RU2378263C2 - Производные 5-фенилтиазола и их применение в качестве ингибиторов рi3 киназы - Google Patents
Производные 5-фенилтиазола и их применение в качестве ингибиторов рi3 киназы Download PDFInfo
- Publication number
- RU2378263C2 RU2378263C2 RU2004129279/04A RU2004129279A RU2378263C2 RU 2378263 C2 RU2378263 C2 RU 2378263C2 RU 2004129279/04 A RU2004129279/04 A RU 2004129279/04A RU 2004129279 A RU2004129279 A RU 2004129279A RU 2378263 C2 RU2378263 C2 RU 2378263C2
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- Prior art keywords
- alkyl
- optionally substituted
- ring
- hydroxy
- displaced
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- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 39
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims abstract 31
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims abstract 27
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 22
- 239000001257 hydrogen Substances 0.000 claims abstract 21
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 21
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims abstract 20
- 150000002825 nitriles Chemical class 0.000 claims abstract 17
- 229910052736 halogen Inorganic materials 0.000 claims abstract 16
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract 16
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims abstract 15
- -1 1-piperidyl Chemical group 0.000 claims abstract 13
- 150000002367 halogens Chemical class 0.000 claims abstract 13
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims abstract 12
- 238000000034 method Methods 0.000 claims abstract 12
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 12
- 239000001301 oxygen Substances 0.000 claims abstract 12
- 150000002431 hydrogen Chemical class 0.000 claims abstract 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 8
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims abstract 5
- 201000010099 disease Diseases 0.000 claims abstract 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 5
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims abstract 4
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims abstract 3
- 206010012601 diabetes mellitus Diseases 0.000 claims abstract 3
- 238000004519 manufacturing process Methods 0.000 claims abstract 3
- 230000001404 mediated effect Effects 0.000 claims abstract 3
- 201000001320 Atherosclerosis Diseases 0.000 claims abstract 2
- 206010020751 Hypersensitivity Diseases 0.000 claims abstract 2
- 206010028980 Neoplasm Diseases 0.000 claims abstract 2
- 201000004681 Psoriasis Diseases 0.000 claims abstract 2
- 230000007815 allergy Effects 0.000 claims abstract 2
- 201000011510 cancer Diseases 0.000 claims abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 29
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000005842 heteroatom Chemical group 0.000 claims 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 125000001188 haloalkyl group Chemical group 0.000 claims 7
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 5
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 4
- 238000006243 chemical reaction Methods 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 108091007960 PI3Ks Proteins 0.000 claims 3
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 claims 3
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 claims 2
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims 2
- 229910052783 alkali metal Inorganic materials 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 230000003993 interaction Effects 0.000 claims 2
- 239000008177 pharmaceutical agent Substances 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000011623 Obstructive Lung disease Diseases 0.000 claims 1
- 208000025747 Rheumatic disease Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical group C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- OKJPEAGHQZHRQV-UHFFFAOYSA-N Triiodomethane Natural products IC(I)I OKJPEAGHQZHRQV-UHFFFAOYSA-N 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 150000001350 alkyl halides Chemical class 0.000 claims 1
- 229910021529 ammonia Inorganic materials 0.000 claims 1
- 239000003054 catalyst Substances 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- WBJINCZRORDGAQ-UHFFFAOYSA-N ethyl formate Chemical compound CCOC=O WBJINCZRORDGAQ-UHFFFAOYSA-N 0.000 claims 1
- 230000026030 halogenation Effects 0.000 claims 1
- 238000005658 halogenation reaction Methods 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- INQOMBQAUSQDDS-UHFFFAOYSA-N iodomethane Chemical compound IC INQOMBQAUSQDDS-UHFFFAOYSA-N 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002560 nitrile group Chemical group 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 229910052763 palladium Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- YBBRCQOCSYXUOC-UHFFFAOYSA-N sulfuryl dichloride Chemical compound ClS(Cl)(=O)=O YBBRCQOCSYXUOC-UHFFFAOYSA-N 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 229910052723 transition metal Inorganic materials 0.000 claims 1
- 150000003624 transition metals Chemical class 0.000 claims 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 17
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 1
- 208000026935 allergic disease Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
- 0 CC(C=C(**)C(*)=C1)(C=C1c1c(*)nc(N*)[s]1)S Chemical compound CC(C=C(**)C(*)=C1)(C=C1c1c(*)nc(N*)[s]1)S 0.000 description 1
Classifications
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- C07—ORGANIC CHEMISTRY
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- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/40—Unsubstituted amino or imino radicals
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- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
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- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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