CY1110266T1 - Δικυκλικες ετεροκυκλικες ενωσεις ως αναστολεις της hiv ιντεγκρασης - Google Patents
Δικυκλικες ετεροκυκλικες ενωσεις ως αναστολεις της hiv ιντεγκρασηςInfo
- Publication number
- CY1110266T1 CY1110266T1 CY20091100068T CY091100068T CY1110266T1 CY 1110266 T1 CY1110266 T1 CY 1110266T1 CY 20091100068 T CY20091100068 T CY 20091100068T CY 091100068 T CY091100068 T CY 091100068T CY 1110266 T1 CY1110266 T1 CY 1110266T1
- Authority
- CY
- Cyprus
- Prior art keywords
- inhibitors
- hiv
- heterocyclic compounds
- bicyclic heterocyclic
- hiv integration
- Prior art date
Links
- 230000010354 integration Effects 0.000 title abstract 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 208000030507 AIDS Diseases 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 108010002459 HIV Integrase Proteins 0.000 abstract 1
- 208000037357 HIV infectious disease Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- -1 cyclic bicyclic pyrimidinone compounds Chemical class 0.000 abstract 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000003612 virological effect Effects 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
Η εφεύρεση περιλαμβάνει σειρά κυκλικών δικυκλικών ενώσεων πυριμιδινόνης του τύπου I οι οποίες αναστέλλουν την HIV ιντεγκράση και εμποδίζουν την ιική ολοκλήρωση στο ανθρώπινο DNA. Η δράση αυτή καθιστά τις ενώσεις χρήσιμες στην αντιμετώπιση της HIV μόλυνσης και του AIDS. Η εφεύρεση επίσης περιλαμβάνει φαρμακευτικές συνθέσεις και μεθόδους για τη θεραπεία ατόμων μολυσμένων με HIV.
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 |
| EP05750075A EP1749011B1 (en) | 2004-05-28 | 2005-05-12 | Bicyclic heterocycles as hiv integrase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1110266T1 true CY1110266T1 (el) | 2015-01-14 |
Family
ID=35456854
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20091100068T CY1110266T1 (el) | 2004-05-28 | 2009-01-19 | Δικυκλικες ετεροκυκλικες ενωσεις ως αναστολεις της hiv ιντεγκρασης |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US7176196B2 (el) |
| EP (1) | EP1749011B1 (el) |
| JP (1) | JP4874959B2 (el) |
| KR (1) | KR101097623B1 (el) |
| AR (1) | AR049124A1 (el) |
| AT (1) | ATE412656T1 (el) |
| AU (1) | AU2005250356C1 (el) |
| BR (1) | BRPI0511623A (el) |
| CA (1) | CA2568356C (el) |
| CY (1) | CY1110266T1 (el) |
| DE (1) | DE602005010690D1 (el) |
| DK (1) | DK1749011T3 (el) |
| ES (1) | ES2315875T3 (el) |
| HR (1) | HRP20090005T3 (el) |
| IL (1) | IL179455A (el) |
| MX (1) | MXPA06013835A (el) |
| NO (1) | NO20065879L (el) |
| NZ (1) | NZ551282A (el) |
| PE (1) | PE20060242A1 (el) |
| PL (1) | PL1749011T3 (el) |
| PT (1) | PT1749011E (el) |
| RS (1) | RS50700B (el) |
| RU (1) | RU2381228C2 (el) |
| SI (1) | SI1749011T1 (el) |
| TW (1) | TWI366567B (el) |
| WO (1) | WO2005118593A1 (el) |
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 |
| JP5116660B2 (ja) * | 2005-03-31 | 2013-01-09 | イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・エルレ・エルレ | Hivインテグラーゼ阻害剤 |
| 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 |
| 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 |
| 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 |
| MX2009000661A (es) * | 2006-07-19 | 2009-03-27 | Univ Georgia Res Found | Piridinon-diceto-acidos: inhibidores de replicacion de vih en terapia de combinacion. |
| 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 |
| WO2010042392A2 (en) * | 2008-10-06 | 2010-04-15 | Merck & Co., Inc. | Hiv integrase inhibitors |
| US8143244B2 (en) * | 2009-02-26 | 2012-03-27 | Bristol-Myers Squibb Company | Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors |
| AU2010305805B2 (en) | 2009-10-13 | 2014-04-03 | Elanco Animal Health Ireland Limited | Macrocyclic integrase inhibitors |
| US8383639B2 (en) | 2009-10-15 | 2013-02-26 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| SG181524A1 (en) | 2009-12-07 | 2012-07-30 | Univ Georgia | Pyridinone hydroxycyclopentyl carboxamides: hiv integrase inhibitors with therapeutic applications |
| EA032868B1 (ru) | 2010-01-27 | 2019-07-31 | Вайв Хелткер Компани | Комбинация для лечения вич-инфекции |
| 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 |
| CA3131037A1 (en) | 2011-11-30 | 2013-06-06 | Emory University | Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections |
| 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 |
| SI2997033T1 (en) | 2013-05-17 | 2018-04-30 | Merck Sharp & Dohme Corp. | FUZYCLE TRICYCLE HETEROCYCLIC COMPOUNDS AS HIV INTEGRATED INHIBITORS |
| EP3008044B1 (en) | 2013-06-13 | 2018-11-21 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
| HK1221648A1 (zh) | 2013-09-27 | 2017-06-09 | Merck Sharp & Dohme Corp. | 用作hiv整合酶抑制劑的取代喹嗪衍生物 |
| WO2016187788A1 (en) | 2015-05-25 | 2016-12-01 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds useful for treating hiv infection |
| WO2017087257A1 (en) | 2015-11-17 | 2017-05-26 | 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 |
| KR20190086017A (ko) | 2016-12-02 | 2019-07-19 | 머크 샤프 앤드 돔 코포레이션 | Hiv 인테그라제 억제제로서 유용한 트리시클릭 헤테로사이클 화합물 |
| 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) |
| US10786488B2 (en) | 2017-01-26 | 2020-09-29 | 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 (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 |
| SI1441735T1 (sl) | 2001-10-26 | 2006-06-30 | Angeletti P Ist Richerche Bio | N-substituirani hidroksipirimidinon-karboksamidniinhibitorji HIV-integraze |
| AU2002334205B2 (en) | 2001-10-26 | 2007-07-05 | Istituto Di Ricerche Di Biologia Molecolara P. Angeletti Spa | Dihydroxypyrimidine carboxamide inhibitors of HIV integrase |
| WO2004002406A2 (en) | 2002-06-26 | 2004-01-08 | Bristol-Myers Squibb Company | Bicyclic pyrimidinones as coagulation cascade inhibitors |
| AU2003292437A1 (en) | 2002-12-27 | 2004-07-22 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa | 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 |
| JP5116660B2 (ja) | 2005-03-31 | 2013-01-09 | イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・エルレ・エルレ | Hivインテグラーゼ阻害剤 |
-
2005
- 2005-05-11 US US11/126,891 patent/US7176196B2/en not_active Expired - Lifetime
- 2005-05-12 WO PCT/US2005/016473 patent/WO2005118593A1/en not_active Ceased
- 2005-05-12 HR HR20090005T patent/HRP20090005T3/xx unknown
- 2005-05-12 AU AU2005250356A patent/AU2005250356C1/en not_active Ceased
- 2005-05-12 JP JP2007515142A patent/JP4874959B2/ja not_active Expired - Fee Related
- 2005-05-12 PT PT05750075T patent/PT1749011E/pt unknown
- 2005-05-12 BR BRPI0511623-6A patent/BRPI0511623A/pt not_active IP Right Cessation
- 2005-05-12 CA CA2568356A patent/CA2568356C/en not_active Expired - Fee Related
- 2005-05-12 ES ES05750075T patent/ES2315875T3/es not_active Expired - Lifetime
- 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 SI SI200530481T patent/SI1749011T1/sl unknown
- 2005-05-12 AT AT05750075T patent/ATE412656T1/de active
- 2005-05-12 DK DK05750075T patent/DK1749011T3/da active
- 2005-05-12 DE DE602005010690T patent/DE602005010690D1/de not_active Expired - Lifetime
- 2005-05-12 MX MXPA06013835A patent/MXPA06013835A/es active IP Right Grant
- 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
- 2005-05-25 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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