Abstract: The invention relates to antimicrobial compounds which interact with zinc in a zinc finger of a bacterial DNA polymerase, methods of screening for such compounds, and methods of using such compounds to inhibit polymerase activity or bacterial growth.

Abstract: Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.

Abstract: Nitramine oxidizers are recovered from propellant, explosive, and pyrotechnic materials with a concentrated mineral acid bath, preferably comprising 70 to 90 wt. % nitric acid, that serves to dissolve the nitramine oxidizers into solution and permit filtration of the binder therefrom. The recovery process is conducted in the absence of organic solvents.

Abstract: Disclosed are thiazolobenzoheterocycles of the general formula Including their isomers, racemates, enantioners and salts thereof, as well as processes for preparing these compounds and medicaments containing them.

Abstract: A pyrrolesulfonamide derivative having the following formula (I): 1

Abstract: The present invention is directed to substituted 1,4-thiazepine and analogs thereof, represented by the general Formula I: 1

Abstract: Hydroxamic acids having the formula 1

Abstract: A pyrrolesulfonamide compound having formula (I) wherein the ring P represented by &agr; is a pyrrole ring having structure &bgr; or &psgr; wherein A represents alkylene, alkenylene or alkynylene; and Y represents a group &dgr; in which W represents CH, C═ or N; m stands for 0 or 1 when W is CH or N, or m stands for 1 when W is C═; B represents a specific divalent group; E1 and E2 each independently represents H or lower alkyl; and D represents an aromatic hydrocarbon group or heterocyclic group; l stands for 0 or 1; the dashed line indicates the presence or absence of a bond; and, when the bond is present, Z2 is not present and Z1 represents H but, when the bond is absent, Z1 represents H and Z2 represents OH or Z1 and Z2 are combined together to represent O or a group NOR5, in which R5 represents H, or alkyl, aralkyl or aryl; and R represents H, alkyl, cycloalkyl, cycloalkyl-alkyl or aralkyl.

Abstract: A compound of the formula: wherein ring A is an optionally substituted benzene ring; ring B′ is an optionally substituted non-aromatic heterocyclic ring having, the same or different, two or more hetero atoms; R1 is a hydrogen atom or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; Y is an optionally substituted amino group or an optionally substituted N-containing saturated heterocyclic group; n denotes an integer of 1 to 10, provided that when the ring B′ is a 5- to 7-membered ring, the ring B′ contains at least one nitrogen atom as hetero atom and n denotes an integer of 2 to 10, or a salt thereof. The compounds and salts thereof have an excellent cholinesterase inhibitory activity and antidepressant activity, and are useful as therapeutic and/or prophylactic medicaments of senile dementia.

Abstract: A pyridine alcohol derivative represented by General Formula III 1

Abstract: The invention relates to substituted 1,4-benzothiazepine-1,1-dioxide derivatives and their acid addition salts. 1,4-Benzothiazepine-1,1-dioxide derivatives of formula 1, wherein R1, R2, R3, and Z have the meanings indicated in the specification, physiologically tolerable salts, and physiologically functional derivatives thereof, and also processes for their preparation, are described. The compounds are suitable, for example, as hypolipidemics.

Abstract: A compound of the formula: in which R1 is hydrogen, optionally substituted lower alkylcarbamoyl(lower)alkylidene, lower alkylidene, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy(lower)alkyl, carboxy(lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbamoyl(lower)alkyl, R2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl, R3 is hydrogen or amidino-protective group, A is lower alkylene or carbonyl, X is Y is lower alkylene, —S— or —SO2—, Z is —S— or —O—, and the line: is a single bond or a double bond, or pharmaceutically acceptable salts thereof, which is useful as a medicament.

Abstract: A pyrrolesulfonamide derivative having the following formula (I): is provided wherein P, A, Y, l, Z1 and Z2 are as described herein, wherein the derivative has strong serotonin-2 receptor antagonistic action, low toxicity and fewer side effects, and its use as a therapeutic for circulatory diseases such as ischemic heart diseases, cerebrovascular disturbances and peripheral circulatory disturbances.

Abstract: Compounds of the formula: ##STR1## wherein A.sup.1 to A.sup.5 form a seven-membered ring containing one optionally substituted nitrogen atom and one heteroatom selected from oxygen and nitrogen;D.sup.1 to D.sup.4 form a substituted six membered ring, optionally containing up to two nitrogen atoms;R is preferably at least one acid containing substituent;R* is is one or more groups chosen from H, Q-C.sub.1-6 alkyl, Q-C.sub.1-6 oxoalkyl, Q-C.sub.2-6 alkenyl, Q-C.sub.3-4 oxoalkenyl, Q-C.sub.3-4 oxoalkynyl, Q-C.sub.2-4 alkynyl, C.sub.3-6 cycloalkyl, Ar or Het;Q is H, C.sub.3-6 cycloalkyl, Het or Ar;R.sup.6 is preferably a basic nitrogen containing substituent;are inhibitors of platelet aggregation.

Abstract: The present invention is concerned with new hypolipidemic compounds, with processes and novel intermediates for their preparation, with pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis.Compounds of the formula (I): ##STR1## wherein R.sup.1 to R.sup.10 and X are as defined in the Specification and useful as hypolipidemic compounds.

Abstract: A compound of the formula ##STR1## in which R.sup.1 is hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy)lower)alkyl, carboxy)lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbamoyl(lower)alkyl,R.sup.2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl,R.sup.3 is hydrogen or amidino-protective group,A is lower alkylene or carbonyl,X is ##STR2## Y is --S-- or --SO.sub.2 --, Z is --S-- or --O--,or pharmaceutically acceptable salts thereofwhich is useful as a medicament.

Abstract: Polycyclic alkaloids of formula (I), ##STR1## wherein R.sub.1 is H, C.sub.1-6 alkyl, or C.sub.6-12 aryl optionally substituted with polar groups; R.sub.2 and R.sub.3 are independently H, OH, C.sub.1-6 alkyl, --C(NH)--NH.sub.2, a positively charged group, or C.sub.7-13 aralkyl optionally substituted with NH.sub.2, OH, C.sub.1-6 alkyl, or halogen; or R.sub.2 and R.sub.3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R.sub.4 is H, C.sub.1-6 alkyl, OR.sub.6, SR.sub.6 or N(R.sub.6).sub.2, wherein each R.sub.6 is independently H, C.sub.1-3 alkyl; X is O, S, SO, SO.sub.2, N--R.sub.5, or C--(R.sub.5).sub.2, wherein each R.sub.5 is independently H, C.sub.1-6 alkyl, or C.sub.7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH.sub.2 then R1 is not CH.sub.3, R.sub.2 and R.sub.3 are not both H, R.sub.4 is not OH, m is not 3 and n is not 0.

Abstract: Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation.

Abstract: The present invention is concerned with new hypolipidemic compounds, with processes and novel intermediates for their preparation, with pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis.Compounds of the formula (I): ##STR1## wherein R.sup.1 to R.sup.10 and X are a defined in the specification and are useful as hypolipidemic compounds.

Abstract: Substituted N-heterocyclyl-1-aryloxyalkyl-4-piperldineamines of formula (I) ##STR1## wherein each of R.sub.1 to R.sub.4, which are the same or different, is hydrogen, optionally branched C.sub.1-4 alkyl, optionally branched C.sub.1-4 alkyloxy, halo, nitro, hydroxy, or trifluoromethyl or trifluoromethoxyl; R.sub.5 is hydrogen, optionally branched C.sub.1-6 alkyl, optionally branched C.sub.7-12 phenylalkyl optionally substituted on the phenyl by one or more radicals having the same definition as R.sub.1 ; W and X are oxygen or sulphur; Y is C.sub.2-6 polymethylene or --CH.sub.2 --CH(OH)--CH.sub.2 --; and n is 0 or 1; and pure R or S isomers of said compounds, where applicable, as well as mixtures thereof, as well as therapeutically-acceptable organic or inorganic salts and hydrates of the compounds and a method for preparing the compounds and their use as drugs are all disclosed.

Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, which are effective for inhibiting platelet aggregation and bone resorption, pharmaceutical compositions for effecting such activity, and a method for using these compounds.

Abstract: The invention is concerned with novel hypolipidemic compounds of formula (I), with processes and novel intermediates for their preparation, pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, and associated diseases such as atherosclerosis.

Abstract: This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents, hypotriglyceridemic agents, antiatherosclerosis agents, antifungal agents, Alzheimer's agents or anti-acne agents.

Abstract: The present invention relates to heterocyclic compounds with the formula ##STR1## in which R.sup.1 to R.sup.7, B, a, and X have the meanings indicated in the specification. These compounds can be used for the treatment of diseases of the rheumatic variety and for the prevention of allergically-induced diseases.

Abstract: An optically active salt of 1,5-benzothiazepine compound of the formula (I) or (II): ##STR1## wherein each of Ring A and Ring B is a substituted or unsubstituted benzene ring, and R.sup.1 and R.sup.2 are the same or different and each is a lower alkyl group, can be prepared by resolving a racemic salt of 1,5-benzothiazepine compound of the formula (I) or (II) by means of preferential crystallization.

Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R.sup.1 represents hydrogen atom or a C.sub.1-6 alkyl group; R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-6 alkyl group, or R.sup.2 and R.sup.3 may combine together to represent a 5- or 6-membered cycloalkyl group; R.sup.4 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.5 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group; x represents --NR.sup.7 --, --O--, --CHR.sup.7 -- or --S-- in which R.sup.7 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.

Abstract: The invention is concerned with novel hypolipidemic compounds of formula (I), with processes and novel intermedites for their preparation, pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, such as atherosclerosis.

Abstract: Novel indole, indoline and quinoline derivatives of formula (I) processes for their preparation, pharmaceutical compositions containing them, and their use in medicine is disclosed. A structurally distinct class of compounds have now been discovered and have been found to exhibit 5HT.sub.1-D antagonist activity. In a first aspect, the present invention therefore provides a compound of formula (I) or a salt thereof, in which P is a 5-7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, A, B, m, R.sup.1 -R.sup.8 are defined in the application.

Abstract: The present invention relates to polycyclic iminooxadiazinediones A corresponding to formula I ##STR1## The present invention also relates to mixtures of these polycyclic iminooxadiazinediones with other isocyanate derivatives and to their use for the production of optionally foamed polyurethane plastics, for the production of paints and coatings and for the production or formulation of active ingredients, pharmaceutical products, etc.

Abstract: The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT.sub.2B -antagonists. The invention is also directed to formulations and methods for treatment.

Abstract: The present invention is concerned with processes for preparing hypolipidaemic benzothiazepine compounds of formula (I) ##STR1## wherein l is an integer of from 0 to 4; m is an integer of from 0 to 5; n is an integer of from 0 to 2; R and R' are atoms or groups independently selected from halogen, nitro, phenylalkoxy, C.sub.1-4 alkoxy, C.sub.1-6 alkyl and --O(CH.sub.2).sub.p SO.sub.3 R" wherein p is an integer of from 1 to 4 and R" is hydrogen or C.sub.1-6 alkyl, wherein said phenylalkoxy, alkoxy and alkyl groups are optionally substituted by one or more halogen atoms; R.sup.4 is C.sub.1-6 straight alkyl group; and R.sup.5 is a C.sub.2-6 straight alkyl group; and their salts, solvates and physiologically functional derivatives; and intermediates useful in said processes.

Abstract: Compounds, useful as plant fungicides, having the formula (I): ##STR1## or a stereoisomer thereof, wherein A is CH or N, B is OCH.sub.3 or NHCH.sub.3, X is CH.sub.2, CH.sub.2 O, O or S, Y is R.sup.1 --C.dbd.C--R.sup.2 or R.sup.1 --CH--CH--R.sup.2 wherein R.sup.1 and R.sup.2 are independently H, halo, hydroxy, alkyl, haloalkyl, alkoxy, haloalkoxy, cyano, nitro, amino, mono- or dialkylamino, alkanoylamino, carboxy, alkoxycarbonyl, aminocarbonyl, mono- or di-alkylaminocarbonyl, alkylcarbonyloxy, optionally substituted aryl, optionally substituted aralkyl or optionally substituted aryloxy or R.sup.1 and R.sup.2 join to form with the carbon atoms to which they are attached an optionally substituted benzene ring, and Z is CH.sub.2, CHCH.sub.3, C(CH.sub.3).sub.2 or C.dbd.O.

Abstract: The invention provides a compound of formula (I), wherein n is an integer of from 0 to 2; R is an optional substituent; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is an atom or group selected from hydrogen, C.sub.1-4 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-4 alkoxy, pyrryl, thienyl, pyridyl, 1,3-benzodioxolo, phenyl and naphthyl, which groups are optionally substituted; R.sup.3 is hydrogen, OH, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or --O C.sub.1-6 acyl; R.sup.4 is a group independently selected from C.sub.1-6 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.2-6 alkenyl, and C.sub.2-6 -alkynyl which groups are optionally substituted; R.sup.5 is a group independently selected from C.sub.2-6 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.2-6 alkenyl and C.sub.2-6 alkynyl, which groups are optionally substituted; or R.sup.4 and R.sup.5, together with the carbon atom to which they are attached, form a C.sub.3-7 spiro cycloalkyl group which is optionally substituted; R.sup.

Abstract: This invention relates to certain benzoxazepinones and benzothiazepinones useful as hypocholesterolemic agents and antiatheroscierosis agents.

Abstract: Compound of formula (1), processes for their preparation and their use as CNS agents are disclosed, in which A is CONR where R is hydrogen or C.sub.1-6 alkyl; Q is an optionally substituted 5 to 7-membered heterocyclic ring containing 1 to 3 heteroatoms selected from oxygen, nitrogen or sulphur, R.sup.1 is hydrogen, halogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, COC.sub.1-6 -alkyl, C.sub.1-6 alkoxy, hydroxy, hydroxyC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkoxy, C.sub.1-6 alkoxyC.sub.1-6 alkoxy, acyl, nitro, trifluoromethyl, cyano, SR.sup.9, SOR.sup.9, SO.sub.2 R.sup.9, SO.sub.2 NR.sup.10 R.sup.11, CO.sub.2 R.sup.10, CONR.sup.10 R.sup.11, CO.sub.2 NR.sup.10 R.sup.11, CONR.sup.10 (CH.sub.2).sub.a CO.sub.2 R.sup.11, (CH.sub.2).sub.a NR.sup.10 R.sup.11, (CH.sub.2).sub.a CONR.sup.10 R.sup.11, (CH.sub.2).sub.a NR.sup.10 COR.sup.11, (CH.sub.2).sub.a CO.sub.2 C.sub.1-6 alkyl, CO.sub.2 (CH.sub.2).sub.a OR.sup.10, NR.sup.10 R.sup.11, NR.sup.10 CO.sub.2l R.sup.11, NR.sup.10 CONR.sup.10 R.sup.11, CR.sup.10 =NOR.sup.11, CNR.

Abstract: The compound of the formula (I) or its salt or a medicament containing the same ##STR1## wherein, A and B represent a carbonyl group or sulfonyl group, m and p are different and represent 0 or 1,R.sup.1 and R.sup.2 may be the same or different from each other and represent a hydrogen atom, an unsubstituted or substituted alkyl group, an unsubstituted or substituted aryl group, an unsubstituted or substituted aralkyl group, an unsubstituted or substituted heterocyclic group containing nitrogen or an unsubstituted or substituted heterocyclic group containing oxygen, or R.sup.1 and R.sup.2, taken together with the nitrogen atom to which they are linked, may form an unsubstituted or substituted heterocyclic group, provided that when B is a sulfonyl group, R.sup.

Abstract: The invention provides novel 1,4-benzothiazepine compounds substituted with hydroxy or a group containing hydroxy, compositions comprising such compounds and their use in the treatment or prophylaxis of treating clinical conditions in which inhibition of bile acid uptake is indicated, for example, hyperlipidemia and atherosclerosis.

Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.

Abstract: There are disclosed novel substituted naphthyl-, quinolyl- and isoquinolyl- sulfonamide derivatives that are useful in a method of treating immuno-inflammatory diseases in a mammalian patient suffering therefrom. Pharmaceutical compositions containing the sulfonamide compounds are also provided.

Abstract: Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula ##STR1## wherein R.sub.1 is hydrogen or an optionally substituted hydrocarbon group; R.sub.2 is hydrogen, an optionally substituted alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic ring group; X' is a substituent comprising an optionally esterified carboxyl group, an optionally substituted carbamoyl group, an optionally substituted hydroxyl group, an optionally substituted amino group or an optionally substituted heterocyclic radical having a protonizable hydrogen; Ring A is an optionally substituted benzene ring or an optionally substituted aromatic heterocyclic ring; Ring J' is a 7- to 8-membered heterocyclic ring containing at most three ring constituting hetero atoms; D is C or N; the Ring J' optionally having, besides R.sub.1, R.sub.

Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.

Abstract: Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower-alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.

Abstract: A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.

Abstract: Methods, compounds and compositions are provided for inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic bacterial infections, such as mycobacterial and clostridium infections, in vivo using bicyclic nitroimidazole compounds of the formula (II): ##STR1## wherein R.sub.1 is hydrogen, halogen, loweralkyl, haloloweralkyl, cycloalkyl, heterocycle, substituted heterocycle and heterocyclicalkyl; X is oxygen, sulfur or NK.sub.2, where R.sub.2 is hydrogen, loweralkyl, aryl, cycloalkyl, heterocycle, substituted heterocycle, heterocyclicalkyl, COR.sub.3 or SO.sub.2 R.sub.4 CONR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are independently selected from hydrogen, loweralkyl, aryl, alkylaryl, alkoxyalkyl, alkoxyaryl, alkoxyalkoxyaryl, alkylheterocycle, and alkoxyheterocycle; n is 1, 2 or 3; Y and Z are independently selected CH.sub.2, CO, CR.sub.4 R.sub.5 or NR.sub.4, where R.sub.4 and R.sub.

Abstract: The present invention is directed to the following compounds of formula (I): ##STR1## wherein l is an integer of from 0 to 4; m is an integer of from 0 to 5; n is an integer of from 0 to 2; R and R' are atoms or groups independently selected from halogen, nitro, phenylalkoxy, C.sub.1-4 alkoxy, C.sub.1-6 alkyl and --O(CH.sub.2).sub.p SO.sub.3 R" wherein p is an integer of from 1 to 4 and R" is hydrogen or C.sub.1-6 alkyl, wherein said phenylalkoxy, alkoxy and alkyl groups are optionally substituted by one or more halogen atoms; R.sup.4 is a C.sub.1-6 straight alkyl group; and R.sup.5 is a C.sub.2-6 straight alkyl group; and their salts, solvates and physiologically functional derivatives, with processes and novel intermediates for their preparation, with pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidaemic conditions, such as atherosclerosis.

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: 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: 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: Compounds of formula I ##STR1## in which n=0, 1 or 2;R.sub.1, R.sub.2, R.sub.6 and R.sub.7 independently represent H or alkyl (optionally substituted by one or more halo);R.sub.3 and R.sub.4 independently represent H or alkyl or together represent a group of formula .dbd.NR.sub.12 where R.sub.12 represents H, hydroxy, alkyl, phenyl or alkoxy; each alkyl, phenyl and alkoxy being optionally substituted with one or more halo;R.sub.5 represents: (a) H, (b) alkyl, (c) a group of formula --COR.sub.13 in which R.sub.13 is H, alkyl or phenyl, when R.sub.3 and R.sub.4 represent H or alkyl (optionally substituted with one or more halo), or (d) a group of formula --S(O).sub.p R.sub.14 in which p=1 or 2 and R.sub.14 is alkyl or phenyl, when R.sub.3 and R.sub.4 represent H or alkyl (optionally substituted with one or more halo); each alkyl and phenyl optionally substituted with one or more halo;and R.sub.8 to R.sub.

Abstract: Compounds characterized generally as benzo-fused thiazopinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is a benzo-fused thiazopinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.