CR20150462A - Inhibidores de erk y sus usos - Google Patents

Inhibidores de erk y sus usos

Info

Publication number
CR20150462A
CR20150462A CR20150462A CR20150462A CR20150462A CR 20150462 A CR20150462 A CR 20150462A CR 20150462 A CR20150462 A CR 20150462A CR 20150462 A CR20150462 A CR 20150462A CR 20150462 A CR20150462 A CR 20150462A
Authority
CR
Costa Rica
Prior art keywords
erk inhibitors
erk
inhibitors
compositions
methods
Prior art date
Application number
CR20150462A
Other languages
English (en)
Inventor
Nadia Haq
Deqiang Niu
Russell C Petter
Lixin Qiao
Juswinder Singh
Zhendong Zhu
Original Assignee
Celgene Avilomics Res 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=51297853&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CR20150462(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Celgene Avilomics Res Inc filed Critical Celgene Avilomics Res Inc
Publication of CR20150462A publication Critical patent/CR20150462A/es

Links

Classifications

    • 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
    • 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
    • A61K31/535—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
    • 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
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • 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
    • 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
    • C07D239/48—Two nitrogen atoms
    • 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
    • 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
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invención proporciona compuestos, sus composiciones y sus métodos de uso.
CR20150462A 2013-02-08 2015-09-03 Inhibidores de erk y sus usos CR20150462A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361762408P 2013-02-08 2013-02-08
US201361785126P 2013-03-14 2013-03-14
PCT/US2014/015256 WO2014124230A2 (en) 2013-02-08 2014-02-07 Erk inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
CR20150462A true CR20150462A (es) 2015-10-26

Family

ID=51297853

Family Applications (1)

Application Number Title Priority Date Filing Date
CR20150462A CR20150462A (es) 2013-02-08 2015-09-03 Inhibidores de erk y sus usos

Country Status (20)

Country Link
US (5) US9145387B2 (es)
EP (1) EP2953457B1 (es)
JP (1) JP2016509012A (es)
KR (1) KR20150119012A (es)
CN (1) CN105188371A (es)
AU (1) AU2014214846A1 (es)
CA (1) CA2900012A1 (es)
CL (1) CL2015002194A1 (es)
CR (1) CR20150462A (es)
EA (1) EA201591051A1 (es)
ES (1) ES2805359T3 (es)
HK (1) HK1217410A1 (es)
IL (1) IL240239A0 (es)
MX (1) MX2015009952A (es)
NI (1) NI201500099A (es)
PE (1) PE20151274A1 (es)
PH (1) PH12015501660A1 (es)
SG (1) SG11201505850WA (es)
TW (1) TW201446745A (es)
WO (1) WO2014124230A2 (es)

Families Citing this family (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2734205T3 (en) 2011-07-21 2018-06-14 Tolero Pharmaceuticals Inc Heterocyclic Protein Kinase Inhibitors
CN105188371A (zh) 2013-02-08 2015-12-23 西建阿维拉米斯研究公司 Erk抑制剂及其用途
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 Ｐ２ｘ７調節劑
ES2689526T3 (es) 2013-03-14 2018-11-14 Janssen Pharmaceutica Nv Moduladores de P2X7
JP6294953B2 (ja) 2013-03-14 2018-03-14 ヤンセン ファーマシューティカ エヌ．ベー． Ｐ２ｘ７調節物質
US9446064B2 (en) 2013-03-14 2016-09-20 Epizyme, Inc. Combination therapy for treating cancer
EA029052B1 (ru) 2013-03-14 2018-02-28 Бёрингер Ингельхайм Интернациональ Гмбх Замещенные (бензилцианометил)амиды 2-азабицикло[2.2.1]гептан-3-карбоновых кислот в качестве ингибиторов катепсина с
PT2970205T (pt) * 2013-03-14 2019-08-26 Tolero Pharmaceuticals Inc Inibidores da jak2 e da alk2 e métodos para a sua utilização
JO3509B1 (ar) 2013-03-14 2020-07-05 Janssen Pharmaceutica Nv معدلات p2x7
US10273224B2 (en) * 2013-08-22 2019-04-30 Jubilant Biosys Limited Substituted pyrimidine compounds, compositions and medicinal applications thereof
US10329270B2 (en) 2013-10-21 2019-06-25 Merck Patent Gmbh Heteroaryl compounds as BTK inhibitors and uses thereof
AU2014360446A1 (en) 2013-12-05 2016-06-09 Pharmacyclics, Llc Inhibitors of Bruton's tyrosine kinase
RU2016129380A (ru) 2013-12-20 2018-01-25 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Замещенные диаминопиримидильные соединения, их композиции и способы лечения с их участием
TW201613864A (en) 2014-02-20 2016-04-16 Takeda Pharmaceutical Novel compounds
WO2016025561A1 (en) * 2014-08-13 2016-02-18 Celgene Avilomics Research, Inc. Forms and compositions of an erk inhibitor
US20170232030A1 (en) * 2014-08-13 2017-08-17 Epizyme, Inc. Combination therapy for treating cancer
HUE047208T2 (hu) 2014-09-12 2020-04-28 Boehringer Ingelheim Int A katepszin-C spirociklikus inhibitorai
AU2015315693B2 (en) 2014-09-12 2020-01-16 Janssen Pharmaceutica Nv P2X7 modulating n-acyl-triazolopyrazines
WO2016039977A1 (en) 2014-09-12 2016-03-17 Janssen Pharmaceutica Nv P2x7 modulators
CA2969587A1 (en) * 2014-12-05 2016-06-09 Centre National De La Recherche Scientifique (Cnrs) Compounds for treating cystic fibrosis
WO2016100452A2 (en) * 2014-12-17 2016-06-23 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CN104860890B (zh) * 2015-04-29 2018-03-13 上海泓博智源医药股份有限公司 T790m突变型egfr的抑制剂及其在制备抗肿瘤药物中的应用
WO2016187028A1 (en) * 2015-05-15 2016-11-24 Celgene Avilomics Research, Inc. Heteroaryl compounds, synthesis thereof, and intermediates thereto
CN105130907B (zh) * 2015-07-29 2018-10-16 沈阳药科大学 嘧啶类化合物及其用途
EP3347097B1 (en) 2015-09-11 2021-02-24 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine derivatives as modulators of the kinases jak, flt3 and aurora
WO2017068412A1 (en) 2015-10-21 2017-04-27 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
CN105646371B (zh) * 2016-01-19 2019-10-01 浙江大学 含异羟肟酸片段的2,4-二芳胺基嘧啶类衍生物及制备和应用
CN105968056A (zh) * 2016-05-28 2016-09-28 大连医科大学 二芳基嘧啶类化合物，组合物及用途
ES2940911T3 (es) * 2016-06-27 2023-05-12 Rigel Pharmaceuticals Inc Compuestos de 2,4-diamino-pirimidina y su uso como inhibidores de IRAK4
SG11201900328WA (en) 2016-07-13 2019-02-27 Jason Marineau Inhibitors of cyclin-dependent kinase 7 (cdk7)
CN106349224A (zh) * 2016-08-03 2017-01-25 山东大学 一种含有4‑氨基‑(1h)‑吡唑结构的jak激酶抑制剂及其制备方法和应用
US10499500B2 (en) * 2016-11-04 2019-12-03 Flex Ltd. Circuit board with embedded metal pallet and a method of fabricating the circuit board
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
WO2018195450A1 (en) 2017-04-21 2018-10-25 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
CN107271672B (zh) * 2017-06-21 2019-01-01 首都医科大学附属北京友谊医院 外泌体p-ERK在制备结直肠癌诊断产品中的应用
EP3686197B1 (en) * 2017-09-21 2023-06-21 Beijing Scitech-MQ Pharmaceuticals Limited 2-substituted pyrazole amino-4-substituted amino-5-pyrimidine formamide compound, composition, and application thereof
JP7425724B2 (ja) * 2017-10-17 2024-01-31 エピザイム，インコーポレイティド Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物及びその誘導体
AU2019209470A1 (en) 2018-01-16 2020-08-13 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
CA3088529A1 (en) 2018-01-16 2019-07-25 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
BR112020020246A8 (pt) 2018-04-05 2022-10-18 Sumitomo Dainippon Pharma Oncology Inc Inibidores de cinase axl e uso dos mesmos
MX2020010556A (es) 2018-04-13 2021-03-02 Sumitomo Pharma Oncology Inc Inhibidores de cinasa de insercion proviral en linfomas murinos (pim) para el tratamiento de neoplasias mieloproliferativas y fibrosis asociadas con cancer.
KR20210038906A (ko) 2018-07-26 2021-04-08 스미토모 다이니폰 파마 온콜로지, 인크. 비정상적 acvr1 발현과 연관된 질환을 치료하는 방법 및 그에 사용하기 위한 acvr1 억제제
JP7413368B2 (ja) 2018-09-28 2024-01-15 ヤンセン ファーマシューティカ エヌ．ベー． モノアシルグリセロールリパーゼ調節因子
MA53721A (fr) 2018-09-28 2021-09-15 Janssen Pharmaceutica Nv Modulateurs de la monoacylglycérol lipase
EP3873462A4 (en) 2018-11-01 2022-08-03 Syros Pharmaceuticals, Inc. CANCER TREATMENT METHODS IN BIOMARKER-IDENTIFIED PATIENTS WITH NON-COVALENT INHIBITORS OF CYCLINE-DEPENDENT KINASE 7 (CDK7)
WO2020128020A2 (de) 2018-12-21 2020-06-25 Saltigo Gmbh Verfahren zur herstellung von 2-alkoxy-4-amino-5-methyl-pyridinen und/oder von 2-alkoxy-4-alkylamino-5-methyl-pyridinen
BR112021011894A2 (pt) 2018-12-21 2021-09-08 Daiichi Sankyo Company, Limited Composição farmacêutica
HUE072069T2 (hu) 2019-02-12 2025-10-28 Sumitomo Pharma America Inc 2-((1R,4R)-4-((3-(3-(trifluormetil)fenil)imidazo[1,2- b]piridazin-6-il)amino)ciklohexil)propán-2-ol sósavas sójának kristályos formája
WO2020257385A1 (en) * 2019-06-20 2020-12-24 Dana-Farber Cancer Institute, Inc. Small molecule inhibitors of src tyrosine kinase
CN114008028B (zh) * 2019-06-20 2024-07-09 昂科比克斯有限公司 抑制癌细胞生长的嘧啶衍生物及其医药用途
AU2020300619A1 (en) 2019-07-03 2022-01-27 Sumitomo Pharma Oncology, Inc. Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof
CA3156100A1 (en) 2019-09-30 2021-04-08 Janssen Pharmaceutica Nv Radiolabelled mgl pet ligands
CA3176946A1 (en) 2020-03-26 2021-09-30 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
CN116710444A (zh) * 2020-10-30 2023-09-05 缆图药品公司 嘧啶化合物、组合物及其医药应用
EP4237418B1 (en) * 2020-10-30 2026-02-11 Blueprint Medicines Corporation Pyrimidine compounds, compositions, and medicinal applications thereof
EP4237088A1 (en) * 2020-10-30 2023-09-06 Blueprint Medicines Corporation Pyrimidine compounds, compositions, and medicinal applications thereof
CN116685583A (zh) * 2020-10-30 2023-09-01 缆图药品公司 嘧啶化合物、组合物及其医药应用
US12668594B2 (en) 2020-12-23 2026-06-30 Sudo Biosciences Limited TYK2 inhibitors and uses thereof
IL305119A (en) 2021-02-19 2023-10-01 Sudo Biosciences Ltd Tyk2 inhibitors and uses thereof
TW202302583A (zh) 2021-02-19 2023-01-16 英商蘇多生物科學有限公司 Ｔｙｋ２抑制劑及其用途
KR20230159421A (ko) 2021-02-19 2023-11-21 수도 바이오사이언시즈 리미티드 Tyk2 억제제 및 이의 용도
EP4306518A1 (en) * 2021-03-11 2024-01-17 Oncobix Co., Ltd. Novel pyrimidine derivative showing inhibition effect on growth of cancer cells
US20220378711A1 (en) * 2021-05-11 2022-12-01 United States Government As Represented By The Department Of Veterans Affairs PH-Responsive Nanoparticles for Treating Cancer
TW202329937A (zh) 2021-12-03 2023-08-01 美商英塞特公司 雙環胺ｃｋ１２抑制劑
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
AU2023372386A1 (en) 2022-10-31 2025-05-08 Sumitomo Pharma America, Inc. Pim1 inhibitor for treating myeloproliferative neoplasms
US20260200857A1 (en) 2022-12-22 2026-07-16 Saltigo Gmbh Process for the production of alkyl-pyridine n-oxides
KR20260019479A (ko) 2023-05-04 2026-02-10 레볼루션 메디슨즈, 인크. Ras 관련 질환 또는 장애를 위한 병용 요법
CN121889155A (zh) 2023-08-07 2026-04-17 锐新医药公司 用于治疗ras蛋白相关疾病或病症的rmc-6291
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
CN117510413B (zh) * 2023-10-26 2025-11-14 杭州医学院 一种dclk1激酶抑制剂及其制备方法和应用
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
KR102948940B1 (ko) * 2024-07-17 2026-04-06 연세대학교 산학협력단 N4-(인돌린-7-일)-n2-(2-알콕시피리딘-3-일)피리미딘-2,4-디아민 유도체
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
CN118878521B (zh) * 2024-09-26 2025-02-14 苏州美诺医药科技有限公司 一种lrrk2抑制剂的制备方法
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026090116A2 (en) 2024-10-21 2026-04-30 Revolution Medicines, Inc. Ras inhibitors
US20260108528A1 (en) 2024-10-22 2026-04-23 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2026090245A1 (en) 2024-10-22 2026-04-30 Revolution Medicines, Inc. Use of ras inhibitors for treating cancer
WO2026106912A1 (en) 2024-11-12 2026-05-21 Revolution Medicines, Inc. Ras inhibitors
WO2026112260A1 (en) 2024-11-21 2026-05-28 Revolution Medicines, Inc. Ras inhibitors
WO2026122764A2 (en) 2024-12-06 2026-06-11 Revolution Medicines, Inc. Ras inhibitors
WO2026128688A2 (en) 2024-12-13 2026-06-18 Revolution Medicines, Inc. Ras inhibitors
WO2026161839A1 (en) 2025-01-27 2026-07-30 Revolution Medicines, Inc. Ras inhibitors
CN120647626B (zh) * 2025-06-09 2026-02-27 江西省肿瘤医院(江西省第二人民医院、江西省癌症中心) 一种靶向egfr、axl靶点的4-氨基嘧啶类化合物及其制备方法和应用

Family Cites Families (211)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1062357A (en) 1965-03-23 1967-03-22 Pfizer & Co C Quinazolone derivatives
US4337341A (en) 1976-11-02 1982-06-29 Eli Lilly And Company 4a-Aryl-octahydro-1H-2-pyrindines
GB8608335D0 (en) 1986-04-04 1986-05-08 Pfizer Ltd Pharmaceutically acceptable salts
JPH0741461A (ja) 1993-05-27 1995-02-10 Eisai Co Ltd スルホン酸エステル誘導体
EP0813525B9 (en) 1995-03-10 2004-02-04 Berlex Laboratories, Inc. Benzamidine derivatives their preparation and their use as anti-coagulants
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
CH691000A5 (de) 1996-03-12 2001-03-30 Ciba Sc Holding Ag Faserreaktive UV-Absorber mit einem Triazinyl- oder Pyrimidinylrest,, ihre Herstellung und Verwendung.
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
GB9622363D0 (en) 1996-10-28 1997-01-08 Celltech Therapeutics Ltd Chemical compounds
ATE401312T1 (de) 1997-12-15 2008-08-15 Astellas Pharma Inc Pyrimidin-5-carboxamid-derivate
US6303652B1 (en) 1998-08-21 2001-10-16 Hughes Institute BTK inhibitors and methods for their identification and use
AU5438299A (en) 1998-08-29 2000-03-21 Astrazeneca Ab Pyrimidine compounds
ES2351149T3 (es) 1998-11-09 2011-02-01 Biogen Idec Inc. Anticuerpo quimérico dirigido contra cd20, el rituxan, para uso en el tratamiento de la leucemia linfocítica crónica.
ID28376A (id) 1998-11-10 2001-05-17 Janssen Pharmaceutica Nv Pirimidina yang menghambat replikasi hiv
US6262088B1 (en) 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
US6127376A (en) 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
EP1150955A2 (en) 1999-02-04 2001-11-07 Millennium Pharmaceuticals, Inc. G-protein coupled heptahelical receptor binding compounds and methods of use thereof
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
AU5835400A (en) 1999-06-29 2001-01-31 Egis Gyogyszergyar Rt. Novel piperazinylalkylthiopyrimidine derivatives, pharmaceutical compositions containing the same, and process for the preparation of the active substance
CA2396693A1 (en) 1999-12-28 2001-07-05 Stephen T. Wrobleski Cytokine, especially tnf-alpha, inhibitors
KR20030024659A (ko) 2000-02-17 2003-03-26 암겐 인코포레이티드 키나제 억제제
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7034019B2 (en) 2000-05-08 2006-04-25 Janssen Pharmaceutica N.V. Prodrugs of HIV replication inhibiting pyrimidines
CA2406562C (en) 2000-05-08 2009-09-15 Janssen Pharmaceutica N.V. Hiv replication inhibiting pyrimidines and triazines
CA2417500C (en) 2000-07-28 2008-11-18 Georgetown University Medical Center Erbb-2 selective small molecule kinase inhibitors
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
US6908906B2 (en) 2001-02-09 2005-06-21 Sankyo Company, Limited Crystalline forms of pyrimidine nucleoside derivative
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
IL161662A0 (en) 2001-11-01 2004-09-27 Janssen Pharmaceutica Nv Heteroaryl amines as glycogen synthase kinase 3 beta inhibitors (gsk3 inhibitors)
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US7459455B2 (en) 2002-02-08 2008-12-02 Smithkline Beecham Corporation Pyrimidine compounds
US7288547B2 (en) 2002-03-11 2007-10-30 Schering Ag CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
WO2003081210A2 (en) 2002-03-21 2003-10-02 Sunesis Pharmaceuticals, Inc. Identification of kinase inhibitors
US20040002395A1 (en) 2002-06-27 2004-01-01 Poynor Raymond L. Bridge weight for metal wood golf club
IL166241A0 (en) 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
CA2439440A1 (en) 2002-09-05 2004-03-05 Emory University Treatment of tuberous sclerosis associated neoplasms
AU2002951853A0 (en) 2002-10-04 2002-10-24 Commonwealth Scientific And Industrial Research Organisation Crystal structure of erbb2 and uses thereof
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
EP1597237B1 (en) 2003-02-07 2016-07-27 Janssen Pharmaceutica NV Pyrimidine derivatives for the prevention of HIV infection
ES2325440T3 (es) 2003-02-20 2009-09-04 Smithkline Beecham Corporation Compuestos de pirimidina.
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
US20050043233A1 (en) 2003-04-29 2005-02-24 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
US7504396B2 (en) 2003-06-24 2009-03-17 Amgen Inc. Substituted heterocyclic compounds and methods of use
ES2421139T3 (es) 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
DK1663242T3 (da) 2003-08-07 2011-08-01 Rigel Pharmaceuticals Inc 2,4-Pyrimidindiamin-forbindelser og anvendelse som antiproliferative midler
ATE542801T1 (de) 2003-08-15 2012-02-15 Novartis Ag Zur behandlung von neoplastischen krankheiten, entzündlichen erkrankungen und erkrankungen des immunsystems geeignete 2,4-pyrimidindiamine
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
AU2004272288B2 (en) 2003-09-18 2008-11-13 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
EP1694652A1 (en) 2003-12-19 2006-08-30 Rigel Pharmaceuticals, Inc. Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
EP1701704A2 (en) 2003-12-31 2006-09-20 Pfizer Products Inc. Solid compositions of low-solubility drugs and poloxamers
ES2389203T3 (es) 2004-01-12 2012-10-24 Ym Biosciences Australia Pty Ltd Inhibidores de quinasa selectivos
CN1930128A (zh) 2004-01-16 2007-03-14 惠氏公司 受体酪氨酸激酶抑制剂的喹啉中间体及其合成
WO2005080350A1 (en) 2004-02-23 2005-09-01 Glaxo Group Limited Pyrimidine derivatives as cannabinoid receptor modulators
US7378448B2 (en) 2004-03-15 2008-05-27 Eli Lilly And Company Diphenylether amide derivatives as opioid receptor antagonists
WO2005105988A2 (en) 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Crystal structure of human jak3 kinase domain complex and binding pockets thereof
JP4812763B2 (ja) 2004-05-18 2011-11-09 ライジェル ファーマシューティカルズ， インコーポレイテッド シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途
EP1598343A1 (de) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
AU2005250484B2 (en) 2004-06-04 2011-08-11 Genentech, Inc. EGFR mutations
ES2328601T3 (es) 2004-06-28 2009-11-16 Bayer Schering Pharma Ag Pirimidinas 4,6-disustituidas y su uso como inhibidores de proteina cinasa.
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
KR101215370B1 (ko) 2004-09-14 2012-12-26 엘지전자 주식회사 기록매체 및 기록매체의 기록 재생 방법 및 장치
EP1805142A4 (en) 2004-09-23 2009-06-10 Reddy Us Therapeutics Inc PYRIDINE-BASED COMPOUNDS, PROCESS FOR THEIR PREPARATION AND COMPOSITIONS CONTAINING SAME
ATE520672T1 (de) 2004-09-30 2011-09-15 Tibotec Pharm Ltd Hiv-hemmende 5-carbo- oder heterozyklisch substituierte pyrimidine
WO2006038001A1 (en) 2004-10-06 2006-04-13 Celltech R & D Limited Aminopyrimidine derivatives as jnk inhibitors
US7799915B2 (en) 2004-10-13 2010-09-21 Wyeth Llc Anilino-pyrimidine analogs
EP2100899A3 (en) 2004-10-20 2009-09-30 Proteolix, Inc. Compounds for proteasome enzyme inhibition
BRPI0517272A (pt) 2004-10-29 2008-10-07 Tibotec Pharm Ltd derivados de pirimidina bicìclicos de inibição de hiv
WO2006053109A1 (en) 2004-11-10 2006-05-18 Synta Pharmaceuticals Corp. Heteroaryl compounds
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
ATE540035T1 (de) 2004-11-24 2012-01-15 Rigel Pharmaceuticals Inc Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
US8211929B2 (en) 2004-12-30 2012-07-03 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
AU2006204724A1 (en) 2005-01-14 2006-07-20 Millennium Pharmaceuticals, Inc. Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity
US7449458B2 (en) 2005-01-19 2008-11-11 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
WO2006086777A2 (en) 2005-02-11 2006-08-17 Memorial Sloan Kettering Cancer Center Methods and compositions for detecting a drug resistant egfr mutant
WO2006101977A2 (en) 2005-03-16 2006-09-28 Targegen, Inc. Pyrimidine compounds and methods of use
DE102005016634A1 (de) 2005-04-12 2006-10-19 Merck Patent Gmbh Neuartige Aza-Hetercyclen als Kinase-Inhibitoren
JP2008540436A (ja) 2005-05-03 2008-11-20 ライジェル ファーマシューティカルズ， インコーポレイテッド Ｊａｋキナーゼインヒビターおよびそれらの使用
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
WO2006128172A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating b cell regulated autoimmune disorders
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2006133426A2 (en) 2005-06-08 2006-12-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CA2626789A1 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Pyrimidinones as casein kinase ii (ck2) modulators
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
WO2007053452A1 (en) 2005-11-01 2007-05-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
CA2626479A1 (en) 2005-11-03 2007-05-18 Irm Llc Protein kinase inhibitors
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
JP2009520038A (ja) 2005-12-19 2009-05-21 ジェネンテック・インコーポレーテッド ピリミジンキナーゼインヒビター
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
EA200870217A1 (ru) 2006-01-30 2009-02-27 Экселиксис, Инк. 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции
KR101411695B1 (ko) 2006-02-17 2014-07-03 리겔 파마슈티칼스, 인크. 자가면역 질환의 치료 또는 예방을 위한 2,4-피리미딘디아민 화합물
WO2007098507A2 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
AU2007233737B2 (en) 2006-03-30 2012-11-29 Janssen Sciences Ireland Uc HIV inhibiting 5-amido substituted pyrimidines
ES2353725T3 (es) 2006-03-30 2011-03-04 Tibotec Pharmaceuticals Pirimidinas sustituidas con 5-(hidroximetileno y aminometileno) que inhiben el vih.
GB0608386D0 (en) 2006-04-27 2006-06-07 Senexis Ltd Compounds
US7560588B2 (en) 2006-04-27 2009-07-14 Intezyne Technologies, Inc. Poly(ethylene glycol) containing chemically disparate endgroups
US7540909B2 (en) 2006-05-12 2009-06-02 Seiko Epson Corporation Ink composition, ink cartridge, recording method, and recorded product
US7553357B2 (en) 2006-05-12 2009-06-30 Iko Epson Corporation Ink composition, ink cartridge, recording method, and recorded product
US7540908B2 (en) 2006-05-12 2009-06-02 Seiko Epson Corporation Ink composition, ink cartridge, recording method, and recorded product
US8604031B2 (en) 2006-05-18 2013-12-10 Mannkind Corporation Intracellular kinase inhibitors
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
AU2007269540B2 (en) 2006-07-05 2013-06-27 Exelixis, Inc. Methods of using IGF1R and Abl kinase modulators
WO2008009458A1 (en) 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
DE102006041382A1 (de) 2006-08-29 2008-03-20 Bayer Schering Pharma Ag Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren
EP2529621B1 (en) 2006-09-22 2016-10-05 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
DK2089369T3 (da) 2006-10-19 2011-05-09 Rigel Pharmaceuticals Inc 2,4-pyrimidindiaminderivater som hæmmere af JAK-kinaser til behandling af autoimmune sygdomme
MX2009004269A (es) 2006-10-23 2009-08-12 Takeda Pharmaceutical Inhibidores de cinasa mapk/erk.
WO2008054827A2 (en) 2006-11-03 2008-05-08 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
WO2008064274A1 (en) 2006-11-21 2008-05-29 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4-pyrimidinediamine compounds and their uses
EA019941B1 (ru) * 2006-12-08 2014-07-30 АйАрЭм ЭлЭлСи Соединения и композиции в качестве ингибиторов протеинкиназы
JP5208123B2 (ja) 2006-12-08 2013-06-12 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
CA2670645A1 (en) 2006-12-19 2008-07-03 Genentech, Inc. Pyrimidine kinase inhibitors
EP1939185A1 (de) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs
EP2109605B1 (en) * 2006-12-22 2013-02-20 Boehringer Ingelheim International GmbH 2- [(phenylamino) -pyrimidin-4ylamin0] -cyclopentane carboxamide derivatives and related compounds as inhibitors of kinases of the cell cycle for the treatment of cancer
US8318736B2 (en) 2006-12-29 2012-11-27 Janssen R&D Ireland HIV inhibiting 5,6-substituted pyrimidines
US9006243B2 (en) 2006-12-29 2015-04-14 Janssen R&D Ireland HIV inhibiting 6-substituted pyrimidines
PE20081636A1 (es) 2007-01-26 2009-01-10 Smithkline Beecham Corp Inhibidores de antranilamida para aurora quinasa
CA2702647C (en) 2007-01-31 2016-03-22 Ym Biosciences Australia Pty Ltd Thiopyrimidine-based compounds and uses thereof
JP4221470B2 (ja) 2007-02-01 2009-02-12 トヨタ自動車株式会社 電動車両制御装置及び電動車両制御方法
DE102007010801A1 (de) 2007-03-02 2008-09-04 Bayer Cropscience Ag Diaminopyrimidine als Fungizide
US20100105674A1 (en) 2007-03-20 2010-04-29 Deanda Jr Felix Chemical Compounds
CA2681250A1 (en) 2007-03-20 2008-09-25 Smithkline Beecham Corporation Chemical compounds
US7947698B2 (en) 2007-03-23 2011-05-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
WO2008118823A2 (en) 2007-03-26 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20120065201A1 (en) 2007-03-28 2012-03-15 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
EP1990342A1 (en) 2007-05-10 2008-11-12 AEterna Zentaris GmbH Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof
WO2008147831A1 (en) 2007-05-23 2008-12-04 Smithkline Beecham Corporation Anthranilamides
US8242271B2 (en) 2007-06-04 2012-08-14 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
CN101903357A (zh) 2007-07-17 2010-12-01 里格尔药品股份有限公司 作为pkc抑制剂的环状胺取代的嘧啶二胺
JP5588865B2 (ja) 2007-07-31 2014-09-10 リジェネロン・ファーマシューティカルズ・インコーポレイテッド ヒトｃｄ２０に対するヒト抗体及びその使用方法
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
US20090088371A1 (en) 2007-08-28 2009-04-02 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
BRPI0815979A2 (pt) 2007-08-28 2017-06-13 Irm Llc compostos e composições com inibidores de quinase, bem como uso dos mesmos
WO2009032703A1 (en) 2007-08-28 2009-03-12 Irm Llc 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma 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
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
CA2710118A1 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
RU2490015C2 (ru) 2008-02-22 2013-08-20 Райджел Фармасьютикалз, Инк. Применение 2,4-пиримидиндиаминов для лечения атеросклероза
US20110098288A1 (en) 2008-03-11 2011-04-28 Jeremy Major Sulfonamides as zap-70 inhibitors
US8205348B2 (en) 2008-03-19 2012-06-26 Zashiki-Warashi Manufacturing Inc. Tile spacer and holder therefor
CL2009000600A1 (es) 2008-03-20 2010-05-07 Bayer Cropscience Ag Uso de compuestos de diaminopirimidina como agentes fitosanitarios; compuestos de diaminopirimidina; su procedimiento de preparacion; agente que los contiene; procedimiento para la preparacion de dicho agente; y procedimiento para combatir plagas de animales y/u hongos dañinos patogenos de plantas.
WO2009127642A2 (en) 2008-04-15 2009-10-22 Cellzome Limited Use of lrrk2 inhibitors for neurodegenerative diseases
AU2009251863B2 (en) 2008-04-16 2014-09-25 Alexion Pharmaceuticals, Inc. 2, 6-diamino-pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
KR20100132550A (ko) 2008-04-16 2010-12-17 포톨라 파마슈티컬스, 인코포레이티드 ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드
CA2722326A1 (en) 2008-04-24 2009-10-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
JP2011523646A (ja) 2008-05-21 2011-08-18 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのリン誘導体
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
AU2009262068C1 (en) 2008-06-27 2015-07-02 Celgene Car Llc Heteroaryl compounds and uses thereof
CN102159214A (zh) 2008-07-16 2011-08-17 药品循环公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
WO2010022121A1 (en) * 2008-08-20 2010-02-25 Schering Corporation Substituted pyridine and pyrimidine derivatives and their use in treating viral infections
WO2010025833A1 (de) 2008-09-03 2010-03-11 Bayer Cropscience Ag Alkoxy- und alkylthio-substituierte anilinopyrimidine
WO2010077740A2 (en) 2008-12-09 2010-07-08 Cytokine Pharmasciences, Inc. Novel antiviral compounds, compositions, and methods of use
CA2748758C (en) 2009-01-15 2017-06-13 F. Hoffmann-La Roche Ag Antibodies against phosphorylated tyrosines on erythropoietin receptor (epor)
US20110071158A1 (en) * 2009-03-18 2011-03-24 Boehringer Ingelheim International Gmbh New compounds
US20120270237A9 (en) 2009-04-03 2012-10-25 Cellzone AG Methods for the identification of kinase interacting molecules and for the purification of kinase proteins
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
MX2011011875A (es) 2009-05-08 2011-12-08 Astellas Pharma Inc Compuesto de carboxamida heterociclica diamino.
TW201100441A (en) 2009-06-01 2011-01-01 Osi Pharm Inc Amino pyrimidine anticancer compounds
EP2440534A2 (en) * 2009-06-10 2012-04-18 Cellzome Limited Pyrimidine derivatives as zap-70 inhibitors
WO2010146132A1 (en) 2009-06-18 2010-12-23 Cellzome Limited Sulfonamides and sulfamides as zap-70 inhibitors
CA2771675A1 (en) 2009-09-11 2011-03-17 Cellzome Limited Ortho substituted pyrimidine compounds as jak inhibitors
US7741330B1 (en) 2009-10-12 2010-06-22 Pharmacyclics, Inc. Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase
WO2011079231A1 (en) 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
WO2011140338A1 (en) 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
US20120071497A1 (en) 2010-06-03 2012-03-22 Pharmacyclics, Inc. Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase
MX380504B (es) 2010-06-03 2025-03-12 Pharmacyclics Llc El uso de inhibidores de la tirosina quinasa de bruton (btk).
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
PH12013500246A1 (en) 2010-08-10 2019-10-11 Celgene Avilomics Res Inc Besylate salt of a btk inhibitor
BR112013010564B1 (pt) 2010-11-01 2021-09-21 Celgene Car Llc Compostos heterocíclicos e composições compreendendo os mesmos
JP5956999B2 (ja) 2010-11-01 2016-07-27 セルジーン アヴィロミクス 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
WO2012061415A1 (en) 2010-11-01 2012-05-10 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
EP2637502B1 (en) 2010-11-10 2018-01-10 Celgene CAR LLC Mutant-selective egfr inhibitors and uses thereof
WO2012078492A1 (en) 2010-12-06 2012-06-14 Celgene Corporation A combination therapy with lenalidomide and a cdk inhibitor for treating multiple myeloma
CN102558149A (zh) 2010-12-29 2012-07-11 中国医学科学院药物研究所 嘧啶衍生物、及其制法和药物组合物与用途
CN102093421B (zh) 2011-01-28 2014-07-02 北京康辰药业有限公司 一种含磷取代基的喹啉类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
EP2694486B1 (en) 2011-04-01 2018-01-10 University of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
AU2012250517B2 (en) 2011-05-04 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
DK2710007T3 (da) 2011-05-17 2020-01-27 Principia Biopharma Inc Kinasehæmmere
US20140303191A1 (en) 2011-10-19 2014-10-09 Pharmacyclics, Inc. Use of inhibitors of bruton's tyrosine kinase (btk)
JP2014532658A (ja) 2011-10-28 2014-12-08 セルジーン アヴィロミクス リサーチ， インコーポレイテッド ブルトン型チロシンキナーゼ疾患または障害を治療する方法
CN103159742B (zh) 2011-12-16 2015-08-12 北京韩美药品有限公司 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用
JP6317320B2 (ja) 2012-03-15 2018-04-25 セルジーン シーエーアール エルエルシー 上皮成長因子受容体キナーゼ阻害剤の塩
ES2880109T3 (es) 2012-03-15 2021-11-23 Celgene Car Llc Formas sólidas de un inhibidor de la cinasa del receptor del factor de crecimiento epidérmico
WO2013173518A1 (en) 2012-05-16 2013-11-21 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
KR101446742B1 (ko) 2012-08-10 2014-10-01 한국화학연구원 Ｎ2,ｎ4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
WO2014039452A1 (en) 2012-09-04 2014-03-13 Celgene Avilomics Research, Inc. Methods of treating a bruton's tyrosine kinase disease or disorder
CN103664878A (zh) 2012-09-12 2014-03-26 山东亨利医药科技有限责任公司 杂芳环及其衍生物类酪氨酸激酶抑制剂
SG11201503459SA (en) 2012-11-02 2015-06-29 Pharmacyclics Inc Tec family kinase inhibitor adjuvant therapy
AU2013341271A1 (en) 2012-11-07 2015-05-14 Novartis Ag Combination therapy
US20140142128A1 (en) 2012-11-20 2014-05-22 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
US20140142129A1 (en) 2012-11-20 2014-05-22 Celgene Avilomics Research, Inc, Methods of treating a disease or disorder associated with bruton's tyrosine kinase
WO2014081712A2 (en) 2012-11-20 2014-05-30 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
US20140140991A1 (en) 2012-11-20 2014-05-22 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with bruton's tyrosine kinase
TW201427666A (zh) 2012-11-20 2014-07-16 Celgene Avilomics Res Inc 治療和布魯頓（ｂｒｕｔｏｎ’ｓ）酪胺酸激酶相關之疾病或失調的方法
US9126950B2 (en) 2012-12-21 2015-09-08 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
CN105188371A (zh) * 2013-02-08 2015-12-23 西建阿维拉米斯研究公司 Erk抑制剂及其用途
JP6800750B2 (ja) 2013-08-02 2020-12-16 ファーマサイクリックス エルエルシー 固形腫瘍の処置方法

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