Nitrogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/245)
  • Publication number: 20140018355
    Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.
    Type: Application
    Filed: June 27, 2013
    Publication date: January 16, 2014
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Timothy L. MACDONALD, Jerry L. NADLER, Peng CUI
  • Publication number: 20140011810
    Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.
    Type: Application
    Filed: September 11, 2013
    Publication date: January 9, 2014
    Applicant: Gatekeeper Pharmaceuticals, Inc.
    Inventors: Nathanael S. Gray, Wenjun Zhou
  • Patent number: 8623854
    Abstract: A method of treating cancer in a subject comprising the step of administering to the subject in need thereof an effective amount of a combination of a compound that binds a nuclear export signal (NES inhibitor) on topoisomerase II? and a topoisomerase inhibitor. Twenty small molecule inhibitors (SMI) that bind to the two nuclear export sequences (NES) topo II? have been identified from the NCI database using computer-generated molecular modeling. These SMI will improve the effectiveness of topo II directed therapeutics, particularly in the treatment of diseases such as multiple myeloma (MM). In vitro apoptosis assays indicate that these drugs may be effective as single agents or in combination with currently used cancer drugs that target topo II.
    Type: Grant
    Filed: June 13, 2011
    Date of Patent: January 7, 2014
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., University of Florida Research Foundation, Inc.
    Inventors: Daniel M. Sullivan, Joel G. Turner, Thomas C. Rowe, David A. Ostrov
  • Patent number: 8618100
    Abstract: The present invention is related to novel compounds of formula (I) having antibacterial activity against Clostridium bacteria, in particular Clostridium perfringens, pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.
    Type: Grant
    Filed: August 4, 2011
    Date of Patent: December 31, 2013
    Assignee: Elanco Animal Health Ireland Limited
    Inventors: Jerome Emile Georges Guillemont, Pierre Jean-Marie Bernard Raboisson, Nacer Lounis
  • Publication number: 20130345218
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Application
    Filed: June 14, 2013
    Publication date: December 26, 2013
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Marion W. Wannamaker, Tiansheng Wang, Francesco G. Salituro
  • Patent number: 8604055
    Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
    Type: Grant
    Filed: June 28, 2006
    Date of Patent: December 10, 2013
    Assignee: Dr. Reddy's Laboratories Ltd.
    Inventors: Anima Baruah, Dibyendu De, Ish Kumar Khanna, Sivaram Pillarisetti, Santanu Maitra, Christopher W. Alexander, Jennepalli Sreenu, Indu Dagar, Shanavas Alikunju
  • Patent number: 8592580
    Abstract: Triazinone derivatives represented by formula (I) wherein: Z, R1, R2, R3, R4, and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: November 26, 2013
    Assignees: Sanofi, Mitsubishi Tanabe Pharma Corporation
    Inventors: Alistair Lochead, Mourad Saady, Philippe Yaiche
  • Patent number: 8592370
    Abstract: The invention relates to a composition for use as a medicament comprising insulin in combination with at least one compound of formula (I) wherein the radicals R1 to R6 have the meaning according to claim 1, and/or physiologically acceptable salts thereof. Another object of the invention concerns a pharmaceutical composition comprising as active ingredients effective amounts of insulin and at least one compound of formula (I), together with pharmaceutically tolerable adjuvants, for the prophylactic or therapeutic treatment and/or monitoring of physiological and/or pathological conditions that are associated with insulin resistance. The invention also relates to a pharmaceutical package comprising insulin in a first dosage unit and at least one compound of formula (I) in a second dosage unit.
    Type: Grant
    Filed: November 13, 2009
    Date of Patent: November 26, 2013
    Assignee: Poxel S.A.S.
    Inventors: Didier Mesangeau, Daniel Cravo, Annick Audet
  • Publication number: 20130310388
    Abstract: The present invention provides compounds which are modulators of TNF-? signaling and methods of use thereof for treating a patient having a TNF-? mediated condition.
    Type: Application
    Filed: July 19, 2013
    Publication date: November 21, 2013
    Applicant: Genzyme Corporation
    Inventors: Scott F. Sneddon, John L. Kane, JR., Bradford H. Hirth, Fred Vinick, Shuang Qiao, Sharon R. Nahill, John M. Williams, Hans-Peter Biemann
  • Patent number: 8586734
    Abstract: The present invention deals with a novel process directed to the preparation of a novel aromatic di-isoimide chemical compound that has utility as a catalyst and as a curing agent in epoxy compositions. The di-isoimide serves effectively as a thermally activated latent catalyst in epoxy curing, thereby increasing shelf life, and avoids premature cross-linking. The process involves the reaction in a non-aqueous dipolar solvent of a dispersion PMDA and a substituted or unsubstituted diamino-triazine, preferably melamine. Reaction in the presence of rubber is also disclosed.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: November 19, 2013
    Assignee: E I du Pont de Nemours and Company
    Inventor: George Elias Zahr
  • Patent number: 8586584
    Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: November 19, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Annapurna Pendri, Zhongxing Zhang, Weixu Zhai, Guo Li, Samuel Gerritz, Paul Michael Scola, Li-Qiang Sun, Qian Zhao, Eric Mull
  • Publication number: 20130303461
    Abstract: The technology described herein is directed to methods of determining oligonucleotide sequences, e.g. by enriching target sequences prior to sequencing the sequences.
    Type: Application
    Filed: March 11, 2013
    Publication date: November 14, 2013
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Anthony John Iafrate, Long Phi Le, Zongli Zheng
  • Publication number: 20130303516
    Abstract: The present invention relates to novel triazine compounds of formula (1), methods of their preparation, pharmaceutical compositions containing these compounds and the use of these compounds to treat proliferative disorders such as tumors and cancers and also other conditions and disorders related to or associated with dysregulation of PI3 Kinases, PI3 Kinase pathway, mTOR and/or the mTOR pathway.
    Type: Application
    Filed: January 25, 2012
    Publication date: November 14, 2013
    Inventors: Sundeep Dugar, Dinesh Mahajan, Chandraban Rhushikesh Deokar, Peter Frank Hollinger, Kamal Kishore Kapoor
  • Patent number: 8580786
    Abstract: The invention provides for Triazine derivatives and their use to modulate protein kinase activity in a variety of conditions and diseases.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: November 12, 2013
    Assignee: Nant Holdings IP, LLC
    Inventors: Neil P. Desai, Patrick Soon-Shiong, Chunlin Tao, Qinwei Wang
  • Publication number: 20130289016
    Abstract: 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: Application
    Filed: June 10, 2013
    Publication date: October 31, 2013
    Inventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
  • Patent number: 8569335
    Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: October 29, 2013
    Assignees: EMS S.A., Universidade Estadual Paulista Julio de Mesquinta Filho—UNESP
    Inventors: Ednir D. Vizioli, Chung M. Chin, Renato F. Menegon, Lorena Blau, Jean L. Santos, Maria D. Longo
  • Publication number: 20130281389
    Abstract: Topoisomerase II alpha (topo II?) is exported from the cell nucleus in human myeloma cells by a chromosome-maintenance protein-1 (CRM1)-dependent mechanism, resulting in topo II inhibitor resistance. The nuclear export signal (NES) of topo II? is unique, making it a potential target for small molecule inhibitors. Small molecules NES inhibitors were identified, which inhibited binding of topo II? to the export receptor CRM1. Inhibition was specific to topo II? as p53 trafficking was unaffected along with topo II? protein expression and function (decatenation). These topo II?-specific nuclear export inhibitors may potentially lead to a new approach in circumventing drug resistance in multiple myeloma. The compounds provide a protocol for treating multiple myeloma or an oncogenic disease. Further, the topoisomerase II nuclear export signal inhibitor may be combined with a topoisomerase II inhibitor.
    Type: Application
    Filed: June 3, 2013
    Publication date: October 24, 2013
    Inventors: Daniel M. Sullivan, Thomas C. Rowe, David A. Ostrov, Joel G. Turner
  • Publication number: 20130281431
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: April 23, 2013
    Publication date: October 24, 2013
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Publication number: 20130274261
    Abstract: Methods of treating pulmonary hypertension are disclosed. Particular methods comprise the administration of a tryptophan hydroxylase inhibitor and a prostacyclin. Pharmaceutical formulations are also disclosed.
    Type: Application
    Filed: March 18, 2013
    Publication date: October 17, 2013
    Inventor: Arthur T. SANDS
  • Publication number: 20130274239
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Application
    Filed: May 8, 2013
    Publication date: October 17, 2013
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. A. Kiryanov
  • Patent number: 8557734
    Abstract: This invention relates to a new herbicidal composition comprising desmedipham and optionally phenmedipham and/or ethofumesate.
    Type: Grant
    Filed: April 1, 2005
    Date of Patent: October 15, 2013
    Assignee: Bayer CropScience LP
    Inventor: David A. Long
  • Publication number: 20130261119
    Abstract: The present invention provides a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or pro-drug thereof. Further provided is a method of treatment of cancer in a subject comprising administering to said subject an effective amount of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is the use of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof in the preparation of a medicament for the treatment of cancer. In addition, the present invention also provides a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof.
    Type: Application
    Filed: October 27, 2011
    Publication date: October 3, 2013
    Applicant: The Walter and Eliza Hall Institute of Medical Research
    Inventors: Antony Wilks Burgess, Francesca Walker, Keith Geoffrey Watson, Helen Witchard, Guillaume Lessene
  • Publication number: 20130261124
    Abstract: The invention provides compounds, compositions and methods for treating myotonic dystrophy. The compounds can selectively bind to CUG repeats in RNA, or to CTG repeats in DNA, and inhibit replication of the nucleic acids.
    Type: Application
    Filed: March 27, 2013
    Publication date: October 3, 2013
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Steven C. ZIMMERMAN, Chun-Ho WONG, Paul J. HERGENROTHER, Jesse PEH
  • Publication number: 20130252818
    Abstract: An amorphous formulation of a herbicidal or pesticidal substance includes a composition of the formula [A]x[MpClq]y, the composition being an ionic liquid with a melting temperature below 150° C., wherein [MpClq] is a metal chloride, x is 1, 2, 3, or 4, p is 1, 2, 3, or 4, q is 1, 2, 3, 4, 5, 6, 7, 8, or 9, and y is 1 or 2, wherein each A is a cation that is a herbicidal or pesticidal substance or a cation precursor that is a herbicidal or pesticidal substance.
    Type: Application
    Filed: March 25, 2013
    Publication date: September 26, 2013
    Inventors: Katherine Lovejoy, Rico Del Sesto, Andrew Koppisch
  • Patent number: 8536170
    Abstract: The present invention deals with a novel curable epoxy composition comprising an aromatic di-isoimide chemical compound. The di-isoimide serves effectively as a thermally activated latent catalyst in epoxy curing, thereby increasing shelf life, and avoids premature cross-linking. Novel laminated articles and printed wiring boards, including encapsulated printed wiring boards are also disclosed.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: September 17, 2013
    Assignee: E I du Pont de Nemours and Company
    Inventor: George Elias Zahr
  • 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: 8507671
    Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: August 13, 2013
    Assignee: Dow Agrosciences LLC
    Inventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
  • Publication number: 20130203758
    Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: February 4, 2013
    Publication date: August 8, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8501939
    Abstract: Compounds of the general formula (I): in which inter alia Q1 represents —NR1R3, —OR1 or —SR1 and Q2 represents —NR2R4, —OR2 or —SR2, and A represents the point of attachment to a support matrix, are useful as protein binding ligands when (a) at least one of R1, R2, R3 and R4 includes an alkyl group —CnH2n+1 in which n is greater than or equal to 7; (b) at least two of R1, R2, R3 and R4 independently include an alkyl group —CnH2n+1 or a cycloalkyl group —CnH2n?1 in which n is greater than or equal to 4; or (c) at least three of R1, R2, R3 and R4 independently include a C1-12 alkyl group substituted by —NR5R6 or aryl.
    Type: Grant
    Filed: June 8, 2006
    Date of Patent: August 6, 2013
    Assignee: Prometic Biosciences Limited
    Inventors: Jason Richard Betley, James Christopher Pearson, Helen Rosemary Tatton, Ben Martin Beacom
  • Publication number: 20130196979
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventor: ARIAD Pharmaceuticals, Inc.
  • Publication number: 20130195997
    Abstract: The invention relates to a method of controlling fungi and spores and to compositions suitable for this purpose and their use. The compositions according to the invention comprise trifloxystrobin, formate and optionally at least one further fungicide.
    Type: Application
    Filed: February 1, 2011
    Publication date: August 1, 2013
    Applicant: LANXESS DISTRIBUTION GMBH
    Inventors: Frank Saalfeld, Johannes Gareiss
  • Publication number: 20130190287
    Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.
    Type: Application
    Filed: January 7, 2013
    Publication date: July 25, 2013
    Applicant: AGIOS PHARMACEUTICALS, INC.
    Inventor: AGIOS PHARMACEUTICALS, INC.
  • 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: 8486944
    Abstract: A composition to enhance efficiency of Photosynthesis and thereby increase agriculture/horticulture yield, containing approximately 5% to 90% Melamine, approximately 10% to 80% Ortho Phosphoric acid, approximately 8% POTASSIUM HYDROXIDE, approximately 8% Sodium Hydroxide, and up to approximately 30% POTASSIUM SULPHATE, with approximately 5% of 0.5% DIETHYL AMINOETHYL HEXANOTE, approximately 10% ZINC SULPHATE MONOHYDRATE, approximately 8% to 15% Octoborate with IGSURF 6000, and approximately 5% to 10% wetting agent to get a product for boosting Photosynthesis in liquid, soluble powder, and/or granule form.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: July 16, 2013
    Assignee: Sree Ramcides Chemicals Pvt Ltd.
    Inventor: Sundaresan Subramanyan
  • Publication number: 20130178475
    Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Application
    Filed: March 10, 2011
    Publication date: July 11, 2013
    Applicant: IRONWOOD PHARMACEUTICALS, INC.
    Inventors: Joel Moore, James Jia, Takashi Nakai, Charles Kim, Thomas Wai-Ho Lee, Jane Yang
  • Publication number: 20130172317
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having an analgesic effect or an improving effect of urination disorder comprising a compound of the formula (I): wherein Rh and Rj are taken together to form a bond; Ra and Rb and/or Rd and Re are taken together to form oxo or the like; Rc is hydrogen, substituted or unsubstituted alkyl or the like; Rf is —(CR4aR4b)n—R2; R4a and R4b are hydrogen, substituted or unsubstituted alkyl or the like; R2 is substituted or unsubstituted cycloalkyl or the like; n is an integer of 1 to 4; —Rg is —X—R3; —X— is —O—, —S— or the like; R3 is substituted or unsubstituted cycloalkyl or the like, or its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: August 9, 2011
    Publication date: July 4, 2013
    Inventors: Hiroyuki Kai, Takayuki Kameyama, Tohru Horiguchi, Kentaro Asahi, Takeshi Endoh, Yasuhiko Fujii, Takuya Shintani, Ken'ichiroh Nakamura, Sae Jikihara, Tsuyoshi Hasegawa, Miho Oohara, Yukio Tada, Toshikatsu Maki, Akira Iida
  • Publication number: 20130171171
    Abstract: The present invention generally relates to prostaglandin transport. More specifically, the invention is directed to compounds that inhibit prostaglandin transport and subsequent COX-2 induction, and methods relating thereto.
    Type: Application
    Filed: July 23, 2012
    Publication date: July 4, 2013
    Inventors: Victor L. Schuster, Yuling Chi, Young-Tae Chang, Jaeki Min
  • Publication number: 20130165427
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Application
    Filed: August 24, 2012
    Publication date: June 27, 2013
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventor: Jayhong A. Chong
  • Publication number: 20130158038
    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: December 10, 2012
    Publication date: June 20, 2013
    Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER
  • Publication number: 20130158039
    Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.
    Type: Application
    Filed: January 22, 2013
    Publication date: June 20, 2013
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130150333
    Abstract: Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor ? (ROR?) activity. This modulation has numerous effects, including inhibition of TH-17 cell function and/or TH-17 cell activity, and inhibition of re-stimulation of TH-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of ROR? results in stimulation of TH-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).
    Type: Application
    Filed: February 13, 2013
    Publication date: June 13, 2013
    Applicant: ORPHAGEN PHARMACEUTICALS
    Inventor: Orphagen Pharmaceuticals
  • Publication number: 20130150355
    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, R3a have meanings given in the description.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 13, 2013
    Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER
  • Publication number: 20130150365
    Abstract: The present invention describes novel triazines, their related pyrimidines and their use in controlling insects. This invention also includes new synthetic procedures, intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects using the compounds.
    Type: Application
    Filed: February 6, 2013
    Publication date: June 13, 2013
    Applicant: Vestaron Corporation
    Inventor: Vestaron Corporation
  • Patent number: 8461331
    Abstract: Process for the preparation of compounds of the formula I in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in claim 1, which comprises the reaction of a compound of the formula II in which R1, R2, R3, R4 have the meanings indicated above, with a compound of the formula III in which R5, R6 have the meanings indicated above.
    Type: Grant
    Filed: January 15, 2009
    Date of Patent: June 11, 2013
    Assignee: Poxel SAS
    Inventors: Matthias Helmreich, Mike Brandner
  • Publication number: 20130143883
    Abstract: The invention relates to compounds of formula wherein R1, R2, R3, R4, and Ar are as defined in the specification and claims, or to pharmaceutically active acid addition salts of such compounds. Compounds of formula I are modulators for amyloid beta and may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
    Type: Application
    Filed: January 4, 2013
    Publication date: June 6, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8455252
    Abstract: Disclosed herein are materials and methods for sensitizing multidrug resistant cancer cells that express ABCG2 and related proteins members of a family of ATP-binding transporter superfamily that mediate drug efflux found in some types of multidrug resistant cancer cells. A series of compounds, including (N-(4-chlorophenyl)-2-[(6-{[4,6-di(4-morpholinyl)-1,3,5-tri-azin-2-yl]amino}-1,3-benzothiazol-2-yl)sulfanyl]acetamide), specifically inhibits ABCG2 and can be used to boost the bio-avail-ability of one or more effective cancer killing drugs, making it possible to use certain widely used chemotherapeutic reagent to treat multidrug resistance cancers. Using these compounds in combination with chemotherapeutic drugs that are substrates for ABCG2 and related proteins may also find utility in treating cancer cells that are not currently identified as multi-drug resistant. Additionally, these compounds appear to accelerate the intercellular degradation of ABCG2 and related proteins.
    Type: Grant
    Filed: October 24, 2009
    Date of Patent: June 4, 2013
    Assignee: Indiana University Research and Technology Corp.
    Inventors: Jian-Ting Zhang, Jing Qi, Hui Peng, Zizheng Dong
  • Patent number: 8455480
    Abstract: The present invention relates to novel active substance combinations which contain firstly at least one known compound of the formula (I) in which R1 and A have the meanings given in the description, and secondly at least one further known active substance from the class of the neonicotinoids, and which are highly suitable for controlling animal pests such as insects and undesired acarids.
    Type: Grant
    Filed: September 13, 2008
    Date of Patent: June 4, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Heike Hungenberg, Peter Jeschke, Robert Velten, Wolfgang Thielert
  • Publication number: 20130137571
    Abstract: The present invention relates to a novel crystalline modification of fipronil, to a process for the preparation of the same, to pesticidal and parasiticidal mixtures and compositions comprising said crystalline modification and to their use for combating pests and parasites.
    Type: Application
    Filed: January 22, 2013
    Publication date: May 30, 2013
    Applicant: BASF SE
    Inventors: Heidi Emilia SAXELL, Peter ERK, Claude TARANTA, Thomas KROEHL, Gerhard COX, Martin SUKOPP, Stefan SCHERER, Antti OJALA, Gautam R. DESIRAJU, Rahul BANERJEE, Prashant M. BHATT
  • Publication number: 20130137634
    Abstract: The disclosure relates to compounds and compositions for forming bone and methods related thereto. In one embodiment, the disclosure relates to a composition comprising a compound disclosed herein, such as 2,4-diamino-1,3,5-triazine derivatives or salts thereof, for use in bone growth processes. In a typical embodiment, a bone graft composition is implanted in a subject at a site of desired bone growth or enhancement.
    Type: Application
    Filed: August 18, 2011
    Publication date: May 30, 2013
    Applicant: EMORY UNIVERSITY
    Inventors: Scott D. Borden, Sreedhara Sangadala
  • Publication number: 20130137688
    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: November 26, 2012
    Publication date: May 30, 2013
    Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF