Class / Patent application number | Description | Number of patent applications / Date published |
514287000 | Three or more hetero atoms in the tetracyclo ring system | 28 |
20080214594 | Inhibitors Of Checkpoint Kinases - The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer. | 09-04-2008 |
20090023767 | Inhibitors of Checkpoint Kinases - The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer. | 01-22-2009 |
20090062324 | CATECHOLAMINE DERIVATIVES AND PRODRUGS THEREOF - The present invention relates to novel catecholamine derivatives of Formula I, to processes for their preparation, pharmaceutical compositions containing them and to their use in therapy. | 03-05-2009 |
20090182001 | Inhibitors of checkpoint kinases - The instant invention provides for compounds which comprise fused imidazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer. | 07-16-2009 |
20090209571 | Phenanthrene derivatives as MPGES-1 inhibitors - The invention encompasses novel compounds of Formula or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed. | 08-20-2009 |
20100056556 | ISOQUINOLINOPYRROLOPYRIDINONES ACTIVE AS KINASE INHIBITORS - Heteroarylpyridinone derivatives represented by formula (I) wherein R | 03-04-2010 |
20100099698 | Compositions for Improving Skin Conditions Comprising Matrine or Its Oxidized Derivatives - The present invention relates to a composition for improving skin conditions comprising matrine and oxymatrine as an active ingredient. Matrine and oxymatrine have lower cytotoxicity than retinol used as anti-wrinkle agents and exhibit the inhibition effect on collagenase activity and promotion effect on collagen biosynthesis at a molecular level, contributing to excellent efficacy in improvement of skin wrinkles. In addition, both matrine and oxymatrine exhibit the inhibition effect on melanin production by inhibiting intracellular tyrosinase activity, the improving effects of UV-induced skin damage and the skin growth promotion or hair loss prevention. Therefore, matrine and oxymatrine have the excellent improvement effects on skin conditions. Furthermore, matrine and oxymatrine have the excellent anti-obesity and anti-oxidation effects. The composition of this invention can be applied to cosmetic, pharmaceutical and food composition having no cytotoxicities and side effects. | 04-22-2010 |
20110003843 | NOVEL COMPOUNDS DERIVED FROM INDOLE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - The present invention relates to a compound derived from indole corresponding to the following formula II: | 01-06-2011 |
20110306629 | NOVEL C-1 ANALOGS OF PANCRATISTATIN AND 7-DEOXYPANCRATISTATIN AND PROCESSES FOR THEIR PREPARATION - The present application relates to novel C-1 substituted analogues of pancratistatin and 7-dexoypancratistatin of Formula (I), pharmaceutical compositions thereof and the use of said compounds of Formula (I) in the treatment of cancer The application also relates to processes for the preparation of said compound of Formula (I) and intermediates thereof. | 12-15-2011 |
20120108624 | TREATMENT OF DYSKINESIA RELATED DISORDERS - Disclosed herein are methods of treating Parkinsons disease while maintaining a low dyskinesia induction profile and methods of reversing dyskinesias comprising administering a therapeutically effective amount of a compound of the invention. The present invention further relates to uses and pharmaceutical compositions of said compounds in the manufacture of medicaments in treating the same. | 05-03-2012 |
20120196889 | CATECHOLAMINE DERIVATIVES AND PRODRUGS THEREOF - The present invention relates to novel catecholamine derivatives of Formula I, to processes for their preparation, pharmaceutical compositions containing them and to their use in therapy. | 08-02-2012 |
20120225903 | Novel 2-Substituted Quinoline Derivatives, And Method For Preparing Same - The invention relates to 2-substituted quinoline derivatives, to a method for preparing same, and to the use thereof for drug production, particularly for treating infections caused by protozoa, such as leishmaniases, trypanosomiases, toxoplasmoses, and/or infections caused by retroviruses such as, for example, HIV or HTLV. | 09-06-2012 |
20120258980 | Antibacterial Agent for Drug-Resistant Bacteria, Method for Screening for Same, and Use of Same - A method for treating an individual infected with drug-resistant bacteria resistant to at least one drug, the method including: administering to the individual an antibacterial agent for drug-resistant bacteria which comprises at least one of a nybomycin and a derivative thereof, wherein the antibacterial agent for drug-resistant bacteria is effective to the drug-resistant bacteria resistant to at least one drug. | 10-11-2012 |
20130184303 | PYRIDO[4,3-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 07-18-2013 |
20130184304 | PYRIDO[4,3-B]INDOLES AND METHODS OF USE - This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 07-18-2013 |
20130231360 | Beta-Carbolines as Inhibitors of Haspin and DYRK Kinases - The present disclosure is directed to compounds of Formula (I) which are inhibitors of Haspin kinase and DYRK kinases. The compounds of the present disclosure, and compositions thereof, are useful in the treatment of disease related to Haspin kinase and DYRK kinase expression and/or activity. | 09-05-2013 |
20130261147 | COMPOSITION FOR PREVENTING OR TREATING DEMENTIA - There is provided use of | 10-03-2013 |
20130281482 | NICOTINIC ACETYLCHOLINE RECEPTOR AGONISTS - The invention provides novel nicotinic acetylcholine receptor agonists, for example, phantasmidine and derivatives thereof, for example a compound of formula (I). Also disclosed are methods of treating disorders responsive to nicotinic acetylcholine receptor agonists such as Alzheimer's disease, schizophrenia, Myasthenia Gravis, Tourette's syndrome, Parkinson's disease, epilepsy, pain, and cognitive dysfunction by treatment with the nicotinic acetylcholine for agonists. | 10-24-2013 |
20130303563 | TREATMENT OF PERITONEAL INJURY USING JAK INHIBITORS - The invention provides, in certain embodiments, a method of preventing and/or treating peritoneal injury and/or diminished function by administering an effective amount of one or more inhibitors of JAK. The invention also provides a pharmaceutical composition including a JAK inhibitor for the treatment of peritoneal injury and/or diminished function. In another aspect, the invention provides a method of detecting an indicator of peritoneal injury. The method entails assaying a biological sample for periostin, wherein the presence of periostin at an elevated level indicates the presence and/or degree of peritoneal injury. Also provided, are methods of identifying subject for treatment of peritoneal injury and/or diminished function, methods of determining progression of these conditions, as well as methods of determining subjects' response to treatment. | 11-14-2013 |
20140221417 | THERAPEUTIC COMPOUNDS - Compounds of formula I: | 08-07-2014 |
20140343089 | NOREPINEPHRINE AND SELECTIVE SEROTONIN RECEPTOR BLOCKER AND USE THEREOF - The present invention relates to a norepinephrine and selective serotonin receptor blocker and the use thereof. The norepinephrine and selective serotonin receptor blocker is a compound of formula I, or isomers, pharmaceutically acceptable salts or solvates thereof, wherein R1 is selected from the group consisting of C1-6 alkyl, C1-6 alkoxy, C6-10 aralkyl, C6-10 arylalkoxy, C1-6 haloalkyl and C1-6 haloalkoxy; and R2 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. R3 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. The compound of the present invention is effective norepinephrine and selective serotonin receptor blocker. | 11-20-2014 |
20150099774 | Pyrido [3,4-C] [1,9] phenanthroline and 11, 12 dihydropyrido [3,4-C] [1,9] phenanthroline derivatives and the use thereof, particularly for treating cancer - New phenanthroline derivatives as drug as well as methods for producing said compounds are provided. | 04-09-2015 |
20150099775 | COMPOSITIONS AND METHODS FOR TREATING CANCERS - The present invention relates to compositions and methods for treating of cancer. In some embodiments, the invention relates to the use of agents that can modulate a component in the CDX2-KLF4 signaling pathway to treat myelodysplastic syndromes (MDS), acute myelogenous leukemia (AML), acute lymphocytic leukemia (ALL), adult T-cell leukaemia (ATLL), lymphoma, gastric cancer, multiple myeloma, or combinations thereof, or a condition associated with abnormal activity of the CDX2-KLF4 signaling pathway. | 04-09-2015 |
20150306092 | TETRAHYDROPROTOBERBINE COMPOUNDS AND USES THEREOF IN THE TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND NEURODEGENERATIVE DISEASES - Tetrahydroprotoberbine (THPB) compounds and their use in the treatment of neurological, psychiatric and neurodegenerative diseases is provided. The compounds include d-govadine, l-govadine and racemic govadine, as well as d-THPBs of general formula (I). Enantioselective processes for preparing compounds of formula (I), and d- and l-govadine are also provided.(I) | 10-29-2015 |
20150344476 | Naphthyridinedione derivatives - The invention relates to compound of the formula (I′) | 12-03-2015 |
20150374669 | ARYL IMIDAZOLES AND THEIR USE AS ANTI-CANCER AGENTS - Therapeutically effective 2,4,5-trisubstituted imidazole compounds are provided. Also provided are methods of preparing the compounds and pharmaceutical compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-cancer agents; wherein: R1 is aryl, substituted aryl, heterocycle, substituted heterocycle, heteroaryl, substituted heteroaryl or amino; R2 and R3 are independently aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, or substituted heteroaryl or R2 and R3 when taken together along with the carbon atoms they are attached to, form aryl or substituted aryl, and R4 is hydrogen, halogen, hydroxyl, thiol, lower alkyl, substituted lower alkyl, lower alkenyl, substituted lower alkenyl, lower alkynyl, substituted lower alkynyl, alkylalkenyl, alkyl alkynyl, alkoxy, alkylthio, aryl, aryloxy, amino, amido, carboxyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, heteroalkyl, cycloalkyl, substituted cycloalkyl, alkylcycloalkyl, alkylcycloheteroalkyl, nitro, cyano or —S(O)o.2R wherein R is alkyl, substituted alkyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, or substituted heteroaryl. | 12-31-2015 |
20160176876 | 2-SUBSTITUTED IMIDAZO[4,5-D]PHENANTHROLINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER | 06-23-2016 |
20160193203 | TREATMENT OF PERITONEAL INJURY USING JAK INHIBITORS | 07-07-2016 |