Abstract: The present invention relates to substituted camptothecin derivatives of formula (I) wherein the symbol - - - - represents a single or double bond; R.sub.1, R.sub.2 and R.sub.3 are as defined under (a) or (b) below: (a) R.sub.1 and R.sub.2 are, each independently, hydrogen; C.sub.1 -C.sub.4 alkyl; C.sub.3 -C.sub.7 cycloalkyl; phenyl C.sub.1 -C.sub.6 alkyl; an optionally substituted phenyl ring; --NR.sub.5 R.sub.6 wherein one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl and the other is hydrogen, C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted benzoyl, phenyl C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted phenoxycarbonyl or phenyl C.sub.1 -C.sub.6 alkoxycarbonyl, or R.sub.5 and R.sub.6, combined together with the nitrogen atom to which they are linked, form a 4-7 membered saturated, optionally substituted, heteromonocyclic ring residue; COOR.sub.8 wherein R.

Abstract: Substituted pydrido?1,2-a!pyrazines of general formula I wherein Ar and Ar.sup.1 represent various carbocyclic and heterocyclic aromatic rings; A represents O, S, SO, SO.sub.2, C.dbd.O, CHOH, or --(CR.sup.3 R.sup.4) and n is 0-2 as well as precursors thereto are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system.

Abstract: A novel compound which is a .delta.-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof. The present invention also provides an immunosuppressive agent, antiallergic agent, anti-inflammatory agent and brain cell-protecting agent comprising the derivative or the salt as an effective ingredient.

Abstract: Non-naturally occuring dynemicin analogs are provided, which are useful as DNA cleaving agents, cytotoxic agents, and/or anti-tumor compounds. Methods of making dynemicin analogs are also provided.

Abstract: The present invention relates to indole derivatives represented by the following compound 1 and the pharmacologically acceptable acid addition salt thereof. ##STR1## The compounds of the present invention were found to exhibit strong antitussive and analgesic actions as a result of pharmacological evaluation, and can be used in the pharmaceutical field as effective antitussives and analgesics.

Abstract: A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumour activity and a high degree of safety, and can be applied as an antitumour medicine for curing tumors of various kinds.

Abstract: A carpet cleaning composition comprising: (a) a powder-form solid adsorbent; (b) rollable particles of porous material, each particle having a length greater than 1 mm, and a diameter equal to at least 10% of the length of the particle; and (c) water.

Abstract: A method is provided for treating an individual afflicted with an impulse-control disorder by administering thereto an amount of one or more opioid receptor antagonists.

Abstract: A rapid-acting remedy for asthma having a bronchodilating action contains at least one pyrido?2,3-d!pyrimidine derivative represented by the general formula (A) or pharmaceutically acceptable salts or metal complexes thereof as an effective component: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each of R.sup.1 and R.sup.2 is hydrogen, alkyl or benzyl; R.sup.3 is hydrogen, hydroxyl, dialkylaminomethyleneamino or --NH--X; X is hydrogen, alkyl, alkenyl, hydroxyl, amino, hydroxyalkyl, benzyl or acyl; R.sup.4 is hydrogen, alkyl, halogen, nitro, amino, hydroxyl, benzyloxy, cyano, carboxyl, alkoxycarbonyl, alkoxysulfonyl, aminosulfonyl, dialkylaminosulfonyl or sulfo; and R.sup.5 is hydrogen, alkyl or amino. The rapid-acting remedy for bronchial asthma is capable of relieving the symptom of laboring breath at the onset of asthma due to its excellent bronchodilating action.

Abstract: The present invention addresses substituted pyridyl pyrroles, as well as compositions containing such compounds and methods of treatment. The compounds in the present invention are glucagon antagonists and inhibitors of the biosynthesis and action of TNF-.alpha. and IL1. The compounds block the action of glucagon at its receptors and thereby decrease the levels of plasma glucose. The instant pyrroles are also inhibitors of TNF-.alpha. and IL1 and may be used as antidiabetic agents as well as other cytokine mediated diseases. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production of one or more cytokines occurs. Interleukin-1 (IL-1) and Tumor Necrosis Factor (TNF) are cytokines produced by a variety of cells, which are involved in immunoregulation and other physiological conditions, such as inflammation.

Abstract: This invention relates to an aqueous liquid composition for external use which contains a tricyclo compound of the chemical formula (I) presented here-under or a pharmaceutically acceptable salt thereof. More particularly, the invention relates to an aqueous liquid composition for external use characterized in that it contains said tricyclo compound and a water-soluble solubilizer. The composition of the invention is used in medical treatment.

Abstract: A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumor activity and a high degree of safety, and can be applied as an antitumor medicine for curing tumors of various kinds.

Abstract: This invention provides novel aconitine compounds of the formula (I) or salt thereof ##STR1## wherein, R.sub.1 is a hydrogen atom or hydroxyl group; R.sub.2 is an acetyloxy group; R.sub.3 is an alkyl having 1-4 carbon atoms; and R.sub.4 is a hydrogen atom, a hydroxyl group, or an acetyloxy group; and antipyretic/analgesic/anti-inflammatory agents containing the compound as an active ingredient which are highly safe and exhibit a powerful analgsic effect and antipyretic/anti-inflammatory activities. The compound is usable alone in painful, pyretic and inflammatory illnesses but its concomitant use with morphine reinforces the analgesic effect of morphine and allows alleviation of morphine side effects through reduction in morphine dosage.

Abstract: Non-naturally occuring dynemicin analogs are provided, which are useful as DNA cleaving agents, cytotoxic agents, and/or anti-tumor compounds. Methods of making dynemicin analogs are also provided.

Abstract: The present invention provides water soluble, stable, highly pharmacologically active camptothecin drugs by solubilizing the camptothecin drugs in liposomes composed of lipids or in micelles composed of surfactants. The invention overcomes both the insolubility problems and instability problems of the drugs administered in their free form. The pH of the internal environment of the liposomes or micelles may be reduced pH which prevents hydrolysis of those camptothecin drugs which have lower affinity for the liposome or micelle membrane. Typically in the liposomes, the lactone ring of drug intercalates in between the lipid acyl chains, in a protected environment well removed from the aqueous interface. In this manner the lactone ring of the drug is stabilized and the biologically active form of camptothecin drugs are conserved.

Abstract: Described herein is a pyrrolocarbazole derivative and a pharmaceutically acceptable salt thereof having the following formula (I): ##STR1## wherein R.sup.1 is lower alkyl or aralkyl; R.sup.2 is hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, or substituted or unsubstituted aralkyl; R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 may be the same or different, and are hydrogen, halogen, nitro, substituted or unsubstituted lower alkanoyl, NR.sup.9 R.sup.10, or OR.sup.11 ; R.sup.8 is hydrogen or is combined with R.sup.3 to form --CONR.sup.12 --; and when R.sup.1 is benzyl; R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are not simultaneously hydrogen. A compound of the present invention stimulates platelet production and is useful for treatment of thrombocytopenia.

Abstract: The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity.This amino acid derivative is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or an acyl group; R.sup.2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent;m and n represent each independently an integer of 0, 1 or 2 andJ represents a cyclic group having an angiotensin I-converting enzyme inhibition activity.

Abstract: An acetamide derivative having the general formula (I): ##STR1## or a pharmacologically acceptable salt thereof; a synthetic intermediate of the above-mentioned acetamide derivative; a treating agent for peptic ulcer and for gastritis which comprises the above-mentioned compound having the general formula (I) as an effective ingredient, and a process for treating peptic ulcer and gastritis using the above-mentioned compound having the general formula (I), are disclosed.

Abstract: The present invention provides water soluble camptothecin analogs of Formula I: ##STR1## which are particularly useful as antineoplastic agents; pharmaceutical compositions thereof; and a method of treating cancer in an animal in need thereof, including human beings, comprising inhibition of the growth of tumor cells in said animal by administration of an effective amount of a compound of Formula I.

Abstract: The present invention provides a water soluble camptothecin analog of Formula I: ##STR1## which is particularly useful as an antineoplastic agent; pharmaceutical compositions thereof; and a method of treating cancer in an animal in need thereof, including human beings, comprising inhibition of the growth of tumor cells in said animal by administration of an effective amount of a compound of Formula I.

Abstract: A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound by the condensation-ring closing reaction. It is abundantly water-soluble, and has an excellent antitumor activity and a high degree of safety, and can be applied as an antitumor medicine for curing tumors of various kinds.

Abstract: Methods of treatment for inflammatory and autoimmune dermatoses which comprises topical and/or systemic administration of a therapeutically-effective amount of thalidomide alone or in combination with other dermatological agents.

Abstract: There is provided a composition for inhibiting the production or secretion of tumor necrosis factor effective for the treatment of cachexia, septic shock, multiple organ failure, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis, osteoarthritis, Behcet disease, systemic lupus erythematosus (SLE), graft versus host disease (GvHD), malaria, acquired immune deficiency syndrome (AIDS), meningitis, hepatitis and Type II diabetes mellitus. The composition comprises a pharmaceutically effective amount of a compound of formula (1).

Abstract: Non-toxic camptothecin prodrugs are prepared by esterifying the 20-position hydroxyl group of camptothecin derivatives.

Abstract: In accordance with the present invention, a method is provided for treating reperfusion injury, ischemia and runaway inflammatory conditions with thalidomide alone or in combination with other drugs selected from the group consisting of nitrates, beta-adrenoceptor blocking agents, anti-platelet/thrombolytic drugs, drugs acting as the arachindonic acid cascade and calcium antagonists. Pharmaceutical compositions comprising thalidomide alone or in combination with other drugs are also provided.

Abstract: The instant invention is directed to the use of a pharmaceutical composition containing an effective amount of adenosine or an adenosine analog or derivative as an agent useful in the treatment of hormone-independent cancers, such as prostate cancer. The invention is also directed to diagnostic uses of these compounds to determine effective treatment regimes for specific tumors, a process for screening for new, therapeutically useful analogs of these compounds, and the use of these compounds in facilitating the extraction of intracellular components.

Abstract: This invention relates to pteridine and 8-deazapteridine compounds and compositions containing the same which are useful for controlling insects in agricultural crops. These pteridines may be represented by the following structure: ##STR1## wherein R and R.sup.1 are independently selected from amino, lower alkylamino, di(lower alkyl)amino (e.g., --N(CH.sub.3).sub.2), or di(lower alkyl)aminomethyleneamino (e.g., --N.dbd.CHN(CH.sub.3).sub.2);R.sup.2 is hydrogen, amino, lower alkyl (e.g., --CH.sub.3, --CH(CH.sub.3).sub.2), di(lower alkyl)aminomethyleneamino, hydroxy, lower alkoxy, phenyl or substituted phenyl, haloalkylphenylalkyl (e.g., 3-trifluoromethylphenylmethyl);Q is N or CH;R.sup.3 is -(n).sub.m -R.sup.4, where m is 0 or 1; wherein, when m is 1,n is a bridging atom or moiety selected from oxygen, sulfur, sulfinyl, sulfonyl, lower alkylene (e.g., --CH.sub.2 --, or --CH.sub.2 CH.sub.2 --), lower alkenylene (e.g., --CH.dbd.CH--), lower alkynylene (e.g., --C.tbd.C--), lower haloalkenylene (e.g., --C(Cl).dbd.

Abstract: A therapeutic method is provided to elevate a depressed mammalian autologous mixed lymphocyte response and to alleviate the diseases associated therewith by the administration of an effective amount of certain selective delta opioid receptor antagonists to a mammal such as a human patient in need of such treatment.

Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.

Abstract: The present invention provides novel tetrahydro-beta-carboline compounds having useful central nervous system activity. Further, there is provided tetrahydro-beta-carboline related compounds which are useful intermediates and have beneficial central nervous system activity. The invention provides formulations and methods for using the novel tetrahydro-beta-carboline and related compounds. Such compounds are particularly useful for the modulation of a 5-HT.sub.2B receptor.

Abstract: An improvement in the process of coacervation of chlorpheniramine maleate is provided whereby a predetermined amount of chlorpheniramine maleate charged to the process is maintained in the microcapsules by pre-saturating the coacervation medium with chlorpheniramine maleate.

Abstract: A compound selected from those of general formula (I): ##STR1## wherein A represents a bivalent radical ##STR2## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and Z are as defined in the description,the isomers and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of depression and anxiety.

Abstract: The invention features novel derivatives of K-252a, as well as novel bis-N-substituted derivatives of staurosporine. The invention also features a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a.

Abstract: Camptothecin compounds are effective inhibitors of plasmodia growth and are useful in treating plasmodia infections in livestock, other domestic animals and humans.

Abstract: The present invention relates to new camptothecin derivatives of the formula (I) ##STR1## wherein B is a group B' or B" ##STR2## wherein each of (x) and (y) is a single or double bond. The present invention also provides processes for their preparation as well as pharmaceutical compositions containing the same.

Abstract: A compound selected from those of general formula (I): ##STR1## wherein A represents a bivalent radical selected from ##STR2## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and Z are as defined in the description,the isomers and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of depression and anxiety.

Abstract: A method is provided for effectively terminating methadone maintenance therapy and the addiction to other legally-available opiates by selectively extinguishing the opiate-taking responses. Selective extinction is produced having sessions in which detoxified addicts make opiate-taking responses while an opiate antagonist blocks the positive reinforcement, interspersed by periods when the antagonist is absent and all responses except opiate-taking can be emitted. A similar method but with instructions not to take the opiate can subsequently be used to protect against resumption of illegal opiate use, or separately with patients addicted to illegal opiates producing reinforcement through the opioidergic system.

Abstract: A compound isolated from Ervatamia microphylla has been found to be effective in inducing a change in cell morphology and growth habits of cultured transformant cell lines, and in reducing the tumor size in a living mammal. The compound is capable of inhibiting the function of oncogenes such as ras and src by inhibiting the function of the oncogene products. The compound is found to be represented by formula (I): ##STR1## Use of the compound as an oncogene function inhibitor, in a treatment of cancer, and in inducing changes in cell morphology and growth habits in transformant cell line are contemplated.

Abstract: Substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment of neurodegenerative disorders or neurotoxic injuries utilizing them, wherein the substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts have the formula: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X and p are as defined in the specification.

Abstract: A method for treating pain and brain perfusion abnormalities using mixed opiate agonist/antagonists is provided.

Abstract: The invention relates to a pharmaceutical composition and a method for treating drug addicts' withdrawal syndrome and detoxifying addicts. The pharmaceutical composition comprises aconitane derivative of formulas I, II, their inorganic acid salts or mixtures thereof, and tetrahydroprotoberberine derivatives of formula II. The method of treatment comprises administering the pharmaceutical composition to drug addicts. The pharmaceutical composition of the present invention produces no drug dependence, excellent effects, fast action and low side-effects.

Abstract: A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

Abstract: An anti-AIDS virus composition comprising a therapeutically effective amount of cepharanthine or a pharmaceutically acceptable salt thereof and a method for treating AIDS which comprises administering a therapeutically effective amount of cepharanthine or a pharmaceutically acceptable salt thereof are disclosed.

Abstract: A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.

Abstract: Administration of protein kinase C inhibitors protect neuronal cells from death from cerebral ischemia. Model for screening compounds for potential for protecting neuronal cells from death from cerebral ischemia comprises adding the compounds to medium containing neuronal cells before, at the same time as, and/or after nitric oxide administration.

Abstract: Novel aconitine compounds of the formula ##STR1## wherein the symbols are as defined in the description, as well as analgesic/anti-inflammatory agent containing them or salts thereof as active ingredient.

Abstract: Camptothecin compounds are effective inhibitors of hemoflagellate growth and are useful in treating leishmaniasis and trypanosomiasis in livestock, other domestic animals and humans.

Abstract: Novel aconitine compounds of the formula ##STR1## wherein the symbols are as defined in the description, as well as analgesic/anti-inflammatory agent containing them or salts thereof as active ingredient.

Abstract: Compounds of the formulas: ##STR1## or pharmaceutically acceptable salts thereof. These compounds are obtainable by cultivation of a pure culture of Actinoplanes sp. SCC2314, ATCC 55600. These compounds are useful as antifungal agents.

Abstract: Novel aconitine compounds of the formula ##STR1## wherein the symbols are as defined in the description, as well as analgesic/anti-inflammatory agent containing them or salts thereof as active ingredient.