Abstract: A family of substituted chiral allosteric effectors of hemoglobin is useful for delivering more oxygen to hypoxic and ischemic tissues by reducing the oxygen affinity of hemoglobin in whole blood.

Abstract: This invention relates to methods and compositions of tripeptides and dipeptides having anti-inflammatory activities that can be used for the treatment of allergic and inflammatory reactions. A peptide of the formula: X-R.sub. 1 -R.sub.2 -R.sub.3 -Y  (I) or X-R.sub. 1 -R.sub.2 -Y  (II) wherein X is selected from the group consisting of H and acetyl; R.sub. 1 is selected from the group consisting of D or L-phenylalanine; tyrosine; tryptophan; phenylglycine; Nor-methylphenylalanine; cyclohexylalanine; and norleucine; R.sub.2 is selected from the group consisting of D or L-glutamate; and aspartate; and in the case of peptide (II), R.sub.3 is selected from the group consisting of glycine; D or L-alanine; beta-alanine; valine; leucine; isoleucine; sarcosine; and gamma-aminobutyric acid or another aliphatic amino acid; and Y is selected from the group consisting of OH and NH.sub.2, but excluding the dipeptides H-L-Phe-L-Glu-OH, H-L-Trp-L-Glu-OH, H-D-Phe-D-Glu-OH and H-D-Trp-D-Glu-OH.

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: A reagent having the general formula of General Formula I: 1

Abstract: Provided are compounds of formula (I) 1

Abstract: Processes for preparing N-methyl-L-alanine derivatives and novel intermediates of the process. The derivatives and intermediates are useful for preparing cell-binding agent/maytansinoid complexes.

Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.

Abstract: This invention encompasses the novel compounds of Formula I, which are useful in the treatment of caspase-3 mediated diseases.

Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides, such as rhGH. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration, are provided, and methods of preparation of the modified amino acid compound are provided.

Abstract: This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula: 1

Abstract: Compounds are provided that lower blood glucose concentrations, lower serum triglyceride concentrations, lower systolic blood pressure, and increase glucose uptake by adipose tissue, but do not affect the expression of PPAR-&ggr; by adipose tissue.

Abstract: A method for performing a peroxidase-based assay by reacting a peroxidase enzyme with a soluble organic p-hydroxyphenyl-containing compound having the formula: wherein Q is a linear or branched 1-12 heteroatom alkyl wherein the heteroatoms are selected from C, N, O, and S, wherein the bonds connecting the heteroatom alkyl chain are single or double, wherein any carbon atom in the heteroatom alkyl chain optionally includes a substituent selected from —OH, —COOH, —NH2, and —SH, and wherein R is selected from —OH, —COOH, —NH2, and —CH3; and converting the soluble organic p-hydroxyphenyl-containing compound into a stable insoluble product which becomes highly fluorescent after illumination, upon excitation.

Abstract: The invention relates to novel amino- and amido-diphenyl ethers, processes for their preparation and their use in pharmaceuticals, in particular for the indications of arteriosclerosis and hypercholesterolaemia.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) useful for oral testosterone replacement therapy. Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. In one embodiment, the SARM compounds bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds bind reversibly to the androgen receptor.

Abstract: Compounds for treating diseases by altering mitochondrial function that affects cellular processes, as well as to compositions and methods related thereto.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis.

Abstract: A process for producing a phenylalkanoic acid amide of the formula [3] by reacting a carboxylic acid of the formula [1] with a dehydrating agent to produce an oxazolinone compound of the formula [2] and then reacting the oxazolinone compound with methyllithium or a methylmagnesium halide and an intermediate for producing the phenylalkanoic acid compound.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.

Abstract: Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: An amide compound of the formula (I): wherein R is amino and the like, A is alkylene and the like, X is O, S and the like, M is arylene and the like, R1, R2, R3 and R4 are H, hydroxy and the like, R5 is H, alkyl and the like, m is an integer of 0-6, R6 is an optionally substituted aryl and the like, and R7 is H, an optionally substituted alkyl and the like, a pharmaceutically acceptable acid addition salt thereof and a pharmaceutical containing same as an active ingredient. The amide compounds exhibit superior suppressive effects on cytokines directly or indirectly involved in inflammations, such as IL-8, IL-1, IL-6, TNF-&agr;, GM-CSF and the like, and are useful for the prophylaxis and treatment of rheumatic diseases, arthritis due to gout and the like.

Abstract: An aminobutyric acid derivative of the formula (I): (wherein all symbols are as defined in the specification) and salt thereof. salt thereof. The compounds of the formula (I) possess an inhibitory activity on matrix metalloproteinase and are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, metastasis of, invasion of or growth of tumor cells, autoimmune disease (e.g. Crohn's disease, Sjogren's syndrome), disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, aorta aneurysm, endometriosis.

Abstract: Disclosed are substituted phenoxyacetic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds, alone or in combination with other therapeutic agents, and methods of treatment employing the compounds and pharmaceutical compositions, as well as methods for their synthesis.

Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide (hereinafter referred to as a “protected/activated salicylamide”). The method comprises the steps of (a) alkylating the protected/activated salicylamide with an alkylating agent to form a protected/activated alkylated salicylamide, and (b) deprotecting and deactivating the protected/activated alkylated salicylamide, simultaneously or in any order, to form the alkylated salicylamide. The alkylated salicylamides prepared by this method are suitable for use in compositions for delivering active agents via oral or other routes of administration to animals.

Abstract: Novel transition metal catalysts with conformationally rigid chiral phosphines and phosphites are developed for asymmetric carbon-hydrogen and carbon—carbon bond formation. The invention emphasizes synthesis of chiral amines, &bgr;-amino acids and related compounds via catalytic asymmetric hydrogenation based on chiral monodentate and bidentate phosphines with cyclic ring structures. The ligands contain rigid ring structures.

Abstract: New thyroid receptor ligands are provided which have the general formula in which: X is —O—, —S—, —CH2—, —CO—, or —NH—; R1 is halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 6 carbons, at least one of R2 and R3 being other than hydrogen; R4 is methyl, ethyl, n-propyl or trifluoromethyl; R5 is hydrogen or lower alkyl; R6 is carboxylic acid, or esters or prodrugs; R7 is hydrogen or an alkanoyl or an aroyl. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

Abstract: New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

Abstract: A compound of the formula (I): wherein: for example, a compound below: wherein: R1 is CH3, H or Na; and X1—X2—X3 is: or its salt or a hydrate thereof is useful as PGD2 antagonist and can be used as a drug for treating diseases in which mast cell dysfunction is involved, for example, systemic mastocytosis and disorder of systemic mast cell activation, and also tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, injury due to ischemic reperfusion, and as an anti-inflammatory agent. It is particularly useful in the treatment of nasal occlusion.

Abstract: According to the invention, waste materials containing amido-carboxylic acid esters, which are generated during the preparation of phenyl ester salts, can be converted into amido-carboxylic acids. The recovered amido-carboxylic acid is then useful in the preparation of additional phenyl ester salt by the original preparation process or other processes known in the art. The process of the invention combines a waste material containing amido-carboxylic acid esters with an aqueous solution of a strong acid having a pH less than about 1 to form a mixture. The process heats the mixture to a temperature of at least 90° C. and maintains the mixture at that temperature for a time sufficient to hydrolyze the amido-carboxylic acid esters to amido-carboxylic acids. Sufficient base is the added to adjust the pH of the mixture to greater than about 2. The mixture is then maintained at a temperature of at least 80° C.

Abstract: The present invention is directed to novel dipeptide thereof, represented by the general Formula I: where R1-R3, X and Y are defined herein. The present invention also relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.

Abstract: The present invention comprises small molecular weight, non-peptidic inhibitors of formula I and II of Protein Tyrosine Phosphatase 1 (PTP1) which are useful for the treatment and/or prevention of Non-Insulin Dependent Diabetes Mellitus (NIDDM).

Abstract: The invention is directed to physiologically active compounds of general formula (I): wherein R1 is hydrogen, halogen, lower alkyl or lower alkoxy; X1, X2 and X6 independently represent N or CR2; and one of X3, X4 and X5 represents CR3 and the others independently represents N or CR2 where R2 is hydrogen, halogen, lower alkyl or lower alkoxy; and R3 represents a group —L1—(CH2)n—C(═O)—N(R4)—CH2—CH2—Y; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).

Abstract: Novel aminobutyric acids derivatives and methods for protecting crops against fungal diseases by applying to the crops or their locus a composition containing an effective amount of said derivatives.

Abstract: Optically active N-(S-2-acetylthiomethyl-1-oxo-3-phenylpropyl)-glycine benzyl ester useful as an enkephalin inhibitory agent or ACE inhibitory agent can be produced at low cost in an industrial manner, by a method comprising subjecting optically active 2-hydroxymethyl-3-phenylpropionic acid and glycine benzyl ester to condensation to subsequently convert the hydroxyl group into an elimination group, and substituting the elimination group with an acetylthio group.

Abstract: Compounds of formula (I), wherein either X is CH or N, Y is OR1 and Z is O, or X is N, Y is NHR8 and Z is O, S or S(═O); R1, R2 and R3 are as defined according to the specification; m is 0, 1 or 2; R5 is, for example, halogen, C1-C6alkyl, halo-C1-C6alkyl or C3-C6cycloalkyl; n is 0, 1, 2, 3 or 4; R9 is methyl, fluoromethyl or difluoromethyl; A and R7 are as defined according to the specification; D is O, S, —S(═O) or S(═O)2; G is C1-C6aalkylene; T—R6 is R6, —C(═N—O—A1—R77)—R6; —SiR14(R15)—R6; —C(═O)—R6; —C(R16)═C(R17)—R6, —C≡C—R6 or —D—R6; R6 is C1-C4alkyl or unsubstituted or substituted aryl or heteroaryl; A1 and R77 are as defined above for A and R7; L is U—R18, P(OR)vR11R12, P(S)wR11R12 or N(aryl)R13; v and w are 0 or 1; U—R18 is —C(═O)—C(═O)—R18; —C(OH)—C(OH)—R18; —C(═N&md

Abstract: The invention provides an improved process for the preparation of a compound containing a 2,4,6-triiodinated benzene ring, said process comprising reacting a 2,4,6-unsubstituted 5-amino-benzoic acid or derivative there of with an iodine halide iodinating agent in an aqueous reaction medium, characterised in that the iodinating agent is added to an aqueous medium containing the 5-amino-benzoic acid or derivative at two different temperature ranges: (A) one or more primary portions of the agent are added at a temperature in the range 40 to 70° C. and then one or more secondary portions of the agent are added at a temperature in the range 75 to 95° C. or (B) one or more primary portions of the agent are added at a temperature in the range 75 to 95° C. and then one or more secondary portions of the agent are added at a temperature of 60 to 70° C.

Abstract: The invention pertains to chiral ferrocene phosphine derivatives and their use with transition metals as asymmetric catalysts in asymmetric hydrogenation.

Abstract: The present invention has as its object providing phenethylamine derivatives that typically function as a motilin receptor antagonist and which are useful as medicines. The invention provides compounds represented by the general formula (1): (wherein A is typically an amino acid residue, R1 is typically R6—CO—, R2 is typically a hydrogen atom, R3 is typically —CO—R7, R4 is typically an alkyl group, R5 is typically a hydroxyl group, R6 is typically an alkyl group, and R7 is typically an amino group).

Abstract: A process for the preparation of preparation of farnesyltransferase inhibitors of formula (I) or pharmaceutically acceptable salts or prodrugs thereof, is disclosed.

Abstract: A method of separating a racemic mixture of amino acid enantiomers, which entails reacting the mixture with a 4-pentenoyl compound, thereby derivatizing the enantiomers to form two diastereomers, and separating the diastereomers.

Abstract: A novel class of tripeptide &agr;-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula M1—AA—AA—AA—CO—NR3R4.

Abstract: Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.

Abstract: The present invention provides compounds having the formula: wherein n is 0 or 1; R is —NH2 or wherein R1 and R2 are independently selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, carboxy, carboxyalkyl, and carbamoyl; Q is R3C(O)— or wherein R5 is selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, and carbamoylalkyl, and R3 and R4 are selected from the group consisting of H, alkyl, alkoxy, arylalkoxy, aralkyl, heteroaralkyl, and carbamoylalkyl; the Q—NH—(CH2)n— and the —C(O)R substituents of the compound of formula I are independently positioned ortho, meta, orpara relative to the carbon atoms that form the bond between the two phenyl groups to which said substituents are bound, with the proviso that said substituents are not both positioned ortho; and the Q—NH—(CH2)n and the —C(O)R substituents of the compound of formula II are positioned meta orpara t

Abstract: A method for protecting a crop against plant-parasitic nematode attack by inducing local and systemic resistance of the crop comprising the application of a composition containing an effective amount of &bgr;-amino butyric acid or derivatives thereof to the crop or its locus.

Abstract: Provided is a process for efficiently producing N-glycyltyrosine of high purity represented by the following formula: a salt thereof, or a solvate thereof, which comprises adding dropwise to an aqueous suspension of tyrosine or a salt thereof 2 equivalents or more of a haloacetyl halide and an aqueous solution of an inorganic base simultaneously in the presence or absence of an organic solvent, and subjecting the resulting N-haloacetyltyrosine to a reaction with an ammonium ion. Also provided are N-glycyl-L-tyrosine dehydrate having the crystal structures showing specific diffraction patterns in X-ray powder diffraction and processes for producing the same which are characterized by comprising crystallizing the dihydrate from an ethanol-water mixed solvent or water.

Abstract: An enantiomerically enriched compound of formula (4) or the opposite enantiomer thereof, wherein R is C1-10 alkyl. This compound, in the form of a transition metal complex, is useful as a catalyst for stereoselective hydrogenation.

Abstract: Process for the preparation of N-acetyl protected amino acids of Formula I by amido carbonylation utilizing carbon monoxide, nitrile, and an aldehyde in the presence of a metal catalyst.

Abstract: The present invention relates to a tandem process of reduction and host-guest complexation using metal-hydride complexes to reduce chemical entities bearing carbonyl groups or their equivalents, and host-guest complexation to achieve improved optical resolution of the reduction product. In the complexation step, the reduction product is optically resolved via inclusion into the crystalline complex where it resides as guest and another complex component acts as host. Additional crystallization stages are performed if further improvements in the enantiomeric excess is desired.

Abstract: A tetrazole derivative of formula (I) ##STR1## wherein R is H, alkyl, alkoxy, carbocyclic ring, alkyl or alkoxy substituted by carbocyclic ring;AA.sup.1 and AA.sup.2 is a bond or ##STR2## and ##STR3## respectively, or AA.sup.1 and AA.sup.2, together, may have the formula (a); ##STR4## and Y is formula (b) ##STR5## wherein the Tet ring is tetrazole; Z is alkylene, alkenylene, O, S, SO, SO.sub.2, NR.sup.26, methylene in alkylene replaced by O, S, --SO--, --SO.sub.2 -- or --NR.sup.26 --; and E is H, alkyl, or COOR.sup.27.

Abstract: Compounds of the general formula I ##STR1## compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are described.

Abstract: A .beta.-phenylisoserine derivative of general formula (I): ##STR1## in the form of a salt or an ester, in which Ar represent an aryl radical, R represents a phenyl or naphthyl or a O--R.sub.1 radical and G.sub.1 represents --CH.sub.2 --Ph radical; and a method of using the same for making taxane derivatives.