Bicyclo Ring System Which Is Indole (including Hydrogenated) Patents (Class 546/277.4)
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Patent number: 8476289Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, A and X have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: March 26, 2009Date of Patent: July 2, 2013Assignee: Janssen Pharmaceutica NVInventors: Eddy Jean Edgard Freyne, Isabelle Noëlle Constance Pilatte, Patrick René Angibaud
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Publication number: 20130165475Abstract: The present invention provides deuterium-enriched heteroaryl-containing urea compounds (I) and use of the same for treating conditions mediated by protein kinase such asType: ApplicationFiled: September 1, 2011Publication date: June 27, 2013Applicant: ASCEPION PHARMACEUTICALS, INC.Inventors: Shan Jiang, Qishan Wang, Xiaoyong Gao
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Publication number: 20130137648Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: January 23, 2013Publication date: May 30, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Publication number: 20130137686Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: November 5, 2012Publication date: May 30, 2013Inventor: Esanex, Inc.
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Publication number: 20130131084Abstract: The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.Type: ApplicationFiled: August 17, 2012Publication date: May 23, 2013Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Catherine GUILLOU, Frank Kozielski, Christophe Labriere, Francoise Gueritte, Sergey Tcherniuk, Dimitrios Skoufias, Claude Thal, Henri-Philippe Husson
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Publication number: 20130112948Abstract: A heterocyclic compound represented by Formula 1A below and an organic light-emitting diode including the same: at least one of R1 to R7 is a group represented by Formula 1B below. in Formulae 1A and 1B, R1 to R9, Ar1, Ar2, A, B, a and b are the same as described in the detailed description section of the present application. The organic light-emitting diode including an organic layer including the heterocyclic compound has a low driving voltage, high luminescence efficiency, and a long lifetime.Type: ApplicationFiled: May 25, 2012Publication date: May 9, 2013Applicant: Samsung Mobile Display Co., Ltd.Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jin-O Lim, Sang-Hyun Han, Soo-Yon Kim, Jin-Young Yun, Jong-Hyuk Lee
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Publication number: 20130084346Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.Type: ApplicationFiled: February 28, 2011Publication date: April 4, 2013Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, B. Wesley Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan Kett, Amy Zartman
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Patent number: 8410144Abstract: The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: March 31, 2010Date of Patent: April 2, 2013Assignee: ArQule, Inc.Inventors: Nivedita Namdev, Manish Tandon, Jianqiang Wang, Audra Dalton, David Vensel, Rocio Palma, Mark A. Ashwell, Neil Westlund
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Publication number: 20130079343Abstract: Disclosed are a 1,3,6-substituted indole compound having inhibitory activity for protein kinases, a pharmaceutically acceptable thereof, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth including the compound as an active ingredient. Since the novel indole compound exhibits superior inhibitory activity for various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.Type: ApplicationFiled: November 24, 2012Publication date: March 28, 2013Applicant: Korea Institute of Science and TechnologyInventor: Korea Institute of Science and Technology
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Patent number: 8404683Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.Type: GrantFiled: November 3, 2010Date of Patent: March 26, 2013Assignee: Janssen Pharmaceutical N.V.Inventors: Jean Ferand Armand Lacrampe, Christophe Meyer, Yannick Aimè Eddy Ligny, Imre Christian Francis Csoka, Luc Van Hijfte, Janine Arts, Bruno Schoentjes, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert
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Patent number: 8394836Abstract: Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.Type: GrantFiled: December 12, 2008Date of Patent: March 12, 2013Assignee: Pulmagen Therapeutics (Asthma) LimitedInventors: George Hynd, John Gary Montana, Harry Finch, Rosa Arienzo, Barbara Avitabile-Woo, Mathias Domostoj
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Patent number: 8377961Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, t, R1, R2, R3, R4, R5, R6, R7, Q, Y and Z have defined meanings.Type: GrantFiled: November 30, 2011Date of Patent: February 19, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Jean Fernand Armand Lacrampe, Christophe Meyer, Bruno Schoentjes, Alain Philippe Poncelet, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert, Luc Van Hijfte
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Patent number: 8377941Abstract: The present invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of List A or a salt thereof, which may be represented, but is not limited to the compound N-[(2-Trifluoromethyl-1H-indol-5-yl)methyl]-2-(trifluoromethyl)-5-pyrimidinecarboxamide.Type: GrantFiled: April 16, 2009Date of Patent: February 19, 2013Assignee: Proximagen LimitedInventors: Kevin Dinnell, Andrew P Lightfoot, Howard Robert Marshall
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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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Publication number: 20130035354Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: September 14, 2012Publication date: February 7, 2013Applicant: NOVARTIS AGInventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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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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Publication number: 20120322800Abstract: Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).Type: ApplicationFiled: October 14, 2010Publication date: December 20, 2012Inventor: Julian Blagg
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Publication number: 20120322831Abstract: Novel small molecule compounds for reduction of A? 42 production and for treatment of Alzheimer's Disease and other neurodegenerative disorders, methods of making them and pharmaceutical compositions containing them are described.Type: ApplicationFiled: January 22, 2011Publication date: December 20, 2012Applicant: KAREUS THERAPEUTICS SAInventors: Venkateswarlu Akella, Uday Saxena, Anji Reddy Kallam
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Patent number: 8329708Abstract: Disclosed are a 1,3,6-substituted indole compound having inhibitory activity for protein kinases, a pharmaceutically acceptable thereof, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth including the compound as an active ingredient. Since the novel indole compound exhibits superior inhibitory activity for various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.Type: GrantFiled: August 17, 2010Date of Patent: December 11, 2012Assignee: Korea Institute of Science and TechnologyInventors: Tae Bo Sim, Young Jin Ham, Kyung Ho Yoo, Chang Hyun Oh, Jung Mi Hah, Hwan Kim, Hwan Geun Choi, Jung-Hun Lee
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Publication number: 20120309769Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects such as significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: June 6, 2012Publication date: December 6, 2012Applicant: SCRIPPS RESEARCH INSTITUTE, THEInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Publication number: 20120309757Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: June 6, 2012Publication date: December 6, 2012Applicant: SCRIPPS RESEARCH INSTITUTE, THEInventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
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Publication number: 20120302576Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.Type: ApplicationFiled: August 9, 2012Publication date: November 29, 2012Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
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Patent number: 8299066Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: GrantFiled: January 20, 2012Date of Patent: October 30, 2012Assignee: Shionogi & Co., Ltd.Inventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka
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Publication number: 20120270879Abstract: Disclosed are CCR1 receptor antagonists of the formula (I) wherein Ar1, Ar2, R1-R3, X and L are disclosed herein. Also disclosed are compositions, methods of making and using compounds of the formula (I).Type: ApplicationFiled: October 21, 2010Publication date: October 25, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Brian Nicholas Cook, Daniel Kuzmich
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Publication number: 20120258948Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of formula I, wherein the variables G, T, D, L, R1, R2, R3 are as described herein, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections in a patient in need thereof.Type: ApplicationFiled: December 6, 2010Publication date: October 11, 2012Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
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Publication number: 20120258947Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: April 18, 2012Publication date: October 11, 2012Applicant: Grunenthal GmbHInventors: Sven KÜHNERT, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
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Patent number: 8283365Abstract: This invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereofType: GrantFiled: April 16, 2009Date of Patent: October 9, 2012Assignee: Proximagen LimitedInventors: Kevin Dinnell, Andrew P Lightfoot, Howard Robert Marshall
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Publication number: 20120244074Abstract: The present invention provides alternative in vivo imaging agents suitable for use in the detection of ?v?6 expressed in a subject. The invention also provides a method for obtaining said in vivo imaging agents, and use of the in vivo imaging agents in determining ?v?6 expressed in a subject.Type: ApplicationFiled: December 16, 2010Publication date: September 27, 2012Inventor: Magne Solbakken
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Publication number: 20120245357Abstract: A Michael adduct of piplartine, to provide inhibition of ALR2 in vitro (supported by molecular docking) and their potential to suppress the accumulation of sorbitol in erythrocytes when incubated under high glucose conditions; a treatment method using a Michael adduct; and a process for preparing a Michael adduct are provided.Type: ApplicationFiled: March 21, 2011Publication date: September 27, 2012Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Madhusudana Rao Janaswamy, Bhanuprakash Reddy Geereddy, Rama Subba Rao Vidadala, Muthenna Puppala
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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: 8232310Abstract: Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.Type: GrantFiled: June 29, 2009Date of Patent: July 31, 2012Assignee: Georgetown UniversityInventors: Jeffrey A. Toretsky, Aykut Üren, Milton Lang Brown, Yali Kong
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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: 8227489Abstract: The invention relates to compounds of general formula (I): Wherein n, X1, X2, X3, X4, Y, Z1, Z2, Z3, Z4, Ra and Rb are as defined herein. The invention also relates to process for the preparation of compounds of formula (I) and their therapeutic use.Type: GrantFiled: January 23, 2009Date of Patent: July 24, 2012Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
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Publication number: 20120184574Abstract: The present invention is directed to compounds and forms and pharmaceutical compositions thereof useful for treating a viral infection, or for affecting viral activity by modulating viral replication.Type: ApplicationFiled: April 5, 2010Publication date: July 19, 2012Applicant: PTC THERAPEUTICS, INC.Inventors: Malcolm Maccoss, F. George Njoroge, Amin Nomeir, Guangming Chen, Song Xiao Huang, Ramesh Kakarla, Gary Mitchell Karp, William Joseph Lennox, Chunshi Li, Ronggang Liu, Yalei Liu, Christie Morrill, Steven D. Paget, Sean W. Smith, James Takasugi, Anthony A. Turpoff, Hongyu Ren, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Publication number: 20120183496Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: ApplicationFiled: December 16, 2011Publication date: July 19, 2012Applicant: COCRYSTAL DISCOVERY, INC.Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Publication number: 20120184582Abstract: The present invention relates to novel compounds which are effective as an inhibitor for xanthine oxidase, a process for preparing the same, and a pharmaceutical composition comprising a therapeutically effective amount of the same.Type: ApplicationFiled: October 4, 2010Publication date: July 19, 2012Inventors: Jeong Uk Song, Geun Tae Kim, Sung Pil Choi, Cheol Kyu Jung, Deok Seong Park, Eun Sil Choi, Tae Hun Kim, Hyun Jung Park, Wan Su Park, Heui Sul Park, Ki Chul Koo, Vasily Artemov
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Patent number: 8222279Abstract: Compounds of Formula I are described along with pharmaceutical formulations thereof, and methods of treating disorders such as diabetes and neurodegenerative diseases with such compounds.Type: GrantFiled: October 11, 2010Date of Patent: July 17, 2012Assignee: Duke UniversityInventor: Michael C. Pirrung
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Publication number: 20120172346Abstract: The invention concerns the use of a nicotinic acetylcholine receptor alpha 7 activators for the treatment, prevention or delay of progression of dyskinesia associated with dopamine agonist therapy in Parkinson's Disease.Type: ApplicationFiled: September 22, 2010Publication date: July 5, 2012Inventors: Thérèse Di Paolo, Dominik Feuerbach, Baltazar Gomez-Mancilla, Donald Johns
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Patent number: 8211918Abstract: This invention provides compounds of formula I where the dashed line represents an optional double bond; where R1 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazyl, furyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, optionally substituted, and other substituents are defined herein. Such compounds are potassium channel modulators.Type: GrantFiled: August 13, 2010Date of Patent: July 3, 2012Assignee: Valeant Pharmaceuticals InternationalInventors: Jean-Michel Vernier, Huanming Chen, Jianlan Song
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Publication number: 20120145238Abstract: The present invention pertains to an electrode layer comprising a porous film made of oxide semiconductor fine particles sensitized with certain methin dyes. Moreover the present invention pertains to a photoelectric conversion device comprising said electrode layer, a dye sensitized solar cell comprising said photoelectric conversion device and to novel methin dyes.Type: ApplicationFiled: August 27, 2010Publication date: June 14, 2012Applicant: BASF SEInventors: Junichi Tanabe, Hiroshi Yamamoto, Shinji Nakamichi, Ryuichi Takahashi
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Publication number: 20120129890Abstract: A compound (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic ring which may have a substituent, a 6-membered aromatic heterocyclic ring which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. 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: July 26, 2010Publication date: May 24, 2012Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuya Tatani, Naohiro Kawamura, Tatsuhiro Kondo, Atsushi Kondo
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Publication number: 20120122839Abstract: The present invention provides compounds of formula (I) or (Ia) which are ligands binding to the HDM2 protein, inducing apoptosis and inhibiting proliferation, and having therapeutic utility in cancer therapy and prevention. Compounds of formula (I) or (Ia) can be used as therapeutics for treating stroke, myocardial infarction, ischemia, multi-organ failure, spinal cord injury, Alzheimer's Disease, injury from ischemic events and heart valvular degenerative disease. Moreover, compounds of formula (I) or (Ia) can be used to decrease the side effects from cytotoxic cancer agents, radiation and to treat viral infections.Type: ApplicationFiled: January 17, 2012Publication date: May 17, 2012Applicant: Priaxon AGInventors: Christoph BURDACK, Cedric Kalinski, Vladimir Khazak, Gunther Ross, Lutz Weber
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Publication number: 20120122931Abstract: A compound represented by the general formula (I) of the present invention, which has an EP1 receptor antagonism: [wherein A represents a benzene ring or the like; Y represents a C1-6 alkylene group or the like; RN represents a hydrogen atom or a C1-6 alkyl group; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents a phenyl group which may have a substituent, a 5-membered aromatic heterocyclic group which may have a substituent, a 6-membered aromatic heterocyclic group which may have a substituent or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like] or a pharmaceutically acceptable salt thereof is provided. 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: July 26, 2010Publication date: May 17, 2012Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Tatsuhiro Kondo, Atsushi Kondo, Kazuya Tatani, Naohiro Kawamura
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Publication number: 20120108611Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.Type: ApplicationFiled: December 29, 2011Publication date: May 3, 2012Inventors: Jean-Michel Altenburger, Valérie Fossey, Gilbert Lassalie, Frédéric Petit, Jean Claude Vernieres, Philip Janiak
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Publication number: 20120101105Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Nav1.3 and Nav1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.Type: ApplicationFiled: May 31, 2010Publication date: April 26, 2012Inventors: Tadashi Inoue, Shuzo Watanabe, Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Kaoru Shimada
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Patent number: 8163778Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof wherein the residues have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.Type: GrantFiled: November 24, 2008Date of Patent: April 24, 2012Assignee: Hoffmann-LA Roche Inc.Inventors: Wolfgang Haap, Paul Hebeisen, Eric Argirios Kitas, Bernd Kuhn, Peter Mohr, Hans Peter Wessel
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Patent number: 8143291Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as sphingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: GrantFiled: January 3, 2011Date of Patent: March 27, 2012Assignee: Allergan, Inc.Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
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Publication number: 20120071508Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, t, R1, R2, R3, R4, R5, R6, R7, Q, Y and Z have defined meanings.Type: ApplicationFiled: November 30, 2011Publication date: March 22, 2012Inventors: Jean Fernand Armand Lacrampe, Christophe Meyer, Bruno Schoentjes, Alain Philippe Poncelet, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert, Luc Van Hijfte
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Publication number: 20120058482Abstract: The invention provides a novel class of cyanine dyes that are functionalized with a linker moiety that facilitates their conjugation to other species and substituent groups which increase the water-solubility, and optimize the optical properties of the dyes. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.Type: ApplicationFiled: August 25, 2011Publication date: March 8, 2012Applicant: Pacific Biosciences of California, Inc.Inventors: Gene Shen, Stephen Yue
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Publication number: 20120058469Abstract: The invention provides a novel class of cyanine dyes that are functionalized with a linker moiety that facilitates their conjugation to other species and substituent groups which increase the water-solubility, and optimize the optical properties of the dyes. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.Type: ApplicationFiled: August 25, 2011Publication date: March 8, 2012Applicant: Pacific Biosciences of California, Inc.Inventor: Gene Shen