Plural Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/234.5)
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Patent number: 8586583Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: GrantFiled: October 2, 2012Date of Patent: November 19, 2013Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Nigel James Parr
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Publication number: 20130303516Abstract: The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.Type: ApplicationFiled: January 25, 2012Publication date: November 14, 2013Inventors: Sundeep Dugar, Dinesh Mahajan, Chandraban Rhushikesh Deokar, Peter Frank Hollinger, Kamal Kishore Kapoor
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Publication number: 20130303536Abstract: The present invention relates to compositions comprising a combination of 10-propargyl-10-deazaaminopterin and an EGFR Kinase inhibitor, including erlotinib, for treatment of non-small cell lung cancer, and methods of treatment for non-small cell lung cancer in a patient in need thereof comprising administering for combination of 10-propargyl-10-deazaaminopterin and an EGFR Kinase inhibitor, including erlotinib, for treatment of non-small cell lung cancer.Type: ApplicationFiled: July 17, 2013Publication date: November 14, 2013Inventor: Gijsbertus J. Pronk
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Publication number: 20130303534Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: March 5, 2013Publication date: November 14, 2013Inventors: PRABHA N. IBRAHIM, DEAN R. ARTIS, RYAN BREMER, GASTON HABETS, SHUMEYE MAMO, MARIKA NESPI, CHAO ZHANG, JIAZHONG ZHANG, YONG-LIANG ZHU, REBECCA ZUCKERMAN, BRIAN WEST, YOSHISA SUZUKI, JIANMING TSAI, KLAUS-PETER HIRTH, GIDEON BOLLAG, WAYNE SPEVAK, HANNA CHO, SAMUEL J. GILLETTE, GUOXIAN WU, HONGYAO ZHU, SHENGHUA SHI
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Publication number: 20130302337Abstract: This disclosure relates to methods and compositions useful for treating Alzheimer's disease. In particular, the disclosure relates to pharmaceutical compositions containing an EGFR-inhibitory compound suitable for administration to treat Alzheimer's disease, as well as to related therapeutic methods. In addition, this disclosure relates to screening methods for identifying compounds useful for treating Alzheimer's disease based on the ability to inhibit the activity of EGFR.Type: ApplicationFiled: July 24, 2013Publication date: November 14, 2013Inventors: Yi Zhong, Hsueh-cheng Chiang, Lei Wang
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Publication number: 20130303535Abstract: The invention provides a compound for the treatment or prophylaxis of pathology involving SNS, specifically diseases such as neuropathic pain, nociceptive pain, dysuria, multiple sclerosis and the like.Type: ApplicationFiled: May 15, 2013Publication date: November 14, 2013Inventors: Katsunori TSUBOI, Yusuke YAMAI, Hitoshi WATANABE, Hironori KINOSHITA
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Publication number: 20130303461Abstract: The technology described herein is directed to methods of determining oligonucleotide sequences, e.g. by enriching target sequences prior to sequencing the sequences.Type: ApplicationFiled: March 11, 2013Publication date: November 14, 2013Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Anthony John Iafrate, Long Phi Le, Zongli Zheng
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Publication number: 20130296319Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.Type: ApplicationFiled: July 11, 2013Publication date: November 7, 2013Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
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PYRROLO[2,3-b]PYRIDIN-4-YL-AMINES AND PYRROLO[2,3-b]PYRIMIDIN-5-YL-AMINES AS JANUS KINASE INHIBITORS
Publication number: 20130296299Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.Type: ApplicationFiled: May 8, 2013Publication date: November 7, 2013Inventors: James D. Rodgers, Haisheng Wang, Andrew P. Combs, Richard B. Sparks -
Publication number: 20130295049Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: October 30, 2012Publication date: November 7, 2013Applicant: ENANTA PHARMACEUTICALS, INCInventor: ENANTA PHARMACEUTICALS, INC
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Patent number: 8575163Abstract: Pyrrolopyridinylpyrimidin-2-ylamine derivatives of the formula (I), in which R1-R6 and R1 have the meanings indicated in claim 1, are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: GrantFiled: November 12, 2010Date of Patent: November 5, 2013Assignee: Merck Patent GmbHInventors: Margarita Wucherer-Plietker, Christina Esdar, Brian Hodous
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Patent number: 8575162Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: GrantFiled: April 28, 2010Date of Patent: November 5, 2013Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr
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Publication number: 20130289016Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.Type: ApplicationFiled: June 10, 2013Publication date: October 31, 2013Inventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
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Publication number: 20130289032Abstract: The present invention relates to particular esters of bendamustine and related compounds, and medical uses thereof.Type: ApplicationFiled: April 25, 2013Publication date: October 31, 2013Inventors: Helmut SCHICKANEDER, Armin Buschauer, Guenther Bernhardt, Christian Schickaneder, Michael Limmert, Stefan Huber
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Patent number: 8569504Abstract: For the prevention and/or treatment of chymase-mediated diseases such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like, a drug is provided having as an active ingredient a compound having extremely strong chymase inhibitory activity, high safety, and high metabolic stability. The compound represented by the formula (I): wherein all symbols have the same meanings as in the description, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a pharmaceutical ingredient having chymase inhibitory activity for preventing and/or treating of chymase-mediated disease, such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like.Type: GrantFiled: June 16, 2010Date of Patent: October 29, 2013Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Jun Takeuchi, Takayuki Inukai, Masaru Sakai
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Patent number: 8569511Abstract: In one aspect, the invention relates to substituted 3-(1H-benzo[d]imidazol-2-yl)-1H-indazole analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the PDK1 kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions for treating disorders associated with dysfunction of the PDK1 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: GrantFiled: March 31, 2012Date of Patent: October 29, 2013Assignee: University of Utah Research FoundationInventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
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Patent number: 8569297Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of novel 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1 and CX3CR1, and to their use in a method for treating or preventing diseases based on the expression of MCP-1 and CX3CR1.Type: GrantFiled: September 14, 2012Date of Patent: October 29, 2013Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Angelo Guglielmotti, Guido Furlotti, Giorgina Mangano, Nicola Cazzolla
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Publication number: 20130281449Abstract: The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in pharmaceutically acceptable salt form, to their preparation, to their medical use and to medicaments comprising them.Type: ApplicationFiled: January 11, 2012Publication date: October 24, 2013Applicant: NOVARTIS AGInventors: Konstanze Hurth, Rainer Martin Lueoend, Rainer Machauer, Ulf Neumann, Heinrich Rueeger, Michael Schaefer, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
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Publication number: 20130281448Abstract: Provided herein are small molecule compounds for the treatment of inflammatory conditions, and pharmaceutical compositions and methods relating thereto. For example, provided herein are compositions comprising small molecule compounds for the treatment of conditions such as multiple sclerosis, type 2 diabetes, psoriasis, rheumatoid arthritis, Hashimoto's thyroiditis, and Crohn's disease. In some embodiments, the pharmaceutical composition and methods described herein pertain to small molecule compounds previously known for the treatment of another condition, such as non-small-cell lung cancer (NSCLC).Type: ApplicationFiled: April 18, 2013Publication date: October 24, 2013Inventor: Marvin B. Brooks
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Publication number: 20130281397Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Applicant: RVX Therapeutics Inc.Inventors: Kevin G. McLure, Peter Ronald Young
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Publication number: 20130274259Abstract: Compounds, compositions and methods useful for treatment of Flt3-mediated diseases or conditions are provided herewith. Also provided herewith are methods for modulating the receptor protein tyrosine like kinase 3(Flt3).Type: ApplicationFiled: March 11, 2013Publication date: October 17, 2013Inventors: Chao Zhang, Gideon Bollag, Gaston Habets, Jiazhong Zhang, Prabha N. Ibrahim, Guoxian Wu
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Publication number: 20130274241Abstract: Compounds of Formula (I) are used for the treatment of inflammation and autoimmune disorders.Type: ApplicationFiled: December 16, 2011Publication date: October 17, 2013Applicant: MERCK SERONO S.A. - INTELLECTUAL PROPERTYInventors: Catherine Jorand-Lebrun, Stefano Crosignani, Jerome Dorbais, Tania Grippi-Vallotton, Adeline Pretre
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Publication number: 20130274252Abstract: The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.Type: ApplicationFiled: November 2, 2012Publication date: October 17, 2013Inventors: Anjali Pandey, Robert M. Scarborough, Kenji Matsuno, Michio Ichimura, Yuji Nomoto, Shinichi Ide, Eiji Tsukuda, Junko Sasaki, Shoji Oda
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Patent number: 8557797Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; R1 is C1-C6 alkyl, C3-C6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R3 and R4 are independently H or C1-C6 alkyl, or R3 and R4 taken together with the nitrogen to which they are attached form a 6-membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is —O— or —S(O)p— wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C3-C6 divalent cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R2NHC(?O)W—; W is a bond, —NH— or —C(RA)(RB), wherein RA and RB are independently H, methyl, ethyl, amino, hydroxyl or halo; and R2 is a radical as dType: GrantFiled: February 16, 2010Date of Patent: October 15, 2013Assignee: Chiesi Farmaceutici S.p.A.Inventors: Harry Finch, John Montana, Monique Bodil Van Niel, Chi-Kit Woo, Jamie Knight, Bohdan Waszkowycz
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Publication number: 20130267493Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.Type: ApplicationFiled: March 15, 2013Publication date: October 10, 2013Applicant: PFIZER INC.Inventors: Samit Bhattacharya, Kimberly Cameron, Matthew Dowling, Dilinie Fernando, David Ebner, Kevin Filipski, Daniel Kung, Esther Lee, Aaron Smith, Meihua Tu
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Publication number: 20130267515Abstract: A method for treating an ATP analog-induced side effect in a subject comprises administering an effective amount of an adenosine receptor antagonist to the subject. A method for treating cancer in a subject comprises administering a nucleobase and/or nucleoside prior to administering an ATP analog.Type: ApplicationFiled: October 26, 2011Publication date: October 10, 2013Applicant: Alberta Health ServicesInventors: Michael Bruce Sawyer, Vijayalakshmi Damaraju
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Publication number: 20130267514Abstract: 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: March 14, 2013Publication date: October 10, 2013Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert Mantei, Todd M. Hansen
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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: 8551990Abstract: The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.Type: GrantFiled: September 14, 2012Date of Patent: October 8, 2013Assignee: Bionomics LimitedInventors: Jonathan Bayldon Baell, Brad Sleebs, Bernard Luke Flynn, Ian Philip Street, Nurul Quazi, Chinh Thien Bui
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Patent number: 8551989Abstract: This invention relates to novel 4-(indazolyl)-1,4-dihydropyridine of the following formula (I) derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.Type: GrantFiled: May 29, 2009Date of Patent: October 8, 2013Assignee: Bayer Intellectual Property GmbHInventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch, Karen Engel
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Patent number: 8551988Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).Type: GrantFiled: June 14, 2010Date of Patent: October 8, 2013Assignee: Mei Pharma, Inc.Inventors: DiZhong Chen, Hong Yan Song, Eric T. Sun, Niefang Yu, Yong Zou
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Publication number: 20130259830Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.Type: ApplicationFiled: June 24, 2011Publication date: October 3, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Timothy Barden, Colleen Hudson, James Jia, Charles Kim, Regina Graul, Ara Mermerian, Joel Moore, Kevin Sprott, Yueh-tyng Chien
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Publication number: 20130261102Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: May 24, 2011Publication date: October 3, 2013Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
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Publication number: 20130261117Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: April 19, 2013Publication date: October 3, 2013Inventors: Prabha N. Ibrahim, Chao Zhang, Jiazhong Zhang, Jianming Tsai, Klaus-Peter Hirth, Gideon Bollag, Wayne Spevak
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Patent number: 8546440Abstract: The present invention is concerned with novel substituted bicyclic imidazole derivatives of Formula (I) wherein R0, R1, R3, R4, X, A1, A2, A3, A4, Y1, Y2 and Y3 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said novel compound as an active ingredient as well as the use of said compounds as a medicament.Type: GrantFiled: December 16, 2009Date of Patent: October 1, 2013Assignee: Janssen Pharmaceuticals, Inc.Inventors: Henricus Jacobus Maria Gijsen, Gregor James MacDonald, François Paul Bischoff, Gary John Tresadern, Andrés Avelino Trabanco-Suárez, Sven Franciscus Anna Van Brandt, Didier Jean-Claude Berthelot
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Patent number: 8546388Abstract: The invention relates to compounds of formulae I(a)-I(d): and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formulae I(a)-I(d) or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formulae I(a)-I(d) or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: October 22, 2009Date of Patent: October 1, 2013Assignee: Purdue Pharma L.P.Inventors: Donald J. Kyle, Laykea Tafesse
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Patent number: 8546389Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:Type: GrantFiled: October 20, 2011Date of Patent: October 1, 2013Assignee: Biota Scientific Management Pty Ltd.Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
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Publication number: 20130251702Abstract: Methods for screening compounds for treating sepsis are disclosed. The present methods and compositions are targeting NOD2 mediated signaling pathway and the agents identified by the present methods are qualified as drug candidates for clinical development. Further Methods and composition for treating sepsis are disclosed.Type: ApplicationFiled: March 21, 2013Publication date: September 26, 2013Applicant: SNU R&DB FOUNDATIONInventors: Doo Hyun CHUNG, Sae Jin OH, Ji Hyung KIM
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Publication number: 20130252954Abstract: Provision of crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride which has a superior rennin inhibitory activity and is useful as a prophylactic or therapeutic agent for hypertension and various organ disorders caused by hypertension, and the like. Crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride having an X-ray powder diffraction pattern showing characteristic peaks at interplanar spacings (d) of around 26.43±0.2, 7.62±0.2 and 4.32±0.2 angstroms.Type: ApplicationFiled: June 15, 2011Publication date: September 26, 2013Inventor: Masato KITAYAMA
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Patent number: 8541584Abstract: Compounds of the formula (I), in which R1, R2 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 tumors.Type: GrantFiled: April 8, 2010Date of Patent: September 24, 2013Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Margarita Wucherer-Plietker, Thomas J. J. Mueller, Eugen Merkul
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Patent number: 8541411Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazoles compounds for treating cancer.Type: GrantFiled: March 13, 2013Date of Patent: September 24, 2013Assignee: GlaxoSmithKline LLCInventors: Junya Qu, Ralph A. Rivero, Robert Sanchez, Rosanna Tedesco
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Publication number: 20130245015Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Inventors: YUJIA DAI, STEVEN K. DAVIDSEN, ANNA M. ERICSSON, KRESNA HARTANDI, ZHIQIN JI, MICHAEL R. MICHAELIDES
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Publication number: 20130245014Abstract: Provided herein are quinazoline 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: October 4, 2012Publication date: September 19, 2013Applicant: Ambit Biosciences Corp.Inventors: Sunny Abraham, Qi Chao, Michael J. Hadd, Mark W. Holladay, Liu Gang, Eduardo Setti
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Patent number: 8536169Abstract: The invention is directed to certain novel compounds directed to 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: September 17, 2013Assignee: Glaxo Group LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Joelle Le, Nigel James Parr, Timothy John Ritchie, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Patent number: 8536168Abstract: The present disclosure relates to compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders; specifically relating to compounds of formula I:Type: GrantFiled: March 13, 2008Date of Patent: September 17, 2013Assignee: Novartis AGInventors: Miao Dai, Feng He, Rishi Kumar Jain, Rajesh Karki, Joseph Kelleher, III, John Lei, Luis Llamas, Michael A. Mcewan, Karen Miller-Moslin, Lawrence Bias Perez, Stefan Peukert, Naeem Yusuff
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Publication number: 20130237522Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: April 19, 2013Publication date: September 12, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Kai GERLACH, Roland PFAU, Norbert HAUEL, Iris KAUFFMANN-HEFNER, Georg DAHMANN, Herbert NAR, Sandra HANDSCHUH, Wolfgang WIENEN, Annette SCHULER-METZ
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Publication number: 20130237538Abstract: The present invention relates to compounds of formulae I and II wherein the variables are as defined herein. These compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: March 12, 2013Publication date: September 12, 2013Applicant: ALLERGAN, INC.Inventors: Clarence E. Hull, III, Thomas C. Malone
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Publication number: 20130237516Abstract: The present invention relates to compounds 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: ApplicationFiled: April 25, 2013Publication date: September 12, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Luc Farmer, Gabriel Martinez-Botella, Albert Pierce, Francesco Salituro, Jian Wang, Wannamaker W. Wannamaker, Tiansheng Wang
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Publication number: 20130237518Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).Type: ApplicationFiled: October 24, 2011Publication date: September 12, 2013Inventors: Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, JR.
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Publication number: 20130236473Abstract: A major object of the present invention is to provide a novel therapeutic or prophylactic agent for at least one disease or symptom selected from the group consisting of autoimmune diseases, inflammatory diseases, allergic diseases, and symptoms accompanying organ transplants; the therapeutic or prophylactic agent artificially controls the activity of IL-6 amplifier, thus controlling immune reactions in living organisms. Another object of the present invention is to provide an immunosuppressant, an inflammatory cytokine production inhibitor, and an IL-6 amplifier inhibitor. The compound that inhibits expression of the function of a protein belonging to ErbB1 pathway provided as means for achieving the object is capable of suppressing the activity of IL-6 amplifier, thereby reducing production of inflammatory cytokine such as IL-6.Type: ApplicationFiled: September 14, 2011Publication date: September 12, 2013Applicant: OSAKA UNIVERSITYInventors: Toshio Hirano, Masaaki Murakami