- PYRROLOPYRIMIDINE ITK INHIBITORS
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Disclosed herein are arylpyridinone compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structures of Formulas (I)-(IV): wherein the R groups, m, n, and X are as defined in the detailed description. Methods of inhibition of ITK activity in a human or animal subject are also provided.
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Paragraph 0677; 0678; 0679
(2020/02/27)
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- Synthetic method of 5-bromo-7-azaindole
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The invention discloses a synthetic method of 5-bromo-7-azaindole. According to the synthetic method, 2, 5-dibromo-2-aminopyridine and 3, 3-diethoxy methyl propionate are subjected to synthesis so asto obtain (E)-3-((3, 5-dibromopyridine-2-yl)imino)methyl propionate; and (E)-3-((3, 5-dibromopyridine-2-yl)imino)methyl propionate is subjected to synthesis so as to obtain 5-bromo-1H-pyrrole [2, 3-b] pyrimidine-3-methyl carboxylate; and 5-bromo-1H-pyrrole [2, 3-b] pyrimidine-3-methyl carboxylate is subjected to synthesis so as to obtain 5-bromo-7-azaindole. Reaction steps are few; operation is convenient; reaction steps are high in yield; industrialized production can be realized; quintal grade production can be realized; and relatively high product yield is ensured.
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Paragraph 0033; 0034; 0037; 0038
(2019/01/08)
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- THERAPEUTIC INHIBITORY COMPOUNDS
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Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma kallikrein. Furthermore, the subject compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.
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Paragraph 00694
(2018/03/26)
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- PYRROLO[2,3-D]PYRIMIDINYL, PYRROLO[2,3-B]PYRAZINYL, PYRROLO[2,3-B]PYRIDINYL ACRYLAMIDES AND EPOXIDES THEREOF
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The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3- b]pyrazinyl,and pyrrolo[2,3-b]pyridinyl acrylamides, epoxides,and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention
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Page/Page column 150
(2016/11/21)
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- NEW DERIVATIVES OF 5-ARYL-1H-PYRROLO [2, 3B] PYRIDINE-3-CARBOXAMIDE OR 5-ARYL-1H-PYRROLO [2, 3B] PYRIDINE-3-CARBOXYLIC ACID
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The present invention relates to new compounds of formula I as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containin
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Page/Page column 21-22
(2008/06/13)
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