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Bruce E. Tomczuk Patents |
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Inventor: Tomczuk; Bruce E.
Address: Collegeville, PA
No. of patents: 42
Patents:
| Patent Number |
Title Of Patent |
Date Issued |
| 7241789 |
Substituted indoles and their use as integrin antagonists |
July 10, 2007 |
| The present invention relates to novel substituted indole compounds that are antagonists of alpha V (.alpha.v) integrins, for example .alpha..sub.v.beta..sub.3 and .alpha..sub.v.beta..sub.5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. T |
| 7029654 |
Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors |
April 18, 2006 |
| Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR00001## wherein X is O or NR.sup.9 and Het, R.sup.1, R.sup.7, R.sup.8, R.sup.12--R.sup.15, R.sup.a, R.sup.b, R.sup.c, Z, and n are set forth in the specification, as well as hyd |
| 6900231 |
Aminopyridyl-substituted phenyl acetamides as protease inhibitors |
May 31, 2005 |
| Phenyl acetamide compounds are described, including compounds of ##STR1##or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R.sup.3 -R.sup.6, R.sup.11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases |
| 6872730 |
Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin an |
March 29, 2005 |
| The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (.alpha.v) integrins, for example .alpha..sub.v.beta..sub.3 and .alpha..sub.v.beta..sub.5 integrins, their pharmaceutically acceptable salts, and pharmaceutica |
| 6855722 |
Substituted indoles and their use as integrin antagonists |
February 15, 2005 |
| The present invention relates to novel substituted indole compounds that are antagonists of alpha V (.alpha.v) integrins, for example .alpha..sub.v.beta..sub.3 and .alpha..sub.v.beta..sub.5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. T |
| 6730783 |
Process for preparing aminoguanidines and alkoxyguanidines as protease inhibitors |
May 4, 2004 |
| Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1##wherein X is O or NR.sup.9 and R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, R.sup.11, R.sup.12, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates |
| 6706765 |
Aminoguanidines and alkoxyguanidines as protease inhibitors |
March 16, 2004 |
| Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1##wherein X is O or NR.sup.9 and R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, R.sup.11, R.sup.12, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates |
| 6706021 |
Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors |
March 16, 2004 |
| Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1##wherein X is O or NR.sup.9 and Het, R.sup.1, R.sup.7, R.sup.8, R.sup.12 -R.sup.15, R.sup.a, R.sup.b, R.sup.c, Z, and n are set forth in the specification, as well as hydrates, |
| 6638931 |
Aminoguanidines and alkoxyguanidines as protease inhibitors |
October 28, 2003 |
| Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1##wherein X is O or NR.sup.9 and R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, R.sup.11, R.sup.12, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates |
| 6566379 |
Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors |
May 20, 2003 |
| Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1##wherein X is O or NR.sup.9 and Het, R.sup.1, R.sup.7, R.sup.8, R.sup.12 -R.sup.15, R.sup.a, R.sup.b, R.sup.c, Z, and n are set forth in the specification, as well as hydrates, |
| 6521663 |
Aminoguanidinyl- and Alkoxyguanidinyl-substituted phenyl acetamides as protease inhibitors |
February 18, 2003 |
| Phenyl acetamide compounds are described, including compounds of Formula I: ##STR1##or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R.sup.3 -R.sup.6, R.sup.11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors o |
| 6518310 |
Aminoguanidines and alkoxyguanidines as protease inhibitors |
February 11, 2003 |
| Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1##wherein X is O or NR.sup.9 and R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, R.sup.11, R.sup.12, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates |
| 6514978 |
Thromboresistant materials incorporating pyrazinone protease inhibitors |
February 4, 2003 |
| Thromboresistant materials are described which incorporate pyrazinone compounds of the Formula I: ##STR1##wherein X is O, NR.sup.11 or CH.dbd.N, R.sup.3 -R.sup.11, R.sup.a, R.sup.b, R.sup.c, W, m, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutic |
| 6472399 |
Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors |
October 29, 2002 |
| Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1##wherein X is O or NR.sup.9 and Het, R.sup.1, R.sup.7, R.sup.8, R.sup.12 -R.sup.15, R.sup.a, R.sup.b, R.sup.c, Z, and n are set forth in the specification, as well as hydrates, |
| 6420397 |
Heteroaryl protease inhibitors and diagnostic imaging agents |
July 16, 2002 |
| Ketothiazole alkoxyguanidine and aminoguanidine analogs are described, including compounds of the Formula I: ##STR1##wherein X is O or NR.sup.9 and Het, A, R.sup.1, R.sup.7, R.sup.8, R.sup.12, R.sup.13, R.sup.a, R.sup.b, R.sup.c, Z, m and n are set forth in the specification, as well |
| 6417161 |
Amino acid amidinohydrazones, alkoxyguanidines and aminoguanidines as protease inhibitors |
July 9, 2002 |
| The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: ##STR1##wherein X is O or NR.sup.19 and A.sup.1, A.sup.2, R.sup.7 -R.sup.10, R.sup.18, R.sup.a, R.sup.b, R.sup.c, n and m are set forth in the specification, as well a |
| 6414020 |
Amidino protease inhibitors |
July 2, 2002 |
| Amidino and benzamidino compounds, including compounds of the formula: ##STR1##wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic en |
| 6350764 |
Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors |
February 26, 2002 |
| Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1##wherein X is O or NR.sup.9 and Het, R.sup.1, R.sup.7, R.sup.8, R.sup.12 -R.sup.15, R.sup.a, R.sup.b, R.sup.c, Z, and n are set forth in the specification, as well as hydrates, |
| 6344486 |
Benzamide and sulfonamide substituted aminoguanidines and alkoxyguanidines as protease inhibitor |
February 5, 2002 |
| The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: ##STR1##wherein X is O or NH, L is --O-- or --SO.sub.2 --, and R.sup.1 -R.sup.4, R.sup.9 -R.sup.19, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the speci |
| 6344484 |
Tyrosine alkoxyguanidines as integrin inhibitors |
February 5, 2002 |
| The present invention relates to novel tyrosine alkoxyguanidine compounds that are inhibitors of alpha V (.alpha.v) integrins, for example .alpha.v.beta.3 and .alpha.v.beta.5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds ma |
| 6344466 |
Benzamide and sulfonamide substitued aminoguanidines and alkoxyguanidines as protease inhibitors |
February 5, 2002 |
| The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: ##STR1##wherein X is O or NH, L is --O-- or --SO.sub.2 --, and R.sup.1 -R.sup.4, R.sup.9 -R.sup.19, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the speci |
| 6326492 |
Heterocyclic protease inhibitors |
December 4, 2001 |
| Described are compounds of the Formula VII: ##STR1##wherein Het, R.sup.1, R.sup.7 and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for pr |
| 6281206 |
Amidino protease inhibitors |
August 28, 2001 |
| Amidino and benzamidino compounds, including compounds of the formula: ##STR1##wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic en |
| 6245763 |
Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors |
June 12, 2001 |
| Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1##wherein X is O or NR.sup.9 and Het, R.sup.1, R.sup.7, R.sup.8, R.sup.12 -R.sup.15, R.sup.a, R.sup.b, R.sup.c, Z, and n are set forth in the specification, as well as hydrates, |
| 6235778 |
Aminoguanidines and alkoxyguanidines as protease inhibitors |
May 22, 2001 |
| Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1##wherein X is O or NR.sup.9 and R.sup.1 14 R.sup.4, R.sup.6 -R.sup.9, R.sup.11, R.sup.12, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates |
| 6225302 |
Amidino protease inhibitors |
May 1, 2001 |
| Amidino and benzamidino compounds, including compounds of the formula: ##STR1##wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic en |
| 6204263 |
Pyrazinone protease inhibitors |
March 20, 2001 |
| Pyrazinone compounds are described, including compounds of the Formula I: ##STR1##wherein X is O, NR.sup.11 or CH.dbd.N, R.sup.3 -R.sup.11, R.sup.a, R.sup.b, R.sup.c, W, m, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereo |
| 6133315 |
Amidino protease inhibitors |
October 17, 2000 |
| Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolyt |
| 6037356 |
Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors |
March 14, 2000 |
| Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1## wherein X is O or NR.sup.9 and Het, R.sup.1, R.sup.7, R.sup.8, R.sup.12 -R.sup.15, R.sup.a, R.sup.b, R.sup.c, Z, and n are set forth in the specification, as well as hydra |
| 6034127 |
Amidino protease inhibitors |
March 7, 2000 |
| Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolyt |
| 5891909 |
Amidinohydrazones as protease inhibitors |
April 6, 1999 |
| Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes s |
| 5792769 |
Guanidino protease inhibitors |
August 11, 1998 |
| Compounds of the formula: ##STR1## wherein R.sup.1 --R.sup.4, R.sup.7 --R.sup.8, R.sup.a, R.sup.b, R.sup.c, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes a |
| 5741819 |
Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors |
April 21, 1998 |
| The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: ##STR1## |
| 5618844 |
Hydroxamic acid and carboxylic acid derivatives, process for their preparation and use thereof |
April 8, 1997 |
| This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of |
| 5514716 |
Hydroxamic acid and carboxylic acid derivatives, process for their preparation and use thereof |
May 7, 1996 |
| This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of |
| 5114944 |
2-phenylpyrazolo[1,5-a]pyrimidine-3-acetic acid derivatives exhibiting therapeutic effects |
May 19, 1992 |
| This invention provides a 2-arylpyrazolo[1,5-a]pyrimidine-3-acetic acid corresponding to the formula: ##STR1## where X is hydrogen or a halogen, hydroxy, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy substituent; Y is hydrogen or a halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 - |
| 5057534 |
3-amino-5-arylpyrazole-4-acetic acid derivatives exhibiting therapeutic effects |
October 15, 1991 |
| This invention provides novel pyrazole-4-acetic acid derivatives which have utility as therapeutic agents which exhibit anxiolytic, anticonvulsant and muscle relaxant effects in warm blooded animals.Illustrative of an invention compound is 3-(dimethylamino)-5-(4-methylphenyl)-1H-pyrazole |
| 4948800 |
Pharmaceutical method using fused imidazoheterocyclic compounds |
August 14, 1990 |
| Imidazoheterocyclic compounds having the formula: ##STR1## wherein the A ring is pyridine in any of its four positions; B is carbonyl, thioxomethyl or hydroxymethylene; Z is hydrogen, halogen, loweralkyl, hydroxy, loweralkoxy, diloweralkylamino or nitro; Ar is phenyl, pyrido, thi |
| 4914109 |
Method of treating animals using fused imidazoheterocyclic compounds |
April 3, 1990 |
| Imidazoheterocyclic compounds having the formula: ##STR1## wherein the A ring is pyridine in any of its four positions; B is carbonyl, thioxomethyl or hydroxymethylene; Z is hydrogen, halogen, loweralkyl, hydroxy, loweralkoxy, diloweralkylamino or nitro; Ar is phenyl, pyrido, thi |
| 4873251 |
Method of treating animals using fused imidazoheterocyclic compounds |
October 10, 1989 |
| Imidazoheterocyclic compounds having the formula: ##STR1## wherein the A ring is pyridine in any of its four positions; B is carbonyl, thioxomethyl or hydroxymethylene; Z is hydrogen, halogen, loweralkyl, hydroxy, loweralkoxy, di-loweralkylamino or nitro; Ar is phenyl, pyrido, th |
| 4824951 |
Fused imidazopyridine compounds |
April 25, 1989 |
| Imidazoheterocyclic compounds having the formula: ##STR1## wherein the A ring is pyridine in any of its four positions; B is carbonyl, thioxomethyl or hydroxymethylene; Z is hydrogen, halogen, loweralkyl, hydroxy, loweralkoxy, diloweralkylamino or nitro; Ar is phenyl, pyrido, thi |
| 4772600 |
Fused imidazoheterocyclic compounds and pharmaceutical compositions |
September 20, 1988 |
| Imidazoheterocyclic compounds having the formula: ##STR1## wherein the A ring is pyridine in any of its four positions; B is carbonyl, thioxomethyl or hydroxymethylene; Z is hydrogen, halogen, loweralkyl, hydroxy, loweralkoxy, diloweralkylamino or nitro; Ar is phenyl, pyrido, thi |
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