Abstract: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: The invention relates to a method for preparing an ester, by admixing a compound having the structure I or IV: ##STR1## with a base and an alcohol to produce an ester, wherein the alcohol is a precursor to Taxol and its analogs. The present invention also relates to compounds having the structure I and IV and methods of making them therefor. The invention also relates to the esterification of an alcohol by adding an alkoxide to a compound having the structure VII: ##STR2## The invention further relates to compounds having the structure I, IV, and VII and methods of making them therefor. The invention further relates to alcohols, and in particular, alcohols that are synthetic precursors to Taxol and analogs thereof.

Abstract: Compounds of the formula: wherein:R.sub.1, R.sub.2, R.sub.3, R.sub.4,R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are, independently, hydrogen, COOR.sub.15, halogen, nitro, cyano, C.sub.1-10 alkoxy, C.sub.1-10 haloalkoxy, sulfonic acid, C.sub.1-10 alkylsulfonyl, C.sub.6-12 arylsulfonyl, C.sub.6-12 aralkylsulfonyl, C.sub.1-10 alkylsulfinyl, C.sub.6-12 arylsufinyl, C.sub.6-12 aralkylsulfinyl, sulfamoyl, C.sub.1-10 alkylsulfamido, C.sub.6-12 arylsulfamido, C.sub.1-10 alkanoyl, C.sub.6-12 aryloyl, C.sub.6-12 aralkanoyl, amino, C.sub.1-10 alkylamino, C.sub.2-10 dialkylamino, C.sub.6-12 aralkylamino, C.sub.6-12 arylamino, carboxamido, C.sub.1-10 alkylcarboxamido, C.sub.6-12 arylcarboxamido, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl, C.sub.2-12 alkenyl, C.sub.6-12 aryl, C.sub.6-12 aralkyl; with the proviso that at least one of R.sub.4 and R.sub.5 is COOR.sub.15 ;R.sub.9 is hydrogen, C.sub.1-10 alkyl and C.sub.1-10 haloalkyl;R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, or C.sub.2-12 alkylidene;R.sub.

Abstract: There is described a process for the preparation of a compound of formula I ##STR1## in which process: a) a compound of formula II ##STR2## is reacted with an organolithium compound of formula IIILi--R.sub.7 (III)b) the resulting lithium complex is reacted with a compound of formula IVY.sub.1 --CO--CO--Y.sub.1 IVto form a compound of formula V ##STR3## c) that compound is, in either order, c1) oximated with O-methylhydroxylamine; or oximated with hydroxylamine and then methylated or fluoromethylated or difluoromethylated;c2) reacted with a chloroformic acid ester.X, m, Y, R.sub.1 to R.sub.3 and R.sub.7 are as defined in the description.

Abstract: To produce an 1-alkoxycarbonyl-3-phenylpropyl derivative having little amount of impurities and good quality by a simple, efficient and highly productive process which comprises catalytically reducing an 1-alkoxycarbonyl-3-oxo-3-phenylpropyl derivative. 1-Alkoxycarbonyl-3-phenyl-propyl derivative is provided and obtained by catalytic redution being carried out in an alcohol or a solvent containing the alcohol in the presence of a strong acid having a concentration of 0.4 to 0.5 N, the amount of the strong acid being at least 3 equivalents based on one equivalent of the 1-alkoxycarbonyl-3-oxo-3-phenylpropyl derivative (1 mole).

Abstract: The invention includes selected novel optically active .alpha.-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.

Abstract: A phenylalkane amide compound having the formula (1): ##STR1## wherein R.sup.1 -R.sup.4, X, n, Y, Z and Q are as defined herein. The compound is useful as an agricultural or horticultural fungicide.

Abstract: An efficient protocol for the synthesis of taxol, taxol analogs and their intermediates is described. The process incudes the attachment of the taxol A-ring side chain to baccatin III and for the synthesis of taxol and taxol analogs with variable A-ring side chain structures. A rapid and highly efficient esterification of O-protected isoserine and 3-phenylisoserine acids having N-benzyoloxycarbonyl groups to the C-13 hydroxyl of 7-O-protected baccatin III is followed by a deprotection-acylation sequence to make taxol, cephalomanninne and various analogs, including photoaffinity labeling candidates.

Abstract: The present invention provides an amino compound represented by Formula: ##STR1## wherein X is CH.sub.2 NH or CONH, Y is CH.sub.2 NH or CONH with the proviso that X and Y are not CONH at the same time; Z is CH.dbd.C(R.sup.4)R.sup.5, CH.sub.2 CH(R.sup.4)R.sup.5 or an alkoxycarbonyl group, R.sup.1 is a hydrogen atom; a lower alkyl group, a cycloalkyl group, a cycloalkyl-substituted alkyl group, an aralkyl group or an aryl group, each group of which is substituted or unsubstituted, R.sup.2 and R.sup.3 are each independently a lower alkyl group or an aralkyl group, each group of which is substituted or unsubstituted, and R.sup.4 and R.sup.

Abstract: A method for producing an optically active erythro-3-amino-2-hydroxybutyric ester as an important intermediate of pharmaceutical agents, specifically HIV protease inhibitor, in high purity and in high yield. The method includes producing an optically active erythro-3-amino-2-hydroxybutyric ester by oxidizing the hydroxyl group at the 2-position of an optically active 3-amino-2-hydroxybutyric ester, optically active at the 3-position, as represented by formula (I): ##STR1## (wherein R.sup.1 represents a phenyl group or a cyclohexyl group; R.sup.2 represents a protective group and R.sup.3 represents an unsubstituted or substituted alkyl residue; the steric configuration of *1 represents S configuration or R configuration), and then reducing erythro-selectively the resulting product by using aluminum alkoxide.

Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.

Abstract: This invention provides sweetener blends comprising N-[N-(3,3-dimethylbutyl)-L-.alpha.-aspartyl]-L-phenylalanine 1-methyl ester and another sweetener. The sweetener blends of this invention exhibit isobole synergy.

Abstract: This invention relates to novel compounds of general formula (I) ##STR1## wherein R.sup.1 represents an organic group, R.sup.2 represents a hydrogen atom or an organic group, and the asterisk denotes that the group R.sup.1 is predominantly in the R- or S-configuration such that the compound is in substantially enantiomerically pure form. The compounds are a useful source of chiral nucleophiles, e.g. undergoing stereoselective Michael addition to .alpha.,.beta.-unsaturated carboxylic acid derivatives.

Abstract: Compounds of formula (I) ##STR1## and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as stromelysin, gelatinase, matrilysin and collagenase, and are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.

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: The present invention provides an efficient route to the C-13 side chain of the anti-cancer drug paclitaxel (TAXOL) and its analogs. The process includes the resolution of racemic erythro 2-hydroxy-3-amino-3-phenylpropionamide by diastereomeric crystallization and its conversion via various intermediates to the threo-ethylester and threo-methylester isomers.

Abstract: The present invention provides compounds having the Formula I ##STR1## The present invention also provides methods of treating atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.

Abstract: The invention concerns novel phenoxyethylamine derivatives having a high affinity for the 5-HT.sub.1A receptor, methods for preparing them, pharmaceutical compositions containing them and their use as medicine and particularly as inhibitors of gastric acid secretion or as antiemetic.

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: Compounds of formula (I) wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X are as defined in the specification and are prepared by elimination of one of the groups X.sub.1 and X.sub.2 from a compound of formula (II) wherein X.sub.1 and X.sub.2 each independently represent a carboxylic acid group or salt thereof, or a protected carboxylic acid group, the non-eliminated group X.sub.1 or X.sub.2 corresponding to the group X in the desired compound of formula (I).

Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitrites thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.

Abstract: A compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: [wherein each of Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 is an aryl group or an aromatic heterocyclic group; A.sup.1 is a C.sub.2-6 chain hydrocarbon group or a group represented by --A.sup.1a --W.sup.1 --A.sup.1b -- (wherein W.sup.1 is an oxygen atom, a sulfur atom, an ethynylene group, a cyclopropylene group or a group represented by --NR.sup.W --; A.sup.2 is a C.sub.2-8 chain hydrocarbon group; each of X and Y is an oxygen atom, a sulfur atom, a carbonyl group or a group represented by --CHR.sup.a -- or by --NR.sup.b --, or X and Y together represent a vinylene group or an ethynylene group; each of R.sup.1, R.sup.2, R.sup.3, R.sup.7 and R.sup.8 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkenyl group or a lower alkoxy group; each of R.sup.4 and R.sup.

Abstract: A process for synthesizing N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine derivatives of the following formula (I): ##STR1## in which the definition of R has the same meaning as given in the description by using a sulfite derivative to activate the C-terminus of the three dimensional structure of an amino acid of N-[1-(S)-ethoxycarbonyl-3- phenylpropyl]-L-alanine, which can effectively couple with another amino acid to form a dipeptide of formula (I). The compound of fomula (I) is an inhibitor of ACE.

Abstract: The invention concernes borneol esters of general formula (I), in which R.sup.1 means T--C(O)--CH(OR.sup.6)--(NR.sup.7a R.sup.7b)--R.sup.8, C(O)--CH(OR.sup.6a)--CH[NR.sup.7 (C(O)--CH(OR.sup.6b)--CH (NR.sup.7a R.sup.7b)--R.sup.8a)]--R.sup.8b ; R.sup.7a R.sup.7b are identical or different and means R.sup.7 ; R.sup.7 means hydrogen, A, --C(O)R.sup.12, --C(O)OR.sup.12, --C(O)SR.sup.12, --C(O)NHR.sup.9d, --C(O)NR.sup.9d R.sup.9e, --SO.sub.2 R.sup.12, C.sub.1 -C.sub.10 alkyl; R.sup.8a, R.sup.8b are identical or different and mean R.sup.8 ; R.sup.8 means (i), heteroaryl substituted by X.sup.3, C.sub.7 -C.sub.16 aralkyl, alkyl; A is B--[O--(CH.sub.2).sub.t --C(O)].sub.0 or 1-, farnesyl--P(O)(OR.sup.9d)--O--(CH.sub.2).sub.t --C(O)--; B means protein kinase-inhibitors or farnesyl protein transferase-inhibitors such as for example farnesyl (ii); and T is a bond, Z.sup.i or a group (iii). The borneol esters can influence tubulin polymerisation and tubulin depolymerisation.

Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: There are described compounds of the general formula I ##STR1## in which the index and the substituents have the following meanings: n is 0, 1, 2, 3 or 4;R is nitro, cyano, halogen,unsubstituted or substituted alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy orin the event that n is greater than 1 additionally an unsubstituted or substituted bridge which is bonded to two adjacent ring atoms;R.sup.1, R.sup.2 are alkyl;R.sup.3 is a substituted pyrazole ?sic! or triazole ?sic! radical of the formulae A.1 to A.3 ##STR2## where the bond marked .circle-solid. is the bond to the oxygen, processes for their preparation, and their use.

Abstract: Disclosed is a process for producing .beta.-amino-.alpha.-hydroxycarboxylic acid derivatives of general formula (2R,3S)- or (2S,3E)-N-(X,Y)-3-amino-2-hydroxy-3-phenyl propionic acid-Z of Formula I, ##STR1## e.g. of (2E,3S)-3-amino-2-hydroxy-3-phenyl propionic acid or (2R,3S)-N-benzoyl-3-amino-2-hydroxy-3-phenyl propionic acid methylester. Compounds of type I are valuable intermediates in the total synthesis of Taxols which can be used in the treatment of various forms of cancer.

Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof.These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure ##STR1## in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L-Ala, L-Ile, L-Phe, L-Trp, L-Thr or an amide such as NHCH.sub.2 C.sub.6 H.sub.5 or NH(CH.sub.2).sub.2 C.sub.6 H.sub.5.

Abstract: The derivatives of N,N'-di(aralkyl)-N,N'-di(carboxyalkyl) alkylene di- or triamine and N-(aralkyl)-N'-(carboxyalkyl)-N'N'-di(carboxyalkyl) alkylene di- or triamine of the formula: ##STR1## and the salts and metallic complexes thereof are disclosed. Use in pharmaceutical or cosmetic compositions used to protect the organism from oxidizing stress situations linked to certain pathological states.

Abstract: Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R.sup.3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R.sup.4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

Abstract: Improvements to a six stage process for production of sodium l-thyroxine from l-tyrosine ?described in U.S. Pat. No. 2,889,363 and U.S. Pat. No. 2,889,364 (Baxter)! are described, the improvements comprising the oxidative coupling of a diiodo-l-thyrosine to form a biphenyl ether derivative, catalysed by a manganese salt in which the amine and acid functionally of the diiodo-l-thyrosine have been protected by suitable protecting groups, characterised in that the reaction is performed at a pressure of about 20 atmospheres in the presence of an organic amine additive using a gaseous oxidant comprising oxygen and optionally an inert diluent. The process optionally further comprises acid hydrolysis of the biphenyl ether derivative with hydrochloric acid to form a l-thyroxine hydrochloride salt and generation of sodium-l-thyroxine from the l-thyroxine hydrochloride salt.

Abstract: The invention features two novel antibiotics, termed 15352A and 15352B, having the structures shown in the figures.

Abstract: Inhibitors for matrix metalloproteases, pharmaueutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each Tis a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 reresents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12, and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.

Abstract: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.

Abstract: Oxalic acid diarylamides are described as useful monomers and comonomers in the polymerization of polycarbonates. The resin products resist degradation by ultra-violet light radiation. They can also be incorporated as comonomer or monomer in the polyester, polyester, polyether, polyethersulfone resins. They can also be used as UV stabilizers in the aforemetioned systems.

Abstract: The present invention relates to benzamidoxime derivatives represented by the formula ?I!; ##STR1## wherein R.sup.1 is unsubstituted or substituted C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted C.sub.2 -C.sub.4 alkenyl or unsubstituted or substituted C.sub.2 -C.sub.4 alkynyl, R.sup.2 is phenyl optionally having substituents or heterocycle optionally having substituents, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are each independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio or the like, and r.sub.1 and r.sub.2 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl or the like, having excellent fungicidal activity and being useful as a fungicide for agricultural and horticultural use, and methods for preparation thereof.

Abstract: The present invention provides novel compounds that affect excitatory amino acid receptors and are useful in the treatment of neurological disorders. This invention also provides synthetic methods for the preparation of the novel compounds.

Abstract: The present invention relates to the derivatives of formula: ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.

Abstract: The invention herein is directed to a process for the preparation of ethyl 3S-amino-4-pentynoate which involves treating 3-(trimethylsilyl)-2-propynal with L-phenylglycinol in toluene to produce .alpha.S-??3-(trimethylsilyl)-2-propynylidene amino!benzenethanol; reacting .alpha.S-??3-(trimethylsilyl)-2-propynylidene!amino!benzenethanol with BrZnCH.sub.2 CO.sub.2 t-Bu in THF/NMP to produce 1,1-dimethylethyl 3S-?(2-hydroxy-1S-phenylethyl)amino!-5-(trimethylsilyl)-4-pentynoate; reacting the 1,1-dimethylethyl 3S-?(2-hydroxy-1S-phenylethyl)amino!-5-(trimethylsilyl)-4-pentynoate with sodium periodate to form 1,1-dimethylethyl 3S-?(phenylmethylene)amino!-5-(trimethylsilyl)-4-pentynoate; hydrolyzing 1,1-dimethylethyl 3S-?(phenylmethylene)amino!-5-(trimethylsilyl)-4-pentynoate to produce 1,1-dimethylethyl 3S-amino-5-(trimethylsilyl)-4-pentynoate; transesterifying 1,1-dimethyl 3S-amino-5-(trimethylsilyl)-4-pentynoate and desilylating to produce ethyl 3S-amino-4-pentynoate.

Abstract: Heterocyclic acyldipeptides of the formula I ##STR1## wherein Z represents an oxygen or sulphur atom or a --CH.sub.2 -group;R.sub.1, R.sub.2 and R.sub.3 individually represent hydrogen or certain organic groups;R.sub.4 and R.sub.5, which are identical or different, represent an OR.sub.6 or NHR.sub.6 group, wherein R.sub.6 is hydrogen or certain organic groups;Y represents a --CH.sub.2 --, .dbd.CH-- or .dbd.N-- group;A represents a --(CH.sub.2).sub.3 -- group when Y is --CH.sub.2 --, the two rings being transcondensed, or a ##STR2## wherein R.sub.7 represents H, F, Br, Cl, nitro, or certain organic groups when Y is .dbd.CH-- or .dbd.N--; and their pharmaceutically acceptable salts are provided. These heterocyclic acyldipeptides and their salts are useful as active compounds in medicaments having immunostimulatory and antitumor activity.

Abstract: Substituted cyclohexene-1,2-dicarboxylic acid derivatives I ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are herein defined, or the agriculturally useful salts of Ia and Ib and intermediates for their preparation, which compounds are useful as herbicides and for the desiccation/defoliation of plants.

Abstract: A process for the preparation of (S)-N,N'-bis?2-hydroxy-1-(hydroxymethyl)ethyl!-5-(2-acetoxy-propionylamino )-2,4,6-triiodo-isophthalamide, an intermediate useful for the synthesis of iopamidol, by reaction between L-5-(2-acetoxy-propionylamino)-2,4,6-triiiodoisophthaloyl dichloride and 2-amino-1 ,3-propanediol in N-methylpyrrolidone and in the presence of a base, is described.

Abstract: Substituted phthalimidocinnamic acid derivatives I ##STR1## wherein the variables are as defined in the description are useful as herbicides and for the desiccation and/or defoliation of plants.

Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formula: ##STR1## wherein T is a substituent and R.sup.24 is a substituted amide moiety. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempera mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.

Abstract: The invention provides certain amino acid conjugates of substituted 2-phenyl-N-?1-(phenyl)-2-(1-heterocycloalkyl- or heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid receptors in mammalian tissue.

Abstract: This invention relates to the method of using specially formulated neurotrophic pipecolic acid derivative compounds having an affinity for FKBP-type immunophilins as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity to stimulate or promote neuronal growth or regeneration.

Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.

Abstract: Disclosed is a 7-(N-substituted amino)-3-oxo-2-phenylheptanoate derivative, 7-(N-substituted amino)-3-hydroxy-2-phenylheptanoate derivative, and 7-(N-substituted amino)-3-benzenesulfonyloxy-2-phenylheptanoate derivative, which are quite important major intermediates for an antidepressant. The 7-(N-substituted amino)-3-oxo-2-phenylheptanoate derivative can be manufactured by condensing an enolate of phenylacetates with a 5-(N-substituted amino) pentanoate derivative.

Abstract: The invention relates to borneol derivatives of general formula I ##STR1## in which R.sup.1 means C(O)--CH(OR.sup.6)--CH(NHR.sup.7)--R.sup.8,R.sup.2 means hydrogen, --OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, --OC(O)R.sup.9a, --OSO.sub.2 R.sup.9a, --OP(O)(OH).sub.2, NHR.sup.9a, NR.sup.9a R.sup.9b,R.sup.3 means hydrogen, --OH, C.sub.1 -C.sub.10 alkoxy, --OC(O)R.sup.9b, --OSO.sub.2 R.sup.9b, --OP(O)(OH).sub.2, orR.sup.2, R.sup.3 together mean an oxygen atom,R.sup.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.n --OR.sup.11a,R.sup.5 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.p --OR.sup.11b, orR.sup.4, R.sup.5 together mean an oxygen atom, a=CHR.sup.10 group,n means 0 to 8,p means 1 to 8,R.sup.7 means --C(O)R.sup.12, --SO.sub.2 R.sup.12, --C(O)OR.sup.12, --C(O)NHR.sup.9d, --C(O)NR.sup.9d R.sup.9e, ##STR2## R.sup.8 means aryl, R.sup.9a-e, R.sup.12 are the same or different and mean C.sub.1 -C.sub.10 alkyl, C.sub.4 -C.sub.8 cycloalkyl, aryl, C.sub.7 -C.sub.16 aralkyl,R.sup.