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 present invention relates to methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compositions comprise a neurotrophic amount of a compound which binds to the FK-506 binding protein (FKBP) and a neurotrophic factor, such as nerve growth factor NGF. The methods comprise treating nerve cells with the above-described compositions or compositions comprising the FKBP binding compound without a neurotrophic factor. The methods of this invention can be used to promote repair of neuronal damage caused by disease or physical trauma.

Abstract: Derivatives useful in the protection of living organisms against damage due to free radical reactions derived from methoxypolyethylene glycols (MPEG), which are modified by chemically attaching chelating groups in an amide or amine linkage to the nonmethyl end of the polymer. Such chelating groups include ethylene-diamine tetraacetic acid (EDTA), diethylene triamine pentaacetic acid (DTPA), and ethylene glycol aminoethyl ether tetraacetic acid (EGTA), and pharmacologically acceptable salts or esters thereof.

Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.

Abstract: The invention comprises a novel pyruvate compound for the treatment of prevention of reperfusion injury following ischemia, diabetic effects, cholesterol levels, injured organs ethanol intoxication oras s foodstuff. The novel pyruvate compound is particularly a puruvate thiolester, a glucerol-pyruvate ester or a dihydoxyacetone-pyruvate ester.

Abstract: The use of L-carnitine or of an alkanoyl L-carnitine or their pharmacologically acceptable salts is described for producing a medicament for inhibiting nephrotoxicity and vasculotoxicity resulting from the administration of an immunosuppressant drug such as cyclosporin-A, tacrolimus, rapamicine and deoxyspergualine.

Abstract: The invention is directed to nitric oxide (NO) donor compounds and to pharmaceutical compositions containing such nitric oxide (NO) donor compounds, for delivering NO to the apical surface of a mucosa, where the nitric oxide is released for passage across the epithelial monolayer of the mucous membrane. The NO donor compounds include polyalkyleneamine NO donors as well as tertiary and quaternary amino aliphatic NO donor compounds. The compounds and compositions of the invention are useful in any situation in which it is desirable to deliver NO across a mucosal surface. For example, the compounds and compositions of the invention are particularly useful in treating pulmonary hypertension, male impotence, and several other specific conditions.

Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: The present invention provides the compound having the structure: ##STR1## wherein each of R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine, or thiozoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, wherein each of R.sub.3 and R.sub.4 are independently the same as or different from each other and are a hydrogen atom, a hydroxyl group, a substituted or unsubstituted, branched or unbranched alkyl, alkenyl, cycloalkyl, aryl, alkyloxy, aryloxy, arylalkyloxy, or pyridine group, or R.sub.3 and R.sub.4 bond together to form a piperidine group and R.sub.2 is a hydroxylamino, hydroxyl, amino, alkylamino, dialkylamino or alkyloxy group; and n is an integer from about 4 to about 8.

Abstract: Described are the use of compounds of Formula (I), depicted below, as active principals for treating skin conditions; compositions containing these compounds; and methods of treating skin conditions using these compounds and compositions. ##STR1## wherein R.sub.4 is (CR.sub.5 R.sub.6 --CR.sub.7 R.sub.8 --X.sub.1).sub.n --CR.sub.9 R.sub.10 --C(.dbd.X.sub.2)X.sub.3 R.sub.11, n is an integer from 1 to 18; R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.11, are independently, hydrogen or non-hydrogen substituents; and X, X.sub.1, X.sub.2, X.sub.3, Y and Z are independently, O, NH, or S.

Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.

Abstract: Amidino derivatives of formula (I) and salts, and pharmaceutically acceptable esters and amides thereof, in which: R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group; Q is an alkylene, alkenylene or alkynylene group having 3 to 6 carbon atoms and which may optionally be substituted by one or more C.sub.1-3 alkyl groups; a group of formula --(CH.sub.2).sub.p X(CH.sub.2).sub.q -- where p is 2 or 3, q is 1 or 2 and X is S(O).sub.x where x is 0, 1 or 2, O or NR.sup.2 where R.sup.2 is H or C.sub.1-6 alkyl; or a group of formula --(CH.sub.2).sub.r A(CH.sub.2).sub.s -- where r is 0, 1 or 2, s is 0, 1 or 2 and A is a 3 to 6 membered carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or diC.sub.

Abstract: A method for preventing settlement of aquatic fouling organisms on surface of an aquatic structure without environmental hazard is provided. The method is based upon absolutely novel concept to prevent the settlement by means of thick slime layer, i.e. bio-jelly, deposited on said surface. The present invention also provides a bio-jelly producing agent and a bio-jelly producing paint both useful for the present method. Further, the present invention provides a novel low toxic antifouling agent.

Abstract: This invention is directed to methods of administering physiologically stable and safe compositions of butyric acid salts and derivatives to a patient for the purpose of wound healing.

Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Abstract: Tat-inhibitory oligocarbamate derivatives of the formula I ##STR1## and analogs thereof, and the biologically and pharmaceutically acceptable salts thereof exhibit advantageous properties, including specific binding to TAR RNA with high affinities, and stability of the resultant oligocarbamate-RNA complexes to proteolytic digestion. Site-specific photocrosslinking experiments using a photoactive analog (4-thio-uracil) containing TAR RNA indicate that these oligocarbamates interact with RNA in the major groove. These oligocarbamates are thus capable of competing with the TAR RNA-binding domain of Tat protein and thus are useful as a therapeutic agents in the treatment of AIDS.

Abstract: A glycine uptake antagonist is administered for augmenting NMDA receptor-mediated neurotransmission treating symptoms of psychosis and of schizophrenia.

Abstract: A method for protecting a crop against fungal diseases by inducing local and systemic resistance of the crop comprising applying to the crop or its locus a composition containing an effective amount of a .beta.-aminobutyric acid or .beta.-amino valeric acid and derivatives thereof.

Abstract: N-?Mercaptoacyl(amino acid or peptide)! compounds and S-lipophilic aliphatic carbonyl derivatives thereof, and pharmaceutical compositions comprising such compounds, as well as the use of these compounds as antihypertensives by the inhibition of neutral endopeptidase and/or peptidyldipeptidase A are disclosed. Methods for preparing such compounds and derivatives are disclosed also.

Abstract: This invention relates to the method of using specially formulated neurotrophic pipecolic acid derivative compounds having an affinity for FKBP-type immunophilins as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity to stimulate or promote neuronal growth or regeneration.

Abstract: A novel amino acid derivative represented by the general formula (I) shown below or a salt thereof have now been provided by chemical synthesis, and it has been found that these new compounds stimulate proliferation and physiological activities of the T cells of mammals, have an immunomodulating activity and also have an antitumor activity or a carcinostatic activity. It has also been found that these new compounds have an effect of stimulating the proliferation of hematopoietic stem cells. ##STR1## wherein y is 0 or 1; R.sup.1 represents an unsubstituted C.sub.1 -C.sub.8 alkyl group or others;R.sup.2 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group or others;R.sup.3 represents a hydrogen atom, a C.sub.1 -C.sub.8 alkyl group or others;R.sup.4 represents a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group or others;R.sup.5 represents a group --OR.sup.42, a group ##STR2## or others.

Abstract: A compound of the formula ##STR1## wherein R.sup.1 is carboxy or protected carboxy,R.sup.2 is hydrogen, hydroxy or protected hydroxy,R.sup.3 is hydrogen, hydroxy, protected hydroxy, etc.,R.sup.4 is hydrogen or halogen,A.sup.1 is lower alkylene,A.sup.2 is bond or lower alkylene,--R.sup.5 is ##STR2## (in which R.sup.6 is mono(or di or tri)aryl(lower)alkyl and Z is N or CH), etc., and ##STR3## and a pharmaceutically acceptable salt thereof which are useful as medicaments.

Abstract: A novel therapeutic use of L-carnitine or alkanoyl L-carnitine is disclosed in combination with a polyunsaturated fatty acid of the omega-3 series, for the prevention and the treatment of lipid metabolism disorders and cardiovascular disorders.

Abstract: The present invention provides 2,5-diamino-3,4-disubstituted-1,6-diphenylhexane (DAD) isosteres comprising benzamide, sulfonamide and anthranilamide subunits, a pharmaceutical composition comprising such compounds, a method of using such compounds to treat retroviral, specifically HIV and more specifically HIV-1 and HIV-2, infections in mammals, particularly humans, a method of synthesizing asymmetric DAD isosteres comprising benzamide, sulfonamide and anthranilamide subunits, and a method of using such compounds to assay new compounds for antiretroviral activity.

Abstract: The present invention is directed to a new class of compound which are useful as inhibitors of the biosynthesis of nitric oxide.

Abstract: This invention is directed to compounds having the structure: ##STR1## wherein R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine or thiazoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, and n is an integer from about 4 to about 8. This invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of the compounds of the present invention and a pharmaceutically acceptable carrier.

Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.

Abstract: This invention provides a compound having the formula R.sup.1 --Y.sup.1 --CHZ.sup.1 --CH(NY.sup.2 Y.sup.3)--CH.sub.2 --Z.sup.2, wherein: R.sup.1 is a straight-chained alkyl, alkenyl or alkynyl group having from 8 to 19 carbon atoms in the aliphatic chain; Y.sup.1 is --CH.dbd.CH--, --C.tbd.C-- or --CH(OH)CH(OH)--; Z.sup.1 is OH or a conversion-inhibiting group; Z.sup.2 is a conversion-inhibiting group; Y.sup.2 is H, a phenyl group, an alkyl-substituted phenyl group having from 1 to about 6 carbons in the alkyl chain, or an alkyl chain having from 1 to 6 carbons; Y.sup.3 is H or a group having the formula --C(O)R.sup.2 or --S(O).sub.2 R.sup.2 ; R.sup.2 is a straight-chained alkyl, alkenyl or alkynyl group having from 1 to 23 carbon atoms in the chain; and when Z.sup.2 is an amino, R.sup.2 is an aliphatic chain having from 1 to 9 or from 19 to 23 carbon atoms in the aliphatic chain.

Abstract: N-arylalkylphenylacetamide compounds of formula (I), and pharmaceutically acceptable salts thereof, possess potent analgesic and anti-inflammatory activities.

Abstract: A method of treating anxiety in a warm blooded animal by administering an anti-anxiety effective amount of a nitric oxide synthase inhibitor, and compositions containing the same.

Abstract: The present invention relates to methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compositions comprise a neurotrophic amount of a compound which binds to the FK-506 binding protein (FKBP) and a neurotrophic factor, such as nerve growth factor NGF. The methods comprise treating nerve cells with the above-described compositions or compositions comprising the FKBP binding compound without a neurotrophic factor. The methods of this invention can be used to promote repair of neuronal damage caused by disease or physical trauma.

Abstract: A human or animal subject having a solid tumour is treated by administering to the subject therapeutically effective amounts of a nitric oxide (NO) synthase inhibitor and a compound which is an imidazole or 1,2,4-triazole derivative of formula (A) ##STR1## wherein X is selected from the group consisting of ##STR2## wherein R is hydrogen or a C.sub.1 -C.sub.6 alkyl group; each of R'.sub.1 to R'.sub.5 is independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, hydroxy(C.sub.1 -C.sub.6 alkyl), phenyl, (C.sub.1 -C.sub.6 alkyl)phenyl and phenyl(C.sub.1 -C.sub.6 alkyl); m is 0 or 1; n is 1 or 2; and Z' represents a leaving group which has the potential for expulsion via an intramolecular cyclisation reaction and which is not negatively-charged; or a physiologically acceptable acid addition salt thereof.

Abstract: A method is disclosed for lowering the concentration of a serum lipid or lipoprotein component in a mammal, including the step of administering to a mammal in need of such treatment a hypolipidemic, therapeutically effective amount of at least one creatine derivative.

Abstract: Dermatosis is treated by a method comprising topically applying an effective amount of an ester of L-carnitine or an acyl L-carnitine with a hydroxy carboxylic acid selected from the group consisting of .alpha.-hydroxybutyric acid, .alpha.-hydroxyisocaproic acid, .alpha.-hydroxyisovaleric acid, malic acid and tartronic acid, to a patient in need thereof.

Abstract: A method of treating emesis in a warm blooded animal by administering an anti-emesis effective amount of a nitric oxide synthase inhibitor and compositions containing the same.

Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.

Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl derivatives, substituted in the 1-position with halo, methyl, hydroxyl, nitro, amino, amido, azido, oxime, cyano, thiol, either or thioether groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) derivatives. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) derivatives of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) derivatives of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.

Abstract: Obesity is treated by the administration to a subject of a compound having the general formula (I): R.sub.4 --(CH.sub.2).sub.n --CO--N(R.sub.1)--CH(R.sub.2)--CO(--R.sub.3), wherein R.sub.1 represents H or CH.sub.3 ; R.sub.2 represents a side chain of a naturally occurring amino acid; R.sub.3 represents OH, OCH.sub.2 CH.sub.3 and NH.sub.2 ; n is 6-18; and R.sub.4 represents CH.sub.3 or a group having the general formula (II): R.sub.3 --CO--CH(R.sub.2)--N(R.sub.1)--CO--, wherein R.sub.1, R.sub.2 and R.sub.3 have the above meanings. The compounds of formula (I) wherein R.sub.4 is a group of formula (II), are novel compounds.

Abstract: A topical treatment for hemorrhoidal pain and for spasms of the sphincters and muscles located in the gastrointestinal (GI) tract is disclosed. The topical preparation includes the amino acid L-arginine in a pharmaceutically acceptable carrier substance, e.g., K-Y jelly, suppository, or ingestible formulation, and can be applied directly to the affected area. The topical preparation of the invention is effective for relieving the pain of hemorrhoids or for treating conditions resulting from spasms of sphincters of the GI tract including anal fissure, post operative rectal pain, hypertrophic pyloric stenosis, and pancreatitis, as well as conditions resulting from general spasm of the muscles of the GI tract.

Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukinprotease activity. The compounds, .alpha.-substituted acetamides a ##STR1## wherein: R.sub.2 =H or alkyl;R.sup.3 =halo, O(CO).sub.0-1 aryl, OPOR.sup.4 R.sup.5 ; ##STR2## where R.sup.4 and R.sup.5 =aryl;R.sup.6 =H, aryl or aralkyl;R.sup.7 =independently selected from R.sup.6, CF.sub.3 and CF.sub.2 CF.sub.3 ;R.sup.1 =R.sup.6 -CO, heteroaryl-CO, heteroaralkyl-CO and amino acid.

Abstract: The present invention is directed to the use of an inhibitor of NO activity, such as a nitric oxide scavenger or an NO synthase inhibitor, as an antitumor therapy to reduce tumor blood flow and oxygenation. The invention is also directed to administration of a nitric oxide scavenger or a nitric oxide synthase inhibitor to enhance the effectiveness of tumor therapy with hypoxic or acidic chemotherapeutic agents or hyperthermia. The invention is also directed to the administration of a nitric oxide synthase substrate to a subject previously administered a nitric oxide synthase inhibitor, in order to selectively inhibit tumor perfusion. In a specific example, administration of cell free hemoglobin, a nitric oxide scavenger, in conjunction with mitomycin C, a hypoxic cytotoxin, results in a significant delay in tumor growth of a human tumor xenograft in a mouse compared to mitomycin C alone.

Abstract: It has been found that certain combinations of substituted imidazoline-based amphoterics and quaternary ammonium compounds show markedly reduced irritation profile in addition to providing excellent cleaning detergency. Moreover, it has further been found that certain substituted imidazoline amphoteric surfactants in combination with didecyl dimethyl ammonium chloride (DIDAC) show unexpected synergistic irritation reduction compared to that observed when the quaternary is an ADBAC type. This allows the formulation of disinfectants and sanitizers with the favored antimicrobial agent while at the same time affording the optimum reduction in irritation potential.

Abstract: A method for inhibiting or relaxing skeletal muscle contractions and for treating disease states resulting from or exacerbated by undesirable skeletal muscle contractions by administering a skeletal muscle relaxing amount of nitroxyl ion(NO.sup.-), nitrosonium ion(NO.sup.+), nitric oxide and nitric oxide adducts or providers. A process for stimulating, improving or enhancing muscle contraction in a mammal by treating the mammal with an effective amount of (i) a nitric oxide synthase inhibitor or (ii) a nitric oxide scavenger.

Abstract: The esters of acyl L-carnitines with gamma-hydroxybutyric acid in the form of pharmacologically acceptable salts of formula (I) ##STR1## wherein X.sup.- is the anion of a pharmacologically acceptable salt, e.g. chloride, bromide, orotate, acid aspartate, acid citrate, acid phosphate, acid fumarate, lactate, acid maleate, acid oxalate, acid sulfate and glucosephosphate or in the form of inner salts of formula (I') ##STR2## wherein R is a straight or branched acyl group having from 2 to 5 carbon atoms, such as e.g. acetyl, propionyl, n,butyryl, isobutyryl and isovaleryl, are active in inhibiting neuronal degeneration (as it occurs in Alzheimer's senile dementia and Parkinson's disease) and in the treatment of coma.

Abstract: The present invention provides a pharmaceutical compositions suitable for the treatment of brain diseases characterized by excessive activity of brain dopamine systems and/or nitric oxide systems. Also provided is a method of treating psychiatric and neurologic diseases.

Abstract: Hydroquinone amino-acid esters having formula (I), pharmaceutical or cosmetic compositions containing them, particularly dermatological compositions having pigment-removing activity, and the pharmaceutical, cosmetic or aesthetic uses thereof. The preparation of these novel hydroquinone esters from natural amino-acid derivatives is also described.

Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.

Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: A preparation for reducing intraocular pressure consisting essentially of a therapeutically effective amount of the fixed combination of dipivalylepinephrine and carbachol (preparation 1) or dipivalylepinephrine and beta-blocker (preparation 2). The preparations may be prepared both as a solution and as a suspension. Either preparation is administered twice daily.

Abstract: The invention concerns 2-aminocarboxylic acids and derivatives of formula ##STR1## processes for their preparation, as well as medicaments containing them for the inhibition of protein kinase C and thus for the prevention and/or treatment of heart and blood vessel diseases, such as thromboses, arterioscleroses, hypertension, of inflammatory processes, allergies, cancers, and certain degenerative damages of the central nervous system.