Tricyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/79)
  • Patent number: 8475939
    Abstract: An m-terphenyl derivative has a structure of formula (I) or (II): wherein A and B are five-membered heterocyclic compounds selected from the group consisting of pyrrole, pyrazole, imidazole, 1,2,3-triazole, 1,2,4-triazole, 1,2,3,4-tetrazole, 1,2-thiazole, 1,3-thiazole and 1,3,4-thiadiazole, each of substituents R, R1 and R2 is a member independently selected from the group consisting of H, halo, cyano, trifluoromethyl, amino, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C20 cycloalkyl, C3-C20 cycloalkenyl, C1-C20 heterocycloalkyl, C1-C20 heterocycloalkenyl, aryl and heteroaryl. The compound of the present invention may have advantages in good electron affinity, low HOMO and thereby achieving hole blocking and may be used for electron transport material and/or electron injection material.
    Type: Grant
    Filed: January 6, 2011
    Date of Patent: July 2, 2013
    Assignee: National Tsing Hua University
    Inventors: Chien-Hong Cheng, Cheng-An Wu, Fang-Iy Wu, Cheng-Hung Shih
  • Patent number: 8476293
    Abstract: The present invention relates to the compound represented by formula (I): (wherein, all the symbols have the same meaning as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.
    Type: Grant
    Filed: April 29, 2011
    Date of Patent: July 2, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuyuki Ohmoto, Masashi Kato, Yoshifumi Kagamiishi, Junichiro Manako
  • Patent number: 8440673
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted pyrazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: May 14, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Patent number: 8431251
    Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including an organic layer that includes the following heterocyclic compound: wherein R1 to R13 are each independently a hydrogen atom, a heavy hydrogen atom, a substituted or unsubstituted C1-C60 alkyl group, a substituted or unsubstituted C2-C60 alkenyl group, a substituted or unsubstituted C2-C60 alkynyl group, a substituted or unsubstituted C3-C60 cycloalkyl group, a substituted or unsubstituted C1-C60 alkoxy group, a substituted or unsubstituted C5-C60 aryloxy group, a substituted or unsubstituted C5-C60 arylthio group, a substituted or unsubstituted C5-C60 aryl group, an amino group substituted with a C5-C60 aryl group or a C3-C60 heteroaryl group, a substituted or unsubstituted C3-C60 heteroaryl group, a substituted or unsubstituted C6-C60 condensed polycyclic group, a halogen atom, a cyano group, a nitro group, a hydroxy group, or a carboxy group.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: April 30, 2013
    Assignee: Samsung Display Co., Ltd.
    Inventors: Jin-O Lim, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Sang-Hyun Han, Chang-Ho Lee, Jong-Hyuk Lee, Hee-Joo Ko
  • Publication number: 20130101684
    Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.
    Type: Application
    Filed: April 15, 2011
    Publication date: April 25, 2013
    Applicant: Chromocell Corporation
    Inventors: Jane V. Leland, Louise Slade, David Hayashi, William P. Jones, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Jessica Langer, Kambiz Shekdar
  • Patent number: 8415031
    Abstract: Compounds comprising an aza-dibenzo moiety and a condensed aromatic moiety having at least three benzene rings are provided. In particular, the compounds may comprise an azadibenzofuran, azadibenzothiophene, or azadibenzoselenophene joined directly or indirectly to an anthracene. The compounds may be used in the electron transport layer of organic light emitting devices to provide devices with improved properties.
    Type: Grant
    Filed: January 24, 2011
    Date of Patent: April 9, 2013
    Assignee: Universal Display Corporation
    Inventors: Chuanjun Xia, Siddharth Harikrishna Mohan, Vadim Adamovich
  • Patent number: 8410130
    Abstract: The present disclosure relates to a series of bis(hydroxymethyl) and its bis(carbamate) of 8H-3a-azacyclopenta[a]indene-1-yl and 5,10-dihydropyrrolo-[1,2-b]isoquinolines derivatives (Formula I-Formula IV) as DNA di-alkylating agents. The preliminary antitumor studies indicated that compounds disclosed herein could exhibit potent cytotoxicity in vitro and antitumor therapeutic efficacy in human tumor xenografts and could have little or no cross-resistance to either Taxol or Vinblastine. The results demonstrated that compounds disclosed herein possess potent antitumor therapeutic efficacy and are expected to have potential for clinical applications.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: April 2, 2013
    Assignee: Academia Sinica
    Inventors: Tsann-Long Su, Ting-Chao Chou
  • Patent number: 8409729
    Abstract: Novel aryl silicon and aryl germanium host materials are described. These compounds improve OLED device performance when used as hosts in the emissive layer of the OLED.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: April 2, 2013
    Assignee: Universal Display Corporation
    Inventors: Lichang Zeng, Alexey B. Dyatkin, Gregg Kottas, Chuanjun Xia, David Z. Li
  • Patent number: 8399108
    Abstract: The present invention relates to a material for an organic electro-optical device and an organic electro-optical device including the same. More particularly, the present invention relates to a material having thermal stability of a glass transition temperature of 120° C. or more and a thermal decomposition temperature of 450° C. or more, and being capable of providing an organic electro-optical device having high efficiency and a long life-span due to less crystallization and improved amorphous properties in a material for an organic electro-optical device. The material for an organic electro-optical device can be used singularly or as a host material in combination with a dopant, and includes an asymmetric fluorene derivative compound. An organic electro-optical device including the material for an organic electro-optical device is also provided.
    Type: Grant
    Filed: May 28, 2008
    Date of Patent: March 19, 2013
    Assignee: Cheil Industries, Inc.
    Inventors: Eun-Sun Yu, Nam-Soo Kim, Young-Hoon Kim, Mi-Young Chae
  • Patent number: 8389131
    Abstract: Provided is an organic electroluminescent device (organic EL device), in which the luminous efficiency of the device is improved, driving stability is sufficiently ensured, and the construction of the device is simple. This organic EL device is an organic electroluminescent device, including a light-emitting layer between an anode and a cathode laminated on a substrate, in which the light-emitting layer contains a phosphorescent light-emitting dopant and an indolocarbazole compound as a host material. Examples of the indolocarbazole compound include a compound represented by the following formula (1).
    Type: Grant
    Filed: March 24, 2010
    Date of Patent: March 5, 2013
    Assignee: Nippon Steel Chemical Co., Ltd.
    Inventors: Takahiro Kai, Masaki Komori, Toshihiro Yamamoto, Megumi Matsumoto
  • Patent number: 8377573
    Abstract: Provided is a compound having a substituted pyridyl group and a pyridoindole ring structure linked through a phenylene group, having formula (1), and an organic EL device with a pair of electrodes and at least one organic layer interposed between the electrodes, wherein the at least one organic layer having the compound:
    Type: Grant
    Filed: January 30, 2009
    Date of Patent: February 19, 2013
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Norimasa Yokoyama, Shuichi Hayashi, Sawa Izumi, Shigeru Kusano
  • Patent number: 8361638
    Abstract: The present invention relates to fluorine derivatives and organic electronic devices in which said compounds are used as a matrix material in the emitting layer and/or as a hole transport material, and/or as an electron blocking or exciton blocking material, and/or as an electron transport material.
    Type: Grant
    Filed: March 11, 2009
    Date of Patent: January 29, 2013
    Assignee: Merck Patent GmbH
    Inventors: Philipp Stoessel, Holger Heil, Dominik Joosten, Christof Pflumm, Anja Gerhard
  • Patent number: 8362030
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.
    Type: Grant
    Filed: March 13, 2009
    Date of Patent: January 29, 2013
    Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.R.L.
    Inventors: Raffaele Ingenito, Philip Jones, Laura Llauger Bufi, Jesus Maria Ontoria Ontoria, Rita Scarpelli
  • Publication number: 20130023521
    Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.
    Type: Application
    Filed: January 17, 2011
    Publication date: January 24, 2013
    Applicant: HYBRIGENICS SA
    Inventors: Roman Lopez, Frederic Colland
  • Publication number: 20130005675
    Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 3, 2013
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kenji OTSUBO, Takahito YAMAUCHI, Yuji OCHI
  • Publication number: 20120329743
    Abstract: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Application
    Filed: June 14, 2012
    Publication date: December 27, 2012
    Inventors: Xianhai Huang, Jason Brubaker, Scott L. Peterson, John W. Butcher, Joshua T. Close, Michelle Martinez, Rachel Nicola MacCoss, Joon O. Jung, Phieng Siliphaivanh, Hongjun Zhang, Robert G. Aslanian, Purakkattle Johny Biju, Li Dong, Ying Huang, Kevin D. McCormick, Anandan Palani, Ning Shao, Wei Zhou
  • Patent number: 8329317
    Abstract: A white light emitting organic electroluminescent element comprising two electrodes having therebetween one or more constituting layers including a light emission layer, the one or more constituting layers comprising at least two phosphorescent compounds, wherein at least one of the phosphorescent compounds is a green light emitting ortho metalated complex; and a spectral ratio of the green light emitting ortho metalated complex in ae emission spectral distribution in a range of 400-800 nm is not less than 60%.
    Type: Grant
    Filed: March 16, 2011
    Date of Patent: December 11, 2012
    Assignee: Konica Minolta Holdings, Inc.
    Inventors: Masato Nishizeki, Tomohiro Oshiyama
  • Patent number: 8293380
    Abstract: A polymer compound containing a structure of the following formula (B): —Ar—??(A) (wherein, Ar represents an arylene group, divalent heterocyclic group, divalent aromatic amine group or divalent group having a metal complex structure.) (wherein, A ring and B ring represent each independently an aromatic ring optionally having a substituent. X1 represents —C(?O)—, —S(?O)—, —S(?O)2—, —P(?O)(R1)—, —C(R1)(R2)—, —C(R2)(R2)—, —B(R1)—, —N(R1)— or —Si(R1)(R1)—. R* represents a hydrogen atom or monovalent or divalent group, R1 represents a hydrogen atom or monovalent group, and R2 represents a monovalent group having a hetero atom. When R1 and R2 are present each in plural number, they may be the same or different).
    Type: Grant
    Filed: December 26, 2005
    Date of Patent: October 23, 2012
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takanobu Noguchi, Hidenobu Kakimoto, Tomoyuki Suzuki
  • Patent number: 8278321
    Abstract: The present disclosure characterizes the activity of Golgicide A (GCA), as a potent, specific and reversible small molecule inhibitor of Golgi BFA resistance factor 1 (GBF1) function. A mutant GBF1 gene that is resistant to GCA is also described. Methods of using GCA and the GCA-resistant GBF1 gene are described including methods for modulating GBF1 activity for research and therapeutic purposes. Also described are compositions incorporating a GCA-resistant GBF1.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: October 2, 2012
    Assignee: Washington University
    Inventor: David B. Haslam
  • Patent number: 8241763
    Abstract: The present invention relates to the compounds of the formulae (1) to (6) and to organic electroluminescent devices, in particular blue-emitting devices, in which these compounds are used as host material or dopant in the emitting layer and/or as hole-transport material and/or as electron-transport material.
    Type: Grant
    Filed: June 20, 2007
    Date of Patent: August 14, 2012
    Assignee: Merck Patent GmbH
    Inventors: Arne Buesing, Philipp Stoessel, Holger Heil
  • Patent number: 8231983
    Abstract: Disclosed is an organic electroluminescent device having high emission luminance, high external quantum efficiency and long lifetime. Also disclosed are a display and an illuminating device.
    Type: Grant
    Filed: March 27, 2006
    Date of Patent: July 31, 2012
    Assignee: Konica Minolta Holdings Inc.
    Inventors: Shuichi Sugita, Tatsuo Tanaka
  • Patent number: 8227610
    Abstract: The disclosure provides, in part, compositions of perfluoro polyether compounds and associated methods for producing cellular labels for tracking cells by MRI and methods for labeling, detecting and quantifying cell numbers in vivo.
    Type: Grant
    Filed: July 10, 2008
    Date of Patent: July 24, 2012
    Assignee: Carnegie Mellon University
    Inventors: Jelena Janjic, Eric T. Ahrens
  • Patent number: 8222269
    Abstract: The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine derivatives of formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: July 17, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher J. Dinsmore, Matthew H. Katcher, Alan B. Northrup
  • Patent number: 8211907
    Abstract: To provide a compound which is useful as an NMDA receptor antagonist. The present inventors have studied a compound having an NMDA receptor antagonistic action, and confirmed that the fused indane compound of the present invention has an excellent NMDA receptor antagonistic action, thereby completed the present invention. The fused indane compound of the present invention has an excellent NMDA receptor antagonistic action and can be used as a prophylactic and/or therapeutic agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, intractable depression, attention deficit hyperactivity disorder, migraines, or the like.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: July 3, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Satoshi Hayashibe, Shingo Yamasaki, Nobuyuki Shiraishi, Hiroaki Hoshii, Takahiko Tobe
  • Publication number: 20120165322
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: June 29, 2011
    Publication date: June 28, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
  • Patent number: 8202880
    Abstract: The compounds of formula I in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings as indicated in the description, are novel effective PDE4 inhibitors.
    Type: Grant
    Filed: August 27, 2008
    Date of Patent: June 19, 2012
    Assignee: NYCOMED GmbH
    Inventors: Ulrich Kautz, Beate Schmidt
  • Patent number: 8173275
    Abstract: The invention provides an azaindenochrysene derivative, and an organic light-emitting device outputting light having high luminance and a long lifetime with high efficiency having an organic compound layer that includes the azaindenochrysene derivative.
    Type: Grant
    Filed: November 5, 2009
    Date of Patent: May 8, 2012
    Assignee: Canon Kabushiki Kaisha
    Inventors: Hiroki Ohrui, Masanori Muratsubaki, Takeshi Sekiguchi, Akihito Saitoh
  • Patent number: 8143269
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: March 27, 2012
    Assignee: Calcimedica, Inc.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Kenneth A. Stauderman, Jack Roos
  • Patent number: 8110583
    Abstract: Compounds of the formula I, in which s, k, I, W, R1, R2, R3, and U have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: May 31, 2006
    Date of Patent: February 7, 2012
    Assignee: Merck Patent GmbH
    Inventors: Wolfgang Staehle, David Bruge, Kai Schiemann, Dirk Finsinger, Hans-Peter Buchstaller, Frank Zenke, Christiane Amendt
  • Patent number: 8097725
    Abstract: The present invention relates to a chemical compound that has applications as a luminescent indicator dye, and to an optical sensor, typically employed for determination of near-neutral pH values of aqueous samples. The optical sensor has particular application in the pH determination of body liquids such as, for example, blood, plasma and serum.
    Type: Grant
    Filed: December 3, 2004
    Date of Patent: January 17, 2012
    Assignee: Roche Diagnostics Operations, Inc.
    Inventors: Huarui He, Mark A. Mortellaro, Susanne T. Young
  • Patent number: 8067473
    Abstract: Disclosed are methods and compositions useful in identifying an E3 ubiquitin ligase inhibitor and modulating cell growth, comprising contacting a cell with an effective amount of an inhibitor of an E3 ubiquitin ligase, and contacting the cell with an effective amount of a topoisomerase inhibitor, wherein the treatment with the E3 ubiquitin ligase inhibitor and topoisomerase inhibitor modulates cell growth in comparison to a cell treated with the topoisomerase inhibitor alone. The present invention further provides methods for identifying and making an E3 ubiquitin ligase inhibitor.
    Type: Grant
    Filed: January 16, 2008
    Date of Patent: November 29, 2011
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Omri Erez, Iris Alchanati, Philippe Nakache
  • Publication number: 20110269705
    Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.
    Type: Application
    Filed: December 4, 2009
    Publication date: November 3, 2011
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kenji Otsubo, Takahito Yamauchi, Yuji Ochi
  • Patent number: 8034944
    Abstract: There are provided a novel benzofluoranthene compound and an organic light-emitting device which uses the benzofluoranthene compound, gives a blue emission hue with extremely good purity, and has an optical output with a high efficiency, a high luminance, and a long life. Specifically, there are provided a benzofluoranthene compound represented by the general formula shown below and an organic light-emitting device including a pair of electrodes including an anode and a cathode one of which is a transparent or translucent electrode material, and an organic compound layer disposed between the pair of electrodes and including a material for an organic light-emitting device containing the benzofluoranthene compound. In the general formula (1), one of X1, X2, X3, X4, X5, and X6 represents a substituted or unsubstituted fused heterocyclic group having four or less rings, and the others of X1, X2, X3, X4, X5, and X6 each represent a hydrogen atom.
    Type: Grant
    Filed: December 12, 2007
    Date of Patent: October 11, 2011
    Assignee: Canon Kabushiki Kaisha
    Inventors: Hiroki Ohrui, Akihito Saitoh, Chika Negishi, Hironobu Iwawaki, Masanori Muratsubaki, Hiroyuki Tomono, Tetsuya Kosuge, Akihiro Senoo
  • Patent number: 8034939
    Abstract: This invention relates to isoindole derivates of Formula I to pharmaceutical compositions comprising such derivatives, and to methods of treatment comprising administering of such derivatives.
    Type: Grant
    Filed: September 28, 2007
    Date of Patent: October 11, 2011
    Assignee: Aventis Pharma S.A..
    Inventors: Patrick Mailliet, Luc Bertin, Didier Benard, Chantal Carrez, François Vallee, Eric Bacque
  • Publication number: 20110201042
    Abstract: The invention relates in part to compounds that act as highly nitric oxide (NO)-specific turn-on fluorescent probes. The present invention also relates to the use of these fluorescein-based sensors to screen selectively for inhibitors of bacterial nitric oxide synthase (bNOS). Compounds of the present invention readily detect nitric oxide produced in vivo. Therefore they can be used in an assay that measures NO production by bNOS. Using a sensor of the invention one can screen libraries of small molecules for inhibitors of bNOS.
    Type: Application
    Filed: December 17, 2008
    Publication date: August 18, 2011
    Applicant: Massachusetts Institute of Technology
    Inventors: Stephen J. Lippard, Lindsey E. McQuade, Evgeny A. Nudler
  • Patent number: 7968716
    Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.
    Type: Grant
    Filed: September 16, 2010
    Date of Patent: June 28, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Guy Brenchley
  • Patent number: 7964726
    Abstract: The present invention relates to the compound represented by formula (I): (wherein, all the symbols has the same meanings as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.
    Type: Grant
    Filed: December 21, 2005
    Date of Patent: June 21, 2011
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuyuki Ohmoto, Masashi Kato, Yoshifumi Kagamiishi, Junichiro Manako
  • Publication number: 20110105512
    Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase AxI. Methods of using the compounds in treating diseases or conditions associated with AxI activity are also disclosed.
    Type: Application
    Filed: July 2, 2009
    Publication date: May 5, 2011
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventor: Rajinder Singh
  • Publication number: 20110105477
    Abstract: The present invention relates to HIV protease, and methods for inhibiting the function of HIV protease. In particular, present invention provides compounds that inhibit or block the biological activity of HIVp, thereby causing the replication of the HIV virus to be inhibited or to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS. The compounds and formulations also find use in diagnostic and research settings.
    Type: Application
    Filed: September 12, 2008
    Publication date: May 5, 2011
    Applicant: The Regents of the University of Michigan
    Inventors: Heather A. Carlson, Kelly L. Damm, Kristen L. Meagher
  • Publication number: 20110092520
    Abstract: The present invention relates to a process for producing a hydrate of 3-(2,6-dichlorophenyl)-4-imino-7-[(2?-methyl-2?,3?-dihydro-1?H-spiro[cyclopropane-1,4?-isoquinolin]-7?-yl)amino]-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one (Compound A) or of a pharmaceutically acceptable salt of Compound A and a crystalline form of Compound A or of a pharmaceutically acceptable salt of Compound A, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.
    Type: Application
    Filed: June 2, 2009
    Publication date: April 21, 2011
    Inventors: Shuntaro Furukawa, Taketo Ikeno, Shinji Kato, Masashi Kawasaki, Hisaki Kojima, Wataru Minagawa, Naotaka Sawada, Fuyuki Yamamoto, Sachin Lohani, Yaling Wang
  • Publication number: 20110092533
    Abstract: The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ER? and ER?). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors.
    Type: Application
    Filed: December 14, 2010
    Publication date: April 21, 2011
    Applicant: STC. UNM
    Inventors: Eric R. PROSSNITZ, Sergey E. Tkatchenko, Chetana M. Revankar, Larry A. Sklar, Jeffrey B. Arterburn, Daniel F. Cimino, Tudor I. Oprea, Cristian-George Bologa, Bruce S. Edwards, Alexander Kiselyov, Susan M. Young
  • Patent number: 7915416
    Abstract: Disclosed are compounds of formula (I), wherein W, R, R1, R2, R3, R4, R5, R6, and R7 have the meanings indicated in claim 1. Said compounds can be used for the treatment of tumors, among other things.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: March 29, 2011
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, David Bruge, Hans-Peter Buchstaller, Dirk Finsinger, Wolfgang Staehle, Christiane Amendt, Ulrich Emde, Frank Zenke
  • Publication number: 20110071136
    Abstract: The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These tricyclic compounds and compositions containing them are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, pathogenic infections, and certain immunological disorders.
    Type: Application
    Filed: September 16, 2010
    Publication date: March 24, 2011
    Applicant: CYLENE PHARMACEUTICALS, INC
    Inventors: Mustapha HADDACH, Fabrice PIERRE
  • Patent number: 7897766
    Abstract: The invention relates to amine-substituted aza-adamantane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. Radiolabelled compounds useful for evaluating the binding affinity to ?7 nicotinic acetylcholine receptors also are described.
    Type: Grant
    Filed: September 7, 2006
    Date of Patent: March 1, 2011
    Assignee: Abbott Laboratories
    Inventors: Michael R. Schrimpf, Kevin B. Sippy, David J. Anderson, William H. Bunnelle, Diana L. Nersesian
  • Patent number: 7875720
    Abstract: Fluorescent monomers are described and claimed which are synthesized by reacting a substituted or non-substituted naphthalic anhydride with an amine and with a moiety containing a polymerizable group. Such monomers are useful for the preparation of tagged treatment polymers. Such tagged treatment polymers are useful as scale inhibitors in industrial water systems.
    Type: Grant
    Filed: September 9, 2003
    Date of Patent: January 25, 2011
    Assignee: Nalco Company
    Inventors: John D. Morris, Barbara E. Moriarty, Mingli Wei, Patrick G. Murray, Jerry L. Reddinger
  • Patent number: 7875721
    Abstract: The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ER? and ER?). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors.
    Type: Grant
    Filed: August 2, 2006
    Date of Patent: January 25, 2011
    Assignee: STC.UNM
    Inventors: Eric R. Prossnitz, Sergey E. Tkatchenko, Chetana M. Revankar, Larry A. Sklar, Jeffrey B. Arterburn, Daniel F. Cimino, Tudor I. Oprea, Cristian-George Bologa, Bruce S. Edwards, Alexander Kiselyov, Susan M. Young
  • Patent number: 7868173
    Abstract: The instant invention relates to novel prodrugs of optically pure benzoquinolizine-2-carboxylic acid and pharmaceutical compositions that include the prodrugs. In particular, the present invention relates to the sulfonic acid salts of L-alanine and L-valine prodrugs of S-(?)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid. The compounds and compositions of the invention can be used to treat bacterial Gram-positive, Gram-negative and anaerobic infections, especially infections caused by resistant Gram-positive organism and Gram-negative organism, mycobacterial infections and emerging nosocomial pathogen infections.
    Type: Grant
    Filed: March 9, 2007
    Date of Patent: January 11, 2011
    Assignee: Wockhardt Limited
    Inventors: Mahesh Vithalbhai Patel, Vijaya Narayan Desai, Prasad Keshav Deshpande, Ravindra Dattatraya Yeole, Rajesh Prabhakar Kale
  • Patent number: 7855295
    Abstract: Tetrahydrocarboline compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the tetrahydrocarboline compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the tetrahydrocarboline compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases.
    Type: Grant
    Filed: January 24, 2005
    Date of Patent: December 21, 2010
    Assignee: Novartis Vaccines and Diagnostics, Inc.
    Inventors: Weibo Wang, Zhi-Jie Ni, Paul Barsanti, Sabina Pecchi, Yi Xia, Nathan Brammeier, Megan C. Phillips, Eliza Jazan, Kelly Wayman, David Dibble, Jie-Kai Cheng
  • Patent number: 7803943
    Abstract: Methods of using dyes and associated technology are provided. A dye, such as a monomeric dye or a dimeric dye, may be used in a nucleic acid gel staining application and/or a nucleic acid detection application. Such a dye and a salt that comprises an anion that is associated with a strong acid and a cation that is associated with a strong base may be used in such an application. A dimeric dye, such as a dimeric dye capable of forming a hairpin-like structure, may be used to stain and/or detect nucleic acids via a release-on-demand mechanism. A dimeric dye having low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, may be used to stain and/or detect nucleic acids.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: September 28, 2010
    Assignee: Biotium, Inc.
    Inventors: Fei Mao, Wai-Yee Leung
  • 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