Entries |
Document | Title | Date |
20080207655 | Diaminopyrimidines as P2X3 and P2X2/3 modulators - Compounds of formula (I): | 08-28-2008 |
20080214588 | Hiv Inhibiting 2-(4-Cyanophenyl)-6-Hydroxylaminopyrimidines - HIV replication inhibitors of formula (I) pharmaceutically acceptable addition salts; or stereochemically isomeric forms thereof, wherein R | 09-04-2008 |
20080255167 | Novel 2-Aminopyrimidine or 2-Aminiopyridinone Derivatives and Their Use - This invention relates to novel compounds having the structural formula I below and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 10-16-2008 |
20080287475 | 4-(3-Aminopyrazole) Pyrimidine Derivatives for Use as Tyrosine Kinase Inhibitors in the Treatment of Cancer - This invention relates to novel compounds having the formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer. | 11-20-2008 |
20080318985 | Novel 2-Aminopyrimidinone Or 2-Aminopyridinone Derivatives and Their Use -
This invention relates to novel compounds having the structural formula Ia or Ib below: (Ia); (Ib) and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 12-25-2008 |
20090023762 | Substituted 2-Aminopyrimidine-4-Ones, Their Pharmaceutical Compositions And Their Use In The Treatment And/Or Prevention Of Ab-Related Pathologies - This invention relates to novel compounds having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel en compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 01-22-2009 |
20090030022 | Fungicidal Composition Comprising Cyprodinil - A fungicidal composition in the form of a liquid concentrate, which, in addition to at least one formulation adjuvant, comprises cyprodinil and an unsaturated C | 01-29-2009 |
20090048280 | Process for the preparation of substituted phenylalanines - Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g., of Formula I) are disclosed: | 02-19-2009 |
20090088447 | SOLID FORMS OF (S)-ETHYL 2-AMINO-3-(4-(2-AMINO-6-((R)-1-(4-CHLORO-2-(3-METHYL-1H-PYRAZOL-1-YL)PHEN- YL)-2,2,2-TRIFLUOROETHOXY)-PYRIMIDIN-4-YL)PHENYL)PROPANOATE AND METHODS OF THEIR USE - Solid forms of (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate and salts thereof are disclosed. | 04-02-2009 |
20090099217 | 2-Aminopyrimidin-4-Ones And Their Use For Treating Or Preventing Alpha Beta-Related Pathologies - This invention relates to novel compounds having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 04-16-2009 |
20090124644 | HIV INHIBITING 2-(4-CYANOPHENYLAMINO) PYRIMIDINE DERIVATIVES - HIV replication inhibitors of formula | 05-14-2009 |
20090124645 | Novel Pyrimidine-2,4-Diamine Derivatives and their Use as Modulators of Small-Conductance Calcium-Activated Potassium Channels - This invention relates to novel pyrimidine-2,4-diamine derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. | 05-14-2009 |
20090197903 | PROCESS FOR PREPARING SPRAY DRIED FORMULATION OF TMC125 - This invention relates to a process for producing a spray-dried powder comprising microcrystalline cellulose in a solid dispersion of the anti-HIV compound etravirine (TMC125) in a water-soluble polymer. | 08-06-2009 |
20090275599 | THERAPEUTIC OR PROPHYLACTIC AGENT FOR MULTIPLE SCLEROSIS - A therapeutic or prophylactic agent for multiple sclerosis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for multiple sclerosis according to the present invention shows the excellent absorbability and in vivo stability when orally administered, and exhibits high therapeutic or prophylactic effects. | 11-05-2009 |
20090286817 | 4-Phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-Based Compounds and Methods of Their Use - Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders: | 11-19-2009 |
20090318481 | Potentiators Of Glutamate Receptors - This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. | 12-24-2009 |
20100041684 | PYRIMIDYL DERIVATIVES AS PROTEIN KINASE INHIBITORS - Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer. | 02-18-2010 |
20100063077 | PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF AMYLOID-RELATED DISEASES - The present invention provides (I) These compounds are useful in prevention and treatment of neurodegenerative disorders, such as Alzheimer's, Parkinson's and Huntington's as well as type II diabetes. | 03-11-2010 |
20100076000 | SULFOXIMINE-SUBSTITUTED PYRIMIDINES AS CDK- AND/OR VEGF INHIBITORS, THEIR PRODUCTION AND USE AS PHARMACEUTICAL AGENTS - This invention relates to pyrimidine derivatives of general formula I | 03-25-2010 |
20100113490 | Substituted Pyrimidine Ether Compounds and use thereof - The invention relates to substituted pyrimidine ether compounds having general formula I: | 05-06-2010 |
20100152214 | NOVEL PYRIMIDINECARBOXAMIDE DERIVATIVES - This disclosure relates to novel HIV integrase inhibitors their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating HIV infections. | 06-17-2010 |
20100184787 | Heataryl-substituted guanidine compounds and use thereof as binding partners for 5-ht5-receptors - The invention relates to the hetaryl-substituted guanidine compounds of general formula (I), enantiomeres, diastereomeres and/or tautomeres thereof, in addition to the pharmaceutically acceptable salts thereof and the prodrugs of the known compounds. The invention also relates to the use of said hetaryl-substituted guanidine compounds as binding partners for 5-HT5-receptors for treating and/or for the prophylaxis of illnesses which are modulated by a 5-HT5-receptor activity, in particular, for treating and/or for the prophylaxis of neurodegenerative and neuropsychiatric disorders, and signs, symptoms and dysfunctions associated with said disorders. | 07-22-2010 |
20100190809 | COMBINATION FORMULATIONS - This invention relates to solid oral dosage forms of the HIV inhibitors containing a combination of TMC114 and TMC125. | 07-29-2010 |
20100240683 | COMBINATION THERAPY, COMPOSITION AND METHODS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS - The present invention relates to a combination therapy for the treatment of cardiovascular disorders. More particularly, the invention relates to compositions combining long-chain optionally substituted amphipatic carboxylates (known as MEDICA drugs) and particularly, M16αα, M16ββ and M18γγ, with HMG-CoA reductase inhibitors (known as statins). The compositions of the invention may particularly be used for the treatment of cardiovascular disorders, for elevating HDL-cholesterol levels, decreasing non-HDL-cholesterol and particularly triglycerides, and decreasing insulin resistance in a subject suffering from Metabolic Syndrome or cardiovascular disorders. The invention further provides methods of treatment of such disorders using these combined compositions. | 09-23-2010 |
20100240684 | MINOXIDIL AQUEOUS COMPOSITION CONTAINING BILE ACID - An object of the present invention is to provide a liquid composition wherein minoxidil can be dissolved at a relatively high concentration (the saturating amount or above), stimulation of skin and stickiness is suppressed without containing an organic solvent, and excellent effects of percutaneous absorption is achieved. The present invention provides a liquid composition comprising (i) minoxidil, (ii) bile acid or a salt thereof, and (iii) an aqueous medium in an amount of 30% by weight or more of the weight of the composition. | 09-23-2010 |
20100267754 | INTEGRIN EXPRESSION INHIBITOR - The present invention provides an integrin expression inhibitor, and an agent for treating arterial sclerosis, psoriasis, cancer, retinal angiogenesis, diabetic retinopathy or inflammatory diseases, an anticoagulant, or a cancer metastasis suppressor on the basis of an integrin inhibitory action. Namely, it provides an integrin expression inhibitor comprising, as an active ingredient, a sulfonamide compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate of them, | 10-21-2010 |
20100280054 | MULTICYCLIC AMINO ACID DERIVATIVES AND METHODS OF THEIR USE - Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders: | 11-04-2010 |
20100292260 | 6-VINYL PYRIMIDINE AND PYRIMIDINONE DERIVATIVES AND THE USE THEREOF - The invention relates to 6-vinyl pyrimidine pyrimidinone derivatives and the use thereof as medicaments in particular for the treatment of HTV infections, the use thereof for preparing pharmaceutical compositions and methods for the preparation thereof. | 11-18-2010 |
20110082161 | POWDERS FOR RECONSTITUTION - This invention relates to drinkable formulations prepared from powders for reconstitution comprising etravirine (TMC125) dispersed in certain water-soluble polymers, which can be used in the treatment of HIV infection. | 04-07-2011 |
20110092526 | Adamantyl Iminocarbonyl-Substituted Pyrimidines As Inhibitors Of 11-Beta-HSD1 826 - A compound of formula (I): | 04-21-2011 |
20110124667 | METHODS FOR THE TREATMENT OF IRRITABLE BOWEL SYNDROME - Methods of treating irritable bowel syndrome (IBS) are disclosed. Assays and kits useful in the treatment of IBS are also disclosed. | 05-26-2011 |
20110207758 | Methods for Therapeutic Renal Denervation - Methods for therapeutic renal denervation are disclosed herein. One aspect of the present application, for example, is directed to methods that block, reduce and/or inhibit renal sympathetic nerve activity to achieve a reduction in central sympathetic tone. Renal sympathetic nerve activity may be altered or modulated along the afferent and/or efferent pathway. The achieved reduction in central sympathetic tone may carry several therapeutic benefits across many disease states. | 08-25-2011 |
20110224243 | FZD2 Molulators in the Treatment of Alopecia - An in vitro method for screening candidate compounds for the preventive or curative treatment of alopecia is described. The method can include determining the capacity of a compound to modulate the expression or the activity of a Frizzled 2 (FZD2) transmembrane receptor. Also described, is the use of modulators of the expression or the activity of the transmembrane receptor for the treatment of alopecia. Methods for the in vitro diagnosis or prognosis of this pathology are also described. | 09-15-2011 |
20110263625 | HIV REPLICATION INHIBITING PYRIMIDINES - This invention concerns the use of compounds of formula | 10-27-2011 |
20110281899 | METHODS OF PREVENTING AND TREATING LOW BONE MASS DISEASES - The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists. | 11-17-2011 |
20110288109 | NEW COMPOUNDS - The present invention includes compounds of general Formula (1), wherein A, X, R | 11-24-2011 |
20110294837 | Aurora Kinase Modulators and Methods of Use - The present invention relates to chemical compounds having a general formula I | 12-01-2011 |
20110294838 | SULFOXIMINE-SUBSTITUTED ANILINOPYRIMIDINE DERIVATIVES AS CDK INHIBITORS, THE PRODUCTION THEREOF, AND USE AS MEDICINE - The invention relates to sulfoximine-substituted anilino-pyrimidine derivatives of formula (I). | 12-01-2011 |
20120028998 | CO-CRYSTAL OF ETRAVIRINE AND NICOTINAMIDE - Etravirine (TMC125) nicotinamide co-crystal, its preparation, and use in the treatment of HIV infection. | 02-02-2012 |
20120028999 | ADMINISTRATION OF TLR7 LIGANDS AND PRODRUGS THEREOF FOR TREATMENT OF INFECTION BY HEPATITIS C VIRUS - This invention relates to methods for treating or preventing hepatitis C virus infections in mammals using Toll-Like Receptor (TLR)7 ligands and prodrugs thereof. More particularly, this invention relates to methods of orally administering a therapeutically effective amount of one or more prodrugs of TLR7 ligands for the treatment or prevention of hepatitis C viral infection. Oral administration of these TLR7 immunomodulating ligands and prodrugs thereof to a mammal provides therapeutically effective amounts and reduced undesirable side effects. | 02-02-2012 |
20120035195 | 1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS - This invention relates to compounds of the formula | 02-09-2012 |
20120041008 | 4-Phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-Based Compounds and Methods of Their Use - Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders: | 02-16-2012 |
20120059021 | COMPOSITIONS AND METHODS FOR TREATING CANCER AND METHODS FOR PREDICTING A RESPONSE TO SUCH TREATMENTS - The present disclosure relates to the regulation and function of the Wnt/β-catenin signaling pathway and the ERK signaling pathway. The disclosure provides methods of treatment for melanoma by administering both an inhibitor of ERK signaling and an activator of Wnt/β-catenin signaling. These methods may be used alone or in combination with other strategies targeting melanoma cell survival. The disclosure also provides diagnostic methods for predicting a patient's clinical response to inhibitors of ERK signaling. | 03-08-2012 |
20120077831 | METHODS AND ASSAYS FOR THE TREATMENT OF IRRITABLE BOWEL SYNDROME - Methods of treating irritable bowel syndrome (IBS) are disclosed. Assays and kits useful in the treatment of IBS are also disclosed. | 03-29-2012 |
20120122904 | SOLID FORMS OF (S)-2-AMINO-3-(4-(2-AMINO-6-((R)-1-(4-CHLORO-2-(3-METHYL-1H-PYRAZOL-1-YL)- PHENYL)-2,2,2-TRIFLUOROETHOXY)PYRIMIDIN-4-YL)PHENYL)PROPANOIC ACID - Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid and salts thereof are disclosed. Pharmaceutical dosage forms and methods of their use are also disclosed. | 05-17-2012 |
20120149722 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 06-14-2012 |
20120157484 | TRYPTOPHAN HYDROXYLASE INHIBITORS - Compounds of formulae I and II are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and manage serotonin-mediated diseases and disorders: | 06-21-2012 |
20120208834 | PROCESS FOR PREPARING SPRAY DRIED FORMULATIONS OF 4-[[6-AMINO-5-BROMO-2-[(4-CYANOPHENYL)AMINO]-4-PYRIMIDINYL]OXY]-3,5-DIMET- HYLBENZONITRILE - This invention relates to a process for producing a spray-dried powder comprising microcrystalline cellulose in a solid dispersion of the anti-HIV compound etravirine (TMC125) in a water-soluble polymer. | 08-16-2012 |
20120220611 | 1,3-BENZOXAZOLYL DERIVATIVES AS KINASE INHIBITORS - Compounds of the formula I, the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases that are caused, mediated and/or propagated by angiogenesis. Compounds of the formula I are effective inhibitors of tyrosine kinases, in particular TIE-2 and VEGFR, and of Raf kinases. (I) | 08-30-2012 |
20120232102 | Methods Of Administration And Treatment - The present invention is directed to methods of administering pazopanib or pharmaceutically acceptable salts or solvates thereof as well as methods of treating cancer and age-related macular degeneration in patients in need thereof. | 09-13-2012 |
20120270889 | COMPOUND, CERTAIN NOVEL FORMS THEREOF, PHARMACEUTICAL COMPOSITIONS THEREOF AND METHODS FOR PREPARATION AND USE - Compound of Formula A and pharmaceutically acceptable salts thereof and crystalline Forms I and II of Compound of Formula A! Also, methods for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods for their uses. | 10-25-2012 |
20120316188 | PREPARATION OF 4-AMINO-THIAZOLES AND 3-AMINO-1,2,4-THIADIAZOLES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to novel compounds of Formula (I), wherein M, P, X, A and (B) | 12-13-2012 |
20130005754 | SOLID FORMS OF (S)-ETHYL 2-AMINO-3-(4-(2-AMINO-6-((R)-1-(4-CHLORO-2-(3-METHYL-1H-PYRAZOL-1-YL)PHEN- YL)-2,2,2-TRIFLUOROETHOXY)-PYRIMIDIN-4-YL)PHENYL)PROPANOATE AND METHODS OF THEIR USE - Solid forms of (S)-ethyl 2-amino-3 -(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate and salts thereof are disclosed. | 01-03-2013 |
20130053409 | 2-(2,4,5-SUBSTITUTED-ANILINO) PYRIMIDINE COMPOUNDS - The present invention relates to certain 2-(2,4,5-substituted-anilino)pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exon19 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof. | 02-28-2013 |
20130059871 | PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF AMYLOID-RELATED DISEASES - The present invention provides (I) these compounds are useful in prevention and treatment of neurodegenerative disorders, such as Alzheimer's, Parkinson's and Huntington's as well as type II diabetes. | 03-07-2013 |
20130096148 | PROCESS FOR ETRAVIRINE INTERMEDIATE AND POLYMORPHS OF ETRAVIRINE - 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-benzonitrile is a key intermediate for the preparation of etravirine. The present invention provides a process for preparation of 4-[[6-chloro-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile. The present invention also provides a novel process for the preparation of etravirine crystalline form I. The present invention further provides novel crystalline forms of etravirine, processes for their preparation and pharmaceutical compositions comprising them. | 04-18-2013 |
20130150389 | Etravirine Formulations and Uses Thereof - Provided herein is a pharmaceutical formulation of etravirine, said formulation comprising: etravirine; a dipolar aprotic solvent; a non-ionic water dispersible surfactant; and water. Further provided is a pharmaceutical formulation of etravirine, said formulation comprising: etravirine; a non-ionic water dispersible surfactant; and water. | 06-13-2013 |
20130150390 | THERAPEUTIC OR PROPHYLACTIC AGENT FOR ALLERGIC DERMATITIS - A therapeutic or prophylactic agent for allergic dermatitis is disclosed. The therapeutic or prophylactic agent comprises as an effective ingredient a glycine derivative having a specific structure or a pharmaceutically acceptable salt thereof, for example, the below-described compound [(E)-2-(2,6-dichlorobenzamido)-5-[4-(isopropyl-pyrimidin-2-ylamino)phenyl]pent-4-enoic acid]. The therapeutic or prophylactic agent for allergic dermatitis according to the present invention has high therapeutic or prophylactic effect. | 06-13-2013 |
20130172376 | SOLID DOSAGE FORMS OF (S)-ETHYL 2-AMINO-3-(4-(2-AMINO-6-((R)-1-(4-CHLORO-2-(3-METHYL-1H-PYRAZOL-1-YL)PHEN- YL)-2,2,2-TRIFLUOROETHOXY)PYRIMIDIN-4-YL)PHENYL)PROPANOATE - Solid pharmaceutical dosage forms comprising (S)-ethyl 2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoate (telotristat) are disclosed, as well as methods of making them and compositions useful in their manufacture. | 07-04-2013 |
20130178489 | METHOD FOR FUNGICIDAL AND/OR BACTERICIDAL TREATMENT OF RESISTANT STRAINS USING ESSENTIAL OIL(S) - The present invention relates to a method for fungicidal and/or bactericidal treatment of plants or foodstuffs using one or more essential oil(s) that enable the treatment of strains resistant to synthetic fungicides and/or bactericides. | 07-11-2013 |
20130178490 | PEST CONTROLLING COMPOSITION AND METHOD FOR CONTROLLING PEST - The present invention provides a composition having an excellent controlling activity on a pest. The composition comprising a compound represented by Formula (1) and one or more carbamate compound(s) selected from Group (A) shows an excellent controlling activity on a pest. Group (A): a group consisting of alanycarb, aldicarb, aldoxycarb, bendiocarb, benfuracarb, carbaryl, carbofuran, carbosulfan, cloethocarb, ethiofencarb, fenobucarb, fenothiocarb, fenoxycarb, furathiocarb, isoprocarb, metolcarb, methomyl, methiocarb, oxamyl, pirimicarb, pro poxur, XMC, thiodicarb and xylylcarb | 07-11-2013 |
20130210846 | USE OF NOVEL PAN-CDK INHIBITORS FOR TREATING TUMORS - The invention relates to the use of selected sulfoximine-substituted anilinopyrimidine derivatives of the formula (I) for treating tumors. | 08-15-2013 |
20130225618 | AGENT FOR INHIBITING EXPRESSION OF LIPID METABOLISM RELATED MRNA - The present invention is intended to provide a pharmaceutical product for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the present invention is also intended to provide a preventive and/or therapeutic agent for various diseases based on inhibition of expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and the present invention relates to an agent for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and relates also to a preventive and/or therapeutic agent for various diseases based on the inhibition of the expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the agent comprising a compound represented by Formula (I), its salt, or a solvate of any of them as an active ingredient: | 08-29-2013 |
20130338176 | METHODS OF PREVENTING AND TREATING HYPERLIPIDEMIA OR ATHEROSCLEROSIS - The present invention provides methods and therapeutic agents for lowering serum or plasma serotonin levels in a patient in order to prevent or treat hyperlipidemia or atherosclerosis. In preferred embodiments, the patient is known to have, or to be at risk for, hyperlipidemia or atherosclerosis and the agents are TPH1 inhibitors. | 12-19-2013 |
20130338177 | Spiro-Amino-Imidazolone and Spiro-Amino-Dihydro-Pyrimidinone Compounds as Beta-Secretase Modulators and Methods of Use - The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I), wherein variables A | 12-19-2013 |
20140005212 | Substituted Pyridines as Sodium Channel Blockers | 01-02-2014 |
20140038993 | NEW COMPOUNDS - The present invention includes compounds of general formula ( | 02-06-2014 |
20140045871 | PROCESS FOR SYNTHESIS OF PHENOXY DIAMINOPYRIMIDINE DERIVATIVES - A method for preparing a compound of formula k | 02-13-2014 |
20140051715 | 3,5 Phenyl-Substituted Beta Amino Acid Derivatives as Integrin Antagonists - Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: | 02-20-2014 |
20140148474 | AMINOPYRIMIDINES AS SYK INHIBITORS - The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis and cancer. | 05-29-2014 |
20140179720 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 06-26-2014 |
20140200232 | COMPOUND, CERTAIN NOVEL FORMS THEREOF, PHARMACEUTICAL COMPOSITIONS THEREOF AND METHODS FOR PREPARATION AND USE - Compound of Formula A and pharmaceutically acceptable salts thereof and crystalline Forms I and II of Compound of Formula A! Also, methods for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods for their uses. | 07-17-2014 |
20140200233 | USE OF MAD2L2 AS A STRATIFICATION MARKER IN THE TREATMENT OF BREAST TUMOURS WITH NOVEL PAN-CDK INHIBITORS - The invention relates to the use of MAD2L2 as stratification marker in the treatment of breast tumours with novel pan-CDK inhibitors of the formula (I). | 07-17-2014 |
20140221408 | PESTICIDAL PYRIMIDINE COMPOUNDS - Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description. | 08-07-2014 |
20140249169 | 1-PYRAZOLYL-3- (4- ((2 -ANILINOPYRIMIDIN- 4 - YL) OXY) NAPTHTHALEN- 1- YL) UREAS AS P38 MAP KINASE INHIBITORS - There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD. | 09-04-2014 |
20140256756 | PIPERIDINYL-SUBSTITUTED LACTAMS AS GPR119 MODULATORS - Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X | 09-11-2014 |
20140296271 | KINASE INHIBITOR - There is provided a compound of formula I, | 10-02-2014 |
20140303197 | METHODS OF TREATING AND PREVENTING LEUKEMIA AND OTHER CANCERS OF THE BLOOD AND BONE - The present invention relates to preventing and treating leukemia and other cancers of the blood and bone, as well as disorders of the blood, by inhibiting gut-derived serotonin. The inhibition of the gut-derived serotonin is accomplished by inhibiting Tph1, an enzyme responsible for the production of gut-derived serotonin. The present invention also relates to preventing and treating leukemia and other cancers of the blood and bone, as well as disorders of the blood, by increasing the number, growth and proliferation of osteoblasts. | 10-09-2014 |
20140303198 | AGENT FOR INHIBITING EXPRESSION OF NPC1L1 AND/OR LIPG MRNA AND AGENT FOR PREVENTING AND/OR TREATING OBESITY - Provided is an agent for treating and/or preventing obesity. An agent for suppressing expression of NPC1L1 (Niemann-Pick disease, type C1, gene-like 1) and/or LIPG (Lipase, endothelial) mRNA, and an agent for preventing and/or treating obesity, each comprising, as an active ingredient, a compound having CETP inhibitory activity, or a salt thereof, or a solvate thereof. | 10-09-2014 |
20140336208 | 1,4,5,6-TETRAHYDRO-PYRIMIDIN-2-YLAMINE COMPOUNDS - This invention relates to compounds of the formula | 11-13-2014 |
20140378488 | 4-SUBSTITUTED-(3-SUBSTITUTED-1H-PYRAZOLE-5-AMINO)-PYRIMIDINE DERIVATIVES HAVING ACTIVITY OF INHIBITING PROTEIN KINASE AND USE THEREOF - Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds. | 12-25-2014 |
20140378489 | METHODS OF PREVENTING AND TREATING DIABETES BY INHIBITING SEROTONIN SYNTHESIS - The present invention provides methods and therapeutic agents for lowering serum or plasma serotonin levels in a patient in order to prevent or treat diabetes. In preferred embodiments, the patient is known to have, or to be at risk for, diabetes and the agents are TPH1 inhibitors. | 12-25-2014 |
20150011574 | (2-HETEROARYLAMINO) SUCCINIC ACID DERIVATIVES - The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by the formula (1) wherein R | 01-08-2015 |
20150051232 | USE OF (RS)-S-CYCLOPROPYL-S-(4--5-(TRIFLUOROMETHYL)PYRIMIDIN-2-YL]AMINO}PH- ENYL)SULFOXIMIDE FOR TREATING SPECIFIC TUMOURS - The invention relates to the use of (R)—S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulphoximide and/or (S)—S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulphoximide for the treatment of specific tumours. | 02-19-2015 |
20150057299 | Methods of Using Diaminopyrimidine P2X3 and P2X 2/3 Receptor Modulators for Treatment of Acute and Sub-Acute Cough, Urge to Cough and Chronic Cough, in Respiratory Diseases - Methods for treating cough, chronic cough and urges to cough associated with respiratory diseases with a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of Formula (I): | 02-26-2015 |
20150065530 | BIOMARKER ASSOCIATED WITH IRRITABLE BOWEL SYNDROME AND CROHN'S DISEASE - The present invention provides compositions and methods for characterizing irritable bowel syndrome. In particular, the present invention provides compositions and methods for determining polymorphisms associated with IBS-D and Crohn's disease. The present invention further provides compositions and methods for determining a treatment course of action in subjects with IBS-D and Crohn's disease. | 03-05-2015 |
20150111908 | METHODS OF DIAGNOSING, PREVENTING, AND TREATING BONE MASS DISEASES - The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists. | 04-23-2015 |
20150141446 | PESTICIDAL PYRIMIDINE COMPOUNDS - Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description. | 05-21-2015 |
20150148358 | NOVEL DGAT2 INHIBITORS - The present invention provides compounds of the Formula below: | 05-28-2015 |
20150306098 | AGENT FOR INHIBITING EXPRESSION OF LIPID METABOLISM RELATED MRNA - The present invention is intended to provide a pharmaceutical product for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the present invention is also intended to provide a preventive and/or therapeutic agent for various diseases based on inhibition of expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and the present invention relates to an agent for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and relates also to a preventive and/or therapeutic agent for various diseases based on the inhibition of the expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the agent comprising a compound represented by Formula (I), its salt, or a solvate of any of them as an active ingredient: | 10-29-2015 |
20150320748 | AGENT FOR INHIBITING EXPRESSION OF LIPID METABOLISM RELATED MRNA - The present invention is intended to provide a pharmaceutical product for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the present invention is also intended to provide a preventive and/or therapeutic agent for various diseases based on inhibition of expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and the present invention relates to an agent for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and relates also to a preventive and/or therapeutic agent for various diseases based on the inhibition of the expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the agent comprising a compound represented by Formula (I), its salt, or a solvate of any of them as an active ingredient: | 11-12-2015 |
20150329496 | Cdc42 INHIBITOR AND USES THEREOF - Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyses of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demonstrate that the described compounds are able to inhibit all tested Cdc42-mediated processes. The compounds effectively inhibit the effects of Cdc42 and effectively Cdc42-related cellular functions involving actin, such as Golgi organization and cell movement. Furthermore, the described Cdc42 inhibitor compounds may be provided as a medicament for the treatment of various conditions. | 11-19-2015 |
20150376140 | 2-AMINOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS - This invention relates to 2-aminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections. | 12-31-2015 |
20160009695 | 1-PYRAZOLYL-3- (4- ((2 -ANILINOPYRIMIDIN- 4 - YL) OXY) NAPTHTHALEN- I - YL) UREAS AS P38 MAPKINASE INHIBITORS | 01-14-2016 |
20160016934 | KINASE INHIBITORS - There are provided compounds of formula I, | 01-21-2016 |
20160025751 | Lipidomic Biomarkers for Identification of High-Risk Coronary Artery Disease Patients - The present invention inter alia provides a method, and use thereof, of predicting severe CVD complications such as AMI or CVD death by detecting the lipid concentrations or lipid ratios of a biological sample and comparing it to a control and has identified specific lipid markers that are more specific and sensitive in predicting these CVD complications than currently utilized clinical markers. Also provided is an antibodies towards said lipids, and the use thereof for predicting, diagnosing, preventing and/or treating CVD complications. The invention additionally relates to kits comprising lipids and/or an antibody thereto, for use in the prediction and/or diagnosis of CVD complications. | 01-28-2016 |
20160031827 | NOVEL FORM OF PYRIMIDINE COMPOUND HAVING DIBENZYLAMINE STRUCTURE - It is an object of the present invention to provide a novel form of (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, which is useful for preventing and/or treating diseases such as dyslipidemia. | 02-04-2016 |
20160045496 | USE OF (RS)-S-CYCLOPROPYL-S-(4--5-(TRIFLUOROMETHYL)PYRIMIDIN-2-YL]AMINO}PH- ENYL)SULFOXIMIDE FOR TREATMENT OF SPECIFIC TUMOURS - The invention relates to the use of (R)-S-cyclopropyl-S-(4-{[4-{[(1R, 2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulphoximide and/or (S)-S-cyclopropyl-S-(4-{[4-{[(1R, 2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulphoximide for treating specific tumours. | 02-18-2016 |
20160130236 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 05-12-2016 |
20160168132 | DI(HETERO)ARYLAMIDES AND SULFONAMIDES, METHODS FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF | 06-16-2016 |
20180022696 | NOVEL N-ACYL-ARYLSULFONAMIDE DERIVATIVES AS AMINOACYL-TRNA SYNTHETASE INHIBITORS | 01-25-2018 |