At Least Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/236)
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Patent number: 8293948Abstract: A reagent for organic synthesis with which a chemical reaction can be conducted in a liquid phase and unnecessary compound(s) can be easily separated at low cost from the liquid phase after completion of the reaction. The reagent for organic synthesis reversibly changes from a liquid-phase state to a solid-phase state with changes in solution composition and/or solution temperature, and is for use in organic synthesis reactions. This reagent for organic syntheses facilitates process development. With the reagent, research on and development of, e.g., medicines through, e.g., compound library synthesis, etc. can be accelerated. It can hence contribute to technical innovations in the biochemical industry and chemical industry.Type: GrantFiled: January 9, 2012Date of Patent: October 23, 2012Assignee: Jitsubo Co., Ltd.Inventors: Kazuhiro Chiba, Shokaku Kim, Yusuke Kono
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Publication number: 20120264739Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.Type: ApplicationFiled: December 30, 2010Publication date: October 18, 2012Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
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Publication number: 20120258927Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.Type: ApplicationFiled: June 19, 2012Publication date: October 11, 2012Applicant: Millenium Pharmaceuticals, Inc.Inventors: Steven P. Langston, Edward J. Olhava, Stepan Vyskocil
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Publication number: 20120258951Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: December 17, 2010Publication date: October 11, 2012Applicant: Mitsubishi Tanage Pharma CorporationInventors: Hiroshi Sato, Kazutoshi Yokoyama, Kazushi Sato
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Publication number: 20120258950Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.Type: ApplicationFiled: April 4, 2012Publication date: October 11, 2012Applicant: PFIZER LIMITEDInventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
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Publication number: 20120245125Abstract: The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for, research, drug screening, and therapeutic applications.Type: ApplicationFiled: June 8, 2012Publication date: September 27, 2012Applicants: Northwestern UniversityInventors: D. Martin Watterson, Linda Van Eldik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Velentza, Wenhui Hu, Magdalena Zasadzki
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Patent number: 8273741Abstract: The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof. A compound represented by the formula (I): wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.Type: GrantFiled: November 3, 2008Date of Patent: September 25, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Nozomu Sakai, Shinichi Imamura, Naoki Miyamoto, Takaharu Hirayama
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Publication number: 20120220581Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.Type: ApplicationFiled: October 27, 2010Publication date: August 30, 2012Applicant: Janssen-Cilag, S.A.Inventors: Joaquin Pastor-Fernández, José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Susana Conde-Ceide, Óscar Delgado-González, Greta Constantia Peter Vanhoof, Michiel Luc Maria Van Gool, María Luz Martín-Martín, Sergio-Alvar Alonso-De Diego
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Patent number: 8252795Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.Type: GrantFiled: October 8, 2009Date of Patent: August 28, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Brian E. Fink, Libing Chen, Ashvinikumar V. Gavai, Liqi He, Soong-Hoon Kim, Andrew James Nation, Yufen Zhao, Litai H. Zhang
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Publication number: 20120214815Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 6, 2012Publication date: August 23, 2012Applicant: UCB Pharma, S.A.Inventors: Benoît KENDA, Yannick QUESNEL, Ali ATES, Philippe MICHEL, Laurent TURET, Joël MERCIER
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Publication number: 20120208805Abstract: The invention relates to novel compounds of formula I where X, A?, Q1, Q2, Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.Type: ApplicationFiled: April 20, 2012Publication date: August 16, 2012Applicant: SANOFIInventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN
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Publication number: 20120196866Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 6, 2012Publication date: August 2, 2012Applicant: UCB PHARMA, S.A.Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
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Patent number: 8231888Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: GrantFiled: June 9, 2011Date of Patent: July 31, 2012Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
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Patent number: 8232278Abstract: Specifically substituted pyrido(3,2-d)pyrimidine derivatives having the structural formula (I) are useful for the treatment of hepatitis C.Type: GrantFiled: June 26, 2006Date of Patent: July 31, 2012Assignee: Gilead Sciences, Inc.Inventors: Steven Cesar Alfons De Jonghe, Piet André Maurits Maria Herdewijn, William A. Lee, William John Watkins
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Publication number: 20120190639Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.Type: ApplicationFiled: April 30, 2010Publication date: July 26, 2012Applicant: UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEEInventors: Steven Albert Everett, Saraj Ulhaq
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Publication number: 20120190666Abstract: The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3K? kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3K?, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: May 12, 2010Publication date: July 26, 2012Applicant: Amgen Inc.Inventors: Christiane Bode, Alessandro Boezio, Alan C. Cheng, Deborah Choquette, James Robert Coats, Katrina Woodin Copeland, Hongbing Huang, Daniel La, Richard Thomas Lewis, Hongyu Liao, Michele Potashman, John Stellwagen, Shuyan Yi, Mark H. Norman, Markian M. Stec, Emily Anne Peterson, Russell Graceffa
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Patent number: 8222251Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer.Type: GrantFiled: September 5, 2008Date of Patent: July 17, 2012Assignee: Amgen Inc.Inventors: Jacob Kaizerman, Brian Lucas, Dustin McMinn, Robert Zamboni
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Publication number: 20120178751Abstract: Disclosed are compounds of formula (I): where X, Y, X, A, R1, R2, and R3 are defined herein. Also disclosed are pharmaceutically acceptable salts of the compounds, compositions containing the compounds, and methods of using the compounds to treat, e.g., cancer.Type: ApplicationFiled: December 22, 2011Publication date: July 12, 2012Inventors: Robert N. Atkinson, Andy J. Ommen, James M. Veal, Kenneth H. Huang, Emilie D. Smith
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Publication number: 20120165326Abstract: The invention relates to novel products of the formula (I) where: (II) is a single or double bond; F is a fluorine atom, Ra is H, HaI, alkoxy, O-cycloalkyl, —O— heterocycloalkyl; —NH-heterocycloalkyl, heteroaryl, phenyl, NHCOalk NHCOcycloalk or NR1 R2; X is S, SO or SO2, A is NH or S; W is H, alkyl, or COR with R being cycloalkyl; alkyl optionally substituted by NR3R4, alkoxy, hydroxy, phenyl, heteroaryl or heterocycloalkyl; alkoxy optionally substituted by NR3R4, i.e. a O—(CH2)n-NR3R4 radical, an O-phenyl or an O—(CH2)n-phenyl radical, with phenyl optionally substituted and n=1 to 4; or the NR1 R2 radical; R1 is H or alk and R2 is H, cycloalkyl or alkyl; R3 and R4 are H, alk, cycloalkyl, heteroaryl or phenyl; R1, R2 and/or R3, R4 form a cycle together with N optionally containing O, S, N and/or NH; heterocycloalkyl, heteroaryl and phenyl and cycles all being optionally substituted; wherein said products can be in any isomer or salt form, and can be used as drugs, in particular as MET inhibitors.Type: ApplicationFiled: February 4, 2010Publication date: June 28, 2012Applicant: SANOFIInventors: Conception Nemecek, Antonio Ugolini, Eric Bacque, Dominique Damour, Gilles Barbalat, Sylvie Wentzler
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Publication number: 20120165196Abstract: The present invention relates to a hydrate of sulfonylurea compound represented by formula (I): having herbicidal activity, a process for producing the same, a suspension formulation containing the same, and the like.Type: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yu YANAGISAWA, Daisaku KAMO
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Publication number: 20120148531Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: December 1, 2011Publication date: June 14, 2012Applicant: Amgen Inc.Inventors: Brian K. ALBRECHT, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie Springer, Markian Stec, Ning Xi, Kevin Yang
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Publication number: 20120149662Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula (I).Type: ApplicationFiled: August 27, 2010Publication date: June 14, 2012Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pravin L. Kotian, V. Satish Kumar, Minwan Wu, Tsu-Hsing Lin
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Patent number: 8198272Abstract: The invention relates to novel compounds of formula I where X, A?, Q1, Q2, Q3, R2, R3, R4, R5, R6, R7, R8 and R9 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.Type: GrantFiled: August 5, 2010Date of Patent: June 12, 2012Assignee: Sanofi-AventisInventors: Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Karl Schoenafinger, Henning Steinhagen
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Publication number: 20120142681Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: ApplicationFiled: August 10, 2010Publication date: June 7, 2012Applicant: NOVARTIS AGInventors: Feng He, Miao Dai, Xingnian Fu, Yue Li, Lei Liu, Yuan Mi, Yao-chang Xu, Guoliang Xun, Zhengtian Yu, Ji Yue Zhang
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Publication number: 20120135986Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: January 25, 2012Publication date: May 31, 2012Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antionette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
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Patent number: 8183241Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: May 31, 2006Date of Patent: May 22, 2012Assignee: UCB Pharma, S.A.Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
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Publication number: 20120122680Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 0, 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: August 3, 2010Publication date: May 17, 2012Applicant: E.I. Du Pont de Nemours and CompanyInventors: Caleb William Holyoke, JR., Wenming Zhang, kanu Maganbhai Patel, George Philip Lahm, My-Hanh Thi Tong
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Publication number: 20120121540Abstract: Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).Type: ApplicationFiled: August 8, 2008Publication date: May 17, 2012Inventors: Franz Ulrich Schmitz, Vincent W.F Tai, Roopa Ral, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Subramanian Baskaran, Irina Slobodov, Jack Maung, Martin Leon Neitzel
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Patent number: 8178533Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: May 31, 2006Date of Patent: May 15, 2012Assignee: UCB Pharma, S.A.Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
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Patent number: 8178534Abstract: Compounds of the following formula are provided for use with cMET: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using the compounds.Type: GrantFiled: August 14, 2009Date of Patent: May 15, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Jerome C. Bressi, Shaosong Chu, Philip Erickson, Mallareddy Komandla, Lily Kwok, John D Lawson, Jeffrey A Stafford, Michael B. Wallace, Zhiyuan Zhang, Sanjib Das
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Publication number: 20120115820Abstract: The present invention relates to a use of a compound having an acid pump antagonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for prevention or treatment of diseases in which abnormal gastrointestinal motility is involved. In addition, the present invention relates to the method of prevention or treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agent. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound having an acid pump antagonistic activity or a pharmaceutically acceptable salt thereof for the prevention or treatment of said diseases.Type: ApplicationFiled: July 9, 2010Publication date: May 10, 2012Inventors: Nobuyuki Takahashi, Shinichi Koizumi
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Patent number: 8173654Abstract: The invention is directed to triazolopyridazine compounds of Formula I: where R1, R5, R6, R7, R8, and A are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of c-Met, and the use of such compounds to reduce or inhibit kinase activity of c-Met in a cell or a subject, and modulate c-Met expression in a cell or subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to c-Met. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.Type: GrantFiled: August 7, 2008Date of Patent: May 8, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Tianbao Lu, Richard Alexander, Richard W. Connors, Maxwell D. Cummings, Robert A. Galemmo, Heather Rae Hufnagel, Dana L. Johnson, Ehab Khalil, Kristi A. Leonard, Thomas P. Markotan, Anna C. Maroney, Jan L. Sechler, Jeremy M. Travins, Robert W. Tuman
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Publication number: 20120108587Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula (I) wherein A1, A2, A3, A4, L, R1, R2, R3, R5 and m are as defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, ankylosing spondylitis, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula (I).Type: ApplicationFiled: October 7, 2009Publication date: May 3, 2012Applicant: AMGEN Inc.Inventors: Andrew Tasker, Liping H. Pettus, Ryan Wurz
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Publication number: 20120107275Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: December 12, 2011Publication date: May 3, 2012Applicant: Amgen Inc.Inventors: Brian K. Albrecht, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie Springer, Markian Stec, Ning Xi, Kevin Yang
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Publication number: 20120108595Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.Type: ApplicationFiled: June 28, 2010Publication date: May 3, 2012Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
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Publication number: 20120101100Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: February 25, 2009Publication date: April 26, 2012Inventors: Shanta Bist, Brian Dangel, Brian Sherer
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Publication number: 20120088741Abstract: Certain aryl-substituted heterocyclic urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: June 4, 2010Publication date: April 12, 2012Inventors: J. Guy Breitenbucher, Mark S. Tichenor, Jeffrey E. Merit, John M. Keith, Natallie A. Hawryluk, Alison L. Chambers
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Patent number: 8153789Abstract: The invention provides novel imidazo[1,2-b]pyridazines of formula (I) and pharmaceutically acceptable salts, polymorphs, hydrates, tautomers, solvates and stereoisomers thereof. Compounds of formula (I) are useful for treating or preventing diseases associated with GABAA receptors modulation, anxiety, epilepsy, sleep disorders including insomnia, and for inducing sedation-hypnosis, anesthesia, sleep and muscle relaxation. The invention also provides synthetic procedures for preparing said compounds and certain intermediates, as well as intermediates themselves.Type: GrantFiled: March 28, 2007Date of Patent: April 10, 2012Assignee: Ferrer Internacional, S.A.Inventors: José Luís Falcó, Albert Palomer, Antonio Guglietta
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Patent number: 8148524Abstract: A process for producing a sulfonyl chloride compound comprising: (A) a step comprising reacting a pyridazine compound represented by the formula (1): wherein R1 represents a hydrogen atom, a halogen atom, an alkyl group which may be substituted with a halogen atom or atoms, or the like, R2 and R3 are the same or different and each represents a hydrogen atom or the like, R4 represent a hydrogen atom, a halogen atom, an alkyl group which may be substituted with a halogen atom or atoms, or the like, with a sulfonating agent; (B) a step comprising contacting the reaction mixture obtained in the step (A) with a chlorinating agent; and (C) a step comprising mixing the reaction mixture obtained in the step (B) with an aqueous inorganic base solution to separate an organic layer containing a sulfonyl chloride compound represented by the formula (2): wherein R1 to R4 are the same meanings as defined above.Type: GrantFiled: August 22, 2006Date of Patent: April 3, 2012Assignee: Sumitomo Chemical Company, LimitedInventor: Koichi Nakazawa
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Publication number: 20120077816Abstract: The present invention is related to heterocycles represented by a compound of Formula I that are novel allosteric modulators of ?7 nAChRs and/or GABAA receptors. The invention also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on ?7 nAChRs and negative allosteric modulation of GABAA receptors in a mammal by administering an effective amount of a compound of Formula I.Type: ApplicationFiled: March 9, 2010Publication date: March 29, 2012Inventors: Timothy B.C. Johnstone, Dark J. Hogenkamp, Kelvin W. Gee
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Publication number: 20120077787Abstract: New compounds of the Formula (I): for the treatment of non-insulin-dependent diabetes mellitus.Type: ApplicationFiled: December 6, 2011Publication date: March 29, 2012Applicant: NOVARTIS AGInventors: Daniel Kaspar Baeschlin, Nils OSTERMANN, Francois GESSIER, Finton SIROCKIN, Kenji NAMOTO
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Patent number: 8143253Abstract: Compounds of formula I in free or salt or solvate form, where R1, R2 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: July 24, 2008Date of Patent: March 27, 2012Assignee: Novartis AGInventors: Dimitrios Lizos, Sven Weiler, Nikolaus Johannes Stiefl
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Publication number: 20120071475Abstract: Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 26, 2010Publication date: March 22, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Daisuke Taniyama, Yasunori Mitsuoka, Kayoko Hata
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Publication number: 20120071474Abstract: The present invention relates to compounds of Formula I, II or III or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: ApplicationFiled: March 19, 2010Publication date: March 22, 2012Applicant: AMGEN INC.Inventors: Yunxin Y. Bo, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Aaron C. Siegmund, Nuria A. Tamayo, Kevin C. Yang
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Publication number: 20120065184Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.Type: ApplicationFiled: September 8, 2011Publication date: March 15, 2012Applicant: IRM LLCInventors: Yi Fan, Jon Loren, Valentina Molteni, Pamela A. Albaugh, Gregory Chopiuk, Jeffrey M. Smith, Brenton T. Flatt
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Publication number: 20120059162Abstract: Provided are a compound represented by general formula (1) and having a TTK inhibitory action and a medicine containing the compound. In formula (1), (X, Y, V, W) is (—N?, ?CR1—, ?N—, —CR7?), (—CR2?, ?N—, ?N—, —CR7?), etc.; A is an (un)substituted aromatic hydrocarbon ring, etc.; L is a single bond, —C(?O)—NRA—, etc.; Z is a group represented by the formula —NR3R4 or a group represented by the formula —OR5; R1 to R3, R6, and R7 each is a hydrogen atom, etc.; R4 and R5 each is an (un)substituted alkyl, etc.; and R8 is an (un)substituted cycloalkyl, etc.Type: ApplicationFiled: July 27, 2011Publication date: March 8, 2012Applicant: Oncotherapy Science, Inc.Inventors: Ken-ichi Kusakabe, Hiroshi Yoshida, Kohei Nozu, Hiroshi Hashizume, Genta Tadano, Jun Sato, Yuusuke Tamura, Yasunori Mitsuoka
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Publication number: 20120058997Abstract: The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.Type: ApplicationFiled: July 21, 2011Publication date: March 8, 2012Applicant: SuperGen, Inc.Inventors: Yong Xu, Benjamin G. Brenning, Steven G. Kultgen, Xiaohui Liu, Michael Saunders, Koc-Kan Ho
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Nitrogen-Containing Fused Heterocyclic Compounds and Their use as Beta Amyloid Production Inhibitors
Publication number: 20120053171Abstract: A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by A?.Type: ApplicationFiled: February 24, 2010Publication date: March 1, 2012Inventors: Noritaka Kitazawa, Daisuke Shinmyo, Koichio Ito, Nobuaki Sato, Daiju Hasegawa, Toshiyuki Uemura, Toru Watanabe -
Publication number: 20120046294Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: ApplicationFiled: February 22, 2011Publication date: February 23, 2012Inventors: John F. Kadow, Richard Pracitto
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Publication number: 20120040987Abstract: The invention relates to novel products of the formula (I) where: (II) is a single or double bond; Rb is a hydrogen or fluorine atom; Ra is a NH-Rc radical in which Rc is an optionally substituted heterocycloalkyl, aryl, heteroaryl or -alkylcycloalkyl radical; X is S, SO, or SO2; A is NH or S; W is H, alkyl, or COR with R being cycloalkyl; alkyl; alkoxy; O-phenyl; —O— (CH2)n-phenyl with n=1 to 4; or NR1R2 with R1 being H or alk and R2 is H, cycloalkyl or alkyl; or R1, R2 form a cycle together with N optionally containing O, S, N and/or NH; all of said radicals being optionally substituted; wherein said products can be in any isomer or salt form, and can be used as drugs, in particular as MET inhibitors.Type: ApplicationFiled: February 4, 2010Publication date: February 16, 2012Applicant: SANOFIInventors: Eric Bacque, Conception Nemecek, Antonio Ugolini, Sylvie Wentzler