Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Single Bonded Directly To Each Other Patents (Class 546/306)
  • Patent number: 10669265
    Abstract: This invention is directed to compounds, which are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: June 2, 2020
    Assignee: ALLERGAN, INC.
    Inventors: Sougato Boral, Thomas C. Malone, Shimiao Wang
  • Patent number: 9670178
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: June 6, 2017
    Assignee: Dow AgroSciences LLC
    Inventors: Qiang Yang, Beth Lorsbach, Gary Roth, Noormohamed M. Niyaz, Jeffrey Nissen, Ronald Ross, Jr., Greg Whiteker, Carl DeAmicis, Kaitlyn Gray, Yu Zhang
  • Patent number: 9475780
    Abstract: The invention relates to a process for the synthesis of cyclic alkylene ureas comprising reacting in the presence of a basic catalyst, a difunctional amine A having two primary amino groups, and an aliphatic organic carbonate component C selected from the group consisting of dialkyl carbonates CD and of alkylene carbonates CA, wherein the ratio of the amount of substance Ji(—NH2) of primary amino groups —NH2 in the difunctional amine A to the sum M(C) of the amount of substance n(CD) of carbonate groups of a dialkyl carbonate CD and the amount of substance n(CA) of carbonate groups in an alkylene carbonate CA, is at least more than 2, and to the product obtained by this process.
    Type: Grant
    Filed: July 19, 2012
    Date of Patent: October 25, 2016
    Assignee: Allnex IP S.ar.L.
    Inventors: Ram Gupta, Irina Kobylanska, Urvee Treasurer, Lawrence Flood
  • Patent number: 9221765
    Abstract: Disclosure is provided for benzimidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: December 29, 2015
    Assignee: North Carolina State University
    Inventors: Christian Melander, Steven A. Rogers, Robert W. Huigens, III
  • Publication number: 20150112077
    Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Inventors: Qiang YANG, Beth LORSBACH, Gary ROTH, Noormohamed M. NIYAZ, Jeffrey NISSEN, Ronald ROSS, JR., Gregory T. WHITEKER, Carl DeAMICIS, Kaitlyn GRAY, Yu ZHANG
  • Patent number: 9000014
    Abstract: The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: April 7, 2015
    Assignee: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
  • Publication number: 20150037253
    Abstract: The present invention relates to copper, gallium and technetium coordinated thiosemicarbazone-pyridylhydrazine (substituted at the pyridine ring with a substituted benzothiazole or stilbene moiety) complexes and methods thereof. Such compounds possess utility in PET imaging and diagnosis of amyloid diseases.
    Type: Application
    Filed: December 6, 2012
    Publication date: February 5, 2015
    Inventors: Paul Donnelly, James Hickey, Kevin Barnham, Sin Chun Lim
  • Publication number: 20150005296
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Application
    Filed: September 18, 2014
    Publication date: January 1, 2015
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, JR.
  • Publication number: 20140357599
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 18, 2014
    Publication date: December 4, 2014
    Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
  • Patent number: 8895585
    Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: November 25, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
  • Publication number: 20140323486
    Abstract: The present invention provides a compound of the following formula, racemates, enantiomers and salts thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
    Type: Application
    Filed: December 21, 2012
    Publication date: October 30, 2014
    Inventors: Edward Malcolm Tyndall, Lloyd George Czaplewski, Colin William Gordon Fishwick, Andrew Ian Yule, Jeffrey Peter Mitchell, Kelly Helen Anderson, Gary Robert William Pitt
  • Patent number: 8859594
    Abstract: Disclosed are a polymorphs I-VI of N-(6-(4-chlorophenoxy)hexyl)-N?-cyano-N?-(4-pyridyl)guanidine or of a solvate thereof, a preparation method thereof, and a use thereof as a biological active ingredient. The polymorphs are useful in treatment of cancers, and diseases or disorders caused by abnormal cell proliferation.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: October 14, 2014
    Assignees: Tianjin Hemay Bio-Tech Co., Ltd., Tianjin Michele Sci-Tech Development Co., Ltd.
    Inventors: Hesheng Zhang, Xin Chen
  • Publication number: 20140242120
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, A, W1, W2, and R?1 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Yu Xie
  • Patent number: 8816076
    Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: August 26, 2014
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8809371
    Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: August 19, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
  • Patent number: 8772320
    Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: July 8, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
  • Publication number: 20140162996
    Abstract: One aspect of the disclosure relates to derivatives of aryl and heterocyclic ureido aryl and heterocyclic carboxamido isobutyric acids, dichlorophenyl urea, curcumin, and 1,3-diazetidine-2,4-dione, and pharmaceutical compositions thereof. The derivatives disclosed herein can modulate development of adipocytes and various cancer cells, including resistant cancer cells and cancer stem cells. Another aspect of the disclosure relates to the use of the derivatives and pharmaceutical compositions disclosed herein in treatment of obesity and various cancers.
    Type: Application
    Filed: July 29, 2013
    Publication date: June 12, 2014
    Applicant: CITY OF HOPE
    Inventors: Samuel RAHBAR, James L. FIGAROLA, Christopher LINCOLN, David HORNE, Rachael MOONEY, Monika POLEWSKI, George SOMLO, Lixin YANG
  • Patent number: 8716283
    Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.
    Type: Grant
    Filed: April 1, 2009
    Date of Patent: May 6, 2014
    Assignees: University of Massachusetts, President and Fellows of Harvard College
    Inventors: Jon Goguen, Ning Pan, Kyungae Lee
  • Publication number: 20140051727
    Abstract: The invention provides pyridonyl guanidine compounds that inhibit F1F0-ATPase, and methods of using pyridonyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: February 20, 2014
    Applicant: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Matthew N. Mattson, Clarke B. Taylor, Chad A. Van Huis
  • Publication number: 20140038910
    Abstract: Disclosed herein are novel pharmaceutical agents which are useful as integrin receptor antagonists that mediate the pathologic processes of angiogenesis and fibrosis and as such are useful in pharmaceutical compositions and in methods for treating conditions mediated by these integrins by inhibiting or antagonizing these integrins. The novel pharmaceutical agents include those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods and intermediates useful for making the pharmaceutical agents and methods of using the pharmaceutical agents are also provided.
    Type: Application
    Filed: July 17, 2013
    Publication date: February 6, 2014
    Applicant: Saint Louis University
    Inventors: Peter RUMINSKI, David GRIGGS
  • Publication number: 20130331570
    Abstract: The present invention relates to novel aryl urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: August 14, 2013
    Publication date: December 12, 2013
    Applicant: Allergan, Inc.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8604065
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, and use for treating cancer thereof are disclosed, wherein, the definitions of X, Y, R1, R2 and n are described in description.
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: December 10, 2013
    Inventors: Hesheng Zhang, Xin Chen, Yingwei Chen, Junjie Cong, Xingwen Li
  • Publication number: 20130310346
    Abstract: The present invention provides methods and compositions for treating or preventing bacterial infections, where a pharmaceutically acceptable iron chelator that reduces biological availability of iron for one or more strains of bacteria, such as VK28 or an analog or derivative thereof is administered to a patient in need of treatment. The method also provides methods and compositions where an iron chelator and an antibiotic are administered to a patient in need of treatment for a bacterial infection.
    Type: Application
    Filed: January 31, 2012
    Publication date: November 21, 2013
    Applicant: Government of the United States, as represented by the Secretary of the Army
    Inventor: Daniel Zurawski
  • Publication number: 20130295051
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
    Type: Application
    Filed: September 2, 2011
    Publication date: November 7, 2013
    Inventors: Kenneth W. Bair, Alexandre J. Buckmelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
  • Publication number: 20130281494
    Abstract: Disclosed are a polymorphs I-VI of N-(6-(4-chlorophenoxy)hexyl)-N?-cyano-N?-(4-pyridyl)guanidine or of a solvate thereof, a preparation method thereof, and a use thereof as a biological active ingredient. The polymorphs are useful in treatment of cancers, and diseases or disorders caused by abnormal cell proliferation.
    Type: Application
    Filed: October 25, 2011
    Publication date: October 24, 2013
    Applicants: Tianjin Michele Sci-Tech Development Co., Ltd., Tianjin Hemay Bio-Tech Co., Ltd.
    Inventors: Hesheng Zhang, Xin Chen
  • Publication number: 20130273034
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Application
    Filed: September 2, 2011
    Publication date: October 17, 2013
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng, Po-Wai Yuen
  • Patent number: 8513286
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Grant
    Filed: February 20, 2008
    Date of Patent: August 20, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Publication number: 20130171067
    Abstract: The invention relates to a compound having formula (I), compositions containing same and preparation methods thereof. The invention also relates to a complex of the compound having formula (I) with technetium-99m and tricine, the use of this complex as a diagnostic probe, diagnostic compositions containing same and methods for preparing the complex and compositions containing same.
    Type: Application
    Filed: November 24, 2011
    Publication date: July 4, 2013
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Yves Guminski, Thierry Imbert, Sabrina Pesnel, Nicolas Guilbaud, Alain Le Pape, Stéphanie Lerondel
  • Publication number: 20130172310
    Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Application
    Filed: September 12, 2012
    Publication date: July 4, 2013
    Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
  • Patent number: 8471013
    Abstract: The present invention provides a process for reacting between a phenol derivative and an aromatic substrate under phenolate forming conditions comprising the following steps: (a) reacting a phenol derivative with a base in a polar organic solvent to obtain a phenolate salt, wherein water is removed form the reaction mixture during the reaction, (b) adding the aromatic substrate to the reaction mixture obtained in step (a), (c) heating the reaction mixture of step (b) to a temperature in the range of 80° to 1300° C., preferably, 90° to 1000° C. for 2 to 7 hours to obtain a phenoxy substituted aromatic substrate, (d) removing the solvent from the mixture of step (c) and optionally further isolating an purifying the phenoxy substituted aromatic substrate. Optionally, the removal of water during step (a) is in conjunction with partial removal of the organic solvent.
    Type: Grant
    Filed: December 16, 2007
    Date of Patent: June 25, 2013
    Assignee: Makhteshim Chemical Works, Ltd.
    Inventors: David Ovadia, Raya Sturkovich, David Leonov
  • Publication number: 20130131111
    Abstract: The invention relates to a nicotinamide mononucleotide (NMN) modulator useful as a neuroprotective medicament in the treatment of neurodegenerative disorders, in particular but not exclusively disorders involving axon degeneration of neuronal tissue such as Wallerian degeneration, to the use of NMN as a biomarker for axon degeneration, to a method of demonstrating axon degeneration using an NMN-based biomarker, to a diagnostic kit for detecting axon degeneration, to a method of screening for an NMN modulator, and to an NMN modulator identified using the aforementioned screening method.
    Type: Application
    Filed: April 19, 2011
    Publication date: May 23, 2013
    Applicant: Babraham Institute
    Inventors: Michael Coleman, Laura Conforti
  • Publication number: 20130053392
    Abstract: A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R—NH—CX—NH—(CH2)n—Ar-Q-SO2—NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n=0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.
    Type: Application
    Filed: February 14, 2011
    Publication date: February 28, 2013
    Inventors: Peter Ebbesen, Claudlu T. Supuran, Andrea Scozzafava, Erik Olai Pettersen, Kaye Williams, Ludwig Dubois, Philippe Lambin
  • Publication number: 20120309797
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, and use for treating cancer thereof are disclosed, wherein, the definitions of X, Y, R1, R2 and n are described in description.
    Type: Application
    Filed: November 18, 2010
    Publication date: December 6, 2012
    Inventors: Hesheng Zhang, Xin Chen, Yingwei Chen, Junjie Cong, Xingwen Li
  • Publication number: 20120295889
    Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: May 16, 2012
    Publication date: November 22, 2012
    Applicant: Merck Serono S.A.
    Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
  • Publication number: 20120289551
    Abstract: Mineralocorticoid receptor antagonists, of which the following is exemplary.
    Type: Application
    Filed: November 7, 2011
    Publication date: November 15, 2012
    Inventors: Xin GUO, Stephen J. BOYER, Di WU, Frank WU
  • Publication number: 20120264755
    Abstract: The present application discloses a compound of the formula (I) wherein Q is optionally substituted pyridyl; p is 0-6. Y is formulae (i), (ii) and (iii) where X is ?O, ?S and ?N—CN, r is 1-12, R is —Z-A, Z is a single bond, —S(?O)2—, >P?O, >C?O, —C(?O)NH—, and —C(?S)NH—; and A is hydrogen, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, and heteroaryl; B is a single bond, —NRN—, —S(?O)2— and —O—; wherein RN is selected from hydrogen, C1-12-alkyl, C3-12-cycloalkyl, —[CH2CH2O]1-10—(C1-6-alkyl), C1-12-alkenyl, aryl, heterocyclyl, and heteroaryl; s is 0-6; and Cy is aryl, cycloalkyl, heterocyclyl, and heteroaryl. The compounds are useful for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT).
    Type: Application
    Filed: June 9, 2010
    Publication date: October 18, 2012
    Applicant: TopoTarget
    Inventors: Mette K. Christensen, Fredrik Bjorkling
  • Publication number: 20120252125
    Abstract: An indicator composition for indicating that an article has undergone an ethylene oxide sterilization process is provided. The indicator composition includes at least one pyridine derivative that reacts with moist ethylene oxide to provide an irreversible color change of the composition.
    Type: Application
    Filed: March 28, 2012
    Publication date: October 4, 2012
    Applicant: lllinois Tool Works Inc.
    Inventor: Shobha Shakher Puntambekar
  • Publication number: 20120252839
    Abstract: Compounds are described that are useful for treating an apoptosis-associated disease, which are specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Also described is a method for treating an apoptosis-associated disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of an active compound that is specifically cytotoxic to tumor cells that are overexpressing Bcl-xL, and are much less cytotoxic in isogenic cells that are not overexpressing Bcl-xL. Several scaffolds of active compounds are described.
    Type: Application
    Filed: April 2, 2012
    Publication date: October 4, 2012
    Applicant: FRED HUTCHINSON CANCER RESEARCH CENTER
    Inventors: David HOCKENBERY, Julian SIMON
  • Publication number: 20120238604
    Abstract: The present invention relates to a compound of general formula (I) or a pharmaceutically acceptable salt or solvate or thereof. In particular, the present invention relates to a method treating diseases involving cell proliferation, migration, apoptosis, or adhesion, comprising administering to a human or non-human mammalian patient an effective amount of a compound of general formula (I) or a pharmaceutically acceptable salt or solvate or thereof.
    Type: Application
    Filed: September 3, 2010
    Publication date: September 20, 2012
    Applicant: Molecular Discovery Systems
    Inventor: Robin Scaife
  • Publication number: 20120157684
    Abstract: The present invention relates to processes for the facile synthesis of diaryl amines and analogues thereof. The processes of the present invention produce diaryl amines in high yield and purity. The present invention also relates to intermediates useful in the process of the present invention.
    Type: Application
    Filed: August 24, 2011
    Publication date: June 21, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: John R. Snoonian, Patricia Ann Oliver-Shaffer
  • Publication number: 20120121527
    Abstract: Novel biaromatic compounds having the general formula (I): and cosmetic/pharmaceutical compositions comprised thereof are useful in human or veterinary medicine (in dermatology and also in the fields of cardiovascular diseases, of immune diseases and/of diseases related to the metabolism of lipids), or, alternatively, in cosmetic compositions.
    Type: Application
    Filed: January 18, 2012
    Publication date: May 17, 2012
    Applicant: Galderma Research & Development
    Inventors: Jean-Guy BOITEAU, Laurence Clary, Corinne Millois Barbuis
  • Publication number: 20120010172
    Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.
    Type: Application
    Filed: August 31, 2009
    Publication date: January 12, 2012
    Applicant: McDERMOTT WILL & EMERY LLP
    Inventors: Mette Knak Christensen, Fredrik Bjorkling
  • Publication number: 20110280803
    Abstract: The present invention provides a method for the synthesis of radioiodinated compounds which is advantageous over prior art methods. Using a hydrazine or an aminoxy in place of a primary amine for indirect radioiodination facilitates a much quicker reaction thus reducing reaction time and increasing the yield. In addition, where there are primary amines in the molecule to be radioiodinated, such as the N-terminus of a peptide or lysine residues, reaction at the hydrazine or aminoxy is greatly favoured.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 17, 2011
    Applicant: GE HEALTHCARE UK LIMITED
    Inventors: Michelle Avory, Jane Brown, Peter Brian Iveson
  • Patent number: 7932395
    Abstract: This invention provides compounds of Formula I, methods for their preparation and use for preparing compounds of Formula II wherein R1, R2, R3, R5, R6, X and n are as defined in the disclosure. This invention also discloses preparation of compounds of Formula III wherein R1, R2, R7, R8, R9 and n are as defined in the disclosure. This invention also pertains to certain compounds of Formula 4 and 6 used to prepare compounds of Formula I. wherein R1, R2, R5, X and n are as defined in the disclosure.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: April 26, 2011
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Gary David Annis
  • Publication number: 20110086891
    Abstract: This invention relates to solid forms of 2-(2,4-difluorophenyl)-6-(1-(2,6-difluorophenyl)ureido)nicotinamide and pharmaceutical compositions thereof, and methods and uses therewith.
    Type: Application
    Filed: February 12, 2010
    Publication date: April 14, 2011
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Hurrey, Dimitar Alargov, Steven C. Johnston, Stefanie Roeper, John R. Snoonian, Brett A. Cowans, Petinka Vlahova, Alexander Eberlin, Mark Eddleston, Christopher Frampton
  • Patent number: 7919513
    Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to inhibitors of ZAP70. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: April 5, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: John Cochran, Vincent Galullo, Guy W. Bemis
  • Publication number: 20110059957
    Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 29, 2009
    Publication date: March 10, 2011
    Applicant: R-TECH UENO, LTD.
    Inventors: Tatsuya Matsukawa, Kazuhiro Masuzaki, Akiko Kawasaki, Akiko Akasaka, Yosuke Kawai
  • Publication number: 20110034463
    Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.
    Type: Application
    Filed: April 1, 2009
    Publication date: February 10, 2011
    Inventors: Jon Goguen, Ning Pan, Kyungae Lee
  • Patent number: 7825279
    Abstract: Novel fused ring dicationic anti-protozoan compounds. Representative protozoan species include but are not limited to Trypanosoma brucei rhodesiense (T.b.r.) and Plasmodium falciparum. Prodrugs of these compounds can be used as an oral treatment for malaria and human African trypanosomiasis.
    Type: Grant
    Filed: November 18, 2004
    Date of Patent: November 2, 2010
    Assignees: The University of North Carolina at Chapel Hill, Georgia State University Research Foundation, Inc.
    Inventors: David W. Boykin, Richard R. Tidwell, W. David Wilson, Reto Brun, Reem K. Arafa, Chad E. Stephens
  • Publication number: 20100240654
    Abstract: A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R1a, R1b, R1c and R1d each independently represent hydrogen, etc., R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc., Z1, Z2 and Z3 each independently represent hydrogen, etc., Z4 represents hydrogen, etc. and X represents a single bond or —CO—, etc.
    Type: Application
    Filed: June 1, 2010
    Publication date: September 23, 2010
    Inventors: Richard CLARK, Shinsuke HIROTA, Hiroshi AZUMA, Kazunobu KIRA, Nobuhisa WATANABE, Tadashi NAGAKURA, Tatsuo HORIZOE