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)
Portuguese (pt)
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

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00—Compounds 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
    • C07C257/10—Compounds 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
    • C07C257/18—Compounds 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/30—Heterocyclic 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
    • C07D207/32—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/98—Nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/14—Heterocyclic 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
    • C07D231/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/14—Heterocyclic 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
    • C07D231/44—Oxygen and nitrogen or sulfur and nitrogen atoms
    • C07D231/46—Oxygen atom in position 3 or 5 and nitrogen atom in position 4
    • C07D231/48—Oxygen atom in position 3 or 5 and nitrogen atom in position 4 with hydrocarbon radicals attached to said nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/04—Heterocyclic 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
    • 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
    • C07D239/06—Heterocyclic 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
    • C07D239/08—Heterocyclic 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
    • C07D239/10—Oxygen or sulfur atoms
    • 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
    • C07D239/20—Heterocyclic 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
    • C07D239/22—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-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
    • C07D249/14—Nitrogen atoms
    • 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
    • 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
    • C07D253/075—Two hetero atoms, in positions 3 and 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic 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
    • C07D263/34—Heterocyclic 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
    • C07D263/48—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/02—1,2-Oxazines; Hydrogenated 1,2-oxazines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic 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
    • C07D277/32—Heterocyclic 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
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic 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
    • C07D307/18—Heterocyclic 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
    • C07D307/22—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic 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
    • C07D333/26—Heterocyclic 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
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/36—Nitrogen 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
    • C07D401/12—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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/10—Heterocyclic 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
    • 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
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/04—Systems containing only non-condensed rings with a four-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/10—Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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
US33189101P 2001-11-21 2001-11-21
US33210701P 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

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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 (https=)
EP (1) EP1438292A1 (https=)
JP (1) JP2005519866A (https=)
BR (1) BR0213092A (https=)
CA (1) CA2462305A1 (https=)
MX (1) MXPA04003163A (https=)
WO (1) WO2003029216A1 (https=)

Families Citing this family (4)

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MD20140044A2 (ro) 2011-11-11 2014-08-31 Pfizer Inc. 2-Tiopirimidinone şi utilizarea lor pentru tratamentul afecţiunilor cardiovasculare
DK2785700T3 (en) 2011-11-29 2016-06-13 Perosphere Inc Agent for preventing the action of anti-coagulants.
AU2016257179A1 (en) 2015-05-05 2017-11-02 Pfizer Inc. 2-thiopyrimidinones
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)

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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
US5441960A (en) 1992-04-16 1995-08-15 Zeneca Limited 1-pyrimidinylacetamide human leukocyte elastate inhibitors
DE69314169T2 (de) 1992-04-16 1998-01-15 Zeneca Ltd Peptide mit eine alphaaminoboronaire gruppe and ihre verwendung als elastasehemmer
US5618792A (en) 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
US6011158A (en) 1994-12-13 2000-01-04 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
US5656645A (en) 1994-12-13 1997-08-12 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
EP0804464B1 (en) 1994-12-13 2002-05-08 Corvas International, Inc. Aromatic heterocyclic derivatives as enzyme inhibitors
US5948785A (en) 1995-04-27 1999-09-07 The Green Cross Corporation Heterocyclic amide compounds and pharmaceutical use of the same
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
JPH11508558A (ja) 1995-06-27 1999-07-27 メルク エンド カンパニー インコーポレーテッド ピリジノン トロンビン阻害剤
CA2245811A1 (en) 1996-02-22 1997-08-28 Merck & Co., Inc. Pyridinone thrombin inhibitors
JP3140790B2 (ja) 1996-04-23 2001-03-05 メルク エンド カンパニー インコーポレーテッド ピラジノン系トロンビン阻害薬
US5668289A (en) 1996-06-24 1997-09-16 Merck & Co., Inc. Pyridinone thrombin inhibitors
WO1998008840A1 (en) 1996-08-29 1998-03-05 Merck & Co., Inc. Integrin antagonists
AU4172397A (en) 1996-09-06 1998-03-26 Biochem Pharma Inc. Lactam inhibitors of thrombin
BR9712000A (pt) 1996-09-06 1999-08-24 Nippon Kayaku Kk Derivados de acetamida sais dos mesmos composi-Æo farmac-utica inibidores de protease de quimase de desgranula-Æo de mastÄcitos ou de libera-Æo de histamina de mastÄcitos e de ativa-Æo de eosinÄfilo ou de libera-Æo de oxig-nio ativo de eosinÄfilo e processo para produzir os dervados de acetamida
CA2264037A1 (en) 1996-09-13 1998-03-19 Merck & Co., Inc. Thrombin inhibitors
US5872138A (en) 1996-09-13 1999-02-16 Merck & Co., Inc. Thrombin inhibitors
EP0932615A1 (en) 1996-10-11 1999-08-04 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
AU743544B2 (en) 1996-10-11 2002-01-31 Millennium Pharmaceuticals, Inc. Selective factor Xa inhibitors
DE69719775T2 (de) 1996-10-24 2004-02-05 Merck & Co., Inc. Thrombin inhibitoren
US5869487A (en) 1996-10-24 1999-02-09 Merck & Co., Inc. Pyrido 3,4-B!pyrazines for use as thrombin inhibitors
EP0940400A4 (en) 1996-10-25 2002-10-02 Mitsubishi Pharma Corp HETEROCYCLIC AMID COMPOUNDS AND THEIR MEDICAL APPLICATION
WO1998031670A1 (en) 1997-01-22 1998-07-23 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
ID22904A (id) 1997-05-02 1999-12-16 Akzo Nobel Nv Penghambat serin protease
EP1014962A4 (en) 1997-06-26 2007-06-27 Lilly Co Eli ANTITHROMBOTIC AGENTS
IL133627A0 (en) 1997-06-26 2001-04-30 Lilly Co Eli Antithrombotic agents
US6372759B1 (en) 1997-06-26 2002-04-16 Eli Lilly And Company Antithrombotic agents
JP2001514227A (ja) 1997-09-05 2001-09-11 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
TWI222441B (en) 1997-11-26 2004-10-21 Dimensional Pharm Inc Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
WO1999026920A1 (en) 1997-11-26 1999-06-03 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
WO1999059591A1 (en) 1998-05-19 1999-11-25 Merck & Co., Inc. Pyrazinone thrombin inhibitors
EP1082324A4 (en) 1998-05-26 2002-01-02 Merck & Co Inc IMIDAZOPYRIDINE COMPOUNDS AS THROMBINE INHIBITORS
AU4330899A (en) 1998-06-03 2000-06-19 Cortech, Inc. Peptoid and nonpeptoid containing alpha-keto oxadiazoles as serine protease inhibitors
JP4554077B2 (ja) 1998-06-11 2010-09-29 オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド ピラジノンプロテアーゼインヒビター
EP0997474B1 (en) 1998-08-14 2003-10-29 Pfizer Inc. Antithrombotic agents
EP1117660A4 (en) 1998-09-28 2002-01-09 Merck & Co Inc Thrombin Inhibitors
WO2000026210A1 (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
US6664255B1 (en) 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
KR20010113969A (ko) 1999-05-19 2001-12-28 추후보정 항응고제로서의 치환된 폴리시클릭 아릴 및 헤테로아릴우라실
EA004867B1 (ru) 1999-05-19 2004-08-26 Фармация Корпорейшн Замещенные пиримидиноновые соединения, композиция и способ лечения, ингибирования или предупреждения тромботических состояний у млекопитающих
CA2373509A1 (en) 1999-05-19 2000-11-23 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones 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
JP2004501077A (ja) 2000-04-17 2004-01-15 ファルマシア・コーポレーション 凝固カスケードの選択的阻害に有用な多環式アリールおよびヘテロアリール置換１，４−キノン
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

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

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