CL2021002882A1 - Inhibidores de fgfr y métodos de uso de los mismos - Google Patents

Inhibidores de fgfr y métodos de uso de los mismos

Info

Publication number
CL2021002882A1
CL2021002882A1 CL2021002882A CL2021002882A CL2021002882A1 CL 2021002882 A1 CL2021002882 A1 CL 2021002882A1 CL 2021002882 A CL2021002882 A CL 2021002882A CL 2021002882 A CL2021002882 A CL 2021002882A CL 2021002882 A1 CL2021002882 A1 CL 2021002882A1
Authority
CL
Chile
Prior art keywords
methods
fgfr inhibitors
compounds
compositions
fgfr
Prior art date
Application number
CL2021002882A
Other languages
English (en)
Inventor
Heike Schoenherr
Alexander M Taylor
Fabrizio Giordanetto
Demetri T Moustakas
Thomas H Mclean
Brandi M Hudson
Mary M Mader
Pelin Ayaz
Dina A Sharon
Ravi Kurukulasuriya
Alessandro Boezio
Bakary-Barry Touré
Original Assignee
Relay Therapeutics Inc
De Shaw Res Llc
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 Relay Therapeutics Inc, De Shaw Res Llc filed Critical Relay Therapeutics Inc
Publication of CL2021002882A1 publication Critical patent/CL2021002882A1/es

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    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07D487/22—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 four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • 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

La presente invención se refiere a nuevos compuestos y composiciones farmacéuticas de los mismos, y a métodos para inhibir la actividad de las enzimas FGFR con los compuestos y composiciones de la invención. La presente invención además se refiere, pero no se limita, a métodos para tratar trastornos asociados con la señalización de FGFR con los compuestos y composiciones de la invención.
CL2021002882A 2019-05-13 2021-11-03 Inhibidores de fgfr y métodos de uso de los mismos CL2021002882A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962846991P 2019-05-13 2019-05-13
US202062993957P 2020-03-24 2020-03-24
US202063011469P 2020-04-17 2020-04-17

Publications (1)

Publication Number Publication Date
CL2021002882A1 true CL2021002882A1 (es) 2022-10-07

Family

ID=73289291

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2021002882A CL2021002882A1 (es) 2019-05-13 2021-11-03 Inhibidores de fgfr y métodos de uso de los mismos

Country Status (15)

Country Link
US (2) US20230104574A1 (es)
EP (2) EP3968999B1 (es)
JP (1) JP2022533570A (es)
KR (1) KR20220007889A (es)
CN (1) CN114126620A (es)
AU (1) AU2020274083A1 (es)
BR (1) BR112021022457A2 (es)
CA (1) CA3137458A1 (es)
CL (1) CL2021002882A1 (es)
IL (1) IL287940A (es)
MX (1) MX2021013146A (es)
PE (1) PE20220573A1 (es)
SG (1) SG11202111327XA (es)
TW (1) TW202108141A (es)
WO (1) WO2020231990A1 (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220007889A (ko) 2019-05-13 2022-01-19 릴레이 테라퓨틱스, 인크. Fgfr 저해제 및 이의 사용 방법
TW202233625A (zh) * 2020-11-18 2022-09-01 美商傳達治療有限公司 Ｆｇｆｒ抑制劑及其製造及使用方法
CN115160319B (zh) * 2021-04-01 2023-12-26 西安新通药物研究股份有限公司 含1,3-苯并二氧戊环结构的化合物及其制备方法与用途
TW202304889A (zh) * 2021-04-03 2023-02-01 大陸商海南耀臻生物醫藥科技有限公司 作為fgfr抑制劑的雜環化合物及其應用
WO2023011581A1 (zh) * 2021-08-04 2023-02-09 江苏恒瑞医药股份有限公司 含氮杂环化合物、其制备方法及其在医药上的应用
WO2023046117A1 (en) * 2021-09-23 2023-03-30 3H Pharmaceuticals Co., Ltd. Fgfr inhibitors and methods of use thereof
WO2023104035A1 (zh) * 2021-12-06 2023-06-15 英矽智能科技(上海)有限公司 取代的单环或双环杂环化合物，其制法与医药上的用途
WO2023151560A1 (en) * 2022-02-08 2023-08-17 Etern Biopharma (Shanghai) Co., Ltd. Bicyclic heteroaryl compounds and uses thereof
WO2023202625A1 (zh) * 2022-04-20 2023-10-26 深圳福沃药业有限公司 Fgfr2抑制剂及使用方法
TW202400175A (zh) * 2022-05-10 2024-01-01 美商傳達治療有限公司 PI3Kα抑制劑及其使用方法
WO2024002157A1 (en) * 2022-06-29 2024-01-04 Insilico Medicine Ip Limited Inhibitors of fgfr2 and fgfr3 and uses thereof
TW202404957A (zh) * 2022-06-29 2024-02-01 大陸商上海翰森生物醫藥科技有限公司 雜環類衍生物抑制劑、其製備方法和應用
CN117402161A (zh) * 2022-07-06 2024-01-16 上海科恩泰生物医药科技有限公司 一种具有fgfr抑制作用的亚砜亚胺类化合物、包含其的药物组合物及其用途
WO2024083111A1 (zh) * 2022-10-18 2024-04-25 首药控股(北京)股份有限公司 一种新型杂环化合物
CN115594682B (zh) * 2022-10-26 2024-03-15 苏州浦合医药科技有限公司 Fgfr2抑制剂

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX9800215A (es) * 1995-07-06 1998-03-31 Novartis Ag Pirrolopirimidas y procesos para su preparacion.
ATE384062T1 (de) * 1996-08-23 2008-02-15 Novartis Pharma Gmbh Substituierte pyrrolopyrimidine und verfahren zu ihrer herstellung
ID24653A (id) 1997-03-19 2000-07-27 Basf Ag Zat-zat terapi
AUPQ441499A0 (en) * 1999-12-02 2000-01-06 Fujisawa Pharmaceutical Co., Ltd. Novel compound
GB0031080D0 (en) * 2000-12-20 2001-01-31 Novartis Ag Organic compounds
AUPR548601A0 (en) * 2001-06-06 2001-06-28 Fujisawa Pharmaceutical Co., Ltd. Pyrazolopyrazinecompound and pharmaceutical use thereof
US7323469B2 (en) * 2001-08-07 2008-01-29 Novartis Ag 7H-pyrrolo[2,3-d]pyrimidine derivatives
EP1661897B1 (en) * 2003-08-26 2013-12-04 Teijin Pharma Limited Pyrrolopyrimidinone derivative
UY28931A1 (es) * 2004-06-03 2005-12-30 Bayer Pharmaceuticals Corp Derivados de pirrolotriazina utiles para tratar trastornos hiper-proliferativos y enfermedades asociadas con angiogenesis
JP2008505084A (ja) * 2004-06-29 2008-02-21 アムゲン インコーポレイティッド フラノピリミジン
AU2005260032A1 (en) * 2004-06-29 2006-01-12 Amgen Inc. Pyrrolo[2,3-d]pyrimidines that modulate ACK1 and LCK activity
DE102005061170A1 (de) * 2005-12-21 2007-07-05 Bayer Healthcare Ag Neue, acyclisch substituierte Furopyrimidin-Derivate und ihre Verwendung
JP5656976B2 (ja) * 2009-04-29 2015-01-21 ローカス ファーマシューティカルズ インコーポレイテッド ピロロトリアジン化合物
CN102286048A (zh) * 2011-06-24 2011-12-21 吉林大学 4-氨基-6-(3-(3-溴苯基)苯基)-5-氰基-7-(β-L-呋喃木糖)吡咯并[2, 3-d]嘧啶、同类衍生物及用于制备抗肿瘤药物
WO2013078254A1 (en) 2011-11-22 2013-05-30 Array Biopharma Inc. Bicyclic heteroaryl derivatives as kinase inhibitors
US8993756B2 (en) 2011-12-06 2015-03-31 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
ES2516392T3 (es) * 2012-01-19 2014-10-30 Taiho Pharmaceutical Co., Ltd. Compuesto de alquinilbenceno 3,5-disustituido y sal del mismo
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
PT3269370T (pt) * 2016-02-23 2020-03-05 Taiho Pharmaceutical Co Ltd Novo composto de pirimidina condensada ou sal do mesmo
CN110022900A (zh) * 2016-09-08 2019-07-16 蓝图药品公司 成纤维细胞生长因子受体4抑制剂与细胞周期蛋白依赖性激酶抑制剂的组合
EP3515916B1 (en) 2016-09-22 2023-06-07 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
MX2019008695A (es) 2017-01-23 2019-09-11 Revolution Medicines Inc Compuestos biciclicos como inhibidores alostericos de shp2.
AU2018239542C1 (en) 2017-03-23 2021-02-11 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as SHP2 inhibitors
KR20220007889A (ko) 2019-05-13 2022-01-19 릴레이 테라퓨틱스, 인크. Fgfr 저해제 및 이의 사용 방법
TW202233625A (zh) 2020-11-18 2022-09-01 美商傳達治療有限公司 Ｆｇｆｒ抑制劑及其製造及使用方法

Also Published As

Publication number Publication date
MX2021013146A (es) 2022-01-24
IL287940A (en) 2022-01-01
BR112021022457A2 (pt) 2022-03-22
JP2022533570A (ja) 2022-07-25
US20230192709A1 (en) 2023-06-22
SG11202111327XA (en) 2021-11-29
AU2020274083A1 (en) 2021-11-18
PE20220573A1 (es) 2022-04-20
TW202108141A (zh) 2021-03-01
EP3968999A1 (en) 2022-03-23
WO2020231990A1 (en) 2020-11-19
EP3968999B1 (en) 2023-12-27
KR20220007889A (ko) 2022-01-19
CA3137458A1 (en) 2020-11-19
US20230104574A1 (en) 2023-04-06
EP3968999A4 (en) 2022-08-03
CN114126620A (zh) 2022-03-01
EP4306529A3 (en) 2024-04-10
EP4306529A2 (en) 2024-01-17
US11780845B2 (en) 2023-10-10

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