Polycyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 548/414)
  • Patent number: 10550140
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an ether (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
    Type: Grant
    Filed: October 18, 2018
    Date of Patent: February 4, 2020
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Jason Allan Wiles, Venkat Rao Gadhachanda, Godwin Pais, Akihiro Hashimoto, Qiuping Wang, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Avinash S. Phadke
  • Patent number: 10106563
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an ether (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
    Type: Grant
    Filed: August 14, 2017
    Date of Patent: October 23, 2018
    Assignee: Achillion Pharmaecuticals, Inc.
    Inventors: Jason Allan Wiles, Venkat Rao Gadhachanda, Godwin Pais, Akihiro Hashimoto, Qiuping Wang, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Avinash S. Phadke
  • Patent number: 9738786
    Abstract: Cyanine dyes with improved fluorescence intensity and photostability.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: August 22, 2017
    Assignee: Illumina Cambridge Limited
    Inventors: Nikolai Romanov, Carole Anastasi, Xiaohai Liu
  • Patent number: 9732104
    Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an ether (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
    Type: Grant
    Filed: February 25, 2015
    Date of Patent: August 15, 2017
    Assignee: Achillion Pharmaceuticals, Inc.
    Inventors: Venkat Rao Gadhachanda, Godwin Pais, Akihiro Hashimoto, Qiuping Wang, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Avinash S. Phadke, Jason Allan Wiles
  • Publication number: 20150137083
    Abstract: Conjugated aromatic derivatives having an electron donating group and an electron accepting group at each end are provided. The conjugated aromatic derivatives of the present invention may be provided with blue light-emitting property and may be applied as a host material, a dopant material, an electron transporting material or a hole transporting material. An OLED device using the conjugated aromatic derivatives is also herein disclosed.
    Type: Application
    Filed: April 16, 2014
    Publication date: May 21, 2015
    Applicant: National Tsing Hua University
    Inventors: Chien-Hong CHENG, Chih-Chun LIN
  • Publication number: 20150119281
    Abstract: A phosphine derivative of DyLight dyes modified with ethylene glycol or (poly)ethylene glycol groups. In one embodiment, the compounds are useful in chemoselective ligation reactions.
    Type: Application
    Filed: October 29, 2014
    Publication date: April 30, 2015
    Applicants: Pierce Biotechnology, Inc., Dyomics GmbH
    Inventors: Greg Hermanson, Peter T. Czerney, Surbhi Desai, Suk J. Hong, Matthias S. Wenzel, Boguslawa R. Dworecki, Frank G. Lehmann
  • Publication number: 20150031833
    Abstract: A compound has Formula I: A, B, C, D, W, X, Y, and Z are independently selected from hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 alkoxy, aryl, aldehyde, protected aldehyde, CH, N, O, S, null, and bond; Q is selected from aldehyde, protected aldehyde, and null, at least one of A, B, C, D, W, X, Y, Z, or Q is an aldehyde or protected aldehyde; the bonds between each of A-B, B-C, C-D, W-X, X-Y, and Y-Z are selected from single bond, double bond, triple bond, and no bond; L is a linker selected from a C1-C12 alkyl, aralkyl, and aryl, any of which is optionally substituted; one or more methylene unit (CH2) of the C1-C12 alkyl is optionally replaced by any combination of oxygen, carbonyl(C?O), and NH; and R1 and R2 are independently selected from —NR3R4, halogen, C1-C8 alkoxy, aralkoxy, alkenyloxy, alkynyloxy, and OCH2CH2CN; R3 and R4 are independently a C1-C4, straight chain or branched alkyl group.
    Type: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Ryan Christopher SMITH, Randall SMITH, Xiaodong ZHAO
  • Publication number: 20140374724
    Abstract: The present invention relates to a novel indole-based compound having superior hole injection and transport capabilities, light-emitting capabilities, and the like, and an organic electroluminescent device which comprises the indole-based compound in one or more organic layers thereof so as to thereby achieve improved characteristics, such as light-emitting efficiency, driving voltage, and lifespan characteristics.
    Type: Application
    Filed: December 7, 2012
    Publication date: December 25, 2014
    Applicant: DOOSAN CORPORATION
    Inventors: Hoe Moon Kim, Sung Moo Kim, Young Bae Kim, Tae Hyung Kim, Ho Cheol Park, Chang Jun Lee, Young Mi Baek, Jin Yong Shin
  • Publication number: 20140364585
    Abstract: An immunoconjugate in which a phosphate-prodrugged DNA minor groove binding agent of formula (I), where X is a nucleophilically displaceable leaving group, is conjugated to an antibody or an antigen binding fragment of an antibody, and compounds that can be used for making such immunoconjugates, and uses of such immunoconjugates.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 11, 2014
    Inventors: Qian ZHANG, Sanjeev Gangwar, Chin Pan, Daniel W. Derwin
  • Patent number: 8889884
    Abstract: A phosphine derivative of DyLight dyes modified with ethylene glycol or (poly)ethylene glycol groups. In one embodiment, the compounds are useful in chemoselective ligation reactions.
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: November 18, 2014
    Assignees: Pierce Biotechnology, Inc., Dyomics GmbH
    Inventors: Greg Hermanson, Peter T. Czerney, Surbhi Desai, Suk J. Hong, Matthias S. Wenzel, Boguslawa Dworecki, Frank G. Lehmann
  • Patent number: 8883764
    Abstract: A compound has Formula I: A, B, C, D, W, X, Y, and Z are independently selected from hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 alkoxy, aryl, aldehyde, protected aldehyde, CH, N, O, S, null, and bond; Q is selected from aldehyde, protected aldehyde, and null, at least one of A, B, C, D, W, X, Y, Z, or Q is an aldehyde or protected aldehyde; the bonds between each of A-B, B-C, C-D, W-X, X-Y, and Y-Z are selected from single bond, double bond, triple bond, and no bond; L is a linker selected from a C1-C12 alkyl, aralkyl, and aryl, any of which is optionally substituted; one or more methylene unit (CH2) of the C1-C12 alkyl is optionally replaced by any combination of oxygen, carbonyl(C?O), and NH; and R1 and R2 are independently selected from —NR3R4, halogen, C1-C8 alkoxy, aralkoxy, alkenyloxy, alkynyloxy, and OCH2CH2CN; R3 and R4 are independently a C1-C4, straight chain or branched alkyl group.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: November 11, 2014
    Assignee: Illumina, Inc.
    Inventors: Ryan Christopher Smith, Randall Smith, Xiaodong Zhao
  • Publication number: 20140315834
    Abstract: The present invention provides novel compounds and pharmaceutical compositions for the prevention and/or treatment of cancer and precancerous conditions thereof, for the treatment of pain and fever, for the treatment of skin disorders, and for treating and/or preventing inflammation-related diseases and/or cardiovascular diseases. The compounds of the invention also have analgesic properties and anti-platelet properties. The compounds of the invention may be provided to animals, including mammals and humans, by administering a suitable pharmaceutical dose in a suitable pharmaceutical dosage form. The compounds of the invention have improved efficacy and safety, including higher potency and/or fewer or less severe side effects, than conventional therapies. The compounds of the invention comprise a biologically active moiety or portion (A) that has, or is modified to have at least one carboxyl group.
    Type: Application
    Filed: September 23, 2013
    Publication date: October 23, 2014
    Applicant: Medicon Pharmaceuticals, Inc.
    Inventor: Basil RIGAS
  • Patent number: 8859110
    Abstract: An organic light-emitting diode comprising at least one cyclic phosphazene compound, a light-emitting layer formed from at least one matrix material and at least one emitter material, wherein the at least one matrix material comprises at least one cyclic phosphazene compound, the use of cyclic phosphazene compounds in organic light-emitting diodes and a device selected from the group consisting of stationary visual display units, mobile visual display units and illumination units comprising at least one inventive organic light-emitting diode, and selected cyclic phosphazene compounds and processes for preparing them.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: October 14, 2014
    Assignees: BASF SE, Koninklijke Philips Electronics N.V., Osram Opto Semiconductors GmbH, Siemens Aktiengesellschaft
    Inventors: Evelyn Fuchs, Oliver Molt, Nicolle Langer, Christian Lennartz, Peter Strohriegl, Pamela Schroegel, Herbert Friedrich Boerner, Volker Van Elsbergen, Arvid Hunze, Ralf Krause, Guenter Schmid
  • Patent number: 8852599
    Abstract: An immunoconjugate in which a phosphate-prodrugged DNA minor groove binding agent of formula (I), where X is a nucleophilically displaceable leaving group, is conjugated to an antibody or an antigen binding fragment of an antibody, and compounds that can be used for making such immunoconjugates, and uses of such immunoconjugates.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: October 7, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Qian Zhang, Sanjeev Gangwar, Chin Pan, Daniel W. Derwin
  • Patent number: 8841257
    Abstract: Compounds which inhibit the activity of signal transducer and activator of transcription 3 (STAT3) are provided together with methods of making and using the same. The compounds are designed to bind to the SH2 domain of STAT3, preventing STAT3 from binding to receptors for interleukin-6 family cytokines, growth factors such as the platelet-derived growth factor, the epidermal growth factor, vascular endothelial growth factor, and other signaling molecules such as leptin. Blocking these interactions prevents STAT3 from being phosphorylated on Tyr705, which is required for the dimerization of STAT3, translocation to the nucleus, binding to STAT3 response elements on promotors, and transcription of genes. In addition to these activities, binding to the SH2 domain of STAT3 breaks up pre-formed dimmers, thereby preventing the transcriptional activity of the inhibitor.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: September 23, 2014
    Assignee: Board of Regents, The University of Texas System
    Inventors: John S. McMurray, Pijus K. Mandal, Warren S. Liao, Fredika Robertson, Xiaomin Chen, Ramesh Rajaopal, Zhiyong Ren
  • Publication number: 20140225046
    Abstract: The present invention describes carbazole derivatives formula (1), where the following applies to the symbols used: Y is on each occurrence, identically or differently, CR or N; X is selected from C(R1)2, O, S, PR1, P(?O)R1 or BR1; characterised in that at least one group R is present which stands, identically or differently on each occurrence, for a group of the following formula (2), and/or in that at least one group R1 is present which stands for a group of the following formula (3) or (4), in particular for use as triplet matrix materials in organic electroluminescent devices. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising same.
    Type: Application
    Filed: August 23, 2012
    Publication date: August 14, 2014
    Applicant: Merck Patent GmbH
    Inventors: Anja Jatsch, Amir Hossain Parham, Christof Pflumm, Philipp Stoessel, Jonas Valentin Kroesser, Rémi Manouk Anémian, Thomas Eberle
  • Publication number: 20140220491
    Abstract: The present invention relates to a photoactive compound having a novel structure and a photosensitive resin composition including the same, and the photoactive compound according to the present invention has excellent sensitivity due to efficient absorption to a UV light source by including a nitro group and a phosphonate structure, and has excellent retention rate, mechanical strength, heat resistance, chemical resistance and developing resistance by improving solubility of the photosensitive resin composition by excellent compatibility of the phosphonate structure and a binder resin. Therefore, the photosensitive resin composition according to the present invention is useful to cure a column spacer, an overcoat, a passivation material and the like of a liquid crystal display device, and is useful in view of a high temperature process property.
    Type: Application
    Filed: May 14, 2012
    Publication date: August 7, 2014
    Applicant: LG CHEM, LTD.
    Inventors: Changho Cho, Won Jin Chung, Raisa Kharbash, Sunghyun Kim, Dongchang Choi, Sang Chul Lee, Han Soo Kim, Yoon Hee Heo, Sunhwa Kim
  • Publication number: 20140203251
    Abstract: Provided are a novel compound and an organic electronic device (OED) including the same. The novel compound has better hole injection and hole transport properties than a conventional material, and thus may enhance thermal stability and efficiency when used as a material for a hole injection or hole transport layer of the OED.
    Type: Application
    Filed: May 25, 2012
    Publication date: July 24, 2014
    Applicant: LMS CO., LTD.
    Inventors: Joon Ho Jung, Jeong Og Choi, Oh Kwan Kwon, Ah Reum Hwang
  • Publication number: 20140178461
    Abstract: Novel compounds and pharmaceutical compositions thereof administered by the respiratory route for prevention and/or treatment of lung and brain cancer and precancerous conditions thereof.
    Type: Application
    Filed: September 23, 2013
    Publication date: June 26, 2014
    Inventor: Basil RIGAS
  • Publication number: 20140171629
    Abstract: Provided is a medicinal agent for medical applications, which can act on the function of a target cell specifically. The medicinal agent for medical applications comprises: a cell-incorporated substance that can be incorporated into a target cell specifically; and an acting substance that can act on the function of the target cell and is bound to the cell-incorporated substance.
    Type: Application
    Filed: August 9, 2012
    Publication date: June 19, 2014
    Applicants: HITACHI ALOKA MEDICAL, LTD., THE NIPPON DENTAL UNIVERSITY
    Inventors: Minako Suzuki, Taka Nakahara, Hiroshi Ishikawa, Akihiro Oyama
  • Patent number: 8748410
    Abstract: The present invention is directed to a method for treating aneurysms in vascular tissue. The method includes administering a bisphosphonate compound to a subject in an amount which is effective against the formation or progression of aneurysm, or which is effective to induce regression of an established aneurysm. In alternative methods, an anti-RANKL neutralizing antibody is administered to the subject to achieve analogous anti-aneurysm effect. The methods of particular advantage in the treatment of subjects having an abdominal aortic aneurysm, a relatively common, and life-threatening, condition.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: June 10, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Dai Yamanouchi, K. Craig Kent, Bo Liu
  • Patent number: 8703302
    Abstract: Disclosed is an organic electroluminescent device (organic EL device) that is improved in the luminous efficiency, fully secured of the driving stability, and of a simple structure and disclosed also is a compound useful therefor. The organic EL device comprises a light-emitting layer disposed between an anode and a cathode piled one upon another on a substrate and the said light-emitting layer comprises a phosphorescent dopant and an indolocarbazole derivative as a host material. The indolocarbazole derivative is represented by the following formula (3) wherein Ar is an aromatic group and L is a direct bond or an aromatic group.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: April 22, 2014
    Assignee: Nippon Steel & Sumikin Chemical Co., Ltd.
    Inventors: Takahiro Kai, Masaki Komori, Toshihiro Yamamoto
  • Publication number: 20140100194
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: December 5, 2013
    Publication date: April 10, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Raymond W Colburn, Scott L. Dax, Christopher M. Flores, Jay M. Matthews
  • Publication number: 20140086844
    Abstract: Dyes and photoluminescent compounds based on polymethine dyes that contain at least one alkyl-phosphonate or substituted alkyl-phosphonate group, including the synthetic precursors, methods of synthesis, and applications thereof. Certain embodiments include heterocyclic ring systems and polymethine linkages selected such that the resulting polymethine dye is a cyanine dye, a merocyanine dye or a styryl dye.
    Type: Application
    Filed: October 7, 2013
    Publication date: March 27, 2014
    Applicant: SETA BIOMEDICALS, LLC
    Inventors: Ewald A. Terpetschnig, Leonid D. Patsenker, Larysa Markova, Iryna A. Fedyunyaeva, Olga S. Kolosova, Sergiy Starko, Anatoliy Tatarets
  • Publication number: 20140077190
    Abstract: A phosphine oxide-based compound represented by Formula 1, and an organic light-emitting device including the phosphine oxide-based compound. wherein Ar1 through Ar3, and a, b, and c are defined as in the specification.
    Type: Application
    Filed: August 30, 2013
    Publication date: March 20, 2014
    Inventors: Mi-Kyung Kim, Kwan-Hee Lee, Chang-Woong Chu, Yun-Hi Kim, Soon-Ki Kwon, Seung-Jin Yoo
  • Patent number: 8673883
    Abstract: The present disclosure relates to pantothenate derivatives for the treatment of neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: March 18, 2014
    Assignee: Retrophin, Inc.
    Inventors: Andrew Vaino, Marek Biestek, Martin Shkreli
  • Publication number: 20140027755
    Abstract: The present invention relates to an electronic device comprising one or more compounds of a formula (I) or (II). Furthermore, the invention encompasses the use of a compound of the formula (I) or (II) in an electronic device, and the provision of certain compounds of the formula (I) or (II).
    Type: Application
    Filed: March 15, 2012
    Publication date: January 30, 2014
    Applicant: Merck Patent GmbH Patents & Scientific Information
    Inventors: Teresa Mujica-Fernaud, Christof Pflumm, Irina Martynova
  • Publication number: 20130320262
    Abstract: The present invention relates to a compound of a formula (I), (II) or (III), to the use of this compound in an electronic device, and to an electronic device comprising one or more compounds of the formula (I), (II) or (III). The invention furthermore relates to a process for the preparation of a compound of the formula (I), (II) or (III) and to a formulation comprising one or more compounds of the formula (I), (II) or (III).
    Type: Application
    Filed: January 18, 2012
    Publication date: December 5, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Irina Martynova, Amir Hossain Parham, Christof Pflumm
  • Publication number: 20130289001
    Abstract: The present disclosure relates to pantothenate derivatives for the treatment of neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders.
    Type: Application
    Filed: April 26, 2013
    Publication date: October 31, 2013
    Applicant: Retrophin, Inc.
    Inventors: Andrew VAINO, Marek Biestek, Martin Shkreli
  • Publication number: 20130161603
    Abstract: Provided are a phosphaphenanthrene-carbazole-based organic light-emitting compound having superior light emitting properties, and an organic light-emitting device including the same.
    Type: Application
    Filed: July 29, 2011
    Publication date: June 27, 2013
    Applicant: INKTEC CO., LTD.
    Inventors: Kwang Choon Chung, Hyun Nam Cho, Ji Hoon Yoo, Yun Ho Jung
  • Publication number: 20130129631
    Abstract: Disclosed is a near-infrared fluorescent imaging agent comprising an indocyanine-based fluorescent dye and a liposome. The near-infrared fluorescent imaging agent of the present invention demonstrates high fluorescence intensity and a long anchoring time in sentinel lymph nodes, thereby making it useful for detecting sentinel lymph nodes in sentinel lymph node navigation surgery. Also disclosed is an indocyanine green derivative that is particularly suitable for use in the near-infrared fluorescent imaging agent of the present invention.
    Type: Application
    Filed: May 31, 2011
    Publication date: May 23, 2013
    Applicant: NATIONAL UNIVERSITY CORPORATION CHIBA UNIVERSITY
    Inventors: Hideki Hayashi, Masanori Fujinami, Taro Toyota, Yutaka Tamura, Akira Aoki, Yutaka Muraki, Kazuki Onoue
  • Patent number: 8445697
    Abstract: The present invention relates to squarylium dyes including an anchoring group, to a method of synthesis of such dye, to an electronic device comprising such dye, and to uses of such dye.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: May 21, 2013
    Assignee: Sony Corporation
    Inventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Akio Yasuda
  • Publication number: 20130119367
    Abstract: The present invention relates to a highly efficient carbazole-based compound and to an organic electroluminescence device including the same. According to the present invention, provided are a compound for an organic electroluminescence device and an organic electroluminescence device including the compound, in which a carbazole-based phosphine oxide compound, which is a compound intended for an organic electroluminescence device, is employed to overcome the problems of conventional compounds for organic electroluminescence devices, i.e. those of instable thermal stability and low efficiency, and particularly, the compound of the present invention exhibits superior efficiency in pure-blue phosphorescent devices.
    Type: Application
    Filed: June 23, 2011
    Publication date: May 16, 2013
    Applicant: INDUSTRY ACADEMIC COOPERATION FOUNDATION, DANKOOK UNIVERSITY
    Inventors: Jun Yeob Lee, Soon Ok Jeon, Hyo Suk Son, Kyoung Soo Yook, Sang Eok Jang
  • Patent number: 8440840
    Abstract: A dye including an anchoring group in its molecular structure, said anchoring group allowing a covalent coupling of said dye to a surface, for example a surface of a nanoporous semiconductor layer, said anchoring group being represented by formula 1 wherein attachment of said anchoring group within said molecular structure of said dye is at the terminal carbon marked with an asterisk in above formula, wherein G is selected from —COOH, —SO3H, —PO3H2, —BO2H2, —SH, —OH, —NH2, preferably —COOH, wherein A is selected from the group comprising H, —CN, —NO2, —COOR, —COSR, —COR, —CSR, —NCS, —CF3, —CONR2-OCF3, C6H5-mFm, wherein m=1-5, R being H or any straight or branched alkyl chain of general formula —CnH2n+I, n=O-12, preferably 0-4, or any substituted or non-substituted phenyl or biphenyl.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: May 14, 2013
    Assignee: Sony Corporation
    Inventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Akio Yasuda
  • Patent number: 8436153
    Abstract: The invention provides a novel class of cyanine dyes that are functionalized with a linker moiety that facilitates their conjugation to other species. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.
    Type: Grant
    Filed: January 5, 2010
    Date of Patent: May 7, 2013
    Assignee: Biosearch Technologies, Inc.
    Inventors: Tim Carter, Mark Reddington
  • Publication number: 20130032787
    Abstract: A heterocyclic compound represented by Formula 1 or Formula 2 below, and an organic light-emitting device including the heterocyclic compound. The organic light-emitting device may include an organic layer containing the heterocyclic compound, and thus may have a low driving voltage, a high-emission efficiency, and long lifespan characteristics. wherein R1 to R12, Ar1, Ar2, A, B, a, and b are defined as in the specification.
    Type: Application
    Filed: November 25, 2011
    Publication date: February 7, 2013
    Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.
    Inventors: Young-Kook Kim, Seok-Hwan Hwang, Hye-Jin Jung, Jin-O Lim, Sang-Hyun Han, Se-Jin Cho, Jong-Hyuk Lee
  • Publication number: 20130030166
    Abstract: Minor groove binder phosphoramidites having unique structures have been synthesized according to particular methods. These minor groove binder phosphoramidites are useful in the preparation of oligonucleotide conjugates, particularly those for use as probes and primers.
    Type: Application
    Filed: July 24, 2012
    Publication date: January 31, 2013
    Inventors: Alexei Vorobiev, Eugeny A. Lukhtanov
  • Publication number: 20130020565
    Abstract: Provided is a material for an organic electroluminescence device having a specific structure in which a dibenzothiophenyl group or a carbazolyl group is bonded to a carbazolyl group at its N-position (9-position) directly or through a linking group. Further provided is an organic electroluminescence device including one or more organic thin film layers including a light emitting layer between a cathode and an anode, in which at least one organic thin film layer contains the material for an organic electroluminescence device of the present invention.
    Type: Application
    Filed: March 29, 2011
    Publication date: January 24, 2013
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Masaki Numata, Hideaki Nagashima
  • Publication number: 20120301490
    Abstract: An immunoconjugate in which a phosphate-prodrugged DNA minor groove binding agent of formula (I), where X is a nucleophilically displaceable leaving group, is conjugated to an antibody or an antigen binding fragment of an antibody, and compounds that can be used for making such immunoconjugates, and uses of such immunoconjugates.
    Type: Application
    Filed: May 22, 2012
    Publication date: November 29, 2012
    Inventors: QIAN ZHANG, SANJEEV GANGWAR, CHIN PAN, DANIEL W. DERWIN
  • Publication number: 20120277194
    Abstract: Compounds of formula I: wherein R1, R2, n and m are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.
    Type: Application
    Filed: July 11, 2012
    Publication date: November 1, 2012
    Inventors: Rainer ALBERT, Eric FRANCOTTE, Frédéric ZECRI, Markus ZOLLINGER
  • Publication number: 20120264703
    Abstract: The present invention provides novel methods and formulations for treating anxiety disorders, including Post Traumatic Stress Disorder, in human subjects employing coordinate treatment using ? and ? blockers alone or in combination with additional psychotherapeutic medications to treat the anxiety disorder and reduce symptomology in treated subjects.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 18, 2012
    Inventors: Arifulla Khan, John Frederick Reinhard, JR.
  • Publication number: 20120225846
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: March 2, 2012
    Publication date: September 6, 2012
    Applicant: BIOENERGENIX
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • Publication number: 20120208784
    Abstract: The present invention relates to a series of substituted 3-aminopropane phosphinic acid derivatives of formula I: wherein R, R1, P1, P2 and P3 are as defined herein. The compounds of this invention are useful in treating a variety of diseases including but not limited to depression, anxiety, certain psychiatric symptoms, cognitive impairment and schizophrenia.
    Type: Application
    Filed: April 24, 2012
    Publication date: August 16, 2012
    Applicant: AVENTIS PHARMACEUTICALS INC.
    Inventors: Yong Mi CHOI-SLEDESKI, Julian LEVELL, Gregory Bernard POLI, Mark CZEKAJ, Alan John COLLIS, Roy VAZ
  • Publication number: 20120184510
    Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.
    Type: Application
    Filed: January 14, 2011
    Publication date: July 19, 2012
    Inventors: Raymond W. Colburn, Scott L. Dax, Christopher Flores, Jay Matthews, Ning Qin, Laura Reany, Christopher Teleha, Mark A. Youngman
  • Publication number: 20120128596
    Abstract: The invention generally relates to novel fluorescent phospholipid compounds, compositions comprising these compounds, and diagnostic methods utilizing these compounds.
    Type: Application
    Filed: May 11, 2010
    Publication date: May 24, 2012
    Applicant: CELLECTAR, INC.
    Inventors: Anatoly Pinchuk, Jamey P. Weichert, Marc Longino, Irawati Kandela, William R. Clarke
  • Publication number: 20120116079
    Abstract: Reagents are provided for the introduction of phosphonate groups into fluorescent dyes. Methods are also provided for preparing dye conjugates.
    Type: Application
    Filed: August 29, 2011
    Publication date: May 10, 2012
    Inventors: Eugeny Lukhtanov, Alexei Vorobiev
  • Publication number: 20120068168
    Abstract: The present invention relates to a carbazole-based phosphine oxide compound, and an organic electroluminescent device including the same. According to the present invention, provided are a compound for an organic electroluminescent device which can improve the thermal stability and efficiency characteristics which are unstable and low, respectively, corresponding to problems of known compounds for organic electroluminescent devices, and particularly, can implement excellent efficiency characteristics in a pure blue phosphorescent device, by using the carbazole-based phosphine oxide compound of the compound for the organic electroluminescent device, and the organic electroluminescent device. According to one aspect of the present invention, the carbazole-based phosphine oxide compound of the compound for the organic electroluminescent device is provided, and the organic electroluminescent device containing the same which can implement thermal stability and high efficiency characteristics is also provided.
    Type: Application
    Filed: November 16, 2009
    Publication date: March 22, 2012
    Applicant: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, DANKOOK UNIVERSITY
    Inventors: Jun-Yeob Lee, Soon-Ok Jeon, Kyoung-Soo Yook, Oh-Young Kim
  • Publication number: 20120058503
    Abstract: A novel indicator platform comprises a plurality of 1H-lndol-3-yl indicator compounds that are capable of converting to a signalophore compound in response to an external stimulus. In one class of indicator compounds, the resulting signalophores are 2-benzylideneindoline compounds that are formed by an intermolecular Aldol-type process; in a further class of indicator compounds, the resulting signalophores are 10H-indolo[1,2-a]indole compounds that are formed by an intramolecular Aldol-type process. The indicators can be used in a wide array of applications relating, for example, to biological systems or optical data storage.
    Type: Application
    Filed: May 6, 2010
    Publication date: March 8, 2012
    Applicant: Biosynth AG
    Inventors: Urs Spitz, Lukas Wick, Alexander Bayer, Christophe Weymuth, Günter Schabert
  • Publication number: 20120035346
    Abstract: Dyes and photoluminescent compounds based on polymethine dyes that contain at least one alkyl-phosphonate or substituted alkyl-phosphonate group, including the synthetic precursors, methods of synthesis, and applications thereof. Certain embodiments include heterocyclic ring systems and polymethine linkage are selected such that the resulting polymethine dye is a cyanine dye, a merocyanine dye, or a styryl dye.
    Type: Application
    Filed: January 15, 2010
    Publication date: February 9, 2012
    Inventors: Ewald A. Terpetschnig, Leonid D. Patsenker, Larysa Markova, Iryna A. Fedyunyaeva, Olga S. Kolosova, Sergiy Starko, Anatoliy Tatarets
  • Publication number: 20120035114
    Abstract: Compounds which inhibit the activity of signal transducer and activator of transcription 3 (STAT3) are provided together with methods of making and using the same. The compounds are designed to bind to the SH2 domain of STAT3, preventing STAT3 from binding to receptors for interleukin-6 family cytokines, growth factors such as the platelet-derived growth factor, the epidermal growth factor, vascular endothelial growth factor, and other signaling molecules such as leptin. Blocking these interactions prevents STAT3 from being phosphorylated on Tyr705, which is required for the dimerization of STAT3, translocation to the nucleus, binding to STAT3 response elements on promotors, and transcription of genes. In addition to these activities, binding to the SH2 domain of STAT3 breaks up pre-formed dimmers, thereby preventing the transcriptional activity of the inhibitor.
    Type: Application
    Filed: April 9, 2010
    Publication date: February 9, 2012
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: John S. McMurray, Pijus K. Mandal, Warren S. Liao, Fredika Robertson, Xiaomin Chen, Ramesh Rajaopal, Zhiyong Ren