Abstract: A method for stimulation of transcription factor AP (activator protein)-1 by administering a compound of the formula (I) wherein R is selected from methyl, ethyl, n-propyl, iso-propyl, c-propyl, n-butyl, sec.-butyl, iso-butyl, tert.-butyl, c-butyl, n-pentyl, sec.-pentyl, iso-pentyl, tert.-pentyl, neo-pentyl, c-pentyl, c-hexyl and c-heptyl; RNa and RNb are the same or different and selected from hydrogen, methyl and ethyl; R2, R3, R5 and R6 are independently selected from hydrogen, methyl, methoxy, thiomethyl, hydroxy, fluoro, chloro, bromo, trifluoromethyl, phenyl and benzyl; n is 1, 2 or 3; R′ and R″ are the same or different and selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, sec.-butyl, and iso-butyl or R′ and R″ together form a saturated heterocyclic ring of 5-7 atoms; and pharmaceutically acceptable salts, hydrates and solvates thereof, to a mammal in need thereof.

Abstract: A methods of treating an infection comprises administering a therapeutically effective amount of a compound described by the Formula (I): wherein: X may be O, S, or NR′ wherein R′ is H or loweralkyl, R1 and R2 may be independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl; R3 and R4 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, and oxyarylalkyl; R5 is represented by a formula selected from the group consisting of: wherein: X1, X2, and X3 are independently selected from O and S; and R6 and R7 are independently selected from the group consisting of loweralkyl, aryl, alkylaryl, oxyaryl, an ester-containing substituent, and oxyalkyl; or a pharmaceutically acceptable salt thereof.

Abstract: Propanolamine derivatives represented by the following formula (I): These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.

Abstract: Disclosed are novel compounds, and methods of making the same, represented by Structural Formula II, IX or XXVII: The compounds can be used to prepare combinatorial libraries based on a multicomponent Ugi reaction.

Abstract: Compounds having the formula (I), 1

Abstract: A method for synthesizing Salacinol, its stereoisomers, and non-naturally occurring selenium and nitrogen analogues thereof having the general formula (I): The compounds are potentially useful as glycosidase inhibitors. The synthetic schemes comprise reacting a cyclic sulfate with a 5-membered ring sugar containing a heteroatom (X). The heteroatom preferably comprises sulfur, selenium, or nitrogen. The cyclic sulfate and ring sugar reagents may be readily prepared from carbohydrate precursors, such as D-glucose, L-glucose, D-xylose and L-xylose. The target compounds are prepared by opening of the cyclic sulfates by nucleophilic attack of the heteroatoms on the 5-membered ring sugars. The resulting heterocyclic compounds have a stable, inner salt structure comprising a heteroatom cation and a sulfate anion. The synthetic schemes yield various stereoisomers of the target compounds in moderate to good yields with limited side-reactions.

Abstract: The invention relates to treating neurodegeneration by selective blocking of NMDA receptor with compounds of formula wherein Ar1 is pyridyl or phenyl, substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group  wherein Z1 is a five membered heterocyclic ring, which contains one or two heteroatoms, selected from N or O; R1 is hydrogen, hydroxy or an oxo group; Ar2 is pyridyl or phenyl, optionally substituted by hydroxy, lower alkyl, halogen, amino, nitro, benzyloxy or lower alkoxy-lower alkoxy, or is the group  wherein Z2 is a five or six membered ring, which optionally contains one or two heteroatoms, selected from N or O; and Q, X, A, Y B are as defined in the specification.

Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to prodrugs of compounds which selectively inhibit cyclooxygenase-2. The use of non-steroidal antiinflammatory drugs (NSAIDs) in treating pain and the swelling associated with inflammation also produce severe side effects, including life threatening ulcers. The recent discovery of an inducible enzyme associated with inflammation (“prostaglandin G/H synthase II” or “cyclooxygenase-2 (COX-2)”) provides a viable target of inhibition which more effectively reduces inflammation and produces fewer and less drastic side effects.

Abstract: Processes for the preparation of pyrrolidones (7 and 8) and pyrrolidines (9 and 10) from tri-O-acetyl-D-erythro-4-pentulosonic acid esters are described. The compounds are aza sugar analogs of D-ribofuranoside and are intermediates to drugs which regulate nucleoside and nucleic acid synthesis.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: The invention relates to a novel process for the alternative preparation of N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide or N-methyl-N-[(1R)-1-phenyl-2-((3R)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide, and the novel compounds N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethane] and N-methyl-N[(1R)-1-phenyl-2-((3R)-3-hydroxypyrrolidin-1-yl) ethane], which are prepared as intermediates.

Abstract: A process for industrially preparing intermediates of aromatic amidine derivatives having anticoagulant activity, i.e.

Abstract: Disclosed are novel compounds represented by Structural Formula II, IX or XXVIII: 1

Abstract: A process for preparing a compound represented by general formulae (5) and (6) in the following reaction scheme or salts thereof, wherein R1 represents a protective group for a nitrogen atom; R2 represents a methanesulfonyl group or p-toluenesulfonyl group; R3 represents a hydrogen atom, an aralkyl group, or an alkyl group having 1 to 6 carbon atoms; and X represents a halogen atom. Reaction Scheme: The above process is useful as an industrial process for preparing intermediates of anticoagulant aromatic amidine derivatives described in Japanese Patent Application Laid-Open (kokai) No. 208946/1993.

Abstract: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.

Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms.

Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-linked sulfonamides of heterocyclic thioesters having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.

Abstract: The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N, O and S and which may be substituted with oxo or (1-6C)alkyl; R1, R2 and R3 are independently H, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxy(1-6C)-alkyl, carbo(1-6C)alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrolidin and 3-(5,6,7,8-tetmhydro-naphth-1-yl-oxy)-pyrolidin. The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.

Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovis replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.

Abstract: Selective inhibitors of the cPLA2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.

Abstract: A process for industrially preparing intermediates of aromatic amidine derivatives having anticoagulant activity (Japanese Patent Application Laid-Open No. 5-208946); i.e., compounds represented by formula (3) or salts thereof by the following reaction scheme including (1), (2), and (3), wherein R1 represents H, an alkanoyl group, an alkoxycarbonyl group, an aralkyl group, an aralkyloxycarbonyl group, or the like; and R3 represents H, an alkyl group, or an alkanoyl group.

Abstract: Pharmaceutical compositions comprising an inhibitor of ras farnesylation of formula (I) wherein, R1 is for example H and further values as defined in the specification; R2 is for example H and further values as defined in the specification; R3 is for example H or a substituent having values as defined in the specification; p is 0-3 in which R3 values can be the same or different; L is a linking moiety for example —CO—NH2— and further values as defined in the specification; A is selected from phenyl; naphthyl; a 5-10 membered monocyclic or bicyclic heteroaryl ring containing up to 5 heteroatoms where the heteroatoms are independently selected from O, N and S; or a —S—S— dimer thereof when R2=H; or an enantiomer, diastereoisomer, pharmaceutically acceptable salt, prodrug or solvate thereof together with a pharmaceutically acceptable diluent or carrier. A particular use is cancer therapy.

Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: 11-aza analogs of PGF2&agr; and methods of their use in treating glaucoma and ocular hypertension are disclosed.

Abstract: A method for treating urinary incontinence, such as incontinence resulting from bladder detrusor muscle instability, using enantiomerically enriched (R, R)-glycopyrrolate. The method comprises administering a therapeutically effective amount of enantiomerically enriched (R, R)-glycopyrrolate, or a pharmaceutically acceptable salt thereof, substantially free of the (S, S)-glycopyrrolate enantiomer. Pharmaceutical compositions for the treament of urinary incontinence comprising enantiomerically enriched (R, R)-glycopyrrolate, or a pharmaceutically acceptable salt thereof, and an acceptable carrier are also disclosed.

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.

Abstract: Pharmaceutical compositions which are useful for the treatment of cancer or illnesses which arise due to an abnormally elevated cell proliferation comprise acyl derivatives of aromatic aldehydes, especially arylidene diesters and .alpha.-alkoxyarylidene esters of general formula (I).

Abstract: A cyclic amine derivative represented by the following formula: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted phenyl group, R.sup.2 represents a substituted of unsubstituted C.sub.1 -C.sub.8 aliphatic acyl group, a substituted or unsubstituted benzoyl group or a C.sub.1 -C.sub.4 alkoxycarbonyl group, and R.sup.3 represents a substituted 3 to 7 membered saturated cyclic amino group which may form a fused ring; or pharmaceutically acceptable salts thereof. The compounds and salts have excellent platelet aggregation inhibitory action. They are useful for the treatment and prevention of such diseases as embolism, thrombosis or arteriosclerosis and for the preparation of pharmaceutical compositions for such uses.

Abstract: Pyrazole, pyrrole and imidazole derivatives having formula (I) or (II): ##STR1## wherein .dbd.X is .dbd.NR.sup.3, .dbd.O or an electron pair and Q comprises certain pyrazole, pyrrole and imidazole structures which, together with the remaining substituents, are defined in the description, are useful for controlling arthropod, nematodes, helminth or protozoan pests.

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: A method for preparing hydroxamic acid derivatives which are useful as analgesic, antiinflammatory, or neuroprotective agents.

Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(perfluoroalkylmethyl)arylimidoyl chloride compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds. In addition, the present invention provides N-(perfluoroalkylmethyl)arylimidoyl chloride compounds which are useful as intermediates in the preparation of arylpyrrole compounds.

Abstract: New oximsulfonate compounds of the formulae I or II, ##STR1## wherein m is 0 or 1; x is 1 or 2; R.sub.1 is, for example phenyl, which is unsubstituted or substituted or R.sub.1 is a heteroaryl radical that is unsubstituted or substituted, or, if m is 0, R.sub.1 additionally is C.sub.2 -C.sub.6 alkoxycarbonyl, phenoxycarbonyl or CN; R'.sub.1 is for example C.sub.2 -C.sub.12 alkylene, phenylene; R.sub.2 has for example one of the meanings of R.sub.1 ; n is 1 or 2; R.sub.3 is for example C.sub.1 -C.sub.18 alkyl, R'.sub.3 when x is 1, has one of the meanings given for R.sub.3, or R'.sub.3 in the formula IV and when x is 2 in the formula 1, is for example C.sub.2 -C.sub.12 alkylene, phenylene; R.sub.4 and R.sub.5 are independently of each other for example hydrogen, halogen, C.sub.1 -C.sub.6 alkyl; R.sub.6 is for example hydrogen, phenyl; R.sub.7 and R.sub.8 are independently of each other for example hydrogen or C.sub.1 -C.sub.12 -alkyl; R.sub.9 is for example C.sub.1 -C.sub.12 alkyl; A is S, O, NR.sub.

Abstract: Anti-pruritic pharmaceutical formulations containing kappa agonist compounds and methods of prevention or treatment of pruritus in a mammal with the anti-pruritic formulations.

Abstract: It is an object of the present invention to provide a process for producing an pyrrolidine derivative of general formula (2) or a salt thereof in a simple and economical manner and with good productivity and high yields.The present invention consists in a process for producing a pyrrolidine derivative of the general formula (2) or a salt thereof which comprises subjecting a compound of the general formula (1) to hydrogenolysis using a metal catalyst in the presence of at least one protic acid selected from the group consisting of hydrochloric acid, sulfuric acid, phosphoric acid, p-toluenesulfonic acid, methanesulfonic acid, acetic acid, n-butyric acid, trifluoroacetic acid and oxalic acid. ##STR1## R represents a 1-cyano-1,1-diphenylmethyl, 1-carbamoyl-1,1-diphenylmethyl, n-butyryloxy, methanesulfonyloxy or p-toluenesulfonyloxy group.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: Crystalline 2S-cis-3-[[(4-mercapto-2-pyrrolidinyl) carbonyl]-amino]benzoic acid and salts and solvates thereof are disclosed. Three different crystalline types are described.

Abstract: A compound of formula (I) ##STR1## and its pharmaceutically acceptable salt, wherein A is hydrogen or OY, wherein Y is a hydroxy protecting group; Ar is phenyl optionally substituted with one or more substituents selected from halo, hydroxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyloxy and carboxy-C.sub.1 -C.sub.4 alkyloxy;X is phenyl, naphthyl, biphenyl, indanyl, benzofuranyl, benzothiophenyl, 1-tetralone-6-yl,C.sub.1 -C.sub.4 alkylenedioxy, pyridyl, furyl and thienyl these groups optionally being substituted with up to three substituents selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, NO.sub.2, CF.sub.3 and SO.sub.2 CH.sub.3 ; andR is hydrogen, C.sub.1 -C.sub.4 alkyl or a hydroxy protecting group.

Abstract: The present invention relates to novel pyrrolidine compounds having the general formula I ##STR1## and pharmaceutically acceptable acid addition salts or hydrates or prodrugs thereof, wherein R.sup.1 is straight or branched C.sub.1-14 -alkyl optionally substituted with C.sub.3-7 -cycloalkyl, C.sub.1-6 -alkoxy, phenoxy, perhalomethyl, halogen, optionally substituted phenyl;CR.sup.2 is optionally C.dbd.R.sup.2 or C--R.sup.2R.sup.2 is oxygen, hydroxy, halogen, amino or mercapto,R.sup.3 and R.sup.4 independently are hydroxy, halogen, amino or mercapto, the use of these compounds as medicament, the use of these medicaments in the treatment of diabetes, pharmaceutical compositions containing these compounds and methods of preparing the compounds.

Abstract: Therapeutically effective amounts of a 3,4-diarylchroman can be administered transdermally by incorporation of the 3,4-diarylchroman in a matrix or liquid reservoir patch suitable for transdermal delivery, which matrix or liquid reservoir patch optionally contains hydrophobic and/or hydrophilic vehicle(s).

Abstract: Prodrugs of COX-2 inhibitors are described as being useful in treating inflammation and inflammation-related disorders.

Abstract: Predetermined combinatorial libraries of non-peptide compounds are disclosed. Compounds useful for generating such libraries are also disclosed.

Abstract: A process for synthesizing a compound of the formula I: ##STR1## or a pharmaceutically acceptable salt or ester thereof, wherein each P independently represents H or a protecting group, and R.sup.1 and R.sup.2 independently represent H, C.sub.1-10 alkyl, aryl or heteroaryl, or substituted C.sub.1-10 alkyl, aryl or heteroaryl, comprising:reacting the compounds: ##STR2## or a pharmaceutically acceptable salt or ester thereof, and ##STR3## or a pharmaceutically acceptable salt or ester thereof, wherein X represents OP(O)(OR).sub.2, or OSO.sub.2 R, wherein R represents C.sub.1-6 alkyl, aryl or perfluoro C.sub.1-6 alkyl, in the presence of an amine selected from the group consisting of: diisopropylamine (DIPA), dicyclohexylamine (DCHA), 2,2,6,6-tetramethylpiperidine (TMP), 1,1,3,3-tetramethylguanidine (TMG), 1,8-diazabicyclo?4.3.0!undec-7-ene (DBU) and 1,5-diazabicyclo?4.3.0!non-5-ene to produce a compound of formula I.

Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 represents a saturated heterocyclic group attached to the bond or group represented by A through a ring carbon atom; R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3a, R.sup.3b, R.sup.3c and R.sup.3d are hydrogen or various other groups or atoms; and A represents a single bond or an alkylene group having from 1 to 6 carbon atoms are serotonin 2 receptor antagonists and have the ability to inhibit the activity of squalene synthase. They can not only prevent and inhibit the development and progression of arteriosclerosis but can also inhibit thrombosis in arteriosclerotic lesions and can improve hemodynamics.

Abstract: The present invention is directed to the use of cyclic amide alkoxylate compounds as additives in fuel compositions having a major amount of a mixture of hydrocarbons in the gasoline boiling range and a minor amount of one or more cyclic amide alkoxylate compounds of the formula: ##STR1## wherein x is from 2 to 20 and y is from 1 to 50. R.sub.1 and R.sub.2 are independently hydrogen or hydrocarbyl of 1 to 100 carbon atoms. R.sub.3 is hydrocarbyl of 1 to 100 carbon atoms and R.sub.4 is independently hydrocarbyl of 2 to 100 carbon atoms. R.sub.5 is hydrogen, hydrocarbyl of 1 to 100 carbon atoms or acyl of 1 to 20 carbon atoms.The invention is also directed to the use of these cyclic amide alkoxylate compounds for decreasing intake valve deposits, controlling octane requirement increases and reducing octane requirement. The invention is further directed to novel cyclic amide alkoxylate compounds.

Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.

Abstract: Pharmaceutical preparations which are suitable for the treatment of inflammatory bowel disorders and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms,R.sup.2 is Ar, orR.sup.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2,R.sup.5 is OH, CH.sub.2 OH,R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring,A is alkyl having 1-7 C atoms,Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.

Abstract: The present invention relates to a mercaptopyrrolidinyl derivative of the following formula ##STR1## suitable for the preparation of carbapenem compounds.