Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4, and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of SP and NKA are useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: A dosage form is disclosed for administering 10 ng to 1200 mg tacrine to a patient in need of tacrine therapy.

Abstract: A new treatment schedule for administration of N-?2-(dimethylamino)ethyl!acridine-4-carboxamide and other related carboxamide anticancer drugs in which the drug is administered in a divided-dose schedule comprising two or more administrations at frequent intervals, for example every hour. Schedules to produce cyclic peaks/troughs in plasma levels are mentioned. The compounds can be used for circumventing multidrug resistance in cancers and may, for example, be used in combination with other cytotoxic drugs, especially non-topo II inhibitors. Treatment of melanoma and advanced colon cancer is included.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: Methods and compositions for treating pathogens in material are described, including methods of decontaminating human fluids prior to processing in the clinical laboratory and methods for decontaminating blood products prior to in vivo use. The techniques handle large volumes of human serum without impairing the testing results. Novel compounds for photodecontaminating biological material are also contemplated which are compatible with clinical testing, in that they do not interfere with serum analytes. In particular, quinacrine mustard is used to inactivate pathogens in red cell compositions with retention of red cell function.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The present invention provides a medicinal feed for fish, which comprises a triphenylmethane derivative or a combination of triphenylmethane derivatives alone or in combination with at least one compound selected from the group consisting of thionine, nitrothiazole, nitrofuran, quinoline and acridine derivatives, compounds splitting off aldehydes, transition metal derivatives, metal colloids, hexamethylenetetramine and/or quaternary ammonium salts as active materials.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: Compounds are described of general formula (I) ##STR1## and salts and solvates thereof, including physiologically acceptable salts and solvates thereof, in which:Z represents either Het, ##STR2## Het represents an optionally substituted bicyclic or tricyclic ring selected from acricine isoquinolin-1-yl, isoquinolin-3-yl,The novel compounds of formula (I) can sensitize multi-drug resistant cancer cells to chemotherapeutic agents and may be formulated for use in therapy, particularly to improve or increase the efficacy of an anti-tumour drug.

Abstract: The claims cover a bioactive compound N-methyl-N-.alpha.-D-glucopyranosil-ammonium-2-acridone-9-on-10-yl-acetate designated CYCLOFERONE which was obtained by chemical synthesis and is a heterocyclic compound. Specifically CYCLOFERONE is an acridanone derivative of formula ##STR1## CYCLOFERONE exhibits interferonogenic, anti-vital (including anti-HIV), anti-parasitic, anti-promotive, and radioprotective effects.

Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.

Abstract: Methods of treating asthma are provided which methods comprise administering to a mammal in need of such treatment an effective amount of a compound of Formula I ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.2, R.sup.3, R.sup.4, R.sup.10 and R.sup.11 have any of the meanings given in the specification.

Abstract: A pharmaceutical composition for treatment of cancer in an animal comprising:(A) a therapeutically effective amount of at least one compound selected from the group consisting of compounds represented by the General Formula (I). ##STR1## wherein Z.sub.1 and Z.sub.2, which may be the same or different, each represents an atomic group necessary to form a 5- or 6-membered ring;R.sub.1, R.sub.2 and R.sub.3, which may be the same or different, each represents an alkyl group or an aryl group;L.sub.1 and L.sub.2 each represents a methine group or a substituted methine group;X represents a pharmaceutically acceptable anion;k represents a number necessary for electrical charge balance;n represents 0 or 1; and(B) a pharmaceutically acceptable carrier or diluent.

Abstract: Azaanthracene-triones of the formula: ##STR1## (in which: R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are the same or are different and each is a hydrogen atom or a lower alkyl group;R.sup.3 is a hydrogen atom, a lower alkyl group, a phenyl group or an amino-substituted phenyl group; andX is a --CH--, .dbd.N-- or --NH--, whereby the ring containing the group X is a benzene, pyridine or dihydropyridene ring)have antitumoral activity.

Abstract: These are provided compounds of formula I ##STR1## wherein A represents an oxygen or a sulphur atom, a bond or a group (CH.sub.2).sub.1 NR.sup.9 (where 1 represents zero or 1 and R.sup.9 represents a hydrogen atom or a methyl group); B represents a C.sub.1-4 alkylene chain optionally substituted by a hydroxyl group, except that the hydroxyl group and moiety A can not be attached to the same carbon atom when A represents an oxygen or sulphur atom or a group (CH.sub.2).sub.1 NR.sup.9, or when A represents a bond B may also represent a C.sub.2-4 alkenylene chain; R.sup.3 represents a hydrogen atom or a C.sub.1-4 alkyl group; m represents 1 or 2; R.sup.7 represents a hydrogen atom or R.sup.3 and R.sup.7 together form a group --(CH.sub.2).sub.n -- where n represents 1 or 2. These compounds can sensitize multidrug-resistant cancer cells to chemotherapeutic agents and may be formulated for use in therapy, particularly to improve or increase the efficacy of an antitumor drug.

Abstract: Hypoxia selective cytotoxins having the structural formula ##STR1## wherein D, E, F and G, independently, are carbon or nitrogen, with the proviso that three or more of D, E, F and G are carbon; R.sub.1 and R.sub.2, independently, are selected from the group consisting of methyl, halo, hydro, trifluoromethyl, methoxy, cyano, and methylsulfo; R.sub.3 and R.sub.4, independently, are selected from the group consisting of methyl, ethyl, phenyl, naphthyl, tertiary butyl, halo, halomethylene, hydro, trifluoromethyl, cyano and methylsulfo, or R.sub.3 and R.sub.4 taken together are a substituted or unsubstituted five or six-membered nonaromatic ring system; n is an integer 1 through 5; X is carbon or nitrogen; and Z is a physiologically acceptable anion, are disclosed. The compounds are useful as radiosensitizers or chemosensitizers, especially in the treatment of cancer patients.

Abstract: A method for the detection of an analyte in a fluid sample using liposomes encapsulating acridinium esters (lumisomes). Hydrophilic polysubstituted aryl acridinium esters are useful as chemiluminescent markers and can be encapsulated within liposome vesicles without significant leakage of the esters from the vesicles. The lumisomes can be coupled to molecules with biological activity, such as antigens, antibodies, and nucleic acids, and used in luminescent assays.

Abstract: This invention relates to new pyridyl, quinoline and acridine bis-acyloxymethyl compounds; to compositions comprising these compounds; and to processes for their utility as fungicides, bactericides and as inhibitors of the growth of cancer in warm-blooded animals.

Abstract: Traumatic acid salts, wherein B is a cation selected from:a) a quaternary ammonium,b) a cation of a linear or branched C.sub.1 -C.sub.20 mono-, di- or trialkanolamine,c) a cation of a biologically active primary, secondary or tertiary amine,d) silver or zinc cation,and relative pharmaceutical compositions administrable by topical or parenteral route For the therapeutic treatment of cutaneous pathologies in which it is important to associate an a bacteriostatic, antibiotic, antifungal or an antiviral activity, to the cicatrizant effect, typical of traumatic acid.

Abstract: Novel antagonists of endothelin are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, metabolic, endocrinological, neurological disorders especially cerebral vasospasm, stroke, and head injury, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease, restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, and diabetes.

Abstract: The present invention provides methods of inhibiting bone loss in mammals via the administration to a mammal in need of such treatment an effective amount of a compound from a series of benzoquinolin-3-ones. Such compounds also are sequentially or concurrently coadministered with a bone antiresorptive agent or a bone anabolic agent.

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: 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: Macrolide compounds such as the FR-900506 and its related compounds are provided for the prevention or treatment of eye diseases, particularly, allergic conjunctivitis. Composition containing such compounds is also disclosed.

Abstract: The present invention provides an anticancer compound having the structure: ##STR1## wherein R is --H, --CH.sub.3, or --C.sub.2 H.sub.5 ; R1 and R2 are independently --H, --OH, --NH.sub.2, --OCH.sub.3, --C(CH.sub.3).sub.3, or a halogen atom; n is 2 to 6; X and X' are independently --N or --NO.sub.2 ; Y and Y' are independently --N, --CH, or --H; and the double-slash represents a double bond or no bond; such that when X or X' is --N, Y or Y' is --CH or --N, and the double-slash is a double bond, and when X or X' is --NO.sub.2, Y or Y' is --H, and the double-slash is no bond. The present invention also provides a pharmaceutical composition comprising the compound above and a pharmaceutically acceptable carrier.

Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.

Abstract: A therapeutic composition derived from a pre-activated photoactive compound and a conveyor for destroying tumor or other pathogenic biological contaminants infecting animal body tissues. The conveyor can either be a matrix support or an antibody. The activation of the photoactive compound to produce the pre-activated photoactive compound is carried out by the use of an activating agent. The pre-activated photoactive compound retains its therapeutic activity subsequent to activation. A method for preparing such a therapeutic composition is disclosed. Methods for treating animal body tissue, either outside the body or inside the body, infected with tumors or other pathogenic biological contaminants are disclosed.

Abstract: Compounds of general formula I, ##STR1## and pharmaceutically acceptable salts thereof, in which R.sup.1 has any of the meanings given in the specification, pharmaceutical compositions comprising them and their use in the treatment of urinary incontinence.

Abstract: Compositions and methods for prevention of adhesion formation, whereby an effective amount of quinacrine as active agent is administered for a period of time sufficient to permit tissue repair. The active agent is preferably administered in conjunction with a delivery vehicle (e.g., microcapsules, microspheres, lipid-based systems, viscous instillates and absorbable mechanical barriers) useful for maintaining local concentrations of the compound at an effective level.

Abstract: Described is a method of treating Alzheimer's disease in a patient comprising administering to said patient an effective amount of tacrine in combination with a P450 1A2 oxidase inhibitor. Preferably, the inhibitor is a heterocyclic guanidine.

Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.

Abstract: Compounds of formula I ##STR1## wherein R.sup.2, R.sup.3, R.sup.4, R.sup.10 and R.sup.11 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: A plant fungicide method comprises applying to the locus of a plant pathogen a fungicidally effective amount of a compound of formula (I) ##STR1## or a salt or a complex thereof, wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently H, halo, NO.sub.2, (C.sub.1 -C.sub.4) alkyl, or halo(C.sub.1 -C.sub.4) alkyl;R.sup.3', R.sup.4', R.sup.5', R.sup.3", R.sup.4", and R.sup.5" are independently H, halo, OH, or CH.sub.3, provided that at least one is OH;R.sup.6 ' and R.sup.6 " are independently H or OH.

Abstract: A method for treating a central nervous system or peripheral nervous system cholinergic deficit state in a mammalian organism in need of such treatment, said method comprising administering to said mammal an amount of thalidomide effective in the treatment of a cholinergic deficit state and for a time sufficient to achieve a suitable blood level to treat said cholinergic deficit state.

Abstract: A method for inhibiting neuronal cell death in a mammal resulting from a disorder of the central or peripheral nervous system including administering to the mammal a neuronal cell death inhibitng amount of a preparation including any of mepacrine, chloroquine, or hydroxychloroquine, the preparation being essentially free of colchicine.

Abstract: Described is a method of inhibiting the enzymatic metabolism of nitrogen substituted acridines of Formula 1 comprising co-administering with the acridine an effective oxidase inhibiting amount of a P450 1A2 inhibitor. The oxidase is one whose activity is induced by beta-naphthaflavone, 3-methylcholanthrene, arochlor, 2,3,7,8-tetrachlorodibenzo-p-dioxin and isosafrole. The oxidase inhibitor may be a naphthyridine, a xanthine, a phenoxy amino alkane, a carbamoyl imidazole, a heterocyclic guanidine, or a quinoline.

Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; X is alkyl of 3-18 carbon atoms, cycloalkyl of 3-7 carbon atoms or cycloalkylloweralkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; R.sub.1 is hydrogen, loweralkyl, loweralkylcarbonyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.

Abstract: Novel 9-aminotetrahydroacridines and related compounds, intermediates and processes for the preparation thereof, and a method of relieving memory dysfunction are disclosed.

Abstract: A method is provided for inactivating viral and/or bacterial and/or parasitic contamination in cellular blood matter or blood plasma protein fractions, using radiation sensitizing chemical compounds and irradiation with, for example, UV radiation.

Abstract: Compounds of general formula I, ##STR1## and pharmaceutically acceptable salts thereof, in which R.sup.1 has any of the meanings given in the specification, pharmaceutical compositions comprising them and their use in the treatment of urinary incontinence.

Abstract: The subject invention discloses methods of inhibiting growth of tumor cells which comprise contacting the cells with a growth inhibiting amount of a compound having one of following structures: ##STR1## wherein R.sup.1 is a hydroxyl or acetyl group; R.sup.2 is hydrogen, --CH.sub.2 --CH.dbd.C(CH.sub.3).sub.2 or a method group; R.sup.3 is a hydroxyl, methoxy or acetyl group; R.sup.4 is hydrogen, --CH.sub.2 --CH.dbd.C(CH.sub.3).sub.2 or a methoxy group; R.sup.5 is a hydroxyl, methoxy or acetyl group; is hydrogen or a hydroxyl, methoxy or acetyl group; and R.sup.10 is a methyl group, ##STR2## wherein R.sup.5 is hydrogen or --CH.sub.2 --CH.dbd.C(CH.sub.3).sub.2 ; R.sup.6 is a hydroxyl group; R.sup.10 is hydrogen or a hydroxyl group; R.sup.11 is a hydroxyl or methoxy group; and R.sup.12 is hydrogen or a methyl group.

Abstract: Ionizable congeners of aromatic and aliphatic alcohols provide potent cytoprotective properties in vivo and in vitro. Alpha-tocopherol succinate, cholesteryl succinate, cholesteryl sulfate, dihydrocholesterol succinate, dihydrocholesterol sulfate, and ergosterol analogs are particularly good cytoprotective agents. In addition, the tris salts of these compounds have superior cytoprotective properties.

Abstract: The use of a pharmaceutically acceptable cholinesterase inhibitor or a prodrug therefor for the treatment of fatigue syndromes, including chronic fatigue syndrome, post-infectious fatigue syndromes, fatigue syndromes associated with human immunodeficiency virus (HIV) infection or with preeclampsia. The acetyl cholinesterase is preferably one that acts substantially selectively at nicotinic receptor sites, and which has selectivity for acetyl cholinesterase as opposed to butyryl cholinesterase. Compounds of the invention include galanthamine and galanthamine derivatives.

Abstract: Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT.sub.1 and AT.sub.2 activity useful in the treatment of hypertension and related disorders and ocular hypertension. ##STR1## where X is --O-- or --N(R.sup.7)--.

Abstract: Hypoxia selective cytotoxins of the general formula ##STR1## wherein n is from 1 to 5, and NO.sub.2 is in at least one of the 2, 4 or 5-positions of the imidazole. Such compounds have utility as radiosensitizers and chemosensitizers.

Abstract: A method of inhibiting the abnormal postnatal axial growth of the eye of a maturing animal during conditions ordinarily leading to said abnormal growth, which comprises (1) determining the neurochemical present in the retina of said eye, eg., dopamine, the concentrations of which is reduced during said conditions, and (2) administering to said eye during post natal maturation effective amounts of said neurochemical, its agonist or its antagonist.

Abstract: An euthanasia solution based upon gamma-hydroxybutramide and a cardiotoxic amount of a compound selected from chloroquine and quinacrine is described. The composition provides effective euthanasia without unwanted side effects.

Abstract: The invention provides the novel compound, 9-(3-cyanophenyl)-3,4,6,7,9,10-hexahydro-1,8-(2H,5H)-acridinedione and pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions containing the compound, and the use of the compound in the treatment of urinary incontinence.

Abstract: Quinoline derivatives of the formula, ##STR1## wherein >A represents a group >N--(CH.sub.2).sub.n --, >C.dbd., >C.dbd.CH(CH.sub.2).sub.n --, or >CH(CH.sub.2).sub.n --, wherein n is an integer of 0-7; Y represents a group >C.dbd.O or >CHOH, R.sup.1 is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group, R.sup.2 is a hydrogen atom, a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, a phenyl group which may have a substituent, a phenoxy group, an alkanoyloxy group, or an amino group which may have a substituent, R.sup.3 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxy group, and m is an integer of 1-3. The compounds and their salts exhibit a superior anti-acetylcholinesterase activity with no side effects and are effective for the prevention or cure of senile dementia or memory disturbance.

Abstract: A novel compound for controlling (treatment and prevention) of ocular inflammation or systemic inflammatory disease is disclosed. The compound, OB-186, is effective at both the early and late phases of inflammation. The compound is useful for the treatment or prevention of inflammation in both the anterior and posterior portions of the eye and systemic inflammatory diseases, such as rheumatoid arthritis, inflammatory bowel disease, glyomerulonephritis, allergic inflammation and allergic encephalomyelitis.