JPWO2020068729A5 - - Google Patents

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Publication number: JPWO2020068729A5
Authority: JP; Japan
Prior art keywords: alkyl; alkylene; membered heterocycloalkyl; cycloalkyl; membered
Prior art date: 2022-06-06
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

JP2021540378A

Other languages

English (en)

Japanese (ja)

Other versions

JP7399968B2 (ja

JP2022502490A (ja

Publication date

2022-06-06

2019-09-24 Application filed filed Critical

2019-09-24 Priority claimed from PCT/US2019/052567 external-priority patent/WO2020068729A1/en

2022-01-11 Publication of JP2022502490A publication Critical patent/JP2022502490A/ja

2022-06-06 Publication of JPWO2020068729A5 publication Critical patent/JPWO2020068729A5/ja

2023-12-18 Application granted granted Critical

2023-12-18 Publication of JP7399968B2 publication Critical patent/JP7399968B2/ja

Status Active legal-status Critical Current

2039-09-24 Anticipated expiration legal-status Critical

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125000000217 alkyl group Chemical group 0.000 claims description 294
125000002947 alkylene group Chemical group 0.000 claims description 260
125000000592 heterocycloalkyl group Chemical group 0.000 claims description 243
-1 C6-10aryl Chemical group 0.000 claims description 210
125000001424 substituent group Chemical group 0.000 claims description 180
150000001875 compounds Chemical class 0.000 claims description 135
125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 109
125000003118 aryl group Chemical group 0.000 claims description 107
125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 98
125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 88
229910052799 carbon Inorganic materials 0.000 claims description 88
125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 82
125000004433 nitrogen atom Chemical group N* 0.000 claims description 56
125000004432 carbon atom Chemical group C* 0.000 claims description 54
229910052739 hydrogen Inorganic materials 0.000 claims description 54
125000005843 halogen group Chemical group 0.000 claims description 53
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 50
229910052717 sulfur Inorganic materials 0.000 claims description 49
125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 44
125000001072 heteroaryl group Chemical group 0.000 claims description 39
125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 36
150000003839 salts Chemical class 0.000 claims description 34
229910052757 nitrogen Inorganic materials 0.000 claims description 32
125000005842 heteroatom Chemical group 0.000 claims description 29
125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 26
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 26
229910052760 oxygen Inorganic materials 0.000 claims description 25
JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims description 24
229920006395 saturated elastomer Polymers 0.000 claims description 24
125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims description 21
125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 17
ZPVFWPFBNIEHGJ-UHFFFAOYSA-N 2-octanone Chemical compound CCCCCCC(C)=O ZPVFWPFBNIEHGJ-UHFFFAOYSA-N 0.000 claims description 14
125000000753 cycloalkyl group Chemical group 0.000 claims description 13
125000004429 atom Chemical group 0.000 claims description 12
OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical group C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 claims description 12
RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 11
125000003003 spiro group Chemical group 0.000 claims description 11
125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 claims description 10
125000004076 pyridyl group Chemical group 0.000 claims description 10
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 9
125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims description 8
125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims description 8
125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims description 8
125000003545 alkoxy group Chemical group 0.000 claims description 8
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 8
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 8
239000008194 pharmaceutical composition Substances 0.000 claims description 8
RFIOZSIHFNEKFF-UHFFFAOYSA-M piperazine-1-carboxylate Chemical compound [O-]C(=O)N1CCNCC1 RFIOZSIHFNEKFF-UHFFFAOYSA-M 0.000 claims description 8
125000004193 piperazinyl group Chemical group 0.000 claims description 8
125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims description 7
125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims description 6
125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 6
125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 6
125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 5
AGRIQBHIKABLPJ-UHFFFAOYSA-N 1-Pyrrolidinecarboxaldehyde Chemical compound O=CN1CCCC1 AGRIQBHIKABLPJ-UHFFFAOYSA-N 0.000 claims description 4
102100034111 Activin receptor type-1 Human genes 0.000 claims description 4
108091008794 FGF receptors Proteins 0.000 claims description 4
101000799140 Homo sapiens Activin receptor type-1 Proteins 0.000 claims description 4
YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims description 4
125000006598 aminocarbonylamino group Chemical group 0.000 claims description 4
125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 4
201000010099 disease Diseases 0.000 claims description 4
208000035475 disorder Diseases 0.000 claims description 4
230000000694 effects Effects 0.000 claims description 4
102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims description 4
125000001153 fluoro group Chemical group F* 0.000 claims description 4
230000002401 inhibitory effect Effects 0.000 claims description 4
230000005764 inhibitory process Effects 0.000 claims description 4
230000003993 interaction Effects 0.000 claims description 4
125000003226 pyrazolyl group Chemical group 0.000 claims description 4
125000006513 pyridinyl methyl group Chemical group 0.000 claims description 4
125000000719 pyrrolidinyl group Chemical group 0.000 claims description 4
125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 3
125000006564 (C4-C8) cycloalkyl group Chemical group 0.000 claims description 3
125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 3
125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims description 2
125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims description 2
125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 2
125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims description 2
125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 2
OJGOVIODTPNPDG-UHFFFAOYSA-N 1,3-dimethyl-4-[3-(1-methylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]piperazin-2-one Chemical compound CN1C(C(N(CC1)C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C)C)=O OJGOVIODTPNPDG-UHFFFAOYSA-N 0.000 claims description 2
CKRDNNGZWMGNEN-UHFFFAOYSA-N 1-(2,2-difluoroethyl)-3-methyl-4-[3-(1-methylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]piperazin-2-one Chemical compound FC(CN1C(C(N(CC1)C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C)C)=O)F CKRDNNGZWMGNEN-UHFFFAOYSA-N 0.000 claims description 2
UVWZIGUNXMXZKB-UHFFFAOYSA-N 1-(2-methoxyethyl)-3-methyl-4-[3-(1-methylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]piperazin-2-one Chemical compound COCCN1C(C(N(CC1)C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C)C)=O UVWZIGUNXMXZKB-UHFFFAOYSA-N 0.000 claims description 2
KCDXXXPORYWJAK-ZACQAIPSSA-N 1-[(3S,5R)-3,5-dimethyl-4-[3-[6-[(3R)-3-methylpiperazin-1-yl]pyridin-3-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]piperazin-1-yl]-2-methoxyethanone Chemical compound C[C@@H]1CN(C[C@@H](N1C=1N=CC2=C(N=1)C(=NN2)C=1C=NC(=CC=1)N1C[C@H](NCC1)C)C)C(COC)=O KCDXXXPORYWJAK-ZACQAIPSSA-N 0.000 claims description 2
QXRCZGTZEWEMCZ-KURKYZTESA-N 1-[(3S,5R)-3,5-dimethyl-4-[3-[6-[(3R)-3-methylpiperazin-1-yl]pyridin-3-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]piperazin-1-yl]-2-methylpropan-1-one Chemical compound C[C@@H]1CN(C[C@@H](N1C=1N=CC2=C(N=1)C(=NN2)C=1C=NC(=CC=1)N1C[C@H](NCC1)C)C)C(C(C)C)=O QXRCZGTZEWEMCZ-KURKYZTESA-N 0.000 claims description 2
NZLQAPPSOICVHD-UHFFFAOYSA-N 1-cyclopropyl-4-[3-(1-methylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]piperazin-2-one Chemical compound C1(CC1)N1C(CN(CC1)C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C)=O NZLQAPPSOICVHD-UHFFFAOYSA-N 0.000 claims description 2
HEJWDMSZDBYDME-UHFFFAOYSA-N 1-methyl-4-[3-(1-methylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]piperazin-2-one Chemical compound CN1C(CN(CC1)C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C)=O HEJWDMSZDBYDME-UHFFFAOYSA-N 0.000 claims description 2
BJYAKDBGFLVCTL-UHFFFAOYSA-N 11-[3-(1-methylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-4,5,11-triazatricyclo[6.2.1.02,6]undeca-2(6),3-diene Chemical compound CN1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2CCC1CC=1NN=CC=12 BJYAKDBGFLVCTL-UHFFFAOYSA-N 0.000 claims description 2
125000004777 2-fluoroethyl group Chemical group [H]C([H])(F)C([H])([H])* 0.000 claims description 2
125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 2
SADOESADMDLRBT-UHFFFAOYSA-N 3-(1-methylpyrazol-4-yl)-5-(1,4,5,7-tetrahydropyrazolo[3,4-c]pyridin-6-yl)-1H-pyrazolo[4,3-d]pyrimidine Chemical compound CN1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1CC2=C(CC1)C=NN2 SADOESADMDLRBT-UHFFFAOYSA-N 0.000 claims description 2
PGRJFPIBHFUXKF-UHFFFAOYSA-N 3-(2-fluoroethyl)-8-[3-(1-methylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound FCCN1C(C2CCC(C1)N2C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C)=O PGRJFPIBHFUXKF-UHFFFAOYSA-N 0.000 claims description 2
JYSONDVLRCKTFC-UHFFFAOYSA-N 3-ethyl-1-methyl-4-[3-(1-methylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]piperazin-2-one Chemical compound C(C)C1C(N(CCN1C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C)C)=O JYSONDVLRCKTFC-UHFFFAOYSA-N 0.000 claims description 2
JOONLELIXITVDH-UHFFFAOYSA-N 3-methyl-1-pyridin-2-ylpiperazine Chemical compound C1CNC(C)CN1C1=CC=CC=N1 JOONLELIXITVDH-UHFFFAOYSA-N 0.000 claims description 2
GPCBZUFGXDIHJK-UHFFFAOYSA-N 3-methyl-4-[3-(1-methylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-1-propan-2-ylpiperazin-2-one Chemical compound C(C)(C)N1C(C(N(CC1)C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C)C)=O GPCBZUFGXDIHJK-UHFFFAOYSA-N 0.000 claims description 2
WMYYMYYQJVEGME-UHFFFAOYSA-N 3-methyl-8-[3-(1-pyridin-3-ylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound CN1C(C2CCC(C1)N2C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C=1C=NC=CC=1)=O WMYYMYYQJVEGME-UHFFFAOYSA-N 0.000 claims description 2
CCDLWXLVTRKUSK-UHFFFAOYSA-N 3-methyl-8-[3-(1-pyridin-4-ylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound CN1C(C2CCC(C1)N2C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C1=CC=NC=C1)=O CCDLWXLVTRKUSK-UHFFFAOYSA-N 0.000 claims description 2
JUEXCQYUGREKRI-UHFFFAOYSA-N 3-methyl-8-[3-[1-(2,2,2-trifluoroethyl)pyrazol-4-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound CN1C(C2CCC(C1)N2C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)CC(F)(F)F)=O JUEXCQYUGREKRI-UHFFFAOYSA-N 0.000 claims description 2
KOPUTUNXLFQNGX-UHFFFAOYSA-N 3-methyl-8-[3-[1-(2-methylpyridin-4-yl)pyrazol-4-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound CN1C(C2CCC(C1)N2C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C1=CC(=NC=C1)C)=O KOPUTUNXLFQNGX-UHFFFAOYSA-N 0.000 claims description 2
LSRBAFLNXOUPIC-UHFFFAOYSA-N 3-methyl-8-[3-[1-(2-morpholin-4-ylethyl)pyrazol-4-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound CN1C(C2CCC(C1)N2C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)CCN1CCOCC1)=O LSRBAFLNXOUPIC-UHFFFAOYSA-N 0.000 claims description 2
DUNLCPJHEDEUQO-UHFFFAOYSA-N 3-methyl-8-[3-[1-(oxan-4-yl)pyrazol-4-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound CN1C(C2CCC(C1)N2C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)C1CCOCC1)=O DUNLCPJHEDEUQO-UHFFFAOYSA-N 0.000 claims description 2
QJLTYACRBMYTNB-UHFFFAOYSA-N 3-methyl-8-[3-[1-(pyridin-4-ylmethyl)pyrazol-4-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound CN1C(C2CCC(C1)N2C=1N=CC2=C(N=1)C(=NN2)C=1C=NN(C=1)CC1=CC=NC=C1)=O QJLTYACRBMYTNB-UHFFFAOYSA-N 0.000 claims description 2
XOKGHILZHIQAIZ-UHFFFAOYSA-N 3-methyl-8-[3-[1-[1-(2-methylpropanoyl)piperidin-4-yl]pyrazol-4-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound C(C(C)C)(=O)N1CCC(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O XOKGHILZHIQAIZ-UHFFFAOYSA-N 0.000 claims description 2
VMUDEFIQYCCVPA-UHFFFAOYSA-N 3-methyl-8-[3-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound CN1C(C2CCC(C1)N2C=1N=CC2=C(N=1)C(=NN2)C=1C=NC(=CC=1)N1CCN(CC1)C)=O VMUDEFIQYCCVPA-UHFFFAOYSA-N 0.000 claims description 2
GZPHSAQLYPIAIN-UHFFFAOYSA-N 3-pyridinecarbonitrile Chemical compound N#CC1=CC=CN=C1 GZPHSAQLYPIAIN-UHFFFAOYSA-N 0.000 claims description 2
NJSKNQLGZMHYIZ-YSZBQJHXSA-N 4-[(1S,5R)-8-[3-[6-[(3R)-3-methylpiperazin-1-yl]pyridin-3-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,8-diazabicyclo[3.2.1]octan-3-yl]benzonitrile Chemical compound C[C@@H]1CN(CCN1)C1=CC=C(C=N1)C1=NNC2=C1N=C(N=C2)N1[C@H]2CN(C[C@@H]1CC2)C1=CC=C(C#N)C=C1 NJSKNQLGZMHYIZ-YSZBQJHXSA-N 0.000 claims description 2
125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 claims description 2
OZCYACNGDDKBEX-IUDNXUCKSA-N 5-(7-azabicyclo[2.2.1]heptan-7-yl)-3-[6-[(3R)-3-methylpiperazin-1-yl]pyridin-3-yl]-1H-pyrazolo[4,3-d]pyrimidine Chemical compound C12CCC(CC1)N2C=1N=CC2=C(N=1)C(=NN2)C=1C=NC(=CC=1)N1C[C@H](NCC1)C OZCYACNGDDKBEX-IUDNXUCKSA-N 0.000 claims description 2
FVAUWSNXHKYZKA-CALCHBBNSA-N 5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]-3-[4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[4,3-d]pyrimidine Chemical compound C[C@H]1N([C@H](CCC1)C)C=1N=CC2=C(N=1)C(=NN2)C1=CC=C(C=C1)N1CCN(CC1)C FVAUWSNXHKYZKA-CALCHBBNSA-N 0.000 claims description 2
RJCVCOCSWGHLMV-OAGGEKHMSA-N 5-[(2R,6S)-2,6-dimethylpiperidin-1-yl]-3-[6-[(3R)-3-methylpiperazin-1-yl]pyridin-3-yl]-1H-pyrazolo[4,3-d]pyrimidine Chemical compound C[C@H]1N([C@H](CCC1)C)C=1N=CC2=C(N=1)C(=NN2)C=1C=NC(=CC=1)N1C[C@H](NCC1)C RJCVCOCSWGHLMV-OAGGEKHMSA-N 0.000 claims description 2
SSQOEMOSGBXDKM-UHFFFAOYSA-N 5-[3-(1-methylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine Chemical compound CN1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1CC2=C(CC1)N=CS2 SSQOEMOSGBXDKM-UHFFFAOYSA-N 0.000 claims description 2
125000004938 5-pyridyl group Chemical group N1=CC=CC(=C1)* 0.000 claims description 2
125000004939 6-pyridyl group Chemical group N1=CC=CC=C1* 0.000 claims description 2
HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 2
SMAIJIZBLFODOY-UHFFFAOYSA-N 8-[3-(1-imidazo[1,2-a]pyridin-6-ylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound N=1C=CN2C=1C=CC(=C2)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O SMAIJIZBLFODOY-UHFFFAOYSA-N 0.000 claims description 2
AVXYKYUDFKFQSI-UHFFFAOYSA-N 8-[3-[1-(2-methoxyethyl)pyrazol-4-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound COCCN1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O AVXYKYUDFKFQSI-UHFFFAOYSA-N 0.000 claims description 2
STFFFMLZTKDEOR-UHFFFAOYSA-N 8-[3-[1-[6-(dimethylamino)pyridin-3-yl]pyrazol-4-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound CN(C1=CC=C(C=N1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O)C STFFFMLZTKDEOR-UHFFFAOYSA-N 0.000 claims description 2
239000002144 L01XE18 - Ruxolitinib Substances 0.000 claims description 2
206010028980 Neoplasm Diseases 0.000 claims description 2
125000004949 alkyl amino carbonyl amino group Chemical group 0.000 claims description 2
125000003806 alkyl carbonyl amino group Chemical group 0.000 claims description 2
201000011510 cancer Diseases 0.000 claims description 2
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 2
239000003937 drug carrier Substances 0.000 claims description 2
HXUSWYFYCFZUIX-MCPYQZEQSA-N methyl (3R,5S)-3,5-dimethyl-4-[3-[4-(1-methylpyrrolidin-3-yl)phenyl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]piperazine-1-carboxylate Chemical compound C[C@@H]1CN(C[C@@H](N1C=1N=CC2=C(N=1)C(=NN2)C1=CC=C(C=C1)C1CN(CC1)C)C)C(=O)OC HXUSWYFYCFZUIX-MCPYQZEQSA-N 0.000 claims description 2
CXZJXVJPISUKMR-IYBDPMFKSA-N methyl (3R,5S)-4-[3-[3-fluoro-4-(4-methylpiperazin-1-yl)phenyl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,5-dimethylpiperazine-1-carboxylate Chemical compound FC=1C=C(C=CC=1N1CCN(CC1)C)C1=NNC2=C1N=C(N=C2)N1[C@@H](CN(C[C@@H]1C)C(=O)OC)C CXZJXVJPISUKMR-IYBDPMFKSA-N 0.000 claims description 2
XTEQFWKBNUKCEQ-XEWABKELSA-N methyl (3R,5S)-4-[3-[4-[1-(2-hydroxyethyl)pyrrolidin-3-yl]phenyl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,5-dimethylpiperazine-1-carboxylate Chemical compound OCCN1CC(CC1)C1=CC=C(C=C1)C1=NNC2=C1N=C(N=C2)N1[C@@H](CN(C[C@@H]1C)C(=O)OC)C XTEQFWKBNUKCEQ-XEWABKELSA-N 0.000 claims description 2
UNHMWPXLLDGEQH-KDURUIRLSA-N methyl (3S,5R)-4-[3-[4-(4-ethylpiperazin-1-yl)-3-methylphenyl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,5-dimethylpiperazine-1-carboxylate Chemical compound C(C)N1CCN(CC1)C1=C(C=C(C=C1)C1=NNC2=C1N=C(N=C2)N1[C@@H](CN(C[C@@H]1C)C(=O)OC)C)C UNHMWPXLLDGEQH-KDURUIRLSA-N 0.000 claims description 2
CMVIHPMIVIZZCE-ZACQAIPSSA-N methyl (3S,5R)-4-[3-[6-[(3R)-3,4-dimethylpiperazin-1-yl]pyridin-3-yl]-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3,5-dimethylpiperazine-1-carboxylate Chemical compound C[C@@H]1CN(CCN1C)C1=CC=C(C=N1)C1=NNC2=C1N=C(N=C2)N1[C@@H](CN(C[C@@H]1C)C(=O)OC)C CMVIHPMIVIZZCE-ZACQAIPSSA-N 0.000 claims description 2
125000002757 morpholinyl group Chemical group 0.000 claims description 2
NMRPBPVERJPACX-UHFFFAOYSA-N octan-3-ol Chemical compound CCCCCC(O)CC NMRPBPVERJPACX-UHFFFAOYSA-N 0.000 claims description 2
239000000546 pharmaceutical excipient Substances 0.000 claims description 2
JSPCTNUQYWIIOT-UHFFFAOYSA-N piperidine-1-carboxamide Chemical compound NC(=O)N1CCCCC1 JSPCTNUQYWIIOT-UHFFFAOYSA-N 0.000 claims description 2
125000003386 piperidinyl group Chemical group 0.000 claims description 2
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims description 2
HFNKQEVNSGCOJV-OAHLLOKOSA-N ruxolitinib Chemical compound C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 HFNKQEVNSGCOJV-OAHLLOKOSA-N 0.000 claims description 2
229960000215 ruxolitinib Drugs 0.000 claims description 2
LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 2
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 55
125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 2
125000006704 (C5-C6) cycloalkyl group Chemical group 0.000 claims 2
125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 1
208000014767 Myeloproliferative disease Diseases 0.000 claims 1
201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 1
125000003342 alkenyl group Chemical group 0.000 claims 1
125000005115 alkyl carbamoyl group Chemical group 0.000 claims 1
125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
238000000034 method Methods 0.000 description 16
125000001188 haloalkyl group Chemical group 0.000 description 11
125000000304 alkynyl group Chemical group 0.000 description 7
125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 description 3
GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 description 1
125000004438 haloalkoxy group Chemical group 0.000 description 1
238000012986 modification Methods 0.000 description 1
230000004048 modification Effects 0.000 description 1
125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 description 1
230000002062 proliferating effect Effects 0.000 description 1
125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 description 1
238000007363 ring formation reaction Methods 0.000 description 1

JP2021540378A 2018-09-25 2019-09-24 Ａｌｋ２及び／またはｆｇｆｒ調節剤としてのピラゾロ［４，３－ｄ］ピリミジン化合物 Active JP7399968B2 (ja)

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2019
- 2019-09-24 JP JP2021540378A patent/JP7399968B2/ja active Active
- 2019-09-24 WO PCT/US2019/052567 patent/WO2020068729A1/en unknown
- 2019-09-24 EP EP19783815.4A patent/EP3856348B1/en active Active
- 2019-09-24 US US16/580,766 patent/US11111247B2/en active Active
- 2019-09-24 MA MA053726A patent/MA53726A/fr unknown
- 2019-09-24 TW TW108134434A patent/TW202028207A/zh unknown
- 2019-09-25 AR ARP190102727A patent/AR116507A1/es unknown
2021
- 2021-08-04 US US17/394,006 patent/US20220017521A1/en active Pending

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