HRP20090005T3 - Bicyclic heterocycles as hiv integrase inhibitors - Google Patents
Bicyclic heterocycles as hiv integrase inhibitorsInfo
- Publication number
- HRP20090005T3 HRP20090005T3 HR20090005T HRP20090005T HRP20090005T3 HR P20090005 T3 HRP20090005 T3 HR P20090005T3 HR 20090005 T HR20090005 T HR 20090005T HR P20090005 T HRP20090005 T HR P20090005T HR P20090005 T3 HRP20090005 T3 HR P20090005T3
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- hydrogen
- alkoxy
- 6alkyl
- cyano
- Prior art date
Links
- 229940099797 HIV integrase inhibitor Drugs 0.000 title 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 title 1
- 239000003084 hiv integrase inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 15
- 229910052739 hydrogen Inorganic materials 0.000 abstract 11
- 239000001257 hydrogen Substances 0.000 abstract 11
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 11
- -1 dioxothiazinyl Chemical group 0.000 abstract 10
- 125000003545 alkoxy group Chemical group 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 1
- 101100440695 Dictyostelium discoideum corB gene Proteins 0.000 abstract 1
- 101100134925 Gallus gallus COR6 gene Proteins 0.000 abstract 1
- 101100203602 Hypocrea jecorina (strain QM6a) sor7 gene Proteins 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000004005 formimidoyl group Chemical group [H]\N=C(/[H])* 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000001786 isothiazolyl group Chemical group 0.000 abstract 1
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 125000001715 oxadiazolyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000005429 oxyalkyl group Chemical group 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001113 thiadiazolyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 abstract 1
- 125000001425 triazolyl group Chemical group 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (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 (4)
| 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 |
| PCT/US2005/016473 WO2005118593A1 (en) | 2004-05-28 | 2005-05-12 | Bicyclic heterocycles as hiv integrase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20090005T3 true HRP20090005T3 (en) | 2009-02-28 |
Family
ID=35456854
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20090005T HRP20090005T3 (en) | 2004-05-28 | 2009-01-07 | Bicyclic heterocycles as hiv integrase inhibitors |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US7176196B2 (xx) |
| EP (1) | EP1749011B1 (xx) |
| JP (1) | JP4874959B2 (xx) |
| KR (1) | KR101097623B1 (xx) |
| AR (1) | AR049124A1 (xx) |
| AT (1) | ATE412656T1 (xx) |
| AU (1) | AU2005250356C1 (xx) |
| BR (1) | BRPI0511623A (xx) |
| CA (1) | CA2568356C (xx) |
| CY (1) | CY1110266T1 (xx) |
| DE (1) | DE602005010690D1 (xx) |
| DK (1) | DK1749011T3 (xx) |
| ES (1) | ES2315875T3 (xx) |
| HK (1) | HK1107343A1 (xx) |
| HR (1) | HRP20090005T3 (xx) |
| IL (1) | IL179455A (xx) |
| MX (1) | MXPA06013835A (xx) |
| NO (1) | NO20065879L (xx) |
| NZ (1) | NZ551282A (xx) |
| PE (1) | PE20060242A1 (xx) |
| PL (1) | PL1749011T3 (xx) |
| PT (1) | PT1749011E (xx) |
| RS (1) | RS50700B (xx) |
| RU (1) | RU2381228C2 (xx) |
| SI (1) | SI1749011T1 (xx) |
| TW (1) | TWI366567B (xx) |
| WO (1) | WO2005118593A1 (xx) |
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 |
| US7981879B2 (en) * | 2005-03-31 | 2011-07-19 | Instituto di Ricerchi 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 |
| AU2006299042B8 (en) * | 2005-10-04 | 2011-09-15 | 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 |
| EP2046328A4 (en) * | 2006-07-19 | 2009-10-28 | Univ Georgia Res Found | PYRIDINONE DIKETOIC 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 |
| 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 |
| CA2738814C (en) * | 2008-10-06 | 2014-01-28 | 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 |
| CN102574854B (zh) | 2009-10-13 | 2014-04-16 | 伊兰科动物健康爱尔兰有限公司 | 大环整合酶抑制剂 |
| US8383639B2 (en) | 2009-10-15 | 2013-02-26 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| JP2013512957A (ja) | 2009-12-07 | 2013-04-18 | 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 | ピリジノンヒドロキシシクロペンチルカルボキサミド類：治療用途を備えたｈｉｖインテグラーゼ阻害剤 |
| CA3003988C (en) | 2010-01-27 | 2020-01-07 | Viiv Healthcare Company | Combinations for use in the inhibition of hiv-1 |
| EP2552923B1 (en) | 2010-04-02 | 2014-03-26 | Janssen R&D Ireland | Macrocyclic integrase inhibitors |
| BR112013000925A2 (pt) | 2010-07-15 | 2020-12-01 | Bayer Intellectual Property Gmbh | compostos heterocíclicos como pesticidas |
| US8791108B2 (en) | 2011-08-18 | 2014-07-29 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| EP3750544A3 (en) | 2011-11-30 | 2021-03-24 | Emory University | Jak inhibitors for use in the prevention or treatment of viral infection |
| EP2807149A2 (en) * | 2012-01-26 | 2014-12-03 | CRO Consulting Limited | Agents for treating neurodegenerative disorders |
| 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 |
| 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 |
| KR101809392B1 (ko) | 2013-09-27 | 2017-12-14 | 머크 샤프 앤드 돔 코포레이션 | Hiv 인테그라제 억제제로서 유용한 치환된 퀴놀리진 유도체 |
| 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 |
| 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) |
| WO2018140368A1 (en) | 2017-01-26 | 2018-08-02 | Merck Sharp & Dohme Corp. | Substituted quinolizine derivatives useful 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 (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1441734E (pt) | 2001-10-26 | 2007-05-31 | Isti Di Ric Di Bio Moleco P An | Di-hidroxipirimidinocarboxamidas inibidoras da integrase do vih |
| ES2258668T3 (es) | 2001-10-26 | 2006-09-01 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Hidroxipirimidina carboxamidas n-sustituidas inhibidoras de hiv integrasa. |
| US7094783B2 (en) | 2002-06-26 | 2006-08-22 | Bristol-Myers Squibb Company | Bicyclic pyrimidinones as coagulation cascade inhibitors |
| EP1578748B1 (en) | 2002-12-27 | 2010-09-15 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | 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 |
| US7981879B2 (en) | 2005-03-31 | 2011-07-19 | Instituto di Ricerchi di Biologia Molecolare P. Angeletti S.p.A. | HIV integrase inhibitors |
-
2005
- 2005-05-11 US US11/126,891 patent/US7176196B2/en active Active
- 2005-05-12 CA CA2568356A patent/CA2568356C/en not_active Expired - Fee Related
- 2005-05-12 DE DE602005010690T patent/DE602005010690D1/de active Active
- 2005-05-12 AU AU2005250356A patent/AU2005250356C1/en not_active Ceased
- 2005-05-12 SI SI200530481T patent/SI1749011T1/sl unknown
- 2005-05-12 ES ES05750075T patent/ES2315875T3/es active Active
- 2005-05-12 PT PT05750075T patent/PT1749011E/pt unknown
- 2005-05-12 WO PCT/US2005/016473 patent/WO2005118593A1/en active Application Filing
- 2005-05-12 BR BRPI0511623-6A patent/BRPI0511623A/pt not_active IP Right Cessation
- 2005-05-12 NZ NZ551282A patent/NZ551282A/en not_active IP Right Cessation
- 2005-05-12 PL PL05750075T patent/PL1749011T3/pl unknown
- 2005-05-12 RU RU2006146970/04A patent/RU2381228C2/ru not_active IP Right Cessation
- 2005-05-12 EP EP05750075A patent/EP1749011B1/en active Active
- 2005-05-12 RS RSP-2008/0569A patent/RS50700B/sr unknown
- 2005-05-12 DK DK05750075T patent/DK1749011T3/da active
- 2005-05-12 MX MXPA06013835A patent/MXPA06013835A/es active IP Right Grant
- 2005-05-12 JP JP2007515142A patent/JP4874959B2/ja not_active Expired - Fee Related
- 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 active Active
- 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 IP Right Cessation
-
2007
- 2007-11-26 HK HK07112893.6A patent/HK1107343A1/xx not_active IP Right Cessation
-
2009
- 2009-01-07 HR HR20090005T patent/HRP20090005T3/xx unknown
- 2009-01-19 CY CY20091100068T patent/CY1110266T1/el unknown
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