JP2017512786A5 - - Google Patents
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- 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
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- -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
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2014
- 2014-03-26 WO PCT/CN2014/074143 patent/WO2015143652A1/en not_active Ceased
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2015
- 2015-03-23 KR KR1020167029495A patent/KR20160132114A/ko not_active Withdrawn
- 2015-03-23 AU AU2015236438A patent/AU2015236438A1/en not_active Abandoned
- 2015-03-23 US US15/129,206 patent/US9862716B2/en active Active
- 2015-03-23 AU AU2015236363A patent/AU2015236363A1/en not_active Abandoned
- 2015-03-23 EP EP15769224.5A patent/EP3122345B1/en active Active
- 2015-03-23 MX MX2016012481A patent/MX2016012481A/es unknown
- 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 CN CN201580027483.7A patent/CN106456581A/zh active Pending
- 2015-03-23 MX MX2016012483A patent/MX2016012483A/es unknown
- 2015-03-23 WO PCT/US2015/021952 patent/WO2015148354A2/en not_active Ceased
- 2015-03-23 JP JP2016558339A patent/JP2017508766A/ja active Pending
- 2015-03-23 RU RU2016141647A patent/RU2016141647A/ru not_active Application Discontinuation
- 2015-03-23 KR KR1020167029497A patent/KR20160131119A/ko not_active Withdrawn
- 2015-03-23 EP EP15769051.2A patent/EP3122344B1/en active Active
- 2015-03-23 WO PCT/US2015/022004 patent/WO2015148373A2/en not_active Ceased
- 2015-03-23 CA CA2942817A patent/CA2942817A1/en not_active Abandoned
- 2015-03-23 RU RU2016141645A patent/RU2016141645A/ru not_active Application Discontinuation
- 2015-03-23 CA CA2942957A patent/CA2942957A1/en not_active Abandoned
- 2015-03-23 CN CN201580027484.1A patent/CN106456582A/zh active Pending