JP2011503068A5 - - Google Patents
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- Publication number
- JP2011503068A5 JP2011503068A5 JP2010533113A JP2010533113A JP2011503068A5 JP 2011503068 A5 JP2011503068 A5 JP 2011503068A5 JP 2010533113 A JP2010533113 A JP 2010533113A JP 2010533113 A JP2010533113 A JP 2010533113A JP 2011503068 A5 JP2011503068 A5 JP 2011503068A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halo
- alkoxy
- cycloalkyl
- alkylamino
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000005843 halogen group Chemical group 0.000 claims 209
- 125000003545 alkoxy group Chemical group 0.000 claims 126
- 125000000217 alkyl group Chemical group 0.000 claims 105
- 150000001875 compounds Chemical class 0.000 claims 61
- -1 O Seo Chemical group 0.000 claims 45
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 43
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 42
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 41
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 40
- 125000001072 heteroaryl group Chemical group 0.000 claims 39
- 125000000753 cycloalkyl group Chemical group 0.000 claims 38
- 125000003282 alkyl amino group Chemical group 0.000 claims 35
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 31
- 125000004043 oxo group Chemical group O=* 0.000 claims 31
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 30
- 125000005366 cycloalkylthio group Chemical group 0.000 claims 30
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 29
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 27
- 125000004414 alkyl thio group Chemical group 0.000 claims 23
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 23
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 21
- 229910052731 fluorine Inorganic materials 0.000 claims 21
- 239000011737 fluorine Substances 0.000 claims 21
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 21
- 150000001408 amides Chemical class 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 20
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 19
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 19
- 125000004093 cyano group Chemical group *C#N 0.000 claims 19
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 claims 18
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 17
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 16
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims 16
- 229910052801 chlorine Inorganic materials 0.000 claims 16
- 239000000460 chlorine Substances 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 16
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 16
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 15
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 15
- 229910052794 bromium Inorganic materials 0.000 claims 15
- 125000005148 cycloalkylalkanesulfinyl group Chemical group 0.000 claims 15
- 125000006517 heterocyclyl carbonyl group Chemical group 0.000 claims 15
- 125000003342 alkenyl group Chemical group 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 12
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 12
- 125000002947 alkylene group Chemical group 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 11
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 11
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 10
- 125000004663 dialkyl amino group Chemical group 0.000 claims 10
- 125000001188 haloalkyl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 10
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 9
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 9
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 claims 9
- 125000000304 alkynyl group Chemical group 0.000 claims 9
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 9
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 8
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000001769 aryl amino group Chemical group 0.000 claims 6
- 125000005241 heteroarylamino group Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 125000004076 pyridyl group Chemical group 0.000 claims 6
- 125000004845 (C1-C6) alkylsulfonylamino group Chemical group 0.000 claims 5
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 5
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 5
- 125000005167 cycloalkylaminocarbonyl group Chemical group 0.000 claims 5
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000004738 (C1-C6) alkyl sulfinyl group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000005145 cycloalkylaminosulfonyl group Chemical group 0.000 claims 4
- 125000005529 alkyleneoxy group Chemical group 0.000 claims 3
- 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 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 3
- 229920002554 vinyl polymer Polymers 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 125000006729 (C2-C5) alkenyl group Chemical group 0.000 claims 2
- LLAPDLPYIYKTGQ-UHFFFAOYSA-N 1-aminoethyl Chemical group C[CH]N LLAPDLPYIYKTGQ-UHFFFAOYSA-N 0.000 claims 2
- 102000008645 11-beta-Hydroxysteroid Dehydrogenase Type 1 Human genes 0.000 claims 2
- 108010088011 11-beta-Hydroxysteroid Dehydrogenase Type 1 Proteins 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 2
- LFBLXBZNMMITTO-UHFFFAOYSA-N 4-(4-fluorophenyl)-4-(2-hydroxyethyl)-1-[1-(4-methoxyphenyl)ethyl]-1,3-diazinan-2-one Chemical compound C1=CC(OC)=CC=C1C(C)N1C(=O)NC(CCO)(C=2C=CC(F)=CC=2)CC1 LFBLXBZNMMITTO-UHFFFAOYSA-N 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 125000004633 N-oxo-pyridyl group Chemical group 0.000 claims 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000001207 fluorophenyl group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- LSLJKAPWUHORLT-GOSISDBHSA-N (4r)-4-methyl-1-(3-methylphenyl)-4-phenyl-1,3-diazinan-2-one Chemical compound CC1=CC=CC(N2C(N[C@](C)(CC2)C=2C=CC=CC=2)=O)=C1 LSLJKAPWUHORLT-GOSISDBHSA-N 0.000 claims 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- TYIWTXBFSKFPKX-UHFFFAOYSA-N 1-(1-cyclohexylethyl)-4-(3-hydroxypropyl)-4-phenyl-1,3-diazinan-2-one Chemical compound C1CC(CCCO)(C=2C=CC=CC=2)NC(=O)N1C(C)C1CCCCC1 TYIWTXBFSKFPKX-UHFFFAOYSA-N 0.000 claims 1
- RDXLZJXIVYZKNT-UHFFFAOYSA-N 1-(1-cyclohexylethyl)-4-(4-fluorophenyl)-4-(3-hydroxypropyl)-1,3-diazinan-2-one Chemical compound C1CC(CCCO)(C=2C=CC(F)=CC=2)NC(=O)N1C(C)C1CCCCC1 RDXLZJXIVYZKNT-UHFFFAOYSA-N 0.000 claims 1
- YUJAXGHCMAHYOR-CISYCMJJSA-N 1-[(1s)-1-(4-bromophenyl)ethyl]-4-(4-fluorophenyl)-4-(3-hydroxypropyl)-3-methyl-1,3-diazinan-2-one Chemical compound CN1C(=O)N([C@@H](C)C=2C=CC(Br)=CC=2)CCC1(CCCO)C1=CC=C(F)C=C1 YUJAXGHCMAHYOR-CISYCMJJSA-N 0.000 claims 1
- QLCKOLMCGHMETH-PVCZSOGJSA-N 1-[(1s)-1-(4-chlorophenyl)ethyl]-4-(4-fluorophenyl)-4-(2-hydroxyethyl)-1,3-diazinan-2-one Chemical compound N1C(=O)N([C@@H](C)C=2C=CC(Cl)=CC=2)CCC1(CCO)C1=CC=C(F)C=C1 QLCKOLMCGHMETH-PVCZSOGJSA-N 0.000 claims 1
- QCIZUNWRIKSICP-ZDGMYTEDSA-N 1-[(1s)-1-(4-chlorophenyl)ethyl]-4-(4-fluorophenyl)-4-(3-hydroxypropyl)-1,3-diazinan-2-one Chemical compound N1C(=O)N([C@@H](C)C=2C=CC(Cl)=CC=2)CCC1(CCCO)C1=CC=C(F)C=C1 QCIZUNWRIKSICP-ZDGMYTEDSA-N 0.000 claims 1
- CYOLONMWNWCSEK-WFFHQLTOSA-N 1-[(1s)-1-[4-(2,4-difluorophenyl)phenyl]ethyl]-4-(4-fluorophenyl)-4-(2-hydroxyethyl)-1,3-diazinan-2-one Chemical compound N1C(=O)N([C@@H](C)C=2C=CC(=CC=2)C=2C(=CC(F)=CC=2)F)CCC1(CCO)C1=CC=C(F)C=C1 CYOLONMWNWCSEK-WFFHQLTOSA-N 0.000 claims 1
- HHDVTFNGTOKZQI-HSYKDVHTSA-N 1-[(1s)-1-[4-(2,4-difluorophenyl)phenyl]ethyl]-4-(4-fluorophenyl)-4-(3-hydroxypropyl)-1,3-diazinan-2-one Chemical compound N1C(=O)N([C@@H](C)C=2C=CC(=CC=2)C=2C(=CC(F)=CC=2)F)CCC1(CCCO)C1=CC=C(F)C=C1 HHDVTFNGTOKZQI-HSYKDVHTSA-N 0.000 claims 1
- BWCWPIIVYWOSFR-SVQMELKDSA-N 1-[(1s)-1-[4-(4-fluorophenyl)phenyl]ethyl]-4-(3-hydroxypropyl)-4-phenyl-1,3-diazinan-2-one Chemical compound N1C(=O)N([C@@H](C)C=2C=CC(=CC=2)C=2C=CC(F)=CC=2)CCC1(CCCO)C1=CC=CC=C1 BWCWPIIVYWOSFR-SVQMELKDSA-N 0.000 claims 1
- TYIWTXBFSKFPKX-PBVYKCSPSA-N 1-[(1s)-1-cyclohexylethyl]-4-(3-hydroxypropyl)-4-phenyl-1,3-diazinan-2-one Chemical compound C1([C@H](C)N2C(NC(CCCO)(CC2)C=2C=CC=CC=2)=O)CCCCC1 TYIWTXBFSKFPKX-PBVYKCSPSA-N 0.000 claims 1
- YUJAXGHCMAHYOR-UHFFFAOYSA-N 1-[1-(4-bromophenyl)ethyl]-4-(4-fluorophenyl)-4-(3-hydroxypropyl)-3-methyl-1,3-diazinan-2-one Chemical compound C=1C=C(Br)C=CC=1C(C)N(C(N1C)=O)CCC1(CCCO)C1=CC=C(F)C=C1 YUJAXGHCMAHYOR-UHFFFAOYSA-N 0.000 claims 1
- LKKJPODTAZOLGK-UHFFFAOYSA-N 1-[1-(4-bromophenyl)propyl]-4-(2,3-dihydroxypropyl)-4-(4-fluorophenyl)-1,3-diazinan-2-one Chemical compound C=1C=C(Br)C=CC=1C(CC)N(C(N1)=O)CCC1(CC(O)CO)C1=CC=C(F)C=C1 LKKJPODTAZOLGK-UHFFFAOYSA-N 0.000 claims 1
- ODBJJXYRVIJKMP-UHFFFAOYSA-N 1-[1-(4-chlorophenyl)ethyl]-4-(2,3-dihydroxypropyl)-4-propan-2-yl-1,3-diazinan-2-one Chemical compound O=C1NC(C(C)C)(CC(O)CO)CCN1C(C)C1=CC=C(Cl)C=C1 ODBJJXYRVIJKMP-UHFFFAOYSA-N 0.000 claims 1
- QLCKOLMCGHMETH-UHFFFAOYSA-N 1-[1-(4-chlorophenyl)ethyl]-4-(4-fluorophenyl)-4-(2-hydroxyethyl)-1,3-diazinan-2-one Chemical compound C=1C=C(Cl)C=CC=1C(C)N(C(N1)=O)CCC1(CCO)C1=CC=C(F)C=C1 QLCKOLMCGHMETH-UHFFFAOYSA-N 0.000 claims 1
- QCIZUNWRIKSICP-UHFFFAOYSA-N 1-[1-(4-chlorophenyl)ethyl]-4-(4-fluorophenyl)-4-(3-hydroxypropyl)-1,3-diazinan-2-one Chemical compound C=1C=C(Cl)C=CC=1C(C)N(C(N1)=O)CCC1(CCCO)C1=CC=C(F)C=C1 QCIZUNWRIKSICP-UHFFFAOYSA-N 0.000 claims 1
- MMRCQVRXFLWAQD-UHFFFAOYSA-N 1-[1-[4-(2,4-difluorophenyl)phenyl]ethyl]-4-(2,3-dihydroxypropyl)-4-(4-fluorophenyl)-1,3-diazinan-2-one Chemical compound C=1C=C(C=2C(=CC(F)=CC=2)F)C=CC=1C(C)N(C(N1)=O)CCC1(CC(O)CO)C1=CC=C(F)C=C1 MMRCQVRXFLWAQD-UHFFFAOYSA-N 0.000 claims 1
- QFPLXKGFPMGUQX-UHFFFAOYSA-N 1-[1-[4-(2,4-difluorophenyl)phenyl]ethyl]-4-(2-hydroxyethyl)-3-methyl-4-thiophen-2-yl-1,3-diazinan-2-one Chemical compound C=1C=C(C=2C(=CC(F)=CC=2)F)C=CC=1C(C)N(C(N1C)=O)CCC1(CCO)C1=CC=CS1 QFPLXKGFPMGUQX-UHFFFAOYSA-N 0.000 claims 1
- GVVPZIDFSHJBIT-UHFFFAOYSA-N 1-[1-[4-(2,4-difluorophenyl)phenyl]ethyl]-4-(2-imidazol-1-ylethyl)-3-methyl-4-phenyl-1,3-diazinan-2-one Chemical compound C=1C=C(C=2C(=CC(F)=CC=2)F)C=CC=1C(C)N(C(N1C)=O)CCC1(C=1C=CC=CC=1)CCN1C=CN=C1 GVVPZIDFSHJBIT-UHFFFAOYSA-N 0.000 claims 1
- FTNIXEZTAPNMLO-UHFFFAOYSA-N 1-[1-[4-(2,4-difluorophenyl)phenyl]ethyl]-4-(4-fluorophenyl)-3-methyl-4-(2-oxopropyl)-1,3-diazinan-2-one Chemical compound C=1C=C(C=2C(=CC(F)=CC=2)F)C=CC=1C(C)N(C(N1C)=O)CCC1(CC(C)=O)C1=CC=C(F)C=C1 FTNIXEZTAPNMLO-UHFFFAOYSA-N 0.000 claims 1
- CYOLONMWNWCSEK-UHFFFAOYSA-N 1-[1-[4-(2,4-difluorophenyl)phenyl]ethyl]-4-(4-fluorophenyl)-4-(2-hydroxyethyl)-1,3-diazinan-2-one Chemical compound C=1C=C(C=2C(=CC(F)=CC=2)F)C=CC=1C(C)N(C(N1)=O)CCC1(CCO)C1=CC=C(F)C=C1 CYOLONMWNWCSEK-UHFFFAOYSA-N 0.000 claims 1
- GSKOVRJNWUFTJV-UHFFFAOYSA-N 1-[1-[4-(2,4-difluorophenyl)phenyl]ethyl]-4-(4-fluorophenyl)-4-(2-methoxyethyl)-3-methyl-1,3-diazinan-2-one Chemical compound O=C1N(C)C(CCOC)(C=2C=CC(F)=CC=2)CCN1C(C)C(C=C1)=CC=C1C1=CC=C(F)C=C1F GSKOVRJNWUFTJV-UHFFFAOYSA-N 0.000 claims 1
- HHDVTFNGTOKZQI-UHFFFAOYSA-N 1-[1-[4-(2,4-difluorophenyl)phenyl]ethyl]-4-(4-fluorophenyl)-4-(3-hydroxypropyl)-1,3-diazinan-2-one Chemical compound C=1C=C(C=2C(=CC(F)=CC=2)F)C=CC=1C(C)N(C(N1)=O)CCC1(CCCO)C1=CC=C(F)C=C1 HHDVTFNGTOKZQI-UHFFFAOYSA-N 0.000 claims 1
- GCFDODCZAKJQIW-UHFFFAOYSA-N 1-[1-[4-(2,4-difluorophenyl)phenyl]ethyl]-4-(4-fluorophenyl)-4-[2-(2-hydroxyethoxy)ethyl]-1,3-diazinan-2-one Chemical compound C=1C=C(C=2C(=CC(F)=CC=2)F)C=CC=1C(C)N(C(N1)=O)CCC1(CCOCCO)C1=CC=C(F)C=C1 GCFDODCZAKJQIW-UHFFFAOYSA-N 0.000 claims 1
- NLXOALDTOUPKJF-UHFFFAOYSA-N 1-[1-[4-(2,4-difluorophenyl)phenyl]propyl]-4-(4-fluorophenyl)-4-(3-hydroxypropyl)-1,3-diazinan-2-one Chemical compound C=1C=C(C=2C(=CC(F)=CC=2)F)C=CC=1C(CC)N(C(N1)=O)CCC1(CCCO)C1=CC=C(F)C=C1 NLXOALDTOUPKJF-UHFFFAOYSA-N 0.000 claims 1
- KINXYMGDZAXCNS-UHFFFAOYSA-N 1-[1-[4-(4-fluorophenyl)phenyl]ethyl]-4-(2-hydroxy-2-methylpropyl)-3-methyl-4-phenyl-1,3-diazinan-2-one Chemical compound C=1C=C(C=2C=CC(F)=CC=2)C=CC=1C(C)N(C(N1C)=O)CCC1(CC(C)(C)O)C1=CC=CC=C1 KINXYMGDZAXCNS-UHFFFAOYSA-N 0.000 claims 1
- ORNYUPKZZZGSIZ-UHFFFAOYSA-N 1-[1-[4-(4-fluorophenyl)phenyl]ethyl]-4-(2-morpholin-4-ylethyl)-4-phenyl-1,3-diazinan-2-one Chemical compound C=1C=C(C=2C=CC(F)=CC=2)C=CC=1C(C)N(C(N1)=O)CCC1(C=1C=CC=CC=1)CCN1CCOCC1 ORNYUPKZZZGSIZ-UHFFFAOYSA-N 0.000 claims 1
- MEWFCLYBYFTDRT-UHFFFAOYSA-N 1-[1-[4-(4-fluorophenyl)phenyl]ethyl]-4-(2-morpholin-4-ylethyl)-4-propan-2-yl-1,3-diazinan-2-one Chemical compound C1CN(C(C)C=2C=CC(=CC=2)C=2C=CC(F)=CC=2)C(=O)NC1(C(C)C)CCN1CCOCC1 MEWFCLYBYFTDRT-UHFFFAOYSA-N 0.000 claims 1
- BWCWPIIVYWOSFR-UHFFFAOYSA-N 1-[1-[4-(4-fluorophenyl)phenyl]ethyl]-4-(3-hydroxypropyl)-4-phenyl-1,3-diazinan-2-one Chemical compound C=1C=C(C=2C=CC(F)=CC=2)C=CC=1C(C)N(C(N1)=O)CCC1(CCCO)C1=CC=CC=C1 BWCWPIIVYWOSFR-UHFFFAOYSA-N 0.000 claims 1
- UJFUDMYXFATZFN-UHFFFAOYSA-N 1-[1-[4-(5-acetylthiophen-2-yl)phenyl]ethyl]-4-(3-fluorophenyl)-4-(3-hydroxypropyl)-1,3-diazinan-2-one Chemical compound C=1C=C(C=2SC(=CC=2)C(C)=O)C=CC=1C(C)N(C(N1)=O)CCC1(CCCO)C1=CC=CC(F)=C1 UJFUDMYXFATZFN-UHFFFAOYSA-N 0.000 claims 1
- DQRDUHUGLWQETK-UHFFFAOYSA-N 1-[1-[4-[5-(aminomethyl)-1,3-thiazol-2-yl]phenyl]ethyl]-4-(3-hydroxypropyl)-4-phenyl-1,3-diazinan-2-one Chemical compound C=1C=C(C=2SC(CN)=CN=2)C=CC=1C(C)N(C(N1)=O)CCC1(CCCO)C1=CC=CC=C1 DQRDUHUGLWQETK-UHFFFAOYSA-N 0.000 claims 1
- JQPBCMQLIHNBEO-UHFFFAOYSA-N 1-[3-(2,4-difluorophenyl)-4-fluorophenyl]-4-(2-fluorophenyl)-4-(2-hydroxyethyl)-1,3-diazinan-2-one Chemical compound O=C1NC(CCO)(C=2C(=CC=CC=2)F)CCN1C(C=1)=CC=C(F)C=1C1=CC=C(F)C=C1F JQPBCMQLIHNBEO-UHFFFAOYSA-N 0.000 claims 1
- DYXTVXTUGZTIIN-UHFFFAOYSA-N 1-[3-(2,6-dichlorophenyl)phenyl]-4-(2-hydroxyethyl)-3-methyl-4-phenyl-1,3-diazinan-2-one Chemical compound CN1C(=O)N(C=2C=C(C=CC=2)C=2C(=CC=CC=2Cl)Cl)CCC1(CCO)C1=CC=CC=C1 DYXTVXTUGZTIIN-UHFFFAOYSA-N 0.000 claims 1
- AWPJZMAWAQBUKY-UHFFFAOYSA-N 1-[6-(2,4-difluorophenyl)pyridin-2-yl]-4-(2-fluorophenyl)-4-(2-hydroxyethyl)-1,3-diazinan-2-one Chemical compound O=C1NC(CCO)(C=2C(=CC=CC=2)F)CCN1C(N=1)=CC=CC=1C1=CC=C(F)C=C1F AWPJZMAWAQBUKY-UHFFFAOYSA-N 0.000 claims 1
- VLIDQEOMDIITOM-UHFFFAOYSA-N 2-[1-[1-[4-(2,4-difluorophenyl)phenyl]ethyl]-2-oxo-4-phenyl-1,3-diazinan-4-yl]acetonitrile Chemical compound C=1C=C(C=2C(=CC(F)=CC=2)F)C=CC=1C(C)N(C(N1)=O)CCC1(CC#N)C1=CC=CC=C1 VLIDQEOMDIITOM-UHFFFAOYSA-N 0.000 claims 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000000389 2-pyrrolyl group Chemical group [H]N1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
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| ATE554078T1 (de) * | 2007-07-26 | 2012-05-15 | Vitae Pharmaceuticals Inc | Synthese von 11-beta-hydroxysteroid-dehydrogenase-1-hemmern |
| AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| WO2009063061A2 (en) | 2007-11-16 | 2009-05-22 | Boehringer Ingelheim International Gmbh | Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use |
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| TW200934490A (en) * | 2008-01-07 | 2009-08-16 | Vitae Pharmaceuticals Inc | Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1 |
| JP5490020B2 (ja) | 2008-01-24 | 2014-05-14 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状カルバゼート及びセミカルバジドインヒビター |
| JP5734666B2 (ja) * | 2008-02-11 | 2015-06-17 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の１，３−オキサアゼパン−２−オン及び１，３−ジアゼパン−２−オン阻害剤 |
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| US8592410B2 (en) | 2008-05-01 | 2013-11-26 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11BETA-hydroxysteroid dehydrogenase 1 |
| CL2009001058A1 (es) | 2008-05-01 | 2010-09-10 | Vitae Pharmaceuticals Inc | Compuestos derivados de oxazinas sustituidas, inhibidores de la 11b-hidroxiesteroide deshidrogenasa de tipo-1; composicion farmaceutica; y uso del compuesto para inhibir la actividad de 11b-hsd1, como en el tratamiento de la diabetes, dislipidemia, hipertension, obesidad, cancer, glaucoma, entre otras. |
| CA2723032A1 (en) * | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| AU2009241727B2 (en) | 2008-05-01 | 2013-05-02 | Vitae Pharmaceuticals, Inc | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| US8765780B2 (en) | 2008-05-13 | 2014-07-01 | Boehringer Ingelheim International Gmbh | Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use |
| JP5379160B2 (ja) | 2008-07-25 | 2013-12-25 | 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 | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター |
| CA2729998A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CA2729993A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
| WO2010046445A2 (en) | 2008-10-23 | 2010-04-29 | Boehringer Ingelheim International Gmbh | Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| CA2744946A1 (en) | 2009-02-04 | 2010-08-12 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| MA33216B1 (fr) | 2009-04-30 | 2012-04-02 | Boehringer Ingelheim Int | Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1 |
| WO2010139673A1 (en) * | 2009-06-02 | 2010-12-09 | Boehringer Ingelheim International Gmbh | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| EP2440537A1 (en) | 2009-06-11 | 2012-04-18 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure |
| JP5749263B2 (ja) * | 2009-07-01 | 2015-07-15 | ヴァイティー ファーマシューティカルズ，インコーポレイテッド | １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター |
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| JP2013531636A (ja) | 2010-05-26 | 2013-08-08 | 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 | ２−オキソ−１，２−ジヒドロピリジン−４−イルボロン酸誘導体 |
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| JP5813106B2 (ja) | 2010-06-25 | 2015-11-17 | 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 | 代謝障害の処置のための１１−β−ＨＳＤ１のインヒビターとしてのアザスピロヘキサノン |
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2008
- 2008-11-06 AR ARP080104852A patent/AR069207A1/es unknown
- 2008-11-07 US US12/745,663 patent/US9079861B2/en not_active Expired - Fee Related
- 2008-11-07 EP EP08846298.1A patent/EP2220052B1/en not_active Not-in-force
- 2008-11-07 CL CL2008003339A patent/CL2008003339A1/es unknown
- 2008-11-07 WO PCT/US2008/012618 patent/WO2009061498A1/en not_active Ceased
- 2008-11-07 JP JP2010533113A patent/JP5695906B2/ja not_active Expired - Fee Related
- 2008-11-07 TW TW097143034A patent/TW200934495A/zh unknown
- 2008-11-07 CA CA2704222A patent/CA2704222A1/en not_active Abandoned