CY1120099T1 - Ενωσεις ν-πυρρολιδινυλ-, ν'-πυραζολυλ- ουριας, θειοουριας, γουανιδινης και κυανογουανιδινης ως αναστολεις trka κινασης - Google Patents

Ενωσεις ν-πυρρολιδινυλ-, ν'-πυραζολυλ- ουριας, θειοουριας, γουανιδινης και κυανογουανιδινης ως αναστολεις trka κινασης

Info

Publication number
CY1120099T1
CY1120099T1 CY20181100348T CY181100348T CY1120099T1 CY 1120099 T1 CY1120099 T1 CY 1120099T1 CY 20181100348 T CY20181100348 T CY 20181100348T CY 181100348 T CY181100348 T CY 181100348T CY 1120099 T1 CY1120099 T1 CY 1120099T1
Authority
CY
Cyprus
Prior art keywords
compounds
thiuuria
pyrazylyl
kianogovanidine
uria
Prior art date
Application number
CY20181100348T
Other languages
English (en)
Inventor
Shelley Allen
Barbara J. BRANDHUBER
Timothy Kercher
Gabrielle R. Kolakowski
Shannon L. WINSKI
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 CY1120099T1 publication Critical patent/CY1120099T1/el

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C403/00Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone
    • C07C403/14Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by doubly-bound oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Ophthalmology & Optometry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Compositions Of Macromolecular Compounds (AREA)

Abstract

Ενώσεις του Τύπου (I) ή στερεοϊσομερή, ταυτομερή ή φαρμακευτικά αποδεκτά άλατα ή προϊόντα επιδιαλύτωσης ή προφάρμακα αυτών, όπου τα R1, R2, Ra, Rb, Rc, Rd, Χ, ο Δακτύλιος Β και ο Δακτύλιος C είναι όπως ορίζεται εδώ και όπου ο Δακτύλιος Β και το τμήμα NH-C(=X)-NH βρίσκονται σε trans στερεοχημική διαμόρφωση, είναι αναστολείς της TrkA κινάσης και είναι χρήσιμες στην αγωγή νοσημάτων που μπορούν να υποβληθούν σε αγωγή με έναν αναστολέα TrkA κινάσης όπως πόνος, καρκίνος, φλεγμονή/φλεγμονώδη νοσήματα, νευροεκφυλιστικά νοσήματα, συγκεκριμένα μολυσματικά νοσήματα, σύνδρομο Sjogren, ενδομητρίωση, διαβητική περιφερική νευροπάθεια, προστατίτιδα ή σύνδρομο πυελικού πόνου.
CY20181100348T 2012-11-13 2018-03-27 Ενωσεις ν-πυρρολιδινυλ-, ν'-πυραζολυλ- ουριας, θειοουριας, γουανιδινης και κυανογουανιδινης ως αναστολεις trka κινασης CY1120099T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261725913P 2012-11-13 2012-11-13
PCT/US2013/069729 WO2014078323A1 (en) 2012-11-13 2013-11-12 N-pyrrolidinyl, n'-pyrazolyl- urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors

Publications (1)

Publication Number Publication Date
CY1120099T1 true CY1120099T1 (el) 2018-12-12

Family

ID=49667600

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20181100348T CY1120099T1 (el) 2012-11-13 2018-03-27 Ενωσεις ν-πυρρολιδινυλ-, ν'-πυραζολυλ- ουριας, θειοουριας, γουανιδινης και κυανογουανιδινης ως αναστολεις trka κινασης

Country Status (32)

Country Link
US (2) US9896435B2 (el)
EP (2) EP3409670B1 (el)
JP (3) JP6316834B2 (el)
KR (1) KR102181915B1 (el)
CN (2) CN107857755B (el)
AU (2) AU2013344943B2 (el)
BR (1) BR112015010875B1 (el)
CA (1) CA2890876C (el)
CL (1) CL2015001261A1 (el)
CY (1) CY1120099T1 (el)
DK (1) DK2922844T3 (el)
ES (2) ES2834027T3 (el)
HK (1) HK1215438A1 (el)
HR (1) HRP20180331T1 (el)
HU (1) HUE038512T2 (el)
IL (1) IL238496B (el)
LT (1) LT2922844T (el)
ME (1) ME02990B (el)
MX (2) MX365733B (el)
MY (1) MY178262A (el)
NO (1) NO2876058T3 (el)
NZ (1) NZ708028A (el)
PH (1) PH12015500939A1 (el)
PL (1) PL2922844T3 (el)
PT (1) PT2922844T (el)
RS (1) RS57001B1 (el)
RU (1) RU2677667C2 (el)
SG (1) SG11201503728XA (el)
SI (1) SI2922844T1 (el)
UA (1) UA116455C2 (el)
WO (1) WO2014078323A1 (el)
ZA (1) ZA201503587B (el)

Families Citing this family (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2350075T3 (pl) 2008-09-22 2014-07-31 Array Biopharma Inc Podstawione związki imidazo[1,2b]pirydazynowe jako inhibitory kinaz Trk
BRPI0919873B8 (pt) 2008-10-22 2021-05-25 Array Biopharma Inc compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
LT3205654T (lt) 2010-05-20 2019-05-27 Array Biopharma, Inc. Makrocikliniai junginiai kaip trk kinazės slopikliai
AU2012256237B2 (en) 2011-05-13 2017-01-05 Array Biopharma Inc. Pyrrolidinyl urea and pyrrolidinyl thiourea 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
WO2014078417A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9969694B2 (en) 2012-11-13 2018-05-15 Array Biopharma Inc. N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9546156B2 (en) 2012-11-13 2017-01-17 Array Biopharma Inc. N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine 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
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
HUE031557T2 (en) 2012-11-13 2017-07-28 Array Biopharma Inc Bicyclic urea, thiourea, guanidine, and cyanoguadinine compounds used to treat pain
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
HUE038512T2 (hu) 2012-11-13 2018-10-29 Array Biopharma Inc N-pirrolidinil-, N'-pirazolil-karbamid, tiokarbamid, guanidin és cianoguanidin vegyületek mint TrkA kináz inhibitorok
US9828360B2 (en) 2012-11-13 2017-11-28 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
MA39069B1 (fr) 2013-11-28 2018-11-30 Kyorin Pharmaceutical Co Ltd Dérivé d'urée ou sel pharmacologiquement acceptable de celui-ci
PL3154959T3 (pl) 2014-05-15 2019-12-31 Array Biopharma, Inc. 1-((3S,4R)-4-(3-Fluorofenylo)-1-(2-metoksyetylo)pirolidyn-3-ylo)-3-(4-metylo-3- (2- metylopirymidyn-5-ylo)-1-fenylo-1H-pirazol-5-ilo)-mocznik jako inhibitor kinazy TrkA
US10160727B2 (en) 2014-08-06 2018-12-25 Shionogi & Co., Ltd. Heterocycle and carbocycle derivatives having TrkA inhibitory activity
PL3699181T3 (pl) 2014-11-16 2023-05-22 Array Biopharma, Inc. Postać krystaliczna wodorosiarczanu (s)-n-(5-((r)-2-(2,5-difluorofenylo) - pirolidyn-1-ylo)-pirazolo[1,5-a]pirimidyn-3-ylo)-3-hydroksypirolidyno-1-karboksyamidu
EP3303631A1 (en) 2015-06-01 2018-04-11 Loxo Oncology Inc. Methods of diagnosing and treating cancer
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
EP3412663B1 (en) 2016-02-04 2022-09-07 Shionogi & Co., Ltd. Nitrogen-containing heterocycle and carbocycle derivatives having trka inhibitory activity
EP3439663B1 (en) 2016-04-04 2024-07-17 Loxo Oncology, Inc. Methods of treating pediatric cancers
GEP20227339B (en) 2016-04-04 2022-01-25 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-hydro-xypyrrolidine-1-carboxamide
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CA3024603A1 (en) 2016-05-18 2017-11-23 Charles Todd Eary Process for the preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide and salts thereof
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
WO2018136661A1 (en) 2017-01-18 2018-07-26 Andrews Steven W SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS
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
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
JP6986565B2 (ja) 2017-09-29 2021-12-22 田辺三菱製薬株式会社 光学活性ピロリジン化合物及びその製造方法
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
TW202410896A (zh) 2017-10-10 2024-03-16 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
MA50456A (fr) 2017-10-26 2020-09-02 Array Biopharma Inc Formulations d'un inhibiteur de kinase trk macrocyclique
CA3087972C (en) 2018-01-18 2023-01-10 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
WO2019143991A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. SUBSTITUTED PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS AS RET KINASE INHIBITORS
TWI802635B (zh) 2018-01-18 2023-05-21 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咯并[2,3-d]嘧啶化合物
PE20210046A1 (es) 2018-03-05 2021-01-08 Bristol Myers Squibb Co Agonistas de fenilpirrolidinona del receptor 2 de formil peptido
CA3095366A1 (en) 2018-03-29 2019-10-03 Loxo Oncology, Inc. Treatment of trk-associated cancers
EP3822266A4 (en) * 2018-07-12 2022-04-27 Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd PYRROLIDINYL UREA DERIVATIVES AND THEIR USE IN TRKA-RELATED DISEASES
KR102653681B1 (ko) 2018-07-31 2024-04-03 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의분무-건조된 분산물 및 제제
CA3111984A1 (en) 2018-09-10 2020-03-19 Array Biopharma Inc. Fused heterocyclic compounds as ret kinase inhibitors
CN110964016B (zh) 2018-09-29 2021-05-28 南京药捷安康生物科技有限公司 氨基降茨烷衍生物及其制备方法与应用
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
CN114364798A (zh) 2019-03-21 2022-04-15 欧恩科斯欧公司 用于治疗癌症的Dbait分子与激酶抑制剂的组合
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
CN112979615B (zh) * 2019-12-17 2024-08-09 上海医药集团股份有限公司 一种喹唑啉脲类化合物、其制备方法、制备中间体、药物组合物及应用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN117836289A (zh) * 2021-04-12 2024-04-05 上海睿跃生物科技有限公司 原肌球蛋白受体激酶(trk)降解化合物及其使用方法
CN113278409B (zh) * 2021-06-22 2022-04-29 西南石油大学 一种高温酸化缓蚀剂
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
WO2024061768A1 (en) 2022-09-19 2024-03-28 Basf Se Azole pesticidal compounds

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU679887B2 (en) 1995-09-11 1997-07-10 Nihon Nohyaku Co., Ltd. Azole derivatives, their use, production and usage
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
JP2001521934A (ja) 1997-11-03 2001-11-13 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 抗炎症薬としての芳香族ヘテロ環式化合物
ES2154253T3 (es) 1997-12-22 2012-01-27 Bayer Healthcare Llc Inhibición de la actividad de p38 cinasa usando ureas heterocíclicas sustituidas.
US7329670B1 (en) 1997-12-22 2008-02-12 Bayer Pharmaceuticals Corporation Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
WO1999032110A1 (en) 1997-12-22 1999-07-01 Bayer Corporation INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS
US6197798B1 (en) 1998-07-21 2001-03-06 Novartis Ag Amino-benzocycloalkane derivatives
CN1326848C (zh) 1998-12-25 2007-07-18 帝国脏器制药株式会社 氨基吡唑衍生物
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
US6410533B1 (en) 2000-02-10 2002-06-25 Genzyme Corporation Antibacterial compounds
AU2001273129A1 (en) 2000-06-30 2002-01-14 Bristol-Myers Squibb Pharma Company N-ureidoheterocycloaklyl-piperidines as modulators of chemokine receptor activity
WO2002088101A2 (en) 2001-04-27 2002-11-07 Vertex Pharmaceuticals Incorporated Inhibitors of bace
GB0110901D0 (en) 2001-05-02 2001-06-27 Smithkline Beecham Plc Novel Compounds
ES2338539T3 (es) 2001-11-01 2010-05-10 Icagen, Inc. Pirazolamidas para uso en el tratamiento del dolor.
WO2003045920A1 (en) 2001-11-27 2003-06-05 Merck & Co., Inc. 4-aminoquinoline compounds
SE0104248D0 (sv) 2001-12-14 2001-12-14 Astrazeneca Ab Method of treatment
JP4498133B2 (ja) 2002-07-02 2010-07-07 シェーリング コーポレイション 新規神経ペプチドyy5レセプターアンタゴニスト
RU2338555C2 (ru) 2002-10-08 2008-11-20 Ринат Ньюросайенс Корп. Способы лечения послеоперационной боли введением антагониста фактора роста нервов и композиции, содержащие фактор роста нервов
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
SI2017265T1 (sl) 2003-06-12 2011-09-30 Abbott Lab Kondenzirane spojine za inhibicijo vaniloidnega receptorja podvrste (VR1) receptorja
CA2545711A1 (en) 2003-11-13 2005-06-02 Ambit Biosciences Corporation Urea derivatives as kinase modulators
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
ATE517885T1 (de) 2004-04-30 2011-08-15 Bayer Healthcare Llc Substituierte pyrazolyl-harnstoff-derivate zur behandlung von krebs
JP2008524213A (ja) 2004-12-20 2008-07-10 アストラゼネカ・アクチエボラーグ 新規なピラゾール誘導体及びニコチン性アセチルコリン受容体のモジュレーターとしてのそれらの使用
JP5197016B2 (ja) 2004-12-23 2013-05-15 デシファラ ファーマスーティカルズ, エルエルシー 酵素モジュレータ及び治療
CA2592116A1 (en) 2004-12-23 2006-08-03 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
JP2008526723A (ja) 2004-12-30 2008-07-24 アステックス、セラピューティックス、リミテッド Cdk、gsk及びオーロラキナーゼの活性を調節するピラゾール誘導体
GB0510141D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B3
WO2007059202A2 (en) 2005-11-15 2007-05-24 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
WO2008016811A2 (en) 2006-07-31 2008-02-07 Neurogen Corporation Aminopiperidines and realted compounds
US7605160B2 (en) 2006-08-09 2009-10-20 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US7897762B2 (en) 2006-09-14 2011-03-01 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of proliferative diseases
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
US7790756B2 (en) 2006-10-11 2010-09-07 Deciphera Pharmaceuticals, Llc Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
MX2009011343A (es) 2007-04-20 2009-11-05 Deciphera Pharmaceuticals Llc Inhibidores quinasa utiles para el tratamiento de enfermedades mieloproliferativas y otras enfermedades proliferativas.
WO2008150899A1 (en) 2007-05-29 2008-12-11 Emory University Combination therapies for treatment of cancer and inflammatory diseases
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
MX2010012457A (es) * 2008-05-13 2010-12-07 Irm Llc Heterociclos que contienen nitrogeno fusionado y composiciones de los mismos como inhibidores de cinasa.
USRE48334E1 (en) 2008-09-19 2020-12-01 Takeda Pharmaceutical Company Limited Nitrogen-containing heterocyclic compound and use of same
PL2350075T3 (pl) 2008-09-22 2014-07-31 Array Biopharma Inc Podstawione związki imidazo[1,2b]pirydazynowe jako inhibitory kinaz Trk
JP2012505173A (ja) 2008-10-09 2012-03-01 エフ.ホフマン−ラ ロシュ アーゲー ピロリジンn−ベンジル誘導体
BRPI0919873B8 (pt) 2008-10-22 2021-05-25 Array Biopharma Inc compostos de pirazol[1,5-a]pirimidina substituídos como inibidores da trk quinase, seus processos de preparação e composições farmacêuticas
ES2605811T3 (es) 2008-11-19 2017-03-16 Merial, Inc. Derivados de 1-arilpirazol diméricos
WO2010077680A2 (en) 2008-12-08 2010-07-08 Vm Discovery Inc. Compositions of protein receptor tyrosine kinase inhibitors
WO2010075376A2 (en) 2008-12-23 2010-07-01 Abbott Laboratories Anti-viral compounds
CA2753061C (en) 2009-02-19 2016-08-09 Alexandros Makriyannis Novel hetero pyrrole analogs acting on cannabinoid receptors
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
AR077468A1 (es) * 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011032291A1 (en) 2009-09-18 2011-03-24 Zalicus Pharmaceuticals Ltd . Selective calcium channel modulators
LT3205654T (lt) 2010-05-20 2019-05-27 Array Biopharma, Inc. Makrocikliniai junginiai kaip trk kinazės slopikliai
WO2012129258A1 (en) * 2011-03-22 2012-09-27 Merck Sharp & Dohme Corp. Amidopyrazole inhibitors of interleukin receptor-associated kinases
AU2012256237B2 (en) * 2011-05-13 2017-01-05 Array Biopharma Inc. Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as TrkA kinase inhibitors
EP2770987B1 (en) 2011-10-27 2018-04-04 Merck Sharp & Dohme Corp. Novel compounds that are erk inhibitors
WO2013096226A1 (en) 2011-12-19 2013-06-27 Abbvie Inc. Trpv1 antagonists
US9181261B2 (en) 2012-05-22 2015-11-10 Merck Sharp & Dohme Corp. TrkA kinase inhibitors, compositions and methods thereof
JP6280554B2 (ja) 2012-09-28 2018-02-14 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. Erk阻害剤である新規化合物
US9226922B2 (en) 2012-09-28 2016-01-05 Merck Sharp & Dohme Corp. 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
HUE031557T2 (en) 2012-11-13 2017-07-28 Array Biopharma Inc Bicyclic urea, thiourea, guanidine, and cyanoguadinine compounds used to treat pain
US9828360B2 (en) 2012-11-13 2017-11-28 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
US9546156B2 (en) 2012-11-13 2017-01-17 Array Biopharma Inc. N-bicyclic aryl,N'-pyrazolyl urea, thiourea, guanidine cyanoguanidine compounds as TrkA kinase inhibitors
HUE038512T2 (hu) 2012-11-13 2018-10-29 Array Biopharma Inc N-pirrolidinil-, N'-pirazolil-karbamid, tiokarbamid, guanidin és cianoguanidin vegyületek mint TrkA kináz inhibitorok
WO2014078372A1 (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
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
US9969694B2 (en) 2012-11-13 2018-05-15 Array Biopharma Inc. N-(arylalkyl)-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

Also Published As

Publication number Publication date
ES2834027T3 (es) 2021-06-16
JP2018048176A (ja) 2018-03-29
NZ708028A (en) 2018-12-21
ES2664331T3 (es) 2018-04-19
PL2922844T3 (pl) 2018-06-29
IL238496A0 (en) 2015-06-30
JP6482629B2 (ja) 2019-03-13
JP2019081786A (ja) 2019-05-30
BR112015010875B1 (pt) 2022-05-03
JP2016501191A (ja) 2016-01-18
EP2922844A1 (en) 2015-09-30
MY178262A (en) 2020-10-07
NO2876058T3 (el) 2018-06-30
LT2922844T (lt) 2018-03-26
PH12015500939B1 (en) 2015-06-29
EP3409670A1 (en) 2018-12-05
CN107857755B (zh) 2020-10-27
RS57001B1 (sr) 2018-05-31
HK1215438A1 (zh) 2016-08-26
MX2019006834A (es) 2019-09-06
CN104781255B (zh) 2017-10-24
CL2015001261A1 (es) 2015-09-25
AU2017206195A1 (en) 2017-08-03
US10851080B2 (en) 2020-12-01
EP3409670B1 (en) 2020-09-09
EP2922844B1 (en) 2018-01-10
HUE038512T2 (hu) 2018-10-29
BR112015010875A8 (pt) 2019-10-01
US20160280682A1 (en) 2016-09-29
AU2013344943A1 (en) 2015-06-04
UA116455C2 (uk) 2018-03-26
SI2922844T1 (en) 2018-04-30
HRP20180331T1 (hr) 2018-05-04
SG11201503728XA (en) 2015-06-29
CN107857755A (zh) 2018-03-30
MX365733B (es) 2019-06-12
CA2890876C (en) 2021-01-19
PT2922844T (pt) 2018-04-02
RU2677667C2 (ru) 2019-01-18
RU2015122414A (ru) 2017-01-10
KR20150084047A (ko) 2015-07-21
US20180179182A1 (en) 2018-06-28
CN104781255A (zh) 2015-07-15
CA2890876A1 (en) 2014-05-22
US9896435B2 (en) 2018-02-20
ZA201503587B (en) 2020-11-25
WO2014078323A1 (en) 2014-05-22
DK2922844T3 (en) 2018-03-05
JP6316834B2 (ja) 2018-04-25
PH12015500939A1 (en) 2015-06-29
IL238496B (en) 2018-02-28
MX2015006046A (es) 2015-12-01
BR112015010875A2 (pt) 2017-07-11
KR102181915B1 (ko) 2020-11-23
AU2013344943B2 (en) 2017-06-29
AU2017206195B2 (en) 2019-01-03
ME02990B (me) 2018-10-20

Similar Documents

Publication Publication Date Title
CY1120099T1 (el) Ενωσεις ν-πυρρολιδινυλ-, ν'-πυραζολυλ- ουριας, θειοουριας, γουανιδινης και κυανογουανιδινης ως αναστολεις trka κινασης
CY1118468T1 (el) Ενωσεις δικυκλικης ουριας, θειοουριας, γουανιδινης και κυανογουανιδινης χρησιμες για την αγωγη του πονου
CY1119014T1 (el) Ενωσεις πυρρολιδινυλ ουριας και πυρρολιδινυλ θειοουριας ως αναστολεις κινασης trka
CY1125214T1 (el) Ενωσεις ν-((ετ)αρυλμεθυλ)-ετεροαρυλ-καρβοξαμιδιων ως αναστολεις καλλικρεϊνης πλασματος
CY1124407T1 (el) Ενωσεις αναστολεα αυτοταξινης
CY1122075T1 (el) 1-((3s,4r)-4-(3-φθοροφαινυλ)-1-(2-μεθοξυαιθυλ)πυρρολιδιν-3-υλ)-3-(4-μεθυλ-(2-μεθυλοπυριμιδιν-5-υλ)-1 -φαινυλ-1 η-πυραζολ-5-υλ)ουρια ή φαρμακευτικα αποδεκτο αλας αυτης, που επιδεικνυει αναστολη κινασης trka
CY1123811T1 (el) Κρυσταλλικη μορφη αναστολεα pde4
CL2016002027A1 (es) Ciclopropilamina como inhibidor de la lsd1
CL2016003422A1 (es) Inhibidores de demetilasa-1 específico de lisina
CL2015000942A1 (es) Compuestos de benceno sustituido.
CL2017002786A1 (es) Referencia cruzada a solicitudes relacionadas
CY1119361T1 (el) 3,4-διυδροισοκινολιν-2(1h)-υλικες ενωσεις
UY33395A (es) Compuestos macrociclicos como inhibidores de quinasa trk
CO7141456A2 (es) Derivados de aril-sultamo como moduladores de rorc
CY1121384T1 (el) Συνδυαστικη θεραπεια για την αγωγη ανθεκτικων βακτηριακων λοιμωξεων
CL2016003423A1 (es) Inhibidores de demetilasa-1 específico de lisina
CY1123914T1 (el) Αντιμετωπιση των αυξημενων επιπεδων ηωσινοφιλων και/ή βασεοφιλων
CY1123582T1 (el) Προφαρμακα των αναστολεων αντιστροφης μεταγραφασης hiv
CL2015002897A1 (es) Inhibidores de bace1
CY1120573T1 (el) Παραγωγα πυριδαζινης για χρηση στην προληψη ή θεραπεια αταξικης διαταραχης
EA201790687A1 (ru) Хинолинкарбоксамиды для применения в лечении множественной миеломы
TR201905218T4 (tr) Nörodejenerati̇f hastaliklarin tedavi̇si̇ i̇çi̇n yararli vi̇tanoli̇dler.
DOP2016000325A (es) Compuestos, composición farmacéutica y su uso en el tratamiento de enfermedades neurodegenerativas
CR20150300A (es) Compuestos de n-pirrolidinil, n´-pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa
TH162021A (th) อนุพันธ์ไดไฮโดร-เบนโซ-ออกซาซีน และไดไฮโดร-ไพริโด-ออกซาซีน