6297-22-9Relevant articles and documents
DOPAMINE D3 RECEPTOR ANTAGONISTS COMPOUNDS
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Page/Page column 146, (2016/05/19)
The disclosure is directed to novel dopamine D3 receptor antagonists, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, including treating drug dependency and psychosis.
BICYCLIC HETEROARYL DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Page/Page column 22-23, (2013/11/05)
Bicyclic heteroaryl derivatives of Formula 1, and pharmaceutically acceptable salts, isomers, hydrates and solvates thereof can selectively and effectively inhibit DGAT1, and thus can be useful as medicines for effectively treating dangerous diseases such as obesity, type 2 diabetes, abnormal lipidemia, metabolic syndrome (syndrome X) and the like, which are caused by DGAT1, with no adverse side effects.
Site-selective oxidation of unactivated C sp 3-H bonds with hypervalent iodine(III) reagents
Moteki, Shin A.,Usui, Asuka,Zhang, Tiexin,Solorio Alvarado, Cesar R.,Maruoka, Keiji
supporting information, p. 8657 - 8660 (2013/09/12)
By design: The site-selective oxidation of unactivated secondary C sp 3-H bonds was accomplished with hypervalent iodine(III) reagents and tert-butyl hydroperoxide (see scheme). The preparation and derivatization of the hypervalent iodine(III) reagent are simple, thus allowing the rational design of these reagents to optimize the site selectivity of the oxidation. Copyright
Discovery of LFF571: An investigational agent for Clostridium difficile infection
Lamarche, Matthew J.,Leeds, Jennifer A.,Amaral, Adam,Brewer, Jason T.,Bushell, Simon M.,Deng, Gejing,Dewhurst, Janetta M.,Ding, Jian,Dzink-Fox, Joanne,Gamber, Gabriel,Jain, Akash,Lee, Kwangho,Lee, Lac,Lister, Troy,McKenney, David,Mullin, Steve,Osborne, Colin,Palestrant, Deborah,Patane, Michael A.,Rann, Elin M.,Sachdeva, Meena,Shao, Jian,Tiamfook, Stacey,Trzasko, Anna,Whitehead, Lewis,Yifru, Aregahegn,Yu, Donghui,Yan, Wanlin,Zhu, Qingming
supporting information; experimental part, p. 2376 - 2387 (2012/06/01)
Clostridium difficile (C. difficile) is a Gram positive, anaerobic bacterium that infects the lumen of the large intestine and produces toxins. This results in a range of syndromes from mild diarrhea to severe toxic megacolon and death. Alarmingly, the prevalence and severity of C. difficile infection are increasing; thus, associated morbidity and mortality rates are rising. 4-Aminothiazolyl analogues of the antibiotic natural product GE2270 A (1) were designed, synthesized, and optimized for the treatment of C. difficile infection. The medicinal chemistry effort focused on enhancing aqueous solubility relative to that of the natural product and previous development candidates (2, 3) and improving antibacterial activity. Structure-activity relationships, cocrystallographic interactions, pharmacokinetics, and efficacy in animal models of infection were characterized. These studies identified a series of dicarboxylic acid derivatives, which enhanced solubility/efficacy profile by several orders of magnitude compared to previously studied compounds and led to the selection of LFF571 (4) as an investigational new drug for treating C. difficile infection.
Compounds Which Modulate The CB2 Receptor
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Page/Page column 73, (2010/02/17)
Compounds of formula (I) are disclosed. Compounds according to the and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
The structure - Activity relationship of the antimalarial ozonide arterolane (OZ277)
Dong, Yuxiang,Wittlin, Sergio,Sriraghavan, Kamaraj,Chollet, Jacques,Charman, Susan A.,Charman, William N.,Scheurer, Christian,Urwyler, Heinrich,Tomas, Josefina Santo,Snyder, Christopher,Creek, Darren J.,Morizzi, Julia,Koltun, Maria,Matile, Hugues,Wang, Xiaofang,Padmanilayam, Maniyan,Tang, Yuanqing,Dorn, Arnulf,Brun, Reto,Vennerstrom, Jonathan L.
experimental part, p. 481 - 491 (2010/05/02)
The structure and stereochemistry of the cyclohexane substituents of analogues of arterolane (OZ277) had little effect on potency against Plasmodium falciparum in vitro.Weak base functional groups were not required for high antimalarial potency, but they were essential for high antimalarial efficacy in P. berghei-infected mice. Five new ozonides with antimalarial efficacy and ADME profiles superior or equal to that of arterolane were identified.
Combined effects on selectivity in Fe-catalyzed methylene oxidation
Chen, Mark S.,White, M. Christina
scheme or table, p. 533 - 571 (2010/10/05)
Methylene C-H bonds are among the most difficult chemical bonds to selectively functionalize because of their abundance in organic structures and inertness to most chemical reagents. Their selective oxidations in biosynthetic pathways underscore the power of such reactions for streamlining the synthesis of molecules with complex oxygenation patterns. We report that an iron catalyst can achieve methylene C-H bond oxidations in diverse natural-product settings with predictable and high chemo-, site-, and even diastereoselectivities. Electronic, steric, and stereoelectronic factors, which individually promote selectivity with this catalyst, are demonstrated to be powerful control elements when operating in combination in complex molecules. This small-molecule catalyst displays site selectivities complementary to those attained through enzymatic catalysis.
Efficient synthesis of a new pipecolic acid analogue with a bicyclic structure
Casabona, Diego,Cativiela, Carlos
, p. 10000 - 10004 (2007/10/03)
This report describes the synthesis of 2-azabicyclo[2.2.2]octane-1-carboxylic acid, a constrained pipecolic acid analogue. The route gives a very good total yield starting from cheap and readily available compounds and uses very easy reactions.
New high affinity H3 receptor agonists without a basic side chain
Kitbunnadaj, Ruengwit,Hoffmann, Marcel,Fratantoni, Silvina A.,Bongers, Gerold,Bakker, Remko A.,Wieland, Kerstin,El Jilali, Ahmed,De Esch, Iwan J. P.,Menge, Wiro M. P. B.,Timmerman, Henk,Leurs, Rob
, p. 6309 - 6323 (2007/10/03)
In this study, we replaced the basic amine function of the known histamine H3 receptor agonists imbutamine or immepip with non-basic alcohol or hydrocarbon moieties. All compounds in this study show a moderate to high affinity for the cloned human H3 receptor and, unexpectedly, almost all of them act as potent agonists. Moreover, in the alcohol series, we consistently observed an increased selectivity for the human H3 receptor over the human H4 receptor, but none of the compounds in this series possess increased affinity and functional activity compared to their alkylamine congeners. In this new series of compounds VUF5657, 5-(1H-imidazol-4-yl)-pentan-1-ol, is the most potent histamine H3 receptor agonist (pKi = 8.0 and pEC50 = 8.1) with a 320-fold selectivity at the human H3 receptor over the human H 4 receptor.
Free radical-mediated carboxylation by radical reaction of alkyl iodides with methyl oxalyl chloride
Kim, Sunggak,Jon, Sang Yong
, p. 7317 - 7320 (2007/10/03)
Free radical-mediated carboxylation is achieved by treatment of alkyl iodides with methyl oxalyl chloride and bis(tributyltin) in benzene at 350 nm to afford the corresponding acid chlorides as a major product along with a small amount of the methyl esters.
