Entries |
Document | Title | Date |
20080207645 | Pyridothienopyrimidine Derivatives - A pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine derivative of formula (I) | 08-28-2008 |
20080214576 | Topoisomerase Inhibitors and Prodrugs - Compositions and methods for treating cancer and other hyperproliferatice disease conditions with topoisomerase inhibitors and their prodrugs are disclosed. | 09-04-2008 |
20080221128 | Metalloprotease inhibitors containing a squaramide moiety - The present invention relates generally to pharmaceutical agents containing a heterocyclic moiety, and in particular, to heterocyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterocyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds with a squaramide or benzoxazinone moiety, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors. | 09-11-2008 |
20090082368 | METHODS OF MODULATING NEUROTROPHIN-MEDIATED ACTIVITY - Disclosed are compositions which modulate the interaction with nerve growth factor and precursors thereof with neurotrophic receptors. Also disclosed are methods of using the compositions of the invention, including methods of administration. | 03-26-2009 |
20090149478 | NOVEL COMBINATION ANTICANCER AGENTS - A cancer therapeutic agent according to the present invention comprises a combination of compound A described below, or a pharmaceutically acceptable salt thereof, and compound B described below, or a pharmaceutically acceptable salt thereof:
| 06-11-2009 |
20090258886 | HETEROALKYL LINKED PYRIMIDINE DERIVATIVES - The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to heteroalkyl linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other conditions or disorders associated with kinases. | 10-15-2009 |
20100010015 | Heterocyclic spiro-compounds as aldosterone synthase inhibitors - The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R | 01-14-2010 |
20100069406 | ASPARTYL PROTEASE INHIBITORS - Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R | 03-18-2010 |
20100075992 | Tetrodotoxin and its derivatives for the treament of peripheral-nervously derived neuropathi pain - The present invention refers to the use of a sodium channel blocker such as tetrodotoxin or saxitoxin, their analogues and derivatives as well as their physiologically acceptable salts, in medicinal products for human therapeutics for the treatment of peripheral-nervously derived neuropathic pain. | 03-25-2010 |
20100087450 | ORGANIC COMPOUNDS - The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment and/or prophylaxis of narcolepsy. | 04-08-2010 |
20100130513 | BENZIMIDAZOLES AND ANALOGS THEREOF AS ANTIVIRALS - Provided are compounds of the formula: | 05-27-2010 |
20100144763 | Pharmaceutical composition for inhibiting topoisomerase I and method for exploiting drug - The invention relates to the compounds isolated from | 06-10-2010 |
20100173913 | PYRIDO-AND PYRIMIDOPYRIMIDINE DERIVATIVES AS ANTI-PROLIFERATIVE AGENTS - The present invention concerns the compounds of formula | 07-08-2010 |
20100190804 | MACROCYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS - The present invention relates to macrocyclic compounds of Formula I: | 07-29-2010 |
20100249150 | STABLE PHARMACEUTICAL COMPOSITION OF FREEZE-DRIED TETRODOXIN POWDER - This invention relates to a stable pharmaceutical composition of freeze-dried tetrodotoxin powder which contains trace amount of tetrodotoxin, substances which can stabilizes tetrodotoxin, including disaccharide(s) or polyglucose(s) or analogues thereof and solvent(s), and solvents which can help tetrodotoxin dissolve. | 09-30-2010 |
20110028494 | HCV NS3 Protease Inhibitors - The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. | 02-03-2011 |
20110046161 | HCV NS3 PROTEASE INHIBITORS - The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. | 02-24-2011 |
20110201627 | FREEZE-DRIED REPARATION OF TETRODOTOXIN AND THE PRODUCING METHOD THEREOF - A stable freeze-dried powder preparation of tetrodotoxin and the producing method thereof. The freeze-dried powder preparation has tetrodotoxin as the main active ingredient, and comprises solubilizer, excipient and stabilizer. The said solubilizer is citric acid. The excipient is sodium chloride, mannitol or their composite. The stabilizer is dextran, trehalose or their composite. The ratio of tetrodotoxin, excipient and stabilizer is 1:150-3000:50-500 or 50-6000. Preferably, the preparation comprises lidocaine hydrochloride as function modulator. The preparation of the present invention can be used for avoiding the dependent abstinence syndrome of drugs such as opiates and cannabis. | 08-18-2011 |
20110251215 | MACROCYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS - The present invention relates to macrocyclic compounds of Formula I: | 10-13-2011 |
20110263616 | 11-(2-PYRROLIDIN-1-YL-ETHOXY)-14,19-DIOXA-5,7,26-TRIAZA-TETRACYCLO[19.3.1.- 1(2,6).1(8,12)]HEPTACOSA-1(25),2(26),3,5,8,10,12(27),16,21,23-DECAENE MALEATE SALT - The present invention relates to certain salts of a 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26triaza-tetra-cyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the maleate salt of this compound. The invention also relates to pharmaceutical compositions containing this salt and methods of use of the salt in the treatment of certain medical conditions. | 10-27-2011 |
20110294831 | 11-(2-PYRROLIDIN-1-YL-ETHOXY)-14,19-DIOXA-5,7,26-TRIAZA-TETRACYCLO[19.3.1.- 1(2,6).1(8,12)]HEPTACOSA-1(25),2(26),3,5,8,10,12(27),16,21,23-DECAENE CITRATE SALT - The present invention relates to certain salts of a 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the citrate salt of this compound. The invention also relates to pharmaceutical compositions containing the citrate salt and methods of use of the citrate salt in the treatment of certain medical conditions. | 12-01-2011 |
20110312978 | PDE1 INHIBITORS FOR OPHTHALMIC DISORDERS - Compounds that inhibit phosphodiesterase 1 (PDE1) are useful to treat glaucoma or elevated intraocular pressure. The PDE1 inhibitors may be administered as monotherapy or in combination with additional intraocular-pressure lowering agents. In addition, the invention provides ophthalmic compositions comprising PDE 1 inhibitors and optionally one or more additional intraocular pressure-lowering agents. Topical and systemic therapy may be used. | 12-22-2011 |
20120184565 | COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION - Compounds of the formula (I) are provided, including pharmaceutically acceptable salts thereof: | 07-19-2012 |
20120196876 | (9E)-15-(2-PYRROLIDIN-1-YL-ETHOXY)-7,12,25-TRIOXA-19,21,24-TRIAZA-TETRACYC- LO[18.3.1.1(2.5).1(14,18)]HEXACOSA-1(24),2,4,9,14,16,18(26),20,22-NONAENE CITRATE SALT - The present invention relates to certain salts of a 9E-15-(2-pyrrolidin-1-yl-ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5). 1(14,18)]hexacosa-1(24),2,4,9, 14,16,18(26),20,22-nonaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the citrate salt of this compound. The invention also relates to pharmaceutical compositions containing the citrate salt and methods of use of the citrate salt in the treatment of certain medical conditions. | 08-02-2012 |
20120214824 | PROTEOSTASIS REGULATORS - The present invention is directed to compounds of Formulae (I), (II), (III), (IV), (V), (VI), (VII), and (VIII), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis. | 08-23-2012 |
20120238589 | ORGANIC COMPOUNDS - 1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them. | 09-20-2012 |
20120264767 | STABLE PHARMACEUTICAL COMPOSITION OF FREEZE-DRIED TETRODOTOXIN POWDER - This invention relates to a stable pharmaceutical composition of freeze-dried tetrodotoxin powder which contains trace amount of tetrodotoxin, substances which can stabilizes tetrodotoxin, including disaccharide(s) or polyglucose(s) or analogues thereof and solvent(s), and solvents which can help tetrodotoxin dissolve. | 10-18-2012 |
20120322812 | RUTAECARPINE DERIVATIVES FOR TREATING INSOMNIA - The teachings provided herein generally relate to compositions comprising a rutaecarpine derivative that activates CYP1A2 through enzyme induction. The uses for such a derivative, in some embodiments can include improving sleep, as well as treating insomnia. Other uses for the derivatives are provided herein. | 12-20-2012 |
20120322813 | RUTAECARPINE DERIVATIVES FOR TREATING CAFFEINE TOXICITY - The teachings provided herein generally relate to compositions comprising a rutaecarpine derivative that activates CYP1A2 through enzyme induction. The compound can be used for treating caffeine toxicity, in some embodiments. Caffeine is just one example of a substrate that can be removed using the derivatives taught herein, and other examples, including theophylline, are provided herein. | 12-20-2012 |
20130150378 | SOLID STATE FORMS OF MACROCYCLIC KINASE INHIBITORS - Provided herein are salt forms of macrocyclic protein kinase inhibitors, pharmaceutical compositions containing the same, methods of making and using these compounds and compositions to treat proliferative disease mediated by kinase activity. | 06-13-2013 |
20130203776 | MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS - Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R | 08-08-2013 |
20130225607 | METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION WITHOUT COMPANION DIAGNOSIS - There is provided a method for treating pulmonary hypertension in a subject, comprising: administering to the subject in need thereof a daily dose of ambrisentan from 1 mg to about 15 mg, wherein the method is carried out without drug labeling instruction to monitor liver aminotransferase levels during ambrisentan treatment. | 08-29-2013 |
20130231353 | PYRIDO- AND PYRIMIDOPYRIMIDINE DERIVATIVES AS ANTI-PROFILERATIVE AGENTS - The present invention concerns the compounds of formula | 09-05-2013 |
20130331400 | METHOD FOR PRODUCING INDIGO-PLANT LEAF EXTRACT - An object of the present invention is to provide a tryptanthrin-containing indigo-plant leaf extract particularly suitable for application to the skin. The present invention provides a method for producing a tryptanthrin-containing indigo-plant leaf extract, the method comprising filtering a mixture of a concentrated ethanol extract of indigo-plant leaves and a polyhydric alcohol, and collecting the filtrate. The present invention further provides an indigo-plant leaf extract produced by this method. | 12-12-2013 |
20140005207 | SASPASE-FLG2 COMPLEX, MODULATING AGENTS, AND USES | 01-02-2014 |
20140080841 | Chemical Permeation Enhancers Enhance Nerve Blockade by Toxins - Chemical permeation enhancers (CPEs) improve access of local anesthetics to the nerve, thereby improving their performance. Surfactants, representing three CPE sub-groups: anionic, cationic, and nonionic surfactants, were co-injected with tetrodotoxin (TTX) or bupivacaine at the sciatic nerve of Sprague-Dawley rats. All enhancers produced marked concentration-dependent improvements in the frequency and duration of block with TTX but not bupivacaine. An in vitro toxicity assay showed a wide range of CPE myotoxicity, but in vivo histological assessment showed no signs of muscle or nerve damage at concentrations of CPEs that produced a half-maximal increase in the duration of block of TTX. There was no systematic relationship between the enhancers' charge or hydrophobicity and their enhancement of block duration or potency. Thus, CPEs can provide marked prolongation of nerve blockade from TTX, without apparent local tissue toxicity, and therefore enhance the clinical applicability of TTX for prolonged-duration local anesthesia. | 03-20-2014 |
20140243354 | COMBINATIONS OF INDIGO NATURALIS AND BERBERINE AND USES THEREOF - Methods and composition for treating or preventing an inflammatory dermatological disease or condition, such as psoriasis, in a subject are described. The methods involve topical applications to the subject a therapeutically effective amount of a composition comprising at least one indigo naturalis composition, beberine and a pharmaceutically acceptable carrier. | 08-28-2014 |
20140256746 | Methods for Treating Osteoarthritis - A method and composition for treating osteoarthritis with ion-channel regulators is disclosed. The ion-channel regulators are used alone or in combination with other osteoarthritis treatment agents, including but not limited to injectable agents such as viscosupplements and steroids. A composition comprising one or more ion-channel regulator(s) and one or more osteoarthritis treatment agent(s) is also disclosed. | 09-11-2014 |
20150290198 | MACROCYCLIC LRRK2 KINASE INHIBITORS - The present invention relates to novel macrocylic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease. | 10-15-2015 |
20150299221 | MACROCYCLIC PURINES FOR THE TREATMENT OF VIRAL INFECTIONS - This invention relates macrocyclic purine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections. | 10-22-2015 |
20150322084 | 11-(2-PYRROLIDIN-1-YL-ETHOXY)-14,19-DIOXA-5,7,26-TRIAZA-TETRACYCLO[19.3.1.- 1(2,6).1(8,12)]HEPTACOSA-1(25),2(26),3,5,8,10,12(27),16,21,23-DECAENE CITRATE SALT - The present invention relates to certain salts of a 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the citrate salt of this compound. The invention also relates to pharmaceutical compositions containing the citrate salt and methods of use of the citrate salt in the treatment of certain medical conditions. | 11-12-2015 |
20150336970 | MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS - Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R | 11-26-2015 |
20160002263 | Inhibitors of Human Immunodeficiency Virus Replication - The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. Formule (I) | 01-07-2016 |
20160009732 | DEUTERATED PACRITINIB | 01-14-2016 |
20160024114 | MACROCYCLIC RIP2 KINASE INHIBITORS - The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of RIP2 and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of RIP2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent. | 01-28-2016 |
20160075702 | NEW PYRIDOPYRIMIDINES DERIVATIVES COMPOUNDS - The present invention describes new pyridopyrimidine derivatives compounds with structure represented by General Formula (I): | 03-17-2016 |
20160375001 | MUSCARINIC COMBINATIONS AND THEIR USE FOR COMBATING HYPOCHOLINERGIC DISORDERS OF THE CENTRAL NERVOUS SYSTEM - A combination of a muscarinic cholinergic receptor agonist, a non-anticholinergic antiemetic agent and a non-selective, peripheral anticholinergic agent for the treatment of hypocholinergic disorders of the central nervous system. | 12-29-2016 |
20160375028 | ORGANIC COMPOUNDS - The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment of psychosis, schizophrenia, schizoaffective disorder, schizophreniform disorder, psychotic disorder, delusional disorder, mania, or bipolar disorder. | 12-29-2016 |