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

Info

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
Authority
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
Original Assignee
Aventis Pharma 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
Application filed by Aventis Pharma Gmbh filed Critical Aventis Pharma Gmbh
Publication of BR0108694A publication Critical patent/BR0108694A/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
    • C07D213/24—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
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P9/10—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
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives 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
    • C07C279/14—Derivatives 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The 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)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Pulmonology (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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US20040185073A1 (en) * 2003-03-17 2004-09-23 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Cosmetic compositions containing salts of malonic acid
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
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
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
MX2007010602A (es) * 2005-03-24 2008-03-04 Warner Lambert Co Formas cristalinas de un inhibidor del factor xa de pirrolidina conocido.
JP2014503474A (ja) 2010-10-20 2014-02-13 バイオフオーミツクス・インコーポレイテツド エネルギー移動手段の存在下での急速回収を用いたメチレンマロナートの合成
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US9617377B1 (en) 2016-06-03 2017-04-11 Sirrus, Inc. Polyester macromers containing 1,1-dicarbonyl-substituted 1 alkenes
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Also Published As

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

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