ME03376B - Makrociklička jedinjenja kао inhibiтori trk kinaze - Google Patents

Makrociklička jedinjenja kао inhibiтori trk kinaze

Info

Publication number
ME03376B
ME03376B MEP-2019-96A MEP201996A ME03376B ME 03376 B ME03376 B ME 03376B ME P201996 A MEP201996 A ME P201996A ME 03376 B ME03376 B ME 03376B
Authority
ME
Montenegro
Prior art keywords
kinaze
trk
inhibitors
macrocyclic compounds
macrocyclic
Prior art date
Application number
MEP-2019-96A
Other languages
German (de)
English (en)
French (fr)
Unknown language (me)
Inventor
Steven Wade Andrews
Kevin Ronald Condroski
Julia Haas
Yutong Jiang
Gabrielle R 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 ME03376B publication Critical patent/ME03376B/me

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains four or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against 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)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
MEP-2019-96A 2010-05-20 2011-05-13 Makrociklička jedinjenja kао inhibiтori trk kinaze ME03376B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34676710P 2010-05-20 2010-05-20
US201061426716P 2010-12-23 2010-12-23
EP17163978.4A EP3205654B1 (en) 2010-05-20 2011-05-13 Macrocyclic compounds as trk kinase inhibitors

Publications (1)

Publication Number Publication Date
ME03376B true ME03376B (me) 2020-01-20

Family

ID=44280661

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2019-96A ME03376B (me) 2010-05-20 2011-05-13 Makrociklička jedinjenja kао inhibiтori trk kinaze

Country Status (34)

Country Link
US (8) US8933084B2 (enExample)
EP (4) EP3521291A1 (enExample)
JP (5) JP5832527B2 (enExample)
KR (4) KR101852169B1 (enExample)
CN (3) CN110003209B (enExample)
AR (1) AR081919A1 (enExample)
AU (4) AU2011256380C1 (enExample)
BR (2) BR122019024201B1 (enExample)
CA (1) CA2800079C (enExample)
CL (1) CL2012003227A1 (enExample)
CO (1) CO6660502A2 (enExample)
CR (1) CR20170098A (enExample)
CY (2) CY1119345T1 (enExample)
DK (2) DK2918588T3 (enExample)
ES (3) ES2534335T3 (enExample)
HR (2) HRP20171140T1 (enExample)
HU (2) HUE044025T2 (enExample)
IL (2) IL223094B (enExample)
LT (2) LT3205654T (enExample)
ME (1) ME03376B (enExample)
MX (4) MX383400B (enExample)
MY (1) MY191934A (enExample)
NZ (1) NZ604708A (enExample)
PH (2) PH12012502276A1 (enExample)
PL (2) PL3205654T3 (enExample)
PT (2) PT3205654T (enExample)
RS (1) RS58537B1 (enExample)
RU (2) RU2735545C2 (enExample)
SG (3) SG10201506593XA (enExample)
SI (2) SI3205654T1 (enExample)
SM (2) SMT201900203T1 (enExample)
TW (4) TWI667241B (enExample)
UY (1) UY33395A (enExample)
WO (1) WO2011146336A1 (enExample)

Families Citing this family (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2464461T3 (es) 2008-09-22 2014-06-02 Array Biopharma, Inc. Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa
SG196855A1 (en) 2008-10-22 2014-02-13 Array Biopharma Inc Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
AU2011256380C1 (en) 2010-05-20 2016-09-08 Array Biopharma Inc. Macrocyclic compounds as Trk kinase inhibitors
HRP20161786T1 (hr) 2011-05-13 2017-03-10 Array Biopharma, Inc. Pirolidinil urea, pirolidinil tiourea i pirolidinil gvanidin spojevi kao inhibitori trka kinaze
WO2013132376A1 (en) * 2012-03-06 2013-09-12 Pfizer Inc. Macrocyclic derivatives for the treatment of proliferative diseases
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
UA117573C2 (uk) 2012-11-13 2018-08-27 Ерей Біофарма Інк. Біциклічні сполуки сечовини, тіосечовини, гуанідину й ціаногуанідину, придатні для лікування болю
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl 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
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
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
UA116455C2 (uk) 2012-11-13 2018-03-26 Еррей Біофарма Інк. Сполуки n-піролідинілсечовини, n'-піразолілсечовини, тіосечовини, гуанідину та ціаногуанідину як інгібітори кінази 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
WO2014078372A1 (en) 2012-11-13 2014-05-22 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
PL3097107T3 (pl) * 2014-01-24 2020-01-31 Turning Point Therapeutics, Inc. Diarylowe związki makrocykliczne jako modulatory kinaz białkowych
AU2015240465B2 (en) 2014-04-04 2020-02-27 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
CN109970614B (zh) 2014-05-15 2023-01-13 阵列生物制药公司 作为trka激酶抑制剂的化合物及其用途
TWI688567B (zh) * 2014-09-11 2020-03-21 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
SG11201701936WA (en) * 2014-09-17 2017-04-27 Oncodesign Sa Macrocyclic lrrk2 kinase inhibitors
WO2016042087A1 (en) * 2014-09-17 2016-03-24 Oncodesign S.A. Macrocyclic rip2 kinase inhibitors
EP3699181B1 (en) 2014-11-16 2023-03-01 Array Biopharma, Inc. Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
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
EP4420732A3 (en) * 2014-12-15 2024-11-27 CMG Pharmaceutical Co., Ltd. Fused ring heteroaryl compounds and their use as trk inhibitors
WO2016116900A1 (en) 2015-01-23 2016-07-28 Gvk Biosciences Private Limited Inhibitors of trka kinase
AU2016270803A1 (en) 2015-06-01 2018-01-04 Loxo Oncology, Inc. Methods of diagnosing and treating cancer
AU2016287568B2 (en) * 2015-07-02 2020-08-20 Turning Point Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
HRP20240780T1 (hr) * 2015-07-06 2024-09-13 Turning Point Therapeutics, Inc. Polimorf diaril makrocikla
JP6816100B2 (ja) 2015-07-16 2021-01-20 アレイ バイオファーマ、インコーポレイテッド ＲＥＴキナーゼ阻害物質としての置換ピラゾロ［１，５−ａ］ピリジン化合物
KR102772574B1 (ko) * 2015-07-21 2025-02-24 터닝 포인트 테라퓨틱스, 인크. 키랄 디아릴 매크로사이클 및 이것의 용도
CA2998885C (en) 2015-09-24 2020-09-01 Cyclenium Pharma Inc. Libraries of heteroaryl-containing macrocyclic compounds and methods of making and using the same
US10724102B2 (en) * 2015-10-26 2020-07-28 Loxo Oncology, Inc. Point mutations in TRK inhibitor-resistant cancer and methods relating to the same
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
SG11201808559PA (en) 2016-04-04 2018-10-30 Loxo Oncology Inc Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
PL3439663T3 (pl) 2016-04-04 2024-11-18 Loxo Oncology, Inc. Sposoby leczenia nowotworów wieku dziecięcego
FI3800189T3 (fi) 2016-05-18 2023-07-31 Loxo Oncology Inc (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin valmistaminen
RU2019105587A (ru) * 2016-07-28 2020-08-28 Тёрнинг Поинт Терапьютикс, Инк. Макроциклические ингибиторы киназ
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
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
JOP20190092A1 (ar) * 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
ES2948194T3 (es) 2017-01-18 2023-09-01 Array Biopharma Inc Compuestos de pirazolo[1,5-a]pirazina sustituida como inhibidores de la cinasa RET
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
JP2020524701A (ja) * 2017-06-22 2020-08-20 サイクルニウム ファーマ インコーポレイテッド ピリジン含有大環状化合物ライブラリーならびにその製造および使用方法
JP7224334B2 (ja) 2017-07-28 2023-02-17 ターニング・ポイント・セラピューティクス・インコーポレイテッド 大環式化合物およびその使用
AU2018320021C1 (en) * 2017-08-23 2023-02-23 Centaurus Biopharma Co., Ltd. Macrocycle containing aminopyrazole and pyrimidine and pharmaceutical composition and use thereof
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
TWI812649B (zh) 2017-10-10 2023-08-21 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
WO2019084285A1 (en) 2017-10-26 2019-05-02 Qian Zhao 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
CA3081790C (en) * 2017-11-10 2023-03-07 Angex Pharmaceutical, Inc. Macrocyclic compounds as trk kinase inhibitors and uses thereof
SI3728271T1 (sl) 2017-12-19 2023-01-31 Turning Point Therapeutics, Inc. Makrociklične spojine za zdravljenje bolezni
CN109956957B (zh) * 2017-12-22 2021-11-09 广州白云山医药集团股份有限公司白云山制药总厂 一种咪唑并[1,2-b]哒嗪大环类激酶抑制剂
CN111362949B (zh) 2017-12-22 2021-12-21 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
JP6997876B2 (ja) 2018-01-18 2022-02-04 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置換ピラゾリル［４，３－ｃ］ピリジン化合物
US11603374B2 (en) 2018-01-18 2023-03-14 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
TW201938169A (zh) 2018-01-18 2019-10-01 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[3,4-d]嘧啶化合物
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
TW201932472A (zh) * 2018-01-30 2019-08-16 大陸商上海吉倍生物技術有限公司 具有大環分子結構的化合物及其用途
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
JP7323748B2 (ja) * 2018-02-28 2023-08-09 ナンジン ザイミン ファーマシューティカル カンパニー リミテッド ピラゾロピリミジン誘導体及びその使用
BR112020018444A2 (pt) * 2018-03-14 2020-12-29 Fochon Pharmaceuticals, Ltd. Compostos de (2-azabiciclo[3,1,0]hexan-2-il)pirazolo[1,5-a]pirimidina substituída e imidazo[1,2-b]piridazina como inibidores de trk cinases
MX2020010116A (es) * 2018-03-28 2020-11-06 Fochon Biosciences Ltd Compuestos macrociclicos como inhibidores de quinasas del receptor de tropomiosina (trk).
EP3773725A1 (en) 2018-03-29 2021-02-17 Loxo Oncology Inc. Treatment of trk-associated cancers
EP3770161B1 (en) * 2018-04-16 2022-08-24 Shenzhen TargetRx, Inc. Di(hetero)aryl macrocyclic compound for inhibiting protein kinase activity
WO2019206069A1 (zh) * 2018-04-25 2019-10-31 北京普祺医药科技有限公司 一种二芳基巨环化合物、药物组合物以及其用途
WO2019210835A1 (zh) * 2018-05-04 2019-11-07 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
CA3224985A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide
CA3111984A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
US20210403485A1 (en) * 2018-09-29 2021-12-30 Shandong Luye Pharmaceutical Co., Ltd. Pyrazolopyrimidine derivative as selective trk inhibitor
JP7631193B2 (ja) 2018-10-22 2025-02-18 アルミス インコーポレイテッド Ｔｙｋ２阻害剤およびその使用
SG11202104609SA (en) 2018-11-09 2021-06-29 Shandong Xuanzhu Pharma Co Ltd Macrocyclic tyrosine kinase inhibitor and uses thereof
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
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
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
CN113490666A (zh) 2018-12-19 2021-10-08 奥瑞生物药品公司 作为fgfr酪氨酸激酶的抑制剂的取代的吡唑并[1,5-a]吡啶化合物
US20220177477A1 (en) 2019-03-19 2022-06-09 Central China Normal University Pyrazolopyrimidine compound, pharmaceutical composition, and application therefor
SG11202110523XA (en) 2019-03-26 2021-10-28 Ventyx Biosciences Inc Tyk2 pseudokinase ligands
AU2020270303B2 (en) 2019-05-08 2023-09-07 Tyk Medicines, Inc. Compound used as kinase inhibitor and application thereof
CN113727984B (zh) * 2019-05-21 2024-03-15 浙江海正药业股份有限公司 大环类衍生物、及其制备方法和用途
CN113773335B (zh) * 2019-06-21 2024-12-03 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
EP4023648A4 (en) * 2019-08-28 2023-09-27 Simcere Pharmaceutical Co. Ltd. CARCINOGENIC FUSIONED KINASE HIBITOR CRYSTAL AND APPLICATIONS THEREOF
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
CN114641478B (zh) * 2019-10-30 2024-07-02 南京再明医药有限公司 吡唑并嘧啶类化合物的制备方法及其中间体
TWI882032B (zh) 2019-11-08 2025-05-01 美商凡帝克斯生物科學公司 Tyk2假激酶配位體
CN114761407B (zh) * 2019-11-18 2024-06-18 广州嘉越医药科技有限公司 作为高选择性ros1抑制剂的化合物及其应用
JP2023504866A (ja) * 2019-12-13 2023-02-07 ▲賽▼▲諾▼哈勃▲薬▼▲業▼（成都）有限公司 大環構造を有するフッ素含有複素環誘導体およびその用途
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
EP4148055A4 (en) * 2020-05-08 2023-10-11 Shandong Xuanzhu Pharma Co., Ltd. CRYSTAL FORM OF A MACROCYCLIC TYROSINE KINASE INHIBITOR AND PROCESS FOR PRODUCTION THEREOF
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
BR112023000463A2 (pt) * 2020-07-10 2023-03-28 Blossomhill Therapeutics Inc Macrociclos e seu uso
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
WO2022150584A1 (en) * 2021-01-08 2022-07-14 Yale University Non-covalent inhibitors of the main protease of sars-cov-2 and methods of use
TWI804266B (zh) * 2021-04-07 2023-06-01 大陸商上海齊魯製藥研究中心有限公司 Tyk2抑制劑及其用途
TWI807830B (zh) * 2021-05-18 2023-07-01 大陸商廣州嘉越醫藥科技有限公司 一種含氰基取代的大環類化合物的晶型及其製備方法
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
CN117597128A (zh) * 2021-08-23 2024-02-23 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
RU2139281C1 (ru) 1993-11-30 1999-10-10 Джи Ди Сирл энд Компани Пиразолилзамещенный бензолсульфонамид или его фармацевтически приемлемая соль, фармацевтическая композиция, способ лечения от воспаления или связанного с воспалением заболевания
US5877016A (en) 1994-03-18 1999-03-02 Genentech, Inc. Human trk receptors and neurotrophic factor inhibitors
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
AU732392B2 (en) 1996-05-08 2001-04-26 Biogen Idec Ma Inc. Ret ligand (retL) for stimulating neural and renal growth
US6677135B1 (en) 1996-05-08 2004-01-13 Biogen, Inc. Ret ligand (RetL) for stimulating neutral and renal growth
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
DE69827786T2 (de) 1997-04-25 2005-11-24 Takeda Pharmaceutical Co. Ltd. Condensierte pyridazine derivate,deren herstellung und verwendung
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
WO2001016169A2 (en) 1999-09-01 2001-03-08 Biogen, Inc. RET LIGAND 5 (Retl5) FROM HUMAN AND MOUSE
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
ATE446366T1 (de) 2000-06-22 2009-11-15 Genentech Inc Agonistische monoklonale antikörper gegen trkc
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
CN101653604A (zh) 2001-05-30 2010-02-24 基因技术股份有限公司 抗ngf抗体用于治疗各种疾病
WO2003020698A2 (en) 2001-09-06 2003-03-13 Prochon Biotech Ltd. Protein tyrosine kinase inhibitors
US20030199525A1 (en) 2002-03-21 2003-10-23 Hirst Gavin C. Kinase inhibitors
CN100343255C (zh) 2002-04-23 2007-10-17 盐野义制药株式会社 吡唑并[1,5－a]嘧啶衍生物和含有该衍生物的NAD(P)H氧化酶抑制剂
US7449488B2 (en) 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
US20060116381A1 (en) 2002-07-24 2006-06-01 Fagin James A 4-4(methylpiperazin-1-ylmethyl)-n-[4-methyl-3-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-ben-zamide 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
US7119200B2 (en) 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
CA2497440C (en) 2002-09-04 2011-03-22 Schering Corporation 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
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines 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)
AU2003298942A1 (en) 2002-12-11 2004-06-30 Merck And 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
WO2004082458A2 (en) 2003-02-21 2004-09-30 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
EP1615697A2 (en) 2003-04-11 2006-01-18 Novo Nordisk A/S New pyrazolo[1,5-a] pyrimidine derivatives and pharmaceutical use thereof
EP1619203A1 (en) 2003-04-28 2006-01-25 Galpharma Co., Ltd. Galectin 9-inducing factor
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
RS20100555A (sr) 2003-07-15 2011-08-31 Amgen Inc. Humana anti-ngf neutrališuća antitela kao selektivni inhibitori ngf signalnog puta
US7642235B2 (en) * 2003-09-22 2010-01-05 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
US20090143399A1 (en) 2003-10-14 2009-06-04 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein Kinase Inhibitors
US7491794B2 (en) * 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
KR20060117329A (ko) 2003-11-21 2006-11-16 노파르티스 아게 단백질 키나제 저해제로서의 1ｈ-이미다조퀴놀린 유도체
TW200529849A (en) 2003-11-28 2005-09-16 Novartis Ag Diaryl urea derivatives in the treatment of protein kinase dependent diseases
US7799772B2 (en) * 2003-12-18 2010-09-21 Janssen Pharmaceutica N.V. Pyrido-and pyrimidopyrimidine derivatives as anti-profilerative agents
CN1925855B (zh) 2003-12-19 2010-06-16 普莱希科公司 开发Ret调节剂的化合物和方法
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
AR049769A1 (es) 2004-01-22 2006-09-06 Novartis Ag Derivados de pirazolo(1,5-a)pirimidin 7-il-amina para utilizarse en el tratamiento de enfermedades dependientes de la 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
EP1772215A4 (en) 2004-06-25 2009-07-29 Mitsubishi Materials Corp METAL COLLOID PARTICLES, METAL COLLOID AND USE OF COLLOID
WO2006017443A2 (en) 2004-08-02 2006-02-16 Osi Pharmaceuticals, Inc. Aryl-amino substituted pyrrolopyrimidine multi-kinase inhibiting compounds
PE20060664A1 (es) 2004-09-15 2006-08-04 Novartis Ag Amidas biciclicas como inhibidores de cinasa
WO2006050076A1 (en) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
US20060127982A1 (en) 2004-10-29 2006-06-15 Shih Jason C Development of an asporogenic bacillus licheniformis and production of keratinase therefrom
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
US7528138B2 (en) 2004-11-04 2009-05-05 Vertex Pharmaceuticals Incorporated Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
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
CN101119996A (zh) 2005-02-16 2008-02-06 阿斯利康(瑞典)有限公司 化学化合物
ES2347172T3 (es) 2005-02-16 2010-10-26 Astrazeneca Ab Compuestos quimicos.
WO2006089298A2 (en) 2005-02-18 2006-08-24 Attenuon, Llc Pyrimidine-fused diazepine derivatives and indole-fused pteridines
US7612067B2 (en) * 2005-03-21 2009-11-03 Eli Lilly And Company Imidazopyridazine compounds
GB0507575D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
CA2604787A1 (en) 2005-04-15 2006-10-26 Cylene Pharmaceuticals, Inc. Quinobenzoxazine analogs and methods of using thereof
US20090005396A1 (en) 2005-04-27 2009-01-01 Astrazeneca Ab Use of Pyrazolyl-Pyrimidine Derivatives in the Treatment of Pain
EP1899323A2 (en) 2005-05-16 2008-03-19 AstraZeneca AB Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors
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
WO2006130673A1 (en) 2005-05-31 2006-12-07 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.
DK2395004T3 (en) 2005-06-22 2016-03-21 Plexxikon Inc Pyrrolo [2,3-b] pyridine derivatives as protein kinase inhibitors
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
BRPI0613962A2 (pt) * 2005-07-25 2009-03-24 Intermune Inc inibidores macrocìclicos inovadores de replicação de vìrus da hepatite c
WO2007013673A1 (en) 2005-07-29 2007-02-01 Astellas Pharma Inc. Fused heterocycles as lck inhibitors
WO2007019058A1 (en) 2005-08-03 2007-02-15 Eastman Chemical Company Tocopheryl polyethylene glycol succinate powder and process for preparing same
WO2007024680A1 (en) 2005-08-22 2007-03-01 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
JP5366548B2 (ja) 2005-08-25 2013-12-11 クレアビリス・セラピューティクス・エスピーエー Ｋ‐２５２ａおよびその誘導体のポリマー結合体
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
BRPI0616985B1 (pt) 2005-10-06 2021-10-26 Merck Sharp & Dohme Corp. Composto de pirazolo[1,5-a]pirimidina, e, uso de um composto
WO2007044407A2 (en) 2005-10-06 2007-04-19 Schering Corporation Pyrazolo (1 , 5a) pyrimidines as protein kinase inhibitors
DK1999129T3 (da) * 2005-10-11 2011-02-07 Intermune Inc Forbindelser og fremgangsmåder til inhibering af replikationen af hepatitis C-virus
EP1948633B1 (en) 2005-10-11 2011-08-10 Centre National De La Recherche Scientifique (Cnrs) 3 -hydroxyflavone derivatives 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)
JP2009519218A (ja) 2005-11-03 2009-05-14 エスジーエックス ファーマシューティカルズ、インコーポレイテッド ピリミジニル−チオフェンキナーゼモジュレータ
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
JP2009518340A (ja) 2005-12-08 2009-05-07 ノバルティス アクチエンゲゼルシャフト ＥｐｈＢおよびＶＥＧＦＲ２キナーゼ阻害剤としてのピラゾロ［１，５−ａ］ピリジン−３−カルボン酸
US20080108611A1 (en) 2006-01-19 2008-05-08 Battista Kathleen A Substituted thienopyrimidine kinase inhibitors
WO2010093928A2 (en) 2009-02-12 2010-08-19 Cell Signaling Technology, Inc. Mutant ros expression in human cancer
KR101452520B1 (ko) 2006-01-27 2014-10-21 샹하이 헨그루이 파마수티컬 컴퍼니 리미티드 피롤로[3,2-ｃ]피리딘-4-온 2-인돌린온 단백질 키나제 억제제
KR100846988B1 (ko) 2006-03-06 2008-07-16 제일약품주식회사 신규한 티에노피리미딘 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 함유하는 약학조성물
MX2008011220A (es) 2006-03-07 2008-09-11 Array Biopharma Inc Compuestos de pirazol heterobiciclicos y metodos de uso.
RU2008140382A (ru) 2006-03-16 2010-04-27 Новартис АГ (CH) Гетероциклические органические соединения, например, для лечения меланомы
EP2001892B1 (en) 2006-03-17 2013-04-24 Ambit Biosciences Corporation Imidazolothiazole compounds for the treatment of proliferative diseases
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
BRPI0711628A2 (pt) 2006-05-15 2011-12-06 Irm Llc composto, composição farmacêutica, uso e processo para preparação do composto
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
TW201345908A (zh) 2006-07-05 2013-11-16 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
JP2010502716A (ja) 2006-09-07 2010-01-28 バイオジェン・アイデック・エムエイ・インコーポレイテッド インターロイキン１受容体関連キナーゼの調節物質
WO2008031551A2 (en) 2006-09-12 2008-03-20 Novartis Forschungsstiftung, Zweigniederlassung Non-neuroendocrine cancer therapy
ES2565683T3 (es) 2006-09-15 2016-04-06 Xcovery, Inc. Compuestos inhibidores de quinasa
KR20090073121A (ko) 2006-09-29 2009-07-02 노파르티스 아게 Ｐｉ3ｋ 지질 키나제 억제제로서의 피라졸로피리미딘
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
CA2667962A1 (en) 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents
US7750007B2 (en) 2006-11-06 2010-07-06 Supergen, Inc. Imidazo[1,2-beta]pyridazine and pyrazolo[1,5-alpha]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
EP2114403A2 (en) 2007-01-19 2009-11-11 Bayer Healthcare, LLC Treatment of cancers having resistance to chemotherapeutic agents
AU2008212758B2 (en) * 2007-02-08 2014-01-30 Medivir Ab Pyrimidine substituted macrocyclic HCV inhibitors
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
CA2682016A1 (en) 2007-03-28 2008-10-02 Inovacia Ab Pyrazolo [1,5-a]pyrimidines as inhibitors of stearoyl-coa desaturase
JP5374492B2 (ja) 2007-04-03 2013-12-25 アレイ バイオファーマ、インコーポレイテッド 受容体チロシンキナーゼ阻害薬としてのイミダゾ［１，２−ａ］ピリジン化合物
US20110189167A1 (en) 2007-04-20 2011-08-04 Flynn Daniel L Methods and Compositions for the Treatment of Myeloproliferative Diseases and other Proliferative Diseases
JP5160637B2 (ja) 2007-05-04 2013-03-13 アイアールエム・リミテッド・ライアビリティ・カンパニー ｃ−ｋｉｔおよびＰＤＧＦＲキナーゼインヒビターとしての化合物および組成物
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
US20100209488A1 (en) 2007-07-16 2010-08-19 The Regents Of The University Of California Protein kinase modulating compounds and methods for making and using them
SG183049A1 (en) 2007-07-20 2012-08-30 Nerviano Medical Sciences Srl Substituted indazole derivatives active as kinase inhibitors
EP2185698B1 (en) 2007-08-07 2015-04-22 Purdue Research Foundation Kinase inhibitors and uses thereof
HRP20141025T1 (hr) 2007-08-10 2015-01-02 Regeneron Pharmaceuticals, Inc. Humana antitijela s visokim afinitetom za humani faktor rasta živaca
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
JP2011500702A (ja) 2007-10-16 2011-01-06 ワイス・エルエルシー チエノピリミジンおよびピラゾロピリミジン化合物ならびにｍＴＯＲキナーゼおよびＰＩ３キナーゼ阻害剤としてのその使用
KR20100089851A (ko) 2007-10-23 2010-08-12 노파르티스 아게 호흡기 질환의 치료를 위한 ｔｒｋｂ 항체의 용도
EP2217601A1 (en) 2007-11-08 2010-08-18 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyridazines for use as protein kinase inhibitors
CA2706946A1 (en) 2007-11-28 2009-06-04 Schering Corporation 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
KR101290503B1 (ko) 2008-01-17 2013-07-26 아이알엠 엘엘씨 개선된 항-ｔｒｋｂ 항체
TW200942537A (en) 2008-02-01 2009-10-16 Irm Llc Compounds and compositions as kinase inhibitors
US20090209496A1 (en) 2008-02-15 2009-08-20 David Chaplin Methods and compositions for enhancing the efficacy of rtk inhibitors
US8822500B2 (en) 2008-03-19 2014-09-02 Chembridge Corporation Tyrosine kinase inhibitors
JP5628145B2 (ja) 2008-03-19 2014-11-19 ケムブリッジ・コーポレーション 新規チロシンキナーゼ阻害剤
WO2009140128A2 (en) 2008-05-13 2009-11-19 Irm Llc Compounds and compositions as kinase inhibitors
EP2303890A4 (en) 2008-06-19 2012-04-11 Progenics Pharm Inc INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE
CA2730190A1 (en) 2008-07-14 2010-01-21 Queen's University At Kingston Pharmaceutical compositions comprising ret inhibitors and methods for the treatment of cancer
WO2010012733A1 (en) 2008-07-29 2010-02-04 Nerviano Medical Sciences S.R.L. Use of a 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
ES2464461T3 (es) 2008-09-22 2014-06-02 Array Biopharma, Inc. Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa
CN102232071B (zh) 2008-09-26 2016-03-23 财团法人卫生研究院 作为蛋白激酶抑制剂的稠合多环化合物
SG196855A1 (en) * 2008-10-22 2014-02-13 Array Biopharma Inc Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors
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
EP2358725A1 (en) 2008-11-06 2011-08-24 Ambit Biosciences Corporation Imidazolothiazole compounds as modulators of protein kinase
WO2010058006A1 (en) 2008-11-24 2010-05-27 Nerviano Medical Sciences S.R.L. Cdk inhibitor for the treatment of mesothelioma
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
TWI410418B (zh) 2009-04-29 2013-10-01 Ind Tech Res Inst 氮雜薁化合物、藥學組合物與抑制一細胞中蛋白質激酶之活性的方法
HUE026647T2 (en) 2009-05-08 2016-07-28 Astellas Pharma Inc Diamino heterocyclic carboxamide compound
EP2440058A4 (en) 2009-06-12 2012-11-21 Dana Farber Cancer Inst Inc MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF
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
ES2658290T3 (es) 2009-10-29 2018-03-09 Genosco Inhibidores de cinasa
EP2498607B1 (en) 2009-11-13 2016-02-17 Genosco Kinase inhibitors
KR101094446B1 (ko) 2009-11-19 2011-12-15 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물
AU2010343102B2 (en) 2009-12-29 2016-03-24 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
SG182361A1 (en) 2010-01-29 2012-08-30 Hanmi Science Co Ltd THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES
KR101483215B1 (ko) 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
US9161944B2 (en) 2010-02-18 2015-10-20 Inserm (Institut National De La Sante Et De La Sante Et De La Recherche Medicale) Method for preventing cancer metastasis
US9469876B2 (en) 2010-04-06 2016-10-18 Caris Life Sciences Switzerland Holdings Gmbh Circulating biomarkers for metastatic prostate cancer
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
TWI510487B (zh) 2010-04-21 2015-12-01 Plexxikon Inc 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
AU2011256380C1 (en) 2010-05-20 2016-09-08 Array Biopharma Inc. Macrocyclic compounds as Trk kinase inhibitors
ES2910305T3 (es) 2010-08-19 2022-05-12 Zoetis Belgium S A Anticuerpos anti-NGF y su uso
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk
WO2012047017A2 (ko) 2010-10-05 2012-04-12 크리스탈지노믹스(주) 2,3-디히드로-이소인돌-1-온 유도체 및 이를 포함하는 조성물
EP2646468B1 (en) 2010-12-01 2018-07-25 AlderBio Holdings LLC Anti-ngf compositions and use thereof
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
SG192795A1 (en) 2011-02-25 2013-09-30 Irm Llc Compounds and compositions 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
PT2693881T (pt) 2011-04-01 2019-12-09 Univ Utah Res Found Análogos de n-fenilpirimidin-2-amina substituídos como inibidores da axl cinase
HRP20161786T1 (hr) 2011-05-13 2017-03-10 Array Biopharma, Inc. Pirolidinil urea, pirolidinil tiourea i pirolidinil gvanidin spojevi kao inhibitori trka kinaze
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
CA2846496C (en) 2011-09-02 2020-07-14 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
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
WO2013042137A1 (en) 2011-09-19 2013-03-28 Aurigene Discovery Technologies Limited Bicyclic heterocycles as irak4 inhibitors
WO2013059740A1 (en) 2011-10-21 2013-04-25 Foundation Medicine, Inc. Novel alk and ntrk1 fusion molecules and uses thereof
HK1202377A1 (en) 2011-11-14 2015-10-02 Tesaro Inc. Modulating certain tyrosine kinases
CA2858958C (en) 2011-12-12 2016-10-04 Dr. Reddy's Laboratories Ltd. Substituted pyrazolo[1,5-a]pyridine as tropomyosin receptor kinase (trk) inhibitors
JP5797345B2 (ja) 2011-12-30 2015-10-21 ハンミ ファーム． シーオー．， エルティーディー． プロテインキナーゼに対する阻害活性を有するチエノ［３，２−ｄ］ピリミジン誘導体
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
ES2605388T3 (es) 2012-04-26 2017-03-14 Ono Pharmaceutical Co., Ltd. Compuesto inhibidor de Trk
CA2871540A1 (en) 2012-05-10 2013-11-14 Synta Pharmaceuticals Corp. Treating cancer with hsp90 inhibitory compounds
PL3290414T3 (pl) 2012-05-23 2020-01-31 Nerviano Medical Sciences S.R.L. Sposób otrzymywania n-[5-(3,5-difluorobenzylo)-1h-indazol-3-ilo]-4-(4-metylopiperazyn-1-ylo)-2-(tetrahydropiran-4-yloamino)benzamidu
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
CN104619841A (zh) 2012-07-26 2015-05-13 日本国立癌症研究中心 Cep55基因与ret基因的融合基因
EP2689778A1 (en) 2012-07-27 2014-01-29 Pierre Fabre Medicament Derivatives of azaindoles or diazaindoles for treating pain
CA2882759C (en) 2012-08-31 2018-11-20 The Regents Of The University Of Colorado Detection of the ntrk1-mprip gene fusion for cancer diagnosis
ES2726605T3 (es) 2012-09-07 2019-10-08 Exelixis Inc Inhibidores de MET, VEGFR y RET para usar en el tratamiento del adenocarcinoma de pulmón
US20140084039A1 (en) 2012-09-24 2014-03-27 Electro Scientific Industries, Inc. Method and apparatus for separating workpieces
JP5759568B2 (ja) 2012-09-25 2015-08-05 中外製薬株式会社 Ｒｅｔ阻害剤
JP2014082984A (ja) 2012-10-23 2014-05-12 Astellas Pharma Inc 新規ｎｔｒｋ２活性化変異の検出法
US9604980B2 (en) 2012-11-07 2017-03-28 Nerviano Medical Sciences S.R.L. Substituted pyrimidinyl and pyridinyl-pyrrolopyridinones, process for their preparation and their use as kinase inhibitors
WO2014075035A1 (en) 2012-11-12 2014-05-15 Cephalon, Inc. Bendamustine derivatives and methods of using same
WO2014078372A1 (en) 2012-11-13 2014-05-22 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
UA116455C2 (uk) 2012-11-13 2018-03-26 Еррей Біофарма Інк. Сполуки n-піролідинілсечовини, n'-піразолілсечовини, тіосечовини, гуанідину та ціаногуанідину як інгібітори кінази trka
UA117573C2 (uk) 2012-11-13 2018-08-27 Ерей Біофарма Інк. Біциклічні сполуки сечовини, тіосечовини, гуанідину й ціаногуанідину, придатні для лікування болю
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl 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
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
EP2925359A2 (en) 2012-11-29 2015-10-07 Yeda Research and Development Co., Ltd. Methods of preventing tumor metastasis, treating and prognosing cancer and identifying agents which are putative metastasis inhibitors
CN103848785B (zh) 2012-12-04 2016-07-13 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
JP6325573B2 (ja) 2012-12-28 2018-05-16 クリスタルジェノミクス・インコーポレイテッドＣｒｙｓｔａｌｇｅｎｏｍｉｃｓ， Ｉｎｃ． Ｂｔｋキナーゼ抑制剤としての２，３−ジヒドロ−イソインドール−１−オン誘導体及びこれを含む薬学的組成物
FR3000494B1 (fr) 2012-12-28 2015-08-21 Oribase Pharma Nouveaux derives d'azaindoles en tant qu'inhibiteurs de proteines kinases
FR3000492B1 (fr) 2012-12-28 2015-09-11 Oribase Pharma Nouveaux derives azaindole en tant qu'inhibiteurs multikinases
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
CA2901332A1 (en) 2013-02-19 2014-08-28 Ono Pharmaceutical Co., Ltd. Trk-inhibiting compound
EP2981613A4 (en) 2013-02-22 2016-11-02 Boris C Bastian FUSION POLYNUCLEOTIDES AND FUSION POLYPEPTIDES ASSOCIATED WITH CANCER, IN PARTICULAR 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
US8937071B2 (en) 2013-03-15 2015-01-20 Glaxosmithkline Intellectual Property Development Limited Compounds as rearranged during transfection (RET) inhibitors
KR20150129847A (ko) 2013-03-15 2015-11-20 더 트러스티스 오브 컬럼비아 유니버시티 인 더 시티 오브 뉴욕 융합 단백질 및 이들의 방법
UA115264C2 (uk) 2013-03-15 2017-10-10 Глаксосмітклайн Інтеллектьюел Проперті Девелопмент Лімітед Піридинові похідні як інгібітори реаранжованої у процесі трансфекції (ret) кінази
EP3795696B1 (en) 2013-03-15 2023-04-26 The Board of Trustees of the Leland Stanford Junior University Identification and use of circulating nucleic acid tumor markers
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
JP2016518123A (ja) 2013-04-17 2016-06-23 ライフ テクノロジーズ コーポレーション 癌に関連付けられる遺伝子融合物及び遺伝子変異型
RU2656591C2 (ru) 2013-07-11 2018-06-06 Бетта Фармасьютикалз Ко., Лтд Модуляторы протеин-тирозинкиназы и способы их применения
US10705087B2 (en) 2013-07-26 2020-07-07 Japanese Foundation For Cancer Research Detection method for NTRK3 fusion
EP3628749A1 (en) 2013-07-30 2020-04-01 Blueprint Medicines Corporation Ntrk2 fusions
US20150057335A1 (en) 2013-08-20 2015-02-26 National Cancer Center Novel fusion genes identified in lung cancer
RU2016111675A (ru) 2013-08-30 2017-10-04 Эмбит Байосайенсиз Корпорейшн Соединения биарилацетамида и способы их применения
MX2016004678A (es) 2013-10-24 2017-03-10 Univ Georgetown Composiciones para el tratamiento del cancer.
WO2015064621A1 (ja) 2013-10-29 2015-05-07 公益財団法人がん研究会 新規融合体及びその検出法
US10212896B2 (en) 2013-11-27 2019-02-26 Enplas Corporation Emitter, and tube for drip irrigation
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
PL3097107T3 (pl) 2014-01-24 2020-01-31 Turning Point Therapeutics, Inc. Diarylowe związki makrocykliczne jako modulatory kinaz białkowych
HUE055357T2 (hu) 2014-02-05 2021-11-29 VM Oncology LLC Vegyületek kompozíciói és azok alkalmazásai
UA123534C2 (uk) 2014-02-14 2021-04-21 Екселіксис, Інк. Кристалічні тверді форми n-{4-[(6,7-диметоксихінолін-4-іл)окси]феніл}-n'-(4-флуорофеніл)циклопропан-1,1-дикарбоксаміду, способи отримання і способи застосування
US10231965B2 (en) 2014-02-20 2019-03-19 Ignyta, Inc. Molecules for administration to ROS1 mutant cancer cells
CN109970614B (zh) 2014-05-15 2023-01-13 阵列生物制药公司 作为trka激酶抑制剂的化合物及其用途
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
JP6665154B2 (ja) 2014-07-17 2020-03-13 ノース・アンド・サウス・ブラザー・ファーマシー・インベストメント・カンパニー・リミテッド 置換尿素誘導体及びその薬学的使用
MX2017001302A (es) 2014-08-01 2017-10-11 Pharmacyclics Llc Biomarcadores para predecir la respuesta del dlbcl al tratamiento con un inhibidor de la btk.
TWI560185B (en) 2014-08-18 2016-12-01 Ono Pharmaceutical Co Acid addition salt of trk inhibitor compound
CN107148418A (zh) 2014-09-08 2017-09-08 葛兰素史密斯克莱知识产权发展有限公司 2‑(4‑(4‑乙氧基‑6‑氧代‑1,6‑二氢吡啶‑3‑基)‑2‑氟苯基)‑n‑(5‑(1,1,1‑三氟‑2‑甲基丙‑2‑基)异噁唑‑3‑基)乙酰胺的晶型
RS58813B1 (sr) 2014-09-10 2019-07-31 Glaxosmithkline Ip Dev Ltd Piridonski derivati korišćeni kao inhibitori kinaze reorganizovane tokom transfekcije (ret)
JP6538153B2 (ja) 2014-09-10 2019-07-03 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｒｅａｒｒａｎｇｅｄ ｄｕｒｉｎｇ ｔｒａｎｓｆｅｃｔｉｏｎ（ｒｅｔ）阻害剤としての新規な化合物
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
US9988452B2 (en) 2014-10-14 2018-06-05 Novartis Ag Antibody molecules to PD-L1 and uses thereof
EP3699181B1 (en) 2014-11-16 2023-03-01 Array Biopharma, Inc. Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
EP4420732A3 (en) * 2014-12-15 2024-11-27 CMG Pharmaceutical Co., Ltd. Fused ring heteroaryl compounds and their use as trk inhibitors
EP3233840B1 (en) 2014-12-16 2018-11-21 Eudendron S.r.l. Heterocyclic derivatives modulating activity of certain protein kinases
US10202365B2 (en) 2015-02-06 2019-02-12 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
AU2016226210A1 (en) 2015-03-03 2017-09-21 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
WO2016168992A1 (en) 2015-04-21 2016-10-27 Ruijin Hospital Affiliated To Shanghai Jiao Tong University School Of Medicine Preparation and use of novel protein kinase inhibitors
IL302102A (en) 2015-05-20 2023-06-01 Dana Farber Cancer Inst Inc shared neoantigens
CN107849113B (zh) 2015-05-29 2022-03-22 亚尼塔公司 用于治疗具有rtk突变细胞的患者的组合物和方法
AU2016270803A1 (en) 2015-06-01 2018-01-04 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
AU2016287568B2 (en) 2015-07-02 2020-08-20 Turning Point Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
GB201512365D0 (en) 2015-07-15 2015-08-19 King S College London Novel therapy
JP6816100B2 (ja) 2015-07-16 2021-01-20 アレイ バイオファーマ、インコーポレイテッド ＲＥＴキナーゼ阻害物質としての置換ピラゾロ［１，５−ａ］ピリジン化合物
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
US10550124B2 (en) 2015-08-13 2020-02-04 San Diego State University 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
US10724102B2 (en) 2015-10-26 2020-07-28 Loxo Oncology, Inc. Point mutations in TRK inhibitor-resistant cancer and methods relating to the same
TWI787018B (zh) 2015-11-02 2022-12-11 美商纜圖藥品公司 轉染過程重排之抑制劑
JP2018537980A (ja) 2015-12-08 2018-12-27 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 癌治療のための非小細胞肺癌（ｎｓｃｌｃ）および甲状腺癌患者を選択するためのバイオマーカーとしてｒｅｔ融合遺伝子を使用する方法
JP6871869B2 (ja) 2016-01-15 2021-05-19 公益財団法人がん研究会 新規融合体及びその検出法
WO2017127835A2 (en) 2016-01-22 2017-07-27 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
SI3269370T1 (sl) 2016-02-23 2020-07-31 Taiho Pharmaceutical Co., Ltd. Nova spojina kondenziranega pirimida ali njegove soli
JPWO2017155018A1 (ja) 2016-03-11 2019-01-17 小野薬品工業株式会社 Ｔｒｋ阻害剤抵抗性の癌治療剤
UY37155A (es) 2016-03-17 2017-10-31 Blueprint Medicines Corp Inhibidores de ret
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
SG11201808559PA (en) 2016-04-04 2018-10-30 Loxo Oncology Inc Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
EP4104837A3 (en) 2016-04-15 2023-04-26 Cancer Research Technology Limited Heterocyclic compounds as ret kinase inhibitors
ES2886587T3 (es) 2016-04-15 2021-12-20 Cancer Research Tech Ltd Compuestos heterocíclicos como inhibidores de la quinasa RET
RU2757905C2 (ru) 2016-04-19 2021-10-22 Экселиксис, Инк. Способ лечения трижды негативного рака молочной железы
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
FI3800189T3 (fi) 2016-05-18 2023-07-31 Loxo Oncology Inc (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin valmistaminen
WO2017201156A1 (en) 2016-05-18 2017-11-23 Duke University Method of treating kras wild-type metastatic colorectal cell carcinoma using cabozantinib plus panitumumab
EP3464625A1 (en) 2016-06-01 2019-04-10 F. Hoffmann-La Roche AG Novel mutations in anaplastic lymphoma kinase predicting response to alk inhibitor therapy in lung cancer patients
US10227329B2 (en) 2016-07-22 2019-03-12 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
CA3049452A1 (en) 2017-01-20 2018-07-26 Gisela Schwab 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
WO2019084285A1 (en) 2017-10-26 2019-05-02 Qian Zhao FORMULATIONS OF A MACROCYCLIC TRK KINASE INHIBITOR

Also Published As

Publication number Publication date
LT2918588T (lt) 2017-08-25
PT3205654T (pt) 2019-04-22
DK2918588T3 (en) 2017-08-28
DK3205654T3 (en) 2019-04-15
CN102971322A (zh) 2013-03-13
MX382699B (es) 2025-03-13
TW201202254A (en) 2012-01-16
KR20130086951A (ko) 2013-08-05
US20170107232A1 (en) 2017-04-20
EP2918588A1 (en) 2015-09-16
AU2016203348B2 (en) 2018-08-09
CN105693720A (zh) 2016-06-22
TWI609019B (zh) 2017-12-21
AU2016203348C1 (en) 2020-11-12
US9718822B2 (en) 2017-08-01
HUE044025T2 (hu) 2019-09-30
PL3205654T3 (pl) 2019-08-30
SI3205654T1 (sl) 2019-07-31
TW201625640A (zh) 2016-07-16
US9840519B2 (en) 2017-12-12
TW201819388A (zh) 2018-06-01
AU2011256380B2 (en) 2016-02-25
KR101852169B1 (ko) 2018-04-26
TWI667241B (zh) 2019-08-01
JP2019104756A (ja) 2019-06-27
CN102971322B (zh) 2016-02-17
ES2534335T3 (es) 2015-04-21
ES2628418T3 (es) 2017-08-02
BR112012029405A8 (pt) 2019-12-17
TW201936197A (zh) 2019-09-16
US20150336970A1 (en) 2015-11-26
JP6523356B2 (ja) 2019-05-29
HK1181756A1 (en) 2013-11-15
EP3205654A1 (en) 2017-08-16
EP2571883B1 (en) 2015-01-07
RU2016128920A (ru) 2018-12-07
US20170112842A1 (en) 2017-04-27
TWI734134B (zh) 2021-07-21
UY33395A (es) 2012-11-30
PH12015500190B1 (en) 2015-10-19
HRP20171140T1 (hr) 2017-10-06
US9750744B2 (en) 2017-09-05
MX2019006154A (es) 2019-08-21
EP3205654B1 (en) 2019-01-02
RU2594742C2 (ru) 2016-08-20
KR20190101498A (ko) 2019-08-30
BR112012029405A2 (pt) 2016-12-06
US10647730B2 (en) 2020-05-12
JP6283636B2 (ja) 2018-02-21
IL257104B (en) 2021-03-25
IL223094A0 (en) 2013-02-03
PH12015500190A1 (en) 2015-10-19
JP2017082018A (ja) 2017-05-18
RU2735545C2 (ru) 2020-11-03
SG185644A1 (en) 2012-12-28
KR102132405B1 (ko) 2020-07-09
AU2011256380C1 (en) 2016-09-08
PH12012502276A1 (en) 2015-04-22
SG10201506591TA (en) 2015-09-29
US20190031684A1 (en) 2019-01-31
AU2011256380A1 (en) 2013-01-10
JP5832527B2 (ja) 2015-12-16
TWI516493B (zh) 2016-01-11
JP2015221834A (ja) 2015-12-10
BR122019024201B1 (pt) 2021-08-03
CL2012003227A1 (es) 2013-02-08
PL2918588T3 (pl) 2017-10-31
US20200291026A1 (en) 2020-09-17
AU2018208676B2 (en) 2020-07-30
JP2021054840A (ja) 2021-04-08
KR20200085364A (ko) 2020-07-14
CR20170098A (es) 2017-07-17
RU2012155278A (ru) 2014-06-27
AU2016203348A1 (en) 2016-06-16
BR112012029405B1 (pt) 2021-01-05
CN110003209A (zh) 2019-07-12
CA2800079C (en) 2020-09-15
MX383400B (es) 2025-03-13
US8933084B2 (en) 2015-01-13
HUE035337T2 (en) 2018-05-02
SI2918588T1 (sl) 2017-09-29
SMT201900203T1 (it) 2019-05-10
ES2718043T3 (es) 2019-06-27
LT3205654T (lt) 2019-05-27
MX365251B (es) 2019-05-28
KR102015402B1 (ko) 2019-08-28
KR20180043407A (ko) 2018-04-27
IL223094B (en) 2018-05-31
MX2012013467A (es) 2013-04-29
US20170114059A1 (en) 2017-04-27
SMT201700372T1 (it) 2017-09-07
CY1119345T1 (el) 2018-02-14
CN110003209B (zh) 2022-01-25
AU2018208676A1 (en) 2018-08-09
PT2918588T (pt) 2017-06-29
CN105693720B (zh) 2019-01-18
US9493476B2 (en) 2016-11-15
US9902741B2 (en) 2018-02-27
IL257104A (en) 2018-03-29
CY1121688T1 (el) 2020-07-31
RS58537B1 (sr) 2019-04-30
HRP20190559T1 (hr) 2019-06-14
MY191934A (en) 2022-07-19
EP3521291A1 (en) 2019-08-07
RU2016128920A3 (enExample) 2019-12-25
US20130203776A1 (en) 2013-08-08
CO6660502A2 (es) 2013-04-30
CA2800079A1 (en) 2011-11-24
US20170283435A1 (en) 2017-10-05
SG10201506593XA (en) 2015-10-29
AU2020205339A1 (en) 2020-08-06
AR081919A1 (es) 2012-10-31
HK1215245A1 (en) 2016-08-19
EP2571883A1 (en) 2013-03-27
NZ604708A (en) 2015-05-29
WO2011146336A1 (en) 2011-11-24
JP2013530142A (ja) 2013-07-25
EP2918588B1 (en) 2017-05-03

Similar Documents

Publication Publication Date Title
ME03376B (me) Makrociklička jedinjenja kао inhibiтori trk kinaze
IL221343B (en) Macrocycles as factor xia inhibitors
BR112013009935C8 (pt) compostos
CR20120576A (es) Inhibidores de pirazolil quinazolina cinasa
DK2540728T3 (da) Heterocyklisk forbindelse
CO6930358A2 (es) Compuestos inhibidores de metaloenzimas
DK2648516T3 (da) Substituerede pyridinon-pyridinylforbindelser
DK2710018T3 (da) Makrocykliske forbindelser som proteinkinasehæmmere
IL229513A0 (en) Imidazopyridine compounds
BR112012031667A2 (pt) composição
CO6801726A2 (es) Compuestos
BR112012032683A2 (pt) composição
PT2626350E (pt) Composto de ciclopropano
DK2649070T3 (da) Triazolpyridinforbindelser
BR112013010643A2 (pt) compostos heterocíclicos
BR112012026803A2 (pt) composto
BR112013014484A2 (pt) compostos inibidores de metaloenzimas
DK2623492T3 (da) Cyclohexanderivatforbindelse
BR112013005210A2 (pt) compostos heterocíclicos como inibidores de dgat1
BR112012030931A2 (pt) derivados de 2-amino-piriidina úteis como inibidores de jnk
BR112013003753A2 (pt) compostos
CU24069B1 (es) Compuestos de pirrolo-pirimidina como inhibidores de cdk4/6
BR112013013549A2 (pt) compostos orgânicos