CO6331439A2 - 1-2 bicíclicos pirimidinona carboxamida como inhibidores de la integrasa del virus de inmunodeficiencia humana - Google Patents
1-2 bicíclicos pirimidinona carboxamida como inhibidores de la integrasa del virus de inmunodeficiencia humanaInfo
- Publication number
- CO6331439A2 CO6331439A2 CO10115016A CO10115016A CO6331439A2 CO 6331439 A2 CO6331439 A2 CO 6331439A2 CO 10115016 A CO10115016 A CO 10115016A CO 10115016 A CO10115016 A CO 10115016A CO 6331439 A2 CO6331439 A2 CO 6331439A2
- Authority
- CO
- Colombia
- Prior art keywords
- pirimidinona
- integress
- carboxamida
- bicycles
- inhibitors
- Prior art date
Links
- 241000725303 Human immunodeficiency virus Species 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000030507 AIDS Diseases 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 108010002459 HIV Integrase Proteins 0.000 abstract 1
- 208000037357 HIV infectious disease Diseases 0.000 abstract 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 abstract 1
- 230000010354 integration Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 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
- C07D498/12—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 three hetero rings
- C07D498/18—Bridged 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
-
- 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
- C07D471/08—Bridged systems
-
- 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
- C07D471/12—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 three hetero rings
- C07D471/18—Bridged systems
-
- 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
- C07D487/08—Bridged systems
-
- 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
- C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
- C07D493/18—Bridged systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Tropical Medicine & Parasitology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3772908P | 2008-03-19 | 2008-03-19 | |
| US12/406,268 US8129398B2 (en) | 2008-03-19 | 2009-03-18 | HIV integrase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6331439A2 true CO6331439A2 (es) | 2011-10-20 |
Family
ID=40863725
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO10115016A CO6331439A2 (es) | 2008-03-19 | 2010-09-16 | 1-2 bicíclicos pirimidinona carboxamida como inhibidores de la integrasa del virus de inmunodeficiencia humana |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8129398B2 (https=) |
| EP (1) | EP2280981B8 (https=) |
| JP (1) | JP2011515412A (https=) |
| KR (1) | KR20100137522A (https=) |
| CN (1) | CN102036996A (https=) |
| AU (1) | AU2009225577A1 (https=) |
| BR (1) | BRPI0910307A2 (https=) |
| CA (1) | CA2718950A1 (https=) |
| CO (1) | CO6331439A2 (https=) |
| EA (1) | EA201001508A1 (https=) |
| IL (1) | IL208068A0 (https=) |
| MX (1) | MX2010009995A (https=) |
| NZ (1) | NZ588031A (https=) |
| WO (1) | WO2009117540A1 (https=) |
| ZA (1) | ZA201006589B (https=) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2391212A4 (en) * | 2009-01-28 | 2012-08-08 | BROKEN COMPOUNDS AS HIV INTEGRASE INHIBITORS | |
| US8143244B2 (en) * | 2009-02-26 | 2012-03-27 | Bristol-Myers Squibb Company | Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors |
| US8383639B2 (en) | 2009-10-15 | 2013-02-26 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US8283366B2 (en) | 2010-01-22 | 2012-10-09 | Ambrilia Biopharma, Inc. | Derivatives of pyridoxine for inhibiting HIV integrase |
| CA2807546C (en) | 2010-08-10 | 2022-08-23 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| US8846659B2 (en) | 2010-12-10 | 2014-09-30 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| WO2012077221A1 (ja) * | 2010-12-10 | 2012-06-14 | アグロカネショウ株式会社 | ３-アミノオキサリルアミノベンズアミド誘導体及びこれを有効成分とする殺虫、殺ダニ剤 |
| US8835411B2 (en) * | 2010-12-10 | 2014-09-16 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| CN102675305B (zh) * | 2011-03-08 | 2014-11-12 | 中国科学院上海药物研究所 | 一类咪唑并吡啶类化合物及其制备方法和用途 |
| WO2013033461A1 (en) | 2011-08-31 | 2013-03-07 | Rempex Pharmaceuticals, Inc. | Heterocyclic boronic acid ester derivatives and therapeutic uses thereof |
| US9156858B2 (en) | 2012-05-23 | 2015-10-13 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US10561675B2 (en) | 2012-06-06 | 2020-02-18 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| WO2014008636A1 (en) * | 2012-07-11 | 2014-01-16 | Merck Sharp & Dohme Corp. | Macrocyclic compounds as hiv integrase inhibitors |
| US8906929B2 (en) * | 2012-08-16 | 2014-12-09 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| EA030003B1 (ru) | 2012-12-21 | 2018-06-29 | Джилид Сайэнс, Инк. | Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции |
| US9241947B2 (en) | 2013-01-04 | 2016-01-26 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| KR20150103269A (ko) | 2013-01-04 | 2015-09-09 | 렘펙스 파머수티클스 인코퍼레이티드 | 보론산 유도체 및 그의 치료적 용도 |
| US9101638B2 (en) | 2013-01-04 | 2015-08-11 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| MX2015008627A (es) | 2013-01-04 | 2015-09-23 | Rempex Pharmaceuticals Inc | Derivados de acido boronico y usos terapeuticos de los mismos. |
| SG10201707409PA (en) | 2013-03-13 | 2017-10-30 | Forma Therapeutics Inc | Novel compounds and compositions for inhibition of fasn |
| JP6268656B2 (ja) * | 2013-03-14 | 2018-01-31 | ビーブ・ヘルスケア・ユーケイ・（ナンバー５）・リミテッドＶｉｉＶ Ｈｅａｌｔｈｃａｒｅ ＵＫ （Ｎｏ．５） Ｌｉｍｉｔｅｄ | ヒト免疫不全ウイルス複製の阻害剤 |
| SI3019503T1 (sl) | 2013-07-12 | 2017-11-30 | Gilead Sciences, Inc. | Policiklične karbamoilpiridonske spojine in njihova uporaba za zdravljenje HIV infekcij |
| NO2865735T3 (https=) | 2013-07-12 | 2018-07-21 | ||
| CN103601613B (zh) * | 2013-11-19 | 2015-07-08 | 浙江林江化工股份有限公司 | 一种3,4,5-三氟溴苯的制备方法 |
| WO2015096651A1 (en) | 2013-12-23 | 2015-07-02 | Merck Sharp & Dohme Corp. | Pyrimidone carboxamide compounds as pde2 inhibitors |
| EP3139930B1 (en) | 2014-05-05 | 2024-08-14 | Melinta Therapeutics, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| ES2750805T3 (es) | 2014-05-05 | 2020-03-27 | Rempex Pharmaceuticals Inc | Síntesis de sales de boronato y usos de las mismas |
| AU2015264418A1 (en) | 2014-05-19 | 2016-11-10 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| NO2717902T3 (https=) | 2014-06-20 | 2018-06-23 | ||
| TW201613936A (en) | 2014-06-20 | 2016-04-16 | Gilead Sciences Inc | Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide |
| TWI677489B (zh) | 2014-06-20 | 2019-11-21 | 美商基利科學股份有限公司 | 多環型胺甲醯基吡啶酮化合物之合成 |
| WO2016003929A1 (en) | 2014-07-01 | 2016-01-07 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US10662205B2 (en) | 2014-11-18 | 2020-05-26 | Qpex Biopharma, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| TWI695003B (zh) | 2014-12-23 | 2020-06-01 | 美商基利科學股份有限公司 | 多環胺甲醯基吡啶酮化合物及其醫藥用途 |
| US20180051041A1 (en) | 2015-03-17 | 2018-02-22 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| WO2016145614A1 (en) | 2015-03-17 | 2016-09-22 | Merck Sharp & Dohme Corp. | Triazolyl pyrimidinone compounds as pde2 inhibitors |
| WO2016154081A1 (en) | 2015-03-26 | 2016-09-29 | Merck Sharp & Dohme Corp. | Pyrazolyl pyrimidinone compounds as pde2 inhibitors |
| JP6402259B2 (ja) | 2015-04-02 | 2018-10-10 | ギリアード サイエンシーズ， インコーポレイテッド | 多環式カルバモイルピリドン化合物およびそれらの薬学的使用 |
| WO2016183741A1 (en) | 2015-05-15 | 2016-11-24 | Merck Sharp & Dohme Corp. | Pyrimidinone amide compounds as pde2 inhibitors |
| US10647727B2 (en) | 2015-06-25 | 2020-05-12 | Merck Sharp & Dohme Corp. | Substituted pyrazolo/imidazolo bicyclic compounds as PDE2 inhibitors |
| WO2017000277A1 (en) | 2015-07-01 | 2017-01-05 | Merck Sharp & Dohme Corp. | Substituted triazolo bicycliccompounds as pde2 inhibitors |
| WO2017059120A1 (en) * | 2015-09-30 | 2017-04-06 | Gilead Sciences, Inc. | Compounds and combinations for the treatment of hiv |
| MX389349B (es) | 2016-06-30 | 2025-03-20 | Qpex Biopharma Inc | Derivados de ácido borónico y usos terapéuticos de los mismos. |
| US11286270B2 (en) | 2017-10-11 | 2022-03-29 | Qpex Biopharma, Inc. | Boronic acid derivatives and synthesis thereof |
| EP3781576B1 (en) | 2018-04-20 | 2024-06-12 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US10793554B2 (en) | 2018-10-29 | 2020-10-06 | Forma Therapeutics, Inc. | Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone |
| WO2020197991A1 (en) * | 2019-03-22 | 2020-10-01 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use |
| IL295677B1 (en) | 2020-02-24 | 2026-04-01 | Gilead Sciences Inc | Tetracyclic compounds for the treatment of HIV infection |
| AU2021266715A1 (en) | 2020-05-05 | 2022-11-17 | Qpex Biopharma, Inc. | Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof |
| CA3192145A1 (en) | 2020-09-30 | 2022-04-07 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and uses thereof |
| FI4196479T3 (fi) | 2021-01-19 | 2024-01-17 | Gilead Sciences Inc | Substituoituja pyridotriatsiiniyhdisteitä ja niiden käyttöjä |
| TWI856796B (zh) | 2022-04-06 | 2024-09-21 | 美商基利科學股份有限公司 | 橋聯三環胺甲醯基吡啶酮化合物及其用途 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US7273859B2 (en) * | 2004-05-12 | 2007-09-25 | Bristol-Myers Squibb Company | HIV integrase inhibitors: cyclic pyrimidinone compounds |
| US7173022B2 (en) * | 2004-05-28 | 2007-02-06 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7157447B2 (en) * | 2004-05-28 | 2007-01-02 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7192948B2 (en) * | 2004-05-28 | 2007-03-20 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7176196B2 (en) * | 2004-05-28 | 2007-02-13 | Bristol-Myers Squibb Company | Bicyclic heterocycles as 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 |
| CA2607151C (en) | 2005-05-10 | 2012-06-19 | Merck & Co., Inc. | Hiv integrase inhibitors |
| US7494984B2 (en) * | 2005-08-31 | 2009-02-24 | Bristol-Myers Squibb Company | Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors |
| US7897592B2 (en) * | 2005-11-15 | 2011-03-01 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US8039458B2 (en) * | 2005-11-17 | 2011-10-18 | 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 |
| US7763630B2 (en) * | 2007-06-06 | 2010-07-27 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| EP2391212A4 (en) * | 2009-01-28 | 2012-08-08 | BROKEN COMPOUNDS AS HIV INTEGRASE INHIBITORS |
-
2009
- 2009-03-18 US US12/406,268 patent/US8129398B2/en active Active
- 2009-03-19 EP EP09722517.1A patent/EP2280981B8/en not_active Not-in-force
- 2009-03-19 JP JP2011500942A patent/JP2011515412A/ja active Pending
- 2009-03-19 NZ NZ588031A patent/NZ588031A/en not_active IP Right Cessation
- 2009-03-19 MX MX2010009995A patent/MX2010009995A/es not_active Application Discontinuation
- 2009-03-19 BR BRPI0910307A patent/BRPI0910307A2/pt not_active IP Right Cessation
- 2009-03-19 KR KR1020107023261A patent/KR20100137522A/ko not_active Withdrawn
- 2009-03-19 WO PCT/US2009/037596 patent/WO2009117540A1/en not_active Ceased
- 2009-03-19 CN CN2009801183261A patent/CN102036996A/zh active Pending
- 2009-03-19 EA EA201001508A patent/EA201001508A1/ru unknown
- 2009-03-19 AU AU2009225577A patent/AU2009225577A1/en not_active Abandoned
- 2009-03-19 CA CA2718950A patent/CA2718950A1/en not_active Abandoned
-
2010
- 2010-09-07 IL IL208068A patent/IL208068A0/en unknown
- 2010-09-14 ZA ZA2010/06589A patent/ZA201006589B/en unknown
- 2010-09-16 CO CO10115016A patent/CO6331439A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EP2280981B1 (en) | 2014-04-23 |
| EA201001508A1 (ru) | 2011-04-29 |
| MX2010009995A (es) | 2010-09-30 |
| EP2280981A1 (en) | 2011-02-09 |
| ZA201006589B (en) | 2012-02-29 |
| CN102036996A (zh) | 2011-04-27 |
| NZ588031A (en) | 2011-12-22 |
| US20090253677A1 (en) | 2009-10-08 |
| AU2009225577A1 (en) | 2009-09-24 |
| KR20100137522A (ko) | 2010-12-30 |
| IL208068A0 (en) | 2010-12-30 |
| WO2009117540A1 (en) | 2009-09-24 |
| JP2011515412A (ja) | 2011-05-19 |
| CA2718950A1 (en) | 2009-09-24 |
| BRPI0910307A2 (pt) | 2019-09-24 |
| US8129398B2 (en) | 2012-03-06 |
| EP2280981B8 (en) | 2014-09-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Application withdrawn |