Nitrogen Attached Indirectly To The Six-membered Hetero Ring Through The Directly Attached Nitrogen By Nonionic Bonding Patents (Class 546/162)
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Patent number: 8058442Abstract: Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, eg. a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, a inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding ageing, and prevention and/or treatment of skin ageing and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety, the neuroprotective function is imparted to the compound e.g. by a neuroprotective peptide, and a combined antiapoptotic and neuroprotective function by a propargyl group.Type: GrantFiled: November 7, 2003Date of Patent: November 15, 2011Assignees: Technion Research and Development Foundation Ltd., Yeda Research and Development Co., Ltd.Inventors: Moussa Youdim, Matitiyahu Fridkin, Hailin Zheng, Abraham Warshawsky, Rivka Warshawsky, legal representative
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Patent number: 8053446Abstract: Novel pyridyl cyanoguanidine compounds of general formula I (I) wherein R1, X, R2 and R3 are as defined herein, exhibit a high antiproliferative activity and may be used in the treatment of hyperproliferative and neo-plastic diseases.Type: GrantFiled: December 20, 2005Date of Patent: November 8, 2011Assignee: Leo Pharma A/SInventors: Fredrik Bjorkling, Heinz Wilhelm Dannacher
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Publication number: 20110237579Abstract: The invention relates to non-macrocyclic, non-peptidic, substituted heterocyclic compounds useful for inhibiting hepatitis C virus (“HCV”) replication, particularly functions of the non-structural 5A (“NS5A”) protein of HCVType: ApplicationFiled: December 2, 2009Publication date: September 29, 2011Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20110230445Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: ApplicationFiled: May 26, 2011Publication date: September 22, 2011Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Publication number: 20110217699Abstract: 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: May 10, 2011Publication date: September 8, 2011Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Jolene A. Bradford, Ching-Ying Cheung, Shih Jung Huang, Patrick R. Pinson, Stephen T. Yue
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Patent number: 8008324Abstract: The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: March 6, 2008Date of Patent: August 30, 2011Assignee: AEterna Zentaris GmbHInventors: Peter Emig, Gerald Bacher, Dietmar Reichert, Silke Basner, Beate Aue, Bernd Nickel, Eckhard Gunther
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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: 20110201592Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: ApplicationFiled: October 23, 2008Publication date: August 18, 2011Applicant: CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Ian Collins, John Jamieson Caldwell, Antony William Oliver, Tony Michael Raynham, Emma Jane Welsh, Cornelius Albertus Johannes Matijssen
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Publication number: 20110190342Abstract: The invention relates to quinoline derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.Type: ApplicationFiled: September 30, 2009Publication date: August 4, 2011Inventors: Markus Henrich, Angela Bauer, Jens Nagel, Meik Sladek, Christopher Graham Raphael Parsons, Wojciech Danysz, Valerjans Kauss, Jevgenijs Rozhkovs, Igos Starchenkovs, Dina Trifanova
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Patent number: 7989453Abstract: The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: December 20, 2007Date of Patent: August 2, 2011Assignee: AEterna Zentaris GmbHInventors: Peter Emig, Gerald Bacher, Dietmar Reichert, Silke Basner, Beate Aue, Bernd Nickel, Eckhard Gunther
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Publication number: 20110172230Abstract: [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.Type: ApplicationFiled: August 22, 2007Publication date: July 14, 2011Inventors: Takahiro Ishii, Takashi Sugane, Akio Kakefuda, Tatsuhisa Takahashi, Tokatoshi Kanayama, Kentaro Sato, Ikumi Kuriwaki, Chika Kitada, Jotaro Suzuki
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Patent number: 7973027Abstract: Compounds with high antimalarial activity; and antimalarial drugs containing the same as an active ingredient. There are provided compounds with antimalarial activity represented by the chemical formula: (wherein R1 is H, Cl or OCH3; R2 is H or CH3; R3 is CH, CH2, C(CH3), CH(CH3) or C(CH3)2; Ar is imidazole, triazole, pyridine, benzene, pyrrole, furan, thiophene or derivatives thereof; n is 1 to 5; and m is 1 to 5). Further, there are provided antimalarial drugs containing these compounds with antimalarial activity or pharmacologically acceptable salts thereof as active ingredients.Type: GrantFiled: February 26, 2007Date of Patent: July 5, 2011Assignee: Nagoya City UniversityInventors: Tsunehiko Higuchi, Hirohisa Omiya, Naoki Umezawa, Hye-Sook Kim, Yusuke Wataya
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Patent number: 7964731Abstract: The invention relates to adenozin A3 receptor ligands labeled with iodine isotops of mass number 125, within those favorably to antagonists and their isomers, to the experimental materials containing them, to a process for the preparation of the compounds of the general formula (I) and their isomers, to the new intermediates of the general formula (II) and to the preparation thereof.Type: GrantFiled: May 14, 2007Date of Patent: June 21, 2011Assignee: Sanofi-AventisInventors: Geza Timari, Kinga Boer, Geza Toth, Csaba Tomboly
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Publication number: 20110142856Abstract: The present invention relates to a compound represented by formula (I-0): wherein symbols in formula have the same meanings as described in the present specification, a salt thereof, an N-oxide thereof or a solvate thereof or a prodrug thereof, and medical use thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoidarthritis, arthritis, retinopathy, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.Type: ApplicationFiled: February 15, 2011Publication date: June 16, 2011Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masaya KOKUBO, Yoshikazu Takaoka, Shiro Shibayama
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Patent number: 7947711Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: GrantFiled: August 21, 2008Date of Patent: May 24, 2011Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Yu-ming Pu, Yi-Yin Ku
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Patent number: 7939661Abstract: This invention is concerned with compounds of the formula wherein A, R1 to R5 are as defined in the specification and G is a pyridine, quinoline or pyrimidine group as defined in the specification, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: GrantFiled: August 30, 2007Date of Patent: May 10, 2011Assignee: Hoffman-La Roche Inc.Inventors: Andreas D. Christ, Rainer E. Martin, Peter Mohr
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Publication number: 20110104315Abstract: The invention provides for compounds of formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of eating disorders, metabolic disorders, obesity, cognitive disorders, neurological disorders, pain disorders, inflammation disorders, in the promotion of smoking cessation and for the treatment of other psychiatric disorders Also provided are pharmaceutical compositions containing such compounds and pharmaceutical combinations of the compounds of the invention with other therapeutic agents.Type: ApplicationFiled: January 5, 2011Publication date: May 5, 2011Inventors: Chongqing Sun, Doree Sitkoff, William R. Ewing, Yanting Huang, Bruce A. Ellsworth, Richard B. Sulsky, Annapurna Pendri, Samuel Gerritz, Natesan Murugesan, Zhengxiang Gu
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Publication number: 20110086877Abstract: Disclosed herein are methods of inhibiting the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing intoxication caused by bacteria of at least one bacterial strain in a subject, and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.Type: ApplicationFiled: October 1, 2010Publication date: April 14, 2011Inventors: SINA BAVARI, RICK GUSSIO, JAMES C. BURNETT
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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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Patent number: 7897774Abstract: The present invention relates to a synthesis study of novel cyclic compounds having a quinolylalkylthio group represented by the formula (1), and pharmacological actions of the compounds. In the formula, the ring X represents: which may have halogen and/or alkyl; R1 and R2 independently represent hydrogen, alkyl, cycloalkyl, aryl or a (non) aromatic heterocycle; R3 represents qinolyl; A represents sulfur, sulfinyl or sulfonyl; and B represents alkylene.Type: GrantFiled: August 30, 2007Date of Patent: March 1, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kenji Kawashima, Takahiro Honda, Hisashi Tajima, Kazuyoshi Okamoto, Minoru Yamamoto
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Publication number: 20110045100Abstract: One aspect of the invention relates to substitute quinolines with antimalarial activity, and compositions and kits comprising at least one of them. Another aspect of the invention relates to methods for the treatment or prevention or both of malaria comprising administering to a subject a therapeutically effective amount of such a compound. Importantly, a number of the compounds show excellent potency against both chloroquine-sensitive and chloroquine-resistant strains.Type: ApplicationFiled: March 5, 2009Publication date: February 24, 2011Applicant: GEORGETOWN UNIVERSITYInventors: Christian Wolf, Paul D. Roepe, Angel C. De Dios
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Publication number: 20110039828Abstract: A novel compound of the formula (I): wherein R1 is alkoxycarbonyl or the like, R2 is alkyl or the like; R3 is hydrogen or the like; R4 is alkylene or the like; R5 is optionally substituted heterocyclic group; R6, R7, R8 and R9 are independently hydrogen; alkyl, alkoxy, or the like; R10 is optionally substituted aromatic ring, or the like; or a pharmaceutically acceptable salt thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP).Type: ApplicationFiled: October 25, 2010Publication date: February 17, 2011Inventors: Hitoshi KUBOTA, Masakatsu Sugahara, Mariko Furukawa, Mayumi Takano, Daisuke Motomura
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Publication number: 20110027178Abstract: The present invention provides novel compounds which may be used as in vivo imaging agents. The compounds of the invention are useful in a method to image the expression of P2X7 receptors in a subject, as a means to facilitate the diagnosis of a range of disease states.Type: ApplicationFiled: February 26, 2009Publication date: February 3, 2011Inventors: Paul Alexander Jones, Ian Wilson, Veronique Morrison-Iveson, Clare Jones, John Woodcraft, Alex Jackson, Duncan Wynn
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Patent number: 7880006Abstract: Disclosed are compounds that have excellent insecticidal activity and are usable as agricultural and horticultural insecticides. Compounds represented by formula (I) or agriculturally and horticulturally acceptable acid addition salts thereof have excellent insecticidal activity and are usable as agricultural and horticultural insecticides.Type: GrantFiled: August 3, 2005Date of Patent: February 1, 2011Assignees: Meiji Seika Kaisha, Ltd., Nippon Kayaku Co., Ltd.Inventors: Kazumi Yamamoto, Ryo Horikoshi, Kazuhiko Oyama, Hiroshi Kurihara, Shizuo Shimano, Takaaki Miyake, Hiroki Hotta, Jun Iwabuchi
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Publication number: 20110021562Abstract: The invention provides methods of treating Friedreich's ataxia using histone deacetylase inhibitors.Type: ApplicationFiled: May 4, 2010Publication date: January 27, 2011Applicant: THE SCRIPPS RESEARCH INSTUTEInventors: KAI JENSSEN, DAVID M. HERMAN, JOEL M. GOTTESFELD, RYAN BURNETT, C. JAMES CHOU
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Publication number: 20110009447Abstract: Substituted benzoic acid amides of formula (I) and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of benzoic acid amides are described.Type: ApplicationFiled: April 24, 2001Publication date: January 13, 2011Inventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch
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Patent number: 7868174Abstract: The present disclosure relates to an improved process for the preparation of enantiomerically enriched alcohols of Formula (I), from the corresponding ketone of Formula (II), by asymmetric transfer hydrogenation, using a hydrogen donor, catalyzed by a ruthenium or rhodium complex of an optically active N-sulfamoyl-1,2-diamine. R is as defined herein.Type: GrantFiled: July 21, 2005Date of Patent: January 11, 2011Assignee: Pliva-Istrazivanje I Razvoj d.o.o.Inventors: Amir Avdagic, Barbara Mohar, Damjan Sterk, Michel Stephan
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Publication number: 20110003851Abstract: The present embodiments relate to compounds with physiological effects, such as the activation of hematopoietic growth factor receptors. The present embodiments also relate to use of the compounds to treat a variety of conditions, diseases and ailments such as hematopoietic conditions and disorders.Type: ApplicationFiled: May 6, 2010Publication date: January 6, 2011Applicant: Ligand Pharmaceuticals, Inc.Inventors: Lin Zhi, Andrew R. Hudson, Cornelis A. Van Oeveren, Steven L. Roach, Jason C. Pickens, Yixing Shen, Catalina Cuervo, Lino J. Valdez, Jillian Basinger, Virgina H. Grant
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Publication number: 20100331315Abstract: The invention provides compounds that inhibit PIM kinases and/or CK2, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.Type: ApplicationFiled: June 18, 2010Publication date: December 30, 2010Inventors: Mustapha HADDACH, David M. RYCKMAN
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Publication number: 20100331293Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: ApplicationFiled: June 25, 2010Publication date: December 30, 2010Applicant: AMGEN INC.Inventors: Timothy D. Cushing, Paul John Dransfield, Felix Gonzalez Lopez De Turiso, Michael G. Johnson, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
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Publication number: 20100324042Abstract: The present invention relates to a heterocyclic compound of the general formula (I) and their use and preparation, methods of making the compounds, compositions containing at least one of said compounds, and methods of treatment using at least one compound.Type: ApplicationFiled: October 19, 2007Publication date: December 23, 2010Applicant: Abbott GmbH & Co. KG.Inventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Kent D. Stewart
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Publication number: 20100324086Abstract: A compound of formula (1) as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder from pain, fever, inflammation and cancer.Type: ApplicationFiled: February 19, 2009Publication date: December 23, 2010Applicant: Novasaid ABInventors: Johan Wannberg, Mathias Alterman, Patric Stenberg, Jacob Westman
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Publication number: 20100317842Abstract: The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.Type: ApplicationFiled: August 25, 2010Publication date: December 16, 2010Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Dhanalakshmi Kasi, Vani P. Mocharla, Bing Wang, Umesh B. Gangadharmath, Brian A. Duclos, Kai Chen, Wei Zhang, Gang Chen, Henry Clifton Padgett, Farhad Karimi, Peter J.H. Scott, Zhiyong Gao, Qianwa Liang, Thomas Lee Collier, Tieming Zhao, Chunfang Xia
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Publication number: 20100280240Abstract: Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.Type: ApplicationFiled: July 9, 2010Publication date: November 4, 2010Inventors: Brett D. Allison, Laurent Gomez, Cheryl A. Grice, Michael D. Hack, Brain J. Morrow, S. Timothy Motley, Alejandro Santillan, JR., Karen J. Shaw, Kimberly L. Schwarz, Liu Y. Tang, Hariharan Venkatesan, John J.M. Wiener
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Publication number: 20100280070Abstract: The invention relates to synthesis and biological screening of novel tetrahydroquinolines of formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them for aromatase inhibition: (I). The present invention also relates to a process for the preparation of the novel tetrahydroquinolines, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. These compounds are useful in for aromatase inhibition, particularly in the treatment and/or prevention of cancer, particularly breast cancer, more particularly hormone dependent breast cancer.Type: ApplicationFiled: January 2, 2009Publication date: November 4, 2010Inventor: Raghuram Rao AKKINEPALLY
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Publication number: 20100274004Abstract: Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.Type: ApplicationFiled: July 9, 2010Publication date: October 28, 2010Inventors: Brett D. Allison, Laurent Gomez, Cheryl A. Grice, Michael D. Hack, Brian J. Morrow, S. Timothy Motley, Alejandro Santillan, JR., Karen J. Shaw, Kimberly L. Schwarz, Liu Y. Tang, Hariharan Venkatesan, John J.M. Wiener
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Publication number: 20100274005Abstract: Antibacterial compounds, compositions containing them, and methods of use for the inhibition of bacterial activity and the treatment, prevention or inhibition of bacterial infection.Type: ApplicationFiled: July 9, 2010Publication date: October 28, 2010Inventors: Brett D. Allison, Laurent Gomez, Cheryl A. Grice, Michael D. Hack, Brian J. Morrow, S. Timothy Motley, Alejandro Santillan, JR., Karen J. Shaw, Kimberly L. Schwarz, Liu Y. Tang, Hariharan Venkatesan, John J. M. Wiener
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Publication number: 20100261679Abstract: Disclosed herein are compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof, compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.Type: ApplicationFiled: October 16, 2008Publication date: October 14, 2010Inventors: James Sutton, Martin Sendzik, Weibo Wang
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Patent number: 7812170Abstract: Compounds of the formula (I) in which Z, is an oxygen atom; or a sulfur atom; Z2 is an oxygen atom; or a sulfur atom; R, is an aryl or heteroaryl group, which is unsubstituted or substituted; R2 is hydrogen; or an organic substituent; R3 is hydrogen; or an organic substituent; R4 is hydrogen; or an organic substituent; or R3 and R4, taken together, form, together with the nitrogen atom, to which they are attached, a ring, which is unsubstituted or substituted; R5 is hydrogen; or an unsubstituted or substituted alkyl group; or forms, taken together with R8 or with a monovalent substituent attached to that atom of R6, via which atom R6 is directly connected with the carbon atom, shown in the formula I, which carries R5, one additional bond; R6 and R7, taken together, form, together with the two carbon atoms, shown in the formula I, to which atoms they are attached, a bicyclic ring system, which ring system is carbocyclic or heterocyclic, which ring system is substituted, in the manner shown in the formula I, byType: GrantFiled: March 2, 2005Date of Patent: October 12, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: David John Hughes, James Edward Peace, Suzanna Riley, Sally Russell, Joseph John Swanborough, Roger Graham Hall, André Jeanguenat, Olivier Loiseleur, Peter Renold, Stephan Trah, Jean Wenger
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Patent number: 7807693Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, L, E, G, J, M, R3, R4, R5 and R13 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures, and the salts thereof.Type: GrantFiled: May 16, 2007Date of Patent: October 5, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Kai Gerlach, Georg Dahmann, Herbert Nar, Roland Pfau, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
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Publication number: 20100234417Abstract: A hetero-dimeric or hetero-oligomeric receptor, comprising at least one thyrotropin releasing hormone receptor subunit associated with at least one orexin receptor subunit.Type: ApplicationFiled: November 9, 2007Publication date: September 16, 2010Applicant: DIMERIX BIOSCIENCE PTY LTD.Inventors: Kevin Donald George Pfleger, Ruth Marie Seeber, Heng See Boon, Karin Ann Eidne
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Publication number: 20100234373Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including autoimmune disease and inflammation. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, L, R1, R2 and R3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of the present invention, methods of use such as treatment of Lck and/or c-Kit kinase mediated diseases by administering the compounds of the invention, or compositions including one or more compounds of the invention, and intermediates and processes useful for the preparation of compounds of the present invention.Type: ApplicationFiled: May 26, 2010Publication date: September 16, 2010Applicant: Amgen Inc.Inventors: Erin F. Dimauro, Jean E. Bemis, Stuart C. Chaffee, Ning Chen, Essa Hu, Roxanne Kunz, Matthew W. Martin, David C. McGowan, Shannon Rumfelt
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Patent number: 7795249Abstract: The present invention provides certain pyrazoline compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions and methods of using the compositions in the treatment of various diseases.Type: GrantFiled: December 19, 2007Date of Patent: September 14, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Ruth S. Adams, Matthew Duffey, Alexandra E. Gould, Paul D. Greenspan, Bheemashankar A. Kulkarni, Tricia J. Vos
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Patent number: 7790756Abstract: The present invention is concerned with novel compounds useful in the treatment of hyperproliferative diseases and mammalian cancers, especially human cancers. The invention also pertains to methods of modulating kinase activities, pharmaceutical compositions, and methods of treating individuals, incorporating or using the compounds. The preferred compounds are active small molecules set forth in formulae Ia-Iww.Type: GrantFiled: October 10, 2007Date of Patent: September 7, 2010Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A Petillo, Michael D Kaufman
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Patent number: 7790746Abstract: Quinoline derivatives, particularly 4-anilinoquinoline derivatives of formula (I), are provided: Such quinoline derivatives can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position, for example via selective inhibition of DNA methyltransferase DNMT 1. Methods for synthesizing numerous 4-anilinoquinoline derivatives and for modulating DNA methylation are provided. Also provided are methods for formulating and administering these compounds or compositions to treat conditions such as cancer and hematological disorders.Type: GrantFiled: December 18, 2007Date of Patent: September 7, 2010Assignee: SuperGen, Inc.Inventors: Pasit Phiasivongsa, Sanjeev G. Redkar, Swarna Gamage, Darby Brooke, William Denny, David J. Bearss, Hariprasad Vankayalapati
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Publication number: 20100222350Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: ApplicationFiled: May 10, 2010Publication date: September 2, 2010Inventors: Alfred Binggeli, Andreas D. Christ, Hans P. Maerki, Rainer E. Martin
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Publication number: 20100190777Abstract: Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.Type: ApplicationFiled: July 16, 2008Publication date: July 29, 2010Applicant: PLEXXIKON INC.Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
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Patent number: 7745462Abstract: Compounds of formula I in free or salt form, wherein —C—Y—, R1 and R2 are G have the meanings as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: April 2, 2004Date of Patent: June 29, 2010Assignee: Novartis AGInventors: Robin Alec Fairhurst, David Andrew Sandham, David Beattie, Ian Bruce, Bernard Cuenoud, Reamonn Madden, Neil John Press, Roger John Taylor, Katharine Louise Turner, Simon James Watson
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Publication number: 20100145056Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.Type: ApplicationFiled: November 23, 2009Publication date: June 10, 2010Inventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth T. TenBrink
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Publication number: 20100130505Abstract: Disclosed are compositions and methods for treating diseases associated with G protein ?? subunit activity.Type: ApplicationFiled: April 28, 2008Publication date: May 27, 2010Applicant: University of RochesterInventors: Alan V. Smrcka, Burns C. Blaxall, Jean M. Bidlack