Abstract: Fused tetracyclic benzodiazepines of the formula (I): ##STR1## where R.sup.1 is a cyclic amine such as 1-piperazine and R.sup.2 is H or a substituent as defined herein are useful as LHRH antagonizing agents. Also, methods for their synthesis, intermediates used in such synthesis, methods for use as medicaments and pharmaceutical compositions are described.
Abstract: Pyrrolidinylidene compounds substituted at the 5-position of the following formula (I): ##STR1## wherein R=H, alkyl or alkanoyl, and their use as hypoglycemic agents, e.g. in the treatment of diabetes, in a manner similar to linogliride.
Type:
Grant
Filed:
August 29, 1986
Date of Patent:
June 2, 1987
Assignee:
McNeilab, Inc.
Inventors:
Joyce E. Epps, Kung-Tat Ng, Robert W. Tuman, Wu-Nan Wu
Abstract: A filtration unit comprising a filtration media sub-unit secured in an outer frame. The sub-unit comprises a fibrous filtration media enclosed in an inner frame having an upstream frame element and a downstream frame element. Each frame element has longitudinal and transverse struts and the intersections of these struts are in a single plane on the side of the frame elements which contact the filtration media. In one embodiment the filtration unit is enclosed in a sock of knit fabric; in another embodiment, there is a piece of knit fabric between the outer frame and the downstream frame element of the inner frame. The longitudinal struts may have portions which are perpendicular to and project beyond the principal plane of the periphery of the downstream frame element. If such perpendicularly projecting portions are provided, they are preferably arcuate in configuration.
Abstract: Four decapeptides found to be analgesics and have antagonist activity to Neurokinin B which is also known as Neuromedin K. The decapeptides are of the following formula (I):A.sup.1 -D-Pro.sup.2 -His.sup.3 -D.sup.4 -Phe.sup.5 -D-Trp.sup.6 -Val.sup.7 -D-Trp.sup.8 -Leu.sup.9 -Nle.sup.10 -NH.sub.2 (I)wherein A.sup.1 and D.sup.4 are Asp or D-Asp amino acids. Also described is an HPLC separation method using piperidine.
Abstract: A dosage of N-(4-hydroxyphenyl)retinamide, also known as fenretimide, of the following formula: ##STR1## with increased bioavailability comprising corn oil and a non-ionic surfactant. The formulation if useful in the treatment of breast or bladder cancer, psoriasis and acne.
Abstract: Heterocyclic acetylenes of the formula (I): ##STR1## wherein Y is alkyl, alkoxy, alkoxyalkyl, chloro, fluoro, bromo or carboxamidoalkyl and R.sup.1 is hydrogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl, chloro, fluoro or dialkylamino, m is 0-2, R.sup.2 is branched alkyl and Het is an aromatic heterocycle. The acetylenes are useful in treating hypertension and/or angina.
Abstract: Acetylenes of the formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2 q, Alk, R.sup.3, n and R.sup.4 are as defined herein and Ar.sup.1 and Ar.sup.2 are aromatic, including the salts and ammonium derivatives of formula (I), in treating angina, hypertension and cardiac arrhythmias. Pharmaceutical compositions, methods of use and synthesis and novel intermediates are also part of the invention.
Abstract: Ureas of the formula (I): ##STR1## where R.sup.1 =alkoxy or alkylthio; R.sup.2 =alkyl; and Ar=substituted or unsubstituted phenyl, useful as anxiolytic agents as well as intermediates useful in the synthesis.
Type:
Grant
Filed:
May 24, 1985
Date of Patent:
April 14, 1987
Assignee:
McNeilab, Inc.
Inventors:
Chris R. Rasmussen, Frank J. Villani, Jr.
Abstract: An efficient synthesis of quanidines, e.g. of the formula (III), by oxidizing a thiourea, e.g. of the following formula (II): ##STR1## with H.sub.2 O.sub.2 and a molybdenum catalyst to yield an aminoiminomethane sulfonic acid which can then be reacted with an amine followed by optional transamination steps.
Type:
Grant
Filed:
May 28, 1986
Date of Patent:
April 7, 1987
Assignee:
McNeilab, Inc.
Inventors:
Cynthia A. Maryanoff, James N. Plampin, Robin C. Stanzione
Abstract: Phenoxypropanol derivatives having a 2-acetylenic moiety on the phenyl group thereof of the following formula (I): ##STR1## and their use as anti-hypertensives, e.g. in man. Also part of the invention are pharmaceutical compositions and intermediates used in the synthesis.
Abstract: Dialkanolamines and nontoxic pharmaceutically-acceptable acid-addition salts of the compounds of the following formula ##STR1## wherein R.sub.1 is hydrogen lower alkyl, or fluoro; R.sub.2 is hydrogen or lower alkyl; R.sub.3 and R.sub.4 are the same or different and selected from the group consisting of hydrogen or lower alkyl or R.sub.3 and R.sub.4 together define a chemical bond directly linking the two alkanol chains so as to form a pyrrolidine ring; Ar, is phenyl or thienyl or phenyl substituted with one to three substituents selected from the group consisting of lower alkyl and halo; and Ar.sub.2 is phenyl and phenyl substituted with one to three substituents selected from the group consisting of lower alkyl and halo which have antidepressant activity.
Abstract: Manually overridable servo controlled valve mechanisms for controlling the flow of fluids through a flexible tube for use in a photoactivatable reagent treatment system wherein photoactivatable reagents, in contact with patient blood cells, are irradiated extracorporeally and then retruned to the patient.
Abstract: A preferred patient blood treatment system for the photoactivation of reagents in contact with a patient's blood employs an infusion pump for adding anti-coagulation reagent to the blood during extracorporeal operations. The infusion pump is preferably driven by a stepper motor and monitored by a periodic photo chopper employing a plurality of sensors. The spacing of the sensors and the spacing of the photo choppers work in concert to detect rotation of the stepper motor and to discriminate such from stutter or other characteristic nonrotational faults associated with stepper motors.
Abstract: Novel 2-amino-4,5-dihydro-1H-imidazole-1-carboxanilides, which are made by reacting 2-amino-4,5-dihydroimidazole with an aryl isocyanate, are made stable to rearrangement when converted to acid addition salt form, and are useful either as antihypertensive agents and/or antisecretary agents, as well as being intermediates to prepare known pharmacologically active N-aryl-N'-(4,5-dihydro-1H-imidazol-2-yl)ureas.
Abstract: Manually overridable servo controlled valve mechanisms for controlling the flow of fluids through a flexible tube for use in a photoactivatable reagent treatment system wherein photoactivatable reagents, in contact with patient blood cells, are irradiated extracorporeally and then returned to the patient.
Abstract: Novel compounds are disclosed, which are derivatives of 1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]-isoquinolines, represented by general formula (I): ##STR1## as well as pharmaceutical compositions and methods for the treatment of depression in warm-blooded animals, e.g., man. Novel intermediates are also part of the invention.
Abstract: Compounds of the following formula (I): ##STR1## wherein Alk is a straight or branched chain alkylene of about 1 to 12 carbons and R.sup.1 is a heterocyclic ring system, have been found to possess potent antisecretory activity and are thus useful in the treatment of hyperacidity.
Abstract: Sulfamates of the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are as herein defined have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and intermediates form part of the present invention.