Entries |
Document | Title | Date |
20080207647 | Pyrazole Derivatives Having Tyrosine Kinase Activity - Compounds of the formula (I), in which R, X, R | 08-28-2008 |
20080214580 | 6-SUBSTITUTED 2-(BENZIMIDAZOLYL)PURINE AND PURINONE DERIVATIVES FOR IMMUNOSUPPRESSION - The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulae I and II: | 09-04-2008 |
20080214581 | Purine Derivatives as Agonists of the Adenosine A2a Receptor - A compound of formula (I): | 09-04-2008 |
20080280926 | Phosphodiesterase Inhibitors - The present invention relates to purine derivatives, which can be used as selective phosphodiesterase (PDE) type IV inhibitors. Compounds disclosed herein can be useful in the treatment of asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Also provided are processes for the preparation of disclosed compounds, pharmaceutical composition containing the disclosed compounds and their use as selective phosphodiesterase (PDE) type IV inhibitors. | 11-13-2008 |
20080287468 | PURINE AND IMIDAZOPYRIDINE DERIVATIVES FOR IMMUNOSUPPRESSION - The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. The compounds are of the general formulas: | 11-20-2008 |
20080318983 | A2B ADENOSINE RECEPTOR ANTAGONISTS - Disclosed are methods for treating asthma, inflammatory gastrointestinal tract disorders, cancer, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis using A | 12-25-2008 |
20090030019 | PURINE DERIVATIVES HAVING, IN PARTICULAR, ANTI-PROLIFERATIVE PROPERTIES, AND THEIR BIOLOGICAL USES - This invention provides 2-, 6, and 9-substituted purine derivatives, particularly 2(1-R hydroxymethylpropylamino)-6-benzylamino-9-isopropyl purine, having, in particular, antiproliferative properties, and suitable for use as pharmaceutical compositions and herbicidal compositions. Also provided are pharmaceutical compositions and herbicidal compositions comprising the 2-, 6, and 9-substituted purine derivatives, and methods of treatment using the 2-, 6, and 9-substituted purine derivatives. | 01-29-2009 |
20090099212 | A3 ADENOSINE RECEPTOR ANTAGONISTS - Disclosed are novel methods of antagonizing the A | 04-16-2009 |
20090209560 | ANTI-INFLAMMATION ACTIVITY OF NEWLY SYNTHESIZED XANTHINE DERIVATIVES KMUP-1 AND KMUP-3 - An anti-inflammation substrate for decreasing the proinflammation induced by the cytokines and inhibiting the lung function degeneration is provided. The anti-inflammation substrate includes one selected from the group consisting of a 7-[2-[4-(2-chlorobenzene)piperazinyl]ethyl]-1,3-dimethylxanthine, a 7-[2-[4-(4-nitrobenzene)piperazinyl]ethyl]-1,3-dimethylxanthine, a respective pharmaceutical acceptable salt thereof, and a combination thereof. | 08-20-2009 |
20090239885 | Inhibitors of nucleoside phoshorylases and nucleosidases - The present invention relates to compounds of the general formula (I) which are inhibitors of purine nucleoside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT), 5′-methylthioadenosine phosphorylases (MTAP), 5′-methylthioadenosine nucleosidases (MTAN) and/or nucleoside hydrolases (NH). The invention also relates to the use of these compounds in the treatment of diseases and infections including cancer, bacterial infections, protozoal infections, and T-cell mediated disease and to pharmaceutical compositions containing the compounds. | 09-24-2009 |
20090281126 | Organic Compounds - A compound of formula (I) and their preparation and use as pharmaceuticals | 11-12-2009 |
20090286813 | Thioxanthine Derivatives and Their Use as Inhibitors of MPO - There are disclosed novel compounds of Formula (I) wherein R | 11-19-2009 |
20100093768 | Agents for Reversing Epigenetic Silencing of Genes - The present invention provides methods for discovering agents that are effective in reversing epigenetic silencing by inhibiting the interaction of methyl-binding (MBD) proteins with methylated genomic DNA. Also provided are methods for reactivating silenced genes having CpG island hypermethylation along with methods for treatment and prevention of diseases, such as cancer and sickle cell anemia, by administering an agent that modulates methyl-binding domain (MBD) protein-mediated transcriptional repression, thereby increasing gene transcription to prevent or treat disease. Additionally, compounds identified by the present invention useful for treatment and prevention of diseases, such as cancer and sickle cell anemia, are provided. | 04-15-2010 |
20100130516 | PURINYL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. | 05-27-2010 |
20100152210 | PURINYL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. | 06-17-2010 |
20100160352 | ADENINE DERIVATIVES - Novel adenine derivatives of the formula (I), in which R | 06-24-2010 |
20100216821 | Benzimidazoles With A Hetero Spiro-Decane Residue As NPY-Y5 Antagonists - The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts, solvates, stereoisomers thereof, | 08-26-2010 |
20100249154 | COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO TRPA1 - Compounds and compositions for treating disorders related to TRPA1 are described herein. | 09-30-2010 |
20110184002 | METHOD OF TREATING HEPATIC DISEASE USING A2B ADENOSINE RECEPTOR ANTAGONISTS - The invention is related to methods of preventing and treating hepatic fibrosis using A | 07-28-2011 |
20110237607 | SUBSTITUTED PURINYL-PYRAZOL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel substituted purinyl-pyrazol derivatives (I) and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. | 09-29-2011 |
20110251217 | SUBSTITUTED PURINYL-PYRAZOL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel substituted purinyl-pyrazol derivatives of formula (I) and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. | 10-13-2011 |
20110257205 | XANTHINE DERIVATIVES AS SELECTIVE HM74A AGONISTS - The present invention relates to compounds which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial. | 10-20-2011 |
20110269780 | AZA-BENZIMIDAZOLONE CHYMASE INHIBITORS - Disclosed are small molecule inhibitors of the formula (I): and the pharmaceutical compositions thereof and processes of making the same. The compounds are useful in treating various diseases and conditions involving chymase. | 11-03-2011 |
20120004246 | PURINYL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. | 01-05-2012 |
20120046305 | METHODS AND COMPOSITIONS FOR TREATING RESPIRATORY DISORDERS - Compounds and compositions for treating disorders related to TRPA1 are described herein. | 02-23-2012 |
20120095027 | SYNTHESIS AND ANTI-PROLIFERATIVE EFFECT OF BENZIMIDAZOLE DERIVATIVES - This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. In particular, the disclosure provides for substituted purine compounds having the general formula | 04-19-2012 |
20120108613 | COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WARFARE AGENT-INDUCED INJURIES - Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein. | 05-03-2012 |
20120122896 | 2,1,3-BENZOXADIAZOL DERIVATIVES FOR THE INHIBITION OF INFLUENZA A AND B VIRUS AND RESPIRATORY SYNCYTIAL VIRUS REPLICATION - A 2,1,3-benzoxadiazole compound as a medicament according to the invention is one of the following compounds: 4-[(4-methoxybenzyl)thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethyl 4-methoxybenzene-1-sulfonate, 4-[(4-methylphenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(2,4-dichlorophenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethan-1-ol, 4-[(4-methylbenzyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(4-fluorophenyl)thio]-7-nitro-2,1,3-benzoxadiazole, 4-[(3-chlorophenyl)-thio]-7-nitro-2,1,3-benzoxadiazole, 2-[(7-nitro-2,1,3-benzoxadiazol-4-yl)thio]ethyl-4-methoxy-benzoate, 5-[4-(tert-butyl)-1,3-thiazol-2-yl]-2,1,3-benzoxadiazole, N-benzyl-4-nitro-2,1,3-benzoxadiazol-5-amine, 4-nitro-7-(phenylmethylsulfanyl)-2,1,3-benzoxadiazole, 4-nitro-7-(phenylmethylsulfonyl)-2,1,3-benzoxadiazole, 2-(hydroxymethyl)-5-[6-[(4-nitro-2,1,3-benzoxadiazol-7-yl)sulfanyl]purin-9-yl]oxolane-3,4-diole, or 2-[2-amino-6-[(4-nitro-2,1,3-benzoxadiazol-7-yl)sulfanyl]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol; or a physiologically tolerable salt, solvate, or physiologically functional derivative thereof. Said compounds are particularly advantageous for treating and/or preventing influenza type A and/or influenza type B infections in humans, mammals and/or birds, and for treating and/or preventing respiratory syncytial virus infections in humans, mammals and/or birds. | 05-17-2012 |
20120142711 | ACID-LABILE TRIGGER UNITS - The present invention relates to a compound comprising an imine bond as an acid-labile trigger group, the use of such an imine bond as an acid-labile trigger group, a process of cleaving the imine bond in said compound, and a pharmaceutical composition comprising said compound. | 06-07-2012 |
20120220608 | METHOD OF PREVENTING AND TREATING HEPATIC DISEASE USING A2B ADENOSINE RECEPTOR ANTAGONISTS - The invention is related to methods of preventing and treating hepatic fibrosis using A | 08-30-2012 |
20120245186 | COMBINATION CANCER THERAPY WITH HSP90 INHIBITORY COMPOUNDS - Disclosed is a method for treating a subject with cancer, comprising administering to the subject an effective amount of paclitaxel or a paclitaxel analogue and an effective amount of a compound represented by the following structural formula: a tautomer, or a pharmaceutically acceptable salt thereof. The variables depicted in the structural formula are defined herein. | 09-27-2012 |
20120264769 | METHANOCARBA ADENOSINE DERIVATIVES AND DENDRIMER CONJUGATES THEREOF - Disclosed are (N)-methanocarba adenine nucleosides, e.g., of the formula (I): as A | 10-18-2012 |
20130085150 | ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS - Compounds represented by formula I | 04-04-2013 |
20130123280 | A2B ADENOSINE RECEPTOR ANTAGONISTS - Disclosed are novel compounds that are A | 05-16-2013 |
20130123281 | Compositions and Methods for Inhibition of TBL-1 Binding to Disease-Associated Molecules - Compositions and methods which modulate diseases and disorders related to transducin β-like protein 1 (TBL1) activity, including but not limited to cancer, inflammation, and bone related diseases. | 05-16-2013 |
20130165455 | TLR AGONISTS - The present invention provides for TLR agonist conjugates (compounds) and compositions, as well as methods of using them. The compounds of the invention are broad-spectrum, long-lasting, and non-toxic combination of synthetic immunostimulatory agents, which are useful for activating the immune system of a mammal, preferably a human and can help direct the pharmacophore to the receptor within the endosomes of target cells and enhance the signal transduction induced by the pharmacophore. | 06-27-2013 |
20130303553 | FUSED HETEROCYCLIC COMPOUNDS - The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): | 11-14-2013 |
20130324561 | ATROPISOMERS OF P13K-INHIBITING COMPOUNDS - The invention provides compounds, compositions and methods to treat certain inflammatory conditions or cancers by administering a compound that inhibits PI3K isoforms, wherein the compounds are optically active atropisomers. It provides optically active stereoisomers of a class of pyrazole-containing compounds, which are useful for these methods, and provides methods to obtain these compounds as well as pharmaceutical compositions containing these compounds. | 12-05-2013 |
20140005208 | COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO TRPA1 | 01-02-2014 |
20140045866 | PURINE-BASED TRIAZOLES - A pharmaceutical composition for inhibiting at least protein kinase in a cell of a subject includes a purine based triazole. | 02-13-2014 |
20140066462 | TREATMENT OF POLYCYSTIC DISEASE - The present invention provides methods of treating polycystic disorders. In particular, methods include the use of inhibitors targeting certain protein kinases, such as mTOR, to treat polycystic disease. | 03-06-2014 |
20140113917 | PYRAZOLE COMPOUNDS AS CRTH2 ANTAGONISTS - The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2 antagonistic activity, wherein L, Y | 04-24-2014 |
20140243358 | METHOD OF PREVENTING AND TREATING HEPATIC DISEASE USING A2B ADENOSINE RECEPTOR ANTAGONISTS - The invention is related to methods of preventing and treating hepatic fibrosis using A | 08-28-2014 |
20140303192 | COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WARFARE AGENT-INDUCED INJURIES - Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein. | 10-09-2014 |
20140371242 | Azathioprine Oral Suspensions and Methods of Use - Compositions of azathioprine oral suspensions are disclosed. Disclosed azathioprine oral suspensions may be used to administer azathioprine to subjects such as children and geriatric patients that may have difficulty in swallowing solid dosage forms. The disclosed azathioprine oral suspension may be used for treating autoimmune diseases such as rheumatoid arthritis, pemphigus, Behcet's disease, autoimmune hepatitis, and inflammatory bowel disease, among others. According to an embodiment, an aqueous or non-aqueous vehicle may be used for azathioprine oral suspension. According to a different embodiment, sugar free azathioprine oral suspension may also be produced. | 12-18-2014 |
20150133475 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF PERIODONTITIS AND RHEUMATOID ARTHRITIS - The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of periodontitis and rheumatoid arthritis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. | 05-14-2015 |
20150141439 | PHARMACEUTICAL COMPOSITION FOR THE PREVENTION OR TREATMENT OF BRAIN TUMOR OR TEMODAL RESISTANT GLIOBLASTOMA MULTIFORM COMPRISING AZATHIOPRINE AS AN ACTIVE INGREDIENT - The present invention relates to a pharmaceutical composition for the prevention or treatment of cancer or Temodal resistant glioblastoma multiform comprising azathioprine as an active ingredient. The azathioprine of the present invention is not only effective in inhibiting the growth of glioblastoma multiform, a kind of brain tumor, but also excellent in treating glioblastoma multiform that displays resistance against Temodal (temozolomide), the conventional therapeutic agent for glioblastoma multiform, so that it can be effectively used as an active ingredient of a pharmaceutical composition for the prevention or treatment of such cancer as brain tumor (particularly, glioblastoma multiform) and particularly Temodal resistant glioblastoma multiform. | 05-21-2015 |
20160002243 | INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses compounds according to generic Formula (I) wherein all variables are defined as described herein, which inhibit BTK. The compounds disclosed herein are useful to modulate the activity of BTK and treat diseases associated with excessive BTK activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient. | 01-07-2016 |
20160002244 | OXIDATED DERIVATIVES OF TRIAZOLYLPURINES USEFUL AS LIGANDS OF THE ADENOSINE A2A RECEPTOR AND THEIR USE AS MEDICAMENTS - The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient. | 01-07-2016 |
20160022686 | PYRAZOLOPYRIMIDINE COMPOUNDS - Compounds of formula (I) and salts thereof: | 01-28-2016 |
20160038499 | COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO TRPA1 - Compounds and compositions for treating disorders related to TRPA1 are described herein. | 02-11-2016 |