Abstract: The present invention is directed to the diastereoisomeric mixture and the individual isomeric components of the formula:

Abstract: Disclosed herein are compounds of Formula I as disclosed herein, methods of modulating the activity of an estrogen receptor and methods of treating a disorder associated with estrogen receptors.

Abstract: Provided is a use of a prodrug composition containing a naphthoquinone-based compound of Formula 1 for the manufacture of a medicament for treatment or prevention of metabolic syndrome diseases. wherein R1 to R10, X, m and n are as defined in the specification.

Abstract: An amorphous form of ramelteon is provided, as well as mixtures of amorphous and crystalline ramelteon. Also provided are methods of preparing amorphous ramelteon and mixtures of amorphous and crystalline ramelteon, pharmaceutical compositions comprising amorphous ramelteon and mixtures of amorphous and crystalline ramelteon, and methods of treatment of insomnia using the compositions of the invention.

Abstract: The present invention relates to compounds of the formula I where X1, X2, R1, R2, A1, A2, Z1, Z2, m, n and rings B and B? are as defined in claim 1.

Abstract: The present application describes deuterium-enriched ramelteon, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The invention provides the use of at least one plant selected from plants of the family Zingiberaceae in the preparation of a medicament for use in the treatment or prophylaxis of allergic diseases. The plant is optionally selected from the genera Siphonochilus, Kaempferia, Cienkowskia and Cienkowskiella and the species is optionally selected from Siphonochilus aethiopicus, Siphonochilus natalensis, Kaempferia aethiopica, Kaempferia natalensis, Kaempferia ethelae, Cienkowskia aethiopica and Cienkowskiella aethiopica. The allergic disease is selected from asthma and atopy.

Abstract: The present invention provides processes and intermediates for the synthesis of ramelteon.

Abstract: The present invention provides a prophylactic or therapeutic agent for irritable bowel syndrome, which comprises a compound represented by formula (I): wherein, R1 represents an optionally substituted hydrocarbon group, etc., R2 represents a hydrogen atom or an optionally substituted hydrocarbon group, R3 represents a hydrogen atom, an optionally substituted hydrocarbon group, etc., X represents CHR4, NR4, CO, O or S (wherein, R4 represents a hydrogen atom, an optionally substituted hydrocarbon group, etc.), Y represents C, CH or N, represents a single bond or double bond, ring A represents an optionally substituted 5- to 7-membered oxygen-containing heterocyclic ring, ring B represents an optionally substituted benzene ring, and m represents an integer of 1 to 4, or a salt thereof.

Abstract: The present invention provides a method for easily and inexpensively preparing a racemate or an optically-active 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione in high yields, 2-acetyl-2,3-dihydro-5-hydroxynaphtho[2,3-b]furan-4,9-dione which is useful as an intermediate for preparing NFD, and an anticancer agent comprising 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione as an active ingredient. Said 2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione is obtained in 4 or 5 steps by using comparatively inexpensive 5-hydroxynaphthalene-1,4-dione (also referred to as juglone) as a starting material.

Abstract: The present invention provides a prophylactic or therapeutic agent for depression or anxiety disorders, comprising (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide.

Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.

Abstract: The present application relates to a novel cyclopenta[b]benzofuran derivatives, processes for their preparation and their use for the manufacture of medicaments, in particular for the prophylaxis and/or therapy of acute or chronic disorders characterized by elevated cellular stress, by local or systemic inflammatory processes or by hyperproliferation.

Abstract: The present invention is directed to the diastereoisomeric mixture and the individual isomeric components of the formula:

Abstract: An object of the present invention is to provide a method for efficiently preparing (S)-2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]-furan-4,9-dione useful as a medicine at a low cost and in large amounts. According to the present invention, the desired (S)-2-(1-hydroxyethyl)-5-hydroxynaphtho[2,3-b]furan-4,9-dione can be prepared with high efficiency at a low cost and in large amounts by asymmetrically reducing 2-acetyl-5-hydroxynaphtho[2,3-b]furan-4,9-dione in the presence of an asymmetric ruthenium complex and a hydrogen donor.

Abstract: A compound of formula (X): wherein R1, R2, equal to or different from each other are hydrogen or a linear or branched saturated or unsaturated C1-C20-alkyl, C3-C20-cycloalkyl, C6-C20-aryl, C7-C20-alkylaryl or C7-C20-arylalkyl radical, optionally containing heteroatoms belonging to groups 13-17 of the Periodic Table of the Elements; or they can form a C4-C7 ring optionally containing O, S, N, P or Si atoms that can bear substituents; R3 is hydrogen or a linear or branched saturated or unsaturated C1-C20-alkyl, C3-C20-cycloalkyl, C6-C20-aryl, C7-C20-alkylaryl or C7-C20-arylalkyl radical, optionally containing heteroatoms belonging to groups 13-17 of the Periodic Table of the Elements; or two adjacent R3 groups can form a C4-C7 ring optionally containing O, S, N, P or Si atoms, wherein said ring can bear substituents; and at least one of R1, R2 or R3 is different from hydrogen.

Abstract: Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Abstract: Provided are intermediates and processes for preparation of Ramelteon.

Abstract: The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-?B-dependent conditions.

Abstract: Compounds of the general formula (I); wherein the substituents are as defined in claim 1, are useful as fungicides.

Abstract: Robust sustained release formulations, solid dosage forms comprising robust sustained release formulations, and methods for making and using these formulations and solid dosage forms are provided. Robustness of the sustained release formulation is related to the particle size of the hydrophilic gum. Sustained release formulations resist dose-dumping when ingested with alcohol. The formulations are useful for treating a patient suffering from a condition, e.g., pain. The formulations comprise at least one drug. In one embodiment, the drug is an opioid, e.g., oxymorphone.

Abstract: The present invention provides a process for preparing benzoprostacycline derivatives of formula (1), i.e. 5,6,7-trinor-4,8-inter-m-phenylene PGI2 derivatives, and vinyl tin compounds of formula (III) as starting materials for the same.

Abstract: Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Abstract: In the compound of the formula (I), where: R1, R2 are each independently, for example, H or a straight-chain or branched alkyl radical p, q are each independently 0 or 1, i.e. at the value zero, —H is present at the appropriate position instead of —F M1 is —CO—O—, —O—CO—, —CH2—O—, —O—CH2—, —CF2—O—, —O—CF2—, —CH?CH—, —CF?CF—, —C?C—, —CH2—CH2—CO——O—, —O—CO—CH2—CH2—, —CH2—CH2—, —CF2—CF2—, —(CH2)4—, —OC(?O)CF?CF— or a single bond A1 is, for example, 1,4-phenylene R5 has the same possible definitions as specified for R1 and R2, with the exception of —M1—A1—R5, but independently of the definition of R1 and R2 X is H, F, OF3, CF3, OCF2H with the following provisos: a) at least one of p, q has to be 1 b) R1 and R2 must not at the same time be H c) R2 and X must not at the same time be H.

Abstract: Novel quinones are provided, as well as compositions comprising these novel quinones. Methods of using the novel quinones in treatment of various indications including cancer are also provided.

Abstract: A process for preparing cyclopentadiene derivatives comprising the steps of: a) coupling a five membered heterocycle ring with a five or six membered heterocycle ring; b) reacting the obtained compound with a carbonilating system: c) reducing the obtained compound.

Abstract: A metallocene compound of formula (I): wherein M is zirconium, titanium and hafnium; X is a hydrogen atom, a halogen atom or a hydrocarbon radical; R1 is a linear C1-C20-alkyl radical; R2 is a hydrogen atom or hydrocarbon R3, R4, R5, R6, R7, and R8, are hydrogen atoms or hydrocarbon radicals, A is a sulphur (S) atom or an oxygen (O) atom; Q is a radical of formula (II), (III) or (IV) being bonded to the indenyl at the position indicated by the symbol *; (II), (III), (IV) wherein T1 is a sulphur atom, an oxygen (O) atom or a NR; R9, R10 and R11 are hydrogen atoms or hydrocarbon radicals; T2, T3, T4, T5, and T6 are carbon atoms (C) or nitrogen atoms (N); m1, m2, m3, m4 and m5 are 0 or 1; R12, R13, R14, R15 and R16 are hydrogen atoms or hydrocarbon radicals with the provisos that at least one of R12, R13, R14, R15 and R16 is different from hydrogen atoms, and that no more than two of T2, T3, T4, T5 and T6 are nitrogen atoms.

Abstract: This invention relates to a novel fused tricyclic heterocycle of the formula (Ia, Ib) and its use for the treatment of hyper-proliferative disorders

Abstract: The invention relates to a method for the synthesis of galanthamifle, the derivatives and analogues thereof of formula (1) where R1=a hydrogen atom.

Abstract: The invention relates to fluorinated aromatics of the formula (I) where X is CH2, C?O, CF2, O or S, Y is H or F, with the proviso that Y has to be F when X is CH2, and where the other parameters are as defined in claim 1, and also to their use in liquid-crystal mixtures, and also to liquid-crystal mixtures comprising these compounds and to liquid-crystal displays comprising these mixtures.

Abstract: The present invention relates to a new process for the preparation of beraprost of formula (I) using new intermediates.

Abstract: This invention provides novel compounds possessing antibacterial and/or antifungal and/or antitumor activity. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.

Abstract: The invention relates to cyclopentabenzofuran derivatives, process for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-?B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.

Abstract: The subject invention provides novel compositions of biologically active linderazulene terpene compounds which can advantageously be used for treating cancer and stopping cell proliferation.

Abstract: Novel quinones are provided, as well as compositions comprising these novel quinones. Methods of using the novel quinones in treatment of various indications including cancer are also provided.

Abstract: The present invention relates to a new process for the preparation of beraprost of formula (I) using new intermediates.

Abstract: The present invention provides compounds and methods of administering compounds to a subject taht can reduce &bgr;APP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce &bgr;APP production and that is not tocix in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease &bgr;APP production.

Abstract: The invention relates to fluorinated aromatics of the formula (I) 1

Abstract: The present invention provides compounds having a cyclopentabenzofuran core and the use of such compounds in therapy as well as compositions comprising said compounds.

Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders.

Abstract: A method of inhibiting mammalian C—C chemokine production by using a mammalian C—C chemokine synthesis inhibitor containing a prostaglandin I derivative as an active component to treat a variety of circulatory diseases, inflammation, allergic diseases, and renal diseases.

Abstract: The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description

Abstract: The invention relates to compounds of formula (I): and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.

Abstract: The invention relates to the use of cycloventabenzofuran derivatives for the production of a medicament for the treatment of nuclear factor of &kgr;B-dependent diseases.

Abstract: The present invention offers a pericyte protective agent having a prostanoic acid derivative as the effective component. The pericyte protective agent to which the present invention relates is effective in the prevention and treatment of diabetic retinopathy, diabetic neuropathy, diabetic nephropathy and the like.

Abstract: The present invention relates to a C—C chemokine production inhibitor containing a prostanoic acid derivative as an active component, and a method of inhibiting C—C chemokine production by using the inhibitor. Medicines of the present invention are effective to cure circulatory diseases, inflammation, allergic diseases, renal diseases, etc.

Abstract: The invention concerns compounds of formula (I) in which: A forms a tricyclic system of formula A1, A2, A3 or A4; R1 represents a hydrogen atom, an alkyl, hydroxy, alkoxy or oxo group; (R2)m and (R3)m′ are such as defined in the description; n represents an integer such that 0≦n≦3; p represents an integer such as defined in the description; B represents a group (a) or (b). The invention is useful for preparing medicines.

Abstract: A compound selected from those of formula (I): wherein: denotes single bond or double bond, n is integer from 1 to 6 inclusive, R1, and R2 represent a group selected from hydrogen, linear or branched (C1-C6)-alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, X represents a group selected from —CH═CH—, oxygen, S(O)m wherein m is integer from 0 to 2 inclusive, and NR3 wherein R3 represents a group as defined in the description, Y represents CH or CH2 depending on whether denotes single bond or double bond, or may have the additional meaning of oxygen when X represents oxygen, T represents monocyclic or polycyclic (C3-C10)cycloalkyl optionally containing within the ring system oxygen, selenium, S(O)p, NR3, or SiR4R5 wherein p, R3, R4, and R5 are as defined in the description, its isomers and addition salts thereof with a pharmaceutically-accep

Abstract: Tricyclic sulfonamide compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: The invention relates to cyclopentabenzofuran derivatives, processes for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-&kgr;B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.