Entries |
Document | Title | Date |
20080275027 | Piperazinone Derivatives Useful as Histamine H3 Receptor Antagonists and/or Inverse Agonists - The invention relates to compounds of formula (I) or salts and solvates thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis: | 11-06-2008 |
20080306047 | Use of Aza-Phenylalanine Compounds For Treating Cardiac Arrhythmia - The present invention relates to the use of certain aza-phenylalanine compounds of formula (I) wherein R | 12-11-2008 |
20090005362 | Compositions Comprising Antihistamines or Mast Cell Stabilizers, and Methods of Making and Using Same - Compositions comprise: (a) a material selected from the group consisting of antihistamines, stabilizers, salts thereof, and combinations thereof; and (b) a vasoconstrictor, decongestant, or a salt thereof, provided when the material consists of an antihistamine or a salt thereof, at least one antihistamine other than ketotifen and salts thereof is present. In certain embodiments, the compositions have a pH maintainable at about 5 or less during storage. The compositions can be used to treat, alleviate or ameliorate ocular allergic conditions. | 01-01-2009 |
20090005363 | Organic Compounds - The present invention relates to novel nicotinic acid derivatives, of formula (I) | 01-01-2009 |
20090069297 | Aurora kinase modulators and method of use - The present invention relates to chemical compounds having a general formula I | 03-12-2009 |
20090181950 | Histamine Receptor Antagonists Comprising an Azepin Core - The present invention relates to compounds of formula (I), and salts thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis. | 07-16-2009 |
20090203672 | Substituted Sulfonamide Compounds - Substituted sulfonamide compounds corresponding to the formula I′ | 08-13-2009 |
20090215750 | Pyrrolopyrazine kinase inhibitors - The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, | 08-27-2009 |
20090258862 | Niacin receptor agonists, compositions containing such compounds and methods of treatment - Compounds of the formula (I): as well as pharmaceutically acceptable salts and solvates are disclosed. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels. Pharmaceutical compositions and methods of treatment are also included. | 10-15-2009 |
20090312307 | HETEROCYCLO INHIBITORS OF POTASSIUM CHANNEL FUNCTION - Novel heterocyclo compounds useful as inhibitors of potassium channel function (especially inhibitors of the K | 12-17-2009 |
20100029619 | FUSED HETEROCYCLIC COMPOUND - The present invention provides a compound represented by the formula (I): | 02-04-2010 |
20100075953 | SUBSTITUTED PIPERAZINES, (1,4) DIAZEPINES, AND 2,5-DIAZABICYCLO (2.2.1) HEPTANES AS HISTAMINE H1 AND/OR H3 ANTAGONISTS OR HISTAMINE H3 REVERSE ANTAGONISTS - The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease. | 03-25-2010 |
20100105660 | ORGANIC COMPOUNDS75074 - A compound of formula (I), or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein M | 04-29-2010 |
20100137285 | SMALL MOLECULE MODULATORS OF CYTOKINE ACTIVITY - The present invention provides compounds having formula (I) or (II): | 06-03-2010 |
20100204209 | CCR2 Receptor Antagonists and Uses Thereof - The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. | 08-12-2010 |
20100210627 | PYRAZINE COMPOUNDS, THEIR USE AND METHODS OF PREPARATION - The invention provides compounds according to formula (I) | 08-19-2010 |
20100210628 | NOVEL sEH INHIBITORS AND THEIR USE - The invention is directed to novel sEH inhibitors and their use in the treatment of diseases mediated by the sEH enzyme. Specifically, the invention is directed to compounds according to Formula I: | 08-19-2010 |
20100216777 | AMINOPYRAZINE ANALOGS FOR TREATING GLAUCOMA AND OTHER RHO KINASE-MEDIATED DISEASES AND CONDITIONS - Methods for using aminopyrazine analogs to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of aminopyrazine analogs, are also disclosed. | 08-26-2010 |
20100273779 | Pyridazinone Derivatives - The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition. | 10-28-2010 |
20100280007 | Pyridazinone Derivatives - The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition. | 11-04-2010 |
20100280008 | AURORA KINASE MODULATORS AND METHOD OF USE - The present invention relates to chemical compounds having a general formula I | 11-04-2010 |
20110065684 | PHTHALAZINE DERIVATIVES AS PARP INHIBITORS - The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) | 03-17-2011 |
20110112074 | CHLOROTHIOPHENE-ISOXAZOLES AS INHIBITORS OF COAGULATION FACTORS XA AND THROMBIN - The present invention relates to compounds of the formula I, | 05-12-2011 |
20110112075 | CHLOROTHIOPHENE-AMIDES AS INHIBITORS OF COAGULATION FACTORS XA AND THROMBIN - The present invention relates to compounds of the formula I, | 05-12-2011 |
20110130386 | DNA-PK INHIBITORS - A compound of formula (I) wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C | 06-02-2011 |
20110160187 | 3-aryl-5,6-disubstituted pyridazines - The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions. | 06-30-2011 |
20110237570 | SUBSTITUTED IMIDAZO[1,2-B]PYRIDAZINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS - The present invention provides substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutically acceptable salts thereof, and tautomers of any of the foregoing, where such compounds inhibit β-site amyloid precursor protein-cleaving enzyme (BACE), which may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention also provides pharmaceutical compositions comprising any of these compounds and the use of any of these compounds and compositions in the treatment of diseases, disorders, or conditions in which BACE is involved. | 09-29-2011 |
20110251179 | 3,4-DIHYDRO-2H-PYRROLO[1,2-a]PYRAZIN-1-ONE DERIVATIVES - Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them. | 10-13-2011 |
20110288074 | NEW ADENOSINE RECEPTOR LIGANDS AND USES THEREOF - The present invention provides new compounds with high affinity for adenosine A | 11-24-2011 |
20110288075 | Pyridazinone Derivatives - The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition/cognitive disorders. | 11-24-2011 |
20110301149 | COMPOSITIONS AND METHODS FOR TREATING ALCOHOL USE DISORDERS, PAIN AND OTHER DISEASES - The present invention provides compounds which antagonize epsilon protein kinase C (PKCε). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds. | 12-08-2011 |
20110312944 | Heterocyclic Compounds Which Modulate The CB2 Receptor - Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. | 12-22-2011 |
20120040967 | Pyrazin-2-yl-pyridin-2-yl-amine and pyrazin-2-yl-pyrimidin-4-yl-amine Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation. | 02-16-2012 |
20120040968 | DIAMINO HETEROCYCLIC CARBOXAMIDE COMPOUND - Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. | 02-16-2012 |
20120046274 | 6-ALKENYL AND 6-PHENYLALKYL SUBSTITUTED 2-QUINOLINONES AND 2-QUINOXALINONES AS POLY(ADP-RIBOSE) POLYMERASE INHIBITORS - The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors | 02-23-2012 |
20120122847 | AURORA KINASE MODULATORS AND METHOD OF USE - The present invention relates to chemical compounds having a general formula I | 05-17-2012 |
20120149690 | Compositions Comprising Azelastine and Methods of Use Thereof - The present invention provides pharmaceutical compositions comprising azelastine, or a pharmaceutically acceptable salt or ester thereof including azelastine hydrochloride, and optionally one or more additional active agents. Preferred such compositions further comprise one or more pharmaceutically acceptable carriers or excipients that reduce the amount of post-nasal drip, and/or that minimize or mask the unpleasant bitter taste associated with post-nasal drip, of the compositions into the oral cavity, upon intranasal or ocular administration of the compositions. Especially effective excipients used in the compositions of the present invention are hypromellose as a viscosity modifier and sucralose as a taste-masking agent. The invention also provides methods of treating or preventing certain disorders, or symptomatic relief therefrom, by administering the compositions of the invention to a patient, e.g., for the symptomatic relief of allergic rhinitis, non-allergic vasomotor rhinitis, allergic conjunctivitis, as well as other disorders. | 06-14-2012 |
20120157446 | MEDICAL USE - The present invention relates to a method for the treatment of urticaria which comprises administering to a patient in need thereof an effective amount of a compound which is 4-[(4-chlorophenyl)methyl]-2-({(2R)-1-[4-(4-{[3-(hexahydro-1H-azepin-1-yl)propyl]oxy}phenyl)butyl]-2-pyrrolidinyl}methyl)-1(2H)-phthalazinone, | 06-21-2012 |
20120165318 | HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus. | 06-28-2012 |
20120190668 | ENHANCEMENT OF CELLULAR TRANSPLANTATION USING SMALL MOLEUCLE MODULATORS OF HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY - The present invention provides methods for enhancing cellular transplantation by exposing cells in vitro or ex vivo, or a recipient of cells, to a small molecule hepatocyte growth factor/scatter factor mimetic. Exemplary compounds are described. | 07-26-2012 |
20120225863 | HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus. | 09-06-2012 |
20130029974 | 6,7-DIHYDROIMIDAZO[1,5-A]PYRAZIN-8(5H)-ONE DERIVATIVES AS PROTEIN KINASE MODULATORS - There are provided 3,5-disubstituted derivatives of 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one compounds of formula (I) or a pharmaceutically acceptable salt thereof as defined in the present specification, which modulate the activity of protein kinases. The compounds are therefore useful in treating diseases caused by dysregulated protein kinase activity. In particular, such diseases to be treated with a compound of formula (I) of the present invention is one caused by and/or associated with disregulated protein kinase activity selected from the group consisting of cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders. The present invention also relates to processes for preparing the compounds of formula (I), combinatorial libraries thereof, pharmaceutical compositions comprising them, and methods of treating diseases utilizing pharmaceutical compositions comprising a compound of formula (I). | 01-31-2013 |
20130035328 | ANTIVIRAL COMPOUNDS AND METHODS - The invention relates to compounds having antiviral activity and methods utilizing the compounds to treat viral infections. | 02-07-2013 |
20130172323 | PYRIDAZINONES AS GPR119 AGONISTS - The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R | 07-04-2013 |
20130190296 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF DISEASE ASSOCIATED WITH TRP-P8 EXPRESSION - Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Tip-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression. | 07-25-2013 |
20130237528 | 6-ALKENYL AND 6-PHENYLALKYL SUBSTITUTED 2-QUINOLINONES AND 2-QUINOXALINONES AS POLY(ADP-RIBOSE) POLYMERASE INHIBITORS - The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors | 09-12-2013 |
20130289020 | CXCR4 Receptor Antagonists - Disclosed are compounds that are antagonists of the CXCR4 receptor. | 10-31-2013 |
20140128376 | PYRAZOL-4-YL-HETEROCYCLYL-CARBOXAMIDE COMPOUNDS AND METHODS OF USE - Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 05-08-2014 |
20140142088 | PYRIDAZINONE DERIVATIVES - The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition. | 05-22-2014 |
20140155385 | 4-IMIDAZOPYRIDAZIN-1-YL-BENZAMIDES AND 4-IMIDAZOTRIAZIN-1-YL-BENZAMIDES AS BTK INHIBITORS - The present invention relates to 6-5 membered fused pyridine ring compounds according to formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Brutons Tyrosine Kinase (Btk) mediated disorders. | 06-05-2014 |
20140171419 | ENHANCEMENT OF CELLULAR TRANSPLANTATION USING SMALL MOLECULE MODULATORS HEPATOCYTE GROWTH FACTOR (SCATTER FACTOR) ACTIVITY - The present invention provides methods for enhancing cellular transplantation by exposing cells in vitro or ex vivo, or a recipient of cells, to a small molecule hepatocyte growth factor/scatter factor mimetic. Exemplary compounds are described. | 06-19-2014 |
20140336182 | Aurora Kinase Modulators and Method of Use - The present invention relates to chemical compounds having a general formula I | 11-13-2014 |
20150031679 | HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus. | 01-29-2015 |
20150072972 | PHTHALAZINE DERIVATIVES AS PARP INHIBITORS - The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) | 03-12-2015 |
20150313909 | ANTIVIRAL COMPOUNDS AND METHODS - The invention relates to compounds having antiviral activity and methods utilizing the compounds to treat viral infections. | 11-05-2015 |
20160060268 | PYRAZINO[1,2-a]INDOLE COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS - The invention refers to compounds of general formula (I) | 03-03-2016 |
20160151364 | 4-IMIDAZOPYRIDAZIN-1-YL-BENZAMIDES AND 4-IMIDAZOTRIAZIN-1-YL-BENZAMIDES AS BTK INHIBITORS | 06-02-2016 |