- AMINO-ETHYL-AMINO-ARYL (AEAA) COMPOUNDS AND THEIR USE
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The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain amino-ethyl-amino-aryl (AEAA) compounds which, inter alia, inhibit protein kinase D (PKD) (e.g., PKD1, PKD2, PKD3). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKD, and in the treatment of diseases and conditions that are mediated by PKD, that are ameliorated by the inhibition of PKD, etc., including proliferative conditions such as cancer, etc.
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Page/Page column 144
(2009/10/06)
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- Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives: new classes of dopamine receptor subtype specific ligands
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Disclosed are compounds of the formula: wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substitutents which may togther form ring structutes; m is zero, one or two; and R5 and R6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
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- CERTAIN AMINOMETHYL PHENYLIMIDAZOLE DERIVATIVES; AND 4-ARYL SUBSTITUTED PIPERAZINYL AND PIPERIDINYLMETHYL PHENYLIMIDAZOLE DERIVATIVES; A NEW CLASS OF DOPAMINE RECEPTOR SUBTYPE LIGANDS
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This invention encompasses compounds of the formulas: STR1 where R. sub.1 R 3, R 4, R 6, X, Y, and Z are T are variables; andM is STR2 where R 2 is a variable; or R. sub.1 and R. sub.2 together may represent--(CH 2) n1 where n 1 is 1, 2, or 3.P
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- 4-ARYL SUBSTITUTED PIPERAZINYLMETHYL PHENYLIMIDAZOLE DERIVATIVES; A NEW CLASS OF DOPAMINE RECEPTOR SUBTYPE SPECIFIC LIGANDS
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This invention encompasses compounds of the formulas: STR1 where R. sub.1 R 3, R 4, R 6, X, Y, and Z are T are variables; andM is STR2 where R 2 is a variable; or R. sub.1 and R. sub.2 together may represent--(CH 2) n 1 where n 1 is 1, 2, or 3.
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- 2-Phenyl-4-(aminomethyl)imidazoles as Potential Antipsychotic Agents. Synthesis and Dopamine D2 Receptor Binding
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A series of 2-phenyl-4-(aminomethyl)imidazoles were designed as conformationally restricted analogs of the dopamine D2 selective benzamide antipsychotics.The title compounds were synthesized and tested for blockade of YM-09151 binding in cloned African green monkey dopamine D2 receptor preparations.The binding affinity data thus obtained were compared against that of the benzamides and a previously described series of 2-phenyl-5-(aminomethyl)pyrroles.
- Thurkauf, Andrew,Hutchison, Alan,Peterson, John,Cornfield, Linda,Meade, Robin,et al.
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p. 2251 - 2255
(2007/10/02)
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- Certain aminomethyl phenylimidazole derivatives; a class of dopamine receptor subtype specific ligands
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This invention encompasses compounds of the formula: STR1 where X, Y, Z, T, R1, R3, R4, and R5 are variables representing various organic and inorganic substituents; M is STR2 R2 and R6 rep
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