- BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF
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Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents.
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Paragraph 0426
(2016/10/04)
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- ARYL LACTAM KINASE INHIBITORS
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The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
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Page/Page column 92
(2015/11/02)
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- TRIAZOLOPYRIDINE COMPOUND, AND ACTION THEREOF AS PROLYL HYDROXYLASE INHIBITOR OR ERYTHROPOIETIN PRODUCTION-INDUCING AGENT
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The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]: wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as well as a prolyl hydroxylase inhibitor or erythropoietin production-inducing agent containing the compound. The compound of the present invention shows a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability and is useful as a prophylactic or therapeutic agent for various diseases and pathologies (disorders) caused by decreased production of erythropoietin.
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Page/Page column 27
(2011/04/19)
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- PYRIDO [4,3-d] PYRIMIDIN-4 (3H) -ONE DERIVATIVES AS CALCIUM RECEPTOR ANTAGONISTS
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The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variables R1, R2, R3, R4 and R5 are as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.
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Page/Page column 17
(2008/06/13)
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- Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors
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Tumor angiogenesis is mediated by KDR and other VEGFR and PDGFR kinases. Their inhibition presents an attractive approach for developing anticancer therapeutics. Here, we report a series of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted k
- Dai, Yujia,Hartandi, Kresna,Soni, Niru B.,Pease, Lori J.,Reuter, David R.,Olson, Amanda M.,Osterling, Donald J.,Doktor, Stella Z.,Albert, Daniel H.,Bouska, Jennifer J.,Glaser, Keith B.,Marcotte, Patrick A.,Stewart, Kent D.,Davidsen, Steven K.,Michaelides, Michael R.
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p. 386 - 390
(2008/04/03)
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- Novel kinase inhibitors
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Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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Page/Page column 18
(2008/06/13)
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- Strategies for the selective functionalization of dichloropyridines at various sites
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Whereas 2,3-dichloropyridine and 2,5-dichloro-4-(lithiooxy)-pyridine undergo deprotonation exclusively at the 4- and 2-positions, respectively, optional site selectivity can be implemented with 2,5- and 3,4-dichloropyridine (which are attacked, depending on the choice of the reagents, at either the 4- or 6- and either the 2- and 5-positions, respectively). Upon treatment with lithium diisopropylamide, 2,4-dichloro-3-iodopyridine, 3,5-dichloro-4-bromopyridine and 2,6-dichloro-3-iodopyridine afford 5-, 2- and 4-lithiated intermediates, but the latter isomerize instantaneously to species in which lithium and iodine have swapped places, the driving force being the low basicity of C-Li bonds when flanked by two neighboring halogens.
- Marzi, Elena,Bigi, Anna,Schlosser, Manfred
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p. 1371 - 1376
(2007/10/03)
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