Benzene Ring In A Substituent E Patents (Class 564/92)
  • Patent number: 10131628
    Abstract: An electrochemical treatment of differently protected aniline or napthylamine results in the preparation of unsymmetrical 2, 2?-diaminebiaryls provided with different protecting groups. The treatment involves the protecting groups prior to the C, C coupling step. The co-reactants generally have different oxidation potentials which results from the selection of the protecting groups. The treatment also enables controlled access to the individual amino functions of the 2, 2?-diaminobiaryls by subsequent selective deprotection.
    Type: Grant
    Filed: July 23, 2015
    Date of Patent: November 20, 2018
    Assignee: EVONIK DEGUSSA GMBH
    Inventors: Katrin Marie Dyballa, Robert Franke, Dirk Fridag, Siegfried R. Waldvogel, Bernd Elsler, Mathias Enders
  • Patent number: 9730913
    Abstract: Inhibitors of beta lactamases and their use in treating bacterial infections are disclosed.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: August 15, 2017
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Ernesto Freire, Rogelio Siles, Patrick C. Ross
  • Patent number: 9051249
    Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R9 are as defined herein.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: June 9, 2015
    Assignee: KalVista Pharmaceuticals Limited
    Inventors: David Michael Evans, Rebecca Louise Davie, Hannah Joy Edwards, David Philip Rooker
  • Patent number: 9035096
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 19, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20150105429
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: GENENTECH, INC.
    Inventors: Benjamin Fauber, Olivier Rene
  • Patent number: 9000045
    Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity. the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: April 7, 2015
    Assignee: Japan Tobacco Inc.
    Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
  • Publication number: 20150080451
    Abstract: Potent low molecular weight, highly selective, competitive non-peptidic serine protease inhibitors and their use in treating serine protease-associated diseases are disclosed.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 19, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Ernesto Freire, Patrick C. Ross, Rogelio Siles
  • Patent number: 8962244
    Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.
    Type: Grant
    Filed: January 8, 2013
    Date of Patent: February 24, 2015
    Assignee: University of Massachusetts
    Inventor: Sean Ryder
  • Publication number: 20150038515
    Abstract: Pharmaceutical compositions of the invention comprise covalently closed circular DNA formation inhibitors having a disease-modifying action in the treatment of diseases associated with the formation of covalently closed circular DNA that include hepatitis B infection, and any disease involving formation of covalently closed circular DNA.
    Type: Application
    Filed: February 28, 2013
    Publication date: February 5, 2015
    Inventors: Andrea Cuconati, Haitao Guo, Timothy M. Block, Ju-Tao Guo, Xiaodong Xu, Huagang Lu, Dawei Cai
  • Publication number: 20150025068
    Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 22, 2015
    Inventors: Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
  • Publication number: 20150024032
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 22, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
  • Publication number: 20140378492
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 10, 2014
    Publication date: December 25, 2014
    Inventors: HAIQING YUAN, RICHARD L. BEARD, MICHAEL E. GARST, JOHN E. DONELLO, XIAOXIA LIU, VEENA VISWANATH
  • Publication number: 20140314675
    Abstract: An objective of the present invention is to provide: a cancer stem cell isolated using a cell marker; a substantively homogeneous cancer stem cell population including said cancer stem cell; and a method of preparing said cancer stem cell population. Another objective of the present invention is to provide: a method for separating cancer stem cells with a high proliferative potential and those with a low proliferative potential; a method for inducing cancer stem cells to have a different proliferative potential; and cancer stem cells separated or induced by these separation or induction methods. A further objective of the present invention is to provide: a method of screening for pharmaceuticals using said cancer stem cell or cancer stem cell population; a method for detecting the presence of said cancer stem cell or cancer stem cell population and for identifying or quantifying the same.
    Type: Application
    Filed: September 7, 2012
    Publication date: October 23, 2014
    Inventors: Tatsumi Yamazaki, Hisafumi Okabe, Shinta Kobayashi, Takeshi Watanabe, Koichi Matsubara, Atsuhiko Kato, Masami Suzuki
  • Publication number: 20140315947
    Abstract: The present invention relates to a pharmaceutical composition for inhibiting angiogenesis and a novel sulfonyl amide derivative compound which can be useful for the prevention or treatment of angiogenesis-related diseases or disorders. Since the compound used as an active ingredient in the pharmaceutical composition of the invention is specifically bound to UQCRB and inhibits biological functions thereof, apoptosis is not induced and angiogenic responses are inhibited. Therefore, the compound used as an active ingredient in the pharmaceutical composition of the invention can be useful as an effective and safe angiogenesis inhibitory agent.
    Type: Application
    Filed: May 23, 2011
    Publication date: October 23, 2014
    Applicant: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
    Inventors: Ho Jeong Kwon, Gyoon Hee Han, Hye Jin Jung, Jeong Jea Seo
  • Patent number: 8859815
    Abstract: A diamine of formula (I) is described in which A is hydrogen or a saturated or unsaturated C1-C20 alkyl group or an aryl group; B is a substituted or unsubstituted C1-C20 alkyl, cycloalkyl, alkaryl, alkaryl or aryl group or an alkylamino group and at least one of X1, X2, Y1, Y2 or Z is a C1-C10 alkyl, cycloalkyl, alkaryl, aralkyl or alkoxy substituting group. The chiral diamine may be used to prepare catalysts suitable for use in transfer hydrogenation reactions.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: October 14, 2014
    Assignee: Bial-Portela & C.A., S.A.
    Inventors: Beatriz Dominguez, Antonio Zanotti-Gerosa, Gabriela Alexandra Grasa, Jonathan Alan Medlock
  • Publication number: 20140256778
    Abstract: Inhibitors of beta lactamases and their use in treating bacterial infections are disclosed.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 11, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Ernesto Freire, Rogelio Siles, Patrick C. Ross
  • Patent number: 8829052
    Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: September 9, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Zhi Hong
  • Publication number: 20140243374
    Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.
    Type: Application
    Filed: October 4, 2012
    Publication date: August 28, 2014
    Inventors: Corinne E. Augelli-Szafran, Dai Lu, HanXun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe, Cuiman Cai
  • Patent number: 8808742
    Abstract: This invention relates to compositions, methods for preparing the compositions and methods for treating or preventing diseases, comprising administering the compositions.
    Type: Grant
    Filed: April 14, 2009
    Date of Patent: August 19, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Barry D. Quart, Colin Edward Rowlings
  • Patent number: 8809584
    Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: August 19, 2014
    Assignee: Institut Univ. de Ciencia i Tecnologia, S.A.
    Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
  • Publication number: 20140221481
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: Allergan, Inc.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Publication number: 20140213578
    Abstract: Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 31, 2014
    Applicant: MT. SINAI SCHOOL OF MEDICINE
    Inventors: Michael Ohlmeyer, Goutham Narla, Neil Dhawan, David Kastrinsky
  • Patent number: 8791161
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Grant
    Filed: February 20, 2013
    Date of Patent: July 29, 2014
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard L. Beard, Michael E. Garst, John E. Donello, Xiaoxia Liu, Veena Viswanath
  • Patent number: 8772541
    Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: July 8, 2014
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: Xiang-qun Xie, Peng Yang, Rentian Feng
  • Publication number: 20140155477
    Abstract: Provided herein are substituted biaryl sulfonamide compounds, pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate initiation of protein translation. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders.
    Type: Application
    Filed: November 27, 2013
    Publication date: June 5, 2014
    Applicant: NOVOMEDIX, LLC
    Inventors: Leah M. Fung, Kyle W.H. Chan, Cathy A. Swindlehurst, Robert W. Sullivan
  • Publication number: 20140107160
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: October 9, 2013
    Publication date: April 17, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C.B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20140039220
    Abstract: The present invention provides a method for producing a compound represented by general formula (1) (wherein R1, R2, R3, R10-R14, A1-A3, n1 and n2 are as defined in the description), which is characterized by reacting a compound represented by general formula (2) (wherein R10-R14, A1-A3, n1, n2 and B are as defined in the description) with a diamine compound represented by general formula (3) (wherein R1-R3 are as defined in the description). The present invention is a method for producing a diamine compound, which is useful for the formation of a ruthenium-diamine complex, under mild conditions, said method being able to be put in industrial practice.
    Type: Application
    Filed: April 27, 2012
    Publication date: February 6, 2014
    Applicant: TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Taichiro Touge, Tomohiko Hakamata, Hideki Nara
  • Patent number: 8642812
    Abstract: A compound having the formula (I) where each of R1, R2, R3 and R4 is independently C6-C18 aryl-, C5-C8 cycloalkyl-, C6-C18 aryl having at least one C1-C20 alkyl substituent, C5-C8 cycloalkyl having at least one C1-C20 alkyl substituent, C4-C20 branched alkyl-, C16-C20 linear alkyl-, RO—, —NRR?, —PRR?, —SR, fluoro substituted forms thereof, and perfluoro forms thereof: and R5 is C6-C18 aryl-, C3-C8 cycloalkyl-, C6-C18 aryl having at least one C1-C20 alkyl substituent, C5-C8 cycloalkyl having at least one C1-C20 alkyl substituent, C3-C20 branched alkyl-, C2-C30 linear alkyl-, fluoro substituted forms thereof, and perfluoro forms thereof; where R and R? are each independently C6-C18 aryl-, C5-C8 cycloalkyl-, C6-C18 aryl having at least one C1-C20 alkyl substituent, C5-C8 cycloalkyl having at least one C1-C20 alkyl substituent, C4-C20 branched alkyl-, C2-C30 linear alkyl-, fluoro substituted forms thereof, and perfluoro forms thereof; A is N, P, S, or O with the proviso that when A is S, R2 is a nullity; and M is
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: February 4, 2014
    Assignee: Stephan Consulting Corporation
    Inventors: Douglas W. Stephan, Gregory C. Welch, Jenny S. J. McCahill
  • Publication number: 20140024608
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Application
    Filed: March 14, 2013
    Publication date: January 23, 2014
    Applicant: METHYLGENE INC.
    Inventors: Robert Deziel, Alain Ajamian
  • Publication number: 20140005271
    Abstract: Provided herein are a composition for preventing or treating inflammatory diseases or infectious diseases which contains m-3M3FBS or a pharmaceutically available salt thereof as an active ingredient, and health supplements for improving or preventing inflammatory diseases or infectious diseases which contain m-3M3FBS. Since m-3M3FBS has a microbicidal effect, inhibition of apoptosis, and inhibition of LPS-involved signal transduction which enables to effectively treat or prevent inflammatory diseases or infectious diseases, so that it may be effectively used as medicine or health supplements for treating or preventing inflammatory diseases or infectious diseases.
    Type: Application
    Filed: March 14, 2012
    Publication date: January 2, 2014
    Inventors: Yoe Sik Bae, Sang Doo Kim
  • Publication number: 20130310384
    Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.
    Type: Application
    Filed: October 4, 2011
    Publication date: November 21, 2013
    Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
    Inventors: Corinne E. Augelli-Szafran, Dai Lu, Hanxun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe
  • Patent number: 8569543
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Grant
    Filed: August 30, 2011
    Date of Patent: October 29, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20130281695
    Abstract: Disclosed are intermediates of Sitagliptin, a preparation process thereof, and a process for synthesizing Sitagliptin using these intermediates. Sitagliptin is synthesized by using chiral amino compounds as a raw material, without having to build a chiral center with a chiral asymmetric catalytic hydrogenation, and high-pressure hydrogenation is avoided.
    Type: Application
    Filed: December 1, 2011
    Publication date: October 24, 2013
    Applicant: ZHEJIANG HISOAR PHARMACEUTICAL CO., LTD.
    Inventors: Xianhua Pan, Weijin Li, Qunhui Zhang, Libo Ruan, Wansheng Yu, Fei Deng, Tianhua Ma, Mingwang Huang, Minhuan He
  • Publication number: 20130261178
    Abstract: A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein Z1 is C1-C4 linear or branched alkyl or alkenyl; R4 is selected from unsubstituted and substituted C3-C3 cycloalkyl, C1-C8 linear or branched alkyl, C2-5 alkenyl, C6-C10 heteroaryl or aryl, or C3-C8 heterocyclyl which may be part unsaturated, and combinations thereof; Z is linear C2-3 alkylene; X1 is selected from NH and O; X2 is selected from unsaturated C and unsaturated S; and X3 is selected from NH and CH2; or one of X1 and X3 is a single bond; or X1 is O and X2 and X3 together are a single bond; and R7 is selected from oxo, F, Cl, Br, CN, NH2, NR92, NO2, CF3, OR9, COR9, OCOR9, COOR9, NR9COR9, CONR92SO2NR92, NR9SO2R9; and R8 is selected from C1-5 alkyl, C1-5 alkoxyl, C2-5 alkenyl or alkynyl, C6-10 aryl and C3-8 cycloalkyl and combinations thereof, which may be unsubstituted or further substituted by one or more F, Cl, Br, CN, NH2, NR32, NO2, CF3;
    Type: Application
    Filed: July 5, 2010
    Publication date: October 3, 2013
    Inventors: Shailesh Mistry, Etienne Daras, Christophe Fromont, Gopal Jadhav, Peter Martin Fischer, Barrie Kellam, Stephen John Hill, Jillian Glenda Baker
  • Publication number: 20130252984
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: March 12, 2013
    Publication date: September 26, 2013
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing YUAN, Richard L. BEARD, Xiaoxia LIU, John E. DONELLO, Veena VISWANATH, Michael E. GARST
  • Publication number: 20130236969
    Abstract: Use of a compound of Formula 1 for inducing differentiation of mesenchymal stem cells to chondrocytes, and a pharmaceutical composition for treating a cartilage disease, which includes chondrocytes in which differentiation from mesenchymal stem cells is induced by the compound of Formula 1, are provided. Differentiation of the mesenchymal stem cells treated with the compound of Formula 1 to chondrocytes is specifically induced, and thus the compound can be used to effectively treat a cartilage disease such as arthritis, cartilage damage, and a cartilage defect.
    Type: Application
    Filed: September 16, 2011
    Publication date: September 12, 2013
    Applicant: Industry-Academic Cooperation Foundation, Yonsei University
    Inventors: Ki Chul Hwang, Yang Soo Jang, Gyoon Hee Han
  • Patent number: 8524778
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl sulfonamides and related compounds (collectively referred to herein as ‘BPSAAA compounds’), as described herein, and including, for example, biphenyl-4-sulfonic acid (hydroxyalkyl-phenyl)-amides and related compounds.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: September 3, 2013
    Assignee: PIMCO 2664 Limited
    Inventors: Iain Robert Greig, Robert Jurgen Van't Hof, Stuart Hamilton Ralston
  • Patent number: 8513461
    Abstract: The invention relates to inhibitors of trypsin-like serine proteases, including those of the general formula (IV) which, as well as plasmin, also inhibit plasma kallikrien, and to their use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.
    Type: Grant
    Filed: February 19, 2013
    Date of Patent: August 20, 2013
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Torsten Steinmetzer, Andrea Schweinitz, Joerg Stuerzebecher, Peter Steinmetzer, Anett Soeffing, Andreas Van De Locht, Silke Nicklisch, Claudia Reichelt, Friedrich-Alexander Ludwig, Alexander Schulze, Mohammed Daghish, Jochen Heinicke
  • Publication number: 20130211139
    Abstract: The invention relates to a method of producing optically active ?-aminoaldehyde compound (3) by reacting imine compound (1-1) or sulfone compound (1-2) with aldehyde compound (2) in the presence of an optically active pyrrolidine compound. wherein each symbol is as defined in the specification.
    Type: Application
    Filed: October 19, 2011
    Publication date: August 15, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Yujiro Hayashi
  • Publication number: 20130190356
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genetech, Inc.
  • Publication number: 20130190288
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genentech, Inc.
  • Publication number: 20130190338
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: March 11, 2013
    Publication date: July 25, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130172388
    Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Applicant: University of Pittsburgh -- Of the Commonwealth System of Higher Education
    Inventor: University of Pittsburgh -- Of the Commonwealth System of Higher Education
  • Publication number: 20130165460
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: February 20, 2013
    Publication date: June 27, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Patent number: 8461134
    Abstract: This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: June 11, 2013
    Assignee: Anacor Pharmaceuticals, Inc.
    Inventors: Vincent S. Hernandez, Xianfeng Li, Suoming Zhang, Tsutomu Akama, Yanchen Zhang, Yang Liu, Jacob J. Plattner, Michael Richard Kevin Alley, Yasheen Zhou, James A. Nieman
  • Publication number: 20130123287
    Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as pro-cymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.
    Type: Application
    Filed: July 21, 2011
    Publication date: May 16, 2013
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Koji Sugimoto, Hiroyuki Hayashi
  • Publication number: 20130090385
    Abstract: The invention relates to compounds of the general formula (I) wherein R1, R2, R3, R4, R5, R6, i and j have the meanings given in claim 1, and to the use thereof as caspase-10 inhibitors, especially for the treatment of diabetic retinopathy.
    Type: Application
    Filed: November 28, 2012
    Publication date: April 11, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventor: Merck Patent Gesellschaft mit Beschrankter Haftu
  • Patent number: 8410310
    Abstract: The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrein, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.
    Type: Grant
    Filed: May 14, 2012
    Date of Patent: April 2, 2013
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Torsten Steinmetzer, Andrea Schweinitz, Joerg Stuerzebecher, Peter Steinmetzer, Anett Soeffing, Andreas Van De Locht, Silke Nicklisch, Claudia Reichelt, Friedrich-Alexander Ludwig, Alexander Schulze, Mohammed Daghish, Jochen Heinicke
  • Patent number: 8377639
    Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: February 19, 2013
    Assignee: University of Massachusetts
    Inventor: Sean Ryder
  • Publication number: 20130018207
    Abstract: A compound having the formula (I) where each of R1, R2, R3 and R4 is independently C6-C18 aryl-, C5-C8 cycloalkyl-, C6-C18 aryl having at least one C1-C20 alkyl substituent, C5-C8 cycloalkyl having at least one C1-C20 alkyl s?bstituent, C4-C20 branched alkyl-, C16-C20 linear alkyl-, RO—, —NRR?, —PRR?, —SR, fluoro substituted forms thereof, and perfluoro forms thereof: and R5 is C6-C18 aryl-, C5-C8cycloalkyl-, C6-C18 aryl having at least one C1-C20 alkyl substituent, C5-C8 cycloalkyl having at least one C1-C20 alkyl substituent, C3-C20 branched alkyl-, C2-C30 linear alkyl-, fluoro substituted forms thereof, and perfluoro forms thereof; where R and R? are each independently C6-C18 aryl-, C5 -C8 cycloalkyl-, C6-C18 aryl having at least one C1-C20 alkyl substituent, C5-C8 cycloalkyl having at least one C1-C20 alkyl substituent, C4-C20 branched alkyl-, C2-C30 linear alkyl-, fluoro substituted forms thereof, and perfluoro forms thereof; A is N, P, S, or O with the proviso that when A is S, R2 is a nullity; and M is
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: STEPHAN CONSULTING CORPORATION
    Inventors: Douglas W. Stephan, Preston A. Chase, Gregory C. Welch