Piperazine Ring Patents (Class 544/121)
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Publication number: 20140213737Abstract: A method for enhancing, by at least 10 fold, the antibacterial activity of an antisense oligonucleotide composed of morpholino subunits linked by phosphorus-containing intersubunit linkages. The method includes one or both of: conjugating an arginine-rich carrier to a 3? or 5? end of the oligonucleotide and modifying the oligonucleotide to contain 20%-50% intersubunit linkages that are positively charged at physiological pH. Also disclosed is an antisense oligonucleotide having enhanced antibacterial activity by virtue of one or both modifications.Type: ApplicationFiled: August 9, 2013Publication date: July 31, 2014Applicant: Sarepta Therapeutics, Inc.Inventors: Dwight D. Weller, Bruce L. Geller, Patrick L. Iversen, Lucas D. Tilley, Jed N. Hassinger
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Publication number: 20140213582Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: ApplicationFiled: December 20, 2013Publication date: July 31, 2014Applicant: EPIZYME, INC.Inventors: KENNETH W. DUNCAN, RICHARD CHESWORTH, MICHAEL JOHN MUNCHHOF
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Publication number: 20140213580Abstract: Provided are compounds with the following structure, formula (I) pharmaceutically acceptable salts thereof, use of those compounds for treating cancer and pharmaceutical compositions comprising those compounds.Type: ApplicationFiled: June 18, 2012Publication date: July 31, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
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Patent number: 8791090Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.Type: GrantFiled: March 31, 2010Date of Patent: July 29, 2014Assignee: Kowa Company, Ltd.Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
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Publication number: 20140206865Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.Type: ApplicationFiled: March 21, 2014Publication date: July 24, 2014Applicant: SYMPHONY EVOLUTION, INC.Inventors: Lynne Canne Bannen, Erick Wang Co, Vasu Jammalamadaka, John M. Nuss, Moon Hwan Kim, Donna Tra Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, Zhaoyang Wen, Wei Xu, Richard George Khoury
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Publication number: 20140200218Abstract: Disclosed are crystalline forms of (3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione benzenesulfonate salt and pharmaceutical compositions thereof. Also disclosed are processes for the preparation the above compounds and methods for use thereof.Type: ApplicationFiled: March 18, 2014Publication date: July 17, 2014Applicant: Glaxo Group LimitedInventors: Richard Bellingham, Andrew Mark Buswell, Victoria Ironmonger, Michael Urquhart
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Patent number: 8778929Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: GrantFiled: September 28, 2009Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Patent number: 8779128Abstract: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.Type: GrantFiled: May 27, 2011Date of Patent: July 15, 2014Assignee: Sarepta Therapeutics, Inc.Inventors: Gunnar J. Hanson, Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
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Publication number: 20140194422Abstract: The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase.Type: ApplicationFiled: June 12, 2012Publication date: July 10, 2014Applicant: EMORY UNIVERSITYInventors: Thota Ganesh, Aiming Sun, Susane M. Smith, John David Lambeth
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Publication number: 20140187540Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.Type: ApplicationFiled: February 15, 2012Publication date: July 3, 2014Applicant: The Johns Hopkins UniversityInventors: Donald J. Zack, Cynthia Berlinicke, Laszlo Hackler, Zhiyong Yang, Joseph P. Steiner, Tomas Vojkovsky, Dana Ferraris, Barbara S. Slusher, James Inglese
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Publication number: 20140187556Abstract: Anti-amyloid compounds are provided along with methods of use thereof.Type: ApplicationFiled: March 2, 2012Publication date: July 3, 2014Applicant: Treventis CorporationInventors: Mark A. Reed, Arun Yadav, Scott C. Banfield, Christopher J. Barden
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Publication number: 20140187531Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.Type: ApplicationFiled: March 3, 2014Publication date: July 3, 2014Applicant: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Xilu Wang, Noah P. Tu, Michael D. Wendt, Alexander R. Shoemaker, Michael J. Mitten
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Patent number: 8765750Abstract: The present invention provides a piperazine compound represented by Formula (I) or a salt thereof, wherein X represents CH or an N atom; R1 represents C1-6 alkyl; R2 represents C1-6 alkyl that may have one or more substituents, C2-6 alkenyl that may have one or more substituents, β(C?O)βN(R3)(R4), or β(C?O)βOR5, R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents; or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; and R5 represents hydrogen or C1-6 alkyl that may have one or more substituents or aralkyl.Type: GrantFiled: January 19, 2011Date of Patent: July 1, 2014Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Yoshihiro Urade, Makoto Kitade, Kazuhiko Shigeno, Keiko Yamane, Katsunao Tanaka
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Publication number: 20140178360Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.Type: ApplicationFiled: February 27, 2014Publication date: June 26, 2014Applicants: DCB-USA LLC, DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Mann-Yan KUO, Ying-Shuan Lee, Paonien Chen, Li Jung Chen, Yann Yu Lu, Yi-Ting Huang, Hung-Yi Hsu, Ping-Kuei Tsai
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Publication number: 20140179666Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: April 20, 2012Publication date: June 26, 2014Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
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Publication number: 20140155387Abstract: The present invention refers to: a compound having the general formula (I), wherein n is 0, 1, 2 or; m is 0, 1, 2 or 3; o is 0, 1, 2 or 3; W, X, Y and Z are independently selected from CH, N or N-oxide; A is NR4, C?O, C?S, OP(O)(O), P?O, CH2, or a heteroarly selected from the group consisting of (a), (b), (c), (d), (e), (f), (g); V is C?O, O, S, CH2, or NR5; as well as its use in treating inflammatory diseases such as asthma, COPD, inflammation post infection, arthritis, atherosclerosis, pain and dermatitis.Type: ApplicationFiled: April 20, 2012Publication date: June 5, 2014Applicants: QURIENT, CO. LTD., INSTITUT PASTEUR KOREAInventors: Zaesung No, Jaeseung Kim, Sung-Jun Han, Jung Hwan Kim, Young Sam Park, Sangchul Lee, Kiyean Nam, Jeongjun Kim, Jinhwa Lee, Sunhee Kang, Min Jung Seo, Saeyeon Lee, Gahee Choi
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Patent number: 8742099Abstract: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.Type: GrantFiled: May 20, 2013Date of Patent: June 3, 2014Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, Deirdre Mary Bernadette Hickey, John Liddle, Andrew McMurtrie Mason
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Publication number: 20140148443Abstract: Disclosed are compounds of Formula I or pharmaceutically acceptable salts thereof, wherein X1, X2, X3, R1, R2 and R3 are as described in this application, and methods of using the compounds in the treatment of cancer.Type: ApplicationFiled: November 20, 2013Publication date: May 29, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Xin-Jie Chu, Allen John Lovey, Binh Thanh Vu, Chunlin Zhao
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Patent number: 8729077Abstract: Disclosed are compounds, stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, their preparation, use, and compositions thereof for treating an infection mediated at least in part by a virus in the Flaviviridae family of viruses.Type: GrantFiled: November 19, 2009Date of Patent: May 20, 2014Assignee: GlaxoSmithKline LLCInventors: Frank Ulrich Schmitz, Roopa Rai, Christopher Don Roberts, Wieslaw Kazmierski, Richard Grimes
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Patent number: 8716286Abstract: The present invention relates to crystalline forms of (3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione benzenesulfonate salt and pharmaceutical compositions thereof. Also disclosed are processes for the preparation the above compounds and methods for use thereof.Type: GrantFiled: October 28, 2010Date of Patent: May 6, 2014Assignee: Glaxo Group LimitedInventors: Richard Bellingham, Andrew Mark Buswell, Victoria Ironmonger, Michael Urquhart
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Publication number: 20140107119Abstract: 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: November 15, 2013Publication date: April 17, 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, Todd M. Hansen
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Publication number: 20140100225Abstract: Novel compounds and their synthesis are described. Methods for using these compounds in the prevention or treatment of cancer, a bacterial infection or a viral infection in a subject are also described.Type: ApplicationFiled: October 4, 2013Publication date: April 10, 2014Applicants: Inhibikase Therapeutics, Inc., Sphaera Pharma Pvt. Ltd., Sphaera Pharma Pte. Ltd.Inventors: Rhushikesh Chandrabhan Deokar, Sundeep Dugar, Dinesh Mahajan, Milton Henry Werner
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Publication number: 20140100224Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.Type: ApplicationFiled: June 26, 2013Publication date: April 10, 2014Applicants: The University of North Carolina at Chapel Hill, U.S. Government represented by the Department of Veterans Affairs, The Regents of the University of CaliforniaInventors: Frank M. Longo, Stephen M. Massa
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Publication number: 20140100210Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.Type: ApplicationFiled: December 6, 2013Publication date: April 10, 2014Applicant: Astellas Pharma Inc.Inventors: Kousei YOSHIHARA, Daisuke SUZUKI, Susumu YAMAKI, Hiroyoshi YAMADA, Hisashi MIHARA, Norio SEKI
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Patent number: 8691184Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.Type: GrantFiled: January 24, 2012Date of Patent: April 8, 2014Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Haibin Zhou, Jianfang Chen, Angelo Aguilar, Jennifer L. Meagher, Duxin Sun, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachem, Jeanne Stuckey, Xiaoqin Li
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Patent number: 8686136Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.Type: GrantFiled: December 12, 2012Date of Patent: April 1, 2014Assignee: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Xiaohong Song, Xilu Wang, Michael Wendt
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Patent number: 8685981Abstract: Compounds exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof: wherein A is selected from among a 3- to 10-membered heterocyclyl group, B is selected from among an amino group, and X is selected from N and CH.Type: GrantFiled: July 14, 2011Date of Patent: April 1, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Daigo Asano
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Publication number: 20140088106Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: October 14, 2013Publication date: March 27, 2014Applicant: AbbVie Inc.Inventors: Milan Bruncko, Yujia Dai, 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, Todd M. Hansen
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Patent number: 8680097Abstract: The invention discloses benzothiophene alkanol piperazine derivatives and their use as antidepressants. The invention discloses the said benzothiophene alkanol piperazine derivative having triple inhibition effect on the reuptake of 5-HT, NA and DA. Compared with clinical used antidepressants so far having single target, e.g. desipramine and fluoxetine, and clinical used antidepressants so far having double targets, e.g venlafaxine and duloxetine, the said benzothiophene alkanol piperazine derivatives of the present invention may have a broader indication range and less toxic and side effects to nervous system. The benzothiophene alkanol piperazine derivatives are the compounds with the following formula or their pharmaceutically acceptable salts, wherein Ar1, R1-R4, X, Y, m and n have the same definition as defined in claim 1.Type: GrantFiled: June 30, 2009Date of Patent: March 25, 2014Assignees: CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co. Ltd., Shanghai Institute of Pharmaceutical IndustryInventors: Jianqi Li, Kai Gao, Na Lv
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Publication number: 20140073584Abstract: The invention relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as PI-3 kinase.Type: ApplicationFiled: September 30, 2013Publication date: March 13, 2014Applicant: SIGNALRX PHARMACEUTICALS, INC.Inventors: Guillermo A. Morales, Kevin Weber, Jessica Newblom, Joseph R. Garlich
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Publication number: 20140073631Abstract: Disclosed are guanidine and biguanidine derivatives which have anti-viral and antibacterial activity. Also disclosed are pharmaceutical compositions containing such compounds as an active ingredient, and anti-viral and anti-bacterial methods utilizing such compounds. Methods of treating infections using the guanidine and biguanidine derivatives are also disclosed.Type: ApplicationFiled: September 10, 2013Publication date: March 13, 2014Applicant: Vymed CorporationInventor: B. Vithal SHETTY
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Publication number: 20140066621Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: July 26, 2013Publication date: March 6, 2014Applicants: The Walter and Eliza Hall Institute of Medical Research, AbbVie Inc.Inventors: Milan Bruncko, Yujia Dai, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. Kunzer, Robert A. Mantei, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiahong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Peter Edward Czabotar, Guillaume Laurent Lessene, Peter Malcolm Colman, William J. McClellan
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Patent number: 8664203Abstract: The present invention relates to thiazole derivatives of formula I and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.Type: GrantFiled: April 21, 2010Date of Patent: March 4, 2014Assignee: Actelion Pharmaceuticals Ltd.Inventors: Eva Caroff, Kurt Hilpert, Francis Hubler, David Lehmann, Emmanuel Meyer, Dorte Renneberg
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Patent number: 8664218Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof.Type: GrantFiled: January 30, 2013Date of Patent: March 4, 2014Assignee: Astex Therapeutics Ltd.Inventors: Brian John Williams, Martyn Frederickson
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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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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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Patent number: 8658649Abstract: The invention is directed to a compound of formula (I): and the prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs. Such a compound has valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.Type: GrantFiled: March 10, 2009Date of Patent: February 25, 2014Assignee: SanofiInventors: Timothy A. Gillespy, Paul Eynott, Elizabeth M. Allen, Kin T. Yu, Asher Zilberstein
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Publication number: 20140051852Abstract: The invention provides a method for the synthesis of dehydrogenated lactam drugs of Formula I:Type: ApplicationFiled: August 2, 2013Publication date: February 20, 2014Applicant: Alkermes Pharma Ireland LimitedInventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
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Patent number: 8653262Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.Type: GrantFiled: May 29, 2008Date of Patent: February 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Heiner Ebel, Silke Hobbie
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Publication number: 20140045815Abstract: Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: September 5, 2013Publication date: February 13, 2014Applicant: Samumed, LLCInventors: John Hood, Sunil Kumar KC
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Publication number: 20140038937Abstract: The invention concerns chromenone compounds of Formula I; or pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, n and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.Type: ApplicationFiled: August 6, 2013Publication date: February 6, 2014Applicant: Astrazeneca ABInventors: Bernard Christophe BARLAAM, Sebastien Louis DEGORCE, Christine Marie Paul LAMBERT-VAN DER BREMPT, Jean-Jacques Marcel LOHMANN, Patrick PLE
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Publication number: 20140010892Abstract: The invention provides compounds of the formula (I): The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Aurora kinases and are therefore useful to treat cancer and viral diseases.Type: ApplicationFiled: May 24, 2013Publication date: January 9, 2014Applicant: Astex Therapeutics LimitedInventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Eva Figueroa NAVARRO, Adrian Liam GILL, Steven HOWARD, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Patent number: 8623857Abstract: The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R1, R2, R3, and R6 are as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway.Type: GrantFiled: May 24, 2011Date of Patent: January 7, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Hon-Chung Tsui, Sunil Paliwal, Hyunjin M. Kim, Angela D. Kerekes, Mary Ann Caplen, Sara J. Esposite, Brian A. McKittrick, Thierry Olivier Fischmann, Ronald J. Doll, Matthew Paul Rainka, Ang Li
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Publication number: 20140005383Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.Type: ApplicationFiled: September 5, 2013Publication date: January 2, 2014Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Publication number: 20140005170Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: September 6, 2013Publication date: January 2, 2014Applicant: Samumed, LLCInventors: John Hood, David Mark Wallace, Sunil Kumar KC
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Patent number: 8618097Abstract: The present invention provides compounds of Formula (I), including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: GrantFiled: July 3, 2008Date of Patent: December 31, 2013Assignees: Array Biopharma, Inc., Genentech, Inc.Inventors: Josef Bencsik, James F. Blake, James M. Graham, Martin F. Hentemann, Nicholas C. Kallan, Ian S. Mitchell, Stephen T. Schlachter, Keith L. Spencer, Dengming Xiao, Rui Xu, Mike Welch, Jun Liang, Brian S. Safina
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Patent number: 8618110Abstract: The present invention includes and relates generally to compounds of structural Formula (I), or a salt, solvate, or prodrug thereof, which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells.Type: GrantFiled: February 9, 2010Date of Patent: December 31, 2013Assignee: VM Discovery Inc.Inventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20130345197Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: June 3, 2013Publication date: December 26, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Luc Farmer, Randy Bethiel, Edmund Harrington, Jeremy Green, John Court, Jon Come, David Lauffer, Alex Aronov, Hayley Binch, Dean Boyall, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Michael Mortimore, Francoise Pierard, Daniel Robinson, Jian Wang, Joanne Pinder, Tiansheng Wang, Albert Pierce
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Patent number: 8614318Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.Type: GrantFiled: July 24, 2006Date of Patent: December 24, 2013Assignee: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, Steven Elmore, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Andrew Petros, Xiaohong Song, Xilu Wang, Noah Tu, Michael Wendt, Alexander R. Shoemaker, Michael J. Mitten
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Publication number: 20130338157Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: February 22, 2013Publication date: December 19, 2013Applicant: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M.K. Pennell, John J. Kim Wright, Wei Chen, Manmohan R. Leleti, Yandong Li, Lianfa Li, Yuan Xu, Mark M. Gleason, Yibin Zeng, Kevin Lloyd Greenman