- NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF
-
An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl g roup, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R 3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R 4 and R 5 e ach independently represent a hydrogen atom; and R 2 and R 4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
- -
-
Paragraph 1173; 1174
(2018/09/08)
-
- NOVEL NICOTINAMIDE DERIVATIVE OR SALT THEREOF
-
The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein R1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R3, R4, R5, n, and X1 have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.
- -
-
Paragraph 0868; 0869; 0870; 0871
(2014/10/29)
-
- Phosphoinositide-3-kinase inhibitors: Evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511
-
Replacement of the piperazine sulfonamide portion of the PI3Kα inhibitor AMG 511 (1) with a range of aliphatic alcohols led to the identification of a truncated gem-dimethylbenzylic alcohol analog, 2-(5-(4-amino-6-methyl-1,3,5-triazin-2-yl)-6-((5-fluoro-6-methoxypyridin-3-yl)amino)pyridin-3-yl)propan-2-ol (7). This compound possessed good in vitro efficacy and pharmacokinetic parameters and demonstrated an EC50 of 239 ng/mL in a mouse liver pharmacodynamic model measuring the inhibition of hepatocyte growth factor (HGF)-induced Akt Ser473 phosphorylation in CD1 nude mice 6 h post-oral dosing.
- Lanman, Brian A.,Reed, Anthony B.,Cee, Victor J.,Hong, Fang-Tsao,Pettus, Liping H.,Wurz, Ryan P.,Andrews, Kristin L.,Jiang, Jian,McCarter, John D.,Mullady, Erin L.,San Miguel, Tisha,Subramanian, Raju,Wang, Ling,Whittington, Douglas A.,Wu, Tian,Zalameda, Leeanne,Zhang, Nancy,Tasker, Andrew S.,Hughes, Paul E.,Norman, Mark H.
-
supporting information
p. 5630 - 5634
(2015/01/08)
-
- 2-AMINOINDOLE COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA
-
The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)- The values and preferred values of the variables in Structural Formula I are defined herein.
- -
-
Page/Page column 93-94
(2011/05/11)
-
- Heteroaryl spiroethercycloalkyl tachykinin receptor antagonists
-
The present invention is directed to certain novel compounds represented by structural formula I: STR1 or a pharmaceutically acceptable salt thereof, wherein R 3, R 6, R 7, R 8, R 11, R 12, R 13, A, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
- -
-
-