Abstract: Disclosed herein are 2,3-dihydro-1H-indole-2-carboxylic acids substitued on the nitrogen with 3-mercapto-2-alkyl-1-oxoalkyl, 3-phosphoryl-2-alkyl-1-oxopropyl, or 2-amino-2-alkyl-1-oxoalkyl derivatives which act as inhibitors of angiotensin converting enzyme and as antihypertensive agents. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen; Y is hydrogen, lower alkyl, or aryl;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is ##STR2## wherein: L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, SR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.10 are, independently, hydrogen, lower alkyl, or aryl);A is O, NR.sub.

Abstract: Disclosed herein are 2,3-dihydro-1H-indole-2-carboxylic acids substituted on the nitrogen with 3-mercapto-2-alkyl-1-oxoalkyl, 3-phosphoryl-2-alkyl-1-oxopropyl, or 2-amino-2-alkyl-1-oxoalkyl derivatives which act as inhibitors of angiotensin converting enzyme and as antihypertensive agents. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is ##STR2## wherein: L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, SR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.10 are, independently, hydrogen, lower alkyl, or aryl);A is O, NR.sub.

Abstract: 2,3,4,10-Tetrahydro-3,3-dimethyl-10-phenylpyrimido[1,2-a]indol-10-ol and the pharmaceutically acceptable acid addition salts thereof are useful in treatment or preventing obesity in mammals. The compounds may be administered in pharmaceutical compositions, optionally with one or more vitamins.

Abstract: Thiazolotriazine derivatives having the formula I ##STR1## their pharmaceutically acceptable salts, pharmaceutically acceptable triazolotriazinium compounds containing the cation having formula II ##STR2## and their zwitterionic forms and pharmaceutically acceptable acid addition salts [where A is hydroxy whilst B is hydrogen or A and B together represent a direct bond; R.sup.1 is aryl; R.sup.2 and R.sup.3 are independently lower alkyl or ar(lower)alkyl] are novel compounds useful as anti-cancer agents.

Abstract: Disclosed herein are (lower)alkylsulfonyl derivatives of various proline amides, thiazolidine carboxylic acid amides and indoline-2-carboxylic acid amides, among others, which inhibit angiotensin converting enzyme and are antihypertensive agents.

Abstract: The invention provides novel thiomorpholines of the formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts wherein n represents 0 or 1, R.sup.1 represents (lower)alkyl, R.sup.2 represents hydrogen or (lower)alkyl, R.sup.3 represents hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, 2-tetrahydrofurylmethyl or cycloalkylmethyl and R.sup.4 represents hydrogen, hydroxy, acyloxy or a protected hydroxy group, with the proviso that when n is 0, R.sup.4 is other than hydrogen. The compounds in which n is 0 and R.sup.4 is lower alkoxy, hydroxy or acyloxy are analgesics and/or opiate antagonists and the compounds in which n is 1 and R.sup.4 is hydrogen are hypotensives or anti-hypertensives. The other compounds of formula (I) are intermediates for the pharmacologically active compounds.

Abstract: The invention concerns compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O,S,--CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or defined substituents and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocyclic or heterocyclic ring optionally carrying one or more defined substituents; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is --CO-- or --CH.sub.

Abstract: Disclosed herein are .alpha.-[(alkylamino)methyl]-.beta.-aryloxy-benzeneethanols exhibiting antiarrhythmic activity and having the following formula: ##STR1## wherein R is hydrogen, halogen, lower alkyl, or lower alkoxy; X is phenyl, 1-naphthyl, or a phenyl group substituted by a halogen, a lower alkyl group, or a lower alkoxy group; R.sub.1 is lower alkyl; and pharmacologically acceptable acid addition salts thereof. Also disclosed is a process for the addition of an aryloxy group at the 3-position of a 3-phenyl-2-oxiranecarboxamide to produce an .alpha.-hydroxy-.beta.-aryloxy-benzenepropanamide, said process comprising contacting an alkali metal aryloxide with said 3-phenyl-2-oxiranecarboxamide in the presence of a crown ether. Such .alpha.-hydroxy-.beta.-aryloxy-benzenepropanamides may then be reduced to produce the compounds of the invention.

Abstract: Disclosed herein are N-(3-mercapto-2-alkyl-1-oxopropyl)-2,3-dihydro-1H-indole-2-carboxylic acids and derivatives thereof which act as inhibitors of angiotensin converting enzyme and as anti-hypertensive agents. Derivatives include those in which the 3-mercapto group is substituted with phosphate derivatives or is replaced by a variously substituted amino group. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is -SH, ##STR2## wherein L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, SR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.

Abstract: Disclosed herein are N-(3-mercapto-2-alkyl-1-oxopropyl)-2,5-dihydro-1H-indole-2-carboxylic acids and derivatives thereof which act as inhibitors of angiotensin converting enzyme and as anti-hypertensive agents. Derivatives include those in which the 5-mercapto group is substituted with phosphate derivatives or is replaced by a variously substituted amino group. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is --SH, ##STR2## wherein L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, SR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.

Abstract: Morpholine derivatives of the formula ##STR1## and their pharmaceutically acceptable acid addition salts[wherein R.sup.1 represents lower alkyl. R.sup.2 represents hydrogen, lower alkyl, benzyl, lower alkoxymethyl or an acyl group; R.sup.3 represents hydrogen, lower alkyl or phenyl; R.sup.4, R.sup.5 and R.sup.6 are independently hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, aryl(lower)alkyl, tetrahydrofurylmethyl or cycloalkylmethyl] possess analgesic and/or opiate antagonistic activity.

Abstract: Disclosed herein are 3[[(2,3-dihydro-1H-indole-2-yl)carbonyl]thio]propanoic (and acetic) acids of the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl, or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen; andY is hydrogen, lower alkyl, or aryl; or salts thereof.These compounds are intermediates for the production of 1H,3H-[1,4]thiazepino[4,3-a]indoles and 1H-[1,4]thiazino[4,3-a]indoles which possess Angiotensin Converting Enzyme inhibition activity and anti-hypertensive activity.

Abstract: Disclosed herein are 2,3-dihydro-1H-indole-2-carboxylic acids substituted on the nitrogen with 3-mercapto-2-alkyl-1-oxoalkyl, 3-phosphoryl-2-alkyl-1-oxopropyl, or 2-amino-2-alkyl-1-oxoalkyl derivatives which act as inhibitors of angiotensin converting enzyme and as antihypertensive agents. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is ##STR2## wherein: L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, SR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.10 are, independently, hydrogen, lower alkyl, or aryl);A is O, NR.sub.

Abstract: The compounds of this invention are designated as quinoxalinyl esters of carbamimidothioic acids and exhibit the pharmacological properties of preventing gastric ulcers, reducing gastric secretions and lowering blood pressure. The compounds have the following structural formula: ##STR1## in which Q is hydrogen or nitro;A is hydrogen, methyl, ethyl, propyl, isopropyl, n-butyl, carbomethoxy, carbethoxy, carbopropoxy, carbisopropoxy, carbobutoxy, carbisobutoxy, or carbo-t-butoxy; andR.sup.1, R.sup.2, and R.sup.3 are, independently, hydrogen, methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, t-butyl, allyl, or R.sup.1 and R.sup.3 may be concatenated with a carbon chain having 4 carbon atoms with R.sup.2 then being hydrogen; except that, when A and Q are hydrogen, R.sup.1, R.sup.2, and R.sup.3 may not all be hydrogen; and with the further exception that, where A is methyl and R.sup.1, R.sup.2, and Q are all hydrogen, R.sup.3 may not be ethyl;or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of the formula: ##STR1## wherein: Y is 2,6-dimethylphenyl, 2,5-dimethylphenyl, [5-bromo-2-methylphenyl], or 5-chloro-2-methylphenyl; andX is propyl, isopropyl, n-butyl, or isobutyl; or a non-toxic, pharmaceutically acceptable acid addition salt thereof; possess anti-arrhythmic activity.

Abstract: Disclosed herein are .alpha.-[(alkylamino)-methyl]-.beta.-aryloxy-benzeneethanols exhibiting antiarrhythmic activity and having the following formula: ##STR1## wherein R is hydrogen, halogen, lower alkyl, or lower alkoxy; X is phenyl, 1-naphthyl, or a phenyl group substituted by a halogen, a lower alkyl group, or a lower alkoxy group; R.sub.1 is lower alkyl; and pharmacologically acceptable acid addition salts thereof. Also disclosed is a process for the addition of an aryloxy group at the 3-position of a 3-phenyl-2-oxiranecarboxamide to produce an .alpha.-hydroxy-.beta.-aryloxy-benzenepropanamide, said process comprising contacting an alkali metal aryloxide with said 3-phenyl-2-oxiranecarboxamide in the presence of a crown ether. Such .alpha.-hydroxy-.beta.-aryloxy-benzenepropanamides may then be reduced to produce the compounds of the invention.

Abstract: Disclosed herein are N-(3-mercapto-2-alkyl-1-oxopropyl)-2,3-dihydro-1H-indole-2-carboxylic acids and derivatives thereof which act as inhibitors of angiotensin converting enzyme and as anti-hypertensive agents. Derivatives include those in which the 3-mercapto group is substituted with phosphate derivatives or is replaced by a variously substituted amino group. The compounds of the invention (excluding disclosed intermediates) have the general formula: ##STR1## wherein: n is 1 or 0;R.sub.1 is hydrogen, lower alkyl, aryl or aralkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen, lower alkyl or aroyl;R.sub.5 is hydroxy, amino, or lower alkoxy;X is hydrogen, hydroxy, lower alkyl, lower alkoxy, or halogen;Y is hydrogen, lower alkyl, or aryl;R.sub.4 is --SH, ##STR2## wherein L is O, NR.sub.7 or S (where R.sub.7 is hydrogen or lower alkyl);M is R.sub.8, OR.sub.8, or NR.sub.9 R.sub.10 (where R.sub.8 is hydrogen, lower alkyl, aryl, or aralkyl; and R.sub.9 and R.sub.

Abstract: Method of suppressing cardiac arrhythmias compounds of the formula: ##STR1## wherein: Y is 2,6-dimethylphenyl, 2,5-dimethylphenyl, 5-bromo-2-methylphenyl, or 5-chloro-2-methylphenyl; andX is propenyl, propynyl, or cyclopropyl; or a non-toxic, pharmaceutically acceptable acid addition salt thereof.

Abstract: Peptides of the formula: ##STR1## wherein: X is H, --NH.sub.2, --NH--Gly--Ala, --NH--D--Ala--Ala, --NH--Gly--Gly--Gly, --NH--acetyl, or --NH--benzoyl;X.sub.1 is His or Arg;X.sub.2 is His, Glu, Tyr, Trp, or Phe;X.sub.3 is Trp, D-Trp, or 6-F-D-Trp; andX.sub.4 is a D-.alpha.-amino acid;or the reduced, linear form thereof, or a non-toxic, pharmaceutically acceptable acid addition salt thereof; inhibit the release of growth hormone, insulin, and glucagon; and show prolonged inhibition activity. Said peptides are prepared by solid-state methodology.

Abstract: Disclosed are substituted-(D-Met.sup.2, D-Ser.sup.5)-enkephalins which elicit analgesic activity when administered peripherally.