AR069334A1 - Inhibidores de la replicacion del virus de inmunodeficiencia humana - Google Patents
Inhibidores de la replicacion del virus de inmunodeficiencia humanaInfo
- Publication number
- AR069334A1 AR069334A1 ARP080104989A ARP080104989A AR069334A1 AR 069334 A1 AR069334 A1 AR 069334A1 AR P080104989 A ARP080104989 A AR P080104989A AR P080104989 A ARP080104989 A AR P080104989A AR 069334 A1 AR069334 A1 AR 069334A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- het
- cycloalkyl
- aryl
- independently selected
- Prior art date
Links
- 241000725303 Human immunodeficiency virus Species 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 230000010076 replication Effects 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 29
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000002947 alkylene group Chemical group 0.000 abstract 7
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 125000005842 heteroatom Chemical group 0.000 abstract 4
- 125000004043 oxo group Chemical group O=* 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000001118 alkylidene group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 2
- 229920006395 saturated elastomer Polymers 0.000 abstract 2
- -1 C3- cycloalkyl 7 Chemical group 0.000 abstract 1
- 208000031886 HIV Infections Diseases 0.000 abstract 1
- 208000037357 HIV infectious disease Diseases 0.000 abstract 1
- 125000000815 N-oxide group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000464 thioxo group Chemical group S=* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Abstract
Los compuestos de formula (1), composiciones farmacéuticas, usos para el tratamiento de infeccion por VIH. Reivindicacion 1: Un isomero, racemato, enantiomero o diastereoisomero de un compuesto caracterizado porque tiene la formula (1): en la que --------- representa un enlace sencillo o doble enlace; X es S o CR5; Y es S o CR7; en la que uno de X o Y es S; R2, R5, R6 y R7 se selecciona cada uno independientemente de: a) halogeno; b) R8, -C(=O)-R8, -C(=O)-O-R8, -O-R8, -S-R8, SO-R8, -SO2-R8, -alquilen C1-6-R8, -alquilen C1-6-C(=O)-R8, -alquilen C1-6-C(=O)-O-R8, -alquilen C1-6-SO-R8 o -alquilen C1-6-SO2-R8, -alquilen C1-6-O-R8 o -alquilen C1-6-S-R8; en los que R8 en cada caso se selecciona independientemente de H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, cicloalquilo C3-7, arilo y Het; y en el que cada uno del arilo y Het está opcionalmente sustituido con 1 a 3 sustituyentes, cada uno independientemente seleccionado de i) halogeno, oxo, tioxo, alquenilo C2-6, haloalquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6-, -OH, -O-alquilo C1-6, -O-haloalquilo C1-6), -SH, -S-alquilo C1-6, -SO-alquilo C1-6, -SO2-alquilo C1-6, -NH2, -NH-alquilo C1-6 y -N(alquilo C1-6)2; ii) alquilo C1-6 opcionalmente sustituido con -OH, -O-haloalquilo C1-6 o -O-alquilo C1-6; y iii) arilo o Het, en el que cada uno del arilo y Het está opcionalmente sustituido con halogeno o alquilo C1-6; y c) -N(R9)R10, -C(=O)N(R9)R10, -O-C(=O)N(R9)R10, -SO2-N(R9)R10, -alquilen C1-6-N(R9)R10, -alquilen C1-6-C(=O)-N(R9)R10, -alquilen C1-6)-O-C(=O)-N(R9)R10 o -alquilen C1-6-SO2-N(R9)R10 en los que R9 en cada caso se selecciona independientemente de H, alquilo C1-6 y cicloalquilo C3-7; y R10 en cada caso se selecciona independientemente de R8, -alquilen C1-6-R8, -SO2-R8, -C(=O)-R8, -C(=O)OR8 y -C(=O)N(R9)R8; en donde R8 y R9 son como se ha definido antes; R3 es alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquil C3-7-alquilo C1-6), aril-alquilo C1-6, Het-alquilo C1-6 o -W-R31, y el enlace c es un enlace sencillo; o R3 es alquilideno C1-6 y el enlace c es un doble enlace: en el que W es O o S y R31 es alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo, cicloalquil C3-7-alquilo C1-6, aril-alquilo C1-6 o Het-alquilo C1-6; en los que cada uno de alquilideno C1-6, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquil C3-7-alquilo C1-6, aril-alquilo C1-6, Het-alquilo C1-6 y -W-R31 está opcionalmente sustituido con 1 a 3 sustituyentes, cada uno independientemente seleccionado de alquilo C1-6, halogeno, ciano, oxo y -O-alquilo C1-6; R4 es arilo o Het, en el que cada uno de los arilo y Het está opcionalmente sustituido con 1 a 5 sustituyentes cada uno independientemente seleccionado de halogeno, alquilo C1-6, alquenilo C2-6, haloalquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6-, -OH, -O-alquilo C1-6, -SH, -S-alquilo C1-6, -NH2, -NH-alquilo C1-6 y -N(alquilo C1-6)2 en los que el alquilo C1-6 está opcionalmente sustituido con hidroxi, -O-alquilo C1-6, ciano u oxo; y en el que Het es un heterociclo de 4 a 7 miembros saturado, insaturado o aromático que tiene de 1 a 4 heteroátomos, cada uno independientemente seleccionado de O, N y S o un heteropoliciclo de 7 a 14 miembros, saturado, insaturado o aromático que tiene, siempre que sea posible, de 1 a 5 heteroátomos, cada uno independientemente seleccionado de O, N y S; en el que cada heteroátomo de N, independientemente y cuando sea posible, puede existir en un estado oxidado de modo que además está unido a un átomo de oxígeno para formar un grupo N-oxido y en el que cada heteroátomo de S, independientemente y cuando sea posible, existe en un estado oxidado de modo que está además unido a uno o dos átomos de oxígeno para formar los grupos SO o SO2 o una de sus sales o ésteres.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98834207P | 2007-11-15 | 2007-11-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR069334A1 true AR069334A1 (es) | 2010-01-13 |
Family
ID=40638277
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080104989A AR069334A1 (es) | 2007-11-15 | 2008-11-14 | Inhibidores de la replicacion del virus de inmunodeficiencia humana |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US7956068B2 (es) |
| EP (2) | EP2574610A1 (es) |
| JP (1) | JP5269085B2 (es) |
| KR (1) | KR20100108337A (es) |
| CN (1) | CN102124011A (es) |
| AR (1) | AR069334A1 (es) |
| AU (1) | AU2008323561B2 (es) |
| BR (1) | BRPI0819328A8 (es) |
| CA (1) | CA2705312C (es) |
| CL (1) | CL2008003405A1 (es) |
| ES (1) | ES2402322T3 (es) |
| IL (1) | IL205746A0 (es) |
| MX (1) | MX2010005292A (es) |
| NZ (1) | NZ585297A (es) |
| RU (1) | RU2503679C2 (es) |
| TW (1) | TW200920363A (es) |
| WO (1) | WO2009062288A1 (es) |
| ZA (1) | ZA201003305B (es) |
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| ES2634490T3 (es) | 2010-07-02 | 2017-09-28 | Gilead Sciences, Inc. | Derivados de ácido napht-2-ylacetico para tratar el sida |
| US8633200B2 (en) | 2010-09-08 | 2014-01-21 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| EP2640705A2 (en) | 2010-11-15 | 2013-09-25 | Katholieke Universiteit Leuven | Novel antiviral compounds |
| EP2640729B1 (en) * | 2010-11-15 | 2016-12-21 | VIIV Healthcare UK Limited | Inhibitors of hiv replication |
| AU2012240314A1 (en) * | 2011-04-04 | 2013-05-02 | Gilead Sciences, Inc. | Process for the preparation of an HIV integrase inhibitor |
| EP2508511A1 (en) | 2011-04-07 | 2012-10-10 | Laboratoire Biodim | Inhibitors of viral replication, their process of preparation and their therapeutical uses |
| EP2511273B8 (en) | 2011-04-15 | 2019-06-26 | Hivih | Inhibitors of viral replication, their process of preparation and their therapeutical uses |
| PE20141066A1 (es) | 2011-04-21 | 2014-09-05 | Gilead Sciences Inc | Compuestos de benzotiazol |
| WO2013012649A1 (en) * | 2011-07-15 | 2013-01-24 | Glaxosmithkline Llc | Azaindole compounds and methods for treating hiv |
| US8791108B2 (en) | 2011-08-18 | 2014-07-29 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| JP6099149B2 (ja) | 2011-10-25 | 2017-03-22 | 塩野義製薬株式会社 | Ｈｉｖ複製阻害剤 |
| PL2781519T3 (pl) * | 2011-11-15 | 2020-06-29 | St Pharm Co., Ltd. | Nowa przeciwwirusowa pochodna pirolopirydyny i sposób jej wytwarzania |
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| US8629276B2 (en) | 2012-02-15 | 2014-01-14 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| US9034882B2 (en) * | 2012-03-05 | 2015-05-19 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
| US9006235B2 (en) | 2012-03-06 | 2015-04-14 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
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| US8906929B2 (en) * | 2012-08-16 | 2014-12-09 | Bristol-Myers Squibb Company | Inhibitors of human immunodeficiency virus replication |
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| EP2716632A1 (en) | 2012-10-05 | 2014-04-09 | Laboratoire Biodim | Inhibitors of viral replication, their process of preparation and their therapeutical uses |
| EP2719685A1 (en) | 2012-10-11 | 2014-04-16 | Laboratoire Biodim | Inhibitors of viral replication, their process of preparation and their therapeutical uses |
| TW201441197A (zh) | 2013-01-31 | 2014-11-01 | Shionogi & Co | Ｈｉｖ複製抑制劑 |
| EP2970273B1 (en) | 2013-03-13 | 2017-03-01 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
| CN105189510B (zh) | 2013-03-13 | 2017-05-17 | 百时美施贵宝公司 | 人免疫缺陷病毒复制的抑制剂 |
| JP2016512511A (ja) | 2013-03-13 | 2016-04-28 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | ヒト免疫不全ウイルス複製の阻害剤 |
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| JP6268656B2 (ja) | 2013-03-14 | 2018-01-31 | ビーブ・ヘルスケア・ユーケイ・（ナンバー５）・リミテッドＶｉｉＶ Ｈｅａｌｔｈｃａｒｅ ＵＫ （Ｎｏ．５） Ｌｉｍｉｔｅｄ | ヒト免疫不全ウイルス複製の阻害剤 |
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| EP2821082A1 (en) | 2013-07-05 | 2015-01-07 | Laboratoire Biodim | Method of producing an inactivated lentivirus, especially HIV, vaccine, kit and method of use |
| EP2821104A1 (en) | 2013-07-05 | 2015-01-07 | Laboratoire Biodim | Inhibitors of viral replication, their process of preparation and their therapeutical uses |
| WO2015123230A1 (en) | 2014-02-12 | 2015-08-20 | Bristol-Myers Squibb Company | Benzothiazole macrocycles as inhibitors of human immunodeficiency virus replication |
| WO2015126743A1 (en) | 2014-02-18 | 2015-08-27 | Bristol-Myers Squibb Company | Pyrazolopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication |
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| JP6579549B2 (ja) | 2014-05-16 | 2019-09-25 | 塩野義製薬株式会社 | Ｈｉｖ複製阻害作用を有する３環性複素環誘導体 |
| AU2016271762B2 (en) | 2015-05-29 | 2020-01-23 | Shionogi & Co., Ltd. | Nitrogen-containing tricyclic derivatives having HIV replication inhibitory activity |
| KR20180025928A (ko) | 2015-07-06 | 2018-03-09 | 비브 헬스케어 유케이 (넘버5) 리미티드 | 인간 면역결핍 바이러스 복제의 억제제로서 피리딘-3-일 아세트산 유도체 |
| CN107835808A (zh) | 2015-07-08 | 2018-03-23 | Viiv保健英国第五有限公司 | 作为人类免疫缺陷性病毒复制的抑制剂的吡啶‑3‑基乙酸衍生物 |
| EP3319954A1 (en) | 2015-07-09 | 2018-05-16 | VIIV Healthcare UK (No.5) Limited | Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
| AU2016290205A1 (en) | 2015-07-09 | 2018-01-18 | VIIV Healthcare UK (No.5) Limited | Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
| CA2994512A1 (en) | 2015-08-07 | 2017-02-16 | VIIV Healthcare UK (No.5) Limited | Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
| KR20180035908A (ko) | 2015-08-10 | 2018-04-06 | 비브 헬스케어 유케이 (넘버5) 리미티드 | 인간 면역결핍 바이러스 복제의 억제제로서의 이미다조피리딘 매크로사이클 |
| AR105653A1 (es) | 2015-08-11 | 2017-10-25 | VIIV HEALTHCARE UK (Nº 5) LTD | Derivados del ácido 5-(n-bencil-tetrahidroisoquinolin-6-il)-piridin-3-il acético como inhibidores de la replicación del virus de la inmunodeficiencia humana |
| TW201718537A (zh) | 2015-08-12 | 2017-06-01 | Ｖｉｉｖ醫療保健英國（Ｎｏ．５）有限公司 | 做為人類免疫缺陷病毒複製抑制劑之吡啶－３－基乙酸衍生物 |
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| WO2019244066A2 (en) | 2018-06-19 | 2019-12-26 | VIIV Healthcare UK (No.5) Limited | Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication |
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| EP2335700A1 (en) * | 2001-07-25 | 2011-06-22 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis C virus polymerase inhibitors with a heterobicylic structure |
| FR2839646B1 (fr) * | 2002-05-17 | 2008-04-11 | Bioalliance Pharma | Utilisation de derives de quinoleine a effet anti-integrase et ses applications |
| EP1541558B1 (en) * | 2002-08-13 | 2008-08-13 | Shionogi & Co., Ltd. | Heterocyclic compounds having hiv integrase inhibitory activity |
| US20060094755A1 (en) * | 2004-10-28 | 2006-05-04 | Bioflexis, Llc | Novel quinoline-based metal chelators as antiviral agents |
| CA2600832C (en) * | 2005-03-31 | 2011-12-13 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Hiv integrase inhibitors |
| ES2667868T5 (es) * | 2005-04-28 | 2023-06-01 | Viiv Healthcare Co | Derivado de carbamoilpiridona policíclico que tiene actividad inhibidora de la integrasa del VIH |
| CA2622639C (en) * | 2005-10-04 | 2012-01-03 | Istituto Di Recerche Di Biologia Molecolare P. Angeletti S.P.A. | Hiv integrase inhibitors |
| ES2569357T3 (es) * | 2005-10-27 | 2016-05-10 | Shionogi & Co., Ltd. | Derivado de carbamoilpiridona policíclico que tiene actividad inhibidora sobre integrasa de HIV |
| US7939545B2 (en) * | 2006-05-16 | 2011-05-10 | Boehringer Ingelheim International Gmbh | Inhibitors of human immunodeficiency virus replication |
-
2008
- 2008-11-03 JP JP2010533394A patent/JP5269085B2/ja active Active
- 2008-11-03 ES ES08850892T patent/ES2402322T3/es active Active
- 2008-11-03 MX MX2010005292A patent/MX2010005292A/es active IP Right Grant
- 2008-11-03 KR KR1020107013084A patent/KR20100108337A/ko not_active Application Discontinuation
- 2008-11-03 US US12/743,143 patent/US7956068B2/en active Active
- 2008-11-03 CA CA2705312A patent/CA2705312C/en not_active Expired - Fee Related
- 2008-11-03 WO PCT/CA2008/001935 patent/WO2009062288A1/en active Application Filing
- 2008-11-03 NZ NZ585297A patent/NZ585297A/en not_active IP Right Cessation
- 2008-11-03 RU RU2010123989/04A patent/RU2503679C2/ru not_active IP Right Cessation
- 2008-11-03 EP EP12199561A patent/EP2574610A1/en not_active Withdrawn
- 2008-11-03 AU AU2008323561A patent/AU2008323561B2/en not_active Ceased
- 2008-11-03 CN CN2008801247470A patent/CN102124011A/zh active Pending
- 2008-11-03 EP EP08850892A patent/EP2220095B1/en active Active
- 2008-11-03 BR BRPI0819328A patent/BRPI0819328A8/pt not_active IP Right Cessation
- 2008-11-14 TW TW097144270A patent/TW200920363A/zh unknown
- 2008-11-14 AR ARP080104989A patent/AR069334A1/es not_active Application Discontinuation
- 2008-11-14 CL CL2008003405A patent/CL2008003405A1/es unknown
-
2010
- 2010-05-11 ZA ZA2010/03305A patent/ZA201003305B/en unknown
- 2010-05-13 IL IL205746A patent/IL205746A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20100305115A1 (en) | 2010-12-02 |
| AU2008323561A1 (en) | 2009-05-22 |
| EP2220095A1 (en) | 2010-08-25 |
| TW200920363A (en) | 2009-05-16 |
| US7956068B2 (en) | 2011-06-07 |
| ZA201003305B (en) | 2011-03-30 |
| CN102124011A (zh) | 2011-07-13 |
| AU2008323561B2 (en) | 2013-07-18 |
| MX2010005292A (es) | 2010-07-05 |
| JP2011503117A (ja) | 2011-01-27 |
| EP2220095A4 (en) | 2011-01-26 |
| EP2220095B1 (en) | 2013-01-02 |
| RU2010123989A (ru) | 2011-12-20 |
| KR20100108337A (ko) | 2010-10-06 |
| NZ585297A (en) | 2012-06-29 |
| ES2402322T3 (es) | 2013-04-30 |
| CA2705312C (en) | 2013-06-25 |
| BRPI0819328A2 (pt) | 2015-05-12 |
| BRPI0819328A8 (pt) | 2016-02-10 |
| CL2008003405A1 (es) | 2010-02-12 |
| IL205746A0 (en) | 2010-11-30 |
| RU2503679C2 (ru) | 2014-01-10 |
| WO2009062288A1 (en) | 2009-05-22 |
| JP5269085B2 (ja) | 2013-08-21 |
| EP2574610A1 (en) | 2013-04-03 |
| CA2705312A1 (en) | 2009-05-22 |
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