Abstract: The present invention relates to the use in the treatment of cognitive disorders associated with the aging processes of the brain and perinatal brain disorders of compounds which act as inhibitors of the enzyme kynurenine aminotransferase (KAT).The present invention also provides, as novel compounds, a selected class of KAT inhibitors which are the compounds of formula (IA) ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.6 -C.sub.10 aryloxy, phenyl-C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, andR.sub.1 is hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, mono-C.sub.1 -C.sub.6 alkylamino, di-C.sub.1 -C.sub.6 alkylamino, hydroxylamino, C.sub.1 -C.sub.4 alkoxyamino or benzyloxyamino,with the provisos that:(i) when R.sub.1 is hydroxy and, at the same time, R is halogen, then this halogen is not fluorine; and(ii) when R.sub.1 is hydroxy and, at the same time, R is C.sub.1 -C.sub.6 alkyl, then this C.sub.1 -C.sub.

Abstract: The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, Q, W, X, Y, Z and n are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.

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: Fullerene derivatives, methods of preparing the same and methods of using the same, wherein the fullerene derivatives are of the formula I ##STR1##

Abstract: 6-dimethylaminomethyl-1-phenyl-cyclohexane compounds, methods of preparing them and the use of these compounds in drugs are described.

Abstract: A fungicidal compound of formula (I): ##STR1## wherein A is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; and one of R.sup.1 and R.sup.2 is optionally substituted isoquinoline while the other is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halogen or cyano.

Abstract: The present invention provides a novel one-step process for preparing substituted aryls which can be used as end-capping monomers for preparing highly branched macromolecule polymers that have highly controlled molecular architectures. The process comprises the steps of (a) reacting an aromatic acid with an activating carbodiimide for a sufficient period of time and under suitable conditions of temperature and pressure to form an activated aromatic intermediate, and (b) reacting said intermediate with a suitable nucleophile for a sufficient period of time and under suitable conditions of temperature and pressure to form said substituted aryl compound.

Abstract: N-arylmethylene ethylenediaminetriacetate, N-arylmethylene iminodiacetate or N,N'-diarylmethylene ethylenediaminediacetate type compounds and their use in combatting oxidative stress, and pharmaceutical and cosmetic compositions comprising said compounds. The invention also concerns a process for the preparation of said compounds.

Abstract: Substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 is R.sup.3 -substituted aryl;Ar.sup.2 is R.sup.4 -substituted aryl;Ar.sup.3 is R.sup.5 -substituted aryl;Y and Z are independently --CH.sub.2 --, --CH(lower alkyl)- or --C(dilower alkyl)-;A is --O--, --S--, --S(O)-- or --S(O).sub.2 --;R.sup.1 is --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.2 is hydrogen, lower alkyl or aryl; or R.sup.1 and R.sub.2 together are .dbd.O;q is 1, 2 or 3; p is 0, 1, 2, 3 or 4;R.sup.5 is 1-3 substituents independently selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.9, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 -lower alkyl, --NR.sup.6 SO.sub.2 -aryl, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 -alkyl, S(O).sub.0-2 -aryl, --O(CH.sub.2).

Abstract: The invention relates to a process for the production of diethylenetriaminepentacarboxylic acid tetraesters of general formula I ##STR1## in which R.sup.1 and Z have different meanings.

Abstract: Diethylenetriaminepentaacetic acid monoamide derivatives, their complexes and complex salts, containing an element of atomic numbers 21-29, 31, 32, 39, 42-44, 49 or 57-83, pharmaceutical agents containing these compounds, their use as contrast media and process for their production.

Abstract: Reaction products of amino-alkylenecarboxylic acids with polyoxyalkylene compounds are used as paraffin dispersants for mineral oil middle distillates.

Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein Ar is a mono- or bicyclic aromatic group optionally containing one or two heteroatoms independently selected from nitrogen, oxygen and sulphur, said group being optionally substituted by one or more atoms or groups independently selected from halogen, nitro, amino, --NRR.sup.1 where R and R.sup.1 are independently selected from hydrogen, C.sub.1-8 alkyl and C.sub.1-8 alkanoyl, cyano, carboxyalkoxy, alkoxycarbonylalkoxy, C.sub.1-8 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-8 alkoxy (including cycloalkoxy and cycloalkylalkoxy), C.sub.

Abstract: Novel butadiene derivatives of the formula [I]: ##STR1## wherein Ring A is tri-lower alkoxyphenyl, R.sup.1 and R.sup.2 combine each other to form a group of the formula: ##STR2## or one of R.sup.1 and R.sup.2 is lower alkoxy, and the other is group of the formula: -NHR.sup.3, in which R.sup.3 is hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted amino, hydroxy or pyridylcarbonyl, or salts thereof, these compounds have excellent antithrombotic activity and are useful as antithrombotic drug, or synthetic intermediate for preparing other antithrombotic drug.

Abstract: Process for enriching the concentration of an enantiomer (or a diastereomer) in a mixture of optically active isomers. The process includes preparing a solution containing the mixture of the optically active isomers and a chiral collector in which the chiral collector and the enantiomer (or diastereomer) are associated with each other. A gas is bubbled through a pool of the solution to form a foam, the surfaces of the bubbles in the foam having the chiral collector and the enantiomer (or diastereomer) preferentially adsorbed thereto so that the concentration ratio of the optically active isomers at said bubble surfaces differs from that in the bulk of the pool. The foam is moved vertically through a column above the pool such that during said movement at least a portion of the bubbles comprising the foam break thereby allowing liquid to drain toward the pool to provide an internal reflux within the column.

Abstract: N-arylmethylene ethylenediaminetriacetate, N-arylmethylene iminodiacetate or N,N'-diarylmethylene ethylenediaminediacetate type compounds and their use in combatting oxidative stress, and pharmaceutical and cosmetic compositions comprising said compounds. The invention also concerns a process for the preparation of said compounds.

Abstract: The invention relates to novel asymmetrically substituted diaminodicarboxylic acid derivatives of the formula ##STR1##

Abstract: There is disclosed a method of synthesizing a compound of the formula ##STR1## and novel analogs of the formula ##STR2## where R and R.sub.1 are fully defined. These compounds exhibit beneficial antiviral properties especially as inhibitors of the influenza virus.

Abstract: Amidinophenol derivatives of the formula (I) ##STR1## wherein the various symbols are as defined herein; which have inhibitory activities on PLA.sub.2 and on various proteases such as trypsin, plasmin, thrombin, kallikrein, especially trypsin, and are useful for the prevention and/or the treatment of various inflammatory diseases, allergic diseases, disseminated intravascular coagulation, pancreatitis, severity in pancreatitis and multiple organ failure.

Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.

Abstract: This invention relates to a method for preparing .beta.-phenylisoserine and analogues thereof having general formula (I) ##STR1## from an aromatic aldehyde and an .alpha.-methylarylamine-S, and through a lactam of general formula (II) as described herein. The acids of general formula (I) (R.dbd.H) may be used to prepare taxane derivatives having remarkable antitumoral and antileukaemic activity.

Abstract: Reduction and resolution methods for the preparation of compounds useful as intermediates in the preparation of taxanes, and particularly for preparation of desired stereoisomers for use in the formation of the C-13 sidechain of pharmaceutically useful taxanes such as paclitaxel.

Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: Compounds of the formula (I): Ar.sub.1 --CH(OH)--CH.sub.2 --NH--CH.sub.2 --X--CH.sub.2 --E--(CH.sub.2).sub.n --Y--Ar.sub.2, in which the substituents and symbols have the meanings given in the description, are novel active compounds having, in particular, a broncholytic action.

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 the formula: ##STR1## wherein R.sup.1 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aralkanoyl, heterocyclylcarbonyl or a group of the formula: ##STR2## R.sup.2 is alkyl, cycloalkylalkyl or aralkyl; R.sup.3 is hydrogen and R.sup.4 is hydroxy or R.sup.3 and R.sup.4 together are oxo; R.sup.5 is alkoxycarbonyl or alkylcarbamoyl; R.sup.6 and R.sup.7 together are trimethylene or tetramethylene optionally substituted by alkyl or on adjacent carbon atoms by tetramethylene; R.sup.8 is alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, aroyl, aralkanoyl or heteroeyelylearbonyl; and R.sup.9 is alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, cyanoalkyl, carbamoyl-alkyl, alkylthioalkyl, alkoxyalkyl or alkoxycarbonylalkyl:and pharmaceutically acceptable acid addition salts of those compounds of formula I which are basic, inhibit aspartyl proteases of viral origin and can be used in the form of medicaments for the prophylaxis or treatment of viral infections.

Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description,its optical isomers and its addition salts thereof with a pharmaceuticaliy-accepable acid or base,and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.

Abstract: Disclosed herein are compounds which inhibit human immunodeficiency virus (HIV) protease activity and inhibit HIV replication in human cells. Thus, the compounds are indicated for the treatment of HIV infections. The compounds can be represented by the formula ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an arylalkyl carbamoyl; A is absent or an amino acid or a derived amino acid; either R.sup.1 or R.sup.2 is hydrogen while the other is alkyl or R.sup.1 and R.sup.2 are joined to form a cyclohexane; Q is hydrogen, hydroxy, halo or lower alkoxy; and Y is a terminal group, for example, an alkylamino, alkoxy or an optionally substituted anilino.

Abstract: Substituted phenols of the formula I ##STR1## processes for their preparation and compositions containing substituted phenols of the formulae I and II ##STR2## for the treatment of disorders caused by cell proliferation, such as psoriasis, tumor disorders and immunological disorders, are described.

Abstract: Acid esters of formula, ##STR1## wherein R2 is lower-alkyl, or acid-addition salts thereof useful as intermediates in the production of beta-aminoalcohols.

Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.

Abstract: The invention relates to a process for the production of diethylenetriaminepentacarboxylic acid tetraesters of general formula I ##STR1## in which R.sup.1 and Z have different meanings.

Abstract: This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.

Abstract: A process and catalyst composition are provided for the highly efficient enantioselective hydrogenation of dehydroamino acid derivatives. The catalyst composition comprises rhodium or iridium and a diphosphinite carbohydrate ligand, wherein the phosphorous atoms are attached to aromatic groups substituted with electron-donating substituents. Also provided is a means to selectively produce .alpha. amino acids in either the L or the D form, based upon use of a sugar in the ligand with phosphinites attached in an absolute Right-Left or Left-Right configuration, respectively.

Abstract: Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; orR.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)- wherein R.sub.7a is loweralkyl or benzyl; orR.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.

Abstract: An N-acylamino acid compound represented by the general formula (1):R--CO--(NH--X--CO).sub.n --OR.sup.1 (1)wherein (NH--X--CO) is an amino acid residue, X in (NX--X--CO) is variable with the kind of amino acid to be used, R--CO is a saturated or an unsaturated fatty acid residue having 6 to 24 carbon atoms, R.sup.1 is hydrogen atom, sodium atom, potassium atom, or methyl group and n is an integer in the range of from 1 to 3, indicating that at least one histidine is contained as a component amino acid is disclosed, which is obtained by causing an N-hydroxysuccinimide ester to react with an amino acid or a peptide.The compound excels in antioxidizing power, emulsifying power, antibacterial power, chelating power, infrared absorbing power, and humidity-retaining power.

Abstract: Fused tricyclic compounds of formula (I) as disclosed herein, and salts and prodrugs thereof, are tachykinin antagonists, useful for treating pain.

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: Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom, an alkyl or alkoxycarbonyl radical or a phenyl radical, optionally substituted,R.sub.2 represents an alkoxy, optionally substituted cycloalkyloxy, cycloalkylalkyloxy, phenylalkyloxy, polyfluoroalkyloxy or cinnamyloxy radical or a radical --NR.sub.5 R.sub.6,R.sub.3 represents a phenylamino radical in which the phenyl ring is optionally substituted, an optionally substituted phenyl radical or a naphthyl, indolyl or quinolyl radical,R.sub.4 represents a substituted phenyl radical,R.sub.5 and R.sub.6, which may be identical or different, represent a hydrogen atom or an alkyl, optionally substituted phenyl, indanyl, cycloalkylalkyl, cycloalkyl or phenylalkyl radical, or alternatively R.sub.5 and R.sub.6, together with the nitrogen atom to which they are attached, form a heterocycle, their preparation and medicinal products containing them.

Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents optionally substituted phenyl, naphthyl, indolyl, benzothiophenyl, benzofuranyl, benzyl or indazolyl; Z represents O, S or NR.sup.8 ; X and Y are H or are together .dbd.O; R.sup.1 and R.sup.2 are H; optionally substituted C.sub.1-6 alkyl; optionally substituted phenyl(C.sub.1-4 alkyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ; R.sup.3 is H or C.sub.1-6 alkyl, R.sup.4 is H , C.sub.1-6 alkyl or optionally substituted phenyl; and R.sup.5 represents optionally substituted phenyl; are tachykinin antagonists. They and compositions thereof are useful in therapy.

Abstract: The present invention relates to the compounds of the formula: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently hydrogen, lower alkyl which is optionally substituted, lower alkoxy which is optionally substituted, hydroxy, acyloxy, or halogen; R.sup.9 is hydrogen, hydroxy, acyloxy, lower alkyl which is optionally substituted, lower alkoxy which is optionally substituted, or lower alkylamino which is optionally substituted; E.sup.1 is hydrogen, or an ester residue; m is an integer of from 1 to 4;or a pharmaceutically acceptable salt thereof. The compounds of the present invention exhibit phospholipase A.sub.2 inhibitory activity, and can be used in treating inflammatory conditions.

Abstract: 6-amino carboxylic acid derivatives having antiasthmatic and antiallergic properties which can be used for the preparation of medicaments. The compounds have the formula: ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen, a straight-chain or branched alkyl radical with 1-6 carbon atoms, benzyl or phenylethyl, R.sub.3 represents hydrogen, a straight-chain or branched alkyl radical with 1-6 carbon atoms or benzyl, X represents hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy, Y.sub.1 and Y.sub.2 represent hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy, where m, n and o can assume the values from 0-4.

Abstract: A compound which is selected from those of formula (I): ##STR1## in which A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined in the description, its optical isomers, and its addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same which are useful for treating a disorder of the melatoninergic system.

Abstract: Process for the enantioselective preparation of phenylisoserine derivatives of general formula (I), in which R represents a phenyl or tert-butoxy radical, R.sub.1 represents a hydrogen atom or an alkyl radical containing 1 to 4 carbon atoms and R.sub.2 represents a hydrogen atom or a group protecting the alcohol function.

Abstract: A process for the production of a .beta.-aminoalcohol 2-[3(S)-amino-2(R)-hydroxy-4-phenylbutyl]-N-tert.butyl-decahydro-(4aS,8aS) -isoquinoline-3(S)-carboxamide of the formula ##STR1## via the oxazolidinone corresponding to the aminoalcohol 10, as well as intermediates occurring in this process.

Abstract: Amidinophenol derivatives of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are (i) H, (ii) C1-4 alkyl, (iii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO.sub.2, (vii) benzoyl, (viii) COOR.sup.4 (in which R.sup.4 is C1-3 alkyl); A is bond, C1-4 alkylene, --C(R.sup.5).dbd.C(R.sup.6)-- (in which R.sup.5 and R.sup.6 are H or C1-4 alkyl; R.sup.3 is (i) CON(R.sup.7)(R.sup.8), (ii) CON(R.sup.9)--CH(R.sup.7)(R.sup.8) or (iii) ##STR2## in which ##STR3## is 4-7 membered, mono-cyclic hetero ring containing 1 or 2 N atom; R.sup.10 is H, C7-10 phenylalkyl or COOR.sup.13 (in which R.sup.13 is H, C1-4 alkyl or C7-10 phenylalkyl)); with the proviso that (i) both R.sup.7 and R.sup.8 do not represent hydrogen at the same time, and (ii) when at least one group in R.sup.7, R.sup.8 and R.sup.9 represents the group containing t-butyl ester, the other groups do not represent tile group containing carboxy; or an acid-addition salt thereof, have inhibitory activities on PLA.sub.

Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.

Abstract: Compounds of general formula I: ##STR1## Wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are variables. These compounds have collagenase inhibition activity and are useful in the management of disease involving collagen degradation. Its uses include rheumatoide arthritis, corneal ulceration, osteoporosis, periodontitis, gingivitis and tumor invasion.

Abstract: Compounds of the formula I ##STR1## where n, W, X, Y, Z, R.sup.1, R.sup.2, and R.sup.3 are as defined herein exhibit fungicidal, insecticidal, and acaracidal activity.

Abstract: The invention relates to carbacyclin derivatives of Formula I ##STR1## wherein the various substituents are defined herein, including, inter alia,if R.sub.2 is a hydrogen atom, their salts with physiologically compatible bases, their cyclodextrin clathrates, and their use as medicinal agents.