Abstract: A thiazoline derivative represented by Formula (I): wherein R is a cyclic hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; X is a bond or a divalent chain hydrocarbon group which may be substituted; X? is a bond or —N(R5)—; Y is a divalent hydrocarbon group which may be substituted; Y? is a bond or —C(?O)—; ring A is a nitrogen-containing heterocycle which may be substituted; Z1 and Z3 are each independently a bond or a divalent chain hydrocarbon group which may be substituted; Z2 is a bond or —N(R6)—; and B is a group represented by the formula: which is useful as a therapeutic drug for thrombosis, is provided.

Abstract: The present invention relates to novel 3,5-substituted 7-azaindole compounds of formula (I), their use in the inhibition of c-Jun N-terminal kinases, their use in medecine and particularly in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation. The invention also provides processes for manufacture of said compounds, compositions containing them and processes for manufacturing such compositions.

Abstract: The present invention provides a filter for electronic display devices, comprising a squarylium compound represented by General Formula (I): [wherein R1 and R2 may be the same or different and each represents a hydrogen atom, an alkyl group optionally having substituent(s), an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), or a heterocyclic group optionally having substituent(s); X represents a group represented by following Formula (A): (wherein R3 and R4 may be the same or different and represents a hydrogen atom, an alkyl group optionally having substituent(s), an alkoxy group optionally having substituent(s), an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), or a heterocyclic group optionally having substituent(s), wherein R3 and R4 may be combined together with the adjacent nitrogen atom thereto form a heterocyclic group optionally having substituent(s))].

Abstract: Azole compounds represented by formula I: wherein ring A is isoxazole and the like, R1 is a substituted or unsubstituted aryl group and the like, R2 is a hydrogen atom and the like, and R3 is a substituted or unsubstituted alkyl group and the like, and pharmaceutically acceptable salts thereof inhibit the physiological activity of lysophosphatidic acid (LPA), and are useful as for the prophylaxis or treatment of diseases in which inhibition of the physiological activity of LPA is useful for the prophylaxis or treatment thereof, such as diseases involving the LPA receptor.

Abstract: The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.

Abstract: The present invention relates to 1,2,4-tri-substituted imidazoline derivatives, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazoline derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these imidazoline derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.

Abstract: The present invention provides an azolylacylquanidine compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.

Abstract: A compound represented by the following general formula (I) or a salt thereof [R1 represents hydrogen atom, or a C1-12 alkyl group; R2 represents a C1-12 alkyl group having one or more maleimide groups, an aryl group having two or more maleimide groups, a group represented by the formula (A): —(CH2)n—CO—N(R11)(R12) (R11 and R12 represent hydrogen atom, a C1-12 alkyl group, a C1-12 alkyl group having one or more maleimide groups, or an aryl group having one or more maleimide groups, and n represents an integer of 1 to 6), or a group represented by the formula (B): —(CH2)m—NH—CO—R13 (R13 represents a C1-12 alkyl group having one or more maleimide groups, or an aryl group having one or more maleimide groups, and m represents an integer of 1 to 6); R3 and R5 represent hydrogen atom, or a halogen atom; R4 represents hydroxyl group, a C1-12 acyloxy group, a C1-12 acyloxymethyloxy group, or an amino group], which is useful as a novel fluorescent labeling agent having a property of emitting intense fluorescence only

Abstract: The present invention provides novel fluorosulfonic acids and salts thereof having greater stability and higher acidity than conventional fluorosulfonic acids; and synthetic intermediates thereof. The invention also provides processes for producing novel fluorosulfonic acids from which various derivatives can be easily synthesized; and uses of these fluorosulfonic acids. Specifically, the invention provides a compound represented by formula (1): R—S(?O)n—CF2—SO3H??(1) wherein R is a group bound to an adjacent sulfur atom through a carbon atom, examples of R being an optionally substituted alkyl group, an optionally substituted haloalkyl group, an optionally substituted alkenyl group, an optionally substituted haloalkenyl group, an optionally substituted alkynyl group, an optionally substituted haloalkynyl group, an optionally substituted cycloalkyl group, etc.; and n is 1 or 2. The invention also provides salts of such a compound, etc.

Abstract: This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylococcus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.

Abstract: 1,2,4-Tiazole-5-ones useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Abstract: There is provided a series of novel phenylcarboxyamides of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and Y as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

Abstract: An alkyl ether derivative represented by the general formula: wherein each of R1 and R2 represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 is an alkylamino group, an amino group, a hydroxyl group or the like; the ring A is a 5-membered or 6-membered heteroaromatic ring or a benzene ring; each of m and n is an integer of 1 to 6; and p is an integer of 1 to 3, or its salt has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is useful as a therapeutic agent for diseases in central and peripheral nerves.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: A process for preparation of crystalline perindopril erbumine of formula (II) which exhibits the X-ray (powder) diffraction pattern like that shown in FIG. 2 The process comprises reacting a solution of perindopril of formula (I), in a solvent selected from N,N-dimethylformamide, dimethyl acetals of lower aliphatic aldehydes, dimethyl ketals of lower aliphatic ketones and 1,2-dialkoxyethane with tertiary butylamine and crystallization of the erbumine salt thus obtained by heating the reaction mixture to reflux, filtering hot, cooling gradually to 20° C. to 30° C., and further cooling to 0° C. to 15° C. for 30 minutes to 1 hour and finally filtering off and drying the crystals.

Abstract: The invention relates to compounds of formula (I), where the groups have the meanings set forth herein and the physiologically-acceptable salts thereof. The compounds are suitable as medicaments for lowering blood sugar levels and for prevention and treatment of diabetes.

Abstract: Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo-2-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 ?-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxy-propionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products.

Abstract: An electronic device comprising a polymer of Formula or structure (I) wherein R1 is hydrogen, halogen, a suitable hydrocarbon, or a heteroatom containing group; R2 is hydrogen, a suitable hydrocarbon, a heteroatom containing group, or a halogen; R3 and R4 are independently a suitable hydrocarbon, hydrogen, a heteroatom containing group, or a halogen; Ar is an aromatic component; x, y, a, b, and c represent the number of groups or rings, respectively; Z represents sulfur, oxygen, selenium, or NR wherein R is hydrogen, alkyl, or aryl; and n represents the number of repeating units.

Abstract: A pyrazole compound of formula (a): wherein R1 represents C1-C4 alkyl or trifluoromethyl, R2 represents C1-C4 alkyl, R3 represents hydrogen or C1-C6 alkyl; R4 represents halogen and so on, m represents 0 to 4 integer; R5 represents halogen and so on, n represents 0 to 4 integer; R6 and R7 are same or different and represents hydrogen, halogen or methyl; X represents oxygen or R8O—N; R8 represents hydrogen, C1-C6 alkyl and the like; has an excellent controlling activity against noxious arthropods.

Abstract: The invention encompasses processes for the preparation of darifenacin hydrobromide.