- SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE
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The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.
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Page/Page column 229
(2020/12/11)
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- Neurotrophic factor tyrosine kinase receptor inhibitor
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The invention provides a neurotrophic factor tyrosine kinase receptor inhibitor. The tyrosine kinase receptor inhibitor provided by the invention has a tricyclic parent core structure, can inhibit theactivity of Trk kinase and can be used for treating mammalian diseases mediated by the Trk kinase.
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Paragraph 0447; 0449-0451
(2018/05/30)
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- Fragment-based discovery of JAK-2 inhibitors
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Fragment-based hit identification coupled with crystallographically enabled structure-based drug design was used to design potent inhibitors of JAK-2. After two iterations from fragment 1, we were able to increase potency by greater than 500-fold to provide sulfonamide 13, a 78-nM JAK-2 inhibitor.
- Antonysamy, Stephen,Hirst, Gavin,Park, Frances,Sprengeler, Paul,Stappenbeck, Frank,Steensma, Ruo,Wilson, Mark,Wong, Melissa
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scheme or table
p. 279 - 282
(2009/04/16)
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- 5-HETEROARYL SUBSTITUTED INDAZOLES AS KINASE INHIBITORS
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The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
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Page/Page column 166
(2009/01/24)
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- 6-AMINOIMIDAZO[1,2-b]PYRIDAZINE ANALOGS AS RHO KINASE INHIBITORS FOR THE TREATMENT OF RHO KINASE-MEDIATED DISEASES AND CONDITIONS
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Methods for using 6-aminoimidazo[1,2-b]pyridazine analogs are disclosed herein to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of 6-aminoimidazo[1,2-b]pyridazine analogs, are disclosed herein.
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Page/Page column 21
(2008/12/06)
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- Thiazole compounds and methods of use
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The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
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Page/Page column 47
(2008/06/13)
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- GLUCOKINASE ACTIVATORS
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Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of wherein the variables are as defined herein.
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Page/Page column 87-88
(2010/11/27)
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- KINASE INHIBITORS
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A compound having the general structure of Formula (I) or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as immunodeficiencies, cancers, cardiovascular diseases, endocrine disorders, Parkinson's disease, metabolic diseases, tumorigenesis, Alzheimer's disease, heart disease, diabetes, neurodegeneration, inflammation, kidney disease, atherosclerosis and airway disease.
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Page/Page column 91
(2008/06/13)
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- Kinase inhibitors
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Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
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- 3-Aminoindazole derivatives
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.Iadd.Pharmaceutical compositions having muscle relaxant and analgesic activity containing 3-aminoindazoles..Iaddend.
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