- HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
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Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and tr
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Page/Page column 21
(2011/07/06)
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- Conversion of systemically-distributed triazole-based stearoyl-CoA desaturase (SCD) uHTS hits into liver-targeted SCD inhibitors
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It has been demonstrated that once-a-day dosing of systemically-distributed SCD inhibitors leads to adverse events in eye and skin. Herein, we describe our efforts to convert a novel class of systemically-distributed potent triazole-based uHTS hits into liver-targeted SCD inhibitors as a means to circumvent chronic toxicity.
- Leclerc, Jean-Philippe,Falgueyret, Jean-Pierre,Girardin, Mélina,Guay, Jocelyne,Guiral, Sébastien,Huang, Zheng,Li, Chun Sing,Oballa, Renata,Ramtohul, Yeeman K.,Skorey, Kathryn,Tawa, Paul,Wang, Hao,Zhang, Lei
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scheme or table
p. 6505 - 6509
(2011/12/04)
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- HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
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Heteroaromatic compounds of structural formula (I) are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and met
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Page/Page column 40-41
(2010/04/27)
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- PIPERIDIN-2-ONE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THESE COMPOUNDS AS THE ACTIVE INGREDIENT
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A piperidin-2-one derivative compound represented by formula (I): wherein all symbols are described in the specification, or a non-toxic salt thereof. The compound represented by formula (I) inhibits activation of p38MAP kinase, and is useful for preventi
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- An Efficient Synthesis of Chloroethylclonidine
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An efficient pathway for the preparation of chloroethylclonidine dihydrochloride (1) is described.
- Zhang, Wei-Yi,Bakthavachalam, Venkatesalu,Gao, Yigong,White, William L.,Neumeyer, John L.
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- Pharmacologically active CNS compound
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The invention provides a series of compounds of formula (I) and salts thereof, wherein for example,R1 and R2, which may be the same or different each represent -NR13R14 where R13 and R14 may each independently represent hydrogen or alkyl or, taken together with the nitrogen atom to which they are attached form a heterocyclic ring, optionally substituted by one or more alkyl or arylalkyl groups and optionally containing a further heteroatom;, R3 is hydrogen, haloalkyl, alkoxymethyl or alkyl;, R4 is hydrogen, nitro or halo;, R5 is hydrogen or halo;, R6 is hydrogen, halo, nitro, amino, alkylamino or dialkylamino;, R7 is hydrogen or halo;, R8 is hydrogen or halo; The compounds may be used for the treatment or prophylaxis of a neurodegenerative or other neurological disorder of the CNS, the aetiology or which includes excessive release of the neurotransmitter glutamate.
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- USE OF 2-[(3,5-DIHALO-4-AMINOBENZYL)] IMIDAZOLINES TO STIMULATE ALPHA-1 ADRENERGIC RECEPTORS AND TO TREAT NASAL CONGESTION
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Disclosed herein are alpha adrenergic and nasal decongestant compounds of the formula STR1 wherein R 1 and R 2, each being the same or different, are halogens, and the pharmaceutically acceptable salts thereof.
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