Polycyclo Ring System Having The 1,3-thiazole Ring As One Of The Cyclos Patents (Class 546/270.1)
-
Publication number: 20120053187Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: August 24, 2011Publication date: March 1, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Alex Aronov, Jon H. Come, Kevin Michael Cottrell, Arnaud Le Tiran, Valerie Marone, Gabriel Martinez Botella, David Messersmith, Emilie Porter Huck, Ronald Lee Grey, JR.
-
Publication number: 20120022255Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
-
Publication number: 20110319425Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, Y, Z1, Z2, Z3, M and (A)m are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 12, 2010Publication date: December 29, 2011Inventors: Christelle Boléa, Sylvain Celanire
-
Publication number: 20110306591Abstract: Heteroaryloxycarbocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 11, 2011Publication date: December 15, 2011Inventors: Jennifer R. Allen, Michael J. Frohn, Paul E. Harrington, Essa Hu, Alexander J. Pickrell, Robert M. Rzasa, Kelvin K. C. Sham
-
Patent number: 8076488Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.Type: GrantFiled: March 1, 2004Date of Patent: December 13, 2011Assignee: Bayer Healthcare LLCInventors: Jacques Dumas, Stephen Boyer, Sharad Verma, Lila Adnane, Yuanwei Chen, Wendy Lee, Barton Phillips, Roger A. Smith, William J. Scott, Jennifer Burke, Jianqing Chen, Zhi Chen, Jianmei Fan, Karl Miranda, Brian Raudenbush, Aniko Redman, Jianxing Shao, Ning Su, Gan Wang, Lin Yi, Qingming Zhu
-
Patent number: 8071595Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described 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. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.Type: GrantFiled: June 24, 2009Date of Patent: December 6, 2011Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
-
Publication number: 20110294780Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
-
Patent number: 8067602Abstract: Asymmetric cyanine fluorescent dyes are represented by general formula I. These kinds of dyes may be used as a staining agent for nucleic acids, with the spectra at 600-900 nm in the near-infrared region and without interference from background fluorescence. These kinds of dyes may be useful with small-type red semiconductor lasers as the light source (such as 633 nm). Compositions comprising these dyes and methods for staining biological samples using these dyes or compositions are also provided.Type: GrantFiled: December 12, 2008Date of Patent: November 29, 2011Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.Inventor: Jianhui Shao
-
Patent number: 8053450Abstract: The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.Type: GrantFiled: April 17, 2008Date of Patent: November 8, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Timothy F. Herpin, George C. Morton, Robert P. Rehfuss, R. Michael Lawrence, Michael A. Poss, Jacques Y. Roberge, Timur Gungor
-
Publication number: 20110263612Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: April 12, 2011Publication date: October 27, 2011Applicant: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
-
Publication number: 20110257165Abstract: 3,4-diaryl-bicyclicpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: December 17, 2009Publication date: October 20, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Chiara Marchionni, Claudia Piutti, Fabio Gasparri
-
Patent number: 8039532Abstract: A compound represented by formula (I-1): wherein R21, R22, R23 and R24 each independently represent a hydrogen atom or a monovalent substituent, with the proviso that compounds, in which R21, R22, R23 and R24 each are an alkylthio group, are excluded; R21 and R22 and/or R23 and R24 each may bond to each other to form a ring, with the proviso that compounds, in which the formed ring is a dithiol ring or a dithiolane ring, are excluded; R25 and R26 each independently represent a hydrogen atom or a monovalent substituent; X21, X22, X23 and X24 each independently represent a hetero atom; compounds, wherein R21, R22, R23 and R24 each represent a cyan group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group or a hydrogen atom, are excluded; and compounds, wherein R21 and R23 each represent a hydrogen atom; R22 and R24 each represent an arylcarbonyl group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group, are eType: GrantFiled: August 15, 2008Date of Patent: October 18, 2011Assignee: Fujifilm CorporationInventors: Naoyuki Hanaki, Masuji Motoki, Toshihiko Yawata
-
Publication number: 20110251386Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.Type: ApplicationFiled: October 15, 2009Publication date: October 13, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Koji Masuda, Shiro Kida, Kyohei Hayashi, Manabu Katou, Naoki Yoshikawa, Akira Kugimiya, Mado Nakajima, Nobuyuki Tanaka
-
Publication number: 20110243846Abstract: This invention relates to compounds (benzothiazoles) suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging.Type: ApplicationFiled: November 28, 2009Publication date: October 6, 2011Inventors: Jorma Hassfeld, Ulrike Roehn, Matthias Friebe, Lutz Lehmann, Tobias Heinrich, Sabine Krause, Damian Brockschnieder, Thomas Dyrks, Andrea Thiele, Ulf Boemer, Ursula Moenning, Markus Berger, Stephan Siegel
-
Publication number: 20110237573Abstract: The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.Type: ApplicationFiled: March 1, 2010Publication date: September 29, 2011Applicant: IRM LLCInventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
-
Publication number: 20110224204Abstract: Di-substituted phenyl 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. The disclosure also relates to methods for treating neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 25, 2009Publication date: September 15, 2011Inventors: Richard Chesworth, Gideon Shapiro, Amy Ripka
-
Publication number: 20110207751Abstract: Novel compounds having a fused bicyclic heteroaromatic ring system substituted with a thiazole ring are disclosed. The compounds inhibit growth of a variety of types of cancer cells, and are thus useful for treating cancer. Efficacy of these compounds is demonstrated with a system for monitoring cell growth/migration, which shows they are potent inhibitors of growth and/or migration of cancer cells. In addition, compounds of the invention were shown to stop growth of tumors in vivo, and to reduce the size of tumors in vivo. Compositions comprising these compounds, and methods to use these compounds and compositions for treatment of cancers, are disclosed.Type: ApplicationFiled: February 18, 2011Publication date: August 25, 2011Inventors: Long Mao, Xiaobo Wang, Xiao Xu, Li Zhao, Jia Liu
-
Publication number: 20110178126Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention have use as therapeutic agents, e.g., they demonstrate anti-proliferative, anti-inflammatory, anti-angiogenic, anti-migration activities. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of, e.g., anti-inflammatory, renal, and hyperproliferative disorders. The compounds of the invention are pyrazolylbenzothiazole derivatives of the following formula (1) wherein X, R1, R2, R3 and R4 are described herein.Type: ApplicationFiled: October 22, 2010Publication date: July 21, 2011Applicant: Valocor Therapeutics, Inc.Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov
-
Publication number: 20110178070Abstract: The invention relates to PI3K/mTOR inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: June 23, 2009Publication date: July 21, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Xianchang Gong, Bohan Jin, Massaki Hirose, Feng Zhou, Qing Dong
-
Publication number: 20110171739Abstract: Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.Type: ApplicationFiled: September 23, 2009Publication date: July 14, 2011Inventors: Steven John Kemp, Lynda Jane Storey, John Mervyn David, Janet Richard, Charles Robert Harrington, Claude Michael Wischik, Scott Clunas, Tobias Kerst Heinrich
-
Patent number: 7977340Abstract: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, —S(O)NR6—, —C(?O)O— or —S(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.Type: GrantFiled: June 21, 2007Date of Patent: July 12, 2011Assignee: Prolysis Ltd.Inventors: David John Haydon, Lloyd George Czaplewski, Nicholas John Palmer, Dale Robert Mitchell, John Frederick Atherall, Christopher Richard Steele, Tamara Ladduwahetty
-
Publication number: 20110166088Abstract: The present invention provides Gyrase B and/or Topoisomerase IV par E inhibitors, which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonas spp., Acenetobacter spp., Moraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Ktycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Corynebacterium, Bacillus spp., Enterobactericeae,’ (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.Type: ApplicationFiled: June 25, 2009Publication date: July 7, 2011Applicant: RANBAXY LABORATORIES LIMITEDInventors: Jitendra A. Sattigeri, Naresh Kumar, Ajay Yadav, Lalima Sharma, Ian A. Cliffe, Shibu B. Varughese, Shaikh Rizwan Shabbir, V. Samuel Raj, Dilip J. Upadhyay, Pradip K. Bhatnager
-
Publication number: 20110144068Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: July 23, 2009Publication date: June 16, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Fabio Zuccotto, Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro', Chiara Marchionni, Michele Modugno
-
Publication number: 20110135603Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: October 15, 2010Publication date: June 9, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Tiansheng Wang, Alexander Aronov, Mark Cornebise, Francois Maltais, Mark Ledeboer, Arnaud Le Tiran, Valerie Marone, David Messesrsmith, Kevin Cottrell, Jon H. Come, Gabriel Martinez Botella
-
Publication number: 20110130397Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.Type: ApplicationFiled: September 21, 2007Publication date: June 2, 2011Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
-
Patent number: 7951954Abstract: The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta adrenoreceptor agonists.Type: GrantFiled: March 12, 2007Date of Patent: May 31, 2011Assignee: AstraZeneca ABInventors: Lilian Alcaraz, Andrew Lister, Garry Pairaudeau
-
Publication number: 20110124005Abstract: Disclosed is a reagent for detecting an abnormal cell in the cervix of uterus, which can detect an abnormal cell contained in a biological sample that contains cells collected from the cervix of uterus. The reagent comprises a dye represented by general formula (I).Type: ApplicationFiled: July 27, 2009Publication date: May 26, 2011Applicant: SYSMEX CorporationInventors: Masakatsu Morita, Akinori Kawai, Yukio Tsujino
-
Publication number: 20110118208Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: March 13, 2009Publication date: May 19, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Darryl Mcconnell, Maria Impagnatiello, Dirk Kessler, Oliver Kraemer, Siegfried Schneider, Lars Van Der Veen, Ulrike Weyer-Czernilofsky, Tobias Wunberg
-
Publication number: 20110118282Abstract: A compound having the structure useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, angina pectoris, thromboses, restenoses, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver in a human or animal patient.Type: ApplicationFiled: September 2, 2008Publication date: May 19, 2011Inventors: Amy R. Bittner, Christopher Joseph Sinz, Jiang Chang, Ronald M. Kim, J.W. Mirc, Emma R. Parmee, Qiang Tan
-
Publication number: 20110112067Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
-
Publication number: 20110112087Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: April 20, 2010Publication date: May 12, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Lars VAN DER VEEN, Maria Impagnatiello, Darryl McConnell, Siegfried Schneider, Tobias Wunberg
-
Publication number: 20110098292Abstract: The present invention provides new compounds of formula (I) as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.Type: ApplicationFiled: June 29, 2005Publication date: April 28, 2011Applicant: AstraZeneca ABInventors: Jonas Malmstrom, Jenny Viklund
-
Publication number: 20110086882Abstract: A compound represented by the formula (I) or pharmacologically acceptable salt thereof exhibits an excellent CRF receptor antagonism wherein X is a nitrogen atom or CH; R1 is -A11-A12; A11 is a single bond or a C1-6 alkylene group; A12 is a hydrogen atom, a C1-6 alkyl group or a C3-6 cycloalkyl group, etc.; R2 is -A21-A22; A21 is a single bond or a C1-6 alkylene group; A22 is a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a non-aromatic heterocyclic group, or a heteroaryl group, etc.; R3 is a C1-6 alkyl group, a C3-6 cycloalkyl group, a C1-6 alkoxy group, a C3-6 cycloalkoxy C1-6 alkyl group, di-C1-6 alkyl amino group, a halogen atom, a cyano group, a formyl group, or a carboxyl group, etc; R4 is a hydrogen atom or a C1-6 alkoxy group; R5 is a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; R6 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group, a C1-6 alkylthio group, or a C1-6 alkyl sulfinyl group etc.Type: ApplicationFiled: October 7, 2010Publication date: April 14, 2011Applicant: Eisai R&D Management Co., Ltd.Inventors: Kogyoku SHIN, Taro TERAUCHI, Yoshinori TAKAHASHI, Minako HASHIZUME, Kunitoshi TAKEDA, Kodo SHIKATA, Akira INOMATA
-
Publication number: 20110076291Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: September 27, 2010Publication date: March 31, 2011Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
-
Publication number: 20110061723Abstract: 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: February 26, 2009Publication date: March 17, 2011Applicant: BASF SEInventors: Kazuhiko Kunimoto, Hiroshi Yamamoto, Shinji Nakamichi, Ryuichi Takahashi, Junichi Tanabe
-
Publication number: 20110059992Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: November 11, 2010Publication date: March 10, 2011Applicants: ASTRAZENECA AB, ASTEX THERAPEUTICS LTD.Inventors: James Arnold, Phil Edwards, Mark Sylvester, Stefan Berg, Jörg Holenz, Annika Kers, Karin Kolmodin, Laszlo Rakos, Liselotte Öhberg, Rotticci Didier, Gianni Chessari, Miles Congreve, Christopher Murray, Sahil Patel
-
Patent number: 7902183Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R5 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: April 5, 2007Date of Patent: March 8, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Bodo Betzemeier, Darryl McConnell, Thomas Gerstberger, Matthias Grauert, Matthias Hoffmann, Maria Impagnatiello, Lars van der Veen, Ulrike Weyer-Czernilofsky
-
Patent number: 7893086Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: June 20, 2008Date of Patent: February 22, 2011Assignee: Sirtris Pharmaceuticals, Inc.Inventors: Jean Bemis, Jeremy S. Disch, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Chi B. Vu
-
Patent number: 7893069Abstract: Substituted imidazo[2,1-b]thiazole compounds corresponding to formula I, a method for producing them, pharmaceutical compositions containing them, and the use thereof for regularing mGluR5 receptors, or for treating or inhibiting disorders or disease states at least partially mediated by mGluR5 receptor such as pain, anxiety attacks, drug or alcohol dependency, and others.Type: GrantFiled: September 9, 2008Date of Patent: February 22, 2011Assignee: Gruenenthal GmbHInventors: Sven Kuehnert, Saskia Zemolka, Michael Haurand, Klaus Schiene
-
Publication number: 20110033417Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: February 10, 2011Inventors: Gopinadhan N. Anilkumar, 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, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
-
Publication number: 20110015175Abstract: The present disclosure provides a series of compounds of the formula (I) which reduce ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: ApplicationFiled: January 7, 2010Publication date: January 20, 2011Inventors: Lawrence R. Marcin, Lorin A. Thompson, III, Kenneth M. Boy, Jason M. Guernon, Mendi A. Higgins, Jianliang Shi, Yong-Jin Wu, Yunhui Zhang, John E. Macor
-
Publication number: 20110015192Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benfit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: September 27, 2010Publication date: January 20, 2011Applicant: Sirtris Pharmaceuticals, Inc.Inventors: Jean Bemis, Jeremy S. Disch, Michael Jirousek, Walter Joseph Lunsmann, Pui Yee Ng, Chi B. Vu
-
Patent number: 7871773Abstract: Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. The subject dyes are virtually non-fluorescent when diluted in aqueous solution, but exhibit bright fluorescence when associated with nucleic acid polymers such as DNA or RNA, or when associated with detergent-complexed proteins. A variety of applications are described for detection and quantitation of nucleic acids and detergent-complexed proteins in a variety of samples, including solutions, electrophoretic gels, cells, and microorganisms.Type: GrantFiled: June 1, 2007Date of Patent: January 18, 2011Assignee: Life Technologies CorporationInventors: Richard Haugland, Stephen Yue
-
Publication number: 20110009418Abstract: The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions comprising an effective amount of a Phenylene Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Phenylene Compound.Type: ApplicationFiled: July 29, 2010Publication date: January 13, 2011Applicant: Purdue Pharma L.P.Inventor: Qun Sun
-
Publication number: 20110003828Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.Type: ApplicationFiled: June 24, 2010Publication date: January 6, 2011Inventors: Laura Cook Blumberg, Julius F. Remenar, Örn Almarsson, Tarek A. Zeidan
-
Publication number: 20100331323Abstract: The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Inventors: Daniel L. Comins, Florence F. Wagner, Pauline Ondachi
-
Publication number: 20100331371Abstract: The invention is concerned with novel substituted benzimidazole derivatives of formula (I) wherein R1 to R10 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.Type: ApplicationFiled: August 25, 2010Publication date: December 30, 2010Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Sven Taylor, Minmin Yang
-
Publication number: 20100331326Abstract: The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.Type: ApplicationFiled: June 28, 2010Publication date: December 30, 2010Inventors: Mark G. BOCK, Christoph GAUL, Venkateshwar Rao GUMMADI, Saumitra SENGUPTA
-
Publication number: 20100311748Abstract: The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R2 or R3 is (Z).Type: ApplicationFiled: August 29, 2008Publication date: December 9, 2010Applicant: ASTRAZENECA ABInventors: Leslie Dakin, Benjamin Fauber, Alexander Hird, James Janetka, Daniel John Russell, Qibin Su, Bin Yang, Xiaolan Zheng
-
Patent number: 7847101Abstract: Pharmaceutical pyrazolybenzothiazole compositions of formula (1) are provided. The compositions may be pharmaceutically acceptable salts. R1, R2 and R3 at each occurrence are independently selected from amino, aminosulfinyl, aminosulfonyl, aryl, azido, halogen, heteroalkyl, heteroaryl, hydrazinyl, hydrocarbyl, hydrogen, hydroxyl, nitro, nitroso, phosphate, phosphinate, phosphonate, phosphonium, phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfinic acid, sulfonamido, sulfonate, sulfonic acid, sulfonyl, sulfoxido, thiol, thioureido, and ureido, and R4 is selected from hydrogen, heteroalkyl, heteroaryl, and hydrocarbyl.Type: GrantFiled: July 23, 2003Date of Patent: December 7, 2010Assignee: Valocor Therapeutics, Inc.Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov