Abstract: This application describes a compound represented by Formula (I): wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X1 is a covalent bond or —CH2CH2—, X2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

Abstract: In certain aspects, provided herein are RNA complexes (e.g., asymmetric RNA complexes, such as asiRNAs and lasiRNAs) that inhibit tyrosinase expression and are therefore useful for reducing melanin production and for treating pigmentation-related disorders associated with excessive melanin production, such as melasma and age spots.

Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

Abstract: The present invention provides methods and compositions for reducing pigmentation.

Abstract: A compound represented by the following general formula (I) which has ADAM17 inhibitory activity, or a salt thereof, or a solvate thereof: wherein X represents a phenylene group; Y represents a hydrogen atom, —(CH2)mR1 or the like; R1 represents —NR5COR2, —NR5SO2R2 or —NR3R4; R2 represents a C1-C6 alkyl group, an aryl group, or a C1-C6 alkoxy group; R3 and R4 represent a C1-C6 alkyl group and the like; R5 represents a hydrogen atom or a C1-C6 alkyl group or the like; m indicates an integer of from 0 to 4; and Z represents a hydrogen atom or a C1-C6 alkyl group.

Abstract: The present invention provides a composition having an excellent controlling activity on a pest. The composition comprising a compound represented by Formula (1) and the cyanamide compound represented by Formula (2) shows an excellent controlling activity on a pest.

Abstract: A compound of formula (I): wherein: R1 is —SR10, —O—C(O)—R11, —NR12R13, where R10 is a C1-8-alkyl group or a phenyl group unsubstituted or substituted by a C1-4-alkyl group, R11 is a thiophenenyl, furanyl or pyrrolyl group, R12 is H or a C1-4-alkyl group and R13 is a C1-8-alkyl group or a phenyl group unsubstituted or substituted by a C1-4-alkyl group; R2 is H or a C1-4-alkyl group; R3 and R4 are independently H or C1-4-alkyl groups; R5 and R6 are independently H, OH or OR14, or taken together are ?O, where R14 is a protecting group; R7 is H or a C1-4-alkyl group; and, R8 is H, R9 is OH and R15 is H, or R15 is H and R8 and R9 taken together are —O—, or R9 is OH and R8 and R15 taken together form a bond; and, R18 and R19 are both H, or R18 and R19 taken together form a bond, or a plant physiologically acceptable salt thereof is useful for inhibiting 9-cis-epoxycarotenoid dioxygenase (NCED) in a plant or seed and is therefore useful for regulating ABA biosynthesis in the plant or seed.

Abstract: The instant invention provides a method for treating patients by administering a JAK inhibitor. The instant invention provides a method for treating patients by administering a JAK inhibitor wherein the JAK inhibitor is a JAK2 inhibitor. The instant invention provides a method for treating patients by administering a JAK inhibitor wherein the JAK inhibitor is selected from selected from Jak2-IA, AG490, Pyridone 6, WP1066, LS104, TG101209, TG101348, CP690,550, CP352,664, INCB18424, WHI-P154, CMP6, SB1518, XL019, CEP-701, INCB20, AUH-6-96 and AZ960.

Abstract: The present invention relates to novel thiourea derivatives as a modulator for vanilloid receptor (VR) and the pharmaceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.

Abstract: An aqueous storage-stable composition comprises from about 10 to about 35% by weight hydrogen cyanamide, from about 3 to about 25% by weight propionic acid, potassium propionate or ammonium propionate, and water, and has a pH of from about 2.5 to about 4, wherein the concentration of hydrogen cyanamide is greater than the concentration of propionic acid.

Abstract: Agricultural crops are protected from the growth of undesirable vegetation as well as nematode and insect infestations, by the application of hydrogen cyanamide in combination with a short-chain, water-soluble monocarboxylic acid, with improved pesticidal effect.

Abstract: Agricultural crops are protected from the growth of undesirable vegetation as well as nematode and insect infestations, by the application of hydrogen cyanamide in combination with a short-chain, water-soluble monocarboxylic or polycarboxylic acid, the acid containing 1-3 carboxy groups and either no hydroxy groups or 1-3 hydroxy groups.

Abstract: The present invention discloses a magnetic nanocomposite for inhibiting/treating cancer and a method for fabricating the same. The magnetic nanocomposite comprises a core formed of a plurality of magnetic nanoparticles made of ferric ferrous oxide (Fe3O4); a shell made of a carboxy-functionalized polyaniline; and an anti-tumor medicine bound to the external surface of the shell. The method of the present invention fast fabricates the magnetic nanocomposite in a simple way. The medicine of the present invention has a longer half life and a better thermal stability. The present invention disperses the water-insoluble medicine in water uniformly to decrease the biological rejection. Moreover, the magnetic nanocomposite of the present invention is guided to the nidus by an external magnetic field to increase the local concentration of the medicine and provide an effective chemotherapy. Therefore, the present invention has competitive advantage over the conventional BCNU.

Abstract: The invention relates to substituted enaminones of Formula I and their derivatives and the discovery that these compounds modulate the effect of ?-aminobutyric acid (GABA) on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.

Abstract: This invention is directed to compounds of formula (I), wherein m, formula (II), R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.

Abstract: The present invention provides methods and compositions for reducing pigmentation.

Abstract: Materials and Methods for inhibiting neuronal damage are provided herein. In particular, materials and methods for inhibiting neuronal damage associated with pathological action of extracellular ATP are provided herein.

Abstract: The invention relates to new chemical compounds acting on the serotonin transporter (SERT), and associated pharmaceutical compositions, methods for use as therapeutic agents, and methods of preparation thereof. In particular the new chemical compounds are useful for the treatment of a variety of central nervous system (CNS) disorders—for example anxiety, depression, epilepsy, obsessive-compulsive disorders, migraine, cognitive disorders, sleep disorders, feeding disorders, panic attacks, disorders related to withdrawl from drug abuse, schizophrenia, or the like, or in the treatment of gastrointestinal disorders such as irritable bowel syndrome.

Abstract: Agricultural crops are protected from the growth of weeds and other undesirable organisms by the application of hydrogen cyanamide in a granular formulation.

Abstract: Dimethyl cyanamide is an active herbicide and nematicide.

Abstract: Agricultural crops are protected from the growth of undesirable vegetation as well as nematode and insect infestations, by the application of hydrogen cyanamide in combination with a short-chain, water-soluble monocarboxylic acid, with improved pesticidal effect.

Abstract: The invention relates to a medicament for IBS, which comprises a dual antagonist for 5-HT2B and 5-HT7 receptors having selective binding affinities for 5-HT2B and 5-HT7 receptors. The pharmaceutical composition of the invention is useful as a drug which is excellent in the therapeutic effect on IBS and shows lessened side effects occurring in the existing remedies for IBS, because it showed good pharmacological actions in comparison with the case of independently using a 5-HT2B receptor antagonist having selective binding affinity for 5-HT2B receptor or a 5-HT7 receptor antagonist having selective binding affinity for 5-HT7 receptor.

Abstract: The present invention relates to novel N?-cyano-N-methylimidamide derivatives of the general formula (I) in which n represents 2, 3, 4 or 5, R represents optionally halogen-substituted C1-C4-alkyl, and X represents halogen, where the substituents X may in each case be identical or different, to processes for their preparation and to their use as pesticides.

Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.

Abstract: Polyacetals comprising a recurring units represented by a formula selected from the group consisting of formula (I) and (II): wherein A comprises at least one acetal group; B is selected from the group consisting of —CH—, —CH(CH3)—, CH2CH—, —CH2C(CH3)—, —CH(CH3)CH—, and —CHCH(CH3)CH(CH3)—; Z is selected from the group consisting of C(O)OR1, C(O)SR1, C(O)NR1R2, and VU; V is a linker group; U is selected from the group consisting of poly(ethyleneimine), poly(propyleneimine), poly(lysine), PAMAM dendrimer, octaamine dendrimer, hexadecaamine dendrimer, enhancer, and targeting receptor; R1 and R2 are each individually selected from the group consisting of hydrogen, C1 to C10 alkyl, and C6 to C10 aryl; D is a linkage selected from the group consisting of carboxylic amide, carboxylic ester, urea, and urethane; and G is selected from the group consisting of C4 to C20 alkyl, C6-C10 aryl, and —(OCH2CH2)n—, where n is in the range of 1 to about 250, are useful in nucleic acid delivery applications.

Abstract: In accordance with the present invention, there are provided various methods for modulating the expression of an exogenous gene in an isolated cell and in a mammalian subject employing modified ecdysone receptors. Also provided are modified ecdysone receptors, as well as homomeric and heterodimeric receptors containing same, nucleic acids encoding invention modified ecdysone receptors, modified hormone response elements, gene transfer vectors, recombinant cells, and transgenic animals containing nucleic acids encoding invention modified ecdysone receptor.

Abstract: Disclosed are methods for inhibiting Ras activity such as cell proliferation associated with vascular injury such as post-angioplasty restenosis and atherosclerosis. Preferred Ras antagonists are S-trans-trans farnesylthiosalicylic acid (FTS) and structurally related compounds (or analogs) thereof.

Abstract: Compounds according to the following formula (I): wherein the variables Q and R1 to R6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F, L and B; pharmaceutical compositions containing such compounds, and method of treating diseases and pathological conditions exacerbated by these cysteine proteases such as, but not limited to rheumatoid arthritis, multiple sclerosis and other autoimmune diseases, osteoporosis, asthma, Alzheimer's disease, atherosclerosis and endometriosis.

Abstract: A polymer comprising recurring units represented by formula (I): wherein X is selected from the group consisting of C(O)OR1, C(O)SR1, C(O)NR1R2, and VZ, where R1 and R2 are each individually selected from the group consisting of hydrogen, C1 to C10 alkyl, and C6 to C10 aryl, where V is a labile linker group, and where Z is selected from the group consisting of poly(ethyleneimine), poly(propyleneimine), poly(lysine), PAMAM dendrimer, octaamine dendrimer, and hexadecaamine dendrimer; and wherein Y is selected from the group consisting of —(CH2)2—, —(CH2)2—O—(CH2)2—, —(CH2)2—O—(CH2)2—, and —(CH2)3—NHC(O)—(CH2)6—C(O)NH—(CH2)3— is useful in nucleic acid delivery applications. Polyacetals of the formula (I) are preferably made by reacting appropriate diols and divinyl ethers. In preferred embodiments, complexes formed between polyacetals of the formula (I) and polynucleotides are useful as transfection reagents.

Abstract: The present invention relates to novel substituted imide derivatives of the general formula (I) in which R1 represents optionally substituted cycloalkyl, R2 represents optionally substituted alkyl or optionally substituted cycloalkyl, R3 represents alkyl, alkoxy, alkylthio, amino, alkylamino or dialkylamino and R4 represents cyano or nitro, and to processes for their preparation and to their use for controlling animal pests and as herbicides.

Abstract: Compounds, preparations and methods for immunosuppressive treatment of autoimmune disorders, graft rejection and/or graft/host disease. Therapeutically effective amounts of certain substituted triarylmethane compounds, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole, are administered to mammalian patients to selectively inhibit the calcium-activated K+ channel (IKCa1) in lymphocytes, monocytes, macrophages, platelets or endothelial cells without concomitant inhibition of P450-dependent enzyme systems, resulting in reduction of antigen-, cytokine-, or mitogen-induced calcium entry through store operated calcium channels in these cells, suppression of cytokine production by these cells, and inhibition of activation of these cells. Such inhibition of the Ca++ activated K+ channel (IKCa1) prevents the pre-Ca++ stage of cell activation and thus causes immunosuppression and an anti-inflammatory response.

Abstract: Compounds, compositions and methods treating arthritic disorders such as osteoarthritis or rheumatoid arthritis, and for treating other diseases associated with altered mitochondrial function, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes.

Abstract: The invention relates to insecticide-comprising polymer-based compositions which, in order to recognize the point in time when the insecticide is exhausted, comprise at least one dye which, after the insecticide has evaporated, turns a different colour.

Abstract: The present invention relates to novel imidamide derivatives of the formula (I) in which R, R1, R2 and R3 are each as defined in the description, to a process for their preparation and to their use for controlling animal pests, such as insects, arachnids and, in particular, nematodes.

Abstract: The present invention relates to novel thiourca derivatives as a modulator for vanilloid receptor (VR) and the phar- maceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflam- matory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.

Abstract: The present invention relates to certain tri-substituted phenyl derivatives and analogues of formula (I), to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: A compound selected from the group consisting of a compound of formula I 1

Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides naphthalene compounds, intermediates, formulations, and methods.

Abstract: A compound selected from the group consisting of a compound of formula I 1

Abstract: There is provided an excellent novel analgesic having an analgesic effect which is effective widely against a pain including a chronic pain or an allodynia accompanied with herpes zoster by acting on a nociceptin receptor.

Abstract: The present invention relates to novel substituted imide derivatives of the general formula (I) 1

Abstract: A drug delivery system for oral administration in solid dry form of greasy/oily/sticky substance(s) and pharmaceutically active substance(s) or pharmaceutically active substance(s) which itself/themselves is/are greasy/oily/sticky) characterized by having a plurality of solid, polymeric matrix beads comprising considerable amounts of greasy/oily/sticky substances and having fast release characteristics and a process for the preparation of such solid, polymeric matrix beads comprising greasy/oily/sticky substances.

Abstract: Compounds, preparations and methods for immunosuppressive treatment of autoimmune disorders, graft rejection and/or graft/host disease. Therapeutically effective amounts of certain substituted triarylmethane compounds, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole, are administered to mammalian patients to selectively inhibit the calcium-activated K+ channel (IKCa1) in lymphocytes, monocytes, macrophages, platelets or endothelial cells without concomitant inhibition of P450-dependent enzyme systems, resulting in reduction of antigen-, cytokine-, or mitogen-induced calcium entry through store operated calcium channels in these cells, suppression of cytokine production by these cells, and inhibition of activation of these cells. Such inhibition of the Ca++ activated K+ channel (IKCa1) prevents the pre-Ca++ stage of cell activation and thus causes immunosuppression and an anti-inflammatory response.

Abstract: In accordance with the present invention, there are provided various methods for modulating the expression of an exogenous gene in an isolated cell and in a mammalian subject employing modified ecdysone receptors. Also provided are modified ecdysone receptors, as well as homomeric and heterodimeric receptors containing same, nucleic acids encoding invention modified ecdysone receptors, modified hormone response elements, gene transfer vectors, recombinant cells, and transgenic animals containing nucleic acids encoding invention modified ecdysone receptor.

Abstract: Amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of amido polybiguanides is also disclosed. The amido polybiguanides are useful in the preservation of pharmaceutical compositions, particulary opthalmic and otic pharmaceutical compositions and compositions for treating contact lenses. The compounds are especially useful for disinfecting contact lenses.

Abstract: The present invention discloses highly packed polycationic ammonium, sulfonium and phosphonium lipid compounds useful for making lipid aggregates for delivery of macromolecules and other compounds into cells. They are especially useful for the DNA-dependent transformation of cells. Methods for their preparation and use as intracellular delivery agents are also disclosed.

Abstract: The (R)-enantiomer of 4-[[(cyanoimino)-[(1,2,2-trimethylpropyl)amino]methyl]amino]-benzonitrile as well as the corresponding (S)-enantiomer are useful for promoting hair growth such as in male pattern baldness.

Abstract: This invention relates to novel compounds of Formula (1), pharmaceutical compositions and their use in the treatment of disease states mediated by the chemokine, Interleukins-8 (IL-8).

Abstract: The present invention relates to new imidic acid derivatives of the formula (I) to a plurality of processes for their preparation, and to their use as pesticides.

Abstract: Guanidine and diaminonitroethene derivatives represented by the formula ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined in the description, compositions thereof and methods for preparing the compounds are described. The se compounds are useful in the treatment of diseases of the central nervous system, cardiovascular system, pulmonary system, gastrointestinal system and endocrinologic system.