PE20180044A1 - Compuestos novedosos - Google Patents
Compuestos novedososInfo
- Publication number
- PE20180044A1 PE20180044A1 PE2017002302A PE2017002302A PE20180044A1 PE 20180044 A1 PE20180044 A1 PE 20180044A1 PE 2017002302 A PE2017002302 A PE 2017002302A PE 2017002302 A PE2017002302 A PE 2017002302A PE 20180044 A1 PE20180044 A1 PE 20180044A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- group
- compounds
- rip2 kinase
- arylalkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
Abstract
Se refiere a un compuesto de Formula I, en la que X representa N o CH, R1 es H, -SO2 alquilo (C1-C4), o alquilo (C1-C4); R2 es SRa, -SORa, entre otros, en donde Ra es alquilo (C1-C6), halo alquilo (C1-C6) heterocicloalquilo, arilo o hereroarilo de 4-7 miembros, en donde dicho alquilo (C1-C6) esta sustituido opcionalmente por uno o dos grupos cada uno seleccionado independientemente del grupo que consiste en ciano, hidroxilo alcoxi, entre otros. Z es fenilo o arilalquil (C1-C4)-, en el que el grupo fenilo o el resto arilo del grupo arilalquil (C1-C4)- esta sustituido con R4, R5, R6, R7; R4 es H, halogeno, ciano, entre otros; Cada uno de R5, R6 y R7 esta seleccionado independientemente del grupo que consiste en H, hidroxilo, halogeno, entre otros. L es un grupo de enlace que comprende una longitud de 4-16 atomos en su longitud mas corta. Dichos compuestos modulan la actividad de la cinasa RIP2 incluyendo la degradacion de la misma que comprenden inhibidores de cinasa RIP2. Tambien se refiere a refiere a compuestos, composiciones, combinaciones y medicamentos que contienen dichos compuestos y a procedimientos para su preparacion. En donde pueden ser utiles para el tratamiento de enfermedades alergicas, autoinmunitarias; o estados inflamatorios, o cualquier estado mediado por la cinasa RIP2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1506872.9A GB201506872D0 (en) | 2015-04-22 | 2015-04-22 | Novel compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20180044A1 true PE20180044A1 (es) | 2018-01-15 |
Family
ID=53299021
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017002302A PE20180044A1 (es) | 2015-04-22 | 2016-04-20 | Compuestos novedosos |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US10435391B2 (es) |
| EP (1) | EP3286169B1 (es) |
| JP (1) | JP2018513867A (es) |
| KR (1) | KR20170139096A (es) |
| CN (1) | CN107709305B (es) |
| AU (1) | AU2016252404B2 (es) |
| BR (1) | BR112017022604A2 (es) |
| CA (1) | CA2983414A1 (es) |
| CL (1) | CL2017002650A1 (es) |
| CO (1) | CO2017011851A2 (es) |
| CR (1) | CR20170478A (es) |
| EA (1) | EA033343B1 (es) |
| ES (1) | ES2841548T3 (es) |
| GB (1) | GB201506872D0 (es) |
| HK (1) | HK1243410A1 (es) |
| IL (1) | IL255067A0 (es) |
| MX (1) | MX2017013556A (es) |
| PE (1) | PE20180044A1 (es) |
| PH (1) | PH12017501921A1 (es) |
| SG (1) | SG11201708311UA (es) |
| WO (1) | WO2016172134A2 (es) |
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| CA2861066C (en) | 2012-01-12 | 2024-01-02 | Yale University | Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase |
| US10441654B2 (en) | 2014-01-24 | 2019-10-15 | Children's Hospital Of Eastern Ontario Research Institute Inc. | SMC combination therapy for the treatment of cancer |
| US10071164B2 (en) * | 2014-08-11 | 2018-09-11 | Yale University | Estrogen-related receptor alpha based protac compounds and associated methods of use |
| US20170327469A1 (en) | 2015-01-20 | 2017-11-16 | Arvinas, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| KR20220029783A (ko) | 2015-01-20 | 2022-03-08 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법 |
| MX2017011919A (es) | 2015-03-18 | 2018-05-22 | Arvinas Inc | Compuestos y metodos para la degradacion mejorada de proteinas especificas. |
| GB201506872D0 (en) | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
| EP3302482A4 (en) | 2015-06-05 | 2018-12-19 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
| WO2017030814A1 (en) | 2015-08-19 | 2017-02-23 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| CA3020792A1 (en) * | 2016-04-20 | 2017-10-26 | Glaxosmithkline Intellectual Property Development Limited | Conjugates comprising ripk2 inhibitors |
| CA3087528C (en) | 2016-09-15 | 2024-01-30 | Arvinas, Inc. | Indole derivatives as estrogen receptor degraders |
| CN110506039A (zh) | 2016-10-11 | 2019-11-26 | 阿尔维纳斯股份有限公司 | 用于雄激素受体靶向降解的化合物和方法 |
| IL304982A (en) | 2016-11-01 | 2023-10-01 | Arvinas Operations Inc | PROTACS Targeted Tau-Protein and Related Methods of Use |
| EP3548483A4 (en) | 2016-12-01 | 2020-06-10 | Arvinas Operations, Inc. | TETRAHYDRONAPHTHALINE AND TETRAHYDROISOQUINOLINE DERIVATIVES AS AN ESTROGEN RECEPTOR-DEGRADING AGENT |
| KR102564201B1 (ko) | 2016-12-23 | 2023-08-07 | 아비나스 오퍼레이션스, 인코포레이티드 | 급속 진행성 섬유육종 폴리펩티드의 표적화 분해를 위한 화합물 및 방법 |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| EP3559006A4 (en) | 2016-12-23 | 2021-03-03 | Arvinas Operations, Inc. | COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF FETAL LIVER KINASE POLYPEPTIDES |
| AU2017382406A1 (en) | 2016-12-23 | 2019-04-18 | Arvinas Operations, Inc. | EGFR proteolysis targeting chimeric molecules and associated methods of use |
| US11191741B2 (en) | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| JP7266526B6 (ja) | 2017-01-26 | 2024-02-15 | アルビナス・オペレーションズ・インコーポレイテッド | エストロゲン受容体タンパク質分解性の調節因子およびその関連方法 |
| WO2019099926A1 (en) | 2017-11-17 | 2019-05-23 | Arvinas, Inc. | Compounds and methods for the targeted degradation of interleukin-1 receptor-associated kinase 4 polypeptides |
| CN107987083A (zh) * | 2017-11-24 | 2018-05-04 | 江苏亚盛医药开发有限公司 | 用于治疗和/或预防与肝炎病毒相关的疾病或病症的双二氮杂双环化合物 |
| JP2021512153A (ja) | 2018-01-26 | 2021-05-13 | イエール ユニバーシティ | タンパク質分解のイミド系モジュレーターおよび使用方法 |
| AU2019249231B2 (en) | 2018-04-04 | 2022-04-21 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
| JPWO2020027225A1 (ja) | 2018-07-31 | 2021-11-11 | ファイメクス株式会社 | 複素環化合物 |
| CN112912376A (zh) | 2018-08-20 | 2021-06-04 | 阿尔维纳斯运营股份有限公司 | 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物 |
| CN112638905A (zh) * | 2018-08-28 | 2021-04-09 | 南京明德新药研发有限公司 | 作为rip2激酶抑制剂的喹唑啉类衍生物 |
| CN113677668A (zh) | 2019-01-30 | 2021-11-19 | 蒙特利诺治疗公司 | 用于雄激素受体靶向泛素化的双官能化合物和方法 |
| US11547759B2 (en) | 2019-01-30 | 2023-01-10 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| CA3133314A1 (en) | 2019-03-21 | 2020-09-24 | Codiak Biosciences, Inc. | Extracellular vesicle conjugates and uses thereof |
| US20220387906A1 (en) | 2019-03-21 | 2022-12-08 | Codiak Biosciences, Inc. | Process for preparing extracellular vesicles |
| EP3999182A1 (en) | 2019-07-17 | 2022-05-25 | Arvinas Operations, Inc. | Tau-protein targeting compounds and associated methods of use |
| JP2021024787A (ja) | 2019-07-31 | 2021-02-22 | ファイメクス株式会社 | 複素環化合物 |
| JPWO2021020585A1 (es) | 2019-07-31 | 2021-02-04 | ||
| KR20220119094A (ko) | 2019-12-19 | 2022-08-26 | 아비나스 오퍼레이션스, 인코포레이티드 | 안드로겐 수용체의 표적화된 분해를 위한 화합물 및 방법 |
| WO2021237100A1 (en) | 2020-05-21 | 2021-11-25 | Codiak Biosciences, Inc. | Methods of targeting extracellular vesicles to lung |
| WO2022061348A1 (en) * | 2020-09-16 | 2022-03-24 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
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| US11981672B2 (en) | 2021-09-13 | 2024-05-14 | Montelino Therapeutics Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| WO2023180388A1 (en) | 2022-03-24 | 2023-09-28 | Glaxosmithkline Intellectual Property Development Limited | 2,4-dioxotetrahydropyrimidinyl derivatives as degrons in protacs |
| US11957759B1 (en) | 2022-09-07 | 2024-04-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use |
| CN115869308B (zh) * | 2022-12-30 | 2024-03-26 | 中山大学肿瘤防治中心（中山大学附属肿瘤医院、中山大学肿瘤研究所） | 一种小分子化合物在制备抗结直肠癌药物中的应用 |
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| BR0312408A (pt) | 2002-07-02 | 2005-04-19 | Novartis Ag | Inibidores de peptìdeo de ligação de proteìna smac a inibidor de apoptose de proteìnas (iap) |
| EP1773348A4 (en) | 2004-07-12 | 2009-05-20 | Idun Pharmaceuticals Inc | TETRA PEPTIDE ANALOGS |
| BRPI0810522B8 (pt) * | 2007-04-13 | 2021-05-25 | Univ Michigan Regents | compostos miméticos diazo bicíclicos de smac, composição farmacêutica e kit compreendendo ditos compostos e uso dos mesmos para o tratamento de câncer |
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| EP2491041B1 (en) | 2009-10-23 | 2017-08-09 | The Regents of the University of Michigan | Bivalent diazo bicyclic smac mimetics and the uses thereof |
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| CA2861066C (en) | 2012-01-12 | 2024-01-02 | Yale University | Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an e3 ubiquitin ligase |
| AU2013306087B2 (en) | 2012-08-23 | 2017-08-10 | The Regents Of The University Of Michigan | Bivalent inhibitors of IAP proteins and therapeutic methods using the same |
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| TW201425307A (zh) | 2012-09-13 | 2014-07-01 | Glaxosmithkline Llc | 作為激酶抑制劑之胺基－喹啉類 |
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| EP2903998B1 (en) | 2012-10-02 | 2017-03-15 | Bristol-Myers Squibb Company | Iap antagonists |
| PE20151083A1 (es) | 2012-12-11 | 2015-08-06 | Hoffmann La Roche | Compuestos dimericos |
| CN105143208B (zh) | 2013-02-21 | 2017-09-26 | 葛兰素史密斯克莱知识产权发展有限公司 | 作为激酶抑制剂的喹唑啉 |
| JP6778114B2 (ja) | 2014-04-14 | 2020-10-28 | アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． | イミド系タンパク質分解モジュレーター及び関連する使用方法 |
| US9346815B2 (en) | 2014-05-23 | 2016-05-24 | Genentech, Inc. | 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds, compositions and methods of use thereof |
| RU2017111200A (ru) | 2014-09-05 | 2018-10-05 | Мерк Патент Гмбх | Циклогексилэтилзамещенные диаза- и триаза-трициклические соединения в качестве антагонистов индоламин-2,3-диоксигеназы для лечения рака |
| GB201506871D0 (en) * | 2015-04-22 | 2015-06-03 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| TW201642860A (zh) | 2015-04-22 | 2016-12-16 | 塞爾基因定量細胞研究公司 | 布羅莫結構域抑制劑 |
| EP3286181B1 (en) | 2015-04-22 | 2021-01-27 | Rigel Pharmaceuticals, Inc. | Pyrazole compounds and method for making and using the compounds |
| GB201506872D0 (en) | 2015-04-22 | 2015-06-03 | Ge Oil & Gas Uk Ltd | Novel compounds |
| GB201516243D0 (en) * | 2015-09-14 | 2015-10-28 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| CA3020792A1 (en) * | 2016-04-20 | 2017-10-26 | Glaxosmithkline Intellectual Property Development Limited | Conjugates comprising ripk2 inhibitors |
-
2015
- 2015-04-22 GB GBGB1506872.9A patent/GB201506872D0/en not_active Ceased
-
2016
- 2016-04-20 EP EP16783708.7A patent/EP3286169B1/en active Active
- 2016-04-20 SG SG11201708311UA patent/SG11201708311UA/en unknown
- 2016-04-20 BR BR112017022604-9A patent/BR112017022604A2/pt not_active Application Discontinuation
- 2016-04-20 PE PE2017002302A patent/PE20180044A1/es unknown
- 2016-04-20 ES ES16783708T patent/ES2841548T3/es active Active
- 2016-04-20 AU AU2016252404A patent/AU2016252404B2/en not_active Ceased
- 2016-04-20 WO PCT/US2016/028332 patent/WO2016172134A2/en active Application Filing
- 2016-04-20 CR CR20170478A patent/CR20170478A/es unknown
- 2016-04-20 CN CN201680036813.3A patent/CN107709305B/zh not_active Expired - Fee Related
- 2016-04-20 EA EA201792047A patent/EA033343B1/ru not_active IP Right Cessation
- 2016-04-20 US US15/568,025 patent/US10435391B2/en not_active Expired - Fee Related
- 2016-04-20 JP JP2017555322A patent/JP2018513867A/ja not_active Ceased
- 2016-04-20 MX MX2017013556A patent/MX2017013556A/es active IP Right Grant
- 2016-04-20 CA CA2983414A patent/CA2983414A1/en not_active Abandoned
- 2016-04-20 KR KR1020177033407A patent/KR20170139096A/ko unknown
-
2017
- 2017-10-16 IL IL255067A patent/IL255067A0/en unknown
- 2017-10-18 CL CL2017002650A patent/CL2017002650A1/es unknown
- 2017-10-20 PH PH12017501921A patent/PH12017501921A1/en unknown
- 2017-11-21 CO CONC2017/0011851A patent/CO2017011851A2/es unknown
-
2018
- 2018-02-28 HK HK18102883.6A patent/HK1243410A1/zh unknown
-
2019
- 2019-08-22 US US16/547,734 patent/US20190382381A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| EP3286169B1 (en) | 2020-10-07 |
| US20190382381A1 (en) | 2019-12-19 |
| MX2017013556A (es) | 2018-08-01 |
| EP3286169A2 (en) | 2018-02-28 |
| IL255067A0 (en) | 2017-12-31 |
| ES2841548T3 (es) | 2021-07-08 |
| EA033343B1 (ru) | 2019-09-30 |
| PH12017501921A1 (en) | 2018-03-19 |
| BR112017022604A2 (pt) | 2018-07-17 |
| EP3286169A4 (en) | 2018-11-21 |
| KR20170139096A (ko) | 2017-12-18 |
| CN107709305A (zh) | 2018-02-16 |
| GB201506872D0 (en) | 2015-06-03 |
| WO2016172134A3 (en) | 2016-12-01 |
| CA2983414A1 (en) | 2016-10-27 |
| SG11201708311UA (en) | 2017-11-29 |
| HK1243410A1 (zh) | 2018-07-13 |
| JP2018513867A (ja) | 2018-05-31 |
| CR20170478A (es) | 2018-01-22 |
| US10435391B2 (en) | 2019-10-08 |
| CL2017002650A1 (es) | 2018-03-16 |
| US20180134688A1 (en) | 2018-05-17 |
| CO2017011851A2 (es) | 2018-02-09 |
| EA201792047A1 (ru) | 2018-04-30 |
| CN107709305B (zh) | 2020-09-29 |
| AU2016252404A1 (en) | 2017-12-07 |
| WO2016172134A2 (en) | 2016-10-27 |
| AU2016252404B2 (en) | 2018-07-26 |
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