JP4494020B2 - Hivインテグラーゼ阻害剤として有用なn−(置換ベンジル)−8−ヒドロキシ−1,6−ナフチリジン−7−カルボキサミド - Google Patents
Hivインテグラーゼ阻害剤として有用なn−(置換ベンジル)−8−ヒドロキシ−1,6−ナフチリジン−7−カルボキサミド Download PDFInfo
- Publication number
- JP4494020B2 JP4494020B2 JP2003575904A JP2003575904A JP4494020B2 JP 4494020 B2 JP4494020 B2 JP 4494020B2 JP 2003575904 A JP2003575904 A JP 2003575904A JP 2003575904 A JP2003575904 A JP 2003575904A JP 4494020 B2 JP4494020 B2 JP 4494020B2
- Authority
- JP
- Japan
- Prior art keywords
- naphthyridine
- hydroxy
- dioxide
- alkyl
- carbonyl
- 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.)
- Expired - Fee Related
Links
- 0 *NC(c1cc(F)ccc1CNC(c1nc(N(CCCC2)S2(=O)=O)c(cccn2)c2c1O)=O)=O Chemical compound *NC(c1cc(F)ccc1CNC(c1nc(N(CCCC2)S2(=O)=O)c(cccn2)c2c1O)=O)=O 0.000 description 6
- NXKMYGNSJDIPLZ-UHFFFAOYSA-N CC(C)(C)OC(NCc(c(C(N)=O)c1)ccc1F)=O Chemical compound CC(C)(C)OC(NCc(c(C(N)=O)c1)ccc1F)=O NXKMYGNSJDIPLZ-UHFFFAOYSA-N 0.000 description 1
- KYWXRBNOYGGPIZ-UHFFFAOYSA-N CC(N1CCOCC1)=O Chemical compound CC(N1CCOCC1)=O KYWXRBNOYGGPIZ-UHFFFAOYSA-N 0.000 description 1
- DWYSVGAODAJSOB-UHFFFAOYSA-N OC(c1nc(N(CCCC2)S2(=O)=O)c(cccn2)c2c1O)=O Chemical compound OC(c1nc(N(CCCC2)S2(=O)=O)c(cccn2)c2c1O)=O DWYSVGAODAJSOB-UHFFFAOYSA-N 0.000 description 1
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
- C07D471/02—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
- C07D471/04—Ortho-condensed 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
-
- 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36492902P | 2002-03-15 | 2002-03-15 | |
| PCT/US2003/007448 WO2003077850A2 (en) | 2002-03-15 | 2003-03-12 | N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as hiv integrase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005527521A JP2005527521A (ja) | 2005-09-15 |
| JP2005527521A5 JP2005527521A5 (https=) | 2006-04-13 |
| JP4494020B2 true JP4494020B2 (ja) | 2010-06-30 |
Family
ID=28041987
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003575904A Expired - Fee Related JP4494020B2 (ja) | 2002-03-15 | 2003-03-12 | Hivインテグラーゼ阻害剤として有用なn−(置換ベンジル)−8−ヒドロキシ−1,6−ナフチリジン−7−カルボキサミド |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US7323460B2 (https=) |
| EP (1) | EP1496836B1 (https=) |
| JP (1) | JP4494020B2 (https=) |
| AT (1) | ATE409187T1 (https=) |
| AU (2) | AU2003218130A1 (https=) |
| CA (1) | CA2478310A1 (https=) |
| DE (1) | DE60323743D1 (https=) |
| WO (2) | WO2003077857A2 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003077857A2 (en) | 2002-03-15 | 2003-09-25 | Merck & Co., Inc. | N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as hiv integrase inhibitors |
| EP1541558B1 (en) | 2002-08-13 | 2008-08-13 | Shionogi & Co., Ltd. | Heterocyclic compounds having hiv integrase inhibitory activity |
| PA8586801A1 (es) | 2002-10-31 | 2005-02-04 | Pfizer | Inhibidores de hiv-integrasa, composiciones farmaceuticas y metodos para su uso |
| BRPI0407052A (pt) | 2003-01-27 | 2006-01-17 | Pfizer | Inibidores da hiv-integrase, composições farmacêuticas, e métodos para sua utilização |
| WO2004080402A2 (en) * | 2003-03-12 | 2004-09-23 | Merck & Co. Inc. | Potassium salt of an hiv integrase inhibitor |
| US20070185007A1 (en) | 2003-09-19 | 2007-08-09 | Haolun Jin | Aza-quinolinol phosphonate integrase inhibitor compounds |
| CA2542047A1 (en) | 2003-10-20 | 2005-05-12 | Merck & Co., Inc. | Hydroxy pyridopyrrolopyrazine dione compounds useful as hiv integrase inhibitors |
| WO2005075475A1 (ja) * | 2004-02-04 | 2005-08-18 | Shionogi & Co., Ltd. | Hivインテグラーゼ阻害活性を有するナフチリジン誘導体 |
| EP1725556A1 (en) * | 2004-03-09 | 2006-11-29 | Merck & Co., Inc. | Hiv integrase inhibitors |
| WO2005103003A2 (en) * | 2004-04-26 | 2005-11-03 | Pfizer Inc. | Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors |
| BRPI0510306A (pt) | 2004-04-26 | 2007-09-04 | Pfizer | inibidores da enzima de hiv integrase,composição farmacêutica contendo os referidos inibidores bem como seu uso |
| JP2009513640A (ja) * | 2005-10-27 | 2009-04-02 | メルク エンド カムパニー インコーポレーテッド | Hivインテグラーゼインヒビター |
| CA2662080C (en) | 2006-09-07 | 2012-07-17 | F. Hoffmann-La Roche Ag | A process for the manufacture of snac (salcaprozate sodium) |
| CN106117196A (zh) * | 2016-06-09 | 2016-11-16 | 青岛辰达生物科技有限公司 | 一种制备抗癌药物达沙替尼的方法 |
| CN107722106A (zh) * | 2016-08-11 | 2018-02-23 | 重庆大学 | Hiv抑制剂 |
| CN112409267A (zh) * | 2019-08-22 | 2021-02-26 | 江苏阿尔法药业有限公司 | 一种索菲布韦中间体的制备方法 |
| AR122928A1 (es) * | 2020-07-10 | 2022-10-19 | Goldfinch Bio Inc | 1,6-naftiridinas sustituidas inhibidoras de cdk5 |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5751837B2 (https=) | 1973-04-05 | 1982-11-04 | ||
| US4416884A (en) * | 1978-04-12 | 1983-11-22 | Otsuka Pharmaceutical Co., Ltd. | Piperazinylbenzoheterocyclic compounds |
| FR2632639B1 (fr) * | 1988-06-09 | 1990-10-05 | Sanofi Sa | Derives d'amino-4 carboxy-3 naphtyridines, leur preparation et compositions pharmaceutiques qui les contiennent |
| IL101860A0 (en) * | 1991-05-31 | 1992-12-30 | Ici Plc | Heterocyclic derivatives |
| TW263498B (https=) * | 1993-11-10 | 1995-11-21 | Takeda Pharm Industry Co Ltd | |
| DK0688772T3 (da) * | 1994-06-16 | 1999-11-01 | Lg Chemical Ltd | Quinolincarboxylsyrederivater med 7-(4-aminomethyl-3-oxim)-pyrrolidinsubstituenter og fremgangsmåde til deres fremstilling |
| US5776944A (en) * | 1994-06-16 | 1998-07-07 | Lg Chemical Ltd. | 7-(4-aminomethyl-3-methyloxyiminopyrroplidin-1-yl)-1-cyclopropyl-6-flu oro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid and the process for the preparation thereof |
| US5681832A (en) | 1995-02-17 | 1997-10-28 | The United States Of America As Represented By The Department Of Health And Human Services | Aroylaniline compounds, pharmaceutical compositions, and methods of using same to inhibit viral activity |
| DE69631423T2 (de) * | 1995-08-02 | 2004-12-02 | Darwin Discovery Ltd., Slough | Chinolone und deren therapeutische verwendung |
| US5945431A (en) * | 1996-03-15 | 1999-08-31 | Biochem Therapeutics Incorporated | Cytomegalovirus inhibiting compounds |
| EP0927164A1 (en) * | 1996-09-10 | 1999-07-07 | PHARMACIA & UPJOHN COMPANY | 8-hydroxy-7-substituted quinolines as anti-viral agents |
| KR100567649B1 (ko) | 1996-09-25 | 2006-04-05 | 아스트라제네카 유케이 리미티드 | 혈관 내피 성장 인자와 같은 성장 인자의 효과를 억제하는 퀴놀린 유도체 |
| DE69828284T2 (de) * | 1997-06-30 | 2005-12-08 | Nippon Kayaku K.K. | Naphthyridinderivate oder salze davon |
| PL338783A1 (en) | 1997-08-25 | 2000-11-20 | Neurogen Corp | Substituted 4-oxo-naphtyridin-3-carboxamides as ligands of cerebral gaba receptors |
| GB9720052D0 (en) | 1997-09-19 | 1997-11-19 | Smithkline Beecham Plc | Novel compounds |
| EP1031563B1 (en) * | 1997-09-30 | 2005-12-28 | Daiichi Pharmaceutical Co., Ltd. | Sulfonyl derivatives |
| WO1999029318A1 (en) * | 1997-12-11 | 1999-06-17 | Biochem Pharma Inc. | Antiviral compounds |
| DE69831506T2 (de) | 1997-12-22 | 2006-06-29 | Pharmacia & Upjohn Co. Llc, Kalamazoo | 4-hydroxychinolin-3-carboxamide und hydrazide als antivirale wirkstoffe |
| EP1086091A4 (en) | 1998-06-03 | 2001-10-10 | Merck & Co Inc | INTEGRASE HIV INHIBITORS |
| WO1999062520A1 (en) | 1998-06-03 | 1999-12-09 | Merck & Co., Inc. | Hiv integrase inhibitors |
| WO1999062513A1 (en) | 1998-06-03 | 1999-12-09 | Merck & Co., Inc. | Hiv integrase inhibitors |
| US6380249B1 (en) * | 1998-06-03 | 2002-04-30 | Merck & Co., Inc. | HIV integrase inhibitors |
| US6306891B1 (en) * | 1998-06-03 | 2001-10-23 | Merck & Co., Inc. | HIV integrase inhibitors |
| US6262055B1 (en) * | 1998-06-03 | 2001-07-17 | Merck & Co., Inc. | HIV integrase inhibitors |
| SE9802550D0 (sv) | 1998-07-15 | 1998-07-15 | Active Biotech Ab | Quinoline derivatives |
| JP2002522541A (ja) | 1998-08-11 | 2002-07-23 | ファイザー・プロダクツ・インク | ホスホジエステラーゼ4阻害剤としての置換1,8−ナフチリジン−4(1h)−オン |
| JP2003503386A (ja) | 1999-06-25 | 2003-01-28 | メルク エンド カムパニー インコーポレーテッド | 1−(芳香族またはヘテロ芳香族置換)−3−(ヘテロ芳香族置換)−1,3−プロパンジオン類およびそれの使用 |
| WO2001095905A1 (fr) * | 2000-06-14 | 2001-12-20 | Shionogi & Co., Ltd. | Inhibiteur d'enzymes possedant deux ions metal divalents en tant que centres actifs |
| US6730682B2 (en) | 2000-07-12 | 2004-05-04 | Pharmacia & Upjohn Company | Heterocycle carboxamides as antiviral agents |
| GB0017676D0 (en) | 2000-07-19 | 2000-09-06 | Angeletti P Ist Richerche Bio | Inhibitors of viral polymerase |
| WO2002009504A1 (en) * | 2000-08-02 | 2002-02-07 | George Robert A | Squirrel-proof bird feeding apparatus and method |
| JP2004513134A (ja) * | 2000-10-12 | 2004-04-30 | メルク エンド カムパニー インコーポレーテッド | Hivインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルケトン類 |
| JP2004517860A (ja) * | 2000-10-12 | 2004-06-17 | メルク エンド カムパニー インコーポレーテッド | Hivインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルカルボキサミド類 |
| US6919351B2 (en) * | 2000-10-12 | 2005-07-19 | Merck & Co., Inc. | Aza-and polyaza-naphthalenyl-carboxamides useful as HIV integrase inhibitors |
| CA2425440C (en) * | 2000-10-12 | 2010-04-13 | Merck & Co., Inc. | Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
| JP3616628B2 (ja) * | 2001-03-01 | 2005-02-02 | 塩野義製薬株式会社 | Hivインテグラーゼ阻害活性を有する含窒素芳香族複素環化合物 |
| AR036256A1 (es) * | 2001-08-17 | 2004-08-25 | Merck & Co Inc | Sal sodica de un inhibidor de integrasa del vih, procesos para su preparacion, composiciones farmaceuticas que lo contienen y su uso para la manufactura de un medicamento |
| NZ533057A (en) | 2001-10-26 | 2005-11-25 | Angeletti P Ist Richerche Bio | N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase |
| EP1441734B1 (en) | 2001-10-26 | 2007-02-28 | Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. | Dihydroxypyrimidine carboxamide inhibitors of hiv integrase |
| WO2003077857A2 (en) | 2002-03-15 | 2003-09-25 | Merck & Co., Inc. | N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as hiv integrase inhibitors |
| EP1499391A2 (en) * | 2002-04-10 | 2005-01-26 | Merck & Co., Inc. | Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant |
-
2003
- 2003-03-12 WO PCT/US2003/007671 patent/WO2003077857A2/en not_active Ceased
- 2003-03-12 AT AT03716466T patent/ATE409187T1/de not_active IP Right Cessation
- 2003-03-12 US US10/508,094 patent/US7323460B2/en not_active Expired - Fee Related
- 2003-03-12 JP JP2003575904A patent/JP4494020B2/ja not_active Expired - Fee Related
- 2003-03-12 EP EP03716466A patent/EP1496836B1/en not_active Expired - Lifetime
- 2003-03-12 CA CA002478310A patent/CA2478310A1/en not_active Abandoned
- 2003-03-12 AU AU2003218130A patent/AU2003218130A1/en not_active Abandoned
- 2003-03-12 WO PCT/US2003/007448 patent/WO2003077850A2/en not_active Ceased
- 2003-03-12 AU AU2003220170A patent/AU2003220170B2/en not_active Ceased
- 2003-03-12 DE DE60323743T patent/DE60323743D1/de not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| AU2003220170A1 (en) | 2003-09-29 |
| DE60323743D1 (en) | 2008-11-06 |
| EP1496836B1 (en) | 2008-09-24 |
| AU2003218130A8 (en) | 2003-09-29 |
| WO2003077850A2 (en) | 2003-09-25 |
| AU2003218130A1 (en) | 2003-09-29 |
| JP2005527521A (ja) | 2005-09-15 |
| AU2003220170B2 (en) | 2008-12-11 |
| ATE409187T1 (de) | 2008-10-15 |
| EP1496836A4 (en) | 2006-03-22 |
| WO2003077850A3 (en) | 2004-11-11 |
| US20050176955A1 (en) | 2005-08-11 |
| EP1496836A2 (en) | 2005-01-19 |
| CA2478310A1 (en) | 2003-09-25 |
| WO2003077857A2 (en) | 2003-09-25 |
| US7323460B2 (en) | 2008-01-29 |
| WO2003077857A3 (en) | 2006-06-08 |
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