TW202302589A - 作為ｊａｋ２ ｖ６１７ｆ抑制劑之螺環內醯胺 - Google Patents
作為ｊａｋ２ ｖ６１７ｆ抑制劑之螺環內醯胺 Download PDFInfo
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- TW202302589A TW202302589A TW111106834A TW111106834A TW202302589A TW 202302589 A TW202302589 A TW 202302589A TW 111106834 A TW111106834 A TW 111106834A TW 111106834 A TW111106834 A TW 111106834A TW 202302589 A TW202302589 A TW 202302589A
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- alkyl
- cycloalkyl
- independently selected
- methyl
- membered heterocycloalkyl
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- 239000003112 inhibitor Substances 0.000 title 1
- 150000003951 lactams Chemical class 0.000 title 1
- -1 lactam compounds Chemical class 0.000 claims abstract description 294
- 102200087780 rs77375493 Human genes 0.000 claims abstract description 8
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims abstract description 7
- 206010028980 Neoplasm Diseases 0.000 claims abstract description 7
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims abstract description 7
- 201000011510 cancer Diseases 0.000 claims abstract description 7
- 230000000694 effects Effects 0.000 claims abstract description 5
- 125000000217 alkyl group Chemical group 0.000 claims description 1410
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 733
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 549
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims description 449
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 443
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 419
- 125000001424 substituent group Chemical group 0.000 claims description 359
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 316
- 125000003118 aryl group Chemical group 0.000 claims description 287
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 285
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 274
- 229910052799 carbon Inorganic materials 0.000 claims description 258
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims description 236
- 125000006719 (C6-C10) aryl (C1-C6) alkyl group Chemical group 0.000 claims description 234
- 229910052739 hydrogen Inorganic materials 0.000 claims description 206
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 184
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 143
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 84
- 150000001875 compounds Chemical class 0.000 claims description 83
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 77
- 125000001072 heteroaryl group Chemical group 0.000 claims description 75
- 150000003839 salts Chemical class 0.000 claims description 73
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 70
- 125000005843 halogen group Chemical group 0.000 claims description 65
- 125000003386 piperidinyl group Chemical group 0.000 claims description 61
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 54
- 125000003545 alkoxy group Chemical group 0.000 claims description 53
- 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 53
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 52
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 48
- 229910052760 oxygen Inorganic materials 0.000 claims description 48
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 46
- 125000002393 azetidinyl group Chemical group 0.000 claims description 44
- 150000001335 aliphatic alkanes Chemical class 0.000 claims description 40
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 38
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 38
- 239000001301 oxygen Substances 0.000 claims description 36
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 35
- 125000002619 bicyclic group Chemical group 0.000 claims description 34
- 125000003725 azepanyl group Chemical group 0.000 claims description 32
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims description 31
- 125000004925 dihydropyridyl group Chemical group N1(CC=CC=C1)* 0.000 claims description 26
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 24
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 24
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims description 21
- 125000002950 monocyclic group Chemical group 0.000 claims description 20
- 150000001924 cycloalkanes Chemical class 0.000 claims description 17
- 238000006467 substitution reaction Methods 0.000 claims description 17
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 16
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 16
- 238000000034 method Methods 0.000 claims description 16
- 229910052721 tungsten Inorganic materials 0.000 claims description 16
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 14
- 125000004674 methylcarbonyl group Chemical group CC(=O)* 0.000 claims description 13
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 11
- 229910052736 halogen Inorganic materials 0.000 claims description 11
- 150000002367 halogens Chemical class 0.000 claims description 11
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims description 11
- 229910052727 yttrium Inorganic materials 0.000 claims description 11
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 10
- 125000004639 dihydroindenyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 10
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 10
- 150000001345 alkine derivatives Chemical class 0.000 claims description 9
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 9
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 9
- 125000006125 ethylsulfonyl group Chemical group 0.000 claims description 8
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 claims description 8
- 125000003003 spiro group Chemical group 0.000 claims description 8
- 125000005936 piperidyl group Chemical group 0.000 claims description 7
- 125000004673 propylcarbonyl group Chemical group 0.000 claims description 7
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims description 6
- 150000001336 alkenes Chemical class 0.000 claims description 6
- 125000000304 alkynyl group Chemical group 0.000 claims description 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 6
- 125000001188 haloalkyl group Chemical group 0.000 claims description 6
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 claims description 6
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims description 6
- 150000001350 alkyl halides Chemical class 0.000 claims description 5
- 230000037429 base substitution Effects 0.000 claims description 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 5
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims description 4
- 125000003705 anilinocarbonyl group Chemical group O=C([*])N([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 125000005958 tetrahydrothienyl group Chemical group 0.000 claims description 4
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical group C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 3
- 229910052805 deuterium Inorganic materials 0.000 claims description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 3
- 108091000080 Phosphotransferase Proteins 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 102000020233 phosphotransferase Human genes 0.000 claims description 2
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 84
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 28
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 10
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 8
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims 6
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims 6
- 125000005344 pyridylmethyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 claims 6
- 125000000168 pyrrolyl group Chemical group 0.000 claims 6
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 5
- 229910052731 fluorine Inorganic materials 0.000 claims 5
- 239000011737 fluorine Substances 0.000 claims 5
- 125000001041 indolyl group Chemical group 0.000 claims 5
- 125000000335 thiazolyl group Chemical group 0.000 claims 5
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 5
- 229920002554 vinyl polymer Polymers 0.000 claims 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 4
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 206010025323 Lymphomas Diseases 0.000 claims 3
- WMSPXQIQBQAWLL-UHFFFAOYSA-N cyclopropanesulfonamide Chemical compound NS(=O)(=O)C1CC1 WMSPXQIQBQAWLL-UHFFFAOYSA-N 0.000 claims 3
- 125000004431 deuterium atom Chemical group 0.000 claims 3
- 125000006001 difluoroethyl group Chemical group 0.000 claims 3
- 206010028537 myelofibrosis Diseases 0.000 claims 3
- 125000004205 trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 3
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 208000003476 primary myelofibrosis Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- LQKUERRPRLVSLZ-UHFFFAOYSA-N 5,6-dihydro-4h-pyrrolo[1,2-b]pyrazole Chemical compound C1=NN2CCCC2=C1 LQKUERRPRLVSLZ-UHFFFAOYSA-N 0.000 claims 1
- 208000002008 AIDS-Related Lymphoma Diseases 0.000 claims 1
- 208000009746 Adult T-Cell Leukemia-Lymphoma Diseases 0.000 claims 1
- 208000016683 Adult T-cell leukemia/lymphoma Diseases 0.000 claims 1
- 206010061424 Anal cancer Diseases 0.000 claims 1
- 208000007860 Anus Neoplasms Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- VGNVVBGRCRXUQZ-UHFFFAOYSA-N CC(C)(C1CNC1)N(CC1)CCC1(C1=C(C(C2=CC=C3N(C)N=CC3=C2)=C(C2=CN(C)N=C2)N2)C2=NC=C1N1C)C1=O Chemical compound CC(C)(C1CNC1)N(CC1)CCC1(C1=C(C(C2=CC=C3N(C)N=CC3=C2)=C(C2=CN(C)N=C2)N2)C2=NC=C1N1C)C1=O VGNVVBGRCRXUQZ-UHFFFAOYSA-N 0.000 claims 1
- QYDDPRJPHKJUKF-UHFFFAOYSA-N CC(CC#N)N1N=CC(C(C=C2)=CC=C2C(C2=C3C45CCCC4)=C(C4=CN(C)N=C4)NC2=NC=C3N(C)C5=O)=C1 Chemical compound CC(CC#N)N1N=CC(C(C=C2)=CC=C2C(C2=C3C45CCCC4)=C(C4=CN(C)N=C4)NC2=NC=C3N(C)C5=O)=C1 QYDDPRJPHKJUKF-UHFFFAOYSA-N 0.000 claims 1
- XSOVTYZLHRVFJB-UHFFFAOYSA-N CC(N(C(CC1)C2)C1CC2(C1=C(C(C2=CC=CC=C2)=C(C2=CC=C(CN(CC3)CCC3S(C)(=O)=O)C=C2)N2)C2=NC=C1N1C)C1=O)=O Chemical compound CC(N(C(CC1)C2)C1CC2(C1=C(C(C2=CC=CC=C2)=C(C2=CC=C(CN(CC3)CCC3S(C)(=O)=O)C=C2)N2)C2=NC=C1N1C)C1=O)=O XSOVTYZLHRVFJB-UHFFFAOYSA-N 0.000 claims 1
- KXVRJCVGOBSVPS-UHFFFAOYSA-N CC(N(C1)CC1(CC#N)N(CC1)CCC1(C1=C(C(C2=CC=CC=C2)=C(C2=CN(C)N=C2)N2)C2=NC=C1N1C)C1=O)=O Chemical compound CC(N(C1)CC1(CC#N)N(CC1)CCC1(C1=C(C(C2=CC=CC=C2)=C(C2=CN(C)N=C2)N2)C2=NC=C1N1C)C1=O)=O KXVRJCVGOBSVPS-UHFFFAOYSA-N 0.000 claims 1
- CUMQZDYAGSUXGK-UHFFFAOYSA-N CC1=NC=C(C(C2=C3C4(CC5)CCN5C5=NC=NC=C5)=C(C5=CN(C)N=C5)NC2=NC=C3N(C)C4=O)S1 Chemical compound CC1=NC=C(C(C2=C3C4(CC5)CCN5C5=NC=NC=C5)=C(C5=CN(C)N=C5)NC2=NC=C3N(C)C4=O)S1 CUMQZDYAGSUXGK-UHFFFAOYSA-N 0.000 claims 1
- RRRFNANMVBSSEL-UHFFFAOYSA-N CCC(C1=C2C3(CC4)CCN4C4=NC=NC=C4)=C(C4=CN(C)N=C4)NC1=NC=C2N(C)C3=O Chemical compound CCC(C1=C2C3(CC4)CCN4C4=NC=NC=C4)=C(C4=CN(C)N=C4)NC1=NC=C2N(C)C3=O RRRFNANMVBSSEL-UHFFFAOYSA-N 0.000 claims 1
- ILGFCDIAVHMDMR-UHFFFAOYSA-N CCCC(N1CCC(C2)(CC2(C2=C(C(C3=CC=C4N(C)N=CC4=C3)=C(C3=CN(C)N=C3)N3)C3=NC=C2N2C)C2=O)CC1)=O Chemical compound CCCC(N1CCC(C2)(CC2(C2=C(C(C3=CC=C4N(C)N=CC4=C3)=C(C3=CN(C)N=C3)N3)C3=NC=C2N2C)C2=O)CC1)=O ILGFCDIAVHMDMR-UHFFFAOYSA-N 0.000 claims 1
- GPNPVSNYVVYUAM-UHFFFAOYSA-N CCNC(N(C1)CC1(CC#N)N(CC1)CCC1(C1=C(C(C2=CC=CC=C2)=C(C2=CN(C)N=C2)N2)C2=NC=C1N1C)C1=O)=O Chemical compound CCNC(N(C1)CC1(CC#N)N(CC1)CCC1(C1=C(C(C2=CC=CC=C2)=C(C2=CN(C)N=C2)N2)C2=NC=C1N1C)C1=O)=O GPNPVSNYVVYUAM-UHFFFAOYSA-N 0.000 claims 1
- OTQBXSFSRVJQHX-UHFFFAOYSA-N CCNC(NC(C1)CC1(CC#N)N(CC1)CCC1(C1=C(C(C2=CC=CC=C2)=C(C2=CN(C)N=C2)N2)C2=NC=C1N1C)C1=O)=O Chemical compound CCNC(NC(C1)CC1(CC#N)N(CC1)CCC1(C1=C(C(C2=CC=CC=C2)=C(C2=CN(C)N=C2)N2)C2=NC=C1N1C)C1=O)=O OTQBXSFSRVJQHX-UHFFFAOYSA-N 0.000 claims 1
- CKDCCNOEKCAACU-UHFFFAOYSA-N CCS(C(C=C1)=CC=C1C(NC(C1=C2C3(CC4)CCN4C4(CC#N)CCC4)=NC=C2N(C)C3=O)=C1C1=CC=C2N(C)N=CC2=C1)(=O)=O Chemical compound CCS(C(C=C1)=CC=C1C(NC(C1=C2C3(CC4)CCN4C4(CC#N)CCC4)=NC=C2N(C)C3=O)=C1C1=CC=C2N(C)N=CC2=C1)(=O)=O CKDCCNOEKCAACU-UHFFFAOYSA-N 0.000 claims 1
- RNQKWQJXVHEBOF-UHFFFAOYSA-N CN(C(C(CC1)(CCN1C1(CC#N)CCC1)C1=C23)=O)C1=CN=C2NC(C1=CN(CCOC)N=C1)=C3C1=CC=C2N(C)N=CC2=C1 Chemical compound CN(C(C(CC1)(CCN1C1(CC#N)CCC1)C1=C23)=O)C1=CN=C2NC(C1=CN(CCOC)N=C1)=C3C1=CC=C2N(C)N=CC2=C1 RNQKWQJXVHEBOF-UHFFFAOYSA-N 0.000 claims 1
- DDJFACKLWXBWFR-UHFFFAOYSA-N CN(C(C(CC1)(CN1C(CC1CCOCC1)=O)C1=C23)=O)C1=CN=C2NC(C1=CC=C(CN(CC2)CCC2S(C)(=O)=O)C=C1)=C3C1=CC=CC=C1 Chemical compound CN(C(C(CC1)(CN1C(CC1CCOCC1)=O)C1=C23)=O)C1=CN=C2NC(C1=CC=C(CN(CC2)CCC2S(C)(=O)=O)C=C1)=C3C1=CC=CC=C1 DDJFACKLWXBWFR-UHFFFAOYSA-N 0.000 claims 1
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- MCPWUDGVOZZXCK-UHFFFAOYSA-N CN(C(C1(CCOCC1)C1=C23)=O)C1=CN=C2NC(C1=CC=C(CN(CC2)CCC2S(C)(=O)=O)C=C1)=C3C1=CC=CC=C1 Chemical compound CN(C(C1(CCOCC1)C1=C23)=O)C1=CN=C2NC(C1=CC=C(CN(CC2)CCC2S(C)(=O)=O)C=C1)=C3C1=CC=CC=C1 MCPWUDGVOZZXCK-UHFFFAOYSA-N 0.000 claims 1
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- PCNWXFIMTKFYRK-UHFFFAOYSA-N CN(C)C(N1CCC(C2)(CC2(C2=C(C(C3=CC=C4N(C)N=CC4=C3)=C(C3=CN(C)N=C3)N3)C3=NC=C2N2C)C2=O)CC1)=O Chemical compound CN(C)C(N1CCC(C2)(CC2(C2=C(C(C3=CC=C4N(C)N=CC4=C3)=C(C3=CN(C)N=C3)N3)C3=NC=C2N2C)C2=O)CC1)=O PCNWXFIMTKFYRK-UHFFFAOYSA-N 0.000 claims 1
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- A61P35/00—Antineoplastic agents
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
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- A—HUMAN NECESSITIES
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- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/18—Bridged systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/20—Spiro-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
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- 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
Landscapes
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- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
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- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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| US4698341A (en) | 1983-07-30 | 1987-10-06 | Godecke Aktiengesellschaft | Use of 1,6-naphthyridinone derivatives in treating pulmonary thrombosis |
| JPS62209062A (ja) | 1986-03-10 | 1987-09-14 | Yamanouchi Pharmaceut Co Ltd | ２−ピリジルメチルチオ−または２−ピリジルメチルスルフイニル−置換縮合環化合物 |
| DE3804990A1 (de) | 1988-02-18 | 1989-08-31 | Basf Ag | Herbizid wirksame, heterocyclisch substituierte sulfonamide |
| CA2053148A1 (en) | 1990-10-16 | 1992-04-17 | Karnail Atwal | Dihydropyrimidine derivatives |
| US5326776A (en) | 1992-03-02 | 1994-07-05 | Abbott Laboratories | Angiotensin II receptor antagonists |
| WO1993017682A1 (en) | 1992-03-04 | 1993-09-16 | Abbott Laboratories | Angiotensin ii receptor antagonists |
| JPH0789957A (ja) | 1993-09-22 | 1995-04-04 | Nissan Chem Ind Ltd | ビフェニルメチルアミン誘導体 |
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| DE4344452A1 (de) | 1993-12-24 | 1995-06-29 | Hoechst Ag | Aza-4-iminochinoline, Verfahren zu ihrer Herstellung und ihre Verwendung |
| AR006520A1 (es) | 1996-03-20 | 1999-09-08 | Astra Pharma Prod | Derivados de 2-arilpirazolisoquinolina y cinolinona y procedimiento para su preparacion. |
| WO1997047601A1 (en) | 1996-06-11 | 1997-12-18 | Yoshitomi Pharmaceutical Industries, Ltd. | Fused heterocyclic compounds and medicinal uses thereof |
| BR9714349A (pt) | 1996-10-16 | 2000-11-14 | Icn Pharmaceuticals | L-nucleosìdeos purina, seus análogos e utilizacões dos mesmos |
| US6177464B1 (en) | 1997-03-14 | 2001-01-23 | Sepracor, Inc. | Ring opening metathesis of alkenes |
| US6339099B1 (en) | 1997-06-20 | 2002-01-15 | Dupont Pharmaceuticals Company | Guanidine mimics as factor Xa inhibitors |
| TR200003429T2 (tr) | 1998-05-26 | 2001-07-23 | Warner-Lambert Company | Hücresel çoğalma inhibitörleri olarak bisiklik pirimidinler ve bisiklik 3,4-dihidropirimidinler. |
| JP2002517486A (ja) | 1998-06-12 | 2002-06-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | ｐ３８のインヒビター |
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| EP4298099A1 (en) | 2024-01-03 |
| AR125273A1 (es) | 2023-07-05 |
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