Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.

Abstract: This invention describes novel protein kinase inhibitors of formula VII: 1

Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: 1

Abstract: Compounds and methods for promoting smoking cessation. The compounds may be used to treat a variety of other conditions and disease states.

Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I and salts thereof, where A=oxygen or sulfur; X1=H, halogen, C1-C4-alkyl; X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl; X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl; R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl, or R1+R2 together with the atom to which they are attached form 3- to 7-membered heterocyclic ring; Q is selected from Q1 to Q40 as defined in the description. Use: As herbicides; for the desiccation/defoliation of plants.

Abstract: There are described cycloalkyl derivatives of the formula (I)

Abstract: This invention provides a method of treating a disease state in mammals that is alleviated by treatment with a protein kinase inhibitor, especially an ERK inhibitor, which method comprises administering a compound having the pharmacophoric features Grp1, Grp2 and Grp3: 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. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein n, m, A, B, C, R, R1, R2 and Ar are as defined herein.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: Disclosed is sun screen formulation, comprising (a) a micronised organic UV absorber, and (b) a cosmetically acceptable carrier, wherein the micronised organic UV absorber is present in the oil phase of the formulation. The sunscreen composition of the invention provides excellent protection of the human skin against the damaging effects of sunlight, while permitting safe tanning of the skin.

Abstract: A method for treating menopausal hot flushes using CGRP antagonists and/or CGRP release inhibitors and the corresponding pharmaceutical compositions containing as active substance one or more CGRP antagonists and/or CGRP release inhibitors, and the preparation thereof.

Abstract: Substituted Polycyclic Aryl and Heteroaryl tetiary-leteroalkylamines Useful for Inhibiting Cholesteryl Ester Transfer Protein Activity Abstract The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.

Abstract: The present invention relates to compounds of the formula (I): wherein R1a, R1b, R2, R3, R4, R5, X and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.

Abstract: The invention relates to new s-triazine derivatives of the formula (I): in which R1 represents an —NH—F radical, wherein F is a screening chromophore; R2 represents an —NH—Z—W radical, wherein Z is a divalent radical providing the connection between —NH— and —W, and W is a silicone-containing radical; and R3 is R1, R2, a linear or branched C1-C20 alkyl radical, a linear or branched C2-C20 hydroxyalkyl radical, a linear or branched C1-C20 alkoxy radical, an NHR8 radical or an N(R8)2 radical, with R8 being a linear or branched C1-C20 alkyl radical. The compounds of the invention are useful as organic sunscreen agents in cosmetic compositions intended for the protection of the skin and the hair against ultraviolet radiation. The invention also relates to the use of the compounds in cosmetic applications and to cosmetic compositions with improved properties containing these compounds.

Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

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. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein n, m, A, B, C, R, R1, R2 and Ar are as defined herein.

Abstract: A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, cancer of uterine cervix, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, pplycystic ovary syndrome and acne vulgaris; is effective as a fertility controlling agent in both sexes (e.g.

Abstract: A composition comprising at least one 1,3,5-triazine derivative and at least one N-acyl amino acid ester and its use in or for the manufacture of compositions, especially cosmetic and dermatological compositions for protecting the skin and/or the lips and/or integuments against ultraviolet radiation, in particular solar radiation. In addition, a cosmetic treatment process comprising the application of the cosmetic composition, and the use of the at least one N-acyl amino acid ester, in anti-sun compositions containing a 1,3,5-triazine derivative to improve the sun protection factor of the composition.

Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): (wherein R is a C2-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group or the like, B0 to B2 and B3 are hydrogen atoms, halogen atoms, cyano groups, C1-C4 haloalkyl groups or the like, n is 0, 1 or 2, and Ar is a phenyl ring, a pyridine ring, a thiophene ring, a pyrazole ring or the like), and insecticides and miticides containing the 3-arylphenyl sulfide derivatives as an active ingredient.

Abstract: The present invention relates to cancer therapies using novel anticancer agents with a specific mechanism of action. The invention also relates to novel chemical compounds and their therapeutic application in man.

Abstract: The present invention relates to 4-aryl triazoles having the formula: 1

Abstract: Compound of the formula I, II, III or IV 1

Abstract: This invention is related to substituted 2-aminoacetamides represented by Formula II: or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1, R2, R3 and R4 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R5, R6 and R7 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R5, is defined as above, and R6 and R7 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR8, CH2, C(O), NR8C(O), C(O)NR8, SO, SO2 or a covalent bond; where R8 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or

Abstract: Phthalazine compounds having formula I wherein , A, B, R, R1, R2 and R3 are as defined herein, useful as phosphodiesterase 4 inhibitors.

Abstract: The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The, invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, formula (I).

Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formula: wherein Z1, Z2, R1, R2, R3, R4, R5, R6, and R7 are defined herein. These compounds are useful as anti-coagulants.

Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Abstract: The present invention relates to cosmetic compositions that comprise: a) a safe and effective amount of a functional aromatic derivative bonding agent having a structure selected from the group consisting of wherein X is one or more cosmetic benefit agents that may or may not be attached to a chemical linker; Y, Z, and W are selected from the group consisting of H, NO2, CN, CF3, SO2R, COR, and X; V is selected from the group consisting of F, I, Br, Cl, NO2, SOPh, N3, Oar, OSO2R, OR, SR, and NH2; V″ and Y″ are selected from the group consisting of C, N, and combinations thereof; Z″ and W″ are selected from the group consisting of F, I, Br, Cl, H, SR, X, or combinations thereof; wherein R is an alkyl or phenyl; and b) a cosmetically acceptable carrier for the bonding agent wherein the composition is administered topically to mammalian proteinaceous substrates and wherein the bonding agent reacts with a protein contained in the substrate such that the bonding agent

Abstract: This invention relates to devices, kits, and methods for eliminating termite colonies.

Abstract: Selected novel urea compounds are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stoke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: Substituted condensation products of -benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of type I diabetes.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.

Abstract: This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases.

Abstract: Concentrates of various classical biocides in a polyester carrier resin when incorporated into a substrate resin, preferably a polyolefin such as polypropylene or polyethylene, provide the substrate polymer which biocidal activity with superior resistance to discoloration (yellowing) than when the biocide is directly incorporated into the substrate polymer as a powder at the same total concentration.

Abstract: A composition is provided that has been specially adapted for parenteral administration, e.g., intranasal, intramuscular, subcutaneous, transdernal or intraveneous administration, wherein the composition is comprised of at least one anti-protozoal drug in a therapeutically effective amount for the treatment or prevention of protozoan infections in man and in animals. In one embodiment, the anti-protozoal drug is a triazine-based anticoccidial agent, e.g., a triazinedione or triazinetrione such as diclazuril, toltrazuril, sulfonotoltrazuril or water-soluble sodium salts thereof. In a presently preferred embodiment, the triazine-based anticoccidial agent is sulfonototrazuril. Methods of treatment of protozoal infections in man and animals are also provided.

Abstract: This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

Abstract: The invention relates to a method for producing an organic compound of formula (I) and optionally its E/Z-isomers, E/Z-isomer mixtures and/or tautomers, each in free or salt form, R1 representing hydrogen or C1-C4 alkyl, R2 representing hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl or a radical —CH2B, Het representing an unsubstituted or substituted heterocyclic radical and B representing phenyl, 3-pyridyl or thiazolyl, these being optionally substituted. The invention is characterized in that a compound of formula (IIa) Q—A—Q, wherein A represents a direct bond or an organic radical, or of formula (IIb), wherein U represents an organic radical, Q representing (1) in the compounds (IIa) and (IIb) and R1, R2 and Het having the meaning given above for formula (I), and optionally their E/Z-isomers, E/Z-isomer mixtures and/or tautomers, each in free or salt form are hydrolyzed.

Abstract: Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having Ki's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an &agr;-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other &pgr;-unsaturation corresponding to the arachidonyl &Dgr;8.9/&Dgr;11.12 and/or oleyl &Dgr;9.10 positions. A preferred &agr;-keto heterocylic head group is &agr;-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).

Abstract: Provided herein are compounds of the formula (I): 1

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.

Abstract: This invention encompasses a method of treating or preventing urinary incontinence in a mammalian patient comprising administering to the patient a compound of formula I: 1

Abstract: The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.

Abstract: A Rho kinase inhibitor is provided as a novel pharmaceutical agent, particularly as a therapeutic agent of hypertension, a therapeutic agent of angina pectoris, a suppressive agent of cerebrovascular contraction, a therapeutic agent of asthma, a therapeutic agent of peripheral circulation disorder, a prophylactic agent of immature birth, a therapeutic agent of arteriosclerosis, an anti-cancer drug, an anti-inflammatory agent, an immunosuppressant, a therapeutic agent of autoimmune disease, an anti-AIDS drug, a contraceptive, a prophylactic agent of digestive tract infection, a therapeutic agent of osteoporosis, a therapeutic agent of retinopathy and a brain function improving drug. In addition, the Rho kinase inhibitor is provided as a reagent and a diagnostic.

Abstract: The present invention concerns novel water-soluble azole compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof; as antifungals; their processes for preparation, composition containing them and their use as a medicine.

Abstract: 8,8a-Dihydroindeno[1,2-d]thiazole derivatives which carry in the 2-position a substituent having a sulfonamide structure or sulfone structure; processes for their preparation and their use as medicaments The invention relates to polycyclic dihydrothiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.

Abstract: This invention is directed to 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives useful as &dgr;-opioid or &mgr;-opioid receptor modulators. Depending on their agonist or antagonist effect, the compounds are useful analgesics, immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.

Abstract: The present invention relates to orally administrable pastes of toltrazuril sulfone, comprising active compound in a concentration of 0.1-20% by weight, with a particle size of from 1 to 10·10−6 m, polyacrylic acids having a degree of polymerization of about 3·106 in a concentration of 0.1-5% by weight and, if appropriate, preservatives and moisturizers, and the remainder to 100% by weight water.

Abstract: The invention relates to novel pyridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.

Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,1-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.