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
Links
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;
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)
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)
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 |
JP2848232B2 (ja) * | 1993-02-19 | 1999-01-20 | 武田薬品工業株式会社 | アルデヒド誘導体 |
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 |
-
1993
- 1993-01-04 GB GB939300048A patent/GB9300048D0/en active Pending
-
1994
- 1994-01-03 ZA ZA948A patent/ZA948B/xx unknown
- 1994-01-04 EP EP00201447A patent/EP1029869B1/en not_active Expired - Lifetime
- 1994-01-04 US US08/481,365 patent/US6235717B1/en not_active Expired - Fee Related
- 1994-01-04 JP JP51579694A patent/JP3529381B2/ja not_active Expired - Fee Related
- 1994-01-04 EP EP94903951A patent/EP0677059A1/en not_active Withdrawn
- 1994-01-04 WO PCT/GB1994/000009 patent/WO1994015956A1/en not_active Application Discontinuation
- 1994-01-04 DE DE69432573T patent/DE69432573T2/de not_active Expired - Fee Related
- 1994-01-04 AU AU58202/94A patent/AU5820294A/en not_active Abandoned
- 1994-01-04 ES ES00201447T patent/ES2193919T3/es not_active Expired - Lifetime
- 1994-01-04 AT AT00201447T patent/ATE238343T1/de not_active IP Right Cessation
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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