EA201001508A1 - Мостиковые гетероциклические соединения в качестве ингибиторов интегразы вич - Google Patents
Мостиковые гетероциклические соединения в качестве ингибиторов интегразы вичInfo
- Publication number
- EA201001508A1 EA201001508A1 EA201001508A EA201001508A EA201001508A1 EA 201001508 A1 EA201001508 A1 EA 201001508A1 EA 201001508 A EA201001508 A EA 201001508A EA 201001508 A EA201001508 A EA 201001508A EA 201001508 A1 EA201001508 A1 EA 201001508A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- bridges
- hiv integrase
- heterocyclic compounds
- integrase inhibitors
- hiv
- Prior art date
Links
- 229940099797 HIV integrase inhibitor Drugs 0.000 title 1
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 239000003084 hiv integrase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000030507 AIDS Diseases 0.000 abstract 1
- 108010002459 HIV Integrase Proteins 0.000 abstract 1
- 241000700605 Viruses Species 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
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
Данное изобретение в общем относится к новьм соединениям формулы I, включая их соли, которые ингибируют интегразу ВИЧ и предотвращают интеграцию вирусов в человеческую ДНК. Этот механизм делает соединения полезными для лечения ВИЧ-инфекции и СПИДа. Данное изобретение охватывает также фармацевтические композиции и способы лечения больных, инфицированных ВИЧ.
Applications Claiming Priority (3)
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 |
PCT/US2009/037596 WO2009117540A1 (en) | 2008-03-19 | 2009-03-19 | Bridged heterocycles as hiv integrase inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
EA201001508A1 true EA201001508A1 (ru) | 2011-04-29 |
Family
ID=40863725
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201001508A EA201001508A1 (ru) | 2008-03-19 | 2009-03-19 | Мостиковые гетероциклические соединения в качестве ингибиторов интегразы вич |
Country Status (15)
Country | Link |
---|---|
US (1) | US8129398B2 (ru) |
EP (1) | EP2280981B8 (ru) |
JP (1) | JP2011515412A (ru) |
KR (1) | KR20100137522A (ru) |
CN (1) | CN102036996A (ru) |
AU (1) | AU2009225577A1 (ru) |
BR (1) | BRPI0910307A2 (ru) |
CA (1) | CA2718950A1 (ru) |
CO (1) | CO6331439A2 (ru) |
EA (1) | EA201001508A1 (ru) |
IL (1) | IL208068A0 (ru) |
MX (1) | MX2010009995A (ru) |
NZ (1) | NZ588031A (ru) |
WO (1) | WO2009117540A1 (ru) |
ZA (1) | ZA201006589B (ru) |
Families Citing this family (48)
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JP2012516333A (ja) * | 2009-01-28 | 2012-07-19 | 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の架橋化合物 |
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 |
JP6266978B2 (ja) | 2010-08-10 | 2018-01-24 | 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 | 環状ボロン酸エステル誘導体およびその治療的使用 |
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 |
US9012491B2 (en) | 2011-08-31 | 2015-04-21 | 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 |
CA3012242C (en) | 2012-12-21 | 2021-11-02 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
US9101638B2 (en) | 2013-01-04 | 2015-08-11 | 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 |
WO2014107536A1 (en) | 2013-01-04 | 2014-07-10 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
US9642869B2 (en) | 2013-01-04 | 2017-05-09 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
RU2737434C2 (ru) | 2013-03-13 | 2020-11-30 | Форма Терапьютикс, Инк. | Новые соединения и композиции для ингибирования 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 |
NO2865735T3 (ru) | 2013-07-12 | 2018-07-21 | ||
JP6411491B2 (ja) | 2013-07-12 | 2018-10-24 | ギリアード サイエンシス インコーポレーテッド | 多環式カルバモイルピリドン化合物およびhiv感染症を処置するためのその使用 |
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 |
LT3140310T (lt) | 2014-05-05 | 2019-11-25 | Rempex Pharmaceuticals Inc | Boronato druskų sintezė ir jų panaudojimas |
WO2015171398A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
BR112016026291A2 (pt) | 2014-05-19 | 2017-08-15 | Rempex Pharmaceuticals Inc | Derivados do ácido borônico e usos terapêuticos dos mesmos |
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 |
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 (ru) | 2014-06-20 | 2018-06-23 | ||
KR20170024087A (ko) | 2014-07-01 | 2017-03-06 | 렘펙스 파머수티클스 인코퍼레이티드 | 보론산 유도체 및 그의 치료적 용도 |
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 |
WO2016154081A1 (en) | 2015-03-26 | 2016-09-29 | Merck Sharp & Dohme Corp. | Pyrazolyl pyrimidinone compounds as pde2 inhibitors |
AU2016244035B2 (en) | 2015-04-02 | 2018-11-01 | 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 |
WO2017059120A1 (en) * | 2015-09-30 | 2017-04-06 | Gilead Sciences, Inc. | Compounds and combinations for the treatment of hiv |
CA3026582A1 (en) | 2016-06-30 | 2018-01-04 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
MX2020003495A (es) | 2017-10-11 | 2020-09-18 | Qpex Biopharma Inc | Derivados de acido boronico y sintesis de los mismos. |
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 |
CA3166480A1 (en) | 2020-02-24 | 2021-09-02 | Lan Jiang | Tetracyclic compounds for treating hiv infection |
PE20231297A1 (es) | 2021-01-19 | 2023-08-22 | Gilead Sciences Inc | Compuestos de piridotriazina sustituidos y usos de estos |
Family Cites Families (17)
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WO2004058757A1 (en) * | 2002-12-27 | 2004-07-15 | 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 |
US7192948B2 (en) | 2004-05-28 | 2007-03-20 | 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 |
US7176196B2 (en) * | 2004-05-28 | 2007-02-13 | 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 |
EP1866313A1 (en) | 2005-03-31 | 2007-12-19 | Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. | Hiv integrase inhibitors |
US7741315B2 (en) | 2005-05-10 | 2010-06-22 | Merck Sharp & Dohme Corp. | 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 |
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 |
JP2012516333A (ja) * | 2009-01-28 | 2012-07-19 | 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の架橋化合物 |
-
2009
- 2009-03-18 US US12/406,268 patent/US8129398B2/en active Active
- 2009-03-19 EA EA201001508A patent/EA201001508A1/ru unknown
- 2009-03-19 NZ NZ588031A patent/NZ588031A/en 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 KR KR1020107023261A patent/KR20100137522A/ko not_active Application Discontinuation
- 2009-03-19 AU AU2009225577A patent/AU2009225577A1/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 CA CA2718950A patent/CA2718950A1/en not_active Abandoned
- 2009-03-19 JP JP2011500942A patent/JP2011515412A/ja active Pending
- 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 |
---|---|
CO6331439A2 (es) | 2011-10-20 |
US20090253677A1 (en) | 2009-10-08 |
KR20100137522A (ko) | 2010-12-30 |
MX2010009995A (es) | 2010-09-30 |
AU2009225577A1 (en) | 2009-09-24 |
ZA201006589B (en) | 2012-02-29 |
NZ588031A (en) | 2011-12-22 |
WO2009117540A1 (en) | 2009-09-24 |
EP2280981B8 (en) | 2014-09-17 |
EP2280981A1 (en) | 2011-02-09 |
CN102036996A (zh) | 2011-04-27 |
US8129398B2 (en) | 2012-03-06 |
BRPI0910307A2 (pt) | 2019-09-24 |
EP2280981B1 (en) | 2014-04-23 |
IL208068A0 (en) | 2010-12-30 |
CA2718950A1 (en) | 2009-09-24 |
JP2011515412A (ja) | 2011-05-19 |
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