101012-32-2Relevant articles and documents
Discovery of N-substituted 7-azaindoline derivatives as potent, orally available M1 and M4 muscarinic acetylcholine receptors selective agonists
Takai, Kentaro,Inoue, Yasunao,Konishi, Yasuko,Suwa, Atsushi,Uruno, Yoshiharu,Matsuda, Harumi,Nakako, Tomokazu,Sakai, Mutsuko,Nishikawa, Hiroyuki,Hashimoto, Gakuji,Enomoto, Takeshi,Kitamura, Atsushi,Uematsu, Yasuaki,Kiyoshi, Akihiko,Sumiyoshi, Takaaki
, p. 3189 - 3193 (2014)
We designed and synthesized novel N-substituted 7-azaindoline derivatives as selective M1 and M4 muscarinic acetylcholine receptors (mAChRs) agonists. Hybridization of compound 2 with the HTS hit compound 5 followed by optimization of the N-substituents of 7-azaindoline led to identification of compound 1, which showed highly selective M1 and M4 mAChRs agonistic activity, weak human ether-a-go-go related gene inhibition, and good bioavailability in multiple animal species.
A spirocyclic oxindole analogue: Synthesis and antitumor activities
Hong, Hui,Huang, Long Jiang,Teng, Da Wei
, p. 1009 - 1012 (2011)
A new synthesis of spirocyclic oxindole analogue spiro[piperidine-4, 3′-pyrrolo[2,3-b]pyridin]-2′(1′H)-one 1 is described. The key steps involve dialkylation of arylacetonitrile and cyclization of the azaoxindole ring by an intramolecular Buchwald-Hartwig amidation of carboxylic amide and aryl chloride. A small library was obtained by reductive amination of 1 with various aldehydes and was screened against human lung cancer cell A549, human liver cancer cell BEL7402, and human colon cancer cell HCT-8. The results show that most of the library compounds 2 have some inhibitory activities. 2-(Trifluoromethoxy) benzylic substituted spirocyclic azaoxindole 2e was identified as a nanomolar inhibitor against human lung cancer cell A-549 (IC50 = 50 nmol/L).
TOPICAL FORMULATIONS
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, (2020/06/10)
Provided herein are gelled topical formulations for the treatment of skin diseases comprising: a) a MEK inhibitor; b) one or more organic solvents in an amount of about 70% to about 99% by weight; and c) a gelling agent; wherein the one or more organic solvents are selected from the group consisting of C2-6 alcohol, a C2-6 alkylene glycol, a di-(C2-6 alkylene) glycol, a polyethylene glycol, C1-3 alkyl-(OCH2CH2)1-5-OH, DMSO, ethyl acetate, acetone, N-methyl pyrrolidone, benzyl alcohol, glycerin, and an oil; the gelling agent is hydroxypropyl cellulose having a molecular weight ranging from about 40,000 Dato about 2,500,000 Da; and wherein the gelled topical formulation has a viscosity of from 1 to 25,000 cps; and DMSO, when present, is combined with at least one other of said organic solvents such that DMSO is present in an amount of less than 50% by weight.
ARYL-ANILINE AND HETEROARYL-ANILINE COMPOUNDS FOR TREATMENT OF SKIN CANCERS
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, (2020/06/10)
Provided herein are compounds and pharmaceutical compositions thereof for treating a skin cancer in a subject in need thereof, wherein the compound is according to any one of formula (I), (II), (III), (IV), and (V): wherein X1, X2, X3, R1, R2, R2a, R13, Rl3a, R23, R23a, R23b, R33, R33a, R33b, R43, R43a, R51, R53, R53a, R53b, bond "a", and subscript n are described herein.
ARYL-ANILINE AND HETEROARYL-ANILINE COMPOUNDS FOR TREATMENT OF BIRTHMARKS
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, (2020/06/10)
Provided herein are compounds and pharmaceutical compositions thereof for treating a birthmark in a subject in need thereof, wherein the compound is according to any one of formula (1), (II), (III), (IV), and (V). wherein X1, X2, X3, R1, R2, R2a, R13, R13a, R23, R23a, R23b, R33, R33a, R33b, R43, R43a, R51, R53, R53a, R53b, bond "a", and subscript n are described herein.
FAK AND FLT3 INHIBITORS
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Page/Page column 141, (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; 139, (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.
THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
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Page/Page column 25, (2009/09/05)
The invention provides a series of thieno[2,3-b]pyridine derivatives wherein Y represents a linkage of formula C(O) or S(O)2; R1 represents hydrogen, halogen, cyano, nitro, C|-6 alkyl, trifluoromethyl, Ci.6 alkoxy, trifluoromethoxy,
THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
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Page/Page column 35-36, (2010/01/12)
A series of thieno[2,3-6]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fus
THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS
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Page/Page column 25-26, (2009/03/07)
A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2- position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment, of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.