Four Or More Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/118)
-
Publication number: 20130303521Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: October 26, 2012Publication date: November 14, 2013Applicant: HYDRA BIOSCIENCES, INCInventor: HYDRA BIOSCIENCES, INC
-
Publication number: 20130296298Abstract: The present invention provides novel LRRK2 kinase inhibitors and methods of treating disease states using these inhibitors.Type: ApplicationFiled: May 2, 2013Publication date: November 7, 2013Applicants: THE UAB RESEARCH FOUNDATION, Southern Research InstituteInventors: Robert A. Galemmo, JR., Andrew B. West, Joseph A. Maddry, Subramaniam Ananthan, Ashish Kumar Pathak, Jacob Valiyaveettil
-
Publication number: 20130289271Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: ApplicationFiled: June 26, 2013Publication date: October 31, 2013Applicant: SIGNAL PHARMACEUTICALS, LLCInventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella I. Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Lida Tehrani, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Weiming Xu, Loui Madakamutil, Kimberly Elizabeth Fultz, Rama Narla, Sabita Sankar, Jan Elsner
-
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
-
Publication number: 20130252936Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.Type: ApplicationFiled: March 8, 2013Publication date: September 26, 2013Applicant: Usher III InitiativeInventors: Roland Werner BÜRLI, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E. Harte
-
Publication number: 20130245254Abstract: Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.Type: ApplicationFiled: April 30, 2013Publication date: September 19, 2013Applicant: SIGNAL PHARMACEUTICALS, LLCInventors: Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Gingsee Lee, Garrick Packard, Jingjing Zhao, Patrick Anthony Jokiel, Deborah Mortensen, Jennifer Riggs, Juan Antonio Gamboa, Marie Georges Beauchamps, Matthew Michael Kreilein, Mohit Atul Kothare, Sophie Perrin-Ninkovic, Philip Pye, William Wei-Hwa Leong, Jan Elsner, Anusuya Choudhury
-
Publication number: 20130225552Abstract: Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.Type: ApplicationFiled: February 28, 2013Publication date: August 29, 2013Applicant: AMGEN INC.Inventor: Amgen Inc.
-
Publication number: 20130225568Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis.Type: ApplicationFiled: July 29, 2011Publication date: August 29, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Lars Burgdorf, Melanie Schultz, Carl Deutsch, Horacio Comas, Dominique Swinnen, Vincent Pomel, Pascale Gaillard, Brian Hodous
-
Publication number: 20130225564Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: ApplicationFiled: March 18, 2013Publication date: August 29, 2013Applicant: Signal Pharmaceuticals, LLCInventor: Signal Pharmaceuticals, LLC
-
Publication number: 20130209543Abstract: The present invention provides for methods and pharmaceutical compositions comprising inhibitors of mTorC1 and/or mTorC2. In some aspects, the invention provides for treatment regimens resulting in enhanced treatment efficacy and better tolerability.Type: ApplicationFiled: November 21, 2012Publication date: August 15, 2013Applicant: Intellikine LLCInventor: Intellikine LLC
-
Patent number: 8507492Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: GrantFiled: November 14, 2011Date of Patent: August 13, 2013Assignee: Signal Pharmaceuticals, LLCInventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Lida Tehrani, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Weiming Xu, Loui Madakamutil, Kimberly Fultz, Rama K. Narla, Sabita Sankar, Jan Elsner
-
Publication number: 20130203986Abstract: Arylamino purine derivatives represented by formula I and their preparation method are disclosed, wherein each substituent is defined as in the description. The derivatives have an inhibitory effect on non-small cell lung cancer with deletion mutation of exon 19 or L858R point mutation of exon 21 in epidermal growth factor receptor (EGFR).Type: ApplicationFiled: December 23, 2010Publication date: August 8, 2013Applicants: SI Chuaan University, CSPC Zhongqi Pharmaceutical Technology (Shijazhuan Co., Ltd.Inventors: Shengyong Yang, Yuquan Wei
-
Publication number: 20130203755Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.Type: ApplicationFiled: May 24, 2011Publication date: August 8, 2013Applicant: UNIVERSITY OF ROCHESTERInventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Torsten Wiemann, Satheesh Babu Ravula, Colin J. Loweth
-
Patent number: 8501946Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.Type: GrantFiled: April 28, 2010Date of Patent: August 6, 2013Assignee: Glaxo Group LimitedInventors: David Kenneth Dean, Jorge Munoz-Muriedas, Mairi Sime, Jon Graham Anthony Steadman, Rachel Elizabeth Anne Thewlis, Giancarlo Trani, Daryl Simon Walter
-
Publication number: 20130197220Abstract: The present invention provides a useful morpholino nucleic acid derivative for synthesizing a morpholino nucleic acid oligomer. The present invention provides a compound represented by the following general formula (1) or a salt thereof. Here, R1 represents hydrogen, trityl and so on. R2 represents an amide or an imine. R3 represents a hydroxy group which may be protected by trialkylsilyl and so on, or a group represented by the following general formula (5): (wherein X represents O or S, Y represents dialkylamino or alkoxy, and Z represents chlorine).Type: ApplicationFiled: September 29, 2011Publication date: August 1, 2013Applicant: NIPPON SHINYAKU CO., LTD.Inventor: Toshihiro Ueda
-
Publication number: 20130196989Abstract: The present invention provides compounds, compositions and methods for dedifferentiating lineage committed mammalian cells into stem cells. The present invention also provides methods of inducing dedifferentiation of lineage committed mammalian cells into stem cells, which can be further differentiated into various lineage committed cells. Methods of identifying additional compounds useful for inducing dedifferentiation of lineage committed cells into stem cells are also provided.Type: ApplicationFiled: August 24, 2012Publication date: August 1, 2013Applicant: The Scripps Research InstituteInventors: Shuibing Chen, Sheng Ding, Peter G. Schultz
-
Publication number: 20130190292Abstract: The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.Type: ApplicationFiled: August 12, 2011Publication date: July 25, 2013Applicant: CELLZOME LIMITEDInventors: Kathryn Bell, Nelly Piton, Claudio Dagostin, Cyrille Boussard, Andrew Ratcliffe, Nigel Ramsden
-
Publication number: 20130184274Abstract: The present invention relates to chemical compounds of formula (I) and methods for their use and preparation. In particular, the invention relates to substituted pyrazolo[3,4-d]pyrimidine based compounds which can be used in treating proliferative disorders, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.Type: ApplicationFiled: July 8, 2011Publication date: July 18, 2013Inventors: Guillaume Laurent Lessene, Jonathan Bayldon Baell, Antony Wilks Burgess, Hiroshi Maruta
-
Publication number: 20130184240Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.Type: ApplicationFiled: September 8, 2011Publication date: July 18, 2013Applicant: Shionogi & Co., Ltd.Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
-
Publication number: 20130172340Abstract: In one aspect, the invention relates to substituted purine analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity 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: June 22, 2011Publication date: July 4, 2013Applicant: University of Central Flordia Research Foundation,Inventors: James Turkson, Patrick Gunning
-
Publication number: 20130172314Abstract: 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: September 14, 2012Publication date: July 4, 2013Applicant: Pharmacyclics, Inc.Inventors: Wei CHEN, David J. Loury
-
Publication number: 20130137685Abstract: The invention relates to oxazolopyrimidine compounds of formula (I), where A, R1, R2 and R3 are defined as stated in the claims. The compounds of formula (I) are suitable, for example, for wound healing.Type: ApplicationFiled: January 12, 2011Publication date: May 30, 2013Applicant: SANOFIInventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Andreas Gille, Katrin Hiss
-
Publication number: 20130137676Abstract: The invention relates to a compound of formula (I) wherein A and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: November 19, 2012Publication date: May 30, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
-
Patent number: 8445675Abstract: Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and in the specification, and an amount of a physiologically acceptable acid or mixture of acids sufficient to dissolve the active substance and act as a stabilizer, optionally together with other formulating excipients suitable for parenteral administration, and a process for preparing the infusible or injectable solutions according to the invention.Type: GrantFiled: February 6, 2009Date of Patent: May 21, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Detlef Mohr, Claus Veit, Fridtjof Traulsen
-
Patent number: 8445487Abstract: Purine 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: February 9, 2012Date of Patent: May 21, 2013Assignee: Genentech, Inc.Inventors: Georgette Castanedo, Irina Chuckowree, Adrian Folkes, Daniel P. Sutherlin, Nan Chi Wan
-
Publication number: 20130123254Abstract: The present invention relates to mGluR5 positive allosteric modulators (PAM) and methods for identifying pharmaceutically acceptable compounds with high tolerability and safety, which method comprises the use of at least one non-competitive mGluR5 allosteric modulator which has a shift factor measured at 10 uM glutamate concentration below 3.Type: ApplicationFiled: September 14, 2012Publication date: May 16, 2013Inventors: Barbara Biemans, Georg Jaeschke, Lothar Lindemann, Wolfgang Muster, Heinz Stadler, Eric Vieira
-
Publication number: 20130116236Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: November 6, 2012Publication date: May 9, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
-
Patent number: 8435987Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R4, R5, R6 and Z are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of P38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: August 3, 2011Date of Patent: May 7, 2013Assignee: Amgen Inc.Inventors: Liping H. Pettus, Andrew Tasker, Shimin Xu, Ryan Wurz
-
Publication number: 20130096114Abstract: A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided: or a pharmaceutically acceptable salt, stereoisomer, or hydrate thereof.Type: ApplicationFiled: December 7, 2012Publication date: April 18, 2013Applicant: SURFACE LOGIX, INC.Inventor: SURFACE LOGIX, INC.
-
Publication number: 20130089512Abstract: New heteroaryl imidazolone derivatives having the chemical structure of formula (I) are disclosed, as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: June 14, 2011Publication date: April 11, 2013Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Elena Gomez Castillo, Jordi Bach Taña
-
Publication number: 20130079303Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: ApplicationFiled: November 19, 2012Publication date: March 28, 2013Applicant: AMGEN INC.Inventor: Amgen Inc.
-
Publication number: 20130079342Abstract: Substituted bicyclic heteroaryls of the following formulae 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 LeukemiaType: ApplicationFiled: June 30, 2011Publication date: March 28, 2013Inventors: Paul John Dransfield, Felix Gonzalez Lopez De Turiso, Vatee Pattaropong, Jillian L. Simard
-
Publication number: 20130079512Abstract: The present invention relates to purine compounds that are useful as kinase inhibitors. More particularly, the present invention relates to purine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative conditions or disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative conditions or disorders including tumours and cancers as well as other disorders or conditions related to or associated with PI3 and/or mTOR kinases.Type: ApplicationFiled: July 20, 2012Publication date: March 28, 2013Applicant: VerastemInventors: Harish K. Nagaraj, Meredith Williams
-
Patent number: 8404674Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: GrantFiled: March 4, 2008Date of Patent: March 26, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Guido Boehmelt, Harald Engelhardt, Ulrich Hirt, Otmar Schaaf, Irene Waizenegger
-
Publication number: 20130071354Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: November 16, 2012Publication date: March 21, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
-
Publication number: 20130072481Abstract: 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: ApplicationFiled: May 18, 2011Publication date: March 21, 2013Applicant: XCOVERY HOLDING COMPANY, LLCInventor: Congxin Liang
-
Publication number: 20130059835Abstract: The present invention provides heterocyclylamine derivatives of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.Type: ApplicationFiled: August 31, 2012Publication date: March 7, 2013Applicant: INCYTE CORPORATIONInventors: Yun-Long Li, Wenqing Yao, Andrew P. Combs, Eddy W. Yue, Song Mei, Wenyu Zhu, Joseph Glenn, Thomas P. Maduskuie, JR., Richard B. Sparks, Brent Douty
-
Publication number: 20130059847Abstract: 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: April 1, 2012Publication date: March 7, 2013Inventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
-
Publication number: 20130059848Abstract: The present specification discloses cannabinoid-2 agonists, compositions comprising such cannabinoid-2 agonists, and methods of treating an individual suffering from a disease by administering compositions comprising such cannabinoid-2 agonists.Type: ApplicationFiled: February 7, 2011Publication date: March 7, 2013Applicant: ALLERGAN, INCInventors: June Chen, Simon Pettit, Hans Flirl
-
Publication number: 20130053346Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.Type: ApplicationFiled: August 23, 2012Publication date: February 28, 2013Applicant: Endo Pharmaceuticals IncInventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
-
Publication number: 20130053371Abstract: There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.Type: ApplicationFiled: January 24, 2011Publication date: February 28, 2013Applicant: CENTRO NACIONAL DE INVESTIGACIONES ONCOLÓGICAS (CNIO)Inventors: Joaquin Pastor Fernández, Sonia Martinez Gonzalez, Rosa Maria Alvarez Escobar, Antonlo Rodriguez Hergueta, José Ignacio Martin Hernando, Francisco Ramos Lima
-
Publication number: 20130035334Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.Type: ApplicationFiled: September 7, 2012Publication date: February 7, 2013Applicant: Pharmacyclics, Inc.Inventors: Lee HONIGBERG, Erik J. Verner, Joseph J. Buggy, David J. Loury, Wei Chen
-
Publication number: 20130035324Abstract: 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: August 17, 2010Publication date: February 7, 2013Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
-
Publication number: 20130023523Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein B, R1, R2, R4, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: July 19, 2012Publication date: January 24, 2013Applicant: ABBOTT LABORATORIESInventors: Gui-Dong Zhu, Jane Gong, Andrew S. Judd, Virajkumar B. Ghandi, Alexander R. Shoemaker, Thomas D. Penning, Michael R. Michaelides, Chunqiu Lai, Keith W. Woods
-
Publication number: 20130023531Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: ApplicationFiled: January 19, 2012Publication date: January 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Andreas MANTOULIDIS, Peter ETTMAYER
-
Publication number: 20130023530Abstract: The present invention is directed to novel compounds of formula I and their use as therapeutic compounds.Type: ApplicationFiled: September 26, 2012Publication date: January 24, 2013Applicant: Euroscreen S.A.Inventor: Euroscreen S.A.
-
Publication number: 20130005687Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
-
Publication number: 20120329780Abstract: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.Type: ApplicationFiled: April 23, 2012Publication date: December 27, 2012Applicant: Origenis GmbHInventors: Michael Thormann, Andreas Treml, Michael Almstetter, Nadine Traube
-
Publication number: 20120329776Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: November 4, 2011Publication date: December 27, 2012Inventors: Pingda Ren, Yi Liu, Liansheng Li, Troy Edward Wilson
-
Publication number: 20120322799Abstract: The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.Type: ApplicationFiled: November 30, 2010Publication date: December 20, 2012Applicant: PHARMATROPHIX, INC.Inventor: Gopal Damodara