Single Bond Between 1,2-positions And Single Bond Between 3,4-positions Patents (Class 546/165)
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Publication number: 20130045480Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins and nucleic acids. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified by the addition of charged and polar groups to provide beneficial properties.Type: ApplicationFiled: June 17, 2009Publication date: February 21, 2013Applicant: ENZO LIFE SCIENCES, INC. C/O ENZO BIOCHEM, INC.Inventors: Yuejun Xiang, Praveen Pande, Rajesh Khazanchi, Elazar Rabbani, Dakai Liu, Wei Cheng
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Publication number: 20130045990Abstract: The present invention provides a compound of the formula below or a pharmaceutical salt thereof, methods of treating diabetes using the compound and a process for preparing the compound.Type: ApplicationFiled: August 9, 2012Publication date: February 21, 2013Applicant: ELI LILLY AND COMPANYInventor: Chafiq Hamdouchi
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Publication number: 20130040907Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: May 4, 2012Publication date: February 14, 2013Applicant: Ardea Biosciences Inc.Inventors: Esmir GUNIC, Jean-Luc GIRARDET, Jean-Michel VERNIER, Martina E. TEDDER, David A. PAISNER
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Patent number: 8362112Abstract: The present invention relates to cure accelerators useful for anaerobic curable compositions, such as adhesives and sealants. The cure accelerators are constructed as urethane/urea/thiourethane (meth)acrylate resins from diols and include a unit embraced within structure A where X is C1-20 alkyl, C2-20 alkenyl, or C7-20 alkaryl, any of which may be interrupted by one or more hereto atoms, and which are functionalized by at least one and preferably at least two groups selected from —OH, —NH2 or —SH and z is 1-3.Type: GrantFiled: October 28, 2011Date of Patent: January 29, 2013Assignees: Henkel Ireland Limited, Henkel CorporationInventors: David P. Birkett, Martin Wyer, Andrew Messana, David P. Dworak, Anthony F. Jacobine
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Publication number: 20130023528Abstract: Compounds for inhibiting hypoxia inducible factor (HIF) prolyl-4-hydroxylases (PHDs) having the general formula (1). Methods of using these and related compounds for treating a patient having a condition that would benefit from inhibiting HIF PHD are also described herein.Type: ApplicationFiled: February 17, 2011Publication date: January 24, 2013Applicant: CORNELL UNIVERSITYInventors: Rajiv R. Ratan, Irina Gazaryan, Natalya Smirnova
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Publication number: 20130023518Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R5 have the significance given in claim 1, can be used as a medicament.Type: ApplicationFiled: September 28, 2012Publication date: January 24, 2013Applicant: Hoffmann-La Roche IncInventor: Hoffmann-La Roche Inc.
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Patent number: 8349830Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: October 26, 2010Date of Patent: January 8, 2013Assignee: Merck Sharp & DohmeInventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem
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Publication number: 20130005759Abstract: MicroRNAs are a class of endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation has the potential to provide new therapeutic approaches to such diseases. microRNA miR-122 is the most abundant microRNA in the liver and is involved in hepatocellular carcinoma development and hepatitis C virus (HCV) infection. Small molecule inhibitors and activators of the microRNA miR-122 are described, and methods for their identification are reported. These small molecule inhibitors reduce viral replication in liver cells and thus represent a new approach to the treatment of HCV infections. Moreover, small molecule activation of miR-122 in liver cancer cells selectively induced apoptosis through caspase activation, and thus has implications in cancer chemotherapy.Type: ApplicationFiled: January 21, 2011Publication date: January 3, 2013Inventors: Alexander Deiters, Douglas D. Young
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Publication number: 20130005769Abstract: 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: wherein n, s, t, R1, R2, R3, R4, R5, X, Y, Q, Z, G, E and D have defined meanings.Type: ApplicationFiled: September 7, 2012Publication date: January 3, 2013Inventors: Pierre Henri Storck, Bruno Schoentjes, Arnaud Marcel Pierre Piettre, Philipp Ermert, Virginie Sophie Poncelet, Imre Christian Francis Csoka
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Publication number: 20130005963Abstract: An organic photoelectric conversion material for use in an organic thin-film photoelectric conversion device, containing a compound represented by formula 1; and an organic thin-film photoelectric conversion device having a photoelectric conversion layer which containing the organic photoelectric conversion material: wherein D represents an electron-donating aromatic substituent whose bonding site atom is a sp2 carbon atom; and a plurality of D may be the same or different from each other.Type: ApplicationFiled: September 7, 2012Publication date: January 3, 2013Applicant: FUJIFILM CORPORATIONInventor: Tetsu KITAMURA
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Patent number: 8344137Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R5 have the significance given in claim 1, can be used as a medicament.Type: GrantFiled: April 7, 2011Date of Patent: January 1, 2013Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Jim Zhen Wu, Mingwei Zhou
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Publication number: 20120316167Abstract: The present invention provides new secondary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. Many of these compounds are active against Candida species such as Candida Albicans and Candida Glabrata.Type: ApplicationFiled: December 28, 2010Publication date: December 13, 2012Applicant: Polichem SAInventors: Stefania Gagliardi, Simone Del Sordo, Federico Mailland, Michela Legora
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Publication number: 20120309751Abstract: New tertiary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. These compounds are also active against Candida species such as Candida Albicans and Candida Glabrata.Type: ApplicationFiled: December 28, 2010Publication date: December 6, 2012Applicant: POLICHEM SAInventors: Stefania Gagliardi, Simone Del Sordo, Federico Mailland, Michela Legora
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Patent number: 8324384Abstract: 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: GrantFiled: February 3, 2010Date of Patent: December 4, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
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Publication number: 20120288855Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.Type: ApplicationFiled: July 26, 2012Publication date: November 15, 2012Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Jolene A. Bradford, Ching-Ying Cheung, Shih-Jung Huang, Patrick R. Pinson, Stephen T. Yue
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Patent number: 8298766Abstract: The present invention provides a category of cyanine dyes having the following general structural Formula I, wherein X is defined as C(CH3)2, O, S or Se; m is an integer from 1 to 18, R1 and R2 are each independently chosen from H, C1-18alkyl, OR7, C1-6alkyl-OR7 or halogen; R3 is pyrrolyl, imidazolyl, piperidinyl, piperazinyl, morpholinyl, guanidino, NHR5 or N(R6)2; R4 is C1-18alkyl, benzyl or (CH2)mR3; R5 is saturated and/or unsaturated, straight-chained and/or branched-chained C1-18alkyl, hydroxy alkyl, mercapto-alkyl, amino alkyl, acyl, phenyl, naphthyl or benzyl; R6 is a C2-18alkyl; R7 is H or a C1-18alkyl; Y? is an anion. The mentioned compounds can be applied to staining biological samples, to the fields of nucleic acids labeling, blood cell analysis, clinical diagnosis, immunological assays and etc.Type: GrantFiled: April 30, 2010Date of Patent: October 30, 2012Inventors: Xiaojun Peng, Tong Wu, Jiangli Fan, Shiguo Sun
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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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Publication number: 20120245344Abstract: A compound represented by the formula (II) is a GPR119 agonist, and is used as an agent for treating diabetes: wherein each of R23, R24, and R25 is hydrogen, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylsulfonyl, or the like; each of Q0 and T0 is CH2 or the like, or Q0 and T0 are combined to form CH?CH or the like; A0 is (CH2)p, C(O), or a bond; B0 is a bond or the like; one of U0 and V0 is N, and the other is CR31 or the like; each of X0 and Y0 is CH2CH2 or the like; Z0 is C(O)OR32 or the like; and each of R21 and R22 is hydrogen, a halogen atom, hydroxyl, C1-8 alkyl, or the like.Type: ApplicationFiled: August 30, 2010Publication date: September 27, 2012Applicant: NIPPON CHEMIPHAR CO., LTD.Inventors: Tsuyoshi Endo, Hiroto Tanaka, Toshihiro Takahashi, Toshihiro Kunigami
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Patent number: 8273768Abstract: The invention relates to a compound of the formula (I) in which: R1, R2 and R3 are independently a methoxy group optionally substituted by one or more fluorine atoms; R4 is a hydrogen atom; R5 and R6 are identical and each represent a hydrogen or fluorine atom; A is a cycle selected from the group including aryl and heteroaryl groups, wherein said groups can be substituted.Type: GrantFiled: April 4, 2008Date of Patent: September 25, 2012Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Mouâd Alami, Jean-Daniel Brion, Olivier Provot, Jean-François Peyrat, Samir Messaoudi, Abdallah Hamze, Anne Giraud, Jérôme Bignon, Joanna Bakala, Jian-Miao Liu
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Patent number: 8263588Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: April 4, 2008Date of Patent: September 11, 2012Assignee: Neurocrine Biosciences, Inc.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
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Publication number: 20120225868Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: February 27, 2012Publication date: September 6, 2012Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20120214824Abstract: The present invention is directed to compounds of Formulae (I), (II), (III), (IV), (V), (VI), (VII), and (VIII), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.Type: ApplicationFiled: December 8, 2011Publication date: August 23, 2012Inventors: Bradley Tait, Christopher Borella, Robert Chambers, Matthew Cullen
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Publication number: 20120202996Abstract: The present invention relates to tetrahydroquinoline derivatives having general formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y—X is C(O)—O, S(O)2-O, NHC(O)—O, NHC(S)—O, OC(O)—O, bond-O, C(O)—NH, S(O)2-NH, NHC(O)—NH, NHC(S)—NH, OC(O)—NH, bond-NH, NH—C(O), O—C(O), NH—S(O)2, or O—S(O)2 or Y—X is a bond; R6 is H, trifluoromethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8,R9-aminocarbonyl(1-4C)alkyl, R8,R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro, hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4CType: ApplicationFiled: October 7, 2011Publication date: August 9, 2012Applicant: N.V. OrganonInventors: Nicole Corine Renée Van Straten, Rudolf Gijsbertus Van Someren, Jurgen Schulz
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Publication number: 20120190700Abstract: The present invention provides compounds of formula or pharmaceutically acceptable salts, esters or stereoisomers thereof, wherein R1 to R4, A and Y have the meanings given herein, as well as methods for making those compounds and their use as medicament, in particular as medicament for the treatment of cancer.Type: ApplicationFiled: January 17, 2012Publication date: July 26, 2012Inventors: Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Jason Christopher Wong, Zhenshan Zhang
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Publication number: 20120190677Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein R1 to R8, A1 to A3 have the are as described herein and compositions including the compounds.Type: ApplicationFiled: January 19, 2012Publication date: July 26, 2012Inventors: Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Shixiang Yan, Hongying Yun, Mingwei Zhou
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Publication number: 20120184533Abstract: Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.Type: ApplicationFiled: July 2, 2010Publication date: July 19, 2012Applicant: ANGION BIOMEDICA CORP.Inventors: Bijoy Panicker, Dong Sung Lim, David E. Smith
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Publication number: 20120165370Abstract: Quinoline derivatives showing anticancer activities against cancer cell lines of hepatocellular carcinoma (Hep3B), lung carcinoma (A549), esophageal squamous cell carcinoma (HKESC-1, HKESC-4 and KYSE150).Type: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Inventors: Johnny Cheuk-on TANG, Albert Sun Chi CHAN, Kim Hung LAM, Sau Hing CHAN
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Patent number: 8207345Abstract: Compounds of the formula (I), in which W, R, R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in Claim 1, can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: June 2, 2006Date of Patent: June 26, 2012Assignee: Merck Patent GmbHInventors: Kai Schiemann, David Bruge, Hans-Peter Buchstaller, Ulrich Emde, Dirk Finsinger, Christiane Amendt, Frank Zenke
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Publication number: 20120157641Abstract: The present invention relates to cure accelerators useful for anaerobic curable compositions, such as adhesives and sealants.Type: ApplicationFiled: October 7, 2011Publication date: June 21, 2012Applicants: Loctite (R&D) Limited, Henkel CorporationInventors: David Birkett, Martin Wyer, Andrew Messana, Philip Klemarczyk, Anthony F. Jacobine
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Patent number: 8178553Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: GrantFiled: January 20, 2010Date of Patent: May 15, 2012Assignee: Schering CorporationInventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta Maria Kosinski, Seong-Heon Kim, De-Yi Yang, Razia K. Rizvi
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Patent number: 8178558Abstract: This invention relates to novel substituted pyridylmethyl bicyclocarboxamide compounds and to their use in therapy. These compounds are particularly useful as modulators of the VR1 (Type I Vanilloid) receptor, and are thus useful for the treatment of pain, neuralgia, neuropathies, nerve injury, burns, migraine, carpal tunnel syndrome, fibromyalgia, neuritis, sciatica, pelvic hypersensitivity, bladder disease, inflammation, or the like in mammals, especially humans.Type: GrantFiled: September 10, 2007Date of Patent: May 15, 2012Assignee: Pfizer Inc.Inventors: Satoshi Nagayama, Yuji Shishido, Hirotaka Tanaka
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Patent number: 8173675Abstract: The invention relates to substituted amino-thiourea compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the substituted amino-thiourea compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such compounds. The substituted amino-thiourea compounds are defined by the following formula (I): wherein A, B, R1, R2, R3, R4, R5.1, R5.2 and R6 are defined as in the description.Type: GrantFiled: May 13, 2008Date of Patent: May 8, 2012Assignee: BASF SEInventors: Christopher Koradin, Markus Kordes, Ernst Baumann, Ronan Le Vezouet, Deborah L. Culbertson
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Publication number: 20120108630Abstract: The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: James K. Chen, Joel M. Hyman, Cory A. Ocasio
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Patent number: 8163729Abstract: The present invention provides compounds of formula (I) and compositions thereof, methods of making them, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.Type: GrantFiled: January 16, 2008Date of Patent: April 24, 2012Assignees: Wyeth, Siena Biotech S.p.A.Inventors: Chiara Ghiron, Arianna Nencini, Iolanda Micco, Riccardo Zanaletti, Laura Maccari, Hendrick Bothmann, Simon N. Haydar, Maurizio Varrone, Carmela Pratelli, Boyd L. Harrison
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Publication number: 20120071506Abstract: The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, 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 which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification, and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms.Type: ApplicationFiled: November 23, 2011Publication date: March 22, 2012Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 8114893Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: GrantFiled: December 17, 2009Date of Patent: February 14, 2012Assignees: Genentech, Inc., Abbott Laboratories, The Walter and Eliza Hall Medical Research InstituteInventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Carl Steven Rye, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Andrew M. Petros, Andrew J. Souers, Peter Czabotar
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Publication number: 20120035187Abstract: The present invention has an object to provide a novel agent for anti-neurodegenerative diseases and solves the object by providing an agent for anti-neurodegenerative diseases containing, as an effective ingredient, the compound(s) represented by the following General formula 1: wherein in General formula 1, R1 through R3 independently represent a hydrogen atom or an appropriate substituent; Z1 represents a heterocyclic ring and Z2 represents the same or different heterocyclic or aromatic ring as in Z1, wherein the heterocyclic and aromatic rings optionally have a substituent; represents an integer of 0, 1 or 2; p represents an integer of 0 or 1, with the proviso that p is 1 when o is 0 or 2, and p is 0 when o is 1; R1 and R2 do not exist when o is 0, while, when p is 0, R3 does not exist and the binding between the carbon atom to which R2 binds and Z2 is a single bond; X1? represents an appropriate counter anion and q represents an integer of 1 or 2.Type: ApplicationFiled: January 25, 2010Publication date: February 9, 2012Applicant: KABUSHIKI KAISHA HAYASHIBARA SEIBUTSU KAGAKU KENKYUJOInventors: Hitomi Ohta, Kenji Akita, Tsunetaka Ohta, Toshio Kawata, Shigeharu Fukuda
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Publication number: 20120035409Abstract: This invention relates to novel bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.Type: ApplicationFiled: February 5, 2010Publication date: February 9, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Mario Lobell, Nicole Teusch, Shendong Yuan
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Publication number: 20120034270Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.Type: ApplicationFiled: October 16, 2009Publication date: February 9, 2012Applicant: Akaal Pharma Pty LtdInventors: Damian W. Grobelny, Gurmit S. Gill
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Patent number: 8110562Abstract: This invention provides nuclear hormone receptor binding compounds, compositions comprising the same and methods of uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, prostate cancer and/or diseases or disorders of bone and muscle.Type: GrantFiled: July 19, 2007Date of Patent: February 7, 2012Assignees: University of Tennessee Research Foundation, The Ohio State University Research FoundationInventors: James T. Dalton, Duane D. Miller, Igor Rakov, Casey Bohl, Michael L. Mohler
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Publication number: 20120022057Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).Type: ApplicationFiled: March 16, 2010Publication date: January 26, 2012Applicant: Schering CorporationInventors: Gang Zhou, Grant Wishart, Pauline C. Ting, Robert G. Aslanian, Nicolas Zorn, Jianhua Cao
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Publication number: 20120004218Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein A1 to A3 and R1 to R10 have the significance given in claim 1, can be used as a medicament. These compounds are useful in the treatment or prophylaxis of diseases that are related to AMPK regulation, such as obesity, dyslipidemia, hyperglycemia, type 1 or type 2 diabetes and cancers.Type: ApplicationFiled: June 27, 2011Publication date: January 5, 2012Inventors: Li Chen, Lichun Feng, Yun He, Mengwei Huang, Yongfu Liu, Hongying Yun, Mingwei Zhou
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Publication number: 20120004197Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.Type: ApplicationFiled: March 31, 2010Publication date: January 5, 2012Applicant: KOWA COMPANY, LTD.Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
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Publication number: 20120004310Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.Type: ApplicationFiled: May 27, 2011Publication date: January 5, 2012Inventors: Frank M. LONGO, Stephen M. Massa, Sandeep Gupta
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Publication number: 20110306624Abstract: 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: February 3, 2010Publication date: December 15, 2011Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
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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
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Publication number: 20110281356Abstract: Methods and small molecule compounds for stem cell differentiation are provided. One example of a class of compounds that may be used is represented by the compound of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4, R5, R5?, R6, R6?, R7, R7? are as described herein.Type: ApplicationFiled: May 13, 2011Publication date: November 17, 2011Applicants: Human BioMolecular Research Institute, Sanford-Burnham Medical Research InstituteInventors: Mark Mercola, John Cashman, Marion Lanier, Erik Willems
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Publication number: 20110262904Abstract: The present invention provides a category of cyanine dyes having the following general structural Formula I, wherein X is defined as C(CH3)2, O, S or Se; m is an integer from 1 to 18, R1 and R2 are each independently chosen from H, C1-18alkyl, OR7, C1-6alkyl-OR7 or halogen; R3 is pyrrolyl, imidazolyl, piperidinyl, piperazinyl, morpholinyl, guanidino, NHR5 or N(R6)2; R4 is C1-18alkyl, benzyl or (CH2)mR3; R5 is saturated and/or unsaturated, straight-chained and/or branched-chained C1-18alkyl, hydroxy alkyl, mercapto-alkyl, amino alkyl, acyl, phenyl, naphthyl or benzyl; R6 is a C2-18alkyl; R7 is H or a C1-18alkyl; Y? is an anion. The mentioned compounds can be applied to staining biological samples, to the fields of nucleic acids labeling, blood cell analysis, clinical diagnosis, immunological assays and etc.Type: ApplicationFiled: April 30, 2010Publication date: October 27, 2011Inventors: Xiaojun Peng, Tong Wu, Jiangli Fan, Shiguo Sun
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Publication number: 20110257151Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R5 have the significance given in claim 1, can be used as a medicament.Type: ApplicationFiled: April 7, 2011Publication date: October 20, 2011Inventors: Li Chen, Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Jim Zhen Wu, Mingwei Zhou
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Publication number: 20110251236Abstract: Therapeutic agents for treatment of Galactosemia and disorders thereof, and other enzyme related disorders thereof are identified. The compounds inhibit galactokinase (GALK) and other kinase activity and are identified by a high throughput screening assay.Type: ApplicationFiled: August 14, 2008Publication date: October 13, 2011Applicant: University of MiamiInventors: Kent Lai, Klass Jan Wierenga, Manshu Tang