- RHO KINASE INHIBITORS
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The present invention relates to inhibitors of ROCK1 and ROCK2, which may be selective for ROCK2, and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and/or ROCK2. Also provided are treatments combining inhibitors of ROCK1 and/or ROCK2 with statins.
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Page/Page column 178
(2010/10/03)
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- RHO KINASE INHIBITORS
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The present invention relates to inhibitors of ROCKl and R0CK2, which may be selective for R0CK2, and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCKl and/or R0CK2. Also provided are treatments combining inhibitors of ROCKl and/or R0CK2 with statins.
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Page/Page column 183
(2008/12/05)
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- PHARMACOKINETICALLY IMPROVED COMPOUNDS
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The present invention relates to inhibitors of ROCKl and R0CK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCKl and or R0CK2 that are useful for the treatment of disease.
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- Studies Directed Towards Total Syntheses of the Tropoloisoquinoline Alkaloids Grandirubrine and Imerubrine. Part 2. Thermolysis of 8,9-Dihydro-2-hydroxy-3,10,11,12-tetramethoxyisoquinobenzotriazin-7-ium Chloride: Competitive Modes of Cyclisa
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Thermolysis of the title compound 8 produced not only the expected azafluoranthene 7 but also the regioisomeric compound 23 and its dihydro counterpart 22.A mechanism for the formation of compounds 7, 22 and 23 from precursor 8 has been advanced.Reaction
- Banwell, Martin G.,Hamel, Ernest,Ireland, Neil K.,Mackay, Maureen F.,Serelis, Algirdas K.
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p. 1905 - 1912
(2007/10/02)
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- Synthesis and identification of the major metabolites of prazosin formed in dog and rat
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The 6 O demethyl and 7 O demethyl analogues of the new antihypertensive drug prazosin [2 [4 (2 furoyl) piperazin 1 yl] 4 amino 6,7 dimethoxyquinazoline hydrochloride] have been unequivocally synthesized via separate ten step reaction sequences starting from isovanillin and vanillin, respectively. The 6 O demethyl derivative was found to be identical with the major prazosin metabolite formed in dog and rat, while the 7 O demethyl derivative was identical with another, less prevalent but significant metabolite. Two minor metabolites of prazosin, 2 (1 piperazinyl) 4 amino 6,7 dimethoxyquinazoline and 2,4 diamino 6,7 dimethoxyquinazoline, are also described. All four metabolites are less potent blood pressure lowering agents in dogs than prazosin but may contribute to its antihypertensive effect, since they account for a major portion of the administered dose.
- Althuis,Hess
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p. 146 - 149
(2007/10/05)
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