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Browse by: INVENTOR PATENT HOLDER PATENT NUMBER DATE
 
 
Inventor:
Krapcho; John
Address:
Somerset, NJ
No. of patents:
67
Patents:


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Patent Number Title Of Patent Date Issued
RE33072 Benzothiazepine derivatives September 26, 1989
Vasodilating activity is exhibited by compounds having the formula ##STR1## n is 2 or 3; X is oxygen or sulfur,R.sub.1 and R.sub.2 are each independently hydrogen alkyl, cycloalkyl, or allyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are pyrrol
5116851 Pharmaceutical composition and method for treating cardiovascular diseases using substituted ani May 26, 1992
A novel pharmaceutical composition and method is disclosed for the treatment of cardiovascular diseases, e.g. myocardial ischemia and/or arrhythmia. The method and composition include an effective amount of a compound of the formula ##STR1## wherein X, Y, R, R.sub.1, A, A', m, n,
4963671 Process for resolving chiral intermediates used in making calcium channel blockers October 16, 1990
This process enables preparation of the preferred (+)-threo enantiomer by resolution of its racemic mixture of a compound of the formula ##STR1## wherein Y.sup.1 and Y.sup.2 are each independently lower alkyl and R.sup.1 is hydrogen or lower alkyl. The compound is treated with a chir
4952692 Benzazepine derivatives August 28, 1990
Novel compounds of the formula ##STR1## exhibit calcium channel blocking activity and are useful as cardiovascular agents.
4946840 Benzazepine and benzothiazepine derivatives August 7, 1990
Vasodilating activity is exhibited by compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein X is --CH.sub.2 -- or --S--;R.sub.1 is ##STR2## or --O--Y.sub.3 ; R.sub.2 is heterocyclo or heteroaryl;R.sub.3 and R.sub.4 are each independentl
4902684 Benzazepine and benzothiazepine derivatives February 20, 1990
Vasodilating activity is exhibited by compounds having the formula ##STR1## wherein X can be --S--or --CH.sub.2 --; andR.sub.2 is ##STR2##depending upon the definition of X.
4752645 Benzazepine derivatives June 21, 1988
Vasodilating activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof.
4748239 Benzazepine derivatives May 31, 1988
Vasodilating activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof.
4709046 Acylmercaptoalkanoyl and mercaptoalkanoyl spiro compounds November 24, 1987
Spiro compounds of the formula ##STR1## wherein X is oxygen or sulfur. These compounds possess antgiotensin converting enzyme inhibition activity and are thus useful as anti-hypertension agents.
4584131 Benzothiazepine derivatives April 22, 1986
Vasodilating activity is exhibited by compounds having the formula ##STR1## n is 2 or 3; X is oxygen or sulfur;R.sub.1 and R.sub.2 are each independently hydrogen alkyl, cycloalkyl, or allyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are pyrrol
4578474 Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids March 25, 1986
Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.
4499287 Certain-4-hydroxy-proline derivatives February 12, 1985
Compounds of the formula ##STR1## are useful as intermediates in the preparation of various hypotensive agents.
4497953 Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids February 5, 1985
Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.
4468519 Esters of phosphinylalkanoyl substituted prolines August 28, 1984
Hypotensive activity is exhibited by compounds having the formula ##STR1## and salts thereof wherein R.sub.1 is alkyl, aryl, arylalkyl, cycloalkyl, or cycloalkylalkyl;R.sub.2 is cycloalkyl, 3-cyclohexenyl or 2-alkyl-3-cyclohexenyl;R.sub.3 is alkyl, cycloalkyl, phenyl or alkoxy;R.sub.4 is
4462943 Carboxyalkyl amino acid derivatives of various substituted prolines July 31, 1984
Carboxyalkyl dipeptides of the formula ##STR1## wherein R.sub.4 is a 3-, 4-, 5-, or 4,4-substituted proline are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity.
4456761 4-Substituted dehydroprolines June 26, 1984
Compounds of the formula ##STR1## are useful as intermediates in the preparation of various hypotensive agents.
4390695 Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids June 28, 1983
Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.
4356182 Mercaptoacyl derivatives of 4-disubstituted prolines October 26, 1982
This invention is directed to compounds of the formula ##STR1## and various intermediates therefore. The final products possess useful hypotensive activity.
4316906 Mercaptoacyl derivatives of substituted prolines February 23, 1982
New mercaptoacyl derivatives of substituted prolines which have the general formula ##STR1## are useful as hypotensive agents.
4316905 Mercaptoacyl derivatives of various 4-substituted prolines February 23, 1982
This invention is directed to compounds of the formula ##STR1## and various intermediates therefore. The final products possess useful hypotensive activity.
4311697 Derivatives of mercaptoacyl prolines and pipecolic acids January 19, 1982
This invention is directed to compounds of the formula ##STR1## and various intermediates therefore. The final products possess useful hypotensive activity.
4310461 Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids January 12, 1982
Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.
4291040 Mercaptoacyl derivatives of 4-disubstituted prolines and 4-substituted dehydroprolines September 22, 1981
This invention is directed to compounds of the formulas ##STR1## and various intermediates therefore. The final products possess useful hypotensive activity.
4267354 Substituted amides having antiinflammatory activity and intermediates May 12, 1981
Compounds having the formula ##STR1## wherein R.sub.1 is alkoxycarbonyl, amido, alkylamido, or dialkylamido; R'.sub.3 is alkylbenzylamino, dialkylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, or 4-alkyl-1-piperazinyl; A.sub.1 is an alkylene group having 2 to 5 carbon atoms
4252943 Carbamate derivatives of mercaptoacyl hydroxy prolines February 24, 1981
New carbamate derivatives of mercaptoacyl hydroxy prolines which have the general formula ##STR1## are useful as hypotensive agents.
4243804 Heterocyclic containing amines January 6, 1981
Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; R.sub.4 is alkoxy; A.sub.1 is a saturat
4234602 Naphthalenone derivatives and analogs November 18, 1980
Compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or aryl; R.sub.2 is alkylamino, dialkylamino, or a nitrogen containing heterocyclic group; R.sub.3 is hydrogen, halogen, alkyl, alkoxy or trifluoromethyl; A.sub.1 is an alkylene group; and n is 1, 2 or 3, ha
4232027 1,2-Dihydro-2-oxo-4-phenyl-3-quinolinecarbonitrile derivatives November 4, 1980
1,2-Dihydro-2-oxo-4-phenyl-3-quinolinecarbonitrile derivatives are provided having the structure ##STR1## wherein (CH.sub.2).sub.n represents a straight chain alkylene group containing 2 to 5 carbons, and R.sub.1 and R.sub.2 are the same or different and may be hydrogen or lower
4217359 Carbamate derivatives of mercaptoacyl hydroxy prolines August 12, 1980
New carbamate derivatives of mercaptoacyl hydroxy prolines which have the general formula ##STR1## are useful as hypotensive agents.
4216335 Azo methine containing compounds August 5, 1980
Compounds having the formulas ##STR1## wherein R.sub.1 is alkoxycarbonyl, amido, alkylamido, or dialkylamido; R.sub.3 ' is alkylbenzylamino, dialkylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, or 4-alkyl-1-piperazinyl; A.sub.1 is an alkylene group having 2 to 5 carbon ato
4214081 Imino containing morpholine compounds July 22, 1980
Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; R.sub.4 is alkoxy; A.sub.1 is a saturat
4199528 Substituted amides having antiinflammatory activity April 22, 1980
Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; R.sub.4 is alkoxy; A.sub.1 is a saturat
4179558 Naphthalenone derivatives and analogs December 18, 1979
Compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or aryl; R.sub.2 is alkylamino, dialkylamino, or a nitrogen containing heterocyclic group; R.sub.3 is hydrogen, halogen, alkyl, alkoxy or trifluoromethyl; A.sub.1 is an alkylene group; and n is 1, 2 or 3, ha
4174317 3,3-Dichloro-2-azetidinone derivatives November 13, 1979
Compounds having the formula ##STR1## wherein A.sub.1 is an alkylene group having 2 to 4 carbon atoms; R.sub.1 is dialkylamino or a nitrogen containing heterocyclic group and R.sub.2 is phenyl, substituted phenyl, naphthyl, or 1,3-benzodioxol-5-yl; have antiinflammatory activity.
4173634 Basically-substituted tricyclic pyrazoles useful as antiinflammatory agents November 6, 1979
Compounds of the structure ##STR1## are provided, wherein n is 1, 2 or 3, m is 2, 3 or 4, X and Y may be the same or different and are hydrogen, halogen, lower alkyl, lower alkoxy, lower alkylthio or trifluoromethyl, and B is di-lower alkylamino, piperidino, pyrrolidino, morpholi
4166907 3,3-Dichloro-2-azetidinone derivatives having antiinflammatory activity September 4, 1979
Compounds having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 car
4166072 Substituted amides having antiinflammatory activity August 28, 1979
Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkoxycarbonyl, amido or substituted amido; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is an alky
4156079 Substituted amides having antiinflammatory activity May 22, 1979
Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; R.sub.4 is alkoxy; A.sub.1 is a saturat
4151354 Substituted amides and sulfonamides having antiinflammatory activity April 24, 1979
Compounds having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group havi
4145541 3,3-Dichloro-2-azetidinone derivatives having basic substituents March 20, 1979
Compounds having the formula ##STR1## wherein X is oxygen or sulfur; R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 t
4127606 Substituted sulfonamides having antiinflammatory activity November 28, 1978
Compounds having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is sulfonyl; R.sub.3 is alkylamino or dialkylamino; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms
4122255 Substituted amides and sulfonamides containing a heterocyclic group having antiinflammatory acti October 24, 1978
Compounds having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group havi
4118558 2-Aryl-6-arylidene-1-(substituted aminoalkoxy)-1-cyclohexenes October 3, 1978
Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, or 4-alkyl-1-piperazinyl, R.sub.2 and R.sub.3 are hydrogen, chloro, fluoro, alkyl, alkoxy or trifluoromethyl, and A
4115382 3,3-Dichloro-2-azetidinone derivatives having basic substituents September 19, 1978
Compounds having the formula ##STR1## wherein X is oxygen or sulfur; R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene
4098789 Omega-(n-aminoalkoxybenzyl-amino)-(n-hydrocarbonoyl-amino)-alkanoic acid esters July 4, 1978
Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkoxycarbonyl, amido or substituted amido; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; A.sub.1 is an alky
4085280 7-Aminoalkyl-3,7-diaryl-3,3a,4,5,6,7-hexahydro-2H-indazoles April 18, 1978
Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; R.sub.2 and R.sub.3 are the same or different and are hydrogen, chloro, fluoro, alkyl, alkoxy or trifl
4085142 2-Aryl-6-arylidene-1-(substituted aminoalkoxy)-1-cyclohexenes April 18, 1978
Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkylamino or dialkylamino, R.sub.2 and R.sub.3 are hydrogen, chloro, fluoro, alkyl, alkoxy or trifluoromethyl, and A.sub.1 is alkylene have antiinflammatory activity.
4085102 2-Amino-8-arylideno-3,4,5,6,7,8-hexahydro-4-arlypyrido[4,3-d]pyrimidines April 18, 1978
Compounds of the formula ##STR1## and the pharmaceutically acceptable acid-addition salts thereof wherein R.sup.1 and R.sup.2 are hydrogen or alkyl of 1 to 4 carbons; R is hydrogen, alkyl of 1 to 4 carbons, alkanoyl of 2 to 5 carbons, or ##STR2## WHEREIN N IS 1, 2, OR 3; R.su
4078062 Substituted 2H-1,4-benzothiazin-3(4H)-ones March 7, 1978
Compounds of the following formula and their pharmaceutically acceptable salts ##STR1## wherein X and X.sub.1 are independently selected from hydrogen, halogen, lower alkyl, lower alkoxy, trifluoromethyl, nitro, or amino; R is hydrogen, lower alkyl, or ##STR2## wherein m
4065617 2-(2,2,2,-Trifluoroet hyl)-3,3a,4,5,6,7-hexahydro-2H-pyrazolo[4,3-c]pyridines December 27, 1977
Antiinflammatory activity is demonstrated by compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, chloro, fluoro, alkyl, alkoxy or trifluoromethyl and R.sub.2 is hydrogen, alkyl, arylalkyl, hydroxyalkyl, or carboximidamide, or pharmaceutically acceptable salts thereof.
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