Abstract: A substance PF1191 having an inhibitory activity to kainic acid toxicity represented by the following formula (I) which is obtained by incubating a fungus belonging to the genus Eupenicillium and isolating the product thus produced from the culture by solvent extraction, adsorption column chromatography, gel filtration, etc.

Abstract: There are disclosed a process for producing the optically active cyclic amino acid ester derivative of the formula (I): by optical resolution method, a process for producing the same and a process for producing an optically active cyclic amino acid using the compound of the formula (I).

Abstract: 3-Pyrroline-2-carboxylic acid derivatives of the formula I ##STR1## are prepared by eliminating the sulfonic acid residue, with the aid of a base, from a compound of the formula II ##STR2##

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: Compounds of formula (I) ##STR1## wherein the substituents are as defined herein, are antiparasitic agents.

Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.

Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: The invention encompasses a method for the stereoselective synthesis of alkyl proline and other amino acid derivatives which are intermediates of the farnesyl-protein transferase inhibiting CA.sup.1 A.sup.2 X motif of the protein Ras. The instant process employs an efficient diastereoselective ?2,3!-Wittig rearrangement of .alpha.-allyloxy amide enolates mediated by a chiral auxiliary to provide acyclic and cyclic precursors.

Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: The invention relates to novel pyrrolidine derivatives represented by formula (1): ##STR1## wherein: R1 represents (1) a lower alkyl group having 1 to 6 carbon atoms, or (2) a 3- to 15-membered mono- or fused cyclic hydrocarbon group which may contain a hetero atom on the ring, or which may be substituted with a substituent(s); each of n and m represents an integer and the sum of n and m is an integer of 0 to 2; each of X and E represents oxygen, NR' (wherein R' is hydrogen or a lower alkyl group having 1 to 6 carbon atoms), sulfur, phenylene, CH.dbd.CH or CH.sub.2 ; A represents an amino acid residue or an imino acid residue, which functional group may be optionally protected, or a glycine residue which may be substituted at the amino moiety thereof; and, Y1 represents a cycloalkyl group having 3 to 8 carbon atoms; or a salt thereof. The pyrrolidine derivatives inhibit a prolyl endopeptidase and are expected to be effective for the treatment of amnesia.

Abstract: A prolineamide derivative represented by the formula (I): ##STR1## or a salt or hydrate thereof or a pharmaceutically acceptable salt thereof, which has a protease inhibition activity and is useful as an active ingredient of pharmaceutical compositions is provided.

Abstract: Disclosed is a compound of the formula ##STR1## wherein R.sup.1 is H, NH.sub.2, or OCH.sub.3, R.sup.2 is an optionally substituted cyclic group optionally containing one or more heteroatoms, R.sup.3 and R.sup.4 are independently H or C.sub.1-4 alkyl, m is 0-4, n is 0-6, p is 0.1, X is CN, CSNH.sub.2, PO(OH).sub.2, COOH, SO.sub.2 NH.sub.2, NH.sub.2, OH, CNHNH.sub.2, tetrazole, triazole, or COR.sup.5 where R.sup.5 is C.sub.1-4 alkyl, CF.sub.3, NH.sub.2, or OC.sub.1-4 alkyl, and Y is O or NH that is useful as a pharmaceutical.

Abstract: A guanidine derivative represented by formula (1), (2), (3) or its acid addition salt and a production process thereof ##STR1## wherein each of A and B is a C.sub.2 -C.sub.8 alkylene, D is a single bond, --CO-- or a C.sub.1 -C.sub.5 alkylene, E is H, a lower alkyl or the like, m is 1 to 6, n is 0 to 6 and R.sup.1 is H, a lower alkyl or the like, l is 1 to 10 and G is H, --OH or the like and a skin cosmetic containing the same. It can exert excellent keratin layer softening effect continuously for a long period of time.

Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: Compounds which suppress human T-lymphocyte proliferation are disclosed.

Abstract: The invention is directed to 3-aminopyrroles of formula I, which are largely new, to methods for the preparation and to their use as medicinal agents and preparations, as well as to anti-convulsive or analgesic preparations containing these 3-aminopyrroles.Disubstituted and monosubstituted amino groups are claimed as 3-amino substituents.The invention pursues the objective of developing largely new 3-aminopyrroles, which have CNS activity, particularly ones which anti-convulsive or analgesic properties, as well as methods for their preparation and their use as medicinal preparations.Pursuant to the invention, the synthesis is carried out by cyclizing open-chain precursors, such as aminoacrylic acid derivative, or by modifying pyrroles.

Abstract: Disclosed herein are compounds of the following formula: ##STR1## wherein R.sup.1 is a group of the formula ##STR2## "X" is CH.sub.2 or N, "Z" is O, S, or N--R.sup.6, "A" is an amino acid residue, and Y, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are substituent variables as defined herein.The compounds are antagonists of tachykinin, and as such are useful for alleviation of pain and for treatment of disorders including asthma, bronchitis, rhinitis, conjunctivitis, dermatitis, arthritis, and urticaria.

Abstract: Compounds which suppress human T-lymphocyte proliferation are disclosed.

Abstract: Nitric esters with pharmacological activity having general formula (I), their pharmaceutical utilisation and process for their preparation.

Abstract: The invention generally relates to compounds of the formula I, which are in equilibrium with their 4-hydroxy tautomers, and their pharmaceutically acceptable salts: ##STR1## where n is 0 to 2; A is S, CH.sub.2, O, NH or Se, and when n is 0, A is not CH.sub.2, and when n is 1, A is not CH.sub.2 or NH; X is a substituted or unsubstituted C.sub.1 -C.sub.3 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.3 alkynyl or amino, or sulfur or oxygen; Ar is a substituted or unsubstituted monocyclic carbocycle or heterocycle, or fused or nonfused polycyclic carbocycle or heterocycle; and R.sub.1 and R.sub.2 are hydrogen or a moiety that forms together with the attached CO.sub.2 a readily hydrolyzable ester group. These compounds and their salts are useful as inhibitors of GARFT or as antiproliferative agents. The invention also pertains to pharmaceutical compositions and methods employing such Compounds as GARFT inhibitors or antiproliferative agents.

Abstract: There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.

Abstract: This invention provides a process for preparing kainic acid and provides intermediates in the synthesis thereof.

Abstract: Compounds that selectively modulate the remodeling pathway of platelet activating factor (PAF) are described. Related pharmaceutical compositions and methods are also disclosed. These compounds, pharmaceutical compositions and methods are useful for reducing or eliminating inflammation.

Abstract: Compounds of formula (I) and pharmaceutical compositions containing the compounds of formula (I): ##STR1## are provided. In formula (I): Ar is a substituted or unsubstituted aromatic or heterocyclic group; R is H or a substituted or unsubstituted straight or branched chain, cyclic or mixture of straight branched and cyclic alkyl, alkenyl, or alkynyl group having from 1-20 carbon atom; A is a functional group that bears a polar moiety; R.sub.1 is R, R--C=0, R substituted with one or more heteroatoms, a substituted or unsubstituted aryl group, or is aryl-(CH.sub.2).sub.n ; R.sub.2 is (CH.sub.2).sub.n, CHR, C(R).sub.2, COO, OCO, NHCO, CONH, SO, SO.sub.2 or NR; R.sub.3 and R.sub.4, which are the same or different or each may be absent, and are .dbd.O, H, O-aryl, OR, O-alkyl or alkyl, aryl, SR, S-aryl, NHR, NH-aryl, NR, or are other heteroaromatic groups; R.sub.5 is H, OH or R; E and F, which are the same or are different, are either N or (CH.sub.2).sub.

Abstract: A process for separating a selected amino acid (enantiomer) from a mixture of different compounds including other amino acids is disclosed, in which process the mixture is contacted with a polymer material which is composed of cross-linked, amino-acid-based monomer units, said polymer material containing a molecular print of the selected amino acid. In the molecular print there is also bound a diastereomeric complex between the selected amino acid (enantiomer), a divalent metallic ion and the amino-acid-based monomer unit. Also the amino-acid-based monomer unit and a process for preparation thereof, as well as a polymer material composed of the amino-acid-based monomer unit and a process for the preparation thereof are disclosed.

Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds on solid supports and synthetic compound libraries comprising pyrrolidine groups prepared by such methods.

Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds and derivatives thereof on solid supports and synthetic compound libraries comprising pyrrolidine groups and derivatives thereof prepared by such methods.

Abstract: 1S,4S and 1R,4R-2-Alkyl-2,5-diazabicyclo[2.2.1]-heptanes useful as intermediates in the synthesis of certain antibacterial quinolones, are prepared respectively, from trans-4-hydroxy-L-proline and trans-4-hydroxy-D-proline via multistep procedures.

Abstract: D,L-, L- and D-phenyl alanine derivatives of formula (I) defined in claim 1 in which R.sub.1 is an amidino-, guanidino-, oxamidino-, aminomethyl- or amino group have been discovered which effectively prevent blood coagulation or thrombosis. The antithrombotically active compounds have low toxicity and may be administered by mouth, subcutaneously or intravenously.

Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, Het and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described. The compounds of formula I are useful in the treatment of cardiovascular diseases.

Abstract: The invention is directed to 3-aminopyrroles of formula I, which are largely new, to methods for the preparation and to their use as medicinal agents and preparations, as well as to anti-convulsive or analgesic preparations containing these 3-aminopyrroles.Disubstituted and monosubstituted amino groups are claimed as 3-amino substituents.The invention pursues the objective of developing largely new 3-aminopyrroles, which have CNS activity, particularly ones which anti-convulsive or analgesic properties, as well as methods for their preparation and their use as medicinal preparations.Pursuant to the invention, the synthesis is carried out by cyclizing open-chain precursors, such as aminoacrylic acid derivative, or by modifying pyrroles.

Abstract: A class of cysteine protease inhibitors which inactivate a cysteine protease by covalently bonding to the protease and releasing a heterocyclic leaving group is presented. The cysteine protease inhibitors of the present invention comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a heterocyclic leaving group. The heterocyclic leaving group of the protease inhibitor is of the formula: --O-- Het, where Het is a heterocycle having 4-7 atoms in the ring, with at least one of the heterocycle atoms being N, O or S.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is aryl, or a group of the formula: ##STR2## wherein X is CH or N, and Z is O or N--R.sup.5,in which R.sup.5 is hydrogen or lower alkyl,R.sup.2 is hydroxy or lower alkoxy,R.sup.3 is hydrogen or lower alkyl which may have suitable substituent(s),R.sup.4 is ar(lower)alkyl which may have suitable substituent(s),A is carbonyl or sulfonyl, andY is a bond or lower alkenylene,and pharmaceutically acceptable salt thereof. The disclosed compounds are useful for treating respiratory diseases such as bronchaedema.

Abstract: This invention is concerned with novel compounds represented by structural formulae I and II. ##STR1## which are useful in the treatment of cardiac arrhythmia.

Abstract: There is provided a simple quantitative procedure for the chlorination of pyrrole compounds containing electron withdrawing substituents via the displacement of bromine with chlorine on the pyrrole nucleus.

Abstract: Novel O.sub.10eq -derivatives of ryanodine and dehydroryanodine characterized as binding strongly to ryanodine receptor, useful in affecting Ca.sup.++ efflux in tissue and also in isolating ryanodine receptor from sarcoplasmic reticulum. Also described are novel radio-iodinated alanine derivatives useful to radio label ryanodine and dehydroryanodine derivatives.

Abstract: The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;each of the B groups, which are the same, isa) a saturated or unsaturated, carbocyclic or condensed carbocyclic ring substituted by one or more acid groups;b) a saturated or unsaturated, heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen, oxygen and sulphur, substituted by one or more acid groups;c) a pyranyl or furanyl sugar residue substituted by one or more acid groups; ord) a --CH.sub.2 (CHA).sub.r CH.sub.2 A group, wherein each A group, being the same or different, is an acid group and r is 0, 1 or 2; and the pharmaceutically acceptable salts thereof, which are useful as angiogenesis inhibitors.

Abstract: Aroyl(piperidinyl and piperazinyl)acyl pyrroles of the following formula have anxiolytic activity: ##STR1## wherein, Y is selected from the group consisting of N, CH or COH;A.sup.1 is selected from the group consisting of ##STR2## n is an integer from 1 to 5;R.sup.1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 and R.sup.3 are selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.4 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; andR.sup.5 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; and acid addition salts thereof.

Abstract: A process for producing pharmacologically active 1-unsubstituted 3-aminopyrroles of the formula ##STR1## by ring transformation of a corresponding 1,2-thiazolium pyrrole in a single step, without producing harmful byproducts.

Abstract: This invention relates to novel polyfluorinated alkyl derivatives of certain tripeptides, to the methods for their preparation, the intermediates therefore, to their use in inhibiting thrombin and lung tryptase and in their end-use application as anti-coagulants useful in treating thrombophlebitis and coronary thrombosis and in the treatment of asthma.

Abstract: The substitution of the L-Pro at the 7-position of the peptide hormone bradykinin or other substituted analogs of bradykinin with a D-configuration hydroxyproline ether or thioether converts bradykinin agonists into bradykinin antagonists. The invention further includes the intermediate compounds and additional modifications at other positions within the novel 7-position modified bradykinin antagonists which increase enzyme resistance, antagonist potency, and/or specificity of the new bradykinin antagonists. The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.

Abstract: Compounds which suppress human T-lymphocyte proliferation are disclosed. The active compounds essentially contain at least the following structure: ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, n, X.sup.1 and Z are defined in the specification.

Abstract: The invention comprises compositions and methods for the treatment of psoriasis.

Abstract: Optically active pyrrolidine derivative represented by the following formula (XI): ##STR1## wherein R.sup.1 represents a benzyl group R.sup.2 represents an alkyl group having 1 to 6 carbon atoms, R.sup.3 represents an alkyl group having 1 to 6 carbon atoms, a benzyl group or an allyl group, R.sup.4 is selected from the group consisting of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms which may be substituted with a protected hydroxyl group, a vinyl group, a phenyl group which may be substituted, a benzyl group which may be substituted, and a heterocyclic ring having 1 to 4 nitrogen or/and oxygen atoms, and R.sup.5 represents a hydrogen atom or a methyl group.This compound can be an intermediate for synthesis of carbapenem antibiotic compounds.

Abstract: The present invention provides a process for the production of calcium salts of hydantoic acids and which comprises the steps of reacting a hydantoin with a calcium base material such as calcium hydroxide in an aqueous medium at a sufficient temperature and for a sufficient period of time to form the calcium salt of the corresponding hydantoic acid and then separating the calcium salt of such acid from the reaction mass. This separation can include the further steps of cooling the reaction mass down to facilitate the precipitation of the acid/salt crystals and then separating the precipitate by means of filtering or centrifugating. These acids can then be subjected to a HNO.sub.2 -mediated decarbamoylation process followed by an optical resolution step to thus provide high yields of D-p-hydroxyphenylglycine which is a key synthetic immediate or building block for semi-synthetic penicillin and cephalosporins.

Abstract: Compounds of the general formula (I): ##STR1## where A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are defined in the description.Medicinal products.

Abstract: Novel alkylenediamine derivatives effectively employable glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5 R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.

Abstract: This invention relates to the preparation of 3- and/or 4-substituted pyrrolidine catalysts corresponding to formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, X.sub.1, X.sub.2, and Y have the meanings described for formula (I) and to use of such catalysts in the polyisocyanate polyaddition process.

Abstract: Nitrogen-containing heterocyclic (poly) peroxycarboxylic acid monopersulfates which have the formula: ##STR1## wherein the symbols have the following meanings: R represents a hydrogen atom or an alkyl, (hetero)cycloalkyl, (hetero)aryl, alkyl-aryl or arylalkyl group, wherein said groups are optionally substituted, or a carboxylic group or a peroxycarboxylic group, or any other substituents non-reactive in the presence of the peroxycarboxylic group;R.sup.1 represents an alkyl group > C.sub.5 ;n is a number selected from 0,1 and 2;m is a number selected from 1, 2 and 3;and the heterocyclic ring may be in its turn condensed with at least one further (hetero) aromatic or (hetero)cycloalkylic ring. The invention relates to a preparation process for, and to their use, as bleaching agents.

Abstract: Novel pyrrolecarboxylic acid derivatives represented by the following formula: ##STR1## where R.sup.1 is a hydrogen atom, an alkyl group of 5 to 25 carbon atoms or an alkenyl group of 5 to 25 carbon atoms, R.sup.2 is a hydrogen atom, a phenyl group or an optionally substituted alkyl group of 1 to 10 carbon atoms, and R.sup.3 is a hydrogen atom, an alkyl group of 5 to 25 carbon atoms or an alkenyl group of 5 to 25 carbon atoms, or pharmaceutically acceptable salts thereof are provided.The compounds are highly effective in reducing the level of triglyceride or cholesterol in serum, and useful as an active ingredient of a pharmaceutical composition for treating hyperlipemia and arteriosclerosis.