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Tricyclo ring system having the five-membered hetero ring as one of the cyclos

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514359000 - Five-membered hetero ring containing at least one nitrogen ring atom (e.g., 1,2,3-triazoles, etc.)

514408000 - The five-membered hetero ring consists of one nitrogen and four carbons

514410000 - Polycyclo ring system having the five-membered hetero ring as one of the cyclos

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Entries
DocumentTitleDate
20100063126Carbazole-Derived Pharmaceutical Compositions - The present invention relates to the use of specific carbazole derivatives in the preparation of medicaments for the treatment, prevention and/or amelioration of disorders relating to pathological processes in lipid rafts.03-11-2010
20080293800Cytotoxic Compounds and Conjugates - The present disclosure provides cytoxic compounds useful as drugs or prodrugs and to drug-cleavable substrate conjugates where the drug and cleavable substrate are optionally linked through a self-immolative linker.11-27-2008
20110196012DEUTERATED MACROCYCLIC INHIBITORS OF VIRAL NS3 PROTEASE - This invention relates to novel macrocyclic protease inhibitors and their pharmaceutically acceptable salts thereof. This invention also provides compositions comprising at least one compound of this invention and the use of such compositions in methods of treating a flavivirus infection or liver fibrosis in a patient in need thereof.08-11-2011
20100076047Amorphous 1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-p- ropanol phosphate salt - The present invention relates to a novel amorphous form of 1-(9H-carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-2-propanol phosphate (Carvedilol dihydrogen phosphate) of Formula (I), and a process for the preparation thereof.03-25-2010
20100076048Isoindol Derivatives As EP4 Receptor Agonists - The present invention relates to indole derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.03-25-2010
20130041007Selective Androgen Receptor Modulators - This invention provides compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and or salts thereof, pharmaceutical compositions comprising a compound of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type II diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of Formula (I), (Ia), (Ib), (Ic), (II), (IIa) or (III) and intermediates useful in the preparation of same.02-14-2013
20100041728HCV INHIBITING MACROCYCLIC PHENYLCARBAMATES - Compounds of the formula 1:02-18-2010
20080287518Use of a Benzoyl Derivative of 3-Aminocarbazole For the Treatment of a Disorder Associated With the Production of Prostaglandin E2 (Pge2) - Use of a benzoyl derivative of 3-aminocarbazole to produce a drug for the preventive or therapeutic treatment of a disorder selected form the group comprising inflammatory processes, pain, fever, tumours, Alzheimer's disease and atherosclerosis. Method for the preventive or therapeutic treatment of a disorder selected from the group comprising inflammatory processes, pain, fever, tumours, Alzheimer's disease and atherosclerosis in which a therapeutically effective quantity of a benzoyl derivative of 3-aminocarbazole according to the invention is administered to an individual.11-20-2008
20130046005TREATMENT OF IMMUNE DISORDERS USING KAINATE RECEPTOR ANTAGONISTS - Allergies and immune system disorders (e.g. autoimmune diseases) are treated by administration of an agent that blocks activation of the kainic acid receptor (KAR) in B cells. The agents include antagonists and weakly activating agonists.02-21-2013
20090306167Pharmaceutical Compositions for Intranasal Administration Comprising a Melatonin Receptor Agonist, Uses Thereof - The present invention relates to intranasally deliverable compositions comprising melatonin receptor agonists and to methods of using such compositions in the treatment of various diseases and disorders.12-10-2009
20090306168SirT Inhibitors That Bind to NAD - Compound of formula (I)12-10-2009
20090093533COMPOUNDS AND METHODS FOR INHIBITING HEPATITIS C VIRAL REPLICATION - Macrocyclic compounds having the structures described herein are useful for inhibiting replication of the hepatitis C virus (HCV). In preferred embodiments, the compounds are active against both the NS3 protease and the NS3 helicase of HCV.04-09-2009
20090270476PHARMACEUTICAL COMPOSITION FOR TREATMENT OR PREVENTION OF NEPHRITIS AND MANUFACTURING METHOD THEREOF - A pharmaceutical composition for treatment of nephritis of the present invention comprises a triprenylphenol compound as an active substance, preferably the triprenylphenol compound represented by the following general formula (1) as an active substance, and further preferably orniplabin represented as n=3 in the following general formula (1) as an active substance.10-29-2009
20100069457Naphthalene Derivatives Used As EP4 Receptor Agonists - A compound of formula (I) or a pharmaceutically acceptable derivative thereof,03-18-2010
20110021594Agents Useful for Reducing Amyloid Precursor Protein and Treating Dementia and Methods of Use Thereof - The present invention provides compounds and methods of administering compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease βAPP production.01-27-2011
20090069399DEUTERIUM-ENRICHED FROVATRIPTAN - The present application describes deuterium-enriched frovatriptan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-12-2009
20090048324ALTERNATE MORPHEEIN FORMS OF ALLOSTERIC PROTEINS AS A TARGET FOR THE DEVELOPMENT OF BIOACTIVE MOLECULES - A composition having an agent adapted to affect a multimeric protein by binding to a binding site of the multimeric protein and thereby affecting an equilibrium of units, wherein the multimeric protein has an assembly having a plurality of said units, wherein each of the units has a first complementary surface and a second complementary surface and wherein the first complementary surface of one unit is associated with the second complementary surface of another unit, provided that the assembly is at least one of different quaternary isoforms on a condition that in the multimeric protein (1) a structure of each of the units determines a structure of the different quaternary isoforms, (2) the units are in the equilibrium and (3) the structure of the different quaternary isoforms influences a function of the multimeric protein.02-19-2009
20090286844Carvedilol phosphate - The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical compositions comprising the novel amorphous and crystalline forms and uses thereof.11-19-2009
20100029737INHIBITORS OF D-AMINO ACID OXIDASE - The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.02-04-2010
20110144176MACROLIDES AND METHODS FOR PRODUCING SAME - This invention relates, in part, to macrolide compounds, actinomycete strains for producing them, and pharmaceutical compositions containing them.06-16-2011
20080207726Process for the purification of carvedilol or its salts thereof - The present invention provides processes for reducing bis impurities ((1,1′-[2-(2-methoxyphenoxy)ethyl]iminobis-[3-(9H-carbazol-4-yloxy)]-propan-2-ol)), in particular Bis 1 and Bis 2, in carvedilol preparations. The process may comprise (a) combining carvedilol base with phosphoric acid in ethanol to obtain a reaction mixture; and (b) precipitating carvedilol phosphate from the reaction mixture, where the carvedilol phosphate comprises low levels of Bis 1 and Bis 2.08-28-2008
20100152268STABLE ATORVASTATIN FORMULATIONS - The present invention provides novel alternative pharmaceutical compositions comprising amorphous atorvastatin or a pharmaceutically acceptable salt thereof and a controlled amount of one or more additional compounds selected from the group consisting of compounds of formula I (formed by ring opening of the epoxide of Formula II to form a diketo dihydroxy derivative), II (diketo epoxide derivative), III (di-epoxide derivative formed by ring closure of the heptanoic acid chain to form a cyclohexanoate substituent), IV (2-oxo derivative with the isopropyl group rearranged to the 3-position) and V (phenantrene derivative of the 2-oxo derivative), together with one or more suitable pharmaceutical excipients, which compositions have improved stability.06-17-2010
20110172283Tricyclic Indeno-Pyrrole Derivatives as Serotonin Receptor Modulators - The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).07-14-2011
20090076117DEUTERIUM-ENRICHED LAROPIPRANT - The present application describes deuterium-enriched laropiprant, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20090312388Benzo [F] Isoindoles As EP4 Receptor Agonists - The present invention relates to naphthalene derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine.12-17-2009
20090286845Carvedilol phosphate - The invention encompasses novel amorphous and crystalline forms of carvedilol phosphate, carvedilol hydrogen phosphate, and carvedilol dihydrogen phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical compositions comprising the novel amorphous and crystalline forms and uses thereof.11-19-2009
20100120884USE OF DITHIINE-TETRACARBOXIMIDES FOR CONTROLLING PHYTOPATHOGENIC FUNGI - The present invention relates to the use of novel and of known dithiine-tetracarboximides for controlling phytopathogenic fungi, and to methods of controlling phytopathogenic fungi in plant protection, and to plant protection compositions comprising these dithiine-tetracarboximides.05-13-2010
20100081699YEAST PLATFORM CONSTRUCTION AND SCREENING METHODS - The present invention relates to a cell which is suitable for screening a candidate agent as being an inhibitor of the metabolism of tryptophan to NAD+ and/or a modulator of NAD+ levels, which cell comprises functional genes of a pathway enabling the metabolism of tryptophan to NAD+ and wherein the cell includes a copy of an exogenous gene of said pathway, from the same or different species as the cell, which exogenous gene is under the control of an inducible or constitutive promoter and wherein any endogenous copy of the gene having the same function as the exogenous gene is a non functioning gene. The present invention also relates to populations of such cells and to methods of screening candidate agents with such cells.04-01-2010
20090170923HCV INHIBITORS - The present invention relates to compounds that are useful in the treatment of viruses belonging to Flaviviridae, including flaviviruses, pestiviruses, and hepaciviruses. The invention includes compounds useful for the treatment or prophylaxis of dengue fever, yellow fever, West Nile virus, and HCV.07-02-2009
20090286843MACROCYCLIC COMPOUNDS AS INHIBITORS OF VIRAL REPLICATION - The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.11-19-2009
20090291997CARVEDILOL DIHYDROGEN PHOSPHATE MONOHYDRATE - Disclosed herein is crystalline carvedilol dihydrogen phosphate monohydrate having high aqueous solubility and the process for preparation thereof. The invention further discloses methods for treating hypertension, congestive heart failure and angina in a mammal, using pharmaceutical compositions comprising the compound of invention.11-26-2009
20120295946Agents Useful for Reducing Amyloid Precursor Protein and Treating Dementia and Methods of Use Thereof - The present invention provides compounds and methods of administering compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease βAPP production.11-22-2012
20080280965Novel tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCPs) - The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.11-13-2008
20100280090TAPE PREPARATION COMPRISING ETODOLAC IN IONIC LIQUID FORM - Disclosed is a tape preparation comprising etodolac in an ionic liquid form, which has high transdermal absorbability. Etodolac is reacted with an organic amine compound to produce an ionic liquid of etodolac. By using the ionic liquid, it becomes possible to increase the transdermal absorbability of etodolac. Further for the purpose of enhancing the transdermal absorbability and the tissue penetration ability of an ionic solution of etodolac, the composition of an organic solvent system for the ionic solution of etodolac is investigated, and it is found that a mixed solvent of an alcohol and an ester (1:2 to 2:1) is suitable as the organic solvent. Still further, an appropriate adhesion force can be achieved by properly selecting a softening agent. In this manner, a tape preparation having good transdermal absorbability can be prepared. The tape preparation can exert its pharmacological efficacy rapidly, and is therefore extremely effective for the teatment of a chronic pain such as rheumatoid arthritis, osteoarthritis and lumbago, an inflammatory diseases such as shoulder periarthritis and tendovaginitis, cervical syndrome, a pain induced by a surgery or an injury, or the like.11-04-2010
20080293799Liver Function Ameliorant - The present invention relates to a liver function ameliorant containing orniplabin as an active ingredient thereof.11-27-2008
20120295947PROCESSES FOR THE PREPARATION OF (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMETHYL)BENZYLOXY)-1,2,3,4-TETRAHYDROC- YCLOPENTA[B]INDOL-3-YL)ACETIC ACID AND SALTS THEREOF - The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (Ia) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).11-22-2012
20090156656USE OF LIGHT-ACTIVE INDOCYANINE GREEN FOR TREATING INFLAMMATORY DISORDERS IN THE ORAL CAVITY - In a process for treating disorders, especially inflammatory disorders, in the oral cavity, by introducing a substance activable by a light source, the substance comprises the active ingredient indocyanine green and the spectrum of the light source emits significant proportions in the range of 700-1000 nm.06-18-2009
20090082417DEUTERIUM-ENRICHED SDX-101 - The present application describes deuterium-enriched SDX-101, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-26-2009
20090005429PROCESS FOR THE PREPARATION OF CARVEDILOL AND ITS ENANTIOMERS - The present invention relates to a process for the preparation of carvedilol as well as of the optically active R and S enantiomers thereof and of mixtures of these enantiomers and, more particularly, relates to an improved process for the preparation of carvedilol and its enantiomers characterized by the use of ethyl acetate as reaction solvent.01-01-2009
20090118349BIS-ALKYLATING AGENTS AND THEIR USE IN CANCER THERAPY - The present invention relates to (i) conjugates comprising two DNA alkylating subunits linked by a moiety fitting to the minor groove of the DNA, (ii) to their preparation and (iii) to their use in cancer therapy. The alkylating subunits are especially cytotoxic under hypoxic conditions found in cancer cells. The compounds of the present invention and compositions thereof are useful in the treatment of cancer in a mammal, both alone or in a combination with other anti-cancer agents (e.g. checkpoint abrogators) and/or radiation. They may also be used as cytotoxic units for gene-directed enzyme-prodrug therapy (GDEPT) and antibody-directed enzyme-prodrug therapy (ADEPT).05-07-2009
20080319042Compositions and methods for treatment of liver disease - The present invention comprises compositions and methods for the treatment of liver disease, particularly treatments for infection by HCV and/or HBV. The present invention comprises antiviral compositions comprising lamiridosin, derivatives of lamiridosin or iridoids that are effective in inhibiting one or more steps in the infection of cells by HCV or HBV. Methods for treating subjects, particularly humans, infected with HCV or HBV are provided.12-25-2008
20090326033Carvedilol - This invention relates to an improved process of preparing carvedilol, as well as a new crystalline hydrate and solvate and forms of carvedilol, processes for the manufacture thereof, and pharmaceutical compositions thereof.12-31-2009
20080262069CARVEDILOL PHOSPHATE SALTS AND/OR SOLVATES THEREOF, CORRESPONDING COMPOSITIONS, AND/OR METHODS OF TREATMENT - The present invention relates to carvedilol phosphate salts, which include novel crystalline forms of carvedilol dihydrogen phosphate (i.e., dihydrogen phosphate salt of 1-(carbazol-4-yloxy-3-[[2-(o-methoxyphenoxy) ethyl]amino]-2-propanol) and/or carvedilol hydrogen phosphate, etc.), and/or solvates thereof, compositions containing the aforementioned salts and/or solvates, and methods of using the aforementioned salts and/or solvates to treat hypertension, congestive heart failure and angina, etc.10-23-2008
201101441781 ,6-DIHYDRO-2H-3-OXA-6-AZA-AS-INDACENE COMPOUNDS - The invention provides new compounds of formula (I) wherein R06-16-2011
20090239925TRICYCLIC INDENO-PYRROLE DERIVATIVES AS SEROTONIN RECEPTOR MODULATORS - The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).09-24-2009
20090118347Method of Treating Down Syndrome - A method of, or the use of compounds of the invention for, treating the cognitive impairments associated with Down syndrome, the method or use comprising treating or administering to a person with an effective amount of phenserine and isomers thereof or a pharmaceutically acceptable salt and derivatives thereof.05-07-2009
20090048325Prophylactic or Therapeutic Agent for Irritable Bowel Syndrome - The present invention provides a prophylactic or therapeutic agent for irritable bowel syndrome, which comprises a compound represented by formula (I):02-19-2009
201100600253-AMINOCARBAZOLE COMPOUND, PHARMACEUTICAL COMPOSITION CONTAINING IT AND PREPARATION METHOD THEREFOR - The present invention relates to novel benzoyl derivatives of 3-aminocarbazole, to a pharmaceutical composition containing them, to a method for preparing them and to the use of such compounds for the production of a drug that is useful in the treatment or prevention of disturbances associated with the production of prostaglandin E03-10-2011
20110060024Modulators of ATP-Binding Cassette Transporters - Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.03-10-2011
20090076116DEUTERIUM-ENRICHED CARVEDIOLO - The present application describes deuterium-enriched carvedilol, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20110112163CBI DERIVATIVES SUBJECT TO REDUCTIVE ACTIVATION - A unique class of N-acyl O-amino phenol prodrugs of CBI-TMI and CBI-indole05-12-2011
20090281158PRODRUGS OF CC-1065 ANALOGS - Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.11-12-2009
20090318523BENZOISOINDOLE DERIVATIVES AND THEIR USE AS EP4 RECEPTOR AGONISTS - The present invention relates to benzoisoindole phenylacetic acid derivatives, corresponding pharmaceutical compositions, preparation processes and uses in medicine as EP4 receptor angonists.12-24-2009
20110015247NOVEL CRYSTALLINE FORM OF CARVEDILOL DIHYDROGEN PHOSPHATE AND RELATED PROCESSES - The present patent application relates to a novel crystalline form (Form S) of Carvedilol dihydrogen phosphate and a process for its preparation. It also relates to an improved process for the preparation of Carvedilol dihydrogen phosphate.01-20-2011
20110144177Carbamoyl Esters That Inhibit Cholinesterase And Release Pharmacologically Active Agents - Carbamoyl esters inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. In one embodiment, the carbamoyl ester has the following structure:06-16-2011
20120245212CONTROLLED RELEASE CARVEDILOL FORMULATION - A controlled release carvedilol formulation for less frequent, preferably once daily administration is described. The controlled release formulation comprises a therapeutically effective amount of carvedilol or a pharmaceutically acceptable salt thereof, a matrix forming polymer, a solubility enhancer and a pharmaceutically acceptable carrier. In one embodiment, a controlled release formulation having a therapeutically effective amount of carvedilol is contained in two or more subunits having different release profiles. The controlled release formulation is usable in the treatment and/or prophylaxis of one or more conditions such as cardiovascular disorders.09-27-2012
2010005660011BETA-HSD1 ACTIVE COMPOUNDS - A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.03-04-2010
20090030061Benzoisoindole Derivatives And Their Use As EP4 Receptor Ligands - A compound of formula (I) or a pharmaceutically acceptable derivative thereof,01-29-2009
20110152339FLUORESCENT REGULATORS OF RASSF1A EXPRESSION AND HUMAN CANCER CELL PROLIFERATION - The invention provides methods for the treatment of cancer in a subject comprising administering a dansyl-carbazole compound.06-23-2011
20120202868METHOD FOR TREATMENT OF BRONCHIAL ASTHMA - The present invention relates to a method for the treatment of bronchial asthma and chronic obstructive pulmonary disease (COPD) comprising administering to the patient suffering from asthama and COPD an effective dose of carbazole derivatives or salt thereof, optionally along with pharmaceutically acceptable excipients. 08-09-2012
20090118348DRUG-INTRODUCED PHOTO-CROSSLINKED HYALURONIC ACID DERIVED GEL - A drug-introduced photo-crosslinked hyaluronic acid derived gel which is a photo-crosslinked hyaluronic acid gel into which a drug is introduced through a covalent bond, and has characteristics that are capable of extruding from an injection device. The drug-introduced photo-cross-linked hyaluronic acid derived gel is capable of extruding, for example, by an injection needle of 20 to 25 gauge with a pressure of 0.5 to 5 kg/cm05-07-2009
20080214643FUSED HETEROCYCLIC SUCCINIMIDE COMPOUNDS AND ANALOGS THEREOF, MODULATORS OF NUCLEAR HORMONE RECEPTOR FUNCTION - Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.09-04-2008
20110118326Androgen Receptor Modulator and Uses Thereof - The present invention relates to the compound of the formula:05-19-2011
20090215852COMPOSITIONS AND METHODS FOR AMELIORATING CACHEXIA - The invention provides preparations, formulations, kits and other products of manufacture (e.g., blister packs) comprising combinations of beneficial ingredients that are serviceable as therapies for improving states and disease symptoms such as involving inflammation, excessive sympathoneural drive, cachexia, anorexia, and anorexia-cachexia, as well as stress or anxiety related thereto, and methods of making and using them. The invention provides compositions and therapies comprising use of a beta adrenergic antagonist (also called “beta blockers”, e.g., propranolol) in combination with an anti-inflammatory agent, e.g., a nonsteroidal anti-inflammatory drug (NSAID), an angiotensin-converting enzyme (ACE) inhibitor, an angiotensin receptor blocker (ARB), an anabolic steroid, a natural oil or fatty acid or any combination thereof.08-27-2009
20100298399Endothelin Single Nucleotide Polymorphisms and Methods of Predicting B-Adrenergic Receptor Targeting Agent Efficacy - The present invention concerns the use of methods for evaluating β-adrenergic receptor targeting agent treatment for a patient, particularly one with a heart condition. In general, the disclosed methods entail determining the presence or absence of one or more polymorphisms in an endothelin gene system member. Based on the results of this determination, a β-adrenergic receptor targeting agent may be prescribed, administered or a treatment regimen altered, including the administration of a β-blocker. Accordingly, methods of treatment are also described.11-25-2010
20090275630COSMETIC COMPOSITION COMPRISING AN IMIDOPERCARBOXYLIC ACID DERIVATIVE AND A N-ACYLATED AMINO ACID ESTER - Composition containing, in a physiologically acceptable medium, at least one imidopercarboxylic acid compound and at least one N-acylated amino acid ester of formula (A) as described herein.11-05-2009
20110201663BENZO (F) ISOINDOL-2-YLPHENYL ACETIC ACID DERIVATIVES AS EP4 RECEPTOR AGONISTS - A compound of formula (I) or a pharmaceutically acceptable derivative thereof,08-18-2011
20110218226ANTI-VIRULENCE COMPOSITIONS AND METHODS - A method of reducing the virulence of a bacterium that expresses accessory gene regulator A (AgrA) includes administering to the bacterium an amount of AgrA antagonist effective to inhibit the synthesis of one or more virulence factors by the bacterium.09-08-2011
20110152338CYCLOALKANE[B]INDOLE ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are compounds that are antagonists of PGD06-23-2011
20100286224METHOD OF TREATING AIRWAY DISEASES WITH BETA-ADRENERGIC INVERSE AGONISTS - The use of β-adrenergic inverse agonists provides a new and highly efficient way of treating a number of pulmonary airway diseases, including asthma, emphysema, and chronic obstructive pulmonary diseases. In general, such a method comprises administering a therapeutically effective amount of a β-adrenergic inverse agonist to the subject to treat the pulmonary airway disease. Particularly preferred inverse agonists include nadolol and carvedilol. In addition, methods are described for long-term administration of such inverse agonists and for determining the suitability of patients for long-term inverse agonist therapy.11-11-2010
20120041044PROCESS FOR THE PREPARATION OF CARVEDILOL AND ITS ENANTIOMERS - The present invention relates to a process for the preparation of carvedilol as well as of the optically active R and S enantiomers thereof and of mixtures of these enantiomers and, more particularly, relates to an improved process for the preparation of carvedilol and its enantiomers characterized by the use of ethyl acetate as reaction solvent.02-16-2012
20080269310Synergistic Combinations - This invention relates to synergistic combinations of non-steroidal anti10-30-2008
200802077273-Aminocarbazole Compounds, Pharmaceutical Composition Containing the Same and Method for the Preparation Thereof - A compound of formula (I), in which R1, R2, R3, R4, R5, R6, X and Y have the meanings indicated in the description, and the pharmaceutically acceptable salts thereof. A pharmaceutical composition containing a compound of formula (I) or a pharmaceutically acceptable salt thereof. A method for preparing the abovementioned compound of formula (I) and the pharmaceutically acceptable salts thereof.08-28-2008
20120172408ACTIVE INGREDIENT COMPRISING INDOCYANINE GREEN AND/OR INFRACYANINE GREEN - The present invention relates to an active ingredient including indocyanine green and/or infracyanine green for use in treating dental or periodontal infectious diseases under irradiation with light, more particularly laser light, from a wavelength range between 790 nm and 830 nm.07-05-2012
20110166195METHOD FOR THE FORMATION OF MEGAMITOCHONDRIA - The present invention relates to an in-vitro method for the formation of megamitochondria in cells, wherein the cells are grown in a suitable fermentation medium acidulated with lactic acid to pH values between 5.3 and 6.7. The invention further concerns H07-07-2011
20120115921FLUORO SUBSTITUTED CYCLOALKANOINDOLES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Fluoro substituted cycloalkanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.05-10-2012
20110092561BENZOISOINDOLE DERIVATIVES FOR THE TREATMENT OF PAIN - A compound of formula (I) or a pharmaceutically acceptable derivative thereof,04-21-2011
20080306132Novel oral compositions of carporen - An improved semisolid composition for an oral veterinary application and a method of making it. A carprofen paste composition is made for orally administering to animals using calibrated syringe dispensers for exact dosages.12-11-2008
20110065767Substituted CC-1065 Analogs and Their Conjugates - This invention relates to novel agents that are analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.03-17-2011
20090131501Agents Useful for Reducing Amyloid Precursor Protein and Treating Dementia and Methods of Use Thereof - The present invention provides compounds and methods of administering compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce βAPP production and that is not toxic in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease βAPP production.05-21-2009
20120252859Tricyclic Indeno-Pyrrole Derivatives as Serotonin Receptor Modulators - The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).10-04-2012
20100010063HETEROCYCLOCARBOXAMIDE DERIVATIVES - The invention relates to a fungicidally active compound of formula (I):01-14-2010
20120225923Dithiinetetra(thio)carboximides - The present invention relates to novel dithiinetetra(thio)carboximides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.09-06-2012
20120225922Effective Amounts of (3aR)-1,3a,8-Trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo [2,3-b]indol-5-yl Phenylcarbamate and Methods of Treating or Preventing Neurodegeneration - The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.09-06-2012
20120232122TRICYCLIC HETEROCYCLIC DERIVATIVES - The present invention relates to a tricyclic heterocyclic 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 pharmaceutical compositions comprising said tricyclic heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of serotonin mediated disorders, such as obesity.09-13-2012
201100461973-AMINOCARBAZOLE COMPOUNDS, PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AND METHOD FOR THE PREPARATION THEREOF - A method for treating an inflammatory process selected from the group consisting of oedema, erythema, articular inflammation, rheumatoid arthritis, arthrosis, a colorectal tumor, a pulmonary carcinoma, an adenocarcinoma, and combinations thereof, in a person in need thereof, the method comprising administering to the person in need thereof, in an amount sufficient to treat the inflammatory process, a 3-aminocarbazole or a salt thereof.02-24-2011
20120329848PROCESSES FOR THE PREPARATION OF S1P1 RECEPTOR MODULATORS AND CRYSTALLINE FORMS THEREOF - The present invention relates to salts, processes, and process intermediates useful in the preparation of (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid of Formula (Ia), salts, and crystalline forms thereof. The compound (R)-2-(9-chloro-7-(4-isopropoxy-3-(trifluoromethyl)benzyloxy)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetic acid has been identified as an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions eases characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).12-27-2012
20100130579CANCER THERAPY - The present invention relates to methods of inducing expression of an epigenetically silenced gene, RASSF1A, in cells, particularly human cells, such as cancer cells. It also relates to methods of treating an individual, prophylactically or therapeutically, for cancer in which RASSF1A is epigenetically silenced.05-27-2010
20110160270DEUTERIUM-ENRICHED SDX-101 - The present application describes deuterium-enriched SDX-101, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.06-30-2011
20080234352Controlled release solid dispersions - A controlled release pharmaceutical composition for oral use comprising a solid dispersion of i) at least one therapeutically, prophylactically and/or diagnostically active substance, which at least partially is in an amorphous form, ii) a pharmaceutically acceptable polymer that has plasticizing properties, and iii) optionally a stabilizing agent, the at least one active substance having a limited water solubility, and the composition being designed to release the active substance with a substantially zero order release. The polymer is typically a poly ethylene glycol and/or polyethylene oxide having a molecular weight of at least about 20,000 in crystalline and/or amorphous form or a mixture of such polymers, and the active substance is typically carvedilol. The composition may comprise a coated matrix, the coating comprising a first cellulose derivative which is substantially insoluble in the aqueous medium, and at least one of a) a second cellulose derivative which is soluble or dispersible in water, b) a plasticizer, and c) a filler.09-25-2008
20110319462Use of Dithiine-tetracarboximides for Controlling Phytopathogenic Fungi - The present invention relates to the use of novel and of known dithiine-tetracarboximides for controlling phytopathogenic fungi, and to methods of controlling phytopathogenic fungi in plant protection, and to plant protection compositions comprising these dithiine-tetracarboximides.12-29-2011

Patent applications in class Tricyclo ring system having the five-membered hetero ring as one of the cyclos