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WO1990012804A3 - Peptides having novel polar n-terminal groups - Google Patents

Peptides having novel polar n-terminal groups Download PDF

Info

Publication number
WO1990012804A3
WO1990012804A3 PCT/US1990/001764 US9001764W WO9012804A3 WO 1990012804 A3 WO1990012804 A3 WO 1990012804A3 US 9001764 W US9001764 W US 9001764W WO 9012804 A3 WO9012804 A3 WO 9012804A3
Authority
WO
WIPO (PCT)
Prior art keywords
renin
inhibitors
peptides
useful
dependent
Prior art date
Application number
PCT/US1990/001764
Other languages
French (fr)
Other versions
WO1990012804A2 (en
Inventor
Suvit Thaisrivongs
Original Assignee
Upjohn Co
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 Upjohn Co filed Critical Upjohn Co
Priority to KR1019900702636A priority Critical patent/KR920700221A/en
Publication of WO1990012804A2 publication Critical patent/WO1990012804A2/en
Publication of WO1990012804A3 publication Critical patent/WO1990012804A3/en

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
    • 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
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P9/12—Antihypertensives

Landscapes

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

Abstract

The present invention provides novel peptides having a non-cleavable transition state insert corresponding to the 10,11-position of the renin substrate (angiotensinogen) and having a novel polar group of formula (L1) (wherein X1 is H2N-, H2NC(CH3)2-, HO2C-, (H2N)(HO2C)CH-, or (HO)2P(O)O-) at the N-terminus of the peptide. These peptides are useful as renin inhibitors and as inhibitors of retroviral proteases. Renin inhibitors are useful for the diagnosis and control of renin-dependent hypertension, congestive heart failure, renin-dependent hyperaldosterism, other renin-dependent cardiovascular disorders and ocular disorders. Inhibitors of retroviral proteases, such as the HIV-I protease, are useful for treating diseases caused by retroviruses, such as human acquired immunodeficiency disease syndrome (AIDS).
PCT/US1990/001764 1989-04-18 1990-04-05 Peptides having novel polar n-terminal groups WO1990012804A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1019900702636A KR920700221A (en) 1989-04-18 1990-04-05 Novel Linin Inhibitor Peptides with Polar N-Terminal Groups

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33975089A 1989-04-18 1989-04-18
US339,750 1989-04-18

Publications (2)

Publication Number Publication Date
WO1990012804A2 WO1990012804A2 (en) 1990-11-01
WO1990012804A3 true WO1990012804A3 (en) 1990-11-29

Family

ID=23330419

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1990/001764 WO1990012804A2 (en) 1989-04-18 1990-04-05 Peptides having novel polar n-terminal groups

Country Status (5)

Country Link
EP (1) EP0468998A1 (en)
JP (1) JPH04504716A (en)
KR (1) KR920700221A (en)
AU (1) AU5407190A (en)
WO (1) WO1990012804A2 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5554728A (en) * 1991-07-23 1996-09-10 Nexstar Pharmaceuticals, Inc. Lipid conjugates of therapeutic peptides and protease inhibitors
DE4126485A1 (en) * 1991-08-10 1993-02-11 Bayer Ag TRIFLUOROMETHYL-CONTAINING PSEUDOPEPTIDE
WO1993006127A1 (en) * 1991-09-17 1993-04-01 Warner-Lambert Company Novel amino acid prodrug renin inhibitors
US5888992A (en) * 1992-03-11 1999-03-30 Narhex Limited Polar substituted hydrocarbons
US6071895A (en) * 1992-03-11 2000-06-06 Narhex Limited Polar-substituted hydrocarbons
ATE253050T1 (en) 1992-03-11 2003-11-15 Narhex Ltd AMINE DERIVATIVES OF OXO- AND HYDROXY-SUBSTITUTED HYDROCARBONS
EP0633881B1 (en) * 1992-03-11 2003-10-29 Narhex Limited Amine derivatives of oxo- and hydroxy-substitued hydrocarbons
JPH07501556A (en) * 1992-03-25 1995-02-16 ファイザー・インコーポレーテッド antiviral peptide
DE4215874A1 (en) * 1992-05-14 1993-11-18 Bayer Ag Dithiolanylglycine-containing HIV protease inhibitors of the hydroxyethylene isostear type

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0104041A1 (en) * 1982-09-15 1984-03-28 Aktiebolaget Hässle Enzyme inhibitors
DE3830825A1 (en) * 1987-09-15 1989-03-23 Sandoz Ag Hydrophilic renin inhibitors, their preparation and use
EP0312157A2 (en) * 1987-10-13 1989-04-19 Merck & Co. Inc. Tetrapeptide renin inhibitors having a novel c-terminal amino acid

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0104041A1 (en) * 1982-09-15 1984-03-28 Aktiebolaget Hässle Enzyme inhibitors
DE3830825A1 (en) * 1987-09-15 1989-03-23 Sandoz Ag Hydrophilic renin inhibitors, their preparation and use
EP0312157A2 (en) * 1987-10-13 1989-04-19 Merck & Co. Inc. Tetrapeptide renin inhibitors having a novel c-terminal amino acid

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Peptides - Chemistry and Biology - Proceedings of the Tenth American Peptide Symposium, 23-28 May 1987, St. Louis, Missouri, US, edited by G.R. Marshall, published by ESCOM, (Leiden, NL), D.J. KEMPF et al.: "Renin Inhibitors based on Novel Dipeptide Analogs: Increased Efficacy through Systematic Inclusion of Polar Functionality", pages 474-475 *

Also Published As

Publication number Publication date
WO1990012804A2 (en) 1990-11-01
EP0468998A1 (en) 1992-02-05
JPH04504716A (en) 1992-08-20
KR920700221A (en) 1992-02-19
AU5407190A (en) 1990-11-16

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