Abstract: Described herein are compounds having the general formula: ##STR1## Ar.sub.1 and Ar.sub.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;wherein any cycloalkyl or aryl substituent is linked to Ar.sub.1 or Ar.sub.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;wherein Ar.sub.1 and Ar.sub.

Abstract: Left ventricular dysfunction is treated by a process, comprising:administering to a subject suffering from left ventricular remodeling a therapeutically effective amount of 5,6-dihydroxy-2-methylaminotetralin, or 5,6-diisobutyroyl-oxy-2-methyl-aminotetralin, or a pharmaceutically acceptable salt thereof in combination with an angiotensin-converting enzyme inhibitor.

Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be calorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.

Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.

Abstract: A composition for the upregulation of expression of cell antigens, without inducing shedding, which comprises a protein kinase C activator is provided by this invention. Further provided by this invention is a method of detecting and treating tumor cells comprising contacting tumor cells with an effective amount of a protein kinase C activator for the upregulation of expression of antigens of tumor cells, without inducing antigen shedding, and detecting the presence of said antigen or then further contacting said tumor cells with an effective amount of an antibody directed to said antigen.

Abstract: A method is provided for inhibiting or treating diseases associated with acid lipase deficiency by administering to a patient an MTP inhibitor, alone or optionally, in combination with another cholesterol lowering drug, such as pravastatin.

Abstract: Phorbol esters and particularly phorbol-12-myristate-13-acetate (TPA) are described as effective in treating patients with neoplastic diseases such as leukemia as well as in increasing the white blood cell count.

Abstract: The use of a combination of an alpha RAR receptor-specific agonist ligand and a gamma RAR receptor-specific antagonist ligand to reduce the rate of apoptosis is disclosed.

Abstract: A pine root (Deutero mycetes) fungal metabolite and analogs thereof having antifungal activity.

Abstract: A method is provided for inhibiting onset of or treating phytosterolemia by administering to a patient an MTP inhibitor, alone or optionally, in combination with another cholesterol lowering drug, such as pravastatin.

Abstract: The compounds of Formula I are useful as immunosuppressive agents.

Abstract: The invention relates to use of betulinic acid and/or its derivatives for treating, inhibiting, and/or preventing tumors or cancer growth more particularly, to treating leukemia, lymphomas, lung, prostate and ovarian cancer. This invention also relates to novel betulinic acid derivatives and a composition containing betulinic acid derivatives with or without betulinic acid.

Abstract: A method is described for treating bacterially induced meningitis, comprising administering a prostane derivative of formula I or Ia ##STR1## wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described below, and the --O--R.sup.3 -- group is in the .alpha.- or .beta.-configuration. The prostane derivative can optionally comprise or serve as an adjuvant, and it can be administered in combination with an antiobiotic.

Abstract: The present invention provides a method of inhibiting influenza and flaviviral replication based on a mechanism of action in which HA-mediated fusion or E protein mediated fusion is inhibited by a fusion inhibiting agent which binds, complexes or otherwise becomes associated with HA or E protein during the translation of the target protein and/or its vesicular transport.

Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.

Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; X and Y represent an oxygen atom, a sulfur atom, a carbonyl group or a group of the formula --CHR.sup.a -- (wherein R.sup.a is a hydrogen atom or a lower alkyl group) or --NR.sup.b -- (wherein R.sup.b is a hydrogen atom or a lower alkyl group), or X and Y together represent a vinylene group or an ethynylene group; R.sup.1, R.sup.2, R.sup.3, R.sup.8 and R.sup.9 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.4 and R.sup.

Abstract: Compounds of formula (I): in which:R.sub.a and R.sub.b, identical or different, represent hydrogen or alkyl or together form a bond,R.sub.C represents hydroxyl optionally substituted alkoxy, or optionally substituted amino,R.sub.1 represents hydrogen or --O--NO.sub.2, --O--NO, or --S--NO,R.sub.2 and R.sub.3, identical or different, represent hydrogen, alkyl, or optionally substituted phenyl,X represents oxygen or --NH--CO--,m represents 0 or 1,n represents an integer such that 0.ltoreq.n.ltoreq.6,p represents 0 or 1,R.sub.4 represents hydrogen, optionally substituted alkyl, optionally substituted phenyl, or a group as defined in the description,R.sub.5 represents hydrogen or alkyl,R.sub.6 represents hydrogen or alkyl,or R.sub.5 and R.sub.6 together form a chain --(CH.sub.2).sub.t -- in which t represents 1 or 2,q represents 0, 1, or 2,r represents an integer such that 0.ltoreq.r.ltoreq.6,R.sub.d and R.sub.

Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification.

Abstract: The invention is novel analogs of 9-cis-retinoic acid which are useful for the treatment and prevention of coronary artery disease and to protect against premature atherosclerosis by increasing HDL levels. The invention includes processes for preparing the novel 9-cis-retinoic acid analogs.

Abstract: A pharmaceutical composition for treating peripheral circulation disorders, which is an emulsion containing an isocarbacyclin having the following formula (1): ##STR1## wherein R.sup.1 is a hydrogen atom or alkyl group and R.sup.2 is a alkyl group which may be substituted with, a alkenyl group or alkynyl group which may be substituted with, or a cycloalkyl group which may be substituted with, in an amount of 0.2 to 1,000 .mu.g per ml of the composition, a vegetable oil in an amount of 0.05 to 0.5 g per ml of the composition, a phospholipid in an amount of 0.01 to 0.5 g per g of the vegetable oil, and water is provided.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: The present invention relates to a composition for treating or preventing brain edemas which comprises containing an endothelin antagonist as an active ingredient, for example, the compound of the following formula (I): ##STR1## or pharmaceutically acceptable salts or hydrates thereof, bosentan, cyclo?D-aspartyl-L-?3-(4-phenylpiperazin-1-ylcarbonyl)!-alanyl-L-aspartyl- D-?2-(2-thienyl)!glycyl-L-leucyl-D-tryptophyl!disodium or cyclo ?D-Asp-L-Pro-D-Val-L-Leu-D-Trp!.Furthermore, the present invention provides a method for treating or preventing brain edemas, which comprises administering an effective amount of an endothelin antagonist and use of an endothelin antagonist for the manufacture of a medicament for treating or preventing brain edemas.An endothelin antagonist exhibits an inhibitory effect, on all brain edemas regardless of the onset mechanism and thus is highly useful in the treatment or prevention of brain edemas.

Abstract: A method of treating cancer with a pharmaceutical composition containing a pine root (Deutero Mycetes) fungal metabolite or an analog or derivative thereof.

Abstract: The present invention relates to the use of pure boswellic acid, a physiologically acceptable salt, a derivative, a salt of said derivative or a vegetable preparation containing boswellic acid for the preparation of a pharmaceutical composition for the treatment of brain tumours.

Abstract: The instant invention provides a series of naphthyl compounds having an oxygen linker at the 1-position which are useful as selective estrogen receptor modulators.

Abstract: Compounds of the formula ##STR1## in which X represents a bond, S, O or NR.sup.a ; and R is as defined in the specification are useful as modulators of metabotropic glutamate receptor function.

Abstract: A nasally administrable composition having a physiologically active peptide dispersed homogeneously in and adsorbed homogeneously onto a unique carrier. The composition contains an effective amount of physiologically active peptide dispersed homogeneously in and adsorbed homogeneously onto a mucosa protecting and/or tissue repairing agent, e.g., gefarnate, aceglutamide aluminum, sucralfate, L-glutamine, sofalcone, teprenone, plaunotol, rebamipide, aldioxa, cetraxate or troxipide.

Abstract: Disclosed is a method of treatment of steroid requiring inflammatory diseases using certain saturated monocyclic and bicyclic terpene compounds. These compounds may be administered in the form of capsules resistant to gastric juice, infusion solutions or intramuscular injection solutions. Because these particular terpene compounds exhibit steroid-like effects but without the harmful side-effects of conventional corticosteroids, the use of corticosteroids is substantially reduced, and in some cases, completely eliminated. Therefore, these terpene compounds are also suitable for long-term therapy and prophylaxis.

Abstract: Substituted amidinonaphthyl ester compounds effective for treatment of thrombosis are represented by the following formula (I) and pharmaceutically acceptable acid addition salts thereof: ##STR1## wherein R.sub.1 represents (4,5-dihydro-1H-imidazol-2-yl)amino group, (4,5-dihydro-1,3-thiazol-2-yl)amino group, amidino group, morpholinomethyl group, nitro group, amino group, dimethylamino group, ##STR2## R.sub.3 represents hydrogen, methoxy group, hydroxyl group, acetylamino group, morpholino group, piperidino group, 1-pyrrolidinyl group or dimethylamino group,m represents 0-4,R.sub.4 represents hydrogen or methyl group,R.sub.2 represents NH.sub.2 CO(CH.sub.2).sub.n --, 2-(carbamoyl)vinyl group or R.sub.5 OOC(CH.sub.2).sub.n --,R.sub.5 represents dimethylcarbamoylmethyl group, hydrogen or lower alkyl group, andn represents 0-2.

Abstract: Disclosed are methods and compositions for reducing coronary artery stenosis, restoring blood flow to infarcted myocardium, improving myocardial perfusion, reducing heart attacks or other adverse cardiovascular events, or treating symptoms of inadequate myocardial function in a mammal involving administering to the mammal (a) a compound that includes eicosapentaeneoic acid or docosahexaeneoic acid and (b) a cholesterol-lowering therapeutic, combined with dietary restrictions (resulting in aggressive loading of marine lipids), whereby a serum LDL concentration of less than 75 mg/dl (and preferably less than 55 mg/dl) is achieved. One particular method involves administering to the mammal a combination that includes (a) a compound that includes an eicosapentaeneoic or docosahexaeneoic acid (for example, a marine lipid) and (b) a cholesterol synthesis or transfer inhibitor, and which may also optionally include aspirin and/or niacin.

Abstract: Natural products such as certain ermophilane sesquiterpenoids and derivatives thereof are described. These compounds are useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. The fungal culture MF6254, Xylaria sp. (ATCC 74397) is also described and disclosed.

Abstract: Methods of inhibiting IL-6 in a cell by administering a therapeutically effective amount of phenylacetate or pharmaceutically acceptable derivatives thereof.

Abstract: Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 and Ar.sup.2 are aryl or R.sup.4 -substituted aryl;Ar.sup.3 is aryl or R.sup.5 -substituted aryl;X, Y and Z are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--;R and R.sup.2 are --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ;R.sup.1 and R.sup.3 are H or lower alkyl;q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is 0 and r is 1, the sum of m, q and n is 1-5;R.sup.4 is selected from lower alkyl, R.sup.5, --CF.sub.3, --CN, --NO.sub.2 and halogen;R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.

Abstract: Compositions and methods of treating anemia, cancer, AIDS, or severe .beta.-chain hemoglobinopathies by administering a therapeutically effective amount of phenylacetate or pharmaceutically acceptable derivatives thereof or derivatives thereof alone or in combination or in conjunction with other therapeutic agents including retinoids, hydroxyurea, and flavonoids. Intravesicle methods of treatment of cancers phenylacetate. Pharmacologically-acceptable salts alone or in combinations and methods of preventing AIDS and malignant conditions, and inducing cell differentiation are also aspects of this invention. A product as a combined preparation of phenylacetate and a retinoid, hydroxyurea, or flavonid (or other mevalonate pathway inhibitor) for simultaneous, separate, or sequential use in treating a neoplastic condition in a subject. Methods of modulating lipid metabolism and/or reducing serum triglycerides in a subject using phenylacetate.

Abstract: Inhibitors of sex steroid activity, for example those having the general structure ##STR1## may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.

Abstract: An apoptosis-controlling agent comprising a carrier and as an effective ingredient 3-?4-hydroxy-3,5-bis(3-methyl-2-butenyl)phenyl!-2-propenoic acid and/or its physiologically acceptable salt(s). The agent promotes the apoptosis of abnormal cells without substantially affecting the apoptosis of normal cells.

Abstract: Pharmaceutical combination compositions including certain cholesterol absorption inhibitors and cholesterol synthesis inhibitors. The compositions are useful for the treatment of hypercholesterolemia and atherosclerosis.

Abstract: This invention provides compounds of the following chemical formula or their pharmaceutically-acceptable salts: ##STR1## wherein R is hydrogen or chloro. Also, the present invention provides a process for the production of the compound of formula I, which comprises cultivating a microorganism having the identifying characteristics of Aspergillus fischeri var. thermomutatis ATCC 18618 or the like, and then isolating the compound of formula I from the fermentation broth. The pyrrolobenzoxazine compounds of formula I of this invention have broad antiparasitic activity, and thus are useful as antiparasitic agents, especially as anthelmintics.

Abstract: A combination of one or more HMG-CoA reductase inhibitors (for example pravastatin, lovastatin, simvastatin, fluvastatin, rivastatin or atorvastatin) with one or more insulin sensitizers (for example troglitazone, pioglitazone, englitazone, BRL-49653, 5-(4-{2-?1-(4-2'-pyridylphenyl)ethylideneaminooxy!-ethoxy}benzyl)thiazolid ine-2,4-dione, 5-{4-(5-methoxy-3-methylimidazo?5,4-b!pyridin-2-yl-methoxy)benzyl}thiazoli dine-2,4-dione or its hydrochloride, 5-?4-(6-methoxy-l-methylbenzimidazol-2-ylmethoxy)benzyl!thiazolidine-2,4-d ione, 5-?4-(l-methylbenzimidazol-2-ylmethoxy)benzyl!-thiazolidine-2,4-dione and 5-?4-(5-hydroxy-1,4,6,7-tetramethylbenzimidazol-2-ylmethoxy) benzyllthiazolidine-2,4-dione) exhibits a synergistic effect and is significantly better at preventing and/or treating arteriosclerosis and/or xanthoma than is either of the components of the combination alone.

Abstract: The invention provides 1,4-naphthoquinone compounds and a method for inhibiting tumor cell growth in a subject by administering such compounds. The compounds are represented by the structures: ##STR1## where R.sub.1 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX where m is 2 or 3 and X is H, methyl, or ethyl; R.sub.2 is halo or NHY, where Y is hydrogen, lower alkyl, halogenated lower alkyl, hydroxylated lower alkyl, lower dialkylaminoalkyl, phenyl, benzyl, or phenethyl; R.sub.3 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX, where m and X are as defined for R.sub.1 above; and R.sub.4 is hydrogen, lower alkyl, lower aminoalkyl, halogenated lower alkyl, phenyl, benzyl, or phenethyl.

Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.

Abstract: Tricyclic retinoids having activity for retinoic acid receptors and/or retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such tricyclic retinoid compounds and methods for their therapeutic use.

Abstract: The invention covers a novel series of .alpha.-mercaptoacrylic acid derivatives that inhibit both calpain I and calpain II with a high affinity and selectivity. The compounds are useful in the treatment of neurodegenerative disorders including cerebrovascular disorders, brain injury, spinal cord, and peripheral nerve injury, cardiac infarction, cataracts, inflammation, restenosis, muscular dystrophy, and platelet aggregation. Pharmaceutical compositions, methods of using processes for preparing and novel intermediates useful in the processes are also disclosed.

Abstract: Novel farnesyl transferase inhibitors of general formula (I) ##STR1## preparation thereof and pharmaceutical compositions containing same. In general formula (I), R.sub.1 is Y--S--A.sub.1 -- (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, or an alkyl or alkoxycarbonyl radical, and A.sub.1 is a C.sub.1-4 alkylene radical optionally .alpha.-substituted in the >C(X.sub.1) (Y.sub.1,) grouping by an amino, alkylamino, alkanoylamino or alkoxycarbonylamino radical wherein the alkyl or alkanoyl portion contains 1-6 carbon atoms; each of X.sub.1 and Y.sub.1 is a hydrogen atom or X.sub.1 and Y.sub.1, taken toether with the carbon atom to which they are attached, form a >C.dbd.O grouping; R'.sub.1 is hydrogen or a C.sub.1-6 alkyl radical; X is an oxygen or sulphur atom; R.sub.2 is a C.sub.1-6 alkyl, alkenyl or alkynyl radical optionally substituted by hydroxy, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl.

Abstract: The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.

Abstract: Novel medicinally-useful compounds are provided herein. These compounds include isomeric cyclic tetramers of formaldehyde and 1-naphthol, and the derivatives or analogues of such cyclic tetramers, and linear oligomers of chromotropic acid, or its derivatives or analogues with naphthalene.

Abstract: Compounds of the formula: ##STR1## wherein R is a hydrogen atom or an OY group; R.sub.1 is a hydrogen atom or in OY' group; R.sub.2 is a hydrogen atom or an OY" group; provided that at lent one among R, R.sub.1 and R.sub.2 is hydrogen but R, R.sub.1, and R.sub.2 are not contemporaneously hydrogen atoms and R.sub.1 and R.sub.2 are not contemporaneously OY' or OY" groups respectively; m is an integer 1 or 2; n is an integer 3 to 8; p is an integer 2, 3, or 4; R.sub.3 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl; R.sub.4 is a phenyl optionally substituted by halogen atom or a C.sub.1 -C.sub.3 alkyl or alkoxy group or a 5- or 6- membered heteroaryl containing one or more heteroatoms selected from oxygen, nitrogen and sulphur, optionally substituted by halogen atoms, hydroxy groups, C.sub.1 -C.sub.3 alkyl or alkoxy groups; X is CH.sub.2, NH, S, SO, SO.sub.2, CO, CF.sub.2, O and, when R.sub.4 is a 5- or 6- membered heteroaryl, X can be also a single bond. Pharmaceutically acceptable salts are described.

Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.

Abstract: New Cyclopentane- or cyclopentene-beta-aminoacid derivatives and their isomers, acid additional salts and metal salt complexes have strong antimicrobial and broad-spectrum antimycotic acitivity. As antimycotics they are especially active against dermatophyte, and biphasic fungi. The new compounds are also low toxicity antibacterial agents, effective against Gram positive bacteria, including antibiotic-resistant strains. The new Cyclopentane- or cyclopentene-beta-aminoacid derivatives are useful in human or veterinary medicine for combating dermatomycosis or systemic mycosis or local or systemic bacterial infections. In addition, the new compounds can also be used as preservatives, especially for water, foods, or organic materials such as polymers, lubricants, paints, fibers, leather, paper or wood.

Abstract: Methods of introducing genetic material into cells of an individual and compositions and kits for practicing the same are disclosed. The methods comprise the steps of contacting cells of an individual with a genetic vaccine facilitator and administering to the cells, a nucleic acid molecule that is free of retroviral particles. The nucleic acid molecule comprises a nucleotide sequence that encodes a protein that comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen or an antigen associated with a hyperproliferative or autoimmune disease, a protein otherwise missing from the individual due to a missing, non-functional or partially functioning gene, or a protein that produce a therapeutic effect on an individual. Methods of prophylactically and therapeutically immunizing an individual against HIV are disclosed. Pharmaceutical compositions and kits for practicing methods of the present invention are disclosed.