JP2014514360A5 - - Google Patents

Download PDF

Info

Publication number
JP2014514360A5
JP2014514360A5 JP2014510416A JP2014510416A JP2014514360A5 JP 2014514360 A5 JP2014514360 A5 JP 2014514360A5 JP 2014510416 A JP2014510416 A JP 2014510416A JP 2014510416 A JP2014510416 A JP 2014510416A JP 2014514360 A5 JP2014514360 A5 JP 2014514360A5
Authority
JP
Japan
Prior art keywords
alkyl
alkoxy
independently selected
optionally substituted
compound
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
JP2014510416A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014514360A (ja
JP5933902B2 (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2012/037003 external-priority patent/WO2012158413A2/en
Publication of JP2014514360A publication Critical patent/JP2014514360A/ja
Publication of JP2014514360A5 publication Critical patent/JP2014514360A5/ja
Application granted granted Critical
Publication of JP5933902B2 publication Critical patent/JP5933902B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2014510416A 2011-05-13 2012-05-09 Trkaキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物 Active JP5933902B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161485858P 2011-05-13 2011-05-13
US61/485,858 2011-05-13
PCT/US2012/037003 WO2012158413A2 (en) 2011-05-13 2012-05-09 Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2016026184A Division JP6382867B2 (ja) 2011-05-13 2016-02-15 Trkaキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物

Publications (3)

Publication Number Publication Date
JP2014514360A JP2014514360A (ja) 2014-06-19
JP2014514360A5 true JP2014514360A5 (enExample) 2015-05-21
JP5933902B2 JP5933902B2 (ja) 2016-06-15

Family

ID=46614580

Family Applications (4)

Application Number Title Priority Date Filing Date
JP2014510416A Active JP5933902B2 (ja) 2011-05-13 2012-05-09 Trkaキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物
JP2016026184A Active JP6382867B2 (ja) 2011-05-13 2016-02-15 Trkaキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物
JP2017090432A Withdrawn JP2017171672A (ja) 2011-05-13 2017-04-28 Trkaキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物
JP2018172485A Pending JP2019001819A (ja) 2011-05-13 2018-09-14 Trkaキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物

Family Applications After (3)

Application Number Title Priority Date Filing Date
JP2016026184A Active JP6382867B2 (ja) 2011-05-13 2016-02-15 Trkaキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物
JP2017090432A Withdrawn JP2017171672A (ja) 2011-05-13 2017-04-28 Trkaキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物
JP2018172485A Pending JP2019001819A (ja) 2011-05-13 2018-09-14 Trkaキナーゼ阻害剤としてのピロリジニル尿素およびピロリジニルチオ尿素化合物

Country Status (35)

Country Link
US (4) US9562055B2 (enExample)
EP (1) EP2712358B1 (enExample)
JP (4) JP5933902B2 (enExample)
KR (2) KR102001364B1 (enExample)
CN (3) CN108329246B (enExample)
AR (1) AR086367A1 (enExample)
AU (2) AU2012256237B2 (enExample)
BR (1) BR112013029201B1 (enExample)
CA (1) CA2835835C (enExample)
CL (1) CL2013003257A1 (enExample)
CO (1) CO6821961A2 (enExample)
CR (1) CR20130646A (enExample)
CY (1) CY1119014T1 (enExample)
DK (1) DK2712358T3 (enExample)
ES (1) ES2615738T3 (enExample)
HR (1) HRP20161786T1 (enExample)
HU (1) HUE030791T2 (enExample)
IL (2) IL229377A (enExample)
LT (1) LT2712358T (enExample)
ME (1) ME02583B (enExample)
MX (2) MX369142B (enExample)
MY (1) MY173181A (enExample)
NZ (1) NZ618795A (enExample)
PH (1) PH12013502319A1 (enExample)
PL (1) PL2712358T3 (enExample)
PT (1) PT2712358T (enExample)
RS (1) RS55582B1 (enExample)
RU (1) RU2606131C2 (enExample)
SG (2) SG194902A1 (enExample)
SI (1) SI2712358T1 (enExample)
SM (2) SMT201700035T1 (enExample)
TW (2) TWI649315B (enExample)
UA (1) UA114711C2 (enExample)
UY (1) UY34067A (enExample)
WO (1) WO2012158413A2 (enExample)

Families Citing this family (96)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2116539A1 (en) 2008-04-25 2009-11-11 Laboratorios Del. Dr. Esteve, S.A. 1-aryl-3-aminoalkoxy-pyrazoles as sigma ligands enhancing analgesic effects of opioids and attenuating the dependency thereof
SI2350075T1 (sl) 2008-09-22 2014-06-30 Array Biopharma, Inc. Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji
CN102264736B (zh) 2008-10-22 2013-08-14 阵列生物制药公司 作为TRK激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
EP2353598A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for use in the prevention and/or treatment of postoperative pain
EP2353591A1 (en) 2010-02-04 2011-08-10 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for potentiating the analgesic effect of opioids and opiates in post-operative pain and attenuating the dependency thereof
BR122019024201B1 (pt) 2010-05-20 2021-08-03 Array Biopharma Inc Composto macrocíclico como inibidores de trk quinase, seu uso, e composição farmacêutica
EP2388005A1 (en) 2010-05-21 2011-11-23 Laboratorios Del. Dr. Esteve, S.A. Sigma ligands for the prevention and/or treatment of emesis induced by chemotherapy or radiotherapy
EP2415471A1 (en) 2010-08-03 2012-02-08 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in opioid-induced hyperalgesia
NZ618795A (en) 2011-05-13 2015-07-31 Array Biopharma Inc Pyrrolidinyl urea, pyrrolidinyl thiourea and pyrrolidinyl guanidine compounds as trka kinase inhibitors
EP2524694A1 (en) 2011-05-19 2012-11-21 Laboratorios Del. Dr. Esteve, S.A. Use of sigma ligands in diabetes type-2 associated pain
WO2014078417A1 (en) * 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrazolyl 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
WO2014078372A1 (en) * 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl 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
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
CA2891334C (en) 2012-11-13 2021-10-19 Array Biopharma Inc. Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
ME02990B (me) * 2012-11-13 2018-10-20 Array Biopharma Inc Jedinjenja n-pirolidinil, n'-pirazolil- uree, tiouree, guanidina i cijanoguanidina kао inhibitori trka kinaze
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
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
MX2015009270A (es) 2013-01-18 2015-10-30 Hoffmann La Roche Pirazoles sustituidos en posicion 3 y uso de los mismos como inhibidores de la cinasa cremallera de leucinas dual (dlk).
EP2818166A1 (en) * 2013-06-26 2014-12-31 Laboratorios del Dr. Esteve S.A. Use of sigma receptor ligands for the prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (IC/BPS)
WO2015039333A1 (en) * 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
WO2015039334A1 (en) 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
EP3305763B1 (en) 2013-11-28 2019-07-24 Kyorin Pharmaceutical Co., Ltd. Deuterated or isotopically labeled urea derivatives or pharmacologically acceptable salts thereof useful as fprl-1 agonists
SG11201604480PA (en) 2013-12-17 2016-07-28 Esteve Labor Dr SEROTONIN-NOREPINEPHRINE REUPTAKE INHIBITORS (SNRIs) AND SIGMA RECEPTOR LIGANDS COMBINATIONS
CN105829296A (zh) 2013-12-18 2016-08-03 巴斯夫欧洲公司 带有亚胺衍生的取代基的唑类化合物
JP2016540811A (ja) 2013-12-20 2016-12-28 ファイザー・リミテッドPfizer Limited N−アシルピペリジンエーテルトロポミオシン関連キナーゼ阻害剤
WO2015143653A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143652A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143654A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
US20170197939A1 (en) 2014-04-15 2017-07-13 Pfizer Inc. Tropomyosin-Related Kinase Inhibitors Containing Both A 1H-Pyrazole And A Pyrimidine Moiety
EP3140298A1 (en) 2014-05-07 2017-03-15 Pfizer Inc. Tropomyosin-related kinase inhibitors
CN106459013B (zh) * 2014-05-15 2019-10-25 阵列生物制药公司 作为trka激酶抑制剂的化合物及其用途
WO2016009296A1 (en) 2014-07-16 2016-01-21 Pfizer Inc. N-acylpiperidine ether tropomyosin-related kinase inhibitors
WO2016020784A1 (en) 2014-08-05 2016-02-11 Pfizer Inc. N-acylpyrrolidine ether tropomyosin-related kinase inhibitors
WO2016021629A1 (ja) * 2014-08-06 2016-02-11 塩野義製薬株式会社 TrkA阻害活性を有する複素環および炭素環誘導体
TWI746426B (zh) 2014-11-16 2021-11-21 美商亞雷生物製藥股份有限公司 (S)-N-(5-((R)-2-(2,5-二氟苯基)-吡咯啶-1-基)-吡唑并[1,5-a]嘧啶-3-基)-3-羥基吡咯啶-1-甲醯胺硫酸氫鹽結晶型
BR112017009701B1 (pt) 2014-12-08 2021-09-08 Fmc Corporation Composto e métodos de preparação de compostos
WO2016161572A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
AU2016266190A1 (en) * 2015-05-27 2018-01-18 Kyorin Pharmaceutical Co., Ltd. Urea derivative or pharmacologically acceptable salt thereof
HK1253093A1 (zh) 2015-06-01 2019-06-06 Loxo Oncology Inc. 诊断和治疗癌症的方法
US10640495B2 (en) 2015-07-07 2020-05-05 Shionogi & Co., Ltd. Heterocycle derivatives having TrkA inhibitory activity
CA2992586A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
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
WO2017108569A1 (en) 2015-12-22 2017-06-29 Syngenta Participations Ag Pesticidally active pyrazole derivatives
WO2017135399A1 (ja) * 2016-02-04 2017-08-10 塩野義製薬株式会社 TrkA阻害活性を有する含窒素複素環および炭素環誘導体
UA125025C2 (uk) 2016-04-04 2021-12-29 Локсо Онколоджі, Інк. Способи лікування дитячих ракових захворювань
UA125026C2 (uk) 2016-04-04 2021-12-29 Локсо Онколоджі, Інк. РІДКІ КОМПОЗИЦІЇ (S)-N-(5-((R)-2-(2,5-ДИФТОРФЕНІЛ)ПІРОЛІДИН-1-ІЛ)ПІРАЗОЛО[1,5-a]ПІРИМІДИН-3-ІЛ)-3-ГІДРОКСИПІРОЛІДИН-1-КАРБОКСАМІДУ
MX392604B (es) 2016-05-18 2025-03-24 Array Biopharma Inc Procesos para la preparacion de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo.
TWI752098B (zh) 2016-10-10 2022-01-11 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
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
JP6888101B2 (ja) 2017-01-18 2021-06-16 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ロ[1,5−a]ピラジン化合物
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
WO2018185187A1 (en) 2017-04-05 2018-10-11 Syngenta Participations Ag Pesticidally active pyrazole derivatives
US11071300B2 (en) 2017-06-19 2021-07-27 Syngenta Participations Ag Pesticidally active pyrazole derivatives
JP2019026646A (ja) * 2017-08-03 2019-02-21 塩野義製薬株式会社 含窒素複素環および炭素環誘導体を含有する、疼痛の治療および/または予防用医薬組成物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
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
CA3080157A1 (en) 2017-10-26 2019-05-02 Array Biopharma Inc. Formulations of a macrocyclic trk kinase inhibitor
CN111433198A (zh) * 2017-11-17 2020-07-17 合帕吉恩治疗公司 作为ask1的抑制剂的脲衍生物
CN111630054B (zh) 2018-01-18 2023-05-09 奥瑞生物药品公司 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物
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
WO2019173182A1 (en) 2018-03-05 2019-09-12 Bristol-Myers Squibb Company Phenylpyrrolidinone formyl peptide 2 receptor agonists
EP3773725A1 (en) 2018-03-29 2021-02-17 Loxo Oncology Inc. Treatment of trk-associated cancers
TWI873098B (zh) 2018-07-03 2025-02-21 瑞士商諾華製藥公司 用於治療與sting活性相關之病症的化合物及組合物
CN112424189B (zh) * 2018-07-12 2023-07-07 漳州片仔癀药业股份有限公司 吡咯烷基脲衍生物及其在TrkA相关疾病的应用
GB201811825D0 (en) 2018-07-19 2018-09-05 Benevolentai Bio Ltd Organic compounds
CA3108065C (en) 2018-07-31 2025-10-07 Loxo Oncology, Inc. SPRAY-DRIED DISPERSIONS, FORMULATIONS AND POLYMORPHIES OF (S)-5-AMINO-3-(4-((5-FLUORO-2-METHOXYBENZAMIDO)METHYL)PHENYL)(1,1,1-TRIFLUOROPROPANE-2-YL)-1H-PYRAZOLE-4-CARBOXAMIDE
GB201813791D0 (en) 2018-08-23 2018-10-10 Benevolental Bio Ltd Organic compounds
ES2922314T3 (es) 2018-09-10 2022-09-13 Array Biopharma Inc Compuestos heterocíclicos condensados como inhibidores de cinasa RET
US12351571B2 (en) 2018-12-19 2025-07-08 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases
WO2020131627A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
WO2020127345A1 (en) 2018-12-21 2020-06-25 Syngenta Participations Ag Pesticidally active pyrazole derivatives
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
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
US12630543B2 (en) 2019-11-14 2026-05-19 Unimatec Co., Ltd. Fluorine-containing pyrazole compound and method for producing same
EP4089087B1 (en) * 2020-01-10 2024-07-03 Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. Method for preparing pyrrolidinyl urea derivative
JP7289017B2 (ja) * 2020-01-10 2023-06-08 ▲ザン▼州片仔▲ファン▼薬業股▲フン▼有限公司 ピロリジニルウレア誘導体の結晶及びその使用
IL294688A (en) 2020-01-22 2022-09-01 Benevolentai Bio Ltd Pharmaceutical compositions and their uses
AU2021209418A1 (en) 2020-01-22 2022-07-21 Benevolentai Bio Limited Topical pharmaceutical compositions comprising imidazo[1,2-b]pyridazine compounds
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2022003377A1 (en) 2020-07-02 2022-01-06 Uni-Pharma Kleon Tsetis Pharmaceutical Laboratories S.A. Thieno[3,4-c]pyrazol-3-yl acetamides as autotaxin inhibitors
JP2024502474A (ja) 2021-01-08 2024-01-19 アイエフエム デュー インコーポレイテッド Sting活性に関連する状態を治療するための、尿素を有するヘテロ二環式化合物または類似体およびその組成物
WO2022150560A1 (en) * 2021-01-08 2022-07-14 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
US20240246955A1 (en) * 2021-04-12 2024-07-25 Cullgen (Shanghai), Inc. Tropomyosin receptor kinase (trk) degradation compounds and methods of use
EP4332092A4 (en) * 2021-04-27 2025-07-16 Unimatec Co Ltd FLUORINE-CONTAINING PYRAZOLE COMPOUND AND PROCESS FOR PRODUCTION THEREOF
WO2022234287A1 (en) 2021-05-06 2022-11-10 Benevolentai Bio Limited Imidazopyridazine derivatives useful as trk inhibitors
CN114031556B (zh) * 2021-11-08 2023-03-31 温州大学 一种绿色的一锅法制备5-氨基-n-芳基-3-芳基吡唑类化合物的合成方法
AU2022391025A1 (en) 2021-11-19 2024-06-06 The Brigham And Women's Hospital, Inc. Bifunctional chimeric molecules for labeling of kinases with target binding moieties and methods of use thereof
WO2024240213A1 (zh) * 2023-05-23 2024-11-28 上海海雁医药科技有限公司 稠合三环取代的异噁唑烷基脲衍生物、其药物组合物及应用
US11970499B1 (en) * 2023-12-22 2024-04-30 King Faisal University Pyrazolo[1,5-c]pyrimidine compounds as CK2 inhibitors

Family Cites Families (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS63198664A (ja) * 1986-03-31 1988-08-17 Sankyo Co Ltd キノロンカルボン酸誘導体
DE3906365A1 (de) * 1988-07-15 1990-01-18 Bayer Ag 7-(1-pyrrolidinyl)-3-chinolon- und -naphthyridoncarbonsaeure-derivate, verfahren sowie substituierte (oxa)diazabicyclooctane und -nonane als zwischenprodukte zu ihrer herstellung, und sie enthaltende antibakterielle mittel und futterzusatzstoffe
EP0561850B1 (en) * 1990-12-05 2000-07-12 NAEJA Pharmaceutical Inc. 7-substituted-6-fluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid compounds useful as antibacterial agents
JP3086837B2 (ja) * 1991-06-06 2000-09-11 三協化学株式会社 3−アミノピロリジン類の製造方法
NZ287139A (en) * 1994-06-14 1997-07-27 Dainippon Pharmaceutical Co Naphthyridine derivatives; preparative process and anti-tumour medicaments
NZ299242A (en) 1995-09-11 1997-12-19 Nihon Nohyaku Co Ltd N-phenyl-n'-(phenyl substituted imidazol-5-yl, -oxazol-4-yl, and -thiazol-4-yl)urea derivatives
CA2206201A1 (en) 1996-05-29 1997-11-29 Yoshiaki Isobe Pyrazole derivatives and their pharmaceutical use
US6083986A (en) 1996-07-26 2000-07-04 Icagen, Inc. Potassium channel inhibitors
US5998424A (en) 1997-06-19 1999-12-07 Dupont Pharmaceuticals Company Inhibitors of factor Xa with a neutral P1 specificity group
AU1367599A (en) 1997-11-03 1999-05-24 Boehringer Ingelheim Pharmaceuticals, Inc. Aromatic heterocyclic compounds as anti-inflammatory agents
IL136768A0 (en) 1997-12-22 2001-06-14 Bayer Ag INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
US6197798B1 (en) 1998-07-21 2001-03-06 Novartis Ag Amino-benzocycloalkane derivatives
KR100711538B1 (ko) 1998-12-25 2007-04-27 아스카 세이야쿠 가부시키가이샤 아미노피라졸 유도체
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
US6387900B1 (en) 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
US6608227B1 (en) * 1999-10-15 2003-08-19 Bristol-Myers Squibb Pharma Benzylcycloalkyl amines as modulators of chemokine receptor activity
US6410533B1 (en) 2000-02-10 2002-06-25 Genzyme Corporation Antibacterial compounds
WO2002002525A2 (en) 2000-06-30 2002-01-10 Bristol-Myers Squibb Pharma Company N-ureidoheterocycloaklyl-piperidines as modulators of chemokine receptor activity
JP2004534017A (ja) 2001-04-27 2004-11-11 バーテックス ファーマシューティカルズ インコーポレイテッド Baceのインヒビター
GB0110901D0 (en) 2001-05-02 2001-06-27 Smithkline Beecham Plc Novel Compounds
AU2002363250A1 (en) 2001-11-01 2003-05-12 Icagen, Inc. Pyrazole-amides and-sulfonamides
EP1451156A4 (en) 2001-11-27 2005-05-25 Merck & Co Inc 4-AMINOCHINOLINVERBINDUNGEN
SE0104248D0 (sv) 2001-12-14 2001-12-14 Astrazeneca Ab Method of treatment
PL215228B1 (pl) 2002-05-20 2013-11-29 Bristol Myers Squibb Co Zwiazki tripeptydowe, ich zastosowanie i kompozycja farmaceutyczna je zawierajaca oraz jej zastosowanie
EP1601666A2 (en) 2002-07-02 2005-12-07 Schering Corporation New neuropeptide y y5 receptor antagonists
WO2004032870A2 (en) 2002-10-08 2004-04-22 Rinat Neuroscience Corp. Methods for treating post-surgical pain by admisnistering a nerve growth factor antagonist and compositions containing the same
ATE368042T1 (de) * 2002-10-30 2007-08-15 Astellas Pharma Inc Cephemverbindungen
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
WO2005024755A2 (en) 2002-12-31 2005-03-17 Deciphera Pharmaceuticals, Llc. Medicaments for the treatment of neurodegenerative disorders or diabetes
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
US20040171075A1 (en) 2002-12-31 2004-09-02 Flynn Daniel L Modulation of protein functionalities
PT1658269E (pt) 2003-06-12 2009-01-09 Abbott Lab Compostos condensados que inibem o receptor vanilóide de subtipo 1 (vr1)
WO2005048953A2 (en) 2003-11-13 2005-06-02 Ambit Biosciences Corporation Amide derivatives as kinase modulators
MY141220A (en) * 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
US20080220497A1 (en) 2003-12-24 2008-09-11 Flynn Daniel L Modulation of protein functionalities
JP4573223B2 (ja) * 2004-01-23 2010-11-04 東レ・ファインケミカル株式会社 光学活性trans−4−アミノ−1−ベンジル−3−ピロリジノールの製造方法
US7838524B2 (en) 2004-04-30 2010-11-23 Bayer Healthcare Llc Substituted pyrazolyl urea derivatives useful in the treatment of cancer
JP2008509179A (ja) * 2004-08-09 2008-03-27 グラクソ グループ リミテッド グルタミン酸受容体を強化する化合物および医学におけるその使用
WO2006068591A1 (en) 2004-12-20 2006-06-29 Astrazeneca Ab Novel pyrazole derivatives and their use as modulators of nicotinic acetylcholine receptors
CA2592116A1 (en) 2004-12-23 2006-08-03 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
CA2592118C (en) 2004-12-23 2015-11-17 Deciphera Pharmaceuticals, Llc Urea derivatives as enzyme modulators
CA2589748C (en) 2004-12-24 2013-08-13 Astrazeneca Ab Heterocyclic compounds as ccr2b antagonists
EP1836188A1 (en) 2004-12-30 2007-09-26 Astex Therapeutics Limited Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases
WO2010104488A1 (en) 2009-02-19 2010-09-16 University Of Connecticut Novel hetero pyrrole analogs acting on cannapinoid receptors
GB0510141D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B3
US20060281768A1 (en) 2005-06-10 2006-12-14 Gaul Michael D Thienopyrimidine and thienopyridine kinase modulators
EP1960394A2 (en) 2005-11-15 2008-08-27 Bayer HealthCare AG Pyrazolyl urea derivatives useful in the treatment of cancer
US7514435B2 (en) 2005-11-18 2009-04-07 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
JP2009518298A (ja) 2005-12-01 2009-05-07 バイエル ヘルスケア リミティド ライアビリティ カンパニー 癌治療に有用な尿素化合物
WO2007089646A1 (en) 2006-01-31 2007-08-09 Array Biopharma Inc. Kinase inhibitors and methods of use thereof
GB0607953D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
WO2008016811A2 (en) 2006-07-31 2008-02-07 Neurogen Corporation Aminopiperidines and realted compounds
EP2049542B1 (en) 2006-08-09 2012-09-19 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US8188113B2 (en) 2006-09-14 2012-05-29 Deciphera Pharmaceuticals, Inc. Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
US7897762B2 (en) 2006-09-14 2011-03-01 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of proliferative diseases
US7790756B2 (en) 2006-10-11 2010-09-07 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
US20090062273A1 (en) 2006-12-15 2009-03-05 Ingo Hartung 3-H-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same.
WO2008140895A1 (en) 2007-04-20 2008-11-20 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
DE602008001983D1 (de) * 2007-04-20 2010-09-09 Hoffmann La Roche Pyrrolidinderivate als doppelte nk1/nk3-rezeptorenantagonisten
WO2008150899A1 (en) 2007-05-29 2008-12-11 Emory University Combination therapies for treatment of cancer and inflammatory diseases
NZ582443A (en) 2007-07-12 2011-04-29 Novartis Ag Oral pharmaceutical solutions containing telbivudine
ITMI20071731A1 (it) 2007-09-06 2009-03-07 Univ Degli Studi Genova Nuovi derivati ureici dell'acido 1h-pirazol-4-carbossilico con attivita inibente nei confronti della chemiotassi di neutrofili
WO2009053694A1 (en) * 2007-10-24 2009-04-30 Cancer Research Technology Limited Therapeutic oxy-phenyl-aryl compounds and their use
EP2070929A1 (en) * 2007-12-11 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Alkynylaryl compounds and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
AU2009226136B2 (en) 2008-03-17 2013-08-15 Ambit Biosciences Corporation Quinazoline derivatives as RAF kinase modulators and methods of use thereof
CA2722418C (en) 2008-05-13 2013-09-17 Irm Llc Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors
KR20110010781A (ko) * 2008-06-16 2011-02-07 에프. 호프만-라 로슈 아게 Nk2 수용체 길항제로서의 피롤리딘 유도체
JP5816087B2 (ja) 2008-08-29 2015-11-18 エンメエッセディ・イタリア・エッセ・エッレ・エッレ Smoアンタゴニストとしての飽和二環式複素環誘導体
USRE49686E1 (en) 2008-09-19 2023-10-10 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound and use of same
SI2350075T1 (sl) 2008-09-22 2014-06-30 Array Biopharma, Inc. Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji
CA2738870A1 (en) * 2008-10-09 2010-04-15 F. Hoffmann-La Roche Ag Pyrrolidine n-benzyl derivatives
CN102264736B (zh) * 2008-10-22 2013-08-14 阵列生物制药公司 作为TRK激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物
US8022099B2 (en) * 2008-11-03 2011-09-20 Hoffmann-La Roche Inc. N-benzyl pyrrolidine derivatives
EA020923B1 (ru) 2008-11-19 2015-02-27 Мериал Лимитед Производные димерного 1-арилпиразола
RU2016116516A (ru) 2008-12-08 2018-12-07 Мандифарма Интернэшнл Корпорейшн Лимитед Композиции ингибиторов тирозинкиназных рецепторов белков
CN102264737A (zh) 2008-12-23 2011-11-30 雅培制药有限公司 抗病毒化合物
GB0904285D0 (en) * 2009-03-12 2009-04-22 Prosidion Ltd Compounds for the treatment of metabolic disorders
WO2010114881A1 (en) * 2009-04-01 2010-10-07 Progenra Inc. Anti-neoplastic compounds, compositions and methods
WO2010125799A1 (ja) 2009-04-27 2010-11-04 塩野義製薬株式会社 Pi3k阻害活性を有するウレア誘導体
US20120083476A1 (en) 2009-06-05 2012-04-05 Janssen Pharmaceutica Nv Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
KR20120059558A (ko) 2009-08-19 2012-06-08 암비트 바이오사이언시즈 코포레이션 바이아릴 화합물 및 이의 사용 방법
US20120220564A1 (en) 2009-09-18 2012-08-30 Zalicus Pharmaceuticals Ltd. Selective calcium channel modulators
US20110144081A1 (en) * 2009-12-15 2011-06-16 Henner Knust Pyrrolidine derivatives
US20110152233A1 (en) * 2009-12-18 2011-06-23 Henner Knust Pyrrolidine compounds
BR122019024201B1 (pt) 2010-05-20 2021-08-03 Array Biopharma Inc Composto macrocíclico como inibidores de trk quinase, seu uso, e composição farmacêutica
WO2011150198A1 (en) 2010-05-27 2011-12-01 Ambit Biosciences Corporation Azolyl urea compounds and methods of use thereof
US9586938B2 (en) * 2010-07-29 2017-03-07 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
US9242981B2 (en) * 2010-09-16 2016-01-26 Merck Sharp & Dohme Corp. Fused pyrazole derivatives as novel ERK inhibitors
AR083904A1 (es) * 2010-11-18 2013-04-10 Prosidion Ltd Derivados de 1,4-pirrolidinas disustituidos y 3-il-aminas y sus usos en el tratamiento de desordenes metabolicos
NZ618795A (en) 2011-05-13 2015-07-31 Array Biopharma Inc Pyrrolidinyl urea, pyrrolidinyl thiourea and pyrrolidinyl guanidine compounds as trka kinase inhibitors
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
US8969325B2 (en) 2011-12-19 2015-03-03 Abbvie Inc. TRPV1 antagonists
WO2013176970A1 (en) 2012-05-22 2013-11-28 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
CA2882950A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
EP2900223B1 (en) 2012-09-28 2017-10-25 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
WO2014078417A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrazolyl 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
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl 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
CA2891334C (en) 2012-11-13 2021-10-19 Array Biopharma Inc. Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain
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
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
ME02990B (me) * 2012-11-13 2018-10-20 Array Biopharma Inc Jedinjenja n-pirolidinil, n'-pirazolil- uree, tiouree, guanidina i cijanoguanidina kао inhibitori trka kinaze
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
WO2015039333A1 (en) 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF

Similar Documents

Publication Publication Date Title
JP2014511892A5 (enExample)
RU2016134751A (ru) Соединения
JP2016501191A5 (enExample)
JP2020505396A5 (enExample)
JP2018502877A5 (enExample)
RU2014141579A (ru) Гетероциклические соединения в качестве ингибиторов бета-лактамаз
JP2017504635A5 (enExample)
HRP20161786T1 (hr) Pirolidinil urea, pirolidinil tiourea i pirolidinil gvanidin spojevi kao inhibitori trka kinaze
JP2014506599A5 (enExample)
AR073551A1 (es) Pirimidinas macrociclicas como inhibidores de proteina cinasa
JP2011509309A5 (enExample)
JP2013509431A5 (enExample)
JP2015522650A5 (enExample)
JP2016506961A5 (enExample)
JP2016530283A5 (enExample)
JP2013010792A5 (enExample)
JP2016506962A5 (enExample)
WO2009082268A3 (ru) ЛИГАНДЫ α-АДРЕНОЦЕПТОРОВ, ДОПАМИНОВЫХ, ГИСТАМИНОВЫХ, ИМИДАЗОЛИНОВЫХ И СЕРОТОНИНОВЫХ РЕЦЕПТОРОВ И ИХ ПРИМЕНЕНИЕ
JP2013512903A5 (enExample)
JP2018527295A5 (enExample)
JP2014526500A5 (enExample)
JP2014037426A5 (enExample)
JP2015535839A5 (enExample)
RU2015106434A (ru) Производные типа азаиндазола или диазаиндазола для лечения боли
JP2012511588A5 (enExample)