Abstract: Novel &bgr;-lactam compounds represented by the following general formula (I) or pharmaceutically acceptable salts thereof which are useful as serum cholesterol-lowering agents: (I) wherein A1, A3 and A4 represent each hydrogen, halogen, C1-5 alkyl, C1-5 alkoxy, —COOR1, a group represented by the following general formula (b): (b) wherein R1 represents hydrogen or C1-5 alkyl, or a group represented by the following general formula (a): (a) wherein R2 represents —CH2OH, —CH2OC(O)—R1 or —CO2—R1; R3 represents —OH or —OC(O)—R1; R4 represents —(CH2)kR5(CH2)l— wherein k and l are each 0 or an integer of 1 or above provided k+l is an integer of not more than 10; and R5 represents a single bond, —CH═CH—, —OCH2—, carbonyl or —CH(OH)—; provided that at least one of A1, A3 and A4 is a group represented by the above formula (a); A2 represents C1-5 alkyl, C1-5 alkoxy, C1-5 alkenyl, C1-5 hydroxyalkyl or C1-5 car

Abstract: Compounds of the formula I, for example, are disclosed, in which R1, R2, R3, R4, R5, and R6 independently of one another are (C0-C30)-alkylene-L or are the meanings given in the description, and where L is shown connected to (C0-C30)-alkylene as follows: where Rx, Ry, Rz have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics.

Abstract: The invention provides compositions and methods for isolating ligand binding polypeptides for a user-specified ligand, and for isolating small molecule ligands for a user-specified target polypeptide using an improved class of hybrid ligand compounds.

Abstract: It is an object of the present invention to provide a method for synthesizing &bgr;-lactams and a method for manufacturing &bgr;-lactams in water of high-temperature and under high-pressure, and the present invention relates to a &bgr;-lactam synthesis method which is characterized in that &bgr;-lactams are synthesized by reacting &bgr;-amino acids in water at high-temperature and under high-pressure, this method being further characterized in that &bgr;-lactams are synthesized at a high speed by cyclizing &bgr;-amino acids in water at high-temperature and under high-pressure in which the temperature range is 200° C. or higher and the pressure range is 10 MPa or greater, and the present invention also relates to a method for manufacturing &bgr;-lactams which is characterized in that &bgr;-lactams are synthesized by reacting &bgr;-amino acids in water at high-temperature and under high-pressure, and are then separated and purified using a column separation medium.

Abstract: Compounds of formula (I) are disclosed. The compounds inhibit the action of gamma secretase, and hence find use in the treatment and prevention of Alzheimer's disease.

Abstract: The present invention relates generally to processes for the efficient production optically active 3-substituted lactams of formula (I) 1

Abstract: The invention relates to novel substituted benzoylcyclohexenones of the formula (I), 1

Abstract: The use of azetidinone compounds that are inhibitors of cholesterol absorption as tools for discovering and characterizing proteins involved in trafficking or absorption of cholesterol and/or cholesteryl esters in biological systems is presented. These compounds can serve as tools for competitive binding assays to discover and characterize other chemical agents useful as cholesterol absorption inhibitors. New compounds of the present invention are also highly efficacious inhibitors of cholesterol absorption.

Abstract: There is disclosed an azetidinones compound of the formula (I): Wherein, R is hydrogen, or hydroxy protecting group, R1 and R2 are each independently alkyl of 1-15 carbon atoms, benzyl or cycloalkyl of 5-6 carbon atom which may have substituent(s), R3 is low alkyl, or low alkyl ester, R4 is aryl, or aryl substituted with halogen, alkoxy of 1-6 carbon atom, nitro groups which is useful as a synthetic intermediate of the 1′&bgr;-methylcarbapenem-type antibacterial agent.

Abstract: Epoxides, aziridines, thiiranes, oxetanes, lactones, lactams and analogous compounds are reacted with carbon monoxide in the presence of a catalytically effective amount of catalyst having the general formula [Lewis acid]z+{[QM(CO)x]w−}y where Q is any ligand and need not be present, M is a transition metal selected from the group consisting of Groups 4, 5, 6, 7, 8, 9 and 10 of the periodic table of elements, z is the valence of the Lewis acid and ranges from 1 to 6, w is the charge of the metal carbonyl and ranges from 1 to 4 and y is a number such that w times y equals z, and x is a number such as to provide a stable anionic metal carbonyl for {[QM(CO)x]w−}y and ranges from 1 to 9 and typically from 1 to 4.

Abstract: A NK1 antagonist having the formula (I), 1

Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the following: (a) an optionally substituted phenyl, (b) an optionally substituted 6-membered monocyclic aromatic group containing one, two, three or four nitrogen atom(s), (c) an optionally substituted 5-membered monocyclic aromatic group containing one heteroatom selected from O, S and N and optionally containing one, two or three nitrogen atom(s) in addition to said heteroatom, (d) an optionally substituted C3-7 cycloalkyl and (e) an optionally substituted benzo-fuzed heterocycle; R1 is hydrogen, C1-4 alkyl or halo; R2 and R3 are independently hydrogen, OH, C1-4 alkoxy, C1-4 alkyl or C1-4 alkyl substituted with halo, OH, C1-4 alkoxy or CN; X is independently selected from H, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, OH, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkylthio, NO2, NH2, di-(C1-4 al

Abstract: A process for the preparation of hydroxy and amino compounds, in which, in a first step, an aldehyde, ketone or imine is reacted in a Reformatsky reaction with a reactive halogen compound and zinc, in carboxylic esters as solvents, the reactive halogen compound being brought into contact with the zinc at the same time as or after contact with the aldehyde, ketone or imine, and in a second step, the reaction product of the first step is hydrolyzed.

Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1

Abstract: A process is provided for the preparation of cyclic lactams of formula (II): 1

Abstract: The invention relates to a method for producing cyclic lactams of formula (II) by reacting a compound (I) of formula (I) with water in the presence of an organic, liquid dilution agent in the liquid phase. In formula (II), n and m respectively can have the values 0, 1, 2, 3, 4, 5, 6, 7, 8 and 9 and the sum of n+m is at least 3, preferably at least 4 and R1 and R2 represent C1-C6 alkyl, C5-C7 cycloalkyl or C6-C12 aryl groups. In formula (I), R1, R2, m and n are defined as above and R represents nitrile, carboxylic acid amide and carboxylic acid groups. The inventive method is characterized in that a) compound (I) is reacted with water in the liquid phase in the presence of an organic, liquid dilution agent (III) to form a mixture (IV) containing a lactam (II) and said mixture (IV) is subjected to an aqueous treatment to obtain a two-phase system.

Abstract: Hypocholesterolemic substituted 2-azetidinone compounds of the formula: 1

Abstract: A first process for producing an optically active perfluoroalkylcarbinol derivative includes (a) reacting an optically active imine with a compound that is a hemiacetal of a perfluoroalkylaldehyde or a hydrate of a perfluoroalkylaldehyde to obtain a condensate; and (b) hydrolyzing the condensate under an acid condition. A second process for increasing optical purity of an optically active 4,4,4-trifluoro-3-hydroxy-1-aryl-1-butanone derivative includes (a) precipitating a racemic crystal of the derivative, from the derivative; and (b) removing the racemic crystal from the derivative. A third process for increasing optical purity of the butanone derivative includes recrystallizing the derivative. Novel compounds are optically active and inactive 4,4,4-trifluoro-3-hydroxybutanoic aryl ester derivatives.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a &bgr;-lactam.

Abstract: Compounds of formula (I) compounds of formula (II) compounds of formula (III) and compounds of formula (IV) or pharmaceutically acceptable salts thereof are useful as H3 receptor antagonists. Processes to make the compounds and methods of treatment using the compounds are also disclosed.

Abstract: A method for the resolution of a mixture of the cis or trans enantiomers of a compound of the formula 1

Abstract: This invention provides compounds having the following general structure: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.

Abstract: Crystalline forms of [2R-[2&agr;(R*),3&bgr;(R*)]]-3-(1-hydroxyethyl)-&ggr;-methyl-&bgr;,4-dioxo-2-azetidinebutanoic acid(4-nitrophenyl)methyl ester and crystalline form of (&ggr; R,2R,3S)-&agr;-diazo-3-[(1R)-1-hydroxyethyl]-&ggr;-methyl-&bgr;,4-dioxo-2-azetidinebutanoic acid (4-nitrophenyl)methyl ester are disclosed.

Abstract: Described are piperidines of Formula I 1

Abstract: The present invention relates to compounds of the general formula I wherein A is a group of the formula and Z is an O or S atom, to the further processing thereof to form novel sec-amidoalkylcarbonic acid derivatives and to those sec-amidoalkylcarbonic acid derivatives.

Abstract: A compound having the formula: wherein all variables are as defined in the specification, for use as a neuramninidase inhibitor.

Abstract: The present invention relates to a method for the preparation of a compound of the general formula (I) wherein

Abstract: Compounds of the formula I, in which R1, R2, R3, R4, R5, and R6 have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics.

Abstract: Compounds, compositions and methods are disclosed useful for enhancing penetration of a pharmacologically active substances across skin or tissue membranes. Compounds for use in such compositions and methods are highly water-soluble N-substituted polyalkylene oxide derivatives of cyclic amides.

Abstract: A method for preparing a N-[(aliphatic or aromatic)carbonyl)]-2-aminoacetamide compound, and for preparing a cyclized compound therefrom, as well as novel resin bound intermediate compounds that are useful for preparing such compounds.

Abstract: Functionalized supports and methods for solid phase synthesis. Preferably, the functionalized support is azlactone-functionalized.

Abstract: The present invention relates to a one-step process to prepare pharmacologically active 2-oxo-5-oxazolidinylmethylacetamides.

Abstract: Compounds of the formula I, 1

Abstract: Compounds of the formula I, 1

Abstract: Compounds of the formula I, 1

Abstract: Taxane derivatives having a 3′ butenyl substituted C13 side chain.

Abstract: A process of synthesizing a compound of structural formula 6 is disclosed wherein R1 represents H or a suitable protecting group for an alcohol; R2 represents a benzyl, C1-6 alkyl or aryl; Y represents C1-3 alkyl, O, NH or S; X represents O, NH, or S and R5 represents a carboxy protecting group, comprising reacting a compound of formula 5: wherein R1, R2, R5, X and Y are as previously described with a phosphite or phosphonite reagent to produce a compound of formula 6. Further disclosed is an efficient method for the synthesis of a compound of formula 2: which comprises reacting a 4-acyl-2-azetidinone with a titanium, zirconium or hafnium enolate of a 1-hydroxy-2-butanone derivative.

Abstract: This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.

Abstract: The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.

Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1

Abstract: Certain novel substituted piperidine compounds 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. Also provided are methods of treating sexual dysfunction with a compound that is a selective agonist of MC-4R over any other human melanocortin receptor.

Abstract: Disclosed is a process for the preparation of a 4-substituted azetidinone derivative, which comprises reacting an azetidinone derivative and an amide compound in the presence of a magnesium compound such as those represented by the following formulas (II): and (IV): represented by the following formula (III): MgR5R6  (III) wherein R5 represents a C1-12 alkyl group, a C2-5 alkenyl group, a 5- to 8-membered alicyclic group which may be substituted by a lower C1-4 alkyl group, a phenyl group which may be substituted by a lower C1-4 alkyl group, a lower C1-4 alkoxy group or a halogen atom or a benzyl group which may be substituted by a lower C1-4 alkyl group, a lower C1-4 alkoxy group or a halogen atom, and R6 represents a halogen atom, a methanesulfonyloxy group, a benzenesulfonyloxy group, a p-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group, an acetoxy group which may be substituted by a halogen atom or a cyano group or an OR7 group (R7 representing

Abstract: Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.

Abstract: The carbapenem derivatives represented by the following formula (I) is disclosed.

Abstract: This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.

Abstract: An efficient method for the synthesis of a compound of formula 2: 1

Abstract: A compound of formula I wherein R1 is hydrogen, methyl, ethyl, methoxy or methylthio; R2 and R3 each independently is hydrogen or lower alkyl; R4 is hydrogen, lower alkyl, methoxy, ethoxy or benzyloxy; R5 is lower alkyl, lower cycloalkyl, (CH2)mC(O)OR6 wherein m is the integer 1 or 2 and R6 is lower alkyl, phenyl optionally substituted; optionally Het or Het(lower alkyl); or R4 and R5 together with the nitrogen atom to which they are attached form a nitrogen containing ring optionally substituted with C(O)O-benzyl or with phenyl optionally substituted with C(O)OR7 wherein R7 is lower alkyl or (lower alkyl)phenyl; and Z is lower alkyl or optionally substituted phenyl or Het; with the proviso that when Z is (CH2)p-(Het), then R2 and R3 each is hydrogen; or a therapeutically acceptable acid addition salt thereof which compound is useful in the treatment of HCMV infections.

Abstract: A process for making a beta methyl carbapenem intermediate is disclosed. A compound of formula I: is contacted in a non-reactive solvent with methyl Meldrum's acid and a base to produce a compound of formula III: Compound III is treated in an aprotic solvent with a scavenging base, an alkali metal halide and a tri-organo silyl protecting compound for nitrogen to produce a compound of formula IV: Compound IV may be reacted with a nucleophile Nu—X in a non-reactive solvent and base, and the mixture acidified to produce a compound of formula V. Compound V may be reacted with mild acid to produce a compound of formula VI.

Abstract: Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X, Y and Z are —CH2—, —CH(lower alkyl)— or —C(dilower alkyl)—; R and R2 are —OR6, —O(CO)R6, —O(CO)OR9 or —O(CO)NR6R7; R1 and R3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5; R4 is selected from lower alkyl, R5, —CF3, —CN, —NO2 and halogen R5 is selected from —OR6, —O(CO)R6, —O(CO)OR9, —O(CH2)1-5OR6, —O(CO)NR6R7, —NR6R7, —NR6(CO)R7, —NR6(CO)OR9, —NR6(CO)NR7R8, —NR6SO2R9, —COOR6, —CONR6R7, —COR6, —SO2NR6R7, S(O)0-2R9, —O(CH2)1-10—COOR