BR0108694A - Derivados de ácido malÈnico, processo para preparação dos mesmos, uso dos mesmos como inibidor de atividade do fator xa e composições farmacêuticas que contêm os mesmos - Google Patents

Derivados de ácido malÈnico, processo para preparação dos mesmos, uso dos mesmos como inibidor de atividade do fator xa e composições farmacêuticas que contêm os mesmos

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Publication number
BR0108694A
BR0108694A BR0108694-4A BR0108694A BR0108694A BR 0108694 A BR0108694 A BR 0108694A BR 0108694 A BR0108694 A BR 0108694A BR 0108694 A BR0108694 A BR 0108694A
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BR
Brazil
Prior art keywords
formula
factor
activity
same
compounds
Prior art date
Application number
BR0108694-4A
Other languages
English (en)
Inventor
Fahad Al-Obeidi
Armin Walser
Peter Wildgoose
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Aventis Pharma Gmbh
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Publication date
Application filed by Aventis Pharma Gmbh filed Critical Aventis Pharma Gmbh
Publication of BR0108694A publication Critical patent/BR0108694A/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic 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
    • C07D213/54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56Amides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C257/00Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/14Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrrole Compounds (AREA)

Abstract

"DERIVADOS DE áCIDO MALÈNICO, PROCESSOS PARA PREPARAçãO DOS MESMOS, USO DOS MESMOS COMO INIBIDOR DE ATIVIDADE DO FATOR XA E COMPOSIçõES FARMACêUTICAS QUE CONTêM OS MESMOS". A presente invenção refere-se a novos compostos para a inibição de proteínas de coagulação sang³ínea e, mais particularmente, a derivados de ácido malónico da fórmula (I), em que R(1), R(2), R(3),R(4), R(5) e R(6) têm os significados indicados nas reivindicações. Os compostos da fórmula (I) são inibidores do fator Xa de enzima de coagulação sang³ínea. A invenção refere-se, também, a processos para a preparação dos compostos da fórmula (I), a métodos para inibir a atividade do fator Xa e para inibir a coagulação sang³ínea, ao uso dos compostos da fórmula (I) no tratamento e profilaxia de doenças, que podem ser tratadas ou evitada pela inibição da atividade do fator Xa, tal como doenças tromboembólicas, e ao uso dos compostos da fórmula (I) na preparação de medicamentos a ser aplicados nessas doenças. A invenção refere-se, ainda, a composições, que contêm um composto da fórmula (I), em mistura ou então em associação com um veículo inerte, particularmente, composições farmacêuticas, que contêm um composto da fórmula (I), junto com substâncias de veículo e substâncias auxiliares farmaceuticamente aceitáveis.
BR0108694-4A 2000-02-26 2001-02-21 Derivados de ácido malÈnico, processo para preparação dos mesmos, uso dos mesmos como inibidor de atividade do fator xa e composições farmacêuticas que contêm os mesmos BR0108694A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP00104041A EP1127884A1 (en) 2000-02-26 2000-02-26 Novel malonic acid derivatives, processes for their preparation, their use as inhibitor of factor XA activity and pharmaceutical compositions containing them
PCT/EP2001/001928 WO2001062735A1 (en) 2000-02-26 2001-02-21 Novel malonic acid derivatives, processes for their preparation, their use as inhibitor of factor xa activity and pharmaceutical compositions containing them

Publications (1)

Publication Number Publication Date
BR0108694A true BR0108694A (pt) 2002-12-10

Family

ID=8167968

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0108694-4A BR0108694A (pt) 2000-02-26 2001-02-21 Derivados de ácido malÈnico, processo para preparação dos mesmos, uso dos mesmos como inibidor de atividade do fator xa e composições farmacêuticas que contêm os mesmos

Country Status (23)

Country Link
US (1) US6794365B2 (pt)
EP (2) EP1127884A1 (pt)
JP (1) JP2003524001A (pt)
KR (1) KR20020079892A (pt)
CN (1) CN1406226A (pt)
AR (1) AR027533A1 (pt)
AT (1) ATE314350T1 (pt)
AU (1) AU2001235486A1 (pt)
BR (1) BR0108694A (pt)
CA (1) CA2400871C (pt)
CZ (1) CZ20022862A3 (pt)
DE (1) DE60116272T2 (pt)
ES (1) ES2254370T3 (pt)
HK (1) HK1052696A1 (pt)
HU (1) HUP0300080A3 (pt)
IL (1) IL151459A0 (pt)
MX (1) MXPA02007398A (pt)
NO (1) NO20024040L (pt)
NZ (1) NZ520982A (pt)
PL (1) PL357183A1 (pt)
RU (1) RU2002125671A (pt)
WO (1) WO2001062735A1 (pt)
ZA (1) ZA200206581B (pt)

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US20040185074A1 (en) * 2003-03-17 2004-09-23 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Odor control in amine salt containing cosmetic compositions
US20040185015A1 (en) * 2003-03-17 2004-09-23 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Sunscreen cosmetic compositions storage stabilized with malonate salts
US20040202689A1 (en) * 2003-03-17 2004-10-14 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Terpenoid fragrance components stabilized with malonic acid salts
US9249265B1 (en) 2014-09-08 2016-02-02 Sirrus, Inc. Emulsion polymers including one or more 1,1-disubstituted alkene compounds, emulsion methods, and polymer compositions
US9279022B1 (en) 2014-09-08 2016-03-08 Sirrus, Inc. Solution polymers including one or more 1,1-disubstituted alkene compounds, solution polymerization methods, and polymer compositions
RU2013122684A (ru) 2010-10-20 2014-11-27 Биоформикс Инк. Синтез метиленмалонатов с применением быстрого извлечения в присутствии средства переноса энергии
US10414839B2 (en) 2010-10-20 2019-09-17 Sirrus, Inc. Polymers including a methylene beta-ketoester and products formed therefrom
US9828324B2 (en) 2010-10-20 2017-11-28 Sirrus, Inc. Methylene beta-diketone monomers, methods for making methylene beta-diketone monomers, polymerizable compositions and products formed therefrom
US9527795B2 (en) 2011-10-19 2016-12-27 Sirrus, Inc. Methylene beta-ketoester monomers, methods for making methylene beta-ketoester monomers, polymerizable compositions and products formed therefrom
JP6188252B2 (ja) 2012-03-30 2017-08-30 シラス・インコーポレイテッド 重合性組成物の活性化方法、重合系およびこれにより形成される製品
EP3153530B1 (en) 2012-03-30 2021-02-24 Sirrus, Inc. Composite and laminate articles and polymerizable systems for producing the same
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Also Published As

Publication number Publication date
ES2254370T3 (es) 2006-06-16
US6794365B2 (en) 2004-09-21
US20020022596A1 (en) 2002-02-21
KR20020079892A (ko) 2002-10-19
HK1052696A1 (zh) 2003-09-26
NO20024040D0 (no) 2002-08-23
DE60116272D1 (de) 2006-02-02
MXPA02007398A (es) 2002-12-09
WO2001062735A1 (en) 2001-08-30
ZA200206581B (en) 2003-07-28
NZ520982A (en) 2004-05-28
HUP0300080A2 (hu) 2003-06-28
EP1127884A1 (en) 2001-08-29
NO20024040L (no) 2002-09-24
HUP0300080A3 (en) 2004-07-28
PL357183A1 (en) 2004-07-26
JP2003524001A (ja) 2003-08-12
EP1265867B1 (en) 2005-12-28
AU2001235486A1 (en) 2001-09-03
DE60116272T2 (de) 2006-08-17
ATE314350T1 (de) 2006-01-15
CZ20022862A3 (cs) 2002-11-13
CN1406226A (zh) 2003-03-26
CA2400871C (en) 2011-04-26
AR027533A1 (es) 2003-04-02
CA2400871A1 (en) 2001-08-30
RU2002125671A (ru) 2004-01-10
IL151459A0 (en) 2003-04-10
EP1265867A1 (en) 2002-12-18

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