HORNYAK, GY.;BERTHA, F.;ZAUER, K.;LEMPERT, K.;FELLER, A.;PJECZKA, E., TETRAHEDRON, 46,(1990) N, C. 2009-2030
作者:HORNYAK, GY.、BERTHA, F.、ZAUER, K.、LEMPERT, K.、FELLER, A.、PJECZKA, E.
DOI:——
日期:——
[EN] TETRAHYDRO-AZACARBOLINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USES THEREOF<br/>[FR] ANTAGONISTES DE LA MCH-1 À BASE DE TÉTRAHYDRO-AZACARBOLINE, LEURS PROCÉDÉS DE FABRICATION ET LEURS UTILISATIONS
申请人:ALBANY MOLECULAR RES INC
公开号:WO2012088124A2
公开(公告)日:2012-06-28
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.
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