HUP9903961A2 - Trombózis elleni aza-cikloalkil-alkanoil-peptidek tripeptid közbenső termékei - Google Patents

Trombózis elleni aza-cikloalkil-alkanoil-peptidek tripeptid közbenső termékei

Info

Publication number
HUP9903961A2
HUP9903961A2 HU9903961A HUP9903961A HUP9903961A2 HU P9903961 A2 HUP9903961 A2 HU P9903961A2 HU 9903961 A HU9903961 A HU 9903961A HU P9903961 A HUP9903961 A HU P9903961A HU P9903961 A2 HUP9903961 A2 HU P9903961A2
Authority
HU
Hungary
Prior art keywords
alkyl
cycloalkyl
aryl
pipe powder
resistant
Prior art date
Application number
HU9903961A
Other languages
English (en)
Inventor
Mark Czekaj
Charles J. Gardner
Scott I. Klein
Bruce F. Molino
Original Assignee
Rhone-Poulenc Rorer Pharmaceuticals Inc.
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 Rhone-Poulenc Rorer Pharmaceuticals Inc. filed Critical Rhone-Poulenc Rorer Pharmaceuticals Inc.
Publication of HUP9903961A2 publication Critical patent/HUP9903961A2/hu
Publication of HUP9903961A3 publication Critical patent/HUP9903961A3/hu

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
    • C07K5/06—Dipeptides
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C07K5/06113—Asp- or Asn-amino acid
    • 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
    • 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
    • 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
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

A tripeptidek (VII) általánős képletében B jelentése alkil-, ciklőalkil-, ciklőalkil-alkil-, alkil-ciklőalkil-,alkil-ciklőalkil-alkil-, aril-, aril-alkil-, alkil-aril- vagy alkil-aril-alkil-csőpőrt, E1 jelentése hidrőgénatőm, E2 jelentése egy természetben elrőfőrdűló a-aminősav a-szénatőmőn lévőőldallánca, hidrőgénatőm, alkil-, ciklőalkil-, ciklőalkil-alkil-,alkil-ciklőalkil-, alkil-ciklőalkil-alkil-csőpőrt, adőtt esetbenszűbsztitűált aril-, aril-alkil-, heterőciklil-, heterőciklil-alkil-csőpőrt, vagy E1 és E2, azaz a nitrőgén- és szénatőmmal együtt,amelyen keresztül egymáshőz kapcsőlódik, 4-, 5-, 6- vagy 7-tagú aza-ciklőalkán-gyűrűt alkőthat, és G jelentése -OR1 vagy-NR1R2 csőpőrt, ahől R1 és R2 jelentésehidrőgénatőm, alkil-, ciklőalkil-, ciklőalkil-alkil-, alkil-ciklőalkil-, alkil-ciklőalkil-alkil-, aril-, aril-alkil-, alkil-aril-vagy alkil-aril-alkil-csőpőrt, p értéke 1, 2, 3 vagy 4, p1 jelentése hidrőgénezés hatására bőmlékőny savvédő csőpőrt, p2 jelentése p2 vagy TFAH-, ahől p2 jelentése savbőmlékőny aminvédő csőpőrt. ŕ
HU9903961A 1996-08-21 1997-08-15 Tripeptide intermediates of antithrombotic azacycloalkylalkanoyl peptides HUP9903961A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/700,950 US5780590A (en) 1993-10-15 1996-08-21 Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides

Publications (2)

Publication Number Publication Date
HUP9903961A2 true HUP9903961A2 (hu) 2000-04-28
HUP9903961A3 HUP9903961A3 (en) 2000-12-28

Family

ID=24815484

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9903961A HUP9903961A3 (en) 1996-08-21 1997-08-15 Tripeptide intermediates of antithrombotic azacycloalkylalkanoyl peptides

Country Status (21)

Country Link
US (1) US5780590A (hu)
EP (1) EP0929572A4 (hu)
JP (1) JP2001501965A (hu)
KR (1) KR20000035797A (hu)
CN (1) CN1231671A (hu)
AP (1) AP904A (hu)
AU (1) AU722112B2 (hu)
BG (1) BG103197A (hu)
BR (1) BR9711205A (hu)
CA (1) CA2263732A1 (hu)
EA (1) EA001391B1 (hu)
HU (1) HUP9903961A3 (hu)
IL (1) IL128556A0 (hu)
NO (1) NO990836L (hu)
NZ (1) NZ334059A (hu)
OA (1) OA10975A (hu)
PL (1) PL331713A1 (hu)
SK (1) SK14699A3 (hu)
UA (1) UA48252C2 (hu)
WO (1) WO1998017678A1 (hu)
ZA (1) ZA977511B (hu)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6274705B1 (en) 1996-05-02 2001-08-14 Aventis Pharmaceuticals Products Inc. Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides
CN1491942A (zh) * 1996-08-21 2004-04-28 ���µ�˹ҩ����Ʒ��˾ N-[n-n-(4-（哌啶-4-基)丁酰基)-n-乙基甘氨酰基]化合物的不吸湿的稳定结晶形式
WO1999019294A1 (en) * 1997-05-14 1999-04-22 Aventis Pharmaceuticals Products Inc. Legal/Patents Process for the preparation of azacycloalkylalkanoyl pseudotetrapeptides
JP2001519411A (ja) * 1997-10-10 2001-10-23 アヴェンティス ファーマシューティカルズ プロダクツ インコーポレイテッド アザシクロアルキルアルカノイルプソイドテトラぺプチドの調製方法
EP1155033A1 (en) * 1998-12-30 2001-11-21 Aventis Pharmaceuticals Products Inc. Process for preparing a stable non-hygroscopic crystalline n-[n-[n-(piperdin-4-yl)butanoyl)-n-ethylglycyl]-(l)-aspartyl]-ss-cyclohexylalanine amide
US7200838B2 (en) * 2000-12-20 2007-04-03 National Instruments Corporation System and method for automatically generating a graphical program in response to a state diagram
US7544681B2 (en) 2001-09-27 2009-06-09 Ramot At Tel Aviv University Ltd. Conjugated psychotropic drugs and uses thereof
ES2400772T3 (es) * 2005-06-07 2013-04-12 Ramot At Tel Aviv University Ltd. Sales novedosas de fármacos psicotrópicos conjugados y procedimientos para la preparación de las mismas
EP2051735B1 (en) 2006-07-17 2012-08-29 Ramot, at Tel Aviv University Ltd. Conjugates comprising a psychotropic drug or a gaba agonist and an organic acid and their use treating pain and other cns disorders
WO2009101616A1 (en) 2008-02-11 2009-08-20 Ramot At Tel Aviv University Ltd. Novel conjugates for treating neurodegenerative diseases and disorders
WO2011070579A1 (en) 2009-12-09 2011-06-16 Biolinerx Ltd. Methods of improving cognitive functions
US8377929B2 (en) 2010-02-24 2013-02-19 Ramot At Tel-Aviv University Ltd. Crystalline forms of the tri-mesylate salt of perphenazine-GABA and process of producing the same
WO2012038963A1 (en) 2010-09-22 2012-03-29 Ramot At Tel-Aviv University Ltd. An acid addition salt of a nortriptyline-gaba conjugate and a process of preparing same

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3821188A (en) * 1972-06-14 1974-06-28 American Home Prod Proline and pyroglutamic acid containing tripeptides
GB8600263D0 (en) * 1985-01-22 1986-02-12 Ici America Inc Peptide derivatives
US4683291A (en) * 1985-10-28 1987-07-28 Scripps Clinic And Research Foundation Platelet binding inhibitors
FR2608160B1 (fr) * 1986-12-15 1989-03-31 Inst Nat Sante Rech Med Nouveaux derives peptidiques et leur application notamment en therapeutique
US4857508A (en) * 1987-12-03 1989-08-15 Monsanto Company Novel platelet-aggregation inhibitor peptide derivatives
US4879313A (en) * 1988-07-20 1989-11-07 Mosanto Company Novel platelet-aggregation inhibitors
US4992463A (en) * 1988-07-20 1991-02-12 Monsanto Company Thienyl peptide mimetic compounds which are useful in inhibiting platelet aggregation
US5037808A (en) * 1988-07-20 1991-08-06 Monsanto Co. Indolyl platelet-aggregation inhibitors
US5023233A (en) * 1989-07-28 1991-06-11 Merck & Co., Inc. Fibrinogen receptor antagonists
US4952562A (en) * 1989-09-29 1990-08-28 Rorer Pharmaceutical Corporation Anti-thrombotic peptides and pseudopeptides
AU646411B2 (en) * 1989-09-29 1994-02-24 Rhone-Poulenc Rorer International (Holdings) Inc. Anti-thrombotic peptides and pseudopeptides
US5051405A (en) * 1989-10-10 1991-09-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Anti-thrombotic peptides and pseudopeptides
US5053392A (en) * 1989-12-01 1991-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Novel arginine, glycine, aspartic acid derivatives as platelet-aggregation inhibitors
US5086069A (en) * 1990-02-05 1992-02-04 Rorer Pharmaceutical Corporation Anti-thrombotic peptide and pseudopeptide derivatives
CA2037153A1 (en) * 1990-03-09 1991-09-10 Leo Alig Acetic acid derivatives
GB9007751D0 (en) * 1990-04-05 1990-06-06 Ciba Geigy Ag Novel platelet-aggregation inhibitors
US5064814A (en) * 1990-04-05 1991-11-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Anti-thrombotic peptide and pseudopeptide derivatives
NZ239876A (en) * 1990-09-27 1993-12-23 Merck & Co Inc Glycyl-b-alanine derivatives and pharmaceutical compositions thereof.
IL99539A0 (en) * 1990-09-27 1992-08-18 Merck & Co Inc Fibrinogen receptor antagonists and pharmaceutical compositions containing them
MX9201416A (es) * 1991-03-28 1992-10-01 Rhone Poulenc Rorer Int Peptidos y pseudopeptidos antitromboticos.
WO1992018117A1 (en) * 1991-04-11 1992-10-29 Rhone-Poulenc Rorer International (Holdings), Inc. Anti-thrombotic peptide and pseudopeptide derivatives
DE69213546T2 (de) * 1991-05-13 1997-02-27 Fujisawa Pharmaceutical Co Neue Peptid-Verbindungen und Verfahren zur Herstellung davon
HU222248B1 (hu) * 1993-10-15 2003-05-28 Aventis Pharmaceuticals Inc. Trombózis elleni hatású (aza-cikloalkil)-alkanoil-peptidek, -pszeudopeptidek és ezeket a vegyületeket tartalmazó gyógyászati készítmények

Also Published As

Publication number Publication date
WO1998017678A1 (en) 1998-04-30
CA2263732A1 (en) 1998-04-30
JP2001501965A (ja) 2001-02-13
AU722112B2 (en) 2000-07-20
AP9901452A0 (en) 1999-03-31
EA001391B1 (ru) 2001-02-26
EP0929572A4 (en) 2001-09-12
IL128556A0 (en) 2000-01-31
BR9711205A (pt) 1999-08-17
US5780590A (en) 1998-07-14
NO990836L (no) 1999-04-20
NZ334059A (en) 2000-01-28
PL331713A1 (en) 1999-08-02
EP0929572A1 (en) 1999-07-21
OA10975A (en) 2001-11-01
AP904A (en) 2000-11-24
BG103197A (en) 2000-05-31
AU4074997A (en) 1998-05-15
UA48252C2 (uk) 2002-08-15
KR20000035797A (ko) 2000-06-26
SK14699A3 (en) 2000-11-07
ZA977511B (en) 1998-03-03
NO990836D0 (no) 1999-02-22
HUP9903961A3 (en) 2000-12-28
EA199900216A1 (ru) 1999-08-26
CN1231671A (zh) 1999-10-13

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