Abstract: Disclosed is a pharmaceutical composition comprising (E)-3,5-dihydroxy-7-[4′-4″-fluorophenyl-2′-cyclopropyl-quinolin-3′-yl]-6-heptenoic acid, or its salt or ester, of which the aqueous solution or dispersion has pH of from 6.8 to 8. The composition has good time-dependent stability and has no change in its outward appearance even after having been stored long.

Abstract: Benzamides of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be arom

Abstract: This invention relates to the use of 5-HT3 receptor antagonists in the treatment of nonconstipated female IBS patients.

Abstract: Inhibitors of serine proteases are provided having formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.

Abstract: Novel dry skin remedies useful for treatment dry skin, containing as the active ingredient spiro [oxathiolane-quinuclidine] derivatives represented by general formula (I) or acid addition salts thereof, desirably cis-2-methylspiro [1,3-oxathiolane-5,3′-quinuclidine] hydrochloride. The remedies promote the secretion of sebaceous and sweat glands through oral or parenteral administration to treat dry skin, thus being useful as drugs.

Abstract: The invention relates to a compound of formula (I): 1

Abstract: The invention relates to a compound of formula (I): 1

Abstract: A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I:

Abstract: A sulfamoyl compound of the general formulae (1): wherein R1 and R2 are each independently C1-4 alkyl, or R1 and R2 together are C4-6 alkylene or C4-6 alkyleneoxy, Y is H, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylthio, C1-8 haloalkyl, C1-8 haloalkoxy or C1-8 haloalkylthio, A is a predetermined heterocyclic group, B is a predetermined heterocyclic group which is identical with or different from A, W is a chemical bond or O, V is O or S, D, E, F and G are each independently N, CR7, CR8, CR9 or CR10, and R3, R4, R5, R6, R7, R8, R9, R10 and R11 are each independently predetermined group such as H, or an unsubstituted or substituted aliphatic, aromatic or heterocyclic group. The sulfamoyl compound is useful as an agricultural and horticultural fungicide.

Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteosome inhibitors.

Abstract: This invention relates to the use of 5-HT3 receptor antagonists in the treatment of nonconstipated female IBS patients.

Abstract: Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula: wherein R1, R2, R3 and R4 are independently selected from the group consisting of H, halo, OH, C1-6alkyl, C1-6alkoxy, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl and others; R5 is selected from the group consisting of SO2Ar, C(O)Ar, Ar and CH2Ar; R6 and R7 are independently selected from the group consisting of H, C1-6alkyl, optionally substituted phenyl and optionally substituted benzyl; ————— represents a single or double bond; n is selected from an integer of from 1-3; X is selected from the group consisting of CR17 and N; Z is selected from the group consisting of C, CH and N, provided that when ————— is a double bond, Z is C and when ————— is a single bond, Z is selected from CH and N; Ar is an optionally substituted aromatic group selected from the group consisting of phenyl, pyridyl, thienyl,

Abstract: Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or “linker” defined as including a covalent bond per se so 29 as to space the aromatic systems at a distance 1.5-15Å, are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.

Abstract: The present invention is directed to the use of 2,4,5-trisubstituted imidazole compounds and compositions in the treatment of CNS injuries to the brain.

Abstract: A quinolizine carboxylic acid derivative of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 have the same meanings the as defined in the specification.

Abstract: A rosacea treating agent is provided, which is effective even on intractable rosacea which cannot be cured completely by antibiotics such as minocycline, has low toxicity, causes little side effect, and is of long duration. The rosacea treating agent of the present invention comprises, as an active ingredient, at least one selected from the group consisting of benzoheterocyclic derivatives represented by the following formula (1): ##STR1## wherein R is a lower alkyl group; and X is a halogen atom, and salts thereof.

Abstract: The present invention relates to a compound of formula I: ##STR1## or a pharmaceutical acid addition salt thereof; which are useful for activating 5-HT.sub.1F receptors and inhibiting neuronal protein extravasation in a mammal.

Abstract: Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof, in which R.sup.1 is vinyl or ethyl; and R.sup.2 is a group R.sup.3, R.sup.4 CH.sub.2 --, or R.sup.5 R.sup.6 C.dbd.CH--; wherein each of R.sup.3 and R.sup.4 is an azabicyclic ring system or R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.

Abstract: Methods are provided for conducting surgical procedures in a patient wherein, during the surgical procedure, autonomous ventricular electrical conductivity and escape beats are reversibly and transiently suppressed to facilitate the surgical procedure. Also provided are compositions which are capable of inducing ventricular asystole in a patient. The compositions may include an AV node blocker. In one embodiment, compositions including an atrioventricular (AV) node blocker and a .beta.-blocker are provided, wherein the .beta.-blocker is present in an amount sufficient to substantially reduce the amount of AV node blocker required to induce ventricular asystole in the patient. The compositions and methods may be used for inducing temporary ventricular asystole in a beating heart, and to facilitate the performance of a variety of surgical techniques, including minimally invasive microsurgical techniques.

Abstract: The invention is concerned with the use of bi- and tricyclic pyridone compounds of the formula where A, R.sup.1, R.sup.3, R.sup.4, and R.sup.7 are described herein and of their pharmaceutically acceptable salts for the production of medicaments for the prophylaxis or treatment of illnesses which are connected with an inhibition of .beta.-amyloid peptide activity, especially for the treatment of Alzheimer's disease.

Abstract: A pharmaceutical composition is disclosed that comprises clioquinol, vitamin B.sub.12, and, optionally, pharmaceutical acceptable carriers and/or excipients. The use of the pharmaceutical composition removes or alleviates the side effects of clioquinol.

Abstract: Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

Abstract: Inhibition of the enzyme poly (ADP-ribose) polymerase can delay the onset of senescence and inhibitors of the enzyme can be used to treat diseases caused or exacerbated by cellular senescence.

Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.

Abstract: The invention is concerned with the use of bi- and tricyclic pyridone compounds of the formula ##STR1## where A, R.sup.1, R.sup.3, R.sup.4, and R.sup.7 are described herein and of their pharmaceutically acceptable salts for the production of medicaments for the prophylaxis or treatment of illnesses which are connected with an inhibition of .beta.-amyloid peptide activity, especially for the treatment of Alzheimer's disease.

Abstract: Compounds of formula (I), or pharmaceutically acceptable salts thereof are provided: ##STR1## in which X.sub.1 --(CH.sub.2).sub.x --X.sub.2 forms a 5-7 membered ring wherein:X.sub.1 is O or S;X.sub.2 is O, S or NR wherein R is hydrogen;x is 1, 2 or 3;R.sub.1 is hydrogen, amino, halo, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkoxy;R.sub.2 is hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, nitro, amino or C.sub.1-6 alkylthio;R.sub.3 is hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or amino;R.sub.4 and R.sub.5 are independently hydrogen or C.sub.1-6 alkyl;Y is NH;Z is of sub-formula (a): ##STR2## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon; andn.sup.1 is 0, 1, 2, 3 or 4;q is 0, 1, 2 or 3;R.sub.a is (CH.sub.2).sub.n.sup.2 --R.sub.7 wherein n.sup.2 is 2 or 3 and R.sub.7 is selected from cyano, hydroxyl, C.sub.1-6 alkoxy, phenoxy, C(O)C.sub.1-6 alkyl, COC.sub.6 H.sub.5, --CONR.sub.8 R.sub.9, NR.sub.8 COR.sub.9, SO.sub.2 NR.sub.8 R.sub.9 or NR.sub.8 SO.sub.2 R.sub.9 whereinR.sub.8 and R.sub.

Abstract: The present invention relates to quaternary nitrogen-containing phosphate compounds, and the pharmaceutically-acceptable salts and esters thereof having the general structure: ##STR1## wherein: Z is a saturated, unsaturated, or aromatic, monocyclic or polycyclic carbocycle or monocyclic or polycyclic heterocycle containing one or more heteroatoms selected from O, S, or N;Y is N.sup.+ (R.sup.8).sub.2 or C(R.sup.1).sub.2 and when Y is C(R.sup.1).sub.2, at least one R.sup.2 must be N.sup.+ (R.sup.8).sub.3 ;R.sup.1, R.sup.2, R.sup.5, and R.sup.8 are defined in claim 1, m and n are integers from 0 to 10; m+n is from 0 to 10;R is COOH; PO.sub.3 H.sub.2 ; SO.sub.3 H; or P(O)(OH)R.sub.4, wherein R.sub.4 is substituted or unsubstituted alkyl of 1-8 carbons atoms.The present invention further relates to pharmaceutical compostions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients.

Abstract: Compounds of formula (I), wherein formula I consists of formulae (I-1) to (I-4), which are defined in the specification, and pharmaceutically acceptable salts thereof, and the use of a compound of formula I or a pharmaceutically acceptable salt thereof, and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorder.

Abstract: This invention relates to compounds of formula (I): ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl; andR.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently represent hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxyC.sub.1-4 alkyl, C.sub.1-4 alkylsulphonyl, trifluoromethylsulphonyl; optionally substituted arylsulphonyl, optionally substituted heteroarylsulphonyl, optionally substituted aralkylsulphonyl, optionally substituted heteroaralkylsulphonyl, nitro, cyano, amino, mono- or di-alkylamino, trifluoromethyl, trifluoromethoxy, hydroxyl, hydroxyC.sub.1-4 alkyl, C.sub.1-4 alkylthio, C.sub.1-4 alkanoyl, C.sub.1-4 alkoxycarbonyl, aminosulphonyl, or mono- or diC.sub.1-4 alkylaminosulphonyl; orR.sup.1 and R.sup.2 together form a linking chain --(CH.sub.2).sub.m Op; (wherein m is 2 to 4 and p is zero or 1) which chain may be optionally substituted by one or two C.sub.1-4 alkyl groups;and Y represents a group of formula (.alpha.

Abstract: Novel 2,4,5-triaryl imidazole compounds and compositions for use in therapy.

Abstract: Compounds of the formula ##STR1## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.

Abstract: Nontoxic substances that block the N-methyl-D-aspartate (NMDA) receptor, e.g., a morphinan such as dextromethorphan or dextrorphan, or that block a major intracellular consequence of NMDA receptor activation, e.g., a ganglioside such as GM.sub.1 or GT.sub.1b, a phenothiazine such as trifluoperazine or a naphthalenesulfonamide such as N-(6-aminohexyl) -5-chloro-1-naphthalenesulfonamide, inhibit the development of tolerance to and/or dependence on addictive drugs, e.g., narcotic analgesics such as morphine, codeine, etc.

Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.

Abstract: Spirocycles of general structural formula: ##STR1## are Class III antiarrhythmic agents.

Abstract: A compound of formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, X.sub.1, X.sub.2, x, Y and Z are as defined in the specification are useful in the treatment or prophylaxis of gastrointestinal disorders, cardiovascular disorders and CNS disorders.

Abstract: Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, selected preferred examples of which include those compounds whereinA is.dbd.CR.sup.6 --;R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl;R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group;R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; andR.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl),as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

Abstract: Antibacterial compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those compounds whereinA is .dbd.CR.sup.6 --;R.sup.1 is cycloalkyl of from three to eight carbon atoms or substituted phenyl;R.sup.2 is selected from the group consisting of ##STR2## R.sup.3 is halogen; R.sup.4 is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group;R.sup.5 is hydrogen, loweralkyl, halo(loweralkyl), or --NR.sup.13 R.sup.14 ; andR.sup.6 is halogen, loweralkyl, halo(loweralkyl), hydroxy-substituted loweralkyl, loweralkoxy(loweralkyl), loweralkoxy, or amino(loweralkyl),as well as pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.

Abstract: The use of a compound of formula (I) or pharmaceutically acceptable salt thereof, in which X.sub.1 --(CH.sub.2).sub.x --X.sub.2 forms a 5-7 membered ring wherein: X.sub.1 is O or S; X.sub.2 is O, S, NR or NRCO wherein R is hydrogen or C.sub.1-6 alkyl; x is 1, 2 or 3; Y is O or NH; Z is sub-formula (a), (b) or (c) in the manufacture of a medicament for use in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.

Abstract: Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, wherein R.sup.1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R.sup.6)--, where R.sup.6 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a group --(CH.sup.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1, 2 or 3; R.sup.5 is a hydrogen atom or an optionally substituted alkyl group; and the salts, solvates, hydrates and N-oxides. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma.

Abstract: The present invention relates to a method of treating or preventing emesis in a mammal, including a human, by administering to the mammal a 5HT.sub.3 receptor antagonist and an NK-1 receptor antagonist (e.g., a substance P receptor antagonist). It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a 5HT.sub.3 receptor antagonist and an NK-1 receptor antagonist.

Abstract: Nontoxic substances that block the N-methyl-D-aspartate (NMDA) receptor, e.g., a morphinan such as dextromethorphan or dextrorphan, or that block a major intracellular consequence of NMDA-receptor activation, e.g., a ganglioside such as GM.sub.1 or GT.sub.1b, a phenothiazine such as trifluoperazine or a naphthalenesulfonamide such as N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide, inhibit the development of tolerance to and/or dependence on addictive drugs, e.g., narcotic analgesics such as morphine, codeine, etc.

Abstract: Compounds of formula (I), ##STR1## wherein L is N or CR.sub.c, wherein R.sub.c is hydrogen, alkoxy, halo, alkyl or cyano; Q is NR.sub.1, CH.sub.2, O, or S; R.sub.a is hydrogen, halo, alkyl, amino, nitro or alkoxy; R.sub.b is hydrogen, halo, alkyl or alkoxy; R.sub.1 is hydrogen, alkyl, alkenyl, aralkyl, alkanoyl, or alkanoylalkyl; R.sub.2 is alkoxy; R.sub.3 is hydrogen, chloro or fluoro; R.sub.4 is hydrogen, alkyl, amino optionally substituted by alkyl, halo, hydroxy or alkoxy; R.sub.5 is hydrogen, halo, alkyl, alkoxy, nitro, amino or alkylthio; R.sub.6 is hydrogen, halo, alkyl, alkoxy or amino; n is 0, 1, 2, 3, or 4; p and m are independently 0, 1 or 2; and R.sub.q is hydrogen or C.sub.1-6 are 5-HT.sub.4 receptor antagonists.

Abstract: The present invention provides methods of inhibiting bone loss in mammals via the administration to a mammal in need of such treatment an effective amount of a compound from a series of benzoquinolin-3-ones. Such compounds also are sequentially or concurrently coadministered with a bone antiresorptive agent or a bone anabolic agent.

Abstract: 5-HT.sub.3 Receptor antagonists are useful in treating panic disorders or obsessive compulsive disorders.

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

Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.

Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.

Abstract: Substituted benzofuran derivatives of the formula (I): ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen or halogen and the other is, independently, an amino group or a C.sub.2 -C.sub.4 alkanoyl amino group; R.sub.3 is hydrogen; a linear or branched C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.2 -C.sub.4 alkoxycarbonyl group; halogen; or phenyl unsubstituted or substituted by a C.sub.1 -C.sub.4 alkyl group; A is a group --(CH.sub.2).sub.n -Het wherein Het is an optionally substituted heteromonocyclic or heterobicyclic ring containing one or two nitrogen atoms, and n is zero or an integer of 1 to 3; and the symbol ..... represents a single or double bond; may be prepared by a process comprising reacting a compound of formula II: ##STR2## in which L is a leaving group and R.sub.4 is hydrogen or a carboxy protecting group, with a compound of formula III;R'.sub.3 --C.dbd.C--R'.sub.