- SHP2 PHOSPHATASE INHIBITORS AND METHODS OF MAKING AND USING THE SAME
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The disclosure is in part directed to crystalline forms of (R)-1′-(3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-3H-spiro[benzofuran-2,4′-piperidin]-3-amine, its salt, and variants thereof.
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Paragraph 0177; 0189-0190
(2021/04/02)
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- SHP2 PHOSPHATASE INHIBITORS AND METHODS OF USE THEREOF
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The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.
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Paragraph 0165
(2019/10/15)
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- PYRAZOLO[3,4-B]PYRAZINE DERIVATIVES AS SHP2 PHOSPHATASE INHIBITORS
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The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the invention. The present invention further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds ad compositions of the invention.
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Paragraph 0127; 0128; 0131
(2018/05/24)
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- 6 SUBSTITUTED 2-HETEROCYCLYLAMINO PYRAZINE COMPOUNDS AS CHK-1 INHIBITORS
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The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, their synthesis, and their use as CHK-1 inhibitors.
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Page/Page column 111-112
(2010/04/03)
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- Substituted imidazolylmethyl pyridine and pyrazine deriviatives GABAa receptor ligands
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Substituted imidazolylmethyl pyridine and pyrazine derivatives that bind to GABAA receptors are provided. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).
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- Metalation of diazines IV. Lithiation of sym-disubstituted pyrazines
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Conditions for the metalation of 2,6-dichloro- and 2-6-dimethoxy-pyrazine are defined and the lithio-derivatives are shown to react with some electrophiles.A convenient synthesis of a diazaxanthone from the lithio-derivative of the dichloro-compund is des
- Turck, A.,Trohay, D.,Mojovic, L.,Ple, N.,Queguiner, G
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p. 301 - 310
(2007/10/02)
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