BRPI0407052A - Inibidores da hiv-integrase, composições farmacêuticas, e métodos para sua utilização - Google Patents
Inibidores da hiv-integrase, composições farmacêuticas, e métodos para sua utilizaçãoInfo
- Publication number
- BRPI0407052A BRPI0407052A BR0407052-6A BRPI0407052A BRPI0407052A BR PI0407052 A BRPI0407052 A BR PI0407052A BR PI0407052 A BRPI0407052 A BR PI0407052A BR PI0407052 A BRPI0407052 A BR PI0407052A
- Authority
- BR
- Brazil
- Prior art keywords
- alkenyl
- alkyl
- alkynyl
- independently selected
- halogen
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 229940099797 HIV integrase inhibitor Drugs 0.000 title 1
- 239000003084 hiv integrase inhibitor Substances 0.000 title 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 108010002459 HIV Integrase Proteins 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- QPVOFYQIOQXCPV-UHFFFAOYSA-N n-hydroxy-9h-pyrido[3,4-b]indole-1-carboxamide Chemical class C12=CC=CC=C2NC2=C1C=CN=C2C(=O)NO QPVOFYQIOQXCPV-UHFFFAOYSA-N 0.000 abstract 2
- 241001103870 Adia Species 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- -1 cyclolalkyl Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Virology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
"INIBIDORES DA HIV-INTEGRASE, COMPOSIçõES FARMACêUTICAS, E MéTODOS PARA SUA UTILIZAçãO". A presente invenção refere-se a compostos de ácido beta-carbolina hidroxâmico representados pela fórmula (1) e fórmula (1b) Ib em que: R~ 1~, R~ 2~, R~ 3~, R~ 4~, R~ 5~ e R~ 6~ são independentemente selecionados de hidrogênio, halogênio, alquila C~ 1~-C~ 6~, alcóxi C~ 1~-C~ 6, alquila, alquenila C~ 2~-C~ 6~, alquinila C~ 2~-C~ 6~, -OR~ c~, -NO~ 2~, e -N(R~ c~)~ 2~, cada R~ c~ é independentemente selecionado de hidrogênio, alquila C~ 1~-C~ 6~, alquenila C~ 2~-C~ 6~, e alquinila C~ 2~-C~ a~; R~ 7~ é alquila C~ 1~-C~ 6~, alquenila C~ 2~-C~ 6~, ou alquenila C~ 2~-C~ 6~ todos dos quais são opcionalmente substituídos por um ou mais substituintes independentemente selecionados de halogênio, alquila C~ 1~-C~ 6~, alquenila C~ 2~-C~ 6~, alquinila C~ 2~-C~ 6~, arila, cicloalquila, heterocicloalquila e heteroarila, em que a dita arila, cicolalquila, e heterocicloalquila são opcionalmente substituídas com um ou mais substituintes independentemente selecionados de halogênio, alquila C~ 1~-C~ 6~, alquenila C~ 2~-C~ 6~, e alquinila C~ 2~-C~ 6~; R~ 8~ e R~ 9~ são independentemente selecionados de hidrogênio, alquila C~ 1~-C~ 6~, alquenila C~ 2~-C~ 6~ e alquinila C~ 2~-C~ 6~, em que a dita alquila, alquenila e alquinila são opcionalmente substituídas com um ou mais substituintes indepedentemente selecionados de halogênio, adia, cicloalquila, heterocicloalquila e grup heteroarila em que a dita arila, cicloalquila, e hterocicloalquila são opcionalmente substituídas com um ou mais substituintes independentemente selecionados de halogênio, alquila C~ 1~-C~ 6~, alquenila C~ 2~-C~ 6~, e alquinila C~ 2~-C~ 6~. Os compostos de ácido beta-carbolina-hidroxâmico e as composições contendo esses compostos podem ser utilizados para inibir ou modular a atividade do enzima integrase do HIV e para tratar doenças e condições mediadas pela integrase do HIV.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US44322303P | 2003-01-27 | 2003-01-27 | |
| PCT/IB2004/000259 WO2004067531A1 (en) | 2003-01-27 | 2004-01-23 | Hiv-integrase inhibitors, pharmaceutical compositions, and methods for their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0407052A true BRPI0407052A (pt) | 2006-01-17 |
Family
ID=32825309
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0407052-6A BRPI0407052A (pt) | 2003-01-27 | 2004-01-23 | Inibidores da hiv-integrase, composições farmacêuticas, e métodos para sua utilização |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US7001912B2 (pt) |
| EP (1) | EP1590349A1 (pt) |
| JP (1) | JP2006516606A (pt) |
| BR (1) | BRPI0407052A (pt) |
| CA (1) | CA2513141A1 (pt) |
| MX (1) | MXPA05007563A (pt) |
| WO (1) | WO2004067531A1 (pt) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PA8586801A1 (es) * | 2002-10-31 | 2005-02-04 | Pfizer | Inhibidores de hiv-integrasa, composiciones farmaceuticas y metodos para su uso |
| MXPA05007563A (es) | 2003-01-27 | 2005-09-21 | Pfizer | Inhibidores de la integrasa del vih, composiciones farmaceuticas y metodos para su uso. |
| CN100503607C (zh) * | 2003-06-02 | 2009-06-24 | 新疆华世丹药物研究有限责任公司 | 去氢骆驼蓬碱衍生物类化合物及其应用 |
| EP1873155A1 (en) * | 2004-04-26 | 2008-01-02 | Pfizer Inc. | Inhibitors of the HIV integrase enzyme |
| ES2292123T3 (es) * | 2004-04-26 | 2008-03-01 | Pfizer Inc. | Inhibidores de la enzima integrasa de vih. |
| BRPI0510319A (pt) * | 2004-04-26 | 2007-10-16 | Pfizer | inibidores da enzima integrase de hiv |
| CA2564372C (en) * | 2004-05-07 | 2011-10-11 | Merck & Co., Inc. | Hiv integrase inhibitors |
| AP2008004400A0 (en) * | 2005-10-07 | 2008-04-30 | Pfizer Prod Inc | Inhibitors of HIV integrase enzyme |
| SG170795A1 (en) * | 2005-12-30 | 2011-05-30 | Gilead Sciences Inc | Methods for improving the pharmacokinetics of hiv integrase inhibitors |
| CL2007003108A1 (es) * | 2006-10-28 | 2008-07-18 | Methylgene Inc Envivo Pharmace | Compuestos derivados de n-hidroxiamida sustituida con heterociclos, inhibidores de histona desacetilasa; composicion farmaceutica que comprende a dichos compuestos; y uso para tratar una enfermedad del grupo que consiste en enfermedad de huntington, |
| US20100256379A1 (en) * | 2007-10-26 | 2010-10-07 | Kagoshima University | Anti-viral agent containing heterocyclic aromatic compound as active ingredient |
| US9151055B2 (en) | 2009-02-25 | 2015-10-06 | Owens Corning Intellectual Capital, Llc | Hip and ridge roofing material |
| US8580294B2 (en) | 2010-10-19 | 2013-11-12 | International Partnership For Microbicides | Platinum-catalyzed intravaginal rings |
| US10137031B2 (en) | 2013-11-14 | 2018-11-27 | International Partnership For Microbicides, Inc. | Combination therapy intravaginal rings |
| CN109369510A (zh) * | 2018-10-31 | 2019-02-22 | 云南大学 | 具有抗hiv活性的双甲氧基取代咔唑类化合物制备及用途 |
| CN116134016A (zh) * | 2020-07-23 | 2023-05-16 | 默克专利股份公司 | 三环杂环 |
| CN119431371A (zh) * | 2024-10-22 | 2025-02-14 | 沈阳药科大学 | 一种β-卡波林3,6,9-位修饰衍生物及其制备方法和用途 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ194747A (en) * | 1979-08-29 | 1988-11-29 | Schering Ag | 9h-pyrido(3,4-b)indol-3-ylcarboxylic acid derivatives |
| GB8720125D0 (en) * | 1987-08-26 | 1987-09-30 | Roussel Lab Ltd | Chemical compounds |
| US6057297A (en) * | 1996-08-06 | 2000-05-02 | Polifarma S.P.A. | Inhibitor compounds of zinc-dependent metalloproteinases associated with pathological conditions, and therapeutic use thereof |
| FR2754262B1 (fr) * | 1996-10-08 | 1998-10-30 | Synthelabo | Derives de 1h-pyrido[3,4-b]indole-4-carboxamide, leur preparation et leur application en therapeutique |
| AU761020B2 (en) * | 1998-06-12 | 2003-05-29 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Beta-carboline compounds |
| EP1209158A1 (en) * | 2000-11-18 | 2002-05-29 | Aventis Pharma Deutschland GmbH | Substituted beta-carbolines |
| IL157638A0 (en) | 2001-03-01 | 2004-03-28 | Shionogi & Co | Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity |
| JP4176477B2 (ja) | 2001-03-01 | 2008-11-05 | 塩野義製薬株式会社 | Ｈｉｖインテグラーゼ阻害活性を有する含窒素芳香族複素環誘導体 |
| JP2003171381A (ja) | 2001-09-25 | 2003-06-20 | Takeda Chem Ind Ltd | エントリー阻害剤 |
| JP2003119137A (ja) | 2001-10-10 | 2003-04-23 | Japan Tobacco Inc | Ｈｉｖ阻害剤 |
| US6933303B2 (en) * | 2001-10-19 | 2005-08-23 | Transtech Pharma, Inc. | Heteroaryl-fused nitrogen heterocycles as therapeutic agents |
| SI1441734T1 (sl) | 2001-10-26 | 2007-08-31 | Angeletti P Ist Richerche Bio | Dihidropirimidin karboksamidni inhibitorji HIV-integraze |
| WO2003047564A1 (en) | 2001-12-05 | 2003-06-12 | Shionogi & Co., Ltd. | Derivative having hiv integrase inhibitory activity |
| CN1617849A (zh) | 2001-12-12 | 2005-05-18 | 布里斯托尔-迈尔斯斯奎布公司 | Hiv整合酶抑制剂 |
| ATE370948T1 (de) | 2002-01-17 | 2007-09-15 | Merck & Co Inc | Hydroxynaphthyridinoncarbonsäureamide, die sich als inhibitoren der hiv-integrase eignen |
| JP4494020B2 (ja) | 2002-03-15 | 2010-06-30 | メルク・シャープ・エンド・ドーム・コーポレイション | Ｈｉｖインテグラーゼ阻害剤として有用なｎ−（置換ベンジル）−８−ヒドロキシ−１，６−ナフチリジン−７−カルボキサミド |
| PA8586801A1 (es) | 2002-10-31 | 2005-02-04 | Pfizer | Inhibidores de hiv-integrasa, composiciones farmaceuticas y metodos para su uso |
| MXPA05007563A (es) | 2003-01-27 | 2005-09-21 | Pfizer | Inhibidores de la integrasa del vih, composiciones farmaceuticas y metodos para su uso. |
-
2004
- 2004-01-23 MX MXPA05007563A patent/MXPA05007563A/es unknown
- 2004-01-23 BR BR0407052-6A patent/BRPI0407052A/pt not_active IP Right Cessation
- 2004-01-23 JP JP2006502388A patent/JP2006516606A/ja not_active Abandoned
- 2004-01-23 CA CA002513141A patent/CA2513141A1/en not_active Abandoned
- 2004-01-23 EP EP04704681A patent/EP1590349A1/en not_active Withdrawn
- 2004-01-23 WO PCT/IB2004/000259 patent/WO2004067531A1/en not_active Ceased
- 2004-01-26 US US10/765,227 patent/US7001912B2/en not_active Expired - Fee Related
-
2005
- 2005-10-14 US US11/251,344 patent/US7138408B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US7001912B2 (en) | 2006-02-21 |
| CA2513141A1 (en) | 2004-08-12 |
| MXPA05007563A (es) | 2005-09-21 |
| WO2004067531A1 (en) | 2004-08-12 |
| US20050165040A1 (en) | 2005-07-28 |
| US20060122211A1 (en) | 2006-06-08 |
| EP1590349A1 (en) | 2005-11-02 |
| JP2006516606A (ja) | 2006-07-06 |
| US7138408B2 (en) | 2006-11-21 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application fees: application dismissed [chapter 8.6 patent gazette] |
Free format text: REFERENTE AS 5A, 6A, 7A E 8A ANUIDADES. |
|
| 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: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2159 DE 22/05/2012. |