- A Novel Synthesis of 1-Alkyl-2-phenyl-1,8-naphthyridin-4-one
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Provided is a novel method for manufacturing 1-alkyl-2-phenyl-1,8-naphthyridin-4-one from 2-chloronicotinic acid. According to the present invention, 1-alkyl-2-phenyl-1,8-naphthyridin-4-one can be synthesized through simple reaction conditions and simple
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Paragraph 0078; 0080
(2017/09/30)
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- THIAZOLE DERIVATIVES FOR THE TREATMENT OF ANIMAL TRYPANOSOMIASIS
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The present invention relates to a novel class of compounds of general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, X and Y are as defined herein, to their use in human and veterinary medicine, and in the treatment of animal trypanosomiasis in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
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Page/Page column 73; 74
(2016/10/04)
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- CONDENSED HETEROCYCLIC COMPOUND
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The present invention provides a compound having a superior PDE10A inhibitory action and use thereof. The compound is a compound represented by the following formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
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Paragraph 0489-0491
(2014/01/08)
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- FUSED PIPERIDINE COMPOUND AND PHARMACEUTICAL AGENT COMPRISING SAME
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The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula
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Page/Page column 28
(2012/02/14)
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- Synthesis and biological evaluation of imidazo[4,5-b]pyridine and 4-heteroaryl-pyrimidine derivatives as anti-cancer agents
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A series of N-phenyl-imidazo[4,5-b]pyridin-2-amines, 4-indazolyl-N- phenylpyrimidin-2-amines and N-phenyl-4-pyrazolo[3,4-b]pyridin-pyrimidin-2- amines have been synthesized. Their anti-proliferative activities were tested in HCT-116 human colon carcinoma and MCF-7 breast carcinoma cell lines. Many exhibited potent anti-proliferative and CDK9 inhibitory activities. A lead compound 18b demonstrated the ability to reduce the level of Mcl-1 anti-apoptotic protein, to activate caspase 3/7 and induce cancer cell apoptosis.
- Lukasik, Pawel M.,Elabar, Sherifa,Lam, Frankie,Shao, Hao,Liu, Xiangrui,Abbas, Abdullah Y.,Wang, Shudong
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p. 311 - 322
(2013/01/15)
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- Fatty acid amide hydrolase inhibitors. 3: Tetra-substituted azetidine ureas with in vivo activity
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We describe here our attempts to optimise the human fatty acid amide hydrolase (FAAH) inhibition and physicochemical properties of our previously reported tetrasubstituted azetidine urea FAAH inhibitor, VER-156084. We describe the SAR of a series of analogues and conclude with the demonstration of in vivo dose-dependant FAAH inhibition in an anandamide-loading study in rats.
- Roughley, Stephen D.,Browne, Helen,MacIas, Alba T.,Benwell, Karen,Brooks, Teresa,D'Alessandro, Jalanie,Daniels, Zoe,Dugdale, Sarah,Francis, Geraint,Gibbons, Ben,Hart, Terance,Haymes, Timothy,Kennett, Guy,Lightowler, Sean,Matassova, Natalia,Mansell, Howard,Merrett, Angela,Misra, Anil,Padfield, Anthony,Parsons, Rachel,Pratt, Robert,Robertson, Alan,Simmonite, Heather,Tan, Kiri,Walls, Steven B.,Wong, Melanie
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supporting information; experimental part
p. 901 - 906
(2012/03/11)
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- Identification of an adamantyl azaquinolone JNK selective inhibitor
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3-[4-((1S,2S,3R,5S,7S)-5-Hydroxyadamantan-2-ylcarbamoyl)benzyl] -4-oxo-1-phenyl-1,4-dihydro-[1,8]naphthyridine-2-carboxylic acid methyl ester (4) was identified as a novel, druglike and selective quinolone pan JNK inhibitor. In this communication, some of the structure-activity relationship of the azaquinolone analogues leading to 4 is discussed. The focus is on how changes at the amide functionality affected the biochemical potency, cellular potency, metabolic properties, and solubility of this class of JNK inhibitors. Optimization of these properties led to the identification of the adamantyl analogue, 4. 4 achieved proof of mechanism in both rat and mouse TNF-α challenge models.
- Haynes, Nancy-Ellen,Scott, Nathan R.,Chen, Li C.,Janson, Cheryl A.,Li, Jia Kui,Lukacs, Christine M.,Railkar, Aruna,Tozzo, Effie,Whittard, Toni,Brown, Nicholas F.,Cheung, Adrian Wai-Hing
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supporting information
p. 764 - 768
(2012/11/14)
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- ADAMANTYL COMPOUNDS
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The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are
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Page/Page column 40-41
(2012/10/18)
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- FUSED DERIVATIVES AS PI3Kdelta INHIBITORS
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The present invention provides fused derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
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Page/Page column 100
(2011/11/01)
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- Fatty acid amide hydrolase inhibitors. Surprising selectivity of chiral azetidine ureas
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We report the discovery of a novel, chiral azetidine urea inhibitor of Fatty Acid Amide Hydrolase (FAAH,) and describe the surprising species selectivity of VER-156084 versus rat and human FAAH and also hCB1.
- Hart, Terance,Macias, Alba T.,Benwell, Karen,Brooks, Teresa,D'Alessandro, Jalanie,Dokurno, Pawel,Francis, Geraint,Gibbons, Ben,Haymes, Timothy,Kennett, Guy,Lightowler, Sean,Mansell, Howard,Matassova, Natalia,Misra, Anil,Padfield, Anthony,Parsons, Rachel,Pratt, Robert,Robertson, Alan,Walls, Steven,Wong, Melanie,Roughley, Stephen
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supporting information; experimental part
p. 4241 - 4244
(2010/04/02)
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- SUBSTITUTED 1,2,4-OXADIAZOLES AND ANALOGS THEREOF AS CB2 RECEPTOR MODULATORS, USEFUL IN THE TREATMENT OF PAIN, RESPIRATORY AND NON-RESPIRATORY DISEASES
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The present invention relates to compounds represented by Formula (I), Formula (II) and Formula (III) and pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This inv
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Page/Page column 48-47
(2009/05/28)
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- AZETIDINECARBOXAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CB1 RECEPTOR MEDIATED DISORDRS
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Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors, such as obesity, wherein: R1 is aryl or heteroaryl; R2 is alkyl, aryl or heteroaryl; R3 is alkyl, aryl, heteroaryl, NR9R10, OR 15, or NR16C(O)R17;Y is C=O, C=S, SO2, or (CR7R8)p; m = 1 or 2; n = 1 or 2; and p=1,2,3 or 4, R7 to R17 being as defined in the specification; wherein if -Y-R3 is -C(O)NH(alkyl) then: R1 and/or R2 is selected from heteroary1; and/or m and/or n is 2; and/or R11 and/or R12 is lower alkyl, or a pharmaceutically acceptable salt or prodrug thereof.
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