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)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Tropical Medicine & Parasitology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Engineering & Computer Science (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 (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ601847A (en) * | 2010-02-26 | 2014-03-28 | Japan Tobacco Inc | 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv integrase inhibitor |
| RU2014113230A (ru) * | 2011-10-12 | 2015-11-20 | Шионоги Энд Ко., Лтд. | Полициклическое производное пиридона, обладающее ингибирующей активностью в отношении интегразы |
| EP2931730B1 (en) * | 2012-12-17 | 2019-08-07 | Merck Sharp & Dohme Corp. | 4-pyridinonetriazine derivatives as hiv integrase inhibitors |
| SI3067358T1 (sl) | 2012-12-21 | 2019-12-31 | Gilead Sciences, Inc. | Policiklične spojine karbamoilpiridona in njihova farmacevtska uporaba |
| AR094311A1 (es) * | 2012-12-27 | 2015-07-22 | Japan Tobacco Inc | Derivados de tetrahidroespiro-ciclopropil-pirido[1,2-a]pirazina inhibidores de la integrasa del hiv |
| 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 |
| NO2865735T3 (es) | 2013-07-12 | 2018-07-21 | ||
| AU2014286993B2 (en) | 2013-07-12 | 2018-10-25 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their use for the treatment of HIV infections |
| PE20160661A1 (es) | 2013-09-12 | 2016-08-05 | Alios Biopharma Inc | Compuesto de azapiridona y sus usos de los mismos |
| 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 |
| NO2717902T3 (es) | 2014-06-20 | 2018-06-23 | ||
| 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 |
| TWI744723B (zh) | 2014-06-20 | 2021-11-01 | 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 |
| WO2016027879A1 (ja) | 2014-08-22 | 2016-02-25 | 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 |
| 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 |
| 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 |
| CN107108467B (zh) * | 2014-12-24 | 2022-08-19 | 北京生命科学研究所 | 细胞坏死抑制剂 |
| CA2980362C (en) | 2015-04-02 | 2020-02-25 | Gilead Sciences, Inc. | Polycyclic-carbamoylpyridone compounds and their pharmaceutical use |
| WO2016187788A1 (en) * | 2015-05-25 | 2016-12-01 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds useful for treating hiv infection |
| US10624912B2 (en) | 2015-11-17 | 2020-04-21 | 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) |
| WO2019070059A1 (ja) | 2017-10-06 | 2019-04-11 | 塩野義製薬株式会社 | 置換された多環性ピリドン誘導体の立体選択的な製造方法 |
| SG11202011386QA (en) | 2018-05-31 | 2020-12-30 | Shionogi & Co | Polycyclic pyridone derivative |
| LT3805220T (lt) | 2018-05-31 | 2024-08-26 | Shionogi & Co., Ltd | Policikliniai karbamoilpiridono dariniai, skirti živ gydymui |
| WO2020197991A1 (en) | 2019-03-22 | 2020-10-01 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use |
| US20200398978A1 (en) | 2019-06-20 | 2020-12-24 | Bell Helicopter Textron Inc. | Low-drag rotor blade extension |
| JPWO2021107066A1 (es) | 2019-11-28 | 2021-06-03 | ||
| BR112022015771A2 (pt) | 2020-02-24 | 2022-10-11 | Gilead Sciences Inc | Compostos tetracíclicos para tratar a infecção por hiv |
| TW202222798A (zh) | 2020-09-30 | 2022-06-16 | 美商基利科學股份有限公司 | 橋接三環胺甲醯基吡啶酮化合物及其用途 |
| 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 |
| CA3202957A1 (en) | 2021-01-19 | 2022-07-28 | Hang CHU | Substituted pyridotriazine compounds and uses thereof |
| TWI843506B (zh) | 2022-04-06 | 2024-05-21 | 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 |
|---|---|---|---|---|
| JP2005538184A (ja) | 2002-09-11 | 2005-12-15 | 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剤として有用な８−ヒドロキシ−１−オキソ−テトラヒドロピロロピラジン化合物 |
| EP1549315A4 (en) | 2002-09-11 | 2007-05-23 | Merck & Co Inc | DIHYDROXYPYRIDOPYRAZINE-1,6-DION COMPOUNDS 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 |
| EP1677599A4 (en) | 2003-10-20 | 2008-10-22 | Merck & Co Inc | HYDROXYPYRIDOPYRROLOPYRAZINDION COMPOUNDS AS HIV INTEGRASE INHIBITORS |
| AU2005227258A1 (en) | 2004-03-09 | 2005-10-06 | Merck & Co., Inc. | HIV integrase inhibitors |
| CN1930161A (zh) * | 2004-03-09 | 2007-03-14 | P·安杰莱蒂分子生物学研究所 | Hiv整合酶抑制剂 |
| CN1964975B (zh) | 2004-05-07 | 2011-11-30 | 默沙东公司 | Hiv整合酶抑制剂 |
| WO2006066414A1 (en) | 2004-12-23 | 2006-06-29 | Virochem Pharma Inc. | Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase |
| US7858788B2 (en) | 2005-02-21 | 2010-12-28 | Shionogi & Co., Ltd. | Bicyclic carbamoylpyridone derivative having HIV integrase inhibitory activity |
| PL3372281T3 (pl) | 2005-04-28 | 2021-12-27 | Viiv Healthcare Company | Policykliczne pochodne karbamoilopirydonu o aktywności inhibitorowej wobec integrazy HIV |
| 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 |
| BRPI0617842A2 (pt) | 2005-10-27 | 2011-08-09 | Shionogi & Co | composto ou um sal farmaceuticamente aceitável ou um solvato do mesmo, e, composição farmacêutica |
| AU2006306355A1 (en) | 2005-10-27 | 2007-05-03 | Merck & Co., Inc. | HIV integrase inhibitors |
| AU2009266421B2 (en) | 2008-07-02 | 2013-07-11 | Avexa Limited | Compounds having antiviral properties |
| EP2291377B1 (en) | 2008-07-02 | 2015-02-18 | Avexa Limited | Imidazopyrimidinones and uses thereof |
| WO2010000030A1 (en) | 2008-07-02 | 2010-01-07 | Avexa Limited | Thiazopyrimidinones and uses thereof |
| NZ601847A (en) * | 2010-02-26 | 2014-03-28 | Japan Tobacco Inc | 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv integrase inhibitor |
| UY33245A (es) | 2010-02-26 | 2011-09-30 | Boehringer Ingelheim Int | Tienopirimidinas que contienen un grupo alquilo sustituido para composiciones farmacéuticas |
| BR112012021086A2 (pt) | 2010-02-26 | 2016-05-17 | Xenon Pharmaceuticals Inc | composições farmacêuticas de composto espiro-oxindole para administração tópica e seu uso como agentes terapêuticos |
| UY33241A (es) | 2010-02-26 | 2011-09-30 | Boehringer Ingelheim Int | ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?. |
| US8754079B2 (en) | 2010-02-26 | 2014-06-17 | Boehringer Ingelheim International Gmbh | Cycloalkyl containing thienopyrimidines for pharmaceutical compositions |
| 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 NZ NZ601847A patent/NZ601847A/en not_active IP Right Cessation
- 2011-02-25 CA CA2789457A patent/CA2789457A1/en not_active Abandoned
- 2011-02-25 MX MX2012009869A patent/MX2012009869A/es active IP Right Grant
- 2011-02-25 WO PCT/JP2011/054404 patent/WO2011105590A1/ja not_active Ceased
- 2011-02-25 PH PH1/2012/501689A patent/PH12012501689A1/en unknown
- 2011-02-25 US US13/034,866 patent/US10065950B2/en not_active Expired - Fee Related
- 2011-02-25 PE PE2012001366A patent/PE20130010A1/es not_active Application Discontinuation
- 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 SG SG2012062881A patent/SG183484A1/en unknown
- 2011-02-25 TW TW100106352A patent/TW201139437A/zh unknown
- 2011-02-25 JP JP2011040159A patent/JP5765965B2/ja not_active Expired - Fee Related
- 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 CN CN2011800206206A patent/CN102858771A/zh active Pending
- 2011-02-25 AR ARP110100588A patent/AR080314A1/es not_active Application Discontinuation
-
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 |
|---|---|
| CN102858771A (zh) | 2013-01-02 |
| EP2540720B1 (en) | 2015-04-15 |
| EP2540720A1 (en) | 2013-01-02 |
| NZ601847A (en) | 2014-03-28 |
| CO6571861A2 (es) | 2012-11-30 |
| JP2011195585A (ja) | 2011-10-06 |
| SG183484A1 (en) | 2012-09-27 |
| CA2789457A1 (en) | 2011-09-01 |
| RU2012140961A (ru) | 2014-04-10 |
| JP5765965B2 (ja) | 2015-08-19 |
| MX2012009869A (es) | 2012-09-12 |
| PE20130010A1 (es) | 2013-02-05 |
| PH12012501689A1 (en) | 2012-11-05 |
| CL2012002355A1 (es) | 2013-01-25 |
| US20180319798A1 (en) | 2018-11-08 |
| WO2011105590A1 (ja) | 2011-09-01 |
| EP2540720A4 (en) | 2013-07-31 |
| US20120108564A1 (en) | 2012-05-03 |
| KR20120130185A (ko) | 2012-11-29 |
| US10065950B2 (en) | 2018-09-04 |
| AU2011221037A1 (en) | 2012-09-06 |
| BR112012021595A2 (pt) | 2017-02-21 |
| TW201139437A (en) | 2011-11-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR080314A1 (es) | Derivado de 1,3,4,8-tetrahidro-2h-pirido (1,2-a) pirazina y su uso como inhibidor de la hiv integrasa | |
| CO6321244A2 (es) | Pirrolopiridinas como inhibidores de cinasa | |
| ES2630079T3 (es) | Moduladores de la ruta del complemento y usos de los mismos | |
| ES2600636T3 (es) | Spiro-[1,3]-oxazinas y spiro-[1,4]-oxazepinas como inhibidores de BACE1 y/o BACE2 | |
| ES2521596T3 (es) | Combinación del compuesto GlyT1 con antipsicóticos | |
| AR068538A1 (es) | Compuesto heterociclico de 5 miembros con actividad supresora de la secrecion de acido | |
| ES2684517T3 (es) | Compuestos de heterociclilo como inhibidores de MEK | |
| CO6321130A2 (es) | Piridinas carboxamidas como inhibidores de la 11 beta-hsd1 | |
| ES2669189T3 (es) | Compuestos de carbazol útiles como inhibidores del bromodominio | |
| ES2613538T3 (es) | Derivados de arilamida como bloqueadores de TTX-S | |
| AR106472A1 (es) | Inhibidores de acc y usos de los mismos | |
| PE20141041A1 (es) | Compuestos, metodos y formulaciones parasiticidas | |
| ES2722409T3 (es) | Moduladores de ROR gamma (RORy) | |
| AR086019A1 (es) | COMPUESTOS DE PIRROLO SULFONAMIDA PARA MODULACION DE LA ACTIVIDAD DEL RECEPTOR HUERFANO g RELACIONADO AL RECEPTOR NUCLEAR HUERFANO RAR (RORg, NR1F3) Y PARA EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS Y AUTOINMUNES CRONICAS | |
| ECSP12012212A (es) | Derivados de ariletinilo | |
| ES2531274T3 (es) | Indazoles sustituidos con oxazol como inhibidores de PI3-cinasas | |
| EA200970493A1 (ru) | Макроциклические ингибиторы вируса гепатита с | |
| AR088449A1 (es) | Benzilindazoles sustituidos | |
| AR075332A1 (es) | Dionas ciclicas como herbicidas | |
| ES2626801T3 (es) | Compuestos de triazolopiridina como inhibidores de pde10a | |
| PE20142081A1 (es) | Inhibidores de quinurenina-3-monooxigenasa, composiciones farmaceuticas y metodo de uso de los mismos | |
| CO6150181A2 (es) | Compuesto 6-(bencilo sustituido con heterociclo)-4-oxoquinolina y su uso como inhibidor de integrasa vih | |
| AR111682A1 (es) | Derivados de imidazopirimidina con sustituyentes fenilo y piridilo que contienen azufre | |
| CO6150150A2 (es) | Derivados de 7-alquinil-1,8-naftiridonas su prepacion y su aplicacion en terapeutica | |
| AR085920A1 (es) | Derivados benzimidazolicos utiles como agentes antitumorales y composiciones farmaceuticas que los contienen |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |