Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines
摘要:
Fourteen 125I-labeled aralkylguanidines were synthesized and evaluated as potential imaging agents for the adrenal medullae and tumors of adrenomedullary origin. These guanidines are radiotracer analogues of guanethidine, an antihypertensive agent thought to mediate neuron blockade by uptake into adrenergic nerves. Dog adrenal medullae were used as a model to test radiotracer affinity for catecholamine storage tissue. Tissue distribution studies revealed that a number of radioiodinated guanidines showed pronounced localization in the adrenal medullae following intravenous injection, in certain cases exceeding that of either (-)-[3H]norepinephrine or [14C]guanethidine. (m-[125I]Iodobenzyl)guanidine (m-IBG, 2b) gave the best combination of high concentration and selectivity. The low adrenomedullary affinity observed with [14C]guanidine and m-[125I]iodobenzylamine demonstrates the uniqueness of the aralkylguanidine structure. Preliminary evidence suggests that 2b is a storage analogue of norepinephrine. [125I]2a is now being used clinically in imaging and radiotherapy of catecholamine tumors, such as pheochromocytoma.
Lactam compounds useful as protein kinase inhibitors
申请人:Blackburn Christopher
公开号:US20060100194A1
公开(公告)日:2006-05-11
The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS
申请人:Blackburn Christopher
公开号:US20120178739A1
公开(公告)日:2012-07-12
The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
[EN] LACTAM COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS<br/>[FR] COMPOSES A BASE DE LACTAME UTILES EN TANT QU'INHIBITEURS DE LA PROTEINE KINASE
申请人:MILLENNIUM PHARM INC
公开号:WO2006041773A2
公开(公告)日:2006-04-20
The present invention provides novel compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A, Re, Rb, Rc, Rd, G1, Y1, and Y2 have the meaning as given in the claims useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.