AR035970A1 - 2-amino-benzoxazol sulfonamidas inhibidoras de amplio espectro de la hiv proteasa, composicion farmaceutica, metodo "in vitro" para inhibir la replicacion retroviral, y utilizacion de estos compuestos en la manufactura de medicamentos - Google Patents
2-amino-benzoxazol sulfonamidas inhibidoras de amplio espectro de la hiv proteasa, composicion farmaceutica, metodo "in vitro" para inhibir la replicacion retroviral, y utilizacion de estos compuestos en la manufactura de medicamentosInfo
- Publication number
- AR035970A1 AR035970A1 ARP020101722A ARP020101722A AR035970A1 AR 035970 A1 AR035970 A1 AR 035970A1 AR P020101722 A ARP020101722 A AR P020101722A AR P020101722 A ARP020101722 A AR P020101722A AR 035970 A1 AR035970 A1 AR 035970A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- het2
- het1
- aryl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 238000004519 manufacturing process Methods 0.000 title abstract 3
- SDCCPSGJFZFNPB-UHFFFAOYSA-N 2-amino-3h-1,3-benzoxazole-2-sulfonamide Chemical compound C1=CC=C2OC(N)(S(N)(=O)=O)NC2=C1 SDCCPSGJFZFNPB-UHFFFAOYSA-N 0.000 title abstract 2
- 238000000338 in vitro Methods 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 230000010076 replication Effects 0.000 title abstract 2
- 230000001177 retroviral effect Effects 0.000 title abstract 2
- 108091005804 Peptidases Proteins 0.000 title 1
- 239000004365 Protease Substances 0.000 title 1
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 title 1
- 238000001228 spectrum Methods 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 18
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 13
- 125000003118 aryl group Chemical group 0.000 abstract 13
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 9
- 229910052739 hydrogen Inorganic materials 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 8
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 5
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000005201 cycloalkylcarbonyloxy group Chemical group 0.000 abstract 2
- 108091005502 Aspartic proteases Proteins 0.000 abstract 1
- 102000035101 Aspartic proteases Human genes 0.000 abstract 1
- -1 C1-4 Chemical group 0.000 abstract 1
- 108010010369 HIV Protease Proteins 0.000 abstract 1
- 241000725303 Human immunodeficiency virus Species 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000005098 aryl alkoxy carbonyl group Chemical group 0.000 abstract 1
- 125000005199 aryl carbonyloxy group Chemical group 0.000 abstract 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 abstract 1
- 125000005200 aryloxy carbonyloxy group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
- C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
- C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
-
- 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
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (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)
- Virology (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
2-amino-benzoxazol sulfonamidas que tienen la fórmula (1), un N-óxido, sal, forma estereoisomérica, mezclas racémicas, prodroga, éster o metabolito del mismo, en la cual R1 y R8 son, independientemente entre sí, hidrógeno, alquilo C1-6, alquenilo C2-6, arilalquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-6, arilo, Het1, Het1-alquilo C1-6, Het2, o Het2-alquilo C1-6; R1 también puede ser un radical de fórmula (R11a)(R11b)N-C(R10a)(R10b)-CHR9- en la cual R9, R10a y R10b son, independientemente entre sí, hidrógeno, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo, mono- o di(alquil C1-4)aminocarbonilo, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6, o alquilo C1-4 opcionalmente sustituido con arilo, Het1, Het2, cicloalquilo C3-7, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo, mono- o di(alquil C1-4)aminocarbonilo, aminosulfonilo, alquil C1-4S(O)t, hidroxi, ciano, halógeno o amino opcionalmente mono- o disustituido, donde los sustituyentes se seleccionan, independientemente entre sí, del grupo formado por alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1-alquilo C1-4 y Het2-alquilo C1-4; con lo cual R9, R10a y los átomos de carbono a los cuales están fijados pueden formar también un radical cicloalquilo C3-7; cuando L es -O-alcanodiilo C1-6-C(=O)- ó -NR8-alcanodiilo C1-6-C(=O)-, entonces R9 puede ser también oxo; R11a es hidrógeno, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo, aminocarbonilo opcionalmente mono- o disustituido, aminoalquilcarboniloxi C1-4 opcionalmente mono- o disustituido, alquiloxicarbonilo C1-4, ariloxicarbonilo, Het1-oxicarbonilo, Het2-oxicarbonilo, ariloxicarbonilalquilo C1-4, aril alquiloxicarbonilo, C1-4, alquilcarbonilo C1-4, cicloalquilcarbonilo C3-7, cicloalquil C3-7 alquiloxicarbonilo C1-4, cicloalquilcarboniloxi C3-7, carboxialquilcarboniloxi C1-4, alquilcarboniloxi C1-4, arilalquilcarboniloxi C1-4, arilcarboniloxi, ariloxicarboniloxi, Het1-carbonilo, Het1-carboniloxi, Het1-alquiloxicarbonilo C1-4, Het2-carboniloxi, Het2-alquilcarboniloxi C1-4, Het2-alquiloxicarboniloxi C1-4 o alquilo C1-4 opcionalmente sustituido con arilo, ariloxi, Het2, halógeno o hidroxi; donde los sustituyentes en los grupos amino se seleccionan independientemente entre sí, del grupo formado por alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1-alquilo C1-4 y Het2-alquilo C1-4; R11b es hidrógeno, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6, arilo, Het1, Het2 o alquilo C1-4 opcionalmente sustituido con halógeno, hidroxi, alquil C1-4 S(O)t, arilo, cicloalquilo C3-7, Het1, Het2, amino opcionalmente mono- o disustituido, donde los sustituyentes, independientemente entre sí, se seleccionan del grupo formado por alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1-alquilo C1-4 y Het2-alquilo C1-4; donde R11b puede estar unido al resto de la molécula a través de un grupo sulfonilo; t es independientemente entre sí 0, 1 ó 2; R2 es hidrógeno o alquilo C1-6; L es -C(=O)-, -O-C(=O)-, -NR8-C(O)-, -O-alcanodiil C1-6-C(=O)-, -NR8-alcanodiil C1-6-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2, donde ya sea el grupo C(=O) o el grupo S(=O)2 está unido a la porción NR2; y con lo cual la porción alcanodiilo C1-6 está opcionalmente sustituida con hidroxi, arilo, Het1 y Het2; R3 es alquilo C1-6, arilo, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4 o arilalquilo C1-4; R4 es hidrógeno, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo, mono- o di(alquil C1-4)aminocarbonilo, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6 o alquilo C1-6 opcionalmente sustituido con uno o más sustituyentes seleccionados, independientemente entre sí, del grupo formado por arilo, Het1, Het2, cicloalquilo C3-7, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo, mono- o di(alquil C1-4) aminocarbonilo, aminosulfonilo, alquil C1-4 S(=O)t, hidroxi, ciano, halógeno y amino opcionalmente mono- o disustituido, donde los sustituyentes se seleccionan, independientemente entre sí, del grupo formado por alquilo C1-4, arilo, arilalquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1-alquilo C1-4 y Het2-alquilo C1-4; R5 es hidrógeno ó alquilo C1-6; R6 es hidrógeno o alquilo C1-6; composición farmacéutica, método "in vitro" para inhibir la replicación retroviral y utilización de estos compuestos en la manufactura de medicamentos. Los compuestos de fórmula (1) son utilizados como inhibidores de la proteasa aspártica, en particular de la proteasa HIV, de allí su acción inhibitoria sobre el virus del SIDA.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01201732 | 2001-05-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR035970A1 true AR035970A1 (es) | 2004-07-28 |
Family
ID=8180286
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020101722A AR035970A1 (es) | 2001-05-11 | 2002-05-10 | 2-amino-benzoxazol sulfonamidas inhibidoras de amplio espectro de la hiv proteasa, composicion farmaceutica, metodo "in vitro" para inhibir la replicacion retroviral, y utilizacion de estos compuestos en la manufactura de medicamentos |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US7622490B2 (es) |
| EP (1) | EP1387842B1 (es) |
| JP (1) | JP4467889B2 (es) |
| KR (1) | KR100878853B1 (es) |
| CN (1) | CN100549007C (es) |
| AP (1) | AP1652A (es) |
| AR (1) | AR035970A1 (es) |
| AT (1) | ATE429431T1 (es) |
| AU (1) | AU2002310818B2 (es) |
| BG (1) | BG66350B1 (es) |
| BR (1) | BR0209594A (es) |
| CA (1) | CA2444895C (es) |
| CY (1) | CY1109247T1 (es) |
| CZ (1) | CZ304524B6 (es) |
| DE (1) | DE60232067D1 (es) |
| DK (1) | DK1387842T3 (es) |
| EA (1) | EA009590B1 (es) |
| EE (1) | EE05307B1 (es) |
| ES (1) | ES2325809T3 (es) |
| HR (1) | HRP20031026B1 (es) |
| HU (1) | HUP0400438A3 (es) |
| IL (1) | IL158093A0 (es) |
| MX (1) | MXPA03010258A (es) |
| NO (1) | NO326883B1 (es) |
| NZ (1) | NZ529250A (es) |
| OA (1) | OA13134A (es) |
| PL (1) | PL209029B1 (es) |
| PT (1) | PT1387842E (es) |
| SK (1) | SK287952B6 (es) |
| WO (1) | WO2002092595A1 (es) |
| ZA (1) | ZA200307799B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2359945C (en) | 1999-11-12 | 2011-04-26 | Abbott Laboratories | Inhibitors of crystallization in a solid dispersion |
| US7364752B1 (en) | 1999-11-12 | 2008-04-29 | Abbott Laboratories | Solid dispersion pharamaceutical formulations |
| DE10026698A1 (de) | 2000-05-30 | 2001-12-06 | Basf Ag | Selbstemulgierende Wirkstoffformulierung und Verwendung dieser Formulierung |
| AU2003202914A1 (en) | 2002-01-07 | 2003-07-24 | Sequoia Pharmaceuticals | Broad spectrum inhibitors |
| US7157489B2 (en) | 2002-03-12 | 2007-01-02 | The Board Of Trustees Of The University Of Illinois | HIV protease inhibitors |
| US8025899B2 (en) | 2003-08-28 | 2011-09-27 | Abbott Laboratories | Solid pharmaceutical dosage form |
| ES2281828T3 (es) * | 2003-09-30 | 2007-10-01 | Tibotec Pharmaceuticals Ltd. | Metodos para la preparacion de compuestos de benzoxazol-sulfonamida y compuestos intermedios de la misma. |
| US8193227B2 (en) | 2003-12-11 | 2012-06-05 | Abbott Laboratories | HIV protease inhibiting compounds |
| US20050131042A1 (en) * | 2003-12-11 | 2005-06-16 | Flentge Charles A. | HIV protease inhibiting compounds |
| DK1725566T3 (da) | 2003-12-23 | 2009-10-05 | Tibotec Pharm Ltd | Fremgangsmåde til fremstilling af (3R,3AS, 6AR)-hexahydrofuro [2,3.B] furan-3-yl (1S,2R)-3-3[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamat |
| JP4818124B2 (ja) | 2003-12-23 | 2011-11-16 | テイボテク・フアーマシユーチカルズ・リミテツド | （３Ｒ，３ａＳ，６ａＲ）−ヘキサヒドロフロ〔２，３−ｂ〕フラン−３−イル（１Ｓ，１Ｒ）−３−〔〔（４−アミノフェニル）スルホニル〕（イソブチル）アミノ〕−１−ベンジル−２−ヒドロキシプロピルカルバマートの製造方法 |
| CA2566340C (en) * | 2004-05-07 | 2014-05-06 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
| PT1856125E (pt) | 2005-02-25 | 2009-11-06 | Tibotec Pharm Ltd | Síntese de precursor de inibidor de proteases |
| AR053845A1 (es) * | 2005-04-15 | 2007-05-23 | Tibotec Pharm Ltd | 5-tiazolilmetil[(1s,2r)-3-[[(2-amino-6-benzoxazolil)sulfonil)](2-metilpropil)amino]-2-hidroxi-1-(fenilmetil)propil]carbamato como mejorador de farmacos metabolizados por el citocromo p450 |
| US20120220520A1 (en) * | 2006-10-17 | 2012-08-30 | Van T Klooster Gerben Albert Eleutherius | Bioavailable combinations for hcv treatment |
| WO2014194519A1 (en) | 2013-06-07 | 2014-12-11 | Merck Sharp & Dohme Corp. | Imidazole derivatives and methods of use thereof for improving pharmacokinetics of drug |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE8204879D0 (sv) | 1982-08-26 | 1982-08-26 | Haessle Ab | Novel chemical intermediates |
| EP0445926B1 (en) | 1990-03-09 | 1996-08-21 | Milliken Research Corporation | Organic materials having sulfonamido linked poly(oxyalkylene) moieties and their preparation |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| ATE154800T1 (de) * | 1992-08-25 | 1997-07-15 | Searle & Co | N-(alkanoylamino-2-hydroxypropyl)-sulfonamide verwendbar als retrovirale proteaseninhibitoren |
| PH30929A (en) | 1992-09-03 | 1997-12-23 | Janssen Pharmaceutica Nv | Beads having a core coated with an antifungal and a polymer. |
| EP0715618B1 (en) * | 1993-08-24 | 1998-12-16 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
| PT721331E (pt) | 1993-10-01 | 2002-05-31 | Astrazeneca Ab | Processo i |
| ATE382041T1 (de) | 1995-01-20 | 2008-01-15 | Searle Llc | Bis-sulfonamid-hydroxyethylamino-derivate als inhibitoren retroviraler proteasen |
| US5756533A (en) * | 1995-03-10 | 1998-05-26 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| US6150556A (en) * | 1995-03-10 | 2000-11-21 | G. D. Dearle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| US5705500A (en) * | 1995-03-10 | 1998-01-06 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| CN1530372A (zh) | 1995-03-10 | 2004-09-22 | G.D.ɪ����˾ | 杂环羰基氨基酸羟乙氨基磺酰胺逆转录病毒蛋白酶抑制剂 |
| AU7722296A (en) | 1995-11-15 | 1997-06-05 | G.D. Searle & Co. | Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| IL124935A (en) | 1996-05-20 | 2001-06-14 | Janssen Pharmaceutica Nv | Dispersible antifungal compositions comprising itraconazole with improved bioavailability |
| EP0969821B1 (en) | 1997-03-26 | 2003-06-04 | Janssen Pharmaceutica N.V. | Pellets having a core coated with an antifungal and a polymer |
| GB9717849D0 (en) | 1997-08-23 | 1997-10-29 | Seal Sands Chemicals Limited | Preparation of pyridene derivatives |
| AU2012199A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| US6436989B1 (en) | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
| BR9814484A (pt) | 1997-12-24 | 2000-10-10 | Vertex Pharma | "pró-drogas de inibidores de aspartil protease" |
| WO1999033792A2 (en) | 1997-12-24 | 1999-07-08 | Vertex Pharmaceuticals Incorporated | Prodrugs os aspartyl protease inhibitors |
| CA2336160C (en) | 1998-06-23 | 2015-02-17 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Use of compounds for treating hiv |
| AU4828199A (en) * | 1998-06-23 | 2000-01-10 | Board Of Trustees Of The University Of Illinois, The | Multi-drug resistant retroviral protease inhibitors and associated methods |
| CN100491360C (zh) * | 2001-04-09 | 2009-05-27 | 泰博特克药品有限公司 | 广谱2-(取代的-氨基)-苯并唑磺酰胺hiv蛋白酶抑制剂 |
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2002
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