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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| CA2678577A1 (en) | 2007-02-26 | 2008-09-04 | Vitae Pharmaceuticals, Inc. | Cyclic urea and carbamate inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| US8575156B2 (en) * | 2007-07-26 | 2013-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 |
| AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| CL2008003407A1 (es) | 2007-11-16 | 2010-01-11 | Boehringer Ingelheim Int | Compuestos derivados de aril- y heteroarilcarbonilo de heterobiciclo sustituido; composicion farmaceutica; procedimiento de preparacion; y su uso en el tratamiento y/o prevencion de trastornos metabolicos, mediado por la inhibicion de la enzima hsd-1. |
| WO2009075835A1 (en) | 2007-12-11 | 2009-06-18 | Vitae Pharmaceutical, Inc | CYCLIC UREA INHIBITORS OF 11β-HYDROXYSTEROID DEHYDROGENASE 1 |
| 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 |
| EP2252598A2 (en) * | 2008-02-11 | 2010-11-24 | Vitae Pharmaceuticals, Inc. | 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| US8598160B2 (en) * | 2008-02-15 | 2013-12-03 | Vitae Pharmaceuticals, Inc. | Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| TW201004945A (en) | 2008-05-01 | 2010-02-01 | Vitae Pharmaceuticals Inc | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| NZ588954A (en) | 2008-05-01 | 2012-08-31 | Vitae Pharmaceuticals Inc | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| EP2291373B1 (en) * | 2008-05-01 | 2013-09-11 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
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| TW200950780A (en) | 2008-05-13 | 2009-12-16 | Boehringer Ingelheim Int | Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use |
| CA2729993A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
| TW201016691A (en) | 2008-07-25 | 2010-05-01 | Boehringer Ingelheim Int | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CN104327062A (zh) | 2008-07-25 | 2015-02-04 | 贝林格尔·英格海姆国际有限公司 | 11β-羟基类固醇脱氢酶1的环状抑制剂 |
| TW201022266A (en) | 2008-10-23 | 2010-06-16 | Boehringer Ingelheim Int | Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| EP2393807B1 (en) | 2009-02-04 | 2013-08-14 | Boehringer Ingelheim International GmbH | Cyclic inhibitors of 11 -hydroxysteroid dehydrogenase 1 |
| MA33216B1 (fr) | 2009-04-30 | 2012-04-02 | Boehringer Ingelheim Int | Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1 |
| EP2438049B1 (en) * | 2009-06-02 | 2014-05-14 | Boehringer Ingelheim International GmbH | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| WO2011011123A1 (en) | 2009-06-11 | 2011-01-27 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure |
| EP2448928B1 (en) * | 2009-07-01 | 2014-08-13 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| EP2496589B1 (en) | 2009-11-05 | 2014-03-05 | Boehringer Ingelheim International GmbH | Novel chiral phosphorus ligands |
| TWI531571B (zh) | 2009-11-06 | 2016-05-01 | 維它藥物公司 | 六氫茚并吡啶及八氫苯并喹啉之芳基－及雜芳基羰基衍生物 |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| WO2011149822A1 (en) | 2010-05-26 | 2011-12-01 | Boehringer Ingelheim International Gmbh | 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives |
| JP5860042B2 (ja) | 2010-06-16 | 2016-02-16 | 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 | 置換５、６及び７員複素環、そのような化合物を含有する医薬及びそれらの使用 |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| EP2585444B1 (en) | 2010-06-25 | 2014-10-22 | Boehringer Ingelheim International GmbH | Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| EA201300522A1 (ru) | 2010-11-02 | 2013-11-29 | Бёрингер Ингельхайм Интернациональ Гмбх | Фармацевтические комбинации для лечения метаболических нарушений |
| TWI537258B (zh) | 2010-11-05 | 2016-06-11 | 百靈佳殷格翰國際股份有限公司 | 六氫茚并吡啶及八氫苯并喹啉之芳基－及雜環芳基羰基衍生物 |
| JP2014524438A (ja) | 2011-08-17 | 2014-09-22 | 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 | インデノピリジン誘導体 |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| EP3235813A1 (en) | 2016-04-19 | 2017-10-25 | Cidqo 2012, S.L. | Aza-tetra-cyclo derivatives |
Family Cites Families (188)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3378587A (en) | 1963-03-14 | 1968-04-16 | Du Pont | 3, 3'-diaminomethyl-1, 1'-biadamantane |
| NL127995C (enExample) | 1963-12-20 | Geigy Ag J R | ||
| US3341538A (en) | 1965-06-18 | 1967-09-12 | Geigy Chem Corp | Certain 2, 6-methano-3-benzazocines |
| GB1304175A (enExample) | 1969-03-31 | 1973-01-24 | ||
| US3681349A (en) | 1970-03-05 | 1972-08-01 | Morton Norwich Products Inc | 1-(substituted benzyl) tetrahydro-2-(1h) pyrimidones |
| US4043927A (en) | 1972-03-07 | 1977-08-23 | Sun Ventures, Inc. | Friction or tractive drive containing ethers of adamantanes |
| DE2338369A1 (de) | 1973-07-26 | 1975-02-13 | Schering Ag | Mikrobiologische hydroxylierung von 2,6-methano-3-benzazocinen |
| US4009171A (en) | 1974-02-21 | 1977-02-22 | Sterling Drug Inc. | N-acylated-11-oxygenated-2,6-methano-3-benzazocine intermediates |
| US4136162A (en) | 1974-07-05 | 1979-01-23 | Schering Aktiengesellschaft | Medicament carriers in the form of film having active substance incorporated therein |
| US4136145A (en) | 1974-07-05 | 1979-01-23 | Schering Aktiengesellschaft | Medicament carriers in the form of film having active substance incorporated therein |
| GB1513961A (en) | 1975-02-25 | 1978-06-14 | Acf Chemiefarma Nv | 6,7-benzomorphans method for their preparation and intermediates |
| US4108857A (en) | 1975-08-18 | 1978-08-22 | Sterling Drug Inc. | Imidazolylmethyl methanobenzazocines |
| US5393735A (en) | 1990-08-09 | 1995-02-28 | Rohm And Haas Company | Herbicidal glutarimides |
| CA2023492A1 (en) | 1989-08-31 | 1991-03-01 | Barry Clifford Lange | Herbicidal glutarimides |
| US5098916A (en) | 1990-03-29 | 1992-03-24 | G. D. Searle & Co. | Propanobicyclic amine derivatives for cns disorders |
| EP0454444A1 (en) | 1990-04-24 | 1991-10-30 | Nissan Chemical Industries Ltd. | Glutarimide derivatives and herbicides |
| US5089506A (en) | 1990-04-30 | 1992-02-18 | G. D. Searle & Co. | Ethanobicyclic amine derivatives for cns disorders |
| US5215992A (en) | 1990-04-30 | 1993-06-01 | G. D. Searle & Co. | Ethanobicyclic amine derivatives for CNS disorders |
| DK204291D0 (da) | 1991-12-20 | 1991-12-20 | Novo Nordisk As | Heterocykliske forbindelser deres fremstilling og anvendelse |
| CA2049244A1 (en) | 1990-08-16 | 1992-02-17 | Steven H. Christiansen | Process for absorption of sulfur compounds from fluids using heterocyclic compounds having at least one ring nitrogen atom |
| HUT66081A (en) | 1990-10-10 | 1994-09-28 | Schering Corp | Process for preparing pyridine and pyridine n-oxide derivatives of diaryl methyl piperidines or piperazines and pharmaceutical compositions containing them |
| GB9023583D0 (en) | 1990-10-30 | 1990-12-12 | Beecham Group Plc | Novel compounds |
| US5610294A (en) | 1991-10-11 | 1997-03-11 | The Du Pont Merck Pharmaceutical Company | Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors |
| HU221816B1 (hu) | 1991-10-11 | 2003-01-28 | Bristol-Myers Squibb Pharma Company | Gyűrűs karbonil vegyületek, és ezeket tartalmazó gyógyászati készítmények |
| ATE194981T1 (de) | 1992-04-30 | 2000-08-15 | Taiho Pharmaceutical Co Ltd | Oxazolidinderivat und sein pharmazeutisch verträgliches salz |
| GB9225377D0 (en) | 1992-12-04 | 1993-01-27 | Ici Plc | Herbicides |
| TW280812B (enExample) | 1993-07-02 | 1996-07-11 | Bayer Ag | |
| EP0640594A1 (en) | 1993-08-23 | 1995-03-01 | Fujirebio Inc. | Hydantoin derivative as metalloprotease inhibitor |
| DE19500118A1 (de) | 1994-05-18 | 1995-11-23 | Bayer Ag | Substituierte Diazacyclohexandi(thi)one |
| FR2729954B1 (fr) | 1995-01-30 | 1997-08-01 | Sanofi Sa | Composes heterocycliques substitues, procede pour leur preparation et compositions pharmaceutiques les contenant |
| US5780466A (en) | 1995-01-30 | 1998-07-14 | Sanofi | Substituted heterocyclic compounds method of preparing them and pharmaceutical compositions in which they are present |
| GB9510459D0 (en) | 1995-05-24 | 1995-07-19 | Zeneca Ltd | Bicyclic amines |
| US5776959A (en) | 1995-06-05 | 1998-07-07 | Washington University | Anticonvulsant and anxiolytic lactam and thiolactam derivatives |
| GB9517622D0 (en) | 1995-08-29 | 1995-11-01 | Univ Edinburgh | Regulation of intracellular glucocorticoid concentrations |
| AU717190B2 (en) | 1996-04-03 | 2000-03-23 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| CA2262502C (en) | 1996-07-31 | 2002-11-26 | Nikken Chemicals Co., Ltd. | 6-phenyltetrahydro-1,3-oxazin-2-one derivatives and pharmaceutical composition containing the same |
| US5866702A (en) | 1996-08-02 | 1999-02-02 | Cv Therapeutics, Incorporation | Purine inhibitors of cyclin dependent kinase 2 |
| US6794390B2 (en) | 1996-08-02 | 2004-09-21 | Cv Therapeutics, Inc. | Purine inhibitors of cyclin dependent kinase 2 & ikappabalpha |
| GB9623944D0 (en) | 1996-11-15 | 1997-01-08 | Zeneca Ltd | Bicyclic amine derivatives |
| WO1998057940A1 (en) | 1997-06-18 | 1998-12-23 | Synaptic Pharmaceutical Corporation | Heterocyclic substituted piperidines and uses thereof |
| US6159990A (en) | 1997-06-18 | 2000-12-12 | Synaptic Pharmaceutical Corporation | Oxazolidinones as α1A receptor antagonists |
| GB9715892D0 (en) | 1997-07-29 | 1997-10-01 | Zeneca Ltd | Heterocyclic compounds |
| US5936124A (en) | 1998-06-22 | 1999-08-10 | Sepacor Inc. | Fluoxetine process from benzoylpropionic acid |
| US7410995B1 (en) | 1998-08-14 | 2008-08-12 | Gpi Nil Holdings Inc. | N-linked sulfonamide of heterocyclic thioesters for vision and memory disorders |
| US7256005B2 (en) | 1999-08-10 | 2007-08-14 | The Chancellor, Masters And Scholars Of The University Of Oxford | Methods for identifying iminosugar derivatives that inhibit HCV p7 ion channel activity |
| EP1206262A4 (en) | 1999-08-26 | 2003-01-02 | Bristol Myers Squibb Co | Y NEUROPEPTID ANTAGONISTS: SPIROISOQUINOLINONE DERIVATIVES |
| HK1045308A1 (zh) | 1999-12-17 | 2002-11-22 | Schering Corporation | 选择性神经激肽拮抗物 |
| US6436928B1 (en) | 1999-12-17 | 2002-08-20 | Schering Corporation | Selective neurokinin antagonists |
| WO2001055063A1 (en) | 2000-01-25 | 2001-08-02 | Idemitsu Petrochemical Co., Ltd. | Novel bisadamantane compounds, process for preparing the same, and novel biadamantane derivatives |
| GB0003397D0 (en) | 2000-02-14 | 2000-04-05 | Merck Sharp & Dohme | Therapeutic agents |
| DE10035908A1 (de) | 2000-07-21 | 2002-03-07 | Asta Medica Ag | Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel |
| DE10035928A1 (de) | 2000-07-21 | 2002-03-07 | Asta Medica Ag | Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel |
| DE10035927A1 (de) | 2000-07-21 | 2002-03-07 | Asta Medica Ag | Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel |
| ATE307127T1 (de) | 2000-08-16 | 2005-11-15 | Neurogen Corp | 2,4-substituierte pyridinderivate |
| AU9087301A (en) | 2000-09-11 | 2002-03-26 | Sepracor Inc | Ligands for monoamine receptors and transporters, and methods of use thereof |
| US7294637B2 (en) | 2000-09-11 | 2007-11-13 | Sepracor, Inc. | Method of treating addiction or dependence using a ligand for a monamine receptor or transporter |
| US6841671B2 (en) | 2000-10-26 | 2005-01-11 | Pfizer Inc. | Spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors |
| US20030143668A1 (en) | 2001-06-18 | 2003-07-31 | National Institute Of Advanced Industrial | Guanosine triphosphate-binding protein coupled receptors |
| HUP0401777A3 (en) | 2001-10-15 | 2008-06-30 | Schering Corp | 3h-[1,2,4]triazolo[5,1-i]purin-5-yl amines as adenosine a2a receptor antagonists and pharmaceutical compositions containing the compounds |
| DE60302150D1 (en) | 2002-04-26 | 2005-12-08 | Pfizer Prod Inc | N-substituiete heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trion metalloproteinase inhibitoren |
| ES2247527T3 (es) | 2002-04-26 | 2006-03-01 | Pfizer Prod Inc | Inhibidores de metaloproteinasa de triaril-oxi-aril-espiro-pirimidina-2,4,6-triona. |
| AU2003229953A1 (en) | 2002-04-30 | 2003-11-17 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| JP5438250B2 (ja) | 2002-05-17 | 2014-03-12 | ジェンケン バイオサイエンスィズ，インコーポレイテッド | オピオイド及びオピオイド様の化合物並びにそれらの使用 |
| ATE358482T1 (de) | 2002-07-03 | 2007-04-15 | Schering Corp | 1-amido-4-phenyl-4-benzyloxymethyl-piperidin derivative und verwandte verbindungen als neurokinin-1 (nk-1) antagonsisten zur behandlung von erbrechen, depressionen, angstzustände und husten |
| AU2003249812A1 (en) | 2002-07-18 | 2004-02-09 | Queen's University At Kingston | Dihydrouracil compounds as anti-ictogenic or anti-epileptogenic agents |
| GB0218630D0 (en) | 2002-08-10 | 2002-09-18 | Tanabe Seiyaku Co | Novel compounds |
| AR041198A1 (es) | 2002-10-11 | 2005-05-04 | Otsuka Pharma Co Ltd | Compuesto 2,3-dihidro-6-nitroimidazo[2,1-b] oxaxol, y composiciones farmaceuticas que lo contienen |
| WO2004046137A1 (en) | 2002-11-21 | 2004-06-03 | Vicore Pharma Ab | New tricyclic angiotensin ii agonists |
| GB0228410D0 (en) | 2002-12-05 | 2003-01-08 | Glaxo Group Ltd | Novel Compounds |
| EP1581520A4 (en) | 2002-12-13 | 2006-08-23 | Smithkline Beecham Corp | COMPOUNDS, COMPOSITIONS AND METHODS |
| WO2004056744A1 (en) | 2002-12-23 | 2004-07-08 | Janssen Pharmaceutica N.V. | Adamantyl acetamides as hydroxysteroid dehydrogenase inhibitors |
| CN1764458A (zh) | 2003-03-26 | 2006-04-26 | 麦克公司 | 作为黑皮质素－4受体激动剂的双环哌啶衍生物 |
| US7700583B2 (en) | 2003-04-11 | 2010-04-20 | High Point Pharmaceuticals, Llc | 11β-hydroxysteroid dehydrogenase type 1 active compounds |
| EP1618090A1 (en) | 2003-04-11 | 2006-01-25 | Novo Nordisk A/S | 11ß-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ACTIVE COMPOUNDS |
| ITMI20031292A1 (it) | 2003-06-25 | 2004-12-26 | Nikem Research Srl | Derivati biciclici nk-2 antagonisti selettivi. |
| DE10358004A1 (de) | 2003-12-11 | 2005-07-14 | Abbott Gmbh & Co. Kg | Ketolactam-Verbindungen und ihre Verwendung |
| US7186844B2 (en) | 2004-01-13 | 2007-03-06 | Mitsubishi Gas Chemical Co., Inc. | Method for producing cyclic carbamate ester |
| CN101014574A (zh) | 2004-03-09 | 2007-08-08 | 默克公司 | Hiv整合酶抑制剂 |
| WO2005090282A1 (en) | 2004-03-12 | 2005-09-29 | Ligand Pharmaceuticals Incorporated | Androgen receptor modulator compounds and methods |
| WO2005108360A1 (en) | 2004-05-07 | 2005-11-17 | Janssen Pharmaceutica N.V. | Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors |
| PL1747198T3 (pl) | 2004-05-07 | 2008-11-28 | Janssen Pharmaceutica Nv | Pochodne adamantylopirolidyn-2-onu jako inhibitory 11ß-dehydrogenazy hydroksysteroidowej |
| GB0411404D0 (en) | 2004-05-21 | 2004-06-23 | Glaxo Group Ltd | Novel compounds |
| MY148480A (en) | 2004-05-24 | 2013-04-30 | Amgen Inc | Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1 |
| JP2008504278A (ja) | 2004-06-24 | 2008-02-14 | インサイト・コーポレイション | アミド化合物およびその医薬としての使用 |
| GB0414438D0 (en) | 2004-06-28 | 2004-07-28 | Syngenta Participations Ag | Chemical compounds |
| DOP2005000123A (es) | 2004-07-02 | 2011-07-15 | Merck Sharp & Dohme | Inhibidores de cetp |
| EP1621539A1 (en) | 2004-07-27 | 2006-02-01 | Aventis Pharma S.A. | Heterocycle -substituted cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors |
| EP1621536A1 (en) | 2004-07-27 | 2006-02-01 | Aventis Pharma S.A. | Amino cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors |
| EP1621535A1 (en) | 2004-07-27 | 2006-02-01 | Aventis Pharma S.A. | Substituted cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors |
| EP1797054A2 (en) | 2004-08-02 | 2007-06-20 | OSI Pharmaceuticals, Inc. | Aryl-amino substituted pyrrolopyrimidine multi-kinase inhibiting compounds |
| EP1784175A4 (en) | 2004-08-23 | 2009-07-22 | Merck & Co Inc | INHIBITORS OF ACT ACTIVITY |
| JP5208505B2 (ja) | 2004-08-30 | 2013-06-12 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | １１−ベータヒドロキシステロイドデヒドロゲナーゼ阻害剤としてのｎ−２アダマンタニル−２−フェノキシ−アセトアミド誘導体 |
| WO2006031715A2 (en) | 2004-09-10 | 2006-03-23 | Janssen Pharmaceutica N.V. | Novel imidazolidin-2-one derivatives as selective androgen receptor modulators (sarms) |
| EP1802623A1 (en) | 2004-10-12 | 2007-07-04 | Novo Nordisk A/S | 11beta-hydroxysteroid dehydrogenase type 1 active spiro compounds |
| EP1809626A2 (en) | 2004-10-13 | 2007-07-25 | Neurogen Corporation | Aryl substituted 8-azabicyclo[3.2.1]octane compounds as ligands of the melanin concentrating hormone receptor |
| AU2005304560C1 (en) | 2004-11-10 | 2013-05-09 | Incyte Holdings Corporation | Lactam compounds and their use as pharmaceuticals |
| GT200500375A (es) | 2004-12-20 | 2006-11-28 | Derivados de piperidina y su uso como agentes antiinflamatorios | |
| JP2008525357A (ja) * | 2004-12-23 | 2008-07-17 | キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ | 抗ムスカリン活性を有するアゾール誘導体 |
| JP5274842B2 (ja) | 2004-12-28 | 2013-08-28 | エグゼリクシス， インコーポレイテッド | 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター（ｐ７０Ｓ６Ｋ、Ａｋｔ−１およびＡｋｔ−２）としての［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジンまたは［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジン化合物 |
| EP1838703A2 (en) | 2005-01-19 | 2007-10-03 | Neurogen Corporation | Heteroaryl substituted piperazinyl-pyridine analogues |
| CA2598457A1 (en) | 2005-02-16 | 2006-08-24 | Schering Corporation | Pyridyl and phenyl substituted piperazine-piperidines with cxcr3 antagonist activity |
| US7763616B2 (en) | 2005-02-16 | 2010-07-27 | Schering Corporation | Piperazine-piperidines with CXCR3 antagonist activity |
| MX2007010067A (es) | 2005-02-16 | 2007-12-07 | Schering Corp | Compuestos heterociclicos novedosos sustituidos con piridina o fenilo con actividad antagonista de cxcr3. |
| PE20061164A1 (es) | 2005-02-16 | 2006-10-27 | Schering Corp | Piperazin-piperidinas sustituidas con pirazinilo con actividad antagonista de cxcr3 |
| WO2006088837A2 (en) | 2005-02-16 | 2006-08-24 | Schering Corporation | Heterocyclic substituted piperazines with cxcr3 antagonist activity |
| ATE523506T1 (de) | 2005-02-16 | 2011-09-15 | Schering Corp | Amingebundene pyridyl- und phenylsubstituierte piperazin-piperidine mit cxcr3-antagonistischer aktivität |
| JPWO2006104280A1 (ja) * | 2005-03-31 | 2008-09-11 | 武田薬品工業株式会社 | 糖尿病の予防・治療剤 |
| CA2604038C (en) | 2005-04-12 | 2013-11-12 | Vicore Pharma Ab | New tricyclic angiotensin ii agonists |
| WO2007008529A2 (en) | 2005-07-08 | 2007-01-18 | Kalypsys, Inc | Celullar cholesterol absorption modifiers |
| BRPI0614801A2 (pt) | 2005-08-16 | 2009-05-19 | Genzyme Corp | compostos de ligação a receptor de quimiocina |
| JP2009511582A (ja) | 2005-10-11 | 2009-03-19 | シェーリング コーポレイション | Ｃｘｃｒ３拮抗薬活性を有する置換複素環式化合物 |
| US7943605B2 (en) | 2005-10-27 | 2011-05-17 | Ucb Pharma S.A. | Compounds comprising a lactam or a lactam derivative moiety, processes for making them, and their uses |
| US20090124598A1 (en) | 2005-11-01 | 2009-05-14 | Henrik Sune Andersen | Pharmaceutical use of substituted amides |
| MX2008006530A (es) | 2005-11-22 | 2008-09-25 | Amgen Inc | Inhibidores de 11-beta-hidroxiesteroide deshidrogenasa tipo 1. |
| TW200804382A (en) | 2005-12-05 | 2008-01-16 | Incyte Corp | Lactam compounds and methods of using the same |
| EP1801098A1 (en) | 2005-12-16 | 2007-06-27 | Merck Sante | 2-Adamantylurea derivatives as selective 11B-HSD1 inhibitors |
| WO2007076055A2 (en) | 2005-12-22 | 2007-07-05 | Entremed, Inc. | Compositions and methods comprising proteinase activated receptor antagonists |
| DE102005062990A1 (de) | 2005-12-28 | 2007-07-05 | Grünenthal GmbH | Substituierte Thiazole und ihre Verwendung zur Herstellung von Arzneimitteln |
| AU2006335110B2 (en) | 2005-12-30 | 2011-04-14 | Merck Sharp & Dohme Corp. | CETP inhibitors |
| WO2007081570A2 (en) * | 2005-12-30 | 2007-07-19 | Merck & Co., Inc. | Cholesteryl ester transfer protein inhibitors |
| AU2006335108B2 (en) | 2005-12-30 | 2011-04-07 | Merck Sharp & Dohme Corp. | CETP inhibitors |
| AU2006332681B2 (en) | 2005-12-30 | 2011-04-07 | Merck Sharp & Dohme Corp. | 1, 3-oxazolidin-2-one derivatives useful as CETP inhibitors |
| US7998959B2 (en) | 2006-01-12 | 2011-08-16 | Incyte Corporation | Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same |
| EP1991112A1 (en) | 2006-02-27 | 2008-11-19 | Bayer Healthcare, LLC | Temperature-adjusted analyte determination for biosensor systems |
| WO2007101270A1 (en) | 2006-03-02 | 2007-09-07 | Incyte Corporation | MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME |
| WO2007103719A2 (en) | 2006-03-03 | 2007-09-13 | Incyte Corporation | MODULATORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USING THE SAME |
| WO2007109456A2 (en) | 2006-03-16 | 2007-09-27 | Pharmacopeia, Inc. | Substituted biphenyl isoxazole sulfonamides as dual angiotensin endothelin receptor antagonists |
| US7435833B2 (en) | 2006-04-07 | 2008-10-14 | Abbott Laboratories | Inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme |
| MX2008013305A (es) | 2006-04-20 | 2008-10-27 | Du Pont | Agentes heterociclicos de cinco miembros para el control de plagas de invertebrados. |
| MY148128A (en) | 2006-04-21 | 2013-02-28 | Lilly Co Eli | Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| CN101541747B (zh) | 2006-04-21 | 2012-11-14 | 伊莱利利公司 | 作为11-β-羟基甾族化合物脱氢酶1的抑制剂的联苯基酰胺内酰胺衍生物 |
| ES2344616T3 (es) | 2006-04-25 | 2010-09-01 | ELI LILLY & COMPANY | Inhibidores de 11-beta-hidroxiesteroide deshidrogenasa 1. |
| US8178005B2 (en) | 2006-06-20 | 2012-05-15 | Chemtura Corporation | Liquid phosphite compositions having different alkyl groups |
| TW200811170A (en) | 2006-06-27 | 2008-03-01 | Sanofi Aventis | Urea derivatives of tropane, their preparation and their therapeutic application |
| WO2008012622A2 (en) | 2006-07-25 | 2008-01-31 | Pfizer Products Inc. | Azabenzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor |
| WO2008012623A1 (en) | 2006-07-25 | 2008-01-31 | Pfizer Products Inc. | Benzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor |
| WO2008021338A2 (en) | 2006-08-15 | 2008-02-21 | Wyeth | Tricyclic oxazolidone derivatives useful as pr modulators |
| US7649007B2 (en) | 2006-08-15 | 2010-01-19 | Wyeth Llc | Oxazolidine derivatives as PR modulators |
| US7538107B2 (en) | 2006-08-15 | 2009-05-26 | Wyeth | Oxazinan-2-one derivatives useful as PR modulators |
| WO2008024497A2 (en) | 2006-08-25 | 2008-02-28 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF 11β -HYDROXYSTEROID DEHYDROGENASE TYPE 1 |
| US20100168103A1 (en) | 2006-09-14 | 2010-07-01 | Neuromed Pharmaceuticals Ltd. | Diaryl piperidine compounds as calcium channel blockers |
| JP5351025B2 (ja) | 2006-09-22 | 2013-11-27 | ノバルティス アーゲー | ヘテロ環式有機化合物 |
| TW200829171A (en) | 2006-11-17 | 2008-07-16 | Nihon Nohyaku Co Ltd | Haloalkyl sulfonanilide derivatives or salts thereof, herbicide using it as effective constituent and use-method thereof |
| EP1935420A1 (en) | 2006-12-21 | 2008-06-25 | Merck Sante | 2-Adamantyl-butyramide derivatives as selective 11beta-HSD1 inhibitors |
| CA2678577A1 (en) * | 2007-02-26 | 2008-09-04 | Vitae Pharmaceuticals, Inc. | Cyclic urea and carbamate inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1 |
| MX2009010207A (es) | 2007-03-23 | 2009-10-19 | Schering Corp | Peptidos de hidrazido como inhibidores de proteasa ns3 de virus de hepatitis c. |
| AU2008233930A1 (en) | 2007-03-29 | 2008-10-09 | F. Hoffmann-La Roche Ag | Heterocyclic antiviral compounds |
| US8575156B2 (en) | 2007-07-26 | 2013-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1 |
| AR069207A1 (es) | 2007-11-07 | 2010-01-06 | Vitae Pharmaceuticals Inc | Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1 |
| CL2008003407A1 (es) | 2007-11-16 | 2010-01-11 | Boehringer Ingelheim Int | Compuestos derivados de aril- y heteroarilcarbonilo de heterobiciclo sustituido; composicion farmaceutica; procedimiento de preparacion; y su uso en el tratamiento y/o prevencion de trastornos metabolicos, mediado por la inhibicion de la enzima hsd-1. |
| WO2009075835A1 (en) | 2007-12-11 | 2009-06-18 | Vitae Pharmaceutical, Inc | CYCLIC UREA INHIBITORS OF 11β-HYDROXYSTEROID DEHYDROGENASE 1 |
| KR101460359B1 (ko) | 2007-12-13 | 2014-11-10 | 삼성전자주식회사 | 이동통신 시스템에서의 핸드오버 방법 및 장치 |
| 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 |
| EP2252598A2 (en) | 2008-02-11 | 2010-11-24 | Vitae Pharmaceuticals, Inc. | 1,3-oxazepan-2-one and 1,3-diazepan-2-one inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| WO2009100872A1 (en) | 2008-02-12 | 2009-08-20 | Boehringer Ingelheim International Gmbh | Urea derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use |
| US8598160B2 (en) | 2008-02-15 | 2013-12-03 | Vitae Pharmaceuticals, Inc. | Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 |
| US8383629B2 (en) | 2008-02-27 | 2013-02-26 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11β-hydroxysteroid dehydrogenase type 1 |
| CA2718264A1 (en) | 2008-03-18 | 2009-09-24 | Vitae Pharmaceuticals, Inc. | Inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
| TW200944526A (en) | 2008-04-22 | 2009-11-01 | Vitae Pharmaceuticals Inc | Carbamate and urea inhibitors of 11β-hydroxysteroid dehydrogenase 1 |
| WO2009134387A1 (en) | 2008-05-01 | 2009-11-05 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| NZ588954A (en) | 2008-05-01 | 2012-08-31 | Vitae Pharmaceuticals Inc | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| EP2291373B1 (en) | 2008-05-01 | 2013-09-11 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| TW201004945A (en) | 2008-05-01 | 2010-02-01 | Vitae Pharmaceuticals Inc | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| TW200950780A (en) | 2008-05-13 | 2009-12-16 | Boehringer Ingelheim Int | Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use |
| EP2303844A1 (en) | 2008-07-23 | 2011-04-06 | BioAlliance Pharma | Styrylquinolines, their process of preparation and their therapeutic uses |
| US20110224242A1 (en) | 2008-07-23 | 2011-09-15 | Bioalliance Pharma | Styrlyquinolines, their process of preparation and their therapeutic uses |
| CA2729993A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 |
| CN104327062A (zh) | 2008-07-25 | 2015-02-04 | 贝林格尔·英格海姆国际有限公司 | 11β-羟基类固醇脱氢酶1的环状抑制剂 |
| WO2010010174A1 (en) | 2008-07-25 | 2010-01-28 | Boehringer Ingelheim International Gmbh | 1,1'-diadamantyl carboxylic acids, medicaments containing such compounds and their use |
| TW201016691A (en) | 2008-07-25 | 2010-05-01 | Boehringer Ingelheim Int | Inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CA2735204C (en) | 2008-08-25 | 2017-06-20 | Boehringer Ingelheim International Gmbh | Aryl- and heteroarylcarbonyl derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| TW201022266A (en) | 2008-10-23 | 2010-06-16 | Boehringer Ingelheim Int | Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use |
| EP2393807B1 (en) | 2009-02-04 | 2013-08-14 | Boehringer Ingelheim International GmbH | Cyclic inhibitors of 11 -hydroxysteroid dehydrogenase 1 |
| CA2750517A1 (en) | 2009-02-04 | 2010-08-12 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| EP2405913A1 (en) | 2009-03-09 | 2012-01-18 | Bristol-Myers Squibb Company | Pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists |
| GEP20156309B (en) | 2009-04-30 | 2015-07-10 | Vitae Pharmaceuticals Inc | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| MA33216B1 (fr) | 2009-04-30 | 2012-04-02 | Boehringer Ingelheim Int | Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1 |
| AR076936A1 (es) | 2009-06-02 | 2011-07-20 | Vitae Pharmaceuticals Inc | Inhibidores de carbamato y urea de la 11 beta hidroxiesteroide deshidrogenasa 1 |
| EP2438049B1 (en) | 2009-06-02 | 2014-05-14 | Boehringer Ingelheim International GmbH | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| WO2011011123A1 (en) | 2009-06-11 | 2011-01-27 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure |
| EP2448928B1 (en) | 2009-07-01 | 2014-08-13 | Vitae Pharmaceuticals, Inc. | Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 |
| CA2773854A1 (en) | 2009-09-11 | 2011-03-17 | Cylene Pharmaceuticals Inc. | Pharmaceutically useful heterocycle-substituted lactams |
| EP2496589B1 (en) | 2009-11-05 | 2014-03-05 | Boehringer Ingelheim International GmbH | Novel chiral phosphorus ligands |
| TWI531571B (zh) | 2009-11-06 | 2016-05-01 | 維它藥物公司 | 六氫茚并吡啶及八氫苯并喹啉之芳基－及雜芳基羰基衍生物 |
| JP5860042B2 (ja) | 2010-06-16 | 2016-02-16 | 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 | 置換５、６及び７員複素環、そのような化合物を含有する医薬及びそれらの使用 |
| EP2585444B1 (en) | 2010-06-25 | 2014-10-22 | Boehringer Ingelheim International GmbH | Azaspirohexanones as inhibitors of 11-beta-hsd1 for the treatment of metabolic disorders |
| EA201300522A1 (ru) | 2010-11-02 | 2013-11-29 | Бёрингер Ингельхайм Интернациональ Гмбх | Фармацевтические комбинации для лечения метаболических нарушений |
-
2008
- 2008-11-06 AR ARP080104852A patent/AR069207A1/es unknown
- 2008-11-07 WO PCT/US2008/012618 patent/WO2009061498A1/en not_active Ceased
- 2008-11-07 US US12/745,663 patent/US9079861B2/en not_active Expired - Fee Related
- 2008-11-07 CA CA2704222A patent/CA2704222A1/en not_active Abandoned
- 2008-11-07 EP EP08846298.1A patent/EP2220052B1/en not_active Not-in-force
- 2008-11-07 JP JP2010533113A patent/JP5695906B2/ja not_active Expired - Fee Related
- 2008-11-07 CL CL2008003339A patent/CL2008003339A1/es unknown
- 2008-11-07 TW TW097143034A patent/TW200934495A/zh unknown
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