MX368491B - Derivados de pirimidina como inhibidores de cinasa. - Google Patents

Derivados de pirimidina como inhibidores de cinasa.

Info

Publication number
MX368491B
MX368491B MX2016000261A MX2016000261A MX368491B MX 368491 B MX368491 B MX 368491B MX 2016000261 A MX2016000261 A MX 2016000261A MX 2016000261 A MX2016000261 A MX 2016000261A MX 368491 B MX368491 B MX 368491B
Authority
MX
Mexico
Prior art keywords
kinase inhibitors
pyrimidine derivatives
compositions
methods
disease
Prior art date
Application number
MX2016000261A
Other languages
English (en)
Other versions
MX2016000261A (es
Inventor
Xu Xiao
Wang Xiaobo
Mao Long
Zhao Li
Xi Biao
Original Assignee
Acea Biosciences 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 Acea Biosciences Inc filed Critical Acea Biosciences Inc
Publication of MX2016000261A publication Critical patent/MX2016000261A/es
Publication of MX368491B publication Critical patent/MX368491B/es

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    • 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/495—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
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    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/553—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
    • 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

Abstract

La invención actual se refiere a compuestos farmacéuticos, composiciones y métodos, especialmente aquellos que se relacionan a composiciones y métodos para el tratamiento y/o prevención de un trastorno de proliferación, un cáncer, un tumor, una enfermedad inflamatoria, una enfermedad autoinmunitaria, psoriasis, ojo seco o una enfermedad inmunológicamente relacionada, y en algunas modalidades, enfermedades o trastornos relacionados con la desregulación de cinasa, tales como, pero no limitados a, EGER (incluyendo HER), Alk, PDGFR, BLK, BMX/ETK, FTL3 (D835Y), ITK, TEC, TXK, BTK, o JAK, y las trayectorias respectivas.
MX2016000261A 2013-07-11 2014-07-11 Derivados de pirimidina como inhibidores de cinasa. MX368491B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361845342P 2013-07-11 2013-07-11
US201461923179P 2014-01-02 2014-01-02
PCT/US2014/046442 WO2015006754A2 (en) 2013-07-11 2014-07-11 Heterocyclic compounds and uses thereof

Publications (2)

Publication Number Publication Date
MX2016000261A MX2016000261A (es) 2016-12-09
MX368491B true MX368491B (es) 2019-10-04

Family

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Family Applications (1)

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MX2016000261A MX368491B (es) 2013-07-11 2014-07-11 Derivados de pirimidina como inhibidores de cinasa.

Country Status (17)

Country Link
US (1) US10562918B2 (es)
EP (1) EP3019496B1 (es)
JP (1) JP6564771B2 (es)
KR (1) KR102173433B1 (es)
CN (3) CN117486865A (es)
AU (1) AU2014287016B2 (es)
BR (1) BR112016000195A8 (es)
CA (1) CA2917364C (es)
DK (1) DK3019496T3 (es)
ES (1) ES2761572T3 (es)
HK (1) HK1223351A1 (es)
IL (1) IL243420A0 (es)
MX (1) MX368491B (es)
NZ (1) NZ715687A (es)
RU (1) RU2677653C2 (es)
SG (1) SG11201600062RA (es)
WO (1) WO2015006754A2 (es)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
EP2802568A1 (en) 2012-01-13 2014-11-19 Acea Biosciences, Inc. Heterocyclic compounds and uses as anticancer agents.
IL289834B1 (en) 2012-06-13 2024-03-01 Incyte Holdings Corp Conversion of tricyclic compounds as FGFR inhibitors
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
SG10201708520YA (en) 2013-04-19 2017-12-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
SG11201600062RA (en) 2013-07-11 2016-02-26 Acea Biosciences Inc Pyrimidine derivatives as kinase inhibitors
EP3508204A1 (en) 2013-08-23 2019-07-10 Neupharma, Inc. Certain chemical entities, compositions, and methods
CN106661000B (zh) * 2014-10-11 2019-04-09 上海翰森生物医药科技有限公司 Egfr抑制剂及其制备和应用
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CN105884695B (zh) * 2015-02-13 2019-02-26 山东轩竹医药科技有限公司 杂环衍生物类酪氨酸激酶抑制剂
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MX2017010673A (es) 2015-02-20 2018-03-21 Incyte Corp Heterociclos biciclicos como inhibidores de receptores del factor de crecimiento fibroblastico (fgfr).
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
CN106146515B (zh) * 2015-04-17 2020-09-04 常州隆赛医药科技有限公司 新型激酶抑制剂的制备及应用
KR101778004B1 (ko) * 2015-06-22 2017-09-15 (주) 에빅스젠 이마티닙을 유효성분으로 포함하는 안구 건조 질환 예방 및 치료용 약학 조성물
US10045985B2 (en) * 2015-07-09 2018-08-14 Merck Patent Gmbh Heteroaryl compounds as BTK inhibitors and uses thereof
CN107949388B (zh) 2015-10-09 2021-10-26 艾森医药公司 吡咯并嘧啶激酶抑制剂的药用盐、物理形态和组合物及其制备方法
CN106608868A (zh) * 2015-10-21 2017-05-03 复旦大学 5-(硫醚基)嘧啶类化合物及其药用组合物和应用
KR20170050453A (ko) * 2015-10-30 2017-05-11 한미약품 주식회사 싸이에노피리미딘 화합물의 신규 제조방법 및 이에 사용되는 중간체
WO2017097113A1 (zh) * 2015-12-10 2017-06-15 深圳市塔吉瑞生物医药有限公司 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物
WO2018004306A1 (en) 2016-06-30 2018-01-04 Daewoong Pharmaceutical Co., Ltd. Pyrazolopyrimidine derivatives as kinase inhibitor
CN106749042B (zh) * 2016-11-16 2019-01-22 大连医科大学 磺酰胺基嘧啶类化合物，组合物及用途
KR20180075228A (ko) * 2016-12-26 2018-07-04 한미약품 주식회사 싸이에노피리미딘 화합물의 신규 제조방법 및 중간체
CA3048376A1 (en) 2016-12-27 2018-07-05 Riken Bmp-signal-inhibiting compound
WO2018139883A1 (ko) * 2017-01-26 2018-08-02 부광약품 주식회사 다중 표적 키나아제 저해제로서 융합피리미딘 유도체
WO2018145525A1 (zh) * 2017-02-08 2018-08-16 中国医药研究开发中心有限公司 吡咯并芳杂环类化合物及其制备方法和医药用途
BR112019020840A2 (pt) 2017-04-07 2020-04-28 Acea Therapeutics Inc sais farmacêuticos, formas físicas e composições de inibidores da pirrolopirimidina quinase e métodos de produção dos mesmos
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
CR20200590A (es) 2018-05-04 2021-04-26 Incyte Corp Formas sólidas de un inhibidor de fgfr y procesos para prepararlas
US11174257B2 (en) 2018-05-04 2021-11-16 Incyte Corporation Salts of an FGFR inhibitor
WO2020029156A1 (en) * 2018-08-09 2020-02-13 ACEA Therapeutics, Inc. Process for manufacture of (s)-n-(3-((2-((4-((1-acetylpyrrolidin-3-yl)(methyl)amino)phenyl)amino)-5-methoxypyrimidin-4-yl)oxy) phenyl)acrylamide, and formulations thereof
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP2022552324A (ja) 2019-10-14 2022-12-15 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての二環式複素環
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
TWI768550B (zh) * 2019-11-22 2022-06-21 大陸商南京明德新藥研發有限公司 作為dna-pk抑制劑的嘧啶并吡咯類螺環化合物及其衍生物
CN111018842B (zh) * 2019-12-04 2021-02-12 宜春市人民医院 一种唑代嘧啶衍生物、其药物组合物和在抗肿瘤中的应用
US11897891B2 (en) 2019-12-04 2024-02-13 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
CN111848631B (zh) * 2020-08-28 2022-04-19 四川大学华西医院 一种靶向EGFR突变的吡咯并[2,3-d]嘧啶衍生物及其制备方法和用途
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
CN114184671B (zh) * 2021-12-09 2024-02-06 中国石油大学(北京) 用于确定表面活性剂在岩石表面的吸附层数的方法
WO2023116527A1 (zh) * 2021-12-21 2023-06-29 微境生物医药科技(上海)有限公司 作为fak抑制剂的化合物及其用途

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3974277A (en) 1974-09-06 1976-08-10 Diamond Shamrock Corporation 2-[2-(5-Nitro-2-furyl)vinyl]-4-(anilino)quinazolines as growth promotants and feed efficiency enhancing agents
EP1230225A2 (en) 1999-11-01 2002-08-14 Eli Lilly And Company Pharmaceutically active 4-substituted pyrimidine derivatives
ATE475652T1 (de) 2001-02-21 2010-08-15 Mitsubishi Tanabe Pharma Corp Chinazolinderivate
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
WO2003026664A1 (en) 2001-09-26 2003-04-03 Bayer Corporation 2-phenylamino-4- (5-pyrazolylamino) -pyramidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
US7560269B2 (en) 2002-12-20 2009-07-14 Acea Biosciences, Inc. Real time electronic cell sensing system and applications for cytotoxicity profiling and compound assays
CN100577811C (zh) 2002-07-20 2010-01-06 美国艾森生物科学公司 基于阻抗分析细胞和颗粒的装置和方法
US7468255B2 (en) 2002-12-20 2008-12-23 Acea Biosciences Method for assaying for natural killer, cytotoxic T-lymphocyte and neutrophil-mediated killing of target cells using real-time microelectronic cell sensing technology
US7732127B2 (en) 2002-12-20 2010-06-08 Acea Biosciences, Inc. Dynamic monitoring of cell adhesion and spreading using the RT-CES system
US7470533B2 (en) 2002-12-20 2008-12-30 Acea Biosciences Impedance based devices and methods for use in assays
EP1551410A2 (en) 2002-09-06 2005-07-13 Smithkline Beecham Corporation Novel compounds
KR20040042896A (ko) 2002-11-15 2004-05-20 미쯔비시 웰 파마 가부시키가이샤 의약 제제 조성물
CA2550274A1 (en) 2003-11-12 2005-05-26 Acea Biosciences, Inc. Real time electronic cell sensing systems and applications for cell-based assays
CA2550361C (en) 2003-12-19 2014-04-29 Prabha Ibrahim Compounds and methods for development of ret modulators
ZA200602666B (en) 2004-01-12 2007-09-26 Cytopia Res Pty Ltd Selective kinase inhibitors
CA2557667A1 (en) 2004-03-02 2005-09-15 Neurogen Corporation Aryl substituted purine analogues
US20060058339A1 (en) 2004-06-17 2006-03-16 Ibrahim Prabha N Compounds modulating c-kit activity and uses therefor
EP1773826A4 (en) 2004-07-02 2009-06-03 Exelixis Inc MODULATORS OF C-MET AND THEIR METHOD OF USE
DK1928872T3 (da) 2005-09-21 2012-05-07 4Sc Ag Hidtil ukendte sulfonylpyrroler som inhibitorer af hdac
BRPI0617241A2 (pt) 2005-10-13 2016-11-08 Glaxo Group Ltd composto ou um sal ou solvato do mesmo, composição farmacêutica, método para tratar uma doença ou condição mediada por atividade syk inadequada em um mamífero, e, uso de um composto ou um sal ou solvato farmaceuticamente aceitável do mesmo
KR100832593B1 (ko) 2005-11-08 2008-05-27 한미약품 주식회사 신호전달 저해제로서의 퀴나졸린 유도체 및 이의 제조방법
GB0526246D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
AU2007224162A1 (en) 2006-03-03 2007-09-13 Aveo Pharmaceuticals, Inc. Processes for synthesizing 7-alkynyl-4-aminoquinazolines and a related intermediate
EA200870385A1 (ru) 2006-03-29 2009-04-28 Фолдркс Фармасьютикалз, Инк. Ингибирование токсичности альфа-синуклеина
US8314234B2 (en) 2006-09-25 2012-11-20 Janssen Pharmaceutica N.V. Bicyclic pyrimidine kinase inhibitors
DK2091918T3 (en) 2006-12-08 2014-12-01 Irm Llc Compounds and Compositions as Protein Kinase Inhibitors
MX2009007944A (es) 2007-01-26 2009-08-07 Irm Llc Compuestos y composiciones de purina como inhibidores de quinasa para el tratamiento de enfermedades relacionadas con plasmodium.
AU2008210266B2 (en) 2007-01-31 2013-09-05 Ym Biosciences Australia Pty Ltd Thiopyrimidine-based compounds and uses thereof
TWI377944B (en) 2007-06-05 2012-12-01 Hanmi Holdings Co Ltd Novel amide derivative for inhibiting the growth of cancer cells
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
US7981903B2 (en) 2007-08-08 2011-07-19 Glaxosmithkline Llc 2-[2-{phenylamino}-1H-pyrrolo[2,3-D]pyrimidin-4-yl)amino] benzamide derivatives as IGF-1R inhibitors for the treatment of cancer
WO2009032694A1 (en) 2007-08-28 2009-03-12 Dana Farber Cancer Institute Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
JP5600063B2 (ja) 2007-10-19 2014-10-01 セルジーン アビロミクス リサーチ， インコーポレイテッド ヘテロアリール化合物およびその使用
NZ588830A (en) 2008-04-22 2012-11-30 Portola Pharm Inc Inhibitors of protein kinases
EP3210609A1 (en) 2008-05-21 2017-08-30 Ariad Pharmaceuticals, Inc. Phosphorous derivatives as kinase inhibitors
CA2986640C (en) * 2008-06-27 2019-03-26 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US8338439B2 (en) * 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
WO2010045451A1 (en) 2008-10-16 2010-04-22 Glaxosmithkline Llc Pyrrolopyrimidine compounds
CN102307875A (zh) 2009-02-09 2012-01-04 苏伯俭股份有限公司 吡咯并嘧啶基axl激酶抑制剂
CA2760794C (en) * 2009-05-05 2017-07-25 Dana Farber Cancer Institute Egfr inhibitors and methods of treating disorders
RU2536586C2 (ru) * 2009-10-22 2014-12-27 Марсель Петер Герард МАЕС Система сигнализации с улучшенной контрастностью
US20110207736A1 (en) * 2009-12-23 2011-08-25 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
CN102639936B (zh) 2009-12-28 2016-05-04 巴西石油公司 高性能燃烧设备和用于生产轻石蜡的流体催化裂化工艺
US20130137709A1 (en) 2010-05-05 2013-05-30 Nathanael S. Gray Compounds that modulate EGFR activity and methods for treating or preventing conditions therewith
NZ605988A (en) * 2010-06-23 2014-11-28 Hanmi Science Co Ltd Novel fused pyrimidine derivatives for inhibition of tyrosine kinase activity
EP2635285B1 (en) * 2010-11-01 2017-05-03 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
US8975249B2 (en) * 2010-11-01 2015-03-10 Celgene Avilomics Research, Inc. Heterocyclic compounds and uses thereof
US8796255B2 (en) * 2010-11-10 2014-08-05 Celgene Avilomics Research, Inc Mutant-selective EGFR inhibitors and uses thereof
CN102583089B (zh) 2011-01-11 2015-11-25 山东新北洋信息技术股份有限公司 薄片类介质处理装置
EP2683444A1 (en) 2011-03-07 2014-01-15 Fondazione Telethon Tfeb phosphorylation inhibitors and uses thereof
WO2012135801A1 (en) 2011-04-01 2012-10-04 University Of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
BR112013027734A2 (pt) * 2011-05-04 2017-08-08 Ariad Pharma Inc compostos para a inibição de proliferação celular em cânceres impulsionados pelo egfr, método e composição farmacêutica
KR102052670B1 (ko) * 2011-05-17 2019-12-06 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 키나아제 저해제
US8828391B2 (en) 2011-05-17 2014-09-09 Boehringer Ingelheim International Gmbh Method for EGFR directed combination treatment of non-small cell lung cancer
EP2802568A1 (en) 2012-01-13 2014-11-19 Acea Biosciences, Inc. Heterocyclic compounds and uses as anticancer agents.
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
ES2618007T3 (es) 2012-08-06 2017-06-20 Acea Biosciences, Inc. Nuevos compuestos de pirrolopirimidina como inhibidores de proteína cinasas
SG11201600062RA (en) 2013-07-11 2016-02-26 Acea Biosciences Inc Pyrimidine derivatives as kinase inhibitors
CN104306348B (zh) 2014-09-30 2017-05-31 地奥集团成都药业股份有限公司 一种辛伐他汀片及其制备方法
CN107949388B (zh) 2015-10-09 2021-10-26 艾森医药公司 吡咯并嘧啶激酶抑制剂的药用盐、物理形态和组合物及其制备方法
BR112019020840A2 (pt) 2017-04-07 2020-04-28 Acea Therapeutics Inc sais farmacêuticos, formas físicas e composições de inibidores da pirrolopirimidina quinase e métodos de produção dos mesmos

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