BR0305771A - Inibidores de protease do hiv oxindol sulfonamida substituìdos de amplo espectro - Google Patents
Inibidores de protease do hiv oxindol sulfonamida substituìdos de amplo espectroInfo
- Publication number
- BR0305771A BR0305771A BR0305771-2A BR0305771A BR0305771A BR 0305771 A BR0305771 A BR 0305771A BR 0305771 A BR0305771 A BR 0305771A BR 0305771 A BR0305771 A BR 0305771A
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- formula
- het
- cycloalkyl
- protease inhibitors
- Prior art date
Links
Classifications
-
- 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
-
- 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
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
"INIBIDORES DE PROTEASE DO HIV OXINDOL SULFONAMIDA SUBSTITUìDOS DE AMPLO ESPECTRO". A presente invenção refere-se aos compostos que possuem a fórmula (I), a N-óxidos, sais, formas estereoisoméricas, misturas racêmicas, pró-drogas, ésteres e metabólitos dos mesmos, em que R~ 1~ e R~ 8~ são cada um H, opcionalmente C~ 1-6~-alquila, C~ 2-6~-alquenila, C~ 3-7~ cicloalquila, arila, Het^ 1^, Het^ 2^; R^ 1^ pode também ser um radical de fórmula (R~ 11a~R~ 11b~)NC (R~ 10a~ e R~ 10b~)CR~ 9~-; t é 0,1 ou 2; R~ 2~ é H ou C~ 1-6~ alquila; L é -C(=0)-, -O-C(=0)-, -NR~ 8-~ C(=0)-, -O-C~ 1-6~ alcanodiil-C(=0)-, -NR~ 8-~ C~ 1-6~ alcanodiil-C(=0)-, -S(=0)~ 2~2-, -O-S(=0)~ 2~-, -NR~ 8~-S(=0)~ 2~; R~ 3~ é C~ 1-6~ alquila, arila, C~ 3-7~ cicloalquila, C~ 3-7~ cicloalquil C~ 1-4~ alquila ou aril C~ 1-4~ alquila; R~ 4~ é H, C~ 1-4~ alquil OC(=O)-, carboxila, amino C(=O), mono- ou di (C~ 1-4~ alquil) amino C(=O), C~ 3-7~ cicLoalquila, C~ 2-6~ alquenila, C~ 2-6~ alquinila ou C~ 1-6~ alquila opcionalmente substituído; a fórmula (II) é a fórmula (III) ou a fórmula (IV); R~ 5a~, e R~ 5b~ São C~ 2-6~ alquenila, C~ 2-6~ alquinila, C~ 3-7~ cicloalquila OU C~ 1-6~ alquila, opcionalmente substituído sobre um ou mais átomos; R~ 5a~, e R~ 5b~ também podem ser hidrogênio, arila, Het^ 1^, Het^ 2^; R~ 6~ é hidrogênio ou C~ 1-6~ alquila opcionalmente substituído sobre um ou mais átomos de carbono. Ela também refere-se ao seu uso como inibidores de protease do HIV de amplo espectro, a processos para a sua preparação assim como composições farmacêuticas e kits para diagnóstico que compreendem as mesmas. Ela também refere-se a combinações das mesmas com um outro agente retroviral e ao seu uso em dosagens como compostos de referência ou como reagentes.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02078384 | 2002-08-14 | ||
| PCT/EP2003/050379 WO2004016619A1 (en) | 2002-08-14 | 2003-08-14 | Broadspectrum substituted oxindole sulfonamide hiv protease inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0305771A true BR0305771A (pt) | 2004-10-05 |
Family
ID=31725465
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0305771-2A BR0305771A (pt) | 2002-08-14 | 2003-08-14 | Inibidores de protease do hiv oxindol sulfonamida substituìdos de amplo espectro |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7199148B2 (pt) |
| EP (1) | EP1546153A1 (pt) |
| JP (1) | JP4681296B2 (pt) |
| KR (1) | KR100994759B1 (pt) |
| CN (1) | CN1688586B (pt) |
| AP (1) | AP2126A (pt) |
| AU (1) | AU2003262574B2 (pt) |
| BR (1) | BR0305771A (pt) |
| CA (1) | CA2493940C (pt) |
| EA (1) | EA010486B1 (pt) |
| HR (1) | HRP20050606B1 (pt) |
| IL (1) | IL166462A (pt) |
| MX (1) | MXPA05001792A (pt) |
| NO (1) | NO331846B1 (pt) |
| NZ (1) | NZ538714A (pt) |
| PL (1) | PL375307A1 (pt) |
| WO (1) | WO2004016619A1 (pt) |
| ZA (1) | ZA200501223B (pt) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1472536A4 (en) * | 2002-01-07 | 2007-02-14 | Sequoia Pharmaceuticals | VERSATILE INHIBITORS |
| EP1732891A4 (en) * | 2004-03-11 | 2009-05-06 | Sequoia Pharmaceuticals Inc | RESISTANT PREVENTIVE INHIBITORS FOR RETROVIRAL PROTEASES |
| MXPA06012909A (es) * | 2004-05-07 | 2007-09-06 | Sequoia Pharmaceuticals Inc | Inhibidores de proteasa retroviral repelente de resistencia. |
| TWI482775B (zh) | 2008-09-01 | 2015-05-01 | Tibotec Pharm Ltd | 用於製備（３ｒ，３ａｓ，６ａｒ）－六氫呋喃并〔２，３－ｂ〕呋喃－３－基（１ｓ，２ｒ）－３－〔〔（４－胺基苯基）磺醯基〕（異丁基）胺基〕－１－苯甲基－２－羥基丙基胺基甲酸酯之方法 |
| US8921415B2 (en) | 2009-01-29 | 2014-12-30 | Mapi Pharma Ltd. | Polymorphs of darunavir |
| PL2528923T3 (pl) | 2010-01-28 | 2015-01-30 | Mapi Pharma Ltd | Sposób wytwarzania darunawiru i pochodnych darunawiru |
| US8580294B2 (en) | 2010-10-19 | 2013-11-12 | International Partnership For Microbicides | Platinum-catalyzed intravaginal rings |
| WO2012092168A1 (en) * | 2010-12-27 | 2012-07-05 | Purdue Research Foundation | Fused 6,5 bicyclic ring system p2 ligands, and methods for treating hiv |
| WO2012092188A1 (en) * | 2010-12-27 | 2012-07-05 | Ghosh Arun K | Hydrogen bond forming p1 ligands and methods for treating hiv |
| US10137031B2 (en) | 2013-11-14 | 2018-11-27 | International Partnership For Microbicides, Inc. | Combination therapy intravaginal rings |
| EP3192794A4 (en) * | 2014-09-11 | 2018-06-27 | Shionogi & Co., Ltd. | Sustained hiv protease inhibitor |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| 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 |
| US5723490A (en) * | 1992-09-08 | 1998-03-03 | Vertex Pharmaceuticals Incorporated | THF-containing sulfonamide inhibitors of aspartyl protease |
| DK0715618T3 (da) | 1993-08-24 | 1999-08-23 | Searle & Co | Hydroxyethylaminosulfonamider til anvendelse som inhibitorer af retrovirale proteaser |
| IL111080A (en) | 1993-10-01 | 1999-08-17 | Astra Ab | Method for treating a finely divided powder medicament |
| DE69637380T2 (de) * | 1995-01-20 | 2009-09-17 | G.D. Searle Llc, Chicago | 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 |
| CN1149223C (zh) * | 1995-03-10 | 2004-05-12 | G·D·瑟尔公司 | 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 |
| 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 |
| JP2000515488A (ja) | 1995-11-15 | 2000-11-21 | ジー．ディー．サール アンド カンパニー | 置換スルホニルアルカノイルアミノヒドロキシエチルアミノスルホンアミド レトロウイルスプロテアーゼ阻害剤 |
| KR19990044257A (ko) | 1996-05-20 | 1999-06-25 | 디르크 반테 | 생체이용율이 개선된 항진균성 조성물 |
| CZ295502B6 (cs) | 1997-03-26 | 2005-08-17 | Janssen Pharmaceutica N. V. | Antifungální peleta, způsob její přípravy a farmaceutická dávková forma s obsahem těchto pelet |
| EP1042280A2 (en) | 1997-12-24 | 2000-10-11 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| AU2012199A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| WO1999033792A2 (en) | 1997-12-24 | 1999-07-08 | Vertex Pharmaceuticals Incorporated | Prodrugs os aspartyl protease inhibitors |
| US6436989B1 (en) | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
| AP1717A (en) * | 1998-06-19 | 2007-01-30 | Vertex Pharma | Sulfonamide inhibitors of aspartyl protease. |
| WO1999067254A2 (en) | 1998-06-23 | 1999-12-29 | The United States Of America Represented By The Secretary, Department Of Health And Human Services | Multi-drug resistant retroviral protease inhibitors and use thereof |
| ES2362404T5 (es) | 1998-06-23 | 2015-11-25 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Ensayo de aptitud y métodos para reducir la resistencia del VIH a terapia |
| EP1272483A2 (en) * | 2000-03-24 | 2003-01-08 | Millenium Pharmaceuticals, Inc. | OXINDOLE INHIBITORS OF FACTOR Xa |
-
2003
- 2003-08-14 NZ NZ538714A patent/NZ538714A/en not_active IP Right Cessation
- 2003-08-14 WO PCT/EP2003/050379 patent/WO2004016619A1/en active Application Filing
- 2003-08-14 MX MXPA05001792A patent/MXPA05001792A/es active IP Right Grant
- 2003-08-14 BR BR0305771-2A patent/BR0305771A/pt not_active IP Right Cessation
- 2003-08-14 CN CN038240955A patent/CN1688586B/zh not_active Expired - Fee Related
- 2003-08-14 EA EA200500350A patent/EA010486B1/ru not_active IP Right Cessation
- 2003-08-14 PL PL03375307A patent/PL375307A1/xx unknown
- 2003-08-14 CA CA2493940A patent/CA2493940C/en not_active Expired - Fee Related
- 2003-08-14 EP EP03787818A patent/EP1546153A1/en not_active Withdrawn
- 2003-08-14 AP AP2005003245A patent/AP2126A/xx active
- 2003-08-14 JP JP2004528524A patent/JP4681296B2/ja not_active Expired - Fee Related
- 2003-08-14 KR KR1020057001812A patent/KR100994759B1/ko not_active IP Right Cessation
- 2003-08-14 US US10/524,451 patent/US7199148B2/en not_active Expired - Fee Related
- 2003-08-14 AU AU2003262574A patent/AU2003262574B2/en not_active Ceased
-
2005
- 2005-01-24 IL IL166462A patent/IL166462A/en not_active IP Right Cessation
- 2005-02-10 ZA ZA200501223A patent/ZA200501223B/en unknown
- 2005-03-14 NO NO20051291A patent/NO331846B1/no not_active IP Right Cessation
- 2005-06-29 HR HRP20050606AA patent/HRP20050606B1/hr not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| AU2003262574B2 (en) | 2009-07-09 |
| HRP20050606B1 (hr) | 2014-04-25 |
| US20060058368A1 (en) | 2006-03-16 |
| NZ538714A (en) | 2007-03-30 |
| US7199148B2 (en) | 2007-04-03 |
| PL375307A1 (en) | 2005-11-28 |
| ZA200501223B (en) | 2006-07-26 |
| IL166462A (en) | 2012-04-30 |
| CA2493940A1 (en) | 2004-02-26 |
| HRP20050606A2 (en) | 2006-02-28 |
| IL166462A0 (en) | 2006-01-15 |
| WO2004016619A1 (en) | 2004-02-26 |
| EA010486B1 (ru) | 2008-10-30 |
| EA200500350A1 (ru) | 2005-08-25 |
| EP1546153A1 (en) | 2005-06-29 |
| MXPA05001792A (es) | 2005-04-25 |
| NO20051291L (no) | 2005-05-18 |
| KR20050042141A (ko) | 2005-05-04 |
| CA2493940C (en) | 2011-11-22 |
| KR100994759B1 (ko) | 2010-11-16 |
| NO331846B1 (no) | 2012-04-23 |
| AU2003262574A1 (en) | 2004-03-03 |
| CN1688586A (zh) | 2005-10-26 |
| AP2005003245A0 (en) | 2005-03-31 |
| CN1688586B (zh) | 2012-05-09 |
| JP2005537305A (ja) | 2005-12-08 |
| JP4681296B2 (ja) | 2011-05-11 |
| AP2126A (en) | 2010-06-03 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| BR0305771A (pt) | Inibidores de protease do hiv oxindol sulfonamida substituìdos de amplo espectro | |
| BR0207862A (pt) | Inibidores de protease de hiv 2-(amino-substituìda)-benzotiazol-sulfonamida de amplo espectro | |
| BRPI0517343A (pt) | derivados de betulina, preparação destes e uso dos mesmos | |
| AR057325A1 (es) | Sintesis de (s)-n-metilnaltrexona, composiciones farmaceuticas y usos | |
| AR066691A1 (es) | Compuestos espiro heterociclicos derivados de imidazol. composiciones farmaceuticas. | |
| CR7042A (es) | Indanil aminas aciladas y su uso como farmacos | |
| IS2714B (is) | Uppsöfnun í frumu á phosphomate hliðstæðum á HIV próteasa hindrandi efnasamböndum | |
| BR0008582A (pt) | Sais orgânicos e inorgânicos, uso dos mesmos, formulações farmacêuticas para uso oral e parental, e, compostos | |
| BRPI0313286A2 (pt) | Composição e atividade antiviral de derivados de piperazina azaindoloxoacético substituìda | |
| BR0110955A (pt) | Derivados de tropano úteis para a terapia | |
| AR064492A1 (es) | Derivados de isoquinolona sustituidos con cicloalquilamina | |
| AR055959A1 (es) | Derivados espiro para la modulacion de actividad de crth2 | |
| MY148430A (en) | Antibacterial agents | |
| HUP0004421A2 (hu) | Karbamidszármazékok és az ezeket tartalmazó gyógyszerkészítmények, alkalmazásuk az IMPDH-enzim által mediált betegségek gyógyítására | |
| TW200833324A (en) | Sulfonamide derivatives | |
| ATE365740T1 (de) | Substituierte pyrazolopyrimidine | |
| UY27619A1 (es) | Ésteres hidroxamato del ácido n-(4-fenil sustituido)- antranílico | |
| MY145464A (en) | Pyrazolone derivatives as 11-beta hsd1 inhibitors | |
| BR0109547A (pt) | teres difenìlicos utilizados em terapêutica | |
| AR044518A1 (es) | Inhibidores de integrasa de hiv | |
| AP1652A (en) | Broadspectrum 2-amino-benzoxazole sulfonamide HIV protease inhibitors. | |
| HN2011002578A (es) | Nuevos derivados de compuestos de [3,2-c]pirazol esteroidal con actividad clucocorticoide. | |
| BR0307027A (pt) | Compostos derivados de nitróxi de compostos esteróides, uso dos compostos, e, formulações farmacêuticas | |
| UY27263A1 (es) | Nuevas arilsulfonamidas como agentes antivirales | |
| BR0314843A (pt) | Novo composto |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B25G | Requested change of headquarter approved |
Owner name: TIBOTEC PHARMACEUTICALS LTD. (IE) Free format text: SEDE ALTERADA CONFORME SOLICITADO NA PETICAO NO 020070001806/RJ DE 05/01/2007. |
|
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 13A ANUIDADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2385 DE 20-09-2016 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013. |