Abstract: The present invention provides a process for preparing atorvastatin hemi-calcium from an atorvastatin ester derivative with calcium hydroxide. The process is conveniently incorporated into a process for preparing atorvastatin hemi-calcium from an acetonide protected, ester protected &bgr;,&dgr;-dihydroxy heptanoic acid precursor compound by a first acid hydrolysis step followed by base hydrolysis with calcium hydroxide. The latter process may be performed as a one-pot process.

Abstract: Novel pyrrolidine 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: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.

Abstract: Novel linkers for linking a donor dye to an acceptor dye in an energy transfer fluorescent dye are provided. These linkers faciliate the efficient transfer of energy between a donor and acceptor dye in an energy transfer dye. One of these linkers for linking a donor dye to an acceptor dye in an energy transfer fluorescent dye has the general structure R21Z1C(O)R22R28 where R21 is a C1-5 alkyl attached to the donor dye, C(O) is a carbonyl group, Z1 is either NH, sulfur or oxygen, R22 is a substituent which includes an alkene, diene, alkyne, a five and six membered ring having at least one unsaturated bond or a fused ring structure which is attached to the carbonyl carbon, and R28 includes a functional group which attaches the linker to the acceptor dye.

Abstract: The invention is directed to physiologically active compounds of general formula (I): 1

Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I).

Abstract: A cyclic amine compound represented by the following general formula (1): wherein, R1, R2 and R3 each independently represent a hydrogen atom or an alkoxy group; W1 and W2 each independently represent N or CH; X represents O, NR4, CONR4 or NR4CO; R4 each independently represents a hydrogen atom, or an alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl group; and l, m and n each represents a number of 0 or 1, a salt thereof and a hydrate thereof are provided. These compounds have inhibitory effects on both cell adhesion and cell infiltration and are useful as anti-asthmatic agents, anti-allergic agents, anti-rheumatic agents, anti-arteriosclerotic agents, anti-inflammatory agents, anti-Sjogren's syndrome agents or the like.

Abstract: The present invention relates to an immunogenic conjugate comprising a carrier molecule coupled to an autoinducer of a Gram negative bacteria. The immunogenic conjugate, when combined with a pharmaceutically acceptable carrier, forms a suitable vaccine for mammals to prevent infection by the Gram negative bacteria. The immunogenic conjugate is also used to raise and subsequently isolate antibodies or binding portions thereof which are capable of recognizing and binding to the autoinducer. The antibodies or binding portions thereof are utilized in a method of treating infections, a method of inhibiting autoinducer activity, and in diagnostic assays which detect the presence of autoinducers or autoinducer antagonists in fluid or tissue samples.

Abstract: The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I).

Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders.

Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.

Abstract: A mono-, bi- and/or polyfunctional amide of the formulae (Ia) and/or (Ib),

Abstract: Trisubstituted pyrroles are useful in the control of coccidiosis in poultry.

Abstract: Disclosed is a photographic element comprising a light-sensitive silver halide emulsion layer having associated therewith a cyan “NB coupler” having the formula (I): 1

Abstract: Described are compounds of formula I wherein at least one of the bonds in the five-membered ring is a double bond; B is any alpha or beta amino acid connected to the ring with an amide or peptide bond; or a salt thereof with a pharmaceutically acceptable acid or base. Pharmaceutical compositions containing these compounds are also described. These compounds are useful for treating type II diabetes.

Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.

Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-[1-chloro-1-(perfluoroalkyl)methyl]arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds.

Abstract: The present invention discloses halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: The present invention relates to a scaleable process for the oxidation of carbon-boron bonds with Oxone®.

Abstract: This invention relates to compounds of formula 1

Abstract: Novel processes and intermediates are provided for the synthesis of derivatives of 4-amino-3-hydroxypyrrole-2-carboxylic acids that are useful as monomers for polyamides capable of binding dsDNA. According to one preferred reaction scheme, an alkyl alkoxymethylene nitroacetate (Formula VIII) is prepared by reaction of a trialkyl orthoformate or orthoacetate with a nitroacetate ester in the presence of a carboxylic anhydride. The compound of Formula VIII is condensed with an N-substituted glycine to yield an N-substituted (2-nitro-2-alkoxycarbonyl)vinyl glycinate ester (Formula VII). Ring closure in the presence of an alkali metal alkoxide yields a 4-nitro-3-hydroxypyrrole-2-carboxylic ester (Formula V). After blocking of the 3-hydroxy group to produce a further intermediate (Formula IV), the 4-nitro group is reduced to a 4-amino group (Formula III), and the 4-amino group is then blocked by reaction with a dicarbonate diester to produce the fully blocked intermediate (Formula II).

Abstract: This invention relates to compounds of formula (I): wherein: Y is Ar or NR1R2; R1 is R″, R″C(O), R″C(S), R″SO2, R″OC(O), R″R′NC(O), or R″R′NC(S); R2 is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R3 is H, C2-6alkenyl, C2-6alkynyl, Het, Ar or C1-6alkyl optionally substituted by OR′, SR′, NR′2, N(R′)C(O)OR″, CO2R′, CO2NR′2, N(C═NH)NH2, Het or Ar; R4 is H, C1-6alkyl, C2-6alkenyl, Ar-C0-6alkyl, or Het-C0-6alkyl; R5 is  Ar-C0-6alkyl, Het-C0-6alkyl, adamantyl-C(O)—, Ar-C(O)—, Het-C(O)— or; R6 is R″, R″C(O), R″C(S), R″SO2, R″OC(O), R″R′NC(O), R″R′NC(S), or R″OC(O)NR′CH(R*)C(O); R7 is C3-6cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl, Ar-C0-6alkoxy, Het-C0-6alkoxy, or C1-6alkyl optionally substituted by OR′, SR′, NR′2, N(R′)C(O)OR″, CO2R&p

Abstract: This invention provides processes for the preparation of a compound of Formula I:

Abstract: Disclosed are &bgr;-amino acid monomers containing cylcoalkyl, cycloalkenyl, and heterocylic substituents which encompass the &agr; and &bgr; carbons of the peptide backbone and &bgr;-polypeptides made from such monomers. Method of generating combinatorial libraries of polypeptides containing the &bgr;-peptide residues and libraries formed thereby are disclosed.

Abstract: The present invention provides novel 3-substituted pyrrolidines of the formula 1

Abstract: Phenylalanine derivatives of formula (1) are described: 1

Abstract: The invention relates to compounds of formula (I):

Abstract: Disclosed is a process for preparing a pyrrolidone derivative, which comprises allowing at least one of &ggr;-butyrolactone, 4-hydroxybutyric acid, and a low-molecular polymer of 4-hydroxybutyric acid to react with an alkylamine, wherein (i) the content of a primary amine in said alkylamine is 85% by weight or lower, and (ii) the molar ratio of the total amount of the charged primary and secondary amines to the total amount of the charged &ggr;-butyrolactone, 4-hydroxybutyric acid, and low-molecular 4hydroxybutyric acid polymers satisfies formula:

Abstract: Disclosed are novel pyrrole derivatives, a process for their manufacture, pharmaceutical compositions containing such compounds and the use of such compounds in the treatment of HIV mediated diseases.

Abstract: The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma.

Abstract: This invention is directed to benzenamine derivatives of formula (I): wherein A, W, m, n, R1, R2, R3, R4, R5 and R6 are defined herein. These compounds are useful as anti-coagulants.

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: The invention relates to novel pesticidal trifluoromethylpyrrolcarboxamides of formula I 1

Abstract: A method for recovering amino acids, which comprises supplying a mixed solution containing inorganic acid salts, amino acids and non-electrolytes such as saccharides to a first-step resin layer comprising an Na type or K type strongly acidic ion exchange resin; separating an effluent into at least a first fraction containing coloring matters, acidic amino acids and ashes, a second fraction containing neutral amino acids and saccharides, and a third fraction containing betaines; supplying the second fraction to a second-step resin layer comprising at least one resin selected from the group consisting of NH4 type, Ca type and Mg type strongly acidic ion exchange resins, and optionally further supplying it to a third-step resin layer comprising an Mg type or Ca type strongly acidic ion exchange resin different from the resin of the second-step resin layer, thereby recovering various kinds of amino acids contained in an effluent.

Abstract: The present invention is directed to pyrrolidine compounds of the formula I: 1

Abstract: The present invention relates to novel substituted diamine derivatives for the formula 1

Abstract: It has been discovered that compounds of the formula: 1

Abstract: A compound of the formula 1

Abstract: A compound of the formula 1

Abstract: The invention relates to compounds having the formula (I) or a pharmaceutically acceptable salt thereof. In the formula (I), X represents a group having the structural formula (II), and Y represents O or S. The compounds of the invention can be used a chloride channel blockers.

Abstract: Compounds of formula (1) are described: wherein L1 is a covalent bond or a linker atom or group; R is a carboxylic acid (—CO2H) or a derivative threof; R6 and R7 which may be the same or different is each an atom or group —L2(Alk2)tL3R12 in which L2, L3, Alk2 and t are as previously defined and R12 is a hydrogen or halogen atom or an —OR9, —NR9R10, —NO2, —CN, —CO2R9, —CONR9R10, —COR9, —N(R9)COR10, —N(R9)CSR10, —SO2N(R9)(R10), —N(R9)SO2R9, —N(R9)CON(R10)(R11), —N(R9)CSN(R10)(R11), —N(R9)SO2N(R10)(R11), or an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group provided that R6 and R7 are not both hydrogen atoms and when R7 is a hydrogen atom then R4 and R5 is each a hydrogen or halogen atom or an alkyl, alkoxy or nitro group; and the salts, solvates, hydrates and N-oxides thereof, for use in modulating cell adhesion.

Abstract: The present invention provides compounds of the formula where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocylic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or —C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.

Abstract: A thrombin receptor antagonist having the formula 1

Abstract: It has been discovered that compounds of the formula: 1

Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, or hydroxy; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Abstract: The present invention relates to a process for the racemization of N-acylamino acids of the formula (I)

Abstract: Methods, compositions, and devices for alleviating the problems of toxic discharge of aldehydes present in waste streams are disclosed. The methods relate to reducing neutralized aldehydes wherein the neutalized aldehydes are formed by treating aldehydes with amino acids and thereinafter are reduced. These reduced, neutralized aldehydes do not revert back to toxic aldehydes, but form amino acids and thus allow waste containing aldehyde to be more environmentally safely disposed.

Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.

Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Abstract: The subject-matter of the present invention is novel compounds of the type of esters derived from alkylenediaminediacetic acid or alkylenediaminetriacetic acid and their-process of preparation. The invention also relates to the use of these compounds in cosmetic and pharmaceutical compositions, in particular for protecting the body against oxidative stress.