Abstract: Diphenyl-cyclopropene derivatives, their nontoxic, pharmaceutically acceptable acid addition salts and compositions are kapa opiods useful in the treatment of pain, inflammation, Parkinsonism, dystonia, cerebral ischemia, diuresis, asthma, psoriasis, irritable bowel syndrome and stroke.

Abstract: Novel amide derivatives of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.

Abstract: The present invention is directed to an improved antihyperlipidemic agent, the dimaleate salt of 2-?2-(dimethylamino)ethyl!-8,8-dipropyl-2-azaspiro?4.5!decane.

Abstract: Compounds of formula I: ##STR1## wherein R.sup.1, R.sup.2, W, X, Y and Z have any of the values defined in the specification, and their pharmaceutically acceptable salts, are inhibitors of monoamine re-uptake and are useful for treating diseases in mammals wherein insufficient synaptic levels of monoamine are implicated. Also disclosed are pharmaceutical compositions, processes for preparing compounds of formula I, and intermediates useful for the synthesis of compounds of formula I.

Abstract: This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors 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 HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.

Abstract: The invention relates to benzimidazole antibacterial compounds of the Formula I: ##STR1## as described herein, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.

Abstract: An improved immunomodulatory agent, the dimaleate salt of N,N-dimethyl-8,8-dipropyl-2-azaspiro?4.5!decane-2-propanamine.

Abstract: Invented are methods of inhibiting the production of cytokines, particularly inhibiting the production of interleukin-1 and inhibiting the production of tumor necrosis factor in a mammal in need thereof which comprises administering to such mammal an effective amount of an azaspirane derivative.

Abstract: Compositions containing (a) L-carnitine, an acyl L-carnitine, or a pharmacologically acceptable salt thereof in combination with (b) an ACE-inhibitor are useful for treating cardiovascular disorders. Orally, parenterally, rectally or transdermally administrable pharmaceutical compositions in unit dosage form contain from about 0.5 to about 2 g of L-carnitine, or an equimolar amount of an acyl L-carnitine or a pharmacologically acceptable salt thereof, and, e.g., from about 5 to about 20 mg of the ACE-inhibitor lisinopril.

Abstract: Kappa-opioid agonists prevent the impairment of renal function otherwise caused by the combination of gaseous anesthesia and surgery or severe trauma. Not only do these agents preserve renal function and maintain urine output, they also maintain plasma electrolyte concentration and osmolality by reducing renal loss of sodium and potassium when compared to other diuretic agents. The preservation of urine flow as well as the ability to retain body sodium, potassium, calcium, and osmolality during surgery or severe trauma under gaseous anesthesia are novel and unique properties associated only with kappa opioid agonists. To date, no other clinically-used diuretic agent has been shown to provide constant urine flow, or to retain electrolytes during anesthesia and surgery. The kappa opioid agonists may be used in surgical patients with normal cardiovascular function, but are particularly useful in patients with compromised cardiovascular and/or renal function.

Abstract: The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.

Abstract: The present invention relates to novel 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, G, X, Y and Z have the meaning given in the description, to processes for their preparation and to intermediates for this purpose. The compounds of the formula (I) are used as pesticides and herbicides.

Abstract: Invented is a method of treating opportunistic infections in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a substituted azaspirane.

Abstract: A pharmaceutical compound of the formula ##STR1## and salts and esters thereof.

Abstract: The present invention relates to spiro?3H-indole-3(2H),3'-pyrrolidine! derivatives of general formula I ##STR1## as defined in the description. The invention also relates to a process for their preparation and to their therapeutic use, in particular for the treatment of complaints associated with melatonin disorders, and to the pharmaceutical and cosmetic compositions comprising them.

Abstract: This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3-???8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspi ro-?4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Abstract: The compounds of formula I: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl or benzyl; or R.sup.1 and R.sup.2, taken together, are benzylidene optionally substituted with R.sup.3 as defined below or alkylidene, or R.sup.1 and R.sup.2, taken together with the carbon to which they are attached, form a carbonyl moiety or a cycloalkyl group; R.sup.3 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido; R.sup.4 is hydrogen or alkyl; m is an integer 0, 1 or 2; n is an integer from 0 to 6, inclusive; Z is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, polycyclo-alkyl, phenyl optionally substituted with R.sup.3 as defined above, phenoxy optionally substituted with R.sup.3 as defined above, naphthyl optionally substituted with R.sup.3 as defined above or naphthyloxy optionally substituted with R.sup.

Abstract: An improved immumomodulatory agent, the dimaleate salt of N,N-diethyl-8,8-dipropyl-2-azaspiro?4.5!decane-2-propanamine.

Abstract: The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.

Abstract: The invention relates to combinations of angiotensin-converting enzyme inhibitors with calcium antagonists, processes for their preparation and their use as medicaments.

Abstract: Derivatives of 2,3-dihydro-5-benzofuranol, intermediates thereof, and processes useful for their preparation. These compounds are free radical scavengers and are useful in the treatment of conditions capable of being treated by free radical scavengers, such as stroke, nervous system trauma and reperfusion damage.

Abstract: Invented is a method of treatment of hyperlipidemia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of an azaspirane derivative. Also invented are pharmaceutical compositions containing an azaspirane derivative.

Abstract: O-substituted fumagillol derivatives and its salts have an angiogenesis inhibiting activity and are useful for prophylaxis and treatment of diseases induced by abnormally stimulated neovascularization.

Abstract: The present invention relates to 1-benzyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## to their preparation and to the pharmaceutical compositions in which they are present. These derivatives have an affinity for the vasopressin and oxytocin receptors.

Abstract: Compounds of formula (I) wherein X is (a) or (b), R is Het as defined in the description. These compounds are oxytocin and vasopressin antagonists useful in the treatment of preterm labor, dysmenorrhea, and for the stoppage of labor preparatory to Cesarean delivery.

Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.

Abstract: Compounds for formula I ##STR1## in which X represents O, NR.sup.a, S, SO or SO.sub.2 and R is as defined in the specification; and non-toxic metabolically labile esters or amides thereof; and pharmaceutically acceptable salts thereof are useful as modulators of metabotropic glutamate receptor function.

Abstract: The invention relates to compounds of formula (I). ##STR1## or a salt, or metabolically labile ester thereof wherein R.sub.1 represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.3 or COR.sub.3 wherein R.sub.3 represents hydroxy, methoxy, or amino; m is zero or an integer 1 or 2;A represents an ethynyl group or an optionally substituted ethenyl group;X represents a bond or a C.sub.1-4 alkylene chain;R.sub.2 represents a bridged cycloalkyl or bridged heterocyclic group; which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.

Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.

Abstract: This invention relates to compositions and methods for achieving a therapeutic effect such as lowering blood pressure and treating congestive heart failure in a mammal. More specifically, this invention relates to synergistic compositions comprising amounts of at least two therapeutic agents selected from the group consisting of a renin inhibitor, an angiotensin I converting enzyme inhibitor and an angiotensin II antagonist, which inhibitors and antagonists are present in amounts sufficient to cause synergistic therapeutic effects such as lowering blood pressure and treating congestive heart failure in a mammal.

Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.

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

Abstract: The invention relates to new 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, X, Y and G have the meanings given in the description, to a plurality of processes for their preparation, and to their use as pesticides.

Abstract: A compound having the structure: ##STR1## pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: The present invention relates to 1-benzyl-1,3-dihydroindol-2-one derivatives of the formula (I). The invention also relates to preparation of these derivatives as well as to the pharmaceutical compositions in which they are present. These derivatives have an affinity for the vasopressin and oxytocin receptors.

Abstract: Invented are methods of inhibiting the production of cytokines, particularly inhibiting the production of interleukin-1 and inhibiting the production of tumor necrosis factor in a mammal in need thereof which comprises administering to such mammal an effective amount of an azaspirane derivative.

Abstract: Invented are substituted azaspirane compounds, pharmaceutical compositions containing these compounds, and methods for using these compounds to induce an immunosuppressive effect in a mammal in need thereof.

Abstract: New fungicidal spiroheterocyclic compounds are described, having the general formula I, ##STR1## or an acid-addition salt thereof, in which R.sup.1 or each R.sup.1 independently represents an optionally substituted alkyl, cycloalkyl, cycloalkylalkyl, alkoxy, cycloalkoxy, alkoxyalkyl, aralkyl, aryl or aryloxy group, or R.sup.1 or each R.sup.1, together with the ring to which they are attached, represents an optionally substituted polycyclic hydrocarbyl group,R.sup.2 represents a hydrogen atom or a C.sub.1-4 alkyl group,R.sup.3 represents a hydrogen atom, a hydroxy group or an optionally substituted alkoxy or acyloxy group,R.sup.4 and R.sup.5 each independently represent a hydrogen atom, an optionally substituted alkyl, alkenyl, alkynyl, cycloalkylalkyl, cycloalkyl, bicycloalkyl, tricycloalkyl, alkoxyalkyl, aryl, aralkyl, haloaralkyl, a 4- to 6- membered heterocyclyl, tetrahydrofurfuryl or dioxolanyl group, or R.sup.4 and R.sup.

Abstract: Compounds of general formula (I), in which r is 1 or 2, R.sub.1 is selected independently from: unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, the 2(beta)-naphthyl group, and heterocyclic, monocyclic or dicyclic groups; R.sub.2 is selected independently from: heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups, and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group comprising from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group.

Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.

Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.

Abstract: There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl, with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.

Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.

Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.

Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.

Abstract: Disclosed are novel compositions comprising mixtures useful to treat the metabolically impaired and to improve patient compliance. Included are non-racemic mixtures of certain chiral spirofluorenehydantoins. Methods of use to treat glucose toxicity and complications arising from diabetes mellitus are also disclosed.

Abstract: The present invention provides methods for blocking sodium channels in cardiac or neuronal tissue using aminocyclohexylamides. This invention also provides kits including aminocyclohexylamides and instructions for the use of the compounds for the treatment of arrhythmia or for the inducement of local anaesthesia.

Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.

Abstract: The invention provides a fungicidal composition comprising at least one systemic, contact and/or soil fungicide and at least one acrylic acid morpholide derivative of the general formula ##STR1## in which R.sub.1 represents a hydrogen, chlorine or bromine atom, a trifluoromethyl, trifluoromethoxy, C.sub.3 -C.sub.7 alkyl, C.sub.3 -C.sub.5 alkoxy, C.sub.3 -C.sub.6 alkenyl, HClFC--CF.sub.2 O--, HClC.dbd.CClO--, cyclohexyl, cyclopentenyl, cyclohexenyl, phenyl, 4-chlorophenyl, 4-ethylphenyl, 4-chlorobenzyl or 4-chlorophenylthio group or a phenoxy group optionally substituted by one or more substituents selected from fluorine and chlorine atoms and methyl and ethoxycarbonyl groups and R.sub.2 represents a hydrogen atom, or R.sub.1 represents a hydrogen atom and R.sub.2 represents a 3-phenoxy group.