Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors .alpha..nu..beta.3, .alpha..nu..beta.5 and/or .alpha..nu..beta.6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, and tumor growth and metastasis.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

Abstract: A multi-compartment container is charged with a plurality of doses of powdered medicament so that the volume of each dose is than that of the respective compartments in which it is contained. A respective protuberance is inserted into each respective compartment, which is then filled with medicament and the protuberance is then removed. The container may take the form of an apertured plate, in which case the filling step can be achieved by placing the container on a porous bed and in communication with a reservoir of particulate material, and then passing gas through the reservoir, the apertures in the container and the bed. There is also shown apparatus for performing the method, the apparatus comprising a reservoir for the particulate material and a conduit for relaying particulate material from the reservoir to the compartments, the conduit including protuberances which are insertable into the compartments to reduce the available volume of the latter.

Abstract: Imidazopyridine derivatives ad pharmacologically acceptable salts having antagonistic properties towards angiotensin II can be used for the treatment of hypertension, aldosteronism and cardiac insufficiency.

Abstract: The invention relates to a liquid-crystalline medium based on a mixture of polar compounds having positive dielectric anisotropy, characterized in that it comprises one or more compounds of the general formula I ##STR1## and simultaneously one or more compounds of the general formula I' ##STR2## in which R.sup.1, R.sup.2, R.sup.0', ##STR3## Y.sup.2' and X.sup.0' are as defined herein.

Abstract: A tachykinin antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep.

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV). ##STR1## The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula I.

Abstract: Oxadiazole substituted benzenesulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.

Abstract: A novel prostaglandin receptor has been identified and DNA encoding the receptor has been isolated, purified, sequenced and expressed in host cells. This DNA encoding the novel prostaglandin receptor and host cells expressing the receptor are used to identify modulators of the prostaglandin receptor.

Abstract: The present invention relates to an oxidation using sodium chlorite in the presence of a catalytic amount of TEMPO and sodium hypochlorite which converts the penultimate intermediate bearing a primary alcohol to the target endothelin antagonist compound of Formula I having a carboxylic acid ##STR1##

Abstract: Certain bisamine compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for direct use in therapeutic compositions are described. A novel process for their preparation is also described.

Abstract: An isolated nucleic acid molecule is disclosed which encodes a novel human cyclin-dependent kinase (CDK) which comprises a novel cyclin binding domain signature sequence and lacks several heretofore conserved amino acid residues involved in regulation of the cdk/cyclin complex. Associated proteins and biologically active mutant forms are also disclosed.

Abstract: Novel oxazolidinone derivatives of the formula I ##STR1## in which R.sup.1 is a phenyl radical which is unsubstituted or is monosubstituted by CN, H.sub.2 N--CH.sub.2 --, A.sub.2 N--CH.sub.2 --, H.sub.2 N--C(.dbd.NH)--, H.sub.2 N--C(.dbd.NH)--NH--, H.sub.2 N--C(.dbd.NH)--NH--CH.sub.2 --, HO--NH--C(.dbd.NH)-- or HO--NH--C(.dbd.NH)--NH--,X is O, S, SO, SO.sub.2, --NH-- or --NA--,B is ##STR2## A is alkyl having from 1 to 6 C atoms, R.sup.2 is H, A, Li, Na, K, NH.sub.4 or benzyl,R.sup.3 is H or (CH.sub.2).sub.n --COOR.sup.2,E is, in each case independently of each other, CH or N,Q is O, S or NH,m is 1, 2 or 3, andn is 0, 1, 2 or 3,and physiologically compatible salts thereof are provided, which inhibit the binding of fibrinogen to the corresponding receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and also tumors.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: The present invention is directed to a novel process for the preparation of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'- yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methyl-propanamide, and salts thereof, which has the structure: ##STR1## and which has the ability to stimulate the release of natural or endogenous growth hormone. This compound may be used to treat conditions which require the stimulation of growth hormone production or secretion such as in humans with a deficiency of natural growth hormone or in animals used for food or wool production where the stimulation of growth hormone will result in a larger, more productive animal.

Abstract: Cyclic sulphones of formula (I) are disclosed, in which: R.sup.1 and R.sup.2 each independently of one another stand for H, A, CF.sub.3, CH.sub.2 F, CHF.sub.2, C.sub.2 F.sub.5, Hal, OH, OA, NH.sub.2, NHA, NA.sub.2, NO.sub.2 or CN; X stands for CR.sup.4 R.sup.5, C.dbd.Z, O, S, NH, NA or NR.sup.3 ; Y stands for CR.sup.6 R.sup.7, C.dbd.Z, O, NH, NA, or NR.sup.3 ; Z stands for O, S, NH, NA, NOH, NOA, CH.sub.2, CHA or CA.sub.2 ; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently of one another stand for H, A, R.sup.3, Hal, OH, OA, SH, SA, NH.sub.2, NHA or NA.sub.2, or alternatively, R.sup.5 and R.sup.6 or R.sup.7 and R.sup.8 can together represent a bond, only one such bond being present in each molecule; R.sup.4 and R.sup.5 together can also stand for O--(CH.sub.2).sub.2 --O or O--(CH.sub.2).sub.3 --O; R.sup.8 and R.sup.9 each independently of one another stand for H or A; A stands for alkyl with 1-6 C atoms; Hal stands for F, Cl, Br or I; and R.sup.

Abstract: The invention relates to TN liquid-crystal displays and supertwist liquid-crystal displays (SLCDs) having very short response times and good steepnesses and angle dependences, and to the novel nematic liquid-crystal mixtures used therein, which are distinguished by the fact that they comprise at least one compound o the formula IA ##STR1## and at least one compound of the formula IB ##STR2## in which R.sup.a, R.sup.b, R.sup.c, Ring A*, L, l and r are as defined in claim 1.

Abstract: The invention relates to quinoline-2-(1H)-one derivatives of the general formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are in each case independently of one another H, Hal, A or OA; R.sup.4 is H, --(CH.sub.2).sub.m --NR.sup.6 R.sup.7 ; R.sup.5 is H, --(CH.sub.2).sub.n --NR.sup.6 R.sup.7 ; R.sup.6 is H, A or, together with R.sup.7, --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --; R.sup.7 is H, A or --(CH.sub.2).sub.m -- with a bond to the same ring or adjacent ring B or D or, together with R.sup.6, --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --; X is --CHR.sup.5 --, --NR.sup.5 --, --O--, --S--; A is alkyl having 1-6 C atoms; Hal is F, Cl, Br or I; m is 1-3 and n is 0-3, where at least one of the two radicals R.sup.4 or R.sup.5 has the meaning --(CH.sub.2).sub.m --NR.sup.6 R.sup.7 or --(CH.sub.2).sub.n --NR.sup.6 R.sup.7, their enantiomers, stereoisomers, salts and solvates. Such compounds are useful for the treatment of neurodegenerative diseases.