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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (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 |
| CN101146811B (zh) * | 2005-03-31 | 2012-01-11 | P.安杰莱蒂分子生物学研究所 | Hiv整合酶抑制剂 |
| 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 |
| 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 |
| US20070129379A1 (en) * | 2005-12-01 | 2007-06-07 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
| US7897593B2 (en) * | 2006-05-30 | 2011-03-01 | Bristol-Myers Squibb Company | 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 |
| JP2011515491A (ja) * | 2008-03-27 | 2011-05-19 | ブリストル−マイヤーズ スクイブ カンパニー | N−[[4−フルオロ−2−(5−メチル−1H−1,2,4−トリアゾール−1−イル)フェニル]メチル]−4,6,7,9−テトラヒドロ−3−ヒドロキシ−9,9−ジメチル−4−オキソ−ピリミド[2,1−c][1,4]オキサジン−2−カルボキシアミド,ナトリウム塩一水和物の結晶形 |
| US8513234B2 (en) * | 2008-10-06 | 2013-08-20 | Merck Sharp & Dohme Corp. | HIV integrase inhibitors |
| US8143244B2 (en) * | 2009-02-26 | 2012-03-27 | Bristol-Myers Squibb Company | Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors |
| MX2012004426A (es) | 2009-10-13 | 2012-07-30 | Elanco Animal Health Ireland | Inhibidores macrociclicos de integrasa. |
| US8383639B2 (en) | 2009-10-15 | 2013-02-26 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| MX2012006485A (es) | 2009-12-07 | 2012-08-23 | Univ Georgia | Piridinon hidroxiclicopentil carboxamidas: inhibidores de la integrasa del vih con aplicaciones terapeuticas. |
| PH12012501537A1 (en) | 2010-01-27 | 2018-02-07 | Viiv Healthcare Co | Antiviral therapy |
| JP5739517B2 (ja) | 2010-04-02 | 2015-06-24 | ヤンセン・アールアンドデイ・アイルランド | 大環状インテグラーゼ阻害剤 |
| CN104086528A (zh) | 2010-07-15 | 2014-10-08 | 拜耳知识产权有限责任公司 | 作为杀虫剂的新杂环化合物 |
| US8791108B2 (en) | 2011-08-18 | 2014-07-29 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| ES3018133T3 (en) | 2011-11-30 | 2025-05-14 | Univ Emory | Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae |
| 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 |
| US9493479B2 (en) | 2013-04-16 | 2016-11-15 | Merck Sharp & Dohme Corp. | Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors |
| WO2014183532A1 (en) | 2013-05-17 | 2014-11-20 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
| US9951079B2 (en) | 2013-06-13 | 2018-04-24 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as HIV integrase inhibitors |
| EA030695B1 (ru) | 2013-09-27 | 2018-09-28 | Мерк Шарп И Доум Корп. | Замещенные производные хинолизина, которые можно использовать как ингибиторы интегразы вич |
| 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 |
| EP3389380B1 (en) | 2015-12-15 | 2021-07-21 | 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 |
| CN110062627A (zh) | 2016-12-02 | 2019-07-26 | 默沙东公司 | 可用作hiv整合酶抑制剂的三环杂环化合物 |
| 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 |
| HRP20040373B1 (en) | 2001-10-26 | 2012-09-30 | Instituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase |
| CA2463975A1 (en) | 2001-10-26 | 2003-05-01 | Maria Emilia Di Francesco | Dihydroxypyrimidine carboxamide inhibitors of hiv integrase |
| AU2003238304A1 (en) | 2002-06-26 | 2004-01-19 | Bristol-Myers Squibb Company | Bicyclic pyrimidinones as coagulation cascade inhibitors |
| HRP20050593A2 (en) | 2002-12-27 | 2006-03-31 | Instituto di Ricerche di Biologia Molecolare P. An | Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors |
| 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 |
| CA2588466A1 (en) | 2004-12-03 | 2006-06-08 | Merck & Co., Inc. | Use of atazanavir for improving the pharmacokinetics of drugs metabolized by ugt1a1 |
| CN101146811B (zh) | 2005-03-31 | 2012-01-11 | P.安杰莱蒂分子生物学研究所 | Hiv整合酶抑制剂 |
-
2005
- 2005-05-11 US US11/126,891 patent/US7176196B2/en not_active Expired - Lifetime
- 2005-05-12 AT AT05750075T patent/ATE412656T1/de active
- 2005-05-12 AU AU2005250356A patent/AU2005250356C1/en not_active Ceased
- 2005-05-12 BR BRPI0511623-6A patent/BRPI0511623A/pt not_active IP Right Cessation
- 2005-05-12 HR HR20090005T patent/HRP20090005T3/xx unknown
- 2005-05-12 RS RSP-2008/0569A patent/RS50700B/sr unknown
- 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 ES ES05750075T patent/ES2315875T3/es not_active Expired - Lifetime
- 2005-05-12 EP EP05750075A patent/EP1749011B1/en not_active Expired - Lifetime
- 2005-05-12 MX MXPA06013835A patent/MXPA06013835A/es active IP Right Grant
- 2005-05-12 WO PCT/US2005/016473 patent/WO2005118593A1/en not_active Ceased
- 2005-05-12 PL PL05750075T patent/PL1749011T3/pl unknown
- 2005-05-12 JP JP2007515142A patent/JP4874959B2/ja not_active Expired - Fee Related
- 2005-05-12 DE DE602005010690T patent/DE602005010690D1/de not_active Expired - Lifetime
- 2005-05-12 DK DK05750075T patent/DK1749011T3/da active
- 2005-05-12 RU RU2006146970/04A patent/RU2381228C2/ru not_active IP Right Cessation
- 2005-05-12 PT PT05750075T patent/PT1749011E/pt unknown
- 2005-05-12 CA CA2568356A patent/CA2568356C/en not_active Expired - Fee Related
- 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 |