136545-11-4Relevant articles and documents
MK2 INHIBITORS AND USES THEREOF
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Paragraph 00972, (2014/10/03)
The present invention provides compounds, compositions thereof, and methods of using the same.
Alpha2C adrenoreceptor agonists
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Page/Page column 31, (2010/11/26)
In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
SUBSTITUTED ARYL-AMINE DERIVATIVES AND METHODS OF USE
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Page/Page column 155, (2008/06/13)
The present invention provides classes of compounds, including-their pharmaceutically acceptable derivatives, useful for treating angiogenesis and related diseases such as cancer. Formula I and II wherein R is a 9- or 10-membered heterocyclyl ring selected from 7-isoquinolinyl,..2-methyl-3-oxo-2,3-dihydroindazol-6-yl, [1,6]-naphthydrin-3-yl, [1,7]-naphthydrin-2-yl, 1-oxo-2,3-dihydrobenzofuran-4-yl, 3-oxo-2,3-dihydrobenzofuran-5-yl, dihydro-benzodioxinyl, 6-quinazolinyl, 2-amino-6-quinazolinyl, 4-methylamino-6-quinazolinyl, 2,4-diamino-6 quinazolinyl, 3-oxo-3,4-dihydro-1,4-benzoxazin-6-yl, 2,2-difluoro-l;3-benzodioxol-5-yl and 2,2,3,3 tetrafluoro-2,3-dihydro-l,4-benzodioxin-6-yl, each of which is optionally substituted with one or more substituents selected from halo, haloakyl, C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, N-dimethylamino-C1-6-alkyl, N-dimethylamino-C1-6-alkoxy, amino, alkyl-carbonylamino, morpholino-sulfonyl, amino-sulfonyl, oxazolyl, pyrrolyl,4 morpholinyl, carboxyl, cyano, and acetyl; wherein R1 in formula I is selected from unsubstituted or substituted phenyl, 5-6 membered heteroaryl, 9-10 membered bicyclic heterocyclyl and 11-14 membered tricyclic heterocyclyl, and R1 in formula II is selected from specific bicyclic heterocycles.
SUBSTITUTED ANTHRANILIC AMIDE DERIVATIVES AND METHODS OF USE
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Page 114, (2010/02/06)
Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Substituted alkylamine derivatives and methods of use
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Page 78, (2010/02/05)
Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Novel potassium channel activators: Synthesis and structure-activity relationship studies of 3,4-dihydro-2H-1,4-benzoxazine derivatives
Matsumoto, Yuzo,Tsuzuki, Ryuji,Matsuhisa, Akira,Takayama, Kazuhisa,Yoden, Toru,Uchida, Wataru,Asano, Masaharu,Fujita, Shigeo,Yanagisawa, Isao,Fujikura, Takashi
, p. 103 - 114 (2007/10/03)
Strong potassium channel-activating effects were found among a series of novel 4-substituted 3,4-dihydro-2H-1,4-benzoxazine derivatives. The key step in preparation was the nucleophilic substitution of 3,4-dihydro-2H-1,4- benzoxazine (3) with activated halogenopyridines, such as halogenopyridine N- oxides (15a-c) and the borane adduct (15d) of 4-bromopyridine. Structure- activity relationship studies identified 2-(3,4-dihydro-2,2-dimethyl-6- nitro-2H-1,4-benzoxazin-4-yl)pyridine-1-oxide (16a: YM934) as the optimal compound. This compound (16a) showed a more potent oral antihypertensive effect than cromakalim in conscious spontaneously hypertensive rats.