- Design, synthesis and biological evaluation of 4-(1- (4(sulphanilamide) phenyl)-3-(methyl)-1H-pyrazol-5-yl)dine urea and N-acyl derivatives as a soluble epoxide hydrolase inhibitors
-
A series of novel sEH inhibitors containing a N-substituted piperidine ring [N-urea (8a-i ) (9a-l) and amide derivatives (6a-l) (7a-l )] with pyrazole (a five-membered polar heterocycle) as a pharmacophore lead for sEH inhibition have been designed, synth
- Nimbarte, Vijaykumar D.,Murtuza, Hadianawala,Phaniraj, Sahishna,Shrivastava, Shweta,Naidu,Satheesh Kumar,Atcha, Krishnam Raju
-
p. 2178 - 2197
(2014/05/06)
-
- Quinoline derivatives as neurokinin receptor antagonists
-
The present invention relates to substituted quinoline hydrazides of Formula (I): wherein R1, R2, R3, R4, R5, X, Y and Z are defined herein, pharmaceutical compositions comprising them and their use in treating diseases mediated by neurokinin-2 and/or neurokinin-3 (NK-3) receptors. These compounds can thus be used in methods of treatment to suppress and treat such disorders.
- -
-
Page/Page column 34-35
(2009/04/24)
-
- SUBSTITUTED CYCLOHEXYL DERIVATIVES AS NK-3 RECEPTOR ANTAGONISTS
-
The present invention relates to the compounds of formula (I): wherein A,B, n, X, Y, Z, R1, R2, R3, R4, R5, R6, R7 and R8 are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them and their use in treating diseases mediated by neurokinin-3 (NK-3) receptors. These compounds can thus be used in methods of treatment to suppress and treat such disorders.
- -
-
Page/Page column 30-31
(2010/11/25)
-
- Regioselective synthesis of 4-(2-alkyl-5-methyl-2H-pyrazol-3-yl)- piperidines
-
The regioselective, scaleable synthesis of three 4-(2-alkyl-5-methyl-2H- pyrazol-3-yl)-piperidines is discussed.
- Dirat, Olivier,Clipson, Alex,Elliott, Jason M.,Garrett, Sasha,Brian Jones,Reader, Michael,Shaw, Duncan
-
p. 1729 - 1731
(2007/10/03)
-
- N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
-
The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.
- -
-
Page/Page column 34
(2010/11/30)
-