89937-77-9Relevant academic research and scientific papers
Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs
Xu, Mingshuo,Wang, Yu,Yang, Feipu,Wu, Chunhui,Wang, Zhen,Ye, Bin,Jiang, Xiangrui,Zhao, Qingjie,Li, Jianfeng,Liu, Yongjian,Zhang, Junchi,Tian, Guanghui,He, Yang,Shen, Jingshan,Jiang, Hualiang
supporting information, p. 606 - 611 (2018/02/06)
In previous study, a series of benzamides was identified as potent antipsychotic agents. As a continuation of the program to discover novel antipsychotics, herein we reported the evaluation of a series of pyridinecarboxamide derivatives. The most promising compound 7h not only held good activities on dopamine D2, serotonin 5-HT1A and 5-HT2A receptors, but also exhibited low potency for α1A, H1 and 5-HT2C receptors, indicating a low propensity of side effects like orthostatic hypotension and weight gain. Furthermore, 7h exhibited more potent antipsychotic-like effect than aripiprazole in behavioral studies. The preliminary results were promising enough for further research around this scaffold.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Paragraph 00909, (2018/09/12)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
cGAS ANTAGONIST COMPOUNDS
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Paragraph 0241, (2017/11/06)
Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
3- HETEROARYL SUBSTITUTED 5-TRIFLUOROMETHYL OXADIAZOLES AS HISTONE DEACETYLASE 6 (HDAC6) INHIBITORS
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Page/Page column 37; 38, (2018/04/11)
The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.
TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
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Page/Page column 61, (2016/03/22)
Provided are quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R 1, R 2, L, X 1, X 2, and X 3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
Discovery, design, and synthesis of indole-based EZH2 inhibitors
Gehling, Victor S.,Vaswani, Rishi G.,Nasveschuk, Christopher G.,Duplessis, Martin,Iyer, Priyadarshini,Balasubramanian, Srividya,Zhao, Feng,Good, Andrew C.,Campbell, Robert,Lee, Christina,Dakin, Les A.,Cook, Andrew S.,Gagnon, Alexandre,Harmange, Jean-Christophe,Audia, James E.,Cummings, Richard T.,Normant, Emmanuel,Trojer, Patrick,Albrecht, Brian K.
supporting information, p. 3644 - 3649 (2015/08/11)
The discovery and optimization of a series of small molecule EZH2 inhibitors is described. Starting from dimethylpyridone HTS hit (2), a series of indole-based EZH2 inhibitors were identified. Biochemical potency and microsomal stability were optimized during these studies and afforded compound 22. This compound demonstrates nanomolar levels of biochemical potency (IC50 = 0.002 μM), cellular potency (EC50 = 0.080 μM), and afforded tumor regression when dosed (200 mpk SC BID) in an EZH2 dependent tumor xenograft model.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Paragraph 0315; 0316, (2015/11/25)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
Modulators of methyl modifying enzymes, compositions and uses thereof
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Paragraph 100; 101, (2015/12/26)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Paragraph 00212; 00213, (2013/06/05)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Paragraph 00166; 00167, (2013/06/05)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein
