1237535-76-0Relevant academic research and scientific papers
CHIRAL SYNTHESIS OF FUSED BICYCLIC RAF INHIBITORS
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Paragraph 0402; 0409-0410; 0437; 0451-0453, (2022/02/09)
The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitor enantiomers of formula (I), (Ia), (Ib), (II), (IIa), or (IIb), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, with high enantiomeric excess (%ee). The disclosure also relates to method of using the compound of formula (I), (Ia), (Ib), (II), (IIa), or (IIb), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
FUSED BICYCLIC RAF INHIBITORS AND METHODS FOR USE THEREOF
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Paragraph 0241-0243, (2022/02/09)
The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method o
FARNESOID X RECEPTOR AGONISTS AND USES THEREOF
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Paragraph 00454, (2020/04/25)
Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
STABLE SOLID DISPERSIONS OF B-RAF KINASE DIMER INHIBITOR, METHODS OF PREPARATION, AND USES THEREFOR
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Paragraph 0179-0180, (2020/08/13)
Disclosed herein is a physically stable solid dispersion comprising Compound 1, i.e., the B-RAF kinase dimer inhibitor 1- ( (1S, 1aS, 6bS) -5- ( (7-oxo-5, 6, 7, 8-tetrahydro-1, 8-naphthyridin-4-yl) oxy) -1a,6b-dihydro-1H-cyclopropa [b] benzofuran-1-yl) -3- (2, 4, 5-trifluorophenyl) urea and a specific stabilizing polymer, the method for preparing the same, and the uses of the solid dispersion. Also disclosed herein is the crystalline form of Compound 1.
Method suitable for large-scale production of B-RAF kinase dimer inhibitor
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Paragraph 0053-0054, (2020/08/18)
The invention relates to a method for large-scale production of a B-RAF kinase dimer inhibitor 1-((1S, 1aS, 6bS)-5-((7-oxo-5, 6, 7, 8-tetrahydro-1, 8-diazanaphthalene-4-yl) oxy)-1a, 6b-dihydro-1H-cyclopropyl [b] benzofuran-1-yl)-3-(2, 4, 5- trifluorophenyl) urea (hereinafter sometimes referred to as a compound 1). The method enables impurities or by-products to be controlled to 0.05% or less without the use of expensive column chromatography operations. Thus, the method greatly reduces cost and is suitable for large-scale production.
Stable crystalline form A of B-RAF kinase dimer inhibitor
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Paragraph 0059; 0060-0061, (2020/08/18)
The invention relates to a stable crystalline form A of a B-RAF kinase dimer inhibitor 1-((1S, 1aS, 6bS)-5-((7-oxo-5, 6, 7, 8-tetrahydro-1, 8-diazanaphthalene-4-yl) oxy)-1a, 6b-dihydro-1H-cyclopropyl[b] benzofuran-1-yl)-3-(2, 4, 5- trifluorophenyl) urea (hereinafter sometimes referred to as a compound 1), a preparation method of the crystalline Form A and therapeutic use of the crystalline Form A.
Amorphous B-RAF kinase dimer inhibitor
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Paragraph 0069; 0070, (2020/08/18)
The invention relates to a stable amorphous form of a B-RAF kinase dimer inhibitor 1-((1S, 1aS, 6bS)-5-((7-oxo-5, 6, 7, 8-tetrahydro-1, 8-diazanaphthalene-4-yl) oxy)-1a, 6b-dihydro-1H-cyclopropyl [b]benzofuran-1-yl)-3-(2, 4, 5- trifluorophenyl) urea (hereinafter sometimes referred to as a compound 1), a prepration method of the amorphous compound and therapeutic use of the amorphous compound.
NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS
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Page/Page column 186, (2016/04/20)
This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their 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.
TETRAHYDROIMIDAZOPYRIDINE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
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Page/Page column 91, (2015/06/25)
A series of substituted 5,6,7,8-tetrahydroimidazo[l,2-α]pyridine derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory di
IMIDAZOPYRIDINE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
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Page/Page column 134, (2014/02/15)
A series of imidazo[l,2-a]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
