Abstract: Heterocyclic compounds IR.sup.1 --X--L (I)whereL is a cyclic carbamate residue, a lactonoxy residue or a lactam residue,X is an oxygen-containing group ##STR1## where A is a linker, and R.sup.1 is an organic radical or a group L,are used as activators for inorganic peroxy compounds, in particular as cold bleach activators or optical brighteners in detergents, cleaners and bleaches and in disinfectants.

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 discloses peptide aldehydes having a lactam group as part of the peptide backbone and having an original mimic group such as an amidinopiperidine or amidinophengyl tail. These compounds are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.

Abstract: A compound of the formula: ##STR1## is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: Compounds having the following formula I, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## wherein: Y.sup.1 and Y.sup.2 are each independently hydrogen, alkyl, aryl, halogen, or alkoxy;X is O or S(O).sub.t ;A is ##STR2## t is zero, one or two; m and n are independently zero or one;and wherein R, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.

Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: Compounds of formula (I), ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, unsubstituted lower alkyl or lower alkyl substituted by lower alkoxy or lower alkyl thio, or acyl which is unsubstituted or substituted by one or more of lower alkyl, lower alkyl substituted by halogen, and lower alkoxy;X is CO or CHOH;Y is CO or CH.sub.2 ; andZ is O or NH, and epimers and enantiomers thereof,or the physiologically usable salts thereof are useful as anti-tumor agents. They can be prepared by fermentation of Aspergillus sp. and, optionally, subsequent modification of functional groups.

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

Abstract: Benzothiophene, benzofuran and indole-thiazepinones, oxazepinones, and diazepinones are effective therapeutic agents for treating viral diseases, including those caused by herpesvirus and HIV.

Abstract: A novel and simple method is proposed for the synthetic preparation of an N,N-disubstituted .beta.-ketothioamide compound represented by the general formulaR.sup.1 R.sup.2 N--CS--CH.sub.2 --CO--R.sup.3,in which R.sup.1 and R.sup.2 are each a monovalent hydrocarbon group or each a divalent hydrocarbon group jointly forming a cyclic structure together with the nitrogen atom and R.sup.3 is a hydrogen atom, a monovalent hydrocarbon group or a divalent hydrocarbon group forming a cyclic structure jointly with R.sup.1, R.sup.1 being a divalent hydrocarbon group and R.sup.2 being a monovalent hydrocarbon group. The method comprises:(a) mixing an N,N-disubstituted amide compound represented by the general formulaR.sup.1 R.sup.2 N--CO--R.sup.3,and a bis(trialkylsilyl)thioketene compound represented by the general formula(R.sub.3 Si).sub.2 C.dbd.C.dbd.

Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating vital infection.

Abstract: Compounds of the formula ##STR1## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents. Processes for preparing these compounds are also disclosed.

Abstract: Compounds of the formula ##STR1## wherein X.sub.1 is ##STR2## are disclosed as possessing inhibotory activity against angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP) and thus being useful as cardiovascular agents.

Abstract: This invention is directed to a process for preparing a compound containing a persalt activators and salts thereof which are derived from imidocarboxylic acids and sulfimidocarboxylic acids of the formula I: ##STR1## in which A is a group of the formula ##STR2## n is the number 0, 1 or 2, R.sup.1 is hydrogen, chlorine, bromine, C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, aryl, or alkylaryl,R.sup.2 is hydrogen, chlorine, bromine, --SO.sub.3 M, --CO.sub.2 M or --OSO.sub.3 M, X is C.sub.1 -C.sub.19 -alkylene or arylene,B is a group of the formula C.dbd.O or SO.sub.2,L is a leaving group.

Abstract: Proposed are an N-(.alpha.-acyloxyethyl) compound, e.g., (N-(.alpha.-acetoxyethyl)-2-pyrrolidone, which is a novel compound and can be converted into an industrially very important N-vinyl compound, e.g., N-vinyl-2-pyrrolidone, by a thermal decomposition reaction under relatively mild conditions as well as a method for the preparation of such an N-(.alpha.-acyloxyethyl) compound. The N-(.alpha.-acyloxyethyl) compound can be synthesized in a high yield by the addition reaction of an NH group-containing compound, e.g., 2-pyrrolidone, with a vinyl carboxylate, e.g., vinyl acetate, in the presence of an alkaline compound such as alkali metal hydroxides.

Abstract: Compounds of formula (I) wherein n is 0, 1 or 2; and R.sup.1 and R.sup.2, which may be the same or different, each represent one or more ring substituent(s) selected from: hydrogen, hydroxy, halogen, cyano, nitro, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or C.sub.1-6 alkoxy (where the alkyl or cycloalkyl moiety may be optionally substituted by one or more substituents selected from halogen atoms and hydroxyl groups); --NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5, which may be the same or different, each represent hydrogen or C.sub.1-6 alkyl; --S(O).sub.m R.sup.6, where m is 0, 1, 2 or 3 and R.sup.6 represents hydrogen, C.sub.1-6 alkyl or C.sub.3-6 cycloakyl; --SO.sub.2 NR.sup.4 R.sup.5 where R.sup.4 et R.sup.5 are each as defined above; phenyl, phenylC.sub.1-3 alkoxy or phenylC.sub.1-3 alkyl where the phenyl group may be optionally substituted by one or more substituents independently selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, nitro, halogen and amino; and --CO.sub.2 H or --COR.sup.7 where R.sup.

Abstract: Compounds of formula (I) wherein n is 0, 1 or 2; and R.sup.1 and R.sup.2, which may be the same or different, each represent one or more ring substituent(s) selected from: hydroxy, halogen, cyano, nitro, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl or C.sub.1-6 alkoxy (where the alkyl or cycloalkyl moiety may be optionally substituted by one or more substituents selected from halogen atoms and hydroxyl groups); --NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 which may be the same or different, each represent hydrogen or C.sub.1-6 are each as defined above; phenyl, phenyl C.sub.1-3 alkoxy or phenyl C.sub.1-3 alkyl where the phenyl group may be optionally substituted by one or more substituents independently selected from C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, nitro, halogen and amino; and --CO.sub.2 H or --COR.sup.7 where R.sup.7 is C.sub.1-6 alkyl or C.sub.3-6 cycloalkyl; R.sup.3 is hydrogen or C.sub.

Abstract: Benzothiophene, benzofuran and indolethiazepinones, oxazepinones and diazepinones as well as methods of preparation thereof are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases; these compounds also inhibit the activation of human immunodeficiency virus (HIV).

Abstract: Disclosed are pyrido[2,3-b][1,5]benzoxazepin (and thiazepin)-5(6H)-ones and -thiones. These are useful in the prevention or treatment of AIDS.

Abstract: Compounds of the class of pyrido[2,3-b][1,4]benzoxazepin (and thiazepin)-6(5H)-ones and -thiones, having the following general structural formula ##STR1## wherein either X or Z is sulfur and the other substituent is oxygen or both X and Z are sulfur, which are inhibitors of HIV-1 reverse transcriptase and useful in the treatment of HIV-1 infection. An exemplary compound is 2-chloro-5-(methylthioethyl)pyrido[2,3-b][1,4]benzoxazepin-6(5H)one.

Abstract: The invention relates to novel eburnamenine derivatives of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 as well as R.sup.3 and R.sup.4, independently from each other, stand for hydrogen, C.sub.2-6 alkyl group, C.sub.2-6 alkenyl group; or a C.sub.3-10 alicyclic group involving 1 to 3 rings, and this latter group may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, together with the adjacent nitrogen atom and optionally with an additional oxygen or nitrogen atom, form a 4- to 6-membered, saturated or unsaturated cyclic group which may be substituted by a C.sub.1-6 alkyl or C.sub.2-6 alkenyl group; two of X, Y and Z are nitrogen whereas the third of them means a methine group; n is 1 or 2; W means oxygen or two hydrogen atoms; and the wavy line means .alpha.-/.alpha.-, .alpha.-/.beta.- or .beta.-/.alpha.- steric position, as well as their acid addition salts and solvates.

Abstract: Novel piperidine-triazine compounds of the formula (I) useful as light stabilizers, heat stabilizers and antioxidants for organic materials.The meanings of R.sub.1, R.sub.2, R.sub.3, R.sub.4, X.sub.1, X.sub.2, X.sub.3, Y.sub.1, Y.sub.2, M and N are defined in the text.

Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E.sub.2 antagonists for the treatment of prostaglandin-E.sub.2 mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin-E.sub.2 mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and for the treatment of prostaglandin E.sub.2 -mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin E.sub.2 -mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.

Abstract: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.

Abstract: Compounds characterized generally as oxazopinyl-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 an oxazopinyl 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--(CH.sub.2).sub.q --C.tbd.C-Vwherein 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.

Abstract: Compounds characterized generally as 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 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--(CH.sub.2).sub.q --C.tbd.C--Vwherein 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.

Abstract: The invention relates to tricyclic heterocycles of the formula I ##STR1## wherein X is oxy, thio, sulphinyl, sulphonyl, amino, (1-4C)alkylamino or methylene;Y is carbonyl or methylene;each R.sup.1 includes hydrogen, halogeno and various other substituents;each of m and n is 1 or 2;A.sup.1, alkylene, alkenylene or alkynylene;Het is a 5 or 6 membered heteroaryl group optionally bearing particular substituents; andG is carboxy, 1H-tetrazol-5-yl or a group of the formula:--CONH--SO.sub.2 R.sup.2wherein R.sup.2 is (1-4C)alkyl, benzyl or phenyl;and pharmaceutically-acceptable salts thereof, which possess anti-hyperalgesic properties. The invention also relates to processes for the manufacture of said tricyclic heterocycles; and to novel pharmaceutical compositions containing them.

Abstract: A purification method of intermediates for the preparation of Diltiazem which consists of the crystallization of a mixture enantiomerically enriched in (2S,3S)-2,3-dihydro-3-hydroxy-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H) -one is described.

Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.

Abstract: Compounds of the formula ##STR1## in which A.sub.1 and A.sub.2 independently of one another are CO--C.sub.1 -C.sub.4 alkyl, COO--C.sub.1 -C.sub.4 alkyl, CO--CF.sub.3, CO--N(R).sub.2 or cyano;A.sub.1 and A.sub.2 together are CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO, CO(X).sub.n --C.sub.1 -C.sub.3 alkylene-(X).sub.n CO which is substituted by C.sub.1 -C.sub.4 alkyl, COOR, CON(R).sub.2, cyano or phenyl, it being possible for the phenyl ring, in turn, to be substituted by halogen, methyl, trifluoromethyl, methoxy, nitro or cyano; CO--N(R)--CO--N(R)--CO;R is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkenyl or C.sub.3 -C.sub.6 alkynyl;X is oxygen, sulfur or N(CH.sub.3);X.sub.1, X.sub.2 and X.sub.3 independently of one another are hydrogen, halogen, methyl, methylthio, methoxy or nitro;n is 0 or 1;including the salts of the compounds of the formula I with agriculturally acceptable organic or inorganic bases, and including the metal complexes; have valuable microbicidal properties.

Abstract: There are provided alkyl esters of 5-heterocyclic-pyridine-2,3-dicarboxylic acids useful as intermediates for the preparation of highly effective 5-heterocyclic-2-(2-imidazolin-2-yl)pyridine herbicidal agents and methods for the preparation thereof.

Abstract: The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents.A compound disclosed is 2,4-diallylamino-6-{4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl) methylamino]piperidin-1-yl}-1,3,5-triazine.

Abstract: This invention relates to a compound of formula I ##STR1## wherein p is 1 to 3;R.sup.1 and R.sup.2 each are independently hydrogen or an acyl group R.sup.6 CO--, in which R.sup.6 is C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-7 alkenyl, aryl or radical of the formula ##STR2## R.sup.3 is hydrogen or chloro; R.sup.4 and R.sup.5 each are independently C.sub.1-6 alkyl.Compounds of formula I are useful for the reversal of multidrug resistance of cancer drugs.

Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in inhibition of absorption of cholesterol and thus lowers serum cholesterol levels. Compounds of the formula below: ##STR1## where R.sup.1 is selected from alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or arylalkyl and R.sup.2 is hydrogen or alkyl or --NR.sup.1 R.sup.2 is morpholine, thiomorpholine or 4-substituted or unsubstituted piperidine and R.sup.3, R.sup.4, R.sup.5, R.sup.6 are hydrogen, alkyl, alkoxy, halogen, nitro, cyano, perhaloalkyl, alkanoyloxy, alkoxycarbonyl or hydroxycarbonyl have been shown to inhibit the enzymes CEH and/or ACAT in in vitro tests to inhibit absorption of radio-labeled cholesterol in rats.

Abstract: Sulfimidoperoxycarboxylic acids of the formula ##STR1## in which A is a group of the formula ##STR2## n is the number 0, 1 or 2, R.sup.1 is hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.20 - alkyl, C.sub.2 -C.sub.20 -alkenyl, aryl or C.sub.1 -C.sub.10 -alkylaryl,R.sup.2 is hydrogen, fluorine, chlorine, bromine or a group of the formula SO.sub.3 M, CO.sub.2 M or OSO.sub.3 M,M is hydrogen, an alkali metal or ammonium ion or the stoichiometric amount of an alkaline earth metal ion andX is C.sub.1 -C.sub.19 -alkylene or ortho-, meta- or para-arylene.These sulfimidoperoxycarboxylic acids are suitable as bleaches, oxidants or disinfectants.

Abstract: A novel class of sulfonamoyl-substituted 1,6-diaza[4.4]spirodilactams, having a sulfonamoyl substituent on the hydrocarbyl group attached to each spiro ring nitrogen atom, is useful for the preparation of polymers, including polyamides and as latent curing agents for epoxy resins.

Abstract: The present invention relates to a pyrimidine derivative having the formula ##STR1## (wherein the variables are defined in the full text of the patent), a method for producing the same, and its use as a herbicide.

Abstract: Mercaptoacyl aminolactam inhibitors of endopeptidases of the formula ##STR1## wherein Y is -(CHR.sup.5).sub.n (CR.sup.3 R.sup.4)- or -(CR.sup.3 R.sup.4).sub.p X(CR.sup.3 R.sup.4).sub.q -,wherein two substituents selected from the group consisting of R.sup.3, R.sup.4 and R.sup.5, can form a benzene, cyclopentane or cyclohexane ring;X is -O-, -S-, -SO- or -SO.sub.2 -;Q is hydrogen or R.sup.6 CO-;m is 1 or 2;n is 1, 2, 3 or 4;p is 1 or 2;q is 2 or 3;R.sup.1 is lower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen, lower alkyl, hydroxylower alkyl, lower alkoxylower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, lower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.5 is hydrogen, lower alkyl, aryllower alkyl, heteroaryllower alkyl, hydroxy, lower alkoxy, mercapto, or lower alkylthio; and R.sup.

Abstract: The invention relates to thiazepine derivatives, which are antagonists of platelet activating factor, of the formula: ##STR1## wherein R.sup.1 is ar(lower)alkyl which may have suitable substituent(s),R.sup.2 is hydrogen, lower alkyl which may have suitable substituent(s), or a group of the formula: ##STR2## in which A is lower alkylene and X is halogen, n is 0, 1 or 2 and Y is --CH.sub.2 --CH.sub.2 -- or ##STR3## or a pharmaceutically acceptable salt thereof.

Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.

Abstract: Cyclic sulfur-containing compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is hydrogen or lower alkyl,R.sup.3 is hydrogen or lower alkyl,X is S--S,m is 0 or 1 andn is 1 or 2, with the proviso that when m is 0,n is 2, and pharmaceutically acceptable salts thereof.Such compounds are useful for treating liver disorders and autoimmune diseases.

Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein R.sub.c is carboxy, esterified carboxy or amidated carboxy;R.sub.2 is hydrogen or lower alkyl or joins with R.sub.a and R.sub.b and the atoms therebetween to form a fused ring ##STR2## and either R.sub.a is methyl and R.sub.b is ##STR3## or R.sub.2 and R.sub.b and the atoms therebetween form a group wherein R.sub.3 and R.sub.4 are either both hydrogen, or together are propylene, butylene, or with the two atoms to which they are attached form a benzene ring. Methods of manufacture and use thereof in the production of angiotensin converting enzyme inhibitors are disclosed.

Abstract: Urethane-protected NCAs and MTAs are prepared by reacting an NCA or NTA with a haloformate in an inert diluent, under anhydrous conditions and in the presence of a tertiary nitrogen-containing base having an atom or functional group sufficiently electron rich and positioned relative to the nitrogen of said base so as to render said atom or group capable of complexing with the H--N< group of said N-carboxyanhydride or N-thiocarboxyanhydride but able to generate N-carboxyanhydride or N-thiocarboxyanhydride anionic complexes capable of reacting with the haloformate.

Abstract: Novel cyclic ester-amides having the formula: ##STR1## where R is an alkyl group having from 2 to 5 carbon atoms, and x ranges from 2 to 6 by reacting a polyethylene glycol monoamine having the formula NH.sub.2 --(CH.sub.2 CH.sub.2 O).sub.x --H, where x is as above, with at least one dicarboxylic acid, where the dicarboxylic acid is selected from the group consisting of glutaric, adipic, pimelic acids and mixtures thereof. The a molar ratio of polyethylene glycol monoamine to dicarboxylic acid should be about 1:1. Catalysts may be optionally used, and may include such compounds as titanium alkoxides; and zinc, manganese and antimony salts of carboxylic acids. This method is anticipated to be a useful step in a new preparation of valuable cyclic products.

Abstract: Novel hexahydro-1H-quino[4,3,2-ef][1,4]benzoxazepines and related compounds, intermediates for the preparation thereof, and a method for relieving memory dysfunction, utilizing the compounds are disclosed.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 substituents selected from the group consisting of halogen and lower alkoxy; R.sub.2 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkanoyl, ##STR2## R.sub.3 and R.sub.4 are independently lower alkyl, phenyl lower alkyl or together form a piperidine or pyrrolidine ring; n is 2 ro 4; m is 1 to 2; and pharmaceutically acceptable acid addition salts thereof, with the proviso that when R.sub.1 is 4-methoxyphenyl, R.sub.2 is hydrogen and R.sub.3 and R.sub.4 are methyl; and n is 2, the compound of formula I cannot be in the (-)-cis form,are described. The compounds of formula I are active as calcium channel blockers and accordingly, are useful as agents for treating ischemia.

Abstract: Certain substituted indazoles, including all geometric and stereoisomers thereof, agricultural compositions containing the indazoles and use of the indazoles as insecticides.