482578-63-2Relevant academic research and scientific papers
IMPROVED METHODS, KITS, COMPOSITIONS AND DOSING REGIMENS FOR THE USE OF HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2
-
Page/Page column 119-120, (2021/05/07)
The present application provides improved compositions, methods, kits and dosing regimens for the use of heterocyclic compounds and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, or stereoisomers thereof. These compositions, methods, kit
HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER
-
Paragraph 0513-0514, (2017/01/02)
The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a
Isosteric analogs of lenalidomide and pomalidomide: Synthesis and biological activity
Ruchelman, Alexander L.,Man, Hon-Wah,Zhang, Weihong,Chen, Roger,Capone, Lori,Kang, Jian,Parton, Anastasia,Corral, Laura,Schafer, Peter H.,Babusis, Darius,Moghaddam, Mehran F.,Tang, Yang,Shirley, Michael A.,Muller, George W.
, p. 360 - 365 (2013/02/23)
A series of analogs of the immunomodulary drugs lenalidomide (1) and pomalidomide (2), in which the amino group is replaced with various isosteres, was prepared and assayed for immunomodulatory activity and activity against cancer cell lines. The 4-methyl and 4-chloro analogs 4 and 15, respectively, displayed potent inhibition of tumor necrosis factor-α (TNF-α) in LPS-stimulated hPBMC, potent stimulation of IL-2 in a human T cell co-stimulation assay, and anti-proliferative activity against the Namalwa lymphoma cell line. Both of these analogs displayed oral bioavailability in rat.
Substituted Spiro-amide Compounds
-
Page/Page column 91, (2010/10/19)
Substituted spiro-amide compounds corresponding to formula I in which R5 through R8, D, X, Y and Z have defined meanings, processes for preparing such spiro-amide compounds, pharmaceutical compositions containing such compounds, and methods of using such spiro-amide compounds for treating and/or inhibiting disorders or disease states mediated at least in part by the bradykinin 1 receptor.
NOVEL HYDRAZIDE CONTAINING TYROSINE KINASE INHIBITORS
-
Page/Page column 37, (2009/10/22)
The present invention relates to compounds of formula (I), and salts thereof, wherein P represents a 5 or 6-membered heteroaryl ring; R1 is aryl or unsaturated heterocyclyl radical optionally substituted by one or more identical or different radicals R5.
Novel compounds useful for bradykinin B1 receptor antagonism
-
Page/Page column 32, (2010/11/25)
Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor.
PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDK' S AND GSK' S
-
Page/Page column 150, (2008/06/13)
The invention provides compounds of the formula (I), or salts, tautomers, N-oxides or solvates thereof wherein: R1 is selected from: (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents for the phenyl group are selected from fluorine, chlorine, methyl and methoxy; (d) a group R0; (e) a group R a; (f) a group Rlb; (g) a group Rlc; (h) a group Rld; and 0) 2,6-difluorophenylamino ; wherein R )0υ, r R> llaa, T Rj I1bD, T R) I1cC, r R> Iidα, r R?2zaa, r R>22bD and RJ are as defined in the claims. The compounds have activity as inhibitors of cdk kinase (such as cdkl or cdk2) and glycogen synthase kinase-3 activity.
COMPOUNDS HAVING ACTIVITY AT 5HT2C RECEPTOR AND USES THEREOF
-
Page 26; 27, (2010/02/09)
Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 is halogen, cyano, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy, C1 6alkylthio, hydroxy, amino, mono or di C1 6alkylamino, an N-linked 4 to 7 memb
DIBENZOCYCLOHEPTENE COMPOUND
-
Page 115, (2010/11/30)
The present invention discloses a dibenzocycloheptene compound represented by the formula (I): ???wherein R1: hydrogen atom, halogen atom, etc., R2: hydrogen atom, halogen atom, etc., A: 5-membered or 6-membered heteroaromatic ring group containing 1 to 3 hetero atom(s) selected from the group consisting of nitrogen atom, oxygen atom and sulfur atom, and the heteroaromatic ring group, etc. may have halogen atom, nitrogen atom, etc. as substituent(s), B: formula; -CH=CH-, formula; -CH2O-, etc., Y: C1-C10 alkylene group which may have halogen atom, etc. as substituent(s), etc., Z: carboxyl group which may be protected, etc., m: an integer of 1 to 4, n: an integer of 1 to 3, ???------ represents a single bond or a double bond, or a pharmaceutically acceptable salt thereof and a medical composition containing the same as an effective ingredient which has leukotriene C4 antagonistic action and leukotriene E4 antagonistic action in addition to potent leukotriene D4 antagonistic action, and useful as antiasthmatic agent, antiallergic agent and anti-inflammatory agent.
