- Propionic Acid Derivatives and Methods of Use Thereof
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Provided herein are compounds and pharmaceutical compositions of formula I where R1, R2, R3, R4, R5 and R6 are as described herein. Also provided pharmaceutically acceptable salts or stereoisomers of these compounds. In addition methods are provided for inhibiting the binding of an integrin to treat various pathophysiological conditions.
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Paragraph 1862; 1863
(2018/11/21)
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- ANTIMICROBIAL AGENTS AND SCREENING METHODS
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Disclosed herein are antibacterial and antimicrobial compositions and methods of use. Also disclosed are screening assays for identification of an agent that specifically inhibits DsbB or bVKOR. Such methods are useful, for example, in identifying antibacterial and antimicrobial agents and compositions.
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Page/Page column 115
(2015/11/10)
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- 2-Cyanopyridazin-3(2H)-ones: Effective and chemoselective electrophilic cyanating agents
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2-Cyanopyridazin-3(2H)-ones are novel, effective, selective and electrophilic cyanating agents. A variety of amino, thiol and carbon nucleophiles are chemoselectively N-, S- or C-cyanated in excellent yield using 2-cyanopyridanzin-3(2H)-ones in water or tetrahydrofuran.
- Kim, Jeum-Jong,Kweon, Deok-Heon,Cho, Su-Dong,Kim, Ho-Kyun,Jung, Eun-Young,Lee, Sang-Gyeong,Falck,Yoon, Yong-Jin
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p. 5889 - 5894
(2007/10/03)
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- N-phenyl-4-pyrazolo[1,5-6]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy
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Glycogen synthase kinase 3 regulates glycogen synthase, the rate-determining enzyme for glycogen synthesis. Liver and muscle glycogen synthesis is defective in type 2 diabetics, resulting in elevated plasma glucose levels. Inhibition of GSK-3 could potentially be an effective method to control plasma glucose levels in type 2 diabetics. Structure-activity studies on a N-phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine series have led to the identification of potent and selective compounds with good cellular efficacy. Molecular modeling studies have given insights into the mode of binding of these inhibitors. Since the initial leads were also potent inhibitors of CDK-2/CDK-4, an extensive SAR was performed at various positions of the pyrazolo[1,5-b] pyridazin core to afford potent GSK-3 inhibitors that were highly selective over CDK-2. In addition, these inhibitors also exhibited very good cell efficacy and functional response. A representative example was shown to have good oral exposure levels, extending their utility in an in vivo setting. These inhibitors provide a viable lead series in the discovery of new therapies for the treatment of type 2 diabetes.
- Tavares, Francis X.,Boucheron, Joyce A.,Dickerson, Scott H.,Griffin, Robert J.,Preugschat, Frank,Thomso, Stephen A.,Wang, Tony Y.,Zhouf, Hui-Qiang
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p. 4716 - 4730
(2007/10/03)
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- Direct functionalization of 4,5-dichloropyridazin-6-one
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Direct functionalization of 4,5-dichloropyridazin-6-one with some nucleophiles in seven solvents gave regioselectively 5-halo- 4-substituted-pyridazin-6-ones as main product. Reaction of 4,5- dichloropyridazin-6-one with 2-mercaptopyrimidine (2 equivalents) also afforded 4,5-di(pyrimidin-2-ylsulfanyl)pyridazin-6-one as the main product.
- Chung, Hyun-A,Kweon, Deok-Heon,Kang, Young-Jin,Park, Jung-won,Yoon, Yong-Jin
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p. 905 - 910
(2007/10/03)
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- Pyridazines with Heteroatom Substituents in Position 3 and 5, Part 1: 5-Hydroxy-3(2H)-pyridazinone and Its Derivatives
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The synthesis of the title compound 7 was achieved starting with mucochloric acid via the pyridazinones 1,2 and 6.The electrolytic ionisation constants for 7 were found to be 4.81 (+/-0.03) and -0.3 (+/-0.3).Crystal structure analyses were performed for 7 and its "fixed" derivatives 6 and 9. - Keywords.Synthesis of 5-methoxy- and 5-hydroxy-3(2H)-pyridazinones; pKa Values of 5-hydroxy-3(2H)-pyridazinone; Crystal structure of 3(2H)-pyridazinones.
- Wagner, Ulrike Gabriella,Kratky, Christoph,Kappe, Thomas
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p. 329 - 342
(2007/10/02)
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