factor ixa inhibitors
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
WO2017134200A1 (en) * 2016-02-05 2017-08-10 Sanovel Ilac Sanayi Ve Ticaret A.S. A novel pharmaceutical composition of vorapaxar and metoprolol
TR201601548A2 (tr) * 2016-02-05 2018-03-21 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Vorapaksar ve metoprololün bi̇r farmasöti̇k kompozi̇syonu
CN107304200B (zh) * 2016-04-22 2021-09-21 江苏天士力帝益药业有限公司 一种新的喜巴辛类似物及其在医药中的应用
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
WO2022018156A1 (en) 2020-07-22 2022-01-27 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
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
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
FR3134314A1 (fr) 2022-04-08 2023-10-13 Cvasthera Composition pharmaceutique à base de vorapaxar et son utilisation pour le traitement des maladies inflammatoires intestinales

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2623810B2 (fr) 1987-02-17 1992-01-24 Sanofi Sa Sels de l'alpha-(tetrahydro-4,5,6,7 thieno(3,2-c) pyridyl-5) (chloro-2 phenyl) -acetate de methyle dextrogyre et compositions pharmaceutiques en contenant
IL106197A (en) 1992-07-30 1999-11-30 Cor Therapeutics Inc Agagonists for the rhombin receptors and pharmaceutical preparations containing them
US5576328A (en) 1994-01-31 1996-11-19 Elf Sanofi Method for the secondary prevention of ischemic events
ZA9810685B (en) * 1997-11-25 1999-12-23 Schering Corp Thrombin receptor antagonists.
US6063847A (en) * 1997-11-25 2000-05-16 Schering Corporation Thrombin receptor antagonists
FR2779726B1 (fr) 1998-06-15 2001-05-18 Sanofi Sa Forme polymorphe de l'hydrogenosulfate de clopidogrel
US20040192753A1 (en) 2000-06-15 2004-09-30 Samuel Chackalamannil Methods of use of thrombin receptor antagonists
MXPA02012447A (es) 2000-06-15 2003-04-25 Schering Corp Antagonistas receptores de trombina.
US7488742B2 (en) 2000-06-15 2009-02-10 Schering Corporation Thrombin receptor antagonists
NZ531869A (en) 2001-10-18 2006-11-30 Schering Corp Himbacine analogues as thrombin receptor antagonists

Also Published As

Publication number Publication date
PT1495018E (pt) 2008-02-19
NZ575139A (en) 2010-08-27
RU2329264C2 (ru) 2008-07-20
LTC1495018I2 (lt) 2017-04-10
EP1495018A1 (en) 2005-01-12
DE60317493T3 (de) 2018-07-12
NL300746I1 (pt) 2016-01-21
CA2482858A1 (en) 2003-10-30
SI2065384T1 (sl) 2011-05-31
CY2015029I2 (el) 2016-04-13
EP2062890A1 (en) 2009-05-27
NZ535880A (en) 2007-11-30
RU2329264C9 (ru) 2009-04-20
ATE455774T1 (de) 2010-02-15
EP1982984B1 (en) 2013-02-13
EP1495018B3 (en) 2011-03-16
ATE378330T1 (de) 2007-11-15
EP1860106A1 (en) 2007-11-28
RU2008106401A (ru) 2009-08-27
BRPI0309309B8 (pt) 2021-05-25
NO330500B1 (no) 2011-05-02
NL300746I2 (pt) 2016-01-21
EP1982984A2 (en) 2008-10-22
IL164585A (en) 2010-11-30
NO2015016I2 (no) 2015-07-09
SG164279A1 (en) 2010-09-29
CY1107184T1 (el) 2012-10-24
DK1495018T3 (da) 2008-02-18
ZA200408342B (en) 2006-05-31
DE60335679D1 (de) 2011-02-17
KR20040099441A (ko) 2004-11-26
KR101026929B1 (ko) 2011-04-04
MY144040A (en) 2011-07-29
HK1123302A1 (en) 2009-06-12
US20070179187A1 (en) 2007-08-02
LU92759I2 (en) 2015-08-31
AU2003221932B2 (en) 2007-11-22
NO2015016I1 (no) 2015-07-20
HK1129893A1 (en) 2009-12-11
IL164585A0 (en) 2005-12-18
PL373332A1 (en) 2005-08-22
ES2297150T3 (es) 2008-05-01
AR039570A1 (es) 2005-02-23
SI1495018T1 (sl) 2008-04-30
TWI343919B (en) 2011-06-21
DK2065384T3 (da) 2011-05-02
CA2482858C (en) 2010-11-30
FR15C0047I2 (fr) 2016-05-06
HK1070887A1 (en) 2005-06-30
EP1860106B1 (en) 2010-01-20
EP2062890B1 (en) 2011-01-05
PT2065384E (pt) 2011-03-16
CN1659162B (zh) 2011-08-31
CN1659162A (zh) 2005-08-24
ES2338171T3 (es) 2010-05-04
CY2015029I1 (el) 2016-04-13
AU2003221932A1 (en) 2003-11-03
ECSP045368A (es) 2005-01-03
MXPA04010308A (es) 2005-02-03
PE20040412A1 (es) 2004-07-12
US20030216437A1 (en) 2003-11-20
CY1111363T1 (el) 2015-08-05
JP2010132710A (ja) 2010-06-17
EP1495018B1 (en) 2007-11-14
JP4558331B2 (ja) 2010-10-06
US7713999B2 (en) 2010-05-11
WO2003089428A1 (en) 2003-10-30
BRPI0309309B1 (pt) 2018-09-04
DE60317493T2 (de) 2008-09-18
TW200404068A (en) 2004-03-16
JP2005528406A (ja) 2005-09-22
RU2004133375A (ru) 2005-07-10
ES2357876T3 (es) 2011-05-03
ATE494284T1 (de) 2011-01-15
PL214718B1 (pl) 2013-09-30
DE60317493D1 (en) 2011-01-13
EP1982984A3 (en) 2008-10-29
EP2065384A1 (en) 2009-06-03
FR15C0047I1 (pt) 2015-08-28
ES2297150T7 (es) 2012-03-16
US7304078B2 (en) 2007-12-04
US20070270439A1 (en) 2007-11-22
NO20044963L (no) 2004-11-15
EP2065384B1 (en) 2011-01-05
DE60331114D1 (de) 2010-03-11

Similar Documents

Publication Publication Date Title
BR0309309A (pt) Antagonistas de receptor de trombina tricìclicos
MY139335A (en) Substituted tricyclic himbacine derivatives that are useful as thrombin receptor antagonists
RU2704129C2 (ru) Соединение 2-аминопиримидина и фармацевтическая композиция и применение данного соединения
RU2495873C2 (ru) Новое урациловое соединение или его соль, обладающие ингибирующей активностью относительно дезоксиуридинтрифосфатазы человека
NO20071140L (no) Nye piperidinderivater som histamin H3 reseptorligander for behandling av depresjon
MX2009003761A (es) Derivados biciclicos y triciclicos como antagonistas del receptor de trombina.
AR049652A1 (es) Sales cuaternarias antagonistas del receptor ccr2
NO20072344L (no) Trombineresptorantagonister.
TW200718697A (en) Spirocyclic thrombin receptor antagonists
RU2011108563A (ru) Способы лечения талассемии
PE20080839A1 (es) Determinadas amidas sustituidas, metodo de elaboracion y metodo de uso de las mismas
EA201100975A1 (ru) Производные 1,2,4-оксадиазола и их применение в терапии
AR057104A1 (es) Diaminopirimidinas como moduladores de p2 x3 y p2x2 /3 y composicion farmaceutica
AR057989A1 (es) Derivados de indol-2-il-amida 1,5-sustituida. procesos de obtencion y composiciones farmaceuticas
AR040626A1 (es) Derivados de quinolina utiles como ligandos del receptor del neuropeptido y (npy)
AR053405A1 (es) Derivados de urea sustituidas, composiciones farmaceuticas y metodos para el tratamiento de cardiopatias
ECSP056016A (es) Nuevos derivados de 2-piridinacarboxamida
AR056883A1 (es) Derivados de 7-azaindol-2 carboxamida, un proceso para la preparacion de los mismos, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades asociadas con la modulacion de receptores de h3
NO20051694L (no) Heterosykliske forbindelser
AR057769A1 (es) Pirazolo pirimidinas como inhibidores de map quinasa p38, metodos para utilizarlos y composiciones farmaceuticas
AR037907A1 (es) Derivados de azaindolilalquilamina como ligandos de 5-hidroxitriptamina-6
MX2013004407A (es) Derivado de piridina y agente medicinal.
NO20073729L (no) Heterocykliske forbindelser som CCR2B-antagonister
MX2009009121A (es) Aminoamidas como antagonistas de orexina.
EP1757594A4 (en) quinazoline derivative

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B25D Requested change of name of applicant approved

Owner name: MERCK SHARP AND DOHME CORP. (US)

B25G Requested change of headquarter approved

Owner name: MERCK SHARP AND DOHME CORP. (US)

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 10 (DEZ) ANOS CONTADOS A PARTIR DE 04/09/2018, OBSERVADAS AS CONDICOES LEGAIS.

B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 14/04/2003 OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF

B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

Free format text: REFERENTE A 20A ANUIDADE.

B24J Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12)

Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2718 DE 07-02-2023 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.