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)
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 (50)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2010088167A1 (en) * | 2009-01-28 | 2010-08-05 | 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 |
KR102087313B1 (ko) | 2010-08-10 | 2020-03-11 | 렘펙스 파머수티클스 인코퍼레이티드 | 고리형 보론산 에스터 유도체의 제조방법 |
US8835411B2 (en) | 2010-12-10 | 2014-09-16 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
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 |
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 |
PL3067358T3 (pl) | 2012-12-21 | 2020-02-28 | Gilead Sciences, Inc. | Policykliczne związki karbamoilopirydonu i ich zastosowanie farmaceutyczne |
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. |
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 |
BR112015023279B1 (pt) | 2013-03-13 | 2021-01-19 | Forma Therapeutics, Inc. | compostos para inibição de 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 |
DK3019503T3 (da) | 2013-07-12 | 2017-11-20 | Gilead Sciences Inc | Polycykliske-carbamoylpyridon-forbindelser og anvendelse deraf til behandling af hiv-infektioner |
NO2865735T3 (es) | 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 |
EP3087060B1 (en) | 2013-12-23 | 2020-05-13 | Merck Sharp & Dohme Corp. | Pyrimidone carboxamide compounds as pde2 inhibitors |
WO2015171430A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Synthesis of boronate salts and uses thereof |
WO2015171398A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
EP3145936B1 (en) | 2014-05-19 | 2020-09-30 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
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 |
NO2717902T3 (es) | 2014-06-20 | 2018-06-23 | ||
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 |
EA201692301A1 (ru) | 2014-07-01 | 2017-06-30 | Ремпекс Фармасьютикалз, Инк. | Производные бороновой кислоты и их терапевтическое применение |
US10662205B2 (en) | 2014-11-18 | 2020-05-26 | Qpex Biopharma, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
TWI738321B (zh) | 2014-12-23 | 2021-09-01 | 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 |
US10287269B2 (en) | 2015-03-26 | 2019-05-14 | Merck Sharp & Dohme Corp. | Pyrazolyl pyrimidinone compounds as PDE2 inhibitors |
EP3277691B1 (en) | 2015-04-02 | 2019-01-30 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
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 |
EP3356355B1 (en) * | 2015-09-30 | 2020-05-13 | Gilead Sciences, Inc. | Compounds and combinations for the treatment of hiv |
WO2018005662A1 (en) | 2016-06-30 | 2018-01-04 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
KR102626967B1 (ko) | 2017-10-11 | 2024-01-18 | 큐펙스 바이오파마 인코포레이티드 | 보론산 유도체 및 이의 합성 |
US12016868B2 (en) | 2018-04-20 | 2024-06-25 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
EP3873214A4 (en) | 2018-10-29 | 2022-07-13 | 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 |
BR112022015771A2 (pt) | 2020-02-24 | 2022-10-11 | Gilead Sciences Inc | Compostos tetracíclicos para tratar a infecção por hiv |
JP2024503116A (ja) | 2021-01-19 | 2024-01-24 | ギリアード サイエンシーズ, インコーポレイテッド | 置換ピリドトリアジン化合物及びその使用 |
TWI843506B (zh) | 2022-04-06 | 2024-05-21 | 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 |
---|---|---|---|---|
AU2003292437A1 (en) * | 2002-12-27 | 2004-07-22 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa | 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 |
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 |
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 |
AU2006228278C1 (en) | 2005-03-31 | 2011-06-23 | Msd Italia S.R.L. | HIV integrase inhibitors |
WO2006121831A2 (en) | 2005-05-10 | 2006-11-16 | 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 |
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 |
WO2007143446A1 (en) * | 2006-05-30 | 2007-12-13 | Bristol-Myers Squibb Company | Spiro-condensed heterotricyclic compounds as 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 |
WO2010088167A1 (en) * | 2009-01-28 | 2010-08-05 | 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 KR KR1020107023261A patent/KR20100137522A/ko not_active Application Discontinuation
- 2009-03-19 MX MX2010009995A patent/MX2010009995A/es not_active Application Discontinuation
- 2009-03-19 EP EP09722517.1A patent/EP2280981B8/en not_active Not-in-force
- 2009-03-19 EA EA201001508A patent/EA201001508A1/ru unknown
- 2009-03-19 JP JP2011500942A patent/JP2011515412A/ja active Pending
- 2009-03-19 CN CN2009801183261A patent/CN102036996A/zh active Pending
- 2009-03-19 CA CA2718950A patent/CA2718950A1/en not_active Abandoned
- 2009-03-19 NZ NZ588031A patent/NZ588031A/en not_active IP Right Cessation
- 2009-03-19 WO PCT/US2009/037596 patent/WO2009117540A1/en active Application Filing
- 2009-03-19 BR BRPI0910307A patent/BRPI0910307A2/pt 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 |
---|---|
AU2009225577A1 (en) | 2009-09-24 |
EP2280981A1 (en) | 2011-02-09 |
MX2010009995A (es) | 2010-09-30 |
US20090253677A1 (en) | 2009-10-08 |
ZA201006589B (en) | 2012-02-29 |
KR20100137522A (ko) | 2010-12-30 |
CA2718950A1 (en) | 2009-09-24 |
JP2011515412A (ja) | 2011-05-19 |
EP2280981B1 (en) | 2014-04-23 |
CN102036996A (zh) | 2011-04-27 |
EA201001508A1 (ru) | 2011-04-29 |
EP2280981B8 (en) | 2014-09-17 |
US8129398B2 (en) | 2012-03-06 |
WO2009117540A1 (en) | 2009-09-24 |
BRPI0910307A2 (pt) | 2019-09-24 |
NZ588031A (en) | 2011-12-22 |
IL208068A0 (en) | 2010-12-30 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA | Application withdrawn |