Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.

Abstract: The present invention relates to certain novel amide derivatives which are pyrido[3,4-d]pyrimidin-7-ylacetamides which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these amide derivatives, processes for preparing the amide derivatives, pharmaceutical compositions containing such amide derivatives and methods for their use.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A-B have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1 -R.sup.4, X, Y, and Z have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful as potassium channel openers for the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: Compounds of formula I ##STR1## wherein X.sup.a, X.sup.b, R, R.sup.1 and R.sup.2 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful as potassium channel openers for the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: A method of treating a mammal having a solid tumor susceptible to treatment with cisplatin comprising: administering to the mammal an effective amount of 3-amino-1,2,4-benzotriazine 1,4-dioxide; and administering to the mammal an effective amount of cisplatin about 0.5 to about five hours after administration of the 3-amino-1,2,4-benzotriazine 1,4-dioxide.

Abstract: Compounds of general formula I, ##STR1## and pharmaceutically acceptable salts thereof, in which R.sup.1 has any of the meanings given in the specification, pharmaceutical compositions comprising them and their use in the treatment of urinary incontinence.

Abstract: Compounds of formula I: ##STR1## wherein, ring C, A-B, R.sup.1, n, R.sup.2, and R.sup.3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinary incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: A physical form of (R)-3-methoxy-4-[1-methyl-5-(2-methyl-4,4,4-trifluorobutylcarbamoyl)indol- 3-ylmethyl]-N-(2-methylphenylsulphonyl)benzamide substantially free of other physical forms, which form is crystalline and has an X-ray powder diffraction pattern with specific peaks at 2.THETA.=14.0.degree., 19.4.degree., 22.0.degree., 22.4.degree. and 24.7.degree., processes for preparing the form and pharmaceutical compositions containing it. The compound is a leukotriene antagonist useful in the treatment of diseases such as asthma.

Abstract: The present invention provides methods of treating graft-versus-host disease comprising administering to a patient having graft-versus-host disease an effective mount of hydroxychloroquine. The present invention aim provides a method of suppressing alloreactivity arising from reactions of donor T lymphocytes against recipient cells comprising administering to said cells an amount of hydroxychloroquine effective to suppress such alloreaetivity.

Abstract: A new class of polyalkylene oxide vinyl sulfone reagents is described. Also described are a method by which these reagents can be prepared as well as a method for using them in hydrated media for the modification of proteins. The novel polymer-to-protein conjugates made by reacting these reagents with proteins have advantages over similar conjugates prepared with prior art reagents in that they are more stable against hydrolysis and retain the positive charge carrying capacity at amine sites at which the modifying reagents are attached.

Abstract: Azole-fused peptides useful as Substance P antagonists and analgesics, for example ##STR1## wherein ##STR2## represents ##STR3## wherein X is O, S or NH and * is D, or as intermediates therefor are prepared by azole and peptide forming methods.

Abstract: A targeting radioactive immunoreagent comprising a compound having the structure ##STR1##

Abstract: The method of use of danazol for reducing or eliminating urinary incontinence and any associated frequent urination in a person suffering therefrom and pharmaceutical compositions therefor are disclosed.

Abstract: A novel Aspergillus species, cyclic dimeric dipeptide derivatives which are biosynthetic products thereof and are useful as Substance P antagonists and therefore as analgesic and/or antiinflammatory agents, and a process for preparation of the biosynthetic products are disclosed.

Abstract: This invention discloses a composition comprised of nanoparticles having a non-ionic surfactant as a surface modifier adsorbed on the surface thereof and a charged phospholipid as a cloud point modifier associated therewith, which cloud point modifier is present in an amount sufficient to increase the cloud point of the surface modifier. A preferred non-ionic surfactant surface modifier is a poloxamine or tyloxapol, and preferred charged phospholipid cloud point modifiers include dimyristoyl phosphatidyl glycerol. This invention further discloses a method of making nanoparticles having a non-ionic surfactant as a surface modifier adsorbed on the surface and a charged phospholipid as a cloud point modifier associated therewith, comprised of contacting said nanoparticles with the cloud point modifier for a time and under conditions sufficient to increase the cloud point of the surface modifier.

Abstract: Compounds having the structure ##STR1## wherein (Z--COO is the residue of an iodinated aromatic acid;n is an integer from 1 to 20;R.sup.1 and R.sup.2 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy or aryloxy;R.sup.3 and R.sup.4 are independently H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxy, aryloxy, halogen, hydroxy or acylamino; andR.sup.5 is alkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl;are useful as contrast agents in x-ray imaging compositions and methods.

Abstract: (S)-(+)-Hydroxychloroquine substantially free of (R)-(-)-hydroxychloroquine, or a pharmaceutically acceptable acid-addition salt thereof and a method of use thereof and a composition containing it for the treatment of malaria, lupus erythematosus or rheumatoid arthritis.

Abstract: A method of inhibiting mammalian topoisomerase II and inhibiting the growth and inducing the regression of malignant cells in mammals by the action of a (S)-3-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine or -benzothiazine of the formula ##STR1## wherein R.sub.1 is hydrogen or fluoro, R.sub.2 and R.sub.3 each independently is hydrogen or alkyl having 1 to 4 carbon atoms, and X is O, S or S=O; a pharmaceutically acceptable acid-addition salt thereof; or a salt thereof with a pharmaceutically acceptable cation; and certain novel compounds of formula I.

Abstract: 4-R.sub.1 -R.sub.2 -R.sub.3 -2-Saccharinylmethyl and 4,7-C-4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates of formulas I and IIA respectively herein, useful in the treatment of degenerative diseases, and compositions containing them, methods for using them to treat degenerative diseases, and processes for their preparation by reaction of the corresponding 2-halomethylsaccharins with a phosphate, phosphonate or phosphinic acid of formula III herein in the presence of an acid-acceptor.