HUE035337T2 - Macrocyclic compounds as TRK kinase inhibitors - Google Patents

Macrocyclic compounds as TRK kinase inhibitors Download PDF

Info

Publication number
HUE035337T2
HUE035337T2 HUE15150036A HUE15150036A HUE035337T2 HU E035337 T2 HUE035337 T2 HU E035337T2 HU E15150036 A HUE15150036 A HU E15150036A HU E15150036 A HUE15150036 A HU E15150036A HU E035337 T2 HUE035337 T2 HU E035337T2
Authority
HU
Hungary
Prior art keywords
fluoro
mmol
ring
hexaazapentacyclo
pyrimidine
Prior art date
Application number
HUE15150036A
Other languages
English (en)
Hungarian (hu)
Inventor
Steven Andrews
Kevin CONDROSKI
Julia Haas
Yutong Jiang
Gabrielle Kolakowski
Jeongbeob Seo
Hong-Woon Yang
Qian Zhao
Original Assignee
Array Biopharma 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 Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of HUE035337T2 publication Critical patent/HUE035337T2/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/22Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/22Heterocyclic 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 systems contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
HUE15150036A 2010-05-20 2011-05-13 Macrocyclic compounds as TRK kinase inhibitors HUE035337T2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34676710P 2010-05-20 2010-05-20
US201061426716P 2010-12-23 2010-12-23

Publications (1)

Publication Number Publication Date
HUE035337T2 true HUE035337T2 (en) 2018-05-02

Family

ID=44280661

Family Applications (2)

Application Number Title Priority Date Filing Date
HUE17163978A HUE044025T2 (hu) 2010-05-20 2011-05-13 Makrociklusos vegyületek mint TRK-kináz inhibitorok
HUE15150036A HUE035337T2 (en) 2010-05-20 2011-05-13 Macrocyclic compounds as TRK kinase inhibitors

Family Applications Before (1)

Application Number Title Priority Date Filing Date
HUE17163978A HUE044025T2 (hu) 2010-05-20 2011-05-13 Makrociklusos vegyületek mint TRK-kináz inhibitorok

Country Status (34)

Country Link
US (8) US8933084B2 (OSRAM)
EP (4) EP3205654B1 (OSRAM)
JP (5) JP5832527B2 (OSRAM)
KR (4) KR101852169B1 (OSRAM)
CN (3) CN102971322B (OSRAM)
AR (1) AR081919A1 (OSRAM)
AU (4) AU2011256380C1 (OSRAM)
BR (2) BR112012029405B1 (OSRAM)
CA (1) CA2800079C (OSRAM)
CL (1) CL2012003227A1 (OSRAM)
CO (1) CO6660502A2 (OSRAM)
CR (1) CR20170098A (OSRAM)
CY (2) CY1119345T1 (OSRAM)
DK (2) DK3205654T3 (OSRAM)
ES (3) ES2628418T3 (OSRAM)
HR (2) HRP20171140T1 (OSRAM)
HU (2) HUE044025T2 (OSRAM)
IL (2) IL223094B (OSRAM)
LT (2) LT3205654T (OSRAM)
ME (1) ME03376B (OSRAM)
MX (4) MX365251B (OSRAM)
MY (1) MY191934A (OSRAM)
NZ (1) NZ604708A (OSRAM)
PH (2) PH12012502276A1 (OSRAM)
PL (2) PL3205654T3 (OSRAM)
PT (2) PT3205654T (OSRAM)
RS (1) RS58537B1 (OSRAM)
RU (2) RU2594742C2 (OSRAM)
SG (3) SG10201506593XA (OSRAM)
SI (2) SI2918588T1 (OSRAM)
SM (2) SMT201700372T1 (OSRAM)
TW (4) TWI516493B (OSRAM)
UY (1) UY33395A (OSRAM)
WO (1) WO2011146336A1 (OSRAM)

Families Citing this family (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8450322B2 (en) 2008-09-22 2013-05-28 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as Trk kinase inhibitors
TR201807039T4 (tr) 2008-10-22 2018-06-21 Array Biopharma Inc Trk kinaz inhibitörleri olarak sübstitüe edilmiş pirazolo[1,5-]pirimidin bileşikleri.
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
ES2628418T3 (es) * 2010-05-20 2017-08-02 Array Biopharma, Inc. Compuestos macrocíclicos como inhibidores de la TRK cinasa
SG10201913053QA (en) 2011-05-13 2020-03-30 Array Biopharma Inc Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors
PT2822953T (pt) * 2012-03-06 2017-04-06 Pfizer Derivados macrocíclicos para o tratamento de doenças proliferativas
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
RS55593B1 (sr) 2012-11-13 2017-06-30 Array Biopharma Inc Jedinjenja biciklične uree, tiouree, guanidina i cijanoguanidina korisna za lečenje bola
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9828360B2 (en) 2012-11-13 2017-11-28 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078325A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078331A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078328A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078408A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
SMT201800169T1 (it) 2012-11-13 2018-05-02 Array Biopharma Inc Composti di n-pirrolidinile, n'-pirazolile-urea, tiourea, guanidina e cianoguanidina come inibitore di chinasi trka
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
LT3636649T (lt) * 2014-01-24 2024-04-10 Turning Point Therapeutics, Inc. Diarilo makrociklai kaip proteinkinazių moduliatoriai
SG11201608303QA (en) 2014-04-04 2016-11-29 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
EP3154959B1 (en) 2014-05-15 2019-07-10 Array Biopharma, Inc. 1-((3s,4r)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a trka kinase inhibitor
TWI736134B (zh) * 2014-09-11 2021-08-11 美商特普醫葯公司 作為蛋白質激酶之調節劑的二芳基巨環
KR102563829B1 (ko) 2014-09-17 2023-08-03 온코디자인 에스.에이. 거대고리 rip2 키나아제 억제제
WO2016042089A1 (en) * 2014-09-17 2016-03-24 Oncodesign S.A. Macrocyclic lrrk2 kinase inhibitors
PT3699181T (pt) 2014-11-16 2023-04-05 Array Biopharma Inc Forma cristalina de hidrogenossulfato de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
US10377775B2 (en) 2014-12-04 2019-08-13 Shin-Etsu Chemical Co., Ltd. Method for producing polyalkylene glycol derivative having amino group at end
US9708350B2 (en) 2014-12-04 2017-07-18 Shin-Etsu Chemical Co., Ltd. Method for producing polyalkylene glycol derivative having amino group at end, polymerization initiator for use in the same, and alcohol compound as raw material for the polymerization initiator
JP6460937B2 (ja) * 2014-12-04 2019-01-30 信越化学工業株式会社 末端にアミノ基を有するポリアルキレングリコール誘導体の製造方法
HRP20240937T1 (hr) * 2014-12-15 2024-10-25 Cmg Pharmaceutical Co., Ltd. Heteroaril spoj sa kondeziranim prstenom i njihova primjena kao trk inhibitora
BR112017015760A2 (pt) 2015-01-23 2018-03-27 Gvk Biosciences Private Limited inibidores de quinase trka
TN2017000502A1 (en) 2015-06-01 2019-04-12 Loxo Oncology Inc Methods of diagnosing and treating cancer
US10316044B2 (en) 2015-07-02 2019-06-11 Tp Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
SMT202400213T1 (it) * 2015-07-06 2024-07-09 Turning Point Therapeutics Inc Polimorfo di diaril macrociclo
RS61485B1 (sr) 2015-07-16 2021-03-31 Array Biopharma Inc Supstituisana pirazolo [1,5-a] piridinska jedinjenja kao inhibitori ret kinaze
ES2818528T3 (es) * 2015-07-21 2021-04-13 Turning Point Therapeutics Inc Macrociclo de diarilo quiral y uso del mismo en el tratamiento del cáncer
JP6783311B2 (ja) 2015-09-24 2020-11-11 サイクレニウム ファーマ インコーポレーテッド ヘテロアリール含有大環状化合物のライブラリならびにその製造方法および使用方法
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
RS65988B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Postupak lečenja pedijatrijskih karcinoma
CN109414442B (zh) 2016-04-04 2024-03-29 洛克索肿瘤学股份有限公司 一种化合物的液体制剂
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
DK3800189T3 (da) 2016-05-18 2023-07-31 Loxo Oncology Inc Fremstilling af (s)-n-(5-((r)-2-(2,5-difluorphenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid
EP3490564A4 (en) * 2016-07-28 2020-02-26 Turning Point Therapeutics, Inc. MACRO CYCLE Kinase Inhibitors
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
EP3571203B1 (en) 2017-01-18 2023-06-07 Array BioPharma Inc. Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
JOP20190213A1 (ar) * 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
US20200190083A1 (en) * 2017-06-22 2020-06-18 Cyclenium Pharma Inc. Libraries of pyridine-containing macrocyclic compounds and methods of making and using the same
EP3658148B1 (en) 2017-07-28 2024-07-10 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof
CN113735881A (zh) 2017-08-23 2021-12-03 正大天晴药业集团股份有限公司 含有氨基吡唑并嘧啶的大环化合物及其药物组合物和用途
TWI876442B (zh) 2017-10-10 2025-03-11 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
EP3700576A1 (en) * 2017-10-26 2020-09-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
CN109516999B (zh) * 2017-11-01 2021-08-17 郑州泰基鸿诺医药股份有限公司 用作蛋白质激酶调节剂的化合物及其应用
US11098046B2 (en) 2017-11-10 2021-08-24 Angex Pharmaceutical, Inc. Macrocyclic compounds as TRK kinase inhibitors and uses thereof
MX2020006490A (es) * 2017-12-19 2020-08-17 Turning Point Therapeutics Inc Compuestos macrociclicos para tratar enfermedades.
CN109456331B (zh) 2017-12-22 2020-06-05 深圳市塔吉瑞生物医药有限公司 一种取代的吡唑并[1,5-a]嘧啶化合物及其药物组合物及用途
WO2019120267A1 (zh) * 2017-12-22 2019-06-27 成都先导药物开发股份有限公司 一种咪唑并[1,2-b]哒嗪大环类激酶抑制剂
CN111615514B (zh) 2018-01-18 2022-10-11 奥瑞生物药品公司 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物
CA3087578C (en) 2018-01-18 2023-08-08 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
EP3740491A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
CN111848622A (zh) * 2018-01-23 2020-10-30 深圳市塔吉瑞生物医药有限公司 取代的吡唑并[1,5-a]嘧啶类的大环化合物
WO2019149131A1 (zh) * 2018-01-30 2019-08-08 上海吉倍生物技术有限公司 具有大环分子结构的化合物及其用途
CN110156813B (zh) * 2018-02-13 2023-07-25 北京诺诚健华医药科技有限公司 作为trk抑制剂的杂环化合物
WO2019165967A1 (zh) * 2018-02-28 2019-09-06 南京明德新药研发有限公司 吡唑并嘧啶衍生物及其用途
JP7294677B2 (ja) * 2018-03-14 2023-06-20 フォチョン・ファーマシューティカルズ・リミテッド TRKキナーゼ阻害剤としての置換(2-アザビシクロ[3.1.0]ヘキサン-2-イル)ピラゾロ[1,5-a]ピリミジン化合物及び置換(2-アザビシクロ[3.1.0]ヘキサン-2-イル)イミダゾ[1,2-b]ピリダジン化合物
CN111971287B (zh) * 2018-03-28 2023-06-02 重庆复尚源创医药技术有限公司 作为trk激酶抑制剂的大环化合物
CA3095366A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers
US11358973B2 (en) 2018-04-16 2022-06-14 Shenzhen Targetrx, Inc. Di(hetero)aryl macrocyclic compound for inhibiting protein kinase activity
PL3786167T3 (pl) * 2018-04-25 2024-11-25 Primegene (Beijing) Co., Ltd. Diarylowy związek makrocykliczny i kompozycja farmaceutyczna oraz ich zastosowanie
CN111918868B (zh) * 2018-05-04 2022-12-30 正大天晴药业集团股份有限公司 作为蛋白激酶调节剂的二芳基大环化合物
CN110577532B (zh) * 2018-06-08 2022-06-03 江苏威凯尔医药科技有限公司 原肌球蛋白受体激酶抑制剂及其制备方法和应用
WO2019233461A1 (zh) * 2018-06-08 2019-12-12 江苏威凯尔医药科技有限公司 原肌球蛋白受体激酶抑制剂及其制备方法和应用
CN110627812B (zh) * 2018-06-25 2022-10-11 北京诺诚健华医药科技有限公司 作为trk抑制剂的杂环化合物
CA3224945C (en) 2018-07-31 2025-11-18 Loxo Oncology, Inc. SPRAY DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPAN-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE
JP2022500383A (ja) 2018-09-10 2022-01-04 アレイ バイオファーマ インコーポレイテッド Retキナーゼ阻害剤としての縮合複素環式化合物
CN112955453B (zh) * 2018-09-29 2022-04-19 山东绿叶制药有限公司 作为选择性Trk抑制剂的吡唑并嘧啶衍生物
FI3870579T3 (fi) 2018-10-22 2025-01-02 Alumis Inc Tyk2-inhibiittoreita ja niiden käyttöjä
CN111171049B (zh) * 2018-11-09 2021-06-04 山东轩竹医药科技有限公司 酪氨酸激酶抑制剂及其用途
SG11202104609SA (en) 2018-11-09 2021-06-29 Shandong Xuanzhu Pharma Co Ltd Macrocyclic tyrosine kinase inhibitor and uses thereof
CN111253402B (zh) * 2018-11-30 2021-08-03 广州白云山医药集团股份有限公司白云山制药总厂 一种trk激酶抑制剂化合物的中间体化合物及制备方法
US12180207B2 (en) 2018-12-19 2024-12-31 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases
CN113474337A (zh) 2018-12-19 2021-10-01 奥瑞生物药品公司 作为fgfr抑制剂用于治疗癌症的7-((3,5-二甲氧基苯基)氨基)喹喔啉衍生物
JP7209415B2 (ja) 2019-03-19 2023-01-20 セントラル チャイナ ノーマル ユニバーシティ ピラゾロピリミジン化合物、医薬組成物、及びその使用
BR112021019070A2 (pt) 2019-03-26 2022-02-15 Ventyx Biosciences Inc Ligantes de pseudoquinase tyk2
WO2020224626A1 (zh) 2019-05-08 2020-11-12 浙江同源康医药股份有限公司 用作激酶抑制剂的化合物及其应用
US12410191B2 (en) 2019-05-21 2025-09-09 Zhejiang Hisun Pharmaceutical Co., Ltd. Macrolide derivatives, preparation method and application thereof
CN112110938B (zh) * 2019-06-21 2021-11-09 成都海博为药业有限公司 一种作为蛋白质激酶抑制剂的化合物及其制备方法和用途
WO2021037156A1 (zh) * 2019-08-28 2021-03-04 南京明德新药研发有限公司 一种致癌性融合激酶抑制剂的晶型及其应用
CN110804059B (zh) * 2019-09-30 2024-03-12 郑州泰基鸿诺医药股份有限公司 氨基甲酸酯类化合物、药物组合物及其应用
WO2021083345A1 (zh) * 2019-10-30 2021-05-06 先声药业有限公司 吡唑并嘧啶类化合物的制备方法及其中间体
IL292785B2 (en) 2019-11-08 2025-09-01 Ventyx Biosciences Inc Tyk2 pseudokinase ligands
EP4063365A4 (en) 2019-11-18 2023-01-11 Guangzhou Joyo Pharmatech Co., Ltd Compound as highly selective ros1 inhibitor and use thereof
KR20220113771A (ko) * 2019-12-13 2022-08-16 시노허브 파마슈티컬 씨오., 엘티디 마크로사이클릭 구조를 갖는 불소-함유 헤테로사이클릭 유도체 및 이의 용도
CN113004305B (zh) * 2019-12-19 2024-04-09 赛诺哈勃药业(成都)有限公司 大环化合物及其制备方法和用途
US20230183265A1 (en) * 2020-05-08 2023-06-15 Shandong Xuanzhu Pharma Co., Ltd. Crystal Form of Macrocyclic Tyrosine Kinase Inhibitor and Preparation Method therefor
CN111777549A (zh) * 2020-07-07 2020-10-16 中瀚(齐河县)生物医药科技有限公司 一种2-甲氧基-3-溴-5-氟吡啶的合成工艺
CA3187834A1 (en) * 2020-07-10 2022-01-13 Blossomhill Therapeutics, Inc. Macrocycles and their use
CN114073704B (zh) * 2020-08-14 2023-08-11 赛诺哈勃药业(成都)有限公司 具有大环结构的含氟并杂环衍生物的应用
CN112174982A (zh) * 2020-09-10 2021-01-05 上海希迈医药科技有限公司 一种洛普替尼晶型及其制备方法
CN111875620B (zh) * 2020-09-28 2020-12-11 上海美迪西生物医药股份有限公司 吡唑并嘧啶类大环衍生物及其应用
US20240092759A1 (en) * 2021-01-08 2024-03-21 Yale University Non-Covalent Inhibitors of the Main Protease of SARS-CoV-2 and Methods of Use
WO2022213980A1 (zh) * 2021-04-07 2022-10-13 上海齐鲁制药研究中心有限公司 Tyk2抑制剂及其用途
CN115368379B (zh) * 2021-05-18 2024-08-02 广州嘉越医药科技有限公司 一种含氰基取代的大环类化合物的晶型及其制备方法
WO2022262671A1 (zh) * 2021-06-15 2022-12-22 中国医药研究开发中心有限公司 杂环大环化合物及其医药用途
WO2023025141A1 (zh) * 2021-08-23 2023-03-02 正大天晴药业集团股份有限公司 含有氨基的大环化合物在治疗trk激酶介导的肿瘤中的用途
CN113754657B (zh) * 2021-09-22 2023-01-17 广州白云山医药集团股份有限公司白云山制药总厂 大环类化合物的晶型及其制备方法和应用
CN113582994B (zh) * 2021-09-28 2022-02-11 北京鑫开元医药科技有限公司 具有trk激酶抑制活性的化合物、制备方法、组合物及其用途
JP2025503592A (ja) * 2022-01-05 2025-02-04 ブロッサムヒル・セラピューティクス・インコーポレイテッド 大環状化合物およびキナーゼ阻害剤としての使用
WO2023208244A1 (zh) * 2022-04-29 2023-11-02 南京明德新药研发有限公司 大环类化合物及其应用
WO2025137541A1 (en) * 2023-12-22 2025-06-26 Neuron23, Inc. Kinase modulators and methods of use thereof

Family Cites Families (324)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US755047A (en) * 1902-03-17 1904-03-22 Alexander Roth Robertson Bottle-seal.
EP0009517A1 (en) 1978-10-04 1980-04-16 THE PROCTER & GAMBLE COMPANY Vaginal contraceptive
KR100263817B1 (ko) 1993-11-30 2000-08-16 윌리암스 로저 에이 염증치료용 치환 피라졸일벤젠술폰아미드
US5844092A (en) 1994-03-18 1998-12-01 Genentech, Inc. Human TRK receptors and neurotrophic factor inhibitors
US5430021A (en) 1994-03-18 1995-07-04 Pharmavene, Inc. Hydrophobic drug delivery systems
US5877016A (en) 1994-03-18 1999-03-02 Genentech, Inc. Human trk receptors and neurotrophic factor inhibitors
US6677135B1 (en) 1996-05-08 2004-01-13 Biogen, Inc. Ret ligand (RetL) for stimulating neutral and renal growth
KR100587556B1 (ko) 1996-05-08 2006-06-08 바이오겐 아이덱 엠에이 인코포레이티드 신경 및 신장 증식을 자극하기 위한 RET리간드(RetL)
CA2206201A1 (en) 1996-05-29 1997-11-29 Yoshiaki Isobe Pyrazole derivatives and their pharmaceutical use
US6682921B1 (en) 1996-08-21 2004-01-27 New York University Crystals of the tyrosine kinase domain of non-insulin receptor tyrosine kinases
JP3898296B2 (ja) 1996-08-28 2007-03-28 ポーラ化成工業株式会社 ピロロピラゾロピリミジン化合物及びこれを有効成分とする医薬
EP0979231B1 (en) 1997-04-25 2004-11-24 Takeda Chemical Industries, Ltd. Condensed pyridazine derivatives, their production and use
US6531152B1 (en) 1998-09-30 2003-03-11 Dexcel Pharma Technologies Ltd. Immediate release gastrointestinal drug delivery system
UA74546C2 (en) * 1999-04-06 2006-01-16 Boehringer Ingelheim Ca Ltd Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition
AU7103900A (en) 1999-09-01 2001-03-26 Biogen, Inc. Ret ligand 5 (retl5) compositions and uses thereof
US6534085B1 (en) 1999-09-23 2003-03-18 Bioresponse L.L.C. Phytochemicals for promoting weight loss
FI20000403A0 (fi) 2000-02-22 2000-02-22 Hannu Sariola GDNF perhesukuisten yhdisteiden käyttö kivessyövän hoitoon tarkoitettujen tuotteiden valmistamiseksi
IL153375A0 (en) 2000-06-22 2003-07-06 Genentech Inc Agonist anti-trk-c monoclonal antibodies
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
ATE522229T1 (de) 2001-05-30 2011-09-15 Genentech Inc Anti-ngf-antikörper zur behandlung verschiedener erkrankungen
AU2002334355A1 (en) 2001-09-06 2003-03-18 Prochon Biotech Ltd. Protein tyrosine kinase inhibitors
US20030199525A1 (en) 2002-03-21 2003-10-23 Hirst Gavin C. Kinase inhibitors
WO2003091256A1 (en) 2002-04-23 2003-11-06 Shionogi & Co., Ltd. PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE AND NAD(P)H OXIDASE INHIBITOR CONTAINING THE SAME
US7449488B2 (en) 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
CA2493000A1 (en) 2002-07-24 2004-01-29 University Of Cincinnati 4-4(methylpiperazin-1-ylmethyl)-n-[4-methyl-3-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide for treating mutated-ret kinase associated diseases
JP4024624B2 (ja) 2002-08-26 2007-12-19 富士通株式会社 半導体装置の製造方法及び製造装置
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7119200B2 (en) 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
AU2003263071B2 (en) 2002-09-04 2007-03-15 Merck Sharp & Dohme Llc Pyrazolopyrimidines as cyclin-dependent kinase inhibitors
US7196078B2 (en) * 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
RU2357967C2 (ru) * 2002-09-16 2009-06-10 Глаксо Груп Лимитед ПРОИЗВОДНЫЕ ПИРАЗОЛО[3, 4-b]ПИРИДИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ (ВАРИАНТЫ), ПРИМЕНЕНИЕ (ВАРИАНТЫ), КОМПОЗИЦИЯ (ВАРИАНТЫ)
WO2004052286A2 (en) 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
US7550470B2 (en) * 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
GB0303910D0 (en) 2003-02-20 2003-03-26 Merck Sharp & Dohme Therapeutic agents
US20070037150A1 (en) 2003-02-21 2007-02-15 The Johns Hopkins University Tyrosine kinome
JP2004277337A (ja) * 2003-03-14 2004-10-07 Sumitomo Pharmaceut Co Ltd ピラゾロ[1,5−a]ピリミジン誘導体
WO2004087707A1 (en) 2003-03-31 2004-10-14 Vernalis (Cambridge) Limited Pyrazolopyrimidine compounds and their use in medicine
US20060094699A1 (en) 2003-04-11 2006-05-04 Kampen Gita Camilla T Combination therapy using an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist to minimize the side effects associated with glucocorticoid receptor agonist therapy
WO2004089415A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S COMBINATIONS OF AN 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITOR AND A GLUCOCORTICOID RECEPTOR AGONIST
WO2004089471A2 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S NEW PYRAZOLO[1,5-a] PYRIMIDINES DERIVATIVES AND PHARMACEUTICAL USE THEREOF
CA2523508A1 (en) 2003-04-28 2004-11-11 Galpharma Co., Ltd. Galectin 9-inducing factors
PA8603801A1 (es) * 2003-05-27 2004-12-16 Janssen Pharmaceutica Nv Derivados de la quinazolina
JP2005008581A (ja) 2003-06-20 2005-01-13 Kissei Pharmaceut Co Ltd 新規なピラゾロ[1,5−a]ピリミジン誘導体、それを含有する医薬組成物およびそれらの用途
DK1648509T3 (da) 2003-07-15 2013-01-07 Amgen Inc Humane anti-NGF-neutraliserende antistoffer som selektive NGF-pathway-inhibitorer
ES2361997T3 (es) * 2003-09-22 2011-06-27 Boehringer Ingelheim International Gmbh Péptidos macrocíclicos activos contra el virus de la hepatitis c.
US7491794B2 (en) * 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
US20090143399A1 (en) 2003-10-14 2009-06-04 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein Kinase Inhibitors
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
BRPI0416801A (pt) 2003-11-21 2007-01-09 Novartis Ag derivados de 1h-imidazoquinolina como inibidores de proteìna sinase
RU2006122853A (ru) 2003-11-28 2008-01-10 Новартис АГ (CH) Производные диарилмочевины для лечения заболеваний, зависимых от протеинкиназы
UA83881C2 (en) * 2003-12-18 2008-08-26 Янссен Фармацевтика Н.В. Pyrido- and pyrimidopyrimidine derivatives as anti-proliferative agents
US7504509B2 (en) 2003-12-19 2009-03-17 Plexxikon, Inc. Compounds and methods for development of Ret modulators
GB0330042D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions them
GB0330043D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions comprising them
PE20051089A1 (es) 2004-01-22 2006-01-25 Novartis Ag Derivados de pirazolo [1,5-a] pirimidin-7-il-amina como inhibidores de quinasa de proteina
US20050222171A1 (en) 2004-01-22 2005-10-06 Guido Bold Organic compounds
WO2005099363A2 (en) 2004-03-26 2005-10-27 Whitehead Institute For Biomedical Research Methods of diagnosing, preventing and treating cancer metastasis
CN1938311A (zh) 2004-03-30 2007-03-28 因特蒙公司 作为病毒复制抑制剂的大环化合物
WO2006001310A1 (ja) 2004-06-25 2006-01-05 Mitsubishi Materials Corporation 金属コロイド粒子、金属コロイド、及び金属コロイドの用途
MX2007001399A (es) 2004-08-02 2007-04-18 Osi Pharm Inc Compuestos que inhiben pirrolopirimidina multi-cinasa aril-amino sustituidas.
PE20060664A1 (es) 2004-09-15 2006-08-04 Novartis Ag Amidas biciclicas como inhibidores de cinasa
WO2007011410A1 (en) 2004-10-29 2007-01-25 North Carolina State University Production of an asporogenic strain of bacillus licheniformis and its use for the production of keratinase
WO2006050076A1 (en) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
US7452847B2 (en) 2004-11-02 2008-11-18 Ricoh Company, Ltd. Reversible thermosensitive recording medium, reversible thermosensitive recording label, reversible thermosensitive recording device, image processing apparatus, and image processing method
DK1812440T3 (da) 2004-11-04 2011-01-31 Vertex Pharma Pyrazolo[1,5-a]pyrimidiner, der kan anvendes som inhibistorer af proteinkinaser
JO3088B1 (ar) * 2004-12-08 2017-03-15 Janssen Pharmaceutica Nv مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف
DE102005003687A1 (de) 2005-01-26 2006-07-27 Sphingo Tec Gmbh Immunoassay zur Bestimmung der Freisetzung von Neurotensin in die Zirkulation
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
SI1853602T1 (sl) 2005-02-16 2010-11-30 Astrazeneca Ab Kemične spojine
CN101119996A (zh) 2005-02-16 2008-02-06 阿斯利康(瑞典)有限公司 化学化合物
WO2006089298A2 (en) 2005-02-18 2006-08-24 Attenuon, Llc Pyrimidine-fused diazepine derivatives and indole-fused pteridines
DK1869049T3 (da) * 2005-03-21 2009-05-18 Lilly Co Eli Imidazopyridazinforbindelser
GB0507575D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
WO2006113509A2 (en) 2005-04-15 2006-10-26 Cylene Pharmaceuticals, Inc. Quinobenzoxazine analogs and methods of using thereof
CN101208093A (zh) 2005-04-27 2008-06-25 阿斯利康(瑞典)有限公司 吡唑-嘧啶衍生物在治疗疼痛中的用途
JP2008540622A (ja) 2005-05-16 2008-11-20 アストラゼネカ アクチボラグ 化合物
US20100047777A1 (en) 2005-05-26 2010-02-25 The Johns Hopkins University Methods for identifying mutations in coding and non-coding dna
EP1896462A2 (en) 2005-05-31 2008-03-12 The Pfahl Family Trust (Dated 9 July 1996) Substituted biarylheterocycle derivatives as protein kinase inhibitors for the treatment of cancer and other diseases
US7541367B2 (en) 2005-05-31 2009-06-02 Janssen Pharmaceutica, N.V. 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders
CN100406650C (zh) 2005-06-05 2008-07-30 徐斌 一种抗特大变位的模块式梳型桥梁伸缩缝装置
ITRM20050290A1 (it) 2005-06-07 2006-12-08 Lay Line Genomics Spa Uso di molecole in grado di inibire il legame tra ngf e il suo recettore trka come analgesici ad effetto prolungato.
TWI473808B (zh) 2005-06-22 2015-02-21 Plexxikon Inc 用於激酶調節的化合物及方法及其適應症
US20070025540A1 (en) 2005-07-07 2007-02-01 Roger Travis Call center routing based on talkativeness
GB0515026D0 (en) 2005-07-21 2005-08-31 Novartis Ag Organic compounds
GEP20105124B (en) * 2005-07-25 2010-11-25 Array Biopharma Inc Novel macrocyclic inhibitors of hepatitis c virus replication
EP1910369A1 (en) 2005-07-29 2008-04-16 Astellas Pharma Inc. Fused heterocycles as lck inhibitors
JP2009503071A (ja) 2005-08-03 2009-01-29 イーストマン ケミカル カンパニー トコフェリルポリエチレングリコールスクシネート粉末及びその製造方法
WO2007024680A1 (en) 2005-08-22 2007-03-01 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
EA017318B1 (ru) 2005-08-25 2012-11-30 Креабилис Терапеутикс С.П.А. Полимерные конъюгаты индолокарбазола и его производных
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
DE102005042742A1 (de) 2005-09-02 2007-03-08 Schering Ag Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
US20070078136A1 (en) 2005-09-22 2007-04-05 Bristol-Myers Squibb Company Fused heterocyclic compounds useful as kinase modulators
JP5102212B2 (ja) 2005-10-06 2012-12-19 メルク・シャープ・アンド・ドーム・コーポレーション プロテインキナーゼインヒビターとしてのピラゾロピリミジン
WO2007044441A2 (en) 2005-10-06 2007-04-19 Schering Corporation Use of pyrazolo [1 , 5 -a] pyrimidine derivatives for inhibiting protein kinases methods for inhibiting protein kinases
BRPI0617274A2 (pt) * 2005-10-11 2011-07-19 Intermune Inc compostos e métodos para a inibição de replicação viral de hepatite c
CA2624772C (en) 2005-10-11 2011-11-29 Centre National De La Recherche Scientifique (Cnrs) Compounds and kits for the detection and the quantification of cell apoptosis
ATE517874T1 (de) 2005-10-21 2011-08-15 Exelixis Inc Pyrimidinone als modulatoren von caseinkinase ii (ck2)
EP1948647A1 (en) 2005-11-03 2008-07-30 SGX Pharmaceuticals, Inc. Pyrimidinyl-thiophene kinase modulators
US20070149523A1 (en) 2005-11-14 2007-06-28 Jan Ehlert Thiazole Analogues and Uses Thereof
EP1785420A1 (en) 2005-11-14 2007-05-16 4Sc Ag Thiazole analogues and uses thereof
WO2007057397A1 (en) 2005-11-15 2007-05-24 Boehringer Ingelheim International Gmbh Treatment of cancer
GB0524436D0 (en) 2005-11-30 2006-01-11 Novartis Ag Organic compounds
RU2008127263A (ru) 2005-12-08 2010-01-20 Новартис АГ (CH) ПИРАЗОЛ [1,5-a] ПИРИДИН-3-КАРБОНОВЫЕ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ EphB-И VEGFR2-КИНАЗЫ
WO2007084815A2 (en) 2006-01-19 2007-07-26 Janssen Pharmaceutica, N.V. Substituted thienopyrimidine kinase inhibitors
BRPI0707312B1 (pt) 2006-01-27 2022-06-07 Shanghai Hengrui Pharmacetical Co., Ltd Inibidores de pirrolo [3,2-c] piridina-4-ona 2-indolinona proteína cinase, seu uso e seu processo de fabricação, intermediário e seus processos de fabricação, composição farmacêutica e seu uso
KR100846988B1 (ko) 2006-03-06 2008-07-16 제일약품주식회사 신규한 티에노피리미딘 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 함유하는 약학조성물
WO2007103308A2 (en) 2006-03-07 2007-09-13 Array Biopharma Inc. Heterobicyclic pyrazole compounds and methods of use
EP2001864A1 (en) 2006-03-16 2008-12-17 Novartis Pharma AG Heterocyclic organic compounds for the treatment of in particular melanoma
TWI409267B (zh) 2006-03-17 2013-09-21 Ambit Biosciences Corp 治療疾病用之咪唑并噻唑化合物
GB0606805D0 (en) 2006-04-04 2006-05-17 Novartis Ag Organic compounds
BRPI0710874A2 (pt) 2006-04-26 2012-02-14 Hoffmann La Roche compostos de tienopirimidina, processos de produção dos referidos compostos, composições farmacêuticas contendo os mesmos, kit, produto, e usos dos compostos
WO2007136465A2 (en) 2006-05-15 2007-11-29 Irm Llc Compositions and methods for fgf receptor kinases inhibitors
US7389632B2 (en) 2006-06-10 2008-06-24 Uhlmann Pac-Systeme Gmbh & Co. Kg Apparatus for distributing small objects in a fill station
EP1873157A1 (en) * 2006-06-21 2008-01-02 Bayer Schering Pharma Aktiengesellschaft Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
TWI419889B (zh) 2006-07-05 2013-12-21 Mitsubishi Tanabe Pharma Corp 吡唑并〔1,5-a〕嘧啶化合物
EP2058309A4 (en) 2006-08-04 2010-12-22 Takeda Pharmaceutical CONDENSED HETEROCYCLIC COMPOUND
US7531539B2 (en) 2006-08-09 2009-05-12 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US8063225B2 (en) 2006-08-14 2011-11-22 Chembridge Corporation Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders
CA2663091A1 (en) 2006-09-07 2008-03-13 Biogen Idec Ma Inc. Modulators of interleukin-1 receptor-associated kinase
EP2067039A2 (en) 2006-09-12 2009-06-10 Novartis Forschungsstiftung, Zweigniederlassung Friedrich Miescher Institute for Biomedical Research Non-neuroendocrine cancer therapy
JP5568304B2 (ja) 2006-09-15 2014-08-06 タイロジェネクス,インコーポレイテッド キナーゼ阻害剤化合物
AU2007302263A1 (en) 2006-09-29 2008-04-03 Novartis Ag Pyrazolopyrimidines as P13K lipid kinase inhibitors
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
EP1918291A1 (en) 2006-10-30 2008-05-07 Novartis AG 3-Aminocarbonyl-substituted fused pyrazolo-derivatives as protein kinase modulators
WO2008052734A1 (en) 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents
MY146474A (en) 2006-11-06 2012-08-15 Supergen Inc Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
WO2008058341A1 (en) 2006-11-15 2008-05-22 Cytopia Research Pty Ltd Inhibitors of kinase activity
US20080199426A1 (en) 2007-01-11 2008-08-21 Sukhatme Vikas P Methods and compositions for the treatment and diagnosis of vascular inflammatory disorders or endothelial cell disorders
US20100173954A1 (en) 2007-01-19 2010-07-08 Bayer Healthcare Llc Treatment of cancers having resistance to chemotherapeutic agents
KR20090110314A (ko) * 2007-02-08 2009-10-21 티보텍 파마슈티칼즈 리미티드 피리미딘 치환된 마크로사이클릭 hcv 억제제
US20080234267A1 (en) 2007-03-20 2008-09-25 Karen Elizabeth Lackey Compounds and Methods of Treatment
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
US20080255153A1 (en) 2007-03-28 2008-10-16 Biovitrum Ab (Publ) New compounds
HRP20130660T1 (en) 2007-04-03 2013-08-31 Array Biopharma, Inc. Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
US20110189167A1 (en) 2007-04-20 2011-08-04 Flynn Daniel L Methods and Compositions for the Treatment of Myeloproliferative Diseases and other Proliferative Diseases
AU2008247442B2 (en) 2007-05-04 2013-01-10 Irm Llc Compounds and compositions as c-kit and PDGFR kinase inhibitors
WO2008138184A1 (fr) 2007-05-14 2008-11-20 Shanghai Hengrui Pharmaceutical Co.Ltd. Dérivés de pyrrolo-azacycles, leur procédé de fabrication et leur utilisation en tant qu'inhibiteurs de protéine kinases
ES2435454T3 (es) * 2007-06-21 2013-12-19 Janssen Pharmaceutica, N.V. Indolin-2-onas y aza-indolin-2-onas
WO2009003136A1 (en) 2007-06-26 2008-12-31 Rigel Pharmaceuticals, Inc. Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders
WO2009012262A1 (en) 2007-07-16 2009-01-22 The Regents Of The University Of California Protein kinase modulating compounds and methods for making and using them
PH12013501594A1 (en) 2007-07-20 2014-05-12 Nerviano Medical Sciences Srl Substituted indazole derivatives active as kinase inhibitors
DK2185698T3 (en) 2007-08-07 2015-07-27 Purdue Research Foundation Kinase Inhibitors and Uses thereof
BRPI0815370B8 (pt) 2007-08-10 2021-05-25 Regeneron Pharma anticorpos humanos de alta afinidade contra o fator de crescimento neural humano e seu uso, molécula de ácido nucleico, vetor de expressão, método para produção de um anticorpo anti-ngf humano e composiçao farmacêutica
EP2025678A1 (en) 2007-08-17 2009-02-18 Oncalis AG Pyrazolo[3,4-d]pyrimidine compounds and their use as modulators of protein kinase
WO2009042646A1 (en) 2007-09-24 2009-04-02 Curis, Inc. Anti-proliferative agents
MX2010004260A (es) 2007-10-16 2010-04-30 Wyeth Llc Compuestos de tienopirimidina y pirazolopirimidina y su uso como inhibidores de mtor cinasa y pi3 cinasa.
KR20100089851A (ko) 2007-10-23 2010-08-12 노파르티스 아게 호흡기 질환의 치료를 위한 trkb 항체의 용도
US20110046127A1 (en) 2007-11-08 2011-02-24 Paolo Pevarello Imidazopyridazines for Use as Protein Kinase Inhibitors
JP2011504931A (ja) 2007-11-28 2011-02-17 シェーリング コーポレイション プロテインキナーゼ阻害剤としての2−フルオロピラゾロ[1,5−a]ピリミジン
JP5420568B2 (ja) 2008-01-17 2014-02-19 アイアールエム・リミテッド・ライアビリティ・カンパニー 改良された抗TrkB抗体
TW200942537A (en) 2008-02-01 2009-10-16 Irm Llc Compounds and compositions as kinase inhibitors
WO2009103076A1 (en) 2008-02-15 2009-08-20 Oxigene, Inc. Methods and compositions for enhancing the efficacy of rtk inhibitors
AU2009226153B2 (en) 2008-03-19 2014-02-20 Chembridge Corporation Novel tyrosine kinase inhibitors
AU2009246687B2 (en) 2008-05-13 2012-08-09 Irm Llc Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors
US20110212053A1 (en) 2008-06-19 2011-09-01 Dapeng Qian Phosphatidylinositol 3 kinase inhibitors
WO2010006432A1 (en) 2008-07-14 2010-01-21 Queen's University At Kingston Pharmaceutical compositions comprising ret inhibitors and methods for the treatment of cancer
US8946226B2 (en) 2008-07-29 2015-02-03 Nerviano Medical Sciences S.R.L. Use of CDK inhibitor for the treatment of glioma
US20100075916A1 (en) 2008-09-05 2010-03-25 Auspex Pharmaceuticals, Inc. Substituted quinazoline inhibitors of growth factor receptor tyrosine kinases
EP2161271A1 (en) 2008-09-08 2010-03-10 Università Degli Studi Di Milano - Bicocca Alpha-carboline inhibitors of NMP-ALK, RET, and Bcr-Abl
US8450322B2 (en) 2008-09-22 2013-05-28 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as Trk kinase inhibitors
KR101718386B1 (ko) 2008-09-26 2017-03-21 내셔날 헬스 리서치 인스티튜트 단백질 키나아제 억제제로서의 융합 다환 화합물
TR201807039T4 (tr) 2008-10-22 2018-06-21 Array Biopharma Inc Trk kinaz inhibitörleri olarak sübstitüe edilmiş pirazolo[1,5-]pirimidin bileşikleri.
JP5769199B2 (ja) 2008-10-31 2015-08-26 ジェネンテック, インコーポレイテッド ピラゾロピリミジンjak阻害剤化合物と方法
WO2010054058A1 (en) 2008-11-06 2010-05-14 Ambit Bioscience Corporation Imidazolothiazole compounds as modulators of protein kinase
JP2012509859A (ja) 2008-11-24 2012-04-26 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 中皮腫の治療のためのcdk阻害物質
KR101061599B1 (ko) 2008-12-05 2011-09-02 한국과학기술연구원 비정상 세포 성장 질환의 치료를 위한 단백질 키나아제 저해제인 신규 인다졸 유도체, 이의 약학적으로 허용가능한염 및 이를 유효성분으로 함유하는 약학적 조성물
DK2881402T3 (en) 2009-02-12 2017-08-28 Cell Signaling Technology Inc Mutant ROS expression in human liver cancer
US8492374B2 (en) 2009-04-29 2013-07-23 Industrial Technology Research Institute Azaazulene compounds
EP2428508B9 (en) 2009-05-08 2016-04-20 Astellas Pharma Inc. Diamino heterocyclic carboxamide compound
JP6073677B2 (ja) 2009-06-12 2017-02-01 デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド 縮合複素環式化合物およびそれらの使用
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
KR101256018B1 (ko) 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
KR101147550B1 (ko) 2009-10-22 2012-05-17 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노[3,2-d]피리미딘 화합물
KR101116756B1 (ko) 2009-10-27 2012-03-13 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 신규의 1,6-치환된 인돌 화합물
KR101690358B1 (ko) 2009-10-29 2017-01-09 제노스코 키나아제 억제제
KR101663637B1 (ko) 2009-11-13 2016-10-07 제노스코 키나아제 억제제
KR101094446B1 (ko) 2009-11-19 2011-12-15 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노[3,2-d]피리미딘 화합물
EP2519517B1 (en) 2009-12-29 2015-03-25 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
KR101483215B1 (ko) 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
CA2786438C (en) 2010-01-29 2015-10-13 Hanmi Science Co., Ltd. Thieno[3,2-d]pyrimidine derivatives having inhibitory activity on protein kinases
DK2536414T3 (en) 2010-02-18 2016-10-03 Inserm (Institut Nat De La Santé Et De La Rech Médicale) METHOD FOR PREVENTING cancer metastasis
WO2011127219A1 (en) 2010-04-06 2011-10-13 Caris Life Sciences Luxembourg Holdings Circulating biomarkers for disease
US8383793B2 (en) 2010-04-15 2013-02-26 St. Jude Children's Research Hospital Methods and compositions for the diagnosis and treatment of cancer resistant to anaplastic lymphoma kinase (ALK) kinase inhibitors
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
US8543395B2 (en) 2010-05-18 2013-09-24 Shazam Entertainment Ltd. Methods and systems for performing synchronization of audio with corresponding textual transcriptions and determining confidence values of the synchronization
ES2628418T3 (es) 2010-05-20 2017-08-02 Array Biopharma, Inc. Compuestos macrocíclicos como inhibidores de la TRK cinasa
JP6121903B2 (ja) 2010-08-19 2017-04-26 ゾエティス・ベルジャム・エス・アー 抗ngf抗体およびその使用
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
WO2012037155A2 (en) 2010-09-13 2012-03-22 Gtx, Inc. Tyrosine kinase inhibitors
WO2012047017A2 (ko) 2010-10-05 2012-04-12 크리스탈지노믹스(주) 2,3-디히드로-이소인돌-1-온 유도체 및 이를 포함하는 조성물
MX359070B (es) 2010-12-01 2018-09-13 Alderbio Holdings Llc Composiciones anti-ngf y uso de las mismas.
US8618146B2 (en) 2011-01-03 2013-12-31 Dr. Reddy's Laboratories Limited Epothilone compound formulations
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
CA2828219A1 (en) 2011-02-25 2012-08-30 Irm Llc Pyrazolo [1,5-a] pyridines as trk inhibitors
US8791112B2 (en) 2011-03-30 2014-07-29 Arrien Pharmaceuticals Llc Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3, 4-B] pyridine and pyrazolo [3, 4-B] pyridine derivatives as protein kinase inhibitors
JP6118794B2 (ja) 2011-04-01 2017-04-19 ザ ユニバーシティ オブ ユタ リサーチ ファウンデイション Axlキナーゼの阻害剤としての置換n−フェニルピリミジン−2−アミン類似体
SG10201913053QA (en) 2011-05-13 2020-03-30 Array Biopharma Inc Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors
RU2477723C2 (ru) 2011-06-16 2013-03-20 Общество С Ограниченной Ответственностью "Фьюжн Фарма" Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе
WO2013016720A2 (en) 2011-07-28 2013-01-31 Gerinda Therapeutics, Inc. Novel substituted biarylheterocycle derivatives as protein kinase inhibitors for the treatment of cancer and other diseases
KR20140047138A (ko) 2011-08-04 2014-04-21 도쿠리츠교세이호진 고쿠리츠간켄큐센터 Kif5b 유전자와 ret 유전자와의 융합 유전자, 및 당해 융합 유전자를 표적으로 한 암 치료의 유효성을 판정하는 방법
BR112014004213A2 (pt) 2011-08-23 2017-06-20 Found Medicine Inc novas moléculas de fusão kif5b-ret e usos das mesmas
WO2013077921A2 (en) 2011-09-02 2013-05-30 The Regents Of The University Of California Substituted pyrazolo[3,4-d]pyrimidines and uses thereof
WO2013036232A2 (en) 2011-09-08 2013-03-14 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
WO2013042137A1 (en) 2011-09-19 2013-03-28 Aurigene Discovery Technologies Limited Bicyclic heterocycles as irak4 inhibitors
CN102408411B (zh) 2011-09-19 2014-10-22 北京康辰药业股份有限公司 一种含喹啉基的羟肟酸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
WO2013059740A1 (en) 2011-10-21 2013-04-25 Foundation Medicine, Inc. Novel alk and ntrk1 fusion molecules and uses thereof
JP2014533286A (ja) 2011-11-14 2014-12-11 テサロ, インコーポレイテッド 特定のチロシンキナーゼの調節
US9045478B2 (en) 2011-12-12 2015-06-02 Dr. Reddy's Laboratories Ltd. Substituted pyrazolo[1,5-a] pyridine as tropomyosin receptor kinase (Trk) inhibitors
EP2797927B1 (en) 2011-12-30 2019-09-25 Hanmi Pharm. Co., Ltd. THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES
JP2015109806A (ja) 2012-03-22 2015-06-18 アステラス製薬株式会社 新規ret融合体の検出法
US9242977B2 (en) 2012-04-26 2016-01-26 Ono Pharmaceutical Co., Ltd. Trk-inhibiting compound
US20150099721A1 (en) 2012-05-10 2015-04-09 Synta Pharmaceuticals Corp. Treating cancer with hsp90 inhibitory compounds
ES2751944T3 (es) 2012-05-23 2020-04-02 Nerviano Medical Sciences Srl Proceso para la preparación de N-[5-(3,5-difluoro-bencil)-1H-indazol-3-il]-4-(4-metil-piperazin-1-il)-2-(tetrahidro-piran-4-ilamino)-benzamida
TWI585088B (zh) 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并[1,2-b]嗒衍生物
JPWO2014017491A1 (ja) 2012-07-26 2016-07-11 国立研究開発法人国立がん研究センター Cep55遺伝子とret遺伝子との融合遺伝子
EP2689778A1 (en) 2012-07-27 2014-01-29 Pierre Fabre Medicament Derivatives of azaindoles or diazaindoles for treating pain
US20150218652A1 (en) 2012-08-31 2015-08-06 The Regents Of The Unversity Of Colorado, A Body Corporate Methods for diagnosis and treatment of cancer
US20150238477A1 (en) 2012-09-07 2015-08-27 Exelixis, Inc. Method of Treating Lung Adenocarcinoma
US20140084039A1 (en) 2012-09-24 2014-03-27 Electro Scientific Industries, Inc. Method and apparatus for separating workpieces
SG11201502211QA (en) 2012-09-25 2015-05-28 Chugai Pharmaceutical Co Ltd Ret inhibitor
JP2014082984A (ja) 2012-10-23 2014-05-12 Astellas Pharma Inc 新規ntrk2活性化変異の検出法
WO2014072220A1 (en) 2012-11-07 2014-05-15 Nerviano Medical Sciences S.R.L. Substituted pyrimidinyl and pyridinyl-pyrrolopyridinones, process for their preparation and their use as kinase inhibitors
EP2917183A1 (en) 2012-11-12 2015-09-16 Ignyta, Inc. Bendamustine derivatives and methods of using same
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
WO2014078331A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078408A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
SMT201800169T1 (it) 2012-11-13 2018-05-02 Array Biopharma Inc Composti di n-pirrolidinile, n'-pirazolile-urea, tiourea, guanidina e cianoguanidina come inibitore di chinasi trka
WO2014078328A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078325A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
RS55593B1 (sr) 2012-11-13 2017-06-30 Array Biopharma Inc Jedinjenja biciklične uree, tiouree, guanidina i cijanoguanidina korisna za lečenje bola
HK1213189A1 (zh) 2012-11-29 2016-06-30 耶达研究及发展有限公司 预防肿瘤转移、癌症治疗和预後及鉴定为推定转移抑制剂的试剂的方法
WO2014086284A1 (zh) 2012-12-04 2014-06-12 上海医药集团股份有限公司 一类氘代3-氰基喹啉类化合物、其药用组合物、制备方法及其用途
FR3000492B1 (fr) 2012-12-28 2015-09-11 Oribase Pharma Nouveaux derives azaindole en tant qu'inhibiteurs multikinases
FR3000494B1 (fr) 2012-12-28 2015-08-21 Oribase Pharma Nouveaux derives d'azaindoles en tant qu'inhibiteurs de proteines kinases
EP2940014B1 (en) 2012-12-28 2018-09-26 Crystalgenomics, Inc. 2,3-dihydro-isoindole-1-on derivative as btk kinase suppressant, and pharmaceutical composition including same
FR3000493A1 (fr) 2012-12-28 2014-07-04 Oribase Pharma Nouveaux inhibiteurs de proteines kinases
US9127055B2 (en) 2013-02-08 2015-09-08 Astellas Pharma Inc. Method of treating pain with anti-human NGF antibody
MX353336B (es) 2013-02-19 2018-01-09 Ono Pharmaceutical Co Compuesto inhibidor de cinasa del receptor de tropomiosina (trk).
WO2014130975A1 (en) 2013-02-22 2014-08-28 Bastian Boris C Fusion polynucleotides and fusion polypeptides associated with cancer and particularly melanoma and their uses as therapeutic and diagnostic targets
US20140243332A1 (en) 2013-02-27 2014-08-28 Oregon Health & Science University Methods of treating cancers characterized by aberrent ros1 activity
PT2970191T (pt) 2013-03-15 2017-03-23 Glaxosmithkline Ip Dev Ltd Derivados de piridina como inibidores da quinase rearranjada durante transfecção(ret)
US8937071B2 (en) 2013-03-15 2015-01-20 Glaxosmithkline Intellectual Property Development Limited Compounds as rearranged during transfection (RET) inhibitors
WO2014152777A2 (en) 2013-03-15 2014-09-25 Insight Genetics, Inc. Methods and compositions for the diagnosis and treatment of cancers resistant to ros1 inhibitors
CN105518151B (zh) 2013-03-15 2021-05-25 莱兰斯坦福初级大学评议会 循环核酸肿瘤标志物的鉴别和用途
WO2014151734A1 (en) 2013-03-15 2014-09-25 The Trustees Of Columbia University In The City Of New York Fusion proteins and methods thereof
EP2986736B1 (en) 2013-04-17 2019-09-18 Life Technologies Corporation Gene fusions and gene variants associated with cancer
JP6510510B2 (ja) 2013-07-11 2019-05-08 ベータ ファーマシューティカルズ カンパニー リミテッド プロテインチロシンキナーゼモジュレーター及び使用方法
JP6534930B2 (ja) 2013-07-26 2019-06-26 公益財団法人がん研究会 Ntrk3融合体の検出法
EP3628749A1 (en) 2013-07-30 2020-04-01 Blueprint Medicines Corporation Ntrk2 fusions
WO2015025866A1 (ja) 2013-08-20 2015-02-26 独立行政法人国立がん研究センター 肺がんで見出された新規融合遺伝子
KR20160055170A (ko) 2013-08-30 2016-05-17 암비트 바이오사이언시즈 코포레이션 바이아릴 아세트아미드 화합물 및 이의 사용 방법
MX2016004678A (es) 2013-10-24 2017-03-10 Univ Georgetown Composiciones para el tratamiento del cancer.
JPWO2015064621A1 (ja) 2013-10-29 2017-03-09 公益財団法人がん研究会 新規融合体及びその検出法
ES2734213T3 (es) 2013-11-27 2019-12-04 Enplas Corp Emisor y tubo para riego por goteo
GB201321146D0 (en) 2013-11-29 2014-01-15 Cancer Rec Tech Ltd Quinazoline compounds
WO2015082887A2 (en) 2013-12-02 2015-06-11 Bergenbio As Use of kinase inhibitors
LT3636649T (lt) 2014-01-24 2024-04-10 Turning Point Therapeutics, Inc. Diarilo makrociklai kaip proteinkinazių moduliatoriai
CA2934043C (en) 2014-02-05 2019-03-12 VM Oncology LLC Trka receptor tyrosine kinase antagonists and uses thereof
MX384828B (es) 2014-02-14 2025-03-14 Exelixis Inc Formas solidas cristalinas de n-{4-[(6,7-dimetoxiquinolin-4-il)oxi]fenil}-n'-(4-fluorofenil)ciclopropan-1,1-dicarboxamida, procesos para elaboracion y metodos de uso.
TWI672141B (zh) 2014-02-20 2019-09-21 美商醫科泰生技 投予ros1突變癌細胞之分子
EP3154959B1 (en) 2014-05-15 2019-07-10 Array Biopharma, Inc. 1-((3s,4r)-4-(3-fluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(4-methyl-3-(2-methylpyrimidin-5-yl)-1-phenyl-1h-pyrazol-5-yl)urea as a trka kinase inhibitor
WO2015183837A1 (en) 2014-05-27 2015-12-03 Brian Haynes Compositions, methods, and uses related to ntrk2-tert fusions
US20170114415A1 (en) 2014-05-30 2017-04-27 The Regents Of The University Of Colorado, A Body Corporate Activating ntrk1 gene fusions predictive of kinase inhibitor therapy
CN105222097A (zh) 2014-06-26 2016-01-06 欧普照明股份有限公司 一种灯具及其光学模组
US10065934B2 (en) 2014-07-17 2018-09-04 Sunshine Lake Pharma Co., Ltd. Substituted urea derivatives and pharmaceutical uses thereof
KR20170042614A (ko) 2014-08-01 2017-04-19 파마싸이클릭스 엘엘씨 Btk 저해제를 이용한 치료에 대한 dlbcl의 반응을 예측하기 위한 바이오마커
AU2015304438B2 (en) 2014-08-18 2019-06-20 Ono Pharmaceutical Co., Ltd. Acid-addition salt of Trk-inhibiting compound
US20170283404A1 (en) 2014-09-08 2017-10-05 Glaxosmithkline Intellectual Property Development Limited Crystalline forms of 2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-n-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamide
PT3191450T (pt) 2014-09-10 2019-05-29 Glaxosmithkline Ip Dev Ltd Derivados de piridona como inibidores da quinase rearranjada durante a transfecção (ret)
EA032030B1 (ru) 2014-09-10 2019-03-29 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Соединения в качестве ингибиторов реаранжированной во время трансфекции (ret) киназы
TWI538914B (zh) 2014-10-03 2016-06-21 國立交通大學 蛋白質激酶之選擇性抑制劑、其醫藥組成物及其用途
EP3206711B1 (en) 2014-10-14 2023-05-31 Novartis AG Antibody molecules to pd-l1 and uses thereof
PT3699181T (pt) 2014-11-16 2023-04-05 Array Biopharma Inc Forma cristalina de hidrogenossulfato de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
HRP20240937T1 (hr) 2014-12-15 2024-10-25 Cmg Pharmaceutical Co., Ltd. Heteroaril spoj sa kondeziranim prstenom i njihova primjena kao trk inhibitora
WO2016096709A1 (en) 2014-12-16 2016-06-23 Eudendron S.R.L. Heterocyclic derivatives modulating activity of certain protein kinases
WO2016127074A1 (en) 2015-02-06 2016-08-11 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors
KR101675984B1 (ko) 2015-02-23 2016-11-14 한양대학교 에리카산학협력단 티에노디아제핀 유도체 또는 이의 약학적으로 허용가능한 염, 및 이를 유효성분으로 포함하는 약학적 조성물
CA2978628A1 (en) 2015-03-03 2016-09-09 Caris Mpi, Inc. Molecular profiling for cancer
WO2016149261A1 (en) 2015-03-16 2016-09-22 Personal Genome Diagnostics, Inc. Systems and methods for analyzing nucleic acid
CN108137593B (zh) 2015-04-21 2021-01-05 上海交通大学医学院附属瑞金医院 蛋白激酶抑制剂的制备和用途
CN108025048B (zh) 2015-05-20 2022-10-25 博德研究所 共有的新抗原
US20180177792A1 (en) 2015-05-29 2018-06-28 Ignyta, Inc. Compositions and methods for treating patients with rtk mutant cells
TN2017000502A1 (en) 2015-06-01 2019-04-12 Loxo Oncology Inc Methods of diagnosing and treating cancer
AU2015101722A4 (en) 2015-06-19 2016-05-19 Macau University Of Science And Technology Oncogenic ros1 and alk kinase inhibitor
US9782400B2 (en) 2015-06-19 2017-10-10 Macau University Of Science And Technology Oncogenic ROS1 and ALK kinase inhibitor
GB201511546D0 (en) 2015-07-01 2015-08-12 Immatics Biotechnologies Gmbh Novel peptides and combination of peptides for use in immunotherapy against ovarian cancer and other cancers
US10316044B2 (en) 2015-07-02 2019-06-11 Tp Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
GB201512365D0 (en) 2015-07-15 2015-08-19 King S College London Novel therapy
RS61485B1 (sr) 2015-07-16 2021-03-31 Array Biopharma Inc Supstituisana pirazolo [1,5-a] piridinska jedinjenja kao inhibitori ret kinaze
EP3120851A1 (en) 2015-07-21 2017-01-25 Pangaea Biotech S.L. 4-amino-6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)-pyrido[2,3-d]pyrimidin-7(8h)-one for treatment of solid cancers
KR101766194B1 (ko) 2015-08-07 2017-08-10 한국과학기술연구원 RET 키나아제 저해제인 신규 3-(이속사졸-3-일)-피라졸로[3,4-d]피리미딘-4-아민 화합물
EP3334430B1 (en) 2015-08-13 2025-02-26 San Diego State University Research Foundation Atropisomerism for increased kinase inhibitor selectivity
MA41559A (fr) 2015-09-08 2017-12-26 Taiho Pharmaceutical Co Ltd Composé de pyrimidine condensé ou un sel de celui-ci
WO2017049462A1 (zh) 2015-09-22 2017-03-30 合肥中科普瑞昇生物医药科技有限公司 一类新型的flt3激酶抑制剂及其用途
CN105255927B (zh) 2015-09-30 2018-07-27 温州医科大学附属第一医院 一种kiaa1217-ret融合基因
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
IL302209B2 (en) 2015-11-02 2024-06-01 Blueprint Medicines Corp Inhibitors of ret
US20190002988A1 (en) 2015-12-08 2019-01-03 Boehringer Ingelheim International Gmbh Method of using a ret fusion gene as a biomarker to select non small cell lung cancer (nsclc) and thyroid cancer patients for a cancer treatment
WO2017122815A1 (ja) 2016-01-15 2017-07-20 公益財団法人がん研究会 新規融合体及びその検出法
US20170224662A1 (en) 2016-01-22 2017-08-10 The Medicines Company Aqueous Formulations and Methods of Preparation and Use Thereof
TWI620748B (zh) 2016-02-05 2018-04-11 National Health Research Institutes 氨基噻唑化合物及其用途
WO2017145050A1 (en) 2016-02-23 2017-08-31 Glaxosmithkline Intellectual Property Development Limited Pyridylpyridone derivative useful as a ret kinase inhibitor in the treatment of ibs and cancer
MD3269370T2 (ro) 2016-02-23 2020-05-31 Taiho Pharmaceutical Co Ltd Compus pirimidinic condensat nou sau sare a acestuia
WO2017155018A1 (ja) 2016-03-11 2017-09-14 小野薬品工業株式会社 Trk阻害剤抵抗性の癌治療剤
WO2017161269A1 (en) 2016-03-17 2017-09-21 Blueprint Medicines Corporation Inhibitors of ret receptor tyrosine kinases
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CN109414442B (zh) 2016-04-04 2024-03-29 洛克索肿瘤学股份有限公司 一种化合物的液体制剂
RS62322B1 (sr) 2016-04-15 2021-10-29 Cancer Research Tech Ltd Heterociklična jedinjenja kao inhibitori ret kinaze
LT3442535T (lt) 2016-04-15 2022-10-25 Cancer Research Technology Limited Heterocikliniai junginiai kaip ret kinazės inhibitoriai
EP3445361A1 (en) 2016-04-19 2019-02-27 Exelixis, Inc. Triple negative breast cancer treatment method
WO2017197051A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Amine-linked c3-glutarimide degronimers for target protein degradation
DK3800189T3 (da) 2016-05-18 2023-07-31 Loxo Oncology Inc Fremstilling af (s)-n-(5-((r)-2-(2,5-difluorphenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid
WO2017201156A1 (en) 2016-05-18 2017-11-23 Duke University Method of treating kras wild-type metastatic colorectal cell carcinoma using cabozantinib plus panitumumab
CN109312406A (zh) 2016-06-01 2019-02-05 豪夫迈·罗氏有限公司 预测肺癌患者中对alk抑制剂疗法的响应的间变性淋巴瘤激酶中的新型突变
WO2018017983A1 (en) 2016-07-22 2018-01-25 Blueprint Medicines Corporation Compounds useful for treating disorders related to ret
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
WO2018136796A1 (en) 2017-01-20 2018-07-26 Exelixis, Inc. Combinations of cabozantinib and atezolizumab to treat cancer
CN108456163A (zh) 2017-02-20 2018-08-28 中国科学院上海药物研究所 含邻氨基杂芳环炔基的化合物及其制备方法和用途
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
EP3700576A1 (en) 2017-10-26 2020-09-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor

Also Published As

Publication number Publication date
US20170114059A1 (en) 2017-04-27
US9718822B2 (en) 2017-08-01
DK2918588T3 (en) 2017-08-28
AU2016203348B2 (en) 2018-08-09
CN105693720A (zh) 2016-06-22
DK3205654T3 (en) 2019-04-15
AU2011256380C1 (en) 2016-09-08
US10647730B2 (en) 2020-05-12
EP3521291A1 (en) 2019-08-07
JP5832527B2 (ja) 2015-12-16
SMT201900203T1 (it) 2019-05-10
IL223094A0 (en) 2013-02-03
CN102971322B (zh) 2016-02-17
PT2918588T (pt) 2017-06-29
ES2534335T3 (es) 2015-04-21
SG185644A1 (en) 2012-12-28
KR102132405B1 (ko) 2020-07-09
TW201819388A (zh) 2018-06-01
CA2800079A1 (en) 2011-11-24
AU2018208676A1 (en) 2018-08-09
BR112012029405A2 (pt) 2016-12-06
AU2016203348C1 (en) 2020-11-12
PL2918588T3 (pl) 2017-10-31
BR112012029405B1 (pt) 2021-01-05
CN110003209A (zh) 2019-07-12
LT3205654T (lt) 2019-05-27
MX365251B (es) 2019-05-28
US20130203776A1 (en) 2013-08-08
SMT201700372T1 (it) 2017-09-07
TWI734134B (zh) 2021-07-21
IL257104B (en) 2021-03-25
AU2018208676B2 (en) 2020-07-30
CN102971322A (zh) 2013-03-13
CR20170098A (es) 2017-07-17
NZ604708A (en) 2015-05-29
JP6523356B2 (ja) 2019-05-29
HRP20190559T1 (hr) 2019-06-14
BR122019024201B1 (pt) 2021-08-03
EP2571883B1 (en) 2015-01-07
CO6660502A2 (es) 2013-04-30
PL3205654T3 (pl) 2019-08-30
US8933084B2 (en) 2015-01-13
US9750744B2 (en) 2017-09-05
AU2016203348A1 (en) 2016-06-16
RU2016128920A3 (OSRAM) 2019-12-25
AU2011256380B2 (en) 2016-02-25
SI3205654T1 (sl) 2019-07-31
TW201625640A (zh) 2016-07-16
ES2628418T3 (es) 2017-08-02
AU2020205339A1 (en) 2020-08-06
TWI516493B (zh) 2016-01-11
US9902741B2 (en) 2018-02-27
ME03376B (me) 2020-01-20
CN105693720B (zh) 2019-01-18
EP2918588A1 (en) 2015-09-16
RU2594742C2 (ru) 2016-08-20
MX383400B (es) 2025-03-13
IL223094B (en) 2018-05-31
IL257104A (en) 2018-03-29
HRP20171140T1 (hr) 2017-10-06
JP2015221834A (ja) 2015-12-10
EP2571883A1 (en) 2013-03-27
PH12015500190B1 (en) 2015-10-19
CA2800079C (en) 2020-09-15
SG10201506591TA (en) 2015-09-29
KR101852169B1 (ko) 2018-04-26
TWI667241B (zh) 2019-08-01
MX382699B (es) 2025-03-13
TW201202254A (en) 2012-01-16
SG10201506593XA (en) 2015-10-29
US20200291026A1 (en) 2020-09-17
PT3205654T (pt) 2019-04-22
US20170283435A1 (en) 2017-10-05
KR20130086951A (ko) 2013-08-05
US9840519B2 (en) 2017-12-12
UY33395A (es) 2012-11-30
RU2735545C2 (ru) 2020-11-03
JP2017082018A (ja) 2017-05-18
AR081919A1 (es) 2012-10-31
KR102015402B1 (ko) 2019-08-28
US20170107232A1 (en) 2017-04-20
CY1121688T1 (el) 2020-07-31
HUE044025T2 (hu) 2019-09-30
CN110003209B (zh) 2022-01-25
PH12012502276A1 (en) 2015-04-22
KR20190101498A (ko) 2019-08-30
TW201936197A (zh) 2019-09-16
US20150336970A1 (en) 2015-11-26
BR112012029405A8 (pt) 2019-12-17
MX2012013467A (es) 2013-04-29
HK1215245A1 (en) 2016-08-19
ES2718043T3 (es) 2019-06-27
HK1181756A1 (en) 2013-11-15
LT2918588T (lt) 2017-08-25
RS58537B1 (sr) 2019-04-30
RU2012155278A (ru) 2014-06-27
US20170112842A1 (en) 2017-04-27
MY191934A (en) 2022-07-19
US9493476B2 (en) 2016-11-15
JP6283636B2 (ja) 2018-02-21
AU2011256380A1 (en) 2013-01-10
EP2918588B1 (en) 2017-05-03
CY1119345T1 (el) 2018-02-14
KR20200085364A (ko) 2020-07-14
CL2012003227A1 (es) 2013-02-08
JP2013530142A (ja) 2013-07-25
MX2019006154A (es) 2019-08-21
TWI609019B (zh) 2017-12-21
EP3205654A1 (en) 2017-08-16
KR20180043407A (ko) 2018-04-27
WO2011146336A1 (en) 2011-11-24
RU2016128920A (ru) 2018-12-07
JP2019104756A (ja) 2019-06-27
SI2918588T1 (sl) 2017-09-29
US20190031684A1 (en) 2019-01-31
JP2021054840A (ja) 2021-04-08
PH12015500190A1 (en) 2015-10-19
EP3205654B1 (en) 2019-01-02

Similar Documents

Publication Publication Date Title
HUE035337T2 (en) Macrocyclic compounds as TRK kinase inhibitors
HK1243058A1 (en) Macrocyclic compounds as trk kinase inhibitors
HK1215245B (en) Macrocyclic compounds as trk kinase inhibitors
HK1181756B (en) Macrocyclic compounds as trk kinase inhibitors
RS56275B1 (sr) Makrociklička jedinjenja kao inhibitori trk kinaze