21297-82-5Relevant academic research and scientific papers
Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification
Clark, Robin D.,Jahangir, Alam,Alam, Muzaffar,Rocha, Cynthia,Lin, Lin,Bjorner, Bodil,Nguyen, Khanh,Grady, Carole,Williams, Timothy J.,Stepan, George,Tang, Hai Ming,Ford, Anthony P.D.W.
, p. 1697 - 1700 (2005)
Replacement of the N-butyl side-chain of lead 5-HT4 receptor antagonist 2 with propanesulfonylpiperidinyl, morpholinyl, and piperazinyl groups led to higher affinity analogs 4-6. In vitro drug metabolism screens and cassette pharmacokinetic studies in the dog led to identification of the N-methylpiperazinyl analog (6b), which displayed pharmacokinetic, selectivity, and safety parameters sufficient for advancement to the clinic for the treatment of urinary incontinence.
AMINO - PYRIMIDINE COMPOUNDS AS INHIBITORS OF TBK1 AND/OR IKK EPSILON
-
Page/Page column 103, (2011/05/05)
The invention relates to certain aminopyrimidine compounds which inhibit TBK1 and/or IKK epsilon and which may therefore find application in treating inflammation, cancer, septic shock and/or Primary open Angle Glaucoma (POAG).
COMPOUNDS AND THERAPEUTIC USES THEREOF
-
Page/Page column 152, (2010/11/03)
The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.
DERIVATIVES OF SUBSTITUTED FUSED RING CYCLOINDOLES AND METHODS OF THEIR USE
-
Page/Page column 73, (2009/10/09)
Disclosed herein are derivatives of substituted fused ring cycloindole useful, inter alia, in combating Hepatitis C infection and entry into cells.
Synthetic studies on condensed-azole derivatives. II. Application of a computer-assisted automated synthesis apparatus for the synthesis of N- substituted sulfamoylpropylthioimidazo[1,2-b]pyridazines
Kuwahara,Kato,Sugawara,Miyake
, p. 1511 - 1515 (2007/10/03)
For the purpose of improving the anti-asthmatic activity of 3- (imidazo[1,2-b]pyridazin-6-yl)thiopropanesulfonamide (I), the computer- assisted automated synthesis apparatus developed at Takeda was used to modify the sulfonamide moiety of I. Several kinds
