Tetrazines Patents (Class 544/179)
  • Patent number: 10376594
    Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.
    Type: Grant
    Filed: December 30, 2015
    Date of Patent: August 13, 2019
    Assignee: TAGWORKS PHARMACEUTICALS B.V.
    Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen, Raffaella Rossin
  • Patent number: 10266556
    Abstract: Disclosed herein are multidentate dinuclear cyclometallated complexes.
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: April 23, 2019
    Assignees: ZHEJIANG UNIVERSITY OF TECHNOLOGY, AAC MICROTECH(CHANGZHOU)CO., LTD.
    Inventors: Guijie Li, Yuanbin She, Xiangdong Zhao, Shaohai Chen
  • Patent number: 10196477
    Abstract: Energetic nitrogen-rich monomers represented by the general Formula I: wherein each of X1 and X2 is independently NR or a covalent bond. R is H or C1-4 alkyl, each of T1 and T2 is independently a moiety selected from the group consisting of a triazole moiety, a tetrazole moiety and a guanidine moiety, at least one of T1 and T2 being substituted by at least one polymerizable group, are disclosed herein, as well as polymers based thereon, and uses of such polymers.
    Type: Grant
    Filed: October 28, 2015
    Date of Patent: February 5, 2019
    Assignee: Technology Innovation Momentum Fund (Israel) Limited Partnership
    Inventors: Michael Gozin, Alex Aizikovich, Avital Shlomovich, Adva Cohen, Tali Pechersky
  • Patent number: 10174064
    Abstract: Energetic materials that are photoactive or believed to be photoactive may include a conventional explosive (e.g. PETN, nitroglycerine) derivatized with an energetic UV-absorbing and/or VIS-absorbing chromophore such as 1,2,4,5-tetrazine or 1,3,5-triazine. Absorption of laser light having a suitably chosen wavelength may result in photodissociation, decomposition, and explosive release of energy. These materials may be used as ligands to form complexes. Coordination compounds include such complexes with counterions. Some having the formula M(L)n2+ were synthesized, wherein M is a transition metal and L is a ligand and n is 2 or 3. These may be photoactive upon exposure to a laser light beam having an appropriate wavelength of UV light, near-IR and/or visible light. Photoactive materials also include coordination compounds bearing non-energetic ligands; in this case, the counterion may be an oxidant such as perchlorate.
    Type: Grant
    Filed: January 11, 2018
    Date of Patent: January 8, 2019
    Assignee: Triad National Security, LLC
    Inventors: David E. Chavez, Susan Kloek Hanson, Robert Jason Scharff, Jacqueline Marie Veauthier, Thomas Winfield Myers
  • Patent number: 10004810
    Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: June 26, 2018
    Assignee: TAGWORKS PHARMACEUTICALS B.V.
    Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen
  • Patent number: 9931408
    Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.
    Type: Grant
    Filed: May 16, 2012
    Date of Patent: April 3, 2018
    Assignee: KONINKLIJKE PHILIPS N.V.
    Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen, Raffaella Rossin
  • Patent number: 9902705
    Abstract: The present application relates to functionalized 1,2,4,5-tetrazine compounds. The compounds are useful in compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reactions for the rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: February 27, 2018
    Assignee: The General Hospital Corporation
    Inventors: Scott A. Hilderbrand, Neal K. Devaraj, Ralph Weissleder, Mark R. Karver
  • Patent number: 9840493
    Abstract: Provided herein are modified amino acids comprising a tetrazine groups according to Formula I: polypeptides, antibodies, payloads and conjugates comprising these modified amino acid residues derived from the modified amino acids, and methods of producing the polypeptides, antibodies, payloads and conjugates comprising the modified amino acid residues. The polypeptides, antibodies, payloads and conjugates are useful in methods of treatment and prevention, methods of detection and methods of diagnosis.
    Type: Grant
    Filed: October 10, 2014
    Date of Patent: December 12, 2017
    Assignee: SUTRO BIOPHARMA, INC.
    Inventors: Wenjin Yang, Qun Yin
  • Patent number: 9714250
    Abstract: Provided in the present invention are a new method for preparing the crystalline forms of Temozolomide and three types of crystalline form of Temozolomide by the method. Said method comprises the following steps: a Temozolomide is dissolved into dimethyl sulphoxide, a second organic solvent is added for recrystallization to prepare the crystalline forms of Temozolomide, wherein the second organic solvent is an alcohol, a ketone, a halohydrocarbon or an ester.
    Type: Grant
    Filed: October 28, 2014
    Date of Patent: July 25, 2017
    Assignee: Jiangsu Tasly Diyi Pharmaceutical Co., Ltd.
    Inventors: Guocheng Wang, Wenzheng Liu, Yuzhe Gao, Hailong Yang, Qingwei Hou, Yu Zhang
  • Patent number: 9421274
    Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.
    Type: Grant
    Filed: May 16, 2012
    Date of Patent: August 23, 2016
    Assignee: Koninklijke Philips N.V.
    Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen
  • Patent number: 9334263
    Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: May 10, 2016
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
  • Patent number: 9034485
    Abstract: The present invention relates to compounds of the formula (1) and to the use thereof in organic electronic devices, and to organic electronic devices which comprise compounds of the formula (1), preferably as hole-transport materials and/or as emitting materials.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: May 19, 2015
    Assignee: Merck Patent GmbH
    Inventors: Arne Buesing, Holger Heil, Philipp Stoessel, Amir Hossain Parham, Rocco Fortte, Jonas Valentin Kroeber
  • Patent number: 9024018
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to 3-substituted-8-substituted-3H-imidazo[5,1-d][1,2,3,5]tetrazin-4-one compounds of the following formula, wherein -A and —B are as defined herein (collectively referred to herein as 38TM compounds): The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.
    Type: Grant
    Filed: June 23, 2010
    Date of Patent: May 5, 2015
    Assignee: Pharminox Limited
    Inventors: Marc Geoffery Hummersone, Malcolm Francis Graham Stevens, David Cousin
  • Publication number: 20150087043
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: April 11, 2014
    Publication date: March 26, 2015
    Applicants: Coferon, Inc, Cornell University
    Inventors: Lee Daniel Arnold, Maneesh Pingle, Douglas S. Werner
  • Patent number: 8946442
    Abstract: Foams of ionic compounds are described. Methods of making the foams are also provided. The foams are ionic and can be used for catalysis, separations, gas storage, biosensors, electronics, and electrochemical applications.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: February 3, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: Mark Brandon Shiflett, Akimichi Yokozeki
  • Publication number: 20150032045
    Abstract: The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In some embodiments, the Photolabile Compounds comprise a light antenna, such as a labeling molecule or an active derivative thereof. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect. In another embodiment, the photoreleasable ligand can be a labeling molecule, such as a fluorescent molecule.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 29, 2015
    Inventors: Rafael Yuste, Roberto Etchenique, Luis Baraldo
  • Patent number: 8940412
    Abstract: An organic electroluminescence device and a material for producing the organic electroluminescence device. The organic electroluminescence device includes an organic thin film layer between a cathode and an anode, the organic thin film layer including one or more layers, in which the organic thin film layer includes one or more light emitting layers and at least one of the light emitting layers includes a phosphorescent material and a host material. The host material has an essential structure in which a naphthalene ring is bonded to a fluorene skeleton, dibenzofuran skeleton, or dibenzothiophene skeleton. The organic electroluminescence device is a phosphorescent device having high efficiency and long lifetime.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: January 27, 2015
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Yoriyuki Takashima, Toshihiro Iwakuma, Toshinari Ogiwara, Chishio Hosokawa, Mitsunori Ito
  • Publication number: 20140364471
    Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene for sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
    Type: Application
    Filed: August 8, 2014
    Publication date: December 11, 2014
    Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
  • Patent number: 8815417
    Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein R1 to R12 are defined as in the specification.
    Type: Grant
    Filed: August 16, 2011
    Date of Patent: August 26, 2014
    Assignee: Samsung Display Co., Ltd.
    Inventors: Young-Kook Kim, Seok-Hwan Hwang, Yoon-Hyun Kwak, Sun-Young Lee, Hye-Jin Jung, Jin-O Lim, Jong-Hyuk Lee
  • Publication number: 20140199331
    Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.
    Type: Application
    Filed: May 16, 2012
    Publication date: July 17, 2014
    Applicant: KONINKLIJKE PHILIPS N.V.
    Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen
  • Patent number: 8748426
    Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of the compounds or their pharmaceutical compositions, to a mammal in need thereof.
    Type: Grant
    Filed: December 30, 2010
    Date of Patent: June 10, 2014
    Assignee: Piramal Enterprises Limited
    Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
  • Patent number: 8715621
    Abstract: The present invention provides a variety of radicals, which are useful as polarizing compounds. Exemplary radicals are represented by compounds of Structural Formulae (I), (II), (III) and (IV) as described herein.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: May 6, 2014
    Assignee: Massachusetts Institute of Technology
    Inventors: Timothy Manning Swager, Robert Guy Griffin, Olesya Haze, Bjorn Corzilius, Albert A. Smith
  • Patent number: 8716471
    Abstract: The present invention provides a process for the preparation of a tetrazine derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein R1 represents a hydrogen atom, a straight or branched C1-C6 alkyl group, C2-C6 alkenyl group or C2-C6 alkynyl group, which C1-C6 alkyl group, C2-C6 alkenyl group and C2-C6 alkynyl group is unsubstituted or substituted with 1, 2 or 3 substituents selected from halogen atoms, straight or branched C1-C4 alkoxy groups, C1-C4 alkylthio groups, C1-C4 alkylsulphinyl groups, C1-C4 alkylsulphonyl groups and phenyl groups, which phenyl groups are unsubstituted or substituted with one or more substituents selected from C1-C4 alkyl groups, C1-C4 alkoxy groups and nitro groups; or R1 represents a C3-C8 cycloalkyl group; and R2 represents a group of formula —(C?O)NR3R4, wherein R3 and R4 are independently selected from hydrogen atoms, C1-C4 alkyl groups, C2-C4 alkenyl groups and C3-C8 cycloalkyl groups, which process comprises: i) providing a compound N of formula (III
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: May 6, 2014
    Assignee: Reliance Life Sciences Pvt. Ltd.
    Inventors: Gupte Rajan, Chaturvedi Rohit, Baviskar Pravin
  • Publication number: 20140121345
    Abstract: Provided is a liquid crystal alignment layer of which a constituent member is a compound represented by the general formula (I).
    Type: Application
    Filed: May 31, 2012
    Publication date: May 1, 2014
    Applicant: DIC CORPORATION
    Inventors: Martin Schadt, Sayaka Nose, Masayuki Iwakubo, Masanao Hayashi, Yutaka Nagashima, Isa Nishiyama, Haruyoshi Takatsu
  • Publication number: 20140093522
    Abstract: The invention relates to a Prodrug activation method, for therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention also relates to a Prodrug kit comprising at least one Prodrug and at least one Activator, wherein the Prodrug comprises a Drug and a first Bio-orthogonal Reactive Group (the Trigger), and wherein the Activator comprises a second Bio-orthogonal Reactive Group. The invention also relates to targeted therapeutics used in the above-mentioned method and kit. The invention particularly pertains to antibody-drug conjugates and to bi- and trispecific antibody derivatives.
    Type: Application
    Filed: May 16, 2012
    Publication date: April 3, 2014
    Applicant: KONINKLIJKE PHILIPS N.V.
    Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen, Raffaella Rossin
  • Publication number: 20140021448
    Abstract: The various inventions and/or their embodiments disclosed herein relate to certain naphthalene diimide (NDI) compounds wherein the NDI groups are bonded to certain subclasses of bridging heteroaryl (hAr) groups, such as the “NDI-hAr-NDI” oligomeric compounds, wherein hAr is a heteroaryl group chosen to provide desirable electronic and steric properties, and the possible identities of the “Rz” terminal peripheral substituent groups are described herein. Transistor and inverter devices can be prepared.
    Type: Application
    Filed: July 15, 2013
    Publication date: January 23, 2014
    Applicant: Georgia Tech Research Corporation
    Inventors: Lauren E. Polander, Shree Prakash Tiwari, Seth Marder, Bernard Kippelen, Raghunath R. Dasari, Yulia Getmanenko, Do Hwang, Mathieu Fenoll
  • Publication number: 20130338104
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.
    Type: Application
    Filed: May 24, 2013
    Publication date: December 19, 2013
    Applicant: Pharminox Limited
    Inventors: Malcolm Francis Graham Stevens, David Cousin, Sharon Jennings, Andrew James McCarroll, John Gareth Williams, Marc Geoffery Hummersone, Jihong Zhang
  • Publication number: 20130319610
    Abstract: The present invention concerns a method for applying a first metal onto a second metal, an isolator or semiconductor substrate by a Diels-Alder reaction, in particular a Diels-Alder reaction with inverse electron demand. The present invention further concerns the binding units L 1960 and F 160.
    Type: Application
    Filed: August 12, 2011
    Publication date: December 5, 2013
    Applicants: FORSCHUNGSZENTRUM JUELICH GMBH, Deutsches Krebsforschungszentrum
    Inventors: Marlen Fleischhacker, Nadja Fleischhacker, Karola Ursula Fleischhacker
  • Patent number: 8597801
    Abstract: A heterocyclic compound includes compounds represented by Formula 1 or Formula 2 below:
    Type: Grant
    Filed: August 25, 2011
    Date of Patent: December 3, 2013
    Assignee: Samsung Display Co., Ltd.
    Inventors: Yoon-Hyun Kwak, Seok-Hwan Hwang, Young-Kook Kim, Sun-Young Lee, Hye-Jin Jung, Jin-O Lim, Sang-Hyun Han, Hee-Joo Ko, Jong-Hyuk Lee
  • Publication number: 20130302246
    Abstract: The present application provides compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reaction for rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target.
    Type: Application
    Filed: February 7, 2013
    Publication date: November 14, 2013
    Inventor: The General Hospital Corporation
  • Publication number: 20130266512
    Abstract: A Diels-Alder adduct of a trans-cyclooctene with a tetrazine is provided, wherein the adduct bears a substituent labeled with a radionuclide. A method of producing a PET or other image of an organ in an animal or human includes forming the Diels-Alder adduct in the animal or human. Trans-cyclooctenes and tetrazines suitable for preparing the adducts are provided.
    Type: Application
    Filed: July 21, 2011
    Publication date: October 10, 2013
    Applicants: University of Southern California, University of Delaware
    Inventors: Joseph M. Fox, Matthew Hassink, Melissa Blackman, Zibo Li, Peter S. Conti, Ramajeyam Selvaraj
  • Patent number: 8552183
    Abstract: The present invention relates to a process for linking two molecules by means of a Diels Alder reaction with inverse electron requirement (DARinv), comprising the following steps: reaction of a (a) triazine or tetrazine with one or more electron-attracting substituents on the ring as a diene component, the electron-attracting substituents being selected from: COOR C(O)NR2 CX3 (X=halogen) halogen CN SO2—R or SO3—R PR2 wherein R?H, alkyl, aryl, heterocycle, which in turn may be substituted, where appropriate, with alkyl, OH, SH, halogen, aryl, heterocycle, nitro, carboxyamido or amine group.
    Type: Grant
    Filed: June 18, 2007
    Date of Patent: October 8, 2013
    Assignee: Deutsches Krebsforschungszentrum Stiftung des Offentlichen Rechts
    Inventors: Manfred Wiessler, Eduard Müller, Peter Lorenz, Christian Kliem, Heinz Fleischhacker
  • Publication number: 20130243698
    Abstract: The present invention provides a variety of radicals, which are useful as polarizing compounds. Exemplary radicals are represented by compounds of Structural Formulae (I), (II), (III) and (IV) as described herein.
    Type: Application
    Filed: March 15, 2012
    Publication date: September 19, 2013
    Applicant: Massachusetts Institute of Technology
    Inventors: Timothy Manning Swager, Robert Guy Griffin, Olesya Haze, Bjorn Corzilius, Albert A. Smith
  • Publication number: 20130203828
    Abstract: The present invention provides for a derivative of monoterpene or sesquiterpene, such as a perillyl alcohol derivative. For example, the perillyl alcohol derivative may be a perillyl alcohol carbamate. The perillyl alcohol derivative may be perillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The present invention also provides for a method of treating a disease such as cancer, comprising the step of delivering to a patient a therapeutically effective amount of a derivative of monoterpene (or sesquiterpene). The route of administration may vary, and can include, inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.
    Type: Application
    Filed: August 3, 2012
    Publication date: August 8, 2013
    Applicant: NEO ONCOLOGY INC.
    Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
  • Publication number: 20130189287
    Abstract: The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs.
    Type: Application
    Filed: December 21, 2012
    Publication date: July 25, 2013
    Applicants: Innate Pharma
    Inventors: Innate Pharma, Paul Scherrer Institut
  • Patent number: 8455112
    Abstract: Organometallic complexes which bear at least one ligand which has a unit having a triplet energy of at least 22 000 cm?1, a process for preparing the organometallic complexes, a mixture comprising at least one of these organometallic complexes, the use of the organometallic complexes or of the mixture in organic light-emitting diodes, the organometallic complexes preferably being used as emitter materials, and specific nitrogen- or phosphorus-substituted triphenylene derivatives and a process for their preparation, the organometallic complex including a monoanionic bidentate ligand of formula (IIa)
    Type: Grant
    Filed: April 4, 2008
    Date of Patent: June 4, 2013
    Assignee: BASF SE
    Inventors: Herbert Friedrich Boerner, Hans-Peter Loebl, Josef Salbeck, Elena Popova
  • Patent number: 8450479
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.
    Type: Grant
    Filed: December 16, 2008
    Date of Patent: May 28, 2013
    Assignee: Pharminox Limited
    Inventors: Malcolm Francis Graham Stevens, David Cousin, Sharon Jennings, Andrew James McCarroll, John Gareth Williams, Marc Geoffery Hummersone, Jihong Zhang
  • Patent number: 8415368
    Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.
    Type: Grant
    Filed: January 26, 2009
    Date of Patent: April 9, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
  • Publication number: 20130012706
    Abstract: The present invention provides a compound of general formula (II), or a salt or solvate thereof: wherein A is independently -A1, -A2, -A3, -A4, -A5, -A6, or -A7, wherein: -A1 is independently C5-12heteroaryl, and is optionally substituted; -A2 is independently thioamido or substituted thioamido; -A3 is independently imidamido, substituted imidamido, N-hydroxyimidamido, or substituted N-hydroxyimidamido; -A4 is independently hydroxamic acid or hydroxamate; -A5 is independently carboxamide or substituted carboxamide; -A6 is independently aliphatic C2-6alkenyl, and is optionally substituted; and -A7 is independently carboxy or C1-4alkyl-carboxylate; and its use in the synthesis of temozolomide and analogues thereof.
    Type: Application
    Filed: February 25, 2011
    Publication date: January 10, 2013
    Applicant: PHARMINOX LIMITED
    Inventors: Marc Geoffery Hummersone, David Cousin
  • Publication number: 20120283280
    Abstract: A series of new chemical agents that demonstrate anti-tumor activity are described herein. The new chemical agents exhibit a dual mode of anti-tumor action: blocking epidermal growth factor receptor (EGFR) mediated signal transduction and damaging DNA by alkylation.
    Type: Application
    Filed: April 18, 2012
    Publication date: November 8, 2012
    Inventor: Bertrand Jean-Claude
  • Publication number: 20120227545
    Abstract: This invention relates to a process for the recovery of precious metal/s from a precious metal-containing material in an aqueous leach slurry or solution. The process includes the step of contacting the precious metal/s in the leach slurry or solution with a ligand selected from dithiooxamide (rubeanic acid), or a substituted dithiooxamide. The leaching of PGMs, gold and silver from their ores using the ligand of the present invention may take place under aqueous alkaline conditions, avoiding both corrosive acidic conditions and the use of cyanide.
    Type: Application
    Filed: July 21, 2010
    Publication date: September 13, 2012
    Applicant: ANGLO OPERATIONS LIMITED
    Inventors: Diandree Padayachee, Makhosazane Chucky Kunene, Marga Retha Burger, Noko Simon Phala
  • Patent number: 8258294
    Abstract: A process for the preparation of compounds of formula IA, where R?CH3 (i.e. temozolomide): comprising diazotizing a compound of the formula IIA: where in R is as defined above in the presence of at least one metal halide, an acid and a source of nitrous acid, followed by conversion of acidic solution containing temozolomide. The conversion can be carried out by a liquid-liquid extraction technique in a water immiscible solvent. The temozolomide may be further purified in an acetone-water mixture.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: September 4, 2012
    Assignee: CIPLA Limited
    Inventors: Srinivas Laxminarayan Pathi, Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan
  • Publication number: 20120220922
    Abstract: The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In some embodiments, the Photolabile Compounds comprise a light antenna, such as a labeling molecule or an active derivative thereof. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect. In another embodiment, the photoreleasable ligand can be a labeling molecule, such as a fluorescent molecule.
    Type: Application
    Filed: December 23, 2011
    Publication date: August 30, 2012
    Applicants: Universidad de Buenos Aires, THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Rafael YUSTE, Roberto Etchenique, Luis Baraldo
  • Patent number: 8236949
    Abstract: Coupling reactions, suitable for use in organic or aqueous media, are performed by contacting a 1,2,4,5-tetrazine with a dienophile. The dienophile may be covalently bonded to a protein, and the coupling reaction may be performed in biological media such as those containing cells or cell lysates. The reactions may be performed in the presence of primary amines, thiols, acetylenes, azides, phosphines, and products of Staudinger and/or Sharpless-Huisgen reactions Novel 3-substituted cyclopropene compounds and trans-cyclooctenes are exemplary dienophiles for these reactions.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: August 7, 2012
    Assignee: University of Delaware
    Inventors: Joseph Michael Fox, Melissa Blackman, Maksim Royzen, Ni Yan
  • Patent number: 8231888
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: July 31, 2012
    Assignee: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
  • Patent number: 8232392
    Abstract: Described is a new process for producing temozolomide, comprising the reaction between 5-aminoimidazole-4-carboxamide and N-succinimidyl-N?-methyl carbamate and the subsequent reaction of the thus obtained carbamoyl 5-aminoimidazole-4-carboxamide with sodium nitrite. Temozolomide is then purified by chromatography on adsorbent polymeric resin and subsequent crystallization from water and acetone.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: July 31, 2012
    Assignee: Chemi S.p.A.
    Inventors: Stefano Turchetta, Lorenzo De Ferra, Maurizio Zenoni, Mauro Anibaldi
  • Patent number: 8217063
    Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: March 15, 2008
    Date of Patent: July 10, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
  • Publication number: 20120108811
    Abstract: This present invention provides an improved process for preparing Temozolomide (TMZ) stable at room temperature for at least 18 months. This present invention also relates to Temozolomide stable at room temperature for at least 18 months.
    Type: Application
    Filed: October 28, 2010
    Publication date: May 3, 2012
    Applicant: FORMOSA LABORATORIES INC.
    Inventors: Mei-Jing Lee, Ching-Peng Wei
  • Patent number: 8153786
    Abstract: Energetic candidate azido heterocycles and their synthesis are described.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: April 10, 2012
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Raja Duddu, Paritosh Dave, Reddy Damavarapu, Rao Surapaneni
  • Publication number: 20120083513
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to 3-substituted-8-substituted-3H-imidazo[5,1-d][1,2,3,5]tetrazin-4-one compounds of the following formula, wherein -A and —B are as defined herein (collectively referred to herein as 38TM compounds): The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.
    Type: Application
    Filed: June 23, 2010
    Publication date: April 5, 2012
    Applicant: PHARMINOX LIMITED
    Inventors: Marc Geoffery Hummersone, Malcolm Francis Graham Stevens, David Cousin