Abstract: Methods are described for treating an influenza viral infection or associated diseases, disorders or mechanisms in a subject, comprising administering to the subject a therapeutically effective amount of a catecholic butane of the general formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 and R2 each independently represents a hydrogen, a lower alkyl, a lower acyl, an alkylene, or —OR1 and —OR2 each independently represents an unsubstituted or substituted amino acid residue or pharmaceutically acceptable salt thereof; R3, R4, R5, R6, R10, R11, R12 and R13 each independently represents a hydrogen, or a lower alkyl; and R7, R8 and R9 each independently represents a hydrogen, —OH, a lower alkoxy, a lower acyloxy, an unsubstituted or substituted amino acid residue or pharmaceutically acceptable salt thereof, or any two adjacent groups together may be an alkyene dioxy; with the proviso in certain circumstances that where one of R7, R8 and R9 represents a hydrogen, then —OR1, —OR2 and the oth

Abstract: The comprehensive pharmacologic therapy for treatment of obesity is a procedure which involves the administration of a desired therapeutic range of Diethylpropion and/or Phentermine in combination with a SSRI medication and nutritional supplementation for brief and long durations which may be 12 months or more. The preferred procedure involves the administration of drugs in combination which are identified as: Citalopram (Celexa) and Phentermine; Citalopram (Celexa) and Diethylpropion; Citalopram (Celexa), Phentermine, and Diethylpropion. In addition nutritional supplementation such as a multivitamin, 5-Hydroxytryptophan, vitamin B6, vitamin C, Tyrosine, Calcium, and Lysine may be used to enhance the performance of the weight loss treatment program.

Abstract: This disclosure relates to methods of inhibiting cell motility or cell migration, and of treating diseases involving cell migration or cell motility, using polyamine analogs, such as conformationally restricted polyamine analogs. The diseases to be treated include immune disorders, inflammatory conditions, infection, abnormal immune responses, undesired angiogenesis, tumor cell metastasis or invasion, atherosclerosis, vascular graft occlusion, transplant rejection, other complications of transplants, glomerulonephritis, arthritis, inflammatory responses subsequent to stroke or ischemia, and asthma.

Abstract: An acid addition salt of a carba-sugar amine derivative represented by the following formula (1): wherein R1 and R2 each independently represents a hydrogen atom, or an alkyl group, an alkenyl group, an alkynyl group, an acyl group, an aryl group or an aralkyl group which may have one or at least two of the following substituent (I) or (II), or R1 and R2 are taken together to represent a substituent (III) (R8 to R12 each independently represents an alkyl group, an alkenyl group, an alkynyl group, an acyl group, an aryl group or an aralkyl group), with the proviso that both R1 and R2 are not a hydrogen atom at the same time; R3, R4 and R7 each independently represents a hydroxyl group or a hydroxyl group having a substituent; and R5 and R6 each independently represents a hydrogen atom, or a hydroxyl group or a hydroxyl group having a substituent, with the proviso that when one of R5 and R6 is a hydrogen atom, the other is a hydroxyl group or a hydroxyl group having a substituent.

Abstract: For controlling the condition of type 2 diabetes, a pharmaceutical including a combination of mitiglinide, a pharmacologically acceptable salt thereof or a hydrate thereof and an ?-glucosidase inhibitor such as voglibose or acarbose, and a therapeutic method using the pharmaceutical are provided. The pharmaceutical according to the present invention has an extremely strong effect of decreasing a morning fasting blood glucose level, a postprandial blood glucose level and HbA1C of a patient with type 2 diabetes, and can improve glucose spike, insulin resistance and lipid metabolism.

Abstract: The invention relates to a pharmaceutical dosage form comprising an analgesic combination for simultaneous or sequential use which comprises a peripherally restricted cannabinoid CB1 receptor agonist having a brain Cmax to plasma Cmax ratio of less than 0.1 and an opioid receptor agonist, as well as to a method for treating pain using said pharmaceutical dosage form.

Abstract: This invention relates to diamondoid derivatives which exhibit therapeutic activity. Specifically, the diamondoid derivatives herein exhibit therapeutic effects in the treatment of viral disorders. Also provided are methods of treatment, prevention and inhibition of viral disorders in a subject in need.

Abstract: A method for treating autism comprising the step of administering an effective amount of a medicament characterized as a NMDA-receptor antagonist or a pharmaceutically acceptable salt thereof.

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.

Abstract: The present invention is directed to pest-controlling compositions comprising as active ingredients one or more ?-diones, particularly ?-diketones and ?-triketones, and to the use of these compositions inter alia for preventing, eradicating, destroying, repelling or mitigating harmful, annoying or undesired pests including insects, arachnids, helminths, molluscs, protozoa and viruses. The present invention is further directed to processes of preparing ?-diones by de novo synthesis or from natural sources such as volatile oil-bearing plants from families including Alliaceae, Apiaceae, Asteraceae, Cannabinaceae, Lamiaceae, Pteridaceae, Myrtaceae, Myoporaceae, Proteaceae, Rutaceae and Zingiberaceae.

Abstract: The present disclosure is directed to methods and formulations for treating, modifying, and/or managing at least one upper gastrointestinal symptom. Methods of using at least one ?3 ?4 nAChR antagonist and formulations comprising at least one ?3 ?4 nAChR antagonist, or pharmaceutically acceptable salt thereof are included.

Abstract: Peptide conjugates in which cytostatic and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.

Abstract: Methods are disclosed for inhibiting or disrupting Janus tyrosine kinase 3 (Jak3) dependent function in cells of lymphoid or myeloid origin, especially for blocking proliferation and function of lymphocytes (e.g., T-cells, B-cells). A Mannich base compound, or a derivative or modified compound, is employed which is capable of selectively inhibiting Jak3 while affecting other protein tyrosine kinase activities to a lesser extent or not at all, to provide beneficial effects such as mitigation of transplant rejection and alleviation of allergic responses with fewer side effects than with conventional immunosuppressive agents.

Abstract: An object of the present invention is to find new pharmacological actions of urea compounds having structure represented by the general formula [1]. The urea compounds having the structure represented by the general formula [1] have excellent angiogenesis inhibitory actions. [wherein “A” is —(NR4)—, —(CR5R6)— or —O—, “B” is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantylalkyl or the like, R3 is aryl or an unsaturated heterocycle, and X is oxygen or sulfur.

Abstract: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.

Abstract: Methods are disclosed for inhibiting or disrupting Janus tyrosine kinase 3 (Jak3) dependent function in cells of lymphoid or myeloid origin, especially for blocking proliferation and function of lymphocytes (e.g., T-cells, B-cells). A Mannich base compound, or a derivative or modified compound, is employed which is capable of selectively inhibiting Jak3 while affecting other protein tyrosine kinase activities to a lesser extent or not at all, to provide beneficial effects such as mitigation of transplant rejection and alleviation of allergic responses with fewer side effects than with conventional immunosuppressive agents.

Abstract: The present invention provides wherein R1 is selected from the group consisting of C1-C10 alkoxy, OH and NR4R5; R2 is selected from the group consisting of C1-C10 alkyl and (CH2)nOH; R3 is selected from the group consisting of C1-C10 alkyl, heteroaryl, e.g. thienyl, furanyl and pyridyl, phenyl, mono, -di-, tri-substituted phenyl and heteroaryl; R4 and R5 are independently selected from the group consisting of H, C1-C10 alkyl, C1-C10 alkyl hydroxyl; m is 0 or an integer from 1 to 3 and n is an integer of from 1 to 4. These compounds are useful in lowering intraocular pressure and/or treating glaucoma or providing neuroprotection to the eye of a human patient.

Abstract: Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.

Abstract: The invention provides compositions, methods and uses comprising a scyllo-inositol compound of the formula Ia or Ib or a compound of the formula Ia or Ib wherein one, two or three hydroxyl groups are replaced by substituents with retention of configuration, or pharmaceutically acceptable salts thereof, in a therapeutically effective amount to provide beneficial effects in the treatment of an amyloid-related disease.

Abstract: The present invention provides 4-substituted-2-azetidinone compounds, bicyclic 2-5-diketopiperazine compounds, and pharmaceutical compositions thereof that are potent, safe and effective neuroprotective agents. Due to their strong central nervous system (CNS) activity, the compounds can be used to enhance memory and to treat a variety of neurological disorders. The compounds are particularly useful for treating neurological disorders caused by, or associated with, CNS trauma.

Abstract: Glycolytic inhibitors are useful in the treatment of solid tumors by attacking anaerobic cells at the center on the tumor. 2-deoxyglucose, oxamate and various analogs thereof are identified as having a natural selective toxicity toward anaerobic cells, and will significantly increase the efficacy of standard cancer chemotherapeutic and radiation regiments as well as new protocols emerging with anti-angiogenic agents.

Abstract: Methods for modulating macrophage proliferation in an individual afflicted with or at risk for a macrophage-associated disease are provided. The methods employ a polyamine analog, or salt or protected derivative thereof. Macrophage proliferation has been implicated in a number of serious disorders, including AIDS (HIV)-associated dementia, AIDS-associated non-Hodgkin's lymphoma, and Alzheimer's disease. The invention also provides methods for aiding diagnosis and monitoring therapy of a macrophage-associated non-HIV associated dementia, especially Alzheimer's disease. The invention also provides methods of delaying development of macrophage-associated non-HIV associated dementias, including Alzheimer's disease, which entail administration of an agent which modulates macrophage proliferation.

Abstract: A method for treating or preventing a disorder or a condition by double inhibition of serotonin (5-HT) and noradrenaline (NA) reuptake in a subject in need thereof, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity, comprising the step of administering to said subject a mixture of enantiomers of milnacipran enriched in the (1S,2R) enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts.

Abstract: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.

Abstract: N,N?-bis(3-aminopropyl)cyclohexane-1,4-diamine, of formula (I), is a new compound that is prepared by hydrogenation with Raney nickel catalyst of N,N?-bis(2-cyanoethyl)-cyclohexane-1,4-diamine, the latter being prepared by reaction between 1,4-cyclohexanediamine and acrylonitrile. The oral administration to genetically alcoholic rats (from the strain UChB of the University of Chile) of the tetrametanesulfonate monohydrate of (I) causes a significant reduction in the alcohol consumption. The activity lasts for some time after the treatment period. Besides, there is a virtually null disulfiram-like adverse effect, what constitutes an advantage over the unpleasant use of some anti-alcoholism agents, such as calcium cyanamide or disulfiram itself.

Abstract: Substituted 1-aminobutane-3-ol compounds, methods for producing them, pharmaceutical compounds containing them, and the use of substituted 1-aminobutane-3-ol compounds for producing pharmaceutical compounds.

Abstract: The present invention concerns the use of a mixture of enantiomers enriched in the dextrogyral enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts, for the preparation of a drug intended to prevent or to treat disorders that can be managed by double inhibition of serotonin (5-HT) and norepinephrine (NE) reuptake, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity.

Abstract: A bioreductive conjugate comprises a bioreductive moiety with at least one therapeutic agent linked thereto and physiologically acceptable derivatives thereof. The bioreductive moiety incorporates an aromatic ring substituted with a nitro group and the conjugate is such that bioreduction of the nitro group causes release of the therapeutic agent by a through bond elimination and the residue of the bioreductive moiety to undergo an intramolecular cyclization reaction in which the nitrogen of the original nitro group provides an atom of the thus formed ring.

Abstract: Unsaturated 1-Amino-alkylcyclohexane compounds which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.

Abstract: Compounds of formula (1): wherein R1, R2, R3, R4, R5 and R6 are independently selected from hydrogen, alkyl, aryl and non-aromatic heterocyclic groups, or each of one or more pair(s) of the substituent groups R1 to R6 may together form a 3,4,5,6,7 or 8-membered ring containing 0,1 or 2 heteroatom(s); R7 is selected from alkyl, aryl and non-aromatic heterocyclic groups; and R8 is selected from hydrogen, halogen, alkyl, aryl and non-aromatic heterocyclic groups; and pharmaceutically acceptable salts and prodrugs thereof, are useful for treating conditions generally associated with abnormalities in glutamatergic transmission.

Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF&agr;) inhibitors and immunomodulators are provided. These compounds have pharmacological applications as well as uses in assays relating to TNF&agr; and other involved cytokines. As pharmaceuticals, these compounds are used to treat inflammatory, infectious, autoimmune or other proliferative diseases and conditions related to the unwanted presence or activity of TNF&agr; and/or one or more other involved cytokines, alone or in combination with other agents.

Abstract: Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to, porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.

Abstract: N,N′-bis(3-aminopropyl)cyclohexane-1,4-diamine, of formula (I), is a new compound that is prepared by hydrogenation with Raney nickel catalyst of N,N′-bis(2-cyanoethyl)-cyclohexane-1,4-diamine, the latter being prepared by reaction between 1,4-cyclohexanediamine and acrylonitrile. The oral administration to genetically alcoholic rats (from the strain UChB of the University of Chile) of the tetrametanesulfonate monohydrate of (I) causes a significant reduction in the alcohol consumption. The activity lasts for some time after the treatment period. Besides, there is a virtually null disulfiram-like adverse effect, what constitutes an advantage over the unpleasant use of some anti-alcoholism agents, such as calcium cyanamide or disulfiram itself. Therefore, the compounds of the invention are useful for the preparation of medicaments for the therapeutic and/or prophylactic treatment of alcoholism in mammals, including human beings.

Abstract: An improved medicinal composition includes an effective amount of a pain relieving and anti-inflammatory pharmaceutical and an effective amount of a nutraceutical in a pharmaceutically acceptable base. At least one of the pharmaceutical and the nutraceutical treats a condition caused by an immune response to a virus, a microorganism, or an atmospheric pollutant or allergen. The pain relieving and anti-inflammatory pharmaceutical is preferably acetaminophen or a non-steroidal anti-inflammatory drug (NSAID). The medicinal composition may additionally include a pharmaceutical decongestant or antihistamine. The nutraceutical is preferably an immune booster, an anti-oxidant, a liver protectant, or a combination thereof. Methods of using these compositions to treat conditions caused by an immune response are also disclosed.

Abstract: Compounds of the general formula I 1

Abstract: An object of the present invention is to provide a modified cyclic aliphatic polyamine having a low viscosity and a small content of unreacted polyamine which can provide, when it is used as a curing agent for epoxy resin, an epoxy resin composition having an improved workability without adding solvent or diluent and an excellent property of epoxy resin cure product. The above modified cyclic aliphatic polyamine is obtained by addition reaction of a cyclic aliphatic polyamine such as isophoronediamine and norbornanediamine and an alkenyl compound such as styrene. The modified cyclic aliphatic polyamine thus obtained is added in epoxy resin to be used as a curing agent for epoxy resin.

Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.

Abstract: This invention concerns the use of cyclopamine in vivo on basal cell carcinomas (BCC's) to achieve therapeutic effect by causing differentiation of the tumor cells and, at the same time, apoptotic death and removal of these tumor cells while preserving the normal tissue cells, including the undifferentiated cells of the normal epidermal basal layer and hair follicles. Causation of apoptosis by cyclopamine is by a non-genotoxic mechanism and thus unlike the radiation therapy and most of the currently used cancer chemotherapeutics which act by causing DNA-damage. These novel effects, previously unachieved by a cancer chemotherapeutic, make the use of cyclopamine highly desirable in cancer therapy, in the treatment of BCC's and other tumors that use the hedgehog/smoothened signal transduction pathway for proliferation and prevention of apoptosis.

Abstract: Therapeutic agents for erectile dysfunction containing as the active ingredient prostaglandin derivatives of formula (I) (wherein symbols have the same meanings as described in the description), nontoxic salts thereof, or cyclodextrin clathrate compounds thereof.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: The present invention relates to novel scyphostatin analogues, which distinguish themselves by acting as SMase inhibitors so that they are of therapeutic use for a number of diseases such as a HIV infection, neurodegenerative diseases, inflammatory diseases, apoplexy, ischemia, myocardial infarction or in the case of atherosclerosis.

Abstract: Cosmetic or pharmaceutical compositions comprising compounds of formula (I) and the corresponding salts thereof: 1

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: Aminocyclohexane and aminoalkylcyclohexane compounds, which are systemic-ally-active as NMDA receptor antagonists, are effective in inhibiting abnormal hyperphosphorylation of microtubule associated protein tau, method of treating disorders resulting from or associated with abnormal hyperphosphorylation of microtubule associated protein tau, and pharmaceutical compositions comprising the same.

Abstract: Methods and compositions for treating disease caused by microorganisms, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.

Abstract: A method for treatment of neuropsychiatric symptoms or disorders emanating from primary brain or systemic impairments includes administration of an effective dose of a dopamine, serotonin, and norepinephrine reuptake inhibitor to a human in need of such treatment. The preferred reuptake inhibitor is sibutramine.

Abstract: Unsaturated 1-Amino-alkylcyclohexane compounds which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.

Abstract: Certain 1-aminoalkylcyclohexanes are anti-trypanosomiasis agents and trypanocides. Pharmaceutical compositions thereof for such purpose and method of making same, as well as a method-of-treating trypanosomiasis therewith.