Tricyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 548/427)
  • Publication number: 20120119171
    Abstract: A near-infrared absorbing dye has an anion of formula (1) wherein A1 is H or CF3, R0 is OH or —OC(?O)—R?, and R? is a monovalent hydrocarbon group. The dye has excellent solvent solubility as well as good optical properties and heat resistance, offering the advantages of easy coating and effective working during film formation. The dye free of heavy metal in its structure is advantageously used in the process of fabricating semiconductor devices.
    Type: Application
    Filed: May 16, 2011
    Publication date: May 17, 2012
    Inventors: Masaki OHASHI, Takeshi Kinsho, Kazumi Noda, Seiichiro Tachibana
  • Patent number: 8168282
    Abstract: The present invention relates to a trimethine cyanine represented by the formula (1): wherein each of the symbols are defined in the specification. The present invention also relates to a use of the above dimeric trimethine cyanine compound as a dye, which is used in an optic element, particularly a high density recordable optical media.
    Type: Grant
    Filed: October 19, 2008
    Date of Patent: May 1, 2012
    Assignee: Orgchem Technologies, Inc.
    Inventors: Chin Kang Sha, Cheng Fen Yang, Hsin Jen Lee
  • Patent number: 8158275
    Abstract: Fluorinated compounds of the invention are represented by the following general formula (I): (in formula (I), Ar1 and Ar2 each independently represent a C10 or greater aromatic hydrocarbon or C4 or greater heterocyclic group, R1 represents hydrogen or a monovalent substituent, R2 and R3 each independently represent a monovalent substituent, and s1 and t1 each independently represent an integer of 0 or greater. When s1 is 2 or greater, the multiple R2 groups may be the same or different, and when t1 is 2 or greater the multiple R3 groups may be the same or different.
    Type: Grant
    Filed: February 22, 2007
    Date of Patent: April 17, 2012
    Assignees: Osaka University, Sumitomo Chemical Company, Limited
    Inventors: Yutaka Ie, Yoshio Aso, Masashi Nitani, Masato Ueda
  • Publication number: 20120088262
    Abstract: Cyanine compounds having the general formula I, conjugates, complexes, and compositions comprising the cyanine compounds are provided. Fluorescence resonance energy transfer (FRET) dye pairs and viability dyes are also provided.
    Type: Application
    Filed: October 6, 2011
    Publication date: April 12, 2012
    Applicant: Millipore Corporation
    Inventors: Ali Dehghani, Kamala Tyagarajan, Kimvan Tran
  • Publication number: 20120077986
    Abstract: The present invention is directed to provide a novel preparation of anticancer-active tricyclic compounds via alkyne coupling reaction. The present invention provides a process for preparing a compound of formula (Ia) or (Ib): wherein R1 is optionally substituted C1-6 alkyl, etc.; W is O, S or NR2; R2 is hydrogen atom, etc., which comprises Step (a) in which a compound of formula (II): wherein R1 is the same as defined above, and a compound of formula (III) or (IV): wherein R2 is the same as defined above; R3 is hydrogen atom, etc.; X is halogen atom, etc., are reacted in the presence of a base, a copper catalyst and a palladium catalyst in an aprotic polar solvent.
    Type: Application
    Filed: July 26, 2011
    Publication date: March 29, 2012
    Applicant: TAHEEBO JAPAN CO., LTD.
    Inventors: Akira IIDA, Kazunori UEDA, Mitsuaki YAMASHITA
  • Publication number: 20120058482
    Abstract: The invention provides a novel class of cyanine dyes that are functionalized with a linker moiety that facilitates their conjugation to other species and substituent groups which increase the water-solubility, and optimize the optical properties of the dyes. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.
    Type: Application
    Filed: August 25, 2011
    Publication date: March 8, 2012
    Applicant: Pacific Biosciences of California, Inc.
    Inventors: Gene Shen, Stephen Yue
  • Publication number: 20120052506
    Abstract: The invention provides a novel class of cyanine dyes that are functionalized with sulfonic acid groups and a linker moiety that facilitates their conjugation to other species and substituent groups which increase the water-solubility, and optimize the optical properties of the dyes. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.
    Type: Application
    Filed: August 25, 2011
    Publication date: March 1, 2012
    Applicant: Pacific Biosciences of California, Inc.
    Inventors: Stephen Yue, Gene Shen, David Sun
  • Patent number: 8119816
    Abstract: The present invention provides a blue laser light-absorbent substance, which is suitably used in organic photo conductor, laser optical data carrier or organic light-emitting diodes. The blue laser light-absorbent substance includes a merocyanine compound of the general formula (1) wherein n is an integer of from 0 to 3; R1 is unsubstituted or phenyl-, halogen-, ester-, siliy-substituted linear or branched alkyl group having 1 to 6 carbon atoms; R2 is unsubstituted or substituted phenyl, benzyl or naphthyl; N and R1R2 together represent aromatic-fused N-containing heterocyclic group (NR1R2); Y1 is unsubstituted or substituted alkoxy group having 1 to 8 carbon atoms; Y2 is cyano, nitro, halogen or carboxylate; or O and Y1Y2 together represent epoxy or N-containing heterocyclic hydrocarbonyl ketone (OY1Y2).
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: February 21, 2012
    Assignee: Taiwan Fluoro Technology Co., Ltd.
    Inventors: Fu-Shing Wang, Kuang-Mei Hsu
  • Patent number: 8106392
    Abstract: An object is to provide a novel anthracene derivative. Another object is to provide a light-emitting element with high luminous efficiency. Yet another object is to provide a light-emitting element with a long lifetime. Still another object is to provide a light-emitting device and an electronic device having a long lifetime by using the light-emitting elements of the present invention. The anthracene derivative represented by General Formula (1) is provided. The ability of the anthracene derivative represented by General Formula (1) to exhibit high luminous efficiency allows the production of a light-emitting element with high luminous efficiency and a long lifetime.
    Type: Grant
    Filed: November 23, 2010
    Date of Patent: January 31, 2012
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Masakazu Egawa, Harue Nakashima, Sachiko Kawakami, Tsunenori Suzuki, Ryoji Nomura
  • Publication number: 20120022096
    Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.
    Type: Application
    Filed: July 7, 2011
    Publication date: January 26, 2012
    Applicant: Board of Regents of The University of Texas System
    Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
  • Publication number: 20110309348
    Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein R1 through R9 are defined as in the specification.
    Type: Application
    Filed: June 20, 2011
    Publication date: December 22, 2011
    Applicant: Samsung Mobile Display Co., Ltd.
    Inventors: Yoon-Hyun KWAK, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jong-Hyuk Lee, Hee-Joo Ko
  • Patent number: 8076348
    Abstract: [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.
    Type: Grant
    Filed: August 7, 2006
    Date of Patent: December 13, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyoshi Yamada, Hirotsune Itahana, Ayako Moritomo, Takaho Matsuzawa, Eisuke Nozawa, Shinobu Akuzawa, Koichiro Harada
  • Publication number: 20110297919
    Abstract: A heterocyclic compound represented by Formula 1 or Formula 2 below and an organic light-emitting device including the heterocyclic compound: wherein X1, X2, and R1 through R16 are defined as in the specification.
    Type: Application
    Filed: May 9, 2011
    Publication date: December 8, 2011
    Applicant: Samsung Mobile Display Co., Ltd.
    Inventors: Yoon-Hyun KWAK, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jong-Hyuk Lee, Hyung-Jun Song
  • Patent number: 8071388
    Abstract: The invention provides compositions and methods for the detection of biological targets, (e.g. nucleic acids and proteins) by nucleic acid-templated chemistry, for example, by generating fluorescent polymethine dyes.
    Type: Grant
    Filed: February 24, 2009
    Date of Patent: December 6, 2011
    Assignee: Ensemble Therapeutics Corporation
    Inventors: Yumei Huang, James M. Coull
  • Publication number: 20110286933
    Abstract: The present invention provides symmetric carbocyanine dyes and dye precursors useful for fluorescence microscopy, and methods of making and using same.
    Type: Application
    Filed: November 9, 2009
    Publication date: November 24, 2011
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Scott A. Hilderbrand, Ralph Weissleder, Fangwei Shao
  • Publication number: 20110280890
    Abstract: The present invention provides prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group containing a sulfonic acid containing phenyl carbamate, in which the protecting group confers enhanced water solubility upon the prodrug, and in which the prodrug also has a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody, and for the therapeutic use of such prodrug and conjugates, and for processes for preparing such prodrugs and conjugates.
    Type: Application
    Filed: July 15, 2011
    Publication date: November 17, 2011
    Applicant: IMMUNOGEN, INC.
    Inventors: Robert ZHAO, Ravi V. J. CHARI
  • Patent number: 8058453
    Abstract: A cost-effective, industrially feasible process for the manufacture of crystalline Carvedilol Form-II using novel Carvedilol salts comprises the steps of reacting 4-(2,3-epoxy propoxy)carbazole (II) with 2-(2-methoxy phenoxy)ethyl amine (III) followed by acidification with mineral acid in presence of an organic solvent to yield acid addition salts, treatment of the said salts with base(s) in presence of organic solvent(s), water and isolation from the organic solvent(s) followed by crystallization from ethyl acetate.
    Type: Grant
    Filed: December 22, 2008
    Date of Patent: November 15, 2011
    Assignee: Matrix Laboratories Ltd.
    Inventors: Gorantla Seeta Ramanjaneyulu, Indukuri Venkata Sunil Kumar, Ketavarapu Narasimha Rao, Jammula Vera Venkata Krishna Kishore
  • Publication number: 20110265878
    Abstract: The present invention relates to a dye comprising a chromophore to which an acyloin group as anchoring group is attached, to a method of synthesis of such dye, to an electronic device comprising such dye and to the use of such dye.
    Type: Application
    Filed: September 23, 2009
    Publication date: November 3, 2011
    Applicant: Sony Corporation
    Inventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Markus Obermaier
  • Patent number: 8049018
    Abstract: The present invention provides novel organic compounds, which absorb the light in the ultra violet and the infrared regions, have improved light tolerance and solubility in solvents, and have thermal tolerance suitable for uses to which the organic compounds are applied, and provides uses of the same. The above objects are solved by providing indolenine compounds and methine dyes, which have a bis-indolenine skeleton composed of two indolenine rings linked together at their respective C-3 positions via a divalent linking group, and by providing optical recording media containing the methine dyes.
    Type: Grant
    Filed: November 7, 2006
    Date of Patent: November 1, 2011
    Assignee: Kabushiki Kaisha Hayashibara Seibutsu Kagaku Kenkyujo
    Inventors: Yasufumi Dan-Oh, Masahiko Toki, Kentaro Yano, Yasushi Aizawa
  • Publication number: 20110262354
    Abstract: This invention relates generally to cyanine-containing compounds; pharmaceutical compositions comprising cyanine-containing compounds; and methods of using cyanine-containing compounds for cancer cell imaging, cancer cell growth inhibition, and detecting cancer cells, for example. Compounds of the invention are preferentially taken up by cancer cells as compared to normal cells. This allows many uses in the cancer treatment, diagnosis, tracking and imaging fields.
    Type: Application
    Filed: July 10, 2008
    Publication date: October 27, 2011
    Inventors: Leland W. K. Chung, Ruoxiang Wang, Haiyen E. Zhau, Lucjan Strekowski, Maged Henary, Gabor Patonay, James J. Krutak, Xiaojian Yang, Guodong Zhu
  • Publication number: 20110254436
    Abstract: Disclosed is a triphenylene based aromatic compound, wherein a benzene center is substituted with a triphenylene group and another aromatic group such as triphenylenyl, pyrenyl, phenylvinyl, carbazolylphenyl, or arylanthryl in the meta position of the benzene center. The meta-substituted aromatic compound of the invention has better thermal stability (Tg) than the conventional para-substituted aromatic compound. The meta-substituted aromatic compound, served as a hole transporting layer or a host material applied in a light emitting layer in an OLED, is more preferable than the conventional para-substituted aromatic compound.
    Type: Application
    Filed: April 18, 2010
    Publication date: October 20, 2011
    Applicant: NATIONAL TSING HUA UNIVERSITY
    Inventors: Chien-Hong Cheng, Fang-Iy Wu, Yin-Yen Tsai, Yu-Han Chen
  • Publication number: 20110230651
    Abstract: The present invention is related to derivatives of benzenesulfonamide represented by formula (I), and the pharmaceutical composition thereof. In addition, the benzenesulfonamide derivatives disclosed in the present invention can serve as potential cell cycle inhibitors, and thereby these benzenesulfonamide derivatives and the pharmaceutical composition thereof can be antitumor drug candidates, which might aim at cell cycle. Particularly, the benzenesulfonamide derivatives disclosed in the present invention may function as antitumor drugs to treat solid cancers.
    Type: Application
    Filed: February 23, 2011
    Publication date: September 22, 2011
    Applicant: Purzer Pharmaceutical Co., LTD.
    Inventors: Ji-Wang Chern, Grace Shiahuy Chen, Pei-Teh Chang, Kuan-Yu Chen, Meng-Ling Chen, Hsueh-Yun Lee, Chiung Hua Huang, Chun-Tang Chiou
  • Publication number: 20110224334
    Abstract: A near-infrared-ray absorbing material which contains a cyanine compound represented by general formula (I), shows a narrow peak of light absorption in the range of wavelengths of 800-1,000 nm, and has excellent light resistance. In formula (I), R1 to R4, Y1, and Y2 each represents a hydrogen atom, a group of formula (II) or (II?), etc., and Anq? represents a q-valent anion, provided that at least R1 is a group of formula (II) or (II') or Anq? is an ion of formula (III); R11 to R13 each represents a hydrogen atom, hydroxy, etc.; and Z1 and Z2 each represents a C1-10 alkyl, etc. In formula (II?), the bond between G? and T? is a double bond or a conjugated double bond; G? represents a carbon atom; T? represents a carbon atom or a nitrogen atom; the ring including G? and T? represents a 6-membered ring, etc.; w? is 0-4; and R01? represents a hydrogen atom, hydroxy, etc. In formula (III), R5 and R6 each represents a C1-8 haloalkyl.
    Type: Application
    Filed: November 18, 2009
    Publication date: September 15, 2011
    Applicant: ADEKA CORPORATION
    Inventors: Yosuke Maeda, Ryoya Otsuki, Koichi Shigeno
  • Patent number: 8012978
    Abstract: The present invention provides prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group containing a sulfonic acid containing phenyl carbamate, in which the protecting group confers enhanced water solubility upon the prodrug, and in which the prodrug also has a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody, and for the therapeutic use of such prodrug and conjugates, and for processes for preparing such prodrugs and conjugates.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: September 6, 2011
    Assignee: ImmunoGen, Inc.
    Inventors: Robert Zhao, Ravi V. J. Chari
  • Publication number: 20110207767
    Abstract: This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
    Type: Application
    Filed: November 3, 2009
    Publication date: August 25, 2011
    Inventors: Patrick Henry Beusker, Rudy Gerardus Elisabeth Coumans, Ronald Christiaan Elgrtsma, Wiro Michaël Petrus Bernardus Menge, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker, Franciscus Marinus Hendrikus De Groot
  • Patent number: 7989638
    Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.
    Type: Grant
    Filed: July 12, 2010
    Date of Patent: August 2, 2011
    Assignee: AnaSpec Incorporated
    Inventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
  • Publication number: 20110182850
    Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.
    Type: Application
    Filed: April 7, 2010
    Publication date: July 28, 2011
    Inventors: Trixi BRANDL, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic
  • Patent number: 7985552
    Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.
    Type: Grant
    Filed: September 1, 2010
    Date of Patent: July 26, 2011
    Assignee: AnaSpec Incorporated
    Inventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
  • Patent number: 7981919
    Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are hexahydroazepinoindole and octahydroazepinoindole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
    Type: Grant
    Filed: August 5, 2008
    Date of Patent: July 19, 2011
    Assignee: Athersys, Inc.
    Inventors: Youssef L. Bennani, David C. Bom, Michael J. Robarge
  • Publication number: 20110172283
    Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
    Type: Application
    Filed: March 25, 2011
    Publication date: July 14, 2011
    Inventors: Youssef L. Bennani, Bayard Huck, Michael J. Robarge
  • Publication number: 20110155249
    Abstract: A photoelectric conversion device capable of improving conversion efficiency is provided. The photoelectric conversion device includes a work electrode, an opposed electrode, and an electrolyte-containing layer. In the work electrode, a metal oxide semiconductor layer supporting a dye is provided. The dye contains a cyanine compound that has a methine chain, an indolenine skeleton bonded with both ends of the methine chain, and anchor groups introduced to a nitrogen atom included in the indolenine skeleton. Electron injection efficiency to the metal oxide semiconductor layer is improved, and the dye is hardly exfoliated from the metal oxide semiconductor layer.
    Type: Application
    Filed: September 9, 2009
    Publication date: June 30, 2011
    Applicants: TDK CORPORATION, ADEKA CORPORATION
    Inventors: Junji Tanabe, Atsushi Monden, Masahiro Shinkai, Mitsuhiro Okada, Toru Yano, Yohei Aoyama, Yusuke Kubota
  • Patent number: 7968586
    Abstract: The present disclosure provides cytoxic compounds useful as drugs or prodrugs and to drug-cleavable substrate conjugates where the drug and cleavable substrate are optionally linked through a self-immolative linker.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: June 28, 2011
    Assignee: Medarex, Inc.
    Inventors: Sanjeev Gangwar, Bilal Sufi
  • Patent number: 7968587
    Abstract: The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly reduced bones mass, osteoporosis, osteopenia, or reduced muscle mass or strength, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof. X-17142.
    Type: Grant
    Filed: November 6, 2007
    Date of Patent: June 28, 2011
    Assignee: Eli Lilly and Company
    Inventors: Konstantinos Gavardinas, Jonathan Edward Green, Prabhakar Kondaji Jadhav, Donald Paul Matthews
  • Patent number: 7955716
    Abstract: It is an object of the present invention to provide a phosphorescence-emitting material that emits light in a wide visible light range from blue to red and has excellent color purity and reliability, etc. The present invention relates to a metal coordination compound represented by any one of Formulae (1) to (6), B: >NR, >O, >S, >C?O, >SO2, >CR2 (in the formulae, M is Ir, Rh, Ru, Os, Pd, or Pt, and n is 2 or 3; when M is Ir, Rh, Ru, or Os and n is 2, another bidentate ligand further bonds to M; ring A is a cyclic compound containing a nitrogen atom bonded to M.
    Type: Grant
    Filed: June 9, 2004
    Date of Patent: June 7, 2011
    Assignee: Hitachi Chemical Co., Ltd.
    Inventors: Satoyuki Nomura, Yoshii Morishita, Yoshihiro Tsuda
  • Publication number: 20110123450
    Abstract: The sensitivity and specificity of the optical modality can be enhanced by the use of highly absorbing compounds as contrast agents. Novel macrocyclic cyanine and indocyanine bioconjugates that absorb and emit light in the near infrared region of electromagnetic spectrum are disclosed. These compounds are especially useful for endoscopic, localized photoacoustic, and sonofluorescence imaging, detection and therapy of tumors and other abnormalities.
    Type: Application
    Filed: November 2, 2010
    Publication date: May 26, 2011
    Applicant: THE WASHINGTON UNIVERSITY
    Inventors: Samuel Achilefu, Yunpeng Ye
  • Publication number: 20110124856
    Abstract: An aminopropylidene derivative having excellent histamine receptor antagonistic action, a compound which is useful as a pharmaceutical composition, especially as an active ingredient, having alleviated side effects in the central nervous system is described. In the aminopropylidene derivative, R1 and R2, which may be identical or different, stand for a hydrogen, a substituted carbonyl, a substituted carbonylalkyl, and acrylic acid, excluding a case where both are hydrogen; R3 and R4, which may be identical or different, stand for hydrogen, an alkyl which may be substituted with phenyl, or the like; A stands for unsubstituted or an oxo; B stands for a carbon or an oxygen; one of X and Y stands for a carbon and the other stands for a sulfur, a broken line part stands for a single bond or a double bond, and a wavy line stands for cis-form and/or trans-form.
    Type: Application
    Filed: July 31, 2009
    Publication date: May 26, 2011
    Applicant: NIPPON ZOKI PHARMACEUTICAL CO., LTD.
    Inventors: Kunihiko Higashiura, Takashi Ogino, Taizo Ito, Koji Kunimasu, Kazuhito Furukawa
  • Patent number: 7947844
    Abstract: A method of effecting a one-pot conversion of a tetrahydronaphthalic anhydride of formula (I): to a nitrate salt of a benzisoindolenine of formula (II): The method comprises heating the tetrahydronaphthalic anhydride of formula (I) with a reagent mixture comprising ammonium nitrate so as to effecting concomitant dehydrogenation during the conversion.
    Type: Grant
    Filed: February 21, 2010
    Date of Patent: May 24, 2011
    Assignee: Silverbrook Research Pty Ltd
    Inventors: Sutharsiny Indusegaram, Simone Charlotte Vonwiller, Damon Donald Ridley, Kia Silverbrook
  • Publication number: 20110118303
    Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.
    Type: Application
    Filed: April 9, 2009
    Publication date: May 19, 2011
    Applicants: EMS S.A., Universidade Estadual Paulista Julio De Mesquita Filho - UNESP
    Inventors: Ednir de Oliveira Vizioli, Chung Man Chin, Renato Farina Menegon, Lorena Blau, Jean Leandro Dos Santos, Maria do Carmo Longo
  • Publication number: 20110111162
    Abstract: A novel indolium compound of general formula (I) and an optical recording material containing the indolium compound. In formula (I), ring A is a benzene ring, etc.; ring B is a 5- or 6-membered heterocyclic ring; R1 is a group of general formula (II), etc.; R2 is an organic group having 1 to 30 carbon atoms, etc.; Y1 is an alkyl group having 1 to 10 carbon atoms, etc.; Z1 and Z2 are each, e.g., an alkyl group having 1 to 8 carbon atoms optionally substituted with a halogen atom and optionally interrupted by —O—, etc.; a is an integer of 0 to 6; b is an integer of 0 to 5; Anq? is a q-valent anion; q is 1 or 2; and p is a number necessary to neutralize an electric charge.
    Type: Application
    Filed: September 26, 2008
    Publication date: May 12, 2011
    Applicant: ADEKA CORPORATION
    Inventors: Toru Yano, Yohei Aoyama
  • Publication number: 20110112163
    Abstract: A unique class of N-acyl O-amino phenol prodrugs of CBI-TMI and CBI-indole2 were synthesized and shown to be prodrugs, subject to reductive activation by nucleophilic cleavage of a weak N—O bond, effectively releasing the free drug in functional cellular assays for cytotoxic activity approaching or matching the activity of the free drug, yet remain essentially stable to ex vivo DNA alkylation conditions. Most impressively, assessment of the in vivo antitumor activity of a representative O-(acylamino) prodrug, 8, indicate that they approach the potency and exceed the efficacy of the free drug itself (CBI-indole2), indicating that the inactive prodrugs not only effectively release the free drug in vivo, but that they offer additional advantages related to a controlled or targeted release in vivo.
    Type: Application
    Filed: November 13, 2008
    Publication date: May 12, 2011
    Inventor: Dale Boger
  • Publication number: 20110105362
    Abstract: The present invention provides methods and non-fluorescent carbocyanine quencher compounds having the general formula: Wherein the A moiety is a substituted pyridinium, unsubstituted pyridinium, substituted quinolinium, unsubstituted quinolinium, substituted benzazolium, unsubstituted benzazolium, substituted indolinium, or substituted indolinium. The invention further provides luminescent donor molecule-quencher pairs and luminescent donor molecule-quencher-luminescent acceptor molecule conjugates wherein the quencher is a cyanine compound of the present invention. The energy transfer pairs are used to detect an analyte of interest in a sample.
    Type: Application
    Filed: January 12, 2011
    Publication date: May 5, 2011
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Rosaria P. Haugland, Ching-Ying Cheung, Stephen Yue
  • Patent number: 7935722
    Abstract: The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly frailty, osteoporosis, osteopenia, and male and female sexual dysfunction comprising administering to a patient in need thereof an effective amount of a compound of formula (I).
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: May 3, 2011
    Assignee: Eli Lilly and Company
    Inventors: Kevin Robert Fales, Jonathan Edward Green, Prabhakar Kondaji Jadhav, Donald Paul Matthews, David Andrew Neel, Edward C R Smith
  • Patent number: 7935830
    Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: May 3, 2011
    Assignee: Athersys, Inc.
    Inventors: Youssef L. Bennani, Bayard Huck, Michael J. Robarge
  • Patent number: 7927830
    Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.
    Type: Grant
    Filed: May 29, 2008
    Date of Patent: April 19, 2011
    Assignee: Life Technologies Corporation
    Inventors: Ching-Ying Cheung, Stephen Yue, Wai-Yee Leung
  • Publication number: 20110081294
    Abstract: A method of detecting a contrast agent for photoacoustic imaging provides a high signal intensity. In a contrast agent for photoacoustic imaging, each particle containing an inorganic material supports at least an organic dye having an absorption coefficient in the near infrared region by means of chemical bonding.
    Type: Application
    Filed: September 29, 2010
    Publication date: April 7, 2011
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Tatsuki Fukui, Fumio Yamauchi, Satoshi Yuasa, Sachiko Inoue
  • Publication number: 20110070166
    Abstract: Reduced dyes, such as hydrocyanines, deuterocyanines, and/or other deuterated dyes capable of detecting one or more reactive oxygen species are described herein. The reduced dyes exhibit little or no fluorescence due to the disrupted ? conjugation. However, upon reaction with ROS, the reduced dyes are oxidized, regenerating the extended ? conjugation and causing a substantial increase in fluorescence intensity. In many case, the oxidized dye is generally membrane impermeable. However, upon reduction, many of the reduced dyes are membrane permeable. Thus, reduced dyes can accumulate in cells and/or tissue to amplify the signal. Once inside the cell or tissue, the reduced dye is reoxidized upon reaction with ROS, and the oxidized dye again becomes membrane impermeable, trapping the dye within the cell. The reduced dyes can be used to image ROS, such as hydroxide radical and superoxide, in serum, cell cultures, tissue explants, and in vivo.
    Type: Application
    Filed: September 28, 2010
    Publication date: March 24, 2011
    Inventors: Niren Murthy, W. Robert Taylor, Kousik Kundu, Sarah F. Knight, Sungmun Lee
  • Publication number: 20110065767
    Abstract: This invention relates to novel agents that are analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
    Type: Application
    Filed: August 1, 2007
    Publication date: March 17, 2011
    Inventors: Patrick Henry Beusker, Henri Johannes Spijker, Johannes Albertus Frederikus Joosten, Tijl Huijbregts, Franciscus Marinus Hendrikus De Groot
  • Publication number: 20110065896
    Abstract: Subject of the present invention are polyether polyol dendron conjugates comprising a specific polyether polyol dendron moiety, at least one certain fluorescent effector molecule (E). Such polyether polyol dendron conjugates may be used for diagnostic and therapeutic purposes, whereby the optical properties of the at least one certain fluorescent effector molecule are enhanced due to the attachment to the polyether polyol dendron conjugate.
    Type: Application
    Filed: March 10, 2009
    Publication date: March 17, 2011
    Applicant: MIVENION GMBH
    Inventors: Kai Licha, Malte Bahner, Michael Schirner, Rainer Haag, Timm Heek, Monika Wyszogrodzka
  • Patent number: 7906545
    Abstract: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: March 15, 2011
    Assignee: Immunogen Inc.
    Inventors: Robert Yongxin Zhao, Ravi V. J. Chari
  • Patent number: RE42802
    Abstract: Compounds of the general formula I wherein rings B, C, D and E may be present or not and, when present, are combined with A as A+C, A+E, A+B+C, A+B+D, A+B+E, A+C+E, A+B+C+D or A+B+C+D+E, rings B, C and E being aliphatic whereas ring D may be aliphatic or aromatic/heteroaromatic, and wherein X is —(CH2)m—, in which m is an integer 1-3, to form a ring E or, when E is absent, a group R1 bound to the nitrogen atom, wherein R1 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 3 carbon atoms, cycloalkyl(alkyl) groups of 3 to 5 carbon atoms (i.e.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: October 4, 2011
    Assignee: H. Lundbeck A/S
    Inventors: Hâkan Vilheim Wikström, Durk Dijkstra, Bastiaan Johan Venhuis