Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.

Abstract: The present invention relates to a process for the preparation of given carboxamido compounds, in particular of 2,4,6-triiodoisophthalic acid derivatives, as useful intermediates for the preparation of X-ray contrast media among which is iopamidol. The said process comprises reacting suitable N-sulfinyl intermediate compounds with a commercially available ?-hydroxyacid or a salt thereof.

Abstract: Disclosed are new colchicine solid complexes, methods of making the solid complexes as well as formulations prepared therefrom and uses thereof.

Abstract: Provided herein are novel bridged cyclic derivatives of the general formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds can inhibit HDACs and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, neurode-generative disorders etc.

Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier wherein the symbols have the following meaning —X- is e.g. and Y being e.g. or the pharmaceutically acceptable salts can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.

Abstract: The present invention relates to a novel cyclic olefin compound, a polymer including the cyclic olefin compound, a liquid crystal alignment film including the polymer, and a liquid crystal display device including the liquid crystal alignment film. Since the polymer includes the cyclic olefin compound as a main chain, the thermal stability is excellent and the photoreactive speed is high. Accordingly, the production time can be reduced, the production cost can be reduced, and the anchoring force of the liquid crystal can be increased because the alignment property is stabilized due to the curing.

Abstract: The present invention relates to novel propionic acid derivatives. More particularly, the present invention relates to beta-phenyl alpha-oxysubstituted propionic acids of the general formula (I). The present invention also relates to processes for the preparation of compounds of the formula (I) and their use in the preparation of compounds of formula (II).

Abstract: There is provided a convenient and inexpensive method of producing a compound which has a high activity of inhibiting replication of hepatitis C virus (HCV) and is useful for preventing and treating a liver disease caused by HCV infection.

Abstract: The present invention provides compositions comprising the ligand binding domain (LBD) of a farnesoid X receptor (FXR) in crystalline form. In alternative embodiments, the LBD of FXR is complexed with a ligand therefor. There are provided high resolution structures of FXR complexed with a novel high affinity agonist fexaramine. The discovered structure of a FXR LBD provides the first three-dimensional view of the structural basis for FXR ligand binding. The present invention further provides a computer for producing a time-dimensional representation of FXR or a complex thereof, and a computer for determining at least a portion of the structure coordinates of FXR or a complex thereof. The present invention further provides methods of using this structural information to predict molecules capable of binding to FXR; to identify compounds with agonist, antagonist or partial agonist activity for FXR; and to determine whether a test compound is capable of binding to the LBD of FXR.

Abstract: A compound of formula: for treating ocular hypertension.

Abstract: The invention relates to novel multifunctional dendrimer structures with a high loading capacity. Said dendrimer structures include a nucleus having at least a first generation or an end generation covalently bonded thereto. The first generation is formed by at least two of the following structures, namely: a spacer, a load, a branching element. In addition, a plurality of sequences (known as intermediary generations) with at least two of the aforementioned structures can be joined to the first generation. The terminal generation is formed by at least three of the following structures, namely: a spacer, a load, a branching element and a terminal.

Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

Abstract: Disclosed is a diamine represented by a general formula of: wherein X is an ester bond, each of m and n is independently a natural number, each of p and r is independently 0 or 1, q is an integer of 0 or more, a sum of m, n, and q is 20 or less, and when q is 0, p is 1 and r is 0.

Abstract: The present invention provides the production method of carboxylic acid compound, as shown in Scheme I.

Abstract: Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from: or the diamines and diisocyanates thereof, wherein each X represents a member independently selected from —CH2COO— (glycolic acid moiety), —CH(CH3)COO— (lactic acid moiety), —CH2CH2OCH2COO— (dioxanone), —CH2CH2CH2CH2CH2COO— (caprolactone moiety), —(CH2)yCOO— where y is one of the numbers 2, 3, 4 or 6-24 inclusive, and —(CH2CH2O)z?CH2COO— where z? is an integer between 2 and 24, inclusive; each Y represents a member independently selected from —COCH2O— (glycolic ester moiety), —COCH(CH3)O— (lactic ester moiety), —COCH2OCH2CH2O— (dioxanone ester), —COCH2CH2CH2CH2CH2O— (caprolactone ester), —CO(CH2)mO— where m is an integer between 2, 3, 4 or 6-24 inclusive, —COCH2O(CH2CH2O)n— where n is an integer between 2 and 24, inclusive; R? is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; p is an integer between 1 and 4, inclusive; and Rn represents one or more

Abstract: The invention relates to compounds corresponding to general formula (I) below: to the compositions containing same, to methods for the preparation thereof and to the use thereof in pharmaceutical compositions for use in human or veterinary medicine, or else in cosmetic compositions.

Abstract: The invention provides pharmacological compositions comprising a stimulator or activator of the soluble guanylate cyclase alone (sGC) or in combination with a PDE5 inhibitor for the treatment of urological disorders comprising of Benign Prostate Syndrome (BPS), Benign Prostate Hyperplasia (BPH), Benign Prostate Enlargement (BPE), Bladder Outlet Obstruction (BOO), Lower Urinary Tract Symptoms (LUTS), genitourinary disorders comprising neurogenic bladder syndrome (OAB) and (IC), urinary incontinence (UI) like mixed-, urge-, stress-, or overflow incontinence (MUI, UUI, SUI, OUI) and pelvic pain (PP).

Abstract: Process for the preparation of compounds of the formula (I) in which X has the meaning indicated in Patent Claim 1, and precursors thereof.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: The present invention includes methods of making and methods of using peptidomimetics compositions that mimic ?-helical BH3 sequences in cells. The peptidomimetics can be used to mimic ?-helical BH3 sequences and kill cancer cells.

Abstract: The invention relates to novel 2-alkoxy-6-alkylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) in which A, B, D, G, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the 2-alkoxy-6-alkylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant tolerance promoter compound.

Abstract: The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of Ru complexes with bidentate ligands, having one amino or imino coordinating group and one phosphino coordinating group, in hydrogenation processes for the reduction of esters or lactones into the corresponding alcohol or diol respectively.

Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.

Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6alkyl or C1-C6alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R8 and R9 are each independently hydrogen atom, C1-C6alkyl, —CON(R18)(R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6alkyl or C1-C6alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R8 and R9 are each independently hydrogen atom, C1-C6alkyl, —CON(R18)(R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.

Abstract: Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features: (1) make use of a particular I3-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxypropionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products.

Abstract: The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof. [Problem] There is need for (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same. [Solution] Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem.

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: The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically acceptable salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.

Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I: methods for their production, pharmaceutical formulations containing these compounds, methods of producing such pharmaceutical formulations and related methods of treating or inhibiting certain diseases or conditions.

Abstract: The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides.

Abstract: Disclosed are novel compound of formula I, As defined herein and their use as pharmaceutically active compounds for reducing blood glucose, and/or treating one or more of type II diabetes, disturbances of lipid and carbohydrate metabolism, arteriosclerotic manifestations, and insulin resistance.

Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.

Abstract: A medicament which has an activity of inhibiting production of tissue factor and comprises an LXR ligand as an active ingredient; and a medicament for treatment and/or prophylaxis of vascular restenosis following angioplasty, endarterectomy, percutaneous transluminal coronary angioplasty (PTCA) or stent implantation, or treatment and/or prophylaxis of blood coagulation diseases, diseases induced by platelet aggregation including stable or unstable angina pectoris, cardiovascular and cerebrovascular diseases including thromboembolism formation diseases accompanying diabetes, rethrombosis following thrombolysis, cerebral ischemic attack, infarction, stroke, ischemia-derived dementia, peripheral artery disease, thromboembolism formation diseases during use of an aorta-coronary artery bypass, glomerulosclerosis, renal embolism, tumor or cancer metastasis, which comprises an LXR ligand as an active ingredient.

Abstract: The present invention provides compounds of formula (I): pharmaceutical compositions thereof, and methods of using the same, processes or preparing the same, and intermediates thereof.

Abstract: Synthesis methods for the preparation of intermediates which are suitable for the preparation of statin derivatives, and especially to synthesis methods for the intermediate of formula (VI) wherein Ra? and Rc? are each independently of the other hydrogen or hydroxy-protecting group, or together are a bridging hydroxy-protecting group; and Rb is a carboxy-protecting group.

Abstract: This invention relates to a method for the regioselective synthesis of 4,6,7,8-substituted benzo[g]quinoline-3-carbonitriles and 4,6,7,8-substituted benzo[g]quinazolines as well as intermediates thereof. The compounds derived from this invention are useful for the treatment of a variety of diseases that are a result of deregulation of these PTK's, and more specifically, are anti-cancer agents and are useful for the treatment of cancer in mammals. In addition, the compounds derived from this invention are useful for the treatment of polycystic kidney disease in mammals.

Abstract: This invention relates to compounds of the formula (I) which are thyroid receptor ligands, and are preferably selective for the thyroid hormone receptor ?, to methods of preparing such compounds and to methods for using such compounds such as in the regulation of metabolism.

Abstract: The present invention relates to compounds of the formula or pharmaceutically acceptable salts thereof, useful for delivering agents having the capacity to diagnose, treat or prevent bone injury or disease to the bone for interaction therewith.

Abstract: The invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 represents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e.

Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.

Abstract: N-Biphenyl(substituted methyl) aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

Abstract: The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of pharmaceutical compositions for the treatment of inflammatory diseases.

Abstract: Disclosed are phenyl-alkylene benzamides useful as orexin antagonists

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Abstract: Mono-substituted and di-substituted alpha-amino acids and derivatives thereof, substituted at the alpha positon with one (mono-) or two (di-) substituents (R2 and/or R3) as shown in Formula 1: N(R4R5)C(R2R3)CO(OR1).

Abstract: The present invention is directed to selective LXR modulators, small molecule compounds corresponding to Formula I and is further directed to a process of treating a condition in a mammal that is modulated by LXR using a therapeutically effective dose of a compound of Formula I.

Abstract: A process for the preparation of fibrates of formula I in which R1 is a halogen atom, a 2,2-dichloro-cyclopropyl group, a (4-chlorophenyul)-hydroxymethyl group, a-4-chlorobenzoyl group or a 2-(4-chlorobenzamido)-ethyl group, and R2 is hydrogen or a C1-C4 alkyl group.

Abstract: The present invention provides a method for preparing dimer of a monohydroxy aromatic compound. In the method of the present invention, oxidative coupling reaction of a monohydroxy aromatic compound represented by formula [I]: Ar—OH??[I] wherein Ar represents an optionally substituted aromatic group is carried out in a nitrogen containing polar solvent in the presence of a copper salt. By the method of the instant invention, dimer of the monohydroxy aromatic compound can be obtained in high yield.