ES2066623T3 - Derivados sustituidos del acido pipecolinico como inhibidores de la vih-proteasa. - Google Patents
Derivados sustituidos del acido pipecolinico como inhibidores de la vih-proteasa.Info
- Publication number
- ES2066623T3 ES2066623T3 ES93103712T ES93103712T ES2066623T3 ES 2066623 T3 ES2066623 T3 ES 2066623T3 ES 93103712 T ES93103712 T ES 93103712T ES 93103712 T ES93103712 T ES 93103712T ES 2066623 T3 ES2066623 T3 ES 2066623T3
- Authority
- ES
- Spain
- Prior art keywords
- hiv
- protease inhibitors
- substituted derivatives
- substitute
- pipecolinic acid
- 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
- 239000004030 hiv protease inhibitor Substances 0.000 title 1
- HXEACLLIILLPRG-UHFFFAOYSA-N pipecolic acid Chemical class OC(=O)C1CCCCN1 HXEACLLIILLPRG-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 241000725303 Human immunodeficiency virus Species 0.000 abstract 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 108091005804 Peptidases Proteins 0.000 abstract 1
- 239000004365 Protease Substances 0.000 abstract 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 abstract 1
- QGLZXHRNAYXIBU-UHFFFAOYSA-N aldicarb Chemical compound CNC(=O)ON=CC(C)(C)SC QGLZXHRNAYXIBU-UHFFFAOYSA-N 0.000 abstract 1
- 150000001413 amino acids Chemical group 0.000 abstract 1
- 230000000120 cytopathologic effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
- 210000005260 human cell Anatomy 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 239000002699 waste material Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (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)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
AQUI DENTRO SE PRESENTAN COMPUESTOS DE LA FORMULA 1 EN DONDE X ES UN GRUPO TERMINAL, POR EJEMPLO, UN ARILOXICARBONILO, UN ALCANOILO O UN CARBAMILO OPCIONALMENTE MONO O DISUSTITUIDO; B ESTA AUSENTE O ES UN RESIDUO AMINOACIDO, POR EJEMPLO, VAL O ASN; R1 ES HIDROGENO O UN SUSTITUYENTE EN FORMA DE ANILLO, POR EJEMPLO, FLUORO O METILO; R2 ES ALQUILO; E Y ES UN SUSTITUYENTE EN FORMA DE ANILLO, POR EJEMPLO, FENOXI, 2PIRIDINILMETOXI, FENILTIO O 2-PIRIDINILTIO. LOS COMPUESTOS INHIBEN LA ACTIVIDAD DE LA PROTEASA DEL VIRUS DE INMUNODEFICIENCIA HUMANA (VIH) E INTERFIEREN EN LOS EFECTOS CITOPATOGENICOS INDUCIDOS POR EL VI EN LAS CELULAS HUMANAS. ESTAS PROPIEDADES HACEN QUE LOS COMPUESTOS SEAN UTILES PARA COMBATIR LAS INFECCIONES PROVOCADAS POR EL VIH.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US85071692A | 1992-03-13 | 1992-03-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2066623T3 true ES2066623T3 (es) | 1995-03-01 |
Family
ID=25308925
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES93103712T Expired - Lifetime ES2066623T3 (es) | 1992-03-13 | 1993-03-09 | Derivados sustituidos del acido pipecolinico como inhibidores de la vih-proteasa. |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US5807870A (es) |
| EP (1) | EP0560268B1 (es) |
| JP (1) | JP3258422B2 (es) |
| KR (1) | KR950700253A (es) |
| AP (1) | AP393A (es) |
| AT (1) | ATE116640T1 (es) |
| AU (1) | AU670582B2 (es) |
| CA (1) | CA2131185C (es) |
| CZ (1) | CZ285589B6 (es) |
| DE (1) | DE69300043T2 (es) |
| DK (1) | DK0560268T3 (es) |
| ES (1) | ES2066623T3 (es) |
| FI (1) | FI944217L (es) |
| GR (1) | GR3015622T3 (es) |
| HU (2) | HUT70617A (es) |
| IL (1) | IL105035A (es) |
| NO (1) | NO302570B1 (es) |
| NZ (1) | NZ251267A (es) |
| OA (1) | OA10092A (es) |
| PH (1) | PH30734A (es) |
| PL (1) | PL176362B1 (es) |
| RU (1) | RU2140911C1 (es) |
| SK (1) | SK280161B6 (es) |
| WO (1) | WO1993018003A1 (es) |
| ZA (1) | ZA931776B (es) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5888992A (en) | 1992-03-11 | 1999-03-30 | Narhex Limited | Polar substituted hydrocarbons |
| ATE253050T1 (de) | 1992-03-11 | 2003-11-15 | Narhex Ltd | Aminderivate von oxo- und hydroxy- substituierten kohlenwasserstoffen |
| US6071895A (en) | 1992-03-11 | 2000-06-06 | Narhex Limited | Polar-substituted hydrocarbons |
| EP0633881B1 (en) | 1992-03-11 | 2003-10-29 | Narhex Limited | Amine derivatives of oxo- and hydroxy-substitued hydrocarbons |
| US5559256A (en) * | 1992-07-20 | 1996-09-24 | E. R. Squibb & Sons, Inc. | Aminediol protease inhibitors |
| KR100296463B1 (ko) | 1992-08-25 | 2001-10-24 | 죤 에이치. 뷰센 | 레트로바이러스프로테아제저해제로서유용한히드록시에틸아미노술폰아미드 |
| US5846993A (en) * | 1992-12-22 | 1998-12-08 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
| US5484926A (en) * | 1993-10-07 | 1996-01-16 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
| EP0610745A3 (en) * | 1993-02-09 | 1994-09-28 | Miles Inc | Novel aminomethylene derivatives as immunosuppressants. |
| IL110898A0 (en) * | 1993-09-10 | 1994-11-28 | Narhex Australia Pty Ltd | Polar-substituted hydrocarbons |
| US5527829A (en) * | 1994-05-23 | 1996-06-18 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
| CA2137406C (en) * | 1994-12-06 | 2005-09-13 | Pierre Louis Beaulieu | Process for key intermediates for hiv protease inhibitors |
| US6037157A (en) | 1995-06-29 | 2000-03-14 | Abbott Laboratories | Method for improving pharmacokinetics |
| US5914332A (en) | 1995-12-13 | 1999-06-22 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| US5883252A (en) * | 1996-01-26 | 1999-03-16 | Vertex Pharmaceuticals Incorporated | Aspartyl protease inhibitors |
| US5705647A (en) * | 1996-09-05 | 1998-01-06 | Agouron Pharmaceuticals, Inc. | Intermediates for making HIV-protease inhibitors |
| US5962725A (en) | 1996-09-05 | 1999-10-05 | Agouron Pharmaceuticals, Inc. | Intermediate compounds useful for making HIV protease inhibitors such as nelfinavir |
| US5925759A (en) | 1996-09-05 | 1999-07-20 | Agouron Pharmaceuticals, Inc. | Methods of making HIV-protease inhibitors and intermediates for making HIV-protease inhibitors |
| US6232333B1 (en) | 1996-11-21 | 2001-05-15 | Abbott Laboratories | Pharmaceutical composition |
| US6001851A (en) * | 1997-03-13 | 1999-12-14 | Agouron Pharmaceuticals, Inc. | HIV protease inhibitors |
| US6084107A (en) * | 1997-09-05 | 2000-07-04 | Agouron Pharmaceuticals, Inc. | Intermediates for making HIV-protease inhibitors |
| US6251906B1 (en) | 1998-05-15 | 2001-06-26 | Abbott Laboratories | Retroviral protease inhibiting compounds |
| DK1248600T3 (da) | 2000-01-19 | 2008-09-08 | Abbott Lab | Forbedrede farmaceutiske formuleringer |
| DE60124080T2 (de) * | 2000-03-23 | 2007-03-01 | Elan Pharmaceuticals, Inc., San Francisco | Verbindungen und verfahren zur behandlung der alzheimerschen krankheit |
| US6992081B2 (en) | 2000-03-23 | 2006-01-31 | Elan Pharmaceuticals, Inc. | Compounds to treat Alzheimer's disease |
| US6846813B2 (en) * | 2000-06-30 | 2005-01-25 | Pharmacia & Upjohn Company | Compounds to treat alzheimer's disease |
| PE20020276A1 (es) | 2000-06-30 | 2002-04-06 | Elan Pharm Inc | COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER |
| US20030096864A1 (en) * | 2000-06-30 | 2003-05-22 | Fang Lawrence Y. | Compounds to treat alzheimer's disease |
| EP1666452A2 (en) | 2000-06-30 | 2006-06-07 | Elan Pharmaceuticals, Inc. | Compounds to treat Alzheimer's disease |
| MXPA02012560A (es) | 2000-06-30 | 2003-05-14 | Elan Pharm Inc | Compuestos para tratar la enfermedad de alzheimer. |
| BR0210721A (pt) * | 2001-06-27 | 2004-07-20 | Elan Pharm Inc | Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição |
| US20070213407A1 (en) * | 2001-06-29 | 2007-09-13 | Elan Pharmaceuticals And Pharmacia & Upjohn Company Llc | Compounds to treat Alzheimer's disease |
| AU2003242405A1 (en) | 2003-05-22 | 2004-12-13 | Lead Chemical Co., Ltd. | Compounds and preparaitons having antiviral effect |
| BRPI0510746A (pt) | 2004-06-10 | 2007-11-20 | Univ Michigan State | sìntese de caprolactama a partir de lisina |
| WO2007015805A1 (en) * | 2005-07-20 | 2007-02-08 | Eli Lilly And Company | 1-amino linked compounds |
| CN101541746B (zh) * | 2007-02-20 | 2013-01-02 | 密执安州立大学董事会 | 用于生产己内酰胺的催化脱氨基 |
| KR101518079B1 (ko) | 2007-03-12 | 2015-05-06 | 넥타르 테라퓨틱스 | 올리고머-프로테아제 억제제 컨주게이트 |
| EP2262538B1 (en) | 2008-03-12 | 2014-12-10 | Nektar Therapeutics | Oligomer-amino acid conjugate |
| WO2010011967A1 (en) * | 2008-07-24 | 2010-01-28 | Draths Corporation | Methods of making cyclic amide monomers, and related derivatives and methods |
| EP2440249A2 (en) | 2009-06-12 | 2012-04-18 | Nektar Therapeutics | Covalent conjugates comprising a protease inhibitor, a water-soluble, non-peptidic oligomer and a lipophilic moiety |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0264106B1 (en) * | 1986-10-14 | 1994-03-16 | Banyu Pharmaceutical Co., Ltd. | 5-Substituted amino-4-hydroxy-pentanoic acid derivatives and their use |
| CA1340588C (en) * | 1988-06-13 | 1999-06-08 | Balraj Krishan Handa | Amino acid derivatives |
| GB8927913D0 (en) * | 1989-12-11 | 1990-02-14 | Hoffmann La Roche | Amino acid derivatives |
| GB8927915D0 (en) * | 1989-12-11 | 1990-02-14 | Hoffmann La Roche | Novel alcohols |
| MY110227A (en) * | 1991-08-12 | 1998-03-31 | Ciba Geigy Ag | 1-acylpiperindine compounds. |
| ZA931777B (en) * | 1992-03-13 | 1993-09-23 | Bio Mega Boehringer Ingelheim | Substituted pyrrolidine derivatives as HIV protease inhibitors. |
| IL110255A (en) * | 1993-07-16 | 1998-12-06 | Merck & Co Inc | Formation and resolution of 2-tert-butylcarboxamido-piperazine |
| US5480887A (en) * | 1994-02-02 | 1996-01-02 | Eli Lilly And Company | Protease inhibitors |
| GB2292146A (en) * | 1994-08-11 | 1996-02-14 | Merck & Co Inc | HIV protease inhibitors useful for the treatment of AIDS |
-
1993
- 1993-03-09 DE DE69300043T patent/DE69300043T2/de not_active Expired - Lifetime
- 1993-03-09 AT AT93103712T patent/ATE116640T1/de active
- 1993-03-09 DK DK93103712.1T patent/DK0560268T3/da active
- 1993-03-09 EP EP93103712A patent/EP0560268B1/en not_active Expired - Lifetime
- 1993-03-09 ES ES93103712T patent/ES2066623T3/es not_active Expired - Lifetime
- 1993-03-10 AP APAP/P/1993/000495A patent/AP393A/en active
- 1993-03-11 PH PH45862A patent/PH30734A/en unknown
- 1993-03-12 WO PCT/CA1993/000096 patent/WO1993018003A1/en active IP Right Grant
- 1993-03-12 PL PL93305166A patent/PL176362B1/pl unknown
- 1993-03-12 CZ CZ942232A patent/CZ285589B6/cs not_active IP Right Cessation
- 1993-03-12 AU AU38808/93A patent/AU670582B2/en not_active Ceased
- 1993-03-12 CA CA002131185A patent/CA2131185C/en not_active Expired - Lifetime
- 1993-03-12 HU HU9402613A patent/HUT70617A/hu unknown
- 1993-03-12 NZ NZ251267A patent/NZ251267A/en unknown
- 1993-03-12 SK SK1090-94A patent/SK280161B6/sk unknown
- 1993-03-12 IL IL105035A patent/IL105035A/xx not_active IP Right Cessation
- 1993-03-12 RU RU94040841A patent/RU2140911C1/ru active
- 1993-03-12 ZA ZA931776A patent/ZA931776B/xx unknown
- 1993-03-15 JP JP05414293A patent/JP3258422B2/ja not_active Expired - Fee Related
-
1994
- 1994-08-05 OA OA60550A patent/OA10092A/en unknown
- 1994-09-12 NO NO943383A patent/NO302570B1/no unknown
- 1994-09-13 KR KR1019940703190A patent/KR950700253A/ko not_active Abandoned
- 1994-09-13 FI FI944217A patent/FI944217L/fi unknown
-
1995
- 1995-03-27 GR GR950400700T patent/GR3015622T3/el unknown
- 1995-06-23 HU HU95P/P00429P patent/HU211854A9/hu unknown
-
1996
- 1996-12-11 US US08/763,464 patent/US5807870A/en not_active Expired - Lifetime
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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