Plural Diazine Rings Patents (Class 544/357)
  • Patent number: 8536166
    Abstract: This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: September 17, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth, Zachary Kevin Sweeney
  • Publication number: 20130225600
    Abstract: The present invention relates to compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).
    Type: Application
    Filed: October 31, 2011
    Publication date: August 29, 2013
    Applicant: LUPIN LIMITED
    Inventors: Nageswara Rao Irlapati, Gokul Keruji Deshmukh, Vijay Pandurang Karche, Santosh Madhukar Jachak, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20130225553
    Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.
    Type: Application
    Filed: March 7, 2013
    Publication date: August 29, 2013
    Applicant: ASTELLAS PHARMA INC.
    Inventor: ASTELLAS PHARMA INC.
  • Patent number: 8518947
    Abstract: The disclosure relates to (heterocycle-tetrahydropyridine)(piperazinyl)-1-alkanone and (heterocycle-dihydropyrrolidine)(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, B, m, n, W, and R2 are as defined in the disclosure; to the methods of preparing said derivatives, and to the therapeutic uses thereof.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: August 27, 2013
    Assignee: Sanofi
    Inventors: Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
  • Patent number: 8518546
    Abstract: The present invention relates to compounds represented by the following Formula I, Ring-A of the Formula I can be, for example an aryl group, and L1 is a chiral or achiral lengthening group. The compound represented by Formula I can be a photochromic compound. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds, such as represented by Formula I.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: August 27, 2013
    Assignee: Transitions Optical, Inc.
    Inventors: Meng He, Sujit Mondal, Darrin R. Dabideen, Anil Kumar, Xiao-Man Dai
  • Publication number: 20130209483
    Abstract: The disclosure relates to cannabinoid derivative compounds, pharmaceutical compositions made thereof, and methods for treating various diseases and disorders including cancer.
    Type: Application
    Filed: November 30, 2012
    Publication date: August 15, 2013
    Applicant: SUTTER WEST BAY HOSPITALS
    Inventor: SUTTER WEST BAY HOSPITALS
  • Patent number: 8507480
    Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: August 13, 2013
    Assignees: Vernalis (R&D) Limited, Cancer Research Technology Limited, The Institute of Cancer Research
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • Publication number: 20130203987
    Abstract: Disclosed are substituted pyridine compounds as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure wherein E, J, T, the ring system denoted by “B”, T, R3, R4, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 8, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventor: Rigel Pharmaceuticals, Inc.
  • Publication number: 20130196952
    Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 1, 2013
    Applicant: PFIZER INC.
    Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
  • Patent number: 8497265
    Abstract: Heteroaryloxyheterocyclyl compounds, 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, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: July 30, 2013
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
  • Publication number: 20130184248
    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: Application
    Filed: January 11, 2013
    Publication date: July 18, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF
  • Patent number: 8481543
    Abstract: A compound, particularly an antimalarial compound, according to formula I: or a pharmaceutically acceptable salt thereof, wherein: X is an electron-withdrawing group; A is an optionally substituted alkanediyl or an optionally substituted cycloalkanediyl that includes 2 to 5 carbon atoms; and R1 and R2 are each individually H, tert-butyl, isopropyl, or optionally substituted cycloalkyl.
    Type: Grant
    Filed: November 17, 2009
    Date of Patent: July 9, 2013
    Assignees: Oregon Health & Science University, The United States of America as represented by the Department of Veterans Affairs
    Inventors: Michael K. Riscoe, Rolf W. Winter, David J. Hinrichs
  • Patent number: 8481544
    Abstract: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, —S(O)NR6—, —C(?O)O— or —S(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N; R2 and R3 are as defined in the description.
    Type: Grant
    Filed: June 7, 2011
    Date of Patent: July 9, 2013
    Assignee: Biota Europe Limited
    Inventors: David John Haydon, Lloyd George Czaplewski, Nicholas John Palmer, Dale Robert Mitchell, John Frederick Atherall, Christopher Richard Steele, Tamara Ladduwahetty
  • Publication number: 20130164259
    Abstract: The present invention relates to 1,4-Substituted Piperazine Derivatives, compositions comprising one or more 1,4-Substituted Piperazine Derivatives, and methods of using the 1,4-Substituted Piperazine Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: December 20, 2010
    Publication date: June 27, 2013
    Inventors: Cliff C. Cheng, Xiaohua Huang, Gerald W. Shipps, JR.
  • Publication number: 20130164280
    Abstract: The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 27, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventor: Gilead Sciences, Inc.
  • Publication number: 20130158042
    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. R1, R2, R3, R4, Q have meanings given in the description.
    Type: Application
    Filed: December 10, 2012
    Publication date: June 20, 2013
    Inventors: Annekatrin HEIMANN, Georg DAHMANN, Marc GRUNDL, Stephan Georg MUELLER, Bernd WELLENZOHN
  • Publication number: 20130158266
    Abstract: The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system. In one aspect, the invention relates to a process for the preparation of compounds of the general formula (I): wherein HA is a pharmaceutically acceptable acid and R1-R4 are each independently selected from the group consisting of hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, and di-C1-C6-alkylamino-C2-C6-alkoxy. The invention also relates to the use of said compound to manufacture a medicament for the treatment of a serotonin-related disorder.
    Type: Application
    Filed: February 15, 2013
    Publication date: June 20, 2013
    Applicant: BIOVITRUM AB (PUBL)
    Inventor: Biovitrum AB (publ)
  • Publication number: 20130144056
    Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.
    Type: Application
    Filed: July 3, 2012
    Publication date: June 6, 2013
    Applicant: SYMPHONY EVOLUTION, INC.
    Inventors: Lynne Canne Bannen, Erick W. Co, Vasu Jammalamadaka, John M. Nuss, Moon Hwan Kim, Donna Tra Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, Zhaoyang Wen, Wei Xu, Richard George Khoury
  • Publication number: 20130137660
    Abstract: The present invention relates to pyridines or pyrazines that inhibit kinases. In particular the compounds of the invention inhibit members of the class III PTK receptor family such as FMS (CSF-IR), c-KIT, PDGFR?, PDGFR? or FLT3 and KDR, SRC, EphA2, EphA3, EphA8, FLT1, FLT4, HCK, LCK, PTK5 (FRK), SYK, DDR1 and DDR2 and RET. The compounds of the invention are useful in the treatment of kinase associated diseases such as immunological and inflammatory diseases; hyperproliferative diseases including cancer and diseases involving neo-angiogenesis; renal and kidney diseases; bone remodeling diseases; metabolic diseases; and vascular diseases.
    Type: Application
    Filed: January 22, 2013
    Publication date: May 30, 2013
    Applicant: YM Biosciences Australia Pty Ltd
    Inventor: YM Biosciences Australia Pty Ltd
  • Patent number: 8450310
    Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: May 28, 2013
    Assignees: Vernalis (R&D) Limited, Cancer Research Technology Ltd., The Institute of Cancer Research
    Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
  • Publication number: 20130129677
    Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.
    Type: Application
    Filed: December 7, 2012
    Publication date: May 23, 2013
    Applicant: Siga Technologies, Inc.
    Inventor: Siga Technologies, Inc.
  • Publication number: 20130126429
    Abstract: Methods for making sulfide scavenging compositions are provided. The compositions are secondary amine-formaldehyde adduct (SAFA) scavengers comprising less than about 40 wt % N-methyl secondary amines therein. The methods include reacting secondary amines with formaldehyde. Methods for removing sulfides from fluid streams are also provided. The methods include adding secondary amine-formaldehyde adduct (SAFA) scavengers to fluid streams. SAFA scavengers comprising less than about 40 wt % N-methyl secondary amines of the total weight of SAFA scavengers are also disclosed.
    Type: Application
    Filed: November 23, 2011
    Publication date: May 23, 2013
    Applicant: GENERAL ELECTRIC COMPANY
    Inventors: Ping Lue, Gregory Kaplan
  • Publication number: 20130131338
    Abstract: A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 14, 2012
    Publication date: May 23, 2013
    Applicant: Glaxo Group Limited
    Inventor: Glaxo Group Limited
  • Publication number: 20130131040
    Abstract: Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: November 23, 2012
    Publication date: May 23, 2013
    Applicant: Portola Pharmaceuticals, Inc.
    Inventor: Portola Pharmaceuticals, Inc.
  • Publication number: 20130119359
    Abstract: The disclosure relates to organic electroluminescent elements, materials for use in the elements, and devices using the elements, which include a compound represented by the following General Formula (1): where R1 to R12 each independently represents a hydrogen atom or a substituent and which may be bound to each other to form a non-aromatic ring, where Z1 to Z4 each independently represents a hydrogen atom or a substituent, and where Z1 and Z2, and Z3 and Z4 may be bound to each other to form a ring.
    Type: Application
    Filed: November 15, 2012
    Publication date: May 16, 2013
    Applicant: UDC Ireland Limited
    Inventor: UDC Ireland Limited
  • Publication number: 20130115194
    Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 9, 2013
    Inventors: Daniel D. LONG, Robert Murray MCKINNELL, Lan JIANG, Mandy LOO, Kassandra LEPACK, Lori Jean VAN ORDEN, Gavin OGAWA, Xiaojun HUANG, Weijiang ZHANG
  • Publication number: 20130109697
    Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
    Type: Application
    Filed: October 29, 2012
    Publication date: May 2, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Armin HECKEL, Sara Frattini, Dieter Hamprecht, Joerg Kley
  • Publication number: 20130109678
    Abstract: The invention relates to novel compounds, processes for their preparation and their use in protecting biological materials from radiation damage (radioprotection).
    Type: Application
    Filed: April 6, 2011
    Publication date: May 2, 2013
    Applicant: PETER MACCALLUM CANCER INSTITUTE
    Inventors: Roger Francis Martin, Jonathan White, Pavel Lobachevsky, David Winkler, Colin Skene, Sebastian Maruccio
  • Patent number: 8431563
    Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 23, 2011
    Date of Patent: April 30, 2013
    Assignee: Amgen Inc.
    Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, Jr., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
  • Publication number: 20130102592
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: December 5, 2012
    Publication date: April 25, 2013
    Applicant: SAREUM LIMITED
    Inventor: Sareum Limited
  • Publication number: 20130102586
    Abstract: Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.
    Type: Application
    Filed: March 30, 2012
    Publication date: April 25, 2013
    Applicant: ARRIEN PHARMACEUTICALS LLC
    Inventors: Hariprasad Vankayalapati, Rajendra P. Appalaneni, Y. Venkata Krishna Reddy
  • Publication number: 20130095193
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Application
    Filed: September 4, 2012
    Publication date: April 18, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Somhairle MacCormick, Pierre-Henri Storck, Joanne Pinder, Michael Edward O'Donnell, Ronald Marcellus Alphonsus Knegtel, Stephen Clinton Young, Philip Michael Reaper, Steven John Durrant, Heather Clare Twin, Christopher John Davis
  • Publication number: 20130096089
    Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
    Type: Application
    Filed: September 7, 2012
    Publication date: April 18, 2013
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Publication number: 20130079349
    Abstract: The present invention relates to novel 5-amino-3,6-dihydro-1H-pyrazin-2-one derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which beta-secretase is involved, such as Alzheimer's disease (AD), mild cognitive impairment, senility, dementia, dementia with Lewy bodies, Down's syndrome, dementia associated with stroke, dementia associated with Parkinson's disease or dementia associated with beta-amyloid.
    Type: Application
    Filed: June 7, 2011
    Publication date: March 28, 2013
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Andrés Avelino Trabanco-Suárez, Gary John Tresadern, Gregor James MacDonald, Juan Antonio Vega Ramiro
  • Publication number: 20130072468
    Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 21, 2013
    Inventors: Eric J. Gilbert, William J. Greenlee, Michael W. Miller, Jack D. Scott, Andrew W. Stamford
  • Publication number: 20130072485
    Abstract: The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.
    Type: Application
    Filed: November 6, 2012
    Publication date: March 21, 2013
    Applicants: Dana-Farber Cancer Institute, Inc., Whitehead Institute for Biomedical Research
    Inventors: Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc.
  • Patent number: 8399461
    Abstract: The present invention relates to bicyclic heterocycles of general formula the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.
    Type: Grant
    Filed: November 3, 2007
    Date of Patent: March 19, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Birgit Jung
  • Publication number: 20130065900
    Abstract: The invention provides a compound of the formula (1): or a salt, N-oxide or tautomer thereof; wherein R1 is cyano or C1-4 alkyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen or C1-4 alkyl; R4 and R5 are the same or different and each is selected from hydrogen, saturated C1-4 hydrocarbyl and saturated C1-4 hydrocarbyloxy; R6 and R7 are the same or different and each is selected from hydrogen, halogen, CN, C1-4 alkyl and C1-4 alkoxy wherein the C1-4 alkyl and C1-4 alkoxy are each optionally substituted with hydroxy, C1-2 alkoxy or by one or more flourine atoms; R8 is hydrogen or C1-4 alkyl; Q is an alkylene chain of 1 to 4 carbon atoms in length between the moiety Ar and the nitrogen atom N, wherein one or more of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with one or two C1-4 alkyl groups, or wherein one carbon atom of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with a group —CH2CH2— which together with the said one carbon atom forms a cyclop
    Type: Application
    Filed: May 12, 2011
    Publication date: March 14, 2013
    Applicant: SENTINEL ONCOLOGY LIMITED
    Inventors: Robert George Boyle, David Winter Walker, Richard Justin Boyce
  • Publication number: 20130053378
    Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.
    Type: Application
    Filed: July 30, 2012
    Publication date: February 28, 2013
    Applicant: Erimos Pharmaceuticals LLC
    Inventors: Qingqi Chen, Jonathan Daniel Heller, Rocio Alejandra Lopez, Amanda Jean Morris
  • Patent number: 8378095
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Grant
    Filed: May 9, 2008
    Date of Patent: February 19, 2013
    Assignee: Saruem Limited
    Inventors: John Charles Reader, John Mark Ellard, Michael Cherry
  • Publication number: 20130040949
    Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Application
    Filed: December 29, 2010
    Publication date: February 14, 2013
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Hwan G. Choi, Xianming Deng, Jianming Zhang
  • Publication number: 20130039906
    Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. 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: Application
    Filed: August 10, 2012
    Publication date: February 14, 2013
    Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Wendy Lee, Vickie H. Tsui, Xiaojing Wang, Zhaoyang Wen
  • Publication number: 20130040948
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.
    Type: Application
    Filed: February 10, 2012
    Publication date: February 14, 2013
    Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Publication number: 20130040930
    Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: April 27, 2011
    Publication date: February 14, 2013
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
  • Publication number: 20130040928
    Abstract: The present invention relates to compounds having general formula I characterised in that wherein in particular: R1 represents one or a plurality of groups such as: trifluoromethyl, halogen such as F, Cl, Br, methyl, nitro. R represents nitrogen T-U represents C?C, V represents N, W represents C?O, R2 represents Cl or H, R3=H and R4=Me, A represents wherein n=m=1, X represents —CH2— and E represents —CH—, and D represents oxygen, along with the various isomers and mixtures thereof in any proportions, and the pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 15, 2011
    Publication date: February 14, 2013
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Isabelle Leroy, Elisabeth Dupont-Passelaigue, Samuel Mialhe, Didier Junquero, Karine Valeille
  • Publication number: 20130040933
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof. Compounds of formula I are inhibitors of Janus kinases and as such are useful for the treatment of various diseases and conditions mediated by said enzymes, such as rheumatoid arthritis, asthma, COPD, ALS, and the like.
    Type: Application
    Filed: April 21, 2011
    Publication date: February 14, 2013
    Inventors: Brandon Cash, Christian Fischer, Yudith Garcia, Joon Jung, Jason Katz, June Kim, Alexey Rivkin, Adam Schell, Tony Siu, David Witter, Hua Zhou
  • Publication number: 20130029968
    Abstract: The present invention relates to compounds of formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.
    Type: Application
    Filed: July 5, 2012
    Publication date: January 31, 2013
    Applicant: PFIZER LIMITED
    Inventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Steven Wade Kortum, Yogesh Anil Sabnis, Florian Michel Wakenhut, Gavin Alistair Whitlock
  • Publication number: 20130029978
    Abstract: There is a need for FAAH inhibitors capable of oral administration and having excellent efficacy, particularly agents for the prevention and treatment of pain. Disclosed are novel arylurea compounds represented by formula (I), salts or solvates thereof, and pharmaceutical compositions comprising the same as an active ingredient. The pharmaceutical composition is used primarily for FAAH inhibitors, or agents for prevention and treatment of pain.
    Type: Application
    Filed: December 24, 2010
    Publication date: January 31, 2013
    Inventors: Tomoyuki Kamino, Yoshitaka Maeda
  • Publication number: 20130030180
    Abstract: Disclosed are compounds and methods for treating neurological and other disorders by administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for GFR? receptor molecules, which can be mimetics of glial-derived neurotrophic factor (GDNF) family ligands (GFLs), GFR?/RET signaling pathway agonists, and/or direct RET agonists (activators).
    Type: Application
    Filed: December 13, 2010
    Publication date: January 31, 2013
    Applicant: GeneCode AS
    Inventors: Mart Saarma, Mati Karelson, Maxim Bespalov, Mehis Pilv
  • Patent number: 8362249
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R6, A, B, X, Y and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: January 29, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John David Ginn, Daniel Richard Marshall, Anthony S. Prokopowicz, Sabine Schlyer, Robert Sibley, Michael Robert Turner, Di Wu, Frank Wu