Tetrazines Patents (Class 544/179)
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Patent number: 11617799Abstract: Disclosed is an advancement in provoked chemical cleavage. Thereby the invention provides the use of a diene as a chemically cleavable group attached to a Construct, and the use of a dienophile to provoke the release of the Construct by allowing the diene to react with a dienophile capable of undergoing an inverse electron demand Diels Alder reaction with the diene. The invention includes a kit for releasing a Construct CA bound to a Trigger TR, the kit having a tetrazine and a dienophile, wherein the Trigger is the tetrazine. The invention also includes the use of the formation of a pyridazine by reacting a tetrazine having a Construct CA bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of the Construct.Type: GrantFiled: June 27, 2017Date of Patent: April 4, 2023Assignees: TAGWORKS PHARMACEUTICALS B.V., SYNCOM B.V.Inventors: Marc Stefan Robillard, Wolter Ten Hoeve, Freek Johannes Maria Hoeben, Ronny Mathieu Versteegen, Hendricus Marie Janssen, Arthur Henry Antoon Marie Van Onzen, Raffaella Rossin
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Patent number: 11597731Abstract: The present invention provides a new process for preparation of imidazo-tetrazine class of chemical entity useful as anticancer agent. The present invention provides a commercially and economically viable process for preparation of Temozolomide of formula (VI). Present invention also relates to an intermediate compound of formula (III) and its preparation useful in the process for preparing Temozolomide.Type: GrantFiled: July 17, 2021Date of Patent: March 7, 2023Assignee: SHIVALIK RASAYAN LIMITEDInventors: Akshay Kant Chaturvedi, Bijan Kumar Panda, Amit Kumar, Deepali Chaturvedi
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Patent number: 11584749Abstract: The present invention relates to a novel phosphor-tetrazine and a use thereof and, more particularly, provides a novel compound having high fluorescence amplification efficiency in various wavelength ranges by using a compound having a novel core skeleton called tert-butyl (3-(7-(6-methyl-1,2,4,5-tetrazin-3-yl)-3-oxo-9-phenyl-1H-pyrrolo[3,4-b]indolizin-2(3H)-yl)propyl)carbamate.Type: GrantFiled: May 31, 2018Date of Patent: February 21, 2023Assignees: Spark Biopharma, Inc., Seoul National University R&DB FoundationInventors: Seung Bum Park, Young Jun Lee
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Patent number: 11034706Abstract: An object of the present invention is to provide a novel complex having at least one carbon-carbon double bond and/or carbon-carbon triple bond, and having at least one Diels-Alder reactive functional group such as tetrazine. The present invention provides a complex represented by a formula (1): [M4O(RCOO)6]p??(1) wherein in the formula (1), at least one of R is an alkenyl group having 2 to 18 carbon atoms or an alkynyl group having 2 to 18 carbon atoms, and at least one of R is a monovalent group represented by a structural formula (2), wherein in the structural formula (2), A1 to A4 each independently represent a nitrogen atom or a carbon atom, X1 represents a single bond or a divalent organic group, and R1 represents a hydrogen atom or a monovalent organic group.Type: GrantFiled: June 24, 2019Date of Patent: June 15, 2021Assignee: SUMITOMO RUBBER INDUSTRIES, LTD.Inventors: Hiroshi Tadaoka, Chiemi Mikura, Kazuyoshi Shiga
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Patent number: 10967069Abstract: 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: GrantFiled: July 15, 2019Date of Patent: April 6, 2021Assignee: TAGWORKS PHARMACEUTICALS B.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen, Raffaella Rossin
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Patent number: 10865209Abstract: The present invention relates to an efficient and industrially advantageous process for preparing temozolomide and the carbamoyl-AICA intermediate through the use of N-methyl carbamoylimidazole in a good overall yield and high purity.Type: GrantFiled: December 19, 2017Date of Patent: December 15, 2020Assignee: CRISTÁLIA PRODUTOS QUÍMICOS FARMACÊUTICOS LTDAInventors: Ogari Pacheco, Vincenzo De Sio, Murilo Massoni, Leandro Camargo
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Patent number: 10774171Abstract: 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: GrantFiled: November 26, 2018Date of Patent: September 15, 2020Assignee: Technology Innovation Momentum Fund (Israel) Limited PartnershipInventors: Michael Gozin, Alex Aizikovich, Avital Shlomovich, Adva Cohen, Tali Pechersky
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Patent number: 10611738Abstract: 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: GrantFiled: February 26, 2018Date of Patent: April 7, 2020Assignee: The General Hospital CorporationInventors: Scott A. Hilderbrand, Neal K. Devaraj, Ralph Weissleder, Mark R. Karver
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Patent number: 10442789Abstract: 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: GrantFiled: December 6, 2017Date of Patent: October 15, 2019Assignee: SUTRO BIOPHARMA, INC.Inventors: Wenjin Yang, Qun Yin
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Patent number: 10376594Abstract: 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: GrantFiled: December 30, 2015Date of Patent: August 13, 2019Assignee: TAGWORKS PHARMACEUTICALS B.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen, Raffaella Rossin
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Patent number: 10266556Abstract: Disclosed herein are multidentate dinuclear cyclometallated complexes.Type: GrantFiled: September 19, 2017Date of Patent: April 23, 2019Assignees: ZHEJIANG UNIVERSITY OF TECHNOLOGY, AAC MICROTECH(CHANGZHOU)CO., LTD.Inventors: Guijie Li, Yuanbin She, Xiangdong Zhao, Shaohai Chen
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Patent number: 10196477Abstract: 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: GrantFiled: October 28, 2015Date of Patent: February 5, 2019Assignee: Technology Innovation Momentum Fund (Israel) Limited PartnershipInventors: Michael Gozin, Alex Aizikovich, Avital Shlomovich, Adva Cohen, Tali Pechersky
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Patent number: 10174064Abstract: 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: GrantFiled: January 11, 2018Date of Patent: January 8, 2019Assignee: Triad National Security, LLCInventors: David E. Chavez, Susan Kloek Hanson, Robert Jason Scharff, Jacqueline Marie Veauthier, Thomas Winfield Myers
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Patent number: 10004810Abstract: 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: GrantFiled: November 23, 2016Date of Patent: June 26, 2018Assignee: TAGWORKS PHARMACEUTICALS B.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen
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Patent number: 9931408Abstract: 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: GrantFiled: May 16, 2012Date of Patent: April 3, 2018Assignee: KONINKLIJKE PHILIPS N.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen, Raffaella Rossin
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Patent number: 9902705Abstract: 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: GrantFiled: March 14, 2013Date of Patent: February 27, 2018Assignee: The General Hospital CorporationInventors: Scott A. Hilderbrand, Neal K. Devaraj, Ralph Weissleder, Mark R. Karver
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Patent number: 9840493Abstract: 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: GrantFiled: October 10, 2014Date of Patent: December 12, 2017Assignee: SUTRO BIOPHARMA, INC.Inventors: Wenjin Yang, Qun Yin
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Patent number: 9714250Abstract: 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: GrantFiled: October 28, 2014Date of Patent: July 25, 2017Assignee: Jiangsu Tasly Diyi Pharmaceutical Co., Ltd.Inventors: Guocheng Wang, Wenzheng Liu, Yuzhe Gao, Hailong Yang, Qingwei Hou, Yu Zhang
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Patent number: 9421274Abstract: 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: GrantFiled: May 16, 2012Date of Patent: August 23, 2016Assignee: Koninklijke Philips N.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen
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Patent number: 9334263Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.Type: GrantFiled: October 17, 2014Date of Patent: May 10, 2016Assignee: BLUEPRINT MEDICINES CORPORATIONInventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
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Patent number: 9034485Abstract: 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: GrantFiled: December 22, 2009Date of Patent: May 19, 2015Assignee: Merck Patent GmbHInventors: Arne Buesing, Holger Heil, Philipp Stoessel, Amir Hossain Parham, Rocco Fortte, Jonas Valentin Kroeber
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Patent number: 9024018Abstract: 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: GrantFiled: June 23, 2010Date of Patent: May 5, 2015Assignee: Pharminox LimitedInventors: Marc Geoffery Hummersone, Malcolm Francis Graham Stevens, David Cousin
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Publication number: 20150087043Abstract: 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: ApplicationFiled: April 11, 2014Publication date: March 26, 2015Applicants: Coferon, Inc, Cornell UniversityInventors: Lee Daniel Arnold, Maneesh Pingle, Douglas S. Werner
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Patent number: 8946442Abstract: 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: GrantFiled: December 21, 2010Date of Patent: February 3, 2015Assignee: E I du Pont de Nemours and CompanyInventors: Mark Brandon Shiflett, Akimichi Yokozeki
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Publication number: 20150032045Abstract: 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: ApplicationFiled: December 21, 2012Publication date: January 29, 2015Inventors: Rafael Yuste, Roberto Etchenique, Luis Baraldo
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Patent number: 8940412Abstract: 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: GrantFiled: December 22, 2009Date of Patent: January 27, 2015Assignee: Idemitsu Kosan Co., Ltd.Inventors: Yoriyuki Takashima, Toshihiro Iwakuma, Toshinari Ogiwara, Chishio Hosokawa, Mitsunori Ito
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Publication number: 20140364471Abstract: 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: ApplicationFiled: August 8, 2014Publication date: December 11, 2014Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
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Patent number: 8815417Abstract: 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: GrantFiled: August 16, 2011Date of Patent: August 26, 2014Assignee: 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
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Publication number: 20140199331Abstract: 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: ApplicationFiled: May 16, 2012Publication date: July 17, 2014Applicant: KONINKLIJKE PHILIPS N.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen
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Patent number: 8748426Abstract: 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: GrantFiled: December 30, 2010Date of Patent: June 10, 2014Assignee: Piramal Enterprises LimitedInventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
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Patent number: 8716471Abstract: 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 (IIIType: GrantFiled: November 24, 2009Date of Patent: May 6, 2014Assignee: Reliance Life Sciences Pvt. Ltd.Inventors: Gupte Rajan, Chaturvedi Rohit, Baviskar Pravin
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Patent number: 8715621Abstract: 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: GrantFiled: March 15, 2012Date of Patent: May 6, 2014Assignee: Massachusetts Institute of TechnologyInventors: Timothy Manning Swager, Robert Guy Griffin, Olesya Haze, Bjorn Corzilius, Albert A. Smith
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Publication number: 20140121345Abstract: Provided is a liquid crystal alignment layer of which a constituent member is a compound represented by the general formula (I).Type: ApplicationFiled: May 31, 2012Publication date: May 1, 2014Applicant: DIC CORPORATIONInventors: Martin Schadt, Sayaka Nose, Masayuki Iwakubo, Masanao Hayashi, Yutaka Nagashima, Isa Nishiyama, Haruyoshi Takatsu
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Publication number: 20140093522Abstract: 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: ApplicationFiled: May 16, 2012Publication date: April 3, 2014Applicant: KONINKLIJKE PHILIPS N.V.Inventors: Marc Stefan Robillard, Hendricus Marie Janssen, Wolter Ten Hoeve, Ronny Mathieu Versteegen, Raffaella Rossin
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Publication number: 20140021448Abstract: 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: ApplicationFiled: July 15, 2013Publication date: January 23, 2014Applicant: Georgia Tech Research CorporationInventors: Lauren E. Polander, Shree Prakash Tiwari, Seth Marder, Bernard Kippelen, Raghunath R. Dasari, Yulia Getmanenko, Do Hwang, Mathieu Fenoll
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Publication number: 20130338104Abstract: 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: ApplicationFiled: May 24, 2013Publication date: December 19, 2013Applicant: Pharminox LimitedInventors: Malcolm Francis Graham Stevens, David Cousin, Sharon Jennings, Andrew James McCarroll, John Gareth Williams, Marc Geoffery Hummersone, Jihong Zhang
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Publication number: 20130319610Abstract: 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: ApplicationFiled: August 12, 2011Publication date: December 5, 2013Applicants: FORSCHUNGSZENTRUM JUELICH GMBH, Deutsches KrebsforschungszentrumInventors: Marlen Fleischhacker, Nadja Fleischhacker, Karola Ursula Fleischhacker
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Patent number: 8597801Abstract: A heterocyclic compound includes compounds represented by Formula 1 or Formula 2 below:Type: GrantFiled: August 25, 2011Date of Patent: December 3, 2013Assignee: 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
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Publication number: 20130302246Abstract: 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: ApplicationFiled: February 7, 2013Publication date: November 14, 2013Inventor: The General Hospital Corporation
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Publication number: 20130266512Abstract: 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: ApplicationFiled: July 21, 2011Publication date: October 10, 2013Applicants: University of Southern California, University of DelawareInventors: Joseph M. Fox, Matthew Hassink, Melissa Blackman, Zibo Li, Peter S. Conti, Ramajeyam Selvaraj
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Patent number: 8552183Abstract: 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: GrantFiled: June 18, 2007Date of Patent: October 8, 2013Assignee: Deutsches Krebsforschungszentrum Stiftung des Offentlichen RechtsInventors: Manfred Wiessler, Eduard Müller, Peter Lorenz, Christian Kliem, Heinz Fleischhacker
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Publication number: 20130243698Abstract: 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: ApplicationFiled: March 15, 2012Publication date: September 19, 2013Applicant: Massachusetts Institute of TechnologyInventors: Timothy Manning Swager, Robert Guy Griffin, Olesya Haze, Bjorn Corzilius, Albert A. Smith
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Publication number: 20130203828Abstract: 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: ApplicationFiled: August 3, 2012Publication date: August 8, 2013Applicant: NEO ONCOLOGY INC.Inventors: Thomas Chen, Daniel Levin, Satish Pupalli
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Publication number: 20130189287Abstract: The present application relates to methods for the functionalization of immunoglobulins, in particular with drugs.Type: ApplicationFiled: December 21, 2012Publication date: July 25, 2013Applicants: Innate PharmaInventors: Innate Pharma, Paul Scherrer Institut
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Patent number: 8455112Abstract: 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: GrantFiled: April 4, 2008Date of Patent: June 4, 2013Assignee: BASF SEInventors: Herbert Friedrich Boerner, Hans-Peter Loebl, Josef Salbeck, Elena Popova
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Patent number: 8450479Abstract: 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: GrantFiled: December 16, 2008Date of Patent: May 28, 2013Assignee: Pharminox LimitedInventors: Malcolm Francis Graham Stevens, David Cousin, Sharon Jennings, Andrew James McCarroll, John Gareth Williams, Marc Geoffery Hummersone, Jihong Zhang
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Patent number: 8415368Abstract: 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: GrantFiled: January 26, 2009Date of Patent: April 9, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
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Publication number: 20130012706Abstract: 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: ApplicationFiled: February 25, 2011Publication date: January 10, 2013Applicant: PHARMINOX LIMITEDInventors: Marc Geoffery Hummersone, David Cousin
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Publication number: 20120283280Abstract: 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: ApplicationFiled: April 18, 2012Publication date: November 8, 2012Inventor: Bertrand Jean-Claude
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Publication number: 20120227545Abstract: 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: ApplicationFiled: July 21, 2010Publication date: September 13, 2012Applicant: ANGLO OPERATIONS LIMITEDInventors: Diandree Padayachee, Makhosazane Chucky Kunene, Marga Retha Burger, Noko Simon Phala