Polycyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/338)
  • Patent number: 9935274
    Abstract: The present invention relates to an organic compound represented by the following formula 1. The organic compound according to the present invention can produce an organic electroluminescent device having low driving voltage, excellent current and power efficiencies, and remarkably improved driving lifespan.
    Type: Grant
    Filed: July 8, 2015
    Date of Patent: April 3, 2018
    Assignee: Rohm and Haas Electronic Materials Korea Ltd.
    Inventors: Hee-Ryong Kang, Hyun-Ju Kang, Doo-Hyeon Moon, Young-Mook Lim, Bitnari Kim, Nam-Kyun Kim
  • Patent number: 9859507
    Abstract: The present disclosure relates to an organic electroluminescent compound of Formula 1 (variables R1-R10 defined herein), and an organic electroluminescent device comprising the same. By using the organic electroluminescent compound according to the present disclosure, it is possible to produce an organic electroluminescent device which can be operated at a lowered driving voltage, shows excellence in luminous efficiency such as current efficiency and power efficiency, and has high color purity and improved lifespan.
    Type: Grant
    Filed: April 30, 2015
    Date of Patent: January 2, 2018
    Assignee: ROHM AND HAAS ELECTRONIC MATERIALS KOREA LTD.
    Inventors: Hee-Ryong Kang, Hyun-Ju Kang, Young-Mook Lim, Mi-Ja Lee, Nam-Kyun Kim, Bitnari Kim, Jin-Ri Hong, Doo-Hyeon Moon, Su-Hyun Lee
  • Patent number: 9273065
    Abstract: The present invention is directed to a class of substituted pyrido[1?2?:4,5]pyrazino[1,2-a]-pyrimidines useful as intermediates in the production of anti-HIV agents. The compounds have the formula (I-24b): wherein Re is one or two halogen; Rz is C1-8alkyl; Rz is hydrogen, C3-6cycloalkyl, heterocyclyl, or C1-8alkyl optionally substituted with hydroxy, C3-6cycloalkyl, alkoxy, heterocyclyl, heteroaryl, C6-14aryl, or amino, wherein said amino may be optionally substituted with —C(O)C1-8alkyl or C1-8alkyl; and P1 is C6-14arylC1-8alkyl; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 30, 2015
    Date of Patent: March 1, 2016
    Assignees: Shionogi & Co., Ltd., ViiV Healthcare Company
    Inventors: Brian A. Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
  • Patent number: 9028728
    Abstract: The present invention relates to photochromic materials that include one or more indeno-fused naphthopyrans that have particular groups at the 7, 11, and 13 positions thereof, and at the position alpha to the oxygen of the pyran ring thereof. With some embodiments, hydrogen or an alkoxy group is bonded to the 7 position, an optionally substituted phenyl is bonded to the 11 position, two alkyl groups are bonded to the 13 position, and two optionally substituted phenyl groups are bonded to the position alpha to the oxygen of the pyran ring of the indeno-fused naphthopyran compound. The 13 position of the indeno-fused naphthopyrans is free of ether groups in which an ether oxygen is bonded to the 13 position, and hydroxyl. The present invention also relates to photochromic articles and compositions that include such indeno-fused naphthopyrans.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: May 12, 2015
    Assignee: Transitions Optical, Inc.
    Inventors: Kevin E. Bancroft, Anu Chopra, Xiao-Man Dai, Beon-Kyu Kim, David B. Knowles, Jason R. Lewis, Victor A. Montes, Stephen D. Straight, Massimiliano Tomasulo, Barry Van Gemert, Robert W. Walters, Wenjing Xiao, Huayun Yu, Elizabeth A. Zezinka
  • Publication number: 20150118606
    Abstract: An electrophotographic photosensitive member includes a photosensitive layer containing a naphthalenediimide derivative represented by the following general formula (1). In the general formula (1), R1 represents an alkyl group having 1 to 10 carbon atoms, an aryl group having 6 to 12 carbon atoms and optionally having an alkyl group having 1 to 10 carbon atoms, an aralkyl group having 7 to 12 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms, or an alkoxy group having 1 to 6 carbon atoms. R2 and R3, independently from each other, each represent an alkyl group having 1 to 4 carbon atoms, a halogen group, or a cyano group.
    Type: Application
    Filed: October 23, 2014
    Publication date: April 30, 2015
    Applicant: KYOCERA Document Solutions Inc.
    Inventor: Hideki OKADA
  • Patent number: 8987281
    Abstract: Described are methods and compositions for treating epithelial tumors with a folate-vinca conjugate in combination with at least one other chemotherapeutic agent in which the tumors include ovarian, endometrial or non-small cell lung cancer tumors, including platinum-resistant ovarian tumors and platinum-sensitive ovarian tumors.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: March 24, 2015
    Assignee: Endocyte, Inc.
    Inventors: Joseph Anand Reddy, Christopher Paul Leamon, Binh Nguyen
  • Publication number: 20150048285
    Abstract: Nonlinear optic chromophores comprising stabilized radical structures, mixtures thereof, methods for their production, nonlinear optical materials containing such chromophores, and the use of such materials in electro-optic, solar conversion, photovoltaic and all-optical nonlinear devices are described.
    Type: Application
    Filed: May 21, 2014
    Publication date: February 19, 2015
    Applicant: Lightwave Logic, Inc.
    Inventors: Frederick J. GOETZ, JR., Andrew Ashton, JR., Frederick J. Goetz, SR., David F. Eaton, Anthony J. Arduengo, Howard E. Simmons, III, Jason W. Runyon
  • Publication number: 20140246659
    Abstract: An organic electroluminescent element including a substrate, a pair of electrodes including an anode and a cathode, disposed on the substrate, and at least one organic layer including a light emitting layer, disposed between the electrodes, in which a compound represented by the following formula (I) is contained in any layer of the at least one organic layer. The organic electroluminescent element has high luminous efficiency and a strong effect of improving the durability by driving aging: wherein X, A1, A2, A3, A4, and R1 to R8 are as defined herein.
    Type: Application
    Filed: August 6, 2012
    Publication date: September 4, 2014
    Applicant: UDC IRELAND LIMITED
    Inventors: Koji Takaku, Tetsu Kitamura, Toru Watanabe, Yosuke Yamamoto, Kimiatsu Nomura, Wataru Sotoyama, Saki Takada, Toshihiro Ise
  • Publication number: 20140174537
    Abstract: The present invention relates to new naphthalene carbodiimide (NTCDI) derivatives, and organic electronic device using the same and especially to an organic solar cell. The new NTCDI derivatives are used as acceptor, electron transport material, and doped electron transport materials.
    Type: Application
    Filed: June 7, 2012
    Publication date: June 26, 2014
    Applicant: Novaled AG
    Inventor: Omrane Fadhel
  • Patent number: 8741448
    Abstract: Disclosed is a fullerene derivative having a formula of F-Cy, wherein F is an open-cage fullerene, and Cy is a chalcogenyl group. The fullerene derivative can be applied to hydrogen storage material and an optoelectronic device such as an organic light emitting diode (OLED), a solar cell, or an organic thin film transistor (TFT).
    Type: Grant
    Filed: August 9, 2011
    Date of Patent: June 3, 2014
    Assignee: Industrial Technology Research Institute
    Inventors: Chih-Ping Chen, Yeu-Ding Chen, Shih-Ching Chuang, Yu-Wei Lin, Fu-Wei Chan
  • Publication number: 20130345425
    Abstract: NLO chromophores of the form of Formula I: and the commercially acceptable salts, solvates and hydrates thereof, wherein Z1-4, X1-4, ?1-2, D and A have the definitions provided herein.
    Type: Application
    Filed: December 27, 2012
    Publication date: December 26, 2013
    Applicant: LIGHTWAVE LOGIC, INC.
    Inventor: LIGHTWAVE LOGIC, INC.
  • Publication number: 20130304089
    Abstract: The present invention relates to compounds which are perylenequinone derivatives, their stereoisomers and atropisomers. These compounds can be particularly useful as photosensitizers or sononsensitizers in photodynamic or sonodynamic therapy. The invention also relates to various methods for using these compounds in photodynamic and/or sonodynamic therapy. The compounds also are useful as therapeutic agents for treating various hyperproliferative disorders.
    Type: Application
    Filed: March 11, 2013
    Publication date: November 14, 2013
    Inventors: Sanjay K. Sharma, Thomas Woo, Selvaraj Naicker
  • Publication number: 20130296564
    Abstract: Herein we describe compositions and methods for the synthesis of [2.2.2]-diazabicyclic structures comprising a domino reaction sequence involving aldol condensation, alkene isomerization, and intramolecular hetero-Diels-Alder cycloaddition. Excellent diastereofacial control during the cycloaddition is enforced with a removable chiral phenyl aminal diketopiperazine substituent. The reaction sequence rapidly generates molecular complexity and is competent with both enolizable and non-enolizable aldehyde substrates. This method provides an efficient route to [2.2.2]-diazabicyclic structures, common to bioactive prenylated indole alkaloids such as the brevianamides and stephacidins.
    Type: Application
    Filed: May 1, 2013
    Publication date: November 7, 2013
    Applicant: College of William and Mary
    Inventor: Jonathan R. Scheerer
  • Publication number: 20130289030
    Abstract: The present invention is directed to novel compounds of formula I and their use as anti-angiogenic agents and anti-cancer agents.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 31, 2013
    Applicants: UNIVERSITE LIBRE DE BRUXELLES, UNIVERSITE CATHOLIQUE DE LOUVAIN
    Inventors: Olivier Feron, Olivier Riant, Robert Kiss, Joelle Leclercq, Gabrielle Chataigne, Nicolas Vandelaer, Carole Lamy
  • Patent number: 8569303
    Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: October 29, 2013
    Assignee: Celtaxsys, Inc.
    Inventors: Damian O Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J Kochanny, Amy Liang, David Light, John Parkinson, David Vogel, Guo Ping Wei, Bin Ye
  • Patent number: 8552201
    Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: October 8, 2013
    Assignee: Sanofi
    Inventors: Jean-Michel Altenburger, Valérie Fossey, Philip Janiak, Gilbert Lassalle, Frédéric Petit, Jean Claude Vernieres
  • Publication number: 20130217672
    Abstract: A (+)-3-hydroxymorphinan-based polycycle derivative of formula (I) is effective as a neuroprotective agent for neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, and ischemic stroke.
    Type: Application
    Filed: May 13, 2011
    Publication date: August 22, 2013
    Applicant: GREEN CROSS CORPORATION
    Inventors: Jinhwa Lee, Jong Yup Kim, Jeongmin Kim, Kwang Woo Ahn
  • Publication number: 20130216909
    Abstract: An electrode active material is based on an organic compound containing in the structural unit thereof a pyrazine structure bound to cycloalkane. The electrode active material and a secondary battery containing it have large energy density, outputting high power, and having excellent cycle characteristics with little reduction in capacity even after repetition of charging and discharging.
    Type: Application
    Filed: March 28, 2013
    Publication date: August 22, 2013
    Applicants: Nard Institute, Ltd., Murata Manufacturing Co., Ltd.
    Inventors: Murata Manufacturing Co., Ltd., Nard Institute, Ltd.
  • Patent number: 8435992
    Abstract: Methods for treating cancer by using compound PM00104, in particular, for treating multiple myeloma are provided.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: May 7, 2013
    Assignee: Pharma Mar S.A.
    Inventors: Enrique Ocio, Atanasio Pandiella, Jesús San Miguel, Pablo Manuel Avilés Marín
  • Patent number: 8404692
    Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof, wherein Z is NR11, NHCO, NHSO2, NHCH2, CH2, CH2CH2, or CH?CH; X is a hydrocarbyl group optionally substituted by one or more R12 groups; R10 and R11 are each independently II or alkyl; R1-R4 are each independently II or (CII2)mR12, where m is O, 1, 2, or 3; each R12 is independently (CH2)aR16, where each R16 is independently selected from O(CH2)bR13, R13, COR13, COOR13, CN, CONR13R14, NR13R14, NR13COR14, SR13, SOR13, SO2R13, NR13SO2R14, SO2OR13, SO2NR13R14, halogen, CF3, and NO2, and wherein each a is 0, 1, 2, or 3 and b is 0, 1, 2, or 3; R13 and R14 are each independently H or (CH2)aR15, where n is 0, 1, 2, or 3; and each R15 is independently selected from alkyl, cycloalkyl, heteroaryl, aralkyl, aryl and heterocycloalkyl, each of which may be optionally substituted by one or more substituents selected from halogen, OH, CN, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(
    Type: Grant
    Filed: October 9, 2006
    Date of Patent: March 26, 2013
    Assignee: Cyclacel Limited
    Inventors: Stuart Jones, Robert Westwood, Mark Thomas, Janice McLachlan, Kenneth Duncan, Fred Scaerou, Daniella I. Zheleva
  • Patent number: 8388872
    Abstract: The present invention provides a photochromic material which is an indeno-fused naphthopyran of structural formulas I or II, having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic material.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: March 5, 2013
    Assignee: Transitions Optical, Inc.
    Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank F. Molock, Jr., Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
  • Publication number: 20120305919
    Abstract: Disclosed is a fullerene derivative having a formula of F-Cy, wherein F is an open-cage fullerene, and Cy is a chalcogenyl group. The fullerene derivative can be applied to hydrogen storage material and an optoelectronic device such as an organic light emitting diode (OLED), a solar cell, or an organic thin film transistor (TFT).
    Type: Application
    Filed: August 9, 2011
    Publication date: December 6, 2012
    Inventors: Chih-Ping CHEN, Yeu-Ding Chen, Shih-Ching Chuang, Yu-Wei Lin, Fu-Wei Chan
  • Patent number: 8314091
    Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.
    Type: Grant
    Filed: August 19, 2008
    Date of Patent: November 20, 2012
    Assignees: MSD OSS B.V., Pharmacopeia, Inc.
    Inventors: Koc-Kan Ho, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer, Andrew John Cooke, Andrew Stanley Edwards, David Jonathan Bennett
  • Patent number: 8283474
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituent
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: October 9, 2012
    Assignee: Glaxo Group Limited
    Inventors: Anna Maria Capelli, Giovanna Tedesco
  • Patent number: 8269004
    Abstract: NLO chromophores of the form of Formula (I): and the acceptable salts, solvates and hydrates thereof, wherein Z1-4, X1-4, ?1-2, D, A and R have the definitions provided herein.
    Type: Grant
    Filed: October 26, 2005
    Date of Patent: September 18, 2012
    Inventors: Frederick J. Goetz, Frederick J. Goetz, Jr.
  • Patent number: 8268457
    Abstract: Disclosed is a novel compound useful as a constituent of an organic EL device. Also disclosed is a practical organic EL device using this compound. This organic EL device has low driving voltage, long life, and reduced leakage current. Specifically disclosed is a compound characterized by having at least one structure (1) shown below in a molecule.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: September 18, 2012
    Assignees: Idemitsu Kosan Co., Ltd., Sony Corporation
    Inventors: Yoshiaki Aoyama, Hironobu Morishita, Chishio Hosokawa, Shigeyuki Matsunami, Yasunori Kijima
  • Patent number: 8247550
    Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: August 21, 2012
    Assignee: Gilead Connecticut, Inc.
    Inventors: Peter A. Blomgren, Kevin S. Currie, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Zhongdong Zhao, Pavel E. Zhichkin, Douglas G. Stafford, Jeffrey E. Kropf
  • Patent number: 8183262
    Abstract: The present invention relates to compounds of formula (I), a process for the manufacture thereof, pharmaceutical compositions containing them, and their use for treating CNS disorders: wherein A, B, X, Y, R1, R2, R3 and R4 are as defined in the description and claims.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: May 22, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Silvia Gatti McArthur, Erwin Goetschi, Juergen Wichmann, Thomas Johannes Woltering
  • Patent number: 8147725
    Abstract: The present invention provides a photochromic material which is an indeno-fused naphthopyran having a pi-conjugation extending group bonded to the 11-position of the indeno-fused naphthopyran, the pi-conjugation extending group having at least one pendent halo-substituted group bonded thereto. The pi-conjugation extending group extends the pi-conjugation system of said indeno-fused naphthopyran. The 13-position of the indeno-fused naphthopyran is substantially free of spiro-substituents. The invention further provides photochromic materials of specified structure, photochromic compositions, photochromic articles and optical elements that include the photochromic material.
    Type: Grant
    Filed: September 1, 2010
    Date of Patent: April 3, 2012
    Assignee: Transitions Optical, Inc
    Inventors: Anu Chopra, Jun Deng, Beon-Kyu Kim, David B. Knowles, Frank Molock, Victor A. Montes, Stephen D. Straight, Wenjing Xiao, Huayun Yu
  • Patent number: 8133847
    Abstract: The present invention relates to a method of controlling plants or inhibiting plant growth which comprises applying to the plants or to the locus thereof a herbicidally effective amount of a compound of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to herbicidal compositions comprising compounds of formula (I) and to certain novel pyrido[2,3-b]pyrazines.
    Type: Grant
    Filed: July 16, 2007
    Date of Patent: March 13, 2012
    Assignee: Syngenta Limited
    Inventors: Neil Brian Carter, Matthew Robert Cordingley, Patrick Jelf Crowley, Michael Drysdale Turnbull
  • Patent number: 8044053
    Abstract: The present invention relates to substituted pyrazoline compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: October 25, 2011
    Assignee: Laboratories del Dr. Esteve, S.A.
    Inventors: Helmut Buschmann, Antonio Torrens-Jover, Josef Mas-Prio, Susana Yenes-Minguez
  • Publication number: 20110203649
    Abstract: The present invention relates to an organic solar cell which comprises at least one photoactive region which comprises at least one indanthrene compound which is in contact with at least one fullerene compound, and to the use of indanthrene compounds in organic photovoltaics, especially in the form of a component cell of a tandem cell.
    Type: Application
    Filed: February 17, 2011
    Publication date: August 25, 2011
    Applicant: BASF SE
    Inventors: Martin Könemann, Regina Höh, Jae Hyung Hwang, Christian Dörr, JianQiang Qu, Gerd Weber, Gabriele Mattern, Peter Erk
  • Patent number: 7994423
    Abstract: Briefly described, embodiments of this disclosure include charge-transport materials, methods of forming charge-transport materials, and methods of using the charge-transport materials.
    Type: Grant
    Filed: June 14, 2005
    Date of Patent: August 9, 2011
    Assignee: Georgia Tech Research Corporation
    Inventors: Seth Marder, Bilal Kaafarani, Steve Barlow, Bernhard Kippelen, Benoit Domercq, Qing Zhang, Takeshi Kondo
  • Publication number: 20110178301
    Abstract: NLO chromophores of the form of Formula I: and the commercially acceptable salts, solvates and hydrates thereof, wherein Z1-4, X1-4, ?1-2, D and A have the definitions provided herein.
    Type: Application
    Filed: April 1, 2011
    Publication date: July 21, 2011
    Inventors: Frederick J. Goetz, Fred J. Goetz, JR.
  • Patent number: 7947683
    Abstract: The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: May 24, 2011
    Assignee: Glaxo Group Limted
    Inventors: Giorgio Bonanomi, Anna Checchia, Elettra Fazzolari, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Silvia Terreni
  • Publication number: 20110105515
    Abstract: (+)-Avrainvillamide, a naturally occurring alkaloid with antiproliferative activity, is shown to bind to the oncoprotein nucleophosmin. Nucleophosmin is known to regulate the tumor suppressor protein p53 and is overexpressed in many different human tumors. The invention provides methods of modulating nucleophosmin and p53 using (+)-avrainvillamide and analogues thereof. These compounds may provide leads for the development of novel anti-cancer therapies that target nucleophosmin.
    Type: Application
    Filed: July 24, 2008
    Publication date: May 5, 2011
    Applicant: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, Jeremy Earle Wulff, Romain Siegrist, Carl Friedrich Nising, Kok Ping Chan
  • Publication number: 20110092495
    Abstract: The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.
    Type: Application
    Filed: December 9, 2010
    Publication date: April 21, 2011
    Applicant: ASTRAZENECA AB
    Inventors: Gloria Breault, Charles Joseph Eyermann, Bolin Geng, Marshall Morningstar, Folkert Reck
  • Patent number: 7919493
    Abstract: This invention relates to antitumoral ecteinascidin derivatives that contain a fused ecteinascidin five ring system with a 1,4-bridge having the structure of formula (VIa) or (VIb) as described herein and compounds in which the —NH2 or —OH of the 1,4-bridge is derivatized, and related pharmaceutical compositions and methods. Such ecteinascidin derivatives include, but are not limited to, those compounds having formula (XVIIb): in which R1 and R4 together form a group of formula (VIa) or (VIb) as described herein, and R5, R7, R8, R14a, R14b, R15, and R21 are as defined herein.
    Type: Grant
    Filed: April 10, 2007
    Date of Patent: April 5, 2011
    Assignee: Pharma Mar, S.A.
    Inventors: Maria Flores, Andres Francesh, Pilar Gallego, Jose Luis Chicharro, Maria Zarzuelo, Carolina Fernandez, Ignacio Manzanares
  • Publication number: 20110026117
    Abstract: A family of bisacenaphthopyrazinoquinoxaline derivatives of formula (I) and (II) is disclosed. These compounds are capable of forming liquid crystal systems that can produce optically isotropic or anisotropic films with desirable optical properties: (I), (II) wherein Ri, R2, Rs, R4, R5 and R& are each independently selected from —H, —SO3M, —OH, —NH2, —Cl, —Br, —I, —NO2, —F, —CF3, —CN, —COOH, —CONH2, alkyl, aryl, alkynyl, alkenyl, alkoxyl, alkylamino, phenoxyl, and phenylamino groups; M is one or more counter ions; j is the number of counter ions associated with the compound; and n is an integer in the range of 1 to S.
    Type: Application
    Filed: March 30, 2009
    Publication date: February 3, 2011
    Inventors: Shijun Zheng, Zongcheng Jiang, Joshua Tillema, Robert Ramirez
  • Patent number: 7820838
    Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxycarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
    Type: Grant
    Filed: July 24, 2008
    Date of Patent: October 26, 2010
    Assignee: Japan Science and Technology Agency
    Inventors: Tohru Fukuyama, Toshiyuki Kan
  • Patent number: 7812024
    Abstract: The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impaired glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.
    Type: Grant
    Filed: May 14, 2007
    Date of Patent: October 12, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guohua Zhao, Chet Kwon, Philip D. Stein
  • Patent number: 7807833
    Abstract: An intermediate compound for total synthesis of ecteinascidins comprising, a compound represented by general formula 2 having thioether group at C4 site, and the substituent R2 of N12 site is trichloroethoxicarbonyl (Troc) to which various substituents can be introduced by mild condition, further having 10 members ring structure which can be converted to a ring of other numbered members.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: October 5, 2010
    Assignee: Japan Science and Technology Agency
    Inventors: Tohru Fukuyama, Toshiyuki Kan
  • Patent number: 7795260
    Abstract: Ecteinascidin compounds with a quinone ring for ring E are active as anti-cancer agents. Related processes and compounds are provided.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: September 14, 2010
    Assignee: Pharma Mar, S.A.
    Inventors: Valentin Martinez Barrasa, Pilar Gallego, Carmen Cuevas, Simon Munt, Ignacio Manzanares, Roberto Menchaca, Natividad Rodriguez, Alberto Rodriguez
  • Patent number: 7737145
    Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
    Type: Grant
    Filed: December 22, 2006
    Date of Patent: June 15, 2010
    Assignee: Estrellita Pharmaceuticals, LLC
    Inventors: Damian Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, David Vogel, Guo Ping Wei, Bin Ye
  • Patent number: 7718586
    Abstract: Disclosed is composition useful for reducing the concentration of mercaptans in hydrocarbons comprising: (A) a first diazo component and (B) a second component comprising a nucleophilic acceptor. The composition can be added to hydrocarbons such as fuel oil to reduce mercaptans without increasing turbidity or color. Triethylene diamine and 1,2-epoxyhexadecane are disclosed to be exemplary diazo and nucleophilic acceptor components.
    Type: Grant
    Filed: February 11, 2004
    Date of Patent: May 18, 2010
    Assignee: Baker Hughes Incorporated
    Inventors: John A. Schield, Weldon John Cappel
  • Publication number: 20100075911
    Abstract: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes.
    Type: Application
    Filed: March 13, 2009
    Publication date: March 25, 2010
    Applicant: TETRALOGIC PHARMACEUTICALS CORPORATION
    Inventors: Stephen M. CONDON, Matthew G. LaPORTE, Yijun DENG, Susan R. RIPPIN
  • Publication number: 20100047178
    Abstract: The present invention relates to compounds which are perylenequinone derivatives, their stereoisomers and atropisomers. These compounds can be particularly useful as photosensitizers or sononsensitizers in photodynamic or sonodynamic therapy. The invention also relates to various methods for using these compounds in photodynamic and/or sonodynamic therapy. The compounds also are useful as therapeutic agents for treating various hyperproliferative disorders.
    Type: Application
    Filed: July 28, 2006
    Publication date: February 25, 2010
    Applicant: QUEST PHARMATECH INC.
    Inventors: Sanjay K. Sharma, Thomas Woo, Selvaraj Naicker
  • Patent number: 7662487
    Abstract: The invention aims at providing a novel azaaromatic compound having an azafluoranthene skeleton which is useful as the constituent of organic EL devices and at realizing a long lifetime, high-efficiency and practical organic EL device by using the compound in at least one of the organic compound layers.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: February 16, 2010
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventor: Toshihiro Iwakuma
  • Publication number: 20090274657
    Abstract: The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Application
    Filed: April 30, 2009
    Publication date: November 5, 2009
    Inventors: Yonghua Gai, Dong Liu, Joel D. Moore, Yat Sun Or, Zhe Wang
  • Patent number: RE41614
    Abstract: The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHC(?O)R? NHC(?O)R?, CN, halogen, ?O, C(?O)H, C(?O)R?, CO2H, CO2R?, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R? groups is independently selected from the group consisting of H, OH, NH2, NO2, SH, CN, halogen, ?O, C(?O)H, C(?O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R7 and R8 may be are joined into a carbocyclic or heterocyclic ring system; and wherein X1 and X2 are each independently defined as above for R1-R8 R1-R6 and R9, and each further includes s
    Type: Grant
    Filed: December 17, 2003
    Date of Patent: August 31, 2010
    Assignee: President and Fellows of Harvard College
    Inventor: Elias J. Corey