Abstract: The present application describes monocyclic and bicyclic lactams and derivatives thereof of Formulae Ia–e: wherein one of one of T1 and T2 is carbonyl, thiocarbonyl, or sulfonyl or pharmaceutically acceptable salt forms thereof. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1–R7, X1, X2, R, Q, and n are as defined herein.

Abstract: The invention relates to coagulation of the blood. Disclosed are novel compounds of formula (I), a method for the production of these compounds, pharmaceutical compositions containing them, and methods of using them for the prevention and/or treatment of various diseases.

Abstract: The invention relates to new crystalline forms I and II of (4R-cis)-6-[2-[3-phenyl-4-(phenyl-carbamoyl)-2-(4-fluoro-phenyl)-5-(1- methyl-ethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl-[1,3]dioxane-4-yl-acetic acid-tertiary butyl ester of the Formula (I) and a process for the preparation thereof.

Abstract: Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section:

Abstract: A process for the vapor phase ammoxidation of alkanes and olefins with a catalyst of the general empirical formula: VSbaMbQcOx wherein M is at least one element selected from magnesium, aluminum, zirconium, silicon, hafnium, titanium and niobium, Q is at least one element selected from rhenium, tungsten, molybdenum, tantalum, manganese, phosphorus, cerium, tin, boron, scandium, bismuth, gallium, indium, iron, chromium, lanthanum, yttrium, zinc, cobalt, nickel, cadmium, copper, strontium, barium, calcium, silver, potassium, sodium and cesium, a is 0.5 to 20, b is 2 to 50, c is 0 to 10 and x is determined by the valence requirements of the elements present. The process has a co-feed of gaseous carbon dioxide with an alkane (paraffin) and/or alkene, ammonia and an oxygen-containing gas which react in the presence of the catalyst to form a nitrile and by-products.

Abstract: The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.

Abstract: The invention provides compounds of general formula (I), in which m, n, Z1, Z2, R1, R2, R3, R4 and R5 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; and their use in therapy

Abstract: A compound of formula (I) F wherein R1 represents a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; x represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: —CO—, —CS—, —CR4(OR5)— or —NR6— wherein each of R4 and R6 represents a hydrogen atom or a hydrocarbon group which may be stubstituted, R5 represents a hydrogen atom or a protective group for a hydroxyl group; m represents an integer of 0 to 3; Y represents an oxygen atom, a sulfur atom, or a group of the formula: —SO—, —SO2—, —NR7—, —CONR7— or —NR7CO— wherein R7 represents a hydrogen atom or a hydrocarbon group which may be substituted; ring A represents an aromatic ring which may further have 1 to 3 substituents; n represents an integer of 1 to 8; ring B represents a nitrogen-containing 5-membered hetero ring which may further be substituted by an alkyl group.

Abstract: The invention relates to compounds of formula (I) pharmaceutical compositions containing the same as well as methods of treating patients suffering from a condition susceptible to amelioration by a Factor Xa inhibitor using the same.

Abstract: Novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism, and cancer metastasis include compounds represented by the following general formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof: wherein each of n1, n2, and n3 is an integer of 1; each of R1, R2, R3, R4, R5, and R6 is independently a hydrogen atom; A1 is imidazole; A2 is imidazole or imidazole substituted with an alkyl group; W is a phenyl group or naphthyl group; X is CH2; D is a group represented by -Q-Y—B, wherein Q is NR12 and R12 is a hydrogen atom or an alkyl group; Y is (CH2)m3 and m3 is an integer of 2 to 4; and B is N(R25R26), wherein each of R25 and R26 are independently a hydrogen atom, a C1–C6 alkyl group or a C3–C6 cycloalkyl group.

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: Crystalline forms of the compounds (R)-2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole and the monohydrochloride thereof, processes for the preparation thereof and the use thereof as pharmaceutical compositions.

Abstract: Compounds having general formula (I) are described, together with their use for the control of phytopathogenic fungi

Abstract: The present invention relates to a new manufacturing method for phosphonate esters, which have utility as a carbon-carbon binding formation agent, as well as a synthesis intermediate for biologically active substances such as medical drugs and agri-chemicals. Specifically the present invention relates to a new industrially advantageous manufacturing method for phosphonate esters in which the phosphonate esters of the subject can be efficiently obtained with a high yield rate through a simple operation while having barely any side reaction or sub-product. More specifically, the present invention pertains to a manufacturing method for phosphonate esters in which secondary phosphonate esters and alkene compounds are reacted in a transition metal catalyst. In addition the present invention relates to a new manufacturing method for allylphosphonate esters in which secondary cyclic phosphonate esters and 1,3-diene compounds are reacted in a palladium catalyst.

Abstract: A method is provided for synthesizing acylamides, useful as protectant for cultivated plants. A benzoxazine, such as 3,4-dihydro-3-methyl-2H-1,4-benzoxazine, is made in a stepwise manner by initially forming an o-nitrophenoxyketone by reacting a haloketone and a nitrophenol. The o-nitrophenoxyketone is hydrogenated to form the corresponding benzoxazine, which is thereafter acylated with an acylhalide to produce the acylamide, such as 4-dichloroacetyl-3,4-dihydro-3-methyl-2H-1,4-benzoxazine.

Abstract: Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Abstract: Compounds of Formula (I), and their N-oxides and suitable slats, are disclosed which are useful as invertebrate pest control agents, wherein A and B are independently O or S; E is C or N; J is a phenyl ring, a naphthyl ring system, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused heterobicyclic ring system wherein each ring or ring system is optionally substituted with 1 to 4 R5; K is taken together with the two contiguous linking carbon atoms to form a 5- or 6-membered nanoaromatic carbocyclic or heterocyclic ring optionally including one or two ring members selected from the group consisting of C(?O), SO or S(O)2, each ring optionally substituted with 1 to 4 R4; and R1, R2, R3, R4 and R5 are as defined in the disclosure.

Abstract: A method of making a metal complex comprises combining a 1-monoacyldipyrromethane with a compound of the formula R1R2MX, wherein M is boron, R1 and R2 are each independently organic substituents; and X is an anion leaving group; to produce a metal complex of the formula DMR1R2 wherein DH is a 1-monoacyldipyrromethane. The methods and complexes are useful for the purification and synthesis of dipyrromethanes and porphyrins.

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.