The Other Cyclo In The Bicyclo Ring System Is Also Six-membered (e.g., Naphthyridines, Etc.) Patents (Class 546/122)
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Publication number: 20110201501Abstract: Substituted pyridines of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the pyridines of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one pyridine compound of the formula I to act on plants, their seed and/or their habitat.Type: ApplicationFiled: October 14, 2009Publication date: August 18, 2011Applicant: BASF SEInventors: Dschun Song, Eike Hupe, Christian Pilger, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andrea Vescovi, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Robert Reinhard, Anja Simon, Ricarda Niggeweg, Bernd Sievernich
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Publication number: 20110201632Abstract: The present invention is directed to 2,5-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: October 15, 2009Publication date: August 18, 2011Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, Anthony J. Roecker, John D. Schreier
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Publication number: 20110195999Abstract: The present invention provides an antifungal agent represented by the formula: wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula —NH—C(?O)—, a group represented by the formula —C(?O)—NH—, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents.Type: ApplicationFiled: March 14, 2011Publication date: August 11, 2011Inventors: Kazutaka NAKAMOTO, Itaru Tsukada, Keigo Tanaka, Masayuki Matsukura, Toru Haneda, Satoshi Inoue, Norihiro Ueda, Shinya Abe, Katsura Hata, Naoaki Watanabe
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Publication number: 20110196150Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: February 10, 2011Publication date: August 11, 2011Inventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
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Publication number: 20110195980Abstract: New compounds, compositions and methods of inhibition of Provirus Integration of Maloney Kinase (PIM kinase) activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one PIM kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: August 31, 2009Publication date: August 11, 2011Inventors: Matthew Burger, Mika Lindvall
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Publication number: 20110183976Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 25, 2009Publication date: July 28, 2011Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20110183997Abstract: The invention provides a novel class of compounds of Formula I: (I) pharmaceutical compositions comprising such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR? and PDGFR? kinases.Type: ApplicationFiled: February 20, 2009Publication date: July 28, 2011Applicant: IRM LLCInventors: Donatella Chianelli, Xiaolin LI, Xiaodong Liu, Jon Loren, Valentina Molteni, Juliet Nabakka, Vince Yeh
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Publication number: 20110178096Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts thereof, pro-drugs thereof, biologically active metabolites thereof, isomers thereof or stereoisomers thereof wherein the variables are as defined herein. The compounds of Formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, rheumatoid arthritis, osteoarthritis, multiple sclerosis and asthma.Type: ApplicationFiled: March 29, 2011Publication date: July 21, 2011Applicant: ABBOTT LABORATORIESInventors: Dawn M. George, Lu X. Wang, Biqin Li, Anna M. Ericsson, Graham K. Ansell
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Publication number: 20110178083Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: July 9, 2009Publication date: July 21, 2011Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20110172256Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: September 10, 2009Publication date: July 14, 2011Inventors: Songnian Lin, Christian P. Stevenson, Emma R. Parmee, Libo Xu, Xibin Liao, Edward metzger, Rui Liang, Fengqi Zhang, John E. Stelmach
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Patent number: 7977351Abstract: The present invention provides a compound represented by the formula: wherein the variables R1, b, R6, Y, Z, X, R and a are defined in the specification. Said compound may be used in a method for treating diseases related to unregulated tyrosine kinase signal transduction, wherein said disease is selected from the group consisting of cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, and metabolic diseases.Type: GrantFiled: March 16, 2007Date of Patent: July 12, 2011Assignee: Allergan, Inc.Inventors: Sougato Boral, Xialing Guo, Shimiao Wang, Julie A. Wurster, Thomas C. Malone
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Publication number: 20110165075Abstract: The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.Type: ApplicationFiled: March 13, 2009Publication date: July 7, 2011Inventors: Milind Rajopadhye, Guojie Ho, Bohumil Bednar, Le T. Duong, Paul J. Coleman
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Publication number: 20110160210Abstract: An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.Type: ApplicationFiled: March 8, 2011Publication date: June 30, 2011Applicant: ALCON, INC.Inventors: Debra L. Fleenor, Iok-Hou Pang, Allan R. Shapard, Mark R. Hellberg, Abbot F. Clark, Peter G. Klimko
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Publication number: 20110160208Abstract: The present invention provides the compounds represented by formula (I): or pharmaceutical salts thereof, wherein: X1 represents oxygen atoms and the like, X2 represents nitrogen atoms and the like, X3 represents nitrogen atoms and the like, X4 represents nitrogen atoms and the like, R1 represents formula (II-1): wherein X5 represents sulfur atoms and the like, A1 represents carbon atoms and the like, A2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being useful for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.Type: ApplicationFiled: March 7, 2011Publication date: June 30, 2011Applicant: Banyu Pharmaceutical Co., Ltd.Inventors: Yukari Hirata, Satoru Ito, Hiroshi Kawamoto, Toshifumi Kimura, Yasushi Nagatomi, Hisashi Ohta, Akio Sato, Atsushi Satoh, Gentaroh Suzuki
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Patent number: 7968664Abstract: The invention described herein provides for novel nitric oxide-releasing polymers that comprise at least two adjacent units derived from acrylonitrile monomer units and containing at least one carbon-bound diazeniumdiolate. The diazeniumdiolated acrylonitrile-derived polymers can be used in medical devices therapeutically. Accordingly, the invention also provides a method of treating a biological disorder and a method of promoting angiogenesis that includes administering a medical device comprising a nitric oxide-releasing polymer comprising at least two adjacent units of acrylonitrile before exposure to nitric oxide and at least one nitric oxide releasing N2O2— group, wherein the N2O2— group is attached directly to the polyacrylonitrile backbone, to a specific location on or within the mammal in an amount effective to treat the biological disorder or promote angiogenesis.Type: GrantFiled: September 27, 2005Date of Patent: June 28, 2011Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Joseph A. Hrabie, Michael L. Citro, Frank DeRosa, Larry K. Keefer
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Patent number: 7968720Abstract: The invention relates to novel secondary amine derivatives of formula (I) and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.Type: GrantFiled: January 31, 2007Date of Patent: June 28, 2011Assignee: Actelion Pharmaceuticals Ltd.Inventors: Olivier Bezencon, Daniel Bur, Olivier Corminboeuf, Daniel Dube, Corinna Grisostomi, Dwight MacDonald, Dan McKay, David Powell, Lubos Remen, Sylvia Richard-Bildstein, John Scheigetz, Michel Therien, Thomas Weller
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Publication number: 20110150831Abstract: The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine and serine/threonine kinases and for the treatment of malignant or benign tumours and other disorders based on pathological cell proliferation, such as, for example, restenosis, psoriasis, arteriosclerosis and cirrhosis of the liver.Type: ApplicationFiled: November 24, 2010Publication date: June 23, 2011Applicant: AETERNA ZENTARIS GmbHInventors: Tilmann SCHUSTER, Matthias GERLACH, Irene SEIPELT, Emmanuel POLYMEROPOULOS, Gilbert MUELLER, Eckhard GUENTHER, Pascal MARCHAND, Julien DEFAUX
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Publication number: 20110150833Abstract: Compounds useful as Rho kinase inhibitors of formula (1) wherein the variables are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.Type: ApplicationFiled: December 18, 2008Publication date: June 23, 2011Applicant: The Scripps Research InstituteInventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Yen Ting Chen, Yan Yin, Hampton Sessions, Michael P. Smolinski, Lei Yao, Bo Wang, Bozena Frackowiak-Wojtasek
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Publication number: 20110152282Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: ApplicationFiled: August 24, 2009Publication date: June 23, 2011Applicant: IRM LLCInventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
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Publication number: 20110124633Abstract: In part, the present invention is directed to antibacterial compounds.Type: ApplicationFiled: July 27, 2010Publication date: May 26, 2011Inventors: Judd Berman, Peter Sampson, Heinz W. Pauls, Jailall Ramnauth, David Douglas Manning, Matthew David Surman, Dejian Xie, Helene Yvonne Decornez
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Patent number: 7947679Abstract: The naphthyridine derivatives of formula (I) a and method of combating or controlling phytopathogenic fungi which comprises applying the compounds of formula (I) to a plant, to a seed of a plant and to the locus of the plant.Type: GrantFiled: December 3, 2003Date of Patent: May 24, 2011Assignee: Syngenta Crop Protection, Inc.Inventors: Patrick Jelf Crowley, Markus Dobler, Urs Mueller, John Williams
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Publication number: 20110118248Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: January 13, 2009Publication date: May 19, 2011Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang
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Publication number: 20110112080Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Inventors: Guido Galley, Roger Norcross, Alessandra Polara
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Publication number: 20110112127Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, or forms thereof are active on Fms protein kinase, or on Fms and Kit protein kinase, or on Fms and Flt-3 protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinase, Kit protein kinase, or Flt-3 protein kinase including rheumatoid arthritis, osteoarthritis, multiple sclerosis, Alzheimer's disease, Parkinson's disease, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, acute myeloid leukemia, melanoma, multiple myeloma, metastatic breast cancer, prostate cancer, pancreatic cancer, neurofibromatosis, brain metastases, and gastrointestinal stromal tumors.Type: ApplicationFiled: November 4, 2010Publication date: May 12, 2011Inventors: Jiazhong Zhang, Prabha N. Ibrahim, Ryan Bremer, Wayne Spevak, Hanna Cho
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Patent number: 7939527Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: GrantFiled: April 9, 2009Date of Patent: May 10, 2011Assignee: Janssen Pharmaceutica NVInventors: Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
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Publication number: 20110104110Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Patent number: 7935725Abstract: Aryl-substituted bridged or fused diamine compounds, pharmaceutical compositions containing them, and methods of using the compounds and the pharmaceutical compositions for leukotriene A4 hydrolase (LTA4H or LTA4H) modulation and for the treatment of disease states, disorders, and conditions mediated by LTA4H activity, such as allergy, asthma, autoimmune diseases, pruritis, inflammatory bowel disease, ulcerative colitis, and cardiovascular disease, including atherosclerosis and prevention of myocardial infarction.Type: GrantFiled: October 30, 2008Date of Patent: May 3, 2011Assignee: Janssen Pharmaceutica NVInventors: Scott D. Bembenek, Wendy Eccles, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Taraneh Mirzadegan, Alejandro Santillán, Jr.
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Publication number: 20110098277Abstract: Compounds are disclosed which are Fab I inhibitors and are useful in the treatment bacterial infections.Type: ApplicationFiled: April 12, 2010Publication date: April 28, 2011Inventors: Walter J. Burgess, Dalia Jakas, William F. Huffman, William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas
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Publication number: 20110092537Abstract: The present invention relates to 2,6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.Type: ApplicationFiled: October 15, 2010Publication date: April 21, 2011Applicant: AC Immune S.A.Inventors: Heiko Kroth, Wolfgang Froestl, Andrea Pfeifer, Andreas Muhs
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Publication number: 20110092495Abstract: The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.Type: ApplicationFiled: December 9, 2010Publication date: April 21, 2011Applicant: ASTRAZENECA ABInventors: Gloria Breault, Charles Joseph Eyermann, Bolin Geng, Marshall Morningstar, Folkert Reck
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Publication number: 20110092480Abstract: Compounds of the general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5, R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their preparation and their use as antimicrobial agents.Type: ApplicationFiled: December 20, 2010Publication date: April 21, 2011Inventors: Steven Joseph Brickner, Jinshan Michael Chen, Zhengong Bryan Li, Anthony Marfat, Mark Joseph Mitton-Fry, Michael A. Plotkin, Usa Datta Reilly, Chakrapani Subramanyam, Zhijun Zhang, Shaughnessy Robinson
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Publication number: 20110092528Abstract: The invention is directed to piperidinyl compounds that selectively bind integrin receptors and methods for treating an integrin mediated disorder.Type: ApplicationFiled: December 22, 2010Publication date: April 21, 2011Inventors: Bart De Corte, Willam A. Kinney, Bruce E. Maryanolf, Shyamali Ghosh, Li Liu
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Publication number: 20110082136Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.Type: ApplicationFiled: June 8, 2009Publication date: April 7, 2011Inventors: Michelle Machacek, Gabriela de Almeida, Jonathan B. Grimm, Rachel N. MacCoss, Eric Romeo, Tony Siu, Catherine White, Kevin Wilson
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Patent number: 7919502Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt form thereof, wherein A, L1, R1, R2, R3, R4, R5, R6, and X are as defined herein. The compounds of Formula I have ALK and/or c-Met inhibitory activity, and may be used to treat ALK- or c-Met-mediated disorders or conditions.Type: GrantFiled: September 24, 2009Date of Patent: April 5, 2011Assignee: Cephalon, Inc.Inventors: Bruce D. Dorsey, Douglas A. Pippin, Jay P. Theroff, Craig A. Zificsak
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Patent number: 7915416Abstract: Disclosed are compounds of formula (I), wherein W, R, R1, R2, R3, R4, R5, R6, and R7 have the meanings indicated in claim 1. Said compounds can be used for the treatment of tumors, among other things.Type: GrantFiled: June 3, 2005Date of Patent: March 29, 2011Assignee: Merck Patent GmbHInventors: Kai Schiemann, David Bruge, Hans-Peter Buchstaller, Dirk Finsinger, Wolfgang Staehle, Christiane Amendt, Ulrich Emde, Frank Zenke
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Publication number: 20110071180Abstract: The present invention relates to compounds of the following formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).Type: ApplicationFiled: March 4, 2009Publication date: March 24, 2011Applicant: Targacept, Inc.Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Scott R. Breining, Philip S. Hammond, Ronald Joseph Heemstra, Anatoly A. Mazurov, Matt S. Melvin, Lan Miao, V. Srinivasa Murthy, Jon-Paul Strachan, Yunde Xiao
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Publication number: 20110062429Abstract: Disclosed is an organic electroluminescent device (organic EL device) that is improved in the luminous efficiency, fully secured of the driving stability, and of a simple structure and also disclosed is a compound for organic EL device useful for the said device. The compound for organic EL device is, for example, an indolocarbazole derivative represented by the following general formula (3). The organic EL device comprises a light-emitting layer disposed between an anode and a cathode piled one upon another on a substrate and the said light-emitting layer comprises a phosphorescent dopant and the aforementioned indolocarbazole derivative as a host material. In general formula (3), L is an aromatic heterocyclic group of a fused-ring structure with a valence of (n+1), Ar1 to Ar3 each is an alkyl group, an aralkyl group, or a substituted or unsubstituted aromatic hydrocarbon or aromatic heterocyclic group, and n is an integer of 0-5.Type: ApplicationFiled: April 30, 2009Publication date: March 17, 2011Inventors: Takahiro Kai, Masaki Komori, Toshihiro Yamamoto
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Publication number: 20110065713Abstract: The present invention is directed to benzazole compounds that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment or prevention of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which BACE is involved.Type: ApplicationFiled: November 19, 2010Publication date: March 17, 2011Applicant: High Point Pharmaceuticals, LLCInventors: Adnan M.M. Mjalli, David Jones, Devi Reddy Gohimmukkula, Guoxiang Huang, Jeff Zhu, Mohan Rao, Robert C. Andrews, Tan Ren
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Patent number: 7906530Abstract: New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy.Type: GrantFiled: August 7, 2007Date of Patent: March 15, 2011Assignee: Laboratorios Almirall, S.A.Inventors: Juan Francisco Caturla Javaloyes, Laura Vidal Gispert, Wenceslao Lumeras Amador
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Publication number: 20110059964Abstract: The present invention relates to the orexin receptor antagonists compounds of the general formula (I) as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic application thereof.Type: ApplicationFiled: February 3, 2010Publication date: March 10, 2011Applicant: sanofi-aventisInventors: Michel Aletru, Peter Aranyi, Maria Balogh, Sandor Batori, Judit Bence, Philippe Bovy, Zoltan Kapui, Endre Mikus, Claudie Namane, Christophe Philippo, Tibor Szabo, Zsuzsanna Tomoskozi, Katalin Urban-Szabo
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Publication number: 20110053897Abstract: Provided herein area novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity.Type: ApplicationFiled: July 26, 2010Publication date: March 3, 2011Applicant: IRM LLCInventors: Jianwei CHE, Bei Chen, Qiang Ding, Xueshi Hao, Xiaohui He, Songchun Jiang, Qihui Jin, Yunho Jin, Hong Liu, Yahua Liu, Barun Okram, Tetsuo Uno, Xu Wu, Kunyong Yang, Xuefeng Zhu
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Publication number: 20110052562Abstract: Compounds useful as Rho kinase inhibitors according to formula IA or IB: wherein A, B, D, E, R1, R2 and Ar1 are as defined herein, and any tautomer, salt, stereoisomer, hydrate, solvent, or prodrug thereof, pharmaceutical compositions, methods of treatment, and synthetic methods are provided.Type: ApplicationFiled: December 18, 2008Publication date: March 3, 2011Applicant: The Scripps Research InstituteInventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Hampton Sessions, Lei Yao, Bo Wang, Michael P. Smolinski, Yen Ting Chen, Yan Yin, Bozena Frackowiak-Wojtasek, Sarwat Chowdhury
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Patent number: 7897772Abstract: The present invention is directed to an irinotecan acid addition salt which is formed through addition of an acid selected from the group consisting of sulfuric acid, nitric acid, phosphoric acid, methanesulfonic acid, citric acid, maleic acid, and succinic acid to irinotecan, to a method for producing the salt, and to a pharmaceutical composition containing the salt. The addition salt requires no heating process during drug preparation and provides an aqueous drug product in which the salt is stably dissolved.Type: GrantFiled: September 29, 2005Date of Patent: March 1, 2011Assignee: Kabushiki Kaisha Yakult HonshaInventors: Hideaki Shimizu, Miyuki Uchida, Seigo Sawada, Norimasa Kaneda, Tsuneo Matsumoto
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Publication number: 20110046162Abstract: The present application relates to novel substituted fused cyanopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: December 9, 2008Publication date: February 24, 2011Applicant: BAYER SCHERING PHARMAInventors: Peter Nell, Alexandros Vakalopoulos, Frank Süssmeier, Barbara Albrecht-Küpper, Katja Zimmermann, Jörg Keldenich, Daniel Meibom
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Publication number: 20110046130Abstract: The invention relates to compounds of formula (I), wherein X1a, X1 to X5, Ra, Rb, n and R have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.Type: ApplicationFiled: March 27, 2009Publication date: February 24, 2011Applicant: Evotec AGInventors: Adam James Davenport, David James Hallett, Frédéric Marlin, Mark Gemkow
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Publication number: 20110044899Abstract: A compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1-C4)alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1-C4) alkyl group or forms together with the group R1—Ar a ring fused with the Ar group, A represents a group of formula (?) or (?): R3 and R4 independently represent a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6) alkenyl group or a group of formula (y): wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a —NO2 group, a —NR5R6 group, a N+R5R6R7X? group, or a —OSO2R12 group, and their addition salts with pharmaceutically acceptable acids.Type: ApplicationFiled: January 28, 2009Publication date: February 24, 2011Applicants: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, UNIVERSITE D'AUVERGNE CLERMONT 1, LABORATOIRES CYCLOPHARMAInventors: Jean-Michel Chezal, Frederic Dolle, Jean-Claude Madelmont, Aurelie Maisonial, Elisabeth Miot-Noirault, Nicole Moins, Janine Papon, Bertrand Kuhnast, Bertrand Tavitian, Raphael Boisgard
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Publication number: 20110039823Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.Type: ApplicationFiled: April 11, 2008Publication date: February 17, 2011Applicant: Actelion Pharmaceuticals LtdInventors: Daniel Bur, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20110038835Abstract: Compounds useful as Rho kinase inhibitors of formula (I): wherein variable are as defined herein are provided. Methods of treatment of malconditions mediated by Rho kinase, and methods of preparation of the compounds, are also provided.Type: ApplicationFiled: December 18, 2008Publication date: February 17, 2011Applicant: The Scripps Research InstituteInventors: Yangbo Feng, Philip LoGrasso, Thomas Bannister, Thomas Schroeter, Xingang Fang, Yen ting Chen, Yan Yin, Michael P. Smolinski, Lei Yao, Bo Wang, Hampton Sessions
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Publication number: 20110034334Abstract: The present invention relates to a method of controlling plants or inhibiting plant growth which comprises applying to the plants or to the locus thereof a herbicidally effective amount of a compound of formula (I): wherein A1, A2, A3, A4, R3, R4 and R5 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to intermediates used in the preparation of compounds of formula (I), to herbicidal compositions comprising compounds of formula (I) and to certain novel pyridopyridines, pyridodiazines and pyridotriazines.Type: ApplicationFiled: January 16, 2009Publication date: February 10, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Matthew Robert Cordingley, Michael Drysdale Turnbull, Nigel James Willetts, Patrick Jelf Crowley
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Publication number: 20110028509Abstract: The invention relates to compounds of formula I wherein R1, R2, R4, Ra, Rb, Rc, Re, A*, W1, W2 and W3 are as defined in claim 16, for the treatment of CXCR3 related diseases.Type: ApplicationFiled: April 8, 2009Publication date: February 3, 2011Applicant: MERCK SERONO SAInventors: Stefano Crosignani, Christophe Cleva, Christos Tsaklakidis, Lars Burgdorf