- POTASSIUM CHANNEL MODULATORS
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Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with potassium channels. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with potassium channels.
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Paragraph 0398; 0403; 0405; 0408
(2018/01/14)
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- Pyridinylpyrimidines selectively inhibit human methionine aminopeptidase-1
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Cellular protein synthesis is initiated with methionine in eukaryotes with few exceptions. Methionine aminopeptidases (MetAPs) which catalyze the process of N-terminal methionine excision are essential for all organisms. In mammals, type 2 MetAP (MetAP2)
- Zhang, Pengtao,Yang, Xinye,Zhang, Feiran,Gabelli, Sandra B.,Wang, Renxiao,Zhang, Yihua,Bhat, Shridhar,Chen, Xiaochun,Furlani, Manuel,Amzel, L. Mario,Liu, Jun O.,Ma, Dawei
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p. 2600 - 2617
(2013/06/27)
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- INHIBITORS OF HUMAN METHIONINE AMINOPEPTIDASE 1 AND METHODS OF TREATING DISORDERS
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Described herein are novel pyrimidine-pyridine compounds, methods of inhibiting methionine aminopeptidase and treating disorders (or symptoms thereof) associated with methionine aminopeptidase, wherein a compound of the invention is administered to a subject.
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Page/Page column 50-51
(2009/06/27)
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- 4-Amino-2-(pyridin-2-yl)pyrimidine as microbicidal active substances
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There are described compounds of formula whereinR1 and R2 are each independently of the other hydrogen; unsubstituted or mono- or polyhalo-substituted C1-C20alkyl, C1-C20alkoxy, C2-C20alkenyl, C2-C20alkynyl, C3-C18cycloalkyl, C3-C7cycloalkyl-C1-C20alkyl; hydroxy; C1-C6alkoxy-C1-C20alkyl; carboxy; C1-C6alkyloxycarbonyl; cyano; mono- or di-C1-C20alkylamino; C1-C6alkylamino-C1-C20alkyl; halogen; phenyl; unsubstituted or C1-C5alkyl-, halo- or hydroxy-substituted phenyl-C1-C20alkyl, phenoxy or phenyl-C1-C20alkoxy; or R1 and R2 form a polymethylene chain of formula -(CH2)m- wherein m = 2-12;R3 is unsubstituted C7-C20alkyl; or amino-, hydroxy-, carboxy- or C1-C6alkyloxycarbonyl-substituted C2-C20alkyl; C8-C18cycloalkyl; C8-C20alkenyl; C8-C20alkynyl; C3-C7cycloalkyl-C8-C20alkyl; C1-C4alkoxy-C8-C20alkyl; R7R8N-C7-C20alkyl; phenyl; phenyl-C1-C4alkyl; or phenyl-C1-C4alkoxy;R4 is hydrogen; unsubstituted or C1-C5alkyl-, halo- or hydroxy-substituted C1-C20alkyl, C2-C20alkenyl, C2-C20alkynyl, C3-C20cycloalkyl, C3-C7cycloalkyl-C1-C20alkyl, C1-C20alkoxy-C1-C6alkyl or R7R8N-C1-C20alkyl, phenyl, phenyl-C1-C20alkyl or phenoxy-C1-C20alkyl;R5 and R6 are each independently of the other hydrogen; C1-C20alkyl; C2-C20alkenyl; C2-C20-alkynyl; C3-C18cycloalkyl; C3-C7cycloalkyl-C1-C20alkyl; hydroxy; C2-C20alkoxy; C1-C6alkoxy-C1-C20alkyl; carboxy; C1-C6alkyloxycarbonyl; cyano; nitro; C1-C20alkylamino; C1-C20alkylaminoalkyl; C1-C20haloalkyl; C1-C20haloalkoxy; halogen; unsubstituted or C1-C5alkyl-, halo- or hydroxy-substituted phenyl, phenoxy or phenyl-C1-C20alkyl or phenyl-C1-C20alkoxy; or R5 and R6 together form a polymethylene chain of formula -(CH2)m- wherein m = 2-12; andR7 and R8 are each independently of the other hydrogen; C1-C20alkyl; C3-C20alkenyl; C3-C20-alkynyl; C3-C7cycloalkyl; C3-C20cycloalkyl-C1-C4alkyl; phenyl; or phenyl-C1-C4alkyl. They are suitable for the antimicrobial treatment of surfaces, as antimicrobial active substances against gram-positive and gram-negative bacteria.
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- Unfused Heterobicycles as Amplifiers of Phleomycin.I Some Pyridinyl- and Pyrazolyl-pyrimidines, Bithiazoles and Thiazolylpyridines
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Syntheses are reported for some simple derivatives of 2-(pyridin-2'-yl)pyrimidine; 4-(pyrazol-1'-yl)pyrimidine; 4-(pyrazol-4'-yl)pyrimidine; 4,5'-bithiazole; 2-, 3-, and 4-(thiazol-4'-yl)pyridine and 2-, 3-, and 4-(thiazol-2'-yl)pyridine.Biological activities, as amplifiers of phleomycin against in vitro cultures of Escherichia coli, are tabulated and discussed.
- Brown, Desmond J.,Cowden, William B.,Grigg, Geoffrey W.,Kavulak, Diana
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p. 2291 - 2298
(2007/10/02)
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