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Browse by: INVENTOR PATENT HOLDER PATENT NUMBER DATE
 
 
Inventor:
Neustadt; Bernard R.
Address:
West Orange, NJ
No. of patents:
66
Patents:


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Patent Number Title Of Patent Date Issued
8114879 Piperazine derivatives useful as CCR5 antagonists February 14, 2012
The use of CCR5 antagonists of the formula ##STR00001## or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R.sup.1 is hydrogen or alkyl; R.sup.2 is substituted phenyl, substituted heteroaryl, naphthyl fluore
7790474 p53 modulators September 7, 2010
The present invention provides compositions as well as methods for identifying compositions useful for treating or preventing cancer.
7741318 Pyrazolo [1,5-A]pyrimidine adenosine A.sub.2a receptor antagonists June 22, 2010
Compounds having the structural formula I ##STR00001## are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is --C(O)-- or --S(O).sub.2--; R.sup.1 is alkyl or cycloalkyl; R.sup.2 is hydrogen, halo or --CN; R.sup.3 is hydrogen or
7709492 Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A.sub.2a receptor antagonists May 4, 2010
Compounds having the structural formula I ##STR00001## or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or pyrrolyl, or cycloalkenyl R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are H,
7465740 2-heteroaryl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonis December 16, 2008
Compounds having the structural formula I ##STR00001## or a pharmaceutically acceptable salt thereof, wherein R is R.sup.1-isoxazolyl, R.sup.1-oxadiazolyl, R.sup.1-dihydrofuranyl, R.sup.1-pyrazolyl, R.sup.1-imidazolyl, R.sup.1-pyrazinyl or R.sup.1-pyrimidinyl; R.sup.1 is 1, 2 or 3
7384944 Piperazine derivatives useful as CCR5 antagonists June 10, 2008
The use of CCR5 antagonists of the formula ##STR00001## or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R.sup.1 is hydrogen or alkyl; R.sup.2 is substituted phenyl, substituted heteroaryl, naphthyl, fluore
7368449 2-alkynyl- and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A.sub. May 6, 2008
Compounds having the structural formula I ##STR00001## or a pharmaceutically acceptable salt thereof, wherein R is ##STR00002## R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are H, alkyl or alkoxyalkyl; R.sup.6 is H, alkyl, hydroxyalkyl or --CH.sub.2F; R.sup.7, R.sup.8 and R.s
7067655 Adenosine A2a receptor antagonists June 27, 2006
Compounds having the structural formula I ##STR00001## or a pharmaceutically acceptable salt thereof, whereinR is optionally substituted phenyl, cycloalkenyl, or heteroaryl;X is alkylene or --C(O)CH.sub.2--;Y is --N(R.sup.2)CH.sub.2CH.sub.2N(R.sup.3)--, --OCH.sub.2CH.sub.2N(R.sup.2)
7041666 Adenosine A2a receptor antagonists May 9, 2006
Disclosed are compounds having the structural formula ##STR00001## or pharmaceutically acceptable salts or solvates thereof, wherein R is optionally substituted heteroaryl, optionally substituted phenyl, cycloalkenyl, --C(.dbd.CH.sub.2)CH.sub.3, --C.ident.C--CH.sub.3, ##STR00002#
6897217 2-Alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a recepto May 24, 2005
Compounds having the structural formula I ##STR1##or a pharmaceutically acceptable salt thereof, wherein R is ##STR2## R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are H, alkyl or alkoxyalkyl; R.sup.6 is H, alkyl, hydroxyalkyl or --CH.sub.2 F; R.sup.7, R.sup.8 and R.sup.9 are H
6897216 Adenosine A2a receptor antagonists May 24, 2005
Compounds having the structural formula I ##STR1##or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or --C(O)CH.sub.2 --; Y is --N(R.sup.2)CH.sub.2 CH.sub.2 N(R.sup.3)--, --OCH.sub.2 CH.sub.2 N(R.sup
6875772 [1,2,4]-Triazole bicyclic adeonsine A2a receptor antagonists April 5, 2005
Compounds having the structural formula I ##STR1##wherein: n is 0, 1, 2 or 3; A is C(R.sup.1) or N; R.sup.1 and R.sup.1a are H, (C.sub.1 -C.sub.6)-alkyl, halo, CN or --CF.sub.3 ; X is --C(O)--, --O--, --SO.sub.0-2 --, or optionally substituted methylene, imino, arylene or het
6689765 Piperazine derivatives useful as CCR5 antagonists February 10, 2004
The use of CCR5 antagonists of the formula ##STR1##or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R.sup.1 is hydrogen or alkyl; R.sup.2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, di
6630475 Adenosine A2a receptor antagonists October 7, 2003
Compounds having the structural formula I ##STR1##or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or --C(O)CH.sub.2 --; Y is --N(R.sup.2)CH.sub.2 CH.sub.2 N(R).sup.3)--, --OCH.sub.2 CH.sub.2 N(R.su
6602885 Piperidine derivatives useful as CCR5 antagonists August 5, 2003
The use of CCR5 antagonists of the formula ##STR1##or a pharmaceutically acceptable salt thereof, wherein ##STR2## R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R.sup.1 is H, alkyl or alkenyl; R.sup.2 is optionally substituted phenyl, phenylalkyl, heteroaryl o
6391865 Piperazine derivatives useful as CCR5 antagonists May 21, 2002
The use of CCR5 antagonists of the formula ##STR1##or a pharmaceutically acceptable salt thereof, whereinR is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl
6387930 Piperidine derivatives useful as CCR5 antagonists May 14, 2002
The use of CCR5 antagonists of the formula ##STR1##or a pharmaceutically acceptable salt thereof, whereinX is --C(R.sup.13).sub.2 --, --C(R.sup.13)(R.sup.19)--, --C(O)--, --O--, --NH--, --N(alkyl)--, ##STR2##R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl;R.sup.1 is H
6329395 Neuropeptide Y5 receptor antagonists December 11, 2001
Compounds of the formula I ##STR1##or a pharmaceutically acceptable salt thereof, whereina and b are 0-2, provided that the sum is 0-3; ##STR2##X is --O--, --S--, --SO--, --SO.sub.2 --, --CH(OR.sup.8)--, --C(O)--, --C(R.sup.23).sub.2 --, optionally substituted alkenyl, alkynyl or; ##
6228985 Derivatives of aminobenzoic and aminobiphenylcarboxylic acids useful as anti-cancer agents May 8, 2001
The present invention provides compounds having the formula: ##STR1##wherein n is 0 or 1;R is --NH.sub.2 or ##STR2##wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, carboxy, carboxyalkyl, and carbamoyl;Q is R.sup.3
6204282 Benzimidazole compounds that are vitronectin receptor antagonists March 20, 2001
The present invention provides compounds having the formula ##STR1##wherein n, p, q and r are each independently selected from 0 or 1;a, b, c, and d each independently represents a carbon or nitrogen atom, with the proviso that no more than two of a, b, c, and d are nitrogen atoms;Y and
5407960 Mercaptocycloacyl aminoacid endopeptidase inhibitors April 18, 1995
Mercaptocycloacyl aminoacid inhibitors of endopeptidase of the formula ##STR1## or a pharmaceutically acceptable salt thereof, alone or in combination with an ACE inhibitor or an ANF, in the treatment of cardiovascular disorders such as hypertension, congestive heart failure, edema a
5393755 Polycyclic guanine derivatives February 28, 1995
Novel polycylic guanine derivatives of the formula: ##STR1## wherein J is oxygen or sulfur, R.sup.1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy;R.sup.2 is hydrogen, aryl, heteroaryl, cycloalkyl, alkyl or alkyl substituted with aryl, heteroaryl, hydroxy, alkoxy, amino
5389610 Carboxyalkylcarbonyl aminoacid endopeptidase inhibitors February 14, 1995
Carboxyalkylcarbonyl aminoacid inhibitors of endopeptidases of the formula: ##STR1## or pharmaceutically acceptable salt thereof, wherein R.sup.1 is H, alkyl, arylalkyl, aryl or aryloxyalkyl; R.sup.2 is alkyl, alkenyl, alkynyl, alkoxy or alkylthio, wherein the alkyl portion is substi
5356925 N-(mercaptoalkyl)ureas and carbamates October 18, 1994
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 inde
5348944 Carboxyalkyl dipeptides September 20, 1994
Compounds of the formula ##STR1## useful as antihypertensive agents are disclosed.
5298492 Diamino acid derivatives as antihypertensives March 29, 1994
Novel diamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of the formula ##STR1## wherein: Z is amino, lower alkylamino, di-(lower alkyl)amino R.sup.9 C(O)NH-- or an optionally substituted guanidino group;R.sup.1 is hydrogen or R.sup.7 R
5262436 Acylamino acid antihypertensives in the treatment of congestive heart failure November 16, 1993
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.
5232920 N-(mercaptoalkyl)amides August 3, 1993
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
5219886 Mercapto-acylamino acids June 15, 1993
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, ary
5208236 N-(acylaminomethyl)glutaryl amino acids and use May 4, 1993
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
5173506 N-(mercaptoalkyl)ureas and carbamates December 22, 1992
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 ind
5075302 Mercaptoacyl aminolactam endopeptidase inhibitors December 24, 1991
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
5061710 Mercapto-acylamino acid antihypertensives October 29, 1991
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.
5017567 Carboxyalkyl dipeptides as antiglaucoma agents May 21, 1991
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 quinazolin
4929641 Mercapto-acylamino acid antihypertensives May 29, 1990
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.
4906635 Carboxyalkyl dipeptides as antiglaucoma agents March 6, 1990
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 quinazolin
4879309 Mercapto-acylamino acids as antihypertensives November 7, 1989
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 co
4840772 Antiglaucoma compositions and methods June 20, 1989
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 treat
4831157 Preparation of angiotensin-converting enzyme inhibitors May 16, 1989
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 proce
4818749 Carboxyalkyl dipeptides and medical use thereof in treating hypertension and congestive heart fa April 4, 1989
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
4808573 Carboxyalkyl dipeptides and anti-hypertensive use thereof February 28, 1989
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
4801609 Mercapto-acylamino acid antihypertensives January 31, 1989
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.
4783444 Antiglaucoma compositions and methods November 8, 1988
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 treat
4778795 Carboxyalkyl dipeptides as antiglaucoma agents October 18, 1988
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 quinazolin
4691049 Process for preparing a specific diastereomer of a monoamino dicarboxylic acid ester September 1, 1987
(Benzothiadiazine, benzamido and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds are disclosed. Compounds of this invention are useful as antihypertensive agents.
4616012 Carboxyalkyl dipeptides as antiglaucoma agents October 7, 1986
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 quinazolin
4587258 Angiotensin-converting enzyme inhibitors May 6, 1986
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.
4584285 Antihypertensive agents April 22, 1986
(Benzothiadiazine, benzamido and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds are disclosed. Compounds of this invention are useful as antihypertensive agents.
4559340 Antihypertensive agents December 17, 1985
There are disclosed benzothiadiazinyl and quinazolinyl substituted carboxylalkyl dipeptides, wherein the benzothiodiazinyl or quinazolinyl portions are joined to the dipeptide portions by an aminocarbonyl group. Compounds of this invention are useful as antihypertensive agents, in the
4511569 Tricyclic lactams and derivatives useful in increasing cardiac contractility April 16, 1985
Disclosed are 5,6-dihydro benzo[f]quinolines and derivatives which are effective in increasing cardiac contractility. These compounds are useful in the treatment of congestive heart failure.
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