BR0011260A - Composto, uso do mesmo, composição farmacêutica e métodos para inibir a trombina e a formação de agregados de plaqueta e de trombo no sangue e para tratar ou prevenir a trombose de veia profunda e o tromboembolismo cardiogênico, a trombose associada com o câncer e a quimioterapia do câncer e a angina instável em um mamìfero e o acidente vascular cerebral em seres humanos e outros mamìferos - Google Patents

Composto, uso do mesmo, composição farmacêutica e métodos para inibir a trombina e a formação de agregados de plaqueta e de trombo no sangue e para tratar ou prevenir a trombose de veia profunda e o tromboembolismo cardiogênico, a trombose associada com o câncer e a quimioterapia do câncer e a angina instável em um mamìfero e o acidente vascular cerebral em seres humanos e outros mamìferos

Info

Publication number
BR0011260A
BR0011260A BR0011260-7A BR0011260A BR0011260A BR 0011260 A BR0011260 A BR 0011260A BR 0011260 A BR0011260 A BR 0011260A BR 0011260 A BR0011260 A BR 0011260A
Authority
BR
Brazil
Prior art keywords
cancer
thrombosis
platelet
aggregates
treat
Prior art date
Application number
BR0011260-7A
Other languages
English (en)
Inventor
Christopher S Burgey
Kyle A Robinson
Peter D Williams
Craig A Coburn
Terry A Lyle
Philip E Sanderson
Original Assignee
Merck & Co Inc
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 Merck & Co Inc filed Critical Merck & Co Inc
Publication of BR0011260A publication Critical patent/BR0011260A/pt

Links

Classifications

    • 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
    • C07D241/18—Oxygen or sulfur 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/26—Radicals substituted by halogen atoms or nitro radicals
    • 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
    • C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • 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
    • C07D213/61—Halogen atoms or nitro radicals
    • 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms
    • C07D213/71—Sulfur atoms to which a second hetero atom is attached
    • 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
    • C07D241/16—Halogen atoms; Nitro radicals
    • 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
    • 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms 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
    • C07D401/14—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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

"COMPOSTO, USO DO MESMO, COMPOSIçãO FARMACêUTICA E MéTODOS PARA INIBIR A TROMBINA E A FORMAçãO DE AGREGADOS DE PLAQUETA E DE TROMBO NO SANGUE E PARA TRATAR OU PREVENIR A TROMBOSE DE VEIA PROFUNDA E O TROMBOEMBOLISMO CARDIOGêNICO, A TROMBOSE ASSOCIADA COM O CâNCER E A QUIMIOTERAPIA DO CâNCER E A ANGINA INSTáVEL EM UM MAMìFERO E O ACIDENTE VASCULAR CEREBRAL EM SERES HUMANOS E OUTROS MAMìFEROS". Os compostos da invenção são úteis na inibição da trombina e oclusões trombóticas associadas que tenham a estrutura (I) onde A é (II), (III) ou (IV) em que Y^ 1^ e Y^ 2^ são independentemente hidrogênio, alquila C~ 1-4~, alcóxi C~ 1-4~, F~ u~H~ v~(C(CH~ 2~)~ 0-1~ O-, em que u e v são 1 ou 2, contanto que quando u for 1, v seja 2 e quando u for 2, v seja 1, cicloalquila C~ 3-7~, alquiltio C~ 1-4~, sulfonilalquila C~ 1-4~, halogênio, ciano ou trifluorometila e em que b é 0 ou 1.
BR0011260-7A 1999-06-04 2000-06-01 Composto, uso do mesmo, composição farmacêutica e métodos para inibir a trombina e a formação de agregados de plaqueta e de trombo no sangue e para tratar ou prevenir a trombose de veia profunda e o tromboembolismo cardiogênico, a trombose associada com o câncer e a quimioterapia do câncer e a angina instável em um mamìfero e o acidente vascular cerebral em seres humanos e outros mamìferos BR0011260A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13753899P 1999-06-04 1999-06-04
US14429199P 1999-07-16 1999-07-16
PCT/US2000/015140 WO2000075134A1 (en) 1999-06-04 2000-06-01 Pyrazinone thrombin inhibitors

Publications (1)

Publication Number Publication Date
BR0011260A true BR0011260A (pt) 2002-03-19

Family

ID=26835338

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0011260-7A BR0011260A (pt) 1999-06-04 2000-06-01 Composto, uso do mesmo, composição farmacêutica e métodos para inibir a trombina e a formação de agregados de plaqueta e de trombo no sangue e para tratar ou prevenir a trombose de veia profunda e o tromboembolismo cardiogênico, a trombose associada com o câncer e a quimioterapia do câncer e a angina instável em um mamìfero e o acidente vascular cerebral em seres humanos e outros mamìferos

Country Status (31)

Country Link
US (1) US6455532B1 (pt)
EP (1) EP1189899B1 (pt)
JP (2) JP4495377B2 (pt)
KR (1) KR20020029653A (pt)
CN (1) CN1353705A (pt)
AT (1) ATE232527T1 (pt)
AU (1) AU761982B2 (pt)
BG (1) BG106263A (pt)
BR (1) BR0011260A (pt)
CA (1) CA2373999C (pt)
CZ (1) CZ20014343A3 (pt)
DE (1) DE60001414T2 (pt)
DK (1) DK1189899T3 (pt)
DZ (1) DZ3264A1 (pt)
EA (1) EA004372B1 (pt)
EE (1) EE200100641A (pt)
ES (1) ES2190417T3 (pt)
HK (1) HK1047277A1 (pt)
HR (1) HRP20010903A2 (pt)
HU (1) HUP0202366A3 (pt)
IL (1) IL146393A0 (pt)
IS (1) IS6158A (pt)
MX (1) MXPA01012505A (pt)
NO (1) NO20015887L (pt)
NZ (1) NZ515454A (pt)
PL (1) PL352558A1 (pt)
SK (1) SK17532001A3 (pt)
TR (1) TR200103491T2 (pt)
UA (1) UA58636C2 (pt)
WO (1) WO2000075134A1 (pt)
YU (1) YU84301A (pt)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001265094A1 (en) 2000-06-01 2001-12-11 Merck And Co., Inc. Pyrazinone thrombin inhibitors
FR2818277B1 (fr) * 2000-12-14 2003-01-24 Servier Lab Nouveaux derives bicycliques d'amino-pyrazinones, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US6528503B2 (en) 2000-12-18 2003-03-04 Merck & Co., Inc. Thrombin inhibitors
CA2431588A1 (en) 2000-12-18 2002-06-27 Merck & Co., Inc. Benzylamine derivatives and their use as thrombin inhibitors
CA2436176A1 (en) 2001-02-09 2002-08-22 Merck & Co., Inc. Thrombin inhibitors
WO2003048127A1 (en) 2001-12-04 2003-06-12 Corvas International, Inc. Aromatic heterocyclic non-covalent inhibitors of urokinase and blood vessel formation
FR2867780B1 (fr) * 2004-03-19 2006-05-19 Servier Lab Nouveaux derives de 4-oxo-4,6,7,8-tetrahydropyrrolo (1,2-a) pyrazine-6-carboxamides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
DE102004022897A1 (de) * 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
DE102008041214A1 (de) 2008-08-13 2010-02-18 Bayer Cropscience Ag N-substituierte Azinylakyl-azincarboxamide und deren Analoge
CA2778922A1 (en) * 2009-11-03 2011-05-12 Diakron Pharmaceuticals, Inc. Process for the preparation of pyrazinone thrombin inhibitor and its intermediates
KR20140090663A (ko) * 2011-11-07 2014-07-17 디아크론 파마슈티칼스, 인코포레이티드 직접 트롬빈 억제제의 연장 방출성 제형
CN115677511B (zh) * 2022-10-26 2024-06-21 南通华祥医药科技有限公司 一种2,2-二氟丙胺盐酸盐的合成方法

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2037738T3 (es) 1986-09-26 1993-07-01 Ciba-Geigy Ag Procedimiento para la obtencion de aminopirazinonas y aminotriazinonas.
TW201303B (pt) 1990-07-05 1993-03-01 Hoffmann La Roche
GB9207145D0 (en) 1991-04-18 1992-05-13 Ici Plc Heterocyclic amides
CA2067663A1 (en) 1991-05-01 1992-11-02 Hitoshi Tone Pyrazine derivatives
DE4127404A1 (de) 1991-08-19 1993-02-25 Thomae Gmbh Dr K Cyclische iminoderivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
TW223629B (pt) 1992-03-06 1994-05-11 Hoffmann La Roche
ES2184763T3 (es) 1993-04-30 2003-04-16 Merck & Co Inc Inhibidores de trombina.
US5672582A (en) 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
US5510369A (en) 1994-07-22 1996-04-23 Merck & Co., Inc. Pyrrolidine thrombin inhibitors
EP0820453A4 (en) 1995-04-04 2001-08-29 Merck & Co Inc THROMBIN INHIBITORS
US5629324A (en) 1995-04-10 1997-05-13 Merck & Co., Inc. Thrombin inhibitors
AU703744B2 (en) 1995-06-27 1999-04-01 Merck & Co., Inc. Pyridinone-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
US5981546A (en) 1996-08-29 1999-11-09 Merck & Co., Inc. Integrin antagonists
AU722429B2 (en) * 1997-01-22 2000-08-03 Merck & Co., Inc. Thrombin inhibitors
JP2001518932A (ja) * 1997-03-24 2001-10-16 メルク エンド カンパニー インコーポレーテッド トロンビン阻害薬
US5866573A (en) 1997-04-21 1999-02-02 Merck & Co., Inc. Pyrazinone thrombin inhibitors
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
AU753479B2 (en) * 1998-05-19 2002-10-17 Merck & Co., Inc. Pyrazinone thrombin inhibitors
CN1351595A (zh) 1999-05-19 2002-05-29 法玛西雅公司 可用于选择性抑制凝血级联的取代的多环芳基与杂芳基吡嗪酮

Also Published As

Publication number Publication date
WO2000075134A1 (en) 2000-12-14
DZ3264A1 (fr) 2000-12-14
NO20015887L (no) 2002-01-23
HUP0202366A2 (en) 2002-10-28
HK1047277A1 (zh) 2003-02-14
AU5457100A (en) 2000-12-28
CA2373999C (en) 2007-01-02
TR200103491T2 (tr) 2002-12-23
US6455532B1 (en) 2002-09-24
IL146393A0 (en) 2002-07-25
PL352558A1 (en) 2003-08-25
HUP0202366A3 (en) 2005-07-28
ES2190417T3 (es) 2003-08-01
EP1189899B1 (en) 2003-02-12
ATE232527T1 (de) 2003-02-15
CZ20014343A3 (cs) 2002-03-13
DE60001414T2 (de) 2003-11-06
JP2003501426A (ja) 2003-01-14
KR20020029653A (ko) 2002-04-19
AU761982B2 (en) 2003-06-12
EA004372B1 (ru) 2004-04-29
CN1353705A (zh) 2002-06-12
JP2010150275A (ja) 2010-07-08
CA2373999A1 (en) 2000-12-14
SK17532001A3 (sk) 2002-05-09
EE200100641A (et) 2003-02-17
UA58636C2 (uk) 2003-08-15
YU84301A (sh) 2004-07-15
NZ515454A (en) 2004-02-27
DE60001414D1 (en) 2003-03-20
BG106263A (en) 2002-06-28
NO20015887D0 (no) 2001-12-03
IS6158A (is) 2001-11-13
JP4495377B2 (ja) 2010-07-07
EA200200005A1 (ru) 2002-06-27
EP1189899A1 (en) 2002-03-27
HRP20010903A2 (en) 2003-04-30
MXPA01012505A (es) 2002-07-02
DK1189899T3 (da) 2003-03-10

Similar Documents

Publication Publication Date Title
BR0011260A (pt) Composto, uso do mesmo, composição farmacêutica e métodos para inibir a trombina e a formação de agregados de plaqueta e de trombo no sangue e para tratar ou prevenir a trombose de veia profunda e o tromboembolismo cardiogênico, a trombose associada com o câncer e a quimioterapia do câncer e a angina instável em um mamìfero e o acidente vascular cerebral em seres humanos e outros mamìferos
BR0313743A (pt) Benzimidazol quinolinonas e usos destas
BR9912109A (pt) Compostos, composições farmacêuticas, processo para a manufatura de um composto, e, método de tratar um mamìfero sofrendo de inflamação patológica e autoimunidade
CO5090836A1 (es) 3s tetrahidro 3 furanil 1s, 2r 3 / 4 aminofenil sulfonil (isobutil) [amino]1 bencil 2/(fosfonooxi)propilcarbamato de calcio
ATE400274T1 (de) Hemmstoffe der akt aktivität
CO4910133A1 (es) Antagonistas de 5-h[1f]
BR9806752A (pt) Ftalazinonas.
EA200000759A1 (ru) Производные 2-(пурин-9-ил)-тетрагидрофуран-3,4-диола
AU1244001A (en) Pyridyl-containing spirocyclic compounds as inhibitors of fibrinogen-dependent platelet aggregation
TR199903331T2 (xx) Farnesil protein transferas engelleyicileri.
BR0012136A (pt) Inibidores de reabsorção de norepinefrina altamente seletivos e métodos de uso dos mesmos
TWI265931B (en) Composition and method for inhibiting platelet aggregation
BR9908811A (pt) Composto, composição farmacêutica e seu uso no tratamento de mamìferos
BR0016817A (pt) Combinações de um inibidor de quinase do receptor de tirosina com um composto orgânico capaz de se ligar à alfa1-glicoproteìna ácida
DE602004023838D1 (de) Hemmer der akt aktivität
ATE512957T1 (de) Hemmer der akt aktivität
TR200202806T2 (tr) 4-Triflorometilsulfinilpirazol türevi hazırlama süreci
EA200200306A1 (ru) Трициклические ингибиторы поли(адф-рибозо)полимераз
BR9814116A (pt) Uso de derivados de quinazolina como inibidores de cinase de tirosina para tratamento de pólipo colÈnico
DK1068870T3 (da) Antitumormidler
BR0012666A (pt) Imidazoimidazóis e triazóis como agentes anti-inflamatórios
RS51123B (sr) Aril fuzionisana azapoliciklična jedinjenja
ATE215074T1 (de) Piperazinone als inhibitoren von blutplattchenaggregation
BR0213731A (pt) Compostos de silìcio
BR0311491A (pt) Composto, composição farmacêutica, uso de um composto, e, método terapêutico para tratar câncer em um mamìfero

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 6A, 7A 8A ANUIDADES.

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 PUBLICADO NA RPI 1962 DE 12/08/2008.