Nitrogen Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 544/277)
  • Publication number: 20140309212
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
  • Publication number: 20140303151
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: September 14, 2011
    Publication date: October 9, 2014
    Applicant: Exelixis, Inc.
    Inventor: James William Leahy
  • Publication number: 20140296261
    Abstract: The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition.
    Type: Application
    Filed: November 14, 2012
    Publication date: October 2, 2014
    Applicants: CENTAURUS BIOPHARMA CO., LTD., CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD,
    Inventors: Dengming Xiao, Jijun Li, Yan Zhu, Yuandong Hu, Huting Wang, Zhe Wang, Zanping Wang, Yongheng Wei, Yinghui Sun, Qiong Wu, Hui Zhang, Yong Peng, Fansheng Kong, Ying Sun, Hong Luo, Yongxin Han
  • Publication number: 20140296260
    Abstract: The invention relates to novel quinazolinone compounds and their use as inhibitors of PI3 kinases, for example, PI3K?, for treating and/or preventing diseases, disorder, and conditions associated with modulating PI3 kinase activity. Novel 3-aryl-2-((arylamino)methyl)quinazolin-4(3H)-one derivatives and pharmaceutically acceptable salts or solvates thereof and their use for the treatment or prevention of diseases, disorders, and conditions associated with the activity of one or more PI3 kinase, such as PI3K?, are disclosed.
    Type: Application
    Filed: March 28, 2014
    Publication date: October 2, 2014
    Inventors: Ben C. Askew, Takeru Furuya
  • Publication number: 20140296206
    Abstract: Compounds and compositions useful for treating disorders related to Kit are described herein.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 2, 2014
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventors: Lucian V. DiPietro, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Steven Mark Wenglowsky, Douglas Wilson, Yulian Zhang
  • Publication number: 20140296207
    Abstract: 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 P13 kinase activity are described herein.
    Type: Application
    Filed: June 11, 2014
    Publication date: October 2, 2014
    Inventors: Pingda REN, Yi LIU, Liansheng LI, Troy Edward WILSON
  • Publication number: 20140296177
    Abstract: A new class of biotin protein ligase (BPL) inhibitors that have antibacterial activity against multiple Staphylococcus aureus isolates, including clinically important methicillin-resistant S. aureus (MRSA) are disclosed that are non-toxic.
    Type: Application
    Filed: September 21, 2012
    Publication date: October 2, 2014
    Inventors: Andrew Abel, Steven Polyak, Grant Booker, John Wallace, Tatiana Soares Da Costa, Angie Jarrad, William Tieu, Kelly Lee Keeling, Daniel Sejer Pederson, Nicole Pendini, Matthew Wilce, Min Yin Yap
  • Patent number: 8846694
    Abstract: Compounds of the formula (I), in which R, X, Y, Z, R3 and R4 have the meanings indicated in claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Grant
    Filed: May 13, 2009
    Date of Patent: September 30, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Mireille Krier, Thorsten Knoechel, Alfred Jonczyk, Frank Zenke, Holger Enderle
  • Patent number: 8846682
    Abstract: The present invention relates to a compound of formula (I): Wherein R1 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; R2 is an alkyl group with 1 to 18 carbon atoms or a substituted or unsubstituted cycloalkyl or aryl group; R3 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; L is a single bond, an alkyl group having 1 to 6 carbon atoms, NHCO, O, S, NHCONH or NHCOO; X, Y and Z are independently O, N, NH, S or CH; W is a single bond or an alkyl group having from 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate of said compound or salt.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: September 30, 2014
    Assignee: Neuropore Therapies, Inc.
    Inventors: Eliezer Masliah, Edward M. Rockenstein, Wolfgang Wrasidlo, Igor Flint Tsigelny
  • Patent number: 8846696
    Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: September 30, 2014
    Assignees: Cyclacel Limited, Cancer Research Technology Limited
    Inventors: Peter Martin Fischer, Michael Jarman, Edward McDonald, Bernard Nutley, Florence Raynaud, Stuart Wilson, Paul Workman
  • Publication number: 20140275013
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicants: UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR COMMERCIALIZATION, IRM LLC
    Inventors: Arnab Kumar CHATTERJEE, Fang LIANG, Casey Jacob Nelson MATHISON, Pranab Kumar MISHRA, Valentina MOLTENI, Advait Suresh Nagle, Frantisek SUPEK, Liying Jocelyn TAN, Agnes VIDAL, Michael Herman GELB, Frederick Simmons BUCKNER, Hari Babu TATIPAKA, Neil Richard NORCROSS, John Robert GILLESPIE
  • Publication number: 20140275508
    Abstract: Artificial nucleosides including 2-methyl-nucleobase-substituted butane-1,3-diol nucleosides are disclosed. Four different stereoisomers of such nucleosides are possible. Oligonucleotides made up of the artificial nucleosides form homoduplexes of greater stability than DNA duplexes and have a reduced ability to hybridize to DNA or RNA.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Elitech Holding B.V.
    Inventors: Noah Scarr, Eugeny A. Lukhtanov
  • Patent number: 8835444
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: September 16, 2014
    Assignee: Novartis AG
    Inventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
  • Patent number: 8835420
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: September 16, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Edcon Chang, Wolfgang Reinhard Ludwig Notz, Michael B. Wallace
  • Publication number: 20140256668
    Abstract: The present disclosure relates to compounds of formula (I-A) using the compounds wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5?, and m are defined herein, to pharmaceutical compositions comprising the compounds, and methods of using the compounds.
    Type: Application
    Filed: May 23, 2013
    Publication date: September 11, 2014
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Stephen CRITCHLEY, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
  • Publication number: 20140249165
    Abstract: Provided herein are methods of treatment of a cystic disease by administering a compound of Formula I. In certain embodiments, the compound for use in the methods provided herein is roscovitine or an analog thereof.
    Type: Application
    Filed: March 10, 2014
    Publication date: September 4, 2014
    Applicant: Genzyme Corporation
    Inventors: Nikolay O. BUKANOV, Oxana BESKROVNAYA
  • Patent number: 8822464
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: November 26, 2012
    Date of Patent: September 2, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
  • Publication number: 20140243359
    Abstract: The compound 2-[1-(6-aminopurin-9-yl)-2-oxoethoxy]prop-2-enal of formula (I), its monohydrate of formula (II), or its corresponding cyclic monohydrate of formula (III), in which the stereochemical chiral center indicated with an asterisk can be R (Rectus), S (Sinister) or racemic, including the tautomers of the adenine ring and the pharmaceutically acceptable salts, are used in the treatment of inflammatory disorders or of pain disorders.
    Type: Application
    Filed: July 20, 2012
    Publication date: August 28, 2014
    Applicant: MEDESTEA RESEARCH & PRODUCTION S.P.A.
    Inventors: Giulia Federica Merizzi, Fabio Grassi, Antonio Soleti
  • Patent number: 8816074
    Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Heptatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.
    Type: Grant
    Filed: May 13, 2011
    Date of Patent: August 26, 2014
    Assignee: University of Georgia Foundation, Inc.
    Inventors: Chung K. Chu, Jianing Wang
  • Publication number: 20140235643
    Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of cancer and inflammatory diseases. In particular, the method comprises administration of a compound of Formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising such compound admixed with at least one pharmaceutically acceptable excipient.
    Type: Application
    Filed: October 4, 2012
    Publication date: August 21, 2014
    Inventors: Jerry B. Evarts, Kamal D. Puri, Roger G. Ulrich, Edward A. Kesicki, Thomas Judge
  • Patent number: 8809349
    Abstract: Polymorphs of chemical compounds 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 P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: August 19, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
  • Patent number: 8809351
    Abstract: The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.
    Type: Grant
    Filed: February 6, 2013
    Date of Patent: August 19, 2014
    Assignee: Innovative Med Concepts, LLC.
    Inventor: William L. Pridgen
  • Publication number: 20140228378
    Abstract: The invention provides novel substituted cyclopropane carboxamide compounds according to Formula (I), their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
    Type: Application
    Filed: July 7, 2012
    Publication date: August 14, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
  • Publication number: 20140227183
    Abstract: Hsp90 inhibitors having are provided having the formula: (I) with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula ā€”Oā€”(CH2)nā€”Oā€”, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.
    Type: Application
    Filed: April 18, 2014
    Publication date: August 14, 2014
    Applicant: MEMORIAL SLOAN KETTERING CANCER CENTER
    Inventors: Gabriela Chiosis, Huazhong He, Laura Llauger-Bufi, Joungnam Kim, Steve M. Larson, Peter Smith-Jones
  • Publication number: 20140221366
    Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: June 11, 2012
    Publication date: August 7, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Timo Heinrich, Nadia Brugger, Kristopher Josephson
  • Patent number: 8791259
    Abstract: The present invention provides a process for the preparation of tenofovir. The present invention also provides a process for the preparation of tenofovir disoproxil or a salt thereof and its pharmaceutical composition using the tenofovir of the present invention.
    Type: Grant
    Filed: November 26, 2012
    Date of Patent: July 29, 2014
    Assignee: Laurus Labs Private Limited
    Inventors: Satyanarayana Chava, Seeta Ramanjaneyulu Gorantla, Venkata Sunil Kumar Indukuri, Sree Rambabu Joga
  • Patent number: 8791126
    Abstract: In the present invention, a novel 2-alkynyl-N9-propargyladenine represented by formula (I) wherein R1 represents a halogen atom, a furyl group, or a triazolyl group; R2 and R3 each represents a hydrogen atom or a C1-8 alkyl group, or form a cycloalkyl group by bonding to each other; and X represents a hydrogen atom or a hydroxyl group, or a pharmaceutically acceptable salt thereof, has a stronger and longer-lasting effect as a therapeutic agent for Parkinsonian syndromes.
    Type: Grant
    Filed: November 24, 2011
    Date of Patent: July 29, 2014
    Assignee: Yamasa Corporation
    Inventors: Kazuki Endo, Kohei Yamada, Kazuki Deguchi
  • Publication number: 20140206684
    Abstract: Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Applicant: INTELLIKINE LLC
    Inventors: Pingda REN, Yi LIU, Troy Edward WILSON, Katrina CHAN, Christian ROMMEL, Liansheng LI
  • Publication number: 20140206697
    Abstract: 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: Application
    Filed: March 26, 2014
    Publication date: July 24, 2014
    Applicant: Signal Pharmaceuticals, LLC
    Inventors: STEVEN CLAREEN, VERONIQUE PLANTEVIN-KRENITSKY, MOORTHY PALANKI, YOSHITAKA SATOH
  • Publication number: 20140206685
    Abstract: The present invention provides heterocyclic compounds for use as kinase inhibitors and in other applications. Also provided are pharmaceutical compositions and methods of treatments of diseases and conditions associated with P13 kinase activity.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Applicant: INTELLIKINE LLC
    Inventors: Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN, Troy Edward WILSON
  • Patent number: 8785453
    Abstract: A novel arylpiperazine-containing purine derivatives and a pharmaceutical composition comprising the same as an active ingredient, which are useful for preventing or treating depressive disorders, are provided.
    Type: Grant
    Filed: November 5, 2010
    Date of Patent: July 22, 2014
    Assignee: Green Cross Corporation
    Inventors: Jinhwa Lee, Eun-Jung Park, Suk Youn Kang, Younggyu Kong, Junwon Lee, Hyun Jung Kim, Myung Eun Jung, Ki-Nam Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
  • Publication number: 20140200229
    Abstract: Disclosed are compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating inflammatory skin diseases.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 17, 2014
    Applicant: CELLCEUTIX CORPORATION
    Inventor: KRISHNA MENON
  • Patent number: 8779131
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed. An exemplary compound disclosed in this application is shown below.
    Type: Grant
    Filed: February 12, 2013
    Date of Patent: July 15, 2014
    Assignee: Icos Corporation
    Inventors: Edward A. Kesicki, Kerry W. Fowler, Danwen Huang, Hua Chee Ooi, Amy Oliver, Kamal Deep Puri, Fuqiang Ruan, Jennifer Treiberg
  • Patent number: 8765940
    Abstract: 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 Lymphob
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: July 1, 2014
    Assignee: Amgen Inc.
    Inventors: Matthew Brown, Yi Chen, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiao He, Todd J. Kohn, Julia Winslow Lohman, Vatee Pattaropong, Jennifer Seganish, Youngsook Shin, Jillian L. Simard
  • Publication number: 20140179689
    Abstract: The subject invention concerns materials and methods for treating diseases and disorders associated with expression of Rho associated kinases (ROCKs). Examples of diseases and disorders contemplated within the scope of the invention include, but are not limited to, oncological disorders, cardiovascular diseases, CNS disorders, and inflammatory disorders. In one embodiment, a method of the invention comprises administering a therapeutically effective amount of one or more compounds of the present invention, or a composition comprising the compounds, to a person or animal in need of treatment. The subject invention also concerns compounds that inhibit ROCKs, and compositions that comprise the inhibitor compounds of the invention. Compounds contemplated within the scope of the invention include, but are not limited to, those compounds shown in Table 5.
    Type: Application
    Filed: March 30, 2012
    Publication date: June 26, 2014
    Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
    Inventors: Nicholas J. Lawrence, Said M. Sebti, ROBERTA PIREDDU
  • Publication number: 20140179718
    Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which n, m, R1, R2, and R3 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3K?. 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 one or more PI3K isoforms, such as PI3K?.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: GILEAD CALISTOGA LLC
    Inventors: Jerry EVARTS, Leena PATEL, Joshua KAPLAN, Jennifer A. TREIBERG, Stephane PERRAULT, Gary PHILLIPS
  • Patent number: 8759360
    Abstract: A compound of the formula: and pharmaceutical compositions for the treatment or prevention of pain.
    Type: Grant
    Filed: March 28, 2011
    Date of Patent: June 24, 2014
    Assignee: Eli Lilly and Company
    Inventors: Adam Jan Sanderson, Peter Charles Astles, Rossella Guidetti, Sean Patrick Hollinshead
  • Patent number: 8759359
    Abstract: The present invention provides fused derivatives of Formula I: 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: Grant
    Filed: December 17, 2010
    Date of Patent: June 24, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Yun-Long Li, Eddy W. Yue, Richard B. Sparks
  • Patent number: 8759345
    Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
  • Patent number: 8754053
    Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: June 17, 2014
    Assignee: Syngenta Crop Protection LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
  • Publication number: 20140155394
    Abstract: 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: Application
    Filed: June 21, 2013
    Publication date: June 5, 2014
    Applicant: Astrazeneca AB
    Inventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
  • Publication number: 20140154772
    Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Application
    Filed: November 27, 2013
    Publication date: June 5, 2014
    Applicant: ICOS CORPORATION
    Inventors: Chanchal SADHU, Ken DICK, Jennifer TREIBERG, C. Gregory SOWELL, Edward A. KESICKI, Amy OLIVER
  • Publication number: 20140155395
    Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.
    Type: Application
    Filed: February 4, 2014
    Publication date: June 5, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Mark R. Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
  • Publication number: 20140155605
    Abstract: The present invention provides a novel class of peptide nucleic acid derivatives, which show good cell penetration and strong binding affinity for nucleic acid.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 5, 2014
    Applicant: CTI BIO
    Inventors: Shin CHUNG, Heui-Yeon KIM, Hyun-Jin PARK, Mi-Ran KIM, Jong-Ook LEE
  • Publication number: 20140148410
    Abstract: Disclosed are nucleopeptide compounds that include a nucleobase, and an amino acid. Certain compounds further comprise a glycoside. The compounds may self-assemble to form supramolecular hydrogels. Also, the compounds may be used as a platform to examine specific biological functions (e.g., binding to DNA and RNA) of a dynamic supramolecular system that is able to interact with both proteins and nucleic acids. Other uses include: methods of growing cells and methods of delivering a substance to a cell.
    Type: Application
    Filed: December 2, 2013
    Publication date: May 29, 2014
    Applicant: Brandeis University
    Inventor: Bing Xu
  • Publication number: 20140142098
    Abstract: Disclosed are compounds of the formula (I) wherein the groups R1 to R3 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: Application
    Filed: November 11, 2013
    Publication date: May 22, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Harald ENGELHARDT, Davide GIANNI, Christian SMETHURST
  • Publication number: 20140128570
    Abstract: The present invention relates to ?-PNA monomers according to Formula I where substituent groups R1, R2, R3, R4, R5, R6, B and P are defined as set forth in the specification. The invention also provides methodology for synthesizing compounds according to Formula I and methodology for synthesizing PNA oligomers that incorporate one or more Formula I monomers.
    Type: Application
    Filed: April 6, 2012
    Publication date: May 8, 2014
    Inventors: Danith H. Ly, Srinivas Rapireddy, Bichismita Sahu
  • Publication number: 20140128390
    Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.
    Type: Application
    Filed: September 5, 2013
    Publication date: May 8, 2014
    Inventors: JACK LIN, JOHN BUELL, KATRINA CHAN, TODD EWING, PRABHA IBRAHIM, MARIKA NESPI, PHUONGLY PHAM, SONGYUAN SHI, WAYNE SPEVAK, GUOXIAN WU, JIAZHONG ZHANG, YING ZHANG
  • Publication number: 20140121222
    Abstract: The present invention provides pyrimidinones 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: Application
    Filed: January 2, 2014
    Publication date: May 1, 2014
    Applicant: Incyte Corporation
    Inventors: Yun-Long Li, Brian W. Metcalf, Andrew P. Combs
  • Publication number: 20140121223
    Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.
    Type: Application
    Filed: October 8, 2013
    Publication date: May 1, 2014
    Applicant: ICOS CORPORATION
    Inventors: Kerry W. Fowler, Danwen Huang, Edward A. Kesicki, Hua Chee Ooi, Amy Oliver, Fuqiang Ruan, Jennifer Treiberg, Kamal Deep Puri