Abstract: This invention relates to 8?-vinyl-11?-(?-substituted)alkyl-estra-1,3,5(10)-trienes of general formula I with ER?-antagonistic activity, process for their production, their intermediate products, pharmaceutical preparations that contain the compounds according to the invention, as well as their use for the production of pharmaceutical agents. The new compounds can be used for contraception in men and women without influencing other estrogen-sensitive organs such as the uterus or the liver. They are also suitable for treating benign or malignant proliferative diseases of the ovary, such as ovarian cancer and granulosa cell tumors.

Abstract: The invention relates to malonamide derivatives of formula wherein each of the variables are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds are ?-secretase inhibitors. Thus, the invention also relates to pharmaceutical compositions containing these compounds and to a method of treating Alzheimer's disease by administering the compounds of the invention.

Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Abstract: Compounds of Formula (I) wherein R1, R3, R4, R5 and X are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared.

Abstract: Compounds are provided having the formula: wherein variables A1, A2, A3, A4, R1, R2, R3, R4, Q and L are as described herein. The subject compounds are useful for treatment of inflammatory and immune conditions and diseases. Compositions and methods of treatment using the subject compounds are also provided. For example, the subject methods are useful for treatment of inflammatory and immune disorders and disease such as multiple sclerosis, rheumatoid arthritis, psoriasis, and inflammatory bowel disease.

Abstract: An optically active (?)-7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido[2,3-d][1,3]oxazin-2-one of the formula (I) or salt thereof.

Abstract: A compound of formula 1? wherein: V is —CH2—, —NH—, or —O—; Ra and Rb are each independently hydrogen, C1-4-alkyl, or halogen-C1-4-alkyl, or Ra and Rb together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R1 and R1? are each independently hydrogen, C1-6-alkyl, C3-6-cycloalkyl, halogen-C1-6-alkyl, halogen-C3-6-cycloalkyl, or C1-6-alkylene-C3-6-cycloalkyl, or R1 and R1? together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R2, R2?, R2?, and R?? are each independently hydrogen, C1-6-alkyl, halogen-C1-6-alkylene, OH, HO—C1-6-alkylene, —O—C1-6-alkyl, C6-10-aryl, C6-10-aryl-C1-4-alkylene, C6-10-aryl-C1-6-alkylene-O, COOH, COOC1-6-alkyl, O—C1-6-alkylene-COOH, O—C1-6-alkylene-COOC1-6-alkyl, NHSO2—C1-6-alkyl, CN, NH2, NH—C1-6-alkyl, N(C1-6-alkyl)2, NO2, S—C1-6-alkyl, SO2—C1-6-alkyl, SO—C1-6-alkyl, O(CO)C1-6-alkyl, COC1-6-alkyl, NHCOC1-6-alkyl, or halogen; and n is 0, 1, or 2, or an optical isomer thereof, or

Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R1 is hydrogen; Y1 and Y2 independently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of X1 and X2 is selected from O, S or NR11 and the other is CH, wherein R11 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl.

Abstract: The invention relates to a combined pharmaceutical preparation comprising an opioid diarylmethyl piperazine compounds and a NSAID. Such a preparation in which the compounds are either given sequentially or simultaneously can be used for the treatment of pain diminishing the side-effects observed in conventional opioid treatments.

Abstract: The present invention provides compound represented by formula (I): where the structural variables are defined herein. The compounds function as sodium channel blockers and may be used to treat a variety of respiratory conditions.

Abstract: The invention relates to 2-substituted pyrimidines of the formula I in which the index n and the substituents R1 to R3 and L are as defined in the description and R4 corresponds to one of the formulae in which Ra, X and Rb are as defined in the description; and also to processes for preparing these compounds, to pesticidal compositions comprising these compounds and to their use as pesticides.

Abstract: The present invention resides in glycine substituted thieno[2,3-d]pyrimidine derivatives according to general formula I, or a pharmaceutically acceptable salt thereof, wherein X is O or H,H A is S, NH, N(R6), O or a bond; R1 is (1-4C)alkyl, (2-4C)alkenyl, phenyl or (2-5C)heteroaryl, the phenyl or heteroaryl ring optionally being substituted with one or more of the group of substituents: hydroxy, halogen, nitro, trifluoromethyl, cyano, amino or (1-4C)(di)alkylamino and R2 is H, (1-4C)alkyl, (1-4C)alkoxy(2-4C)alkyl or hydroxy(2-4C)alkyl; R3 and R4 can be independently selected from H and hydroxy(1-4C)alkyl; R5 is H or (1-4C)alkyl; R6 can be selected from the same groups as described for R1. The compounds of the invention have LH as well as FSH receptor activating activity and can be used in fertility regulating therapies.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain.

Abstract: Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance ?-MSH activity.

Abstract: The present invention provides a method of administering vitamin B6 related compounds for treatment of hypertriglyceridemia. Vitamin B6 related compounds include pyridoxal, pyridoxal-5?-phosphate, pyridoxamine, a 3-acylated analogue of pyridoxal, a 3-acylated analogue of pyridoxal-4,5-aminal, and mixtures thereof. Embodiments of the present invention also comprise co-administering a lipid lowering agent, such as a nicotinic acid, a fibrate, a HMG CoA reductase inhibitor, a cholesteryl ester transfer protein inhibitor, and combinations thereof.

Abstract: The present invention provides nitrogen-containing fused-ring derivatives represented by the following general formula, or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R1 represent H, an optionally substituted alkyl group, analkenyl group, etc.; R2 represent H, a halogen atom or an alkyl group; R3 and R4 represent H, OH, a halogen atom, an optionally substituted alkyl group, etc.; Y represents CH or N; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; G represents a group represented by the following general formula (G-1) or (G-2) (in which E1 represents H, F or OH; and E2 represents H, F, a methyl group, etc.

Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: There are provided novel 4(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is OH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N—R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxy-carbonyl group, or the like. The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid ? antagonistic activity and are useful for the treatment or prevention of side effects which are caused by ? receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.

Abstract: Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) where two of the neighboring R1, R2, R3 and R4 groups form an imidazole ring fused to the benzene ring of the indole nucleus, and the other two of R1, R2, R3 and R4 groups are hydrogen atoms, R5 and R6 together with the nitrogen between them form a saturated or unsaturated, 4-6 membered heterocyclic ring, which is substituted by phenoxy, phenyl-(C1-C4 alkyl), phenyl-(C1-C4 alkoxy), phenoxy-(C1-C4 alkyl), or benzoyl, optionally substituted on the aromatic ring by one or more halogen atoms, cyano or hydroxy groups, C1-C4 alkyl or C1-C4 alkoxy groups, X is NH—, Y is a —CH— group, or pharmaceutically acceptable salts thereof formed with acids or bases.

Abstract: The present invention relates to polypeptides, and nucleic acids DNA encoding these polypeptides, capable of eliciting an immune reaction against cancer, methods for generating T lymphocytes capable of recognizing and destroying tumor cells, and pharmaceutical compositions for the treatment, prophylaxis or diagnosis of cancer.

Abstract: The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to phenyl-indole molecules that are cellular proliferation inhibitors and thus are useful as anticancer agents. This invention further relates to small molecules which suppress cytokines and leukocytes.

Abstract: The present invention provides an amide-type carboxamide derivative of the formula [1]: wherein X is a group of the formula: —N? or the formula: —CH?; R1 is a halogen atom, a lower alkyl group, and the like; R2 is a group of the formula: and the like; Y1 and Y2 are the same or different and each is a group selected from a halogen atom, a lower alkyl group, a lower alkoxy group, and the like; Ring A is phenyl group, and the like, or a pharmaceutically acceptable salt thereof, which is useful as an inhibitor of FXa.

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

Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.

Abstract: Compounds useful to control pests are provided.

Abstract: The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

Abstract: The use is described of derivatives of ?-phenylthiocarboxylic and ?-phenyloxycarboxylic acids with formula (i): in which the substituents have the meanings described in the text, for the preparation of a medicine for the prophylaxis and treatment of diabetes, particularly type 2 diabetes, its complications, the various forms of insulin resistance, and hyperlipidaemias

Abstract: Provided are MC4-R binding compounds of the formula XVII: wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, Z5, t, s, and R are as described in the specification. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also provided.

Abstract: The present invention discloses novel compounds of general formula (I) or a pharmaceutically acceptable salt or prodrug thereof (in which X1-X5, R5-R8b, Z1-Z2 and Ar1 are defined herein), a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain in mammals, and pharmaceutical compositions including those compounds and a process for making those compounds.

Abstract: The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.

Abstract: The present invention relates to a compound of formula (I): wherein R is hydrogen atom, hydroxyl group or carbamoyl group, and n is 1 or 2, or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of Formula I, commonly referred to as bis-indole pyrroles, including isolated naturally-occurring compounds, synthetic and semi-synthetic derivatives thereof having antimicrobial properties and to antimicrobial compositions that include one or more of bis-indole pyrroles and their derivatives or analogs having antimicrobial properties are disclosed. Pharmaceutical compositions comprising such compounds and methods of treating bacterial infections with the disclosed compounds or the disclosed pharmaceutical compositions are also disclosed.

Abstract: The invention relates to compounds of the general formula (I) below: in which R1, R2, R3, R4, R5, R6 and X are as defined in claim 1. These compounds can be used in the treatment of pathologies associated with insulin resistance syndrome.

Abstract: The present invention provides novel compounds and methods for using them to treat diseases with aminothiophene inhibitors of IKK-? phosphorylation of I?B. In so doing these aminothiophene inhibitors block pathological activation of transcription factor NF-?B in which diseases excessive activation of NF-?B is implicated.

Abstract: Compounds and compositions of the following formula: and analogs and stereoisomers thereof (and pharmaceutically acceptable carriers). Additionally disclosed is a method of inhibiting hypoxia-inducible factor-1 function in a patient or sample thereof, comprising administering to the patient or sample an effective inhibiting amount of a compound or composition of the present invention.

Abstract: A method for inhibiting and/or ameliorating the occurrence of diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals in a subject whereby a subject is administered a carotenoid analog or derivative, either alone or in combination with another carotenoid analog or derivative, or co-antioxidant formulation. The analog or derivative is administered such that the subject's risk of experiencing diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals may be thereby reduced. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of any disease that involves production of reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals. In some embodiments, the invention may include a pharmaceutical composition including a carotenoid analog or derivative. The carotenoid analog may include a conjugated polyene with between 7 to 14 double bonds.

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: The invention concerns novel molecules, their preparation and their uses, in particular in the field of human and veterinary medicine and cosmetics. The inventive compounds are partly fatty acid derivatives and exhibit advantageous pharmacological and cosmetic properties. The invention also concerns various uses of said compounds, the pharmaceutical compositions containing them and methods for preparing them. The inventive compounds are useful in particular for preventing and/or treating dyslipidemiae, cardiovascular diseases, syndrome X, restenosis, diabetes, obesity, hypertension, certain cancers, dermatological diseases and in cosmetics, for fighting against skin aging and its effects notably against wrinkles and the like.

Abstract: NMDA receptor blockers, including pH-sensitive NMDA receptor blockers, are provided as neuroprotective drugs that are useful in stroke, traumatic brain injury, epilepsy, and other neurologic events that involve acidification of brain or spinal cord tissue. Compositions and methods of this invention are used for treating neurodegeneration resulting from NMDA receptor activation. The compounds described herein have enhanced activity in brain tissue having lower-than normal pH due to pathological conditions such as hypoxia resulting from stroke, traumatic brain injury, global ischemia that may occur during cardiac surgery, hypoxia that may occur following cessation of breathing, pre-eclampsia, spinal cord trauma, epilepsy, chronic pain, vascular dementia and glioma tumors.

Abstract: The present invention provides methods of treating cancers, chemoprevention, selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

Abstract: Pentafluorosulfanylbenzoylguanidines of the formula I and II in which R1 to R4 have the meanings stated in the claims, are suitable as antiarrhythmic medicaments with a cardioprotective component for the prophylaxis of infarction and treatment of infarction and for the treatment of angina pectoris. They also inhibit preventively the pathophysiological processes associated with the development of ischemia-induced damage, especially in the triggering of ischemia-induced cardiac arrhythmias.

Abstract: A transdermal patch for the treatment of iron deficiency including a drug reservoir layer containing an hematinic substance; a rate-controlling membrane secured to said reservoir layer; and a contact adhesive secured to said rate-controlling membrane, wherein said hematinic substance is selected from the class consisting of ferrous sulfate, ferrous lactate, ferrous iodide, ferrous gluconate, ferrous fumarate, ferrous citrate, ferrous carbonate saccharated, ferrous carbonate mass, ferronascin, ferroglycine sulfate, and ferrocholinate.

Abstract: A process and apparatus for rapidly producing an emulsion and microcapsules in a simple manner is provided wherein a dispersion phase is ejected from a dispersion phase-feeding port toward a continuous phase flowing in a microchannel in such a manner that flows of the dispersion phase and the continuous phase cross each other, thereby obtaining microdroplets, formed by the shear force of the continuous phase, having a size smaller than the width of the channel for feeding the dispersion phase.

Abstract: The invention concerns a gum carob with average mole weight (Mw) ranging between 2.5.105 and 1.5.106 g/mol and whereof at least 60 wt. % of said gum is soluble in an aqueous medium at a temperature not higher than 60° C.

Abstract: A carbonaceous feedstock to alcohol conversion process in which carbon dioxide and a portion of the hydrogen produced are removed from the syngas stream issuing from a feedstock reformer, to yield a reduced hydrogen, carbon monoxide and methane syngas stream. The hydrogen and the carbon dioxide are passed through a Fischer Tropsch reactor which is catalyzed to favor the production of methanol. The methanol produced in the Fischer-Tropsch reactor is passed with the reduced hydrogen syngas through a second Fischer-Tropsch reactor which is catalyzed to favor the production of ethanol. Also disclosed, without limitation, are a unique catalyst, a method for controlling the content of the syngas formed in the feedstock reformer, and a feedstock handling system.

Abstract: Embodiments of the invention relate to processes and apparatus for the washing and recovery of metal-containing catalyst solids in a form suitable for reclamation. More specifically, a catalyst recovery process comprises removing an organic residue with a washing medium from a metal-containing catalyst solids, recovering washed solids, and treating the washed solids under oxidative conditions to form non-reactive solids. The treatment oxidative conditions may be effective to convert the metal(s) into an oxide form and/or may facilitate the removal of remaining organic residue from the washed solids. The treatment of the washed solids may comprise calcination. In some embodiments, the metal-containing catalyst solids may be recovered from a slurry stream, and the process further comprises passing the slurry stream though a separation unit to obtain a catalyst-enriched retentate slurry.

Abstract: Disclosed are radiation-curable, abrasion resistant coating compositions for thermoplastic substrates which provides superior abrasion, chemical, and impact resistance properties. The coating composition includes at least one flexible diacrylate component, at least one aromatic diacrylate component, and at least one urethane acrylate. Also disclosed are shaped articles having the coating composition applied to at least one surface and cured by exposure to radiation.

Abstract: There is provided an inkjet ink comprising a photo-acid generating agent which is capable of generating an acid as it is irradiated with light, a color component, and an acid-polymerizable compound which can be polymerized in the presence of an acid, wherein at least 40% of the acid-polymerizable solvent is a vinyl ether compound represented by the following general formula (1): R13—R14—(R13)p ??(1) (Wherein R13(s) is a group selected from the group consisting of a vinyl ether group, a group having a vinyl ether skeleton, an alkoxy group, substituted hydroxyl group and hydroxyl group wherein at least one of R13(s) is vinyl ether group or a group having a vinyl ether skeleton, R14 is a group comprising a substituted or unsubstituted cyclic skeleton and having a valence of (p+1), and p is a positive integer including zero).

Abstract: An extrudable PVA-containing composition is disclosed, which enables PVA articles to be manufactured on conventional extrusion apparatus. The composition includes a lubricant, such as a fatty acid amide, and is formed into pellets by cold pressing. The compositions are suitable for manufacturing a variety of products.

Abstract: Ink jet recording method and apparatus is provided in which a color image is recorded by discharging, onto a recording medium, a black ink and at least one of a cyan ink, a magenta ink and a yellow ink from a black-ink recording head that ejects the black ink onto the recording medium, and a color-ink recording head that ejects the at least one of a cyan ink, a magenta ink and a yellow ink onto the recording medium, wherein the black ink contains carbon black, water, a water-soluble organic solvent, and a water-soluble polymer having an anionic functional group, and has a drying time of 5 seconds or more on the recording medium, and at least one type of the color ink contains a color material, water, a water-soluble organic solvent, and a coagulating agent, and has a drying time of 5 seconds or less on the recording medium.