Abstract: The invention relates to compounds of the formula (I) in which A1, A2, R1, R2, R3, R4, R5 and X are as defined in the description, to processes and intermediates for their preparation, and to their use for controlling pests.

Abstract: The invention provides 19-nor-D-homosteroids, having a mixed androgenic/progestagenic profile, which are orally active, prevent trabecular bone mineral density (BMD) loss, and which lack liver toxicity, having a structure according to the formula (I) wherein, R1 is O, or NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl, R2 is methyl or ethyl, and R3 is hydrogen or (C1-15)acyl.

Abstract: The present invention pertains to certain ketones and reduced ketones and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formulae: (1) (2) wherein: Ar1 is independently a biphenyl, phenanthryl, fluorenyl, or carbazolyl, and is optionally substituted; Ralk is independently a C2-10alkylene group, and is optionally substituted; —ORO, if present, is independently —OH or —ORK; —ORK, if present, is independently selected from: —O—RK1; —O—C(?O)RK2; —O—C(?O)ORK3; —O—S(?O)2ORK4; Q is independently —OH or —OROT; wherein: —OROT, if present, is independently selected from: —O—RE1; —O—C(?O)—RE2; —O—C(?O)—O—RE3; —O—C(?O)—O—SO3RE4; —O—C(?O)—O—(CH2)n—COORE5; —O—C(?O)—(CH2)n—NRN1RN2; —O—C(?O)—(CH2)n—NH—C(?O)RE6; —O—C(?O)—(CH2)n—C(?O)—NRN3RN4; —O—P(?O)(ORE7)(ORE8); —O—RPA; RPA, if present, is an organic group which incorporates a phosphonic acid group; with the proviso that if —OROT is —O—RE1, then RE1 is

Abstract: Compounds of formula wherein A0, A1 and A2 are each independently of the others a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge which is unsubstituted or substituted by from one to six identical or different substituents selected from halogen and C3-C8cycloalkyl; Y is, for example, O, S, SO or SO2; M is O or NOR6, X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylcarbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C2-C6alkynyl; Q is, for example, O, S, SO or SO2; W is, for example, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; D is CH or N; R4 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R5 is, for example, C1-C12alkyl, C3-C8cycloalkyl or —N(R7)2; R7 is H, C1-C6alkyl, C1-C3haloalkyl, C1-C6alkylcarbonyl, C1-C3haloalkylcarbonyl, C1-C6alkoxycarbonyl, C3-C8cycloalkyl, C3-C8 cycloalkyl

Abstract: A method of treating a subject for a serotonergic neurotransmission dysregulation disorder, comprises administering the subject a serotonin enhancer (e.g., a serotonin reuptake inhibitor) in an amount effective to treat the disorder; and concurrently administering the subject 5-hydroxytryptophan in an amount effective to enhance the activity of the serotonin enhancer, (e.g., serotonin reuptake inhibitor). In preferred embodiments the disorder is depression, anxiety, or substance abuse.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 2?,4?-dichloro-biphenyl-4-yl-hydroxy-ketones and related compounds (collectively referred to herein as “DCBP compounds”), and more particularly to compounds selected from compounds of the following formula and pharmaceutically acceptable salts, solvates, and hydrates thereof: wherein: n is independently 1, 2, 3, or 4; W is independently —C(?O)—, —CH(OH)—, or —C(?NOROX)—; ROX is independently —H or C1-3alkyl; J is independently: —H, —RE1, —C(?O)—RE2, —C(?O)—O—RE3, —C(?O)—O—S(?O)2ORE4, —C(?O)—(CH2)n—C(?O)ORE5, —C(?O)—(CH2)n—NRNE1RNE2, —C(?O)—(CH2)n—NRNE3—C(?O)RE6, —C(?O)—(CH2)n—C(?O)—NRNE4RNE5, or —P(?O)(ORE7)(ORE8); wherein each of RE1, RE2, RE3, RE4, RE5, RE6, and RE7 is independently: —H, C1-3alkyl, -Ph, or —CH2-Ph.

Abstract: This invention provides compounds which specifically inhibit TRPA1 but not other members of the thermoTRP ion channel family. Also provided in the invention are methods of using TRPA1-specific inhibitors to treat or alleviate pains mediated by noxious mechanosensation.

Abstract: Compounds of formula (I) wherein R1, R2, R3, m, and Y are defined in the specification are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

Abstract: A method for determining the appropriate medication for a patient suffering from depression. A patient will take a questionnaire wherein the patient answers a number of questions with scaled responses concerning the degree to which the patient's mental state is affected by at least one or both of impaired modulation and impaired activation. Next, the patient's answers will be processed to arrive at scores for the at least one impaired modulation and impaired activation. Depending upon the patient's scores for demodulation and deactivation, at least one medication which affects the at least one impaired modulation and impaired activation is recommended.

Abstract: The present invention is directed to compounds having the structure (I) wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals.

Abstract: A composition of matter that is suitable for use on skin or hair. The composition comprises one or more compounds of formula wherein Rx, Ry, R3 and R5 are as defined in the specification, and at least one other component or element.

Abstract: 2-cyclopenten-1-one oxime derivatives represented by Formula (I), or pharmaceutically acceptable salts thereof inhibit the production of TNF-? or PDE4, and therefore show therapeutic effect in inflammatory or immunological disorders mediated through TNF-? or PDE4.

Abstract: Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RAR? agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.

Abstract: The present patent application relates to 11?-benzaldoxime derivatives of D-homooestra-4,9-dien-3-ones of formula I: wherein R1 is a hydrogen atom or a C1-C6-alkyl, C1-C6-acyl, C1-C4-alkoxycarbonyl, C1-C4-alkylthiocarbonyl, C1-C6-alkylaminocarbonyl or arylaminocarbonyl group; and R2 is a hydrogen atom or a C1-C6-alkyl or C1-C6-acyl group. Compounds of formula I bind more strongly to the glucocorticoid receptor than to the progesterone receptor and are effective antiglucocorticoids. According to the invention, they are suitable for the treatment and/or prevention of symptoms and/or diseases that are attributable to an androgen deficiency induced by glucocorticoids, especially cortisol.

Abstract: The invention relates to compounds of formula (I): where X+Y=keto, or X=OH and Y=H, or X+Y=oxime or methyloxime, B=OH and C+D=H, or C+D=C1-C4 linear or branched alkyl, or C=H and D=C1-C4 linear or branched alkyl, or B+C=keto and D=methyl, hydroxyl, or methylamino, or B and C=H and D=methylamino, or B+C=oxime and D=methyl and R=C1-C10 linear or branched alkyl, the salts, esters, or salts of esters thereof as medicament, in particular as neuroprotectors, novel compounds of formula (I) and pharmaceutical compositions.

Abstract: A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a concentrated formulation of aztreonam lysinate delivered as an aerosol or dry powder formulation.

Abstract: The present invention relates to methods for treating diseases, conditions or disorders using hydroxyamine compounds, and in particular, N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl chloride (Compound I) alone or in combination with one or more other therapeutic agents for the treatment of conditions, disorders or diseases associated with neurodegeneration in the central nervous system. Additional therapeutic agents are provided. The present invention also relates to pharmaceutical compositions comprising hydroxyamine compounds, an additional therapeutic agent and a pharmaceutically acceptable carrier and methods for treating diseases using them.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 2?,4?-dichloro-biphenyl-4-yl-hydroxy-ketones and related compounds (collectively referred to herein as “DCBP compounds”), and more particularly to compounds selected from compounds of the following formula and pharmaceutically acceptable salts, solvates, and hydrates thereof: wherein: n is independently 1, 2, 3, or 4; W is independently —C(?O)—, —CH(OH)—, or —C(?NOROX)—; ROX is independently —H or C1-3alkyl; J is independently: —H, —RE1, —C(?O)—RE2, —C(?O)—O—RE3, —C(?O)—O—S(?O)2ORE4, —C(?O)—(CH2)n—C(?O)ORE5, —C(?O)—(CH2)n—NRNE1RNE2, —C(?O)—(CH2)n—NRNE3—C(?O)RE6, —C(?O)—(CH2)n—C(?O)—NRNE4RNE5, or —P(?O)(ORE7)(ORE8); wherein each of RE1, RE2, RE3, RE4, RE5, RE6, and RE7 is independently: —H, C1-3alkyl, -Ph, or —CH2-Ph.

Abstract: Compounds of formula wherein A0, A1 and A2 are each independently of the others a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge which is unsubstituted or substituted by from one to six identical or different substituents selected from halogen and C3-C8cycloalkyl; Y is, for example, O, S, SO or SO2; M is O or NOR6, X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylcarbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C2-C6alkynyl; Q is, for example, O, S, SO or SO2; W is, for example, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; D is CH or N; R4 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R5 is, for example, C1-C12alkyl, C3-C8cycloalkyl or —N(R7)2; R7 is H, C1-C6alkyl, C1-C3haloalkyl, C1-C6alkylcarbonyl, C1-C3haloalkylcarbonyl, C1-C6alkoxycarbonyl, C3-C8cycloalkyl, C3-C8 cycloalkyl

Abstract: Compositions and methods are disclosed for treating melanoma wherein a betulinic acid derivative is the active compound in the composition to be administered. The compositions are optionally applied topically is inserted therefor.

Abstract: Compositions of matter and methods of treating cancer patients are used to prevent or limit cardiotoxicity during or after cancer treatment with anthracycline drugs, and to prevent or lower resistance to anthracycline drugs, both of which are believed to be caused by the human enzyme carbonyl reductase. Thus, the compositions and methods may be used to reduce the dosages of anthracycline anti-cancer drugs necessary to produce a desired cancer-cell-killing performance. Preferred embodiments comprise treating cancer patients with a pharmaceutical composition comprising compounds having halogenated (or pseudo-halogenated) aryl groups, preferably halogenated (or pseudo-halogenated) arylcyanooximes or phenylcyanooximes and derivatives or analogs thereof, including those comprising —CL or —F, or other substituents on an aryl/phenyl ring.

Abstract: Novel pharmaceutical formulations of ?-(2,4-disulfophenyl)-N-tert-butylnitrone and pharmaceutically acceptable salts thereof and the use of such formulations in the treatment of various diseases and conditions, especially stroke, are disclosed.

Abstract: Disclosed herein is a pharmaceutical composition comprising a relaxant and a pan-alpha-2 receptor agonist. The composition is effective for treating gastrointestinal motility disorders, and methods of treating such disorders using the composition and compounds comprising it are also disclosed.

Abstract: The present invention relates to benefit agent containing delivery particles, compositions comprising said particles, and processes for making and using the aforementioned particles and compositions. When employed in compositions, for example, personal care, cleaning or fabric care compositions, such particles increase the efficiency of benefit agent delivery, there by allowing reduced amounts of benefit agents to be employed. In addition to allowing the amount of benefit agent to be reduced, such particles allow a broad range of benefit agents to be employed.

Abstract: The present invention relates to a microbicide composition for plants, containing at least two active ingredient components in an amount producing synergistic activity, together with an appropriate filler, wherein component I is the compound 2-[?-{[(?-methyl-3-trifluoromethyl-benzyl)imino]-oxy}-o-tolyl]-glyoxylic acid-methylester-O-methyloxime, and component II is a compound selected from the group consisting of IIA) 5,7-dichloro-4-(4-fluorophenoxy)quinoline (“Quinoxyfen”); IIB) 4-cyclopropyl-6-methyl-N-phenyl-2-pyrimidinamine (“Cyprodinil”); IIC) benzo(1,2,3) thiadiazole-7-carbothio-acid-S-methylester (“Acibenzolar-S-methyl”); IID) 3-anilino-5-methyl-5-(4-phenoxyphenyl)-1,3-oxazolidine-2,4-dione (“Famoxadone”); IIE) 8-(1,1-dimethylethyl)-N-ethyl-N-propyl-1,4-dioxaspiro[4.

Abstract: The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them. Compounds according to the present invention are based upon the chemical formula: wherein the substituents have the values mentioned herein.

Abstract: This invention provides estrogen receptor modulators having the structure where R1–R5 are as defined in the specification; or a pharmaceutically acceptable salt thereof.

Abstract: Human muscle tissues involve striated and smooth muscles. Each muscle tissue possesses its own special function. Differences of physiology functions among the muscle tissues are mainly determined by their various initiation and signal transmission systems, defined as the pre-muscle molecular motor mechanism, or initiating and regulating mechanism. The current medications, drugs, and therapies for diseases and symptoms related abnormal increased muscle tone or excessive muscle contraction are aimed just at the pre-muscle molecular motor mechanisms, whereas without directly intending to effect on the muscle molecular motor mechanism i.e. the contractile apparatus mechanism at all, which, however, is in common for all kinds of muscle tissues. The muscle molecular motor mechanism mainly involves recycling of actin-myosin filament cross-bridge formation and sliding movement. In the process, bio-energy provided by ATP hydrolysis is necessarily required.

Abstract: A process for manufacturing bulk solutions and lyophilized pure ?-aztreonam lysinate for large scale production of an inhalable aztreonam is disclosed, as is a pure ?-aztreonam lysinate for inhalation. A dry powder or lyophilized pure ?-aztreonam lysinate composition for inhalation is also disclosed.

Abstract: The invention relates to compositions for treating dandruff comprising compounds that are non-polymeric and/or have a weight average molecular weight of less than about 1000. These compounds, when used at a concentration of about 0.001% or less, inhibit the activity of any Malassezia globosa lipase by at least 50%. The invention also relates to the use of these compounds for inhibiting lipase activity.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Abstract: A wood treatment composition having a synergistic combination of fungicides which may include two or more compounds. These combinations are shown to be especially effective in providing resistance to decay, mold and mildew when wood is treated with these combinations. Also provided is wood treated by these combinations, and a method of treatment for composite wood.

Abstract: Fungicidal mixtures, comprising as active components a) a morpholine or piperidine derivative I selected from the group of the compounds Ia, Ib, Ic and Id and b) compounds of the formula II in a synergistically effective amount are described.

Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compoundsd and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R1–R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.

Abstract: The invention relates to the use of novel anthracene based compounds for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of hydroanthracene based compounds for the inhibition and/or prevention of cancer of the colon, pancreas, prostate, lung, larynx, ovary, breast, glioblastoma, oral cavity, endothelial cells and leukemias. The agents of the invention form a distinct class, distinct from the anthracene, anthrone or anthraquinone derivatives.

Abstract: Dihalopropene compounds, process for their preparation, compositions comprising them and their use as pesticides What is described are dihalopropene compounds of the formula (I) in which R1 and R2 are halogen, Y is —O—, —S— or —NH—, X is —O—, —S(O)r— or —NR5— (where r=0, 1, 2 and R5 is hydrogen or C1-C8-alkyl), X? is a direct C—C bond, —O—, —S(O)r— or —NR5— (where R5 is as defined above), R3 is hydrogen, halogen, nitro, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, C3-C10-cycloalkyl or has one of the meanings defined for A, A has the meaning given in the description (inter alia aryl, heterocyclyl), B is a divalent bridge having the meanings given in the description (inter alia alkylene) and R4 is a monovalent C6-C14-aryl radical or nitrogen-containing heteroaryl radical having at least one ring heteroatom which has the meanings given in the description. These compounds can be used for preparing pesticides.

Abstract: The present invention relates to the use of certain resorcinol derivatives as skin lightening agents.

Abstract: The invention relates to novel fungicidally active compound combinations of

Abstract: A substituted apicidin derivative, a method of synthesis therefore, and an anti-tumor composition comprising the same are disclosed. The substituent of the derivative is preferably semicarbazone, thiosemicarbazone, hydrazone, tert-butylhydrazone, phenylhydrazone, 2,4-dinitrophenylhydrazone, 4-methoxyphenylhydrazone, 3-methoxyphenylhydrazone, 4-nitrophenylhydrazone, benzylhydrazone, methanesulfonylhydrazone, benzenesulfonylhydrazone, 4-methylbenzenesulfonylhydrazone, benzoylhydrazone, 4-nitrobenzoylhydrazone, carbohydrazone, benzyloxime or acetoxime. The compound has strong inhibition effect against histone deacetylase and detransforming activities and specifically inhibit growth of cancer cells. Therefore, it is useful in preparation of an anti-tumor composition.

Abstract: The present invention relates to bicyclic derivatives, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG/S1P receptor mediated signal transduction.

Abstract: The present invention relates to the use of certain resorcinol derivatives as skin lightening agents.

Abstract: Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.

Abstract: 3,4,5-trisubstituted aryl nitrone compounds having the formula: 1

Abstract: Compounds having quinone and quinone analogs useful for pharmaceutical preparations have now been found which inhibit cysteine proteases, in particular, caspases and 3C-cysteine proteases. The cysteine protease inhibitors of the present invention can be identified by their mode of action in disrupting the ability of cysteine proteases and, in particular, caspases to cleave a peptide chain. These compounds are useful in inhibiting cysteine protease or cysteine protease-like proteins and for treating infections diseases or physiopathological diseases or disorders attributed to the presence of excessive or insufficient levels of cysteine proteases.

Abstract: Disclosed are 3,4,5-trisubstituted aryl nitrone compoundsd and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R1-R4 are as defined in the specification. The disclosed compositions are useful as therapeutics for inflammation-related conditions in mammals, such as arthritis, and as analytical reagents for detecting free radicals.

Abstract: The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, 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: Methods of treating a bacterial infection and of killing or inhibiting bacteria are disclosed. The methods use derivatives of triterpenes that are abundant in birch bark and other plants. The triterpenes include betulin, allobetulin, and lupeol.

Abstract: The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.

Abstract: The present invention relates to biphenylyl derivatives, processes for their production, their uses and pharmaceutical compositions containing them.

Abstract: New spisulosine derivatives of use in treating tumors are of the formula (I) wherein: each X is the same or different, and represents H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, CN, halogen, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups X may together form ═O; Y is NR1, OR1, PR1, SR1, or halogen, wherein the number of substituents R1 is selected to suit the valency and each R1 is independently selected of H, OH, C(═O)R′, P(═O)R′R″, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, and wherein the dotted line indicates an optional double bond; each Z is the same different, and represents H, OH,