148214-86-2Relevant articles and documents
TLR2 MODULATOR COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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Paragraph 00596-00597, (2021/12/08)
The present disclosure relates to compounds which modulate the activity of Toll-like receptor (TLR) proteins, including agonists or activators, partial agonists, and antagonists. Of particular interest of compounds that modulate the activity of TLR2, as well as methods of using such compounds to treat cancer and other disorders associated with a TLR2 pathway.
Substituted Quinazoline and Pyridopyrimidine Derivatives Useful as Anticancer Agents
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Paragraph 0654; 0655, (2019/08/22)
Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
ANTIBACTERIAL BASIC BIAROMATIC DERIVATIVES WITH AMINOALKOXY SUBSTITUTION
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Page/Page column 86, (2016/12/26)
The invention relates to antibacterial compounds of formula I wherein R1a, R2a, R2b, R3a, R3b, R4, R5, U1, U2, U3, U4, V1, V2, V3, V4, X and Q and n are as defined in the specification. It further relates pharmaceutical compositions containing these compounds and the uses of these compounds in the manufacture of medicaments for the treatment of bacterial infections. These compounds are useful antimicrobial agents effective against a variety of human and veterinary pathogens including among others Gram-positive and Gram-negative aerobic and anaerobic bacteria.
PYRROLIDYL DERIVATIVES OF HETEROAROMATIC COMPOUNDS AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 53, (2008/06/13)
The invention pertains to new pyrrolidyl derivatives of benzo-fused aza heteroaromatic compounds that serve as effective phosphodiesterase (PDE) inhibitors. The invention also relates to compounds that are selective inhibitors of PDE-IO. The invention fur
Efficient stereospecific synthesis of (S,S)-3-methoxy-4-methylaminopyrrolidine
Tsuzuki, Yasunori,Chiba, Katsumi,Hino, Katsuhiko
, p. 1793 - 1799 (2007/10/03)
Efficient stereospecific synthesis of (S,S)-3-methoxy-4-methylaminopyrrolidine, an important intermediate for a novel quinolone antitumor agent AG-7352 is presented. Starting from either D- or L-tartaric acid, a stereospecific synthesis of the chiral pyrrolidine was achieved via two SN2 displacement reactions. From the results of this synthetic study, the absolute structure of AG-7352 was chemically determined.
Synthesis and structure-activity relationship of 7-(3'-amino-4'-methoxypyrrolidin-1'-yl)-1-cyclopropyl-6,8-difluoro-1,4 -dihydro-4-oxoquinoline-3-carboxylic acids
Okada,Sato,Tsuji,Tsushima,Nakai,Yoshida,Matsuura
, p. 132 - 138 (2007/10/02)
A new series of quinolone derivatives 3a-l bearing 3-amino-4-methoxypyrrolidines of different configurations and chirality were synthesized and their antibacterial activities as well as some of their toxicological properties were examined. As predicted by our previous quantitative structure-activity relationships (QSAR) analysis of C-7 heterocyclic amine substituted quinolonecarboxylic acid antibacterial agents, these pyrrolidine derivatives showed higher in vitro and in vivo antibacterial activities against both gram-positive and gram-negative bacteria than the analogs bearing various 3-substituted azetidines. Furthermore, the amino and methoxy substituent groups on the pyrrolidine ring exhibited strong configurational and chiral effects on the in vitro and in vivo antibacterial activities of these compounds: (1) cis compounds showed higher antibacterial activities against most of the pathogens examined; (2) N-methylation of the 3-amino group on the pyrrolidine ring lowered in vitro but not in vivo antibacterial activities, particularly leading to superior in vivo anti-pseudomonal activity; (3) the (3'S,4'R)-derivative showed substantially higher activity that the (3'R,4'S)-one. These findings led to the selection of compound 3k for further evaluation as it possessed the highest in vivo antibacterial activity and no cytotoxicity.
Quinoline-3-carboxylic acid derivatives
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, (2008/06/13)
Compounds of formula (I): STR1 (in which R1 is alkoxy, R is alkyl, haloalkyl, alkylamino, cycloalkyl or optionally substituted phenyl, X is chlorine or fluorine and Y is selected from certain specific heterocycles) have excellent antibacterial activity. They may be prepared by introducing the group represented by Y into the corresponding compound in which Y is replaced by a halogen atom.