JP2013518845A5 - - Google Patents
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- Publication number
- JP2013518845A5 JP2013518845A5 JP2012551586A JP2012551586A JP2013518845A5 JP 2013518845 A5 JP2013518845 A5 JP 2013518845A5 JP 2012551586 A JP2012551586 A JP 2012551586A JP 2012551586 A JP2012551586 A JP 2012551586A JP 2013518845 A5 JP2013518845 A5 JP 2013518845A5
- Authority
- JP
- Japan
- Prior art keywords
- chloro
- methyl
- trans
- cyclohexyl
- ylmethyl
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 239000001257 hydrogen Substances 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 14
- 150000002431 hydrogen Chemical class 0.000 claims 9
- 150000003839 salts Chemical group 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 102000012289 Corticotropin-Releasing Hormone Human genes 0.000 claims 5
- 108010022152 Corticotropin-Releasing Hormone Proteins 0.000 claims 5
- 239000000055 Corticotropin-Releasing Hormone Substances 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 125000001188 haloalkyl group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- -1 4-((4- (4-chlorophenyl) -5-methyl-1H-pyrazol-3-ylamino) methyl) cyclohexyl Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- GSQGCFTWOSTTHY-UHFFFAOYSA-N 5-chloro-2-methyl-n-[4-[(3,4,5-trimethylpyrazol-1-yl)methyl]cyclohexyl]pyridine-3-carboxamide Chemical compound CC1=C(C)C(C)=NN1CC1CCC(NC(=O)C=2C(=NC=C(Cl)C=2)C)CC1 GSQGCFTWOSTTHY-UHFFFAOYSA-N 0.000 claims 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 239000002671 adjuvant Substances 0.000 claims 2
- 125000005605 benzo group Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 229910052805 deuterium Inorganic materials 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000002464 receptor antagonist Substances 0.000 claims 2
- 229940044551 receptor antagonist Drugs 0.000 claims 2
- CWCYNBYBTACELK-UHFFFAOYSA-N 2-chloro-5-(trifluoromethyl)-n-[4-[(3,4,5-trimethylpyrazol-1-yl)methyl]cyclohexyl]benzamide Chemical compound CC1=C(C)C(C)=NN1CC1CCC(NC(=O)C=2C(=CC=C(C=2)C(F)(F)F)Cl)CC1 CWCYNBYBTACELK-UHFFFAOYSA-N 0.000 claims 1
- AIAQEHWTQAOGLA-UHFFFAOYSA-N 2-chloro-n-[4-[(3-phenylpyrazol-1-yl)methyl]cyclohexyl]-5-(trifluoromethyl)benzamide Chemical compound FC(F)(F)C1=CC=C(Cl)C(C(=O)NC2CCC(CN3N=C(C=C3)C=3C=CC=CC=3)CC2)=C1 AIAQEHWTQAOGLA-UHFFFAOYSA-N 0.000 claims 1
- QJLODLOESBNNPM-UHFFFAOYSA-N 2-chloro-n-[4-[(4-chloro-3,5-dimethylpyrazol-1-yl)methyl]cyclohexyl]-5-(trifluoromethyl)benzamide Chemical compound CC1=C(Cl)C(C)=NN1CC1CCC(NC(=O)C=2C(=CC=C(C=2)C(F)(F)F)Cl)CC1 QJLODLOESBNNPM-UHFFFAOYSA-N 0.000 claims 1
- SUUSNFSQMHCMDE-UHFFFAOYSA-N 2-chloro-n-[4-[[3-(4-methoxyphenyl)-5-methylpyrazol-1-yl]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide Chemical compound C1=CC(OC)=CC=C1C1=NN(CC2CCC(CC2)NC(=O)C=2C(=CC=C(C=2)C(F)(F)F)Cl)C(C)=C1 SUUSNFSQMHCMDE-UHFFFAOYSA-N 0.000 claims 1
- MRZCTSJNLTVOQB-UHFFFAOYSA-N 2-chloro-n-[4-[[4-chloro-3-(hydroxymethyl)pyrazol-1-yl]methyl]cyclohexyl]-5-(trifluoromethyl)benzamide Chemical compound C1=C(Cl)C(CO)=NN1CC1CCC(NC(=O)C=2C(=CC=C(C=2)C(F)(F)F)Cl)CC1 MRZCTSJNLTVOQB-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- YFGJKTCILASHFF-UHFFFAOYSA-N 5-chloro-n-[4-[(3,5-diethylpyrazol-1-yl)methyl]cyclohexyl]-2-methylpyridine-3-carboxamide Chemical compound N1=C(CC)C=C(CC)N1CC1CCC(NC(=O)C=2C(=NC=C(Cl)C=2)C)CC1 YFGJKTCILASHFF-UHFFFAOYSA-N 0.000 claims 1
- FZPRQRQELHONGW-UHFFFAOYSA-N 5-chloro-n-[4-[(3,5-dimethylpyrazol-1-yl)methyl]cyclohexyl]-2-methylpyridine-3-carboxamide Chemical compound N1=C(C)C=C(C)N1CC1CCC(NC(=O)C=2C(=NC=C(Cl)C=2)C)CC1 FZPRQRQELHONGW-UHFFFAOYSA-N 0.000 claims 1
- JRBVOUREXIRPPY-UHFFFAOYSA-N 5-chloro-n-[4-[(4-chloro-3,5-dimethylpyrazol-1-yl)methyl]cyclohexyl]-2-methylpyridine-3-carboxamide Chemical compound CC1=C(Cl)C(C)=NN1CC1CCC(NC(=O)C=2C(=NC=C(Cl)C=2)C)CC1 JRBVOUREXIRPPY-UHFFFAOYSA-N 0.000 claims 1
- KQQMWFWXNSJHJA-UHFFFAOYSA-N 5-chloro-n-[4-[[(5-ethyl-4-methyl-1h-pyrazol-3-yl)amino]methyl]cyclohexyl]-2-methylpyridine-3-carboxamide Chemical compound CC1=C(CC)NN=C1NCC1CCC(NC(=O)C=2C(=NC=C(Cl)C=2)C)CC1 KQQMWFWXNSJHJA-UHFFFAOYSA-N 0.000 claims 1
- 239000000275 Adrenocorticotropic Hormone Substances 0.000 claims 1
- CVWWTNXFLUGTDI-ZHTAKFGLSA-N CC(C(O)=O)c1ccc(NC[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)cc1 Chemical compound CC(C(O)=O)c1ccc(NC[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)cc1 CVWWTNXFLUGTDI-ZHTAKFGLSA-N 0.000 claims 1
- DLODGACIEXJIID-KOMQPUFPSA-N CC(C)(C)c1ccn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 Chemical compound CC(C)(C)c1ccn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 DLODGACIEXJIID-KOMQPUFPSA-N 0.000 claims 1
- WQYAOEVXNPHQHJ-JCNLHEQBSA-N CC(C)c1c(C)cnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F Chemical compound CC(C)c1c(C)cnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F WQYAOEVXNPHQHJ-JCNLHEQBSA-N 0.000 claims 1
- CSYALHPPMSVBIL-SAABIXHNSA-N CC(C)c1cc(C(C)C)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 Chemical compound CC(C)c1cc(C(C)C)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 CSYALHPPMSVBIL-SAABIXHNSA-N 0.000 claims 1
- XIRJFRYFIXCOCZ-SAABIXHNSA-N CC(C)c1cc(C)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)n1 Chemical compound CC(C)c1cc(C)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)n1 XIRJFRYFIXCOCZ-SAABIXHNSA-N 0.000 claims 1
- VFTPTHOIZIMBGU-SAABIXHNSA-N CC(C)c1cc(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(Cl)cnc1C Chemical compound CC(C)c1cc(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(Cl)cnc1C VFTPTHOIZIMBGU-SAABIXHNSA-N 0.000 claims 1
- FKFUKPZBLDIDCA-KOMQPUFPSA-N CC(C)c1cc(CO)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F Chemical compound CC(C)c1cc(CO)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F FKFUKPZBLDIDCA-KOMQPUFPSA-N 0.000 claims 1
- KTYIVOVFFAQTSQ-SAABIXHNSA-N CC(C)c1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)cc1C Chemical compound CC(C)c1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)cc1C KTYIVOVFFAQTSQ-SAABIXHNSA-N 0.000 claims 1
- VDHCHJQTFOXAKF-JCNLHEQBSA-N CC(C)c1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)cc1C Chemical compound CC(C)c1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)cc1C VDHCHJQTFOXAKF-JCNLHEQBSA-N 0.000 claims 1
- SIVDZRMKCXLRPY-CZIWCDLHSA-N CC1=NC=C(Cl)C=C1C(=O)N[C@@H]1CC[C@@H](CN2C=3CCCC=3C=N2)CC1 Chemical compound CC1=NC=C(Cl)C=C1C(=O)N[C@@H]1CC[C@@H](CN2C=3CCCC=3C=N2)CC1 SIVDZRMKCXLRPY-CZIWCDLHSA-N 0.000 claims 1
- UVKGWNIRLPNREG-CZIWCDLHSA-N CC1=NC=C(Cl)C=C1C(=O)N[C@@H]1CC[C@@H](CN2N=C3CCCC3=C2)CC1 Chemical compound CC1=NC=C(Cl)C=C1C(=O)N[C@@H]1CC[C@@H](CN2N=C3CCCC3=C2)CC1 UVKGWNIRLPNREG-CZIWCDLHSA-N 0.000 claims 1
- VCERYFYYVGYTNI-KOMQPUFPSA-N CCOC(=O)c1c(C)cnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F Chemical compound CCOC(=O)c1c(C)cnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F VCERYFYYVGYTNI-KOMQPUFPSA-N 0.000 claims 1
- PZRFQJADLUWQGZ-MQMHXKEQSA-N CCOC(=O)c1c(Cl)cnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F Chemical compound CCOC(=O)c1c(Cl)cnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F PZRFQJADLUWQGZ-MQMHXKEQSA-N 0.000 claims 1
- WLLGCGVEZFNTLJ-CTYIDZIISA-N CCOC(=O)c1ccn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 Chemical compound CCOC(=O)c1ccn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 WLLGCGVEZFNTLJ-CTYIDZIISA-N 0.000 claims 1
- BRXWMNWQXMTVID-CTYIDZIISA-N CCOC(=O)c1ccnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F Chemical compound CCOC(=O)c1ccnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F BRXWMNWQXMTVID-CTYIDZIISA-N 0.000 claims 1
- XZMXFOVTHOXSOH-KOMQPUFPSA-N CCOC(=O)c1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)cc1C Chemical compound CCOC(=O)c1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)cc1C XZMXFOVTHOXSOH-KOMQPUFPSA-N 0.000 claims 1
- VBHAOZNATJEEMB-JCNLHEQBSA-N CCc1c(C)cnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(Cl)cnc1C Chemical compound CCc1c(C)cnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(Cl)cnc1C VBHAOZNATJEEMB-JCNLHEQBSA-N 0.000 claims 1
- LMFKNZJLPGRGKR-KOMQPUFPSA-N CCc1c(C)cnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F Chemical compound CCc1c(C)cnn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F LMFKNZJLPGRGKR-KOMQPUFPSA-N 0.000 claims 1
- FSQVOSCRZKKFOF-CTYIDZIISA-N CCc1c(Cl)c(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F Chemical compound CCc1c(Cl)c(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F FSQVOSCRZKKFOF-CTYIDZIISA-N 0.000 claims 1
- KUKANTJOKSAEMK-CZIWCDLHSA-N CCc1cc(C)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 Chemical compound CCc1cc(C)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 KUKANTJOKSAEMK-CZIWCDLHSA-N 0.000 claims 1
- CQDAKWJVFKETDG-KOMQPUFPSA-N CCc1cc(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F Chemical compound CCc1cc(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F CQDAKWJVFKETDG-KOMQPUFPSA-N 0.000 claims 1
- YRZWOGUFXLWUKM-CZIWCDLHSA-N CCc1cc(CC)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 Chemical compound CCc1cc(CC)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 YRZWOGUFXLWUKM-CZIWCDLHSA-N 0.000 claims 1
- VNUJFEHKOZBNKG-JCNLHEQBSA-N CCc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)cc1C Chemical compound CCc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)cc1C VNUJFEHKOZBNKG-JCNLHEQBSA-N 0.000 claims 1
- WYPKJBZTZFZUPF-CTYIDZIISA-N CCc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)c(C)c1Cl Chemical compound CCc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)c(C)c1Cl WYPKJBZTZFZUPF-CTYIDZIISA-N 0.000 claims 1
- KUHXDWVHYWXSOZ-CTYIDZIISA-N CCc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)c(CC)c1Cl Chemical compound CCc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)c(CC)c1Cl KUHXDWVHYWXSOZ-CTYIDZIISA-N 0.000 claims 1
- UXTJTLDUDAQOMQ-KOMQPUFPSA-N CCc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)cc1C Chemical compound CCc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)cc1C UXTJTLDUDAQOMQ-KOMQPUFPSA-N 0.000 claims 1
- UFNOQJNGEZPSNX-MQMHXKEQSA-N COc1c(Cl)c(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F Chemical compound COc1c(Cl)c(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F UFNOQJNGEZPSNX-MQMHXKEQSA-N 0.000 claims 1
- LUOQQPVHUYVFNA-KOMQPUFPSA-N COc1cc(C)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)n1 Chemical compound COc1cc(C)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)n1 LUOQQPVHUYVFNA-KOMQPUFPSA-N 0.000 claims 1
- ASLHIRDCUBBIEL-CTYIDZIISA-N COc1cc(C)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 Chemical compound COc1cc(C)n(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 ASLHIRDCUBBIEL-CTYIDZIISA-N 0.000 claims 1
- JOSMVOMZCLJNAS-KOMQPUFPSA-N COc1cc(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(Cl)cnc1C Chemical compound COc1cc(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(Cl)cnc1C JOSMVOMZCLJNAS-KOMQPUFPSA-N 0.000 claims 1
- KJEKFLMCRQCNRL-CTYIDZIISA-N COc1cc(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F Chemical compound COc1cc(C)nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F KJEKFLMCRQCNRL-CTYIDZIISA-N 0.000 claims 1
- WYTQVDBYGFCFCU-CTYIDZIISA-N COc1ccc(Cl)c(NC[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)n1 Chemical compound COc1ccc(Cl)c(NC[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)n1 WYTQVDBYGFCFCU-CTYIDZIISA-N 0.000 claims 1
- MURHVXZELMNENA-RUCARUNLSA-N COc1ccc(cc1)-c1ccn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 Chemical compound COc1ccc(cc1)-c1ccn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)n1 MURHVXZELMNENA-RUCARUNLSA-N 0.000 claims 1
- SCPATYFCJLYFTI-CTYIDZIISA-N COc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)c(C)c1Cl Chemical compound COc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(Cl)cnc2C)c(C)c1Cl SCPATYFCJLYFTI-CTYIDZIISA-N 0.000 claims 1
- LQOCDLGXBNNPRZ-MQMHXKEQSA-N COc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)c(C)c1Cl Chemical compound COc1nn(C[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)c(C)c1Cl LQOCDLGXBNNPRZ-MQMHXKEQSA-N 0.000 claims 1
- KEVHTHIFWWAZOE-RHDGDCLCSA-N Cc1[nH]nc(NC[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)c1-c1ccc(F)cc1 Chemical compound Cc1[nH]nc(NC[C@H]2CC[C@@H](CC2)NC(=O)c2cc(ccc2Cl)C(F)(F)F)c1-c1ccc(F)cc1 KEVHTHIFWWAZOE-RHDGDCLCSA-N 0.000 claims 1
- NICNGJBCHOEQET-MQMHXKEQSA-N Cc1c(Cl)c(nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(Cl)cnc1C)C(F)(F)F Chemical compound Cc1c(Cl)c(nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(Cl)cnc1C)C(F)(F)F NICNGJBCHOEQET-MQMHXKEQSA-N 0.000 claims 1
- XDRNJBXWFMSCQY-KOMQPUFPSA-N Cc1c2COCCc2nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F Chemical compound Cc1c2COCCc2nn1C[C@H]1CC[C@@H](CC1)NC(=O)c1cc(ccc1Cl)C(F)(F)F XDRNJBXWFMSCQY-KOMQPUFPSA-N 0.000 claims 1
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Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10703722B2 (en) | 2010-04-27 | 2020-07-07 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
| RS65839B1 (sr) | 2014-01-21 | 2024-09-30 | Neurocrine Biosciences Inc | Crf1 receptor antagonisti za tretman kongenitalne adrenalne hiperplazije |
| EP3778595B1 (en) | 2015-02-27 | 2021-08-25 | Calcimedica, Inc. | Pancreatitis treatment |
| CA2995094A1 (en) | 2015-08-07 | 2017-02-16 | Calcimedica, Inc. | Use of crac channel inhibitors for the treatment of stroke and traumatic brain injury |
| JOP20170153A1 (ar) | 2016-07-15 | 2019-01-30 | Lilly Co Eli | نظائر urocortin-2 جديدة معدلة بحمض دهني لعلاج داء السكري وأمراض الكلى المزمنة |
| EP3661500B1 (en) | 2017-07-31 | 2026-01-07 | Novartis AG | Use of mavoglurant in the reduction of cocaine use or in preventing relapse into cocaine use |
| EP3716972A4 (en) | 2017-11-29 | 2021-08-25 | The Rockefeller University | PYRANOPYRAZOLE AND PYRAZOLOPYRIDINE IMMUNOMODULATORS FOR THE TREATMENT OF AUTOIMMUNE DISEASES |
| WO2019118785A2 (en) | 2017-12-13 | 2019-06-20 | Praxis Biotech LLC | Inhibitors of integrated stress response pathway |
| EP3774739B1 (en) * | 2018-04-09 | 2022-05-11 | RaQualia Pharma Inc. | Fused cyclic urea derivatives as crhr2 antagonist |
| WO2019236710A1 (en) | 2018-06-05 | 2019-12-12 | Praxis Biotech LLC | Inhibitors of integrated stress response pathway |
| US20220023266A1 (en) | 2018-12-07 | 2022-01-27 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia |
| MX2021015210A (es) * | 2019-06-12 | 2022-01-18 | Praxis Biotech LLC | Inhibidores de la via de respuesta al estres integrada. |
| JP2022536663A (ja) | 2019-06-12 | 2022-08-18 | プラクシス バイオテック エルエルシー | 統合的ストレス応答経路のモジュレーター |
| JP7623365B2 (ja) | 2019-09-27 | 2025-01-28 | ニューロクライン バイオサイエンシーズ,インコーポレイテッド | Crf受容体アンタゴニストおよび使用方法 |
| TW202140480A (zh) * | 2020-01-15 | 2021-11-01 | 日商拉夸里亞創藥股份有限公司 | 作為crhr2拮抗劑之螺雜環衍生物 |
| JP2023528537A (ja) | 2020-03-20 | 2023-07-04 | カルシメディカ,インク. | 急性肺傷害及び急性呼吸窮迫症候群を処置するための方法及び組成物 |
| JP2023545256A (ja) | 2020-09-30 | 2023-10-27 | ラクオリア創薬株式会社 | Crhr2拮抗薬としての3-ヒドロキシオキシインドール誘導体 |
| CA3198798A1 (en) | 2020-11-13 | 2022-05-19 | Kenneth Stauderman | Improved synthesis of crac channel inhibitors |
Family Cites Families (198)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
| US6403599B1 (en) | 1995-11-08 | 2002-06-11 | Pfizer Inc | Corticotropin releasing factor antagonists |
| TW544448B (en) | 1997-07-11 | 2003-08-01 | Novartis Ag | Pyridine derivatives |
| GB9802251D0 (en) | 1998-02-03 | 1998-04-01 | Ciba Geigy Ag | Organic compounds |
| ID29095A (id) | 1998-10-02 | 2001-07-26 | Novartis Ag Cs | Antagonis mglur5 untuk pengobatan rasa sakit dan kegelisahan |
| US6525203B1 (en) | 1999-03-12 | 2003-02-25 | Bristol-Myers Squibb Company | Heterocyclic aromatic compounds useful as growth hormone secretagogues |
| GB0028702D0 (en) | 2000-11-24 | 2001-01-10 | Novartis Ag | Organic compounds |
| PL363907A1 (en) | 2001-03-26 | 2004-11-29 | Novartis Ag | Fused pyridine derivatives for use as vanilloid receptor antagonists for treating pain. |
| CA2905585C (en) | 2001-03-29 | 2020-02-18 | Bausch Health Ireland Limited | Guanylate cyclase receptor agonists for the treatment and/or prevention of cancer or polyps |
| JP3894035B2 (ja) | 2001-07-04 | 2007-03-14 | 東レ株式会社 | 炭素繊維強化基材、それからなるプリフォームおよび複合材料 |
| TW200306839A (en) | 2002-02-06 | 2003-12-01 | Novartis Ag | Quinazolinone derivatives and their use as CB agonists |
| US6696468B2 (en) | 2002-05-16 | 2004-02-24 | Dainippon Pharmaceutical Co., Ltd. | (s)-4-amino-5-chloro-2-methoxy-n-[1-[1-(2-tetrahydrofuryl-carbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamide, process for the preparation thereof, pharmaceutical composition containing the same, and intermediate therefor |
| SE0201940D0 (sv) | 2002-06-20 | 2002-06-20 | Astrazeneca Ab | New combination II |
| DOP2003000703A (es) | 2002-09-20 | 2004-03-31 | Pfizer | Compuestos de imidazopiradina como agonistas del receptor 5-ht4 |
| GB0223730D0 (en) | 2002-10-11 | 2002-11-20 | Novartis Ag | Organic compounds |
| PE20040844A1 (es) | 2002-11-26 | 2004-12-30 | Novartis Ag | Acidos fenilaceticos y derivados como inhibidores de la cox-2 |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| GB0302876D0 (en) | 2003-02-07 | 2003-03-12 | Novartis Ag | Organic compounds |
| JP2007524596A (ja) | 2003-02-28 | 2007-08-30 | トランスフォーム・ファーマシューティカルズ・インコーポレイテッド | 共結晶医薬組成物 |
| JP2004277318A (ja) | 2003-03-14 | 2004-10-07 | Dainippon Pharmaceut Co Ltd | 1−(1−置換カルボニル−4−ピペリジニルメチル)ピペリジン誘導体およびそれを含有する医薬組成物 |
| JP2004277319A (ja) | 2003-03-14 | 2004-10-07 | Dainippon Pharmaceut Co Ltd | 1−(4−ピペリジニルメチル)ピペリジニルアミド誘導体およびそれを含有する医薬組成物 |
| JP2007501866A (ja) | 2003-06-13 | 2007-02-01 | マイクロバイア インコーポレイテッド | 胃腸疾患の治療のための方法および組成物 |
| US7491695B2 (en) | 2003-06-18 | 2009-02-17 | Tranzyme Pharma Inc. | Methods of using macrocyclic modulators of the ghrelin receptor |
| US7476653B2 (en) | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, Inc. | Macrocyclic modulators of the ghrelin receptor |
| EP1505064A1 (en) | 2003-08-05 | 2005-02-09 | Bayer HealthCare AG | 2-Aminopyrimidine derivatives |
| JP2007501822A (ja) | 2003-08-12 | 2007-02-01 | エフ.ホフマン−ラ ロシュ アーゲー | コルチコトロピン放出性因子(crf)アンタゴニストとしてのスピロ置換テトラヒドロキナゾリン |
| ES2293317T3 (es) | 2003-08-12 | 2008-03-16 | F. Hoffmann-La Roche Ag | Derivados de tetrahidroquinazolina com antagonistas de cfr. |
| WO2005068448A1 (en) | 2003-08-29 | 2005-07-28 | Ionix Pharmaceuticals Limited | Sulfonamides antagonising n-type calcium channels |
| CA2537916A1 (en) | 2003-09-03 | 2005-03-31 | Neurogen Corporation | 5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds |
| UA86204C2 (uk) | 2003-09-03 | 2009-04-10 | Пфайзер Инк. | Сполуки бензімідазолону, які мають 5-нт4 рецепторну агоністичну активність |
| AR045582A1 (es) | 2003-09-05 | 2005-11-02 | Neurogen Corp | Piridinas pirazinas y pirimidinas heteroarilo fusionadas como ligandos receptores de crf1 |
| JP2005082508A (ja) | 2003-09-05 | 2005-03-31 | Dainippon Pharmaceut Co Ltd | 2−アルコキシ−6−アミノ−5−ハロゲノ−n−(1−置換−4−ピペリジニル)ピリジン−3−カルボキサミド誘導体およびそれを含有する医薬組成物 |
| AU2004272437A1 (en) | 2003-09-09 | 2005-03-24 | Ono Pharmaceutical Co., Ltd. | CRF antagonists and heterobicyclic compounds |
| GB0322612D0 (en) | 2003-09-26 | 2003-10-29 | Novartis Ag | Organic compounds |
| KR20060111466A (ko) | 2003-09-30 | 2006-10-27 | 얀센 파마슈티카 엔.브이. | 퀴녹살린 화합물 |
| JP2005104896A (ja) | 2003-09-30 | 2005-04-21 | Dainippon Pharmaceut Co Ltd | 2−アルコキシ−6−アミノ−5−ハロゲノピリジン−3−カルボキサミド誘導体およびそれを含有する医薬組成物 |
| RU2006110561A (ru) | 2003-09-30 | 2007-10-10 | Янссен Фармацевтика Н.В. (Be) | Соединения бензоимидазола |
| EP1677791A4 (en) | 2003-10-31 | 2007-08-15 | Takeda Pharmaceutical | NITROGENIC CONDENSED HETEROCYCLIC COMPOUNDS |
| EP1677789A1 (en) | 2003-10-31 | 2006-07-12 | AstraZeneca AB | Alkynes i |
| CN1922156A (zh) | 2003-11-10 | 2007-02-28 | 默克公司 | 作为钠通道阻断剂的取代的三唑 |
| US7208596B2 (en) | 2003-11-25 | 2007-04-24 | Bristol-Myers Squibb Pharma Company | Processes for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof |
| WO2005054239A1 (en) | 2003-12-05 | 2005-06-16 | Bayer Healthcare Ag | 2-aminopyrimidine derivatives |
| US7211568B2 (en) | 2003-12-18 | 2007-05-01 | Kosan Biosciences Incorporated | 9-Desoxoerythromycin compounds as prokinetic agents |
| CA2548039A1 (en) | 2003-12-19 | 2005-07-21 | Astrazenca Ab | 5-fluoro-, chloro- and cyano-pyridin-2-yl-tetrazoles as ligands of the metabotropic glutamate receptor-5 |
| MY143499A (en) * | 2003-12-22 | 2011-05-31 | Sb Pharmco Inc | Crf receptor antagonist and methods relating thereto |
| JP2005206590A (ja) | 2003-12-25 | 2005-08-04 | Mitsubishi Pharma Corp | ナトリウムチャネルサイト2選択的阻害剤 |
| RU2374244C2 (ru) | 2004-01-07 | 2009-11-27 | Арикс Терапьютикс | Стереоизомерные соединения и способы лечения желудочно-кишечных расстройств и расстройств центральной нервной системы |
| TW200530181A (en) | 2004-01-13 | 2005-09-16 | Bristol Myers Squibb Co | Heterocyclic compounds useful as growth hormone secretagogues |
| DE602005005167T2 (de) | 2004-01-29 | 2009-04-30 | Pfizer Inc. | 1-isopropyl-2-oxo-1,2-dihydropyridin-3-carbonsäureamidderivate mit agonistischer wirkung am 5-ht4-rezeptor |
| WO2005077345A1 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Compounds for the treatment of gastro-esophageal reflux disease |
| WO2005077373A2 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
| US20070185100A1 (en) | 2004-02-18 | 2007-08-09 | Astrazeneca Ab | Poly-heterocyclic compounds and their use as metabotropic glutamate receptor antagonists |
| TW200531694A (en) | 2004-02-18 | 2005-10-01 | Astrazeneca Ab | Acetylinic piperazine compounds and their use as metabotropic glutamate receptor antagonists |
| DE602005008558D1 (de) | 2004-02-18 | 2008-09-11 | Astrazeneca Ab | Kondensierte heterocyclische verbindungen und deren verwendung als antagonisten des metabotropen reznkungen |
| WO2005080356A1 (en) | 2004-02-18 | 2005-09-01 | Astrazeneca Ab | Tetrazole compounds and their use as metabotropic glutamate receptor antagonits |
| US7585881B2 (en) | 2004-02-18 | 2009-09-08 | Astrazeneca Ab | Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists |
| RU2006127575A (ru) | 2004-02-18 | 2008-03-27 | Астразенека Аб (Se) | Соединение триазола и их применение в качестве антагонистов метаботропного рецептора глутамата |
| TW200533348A (en) | 2004-02-18 | 2005-10-16 | Theravance Inc | Indazole-carboxamide compounds as 5-ht4 receptor agonists |
| TW200538108A (en) | 2004-02-19 | 2005-12-01 | Astrazeneca Ab | Fused heterocyclic compounds and their use as metabotropic glutamate receptor antagonists |
| TW200538180A (en) | 2004-02-20 | 2005-12-01 | Astrazeneca Ab | New compounds |
| WO2005092882A1 (en) | 2004-03-01 | 2005-10-06 | Pfizer Japan, Inc. | 4-amino-5-halogeno-benzamide derivatives as 5-ht4 receptor agonists for the treatment of gastrointestinal, cns, neurological and cardiovascular disorders |
| US7087749B2 (en) | 2004-03-11 | 2006-08-08 | Adolor Corporation | Substituted piperidine compounds and methods of their use |
| AU2005226729B2 (en) | 2004-03-25 | 2010-01-28 | Janssen Pharmaceutica N.V. | Imidazole compounds |
| EP1732564A1 (en) | 2004-03-29 | 2006-12-20 | Merck & Co., Inc. | Biaryl substituted pyrazinones as sodium channel blockers |
| WO2005097788A2 (en) | 2004-04-02 | 2005-10-20 | Elixir Pharmaceuticals, Inc. | Sulfonamides and uses thereof |
| TWI351282B (en) | 2004-04-07 | 2011-11-01 | Theravance Inc | Quinolinone-carboxamide compounds as 5-ht4 recepto |
| EP1734820A4 (en) | 2004-04-16 | 2008-01-23 | Neurogen Corp | Imidazopyrrazine, imidazopyridine, and imidazo-pyrimidine as CRF1 receptor ligands |
| GB0412769D0 (en) | 2004-06-08 | 2004-07-07 | Novartis Ag | Organic compounds |
| GB0412768D0 (en) | 2004-06-08 | 2004-07-07 | Novartis Ag | Organic compounds |
| CA2569654C (en) | 2004-06-15 | 2010-12-21 | Pfizer Inc. | Benzimidazolone carboxylic acid derivatives |
| PE20060526A1 (es) | 2004-06-15 | 2006-07-13 | Schering Corp | Compuestos triciclicos como antagonistas de mglur1 |
| SE0401653D0 (sv) | 2004-06-24 | 2004-06-24 | Astrazeneca Ab | New compounds |
| WO2006006740A1 (ja) | 2004-07-14 | 2006-01-19 | Japan Tobacco Inc. | 3−アミノベンズアミド化合物及びバニロイド受容体1型(vr1)活性阻害剤 |
| MX2007000480A (es) | 2004-07-15 | 2007-03-29 | Japan Tobacco Inc | Compuesto de benzamida fusionado e inhibidor de actividad de receptor de vainilloide 1. |
| US20080039430A1 (en) | 2004-07-19 | 2008-02-14 | Ali Ouaissi | Pharmaceutical Compositions For The Treatment Of Leishmaniasis |
| PE20060574A1 (es) | 2004-07-28 | 2006-06-24 | Glaxo Group Ltd | Derivados de arilpiperazina sulfonamida como agonistas de los receptores de secretagogos de la hormona del crecimiento (ghs) |
| ITMI20041566A1 (it) | 2004-07-30 | 2004-10-30 | Indena Spa | "trpv1 agonisti, formulazioni che li contengono e loro usi" |
| WO2006016218A1 (en) | 2004-08-03 | 2006-02-16 | Pfizer Japan Inc. | Aryl or heteroaryl carbonyl derivatives derivatives useful as vanilloid receptor 1 (vr1) antagonists |
| WO2006023757A2 (en) | 2004-08-19 | 2006-03-02 | University Of Virginia Patent Foundation | Novel tricyclic, bicyclic, monocyclic, and acyclic amines as potent sodium channel blocking agents |
| AU2005284904A1 (en) | 2004-09-13 | 2006-03-23 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| GB0420424D0 (en) | 2004-09-14 | 2004-10-20 | Ionix Pharmaceuticals Ltd | Therapeutic compounds |
| US20060063792A1 (en) | 2004-09-17 | 2006-03-23 | Adolor Corporation | Substituted morphinans and methods of their use |
| SE0402284D0 (sv) | 2004-09-21 | 2004-09-21 | Astrazeneca Ab | New heterocyclic amides |
| EP1797090A4 (en) | 2004-09-27 | 2009-11-11 | Elixir Pharmaceuticals Inc | SULFONAMIDES AND USES THEREOF |
| WO2006038594A1 (ja) | 2004-10-04 | 2006-04-13 | Ono Pharmaceutical Co., Ltd. | N型カルシウムチャネル阻害薬 |
| CA2583572C (en) | 2004-10-07 | 2016-07-12 | Merck & Co., Inc. | Thiazolyl mglur5 antagonists and methods for their use |
| JP2008515884A (ja) | 2004-10-08 | 2008-05-15 | アストラゼネカ・アクチエボラーグ | 新規なヒドロキシメチルベンゾチアゾールアミド |
| US8143425B2 (en) | 2004-10-12 | 2012-03-27 | Bristol-Myers Squibb Company | Heterocyclic aromatic compounds useful as growth hormone secretagogues |
| WO2006044527A1 (en) | 2004-10-15 | 2006-04-27 | Amgen Inc. | Imidazole derivatives as vanilloid receptor ligands |
| US7652035B2 (en) | 2004-10-19 | 2010-01-26 | Neurocrine Bioscience, Inc. | CRF receptor antagonists and methods relating thereto |
| GB0519957D0 (en) * | 2005-09-30 | 2005-11-09 | Sb Pharmco Inc | Chemical compound |
| EP1807418A2 (en) | 2004-10-22 | 2007-07-18 | Amgen, Inc | Substituted nitrogen-containing heterocycles as vanilloid receptor ligands and their uses as medicament |
| WO2006048771A1 (en) | 2004-11-04 | 2006-05-11 | Addex Pharmaceuticals Sa | Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors |
| EP1807423B1 (en) | 2004-11-05 | 2009-05-20 | Theravance, Inc. | Quinolinone-carboxamide compounds |
| ATE441646T1 (de) | 2004-11-05 | 2009-09-15 | Theravance Inc | 5-ht4-rezeptoragonistenverbindungen |
| EP1812113A1 (en) | 2004-11-11 | 2007-08-01 | Argenta Discovery Limited | Pyrimidine compounds as histamine modulators |
| US20060111416A1 (en) | 2004-11-24 | 2006-05-25 | Lane Charlotte A L | Octahydropyrrolo[3,4-C]pyrrole derivatives |
| NZ555318A (en) | 2004-11-24 | 2011-01-28 | Abbott Lab | Chromanylurea compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor and uses thereof |
| WO2006058338A2 (en) | 2004-11-29 | 2006-06-01 | Janssen Pharmaceutica N.V. | 4 - piperidinecarboxamide derivatives as modulators of vanilloid vr1 receptor |
| US7875627B2 (en) | 2004-12-07 | 2011-01-25 | Abbott Laboratories | Thienopyridyl compounds that inhibit vanilloid receptor subtype 1 (VR1) and uses thereof |
| US20060128710A1 (en) | 2004-12-09 | 2006-06-15 | Chih-Hung Lee | Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof |
| US7615570B2 (en) | 2004-12-13 | 2009-11-10 | Abbott Laboratories | Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof |
| SE0403117D0 (sv) | 2004-12-21 | 2004-12-21 | Astrazeneca Ab | New compounds 1 |
| SE0403118D0 (sv) | 2004-12-21 | 2004-12-21 | Astrazeneca Ab | New compounds 2 |
| ATE469897T1 (de) | 2004-12-22 | 2010-06-15 | Theravance Inc | Indazolcarbonsäureamidverbindungen |
| SE0403171D0 (sv) | 2004-12-23 | 2004-12-23 | Astrazeneca Ab | New compounds |
| BRPI0606644A2 (pt) | 2005-01-14 | 2009-07-14 | Hoffmann La Roche | derivados de 4-carboxamida tiazola |
| EP1836203A2 (en) | 2005-01-14 | 2007-09-26 | Neurogen Corporation | Heteroaryl substituted quinolin-4-ylamine analogues |
| US7429608B2 (en) | 2005-01-20 | 2008-09-30 | Amgen Inc. | Benzo[d]imidazol analogs as vanilloid receptor ligands and their use in treatments |
| US7301022B2 (en) | 2005-02-15 | 2007-11-27 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| WO2006088988A1 (en) | 2005-02-17 | 2006-08-24 | Theravance, Inc. | Crystalline form of an indazole-carboxamide compound |
| GB0503646D0 (en) | 2005-02-22 | 2005-03-30 | Novartis Ag | Organic compounds |
| DE602006014531D1 (de) | 2005-03-03 | 2010-07-08 | Janssen Pharmaceutica Nv | Substituierte oxadiazaspiro-ä5.5ü-undecanonderivate und ihre verwendung als neurokininantagonisten |
| ES2331153T3 (es) | 2005-03-10 | 2009-12-22 | Pfizer Inc. | Compuestos de n-sulfonilaminofeniletil-2-fenoxiacetamida sustituidos. |
| US20060211710A1 (en) | 2005-03-17 | 2006-09-21 | Pfizer Inc | Substituted aryl 1,4-pyrazine derivatives |
| GB0506147D0 (en) | 2005-03-24 | 2005-05-04 | Merck Sharp & Dohme | Therapeutic agents |
| WO2006102645A1 (en) | 2005-03-24 | 2006-09-28 | Janssen Pharmaceutica, N.V. | Biaryl derived amide modulators of vanilloid vr1 receptor |
| WO2006105117A2 (en) | 2005-03-28 | 2006-10-05 | Dynogen Pharmaceuticals, Inc. | Method of treating disorders and conditions using peripherally-restricted antagonists and inhibitors |
| TWI377206B (en) | 2005-04-06 | 2012-11-21 | Theravance Inc | Crystalline form of a quinolinone-carboxamide compound |
| WO2006113769A1 (en) | 2005-04-15 | 2006-10-26 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| GB0508314D0 (en) | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
| GB0508318D0 (en) | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
| US20060241296A1 (en) | 2005-04-25 | 2006-10-26 | Doherty Elizabeth M | Vanilloid receptor ligands and their use in treatments |
| GB0508319D0 (en) | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
| AU2006243987B2 (en) | 2005-05-11 | 2011-11-24 | Abbott Laboratories | Antagonists of the vanilloid receptor subtype 1 (VR1) and uses thereof |
| US20090298856A1 (en) | 2005-05-11 | 2009-12-03 | Rebecca Elizabeth Brown | 2,3 Substituted fused bicyclic pyrimidin-4(3H)-ones modulating the function of the vanilliod-1receptor (VR1) |
| GB0509573D0 (en) | 2005-05-11 | 2005-06-15 | Merck Sharp & Dohme | Therapeutic compounds |
| WO2006124753A2 (en) | 2005-05-12 | 2006-11-23 | Amgen Inc. | Antipyretic agents against vr1-antagonist-induced increases in body temperature |
| EP1893606A2 (en) | 2005-05-18 | 2008-03-05 | Addex Pharma SA | Substituted oxadiazole derivatives as positive allosteric modulators of metabotropic glutamate receptors |
| DE102005023588A1 (de) | 2005-05-18 | 2006-11-23 | Grünenthal GmbH | Salze substituierter Allophansäureester und deren Verwendung in Arzneimitteln |
| DE102005038947A1 (de) | 2005-05-18 | 2006-11-30 | Grünenthal GmbH | Substituierte Benzo[d]isoxazol-3-yl-amin-Verbindungen und deren Verwendung in Arzneimitteln |
| GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
| GB0510142D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds A1 |
| GB0510141D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B3 |
| GB0510140D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B2 |
| DE102005044814A1 (de) | 2005-05-19 | 2006-11-23 | Grünenthal GmbH | Substituierte Sprio-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln |
| DE102005023784A1 (de) | 2005-05-19 | 2006-11-30 | Grünenthal GmbH | Substituierte Spiro-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln |
| DE102005044813A1 (de) | 2005-05-19 | 2007-10-04 | Grünenthal GmbH | Substituierte Spiro-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln |
| DE102005024012A1 (de) | 2005-05-20 | 2006-11-23 | Grünenthal GmbH | Verwendung von 2,5-disubstituierten Thiazol-4-on-Derivaten in Arzneimitteln |
| US7582611B2 (en) | 2005-05-24 | 2009-09-01 | Pfizer Inc. | Motilide compounds |
| MY147756A (en) | 2005-05-25 | 2013-01-15 | Theravance Inc | Benzimidazole-carboxamide compounds as 5-ht4 receptor agonists |
| US7317022B2 (en) | 2005-06-07 | 2008-01-08 | Theravance, Inc. | Benzoimidazolone-carboxamide compounds as 5-HT4 receptors agonists |
| CN101248042A (zh) | 2005-06-10 | 2008-08-20 | 伊利舍医药品公司 | 磺酰胺类化合物及其用途 |
| US20100069346A1 (en) | 2005-06-23 | 2010-03-18 | Sara Holmqvist | New Azetidine Derivatives as Neurokinin Receptor Antagonists for the Treatment of Gastrointestinal Diseases |
| JP2008546768A (ja) | 2005-06-23 | 2008-12-25 | アストラゼネカ・アクチエボラーグ | 胃腸疾患を治療するためのニューロキニン受容体アンタゴニストとしての新規なアゼチジン誘導体 |
| US20090170872A1 (en) | 2005-07-05 | 2009-07-02 | Orchid Research Laboratories Limited | Compounds and Their Pharmaceutical Use |
| WO2007005951A2 (en) | 2005-07-05 | 2007-01-11 | Aryx Therapeutics, Inc. | Stereoisomeric pyridyl and pyridonyl compounds and methods for the treatment of gastrointestinal and central nervous system disorders |
| EP1902022A1 (en) | 2005-07-12 | 2008-03-26 | Glaxo Group Limited | Piperazine heteroaryl derivates as gpr38 agonists |
| RU2416612C9 (ru) | 2005-07-22 | 2012-03-27 | Ипсен Фарма С.А.С. | Стимуляторы секреции гормона роста |
| CA2615611C (en) | 2005-07-22 | 2011-09-27 | Pfizer Inc. | Indazole derivatives |
| SI1907374T1 (sl) | 2005-07-26 | 2012-11-30 | Glaxo Group Ltd | Derivati benzilpiperazina uporabni za zdravljenje gastrointestinalnih motenj |
| EP1757290A1 (en) | 2005-08-16 | 2007-02-28 | Zentaris GmbH | Novel triazole derivatives as ghrelin analogue ligands of growth hormone secretagogue receptors |
| WO2007022531A2 (en) | 2005-08-19 | 2007-02-22 | Microbia, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| WO2007023242A1 (en) | 2005-08-24 | 2007-03-01 | Merz Pharma Gmbh & Co. Kgaa | Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors |
| EP1943247A1 (en) | 2005-08-25 | 2008-07-16 | Merz Pharma GmbH & Co.KGaA | Tetrahydroquinolinones and their use as modulators of metabotropic glutamate receptors |
| WO2007030761A2 (en) | 2005-09-08 | 2007-03-15 | Smithkline Beecham Corporation | Acyclic 1,4-diamines and uses thereof |
| CA2622372A1 (en) | 2005-09-13 | 2007-03-22 | Palau Pharma, S.A. | 2-aminopyrimidine derivatives as modulators of the histamine h4 receptor activity |
| AR056087A1 (es) | 2005-09-29 | 2007-09-19 | Astrazeneca Ab | Derivados de azetidina como antagonistas de receptores de neuroquina nk |
| UY29796A1 (es) | 2005-09-29 | 2007-04-30 | Astrazeneca Ab | Nuevos compuestos para el tratamiento de trastornos neurológicos, psiquiátricos o del dolor |
| AR057828A1 (es) | 2005-09-29 | 2007-12-19 | Astrazeneca Ab | Compuestos derivados de azetidina, su preparacion y composicion farmaceuutica |
| HUP0500920A2 (en) | 2005-10-05 | 2007-07-30 | Richter Gedeon Nyrt | Oxadiazole derivatives, process for their preparation and their use |
| HUP0500921A2 (en) | 2005-10-05 | 2007-07-30 | Richter Gedeon Nyrt | Tetrazole derivatives, process for their preparation and their use |
| JP2009511465A (ja) | 2005-10-07 | 2009-03-19 | グレンマーク・ファーマシューティカルズ・エスエー | 置換ベンゾ縮合誘導体およびバニロイド受容体リガンドとしてのその使用 |
| DK1940821T3 (da) | 2005-10-19 | 2013-06-10 | Gruenenthal Gmbh | Nye vanilloid-receptorligander og deres anvendelse til fremstilling af lægemidler. |
| US7902251B2 (en) | 2005-10-19 | 2011-03-08 | Allergan, Inc. | Method for treating pain |
| US20070088073A1 (en) | 2005-10-19 | 2007-04-19 | Allergan, Inc. | Method for treating pain |
| US7538110B2 (en) | 2005-10-27 | 2009-05-26 | Adolor Corporation | Opioid antagonists |
| CN101365684A (zh) | 2005-10-28 | 2009-02-11 | 艾博特公司 | 抑制trpv1受体的吲唑衍生物 |
| WO2007048643A1 (en) | 2005-10-28 | 2007-05-03 | Glaxo Group Limited | Novel compound |
| JP2007122605A (ja) | 2005-10-31 | 2007-05-17 | Fujitsu Ltd | インピーダンス回路、電源装置 |
| US20070105920A1 (en) | 2005-11-08 | 2007-05-10 | Akzo Nobel N.V. | 2-(Benzimidazol-1-Yl)-N-(4-phenylthiazol-2-yl) acetamide derivatives |
| GB0525661D0 (en) | 2005-12-16 | 2006-01-25 | Glaxo Group Ltd | Novel compounds |
| NL2000323C2 (nl) | 2005-12-20 | 2007-11-20 | Pfizer Ltd | Pyrimidine-derivaten. |
| WO2007090853A1 (en) | 2006-02-10 | 2007-08-16 | Cellzome (Uk) Ltd. | Enantiomers of amino pyrimidine compounds for the treatment of inflammatory disorders |
| EP1829879A1 (en) | 2006-02-10 | 2007-09-05 | Cellzome (UK) Ltd. | Amino pyrimidine compounds for the treatment of inflammatory disorders |
| WO2007090854A1 (en) | 2006-02-10 | 2007-08-16 | Cellzome (Uk) Ltd. | Azetidine amino pyrimidine compounds for the treatment of inflammatory disorders |
| GB0603550D0 (en) | 2006-02-22 | 2006-04-05 | Glaxo Group Ltd | Novel compounds |
| WO2007101158A2 (en) | 2006-02-24 | 2007-09-07 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| WO2007101161A2 (en) | 2006-02-24 | 2007-09-07 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| US8597562B2 (en) | 2006-03-30 | 2013-12-03 | GM Global Technology Operations LLC | Composite products and methods of making the same |
| PE20080176A1 (es) | 2006-03-31 | 2008-04-25 | Glaxo Group Ltd | Compuestos de arilpiperazina sulfonamida como agonista de los receptores de secretagogos de la hormona de crecimiento (ghs) |
| PL2007752T3 (pl) | 2006-03-31 | 2011-02-28 | Janssen Pharmaceutica Nv | Benzoimidazol-2-ilopirymidyny i pirazyny jako modulatory receptora histaminowego H4 |
| DE602007008859D1 (de) | 2006-03-31 | 2010-10-14 | Janssen Pharmaceutica Nv | Benzoimidazol-2-yl pyridine als modulatoren des histamin-h4-rezeptors |
| EP2010172B1 (en) | 2006-04-07 | 2012-08-29 | Janssen Pharmaceutica N.V. | Indoles and benzoimidazoles as modulators of the histamine h4 receptor |
| EP2007716A1 (en) | 2006-04-13 | 2008-12-31 | Glaxo Group Limited | Aryl and heteroaryl sulphonamides as growth hormone secretagogue receptor agonists |
| MX2009000110A (es) | 2006-06-28 | 2009-01-23 | Glaxo Group Ltd | Derivados de piperazinilo utiles en el tratamiento de enfermedades mediadas por el receptor grp38. |
| US8088733B2 (en) | 2006-07-06 | 2012-01-03 | Tranzyme Pharma Inc. | Methods of using macrocyclic agonists of the ghrelin receptor for treatment of gastrointestinal motility disorders |
| CL2007003874A1 (es) * | 2007-01-03 | 2008-05-16 | Boehringer Ingelheim Int | Compuestos derivados de benzamida; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar enfermedades cardiovasculares, hipertension, aterosclerosis, reestenosis, ictus, insuficiencia cardiaca, lesion isquemica, hipertensio |
| CN101657436A (zh) | 2007-02-09 | 2010-02-24 | 特兰齐姆制药公司 | 大环生长素释放肽受体调节剂及其使用方法 |
| ES2390195T3 (es) | 2007-08-27 | 2012-11-07 | Theravance, Inc. | Compuestos de amidoalquil-8-azabiciclo(3,2,1)octano, como antagonistas del receptor opioide mu |
| EP2195313B1 (en) | 2007-08-27 | 2014-04-02 | Theravance, Inc. | Heteroarylalkyl-8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists |
| ATE502939T1 (de) | 2007-08-27 | 2011-04-15 | Theravance Inc | Disubstituierte alkyl-8-azabicycloä3.2.1üoktan- verbindungen als mu-opioid-rezeptorantagonisten |
| TWI423801B (zh) | 2007-08-27 | 2014-01-21 | Theravance Inc | 作為μ類鴉片受體拮抗劑之8-氮雜雙環〔3.2.1〕辛基-2-羥基苯甲醯胺化合物 |
| US20110021538A1 (en) | 2008-04-02 | 2011-01-27 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
| US20110039860A1 (en) * | 2008-05-07 | 2011-02-17 | Cangming Yang | Soluble epoxide hydrolase inhibitors, compositions containing such compounds and methods of treatment |
| US20090298834A1 (en) * | 2008-06-02 | 2009-12-03 | Hassan Pajouhesh | 4-(aminomethyl)cyclohexanamine derivatives as calcium channel blockers |
| TW201010997A (en) * | 2008-06-18 | 2010-03-16 | Pfizer Ltd | Nicotinamide derivatives |
| US8273900B2 (en) * | 2008-08-07 | 2012-09-25 | Novartis Ag | Organic compounds |
-
2011
- 2011-01-31 JP JP2012551586A patent/JP5748777B2/ja not_active Expired - Fee Related
- 2011-01-31 ES ES11701824.2T patent/ES2527849T3/es active Active
- 2011-01-31 WO PCT/EP2011/051293 patent/WO2011095450A1/en not_active Ceased
- 2011-01-31 EP EP11701824.2A patent/EP2531490B1/en not_active Not-in-force
- 2011-01-31 CN CN201180007786.4A patent/CN102753527B/zh not_active Expired - Fee Related
- 2011-01-31 US US13/576,040 patent/US8835444B2/en not_active Expired - Fee Related
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