Patents by Inventor Bernard R. Neustadt

Bernard R. Neustadt has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5262436
    Abstract: Mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
    Type: Grant
    Filed: August 6, 1991
    Date of Patent: November 16, 1993
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 5232920
    Abstract: Novel N-(mercaptoalkyl)amides of the formula ##STR1## wherein R.sub.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sub.2 is (COR.sub.3)-aryl, heteroaryl, substituted (COR.sub.3)-aryl or substituted heteroaryl, wherein the substituents are 1-3 substituents selected from the group consisting of carboxy, alkoxycarbonyl, lower alkyl, hydroxy, halo, lower alkoxy, cyclolower alkyl, cyano, trifluoromethyl, phenyl, phenoxy and phenylthio;R.sub.3 is --OR.sub.4 or --NR.sub.4 R.sub.5 ;R.sub.4 and R.sub.5 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sub.4 and R.sub.5 together with the nitrogen to which they are attached form a 5-, 6- or 7-membered ring;Q is hydrogen or R.sub.6 CO--;R.sub.
    Type: Grant
    Filed: December 21, 1990
    Date of Patent: August 3, 1993
    Assignee: Schering Corporation
    Inventor: Bernard R. Neustadt
  • Patent number: 5219886
    Abstract: Novel mercapto-acylamino acids of the formula ##STR1## wherein Q is hydrogen or R.sup.7 CO--;R.sup.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen; lower alkyl; cyclolower alkyl; lower alkyl substituted with hydroxy, lower alkoxy, mercapto, lower alkylthio, aryl or heteroaryl; aryl; or heteroaryl;R.sup.3 is --OR.sup.5 or --NR.sup.5 R.sup.6 ;R.sup.4 and R.sup.9 are independently --(CH.sub.2).sub.q R.sup.8, provided that when R.sup.4 and R.sup.9 are both hydrogen, R.sup.2 is biphenylyl, phenoxyphenyl, phenylthiophenyl, naphthyl, heteroaryl, or lower alkyl substituted with hydroxy, lower alkoxy, mercapto or lower alkylthio;R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sup.5 and R.sup.6 together with the nitrogen to which they are attached form a 5-7 membered ring;R.sup.7 is hydrogen, lower alkyl or aryl;R.sup.
    Type: Grant
    Filed: October 1, 1991
    Date of Patent: June 15, 1993
    Assignee: Schering Corporation
    Inventors: Elizabeth M. Smith, Philip M. DeCapite, Bernard R. Neustadt
  • Patent number: 5208236
    Abstract: Novel glutarylamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of the formula ##STR1## wherein: R.sup.1 and R.sup.3 are independently hydroxy, lower alkoxy, aryllower alkoxy, amino, lower alkylamino and di-(lower alkyl)amino;R.sup.2 is H or hydroxy;R.sup.4 is aryl, substituted aryl, heteroaryl or substituted heteroaryl;R.sup.6 is H or R.sup.7 --(CH.sub.2).sub.3 --, wherein R.sup.7 is amino or (aryllower alkoxy)carbonylamino;Q is --C(O)-- or --SO.sub.2 --;Y is lower alkyl, lower alkoxy, aryllower alkoxy, amino, lower alkylamino, di-(lower alkyl)amino, or a group of the formula ##STR2## wherein A is a bond, --N(R.sup.5)--, or --O--; and R.sup.5 is H or lower alkyl;B is H or Z--(CH.sub.2).sub.m --Z is amino, lower alkylamino, di-(lower alkyl)amino, (aryllower alkoxy)carbonylamino, 1-pyrrolidino or 1-piperidino;m=1,2,3,4 or 5; and n=1,2 or 3; oror a pharmaceutically acceptable addition salt thereof; useful in the treatment of cardiovascular disorders, are disclosed.
    Type: Grant
    Filed: September 23, 1992
    Date of Patent: May 4, 1993
    Assignee: Schering Corporation
    Inventor: Bernard R. Neustadt
  • Patent number: 5173506
    Abstract: Novel N-(mercaptoalkyl)urea or carbamates of the formulae I and II ##STR1## wherein A is a monocyclic or bicyclic arylene or heteroarylene;Q is hydrogen or R.sub.9 CO--;Y is --O--, --S-- or --NR.sub.8 --;R.sub.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sub.2 and R.sub.8 are independently hydrogen; lower alkyl; cyclolower alkyl; lower alkyl substituted with hydroxy, lower alkoxy, mercapto, lower alkylthio, aryl or heteroaryl; aryl; or heteroaryl;R.sub.3 is --OR.sub.5 or --NR.sub.5 R.sub.6 ;R.sub.4 is --(CH.sub.2).sub.q R.sub.7 ; or R.sub.2 and R.sub.4 and the carbons to which they are attached complete a 5-, 6- or 7-membered carbocyclic ring;R.sub.5 and R.sub.6 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached form a 5-, 6- or 7-membered ring;R.sub.
    Type: Grant
    Filed: August 16, 1990
    Date of Patent: December 22, 1992
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, Alan Bronnenkant
  • Patent number: 5075302
    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.
    Type: Grant
    Filed: March 9, 1990
    Date of Patent: December 24, 1991
    Assignee: Schering Corporation
    Inventor: Bernard R. Neustadt
  • Patent number: 5061710
    Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
    Type: Grant
    Filed: December 16, 1987
    Date of Patent: October 29, 1991
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 5017567
    Abstract: Methods and pharmaceutical compositions are disclosed for reducing intraocular pressure. The methods and compositions employ an active ingredient which comprises certain benzothiadiazinyl and quinazolinyl substituted carboxyalkyl dipeptides wherein the benzothiadiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group.
    Type: Grant
    Filed: January 3, 1990
    Date of Patent: May 21, 1991
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, David R. Andrews, Paul E. McNamara, Robert W. Watkins
  • Patent number: 4929641
    Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
    Type: Grant
    Filed: May 11, 1988
    Date of Patent: May 29, 1990
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 4906635
    Abstract: Methods and pharmaceutical compositions are disclosed for reducing intraocular pressure. The methods and compositions employ an active ingredient which comprises certain benzothiadiazinyl and quinazolinyl substituted carboxyalkyl dipeptides wherein the benzothiadiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group.
    Type: Grant
    Filed: July 18, 1988
    Date of Patent: March 6, 1990
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, David R. Andrews, Paul E. McNamara, Robert W. Watkins
  • Patent number: 4879309
    Abstract: Novel mercapto-acylamino acids useful as analgesic, as well as in the treatment of hypertension and congestive heart failure and combinations of mercapto acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension and congestive heart failure are disclosed.
    Type: Grant
    Filed: January 30, 1989
    Date of Patent: November 7, 1989
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Bernard R. Neustadt
  • Patent number: 4840772
    Abstract: The present invention relates to ophthalmological pharmaceutical compositions comprising (benzothiadiazine, benzamide and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds and to methods for using said composition in reducing intraocular pressure, e.g., in the treatment of glaucoma.
    Type: Grant
    Filed: August 3, 1988
    Date of Patent: June 20, 1989
    Assignee: Schering Corporation
    Inventors: Robert Watkins, Ronald J. Doll, Bernard R. Neustadt, Elizabeth M. Smith, Charles V. Magatti, Elijah H. Gold
  • Patent number: 4831157
    Abstract: Novel compounds with angiotensin-converting enzyme inhibitory activity are disclosed. Such compounds are useful in the treatment of cardiovascular disorders, especially hypertension and congestive heart failure, and are useful in the treatment of glaucoma. Also disclosed is a novel process for preparing intermediates useful in the preparation of the claimed compounds.
    Type: Grant
    Filed: September 28, 1988
    Date of Patent: May 16, 1989
    Assignee: Schering Corporation
    Inventors: Elijah H. Gold, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 4818749
    Abstract: The present invention relates to carboxyalkyl dipeptides which are inhibitors of angiotensin-converting enzyme and are useful as antihypertensive agents and in the treatment of congestive heart failure.The compounds of the present invention are compounds of the formulae ##STR1## and the pharmaceutically acceptable salts thereof, wherein R and R.sup.6 are the same or different and are hydroxy or lower alkoxy;R.sup.1 is benzyloxylower alkyl or benzylthiolower alkyl;R.sup.2 is benzylthiomethyl, 2-phyenylethylthiomethyl, napthylmethylthiomethyl, methylbenzylthiomethyl, 2-(carboxyphenyl)ethyl or 2-(alkoxycarbonylphenyl)ethyl) andR.sup.3 is hydrogen, lower alkyl or aminolower alkyl.
    Type: Grant
    Filed: November 4, 1987
    Date of Patent: April 4, 1989
    Assignee: Schering Corporation
    Inventors: Elijah H. Gold, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 4808573
    Abstract: The present invention relates to carboxyalkyl dipeptides which are inhibitors of angiotensin-converting enzyme and are useful as antihypertensive agents and in the treatment of congestive heart failure.The compounds of the present invention are compounds of the formulae ##STR1## and the pharmaceutically acceptable salts thereof, wherein R and R.sup.6 are the same or different and are hydroxy or lower alkoxy;R.sup.1 is benzyloxylower alkyl or benzylthiolower alkyl;R.sup.2 is benzylthiomethyl, 2-phenylethylthiomethyl, naphthylmethylthiomethyl, methylbenzylthiomethyl; 2-(carboxyphenyl)ethyl or 2-(alkoxycarbonylphenyl)ethyl; andR.sup.3 is hydrogen, lower alkyl or aminolower alkyl.
    Type: Grant
    Filed: March 23, 1987
    Date of Patent: February 28, 1989
    Assignee: Schering Corporation
    Inventors: Elijah H. Gold, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 4801609
    Abstract: Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic peptides useful for treating hypertension are disclosed.
    Type: Grant
    Filed: March 27, 1987
    Date of Patent: January 31, 1989
    Assignee: Schering Corporation
    Inventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
  • Patent number: 4783444
    Abstract: The present invention relates to ophthalmological pharmaceutical compositions comprising (benzothiadiazine, benzamide and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds and to methods for using said composition in reducing intraocular pressure, e.g., in the treatment of glaucoma.
    Type: Grant
    Filed: April 4, 1986
    Date of Patent: November 8, 1988
    Assignee: Schering Corporation
    Inventors: Robert Watkins, Ronald J. Doll, Bernard R. Neustadt, Elizabeth M. Smith, Charles V. Magatti, Elijah H. Gold
  • Patent number: 4778795
    Abstract: Methods and pharmaceutical compositions are disclosed for reducing intraocular pressure. The methods and compositions employ an active ingredient which comprises certain benzothiadiazinyl and quinazolinyl substituted carboxyalkyl dipeptides wherein the benzothiadiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group.
    Type: Grant
    Filed: September 3, 1986
    Date of Patent: October 18, 1988
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, David R. Andrews, Paul E. McNamara, Robert W. Watkins
  • Patent number: 4691049
    Abstract: (Benzothiadiazine, benzamido and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds are disclosed. Compounds of this invention are useful as antihypertensive agents.
    Type: Grant
    Filed: February 20, 1986
    Date of Patent: September 1, 1987
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Bernard R. Neustadt, Elizabeth M. Smith, Charles V. Magatti, Elijah H. Gold
  • Patent number: 4616012
    Abstract: Methods and pharmaceutical compositions are disclosed for reducing intraocular pressure. The methods and compositions employ an active ingredient which comprises certain benzothiadiazinyl and quinazolinyl substituted carboxyalkyl dipeptides wherein the benzothiadiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group.
    Type: Grant
    Filed: November 12, 1985
    Date of Patent: October 7, 1986
    Assignee: Schering Corporation
    Inventors: Bernard R. Neustadt, David R. Andrews, Paul E. McNamara, Robert W. Watkins