167262-68-2Relevant articles and documents
Structural optimization elaborates novel potent Akt inhibitors with promising anticancer activity
Liu, Yang,Yin, Yanzhen,Zhang, Zhen,Li, Carrie J.,Zhang, Hui,Zhang, Daoguang,Jiang, Changying,Nomie, Krystle,Zhang, Liang,Wang, Michael L.,Zhao, Guisen
, p. 543 - 551 (2017/07/12)
Targeting of Akt has been validated as a well rationalized approach to cancer treatment, and represents a promising therapeutic strategy for aggressive hematologic malignancies. We describe herein an exploration of novel Akt inhibitors for cancer therapy through structural optimization of previously described 4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives. Our studies yielded a novel series of pyrrolopyrimidine based phenylpiperidine carboxamides capable of potent inhibition of Akt1. Notably, 10h exhibited robust antiproliferative effects in both mantle cell lymphoma cell lines and primary patient tumor cells. Low micromolar doses of 10h induced cell apoptosis and cell cycle arrest in G2/M phase, and significantly downregulated the phosphorylation of Akt downstream effectors GSK3β and S6 in Jeko-1 cells.
A nitrogen-containing heterocyclic phenyl piperidine compound and its preparation method and application
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, (2017/09/01)
The invention discloses a nitrogen-containing heterocyclic phenyl piperidine compound or pharmaceutical salt thereof. The general structural formula a of the compound is as shown in specification, wherein R represents hydrogen, mono-substituted or poly-substituted halogen, methyl, methoxyl, tertiary butyl or trifluoromethyl; and R2 is hydrogen, chlorine, bromine, methyl or ethyl. The compound disclosed by the invention is novel in structure; and by introducing the active amino in the form of a piperidine ring, the configuration of the side-chain amino is reinforced and the rigidity of the compound is enhanced. Through the design transformation, the Akt1 kinase inhibitory activity and the PC-3 cell line growth inhibitory activity of the compound are significantly enhanced.
KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
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Page/Page column 183, (2011/10/31)
The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are a pharmaceutical composition and method of use thereof.
Collection of traceable compounds and uses thereof
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, (2010/07/06)
The use of a collection of compounds of general formula (I), wherein: n is 0 or 1; p represents an integer between 1 and 6; r represents an integer between 1 and 12; R1 and R′1 represent in particular a hydrogen atom; R2 represents an amino acid side chain or an amino acid derivative; R3 represents a group derived from a carboxylic acid, bearing a basic entity; R4 represents in particular an alkyl group containing 1 to 10 carbon atoms; and A represents a hydrogen atom, a protecting group or a tracing group, in particular a fluorophor, a coloring agent or a quencher, for determining, through binding studies, ligands of receptors whose ligand is unknown or whose ligand useful for carrying out specific affinity binding assays is unknown.
Substituted Heterocyclic Ethers and Their Use in CNS Disorders
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Page/Page column 40, (2009/01/24)
The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.
Dual NK2/NK3-antagonists, pharmaceutical compositions comprising them, and processes for their preparation
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Page/Page column 23-24, (2010/11/28)
Dual NK2/NK3-antagonists corresponding to formula I: and physiologically compatible salts of such compounds in which X and R1 to R5 have specific defined meanings, pharmaceutical compositions containing such compounds, methods of using such compounds to treat or inhibit disorders mediated by tachykinin receptors, and a process for preparing such compounds.
NOVEL DUAL NK2/NK3-ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND PROCESSES FOR THEIR PREPARATIONS
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Page/Page column 59, (2010/11/28)
The present invention relates to novel dual NK2/NK3-antagonists of formula (I) wherein the meaning of X and R1 to R5 is defined in the claims and in the description and also to pharmaceutical compositions comprising these compounds. Furthermore, the invention relates to processes for the preparation of the novel dual NK2/NK3-antagonists and to their uses.
NK-1 AND SEROTONIN TRANSPORTER INHIBITORS
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Page/Page column 56, (2010/11/28)
The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.
PYRAZOLONE COMPOUNDS AS METABOTROPIC GLUTAMATE RECEPTOR AGONISTS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
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Page/Page column 244, (2008/06/13)
Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, X, and n are as defined for Formula (I) in the description, processes for the preparation of the compounds and new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and the use of the compounds in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction.
Synthesis of functionalized nitrogen heterocycles by radical decarboxylation of β- and γ-amino acids
Boto, Alicia,Hernandez, Rosendo,De Leon, Yolanda,Murguia, Jose R.,Rodriguez-Afonso, Abigail
, p. 673 - 682 (2007/10/03)
Iodinated or oxygenated nitrogen heterocycles are obtained by radical decarboxylation of β- and γ-amino acids. This mild, versatile reaction is applied to the synthesis of bioactive products, such as 4-arylpiperidines, hydroxylated piperidines, and new antifungal agents.