ES2161759T3 - Derivados de profarmacos de inhibidores de enzimas con grupos hidroxilo, procedimiento para su preparacion y su utilizacion. - Google Patents
Derivados de profarmacos de inhibidores de enzimas con grupos hidroxilo, procedimiento para su preparacion y su utilizacion.Info
- Publication number
- ES2161759T3 ES2161759T3 ES94909071T ES94909071T ES2161759T3 ES 2161759 T3 ES2161759 T3 ES 2161759T3 ES 94909071 T ES94909071 T ES 94909071T ES 94909071 T ES94909071 T ES 94909071T ES 2161759 T3 ES2161759 T3 ES 2161759T3
- Authority
- ES
- Spain
- Prior art keywords
- pct
- projects
- derivatives
- procedure
- preparation
- 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
- 102000004190 Enzymes Human genes 0.000 title 1
- 108090000790 Enzymes Proteins 0.000 title 1
- -1 HYDROXYL GROUPS Chemical group 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000002532 enzyme inhibitor Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 229940125532 enzyme inhibitor Drugs 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 1
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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
- C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
- C07C323/52—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/50—Organo-phosphines
- C07F9/53—Organo-phosphine oxides; Organo-phosphine thioxides
- C07F9/5304—Acyclic saturated phosphine oxides or thioxides
-
- 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
-
- 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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Crystallography & Structural Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Saccharide Compounds (AREA)
- Steroid Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Quinoline Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
LA INVENCION SE REFIERE A MEDICAMENTOS DE INHIBIDORES DE ENZIMA DONDE AL MENOS UN GRUPO OH HA SIDO CONVERTIDO EN EL INHIBIDOR DE ENZIMA EN UN DERIVADO POR MEDIO DE UNA AGRUPACION DE LA FORMULA (III HASTA V) EN DONDE LOS GRUPOS R{SUP,11} HASTA R{SUP,25} Y S,L,M,O,Q Y R SE DEFINEN COMO EN LA DESCRIPCION. TALES MEDICAMENTOS EXHIBEN UNA SOLUBILIDAD MEJORA EN AGUA Y CARACTERISTICAS FARMACOCINETICAS MEJORADAS.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4308096A DE4308096A1 (de) | 1993-03-13 | 1993-03-13 | Prodrug-Derivate von Enzyminhibitoren mit Hydroxylgruppen, Verfahren zu deren Herstellung und ihre Verwendung |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2161759T3 true ES2161759T3 (es) | 2001-12-16 |
Family
ID=6482773
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES94909071T Expired - Lifetime ES2161759T3 (es) | 1993-03-13 | 1994-02-25 | Derivados de profarmacos de inhibidores de enzimas con grupos hidroxilo, procedimiento para su preparacion y su utilizacion. |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US5804559A (es) |
| EP (1) | EP0688314B1 (es) |
| JP (1) | JPH08507770A (es) |
| AT (1) | ATE206393T1 (es) |
| AU (1) | AU6207094A (es) |
| DE (2) | DE4308096A1 (es) |
| DK (1) | DK0688314T3 (es) |
| ES (1) | ES2161759T3 (es) |
| PT (1) | PT688314E (es) |
| WO (1) | WO1994021604A1 (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5753652A (en) * | 1991-07-03 | 1998-05-19 | Novartis Corporation | Antiretroviral hydrazine derivatives |
| US5643878A (en) * | 1991-09-12 | 1997-07-01 | Ciba-Geigy Corporation | 5-amino-4-hydroxyhexanoic acid derivatives |
| MXPA93002392A (es) | 1992-03-11 | 2005-02-04 | Narhex Ltd | Derivados amino de hidrocarburos-oxo e hidroxi-substituidos. |
| EP1302468B1 (en) * | 1992-12-29 | 2008-12-17 | Abbott Laboratories | Processes and intermediates for manufacturing retroviral protease inhibiting compounds |
| IL110898A0 (en) * | 1993-09-10 | 1994-11-28 | Narhex Australia Pty Ltd | Polar-substituted hydrocarbons |
| AU2012199A (en) * | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| AU2004233898B2 (en) | 2003-04-25 | 2010-12-23 | Gilead Sciences, Inc. | Antiviral phosphonate analogs |
| EP1656387A2 (en) | 2003-07-30 | 2006-05-17 | Gilead Sciences, Inc. | Nucleobase phosphonate analogs for antiviral treatment |
| ES2363160T3 (es) | 2004-07-27 | 2011-07-22 | Gilead Sciences, Inc. | Conjugados de fosfonato nucelosidico como agentes anti-vih. |
| BRPI0713961A2 (pt) | 2006-07-07 | 2012-11-27 | Gilead Sciences Inc | compostos fosfinatos antivirais |
| TWI444384B (zh) | 2008-02-20 | 2014-07-11 | Gilead Sciences Inc | 核苷酸類似物及其在治療惡性腫瘤上的用途 |
| JP5620376B2 (ja) | 2008-07-08 | 2014-11-05 | ギリアード サイエンシーズ, インコーポレイテッド | Hiv阻害剤化合物の塩 |
| HK1205697A1 (zh) * | 2012-04-25 | 2015-12-24 | Ascendis Pharma A/S | 含有羟基的药物的前药 |
| US9765022B2 (en) * | 2013-02-28 | 2017-09-19 | Tufts University | Disulfide compounds for delivery of pharmaceutical agents |
| ES2892402T3 (es) | 2017-08-01 | 2022-02-04 | Gilead Sciences Inc | Formas cristalinas de ((S)-((((2R,5R)-5-(6-amino-9H-purin-9-il)-4-fluoro-2,5-dihidrofuran-2-il)oxi)metil)(fenoxi)fosforil)-L-alaninato de etilo para tratar infecciones virales |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0428849A3 (en) * | 1989-09-28 | 1991-07-31 | Hoechst Aktiengesellschaft | Retroviral protease inhibitors |
| AU1677092A (en) * | 1991-03-20 | 1992-10-21 | Vertex Pharmaceuticals Incorporated | Tetrahydroxyalkane derivatives as inhibitors of hiv aspartyl protease |
-
1993
- 1993-03-13 DE DE4308096A patent/DE4308096A1/de not_active Withdrawn
-
1994
- 1994-02-25 WO PCT/EP1994/000561 patent/WO1994021604A1/de not_active Ceased
- 1994-02-25 JP JP6520566A patent/JPH08507770A/ja not_active Ceased
- 1994-02-25 EP EP94909071A patent/EP0688314B1/de not_active Expired - Lifetime
- 1994-02-25 PT PT94909071T patent/PT688314E/pt unknown
- 1994-02-25 ES ES94909071T patent/ES2161759T3/es not_active Expired - Lifetime
- 1994-02-25 DK DK94909071T patent/DK0688314T3/da active
- 1994-02-25 AT AT94909071T patent/ATE206393T1/de not_active IP Right Cessation
- 1994-02-25 AU AU62070/94A patent/AU6207094A/en not_active Abandoned
- 1994-02-25 DE DE59409894T patent/DE59409894D1/de not_active Expired - Lifetime
- 1994-02-25 US US08/525,525 patent/US5804559A/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| AU6207094A (en) | 1994-10-11 |
| ATE206393T1 (de) | 2001-10-15 |
| DE59409894D1 (de) | 2001-11-08 |
| EP0688314B1 (de) | 2001-10-04 |
| PT688314E (pt) | 2002-03-28 |
| EP0688314A1 (de) | 1995-12-27 |
| JPH08507770A (ja) | 1996-08-20 |
| DE4308096A1 (de) | 1994-09-15 |
| WO1994021604A1 (de) | 1994-09-29 |
| DK0688314T3 (da) | 2001-12-10 |
| US5804559A (en) | 1998-09-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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