Substituted imidazolyl-alkyl-piperazine and -diazepine derivatives

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United States of America Patent

PATENT NO 5043447
SERIAL NO

07260969

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Abstract

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Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R.sup.1 is aryl, lower alkyl, cycloalkyl or hydrogen; R.sup.2 is aryl, lower alkyl or hydrogen; R.sup.3 is lower alkyl, hydroxy, or hydrogen; R.sup.4 is aryl or hydrogen; R.sup.5 is aryl or hydrogen; m is two or three; n is zero, one or two, provided that when R.sup.3 is hydroxy, n is one or two; and q is zero, one, two, or three; and the pharmaceutically acceptable salts thereof, are useful for treating mammals having any of a variety of disease states including: diseases treated by direct neuronal protection, such as ischemia including focal and global ischemia, spinal injuries, head trauma, and neurological diseases such as Alzheimer's and Huntington's chorea; diseases treated by inhibition of sodium ion, such as uremic and hyponatremic encephalopathy; and diseases treated with calcium channel antagonists, including: diseases treated by inhibiting cerebrovascular vasospasm and by cerebrovascular vasodilation, such as migraine, stroke, vasospasm due to subarachnoid hemorrhage, epilepsy or epileptic psychotic symptoms, and cerebrovascular ischemia induced by cocaine abuse; and cardiovascular diseases, such as hypertension, angina, stable and unstable angina, Prinzmetal angina, arrhythmia, thrombosis, embolism, and congestive heart failure such as chronic or acute cardiac failure; and ischemia of lower legs due to peripheral vascular disease, e.g., intermittent claudication; spasms of smooth muscle: such as the ureter, the bladder, uterine cramps, diuresis, and irritable bowel syndrome; and uses during surgery: such as bypass grafts, angiography, angioplasty, organ preservation during transplant, hypertensive crisis, or post operative hypertension.

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SYNTEX PHARMACEUTICALS LTD SYNTEX HOUSE ST IVERS ROAD MAIDENHEAD BERKSHIRE SL6 1RD ENGLAND A CORP OF UNITED KINGDOMNot Provided

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Alps, Brian J Linlithgow, GB6 9 94
Beranger, Serge Bretigny-Sur-Cedres, FR 10 50
Dow, Robert J Edinburgh, GB6 3 57
Lee, Chi-Ho Palo Alto, CA 22 93
Macfarlane, Calum B Linlithgow, GB6 6 170
Pascal, Jean C Cachan, FR 9 73
Pinhas, Henri Paris, FR 16 100
Whiting, Roger L Los Altos, CA 11 95

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