ES2177816T3 - Derivados de azahexano como isosteros de sustrato de aspartato proteasas retroviricas. - Google Patents
Derivados de azahexano como isosteros de sustrato de aspartato proteasas retroviricas.Info
- Publication number
- ES2177816T3 ES2177816T3 ES96939024T ES96939024T ES2177816T3 ES 2177816 T3 ES2177816 T3 ES 2177816T3 ES 96939024 T ES96939024 T ES 96939024T ES 96939024 T ES96939024 T ES 96939024T ES 2177816 T3 ES2177816 T3 ES 2177816T3
- Authority
- ES
- Spain
- Prior art keywords
- retroviricas
- proteasas
- isosteros
- azahexano
- aspartato
- 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
- 239000000758 substrate Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 101000898643 Candida albicans Vacuolar aspartic protease Proteins 0.000 abstract 1
- 101000898783 Candida tropicalis Candidapepsin Proteins 0.000 abstract 1
- 101000898784 Cryphonectria parasitica Endothiapepsin Proteins 0.000 abstract 1
- 101000933133 Rhizopus niveus Rhizopuspepsin-1 Proteins 0.000 abstract 1
- 101000910082 Rhizopus niveus Rhizopuspepsin-2 Proteins 0.000 abstract 1
- 101000910079 Rhizopus niveus Rhizopuspepsin-3 Proteins 0.000 abstract 1
- 101000910086 Rhizopus niveus Rhizopuspepsin-4 Proteins 0.000 abstract 1
- 101000910088 Rhizopus niveus Rhizopuspepsin-5 Proteins 0.000 abstract 1
- 101000898773 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) Saccharopepsin Proteins 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004802 cyanophenyl group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000001177 retroviral effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C271/06—Esters of carbamic acids
- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
-
- 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
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Enzymes And Modification Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Helmets And Other Head Coverings (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Prostheses (AREA)
Abstract
LA INVENCION SE REFIERE A COMPUESTOS DE FORMULA (I); DONDE R 1 Y R 10 SON, CADA UNO INDEPENDIENTEMENTE DEL OTRO, ALCOXICARBONILO INFERIOR; R 2 , R 3 O R 4 SON, CADA UNO INDEPENDIENTEMENTE DEL RESTO, ALQUILO C 1 - C SUB,4 Y R 7 , R 8 Y R 9 SE SELECCIONAN CADA UNO INDEPENDIENTEMENTE A PARTIR DE HIROGENO Y ALQUILO C 1 C SUB,4 , SIENDO NO MAS DE DOS RADICALES HIDROGENO; O R 7 , R 8 Y R 9 SON, CADA UNO INDEPENDIENTEMENTE DEL OTRO, ALQUILO C 1 - C 4 Y R 2 , R 3 Y R 4 SE SELECCIONAN CADA UNO A PARTIR DE HIDROGENO Y ALQUILO C 1 C 4 , SIENDO 1 O 2 DE LOS RADICALES HIDROGENO; R 5 ES FENILO O CICLOHEXILO; Y R 6 ES FENILO O CIANOFENILO; O LAS SALES DE LOS MISMOS. DICHOS COMPUESTOS SON INHIBIDORES DE LAS PROTEASAS DE ASPARTATO VIRALES Y SON EFECTIVOS, POR EJEMPLO, FRENTE AL VIH.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH329695 | 1995-11-21 | ||
| CH168696 | 1996-07-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2177816T3 true ES2177816T3 (es) | 2002-12-16 |
Family
ID=25688382
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES96939024T Expired - Lifetime ES2177816T3 (es) | 1995-11-21 | 1996-11-13 | Derivados de azahexano como isosteros de sustrato de aspartato proteasas retroviricas. |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US6225345B1 (es) |
| EP (1) | EP0876336B1 (es) |
| JP (1) | JPH11514996A (es) |
| AT (1) | ATE218538T1 (es) |
| AU (1) | AU7623796A (es) |
| CA (1) | CA2237016A1 (es) |
| DE (1) | DE69621651T2 (es) |
| ES (1) | ES2177816T3 (es) |
| WO (1) | WO1997019055A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1997046514A1 (en) * | 1996-05-31 | 1997-12-11 | Novartis Ag | Process for the preparation of hydrazine derivatives useful as intermediates for the preparation of peptide analogues |
| PT2336134T (pt) | 1998-06-23 | 2016-10-19 | The Board Of Trustees Of The Univ Of Illionis | Ensaio de aptidão e métodos para reduzir a resistência do hiv à terapia |
| WO1999067254A2 (en) * | 1998-06-23 | 1999-12-29 | The United States Of America Represented By The Secretary, Department Of Health And Human Services | Multi-drug resistant retroviral protease inhibitors and use thereof |
| EP1299352B1 (en) * | 2000-06-30 | 2005-12-28 | Elan Pharmaceuticals, Inc. | Compounds to treat alzheimer's disease |
| CA2448084A1 (en) * | 2001-05-22 | 2002-11-28 | Elan Pharmaceuticals, Inc. | Aza hydroxylated ethyl amine compounds |
| US7157489B2 (en) | 2002-03-12 | 2007-01-02 | The Board Of Trustees Of The University Of Illinois | HIV protease inhibitors |
| CA2549228C (en) * | 2003-12-11 | 2013-03-19 | Abbott Laboratories | Hiv protease inhibiting compounds |
| ATE539074T1 (de) * | 2003-12-11 | 2012-01-15 | Abbott Lab | Die hiv-protease hemmende verbindungen |
| US7713885B2 (en) * | 2005-05-11 | 2010-05-11 | Micron Technology, Inc. | Methods of etching oxide, reducing roughness, and forming capacitor constructions |
| JP5599611B2 (ja) | 2006-07-21 | 2014-10-01 | ギリアード サイエンシーズ， インコーポレイテッド | 抗ウイルスプロテアーゼインヒビター |
| WO2011080562A1 (en) | 2009-12-29 | 2011-07-07 | Hetero Research Foundation | Novel aza-peptides containing 2,2-disubstituted cyclobutyl and/or substituted alkoxy benzyl derivatives as antivirals |
| UY37592A (es) | 2017-02-06 | 2018-08-31 | Gilead Sciences Inc | Compuestos inhibidores del vih |
| TWI829205B (zh) | 2018-07-30 | 2024-01-11 | 美商基利科學股份有限公司 | 抗hiv化合物 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL89900A0 (en) * | 1988-04-12 | 1989-12-15 | Merck & Co Inc | Hiv protease inhibitors useful for the treatment of aids and pharmaceutical compositions containing them |
| ES2093237T3 (es) | 1991-07-03 | 1996-12-16 | Ciba Geigy Ag | Derivados de hidrazina farmacologicamente activos y procedimiento para su obtencion. |
| ES2093394T3 (es) | 1992-12-23 | 1996-12-16 | Ciba Geigy Ag | Derivados de hidrazina antiretrovirales. |
| US5461067A (en) | 1993-02-25 | 1995-10-24 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US5538997A (en) * | 1993-03-12 | 1996-07-23 | Sandoz Ltd. | 2,4-diamino-3-hydroxycarboxylic acid derivatives |
-
1996
- 1996-11-13 DE DE69621651T patent/DE69621651T2/de not_active Expired - Fee Related
- 1996-11-13 EP EP96939024A patent/EP0876336B1/en not_active Expired - Lifetime
- 1996-11-13 JP JP9514529A patent/JPH11514996A/ja not_active Ceased
- 1996-11-13 AT AT96939024T patent/ATE218538T1/de not_active IP Right Cessation
- 1996-11-13 US US09/068,876 patent/US6225345B1/en not_active Expired - Fee Related
- 1996-11-13 WO PCT/EP1996/004968 patent/WO1997019055A1/en not_active Ceased
- 1996-11-13 CA CA002237016A patent/CA2237016A1/en not_active Abandoned
- 1996-11-13 AU AU76237/96A patent/AU7623796A/en not_active Abandoned
- 1996-11-13 ES ES96939024T patent/ES2177816T3/es not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| EP0876336A1 (en) | 1998-11-11 |
| AU7623796A (en) | 1997-06-11 |
| DE69621651D1 (de) | 2002-07-11 |
| ATE218538T1 (de) | 2002-06-15 |
| WO1997019055A1 (en) | 1997-05-29 |
| US6225345B1 (en) | 2001-05-01 |
| EP0876336B1 (en) | 2002-06-05 |
| JPH11514996A (ja) | 1999-12-21 |
| DE69621651T2 (de) | 2002-11-21 |
| CA2237016A1 (en) | 1997-05-29 |
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