Abstract: A variety of diseases and disorders associated with the metabolic pathways involved in the activities of cyclooxygenase and the synthesis of prostaglandins, for example type 2 diabetes mellitus and its sequelae, ischemic vascular diseases, pain associated with inflammation, inflammatory skin conditions, spinal cord injury, peripheral neuropathy, multiple sclerosis, inflammatory bowel disease and rheumatoid arthritis, as well as various types of cancer may be treated or prevented by the use of an agent which selectively enhances production of 15-deoxy-prostaglandin J2.

Abstract: The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin- 4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and are as described herein.

Abstract: A compound having the formula (I) wherein ring A represents a substituted or unsubstituted monocyclic or multicyclic ring; m=any positive integer; n=0-5; X=CH and Y=—C(O)NR1R2, —NR1R2 or —S(O)2R4, where R1, R2 and R4 are each individually selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring, or any combination thereof, or R1 and R2 are linked so as to form part of a substituted or unsubstituted heterocyclic ring, or X=N and Y=—S(O)2R3 or —C(O)R3, where R3 is selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted amine, substituted or unsubstituted carbocyclic ring, substituted or unsubstituted heterocyclic ring or any combination thereof.

Abstract: Fluorous-tagged oligonucleotide reagents and an oligonucleotide purification methodology making use thereof, the method comprising: Synthesizing oligonucleotides using oligonucleotide reagents each bearing at least one fluorous group to yield a mixture of synthesis products and reagents, the mixture including at least one target synthesized oligonucleotide bearing at least one fluorous group; passing the mixture through a separation medium having an affinity for the at least one fluorous group so that the target synthesized oligonucleotide bearing at least one fluorous group is adsorbed by the separation medium; washing the separation medium with at least a first solvent to selectively dissociate therefrom substantially all synthesis products and reagents of the heterogenous mixture other than the at least one target synthesized oligonucleotide bearing at least one fluorous group; and subsequently dissociating the at least one synthesized oligonucleotide from the separation medium, with or without the fluorou

Abstract: Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH2—; R is a mono- to tetra-substituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl-C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R ; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n=0, 1 or 2; m=0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.

Abstract: The present invention relates to a compound having benzopyran core, a preparation method of the derivatives by liquid phase synthesis and solid phase synthesis through diversity-oriented synthesis, and an anticancer agent comprising the compound that exhibit excellent cytotoxicity against cancer cells.

Abstract: There are provided compounds of the general formulas wherein X, Y, R1, R2, R3 and R4 are as described herein. The compounds exhibit anticancer activity.

Abstract: The disclosure relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I) in which J, X, Y, m and CKE are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the disclosure relates to selective herbicidal compositions comprising, firstly, the cycloalkylphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The disclosure furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.

Abstract: The present invention relates to a 11?-hydroxysteroid dehydrogenase 1 inhibitor comprising a compound represented by the formula (1): wherein each symbol is as defined in the description, or a salt thereof, or a prodrug thereof. The 11?-hydroxysteroid dehydrogenase 1 inhibitor of the present invention has a superior activity, and is useful as a pharmaceutical agent such as agents for the prophylaxis or treatment of diabetes, insulin resistance, obesity, abnormal lipid metabolism, hypertension and the like, and the like.

Abstract: Compounds of formula (I): [in which: X is a group of formula >CR1R2 or >SO2; Y is a group of formula >NH or >CR1R2; Z is a group of formula >C?O or >CH2 or a direct bond; R1 is hydrogen and R2 is hydrogen, carboxy or hydroxy; or R1 and R2 together represent an oxo group, a methylenedioxy group or a hydroxyimino group; R3 is hydrogen or lower alkyl; R4 represents two hydrogen atoms, or an oxo or hydroxyimino group; R5 is hydrogen, lower alkyl or halogen; R6 is hydrogen, lower alkoxy or carboxy; R7 and R8 are each hydrogen, lower alkyl or halogen; and pharmaceutically acceptable salts and esters thereof can be used for the treatment or prophylaxis of acute or chronic neurodegenerative diseases or conditions such as Alzheimer's Disease, Parkinson's Disease, Huntington's Chorea, Multiple Sclerosis or the sequelae to acute ischaemic events such as heart attack, stroke or head injury and for protection against ischaemic damage to tissues of peripheral organs.

Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

Abstract: [Object] To provide a substituted cycloalkene derivative having an action to suppress intracellular signal transduction or cell activation induced by endotoxin and to suppress cell responses due to the intracellular signal transduction and cell activation such as an excess generation of inflammatory mediators such as TNF-?, pharmacologically acceptable salts therefor, a medicament containing them as an active ingredient, a preparation method therefor, and a medicament containing the aforementioned substituted cycloalkene derivative as an active ingredient which is superior in prophylaxis and/or treatment of diseases such as sepsis (septic shock, disseminated intravascular coagulation, multiple organ failure and the like), that are associated with intracellular signal transduction or cell activation induced by endotoxin and to cell responses to the intracellular signal transduction and cell activation.

Abstract: Various non-limiting embodiments disclosed herein relate generally to photochromic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. Other non-limiting embodiments relate to photochromic-dichroic compounds, which may be thermally reversible or non-thermally reversible, and articles made therefrom. For example, one non-limiting embodiment provides a thermally reversible, photochromic compound adapted to have at least a first state and a second state, wherein the thermally reversible, photochromic compound has an average absorption ratio greater than 2.3 in at least one state as determined according to CELL METHOD.

Abstract: Provided are an organic electroluminescence device and an aromatic amine derivative for realizing the device. The aromatic amine derivative improves the luminous efficiency of an organic electroluminescence device using the derivative, and its molecules hardly crystallize. The organic electroluminescence device has an organic thin film layer composed of one or a plurality of layers including at least a light emitting layer, the organic thin film layer being interposed between a cathode and an anode, and at least one layer of the organic thin film layer, especially a hole transporting layer contains the aromatic amine derivative alone or as a component of a mixture, so the organic electroluminescence device can be produced in improved yield, and has a long lifetime.

Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.

Abstract: The present invention provides methods of parasitic infections, thymoma, and lymphoid malignancies in a subject by administering to the subject a therapeutically effective amount of one or more of the compounds of the invention.

Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a method for producing them, pharmaceutical compositions containing them, and methods of using them.

Abstract: Compounds useful in the fluorescent labeling of biological materials are provided along with methods for their use and preparation.

Abstract: Spirocyclic cyclohexane compounds corresponding to formula I a process for manufacturing such compounds, pharmaceutical compositions that contain such compounds, and the use of such spirocyclic cyclohexane compounds for the production of pharmaceuticals, and particularly for the treatment of pain.

Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.

Abstract: Compounds of formula (I): wherein: X1 represents an atom or group selected from CR4aR4b, O, S(O)q1 and NR5, wherein R4a, R4b, q1 and R5 are as defined in the description, m1 represents zero or an integer from 1 to 4 inclusive, m2 represents an integer from 1 to 4 inclusive, n1 and n2, which may be identical or different, each represent an integer from 1 to 3 inclusive, R1 represents hydrogen or a group selected from carboxy, alkoxycarbonyl, optionally substituted carbamoyl and optionally substituted alkyl, R2 represents hydrogen or alkyl, Ak represents an optionally substituted alkylene chain, p represents zero, 1 or 2, R3 represents hydrogen or cyano, X2 and X3, which may be identical or different, each represent either S(O)q2, or CR6aR6b, wherein q2, R6a and R6b are as defined in the description, its optical isomers, where they exist, and its addition salts with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful as DPP-IV inhibitors.

Abstract: A method for the production of acetals and ketals of 3-amino-5-(hydroxymethyl) cyclopenlane-1,2-diols of formula (I): (and/or the enantiomer), where R1 is H, C1-6-alkyl, C3-8-cycloalkyl or benzyl and (i) R2 is methyl and R3 is ethyl, (ii) R2 is H and R3 is C1-6-alkyl or phenyl or (iii) R2 and R3 together form a group of formula —(CH2)n— with n=4 to 6, present as free amines or as salts of di- or tri-basic organic acids, starting from 2-acetyl-2-aza-bicyclo[2.2.1]hept-5-en-3-one of formula (II): (and/or the enantiomer). The method is equally useful, depending on the starting material, for the production of enantiomerically-pure compounds, or mixtures with arbitrary enantiomeric content.

Abstract: A compound represented by, e.g. the formula (I): [wherein X, Y, Z, and W each independently represent optionally substituted methine; A, B, and D each independently represent —C(O)—, etc.; Q represents a methine or a nitrogen; and R represents the formula (II-1), optionally substituted with lower alkyl, etc.; (wherein R6 represents a lower alkyl, etc; and R7 and R8 each independently represents a lower alkyl, etc.)] or a pharmaceutically acceptable salt of the compound. The compounds and salt have antagonistic activity against a histamine H3 receptor or inverse agonistic activity against a histamine H3 receptor. They are useful in the prevention or treatment of metabolic diseases, circulatory diseases, or neurotic diseases.

Abstract: Compounds of formula (I): are useful in the treatment of diseases associated with deposition of ?-amyloid in the brain.

Abstract: Compounds of formula (I): [in which: X is a group of formula >CR1R2 or >SO2; Y is a group of formula >NH or >CR1R2; Z is a group of formula >C?O or >CH2 or a direct bond; R1 is hydrogen and R2 is hydrogen, carboxy or hydroxy; or R1 and R2 together represent an oxo group, a methylenedioxy group or a hydroxyimino group; R3 is hydrogen or lower alkyl; R4 represents two hydrogen atoms, or an oxo or hydroxyimino group; R5 is hydrogen, lower alkyl or halogen; R6 is hydrogen, lower alkoxy or carboxy; R7 and R8 are each hydrogen, lower alkyl or halogen; and pharmaceutically acceptable salts and esters thereof can be used for the treatment or prophylaxis of acute or chronic neurodegenerative diseases or conditions such as Alzheimer's Disease, Parkinson's Disease, Huntington's Chorea, Multiple Sclerosis or the sequelae to acute ischaemic events such as heart attack, stroke or head injury and for protection against ischaemic damage to tissues of peripheral organs.

Abstract: The invention relates to intermediate compounds of the formula wherein R1 is H or a protecting group, R2 and R3 each independently represent H, methyl, or a leaving group, provided that at least one, but not both, of R2 and R3 is a leaving group. The intermediate compounds are useful for the synthesis of discodermolide, its derivatives, and related compounds.

Abstract: Spirocyclic cyclohexane compounds, methods for their production, pharmaceutical compositions containing these compounds, and the use of these spirocyclic cyclohexane compounds for treating conditions associated with the nociceptin/ORL1 receptor system, e.g. pain, drug withdrawal, anxiety, etc.

Abstract: The invention relates to novel 3-phenyl-substituted, 3-substituted 4-ketolactams and -lactones of the formula (I) in which Q, W, X, Y, A, B and G are as defined in the disclosure, to processes and intermediates for their preparation and to their use as pesticides and herbicides.

Abstract: The invention relates to intermediate compounds of the formula wherein R1 is H or a protecting group, R2 and R3 each independently represent H, methyl, or a leaving group, provided that at least one, but not both, of R2 and R3 is a leaving group. The intermediate compounds are useful for the synthesis of discodermolide, its derivatives, and related compounds.

Abstract: The present invention discloses synthesis of 2,2?-disubstituted 9,9?-spirobifluorene-based triaryldiamine. First, 2,2?-diamino-9,9?-spirobifluorene, a Pd-catalyst as auxiliary and aryl halide BX are provided, wherein X is selected from the group consisting of: Cl, Br and I, B comprises one of the following group: aryl moiety, hetero cycle, multiple fused ring, multiple fused ring with hetero atom(s). Next, a substitution reaction is performed to react the 2,2?-diamino-9,9?-spirobifluorene with the aryl halide BX to produce the 2,2?-disubstituted 9,9?-spirobifluorene-based triaryldiamines. In addition, the present invention discloses organic light emitting devices comprising hole transporting material comprising 2,2?-bis(N,N-disubstituted amino)-9,9?-spirobifluorenes.

Abstract: The present invention relates to spirocyclic cyclohexane compounds, to methods for their production, to pharmaceutical compositions containing these compounds, to methods of treatment using such compounds and to the use of such spirocyclic cyclohexarie compounds for producing pharmaceutical compositions.

Abstract: The present invention relates compounds of the formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, and R10 represent a variety of substituents; A represents NR9 or O; B represents a bond, CH2, NR9 or O, wherein one or both hydrogen atoms in said CH2 moiety may be replaced with one or both of R7 and R8, or alternatively, one of the hydrogen atoms in said CH2 moiety together with a hydrogen atom from an adjacent carbon are replaced by a double bond; with the proviso that when A is O, then B is NR9; n is zero, 1 or 2; and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides a method for making substituted indole compounds of general formula III comprising the step of: (a) reacting a 2-bromoaniline or 2-chloroaniline of general formula (I) (I) wherein: X, R and R1 are defined herein with a substituted acetylene of formula (II) wherein R2 and R3 are defined herein in the presence of a palladium catalyst, a ligand, and a base in a solvent at a suitable temperature to give a compound of formula (III);

Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceuticals compositions. Methods of treatment and combinations with other agents are also disclosed.

Abstract: A process produces an optically active amine or its salt and includes the steps of reacting a ketone of Formula (1a): wherein R1 is typically an unsubstituted or substituted hydrocarbon group; and R2a is typically a hydrocarbon group having at least one oxo group and optionally having other substituent, with an optically active amine of Formula (2): wherein R3 is an unsubstituted or substituted aryl group; R4 is an unsubstituted or substituted lower alkyl group; and C1 is an asymmetric carbon atom, in the presence of an organic acid to thereby yield a corresponding optically active imine, hydrogenating the imine in the presence of a catalyst to yield a corresponding amine, subjecting the amine or its salt to hydrogenolysis in the presence of a catalyst, and reducing the hydrogenolyzed product with a reducing agent.

Abstract: The present application describes novel spiro-cyclic ?-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms a 3-11 membered spiro-carbocycle or spiro-heterocycleon ring B, and the other variables are defined in the present specification, which are useful as as matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), and/or aggrecanase inhibitors.

Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.

Abstract: Compounds of Formula I and the pharmaceutically acceptable salts and esters thereof, wherein Z is selected from the group consisting of: (a) Formula Ia ?and (b) Formula Ib are novel LXR agonists and are useful in the treatment of dyslipidemic conditions particularly depressed levels of HDL cholesterol.

Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.

Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.

Abstract: Spiro compounds of the formula (I), in which at least one of the radicals K1, L, M, N1, R1, R2, R3, R4 is one of the following groups are suitable as charge transport materials, in particular for photovoltaic cells, and as electroluminescence materials.

Abstract: This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.

Abstract: The present invention relates to spirobenzofuran lactam derivatives of the formula I 1

Abstract: The present invention relates to therapeutically active novel spiro[2,4]heptane amino carboxy compounds and derivatives thereof. Also provided is a method of preparing compounds of Formula (I), and pharmaceutical compositions comprising the compounds. The novel compounds act as modulators of metabotropic glutamate receptors and, as such, are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.

Abstract: Photochromic pyran compounds and their use in synthetic resin objects of all types, especially for ophthalmic applications, particularly spiro compounds having a fluorene structure derived from naphthopyrans, which are known as spirofluorenopyrans. By introducing respectively only one strongly electron donating or withdrawing group at specific positions in the periphery of the pyran dye, photochromic compounds obtained which in the excited state are distinguished by an expanded color spectrum, while simulataneously offering comparably good bleaching rates and good durability.

Abstract: The present invention relates to a photochromic spirobenzopyran compound of the formula (1) and its derivatives, a spirobenzopyran group having unsaturated terminal groups, a polymer prepared therefrom, a method for the production thereof, a composition comprising said spirobenzopyran or said spirobenzopyran group-containing polymer and a photochromic switch film using the same: 1

Abstract: The present application describes novel spiro-cyclic &bgr;-amino acid derivatives of formula I: 1

Abstract: The present invention provides compounds of general formula I or II: wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I or II, intermediates and processes useful for preparing compounds of formula I or II, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I or II.

Abstract: A compound of formula (I) or its enantiomers or diastereoisomers thereof: 1