Abstract: The invention provides a device and a compound for the prevention and/or treatment of uterine fibroids in human patients, wherein the compound is dispensed from the device and is administered locally to the uterine tissue.

Abstract: Provided herein are compositions of a class of substituted diazabicycloalkane derivative compounds, which are useful as modulators of nicotinic acetylcholine receptors. The compounds are useful in treating conditions and disorders prevented by, or ameliorated by, nicotinic acetylcholine receptors.

Abstract: Provided are novel methods of treating and/or preventing a disease or condition caused by or associated with a virus belonging to the Bunyaviridae or Togaviridae family using iminosugars, such as DNJ derivatives.

Abstract: Sulfanyl-tetrahydropyran-based compounds, pharmaceutical compositions comprising them, and methods of their use for the treatment of diseases and disorders such as diabetes and obesity are disclosed.

Abstract: The present invention relates to the use of certain derivatives of cycloheximide or the pharmaceutically acceptable salts thereof for the manufacture of a medicament for the treatment or prevention of ischaemias, of cardiopathies, of endothelial disorders, of traumata, of necroses, of pulmonary disorders, of vascular disorders, of forms of shock, of blood flow impairments or of stroke; or for the manufacture of a medicament for the treatment or prevention of diseases caused by ischaemia; or for the manufacture of a composition for the preservation and/or storage of transplants, especially of organs.

Abstract: Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.

Abstract: Provided is a method of increasing the stability of wild-type ?-glucocerebrosidase. Also provided are methods of treating and/or preventing an individual having a neurological disease in which increased expression or activity of ?-glucocerebrosidase in the central nervous system would be beneficial. This method includes administering an effective amount of a pharmacologic chaperone for ?-glucocerebrosidase, with the proviso that the individual does not have a mutation in the gene encoding ?-glucocerebrosidase. Further provided are ?-glucocerebrosidase inhibitors which have been identified as specific pharmacologic chaperones and which have been shown to increase activity of ?-glucocerebrosidase in vivo in the central nervous system.

Abstract: The invention provides methods, reagents and systems to preferentially mark fast-proliferating cells/tissues (such as cancer), by incorporating non-natural amino acids into proteins, preferably in vivo, using the endogenous protein synthesis machinery of an organism. The incorporated non-natural amino acids contain reactive groups for further chemical reagents, which may serve as a “handle” to for a number of uses, such as imaging of cancer cells, targeting drugs to preferentially kill cancer cells, and proteomic analysis in the context of large scale or high throughput screening for candidate drug leads that affects the proliferation of a target cell, etc.

Abstract: Embodiments of this invention provide methods for thereapeutic use of cyclic G-2-Allyl Proline to treat disorders of dopaminergic neurons, including Parkinson's disease. Cyclic G-2Allyl P is neuroprotective and has utility as a therapeutic agent for treatment of diseases and other conditions characterised by degeneration and/or death of dopaminergic neurons and the adverse symptoms of such degeneration and/or death. Such symptoms include loss of cognition and motor function. Compounds are also useful for manufacture of medicaments including tablets, capsules and injectable solutions that are useful for treatment of such conditions.

Abstract: This invention relates to pulsatile dose administration of gossypol or pharmaceutical compositions thereof for treating diseases, disorders and conditions responsive to gossypol, inhibiting the activity of anti-apoptotic Bcl-2 family proteins, inducing apoptosis in cells and increasing the sensitivity of cells to inducers of apoptosis.

Abstract: The present invention provides novel hydroxy piperidine (HP) derivatives having (i) a positive charge at the position corresponding to the anomeric position of a pyranose ring; (ii) a short, flexible linker emanating from the corresponding position of the ring oxygen in a pyranose; and (iii) a lipophilic moiety connected to the linker and pharmaceutically acceptable salts thereof. The linker can be absent if the lipophilic moiety corresponds to a hydrocarbon chain with a linear length of 6 or more carbons. The present invention further provides a method for treating individuals having Gaucher disease by administering the novel HP derivative as “active-site specific chaperones” for the mutant glucocerebrosidase associated with the disease.

Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.

Abstract: The present invention relates to new triazole modulators of aromatase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: 1,5-Dideoxy-1,5-imino-D-glucitol compounds as shown in the specification. Also disclosed is a method of treating a hexosaminidase-associated disease.

Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.

Abstract: The present invention provides methods for treating a flavivirus infection, including hepatitis C virus (HCV) infection, in an individual suffering from a flavivirus infection. In some embodiments, the methods involve administering to an individual in need thereof an effective amount of an agent that inhibits enzymatic activity of a membrane-bound ?-glucosidase inhibitor. In other embodiments, the methods involve administering to an individual in need thereof effective amounts of an ?-glucosidase inhibitor and at least one additional therapeutic agent.

Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.

Abstract: Novel pamoate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4-dimethylpiperidin-2,6-diones and pharmacologically acceptable solvates thereof are devoid of the weight loss and hepatocyte changes in the rat which limited to marginally effective levels the permitted clinical doses of the corresponding hydrochlorides in the treatment or prophylaxis of stress-related affective disorders such as anxiety, depression, migraine and sleep apnoea. The preferred pamoate salts are 3(3,5-dimethoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate.

Abstract: Novel pamoate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4-dimethylpiperidin-2,6-diones and pharmacologically acceptable solvates thereof are devoid of the weight loss and hepatocyte changes in the rat which limited to marginally effective levels the permitted clinical doses of the corresponding hydrochlorides in the treatment or prophylaxis of stress-related affective disorders such as anxiety, depression, migraine and sleep apnoea. The preferred pamoate salts are 3(3,5-dimethoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione pamoate.

Abstract: The present invention relates to essentially pure diastereomers of 4-aryloxy-3-hydroxypiperidines, including purified diastereomers of ifoxetine, methods of purifying said diastereomers, pharmaceutical compositions comprising said diastereomers and methods of treatment utilizing said pharmaceutical compositions.

Abstract: The present invention relates to essentially pure diastereomers of 4-aryloxy-3-hydroxypiperidines, including purified diastereomers of ifoxetine, methods of purifying said diastereomers, pharmaceutical compositions comprising said diastereomers and methods of treatment utilizing said pharmaceutical compositions.

Abstract: The present invention relates to novel piperidine derivatives that are useful as inhibitors of glucosylceramide synthase (GCS) for use in the treatment and prevention of diseases or disorders mediated by GCS, including cancer, infectious diseases, neuronal disorders or injury and inflammatory diseases. The invention further relates to the pharmaceutical composition comprising the novel piperidine derivatives and methods for preparing the same.

Abstract: Compounds and pharmaceutical compositions comprising them are disclosed that may be useful for the treatment of diseases and disorders such as diabetes and obesity.

Abstract: The present invention relates to compounds according to the general formula wherein the dotted lines denote a single bond which is optionally present, with 2 dotted lines denoting a double bond; wherein, in case no double bond is present and a free valence exists, this valence is occupied by H; and wherein the symbols have the meanings defined in the text, or a pharmaceutically acceptable salt thereof, and which lend themselves for the manufacture of drugs useful in the inhibtion of DNA methylation, the inhibition of DNA methyltransferases, and may therefore be useful for the manufacture of pharmaceuticals for the treatment of developmental disorders such as Prader-Willi-Syndrome, Angelman-Syndrome (Happy Puppet Syndrome), Beckwith-Wiedemann-Syndrome, and proliferative diseases, such as coronary restenosis and neoplastic diseases, particularly colon carcinoma, familiary adenomatous polyposis carcinoma and hereditary non-polyposis colorectal cancer, prostate carcinoma, melanoma, non-Hodgkin lymphoma, acu

Abstract: A method for treating a glycolipid storage-related disorder, comprising administering a therapeutically effective amount of an inhibitor of glycolipid synthesis in combination with an agent capable of increasing the rate of glycolipid degradation or in combination with bone marrow transplantation. Inhibitors of glycolipid synthesis include N-butyldeoxynojirimycin (NB-DNJ), N-butyldeoxygalactonojirimycin (NB-DGJ) or N-nonyldeoxynojirimycin (NN-DNJ). Glycolipid storage-related disorders include Gaucher disease, Sandhoff's disease, Fabry's disease, Tay-Sach's disease, Niemann-Pick C storage disease, GM1 gangliosidosis, genetic disorders in which neuronal glycolipid accumulation contributes to disease pathology.

Abstract: Sex steroid potentiated disorders including, prostate cancer and breast cancer, in a patient in need of treatment thereof, are treated with an amount of nitric oxide donating compound and/or nitrosoglutathione reductase inhibitor and/or cysteine binder different from that provided by nitric oxide donating compound effective to inhibit activation of steroid receptor. Variations include using only nitric oxide donating agent as treating agent; using only nitrosoglutathione reductase inhibitors as treating agent, using nitric oxide donating agent plus nitrosoglutathione reductase inhibiting agent; for prostate cancer treatment using prostate cancer drug modified to contain nitric oxide donating moiety or FDA approved nitric oxide donating agent and FDA approved prostate cancer treating agent. Also disclosed is an assay for assessing mutagenic potential of prostate cancer in a patient.

Abstract: Novel bisulphate salts of certain 3-phenyl-3-dimethylaminoalkyl-4,4-dimethylpiperidin-2,6-diones and pharmacologically acceptable solvates thereof are devoid of the weight loss and hepatocyte changes in the rat which limited to marginally effective levels the permitted clinical doses of the corresponding hydrochlorides in the treatment or prophylaxis of stress-related affective disorders such as anxiety, depression, migraine and sleep apnea. The preferred bisulphate salts are 3(3,5-dimethoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione bisulphate and, especially, 3(3-methoxyphenyl)-3-(3-dimethylaminopropyl)-4,4-dimethylpiperidine-2,6-dione bisulphate.

Abstract: The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof. The inhibitors according to the present invention are useful as therapeutic agents for kidney diseases, cerebrovascular diseases, or circulatory diseases. In addition, the present invention also provides novel hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof.

Abstract: The present invention provides compounds having formula (II): wherein X, n, R1–R12 are defined herein, or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound represented by formula (II) and a pharmaceutically acceptable carrier or excipient. The invention further provides a method for treating cancer comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound represented by formula (II).

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.

Abstract: Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and for the treatment of tumors

Abstract: The present invention provides compounds having formula (I): and formula (II): wherein X, n, and R1-R12 are defined herein, or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound represented by formula (I) or (II) and a pharmaceutically acceptable carrier or excipient. The invention further provides a method for treating cancer comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound represented by formula (I) or (II).

Abstract: The present invention is directed to compounds useful as selective serine protease or dual-serine protease inhibitors, compositions thereof and methods for treating serine protease or dual-serine protease mediated disorders.

Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.

Abstract: A method of enhancing the activity of lysosomal &agr;-Galactosidase A (&agr;-Gal A) in mammalian cells and for treatment of Fabry disease by administration of 1-deoxy-galactonojirimycin and related compounds.

Abstract: This application provides methods of improving gene therapy by combining gene therapy with active site-specific chaperones (ASSCs). The ASSC increases the stability and efficiency of the protein encoded by the recombinant gene that is administered.

Abstract: Designed imminocyclitols have potent inhibition activity with respect to hexoaminidases and glycosidases.

Abstract: The invention relates to Siglec inhibitors that have an increased affinity for the receptor molecule. The Siglec inhibitors provided by the invention are preferably selective of a given Siglec molecule. The invention further relates to a method for producing Siglec inhibitors and to a method for increasing the binding selectivity for a given Siglec molecule. The invention also relates to pharmaceutical compositions that contain the Siglec inhibitors and to medical indications for the Siglec inhibitors.

Abstract: A method and compositions for controlling weight in human beings.

Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.

Abstract: Compounds of formula (I): 1

Abstract: Compounds of general structural formula (1) are shown to have AMPA receptor enhancing properties. The compounds are useful for such therapeutic purposes as facilitating the learning of behaviors dependent upon AMPA receptors, and in treating conditions, such as memory impairment, in which AMPA receptors, or synapses utilizing these receptors, are reduced in numbers or efficiency. They may also be used to enhance excitatory synaptic activity in order to restore an imbalance between brain subregions, as in treatment of schizophrenia or schizophreniform behavior.

Abstract: Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1-C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.

Abstract: Heterocyclic compound represented by the formula I 1

Abstract: The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1 may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, an optionally substituted heterocyclic group or SR2, etc., X1 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group or —NR3—, etc, X2 is a bond, an optionally substituted divalent C1-3 aliphatic hydrocarbon group, —NR4—, —O— or —S(O)p— (wherein p is 0, 1 or 2), each Y may be same or different and is a hydrogen atom, an optionally substituted hydrocarbon group, a halogen atom, a carboxyl group, an acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, SR5, an oxo group, a thioxo group, an optionally substituted imino group, a nitro group, a cyano group, etc.

Abstract: A combination drug therapy is disclosed for the treatment of a patient affected with Gaucher's disease or other such glycolipid storage diseases. The method comprises administering to said patient a therapeutically effective amount of both a N-alkyl derivative of deoxynojirimycin (DNJ) and a glucocerebrosidase enzyme to alleviate or inhibit the glycolipid storage disease. The alkyl group has from about two to about 20 carbon atoms and preferably is butyl, nonyl or decyl.

Abstract: A compound of formula (I) wherein: n is 1 or 2; R1 is chloro, fluoro, bromo, methyl or methoxy; R2 is as defined within; R3 is as defined within; and R4 is hydrogen or fluoro; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.

Abstract: Methods for treating lipid storage diseases using compounds that inhibit glucosyltransferase enzymes are disclosed herein. The invention relates to the treatment of lipid storage disease with compounds that inhibit glucosyltransferase activity in the affected cells. It relates particularly to the use of 1,5-dideoxy-1,5-imino-D-glucitol and derivatives thereof.

Abstract: A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I with an alkylating agent of structure III in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N?-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.