860624-90-4Relevant articles and documents
3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent
Kerns, Jeffrey K.,Busch-Petersen, Jakob,Fu, Wei,Boehm, Jeffrey C.,Nie, Hong,Muratore, Michael,Bullion, Ann,Lin, Guoliang,Li, Huijie,Davis, Roderick,Lin, Xichen,Lakdawala, Ami S.,Cousins, Rick,Field, Rita,Payne, Jeremy,Miller, David D.,Bamborough, Paul,Christopher, John A.,Baldwin, Ian,Osborn, Ruth R.,Yonchuk, John,Webb, Edward,Rumsey, William L.
supporting information, p. 1164 - 1169 (2018/11/23)
IκB kinase β (IKKβ or IKK2) is a key regulator of nuclear factor kappa B (NF-κB) and has received attention as a therapeutic target. Herein we report on the optimization of a series of 3,5-disubstituted-indole-7-carboxamides for oral activity. In doing so
PLANT GROWTH REGULATOR
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Paragraph 0039, (2018/05/30)
PROBLEM TO BE SOLVED: To provide a plant growth regulator. SOLUTION: The plant growth regulator comprises a compound represented by formula 1, or a salt or ester thereof as an active ingredient. (R1 is H, a halogen atom, a hydroxy group, an alkyl group, or an alkoxy group; R2 is H, a halogen atom, a hydroxy group, an alkyl group, or an alkoxy group; and R3 is a hydroxy group, an alkoxy group, or an amino group.) SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
CD38 INHIBITORS AND METHODS OF TREATMENT
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, (2016/06/28)
Compounds of Formula (I) and methods of treating diseases of metabolism by modulating cellular NAD+ levels through the inhibition of the CD38 enzyme, are disclosed. Formula (I).
3,5-Disubstituted-indole-7-carboxamides: The discovery of a novel series of potent, selective inhibitors of IKK-β
Miller, David D.,Bamborough, Paul,Christopher, John A.,Baldwin, Ian R.,Champigny, Aurelie C.,Cutler, Geoffrey J.,Kerns, Jeffrey K.,Longstaff, Timothy,Mellor, Geoffrey W.,Morey, James V.,Morse, Mary A.,Nie, Hong,Rumsey, William L.,Taggart, John J.
, p. 2255 - 2258 (2011/05/15)
The discovery and hit-to-lead exploration of a novel series of selective IKK-β kinase inhibitors is described. The initial lead fragment 3 was identified by pharmacophore-directed virtual screening. Homology model-driven SAR exploration of the template le
INDOLE CARBOXAMIDES AS IKK2 INHIBITORS
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, (2008/12/04)
The invention is directed to novel indole carboxamide compounds. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKKβ) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
CHEMICAL COMPOUNDS
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Page/Page column 39, (2010/11/27)
The invention is directed to novel indolecarboxamide derivatives, Specifically, the invention is directed to compounds according to formula (I), where R1 , R2, R3 and X are defined below. These compounds are useful in the treatment of disorders associated
Indole, indazole and indoline derivatives as CETP inhibitors
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Page/Page column 22, (2010/02/15)
The present invention relates to compounds of formula (I): wherein —X—Y—, R1 to R11 and n are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are mediated by CETP inhibitors.
CHEMICAL COMPOUNDS
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Page/Page column 73-74, (2010/10/20)
The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (1): where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds o
INDOLE DERIVATIVES AND USE THEREOF AS KINASE INHIBITORS IN PARTICULAR IKK2 INHIBITORS
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Page/Page column 39, (2010/02/13)
Indole carboxamide compounds of Formula (I): are provided as inhibitors of kinase activity, in particular IKK2 activity as well as compositions and medicaments containing them, for use in inflammatory and tissue repair disorders.