JP2017512786A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017512786A5 JP2017512786A5 JP2016558347A JP2016558347A JP2017512786A5 JP 2017512786 A5 JP2017512786 A5 JP 2017512786A5 JP 2016558347 A JP2016558347 A JP 2016558347A JP 2016558347 A JP2016558347 A JP 2016558347A JP 2017512786 A5 JP2017512786 A5 JP 2017512786A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- trifluoromethyl
- benzamide
- fluoro
- pyrimidin
- 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.)
- Pending
Links
- -1 pyrazolopyrimidinyl Chemical group 0.000 claims 53
- 125000000217 alkyl group Chemical group 0.000 claims 29
- 125000000623 heterocyclic group Chemical group 0.000 claims 26
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 239000001257 hydrogen Substances 0.000 claims 23
- 150000003839 salts Chemical class 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 18
- 150000002431 hydrogen Chemical group 0.000 claims 17
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 15
- GKIRPKYJQBWNGO-OCEACIFDSA-N clomifene Chemical compound C1=CC(OCCN(CC)CC)=CC=C1C(\C=1C=CC=CC=1)=C(\Cl)C1=CC=CC=C1 GKIRPKYJQBWNGO-OCEACIFDSA-N 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000003226 pyrazolyl group Chemical group 0.000 claims 8
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 125000002971 oxazolyl group Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 102000015336 Nerve Growth Factor Human genes 0.000 claims 4
- 108010025020 Nerve Growth Factor Proteins 0.000 claims 4
- 125000002393 azetidinyl group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims 4
- 229940053128 nerve growth factor Drugs 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 229910052731 fluorine Inorganic materials 0.000 claims 3
- 239000011737 fluorine Substances 0.000 claims 3
- PAMCRRDMORMCSM-UHFFFAOYSA-N n-(trifluoromethyl)benzamide Chemical compound FC(F)(F)NC(=O)C1=CC=CC=C1 PAMCRRDMORMCSM-UHFFFAOYSA-N 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- MPVRBTDECKCFEY-UHFFFAOYSA-N CC(N)C1=CC2=NN(C(NC(=O)C3=C(F)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)=C2C=C1)C1=CC=CC=C1 Chemical compound CC(N)C1=CC2=NN(C(NC(=O)C3=C(F)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)=C2C=C1)C1=CC=CC=C1 MPVRBTDECKCFEY-UHFFFAOYSA-N 0.000 claims 2
- 208000016192 Demyelinating disease Diseases 0.000 claims 2
- 206010012305 Demyelination Diseases 0.000 claims 2
- 206010067601 Dysmyelination Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 101150111783 NTRK1 gene Proteins 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 230000006378 damage Effects 0.000 claims 2
- 230000004064 dysfunction Effects 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- XUZRZKLRCQZFRE-UHFFFAOYSA-N 2-fluoro-4-methyl-N-[6-[2-(methylamino)-2-oxoethyl]-2-phenylindazol-3-yl]-5-pyrimidin-2-ylbenzamide Chemical compound CNC(=O)Cc1ccc2c(NC(=O)c3cc(c(C)cc3F)-c3ncccn3)n(nc2c1)-c1ccccc1 XUZRZKLRCQZFRE-UHFFFAOYSA-N 0.000 claims 1
- ITZLPHSULOBASY-UHFFFAOYSA-N 2-fluoro-N-[5-(hydroxymethyl)-2-phenylpyrazolo[4,3-b]pyridin-3-yl]-5-pyrimidin-2-yl-4-(trifluoromethyl)benzamide Chemical compound OCC1=NC2=C(NC(=O)C3=C(F)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)N(N=C2C=C1)C1=CC=CC=C1 ITZLPHSULOBASY-UHFFFAOYSA-N 0.000 claims 1
- ZJANXHIOPJZRFG-UHFFFAOYSA-N C(#N)C1=CC2=C(N(N=C2C=C1)C1=CC=CC=C1)NC(C1=CC(=C(C=C1)C(F)(F)F)C1=NN(C=C1)C)=O Chemical compound C(#N)C1=CC2=C(N(N=C2C=C1)C1=CC=CC=C1)NC(C1=CC(=C(C=C1)C(F)(F)F)C1=NN(C=C1)C)=O ZJANXHIOPJZRFG-UHFFFAOYSA-N 0.000 claims 1
- RVPFEMHDILVAKN-UHFFFAOYSA-N C(C)(=O)NCC=1C=C(C=CC1)N1N=C2C(N=CC=C2)=C1NC(C1=C(C=C(C(=C1)C1=NC=CC=N1)C(F)(F)F)F)=O Chemical compound C(C)(=O)NCC=1C=C(C=CC1)N1N=C2C(N=CC=C2)=C1NC(C1=C(C=C(C(=C1)C1=NC=CC=N1)C(F)(F)F)F)=O RVPFEMHDILVAKN-UHFFFAOYSA-N 0.000 claims 1
- CSIQWYJANFGMGW-UHFFFAOYSA-N C1(=CC=CC=C1)N1N=C2C(N=CC(=C2)C(=O)N)=C1NC(=O)C1=CC(=C(C=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound C1(=CC=CC=C1)N1N=C2C(N=CC(=C2)C(=O)N)=C1NC(=O)C1=CC(=C(C=C1)C(F)(F)F)C1=NC=CC=N1 CSIQWYJANFGMGW-UHFFFAOYSA-N 0.000 claims 1
- WYGHKVWQCCSHOV-UHFFFAOYSA-N CC(O)C1=CC2=C(NC(=O)C3=C(F)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)N(N=C2C=C1)C1=CC=CC=C1 Chemical compound CC(O)C1=CC2=C(NC(=O)C3=C(F)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)N(N=C2C=C1)C1=CC=CC=C1 WYGHKVWQCCSHOV-UHFFFAOYSA-N 0.000 claims 1
- MDANURKSLYFPRZ-UHFFFAOYSA-N CC(O)C1=CC2=C(NC(=O)C3=CC=C(C(=C3)C3=NN(C)C=C3)C(F)(F)F)N(N=C2C=C1)C1=CC=CC=C1 Chemical compound CC(O)C1=CC2=C(NC(=O)C3=CC=C(C(=C3)C3=NN(C)C=C3)C(F)(F)F)N(N=C2C=C1)C1=CC=CC=C1 MDANURKSLYFPRZ-UHFFFAOYSA-N 0.000 claims 1
- LLVGDVKKDXMYDS-UHFFFAOYSA-N CC(O)C1=CC2=NN(C(NC(=O)C3=C(Cl)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)=C2C=C1)C1=CC=CC=C1 Chemical compound CC(O)C1=CC2=NN(C(NC(=O)C3=C(Cl)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)=C2C=C1)C1=CC=CC=C1 LLVGDVKKDXMYDS-UHFFFAOYSA-N 0.000 claims 1
- FHQGBHLHSCXWTJ-UHFFFAOYSA-N CC(O)C1=CC2=NN(C(NC(=O)C3=C(Cl)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)=C2N=C1)C1=CC=CC=C1 Chemical compound CC(O)C1=CC2=NN(C(NC(=O)C3=C(Cl)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)=C2N=C1)C1=CC=CC=C1 FHQGBHLHSCXWTJ-UHFFFAOYSA-N 0.000 claims 1
- KFUMLBPRQSNFIS-UHFFFAOYSA-N CC(O)C1=CC2=NN(C(NC(=O)C3=C(F)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)=C2C=N1)C1=CC=CC=C1 Chemical compound CC(O)C1=CC2=NN(C(NC(=O)C3=C(F)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)=C2C=N1)C1=CC=CC=C1 KFUMLBPRQSNFIS-UHFFFAOYSA-N 0.000 claims 1
- CDGQZCLRDVGCPS-UHFFFAOYSA-N CC(O)C1=CC2=NN(C(NC(=O)C3=C(F)C=C(C(=C3)C3=NN(C)C=C3)C(F)(F)F)=C2N=C1)C1=CC=CC=C1 Chemical compound CC(O)C1=CC2=NN(C(NC(=O)C3=C(F)C=C(C(=C3)C3=NN(C)C=C3)C(F)(F)F)=C2N=C1)C1=CC=CC=C1 CDGQZCLRDVGCPS-UHFFFAOYSA-N 0.000 claims 1
- OHTZNYGIBTVDIF-UHFFFAOYSA-N CC(O)C1=NC2=C(NC(=O)C3=C(F)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)N(N=C2C=C1)C1=CC=CC=C1 Chemical compound CC(O)C1=NC2=C(NC(=O)C3=C(F)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)N(N=C2C=C1)C1=CC=CC=C1 OHTZNYGIBTVDIF-UHFFFAOYSA-N 0.000 claims 1
- BBERDCONFQXSPX-UHFFFAOYSA-N CN(C)CC1=CC2=C(N(N=C2C=C1)C1=CC=CC=C1)NC(C1=CC(=C(C=C1)C(F)(F)F)C1=NN(C=C1)C)=O Chemical compound CN(C)CC1=CC2=C(N(N=C2C=C1)C1=CC=CC=C1)NC(C1=CC(=C(C=C1)C(F)(F)F)C1=NN(C=C1)C)=O BBERDCONFQXSPX-UHFFFAOYSA-N 0.000 claims 1
- VXAVCZZIGYUMSQ-UHFFFAOYSA-N CN1N=C(C=C1)C=1C=C(C=CC1C(F)(F)F)C(=O)NC=1N(N=C2C1N=CC(=C2)C(=O)N)C2=CC=CC=C2 Chemical compound CN1N=C(C=C1)C=1C=C(C=CC1C(F)(F)F)C(=O)NC=1N(N=C2C1N=CC(=C2)C(=O)N)C2=CC=CC=C2 VXAVCZZIGYUMSQ-UHFFFAOYSA-N 0.000 claims 1
- ZCNGBXMCQVZBFM-UHFFFAOYSA-N CN1N=C(C=C1)C=1C=C(C=CC1C(F)(F)F)C(=O)NC=1N(N=C2C=C(C=CC12)C(=O)N)C1=CC=CC=C1 Chemical compound CN1N=C(C=C1)C=1C=C(C=CC1C(F)(F)F)C(=O)NC=1N(N=C2C=C(C=CC12)C(=O)N)C1=CC=CC=C1 ZCNGBXMCQVZBFM-UHFFFAOYSA-N 0.000 claims 1
- AXFSAIJYBOTAFJ-UHFFFAOYSA-N CN1N=C(C=C1)C=1C=C(C=CC1C(F)(F)F)C(=O)NC=1N(N=C2C=CC(=CC12)C(=O)N)C1=CC=CC=C1 Chemical compound CN1N=C(C=C1)C=1C=C(C=CC1C(F)(F)F)C(=O)NC=1N(N=C2C=CC(=CC12)C(=O)N)C1=CC=CC=C1 AXFSAIJYBOTAFJ-UHFFFAOYSA-N 0.000 claims 1
- NRBMTQFGYWJGBX-UHFFFAOYSA-N ClC1=C(C(=O)NC=2N(N=C3C=2N=C(C=C3)CO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound ClC1=C(C(=O)NC=2N(N=C3C=2N=C(C=C3)CO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 NRBMTQFGYWJGBX-UHFFFAOYSA-N 0.000 claims 1
- LNPFNUJPXPEIBG-UHFFFAOYSA-N ClC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)C(C)(C)O)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound ClC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)C(C)(C)O)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 LNPFNUJPXPEIBG-UHFFFAOYSA-N 0.000 claims 1
- BVMGHNSPKPYMDY-UHFFFAOYSA-N ClC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)CO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound ClC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)CO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 BVMGHNSPKPYMDY-UHFFFAOYSA-N 0.000 claims 1
- HNMGFURPOCLUBZ-UHFFFAOYSA-N ClC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=C1)C(=O)NC=1N(N=C2C=1N=CC(=C2)C(=O)N)C1=CC=CC=C1 Chemical compound ClC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=C1)C(=O)NC=1N(N=C2C=1N=CC(=C2)C(=O)N)C1=CC=CC=C1 HNMGFURPOCLUBZ-UHFFFAOYSA-N 0.000 claims 1
- GBNVSNXLEIWGNC-UHFFFAOYSA-N ClC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=C1)C(=O)NC=1N(N=C2C=C(C=CC=12)C(=O)N)C1=CC=CC=C1 Chemical compound ClC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=C1)C(=O)NC=1N(N=C2C=C(C=CC=12)C(=O)N)C1=CC=CC=C1 GBNVSNXLEIWGNC-UHFFFAOYSA-N 0.000 claims 1
- VMRBTIOELUXXOS-UHFFFAOYSA-N ClC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C=C(C=CC12)C(=O)NCCO)C1=CC=CC=C1 Chemical compound ClC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C=C(C=CC12)C(=O)NCCO)C1=CC=CC=C1 VMRBTIOELUXXOS-UHFFFAOYSA-N 0.000 claims 1
- ODJPBHRPHYLZGR-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C2N=CC(=C3)C(C)(C)O)C3=CC=CC=C3)C=C(C(=C1)C(F)(F)F)C1=NNC=C1 Chemical compound FC1=C(C(=O)NC=2N(N=C3C2N=CC(=C3)C(C)(C)O)C3=CC=CC=C3)C=C(C(=C1)C(F)(F)F)C1=NNC=C1 ODJPBHRPHYLZGR-UHFFFAOYSA-N 0.000 claims 1
- IWURPFDWEVICJW-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=2C=NC(=C3)C(=O)N)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound FC1=C(C(=O)NC=2N(N=C3C=2C=NC(=C3)C(=O)N)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 IWURPFDWEVICJW-UHFFFAOYSA-N 0.000 claims 1
- KUVFCTFHZSUVLM-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=2N=CC(=C3)C(=O)N)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound FC1=C(C(=O)NC=2N(N=C3C=2N=CC(=C3)C(=O)N)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 KUVFCTFHZSUVLM-UHFFFAOYSA-N 0.000 claims 1
- JQEZBHLEXLABRF-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)C(=O)N)C2=C(C=CC=C2)C)C=C(C(=C1)C(F)(F)F)C1=NN(C=C1)C Chemical compound FC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)C(=O)N)C2=C(C=CC=C2)C)C=C(C(=C1)C(F)(F)F)C1=NN(C=C1)C JQEZBHLEXLABRF-UHFFFAOYSA-N 0.000 claims 1
- NDIAMNTZKTYHGQ-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)C(=O)N)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NN(C=C1)C Chemical compound FC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)C(=O)N)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NN(C=C1)C NDIAMNTZKTYHGQ-UHFFFAOYSA-N 0.000 claims 1
- DIJLWKUDISEUSD-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)CNCCO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NN(C=C1)C Chemical compound FC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)CNCCO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NN(C=C1)C DIJLWKUDISEUSD-UHFFFAOYSA-N 0.000 claims 1
- NCSKJOFRPAWSMQ-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)CO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound FC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)CO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 NCSKJOFRPAWSMQ-UHFFFAOYSA-N 0.000 claims 1
- KUWWQOJJZDEENF-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)CO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NNC=C1 Chemical compound FC1=C(C(=O)NC=2N(N=C3C=C(C=CC23)CO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NNC=C1 KUWWQOJJZDEENF-UHFFFAOYSA-N 0.000 claims 1
- ASVQVVFLEKIMIE-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=C(C=CC=23)C(=O)N)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound FC1=C(C(=O)NC=2N(N=C3C=C(C=CC=23)C(=O)N)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 ASVQVVFLEKIMIE-UHFFFAOYSA-N 0.000 claims 1
- PVWWJVBOYHULJD-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=CC(=CC23)CCO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound FC1=C(C(=O)NC=2N(N=C3C=CC(=CC23)CCO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 PVWWJVBOYHULJD-UHFFFAOYSA-N 0.000 claims 1
- DPFLQQUIFVLOJF-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=CC(=CC=23)CO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound FC1=C(C(=O)NC=2N(N=C3C=CC(=CC=23)CO)C2=CC=CC=C2)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 DPFLQQUIFVLOJF-UHFFFAOYSA-N 0.000 claims 1
- KXECLFFOKKSMQT-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=CC(=CC=23)CO)C2=NNC(=C2)C)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound FC1=C(C(=O)NC=2N(N=C3C=CC(=CC=23)CO)C2=NNC(=C2)C)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 KXECLFFOKKSMQT-UHFFFAOYSA-N 0.000 claims 1
- AADZKIQXCDCINB-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3C=NC(=CC32)CO)C3=CC=CC=C3)C=C(C(=C1)C(F)(F)F)C1=NN(C=C1)C Chemical compound FC1=C(C(=O)NC=2N(N=C3C=NC(=CC32)CO)C3=CC=CC=C3)C=C(C(=C1)C(F)(F)F)C1=NN(C=C1)C AADZKIQXCDCINB-UHFFFAOYSA-N 0.000 claims 1
- NIJMADWXVFTQKO-UHFFFAOYSA-N FC1=C(C(=O)NC=2N(N=C3N=CC(=CC32)C(C)(C)O)C3=CC=CC=C3)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 Chemical compound FC1=C(C(=O)NC=2N(N=C3N=CC(=CC32)C(C)(C)O)C3=CC=CC=C3)C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1 NIJMADWXVFTQKO-UHFFFAOYSA-N 0.000 claims 1
- APOONGNZUGSHGT-UHFFFAOYSA-N FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=C1)C(=O)NC=1N(N=C2C1N=CC(=C2)C(=O)N)C2=CC=CC=C2 Chemical compound FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=C1)C(=O)NC=1N(N=C2C1N=CC(=C2)C(=O)N)C2=CC=CC=C2 APOONGNZUGSHGT-UHFFFAOYSA-N 0.000 claims 1
- VJJNXINELPSTKN-UHFFFAOYSA-N FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=C1)C(=O)NC=1N(N=C2C=C(C=CC=12)C(=O)N)C1=CC=CC=C1 Chemical compound FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=C1)C(=O)NC=1N(N=C2C=C(C=CC=12)C(=O)N)C1=CC=CC=C1 VJJNXINELPSTKN-UHFFFAOYSA-N 0.000 claims 1
- DSHCMFAIYUYYRV-UHFFFAOYSA-N FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C(=CC=CC12)C(=O)N)C1=CC=CC=C1 Chemical compound FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C(=CC=CC12)C(=O)N)C1=CC=CC=C1 DSHCMFAIYUYYRV-UHFFFAOYSA-N 0.000 claims 1
- QSBXBHUEPYNQTB-UHFFFAOYSA-N FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C1N=C(C=C2)C(=O)N)C2=CC=CC=C2 Chemical compound FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C1N=C(C=C2)C(=O)N)C2=CC=CC=C2 QSBXBHUEPYNQTB-UHFFFAOYSA-N 0.000 claims 1
- ZYJJNZCNBOVLCR-UHFFFAOYSA-N FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C1N=CC(=C2)C(=O)N)C2=C(C=CC=C2)C Chemical compound FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C1N=CC(=C2)C(=O)N)C2=C(C=CC=C2)C ZYJJNZCNBOVLCR-UHFFFAOYSA-N 0.000 claims 1
- HYSMHBHSBGHVHB-UHFFFAOYSA-N FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C=C(C=CC=12)C(=O)N)C1=C(C=CC=C1)C Chemical compound FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C=C(C=CC=12)C(=O)N)C1=C(C=CC=C1)C HYSMHBHSBGHVHB-UHFFFAOYSA-N 0.000 claims 1
- YAOPRVSKJLEMOO-UHFFFAOYSA-N FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C=C(C=CC=12)C(=O)NCCO)C1=CC=CC=C1 Chemical compound FC1=C(C=C(C(=C1)C(F)(F)F)C1=NC=CC=N1)C(=O)NC=1N(N=C2C=C(C=CC=12)C(=O)NCCO)C1=CC=CC=C1 YAOPRVSKJLEMOO-UHFFFAOYSA-N 0.000 claims 1
- VETNEPBRBSGTPG-UHFFFAOYSA-N FC1=C(C=C(C(=C1)C(F)(F)F)C1=NN(C=C1)C)C(=O)NC=1N(N=C2C1N=CC(=C2)C(=O)N)C2=CC=CC=C2 Chemical compound FC1=C(C=C(C(=C1)C(F)(F)F)C1=NN(C=C1)C)C(=O)NC=1N(N=C2C1N=CC(=C2)C(=O)N)C2=CC=CC=C2 VETNEPBRBSGTPG-UHFFFAOYSA-N 0.000 claims 1
- VVZWYJXHLGUKAL-UHFFFAOYSA-N FC1=C(C=C(C(=C1)C(F)(F)F)C1=NNC=C1)C(=O)NC=1N(N=C2C=C(C=CC12)C(=O)N)C1=CC=CC=C1 Chemical compound FC1=C(C=C(C(=C1)C(F)(F)F)C1=NNC=C1)C(=O)NC=1N(N=C2C=C(C=CC12)C(=O)N)C1=CC=CC=C1 VVZWYJXHLGUKAL-UHFFFAOYSA-N 0.000 claims 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 1
- FKUSMPPXJLOXCR-UHFFFAOYSA-N N-[5-(2,2-difluoro-1-hydroxyethyl)-2-phenylindazol-3-yl]-2-fluoro-5-pyrimidin-2-yl-4-(trifluoromethyl)benzamide Chemical compound OC(C(F)F)C1=CC2=C(NC(=O)C3=C(F)C=C(C(=C3)C3=NC=CC=N3)C(F)(F)F)N(N=C2C=C1)C1=CC=CC=C1 FKUSMPPXJLOXCR-UHFFFAOYSA-N 0.000 claims 1
- YLIPQRCSRJTFHZ-UHFFFAOYSA-N N-[6-(2-amino-2-oxoethyl)-2-phenylpyrazolo[4,3-b]pyridin-3-yl]-2-chloro-4-methyl-5-pyrimidin-2-ylbenzamide Chemical compound CC1=CC(Cl)=C(C=C1C1=NC=CC=N1)C(=O)NC1=C2N=CC(CC(N)=O)=CC2=NN1C1=CC=CC=C1 YLIPQRCSRJTFHZ-UHFFFAOYSA-N 0.000 claims 1
- HSZLGMGLKICUOQ-UHFFFAOYSA-N NCC=1C=CC2=C(N(N=C2C1)C1=CC=CC=C1)NC(C1=C(C=C(C(=C1)C1=NN(C=C1)C)C(F)(F)F)F)=O Chemical compound NCC=1C=CC2=C(N(N=C2C1)C1=CC=CC=C1)NC(C1=C(C=C(C(=C1)C1=NN(C=C1)C)C(F)(F)F)F)=O HSZLGMGLKICUOQ-UHFFFAOYSA-N 0.000 claims 1
- GXHGCXDPSFWOQQ-UHFFFAOYSA-N O=C1N(C(CN1)=O)CC=1C=2C(N=CC1)=C(N(N2)C2=CC=CC=C2)NC(C2=C(C=C(C(=C2)C2=NN(C=C2)C)C(F)(F)F)F)=O Chemical compound O=C1N(C(CN1)=O)CC=1C=2C(N=CC1)=C(N(N2)C2=CC=CC=C2)NC(C2=C(C=C(C(=C2)C2=NN(C=C2)C)C(F)(F)F)F)=O GXHGCXDPSFWOQQ-UHFFFAOYSA-N 0.000 claims 1
- KGAQXHWMFVCAJX-UHFFFAOYSA-N OC(C(F)F)c1ccc2c(NC(=O)c3cc(-c4ncccn4)c(cc3F)C(F)(F)F)n(nc2c1)-c1ccccc1 Chemical compound OC(C(F)F)c1ccc2c(NC(=O)c3cc(-c4ncccn4)c(cc3F)C(F)(F)F)n(nc2c1)-c1ccccc1 KGAQXHWMFVCAJX-UHFFFAOYSA-N 0.000 claims 1
- ZFLNPQMSUGXZTP-UHFFFAOYSA-N OC(C)(C)C1=CC=2C(N=C1)=C(N(N2)C2=CC=CC=C2)NC(C2=CC(=C(C=C2)C(F)(F)F)C2=NN(C=C2)C)=O Chemical compound OC(C)(C)C1=CC=2C(N=C1)=C(N(N2)C2=CC=CC=C2)NC(C2=CC(=C(C=C2)C(F)(F)F)C2=NN(C=C2)C)=O ZFLNPQMSUGXZTP-UHFFFAOYSA-N 0.000 claims 1
- UFPNZOKJIKFUGS-UHFFFAOYSA-N OC1(CC1)C1=CC2=C(N(N=C2C=C1)C1=CC=CC=C1)NC(C1=CC(=C(C=C1)C(F)(F)F)C1=NN(C=C1)C)=O Chemical compound OC1(CC1)C1=CC2=C(N(N=C2C=C1)C1=CC=CC=C1)NC(C1=CC(=C(C=C1)C(F)(F)F)C1=NN(C=C1)C)=O UFPNZOKJIKFUGS-UHFFFAOYSA-N 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 230000001594 aberrant effect Effects 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2014/074143 | 2014-03-26 | ||
| PCT/CN2014/074143 WO2015143652A1 (en) | 2014-03-26 | 2014-03-26 | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| PCT/US2015/021952 WO2015148354A2 (en) | 2014-03-26 | 2015-03-23 | TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017512786A JP2017512786A (ja) | 2017-05-25 |
| JP2017512786A5 true JP2017512786A5 (enExample) | 2018-05-10 |
Family
ID=54193893
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016558339A Pending JP2017508766A (ja) | 2014-03-26 | 2015-03-23 | ＴｒｋＡキナーゼ阻害薬、その組成物および方法 |
| JP2016558347A Pending JP2017512786A (ja) | 2014-03-26 | 2015-03-23 | ＴｒｋＡキナーゼ阻害薬、その組成物および方法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016558339A Pending JP2017508766A (ja) | 2014-03-26 | 2015-03-23 | ＴｒｋＡキナーゼ阻害薬、その組成物および方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US9862716B2 (enExample) |
| EP (2) | EP3122345B1 (enExample) |
| JP (2) | JP2017508766A (enExample) |
| KR (2) | KR20160131119A (enExample) |
| CN (2) | CN106456582A (enExample) |
| AU (2) | AU2015236363A1 (enExample) |
| CA (2) | CA2942957A1 (enExample) |
| MX (2) | MX2016012481A (enExample) |
| RU (2) | RU2016141645A (enExample) |
| WO (3) | WO2015143652A1 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105418615B (zh) * | 2015-12-09 | 2018-02-02 | 北京工业大学 | 苯甲酰胺衍生物及制备和应用 |
| WO2018236856A1 (en) * | 2017-06-19 | 2018-12-27 | University Of Maryland, Baltimore | Car activator agents for cyclophosphamide-based treatments of cancer |
| AU2018346331B2 (en) | 2017-10-04 | 2023-08-24 | Dana-Farber Cancer Institute, Inc. | Small molecule inhibition of transcription factor SALL4 and uses thereof |
| KR20190043437A (ko) | 2017-10-18 | 2019-04-26 | 씨제이헬스케어 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| PL3724191T3 (pl) * | 2017-12-15 | 2022-04-25 | Pyramid Biosciences, Inc. | Pochodne 5-(2-(2,5-difluorofenylo)pirolidyn-1-ylo)-3-(1h-pirazol-1-ilo)pirazolo[1,5-a]pirymidyny i pokrewne związki jako inhibitory kinaz trk do leczenia nowotworu |
| CA3096746A1 (en) | 2018-04-12 | 2019-10-17 | Bayer Aktiengesellschaft | N-(cyclopropylmethyl)-5-(methylsulfonyl)-n-{1-[1-(pyrimidin-2-yl)-1h-1,2,4-triazol-5-yl]ethyl}benzamide derivatives and the corresponding pyridine-carboxamide derivatives as pesticides |
| KR102129114B1 (ko) * | 2018-07-26 | 2020-07-02 | 주식회사 온코파마텍 | TrkA 저해 활성을 갖는 화합물 및 이를 유효성분으로 함유하는 통증의 예방 또는 치료용 약학적 조성물 |
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| IL280984B2 (en) * | 2018-08-22 | 2025-02-01 | Cullgen Shanghai Inc | Tropomyosin receptor kinase (TRK) inhibitor compounds and methods of use |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
| 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 |
| BR112021018168B1 (pt) | 2019-03-21 | 2023-11-28 | Onxeo | Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer |
| BR112022006791A2 (pt) | 2019-10-09 | 2022-06-28 | Bayer Ag | Novos compostos heteroaril-triazol como pesticidas |
| CA3159348A1 (en) | 2019-11-08 | 2021-05-14 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| TW202134226A (zh) | 2019-11-18 | 2021-09-16 | 德商拜耳廠股份有限公司 | 作為殺蟲劑之新穎雜芳基-三唑化合物 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| EP4110772A4 (en) | 2020-02-26 | 2024-04-03 | Cullgen (Shanghai), Inc. | TROPOMYOSIN RECEPTOR KINASE (TRK) DEGRADATION COMPOUNDS AND METHODS OF USE |
| CN115916771B (zh) * | 2020-04-02 | 2025-04-01 | 浙江华海药业股份有限公司 | 多靶点的抗肿瘤化合物及其制备方法和应用 |
| AR122141A1 (es) | 2020-05-28 | 2022-08-17 | Lilly Co Eli | Inhibidor de trka |
| CN113666862B (zh) * | 2021-08-18 | 2024-05-31 | 山东大学 | 一种通过镍催化不对称硝化反应制备手性3-硝基吲哚类化合物的方法 |
Family Cites Families (66)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB599834A (en) * | 1943-04-08 | 1948-03-22 | Francolor Sa | Improvements in or relating to the manufacture of azodyestuffs |
| EP0714898B1 (en) * | 1994-06-21 | 2001-11-14 | Otsuka Pharmaceutical Factory, Inc. | PYRAZOLO [1,5-a]PYRIMIDINE DERIVATIVE |
| IT1306704B1 (it) | 1999-05-26 | 2001-10-02 | Sirs Societa Italiana Per La R | Anticorpi monoclonali e suoi derivati sintetici o biotecnologici ingrado di agire come molecole antagoniste per il ngf. |
| DE19946322A1 (de) | 1999-09-28 | 2001-03-29 | Bayer Ag | Verfahren zur Konditionierung von Ionenaustauscherharzen |
| FR2807660A1 (fr) | 2000-04-13 | 2001-10-19 | Warner Lambert Co | Utilisation d'antagonistes du ngf pour la prevention ou le traitement de douleurs viscerales chroniques |
| WO2001081345A1 (en) * | 2000-04-20 | 2001-11-01 | Mitsubishi Pharma Corporation | Aromatic amide compounds |
| US20050009876A1 (en) * | 2000-07-31 | 2005-01-13 | Bhagwat Shripad S. | Indazole compounds, compositions thereof and methods of treatment therewith |
| US6897231B2 (en) * | 2000-07-31 | 2005-05-24 | Signal Pharmaceuticals, Inc. | Indazole derivatives as JNK inhibitors and compositions and methods related thereto |
| KR100713137B1 (ko) * | 2001-06-28 | 2007-05-02 | 동화약품공업주식회사 | 신규의 2,4-디플루오로벤즈아미드 유도체 |
| ES2357502T3 (es) * | 2001-09-26 | 2011-04-27 | Pfizer Italia S.R.L. | Derivados de aminoindazol activos como inhibidores de quinasa, procedimiento para su preparación y composiciones farmaceuticas que los contienen. |
| US20030144518A1 (en) * | 2001-12-07 | 2003-07-31 | The Procter & Gamble Company | Process for preparing 3-acylamino-imidazo[1,2-a]pyridines |
| JP2003231687A (ja) * | 2002-02-04 | 2003-08-19 | Japan Tobacco Inc | ピラゾリル縮合環化合物及びその医薬用途 |
| WO2003068773A1 (en) * | 2002-02-12 | 2003-08-21 | Glaxo Group Limited | Pyrazolopyridine derivatives |
| US7098334B2 (en) * | 2002-03-25 | 2006-08-29 | Industrial Research Limited | 4-amino-5H-pyrrolo[3,2-d]pyrimidine inhibitors of nucleoside phosphorylases and nucleosidases |
| EP1388341A1 (en) | 2002-08-07 | 2004-02-11 | Aventis Pharma Deutschland GmbH | Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals |
| UA80447C2 (en) | 2002-10-08 | 2007-09-25 | Methods for treating pain by administering nerve growth factor antagonist and opioid analgesic | |
| CN102746399B (zh) | 2002-12-24 | 2016-03-02 | 里纳特神经系统学公司 | 抗ngf抗体及其使用方法 |
| AU2004236240C1 (en) | 2003-05-01 | 2010-11-04 | Bristol-Myers Squibb Company | Aryl-substituted pyrazole compounds useful as kinase inhibitors |
| CN1849138B (zh) | 2003-07-15 | 2011-11-30 | 安姆根有限公司 | 作为选择性ngf途径抑制剂的人抗ngf中和抗体 |
| JP2007506741A (ja) | 2003-09-23 | 2007-03-22 | メルク エンド カムパニー インコーポレーテッド | 向代謝性グルタミン酸受容体のピラゾール系調節剤 |
| US20050143384A1 (en) | 2003-10-30 | 2005-06-30 | Eric Sartori | Amide thiadiazole inhibitors of plasminogen activator inhibitor-1 |
| ITRM20030601A1 (it) | 2003-12-24 | 2005-06-25 | Lay Line Genomics Spa | Metodo per l'umanizzazione di anticorpi e anticorpi umanizzati con esso ottenuti. |
| EP1720855A4 (en) * | 2004-03-02 | 2008-12-17 | Smithkline Beecham Corp | HEMMER OF ACT ACTIVITY |
| ATE517885T1 (de) | 2004-04-30 | 2011-08-15 | Bayer Healthcare Llc | Substituierte pyrazolyl-harnstoff-derivate zur behandlung von krebs |
| EP1853602B1 (en) | 2005-02-16 | 2010-07-14 | AstraZeneca AB | Chemical compounds |
| CN101208093A (zh) | 2005-04-27 | 2008-06-25 | 阿斯利康(瑞典)有限公司 | 吡唑-嘧啶衍生物在治疗疼痛中的用途 |
| BRPI0610184A2 (pt) | 2005-05-16 | 2012-09-25 | Astrazeneca Ab | composto, sal farmaceuticamente aceitável de um composto, processo para preparar um composto ou um sal farmaceuticamente aceitável do mesmo, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, métodos para a inibição da atividade de trk, para o tratamento ou profilaxia de cáncer e para a produção de um efeito anti-proliferativo em um animal de sanque quente, e, composição farmacêutica |
| 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. |
| ITRM20050332A1 (it) | 2005-06-24 | 2006-12-25 | Lay Line Genomics Spa | Uso di molecole in grado di bloccare l'attivita' di trka per potenziare gli effetti di analgesici oppiacei sul dolore. |
| KR20080032188A (ko) * | 2005-07-14 | 2008-04-14 | 다케다 샌디에고, 인코포레이티드 | 히스톤 탈아세틸화 효소 억제제 |
| EP1910369A1 (en) | 2005-07-29 | 2008-04-16 | Astellas Pharma Inc. | Fused heterocycles as lck inhibitors |
| DE102005042742A1 (de) | 2005-09-02 | 2007-03-08 | Schering Ag | Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
| CN101287707A (zh) | 2005-10-13 | 2008-10-15 | 德福根有限公司 | 激酶抑制剂 |
| JP2009519208A (ja) | 2005-12-15 | 2009-05-14 | 塩野義製薬株式会社 | アミド誘導体を含有する医薬組成物 |
| JP5153773B2 (ja) | 2006-07-07 | 2013-02-27 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | フェニル置換ヘテロアリール誘導体及び抗癌剤としてのその使用 |
| EP2058309A4 (en) * | 2006-08-04 | 2010-12-22 | Takeda Pharmaceutical | CONDENSED HETEROCYCLIC COMPOUND |
| JP2010508315A (ja) | 2006-10-30 | 2010-03-18 | ノバルティス アーゲー | 抗炎症剤としてのヘテロ環式化合物 |
| ES2534573T3 (es) | 2007-04-06 | 2015-04-24 | Neurocrine Biosciences, Inc. | Antagonistas del receptor de la hormona liberadora de gonadotropina y métodos relacionados con los mismos |
| GB0708188D0 (en) * | 2007-04-27 | 2007-06-06 | Merck Sharp & Dohme | Therapeutic compounds |
| SG182187A1 (en) * | 2007-06-08 | 2012-07-30 | Abbott Gmbh & Co Kg | 5-heteroaryl substituted indazoles as kinase inhibitors |
| JP2010531850A (ja) | 2007-07-02 | 2010-09-30 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規化合物 |
| CL2008001943A1 (es) | 2007-07-02 | 2009-09-11 | Boehringer Ingelheim Int | Compuestos derivados de fenil-triazol, inhibidores de enzimas de señales especificas que participan del control de la proliferacion celular; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar cancer, infecciones, enfermedades inflamatorias y autoinmunes. |
| EA018503B1 (ru) * | 2007-07-20 | 2013-08-30 | НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. | Замещенные производные индазола, активные как ингибиторы киназы |
| NZ585237A (en) | 2007-10-09 | 2012-03-30 | Merck Patent Gmbh | N-(pyrazole-3-yl)-benzamide derivatives as glucokinase activators |
| DK2350075T3 (da) | 2008-09-22 | 2014-05-26 | Array Biopharma Inc | Substituerede imidazo[1,2b]pyridazinforbindelser som trk-kinase-inhibitorer |
| US8703962B2 (en) | 2008-10-24 | 2014-04-22 | Purdue Pharma L.P. | Monocyclic compounds and their use as TRPV1 ligands |
| KR101048448B1 (ko) * | 2008-11-21 | 2011-07-11 | 한국화학연구원 | 신규 피라졸로[4,3-ｂ]피리딘 유도체 또는 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물 |
| US9040508B2 (en) | 2008-12-08 | 2015-05-26 | Vm Pharma Llc | Compositions of protein receptor tyrosine kinase inhibitors |
| JP2012522013A (ja) | 2009-03-27 | 2012-09-20 | ザ ユーエービー リサーチ ファウンデーション | 調節ｉｒｅｓ媒介翻訳 |
| US20130017188A1 (en) * | 2009-07-31 | 2013-01-17 | The Brigham And Women's Hospital, Inc. | Modulation of sgk1 expression in th17 cells to modulate th17-mediated immune responses |
| RU2608611C2 (ru) * | 2009-11-05 | 2017-01-23 | Юниверсити Оф Нотр Дам Дю Лак | СОЕДИНЕНИЯ ИМИДАЗО[1,2-а] ПИРИДИНА, ИХ СИНТЕЗ И СПОСОБЫ ПРИМЕНЕНИЯ |
| MX2012015105A (es) | 2010-07-02 | 2013-05-28 | Gilead Sciences Inc | Inhibidores de cinasa de regulacion mediante señal de apoptosis. |
| KR20130108543A (ko) * | 2010-08-05 | 2013-10-04 | 암젠 인코포레이션 | 역형성 림프종 키나제를 억제하는 벤즈이미다졸 및 아자벤즈이미다졸 화합물 |
| EP2611785B1 (de) | 2010-09-01 | 2014-06-04 | Bayer Intellectual Property GmbH | N-(tetrazol-5-yl)- und n-(triazol-5-yl)arylcarbonsäureamide und ihre verwendung als herbizide |
| WO2012044090A2 (ko) * | 2010-09-29 | 2012-04-05 | 크리스탈지노믹스(주) | 단백질 키나제 억제 활성을 갖는 신규한 아미노퀴나졸린 화합물 |
| WO2012100223A1 (en) | 2011-01-21 | 2012-07-26 | John Irwin | Synthetic lethal targeting of glucose transport |
| AR085318A1 (es) | 2011-02-09 | 2013-09-25 | Syngenta Participations Ag | Derivados de triazol que tienen actividad insecticida |
| MY173181A (en) | 2011-05-13 | 2020-01-02 | Array Biopharma Inc | Pyrrolidinyl urea, pyrrolidinyl thiourea and pyrrolidinyl guanidine compounds as trka kinase inhibitors |
| CN102796103A (zh) | 2011-05-23 | 2012-11-28 | 南京英派药业有限公司 | 6-（芳基甲酰）咪唑并[1,2-a]嘧啶和6-（芳基甲酰）[1,2,4]三唑并[4,3-a]嘧啶作为Hedgehog抑制剂及其应用 |
| PL2714668T3 (pl) | 2011-05-23 | 2017-06-30 | Merck Patent Gmbh | Pochodne tiazolowe |
| EP2731439A4 (en) * | 2011-07-12 | 2014-12-03 | Merck Sharp & Dohme | TRKA KINASE INHIBITORS, COMPOSITIONS AND METHOD THEREFOR |
| EP2779833A4 (en) * | 2011-11-14 | 2015-03-18 | Tesaro Inc | MODULATION OF SPECIFIC TYROSINE KINASES |
| WO2013088257A1 (en) * | 2011-12-12 | 2013-06-20 | Dr. Reddy's Laboratories Ltd. | Substituted heterocyclic compounds as tropomyosin receptor kinase a (trka) inhibitors |
| EP2689778A1 (en) * | 2012-07-27 | 2014-01-29 | Pierre Fabre Medicament | Derivatives of azaindoles or diazaindoles for treating pain |
| EP2689779A1 (en) | 2012-07-27 | 2014-01-29 | Pierre Fabre Medicament | Derivatives of azaindazole or diazaindazole type for treating a cancer overexpressing trk |
| TWI652014B (zh) * | 2013-09-13 | 2019-03-01 | 美商艾佛艾姆希公司 | 雜環取代之雙環唑殺蟲劑 |
-
2014
- 2014-03-26 WO PCT/CN2014/074143 patent/WO2015143652A1/en not_active Ceased
-
2015
- 2015-03-23 WO PCT/US2015/022004 patent/WO2015148373A2/en not_active Ceased
- 2015-03-23 CN CN201580027484.1A patent/CN106456582A/zh active Pending
- 2015-03-23 CA CA2942957A patent/CA2942957A1/en not_active Abandoned
- 2015-03-23 RU RU2016141645A patent/RU2016141645A/ru not_active Application Discontinuation
- 2015-03-23 MX MX2016012481A patent/MX2016012481A/es unknown
- 2015-03-23 RU RU2016141647A patent/RU2016141647A/ru not_active Application Discontinuation
- 2015-03-23 EP EP15769224.5A patent/EP3122345B1/en active Active
- 2015-03-23 CA CA2942817A patent/CA2942817A1/en not_active Abandoned
- 2015-03-23 EP EP15769051.2A patent/EP3122344B1/en active Active
- 2015-03-23 WO PCT/US2015/021952 patent/WO2015148354A2/en not_active Ceased
- 2015-03-23 AU AU2015236363A patent/AU2015236363A1/en not_active Abandoned
- 2015-03-23 JP JP2016558339A patent/JP2017508766A/ja active Pending
- 2015-03-23 KR KR1020167029497A patent/KR20160131119A/ko not_active Withdrawn
- 2015-03-23 US US15/129,206 patent/US9862716B2/en active Active
- 2015-03-23 CN CN201580027483.7A patent/CN106456581A/zh active Pending
- 2015-03-23 AU AU2015236438A patent/AU2015236438A1/en not_active Abandoned
- 2015-03-23 KR KR1020167029495A patent/KR20160132114A/ko not_active Withdrawn
- 2015-03-23 JP JP2016558347A patent/JP2017512786A/ja active Pending
- 2015-03-23 US US15/128,793 patent/US9862707B2/en active Active
- 2015-03-23 MX MX2016012483A patent/MX2016012483A/es unknown
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2017512786A5 (enExample) | ||
| RU2016141647A (ru) | ИНГИБИТОРЫ TrkA КИНАЗЫ, ОСНОВАННЫЕ НА НИХ КОМПОЗИЦИИ И СПОСОБЫ | |
| JP2017508766A5 (enExample) | ||
| JP2017512794A5 (enExample) | ||
| JP2018519323A5 (enExample) | ||
| JP5140600B2 (ja) | オーロラキナーゼのアザインドール阻害薬 | |
| JP2007519694A5 (enExample) | ||
| JP2016517417A5 (enExample) | ||
| JP2009524670A5 (enExample) | ||
| JP2016526576A5 (enExample) | ||
| KR20150132384A (ko) | 항암 및 항-증식 활성을 나타내는 n-아실-n''-(피리딘-2-일) 우레아 및 유사체 | |
| JP2017501234A5 (enExample) | ||
| JP2016523911A5 (enExample) | ||
| JP2009510161A5 (enExample) | ||
| JP2017537948A5 (enExample) | ||
| JP2016519685A5 (enExample) | ||
| JP2014037426A5 (enExample) | ||
| RU2009117475A (ru) | Соединения, модулирующие активность c-fms и/или c-kit, и их применения | |
| JP2012532931A5 (enExample) | ||
| JP2009529047A5 (enExample) | ||
| JP2018503673A5 (enExample) | ||
| RU2017121044A (ru) | Производные амидотиадиазола в качестве ингибиторов надфн-оксидазы | |
| JP2014531449A5 (enExample) | ||
| JP2017523223A5 (enExample) | ||
| JP2020502230A5 (enExample) |