WO1988003927A3 - Inhibiteurs de la renine - Google Patents

Inhibiteurs de la renine Download PDF

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Publication number
WO1988003927A3
WO1988003927A3 PCT/US1987/002820 US8702820W WO8803927A3 WO 1988003927 A3 WO1988003927 A3 WO 1988003927A3 US 8702820 W US8702820 W US 8702820W WO 8803927 A3 WO8803927 A3 WO 8803927A3
Authority
WO
WIPO (PCT)
Prior art keywords
novel
renin inhibitors
renin
intermediates
treating
Prior art date
Application number
PCT/US1987/002820
Other languages
English (en)
Other versions
WO1988003927A2 (fr
Inventor
James P Hudspeth
James S Kaltenbronn
Elizabeth A Lunney
Joseph T Repine
W Howard Roark
Michael A Stier
Francis J Tinney
Peter W K Woo
Ernest D Nicolaides
Original Assignee
Warner Lambert Co
James P Hudspeth
James S Kaltenbronn
Elizabeth A Lunney
Joseph T Repine
W Howard Roark
Michael A Stier
Francis J Tinney
Peter W K Woo
Ernest D Nicolaides
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 Warner Lambert Co, James P Hudspeth, James S Kaltenbronn, Elizabeth A Lunney, Joseph T Repine, W Howard Roark, Michael A Stier, Francis J Tinney, Peter W K Woo, Ernest D Nicolaides filed Critical Warner Lambert Co
Publication of WO1988003927A2 publication Critical patent/WO1988003927A2/fr
Publication of WO1988003927A3 publication Critical patent/WO1988003927A3/fr

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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0227—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the (partial) peptide sequence -Phe-His-NH-(X)2-C(=0)-, e.g. Renin-inhibitors with n = 2 - 6; for n > 6 see C07K5/06 - C07K5/10
    • 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
    • C07K5/0205—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)3-C(=0)-, e.g. statine or derivatives thereof
    • 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
    • C07K5/0207—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)4-C(=0), e.g. 'isosters', replacing two amino acids
    • 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
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S530/00—Chemistry: natural resins or derivatives; peptides or proteins; lignins or reaction products thereof
    • Y10S530/86—Renin inhibitors
    • 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
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S930/00—Peptide or protein sequence
    • Y10S930/01—Peptide or protein sequence
    • Y10S930/27—Cyclic peptide or cyclic protein

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Des nouveaux peptides inhibiteurs de la rénine sont utiles pour traiter l'hypertension associée à la rénine et pour traiter l'hyperaldostéronisme. De nouveaux intermédiaires, des procédés de préparation à la fois des intermédiaires et des nouveaux peptides, des compositions pharmaceutiques et des méthodes de traitement sont également décrits.
PCT/US1987/002820 1986-11-21 1987-10-21 Inhibiteurs de la renine WO1988003927A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US920,330 1986-11-21
US06/920,330 US4743585A (en) 1986-11-21 1986-11-21 Renin inhibitors

Publications (2)

Publication Number Publication Date
WO1988003927A2 WO1988003927A2 (fr) 1988-06-02
WO1988003927A3 true WO1988003927A3 (fr) 1988-08-11

Family

ID=25443569

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1987/002820 WO1988003927A2 (fr) 1986-11-21 1987-10-21 Inhibiteurs de la renine

Country Status (4)

Country Link
US (1) US4743585A (fr)
AU (1) AU8336187A (fr)
GR (1) GR871770B (fr)
WO (1) WO1988003927A2 (fr)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4826958A (en) * 1984-12-14 1989-05-02 Abbott Laboratories Renin inhibiting compounds
MY103189A (en) * 1986-10-31 1993-05-29 Pfizer Nor-statine and nor-cyclostatine polypeptides
US4977141A (en) * 1987-10-01 1990-12-11 G. D. Searle & Co. Peptidyl α-aminoacyl aminodiol carbamates as anti-hypertensive agents
ATE107658T1 (de) * 1988-01-26 1994-07-15 Sankyo Co Renin inhibierende polypeptide, ihre herstellung und anwendung.
US5114937A (en) * 1989-11-28 1992-05-19 Warner-Lambert Company Renin inhibiting nonpeptides
NZ249022A (en) * 1992-02-13 1996-06-25 Warner Lambert Co Preparation of (-)-(s)- and (+)-(r)- ethyl (5-amino-1,2-dihydro-2-methyl-3-phenyl-pyrido[3,4-b]pyrazin-7 -yl) carbamate; pyridyl amino hydroxamic acid precursors
US5455271A (en) * 1992-06-18 1995-10-03 The Scripps Research Institute Tight-binding inhibitors of leukotriene A4 hydrolase
US20080207527A1 (en) * 2004-09-17 2008-08-28 Comentis, Inc. Bicyclic Compounds Which Inhibit Beta-Secretase Activity and Methods of Use Thereof
KR20080015079A (ko) 2005-04-08 2008-02-18 코멘티스, 인코포레이티드 베타 세크레타제 활성을 억제하는 화합물 및 이것의 사용방법
EP1913017A1 (fr) * 2005-08-03 2008-04-23 Boehringer Ingelheim International GmbH Ethane-1,2-diamines substitues pour le traitement de la maladie d'alzheimer ii
CA2814905A1 (fr) * 2010-10-29 2012-05-03 Merz Pharma Gmbh & Co. Kgaa Derives d'indole et procede pour leur preparation
JP6430936B2 (ja) * 2012-07-24 2018-11-28 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ 関節症の処置のためのヒドロキシスタチン誘導体

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0104964A1 (fr) * 1982-08-17 1984-04-04 Sanofi S.A. Dérivés peptidiques inhibiteurs de protéases acides
WO1984003044A1 (fr) * 1983-02-07 1984-08-16 Ferring Ab Inhibiteurs enzymatiques
EP0163237A2 (fr) * 1984-05-29 1985-12-04 Merck & Co. Inc. Inhibiteurs di- et tri-peptidiques de la rénine
EP0173481A2 (fr) * 1984-08-06 1986-03-05 The Upjohn Company Peptides
EP0179352A2 (fr) * 1984-10-20 1986-04-30 MERCK PATENT GmbH Peptides
WO1987005302A2 (fr) * 1986-02-27 1987-09-11 Upjohn Co Nouveaux peptides inhibiteurs de la renine possedant un segment d'insertion a l'etat de transition a base d'un isostere de dihydroxyethylene

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO812612L (no) * 1980-08-06 1982-02-08 Ferring Pharma Ltd Enzym-inhibitorer.
US4609643A (en) * 1980-08-06 1986-09-02 Aktiebolaget Hassle Renin inhibitors, treatments and dipeptide synthesis
US4478826A (en) * 1981-10-08 1984-10-23 Merck & Co., Inc. Renin inhibitory peptides
US4384994A (en) * 1981-10-08 1983-05-24 Merck & Co., Inc. Renin inhibitory peptides
US4470971A (en) * 1981-10-19 1984-09-11 Merck & Co., Inc. Renin inhibitory peptides having His13
US4479941A (en) * 1981-12-10 1984-10-30 Merck & Co., Inc. Renin inhibitory peptides having PHE13 delection
DE3320746A1 (de) * 1982-06-17 1983-12-22 Sandoz-Patent-GmbH, 7850 Lörrach Benzolderivate, ihre herstellung und pharmazeutische praeparate welche sie enthalten
US4650661A (en) * 1982-09-15 1987-03-17 Aktiebolaget Hassle Enzyme inhibitors
US4595677A (en) * 1982-12-03 1986-06-17 Ciba-Geigy Corporation Substituted tetrapeptides
US4668770A (en) * 1982-12-27 1987-05-26 Merck & Co., Inc. Renin inhibitory tripeptides
JPS59227851A (ja) * 1983-06-09 1984-12-21 Sankyo Co Ltd レニン阻害作用を有するペプチド類
US4485099A (en) * 1983-06-15 1984-11-27 Merck & Co., Inc. Renin inhibitors containing a C-terminal amide cycle
US4477440A (en) * 1983-09-14 1984-10-16 Merck & Co., Inc. Renin inhibitors containing an n-terminal disulfide cycle
US4477441A (en) * 1983-09-14 1984-10-16 Merck & Co., Inc. Renin inhibitors containing a C-terminal disulfide cycle
US4661473A (en) * 1984-03-27 1987-04-28 Merck & Co., Inc. Renin inhibitors containing peptide isosteres
US4636491A (en) * 1984-03-27 1987-01-13 Merck & Co., Inc. Renin inhibitory peptides having improved solubility
US4665052A (en) * 1984-03-27 1987-05-12 Merck & Co., Inc. Renin inhibitors containing homophe8 and a C-terminal amide cycle
US4668663A (en) * 1984-03-27 1987-05-26 Merck & Co., Inc. Renin inhibitors containing homophe8
US4663310A (en) * 1984-04-04 1987-05-05 Merck & Co., Inc. Renin inhibitors containing 2-substituted statine
US4618600A (en) * 1984-04-19 1986-10-21 Biotechnology Research Associates, J.V. Novel polypeptide diuretic/vasodilators
US4652551A (en) * 1984-06-22 1987-03-24 Abbott Laboratories Renin inhibiting compounds
US4629724A (en) * 1984-12-03 1986-12-16 E. R. Squibb & Sons, Inc. Amino acid ester and amide renin inhibitors
US4609641A (en) * 1984-12-03 1986-09-02 Merck & Co., Inc. Renin-inhibitory peptide analogs
US4665193A (en) * 1984-12-14 1987-05-12 E. R. Squibb & Sons, Inc. Amino acid ester renin inhibitors
US4665055A (en) * 1985-06-17 1987-05-12 Merck & Co., Inc. Peptide renin inhibitors
US4668769A (en) * 1985-08-02 1987-05-26 Hoover Dennis J Oxa- and azahomocyclostatine polypeptides

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0104964A1 (fr) * 1982-08-17 1984-04-04 Sanofi S.A. Dérivés peptidiques inhibiteurs de protéases acides
WO1984003044A1 (fr) * 1983-02-07 1984-08-16 Ferring Ab Inhibiteurs enzymatiques
EP0163237A2 (fr) * 1984-05-29 1985-12-04 Merck & Co. Inc. Inhibiteurs di- et tri-peptidiques de la rénine
EP0173481A2 (fr) * 1984-08-06 1986-03-05 The Upjohn Company Peptides
EP0179352A2 (fr) * 1984-10-20 1986-04-30 MERCK PATENT GmbH Peptides
WO1987005302A2 (fr) * 1986-02-27 1987-09-11 Upjohn Co Nouveaux peptides inhibiteurs de la renine possedant un segment d'insertion a l'etat de transition a base d'un isostere de dihydroxyethylene

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
Chemical Abstracts, vol. 101, 1984, (American Chemical Society, Columbus, Ohio, US), R.L. Johnson: "Synthesis of epoxypolypeptides as inhibitors of renin", see page 278, abstract no. 68311m, Pept.: Struct. Funct., Proc. Am. Pept. Symp., 8th 1983, 587-90 *
Peptides, Structure & Function, Proceedings of the American Peptide Symposium, 9th Proceeding, 1985 (C.M. Deber et al., Pierce Chemical Co., Rockford, US), G. Precigoux et al.: "crystallographic analysis of a pepstatin analogue: BOC"LEU=LEU"-STA-ALA-STA-Ome", pages 763-766 *
Peptides, Structure & Function, Proceedings of the American Peptide Symposium, 9th Proceeding, 1985, (C.M. Deber et al., Pierce Chemical Co., Rockford, US), B.E. Evans et al.: "A stereocontrolled synthesis of hydroxyethylene dipeptide isosteres using novel, chiral amino-alkyl epoxides; new renin inhibitor analogs", pages 743-746 *
Progress in Drug Research, vol. 31, 1987, (Ernst Jucker, Birkhauser Verlag, Basel, CH), M.J. Antonaccio et al.: "Enzyme inhibitors of the renin-angiotensin system", see pages 161-189 *
The Journal of Organic Chemistry, vol. 50, no. 25, 13 December 1985 (The American Chemical Society, US), G.J. Hanson et al.: "Synthesis of new dipeptide analogues containing novel ketovinyl and hydroxyethylidene isosteres via Grignard addition to addition to chiral alpha-amino aldehydes", pages 5399-5401 *

Also Published As

Publication number Publication date
GR871770B (en) 1988-03-17
AU8336187A (en) 1988-06-16
WO1988003927A2 (fr) 1988-06-02
US4743585A (en) 1988-05-10

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