- Novel benzoylpiperidine-based stearoyl-CoA desaturase-1 inhibitors: Identification of 6-[4-(2-methylbenzoyl)piperidin-1-yl]pyridazine-3-carboxylic acid (2-hydroxy-2-pyridin-3-ylethyl)amide and its plasma triglyceride-lowering effects in Zucker fatty rats
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Starting from a known piperazine-based SCD-1 inhibitor, we obtained more potent benzoylpiperidine analogs. Optimization of the structure of the benzoylpiperidine-based SCD-1 inhibitors resulted in the identification of 6-[4-(2-methylbenzoyl)piperidin-1-yl]pyridazine-3-carboxylic acid (2-hydroxy-2-pyridin-3-yl-ethyl)amide (24) which showed strong inhibitory activity against both human and murine SCD-1. In addition, this compound exhibited good oral bioavailability and demonstrated plasma triglyceride lowering effects in Zucker fatty rats in a dose-dependent manner after a 7-day oral administration (qd).
- Uto, Yoshikazu,Ogata, Tsuneaki,Kiyotsuka, Yohei,Ueno, Yuko,Miyazawa, Yuriko,Kurata, Hitoshi,Deguchi, Tsuneo,Watanabe, Nobuaki,Konishi, Masahiro,Okuyama, Ryo,Kurikawa, Nobuya,Takagi, Toshiyuki,Wakimoto, Satoko,Ohsumi, Jun
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scheme or table
p. 341 - 345
(2010/04/05)
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- 7-fused 2-(piperazinoalkyl) indole derivatives, intermediates and compositions thereof
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Pharmacologically active compounds having anti-allergic properties corresponding to the formula I STR1 which can be mono- or disubstituted in the phenyl ring and their acid addition salts and/or S-mono- or dioxides of sulfur-containing compounds of the formula I are described, together with processes and intermediates for their preparation.
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- Pyrroloazepine derivatives
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Disclosed herein are pyrroloazepine derivatives, which are useful as therapeutics for circulatory diseases, represented by the following formula (I): STR1 wherein R means a hydrogen atom, a linear or branched C1-6 alkyl group or a C7-10 aralkyl group, A denotes a linear or branched C2-10 alkylene, alkenylene or alkynylene group, Z stands for O, NOR1 or NOCOR5 in which R1 and R5 is a hydrogen atom or an alkyl, aryl or aralkyl group, and Y means a particular piperidinyl or pyrrolidinyl group; and salts thereof. Their preparation processes are also disclosed.
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- 1,5-Disubstituted-1,2-dihydro-2H-1,4-benzodiazepin-2-ones
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1,5-Disubstituted-1,2-dihydro-2H-1,4-benzodiazepin-2-ones of the formula STR1 wherein R is hydrogen or fluoro, R1 is hydrogen, fluoro chloro, bromo or trifluoromethyl, and n is 2 to 4, having anticonvulsant activity and useful as anti-anxiety agents, are disclosed.
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- Benzoylpiperidylalkylindoles
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New benzoylpiperidylalkylindoles and related compounds possessing tranquilizing, anti-hypertensive and analgesic properties and a process for the preparation thereof are described.
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