BR0213092A - Compostos heterocìclicos de 6 elementos úteis para a inibição seletiva da cascata de coagulação - Google Patents

Compostos heterocìclicos de 6 elementos úteis para a inibição seletiva da cascata de coagulação

Info

Publication number
BR0213092A
BR0213092A BR0213092-0A BR0213092A BR0213092A BR 0213092 A BR0213092 A BR 0213092A BR 0213092 A BR0213092 A BR 0213092A BR 0213092 A BR0213092 A BR 0213092A
Authority
BR
Brazil
Prior art keywords
selective inhibition
heterocyclic compounds
coagulation cascade
compounds useful
element heterocyclic
Prior art date
Application number
BR0213092-0A
Other languages
English (en)
Inventor
Michael S South
Ronald K Webber
Horng-Chih Huang
Mihaly V Toth
Alan E Moormann
Jeffrey A Scholten
Danny J Garland
Melvin L Rueppel
William L Neumann
Scott Long
Huang Wei
John Trujillo
John J Parlow
Darin E Jones
Brenda Case
Michael J Hayes
Original Assignee
Pharmacia Corp
Jeffery S Snyder
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 Pharmacia Corp, Jeffery S Snyder filed Critical Pharmacia Corp
Publication of BR0213092A publication Critical patent/BR0213092A/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/56Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/98Nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C07D231/38Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or 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
    • C07D231/44Oxygen and nitrogen or sulfur and nitrogen atoms
    • C07D231/46Oxygen atom in position 3 or 5 and nitrogen atom in position 4
    • C07D231/48Oxygen atom in position 3 or 5 and nitrogen atom in position 4 with hydrocarbon radicals attached to said nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/04Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having less than three double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/06Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/10Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/20Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings 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
    • C07D241/20Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/14Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D253/00Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02Heterocyclic 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
    • C07D253/061,2,4-Triazines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D253/00Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02Heterocyclic 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
    • C07D253/061,2,4-Triazines
    • C07D253/0651,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/071,2,4-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
    • C07D253/075Two hetero atoms, in positions 3 and 5
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or 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
    • C07D263/48Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/021,2-Oxazines; Hydrogenated 1,2-oxazines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or 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
    • C07D277/38Nitrogen atoms
    • C07D277/42Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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
    • C07D307/22Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/30Hetero atoms other than halogen
    • C07D333/36Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/04Systems containing only non-condensed rings with a four-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/06Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/10Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated

Abstract

"COMPOSTOS HETEROCìCLICOS DE 6 ELEMENTOS úTEIS PARA A INIBIçãO SELETIVA DA CASCATA DE COAGULAçãO". A presente invenção refere-se a compostos e pró-drogas dos mesmos, a composições e métodos úteis para a prevenção e tratamento de condições trombóticas em mamíferos. Os compostos da presente invenção e pró-drogas dos mesmos inibem seletivamente determinadas proteases da cascata de coagulação.
BR0213092-0A 2001-10-03 2002-10-03 Compostos heterocìclicos de 6 elementos úteis para a inibição seletiva da cascata de coagulação BR0213092A (pt)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US32672101P 2001-10-03 2001-10-03
US33862301P 2001-10-24 2001-10-24
US33285701P 2001-11-06 2001-11-06
US35005201P 2001-11-07 2001-11-07
US33210701P 2001-11-21 2001-11-21
US33189101P 2001-11-21 2001-11-21
PCT/US2002/031769 WO2003029216A1 (en) 2001-10-03 2002-10-03 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade

Publications (1)

Publication Number Publication Date
BR0213092A true BR0213092A (pt) 2004-10-19

Family

ID=27559729

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0213092-0A BR0213092A (pt) 2001-10-03 2002-10-03 Compostos heterocìclicos de 6 elementos úteis para a inibição seletiva da cascata de coagulação

Country Status (7)

Country Link
US (2) US6969715B2 (pt)
EP (1) EP1438292A1 (pt)
JP (1) JP2005519866A (pt)
BR (1) BR0213092A (pt)
CA (1) CA2462305A1 (pt)
MX (1) MXPA04003163A (pt)
WO (1) WO2003029216A1 (pt)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GEP201706656B (en) 2011-11-11 2017-04-25 Pfizer 2-thiopyrimidinones
US9522892B2 (en) 2011-11-29 2016-12-20 Perosphere Inc. Anticoagulant reversal agents
JP2018515480A (ja) 2015-05-05 2018-06-14 ファイザー・インク 2−チオピリミジノン
CN110117257B (zh) * 2018-02-05 2022-12-06 安徽省新星药物开发有限责任公司 一种含胍基的p2y12受体拮抗剂、制备方法及其用途

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5910541A (ja) * 1982-07-09 1984-01-20 Takeda Chem Ind Ltd キノン化合物
JPS60255749A (ja) * 1984-05-31 1985-12-17 Univ Nagoya キノン誘導体
US5304658A (en) * 1984-08-01 1994-04-19 Takeda Chemical Industries, Ltd. Quinone derivatives, their production and use
IL81264A (en) * 1986-01-30 1990-11-05 Takeda Chemical Industries Ltd Quinone derivatives,their production and pharmaceutical compositions containing them
DE3826846A1 (de) 1988-08-06 1990-02-08 Goedecke Ag Alkoxy-4(1h)-pyridon-derivate, verfahren zu deren herstellung und deren verwendung als arzneimittel
GB9216272D0 (en) 1991-08-15 1992-09-09 Ici Plc Substituted heterocycles
DE69314169T2 (de) 1992-04-16 1998-01-15 Zeneca Ltd Peptide mit eine alphaaminoboronaire gruppe and ihre verwendung als elastasehemmer
US5441960A (en) * 1992-04-16 1995-08-15 Zeneca Limited 1-pyrimidinylacetamide human leukocyte elastate inhibitors
US5618792A (en) * 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
US5656645A (en) 1994-12-13 1997-08-12 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
US5658930A (en) * 1994-12-13 1997-08-19 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
AU693636B2 (en) * 1994-12-13 1998-07-02 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
US6011158A (en) 1994-12-13 2000-01-04 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
KR100400639B1 (ko) 1995-04-27 2003-12-31 미쯔비시 웰 파마 가부시키가이샤 복소환식아미드화합물및그의의약용도
US5612378A (en) 1995-06-06 1997-03-18 3-Dimensional Pharmaceuticals, Inc. Bis-arylsulfonylaminobenzamide derivatives and the use thereof as factor Xa inhibitors
US5741819A (en) * 1995-06-07 1998-04-21 3-Dimensional Pharmaceuticals, Inc. Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors
EP0835109A4 (en) 1995-06-27 1999-02-03 Merck & Co Inc PYRIDINONE-BASED THROMBIN INHIBITORS
EP0923372A4 (en) 1996-02-22 2001-09-05 Merck & Co Inc PYRIDINONE THROMBINE INHIBITORS
WO1999011267A1 (en) 1997-09-05 1999-03-11 Merck & Co., Inc. Pyrazinone thrombin inhibitors
WO1997040024A1 (en) 1996-04-23 1997-10-30 Merck & Co., Inc. Pyrazinone thrombin inhibitors
US5668289A (en) * 1996-06-24 1997-09-16 Merck & Co., Inc. Pyridinone thrombin inhibitors
CA2263999A1 (en) 1996-08-29 1998-03-05 Merck & Co., Inc. Integrin antagonists
MXPA99002203A (es) 1996-09-06 2003-09-15 Nippon Kayaku Kk Nuevos derivados de acetamida e inhibidores de proteasa.
AU4172397A (en) 1996-09-06 1998-03-26 Biochem Pharma Inc. Lactam inhibitors of thrombin
US5872138A (en) * 1996-09-13 1999-02-16 Merck & Co., Inc. Thrombin inhibitors
AU725403B2 (en) 1996-09-13 2000-10-12 Merck & Co., Inc. Thrombin inhibitors
CA2268381A1 (en) 1996-10-11 1998-04-23 Cor Therapeutics, Inc. Selective factor xa inhibitors
EP0932608A1 (en) 1996-10-11 1999-08-04 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
WO1998017274A1 (en) 1996-10-24 1998-04-30 Merck & Co., Inc. Thrombin inhibitors
US5869487A (en) * 1996-10-24 1999-02-09 Merck & Co., Inc. Pyrido 3,4-B!pyrazines for use as thrombin inhibitors
US6080738A (en) 1996-10-25 2000-06-27 Yoshitomi Pharmaceuticals Industries, Ltd. Heterocyclic amide compounds and medicinal uses thereof
AU722429B2 (en) 1997-01-22 2000-08-03 Merck & Co., Inc. Thrombin inhibitors
US5792779A (en) * 1997-02-19 1998-08-11 Merck & Co., Inc. Pyridinone thrombin inhibitors
CA2283704A1 (en) 1997-03-24 1998-10-01 Merck & Co., Inc. Thrombin inhibitors
US5866573A (en) * 1997-04-21 1999-02-02 Merck & Co., Inc. Pyrazinone thrombin inhibitors
IL123986A (en) 1997-04-24 2011-10-31 Organon Nv Medicinal compounds
CN1254345A (zh) 1997-05-02 2000-05-24 阿克佐诺贝尔公司 丝氨酸蛋白酶抑制剂
ES2241151T3 (es) 1997-06-26 2005-10-16 Eli Lilly And Company Agentes antitromboticos.
WO1999000126A1 (en) 1997-06-26 1999-01-07 Eli Lilly And Company Antithrombotic agents
IL133621A0 (en) 1997-06-26 2001-04-30 Lilly Co Eli Antithrombotic agents
US6037356A (en) 1997-11-26 2000-03-14 3-Dimensional Pharmaceuticals, Inc. Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
AU1605699A (en) 1997-11-26 1999-06-15 Corvas International, Inc. Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (ii)
JP2002509153A (ja) 1998-01-20 2002-03-26 ワーナー−ランバート・カンパニー インターロイキン−1β変換酵素(ICE)のインビボ阻害剤としてのN−[2−(5−ベンジルオキシカルボニル−アミノ−6−オキソ−2−(4−フルオロフェニル)−1,6−ジヒドロ−1−ピリミジニル)アセトキシル]−L−アスパラギン酸アルデヒド
AU2881199A (en) 1998-02-26 1999-09-15 Neurogen Corporation Substituted 1,4-dihydro-4-oxonicotinic carboxamides: gaba brain receptor ligands
GB9806102D0 (en) 1998-03-20 1998-05-20 Merck Sharp & Dohme Therapeutic agents
JP2002515434A (ja) 1998-05-19 2002-05-28 メルク エンド カムパニー インコーポレーテッド ピラジノン系トロンビン阻害薬
CA2333040A1 (en) 1998-05-26 1999-12-02 Merck & Co., Inc. Imidazopyridine thrombin inhibitors
JP2003520185A (ja) 1998-06-03 2003-07-02 コーテック インコーポレーテッド セリンプロテアーゼ阻害剤としてのα−ケトオキサジアゾール類
AU759427B2 (en) 1998-06-11 2003-04-17 3-Dimensional Pharmaceuticals, Inc. Pyrazinone protease inhibitors
DK0997474T3 (da) * 1998-08-14 2004-02-09 Pfizer Antithrombotiske midler
CA2343109A1 (en) 1998-09-28 2000-04-06 Merck & Co., Inc. Thrombin inhibitors
CA2348530A1 (en) 1998-10-30 2000-05-11 Merck & Co., Inc. Thrombin inhibitors
CA2348734A1 (en) 1998-10-30 2000-05-11 Merck & Co., Inc. Thrombin inhibitors
DE19851421A1 (de) 1998-11-07 2000-05-11 Boehringer Ingelheim Pharma Neue Pyrimidine, deren Herstellung und Verwendung
FR2786482B1 (fr) 1998-11-27 2002-08-09 Synthelabo Nouveaux derives de 2-pyridone, leur preparation et leur application en therapeutique
WO2000038683A1 (en) 1998-12-23 2000-07-06 Du Pont Pharmaceuticals Company THROMBIN OR FACTOR Xa INHIBITORS
KR20010113970A (ko) 1999-05-19 2001-12-28 추후보정 응고 캐스케이드의 선택적 억제에 유용한 치환 폴리시클릭아릴 및 헤테로아릴 피리돈
JP2002544263A (ja) 1999-05-19 2002-12-24 ファルマシア・コーポレイション 抗凝血剤としての置換多環式アリールおよびヘテロアリールウラシル
MXPA01011804A (es) 1999-05-19 2003-09-04 Pharmacia Corp Aril y heteroaril pirimidinonas policiclicas sustituidas utiles como anticoagulantes.
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
WO2001068605A1 (en) 2000-03-13 2001-09-20 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
ATE289299T1 (de) 2000-04-05 2005-03-15 Pharmacia Corp Polyzyclisch aryl und heteroaryl substituierte 4- pyronen verwendbar als selektive hemmung von dem koagulationsprozess
EP1268428A2 (en) 2000-04-05 2003-01-02 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
WO2001087842A1 (en) 2000-05-18 2001-11-22 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
EP1351686A2 (en) 2000-11-20 2003-10-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade

Also Published As

Publication number Publication date
MXPA04003163A (es) 2004-07-08
US20030139405A1 (en) 2003-07-24
US20050267123A1 (en) 2005-12-01
JP2005519866A (ja) 2005-07-07
WO2003029216A1 (en) 2003-04-10
US6969715B2 (en) 2005-11-29
CA2462305A1 (en) 2003-04-10
EP1438292A1 (en) 2004-07-21

Similar Documents

Publication Publication Date Title
WO2002042272A8 (en) Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
WO2003028729A3 (en) Prodrugs of substituted polycyclic compounds useful for selective inhibition of the coagulation cascade
RS43604A (en) Inhibitors of factor xa and other serine proteases involved in the coagulation cascade
BR9712544A (pt) Inibidores de proteases de serina, particularmente protease ns3 do vìrus hapatite c
BRPI0407993B8 (pt) compostos inibidores de p38 e composições farmacêuticas compreendendo os mesmos
WO2002088101A3 (en) Inhibitors of bace
BR9809819A (pt) Compostos e métodos para a inibição da expressão de vcam-1
HUP0103160A2 (hu) Pulmonalis betegségek kezelésére alkalmas PDE4 inhibítort tartalmazó gyógyászati készítmények
CY1110527T1 (el) Διαρυλ ενωσεις ως αναστολεις πρωτεασης σερινης
DE60238086D1 (de) Platelet adp rezeptor inhibitoren
BRPI0519424A2 (pt) composiÇÕes e mÉtodos para tratamento de distérbios de proliferaÇço celular
BR0104424A (pt) Composições de pirazol úteis como inibidores de erk
NO20003018L (no) Triazinangiogenese-inhibitorer
TR200002940T2 (tr) Parazitlerin sebep olduğu hastalıkların papain süperfamilyasından sistein proteazların inhibisyonu yoluyla tedavisi
BR9815786A (pt) Quinolonas como inibidores de protease de serina
DK1456380T3 (da) SMAD7-inhibitorer til behandling af CNS-sygdomme
BR0213126A (pt) Compostos heterocìclicos insaturados de 6 membros úteis para inibição seletiva da cascata de coagulação
WO2008036379A3 (en) Serine hydrolase inhibitors
EA200201175A1 (ru) Применение ингибиторов il-18 для лечения и/или предотвращения атеросклероза
BR0316723A (pt) Derivados de anilinopirazol úteis para o tratamento de diabetes
UY26155A1 (es) Aril y heteroaril pirazinonas policiclicas sustituidas útiles para la inhibición selectiva de la cascada de coagulación.
BR0213099A (pt) Compostos policìclicos de 5 membros substituìdos úteis para inibição seletiva da cascata de coagulação
ATE516027T1 (de) Orazamid orotat zur vorbeugung von leberschäden
IS5966A (is) Nýjar amídínóafleiður og notkun þeirra sem þrombínhemlar
BR0316163A (pt) Inibidores de histona desacetilase para tratamento de doenças degenerativas do olho

Legal Events

Date Code Title Description
B08F Application fees: application dismissed [chapter 8.6 patent gazette]

Free format text: REFERENTE A 5O, 6O E 7O ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 DA RPI 2029 DE 24/11/2009.