MA29879B1 - Derive de carbamoylpyridone polycyclique ayant une activite d'inhibition sur l'integrase du vih - Google Patents
Derive de carbamoylpyridone polycyclique ayant une activite d'inhibition sur l'integrase du vihInfo
- Publication number
- MA29879B1 MA29879B1 MA30862A MA30862A MA29879B1 MA 29879 B1 MA29879 B1 MA 29879B1 MA 30862 A MA30862 A MA 30862A MA 30862 A MA30862 A MA 30862A MA 29879 B1 MA29879 B1 MA 29879B1
- Authority
- MA
- Morocco
- Prior art keywords
- optionally substituted
- lower alkyl
- substituted lower
- heterocycle
- hydrogen
- Prior art date
Links
- 108010002459 HIV Integrase Proteins 0.000 title abstract 2
- OHEKQGOBJIKKIF-AWEZNQCLSA-N (12as)-n-[(4-fluorophenyl)methyl]-7-hydroxy-6,8-dioxo-3,4,12,12a-tetrahydro-2h-pyrido[5,6]pyrazino[2,6-b][1,3]oxazine-9-carboxamide Chemical class C([C@@H]1OCCCN1C(=O)C1=C(C2=O)O)N1C=C2C(=O)NCC1=CC=C(F)C=C1 OHEKQGOBJIKKIF-AWEZNQCLSA-N 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 150000002431 hydrogen Chemical class 0.000 abstract 3
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 2
- 125000003107 substituted aryl group Chemical group 0.000 abstract 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 239000002259 anti human immunodeficiency virus agent Substances 0.000 abstract 1
- 229940124411 anti-hiv antiviral agent Drugs 0.000 abstract 1
- 230000000840 anti-viral effect Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic 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
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/20—Spiro-condensed systems
-
- 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
- C07D498/12—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 three hetero rings
- C07D498/14—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)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Molecular Biology (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Communicable Diseases (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 Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Consiste à proposer un nouveau composé ayant une activité anti-virale, particulièrement une activité inhibitrice de l'intégrase du VIH, et une composition pharmaceutique, particulièrement un agent anti-VIH. (dans laquelle R1 est un hydrogène ou un alkyle inférieur ; X est un alkylène inférieur, etc. : R2 est un aryle facultativement substitué ; R3 est un hydrogène, un halogène, un hydroxy, un alkyle inférieur facultativement substitué, etc. : R4 est un hydrogène, un alkyle inférieur facultativement substitué, un cycloalkyle facultativement substitué, un cycloalkyle alkyle inférieur facultativement substitué, un aryle facultativement substitué, un aryle alkyle inférieur facultativement substitué, un groupement hétérocyclique facultativement substitué, un hétérocycle alkyle inférieur facultativement substitué, etc. : Une ligne de tirets indique la présence ou l'absence d'une liaison ; B1 et B2 sont tels que l'un quelconque d'entre eux est un CR20R21, et l'autre est un NR22 et, dans ce cas, il n'y a pas de ligne de tirets. Quand B2 est un NR22, R4 et R22 peuvent être pris ensemble pour former un hétérocycle facultativement substitué ; Quand B2 est CHR21, R4 et R21 peuvent être pris ensemble pour former un hétérocycle facultativement substitué. À titre d'alternative, B1 et B2 sont indépendamment un C, un CR23 ou un N et, dans ce cas, B1 et B2 peuvent être pris ensemble pour former un hétérocycle. R20, R21, R22 et R23 sont indépendamment un hydrogène, un alkyle inférieur facultativement substitué, un cycloalkyle facultativement substitué, un cycloalkyle alkyle inférieur facultativement substitué, etc.)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2005312076 | 2005-10-27 | ||
| JP2006223875 | 2006-08-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MA29879B1 true MA29879B1 (fr) | 2008-10-03 |
Family
ID=37967785
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA30862A MA29879B1 (fr) | 2005-10-27 | 2008-04-23 | Derive de carbamoylpyridone polycyclique ayant une activite d'inhibition sur l'integrase du vih |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US8188271B2 (fr) |
| EP (1) | EP1950212B1 (fr) |
| JP (1) | JP5131689B2 (fr) |
| KR (1) | KR20080064182A (fr) |
| AU (1) | AU2006307101A1 (fr) |
| BR (1) | BRPI0617842A2 (fr) |
| CA (1) | CA2626956A1 (fr) |
| EA (1) | EA200801144A1 (fr) |
| ES (1) | ES2569357T3 (fr) |
| IL (1) | IL190879A0 (fr) |
| MA (1) | MA29879B1 (fr) |
| MX (1) | MX2008005137A (fr) |
| NO (1) | NO20081892L (fr) |
| TW (1) | TW200800988A (fr) |
| WO (1) | WO2007049675A1 (fr) |
Families Citing this family (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101363875B1 (ko) | 2005-04-28 | 2014-02-21 | 시오노기세야쿠 가부시키가이샤 | Hiv 통합효소 억제 활성을 가지는 다환식카르바모일피리돈 유도체 |
| MX2008005137A (es) | 2005-10-27 | 2008-09-29 | Shionogi & Co | Derivado de carbamoilpiridona policiclica que tiene actividad inhibidora en vih integrasa. |
| US7482345B2 (en) * | 2005-12-05 | 2009-01-27 | Meng-Hsin Chen | P38 kinase inhibiting agents |
| ATE541841T1 (de) | 2007-11-15 | 2012-02-15 | Boehringer Ingelheim Int | Inhibitoren der replikation des human immunodeficiency virus |
| ES2402322T3 (es) * | 2007-11-15 | 2013-04-30 | Gilead Sciences, Inc. | Inhibidores de la replicación del virus de la inmunodeficiencia humana |
| EA019259B1 (ru) | 2007-11-16 | 2014-02-28 | Джилид Сайенсиз, Инк. | Ингибиторы репликации вируса иммунодефицита человека |
| WO2010011814A1 (fr) | 2008-07-25 | 2010-01-28 | Smithkline Beecham Corporation | Composés chimiques |
| CN102245572B (zh) | 2008-12-11 | 2015-03-25 | 盐野义制药株式会社 | 氨甲酰基吡啶酮hiv整合酶抑制剂的方法和中间体 |
| KR101733625B1 (ko) | 2008-12-11 | 2017-05-10 | 시오노기세야쿠 가부시키가이샤 | 카르바모일피리돈 hiv 인테그라제 억제제 및 중간체의 합성 |
| TWI518084B (zh) | 2009-03-26 | 2016-01-21 | 鹽野義製藥股份有限公司 | 哌喃酮與吡啶酮衍生物之製造方法 |
| US8927710B2 (en) * | 2009-06-15 | 2015-01-06 | Shionogi & Co., Ltd. | Substituted polycyclic carbamoylpyridone derivative |
| ES2446720T3 (es) * | 2009-10-13 | 2014-03-10 | Elanco Animal Health Ireland Limited | Inhibidores de la integrasa macrocíclica |
| CA2789457A1 (fr) | 2010-02-26 | 2011-09-01 | Susumu Miyazaki | Derive de 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine et son utilisation comme inhibiteur d'integrase de vih |
| TWI582097B (zh) | 2010-03-23 | 2017-05-11 | Viiv醫療保健公司 | 製備胺甲醯吡啶酮衍生物及中間體之方法 |
| US9216995B2 (en) * | 2010-04-12 | 2015-12-22 | Shionogi & Co., Ltd. | Pyridone derivative having integrase inhibitory activity |
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| RU2014113230A (ru) * | 2011-10-12 | 2015-11-20 | Шионоги Энд Ко., Лтд. | Полициклическое производное пиридона, обладающее ингибирующей активностью в отношении интегразы |
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| WO2013102142A1 (fr) | 2011-12-28 | 2013-07-04 | Global Blood Therapeutics, Inc. | Composés benzaldéhyde substitués et procédés d'utilisation de ceux-ci dans l'augmentation de l'oxygénation des tissus |
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| TW201613936A (en) | 2014-06-20 | 2016-04-16 | Gilead Sciences Inc | Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide |
| NO2717902T3 (fr) | 2014-06-20 | 2018-06-23 | ||
| JPWO2016027879A1 (ja) | 2014-08-22 | 2017-06-01 | 塩野義製薬株式会社 | インテグラーゼ阻害活性を有する多環性ピリドン誘導体 |
| TWI695003B (zh) | 2014-12-23 | 2020-06-01 | 美商基利科學股份有限公司 | 多環胺甲醯基吡啶酮化合物及其醫藥用途 |
| MA41841A (fr) | 2015-03-30 | 2018-02-06 | Global Blood Therapeutics Inc | Composés aldéhyde pour le traitement de la fibrose pulmonaire, de l'hypoxie, et de maladies auto-immunes et des tissus conjonctifs |
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| US20240018145A1 (en) * | 2020-07-27 | 2024-01-18 | Merck Sharp & Dohme Llc | Polycyclic cap-dependent endonuclease inhibitors for treating or preventing influenza |
| ES3064867T3 (en) | 2020-09-30 | 2026-04-29 | Gilead Sciences Inc | Bridged tricyclic carbamoylpyridone compounds for a use in the treatment of hiv |
| US11613546B2 (en) | 2021-01-19 | 2023-03-28 | Gilead Sciences, Inc. | Substituted pyridotriazine compounds and uses thereof |
| TW202446773A (zh) | 2022-04-06 | 2024-12-01 | 美商基利科學股份有限公司 | 橋聯三環胺甲醯基吡啶酮化合物及其用途 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JPH0296506A (ja) | 1988-09-30 | 1990-04-09 | Daicel Chem Ind Ltd | 除草剤組成物 |
| JP2551472B2 (ja) | 1988-10-18 | 1996-11-06 | ダイセル化学工業株式会社 | 5−アルコキシ−γ−ピロン−3−カルボキサミド誘導体とその製造方法及び植物成長抑制剤 |
| JP2533796B2 (ja) | 1988-10-18 | 1996-09-11 | ダイセル化学工業株式会社 | 5−アルコキシピリジン−3−カルボキサミド誘導体とその製造方法及び植物成長抑制剤 |
| PL360944A1 (en) * | 2000-10-12 | 2004-09-20 | Merck & Co, Inc. | Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
| ES2572030T3 (es) | 2001-08-10 | 2017-07-19 | Shionogi & Co., Ltd. | Agente antiviral |
| ATE355064T1 (de) | 2001-10-26 | 2006-03-15 | Angeletti P Ist Richerche Bio | Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase |
| US7300364B2 (en) | 2004-02-06 | 2007-11-27 | Acushnet Company | Multi-layer golf ball having velocity gradient from faster center to slower cover |
| US7109186B2 (en) | 2002-07-09 | 2006-09-19 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| ATE404537T1 (de) | 2002-08-13 | 2008-08-15 | Shionogi & Co | Heterocyclische verbindungen mit hiv-integrase- hemmender wirkung |
| CA2498111A1 (fr) | 2002-09-11 | 2004-03-25 | Merck & Co., Inc. | Composes de dihydroxypyridopyrazine-1,6-diones utiles en tant qu'inhibiteurs de l'integrase du vih |
| 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 |
| JP2004244320A (ja) | 2003-02-10 | 2004-09-02 | Shionogi & Co Ltd | 含窒素複素環抗ウイルス剤 |
| TW200510425A (en) | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
| US20070161639A1 (en) * | 2004-03-09 | 2007-07-12 | Philip Jones | Hiv integrase inhibitors |
| WO2006066414A1 (fr) * | 2004-12-23 | 2006-06-29 | Virochem Pharma Inc. | Hydroxydihydropyridopy razine-1,8-diones et procedes d’inhibition de l’integrase du vih |
| ATE516026T1 (de) | 2005-02-21 | 2011-07-15 | Shionogi & Co | Bicyclisches carbamoylpyridonderivat mit hiv- integrase-hemmender wirkung |
| KR101363875B1 (ko) | 2005-04-28 | 2014-02-21 | 시오노기세야쿠 가부시키가이샤 | Hiv 통합효소 억제 활성을 가지는 다환식카르바모일피리돈 유도체 |
| JP2005312076A (ja) | 2005-05-26 | 2005-11-04 | Olympus Corp | 電子撮像装置 |
| MX2008005137A (es) | 2005-10-27 | 2008-09-29 | Shionogi & Co | Derivado de carbamoilpiridona policiclica que tiene actividad inhibidora en vih integrasa. |
-
2006
- 2006-10-26 MX MX2008005137A patent/MX2008005137A/es not_active Application Discontinuation
- 2006-10-26 WO PCT/JP2006/321335 patent/WO2007049675A1/fr not_active Ceased
- 2006-10-26 AU AU2006307101A patent/AU2006307101A1/en not_active Abandoned
- 2006-10-26 CA CA002626956A patent/CA2626956A1/fr not_active Abandoned
- 2006-10-26 TW TW095139466A patent/TW200800988A/zh unknown
- 2006-10-26 KR KR1020087012320A patent/KR20080064182A/ko not_active Withdrawn
- 2006-10-26 EP EP06822311.4A patent/EP1950212B1/fr active Active
- 2006-10-26 BR BRPI0617842-1A patent/BRPI0617842A2/pt not_active IP Right Cessation
- 2006-10-26 EA EA200801144A patent/EA200801144A1/xx unknown
- 2006-10-26 US US12/084,128 patent/US8188271B2/en not_active Expired - Fee Related
- 2006-10-26 ES ES06822311.4T patent/ES2569357T3/es active Active
- 2006-10-26 JP JP2007542639A patent/JP5131689B2/ja not_active Expired - Fee Related
-
2008
- 2008-04-15 IL IL190879A patent/IL190879A0/en unknown
- 2008-04-22 NO NO20081892A patent/NO20081892L/no not_active Application Discontinuation
- 2008-04-23 MA MA30862A patent/MA29879B1/fr unknown
-
2012
- 2012-03-23 US US13/428,242 patent/US20120208998A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP5131689B2 (ja) | 2013-01-30 |
| US20120208998A1 (en) | 2012-08-16 |
| BRPI0617842A2 (pt) | 2011-08-09 |
| EP1950212A4 (fr) | 2010-08-04 |
| EP1950212A1 (fr) | 2008-07-30 |
| NO20081892L (no) | 2008-06-23 |
| US8188271B2 (en) | 2012-05-29 |
| EA200801144A1 (ru) | 2008-10-30 |
| CA2626956A1 (fr) | 2007-05-03 |
| US20090143356A1 (en) | 2009-06-04 |
| ES2569357T3 (es) | 2016-05-10 |
| KR20080064182A (ko) | 2008-07-08 |
| TW200800988A (en) | 2008-01-01 |
| JPWO2007049675A1 (ja) | 2009-04-30 |
| MX2008005137A (es) | 2008-09-29 |
| IL190879A0 (en) | 2008-11-03 |
| EP1950212B1 (fr) | 2016-02-24 |
| AU2006307101A1 (en) | 2007-05-03 |
| WO2007049675A1 (fr) | 2007-05-03 |
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