Abstract: Disclosure is a method for preparing &agr;-aspartyl-&bgr;-cyclohexylalaninamide, comprising carrying out a first step of amide formation of an &agr;-aspartyl phenylamine ester of general formula (II) wherein: R is a C1-C4 alkyl radical, and then performing a catalytic hydrogenation of the resulting &agr;-aspartyl phenylalaninamide ammonium salt, optionally released previously from its salt, and optionally transforming it into an addition acis salt.

Abstract: Treatment of the anxiety disorders and insomnia in humans may be accomplished by administering gabapentin in an effective amount.

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: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Abstract: The current invention discloses halogenated amidino amino acid derivatives useful as nitric oxide synthase inhibitors, and pharmaceutically acceptable salts thereof.

Abstract: The invention provides a multistep synthesis for the preparation of 4,5-diamino shikimic acid derivatives of formula 1

Abstract: GABA analogs such as gabapentin and pregabalin are useful to prevent and treat inflammatory diseases.

Abstract: A process for producing optically active amino acid derivatives having a cyclohexyl group or a substituted cyclohexyl group by hydrogenating an amino acid derivative containing an aromatic group in the presence of a ruthenium catalyst. The starting material may be an unprotected amino acid or an N- and/or C-protected derivative thereof. An major advantage of the process is that the reduction may be accomplished without substantial racemization.

Abstract: Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and epileptogenesis. Methods for preparing the compounds of the invention are also described.

Abstract: An improved process for the preparation of a cyclic amino acid by a novel synthesis is described where benzonitrile is treated with an alkali metal and an amine under Birch reduction conditions to generate in situ an anionic intermediate which is alkylated with an &agr;-haloacetic acid moiety which is subsequently converted to the desired product, as well as valuable intermediates used in the process.

Abstract: Compounds of the formula (I) where X is a —CO2H or —CONHOH group; Y and Z are independently sulphur or oxygen, at least one being sulphur; R1 is hydrogen, hydroxy, (C1-C6)alkyl, (C2-C6)alkenyl, or (C3-C8cycloalkyl; R2 is a (C1-C24)alkyl, phenyl(C1-C6)alkyl, or phenyl(C0-C6alkyl)O)C1-C6)alkyl, any of which may be optionally substituted by (C1-C6)alkyl, (C1-C6)alkoxy, halo or cyano (CN); R3 is the characterising side chain of a natural &agr;-amino acid in which any functional groups may be protected, (C1-C6)alkyl which may be optionally substituted, or cycloalkyl(C1-C6)alkyl; R4 is hydrogen, (C1-C6)alkyl, phenyl(C1-C6)alkyl, optionally substituted phenyl or heteroaryl, or a group of formula —(Q—O)n—Q where Q is a straight or branched (C1-C6)alkyl, where n is an integer >1 and no continuous linear sequence of atoms in the group R4 is >12; or a salt, hydrate or solvate thereof.

Abstract: There is disclosed a method of converting gabapenting hydrochloride substantially free of inorganic salts to gabapenting form II. The method comprises the steps of: (1) obtaining gabapentin hydrochloride that is substantially free of inorganic salts; (2) mixing a solution of the gabapenting hydrochloride with an additional amine in a first solvent so as to obtain a precipitate comprising gabapenting; and then (3) recovering gabapentin form II from the precipitate. The precipitated gabapentin is a novel polymorphic form of gabapentin possessing a crystalline structure characterized by novel sets of peaks in the powder X-ray diffraction pattern and in the FTIR spectra. This newly disclosed polymorph of gabapentin is characterized herein as gabapentin form III.

Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.

Abstract: The invention relates to precursors of the A-ring of vitamin D, of the formula (I): in which A, R, R1 and R2 are as defined in the specification. The invention also relates to a method of preparing compounds (I) comprising the enzymatic asymmetrization of 3,5-dihydroxybenzoic acid derivatives, as well as intermediates of preparation of said compounds.

Abstract: This invention is directed to a process for preparing a pseudotetrapeptide of formula I or a salt or prodrug thereof wherein is optionally nitrogen protected azaheterocyclyl; is a single or double bond; q is 1-5; B is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl; Q2 is H or a carboxylic acid protecting group; J is —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl; L is OR1, or NR1R2, where R1 and R2 are independently —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl or alkylaralkyl; and p is 1 or 2 which comprises the coupling of two dipeptides or psuedopeptides.

Abstract: Mammals are treated for infection or for conditions associated with pathologically proliferating mammalian cell growth (for example, certain cancers, restenosis, benign prostatic hypertrophy) by administration of a manipulator of nitrosative stress to selectively kill or reduce the growth of the microbes or helminths causing the infection or of host cells infected with the microbes or of the pathologically proliferating mammalian cells. Novel agents include &agr;-alkyl-S-alkyl-homocysteine sulfoximines wherein the &agr;-alkyl contains 2 to 8 carbon atoms, and the S-alkyl- contains 1 to 10 carbon atoms. In another invention herein, mammals in need of increased nitrosative stress defenses are treated, e.g., humans at risk for a stroke because of having had a transient ischemic attack, are treated.

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: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.

Abstract: Substituted cyclic amino acids of formula ##STR1## are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.

Abstract: Compounds which can chelate paramagnetic bi- and trivalent metal ions, their chelates with said metal ions and their use as contrast agents in magnetic resonance imaging (MRI), the compounds having formula (I) ##STR1## wherein R is a --(CH.sub.2).sub.m --O--R.sub.2 group or hydrogen,R.sub.2 is a (C.sub.6 -C.sub.10) aryl, or an alkyl(C.sub.1 -C.sub.5)-aryl(C.sub.6 -C.sub.10) group, substituted or not by a group L corresponding to a OH group or a OR.sub.3 group, wherein R.sub.3 is a linear or branched (C.sub.1 -C.sub.5) alkyl group; or L is NH.sub.2, halogen, COOH or CONR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are independently hydrogen, or a linear or branched (C.sub.1 -C.sub.5) alkyl which can be substituted by 1-6 hydroxy groups and/or 1-6 alkoxy groups,R.sub.1 can have the same meanings as R, independently from it, except for hydrogen,Z is independently OH or OR.sub.6, or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are as previously defined, and R.sub.6 is a (C.sub.1 -C.sub.

Abstract: The present invention relates to compounds having the formulae ##STR1## wherein R, R.sup.1, R.sup.6, R.sup.7, Rn.sup.8, X, and Z are defined herein, which are useful in the treatment or prophylaxis of malaria. The compounds of the present invention are especially useful in the treatment or prophylaxis of chloroquine-sensitive and chloroquine-resistant malaria.

Abstract: The present invention provides modified amino acids for delivering active agents, and particularly biologically or chemically active agents. The preferred modified amino acids of the present invention include N-acylated or sulfonated amino acids. These modified amino acids are used as carriers to facilitate the delivery of a cargo to a target. Such modified amino acids are well suited to form non-covalent mixtures with biologically-active agents for oral administration to animals. Methods for the preparation and administration of the modified amino acids and compositions including the same are also provided.

Abstract: The present invention concerns cyclic amino acids of formula ##STR1## substantially free from the lactam ##STR2## wherein n is an integer of from 4 to 6, a process for the preparation thereof, compositions containing the compounds and methods of using them.

Abstract: The compounds of Formula I are useful as immunosuppressive agents.

Abstract: Bridged cyclic amino acids of formula ##STR1## are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.

Abstract: A process for selective, direct oxidation of amine or amine hydrochloride mpounds is described. It uses mixed oxidizing agents of monopersulfate and ozone.

Abstract: A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)amino(alkyl or substituted alkyl) methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.

Abstract: Diamine carbamates are prepared by spraying liquid diamine into carbon dioxide gas, in the optional presence of a propellant.

Abstract: The invention is directed to optically active 1-amino-hydroxycycloalkanecarboxylic acid compounds represented by the formula: ##STR1## wherein n is 0, 1, 2, 3, or 4; methods of their synthesis; and their use as compounds to fix the confirmation of a peptide or protein molecule when introduced into the peptide or protein in the place of a normal amino acid.

Abstract: Disclosed is an acid-funtionalized polyurethane adduct and a process for the preparation of such adduct. The adduct having a linear or preferably branched structure comprises a plurality of internal urethane linkages and one or more terminal carboxylic acid groups per molecule. Such acid-funtionalized polyurethane adducts find value in the manufacture of crosslinked aqueous rubber latexes such as might be used in paint compositions.

Abstract: The present invention relates to mixtures of .alpha.-amino acids and/or derivatives thereof and cyclopentane-.beta.-amino acids and/or derivatives thereof, dipeptides of the abovementioned .alpha.-amino acids and cyclopentane-.beta.-amino acids and mixtures of the abovementioned mixtures and dipeptides which have an improved tolerability in warm-blooded animals compared with the pure cyclopentane-.beta.-amino acids.

Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.

Abstract: Compounds of formula I: ##STR1## wherein R.sub.a, R.sub.b, .PHI., B and R are as defined in the disclosure, have antagonistic activity on osteoclast hyper-reactivity.

Abstract: Mesogens are provided based on substituted unsaturated carboxylic acids such as acrylic and methacrylic acid. Substitution of a variety of hydrophobic tails onto the carboxylic acid or acid derivative via the vinyl carbon proximal to the carbonyl of the carboxylic acid results in mesogens that are capable of forming thermotropic and single-phase lyotropic mesophases over a broad range of compositions. The mesophases can be polymerized to lock in the ordered phases.

Abstract: Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N.sup..alpha. (.omega.-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N.sup..alpha. (.omega.-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.

Abstract: The present invention relates to a new method for obtaining a purity of about 93% to 100% of the trans form of 2- or 4-substituted cyclohexanecarboxylic acid or reactive derivatives thereof from the cis form or a mixture of the cis and trans forms by a single step, particularly, to a method for obtaining a purity of substantially 100% of the trans form of 4-substituted cyclohexanecarboxylic acid.

Abstract: The invention provides novel amino acid compounds of use in detecting and evaluating brain and body tumors. These compounds combine the advantageous properties of 1-amino-cycloalkyl-1-carboxylic acids, namely, their rapid uptake and prolonged retention in tumors with the properties of halogen substituents, including certain useful halogen isotopes including fluorine-18, iodine-123, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77 and bromine-82. In one aspect, the invention features amino acid compounds that have a high specificity for target sites when administered to a subject in vivo. Preferred amino acid compounds show a target to non-target ratio of at least 5:1, are stable in vivo and substantially localized to target within 1 hour after administration. An especially preferred amino acid compound is ?.sup.18 F!-1-amino-3-fluorocyclobutane-1-carboxylic acid (FACBC). In another aspect, the invention features pharmaceutical compositions comprised of an .alpha.

Abstract: The present invention relates to certain purine nucleoside analogues containing a carbocyclic ring in place of the sugar residue, salts, esters and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and to the use of such compounds in therapy, particularly the treatment or prophylaxis of certain viral infections.

Abstract: The invention provides novel amino acid compounds of use in detecting and evaluating brain and body tumors. These compounds combine the advantageous properties of 1-amino-cycloalkyl-1-carboxylic acids, namely, their rapid uptake and prolonged retention in tumors with the properties of halogen substituents, including certain useful halogen isotopes including fluorine-18, iodine-123, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77 and bromine-82.In one aspect, the invention features amino acid compounds that have a high specificity for target sites when administered to a subject in vivo. Preferred amino acid compounds show a target to non-target ratio of at least 5:1, are stable in vivo and substantially localized to target within 1 hour after administration. An especially preferred amino acid compound is ?.sup.18 F!-1-amino-3-fluorocyclobutane-1-carboxylic acid (FACBC).In another aspect, the invention features pharmaceutical compositions comprised of an .alpha.

Abstract: A compound of the formula ##STR1## wherein Q is an organic group of at least two carbon atoms having at least m substituents,m is 1, 2, 3, 4, 5 or 6, andn is 0 or 1.R.sup.3 is H or methyl,R.sup.8 and R.sup.9 are independently hydrogen, alkyl group or aryl,R.sup.12 and R.sup.13 are independently selected from the group consisting of an alkyl group or a cation, andR.sup.10 is independently selected from the group consisting of hydrogen, an alkyl group, aryl group, and highly-fluorinated alkyl group,R.sup.4 may be hydrogen or alkyl group, andR.sup.7 may be hydrogen or lower alkyl group, provides excellent stability to dispersions.

Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The invention concerns the discovery of the surprising and unexpected therapeutic effects of hydroxyl ions. The observed medicinal properties of these ions are both novel and broad in scope. The acute corrosive effects and toxicity of hydroxyl ions on living tissue has previously overwhelmed their therapeutic attributes. Unique hydroxyl ion modulating compounds have been discovered and are within the scope of the invention. When used appropriately as companions with hydroxyl ions, these modulating compounds obviate and attenuate the harmful effects of hydroxyl ions, unmasking and revealing their previously unknown and undemonstratable therapeutic properties. These hydroxyl ion modulating compounds do not significantly interfere with the surprising and unexpected therapeutic benefits of the hydroxyl ions. The novel hydroxyl ion modulating compounds are generally characterized as N,N-disubstituted-aminoalkanoate salts and substituted N,N-substituted-aminoalkanoate salts.

Abstract: (1) Prostaglandin (PG) E.sub.2 antagonist or agonist containing carbocyclic sulfonamides represented by the compound of the formula (I): ##STR1## cyclodextrin clathrates thereof, non-toxic salts thereof as active ingredient, (2) carbocyclic sulfonamides represented by the compound of the formula (II): ##STR2## cyclodextrin clathrates thereof, non-toxic salts thereof, (3) process for the preparation of the compound represented by the compound of the formula (II) described hereinbefore, (4) PGE.sub.2 antagonist or agonist containing the compound represented by the compound of the formula (II) as active ingredient.The compounds represented by the compounds of the formula (I) and (II) can be adapted to medicines which possess an inhibitory effect of uterine contraction, an analgetic action, an inhibitory effect of digestive peristalsis, a sleep-inducing effect as PGE.sub.

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

Abstract: A method of combating pests which comprises applying to such pests or to a pest habitat a pesticidally effective amount of a substituted 2-cyclohexen-1-yl-amine derivative of the formula ##STR1## and addition products thereof with acids and metal salts. Most of the compounds are new.

Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV Protease.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

Abstract: A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)-amino(alkyl or substituted alkyl)methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.