Abstract: The amount of penetration into the skin in adhesive patches generally tends to show a certain peak and trough. An adhesive patch is provided in which the drug shows satisfactory penetrability because of a polymer proportion and drug penetration is constant over a certain period. The adhesive patch for external use has a pressure-sensitive adhesive layer containing a drug. It is characterized in that the pressure-sensitive adhesive layer comprises: polyvinylpyrrolidone and/or a copolymer of monomers including vinylpyrrolidone as the main ingredient; and a (meth)acrylic ester copolymer having a basic nitrogen atom and/or cationic nitrogen atom.

Abstract: Controlled-release preparations of oxcarbazepine and derivatives thereof for once-a-day administration are disclosed. The inventive compositions comprise solubility- and/or release enhancing agents to provide tailored drug release profiles, preferably sigmoidal release profiles. Methods of treatment comprising the inventive compositions are also disclosed.

Abstract: Methods of treating or preventing chronic pain or convulsion are disclosed by administering to an animal a sodium channel blocker and at least one of gabapentin and pregabalin. Also disclosed are pharmaceutical compositions and kits for the treatment or prevention of chronic pain or convulsion.

Abstract: A method and a composition for the treatment of an Inflammatory Bowel Disease (IBD) or intestine polyposes is described. The method includes the local administration to the colon of a therapeutically effective amount of at least one Selective Serotonin Reuptake Inhibitor (SSRI) or at least one tricyclic antidepressant (TCA).

Abstract: The present invention is a method for the treatment of depression comprising administering to a subject in need thereof a therapeutically effective amount of one or more carbamate compounds of Formula 1 and/or Formula 2 as herein defined and shown below for the treatment of depression. The present invention is directed to a method for the treatment of depression, which includes mono-therapy and alternatively, co-therapy with at least one additional antidepressant.

Abstract: The present invention relates to a novel dispersible tablet composition, which comprises of a pharmacologically active ingredient and at least one excipient, which reduces the sedimentation rate of active ingredient. This invention further relates to a process for the preparation of a dispersible tablet of a pharmacologically active ingredient.

Abstract: A compound of formula (I) or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, T, L, W, X, Y and A are as defined herein for the for treatment of conditions mediated by the blockade of an epithelial sodium channel, particularly an inflammatory or allergic condition.

Abstract: The present invention relates to the use of carbamazepine derivatives in treating tinnitus.

Abstract: The invention relates to the use of sabcomeline or a pharmaceutically acceptable salt thereof in monotherapy for the treatment of bipolar disorder or mania or and to adjunctive and simultaneous combination therapies for the treatment of bipolar disorder or mania in which sabcomeline or a pharmaceutically acceptable salt thereof and at least one other mood stabilizing or antimanic agent are administered adjunctively or simultaneously. The invention provides methods of treatment of bipolar disorder or mania utilizing such monotherapy and such adjunctive or simultaneous therapeutic combination therapies, therapeutic combinations for use therein and pharmaceutical compositions comprising them.

Abstract: The present invention includes compositions and methods treat a patient suffering from one or more symptoms of cardiac hypertrophy, hypertension and/or ischemia by administering a pharmaceutically effective amount of a pharmaceutical composition having an anti-epileptic drug and an antibiotic to the patient, for example, the anti-epileptic drug may be carbamazepine and the antibiotic may be doxycycline.

Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt 6f amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.

Abstract: Process for preparing a cocrystal of an active substance and a cocrystal former, the process involving precipitating the active substance and the cocrystal former together from solution or suspension, in the presence of a supercritical or near-critical fluid, in particular using a GAS, SAS, SEDS or SAS-EM process. The invention also provides a cocrystal prepared using such a process, and its use as a seed crystal in a subsequent process for precipitating a cocrystal of an active substance and a cocrystal former.

Abstract: Compounds that inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. The compounds of the invention are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the compound can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

Abstract: In accordance with the present invention, it has been discovered that compounds exhibiting activity as a potent noradrenaline reuptake inhibitor (e.g., a NA:5HT ratio of greater than or equal to about 1000:1), and activity at the dopamine D2 receptor sites (e.g., lofepramine) are effective in the treatment and prevention of various diseases and disorders associated with noradreanaline reuptake, such as ADHD, CFS, fibromyalgia, and depression with pain.

Abstract: Described are controlled release nanoparticulate formulations comprising a nanoparticulate agent to be administered and a rate-controlling polymer which functions to prolong the release of the agent following administration. The novel compositions release the agent following administration for a time period ranging from about 2 to about 24 hours or longer.

Abstract: The present invention provides compositions, methods and kits for treating, preventing or reducing the risk of developing a CNS disorder. In general, the invention involves utilizing caffeine for preventing or alleviating pathological symptoms of a CNS disorder, such as headache, epilepsy, pain, Parkinson's disease, psychiatric disorders such as anxiety, bipolar disorder, depression, and schizophrenia, ADD, and ADHD.

Abstract: The present invention relates to compositions and methods for the detecting, preventing, treating, and empirically investigating seizures and seizure related disorders (e.g., West syndrome, TSC, childhood absence epilepsy, benign focal epilepsies of childhood, juvenile myoclonic epilepsy (JME), temperol lobe epilepsy, frontal lobe epilepsy, Lennox-Gastaut syndrome, occipital lobe epilepsy). In particular, the present invention provides compositions and methods for detecting, treating, preventing and empirical investigating seizures and seizure related disorders through inhibition of mTOR function. In addition, the present invention provides methods and compositions that utilize mTOR inhibiting agents (e.g., rapamycin) in the detecting, preventing, treating, and empirical investigating of seizures and seizure related disorders.

Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).

Abstract: Methods of treating and or preventing substance abuse/dependence, and alcohol abuse/dependence in particular. Combinations of medications are also disclosed.

Abstract: The invention relates to 6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl derivatives of formula I wherein R1, R2 and R3 are as defined herein. The compounds are ?-secretase inhibitors useful in the treatment of Alzheimer's disease or common cancer, including, but not limited to, cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.

Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.

Abstract: This invention provides novel methods of treatment to ameliorate or prevent cognitive disorder/dysfunction in pre- or asymptomatic subject having one or more mutations in the Huntington gene. The methods involve increasing the expression or activity of the neurotrophin BDNS in the brain of said subject.

Abstract: The invention relates to an oral multiparticle pharmaceutical dosage form in the form of a receptacle reducing the pH values of stomach, containing a plurality of pellets, particles, granules or agglomerates whose mean diameter ranges from 50 to 2500 ?n substentially consisting of a) an internal matrix layer containing an active agent which is neither peptide or protein, nor the derivatives or conjugates thereof, a lipophilic matrix whose melting point is greater than 37° C. and a polymer with mucoadhesive effect, b) an external film coating substentially consisting of a polymer or an anionic copolymer which is optionally formulated with conventional pharmaceutical additives, wherein the active agent has a water solubility according to DAB 10, of at least 30 volume parts of water for one part by weight of the active agent and is coated with the lipophilic matrix and said active agent-containing lipophilic matrix is coated with a matrix made of a polymer with mucoadhesive effect.

Abstract: Methods of treating or preventing chronic pain or convulsion are disclosed by administering to an animal a sodium channel blocker and at least one of gabapentin and pregabalin. Also disclosed are pharmaceutical compositions and kits for the treatment or prevention of chronic pain or convulsion.

Abstract: Disclosed herein is a pharmaceutical composition comprising a serotonin-norepinephrine reuptake inhibitor and a pan-alpha-2 receptor agonist. The composition is effective for treating chronic pain, and methods of treating pain using the composition and compounds comprising it are also disclosed.

Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.

Abstract: A pharmaceutical dosage form comprising a mixture of a therapeutically effective amount of oxcarbazepine having median particle size ranging from about 15 ?m to about 26 ?m and one or more hydrophilic polymers, said mixture being formed by subjecting a suspension comprising said oxcarbazepine and a hydrophilic polymer in a solvent, to mixing in a homogenizer, optionally removing the solvent and converting the said mixture into a dosage form.

Abstract: The subject invention provides a composition comprising a mixture of polypeptides in the form of a tannate salt wherein each polypeptide is a copolymer of the amino acids L-glutamic acid, L-alanine, L-tyrosine and L-Lysine, methods of preparation and uses thereof.

Abstract: The present invention is a method for the treatment of Disruptive Behavior Disorders including both Conduct Disorder and Oppositional Defiant Disorder comprising administering to a subject in need thereof a therapeutically effective amount of one or more carbamate compounds of Formula 1 and/or Formula 2 as herein defined and shown below. The present invention is directed to a method for the treatment of Disruptive Behavior Disorders including both Conduct Disorder and Oppositional Defiant Disorder, which includes mono-therapy and alternatively, co-therapy with at least one additional psychoactive medication.

Abstract: Provided herein methods of screening for potential antidepressant compounds effective to increase production of cellular CDP-diacylglycerol and synthesis of inositol phospholipid in depression-related areas of the brain. Also, provided are methods of diagnosing and treating depressive or mood disorders in a subject by administering these screened antidepressant compounds. Further provided is a method of determining the therapeutic efficacy of an antidepressant drug regimen by comparing the ratio of CDP-diacylglycerol/inositol phosphate after treatment to a basal ratio in a subject.

Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.

Abstract: The present invention relates to methods of treatment using the compound (+)-isopropyl 2-methoxyethyl 4-(2-chloro-3-cyano-phenyl)-1,4-dihydro-2,6-dimethyl-pyridine-3,5-dicarboxylate, as a sole active agent or in combination with other pharmacological agents.

Abstract: A process for micronization of pharmaceutically active agents.

Abstract: The invention relates to methods and compositions for treating premature ejaculation in a male or prolonging intercourse comprising administering to the male an antidepressant via a route selected from the group consisting of mucosal administration (preferably nasal, buccal or rectal), administration to the lungs (preferably by inhalation), local administration to at least a part of the male genitalia (applied to the penis for example, in the form of a gel) and combinations thereof.

Abstract: The present invention provides for new crystal forms of oxcarbazepine, more particularly oxcarbazepine Forms B, C, D and E. The present invention further provides processes for preparation of these forms. Form B is prepared by evaporating the solvents from a solution of oxcarbazepine in toluene and dichloromethane. Form B is also obtained by immediately cooling the solution of oxcarbazepine and toluene. Cooling the same solution at a slower rate, but still fairly rapidly, results in oxcarbazepine Form C. Cooling the same solution at even a slower rate results in another Form, oxcarbazepine Form D. Oxcarbazepine Form E, a solvate of chloroform, is obtained by precipitating a solution of oxcarbazepine and chloroform. The present invention also provides processes for converting one of the newly discovered crystal forms of oxcarbazepine into another crystal form, including Form A, which is in the prior art.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: The invention relates to pharmaceutically active compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention and particularly useful for the treatment or prophylaxis of diseases associated with parasitic infection such as pneumocystis pneumonia, toxoplasmosis, cryptosporidiosis, leischmaniasis and malaria.

Abstract: Basic monocyclic compounds having general formula (I) useful as NK-2 antagonists are described, processes for their preparation and pharmaceutical compositions containing them are also described.

Abstract: This invention relates to cyclized conotoxin peptides, processes for their preparation and their pharmaceutical use.

Abstract: The present invention provides substituted 11-phenyl-dibenzazepine compounds which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Abstract: A method of treating pain by the co-administration of an antidepressant together with one or more precursors or inducers of neurotransmitters, particularly amino acids selected from L-phenylalanine, L-tyrosine, L-tryptophan and L-DOPA.

Abstract: Carbamazepine, in extended release form, is useful in the treatment of patients suffering from bipolar disorder. In order to minimize the time it takes to reach efficacy, carbamazepine, in extended release form, can be administered to the patient at an initial daily dose which is then increased in daily increments until clinical efficacy is achieved.

Abstract: The present invention relates compounds of the formula (I): wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of: (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l) and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R?17, R18, R19, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.

Abstract: The object of the present invention is to provide soluble ?-amyloid precursor protein secretory stimulators, which are effective in treating neurodegenerative diseases as well as cerebrovascular disorder-induced neuronopathy. More specifically, the present invention provides a novel compound of the following Formula (I) or a salt or prodrug thereof: [wherein R1 and R2 each represent a hydrogen atom or a lower alkyl group, etc., Ar1 and the ring B each represent an optionally substituted aromatic group, the ring A represents an optionally substituted benzene ring, the ring C represents an optionally substituted 4- to 8-membered ring which may further be condensed with an optionally substituted ring, X represents CH or N, and Y represents CH or N].

Abstract: A compound having a general formula (II) wherein R1 is saturated or unsaturated alkyl, amino-alcohol, diamino, cycloalkyl, and C(?O)(CH2)nNR?R?, (CH2)nCHOHCH2NR?R?, wherein n is an integer, RQ, RT, R?, and R? are each independently a hydrogen, halogen, hydroxyl, saturated, unsaturated, aliphatic, or branched alkyl, substituted or unsubstituted (CH2)m-(hetero)aryl, and sulfonylamide; q and r are each an integer independently selected from 1-4; and pharmaceutically acceptable salts thereof, and the new therapeutic uses thereof and similar compounds as defibrillating, and/or anti-fibrillatory, and/or anti-arrhythmic and/or anti-ischemic drugs.

Abstract: A high-yielding method and a useful intermediate, 10-chloro-10,11-dihydro-5H-dibenz/b,f/azepine-5-carboxamide (VII) is disclosed. Also disclosed are methods for the racemisation of optically pure or optically enriched mixtures of (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (I) and (R)-(−)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (II) to racemic (±)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (III).

Abstract: Novel spirobenzoazepine compounds, novel processes for the preparation of nonpeptide substituted spirobenzoazepine derivatives, and novel processes for the preparation of intermediates in the preparation of such derivatives. Novel intermediates in the preparation of nonpeptide substituted spirobenzoazepine derivatives.

Abstract: The present invention provides compositions and methods for the treatment of central nervous system damage in a subject. More particularly, the invention provides a combination therapy for the treatment of a central nervous system ischemic condition or a central nervous system traumatic injury comprising the administration to a subject of a sodium ion channel blocker in combination with a cyclooxygenase-2 selective inhibitor.

Abstract: Cyclic and heterocyclic N-substituted &agr;-iminohydroxamic and -carboxylic acids Compounds of the formula I are suitable for preparing pharmaceuticals for the treatment of disorders in the course of which is involved an increased activity of matrix-degrading metalloproteinases.

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.