Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable H3 receptor antagonists and β-amyloid aggregation inhibitors for the treatment of Alzheimer’s disease
functional agents for therapy of Alzheimer’s disease, through introducing alkyloxy moiety into 4-pyridinone ring to avoid the possible phase II metabolism of 3-hydroxy-4-pyridinone in lead compound 3-hydroxy-2-methyl-1-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)-pyridin-4(1H)-one (4). In vitro studies indicated that most of these compounds exhibit excellent H3 receptor antagonistic activities and potent
SUBSTITUTED QUINONES OR ANALOGUES AS COLOURING AGENTS
申请人:MERCK PATENT GMBH
公开号:US20150315177A1
公开(公告)日:2015-11-05
The invention relates to protein-adhesive dyes, to the preparation thereof and to preparations comprising same, and to a method for colouring keratin-containing fibres, in particular for colouring human hair.
Thioxanthine derivatives and their use as inhibitors of MPO
申请人:AstraZeneca AB
公开号:US08026244B2
公开(公告)日:2011-09-27
There are disclosed novel compounds of Formula (I) wherein L, R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.
Thioxanthine Derivatives and Their Use as Inhibitors of MPO
申请人:Tiden Anna-Karin
公开号:US20090149475A1
公开(公告)日:2009-06-11
There are disclosed novel compounds of Formula (I) wherein L, R
1
, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.
FLAVOR COMPOSITION OR FRAGRANCE COMPOSITION, AND FLAVOR-IMPROVING AGENT
申请人:Takasago International Corporation
公开号:EP1944354A1
公开(公告)日:2008-07-16
The present invention relates to a flavor composition or fragrance composition which can satisfy diversified requirements for flavored products, as well as to a flavor-improving agent which can improve the quality and release of aroma of a beverage or food. More particularly, the present invention relates to a flavor composition or fragrance composition which comprises an optically active S-alkyl 2-methylbutanethioate as an active ingredient, a flavor- or fragrance-added product, a flavor-improving agent which comprises an optically active S-alkyl 2-methylbutanethioate as an active ingredient, and a beverage or food having an improved flavor. The optically active S-alkyl 2-methylbutanethioate includes S-alkyl (R)-2-methylbutanethioate and S-alkyl (S)-2-methylbutanethioate.