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PE20221628A1 - Compuestos inhibidores de rip1 y metodos para hacer y utilizar los mismos - Google Patents

Compuestos inhibidores de rip1 y metodos para hacer y utilizar los mismos

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Publication number
PE20221628A1
PE20221628A1 PE2022000369A PE2022000369A PE20221628A1 PE 20221628 A1 PE20221628 A1 PE 20221628A1 PE 2022000369 A PE2022000369 A PE 2022000369A PE 2022000369 A PE2022000369 A PE 2022000369A PE 20221628 A1 PE20221628 A1 PE 20221628A1
Authority
PE
Peru
Prior art keywords
oxo
making
methods
oxazepin
methyl
Prior art date
Application number
PE2022000369A
Other languages
English (en)
Inventor
Yan Chen
Jiaxin Yu
Simon Shaw
Ihab Darwish
Vanessa Taylor
Somasekhar Bhamidipati
Zhushou Luo
Rao Kolluri
Original Assignee
Rigel Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Rigel Pharmaceuticals Inc filed Critical Rigel Pharmaceuticals Inc
Publication of PE20221628A1 publication Critical patent/PE20221628A1/es

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Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 4-OXO-2,3,4,5-TETRAHIDROBENZO[B][1,4]OXAZEPINA DE FORMULA (I) DONDE R1, R2, R3, R4, L, Z, m, n Y EL ANILLO B SON TAL COMO SE DESCRIBEN EN EL PRESENTE DOCUMENTO. SON COMPUESTOS PREFERIDOS: (S)-N-(7-((1-HIDROXICICLOPENTIL)ETINIL)-5-METIL-4-OXO-2,3,4,5-TETRAHIDROBENZO[B][1,4]OXAZEPIN-3-IL)-4-FENOXIPICOLINAMIDA; (S)-N-(5-METIL-7-(3-METILBUT-3-EN-1-IN-1-IL)-4-OXO-2,3,4,5-TETRAHIDROBENZO[B][1,4]OXAZEPIN-3-IL)-4-FENOXIPICOLINAMIDA; (S)-4-(4-FLUOROFENOXI)-N-(7-(3-HIDROXI-3-METILBUT-1-IN-1-IL)-5-METIL-4-OXO-2,3,4,5-TETRAHIDROBENZO[B][1,4]OXAZEPIN-3-IL)PICOLINAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA PROTEINA QUINASA 1 QUE INTERACTUA CON EL RECEPTOR (RIP1) SIENDO UTILES EN EL TRATAMIENTO DE TRASTORNOS AUTOINMUNES Y PROLIFERATIVOS.
PE2022000369A 2019-09-06 2020-09-04 Compuestos inhibidores de rip1 y metodos para hacer y utilizar los mismos PE20221628A1 (es)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201962897223P 2019-09-06 2019-09-06
US201962932404P 2019-11-07 2019-11-07
US202063001016P 2020-03-27 2020-03-27
US202063004319P 2020-04-02 2020-04-02
US202063004301P 2020-04-02 2020-04-02
US202063004290P 2020-04-02 2020-04-02
PCT/US2020/049487 WO2021046407A1 (en) 2019-09-06 2020-09-04 Rip1 inhibitory compounds and methods for making and using the same

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Families Citing this family (27)

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Publication number Priority date Publication date Assignee Title
RU2716136C2 (ru) * 2015-07-02 2020-03-06 Ф. Хоффманн-Ля Рош Аг Бициклические лактамы и способы их применения
WO2018073193A1 (en) 2016-10-17 2018-04-26 F. Hoffmann-La Roche Ag Bicyclic pyridone lactams and methods of use thereof
BR112020022423A2 (pt) * 2018-05-03 2021-02-02 Rigel Pharmaceuticals, Inc. composto, composição farmacêutica, método, método para tratar uma doença em um indivíduo e método para fabricar o composto
KR102808215B1 (ko) 2018-05-03 2025-05-19 리겔 파마슈티칼스, 인크. Rip1 억제 화합물 및 이를 제조하고 사용하는 방법
PH12022550536A1 (en) * 2019-09-06 2023-07-31 Rigel Pharmaceuticals Inc Rip1 inhibitory compounds and methods for making and using the same.
JOP20220056A1 (ar) 2019-09-06 2023-01-30 Rigel Pharmaceuticals Inc مركبات rip1 تثبيطية وطرق عملها واستخدامها
LT4055021T (lt) * 2019-11-07 2026-01-12 Rigel Pharmaceuticals, Inc. Heterocikliniai junginiai, slopinantys rip1
EP4110765A4 (en) * 2020-02-28 2024-03-06 Board of Regents, The University of Texas System INHIBITORS OF RECEPTOR INTERACTING PROTEIN KINASE I FOR THE TREATMENT OF DISEASES
AR121717A1 (es) 2020-04-02 2022-06-29 Rigel Pharmaceuticals Inc Inhibidores de rip1k
AR122703A1 (es) 2020-07-01 2022-09-28 Rigel Pharmaceuticals Inc Inhibidores de rip1k
WO2022171111A1 (en) * 2021-02-10 2022-08-18 Zai Lab (Us) Llc Heteroaryl-fused bicyclic compound as rip1-kinase inhibitors and uses thereof
AR125587A1 (es) * 2021-03-11 2023-08-02 Rigel Pharmaceuticals Inc Inhibidores heterocíclicos de la quinasa de rip1
CN113045560B (zh) * 2021-03-30 2022-09-06 港科鹏禾生物(苏州)有限公司 一种酰胺类衍生物及其制备方法和应用
US20240228506A1 (en) * 2021-04-27 2024-07-11 Merck Sharp & Dohme Llc Ripk1 inhibitors and methods of use
WO2022231927A1 (en) * 2021-04-27 2022-11-03 Merck Sharp & Dohme Llc Phenyl azepines as ripk1 inhibitors and methods of use thereof
CN114989156B (zh) * 2021-05-19 2024-07-05 成都贝诺科成生物科技有限公司 一种受体相互作用蛋白抑制剂及其制备方法和用途
WO2023020486A1 (zh) * 2021-08-17 2023-02-23 广州市恒诺康医药科技有限公司 Rip1激酶抑制剂类化合物及其组合物和用途
CN115737650B (zh) * 2021-09-03 2024-06-28 复旦大学 一种嘧啶类衍生物或其药学上可接受的盐在制备治疗结核病药物中的应用
IL311505A (en) * 2021-09-17 2024-05-01 Bisichem Co Ltd Fused heterocyclic rings as ripk1 inhibitors
WO2023138317A1 (zh) * 2022-01-21 2023-07-27 中国科学院上海药物研究所 具有ripk1抑制活性的化合物、其制备方法及其用途
US20250197390A1 (en) * 2022-03-16 2025-06-19 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Fused heterocyclic compound, and preparation method therefor and medical use thereof
CN114736197B (zh) * 2022-06-13 2022-09-13 南京医工医药技术有限公司 咪唑啉酮衍生物及其用途
CN115353513A (zh) * 2022-07-29 2022-11-18 中国人民解放军海军军医大学 一种抑制程序性细胞坏死的硫代七元环衍生物及其应用
WO2025006391A1 (en) * 2023-06-26 2025-01-02 Athos Therapeutics, Inc. Small molecules for the treatment of autoimmune disorders
WO2025045253A1 (zh) * 2023-08-31 2025-03-06 杭州百诚医药科技股份有限公司 苯并氮杂䓬酮类衍生物及其用途
WO2025153090A1 (zh) * 2024-01-19 2025-07-24 无锡奕拓医药科技有限责任公司 一种多并环化合物、其药物组合物及其用途
CN120365288A (zh) * 2024-01-23 2025-07-25 南京天印健华医药科技有限公司 作为ripk1抑制剂的杂环化合物

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5087240A (en) 1983-08-18 1992-02-11 Drug Delivery Systems Inc. Transdermal drug patch with conductive fibers
US4921475A (en) 1983-08-18 1990-05-01 Drug Delivery Systems Inc. Transdermal drug patch with microtubes
US4738851A (en) 1985-09-27 1988-04-19 University Of Iowa Research Foundation, Inc. Controlled release ophthalmic gel formulation
US5163899A (en) 1987-03-20 1992-11-17 Drug Delivery Systems Inc. Transdermal drug delivery system
US5312325A (en) 1987-05-28 1994-05-17 Drug Delivery Systems Inc Pulsating transdermal drug delivery system
GB8804164D0 (en) 1988-02-23 1988-03-23 Tucker J M Bandage for administering physiologically active compound
US4882150A (en) 1988-06-03 1989-11-21 Kaufman Herbert E Drug delivery system
US5008110A (en) 1988-11-10 1991-04-16 The Procter & Gamble Company Storage-stable transdermal patch
US5088977A (en) 1988-12-21 1992-02-18 Drug Delivery Systems Inc. Electrical transdermal drug applicator with counteractor and method of drug delivery
US5521222A (en) 1989-09-28 1996-05-28 Alcon Laboratories, Inc. Topical ophthalmic pharmaceutical vehicles
ES2055280T3 (es) 1989-12-04 1994-08-16 Searle & Co Sistema monocapa para la administracion transdermica de farmacos.
US5112596A (en) 1990-04-23 1992-05-12 Alkermes, Inc. Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability
US5268164A (en) 1990-04-23 1993-12-07 Alkermes, Inc. Increasing blood-brain barrier permeability with permeabilizer peptides
US5077033A (en) 1990-08-07 1991-12-31 Mediventures Inc. Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide
EP0495421B1 (en) 1991-01-15 1996-08-21 Alcon Laboratories, Inc. Use of carrageenans in topical ophthalmic compositions
US5352456A (en) 1991-10-10 1994-10-04 Cygnus Therapeutic Systems Device for administering drug transdermally which provides an initial pulse of drug
EP0617665B1 (en) 1991-12-18 1999-03-31 Minnesota Mining And Manufacturing Company Multilayered barrier structures
EP0553769B1 (de) 1992-01-29 1996-01-03 FRANZ VÖLKL GmbH & CO. SKI UND TENNIS SPORTARTIKELFABRIK KG Ballspielschläger, insbesondere Tennisschläger
IL114193A (en) 1994-06-20 2000-02-29 Teva Pharma Ophthalmic pharmaceutical compositions based on sodium alginate
ES2094688B1 (es) 1994-08-08 1997-08-01 Cusi Lab Manoemulsion del tipo de aceite en agua, util como vehiculo oftalmico y procedimiento para su preparacion.
IT1283911B1 (it) 1996-02-05 1998-05-07 Farmigea Spa Soluzioni oftalmiche viscosizzate con polisaccaridi della gomma di tamarindo
US5800807A (en) 1997-01-29 1998-09-01 Bausch & Lomb Incorporated Ophthalmic compositions including glycerin and propylene glycol
US6261547B1 (en) 1998-04-07 2001-07-17 Alcon Manufacturing, Ltd. Gelling ophthalmic compositions containing xanthan gum
US6197934B1 (en) 1998-05-22 2001-03-06 Collagenesis, Inc. Compound delivery using rapidly dissolving collagen film
WO2009023272A1 (en) 2007-08-15 2009-02-19 President And Fellows Of Harvard College Heterocyclic inhibitors of necroptosis
TWI648274B (zh) * 2013-02-15 2019-01-21 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類 (二)
EP2968276A4 (en) 2013-03-15 2017-02-15 President and Fellows of Harvard College Hybrid necroptosis inhibitors
WO2016027253A1 (en) * 2014-08-21 2016-02-25 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors as medicaments
JP2018505199A (ja) 2015-02-13 2018-02-22 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited (S)−5−ベンジル−N−(5−メチル−4−オキソ−2,3,4,5テトラヒドロベンゾ[b][1,4]オキサゼピン−3−イル)−4H−1,2,4−トリアゾール−3−カルボキサミドの結晶形
RU2716136C2 (ru) 2015-07-02 2020-03-06 Ф. Хоффманн-Ля Рош Аг Бициклические лактамы и способы их применения
DK3362449T3 (da) 2015-10-13 2021-07-19 Inst Nat Sante Rech Med Sibirilin-derivater til anvendelse til at forebygge og/eller behandle lidelser associeret med cellulær nekroptose
AU2016340527B2 (en) 2015-10-23 2020-09-17 Takeda Pharmaceutical Company Limited Heterocyclic compound
WO2017109724A1 (en) 2015-12-21 2017-06-29 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
JP6974331B2 (ja) 2016-02-05 2021-12-01 デナリ セラピューティクス インコーポレイテッドDenali Therapeutics Inc. 化合物、組成物及び方法
WO2018073193A1 (en) 2016-10-17 2018-04-26 F. Hoffmann-La Roche Ag Bicyclic pyridone lactams and methods of use thereof
US11072607B2 (en) 2016-12-16 2021-07-27 Genentech, Inc. Inhibitors of RIP1 kinase and methods of use thereof
CA3052767A1 (en) 2017-02-27 2018-08-30 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
BR112020022423A2 (pt) 2018-05-03 2021-02-02 Rigel Pharmaceuticals, Inc. composto, composição farmacêutica, método, método para tratar uma doença em um indivíduo e método para fabricar o composto
KR102808215B1 (ko) * 2018-05-03 2025-05-19 리겔 파마슈티칼스, 인크. Rip1 억제 화합물 및 이를 제조하고 사용하는 방법
CA3104757A1 (en) 2018-06-26 2020-01-02 Shanghai Institute Of Organic Chemistry, Chinese Academy Of Sciences Cell necrosis inhibitor, preparation method therefor and use thereof
CN109134448B (zh) * 2018-10-16 2020-11-27 中南大学湘雅医院 杂环化合物及其盐、制备方法、用途和药物
CN111138448B (zh) 2018-11-02 2022-08-02 中国科学院上海药物研究所 抑制rip1激酶的杂环酰胺及其用途
JP7045526B2 (ja) 2018-11-02 2022-03-31 中国科学院上海薬物研究所 Rip1キナーゼを阻害する複素環状アミド及びその使用
JOP20220056A1 (ar) 2019-09-06 2023-01-30 Rigel Pharmaceuticals Inc مركبات rip1 تثبيطية وطرق عملها واستخدامها
PH12022550536A1 (en) 2019-09-06 2023-07-31 Rigel Pharmaceuticals Inc Rip1 inhibitory compounds and methods for making and using the same.
LT4055021T (lt) * 2019-11-07 2026-01-12 Rigel Pharmaceuticals, Inc. Heterocikliniai junginiai, slopinantys rip1
AR121717A1 (es) 2020-04-02 2022-06-29 Rigel Pharmaceuticals Inc Inhibidores de rip1k
AR122703A1 (es) 2020-07-01 2022-09-28 Rigel Pharmaceuticals Inc Inhibidores de rip1k

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