CN1406226A - 新型丙二酸衍生物,它们的制备方法,它们作为因子xa活性的抑制剂的用途和含有它们的药物组合物 - Google Patents

新型丙二酸衍生物,它们的制备方法,它们作为因子xa活性的抑制剂的用途和含有它们的药物组合物 Download PDF

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Publication number
CN1406226A
CN1406226A CN01805589A CN01805589A CN1406226A CN 1406226 A CN1406226 A CN 1406226A CN 01805589 A CN01805589 A CN 01805589A CN 01805589 A CN01805589 A CN 01805589A CN 1406226 A CN1406226 A CN 1406226A
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China
Prior art keywords
benzyl
methyl
amino
general formula
alkyl
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Pending
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CN01805589A
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English (en)
Chinese (zh)
Inventor
F·阿尔－欧拜迪
A·沃瑟尔
P·维尔德谷斯
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Sanofi Aventis Deutschland GmbH
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Aventis Pharma Deutschland GmbH
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Publication of CN1406226A publication Critical patent/CN1406226A/zh
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Diabetes (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)
CN01805589A 2000-02-26 2001-02-21 新型丙二酸衍生物,它们的制备方法,它们作为因子xa活性的抑制剂的用途和含有它们的药物组合物 Pending CN1406226A (zh)

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
EP00104041.9 2000-02-26

Publications (1)

Publication Number Publication Date
CN1406226A true CN1406226A (zh) 2003-03-26

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CN01805589A Pending CN1406226A (zh) 2000-02-26 2001-02-21 新型丙二酸衍生物,它们的制备方法,它们作为因子xa活性的抑制剂的用途和含有它们的药物组合物

Country Status (23)

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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN111018734A (zh) * 2019-12-13 2020-04-17 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

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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
US20040185073A1 (en) * 2003-03-17 2004-09-23 Unilever Home & Personal Care Usa, Division Of Conopco, Inc. Cosmetic compositions containing salts of malonic acid
MX2007010602A (es) * 2005-03-24 2008-03-04 Warner Lambert Co Formas cristalinas de un inhibidor del factor xa de pirrolidina conocido.
WO2012054633A2 (en) 2010-10-20 2012-04-26 Bioformix, Llc Synthesis of methylene malonates using rapid recovery in the presence of a heat transfer agent
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
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
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
US10414839B2 (en) 2010-10-20 2019-09-17 Sirrus, Inc. Polymers including a methylene beta-ketoester and products formed therefrom
MX360463B (es) 2011-10-19 2018-11-05 Sirrus Inc Monomeros de beta-cetoester de metileno, procedimientos de fabricación de monomeros de beta-cetoester de metileno, composiciones polimerizables y productos formados a partir de las mismas.
US9234107B2 (en) 2012-03-30 2016-01-12 Sirrus, Inc. Ink coating formulations and polymerizable systems for producing the same
WO2013149165A1 (en) 2012-03-30 2013-10-03 Bioformix Inc. Methods for activating polymerizable compositions, polymerizable systems, and products formed thereby
US10913875B2 (en) 2012-03-30 2021-02-09 Sirrus, Inc. Composite and laminate articles and polymerizable systems for producing the same
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
CN105164797B (zh) 2012-11-30 2019-04-19 瑟拉斯公司 用于电子应用的复合组合物
EP2943462B1 (en) 2013-01-11 2018-06-27 Sirrus, Inc. Method to obtain methylene malonate via bis(hydroxymethyl) malonate pathway
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
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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
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
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US10428177B2 (en) 2016-06-03 2019-10-01 Sirrus, Inc. Water absorbing or water soluble polymers, intermediate compounds, and methods thereof
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN111018734A (zh) * 2019-12-13 2020-04-17 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

Also Published As

Publication number Publication date
HUP0300080A3 (en) 2004-07-28
IL151459A0 (en) 2003-04-10
ATE314350T1 (de) 2006-01-15
ZA200206581B (en) 2003-07-28
AR027533A1 (es) 2003-04-02
NO20024040L (no) 2002-09-24
US6794365B2 (en) 2004-09-21
HUP0300080A2 (hu) 2003-06-28
US20020022596A1 (en) 2002-02-21
EP1265867A1 (en) 2002-12-18
NO20024040D0 (no) 2002-08-23
DE60116272T2 (de) 2006-08-17
CA2400871A1 (en) 2001-08-30
CA2400871C (en) 2011-04-26
KR20020079892A (ko) 2002-10-19
NZ520982A (en) 2004-05-28
HK1052696A1 (zh) 2003-09-26
EP1265867B1 (en) 2005-12-28
ES2254370T3 (es) 2006-06-16
AU2001235486A1 (en) 2001-09-03
RU2002125671A (ru) 2004-01-10
BR0108694A (pt) 2002-12-10
PL357183A1 (en) 2004-07-26
EP1127884A1 (en) 2001-08-29
CZ20022862A3 (cs) 2002-11-13
WO2001062735A1 (en) 2001-08-30
JP2003524001A (ja) 2003-08-12
MXPA02007398A (es) 2002-12-09
DE60116272D1 (de) 2006-02-02

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