Chalcogen Attached Indirectly To The Bicyclo Ring System By Acyclic Nonionic Bonding Patents (Class 548/509)
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Patent number: 9708257Abstract: A photoacid includes a nucleophilic (NuH) moiety having a photodissociable proton, an electron accepting (EA) moiety, and a bridge structure (X) bonded to both the NuH moiety and EA moiety positioned between the NuH and EA moieties. The NuH and EA moieties each include respective structure so that the EA moiety bonds to a proton photodissociated form of the NuH moiety during a reversible photoinduced intramolecular reaction to form a ring, which has been found to significantly increase the lifetime of the proton dissociation state.Type: GrantFiled: January 23, 2013Date of Patent: July 18, 2017Assignee: University of Central Florida Research Foundation, Inc.Inventor: Yi Liao
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Patent number: 8993616Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.Type: GrantFiled: May 16, 2013Date of Patent: March 31, 2015Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Patent number: 8987321Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.Type: GrantFiled: June 27, 2013Date of Patent: March 24, 2015Assignee: University of Virginia Patent FoundationInventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
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Publication number: 20150065487Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: November 11, 2014Publication date: March 5, 2015Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Patent number: 8957104Abstract: This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.Type: GrantFiled: July 15, 2013Date of Patent: February 17, 2015Assignee: GlaxoSmithKline Intellectual Property (No. 2) LimitedInventors: Philip Stewart Turnbull, Rodolfo Cadilla
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Publication number: 20150031722Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: October 6, 2014Publication date: January 29, 2015Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Patent number: 8871948Abstract: An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.Type: GrantFiled: February 15, 2013Date of Patent: October 28, 2014Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Maria Alessandra Alisi, Guido Furlotti, Nicola Cazzolla, Caterina Maugeri, Patrizia Dragone, Barbara Garofalo, Isabella Coletta, Giorgina Mangano, Beatrice Garrone
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Publication number: 20140296524Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.Type: ApplicationFiled: May 5, 2014Publication date: October 2, 2014Applicant: Nanoquantum Sciences, Inc.Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
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Patent number: 8829040Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.Type: GrantFiled: February 28, 2014Date of Patent: September 9, 2014Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Publication number: 20140234883Abstract: Use of photochemically cleavable compounds in course of one or multi-photon irradiation experiments.Type: ApplicationFiled: October 3, 2012Publication date: August 21, 2014Applicant: FEMTONICS KFTInventors: Imre Gyula Csizmadia, Zoltan Mucsi, Gergely Szalay, Attila Kaszas, Csilla Lukacsne Haveland, Orsolya Majercsik, Attila Potor, Gergely Katona, Jozsef Balazs Rozsa, Dorina Gundisch, Balazs Chiovini, Denes Palfi
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Patent number: 8801976Abstract: Photochromic dyes are disclosed. A photochromic dye can include a first photo-reactive group and a second photo-reactive group. A first photochromic reaction can be induced in the first photo-reactive group of the photochromic dye by radiation having a first wavelength, and a second photochromic reaction can be induced in the second photo-reactive group of the photochromic dye by radiation having a second wavelength.Type: GrantFiled: September 28, 2012Date of Patent: August 12, 2014Assignee: Korea University Research and Business FoundationInventor: Dong Hoon Choi
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Patent number: 8796247Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a pyridine ring, a furan ring, or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents —C(?O)—NH—SO2R6, an acidic 5-membered hetero ring group, or the like; R2 represents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: GrantFiled: January 24, 2012Date of Patent: August 5, 2014Assignees: Kissei Pharmaceutical Co., Ltd., Kyorin Pharmaceutical Co., Ltd.Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
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Publication number: 20140155431Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: December 19, 2013Publication date: June 5, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Patent number: 8680133Abstract: Compounds and methods for treating cancer or inducing apoptosis in proliferating cells. The compounds are shown in formula I: wherein X is selected from hydroxyl, thiol, and amino; Y is selected from carboxyl and sulfonyl; R1, R2, R3, and R4 are selected from hydrogen, lower alkyl, and combinations thereof; R5, R6, and R7 are selected from hydrogen, halo, ni tro, amino, methoxy, and combinations thereof; and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 26, 2012Date of Patent: March 25, 2014Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Jing-Ru Weng
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Publication number: 20140018335Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a pyridine ring, a furan ring, or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents —C(?O)—NH—SO2R6, an acidic 5-membered hetero ring group, or the like; R2 represents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: ApplicationFiled: January 24, 2012Publication date: January 16, 2014Applicant: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
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Publication number: 20140018355Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.Type: ApplicationFiled: June 27, 2013Publication date: January 16, 2014Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Timothy L. MACDONALD, Jerry L. NADLER, Peng CUI
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Publication number: 20140011807Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.Type: ApplicationFiled: March 15, 2012Publication date: January 9, 2014Applicants: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD., MITSUBISHI TANABE PHARMA CORPORATIONInventors: Toru Iijima, Hiroshi Sugama, Takayuki Kawaguchi, Jingkang Shen, Guangxin Xia, Jianshu Xie
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Publication number: 20130331419Abstract: Disclosed are the compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, which are useful for treating aldosterone-mediated diseases. The processes for preparing compounds of the Formula (I), the use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and the pharmaceutical compositions which comprise compounds of the formula (I) are disclosed too.Type: ApplicationFiled: January 19, 2012Publication date: December 12, 2013Inventors: Alejandro Crespo, Ping Lan, Rudrajit Mal, Anthony Ogawa, Hong Shen, Peter J. Sinclair, Zhongxiang Sun, Ellen K. Vande Bunte, Zhicai Wu, Kun Liu, Robert J. DeVita, Dong-Ming Shen, Min Shu, John Qiang Tan, Changhe Qi, Yuguang Wang, Richard Beresis
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Publication number: 20130317223Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.Type: ApplicationFiled: November 6, 2012Publication date: November 28, 2013Applicant: The Board of Trustees of the University of IllinoisInventors: Martin D. Burke, David M. Knapp, Eric P. Gillis
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Publication number: 20130296281Abstract: The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R1, and Z1-Z5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: June 16, 2011Publication date: November 7, 2013Applicant: Purdue Pharma L.P.Inventors: Donald J. Kyle, Chiyou Ni, Laykea Tafesse, Jiangchao Yao
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Patent number: 8546392Abstract: The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases. The invention further relates to suitable inhibitors and to a method for the production thereof.Type: GrantFiled: March 27, 2008Date of Patent: October 1, 2013Assignee: Universitaet des SaarlandesInventors: Rolf Hartmann, Martin Frotscher, Sandrine Oberwinkler, Erika Ziegler, Josef Messinger, Heinrich-Hubert Thole
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Publication number: 20130231604Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.Type: ApplicationFiled: March 3, 2012Publication date: September 5, 2013Applicant: NANOQUANTUM SCIENCES, INC.Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
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Publication number: 20130217876Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) catalyst compositions comprising phosphacycle ligands; and (c) methods of using such phosphacycle ligands and catalyst compositions in bond forming reactions.Type: ApplicationFiled: August 21, 2012Publication date: August 22, 2013Applicant: ABBVIE INC.Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
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Publication number: 20130192978Abstract: A photoacid includes a nucleophilic (NuH) moiety having a photodissociable proton, an electron accepting (EA) moiety, and a bridge structure (X) bonded to both the NuH moiety and EA moiety positioned between the NuH and EA moieties. The NuH and EA moieties each include respective structure so that the EA moiety bonds to a proton photodissociated form of the NuH moiety during a reversible photoinduced intramolecular reaction to form a ring, which has been found to significantly increase the lifetime of the proton dissociation state.Type: ApplicationFiled: January 23, 2013Publication date: August 1, 2013Applicant: University of Central Florida Research Foundation, Inc.Inventor: University of Central Florida Research Foundation, Inc.
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Publication number: 20130190339Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protecting from neuron cell death.Type: ApplicationFiled: December 10, 2012Publication date: July 25, 2013Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEMInventor: Board of Regents of the University of Texas System
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Publication number: 20130158269Abstract: An (aza)indole derivative substituted in position 5, of formula (I) in which X, Y, Z, G1, G2, G3, R1, W, and R2 have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.Type: ApplicationFiled: February 15, 2013Publication date: June 20, 2013Applicant: AZIENDE CHIMICHE RIUNITE ANGELIN FRANCESCO A.C.R.A.F. S.P.A.Inventor: Aziende Chimiche Riunite Angelin Francesco A.C.R.A.F S.P.A.
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Patent number: 8466152Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.Type: GrantFiled: May 26, 2011Date of Patent: June 18, 2013Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
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Patent number: 8445697Abstract: The present invention relates to squarylium dyes including an anchoring group, to a method of synthesis of such dye, to an electronic device comprising such dye, and to uses of such dye.Type: GrantFiled: October 27, 2008Date of Patent: May 21, 2013Assignee: Sony CorporationInventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Akio Yasuda
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Patent number: 8440711Abstract: The present invention relates to (R,S) 2-aryl-2-fluoropropanoic acids, their single enantiomers (R) and (S), their derivatives amides and acylsulfonamides and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PMN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: December 18, 2007Date of Patent: May 14, 2013Assignee: Dompe Pha.r.ma S.p.A.Inventors: Marcello Allegretti, Andrea Aramini, Maria Candida Cesta
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Patent number: 8440840Abstract: A dye including an anchoring group in its molecular structure, said anchoring group allowing a covalent coupling of said dye to a surface, for example a surface of a nanoporous semiconductor layer, said anchoring group being represented by formula 1 wherein attachment of said anchoring group within said molecular structure of said dye is at the terminal carbon marked with an asterisk in above formula, wherein G is selected from —COOH, —SO3H, —PO3H2, —BO2H2, —SH, —OH, —NH2, preferably —COOH, wherein A is selected from the group comprising H, —CN, —NO2, —COOR, —COSR, —COR, —CSR, —NCS, —CF3, —CONR2-OCF3, C6H5-mFm, wherein m=1-5, R being H or any straight or branched alkyl chain of general formula —CnH2n+I, n=O-12, preferably 0-4, or any substituted or non-substituted phenyl or biphenyl.Type: GrantFiled: October 27, 2008Date of Patent: May 14, 2013Assignee: Sony CorporationInventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Akio Yasuda
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Publication number: 20130095040Abstract: The present invention relates to sulfonated unsymmetrical pentamethine optical dye compositions, especially dyes suitable for biological applications in vitro, and for in vivo imaging. Improved dye compositions and intermediates are provided, which enable the suppression of undesirable newly-identified impurities. Also provided is the use of the improved dye compositions in the preparation of conjugates with biological targeting molecules.Type: ApplicationFiled: June 29, 2011Publication date: April 18, 2013Applicant: GE HEALTHCARE ASInventor: Umamaheshwar P. Mokkapati
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Publication number: 20130040977Abstract: 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.Type: ApplicationFiled: August 24, 2012Publication date: February 14, 2013Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
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Patent number: 8367665Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.Type: GrantFiled: April 16, 2009Date of Patent: February 5, 2013Assignee: Karo Bio ABInventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20130030008Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: October 1, 2012Publication date: January 31, 2013Applicant: SANOFIInventor: Sanofi -
Patent number: 8304537Abstract: Heterocyclic compounds incorporating a [1,3]oxazine ring may be used to make chromogenic materials. These molecules switch from a colorless state to a colored form upon addition of either acid or base. In both instances, the [1,3]oxazine ring opens in response to the pH change forming an indolium cation, after the addition of acid, or a phenolate anion, after the addition of base. Alternatively, the switch may occur in response to a change in electrical current or potential or a change in temperature. Chromophores absorb in the visible region of the electromagnetic spectrum. Hence, their formation translates into the appearance of color. These processes are fully reversible and the original colorless state can be regenerated by switching the pH back to neutral. Thus, these halochromic compounds can be used to develop displays, filters, indicators, lenses, sensors, switches, or windows able to switch their color in response to pH changes.Type: GrantFiled: October 17, 2008Date of Patent: November 6, 2012Assignee: The University of MiamiInventors: Massimiliano Tomasulo, Francisco M. Raymo
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Patent number: 8298453Abstract: Photochromic dyes are disclosed. A photochromic dye can include a first photo-reactive group and a second photo-reactive group. A first photochromic reaction can be induced in the first photo-reactive group of the photochromic dye by radiation having a first wavelength, and a second photochromic reaction can be induced in the second photo-reactive group of the photochromic dye by radiation having a second wavelength.Type: GrantFiled: January 6, 2010Date of Patent: October 30, 2012Assignee: Korea University Research and Business FoundationInventor: Dong Hoon Choi
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Patent number: 8287775Abstract: Photochromic dyes are disclosed. A photochromic dye can include a first photo-reactive group and a second photo-reactive group. A first photochromic reaction can be induced in the first photo-reactive group of the photochromic dye by radiation having a first intensity, and a second photochromic reaction can be induced in the second photo-reactive group of the photochromic dye by radiation having a second intensity. The second intensity may be greater than the first intensity.Type: GrantFiled: February 17, 2010Date of Patent: October 16, 2012Assignee: Korea University Research and Business FoundationInventor: Dong Hoon Choi
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Publication number: 20120232070Abstract: Compounds derived from indole, notably useful in therapeutics, selected from: i) the compounds of formula: and ii) the pharmaceutically acceptable salts of the compounds of formula (I); in which R1, R2, R3, R4, R5, R6, R8, R9 and Cy have defined meanings, and the use of such compounds in pharmaceuticals for the treatment of neurodegenerative diseases, particularly Parkinson's disease.Type: ApplicationFiled: March 9, 2012Publication date: September 13, 2012Applicant: Laboratoires Fournier SAInventors: Jerome Amaudrut, Benaissa Boubia, Maria Johanna Petronella Van Dongen, Fabrice Guillier, Olivia Poupardin-Olivier
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Publication number: 20120225873Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.Type: ApplicationFiled: April 13, 2012Publication date: September 6, 2012Applicant: Myrexis, Inc.Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
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Patent number: 8252209Abstract: We have designed a molecular switch based on the photoinduced opening and thermal closing of a [1,3]oxazine ring. A substituted [1,3]oxazine compound described as having a general (i.e., unsubstituted) structure with fused indoline and benzooxazine fragments such that they share a common bond in the [1,3]oxazine compound: (i) the bond connecting positions 1 and 2 of the indoline fragment and (ii) the bond connecting positions 2 and 3 of the benzooxazine fragment. Irradiation by light of suitable wavelength and intensity of this photochromic compound induces cleavage of a [C—O] bond of the [1,3]oxazine ring to form a phenolate chromophore. The photogenerated (e.g., colored) isomer may revert thermally to the starting (e.g., colorless) oxazine. Alternatively, the switch may be between isomers of the compound that absorb at different wavelengths. Reversible coloration of silica or polymeric materials and switching optical signals may involve many cycles of interconversion between different colored states.Type: GrantFiled: August 6, 2010Date of Patent: August 28, 2012Assignee: The University of MiamiInventors: Francisco M. Raymo, Massimiliano Tomasulo
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Patent number: 8232312Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: GrantFiled: March 14, 2008Date of Patent: July 31, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
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Patent number: 8153680Abstract: Compounds and methods for treating cancer or inducing apoptosis in proliferating cells. The compounds are shown in formula I: wherein X is selected from hydroxyl, thiol, and amino; Y is selected from carboxyl and sulfonyl; R1, R2, R3, and R4 are selected from hydrogen, lower alkyl, and combinations thereof; R5, R6, and R7 are selected from hydrogen, halo, nitro, amino, methoxy, and combinations thereof; and pharmaceutically acceptable salts thereof.Type: GrantFiled: August 25, 2009Date of Patent: April 10, 2012Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Jing-Ru Weng
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Patent number: 8129424Abstract: This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their salts and solvates. These compounds have H3 histamine receptor antagonist activity. This invention also relates to pharmaceutical compositions containing these compounds and to a method of treating disorders in which histamine H3 receptor blockade is beneficial.Type: GrantFiled: November 10, 2010Date of Patent: March 6, 2012Assignee: Athersys, Inc.Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emilie Porter Huck
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Patent number: 8119683Abstract: Aryl substituted sulfonamide compounds of formula (I): wherein bond, X, Y, R1, R2, R3, m, and n are defined herein. Also disclosed is a method for treating cancer with these compounds.Type: GrantFiled: August 9, 2010Date of Patent: February 21, 2012Assignees: Taipei Medical University, DCB-USA LLC, National Health Research InstitutesInventors: Jing-Ping Liou, Jang-Yang Chang
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Publication number: 20120041207Abstract: A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.Type: ApplicationFiled: August 10, 2011Publication date: February 16, 2012Applicant: Sterix LimitedInventors: Nigel Vicker, Su Xiangdong, Dharshini Ganeshapillai, Atul Purohit, Michael John Reed, Barry Victor Lloyd Potter
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Publication number: 20120035371Abstract: The current invention describes novel chiral synthetic routes and intermediates for the manufacture of chiral anti-inflammatory agents of general formula VIII in which at least one of the groups X1, X2, X3 is selected from fluoro, chloro, bromo, hydroxy, methoxy, ethoxy, trifluoromethyl, amino whereas the other groups X1, X2, X3 have the meaning of a hydrogen atom, in which at least one of the groups Z1, Z2, Z3 is selected from —O—, —S—, —NH—, —N(—CH3)—, whereas the other groups Z1, Z2, Z3 have the meaning of a —CH2— group, and in which Ar is an aromatic group.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Inventor: Steffen SCHWEIZER
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Publication number: 20110286933Abstract: The present invention provides symmetric carbocyanine dyes and dye precursors useful for fluorescence microscopy, and methods of making and using same.Type: ApplicationFiled: November 9, 2009Publication date: November 24, 2011Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Scott A. Hilderbrand, Ralph Weissleder, Fangwei Shao
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Patent number: 8063234Abstract: The present application relates to novel 7-sulfanylmethyl-, 7-sulfinylmethyl- and 7-sulfonylmethylindole derivatives, processes for the preparation thereof, the use thereof alone or in combinations for the treatment and/or prevention of diseases, and the use thereof for the manufacture of medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: June 24, 2009Date of Patent: November 22, 2011Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Peter Kolkhof, Astrid Brüns, Kai Thede, Karl-Heinz Schlemmer, Alexander Hillisch, Dieter Lang, Michael Gerisch, Andreas Goeller, Rolf Grosser, Carsten Schmeck, Elisabeth Woltering, Olaf Prien, Holger Paulsen, Armin Kern
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Publication number: 20110245315Abstract: Indolyl or indolinyl compounds of formula (I): wherein bond, n, R1, R2, R3, R4, R5, and R6, are defined herein. Also disclosed is a method for treating cancer with these compounds.Type: ApplicationFiled: March 29, 2011Publication date: October 6, 2011Applicants: Taipei Medical University, Ohio State University, National Taiwan UniversityInventors: Ching-Shih Chen, Jing-Ping Liou, Hsing-Jin Liu, Kuo-Sheng Hung, Pei-Wen Shan, Wen-Ta Chiu, Che-Ming Teng
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Publication number: 20110230651Abstract: The present invention is related to derivatives of benzenesulfonamide represented by formula (I), and the pharmaceutical composition thereof. In addition, the benzenesulfonamide derivatives disclosed in the present invention can serve as potential cell cycle inhibitors, and thereby these benzenesulfonamide derivatives and the pharmaceutical composition thereof can be antitumor drug candidates, which might aim at cell cycle. Particularly, the benzenesulfonamide derivatives disclosed in the present invention may function as antitumor drugs to treat solid cancers.Type: ApplicationFiled: February 23, 2011Publication date: September 22, 2011Applicant: Purzer Pharmaceutical Co., LTD.Inventors: Ji-Wang Chern, Grace Shiahuy Chen, Pei-Teh Chang, Kuan-Yu Chen, Meng-Ling Chen, Hsueh-Yun Lee, Chiung Hua Huang, Chun-Tang Chiou