BR0208796A - Inibidores 2-(amino substituìdo)-benzoxazol sulfonamida hiv protease de amplo espectro - Google Patents
Inibidores 2-(amino substituìdo)-benzoxazol sulfonamida hiv protease de amplo espectroInfo
- Publication number
- BR0208796A BR0208796A BR0208796-0A BR0208796A BR0208796A BR 0208796 A BR0208796 A BR 0208796A BR 0208796 A BR0208796 A BR 0208796A BR 0208796 A BR0208796 A BR 0208796A
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- het
- alkanediyl
- aryl
- amino
- Prior art date
Links
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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- 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
-
- 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
- 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
- C07D417/14—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 three or more hetero rings
-
- 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
Abstract
"INIBIDORES 2-(AMINO SUBSTITUìDO)BENZOXAZOL SULFONAMIDA HIV PROTEASE DE AMPLO ESPECTRO". A presente invenção refere-se a compostos tendo a fórmula (I), seus N-óxidos, sais, formas estereoisoméricas, misturas racêmicas, pró-drogas, ésteres e metabólitos, em que R~ 1~ e R~ 8~ cada um são H, alquila C~ 1-6~, alquenila C~ 2-6~, cicloalquila C~ 3-7~, arila, Het^ 1^, Het^ 2^; R~ 1~ pode também ser um radical de fórmula (R11 aR11 b)NC(R10aR10b)CR9-; t é zero, 1 ou 2; R~ 2~ é H ou alquila C~ 1-6~; L é -C(=O)-, -0-C(=O)-, -NR~ 8~-C(=O)-, -O-C~ 1-6~ alcanodiila -C(=O)-, -NR~ 8~-C~ 1-6~ alcanodiila -C(=O)-, -S(=0)~ 2~-, -0-S(=0)~ 2~-, -NR~ 3~-S(=0)~ 2~; R~ 3~ é alquila C~ 1-6~, arila, cicloalquila C~ 3-7~, C~ 3-7~ cicloalquil C~ 1-4~ alquila, ou aril C~ 1-4~ alquila; R~ 4~ é H, C~ 1-4~ alquila OC(=O), carboxila, aminoC(=O), mono- ou diamino(alquila C~ 1-4~)C(=O), cicloalquila C~ 3-7~, alquenila C~ 2-6~, alquinila C~ 2-6~, ou alquila C~ 1-6~ opcionalmente substituída; A é alcanodiila C~ 1-6~, -C(=O)-, -C(=S)-, -S(=0)~ 2-~, C~ 1-6~ alcanodiila -C(=O)-, C~ 1-6~ alcanodiila -C(=S)- ou C~ 1-6~alcanodiila -S(=0)~ 2~; R~ 5~ é H, OH, alquila C~ 1-6~, Het^ 1^C~ 1-6~alquila, Het^ 2~C~ 1-6~alquila, amino C~ 1-6~ alquila opcionalmente substituída; R~ 6~ é alquila0 C~ 1-6~, Het^ 1^, Het^ 1^O, Het^ 2^, Het^ 2^O, arila, arilaO, alquiloxicarbonilamino C~ 1-6~ ou amino; e no caso de -Aser diferente de alcanodiila C~ 1-6~ então R~ 6~ pode também ser alquila C~ 1-6~, Het^ 1^ C~ 1-4~alquila, Het^ 1^O C~ 1-4~ alquila, Het^ 2^ C~ 1-4~alquila, Het^ 2^O C~ 1-4~ alquila, aril C~ 1-4~ alquila, arila0 C~ 1-4~ alquila ou amino C~ 1-4~ alquila; por meio do qual cada um dos grupos de amino na definição de R~ 6~, pode opcionalmente ser substituído; -A-R~ 6~ é hidróxi C~ 1-6~ alquila; R~ 5~ e -A-R~ 6~ tomados juntos com o átomo de nitrogênio ao qual eles são ligados podem também formar Het^ 1^ ou Het^ 2^. Ainda diz respeito a seu uso como inibidores da HIV protease de amplo espectro, processos para a sua preparação, assim como composições farmacêuticas e kits de diagnóstico compreendendo-as. Também diz respeito a combinações destas com outro agente anti-retroviral, e a seu uso em ensaios como compostos de referência ou como reagentes.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP01201308 | 2001-04-09 | ||
US28770401P | 2001-05-02 | 2001-05-02 | |
PCT/EP2002/004012 WO2002081478A2 (en) | 2001-04-09 | 2002-04-09 | Broadspectrum 2-(substituted-amino)-benzoxazole sulfonamide hiv protease inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
BR0208796A true BR0208796A (pt) | 2004-03-09 |
Family
ID=26076876
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR0208796-0A BR0208796A (pt) | 2001-04-09 | 2002-04-09 | Inibidores 2-(amino substituìdo)-benzoxazol sulfonamida hiv protease de amplo espectro |
Country Status (25)
Country | Link |
---|---|
US (2) | US7244752B2 (pt) |
EP (1) | EP1397367A2 (pt) |
JP (1) | JP4417010B2 (pt) |
KR (1) | KR100872029B1 (pt) |
CN (1) | CN100491360C (pt) |
AP (1) | AP1544A (pt) |
AR (1) | AR035819A1 (pt) |
AU (1) | AU2002257774B2 (pt) |
BG (1) | BG66371B1 (pt) |
BR (1) | BR0208796A (pt) |
CA (1) | CA2442870C (pt) |
CZ (1) | CZ303139B6 (pt) |
EA (1) | EA007383B1 (pt) |
EE (1) | EE05384B1 (pt) |
HR (1) | HRP20030905B1 (pt) |
HU (1) | HUP0303744A3 (pt) |
IL (1) | IL158092A0 (pt) |
MX (1) | MXPA03009179A (pt) |
NO (1) | NO328896B1 (pt) |
NZ (1) | NZ528954A (pt) |
OA (1) | OA12464A (pt) |
PL (1) | PL367084A1 (pt) |
SK (1) | SK288232B6 (pt) |
WO (1) | WO2002081478A2 (pt) |
ZA (1) | ZA200307683B (pt) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AP1544A (en) * | 2001-04-09 | 2006-01-12 | Tibotec Pharm Ltd | Broadspectrum 2- (substituted-amino) -benzoxazole sulfonamide HIV protease inhibitors. |
EA009590B1 (ru) * | 2001-05-11 | 2008-02-28 | Тиботек Фармасьютикалз Лтд. | 2-аминобензоксазолсульфонамидные ингибиторы вич-протеазы широкого спектра |
US7285566B2 (en) * | 2002-01-07 | 2007-10-23 | Erickson John W | Resistance-repellent retroviral protease inhibitors |
US7109230B2 (en) | 2002-01-07 | 2006-09-19 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
US7157489B2 (en) | 2002-03-12 | 2007-01-02 | The Board Of Trustees Of The University Of Illinois | HIV protease inhibitors |
ATE371652T1 (de) * | 2002-05-17 | 2007-09-15 | Tibotec Pharm Ltd | Substituierte benzisoxazolsulfonamide mit breitbändiger hiv-protease hemmender wirkung |
JP2007528423A (ja) * | 2004-03-11 | 2007-10-11 | セコイア、ファーマシューティカルズ、インコーポレイテッド | 耐性防止レトロウイルスプロテアーゼ阻害薬 |
JP5073480B2 (ja) * | 2004-05-07 | 2012-11-14 | セコイア、ファーマシューティカルズ、インコーポレイテッド | 耐性防止レトロウイルスプロテアーゼ阻害薬 |
WO2006089942A1 (en) | 2005-02-25 | 2006-08-31 | Tibotec Pharmaceuticals Ltd. | Protease inhibitor precursor synthesis |
DE102010044584A1 (de) * | 2010-09-07 | 2012-03-08 | Kautex Textron Gmbh & Co. Kg | Kraftstoffbehälter aus thermoplastischem Kunststoff |
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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US4448192A (en) | 1982-03-05 | 1984-05-15 | Hewlett Packard Company | Medical ventilator device parametrically controlled for patient ventilation |
IT1185906B (it) | 1985-09-13 | 1987-11-18 | Luciano Gattinoni | Sistema ed apparecchio biomedicale per la misurazione con precisione dei valori di variazione di pressione e volume nei polmoni di un paziente |
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DE3919840A1 (de) | 1989-06-17 | 1991-01-17 | Hoechst Ag | Verfahren zur herstellung von aromatischen sulfonsaeurechloriden |
ATE141635T1 (de) | 1990-03-09 | 1996-09-15 | Milliken Res Corp | Organische materialien, die sulfonamidogebundene poly(oxyalkylen)gruppen tragen und ihre herstellung |
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CZ300031B6 (cs) * | 1999-10-06 | 2009-01-14 | Tibotec Pharmaceuticals Ltd. | Hexahydrofuro[2,3-b]furan-3-yl-N-{3-[(1,3-benzodioxol-5-ylsulfonyl) (isobutyl)amino]-1-benzyl-2-hydroxypropyl}karbamát a farmaceutický prípravek s jeho obsahem |
AP1544A (en) * | 2001-04-09 | 2006-01-12 | Tibotec Pharm Ltd | Broadspectrum 2- (substituted-amino) -benzoxazole sulfonamide HIV protease inhibitors. |
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2002
- 2002-04-09 AP APAP/P/2003/002882A patent/AP1544A/en active
- 2002-04-09 CN CNB028114809A patent/CN100491360C/zh not_active Expired - Fee Related
- 2002-04-09 CZ CZ20032936A patent/CZ303139B6/cs not_active IP Right Cessation
- 2002-04-09 SK SK1339-2003A patent/SK288232B6/sk not_active IP Right Cessation
- 2002-04-09 AU AU2002257774A patent/AU2002257774B2/en not_active Ceased
- 2002-04-09 PL PL02367084A patent/PL367084A1/xx unknown
- 2002-04-09 HU HU0303744A patent/HUP0303744A3/hu unknown
- 2002-04-09 EP EP02727554A patent/EP1397367A2/en not_active Withdrawn
- 2002-04-09 JP JP2002579466A patent/JP4417010B2/ja not_active Expired - Fee Related
- 2002-04-09 AR ARP020101301A patent/AR035819A1/es not_active Application Discontinuation
- 2002-04-09 EA EA200301110A patent/EA007383B1/ru not_active IP Right Cessation
- 2002-04-09 IL IL15809202A patent/IL158092A0/xx not_active IP Right Cessation
- 2002-04-09 CA CA2442870A patent/CA2442870C/en not_active Expired - Fee Related
- 2002-04-09 MX MXPA03009179A patent/MXPA03009179A/es active IP Right Grant
- 2002-04-09 NZ NZ528954A patent/NZ528954A/en not_active IP Right Cessation
- 2002-04-09 KR KR1020037013144A patent/KR100872029B1/ko not_active IP Right Cessation
- 2002-04-09 US US10/474,162 patent/US7244752B2/en not_active Expired - Fee Related
- 2002-04-09 OA OA1200300253A patent/OA12464A/en unknown
- 2002-04-09 BR BR0208796-0A patent/BR0208796A/pt not_active IP Right Cessation
- 2002-04-09 EE EEP200300494A patent/EE05384B1/xx not_active IP Right Cessation
- 2002-04-09 WO PCT/EP2002/004012 patent/WO2002081478A2/en active IP Right Grant
-
2003
- 2003-10-01 BG BG108218A patent/BG66371B1/bg unknown
- 2003-10-01 ZA ZA2003/07683A patent/ZA200307683B/en unknown
- 2003-10-08 NO NO20034505A patent/NO328896B1/no not_active IP Right Cessation
- 2003-11-07 HR HR20030905A patent/HRP20030905B1/xx not_active IP Right Cessation
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2007
- 2007-01-23 US US11/626,183 patent/US7595334B2/en not_active Expired - Fee Related
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Owner name: TIBOTEC PHARMACEUTICALS LTD. (IE) Free format text: SEDE ALTERADA CONFORME SOLICITADO NA PETICAO NO 020070001806/RJ DE 05/01/2007. |
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B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
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B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
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