WO2002098856A3 - Piperazine oxyquinoline (naphthaline) platelet adenosine diphosphate receptor antagonists - Google Patents

Piperazine oxyquinoline (naphthaline) platelet adenosine diphosphate receptor antagonists Download PDF

Info

Publication number
WO2002098856A3
WO2002098856A3 PCT/US2002/017821 US0217821W WO02098856A3 WO 2002098856 A3 WO2002098856 A3 WO 2002098856A3 US 0217821 W US0217821 W US 0217821W WO 02098856 A3 WO02098856 A3 WO 02098856A3
Authority
WO
WIPO (PCT)
Prior art keywords
naphthaline
oxyquinoline
piperazine
adenosine diphosphate
receptor antagonists
Prior art date
Application number
PCT/US2002/017821
Other languages
French (fr)
Other versions
WO2002098856A2 (en
Inventor
Judi A Bryant
Brad O Buckman
Imadul Islam
Raju Mohan
Michael M Morrissey
Guo Ping Wei
Wei Xu
Shendong Yuan
Original Assignee
Schering Ag
Judi A Bryant
Brad O Buckman
Imadul Islam
Raju Mohan
Michael M Morrissey
Guo Ping Wei
Wei Xu
Shendong Yuan
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 Ag, Judi A Bryant, Brad O Buckman, Imadul Islam, Raju Mohan, Michael M Morrissey, Guo Ping Wei, Wei Xu, Shendong Yuan filed Critical Schering Ag
Priority to JP2003501845A priority Critical patent/JP4409936B2/en
Priority to EP02746471A priority patent/EP1412349A2/en
Priority to AU2002316191A priority patent/AU2002316191A1/en
Publication of WO2002098856A2 publication Critical patent/WO2002098856A2/en
Publication of WO2002098856A3 publication Critical patent/WO2002098856A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/205—Radicals derived from carbonic acid
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Compounds of the following formula (I): where a, b, R?1, R2, R3, R4 and R6¿ are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.
PCT/US2002/017821 2001-06-06 2002-06-06 Piperazine oxyquinoline (naphthaline) platelet adenosine diphosphate receptor antagonists WO2002098856A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
JP2003501845A JP4409936B2 (en) 2001-06-06 2002-06-06 Platelet adenosine diphosphate receptor antagonist
EP02746471A EP1412349A2 (en) 2001-06-06 2002-06-06 Piperazine oxyquinoline (naphthaline) platelet adenosine diphosphate receptor antagonists
AU2002316191A AU2002316191A1 (en) 2001-06-06 2002-06-06 Piperazine oxyquinoline (naphthaline) platelet adenosine diphosphate receptor antagonists

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US29649801P 2001-06-06 2001-06-06
US60/296,498 2001-06-06
US10/163,742 2002-06-05
US10/163,742 US6861424B2 (en) 2001-06-06 2002-06-05 Platelet adenosine diphosphate receptor antagonists

Publications (2)

Publication Number Publication Date
WO2002098856A2 WO2002098856A2 (en) 2002-12-12
WO2002098856A3 true WO2002098856A3 (en) 2004-03-04

Family

ID=26859907

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/017821 WO2002098856A2 (en) 2001-06-06 2002-06-06 Piperazine oxyquinoline (naphthaline) platelet adenosine diphosphate receptor antagonists

Country Status (5)

Country Link
US (4) US6861424B2 (en)
EP (1) EP1412349A2 (en)
JP (1) JP4409936B2 (en)
AU (1) AU2002316191A1 (en)
WO (1) WO2002098856A2 (en)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7998986B2 (en) 2001-12-21 2011-08-16 Exelixis Patent Company Llc Modulators of LXR
US7482366B2 (en) 2001-12-21 2009-01-27 X-Ceptor Therapeutics, Inc. Modulators of LXR
OA12970A (en) * 2002-12-11 2006-10-13 Schering Ag 2-aminocarbonyl-quinoline compounds as platelet adenosine diphosphate receptor antagonists.
US7488739B2 (en) * 2003-07-24 2009-02-10 Astellas Pharma Inc. Quinolone derivative or salt thereof
CA2581638A1 (en) * 2004-09-29 2006-04-13 Portola Pharmaceuticals, Inc. Substituted 2h-1,3-benzoxazin-4(3h)-ones
TW200640877A (en) * 2005-04-28 2006-12-01 Actelion Pharmaceuticals Ltd Pyrimidine derivatives
EP1920048A4 (en) * 2005-07-29 2009-12-09 Childrens Hosp Medical Center Gtpase inhibitors and methods of use and crystal structure of rac-1 gtpase
JP4976394B2 (en) * 2005-08-17 2012-07-18 シェーリング コーポレイション A novel high affinity quinoline-based kinase ligand
AR057836A1 (en) 2005-10-21 2007-12-19 Actelion Pharmaceuticals Ltd PIPERIZINAS AS AGENTS AGAINST MALARIA
US7615556B2 (en) * 2006-01-27 2009-11-10 Bristol-Myers Squibb Company Piperazinyl derivatives as modulators of chemokine receptor activity
TWI391378B (en) 2006-03-16 2013-04-01 Astellas Pharma Inc Quinolone derivative or pharmaceutically acceptable salt thereof
EP1999117A2 (en) * 2006-03-29 2008-12-10 Takeda Pharmaceutical Company Limited Renin inhibitors
US20070254861A1 (en) * 2006-04-28 2007-11-01 Astellas Pharma Inc. Methods for the prevention and/or treatment of peripheral arterial disease
CL2007002920A1 (en) 2006-10-13 2008-06-06 Actelion Pharmaceuticals Ltd COMPOUNDS DERIVED FROM 2-AMINOCARBONYLPIRIDINE; PHARMACEUTICAL COMPOSITION; AND USE FOR THE TREATMENT OF OCLUSIVE VASCULAR DISORDERS.
CL2007003038A1 (en) * 2006-10-25 2008-06-06 Actelion Pharmaceuticals Ltd COMPOUNDS DERIVED FROM 2-PHENYL-6-AMINOCARBONIL-PYRIMIDINE; PHARMACEUTICAL COMPOSITION; AND USE IN THE TREATMENT OF OCLUSIVE VASCULAR DISORDERS.
EP1967513A1 (en) * 2007-03-08 2008-09-10 Rheinische Friedrich-Wilhelms-Universität Bonn Novel P2Y12 receptor antagonists
WO2008128647A1 (en) * 2007-04-23 2008-10-30 Sanofi-Aventis Quinoline-carboxamide derivatives as p2y12 antagonists
WO2008155022A1 (en) 2007-06-18 2008-12-24 Sanofi-Aventis Pyrrole derivatives as p2y12 antagonists
RU2483072C2 (en) * 2007-11-29 2013-05-27 Актелион Фармасьютиклз Лтд Phosphonic acid derivatives and use thereof as p2y12 receptor antagonists
EP2238128B1 (en) 2007-12-26 2012-08-22 Sanofi Heterocyclic pyrazole-carboxamides as p2y12 antagonists
AR071652A1 (en) * 2008-04-11 2010-07-07 Actelion Pharmaceuticals Ltd DERIVATIVES 2- SUBSTITUTED PHENYL-PYRIDINE
AR071653A1 (en) * 2008-04-11 2010-07-07 Actelion Pharmaceuticals Ltd DERIVATIVES 2-FENIL-4-CICLOPROPIL-PYRIMIDINE
US20130303477A1 (en) 2008-05-13 2013-11-14 The Medicines Company Maintenance of Platelet Inhibition During Antiplatelet Therapy
WO2009140092A1 (en) 2008-05-13 2009-11-19 The Medicines Company Maintenance of platelet inhibition during antiplatelet therapy
US8759316B2 (en) 2008-05-13 2014-06-24 The Medicines Company Maintenance of platelet inhibition during antiplatelet therapy
US20120141468A1 (en) 2008-05-13 2012-06-07 Lisa Ruderman Chen Maintenance of platelet inhibition during antiplatelet therapy
US9427448B2 (en) 2009-11-11 2016-08-30 The Medicines Company Methods of treating, reducing the incidence of, and/or preventing ischemic events
WO2010075356A1 (en) * 2008-12-23 2010-07-01 Forest Laboratories Holdings Limited Novel piperazine derivatives as inhibitors of stearoyl-coa desaturase
BRPI1014039A2 (en) 2009-04-08 2018-04-03 Actelion Pharmaceuticals Ltd 6- (3-aza-bicyclo [3.1.0] hex-3-yl) -2-phenyl-pyrimidines
NZ596388A (en) 2009-04-22 2013-05-31 Actelion Pharmaceuticals Ltd Thiazole derivatives and their use as p2y12 receptor antagonists
US8729095B2 (en) 2009-08-28 2014-05-20 Daiichi Sankyo Company, Limited 3-(biaryloxy)propionic acid derivatives for prevention and/or treatment of thromboembolic diseases
CA2778880C (en) 2009-11-11 2018-02-13 The Medicines Company Methods of treating or preventing stent thrombosis
US10376532B2 (en) 2009-11-11 2019-08-13 Chiesi Farmaceutici, S.P.A. Methods of treating, reducing the incidence of, and/or preventing ischemic events
JP2013512246A (en) 2009-11-25 2013-04-11 メルク・シャープ・アンド・ドーム・コーポレーション Condensed tricyclic compounds and derivatives useful for the treatment of viral diseases
US20130156731A1 (en) 2009-12-22 2013-06-20 Kevin X. Chen Fused tricyclic compounds and methods of use thereof for the treatment of viral diseas
US8889688B2 (en) 2010-01-05 2014-11-18 Actelion Pharmaceuticals Ltd. Piperazines as antimalarial agents
JP2013522202A (en) 2010-03-09 2013-06-13 メルク・シャープ・エンド・ドーム・コーポレイション Fused tricyclic silyl compounds and methods of use thereof for the treatment of viral diseases
WO2013039876A1 (en) 2011-09-14 2013-03-21 Merck Sharp & Dohme Corp. Silyl-containing heterocyclic compounds and methods of use thereof for the treatment of viral diseases
GB201218084D0 (en) * 2012-10-09 2012-11-21 Univ Aston Novel compounds and methods for use in medicine
CN105189485B (en) 2013-03-15 2017-10-24 埃科特莱茵药品有限公司 It is used as the novel propylene amide derivatives of anti-malarial agents
EP3515924B1 (en) 2016-09-22 2021-12-15 Idorsia Pharmaceuticals Ltd Crystalline forms
CN110381947A (en) 2017-03-15 2019-10-25 爱杜西亚药品有限公司 P2Y12The subcutaneous administration of receptor antagonist
MA49452A (en) 2017-06-23 2021-05-05 Chiesi Farm Spa METHOD FOR PREVENTING SHUNT THROMBOSIS OF THE SYSTEMIC-PULMONARY ARTERY
EP4031542A4 (en) * 2019-09-18 2023-10-25 Merck Sharp & Dohme LLC Small molecule inhibitors of kras g12c mutant
MX2022005053A (en) 2019-10-28 2022-05-18 Merck Sharp & Dohme Llc Small molecule inhibitors of kras g12c mutant.
US11945790B2 (en) * 2020-12-22 2024-04-02 Immunomolecular Therapeutics, Inc. Compounds and methods for treating autoimmune disorders by targeting HLA-DQ2

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992008709A1 (en) * 1990-11-15 1992-05-29 Pentapharm Ag Meta-substituted phenyl alanine derivatives
EP0739886A2 (en) * 1995-04-28 1996-10-30 LG Chemical Limited Selective thrombin inhibitors
WO1998056771A2 (en) * 1997-06-12 1998-12-17 Schering Aktiengesellschaft Piperazine derivatives and their use as anti-inflammatory agents

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1334705A (en) 1970-06-19 1973-10-24 Ici Ltd Pharmaceutical compositions containing kynurenic acid derivatives
US4258192A (en) 1977-12-16 1981-03-24 Mitsubishi Chemical Industries Limited N2 -Arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
US5346907A (en) 1988-04-05 1994-09-13 Abbott Laboratories Amino acid analog CCK antagonists
AU5878194A (en) 1993-02-10 1994-08-29 Pentapharm Ag Piperazides of substituted phenylalanine derivates as thrombin inhibitors
JP2003502314A (en) * 1999-06-14 2003-01-21 イーライ・リリー・アンド・カンパニー Compound

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992008709A1 (en) * 1990-11-15 1992-05-29 Pentapharm Ag Meta-substituted phenyl alanine derivatives
EP0739886A2 (en) * 1995-04-28 1996-10-30 LG Chemical Limited Selective thrombin inhibitors
WO1998056771A2 (en) * 1997-06-12 1998-12-17 Schering Aktiengesellschaft Piperazine derivatives and their use as anti-inflammatory agents

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DULLWEBER,F. ET AL.: "Factorising Ligand Affinity : A Combined Thermodynamic and Crysstallographic Study of Trypsin and Thrombin Inhibition", J.MOL.BIOL., vol. 313, 2001, pages 593 - 614, XP002226502 *
KAMM,W. ET AL.: "Transport of Peptidomimetic Thrombin Inhibitors with a 3-amidino-Phenylalanine Structure : Permeability and Efflux Mechanism in Monolayers of a Human Intestinal Cell Line (Caco-2)", PHARM.RES., vol. 18, no. 8, 2001, pages 1110 - 1118, XP009003114 *
PIERCE,A.C ET AL.: "Estimation of Binding Affinities for Selective Thrombin Inhibitors via Monte Carlo Simulations", J.MED.CHEM., vol. 44, no. 7, 2001, WASHINGTON, pages 1043 - 1050, XP002226501 *

Also Published As

Publication number Publication date
US7176207B2 (en) 2007-02-13
WO2002098856A2 (en) 2002-12-12
US7026323B2 (en) 2006-04-11
US6861424B2 (en) 2005-03-01
JP4409936B2 (en) 2010-02-03
US20050038037A1 (en) 2005-02-17
US20030060474A1 (en) 2003-03-27
AU2002316191A1 (en) 2002-12-16
US6995156B2 (en) 2006-02-07
US20060135532A1 (en) 2006-06-22
JP2004532886A (en) 2004-10-28
US20050065163A1 (en) 2005-03-24
EP1412349A2 (en) 2004-04-28

Similar Documents

Publication Publication Date Title
WO2002098856A3 (en) Piperazine oxyquinoline (naphthaline) platelet adenosine diphosphate receptor antagonists
WO2003086303A3 (en) Farnesoid x-activated receptor agonists
DE60204452D1 (en) [1,5] pyridine derivatives
SE9904652D0 (en) Novel Compounds
DK0911333T3 (en) Pyrazole [4,3-d] pyrimidine derivatives and pharmaceutical compositions containing them
DE60112609D1 (en) Pyrazolopyridine
NO20052496L (en) Selected CGRP antagonists, methods for their preparation and use thereof as drugs.
WO2001042219A3 (en) Novel substituted phenanthridinones and methods of use thereof
HK1155146A1 (en) Indene derivatives as pharmaceutical agents
BG103485A (en) Ketobanzamides as calpain inhibitors
EP1253142A4 (en) Compounds exhibiting thrombopoietin receptor agonism
NO20025821L (en) 2-aminocarbonyl-9H-purine
IL143545A0 (en) Thrombin inhibitors
WO2003095455A3 (en) Substituted pyrazolopyrimidines
CA2390649A1 (en) 5-aryl-1h-1,2,4-triazole compounds as inhibitors of cyclooxygenase-2 and pharmaceutical compositions containing them
TR200101155T2 (en) 4-Aroil Piperidine CCR-3 Receptor Antagonists III
WO2003002489A3 (en) Solid-phase electrophilic fluorination
WO2002048148A3 (en) Pyrazolopyridine derivatives
RS20050450A (en) 2-aminocarbonyl-quinoline compounds as platelet adenosine diphosphate receptor antagonists
WO2004082623A3 (en) Substituted piperidine compounds
WO2004112704A3 (en) Substituted piperidine compounds and methods of their use
WO2003053971A8 (en) Pyridoquinoxaline antivirals
MA26418A1 (en) PIPERIDONES, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
CA2412596A1 (en) Cyclic gmp-specific phosphodiesterase inhibitors
WO1999062893A3 (en) Novel neurokinin antagonists, method for the production thereof and pharmaceutical compositions containing said compounds

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SD SE SG SI SK SL TJ TM TN TR TT TZ UA UG US UZ VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
WWE Wipo information: entry into national phase

Ref document number: 2002746471

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 2003501845

Country of ref document: JP

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWP Wipo information: published in national office

Ref document number: 2002746471

Country of ref document: EP