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)
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 (https=) |
| EP (1) | EP1749011B1 (https=) |
| JP (1) | JP4874959B2 (https=) |
| KR (1) | KR101097623B1 (https=) |
| AR (1) | AR049124A1 (https=) |
| AT (1) | ATE412656T1 (https=) |
| AU (1) | AU2005250356C1 (https=) |
| BR (1) | BRPI0511623A (https=) |
| CA (1) | CA2568356C (https=) |
| CY (1) | CY1110266T1 (https=) |
| DE (1) | DE602005010690D1 (https=) |
| DK (1) | DK1749011T3 (https=) |
| ES (1) | ES2315875T3 (https=) |
| HR (1) | HRP20090005T3 (https=) |
| IL (1) | IL179455A (https=) |
| MX (1) | MXPA06013835A (https=) |
| NO (1) | NO20065879L (https=) |
| NZ (1) | NZ551282A (https=) |
| PE (1) | PE20060242A1 (https=) |
| PL (1) | PL1749011T3 (https=) |
| PT (1) | PT1749011E (https=) |
| RS (1) | RS50700B (https=) |
| RU (1) | RU2381228C2 (https=) |
| SI (1) | SI1749011T1 (https=) |
| TW (1) | TWI366567B (https=) |
| WO (1) | WO2005118593A1 (https=) |
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 |
| CA2600832C (en) * | 2005-03-31 | 2011-12-13 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | 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 |
| US7939537B2 (en) | 2005-10-04 | 2011-05-10 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | 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 |
| JP2009543865A (ja) * | 2006-07-19 | 2009-12-10 | ユニバーシティ オブ ジョージア リサーチ ファウンデーション， インコーポレーテッド | ピリジノンジケト酸：併用療法におけるｈｉｖ複製の阻害剤 |
| 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 |
| WO2009120841A1 (en) * | 2008-03-27 | 2009-10-01 | 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 |
| WO2010042391A2 (en) * | 2008-10-06 | 2010-04-15 | 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 |
| 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 |
| EA201270651A1 (ru) | 2009-12-07 | 2013-01-30 | Юниверсити Оф Джорджия Рисерч Фаундейшн, Инк. | Карбоксамиды пиридинон гидроксициклопентила: ингибиторы вич интегразы и области терапевтического применения |
| LT3494972T (lt) | 2010-01-27 | 2024-03-12 | Viiv Healthcare Company | Dolutegraviro ir lamivudino kompozicija živ infekcijai gydyti |
| WO2011121105A1 (en) | 2010-04-02 | 2011-10-06 | Tibotec Pharmaceuticals | Macrocyclic integrase inhibitors |
| JP5996532B2 (ja) | 2010-07-15 | 2016-09-21 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 有害生物防除剤としての新規複素環式化合物 |
| 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 |
| WO2013111118A2 (en) * | 2012-01-26 | 2013-08-01 | Cro Consulting Limited | Agents for treating neurodegenerative disorders |
| EP2931730B1 (en) | 2012-12-17 | 2019-08-07 | 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 |
| RS56701B1 (sr) | 2013-05-17 | 2018-03-30 | Merck Sharp & Dohme | Fuzionisana triciklična heterociklična jedinjenja kao inhibitori hiv integraze |
| EP3008044B1 (en) | 2013-06-13 | 2018-11-21 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
| UA117499C2 (uk) | 2013-09-27 | 2018-08-10 | Мерк Шарп Енд Доум Корп. | Заміщені похідні хінолізину, які можна використовувати як інгібітори інтегрази віл |
| 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 |
| US10544155B2 (en) | 2015-12-15 | 2020-01-28 | 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 |
| 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) |
| CA3042314A1 (en) | 2016-12-02 | 2018-06-07 | Merck Sharp & Dohme Corp. | Tricyclic heterocycle compounds useful as hiv integrase inhibitors |
| 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 |
| IL161337A0 (en) | 2001-10-26 | 2004-09-27 | Angeletti P Ist Richerche Bio | N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase |
| EP1539762A2 (en) | 2002-06-26 | 2005-06-15 | Bristol-Myers Squibb Company | Bicyclic pyrimidinones as coagulation cascade inhibitors |
| NZ540729A (en) | 2002-12-27 | 2008-03-28 | Angeletti P Ist Richerche Bio | 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 |
| 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 |
| CA2600832C (en) | 2005-03-31 | 2011-12-13 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Hiv integrase inhibitors |
-
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 RU RU2006146970/04A patent/RU2381228C2/ru not_active IP Right Cessation
- 2005-05-12 RS RSP-2008/0569A patent/RS50700B/sr unknown
- 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 WO PCT/US2005/016473 patent/WO2005118593A1/en not_active Ceased
- 2005-05-12 NZ NZ551282A patent/NZ551282A/en not_active IP Right Cessation
- 2005-05-12 CA CA2568356A patent/CA2568356C/en not_active Expired - Fee Related
- 2005-05-12 BR BRPI0511623-6A patent/BRPI0511623A/pt not_active IP Right Cessation
- 2005-05-12 ES ES05750075T patent/ES2315875T3/es not_active Expired - Lifetime
- 2005-05-12 DK DK05750075T patent/DK1749011T3/da active
- 2005-05-12 HR HR20090005T patent/HRP20090005T3/xx unknown
- 2005-05-12 MX MXPA06013835A patent/MXPA06013835A/es active IP Right Grant
- 2005-05-12 PT PT05750075T patent/PT1749011E/pt unknown
- 2005-05-12 PL PL05750075T patent/PL1749011T3/pl unknown
- 2005-05-12 SI SI200530481T patent/SI1749011T1/sl unknown
- 2005-05-12 JP JP2007515142A patent/JP4874959B2/ja not_active Expired - Fee Related
- 2005-05-12 AU AU2005250356A patent/AU2005250356C1/en not_active Ceased
- 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 |