The synthesis and some reactions OF 3-(2-aminophenyl)-2-iminothiazolidines. ring closure of -(2-thiocyanaoethyl,)-phenylenediamines; thiazolidine . 3,1,6-benzothiadiazocine formation
When treated with strong acids, the N-(2-thiocyanatoethyl)-o-phenylenediamines (1g-1v) are cyclized exclusively to 3-(2-aninophen- yl)-2-iminothiazolidines (6) while the related tertiary amines (1a-1f) gave, under the same conditions, benzothiadiazocines of types (2) or (3). Some of the type (6) compounds are highly active antidepressants of low toxicity. Thermal reactions of compound (6b) and its
HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
申请人:Chytil Milan
公开号:US20100204214A1
公开(公告)日:2010-08-12
Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
Histamine H3 Inverse Agonists and Antagonists and Methods of Use Thereof
申请人:Chytil Milan
公开号:US20110065694A1
公开(公告)日:2011-03-17
Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
TETRAHYDRO-AZACARBOLINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USES THEREOF
申请人:SURMAN Matthew D.
公开号:US20120157460A1
公开(公告)日:2012-06-21
The present invention relates to tetrahydro-azacarboline derivatives of formula (I):
having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.
Use of quaternary polysiloxanes in cleaning and care compositions
申请人:Meder Markus
公开号:US20070041930A1
公开(公告)日:2007-02-22
The invention relates to the use of polysiloxanes which comprise a plurality of quaternary ammonium groups in the molecule in cosmetic or pharmaceutical compositions for the cleaning and care of keratin fibers, in particular of human hair. The improvement in the shine and in the color protection of the hair is achieved if the polysiloxanes are used in an amount in the range from 0.01 to 30%.