308362-93-8Relevant academic research and scientific papers
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Part 2
Sasmal, Sanjita,Balasubrahmanyam,Kanna Reddy, Hariprasada R.,Balaji, Gade,Srinivas, Gujjary,Cheera, Srisailam,Abbineni, Chandrasekhar,Sasmal, Pradip K.,Khanna, Ish,Sebastian,Jadhav, Vikram P.,Singh, Manvendra P.,Talwar, Rashmi,Suresh,Shashikumar, Dhanya,Harinder Reddy,Sihorkar,Frimurer, Thomas M.,Rist, ?ystein,Elster, Lisbeth,H?gberg, Thomas
, p. 3163 - 3167 (2012/06/04)
Melanin concentrating hormone receptor 1 (MCHR1) antagonists have potential for the treatment of obesity and several CNS disorders. In the preceding article, we have described a novel series of quinazolines as MCHR1 antagonists and demonstrated in vivo proof of principle with an early lead. Herein we describe the detailed SAR and SPR studies to identify an optimized lead candidate having good efficacy in a sub-chronic DIO model with a good cardiovascular safety window.
SUBSTITUTED OXIMES AND HYDRAZONES AS NEUROKININ ANTAGONISTS
-
Page 37; 38, (2010/02/08)
Compound represented by structural formula (I) or a pharmaceutical acceptable salt thereof, wherein a is 0-3; b, d and e are 0-2; R is H, alkyl, F or -OR; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, -C(O)-, -O-, -NR-, -S(O)e-, -N(R)C(O)-, -C(O)N(R)-, -OC(O)NR-, -OC(=S)NR-, -N(R)C(=S)O-, -S(O)2N(R)-, -N(R)S(O)2-, -N(R)C(O)O-, -OC(O)- or -N(R)C(O)NR-; or d is 0 and X is a bond or -NR-; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, napthyl or heteroaryl; R is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R is R or -OR, R, R, R and R are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g., piperidinyl, substituted by a heterocyclo- or heterocycloalkyl group; wherein phenyl, benzyl, aryl, heterocycloalkyl, heteroaryl and cycloalkyl groups are optionally substituted; methods of treating diseases such as asthma, cough, bronchospasm, depression, emesis, inflammatory diseases, and gastrointestinal disorders with said compounds, and pharmaceutical compositions comprising said compounds are disclosed.
