- PHARMACEUTICAL COMPOSITION FOR TREATING DIABETES
-
Provided is a compound represented by the following general formula (I), or a pharmaceutically acceptable salt thereof. This novel compound has a glycogen-synthase activation ability, but activates a receptor PPAR to a low degree and is highly safe. In th
- -
-
Paragraph 0051
(2014/09/29)
-
- 4-AMINOETHOXY INDOLONE DERIVATIVES
-
A compound of formula (I) in which Y is hydrogen, halogen or lower alkoxy; R1 is hydrogen, lower alkyl or aryl(lower)alkyl; R2 is hydrogen, lower alkyl or -(CH2)nXpAr, where X is oxygen or carbonyl; Ar is cycloalkyl, aryl or arylaryl, oxindolyl, benzimidazolyl, indolyl, 2-oxobenzimidazolyl or 2-thioxobenzimidazolyl; or R1 and R2, taken together with the nitrogen atom to which they are attached, complete a 3,4-dihydro-1H-isoquinolinyl or 1,3-dihydro-isoindolyl; n is one of the integers 1,2,3,4,5 or 6; p is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs.
- -
-
-
- A practical approach to highly functionalized benzodihydrofurans
-
A number of aromatic dibromides have been treated with 2-3 equivalents of n-butyllithium in order to initiate two sequential chemical events, a Parham cyclization and an intermolecular reaction with DMF. (C) 2000 Elsevier Science Ltd.
- Plotkin, Michael,Chen, Sanyou,Spoors, P. Grant
-
p. 2269 - 2273
(2007/10/03)
-
- New generation dopaminergic agents. 6. Structure-activity relationship studies of a series of 4-(aminoethoxy)indole and 4-(aminoethoxy)indolone derivatives based on the newly discovered 3-hydroxyphenoxyethylamine D2 template
-
A series of 4-(aminoethoxy)indoles 7 and a related series of 4- (aminoethoxy)indolones 8 were synthesized and evaluated for their affinity for both the high- and low-affinity agonist states (D2(High) and D2(Low), respectively) of the dopamine (DA) D2 receptor. The 4-aminoethoxy derivatives (i.e., 7 and 8) were designed as bioisosteric analogues based on the phenol prototype 4. The indolones 8 were observed to have high affinity for the D2(High) receptor. Comparison of their previously reported chroman analogues with the more flexible 4-(aminoethoxy)indoles revealed the chroman analogues to be more potent, whereas little loss in D2(High) affinity was observed when comparing the 4-(aminoethoxy)indolones with their respective chroman analogues. Several regions of the phenoxyethylamine framework were modified and recognized as potential sites to modulate the level of intrinsic activity. A conformational analysis was performed and a putative bioactive conformation was proposed which fulfilled the D2 agonist pharmacophore criteria based on the McDermed model. Structure-activity relationships gained from these studies have aided in the synthesis of D2 partial agonists of varying intrinsic activity levels. These agents should be of therapeutic value in treating disorders resulting from hypo- and hyperdopaminergic activity, without the side effects associated with complete D2 agonism or antagonism.
- Mewshaw, Richard E.,Webb, Michael B.,Marquis, Karen L.,McGaughey, Georgia B.,Shi, Xiaojie,Wasik, Theodore,Scerni, Rosemary,Brennan, Julie A.,Andree, Terrance H.
-
p. 2007 - 2020
(2007/10/03)
-
- 4-AMINOETHOXY INDOLONE DERIVATIVES
-
A compound of the formula I: STR1 in which Y is hydrogen, halogen or lower alkoxy; R 1 is hydrogen, lower alkyl or aryl(lower) alkyl; R. sub.2 is hydrogen, lower alkyl or--(CH 2) n X p Ar, where X is oxygen or carbonyl; Ar is cycloalkyl, aryl or arylaryl, oxindolyl, benzimidazolyl, indolyl, 2-oxobenzimidazolyl or 2-thioxobenzimidazolyl; or R 1 and R 2, taken together with the nitrogen atom to which they are attached, complete a 3,4-dihydro-1H-isoquinolinyl or 1,3-dihydro-isoindolyl; n is one of the integers 1,2,3, 4,5 or 6; p is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analogous drugs.
- -
-
-
- New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates
-
Described in this report is a systematic study which led to the identification of two new dopamine D2 partial agonists (5 and 17). Phenols 5 and 17 represent prototypes of two new classes of D2 partial agonist as well as templates for the future design of novel dopaminergic agents.
- Mewshaw, Richard E.,Husbands, Morris,Gildersleeve, Elizabeth S.,Webb, Michael B.,Shi, Xiaojie,Mazandarani, Hossein,Cockett, Mark I.,Ochalski, Rafal,Brennan, Julie A.,Abou-Gharbia, Magid,Marquis, Karen,McGaughey, Georgia B.,Coupet, Joseph,Andree, Terrance H.
-
p. 295 - 300
(2007/10/03)
-