PE13399A1 - Inhibidores de pirazinona para trombina - Google Patents

Inhibidores de pirazinona para trombina

Info

Publication number
PE13399A1
PE13399A1 PE1997000308A PE00030897A PE13399A1 PE 13399 A1 PE13399 A1 PE 13399A1 PE 1997000308 A PE1997000308 A PE 1997000308A PE 00030897 A PE00030897 A PE 00030897A PE 13399 A1 PE13399 A1 PE 13399A1
Authority
PE
Peru
Prior art keywords
thrombin
pirazinone
inhibitors
compounds
useful
Prior art date
Application number
PE1997000308A
Other languages
English (en)
Inventor
Richard J Varsolona
Bruce D Dorsey
Philip E Sanderson
Terry A Lyle
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
Priority claimed from GBGB9609714.2A external-priority patent/GB9609714D0/en
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of PE13399A1 publication Critical patent/PE13399A1/es

Links

Classifications

    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (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)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I), EN DONDE: "W" ES H o FENILO O UN HETEROCICLO, ENTRE OTROS; R3 ES H o ALQUILO C1-C4, ENTRE OTROS; "X" ES H o HALOGENO; "A" ES UN RADICAL DE FORMULA (i), (ii) o (iii); UN COMPUESTO (I) PREFERIDO ES EL DIHIDROCLORURO DE 3-(2-FENILETILAMINO)-6-METIL-5-METILCARBOXAMIDOMETILPIRIDINIL)-PIRAZINONA QUE EXISTE COMO: UN MONOHIDRATO TIPO A EN FORMA CRISTALINA POLIMORFICA CON UN PATRON DE DIFRACCION DE RAYOS X CARACTERIZADO POR d-SEPARACIONES ESPECTRALES DE 13,06; 12,16; 7,4; 5,71; 4,92; 4,48; 4,4; 3,63; 3,07; 2,98; 2,86 Y 2,62 A; UN MONOHIDRATO TIPO B EN FORMA CRISTALINA POLIMORFICA CON UN PATRON DE DIFRACCION DE RAYOS X CARACTERIZADO POR d-SEPARACION ESPECTRALES DE 12,98; 11,91; 7,24; 5,98; 4,9; 4,46; 4,23; 3,99; 3,75; 3,61; 3,41; 2,94 Y 2,61 A. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION DEL MONOHIDRATO TIPO A, QUE COMPRENDE: DISOLVER LA FORMA BASICA EN UN SOLVENTE DE ACIDO ACETICO Y ANADIR HCl ACUOSO, EN DONDE EL CONTENIDO FINAL DE AGUA EN ACIDO ACETICO ES DE 1% A 5% DEL PESO DE HCl; Y DEL MONOHIDRATO TIPO B, QUE COMPRENDE: DISOLVER LA FORMA BASICA EN UN SOLVENTE DE ACIDO HIDROCLORICO. LOS COMPUESTOS DE FORMULA (I) ACTUAN COMO INHIBIDORES DE LA TROMBINA, SIENDO UTILES EN LA PREVENCION Y EL TRATAMIENTO DE LA TROMBOSIS, DEL TROMBOEMBOLISMO VENOSO Y EMBOLISMO PULMONAR, ENTRE OTROS
PE1997000308A 1996-04-23 1997-04-23 Inhibidores de pirazinona para trombina PE13399A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US1604196P 1996-04-23 1996-04-23
GBGB9609714.2A GB9609714D0 (en) 1996-05-09 1996-05-09 Pyridinone thrombin inhibitors
US4300997P 1997-04-14 1997-04-14

Publications (1)

Publication Number Publication Date
PE13399A1 true PE13399A1 (es) 1999-02-11

Family

ID=27268274

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1997000308A PE13399A1 (es) 1996-04-23 1997-04-23 Inhibidores de pirazinona para trombina

Country Status (21)

Country Link
EP (1) EP0900207B1 (es)
JP (1) JP3140790B2 (es)
KR (1) KR20000010650A (es)
AT (1) ATE209191T1 (es)
AU (1) AU714985B2 (es)
BG (1) BG102948A (es)
BR (1) BR9708859A (es)
CA (1) CA2252964A1 (es)
CZ (1) CZ340898A3 (es)
DE (1) DE69709727T2 (es)
EE (1) EE9800353A (es)
HR (1) HRP970211A2 (es)
IL (1) IL126404A0 (es)
IS (1) IS4853A (es)
NO (1) NO984928L (es)
NZ (1) NZ331993A (es)
PE (1) PE13399A1 (es)
PL (1) PL329441A1 (es)
SK (1) SK145398A3 (es)
TR (1) TR199802133T2 (es)
WO (1) WO1997040024A1 (es)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU746024B2 (en) * 1996-04-23 2002-04-11 Merck & Co., Inc. Pyrazinone thrombin inhibitors
US6159980A (en) * 1996-09-16 2000-12-12 Dupont Pharmaceuticals Company Pyrazinones and triazinones and their derivatives thereof
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
US6011038A (en) * 1997-09-05 2000-01-04 Merck & Co., Inc. Pyrazinone thrombin inhibitors
AU753479B2 (en) * 1998-05-19 2002-10-17 Merck & Co., Inc. Pyrazinone thrombin inhibitors
US6147078A (en) * 1998-05-19 2000-11-14 Merck & Co., Inc. Pyrazinone thrombin inhibitors
WO1999061442A1 (en) * 1998-05-26 1999-12-02 Merck & Co., Inc. Imidazopyridine thrombin inhibitors
US6204263B1 (en) 1998-06-11 2001-03-20 3-Dimensional Pharmaceuticals, Inc. Pyrazinone protease inhibitors
PT997474E (pt) 1998-08-14 2004-01-30 Pfizer Agentes antitromboticos
WO2000018762A1 (en) * 1998-09-28 2000-04-06 Merck & Co., Inc. Thrombin inhibitors
US6610692B1 (en) 1998-10-30 2003-08-26 Merck & Co., Inc. Thrombin inhibitors
AU752186B2 (en) 1998-10-30 2002-09-12 Merck & Co., Inc. Thrombin inhibitors
AU3127900A (en) 1998-12-23 2000-07-31 Du Pont Pharmaceuticals Company Thrombin or factor xa inhibitors
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
JP2002544264A (ja) * 1999-05-19 2002-12-24 ファルマシア・コーポレイション 凝固カスケードの選択的阻害に有用な置換多環式アリールおよびヘテロアリールピラジノン
US6664255B1 (en) * 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
EP1586565A1 (en) * 1999-05-19 2005-10-19 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6750342B1 (en) 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
UA58636C2 (uk) * 1999-06-04 2003-08-15 Мерк Енд Ко., Інк. Піразинонові інгібітори тромбіну, фармацевтична композиція, спосіб інгібування утворення тромбів у крові, спосіб лікування станів, пов'язаних із тромбоутворенням
WO2001005772A1 (en) * 1999-07-19 2001-01-25 Merck Frosst Canada & Co. Pyrazinones, compositions containing such compounds
EP1259506A1 (en) 1999-11-23 2002-11-27 Merck & Co., Inc. Pyrazinone thrombin inhibitors
AU2001243598A1 (en) 2000-03-13 2001-09-24 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
JP2003527426A (ja) 2000-03-23 2003-09-16 メルク エンド カムパニー インコーポレーテッド トロンビン阻害薬
US6875791B2 (en) 2000-04-05 2005-04-05 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
AU2001251315A1 (en) 2000-04-05 2001-10-23 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
US6506761B1 (en) 2000-04-14 2003-01-14 Corvas International, Inc. Substituted hydrazinyl heteroaromatic inhibitors of thrombin
US6506760B1 (en) 2000-04-14 2003-01-14 Corvas International, Inc. Substituted hydrazinyl heteroaromatic inhibitors of thrombin
WO2001079193A2 (en) * 2000-04-14 2001-10-25 Corvas International, Inc. Substituted hydrazinyl heteroaromatic inhibitors of thrombin
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
US6476016B2 (en) 2000-07-17 2002-11-05 3-Dimensional Pharmaceuticals, Inc. Cyclic oxyguanidine pyrazinones as protease inhibitors
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
WO2002042272A2 (en) 2000-11-20 2002-05-30 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
US7015223B1 (en) 2000-11-20 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
US7119094B1 (en) 2000-11-20 2006-10-10 Warner-Lambert Company Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
WO2003029216A1 (en) 2001-10-03 2003-04-10 Pharmacia Corporation 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade
AU2002367752A1 (en) 2001-10-03 2003-11-17 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
OA12771A (en) 2002-02-14 2006-07-04 Pharmacia Corp Substituted pyridinones as modulators of P38 map kinase.
GB0306615D0 (en) * 2003-03-22 2003-04-30 Astrazeneca Ab New use
EP1526131A1 (en) * 2003-10-22 2005-04-27 Graffinity Pharmaceuticals Aktiengesellschaft Aminoalkyl-pyrazinones and -pyridones as thrombin inhibitors
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
BRPI0612045A2 (pt) * 2005-06-17 2018-07-24 Astrazeneca Ab composto, formulação farmacêutica, uso de um composto, método de tratamento de uma condição, e, processo para preparação de um composto
WO2017067670A1 (en) 2015-10-23 2017-04-27 Pharmathen S.A. A novel process for the preparation of tryptamines and derivatives thereof

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DE3775686D1 (de) * 1986-09-26 1992-02-13 Ciba Geigy Ag Aminopyrazinone und aminotriazinone.

Also Published As

Publication number Publication date
HRP970211A2 (en) 1998-06-30
CZ340898A3 (cs) 1999-02-17
EP0900207B1 (en) 2001-11-21
BG102948A (bg) 1999-11-30
IS4853A (is) 1998-09-25
EE9800353A (et) 1999-04-15
BR9708859A (pt) 1999-08-03
EP0900207A1 (en) 1999-03-10
DE69709727D1 (de) 2002-02-21
NZ331993A (en) 2000-04-28
ATE209191T1 (de) 2001-12-15
AU2679997A (en) 1997-11-12
CA2252964A1 (en) 1997-10-30
JP3140790B2 (ja) 2001-03-05
TR199802133T2 (xx) 2000-09-21
JP2000508334A (ja) 2000-07-04
IL126404A0 (en) 1999-05-09
PL329441A1 (en) 1999-03-29
KR20000010650A (ko) 2000-02-25
SK145398A3 (en) 1999-05-07
DE69709727T2 (de) 2002-08-08
WO1997040024A1 (en) 1997-10-30
AU714985B2 (en) 2000-01-13
NO984928L (no) 1998-12-22
NO984928D0 (no) 1998-10-22

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Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed