| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 514157000 | The hetero ring is six-membered and includes at least two nitrogens and no other hetero atoms | 49 |
| 20100204187 | Purine Derivatives - Purine derivatives of Formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK3 kinase inhibitors. | 08-12-2010 |
| 20100261683 | Selective Inhibitors for Cyclin-Dependent Kinases - This invention provides a class of compounds which are useful for specifically inhibiting cyclin-dependent kinases. This class of compounds finds use in treating diseases resulting from inappropriate activity of cyclin-dependent kinases, including cancer, viral infections (e.g., HIV) neurodegenerative disorders (e.g. Alzheimer's disease), and cardiovascular disorders (e.g. atherosclerosis). Moreover, certain members of this class are particularly useful for inhibiting cyclin-dependent kinase 7 and are especially useful for the treatment of breast cancer. | 10-14-2010 |
| 20100279986 | HETEROCYCLIC DERIVED METALLOPROTEASE INHIBITORS - This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: | 11-04-2010 |
| 20100323994 | SUBSTITUTED IMIDAZOPYRIDAZINES USEFUL AS KINASE INHIBITORS - The invention provides compounds of formula I | 12-23-2010 |
| 20110021467 | INDAZOLECARBOXAMIDE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF MALARIA - The invention relates to methods of treating or preventing malaria which comprises administering to a patient in need thereof, an effective amount of a 1H-indazole-3-carboxamide derivative of general formula (I), in the form of a base or of an addition salt with an acid, or in the form of a hydrate or of a solvate of said base or acid addition salt. | 01-27-2011 |
| 20110046093 | PYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - The present invention relates to a compound of formula (VII)I, or a pharmaceutically acceptable salt or ester thereof, wherein: X is NR | 02-24-2011 |
| 20110082117 | PHENYL SULFONAMIDES AS MODULATORS OF ION CHANNELS - The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 04-07-2011 |
| 20110144066 | SMALL MOLECULE INHIBITORS OF THE PLECKSTRIN HOMOLOGY DOMAIN AND METHODS FOR USING SAME - Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein. | 06-16-2011 |
| 20110144067 | N-Acyloxysulfonamide and N-Hydroxy-N-Acylsulfonamide Derivatives - The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy. | 06-16-2011 |
| 20110144068 | 3,4-DIARYLPYRAZOLES AS PROTEIN KINASE INHIBITORS - 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer. | 06-16-2011 |
| 20110172195 | AQUAPORIN MODULATORS AND METHODS OF USING THEM FOR THE TREATMENT OF EDEMA AND FLUID IMBALANCE - Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins. | 07-14-2011 |
| 20110190241 | TARGETING AN HIV-1 NEF-HOST CELL KINASE COMPLEX - Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro. | 08-04-2011 |
| 20110212929 | Protein Kinase Inhibitors - Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: | 09-01-2011 |
| 20110218178 | IMIDAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: | 09-08-2011 |
| 20110237553 | APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES - Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. | 09-29-2011 |
| 20110263541 | KINASE INHIBITORS AND THEIR USE AS PHARMACEUTICAL AGENTS - Described herein are compounds that are inhibitors of one or more protein kinases. Also described are pharmaceutical compositions and medicaments that include the compounds described herein. Also described herein are methods of using such protein kinase inhibitors, alone and in combination with other compounds, for conditions or diseases mediated or dependent upon protein kinases. | 10-27-2011 |
| 20110269721 | METHODS OF TREATING THALASSEMIA - Provided herein are method of treating, ameliorating, or delaying at least one symptom of a genetic blood disorder, e.g. sickle cell disorder or thalassemia, in a patient in need thereof, comprising administering a therapeutically effective amount of a Jak2 inhibitor. Also provided in part is a method of reducing an enlarged spleen in a patient suffering from thalassemia, comprising administering a therapeutically effective amount of a Jak2 inhibitor. | 11-03-2011 |
| 20110294761 | STEM CELL CULTURES - The present invention relates compounds for stabilizing cells and methods of their use. | 12-01-2011 |
| 20110301128 | Pyrrole Derivatives As Pharmaceutical Agents - Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors. | 12-08-2011 |
| 20120083474 | HETEROCYCLIC AMIDES AS MODULATORS OF TRPA1 - Certain heterocyclic amide compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPA1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease. | 04-05-2012 |
| 20120101072 | TRIAZOLE COMPOUNDS THAT MODULATE HSP90 ACTIVITY - The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound. | 04-26-2012 |
| 20120165298 | SULFONAMIDE COMPOUNDS - The present invention includes novel compound and methods of treating a disease or disorder by antagonizing Bcl-2 family proteins, particularly compounds of formula (I): | 06-28-2012 |
| 20120190654 | NOVEL BICYCLIC UREA COMPOUNDS - The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer. | 07-26-2012 |
| 20120208790 | ION CHANNEL MODULATORS AND METHODS OF USE - In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels. | 08-16-2012 |
| 20130023499 | CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF - Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B-cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample. | 01-24-2013 |
| 20130029944 | INHIBITORS OF PROTEIN KINASES - The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 01-31-2013 |
| 20130116216 | TRANSGLUTAMINASE TG2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF - Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents. | 05-09-2013 |
| 20130150334 | TOPICAL FORMULATION FOR ADMINISTERING A COMPOUND - Embodiments of topical formulations for administering compound I or a pharmaceutically acceptable salt or solvate thereof are disclosed. Embodiments of methods for using the topical formulations in the treatment of dermatological disorders such as cutaneous collagen vascular diseases, e.g., cutaneous lupus, also are disclosed. | 06-13-2013 |
| 20130303491 | Antiviral Drugs for Treatement or Prevention of Dengue Infection - Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus. | 11-14-2013 |
| 20130310348 | QUINOLINE DERIVATIVES AND USES THEREOF - This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQ | 11-21-2013 |
| 20130345180 | 2,4- DIAMINOPYRIMIDINE DERIVATIVES - There are provided compounds of formula I | 12-26-2013 |
| 20140018326 | SULFONAMIDES AS HIB PROTEASE INHIBITORS - Compounds of Formula I are disclosed: wherein L, A, R | 01-16-2014 |
| 20140243295 | USE OF SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINES - The present invention relates to: —use of a 2,3-dihydroimidazo[1,2-c]quinazoline compound, or of a pharmaceutical composition containing same, as a sole active agent, or of a combination of a) said compound or a pharmaceutical composition containing said compound and b) one or more further active agents, for the preparation of a medicament for the treatment or prophylaxis of cancer; —combinations of a) said compound and b) one or more further active agents; —a pharmaceutical composition comprising said compound as a sole active agent for the treatment of breast cancer; —a pharmaceutical composition comprising a combination of a) said compound and b) one or more further active agents; —use of biomarkers involved in the modification of Bel expression, HER family expression and/or activation, PIK3CA signaling and/or loss of PTEN for predicting the sensitivity and/or resistance of a cancer patient to said compound and providing a rationale-based synergistic combination as defined herein to increase sensitivity and/or to overcome resistance; and —a method of determining the level of a component of one or more of Bcl expression, HER family expression and/or activation, PIK3CA signaling and/or loss of PTEN. | 08-28-2014 |
| 20150031652 | POLY (ADP-RIBOSE) POLYMERASE (PARP) INHIBITORS - Disclosed are compounds of the following formula: | 01-29-2015 |
| 20150094283 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof. | 04-02-2015 |
| 20150291598 | COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES - The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease, such as malaria, caused by a | 10-15-2015 |
| 20150352108 | AMINO-PYRIMIDINE COMPOUNDS AS INHIBITORS OF TBK1 AND/OR IKK EPSILON - The invention relates to certain amino-pyrimidine compounds which inhibit TBK1 and/or IKK epsilon and which may therefore find application in treating inflammation, cancer, septic shock and/or Primary open Angle Glaucoma (POAG). | 12-10-2015 |
| 20150368209 | 4-Pyrimidinylamino-benzenesulfonamide derivatives and their use for the inhibition of polo-like kinase 1 (PLK1) for the treatment of cancer and their use for the treatment of bacterial infections - The present invention relates to 4-pyrimidinylamino-benzenesulfonamide derivatives of general formula (I) and pharmaceutically acceptable salts, solvates, hydrates, regioisomeric and polymorphic forms thereof, processes for manufacturing of them, the use of them, as well as pharmaceutical compositions containing at least one of them as pharmaceutically active agent(s) together with pharmaceutically acceptable carrier, excipient and/or diluents, especially for the inhibition of polo-like kinases (PLKs) and the treatment of cancer. Said 4-pyrimidinylamino-benzenesulfonamide compounds have been also identified as new drug candidates for the prevention and/or treatment of infectious diseases like bacterial diseases e.g. tuberculosis, including the currently multidrug-resistant tuberculosis (MDR-TB), extensively drug-resistant tuberculosis (XDR-TB) as well as for preventing tuberculosis. | 12-24-2015 |
| 20150376132 | Quinoline Sulfonyl Derivatives And Uses Thereof - The present disclosure relates to quinoline sulfonyl compounds, compositions comprising these compounds and their use, in particular for the treatment of cancer. In particular, the present disclosure includes compounds of Formula (I), and compositions and uses thereof: | 12-31-2015 |
| 20150376139 | ANTI-PCSK9 COMPOUNDS AND METHODS FOR THE TREATMENT AND/OR PREVENTION OF CARDIOVASCULAR DISEASES - Disclosed are compounds that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (PCSK9), and methods of using these modulators to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease (CVD), including treatment of hypercholesterolemia. | 12-31-2015 |
| 20160008338 | DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS | 01-14-2016 |
| 20160008365 | METHODS OF TREATING A CANCER USING SUBSTITUTED PYRROLOPYRIMIDINE COMPOUNDS, COMPOSITIONS THEREOF | 01-14-2016 |
| 20160009687 | BCL-2-SELECTIVE APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE DISEASES | 01-14-2016 |
| 20160083384 | SALTS AND CRYSTALLINE FORMS OF AN APOPTOSIS-INDUCING AGENT - Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}-sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. | 03-24-2016 |
| 20160102082 | TARTRATE SALT OF 5-CHLORO-THIOPHENE-2-CARBOXYLIC ACID [(S)-2-[METHYL-3-(2-OXO-PYRROLIDIN-1-YL)-BENZENESULFONYLAMINO]-3-(4-METHY- L-PIPERAZIN-1-YL)-3-OXO-PROPYL]AMIDE - The invention relates to the tartrate salt of 5-chloro-thiophene-2-carboxylic acid [(S)-2-[methyl-3-(2-oxo-pyrrolidin-1-yl) -benzenesulfonylamino]-3-(4-methyl-piperazin-1-yl)-3-oxo-propyl]amide, to its crystalline form, to its preparation and to its therapeutic use. | 04-14-2016 |
| 20160146784 | COMPOSITIONS AND METHODS OF SCREENING FOR COMPOUNDS THAT MODULATE ACTIVITY AT A TWEAK BINDING SITE ON A CRD OF FN14 - The present disclosure is directed to methods of screening a compound for modulating activity at a TNF-like weak inducer of apoptosis (TWEAK) binding site on a cysteine-rich domain (CRD) of fibroblast growth factor-inducible 14 (Fn14). The present disclosure also provides heterocyclic compounds and pharmaceutically acceptable salts thereof and methods for the prevention, treatment, and amelioration of cell proliferative disorders with these compounds. | 05-26-2016 |
| 20160176826 | INHIBITORS OF ACK1/TNK2 TYROSINE KINASE | 06-23-2016 |
| 20160185736 | NOVEL, TRIAZINE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides a novel P2X | 06-30-2016 |
| 20160250233 | ANTIVIRAL DRUGS FOR TREATMENT OR PREVENTION OF DENGUE INFECTION | 09-01-2016 |
