Abstract: The pyrazoles and pyzazolopyrimidines of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A are as defined herein, have corticotropin releasing factor (CRF) antagonist activity. As such, they are effective in the treatment of a wide range of diseases including stress-related illnesses.

Abstract: A method of blocking N-methyl-D-aspartic acid (NMDA) receptor sites in a mammal in need thereof with an effective NMDA blocking (neuroprotective and antiischemic) amount of 2-piperidino-1-alkanol derivatives and 2-azabicyclo-1-alkanol derivatives and analogs and pharmaceutically acceptable salts thereof; methods of using these compounds in the treatment of stroke, spinal cord trauma, traumatic brain injury, multiinfarct dementia, CNS degenerative diseases such as Alzheimer's disease, senile dementia of the Alzheimer's type, Huntington's disease, Parkinson's disease, epilepsy, amyotrophic lateral sclerosis, pain, AIDS dementia, psychotic conditions, drug addictions, migraine, hypoglycemia, anxiolytic conditions, urinary incontinence and an ischemic event arising from CNS surgery, open heart surgery or any procedure during which the function of the cardiovascular system is compromised.

Abstract: The present invention relates to novel DNA sequences that encode for the branched-chain alpha-ketoacid dehydrogenase complex of an organism belonging to the genus Streptomyces and to novel polypeptides produced by the expression of such sequences. It also relates to novel methods of enhancing the production of natural avermectin, of producing a Streptomyces avermitilis bkd mutant and of producing novel avermectins through fermentation.

Abstract: Compounds of formula: ##STR1## or a biolabile ester thereof, or a pharmaceutically acceptable salt of either,whereinR.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently selected from H or C.sub.1 -C.sub.4 alkyl;R.sup.5 is (CH.sub.2).sub.m SO.sub.2 R.sup.6, (CH.sub.2).sub.m NHSO.sub.2 R.sup.6 or (CH.sub.2).sub.m NHCOR.sup.7 ;R.sup.6 and R.sup.7 are C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 perfluoroalkyl-(CH.sub.2).sub.n, C.sub.3 -C.sub.6 cycloalkyl(CH.sub.2).sub.n, aryl(CH.sub.2).sub.n or heteroaryl(CH.sub.2).sub.n ; orR.sup.6 is NR.sup.8 R.sup.9 ;R.sup.8 is H or C.sub.1 -C.sub.4 alkyl;R.sup.9 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl(CH.sub.2).sub.n, aryl(CH.sub.2).sub.n or heteroaryl(CH.sub.2).sub.n ; orR.sup.8 and R.sup.9 together with the nitrogen atom to which they are attached from a 5- to 7-membered heterocyclic ring;X is CH.sub.2, CHCH.sub.3, C(OH)CH.sub.3, C.dbd.CH.sub.2 or O;m is 0 or 1;n is 0, 1, 2 or 3; andHet is 3- or 4-pyridyl or 1-imidazolyl;are combined thromboxane A.sub.

Abstract: The compounds of the formula ##STR1## wherein A, R.sub.1, R.sub.3, Z and Y are as defined herein, have corticotropin-releasing factor (CRF) antagonist activity. They are useful in the treatment of illnesses induced by CRF, such as stress and anxiety related disorders.

Abstract: Compounds of the formula: ##STR1## wherein X represents a single or a double bond; R.sup.1 is H or OH; provided that when X is a single bond, R.sup.1 is H or OH, and when X is a double bond, R.sup.1 is absent;R.sup.2 is H, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.8 alkynyl, alkoxy-alkyl or alkylthioalkyl containing from 1 to 6 carbon atoms in each alkyl or alkoxy group, wherein any of said alkyl, alkoxy alkenyl or alkynyl groups may be substituted by one or more halo atoms; or a C.sub.3 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkenyl group, either of which may be substituted by methylene or one or more C.sub.1 -C.sub.4 alkyl groups or halo atoms; or a 3 to 6 membered oxygen or sulphur containing heterocyclic ring which may be saturated, or fully or partially unsaturated and which may be substituted by one or more C.sub.1 -C.sub.4 alkyl groups or halo atoms; or a group of the formula SR.sup.5 wherein R.sup.5 is C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.2 -C.sub.

Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein A, W, P, R.sup.3, Q and R.sup.1 are as defined herein. The compounds of formula I, and pharmaceutically acceptable salts thereof, are substance P antagonists and as such are useful in the treament of various inflammatory and central nervous system disorders.

Abstract: Certain steroidal glycosides are useful as hypochoelsterolemic agents and antiatherosclerosis agents.

Abstract: Methods for the treatment of bone disorders utilizing certain prostaglandin agonists/antagonists.

Abstract: This invention relates to certain steroidal glycosides of Formula I ##STR1## wherein the values for the variables are described herein, which are useful as hypocholesterolemic agents and antiatherosclerosis agents and certain protected intermediates useful in the preparation of said steroidal glycosides.

Abstract: Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;X is O, S or (CH.sub.2).sub.m ;R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or ?(C.sub.1 -C.sub.3)alkoxy!carbonyl groups;n is 0, 1 or 2;m is 1 or 2;Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group;Z is CH.sub.2, NR.sup.2, O or S; andR.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl;are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.

Abstract: An asymmetric membrane, osmotic, delivery device having coated macroparticulate solubility modifiers. The device comprises a beneficial agent, an osmagent, a coated macroparticulate solubility modifier and an asymmetric membrane that surrounds the device components. The device is useful for dispensing a beneficial agent to an aqueous environment of use. The coated macroparticles modify the solubility of the beneficial agent so that it's release can be controlled. The larger size of the solubility modifier macroparticles provides, for example, a longer release duration than would have been possible with a smaller size.

Abstract: Quinuclidine derivatives of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein m, P, Z, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined below. The compounds are substance P antagonists and, therefore, are useful in treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, pain and migraine.

Abstract: A device for controlled release of an active substance through one or more asymmetric membranes by diffusion and/or osmotic pumping.

Abstract: Preparation of 4'-deoxy-O-mycaminosyltylonolide by feeding repromicin to a fermentation broth of a strain of the microorganism Streptomyces fradiae (ATCC 31733) under aerobic conditions in an aqueous nutrient medium containing inorganic salts and assimilable sources of carbon and nitrogen.

Abstract: This invention provides vaccine compositions, methods of producing same and methods for protecting porcine animals against disease associated with infection by toxigenic Pasteurella multocida. The vaccines of this invention contain effective amounts of a P. multocida bacterin with a cell-bound toxoid and, optionally, a P. multocida free toxoid.

Abstract: Phenolic prodrug esters of certain 1-(hydroxyphenyl)-2-piperidino-1-alkanol derivatives, which are useful in the treatment of stroke, traumatic head injury and CNS degenerative disease; and intermediates useful in their synthesis.

Abstract: This invention relates to a method of inhibiting 5-lipoxygenase in a mammal in need thereof by administering compounds of the core of formula ##STR1## the racemic, racemic-diastereomeric mixtures and optical isomers of said compounds and the pharmaceutically acceptable salts thereof.

Abstract: Compounds of formula (I) ##STR1## and the pharmaceutically acceptable base salts thereof, wherein R is --CO.sub.2 H or tetrazol-5 yl; R.sup.1 is C.sub.3 -C.sub.8 alkyl optionally substituted by fluoro; and R.sup.2 is C.sub.2 -C.sub.4 alkyl, together with compositions containing, uses of, process for the preparation of, and intermediates used in the preparation of, such compounds. The compounds have steroid 5.alpha.-reductase inhibitory activity and are useful for treating a disease such as benign prostatic hypertrophy.

Abstract: Actinomadura roseorufa mutants characterized by the ability to produce by fermentation UK-61,689, an acidic polycyclic ether anticoccidial antibiotic previously available only by selective acid hydrolysis of UK-58,852; and Actinomadura roseorufa having the identifying characteristics of ATCC 53,666, ATCC 53,665, ATCC 53,664 and ATCC 53,674.