- AMINO-QUINOLINES AS KINASE INHIBITORS
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Disclosed are compounds having the formula:wherein R 1 , R 2 , R 3 and Z are as defined herein, and methods of making and using the same.
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Page/Page column 70; 71
(2018/06/22)
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- AMINO-QUINOLINES AS KINASE INHIBITORS
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Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
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Page/Page column 81; 82
(2018/05/15)
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- AMINO-QUINOLINES AS KINASE INHIBITORS
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Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
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Paragraph 0139
(2016/10/31)
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- COMBINATION THERAPIES FOR TREATMENT OF CANCER
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Combination therapies for treatment of cancers associated with mutations in the KRAS gene are provided. Compositions comprising therapeutic agents for treatment of cancers associated with mutations in the KRAS gene are also provided.
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Page/Page column 248; 249
(2016/04/09)
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- INHIBITORS OF KRAS G12C
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Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
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Page/Page column 196
(2015/04/28)
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- Design, synthesis, and evaluation of novel 3,6-diaryl-4- aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2
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Agonists of somatostatin receptor subtype 2 (sst2) have been proposed as therapeutics for the treatment of proliferative diabetic retinopathy and exudative age-related macular degeneration. An HTS screen identified 2-quinolones as weak agonists of sst2, and these were optimized to provide small molecules with sst2 binding and functional potency comparable to peptide agonists. Agonist 21 was shown to inhibit rat growth hormone secretion following systemic administration and to inhibit ocular neovascular lesion formation after local administration.
- Wolkenberg, Scott E.,Zhao, Zhijian,Thut, Catherine,Maxwell, Jill W.,McDonald, Terrence P.,Kinose, Fumi,Reilly, Michael,Lindsley, Craig W.,Hartman, George D.
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supporting information; experimental part
p. 2351 - 2358
(2011/06/17)
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- Controlled derivatization of polyhalogenated quinolines utilizing selective cross-coupling reactions
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Straightforward procedures for the derivatization of tri- and tetrahalogenated quinolines utilizing sequential selective Pd-catalyzed cross-coupling reactions are described. Taking advantage of intrinsic halide reactivity, substrate control, and appropria
- Brad Nolt,Zhao, Zhijian,Wolkenberg, Scott E.
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p. 3137 - 3141
(2008/09/20)
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- SOMATOSTATIN AGONISTS
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This invention relates to compounds which are agonists of somatostatin and selective toward somatostatin receptor subtype SSTR2. The compounds are useful in the treatment and prevention of diabetes, and diabetes-related pathologies, including retinopathy,
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Page/Page column 19; 20
(2008/12/05)
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