6635-88-7Relevant academic research and scientific papers
FTO INHIBITORS
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Paragraph 0133; 0134; 0135, (2017/01/31)
The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
FAK AND FLT3 INHIBITORS
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Page/Page column 140, (2014/03/22)
The use of a compound of the formula (I): (Formula (I)) in the preparation of a medicament for treating Acute Myeloid Leukemia or a disease ameliorated by the inhibition of Flt3, or Flt3 and FAK.
FAK INHIBITORS
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Page/Page column 138, (2012/09/10)
A compound of the formula (I): where R1 or R2 is a cycle amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate
Press, Neil J.,Taylor, Roger J.,Fullerton, Joseph D.,Tranter, Pamela,McCarthy, Clive,Keller, Thomas H.,Arnold, Nicola,Beer, David,Brown, Lyndon,Cheung, Robert,Christie, Julie,Denholm, Alastair,Haberthuer, Sandra,Hatto, Julia D. I.,Keenan, Mark,Mercer, Mark K.,Oakman, Helen,Sahri, Helene,Tuffnell, Andrew R.,Tweed, Morris,Tyler, John W.,Wagner, Trixie,Fozard, John R.,Trifilieff, Alexandre
, p. 7472 - 7479 (2012/11/06)
The solubility-driven optimization of a series of 1,7-napthyridine phosphodiesterase-4 inhibitors is described. Directed structural changes resulted in increased aqueous solubility, enabling superior pharmacokinetic properties with retention of PDE4 inhib
Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4)
Day, Jonathan P.,Lindsay, Barbara,Riddell, Tracy,Jiang, Zhong,Allcock, Robert W.,Abraham, Achamma,Sookup, Sebastian,Christian, Frank,Bogum, Jana,Martin, Elisabeth K.,Rae, Robert L.,Anthony, Diana,Rosair, Georgina M.,Houslay, Daniel M.,Huston, Elaine,Baillie, George S.,Klussmann, Enno,Houslay, Miles D.,Adams, David R.
supporting information; experimental part, p. 3331 - 3347 (2011/07/09)
Figure Presented. A survey of PDE4 inhibitors reveals that some compounds trigger intracellular aggregation of PDE4A4 into accretion foci through association with the ubiquitin-binding scaffold protein p62 (SQSTM1). We show that this effect is driven by i
A scalable synthesis of a 1,7-naphthyridine derivative, a PDE-4 inhibitor
Jiang, Xinglong,Lee, George T.,Villhauer, Edwin B.,Prasad, Kapa,Prashad, Mahavir
scheme or table, p. 883 - 889 (2011/03/20)
A six-step synthesis of a 4-[8-(3-fluorophenyl)[1,7]naphthyridin-6-yl]- trans-cyclohexanecarboxylic acid with an overall yield of 27% starting from 2-cyano-3-methylpyridine, cyclohexane-1,4-dicarboxylic acid dimethyl ester, and 3-fluorophenylboronic acid is described. The trans stereochemistry in the cyclohexane moiety was achieved through a series of equilibration steps at different stages of the synthesis.
Substituted indoles as inhibitors of poly (ADP-ribose) polymerase (PARP)
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Page/Page column 23, (2010/02/11)
The present invention relates to a series of substituted indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.
ARYLPIPERAZINYL-CYCLOHEXYL INDOLE DERIVATIVES FOR THE TREATMENT OF DEPRESSION
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Page 49, (2010/02/07)
Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise (I) wherein: Ra, R1, R2 and R3 are each, independently, hydrogen, or a substituent selected from halogen, CF3, alkyl, alkoxy, MeSO2, amino or aminocarbonyl (each optionally substituted by one or two groups selected from alkyl and benzyl) carboxy, or alkoxycarbonyl; or two adjacent of Ra and R1-4 together can form a 5-7 membered carbocyclic or heterocyclic ring which is optionally substituted by a substituent defined above; R4 is hydrogen, halogen, or alkyl; R5 is hydrogen, alkyl, arylalkyl, or aryl; R6 is hydrogen, halogen, CF3, CN, carbamide, alkoxy or benzyloxy; X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen; Y is CH or nitrogen; and Z is carbon or nitrogen; or pharmaceutically acceptable salts thereof.
Substituted 1,3-Dihydro-2H-pyrrolopyridin-2-ones as Potential Antiinflammatory Agents
Ting, Pauline C.,Kaminski, James J.,Sherlock, Margaret H.,Tom, Wing C.,Lee, Joe F.,et al.
, p. 2697 - 2706 (2007/10/02)
A series of analogues based on the 1,3-dihydro-2H-pyrrolopyridin-2-one ring system have been synthesized and shown to possess oral antiinflammatory activity in both the reverse passive Arthus reaction (RPAR) pleural cavity assay in rats and in the adjuvant-induced arthritic rat model (AAR).Several members of this series additionally exhibit an inhibitory effect on the in vivo production of prostaglandin- and leukotriene-derived products or arachidonic acid metabolism although these compounds exhibit no significant inhibitory activity against the cyclooxygenase and 5-lipoxygenase enzymes in vitro.Structure-activity relationships in this series are discussed.
