Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, m, n and q are defined as in the specification, and the pharmaceutically acceptable salts thereof. The compounds have calcium entry blocking activity with selectivity for cerebral blood vessels, and have protective activity against some of the deleterious effects resultant upon cerebral ischemia.

Abstract: Piperazine derivatives, particularly ranolazine, are useful for treatment of tissues experiencing a physical or chemical insult, and specifically for treating cardioplegia, hypoxic and/or reperfusion injury to cardiac or skeletal muscle or brain tissue, and for use in transplants.

Abstract: Compounds of the formula: ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification or a pharmaceutically acceptable acid addition salt or N-oxide thereof, are calcium and sodium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism, and also for treatment of spinal injuries.

Abstract: The invention provides a new and efficient process for preparing 2,4(5)-substituted or 1,2,4-substituted imidazole derivatives.The invention also provides a process for preparing substituted aminoalkylimidazole derivatives, useful for the treatment of mammals having a variety of disease states, including stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism, and the like.

Abstract: The invention provides a new and efficient process for preparing 2,4(5)-substituted or 1,2,4-substituted imidazole derivatives.The invention also provides a process for preparing substituted aminoalkylimidazole derivatives, useful for the treatment of mammals having a variety of disease states, including stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism, and the like.The invention also relates to novel aminoalkylimidazole compounds.

Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives and the pharmaceutically acceptable salts thereof are useful for treating mammals having any of a variety of disease states. These disease states include: 1) diseases treated by direct neuronal protection, including focal and global ischemia, spinal injuries, and head trauma, and neurological diseases including Alzheimer's and Huntington's chorea; 2) uraemic and hyponatraemic encephalopathy; 3) diseases treated by diuresis; 4) diseases treated by calcium channel antagonism, including cardiovascular diseases (i.e. hypertension, angina, stable and unstable angina, Prinzmetal angina, arrhythmia, thrombosis, embolism, and congestive heart failure including chronic or acute cardiac failure), diseases characterized by ischemia of lower legs due to peripheral vascular disease (e.g., intermittent claudication), diseases characterized by spasms of smooth muscle (i.e.

Abstract: 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 oneor two; andq is zero, one, two, or three;and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.

Abstract: 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; andq is zero, one, two, or three;and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.

Abstract: A pharmaceutical formulation suitable for parenteral (preferably intravenous) administration includes an effective amount of 1-diphenylmethyl-4-[(2-(4-methylphenyl)-5-methyl-1H-imidazol-4-yl)methyl]p iperazine and a suitable amount of an acid to generate a pharmaceutically acceptable salt having a pH above about 3.0 and a solubility above about 4.0 mg/ml. The intravenous formulation optionally includes a suitable tonicifier in a quantity sufficient to achieve isotonicity with body fluids. The salt is formed in situ during the formulation process. The salt of tartaric acid is preferred; suitable salts for lower concentration dosages are the citric acid and methane sulphonic acid salts.

Abstract: 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.

Abstract: 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; andq is zero, one, two, or three;and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.

Abstract: A pharmaceutical formulation suitable for parenteral (preferably intravenous) adminstration includes an effective amount of 1-diphenylmethyl-4-[(2-(4-methylphenyl)-5-methyl-1H-imidazol-4-yl)methyl]p iperazine and a suitable amount of an acid to generate a pharmaceutically acceptable salt having a pH above about 3.0 and a solubility above about 4.0 mg/ml. The intravenous formulation optionally includes a suitable tonicifier in a quantity sufficient to achieve isotonicity with body fluids. The salt is formed in situ during the formulation process. The slat of tartaric acid is preferred; suitable salts for lower concentration dosages are the citric acid and methane sulphonic acid salts.

Abstract: 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 lower alkyl, hydroxy, or hydrogen;R.sup.4 aryl or hydrogen;R.sup.5 aryl or hydrogen;m is two or three;n is zero, one or two,provided that when R.sup.3 hydroxy, n is one or two; andq is zero, one, two, or three;and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilipsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.

Abstract: 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; andq is zero, one, two, or three;and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.