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AR027533A1 - Derivados de acido malonico, procesos para su preparacion, su uso y composiciones farmaceuticas que los contienen - Google Patents

Derivados de acido malonico, procesos para su preparacion, su uso y composiciones farmaceuticas que los contienen

Info

Publication number
AR027533A1
AR027533A1 ARP010100806A ARP010100806A AR027533A1 AR 027533 A1 AR027533 A1 AR 027533A1 AR P010100806 A ARP010100806 A AR P010100806A AR P010100806 A ARP010100806 A AR P010100806A AR 027533 A1 AR027533 A1 AR 027533A1
Authority
AR
Argentina
Prior art keywords
formula
compounds
preparation
compositions containing
refers
Prior art date
Application number
ARP010100806A
Other languages
English (en)
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 AR027533A1 publication Critical patent/AR027533A1/es

Links

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)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Hematology (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

La presente se refiere a nuevos compuestos para la inhibicion de las proteínas coagulado sangre, y más particularmente se refiere a derivados de ácidomalonico de la Formula (1) en la cual R1, R2, R3, R4, R5 y R6 tienen los significados indicados en l as reivindicaciones. Los compuestos de la Formula (1) soninhibidores del factor Xa enzima de la coagulacion de la sangre. La presente se refiere también a procesos para la preparacion de los compuestos de la Formula(1), a métodos para inhibir la acti vidad del factor Xa y para inhibir la coagulacion de la sangre, al uso de los compuestos de la Formula (1) en el tratamientoy profilaxis de enfermedades que pueden ser tratadas o prevenidas mediante la inhibicion de la actividad del factor Xa tales c omo las enfermedadestromboembolicas, y al uso de los compuestos de la Formula (1) en la preparacion de medicamentos a ser aplicados en dichas enfermedades. La presente se refieretambién a composiciones que contienen un compuesto de la Formula (1) mez clado junto con o asociado de alguna otra manera con un vehículo o portador inerte, enparticular composiciones farmacéuticas que contienen un compuesto de la Formula (1) junto con sustancias vehículo y sustancias auxiliares, farmacéuticamenteaceptabl es.
ARP010100806A 2000-02-26 2001-02-22 Derivados de acido malonico, procesos para su preparacion, su uso y composiciones farmaceuticas que los contienen AR027533A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
AR027533A1 true AR027533A1 (es) 2003-04-02

Family

ID=8167968

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010100806A AR027533A1 (es) 2000-02-26 2001-02-22 Derivados de acido malonico, procesos para su preparacion, su uso y composiciones farmaceuticas que los contienen

Country Status (23)

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

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US20030224023A1 (en) * 2002-05-29 2003-12-04 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Cosmetic compositions with hydroxy amine 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
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
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
US20040185073A1 (en) * 2003-03-17 2004-09-23 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Cosmetic compositions containing salts of malonic acid
US8609885B2 (en) 2010-10-20 2013-12-17 Bioformix Inc. Synthesis of methylene malonates substantially free of impurities
US10414839B2 (en) 2010-10-20 2019-09-17 Sirrus, Inc. Polymers including a methylene beta-ketoester and products formed therefrom
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
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
CA2853073A1 (en) 2011-10-19 2013-04-25 Bioformix Inc. Methylene beta-diketone monomers, methods for making methylene beta-diketone monomers, polymerizable compositions and products formed therefrom
EP2831185B1 (en) 2012-03-30 2019-09-25 Sirrus, Inc. Ink and coating formulations and polymerizable systems for producing the same
US10913875B2 (en) 2012-03-30 2021-02-09 Sirrus, Inc. Composite and laminate articles and polymerizable systems for producing the same
US9181365B2 (en) 2012-03-30 2015-11-10 Sirrus, Inc. Methods for activating polymerizable compositions, polymerizable systems, and products formed thereby
WO2013181600A2 (en) 2012-06-01 2013-12-05 Bioformix Inc. Optical material and articles formed therefrom
EP2920231B1 (en) 2012-11-16 2020-05-06 Sirrus, Inc. Plastics bonding systems and methods
EP3712928A1 (en) 2012-11-30 2020-09-23 Sirrus, Inc. Composite compositions for electronics applications
CN110204441A (zh) 2013-01-11 2019-09-06 瑟拉斯公司 经过双(羟甲基)丙二酸酯的途径获得亚甲基丙二酸酯的方法
US9315597B2 (en) 2014-09-08 2016-04-19 Sirrus, Inc. Compositions containing 1,1-disubstituted alkene compounds for preparing polymers having enhanced glass transition temperatures
US9416091B1 (en) 2015-02-04 2016-08-16 Sirrus, Inc. Catalytic transesterification of ester compounds with groups reactive under transesterification conditions
US10501400B2 (en) 2015-02-04 2019-12-10 Sirrus, Inc. Heterogeneous catalytic transesterification of ester compounds with groups reactive under transesterification conditions
US9334430B1 (en) 2015-05-29 2016-05-10 Sirrus, Inc. Encapsulated polymerization initiators, polymerization systems and methods using the same
US9217098B1 (en) 2015-06-01 2015-12-22 Sirrus, Inc. Electroinitiated polymerization of compositions having a 1,1-disubstituted alkene compound
US9518001B1 (en) 2016-05-13 2016-12-13 Sirrus, Inc. High purity 1,1-dicarbonyl substituted-1-alkenes and methods for their preparation
US9617377B1 (en) 2016-06-03 2017-04-11 Sirrus, Inc. Polyester macromers containing 1,1-dicarbonyl-substituted 1 alkenes
US10428177B2 (en) 2016-06-03 2019-10-01 Sirrus, Inc. Water absorbing or water soluble polymers, intermediate compounds, and methods thereof
US9567475B1 (en) 2016-06-03 2017-02-14 Sirrus, Inc. Coatings containing polyester macromers containing 1,1-dicarbonyl-substituted 1 alkenes
US10196481B2 (en) 2016-06-03 2019-02-05 Sirrus, Inc. Polymer and other compounds functionalized with terminal 1,1-disubstituted alkene monomer(s) and methods thereof
CN106501472A (zh) * 2016-11-29 2017-03-15 昆明理工大学 一种基于抗凝血生化指数评价三七活血作用的方法
CN111018734B (zh) * 2019-12-13 2020-12-22 福建海西新药创制有限公司 一种盐酸西那卡塞中间体的合成方法
WO2023223296A1 (en) * 2022-05-20 2023-11-23 Radius Health, Inc. Process of making abaloparatide
CN115299636B (zh) * 2022-08-17 2025-02-14 中国烟草总公司郑州烟草研究院 一种卷烟滤嘴用功能吸附丸芯及其制备方法和烟支

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ID29979A (id) * 1999-01-02 2001-10-25 Aventis Pharma Gmbh Turunan asam malonat baru, proses pembuatannya, penggunaannya dan komposisi sediaan farmasi yang mengandung bahan tersebut (penghambatan aktivitas faktor xa)
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HUP0202647A3 (en) 1999-01-02 2003-12-29 Aventis Pharma Gmbh Arylalkanoyl derivatives, processes for their preparation, their use and pharmaceutical compositions containing them

Also Published As

Publication number Publication date
MXPA02007398A (es) 2002-12-09
KR20020079892A (ko) 2002-10-19
NZ520982A (en) 2004-05-28
NO20024040L (no) 2002-09-24
DE60116272D1 (de) 2006-02-02
CN1406226A (zh) 2003-03-26
NO20024040D0 (no) 2002-08-23
US20020022596A1 (en) 2002-02-21
AU2001235486A1 (en) 2001-09-03
WO2001062735A1 (en) 2001-08-30
CA2400871A1 (en) 2001-08-30
CZ20022862A3 (cs) 2002-11-13
CA2400871C (en) 2011-04-26
ES2254370T3 (es) 2006-06-16
HUP0300080A3 (en) 2004-07-28
HK1052696A1 (zh) 2003-09-26
ATE314350T1 (de) 2006-01-15
EP1265867A1 (en) 2002-12-18
US6794365B2 (en) 2004-09-21
PL357183A1 (en) 2004-07-26
HUP0300080A2 (hu) 2003-06-28
JP2003524001A (ja) 2003-08-12
EP1127884A1 (en) 2001-08-29
RU2002125671A (ru) 2004-01-10
BR0108694A (pt) 2002-12-10
EP1265867B1 (en) 2005-12-28
ZA200206581B (en) 2003-07-28
DE60116272T2 (de) 2006-08-17
IL151459A0 (en) 2003-04-10

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