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Patent No. 5076029

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Assignee: 3-Dimensional Pharmaceuticals, Inc.


Location: Exton, PA
No. of patents: 66

1    
NumberTitleIssue Date
7482376Conjugated complement cascade inhibitors
The present invention is directed to conjugated complement cascade inhibitors, and a method of treating a patient using a conjugated complement cascade inhibitor. ...
01/27/2009
7429603C-fms kinase inhibitors
The invention is directed to compounds of Formulae I, II and III: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomer...
09/30/2008
7138374Methods of using analogs of human basic fibroblast growth factor mutated at one or more of the positions glutamate 89, asparate 101 or leucine 137
The present invention relates to novel muteins of human basic fibroblast growth factor with superagonist properties. Both protein and the respective encoding nucleic acid species are disclosed. The invention also embodies vectors and host cells for the propagation o...
11/21/2006
7060706Quinazolinones
Quinazolinones of formula (I) in which R, R1, R2, R3, R4, Y, n and m have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists ...
06/13/2006
6962942Azacycloalkanone serine protease inhibitors
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 having F...
11/08/2005
6900231Aminopyridyl-substituted phenyl acetamides as protease inhibitors
Phenyl acetamide compounds are described, including compounds of or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the s...
05/31/2005
6890930Quinazolinones
Quinazolinones of formula (I) in which R, R1, R2, R3, R4, Y, Z, and m have the meaning indicated in patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists. ...
05/10/2005
6872730Substituted benzofurans and benzothiophenes, methods of making and methods of use as integrin antagonists
The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts...
03/29/2005
6767722Analogs of human basic fibroblast growth factor mutated at one or more of the positions glutamate 89, Aspartate 101 or Leucine 137
The present invention relates to muteins of human basic fibroblast growth factor with superagonist properties. Both protein and the respective encoding nucleic acid species are disclosed. The invention also embodies vectors and host cells for the propagation of said...
07/27/2004
6737404Methods of using analogs of human basic fibroblast growth factor mutated at one or more of the positions glutamate 89, aspartate 101 or leucine 137
The present invention relates to novel muteins of human basic fibroblast growth factor with superagonist properties. Both protein and the respective encoding nucleic acid species are disclosed. The invention also embodies vectors and host cells for the propagation o...
05/18/2004
6730783Process for preparing aminoguanidines and alkoxyguanidines as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra
05/04/2004
6706021Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, R
03/16/2004
6706765Aminoguanidines and alkoxyguanidines as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra
03/16/2004
6638931Aminoguanidines and alkoxyguanidines as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1## wherein X is O or NR9 and R1 -R4, R6 -R9, R11, R12, Ra, Rb, R
10/28/2003
6586453Substituted thiazoles and the use thereof as inhibitors of plasminogen activator inhibitor-1
The present invention relates to the use of aminothiazole derivatives of Formula I of as inhibitors of PAI-1, and to novel classes of aminothiazole derivatives, their synthesis and their use as inhibitors of PAI-1. It has been discovered that compounds of...
07/01/2003
6571227Method, system and computer program product for non-linear mapping of multi-dimensional data
A method, system and computer program product for scaling, or dimensionally reducing, multi-dimensional data sets, that scales well for large data sets. The invention scales multi-dimensional data sets by determining one or more non-linear functions betwe...
05/27/2003
6566379Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1## wherein X is O or NR9 and Het, R1, R7, R8, R12 -R15, Ra, Rb
05/20/2003
6562840Heteroaryl amidines, methylamidines and guanidines, and the use thereof as protease inhibitors
The present invention is directed to compounds of Formula I: ##STR1## wherein X is O, S or NR7 and R1 --R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts the...
05/13/2003
6521663Aminoguanidinyl- and Alkoxyguanidinyl-substituted phenyl acetamides as protease inhibitors
Phenyl acetamide compounds are described, including compounds of Formula I: ##STR1## or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3 -R6, R11, B, Y and W are set forth in the specification. Th...
02/18/2003
65182661- Aryl-3-thioalkyl pyrazoles, the synthesis thereof and the use thereof as insecticides
The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I: ##STR1## or a salt thereof, where R1 represents R5 O, R5 SO2, R5...
02/11/2003
6518310Aminoguanidines and alkoxyguanidines as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: ##STR1## wherein X is O or NR9 and R1 -R4, R6 -R9, R11, R12, Ra, Rb, R
02/11/2003
6515002Compounds and compositions for treating C1s-mediated diseases and conditions
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of...
02/04/2003
6514978Thromboresistant materials incorporating pyrazinone protease inhibitors
Thromboresistant materials are described which incorporate pyrazinone compounds of the Formula I: ##STR1## wherein X is O, NR11 or CH.dbd.N, R3 -R11, Ra, Rb, Rc, W, m, and n are set forth i...
02/04/2003
6506784Use of 1,3-substituted pyrazol-5-yl sulfonates as pesticides
The present invention is directed to inhibiting pest GABA receptors by contacting said receptors with a compound of Formula I: ##STR1## The invention is also directed to methods of controlling pests, especially insects and arachnids such as fleas and tick...
01/14/2003
6492403Methods of treating C1s-mediated diseases and conditions and compositions thereof
Disclosed is a method for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of...
12/10/2002
6486174Tetrahydroisoquinoline-3-carboxylic acid alkoxyguanidines as integrin antagonists
The present invention relates to novel tetrahydroisoquinoline-3-carboxylic acid alkoxyguanidine compounds that are antagonists of alpha V (଱v) integrins, for example ଱vଲ.sub.3 and ଱vଲ.sub.5 integrins, th...
11/26/2002
6476016Cyclic oxyguanidine pyrazinones as protease inhibitors
Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: ##STR1## wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically ...
11/05/2002
6472399Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1## wherein X is O or NR9 and Het, R1, R7, R8, R12 -R15, Ra, Rb
10/29/2002
6469029Azacycloalkanone serine protease inhibitors
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 compoun...
10/22/2002
6453246System, method, and computer program product for representing proximity data in a multi-dimensional space
A system, method and computer program product for representing precise or imprecise measurements of similarity/dissimilarity (relationships) between objects as distances between points in a multi-dimensional space that represents the objects. Self-organiz...
09/17/2002
6434490Method of generating chemical compounds having desired properties
A computer based, iterative process for generating chemical entities with defined physical, chemical and/or bioactive properties. During each iteration of the process, (1) a directed diversity chemical library is robotically generated in accordance with r...
08/13/2002
6423948Microtiter plate with integral heater
A microtiter plate system includes an integral heater. In an embodiment, the integral heater includes a heater plate. In another embodiment, the integral heater includes resistive heater wires positioned beneath and/or between the wells of a microtiter pl...
07/23/2002
6420397Heteroaryl protease inhibitors and diagnostic imaging agents
Ketothiazole alkoxyguanidine and aminoguanidine analogs are described, including compounds of the Formula I: ##STR1## wherein X is O or NR9 and Het, A, R1, R7, R8, R12, R13, Ra, ...
07/16/2002
6417161Amino acid amidinohydrazones, alkoxyguanidines and aminoguanidines as protease inhibitors
The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: ##STR1## wherein X is O or NR19 and A1, A2, R7 -R10, R18, Ra,...
07/09/2002
6409988Radiolabeled 1-aryl pyrazoles, the synthesis thereof and the use thereof as pest GABA receptor ligands
The present invention is directed to radiolabeled compounds of Formula I: ##STR1## or salts thereof, where R1 represents R8, R8 O, R8 SO2, R8 SO or R8 S in which R8 is trit...
06/25/2002
6403633Heteroaryl amidines, methylamidines and guanidines, and use thereof as protease inhibitors
The present invention is directed to compounds of Formula I: ##STR1## wherein X is O, S or NR7 and R1 -R7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts ther...
06/11/2002
6350764Heteroaryl aminoguanidines and alkoxyguanidines and their use as protease inhibitors
Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: ##STR1## wherein X is O or NR9 and Het, R1, R7, R8, R12 -R15, Ra, Rb
02/26/2002
6344486Benzamide and sulfonamide substituted aminoguanidines and alkoxyguanidines as protease inhibitors
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 --SO2 --, and R1 -R4, R9 -R19, Ra...
02/05/2002
6344484Tyrosine alkoxyguanidines as integrin inhibitors
The present invention relates to novel tyrosine alkoxyguanidine compounds that are inhibitors of alpha V (଱v) integrins, for example ଱v댣 and ଱v댥 integrins, their pharmaceutically acceptable salts, and pharmaceutical composi...
02/05/2002
6326492Heterocyclic protease inhibitors
Described are compounds of the Formula VII: ##STR1## wherein Het, R1, R7 and A are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as t...
12/04/2001
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