Patents Assigned to Activesite Pharmaceuticals, Inc.
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Patent number: 11306061Abstract: Pure crystalline forms of 1-benzyl-N-(4-carbamimidoylbenzyl)-1H-pyrazole-4-carboxamide acetate, and an amorphous form, pharmaceutical compositions thereof, and methods for making the same, are disclosed.Type: GrantFiled: July 7, 2020Date of Patent: April 19, 2022Assignees: Rezolute, Inc., ActiveSite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Chilcote, Julian Scott Northen, Jamie Marshall
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Patent number: 11267790Abstract: A process for preparing and purifying a compound of Formula I is provided: or a salt thereof, wherein the subscript m is an integer of from 0 to 3; each Ra is independently selected from the group consisting of (C3-C8)cycloalkyl, (C1-C4)haloalkyl, halogen, —OH, —OR1, —SH, —SR1, —S(O)R1, —S(O)2R1, —SO2NH2, —C(O)NH2, —C(O)NHR1, —C(O)N(R1)2, —C(O)R1, —C(O)H, —CO2R1, —NO2, —NH2, —NHR1, —N(R1)2, wherein each R1 is independently (C1-C8)alkyl; L is a linking group selected from the group consisting of a bond or CH2; Qa, Qb, and Qc are each members independently selected from the group consisting of N, S, O and C(Rq) wherein each Rq is independently selected from the group consisting of H, C1-8 alkyl, halo and phenyl, and the ring having Qa, Qb, Qc and Y as ring vertices is a five-membered ring having two double bonds; and Y is selected from the group consisting of C and N.Type: GrantFiled: July 7, 2020Date of Patent: March 8, 2022Assignees: Rezolute, Inc., ActiveSite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Chilcote, Baburaj Krishnan, Ganapati Bhat, Vineet Malik
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Publication number: 20140128436Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:Type: ApplicationFiled: November 8, 2013Publication date: May 8, 2014Applicant: ActiveSite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Patent number: 8691861Abstract: This invention provides new pharmaceutically useful compounds that are prodrugs of inhibitors of plasma kallikrein and methods and compositions for preventing or treating plasma kallikrein dependent diseases or conditions, such as diabetic macular edema or hemorrhagic stroke, by administering prodrugs of the formula:Type: GrantFiled: April 12, 2012Date of Patent: April 8, 2014Assignee: ActiveSite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote, Joghee Raju Suresh, Sriram Narasimhan
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Patent number: 8658685Abstract: We have identified classes of kallikrein inhibitors as compounds that are useful in the reduction of vascular permeability (e.g., retinal vascular permeability and cerebral vascular permeability) and astrocyte activation. Diseases and conditions associated with increased vascular permeability include diabetic retinopathy, hemorrhagic stroke, and macular edema. Diseases and conditions associated with astrocyte activation include Alzheimer's disease, multiple sclerosis, Parkinson's disease, amyotrophic lateral sclerosis, Creutzfeldt-Jakob disease, stroke, epilepsy, and brain trauma.Type: GrantFiled: January 30, 2009Date of Patent: February 25, 2014Assignees: Activesite Pharmaceuticals, Inc., Joslin Diabetes CenterInventors: Lloyd P. Aiello, Tamie Jo Chilcote, Sukanto Sinha, Edward P. Feener
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Patent number: 8609866Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:Type: GrantFiled: December 17, 2010Date of Patent: December 17, 2013Assignee: ActiveSite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20120264798Abstract: This invention provides new pharmaceutically useful compounds that are prodrugs of inhibitors of plasma kallikrein and methods and compositions for preventing or treating plasma kallikrein dependent diseases or conditions, such as diabetic macular edema or hemorrhagic stroke, by administering prodrugs of the formula:Type: ApplicationFiled: April 12, 2012Publication date: October 18, 2012Applicant: Activesite Pharmaceuticals, Inc.Inventors: Sukanto SINHA, Tamie Jo Chilcote, Joghee Raju Suresh, Sriram Narasimhan
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Patent number: 8258170Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.Type: GrantFiled: June 6, 2011Date of Patent: September 4, 2012Assignee: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20110152533Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:Type: ApplicationFiled: December 17, 2010Publication date: June 23, 2011Applicant: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20110065757Abstract: We have identified classes of kallikrein inhibitors as compounds that are useful in the reduction of vascular permeability (e.g., retinal vascular permeability and cerebral vascular permeability) and astrocyte activation. Diseases and conditions associated with increased vascular permeability include diabetic retinopathy, hemorrhagic stroke, and macular edema. Diseases and conditions associated with astrocyte activation include Alzheimer's disease, multiple sclerosis, Parkinson's disease, amyotrophic lateral sclerosis, Creutzfeldt-Jakob disease, stroke, epilepsy, and brain trauma.Type: ApplicationFiled: January 30, 2009Publication date: March 17, 2011Applicants: JOSKIN DIABETES CENTER, ACTIVESITE PHARMACEUTICALS, INC.Inventors: Lloyd P. Aiello, Tamie Jo Chilcote, Sukanto Sinha, Edward P. Feener
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Publication number: 20100130563Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.Type: ApplicationFiled: November 20, 2009Publication date: May 27, 2010Applicant: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Patent number: 7625944Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.Type: GrantFiled: July 30, 2007Date of Patent: December 1, 2009Assignee: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20080038276Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.Type: ApplicationFiled: July 30, 2007Publication date: February 14, 2008Applicant: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Chilcote