JP2007528379A5 - - Google Patents
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- JP2007528379A5 JP2007528379A5 JP2007502381A JP2007502381A JP2007528379A5 JP 2007528379 A5 JP2007528379 A5 JP 2007528379A5 JP 2007502381 A JP2007502381 A JP 2007502381A JP 2007502381 A JP2007502381 A JP 2007502381A JP 2007528379 A5 JP2007528379 A5 JP 2007528379A5
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- Prior art keywords
- alkyl
- independently
- hetf
- ring
- substituents
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 69
- 150000001875 compounds Chemical class 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 21
- 229910052799 carbon Inorganic materials 0.000 claims 19
- 125000001424 substituent group Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 8
- 208000030507 AIDS Diseases 0.000 claims 6
- 208000031886 HIV Infections Diseases 0.000 claims 6
- 208000037357 HIV infectious disease Diseases 0.000 claims 6
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 6
- 125000004434 sulfur atom Chemical group 0.000 claims 6
- 125000001624 naphthyl group Chemical group 0.000 claims 5
- -1 —O—C 1-6 haloalkyl Chemical group 0.000 claims 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- 108010002459 HIV Integrase Proteins 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- GTCAXTIRRLKXRU-UHFFFAOYSA-N methyl carbamate Chemical compound COC(N)=O GTCAXTIRRLKXRU-UHFFFAOYSA-N 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000004430 oxygen atom Chemical group O* 0.000 claims 4
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical group C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims 2
- 125000001246 bromo group Chemical group Br* 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 239000002777 nucleoside Substances 0.000 claims 2
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- AUUWKCMVGVUDLA-ZIAGYGMSSA-N (+/-) trans n-[7-(4-fluorobenzyl)-5-hydroxy-4,6-dioxo-2,4,6,7,8,8a-hexahydro-1h- 3,7,8b-triazaacenaphthylen-2-yl]-n,n',n'-trimethylethanediamide Chemical compound C([C@H]1C[C@H](C2=NC(=O)C(O)=C(N12)C1=O)N(C)C(=O)C(=O)N(C)C)N1CC1=CC=C(F)C=C1 AUUWKCMVGVUDLA-ZIAGYGMSSA-N 0.000 claims 1
- PEHPFDCKYDXVTF-UHFFFAOYSA-N 3,10-bis[(4-fluorophenyl)methyl]-7-hydroxy-3-(methylamino)-5,10,12-triazatricyclo[6.3.1.04,12]dodeca-4,7-diene-6,9-dione Chemical compound C1C(N23)CN(CC=4C=CC(F)=CC=4)C(=O)C3=C(O)C(=O)N=C2C1(NC)CC1=CC=C(F)C=C1 PEHPFDCKYDXVTF-UHFFFAOYSA-N 0.000 claims 1
- OVLCJVQMKOVZEH-UHFFFAOYSA-N 3-(dimethylamino)-10-[(4-fluorophenyl)methyl]-7-hydroxy-5,10,12-triazatricyclo[6.3.1.04,12]dodeca-4,7-diene-6,9-dione Chemical compound O=C1C(N23)=C(O)C(=O)N=C3C(N(C)C)CC2CN1CC1=CC=C(F)C=C1 OVLCJVQMKOVZEH-UHFFFAOYSA-N 0.000 claims 1
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 1
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 claims 1
- 229940122440 HIV protease inhibitor Drugs 0.000 claims 1
- ABMXEBCXEFIGGA-UHFFFAOYSA-N N'-[10-[(3-chloro-4-fluorophenyl)methyl]-7-hydroxy-6,9-dioxo-5,10,12-triazatricyclo[6.3.1.04,12]dodeca-4,7-dien-3-yl]-N,N,N'-trimethyloxamide Chemical compound O=C1C(N23)=C(O)C(=O)N=C3C(N(C)C(=O)C(=O)N(C)C)CC2CN1CC1=CC=C(F)C(Cl)=C1 ABMXEBCXEFIGGA-UHFFFAOYSA-N 0.000 claims 1
- AUUWKCMVGVUDLA-UHFFFAOYSA-N N'-[10-[(4-fluorophenyl)methyl]-7-hydroxy-6,9-dioxo-5,10,12-triazatricyclo[6.3.1.04,12]dodeca-4,7-dien-3-yl]-N,N,N'-trimethyloxamide Chemical compound O=C1C(N23)=C(O)C(=O)N=C3C(N(C)C(=O)C(=O)N(C)C)CC2CN1CC1=CC=C(F)C=C1 AUUWKCMVGVUDLA-UHFFFAOYSA-N 0.000 claims 1
- 230000000840 anti-viral effect Effects 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000002532 enzyme inhibitor Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 239000004030 hiv protease inhibitor Substances 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000010839 reverse transcription Methods 0.000 claims 1
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US55160104P | 2004-03-09 | 2004-03-09 | |
| PCT/GB2005/000746 WO2005087766A1 (en) | 2004-03-09 | 2005-03-01 | Hiv integrase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007528379A JP2007528379A (ja) | 2007-10-11 |
| JP2007528379A5 true JP2007528379A5 (https=) | 2008-09-18 |
Family
ID=34961192
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007502381A Withdrawn JP2007528379A (ja) | 2004-03-09 | 2005-03-01 | Hivインテグラーゼ阻害薬 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US20070161639A1 (https=) |
| EP (1) | EP1725554A1 (https=) |
| JP (1) | JP2007528379A (https=) |
| CN (1) | CN1930161A (https=) |
| AU (1) | AU2005221864A1 (https=) |
| CA (1) | CA2557926A1 (https=) |
| WO (1) | WO2005087766A1 (https=) |
Families Citing this family (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200510425A (en) | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
| JP2007528394A (ja) * | 2004-03-09 | 2007-10-11 | 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 |
| EP1725556A1 (en) * | 2004-03-09 | 2006-11-29 | Merck & Co., Inc. | Hiv integrase inhibitors |
| JP2007528396A (ja) * | 2004-03-09 | 2007-10-11 | 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 |
| EP1973906A1 (en) * | 2004-12-23 | 2008-10-01 | Virochem Pharma Inc. | Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase |
| US8129385B2 (en) | 2005-04-28 | 2012-03-06 | Shionogi & Co., Ltd. | Substituted 5-hydroxy-3,4,6,9,9a, 10-hexanhydro-2h-1-oxa04a,8a-diaza-anthracene-6,10-dioness |
| CA2607151C (en) * | 2005-05-10 | 2012-06-19 | Merck & Co., Inc. | Hiv integrase inhibitors |
| CA2616314A1 (en) * | 2005-07-27 | 2007-02-01 | Gilead Sciences, Inc. | Antiviral phosphonate conjugates for inhibition of hiv |
| CA2622639C (en) * | 2005-10-04 | 2012-01-03 | Istituto Di Recerche Di Biologia Molecolare P. Angeletti S.P.A. | Hiv integrase inhibitors |
| 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 |
| EA200801144A1 (ru) | 2005-10-27 | 2008-10-30 | Сионоги Энд Ко., Лтд. | Полициклическое карбамоилпиридоновое производное, обладающее ингибиторной активностью в отношении интегразы вич |
| WO2008048538A1 (en) * | 2006-10-18 | 2008-04-24 | Merck & Co., Inc. | Hiv integrase inhibitors |
| EP2320909B8 (en) | 2008-07-25 | 2016-03-30 | VIIV Healthcare Company | Chemical compounds |
| CA2744019C (en) | 2008-12-11 | 2017-03-14 | Shionogi & Co., Ltd. | Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates |
| KR101682058B1 (ko) | 2008-12-11 | 2016-12-02 | 비이브 헬쓰케어 컴퍼니 | 카르바모일피리돈 hiv 인테그라제 억제제를 위한 제조방법 및 중간체 |
| TWI518084B (zh) | 2009-03-26 | 2016-01-21 | 鹽野義製藥股份有限公司 | 哌喃酮與吡啶酮衍生物之製造方法 |
| LT2444400T (lt) | 2009-06-15 | 2018-06-11 | Shionogi & Co., Ltd. | Pakeistasis policiklinis karbamoilpiridono darinys |
| WO2011045330A1 (en) | 2009-10-13 | 2011-04-21 | Tibotec Pharmaceuticals | Macrocyclic integrase inhibitors |
| US8283366B2 (en) | 2010-01-22 | 2012-10-09 | Ambrilia Biopharma, Inc. | Derivatives of pyridoxine for inhibiting HIV integrase |
| PE20130010A1 (es) | 2010-02-26 | 2013-02-05 | Japan Tobacco Inc | Derivado de 1,3,4,8-tetrahidro-2h-pirido[1,2-a]pirazina como inhibidor de la integrasa del vih |
| TWI582097B (zh) | 2010-03-23 | 2017-05-11 | Viiv醫療保健公司 | 製備胺甲醯吡啶酮衍生物及中間體之方法 |
| RU2567385C2 (ru) | 2010-04-02 | 2015-11-10 | ЯНССЕН Ар ЭНД Ди АЙРЛЭНД | Макроциклические ингибиторы интегразы |
| MX2013003139A (es) | 2010-09-24 | 2013-06-18 | Shionogi & Co | Profarmaco de derivado de carbamoilpiridona policiclica substituida. |
| EP4556010A3 (en) | 2011-11-30 | 2025-07-23 | Emory University | Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae |
| ES2643403T3 (es) | 2011-12-28 | 2017-11-22 | Global Blood Therapeutics, Inc. | Compuestos de benzaldehído sustituidos y métodos para su uso en el aumento de la oxigenación tisular |
| HK1203412A1 (en) | 2011-12-28 | 2015-10-30 | Global Blood Therapeutics, Inc. | Substituted heteroaryl aldehyde compounds and methods for their use in increasing tissue oxygenation |
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| KR20230031990A (ko) | 2018-02-28 | 2023-03-07 | 노파르티스 아게 | 인플루엔자의 치료를 위한 오르토믹소바이러스 복제의 억제제로서의 10-(디(페닐)메틸)-4-히드록시-8,9,9a,10-테트라히드로-7h-피롤로[1',2':4,5]피라지노[1,2-b]피리다진-3,5-디온 유도체 및 관련 화합물 |
| US11014884B2 (en) | 2018-10-01 | 2021-05-25 | Global Blood Therapeutics, Inc. | Modulators of hemoglobin |
| WO2020221294A1 (zh) * | 2019-04-30 | 2020-11-05 | 上海拓界生物医药科技有限公司 | 桥环-3,4-二氢-吡啶并[1,2-a]吡嗪-1,8-二酮化合物及其药物用途 |
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Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
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| 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 |
| CA2425440C (en) | 2000-10-12 | 2010-04-13 | Merck & Co., Inc. | Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
| 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 |
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| US6919351B2 (en) | 2000-10-12 | 2005-07-19 | Merck & Co., Inc. | Aza-and polyaza-naphthalenyl-carboxamides useful as HIV integrase inhibitors |
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| 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 |
| EP1467970B1 (en) | 2002-01-17 | 2007-08-22 | Merck & Co., Inc. | Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors |
| US7109186B2 (en) | 2002-07-09 | 2006-09-19 | Bristol-Myers Squibb Company | HIV 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 |
| JP2007528394A (ja) * | 2004-03-09 | 2007-10-11 | 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 |
| EP1725556A1 (en) * | 2004-03-09 | 2006-11-29 | Merck & Co., Inc. | Hiv integrase inhibitors |
| JP2007528396A (ja) * | 2004-03-09 | 2007-10-11 | 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 |
| EP1973906A1 (en) * | 2004-12-23 | 2008-10-01 | Virochem Pharma Inc. | Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase |
-
2005
- 2005-03-01 WO PCT/GB2005/000746 patent/WO2005087766A1/en not_active Ceased
- 2005-03-01 CA CA002557926A patent/CA2557926A1/en not_active Abandoned
- 2005-03-01 US US10/587,601 patent/US20070161639A1/en not_active Abandoned
- 2005-03-01 JP JP2007502381A patent/JP2007528379A/ja not_active Withdrawn
- 2005-03-01 CN CNA2005800074413A patent/CN1930161A/zh active Pending
- 2005-03-01 AU AU2005221864A patent/AU2005221864A1/en not_active Abandoned
- 2005-03-01 EP EP05717825A patent/EP1725554A1/en not_active Withdrawn
-
2008
- 2008-12-09 US US12/316,027 patent/US20090099168A1/en not_active Abandoned
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