Patents Assigned to 3-Dimensional Pharmaceuticals
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Patent number: 6291514Abstract: The present invention is directed to compounds of Formula I: 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 thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.Type: GrantFiled: August 11, 1999Date of Patent: September 18, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Carl R. Illig, Nalin L. Subasinghe, James B. Hoffman, Kenneth J. Wilson, M. Jonathan Rudolph, Juan José Marugán
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Publication number: 20010020004Abstract: 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 of said nucleic acid sequences and the production of said muteins. Also disclosed are methods for stimulating cell division, treating a wound, treating ischemia, treating heart disease, treating neural injury, treating peripheral vascular disease, treating a gastric ulcer and treating a duodenal ulcer.Type: ApplicationFiled: April 5, 2001Publication date: September 6, 2001Applicant: 3-Dimensional Pharmaceuticals, Inc.Inventors: Barry A. Springer, Michael W. Pantoliano, Celia M. Sharp
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Patent number: 6281206Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, 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 are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: February 11, 2000Date of Patent: August 28, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6274712Abstract: 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 the nucleic acid sequences and the production of the muteins.Type: GrantFiled: December 23, 1998Date of Patent: August 14, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Barry A. Springer, Michael W. Pantoliano, Celia M. Sharp
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Patent number: 6274628Abstract: The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NH, L is —O— or —SO2—, and R1-R4, R9-R19, Ra, Rb, Rc, 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 such as thrombin. Also described are methods for preparing the compounds of Formula I. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal.Type: GrantFiled: April 1, 1999Date of Patent: August 14, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Richard M. Soll, Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Patent number: 6268158Abstract: The present invention is a method for ranking the affinity of each of a multiplicity of different molecules for a target molecule which is capable of denaturing due to a thermal change.Type: GrantFiled: December 10, 1999Date of Patent: July 31, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Michael W. Pantoliano, Eugenio C. Petrella, Francis R. Salemme, Barry A. Springer
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Patent number: 6268218Abstract: The present invention provides an assay apparatus for that includes a temperature adjusting device for simultaneously heating a plurality of samples, and a receiving device for receiving spectral emission from the samples while the samples are being heated. In further aspects of the invention, the receiving device can be configured to receive fluorescent emission, ultraviolet light, and visible light. The receiving device can be configured to receive spectral emission from the samples in a variety of ways, e.g., one sample at a time, simultaneously from more than one sample, or simultaneously from all of the samples. The temperature adjusting device can be configured with a temperature controller for changing temperature in accordance with a pre-determined profile.Type: GrantFiled: December 14, 1999Date of Patent: July 31, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Michael W. Pantoliano, Roger F. Bone, Alexander W. Rhind, Francis R. Salemme
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Patent number: 6245763Abstract: 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, Ra, Rb, Rc, Z, and n 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 preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.Type: GrantFiled: January 14, 2000Date of Patent: June 12, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Patent number: 6235778Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R114 R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: November 26, 1997Date of Patent: May 22, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
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Patent number: 6232085Abstract: The present invention is a method for ranking the affinity of each of a multiplicity of different molecules for a target molecule which is capable of denaturing due to a thermal change.Type: GrantFiled: December 10, 1999Date of Patent: May 15, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Michael W Pantoliano, Eugenio C Petrella, Francis R Salemme, Barry A Springer
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Patent number: 6225302Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, 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 are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: August 1, 2000Date of Patent: May 1, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6214293Abstract: The present invention provides an assay apparatus for that includes a temperature adjusting means for simultaneously heating a plurality of samples, and a receiving means for receiving spectral emission from the samples while the samples are being heated. In further aspects of the invention, the receiving means can be configured to receive fluorescent emission, ultraviolet light, and visible light. The receiving means can be configured to receive spectral emission from the samples in a variety of ways, e.g., one sample at a time, simultaneously from more than one sample, or simultaneously from all of the samples. The temperature adjusting means can be configured with a temperature controller for changing temperature in accordance with a pre-determined profile.Type: GrantFiled: December 14, 1999Date of Patent: April 10, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Michael W. Pantoliano, Roger F. Bone, Alexander W. Rhind, Francis R. Salemme
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Patent number: 6204263Abstract: Pyrazinone compounds are described, including compounds of the Formula I: wherein X is O, NR11 or CH═N, R3-R11, Ra, Rb, Rc, W, m, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: June 11, 1999Date of Patent: March 20, 2001Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan
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Patent number: 6133315Abstract: 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 enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: March 16, 1999Date of Patent: October 17, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6127191Abstract: The present invention provides a library of compounds, each comprised of a common aminobenzenedicarboxylic acid core structure (scaffold) that serves as a template for synthesizing approximately 10.sup.1 -10.sup.6 compounds which are analogs of the scaffold. The library is employed to study ligand binding by biological receptors, such as enzymes, G-protein coupled receptors and membrane channels. For example, certain individual compounds within the library selectively bind and inhibit the action of trypsin-like serine proteases. The present invention also relates to combinatorial synthetic methods for making such libraries of compounds. Additionally, the present invention relates to novel scaffold-modified solid supports, particularly scaffold-modified polymer resins and methods for preparing said resins.Type: GrantFiled: November 26, 1997Date of Patent: October 3, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Todd L. Graybill, Zhengdong Wu, Nalin Subasinghe, Cynthia L. Fedde, Joseph M. Salvino
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Patent number: 6037356Abstract: 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, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin.Type: GrantFiled: November 25, 1998Date of Patent: March 14, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Patent number: 6036920Abstract: The present invention provides an assay apparatus for that includes a temperature adjusting device for simultaneously heating a plurality of samples, and a receiving device for receiving spectral emission from the samples while the samples are being heated. In further aspects of the invention, the receiving device can be configured to receive fluorescent emission, ultraviolet light, and visible light. The receiving device can be configured to receive spectral emission from the samples in a variety of ways, e.g., one sample at a time, simultaneously from more than one sample, or simultaneously from all of the samples. The temperature adjusting device can be configured with a temperature controller for changing temperature in accordance with a pre-determined profile.Type: GrantFiled: May 9, 1997Date of Patent: March 14, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Michael W. Pantoliano, Roger F. Bone, Alexander W. Rhind, Francis R. Salemme
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Patent number: 6034127Abstract: 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 enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: December 27, 1996Date of Patent: March 7, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6020141Abstract: The present invention is a method for ranking the affinity of each of a multiplicity of different molecules for a target molecule which is capable of denaturing due to a thermal change. The method comprises contacting the target molecule with one molecule of the multiplicity of different molecules in each of a multiplicity of containers, simultaneously heating the multiplicity of containers, measuring in each of the containers a physical change associated with the thermal denaturation of the target molecule resulting from the heating in each of the containers, generating a thermal denaturation curve for the target molecule as a function of temperature for each of the containers and determining a midpoint temperature (T.sub.m) therefrom, comparing the T.sub.m of each of the thermal denaturation curves with the T.sub.Type: GrantFiled: May 9, 1997Date of Patent: February 1, 2000Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Michael W. Pantoliano, Alexander W. Rhind, Francis R. Salemme
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Patent number: 5901069Abstract: 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 robotic synthesis instructions; (2) the compounds in the directed diversity chemical library are analyzed to identify compounds with the desired properties; (3) structure-property data are used to select compounds to be synthesized in the next iteration; and (4) new robotic synthesis instructions are automatically generated to control the synthesis of the directed diversity chemical library for the next iteration.Type: GrantFiled: August 1, 1997Date of Patent: May 4, 1999Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Dimitris K. Agrafiotis, Roger F. Bone, Francis R. Salemme, Richard M. Soll