The Other Cyclo In The Bicyclo Ring System Is Five-membered Patents (Class 544/280)
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Publication number: 20140073657Abstract: The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases.Type: ApplicationFiled: November 8, 2013Publication date: March 13, 2014Inventors: Yun-Long Li, James D. Rodgers
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Publication number: 20140066463Abstract: There is provided polymorphs and amorphous form of pemetrexed or its pharmaceutical acceptable salts and process for making thereof.Type: ApplicationFiled: April 5, 2013Publication date: March 6, 2014Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY'S LABORATORIES LTD.Inventors: Raghavendracharyulu Venkata Palle, Sekhar Munaswamy Nariyam, Vijay Bhailalbhai Patel, Raghupati Rama Subrahmanyam Vinjamuri, Surya Narayana Devarakonda, Sesha Reddy Yarraguntla, Vamsi Krishna Mudapaka, Venu Nalivela
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Patent number: 8658635Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: GrantFiled: June 3, 2009Date of Patent: February 25, 2014Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Patent number: 8658637Abstract: Compounds of Formula (IA) wherein R1, R2, R3, A, B, C, D, E, G, X, Y, and Z are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: November 29, 2007Date of Patent: February 25, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Daniel Kuzmich, Darren DiSalvo, Hossein Razavi, Michael Jason Burke
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Publication number: 20140051654Abstract: The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: October 16, 2013Publication date: February 20, 2014Applicant: EPIZYME, INC.Inventors: Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz, Victoria M. Richon, Roy M. Pollock, Scott R. Daigle
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Patent number: 8648086Abstract: The present invention provides 5,6-bicyclic heteroaryl-containing urea compounds of Formula I or II and use of the same for treating conditions mediated by protein kinase such as VEGFR2, c-Met, PDGFR? c-Kit, CSF1R, or EphA2.Type: GrantFiled: August 20, 2010Date of Patent: February 11, 2014Assignee: Ascepion Pharmaceuticals, Inc.Inventors: Shan Jiang, Xinglong Xing, Qishan Wang, Ren Kong
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Publication number: 20140038940Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.Type: ApplicationFiled: March 15, 2013Publication date: February 6, 2014Inventors: Xiao XU, Xiaobo Wang, Long Mao, Li Zhao, Biao Xi
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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: 20140038981Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.Type: ApplicationFiled: June 13, 2013Publication date: February 6, 2014Inventors: Xiao XU, Xiaobo WANG, Long MAO, Li ZHAO, Biao XI
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Patent number: 8642604Abstract: The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tyrosine kinase, PI3 kinase and mTOR, or PI33 kinase, mTOR and tyrosine kinase.Type: GrantFiled: July 24, 2009Date of Patent: February 4, 2014Assignee: The Regents of the University of CaliforniaInventors: Zachary A. Knight, Beth Apsel, Kevan M. Shokat
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Publication number: 20140024661Abstract: A group of fused two ring pyrimidine compounds having a heterocycles substituent at the 2 position and a substituted amine at the 4 position as well as optional aliphatic, functional and/or aromatic components substituted at other positions of the pyrimidine and other ring are disclosed. In addition a group of quinazoline compounds having similar substituents at the 2 and 4 positions as well as at other positions are disclosed. These compounds are inhibitors of the AAA proteasome complex containing p97 and are effective medicinal agents for treatment of diseases associated with p97 bioactivity.Type: ApplicationFiled: July 19, 2013Publication date: January 23, 2014Applicant: Cleave Biosciences, Inc.Inventors: Han-Jie Zhou, Francesco Parlati
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Patent number: 8633206Abstract: Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.Type: GrantFiled: October 13, 2010Date of Patent: January 21, 2014Assignee: Pfizer Inc.Inventors: Michele Ann Promo, Jin Xie, Brad A. Acker, Susan J. Hartmann, Sergey Gregory Wolfson, Horng-Chih Huang, Eric Jon Jacobsen
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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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Patent number: 8633205Abstract: The present invention relates to compounds of the following formula: which are useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: February 2, 2006Date of Patent: January 21, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark Ledeboer, Albert Pierce, Guy Bemis, Luc Farmer, Tiansheng Wang, David Messersmith, John Duffy, Francesco Salituro, Jian Wang
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Publication number: 20140018361Abstract: The present invention provides furano- and pyrrolo-pyrimidine and pyridine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Geraldine C. Harriman, Donna L. Romero, Craig E. Masse, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Publication number: 20140011810Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.Type: ApplicationFiled: September 11, 2013Publication date: January 9, 2014Applicant: Gatekeeper Pharmaceuticals, Inc.Inventors: Nathanael S. Gray, Wenjun Zhou
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Publication number: 20140005183Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.Type: ApplicationFiled: June 27, 2013Publication date: January 2, 2014Inventors: Paul Galatsis, Matthew Merrill Hayward, Bethany Lyn Kormos, Travis T. Wager, Lei Zhang, Antonia Friederike Stepan, Jaclyn Louise Henderson, Ravi G. Kurumbail, Patrick Robert Verhoest
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Publication number: 20140005166Abstract: The present invention provides piperidinylcyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I, as defined herein, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: May 17, 2013Publication date: January 2, 2014Applicant: Incyte CorporationInventors: JAMES D. RODGERS, Stacey Shepard, Wenyu Zhu, Lixin Shao, Joseph Glenn
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Publication number: 20140005198Abstract: The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, A5, A6, A7, A8, A9, bond B, X, rings Z1 and Z2, R1 and R3 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: August 28, 2013Publication date: January 2, 2014Applicant: AMGEN INC.Inventors: Adrian L. SMITH, Elizabeth M. DOHERTY, Qi HUANG, Gang LIU
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Publication number: 20130345219Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: August 28, 2013Publication date: December 26, 2013Applicant: Synta Pharmaceuticals Corp.Inventors: Chi-Wan Lee, Teresa Prezewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
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Publication number: 20130345192Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.Type: ApplicationFiled: October 28, 2011Publication date: December 26, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
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Publication number: 20130345243Abstract: The present invention relates to pyrimidinedione compounds of formula (I), salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds of formula (I) or salts thereof as activators of AMPK.Type: ApplicationFiled: March 5, 2012Publication date: December 26, 2013Applicant: GLAXOSMITHKLINE LLCInventors: Anne Marie Jeanne Bouillot, Alain Claude-Marie Daugan, Yann Lamotte, Olivier Mirguet
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Patent number: 8614208Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.Type: GrantFiled: August 25, 2010Date of Patent: December 24, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Hiroshi Banno, Toshio Tanaka, Satoshi Sasaki
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Publication number: 20130338152Abstract: The present invention provides a compound the invention, and its use as a IGF-1R inhibitor. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: March 8, 2012Publication date: December 19, 2013Applicants: IRM LLC, NOVARTIS AGInventors: Bei Chen, Robin Alec Fairhurst, Songchun Jiang, Wenshuo Lu, Thomas H. Marsilje, III, Clive McCarthy, Pierre-Yves Michellys, Stefan Stutz
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Publication number: 20130338173Abstract: The present invention relates to carbocycle-substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 5, 2011Publication date: December 19, 2013Applicant: EPIZYME, INC.Inventors: Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz
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Publication number: 20130338094Abstract: The present disclosure relates to compounds of formula (I-A) using the compounds wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5?, and m are defined herein, to pharmaceutical compositions comprising the compounds, and methods of using the compounds.Type: ApplicationFiled: May 23, 2013Publication date: December 19, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Stephen CRITCHLEY, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
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Publication number: 20130338175Abstract: Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of cabazitaxel-based compounds. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the pemetrexed-based compound is achieved.Type: ApplicationFiled: December 21, 2011Publication date: December 19, 2013Applicant: Nektar TherapeuticsInventors: Lin Cheng, Jinnifer Riggs-Sauthier
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Publication number: 20130338137Abstract: The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.Type: ApplicationFiled: August 30, 2012Publication date: December 19, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Nils GRIEBENOW, Dieter LANG, Frank WUNDER, Walter HÃœBSCH, Niels LINDNER, Alexandros VAKALOPOULOS, Adrian TERSTEEGEN
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Patent number: 8609647Abstract: A compound of the following general formula [I]: wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.Type: GrantFiled: July 30, 2010Date of Patent: December 17, 2013Assignee: Japan Tobacco Inc.Inventors: Satoru Noji, Makoto Shiozaki, Tomoya Miura, Yoshinori Hara, Hiroshi Yamanaka, Katsuya Maeda, Akimi Hori, Masafumi Inoue, Yasunori Hase
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Publication number: 20130331375Abstract: There are provided compounds of the formula (I) wherein Q, R1 and R2 are defined herein. The compounds have activity as anticancer agents.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Nancy-Ellen Haynes, Johannes Hermann, Kyungjin Kim, Nathan Robert Scott, Lin Yi, Mark Zak
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Patent number: 8604043Abstract: The present invention relates to the Janus kinase (JAK) inhibitors 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]octanenitrile or 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]heptanenitrile, as well as its compositions and methods of use, which is useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, skin disorders, cancer, and other diseases.Type: GrantFiled: May 21, 2010Date of Patent: December 10, 2013Assignee: Incyte CorporationInventors: Yun-Long Li, James D. Rodgers
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Publication number: 20130324562Abstract: The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: March 1, 2012Publication date: December 5, 2013Inventors: Chad E. Bennett, Duane A. Burnett, Hongmei Li, Yonggang Chen, Troy McCracken, Monica Vicarel
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Publication number: 20130324565Abstract: The present invention relates to optionally substituted (5- or 7-oxy)-3,4-dihydro-(optionally 4-oxo, 4-thioxo or 4-imino)-1H-pyrrolo[3,4-d]pyrimidin-2(3H,6H)-ones, e.g., Compounds of Formula II-A? or II-B? as described herein, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: ApplicationFiled: May 31, 2011Publication date: December 5, 2013Applicant: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Jun Zhao
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Patent number: 8598156Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: March 23, 2011Date of Patent: December 3, 2013Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Patent number: 8592432Abstract: 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 anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-1R), and/or insulin receptor (InsR) or a combination thereof.Type: GrantFiled: April 3, 2009Date of Patent: November 26, 2013Inventors: Bei Chen, Tao Jiang, Thomas H. Marsilje, Pierre-Yves Michellys, Truc Ngoc Nguyen, Wei Pei, Baogen Wu, Zhaobo Gao, Yonghui Ge, Chen Huang, Yuncheng Li, Xuefeng Zhu
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Publication number: 20130310340Abstract: A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation.Type: ApplicationFiled: May 15, 2013Publication date: November 21, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Donald G. Payan, Esteban Masuda, Todd Kinsella
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Patent number: 8586739Abstract: Substituted bicyclic heteroaryls having the general structure: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.Type: GrantFiled: May 10, 2012Date of Patent: November 19, 2013Assignee: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian S. Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer L. Seganish, Youngsook Shin, Dawei Zhang
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Patent number: 8586505Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.Type: GrantFiled: July 15, 2010Date of Patent: November 19, 2013Assignee: SDS Biotech K. K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Ryutaro Katsuki, Tomoko Muraki
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Publication number: 20130303533Abstract: Provided herein are azolopyridine and azolopyrimidine compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 31, 2011Publication date: November 14, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Qi Chao, Michael J. Hadd, Mark W. Holladay, Martin Rowbottom
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Patent number: 8580802Abstract: The present invention relates to compounds of the following structural formula: which are useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: September 28, 2006Date of Patent: November 12, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Luc Farmer, Tiansheng Wang, Jian Wang, Randy Bethiel, Marion Wannamaker, Gabriel Martinez-Botella, John Duffy, Alexander Aronov, David Lauffer, Albert Pierce
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Publication number: 20130289037Abstract: 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: March 14, 2013Publication date: October 31, 2013Inventor: MILLENNIUM PHARMACEUTICALS, INC
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Publication number: 20130289017Abstract: Compounds of the formula (I), in which R1, R2, R2a and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: December 15, 2011Publication date: October 31, 2013Applicant: MERCK PATENT GMBHInventors: Dieter Dorsch, Margarita Wucherer-Plietker, Thomas J.J. Mueller, Eugen Merkul
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Publication number: 20130281438Abstract: The invention relates to a novel class of 2,4-diamino-6,7-dihydro-5H-pyrrolo[2,3]pyrimidine derivatives as a FAK and/or Pyk2 inhibitor, to a process for their preparation, and to a composition thereof, as well as to use of the compounds for the inhibiting FAK and/or Pyk2 and method for the treatment of a FAK and/or Pyk2 mediated disorder or disease.Type: ApplicationFiled: January 7, 2012Publication date: October 24, 2013Applicant: CENTAURUS BIOPHARMA CO., LTD.Inventors: Dengming Xiao, Liang Cheng, Xijie Liu, Yuandong Hu, Xinhe Xu, Zhihua Liu, Lipeng Zhang, Wei Wu, Shulong Wang, Yu Shen, Gen Li, Yin Wang, Sheng Zhao, Chonglong Li, Jia Tang, Honghao Yu
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Publication number: 20130274268Abstract: The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.Type: ApplicationFiled: December 29, 2011Publication date: October 17, 2013Applicant: HANMI PHARM. CO., LTDInventors: Jung Beom Son, Nam Du Kim, Young Kil Chang, Hee Cheol Kim, Ji Sook Kim, Young Hee Jung
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Publication number: 20130274220Abstract: The present invention discloses methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5?-methylthioinosine phosphorylase (MTIP) inhibitor, as well as assays for identifying such inhibitors, and compounds and pharmaceutical compositions comprising the inhibitors.Type: ApplicationFiled: November 28, 2011Publication date: October 17, 2013Applicants: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Keith Clinch, Peter Charles Tyler, Gary Brian Evans, Richard Hubert Furneaux
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Publication number: 20130266563Abstract: Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.Type: ApplicationFiled: May 17, 2013Publication date: October 10, 2013Inventors: Ganga Raju Gokaraju, Sudhakar Kasina, Venkateswarlu Somepalli, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Kiran Bhupathiraju, Trimurtulu Golakoti, Krishanu Sengupta, Venkata Krishna Raju Alluri
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Patent number: 8552014Abstract: A method for treating cancer tumors, particularly ovarian cancer tumors, is described, where fused cyclic pyrimidine having a cancer treating ability is selectively delivered to an FR expressing cancerous tumor.Type: GrantFiled: July 30, 2012Date of Patent: October 8, 2013Assignees: Duquesne University of The Holy Ghost, Wayne State UniversityInventors: Aleem Gangjee, Larry H. Matherly
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Patent number: 8551965Abstract: A compound of formula (I) wherein Ar can be one six-membered or two fused six-membered aromatic rings; R8 and R9 can be hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, or aryl; Q can be O, S or CY2, where Y may be H, alkyl or halogens; X can be O, NH, S, N-alkyl, (CHR2)m where m is 1 to 10, and CY2; Z can be O, S, NH, or N-alkyl; U? is H and U? can be H or CH2; wherein: T can be OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH2. or N3; T? and T? can be H or halogen; and W can be H or a phosphate group. Compounds show anti-viral activity, for example with respect to varicella zoster virus.Type: GrantFiled: September 24, 2010Date of Patent: October 8, 2013Assignees: University College Cardiff Consultants Limited, Rega FoundationInventors: Christopher McGuigan, Jan Balzarini
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Patent number: 8546408Abstract: Fused heteroaryl pyridyl benzenesulfonamides are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists.Type: GrantFiled: December 22, 2010Date of Patent: October 1, 2013Assignee: Chemocentryx, Inc.Inventors: Antoni Krasinski, Sreenivas Punna, Solomon Ungashe, Qiang Wang, Yibin Zeng
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Patent number: 8546407Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (Ic) or salts, tautomers or N-oxides thereof.Type: GrantFiled: October 25, 2005Date of Patent: October 1, 2013Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: Valerio Berdini, Robert George Boyle, Gordon Saxty, David Winter Walker, Steven John Woodhead, Paul Graham Wyatt, Alastair Donald, John Caldwell, Ian Collins, Tatiana Faria Da Fonseca