- HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF ABNORMAL CELLULAR PROLIFERATION
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This invention is in the area of heterocyclic-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
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Page/Page column 127-129
(2019/07/20)
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- PYRIMIDINYL-PYRIDYLOXY-NAPHTHYL COMPOUNDS AND METHODS OF TREATING IRE1-RELATED DISEASES AND DISORDERS
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Described herein are pyrimidinyl-pyridyloxy-naphthyl compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formula (I) or (I') structure : or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula (I) or (I') compounds, as well as methods of using such IRE1 modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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Paragraph 1210; 1211
(2018/10/19)
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- (3S, 4R) - 3-amino-4-methyl-piperidin-1-carboxylic acid tert-butyl ester preparation method
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The invention discloses a high-stereoselectivity preparation method of (3S, 4R)-3-amido-4-methyl piperidine-1-tertiary butyl carboxylate, which is mainly used for solving the problems that compounds reported by conventional documents have long synthesis routes and poor stereoselectivity. The preparation method comprises the following steps: carrying out ylide reaction under an alkaline condition by taking a compound R)-1-(1-tert-butyloxycarbonyl)-4-oxo-3-piperidyl hydrazine-1,2-dibenzyl dicarboxylate as a starting material to obtain (S)-1-(1-tert-butyloxycarbonyl)-4-methylene -3-piperidyl hydrazine-1,2-dibenzyl dicarboxylate; then, obtaining (3S, 4R)-3- diazanyl-4-methyl piperidine-1-tertiary butyl carboxylate by catalytic hydrogenation under action of a metal hydrogenation catalyst and hydrogen gas; and finally, reducing under action of the metal hydrogenation catalyst and hydrogen gas to obtain the (3S, 4R)-3-amido-4-methyl piperidine-1-tertiary butyl carboxylate. And the total yield is 34.5%.
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Paragraph 0037; 0038; 0042
(2017/04/27)
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- The protection of the nitrogen of (3R, 4R) -3 - methylamino -4 - methyl piperidine asymmetric synthesis method, relevant intermediate and a method for preparing raw materials thereof
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The invention relates to a preparation method of nitrogen protected (3R,4R)-3-methylamino-4-methylpiperidine (I). The method comprises the following steps: carrying out a reductive amination reaction on a compound of formula (III) and (R)-1-phenylethylamine to obtain a compound of formula (II), removing chiral prosthetic groups from the compound of formula (II), and adding a methyl group to the amino group of the compound of formula (II) in order to obtain nitrogen protected (3R,4R)-3-methylamino-4-methylpiperidine (I), wherein R in each of the formula (I), the formula (II) and the formula (III) is an amino protection group or hydrogen, and the amino protection group can be C1-4 alkoxycarbonyl, benzyloxycarbonyl or benzyl groups which can be removed through hydrolysis or hydrogenation. The asymmetric synthesis method of nitrogen protected (3R,4R)-3-methylamino-4-methylpiperidine (I) has the advantages of reasonable technology, concise route, obtaining of the required product in a high ee value manner by constructing two chiral centers through chiral induced one-step reductive amination, cheap raw materials, and no waste isomer emission, and is suitable for large-scale industrialized production.
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Paragraph 0049; 0050; 0051
(2016/10/09)
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- BRUTON'S TYROSINE KINASE INHIBITORS
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The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
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Page/Page column 160; 162
(2011/04/14)
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