- TLR2 MODULATOR COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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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.
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Paragraph 00600-00601
(2021/12/08)
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- ERK INHIBITORS
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The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.
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- Highly active organocatalysts for asymmetric anti-mannich reactions
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Lighten the load! A family of enantiopure 4-oxy-substituted 3-aminopyrrolidines arising from the enantioselective ring-opening of meso-3-pyrroline oxide have been developed as catalysts for the asymmetric, anti-selective Mannich reaction (see scheme; PMP=
- Martín-Rapún, Rafael,Fan, Xinyuan,Sayalero, Sonia,Bahramnejad, Mahboubeh,Cuevas, Félix,Pericàs, Miquel A.
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supporting information; experimental part
p. 8780 - 8783
(2011/09/15)
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- NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION
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The present invention relates to a compound of Formula (I): wherein: R1 is H or C1-2 alkyl; R2 is H or C1-3 alkyl; R3 and R4 are each independently H or C1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents
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Page/Page column 36-37
(2010/11/04)
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- Design of novel aminopyrrolidine factor Xa inhibitors from a screening hit
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Starting from a hit identified by focused screening, 3-aminopyrrolidine factor Xa inhibitors were designed. The binding mode as determined by X-ray structural analysis as well as the pharmacokinetic behaviour of selected compounds is discussed.
- Zbinden, Katrin Groebke,Anselm, Lilli,Banner, David W.,Benz, Joerg,Blasco, Francesca,Decoret, Guillaume,Himber, Jacques,Kuhn, Bernd,Panday, Narendra,Ricklin, Fabienne,Risch, Philippe,Schlatter, Daniel,Stahl, Martin,Thomi, Stefan,Unger, Robert,Haap, Wolfgang
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body text
p. 2787 - 2795
(2009/10/17)
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- Cyclic amines
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The invention is concerned with cyclic amines of formula (I) wherein X1 to X3, Y1 to Y3, R1′, R1″ and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit coagulation factor Xa and can be used as medicaments and for treating diseases associated with coagulation factor Xa.
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Page/Page column 37
(2010/11/24)
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- A short, simple and general approach for the synthesis of (3S,4S)-3-methoxy-4-methylamino pyrrolidine and (3S,4R)-3-methoxy-4-methylamino pyrrolidine
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A general and efficient stereoselective approach for the synthesis of (3S,4S) and (3S,4R)-3-methoxy-4-methylamino pyrrolidines, a part of the structure of AG-7352, a naphthyridine antitumor agent and quinoline antibacterial compounds has been described.
- Kumar, A. Ravi,Reddy, J. Santhosh,Rao, B. Venkateswara
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p. 5687 - 5689
(2007/10/03)
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- Practical synthesis of (3S,4S)-3-methoxy-4-methylaminopyrrolidine
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Three synthetic methods for the preparation of (3S,4S)-3-methoxy-4-methylaminopyrrolidine, an important intermediate in the synthesis of the novel quinolone antitumur agent, AG-7352, have been developed. By one route, an efficient and large-scale preparation of the chiral pyrrolidine could be achieved through resolution of (±)-1-Boc-3-benzylamino-4-hydroxypyrrolidine, which is prepared from either 3-pyrroline or 1,4-dichloro-2-butene.
- Tsuzuki, Yasunori,Chiba, Katsumi,Mizuno, Kazuhiro,Tomita, Kyoji,Suzuki, Kenji
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p. 2989 - 2997
(2007/10/03)
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- Efficient stereospecific synthesis of (S,S)-3-methoxy-4-methylaminopyrrolidine
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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.
- Tsuzuki, Yasunori,Chiba, Katsumi,Hino, Katsuhiko
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p. 1793 - 1799
(2007/10/03)
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- 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
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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.
- Okada,Sato,Tsuji,Tsushima,Nakai,Yoshida,Matsuura
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p. 132 - 138
(2007/10/02)
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