The Additional Hetero Ring Is A Diazine Patents (Class 514/252.02)
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Publication number: 20140100231Abstract: Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 7, 2013Publication date: April 10, 2014Inventors: Kenneth L. Arrington, Christopher Burgey, Robert Gilfillan, Yongxin Han, Mehul Patel, Chun Sing Li, Yaozong Li, Yunfu Luo, Zhiyu Lei
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Publication number: 20140100214Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: December 6, 2013Publication date: April 10, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. CASTRO, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Patent number: 8686155Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: June 28, 2011Date of Patent: April 1, 2014Assignee: Amgen Inc.Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
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Publication number: 20140079736Abstract: The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula (I): Q-Y—R1—R2 (I), wherein Q, Y, R1, and R2 are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula (I) in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.Type: ApplicationFiled: April 11, 2012Publication date: March 20, 2014Applicant: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventor: Sanjay A. Desai
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Publication number: 20140073634Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: ApplicationFiled: August 23, 2013Publication date: March 13, 2014Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer CenterInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Joe Marszalek, Gang Liu, Zhijun Kang, Chris Carroll, Timothy McAfoos, Barbara Czako
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Publication number: 20140073620Abstract: This invention relates to a compound of the formula (I): The invention also relates to processes for the preparation of the compound of the formula (I), pharmaceutical agents or compositions containing the compound or a method of using the compound for the treatment of proliferative diseases, such as cancer, as well as the treatment of diseases ameliorated by the control and/or inhibition of lymphangiogenesis.Type: ApplicationFiled: August 16, 2013Publication date: March 13, 2014Applicant: CANCER THERAPEUTICS CRC PTY LIMITEDInventors: Richard Charles FOITZIK, Benjamin Joseph Morrow, Catherine Fae Hemley, Gillian Elizabeth Lunniss, Michelle Ang Camerino, Danny Ganame, Paul Anthony Stupple, Romina Lessene, Wilhelmus Johannes Antonius Kersten, Andrew John Harvey, Ian Peter Holmes
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Publication number: 20140066430Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: ApplicationFiled: October 3, 2013Publication date: March 6, 2014Applicant: Amgen Inc.Inventors: Victor J. CEE, Holly L. DEAK, Bingfan DU, Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Hanh Nho NGUYEN, Philip R. Olivieri, Vinod F. Patel, Karina ROMERO, Laurie Schenkel
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Publication number: 20140057890Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: October 18, 2013Publication date: February 27, 2014Applicant: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
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Publication number: 20140057889Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: October 18, 2013Publication date: February 27, 2014Applicant: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
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Patent number: 8658643Abstract: Compounds selected from the group according to claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: August 3, 2012Date of Patent: February 25, 2014Assignee: Merck Patent GmbHInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Publication number: 20140051672Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: August 7, 2013Publication date: February 20, 2014Inventors: Atwood Kim CHEUNG, Donovan Noel CHIN, Natalie DALES, Aleem FAZAL, Timothy Brian HURLEY, John KERRIGAN, Gary O'BRIEN, Lei SHU, Robert SUN, Moo Je SUNG
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Publication number: 20140050699Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.Type: ApplicationFiled: October 10, 2013Publication date: February 20, 2014Applicant: CALITHERA BIOSCIENCES INC.Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
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Publication number: 20140045849Abstract: This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.Type: ApplicationFiled: April 10, 2012Publication date: February 13, 2014Inventors: David McGowan, Pierr Jeane-Marie Bernar Raboisson, Werner Embrechts, Tim Hugo Maria Jonckers, Stefaan Julien Last, Serge Maria Aloysius Pieters, Jaromir Vlach
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Publication number: 20140038957Abstract: This invention relates to pyrrolopyrimidine derivatives of formula (I): where R1, X, p, R4, R2 and R3 are as defined herein, and their use as pharmaceuticals.Type: ApplicationFiled: December 15, 2011Publication date: February 6, 2014Inventors: David R. Witty, David Norton, Jason Paul Tierney, Ghislaine Lorthioir, Mairi Sime, Karen Louise Philpott
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Publication number: 20140038960Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: October 4, 2013Publication date: February 6, 2014Applicant: MERCK PATENT GMBHInventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Publication number: 20140031354Abstract: The present invention relates to compounds of Formula I: as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.Type: ApplicationFiled: July 30, 2012Publication date: January 30, 2014Applicant: Astar Biotech LLCInventors: Chunrong YU, Haihong Huang, Dongfeng Zhang, Peng Li
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Publication number: 20140031343Abstract: Drug combinations which contain a PDE4-inhibitor and a non-steroidal anti-inflammatory drug (NSAID), processes for preparing them, and their use in treating in particular respiratory complaints such as COPD, chronic sinusitis, and asthma. The PDE4 inhibitors of the drug combinations include compounds of general formula 1 wherein X is SO or SO2, but preferably SO, R3 is an optionally substituted, mono- or bicyclic, unsaturated, partly saturated or saturated heterocyclic group or an optionally substituted, mono- or bicyclic heteroaryl, and R1 and R2 have the meanings given in claim 1.Type: ApplicationFiled: August 15, 2013Publication date: January 30, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Peter NICKOLAUS, Rolf GOEGGEL, Daniel PETER
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Patent number: 8637518Abstract: Compounds of the formula (I), in which Y, R1, R2, R3 and R3? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: November 24, 2009Date of Patent: January 28, 2014Assignee: MERCK PATENT GmbHInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Publication number: 20140024648Abstract: The invention relates to pyridazinone and pyridone compounds having formula (I) or (I?), and pharmaceutically acceptable salts, hydrates, and solvates thereof (I) wherein R1/R4 and X and X3 are as defined in the claims. The invention further relates to their use as inhibitors of copper-containing amine oxidases. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds, pharmaceutically acceptable salts, hydrates, or solvates thereof.Type: ApplicationFiled: March 6, 2012Publication date: January 23, 2014Applicant: BIOTIE THERAPIES CORPORATIONInventors: Marjo Pihlavisto, David Smith, Auni Juhakoski, Ferenc Fulop, Laszlo Lazar, Istvan Szatmari, Ferenc Miklos, Zsolt Szakonyi, Lorand Kiss, Marta Palko
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Patent number: 8633193Abstract: Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: January 26, 2011Date of Patent: January 21, 2014Assignee: Novartis AGInventors: Jun Yuan, Peter Hrnciar, Qin Guo, George D. Maynard
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Publication number: 20140011770Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: September 10, 2013Publication date: January 9, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
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Publication number: 20140011798Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: January 24, 2013Publication date: January 9, 2014Applicant: NOVARTIS AGInventors: Pascal FURET, Vito GUAGNANO, Philipp HOLZER, Joerg KALLEN, Lv LIAO, Robert MAH, Liang MAO, Keiichi MASUYA, Achim SCHLAPBACH, Stefan STUTZ, Andrea VAUPEL
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Publication number: 20140005168Abstract: 5-Azaindazole compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: June 26, 2013Publication date: January 2, 2014Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Vickie H. Tsui, Xiaojing Wang
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Publication number: 20130338139Abstract: Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.Type: ApplicationFiled: June 18, 2013Publication date: December 19, 2013Inventors: Amy Allan, Bryan Branstetter, James Breitenbucher, Brian Dyck, Tawfik Gharbaoui, Laurent Gomez, Andrew Richard Hudson, Tami Jo Marrone, Troy Vickers, Michael I. Weinhouse
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Publication number: 20130338162Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: July 29, 2013Publication date: December 19, 2013Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Lijun Sun, Keizo Koya, Shoujun Chen, Zachary Demko, Zhi-Qiang Xia
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Publication number: 20130331382Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, J, and X3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.Type: ApplicationFiled: March 12, 2013Publication date: December 12, 2013Inventors: Robert D. HUBBARD, Le WANG, Chang H. PARK, Chaohong SUN, Keith F. McDANIEL, John K. PRATT, Todd N. SOLTWEDEL, Michael D. WENDT, John H. HOLMS, Dachun LIU, George S. SHEPPARD
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Patent number: 8604037Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.Type: GrantFiled: August 18, 2011Date of Patent: December 10, 2013Assignee: Purdue Pharma, L.P.Inventors: Qun Sun, Laykea Tafesse, Sam Victory
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Patent number: 8604036Abstract: Compounds of the formula (I), in which R1, R2, R3, W and D have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: March 24, 2009Date of Patent: December 10, 2013Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
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Patent number: 8604016Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.Type: GrantFiled: November 19, 2012Date of Patent: December 10, 2013Assignee: Calithera Biosciences Inc.Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
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Patent number: 8598175Abstract: The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: GrantFiled: October 27, 2009Date of Patent: December 3, 2013Assignees: Sanofi, Mitsubishi Tanabe Pharma CorporationInventors: Nathalie Chereze, Thierry Gallet, Alistair Lochead, Mourad Saady, Corinne Veronique, Philippe Yaiche
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Patent number: 8598176Abstract: A pyridazine compound of the formula: has an excellent plant disease controlling effect.Type: GrantFiled: December 13, 2011Date of Patent: December 3, 2013Assignee: Sumitomo Chemical Company, LimitedInventor: Akio Manabe
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Patent number: 8592400Abstract: Drug combinations which contain a PDE4-inhibitor and a non-steroidal anti-inflammatory drug (NSAID), processes for preparing them, and their use in treating in particular respiratory complaints such as COPD, chronic sinusitis, and asthma. The PDE4 inhibitors of the drug combinations include compounds of general formula 1 wherein X is SO or SO2, but preferably SO, R3 is an optionally substituted, mono- or bicyclic, unsaturated, partly saturated or saturated heterocyclic group or an optionally substituted, mono- or bicyclic heteroaryl, and R1 and R2 have the meanings given in claim 2.Type: GrantFiled: February 18, 2010Date of Patent: November 26, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Peter Nickolaus, Rolf Goeggel, Daniel Peter
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Publication number: 20130310361Abstract: The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or analplastic lymphoma kinase (ALK).Type: ApplicationFiled: July 23, 2013Publication date: November 21, 2013Inventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Christian Cho-Hua Lee, Songchun Jiang, Kunyong Yang
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Publication number: 20130310364Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: July 16, 2013Publication date: November 21, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
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Publication number: 20130310375Abstract: The present invention relates to compositions and methods for modulating the Wnt signaling pathway.Type: ApplicationFiled: July 22, 2013Publication date: November 21, 2013Applicant: IRM LLCInventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
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Publication number: 20130310342Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.Type: ApplicationFiled: October 24, 2012Publication date: November 21, 2013Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
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Publication number: 20130303461Abstract: The technology described herein is directed to methods of determining oligonucleotide sequences, e.g. by enriching target sequences prior to sequencing the sequences.Type: ApplicationFiled: March 11, 2013Publication date: November 14, 2013Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Anthony John Iafrate, Long Phi Le, Zongli Zheng
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Patent number: 8580781Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: April 29, 2008Date of Patent: November 12, 2013Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
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Patent number: 8580790Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.Type: GrantFiled: June 7, 2012Date of Patent: November 12, 2013Assignee: SanofiInventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
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Publication number: 20130296332Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: Hans ALLGEIER, Yves AUBERSON, David CARCACHE, Philipp FLOERSHEIM, Christel GUIBOURDENCHE, Wolfgang FROESTL, Jörg KALLEN, Manuel KOLLER, Henri MATTES, Joachim NOZULAK, David ORAIN, Johanne RENAUD
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Publication number: 20130281426Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.Type: ApplicationFiled: June 18, 2013Publication date: October 24, 2013Inventors: Youhong HU, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
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Patent number: 8563565Abstract: A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has a potential use of a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.Type: GrantFiled: October 4, 2012Date of Patent: October 22, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Yoshihiko Norimine, Kunitoshi Takeda, Koji Hagiwara, Yuichi Suzuki, Yuki Ishihara, Nobuaki Sato
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Patent number: 8557813Abstract: Compounds of the formula I in which R1, R2, R3, R4? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: November 25, 2008Date of Patent: October 15, 2013Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
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Patent number: 8551984Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: GrantFiled: December 15, 2010Date of Patent: October 8, 2013Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Michael H. Reutershan, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hua Zhou
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Publication number: 20130261103Abstract: Pyridazinone compounds of Formula I including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: August 31, 2011Publication date: October 3, 2013Applicants: GENENTECH, INC., GILEAD CONNECTICUT, INC.Inventors: Kevin S. Currie, Xiaojing Wang, Wendy B. Young
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Publication number: 20130252963Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, or example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.Type: ApplicationFiled: December 5, 2011Publication date: September 26, 2013Inventors: Yun Jin, Zehong Wan, Qing Zhang
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Publication number: 20130252934Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: March 1, 2013Publication date: September 26, 2013Applicants: Genentech, Inc., Array BioPharma Inc.Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
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Publication number: 20130245033Abstract: A compound represented by formula (I) and the pharmaceutical acceptable salt thereof are disclosed, wherein, R1, R2, R3, R4, R5 and Ar are defined as those in the specification.Type: ApplicationFiled: September 6, 2010Publication date: September 19, 2013Applicant: Guangzhou Institutes of Biomedicine and Health, Chinese Academy of SciencesInventors: Wenhui Hu, Guifa Zhong, Ling Yang, Hongjiang Xu
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Publication number: 20130245022Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl 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, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Applicant: Janssen Pharmaceutica NVInventors: J. GUY BREITENBUCHER, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Sierestad
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Publication number: 20130237515Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, L1, L2, U and B are as defined in the application, which have valuable pharmacological properties, and in particular modulate the activity of the MCH receptor.Type: ApplicationFiled: February 28, 2013Publication date: September 12, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Thorsten OOST, Ralf LOTZ, Dirk STENKAMP