Abstract: A conductive coating comprising polymers of meso-meso, ?-? doubly linked fused and/or meso-?, ?-meso doubly linked fused and/or meso-meso, ?-?, ?-?triply linked fused (poly)porphyrins. A method for forming on a substrate a thin conductive coating of polymers of meso-meso, ?-? doubly and/or meso-?, ?-meso doubly and/or meso- meso, ?-?, ?-? triply linked fused (poly)porphyrins, the method comprising the steps of providing a substrate in a vacuum chamber, performing on the substrate an oxidative chemical vapour deposition reaction with an oxidant and at least one porphyrin monomer.

Abstract: A pharmaceutical composition, comprising a combination of an antibiotically active compound of the formula (I): with a ?-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another ?-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).

Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.

Abstract: Disclosed are an N-acyl-?-lactam derivative represented by the following general formula, from which a photoresist composition capable of controlling an acid diffusion length to be short is obtained; a polymer obtained by polymerizing the N-acyl-?-lactam derivative represented by the following general formula as one of starting materials; and a photoresist composition containing the polymer.

Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.

Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.

Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

Abstract: A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0° C.

Abstract: Disclosed are an N-acyl-?-lactam derivative represented by the following general formula, from which a photoresist composition capable of controlling an acid diffusion length to be short is obtained; a polymer obtained by polymerizing the N-acyl-?-lactam derivative represented by the following general formula as one of starting materials; and a photoresist composition containing the polymer.

Abstract: Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.

Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.

Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

Abstract: The present invention relates to novel Pyrrolidine, Piperidine and Piperazine Derivatives, pharmaceutical compositions comprising the Pyrrolidine, Piperidine and Piperazine Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity, an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.

Abstract: A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0° C.

Abstract: The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.

Abstract: Disclosed are compounds of the formula wherein Z1 is —CH2—or —C(O)—, R4 and R5 are carbon chains (and optionally, together can form a C2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R2 is heteroaryl, and R1 and R3 are as defined herein. Also disclosed are methods of treating pain, and methods of inhibiting the absorption of cholesterol using a compound of formula I.

Abstract: The present invention relates to Azetidinone Derivatives of structural formula 1: and compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.

Abstract: A process for the production of a compound of formula (I) wherein ALINKERB represents a linker moiety of formula (V): A[G1-G2*-G3]B; wherein A and B indicate the orientation of the group of formula (V) in formula (I); G1, G2 and G3 have specific meanings described herein and may be present or absent, with the proviso that at least one of G1 or G3 is present; which linker group may furthermore optionally contain one or more groups of formula (VI); and/or other substituents; and R1 represents hydrogen or a C1-C4-alkyl group; R2 represents hydrogen or a C1-C4-alkyl group; R3 independently at each occurrence, represents hydrogen or a C1-C4-alkyl group; x is 0 or 1; y is 0 or 1; z independently at each occurrence, is 0 or 1; and (—) represents a single bond between a primary, secondary or tertiary carbon atom of the moiety ALINKERB and the adjacent nitrogen atom; in which process (A) a compound of formula (II) is reacted with a compound of formula (III) wherein Pr represents an amino protecting group selected from

Abstract: A class of 7-oxo-2,6-diazabicyclo-[3.2.0]-heptane-6-sulfonic acid compounds substituted at the two position of the bicyclic ring with a heterocyclylaminocarbonyl group or a carbocyclylaminocarbonyl group are ?-lactamase inhibitors. The compounds and their prodrugs and pharmaceutically acceptable salts are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds are suitable for use with ?-lactam antibiotics (e.g., imipenem and ceftazidime) against micro-organisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.

Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.

Abstract: Disclosed is a total synthesis of a biologically active ?-Lactam—Compound 3, which is related to Salinosporamide A and Omuralide, both structurally and by its activity as a proteasome inhibitor. Also disclosed are proteasome inhibiting compounds having the formula: wherein: R1 is a cyclolower alkyl group; or R1 is a lower alkyl group; and R2 is either hydrogen or a lower alkyl group; R3 is either hydrogen or a lower alkyl group; R4 a halo-lower alkyl group; and R5 is either hydrogen or a lower alkyl group.

Abstract: The present invention relates to Spirocyclic Azetidinone Compounds, compositions comprising a Spirocyclic Azetidinone Compound and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of a Spirocyclic Azetidinone Compound.

Abstract: The present invention refers to highly functionalised spiro-fused azetidinones of formula I: having a cyclohexane moiety with the desired number of protected or unprotected hydroxyl groups which are introduced with high stereo and regioselectivity, as well as processes for their synthesis.

Abstract: The present invention is directed to a compound of formula I: wherein R1 and R2 are independently selected from H, halogen, protected or unprotected hydroxy, alkylsilyloxy, substituted or unsubstituted alkyl or cycloalkyl, substituted or unsubstituted alkoxy or aryloxy, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, nitro, amino, mercapto or alkylthio; R3 and R4 are independently selected from H, substituted alkyl, substituted or unsubstituted alkoxy or aryloxy, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl; Z is —(CRaRb)n— wherein n is a number selected from 1, 2, 3 and Ra and Rb are each independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy, substituted or unsubstituted amino or halogen; Y is

Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.

Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Abstract: There are described compounds of the formula in which R signifies lower alkoxycarbonyl, lower alkoxy-carbonylamino, the acyl residue of an &agr;- or &bgr;-amino acid or a residue of the general formula Q—X—Y—  (a) wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulfur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear “spacer” with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulfur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulfur, and Y represents one of the groups —CO—, —CS—, —CONH— and (where X contains neither sulfur nor carbonyl as a terminal component) —SO2—; and in which R1 and R2 together signify a group of the formula wherein A represents hydrogen or a residue which is usable in the 3-position of cephalosporin antibiotics, and in which R3 represents

Abstract: The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor.

Abstract: The present invention provides a method of limiting the presence of a microorganism by contacting the microorganism with polymer-bound metal-containing compositions. The compositions include metal-containing compounds that may be prepared by reacting or polymerizing metal-containing monomers. The microorganism may be present in a liquid that is contacted with the polymer-bound metal-containing composition. Alternatively, the microorganism may be present in a solid that is contacted with the polymer-bound metal-containing composition.

Abstract: The invention is directed to aza-bridged-bicyclic compounds having Formula (I): 1

Abstract: The invention relates to a process for the preparation of N,N′-carbonylbislactams by reaction of phosgene with at least one lactam which is characterized in that the tertiary amine is chosen from the group consisting of non-nucleophilic aliphatic tertiary amines.

Abstract: A method for separation of enantiomers of a lactam represented by formula (I): 1

Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1C receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotence, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1C receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: This invention relates to the use of compounds having the general structure: wherein: Z1 and Z2 each independently represent an arene nucleus, which has from 5 to 14 ring atoms; G1 and G2 each independently represent a metal ligating group; R represents a hydrogen atom, a halogen atom, an alkyl group, an acylamino group, an alkoxy group, a sulfonamido group, an aryl group, a thiol group, an alkylthio group, an arylthio group, an alkylamino group, an arylamino group, an amino group, an alkoxycarbonyl group, an acyloxy group, a nitro group, a cyano group, an alkylsulfonyl group, an arylsulfonyl group, an alkylsulfoxyl group, an arylsulfoxyl group, an aryloxyl group, a hydroxyl group, a thioamido group, a carbamoyl group, a suffamoyl group, a formyl group, an acyl group, a ureido group, an aryloxycarbonyl group, a silyl group, or a sulfoalkoxy group; L1 represents a nitrogen heterocycle; L2 represents a monodentate or polydentate (e.g.

Abstract: Bicyclic .beta.-lactams comprising a 5- or 6-membered lactone or lactam ring are obtained in a process comprising a base induced intramolecular cyclization of a 4-substututed .beta.-lactam having a leaving group in the 1-position. An intramolecular nucleophile transfer reaction is proposed as the operative mechanism and the bicyclic .beta.-lactams are obtained in the required stereochemical form for biological activity. The compounds provided are useful intermediates for the preparation of antibiotics and .beta.-lactamase inhibitors.

Abstract: This invention provides a process for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, particularly for azetidinones substituted in the C-3 and C-4 positions and optionally substituted at the ring nitrogen, comprising reacting a .beta.-(substituted-amino)amide, a .beta.-(substituted-amino)acid ester, or a .beta.-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent.

Abstract: Disclosed is a novel .beta.-lactam compound, a 7-substituted-2-oxa-7-azabicyclo?3.2.0!heptan-6-one represented by the general formula ##STR1## in which R is an alkyl, cycloalkyl, aryl, halogen-substituted aryl or alkaryl group, having usefulness as an intermediate for the synthesis of various biologically active compounds. The compound can be prepared by the reaction of an isocyanate compound RNCO, R being the same as above, and 2,3-dihydrofuran, preferably, under pressurization up to 2000 atmospheres or higher.

Abstract: Novel compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sub.1 is ##STR2## R.sub.2 and R.sub.3 are independently selected from --CH.sub.2 --, --CH(lower alkyl)--, --C(di-lower alkyl)--, --CH.dbd.CH-- and --C(lower alkyl).dbd.CH--; or R.sub.1 with R.sub.2, or R.sub.1 with R.sub.3, form --CH.dbd.CH-- or --CH.dbd.C(lower alkyl)--;u and v are independently 0-3, provided both are not zero;R.sub.4 is B--(CH.sub.2).sub.m C(O)--; m is 0-5;B--(CH.sub.2).sub.q --; q is 0-6;B--(CH.sub.2).sub.e --Z--(CH.sub.2).sub.r ; Z is --O--, --C(O)--, phenylene, --N(R.sub.8)-- or --S(O).sub.0-2 --, e and r is 0-5; the sum of e and r is 0-6;B--(C.sub.2 -C.sub.6 alkenylene)--; B'--(C.sub.4 -C.sub.6 alkadienylene)--;B--(CH.sub.2).sub.t --Z--(C.sub.2 -C.sub.6 alkenylene)--; t is 0-3; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6;B--(CH.sub.2).sub.f --V--(CH.sub.2).sub.g --; V is cycloalkylene, f is 1-5, g is 0-5; the sum of f and g is 1-6;B--(CH.sub.2).sub.t --V--(C.

Abstract: 4-[(Heterocycloalkyl or heteroaromatic)-substituted phenyl]-2-azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: A is optionally substituted heterocycloalkyl, heteroaryl, benzofused heterocycloalkyl, or benzofused heteroaryl;Ar.sup.1 and Ar.sup.2 are optionally substituted aryl;Q is a bond or, with the 3-position ring carbon of the azetidinone, forms a spiro group; andR.sup.1 is alkylene; alkylene wherein a carbon in the chain is replaced by --O--, --C(O)--, phenylene, --NR.sup.8 --, --S(O).sub.0-2 -- or cycloalkylene; or alkenylene; or, when Q is a bond, R.sup.1 can be alkylene substituted by one or two hydroxy groups or hydroxy derivatives, wherein the alkylene chain can optionally be joined to Ar.sup.1 through --O-- or --S(O).sub.0-2 -- or joined to the azetidinone ring through a --S(O).sub.

Abstract: A process for producing a compound of the formula ##STR1## comprises the following sequence of steps: ##STR2## wherein the various radicals are as defined in the specification.

Abstract: Disclosed is a method for the preparation of a .beta.-thiolactam compound, i.e. a 7-substituted-2-oxa-7-azabicyclo [3.2.0]-heptan-6-thione, represented by the general formula ##STR1## in which R is an alkyl or aryl group, having usefulness as an intermediate for the synthesis of various biologically active compounds. The compound can be prepared by the reaction of an isothiocyanate compound R--NCS, R being the same as above, and 2,3-dihydrofuran, preferably, under pressurization up to 2000 atmospheres or higher at an elevated temperature.

Abstract: Disclosed is a novel .beta.-lactam compound, a 7-substituted-2-oxa-7-azabicyclo[3.2.0]heptan-6-one represented by the general formula ##STR1## in which R is an alkyl, cycloalkyl, aryl, halogen-substituted aryl or alkaryl group, having usefulness as an intermediate for the synthesis of various biologically active compounds. The compound can be prepared by the reaction of an isocyanate compound RNCO, R being the same as above, and 2,3-dihydrofuran, preferably, under pressurization up to 2000 atmospheres or higher.

Abstract: There are described compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxycarbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formulaQ--X--Y-- (a)wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulphur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear "spacer" with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulphur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups --CO--, --CS--, --CONH-- and (where X contains neither sulphur nor carbonyl as a terminal component) --SO.sub.2 --;and in which R.sup.1 signifies hydrogen, halogen, carbamoyloxy, lower alkanoyloxy or a group of the formula --S--Het, wherein Het represents a 5- or 6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen, and R.sup.2 represents the sulpho group --SO.sub.3 H or R.sup.

Abstract: The invention provides 1,3,4 substituted and bicyclic derivatives of 2-azetidinones and processes therefor. These compounds are valuable intermediates useful in the preparation of 1-carba(dethia)cephalosporin antibiotics.

Abstract: The present invention relates to porphyrin and metal ion-containing monomers and polymers. The monomers ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from H, alkyl having 1 to 6 carbon atoms, phenyl or phenyl substituted with 1 to 3 alkyl groups each having 1 to 6 carbons or with 1 to 3 halogen atoms and A is a metal atom, are used with a diamine or a dialdehyde respectively to produce a porphyrin polymer or a metal ion containing porphyrin polymer. These polymers are useful as electrical conductors and as liquid crystal polymers.

Abstract: This invention relates to spiro-lactams and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.

Abstract: The invention concerns pharmaceutially useful heterocyclic nitromethane compounds of the formula I: ##STR1## in which ring Q is a heterocycle of 4 to 7 ring atoms, the fragment completing the ring Q having 2 to 5 atoms, one of which is carbon, oxygen, sulphur or a group of the formula --NRa--, and the remainder are carbon; Ra is hydrogen, (1-6C)alkyl, (2-6C)alkanoyl, trifluoroacetyl, phenyl, benzoyl, or phenyl(1-4C)alkyl, the latter three optionally substituted; and R.sup.1 R.sup.2 and R.sup.3 are independently hydrogen, hydroxy, (1-6C)alkyl, (1-6C)alkoxy, phenyl, phenoxy or phenyl(1-4C)alkyl, the last three optionally substituted, or two of R.sup.1, R.sup.2 and R.sup.3 situated on adjacent ring carbon atoms and together with said carbon atoms form a benzene ring fused to ring Q, the benzene ring itself optionally substituted, provided that when the fragment completion ring Q is of 3 atoms then at least one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen; and salts thereof.

Abstract: Provided are new antibacterial spirocyclic 6-amido carbapenems of the formula: ##STR1## wherein: R.sup.1 is hydrogen, C.sub.1-8 substituted or unsubstituted alkyl or C.sub.6-10 substituted or unsubstituted aryl;R.sup.2 is hydrogen, C.sub.1-8 substituted or unsubstituted alkyl or C.sub.2-8 substituted or unsubstituted acyl;R.sup.3 is hydrogen, C.sub.1-8 substituted or unsubstituted thioalkyl or C.sub.6-10 substituted or unsubstituted thioaryl, or 5 or 6 membered substituted or unsubstituted thioheteroaryl; andR.sup.4 is hydrogen, pharmaceutically acceptable alkali metal salt or biolabile ester,and a process for their synthesis through novel intermediates.

Abstract: Certain spirocyclic heterocyclic compounds, and their pharmaceutically-acceptable salts, are inhibitors of the aldose reductase enzyme, and so are useful for the control of diabetic complications. Exemplary compounds include compounds of the formula ##STR1## wherein Y is ##STR2## X is --O-- or ##STR3## R.sub.1 and R.sub.2 are each independently H, alkyl C.sub.1 -C.sub.6,aryl or arylalkyl (C.sub.1 -C.sub.6);W.sub.1 and W.sub.2 are each independently hydrogen, halogen or nitro; andthe pharmaceutically acceptable base addition salts thereof.