Abstract: Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.

Abstract: The present invention relates to antimnemonic therapy for the treatment of behaviroal disorders such as addiction, obsessive-compulsive disorder, Tourette's Syndrome, post-traumatic stress disorder (PTSD), bipolar disorder, depression, schizophrenia, anxiety disorders and personality disorders. Antimnemonic therapy may involve cue- or psychotherapy-induced reactivation of memories in combination with the administration of antimnemonic drugs.

Abstract: Compounds having the formula 1

Abstract: A pharmaceutical combination preparation for the treatment of cardiac and cardiovascular disorders, such as hypertension, angina pectoris, cardiac insufficiency and illnesses associated therewith, contains the active substances carvedilol, or a pharmaceutically acceptable salt thereof, and hydrochlorothiazide, or a pharmaceutically acceptable salt thereof, as well as pharmaceutically usual additives.

Abstract: Tumor growth and metastases in cancer patients are inhibited by administration of a combination therapy including effective amounts of 5-Fluorouracil and a methylol transfer agent such as taurolidine, taurultam or mixtures thereof.

Abstract: The present invention relates to new 4-hydroxy-2H-thieno[2,3-e]-1,2-thiazine-3-carboxamide-1,1-dioxides of general formula 1

Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1

Abstract: Novel compounds of the formula I in which W, X, Y, T, R1 and R2 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.

Abstract: This invention relates generally to amino-thio-acrylonitriles of formula Ia or Ib: 1

Abstract: PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs.

Abstract: Nobel PDF inhibitors and novel methods for their use are provided.

Abstract: The present invention provides 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of cancers, namely breast cancer. This invention further provides a method of synthesis of 2-(alkylthio)isoflavones that can be carried out at ambient conditions. This invention further provides a method of synthesis of the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one from a 2-(alkylthio)isoflavone. The invention further provides methods of using the 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of breast cancer in mammals.

Abstract: The present invention relates to substituted xanthines of general formula 1

Abstract: The present invention provides compounds comprising a bicyclic aryl moiety, such as 2H-phthalazin-1-one or derivatives thereof, compositions comprising the same, and methods for producing and using the same.

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: Novel biphenyl and biphenyl-like cannabinoid compounds are presented. These compounds, when administered in a therapeutically effective amount to an individual or animal, result in a sufficiently high level of that compound in the individual or animal to cause a physiological response. The physiological response useful to treat a number of physiological conditions.

Abstract: The invention describes novel compositions containing at least one phosphodiesterase inhibitor, and at least one compound that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.

Abstract: Disclosed is a method of treating Malaria comprising administering an effective amount of an FPT inhibitor to a patient in need of such treatment alone or in combination with an additional antimalarial agent and/or agent for reversing antimalarial resistance.

Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: 1

Abstract: Disclosed are novel diaminothiazoles that are selective inhibitors of Cdk4. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds as well as intermediates useful in the preparation of the compounds.

Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.

Abstract: The efficacy of levodopa therapy in patients being treated for Parkinson's disease is enhanced by administering high doses of a partial glycine agonist. The frequency and severity of levodopa-induced side effects in Parkinson's disease patients are also reduced by administration of a partial glycine agonist.

Abstract: The present invention relates to the pharmaceutical useful for the prevention and the treatment of diabetic complications such as diabetic nephropathy, diabetic neuropathy, diabetic retinopathy and diabetic angiopathy among others, and to the prophylaxis and/or treatment drug for diabetic complications with the compound shown in the formula (1) 1

Abstract: The invention relates to pyrimidone derivative represented by formula (I) or a salt thereof wherein X represents hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group, a 1,2-cyclopropylene, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxyde group, a carbonyl group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; R1 represent a 2,3 or 4-pyridyl group optionally substituted by a C3-6cycloalkyl group a C1-4alkyl group, a C1-4alkoxy group, a benzyl group or a halogen atom; when Y represents a bond, a methylene group optionally substituted or a carbonyl group then R2 represent a C1-16alkyl group, a C3-6cycloalkyl group, a C1-4alkylthio group, a C1-4alkoxy group, a C1-2perhalogenated alkyl group, a C1-3halogenated alkyl group, a 5,6,7,8-tetrahydronaphthyl ring, a naphthyl ring, a phenylthio group, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrol

Abstract: Pyrazolopyrimidine compounds which are selective inhibitors of cGMP PDE are useful in the treatment of erectile dysfunction (impotence) in male animals, including man.

Abstract: Compounds of formula I 1

Abstract: Compounds containing the pyrimidine nucleus and their use to treat diseases and conditions related to inappropriate Interleukin-8 receptor activity are disclosed.

Abstract: There is disclosed the use of metal-oxides pigments as photodegradation stabilizers in topical compositions containing brivudine.

Abstract: The present invention provides a novel amino acid of the formula: 1

Abstract: The present invention provides a compound of the formula (I): 1

Abstract: The present invention provides compound having the structure: and pharmaceutically acceptable salts or derivatives thereof, as well as compositions including such compounds. The invention also provides methods of (1) preventing pain, (2) treating pain, (3) inducing sedation, (4) treating opiate addiction, (5) treating opiate withdrawal (abstinence syndrome) and/or (6) treating cough in a patient in need thereof by administering a compound or composition of the invention.

Abstract: Active cooling of a person, such as to induce mild/moderate hypothermia, is accomplished by transferring heat from the persons body. Heat transfer and patient comfort are aided by administration of an anti-shivering drug and an anti-emetic drug.

Abstract: The present invention provides a method for increasing analgesic potency of a bimodally-acting opioid agonist in a subject, by inhibiting GM1-ganglioside in nociceptive neurons. The present invention further provides a method for treating pain in a subject in need of treatment thereof. Also provided in the present invention is a method for treating chronic pain in a subject in need of treatment thereof. Additionally, the present invention provides a method for treating tolerance to or an addiction to a bimodally-acting opioid agonist in a subject in need of treatment thereof. Finally, the present invention provides a pharmaceutical composition of analgesic agents and a pharmaceutically-acceptable carrier.

Abstract: This invention relates to pharmaceuticals for neuropathic pains comprising an mGluR1 receptor antagonist for systemic administration. Drugs efficacious in treating various neuropathic pain can be provided by the invention.

Abstract: Problem: A large scale production of camptothecin, which is a starting compound of irinotecan hydrochloride and various camptothecin derivatives, at a low cost and with ease.

Abstract: We have surprisingly discovered that the administration of a G1 and/or S phase drug such as &bgr;-lapachone in combination with a G2/M drug such as a taxane derivative such as paclitaxel resulted in an unexpected greater than additive (i.e., synergistic) reduction in the number of tumors (and tumor volume) as compared with the administration of these agents alone. In addition, no signs of toxicity or weight loss were observed. The present invention relates to a method for treating a mammalian tumor using combinations such as a taxane derivative, preferably paclitaxel, and a &bgr;-lapachone, or a derivative or analog thereof.

Abstract: Methods and composition are provided for treating cancer, the methods including the step a administering, either sequentially or simultaneously, (i) a compound of the xanthenone acetic acid group of compounds, and (ii) at least one compound selected from compounds which modulate TNF production and compounds which act on biochemical pathways leading to TNF synthesis. Compositions include a combination of (i) and (ii) above, together with acceptable pharmaceutical carriers and/or vehicles.

Abstract: A method is provided for increasing lacrimal gland tearing in a patient's eye. Specifically, tacrolimus in a pharmaceutically acceptable vehicle is topically administered to the patient's eye.

Abstract: A method is provided for preventing or reducing the formation of adhesions or scar tissue either from the result of a surgical procedure or due to other irritation, trauma or other type of disruption of the tissue, by applying rapamycin or its derivatives or variants to a tissue.

Abstract: The invention relates to a method and composition for treating aged or photo-damaged skin. In one embodiment, the invention includes using a composition comprising about 1% to about 2% of 1-isobutyl-1 H-imidazo [4,5,-C] quinolin-4-amine in a topical preparation or cream. In further embodiments, the method includes identifying topical compositions that can diagnose or identify precancerous region of the skin, as well as methods for treating aged or photo-damaged skin by applying a Toll-like receptor activator, such as 1 -isobutyl-1 H-imidazo [4,5,-C] quinolin-4-amine.

Abstract: The present invention relates to novel cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]triazolo-pyridines, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Abstract: The invention provides compounds of Formula I: 1

Abstract: The present invention relates to new anticholinergics of general formula 1 1

Abstract: An objective of the present invention is to provide an ectoparasite control agent for homothermic animals, which has high control effect and is safe.

Abstract: Quinolylpropylpiperidine derivatives of general formula (I) in which R1 is hydrogen or fluorine, R2 is carboxyl, carboxymethyl or hydroxymethyl, R3 is alkyl substituted either with phenylthio optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino, or with cycloalkylthio (3 to 7 members) optionally substituted with halogen or trifluoromethyl, or with heteroarylthio (5 to 6 members and 1 to 4 heteroatoms chosen from N, O and S), optionally substituted with halogen, hydroxyl, alkyl, alkyloxy, trifluoromethyl, trifluoromethoxy, carboxyl, alkyloxycarbonyl, cyano or amino or R3 is propargyl substituted by phenyl or heteroaryl as defined above and R4 is alkyl, alkenyl-CH2— or alkynyl-CH2—, cycloalkyl or cycloalkylalkyl, in their various isomeric forms, separate or as mixtures, and also their salts, their preparation process and intermediates and the compositions containing them.

Abstract: The present invention provides a compound of the formula (I): 1

Abstract: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more substituents selected from halogen, cyano, nitro, and C1-C8-alkyl optionally substituted by cyano or halogen, Ar2 is phenyl optionally which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R1 is C1-C8-alkyl substituted by hydroxy, C1-C8-alkoxy, acyloxy, —N(R2)R3, halogen, carboxy, C1-C8-alkoxycarbonyl, phenyl-C1-C8-alkoxycarbonyl, -CON(R4)R5 or by a monovalent cyclic organic group, R2 and R?3 are each independently hydrogen or C1-C8-alkyl, or R2 is hydrogen and R3 is acyl or SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen, C1-C8-alkyl optionally substituted by hydroxy or phenyl, or phenyl optionally substituted by C1-C8-alkyl, halogen, cyano or C1-C8-alkoxy, or R4

Abstract: A novel benzamide derivative represented by the following general formula: 1

Abstract: Therapeutically active pyrazole derivatives of formula (I) wherein R1-R3 are as defined in the specification, processes for the preparation thereof, the use thereof in therapy, particularly in the treatment or prophylaxis of disorders characterised by overexpression of transforming growth factor &bgr; (TGF-&bgr;), and pharmaceutical compositions for use in such therapy, Formula (I) 1

Abstract: Compounds of formula (I) 1