- Discovery and Structure-Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials
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A phenotypic high-throughput screen allowed discovery of quinazolinone-2-carboxamide derivatives as a novel antimalarial scaffold. Structure-activity relationship studies led to identification of a potent inhibitor 19f, 95-fold more potent than the origin
- Laleu, Beno?t,Akao, Yuichiro,Ochida, Atsuko,Duffy, Sandra,Lucantoni, Leonardo,Shackleford, David M.,Chen, Gong,Katneni, Kasiram,Chiu, Francis C. K.,White, Karen L.,Chen, Xue,Sturm, Angelika,Dechering, Koen J.,Crespo, Benigno,Sanz, Laura M.,Wang, Binglin,Wittlin, Sergio,Charman, Susan A.,Avery, Vicky M.,Cho, Nobuo,Kamaura, Masahiro
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p. 12582 - 12602
(2021/09/13)
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- POLY-ADP RIBOSE POLYMERASE (PARP) INHIBITORS
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The present invention is related to a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by the following structural formula: The present invention is also related a method of treating a subject with a disease which can be ameliorated by inhibition of poly(ADP-ribose)polymerase (PARP). The definitions of the variables are provided herein.
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Page/Page column 110
(2018/07/29)
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- 2- [ (2-{PHENYLAMINO}-1H-PYRROLO [2, 3-D] PYRIMIDIN-4-YL) AMINO] BENZAMIDE DERIVATIVES AS IGF-1R INHIBITORS FOR THE TREATMENT OF CANCER
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Novel pyrrolopyrimidines as shown in formula (I) and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.
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Page/Page column 73
(2009/04/25)
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- Comparative catalytic C-H vs. C-Si activation of arenes with Pd complexes directed by urea or amide groups
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Analysis of regiocontrol in Pd-catalysed C-H activation leads to observations of aryltrimethylsilyl activation and to superior results with urea-based substrates.
- Rauf, Waqar,Thompson, Amber L.,Brown, John M.
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supporting information; experimental part
p. 3874 - 3876
(2010/01/06)
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- HETERO BICYCLIC CARBOXAMIDE DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS
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The present invention relates to compounds of Formula (I)I and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds
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Page/Page column 128
(2009/01/24)
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- Aryl and biaryl piperidines with MCH modulatory activity
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In one embodiment, this invention provides a novel class of compounds as antagonists of the MCH receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration or one or more of diseases associated with the MCH receptor. An illustrative inventive compound is shown below: 1
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- Process to obtain benzoxazines to be used for the synthesis of ofloxazine, levofloxazine and derivatives
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A process to obtain benzoxazines useful for the synthesis of Ofloxazine, Levofloxazine and derivatives. The benzoxacines (I) where Xb is an halogen and R1 is H, alkyl or alkenyl of up to 6 atoms of C or aryl, can be obtained by means of cycling a compound of formula (II) through the reaction with triphenylphosphine and ethyl azodicarboxilate. The compounds of formula (II) can be obtained through the reaction of a compound (III) with an adequate epoxide. Through the use of the adequate chiral epoxide it is possible to obtain the enantiomerically desired intermediate and, therefore and selectively, it is possible to obtain the desired final product with the adequate enantiomeric form without the need to carry out a resolution stage. The Compounds (I) are useful and key intermediates for the synthesis of the antimicrobials Oflixazine and Levofloxazine. STR1
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- A practical route to C-8 substituted fluoroquinolones
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The ortho metalation of N-(tert-butoxycarbonyl)-3,4-difluoroaniline, with t-BuLi at -78°C in THF occurred regioselectively at C-2 position. The resulting lithiated species reacted with a variety of electrophiles to give 2-substituted-3,4-difluoranilines i
- Carretero,Garcia Ruano,Vicioso
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p. 7373 - 7382
(2007/10/02)
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