KR101853026B1 - ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물 - Google Patents

ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물 Download PDF

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KR101853026B1
KR101853026B1 KR1020177027624A KR20177027624A KR101853026B1 KR 101853026 B1 KR101853026 B1 KR 101853026B1 KR 1020177027624 A KR1020177027624 A KR 1020177027624A KR 20177027624 A KR20177027624 A KR 20177027624A KR 101853026 B1 KR101853026 B1 KR 101853026B1
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pyrazolo
pyrimidin
alkyl
mmol
pyrrolidin
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KR20170116220A (ko
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줄리아 하스
스티븐 더블유. 앤드류스
유통 지앙
간 장
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어레이 바이오파마 인크.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • C07D519/02—Ergot alkaloids of the cyclic peptide type
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
KR1020177027624A 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물 Expired - Fee Related KR101853026B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US10761608P 2008-10-22 2008-10-22
US61/107,616 2008-10-22
PCT/US2009/061519 WO2010048314A1 (en) 2008-10-22 2009-10-21 SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS

Related Parent Applications (1)

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KR1020167022867A Division KR101784798B1 (ko) 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물

Related Child Applications (1)

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KR1020187011433A Division KR102037619B1 (ko) 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물

Publications (2)

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KR20170116220A KR20170116220A (ko) 2017-10-18
KR101853026B1 true KR101853026B1 (ko) 2018-04-27

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KR1020167022867A Active KR101784798B1 (ko) 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
KR1020187011433A Expired - Fee Related KR102037619B1 (ko) 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
KR1020147029018A Expired - Fee Related KR101652189B1 (ko) 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
KR1020117011561A Active KR101634833B1 (ko) 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
KR1020177027624A Expired - Fee Related KR101853026B1 (ko) 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물

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KR1020167022867A Active KR101784798B1 (ko) 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
KR1020187011433A Expired - Fee Related KR102037619B1 (ko) 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
KR1020147029018A Expired - Fee Related KR101652189B1 (ko) 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물
KR1020117011561A Active KR101634833B1 (ko) 2008-10-22 2009-10-21 ＴＲＫ 키나아제 억제제로서 치환된 피라졸로［１,５­ａ］ 피리미딘 화합물

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US (11) US8513263B2 (enExample)
EP (4) EP2725028B1 (enExample)
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KR (5) KR101784798B1 (enExample)
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AR (2) AR074052A1 (enExample)
AU (1) AU2009308465B2 (enExample)
BR (1) BRPI0919873B8 (enExample)
CA (1) CA2741313C (enExample)
CL (1) CL2011000880A1 (enExample)
CO (1) CO6440551A2 (enExample)
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PL (4) PL2725028T3 (enExample)
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RU (1) RU2018131134A (enExample)
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SI (4) SI3106463T1 (enExample)
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TW (4) TWI670272B (enExample)
UA (1) UA106054C2 (enExample)
UY (1) UY32192A (enExample)
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Families Citing this family (140)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS53350B (sr) 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze
PT2725028T (pt) 2008-10-22 2016-08-31 Array Biopharma Inc Compostos de pirazolo[1,5-]pirimidina substituídos como intermediários na síntese de inibidores de cinase trk
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
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
HUE044025T2 (hu) * 2010-05-20 2019-09-30 Array Biopharma Inc Makrociklusos vegyületek mint TRK-kináz inhibitorok
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
GEP20156285B (en) * 2011-02-25 2015-05-11 Aierem Elelsi Compounds and compositions as trk inhibitors
UA114711C2 (uk) * 2011-05-13 2017-07-25 Еррей Біофарма Інк. Сполуки піролідинілсечовини й піролідинілтіосечовини як інгібітори кінази trka
MX356401B (es) * 2011-12-12 2018-05-21 Dr Reddys Laboratories Ltd Pirazol[1,5-a]piridina sustituida como inhibidores de la cinasa del receptor de tropomiosina (trk).
HUE038786T2 (hu) * 2012-03-09 2018-11-28 Lexicon Pharmaceuticals Inc Pirazolo[1,5-a]pirimidin-alapú vegyületek, ezeket tartalmazó kompozíciók és eljárások alkalmazásukra
WO2014078378A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl 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
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
HRP20161613T1 (hr) 2012-11-13 2017-01-13 Array Biopharma, Inc. Tvari bicikličke ureje, tioureje, gvanidina i cijanogvanidina korisne za liječenje boli
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
EP2922844B1 (en) 2012-11-13 2018-01-10 Array Biopharma, Inc. N-pyrrolidinyl, 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
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
US9790210B2 (en) 2012-11-13 2017-10-17 Array Biopharma Inc. N-(monocyclic aryl),N'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9790178B2 (en) 2012-11-13 2017-10-17 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
ES2649156T3 (es) 2013-01-14 2018-01-10 Incyte Holdings Corporation Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim
CA2897333C (en) 2013-01-15 2021-07-06 Incyte Corporation Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors
CR20160135A (es) 2013-08-23 2016-08-05 Incyte Corp Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de cinasas pim
TW201542550A (zh) * 2013-09-06 2015-11-16 Lexicon Pharmaceuticals Inc 吡唑并［１，５－ａ］嘧啶基化合物、包含彼之組合物以及使用彼之方法
CN110317214B (zh) 2014-01-24 2022-11-22 特普医药公司 作为蛋白质激酶的调节剂的二芳基巨环
CA2938884C (en) * 2014-02-07 2024-02-13 eXIthera Pharmaceuticals Inc. Substituted azetidine compounds and their use as factor xia or kallikrein inhibitors
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
RU2719489C2 (ru) 2014-05-15 2020-04-17 Эррэй Биофарма Инк. 1-((3S,4R)-4-(3-ФТОРФЕНИЛ)-1-(2-МЕТОКСИЭТИЛ)ПИРРОЛИДИН-3-ИЛ)-3-(4-МЕТИЛ-3-(2-МЕТИЛПИРИМИДИН-5-ИЛ)-1-ФЕНИЛ-1Н-ПИРАЗОЛ-5-ИЛ)МОЧЕВИНА В КАЧЕСТВЕ ИНГИБИТОРА TrkA КИНАЗЫ
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
FI3699181T3 (fi) * 2014-11-16 2023-03-28 Array Biopharma Inc Kiteinen muoto (s)-n-(5-((r)-2-(2,5-diluorifenyyli)-pyrrolidin-1-yyli)-pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidivetyysulfaatista
KR102595599B1 (ko) 2014-12-02 2023-11-02 이그니타, 인코포레이티드 신경모세포종의 치료를 위한 병용
AU2015365587B2 (en) 2014-12-15 2020-07-23 Cmg Pharmaceutical Co., Ltd. Fused ring heteroaryl compounds and their use as TRK inhibitors
US10329294B2 (en) 2015-03-12 2019-06-25 Merck Sharp & Dohme Corp. Pyrazolopyrimidine inhibitors of IRAK4 activity
EP3268367B8 (en) 2015-03-12 2022-11-16 Merck Sharp & Dohme LLC Carboxamide inhibitors of irak4 activity
EP3303382A4 (en) * 2015-05-29 2018-12-19 Ignyta, Inc. Compositions and methods for treating patients with rtk mutant cells
US9540347B2 (en) 2015-05-29 2017-01-10 Incyte Corporation Pyridineamine compounds useful as Pim kinase inhibitors
MX2017015461A (es) * 2015-06-01 2018-08-15 Loxo Oncology Inc Métodos para diagnosticar y tratar el cáncer.
JP6871903B2 (ja) * 2015-07-02 2021-05-19 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Ｔｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子
JP6917974B2 (ja) 2015-07-06 2021-08-11 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Ｔｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． ジアリール大環状多形
PL3322706T3 (pl) 2015-07-16 2021-07-19 Array Biopharma, Inc. Podstawione związki pirazolo[1,5-a]pirydynowe jako inhibitory kinazy ret
JP6817287B2 (ja) 2015-07-21 2021-01-20 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Ｔｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． キラルジアリール大環状分子及びその使用
HK1255330A1 (zh) 2015-08-26 2019-08-16 缆图药品公司 适用於治疗与ntrk相关的病症的化合物和组合物
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Ｐｉｍ激酶抑制劑之鹽
TW201718546A (zh) 2015-10-02 2017-06-01 英塞特公司 適用作pim激酶抑制劑之雜環化合物
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate Point mutations in trk inhibitor-resistant cancer and methods relating to the same
TWI733713B (zh) 2015-11-19 2021-07-21 美商纜圖藥品公司 用於治療神經促進性酪氨酸受體激酶相關之異常的化合物與組成物
EP3389645A4 (en) 2015-12-18 2019-12-18 Ignyta, Inc. COMBINATIONS FOR TREATING CANCER
RS65987B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Tečne formulacije (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CA3019661A1 (en) * 2016-04-04 2017-10-12 Loxo Oncology, Inc. Methods of treating pediatric cancers
EP3800189B1 (en) 2016-05-18 2023-06-28 Loxo Oncology, Inc. Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
US10689400B2 (en) 2016-07-28 2020-06-23 Turning Point Therapeutics, Inc. Macrocycle 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
MX380283B (es) 2016-10-28 2025-03-12 Chia Tai Tianqing Pharmaceutical Group Co Ltd Compuesto de amino pirazolopirimidina usado como inhibidor del receptor de tirosina cinasa del factor neurotrófico
CN108003161B (zh) * 2016-10-28 2020-10-09 正大天晴药业集团股份有限公司 神经营养因子酪氨酸激酶受体抑制剂
AR110252A1 (es) 2016-11-30 2019-03-13 Gilead Sciences Inc Compuestos heterocíclicos fusionados como inhibidores de la quinasa cam
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
US11168090B2 (en) 2017-01-18 2021-11-09 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazines as RET kinase 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
WO2019018570A1 (en) 2017-07-19 2019-01-24 Ignyta, Inc. PHARMACEUTICAL COMPOSITIONS CONTAINING ENTRECTINIB
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
FI3661935T3 (fi) * 2017-08-11 2023-01-13 Kinaasin estäjinä käyttökelpoiset pyratsolipyrimidiinit
US10180422B1 (en) 2017-08-22 2019-01-15 Scripps Health Methods of treating a neuroendocrine tumor
FI3674307T3 (fi) * 2017-08-23 2023-09-11 Chia Tai Tianqing Pharmaceutical Group Co Ltd Aminopyratsolin ja pyrimidiinin sisältävä makrosykli ja sen farmaseuttinen koostumus ja käyttö
CN107445879B (zh) * 2017-09-21 2020-07-24 苏州立新制药有限公司 拉曲替尼中间体的制备方法
CN107556226B (zh) * 2017-09-21 2020-06-30 苏州明锐医药科技有限公司 一种拉曲替尼中间体的制备方法
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
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
JP7311498B2 (ja) 2017-10-17 2023-07-19 イグナイタ インコーポレイテッド 薬学的組成物および剤形
US20190247398A1 (en) 2017-10-26 2019-08-15 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
HRP20251226T1 (hr) 2017-10-31 2025-12-05 Assia Chemical Industries Ltd. Soli i oblici larotrectiniba u čvrstom stanju
US11098046B2 (en) 2017-11-10 2021-08-24 Angex Pharmaceutical, Inc. Macrocyclic compounds as TRK kinase inhibitors and uses thereof
CN107987082B (zh) * 2017-11-14 2019-09-20 苏州东南药业股份有限公司 一种Larotrectinib的制备方法及其中间体
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
EP3724191B9 (en) * 2017-12-15 2022-05-18 Pyramid Biosciences, Inc. 5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3-(1h-pyrazol-1-yl)pyrazolo[1,5-a]pyrimidine derivatives and related compounds as trk kinase inhibitors for treating cancer
JOP20200152A1 (ar) 2017-12-19 2022-10-30 Turning Point Therapeutics Inc مركبات حلقية كبرى لعلاج مرض
JP7150356B2 (ja) * 2017-12-22 2022-10-11 深▲チェン▼市塔吉瑞生物医薬有限公司 置換ピラゾロ［１，５－ａ］ピリミジン化合物並びにその医薬組成物および使用
EP3740486A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds 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
CA3087578C (en) 2018-01-18 2023-08-08 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
WO2019144885A1 (zh) 2018-01-23 2019-08-01 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
CN111511749B (zh) * 2018-01-30 2022-02-08 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
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
CN110305138B (zh) * 2018-03-27 2021-04-23 海创药业股份有限公司 一种治疗癌症的化合物及其用途
WO2019191659A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers
EP3779071B1 (en) 2018-03-30 2024-02-21 Sumitomo Heavy Industries, Ltd. Construction machine operation assistance system, and construction machine
US12129258B2 (en) 2018-04-25 2024-10-29 Primegene (Beijing) Co., Ltd Diaryl macrocyclic compound and pharmaceutical composition, and use thereof
CN110294761B (zh) * 2018-06-08 2020-09-08 南京雷正医药科技有限公司 作为Trk激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物
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
CN117281803A (zh) 2018-07-31 2023-12-26 罗索肿瘤学公司 喷雾干燥的分散体和制剂
MX2021001752A (es) 2018-08-14 2021-06-23 Osteoqc Inc Compuestos de pirrolo-dipiridina.
JP7695496B2 (ja) 2018-08-14 2025-06-19 オシフィ セラピューティクス リミティド ライアビリティ カンパニー フルオロβ－カルボリン化合物
CN110857304B (zh) * 2018-08-24 2021-05-18 北京富龙康泰生物技术有限公司 Trk抑制剂、其制备方法和用途
CN112739691B (zh) 2018-09-03 2023-05-23 泰励生物科技（上海）有限公司 用作抗癌药的trk抑制剂
WO2020055672A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
WO2020063965A1 (zh) * 2018-09-29 2020-04-02 南京明德新药研发有限公司 作为选择性Trk抑制剂的吡唑并嘧啶衍生物
CN111039947A (zh) * 2018-10-15 2020-04-21 上海轶诺药业有限公司 一类蛋白受体激酶抑制剂的制备和应用
CN111171020A (zh) 2018-11-13 2020-05-19 上海轶诺药业有限公司 一类六元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途
CN111171019A (zh) 2018-11-13 2020-05-19 上海轶诺药业有限公司 一类五元并六元杂环化合物及其作为蛋白受体激酶抑制剂的用途
CN109232582B (zh) * 2018-11-28 2021-02-05 安礼特（上海）医药科技有限公司 拉洛替尼硫酸氢盐晶型及其制备和应用
CN111269233A (zh) * 2018-12-05 2020-06-12 上海轶诺药业有限公司 一类咪唑并芳环类化合物的制备和应用
CN109608464B (zh) 2018-12-12 2021-09-24 上海健康医学院 一种放射性碘标记Larotrectinib化合物及其制备方法和应用
CN109705124B (zh) * 2018-12-14 2021-09-24 上海健康医学院 一种放射性氟标记Larotrectinib化合物及其制备方法
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
JP2022515197A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド がんを治療するためのｆｇｆｒ阻害剤としての７－（（３，５－ジメトキシフェニル）アミノ）キノキサリン誘導体
CN111362946A (zh) * 2018-12-25 2020-07-03 上海度德医药科技有限公司 一种药物化合物及其组合物和应用
CN109942574B (zh) * 2019-01-11 2022-04-01 成都阿奇生物医药科技有限公司 天奇替尼及其制备方法和用途
CN109942582B (zh) * 2019-03-15 2020-12-01 上海健康医学院 一种靶向原肌球蛋白激酶trk融合蛋白的pet探针及其合成与应用
WO2020187291A1 (zh) 2019-03-19 2020-09-24 华中师范大学 吡唑并嘧啶化合物和药物组合物及其应用
JP2022526713A (ja) 2019-03-21 2022-05-26 オンクセオ がんの処置のための、キナーゼ阻害剤と組み合わせたＤｂａｉｔ分子
CN111848626B (zh) * 2019-04-30 2021-11-30 江苏柯菲平医药股份有限公司 Trk激酶抑制剂及其用途
AU2020270303B2 (en) 2019-05-08 2023-09-07 Tyk Medicines, Inc. Compound used as kinase inhibitor and application thereof
US20200398978A1 (en) * 2019-06-20 2020-12-24 Bell Helicopter Textron Inc. Low-drag rotor blade extension
WO2021023858A1 (en) * 2019-08-08 2021-02-11 Université De Strasbourg TrkB POSITIVE ALLOSTERIC MODULATORS
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
CN110643672A (zh) * 2019-10-15 2020-01-03 西安交通大学 高表达TrkB作为新型靶点在抑制胰腺癌转移方面的医药用途
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
CN112812118A (zh) * 2019-11-18 2021-05-18 上海轶诺药业有限公司 一类蛋白受体激酶抑制剂的制备和应用
CN111138437B (zh) * 2019-12-04 2021-03-05 杭州华东医药集团新药研究院有限公司 取代的吡唑并[1,5-a]嘧啶氨基酸衍生物及其用途
CN112979654B (zh) * 2019-12-16 2024-03-19 赛诺哈勃药业（成都）有限公司 杂芳基稠环化合物、其制备方法及应用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021187878A1 (ko) * 2020-03-17 2021-09-23 제이투에이치바이오텍 주식회사 변이성 trk 융합 단백질 억제용 화합물, 이의 의약 용도 및 제조 방법
CN113563343B (zh) * 2020-07-27 2022-05-24 杭州邦顺制药有限公司 取代的吡唑并[1,5-a]嘧啶化合物及其用途
CN114276352A (zh) * 2020-10-13 2022-04-05 上海健康医学院 一种碳-11标记Larotrectinib化合物及其制备方法
WO2022168115A1 (en) 2021-02-05 2022-08-11 Mylan Laboratories Limited A process for the preparation of larotrectinib or its salts
IT202100003887A1 (it) 2021-02-19 2022-08-19 Olon Spa Procedimento per la preparazione di larotrectinib ad elevato grado di purezza
CN116120322B (zh) * 2021-11-15 2024-11-15 石药集团中奇制药技术（石家庄）有限公司 氮杂稠环酰胺类化合物的盐、其结晶形式及其用途
CN116003469B (zh) * 2022-03-23 2023-10-17 南京知和医药科技有限公司 嘧啶基抗病毒化合物的制备与使用方法
CN114907315B (zh) * 2022-05-17 2023-09-12 重庆医科大学 Selitrectinib中间体的合成方法
CN117343064B (zh) * 2022-07-05 2024-04-16 南京知和医药科技有限公司 一种具有抗病毒作用的嘧啶衍生物的制备与应用
WO2024023836A1 (en) 2022-07-27 2024-02-01 Mylan Laboratories Limited Polymorphic form of larotrectinib sulfate
CN117659043A (zh) 2022-09-07 2024-03-08 苏州朗睿生物医药有限公司 一种大环咪唑并[1,2-b]哒嗪衍生物及其制备方法和用途
EP4382529A1 (en) 2022-12-07 2024-06-12 Bayer Consumer Care AG A process for preparing pure (3s)-pyrrolidin-3-ol and pure (3s)-pyrrolidin-3-ol hydrochloride
WO2024242416A1 (ko) * 2023-05-22 2024-11-28 주식회사 셀러스 신규한 cdk7 억제 화합물 및 이의 용도
WO2025014639A2 (en) * 2023-07-07 2025-01-16 The Johns Hopkins University Neutral sphingomyelinase inhibitors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006087538A1 (en) 2005-02-16 2006-08-24 Astrazeneca Ab Chemical compounds

Family Cites Families (199)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1017286A (en) 1909-03-01 1912-02-13 Du Pont Powder Co Apparatus for treating explosive powder.
US1001160A (en) 1910-04-05 1911-08-22 Paul A Otto Aerodrome.
US1004709A (en) 1910-05-20 1911-10-03 Albert E Yerkes Spraying device.
US1013712A (en) 1911-06-03 1912-01-02 Alfred D Williams Tie and rail-fastener.
NZ234143A (en) 1989-06-28 1991-10-25 Mcneil Ppc Inc Aqueous pharmaceutical suspension formulation for administering substantially insoluble pharmaceutical agents
GB9212308D0 (en) 1992-06-10 1992-07-22 Ici Plc Therapeutic compositions
NZ276885A (en) 1993-11-30 1999-08-30 Searle & Co Substituted pyrazolyl-benzenesulphonamide derivatives, preparation and pharmaceutical compositions thereof
US5844092A (en) 1994-03-18 1998-12-01 Genentech, Inc. Human TRK receptors and neurotrophic factor inhibitors
US5877016A (en) 1994-03-18 1999-03-02 Genentech, Inc. Human trk receptors and neurotrophic factor inhibitors
US5430021A (en) 1994-03-18 1995-07-04 Pharmavene, Inc. Hydrophobic drug delivery systems
US6458811B1 (en) 1996-03-26 2002-10-01 Eli Lilly And Company Benzothiophenes formulations containing same and methods
CA2206201A1 (en) 1996-05-29 1997-11-29 Yoshiaki Isobe Pyrazole derivatives and their pharmaceutical use
JPH1020683A (ja) 1996-07-05 1998-01-23 Fuji Xerox Co Ltd 画像形成装置
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
US6248740B1 (en) 1997-04-25 2001-06-19 Takeda Chemical Industries, Ltd. Condensed pyridazine derivatives, their production and use
UA67825C2 (uk) 1999-01-21 2004-07-15 Брістол-Майерс Сквібб Ко. КОМПЛЕКС ІНГІБІТОРА RAS-ФАРНЕЗИЛТРАНСФЕРАЗИ ТА ПРОСТОГО СУЛЬФОБУТИЛОВОГО ЕФІРУ 7-<font face="Symbol">b</font>-ЦИКЛОДЕКСТРИНУ АБО 2-ГІДРОКСИПРОПІЛ-<font face="Symbol">b</font>-ЦИКЛОДЕКСТРИНУ, КОМПОЗИЦІЯ ІНГІБІТОРА RAS-ФАРНЕЗИЛТРАНСФЕРАЗИ ТА ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ
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
US6534085B1 (en) 1999-09-23 2003-03-18 Bioresponse L.L.C. Phytochemicals for promoting weight loss
PL208113B1 (pl) 2000-06-22 2011-03-31 Genentech Inc Agonistyczne przeciwciało monoklonalne anty-trkC, mysie agonistyczne przeciwciało monoklonalne, ludzkie agonistyczne przeciwciało monoklonalne, wyizolowana cząsteczka kwasu nukleinowego kodująca mysie agonistyczne przeciwciało monoklonalne, wyizolowana cząsteczka kwasu nukleinowego kodująca ludzkie przeciwciało anty-trkC, cząsteczka kwasu nukleinowego, linia komórek gospodarza, linia komórek hybrydomy, przeciwciało wytwarzane przez tę linię komórek hybrydomy, wyizolowana cząsteczka kwasu nukleinowego i wektor zawierający tę cząsteczkę kwasu nukleinowego, przeciwciało, polipeptyd, kompozycja
GB0028575D0 (en) 2000-11-23 2001-01-10 Elan Corp Plc Oral pharmaceutical compositions containing cyclodextrins
CA2432008A1 (en) 2000-12-22 2002-07-04 Astrazeneca Ab Carbazole derivatives and their use as neuropeptide y5 receptor ligands
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
WO2002096458A1 (en) 2001-05-30 2002-12-05 Genentech, Inc. Anti-ngf antibodies for the treatment of various disorders
US7101572B2 (en) 2001-12-07 2006-09-05 Unilab Pharmatech, Ltd. Taste masked aqueous liquid pharmaceutical composition
US20030199525A1 (en) 2002-03-21 2003-10-23 Hirst Gavin C. Kinase inhibitors
MXPA04010441A (es) * 2002-04-23 2005-02-14 Shionogi & Co Derivado de pirazolo[1,5-a]pirimidina e inhibidor de nad(p)h oxidasa que contiene el mismo.
US7449488B2 (en) * 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
US6982253B2 (en) 2002-06-05 2006-01-03 Supergen, Inc. Liquid formulation of decitabine and use of the same
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
DK1537116T3 (da) * 2002-09-04 2010-09-27 Schering Corp Pyrazolopyrimidiner egnede til behandling af cancersygdomme
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7119200B2 (en) 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7262199B2 (en) 2002-12-11 2007-08-28 Merck & Co., Inc. Tyrosine kinase inhibitors
AU2003299651A1 (en) 2002-12-11 2004-06-30 Merck And Co., Inc. 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
US20070179161A1 (en) 2003-03-31 2007-08-02 Vernalis (Cambridge) Limited. Pyrazolopyrimidine compounds and their use in medicine
JP2006522744A (ja) 2003-04-11 2006-10-05 ノボ　ノルディスク　アクティーゼルスカブ グルココルチコイド受容体アゴニスト療法に伴う副作用を最小化するための、１１β−ヒドロキシステロイドデヒドロゲナーゼ１型阻害剤およびグルココルチコイド受容体アゴニストを使用する併用療法
EP1615697A2 (en) 2003-04-11 2006-01-18 Novo Nordisk A/S New pyrazolo[1,5-a] pyrimidine derivatives and pharmaceutical use thereof
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
KR20060011977A (ko) 2003-04-28 2006-02-06 가르파마 컴퍼니 리미티드 갈렉틴 9 유도 인자
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
EA009517B1 (ru) 2003-06-27 2008-02-28 Байер Кропсайенс Аг Пиразолопиримидины
TWI503328B (zh) 2003-07-15 2015-10-11 Amgen Inc 作為選擇性神經生長因子（ｎｇｆ）通道抑制劑之人類抗-ｎｇｆ中和抗體
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
CA2549869C (en) 2003-12-18 2015-05-05 Janssen Pharmaceutica N.V. Pyrido- and pyrimidopyrimidine derivatives as anti- proliferative agents
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
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
CN101119996A (zh) * 2005-02-16 2008-02-06 阿斯利康(瑞典)有限公司 化学化合物
PT1869049E (pt) 2005-03-21 2009-05-26 Lilly Co Eli Compostos de imidazopiridazina
JP2008540335A (ja) 2005-04-27 2008-11-20 アストラゼネカ・アクチエボラーグ ピラゾリル・ピリミジン誘導体の疼痛治療における使用
US20080287437A1 (en) 2005-05-16 2008-11-20 Astrazeneca Ab Pyrazolylaminopyrimidine Derivatives Useful as Tyrosine Kinase Inhibitors
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.
US20070025540A1 (en) 2005-07-07 2007-02-01 Roger Travis Call center routing based on talkativeness
NZ565059A (en) 2005-07-25 2011-08-26 Intermune Inc Novel macrocyclic inhibitors of hepatitus C virus replication
US20100216798A1 (en) * 2005-07-29 2010-08-26 Astellas Pharma Inc Fused heterocycles as lck inhibitors
CN101232871A (zh) 2005-08-03 2008-07-30 伊士曼化工公司 生育酚聚乙二醇琥珀酸酯粉末及其制备方法
US20070191306A1 (en) 2005-08-17 2007-08-16 Bristol-Myers Squibb Company FACTOR Xa INHIBITOR FORMULATION AND METHOD
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
HRP20140218T4 (hr) 2005-08-25 2017-06-16 Creabilis Therapeutics S.P.A. Polimerni konjugati k-252a i njihovi derivati
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
US20070082900A1 (en) * 2005-10-06 2007-04-12 Schering Corporation Methods for inhibiting protein kinases
CA2624500A1 (en) 2005-10-06 2007-04-19 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
ATE519757T1 (de) 2005-10-11 2011-08-15 Centre Nat Rech Scient 3 hydroxyflavon-derivate zur erkennung und quantifizierung von zell-apoptosen
BRPI0617274A2 (pt) 2005-10-11 2011-07-19 Intermune Inc compostos e métodos para a inibição de replicação viral de hepatite c
CA2626742A1 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators
GB0524436D0 (en) 2005-11-30 2006-01-11 Novartis Ag Organic compounds
US20070166336A1 (en) 2005-12-13 2007-07-19 David Delmarre Stable and palatable oral liquid sumatriptan compositions
US20080108611A1 (en) 2006-01-19 2008-05-08 Battista Kathleen A Substituted thienopyrimidine kinase inhibitors
KR100846988B1 (ko) 2006-03-06 2008-07-16 제일약품주식회사 신규한 티에노피리미딘 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 함유하는 약학조성물
JP2009529047A (ja) 2006-03-07 2009-08-13 アレイ バイオファーマ、インコーポレイテッド ヘテロ二環系ピラゾール化合物およびその使用
GB0606805D0 (en) 2006-04-04 2006-05-17 Novartis Ag Organic compounds
PT2024372E (pt) 2006-04-26 2010-09-16 Hoffmann La Roche Derivado de tieno[3,2-d]pirimidina útil como inibidor de pi3k
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
US8044049B2 (en) 2006-08-04 2011-10-25 Takeda Pharmaceutical Company Limited Fused heterocyclic derivative and use thereof
WO2008016131A1 (en) * 2006-08-04 2008-02-07 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
US7531539B2 (en) 2006-08-09 2009-05-12 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
AU2007292924A1 (en) 2006-09-07 2008-03-13 Biogen Idec Ma Inc. IRAK modulators for treating an inflammatory condition, cell proliferative disorder, immune disorder
MX2009003185A (es) * 2006-09-29 2009-04-03 Novartis Ag Pirazolopirimidinas como inhibidores de lipido cinasa pi3k.
CN101522682A (zh) * 2006-10-30 2009-09-02 诺瓦提斯公司 作为抗炎剂的杂环化合物
CN101600718B (zh) 2006-11-06 2013-07-03 特雷罗药物股份有限公司 咪唑并[1,2-b]哒嗪和吡唑并[1,5-a]嘧啶衍生物及其作为蛋白激酶抑制剂的用途
US7820684B2 (en) 2007-03-01 2010-10-26 Supergen, Inc. Pharmaceutical formulations comprising salts of a protein kinase inhibitor and methods of using same
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
WO2008124323A1 (en) 2007-04-03 2008-10-16 Array Biopharma Inc. Imidazo[1,2-a]pyridine compounds as receptor tyrosine kinase inhibitors
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
WO2008155421A2 (en) 2007-06-21 2008-12-24 Janssen Pharmaceutica Nv Indolin-2-ones and aza-indolin-2-ones
US8299057B2 (en) 2007-07-20 2012-10-30 Nerviano Medical Sciences S.R.L. Substituted indazole derivatives active as kinase inhibitors
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
MY161564A (en) 2007-08-10 2017-04-28 Regeneron Pharma High affinity human antibodies to human nerve growth factor
WO2009052145A1 (en) 2007-10-16 2009-04-23 Wyeth Thienopyrimidine and pyrazolopyrimidine compounds and their use as mtor kinase and pi3 kinase inhibitors
JP2011501760A (ja) 2007-10-23 2011-01-13 ノバルティス アーゲー 呼吸器疾患の処置のためのｔｒｋｂ抗体の使用
US20110046127A1 (en) 2007-11-08 2011-02-24 Paolo Pevarello 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
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
AU2009205937B2 (en) 2008-01-17 2013-02-07 Novartis Ag Improved anti-TrkB antibodies
WO2009109547A1 (en) 2008-03-03 2009-09-11 Ucb Pharma, S.A. Pharmaceutical solutions, process of preparation and therapeutic uses
KR100963051B1 (ko) 2008-03-14 2010-06-09 광동제약 주식회사 입자크기가 조절된 술포데히드로아비에트산을 함유한쓴맛이 저감된 경구용 액상 조성물
US20090275622A1 (en) 2008-04-30 2009-11-05 Prasoona Linga Nizatidine formulations
EP2300469B1 (en) * 2008-05-13 2015-06-24 Novartis AG Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors
WO2010012733A1 (en) 2008-07-29 2010-02-04 Nerviano Medical Sciences S.R.L. Use of a cdk inhibitor for the treatment of glioma
RS53350B (sr) 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze
PT2725028T (pt) 2008-10-22 2016-08-31 Array Biopharma Inc Compostos de pirazolo[1,5-]pirimidina substituídos como intermediários na síntese de inibidores de cinase trk
BRPI0914404A2 (pt) 2008-10-31 2019-03-06 Genentech Inc "compostos, composição farmacêutica e método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak quinase em um paciente"
WO2010058006A1 (en) 2008-11-24 2010-05-27 Nerviano Medical Sciences S.R.L. Cdk inhibitor for the treatment of mesothelioma
PL2881402T3 (pl) 2009-02-12 2017-10-31 Cell Signaling Technology Inc Ekspresja zmutowanej ROS w ludzkim raku wątroby
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011084486A1 (en) 2009-12-21 2011-07-14 Epitherix, Llc 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
ES2594927T3 (es) 2010-02-18 2016-12-23 INSERM (Institut National de la Santé et de la Recherche Médicale) Métodos para prevenir las metástasis cancerosas
CA2795776A1 (en) 2010-04-06 2011-10-13 Caris Life Sciences Luxembourg Holdings, S.A.R.L. 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
HUE044025T2 (hu) 2010-05-20 2019-09-30 Array Biopharma Inc Makrociklusos vegyületek mint TRK-kináz inhibitorok
EP2580322B1 (en) 2010-06-09 2018-01-10 Dana-Farber Cancer Institute, Inc. A mek 1 mutation conferring resistance to raf and mek inhibitors
EP3333188B1 (en) 2010-08-19 2022-02-09 Zoetis Belgium S.A. Anti-ngf antibodies and their use
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
EP3434691A1 (en) 2010-12-01 2019-01-30 AlderBio Holdings LLC Anti-ngf compositions and use thereof
GEP20156285B (en) 2011-02-25 2015-05-11 Aierem Elelsi Compounds and compositions as trk inhibitors
UA114711C2 (uk) 2011-05-13 2017-07-25 Еррей Біофарма Інк. Сполуки піролідинілсечовини й піролідинілтіосечовини як інгібітори кінази trka
WO2013059740A1 (en) 2011-10-21 2013-04-25 Foundation Medicine, Inc. Novel alk and ntrk1 fusion molecules and uses thereof
MX2014005632A (es) 2011-11-14 2014-10-17 Tesaro Inc Modulacion de ciertas cinasas de tirosina.
MX356401B (es) 2011-12-12 2018-05-21 Dr Reddys Laboratories Ltd Pirazol[1,5-a]piridina sustituida como inhibidores de la cinasa del receptor de tropomiosina (trk).
WO2013161919A1 (ja) 2012-04-26 2013-10-31 小野薬品工業株式会社 Ｔｒｋ阻害化合物
NZ716487A (en) 2012-05-23 2017-01-27 Nerviano Medical Sciences Srl Process for the preparation of n-[5-(3,5-difluoro-benzyl)-1h-indazol-3-yl]-4-(4-methyl-piperazin-1-yl)-2-(tetrahydro-pyran-4-ylamino)-benzamide
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
ES2600628T3 (es) 2012-06-28 2017-02-10 Johnson & Johnson Consumer Inc. Composición líquida de racecadotril
EP3550031A1 (en) 2012-07-24 2019-10-09 Pharmacyclics, LLC Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
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
US20140084039A1 (en) 2012-09-24 2014-03-27 Electro Scientific Industries, Inc. Method and apparatus for separating workpieces
JP2014082984A (ja) 2012-10-23 2014-05-12 Astellas Pharma Inc 新規ｎｔｒｋ２活性化変異の検出法
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
EP2922844B1 (en) 2012-11-13 2018-01-10 Array Biopharma, Inc. N-pyrrolidinyl, 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
US9790178B2 (en) 2012-11-13 2017-10-17 Array Biopharma Inc. Pyrrolidinyl 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
HRP20161613T1 (hr) 2012-11-13 2017-01-13 Array Biopharma, Inc. Tvari bicikličke ureje, tioureje, gvanidina i cijanogvanidina korisne za liječenje boli
US9790210B2 (en) 2012-11-13 2017-10-17 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
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US20150290233A1 (en) 2012-11-29 2015-10-15 Yeda Research And Development Co.Ltd. At The Weizmann Institute Of Science Methods of preventing tumor metastasis, treating and prognosing cancer and identifying agents which are putative metastasis inhibitors
US9127055B2 (en) 2013-02-08 2015-09-08 Astellas Pharma Inc. Method of treating pain with anti-human NGF antibody
EP2960234B1 (en) 2013-02-19 2018-12-19 ONO Pharmaceutical Co., Ltd. Trk-inhibiting compound
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
ES2900301T3 (es) 2013-03-15 2022-03-16 Novartis Ag Biomarcadores asociados con la inhibición de BRM
EP2968551B1 (en) 2013-03-15 2021-05-05 The Trustees of Columbia University in the City of New York Fusion proteins and methods thereof
ES3042844T3 (en) 2013-03-15 2025-11-24 Univ Leland Stanford Junior 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
CN118910253A (zh) 2013-04-17 2024-11-08 生命技术公司 与癌症相关的基因融合体和基因变异体
TWI610923B (zh) 2013-07-11 2018-01-11 Betta Pharmaceuticals Co Ltd 酪氨酸蛋白激酶調節劑及其應用方法
WO2015012397A1 (ja) 2013-07-26 2015-01-29 公益財団法人がん研究会 Ｎｔｒｋ３融合体の検出法
EP3027655B1 (en) 2013-07-30 2019-08-21 Blueprint Medicines Corporation Ntrk2 fusions
KR20160065986A (ko) 2013-10-24 2016-06-09 조지타운 유니버시티 암 치료용 방법 및 조성물
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
CN110317214B (zh) 2014-01-24 2022-11-22 特普医药公司 作为蛋白质激酶的调节剂的二芳基巨环
WO2015120136A1 (en) 2014-02-05 2015-08-13 VM Oncology LLC Compositions of compounds and uses thereof
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
RU2719489C2 (ru) 2014-05-15 2020-04-17 Эррэй Биофарма Инк. 1-((3S,4R)-4-(3-ФТОРФЕНИЛ)-1-(2-МЕТОКСИЭТИЛ)ПИРРОЛИДИН-3-ИЛ)-3-(4-МЕТИЛ-3-(2-МЕТИЛПИРИМИДИН-5-ИЛ)-1-ФЕНИЛ-1Н-ПИРАЗОЛ-5-ИЛ)МОЧЕВИНА В КАЧЕСТВЕ ИНГИБИТОРА TrkA КИНАЗЫ
WO2015183837A1 (en) 2014-05-27 2015-12-03 Brian Haynes Compositions, methods, and uses related to ntrk2-tert fusions
WO2015184443A1 (en) 2014-05-30 2015-12-03 The Regents Of The University Of Colorado Activating ntrk1 gene fusions predictive of kinase inhibitor therapy
AU2015296010A1 (en) 2014-08-01 2017-02-02 Pharmacyclics Llc Biomarkers for predicting response of DLBCL to treatment with a BTK inhibitor
TWI560185B (en) 2014-08-18 2016-12-01 Ono Pharmaceutical Co Acid addition salt of trk inhibitor compound
CA2964367C (en) 2014-10-14 2024-01-30 Novartis Ag Antibody molecules to pd-l1 and uses thereof
FI3699181T3 (fi) 2014-11-16 2023-03-28 Array Biopharma Inc Kiteinen muoto (s)-n-(5-((r)-2-(2,5-diluorifenyyli)-pyrrolidin-1-yyli)-pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidivetyysulfaatista
AU2015365587B2 (en) 2014-12-15 2020-07-23 Cmg Pharmaceutical Co., Ltd. Fused ring heteroaryl compounds and their use as TRK inhibitors
CN104672121B (zh) 2015-02-16 2017-10-24 上海华默西医药科技有限公司 2r‑(2,5‑二氟苯基)吡咯烷盐酸盐的制备方法
IL302102A (en) 2015-05-20 2023-06-01 Dana Farber Cancer Inst Inc shared neoantigens
EP3303382A4 (en) 2015-05-29 2018-12-19 Ignyta, Inc. Compositions and methods for treating patients with rtk mutant cells
MX2017015461A (es) 2015-06-01 2018-08-15 Loxo Oncology Inc Métodos para diagnosticar y tratar el cáncer.
US9782400B2 (en) 2015-06-19 2017-10-10 Macau University Of Science And Technology Oncogenic ROS1 and ALK kinase inhibitor
AU2015101722A4 (en) 2015-06-19 2016-05-19 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
JP6871903B2 (ja) 2015-07-02 2021-05-19 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Ｔｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． プロテインキナーゼのモジュレーターとしてのキラルジアリール大環状分子
EP3368039A1 (en) 2015-10-26 2018-09-05 The Regents of The University of Colorado, A Body Corporate Point mutations in trk inhibitor-resistant cancer and methods relating to the same
WO2017127835A2 (en) 2016-01-22 2017-07-27 The Medicines Company Aqueous formulations and methods of preparation and use thereof
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
RS65987B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Tečne formulacije (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)-pirazolo[1,5-]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
CA3019661A1 (en) 2016-04-04 2017-10-12 Loxo Oncology, Inc. Methods of treating pediatric cancers
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CA3021445A1 (en) 2016-04-19 2017-10-26 Exelixis, Inc. Triple negative breast cancer treatment method
EP3800189B1 (en) 2016-05-18 2023-06-28 Loxo Oncology, Inc. Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
WO2017201156A1 (en) 2016-05-18 2017-11-23 Duke University Method of treating kras wild-type metastatic colorectal cell carcinoma using cabozantinib plus panitumumab
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
US20190247398A1 (en) 2017-10-26 2019-08-15 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
WO2019191659A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006087538A1 (en) 2005-02-16 2006-08-24 Astrazeneca Ab Chemical compounds

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