Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/443)
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Patent number: 8835487Abstract: The invention provides methods for treating multiple sclerosis by administering biotin. The invention also provides methods for treating sequalae after multiple sclerosis attacks by administering biotin.Type: GrantFiled: October 4, 2012Date of Patent: September 16, 2014Assignee: Assistance Publique Hopitaux De ParisInventor: Frédéric Sedel
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Patent number: 8835654Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: GrantFiled: September 20, 2011Date of Patent: September 16, 2014Assignee: BHI Limited PartnershipInventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
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Publication number: 20140256784Abstract: Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.Type: ApplicationFiled: May 21, 2014Publication date: September 11, 2014Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Jason Patrick HEALY, Qiang HAN, Ross MABON, Praveen PABBA, James TARVER, JR., Kristen M. TERRANOVA, Ashok TUNOORI, Xiaolian XU
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Publication number: 20140256712Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.Type: ApplicationFiled: March 12, 2014Publication date: September 11, 2014Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.Inventors: Liming SHAO, John Emmerson CAMPBELL, Michael Charles HEWITT, Una CAMPBELL, Taleen G. HANANIA
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Publication number: 20140248268Abstract: This invention relates to compounds and their use as inhibitors or activators of Rab7 GTPase to treat or prevent the onset of Rab 7 GTPase-associated disorders such as neuropathies, cancer, metabolic diseases of bone and lipid storage. The invention is also applicable to infectious diseases where Rab7 is inactivated or its protein-protein interactions are modulated to facilitate intracellular survival of pathogens. The compound described acts as a competitive inhibitor of nucleotide binding and as such also has utility as a scaffold for targeting other small GTPases. In one aspect, methods of treatment of the invention are used to treat or prevent the onset of hereditary sensory neuropathies such as Charcot-Marie-Tooth type 2B disease. Related pharmaceutical compositions, assays, and drug screens are also provided.Type: ApplicationFiled: May 15, 2014Publication date: September 4, 2014Inventors: Angela Wandinger-Ness, Larry Sklar, Jacob Agola, Zurab Surviladze, Jeffrey Aube, Jennifer Golden, Chad E. Schroeder, Denise S. Simpson
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Patent number: 8822523Abstract: Compounds of formula (I) wherein R1 is C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4halogenalkyl; X is methine or nitrogen; A is R5 is hydrogen, halogen, -?-C1-C6alkyl, -?-C3-C7cycloalkyl or -?-aryl; R6 is hydrogen, halogen, -?-C1-C6alkyl, -?-C3-C7cycloalkyl or -?-aryl; and agrochemically acceptable salts/isomers/structural isomers/stereoisomers/diastereoisomers/enantiorners/tautorriers and N-oxides of those compounds are suitable for use as microbiocides.Type: GrantFiled: February 16, 2012Date of Patent: September 2, 2014Assignee: Syngenta Participations AGInventors: Harald Walter, Daniel Stierli
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Publication number: 20140243329Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: ApplicationFiled: May 7, 2014Publication date: August 28, 2014Applicant: Janssen Pharmaceutica, NVInventor: Jay M Matthews
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Publication number: 20140243334Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 5, 2014Publication date: August 28, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
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Publication number: 20140235681Abstract: Disclosed herein is method of treating glaucoma or ocular hypertension comprising administering a prostaglandin agonist and a second therapeutically active agent to a mammal in need thereof, wherein said second therapeutically active agent is selected from: ?-Blockers, Adrenergic Agonists, non-selective adrenergic agonists, ?2-selective adrenergic agonists, Carbonic Anhydrase Inhibitors, Cholinergic Agonists, direct acting cholinergic agonists, chlolinesterase inhibitors, Glutamate Antagonists, Ca2+ channel blockers, Prostamides, Prostaglandins, Cannabinoids, and combinations thereof. Compositions and medicaments containing a combination of these two active agents are also disclosed.Type: ApplicationFiled: December 6, 2013Publication date: August 21, 2014Applicant: ALLERGAN, INC.Inventors: SCOTT M. WHITCUP, ROBERT M. BURK, DAVID W. OLD, YARIV DONDE, WHA-BIN IM, MARK A. HOLOBOSKI
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Publication number: 20140235660Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.Type: ApplicationFiled: February 12, 2014Publication date: August 21, 2014Applicant: NOVARTIS AGInventors: Heather Elizabeth BURKS, Michael A. DECHANTSREITER, Guo HE, Jill NUNEZ, Stefan PEUKERT, Clayton SPRINGER, Yingchuan SUN, Noel Marie-France THOMSEN, George Scott TRIA, Bing YU
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Publication number: 20140235702Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having sulfonamido-1-hydroxynaphthalene structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.Type: ApplicationFiled: October 8, 2012Publication date: August 21, 2014Inventors: Zaneta Nikolovska-Coleska, Hollis D. Showalter, Chenzhong Liao, Ramzi Mohammad, Fardokht Abulwerdi
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Publication number: 20140235619Abstract: This invention relates to methods of screening for modulators of mammalian cell injury cause by TRPM7 gene and protein activity, compounds that modulate TRPM7 gene and protein activity and methods of treatment of mammalian cell injury using modulators of TRPM7 gene and protein activity.Type: ApplicationFiled: November 26, 2013Publication date: August 21, 2014Applicant: NONO INC.Inventors: Xiujun Sun, Michael Tymianski, David Garman
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Patent number: 8809327Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: GrantFiled: February 28, 2012Date of Patent: August 19, 2014Assignee: Janssen Pharmaceutica, NVInventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
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Publication number: 20140228416Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: September 12, 2013Publication date: August 14, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Patent number: 8802721Abstract: The invention relates to compounds of structural formulas (I) and (XVI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, Z, L, L2, R1, R2, R3, R21, n, q, and t are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: January 25, 2006Date of Patent: August 12, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Shoujun Chen, Jun Jiang, Zhi-Qiang Xia, Yu Xie, Chih-Yi Yu
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Publication number: 20140221431Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.Type: ApplicationFiled: June 26, 2012Publication date: August 7, 2014Applicants: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-think Pharmaceutical Co., LtdInventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
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Patent number: 8796275Abstract: The present invention provides tricyclic compounds, arylamide compounds, and other compounds, and compositions comprising the same, for treating malaria, and methods of treating malaria comprising administering such compounds to an animal.Type: GrantFiled: July 28, 2009Date of Patent: August 5, 2014Assignees: The Trustees of the University of Pennsylvania, Cellceutix CorporationInventors: Richard W. Scott, Doron Greenbaum, Dahui Liu, Xiaodong Fan, Yongjiang Xu, Haizhong Tang, Ehab Khalil
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Publication number: 20140213552Abstract: The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.Type: ApplicationFiled: March 20, 2014Publication date: July 31, 2014Applicant: Endo Pharmaceuticals Inc.Inventors: Scott Kevin Thompson, Roger Astbury Smith, Sandeep Gupta, Tony Priestley, Nicholas James Laping, Ashis K. Saha, Sonali Rudra
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Publication number: 20140193376Abstract: The present embodiments provide for combinations of modulators that increase hematopoietic stem cell engraftment or increase mobilization in vivo. Methods and compositions for modulating the mobilization of stem cells, particularly for promoting or increasing the mobilization of hematopoietic stem cells (HSCs) from the bone marrow to the peripheral blood are disclosed. One aspect of the invention relates to the use of a CXCR4 antagonist that act in concert with specific molar ratios of S1P receptor 1 (S1PR1) modulator agents to promote HSC mobilization. The invention also relates to methods of using these combinations of CXCR4 antagonists and S1PR1 modulator agents for enhancing the mobilization of hematopoietic stem cells when harvesting of the stem cells, for example for the treatment of diseases, disabilities or conditions whereby transplantation of such cells would be beneficial in ameliorating a symptom associated with such diseases, disabilities or conditions.Type: ApplicationFiled: June 18, 2012Publication date: July 10, 2014Applicant: CHILDREN'S MEDICAL CENTER CORPORATIONInventors: Leonard I Zon, Owen J. Tamplin
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Patent number: 8772489Abstract: Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.Type: GrantFiled: January 28, 2011Date of Patent: July 8, 2014Assignee: Jiangsu Vcare PharmaTech Co. Ltd.Inventors: Hongbin Sun, Jiaqi Shan, Boyu Zhang, Fang Yuan
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Patent number: 8765803Abstract: This invention relates to compounds and their use as inhibitors or activators of Rab7 GTPase to treat or prevent the onset of Rab 7 GTPase-associated disorders such as neuropathies, cancer, metabolic diseases of bone and lipid storage. The invention is also applicable to infectious diseases where Rab7 is inactivated or its protein-protein interactions are modulated to facilitate intracellular survival of pathogens. The compound described acts as a competitive inhibitor of nucleotide binding and as such also has utility as a scaffold for targeting other small GTPases. In one aspect, methods of treatment of the invention are used to treat or prevent the onset of hereditary sensory neuropathies such as Charcot-Marie-Tooth type 2B disease. Related pharmaceutical compositions, assays, and drug screens are also provided.Type: GrantFiled: February 24, 2012Date of Patent: July 1, 2014Assignees: STC.UNM, University of KansasInventors: Angela Wandinger-Ness, Larry Sklar, Jacob Agola, Zurab Surviladze, Jeffrey Aubé, Jennifer Golden, Chad E. Schroeder, Denise S. Simpson
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Publication number: 20140179752Abstract: The specification discloses compositions and methods for treating a soft tissue defect of an individual.Type: ApplicationFiled: February 25, 2014Publication date: June 26, 2014Applicant: Allergan, Inc.Inventors: Dennis E. Van Epps, Guan-Liang Jiang, Wha Bin Im
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Publication number: 20140171444Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.Type: ApplicationFiled: March 3, 2014Publication date: June 19, 2014Applicant: THE TEXAS A&M UNIVERSITY SYSTEMInventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
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Publication number: 20140171445Abstract: The invention provides a method of enhancing the efficacy of antibiotic treatment of tuberculosis, trypanosomiasis, leprosy, and leishmaniasis involving co-administering to a mammal undergoing antibiotic treatment therapeutically effective amounts of a first compound that is an inhibitor of 5-lipoxygenase and optionally a second compound that is a product of the cyclooxygenase pathways. The invention also provides a pharmaceutical composition comprising an antibiotic, an inhibitor of 5-lipoxygenase, and a product of the cyclooxygenase pathways.Type: ApplicationFiled: August 2, 2012Publication date: June 19, 2014Applicant: The USA, as represented by the Secretary, Department of Health and Human ServicesInventors: Katrin Mayer-Barber, Bruno de Bezerril Andrade, Alan Sher, Daniel Leo Barber
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Publication number: 20140163042Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(?O), —S(?O)2—, —C(?O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic rType: ApplicationFiled: February 13, 2014Publication date: June 12, 2014Applicant: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Charles Moffat, Kenneth William John Baker, Alastair David Graham Donald
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Patent number: 8748478Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: GrantFiled: March 28, 2013Date of Patent: June 10, 2014Assignee: Janssen Pharmaceutica, NVInventor: Jay M Matthews
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Publication number: 20140155415Abstract: The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 4, 2012Publication date: June 5, 2014Inventors: Michael David Bartberger, Michael D. Croghan, Christopher H. Fotsch, Mark H. Norman, Lewis Dale Pennington, Andreas Reichelt, David J. St. Jean, JR., Christopher M. Tegley
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Publication number: 20140154319Abstract: Provided is a pharmaceutical composition for the treatment and prevention of cardiac diseases, containing (a) a therapeutically effective amount of a compound represented by Formula 1 or 2 or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, and (b) a pharmaceutically acceptable carrier, diluent or excipient or any combination thereof.Type: ApplicationFiled: June 21, 2013Publication date: June 5, 2014Inventors: Taehwan KWAK, Myung-Gyu Park
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Publication number: 20140142107Abstract: Antimicrobial agents, compositions that include the agent(s) and use(s) thereof are provided. Also disclosed are screening assays for identifying antimicrobial agents.Type: ApplicationFiled: September 4, 2013Publication date: May 22, 2014Applicant: University of MassachusettsInventors: Paul Kaufman, Jessica Lopes Da Rosa-Spiegler, Reeta Prusty Rao, Ahmed Fazly
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Patent number: 8729068Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.Type: GrantFiled: October 26, 2012Date of Patent: May 20, 2014Assignee: Astellas Pharma Inc.Inventors: Shunichiro Hachiya, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
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Publication number: 20140135322Abstract: The present invention relates to novel chemical compounds formula (I) (C)n—B-(A)m-B—(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (—CO—), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.Type: ApplicationFiled: July 13, 2012Publication date: May 15, 2014Inventors: Peter Asberg, Kristin Hammer, Johan Olsson, Martin Henriksson
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Publication number: 20140121246Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: October 15, 2013Publication date: May 1, 2014Applicant: Metabolex, Inc.Inventors: Dong Fang Shi, Jiangao Song, Christopher J. Rabbat, Jingyuan Ma, Aaron Novack, Imad Nashashibi, Xin Chen
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Patent number: 8710245Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.Type: GrantFiled: December 3, 2010Date of Patent: April 29, 2014Assignees: PsychoGenics Inc., Sunovion Pharmaceuticals Inc.Inventors: Liming Shao, John Emmerson Campbell, Michael Charles Hewitt, Una Campbell, Taleen G. Hanania
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Quinoid thiophene organic photoelectric material, preparation method thereof and application thereof
Patent number: 8710094Abstract: Quinoid thiophene organic photoelectric material with formula (1), method for its preparation and application thereof are provided, wherein R1, R2, R3, R4, R5 and R6, which are identical or different, represent H, C1˜C30 alkyl or alkoxy, m and n, which are identical or different, represent integers between 1 and 20. The quinoid thiophene organic photoelectric material with formula (1) has wide spectral response, good thermal stability and environmental stability.Type: GrantFiled: January 30, 2010Date of Patent: April 29, 2014Assignee: Ocean's King Lighting Science & Technology Co., Ltd.Inventors: Mingjie Zhou, Jie Huang, Hui Liu -
Patent number: 8709747Abstract: The invention relates to compounds of formula (I) wherein the groups A and B represent independently from each other —CH?CH—, or —C?C—, the terms t, u, v, w represent, independently from each other, values ranging from 0 to 9, the groups Y1 and Y2 can represent independently from each other an alkyl group (linear, branched or substituted) carrying from 1 to 9 carbon atoms, the groups Z1, Z2, Z3, and Z4 can represent independently from each other a chemically reactive group W, such as OH, NH2, SH, the groups Z5 and Z6 represent independently from each other a hydrogen atom, silica nanoparticles functionalized by these compounds, and their use as drugs.Type: GrantFiled: December 7, 2010Date of Patent: April 29, 2014Assignees: Centre National de la Recherche Scientifique, Universite de Rennes 1, I.N.S.E.R.M. (Institut National de la Sante et de la Recherche Medicale), Universite Montpellier 2 Sciences et TechniquesInventors: David Brevet, Laurence Raehm, Mireille Blanchard-Desce, Olivier Mongin, Magali Gary-Bobo-Sable-Teychene, Marcel Garcia, Alain Morere, Jean-Olivier Durand
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Patent number: 8703970Abstract: Disclosed herein are compounds having photoremovable protecting groups which are removed after the compounds absorbs light of a given wavelength and undergo an electrocyclic reaction between a chromophore in the compound attached via an anilide to a benzothiophene ring.Type: GrantFiled: February 27, 2013Date of Patent: April 22, 2014Assignee: Marquette UniversityInventors: Mark G. Steinmetz, Majher I. Sarker, Tasnuva Shahrin
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Patent number: 8697744Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, Y, Z1, Z2, Z3, M and (A)m are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: GrantFiled: January 12, 2010Date of Patent: April 15, 2014Assignee: Addex Pharma S.A.Inventors: Christelle Boléa, Sylvain Celanire
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Patent number: 8691839Abstract: The present application relates generally to amino tetraline derivative compounds and methods of use, specifically, embodiments including compounds of formula (I) described herein, pharmaceutically acceptable salts and solvates. More specifically, this application relates to amino tetraline derivative compounds and uses of such compounds producing medicaments for the treatment of various disease and conditions including movement disorders and disorders of the central nervous system.Type: GrantFiled: August 15, 2013Date of Patent: April 8, 2014Inventors: Peter Gmeiner, Miriam Ruberg, Harald Huebner
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Publication number: 20140094507Abstract: The present invention provides compounds and compositions that can modulate formation of Toll-like receptor 3 (TLR3) and double-stranded RNA (dsRNA) complex, and methods for using the same. In particular, some aspects of the invention provide compounds of the formula: compositions comprising and methods for using the same, where n, Ar1, Ar2, X1, X2, X3, Z1, and Z2 are those defined herein.Type: ApplicationFiled: January 13, 2012Publication date: April 3, 2014Applicant: The Regents of the University of Colorado, a body corporateInventors: Hang Yin, Kui Cheng
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Publication number: 20140088079Abstract: The present invention relates to a compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The present invention also provides a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.Type: ApplicationFiled: June 1, 2012Publication date: March 27, 2014Applicant: GREEN CROSS CORPORATIONInventors: Soongyu Choi, Kwang Seop Song, Suk Ho Lee, Min Ju Kim, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, So Ok Park, Hyunku Kang, Myung Eun Jung, Kinam Lee, Hyun Jung Kim, Jun Sung Lee, Min Woo Lee, Mi-Soon KIM, Dong Ho Hong, Misuk Kang
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Patent number: 8680100Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: GrantFiled: December 1, 2009Date of Patent: March 25, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Patent number: 8680137Abstract: This invention relates to methods of screening for modulators of mammalian cell injury cause by TRPM7 gene and protein activity, compounds that modulate TRPM7 gene and protein activity and methods of treatment of mammalian cell injury using modulators of TRPM7 gene and protein activity.Type: GrantFiled: December 13, 2010Date of Patent: March 25, 2014Assignee: Nono Inc.Inventors: Xiujun Sun, Michael Tymianski, Jonathan David Garman
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Patent number: 8680138Abstract: A soluble oligomeric compound for forming an organic thin film transistor, has repeat units comprising two or more fused thiophene residues. The repeat units comprise the structure: The compound may include two or more terminating groups comprising solvating groups. A solution of the material can be used to form a thin film transistor by ink jet printing.Type: GrantFiled: November 27, 2009Date of Patent: March 25, 2014Assignee: Cambridge Display Technology LimitedInventors: Tania Zuberi, Sheena Zuberi
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Publication number: 20140066494Abstract: The invention relates to the use of lipooxigenase inhibitors for treating acne, particularly inflammatory acne. The inventive lipooxigenase inhibitor can be used alone or in combination with other lipooxigenase inhibitors or anti-acne active agents in a pharmaceutically suitable composition, particularly through oral and/or local-topic application.Type: ApplicationFiled: December 17, 2012Publication date: March 6, 2014Inventor: Christos C. Zouboulis
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Patent number: 8664263Abstract: An object is to provide a novel stilbene compound suitable for an organic EL light-emitting material. Provided is a novel stilbene compound represented by a general formula (G1) below. In the formula, Q1 and Q2 separately represent an oxygen atom or a sulfur atom; R1 to R9 and R11 to R17 separately represent any one of a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted phenyl group, and a substituted or unsubstituted biphenyl group; ?1 to ?6 separately represent a substituted or unsubstituted phenylene group; Ar1 and Ar2 separately represent any one of a substituted or unsubstituted aryl group having 6 to 12 carbon atoms forming a ring, a substituted or unsubstituted dibenzothiophen-2-yl group, and a substituted or unsubstituted dibenzofuran-2-yl group; and j, k, m, n, p, and q separately represent 0 or 1.Type: GrantFiled: January 12, 2012Date of Patent: March 4, 2014Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Harue Osaka, Nobuharu Ohsawa
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Publication number: 20140051711Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: October 14, 2013Publication date: February 20, 2014Applicant: CalciMedica Inc.Inventors: Jeffrey P. WHITTEN, Yazhong PEI, Jianguo CAO, Zhijun WANG, Evan ROGERS
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Patent number: 8653285Abstract: An aminopropylidene derivative having excellent histamine receptor antagonistic action, a compound which is useful as a pharmaceutical composition, especially as an active ingredient, having alleviated side effects in the central nervous system is described. In the aminopropylidene derivative, R1 and R2, which may be identical or different, stand for a hydrogen, a substituted carbonyl, a substituted carbonylalkyl, and acrylic acid, excluding a case where both are hydrogen; R3 and R4, which may be identical or different, stand for hydrogen, an alkyl which may be substituted with phenyl, or the like; A stands for unsubstituted or an oxo; B stands for a carbon or an oxygen; one of X and Y stands for a carbon and the other stands for a sulfur, a broken line part stands for a single bond or a double bond, and a wavy line stands for cis-form and/or trans-form.Type: GrantFiled: July 31, 2009Date of Patent: February 18, 2014Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Kunihiko Higashiura, Takashi Ogino, Taizo Ito, Koji Kunimasu, Kazuhito Furukawa
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Publication number: 20140045821Abstract: Compounds according to Formula (I), are potent inhibitors of protein kinase D (pan-PKD) activity. PKD controls key signaling cascades in cells, affecting cell proliferation, gene transcription, and protein trafficking. Accordingly, pharmaceutically acceptable compositions of the inventive compounds are candidate therapeutics for pathological conditions conditioned by changes in PKD activity.Type: ApplicationFiled: December 8, 2011Publication date: February 13, 2014Inventors: Peter Wipf, Qiming Jan Wang
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Publication number: 20140045884Abstract: Methods for the treatment of cognitive, emotional and mental ailments using therapeutically effective amounts of compositions including leukotriene receptor antagonists, leukotriene synthesis inhibitors or leukotriene modifiers, zafirlukasts, montelukasts, other members of the family—lukasts, zileutons.Type: ApplicationFiled: October 18, 2013Publication date: February 13, 2014Inventor: Jack William Schultz
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Publication number: 20140044799Abstract: The present invention concerns a molecular signature of cutaneous pigmentary spots, comprising the genes MXRA5, LYZ, CTSL2, PLAU, TIMP1, EFEMP1, ECM1, ASPN, HS3ST6, PAPLN, CHSY1 and FLRT2, and various applications of this signature. In particular, the invention concerns a method for characterizing a known or suspected pigmentary spot in a human being, comprising comparing the levels of expression in skin samples obtained from said spot and from adjacent undamaged skin, of at least one dermal gene linked to matrix remodelling or to its extracellular proteoglycan and glycoprotein components, selected from the list constituted by the genes MXRA5, LYZ, CTSL2, PLAU, TIMP1, EFEMP1, ECM1, ASPN, HS3ST6, PAPLN, CHSY1 and FLRT2. The invention also concerns methods for evaluating the efficacy of a pigmentary spot treatment, cosmetic and therapeutic methods for the treatment of pigmentary spots, and various modulators for said genes, and their use.Type: ApplicationFiled: April 20, 2012Publication date: February 13, 2014Applicant: L'OREALInventors: Francoise Bernerd, Christine Duval, Olivier De Lacharriere, Stephanie Nouveau, Xavier Marat