Plural Ring Nitrogens In The Tricyclo Ring System Patents (Class 514/292)
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Patent number: 9655886Abstract: The present invention relates to a method of antagonizing a 5-HT6 serotonin receptor, comprising administering to the cell a compound of formula 1.2, or a pharmaceutically acceptable salt thereof, wherein: R1 is a C1-C5 alkyl; R2i is independently hydrogen, halogen, a C1-C3 alkyl, CF3, OCF3 or OCH3; i is 1, 2, 3 or 4; Ar is an unsubstituted phenyl or a substituted phenyl substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group or trifluoromethyl; or Ar is a substituted or unsubstituted 6-membered aromatic heterocycle with one or two nitrogen atoms in the heterocycle. The invention also relates to pharmaceutical compositions and method for treating a cognitive disorder or neurodegenerative disease in a subject in need thereof comprising administering an effective dose to the subject of a compound of formula 1.2 according to claim 1, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 3, 2015Date of Patent: May 23, 2017Inventors: Alexandre Vasilievich Ivachtchenko, Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk
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Patent number: 9572817Abstract: The present invention relates to the field of therapy and prophylaxis of vascular tissue damage and/or complications and/or disease of vascular tissue by vascular regeneration and endothelium repair. The inventors have found that administration of an androgen receptor agonist alleviates one or more adverse vascular diseases and/or vascular complications thereof or adverse effects of androgen deficiency, with implications for prophylactic and therapeutic interventions.Type: GrantFiled: July 4, 2008Date of Patent: February 21, 2017Assignee: THE HEART RESEARCH INSTITUTE LTD.Inventors: Daniel Peter Sieveking, Martin Kean Chong Ng
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Patent number: 9527854Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.Type: GrantFiled: March 6, 2015Date of Patent: December 27, 2016Assignee: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain, Michael John Green
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Patent number: 9526776Abstract: Serogroup B meningococcus antigens can successfully be combined with diphtheria, tetanus and pertussis toxoids (“DTP”) to provide effective combination vaccines for protecting against multiple pathogens. These combinations are effective with a range of different adjuvants, and with both pediatric-type and booster-type DTP ratios. The adjuvant can improve the immune response which the composition elicits; alternatively, by including an adjuvant it is possible for the compositions to have a relatively lower amount of antigen while nevertheless having immunogenicity which is comparable to unadjuvanted combination vaccines.Type: GrantFiled: September 6, 2013Date of Patent: December 27, 2016Assignee: GlaxoSmithKline Biologicals SAInventors: Barbara Baudner, Derek O'Hagan, Manmohan Singh, Simone Bufali
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Patent number: 9517263Abstract: The invention provides, inter alia, immunogenic compositions that comprise (a) a first antigen, (b) polymeric particles and (c) a benzonaphthyridine compound, which compositions elicits an immune response when administered to a vertebrate subject. The invention also provides, inter alia, methods of producing immunogenic compositions and methods for using immunogenic compositions (e.g., for treatment), among other benefits.Type: GrantFiled: June 10, 2010Date of Patent: December 13, 2016Assignee: GlaxoSmithKline Biologicals SAInventors: Derek O'Hagan, Manmohan Singh, Siddhartha Jain, Sushma Kommareddy
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Patent number: 9394296Abstract: The present invention features tryptoline derivatives and related compounds having kinase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions, such as cancers, inflammatory disorders, or autoimmune disorders.Type: GrantFiled: January 9, 2013Date of Patent: July 19, 2016Assignee: X-Chem, Inc.Inventors: Anthony D. Keefe, Richard W. Wagner, Matthew Clark, Ying Zhang, Diana Gikunju, John Cuozzo, Heather Thomson
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Patent number: 9394298Abstract: An object of the present invention is to provide a pyrroloquinoline quinone tetraalkali salt needing no special reagent, having a high solubility in a solvent, being capable of providing a high-concentration pyrroloquinoline quinone aqueous solution, being hardly changed in color even if being concurrently used with ascorbic acid, and being of a high quality and a high purity; a crystal of a pyrroloquinoline quinone tetrasodium salt; a composition; and a simple method for producing the pyrroloquinoline quinone tetraalkali salt. The pyrroloquinoline quinone tetraalkali salt is represented by the formula (1): wherein M is each independently one selected from the group consisting of Li, K, Na, Rb and Cs.Type: GrantFiled: August 14, 2013Date of Patent: July 19, 2016Assignee: Mitsubishi Gas Chemical Company, Inc.Inventor: Kazuto Ikemoto
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Patent number: 9359379Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.Type: GrantFiled: October 1, 2013Date of Patent: June 7, 2016Assignee: InterMune, Inc.Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
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Patent number: 9326981Abstract: The invention features methods involving the use of sublingual film formulations of apomorphine for treating Parkinson's disease. The methods involve providing the sublingual film formulation and administering the sublingual film formulation sublingually in the mouth of a subject by contacting sublingual mucosal tissue with the film.Type: GrantFiled: April 10, 2015Date of Patent: May 3, 2016Assignee: Cynapsus Therapeutics, Inc.Inventors: Anthony John Giovinazzo, David Bruce Hedden, Marc L. De Somer, Nathan John Bryson
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Patent number: 9314468Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, tautomers, stereoisomers, and/or esters thereof. These compounds, and pharmaceutical composition comprising such compounds are useful treating or preventing HIV infections, and in treating proliferative disorders such as inhibiting the metastasis of various cancers.Type: GrantFiled: November 15, 2012Date of Patent: April 19, 2016Assignee: Altiris Therapeutics, Inc.Inventors: Michael P Clark, Florence F Wagner, Michael G Natchus, Brandon C Doroh, Tricia L Johnson, Yesim Altas Tahirovic, Lawrence Wilson, John M Wiseman, Jason W Skudlarek, Mark A Lockwood
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Patent number: 9283240Abstract: Disclosed are nutritional compositions including human milk oligosaccharides that can be administered to preterm infants, term infants, toddlers, and children for reducing inflammation and the incidence of inflammatory diseases.Type: GrantFiled: December 22, 2011Date of Patent: March 15, 2016Assignee: ABBOTT LABORATORIESInventors: Rachael Buck, Geralyn O. Duska-McEwen, Joseph P. Schaller
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Patent number: 9255094Abstract: Provided are new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Also provided are pyrido[4,3-b]indoles, as are pharmaceutical compositions comprising the compounds and 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.Type: GrantFiled: April 29, 2010Date of Patent: February 9, 2016Assignee: Medivation Technologies, Inc.Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
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Patent number: 9221817Abstract: The invention relates to a compound of formula (I), more specifically in the levorotatory form (1a) thereof, in particular the form having a rotatory power [?]D=?38.6+0.7 at a concentration of 0.698 mg/ml in methanol. The compound may be in the form of a base or an acid addition salt, in particular a pharmaceutically acceptable acid. The compound is a selective Aurora A and B kinase inhibitor and can be used as an anticancer drug.Type: GrantFiled: June 2, 2015Date of Patent: December 29, 2015Assignee: SANOFIInventors: Jean-Christophe Carry, Michel Cheve, Francois Clerc, Cecile Combeau, Sylvie Gontier, Alain Krick, Sylvette Lachaud, Laurent Schio
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Patent number: 9216186Abstract: This invention relates to the use of 4-methyl-8-phenoxy-1-(2-phenylethyl)-2,3-dihydro-1H-pyrrolo[3,2-c]quinoline or a pharmaceutically acceptable derivative thereof in combination with an aminoglycoside antimicrobial agent for the prevention and/or treatment of microbial infections.Type: GrantFiled: August 5, 2011Date of Patent: December 22, 2015Assignee: HELPERBY THERAPEUTICS LIMITEDInventors: Yanmin Hu, Anthony R. M. Coates
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Patent number: 9169246Abstract: The invention relates to compounds corresponding to formula (I) in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.Type: GrantFiled: September 26, 2011Date of Patent: October 27, 2015Assignee: SANOFIInventors: Alexandre Benazet, Olivier Duclos, Nathalie Guillo, Gilbert Lassalle, Karim Macary, Valérie Vin
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Patent number: 9163014Abstract: A crystal of pyrroloquinoline quinone disodium salt having peaks at 2? 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 K? radiation, or a crystal of pyrroloquinoline quinone trisodium salt having peaks at 2? 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 K? radiation.Type: GrantFiled: June 9, 2010Date of Patent: October 20, 2015Assignee: MITSUBISHI GAS CHEMICAL COMPANY, INC.Inventors: Junichi Edahiro, Hitoshi Sakamoto, Kazuto Ikemoto, Hajime Shimizu, Tatsuya Hasegawa
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Patent number: 9133073Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: GrantFiled: June 18, 2013Date of Patent: September 15, 2015Assignee: Wellstat Therapeutics CorporationInventor: Shalini Sharma
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Patent number: 9078889Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine, or 1-(2-methylpropyl)-1H-imidazo[4,5 c]quinolin-4-amine, i.e., imiquimod, to treat genital/perianal warts with shorter durations of therapy than currently prescribed for the commercially available for Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating genital/perianal warts with an acceptable safety profile and dosing regimens that are shorter and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat genital/perianal warts are also disclosed and described.Type: GrantFiled: November 27, 2013Date of Patent: July 14, 2015Assignee: Medicis Pharmaceutical CorporationInventors: Michael T. Nordsiek, Jefferson J. Gregory
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Patent number: 9079915Abstract: The present invention relates to substituted thienyl- and furanyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thienyl and furanyl-isoquinolinones and to their use in treating various diseases and disorders.Type: GrantFiled: December 13, 2013Date of Patent: July 14, 2015Inventors: Roberto Pellicciari, Flavio Moroni, Eric Christian Hansen, Adam Matthew Gilbert, Peter John Larkin
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Patent number: 9073917Abstract: The invention relates to a compound of formula (I), more specifically in the levorotatory form (1a) thereof, in particular the form having a rotatory power [?]D=?38.6+0.7 at a concentration of 0.698 mg/ml in methanol. The compound may be in the form of a base or an acid addition salt, in particular a pharmaceutically acceptable acid. The compound is a selective Aurora A and B kinase inhibitor and can be used as an anticancer drug.Type: GrantFiled: May 17, 2010Date of Patent: July 7, 2015Assignee: SANOFIInventors: Jean-Christophe Carry, Michel Cheve, Francois Clerc, Cecile Combeau, Sylvie Gontier, Alain Krick, Sylvette Lachaud, Laurent Schio
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Patent number: 9044475Abstract: The invention features sublingual formulations of apomorphine that is a mucoadhesive polymer film or a strip having a first portion including an acid addition salt of apomorphine and a second portion including a pH neutralizing agent, and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders by administering sublingually the film or strip.Type: GrantFiled: June 11, 2010Date of Patent: June 2, 2015Assignee: Cynapsus Therapeutics, Inc.Inventors: Anthony John Giovinazzo, David Bruce Hedden, Marc L. de Somer, Nathan John Bryson
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Patent number: 9035056Abstract: 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 ?2B, ?1B or ?2A. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption, or to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. The compounds may also be used to treat diseases or conditions that are expected to be responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular, renal disorders or type 2 diabetes is particularly described.Type: GrantFiled: February 17, 2012Date of Patent: May 19, 2015Assignee: Medivation Technologies, Inc.Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Patent number: 9034880Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. 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.Type: GrantFiled: March 8, 2013Date of Patent: May 19, 2015Assignee: Medivation Technologies, Inc.Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sundeep Dugar, Sarvajit Chakravarty
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Publication number: 20150133488Abstract: 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.Type: ApplicationFiled: April 14, 2014Publication date: May 14, 2015Inventors: Spyros Deftereos, Andreas Persidis
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Patent number: 9029387Abstract: The present invention relates to benzonaphthyridinamines of the formula (I) as autotaxin inhibitors and to the use thereof in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in which the inhibition, regulation and/or modulation of phosphodiesterase or lysophospholipase autotaxin plays a role, in particular of various types of cancer and autoimmune and inflammatory diseases.Type: GrantFiled: February 28, 2011Date of Patent: May 12, 2015Assignee: Merck Patent GmbHInventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
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Publication number: 20150125550Abstract: A method of inhibiting cancer cell growth is provided. In some versions, the method includes exposing lung cancer cells or glioma cells to 2,9-di-sec-butyl-1,10-phenanthroline (SBP) or derivatives of SBP in an amount effective to inhibit glioma cell growth. Also, a method of treating a lung cancer or a glioma tumor in a subject in need of such treatment is provided. The method includes administering SBP or derivatives of SBP to the subject in an amount effective to treat the lung cancer or glioma tumor. For either method, the method can further include exposing or administering pseudo five coordinate gold(III) complexes of SBP derivatives.Type: ApplicationFiled: August 29, 2014Publication date: May 7, 2015Inventors: Jack F. Eichler, Clement N. David, Emma H. Wilson
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Publication number: 20150111919Abstract: 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.Type: ApplicationFiled: April 14, 2014Publication date: April 23, 2015Inventors: Spyros Deftereos, Andreas Persidis
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Patent number: 9006263Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?1B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.Type: GrantFiled: March 7, 2013Date of Patent: April 14, 2015Assignee: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain, Michael John Green
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Patent number: 8999978Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. 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.Type: GrantFiled: November 16, 2012Date of Patent: April 7, 2015Assignee: Medivation Technologies, Inc.Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sundeep Dugar, Sarvajit Chakravarty
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Publication number: 20150087512Abstract: The subject invention is directed toward antimicrobial agents and methods of treating and preventing infection by pathogenic microorganisms and endophytic microorganisms in a plant through the use of SecA inhibitors.Type: ApplicationFiled: September 26, 2014Publication date: March 26, 2015Inventors: Nian WANG, Nagaraju AKULA
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Publication number: 20150080324Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.Type: ApplicationFiled: November 25, 2014Publication date: March 19, 2015Inventors: Gavin David Heffernan, David Penman Jacobus, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
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Publication number: 20150080425Abstract: 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.Type: ApplicationFiled: July 16, 2014Publication date: March 19, 2015Applicant: FibroGen, Inc.Inventors: STEPHEN J. KLAUS, Al Y. Lin, Thomas B. Neff, Qingjian Wang, Volkmar Guenzler-Pukall, Lee A. Flippin, Michael P. Arend, Alex Melekhov
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Publication number: 20150065471Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
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Publication number: 20150065498Abstract: The present invention is directed to N-linked lactam compounds of general 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.Type: ApplicationFiled: May 11, 2012Publication date: March 5, 2015Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
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Patent number: 8969563Abstract: 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.Type: GrantFiled: September 22, 2011Date of Patent: March 3, 2015Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Kazuto Ikemoto, Masahiko Nakano
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Publication number: 20150057301Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protectiong from neuron cell death.Type: ApplicationFiled: July 24, 2014Publication date: February 26, 2015Inventors: Steven L. McKnight, Joseph M. Ready, Andew A. Pieper, Jef K. De Brabander
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Publication number: 20150051204Abstract: Present invention refers to new compounds of formula I or II, its synthesis and its use in the treatment of metabolic syndrome, particularly for the treatment of type I or type II diabetes and/or metabolic syndrome or metabolic disease or metabolic disorders.Type: ApplicationFiled: March 28, 2012Publication date: February 19, 2015Applicant: SJT MOLECULAR RESEARCH, S.L.Inventors: Juan Carlos Agreda Navajas, Roberto Mikio Kassuya
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Publication number: 20150051242Abstract: 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.Type: ApplicationFiled: November 30, 2012Publication date: February 19, 2015Applicant: ZHEJIANG ZYLOX MEDICAL DEVICE CO., LTD.Inventor: Jonathon Z. Zhao
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Publication number: 20150051218Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. 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.Type: ApplicationFiled: November 3, 2014Publication date: February 19, 2015Inventors: David T. HUNG, Andrew A. PROTTER, Rajendra Parasmal JAIN, Sarvajit CHAKRAVARTY
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Publication number: 20150050260Abstract: The present invention provides pharmaceutical and dietary compositions in which pyrroloquinoline quinone (PQQ) and its derivatives are combined with other biologically active compounds to produce a synergistic beneficial effect beyond the effect produced by PQQ or its derivatives alone. The present invention also provides methods for providing various beneficial effects which comprise administering these compositions to a mammalian subject.Type: ApplicationFiled: August 15, 2014Publication date: February 19, 2015Inventor: John H. Owoc
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Patent number: 8957086Abstract: 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.Type: GrantFiled: May 4, 2011Date of Patent: February 17, 2015Assignee: The Board of Trustees of the University of IllinoisInventors: Gregory R. J. Thatcher, Zhihui Qin, Jia Luo
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Publication number: 20150038509Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).Type: ApplicationFiled: June 12, 2014Publication date: February 5, 2015Inventors: Gary J. Bridger, Renato T. Skerlj, Al Kaller, Curtis Harwig, David Earl Bogucki, Trevor R. Wilson, Jason B. Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosario DiFluri
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Publication number: 20150038526Abstract: 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.Type: ApplicationFiled: November 1, 2012Publication date: February 5, 2015Inventors: Sergey Olegovich Bachurin, Aleksey Anatolyevich Ustugov, Natalya Nikolaevna Ninkina, Vladimir Borisovich Sokolov, Aleksey Yuryevich Aksinenko, Tatyana Aleksandrovna Shelkovnikova, Aleksey Viktorovich Bolkunov
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Patent number: 8946423Abstract: 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. According to the present invention, there are provided an ammonium salt of pyrroloquinoline quinone having a high solubility in water and in an organic solvent, consisting of a pyrroloquinoline quinone ion and an ammonium salt having a hydroxyl group.Type: GrantFiled: November 25, 2011Date of Patent: February 3, 2015Assignee: Mitsubishi Gas Chemical Company, Inc.Inventor: Kazuto Ikemoto
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Publication number: 20150024060Abstract: 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.Type: ApplicationFiled: September 12, 2014Publication date: January 22, 2015Applicant: BIOACTIVES LLCInventors: Doddabele L. Madhavi, Daniel I. Kagan
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Publication number: 20150025104Abstract: 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.Type: ApplicationFiled: July 16, 2013Publication date: January 22, 2015Applicant: BIOACTIVES LLCInventors: Doddabele L. Madhavi, Daniel I. Kagan
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Publication number: 20150018369Abstract: The disclosure provides methods of treating glioblastoma, methods of screening for compounds that treat glioblastoma, and pharmaceutical compositions useful in the treatment of glioblastoma.Type: ApplicationFiled: January 9, 2013Publication date: January 15, 2015Inventors: Nephi Stella, Philippe Diaz
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Publication number: 20150011509Abstract: Compounds of Formula (I) can be selectively lethal toward a variety of different cancer cell types. The compounds are useful for the management, treatment, control, or adjunct treatment of diseases, where the selective lethality is beneficial in chemotherapeutic therapy.Type: ApplicationFiled: October 12, 2012Publication date: January 8, 2015Applicants: The Board of Trustees of the University of Illnois, The Board of Regents of the University of Texas SystemInventors: Paul J. Hergenrother, David A. Boothman, Joseph S. Bair, Rahul Palchaudhuri, Elizabeth I. Parkinson
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Publication number: 20150011522Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.Type: ApplicationFiled: September 22, 2014Publication date: January 8, 2015Applicants: IRM LLC, Novartis AGInventors: Arnab Kumar Chatterjee, Advait Suresh Nagle, Prasuna Paraselli, Ravinder Reddy Kondreddi, Seh Yong Leong, Pranab Kumar Mishra, Robert Joseph Moreau, Jason Thomas Roland, Wei Lin Sandra Sim, Oliver Simon, Liying Jocelyn Tan, Bryan KS Yeung, Bin Zou, Venkatataiah Bollu
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Patent number: 8927570Abstract: Provided are 1-aryl or 1-heteroaryl substituted beta-carboline compounds or indole analogs thereof having the structure: where X is NH, N—C1-C4 alkyl, S, or O; R1 is 1-naphthyl or 1-dihydroacenaphthenyl, each optionally substituted with a halogen; and R2, R3, R4, R5, R6, and R7 are independently H H, OH, halogen, CN, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl with the proviso that X is NH, R1 is 1-naphthyl or 1-naphthyl substituted with a halogen and one of R5, R6, or R7 is C1-C4 alkoxy, then R2, R3, R4, R5, R6, and R7 are independently H, OH, halogen, CN, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl such that at least two of R2, R3, R4, R5, R6, and R7 are other than H. Also provided are methods for inhibiting proliferation of cells associated with a cell proliferative disease by contacting the cell with the compounds provided herein.Type: GrantFiled: October 30, 2012Date of Patent: January 6, 2015Inventor: John K. Buolamwini