Entries |
Document | Title | Date |
20080207673 | Method for Treating Cancer, Coronary, Inflammatory and Macular Disease, Combining the Modulation of Zinc-and/or Copper Dependent Proteins - A method for treating diseases selected among cancer, coronary disease, inflammatory disease and macular disease by chelation therapy is disclosed. | 08-28-2008 |
20080214597 | Tricyclic Lactam Derivatives as 11-Beta Hydroxysteroid Dehydrogenase Inhibitors - the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein
| 09-04-2008 |
20080221145 | Pyrroloquinoline quinone drugs for treatement of cardiac injury and methods of use thereof - The invention includes compositions comprising substantially purified pyrroloquinoline quinone, that are useful in methods for the treatment and prevention of cardiac injury caused by hypoxia or ischemia. The invention also includes methods for the treatment and prevention of cardiac injury comprising contacting a composition of the invention with a human patient. | 09-11-2008 |
20080221146 | INHIBITORS OF NUCLEOPHOSMIN (NPM) AND METHODS FOR INDUCING APOPTOSIS - Nucleophosmin inhibitors are disclosed which inhibit the multimerization of nucleophosmin and the biological activity of nucleophosmin, such as the ability of nucleophosmin to inhibit apoptosis and inhibit cellular differentiation. These small molecule inhibitors are useful for treating diseases and disorders, such as cancer associated with dysregulated nucleophosmin expression. Methods for identifying small molecule inhibitors of nucleophosmin involving multimerization sites for nucleophosmin are also disclosed. An exemplary small molecule inhibitor of nucleophosmin is NSC348884 which has the following chemical structure: | 09-11-2008 |
20080234310 | Methods and Compositions for Slowing Aging - The present invention provides a pharmacological agent based on derivatives of hydrogenated pyrido (4,3-b) indoles and uses thereof. Specifically, the invention provides a geroprotector in the series of hydrogenated pyrido (4,3-b) indoles (several derivatives), which can be used for slowing aging, prolonging lifespan of an individual or cells in an individual, and/or improving quality of life of an individual developing or having a risk of developing age-associated manifestations and/or pathologies. | 09-25-2008 |
20080249125 | HETEROCYCLIC DERIVATIVES AS OREXIN ANTAGONISTS - The present invention relates to compounds of formula | 10-09-2008 |
20080262019 | Optical Isomers of (+) and (-)-Trans-2,3,4,4A,5,9B-Hexahydro-2,8-Dimethyl-1H-Pyrido[4,3-B] Indole - The present invention represents novel optical isomers produced according the invention that are optic antipodes to each other having individual biological activity which can be used as active ingredients in pharmaceutical compositions with nootropic and sedative activity for treatment of different individual conditions of patients. | 10-23-2008 |
20080262020 | 6-Heteroarylpyridoindolone Derivatives, Their Preparation and Therapeutic Use Thereof - The disclosure relates to compounds of formula (I): | 10-23-2008 |
20080280941 | 8-Phenoxy-Gamma Carboline Derivatives - Compounds of Formula I and corresponding pharmaceutical compositions are disclosed. | 11-13-2008 |
20080280942 | Tetrahydro-Beta-Carbolin-Sulfonamide Derivatives as 5-Ht6 Ligands - The present invention relates to new tetrahydro-β-carbolin-sulfonamide derivatives of general formula (I), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemates or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or corresponding physiologically acceptable salts or corresponding solvates. These compounds are suitable as pharmacologically active agents in a medicament for the prophylaxis and/or treatment of disorders or diseases related to 5-HT | 11-13-2008 |
20080280943 | METHODS AND PACKAGES TO ENHANCE SAFETY WHEN USING IMIQUIMOD TO TREAT CHILDREN DIAGNOSED WITH SKIN DISORDERS - Pharmaceutical packages and methods for enhancing the safety of imiquimod when used to treat children affected by skin disorders are disclosed. More particularly, the safety profile of imiquimod use is enhanced by providing information to the children, guardians of the children, including parents and health care professionals, that systemic absorption of imiquimod and other effects may be observed when imiquimod therapy is used to treat children of between about 2 and about 12 years of age. Examples of systemic absorption include a serum imiquimod concentrations of less than about 2 ng/mL, a decrease in median white blood cell count by about 1.4*10 | 11-13-2008 |
20080318997 | NOVEL 4-PHENYL SUBSTITUTED TETRAHYDROISOQUINOLINES AND THERAPEUTIC USE THEREOF - Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein. | 12-25-2008 |
20090018155 | METHODS OF TREATING DERMATOLOGICAL DISORDERS AND INDUCING INTERFERON BIOSYNTHESIS WITH SHORTER DURATIONS OF IMIQUIMOD THERAPY - Pharmaceutical formulations and methods for the topical and/or transdermal delivery of imiquimod, including creams, ointments and pressure-sensitive adhesive compositions to treat dermatological disorders, namely, viral infections, such as Type I or Type II Herpes simplex infections and genital warts, actinic keratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis, with shorter durations of therapy, than currently approved for imiquimod by the Food & Drug Administration (“FDA”). | 01-15-2009 |
20090030029 | Novel benzonaphthyridines - The compounds of formula I | 01-29-2009 |
20090042924 | Pyridoindolone Derivatives Substituted in the 3-position by a Heterocyclic Group, Their Preparation and Their Application in Therapeutics - The present disclosure relates to pyridoindolone derivatives of general formula (I): | 02-12-2009 |
20090062327 | Inhibitors of AKT Activity - The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 03-05-2009 |
20090069367 | METHODS FOR TREATMENT OF CANCER - A method for treating or preventing cancer in a subject comprising administering a treatment effective amount of a chemotype 4 compound. | 03-12-2009 |
20090093512 | 1, 2, 3, 3A, 8, 8A-HEXAHYDRO-2, 7A-DIADA-CYCLOPENTA[A]INDEN-7-ONE DERIVATIVES WHICH BIND TO NEURONAL NICOTINIC ACETYLCHOLINE SPECIFIC RECEPTOR SITES AND ARE USEFUL IN MODULATING CHOLINERGIC FUNCTION AND IN THE TREATMENT OF ADDICTIVE DISORDERS - The present invention relates to novel fused bicyclicpyrrolidine pyridone compounds of the formula (I) wherein R, R | 04-09-2009 |
20090093513 | Method to Use Compositions Having Antidepressant Anxiolytic and Other Neurological Activity and Compositions of Matter - The sponges were collected from a variety of locations in the Florida Keys and separated based on morphology and color. The samples were identified as three species, two of which are well known: | 04-09-2009 |
20090099226 | Quinoline derivatives as ep4 antagonists - The invention is directed to quinoline derivatives as prostaglandin E type receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. The derivatives have the following structure of formula (I): wherein A and B represents either a nitrogen atom or a CH group with the proviso that they cannot both simultaneously be CH, Q can represent a nitrogen or a carbon atom, and Y and Z are either a nitrogen atom, a N(O) group or a C(R | 04-16-2009 |
20090137622 | USE OF PYRROLOQUINOLINE COMPOUNDS TO KILL CLINICALLY LATENT MICROORGANISMS - There is provided the use of compounds of formula I | 05-28-2009 |
20090143419 | METHODS AND COMPOSITIONS FOR CONTROLLING ECTOPARASITES - A method of treating or preventing ectoparasite infestation in a plant or animal host is provided comprising applying an effective amount of at least one metalloprotease inhibitor and/or at least one metal chelating agent, wherein the metal chelating agent is a compound comprising at least two heteroatoms able to simultaneously coordinate with a metal ion, at least one of the two heteroatoms being selected from nitrogen, sulfur, oxygen and phosphorus, wherein the compound comprises at least one carbocyclic ring substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom, or the compound comprises at least one heterocyclic ring containing at least one heteroatom, wherein said heterocyclic ring is optionally substituted with at least one heteroatom and/or with a substituent containing at least one heteroatom. | 06-04-2009 |
20090156630 | ANTI-TUMOUR POLYCYCLIC CARBOXAMIDES - This invention relates to polycyclic carboxamide compounds of the formula I: | 06-18-2009 |
20090170891 | Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment - The present invention encompasses compounds of Formula I: | 07-02-2009 |
20090221627 | Fluoro-containing derivatives of hydrogenated pyrido[4,3-b]indoles with neuroprotective and cognition enhancing properties, process for preparing, and use - Some exemplary embodiments comprise fluoro-containing derivatives of pyrido[4,3-b]indoles (and exemplary methods of making the same) that may be administered to a mammal (including a human) in an effective amount for potential use in the treatment or prophylaxis of neurological disorders including AD, mild cognitive impairment, senile and vascular dementia, HD, ALS, Parkinson's disease, AIDS-related dementia, ischaemic cerebral pathologies, neuropathic pain, ADHD (attention deficit disorder/hyperactivity syndrome), eating disorders such as anorexia and bulimia, panic attacks, withdrawal from drug abuse such as cocaine, ethanol, nicotine and benzodiazepines, schizophrenia (in particular the cognitive deficit of schizophrenia), stroke and also disorders associated with spinal trauma and/or head injury. These derivatives may also be useful for the treatment of borderline personality disorder, obesity, and for use as geroprotectors. The compounds may also be used as “pharmacological tools” for an investigation of the mechanism of protection against neurodegeneration disorders in vivo or in vitro. | 09-03-2009 |
20090258892 | FUSED PYRAZOLE DERIVATIVES AND METHODS OF TREATMENT OF METABOLIC-RELATED DISORDERS THEREOF - The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. | 10-15-2009 |
20090258893 | FUSED QUINOLINE DERIVATIVE AND USE THEREOF - The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) | 10-15-2009 |
20090264457 | Combination of at least two 5HT6-Ligands - The present invention relates to a Combination of at least two 5HT6-Ligands of which one is a partial or agonist while the other is a full antagonist or an inverse agonist, a medicament comprising this comination, the use of the combiantion in the manufacture of a medicament for the treatment of memory disorders ADHD, and methods of treatment using the combination or its members. | 10-22-2009 |
20090270442 | POLYMORPHS OF HYDROCHLORIDE SALT OF 5-(3-(ETHYLSULFONYL)PHENYL)-3,8-DIMETHYL-N-(1-METHYLPIPERIDIN-4-YL)-9H-PY- RIDO[2,3-B]INDOLE-7-CARBOXAMIDE AND METHODS OF USE THEREFOR - Polymorphic forms of the hydrochloride salt of 5-(3-(ethylsulfonyl)phenyl)-3,8-dimethyl-N-(1-methylpiperidin-4-yl)-9h-pyrido[2,3-b]indole-7-carboxamide (referred to herein as Compound 1) which has the formula: | 10-29-2009 |
20090291976 | Neuronal circuit-dependent neuroprotection by interaction between nicotinic receptors - A method of inhibiting excitotoxicity by indirectly activating α4β2 nicotinic acetylcholine receptors (nAChRs) which indirectly activate synaptic AMPA and NMDA receptors is disclosed. Inhibitors of α7 nACHRs, such as macrocyclic diterpenoids, more specifically cembranoids or methyllycaconitine (MLA), indirectly activate α4β2 nAChRs and can be used to treat neurodegenerative diseases, including, but not limited to, Alzheimer's Disease, Parkinson Disease, AIDS related dementia and the delayed effects of stroke. They can also be used to treat diseases associated with neuronal impairment, including, but not limited to glaucoma caused by optical nerve damage, delayed effects of epilepsy; and multiple sclerosis. | 11-26-2009 |
20090318491 | Cytisine and Acetylcholine Analogs and Methods of Treating Mood Disorders - The present invention relates to compounds which are derivatives of cytisine or acetylcholine which exhibit activity as agonists, partial agonists or antagonists of nicotinic acetylcholine receptors and may be used in modulating these receptors and in treating mood disorders in patients in need of therapy. | 12-24-2009 |
20100022580 | NEW 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLE COMPOUNDS AND METHODS OF USE THEREOF - This disclosure relates to new tricyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds are described, including new 2,3,4,5-tetrahydro- | 01-28-2010 |
20100029706 | HYDROGENATED PYRIDO[4,3-b]INDOLES FOR THE TREATMENT OF OXIDATIVE STRESS - Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, and diseases of aging such as diabetes and cancer with hydrogenated pyrido[4,3-b]indoles such as dimebolin, are disclosed. | 02-04-2010 |
20100035912 | Small Molecule Inhibitors of Retroviral Assembly and Maturation - Chemical compounds that disrupt retroviral assembly and maturation are presented herein. More particularly, this disclosure provides small molecule compounds that disrupt the formation and maturation of virus particles and methods of using such small molecules to treat HIV-1 infection. | 02-11-2010 |
20100041691 | PHARMACEUTICAL COMPOSITIONS COMPRISING COMBINATIONS OF AN AMPA/KAINATE ANTAGONISTIC COMPOUND AND AN INHIBITOR OF A MULTIDRUG RESISTANCE PROTEIN - This invention relates to pharmaceutical compositions comprising a combination of an AMPA/kainate antagonistic compound and an inhibitor of a multidrug resistance protein and its use for combating epileptic disorders. | 02-18-2010 |
20100041692 | PYRROLO[4,3,2-DE]QUINOLIN-8-AMINE COMPOUNDS AND METHODS OF THEIR PREPARATION AND USE - The present invention relates to compounds of formula I: | 02-18-2010 |
20100048606 | 10-Substituted Cytisine Derivatives and Methods of Use Thereof - The present invention relates to substituted cytisine compounds that are useful in treating diseases impacted by a nicotinic ACh receptor. One aspect of the invention relates to 10-substituted cytisine compounds. In certain instances, the cytisine is substituted in the 10-position by an alkyl, aryl or aralkyl group. The present invention also relates to a pharmaceutical composition comprises the substituted cytisine compound or the 10-substituted cytisine compound. The invention also relates to a method of modulation a nicotinic ACh receptor in a mammal, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine. Another aspect of the present invention relates a method of treating a disease impacted by a nicotinic ACh receptor, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine. | 02-25-2010 |
20100063085 | METHOD OF TREATING LEARNING IMPAIRMENT IN DOWN'S SYNDROME SUBJECTS - The present invention provides compounds for use in the preparation of pharmaceutical formulations and medicaments, which alleviate learning and/or mental impairment in people suffering from Down's syndrome. | 03-11-2010 |
20100076011 | Enantiomer-Pure Hexahydro-Pyrrolocyclopenta-Pyridine Derivatives - The invention relates to the novel therapeutically valuable enantiomer-pure [3aα,8bα]-1,2,3a,4,8b-hexahydropyrrolocyclopentapyridine derivatives of the general formula (I), wherein Z is a single bond or CH | 03-25-2010 |
20100093780 | INSULIN RESISTANCE IMPROVING AGENT - An object of the present invention is to provide a safe and highly effective insulin resistance improving agent or therapeutic agent for type II diabetes. According to the present invention, an insulin resistance improving agent or a therapeutic agent for type II diabetes comprising a compound represented by general formula (I) | 04-15-2010 |
20100099700 | HYDROGENATED PYRIDO (4,3-B) INDOLES FOR TREATING AMYOTROPHIC LATERAL SCLEROSIS (ALS) - The invention provides methods for treating and/or preventing and/or slowing the onset and/or development of ALS using hydrogenated pyrido(4,3-b)indoles, such as dimebon. | 04-22-2010 |
20100105718 | NAPHTHALENE AND QUINOLINE SULFONYLUREA DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS - The invention is directed to naphthalene and quinoline sulfonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included. | 04-29-2010 |
20100113502 | Novel Tetrahydro-1H-Pyrido[4,3-b] Indole Derivatives as CB1 Receptor Ligands - Compounds of formulae I, or pharmaceutically acceptable salts thereof: wherein R | 05-06-2010 |
20100113503 | CYCLOALKANE[B]AZAINDOLE ANTAGONISTS OF PROSTAGLANDIN D2 RECEPTORS - Described herein are compounds that are antagonists of PGD | 05-06-2010 |
20100125085 | PYRIDOINDOLE MODULATORS OF NMDA RECEPTOR AND ACETYLCHOLINESTERASE - The present invention relates to new pyridoindole modulators of NMDA receptors, AMPA receptors, and/or L-type calcium channels, and/or inhibitors of acetylcholinesterase, pharmaceutical compositions thereof, and methods of use thereof. | 05-20-2010 |
20100130528 | ADAMANTANE MODULATORS OF NMDA RECEPTOR AND/OR 5HT3 RECEPTOR - The present invention relates to new adamantane modulators of NMDA receptors and/or 5HT3 receptors, pharmaceutical compositions thereof, and methods of use thereof. | 05-27-2010 |
20100137353 | TRICYCLIC COMPOUNDS AS ANTIBACTERIALS - Tricyclic nitrogen containing compounds and their use as antibacterials. | 06-03-2010 |
20100144778 | Niacin Receptor Agonists, Compositions Containing Such Compounds and Methods of Treatment - The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included. | 06-10-2010 |
20100144779 | Marine Alkalod Makaluvamines and Derivatives Thereof - The present disclosure provides compounds based on the marine alkaloid makaluvamine. Described are compounds of the general formula (I) and (II). Also described are pharmaceutical compositions comprising one or more of the compounds of the general formula (I) and (II). The compounds and pharmaceutical compositions described inhibit the growth of several cancer lines, induce apoptosis and cell cycle arrest, display topoisomerase II inhibitory activity and modulate the activity and/or expression of key proteins involved in the regulation of cell growth. Methods of treatment and prevention using the compounds and pharmaceutical compositions described are also provided. | 06-10-2010 |
20100152225 | HYDROGENATED PYRIDO [4,3-B] INDOLES SUCH AS DIMEBON FOR TREATING CANINE COGNITIVE DYSFUNCTION SYNDROME - The invention provides method for treating Cognitive Dysfunction Syndrome (CCDS), slowing the onset and/or development and/or progression of CCDS or preventing the development of CCDS in canines, such as dogs, using hydrogenated pyrido[4,3-b]indoles, including dimebon. | 06-17-2010 |
20100160367 | PHARMACEUTICAL COMPOSITIONS CONTAINING PYRROLOQUINOLINE QUINONE AND NEPHROPROTECTANT FOR TREATING ISCHEMIA REPERFUSION INJURIES - The invention includes compositions comprising substantially purified pyrroloquinoline quinone, that are useful in methods for the treatment and prevention of cardiac injury caused by hypoxia or ischemia. The invention also includes methods for the treatment and prevention of cardiac injury comprising contacting a composition of the invention with a human patient. | 06-24-2010 |
20100168152 | Fat regulation - The present invention provides methods and compounds for regulating fat metabolism and achieving fat homeostasis in a subject. Methods and compound for regulating body weight, reducing body fat, and inducing weight loss are also provided, as are methods and compounds for treating or preventing obesity and for preventing or treating conditions associated with altered fat metabolism including, e.g., obesity, diabetes, atherosclerosis, etc. | 07-01-2010 |
20100184799 | OXADIAZOLE BETA CARBOLINE DERIVATIVES AS ANTIDIABETIC COMPOUNDS - Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety. | 07-22-2010 |
20100190815 | HYPERTENSION-AMELIORATING AGENT - It is an objective of the present invention to provide a safe and highly effective hypertension-ameliorating agent. | 07-29-2010 |
20100190816 | KINASE INHIBITORS - Compounds, pharmaceutical compositions, kits and methods are provided for use with kinases that comprise a compound selected from the group consisting of: | 07-29-2010 |
20100197720 | HETEROARYL-SUBSTITUTED DIAZATRICYCLOALKANES AND METHODS OF USE THEREOF - The present invention relates to amide and urea derivatives of heteroaryl-substituted diazatricycloalkanes, pharmaceutical compositions including the compounds, methods of preparing the compounds, and methods of treatment using the compounds. More specifically, the methods of treatment involve modulating the activity of the α7 nAChR subtype by administering one or more of the compounds to treat or prevent disorders mediated by the α7 nAChR subtype. The diazatricycloalkanes typically consist of a 1-azabicyclooctane fused to pyrrolidine ring. The substituent heteroaryl groups are 5- or 6-membered ring heteroaromatics, such as 3-pyridinyl and 5-pyrimidinyl moieties, which are attached directly to the diazatricycloalkane. The secondary nitrogen of the pyrrolidine moiety is substituted with an arylcarbonyl (amide type derivative) or an arylaminocarbonyl (N-arylcarbamoyl) (urea type derivative) group. The compounds are beneficial in therapeutic applications requiring a selective interaction at certain nAChR subtypes. That is, the compounds modulate the activity of certain nAChR subtypes, particularly the α7 nAChR subtype, and do not have appreciable activity toward muscarinic receptors. Radiolabeled versions of the compounds can be used in diagnostic methods. | 08-05-2010 |
20100197721 | PYRROLO [3, 4-h] ISOQUINOLINE COMPOUNDS AND METHODS FOR MODULATING GATED ION CHANNELS - The present invention relates to compositions and methods to modulate the activity of gated ion channels. | 08-05-2010 |
20100216832 | Method for Assaying FTO (2-Oxoglutarate Dependent Oxygenase) Activity - The present invention provides a method for assaying oxygenase activity, the method comprising monitoring oxygenase activity of FTO. | 08-26-2010 |
20100216833 | TETRAHYDROCARBAZOLES AND DERIVATIVES - The present invention relates to compounds of the formula (I) | 08-26-2010 |
20100222377 | BIS-QUATERNARY AMMONIUM CYCLOPHANE COMPOUNDS THAT INTERACT WITH NEURONAL NICOTINIC ACETYLCHOLINE RECEPTORS - Provided are bis-quaternary ammonium cyclophane compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders. | 09-02-2010 |
20100240692 | [1,10]-PHENANTHROLINE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE OR HAEMATOLOGICAL DISEASES - The present invention relates to a new family of [1,10]-phenantroline derivatives of formula (I), which are useful for the treatment or profilaxis of a neurodegenerative or haematological disease or condition, their use as a medicament, especially for treating a treatment neurodegenerative or haematological disease or condition, and a pharmaceutical composition comprising the compounds. | 09-23-2010 |
20100261749 | METHOD OF PREVENTING OR AMELIORATING PSORIASIS USING PYRROLOQUINOLINE QUINONE COMPOUNDS - It is an object of the present invention to provide a safe and highly effective preventing or ameliorating agent for skin psoriasis. | 10-14-2010 |
20100286188 | MEANS FOR IMPROVING COGNITIVE FUNCTIONS AND MEMORY BASED ON HYDROGENATED PYRIDO(4,3-B)INDOLES (VARIANTS), PHARMACOLOGICAL MEANS BASED THEREON AND METHOD FOR THE USE THEREOF - A means for improving cognitive functions and memory based on hydrogenated pyrido (4,3-b) indoles (variants), a pharmacological means based thereon and a method for the use thereof relate to the use of chemical compounds in the field of medicine and may be used to extend the arsenal of means which can be utilized for substantial enhancement of memory and activation of the learning process, for the treatment of impaired cognitive functions and memory in the elderly and in mild cognitive impairment, in brain trauma, in chronic cerebrovascular insufficiency, in hypoxic encephalopathies, resulting from chronic alcoholism and in delayed development in children. Said task is resolved by the use of hydrogenated pyrido ([4, 3-b]) indoles of formula (1) or formula (2) as means for improving cognitive functions and memory. | 11-11-2010 |
20100331357 | PHARMACEUTICAL COMPOSITION - The present invention provides a pharmaceutical composition, wherein solubility and stability of a water-insoluble or slightly water-soluble compound represented by formula (I): wherein each symbol is as defined in the specification, are improved, by combination of the above-mentioned compound and a cyclodextrin derivative and a method for improving solubility, stability and the like of the above-mentioned compound. | 12-30-2010 |
20110021554 | IMMUNE RESPONSE MODIFIER FORMULATIONS AND METHODS - An aqueous parenteral pharmaceutical formulation of the IRM drug compound N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin- | 01-27-2011 |
20110046174 | KAPPA-OPIATE AGONISTS FOR THE TREATMENT OF DIARRHEA-PREDOMINANT IRRITABLE BOWEL SYNDROME - The present invention concerns methods useful in treating a subject having diarrhea-predominant IBS (IBS-D) by administering N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide and/or a pharmaceutically acceptable salt thereof to the subject. | 02-24-2011 |
20110059999 | Hydroxymethylcyclohexylamines - The invention relates to compounds which have an affinity for the μ opioid receptor and the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments. | 03-10-2011 |
20110092534 | Ammosamides as Anticancer Agents - A compound having the general the general structure I is provided: (Formula I), wherein Z is a substituent selected from a group consisting of S and O; X is a substituent selected from a group consisting of Cl, Br, I, OH and NH2; each of R | 04-21-2011 |
20110112132 | MEANS FOR THE TREATMENT OF ACUTE AND CHRONIC DISORDERS OF CEREBRAL CIRCULATION, INCLUDING INSULT, BASED ON HYDROGENATED PYRIDO (4,3-B) INDOLES (VARIANTS), PHARMACOLOGICAL MEANS BASED THEREON AND METHOD FOR THE USE THEREOF - A means for the treatment of insult based on hydrogenated pyrido(4,3-b)indoles (variants) of formula (1) or formula (2) a pharmacological means based thereon and a method for the use thereof relate to the use of chemical compounds in the field of medicine and may be used for the treatment of ischemic and hemorrhagic insults and their consequences. | 05-12-2011 |
20110112133 | DIHYDRO PYRROLOQUINOLINE DERIVATIVES - A compound represented by the formula (I) | 05-12-2011 |
20110112134 | Tricyclic Antagonists of Prostaglandin D2 Receptors - Described herein are compounds that are antagonists of PGD | 05-12-2011 |
20110118299 | TREATMENT OF MCI AND ALZHEIMER'S DISEASE - The present invention provides, among other things, therapeutic compositions and methods that can effectively treat, slow or prevent a neurological disease (e.g., a neurodegenerative disease, e.g., mild cognitive impairment (MCI) or Alzheimer's disease (AD)), in particular, based on therapeutically effective amount of nifedipine, oxidized or nitroso nifedipine derivatives, lactam (e.g., a compound of formula (Ic) or (Ic-i), e.g., NFD-L1), thyroxine (T4), triiodothyronine (T3) and combinations thereof. | 05-19-2011 |
20110136853 | LIGAND WITH A BROAD SPECTRUM OF PHARMACOLOGICAL ACTIVITY, A PHARMACEUTICAL COMPOSITION, A MEDICINAL AGENT AND A METHOD OF TREATMENT - The present invention is directed to the novel ligand with wide range of pharmacological activity including activity to GPCR receptors, ion channels and monoamine transporters representing 3-methyl-9-benzyl-1,2,3,4-tetrahydrocarboline naphthalene-1,5-disulfonate of formula 1 | 06-09-2011 |
20110152308 | AZA-RING FUSED INDOLE AND INDOLINE DERIVATIVES - The present application relates to indole and indoline derivatives of formula (I) | 06-23-2011 |
20110152309 | PHARMACEUTICAL, FOOD OR BEVERAGE HAVING INHIBITORY ACTIVITY ON SEROTONIN TRANSPORTER - There is provided a pharmaceutical agent, food, or beverage for treating or preventing a disease or condition that can be ameliorated by inhibiting serotonin reuptake, comprising a clinically-effective amount of (1S,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid. | 06-23-2011 |
20110160240 | POLYMORPHS AND SALTS OF A KINASE INHIBITOR - The present invention relates to novel crystalline polymorphic salt forms of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid, processes for the preparation thereof, compositions thereof and their use in methods of treatment and prevention of conditions mediated by casein kinase (CK) and/or poly(ADP-ribose)polymerase (PARD). | 06-30-2011 |
20110172262 | COMPOSITIONS AND METHODS FOR TREATING EPILEPSY - Compositions and methods for treating epilepsy and epileptic syndromes are described herein. The compositions and methods include therapeutically effective amounts of one or more dimebolins, or pharmaceutically acceptable salts thereof. | 07-14-2011 |
20110178115 | AZAINDOLE DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS - Compounds of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma. | 07-21-2011 |
20110207765 | TOPICAL COMPOSITION COMPRISING A COMBINATION OF AT LEAST TWO PENETRATION ENHANCING AGENTS - The present invention relates to a composition for improved transdermal drug delivery comprising a drug, a combination of at least two penetration enhancing agents, wherein at least one of the penetration enhancing agents is selected from the group consisting of esters of saturated or unsaturated fatty acids and lower alcohols, and iso-form alcohols; wherein at least one of the penetration enhancing agents is selected from the group consisting of aliphatic diols and triols; and wherein the components are present in a non-aqueous solvent system. A preferred topical composition comprises the active substance imiquimod and the penetration enhancing agents isopropyl myristate and propylene glycol. | 08-25-2011 |
20110230517 | CALCIUM RECEPTOR MODULATING AGENTS - The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula (I). Where Cy | 09-22-2011 |
20110275660 | BETA CARBOLINE SULPHONYLUREA DERIVATIVES AS EP4 RECEPTOR ANTAGONISTS - The invention is directed to β-carboline sulphonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, inflammation, osteoarthritis, and rheumatoid arthritis. Pharmaceutical compositions and methods of use are also included. | 11-10-2011 |
20110275661 | TRICYCLIC NITROGEN COMPOUNDS USED AS ANTIBACTERIALS - The present invention relates to tricyclic nitrogen containing compounds of Formula (I): | 11-10-2011 |
20110306631 | TRIPLE SUBSTITUTED PHENANTHROLINE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE OR HAEMATOLOGICAL DISEASES OR CONDITIONS, OR CANCER - The present invention relates to a new family of triple substituted phenantroline derivatives of formula (I), which are useful for the treatment or profilaxis of a neurodegenerative or haematological disease or condition or cancer, their use as a medicament, especially for treating a neurodegenerative or haematological disease or condition or cancer, and a pharmaceutical composition comprising the compounds. | 12-15-2011 |
20120022096 | PRO-NEUROGENIC COMPOUNDS - This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like. | 01-26-2012 |
20120029010 | METHOD TO USE COMPOSITIONS HAVING ANTIDEPRESSANT ANXIOLYTIC AND OTHER NEUROLOGICAL ACTIVITY AND COMPOSITIONS OF MATTER - The sponges were collected from a variety of locations in the Florida Keys and separated based on morphology and color. The samples were identified as three species, two of which are well known: | 02-02-2012 |
20120035204 | Methods for Treating Obesity and Disorders Associated with Hyperlipidemia in a Mammal - The disclosure relates to methods for treating hyperlipidemia in a mammal. The present disclosure also relates to methods for treating and/or controlling obesity in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, AEGR-733 and implitapide) and a DGAT inhibitor (for example, JTT-553 or PF-04415060). Co-administration of the MTP inhibitor with the DGAT inhibitor produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit. | 02-09-2012 |
20120101121 | DRUG DEMONSTRATING ANXIOLYTIC EFFECT BASED ON HYDROGENATED PYRIDO (4,3-B) INDOLES, ITS PHARMACOLOGICAL COMPOUND AND APPLICATION METHOD - Compositions based on hydrogenated pyrido[4,3-b]indoles (variants) of formula (1) or formula (2): are provided, as are methods and kits using those compositions for the treatment of anxiety or mood disorders characterized by stresses, anxiety, neuroses, obsessive fears and their consequences. | 04-26-2012 |
20120122914 | Sustained-release composition containing tetrahydropyrido[4,3-b]indole derivatives and preparation of the derivatives - The present invention relates to a sustained-release composition containing 2,3,4,5-tetrahydro-2,8-dimethyl-5-[2-(6-methyl-3-pyridyl)ethyl]-1H-pyrido[4,3-b]indole or a pharmaceutically acceptable salt thereof as an active ingredient, preparation thereof and the compound. The composition is suitable for oral administration by one time per day, and achieves the peak plasma concentration at 1.0 to 3 hours after oral administration. The composition is suitable for manufacturing a medicament for treatment of cognitive dysfunction syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, or senile dementia. | 05-17-2012 |
20120214838 | THERAPEUTICALLY USEFUL SUBSTITUTED HYDROPYRIDO [3,2,1-ij] QUINOLINE COMPOUNDS - Disclosed herein are compounds represented by the structural formula: | 08-23-2012 |
20120220620 | Antitubercular alkaloid - A derivative of β-carboline alkaloid harmine, 10,12-diheptanoyl-11-hydroxy-3-methyl-β-carboline, prepared by a Friedel-Crafts acylation of harmine is reported as a novel potent antitubercular drug. | 08-30-2012 |
20120220621 | ANTI-CANCER COMPOUND AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME - The invention relates to a compound of formula (I), more specifically in the levorotatory form (1 | 08-30-2012 |
20120264777 | OXADIAZOLE BETA CARBOLINE DERIVATIVES AS ANTIDIABETIC COMPOUNDS - Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin sub-type receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety. | 10-18-2012 |
20120309781 | TETRAHYDRO-beta-CARBOLINE DERIVATIVES, SYNTHESIS AND USE THEREOF - Certain 2-halophenyl, 2,4-dihalophenyl (e.g. 2,4-dichlorophenyl), 3,4-dichlorophenyl (e.g. 3,4-dichlorophenyl), 2,6-dichlorophenyl (2,6-dichlorophenyl) and 2,5-diakoxyphenyl (e.g. 2,5-dimethoxyphenyl) derivatives of tetrahydro-β-carbolines are provided, along with their pharmaceutically acceptable salts; prodrugs and solvates, and compositions containing the compounds. The compounds are useful for the prevention and treatment of cancer, and other indications where PDE5 inhibitors have shown benefits including erectile dysfunction, pulmonary hypertension, enhancing cognitive function, cystic fibrosis, or enhancing the activity of conventional chemotherapeutic drugs. Methods for fabricating the compounds are also provided. | 12-06-2012 |
20120309782 | THERAPEUTICALLY USEFUL SUBSTITUTED HYDROPYRIDO [3,2,1-ij] QUINOLINE COMPOUNDS - Disclosed herein are compounds represented by the structural formula: | 12-06-2012 |
20130059879 | Small Molecule Inhibitors of PFKFB3 and Glycolytic Flux and Their Methods of Use as Anti-Cancer Therapeutics - Small molecule inhibitors of 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) having the following formula: Formula (1) are provided herein. Also provided herein are pharmaceutical compositions containing Formula I compounds, together with methods of treating cancer, methods of inhibiting PFK.FB3 enzymatic activity, methods of inhibiting glycolytic flux, and methods of treating tumors by administering an effective amount of a Formula I compound. | 03-07-2013 |
20130096151 | NOVEL COMBINATION AND USE - The present invention relates to the use of an anesthetic agent for killing clinically latent microorganisms associated with microbial infections and to novel combinations comprising an anesthetic agent and an antimicrobial agent for the treatment of microbial infections. | 04-18-2013 |
20130116272 | HETEROCYCLIC FUSED PHENANTHROLINONE M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS - The present invention is directed to heterocyclic fused phenanthrolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 05-09-2013 |
20130116273 | BETA CARBOLINE DERIVATIVES USEFUL IN THE TREATMENT OF PROLIFERATIVE DISORDERS - The invention provides novel beta-carboline derivatives of formulae (Ia) and (Ib) useful in the treatment of proliferative disorders including cancer, intermediates used in their preparation, processes for preparing the same and uses thereof. | 05-09-2013 |
20130131099 | COMPOUNDS AND METHODS OF TREATING BRAIN DISORDERS - Nitrated and non-nitrated compounds capable of protecting brain tissue from injury and useful as therapeutic agents to treat neurodegenerative diseases and conditions are disclosed. Methods of using the compounds in therapeutic treatments, and methods of preparing the compounds, also are disclosed. | 05-23-2013 |
20130190347 | 2,3,4,5-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLE COMPOUNDS AND METHODS OF USE THEREOF - This disclosure relates to new tricyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds are described, including new 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole compounds. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 07-25-2013 |
20130203800 | METHOD FOR DETECTING NON-TRANSFERRIN BOUND IRON - A method of quantifying non-transferrin bound iron (NTBI) in a biological fluid is provided, the method comprising: | 08-08-2013 |
20130225632 | CALCIUM SALT OF PYRROLOQUINOLINE QUINONE - An object of the present invention is to provide an industrially useful method for producing a calcium salt of pyrroloquinoline quinone, without using large amounts of organic solvents, and highly pure crystals produced thereby. According to the present invention, a highly pure calcium salt of pyrroloquinoline quinone can be produced by reacting an alkali metal salt of pyrroloquinoline quinone with a source of calcium ions. | 08-29-2013 |
20130237560 | NEURONAL CIRCUIT-DEPENDENT NEUROPROTECTION BY INTERACTION BETWEEN NICOTINIC RECEPTORS - A method of inhibiting excitotoxicity by indirectly activating α4β2 nicotinic acetylcholine receptors (nAChRs) which indirectly activate synaptic AMPA and NMDA receptors is disclosed. Inhibitors of α7 nACHRs, such as macrocyclic diterpenoids, more specifically cembranoids or methyllycaconitine (MLA), indirectly activate α4β2 nAChRs and can be used to treat neurodegenerative diseases, including, but not limited to, Alzheimer's Disease, Parkinson Disease, AIDS related dementia and the delayed effects of stroke. They can also be used to treat diseases associated with neuronal impairment, including, but not limited to glaucoma caused by optical nerve damage, delayed effects of epilepsy; and multiple sclerosis. | 09-12-2013 |
20130245060 | NOVEL COMPOSITION - This invention relates to topical pharmaceutical compositions comprising the active agent 4-methyl-1-(2-phenylethyl)-8-phenoxy-2,3-dihydro-1H-pyrrolo[3,2-c]-quinoline or a pharmaceutically acceptable derivative thereof and a hydrophobic excipient, to a process for preparing such compositions, and to the use of such compositions for the treatment of microbial infections. | 09-19-2013 |
20130253001 | HIGHLY SOLUBLE SALT OF PYRROLOQUINOLINE QUINONE AND METHOD FOR PRODUCING THE SAME - An object of the present invention is to provide a salt of pyrroloquinoline quinone having a high solubility in water and in an organic solvent and a method for producing the same. | 09-26-2013 |
20130281484 | HDAC Inhibitors and Therapeutic Methods of Using Same - Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed. | 10-24-2013 |
20140005220 | BETA CARBOLINE DERIVATIVES USEFUL IN THE TREATMENT OF PROLIFERATIVE DISORDERS | 01-02-2014 |
20140011835 | [1,10]-PHENANTHROLINE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE OR HAEMATOLOGICAL DISEASES - The present invention relates to a new family of [1,10]-phenantroline derivatives of formula (I), which are useful for the treatment or prophylaxis of a neurodegenerative or hematological disease or condition, their use as a medicament, especially for treating a neurodegenerative or hematological disease or condition, and a pharmaceutical composition comprising the compounds. | 01-09-2014 |
20140038999 | Aryl Lactam Kinase Inhibitors - The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1. | 02-06-2014 |
20140045882 | Carboxamide, Sulfonamide and Amine Compounds and Methods for Using The Same - Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 02-13-2014 |
20140080859 | Bis-Quaternary Ammonium Cyclophane Compounds that Interact with Neuronal Nicotinic Acetylcholine Receptors - Provided are bis-quaternary ammonium cyclophane compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders. | 03-20-2014 |
20140094487 | Dihydro-6-Azaphenalene Derivatives for the Treatment of CNS, Oncological Diseases and Related Disorders - In one embodiment, the present application discloses 2-aza-, 2-oxa- and 2-thia-2,3-dihydro-6-azaphenalene compounds and compositions, and methods for treating a neurological disease in a patient in need thereof using the compounds and compositions as disclosed herein. | 04-03-2014 |
20140100242 | INHIBITION OF QUORUM SENSING-MEDIATED PROCESSES IN BACTERIA - Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production. | 04-10-2014 |
20140135359 | METHODS OF DESIGNING, PREPARING, AND USING NOVEL PROTONOPHORES - The present invention provides a computer-assisted method of generating a protonophore requiring the use of a computer including a processor. The method includes: designing the protonophore, calculating, using the processor, an estimated protonophoric activity; producing the protonophore if the estimated protonophoric activity corresponds to an U | 05-15-2014 |
20140148476 | METHODS FOR TREATING OBESITY AND DISORDERS ASSOCIATED WITH HYPERLIPIDEMIA IN A MAMMAL - The disclosure relates to methods for treating hyperlipidemia in a mammal. The present disclosure also relates to methods for treating and/or controlling obesity in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, AEGR-733 and implitapide) and a DGAT inhibitor (for example, JTT-553 or PF-04415060). Co-administration of the MTP inhibitor with the DGAT inhibitor produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit. | 05-29-2014 |
20140179732 | TRICYCLIC LACTAM DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS - Compounds of the formula (I) useful as 11-Beta Hydroxysteroid Dehydrogenase Inhibitors | 06-26-2014 |
20140200238 | DRUG TREATMENT OF OVERACTIVE BLADDER - Provided are methods of treating an overactive bladder in a patient which include: administering a Myosin II ATPase inhibitor compound; or administering an X group and Y group substituted (3a-hydroxy-1-phenyl-1,2,3,3a-tetrahydro-4H-pyrollo[2, 3b] quinolin-4-one) compound of Formula 1 or administering an X group and Y group substituted (3a-hydroxy-1-phenyl-1,2,3,3a-tetrahydro-4H-pyrollo[2,3b] quinolin-4-one) compound of Formula II; or administering pharmaceutically-acceptable salts, racemic mixtures, enantiomers, or prodrugs of said compounds, useful in their active form as inhibitors of Myosin H ATPase related to over-active bladder. Optionally the compounds are administered intervesicularly into the bladder. Also provided are pharmaceutical compositions comprising said compounds useful in their active form, as methods of treating a patient suffering from an over-active bladder related to inhibition of Myosin II ATPase. These pharmaceutical compositions also may contain one or more other compounds useful in their active form, as methods of treating a patient suffering from an over-active bladder. | 07-17-2014 |
20140206711 | PYRIDO[4,3-b]INDOLE AND PYRIDO[3,4-b]INDOLE DERIVATIVES AND METHODS OF USE - This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. The compounds may bind to and antagonize receptor α | 07-24-2014 |
20140213609 | PROMOTING AXON RENEGERATION IN THE ADULT CNS THROUGH CONTROL OF PROTEIN TRANSLATION - Survival of, or axon regeneration in a lesioned mature central nervous system (CNS) neuron is promoted by (a) contacting the neuron with a therapeutically effective amount of an exogenous activator of protein translation; and (b) detecting the resultant promotion of the survival of, or axon regeneration in the neuron. | 07-31-2014 |
20140329849 | HDAC INHIBITORS TO TREAT CHARCOT-MARIE-TOOTH DISEASE - The disclosure relates to diseases in the peripheral nervous system, particularly hereditary neuropathies, such as Charcot-Marie-Tooth (CMT) disease. It is shown that this disease is associated with decreased acetylated tubulin levels, which can be overcome by inhibition of histone deacetylases (HDACs). Using HDAC inhibitors, it is shown herein that the symptoms of the CMT phenotype can be overcome both in vitro and in vivo. Also provided herein are two different mouse models of CMT disease. | 11-06-2014 |
20140336216 | PHYSIOLOGICAL LIGANDS FOR GPR139 - Provided herein are compounds capable of activating GPR139. Also provided are methods of increasing and decreasing the activity of GPR139. Methods of using the identified compounds to modulate GPR139 activity or conditions that may be affected by GPR139 activity are also disclosed. | 11-13-2014 |
20140343092 | Pyrrolopyridinone Compounds And Methods For Treating HIV - Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV). | 11-20-2014 |
20140357661 | CHEMICAL COMPOUNDS - The invention concerns compounds of Formula (I) | 12-04-2014 |
20140378502 | Par1 Inhibitors for Use in the Treatment or Prevention of Paramyxoviridae Infections - The present invention is concerned with the use of Protease-Activated Receptor-1 (PAR1) inhibitors for preventing or treating a Paramyxoviridae infection in a subject. Described herein are methods, compounds and pharmaceutical compositions useful in addressing such infections, and more particularly infections from human respiratory syncytial virus (hRSV) and human metapneumovirus (hMPV). | 12-25-2014 |
20150025104 | Nutraceuticals Having Sustained Release for Improved Bioavailability and Method of Production - The present disclosure describes economical processes to improve the bioavailability of nutraceuticals by formulations that induce micronization and sustained release. The inventive process can be used to increase the solubility and bioavailability of lipophilic and moderately water-soluble nutraceuticals by combining excipients that increase the solubility and induce sustained release of the active compounds. The inventive process also can be used to increase the residence time of highly water-soluble nutraceuticals that are metabolized and eliminated quickly from the body, consequently increasing the therapeutic potential. The disclosed formulations advantageously are freely flowing powders that can be used to formulate with other ingredients into tablets, capsules, or the like; or used as bulk powders. | 01-22-2015 |
20150038526 | FLUORINE-CONTAINING 5-[2-(PYRID-3-YL)-ETHYL]-2,3,4-TETRAHYDRO-1H-PYRIDO[4,3-B]INDOLES AS AGENTS FOR REDUCING UNCONTROLLED PROTEIN AGGREGATION - The claimed fluorine-containing substituted 5-[2-(pyrid-3-yl)-ethyl]-2,3,4-tetrahydro-1H-pyrido[4,3-b]indoles and hydrochlorides and hydrobromides thereof, which have the general formula (I), as agents for reducing uncontrolled protein aggregation in the nervous system, the pharmacological agent based thereon and the method for using same relate to the field of medicine and solve the problem of increasing the range of agents for combating the development of destructive processes in the central and peripheral nervous system. | 02-05-2015 |
20150051242 | RAFAMYCIN ANALOGS AND METHODS FOR MAKING SAME - A semi-synthetic rapamycin analog with a triazole moiety or a pharmaceutically acceptable salt or prodrug thereof, is a broad-spectrum cytostatic agent and a mTOR inhibitor, and is useful in the treatment of various cancers, or tumors in organs such as kidney, liver, breast, head and neck, lung, prostate, and restenosis in coronary arteries, peripheral arteries, and arteries in the brain, immune and autoimmune diseases. Also disclosed are fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such triazole-moiety containing rapamycin analog is in treating renal carcinoma, lung cancer, colon cancer, and breast cancers wherein potency of the drug, its half-life, tissue distribution properties, and its pharmacokinetic properties including bioavailability through oral and intravenous routes are essential to the clinical outcomes. | 02-19-2015 |
20150080425 | METHODS FOR TREATING ANEMIA IN SUBJECTS HAVING KIDNEY FAILURE USING INHIBITORS OF HYPOXIA-INDUCIBLE FACTOR (HIF) HYDROXYLASE - The present invention provides methods for treating anemia in a subject having kidney failure by administering a compound that inhibits hypoxia-inducible factor (HIF) prolyl hydroxylase. | 03-19-2015 |
20150111919 | COMPOSITIONS AND METHODS FOR TREATING MULTIPLE SCLEROSIS - Described herein are compositions and methods for treating multiple sclerosis. In particular, described herein are compositions that include one or more dimebolins and/or pharmaceutically acceptable salts thereof and methods for using the compositions for treating multiple sclerosis. | 04-23-2015 |
20150133488 | COMPOSITIONS AND METHODS FOR TREATING EPILEPSY - Compositions and methods for treating epilepsy and epileptic syndromes are described herein. The compositions and methods include therapeutically effective amounts of one or more dimebolins, or pharmaceutically acceptable salts thereof. | 05-14-2015 |
20150291583 | CRYSTALLINE FORMS OF PYRROLOQUINOLINE QUINONE DISODIUM SALT - The present invention relates to crystalline forms of pyrroloquinoline quinone disodium salt. The present invention provides crystalline Form A and crystalline Form B of pyrroloquinoline quinone disodium salt, and the methods and uses for the preparation thereof. The X-ray powder diffraction patterns of crystalline Form A and crystalline Form B are as shown by FIG. | 10-15-2015 |
20150320877 | Epimorphic Regeneration and Related Hidrogel Delivery Systems - Methods and compositions are described for enhancing tissue regeneration or wound repair in a mammalian subject comprising a composition comprising (a) a proline hydroxylase inhibitor component or molecule that increases or upregulates HIF1a and (b) a carrier component comprising a hydrogel. | 11-12-2015 |
20150352088 | Bis-Quaternary Ammonium Cyclophane Compounds that Interact with Neuronal Nicotinic Acetylcholine Receptors - Provided are bis-quaternary ammonium cyclophane compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and or gastrointestinal tract disorders. | 12-10-2015 |
20150368226 | PIPERIDINYLCARBAZOLES - The present invention provides compounds of Formula (I) for the treatment of parasitic diseases including malaria, as well as neurodegenerative diseases. Formula (I) wherein R | 12-24-2015 |
20160000766 | HDAC INHIBITORS TO TREAT CHARCOT-MARIE-TOOTH DISEASE - The present application relates to diseases in the peripheral nervous system, particularly hereditary neuropathies, most particularly, Charcot-Marie-Tooth (CMT) disease. It is shown that this disease is associated with decreased acetylated tubulin levels, which can be overcome by inhibition of histone deacetylases (HDACs). Using HDAC inhibitors, it is shown herein that the symptoms of the CMT phenotype can be overcome both in vitro and in vivo. Also provided herein are two different mouse models of CMT disease. | 01-07-2016 |
20160002229 | TRICYCLIC LACTAM DERIVATIVES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS - Compounds of the formula (I) useful as 11-Beta Hydroxysteroid Dehydrogenase Inhibitors | 01-07-2016 |
20160016893 | SCREENING METHODS FOR THE BINDING AFFINITY OF CHEMICAL ENTITIES TO BIOLOGICAL MOLECULES AND NEDD4-1 INHIBITORS IDENTIFIED BY THE SCREENING METHODS - Disclosed are methods for screening for the binding affinity of chemical entities to other bioactive molecules. The screened chemical entities may be utilized in pharmaceutical composition or therapeutic methods for treating disease or disorders associated with the bioactive molecules including NEDD4-1. | 01-21-2016 |
20160024083 | COMPOUNDS AND METHODS FOR TREATING CANCERS - Provided are carbazole and carbazole-like compounds (e.g., pyridoindole and pyrrolodipyridine) compounds, that can be used to selectively kill cancer cells, specifically androgen-receptor expressing prostate cancer cells. Also provided is a method of treating AR-positive prostate cancer in a subject diagnosed with or suspected of having AR positive or negative cancer, comprising administering an effective amount of a carbazole and carbazole-like compound to said subject. | 01-28-2016 |
20160030389 | USE OF INDOLE COMPOUNDS FOR FAT REDUCTION AND SKIN AND SOFT TISSUE TIGHTENING - The present invention relates to indole compounds and compositions and uses thereof, including uses of the indole compounds and compositions for the reduction or removal of localized fat deposits and/or tightening of skin and soft tissue laxity in subjects. The indole compounds can be employed, for example, in the cosmetic sector or for producing pharmaceutical products. | 02-04-2016 |
20160039816 | CRYSTALS OF PYRROLOQUINOLINEQUINONE SODIUM SALTS - A crystal of pyrroloquinoline quinone disodium salt having peaks at 2θ of 9.1°, 10.3°, 13.8°, 17.7°, 18.3°, 24.0°, 27.4°, 31.2° and 39.5° (±0.2° for each) in powder X-ray diffractometry using Cu Kα radiation, or a crystal of pyrroloquinoline quinone trisodium salt having peaks at 2θ of 6.6°, 11.4°, 13.0°, 22.6°, 26.9°, 27.9°, 37.0°, 38.9° and 43.4° (±0.2° for each) in powder X-ray diffractometry using Cu Kα radiation. | 02-11-2016 |
20160039845 | BIS-B-CARBOLINE COMPOUND AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF - Disclosed in the present invention are a bis-β-carboline compound and a preparation method, a pharmaceutical composition and the use thereof. In particular, the bis-β-carboline compound and a pharmaceutical salt thereof are described as general formula I, and the bis-β-carboline compound is prepared through the condensation of β-carboline intermediate and dihaloalkane. Also disclosed in the present invention are a pharmaceutical composition comprising an effective dose of the bis-β-carboline compound as shown in formula I and a pharmaceutically acceptable carrier, and the use of the bis-β-carboline compound in preparing drugs resistant to tumours such as melanoma, stomach cancer, lung cancer, breast cancer, kidney cancer, liver cancer, oral epidermoid carcinoma, cervical cancer, ovarian cancer, pancreatic cancer, prostate cancer, and colon cancer. | 02-11-2016 |
20160075700 | YELLOW REDUCED PYRROLOQUINOLINE QUINONE CRYSTAL AND METHOD OF PRODUCING THE SAME, AND FOOD, PHARMACEUTICAL, GEL, COMPOSITION AND METHOD OF PRODUCING COMPOSITION - A yellow reduced pyrroloquinoline quinone crystal having a solubility in water of 0.040 to 0.20 (mg/mL). | 03-17-2016 |
20160106721 | HUMAN THERAPEUTIC AGENTS - Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers. | 04-21-2016 |
20160106722 | HUMAN THERAPEUTIC AGENTS - Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers. | 04-21-2016 |
20160106724 | HUMAN THERAPEUTIC AGENTS - Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers. | 04-21-2016 |
20160122340 | HISTONE DEACETYLASE INHIBITORS BASED ON DERIVATIVES OF TRICYCLIC POLYHYDROACRIDINE AND ANALOGS POSSESSING FUSED SATURATED FIVE-AND-SEVEN-MEMBERED RINGS - The present invention refers to compounds of formula (I): | 05-05-2016 |
20160137641 | PYRROLOQUINOLINE QUINONE LITHIUM SALT CRYSTAL AND PREPARATION METHOD AND APPLICATION THEREOF - The present invention provides pyrroloquinoline quinone lithium salt crystal and a preparation method and application thereof. Characteristic absorption peaks appear when the diffraction angles are 6.222±0.2°, 7.379±0.2°, 7.941±0.2°, 23.631±0.2°, 24.044±0.2°, 25.497±0.2°, 27.541±0.2°, 30.736±0.2°, and 32.306±0.2° degrees in a powder X-ray diffraction pattern of the pyrroloquinoline quinine lithium salt crystal. The maximum value of thermal absorption of the pyrroloquinoline quinine lithium salt crystal appears between 90° C. and 96° C. through differential scanning calorimetry. Peaks appear when infrared spectroscopy of the pyrroloquinoline quinine lithium salt crystal is at 3396.03 cm | 05-19-2016 |
20160374998 | MACROLIDE PARTICULATES, METHODS FOR PREPARATION, AND MEDICAL DEVICES ASSOCIATED THEREWITH - The disclosure provides macrolide particulates including a macrolide therapeutic agent such as rapamycin at high concentration in the particulate. In one method the particulates are made by adding a composition containing an polyoxyethylene sorbitan n-acyl ester, poly(ethyleneimine), or alkylated quaternary ammonium salt to a composition including macrolide dissolved in an alcohol such as ethanol. In another method the particulates are made by adding a non-solvent composition to a composition including macrolide and an alkyl-substituted chromanol dissolved in an alcohol such as ethanol. The formed macrolide particulates have one or more desirable properties including sizes in the range of 0.1 μm to 10 μm, spherical or near spherical shapes, low polydispersity, and/or stability. The macrolide particulates can be used for therapeutic compositions, or in association with an implantable or insertable medical device, such as associated with a polymeric coating on a device. | 12-29-2016 |
20160376272 | FACTOR XIa INHIBITORS - The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein. | 12-29-2016 |