Entries |
Document | Title | Date |
20080200444 | SOLUBLE EPOXIDE HYDROLASE INHIBITORS - Disclosed are urea compounds of formula I, stereoisomer, or pharmaceutical acceptable salts thereof, and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetic-related diseases. | 08-21-2008 |
20080207584 | Compound Having S1P Receptor Binding Potency and Use Thereof - Provided are: a compound represented by formula (I): | 08-28-2008 |
20080227767 | METHODS AND COMPOUNDS FOR INHIBITING AMYLOID DEPOSITS - Methods and compositions which are useful in the treatment of amyloidosis. In particular, methods and compositions are provided for inhibiting, preventing and treating amyloid deposition, e.g., in pancreatic islets, wherein the amyloidotic deposits are islet amyloid polypeptide (IAPP)-associated amyloid deposition or deposits. The methods of the invention involve administering to a subject a therapeutic compound which inhibits IAPP-associated amyloid deposits. Accordingly, the compositions and methods of the invention are useful for inhibiting IAPP-associated amyloidosis in disorders in which such amyloid deposition occurs, such as diabetes. | 09-18-2008 |
20080234247 | Heterocyclic analgesic compounds and methods of use thereof - One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics. | 09-25-2008 |
20080280867 | COMBINATION THERAPY WITH PARP INHIBITORS - The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with temozolomide (TMZ). | 11-13-2008 |
20080293684 | Heterocyclic Acetophenone Potentiators of Metabotropic Glutamate Receptors - The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved. | 11-27-2008 |
20080293685 | SPIRO AND OTHER DERIVATIVES OF DIAMONDOIDS POSSESSING THERAPEUTIC ACTIVITY IN THE TREATMENT OF VIRAL DISORDERS - This invention relates to diamondoid derivatives which exhibit therapeutic activity. Specifically, the diamondoid derivatives herein exhibit therapeutic effects in the treatment of viral disorders. Also provided are methods of treatment, prevention and inhibition of viral disorders in a subject in need. | 11-27-2008 |
20080293686 | SEMI-SOLID SYSTEMS CONTAINING AZETIDINE DERIVATIVES - The present invention relates to novel formulations of azetidine derivatives for oral administration comprising at least one azetidine compound of formula (Ia) or (Ib): | 11-27-2008 |
20080312205 | METHOD AND INTERMEDIATES FOR THE PREPARATION OF DERIVATIVES OF N (1-BENZHYDRYLAZETIDIN-3-YL)-N-PHENYLMETHYLSULFONAMIDE - The invention relates to a novel method for the synthesis of N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5-difluorophenyl)methylsulfonamide. | 12-18-2008 |
20090029962 | 2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS - The present invention relates to compounds of formula I | 01-29-2009 |
20090042851 | SULFONAMIDE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF AS ANTAGONISTS OF OREXIN 2 RECEPTORS - The present invention is directed to a compound of formula (I): | 02-12-2009 |
20090048223 | Sulfonamide compound - A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G | 02-19-2009 |
20090048224 | COMPOUNDS AND METHODS OF USE - Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. | 02-19-2009 |
20090093451 | IL-8 Receptor Antagonists - This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). | 04-09-2009 |
20090170824 | Diarylsulfones as 5-HT2A Antagonists - Compounds of formula I: | 07-02-2009 |
20090197856 | ANTIVIRAL COMPOUNDS - Provided are compounds of Formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds and compositions are useful for treating viral infections caused by the Flaviviridae family of viruses. | 08-06-2009 |
20090197857 | CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING METABOLIC DISORDERS, INCLUDING OBESITY AND DIABETES - The present invention provides novel substituted amino-azetidines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof. | 08-06-2009 |
20090203663 | CHEMICAL COMPOUNDS - The present invention relates to compounds that inhibit a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins. | 08-13-2009 |
20090253669 | Substituted Sulfonamide Compounds - Substituted sulfonamide compounds corresponding to the formula I: | 10-08-2009 |
20090253670 | AMIDE DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS AND METHODS OF USE THEREOF - The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions. | 10-08-2009 |
20090264398 | METHOD FOR INDUCING TUMOR APOPTOSIS BY INCREASING NITRIC OXIDE LEVELS - The present invention refers to a method for inducing tumor apoptosis by influencing the ROS (reactive oxygen species) signaling pathway in tumor cells. Increasing the level of ROS leads to the selective inactivation of a tumor cell catalase and subsequently to an apoptosis of these cells. The level of ROS can be increased by increasing the level of nitric oxide through inhibition of the enzymes nitric oxide dioxygenase or arginase. | 10-22-2009 |
20090281072 | Diaminopyrimidinecarboxamide Derivative - A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. | 11-12-2009 |
20090291935 | X-NITRO COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF AND USES THEREOF - The present invention provides X-nitro compound, pharmaceutical compositions of X-nitro compounds and methods of using X-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease. | 11-26-2009 |
20090306037 | Combination of a Dipeptidyl Peptidase-IV Inhibitor and a Cannabinoid CB1 Receptor Antagonist for the Treatment of Diabetes and Obesity - The present invention relates to pharmaceutical compositions comprising a combination of a particular dipeptidyl peptidase-IV (DPP-IV) inhibitor and a particular cannabinoid CB?1#191 receptor antagonist/inverse agonist, kits containing such combinations and methods of using such compositions for the treatment of diabetes, diabetes associated with obesity, diabetes-related disorders, obesity, and obesity-related disorders. | 12-10-2009 |
20100016272 | HETEROARYLACRYLAMIDES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to heteroarylacrylamides of the formula I, | 01-21-2010 |
20100022501 | INJECTABLE OR ORALLY DELIVERABLE FORMULATIONS OF AZETIDINE DERIVATIVES - The invention concerns injectable or orally deliverable binary or ternary formulations of azetidine derivatives. The azetidine derivatives used in the inventive pharmaceutical compositions can be represented by the general formulae (Ia) or (Ib), wherein Ar is an aromatic or heteroaromatic group optionally substituted by one or more among (C | 01-28-2010 |
20100063021 | Modulators of muscarinic receptors - The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases. | 03-11-2010 |
20100075941 | PREVENTIVE/REMEDY FOR RETINAL NERVE DISEASES CONTAINING ALKYL ETHER DERIVATIVES OR SALTS THEREOF - An alkyl ether derivative represented by the following general formula [1] | 03-25-2010 |
20100087414 | METHOD AND INTERMEDIATES FOR THE PREPARATION OF DERIVATIVES OF N (1-BENZHYDRYLAZETIDIN-3-YL)-N-PHENYLMETHYLSULFONAMIDE - The invention relates to a novel method for the synthesis of N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5 -difluorophenyl)methylsulfonamide. | 04-08-2010 |
20100113409 | Hydrochloride salt of 5-[3-(3-hydroxyphenoxy) azetidin-1-yl]-5-methyl-2,2-diphenylhexanamide - This invention relates to the hydrochloride salt of 5-[3-{3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenyl-hexanamide or derived form thereof and its use as a medicament. | 05-06-2010 |
20100125058 | NAPHTHYLACETIC ACIDS - The invention is concerned with the compounds of formula I: | 05-20-2010 |
20100160279 | Azetidine Derivatives as Muscarinic Receptor Antagonists - The invention relates to compounds of formula (I) processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical compositions containing them. | 06-24-2010 |
20100222316 | INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME - The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action. | 09-02-2010 |
20100227844 | CANNABINOID-1 RECEPTOR MODULATORS USEFUL FOR THE TREATMENT OF ALZHEIMER'S DISEASE - The present invention relates to methods of treating Alzheimer's Disease and Alzheimer's Disease related disorders comprising administration of a compound of structural formula: (I), or a pharmaceutically acceptable salt thereof, as a monotherapy or in combination with an anti-Alzheimer's Disease agent. The present invention further provides for pharmaceutical compositions, medicaments, and kits useful in carrying out these methods. | 09-09-2010 |
20100234340 | Substituted Spiroamide Compounds - Substituted spiroamide compounds corresponding to formula (I): | 09-16-2010 |
20100261696 | SULFONYL-AZETIDIN-3-YL-METHYLAMINE AMIDE ANALOGS AS GLYT1 INHIBITORS, METHODS FOR MAKING SAME, AND USE OF SAME IN TREATING PSYCHIATRIC DISORDERS - In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (G1yT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (G1yT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 10-14-2010 |
20100279996 | NOVEL ANALGESIC THAT BINDS FILAMIN A - A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula I, wherein R | 11-04-2010 |
20100279997 | ANALGESIC THAT BINDS FILAMIN A - A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R | 11-04-2010 |
20100279998 | PIPERIDINYLALKYLCARBAMATE DERIVATIVES, METHODS FOR THEIR PREPARATION AND THE THERAPEUTIC USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS - The present invention relates to piperidinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of a large variety of diseases and other pathological conditions are not generated and the incidence of the disease is greatly reduced. | 11-04-2010 |
20100286109 | AMIDE DERIVATIVES AS POSITIVE ALLOSTERIC MODULATORS AND METHODS OF USE THEREOF - The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions. | 11-11-2010 |
20110053903 | PHARMACEUTICAL COMPOSITIONS BASED ON AZETIDINE DERIVATIVES - A stable pharmaceutical composition comprising azetidine compound of formula (Ib): | 03-03-2011 |
20110071124 | Compounds that Inhibit Production of sAPPB and AB and Uses Thereof - The present invention relates to compounds with activity as inhibitors of sAPPβ and Aβ production, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease and pharmaceutical compositions containing such candidate compounds. | 03-24-2011 |
20110077231 | COMPOUNDS - Novel compounds, with the following being exemplary: | 03-31-2011 |
20110195947 | METHODS OF SYNTHESIZING AND ISOLATING N-(BROMOACETYL)-3,3-DINITROAZETIDINE AND A COMPOSITION INCLUDING THE SAME - A method of synthesizing and isolating N-(bromoacetyl)-3,3-dinitroazetidine (ABDNAZ) by reacting DNAZ with bromoacetyl bromide and boron trifluoride etherate to produce a mixture comprising ABDNAZ and a salt of DNAZ. Water and a solvent are added to the mixture to form an organic phase comprising the ABDNAZ and an aqueous phase comprising the salt of DNAZ. The organic phase and the aqueous phase are separated to produce an ABDNAZ/solvent solution comprising the ABDNAZ and the aqueous phase comprising the salt of DNAZ. A nonsolvent is added to the ABDNAZ/solvent solution to produce an ABDNAZ/solvent/nonsolvent mixture. The ABDNAZ is subsequently recovered. A composition comprising ABDNAZ is also disclosed. | 08-11-2011 |
20110207709 | MODULATORS OF SEROTONIN RECEPTOR - Certain biphenyl compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases. | 08-25-2011 |
20110257148 | NOVEL 1-ALKYL-3-HYDROXY-3-PHENYLAZETIDINE DERIVATIVES USEFUL AS MODULATORS OF CORTICAL CATECHOLAMINERGIC NEUROTRANSMISSION - The present invention relates to novel 3-phenyl-azetidine derivatives, useful for modulating dopamine neurotransmission and extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically for the treatment of central nervous system disorders. In other aspects the invention relates to pharmaceutical compositions comprising the 3-phenyl-azetidine derivatives of the invention and to the use of these compounds for therapeutic applications. X is OH; R | 10-20-2011 |
20110263556 | New Compounds - This invention relates to compounds of formula I, | 10-27-2011 |
20110281835 | NOVEL 3-PHENYL-AZETIDINE DERIVATIVES USEFUL AS MODULATORS OF CORTICAL CATECHOLAMINERGIC NEUROTRANSMISSION - The present invention relates to novel 3-phenyl-azetidine derivatives, useful for modulating extracellular levels of catecholamines, dopamine and norepinephrine, in cerebral cortical areas of the mammalian brain, and more specifically for the treatment of central nervous system disorders. In other aspects the invention relates to pharmaceutical compositions comprising the 3-phenyl-azetidine derivatives of the invention and to the use of these compounds for therapeutic applications. | 11-17-2011 |
20110294775 | NOVEL COMPOUNDS - Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases. The following is exemplary: | 12-01-2011 |
20120004206 | INHIBITORS OF THE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 ENZYME - The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action. | 01-05-2012 |
20120004207 | THERAPEUTIC USES OF DERIVATIVES OF PIPERIDINYL-AND PIPERIDINYL-ALKYL CARBAMATES - Compound corresponding to the general formula (I): | 01-05-2012 |
20120022039 | NOVEL SUBSTITUTED INDANES, METHOD FOR THE PRODUCTION THEREOF, AND USE THEREOF AS DRUGS - The invention relates to substituted indanes and derivatives thereof, to physiologically acceptable salts and physiologically functional derivatives thereof, to the production thereof, to drugs containing at least one substituted indane according to the invention or derivative thereof, and to the use of the substituted indanes according to the invention and to derivatives thereof as MCH antagonists. | 01-26-2012 |
20120040947 | TETRALINE AND INDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to tetraline and indane derivatives of the formula (I) | 02-16-2012 |
20120088746 | AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME - Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others. | 04-12-2012 |
20120094971 | Compositions Including 6-Aminohexanoic Acid Derivatives As HDAC Inhibitors - This invention relates to compounds of Formula (I) wherein Cy | 04-19-2012 |
20120142659 | COMPOUNDS AND THEIR USE AS IKACH BLOCKERS - The invention relates to compounds according to Formula I: | 06-07-2012 |
20120202781 | INDANE DERIVATIVES - The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease. | 08-09-2012 |
20120302539 | TRANSGLUTAMINASE TG2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF - Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents. | 11-29-2012 |
20130059829 | TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS - A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-β-hydroxysteroid dehydrogenase Type 1 enzyme activity. | 03-07-2013 |
20130116227 | BIARYL AMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF - Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R | 05-09-2013 |
20130123229 | CB1 Receptor Antagonists and Uses Thereof - Neutral antagonists of the CB1 cannabinoid receptor, means for identifying neutral antagonists of the CB1 cannabinoid receptor, and uses thereof. Antagonists of the CB1 cannabinoid receptor can be used to prevent, treat or reduce the severity of various medical conditions and symptoms, including, but not limited to obesity, appetite disorder, another metabolic disorder, drug addiction and/or mental illness. Administering neutral CB1 cannabinoid receptor antagonists in place of or in combination with known CB1 cannabinoid receptor antagonists or inverse CB1 cannabinoid receptor agonists in an individual or animal to treat a medical condition with a reduction of unwanted side effects. A method of detecting a neutral CB1 cannabinoid receptor antagonist, including identifying a candidate compound; subjecting the candidate compound to one or more of a cAMP assay, CB1 competitive binding assay, food intake assay, thermoregulation assay, or emesis assay; and selecting the compound if it exhibits neutral antagonist activity. | 05-16-2013 |
20130131034 | DERIVATIVES OF AMINOINDANES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS - The instant invention relates to derivatives of formula (I) | 05-23-2013 |
20130143858 | COMPOUNDS AND THEIR USE AS IKACH BLOCKERS - The invention relates to compounds according to Formula I: | 06-06-2013 |
20130203727 | NAPHT-2-YLACETIC ACID DERIVATIVES TO TREAT AIDS - The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I). | 08-08-2013 |
20130231319 | Bridged Spiro[2.4]heptane Ester Derivatives - The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method. | 09-05-2013 |
20130237513 | AZETIDINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPY - The invention relates to azetidine derivatives having the formula (I): | 09-12-2013 |
20130261099 | Fatty Acid Inhibitors - Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein. | 10-03-2013 |
20130324514 | INDANYLOXYPHENYLCYCLOPROPANECARBOXYLIC ACIDS - The present invention relates to compounds of general formula I, | 12-05-2013 |
20140018341 | METHOD OF INHIBITING TAU PHOSPHORYLATION - A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. | 01-16-2014 |
20140038934 | MODULATORS OF SEROTONIN RECEPTORS - Certain biphenyl compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases. | 02-06-2014 |
20140066420 | HETEROCYCLIC COMPOUND - The present invention relates to | 03-06-2014 |
20140094445 | SUBSTITUTED (E)-N'-(1-PHENYLETHYLIDENE)BENZOHYDRAZIDE ANALOGS AS HISTONE DEMETHYLASE INHIBITORS - In one aspect, the invention relates to substituted (E)-N′-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 04-03-2014 |
20140094446 | Cyclic Amino Acids for the Treatment of Pain - Compositions comprising cyclic amino acids or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. Said compositions are for use in the treatment of pain. Pain includes both acute and chronic forms of pain. The preferred cyclic amino acid is 1-aminocyclobutane-1-carboxylic acid (ACBC). | 04-03-2014 |
20140128360 | NOVEL MODULATORS OF CORTICAL DOPAMINERGIC- AND NMDA-RECEPTOR-MEDIATED GLUTAMATERGIC NEUROTRANSMISSION - The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission. 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. | 05-08-2014 |
20140128361 | CYCLIC AMIDE BACE-1 INHIBITORS HAVING A BENZAMIDE SUBSTITUENT - Disclosed are compounds of the formula | 05-08-2014 |
20140179660 | N1-Cyclic Amine-N5-Substituted Phenyl Biguanide Derivatives, Methods of Preparing the Same and Pharmaceutical Composition Comprising the Same - An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome. | 06-26-2014 |
20140179661 | N1-Cyclic Amine-N5-Substituted Biguanide Derivatives, Methods of Preparing the Same and Pharmaceutical Composition Comprising the Same - A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome. | 06-26-2014 |
20140256698 | CATHEPSIN INHIBITORS - The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors. | 09-11-2014 |
20140288040 | SUBSTITUTED BENZYLAMINE COMPOUNDS, THEIR USE IN MEDICINE, AND IN PARTICULAR THE TREATMENT OF HEPATITIS C VIRUS (HCV) INFECTION - The invention provides compounds of the formula (6): | 09-25-2014 |
20140309206 | AMINOINDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to aminoindane derivatives of the formula (I) | 10-16-2014 |
20140315877 | NICOTINIC RECEPTOR NON-COMPETITIVE ANTAGONISTS - The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions. | 10-23-2014 |
20150025054 | (HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS - The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. | 01-22-2015 |
20150038480 | COMPOUNDS THAT MODULATE AUTOIMMUNITY AND METHODS OF USING THE SAME - The invention provides methods of preventing, treating or ameliorating autoimmune diseases, such as diabetes and celiac disease, by decreasing the binding of MHC class II molecules to antigenic peptides or fragments of antigenic peptides of the autoimmune disease by the administration of small organic compounds. The invention also provides pharmaceutical compositions comprising the therapeutically effective small organic compounds and methods of using the same. | 02-05-2015 |
20150072969 | PHENYL ALKANOIC ACID DERIVATIVES AS GPR AGONISTS - The present invention relates to phenyl alkanoic acid derivatives (the compounds of Formula (I)); and their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs, N-oxides, S-oxides or carboxylic acid isosteres thereof. The invention also relates to processes for the preparation of compounds of Formula (I) | 03-12-2015 |
20150322002 | N-SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF - The invention provides novel compounds having the general formula (I) and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X | 11-12-2015 |
20160008323 | NICOTINIC RECEPTOR NON-COMPETITIVE ANTAGONISTS | 01-14-2016 |
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