BRPI0408444A - derivados de 1-n-(fenil)-2-n-(fenil) pirazolidina-1,2-dicarboxamida como inibidores de fator xa de coagulação para o tratamento de trombose - Google Patents

derivados de 1-n-(fenil)-2-n-(fenil) pirazolidina-1,2-dicarboxamida como inibidores de fator xa de coagulação para o tratamento de trombose

Info

Publication number
BRPI0408444A
BRPI0408444A BRPI0408444-6A BRPI0408444A BRPI0408444A BR PI0408444 A BRPI0408444 A BR PI0408444A BR PI0408444 A BRPI0408444 A BR PI0408444A BR PI0408444 A BRPI0408444 A BR PI0408444A
Authority
BR
Brazil
Prior art keywords
phenyl
treatment
inhibitors
coagulation factor
pyrazolidine
Prior art date
Application number
BRPI0408444-6A
Other languages
English (en)
Inventor
Werner Mederski
Christos Tsaklakidis
Dieter Dorsch
Bertram Cezanne
Johannes Gleitz
Original Assignee
Merck Patent Gmbh
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 DE10315377A external-priority patent/DE10315377A1/de
Priority claimed from DE2003129295 external-priority patent/DE10329295A1/de
Priority claimed from DE10336570A external-priority patent/DE10336570A1/de
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of BRPI0408444A publication Critical patent/BRPI0408444A/pt

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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—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
    • 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
    • C07D231/04—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/06—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

"DERIVADOS DE 1-N-(FENIL)-2-N-(FENIL) PIRAZOLIDINA-1,2-DICARBOXAMIDA COMO INIBIDORES DE FATOR XA DE COAGULAçãO PARA O TRATAMENTO DE TROMBOSE". A presente invenção refere-se a compostos de fórmula (I), em que R, R¬ 1¬, R¬ 2¬ e R¬ 3¬ têm os significados indicados na reivindicação 1, são inibidores de fator de coagulação Xa e podem ser empregados para profilaxia e/ou terapia de doenças tromboembólicas e para o tratamento de tumores.
BRPI0408444-6A 2003-04-03 2004-03-09 derivados de 1-n-(fenil)-2-n-(fenil) pirazolidina-1,2-dicarboxamida como inibidores de fator xa de coagulação para o tratamento de trombose BRPI0408444A (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE10315377A DE10315377A1 (de) 2003-04-03 2003-04-03 Carbonylverbindungen
DE2003129295 DE10329295A1 (de) 2003-06-30 2003-06-30 Carbonylverbindungen
DE10336570A DE10336570A1 (de) 2003-08-08 2003-08-08 Azaprolinderivate
PCT/EP2004/002407 WO2004087696A1 (de) 2003-04-03 2004-03-09 Pirazolidin-1,2-dicarbonsaüre-1-((phenyl)-amid)-2-((phenyl)-amid) derivate als koagulationsfaktor xa inhibitoren zur behandlung von thrombosen

Publications (1)

Publication Number Publication Date
BRPI0408444A true BRPI0408444A (pt) 2006-04-04

Family

ID=33135448

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0408444-6A BRPI0408444A (pt) 2003-04-03 2004-03-09 derivados de 1-n-(fenil)-2-n-(fenil) pirazolidina-1,2-dicarboxamida como inibidores de fator xa de coagulação para o tratamento de trombose

Country Status (14)

Country Link
US (1) US7557102B2 (pt)
EP (1) EP1608645B1 (pt)
JP (1) JP4624982B2 (pt)
KR (1) KR20050109617A (pt)
AR (1) AR043833A1 (pt)
AT (1) ATE361296T1 (pt)
AU (1) AU2004226281B2 (pt)
BR (1) BRPI0408444A (pt)
CA (1) CA2520894C (pt)
DE (1) DE502004003688D1 (pt)
ES (1) ES2285444T3 (pt)
MX (1) MXPA05010445A (pt)
PL (1) PL377864A1 (pt)
WO (1) WO2004087696A1 (pt)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10358814A1 (de) 2003-12-16 2005-07-21 Merck Patent Gmbh Prolinylarylacetamide
DE102004016605A1 (de) * 2004-04-03 2005-10-20 Merck Patent Gmbh Thiocarbamoylproline
BRPI0618523A2 (pt) * 2005-11-11 2011-09-06 Hoffmann La Roche compostos de aminas cìclicas fundidas carbocìclicas, composições farmacêuticas e usos dos mesmos
US7601752B2 (en) 2005-11-16 2009-10-13 Hoffmann-La Roche Inc. Pyrrolidine derivatives
US8673920B2 (en) * 2009-05-06 2014-03-18 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2632465B1 (en) 2010-10-27 2015-12-30 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2012058134A1 (en) 2010-10-29 2012-05-03 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
TW201249824A (en) 2011-03-09 2012-12-16 Glaxosmithkline Llc Peptide deformylase inhibitors
ES2605164T3 (es) 2011-08-19 2017-03-13 Merck Sharp & Dohme Corp. Inhibidores del canal de potasio de la médula renal externa
WO2013039802A1 (en) 2011-09-16 2013-03-21 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2771004B1 (en) 2011-10-25 2016-05-18 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2771005B1 (en) 2011-10-25 2016-05-18 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2773199B1 (en) 2011-10-31 2019-04-10 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9108947B2 (en) 2011-10-31 2015-08-18 Merck Sharp & Dohme Corp. Inhibitors of the Renal Outer Medullary Potassium channel
US9493474B2 (en) 2011-10-31 2016-11-15 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013088456A1 (en) 2011-12-15 2013-06-20 Council Of Scientific & Industrial Research A new organocatalytic synthesis of chiral pyrazolidines and their analogues
US9206199B2 (en) 2011-12-16 2015-12-08 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
AR092031A1 (es) 2012-07-26 2015-03-18 Merck Sharp & Dohme Inhibidores del canal de potasio medular externo renal
WO2014085210A1 (en) 2012-11-29 2014-06-05 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2014099633A2 (en) 2012-12-19 2014-06-26 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2956142B1 (en) 2013-02-18 2017-09-20 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9765074B2 (en) 2013-03-15 2017-09-19 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9751881B2 (en) 2013-07-31 2017-09-05 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
US9951052B2 (en) 2013-10-31 2018-04-24 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001064642A2 (en) 2000-02-29 2001-09-07 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
DE10113402A1 (de) * 2001-03-20 2002-09-26 Merck Patent Gmbh Biurethanderivate
US6821971B2 (en) 2001-09-20 2004-11-23 The Procter & Gamble Company Fused pyrazolone compounds which inhibit the release of inflammatory cytokines

Also Published As

Publication number Publication date
EP1608645A1 (de) 2005-12-28
US7557102B2 (en) 2009-07-07
ES2285444T3 (es) 2007-11-16
US20060183742A1 (en) 2006-08-17
EP1608645B1 (de) 2007-05-02
WO2004087696A1 (de) 2004-10-14
JP4624982B2 (ja) 2011-02-02
MXPA05010445A (es) 2005-11-04
ATE361296T1 (de) 2007-05-15
JP2006522038A (ja) 2006-09-28
AR043833A1 (es) 2005-08-17
DE502004003688D1 (de) 2007-06-14
AU2004226281A1 (en) 2004-10-14
AU2004226281B2 (en) 2010-06-10
KR20050109617A (ko) 2005-11-21
CA2520894C (en) 2013-02-05
CA2520894A1 (en) 2004-10-14
PL377864A1 (pl) 2006-02-20

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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 AS 5A, 6A, 7A E 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 8.6 PUBLICADO NA RPI 2159 DE 22/05/2012.