- Discovery of potent selective orally active benzoxazepine-based orexin-2 receptor antagonists
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During our efforts to identify a series of potent, selective, orally active human Orexin-2 Receptor (OX2R) antagonists, we elucidated structure-activity relationship (SAR) on the 7-position of a benzoxazepine scaffold by utilizing Hammett rp and Hansch-Fu
- Fujimoto, Tatsuhiko,Kunitomo, Jun,Tomata, Yoshihide,Marui, Shogo,Nishiyama, Keiji,Nakashima, Masato,Yoshikubo, Shin-Ichi,Hirai, Keisuke,Hirozane, Mariko
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p. 6414 - 6416
(2011/11/29)
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- Spiro-benzopyran derivatives and useful for treating asthma and hypertension
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The present invention relates to novel benzopyran derivatives of formula(I) which have exellent effectiveness in the treatment of asthma as well as hypertension. STR1 wherein R1 is --CN, --NO2, --OCX1 X2 X3, --NH2, --NHSO2 RA, STR2 --SO2 RC or --SO2 NRC RD wherein X1, X2 and X3 are, each independently, F, Cl or H, except for that X1, X2 and X3 may not be hydrogen atom simulaneously; RA and RB are, each independently, a hydrogen atom, or a C1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C1-3 alkyl group; and RC and RD are, each independently, a hydrogen atom or a C1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C1-3 alkyl group; R2 is a C1-4 straight or branched alkyl group; R3 is a C1-4 straight or branched alkyl group, STR3 wherein RG and RH are, each independently, a C1-6 alkyl group or optionally substituted phenyl group with a halogen atom, or a straight or branched C1-3 alkyl group, A and B are, each independently, S or O; and Z is a C1-3 straight or branched alkyl group; X is N or N→O.
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- Benzopyran derivatives and processes for the preparation thereof
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The present invention relates to novel benzopyran derivatives of formula (I) which have superior selectivity in the treatment of hypertension by lowering blood pressure with a relaxation activity on vascular smooth muscle. The present invention also relat
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- Novel benzopyran derivatives and processes for the preparation thereof
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The present invention relates to novel benzopyran derivatives of formula(I) which have superior selectivity in the treatment of hypertension by lowering blood pressure with a relaxation activity on vascular smooth muscle. The present invention also relate
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- Novel benzopyran derivatives and processes for the preparation thereof
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The present invention relates to novel benzopyran derivatives of formula(I) which have exellent effectiveness in the treatment of asthma as well as hypertension. The present invention also relates to processes for preparing such compounds and to pharmaceutical compositions containing such compounds as an effective ingredient: wherein: R1 is-CN, -NO2, -OCX1X2X3, -NH2, -NHSO2RA, -SO2RCor -SO2NRCRDwherein X1, X2 and X3 are, each independently, F, Cl or H, except for that X1, X2 and X3 may not be hydrogen atom simulaneously; RAand RBare, each independently, a hydrogen atom, or a C1 6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C1 3 alkyl group; and RCand RDare, each independently, a hydrogen atom or a C1 6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C1 3 alkyl group; R2 isa C1 4 straight or branched alkyl group; R3 isa C1 4 straight or branched alkyl group, wherein RGand RHare, each independently, a C1 6 alkyl group or optionally substituted phenyl group with a halogen atom, or a straight or branched C1 3 alkyl group, A and B are, each independently, S or O; and Z is a C1 3 straight or branched alkyl group; X isN or N → O, provided, however, when X is in 2-position, R3 is and Y isa hydrogen or halogen atom, or an amino, hydroxy, a lower alkoxy or lower alkyl group.
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