AR080314A1 - Derivado de 1,3,4,8-tetrahidro-2h-pirido (1,2-a) pirazina y su uso como inhibidor de la hiv integrasa - Google Patents
Derivado de 1,3,4,8-tetrahidro-2h-pirido (1,2-a) pirazina y su uso como inhibidor de la hiv integrasaInfo
- Publication number
- AR080314A1 AR080314A1 ARP110100588A ARP110100588A AR080314A1 AR 080314 A1 AR080314 A1 AR 080314A1 AR P110100588 A ARP110100588 A AR P110100588A AR P110100588 A ARP110100588 A AR P110100588A AR 080314 A1 AR080314 A1 AR 080314A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- atom
- nitrogen atom
- optionally substituted
- different
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 12
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 7
- 125000004432 carbon atom Chemical group C* 0.000 abstract 6
- 125000005842 heteroatom Chemical group 0.000 abstract 6
- 125000001424 substituent group Chemical group 0.000 abstract 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 229910052717 sulfur Inorganic materials 0.000 abstract 5
- 125000004434 sulfur atom Chemical group 0.000 abstract 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 4
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 4
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 abstract 2
- 125000004429 atom Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- 229910003827 NRaRb Inorganic materials 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000001924 cycloalkanes Chemical class 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- 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
- 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
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Reivindicacion 1: Un compuesto representado por la siguiente formula (1) o una de sus sales farmacéuticamente aceptables o uno de sus solvatos: caracterizado porque R1 es (1) un grupo alquilo C1-6 opcionalmente sustituido con 1 a 5 sustituyentes iguales o diferentes seleccionados de (i) un grupo cicloalquilo C3-8 y (ii) un grupo alcoxi C1-6, (2) un grupo cicloalquilo C3-8 o (3) un grupo heterocíclico monocíclico saturado que contiene, además de átomos de carbono, 1 a 3 heteroátomos seleccionados de un átomo de nitrogeno, un átomo de oxígeno y un átomo de azufre, R2, R3, R4 y R5 son iguales o diferentes y cada uno es (1) un átomo de hidrogeno, (2) un grupo carboxilo, (3) -CO-NRaRb en donde Ra y Rb son iguales o diferentes y cada uno es (i) un átomo de hidrogeno, (ii) un grupo alquilo C1-6 opcionalmente sustituido con 1 a 5 sustituyentes iguales o diferentes seleccionados del siguiente grupo B o (iii) un grupo cicloalquilo C3-8 o Ra y Rb forman opcionalmente, junto con el átomo de nitrogeno al que están unidos, un heteroanillo monocíclico saturado que opcionalmente contiene, además de átomos de carbono y un átono de nitrogeno, 1 a 5 heteroátomos seleccionados de un átomo de nitrogeno, un átomo de oxígeno y un átomo de azufre y opcionalmente sustituido con 1 a 5 sustituyentes iguales o diferentes seleccionados del siguiente grupo B, (4) un grupo alquilo C1-6 opcionalmente sustituido con 1 a 5 sustituyentes iguales o diferentes seleccionados del siguiente grupo A o (5) un grupo ciano, o R2 y R3 o R4 y R5 forman opcionalmente, junto con el átomo de carbono al que están unidos, i) cicloalcano C3-8 o ii) un heteroanillo monocíclico saturado que contiene, además de átomos de carbono, 1 a 6 heteroátomos seleccionados de un átomo de nitrogeno, un átomo de oxígeno y un átomo de azufre, en donde R2, R3, R4 y R5 no son átomos de hidrogeno al mismo tiempo, R6 es (1) un grupo alquilo C1-6 opcionalmente sustituido con los mismos o diferentes 1 a 5 átomos de halogeno, (2) un grupo alcoxi C1-6, (3) un átomo de halogeno o (4) un grupo cicloalquilo C3-8, Y es (1) CH o (2) un átomo de nitrogeno, m es un numero entero de 1 a 5 y cuando m es un numero entero de 2 a 5, entonces cada R6 puede ser igual o diferente, y n es un numero entero de 1 a 3, grupo A: (a) -CO-NRA1RA2 en donde RA1 y RA2 son iguales o diferentes y cada uno es (i) un átomo de hidrogeno, (ii) un grupo alquilo C1-6 opcionalmente sustituido con 1 a 5 sustituyentes iguales o diferentes seleccionados del siguiente grupo B o (iii) un grupo cicloalquilo C3-8 o RA1 y RA2 forman opcionalmente, junto con el átomo de nitrogeno al que están unidos, un heteroanillo monocíclico saturado que opcionalmente contiene, además de átomos de carbono y un átomo de nitrogeno, 1 a 3 heteroátomos seleccionados de un átomo de nitrogeno, un átomo de oxígeno y un átomo de azufre y opcionalmente sustituido con 1 a 5 sustituyentes iguales o diferentes seleccionados del siguiente grupo B, (b) un grupo hidroxilo, (c) un grupo alcoxi C1-6, (d) un grupo alcoxi C1-6-alcoxi C1-6, (e) un grupo ciano, (f) -NRA3RA4 en donde RA3 y RA4 son iguales o diferentes y cada uno es (i) un átomo de hidrogeno, (ii) un grupo alquilo C1-6, (iii) un grupo alquil C1-6-carbonilo o (iv) un grupo alquil C1-6-sulfonilo o RA3 y RA4 forman opcionalmente, junto con el átomo de nitrogeno al que están unidos, un heteroanillo que opcionalmente contiene, además de átomos de carbono y un átomo de nitrogeno, 1 a 5 heteroátomos seleccionados de un átomo de nitrogeno, un átomo de oxígeno y un átomo de azufre y opcionalmente sustituido con 1 o 2 grupos oxo, (g) un grupo carboxilo, (h) un grupo alquil C1-6-sulfonilo y (i) un grupo alquil C1-6-carbonilo; grupo B: (a) un grupo hidroxilo, (b) un grupo alcoxi C1-6, (c) un grupo alcoxi C1-6-alquilo C1-6, (d) un grupo cicloalquilo C3-8 y (e) un grupo oxo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2010043567 | 2010-02-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080314A1 true AR080314A1 (es) | 2012-03-28 |
Family
ID=44506987
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100588A AR080314A1 (es) | 2010-02-26 | 2011-02-25 | Derivado de 1,3,4,8-tetrahidro-2h-pirido (1,2-a) pirazina y su uso como inhibidor de la hiv integrasa |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US10065950B2 (es) |
| EP (1) | EP2540720B1 (es) |
| JP (1) | JP5765965B2 (es) |
| KR (1) | KR20120130185A (es) |
| CN (1) | CN102858771A (es) |
| AR (1) | AR080314A1 (es) |
| AU (1) | AU2011221037A1 (es) |
| BR (1) | BR112012021595A2 (es) |
| CA (1) | CA2789457A1 (es) |
| CL (1) | CL2012002355A1 (es) |
| CO (1) | CO6571861A2 (es) |
| MX (1) | MX2012009869A (es) |
| NZ (1) | NZ601847A (es) |
| PE (1) | PE20130010A1 (es) |
| PH (1) | PH12012501689A1 (es) |
| RU (1) | RU2012140961A (es) |
| SG (1) | SG183484A1 (es) |
| TW (1) | TW201139437A (es) |
| WO (1) | WO2011105590A1 (es) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2012009869A (es) * | 2010-02-26 | 2012-09-12 | Japan Tobacco Inc | Derivado de 1, 3,4, 8-tetrahidro-2h-pirido[1, 2-a]pirazina y sus uso como inhibidor de la integrasa del vih. |
| CA2851218A1 (en) | 2011-10-12 | 2013-04-18 | Shionogi & Co., Ltd. | Polycyclic pyridone derivative having integrase-inhibiting activity |
| WO2014099586A1 (en) * | 2012-12-17 | 2014-06-26 | Merck Sharp & Dohme Corp. | 4-pyridinonetriazine derivatives as hiv integrase inhibitors |
| CA2893843C (en) | 2012-12-21 | 2018-09-04 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| HK1214817A1 (en) | 2012-12-27 | 2016-08-05 | Japan Tobacco Inc. | Substituted spiropyrido[1,2-a]pyrazine derivative and medicinal use thereof as hiv integrase inhibitor |
| PT2997033T (pt) * | 2013-05-17 | 2018-01-25 | Merck Sharp & Dohme | Compostos heterocíclicos tricíclicos fundidos como inibidores de vih integrase |
| WO2014200880A1 (en) | 2013-06-13 | 2014-12-18 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
| DK3019503T3 (da) | 2013-07-12 | 2017-11-20 | Gilead Sciences Inc | Polycykliske-carbamoylpyridon-forbindelser og anvendelse deraf til behandling af hiv-infektioner |
| NO2865735T3 (es) | 2013-07-12 | 2018-07-21 | ||
| KR102323515B1 (ko) | 2013-09-12 | 2021-11-05 | 얀센 바이오파마, 인코퍼레이트. | 아자-피리돈 화합물 및 이의 용도 |
| CN103736081A (zh) * | 2013-12-18 | 2014-04-23 | 首都医科大学附属北京佑安医院 | Ontak在制备清除潜伏hiv病毒药物中的应用 |
| WO2015089847A1 (en) * | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Spirocyclic heterocycle compounds useful as hiv integrase inhibitors |
| 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 (es) | 2014-06-20 | 2018-06-23 | ||
| TWI677489B (zh) | 2014-06-20 | 2019-11-21 | 美商基利科學股份有限公司 | 多環型胺甲醯基吡啶酮化合物之合成 |
| EP3757105B1 (en) | 2014-08-22 | 2024-07-24 | Shionogi & Co., Ltd. | Polycyclic pyridone derivative having integrase inhibitory activity |
| EP3229804B1 (en) * | 2014-12-09 | 2020-05-06 | Merck Sharp & Dohme Corp. | Spirocyclic heterocycle compounds useful as hiv integrase inhibitors |
| WO2016090545A1 (en) * | 2014-12-09 | 2016-06-16 | Merck Sharp & Dohme Corp. | Spirocyclic heterocycle compounds useful as hiv integrate inhibitors |
| TWI738321B (zh) | 2014-12-23 | 2021-09-01 | 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 |
| JP6772141B2 (ja) * | 2014-12-24 | 2020-10-21 | ナショナル・インスティチュート・オブ・バイオロジカル・サイエンシズ，ベイジン | ネクローシス阻害薬 |
| TR201905009T4 (tr) | 2015-04-02 | 2019-05-21 | Gilead Sciences Inc | Polisiklik-karbamoilpiridon bileşikleri ve bunların farmasötik kullanımları. |
| WO2016187788A1 (en) | 2015-05-25 | 2016-12-01 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds useful for treating hiv infection |
| EP3377065B1 (en) | 2015-11-17 | 2022-05-18 | Merck Sharp & Dohme Corp. | Spirocyclic pyridotriazine derivatives useful as hiv integrase inhibitors |
| WO2017087257A1 (en) * | 2015-11-17 | 2017-05-26 | Merck Sharp & Dohme Corp. | Amido-substituted pyridotriazine derivatives useful 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) |
| AU2018344739B2 (en) | 2017-10-06 | 2023-04-13 | Shionogi & Co., Ltd. | Stereoselective process for preparing substituted polycyclic pyridone derivatives |
| US11453669B2 (en) | 2018-05-31 | 2022-09-27 | Shionogi & Co., Ltd. | Polycyclic pyridone derivative |
| CA3102063A1 (en) | 2018-05-31 | 2019-12-05 | Shionogi & Co., Ltd. | Polycyclic carbamoylpyridone derivative |
| IL286328B1 (en) | 2019-03-22 | 2026-04-01 | Gilead Sciences Inc | Tricyclic bridging compounds of carbamoylpyridone and their pharmaceutical use |
| US20200398978A1 (en) | 2019-06-20 | 2020-12-24 | Bell Helicopter Textron Inc. | Low-drag rotor blade extension |
| EP4066839A4 (en) | 2019-11-28 | 2023-12-27 | Shionogi & Co., Ltd | PROPHYLACTIC AND THERAPEUTIC MEDICINAL PRODUCT FOR HIV INFECTIOUS DISEASES, CHARACTERIZED BY CONTAINING THE COMBINATION OF INTEGRAS INHIBITORS AND ANTI-HIV AGENTS |
| US12577241B2 (en) | 2019-11-28 | 2026-03-17 | Shionogi & Co., Ltd. | Polycyclic pyridopyrazine derivative |
| CR20220418A (es) | 2020-02-24 | 2022-10-10 | Gilead Sciences Inc | Compuestos tetracíclicos para el tratamiento de infecciones por vih |
| CA3192145A1 (en) | 2020-09-30 | 2022-04-07 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and uses thereof |
| CN112574155A (zh) * | 2020-11-25 | 2021-03-30 | 南京杰运医药科技有限公司 | 一种3-(苄氧基)-4-氧代-4h-吡喃-2-羧酸的合成方法 |
| JP7591155B2 (ja) | 2021-01-19 | 2024-11-27 | ギリアード サイエンシーズ， インコーポレイテッド | 置換ピリドトリアジン化合物及びその使用 |
| TWI856796B (zh) | 2022-04-06 | 2024-09-21 | 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 |
| CN116969940B (zh) * | 2023-08-03 | 2025-08-12 | 浙江大学 | 3-羟基吡啶酮-5-酰胺类化合物及医药用途 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7517532B2 (en) | 2002-09-11 | 2009-04-14 | Merck & Co., Inc. | Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors |
| US7399763B2 (en) | 2002-09-11 | 2008-07-15 | Merck & Co., Inc. | 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as HIV integrase inhibitors |
| TW200510425A (en) | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
| JP2007509149A (ja) | 2003-10-20 | 2007-04-12 | メルク エンド カムパニー インコーポレーテッド | Ｈｉｖインテグラーゼ阻害薬として有用なヒドロキシピリドピロロピラジンジオン化合物 |
| CA2557926A1 (en) | 2004-03-09 | 2005-09-22 | Monica Donghi | Hiv integrase inhibitors |
| JP2007528394A (ja) | 2004-03-09 | 2007-10-11 | メルク エンド カムパニー インコーポレーテッド | Ｈｉｖインテグラーゼ阻害薬 |
| EP1756114B1 (en) | 2004-05-07 | 2014-11-19 | Merck Sharp & Dohme Corp. | Hiv integrase inhibitors |
| WO2006066414A1 (en) | 2004-12-23 | 2006-06-29 | Virochem Pharma Inc. | Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase |
| ATE516026T1 (de) | 2005-02-21 | 2011-07-15 | Shionogi & Co | Bicyclisches carbamoylpyridonderivat mit hiv- integrase-hemmender wirkung |
| PT1874117E (pt) | 2005-04-28 | 2013-10-17 | Shionogi & Co | Derivado policíclico de carbamoílpiridona possuindo actividade inibidora de hiv-integrasse |
| AU2006306355A1 (en) | 2005-10-27 | 2007-05-03 | Merck & Co., Inc. | HIV integrase inhibitors |
| CN101346376A (zh) * | 2005-10-27 | 2009-01-14 | 盐野义制药株式会社 | 具有hiv整合酶抑制活性的多环性氨基甲酰基吡啶酮衍生物 |
| AU2006307101A1 (en) | 2005-10-27 | 2007-05-03 | Shionogi & Co., Ltd. | Polycyclic carbamoylpyridone derivative having inhibitory activity on HIV integrase |
| US8426405B2 (en) | 2008-07-02 | 2013-04-23 | Avexa Limited | Thiazopyrimidinones and uses thereof |
| EP2291377B1 (en) | 2008-07-02 | 2015-02-18 | Avexa Limited | Imidazopyrimidinones and uses thereof |
| BRPI0913934A2 (pt) | 2008-07-02 | 2015-10-20 | Avexa Ltd | compostos tendo propriedades antivirais |
| MX2012009869A (es) * | 2010-02-26 | 2012-09-12 | Japan Tobacco Inc | Derivado de 1, 3,4, 8-tetrahidro-2h-pirido[1, 2-a]pirazina y sus uso como inhibidor de la integrasa del vih. |
| AR080328A1 (es) | 2010-02-26 | 2012-03-28 | Boehringer Ingelheim Int | Tienopirimidinas que contienen un grupo alquilo sustituido inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otros |
| UY33241A (es) | 2010-02-26 | 2011-09-30 | Boehringer Ingelheim Int | ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?. |
| EA201201191A1 (ru) | 2010-02-26 | 2013-04-30 | Бёрингер Ингельхайм Интернациональ Гмбх | 4-[циклоалкилокси(гетеро)ариламино]тиено[2,3-d]пиримидины, обладающие ингибирующей активностью по отношению к mnkl/mnk2, предназначенные для фармацевтических композиций |
| NZ601667A (en) | 2010-02-26 | 2014-10-31 | Xenon Pharmaceuticals Inc | Pharmaceutical compositions of spiro-oxindole compound for topical administration and their use as therapeutic agents |
| JP5766690B2 (ja) | 2010-04-12 | 2015-08-19 | 塩野義製薬株式会社 | インテグラーゼ阻害活性を有するピリドン誘導体 |
-
2011
- 2011-02-25 MX MX2012009869A patent/MX2012009869A/es active IP Right Grant
- 2011-02-25 RU RU2012140961/04A patent/RU2012140961A/ru not_active Application Discontinuation
- 2011-02-25 BR BR112012021595A patent/BR112012021595A2/pt not_active IP Right Cessation
- 2011-02-25 AU AU2011221037A patent/AU2011221037A1/en not_active Abandoned
- 2011-02-25 CN CN2011800206206A patent/CN102858771A/zh active Pending
- 2011-02-25 PE PE2012001366A patent/PE20130010A1/es not_active Application Discontinuation
- 2011-02-25 US US13/034,866 patent/US10065950B2/en not_active Expired - Fee Related
- 2011-02-25 TW TW100106352A patent/TW201139437A/zh unknown
- 2011-02-25 KR KR1020127022133A patent/KR20120130185A/ko not_active Withdrawn
- 2011-02-25 EP EP11747546.7A patent/EP2540720B1/en active Active
- 2011-02-25 CA CA2789457A patent/CA2789457A1/en not_active Abandoned
- 2011-02-25 WO PCT/JP2011/054404 patent/WO2011105590A1/ja not_active Ceased
- 2011-02-25 SG SG2012062881A patent/SG183484A1/en unknown
- 2011-02-25 JP JP2011040159A patent/JP5765965B2/ja not_active Expired - Fee Related
- 2011-02-25 AR ARP110100588A patent/AR080314A1/es not_active Application Discontinuation
- 2011-02-25 PH PH1/2012/501689A patent/PH12012501689A1/en unknown
- 2011-02-25 NZ NZ601847A patent/NZ601847A/en not_active IP Right Cessation
-
2012
- 2012-08-24 CL CL2012002355A patent/CL2012002355A1/es unknown
- 2012-09-20 CO CO12163009A patent/CO6571861A2/es active IP Right Grant
-
2018
- 2018-07-25 US US16/045,594 patent/US20180319798A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CL2012002355A1 (es) | 2013-01-25 |
| PE20130010A1 (es) | 2013-02-05 |
| SG183484A1 (en) | 2012-09-27 |
| EP2540720A1 (en) | 2013-01-02 |
| EP2540720A4 (en) | 2013-07-31 |
| EP2540720B1 (en) | 2015-04-15 |
| PH12012501689A1 (en) | 2012-11-05 |
| CO6571861A2 (es) | 2012-11-30 |
| JP5765965B2 (ja) | 2015-08-19 |
| US20180319798A1 (en) | 2018-11-08 |
| TW201139437A (en) | 2011-11-16 |
| NZ601847A (en) | 2014-03-28 |
| CA2789457A1 (en) | 2011-09-01 |
| US20120108564A1 (en) | 2012-05-03 |
| RU2012140961A (ru) | 2014-04-10 |
| BR112012021595A2 (pt) | 2017-02-21 |
| JP2011195585A (ja) | 2011-10-06 |
| KR20120130185A (ko) | 2012-11-29 |
| MX2012009869A (es) | 2012-09-12 |
| US10065950B2 (en) | 2018-09-04 |
| AU2011221037A1 (en) | 2012-09-06 |
| WO2011105590A1 (ja) | 2011-09-01 |
| CN102858771A (zh) | 2013-01-02 |
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