EA200101214A1 - SUBSTITUTED POLYCYCLIC ARYL- AND HETEROYARYL-PYRIMIDINONES USED AS ANTICOAGULANTS - Google Patents

SUBSTITUTED POLYCYCLIC ARYL- AND HETEROYARYL-PYRIMIDINONES USED AS ANTICOAGULANTS

Info

Publication number
EA200101214A1
EA200101214A1 EA200101214A EA200101214A EA200101214A1 EA 200101214 A1 EA200101214 A1 EA 200101214A1 EA 200101214 A EA200101214 A EA 200101214A EA 200101214 A EA200101214 A EA 200101214A EA 200101214 A1 EA200101214 A1 EA 200101214A1
Authority
EA
Eurasian Patent Office
Prior art keywords
polycyclic aryl
substituted polycyclic
heteroyaryl
pyrimidinones
anticoagulants
Prior art date
Application number
EA200101214A
Other languages
Russian (ru)
Other versions
EA004867B1 (en
Inventor
Майкл С. Саут
Эштон Т. II Хамме
Уилльям Ньюманн
Дэрин Е. Джоунс
Мелвин Л. Руппел
Original Assignee
Фармация Корпорейшн
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 Фармация Корпорейшн filed Critical Фармация Корпорейшн
Publication of EA200101214A1 publication Critical patent/EA200101214A1/en
Publication of EA004867B1 publication Critical patent/EA004867B1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • A61P9/10—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members 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
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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

Настоящее изобретение относится к замещенным полициклическим арил- и гетероарилпиримидиноновым соединениям, полезным в качестве ингибиторов сериновых протеаз каскада кагулирования, а также к соединениям, композициям и к способам, используемым в антикоагулянтной терапии для лечения и предупреждения различных тромботических состояний, включая поражения коронарной артерии и цереброваскулярные заболевания.Международная заявка была опубликована вместе с отчетом о международном поиске.The present invention relates to substituted polycyclic aryl and heteroarylpyrimidinone compounds useful as inhibitors of the cascade of cagulation serine proteases, as well as compounds, compositions and methods used in anticoagulant therapy for the treatment and prevention of various thrombotic conditions, including coronary artery disease and cerebrovascular diseases The international application was published along with an international search report.

EA200101214A 1999-05-19 2000-05-17 Substituted pyrymidinone compounds, composition and method for the treatment, inhibiting and prevention of thrombotic conditions in mammals EA004867B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13479499P 1999-05-19 1999-05-19
PCT/US2000/009806 WO2000069832A1 (en) 1999-05-19 2000-05-17 Substituted polycyclic aryl and heteroaryl pyrymidinones useful as anticoagulants

Publications (2)

Publication Number Publication Date
EA200101214A1 true EA200101214A1 (en) 2002-06-27
EA004867B1 EA004867B1 (en) 2004-08-26

Family

ID=22465042

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200101214A EA004867B1 (en) 1999-05-19 2000-05-17 Substituted pyrymidinone compounds, composition and method for the treatment, inhibiting and prevention of thrombotic conditions in mammals

Country Status (22)

Country Link
EP (1) EP1178970A1 (en)
JP (1) JP2002544262A (en)
KR (1) KR20010114271A (en)
CN (1) CN1157380C (en)
AR (1) AR030021A1 (en)
AU (2) AU771718B2 (en)
BR (1) BR0010758A (en)
CA (1) CA2373614A1 (en)
CZ (1) CZ20014116A3 (en)
EA (1) EA004867B1 (en)
HU (1) HUP0201242A3 (en)
IL (1) IL146243A0 (en)
MX (1) MXPA01011804A (en)
NO (1) NO20015604L (en)
NZ (1) NZ514874A (en)
PE (1) PE20010229A1 (en)
PL (1) PL352827A1 (en)
SK (1) SK15852001A3 (en)
TW (1) TWI222445B (en)
UY (1) UY26156A1 (en)
WO (1) WO2000069832A1 (en)
ZA (2) ZA200109339B (en)

Families Citing this family (26)

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Publication number Priority date Publication date Assignee Title
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
AU771740B2 (en) * 1999-05-19 2004-04-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6660885B2 (en) 2000-03-13 2003-12-09 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
EP1268463B1 (en) 2000-04-05 2005-02-16 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
AU2001251315A1 (en) 2000-04-05 2001-10-23 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
US20040171616A9 (en) 2000-04-17 2004-09-02 South Michael S. Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
AU2001222501A1 (en) * 2000-05-18 2001-11-26 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
US7015223B1 (en) 2000-11-20 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
CA2430037A1 (en) 2000-11-20 2002-05-30 Michael S. South Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
US7119094B1 (en) 2000-11-20 2006-10-10 Warner-Lambert Company Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
EP1438292A1 (en) 2001-10-03 2004-07-21 Pharmacia Corporation 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade
BR0213126A (en) * 2001-10-03 2004-08-24 Pharmacia Corp 6-membered unsaturated heterocyclic compounds useful for selective inhibition of coagulation cascade
CA2462645A1 (en) 2001-10-03 2003-11-13 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
BR0307584A (en) 2002-02-22 2005-02-01 Upjohn Co Pyrimidinones and substituted pyrimidinines
TW200307667A (en) 2002-05-06 2003-12-16 Bristol Myers Squibb Co Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
WO2004089297A2 (en) 2003-04-02 2004-10-21 Suntory Pharmaceutical Research Laboratories, Llc Compounds and methods for treatment of thrombosis
US7182738B2 (en) 2003-04-23 2007-02-27 Marctec, Llc Patient monitoring apparatus and method for orthosis and other devices
WO2006133242A2 (en) * 2005-06-07 2006-12-14 Pharmacopeia, Inc. Azinone and diazinone v3 inhibitors for depression and stress disorders
CN104311537B (en) * 2014-09-19 2016-08-24 广东东阳光药业有限公司 Containing pyrimidone acetyl substituents pyrazole compound and combinations thereof thing and purposes

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5441960A (en) * 1992-04-16 1995-08-15 Zeneca Limited 1-pyrimidinylacetamide human leukocyte elastate inhibitors
CN1131210C (en) * 1995-04-27 2003-12-17 三菱制药株式会社 Heterocyclic amide compounds and medicinal use of the same

Also Published As

Publication number Publication date
TWI222445B (en) 2004-10-21
KR20010114271A (en) 2001-12-31
AU771718B2 (en) 2004-04-01
NO20015604L (en) 2002-01-11
CZ20014116A3 (en) 2002-06-12
BR0010758A (en) 2003-06-10
UY26156A1 (en) 2000-12-29
EA004867B1 (en) 2004-08-26
AR030021A1 (en) 2003-08-13
WO2000069832A1 (en) 2000-11-23
HUP0201242A2 (en) 2002-12-28
EP1178970A1 (en) 2002-02-13
MXPA01011804A (en) 2003-09-04
AU4973400A (en) 2000-12-05
JP2002544262A (en) 2002-12-24
NO20015604D0 (en) 2001-11-16
SK15852001A3 (en) 2003-06-03
PL352827A1 (en) 2003-09-08
CN1157380C (en) 2004-07-14
HUP0201242A3 (en) 2003-02-28
IL146243A0 (en) 2002-07-25
CA2373614A1 (en) 2000-11-23
PE20010229A1 (en) 2001-03-07
AU2004202375A1 (en) 2004-06-24
CN1351593A (en) 2002-05-29
ZA200109339B (en) 2004-05-26
NZ514874A (en) 2004-11-26
ZA200400448B (en) 2004-09-29

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Legal Events

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU