Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/234.2)
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Publication number: 20150087627Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject.Type: ApplicationFiled: April 15, 2014Publication date: March 26, 2015Applicant: Intellikine LLCInventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
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Publication number: 20150087632Abstract: The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: wherein X, Y, Z, L, A, R5, n and m are defined above, 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: December 1, 2014Publication date: March 26, 2015Applicant: INCYTE CORPORATIONInventors: James D. Rodgers, Stacey Shepard, Wenyu Zhu, Lixin Shao, Joseph Glenn
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Publication number: 20150087644Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
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Patent number: 8987280Abstract: Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. 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: GrantFiled: January 29, 2009Date of Patent: March 24, 2015Assignees: Genentech, Inc., F. Hoffmann-La Roche AGInventors: Jennafer Dotson, Tim Heffron, Alan Olivero, Daniel P. Sutherlin, Shumei Wang, Bing-Yan Zhu, Irina Chuckowree, Adrian Folkes, Nan Chi Wan
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NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
Publication number: 20150080391Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, R4, L, and X are as defined herein. The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and their use in the prophylaxis and/or treatment of inflammatory conditions, type 2 diabetes, neurological and/or neurodegenerative diseases, autoimmune diseases, proliferative diseases (in particular metastatic diseases, and/or cancer), abnormal angiogenesis associated diseases, degradation of cartilage, and/or disruption of cartilage homeostasis, in particular in the prophylaxis and/or treatment of cancer. The present invention also discloses methods of treatment using the same compounds, for the prophylaxis and/or treatment of said diseases by administering the compound of the invention.Type: ApplicationFiled: August 18, 2014Publication date: March 19, 2015Inventors: Laurent Raymond Maurice SANIÈRE, Jacques HUCK, Graeme James DYKES, Benoit Antoine SCHMITT, Javier BLANC, Anna Sara BUTLER, Florence Marie-Emilie BONNATERRE, Stéphane Nicolas Alain BEAUMONT -
Publication number: 20150072982Abstract: Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compounds. Examples of an orthomyxovirus viral infection include an influenza infection.Type: ApplicationFiled: September 10, 2014Publication date: March 12, 2015Inventors: Robert Than Hendricks, Leonid Beigelman, David Bernard Smith, Antitsa Dimitrova Stoycheva
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Publication number: 20150072981Abstract: 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: August 7, 2014Publication date: March 12, 2015Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Patent number: 8975250Abstract: The present invention relates to 5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives having Formula (I) as defined herein, their preparation and their therapeutic use.Type: GrantFiled: July 9, 2012Date of Patent: March 10, 2015Assignee: SANOFIInventors: Philippe Beauverger, Guillaume Begis, Sandrine Biscarrat, Olivier Duclos, Gary McCort
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Publication number: 20150065483Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Publication number: 20150064196Abstract: The present disclosure provides hetero-bicyclic compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, hydrates, N-oxides, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by Bruton's tyrosine kinase (Btk) activity, The disclosure also relates to the process of preparation of compounds of Formula (I). These compounds are useful in the treatment, prevention, prophylaxis, management, or adjunct treatment of all medical conditions related to inhibition of Bruton's tyrosine kinase (Btk), such as inflammatory and/or autoimmune disorder, cell proliferation, rheumatoid arthritis, psoriasis, psoriatic arthritis, transplant rejection, graft-versus-host disease, multiple sclerosis, inflammatory bowel disease, allergic diseases, asthma, type 1 diabetes, myasthenia gravis, hematopoetic disfunction, B-cell malignancies, systemic lupus, erythematosus or other disorders.Type: ApplicationFiled: October 8, 2014Publication date: March 5, 2015Inventors: Mahesh Thakkar, Summon Koul, Debnath Bhuniya, Kasim Mookhtiar, Santosh Kurhade, Yogesh Munot, Tanaji Mengawade, Bheemashankar A. Kulkarni
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Publication number: 20150065501Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.Type: ApplicationFiled: March 27, 2013Publication date: March 5, 2015Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
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Publication number: 20150065495Abstract: The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.Type: ApplicationFiled: August 28, 2014Publication date: March 5, 2015Applicant: UNIVERSITY OF UTAHInventors: Hariprasad Vankayalapati, Sunil Sharma, Venkataswamy Sorna
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Patent number: 8969341Abstract: 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: GrantFiled: November 28, 2012Date of Patent: March 3, 2015Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Patent number: 8962619Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: November 8, 2013Date of Patent: February 24, 2015Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Kenichi Yoshida, Takanori Yamazaki, Takahiro Kitamura, Takeshi Isoyama
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Patent number: 8962620Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: November 4, 2013Date of Patent: February 24, 2015Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Publication number: 20150051208Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3 and X1 through X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: ApplicationFiled: August 11, 2014Publication date: February 19, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald ENGELHARDT, Laetitia MARTIN, Christian SMETHURST
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Patent number: 8957065Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.Type: GrantFiled: June 20, 2011Date of Patent: February 17, 2015Assignee: Hanmi Science Co., LtdInventors: Mi Young Cha, Seok Jong Kang, Mi Ra Kim, Ju Yeon Lee, Ji Young Jeon, Myoung Gi Jo, Eun Joo Kwak, Kwang Ok Lee, Tae Hee Ha, Kwee Hyun Suh, Maeng Sup Kim
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Publication number: 20150045349Abstract: The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: February 19, 2013Publication date: February 12, 2015Inventors: Hiroyuki Nagamiya, Masato Yoshida, Masaki Seto, Shogo Marui, Tsuneo Oda, Yuji Ishichi, Hideo Suzuki, Tomokazu Kusumoto, Takatoshi Yogo, Chul Yun Rhim, Cheolhwan Yoon, Gil Nam Lee, Hyun Bin Kang, Kwang Ok Kim, Hye Sun Jeon
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Publication number: 20150045359Abstract: The present invention relates to compounds of formula wherein R1 and R2 are as described herein. Compounds of the invention are useful in the treatment and/or prophylaxis of diseases associated with TAAR modulation.Type: ApplicationFiled: January 8, 2013Publication date: February 12, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Guido Galley, Annick Goergler, Roger Norcross, Philippe Pflieger
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Publication number: 20150045360Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:Type: ApplicationFiled: August 21, 2014Publication date: February 12, 2015Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Publication number: 20150045324Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Applicant: HANMI SCIENCE CO., LTDInventors: Mi Young CHA, Seok Jong KANG, Mi Ra KIM, Ju Yeon LEE, Ji Young JEON, Myoung Gi JO, Eun Joo KWAK, Kwang Ok LEE, Tae Hee HA, Kwee Hyun SUH, Maeng Sup KIM
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Publication number: 20150045361Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: October 22, 2014Publication date: February 12, 2015Inventors: 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: 8952058Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: GrantFiled: October 12, 2012Date of Patent: February 10, 2015Assignee: Ambit Biosciences CorporationInventors: Michael J. Hadd, Michael D. Hocker, Mark W. Holladay, Gang Liu, Martin W. Rowbottom, Shimin Xu
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Publication number: 20150038488Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.Type: ApplicationFiled: July 31, 2014Publication date: February 5, 2015Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
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Publication number: 20150038494Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.Type: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&DInventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
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Publication number: 20150031693Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of Fragile X syndrome.Type: ApplicationFiled: November 2, 2012Publication date: January 29, 2015Applicant: AFRAXIS HOLDINGS, INC.Inventors: John C. Mckew, Wenwei Huang, David Campbell, Sergio G. Durön, Mark Behnke, Min Shen
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Publication number: 20150031674Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5, Ra, Rb, Rc, Rd, Re, n, r, s and t are as defined herein and which compounds are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: ApplicationFiled: July 25, 2014Publication date: January 29, 2015Applicant: GENENTECH, INC.Inventors: Joachim Rudolph, Lewis J. Gazzard, James J. Crawford, Chudi Ndubaku, Joy Drobnick, Wendy Lee
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Publication number: 20150031694Abstract: The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.Type: ApplicationFiled: March 21, 2013Publication date: January 29, 2015Inventors: Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
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Publication number: 20150031672Abstract: 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 PI3 kinase activity, are described herein.Type: ApplicationFiled: October 10, 2014Publication date: January 29, 2015Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
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Publication number: 20150025070Abstract: The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.Type: ApplicationFiled: July 13, 2012Publication date: January 22, 2015Applicant: Novartis AGInventors: Atwood Kim Cheung, Donovan Noel Chin, Jianmei Fan, Karen Marie Miller-Moslin, Michael David Shultz, Troy D. Smith, Ronald Charles Tomlinson, Bakary-Barry Toure, Michael Scott Visser
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Publication number: 20150018336Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: ApplicationFiled: December 28, 2012Publication date: January 15, 2015Inventors: Wei Chen, David J. Loury
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Publication number: 20150018350Abstract: The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: May 15, 2014Publication date: January 15, 2015Inventors: David G. Bourke, Christopher J. Burns, Anthony N. Cuzzupe, John T. Feutrill, Marcel R. Kling, Tracy L. Nero
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Publication number: 20150018309Abstract: In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6-carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: February 23, 2013Publication date: January 15, 2015Inventors: Craig W Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, James C. Tarr, James M. Salovich
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Publication number: 20150017651Abstract: Methods and composition for tumor therapy, especially esophageal adenocarcinoma (EAC), are described. For example, in certain aspects methods for determining Hedgehog and mTOR signaling pathway status to select patients for administering a combination therapy of Hedgehog and mTOR signaling inhibitors are described. Furthermore, the invention provides compositions that involve testing kits for determining signaling status.Type: ApplicationFiled: January 14, 2013Publication date: January 15, 2015Applicant: Board of Regents, The University of Texas SystemInventors: Mien-Chie Hung, Yan Wang, Jaffer Ajani
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Publication number: 20150018337Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 29, 2014Publication date: January 15, 2015Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Publication number: 20150018349Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: March 27, 2014Publication date: January 15, 2015Applicant: University of Utah Research FoundationInventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
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Patent number: 8933073Abstract: The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with antiinflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.Type: GrantFiled: January 24, 2014Date of Patent: January 13, 2015Assignee: Basilea Pharmaceutica AGInventors: Johannes Laurenz Kellenberger, Jürg Dreier
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Publication number: 20150011545Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.Type: ApplicationFiled: July 15, 2014Publication date: January 8, 2015Applicant: AstraZeneca ABInventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle Laurae LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
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Publication number: 20150011546Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.Type: ApplicationFiled: February 11, 2013Publication date: January 8, 2015Inventors: Brian K. Albrecht, James Edmund Audia, Andrew S. Cook, Les A. Dakin, Martin Duplessis, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
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Publication number: 20150011547Abstract: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.Type: ApplicationFiled: September 2, 2014Publication date: January 8, 2015Applicant: ASANA BIOSCIENCES, LLCInventors: Roger Astbury Smith, Scott Kevin Thompson, Subramanya Hosahalli, Mallesham Bejugam, Srinivas Nanduri, Sunil Kumar Panigrahi, Natarajan Mahalingam
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Patent number: 8927545Abstract: EphB3 kinase inhibitor compounds, including certain pyrazolo[1,5-a]pyridine and imidazo[1,2-a]pyridine compounds, inhibit EphB3 kinase. The EphB3 kinase inhibitor compounds can have greater potency for the inhibition of EphB3 kinase than general kinase inhibitors. Pharmaceutical compositions, such as neuroprotective agents, comprising the EphB3 kinase inhibitor compounds are also provided. The EphB3 kinase inhibitor compounds and pharmaceutical compositions are useful, for example, to provide neuroprotection and/or repair of neuronal tissue damaged during an ischemic event, such as a stroke.Type: GrantFiled: March 30, 2010Date of Patent: January 6, 2015Assignees: Duke University, The Brigham and Women's Hospital, Inc.Inventors: Lixin Qiao, Marcie Glicksman, Thomas Gainer, Donald C. Lo, Ross L. Stein, Sungwoon Choi, Gregory D. Cuny
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Patent number: 8921336Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.Type: GrantFiled: November 28, 2008Date of Patent: December 30, 2014Assignees: Dana-Farber Cancer Institute, Inc., The Scripps Research InstituteInventors: Nathanael Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang
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Publication number: 20140378450Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: Novartis AGInventors: Giorgio CARAVATTI, Robin Alec FAIRHURST, Pascal FURET, Clive MCCARTHY, Heinrich RUEEGER, Frank Hans SEILER, Frédéric STAUFFER
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Publication number: 20140378431Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.Type: ApplicationFiled: December 21, 2012Publication date: December 25, 2014Applicant: MERCK PATENT GMBHInventors: Dieter Dorsch, Guenter Hoelzemann, Kai Schiemann, Ansgar Wegener
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Publication number: 20140378452Abstract: Treatment of neurodegenerative diseases is achieved using small molecule purine scaffold compounds that inhibit Hsp90 and that possess the ability to cross the blood-brain barrier or are other wise delivered to the brain.Type: ApplicationFiled: September 10, 2014Publication date: December 25, 2014Inventor: Gabriela Chiosis
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Publication number: 20140378451Abstract: The present invention relates to cannabinoid-2-receptor (CB2R) agonist compounds. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them and to their use as therapeutic agents for the treatment and/or prevention of diseases or conditions in which CB2R stimulation is beneficial (especially inflammatory conditions).Type: ApplicationFiled: September 19, 2012Publication date: December 25, 2014Inventors: Ivy Christou, Rebecca Lillian Cross, Matteo Gianella-Borradori, David Robert Greaves, Angela Jane Russell, Graham Michael Wynne
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Publication number: 20140371219Abstract: Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases.Type: ApplicationFiled: December 27, 2012Publication date: December 18, 2014Applicant: HANMI PHARM. CO., LTDInventors: In Hwan Bae, Jung Beom Son, Sang Mi Han, Eun Joo Kwak, Ho Seok Kim, Ji Young Song, Eun Young Byun, Seung Ah Jun, Young Gil Ahn, Kwee Hyun Suh
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Publication number: 20140371203Abstract: The present invention provides compounds of formula (I): (Formula (I); wherein A, R1, R2, R3I, V, X, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof.Type: ApplicationFiled: November 15, 2012Publication date: December 18, 2014Inventors: David Madge, Fiona Chan, Derek Edward John, Simon D. Edwards, Richard Blunt, Basil Hartzoulakis, Lindsay Brown
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Patent number: 8912178Abstract: The 4-urea-phenyl substituted 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine derivatives are potent and selective inhibitors of mTOR kinase and are useful in treating disorders related to abnormal mTOR activities such as cancer, immune disorders, cardiovascular disease, ocular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.Type: GrantFiled: May 18, 2011Date of Patent: December 16, 2014Assignee: Xcovery Holdings Company, LLCInventor: Congxin Liang
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Patent number: 8912179Abstract: The present invention relates to heterocyclyl compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors, for example cognitive disorders, sleep disorders, obesity and pain.Type: GrantFiled: November 15, 2010Date of Patent: December 16, 2014Assignee: Suven Life Sciences LimitedInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Rambabu Namala, Adi Reddy Dwarampudi, Laxman Kota, Murlimohan Gampa, Padmavathi Kodru, Taraka Naga Vinaykumar Tiriveedhi, Vishwottam Nagaraj Kandikere, Nageshwara Rao Muddana, Ramanatha Shrikantha Saralaya, Pradeep Jayarajan, Dhanalakshmi Shanmuganathan, Ishtiyaque Ahmad, Venkateswarlu Jasti