Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
321 words
A compound of the formula: wherein: R is hydrogen; alkyl of from 1 to 12 carbon atoms which include branched, cyclic and unsaturated alkyl groups; substituted loweralkyl wherein the substituent can be halo, hydroxy, carboxy, loweralkylthio, loweralkoxy, loweralkoxycarbonyl, loweraralkoxycarbonyl, amino, loweralkylamino, lowerdialkylamino, or acylamino substituted loweralkyl having the formula R 1 (CH 2 ) n -Q-(CH 2 ) m wherein n is A 0 -2, m is 1-3, R 1 is aryl or heteroaryl A optionally substituted by amino, lowerdialkylamino, loweralkylamino, hydroxy, hydroxyloweralkyl, aminoloweralkyl, trihaloloweralkyl, cyano, nitro, sulfonamido, aroyl, loweralkyl, halo, dihalo, and loweralkoxy, and Q is O, S, N- , , CO, CH=CH wherein is hydrogen, loweralkyl, aryl, aralkyl, loweralkanoyl, or aroyl, and R 1 is hydrogen, or loweralkyl; C aryl; substituted aryl wherein the substituent is loweralkyl, aminoloweralkyl, loweralkoxy, aryloxy, aroyl, hydroxy, halo, or dihalo; aralkyl or heteroaralkyl which include branched loweralkyi groups; substituted aralkyl or substituted heteroaralkyl which include branched loweralkyl groups wherein the loweralkyl groups can be substituted by amino, acylamino, or hydroxyl and the aryl and heteroaryl groups can be substituted by halo, dihalo, loweralkyl, hydroxy, loweralkoxy, aryloxy, aroyl, arylthio, amino, aminoloweralkyl, loweralkanoylamino, aroylamino, lowerdialkylamino, loweralkylamino, hydroxyloweralkyl, trihaloloweralkyl, nitro, cyano, or sulfonamido; R 2 and R 4 are independently hydroxy; loweralkoxy; loweralkenyloxy; arloweralkoxy; acylloweralkoxy; amino; loweralkylamino; diloweralkylamino; carboxymethylamino; carboxamidomethylamino; or aryloxy, or mono-or disubstituted aryloxy wherein the substituents are chloro; m is 1-4; R 3 is where n is 2-5; provided that where n=3 or 4, the carbon chain may be unsaturated between carbons 2-3 for n=3, and between carbons 2-3 or 3-4 or both for n=4; the R a 's are independently hydrogen; hydroxy; amino; mono- or diloweralkylamino; loweralkyl; phenyl; phenoxy; phenylloweralkyl; hydroxyphenylloweralkyl; aminoloweralkyl; hydroxyloweralkyl; mercaptoloweralkyl; loweralkylthioloweralkyl; imidazolylloweralkyl; indolylloweralkyl; carboxyl; carboxamide; loweralkoxycarbonyl; carboxyloweralkyl; carboxamidoloweralkyl; or loweralkoxycarbonylloweralkyl; and the R b 's are independently hydrogen or loweralkyl; R 5 is hydrogen; halo: hydroxy; loweralkyl; loweralkoxy; amino; or mono- or diloweralkylamino; and a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
321 words
A compound of the formula: wherein: R is hydrogen; alkyl of from 1 to 12 carbon atoms which include branched, cyclic and unsaturated alkyl groups; substituted loweralkyl wherein the substituent can be halo, hydroxy, carboxy, loweralkylthio, loweralkoxy, loweralkoxycarbonyl, loweraralkoxycarbonyl, amino, loweralkylamino, lowerdialkylamino, or acylamino substituted loweralkyl having the formula R 1 (CH 2 ) n -Q-(CH 2 ) m wherein n is A 0 -2, m is 1-3, R 1 is aryl or heteroaryl A optionally substituted by amino, lowerdialkylamino, loweralkylamino, hydroxy, hydroxyloweralkyl, aminoloweralkyl, trihaloloweralkyl, cyano, nitro, sulfonamido, aroyl, loweralkyl, halo, dihalo, and loweralkoxy, and Q is O, S, N- , , CO, CH=CH wherein is hydrogen, loweralkyl, aryl, aralkyl, loweralkanoyl, or aroyl, and R 1 is hydrogen, or loweralkyl; C aryl; substituted aryl wherein the substituent is loweralkyl, aminoloweralkyl, loweralkoxy, aryloxy, aroyl, hydroxy, halo, or dihalo; aralkyl or heteroaralkyl which include branched loweralkyi groups; substituted aralkyl or substituted heteroaralkyl which include branched loweralkyl groups wherein the loweralkyl groups can be substituted by amino, acylamino, or hydroxyl and the aryl and heteroaryl groups can be substituted by halo, dihalo, loweralkyl, hydroxy, loweralkoxy, aryloxy, aroyl, arylthio, amino, aminoloweralkyl, loweralkanoylamino, aroylamino, lowerdialkylamino, loweralkylamino, hydroxyloweralkyl, trihaloloweralkyl, nitro, cyano, or sulfonamido; R 2 and R 4 are independently hydroxy; loweralkoxy; loweralkenyloxy; arloweralkoxy; acylloweralkoxy; amino; loweralkylamino; diloweralkylamino; carboxymethylamino; carboxamidomethylamino; or aryloxy, or mono-or disubstituted aryloxy wherein the substituents are chloro; m is 1-4; R 3 is where n is 2-5; provided that where n=3 or 4, the carbon chain may be unsaturated between carbons 2-3 for n=3, and between carbons 2-3 or 3-4 or both for n=4; the R a 's are independently hydrogen; hydroxy; amino; mono- or diloweralkylamino; loweralkyl; phenyl; phenoxy; phenylloweralkyl; hydroxyphenylloweralkyl; aminoloweralkyl; hydroxyloweralkyl; mercaptoloweralkyl; loweralkylthioloweralkyl; imidazolylloweralkyl; indolylloweralkyl; carboxyl; carboxamide; loweralkoxycarbonyl; carboxyloweralkyl; carboxamidoloweralkyl; or loweralkoxycarbonylloweralkyl; and the R b 's are independently hydrogen or loweralkyl; R 5 is hydrogen; halo: hydroxy; loweralkyl; loweralkoxy; amino; or mono- or diloweralkylamino; and a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
59 words
A compouna according to Claim 1 selected from the group consisting essentially of: 1-ethoxycarbonylethyl-3-(1-carboethoxy-3-phenyl-1-propyl)aminohomodihydrocarbostyril; 1-carboxyethyl-3-(1-carboxy-3-phenyl-1-propyl)aminohomodihydrocarbostyril; 1-ethoxycarbonylethyl-3-(1-carboethoxy-3-phenyl-1-propyl)aminohexahydrobenzoazocine-2-one; 1-carboxyethyl-3-(1-carboxy-3-phenyl-1-propyl) aminohexahydrobenzoazocine-2-one, and ethyl diester; 1-(3-carboxypropyl)-3-(l-carboxy-3-phenyl-l-propyl) aminohomodihydrocarbostyril, and ethyl diester; 1-(4-carboxybutyl)-3-(1-carboxy-3-phenyl-1-propyl) aminohomodihydrocarbostyril, and ethyl diester; 1-carboxyethyl-3-(1-carboxy-3-phenyl-1-propyl) aminodihydrocarbostyril, and ethyl diester; 1-(3-carboxypropyl)-3-(1-carboxy-3-phenyl-1-propyl) aminohexahydrobenzoazocine-2-one, and ethyl diester; 1-(4-carboxybutyl)-3-(1-carboxy-3-phenyl-1-propyl) aminohexahydrobenzoazocine-2-one, and ethyl diester; 1-(3-carboxypropyl)-3-(1-carboxy-3-phenyl 1-propyl) aminodihydrocarbostyril, and ethyl diester; 1-(4-carboxybutyl)-3-(l-carboxy-3-phenyl-l-propyl) aminodihydrpcarbostyril, and ethyl diester; 1-ethoxycarbonylethyl-3-(1-carboxy-3-phenyl-1-propyl) aminohomodihydrocarbostyril.
Claim 4
Dependent Claim
23 words
A pharmaceutical composition useful in treating hypertension comprising a pharmaceutically acceptable carrier and an antihypertensively effective amount of a compound of Claim 1:
Claim 5
Dependent Claim
64 words
A composition according to Claim 3 wherein said compound is a member selected from the group consisting essentially of: 1-ethoxycarbonylethyl-3-(1-carboethoxy-3-phenyl-1-propyl)aminohomodihydrocarbostyril; 1-carboxyethyl-3-(1-carboxy-3-phenyl-1-propyl)aminohomodihydrocarbostyril; 1-ethoxycarbonylethyl-3-(1-carboethoxy-3-phenyl-1-propyl)aminohexahydrobenzoazocine-2-one; 1-carboxyethyl-3-(1-carboxy-3-phenyl-1-propyl) aminohexahydrobenzoazocine-2-one, and ethyl diester; 1-(3-carboxypropyl)-3-(1-carboxy-3-phenyl-1-propyl) aminohomodihydrocarbostyril, and ethyl diester; 1-(4-carboxybutyl)-3-(1-carboxy-3-phenyl-1-propyl) aminohomodihydrocarbostyril, and ethyl diester; l-carboxyethyl-3-(l-carboxy-3-phenyl-l-propyl) aminodihydrocarbostyril, and ethyl diester; 1-(3-carboxypropyl)-3-(1-carboxy-3-phenyl-1-propyl) aminohexahydrobenzoazocine-2-one, ana ethyl diester; 1-(4-carboxybutyl)-3-(1-carboxy-3-phenyl-l-propyl) aminohexahydrobenzoazocine-2-one, and ethyl diester; 1-(3-carboxypropyl)-3-(1-carboxy-3-phenyl-1-propyl) aminodihydrocarbostyril, and ethyl diester; 1-(4-carboxybutyl)-3-(1-carboxy-3-phenyl-1-propyl) aminodihydrocarbostyril, and ethyl diester; l-ethoxycarbonylethyl-3-(l-carboxy-3-phenyl-l-propyl) aminohomodihydrocarbostyril.
Claim 6
Dependent Claim
101 words
A composition according to Claim 3 which includes an antihypertensively effective amount of an antihypertensive and/or diuretic compound selected from the group consisting of acetazolamide, amiloride, aminophylline, atenolol, bendroflumethiazide, benzthiazide, bumetanide, chlorothalidone, chlorothiazide, clonidine, cryptenamine acetates and cryptenamine tannates, cyclothiazide, deserpidine, diazoxide, diltiazem, (S)-1-[[2-(3,4-dimethoxyphenyl)-ethyl]amino]-3-[[4-(2-thienyl)-lH-imidazol-2-yl]-phenox y]-2-propanol, ethacrynic acid, flumethiazide, furosemide, guanethidene sulfate, hydralazine hydrochloride, hydrochlorothiazaide, hydro- flumethiazide, (+)-4-[3-[-[2-(1-hydroxycyclohexyl)ethyl]4-oxo-2-thiazolidinyl]propyl]-benzoic acid, indacrinone and variable ratios of its enantiomers, merethoxylline procaine, methylclothiazide, methyldopa, methyldopate hydrochloride, metolazone, metoprolol tartate, minoxidil, naldolol, nifedipine, pargyline hydrochloride, pindolol, polythiazide, prazosin, propranolol, quinethazone, rauwolfia serpentina, rescinnamine, reserpine, sodium ethacrynate, sodium nitroprusside, spironolactone, ticrynafen, timolol, triamterene, trichlormethiazide, trimethophan camsylate, and verapamil.