RU2329265C2 - ТЕТРАГИДРО-4Н-ПИРИДО[1,2-а]ПИРИМИДИНЫ И РОДСТВЕННЫЕ СОЕДИНЕНИЯ, ПОЛЕЗНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ВИЧ-ИНТЕГРАЗЫ - Google Patents
ТЕТРАГИДРО-4Н-ПИРИДО[1,2-а]ПИРИМИДИНЫ И РОДСТВЕННЫЕ СОЕДИНЕНИЯ, ПОЛЕЗНЫЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ВИЧ-ИНТЕГРАЗЫ Download PDFInfo
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- RU2329265C2 RU2329265C2 RU2005123807/04A RU2005123807A RU2329265C2 RU 2329265 C2 RU2329265 C2 RU 2329265C2 RU 2005123807/04 A RU2005123807/04 A RU 2005123807/04A RU 2005123807 A RU2005123807 A RU 2005123807A RU 2329265 C2 RU2329265 C2 RU 2329265C2
- Authority
- RU
- Russia
- Prior art keywords
- oxo
- hydroxy
- amino
- fluorobenzyl
- tetrahydro
- Prior art date
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- 230000008030 elimination Effects 0.000 description 1
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- MVEAAGBEUOMFRX-UHFFFAOYSA-N ethyl acetate;hydrochloride Chemical compound Cl.CCOC(C)=O MVEAAGBEUOMFRX-UHFFFAOYSA-N 0.000 description 1
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- VZCYOOQTPOCHFL-OWOJBTEDSA-L fumarate(2-) Chemical compound [O-]C(=O)\C=C\C([O-])=O VZCYOOQTPOCHFL-OWOJBTEDSA-L 0.000 description 1
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- PUYCICVJCRLABY-UHFFFAOYSA-N heptane;oxolane Chemical compound C1CCOC1.CCCCCCC PUYCICVJCRLABY-UHFFFAOYSA-N 0.000 description 1
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- IGYWDTYEDKKTLK-UHFFFAOYSA-N methyl 3-hydroxy-4-oxo-7,8,9,10-tetrahydro-6h-pyrimido[1,2-a]azepine-2-carboxylate Chemical compound C1CCCCN2C(=O)C(O)=C(C(=O)OC)N=C21 IGYWDTYEDKKTLK-UHFFFAOYSA-N 0.000 description 1
- IWOUDGARURIUCJ-UHFFFAOYSA-N methyl 4-oxo-3-phenylmethoxy-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidine-2-carboxylate Chemical compound COC(=O)C=1N=C2CCCCN2C(=O)C=1OCC1=CC=CC=C1 IWOUDGARURIUCJ-UHFFFAOYSA-N 0.000 description 1
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- QUHQMUZDZWHIPO-UHFFFAOYSA-N n-[(4-fluorophenyl)methyl]-3-hydroxy-9-(methylamino)-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidine-2-carboxamide Chemical compound CNC1CCCN(C(C=2O)=O)C1=NC=2C(=O)NCC1=CC=C(F)C=C1 QUHQMUZDZWHIPO-UHFFFAOYSA-N 0.000 description 1
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- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 description 1
- 108700004029 pol Genes Proteins 0.000 description 1
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- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
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- JUJWROOIHBZHMG-RALIUCGRSA-N pyridine-d5 Chemical compound [2H]C1=NC([2H])=C([2H])C([2H])=C1[2H] JUJWROOIHBZHMG-RALIUCGRSA-N 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Virology (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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| US52877603P | 2003-12-12 | 2003-12-12 | |
| US60/528,776 | 2003-12-12 |
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| RU2005123807A RU2005123807A (ru) | 2006-01-20 |
| RU2329265C2 true RU2329265C2 (ru) | 2008-07-20 |
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| EC (1) | ECSP055890A (enExample) |
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| PL (1) | PL377354A1 (enExample) |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2561130C2 (ru) * | 2009-07-02 | 2015-08-20 | Санофи | НОВЫЕ ПРОИЗВОДНЫЕ 1,2,3,4-ТЕТРАГИДРОПИРИМИДО{1,2-a}ПИРИМИДИН-6-ОНА, ИХ ПОЛУЧЕНИЕ И ФАРМАЦЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ |
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| US7135467B2 (en) * | 2003-01-13 | 2006-11-14 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| JP2007509149A (ja) * | 2003-10-20 | 2007-04-12 | 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ヒドロキシピリドピロロピラジンジオン化合物 |
| AR046938A1 (es) * | 2003-12-12 | 2006-01-04 | Merck & Co Inc | Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares |
| TW200526635A (en) * | 2003-12-22 | 2005-08-16 | Shionogi & Co | Hydroxypyrimidinone derivative having HIV integrase inhibitory activity |
| US7273859B2 (en) * | 2004-05-12 | 2007-09-25 | Bristol-Myers Squibb Company | HIV integrase inhibitors: cyclic pyrimidinone compounds |
| US7115601B2 (en) | 2004-05-18 | 2006-10-03 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7176196B2 (en) * | 2004-05-28 | 2007-02-13 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7173022B2 (en) * | 2004-05-28 | 2007-02-06 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7157447B2 (en) | 2004-05-28 | 2007-01-02 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7192948B2 (en) * | 2004-05-28 | 2007-03-20 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| WO2006060225A2 (en) * | 2004-11-23 | 2006-06-08 | Merck & Co., Inc. | Process for asymmetric synthesis of hexahydropyrimido[1,2-a] azepine-2-carboxamides and related compounds |
| MX2007006637A (es) * | 2004-12-03 | 2007-06-19 | Merck & Co Inc | Uso de atazanavir para mejorar los parametros farmacocineticos de farmacos metabolizados por isoforma 1a1 de udp-glucuronosil- transferasa. |
| UA87884C2 (uk) * | 2004-12-03 | 2009-08-25 | Мерк Энд Ко., Инк. | Безводна кристалічна калієва сіль інгібітора віл-інтегрази |
| JP5228488B2 (ja) * | 2004-12-03 | 2013-07-03 | メルク・シャープ・アンド・ドーム・コーポレーション | 放出速度調節組成物を含有しているカルボキサミドｈｉｖインテグラーゼ阻害薬の医薬配合物 |
| TR201907729T4 (tr) | 2004-12-03 | 2019-06-21 | Merck Sharp & Dohme | Bir anti-çekirdekleştirici ajan içeren farmasötik bileşim. |
| ATE516026T1 (de) * | 2005-02-21 | 2011-07-15 | Shionogi & Co | Bicyclisches carbamoylpyridonderivat mit hiv- integrase-hemmender wirkung |
| AU2006228278C1 (en) * | 2005-03-31 | 2011-06-23 | Msd Italia S.R.L. | HIV integrase inhibitors |
| PT1874117E (pt) | 2005-04-28 | 2013-10-17 | Shionogi & Co | Derivado policíclico de carbamoílpiridona possuindo actividade inibidora de hiv-integrasse |
| EP1896448A1 (en) | 2005-06-30 | 2008-03-12 | Wyeth | AMINO-5-(6-MEMBERED)HETEROARYLIMIDAZOLONE COMPOUNDS AND THE USE THEREOF FOR ß-SECRETASE MODULATION |
| US7494984B2 (en) * | 2005-08-31 | 2009-02-24 | Bristol-Myers Squibb Company | Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors |
| CA2622639C (en) * | 2005-10-04 | 2012-01-03 | Istituto Di Recerche Di Biologia Molecolare P. Angeletti S.P.A. | Hiv integrase inhibitors |
| AU2006306355A1 (en) * | 2005-10-27 | 2007-05-03 | Merck & Co., Inc. | HIV integrase inhibitors |
| AU2006307101A1 (en) | 2005-10-27 | 2007-05-03 | Shionogi & Co., Ltd. | Polycyclic carbamoylpyridone derivative having inhibitory activity on HIV integrase |
| WO2007058646A1 (en) * | 2005-11-15 | 2007-05-24 | Bristol-Myers Squibb Company | Hiv integrase inhibitors: cyclic pyrimidinone compounds |
| US7897592B2 (en) * | 2005-11-15 | 2011-03-01 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7902182B2 (en) * | 2005-11-16 | 2011-03-08 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US8039458B2 (en) * | 2005-11-17 | 2011-10-18 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
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| RU2561130C2 (ru) * | 2009-07-02 | 2015-08-20 | Санофи | НОВЫЕ ПРОИЗВОДНЫЕ 1,2,3,4-ТЕТРАГИДРОПИРИМИДО{1,2-a}ПИРИМИДИН-6-ОНА, ИХ ПОЛУЧЕНИЕ И ФАРМАЦЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ |
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| EP1578748A1 (en) | 2005-09-28 |
| AU2003292436A1 (en) | 2004-07-22 |
| CN1753892A (zh) | 2006-03-29 |
| CN100343253C (zh) | 2007-10-17 |
| US20080176869A1 (en) | 2008-07-24 |
| IS7892A (is) | 2005-06-13 |
| MA27583A1 (fr) | 2005-10-03 |
| AU2003292436B2 (en) | 2009-07-30 |
| JP4733986B2 (ja) | 2011-07-27 |
| US7968553B2 (en) | 2011-06-28 |
| JP2006513200A (ja) | 2006-04-20 |
| NZ540729A (en) | 2008-03-28 |
| US20060046985A1 (en) | 2006-03-02 |
| KR20050087865A (ko) | 2005-08-31 |
| CA2509554C (en) | 2011-02-01 |
| AU2003292437A1 (en) | 2004-07-22 |
| NO20053624L (no) | 2005-09-26 |
| MXPA05007010A (es) | 2005-08-18 |
| ATE481401T1 (de) | 2010-10-15 |
| EP1578748B1 (en) | 2010-09-15 |
| RU2005123807A (ru) | 2006-01-20 |
| ECSP055890A (es) | 2005-09-20 |
| US7414045B2 (en) | 2008-08-19 |
| WO2004058757A1 (en) | 2004-07-15 |
| PL377354A1 (pl) | 2006-01-23 |
| WO2004058756A1 (en) | 2004-07-15 |
| HRP20050593A2 (en) | 2006-03-31 |
| BR0317749A (pt) | 2005-11-22 |
| CA2509554A1 (en) | 2004-07-15 |
| NO20053624D0 (no) | 2005-07-26 |
| DE60334248D1 (de) | 2010-10-28 |
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