Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: A class of predominantly hydrophobic non-azo N-substituted 1,8-naphthalimide compounds, each bearing, at its 3-position, a nucleofuge and, at its 4-position, a heteroatomic electron-releasing group. The heteroatomic electron-releasing group is being characterized as having a heteroatom directly linked to the 4-position of the ring, and having at least one hydrogen directly attached to the heteroatom. Upon activation by an activating agent in an environment independent of the presence or absence of oxygen, these compounds generate activated species. The activated species initiate chemical changes in lipid bilayer membranes of viruses and other target cells. These changes can eradicate viruses and other target cells. The activated species can also cause structural changes in lipid and any associated proteins and polypeptides at a level beneath the surface of the membrane, leading to polymerization and crosslinking.

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: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: This invention relates to 3-Pyrimidinyl Bisnaphthalimides as Anticancer Agents and pharmaceutically acceptable salts thereof, of the formula: ##STR1## and processes for the preparation of such compounds, pharmaceutical composition containing such compounds, and methods of using such compounds to treat cancer, particularly solid tumor carcinomas, in mammals.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Disclosed herein are compounds pharmaceutical compositions containing same of the formula1. A compound of the Formula ##STR1## wherein X, X', X" and X'", A, B, D, R, and R' are as identified in the specification and their preparation. Pharmaceutical compositions containing same can be used in the treatment of cancer.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: The present invention provides novel bis-naphthalimides characterized by having a linker containing a heteroatom, their preparation, pharmaceutical compositions thereof, and various methods of using the bis-naphthalimides. Particularly preferred bis-naphthalimides have a linker of about 8-16 atoms where the heteroatom is oxygen, sulfur, sulfur oxide or sulfur dioxide. The bis-naphthalimides provided herein have exceptional DNA binding properties and demonstrate cytotoxicity in both in vitro and in vivo tumor models, in particular, against melanoma.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: The present invention provides novel bis-naphthalimides characterized by having a linker containing a heteroatom, their preparation, pharmaceutical compositions thereof, and various methods of using the bis-naphthalimides. Particularly preferred bis-naphthalimides have a linker of about 8-16 atoms where the heteroatom is oxygen, sulfur, sulfur oxide or sulfur dioxide. The bis-naphthalimides provided herein have exceptional DNA binding properties and demonstrate cytotoxicity in both in vitro and in vivo tumor models, in particular, against melanoma. Also provided a novel mono-naphthalimides linked to a DNA alkylating agent. These agents are shown to have conformational effects on double stranded DNA and to form covalent adducts after an extended incubation period.

Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof; pharmaceutical compositions containing the compounds and a method for treating serotonin mediated condition with the compositionswhich act as 5-HT.sub.4 agonists or antagonists and/or 5-HT.sub.3 antagonists.

Abstract: The invention relates to substituted 1-naphthyl-3-pyrazolecarboxamides of formula I: ##STR1## Application: These compounds are useful for the treatment of neuropsychiatric disorders, especially those associated with a dysfunction of the dopaminergic systems.

Abstract: This invention relates to 2-(1'-azabicyclo[2.2.2]oct-3'S-yl)-6-hydroxy-2,4,5,6-tetrahydro-1H-benz[de ]isoquinolin-1-one and 2-(1'-azabicyclo[2.2.2]oct-3'S-yl)-6-hydroxy-2,3,3a,4,5,6-hexahydro-1H-ben z[de]isoquinolin-1-one and their individual stereoisomers and uses and the processes for their making.

Abstract: Prostate cancer particularly hormone-unresponsive metastatic prostate cancer, is treated by cyclophosphamide or other normally substantially inactive agent. Potentiation of the anti-cancer activity and amelioration of cyclophosphamide-associated toxicity is achieved by an initial intravenous infusion of DPPE over an approximately one hour period prior to cyclophosphamide treatment.

Abstract: The monohydrochloride and the monomethanesulfonate of amonafide are described. The salts have good pharmaceutical properties besides their antitumor action.

Abstract: A class of predominantly hydrophobic non-azo N-substituted 1,8-naphthalimide compounds, each bearing, at its 3-position, a nucleofuge and, at its 4-position, a heteroatomic electron-releasing group. The heteroatomic electron-releasing group is being characterized as having a heteroatom directly linked to the 4-position of the ring, and having at least one hydrogen directly attached to the heteroatom. Upon activation by an activating agent in an environment independent of the presence or absence of oxygen, these compounds generate activated species. The activated species initiate chemical changes in lipid bilayer membranes of viruses and other target cells. These changes can eradicate viruses and other target cells. The activated species can also cause structural changes in lipid and any associated proteins and polypeptides at a level beneath the surface of the membrane, leading to polymerization and crosslinking.

Abstract: This invention relates to unsymmetrical mono-3-nitro bis-naphthalimides of formula ##STR1## including (R,R)-2-{2-[2-((2-(1,3-dioxo-1H-benz[de]isoquinolin-2-(3H)-yl)-propylamino ))ethylamino]-1-methylethyl}-5-nitro-1H-benz[de]isoquinolin-1,3-(2H)-dione, processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer, particularly solid tumor carcinomas, in mammals.

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

Abstract: An euthanasia solution based upon gamma-hydroxybutramide, a cardiotoxic amount of a compound selected from a chloroquine and quinacrine compound and lidocaine as a base or as a water soluble salt is described. The composition provides effective euthanasia without unwanted side effects, particularly in dogs, cats and horses. In addition, it does not contain substances controlled by the Federal Drug Control Administration.

Abstract: Quinolone carboxylic acids 7-substituted by azabicyclo groups have antibacterial activity.

Abstract: An edible composition comprising an amino acid capable of accelerating a release of glucagon, known as an adipokinetic hormone, a xanthine derivative capable of degrading body fats, and a thiamine compound essential to caloric metabolism, is provided. The composition is advantageously useful in the enhanced mobilization of depot body fats through physical activities such as sports, work, aerobic movements, jogging, and the like.

Abstract: This invention relates to bis-naphthalimides, including 2,2'-[1,2-ethanediylbis[imino(1-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione] and 2,2'-[1,2-ethanediylbis[imino(2-methyl-2,1-ethanediyl)]]-bis[5-nitro-1H-be nz[de]isoquinoline-1,3(2H)-dione], processes for their preparation, pharmaceutical compositions containing them, and methods of using them to treat cancer in mammals.

Abstract: There are provided novel bis-naphthalimide compounds useful as antitumor agents, pharmaceutical compositions containing them and processes for preparing such compounds.

Abstract: Compounds of Formula I: ##STR1## in which Z is CH.sub.2 or C.dbd.O;X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino; and R.sup.1 is a group selected from Formulae (a), (b), (c) (d) and (e): ##STR2## in which p is 0 or 1;n is 1, 2 or 3;R.sup.2 is hydrogen, lower alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.12 alkyl, or a group R.sup.6 -C.sub.1-2 alkyl in which R.sup.6 is thienyl, pyrrolyl or furyl optionally substituted by one or two substituents selected from lower alkyl, lower alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C.sub.1-4 alkyl optionally further substituted by hydroxy, C.sub.1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy;each R.sup.

Abstract: The present invention is directed to 5-HT.sub.3 receptor antagonist compounds of formula I: ##STR1## in which the dashed line denotes an optional double bond;n is 1, 2 or 3;p is 0, 1, 2 or 3;q is 0, 1 or 2;each R.sup.1 is independently selected from halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, amino carbonyl, (lower alkyl)amino, di(lower alkyl)amino, and (lower alkanoyl)amino;each R.sup.2 is lower alkyl; andR.sup.3 is a group selected from Formulae (a), (b), (c) and (d): ##STR2## in which u is 0 or 1;z is 1, 2 or 3; andR.sup.4 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl, or a group (CH.sub.2).sub.t R.sup.5 where t is 1 or 2 and R.sup.5 is thienyl, pyrrolyl, or furyl, each optionally further substituted by one or two substituents selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C.sub.

Abstract: N-(2-dimethylaminoethyl)-3-amino-1,8-naphthalimide (amonafide) is an effective agent for the treatment of leukemias and solid tumors.

Abstract: A method to treat or prevent retroviral infection by administering a novel conjugate is described. Lucifer Yellow and its analogs are conjugated to compounds having carbonyl functional groups for reaction with the semicarbazide moiety of Lucifer Yellow to obtain the semicarbazone conjugate.

Abstract: The invention relates to a compound of the formula: ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen or lower alkyl,R.sup.3 is aryl or unsaturated, 5- or 6-membered heterocyclic group containing a sulfur atom, each of which may be substituted by one or more substituent(s) selected from the group consisting of halogen, hydroxy, lower alkyl, aryloxy, trihalo(lower)alkyl, lower alkoxy and mono- or di(lower)alkylamino,R.sup.4 is hydrogen, halogen or lower alkyl,A is methylene, methine, oxa, thia, sulfinyl or sulfonyl,Y is vinylene or ethylene.Z is a group of the formula: ##STR2## wherein R.sup.5 is carboxy or protected carboxy, andR.sup.6 is hydrogen or hydroxy-protective group, andthe line is of a single or double bond, or a pharmaceutically acceptable salt thereof, useful as a 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor.

Abstract: A series of novel 5-substituted imidazolidinedione derivatives and their base salts with pharmacologically acceptable cations are disclosed. These particular compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. 5-Naphthalimido-imidazolidine-2,4-dione and 5-[3-(4'-bromo-2'-fluorobenzyl)-3,4-dihydro-4-oxophthalazin-1-yl]-imidazol idine-2,4-dione represent typical and preferred member compounds. Methods for preparing all these compounds from known starting materials are provided.

Abstract: The invention relates to compounds of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene chain and R.sup.3 is a hydrogen atom; orR.sup.1 and R.sup.3 together form a C.sub.2-4 alkylene chain and R.sup.2 is a hydrogen atom;A-B represents the group R.sup.4 R.sup.5 C--CH.sub.2 or R.sup.4 C.dbd.CH;R.sup.4 and R.sup.5, which may be the same or different, each represent a hydrogen atom or a C.sub.1-6 alkyl group; andIm represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.6, R.sup.7 and R.sup.8 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;and physiologically acceptable salts and solvates thereof.The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.

Abstract: Use of a mono or dicyclic carboxylic or heterocyclic carboxylic acid ester or amide of an alcohol or amine nitrogen as a ring atom in free base form or in acid addition or quaternary ammonium salt form as a 5-HT.sub.3 antagonist in the manufacture of a medicament suitable for the treatment of serotonin induced gastrointestinal disturbances.

Abstract: This invention concerns novel 2-heteroarylalkyl-1H-benz[de]isoquinoline-1,3(2H)-diones which are useful as inhibitors of thromboxane synthetase and/or as hypotensive agents in the treatment of hypertension and myocardial ischemia.

Abstract: Chemical compounds are provided that are novel 3,6-disubstituted-1,8-naphthalimides (I), as well as methods for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. Compounds of the invention have pharmacological properties and are useful antimicrobial agents and antitumor agents.

Abstract: 1,3-dioxo-1H-benz(de)isoquinoline-2(3H) butyric acid having the following ructural formula ##STR1## A pharmaceutical composition for treating diabetes mellitus complications comprises an active agent and a pharmaceutical base material, wherein the active agent is a compound selected from the group consisting of 1,3-dioxo-1H-benz(de)isoquinoline-2(3H) butyric acid, and the sodium and potassium salts thereof.

Abstract: This invention relates to thermoplastic coating compositions which utilize organic solvent solutions of acrylic copolymer as film-forming media.Enhanced distortion resistance is obtained by utilizing acrylic polymer which comprises two types of polar group, the two types interacting strongly. A further embodiment utilizes in addition a plasticizer which comprises a chain of units of the formula --CO--(CH.sub.2).sub.5 --O--.The compositions are useful as lacquers for the automotive and refinish industries.

Abstract: Chemical compounds are provided that are novel 3,6-disubstituted-1,8-naphthalimides (I), as well as methods for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. Compounds of the invention have pharmacological properties and are useful antimicrobial agents.

Abstract: 1,4-Dihydropyridines of the formula ##STR1## in which n is 0,1 or 2, andR.sup.1 to R.sup.7 can have a wide variety of meanings, which possess inotropic action, and many of which are new, are useful in increasing the influx of Ca.sup.++ into cells, particularly in combatting coronary and vascular diseases, hypertension swelling in the mucous membranes and diseases involving increased blood sugar or an incorrect salt and fluid balance.