AR039887A1 - Inhibidores de la proteasa de hiv de benzisoxazol sulfonamida sustituida de amplio espectro, composiciones y combinaciones farmaceuticas, y uso de dichos inhibidores para la elaboracion de un medicamento para tratar condiciones asociadas con hiv y otros retrovirus patogenos - Google Patents
Inhibidores de la proteasa de hiv de benzisoxazol sulfonamida sustituida de amplio espectro, composiciones y combinaciones farmaceuticas, y uso de dichos inhibidores para la elaboracion de un medicamento para tratar condiciones asociadas con hiv y otros retrovirus patogenosInfo
- Publication number
- AR039887A1 AR039887A1 ARP030101725A ARP030101725A AR039887A1 AR 039887 A1 AR039887 A1 AR 039887A1 AR P030101725 A ARP030101725 A AR P030101725A AR P030101725 A ARP030101725 A AR P030101725A AR 039887 A1 AR039887 A1 AR 039887A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- het1
- het2
- aryl
- cycloalkyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 4
- OIFAKIJHBGJKLD-UHFFFAOYSA-N 1,2-benzoxazole-3-sulfonamide Chemical compound C1=CC=C2C(S(=O)(=O)N)=NOC2=C1 OIFAKIJHBGJKLD-UHFFFAOYSA-N 0.000 title abstract 2
- 239000000203 mixture Substances 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
- 229940126601 medicinal product Drugs 0.000 title 1
- 238000001228 spectrum Methods 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 22
- 125000003118 aryl group Chemical group 0.000 abstract 15
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 12
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 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
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 5
- -1 C3- cycloalkyl 7 Chemical group 0.000 abstract 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 4
- 125000005196 alkyl carbonyloxy 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
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000003277 amino group Chemical group 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 2
- 125000004104 aryloxy group Chemical group 0.000 abstract 2
- 125000005708 carbonyloxy group Chemical group [*:2]OC([*:1])=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
- 125000005740 oxycarbonyl group Chemical group [*:1]OC([*:2])=O 0.000 abstract 2
- 108010010369 HIV Protease Proteins 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 abstract 1
- 125000005194 alkoxycarbonyloxy group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000002431 aminoalkoxy group Chemical group 0.000 abstract 1
- 125000005122 aminoalkylamino 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
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000001717 pathogenic effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition 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
- 241001430294 unidentified retrovirus Species 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/20—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
-
- 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
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Virology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (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)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Inhibidores de la proteasa de HIV de benzisoxazol sulfonamida sustituidos que tienen la fórmula (1), un N-óxido, sal, forma estereoisomérica, mezcla racémica, profármaco, éster o metabolito del mismo, en donde: R1 y R8 son, cada uno en forma independiente, hidrógeno, alquilo C1-6, alquenilo C2-6, aril alquilo C1-6, cicloalquilo C3-7, cicloalquilo C3-7 alquilo C1-6, arilo, Het1, Het1alquilo C1-6, Het2, Het2 alquilo C1-6; R1 también puede ser un radical de fórmula (2) en donde: R9, R10a y R10b son, cada uno independientemente, hidrógeno, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo, mono o di(alquilo 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(alquilo C1-4)aminocarbonilo, aminosulfonilo, alquilo C1-4 S(O)t, hidroxi, ciano, halógeno o amino opcionalmente mono o disustituido, donde los sustituyentes se seleccionan, cada uno en forma independiente, entre alquilo C1-4, arilo, aril alquilo C1-4, cicloalquilo C3-7, cicloalquilo C3-7 alquilo C1-4, Het1, Het2, Het1alquilo C1-4 y Het2 alquilo C1-4; en donde R9, R10a y los átomos de carbono a los cuales están unidos pueden formar también un radical cicloalquilo C3-7; cuando L es -O-alcanodiilo C1-6-C(=O)- o -NR8-alcanodiilo C1-6-C(=O)-, entonces R9 también puede ser oxo; R11a es hidrógeno, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo, aminocarbonilo opcionalmente mono o disustituido, amino alquilcarboniloxi C1-4 opcionalmente mono o disustituido, alquiloxicarbonilo C1-4, ariloxicarbonilo, Het1 oxicarbonilo, Het2 oxicarbonilo, ariloxicarbonil alquilo C1-4, aril alquiloxicarbonilo C1-4, alquilcarbonilo C1-4, cicloalquilcarbonilo C3-7, cicloalquil C3-7-alquiloxicarbonilo C1-4, cicloalquilcarboniloxi C3-7, carboxil alquilcarboniloxi C1-4, alquilcarboniloxi C1-4, aril alquilcarboniloxi 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; en donde los sustituyentes en los grupos amino se seleccionan, cada uno en forma independientemente, entre alquilo C1-4, arilo, aril alquilo C1-4, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, Het1, Het2, Het1 alquilo C1-4 y Het2alquilo 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, alquilo C1-4S(=O)t, arilo, cicloalquilo C3-7, Het1, Het2, amino opcionalmente mono o disustituido, donde los sustituyentes se seleccionan, cada uno en forma independiente, entre alquilo C1-4, arilo, aril alquilo C1-4, cicloalquilo C3-7, cicloalquilo C3-7 alquilo C1-4, Het1, Het2, Het1 alquilo C1-4 y Het2 alquilo C1-4; donde R11b puede estar ligado al resto de la molécula por medio de un grupo sulfonilo; t es, cada uno de manera independiente, 0, 1 ó 2; R2 es hidrógeno o alquilo C1-6; L es -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-alcanodiilo C1-6 -C(=O)-, -NR8-alcanodiilo C1-6-C(=O)-, -S(=O)2-, -O-S(=O)2-, -NR8-S(=O)2-, en donde el grupo C(=O) o el grupo S(=O)2 está unido a la porción NR2; n donde la porción alcanodiilo C1-6 está opcionalmente sustituida con un sustituyente seleccionado entre hidroxi, arilo, Het1 y Het2; R3 es alquilo C1-6, arilo, cicloalquilo C3-7, cicloalquil C3-7 alquilo C1-4, o aril alquilo C1-4; R4 es hidrógeno, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo, mono o di(alquilo C1-4) aminocarbonilo, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6, o alquilo C1-6 opcionalmente sustituido con uno o más sustituyentes seleccionados, cada uno en forma independiente, entre arilo, Het1, Het2, cicloalquilo C3-7, alquiloxicarbonilo C1-4, carboxilo, aminocarbonilo, mono o di(alquilo C1-4) aminocarbonilo, aminosulfonilo, alquilo C1-4 S(=O)t, hidroxi, ciano, halógeno y amino opcionalmente mono o disustituido, donde los sustituyentes se seleccionan, cada uno en forma independiente, entre alquilo C1-4, arilo, aril alquilo C1-4, cicloalquilo C3-7, cicloalquilo C3-7- alquilo C1-4, Het1, Het2, Het1alquilo C1-4 y Het2alquilo C1-4; R2 es -NH2 o -N(R5)(A-R6) en donde A es alcanodiilo C1-6, -C(=O)-, -C(=S)-, -S(=O)2-, alcanodiilo C1-6 -C(=O)-, alcanodiilo C1-6-C(=S)-, o alcanodiilo C1-6-S(=O)2-; en donde el punto de unión de A a la función amino sobre la cual está sustituido es el grupo alcanodiilo C1-6 en aquellos significados de A que contengan dicho grupo alcanodiilo C1-6; R5 es hidrógeno, hidroxi, alquilo C1-6, Het1alquilo C1-6, Het2alquilo C1-6, amino alquilo C1-6, donde el grupo amino puede estar opcionalmente mono o disustituido con alquilo C1-4; R6 es hidrógeno, alquiloxi C1-6, Het1, Het1oxi, Het2, Het2oxi, arilo, ariloxi, ariloxi alquilo C1-4, alquiloxiarilo C1-4, alquiloxi C1-4 Het1, alquiloxi C1-4Het2, alquiloxicarbonilamino C1-4, amino alquilamino C1-4, amino o amino alquiloxi C1-4, y en el caso que A no sea alcanodiilo C1-6, entonces R6 también puede ser alquilo C1-6, Het1 alquilo C1-4, Het1 oxi alquilo C1-4, Het2 alquilo C1-4, Het2oxi alquilo C1-4, aril alquilo C1-4, ariloxi alquilo C1-4, o amino alquilo C1-4; donde cada grupo amino puede estar opcionalmente mono o, cuando fuera posible, disustituido con alquilo C1-4; -A-R6 también puede ser hidroxi alquilo C1-6; R5 y -A-R6 tomados junto con el átomo de nitrógeno al cual están unidos también pueden formar Het1 o Het2; procedimientos para su preparación así como composiciones y combinaciones farmacéuticas, y uso de dichos inhibidores para la elaboración de un medicamento para tratar condiciones asociadas con HIV y otros retrovirus patógenos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02076957 | 2002-05-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR039887A1 true AR039887A1 (es) | 2005-03-09 |
Family
ID=29433159
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030101725A AR039887A1 (es) | 2002-05-17 | 2003-05-16 | Inhibidores de la proteasa de hiv de benzisoxazol sulfonamida sustituida de amplio espectro, composiciones y combinaciones farmaceuticas, y uso de dichos inhibidores para la elaboracion de un medicamento para tratar condiciones asociadas con hiv y otros retrovirus patogenos |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US7462636B2 (es) |
| EP (1) | EP1517899B1 (es) |
| JP (2) | JP4674084B2 (es) |
| KR (2) | KR20100130234A (es) |
| CN (1) | CN100582097C (es) |
| AP (1) | AP2004003190A0 (es) |
| AR (1) | AR039887A1 (es) |
| AT (1) | ATE371652T1 (es) |
| AU (1) | AU2003238074B2 (es) |
| BR (1) | BR0310089A (es) |
| CA (1) | CA2485903C (es) |
| CY (1) | CY1107040T1 (es) |
| DE (1) | DE60315984T2 (es) |
| DK (1) | DK1517899T3 (es) |
| EA (1) | EA010908B1 (es) |
| ES (1) | ES2292976T3 (es) |
| HR (1) | HRP20050607B1 (es) |
| IL (1) | IL165043A0 (es) |
| MX (1) | MXPA04011466A (es) |
| MY (1) | MY135226A (es) |
| NO (1) | NO330184B1 (es) |
| NZ (1) | NZ536496A (es) |
| PL (1) | PL373425A1 (es) |
| PT (1) | PT1517899E (es) |
| SI (1) | SI1517899T1 (es) |
| TW (1) | TWI356700B (es) |
| WO (1) | WO2003097616A1 (es) |
| ZA (1) | ZA200410156B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL165043A0 (en) * | 2002-05-17 | 2005-12-18 | Tibotec Pharm Ltd | broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors |
| US7807845B2 (en) * | 2004-03-11 | 2010-10-05 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
| 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 |
| EP2139883A4 (en) * | 2007-03-23 | 2011-06-22 | Univ Massachusetts | HIV-1 protease inhibitor |
| EP2170289B1 (en) * | 2008-03-25 | 2012-02-15 | Formac Pharmaceuticals N.v. | Preparation method for solid disupersions |
| WO2011061590A1 (en) | 2009-11-17 | 2011-05-26 | Hetero Research Foundation | Novel carboxamide derivatives as hiv inhibitors |
| DE102010004957A1 (de) * | 2010-01-14 | 2011-07-21 | Universitätsklinikum Jena, 07743 | Biologisch wirksame Moleküle zur Beeinflussung von Virus-, Bakterien-, Parasiten-infizierten Zellen und/oder Tumorzellen und Verfahren zu deren Anwendung |
| BR112015009751A2 (pt) | 2012-10-31 | 2017-07-11 | Bayer Cropscience Ag | novos compostos heterocíclicos como pesticidas |
| CN105025887B (zh) * | 2013-03-07 | 2017-07-28 | 陶氏环球技术有限责任公司 | 新颖极低粘度酯化纤维素醚 |
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| US5004751A (en) * | 1987-08-28 | 1991-04-02 | Mochida Pharmaceutical Co., Ltd. | Hydantoin derivatives |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| ES2177868T3 (es) * | 1992-08-25 | 2002-12-16 | Searle & Co | Hidroxietilaminosulfonamidas de alfa- y beta-aminoacidos utiles como inhibidores de proteasas retroviricas. |
| PH30929A (en) | 1992-09-03 | 1997-12-23 | Janssen Pharmaceutica Nv | Beads having a core coated with an antifungal and a polymer. |
| IS2334B (is) * | 1992-09-08 | 2008-02-15 | Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) | Aspartyl próteasi hemjari af nýjum flokki súlfonamíða |
| 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 |
| US5705500A (en) * | 1995-03-10 | 1998-01-06 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
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| EP0969821B1 (en) | 1997-03-26 | 2003-06-04 | Janssen Pharmaceutica N.V. | Pellets having a core coated with an antifungal and a polymer |
| 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 |
| 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 |
| 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 |
| ATE398623T1 (de) | 1999-10-06 | 2008-07-15 | Tibotec Pharm Ltd | Hexahydrofuro-2,3-b furan-3-yl-n- 3-,(1,3- benzodioxol-5-ylsulfonyl)(isobutyl)amino -1- benzyl-2-hydroxypropyl carbamat als retrovirusproteasehemmer |
| 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 |
| IL165043A0 (en) * | 2002-05-17 | 2005-12-18 | Tibotec Pharm Ltd | broadspectrum substituted benzisoxazole sulfonamide hiv protease inhibitors |
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2003
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- 2003-05-16 EP EP03735707A patent/EP1517899B1/en not_active Expired - Lifetime
- 2003-05-16 KR KR1020107025714A patent/KR20100130234A/ko not_active Withdrawn
- 2003-05-16 DE DE60315984T patent/DE60315984T2/de not_active Expired - Lifetime
- 2003-05-16 NZ NZ536496A patent/NZ536496A/en not_active IP Right Cessation
- 2003-05-16 DK DK03735707T patent/DK1517899T3/da active
- 2003-05-16 WO PCT/EP2003/050173 patent/WO2003097616A1/en not_active Ceased
- 2003-05-16 PT PT03735707T patent/PT1517899E/pt unknown
- 2003-05-16 CN CN03816458A patent/CN100582097C/zh not_active Expired - Fee Related
- 2003-05-16 SI SI200331012T patent/SI1517899T1/sl unknown
- 2003-05-16 EA EA200401524A patent/EA010908B1/ru not_active IP Right Cessation
- 2003-05-16 PL PL03373425A patent/PL373425A1/xx unknown
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- 2003-05-16 CA CA2485903A patent/CA2485903C/en not_active Expired - Fee Related
- 2003-05-16 HR HRP20050607AA patent/HRP20050607B1/hr not_active IP Right Cessation
- 2003-05-16 ES ES03735707T patent/ES2292976T3/es not_active Expired - Lifetime
- 2003-05-16 AT AT03735707T patent/ATE371652T1/de active
- 2003-05-16 MY MYPI20031819A patent/MY135226A/en unknown
- 2003-05-16 BR BR0310089-8A patent/BR0310089A/pt not_active IP Right Cessation
- 2003-05-16 AU AU2003238074A patent/AU2003238074B2/en not_active Ceased
- 2003-05-16 AP AP2004003190A patent/AP2004003190A0/xx unknown
- 2003-05-16 KR KR1020047018261A patent/KR101019648B1/ko not_active Expired - Fee Related
- 2003-05-16 AR ARP030101725A patent/AR039887A1/es active IP Right Grant
- 2003-05-16 JP JP2004505349A patent/JP4674084B2/ja not_active Expired - Fee Related
- 2003-05-16 US US10/514,539 patent/US7462636B2/en not_active Expired - Fee Related
- 2003-05-16 MX MXPA04011466A patent/MXPA04011466A/es active IP Right Grant
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2004
- 2004-12-14 NO NO20045444A patent/NO330184B1/no not_active IP Right Cessation
- 2004-12-15 ZA ZA2004/10156A patent/ZA200410156B/en unknown
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2007
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2010
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