Patent application number | Description | Published |
20100278905 | STABILIZED LIPID FORMULATION OF APOPTOSIS PROMOTER - An orally deliverable pharmaceutical composition comprises a Bcl-2 family protein inhibitory compound, e.g., ABT-263, a heavier-chalcogen antioxidant and a substantially non-aqueous lipid carrier, wherein said compound and said antioxidant are in solution in the carrier. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 11-04-2010 |
20100278921 | SOLID ORAL FORMULATION OF ABT-263 - An orally deliverable pharmaceutical composition comprises (a) a pharmaceutically acceptable acid addition salt of ABT-263 in solid particulate form, and (b) a plurality of pharmaceutically acceptable excipients including at least a solid diluent and a solid disintegrant; wherein the salt is formed from more than one equivalent of acid per equivalent of ABT-263. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 11-04-2010 |
20100280031 | LIPID FORMULATION OF APOPTOSIS PROMOTER - An orally deliverable pharmaceutical composition comprises a drug-carrier system having a Bcl-2 family protein inhibitory compound, e.g., ABT-263, in solution in a substantially non-aqueous carrier that comprises at least one phospholipid and a pharmaceutically acceptable solubilizing agent. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 11-04-2010 |
20100297194 | FORMULATION FOR ORAL ADMINISTRATION OF APOPTOSIS PROMOTER - An orally deliverable pharmaceutical composition comprises as a sole or first active ingredient a compound of Formula I defined herein or a pharmaceutically acceptable salt thereof, for example ABT-263 free base or ABT-263 bis-HCl salt, dispersed, in a free base equivalent amount of at least about 2.5% by weight of the composition, in a pharmaceutically acceptable carrier; wherein said active ingredient is in solid-state form and/or the composition further comprises, dispersed in the carrier, a pharmaceutically acceptable heavier-chalcogen antioxidant in an amount effective to inhibit oxidation of the active ingredient at a thioether linkage thereof. The composition is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 11-25-2010 |
20100311751 | SOLID DISPERSIONS CONTAINING AN APOPTOSIS-PROMOTING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound, e.g., ABT-263, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 12-09-2010 |
20110159085 | ABT-263 CAPSULE - A pharmaceutical capsule comprises a shell having encapsulated therewithin a liquid solution of ABT-263 or a pharmaceutically acceptable salt thereof in a substantially non-ethanolic carrier that comprises as pharmaceutically acceptable excipients (a) at least one phospholipid, (b) at least one solubilizing agent for the at least one phospholipid, selected from the group consisting of glycols, glycerides and mixtures thereof, (c) at least one non-phospholipid surfactant and (d) at least one sulfur-containing antioxidant. The capsule is useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 06-30-2011 |
20120108590 | MELT-EXTRUDED SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease. | 05-03-2012 |
20120277210 | SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 11-01-2012 |
20150148331 | MELT-EXTRUDED SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease. | 05-28-2015 |
20150157639 | SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 06-11-2015 |
Patent application number | Description | Published |
20080248126 | PARTICULATE DRUG DELIVERY - Methods for efficient preparation of drug-polymer (or oligomer) conjugates which are useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications. The invention additionally provides certain drug-polymer and drug-oligomer conjugates which are useful in the preparation of particles for delivery of the drug in vivo. The invention also provides nanoparticles of this invention prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention. | 10-09-2008 |
20110085974 | SMALL MOLECULE LIGAND-DRUG CONJUGATES FOR TARGETED CANCER THERAPY - The present invention describes small molecule ligand-drug conjugates and methods of using the small molecule ligand-drug conjugates for targeted treatment of cancer in a patient in need thereof. Further described are methods of sterilizing circulating tumor cells and determining drug concentration in cancer tissue. | 04-14-2011 |
20150210659 | PARTICULATE DRUG DELIVERY METHODS - The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells. | 07-30-2015 |
20150314006 | PARTICULATE DRUG DELIVERY METHODS - Methods for efficient preparation of drug-polymer (or oligomer) conjugates useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications are provided. The invention also provides nanoparticles prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention. The drug conjugates are formed during polymerization of the polymer or oligomer in which the drug is employed as an initiator of the polymerization of the monomers which form the polymer and/or oligomer. More specifically, the drug conjugates are formed by ring-opening polymerization of cyclic monomers in the presence of an appropriate ring-opening polymerization catalyst and the initiator (the drug). The method is particularly useful for formation of polymer/oligomer conjugates with drugs and other chemical species containing one or more hydroxyl groups or thiol groups. | 11-05-2015 |
Patent application number | Description | Published |
20100183743 | BENZTHIAZOLE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE - Inhibitors of poly(ADP-ribose)polymerase having a structure of Formula (I), ways to make them and methods of treating patients using them are disclosed. | 07-22-2010 |
20110015172 | PYRROLOPYRAZINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 01-20-2011 |
20110015173 | PYRROLOPYRIDINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 01-20-2011 |
20110257152 | PYRROLOPYRIDINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 10-20-2011 |
20110293744 | BENZOXAZOLE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE - Inhibitors of poly(ADP-ribose)polymerase having a structure of Formula (I), ways to make them and methods of treating patients using them are disclosed. | 12-01-2011 |
20120220572 | TRICYCLIC INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 08-30-2012 |
20140275004 | PYRROLOPYRIMINDINE CDK9 KINASE INHIBITORS - Disclosed are compound of Formula (Ia), | 09-18-2014 |
20140275027 | PYRROLO[2,3-B]PYRIDINE CDK9 KINASE INHIBITORS - Disclosed are compounds of Formula (IIIa), | 09-18-2014 |
20140275153 | CDK9 KINASE INHIBITORS - Disclosed are compound of Formula (Ia), | 09-18-2014 |
20140357616 | PYRROLOPYRIDINE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 12-04-2014 |
20150218165 | TETRACYCLIC CDK9 KINASE INHIBITORS - Disclosed are compounds of Formula (Ia), and pharmaceutically acceptable salts thereof, | 08-06-2015 |
20160060257 | PYRROLO [2,3-B] PYRIDINE CDK9 KINASE INHIBITORS - Disclosed are compounds of Formula (IIa), | 03-03-2016 |