Abstract: Benzimidazole and indole derivatives that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided.

Abstract: The present invention relates to compounds of formula I, 1

Abstract: TNF-&agr; inhibitors containing a heterocyclic compound having angiotensin II antagonistic activity which are useful as preventives/remedies for inflammatory diseases, etc.

Abstract: The present invention provides novel methods of treating disorders of attention or improving attention in humans by administering an effective amount of a cholinesterase inhibitor.

Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.

Abstract: The present invention is a compound of formula 1

Abstract: The invention provides compounds of Formula I: 1

Abstract: This invention provides novel pyrazole compounds that are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3. The compounds may be used to treat abnormal physiological function leading to diseases such as cancer, diabetes and Alzheimer's disease.

Abstract: Compounds of general formula (I) 1

Abstract: The present invention provides novel tricyclic pyridyl carboxamides as well as methods and pharmaceutical compositions utilizing them compounds for the treatment and/or prevention and/or suppression of disorders which may be remedied or alleviated by oxytocin antagonist activity, including prevention and/or suppression of preterm labor, suppression of labor at term prior to caesarean delivery, and for the treatment of dysmenorrhea. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

Abstract: This invention provides novel substituted tricyclic pyridyl carboxamides which act as oxytocin receptor competitive antagonists, as well as methods of their manufacture, pharmaceutical compositions and methods of their use in treatment, inhibition, suppression or prevention of preterm labor, dysmenorrhea, endometritis, suppression of labor at term prior to caesarean delivery, and to facilitate antinatal transport to a medical facility. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

Abstract: The present invention relates to compositions comprising S-tofisopam substantially free of R-tofisopam, and methods for treating or preventing convulsions and/or seizures comprising administration of the composition to subjects in need of treatment therefor. Also provided are compositions and methods for treating or preventing convulsions and/or seizures comprising administering S-tofisopam substantially free of R-tofisopam with another anti-convulsant.

Abstract: The invention relates to compounds of the formula 1 1

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.

Abstract: The present invention provides an ophthalmic aqueous pharmaceutical preparation, which is excellent in anti-inflammatory effect, which is less stimulative and which has high safety and excellent storage stability. The ophthalmic aqueous pharmaceutical preparation comprises meloxicam and trometamol.

Abstract: The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP&agr;), said prodrug having a cleavage site which is recognised by FAP&agr;, and said drug being cytotoxic or cytostatic under physiological conditions.

Abstract: The present invention relates to compounds of the formula 1 1

Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.

Abstract: The present invention relates to novel benzimidazole derivatives, pharmaceutical composition containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABA receptor complex, and in particular for inducing and maintaining anesthesia, sedation and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.

Abstract: The present invention discloses new and useful compounds including methyl p-hydroxyphenyllactate, its analogues, chemical derivatives and chemically related compounds and their use as antitumor and immune suppressive agents, as inhibitors of proliferative cell growth and as prophylactic agents to inhibit and prevent cancer and non-malignant cell growth.

Abstract: The invention relates to novel benzimidazole derivatives with general formula I, whereby radicals R1, R2, R3, A, B and Y have the meanings that are indicated in the description and the claims, the use of these compounds for the production of a pharmaceutical agent for treating and for preventing diseases that are associated with microglia activation, as well as pharmaceutical preparations that contain these compounds.

Abstract: This invention relates to pharmaceutical compositions and methods of treatment utilizing a PTPase (protein-tyrosine phosphatase) inhibitors and an angiotensin converting enzyme (ACE) inhibitor to lower the risk of cardiovascular disease and cardiovascular events in a mammal experiencing or subject to type II diabetes in mammals experiencing or subject to type II diabetes (non-insulin-dependent diabetes mellitus), preferably in human type II diabetics, or Syndrome X.

Abstract: The present invention describes novel imidazo-pyridines, -pyridazines, and -triazines of formula I: 1

Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by a (cyano)(fluoro)phenyl moiety, being selective ligands for GABAA receptors, in particular having good affinity for the &agr;2 and/or &agr;3 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety and convulsions.

Abstract: Substituted pyrido[1,2-a]pyrazines of general formula I; wherein Ar and Ar1 represent various carbocyclic and heterocyclic aromatic rings; A represents O, S, SO, SO2, CHOH, C═O, or —(CR3R4); and n is 0-2, as well as precursors thereto, are ligands for dopamine receptor subtypes and serotonin (5HT) within the body and are therefore useful in the treatment of disorders of the dopamine and serotonin systems: 1

Abstract: The present invention relates to compounds represented by the structural Formula I: 1

Abstract: The R-stereoisomer of 6-hydroxy-buspirone is an effective treatment for anxiety, depression, and other psychogenic disorders. The R-isomer exhibits greater receptor specificity than the S-isomer and should have reduced potential for the adverse effects associated with the racemic mixture and with buspirone.

Abstract: The present invention relates to a piperazine compound of the formula 1

Abstract: A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.

Abstract: The invention disclosed some 1,4-dihydropiridine derivative chemically have pharmacologically with adrenoceptor blocking and calcium channel blocker is now emerging.

Abstract: A liquid suspension comprising an antifungally effective amount of the micronized compound represented by the chemical structural formula I: 1

Abstract: This invention describes novel pyrazole compounds of formula IIc: 1

Abstract: The novel compounds of formula I: 1

Abstract: This invention is directed to the use phosphodiesterase type 5 (PDE5) inhibitors in the treatment of selective serotonin reuptake inhibitor (SSRI) induced sexual dysfunction. Specifically, this invention is directed to a method for treating an animal to cure; prevent or ameliorate SSRI induced sexual dysfunction which comprises administering to the animal an effective amount of the inhibitor. The animal may be a male or a female human. The invention also includes the use of such inhibitors in the manufacture of a medicament to prevent; cure or ameliorate SSRI induced sexual dysfunction. Moreover, the invention includes a kit comprising a SSRI, such as sertraline, fluoxetine, paroxetine, and a PDE5 inhibitor, such as sildenafil citrate, for the treatment or prevention of serotonergic associated disorders such as depression, obsessive compulsive disorder or panic disorder, while reducing or preventing sexual dysfunction.

Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: This invention provides a method for treating a Pin1-associated state in a subject including administering to a subject an effective amount of a fredericamycin A compound such that the Pin1-associated state is treated. In another aspect, this invention includes the above described method, wherein the Pin1-associated state is a cyclin D1 elevated state, neoplastic transformation, and/or tumor growth. In an embodiment, this invention provides the above described methods, wherein the Pin1-associated state is colon cancer, breast cancer, a sarcoma, a malignant lymphoma, and/or esophageal cancer. This invention also provides a method for treating cyclin D1 overexpression in a subject including administering to a subject an effective amount of a combination of a fredericamycin A compound and a hyperplastic inhibitory agent such that the cyclin D1 overexpression is treated.

Abstract: It was found that an inducible nitric oxygen synthase (i-NOS) inhibitor is effective for Sjögren's syndrome, and based on this knowledge, an agent for treating and/or preventing Sjögren's syndrome comprising the i-NOS inhibitor as an active ingredient has been completed.

Abstract: The present invention relates to a hydrohalogenide of 1′-[4-[1-(4-fluorophenyl)-1H-indole-3-yl]-1-butyl]-spiro[isobenzofuran-1(3H),4′-piperidine], pharmaceutical compositions containing the acid addition salts and the use thereof for the treatment of psychic and neurological disorders.

Abstract: Controlled release formulations of drugs such as fentanyl and sufentanil are disclosed. The formulations are comprised of two or more different groups of particles wherein the particles of a given group are substantially identical but are different from the particles in any other group. The combined effect of the groups provides steady state blood levels which are particularly useful when administering opioids compound such as fentanyl by injection. A method of reducing unwanted diversion of narcotics is also disclosed.

Abstract: Novel compounds of the general formula (I), the use of these compounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPAR&ggr; response in a partial agonist manner.

Abstract: Prostaglandin D2 receptor antagonists in conjunction with an antihistamine and/or a leukotriene antagonist are useful in the treatment of allergic conditions.

Abstract: The use of phanquinone (4,7-phenanthroline-5,6-dione) for the treatment or prevention of memory impairment is suggested. Also a method for improving the learning or memory of a normal subject is suggested, said method comprising the administering of phanquinone, optionally together with one or more pharmaceutically acceptable carrier(s).

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: A compound according to formula (I) 1

Abstract: The present invention provides compounds of formula (I): wherein W represents hydrogen, C1-C4 alkyl, —CH2CO2H, or CO2H; and X represents hydrogen, C1-C4 alkyl, —CH2CO2H, or CO2H; with the proviso that at least one of W or X must be other than hydrogen; or a prodrug or a pharmaceutically acceptable salt thereof; which are useful for treating migraine.

Abstract: Polymorphs Form B, Form C, and amorphous of 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone, commonly known as cilostazol, have been identified. These polymorphs may be formed in pure form, in combination with each other, in combination with other polymorphs of cilostazol, or together with other pharmaceutical agents. Processes for preparing these polymorphs, and combinations of these polymorphs, as well as methods of use and unit dosages of these polymorphic forms, and their combinations, are described.

Abstract: The present invention relates to a method of providing an antihistaminic effect in a hepatically impaired patient in need thereof comprising administering to said patient an effective antihistaminic amount of a compound of the formula 1

Abstract: The present invention provides substituted benzofuran, indene, thianaphthene and oxidized thianaphthene compounds and methods of treatment and pharmaceutical compositions that comprise such compounds. Preferred compounds of the invention contain benzofuran, indene or thianaphthene group substituted with a tetrahydrofuran or other alicyclic group.

Abstract: The present invention provides compounds and pharmaceutical compositions that act as antagonists at metabotropic glutamate receptors, and that are useful for treating neurological diseases and disorders. Methods of preparing the compounds also are disclosed.

Abstract: Compounds of formula (I): 1