Abstract: The invention relates to novel 1-(p-thienylbenzy)imidazoles of formula (I) where the radicals R(1) to R(6), X, and Y have the meaning indicated in the description, which are potent agonists of angiotensin (1-7) receptors and owing to the production and release of the vasorelaxant, antithrombotic, and cardioprotective messengers cyclic 3′,5′-guanosine monophosphate (cGMP) and nitrogen monoxide (NO) associated with the stimulation of these receptors on endothelial cells are valuable pharmaceuticals for the treatment and prophylaxis of high blood pressure, cardiac hypertrophy, cardiac insufficiency, coronary heart diseases such as angina pectoris, cardiac infarct, vascular restenosis after angioplasty, cardiomyopathies, endothelial dysfunction or endothelial damage, e.g., as a result of arteriosclerotic processes or diabetes mellitus, and also of arterial and venous thromboses.

Abstract: The present invention relates to novel [(2-substituted-5-[3-thienyl])-benzyl]-[2-([2-isopropoxy-5-fluoro]-phenoxy)-ethyl]-amine derivatives having formula (1) and the use thereof as medicaments, especially anti-psychotic medicaments.

Abstract: An epoxycyclododecane compound is produced by a catalytic hydrogenation reaction of 1,2-epoxy-5,9-cyclododecadiene, using a specific platinum-containing catalyst having a long life, under a hydrogen gas pressure of 0.8 to 9 MPa, and with a high yield of the target compound.

Abstract: The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N,O and S and which may be substituted with oxo or (1-6C) alkyl; R1, R2 and R3 are independently H, (1-6C) alkyl, (1-6C) alkoxy,(1-6C) alkoxy-(1-6C) alkyl, carbo(1-6C) alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrrolidin and 3-(5,6,7,8-tetrahydro-napth-1-yl-oxy)-pyrrolidin. The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.

Abstract: This invention relates to novel xanthone compounds, their preparation and use as medicament. More particularly this invention is directed to the isolation of the novel xanthone natural product sootepenseone from Dasymaschalon sootepense Craib, Annonaceae, its identification and derivatization, and the use of sootepenseone and its derivatives as anticancer agents.

Abstract: The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.

Abstract: Novel 4-methylene-1,3-dioxolanes of the general formula I in which R1 denotes hydrogen or alkyl, X denotes a single bond, C1-C18 alkylene, cycloalkylene, arylalkylene, —CH2(OCH2CH2)n— or —CH2(OCH(CH3)CH2)n—, in which n is an integer from 1 to 100, and Z means a functional group selected from among —OH, —COOR′ or —OCOR′, in which R′ denotes hydrogen or C1-C8 alkyl, are described, as are a process for the production thereof and the intermediates used in this process.

Abstract: Norlabdane oxide, which is a well known fragrance material having ambergris-type odors, is prepared from 12-acetoxy-norlabdane oxide by a hydrogenation reaction.

Abstract: 4-substituted cyclohexanes substituted in the 1-position with quinazoline either directly or through a C1-C4alkyl, C1-C4alkenyl, C1-C4alkynyl, C1-C4alkoxy, amino, aminoC1-C4alkyl, hydroxyC1-C4alkyl, carbonyl, cycloC3-C6alkyl or aminocarbonyl chain are effective as NMDA NR2B antagonists useful for relieving pain.

Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.

Abstract: Pyrrole compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.

Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.

Abstract: The present invention provides a crystalline or crystallized acid addition salt of Losartan useful for obtaining highly pure 2-n-butyl-4-chloro-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol (Losartan), and a purification method of Losartan that includes production of the crystalline or crystallized acid addition salt.

Abstract: The present invention is related to a method for preparing lactam represented by the following formula: wherein R is C2-10 alkylene which may be optionally substituted with C1-6 alkyl or phenyl; R′ is a hydrogen atom, C1-6 alkyl, C1-6 hydroxyalkyl or phenyl. The method for preparing lactam comprises an amination reaction using crystalline aluminosilicate zeolites as catalysts under the condition of gas phase in the presence of (a) lactone, (b) amine and/or ammonia and (c) water.

Abstract: Processes for producing compounds of the formula (VI) are disclosed. Benzothiophenecarboxylic acid derivatives of the formula (I), which are useful as starting materials for producing drugs, are disclosed. Particularly, disclosed is a process for preparing 5-dydroxybenzo[b]-thiophene-3-carboxylic acid derivatives of the formula (VI), which are specific PGD2 antagonists are also disclosed.

Abstract: The invention relates to novel N-substituted indole-3-glyoxylamides, to processes for their preparation and to their pharmaceutical use. The compounds have antiasthmatic, antiallergic and immunosuppressant/immunomodulating actions.

Abstract: The invention is relative to a compound of formula (I) and its use as an inhibitor of the CCK-inactivating peptidase tripeptidyl peptidase (TPP II). The invention concerns in particular the treatment of eating disorder, obesity, psychotic syndrome and associated psychiatric disorders. It concerns also the cosmetic use of a compound (I) in particular to aid slimming.

Abstract: Optically pure thiazolidinedione alcohols and ethers, and synthetic intermediates for preparing said alcohols and ethers. These compounds have utility as hypoglycemic and hypocholesterolemic agents.

Abstract: The present invention relates to specific photochromic 3H-naphtho[2,1-b]pyran derivatives and to their use in plastics of all types, especially for ophthalmic purposes. In particular, the present invention relates to spiro compounds derived from naphthopyrans and having a fluorene structure, referred to as spirofluorenopyrans, in which an annelated ring system is joined by a spiro bond to the central carbon atom of the fluorene structure.

Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are represented by the following formula I: wherein wavy line attachments indicate either the alpha (&agr;) or beta (&mgr;) configuration; dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, R1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of —OR1 and —N(R1)2, Y is =O or represents 2 hydrogen radicals. Certain of the compounds represented by Formula I comprise another aspect of the present invention.