289677-11-8Relevant academic research and scientific papers
PHARMACEUTICAL COMPOUNDS
-
Page/Page column 77, (2018/02/28)
The present invention relates to compounds of Formula (I) that are useful as inhibitors of the activity of the ubiquitin specific protease USP19. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in therapy.
NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN TREATING METABOLIC DISORDERS
-
Page/Page column 49, (2011/12/14)
The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.
4-Amino-2-alkyl-butyramides as small molecule CCR2 antagonists with favorable pharmacokinetic properties
Butora, Gabor,Morriello, Gregori J.,Kothandaraman, Shankaran,Guiadeen, Deodialsingh,Pasternak, Alexander,Parsons, William H.,MacCoss, Malcolm,Vicario, Pasquale P.,Cascieri, Margaret A.,Yang, Lihu
, p. 4715 - 4722 (2007/10/03)
A systematic examination of the central aromatic portion of the lead (2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-(4-fluorophenyl)-4-(1′H-spiro[indene-1,4′-piperidin]-1′-yl)butanamide (9) led to the discovery of a novel class of CCR2 receptor antagonists, which carry small alicyclic groups such as cyclopropyl, cylobutyl, or cyclopropylmethyl attached at C2 of the carbon backbone. The most potent compound discovered, namely (2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-cyclopropyl-4-[(1R,3′R)-3′-methyl-1′H-spiro[indene-1,4′-piperidin]-1′-yl]butanamide (29), showed very high binding affinity (IC50 = 4 nM, human monocyte) and excellent selectivity toward other related chemokine receptors. The excellent pharmacokinetic profile of this new lead compound allows for extensive in vivo evaluation.
Novel small renin inhibitors containing 4,5- or 3,5-Dihydroxy-2-substituted-6-phenylhexanamide replacements at the P2-P3 sites
Jung, Grace L.,Anderson, Paul C.,Bailey, Murray,Baillet, Monique,Bantle, Gary W.,Berthiaume, Sylvie,Lavallee, Pierre,Llinas-Brunet, Montse,Thavonekham, Bounkham,Thibeault, Diane,Simoneau, Bruno
, p. 2317 - 2336 (2007/10/03)
Renin inhibitors containing a 4,5- or a 3,5-dihydroxy-2-substituted-6-phenylhexanamide fragment at the P2-P3 sites have been prepared and evaluated. The four possible diastereomeric diols of the two series of inhibitors were synthesi
RENIN INHIBITING POLYHYDROXY-MONOAMIDES
-
, (2008/06/13)
Disclosed herein are compounds of the formula:R 1 CH 2 CH(X)CH(Y)CH(Z)CHR 2 C(O)NHCHR 3 CH(OH) CH(OH)R 4wherein R 1 is a terminal unit, for example lower cycloalkyl or phenyl; R 2 is, for example, an optionally substituted alkyl, cycloalkylme
