ES2446720T3 - Inhibidores de la integrasa macrocíclica - Google Patents
Inhibidores de la integrasa macrocíclica Download PDFInfo
- Publication number
- ES2446720T3 ES2446720T3 ES10772998.0T ES10772998T ES2446720T3 ES 2446720 T3 ES2446720 T3 ES 2446720T3 ES 10772998 T ES10772998 T ES 10772998T ES 2446720 T3 ES2446720 T3 ES 2446720T3
- Authority
- ES
- Spain
- Prior art keywords
- mmol
- naphthyridine
- methyl
- mixture
- compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- 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
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
- C07D513/18—Bridged 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- 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
- 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
-
- 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
- C07D498/22—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 four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
- C07D515/18—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Epidemiology (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 (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09172853 | 2009-10-13 | ||
| EP09172853 | 2009-10-13 | ||
| PCT/EP2010/065300 WO2011045330A1 (en) | 2009-10-13 | 2010-10-13 | Macrocyclic integrase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2446720T3 true ES2446720T3 (es) | 2014-03-10 |
Family
ID=41720665
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES10772998.0T Active ES2446720T3 (es) | 2009-10-13 | 2010-10-13 | Inhibidores de la integrasa macrocíclica |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8497270B2 (pt-PT) |
| EP (1) | EP2488521B1 (pt-PT) |
| JP (1) | JP5624148B2 (pt-PT) |
| KR (1) | KR20120087916A (pt-PT) |
| CN (1) | CN102574854B (pt-PT) |
| AU (1) | AU2010305805B2 (pt-PT) |
| BR (1) | BR112012008586A2 (pt-PT) |
| CA (1) | CA2777664C (pt-PT) |
| EA (1) | EA019558B1 (pt-PT) |
| ES (1) | ES2446720T3 (pt-PT) |
| IL (1) | IL218845A0 (pt-PT) |
| MX (1) | MX2012004426A (pt-PT) |
| NZ (1) | NZ598766A (pt-PT) |
| WO (1) | WO2011045330A1 (pt-PT) |
| ZA (1) | ZA201202516B (pt-PT) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2487176A1 (en) * | 2011-02-14 | 2012-08-15 | Elanco Animal Health Ireland Limited | Macrocyclic integrase inhibitors for use in the treatment of feline immunodeficiency virus |
| WO2014008636A1 (en) * | 2012-07-11 | 2014-01-16 | Merck Sharp & Dohme Corp. | Macrocyclic compounds as hiv integrase inhibitors |
| US9714243B2 (en) | 2012-12-17 | 2017-07-25 | 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 |
| ME02977B (me) | 2013-05-17 | 2018-10-20 | Merck Sharp & Dohme | Fuzionisana triciklicna heterociklicna jedinjenja као inhibiтori hiv integraze |
| US9951079B2 (en) | 2013-06-13 | 2018-04-24 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as HIV integrase inhibitors |
| WO2015048363A1 (en) | 2013-09-27 | 2015-04-02 | Merck Sharp & Dohme Corp. | Substituted quinolizine derivatives useful as hiv integrase inhibitors |
| WO2016187788A1 (en) | 2015-05-25 | 2016-12-01 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds useful for treating hiv infection |
| ES2864839T3 (es) * | 2015-07-02 | 2021-10-14 | Turning Point Therapeutics Inc | Macrociclos de diarilo quirales como moduladores de proteína quinasas |
| CN108026109B (zh) | 2015-07-21 | 2021-03-02 | 特普医药公司 | 手性二芳基大环及其用途 |
| WO2017087257A1 (en) | 2015-11-17 | 2017-05-26 | Merck Sharp & Dohme Corp. | Amido-substituted pyridotriazine derivatives useful as hiv integrase inhibitors |
| EP3389380B1 (en) | 2015-12-15 | 2021-07-21 | 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 |
| RU2749043C2 (ru) | 2016-12-02 | 2021-06-03 | Мерк Шарп И Доум Корп. | Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич |
| 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) |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| EP3573984A4 (en) | 2017-01-26 | 2020-07-29 | Merck Sharp & Dohme Corp. | USEFUL SUBSTITUTE QUINOLIZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS |
| JP7224334B2 (ja) | 2017-07-28 | 2023-02-17 | ターニング・ポイント・セラピューティクス・インコーポレイテッド | 大環式化合物およびその使用 |
| ES2929467T3 (es) | 2017-12-19 | 2022-11-29 | Turning Point Therapeutics Inc | Compuestos macrocíclicos para tratar enfermedades |
| LT3938047T (lt) | 2019-03-22 | 2022-10-10 | Gilead Sciences, Inc. | Tilteliniai tricikliniai karbamoilpiridono junginiai ir jų naudojimas farmacijoje |
| JP7453399B2 (ja) | 2020-02-24 | 2024-03-19 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｉｖ感染症を治療するための四環式化合物及びその使用 |
| CN112358477A (zh) * | 2020-11-10 | 2021-02-12 | 牡丹江医学院 | 一种用于治疗胆囊炎的药物及其制备方法 |
| KR20230134529A (ko) | 2021-01-19 | 2023-09-21 | 길리애드 사이언시즈, 인코포레이티드 | 치환된 피리도트리아진 화합물 및 이의 용도 |
| TW202400172A (zh) | 2022-04-06 | 2024-01-01 | 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 (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CS210880B1 (cs) | 1979-10-19 | 1982-01-29 | Jiri Krepelka | Substituované imidy kyselin 4-arylnaftalen-2,3-dikarboxylových |
| CS225002B1 (cs) | 1980-12-12 | 1984-02-13 | Krepelka Jiri | Deriváty 9-fenyl-1H-benzo/f/isoindol-1,3-dionu a způsob jejich výroby |
| JPH04217684A (ja) | 1990-05-30 | 1992-08-07 | Shionogi & Co Ltd | アルド−ス還元酵素阻害物質 |
| US5760065A (en) * | 1994-09-13 | 1998-06-02 | Kyowa Hakko Kogyo Co., Ltd. | Anti-HIV agent |
| AU1532802A (en) | 2000-10-12 | 2002-04-22 | Merck & Co Inc | Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors |
| US6841558B2 (en) | 2000-10-12 | 2005-01-11 | Merck & Co., Inc. | Aza-and polyaza-naphthalenyl carboxamides useful as HIV intergrase inhibitors |
| WO2002036734A2 (en) | 2000-10-12 | 2002-05-10 | Merck & Co., Inc. | Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors |
| ATE430745T1 (de) * | 2000-10-12 | 2009-05-15 | Merck & Co Inc | Aza- und polyaza naphthalenyl karboxamide als inhibitoren der hiv-integrase |
| WO2004035577A2 (en) | 2002-10-16 | 2004-04-29 | Gilead Sciences, Inc. | Pre-organized tricyclic integrase inhibitor compounds |
| CZ2004764A3 (cs) | 2002-11-20 | 2005-02-16 | Japan Tobacco Inc | 4-Oxochinolinová sloučenina a její použití jako inhibitoru HIV-integrázy |
| KR20050087865A (ko) | 2002-12-27 | 2005-08-31 | 이스티투토 디 리세르쉐 디 비올로지아 몰레콜라레 피. 안젤레티에스.피.에이. | ＨＩＶ 인테그라제 억제제로서 유용한테트라하이드로-4Ｈ-피리도[1,2-ａ]피리미딘 및 관련화합물 |
| US6890942B2 (en) | 2003-05-16 | 2005-05-10 | Bristol-Myers Squibb Company | Acyl sulfonamides as inhibitors of HIV integrase |
| ATE433974T1 (de) | 2003-09-19 | 2009-07-15 | Gilead Sciences Inc | Azachinolinolphosphonatverbindungen als integraseinhibitoren |
| CN1930161A (zh) | 2004-03-09 | 2007-03-14 | P·安杰莱蒂分子生物学研究所 | Hiv整合酶抑制剂 |
| US7176196B2 (en) | 2004-05-28 | 2007-02-13 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| LT3284520T (lt) | 2005-04-28 | 2019-09-25 | Viiv Healthcare Company | Policiklinis karbamoilpiridono darinys, turintis živ integrazę slopinantį poveikį |
| US20080214527A1 (en) * | 2005-08-04 | 2008-09-04 | Takashi Kawasuji | Hiv Integrase Inhibitors |
| KR20080064182A (ko) * | 2005-10-27 | 2008-07-08 | 시오노기세야쿠 가부시키가이샤 | Ｈｉｖ 인테그라아제 억제활성을 가지는 다환성카르바모일피리돈 유도체 |
| US8039458B2 (en) * | 2005-11-17 | 2011-10-18 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| TW200811153A (en) | 2006-06-23 | 2008-03-01 | Japan Tobacco Inc | 6-(heterocyclyl-substituted benzyl)-4-oxoquinoline compound and use thereof as HIV integrase inhibitor |
| ES2424982T3 (es) * | 2008-03-10 | 2013-10-10 | Janssen Pharmaceutica, N.V. | 4-Aril-2-anilino-pirimidinas como inhibidores de cinasas PLK |
-
2010
- 2010-10-13 CN CN201080046163.3A patent/CN102574854B/zh active Active
- 2010-10-13 CA CA2777664A patent/CA2777664C/en active Active
- 2010-10-13 EA EA201270540A patent/EA019558B1/ru not_active IP Right Cessation
- 2010-10-13 NZ NZ598766A patent/NZ598766A/xx not_active IP Right Cessation
- 2010-10-13 BR BR112012008586A patent/BR112012008586A2/pt not_active IP Right Cessation
- 2010-10-13 KR KR1020127009345A patent/KR20120087916A/ko active IP Right Grant
- 2010-10-13 EP EP10772998.0A patent/EP2488521B1/en active Active
- 2010-10-13 JP JP2012533614A patent/JP5624148B2/ja active Active
- 2010-10-13 AU AU2010305805A patent/AU2010305805B2/en active Active
- 2010-10-13 WO PCT/EP2010/065300 patent/WO2011045330A1/en active Application Filing
- 2010-10-13 MX MX2012004426A patent/MX2012004426A/es active IP Right Grant
- 2010-10-13 US US13/395,891 patent/US8497270B2/en active Active
- 2010-10-13 ES ES10772998.0T patent/ES2446720T3/es active Active
-
2012
- 2012-03-26 IL IL218845A patent/IL218845A0/en unknown
- 2012-04-05 ZA ZA2012/02516A patent/ZA201202516B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011045330A1 (en) | 2011-04-21 |
| CN102574854B (zh) | 2014-04-16 |
| IL218845A0 (en) | 2012-06-28 |
| EA019558B1 (ru) | 2014-04-30 |
| BR112012008586A2 (pt) | 2016-11-29 |
| CA2777664A1 (en) | 2011-04-21 |
| NZ598766A (en) | 2013-09-27 |
| EP2488521A1 (en) | 2012-08-22 |
| JP5624148B2 (ja) | 2014-11-12 |
| US20120172367A1 (en) | 2012-07-05 |
| MX2012004426A (es) | 2012-07-30 |
| EP2488521B1 (en) | 2013-12-18 |
| EA201270540A1 (ru) | 2012-09-28 |
| AU2010305805A1 (en) | 2012-04-19 |
| US8497270B2 (en) | 2013-07-30 |
| JP2013507423A (ja) | 2013-03-04 |
| CA2777664C (en) | 2014-06-10 |
| CN102574854A (zh) | 2012-07-11 |
| ZA201202516B (en) | 2013-09-25 |
| AU2010305805B2 (en) | 2014-04-03 |
| KR20120087916A (ko) | 2012-08-07 |
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