AU2010305805B2 - Macrocyclic integrase inhibitors - Google Patents
Macrocyclic integrase inhibitors Download PDFInfo
- Publication number
- AU2010305805B2 AU2010305805B2 AU2010305805A AU2010305805A AU2010305805B2 AU 2010305805 B2 AU2010305805 B2 AU 2010305805B2 AU 2010305805 A AU2010305805 A AU 2010305805A AU 2010305805 A AU2010305805 A AU 2010305805A AU 2010305805 B2 AU2010305805 B2 AU 2010305805B2
- Authority
- AU
- Australia
- Prior art keywords
- mmol
- methyl
- mixture
- naphthyridine
- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (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 |
|---|---|---|---|
| EP09172853.5 | 2009-10-13 | ||
| EP09172853 | 2009-10-13 | ||
| PCT/EP2010/065300 WO2011045330A1 (en) | 2009-10-13 | 2010-10-13 | Macrocyclic integrase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2010305805A1 AU2010305805A1 (en) | 2012-04-19 |
| AU2010305805B2 true AU2010305805B2 (en) | 2014-04-03 |
Family
ID=41720665
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2010305805A Active AU2010305805B2 (en) | 2009-10-13 | 2010-10-13 | Macrocyclic integrase inhibitors |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8497270B2 (enExample) |
| EP (1) | EP2488521B1 (enExample) |
| JP (1) | JP5624148B2 (enExample) |
| KR (1) | KR20120087916A (enExample) |
| CN (1) | CN102574854B (enExample) |
| AU (1) | AU2010305805B2 (enExample) |
| BR (1) | BR112012008586A2 (enExample) |
| CA (1) | CA2777664C (enExample) |
| EA (1) | EA019558B1 (enExample) |
| ES (1) | ES2446720T3 (enExample) |
| IL (1) | IL218845A0 (enExample) |
| MX (1) | MX2012004426A (enExample) |
| NZ (1) | NZ598766A (enExample) |
| WO (1) | WO2011045330A1 (enExample) |
| ZA (1) | ZA201202516B (enExample) |
Families Citing this family (28)
| 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 |
| EP2931730B1 (en) | 2012-12-17 | 2019-08-07 | 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 |
| AU2014267951A1 (en) | 2013-05-17 | 2015-11-19 | Merck Sharp & Dohme Corp. | Fused Tricyclic Heterocyclic compounds as HIV integrase inhibitors |
| WO2014200880A1 (en) | 2013-06-13 | 2014-12-18 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
| JP6081662B2 (ja) | 2013-09-27 | 2017-02-15 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | Ｈｉｖインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体 |
| PL3097107T3 (pl) | 2014-01-24 | 2020-01-31 | Turning Point Therapeutics, Inc. | Diarylowe związki makrocykliczne jako modulatory kinaz białkowych |
| WO2016187788A1 (en) | 2015-05-25 | 2016-12-01 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds useful for treating hiv infection |
| AU2016287568B2 (en) * | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| HRP20240780T1 (hr) | 2015-07-06 | 2024-09-13 | Turning Point Therapeutics, Inc. | Polimorf diaril makrocikla |
| KR102772574B1 (ko) | 2015-07-21 | 2025-02-24 | 터닝 포인트 테라퓨틱스, 인크. | 키랄 디아릴 매크로사이클 및 이것의 용도 |
| EP3377066B1 (en) | 2015-11-17 | 2021-04-07 | Merck Sharp & Dohme Corp. | Amido-substituted pyridotriazine derivatives useful as hiv integrase inhibitors |
| WO2017106071A1 (en) | 2015-12-15 | 2017-06-22 | 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 |
| 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) |
| RU2749043C2 (ru) | 2016-12-02 | 2021-06-03 | Мерк Шарп И Доум Корп. | Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич |
| 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 |
| SI3728271T1 (sl) | 2017-12-19 | 2023-01-31 | Turning Point Therapeutics, Inc. | Makrociklične spojine za zdravljenje bolezni |
| HUE059677T2 (hu) | 2019-03-22 | 2022-12-28 | Gilead Sciences Inc | Áthidalt triciklusos karbamoilpiridon-vegyületek és ezek gyógyszerészeti alkalmazása |
| CR20220418A (es) | 2020-02-24 | 2022-10-10 | Gilead Sciences Inc | Compuestos tetracíclicos para el tratamiento de infecciones por vih |
| JP7691494B2 (ja) | 2020-09-30 | 2025-06-11 | ギリアード サイエンシーズ， インコーポレイテッド | 架橋三環式カルバモイルピリドン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 |
| LT4196479T (lt) | 2021-01-19 | 2023-12-11 | Gilead Sciences, Inc. | Pakeistieji piridotriazino junginiai ir jų panaudojimo būdai |
| 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 |
| CN115974886A (zh) * | 2022-11-22 | 2023-04-18 | 国科大杭州高等研究院 | 一种含有二氢苯并呋喃骨架的大环内酰胺化合物及其制备方法 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002030931A2 (en) * | 2000-10-12 | 2002-04-18 | Merck & Co., Inc. | Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
Family Cites Families (20)
| 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 |
| WO1996008478A1 (en) * | 1994-09-13 | 1996-03-21 | Kyowa Hakko Kogyo Co., Ltd. | Anti-hiv drug |
| ATE345129T1 (de) | 2000-10-12 | 2006-12-15 | Merck & Co Inc | Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer |
| ES2287170T3 (es) | 2000-10-12 | 2007-12-16 | MERCK & CO., INC. | Aza- y poliaza-naftalenil-carboxamidas utilies como inhibidores de la vih integrasa. |
| US20050010048A1 (en) | 2000-10-12 | 2005-01-13 | Linghang Zhuang | Aza-and polyaza-naphthalenly ketones useful as hiv integrase inhibitors |
| WO2004035577A2 (en) | 2002-10-16 | 2004-04-29 | Gilead Sciences, Inc. | Pre-organized tricyclic integrase inhibitor compounds |
| DE60329318D1 (de) | 2002-11-20 | 2009-10-29 | Japan Tobacco Inc | 4-oxochinolinverbindungen und deren verwendung als hiv-integrase-inhibitoren |
| AU2003292436B2 (en) | 2002-12-27 | 2009-07-30 | Msd Italia S.R.L. | Tetrahydro-4H-pyrido[1,2-A]pyrimidines and related compounds useful as HIV integrase inhibitors |
| US6890942B2 (en) | 2003-05-16 | 2005-05-10 | Bristol-Myers Squibb Company | Acyl sulfonamides as inhibitors of HIV integrase |
| EP1664046B1 (en) | 2003-09-19 | 2009-06-17 | Gilead Sciences, Inc. | Aza-quinolinol phosphonate integrase inhibitor compounds |
| WO2005087766A1 (en) | 2004-03-09 | 2005-09-22 | Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa | Hiv integrase inhibitors |
| US7176196B2 (en) | 2004-05-28 | 2007-02-13 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| KR101580310B1 (ko) | 2005-04-28 | 2016-01-04 | 비이브 헬쓰케어 컴퍼니 | Ｈｉｖ 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체 |
| EP1910363A4 (en) * | 2005-08-04 | 2010-05-26 | Glaxosmithkline Llc | INHIBITORS OF HIV INTEGRASE |
| CA2626956A1 (en) * | 2005-10-27 | 2007-05-03 | Shionogi & Co., Ltd. | Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity |
| 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 |
| JP5480824B2 (ja) * | 2008-03-10 | 2014-04-23 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｐｌｋキナーゼ阻害剤としての４−アリール−２−アニリノ−ピリミジン |
-
2010
- 2010-10-13 CA CA2777664A patent/CA2777664C/en active Active
- 2010-10-13 EP EP10772998.0A patent/EP2488521B1/en active Active
- 2010-10-13 ES ES10772998.0T patent/ES2446720T3/es active Active
- 2010-10-13 US US13/395,891 patent/US8497270B2/en active Active
- 2010-10-13 KR KR1020127009345A patent/KR20120087916A/ko not_active Abandoned
- 2010-10-13 WO PCT/EP2010/065300 patent/WO2011045330A1/en not_active Ceased
- 2010-10-13 AU AU2010305805A patent/AU2010305805B2/en active Active
- 2010-10-13 EA EA201270540A patent/EA019558B1/ru not_active IP Right Cessation
- 2010-10-13 BR BR112012008586A patent/BR112012008586A2/pt not_active IP Right Cessation
- 2010-10-13 CN CN201080046163.3A patent/CN102574854B/zh active Active
- 2010-10-13 NZ NZ598766A patent/NZ598766A/xx not_active IP Right Cessation
- 2010-10-13 MX MX2012004426A patent/MX2012004426A/es active IP Right Grant
- 2010-10-13 JP JP2012533614A patent/JP5624148B2/ja active Active
-
2012
- 2012-03-26 IL IL218845A patent/IL218845A0/en unknown
- 2012-04-05 ZA ZA2012/02516A patent/ZA201202516B/en unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002030931A2 (en) * | 2000-10-12 | 2002-04-18 | Merck & Co., Inc. | Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2488521B1 (en) | 2013-12-18 |
| EA019558B1 (ru) | 2014-04-30 |
| CA2777664A1 (en) | 2011-04-21 |
| KR20120087916A (ko) | 2012-08-07 |
| JP2013507423A (ja) | 2013-03-04 |
| CA2777664C (en) | 2014-06-10 |
| ZA201202516B (en) | 2013-09-25 |
| NZ598766A (en) | 2013-09-27 |
| AU2010305805A1 (en) | 2012-04-19 |
| CN102574854B (zh) | 2014-04-16 |
| IL218845A0 (en) | 2012-06-28 |
| MX2012004426A (es) | 2012-07-30 |
| BR112012008586A2 (pt) | 2016-11-29 |
| US20120172367A1 (en) | 2012-07-05 |
| CN102574854A (zh) | 2012-07-11 |
| US8497270B2 (en) | 2013-07-30 |
| WO2011045330A1 (en) | 2011-04-21 |
| EA201270540A1 (ru) | 2012-09-28 |
| JP5624148B2 (ja) | 2014-11-12 |
| ES2446720T3 (es) | 2014-03-10 |
| EP2488521A1 (en) | 2012-08-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |