207296-89-7Relevant academic research and scientific papers
Identification of novel aminopiperidine derivatives for antibacterial activity against Gram-positive bacteria
Lee, Hee-Yeol,An, Kyung-Mi,Jung, Juyoung,Koo, Je-Min,Kim, Jeong-Geun,Yoon, Jong-Min,Lee, Myong-Jae,Jang, Hyeonsoo,Lee, Hong-Sub,Park, Soobong,Kang, Jae-Hoon
, p. 3148 - 3152 (2016/06/13)
We have previously reported amidopiperidine derivatives as a novel peptide deformylase (PDF) inhibitor and evaluated its antibacterial activity against Gram-positive bacteria, but poor pharmacokinetic profiles have resulted in low efficacy in in vivo mouse models. In order to overcome these weaknesses, we newly synthesized aminopiperidine derivatives with remarkable antimicrobial properties and oral bioavailability, and also identified their in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE) and penicillin-resistant Streptococcus pneumoniae (PRSP).
AMIDINE COMPOUND AND BACTERICIDAL AGENT
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, (2017/04/14)
PROBLEM TO BE SOLVED: To provide a novel amidine compound excellent in bactericidal property and safety and capable of being industrially advantageously synthesized and a bactericidal agent or plant disease control agent containing the amidine compound as an active ingredient. SOLUTION: There is provided a compound represented by the formula [I] or a salt hereof. [I], where Y is an unsubstituted/substituted bivalent cyclic amine residue, X and Z are each independently an unsubstituted/substituted alkylene group or the like, W is a singe bond or -N(R5)-, R5 is H, an unsubstituted/substituted heterocycle group or the like, R1 to R3 are each independently H, an unsubstituted/substituted hydrocarbon group or the like, A is an aryl group or a heteroaryl group substituted by carboxy amidine. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
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, (2015/05/05)
The present invention provides novel compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g.,leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. (I)
BENZAMIDE CGRP RECEPTOR ANTAGONISTS
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Page/Page column 77, (2015/11/09)
The present invention is directed to benzamide compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
QUINAZOLINE INHIBITORS OF PI3K
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Paragraph 00249, (2014/10/15)
The invention is directed to compounds of formula I: and pharmaceutically acceptable salts as well as methods of making and using the compounds to inhibit PI3K.
Synthesis and structure-activity relationships of potent and orally active 5-HT4 receptor antagonists: Indazole and benzimidazolone derivatives
Schaus, John M.,Thompson, Dennis C.,Bloomquist, William E.,Susemichel, Alice D.,Calligaro, David O.,Cohen, Marlene L.
, p. 1943 - 1955 (2007/10/03)
A series of indole-3-carboxamides, indazole-3-carboxamides, and benzimidazolone-3-carboxamides was synthesized and evaluated for antagonist affinity at the 5-HT4 receptor in the rat esophagus. The endo-3-tropanamine derivatives in the indazole
