BR0107804A - Processo para a preparação de acetil-amidiniofenilalanil-ciclohexilglicil-piridinioa laninamidas - Google Patents

Processo para a preparação de acetil-amidiniofenilalanil-ciclohexilglicil-piridinioa laninamidas

Info

Publication number
BR0107804A
BR0107804A BR0107804-6A BR0107804A BR0107804A BR 0107804 A BR0107804 A BR 0107804A BR 0107804 A BR0107804 A BR 0107804A BR 0107804 A BR0107804 A BR 0107804A
Authority
BR
Brazil
Prior art keywords
acetyl
preparation
salt
amidiniophenylalanyl
cyclohexylglycyl
Prior art date
Application number
BR0107804-6A
Other languages
English (en)
Inventor
Gerhard Breipohl
Wolfgang Holla
Heiner Jendralla
Gerhard Beck
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 BR0107804A publication Critical patent/BR0107804A/pt

Links

Classifications

    • 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
    • C07K5/08—Tripeptides
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • 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
    • 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
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic

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)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hematology (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)

Abstract

"PROCESSO PARA A PREPARAçãO DE ACETIL-AMIDINIOFENILALANIL-CICLOHEXILGLICIL-PIRIDINIOA LANINAMIDAS". A presente invenção refere-se à um processo para a preparação de acetil-amidiniofenilalanil-ciclo-hexilglicil-piridinioalaninamidas da fórmula (I), no qual os ânions X são ânions fisiologicamente aceitáveis, e seus análogos, que são inibidores eficazes do fator Xa de coagulação do sangue e que pode ser empregado, por exemplo, para a prevenção de trombose. O processo de acordo com a invenção compreende a união de ácido 2-[2acetilamino-3-(4-amidinofenil)propionilamino]-2-ciclohexilacético, que é obtido de ácido 2-[2-acetilamino-3-(4-cianofenil)-acriloilamino]-2-ciclohexilacético por hidrogenação assimétrica e conversão do grupo de ciano na amidina, ou um sal deste, com um sal de 3-(2-amino-2-carbamoiletil)-1-metilpiridínio ou um sal deste. A invenção, além disso, fornece materiais de partida e intermediários para este processo, processos para sua preparação e acetil -(S)4-amidiniofenilalanil-(S)-ciclohexilglicil-(S)-(1-metil-3-piridínio)alani namida como sal de ditosilato.
BR0107804-6A 2000-01-28 2001-01-18 Processo para a preparação de acetil-amidiniofenilalanil-ciclohexilglicil-piridinioa laninamidas BR0107804A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10003586 2000-01-28
PCT/EP2001/000523 WO2001055175A2 (en) 2000-01-28 2001-01-18 Process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides

Publications (1)

Publication Number Publication Date
BR0107804A true BR0107804A (pt) 2002-10-22

Family

ID=7628946

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0107804-6A BR0107804A (pt) 2000-01-28 2001-01-18 Processo para a preparação de acetil-amidiniofenilalanil-ciclohexilglicil-piridinioa laninamidas

Country Status (30)

Country Link
US (2) US20010031858A1 (pt)
EP (1) EP1254159B9 (pt)
JP (1) JP4778181B2 (pt)
KR (1) KR100758141B1 (pt)
CN (1) CN1176104C (pt)
AR (1) AR027246A1 (pt)
AT (1) ATE325810T1 (pt)
AU (1) AU779722B2 (pt)
BR (1) BR0107804A (pt)
CA (1) CA2398497C (pt)
CZ (1) CZ20022583A3 (pt)
DE (1) DE60119491T2 (pt)
DK (1) DK1254159T3 (pt)
EE (1) EE200200410A (pt)
ES (1) ES2262632T3 (pt)
HK (1) HK1051866A1 (pt)
HR (1) HRP20020631A2 (pt)
HU (1) HUP0301986A2 (pt)
IL (2) IL150897A0 (pt)
MX (1) MXPA02006762A (pt)
NO (1) NO20023577L (pt)
NZ (1) NZ520427A (pt)
PL (1) PL356801A1 (pt)
PT (1) PT1254159E (pt)
RU (1) RU2250212C2 (pt)
SK (1) SK10842002A3 (pt)
TW (1) TWI236481B (pt)
WO (1) WO2001055175A2 (pt)
YU (1) YU51202A (pt)
ZA (1) ZA200205990B (pt)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH695999A5 (de) * 2002-02-28 2006-11-15 Wilex Ag Verfahren zur Herstellung von 3- Amidinophenylalanin-Derivaten.
US20090215025A1 (en) * 2005-12-07 2009-08-27 Technische Universitat Munchen Small peptidic and peptido-mimetic affinity ligands for factor viii and factor viii-like proteins
CN101774942B (zh) * 2010-01-27 2012-08-22 宁波武盛化学有限公司 制备n-乙酰基-dl-环己基甘氨酸的方法
EP2560493B1 (en) * 2010-04-20 2018-06-06 Chiral Quest, Inc. An enantioselective process for cycloalkenyl b-substituted alanines
EP2646150A4 (en) * 2010-11-29 2014-10-08 Takasago Perfumery Co Ltd CATALYST FOR ASYMMETRIC HYDROGENATION AND METHOD FOR PRODUCING AN OPTICALLY ACTIVE CARBONYL COMPOUND THEREWITH
CN115068469B (zh) * 2022-07-08 2024-02-27 深圳市小分子新药创新中心有限公司 Tigit抑制剂及其应用

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2916711A1 (de) 1979-04-25 1980-11-06 Behringwerke Ag Blutgerinnungsfaktoren und verfahren zu ihrer herstellung
US4440679A (en) * 1980-03-05 1984-04-03 Cutter Laboratories, Inc. Pasteurized therapeutically active protein compositions
US4623717A (en) * 1980-03-05 1986-11-18 Miles Laboratories, Inc. Pasteurized therapeutically active protein compositions
SI9520044B (sl) * 1994-04-26 2004-08-31 Aventis Pharmaceuticals Inc. Inhibitorji Xa faktorja
US5849510A (en) 1994-04-26 1998-12-15 Selectide Corporation Factor Xa inhibitors
AU717995B2 (en) * 1995-12-20 2000-04-06 Aventis Pharmaceuticals Inc. Novel process for preparing N-acetyl(L)-4-cyanophenylalanine Ac-(l)-Phe(4-CN)-OH and N-Acetyl-(L)-p-amidinophenylalanine -cyclohexylglycine-beta-(3-N-methylpyridinium)-alanine Ac- (L)-pAph-Cgh-PalMe(3)-NH2
DE19856443A1 (de) 1998-12-08 2000-06-21 Centeon Pharma Gmbh Stabilisiertes Antithrombin III-Präparat

Also Published As

Publication number Publication date
KR100758141B1 (ko) 2007-09-13
US7084250B2 (en) 2006-08-01
CN1176104C (zh) 2004-11-17
CA2398497A1 (en) 2001-08-02
IL150897A0 (en) 2003-02-12
DK1254159T3 (da) 2006-09-11
IL150897A (en) 2008-08-07
DE60119491T2 (de) 2006-11-16
YU51202A (sh) 2005-11-28
MXPA02006762A (es) 2002-10-23
PT1254159E (pt) 2006-07-31
US20010031858A1 (en) 2001-10-18
NZ520427A (en) 2004-02-27
AU4051601A (en) 2001-08-07
SK10842002A3 (sk) 2003-04-01
EP1254159A2 (en) 2002-11-06
JP2003523364A (ja) 2003-08-05
AU779722B2 (en) 2005-02-10
RU2250212C2 (ru) 2005-04-20
KR20030019306A (ko) 2003-03-06
HK1051866A1 (en) 2003-08-22
CA2398497C (en) 2011-04-26
PL356801A1 (en) 2004-07-12
TWI236481B (en) 2005-07-21
ES2262632T3 (es) 2006-12-01
EP1254159B9 (en) 2006-06-28
ATE325810T1 (de) 2006-06-15
US20040225109A1 (en) 2004-11-11
WO2001055175A2 (en) 2001-08-02
HRP20020631A2 (en) 2004-12-31
NO20023577L (no) 2002-08-28
EP1254159B1 (en) 2006-05-10
JP4778181B2 (ja) 2011-09-21
ZA200205990B (en) 2003-04-30
CZ20022583A3 (cs) 2002-10-16
WO2001055175A3 (en) 2002-02-21
HUP0301986A2 (hu) 2003-09-29
RU2002123046A (ru) 2004-01-10
AR027246A1 (es) 2003-03-19
EE200200410A (et) 2003-12-15
DE60119491D1 (de) 2006-06-14
CN1396928A (zh) 2003-02-12
NO20023577D0 (no) 2002-07-26

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Legal Events

Date Code Title Description
B25D Requested change of name of applicant approved

Owner name: SANOFI-AVENTIS DEUTSCHLAND GMBH (DE)

Free format text: ALTERADO DE: AVENTIS PHARMA DEUTSCHLAND GMBH

B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements