Abstract: Disclosed herein is a compound of Formula I or a pharmaceutically acceptable salt thereof, in which A, G, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions of the compounds are suitable for the treatment of HCV infection in mammals and are also useful to modulate or inhibit NS3/4 dimerization.

Abstract: The invention provides a compound conforming to the structure of Formula (CXX) The invention also provides a thermoplastic polymer composition comprising a polyolefin polymer and a compound conforming to the structure of Formula (CXX) as a nucleating agent.

Abstract: In accordance with certain embodiments of the present disclosure, a self-assembling biodegradable nanoparticle is provided. The nanoparticle includes Cys-Val-Val-Val-Val-Val-Val-Lys-Lys conjugated with a synthetic polymer and has a diameter of from about 50 nm to about 150 nm.

Abstract: This invention relates generally to methods and agents for modulating adiposity-related conditions. More particularly, the present invention relates to the use of TRAIL death receptor agonists, including nucleic acids such as TRAIL polynucleotides, peptides and polypeptides including TRAIL polypeptides, TRAIL DR agonist antigen-binding molecules, TRAIL DR peptide agonists as well as small molecule TRAIL DR agonists in compositions and methods for treating or preventing adiposity-related conditions such as obesity, diabetes mellitus and metabolic syndrome.

Abstract: The present invention relates to compounds that have the ability to modulate the activity of GPR40 and are therefore useful in the treatment of GPR40 related disorders. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders related to GPR40 activity.

Abstract: The disclosure relates to a process for preparing benzofuran derivatives of general formula I: in which R, R1, and R2 are as defined in the disclosure; by coupling the hydroxylamine with a diketone of general formula III: in order to form an oxime that is then cyclized by heating in order to form the desired compound.

Abstract: The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.

Abstract: Pharmaceutical compositions and their methods of use are provided, where the pharmaceutical compositions comprise an amphetamine prodrug that provides enzymatically-controlled release of amphetamine or an amphetamine analog. The composition can further comprise an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of amphetamine or the amphetamine analog from the amphetamine prodrug so as to attenuate enzymatic cleavage of the amphetamine prodrug.

Abstract: In accordance with certain embodiments of the present disclosure, a self-assembling biodegradable nanoparticle is provided. The nanoparticle includes Cys-Val-Val-Val-Val-Val-Val-Lys-Lys conjugated with a synthetic polymer and has a diameter of from about 50 nm to about 150 nm.

Abstract: The invention relates to a compound of the formula (I) or the formula (II) in which: W is an oxygen atom or a radical of the formula NH; X is hydrogen or an alkaline cation or a C1-C8 alkyl or a —(CH2)n3—C(R4)(R5)(R6) radical; X and R on the one hand and X and R1 on the other hand may independently form an optionally substituted cycle with 5, 6 or 7 links. The invention also relates to complexes of said compounds with at least one metal selected from the group comprising copper, palladium, ruthenium, iridium and rhodium, and to a method for the synthesis of these compounds. These compounds and complexes can be used in various asymmetrical catalysis methods.

Abstract: The present invention discloses processes for the preparation and isolation of [1,2,4]oxadiazo-3-yl derivatives of carboxylic acids. The derivatives are useful in the treatment of inflammatory diseases and conditions.

Abstract: Disclosed are rigid random coils, having a contour length larger than a diameter thereof, an average bending ratio Db of 0.1˜0.8, and a weight average molecular weight of 1×108˜9×108 g/mole, and a resin composition or organic solvent composition including the same. The rigid random coils have the properties intermediate between those of polymers and rigid rod particles, and thus may be used as filler of various resins, aqueous solutions or organic solvents.

Abstract: Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.

Abstract: This invention relates to certain chirally-correct mitoprotectant phosphorylated heterocyclic agents [formula (I)], which are useful for the treatment of dermatological disorders that include challenged skin from cancer, diabetes, radiation treatments, chemotherapy, and sun-burn; mitochondrial dysfunction; age spots; acne, loss of cellular antioxidants; skin changes associated with aging including collagen loss, loss of skin pliability, loss of skin suppleness, skin wrinkles and fine lines, oxidation, damage from radiation, damage from free radicals, and damage from UV; dry skin; xerosis; ichthyosis; dandruff; brownish spots; keratoses; melasma; lentigines; liver spots; skin pigmentation including pigmented spots, dark circles under the eyes, darkened skin, and blemishes; oily skin; warts; eczema; pruritic skin; psoriasis; inflammatory dermatoses; topical inflammation; disturbed keratinization; scalp dryness; skin depigmentation, and combinations thereof;

Abstract: The present invention relates to novel oxime derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: A curing resin composition that cures in two stages: photo cure and thermal cure, hardly contaminates a liquid or liquid crystals when in contact with, and provides high adhesive strength, particularly a curing composition that photocures sufficiently even when shadowed by TFT wires, a black matrix, etc. in photocuring; and a sealant, a sealant for ODF (one-drop-fill), and an LCD containing the curing resin composition. The curing resin composition contains (A) an oxime ester radical initiator represented by general formula (I), where symbols are as defined in the description, (B) a radical curing resin, (C) a latent epoxy curing agent, and (D) an epoxy resin.

Abstract: This invention relates to a prodrug comprising a partial structure having the general formula (I) or (II), where R1 and R2 are hydrogen, alkyl, or aryl radicals.

Abstract: A drug using the magnetic properties of a metal salen complex as represented by the following general formula in order to magnetize the intended drug by chemically binding the drug to a metal salen complex so that the drug can be delivered to the target diseased site. The drug can be delivered to the diseased site using the magnetic properties of the drug per se without using a carrier made of a magnetic substance as in the conventional methods.

Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta (TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.

Abstract: The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof and to the pharmaceutical composition as well as the preparation method of the compounds. The compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.

Abstract: The present invention provides symmetric carbocyanine dyes and dye precursors useful for fluorescence microscopy, and methods of making and using same.

Abstract: Certain chemical entities are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Abstract: The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.

Abstract: A compound of formula A1 or A2 for use in the treatment of a demyelinating peripheral neuropathy: wherein A is COOR5, OPO(OR5)2, PO(OR5)2, SO2OR5, POR5OR5 or 1H-tetrazol-5-yl, R5 being H or an ester-forming group, optionally C1-6alkyl; W is a bond, C1-3alkylene or C2-3alkenylene; Y is C6-10aryl or C2-9heteroaryl eg C3-9heteroaryl, optionally substituted by 1 to 3 radicals selected from halogen, OH, NO2, C1-6alkyl, C1-6alkoxy; halo-substituted C1-6alkyl and halo-substituted C1-6alkoxy; Z is chosen from: wherein the asterisks of Z indicate the point of attachment between —C(R3)(R4)— and A of Formula Ia or Ib, respectively; R6 is chosen from hydrogen and C1-6alkyl; and J1 and J2 are independently methylene or a heteroatom chosen from S, O and NR5; wherein R5 is chosen from hydrogen and C1-6alkyl; and any alkylene of Z can be further substituted by one to three radicals chosen from halo, hydroxy, C1-6alkyl; or R6 can be attached to a carbon atom of Y to form a 5-7 member ring; R1 is C6-10aryl or C

Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.

Abstract: The present invention relates to a product of reaction between a primary and/or secondary amine and one or more active ingredients. By the present invention, there is provided a release of the active component over a longer period of time than by the use of the active itself.

Abstract: The invention relates to a method for improving the bioavailability of pharmaceutical substances and for allowing the pharmaceutical substances to permeate the blood-brain barrier, the pharmaceutical substances having at least one or more amidine, guanidine, N-hydroxyamidine (amidoxime) or N-hydroxyguanidine functions. The invention also relates to medicaments containing the correspondingly modified pharmaceutical substances.

Abstract: This invention relates to certain skin and hair care agents of formula (I), derived from natural amino acids and peptides.

Abstract: The invention relates to a compound of the formula (I) or the formula (II) in which: W is an oxygen atom or a radical of the formula NH; X is hydrogen or an alkaline cation or a C1-C8 alkyl or a —(CH2)n3—C(R4)(R5)(R6) radical; X and R on the one hand and X and R1 on the other hand may independently form an optionally substituted cycle with 5, 6 or 7 links. The invention also relates to complexes of said compounds with at least one metal selected from the group comprising copper, palladium, ruthenium, iridium and rhodium, and to a method for the synthesis of these compounds. These compounds and complexes can be used in various asymmetrical catalysis methods.

Abstract: A compound of formula (III): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20alkyl group; L? is a single bond, —O— or —C(?O)—; A is selected from the group consisting of: formulae (i) (ii) (iii) wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; D is selected from: formulae (i) (ii) (iii) (iv) (v) (vii) (viii) (ix) B is selected from the group consisting of: formulae (A) (B) where RP6 is selected from fluoro and chloro; and R2 is either: (i) —CO2H; (ii) —CONH2; (iii) —CH2—OH; or (iv) tetrazol-5-yl.

Abstract: Formula 1 is an antioxidant compound, wherein R, R1, or D is an antioxidant substituent; R and D are each independently selected from hydrogen or groups containing cysteine, thiols, disulfides, amino acids, amines, amides, or carboxylic acids; when one of R or D is hydrogen, the other includes a thiol, disulfide, or carboxylic acid; A is CO, SO, SO2, or C?S; E is one or more ring groups which are aromatic, carbocyclic, and/or heterocyclic 5, 6 and 7 membered rings being mono, bi, tri, tetra, penta, hexa, hepta or octa cyclic fused rings that are substituted or unsubstituted, each heterocyclic ring can include hetero atoms chosen from to O, S, N, Se, or P; each R1 is at a para, meta, and/or ortho position; n is 1, 2, 3, 4, or 5 for each ring; and each R1 is hydrogen or an antioxidant substituent.

Abstract: In one embodiment of the present disclosure, an inactivator of protein arginine deiminase 4 is disclosed. The inactivator includes: (I) and x includes F; Cl, and H, y includes OH and NH2, R includes H, an alkyl group, an alkenyl group, an alknyl group, and n is greater than 0.

Abstract: An object of the present invention is to provide an angiogenesis inhibitor. The angiogenesis inhibitor according to the present invention contains a compound represented by the following general formula [I] or a salt thereof as an active ingredient. In the formula, the ring A represents a benzene ring or a naphthalene ring; X represents a single bond, an alkylene group or —CH2COOCH2—; Y represents an oxygen atom or N(R6); R1, R2 and R3 are the same or different and represent a hydrogen atom or an alkyl group, or R1 and R3 may be joined together to form a ring having one or more double bonds; R4 and R5 are the same or different and represent a hydrogen atom or an alkyl group; and R6 represents a hydrogen atom or an alkyl group.

Abstract: This invention relates to certain skin and hair care agents of formula (I), derived from natural amino acids and peptides. These agents provide multi-functional treatment of enzyme-related topical problems, for example, darkened skin including age spots, circles around eyes and stretch marks; skin conditions related to acne including excess facial oil and facial pore size; premature hair aging including hair loss and graying; inflammation including intra-cellular and extra-cellular inflammation; skin aging including wrinkles and fine lines; loss of collagen including thinning skin and loss of skin pliability; malfunction of tyrosinase group of enzymes; malfunction of matrix metalloprotease group of enzymes; and combinations thereof: Wherein, R, R?, and R?=any substituent(s); and M=H, Li, Na, K, Ca, Mg, Zn, Mn, Cu, Fe, Co, Mo, V, Cr, Ammonium, Alkyl ammonium, and Nitrogen Heterocyclic ammonium.

Abstract: It is an object of the present invention to provide 2-iminocarboxylic acid derivatives, and a practically suitable industrial method for producing benzazepinones in a short process under mild conditions. The present invention provides a method for producing a benzazepinone or a salt thereof, which comprises opening a ring of an isoquinoline derivative and subsequently converting the thus generated amine into a benzazepinone through lactamization reaction.

Abstract: This invention relates to a method for preparing tetrafluorobenzyl-5-aminosalicylic acid derivative and its pharmaceutically acceptable salt compounds. In particular, this invention relates to a method for preparing tetrafluorobenzyl-5-aminosalicylic acid derivative and its pharmaceutically acceptable salts by using tetrafluorobenzilidine-5-aminosalicylic acid derivative as an intermediate.

Abstract: A new class of non-glycosidic and non-peptidic inhibitors of selectins with low molecular weight according to the general formula 1 is described, as well as methods for their production. These compounds represent a new class of non-toxic, in vivo anti-inflammatory effective inhibitors of selectins, and do not exhibit the disadvantages of the glycosidic inhibitor complexes, and are furthermore more potent in vitro, compared to the known drug bimosiamose. Furthermore, medicaments containing the compounds and their uses in the treatment of diseases are described.

Abstract: Disclosed are Compounds of formula I And methods of use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes.

Abstract: The present invention relates to substituted aryl oximes and methods of using them.

Abstract: This invention relates to certain skin and hair care agents of formula (I), derived from natural amino acids and peptides. These agents provide multi-functional treatment of enzyme-related topical problems, for example, darkened skin including age spots, circles around eyes and stretch marks; skin conditions related to acne including excess facial oil and facial pore size; premature hair aging including hair loss and graying; inflammation including intra-cellular and extra-cellular inflammation; skin aging including wrinkles and fine lines; loss of collagen including thinning skin and loss of skin pliability; malfunction of tyrosinase group of enzymes; malfunction of matrix metalloprotease group of enzymes; and combinations thereof: Wherein, R, R?, and R?=any substituent(s); and M=H, Li, Na, K, Ca, Mg, Zn, Mn, Cu, Fe, Co, Mo, V, Cr, Ammonium, Alkyl ammonium, and Nitrogen Heterocyclic ammonium.

Abstract: Compounds of the formula where the variables have the values described in the specification are antagonists of RAR?retinoid receptors.

Abstract: This invention relates to Schiff's bases derived from amino acids and hydroxyaryl alkyl ketones, or a plant extract containing the same, having general chemical structure in FIG. 1 for topical application. This invention also relates to certain metal complex of said Schiff's bases, which have a crown-like appearance in their three-dimensional chemical structure, as in FIG. 2. The Schiff's bases and their metal complexes of the present invention are useful for the modulation of metal-activated enzymes and metalloenzymes, such as Phenylalanine Hydroxylase, Tyrosine Transaminase, Phenylalanine Transaminase, Tyrosinase, various MMP (Matrix metalloproteases), Superoxide dismutase, 5-Alpha Reductase, and citrate lyase. These are further suitable for multifunctional topical methods for skin whitening, skin wrinkles reduction, skin antiaging, collagen synthesis, acne control, hair loss prevention, hair graying control, and facial oil control.

Abstract: The present invention relates to substituted aryl oximes and methods of using them.

Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.

Abstract: Compounds of the formula (I) or (II) wherein R1 is C1-C10haloalkylsulfonyl, halobenzenesulfonyl, C2- C10haloalkanoyl, halobenzoyl; R2 is halogen or C1-C10 haloalkyl; Arl is phenyl, biphenylyl, fluorenyl, naphthyl, anthracyl, phenanthryl, or heteroaryl, all of which are optionally substituted; Ar?1 is for example phenylene, naphthylene, diphonylene, heteroarylene, oxydiphenylene, phenyleneD-D1-D-phenylene or —Ar?1-A1—Y1-A1—Ar?1—; wherein these radicals optionally are substituted; Ae?, is phenylene, naphthylene, anthracylene, phenanthrylene, or heteroarylene, all optionally substituted; A, is for example a direct bond, —0—, —S—, or —NR6—; Y, inter alia is C1-C18alkylene; X is halogen; D is for example —0—, —S— or —NR6—; D, inter alia is C1-C18alkylene; are particularly suitable as photolatent acids in ArF resist technology.

Abstract: Compound of formula (I): wherein: R1 represents aryl, heteroaryl or alkyl which is optionally substituted, or a group of formula —(CO)—CR6R7NR8R9 wherein R6, R7, R8 and R9 are as defined in the description, R2 represents hydrogen or alkyl, R3 represents hydrogen or optionally substituted alkyl, R4 represents a saturated or unsaturated, 7- to 15-membered bicyclic system or optionally substituted alkyl, or R3 and R4, together with the carbon atom carrying them, form a saturated or unsaturated, 3- to 18-membered, mono-, bi- or tri-cyclic system optionally containing one or more hetero atoms selected from O, S and N and optionally substituted, n represents 1 or 2, Ar represents aryl or heteroaryl, R5 represents amino, guanidino, cyano or amidino which is optionally substituted, its optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in pathological conditions involving activated protein C.

Abstract: A compound for use in inducing necrosis in vascular tissue of a tumor in an animal. The compound contains a first moiety which is a cis-stilbene moiety and a second moiety which is an inhibitor of the formation or action of nitric acid. Also, a method for inducing necrosis in vasculature of a tumor in an animal by administering to the animal the compound in an amount effective for inducing the necrosis.

Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.

Abstract: The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is increased at elevated concentrations of reducing sugars in the blood and in the intracellular environment such as occurs with diabetes. The structural and functional integrity of the affected molecules become disturbed by these modifications and can result in severe consequences. The compounds of the present invention can be used to inhibit this process of nonenzymatic glycation and therefore to inhibit some of the ill effects caused by diabetes or by aging. The compounds are also useful for preventing premature aging, spoilage of proteins in food and can prevent discoloration of teeth.

Abstract: Prodrug compounds capable of permeating a desired biological compartment and releasing a biologically active molecule in active form to effect a therapeutic functional change in the compartment to which it is introduced.