DE60124577T2 - Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer - Google Patents
Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer Download PDFInfo
- Publication number
- DE60124577T2 DE60124577T2 DE60124577T DE60124577T DE60124577T2 DE 60124577 T2 DE60124577 T2 DE 60124577T2 DE 60124577 T DE60124577 T DE 60124577T DE 60124577 T DE60124577 T DE 60124577T DE 60124577 T2 DE60124577 T2 DE 60124577T2
- Authority
- DE
- Germany
- Prior art keywords
- alkyl
- substituted
- fluoroalkyl
- halogen
- independently selected
- 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
- PVOAHINGSUIXLS-UHFFFAOYSA-N CN1CCNCC1 Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 description 1
- BDDLIVBPPQOEIT-UHFFFAOYSA-N NOc1c(C(N(CC2)CC2c2ccccc2)=O)ncc2c1nccc2 Chemical compound NOc1c(C(N(CC2)CC2c2ccccc2)=O)ncc2c1nccc2 BDDLIVBPPQOEIT-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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (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)
- Indole Compounds (AREA)
- Pyrrole Compounds (AREA)
- Decoration By Transfer Pictures (AREA)
- Compression Or Coding Systems Of Tv Signals (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23967900P | 2000-10-12 | 2000-10-12 | |
| US239679P | 2000-10-12 | ||
| PCT/US2001/042565 WO2002055079A2 (en) | 2000-10-12 | 2001-10-09 | Aza-and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60124577D1 DE60124577D1 (en) | 2006-12-28 |
| DE60124577T2 true DE60124577T2 (de) | 2007-09-27 |
Family
ID=22903252
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60124577T Expired - Fee Related DE60124577T2 (de) | 2000-10-12 | 2001-10-09 | Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US6841558B2 (enExample) |
| EP (1) | EP1326610B1 (enExample) |
| JP (1) | JP2004517860A (enExample) |
| AT (1) | ATE345129T1 (enExample) |
| AU (1) | AU2002246499B2 (enExample) |
| CA (1) | CA2425625A1 (enExample) |
| DE (1) | DE60124577T2 (enExample) |
| ES (1) | ES2274913T3 (enExample) |
| WO (1) | WO2002055079A2 (enExample) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL365027A1 (en) | 2001-03-01 | 2004-12-27 | Shionogi & Co, Ltd. | Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity |
| DK1441734T3 (da) * | 2001-10-26 | 2007-06-11 | Angeletti P Ist Richerche Bio | Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase |
| HU230248B1 (hu) * | 2001-10-26 | 2015-11-30 | Msd Italia S.R.L. | N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok |
| CA2478310A1 (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 |
| JP3908248B2 (ja) | 2002-08-13 | 2007-04-25 | 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ヘテロ環化合物 |
| EP1539714B1 (en) | 2002-09-11 | 2008-08-13 | Merck & Co., Inc. | 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors |
| CA2498111A1 (en) * | 2002-09-11 | 2004-03-25 | Merck & Co., Inc. | Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors |
| WO2004035577A2 (en) | 2002-10-16 | 2004-04-29 | Gilead Sciences, Inc. | Pre-organized tricyclic integrase inhibitor compounds |
| EP3406596A1 (en) | 2002-11-20 | 2018-11-28 | Japan Tobacco Inc. | 4-oxoquinoline compound and use thereof as hiv integrase inhibitor |
| WO2004058756A1 (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 |
| KR20060006047A (ko) * | 2003-04-28 | 2006-01-18 | 티보텍 파마슈티칼즈 리미티드 | Hiv 인테그레이즈 저해제 |
| WO2004101512A2 (en) * | 2003-05-13 | 2004-11-25 | Smithkline Beecham Corporation | Naphthyridine integrase inhibitors |
| TW200510425A (en) | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
| US7462721B2 (en) | 2003-09-19 | 2008-12-09 | Gilead Sciences, Inc. | Aza-quinolinol phosphonate integrase inhibitor compounds |
| WO2005041664A1 (en) | 2003-10-20 | 2005-05-12 | Merck & Co., Inc. | Hydroxy pyridopyrrolopyrazine dione compounds useful as hiv integrase inhibitors |
| EP1714966A4 (en) * | 2004-02-04 | 2008-01-02 | Shionogi & Co | NAPHTHYLIDINE DERIVATIVE HAVING HIGH INTEGRASE HIV INHIBITING ACTIVITY |
| BRPI0507628A (pt) | 2004-02-11 | 2007-07-03 | Smithkline Beecham Corp | composto ou sal farmaceuticamente aceitável do mesmo, método de tratamento de uma infecção viral em um ser humano, uso de um composto composição farmacêutica, e, processo para a preparação de um composto |
| AU2005222391B2 (en) * | 2004-03-09 | 2010-11-11 | Merck Sharp & Dohme Corp. | HIV integrase inhibitors |
| 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 |
| AU2005220767A1 (en) | 2004-03-09 | 2005-09-22 | Merck & Co., Inc. | HIV integrase inhibitors |
| EP1725102A4 (en) * | 2004-03-09 | 2009-04-29 | Merck & Co Inc | HIV integrase |
| US7538112B2 (en) * | 2004-05-07 | 2009-05-26 | Merck & Co., Inc. | HIV integrase inhibitors |
| WO2005113509A1 (en) | 2004-05-20 | 2005-12-01 | Japan Tobacco Inc. | Novel 4-oxoquinoline compound and use thereof as hiv integrase inhibitor |
| MY134672A (en) | 2004-05-20 | 2007-12-31 | Japan Tobacco Inc | Stable crystal of 4-oxoquinoline compound |
| US8633219B2 (en) | 2004-05-21 | 2014-01-21 | Japan Tobacco Inc. | Combination therapy |
| US7476666B2 (en) | 2004-06-09 | 2009-01-13 | Merck & Co., Inc. | HIV integrase inhibitors |
| US7981879B2 (en) * | 2005-03-31 | 2011-07-19 | Instituto di Ricerchi di Biologia Molecolare P. Angeletti S.p.A. | HIV integrase inhibitors |
| EP1881825B1 (en) * | 2005-05-10 | 2013-07-24 | Merck Sharp & Dohme Corp. | Hiv integrase inhibitors |
| AU2006299042B8 (en) * | 2005-10-04 | 2011-09-15 | Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa | HIV integrase inhibitors |
| AU2006306355A1 (en) * | 2005-10-27 | 2007-05-03 | Merck & Co., Inc. | HIV integrase inhibitors |
| EP1790342A1 (de) | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| US8217042B2 (en) | 2005-11-11 | 2012-07-10 | Zentaris Gmbh | Pyridopyrazines and their use as modulators of kinases |
| US7902182B2 (en) * | 2005-11-16 | 2011-03-08 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| RS54047B1 (sr) | 2006-03-06 | 2015-10-30 | Japan Tobacco Inc. | Postupak za dobijanje jedinjenja 4-oksohinolina |
| CA2651579A1 (en) | 2006-05-16 | 2007-11-29 | Gilead Sciences, Inc. | Integrase inhibitors |
| EP2044068A4 (en) * | 2006-07-17 | 2010-07-21 | Merck Sharp & Dohme | 1-HYDROXY Naphthyridine Compounds as Anti- HIV Drugs |
| BRPI0717511A2 (pt) | 2006-09-29 | 2013-11-19 | Idenix Pharmaceuticals Inc | Composto puro, composição farmacêutica, métodos para tratar uma infecção por hiv, para prevenir uma infecção por hiv, para inibir a replicação de hiv, e, uso de um composto |
| JP2010506913A (ja) * | 2006-10-18 | 2010-03-04 | 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剤 |
| EP1972627A1 (en) * | 2007-03-19 | 2008-09-24 | Technische Universität Carolo-Wilhelmina zu Braunschweig | Amino-napthyridine derivatives |
| US8513420B2 (en) * | 2007-03-19 | 2013-08-20 | Monika Mazik | Amino-naphthyridine derivatives |
| CN105055432A (zh) | 2008-01-25 | 2015-11-18 | 奇默里克斯公司 | 治疗病毒感染的方法 |
| DE102009038123A1 (de) * | 2009-08-17 | 2011-02-24 | Aicuris Gmbh & Co. Kg | Substituierte (Thiazolyl-carbonyl)imidazolidinone und ihre Verwendung |
| WO2011045330A1 (en) | 2009-10-13 | 2011-04-21 | Tibotec Pharmaceuticals | Macrocyclic integrase inhibitors |
| EP2534150B1 (en) | 2010-02-12 | 2017-04-05 | Chimerix, Inc. | Methods of treating viral infection |
| CN102958935B (zh) | 2010-04-02 | 2015-12-09 | 爱尔兰詹森科学公司 | 大环整合酶抑制剂 |
| US9029391B2 (en) | 2011-01-24 | 2015-05-12 | Viiv Healthcare Uk Limited | Isoquinoline compounds and methods for treating HIV |
| EP2996691A1 (en) | 2013-05-16 | 2016-03-23 | The U.S.A. as represented by the Secretary, Department of Health and Human Services | Compounds for inhibiting drug-resistant strains of hiv-1 integrase |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5751837B2 (enExample) * | 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 |
| 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 |
| ES2211965T3 (es) * | 1995-08-02 | 2004-07-16 | Darwin Discovery Limited | Quinolonas y su utilizacion terapeutica. |
| US5945431A (en) * | 1996-03-15 | 1999-08-31 | Biochem Therapeutics Incorporated | Cytomegalovirus inhibiting compounds |
| WO1998011073A1 (en) * | 1996-09-10 | 1998-03-19 | 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 |
| AU729995B2 (en) * | 1997-06-30 | 2001-02-22 | Nippon Kayaku Kabushiki Kaisha | Novel naphthyridine derivatives or salts thereof |
| KR20010023313A (ko) | 1997-08-25 | 2001-03-26 | 해피 페너 ; 해리 에이치. 페너 2세 | Gaba 뇌 수용체 리간드로서의 치환된4-옥소-나프티리딘-3-카르복스아미드 |
| US6143760A (en) * | 1997-08-25 | 2000-11-07 | Neurogen Corporation | Substituted 4-oxo-napthyridine-3-carboxamides: GABA brain receptor ligands |
| GB9720052D0 (en) * | 1997-09-19 | 1997-11-19 | Smithkline Beecham Plc | Novel compounds |
| CN1278793A (zh) * | 1997-09-30 | 2001-01-03 | 第一制药株式会社 | 磺酰基衍生物 |
| DE69831506T2 (de) | 1997-12-22 | 2006-06-29 | Pharmacia & Upjohn Co. Llc, Kalamazoo | 4-hydroxychinolin-3-carboxamide und hydrazide als antivirale wirkstoffe |
| US6306891B1 (en) * | 1998-06-03 | 2001-10-23 | Merck & Co., Inc. | HIV integrase inhibitors |
| US6380249B1 (en) * | 1998-06-03 | 2002-04-30 | Merck & Co., Inc. | HIV integrase inhibitors |
| US6262055B1 (en) * | 1998-06-03 | 2001-07-17 | Merck & Co., Inc. | HIV integrase inhibitors |
| WO2001000578A1 (en) | 1999-06-25 | 2001-01-04 | Merck & Co., Inc. | 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof |
| 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 |
| HU230248B1 (hu) | 2001-10-26 | 2015-11-30 | Msd Italia S.R.L. | N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok |
| DK1441734T3 (da) | 2001-10-26 | 2007-06-11 | Angeletti P Ist Richerche Bio | Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase |
-
2001
- 2001-10-09 JP JP2002555813A patent/JP2004517860A/ja not_active Withdrawn
- 2001-10-09 EP EP01994068A patent/EP1326610B1/en not_active Expired - Lifetime
- 2001-10-09 WO PCT/US2001/042565 patent/WO2002055079A2/en not_active Ceased
- 2001-10-09 ES ES01994068T patent/ES2274913T3/es not_active Expired - Lifetime
- 2001-10-09 AU AU2002246499A patent/AU2002246499B2/en not_active Ceased
- 2001-10-09 DE DE60124577T patent/DE60124577T2/de not_active Expired - Fee Related
- 2001-10-09 US US10/398,988 patent/US6841558B2/en not_active Expired - Fee Related
- 2001-10-09 CA CA002425625A patent/CA2425625A1/en not_active Abandoned
- 2001-10-09 AT AT01994068T patent/ATE345129T1/de not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| EP1326610A2 (en) | 2003-07-16 |
| DE60124577D1 (en) | 2006-12-28 |
| CA2425625A1 (en) | 2002-07-18 |
| WO2002055079A3 (en) | 2002-09-06 |
| US20040044207A1 (en) | 2004-03-04 |
| AU2002246499B2 (en) | 2005-12-22 |
| EP1326610B1 (en) | 2006-11-15 |
| ATE345129T1 (de) | 2006-12-15 |
| ES2274913T3 (es) | 2007-06-01 |
| US6841558B2 (en) | 2005-01-11 |
| EP1326610A4 (en) | 2004-06-09 |
| JP2004517860A (ja) | 2004-06-17 |
| WO2002055079A2 (en) | 2002-07-18 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8381 | Inventor (new situation) |
Inventor name: ANTHONY, NEVILLE, J., RAHWAY, NJ 07065-0907, US Inventor name: GOMEZ, ROBERT, P., RAHWAY, NJ 07065-0907, US Inventor name: BENNETT, JENNIFER, J., RAHWAY, NJ 07065-0907, US Inventor name: YOUNG, STEVEN, D., RAHWAY, NJ 07065-0907, US |
|
| 8364 | No opposition during term of opposition | ||
| 8327 | Change in the person/name/address of the patent owner |
Owner name: MERCK & CO., INC., RAHWAY, N.J., US |
|
| 8339 | Ceased/non-payment of the annual fee |