Abstract: There is provided a pharmaceutical dosage form adapted for administration to the gastrointestinal tract of a patient, comprising darifenacin, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable adjuvant, diluent or carrier, characterized in that the dosage form is adapted to deliver at least 10% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof, to the lower gastrointestinal tract of the patient. The formulation minimizes unwanted side-effects and increases the bioavailability of darifenacin.

Abstract: The present invention provides novel methods of inhibiting pathological conditions related to organ systems which respond to estrogen agonists comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I ##STR1##

Abstract: Compounds of Formula (1) wherein R.sub.6 is carboxy, (C.sub.1 -C.sub.8)alkoxycarbonyl, benzyloxycarbonyl, C(O)NR.sub.8 R.sub.9 or C(O)R.sub.12 as glucogen phosphorylase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat diabetes, hyperglycemia, hypercholesterolemia, hypertension, hyperinsulinemia, hyperlipidemia, atherosclerosis and myocardial ischemia in mammals.

Abstract: The invention provides compounds of formula (I), ##STR1## wherein R.sup.1 represents C.sub.1-4 alkoxy optionally substituted by one or more fluorine atoms; R.sup.2 represents H or C.sub.1-6 alkoxy optionally substituted by one or more fluorine atoms; R.sup.3 represents one or more groups independently selected from H, halogen, C.sub.1-4 alkoxy and CF.sub.3 ; in addition, R.sup.2 and one R.sup.3 group may together represent --OCH.sub.2 --, the methylene group being attached to the ortho-position of the pendant phenyl ring; R.sup.4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and pharmaceutically acceptable salts thereof.

Abstract: This invention relates to Streptomyces avermitilis lacking branched-chain amino acid transaminase activity, branched-chain 2-oxo acid biosynthetic activity and, optionally and preferably, avermectin B-O-methyl transferase activity, methods for preparation thereof, and use thereof to produce natural and non-natural avermectins from branched-chain fatty acid or branched-chain 2-oxo acid precursors. Such avermectins are useful as parasiticides.

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 novel compound having antibacterial activity according to the the formula ##STR1## The compound of the present invention may be prepared from (9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido [3,2,1-ij]-1,3,4-benzadiazine-6-carboxylic acid by treatment with an oxidizing agent, such as hydrogen peroxide in the presence of an aqueous inorganic base. Additionally, there are provided methods for treating animals, including humans, suffering from bacterial infections.

Abstract: The present invention provides novel methods of treating or preventing osteoporosis comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different provided that, when R.sup.1 and R.sup.2 are the same, each is a methyl or ethyl group, and, when R.sup.1 and R.sup.2 are different, one of them is a methyl or ethyl group and the other is hydrogen or a benzyl group; or a pharmaceutically acceptable salt thereof; together with a bone resorption inhibiting polyphosphonate, or with parathyroid hormone.

Abstract: The invention relates to compounds of the formula I ##STR1## and to pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, Q, X, Y and Z are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I, methods of using said compounds of formula I in the treatment of infections, and methods of preparing said compounds of formula I.

Abstract: A method of treating male erectile dysfunction comprising administering to a male human a pyrimidine compound of formula I.

Abstract: The invention relates to processes for preparing a compound of the formula (X) and the enantiomer of said compound, wherein the benzoic acid moiety is attached at position 6 or 7 of the chroman ring, and R.sup.1, R.sup.2 and R.sup.3 are as defined herein. The invention further relates to intermediates that are useful in the preparation of the compound of formula (X).

Abstract: A process for the preparation of the compound of the formula: ##STR1## wherein R.sup.1 is OH, which comprises the steps of a) treating the compound of the formula: ##STR2## with an inorganic fluoride, of the formula M.sup.2 F wherein M.sup.2 is an alkali metal cation, at an elevated temperature in the presence of a compound of the formula R.sup.4 P.sup.+ Z.sup.- and a compound of the formula R.sup.5 vic (COW).sub.2 wherein R.sup.4 and R.sup.5 are each selected from optionally substituted (C.sub.6 -C.sub.10) aryl and optionally substituted (C.sub.1 -C.sub.6) alkyl, and W is halo; to form the compound of the formula: ##STR3## and b) I) treating the compound of the formula IV with an aqueous solution of a base, of the formula MOH, wherein M is an alkali metal cation, andii) treating the product of step i) with a mineral acid. A compound of the formula: ##STR4## wherein R.sup.1 is selected from the group consisting of, halo, R.sup.7 O, R.sup.7 COO and N(R.sup.8).sub.2 wherein R.sup.7 is (C.sub.1 -C.sub.

Abstract: A new pyridine carbaldehyde is useful for the synthesis of compounds which are effective for treating neurodegeneration conditions and CNS trauma.

Abstract: The instant invention relates to intermediates of Formula II, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, and to processes for preparing such intermediates. This invention also relates to processes for preparing compounds of Formula III, ##STR2## and enantiomers thereof, wherein R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification. Compounds of Formula II and Formula III are intermediates in the preparation of a potent .beta..sub.3 adrenergic receptor agonist. The instant invention also relates to processes for preparing the .beta..sub.3 adrenergic receptor agonist using the compounds of Formula II and Formula III.

Abstract: Compounds of formula (I): ##STR1## or pharmaceutically, veterinarily or agriculturally acceptable salts thereof, or pharmaceutically, veterinarily or agriculturally acceptable solvates of either entity, wherein R.sup.1 is 2,4,6-trisubstituted phenyl or 3,5-disubstituted pyridin-2-yl; R.sup.3 is hydrogen; C.sub.2 to C.sub.5 alkyl substituted with one or more halo and with hydroxy; C.sub.2 to C.sub.5 alkanoyl substituted with one or more halo; C.sub.2 to C.sub.6 alkenyl optionally substituted with one or more halo; halo; amino or CONH.sub.2 ; R.sup.5 is hydrogen, amino or halo; R.sup.2 and R.sup.4 are each independently selected from hydrogen, fluoro, chloro and bromo; R.sup.6 and R.sup.8 are hydrogen; and R.sup.7 is hydrogen or C.sub.1 to C.sub.4 alkyl optionally substituted with one or more halo; are parasiticidal agents.

Abstract: Compounds of formula (I): ##STR1## where the substituents are as defined herein, and salts thereof, are matrix metalloprotease inhibitors.

Abstract: A compound of the formula ##STR1## wherein Q is as defined above, are useful in the treatment of a condition selected from the group consisting of arthritis (including osteoarthritis and rheumatoid arthritis), inflammatory bowel disease, Crohn's disease, emphysema, chronic obstructive pulmonary disease, Alzheimer's disease, organ transplant toxicity, cachexia, allergic reactions, allergic contact hypersensitivity, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, osteoporosis, loosening of artificial joint implants, atherosclerosis (including atherosclerotic plaque rupture), aortic aneurysm (including abdominal aortic aneurysm and brain aortic aneurysm), congestive heart failure, myocardial infarction, stroke, cerebral ischemia, head trauma, spinal cord injury, neuro-degenerative disorders (acute and chronic), autoimmune disorders, Huntington's disease, Parkinson's disease, migraine, depression, peripheral neuropathy, pain, cerebral amyloid angiopathy, nootropic or cognition e

Abstract: This invention relates to an optically pure androgen mediator, pharmaceutical compositions containing the stereoisomer and the use of the stereoisomer to aid in the prevention and restoration of for example, age-related decline in muscle mass and strength and the treatment of conditions which present with low bone mass in mammals, including humans.

Abstract: A compound of the chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein Y is C.sub.2 -C.sub.4 alkylene; Z is a valence bond or C.sub.1 -C.sub.6 alkylene; R.sup.1 is substituted or unsubstituted aryl (e.g., phenyl and naphthyl) or heteroaryl (e.g., thienyl and furyl); R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.3 is hydrogen, hydroxy or the like; R.sup.4 is substituted or unsubstituted benzyl or the like. Typical examples are (2S*,3S*,4R*,5R*)-4-Carboxy-3-[N-(5-Isopropyl-2-methoxy-benzyl)amino]-5-me thyl-2-phenylpyrrolidine and (2S*,3S*,5S*)-5-Carboxy-3-[N-(2-methoxy-5-trifluoromethoxybenzyl)amino]-2- phenylpiperidine. The novel substituted azaheterocyclecarboxylic acids in this invention have excellent substance P antagonistic activity and are thus useful for the treatment of gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis or migraine in mammals, especially humans.