PE20060242A1 - Heterociclicos biciclicos como inhibidores de la integrasa del vih - Google Patents
Heterociclicos biciclicos como inhibidores de la integrasa del vihInfo
- Publication number
- PE20060242A1 PE20060242A1 PE2005000602A PE2005000602A PE20060242A1 PE 20060242 A1 PE20060242 A1 PE 20060242A1 PE 2005000602 A PE2005000602 A PE 2005000602A PE 2005000602 A PE2005000602 A PE 2005000602A PE 20060242 A1 PE20060242 A1 PE 20060242A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- fluoro
- phenyl
- oxazin
- carboxamide
- Prior art date
Links
- 108010002459 HIV Integrase Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- -1 (4-FLUOROPHENYL) METHYL Chemical group 0.000 abstract 3
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 3
- BAVYZALUXZFZLV-UHFFFAOYSA-N Methylamine Chemical compound NC BAVYZALUXZFZLV-UHFFFAOYSA-N 0.000 abstract 2
- YHWMFDLNZGIJSD-UHFFFAOYSA-N 2h-1,4-oxazine Chemical compound C1OC=CN=C1 YHWMFDLNZGIJSD-UHFFFAOYSA-N 0.000 abstract 1
- LDSKYBVNIGKJHA-UHFFFAOYSA-N 2h-1,4-oxazine-2-carboxamide Chemical compound NC(=O)C1OC=CN=C1 LDSKYBVNIGKJHA-UHFFFAOYSA-N 0.000 abstract 1
- HFHGVIBGEFYIFU-UHFFFAOYSA-N 3h-oxazepine-2-carboxamide Chemical compound NC(=O)N1CC=CC=CO1 HFHGVIBGEFYIFU-UHFFFAOYSA-N 0.000 abstract 1
- UGFAIRIUMAVXCW-UHFFFAOYSA-N Carbon monoxide Chemical compound [O+]#[C-] UGFAIRIUMAVXCW-UHFFFAOYSA-N 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 208000037357 HIV infectious disease Diseases 0.000 abstract 1
- 102100034343 Integrase Human genes 0.000 abstract 1
- 108010061833 Integrases Proteins 0.000 abstract 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 abstract 1
- SFJGCXYXEFWEBK-UHFFFAOYSA-N oxazepine Chemical compound O1C=CC=CC=N1 SFJGCXYXEFWEBK-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/04—Ortho-condensed 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring 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
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE R1 ES (4-FLUOROFENIL)METIL, [4-FLUORO-2-(METILAMINO-CARBONIL)FENIL]METIL, 3-[3,4-DICLOROFENIL]PROPIL, ENTRE OTROS; R2 ES H, ALQUILO (C1-C6), OH, O-(ALQUILO C1-C6); R3 ES H, HALO, CIANO, ENTRE OTROS; X, Y, Z JUNTO AL ANILLO AL QUE ESTA UNIDO ES DE PREFERENCIA PIRIMIDO[2,1-c][1,4]OXAZIN, PIRIMIDO[2,1-c][1,4]OXAZEPIN. SON COMPUESTOS PREFERIDOS: N-[[4-FLUORO-2-[(METILAMINO)CARBONIL]FENIL]METIL]-4,6,7,9-TETRAHIDRO-3-HIDROXI-9,9-DIMETIL-4-OXO-PIRIMIDO[2,1-C][1,4]OXAZIN-2-CARBOXAMIDA; 9,9-DIETIL-N-[[4-FLUORO-2-(1H-1,2,4-TRIAZOL-1-IL)FENIL)METIL]-4,6,7,9-TETRAHIDRO-3-HIDROXI-4-OXO-PIRIMIDO[2,1-C][1,4]OXAZIN-2-CARBOXAMIDA, N-[[4-FLUORO-2-(1H-1,2,4-TRIAZOL-1-IL]FENIL]METIL]-4,7,8,10-TETRAHIDRO-3-HIDROXI-10,10-DIMETIL-4-OXO-6H-PIRIMIDO[2,1-C][1,4]OXAZEPIN-2-CARBOXAMIDA. REFERIDA TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA INTEGRASA DEL VIH, UTILES EN EL TRATAMIENTO DE INFECCION POR VIH
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US57551304P | 2004-05-28 | 2004-05-28 | |
| US60337104P | 2004-08-20 | 2004-08-20 | |
| US11/126,891 US7176196B2 (en) | 2004-05-28 | 2005-05-11 | Bicyclic heterocycles as HIV integrase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20060242A1 true PE20060242A1 (es) | 2006-03-31 |
Family
ID=35456854
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2005000602A PE20060242A1 (es) | 2004-05-28 | 2005-05-30 | Heterociclicos biciclicos como inhibidores de la integrasa del vih |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US7176196B2 (es) |
| EP (1) | EP1749011B1 (es) |
| JP (1) | JP4874959B2 (es) |
| KR (1) | KR101097623B1 (es) |
| AR (1) | AR049124A1 (es) |
| AT (1) | ATE412656T1 (es) |
| AU (1) | AU2005250356C1 (es) |
| BR (1) | BRPI0511623A (es) |
| CA (1) | CA2568356C (es) |
| CY (1) | CY1110266T1 (es) |
| DE (1) | DE602005010690D1 (es) |
| DK (1) | DK1749011T3 (es) |
| ES (1) | ES2315875T3 (es) |
| HR (1) | HRP20090005T3 (es) |
| IL (1) | IL179455A (es) |
| MX (1) | MXPA06013835A (es) |
| NO (1) | NO20065879L (es) |
| NZ (1) | NZ551282A (es) |
| PE (1) | PE20060242A1 (es) |
| PL (1) | PL1749011T3 (es) |
| PT (1) | PT1749011E (es) |
| RS (1) | RS50700B (es) |
| RU (1) | RU2381228C2 (es) |
| SI (1) | SI1749011T1 (es) |
| TW (1) | TWI366567B (es) |
| WO (1) | WO2005118593A1 (es) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7115601B2 (en) | 2004-05-18 | 2006-10-03 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| AU2006228278C1 (en) * | 2005-03-31 | 2011-06-23 | Msd Italia S.R.L. | HIV integrase inhibitors |
| US7494984B2 (en) * | 2005-08-31 | 2009-02-24 | Bristol-Myers Squibb Company | Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors |
| WO2007039218A1 (en) * | 2005-10-04 | 2007-04-12 | Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa | Hiv integrase inhibitors |
| US7902182B2 (en) * | 2005-11-16 | 2011-03-08 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| WO2007064316A1 (en) * | 2005-11-30 | 2007-06-07 | Bristol-Myers Squibb Company | Bicyclic heterocycles as hiv integrase inhibitors |
| US20070129379A1 (en) * | 2005-12-01 | 2007-06-07 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
| WO2007064502A1 (en) * | 2005-12-01 | 2007-06-07 | Bristol-Myers Squibb Company | Forms of n-[(4-fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide |
| WO2007143446A1 (en) * | 2006-05-30 | 2007-12-13 | Bristol-Myers Squibb Company | Spiro-condensed heterotricyclic compounds as hiv integrase inhibitors |
| US7893055B2 (en) * | 2006-06-28 | 2011-02-22 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US20100092427A1 (en) * | 2006-07-19 | 2010-04-15 | The University Of Georgia Research Foundation | Pyridinone Diketo Acids: Inhibitors of HIV Replication in Combination Therapy |
| US7763630B2 (en) * | 2007-06-06 | 2010-07-27 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US8129398B2 (en) * | 2008-03-19 | 2012-03-06 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| EP2280980B1 (en) * | 2008-03-27 | 2016-03-23 | Bristol-Myers Squibb Company | Crystalline form of n-[[4-fluoro-2-(5-methyl-1h-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate |
| CN102239172A (zh) * | 2008-10-06 | 2011-11-09 | 默沙东公司 | Hiv整合酶抑制剂 |
| US8143244B2 (en) * | 2009-02-26 | 2012-03-27 | Bristol-Myers Squibb Company | Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors |
| ES2446720T3 (es) | 2009-10-13 | 2014-03-10 | Elanco Animal Health Ireland Limited | Inhibidores de la integrasa macrocíclica |
| US8383639B2 (en) * | 2009-10-15 | 2013-02-26 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| PH12012501095A1 (en) | 2009-12-07 | 2015-04-22 | Univ Georgia | Pyridinone hydroxycyclopentyl carboxamides: hiv integrase inhibitors with therapeutic applications |
| SMT201800290T1 (it) | 2010-01-27 | 2018-07-17 | Viiv Healthcare Co | Terapia antivirale |
| US8716293B2 (en) | 2010-04-02 | 2014-05-06 | Janssen R&D Ireland | Macrocyclic integrase inhibitors |
| ES2603032T3 (es) | 2010-07-15 | 2017-02-23 | Bayer Intellectual Property Gmbh | Compuestos de 3-piridil-heteroarilcarboxamida como pesticidas |
| US8791108B2 (en) | 2011-08-18 | 2014-07-29 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| EP2785184B1 (en) | 2011-11-30 | 2020-06-10 | Emory University | Compositions comprising jak inhibitors and haart drugs for use in the prevention or treatment of hiv |
| JP2015508417A (ja) * | 2012-01-26 | 2015-03-19 | クロ コンサルティング リミテッド | 神経変性障害を治療するためのジアジリジン |
| WO2014099586A1 (en) | 2012-12-17 | 2014-06-26 | 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 |
| EP2997033B1 (en) | 2013-05-17 | 2017-11-15 | 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 |
| TN2016000090A1 (en) | 2013-09-27 | 2017-07-05 | Merck Sharp & Dohme | Substituted quinolizine derivatives useful as hiv integrase inhibitors. |
| WO2016187788A1 (en) | 2015-05-25 | 2016-12-01 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds useful for treating hiv infection |
| US10548910B2 (en) | 2015-11-17 | 2020-02-04 | 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 |
| EP3548031B1 (en) | 2016-12-02 | 2023-07-19 | Merck Sharp & Dohme LLC | Tricyclic heterocycle compounds useful 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) |
| EP3573984A4 (en) | 2017-01-26 | 2020-07-29 | Merck Sharp & Dohme Corp. | USEFUL SUBSTITUTE QUINOLIZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS |
| WO2021050555A1 (en) * | 2019-09-10 | 2021-03-18 | X-Chem, Inc. | Compositions and uses thereof |
| CN113912622B (zh) * | 2020-07-10 | 2023-12-01 | 上海纽思克生物科技有限公司 | 三环嘧啶酮类化合物、其制备方法、其组合物和用途 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5693641A (en) * | 1996-08-16 | 1997-12-02 | Berlex Laboratories Inc. | Bicyclic pyrimidine derivatives and their use as anti-coagulants |
| ATE355064T1 (de) | 2001-10-26 | 2006-03-15 | Angeletti P Ist Richerche Bio | Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase |
| CN102229605B (zh) | 2001-10-26 | 2015-01-14 | Msd意大利有限公司 | 关于hiv整合酶的n-取代的羟基嘧啶酮甲酰胺抑制剂 |
| EP1539762A2 (en) * | 2002-06-26 | 2005-06-15 | Bristol-Myers Squibb Company | Bicyclic pyrimidinones as coagulation cascade inhibitors |
| MXPA05007010A (es) | 2002-12-27 | 2005-08-18 | Angeletti P Ist Richerche Bio | Tetrahidro-4h-pirido[1,2-a]pirimidinas y compuestos relacionados utiles como inhibidores de la integrasa del virus de inmunodeficiencia humana. |
| 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 |
| BRPI0518741A2 (pt) | 2004-12-03 | 2008-12-02 | Merck & Co Inc | uso de uma combinaÇço de uma droga diretamente metabolizada por ugt1a1 ou um seu sal farmaceuticamente aceitÁvel e atazanavir ou um seu sal farmaceuticamente aceitÁvel, e, combinaÇço farmacÊutica para administraÇço oral a um mamÍfero |
| AU2006228278C1 (en) | 2005-03-31 | 2011-06-23 | Msd Italia S.R.L. | HIV integrase inhibitors |
-
2005
- 2005-05-11 US US11/126,891 patent/US7176196B2/en not_active Expired - Lifetime
- 2005-05-12 DK DK05750075T patent/DK1749011T3/da active
- 2005-05-12 ES ES05750075T patent/ES2315875T3/es not_active Expired - Lifetime
- 2005-05-12 SI SI200530481T patent/SI1749011T1/sl unknown
- 2005-05-12 NZ NZ551282A patent/NZ551282A/en not_active IP Right Cessation
- 2005-05-12 PT PT05750075T patent/PT1749011E/pt unknown
- 2005-05-12 AU AU2005250356A patent/AU2005250356C1/en not_active Ceased
- 2005-05-12 HR HR20090005T patent/HRP20090005T3/xx unknown
- 2005-05-12 RU RU2006146970/04A patent/RU2381228C2/ru not_active IP Right Cessation
- 2005-05-12 EP EP05750075A patent/EP1749011B1/en not_active Expired - Lifetime
- 2005-05-12 DE DE602005010690T patent/DE602005010690D1/de not_active Expired - Lifetime
- 2005-05-12 PL PL05750075T patent/PL1749011T3/pl unknown
- 2005-05-12 RS RSP-2008/0569A patent/RS50700B/sr unknown
- 2005-05-12 JP JP2007515142A patent/JP4874959B2/ja not_active Expired - Fee Related
- 2005-05-12 BR BRPI0511623-6A patent/BRPI0511623A/pt not_active IP Right Cessation
- 2005-05-12 MX MXPA06013835A patent/MXPA06013835A/es active IP Right Grant
- 2005-05-12 CA CA2568356A patent/CA2568356C/en not_active Expired - Fee Related
- 2005-05-12 WO PCT/US2005/016473 patent/WO2005118593A1/en not_active Ceased
- 2005-05-12 AT AT05750075T patent/ATE412656T1/de active
- 2005-05-25 TW TW094117105A patent/TWI366567B/zh not_active IP Right Cessation
- 2005-05-27 AR ARP050102187A patent/AR049124A1/es not_active Application Discontinuation
- 2005-05-30 PE PE2005000602A patent/PE20060242A1/es not_active Application Discontinuation
-
2006
- 2006-08-16 US US11/505,149 patent/US7511037B2/en not_active Expired - Lifetime
- 2006-11-21 IL IL179455A patent/IL179455A/en not_active IP Right Cessation
- 2006-12-19 NO NO20065879A patent/NO20065879L/no not_active Application Discontinuation
- 2006-12-27 KR KR1020067027455A patent/KR101097623B1/ko not_active Expired - Fee Related
-
2009
- 2009-01-19 CY CY20091100068T patent/CY1110266T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |