BRPI0511623A - heterociclos bicìclicos como inibidores de hiv integrase - Google Patents
heterociclos bicìclicos como inibidores de hiv integraseInfo
- Publication number
- BRPI0511623A BRPI0511623A BRPI0511623-6A BRPI0511623A BRPI0511623A BR PI0511623 A BRPI0511623 A BR PI0511623A BR PI0511623 A BRPI0511623 A BR PI0511623A BR PI0511623 A BRPI0511623 A BR PI0511623A
- Authority
- BR
- Brazil
- Prior art keywords
- hiv integrase
- hiv
- bicyclic heterocycles
- integrase inhibitors
- bicyclic
- Prior art date
Links
- 125000002618 bicyclic heterocycle group Chemical group 0.000 title abstract 2
- 229940099797 HIV integrase inhibitor Drugs 0.000 title 1
- 239000003084 hiv integrase inhibitor Substances 0.000 title 1
- 108010002459 HIV Integrase Proteins 0.000 abstract 2
- 208000030507 AIDS Diseases 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 208000037357 HIV infectious disease Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- -1 cyclic bicyclic pyrimidinone compounds Chemical class 0.000 abstract 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000010354 integration Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000003612 virological effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring 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
-
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
HETEROCICLOS BICìCLICOS COMO INIBIDORES DE HIV INTEGRASE. A invenção abrange uma série de compostos de pirimidinona bicíclicos cíclicos de Fórmula que inibem HIV integrase e impedem integração viral em DNA humano. Esta ação toma os compostos úteis para tratamento de infecção por HIV e AIDS. A invenção também abrange composições farmacêuticas e métodos para tratamento daqueles infetados com HIV.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US57551304P | 2004-05-28 | 2004-05-28 | |
| US60337104P | 2004-08-20 | 2004-08-20 | |
| US11/126,891 US7176196B2 (en) | 2004-05-28 | 2005-05-11 | Bicyclic heterocycles as HIV integrase inhibitors |
| PCT/US2005/016473 WO2005118593A1 (en) | 2004-05-28 | 2005-05-12 | Bicyclic heterocycles as hiv integrase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0511623A true BRPI0511623A (pt) | 2008-03-11 |
Family
ID=35456854
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0511623-6A BRPI0511623A (pt) | 2004-05-28 | 2005-05-12 | heterociclos bicìclicos como inibidores de hiv integrase |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US7176196B2 (pt) |
| EP (1) | EP1749011B1 (pt) |
| JP (1) | JP4874959B2 (pt) |
| KR (1) | KR101097623B1 (pt) |
| AR (1) | AR049124A1 (pt) |
| AT (1) | ATE412656T1 (pt) |
| AU (1) | AU2005250356C1 (pt) |
| BR (1) | BRPI0511623A (pt) |
| CA (1) | CA2568356C (pt) |
| CY (1) | CY1110266T1 (pt) |
| DE (1) | DE602005010690D1 (pt) |
| DK (1) | DK1749011T3 (pt) |
| ES (1) | ES2315875T3 (pt) |
| HR (1) | HRP20090005T3 (pt) |
| IL (1) | IL179455A (pt) |
| MX (1) | MXPA06013835A (pt) |
| NO (1) | NO20065879L (pt) |
| NZ (1) | NZ551282A (pt) |
| PE (1) | PE20060242A1 (pt) |
| PL (1) | PL1749011T3 (pt) |
| PT (1) | PT1749011E (pt) |
| RS (1) | RS50700B (pt) |
| RU (1) | RU2381228C2 (pt) |
| SI (1) | SI1749011T1 (pt) |
| TW (1) | TWI366567B (pt) |
| WO (1) | WO2005118593A1 (pt) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7115601B2 (en) | 2004-05-18 | 2006-10-03 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| CN101146811B (zh) * | 2005-03-31 | 2012-01-11 | P.安杰莱蒂分子生物学研究所 | Hiv整合酶抑制剂 |
| US7494984B2 (en) * | 2005-08-31 | 2009-02-24 | Bristol-Myers Squibb Company | Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors |
| CA2622639C (en) * | 2005-10-04 | 2012-01-03 | Istituto Di Recerche Di Biologia Molecolare P. Angeletti S.P.A. | Hiv integrase inhibitors |
| US7902182B2 (en) * | 2005-11-16 | 2011-03-08 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| WO2007064316A1 (en) * | 2005-11-30 | 2007-06-07 | Bristol-Myers Squibb Company | Bicyclic heterocycles as hiv integrase inhibitors |
| WO2007064502A1 (en) * | 2005-12-01 | 2007-06-07 | Bristol-Myers Squibb Company | Forms of n-[(4-fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide |
| US20070129379A1 (en) * | 2005-12-01 | 2007-06-07 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
| US7897593B2 (en) * | 2006-05-30 | 2011-03-01 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7893055B2 (en) * | 2006-06-28 | 2011-02-22 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| EP2046328A4 (en) * | 2006-07-19 | 2009-10-28 | Univ Georgia Res Found | PYRIDINONE DIKETOIC ACIDS: INHIBITORS OF HIV REPLICATION IN COMBINATION THERAPY |
| US7763630B2 (en) * | 2007-06-06 | 2010-07-27 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US8129398B2 (en) * | 2008-03-19 | 2012-03-06 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| AU2009228254A1 (en) * | 2008-03-27 | 2009-10-01 | Bristol-Myers Squibb Company | Crystalline form of N-[[4-fluoro-2- (5-methyl-1H-1,2,4-triazol-1-yl) phenyl]methyl]-4,6,7,9-tetrahydro-3- hydroxy-9,9-dimethyl-4-oxo-pyrimido [2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate |
| WO2010042392A2 (en) * | 2008-10-06 | 2010-04-15 | Merck & Co., Inc. | Hiv integrase inhibitors |
| US8143244B2 (en) * | 2009-02-26 | 2012-03-27 | Bristol-Myers Squibb Company | Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors |
| WO2011045330A1 (en) | 2009-10-13 | 2011-04-21 | Tibotec Pharmaceuticals | Macrocyclic integrase inhibitors |
| US8383639B2 (en) | 2009-10-15 | 2013-02-26 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| WO2011071849A2 (en) | 2009-12-07 | 2011-06-16 | University Of Georgia Research Foundation, Inc. | Pyridinone hydroxycyclopentyl carboxamides: hiv integrase inhibitors with therapeutic applications |
| PE20121524A1 (es) | 2010-01-27 | 2012-12-03 | Viiv Healthcare Co | Combinaciones de compuestos que comprenden inhibidores de la integrasa de vih y otros agentes terapeuticos |
| RU2567385C2 (ru) | 2010-04-02 | 2015-11-10 | ЯНССЕН Ар ЭНД Ди АЙРЛЭНД | Макроциклические ингибиторы интегразы |
| WO2012007500A2 (de) | 2010-07-15 | 2012-01-19 | Bayer Cropscience Ag | Neue heterocyclische verbindungen als schädlingsbekämpfungsmittel |
| US8791108B2 (en) | 2011-08-18 | 2014-07-29 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| EP4556010A3 (en) | 2011-11-30 | 2025-07-23 | Emory University | Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae |
| EP2807149A2 (en) * | 2012-01-26 | 2014-12-03 | CRO Consulting Limited | Agents for treating neurodegenerative disorders |
| EP2931730B1 (en) | 2012-12-17 | 2019-08-07 | Merck Sharp & Dohme Corp. | 4-pyridinonetriazine derivatives as hiv integrase inhibitors |
| EP2986291B1 (en) | 2013-04-16 | 2020-05-27 | Merck Sharp & Dohme Corp. | 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors |
| AU2014267951A1 (en) | 2013-05-17 | 2015-11-19 | Merck Sharp & Dohme Corp. | Fused Tricyclic Heterocyclic compounds as HIV integrase inhibitors |
| US9951079B2 (en) | 2013-06-13 | 2018-04-24 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as HIV integrase inhibitors |
| MD4794B1 (ro) | 2013-09-27 | 2022-02-28 | Merck Sharp & Dohme Corp | Derivaţi de chinolizină substituiţi utili ca inhibitori de integrază HIV |
| WO2016187788A1 (en) | 2015-05-25 | 2016-12-01 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds useful for treating hiv infection |
| US10548910B2 (en) | 2015-11-17 | 2020-02-04 | Merck Sharp & Dohme Corp. | Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors |
| WO2017106071A1 (en) | 2015-12-15 | 2017-06-22 | Merck Sharp & Dohme Corp. | Spirocyclic quinolizine derivatives useful as hiv integrase inhibitors |
| WO2017113288A1 (en) | 2015-12-31 | 2017-07-06 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
| US10934312B2 (en) | 2016-12-02 | 2021-03-02 | Merck Sharp & Dohme Corp. | Tricyclic heterocycle compounds useful as HIV integrase inhibitors |
| JOP20190130A1 (ar) | 2016-12-02 | 2019-06-02 | Merck Sharp & Dohme | مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv) |
| WO2018140368A1 (en) | 2017-01-26 | 2018-08-02 | Merck Sharp & Dohme Corp. | Substituted quinolizine derivatives useful as hiv integrase inhibitors |
| WO2021050555A1 (en) * | 2019-09-10 | 2021-03-18 | X-Chem, Inc. | Compositions and uses thereof |
| CN113912622B (zh) * | 2020-07-10 | 2023-12-01 | 上海纽思克生物科技有限公司 | 三环嘧啶酮类化合物、其制备方法、其组合物和用途 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5693641A (en) * | 1996-08-16 | 1997-12-02 | Berlex Laboratories Inc. | Bicyclic pyrimidine derivatives and their use as anti-coagulants |
| NZ533057A (en) | 2001-10-26 | 2005-11-25 | Angeletti P Ist Richerche Bio | N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase |
| EP1441734B1 (en) | 2001-10-26 | 2007-02-28 | Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. | Dihydroxypyrimidine carboxamide inhibitors of hiv integrase |
| EP1539762A2 (en) | 2002-06-26 | 2005-06-15 | Bristol-Myers Squibb Company | Bicyclic pyrimidinones as coagulation cascade inhibitors |
| EP1578748B1 (en) | 2002-12-27 | 2010-09-15 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors |
| AR046938A1 (es) | 2003-12-12 | 2006-01-04 | Merck & Co Inc | Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares |
| TW200526635A (en) | 2003-12-22 | 2005-08-16 | Shionogi & Co | Hydroxypyrimidinone derivative having HIV integrase inhibitory activity |
| RU2403066C2 (ru) | 2004-12-03 | 2010-11-10 | Мерк Шарп Энд Домэ Корп | Применение атазанавира для улучшения фармакокинетики лекарственных средств, метаболизируемых ugt1a1 |
| CN101146811B (zh) | 2005-03-31 | 2012-01-11 | P.安杰莱蒂分子生物学研究所 | Hiv整合酶抑制剂 |
-
2005
- 2005-05-11 US US11/126,891 patent/US7176196B2/en not_active Expired - Lifetime
- 2005-05-12 MX MXPA06013835A patent/MXPA06013835A/es active IP Right Grant
- 2005-05-12 RS RSP-2008/0569A patent/RS50700B/sr unknown
- 2005-05-12 SI SI200530481T patent/SI1749011T1/sl unknown
- 2005-05-12 JP JP2007515142A patent/JP4874959B2/ja not_active Expired - Fee Related
- 2005-05-12 ES ES05750075T patent/ES2315875T3/es not_active Expired - Lifetime
- 2005-05-12 HR HR20090005T patent/HRP20090005T3/xx unknown
- 2005-05-12 DE DE602005010690T patent/DE602005010690D1/de not_active Expired - Lifetime
- 2005-05-12 AT AT05750075T patent/ATE412656T1/de active
- 2005-05-12 PT PT05750075T patent/PT1749011E/pt unknown
- 2005-05-12 AU AU2005250356A patent/AU2005250356C1/en not_active Ceased
- 2005-05-12 DK DK05750075T patent/DK1749011T3/da active
- 2005-05-12 EP EP05750075A patent/EP1749011B1/en not_active Expired - Lifetime
- 2005-05-12 WO PCT/US2005/016473 patent/WO2005118593A1/en not_active Ceased
- 2005-05-12 BR BRPI0511623-6A patent/BRPI0511623A/pt not_active IP Right Cessation
- 2005-05-12 NZ NZ551282A patent/NZ551282A/en not_active IP Right Cessation
- 2005-05-12 RU RU2006146970/04A patent/RU2381228C2/ru not_active IP Right Cessation
- 2005-05-12 CA CA2568356A patent/CA2568356C/en not_active Expired - Fee Related
- 2005-05-12 PL PL05750075T patent/PL1749011T3/pl unknown
- 2005-05-25 TW TW094117105A patent/TWI366567B/zh not_active IP Right Cessation
- 2005-05-27 AR ARP050102187A patent/AR049124A1/es not_active Application Discontinuation
- 2005-05-30 PE PE2005000602A patent/PE20060242A1/es not_active Application Discontinuation
-
2006
- 2006-08-16 US US11/505,149 patent/US7511037B2/en not_active Expired - Lifetime
- 2006-11-21 IL IL179455A patent/IL179455A/en not_active IP Right Cessation
- 2006-12-19 NO NO20065879A patent/NO20065879L/no not_active Application Discontinuation
- 2006-12-27 KR KR1020067027455A patent/KR101097623B1/ko not_active Expired - Fee Related
-
2009
- 2009-01-19 CY CY20091100068T patent/CY1110266T1/el unknown
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06T | Formal requirements before examination [chapter 6.20 patent gazette] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] | ||
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |