ES2193919T3 - Inhibidores de la enzima convertidora de endotelina. - Google Patents

Inhibidores de la enzima convertidora de endotelina.

Info

Publication number
ES2193919T3
ES2193919T3 ES00201447T ES00201447T ES2193919T3 ES 2193919 T3 ES2193919 T3 ES 2193919T3 ES 00201447 T ES00201447 T ES 00201447T ES 00201447 T ES00201447 T ES 00201447T ES 2193919 T3 ES2193919 T3 ES 2193919T3
Authority
ES
Spain
Prior art keywords
inhibitors
endoteline
converter enzyme
enzyme
compounds
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES00201447T
Other languages
English (en)
Inventor
Johann Jakob Leban
Douglas Byron Sherman
James Frederick Sigafoos
Andreas Spaltenstein
Osvaldo Humberto Viveros
David Chi-Cheong Wan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Wellcome Foundation Ltd
Original Assignee
Wellcome Foundation Ltd
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 Wellcome Foundation Ltd filed Critical Wellcome Foundation Ltd
Application granted granted Critical
Publication of ES2193919T3 publication Critical patent/ES2193919T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—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)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • 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
    • 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
    • C07K5/06043—Leu-amino acid
    • 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
    • C07K5/06052—Val-amino acid
    • 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
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/06156—Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; 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
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • C07K5/0819—Tripeptides with the first amino acid being acidic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

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

Abstract

Un compuesto de fórmula (I) o una sal del mismo **FORMULA** en el que: R1 es arilo C5-7; arilo C5-7-alquilo C1-7; arilo C5-7-alcoxi C1-4; ariloxi C5-7-alquilo C1-4; carboxialquilo C1-4; alcoxi C1-4-carbonilalquilo C1-4; alquilo C1-4 o difenilalquilo C1-4, estando sustituidos opcionalmente tales grupos arilo o restos arilo o grupos que contienen arilo con alquilo C1-4, halo, nitro, carboxilo o sulfonilo, o R1 es un grupo de fórmula IIa, IIb o IIc: **FORMULA** donde n = 0 ó 1; **FORMULA** donde n = 0 ó 1 y donde Z es -CONH- o -CH2- y R5 es benciloxi; 1, 2, 3, 6-tetrahidro-2, 6-dioxo-4pirimidinilo; o 2, 5-dioxo-4-imidazolidinilo; o **FORMULA** donde R6 es hidrógeno o alquilo C1-4;
ES00201447T 1993-01-04 1994-01-04 Inhibidores de la enzima convertidora de endotelina. Expired - Lifetime ES2193919T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB939300048A GB9300048D0 (en) 1993-01-04 1993-01-04 Endothelin converting enzyme inhibitors

Publications (1)

Publication Number Publication Date
ES2193919T3 true ES2193919T3 (es) 2003-11-16

Family

ID=10728286

Family Applications (1)

Application Number Title Priority Date Filing Date
ES00201447T Expired - Lifetime ES2193919T3 (es) 1993-01-04 1994-01-04 Inhibidores de la enzima convertidora de endotelina.

Country Status (10)

Country Link
US (1) US6235717B1 (es)
EP (2) EP1029869B1 (es)
JP (1) JP3529381B2 (es)
AT (1) ATE238343T1 (es)
AU (1) AU5820294A (es)
DE (1) DE69432573T2 (es)
ES (1) ES2193919T3 (es)
GB (1) GB9300048D0 (es)
WO (1) WO1994015956A1 (es)
ZA (1) ZA948B (es)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU673731B2 (en) * 1993-06-03 1996-11-21 Banyu Pharmaceutical Co., Ltd. Novel endothelin antagonistic peptide
EP0731107A1 (en) * 1995-02-13 1996-09-11 Takeda Chemical Industries, Ltd. Production of aldehyde derivatives
DE19745146A1 (de) * 1997-10-14 1999-04-15 Basf Ag Neue pharmazeutisch wirksame Verbindungen, ihre Herstellung und Verwendung
US6649593B1 (en) * 1999-10-13 2003-11-18 Tularik Inc. Modulators of SREBP processing
AU2001252958A1 (en) * 2000-03-23 2001-10-03 Elan Pharmaceuticals, Inc. Compounds and methods to treat alzheimer's disease
WO2002006280A2 (en) * 2000-07-13 2002-01-24 Millennium Pharamaceuticals, Inc. INHIBITORS OF FACTOR Xa
US7842727B2 (en) * 2001-03-27 2010-11-30 Errant Gene Therapeutics, Llc Histone deacetylase inhibitors
AU2003243272A1 (en) * 2002-05-22 2003-12-12 Errant Gene Therapeutics, Llc Histone deacetylase inhibitors based on alpha-ketoepoxide compounds
EP1511729A4 (en) * 2002-05-22 2006-09-06 Errant Gene Therapeutics Llc HISTONDEACETYLASEINHIBITORS BASED ON ALPHACHALCOGEN METHYL CARBONYL COMPOUNDS
US8198270B2 (en) 2004-04-15 2012-06-12 Onyx Therapeutics, Inc. Compounds for proteasome enzyme inhibition
CN103554222A (zh) 2004-04-15 2014-02-05 欧尼斯治疗公司 用于抑制蛋白酶体酶的化合物
JP5108509B2 (ja) 2004-05-10 2012-12-26 プロテオリックス， インコーポレイテッド 酵素阻害のための化合物
US7531517B2 (en) * 2005-08-10 2009-05-12 4Sc Ag Inhibitors of cancer cell, T-cell and keratinocyte proliferation
EP1752467A1 (en) * 2005-08-10 2007-02-14 4Sc Ag Inhibitors of cancer cell, t-cell and keratinocyte proliferation
NZ595196A (en) 2005-11-09 2013-03-28 Proteolix Inc Peptide-based compounds for enzyme inhibition
PL2041158T3 (pl) * 2006-06-19 2013-08-30 Onyx Therapeutics Inc Peptydowe epoksyketony do hamowania proteasomu
PL2207791T5 (pl) * 2007-10-04 2020-07-27 Onyx Therapeutics, Inc. Krystaliczne peptydo- epoksy ketonowe inhibitory proteazy i synteza keto-epoksydów Aminokwasowych
AP2011005690A0 (en) 2008-10-21 2011-06-30 Onyx Therapeutics Inc Combination therapy with peptide epoxyketones.
TWI504598B (zh) 2009-03-20 2015-10-21 Onyx Therapeutics Inc 結晶性三肽環氧酮蛋白酶抑制劑
JP5919196B2 (ja) 2009-11-13 2016-05-18 オニキス セラピューティクス， インク．Ｏｎｙｘ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． 転移抑制のためのペプチドエポキシケトンの使用
BR112012022060A2 (pt) 2010-03-01 2018-05-08 Onyx Therapeutics Inc composto para a inibição de imunoproteassoma
NZ602872A (en) 2010-04-07 2014-05-30 Onyx Therapeutics Inc Crystalline peptide epoxyketone immunoproteasome inhibitor
JP2015524394A (ja) 2012-07-09 2015-08-24 オニキス セラピューティクス， インク．Ｏｎｙｘ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． ペプチドエポキシケトンプロテアーゼ阻害剤のプロドラッグ

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL90218A0 (en) 1988-05-13 1989-12-15 Abbott Lab Retroviral protease inhibitors
CA2043741C (en) 1990-06-07 2003-04-01 Kiyofumi Ishikawa Endothelin antagonistic peptide derivatives
EP0472077A3 (en) 1990-08-24 1993-03-31 Bayer Ag Phosphonate containing hydroxyethylamin- and norstatin-type pseudopeptides
US5444042A (en) * 1990-12-28 1995-08-22 Cortex Pharmaceuticals Method of treatment of neurodegeneration with calpain inhibitors
US5382569A (en) * 1991-05-16 1995-01-17 Warner-Lambert Company Endotherlin antagonists
JPH05105698A (ja) 1991-06-13 1993-04-27 Takeda Chem Ind Ltd ホスホン酸誘導体、その製造法および用途
US5504070A (en) * 1991-12-05 1996-04-02 Berlex Laboratories, Inc. Inhibitors of the conversion of big endothelin to endothelin
US5610297A (en) * 1991-12-27 1997-03-11 Georgia Tech Research Corp. Peptides ketoamides
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US5607831A (en) * 1993-03-25 1997-03-04 The United States Of America As Represented By The Department Of Health And Human Services In vitro methods for assessing the susceptibility of HIV-1-infected individuals to cysteine protease-mediated activation-induced programmed cell death
WO1994028012A1 (en) * 1993-05-28 1994-12-08 Warner-Lambert Company Hydroxamate inhibitors of endothelin converting enzyme
US5693617A (en) * 1994-03-15 1997-12-02 Proscript, Inc. Inhibitors of the 26s proteolytic complex and the 20s proteasome contained therein

Also Published As

Publication number Publication date
EP1029869B1 (en) 2003-04-23
US6235717B1 (en) 2001-05-22
EP1029869A1 (en) 2000-08-23
JPH08506569A (ja) 1996-07-16
ZA948B (en) 1995-07-03
DE69432573D1 (de) 2003-05-28
JP3529381B2 (ja) 2004-05-24
DE69432573T2 (de) 2004-01-08
AU5820294A (en) 1994-08-15
EP0677059A1 (en) 1995-10-18
GB9300048D0 (en) 1993-03-03
ATE238343T1 (de) 2003-05-15
WO1994015956A1 (en) 1994-07-21

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