- MACROCYCLIC AZOLOPYRIDINE DERIVATIVES AS EED AND PRC2 MODULATORS
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The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula (I), or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X1, X2, X3, A1, A2, Y, R1, R2, R3, and R4 are as described herein.
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Paragraph 0975
(2020/10/09)
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- Protein kinase inhibitor and its preparation method and medical application
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The invention provides a compound shown in the structural formula I or its tautomer, mesomer, racemate, enantiomer, diastereoisomer or their mixture, or a pharmaceutically acceptable salt or solvate of the compound shown in the structural formula I or its tautomer, mesomer, racemate, enantiomer, diastereoisomer or their mixture. The ring A, R1, R2, R3 and R4 are defined in the specification. The invention also provides a preparation method of the compound shown in the structural formula I and a use of the compound in preparation of a drug for treating cell proliferative disorder.
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Paragraph 0310-0313
(2017/05/26)
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- PYRIDYLPYRIDONE DERIVATIVE USEFUL AS A RET KINASE INHIBITOR IN THE TREATMENT OF IBS AND CANCER
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This invention relates to a novel compound which is an inhibitor of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing it, to processes for its preparation, and to its use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity. Formula (I)
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Page/Page column 25-26
(2017/09/09)
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- CHEMOKINE RECEPTOR BINDING COMPOUNDS
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The present invention relates to chemokine receptor binding compounds, pharmaceutical compositions and their use. More specifically, the present invention relates to modulators of chemokine receptor activity, preferably modulators of CCR4 or CCR5. In one aspect, these compounds demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
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Page/Page column 51
(2010/11/26)
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