HRP20171913T1 - Aminopirimidinilni spojevi kao inhibitori jak - Google Patents
Aminopirimidinilni spojevi kao inhibitori jak Download PDFInfo
- Publication number
- HRP20171913T1 HRP20171913T1 HRP20171913TT HRP20171913T HRP20171913T1 HR P20171913 T1 HRP20171913 T1 HR P20171913T1 HR P20171913T T HRP20171913T T HR P20171913TT HR P20171913 T HRP20171913 T HR P20171913T HR P20171913 T1 HRP20171913 T1 HR P20171913T1
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- amino
- pyrimidin
- diazabicyclo
- oct
- Prior art date
Links
- -1 Aminopyrimidinyl compounds Chemical class 0.000 title claims 17
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 86
- 125000001072 heteroaryl group Chemical group 0.000 claims 35
- 150000001875 compounds Chemical class 0.000 claims 32
- 125000003118 aryl group Chemical group 0.000 claims 31
- 150000003839 salts Chemical class 0.000 claims 29
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 26
- 229910052739 hydrogen Inorganic materials 0.000 claims 24
- 239000001257 hydrogen Substances 0.000 claims 24
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 23
- 150000002431 hydrogen Chemical group 0.000 claims 21
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 229910052805 deuterium Inorganic materials 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 150000002367 halogens Chemical class 0.000 claims 18
- 125000000623 heterocyclic group Chemical group 0.000 claims 18
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 9
- 125000003282 alkyl amino group Chemical group 0.000 claims 9
- 125000001153 fluoro group Chemical group F* 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 125000002950 monocyclic group Chemical group 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 7
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 6
- 125000004663 dialkyl amino group Chemical group 0.000 claims 5
- 229910052731 fluorine Inorganic materials 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 3
- 201000004384 Alopecia Diseases 0.000 claims 2
- NNXCVXSDVVSEDL-VHRNVKJDSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(CC#N)C Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(CC#N)C NNXCVXSDVVSEDL-VHRNVKJDSA-N 0.000 claims 2
- ZEIXJLFZPBDRBT-SRABZTEZSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C[C@@H]1[C@H](C1)C#N Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C[C@@H]1[C@H](C1)C#N ZEIXJLFZPBDRBT-SRABZTEZSA-N 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- VGQRFGDVWYLOHZ-LJISPDSOSA-N F[C@H]1[C@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C Chemical compound F[C@H]1[C@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C VGQRFGDVWYLOHZ-LJISPDSOSA-N 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 206010063837 Reperfusion injury Diseases 0.000 claims 2
- 206010040070 Septic Shock Diseases 0.000 claims 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 231100000360 alopecia Toxicity 0.000 claims 2
- AIMMVWOEOZMVMS-UHFFFAOYSA-N cyclopropanecarboxamide Chemical compound NC(=O)C1CC1 AIMMVWOEOZMVMS-UHFFFAOYSA-N 0.000 claims 2
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010003827 Autoimmune hepatitis Diseases 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 208000014644 Brain disease Diseases 0.000 claims 1
- 206010048962 Brain oedema Diseases 0.000 claims 1
- GJCRLBVUCZFFSC-UHFFFAOYSA-N C(#N)CC(=O)N1C2CN(CC1CC2)C1=NC(=NC=C1)NC1=CC=C(C(=O)NCC)C=C1 Chemical compound C(#N)CC(=O)N1C2CN(CC1CC2)C1=NC(=NC=C1)NC1=CC=C(C(=O)NCC)C=C1 GJCRLBVUCZFFSC-UHFFFAOYSA-N 0.000 claims 1
- GLDCJIZKNLVKGU-IYBDPMFKSA-N C(#N)CNC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)C)C(NC)=O Chemical compound C(#N)CNC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)C)C(NC)=O GLDCJIZKNLVKGU-IYBDPMFKSA-N 0.000 claims 1
- RDBPTNPTWAHSBQ-OKILXGFUSA-N C(#N)CNC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C Chemical compound C(#N)CNC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C RDBPTNPTWAHSBQ-OKILXGFUSA-N 0.000 claims 1
- XALRWMAIPZZSON-AQEPXONASA-N C(#N)[C@@H]1C[C@H](C1)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C Chemical compound C(#N)[C@@H]1C[C@H](C1)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C XALRWMAIPZZSON-AQEPXONASA-N 0.000 claims 1
- ORWOPBYTIYCBHF-KCBSTHEDSA-N C(#N)[C@@H]1[C@H](C1)C(=O)N[C@@]12CN(C[C@H]2[C@H]1C)C1=NC(=NC=C1C)NC=1C=NC(=CC=1)OCCO Chemical compound C(#N)[C@@H]1[C@H](C1)C(=O)N[C@@]12CN(C[C@H]2[C@H]1C)C1=NC(=NC=C1C)NC=1C=NC(=CC=1)OCCO ORWOPBYTIYCBHF-KCBSTHEDSA-N 0.000 claims 1
- XALRWMAIPZZSON-JEGGMEIXSA-N C(#N)[C@H]1C[C@H](C1)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C Chemical compound C(#N)[C@H]1C[C@H](C1)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C XALRWMAIPZZSON-JEGGMEIXSA-N 0.000 claims 1
- UWQSTCJFSDJPFR-DZJNRPSUSA-N C(#N)[C@H]1[C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C Chemical compound C(#N)[C@H]1[C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C UWQSTCJFSDJPFR-DZJNRPSUSA-N 0.000 claims 1
- CDGJDGPVKVTIAZ-ARLBYUKCSA-N C(#N)[C@H]1[C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)F Chemical compound C(#N)[C@H]1[C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)F CDGJDGPVKVTIAZ-ARLBYUKCSA-N 0.000 claims 1
- HVCNWUWMNGAGRC-UHFFFAOYSA-N C(C)NC(=O)C1=C(C=C(C=C1)NC1=NC=C(C(=N1)N1CC2CCC(C1)N2C(=O)OC(C)(C)C)F)C Chemical compound C(C)NC(=O)C1=C(C=C(C=C1)NC1=NC=C(C(=N1)N1CC2CCC(C1)N2C(=O)OC(C)(C)C)F)C HVCNWUWMNGAGRC-UHFFFAOYSA-N 0.000 claims 1
- LNJJWYXXKNGHHM-IYBDPMFKSA-N C(C)NC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)C)C(NC)=O Chemical compound C(C)NC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)C)C(NC)=O LNJJWYXXKNGHHM-IYBDPMFKSA-N 0.000 claims 1
- FVXQLOUYMAEKMF-OKILXGFUSA-N C(C)NC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)C(NC)=O Chemical compound C(C)NC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)C(NC)=O FVXQLOUYMAEKMF-OKILXGFUSA-N 0.000 claims 1
- RSTDYANUDZASGW-BETUJISGSA-N C(C)NC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NNC=1 Chemical compound C(C)NC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NNC=1 RSTDYANUDZASGW-BETUJISGSA-N 0.000 claims 1
- SDCIUEURTOJUFC-BETUJISGSA-N C(C)NC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NSC=1 Chemical compound C(C)NC(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NSC=1 SDCIUEURTOJUFC-BETUJISGSA-N 0.000 claims 1
- AQPRACGFZBUKTK-UHFFFAOYSA-N C(C)NC(C1=C(C=C(C=C1)NC1=NC=C(C(=N1)N1CC2CCC(C1)N2C(C(F)(F)F)=O)F)C)=O Chemical compound C(C)NC(C1=C(C=C(C=C1)NC1=NC=C(C(=N1)N1CC2CCC(C1)N2C(C(F)(F)F)=O)F)C)=O AQPRACGFZBUKTK-UHFFFAOYSA-N 0.000 claims 1
- YGNCUNZCKQWGDT-UHFFFAOYSA-N C(C)NC(C1=C(C=C(C=C1)NC1=NC=C(C(=N1)N1CC2N(C(C1)C2)C(C(C)(C)F)=O)F)C)=O Chemical compound C(C)NC(C1=C(C=C(C=C1)NC1=NC=C(C(=N1)N1CC2N(C(C1)C2)C(C(C)(C)F)=O)F)C)=O YGNCUNZCKQWGDT-UHFFFAOYSA-N 0.000 claims 1
- RSLHVVRCDKXPEP-UHFFFAOYSA-N C(C)NC(C1=C(C=C(C=C1)NC1=NC=C(C(=N1)N1CC2N(C(C1)C2)C(C(F)(F)F)=O)F)C)=O Chemical compound C(C)NC(C1=C(C=C(C=C1)NC1=NC=C(C(=N1)N1CC2N(C(C1)C2)C(C(F)(F)F)=O)F)C)=O RSLHVVRCDKXPEP-UHFFFAOYSA-N 0.000 claims 1
- AMEULLJURQUSGL-UHFFFAOYSA-N C(C)NC(C1=C(C=C(C=C1)NC1=NC=CC(=N1)N1CC2N(C(C1)C2)C(C(F)(F)F)=O)C)=O Chemical compound C(C)NC(C1=C(C=C(C=C1)NC1=NC=CC(=N1)N1CC2N(C(C1)C2)C(C(F)(F)F)=O)C)=O AMEULLJURQUSGL-UHFFFAOYSA-N 0.000 claims 1
- MHHFHCHCZMIUDH-UHFFFAOYSA-N C1(CC1)C(=O)N1C2CN(CC1C2)C1=NC(=NC=C1)NC1=CC(=C(C(=O)NCC)C=C1)C Chemical compound C1(CC1)C(=O)N1C2CN(CC1C2)C1=NC(=NC=C1)NC1=CC(=C(C(=O)NCC)C=C1)C MHHFHCHCZMIUDH-UHFFFAOYSA-N 0.000 claims 1
- QZUWXMXRQHXTOB-UHFFFAOYSA-N C1(CC1)C(=O)N1C2CN(CC1CC2)C1=NC(=NC=C1F)NC1=CC=C(C(=O)NCC)C=C1 Chemical compound C1(CC1)C(=O)N1C2CN(CC1CC2)C1=NC(=NC=C1F)NC1=CC=C(C(=O)NCC)C=C1 QZUWXMXRQHXTOB-UHFFFAOYSA-N 0.000 claims 1
- CWSVAVIMQYPSFF-IYBDPMFKSA-N C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)N)C Chemical compound C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)N)C CWSVAVIMQYPSFF-IYBDPMFKSA-N 0.000 claims 1
- JXABGVLMINGKAY-CALCHBBNSA-N C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C Chemical compound C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C JXABGVLMINGKAY-CALCHBBNSA-N 0.000 claims 1
- LUUOFVWWSXLXCD-HDICACEKSA-N C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NCC)C Chemical compound C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NCC)C LUUOFVWWSXLXCD-HDICACEKSA-N 0.000 claims 1
- NFDUKDPMYWCESJ-GASCZTMLSA-N C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C Chemical compound C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C NFDUKDPMYWCESJ-GASCZTMLSA-N 0.000 claims 1
- BGSBLEACDOXVBT-IYBDPMFKSA-N C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)CCO Chemical compound C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)CCO BGSBLEACDOXVBT-IYBDPMFKSA-N 0.000 claims 1
- WYIJQOWAMUZNPW-OKILXGFUSA-N C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NSC=1 Chemical compound C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NSC=1 WYIJQOWAMUZNPW-OKILXGFUSA-N 0.000 claims 1
- IVGALBBQTUXXJL-OKILXGFUSA-N C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1F)NC1=CN=NC=C1 Chemical compound C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1F)NC1=CN=NC=C1 IVGALBBQTUXXJL-OKILXGFUSA-N 0.000 claims 1
- LAPJRNLLQCOCFQ-OKILXGFUSA-N C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1F)NC1=NNC(=C1)C(=O)NCCC Chemical compound C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1F)NC1=NNC(=C1)C(=O)NCCC LAPJRNLLQCOCFQ-OKILXGFUSA-N 0.000 claims 1
- KMIUZNUOEYYSRI-GASCZTMLSA-N C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1F)NC=1C=CC=2N(C=1)C=C(N=2)C(=O)N Chemical compound C1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1F)NC=1C=CC=2N(C=1)C=C(N=2)C(=O)N KMIUZNUOEYYSRI-GASCZTMLSA-N 0.000 claims 1
- ZIVIAGNSDGIEPS-PVSQZPHNSA-N C1(CC1)C(=O)N[C@@]12CN(C[C@H]2[C@H]1C)C1=NC(=NC=C1F)NC=1C=C(C(=NC=1)C(=O)NC)C Chemical compound C1(CC1)C(=O)N[C@@]12CN(C[C@H]2[C@H]1C)C1=NC(=NC=C1F)NC=1C=C(C(=NC=1)C(=O)NC)C ZIVIAGNSDGIEPS-PVSQZPHNSA-N 0.000 claims 1
- ZIVIAGNSDGIEPS-ZNVLZIIHSA-N C1(CC1)C(=O)N[C@]12CN(C[C@@H]2[C@@H]1C)C1=NC(=NC=C1F)NC=1C=C(C(=NC=1)C(=O)NC)C Chemical compound C1(CC1)C(=O)N[C@]12CN(C[C@@H]2[C@@H]1C)C1=NC(=NC=C1F)NC=1C=C(C(=NC=1)C(=O)NC)C ZIVIAGNSDGIEPS-ZNVLZIIHSA-N 0.000 claims 1
- ZXVVBFKTMAKEGN-TXEJJXNPSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)N Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)N ZXVVBFKTMAKEGN-TXEJJXNPSA-N 0.000 claims 1
- CLRRDVPHOPGUPT-GASCZTMLSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)NC(C)C Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)NC(C)C CLRRDVPHOPGUPT-GASCZTMLSA-N 0.000 claims 1
- NJZRKNAKJSUCKN-IYBDPMFKSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)NC1=NC=C(C=C1)C(F)(F)F Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)NC1=NC=C(C=C1)C(F)(F)F NJZRKNAKJSUCKN-IYBDPMFKSA-N 0.000 claims 1
- CCPZFLPAWVBBRN-HNKHHVNMSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)[C@@H]1[C@@H](C1)C#N Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)[C@@H]1[C@@H](C1)C#N CCPZFLPAWVBBRN-HNKHHVNMSA-N 0.000 claims 1
- CCPZFLPAWVBBRN-DMRZNYOFSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)[C@H]1[C@H](C1)C#N Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)[C@H]1[C@H](C1)C#N CCPZFLPAWVBBRN-DMRZNYOFSA-N 0.000 claims 1
- HMDCZVBGULZIIM-CALCHBBNSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C1(CN(C1)S(=O)(=O)C)CC#N Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C1(CN(C1)S(=O)(=O)C)CC#N HMDCZVBGULZIIM-CALCHBBNSA-N 0.000 claims 1
- JSOOKLFPJNXYMJ-IYBDPMFKSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C1(COC1)CC#N Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C1(COC1)CC#N JSOOKLFPJNXYMJ-IYBDPMFKSA-N 0.000 claims 1
- GTXCSFLZRFJUBT-CALCHBBNSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C1=NC=CC(=C1)C#N Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C1=NC=CC(=C1)C#N GTXCSFLZRFJUBT-CALCHBBNSA-N 0.000 claims 1
- PSERGXHXHPELAD-JOHJCKIYSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C1CC(C1)C#N Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C1CC(C1)C#N PSERGXHXHPELAD-JOHJCKIYSA-N 0.000 claims 1
- KTZHNYAOPYBKQW-GASCZTMLSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C1CN(C1)S(=O)(=O)C Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C1CN(C1)S(=O)(=O)C KTZHNYAOPYBKQW-GASCZTMLSA-N 0.000 claims 1
- XJSBQOKCJDKSQL-OKILXGFUSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C=1OC(=CN=1)C#N Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C=1OC(=CN=1)C#N XJSBQOKCJDKSQL-OKILXGFUSA-N 0.000 claims 1
- RHSAUTOLPSZJCQ-GASCZTMLSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC1=CC=NO1 Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC1=CC=NO1 RHSAUTOLPSZJCQ-GASCZTMLSA-N 0.000 claims 1
- JBBPGDSGSVYYSG-GASCZTMLSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC1=CC=NS1 Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC1=CC=NS1 JBBPGDSGSVYYSG-GASCZTMLSA-N 0.000 claims 1
- CFJPJHNMCCTOCJ-IYBDPMFKSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC=1C=NOC=1 Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC=1C=NOC=1 CFJPJHNMCCTOCJ-IYBDPMFKSA-N 0.000 claims 1
- JNJSPLOLHQBPLT-GASCZTMLSA-N CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC=1SC=CN=1 Chemical compound CN1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC=1SC=CN=1 JNJSPLOLHQBPLT-GASCZTMLSA-N 0.000 claims 1
- SIIQDEMADVUFSV-CALCHBBNSA-N CNC(=O)C1=NC=C(C=C1C)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC1=CC=NO1 Chemical compound CNC(=O)C1=NC=C(C=C1C)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC1=CC=NO1 SIIQDEMADVUFSV-CALCHBBNSA-N 0.000 claims 1
- 241000222122 Candida albicans Species 0.000 claims 1
- 206010007134 Candida infections Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- GYSKAZTUAKFQGF-GASCZTMLSA-N ClC=1C(=NC=C(C=1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)C1CC1)C(=O)NC Chemical compound ClC=1C(=NC=C(C=1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)C1CC1)C(=O)NC GYSKAZTUAKFQGF-GASCZTMLSA-N 0.000 claims 1
- ZDEZZXWQZCPDAM-MJBXVCDLSA-N ClC=1C(=NC=C(C=1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)[C@H]1C(C1)(F)F)C(=O)NC Chemical compound ClC=1C(=NC=C(C=1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)[C@H]1C(C1)(F)F)C(=O)NC ZDEZZXWQZCPDAM-MJBXVCDLSA-N 0.000 claims 1
- NATIWSKQHJEQLR-OKILXGFUSA-N ClC=1C=C(C=NC=1C(NC)=O)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)NCC Chemical compound ClC=1C=C(C=NC=1C(NC)=O)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)NCC NATIWSKQHJEQLR-OKILXGFUSA-N 0.000 claims 1
- WGHSWYHCROPHPI-ZNMIVQPWSA-N ClC=1C=C(C=NC=1CCO)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)[C@H]1C(C1)(F)F Chemical compound ClC=1C=C(C=NC=1CCO)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)[C@H]1C(C1)(F)F WGHSWYHCROPHPI-ZNMIVQPWSA-N 0.000 claims 1
- AAWJXJTWXOTSRP-FBWDIHGXSA-N ClC=1C=C(C=NC=1CO)NC1=NC=C(C(=N1)N1C[C@@]2([C@@H]([C@@H]2C1)C)NC(=O)C1CC1)F Chemical compound ClC=1C=C(C=NC=1CO)NC1=NC=C(C(=N1)N1C[C@@]2([C@@H]([C@@H]2C1)C)NC(=O)C1CC1)F AAWJXJTWXOTSRP-FBWDIHGXSA-N 0.000 claims 1
- FSMINCWIXBWFEQ-ZNMIVQPWSA-N ClC=1C=C(C=NC=1OCCO)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)[C@H]1C(C1)(F)F Chemical compound ClC=1C=C(C=NC=1OCCO)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(=O)[C@H]1C(C1)(F)F FSMINCWIXBWFEQ-ZNMIVQPWSA-N 0.000 claims 1
- RWTNRTXQUOTJNI-KMFKOQNUSA-N ClC=1C=C(C=NC=1[C@@H](C)O)NC1=NC=C(C(=N1)N1C[C@@]2([C@@H]([C@@H]2C1)C)NC(=O)C1CC1)F Chemical compound ClC=1C=C(C=NC=1[C@@H](C)O)NC1=NC=C(C(=N1)N1C[C@@]2([C@@H]([C@@H]2C1)C)NC(=O)C1CC1)F RWTNRTXQUOTJNI-KMFKOQNUSA-N 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 1
- 206010013935 Dysmenorrhoea Diseases 0.000 claims 1
- 208000032274 Encephalopathy Diseases 0.000 claims 1
- 201000009273 Endometriosis Diseases 0.000 claims 1
- 206010014824 Endotoxic shock Diseases 0.000 claims 1
- 206010015150 Erythema Diseases 0.000 claims 1
- QBRKCFGRAFDLLV-UHFFFAOYSA-N FC(C(=O)N1C2CN(CC1C2)C1=NC(=NC=C1)NC1=CC=C(C(=O)NCC)C=C1)(C)F Chemical compound FC(C(=O)N1C2CN(CC1C2)C1=NC(=NC=C1)NC1=CC=C(C(=O)NCC)C=C1)(C)F QBRKCFGRAFDLLV-UHFFFAOYSA-N 0.000 claims 1
- UDIPGJHIDQGUMQ-UHFFFAOYSA-N FC(C(=O)N1C2CN(CC1C2)C1=NC(=NC=C1F)NC1=CC(=C(C(=O)NCC)C=C1)C)(C)F Chemical compound FC(C(=O)N1C2CN(CC1C2)C1=NC(=NC=C1F)NC1=CC(=C(C(=O)NCC)C=C1)C)(C)F UDIPGJHIDQGUMQ-UHFFFAOYSA-N 0.000 claims 1
- MUZOPNUVNZDWFF-YIONKMFJSA-N FC1(C(C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)N)C)F Chemical compound FC1(C(C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)N)C)F MUZOPNUVNZDWFF-YIONKMFJSA-N 0.000 claims 1
- CBQRXVIZYPISHJ-QXMXGUDHSA-N FC1(C(C1)CN1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NNC=1)F Chemical compound FC1(C(C1)CN1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NNC=1)F CBQRXVIZYPISHJ-QXMXGUDHSA-N 0.000 claims 1
- WUBDSQXZQWXQOO-OKILXGFUSA-N FC1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C Chemical compound FC1(CC1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C WUBDSQXZQWXQOO-OKILXGFUSA-N 0.000 claims 1
- VIXNYZLRQAAYHS-XHSDSOJGSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC1=CC(=NC(=C1)C)C(=O)NC)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC1=CC(=NC(=C1)C)C(=O)NC)F VIXNYZLRQAAYHS-XHSDSOJGSA-N 0.000 claims 1
- DDSWYIFIOLPNTC-XHSDSOJGSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC1=CC(=NC(=C1)CO)C(=O)NC)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC1=CC(=NC(=C1)CO)C(=O)NC)F DDSWYIFIOLPNTC-XHSDSOJGSA-N 0.000 claims 1
- ISYDIPVXAKDSTF-XHSDSOJGSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C)F ISYDIPVXAKDSTF-XHSDSOJGSA-N 0.000 claims 1
- HXQIMHKPRITQSI-MJBXVCDLSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)F)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)F)F HXQIMHKPRITQSI-MJBXVCDLSA-N 0.000 claims 1
- SMDARHPYQAFXMU-BBWFWOEESA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=CC(=NC=1)C(C#N)(C)C)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=CC(=NC=1)C(C#N)(C)C)F SMDARHPYQAFXMU-BBWFWOEESA-N 0.000 claims 1
- BMASSXKNVQHFPK-ZNMIVQPWSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)CCO)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)CCO)F BMASSXKNVQHFPK-ZNMIVQPWSA-N 0.000 claims 1
- HMZBJXPSSIANDY-MJBXVCDLSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)CO)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)CO)F HMZBJXPSSIANDY-MJBXVCDLSA-N 0.000 claims 1
- WNTYMRBAVODLGO-LZWOXQAQSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)N1CC(C1)O)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)N1CC(C1)O)F WNTYMRBAVODLGO-LZWOXQAQSA-N 0.000 claims 1
- KOSULRGUNRLXHZ-TWMKSMIVSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)N1C[C@@H](CC1)O)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)N1C[C@@H](CC1)O)F KOSULRGUNRLXHZ-TWMKSMIVSA-N 0.000 claims 1
- KOSULRGUNRLXHZ-YVSFHVDLSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)N1C[C@H](CC1)O)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=C(C=1)F)N1C[C@H](CC1)O)F KOSULRGUNRLXHZ-YVSFHVDLSA-N 0.000 claims 1
- USHFAMMZMYXKIJ-SIXLDLHFSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=CC=1)[C@@H](CO)C)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=CC=1)[C@@H](CO)C)F USHFAMMZMYXKIJ-SIXLDLHFSA-N 0.000 claims 1
- USHFAMMZMYXKIJ-LLLHUVSDSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=CC=1)[C@H](CO)C)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NC(=CC=1)[C@H](CO)C)F USHFAMMZMYXKIJ-LLLHUVSDSA-N 0.000 claims 1
- BUWBRTXGQRBBHG-MJBXVCDLSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C)F BUWBRTXGQRBBHG-MJBXVCDLSA-N 0.000 claims 1
- AOWNNGGDTLHAQU-XQQFMLRXSA-N FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NNC=1)F Chemical compound FC1([C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NNC=1)F AOWNNGGDTLHAQU-XQQFMLRXSA-N 0.000 claims 1
- ANYNIPZJSZWMMO-FSTCNJTKSA-N FC1([C@@H](C1)C(=O)N[C@@]12CN(C[C@H]2[C@H]1C)C1=NC(=NC=C1F)NC=1C=NN(C=1)C1COC1)F Chemical compound FC1([C@@H](C1)C(=O)N[C@@]12CN(C[C@H]2[C@H]1C)C1=NC(=NC=C1F)NC=1C=NN(C=1)C1COC1)F ANYNIPZJSZWMMO-FSTCNJTKSA-N 0.000 claims 1
- ZMSCCFCSCKTZSZ-YMRXKLBXSA-N FC1([C@@H](C1)C(=O)N[C@@]12CN(C[C@]2(C1)CO)C1=NC(=NC=C1F)NC=1C=NN(C=1)C)F Chemical compound FC1([C@@H](C1)C(=O)N[C@@]12CN(C[C@]2(C1)CO)C1=NC(=NC=C1F)NC=1C=NN(C=1)C)F ZMSCCFCSCKTZSZ-YMRXKLBXSA-N 0.000 claims 1
- VFTQZQGHFFDMQS-TVPBPMQISA-N FC1([C@@H](C1)C(=O)N[C@]12CN(C[C@@H]2[C@@H]1C)C1=NC(=NC=C1F)NC=1C=NN(C=1)C)F Chemical compound FC1([C@@H](C1)C(=O)N[C@]12CN(C[C@@H]2[C@@H]1C)C1=NC(=NC=C1F)NC=1C=NN(C=1)C)F VFTQZQGHFFDMQS-TVPBPMQISA-N 0.000 claims 1
- LRZYHCZKTOWDMP-BHYGNILZSA-N FC1([C@@H](C1)CN1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C)F Chemical compound FC1([C@@H](C1)CN1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C)F LRZYHCZKTOWDMP-BHYGNILZSA-N 0.000 claims 1
- BQSFRXRHBCYARB-AEGPPILISA-N FC1([C@@H](C1)CN1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C)F Chemical compound FC1([C@@H](C1)CN1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C)F BQSFRXRHBCYARB-AEGPPILISA-N 0.000 claims 1
- HXQIMHKPRITQSI-HZSPNIEDSA-N FC1([C@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)F)F Chemical compound FC1([C@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)F)F HXQIMHKPRITQSI-HZSPNIEDSA-N 0.000 claims 1
- VFTQZQGHFFDMQS-OFVQYIOZSA-N FC1([C@H](C1)C(=O)N[C@@]12CN(C[C@H]2[C@H]1C)C1=NC(=NC=C1F)NC=1C=NN(C=1)C)F Chemical compound FC1([C@H](C1)C(=O)N[C@@]12CN(C[C@H]2[C@H]1C)C1=NC(=NC=C1F)NC=1C=NN(C=1)C)F VFTQZQGHFFDMQS-OFVQYIOZSA-N 0.000 claims 1
- VFTQZQGHFFDMQS-PYBISEQSSA-N FC1([C@H](C1)C(=O)N[C@]12CN(C[C@@H]2[C@@H]1C)C1=NC(=NC=C1F)NC=1C=NN(C=1)C)F Chemical compound FC1([C@H](C1)C(=O)N[C@]12CN(C[C@@H]2[C@@H]1C)C1=NC(=NC=C1F)NC=1C=NN(C=1)C)F VFTQZQGHFFDMQS-PYBISEQSSA-N 0.000 claims 1
- LRZYHCZKTOWDMP-OIISXLGYSA-N FC1([C@H](C1)CN1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C)F Chemical compound FC1([C@H](C1)CN1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C)F LRZYHCZKTOWDMP-OIISXLGYSA-N 0.000 claims 1
- BQSFRXRHBCYARB-YUELXQCFSA-N FC1([C@H](C1)CN1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C)F Chemical compound FC1([C@H](C1)CN1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NN(C=1)C)F BQSFRXRHBCYARB-YUELXQCFSA-N 0.000 claims 1
- CKKDIYXESFCOLI-PKQAIAMASA-N FC=1C(=NC(=NC=1)NC=1C=NC(=CC=1)CCO)N1C[C@@]2([C@@H]([C@@H]2C1)C)NC(=O)C1CC1 Chemical compound FC=1C(=NC(=NC=1)NC=1C=NC(=CC=1)CCO)N1C[C@@]2([C@@H]([C@@H]2C1)C)NC(=O)C1CC1 CKKDIYXESFCOLI-PKQAIAMASA-N 0.000 claims 1
- XGJMGQJMDCKJJJ-NJPZHQSLSA-N FC=1C(=NC(=NC=1)NC=1C=NC(=CC=1)[C@@H](CO)C)N1C[C@@]2([C@@H]([C@@H]2C1)C)NC(=O)C1CC1 Chemical compound FC=1C(=NC(=NC=1)NC=1C=NC(=CC=1)[C@@H](CO)C)N1C[C@@]2([C@@H]([C@@H]2C1)C)NC(=O)C1CC1 XGJMGQJMDCKJJJ-NJPZHQSLSA-N 0.000 claims 1
- XGJMGQJMDCKJJJ-PPHVIZSJSA-N FC=1C(=NC(=NC=1)NC=1C=NC(=CC=1)[C@H](CO)C)N1C[C@@]2([C@@H]([C@@H]2C1)C)NC(=O)C1CC1 Chemical compound FC=1C(=NC(=NC=1)NC=1C=NC(=CC=1)[C@H](CO)C)N1C[C@@]2([C@@H]([C@@H]2C1)C)NC(=O)C1CC1 XGJMGQJMDCKJJJ-PPHVIZSJSA-N 0.000 claims 1
- KIHZWVVXKDIMBF-YVSFHVDLSA-N F[C@@H]1[C@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C Chemical compound F[C@@H]1[C@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C KIHZWVVXKDIMBF-YVSFHVDLSA-N 0.000 claims 1
- KIHZWVVXKDIMBF-YYIAUSFCSA-N F[C@H]1[C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C Chemical compound F[C@H]1[C@@H](C1)C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=C(C(=NC=1)C(=O)NC)C KIHZWVVXKDIMBF-YYIAUSFCSA-N 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- 206010018634 Gouty Arthritis Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000000112 Myalgia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- XWQKSEWBFRDMOR-LQDVMPOASA-N N1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(CC#N)C Chemical compound N1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2C(CC#N)C XWQKSEWBFRDMOR-LQDVMPOASA-N 0.000 claims 1
- CWFZISZFDCTJJR-GASCZTMLSA-N N1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC1(CC1)C#N Chemical compound N1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CC1(CC1)C#N CWFZISZFDCTJJR-GASCZTMLSA-N 0.000 claims 1
- WPJBRIKPIROPTE-OKILXGFUSA-N N1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CCC#N Chemical compound N1N=CC(=C1)NC1=NC=CC(=N1)N1C[C@H]2CC[C@@H](C1)N2CCC#N WPJBRIKPIROPTE-OKILXGFUSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- FVIKTAZVQBLBAI-BETUJISGSA-N O1N=CC=C1C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NNC=1 Chemical compound O1N=CC=C1C(=O)N1[C@H]2CN(C[C@@H]1CC2)C1=NC(=NC=C1)NC=1C=NNC=1 FVIKTAZVQBLBAI-BETUJISGSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 201000010133 Oligodendroglioma Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 1
- 206010037660 Pyrexia Diseases 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038910 Retinitis Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 201000010001 Silicosis Diseases 0.000 claims 1
- 208000006045 Spondylarthropathies Diseases 0.000 claims 1
- 206010042496 Sunburn Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 206010044248 Toxic shock syndrome Diseases 0.000 claims 1
- 231100000650 Toxic shock syndrome Toxicity 0.000 claims 1
- 208000028552 Treatment-Resistant Depressive disease Diseases 0.000 claims 1
- 206010046914 Vaginal infection Diseases 0.000 claims 1
- 201000008100 Vaginitis Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- 208000006752 brain edema Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 201000003984 candidiasis Diseases 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 201000001981 dermatomyositis Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 206010014599 encephalitis Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- CKJNUZNMWOVDFN-UHFFFAOYSA-N methanone Chemical compound O=[CH-] CKJNUZNMWOVDFN-UHFFFAOYSA-N 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000006938 muscular dystrophy Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- IBBMAWULFFBRKK-UHFFFAOYSA-N picolinamide Chemical compound NC(=O)C1=CC=CC=N1 IBBMAWULFFBRKK-UHFFFAOYSA-N 0.000 claims 1
- 208000005987 polymyositis Diseases 0.000 claims 1
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 1
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims 1
- 201000003651 pulmonary sarcoidosis Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 201000005671 spondyloarthropathy Diseases 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/16—Emollients or protectives, e.g. against radiation
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/02—Antidotes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- H—ELECTRICITY
- H04—ELECTRIC COMMUNICATION TECHNIQUE
- H04N—PICTORIAL COMMUNICATION, e.g. TELEVISION
- H04N7/00—Television systems
- H04N7/18—Closed-circuit television [CCTV] systems, i.e. systems in which the video signal is not broadcast
- H04N7/188—Capturing isolated or intermittent images triggered by the occurrence of a predetermined event, e.g. an object reaching a predetermined position
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Communicable Diseases (AREA)
- Toxicology (AREA)
- Obesity (AREA)
- Pulmonology (AREA)
- Gynecology & Obstetrics (AREA)
- Hospice & Palliative Care (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462039969P | 2014-08-21 | 2014-08-21 | |
EP15766627.2A EP3183247B9 (en) | 2014-08-21 | 2015-08-07 | Aminopyrimidinyl compounds as jak inhibitors |
PCT/IB2015/056021 WO2016027195A1 (en) | 2014-08-21 | 2015-08-07 | Aminopyrimidinyl compounds as jak inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20171913T1 true HRP20171913T1 (hr) | 2018-02-09 |
Family
ID=54148580
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20171913TT HRP20171913T1 (hr) | 2014-08-21 | 2017-12-11 | Aminopirimidinilni spojevi kao inhibitori jak |
Country Status (48)
Families Citing this family (68)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2336117A1 (en) | 2005-05-26 | 2011-06-22 | Neuron Systems, Inc | Heterocyclic compounds for treating retinal diseases |
KR102243169B1 (ko) | 2013-01-23 | 2021-04-22 | 알데이라 테라퓨틱스, 아이엔씨. | 독성 알데히드 관련된 질병 및 치료 |
US10138251B2 (en) | 2014-04-11 | 2018-11-27 | Boehringer Ingelheim International Gmbh | Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-P53 inhibitors |
JP6503386B2 (ja) | 2014-07-03 | 2019-04-17 | 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 | MDM2−p53阻害剤としての新しいスピロ[3H−インドール−3,2’−ピロリジン]−2(1H)−オン化合物および誘導体 |
AU2015306128B2 (en) | 2014-08-21 | 2020-03-26 | Boehringer Ingelheim International Gmbh | New spiro[3H-indole-3,2´-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-p53 inhibitors |
NO2721710T3 (US06244707-20010612-C00010.png) | 2014-08-21 | 2018-03-31 | ||
CA2996183A1 (en) | 2015-08-21 | 2017-03-02 | Aldeyra Therapeutics, Inc. | Deuterated compounds and uses thereof |
EP3347097B1 (en) | 2015-09-11 | 2021-02-24 | Sunshine Lake Pharma Co., Ltd. | Substituted aminopyrimidine derivatives as modulators of the kinases jak, flt3 and aurora |
MX2018004207A (es) | 2015-10-09 | 2018-07-06 | Boehringer Ingelheim Int | Nuevos compuestos de espiro[3h-indol-3,2â´-pirrolidin]-2(1h)-ona y derivados como inhibidores de mdm2-p53. |
KR102244257B1 (ko) * | 2016-04-28 | 2021-04-26 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | Jak 키나제 저해제로서 피리미딘 화합물 |
EP3454858A4 (en) | 2016-05-09 | 2020-01-15 | Aldeyra Therapeutics, Inc. | POLYTHERAPY OF DISORDERS AND INFLAMMATORY EYE DISEASES |
CA3036384A1 (en) | 2016-09-14 | 2018-03-22 | Gilead Sciences, Inc. | Syk inhibitors |
TW201822764A (zh) | 2016-09-14 | 2018-07-01 | 美商基利科學股份有限公司 | Syk抑制劑 |
TWI763722B (zh) * | 2016-10-14 | 2022-05-11 | 美商林伯士拉克許米公司 | Tyk2抑制劑及其用途 |
ES2968462T3 (es) | 2017-03-16 | 2024-05-09 | Aldeyra Therapeutics Inc | Sal polimórfica de 6-cloro-3-amino-2(2-hidroxiprolil) quinolina y usos de la misma |
WO2018195471A1 (en) | 2017-04-21 | 2018-10-25 | Gilead Sciences, Inc. | Syk inhibitors in combination with hypomethylating agents |
CN108864057B (zh) * | 2017-05-16 | 2020-03-31 | 山东大学 | 含有4-氨基吡唑结构的jak与hdac双靶点抑制剂及其制备方法和应用 |
CN109422753B (zh) * | 2017-09-03 | 2021-12-31 | 上海美志医药科技有限公司 | 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物 |
MX2020003425A (es) | 2017-10-10 | 2020-07-29 | Aldeyra Therapeutics Inc | Tratamiento de trastornos inflamatorios. |
PT3672965T (pt) * | 2017-10-27 | 2022-09-29 | Theravance Biopharma R&D Ip Llc | Composto de pirimidina como inibidor de jak cinase |
JP7254076B2 (ja) | 2017-11-19 | 2023-04-07 | サンシャイン・レイク・ファーマ・カンパニー・リミテッド | 置換ヘテロアリール化合物及び使用方法 |
EP3749667A1 (en) | 2018-02-05 | 2020-12-16 | Alkermes, Inc. | Compounds for the treatment of pain |
WO2020017569A1 (ja) | 2018-07-17 | 2020-01-23 | 日本ケミファ株式会社 | T型カルシウムチャネル阻害剤 |
WO2020033344A1 (en) | 2018-08-06 | 2020-02-13 | Aldeyra Therapeutics, Inc. | Polymorphic compounds and uses thereof |
AU2019350717A1 (en) | 2018-09-25 | 2021-05-27 | Cardurion Pharmaceuticals, Llc | Aminopyrimidine compound |
WO2020068846A1 (en) * | 2018-09-25 | 2020-04-02 | Heterocyclic Compound | Heterocyclic compound |
GB201816369D0 (en) | 2018-10-08 | 2018-11-28 | Sareum Ltd | Pharmaceutical compounds |
CN109364248B (zh) * | 2018-10-16 | 2021-05-18 | 哈尔滨医科大学 | ENaC及其抑制剂在预防、缓解和/或治疗动脉粥样硬化中的应用 |
TW202033198A (zh) * | 2018-10-17 | 2020-09-16 | 美商美國禮來大藥廠 | 以巴瑞克替尼(baricitinib)治療原發性膽汁性膽管炎及原發性硬化性膽管炎 |
TWI820301B (zh) * | 2019-02-15 | 2023-11-01 | 美商輝瑞股份有限公司 | 結晶型嘧啶基-3,8-二氮雜雙環〔3.2.1〕辛烷基甲酮化合物及其用途 |
CN111658628B (zh) * | 2019-03-08 | 2022-03-01 | 中国科学院动物研究所 | Gli2抑制剂的用途以及抑制gli2的化合物的筛选方法 |
EP3939979A4 (en) | 2019-03-14 | 2022-04-06 | Shanghai Synergy Pharmaceutical Sciences Co., Ltd | KINASE JAK INHIBITOR, METHOD FOR PREPARING IT AND ITS APPLICATIONS IN THE FIELD OF MEDICINE |
CA3129665A1 (en) | 2019-03-21 | 2020-09-24 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
JPWO2020203609A1 (US06244707-20010612-C00010.png) | 2019-03-29 | 2020-10-08 | ||
PL3958969T3 (pl) | 2019-04-24 | 2024-05-20 | Theravance Biopharma R&D Ip, Llc | Estrowe i węglanowe związki pirymidynowe jako inhibitory kinaz |
CA3135388A1 (en) | 2019-04-24 | 2020-10-29 | Theravance Biopharma R&D Ip, Llc | Pyrimidine jak inhibitors for the treatment of skin diseases |
JP2022537877A (ja) | 2019-04-30 | 2022-08-31 | セルジーン コーポレイション | アプレミラストおよびtyk2阻害剤を含む併用療法 |
US20220348572A1 (en) * | 2019-08-09 | 2022-11-03 | The National Institutes of Pharmaceutical R&D Co., Ltd. | Bridged heterocyclyl-substituted pyrimidine compound, preparation method therefor, and pharmaceutical use thereof |
CA3153676A1 (en) * | 2019-09-11 | 2021-03-18 | Pfizer Inc. | Treatment of hidradenitis with jak inhibitors |
US11992490B2 (en) | 2019-10-16 | 2024-05-28 | Incyte Corporation | Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP) |
CN110862376A (zh) * | 2019-10-24 | 2020-03-06 | 嘉兴特科罗生物科技有限公司 | 一种小分子化合物 |
KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
CN113372364B (zh) * | 2020-03-10 | 2024-05-31 | 明慧医药(上海)有限公司 | 一类jak激酶抑制剂及其制备和应用 |
TW202136269A (zh) * | 2020-03-17 | 2021-10-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 稠合二環類衍生物、其製備方法及其在醫藥上的應用 |
AU2021248720A1 (en) | 2020-04-04 | 2022-11-03 | Pfizer Inc. | Methods of treating coronavirus disease 2019 |
GB202005114D0 (en) | 2020-04-07 | 2020-05-20 | Sareum Ltd | Crystalline Forms of a Pharmaceutical Compound |
CN111423420A (zh) * | 2020-04-30 | 2020-07-17 | 广州博济医药生物技术股份有限公司 | 作为己酮糖激酶抑制剂的并环化合物 |
CN113698403B (zh) * | 2020-05-21 | 2022-06-28 | 南京亘泰医药技术有限公司 | (1r,4r,7r)-7-氨基-2-氮杂双环[2,2,1]庚烷衍生物及制备方法 |
WO2021249367A1 (zh) * | 2020-06-09 | 2021-12-16 | 苏州晶云药物科技股份有限公司 | 二氮杂双环类化合物的对甲苯磺酸盐新晶型及其制备方法 |
TWI785660B (zh) | 2020-07-02 | 2022-12-01 | 美商輝瑞大藥廠 | 嘧啶基-3,8-二氮雜雙環[3.2.1]辛烷基甲酮衍生物及其鹽之製備 |
TWI782599B (zh) * | 2020-07-02 | 2022-11-01 | 美商輝瑞股份有限公司 | 胺基嘧啶基衍生物 |
CA3189561A1 (en) | 2020-07-17 | 2022-01-20 | Pfizer Inc. | Stable pharmaceutical topical formulation containing immunosuppressant for treating dermatological conditions |
MX2023002850A (es) | 2020-09-10 | 2023-07-07 | Precirix N V | Fragmento de anticuerpo contra proteina activadora de fibroblastos (fap). |
AU2022206999A1 (en) * | 2021-01-14 | 2023-07-13 | The National Institutes Of Pharmaceutical R&D Co., Ltd | Bridged heterocyclyl-substituted pyrimidine compounds, preparation method and medical use thereof |
CN114835717A (zh) * | 2021-02-01 | 2022-08-02 | 杭州领业医药科技有限公司 | Brepocitinib甲苯磺酸盐的晶型及其制备方法和用途 |
AU2022239717A1 (en) | 2021-03-15 | 2023-11-02 | Maze Therapeutics, Inc. | Inhibitors of glycogen synthase 1 (gys1) and methods of use thereof |
CN113698409B (zh) * | 2021-08-10 | 2022-07-19 | 上海凌凯医药科技有限公司 | 一种多用途的二氮杂双环类化合物、制备方法及在合成药物中的应用 |
CN113999239B (zh) * | 2021-07-14 | 2022-11-11 | 上海凌富药物研究有限公司 | 一种二氮杂桥化合物的合成方法 |
CN113461687B (zh) * | 2021-08-10 | 2022-04-19 | 四川大学华西医院 | 2,8-氮杂-[4,5]十螺环酮衍生物及其制备方法和用途 |
CA3231865A1 (en) * | 2021-09-17 | 2023-03-23 | Tingting SHANG | Fused bicyclic derivative, pharmaceutically acceptable salt, crystal form thereof and preparation method therefor |
CA3236262A1 (en) | 2021-10-25 | 2023-05-04 | Isaac Marx | Tyk2 degraders and uses thereof |
CN114181097B (zh) * | 2021-12-10 | 2024-05-14 | 广东嘉博制药有限公司 | 一种盐酸甲氧明的合成方法 |
US20230293544A1 (en) * | 2022-03-17 | 2023-09-21 | Pfizer Inc. | Methods, dosage regimens, and compositions for treating hidradenitis |
WO2023203135A1 (en) | 2022-04-22 | 2023-10-26 | Precirix N.V. | Improved radiolabelled antibody |
WO2023213801A1 (en) | 2022-05-02 | 2023-11-09 | Precirix N.V. | Pre-targeting |
CN118005609A (zh) * | 2022-11-09 | 2024-05-10 | 沈阳药科大学 | 2-氨基嘧啶类化合物及其用途 |
CN116396298A (zh) * | 2023-06-06 | 2023-07-07 | 四川维亚本苑生物科技有限公司 | CDK Ligand-1的中间体XII及CDK Ligand-1的制备方法 |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE4131139A1 (de) | 1991-09-19 | 1993-03-25 | Bayer Ag | Verfahren zur herstellung von 1-fluor-cyclopropan-1-carbonsaeure |
US7381833B2 (en) | 2004-03-31 | 2008-06-03 | Daiichi Pharmaceutical Co., Ltd. | Process for producing 1,2-cis-2-fluorocyclopropane-1-carboxylic ester compound |
JPWO2006109846A1 (ja) | 2005-04-06 | 2008-11-20 | 武田薬品工業株式会社 | トリアゾール誘導体およびその用途 |
CA2625109A1 (en) | 2005-10-13 | 2007-04-19 | Glaxo Group Limited | Pyrrolopyrimidine derivatives as syk inhibitors |
NL2000323C2 (nl) | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine-derivaten. |
NZ592968A (en) * | 2006-01-17 | 2012-08-31 | Vertex Pharma | Azaindoles substituted with either triazine or pyrimidine useful as inhibitors of janus kinases consisting of JAK1, JAK2, JAK3, and TYK2 |
WO2008032033A1 (en) * | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
CN101595103A (zh) * | 2006-09-14 | 2009-12-02 | 阿斯利康(瑞典)有限公司 | 嘧啶衍生物 |
CL2008000467A1 (es) * | 2007-02-14 | 2008-08-22 | Janssen Pharmaceutica Nv | Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma |
CN101679440A (zh) * | 2007-04-02 | 2010-03-24 | 帕劳制药股份有限公司 | 作为jak3抑制剂的吡咯并嘧啶衍生物 |
WO2009005675A1 (en) | 2007-06-28 | 2009-01-08 | Abbott Laboratories | Novel triazolopyridazines |
US8076491B2 (en) | 2007-08-21 | 2011-12-13 | Senomyx, Inc. | Compounds that inhibit (block) bitter taste in composition and use thereof |
JP5368556B2 (ja) | 2008-07-16 | 2013-12-18 | エフ.ホフマン−ラ ロシュ アーゲー | 心臓血管疾患の処置のための新規ヘテロシクリル化合物 |
WO2010075273A1 (en) | 2008-12-23 | 2010-07-01 | Schering Corporation | Bicyclic heterocycle derivatives and methods of use thereof |
US9346809B2 (en) * | 2009-07-08 | 2016-05-24 | Leo Pharma A/S | Heterocyclic compounds as JAK receptor and protein tyrosine kinase inhibitors |
WO2012022681A2 (en) | 2010-08-20 | 2012-02-23 | Cellzome Limited | Heterocyclyl pyrazolopyrimidine analogues as selective jak inhibitors |
CA2849336A1 (en) | 2011-09-22 | 2013-03-29 | Merck Sharp & Dohme Corp. | Cyanomethylpyrazole carboxamides as janus kinase inhibitors |
BR112014014675A2 (pt) | 2011-12-16 | 2017-06-13 | Invista Tech Sarl | método para biossintetizar um ou mais produtos e hospedeiro recombinante |
AU2015306128B2 (en) | 2014-08-21 | 2020-03-26 | Boehringer Ingelheim International Gmbh | New spiro[3H-indole-3,2´-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-p53 inhibitors |
NO2721710T3 (US06244707-20010612-C00010.png) | 2014-08-21 | 2018-03-31 |
-
2012
- 2012-06-19 NO NO12803361A patent/NO2721710T3/no unknown
-
2015
- 2015-08-07 SG SG11201700957WA patent/SG11201700957WA/en unknown
- 2015-08-07 UA UAA201701672A patent/UA117976C2/uk unknown
- 2015-08-07 EP EP15766627.2A patent/EP3183247B9/en active Active
- 2015-08-07 PT PT157666272T patent/PT3183247T/pt unknown
- 2015-08-07 MD MDA20170016A patent/MD4800C1/ro active IP Right Grant
- 2015-08-07 MA MA040587A patent/MA40587A/fr unknown
- 2015-08-07 KR KR1020177007276A patent/KR101877189B1/ko active IP Right Grant
- 2015-08-07 MX MX2017002241A patent/MX2017002241A/es active IP Right Grant
- 2015-08-07 RS RS20180079A patent/RS56807B1/sr unknown
- 2015-08-07 HU HUE15766627A patent/HUE035553T2/hu unknown
- 2015-08-07 SI SI201530156T patent/SI3183247T1/en unknown
- 2015-08-07 CN CN201580057140.5A patent/CN107074867B/zh active Active
- 2015-08-07 AU AU2015304883A patent/AU2015304883B2/en active Active
- 2015-08-07 AP AP2017009748A patent/AP2017009748A0/en unknown
- 2015-08-07 CU CU2017000015A patent/CU24435B1/es unknown
- 2015-08-07 ES ES15766627.2T patent/ES2655971T3/es active Active
- 2015-08-07 JP JP2017509666A patent/JP6218260B2/ja active Active
- 2015-08-07 ME MEP-2017-284A patent/ME02856B/me unknown
- 2015-08-07 PL PL15766627T patent/PL3183247T3/pl unknown
- 2015-08-07 PE PE2017000248A patent/PE20171177A1/es unknown
- 2015-08-07 DK DK15766627.2T patent/DK3183247T3/en active
- 2015-08-07 MY MYPI2017700538A patent/MY192109A/en unknown
- 2015-08-07 EA EA201700077A patent/EA032609B1/ru unknown
- 2015-08-07 WO PCT/IB2015/056021 patent/WO2016027195A1/en active Application Filing
- 2015-08-07 GE GEAP201514430A patent/GEP20197003B/en unknown
- 2015-08-07 BR BR112017003054-3A patent/BR112017003054B1/pt active IP Right Grant
- 2015-08-07 TN TN2017000044A patent/TN2017000044A1/en unknown
- 2015-08-07 LT LTEP15766627.2T patent/LT3183247T/lt unknown
- 2015-08-07 CR CR20170066A patent/CR20170066A/es unknown
- 2015-08-07 NZ NZ729005A patent/NZ729005A/en unknown
- 2015-08-18 CA CA2900855A patent/CA2900855C/en active Active
- 2015-08-19 US US14/829,753 patent/US9663526B2/en active Active
- 2015-08-19 UY UY0001036275A patent/UY36275A/es active IP Right Grant
- 2015-08-20 TW TW104127204A patent/TWI583681B/zh active
- 2015-08-20 AR ARP150102681A patent/AR101599A1/es active IP Right Grant
-
2017
- 2017-02-09 ZA ZA2017/01005A patent/ZA201701005B/en unknown
- 2017-02-14 PH PH12017500276A patent/PH12017500276A1/en unknown
- 2017-02-16 EC ECIEPI201710156A patent/ECSP17010156A/es unknown
- 2017-02-16 SV SV2017005384A patent/SV2017005384A/es unknown
- 2017-02-17 CO CONC2017/0001603A patent/CO2017001603A2/es unknown
- 2017-02-20 NI NI201700020A patent/NI201700020A/es unknown
- 2017-02-20 CL CL2017000406A patent/CL2017000406A1/es unknown
- 2017-02-21 DO DO2017000048A patent/DOP2017000048A/es unknown
- 2017-02-21 IL IL250709A patent/IL250709B/en active IP Right Grant
- 2017-02-21 GT GT201700035A patent/GT201700035A/es unknown
- 2017-05-03 US US15/585,626 patent/US10463675B2/en active Active
- 2017-12-11 HR HRP20171913TT patent/HRP20171913T1/hr unknown
-
2018
- 2018-01-10 CY CY20181100036T patent/CY1119771T1/el unknown
-
2019
- 2019-09-24 US US16/580,667 patent/US10980815B2/en active Active
-
2020
- 2020-07-02 US US16/920,027 patent/US11197867B2/en active Active
-
2021
- 2021-08-06 US US17/396,094 patent/US20210377495A1/en not_active Abandoned
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
HRP20171913T1 (hr) | Aminopirimidinilni spojevi kao inhibitori jak | |
JP2016523911A5 (US06244707-20010612-C00010.png) | ||
JP2019535664A5 (US06244707-20010612-C00010.png) | ||
AU2012299080B2 (en) | Pyrimidine PDE10 inhibitors | |
JP2018534326A5 (US06244707-20010612-C00010.png) | ||
JP2013515729A5 (US06244707-20010612-C00010.png) | ||
HRP20160326T1 (hr) | Derivati piperidin-4-il azetidina kao inhibitori jak1 | |
RU2019115115A (ru) | Производные пиперидина в качестве ингибиторов убиквитин-специфической протеазы 7 | |
HRP20140778T1 (hr) | Derivati tetrahidro-pirido-pirimidina | |
JP2013533300A (ja) | ブルトン型チロシンキナーゼの阻害剤 | |
JP2018503673A5 (US06244707-20010612-C00010.png) | ||
JP2017524007A5 (US06244707-20010612-C00010.png) | ||
EP3209664A1 (en) | Bicyclic heteroaryl amine compounds as pi3k inhibitors | |
JP2020502230A5 (US06244707-20010612-C00010.png) | ||
EA037598B1 (ru) | Производные 3-((гетеро-)арил)-8-амино-2-оксо-1,3-диазаспиро[4,5]декана | |
HRP20161495T1 (hr) | Novi derivati pirimidina kao inhibitori fosfodiesteraze 10 (pde-10) | |
WO2023076133A1 (en) | Spirotricycle ripk1 inhibitors and methods of uses thereof | |
OA18225A (en) | Aminopyrimidinyl compounds as Jak inhibitors. | |
RU2021138377A (ru) | Производные пиридопиримидинов в качестве ингибиторов p2x3 | |
JPWO2020239953A5 (US06244707-20010612-C00010.png) |