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
Abstract
La invención se refiere generalmente a los nuevos compuestos de la fórmula I,incluyendo sus sales, los cuales inhiben VIH integrasa e impiden la integración viral en ADN humano. Esta acción hace a los compuestos útiles para tratar infección por VIH y SIDA. La invención abarca también composiciones farmacéuticas y métodos para tratar a aquellos infectados con VIH.
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 (es) |
EP (1) | EP2280981B8 (es) |
JP (1) | JP2011515412A (es) |
KR (1) | KR20100137522A (es) |
CN (1) | CN102036996A (es) |
AU (1) | AU2009225577A1 (es) |
BR (1) | BRPI0910307A2 (es) |
CA (1) | CA2718950A1 (es) |
CO (1) | CO6331439A2 (es) |
EA (1) | EA201001508A1 (es) |
IL (1) | IL208068A0 (es) |
MX (1) | MX2010009995A (es) |
NZ (1) | NZ588031A (es) |
WO (1) | WO2009117540A1 (es) |
ZA (1) | ZA201006589B (es) |
Families Citing this family (48)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2010208470A1 (en) * | 2009-01-28 | 2011-08-04 | Merck Sharp & Dohme Corp. | Bridged 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 |
MY188960A (en) | 2010-08-10 | 2022-01-14 | Melinta Therapeutics Llc | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
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 |
US8846659B2 (en) | 2010-12-10 | 2014-09-30 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
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 |
MY191741A (en) | 2012-12-21 | 2022-07-13 | Gilead Sciences Inc | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
CN104981239B (zh) | 2013-01-04 | 2019-01-04 | 莱姆派克斯制药公司 | 硼酸衍生物及其治疗用途 |
US9101638B2 (en) | 2013-01-04 | 2015-08-11 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
AU2014204045B2 (en) | 2013-01-04 | 2018-10-18 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
US9241947B2 (en) | 2013-01-04 | 2016-01-26 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
CN105492008B (zh) | 2013-03-13 | 2020-11-27 | 福马治疗股份有限公司 | 用于抑制fasn的化合物及组合物 |
EP2970297A1 (en) * | 2013-03-14 | 2016-01-20 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
NO2865735T3 (es) | 2013-07-12 | 2018-07-21 | ||
HUE037347T2 (hu) | 2013-07-12 | 2018-08-28 | Gilead Sciences Inc | Policiklusos karmaboilpiridon vegyületek és alkalmazásuk HIV fertõzések kezelésére |
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 |
US9815796B2 (en) | 2013-12-23 | 2017-11-14 | Merck Sharp & Dohme Corp. | Pyrimidone carboxamide compounds as PDE2 inhibitors |
SI3140310T1 (sl) | 2014-05-05 | 2020-01-31 | Rempex Pharmaceuticals, Inc. | Sinteza boronatnih soli in njihova uporaba |
WO2015171398A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
JP6672176B2 (ja) | 2014-05-19 | 2020-03-25 | レンペックス・ファーマシューティカルズ・インコーポレイテッド | ボロン酸誘導体およびその治療的使用 |
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 |
TWI744723B (zh) | 2014-06-20 | 2021-11-01 | 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 |
NO2717902T3 (es) | 2014-06-20 | 2018-06-23 | ||
CA2952968A1 (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 |
WO2016145614A1 (en) | 2015-03-17 | 2016-09-22 | Merck Sharp & Dohme Corp. | Triazolyl pyrimidinone compounds as pde2 inhibitors |
WO2016149393A1 (en) | 2015-03-17 | 2016-09-22 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
EP3285581B1 (en) | 2015-03-26 | 2021-08-11 | Merck Sharp & Dohme Corp. | Pyrazolyl pyrimidinone compounds as pde2 inhibitors |
PL3277691T3 (pl) | 2015-04-02 | 2019-07-31 | Gilead Sciences, Inc. | Policykliczne związki karbamoilopirydonowe i ich zastosowanie farmaceutyczne |
WO2016183741A1 (en) * | 2015-05-15 | 2016-11-24 | Merck Sharp & Dohme Corp. | Pyrimidinone amide compounds as pde2 inhibitors |
WO2016209749A1 (en) | 2015-06-25 | 2016-12-29 | 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 |
PL3478693T3 (pl) | 2016-06-30 | 2021-12-13 | Qpex Biopharma, Inc. | Pochodne kwasu boronowego i ich zastosowania terapeutyczne |
CA3078627A1 (en) | 2017-10-11 | 2019-04-18 | Qpex Biopharma, Inc. | Boronic acid derivatives and synthesis 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 |
UA127822C2 (uk) * | 2019-03-22 | 2024-01-10 | Гіліад Сайєнсіз, Інк. | Місткові трициклічні карбамоїлпіридонові сполуки та їх фармацевтичне застосування |
US11697652B2 (en) | 2020-02-24 | 2023-07-11 | Gilead Sciences, Inc. | Tetracyclic compounds and uses thereof |
SI4196479T1 (sl) | 2021-01-19 | 2024-01-31 | Gilead Sciences, Inc. | Substituirane piridotriazinske spojine in njihove uporabe |
Family Cites Families (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BR0317749A (pt) * | 2002-12-27 | 2005-11-22 | Angeletti P Ist Richerche Bio | Composto, composição farmacêutica, e, uso de um composto |
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 |
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 |
US7157447B2 (en) * | 2004-05-28 | 2007-01-02 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
AU2006228278C1 (en) | 2005-03-31 | 2011-06-23 | Msd Italia S.R.L. | HIV integrase inhibitors |
JP4982482B2 (ja) | 2005-05-10 | 2012-07-25 | 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−ゼ阻害剤 |
US7494984B2 (en) * | 2005-08-31 | 2009-02-24 | Bristol-Myers Squibb Company | Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors |
WO2007059125A2 (en) * | 2005-11-15 | 2007-05-24 | 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 |
AU2010208470A1 (en) * | 2009-01-28 | 2011-08-04 | Merck Sharp & Dohme Corp. | Bridged compounds as HIV integrase inhibitors |
-
2009
- 2009-03-18 US US12/406,268 patent/US8129398B2/en active Active
- 2009-03-19 AU AU2009225577A patent/AU2009225577A1/en not_active Abandoned
- 2009-03-19 JP JP2011500942A patent/JP2011515412A/ja active Pending
- 2009-03-19 KR KR1020107023261A patent/KR20100137522A/ko not_active Application Discontinuation
- 2009-03-19 CA CA2718950A patent/CA2718950A1/en not_active Abandoned
- 2009-03-19 MX MX2010009995A patent/MX2010009995A/es not_active Application Discontinuation
- 2009-03-19 WO PCT/US2009/037596 patent/WO2009117540A1/en active Application Filing
- 2009-03-19 EA EA201001508A patent/EA201001508A1/ru unknown
- 2009-03-19 BR BRPI0910307A patent/BRPI0910307A2/pt not_active IP Right Cessation
- 2009-03-19 CN CN2009801183261A patent/CN102036996A/zh active Pending
- 2009-03-19 EP EP09722517.1A patent/EP2280981B8/en not_active Not-in-force
- 2009-03-19 NZ NZ588031A patent/NZ588031A/en not_active IP Right Cessation
-
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 |
---|---|
JP2011515412A (ja) | 2011-05-19 |
EP2280981B8 (en) | 2014-09-17 |
IL208068A0 (en) | 2010-12-30 |
ZA201006589B (en) | 2012-02-29 |
US20090253677A1 (en) | 2009-10-08 |
EP2280981A1 (en) | 2011-02-09 |
EP2280981B1 (en) | 2014-04-23 |
CA2718950A1 (en) | 2009-09-24 |
EA201001508A1 (ru) | 2011-04-29 |
KR20100137522A (ko) | 2010-12-30 |
BRPI0910307A2 (pt) | 2019-09-24 |
AU2009225577A1 (en) | 2009-09-24 |
MX2010009995A (es) | 2010-09-30 |
WO2009117540A1 (en) | 2009-09-24 |
CN102036996A (zh) | 2011-04-27 |
US8129398B2 (en) | 2012-03-06 |
NZ588031A (en) | 2011-12-22 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA | Application withdrawn |