Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.

Abstract: The present invention relates to new aromatic compounds, to their preparation and to their use in human and veterinary medicine and in cosmetic compositions.

Abstract: The present invention relates to hydroxy alkyl piperidine compounds and pharmaceutical compositions thereof which can be used to treat diabetes.

Abstract: To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, >N--R.sup.6 or>CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc-; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.

Abstract: The current invention discloses useful pharmaceutical compositions containing azepine derivatives useful as nitric oxide synthase inhibitors.

Abstract: The present invention provides a method for sensitizing hypoxic cells in a tumor to radiation, wherein nitric oxide is delivered to target hypoxic cells through the administration of a nitric oxide-containing compound that spontaneously releases nitric oxide under physiological conditions without requiring the presence of oxygen. Also provided are methods of protecting noncancerous cells or tissues in a mammal from radiation, sensitizing cancerous cells in a mammal to chemotherapeutic agents, and protecting noncancerous cells or tissues in a mammal from chemotherapeutic agents, all by administration of the same compounds.

Abstract: The present invention provides a method for sensitizing hypoxic cells in a tumor to radiation, wherein nitric oxide is delivered to target hypoxic cells through the administration of a nitric oxide-containing compound that spontaneously releases nitric oxide under physiological conditions without requiring the presence of oxygen. Also provided are methods of protecting noncancerous cells or tissues in a mammal from radiation, sensitizing cancerous cells in a mammal to chemotherapeutic agents, and protecting noncancerous cells or tissues in a mammal from chemotherapeutic agents, all by administration of the same compounds.

Abstract: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.6, Q, W and X are as defined herein.

Abstract: The invention relates to a therapeutic composition for topical application containing at least one product with an irritant side effect and a substance P antagonist for reducing or even eliminating the irritant effect of this product.It also relates to the use of a substance P antagonist for the preparation of a pharmaceutical composition for topical application containing at least one product with an irritant side effect for reducing or even eliminating the irritant effect of this product.The substance P antagonist may be a peptide compound or a nitrogen-containing compound or a nitrogen-, sulphur- or oxygen-containing heterocyclic compound.

Abstract: A method for the treatment of mammalian tissue injured or at risk of injury during sepsis or shock including the administration to a mammal a diazeniumdiolate which releases a therapeutically effective amount of nitric oxide sufficient to protect the tissue from sepsis- or shock-induced injury.

Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.

Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.

Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.

Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.

Abstract: Bi-aromatic compounds are provided along with methods for their preparation and use.

Abstract: The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Abstract: The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of the formula ##STR1## wherein W, R.sup.1, R.sup.2, R.sup.3 and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: Compounds of the formula ##STR1## are inhibitors of peptide binding to major histocompatibility complex type II proteins and are useful in the treatment and prevention of autoimmune diseases including: rheumatoid arthritis, Type I diabetes, multiple sclerosis, lupus erythematosis, Graves disease and pemphigus. The present invention also provides novel compositions, methods of treatment employing the compounds of the present invention and methods of manufacture of the compounds of structural formula (I).

Abstract: A method for the treatment of mammalian tissue injured or at risk of injury during sepsis or shock including the administration to a mammal a diazeniumdiolate which releases a therapeutically effective amount of nitric oxide sufficient to protect the tissue from sepsis- or shock-induced injury.

Abstract: A new family of compounds having anti-inflammatory, anti-viral, and brocho-dilating activity having the following linear and cyclic formulas: ##STR1## and compositions of these, which alone, and in combination with reverse transcriptase inhibitors thereby resulting in an additive or synergistic effect, are useful in inhibiting or suppressing viruses including those exhibiting retroviral replication, or in treating viruses including a retrovirus such as HIV in a human cell population and methods of using these compositions, compounds, and salts thereof.

Abstract: A method for inhibiting the adherence between cancerous cells and noncancerous structures in a mammal, comprising the administration to the mammal of a nitric oxide-releasing compound containing a nitric oxide-releasing N.sub.2 O.sub.2.sup.- functional group. The compound is capable of releasing an adherence-inhibiting effective amount of nitric oxide to the mammal.

Abstract: N-(3-Pyrrodinyl)benzamide derivatives represented by the following general formula (I) which have potent and selective antagonism against dopamine D.sub.3 and/or D.sub.4 receptor and are useful as a psychotropic, a schizophrenia-treating agent and the like, or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation thereof.

Abstract: The present invention provides a method for sensitizing hypoxic cells in a tumor to radiation, wherein nitric oxide is delivered to target hypoxic cells through the administration of a nitric oxide-containing compound that spontaneously releases nitric oxide under physiological conditions without requiring the presence of oxygen. Also provided are methods of protecting noncancerous cells or tissues in a mammal from radiation, sensitizing cancerous cells in a mammal to chemotherapeutic agents, and protecting noncancerous cells or tissues in a mammal from chemotherapeutic agents, all by administration of the same compounds.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are Factor Xa inhibitors. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.

Abstract: N,N-disubstituted-guanidines, e.g., of the formula ##STR1## wherein R and R' are substituted or unsubstituted hydrocarbon groups. Methods are provided for the treatment of psychosis and hypertension by administering an effective amount of an N,N'-disubstituted guanidine which, preferably, has a high affinity for the sigma receptor.

Abstract: The present invention relates to novel azanorbornane derivatives having the formula ##STR1## wherein R.sup.1 through R.sup.12 are defined as below, and to novel intermediates used in their synthesis. The compounds having formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: Ionene polymers having biologically-active organic and/or inorganic anions are described. Methods to prepare the ionene polymers, compositions containing them and their methods of use are also described.

Abstract: The present invention is concerned with antiretroviral (e.g. anti-HIV-1) compounds having the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are halo or methyl; R.sup.3 is hydrogen, halo, nitro or trifluoromethyl; R.sup.4 is trifluoromethyl or methylcarbonyl; or a radical --C(.dbd.X)--NR.sup.5 R.sup.6 wherein X is O or S, and R.sup.5 and R.sup.6 each independently are hydrogen or C.sub.1-4 alkyl; or a radical --Alk--R.sup.7, wherein Alk is C.sub.1-4 alkanediyl; and R.sup.7 is hydrogen or hydroxy; Het is a heterocyclic radical of formula: ##STR2## Pharmaceutical compositions containing said compounds of formula (I) and processes of preparing said compounds and compositions.

Abstract: Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro,Y is an amino, methylamino or dimethylamino group,Z is a group CHCH.sub.3, CHOCH.sub.3 or NOCH.sub.3,R is hydrogen or alkyl,A is hydrogen, alkyl, haloalkyl or cycloalkyl,B is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl or the group ##STR2## where W is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino, unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted aryloxy, arylthio, arylamino or aryl-N-(C.sub.1 -C.sub.6 -alkyl)amino, heteroaryloxy, heteroarylthio, heteroarylamino or heteroaryl-N-(alkyl)amino orA and B, together with the C atom whose substituents they are, are an isocyclic or heterocyclic ring which can also be quinonoid,and fungicides containing these compounds.

Abstract: Novel substituted 2-arylpyrroles of the formula (I) are described ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, Ar, Y.sup.1 and Y.sup.2 have the meaning given in the description, as is a process for their preparation.The novel 2-arylpyrroles are used as agents for combating pests.

Abstract: Compounds of formula I ##STR1## wherein X is oxygen or sulphur, W is CH or N, m is 0 or 1, and either a) n is 1 and Q is a non-aromatic heterocyclic ring of 3 to 10 ring atoms, containing one to three hetero atoms selected from oxygen, sulphur and nitrogen, which may be substituted and may be fused to another ring, with the proviso a) that if Q is thiazol-2-in-2-yl, it is substituted but not by methylene, and b) Q is not a six membered ring containing only two nitrogen atoms, or b) n is 0 or 1 and Q is ##STR2## where R.sup.1 is alkyl, alkoxy or alkylthio, and R.sup.2 is heteroaryl, non aromatic heterocyclyl, optionally substituted cycloalkyl or optionally substituted alkyl containing at least 5 carbon atoms, phenyl substituted by one or more groups selected from halogen, optionally substituted alkyl, alkoxy, haloalkoxy, aryloxy, alkylthio and alkoxycarbonyl, and when R.sup.1 is alkyl or alkoxy, or, when W is nitrogen, R.sup.2 can also be unsubstituted phenyl, have pesticidal especially fungicidal activity.

Abstract: Benzyl derivatives of the formula I ##STR1## where A is CH.sub.2, CHCl, CH-alkyl, CH-alkoxy, CH-alkylthio or N-alkoxy,B is OH, alkylthio, alkoxy or alkylamino,U, V, W are hydrogen, halogen, alkyl or alkoxy,D is ##STR2## where R' is hydrogen or alkyl andR is hydrogen, alkyl, cycloalkyl, haloalkyl, halocycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aryl, arylalkyl, hetaryl, hetaryl-alkyl, hetaryloxyalkyl or heterocyclyl, and fungicides containing these compounds.

Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, Het and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula I are useful in the treatment of cardiovascular diseases.

Abstract: The present invention provides insecticidal and acaricidal suspension concentrate compositions of arylpyrrole compounds.

Abstract: The present invention comprises dipeptide analogs that inhibit the farnesylation of Ras. These farnesyl-protein transferase inhibitors are characterized by the inclusion of a cyclic amine in the backbone of the dipeptide. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

Abstract: Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.

Abstract: This invention relates to a method for administering systemically active agents through the skin or mucosal membranes of humans and animals and into the bloodstream in a transdermal device or formulation comprising topically administrating with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula ##STR1## or the pharmaceutically acceptable salt thereof wherein W represents oxygen, sulfur or two hydrogen radicals; Z represents --CH.sub.2 --; R represents alkyl optionally substituted with one to three double or triple bonds, --SR"', --OR"', --NHR"', or --COOR.sub.1 ; R"' represents alkyl, alkylthioalkyl, alkoxyalkyl, amino alkyl, optionally substituted with a phenyl, or benzoyl; R' represents hydrogen, alkyl, alkoxy, acyloxy, alkylthio, hydroxy or --(CH.sub.2).sub.y COOR.sub.1 ; R" represents hydrogen or --(CH.sub.2).sub.y COOR.sub.1 ; R.sub.

Abstract: The instant invention is directed to the use of a biologically compatible composition, containing an effective amount of a metal independent nitroxide compound which is preferably represented by the formula ##STR1## wherein R.sub.1 is --CH.sub.3 ; R.sub.2 is --C.sub.2 H.sub.5, --C.sub.3 H.sub.7, --C.sub.4 H.sub.9, --C.sub.5 H.sub.11, --C.sub.6 H.sub.13, --CH.sub.2 --CH(CH.sub.3).sub.2, --CHCH.sub.3 C.sub.2 H.sub.5, or --(CH.sub.2).sub.7 --CH.sub.3, or wherein R.sub.1 and R.sub.2 together form spirocyclopentane, spirocyclohexane, spirocycloheptane, spirocyclooctane, 5-cholestane, or norbornane, R.sub.3 is --O. or --OH, or a physiologically acceptable salt thereof, and a pharmaceutically acceptable carrier, as antioxidants capable of protecting cells, tissues, organs, and whole organisms against the deleterious effects of harmful oxygen-derived species generated during oxidative stress.

Abstract: There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted) pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.

Abstract: A cycloalkylurea compound of the formula (I): ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, which compound inhibits ACAT and is useful as hypolipidemic and antiatherosclerotic medicine.

Abstract: Benzyl derivatives of the formula I ##STR1## where A isCH.sub.2, CHCl, CH-alkyl, CH-alkoxy, CH-alkylthio or N-alkoxy,B isOH, alkylthio, alkoxy or alkylamino,U, V, W arehydrogen, halogen, alkyl or alkoxy,D is ##STR2## where R' ishydrogen or alkyl andR ishydrogen, alkyl, cycloalkyl, haloalkyl, halocycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aryl, arylalkyl, hetaryl, hetaryl-alkyl, hetaryloxyalkyl or heterocyclyl, and fungicides containing these compounds.

Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.

Abstract: There are disclosed cardiovascularly active compounds possessing antihypertensive properties, and pharmaceutical compositions containing these agents and a method of treating cardiovascular disorders with the compounds. The active components of the pharmaceutical compositions are compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from straight chain and branched chain alkyl and olefinic groups, which may be unsubstituted or substituted; or R.sub.1 and R.sub.2 together with the nitrogen atom they are bonded to form a heterocyclic group; and R.sub.3 is a pharmaceutically acceptable organic group selected from alkyl and olefinic groups which may be unsubstituted or substituted, acyl, a sulfonyl, sulfinyl, sulfenyl, carbonate, or carbamate derivative; or R.sub.3 is a group of the formula--(CH.sub.2).sub.n ONN(O)NR.sub.1 R.sub.2, wherein n is 2-8, and R.sub.1 and R.sub.2 are as described above. Novel compounds are disclosed wherein at least one of R.sub.1, R.sub.2 and R.sub.

Abstract: A derivative of general formula: ##STR1## wherein Y is --SO.sub.2 -- or ##STR2## (i) R.sup.1 and R.sup.2, which may the same or different, each represent, (1) --H, (2) C1-16 alkyl or (3) the formula: --X--A-- (R.sup.4)n wherein X is single-bond, --SO.sub.2 --, C1-4 alkylene, C1-4 alkylene substituted by --COOH or ##STR3## --A-- is a pyridyl or pyrrolyl ring, n is 1.about.5, R.sup.4 is 1 --H or C1-8 alkyl, 2 C1-14 alkoxy, 3 C1-6 alkylthio, 4 --OH, halogen, --NO.sub.2 or trihalomethyl, 5 the formula: --NR.sup.41 R.sup.42 wherein R.sup.41 and R.sup.42 each represents halogen or C1-4 alkyl, 6 tetrazole, 7 --SO.sub.3 H or --CH.sub.2 OH, 8 the formula: --SO.sub.2 NR.sup.41 R.sup.42 9 the formula: --Z.sup.41 --COOR.sup.43 wherein Z.sup.41 is single-bond, C1-4 alkylene or C2-4 alkenylene, R.sup.

Abstract: A naphthoic acid derivative represented by the following general formula or a salt thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, a lower alkanoyloxy group, a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkanoyloxy-lower alkyl group or an aralkyloxy group;R.sub.4 is a hydrogen atom or a lower alkyl group;R.sub.5 is a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaromatic group;X is a group ##STR2## a cycloalkylene group, a bivalent nitrogen-containing heterocyclic group, or a group ##STR3## --R.sub.8 --NH-- or --NH--R.sub.8, where R.sub.6 and R.sub.7 are each a hydrogen atom or a lower alkyl group and R.sub.8 is a cycloalkylene group, or R.sub.6 and R.sub.7, together with R.sub.4, may form an alkylene group of 1-3 carbon atoms;Y is --S(O).sub.p --, --(CH.sub.2).sub.

Abstract: Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are each (C.sub.2 -C.sub.6)alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R.sup.3 and R.sup.4 are the same as R.sup.1 and R.sup.2 or are H and Ar is a heteroaromatic ring and the pharmaceutically acceptable salts thereof.

Abstract: Compounds of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is hydrogen, amino, protected amino, acylamino or lower alkyl optionally substituted by aryl, hydroxy, protected hydroxy, amino, protected amino, acylamino, maleimido, succinimido, naphthalimido, 2,3-dihydro-1,3-dioxo-1H-benz[d,e]isoquinol-2-yl, carboxy, protected carboxy, carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, carboxy-lower alkanoylamino, pyrrolidino or morpholino; R.sup.2 is hydrogen or lower alkyl optionally substituted by aryl, amino, protected amino, di(lower alkyl)- amino, guanidino, carboxyl, protected carboxyl, carbamoyl, mono(lower alkyl) carbamoyl, di(lower alkyl)carbamoyl, di(lower alkoxy)phosphinyl, dihydroxyphosphinyl, pyrrolidino, piperidino or morpholino; R.sup.3 is hydrogen or lower alkyl optionally substituted by hydroxy, protected hydroxy, amino or protected amino; R.sup.4 is hydrogen, hydroxy, lower alkoxy or benzyloxy; and R.sup.

Abstract: Compounds of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, m, n, and R are as defined in the Specification.Medicinal products containing the same are useful in the treatment or prevention of thrombotic afflictions due to their thromboxane A.sub.2 receptor antagonistic activity and their thromboxane A.sub.2 synthase inhibitory activity.

Abstract: An oral solid preparation comprising an organic acid or its salt and a catechol compound. The catechol compound is, for example, a pyrrolidine derivative having a catechol group of the following general formula (I). It exhibits an improved absorbability in vivo.