Class / Patent application number | Description | Number of patent applications / Date published |
514263210 | The additional hetero ring is a 1,3-diazine ring (including hydrogenated) | 52 |
20080269260 | PHOSPHODIESTERASE 4 INHIBITORS - PDE4 inhibition is achieved by novel compounds of the Formula I: | 10-30-2008 |
20080275067 | Quinazolinones as Inhibitors of Human Phosphatidylinositol 3-Kinase Delta - Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 11-06-2008 |
20080287469 | Phosphoinositide 3-Kinase Inhibitors for Inhibiting Leukocyte Accumulation - The invention relates generally to phosphoinositide 3-kinases (PI3Ks), and more particularly to methods of inhibiting leukocyte accumulation comprising selectively inhibiting phosphoinositide 3-kinase delta (PI3Kδ) and phosphoinositide 3-kinase gamma (PI3Kγ) activities in endothelial cells. The disclosed methods may be used to treat individuals having an inflammatory condition where leukocytes are found to be accumulating at the site of insult or inflamed tissue. The inflammatory condition may be attributed to or associated with an underlying disorder not typically associated with inflammation, e.g. cancer, coronary vascular disease, etc. | 11-20-2008 |
20090054468 | New Use 938 - The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection. | 02-26-2009 |
20090215798 | Inhibitor Compounds - The present invention relates to compounds and uses of compounds which interact with chitinase enzymes, in particular inhibition of those enzymes. | 08-27-2009 |
20090325982 | PHOSPHODIESTERASE 4 INHIBITORS | 12-31-2009 |
20100029693 | NOVEL PI3K DELTA INHIBITORS AND METHODS OF USE THEREOF - The present invention relates generally to phosphoinositide 3-kinases (PI3Ks), and more particularly to specific, selective, improved PI3Kδ inhibitors and methods of inhibiting undesirable levels of PI3Kδ activity using these PI3Kδ inhibitors to treat disorders mediated by PI3Kδ. | 02-04-2010 |
20100152211 | INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo. | 06-17-2010 |
20100168139 | INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo. | 07-01-2010 |
20100249155 | ATROPISOMERS OF 2-PURINYL-3-TOLYL-QUINAZOLINONE DERIVATIVES AND METHODS OF USE - The invention provides compounds, compositions and methods to treat certain inflammatory conditions and/or oncology by administering a compound that inhibits PI3K isoforms, particularly the delta isoform. It further provides specific stereoisomers of a compound useful for these methods. In particular, the compound is an optically active atropisomer of 2-((6-amino-9H-purin-9-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one. | 09-30-2010 |
20110046165 | CERTAIN CHEMICAL ENTITLES, COMPOSITIONS AND METHODS - Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein. | 02-24-2011 |
20110065731 | USES OF DPP-IV INHIBITORS - The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments. | 03-17-2011 |
20110301182 | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy comprising a DPP-IV inhibitor - The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for improving glycemic control in type 2 diabetes patients with inadequate glycemic control despite metformin therapy. | 12-08-2011 |
20110306622 | METHODS OF TREATING HEMATOLOGICAL DISORDERS WITH QUINAZOLINONE COMPOUNDS IN SELECTED SUBJECTS - This disclosure relates to methods of selecting a subset of subjects having a hematological disorder and treating the selected group with a PI3K-delta inhibitor. In particular, the methods disclose evaluating levels of characteristic chemokine biomarkers, such as CCL2, CCL3, CCL4, CCL5, CXCL13, CCL17, CCL22, or TNF-alpha to select subjects that would have a greater chance of benefiting from treatment with a PI3K-delta inhibitor. The PI3K-delta inhibitors disclosed in this application are a type of quinazolinone-purinyl family of compounds. | 12-15-2011 |
20120015964 | QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 01-19-2012 |
20120129874 | SALT FORMS OF ORGANIC COMPOUND - The present invention relates to novel salt forms of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine, a DPP-4 inhibitor and their use in pharmaceutical compositions useful in the treatment of type 2, diabetes, as well as their production. | 05-24-2012 |
20120208831 | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions - The present invention relates to substituted xanthines of general formula | 08-16-2012 |
20130109703 | Combination of a GPR119 Agonist and the DPP-IV Inhibitor Linagliptin for Use in the Treatment of Diabetes and Related Conditions | 05-02-2013 |
20130116266 | QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Compounds that inhibit P13Kδ activity, including compounds that selectively inhibit P13Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (P13Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which P13Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 05-09-2013 |
20130116267 | Role of PI3K P110 Delta Signaling in Retroviral Infection and Replication - The invention includes compositions and methods for regulating PI3K p110 delta as an anti-retroviral therapy. The invention includes a method of inhibiting p110 delta, a component of PI3K p110 delta signaling pathway, or any combination thereof in a cell as an anti-retroviral therapeutic approach for treating a retroviral infection, for example HTV. The invention includes a method of modulating PI3K p110 delta in a cell infected with a retrovirus by contacting the cell with an effective amount of a composition comprising an inhibitor of PI3K P110 delta. | 05-09-2013 |
20130123282 | SOLID STATE FORMS OF LINAGLIPTIN - The present invention provides solid state forms of Linagliptin, processes for preparing the solid state forms, and pharmaceutical compositions thereof. | 05-16-2013 |
20130143902 | COMPOSITIONS AND METHODS OF TREATING A PROLIFERATIVE DISEASE WITH A QUINAZOLINONE DERIVATIVE - Provided are methods that relate to a novel therapeutic strategy for the treatment of cancers. In particular, the method comprises administration of Compound A, | 06-06-2013 |
20130178485 | PROCESS FOR THE PREPARATION OF CHIRAL 8-(3-AMINOPIPERIDIN-1-YL)-XANTHINES - The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines. | 07-11-2013 |
20130252976 | POLYMORPHIC FORMS OF (S)-2-(1-(9H-PURIN-6-YLAMINO)PROPYL)-5-FLUORO-3-PHENYLQUINAZOLIN-4(3H)-ON- E - Polymorphs of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed. | 09-26-2013 |
20130274273 | Inhibiting Transient Receptor Potential Ion Channel TRPA1 - This disclosure describes a novel compounds and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain. | 10-17-2013 |
20130303554 | USE OF A DPP-4 INHIBITOR IN SIRS AND/OR SEPSIS - The present invention relates to methods for treating and/or preventing SIRS and/or sepsis comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for treating and/or preventing a metabolic disease in a patient with or at risk of SIRS and/or sepsis. | 11-14-2013 |
20130317046 | USE OF A DPP-4 INHIBITOR IN AUTOIMMUNE DIABETES, PARTICULARLY LADA - The present invention relates to methods for treating and/or preventing autoimmune diabetes, particularly LADA, as well as diseases related or associated therewith, comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for modifying disease trajectory of autoimmune diabetes (particularly LADA). | 11-28-2013 |
20140100236 | Use of selectively moisture-adjusted tabletting material in the production of mechanically stable tablets which contain at least one hydrate-forming active substance and/or adjuvant relevant to the mechanical stability of the tablets, particularly arginine-containing tablets - The present invention relates inter alia to the use of selectively moisture-adjusted tabletting material in the preparation of mechanically stable oral tablets which contain at least one hydrate-forming active substance and/or adjuvant relevant to the mechanical stability of the tablets, particularly arginine-containing oral tablets. | 04-10-2014 |
20140121223 | QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 05-01-2014 |
20140121224 | QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYOSITOL 3-KINASE DELTA - Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 05-01-2014 |
20140121225 | POLYMORPH OF LINAGLIPTIN BENZOATE - The present invention relates to a novel polymorph of Linagliptin benzoate and to methods for its preparation. Furthermore the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of Linagliptin benzoate. | 05-01-2014 |
20140135348 | USES OF DPP IV INHIBITORS - The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments. | 05-15-2014 |
20140163048 | COMPOSITIONS WITH INCREASED STABILITY FOR INHIBITING TRANSIENT RECEPTOR POTENTIAL ION CHANNEL TRPA1 - This disclosure describes solid forms of the compound of Formula (I) and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain. | 06-12-2014 |
20140179718 | PHOSPHATIDYLINOSITOL 3-KINASE INHIBITORS - The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), | 06-26-2014 |
20140221400 | USE OF MYELOPEROXIDASE (MPO) INHIBITORS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF TO TREAT MULTIPLE SYSYEM ATROPHY (MSA) 938 - The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection. | 08-07-2014 |
20140296260 | 3-Aryl-2-((Arylamino)Methyl)Quinazolin-4-(3H)-Ones - The invention relates to novel quinazolinone compounds and their use as inhibitors of PI3 kinases, for example, PI3Kδ, for treating and/or preventing diseases, disorder, and conditions associated with modulating PI3 kinase activity. Novel 3-aryl-2-((arylamino)methyl)quinazolin-4(3H)-one derivatives and pharmaceutically acceptable salts or solvates thereof and their use for the treatment or prevention of diseases, disorders, and conditions associated with the activity of one or more PI3 kinase, such as PI3Kδ, are disclosed. | 10-02-2014 |
20140303194 | SALT FORMS OF ORGANIC COMPOUND - The present invention relates to novel salt forms of a certain DPP-4 inhibitor and their use in pharmaceutical compositions useful in the treatment of type 2 diabetes, as well as their production. | 10-09-2014 |
20140371243 | MEDICAL USE OF A DPP-4 INHIBITOR - The present invention relates to the use of a certain DPP-4 inhibitor along with angioplasty or stenting, and/or to its use for treating and/or preventing restenosis from angioplasty or stenting. | 12-18-2014 |
20140378479 | QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 12-25-2014 |
20150025089 | PROCESS FOR THE PREPARATION OF CHIRAL 8-(3-AMINOPIPERIDIN-1-YL)-XANTHINES - The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines. | 01-22-2015 |
20150051228 | AMORPHOUS FORM OF LINAGLIPTIN AND PROCESS FOR PREPARATION THEREOF - The present invention relates to an amorphous form of linagliptin and processes for the preparation thereof. The invention also relates to a pharmaceutical composition comprising therapeutically effective amount of an amorphous form of linagliptin and use of said composition for treatment of diabetes especially type-I or type-II, prediabetes or reduction of glucose tolerance. | 02-19-2015 |
20150099768 | NOVEL PHARMACEUTICAL FORMULATIONS - There is provided inter alia a dry powder pharmaceutical formulation for inhalation comprising: (i) 6-(2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl) methyl)-3-(2-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-5-yl)-N,N-bis(2-methoxyethyl)hex-5-ynamide or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof and solvates thereof in particulate form as active ingredient; (ii) particulate lactose as carrier; and (iii) a particulate stabilizing agent selected from metal salts of stearic acid such as magnesium stearate and metal salts of stearyl fumarate. | 04-09-2015 |
20150290199 | LINAGLIPTIN SOLID DISPERSION - The present invention provides a novel amorphous solid dispersion of linagliptin in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it. | 10-15-2015 |
20150353551 | SUBSTITUTED PURINONE COMPOUNDS - The invention relates to compounds of formula (I): (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of as MDM2 and/or MDM4, and combinations comprising such compounds. | 12-10-2015 |
20160058769 | TREATMENT FOR DIABETES IN PATIENTS WITH INSUFFICIENT GLYCEMIC CONTROL DESPITE THERAPY WITH AN ORAL OR NON-ORAL ANTIDIABETIC DRUG - The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients with insufficient glycemic control despite a therapy with an oral and/or a non-oral antidiabetic drug. | 03-03-2016 |
20160067249 | 3-Aryl-2-((Arylamino)Methyl)Quinazolin-4-(3H)-Ones - The invention relates to novel quinazolinone compounds and their use as inhibitors of PI3 kinases, for example, PI3Kδ, for treating and/or preventing diseases, disorder, and conditions associated with modulating PI3 kinase activity. Novel 3 -aryl-2-((arylamino)methyl)quinazolin-4(3H)-one derivatives and pharmaceutically acceptable salts or solvates thereof and their use for the treatment or prevention of diseases, disorders, and conditions associated with the activity of one or more PI3 kinase, such as PI3Kδ, are disclosed. | 03-10-2016 |
20160108044 | COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASES AND CARDIOMYOPATHY - Disclosed herein inter alia are compositions and methods useful in the treatment neurodegenerative diseases and cardiomyopathy, and for modulating the activity of PINK1. | 04-21-2016 |
20160122352 | POLYMORPHS - The invention relates to polymorphous crystal modifications of a DPP-IV inhibitor, the preparation thereof and the use thereof for preparing a medicament. | 05-05-2016 |
20160145258 | Inhibitor Crystalline Form and Preparation Method and Use Thereof - The present invention relates to a new crystalline forms of the inhibitor, 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazoline-4-one; the new crystalline form, compared to known forms, has one or more improved properties. The present invention also relates to a method for preparing a new crystalline form of 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one, a pharmaceutical composition thereof and a use thereof in preparation of a pharmaceutical for the treatment and/or prevention of diseases such as chronic lymphocytic leukemia and indolent non-Hodgkin's lymphoma. | 05-26-2016 |
20160168131 | Substituted Quinazolin-4-one Derivatives | 06-16-2016 |
20160376274 | POLYMORPHIC FORMS OF (S)-2-(1-(9H-PURIN-6-YLAMINO)PROPYL)-5-FLUORO-3-PHENYLQUINAZOLIN-4(3H)-ON- E - Polymorphs of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one, compositions thereof, methods for their preparation, and methods for their use are disclosed. | 12-29-2016 |
20190144453 | NOVEL QUINAZOLINONE DERIVATIVES INHIBITING PI3K AND PHARMACEUTICAL COMPOSITION CONTAINING SAME | 05-16-2019 |