Abstract: Substituted piperidines and related compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are herein defined are disclosed.

Abstract: Certain novel 3-acyl-4-amino-8-alkoxyquinoline compounds have been prepared, including their pharmaceutically-acceptable salts. These compounds are useful for inhibiting gastric acid secretion in mammals and therefore, are of value in therapy as anti-ulcer agents. They are also useful for treating osteoporosis in a mammalian subject afflicted with said condition. Methods for preparing these compounds from known starting materials are provided.

Abstract: A process is disclosed for site-directed chemical modification of peptides and proteins that consists of two steps; (a) selective oxidation of a 2-hydroxyethylamine moiety, --CH(NH.sub.2)--CH(OH)--, in the peptide or protein to generate an aidehyde, and (b) reaction of the new aldehyde with a second reagent to form a product in which the native biological properties of the peptide are augmented by new and useful properties conferred by the second reagent. Additionally, the invention pertains to certain specified types of product formed by the above process.

Abstract: Compounds of the formula ##STR1## wherein R.sup.21 and R.sup.22 are as defined in the specification which are intermediates useful in the preparation of compounds of the formula ##STR2## and the pharmaceutically acceptable salts thereof, wherein Q and R.sup.1 are as defined in the specification. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.

Abstract: Aqueous solutions for treating inflammations of the eye, comprising: from about 0.03-3 weight percent of piroxicam; an effective amount of a buffer; from about 0 to about 1 weight percent of a wetting agent; from about 0 to about 5 weight percent of a pH adjusting agent; from about 0 to about 5 weight percent of a tonicity agent; an effective amount of a preservative; from about 0 to about 3 weight percent of a demulcent polymer; from about 0 to about 40 weight percent of a complexing agent; and from about 0 to about 0.1 weight percent of a stabilizer; and having a pH between about 7 and about 10.

Abstract: Compounds of formula (I) are diuretic agents for treating various cardiovascular diseases including hypertension, heart failure and renal insufficiency.

Abstract: A prosthesis for the correction of a flatfoot condition of a patient, which is designed for insertion inside a recess or tarsal sinus defined between a first bone or astragalus and a second bone or calcaneus; wherein the prosthesis is made of bioreabsorbable material. The prosthesis has a club-shaped body or a slightly conical body.

Abstract: This invention relates to pharmaceutical compositions for rectal administration containing semi-synthetic glycerides produced by interesterification, and, as the active ingredient, triazole derivatives of the formula ##STR1## wherein R.sup.1 is phenyl optionally sustituted with from one to three substituents independently selected from the group consisting of F, Cl, Br, I, CF.sub.3,(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, and 5-chloropyrid-2-yl; X is OH, F, Cl or Br; R.sub.2 is H.sub.2, CH.sub.3 or F; and R.sub.3 is H or F.

Abstract: Compounds of formula (1), wherein X is CH or N; Z is CH.dbd.CH or S; A is CH.sub.2 CH.sub.2, CH.dbd.CH, CH(OH)CH.sub.2, or COCH.sub.2 ; B is a direct link or --CH.sub.2 --, --CH(CH.sub.3)-- or --C(CH.sub.3).sub.2 --; or when Z is CH.dbd.CH, B may form a cyclopentane ring fused to the attached benzene ring; Y completes a fused benzo or thienyl ring which is optionally substituted by halo or C.sub.1 -C.sub.4 alkyl; n is 0, 1 or 2; and m is 0 or 1; are antagonists of both PAF and histamine H.sub.1 having utility in the treatment of allergic inflammatory conditions such as allergic rhinitis.

Abstract: A process for preparing the compound of the formula ##STR1## which comprises treating a compound of the formula ##STR2## wherein R.sup.2 is hydrogen, CN or CO.sub.2 R.sup.1 and R.sup.1 is hydrogen or (C.sub.1 -C.sub.6)alkyl with a reducing agent with the proviso that when R.sup.2 is CN or CO.sub.2 R.sup.1 and R.sup.1 is (C.sub.1 -C.sub.6)alkyl the product of the reduction is heated with an acid. Compounds of formula II wherein R.sup.2 is CN or CO.sub.2 R.sup.1 and R.sup.1 is (C.sub.1 -C.sub.6)alkyl or R.sup.2 is hydrogen and R.sup.1 is (C.sub.1 -C.sub.6)alkyl or hydrogen. The compound of formula VII R.sup.1 is (C.sub.1 -C.sub.6)alkyl. The compound of formula III. The compound of formula I is useful in the treatment of psychotic disorders.

Abstract: An osmotic bursting device for dispensing a beneficial agent to an aqueous environment. The device comprises a beneficial agent and osmagent surrounded at least in part by a semipermeable membrane. Alternatively the beneficial agent may also function as the osmagent. The semipermeable membrane is permeable to water and substantially impermeable to the beneficial agent and osmagent. A trigger means is attached to the semipermeable membrane (e.g., joins two capsule halves). The trigger means is activated by a pH of from 3 to 9 and triggers the eventual, but sudden, delivery of the beneficial agent. These devices enable the pH-triggered release of the beneficial agent core as a bolus by osmotic bursting.

Abstract: Macrolides of formula (I) and methods of treatment of resistance to transplantation, fungal infections and autoimmune diseases such as rheumatoid arthritis and psoriasis using said macrolides of formula (I), ##STR1## wherein n is 1 or 2; A and B taken together form .dbd.O or A and B taken separately are each H or A is OH and B is H; R.sup.1 is a group of the formula ##STR2## R.sup.2 is OH or a desosaminyloxy group; and R.sup.3 is an alkyl or allyl group.

Abstract: There is disclosed a low calorie fat substitute comprising an outer coating of a digestible fat surrounding an inner core of a low caloric or non-caloric material.

Abstract: 3-Piperidino-1-chromanol derivatives and analogs having the formula ##STR1## wherein A and B are taken together and are --CH.sub.2 CH.sub.2 -- or A and B are taken separately and are each H;X is CH.sub.2 or O;X.sup.1 is H or OH;Z is H, F, Cl, Br or OH;Z.sup.1 is H, F, Cl, Br or (C.sub.1 -C.sub.3)alkyl;n is 0 or 1; andm is 0 or an integer from 1 to 6;pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

Abstract: Compounds of the formula ##STR1## and pharmaceutical compositions comprising them, wherein R.sup.1, Z, X, W and Y are as defined below. The compounds are useful in the treatment of psychosis and anxiety.

Abstract: An acidic polycyclic ether antibiotic, having structure established by X-ray crystallography, is formed by fermentation of a novel microorganism, Actinomadura sp. ATCC 55027. This novel antibiotic is useful as an anticoccidial in poultry, in the prevention and treatment of swine dysentery and as a growth promotant in cattle and swine.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, C.sub.3 -C.sub.5 cycloalkyl or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.2 is H, C.sub.1 -C.sub.6 alkyl optionally substituted by OH, C.sub.1 -C.sub.3 alkoxy or C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 perfluoroalkyl or (C.sub.3 -C.sub.6 cycloalky)C.sub.1 -C.sub.6 alkyl; R.sup.4 taken together with the nitrogen atom to which it is attached completes a pyrrolidinyl, piperidino, morpholino, or 4-N-(R.sup.6)-piperazinyl group; R.sup.5 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 alkoxy, NR.sup.7 R.sup.8, or CONR.sup.7 R.sup.8 ; R.sup.6 is H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.3 alkoxy) C.sub.2 -C.sub.6 alkyl, hydroxy C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 N)C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 NCO)C.sub.1 -C.sub.6 alkyl, CONR.sup.7 R.sup.8, CSNR.sup.7 R.sup.

Abstract: According to the invention there is provided a compound of formula (I): R.sup.1 --O(CH.sub.2).sub.m A(CH.sub.2).sub.n XR or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is a group of formula (a or b) where Z is --(CH.sub.2).sub.2-, --CH.dbd.CH--, --CH.sub.2 --S-- or --CH.sub.2 --O--; R is a group of formula (c, d or Het) and A is a group of formula (e, f or g) in which the N atom is attached to the group (CH.sub.2)n; m is 1 or 2; n is an integer of from 1 to 4; p is 1, 2 or 3; R.sup.2 and R.sup.3 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy-(C.sub.1 -C.sub.4 alkyl), hydroxy, C.sub.1 -C.sub.4 alkoxy, halo, trifluoromethyl, nitro, cyano, sulphamoyl, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), carboxy, --CO.sub.2 (C.sub.1 -C.sub.4 alkyl), --CH.sub.2).sub.q CONR.sup.4 R.sup.5, -- (CH.sub.2).sub.q OCONR.sup.4 R.sup.5, --CH.sub.2).sub.q NR.sup.6 R.sup.7 or --NHSO.sub.2 NH.sub.2 in which R.sup.4 and R.sup.5 are each independently H or C.sub.1 -C.sub.

Abstract: Racemic or optically active compound of the formula ##STR1## wherein X is O or NH, R.sup.1 is a (C.sub.7 -C.sub.11)polycycloalkyl group, R.sup.2 is methyl or ethyl, Y is ##STR2## R.sup.3 is hydrogen, (C.sub.1 -C.sub.3)alkyl, (C.sub.2 -C.sub.3)alkenyl, benzyl or phenethyl, and R.sup.4 is hydrogen, (C.sub.1 -C.sub.3)alkyl or (C.sub.2 -C.sub.3)alkanoyl, are useful in the treatment of asthma or inflammatory airway or skin diseases.

Abstract: The present invention relates to a method of treating or preventing urinary incontinence in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives and related compounds.