Plural Double Bonds Between Ring Members Of The Hetero Ring Patents (Class 549/471)
  • Patent number: 10457693
    Abstract: Embodiments of the present disclosure provide for methods of making an organoboron compound, organoboron compounds, and the like.
    Type: Grant
    Filed: August 22, 2018
    Date of Patent: October 29, 2019
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Suzanne A. Blum, Joshua J. Hirner, Darius J. Faizi
  • Patent number: 10183957
    Abstract: Embodiments of the present disclosure provide for methods of making an organoboron compound, organoboron compounds, and the like.
    Type: Grant
    Filed: October 18, 2016
    Date of Patent: January 22, 2019
    Assignee: The Regents of the University of California
    Inventors: Suzanne A. Blum, Joshua J. Hirner, Darius J. Faizi
  • Patent number: 9512147
    Abstract: Embodiments of the present disclosure provide for methods of making an organoboron compound, organoboron compounds, and the like.
    Type: Grant
    Filed: November 16, 2015
    Date of Patent: December 6, 2016
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Suzanne A. Blum, Joshua J. Hirner, Darius J. Faizi
  • Patent number: 9334254
    Abstract: The invention relates to a process for preparing 5-sulfonamido-benzofuran derivatives of general formula: formula (I) in which R represents an alkyl or aryl group and R1 and R2 represent hydrogen or an alkyl or aryl group. According to the invention, the compounds of formula I are prepared by coupling a benzofuran derivative of general formula II, where X represents chlorine, bromine or iodine or a sulfonate group: formula (II) with a sulfonamide derivative of formula R—SO2—NH2, in the presence of a basic agent and of a catalyst system formed from a complex between a palladium compound and a ligand.
    Type: Grant
    Filed: March 30, 2011
    Date of Patent: May 10, 2016
    Assignee: SANOFI
    Inventors: Thomas Priem, Philippe Paul Vayron
  • Patent number: 9023874
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: May 5, 2015
    Assignee: Merial, Inc.
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Publication number: 20150111810
    Abstract: The present invention is directed to a novel fragrance compound, 3-methyl-benzofuran-5-ol, and a method of improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount of 3-methyl-benzofuran-5-ol.
    Type: Application
    Filed: October 18, 2013
    Publication date: April 23, 2015
    Applicant: International Flavors & Fragrances Inc.
    Inventors: Feng Geng, Michael G. Monteleone, Anubhav P.S. Narula
  • Publication number: 20150051257
    Abstract: Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted; or 9- or 10-membered bicyclic group, linked to —(O)x—(CH2)y— through one of its aromatic carbon atoms, consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5- or 6-membered non-aromatic heterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1-C3-alkyls; D represents a group selected from: phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted; thiophene unsubstituted or substituted; bicyclic group consisting of imidazolering fused with 5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2 heteroatoms independently selected from the group consisting of N, O and
    Type: Application
    Filed: March 20, 2013
    Publication date: February 19, 2015
    Applicant: ADAMED SP. ZO.O
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Tomasz Lysakowski, Maciej Pawlowski
  • Publication number: 20150018547
    Abstract: The present invention provides a compound having a GOAT inhibitory action, which is useful for the prophylaxis or treatment of obesity and the like, and has superior efficacy. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: February 22, 2013
    Publication date: January 15, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Nobuyuki Takakura, Yoshihiro Banno, Yoshito Terao, Atsuko Ochida, Sachie Morimoto, Shuji Kitamura, Yoshihide Tomata, Tsuneo Yasuma, Minoru Ikoma, Kei Masuda
  • Publication number: 20150005500
    Abstract: Disclosed are novel ruthenium compounds of formula (Ia) and (Ib): wherein R1 and the moiety are defined herein. Also disclosed is a process for using these novel ruthenium compounds as catalysts for asymmetric hydrogenation and transfer hydrogenation of ketones with high reactivities and excellent selectivities.
    Type: Application
    Filed: June 24, 2014
    Publication date: January 1, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Nizar HADDAD, Heewon LEE, Bo QU, Sonia RODRIGUEZ, Chris Hugh SENANAYAKE
  • Publication number: 20140343078
    Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.
    Type: Application
    Filed: July 29, 2014
    Publication date: November 20, 2014
    Inventors: Michael EISSENSTAT, Dehui DUAN, Ji-Hye KANG
  • Publication number: 20140315881
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Publication number: 20140296516
    Abstract: The invention relates to metal complexes of general formula (I) and to a method for the production thereof, in which M, R1, R2, R3, X and Y in addition to Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh can have the meanings defined in the claims. Said metal complexes form air-stable compounds and are suitable as pre-catalysts in the olefin metathesis.
    Type: Application
    Filed: February 23, 2012
    Publication date: October 2, 2014
    Applicant: STUDIENGESELLSCHAFT KOHLE MBH
    Inventors: Alois Furstner, Johannes Heppekausen
  • Publication number: 20140249199
    Abstract: The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula (I), pharmaceutical compositions having a compound of formula (I), and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula (I) to a subject in need thereof.
    Type: Application
    Filed: July 19, 2012
    Publication date: September 4, 2014
    Applicants: HEALTH RESEARCH, INC., EMORY UNIVERSITY
    Inventors: Huw M. L. Davies, Spandan Chennamadhavuni, Andrei Bakin
  • Patent number: 8822708
    Abstract: Triphenylene containing benzo-fused thiophene compounds are provided. Additionally, triphenylene containing benzo-fused furan compounds are provided. The compounds may be useful in organic light emitting devices, particularly as hosts in the emissive layer of such devices, or as materials for enhancement layers in such devices, or both.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 2, 2014
    Assignee: Universal Display Corporation
    Inventors: Bin Ma, Yonggang Wu, Chun Lin, Raymond Kwong
  • Patent number: 8816103
    Abstract: The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di-n-butylamino)-propoxy]benzoyl}benzofuran-5-yl]-methanesulfonamide of formula I: and pharmaceutically acceptable salts thereof wherein the acyl group of the benzofuran derivative of the general formula II: where R represents C1-4 alkyl-, C1-4 alkoxy- or aryl group, is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.
    Type: Grant
    Filed: January 14, 2013
    Date of Patent: August 26, 2014
    Assignee: Sanofi
    Inventors: Antal Friesz, Csaba Huszar
  • Patent number: 8716335
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.
    Type: Grant
    Filed: May 1, 2012
    Date of Patent: May 6, 2014
    Assignee: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn, Gabriel Kremmidiotis
  • Publication number: 20140113897
    Abstract: The present invention embraces compounds that modulate the activity of Epstein-Barr Nuclear Antigen 1 (BBNA1) protein and use thereof in methods for treating latent Epstein-Barr virus infection. R7 is a substituted or unsubstituted phenyl, pyridyl, or pyrimidinyl group. A pharmaceutical composition comprising a compound of the invention in admixture with a pharmaceutically acceptable carrier is also provide as are methods for modulating the activity of Epstein-Barr Nuclear Antigen 1 (EBNA1) protein and treating a latent EpsteinBarr virus infection with a composition of the present invention.
    Type: Application
    Filed: May 22, 2012
    Publication date: April 24, 2014
    Applicant: THE WISTAR INSTITUTE
    Inventors: Paul M. Lieberman, Troy Messick
  • Patent number: 8680135
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: March 25, 2014
    Assignee: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn, Gabriel Kremmidiotis
  • Publication number: 20140058106
    Abstract: Described herein are fluorinated organic compounds and methods of making fluorinated organic compounds, for example, using palladium complexes. Also described herein are compositions and kits containing compounds and palladium complexes described herein.
    Type: Application
    Filed: July 29, 2013
    Publication date: February 27, 2014
    Inventors: Tobias Ritter, Takeru Furuya, Hanns M. Kaiser
  • Patent number: 8614239
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases (e.g., cancer and inflammation).
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: December 24, 2013
    Assignee: Novartis AG
    Inventors: Dinesh Chikkanna, Mark Gary Bock, Clive McCarthy, Henrik Moebitz, Chetan Pandit, Ramulu Poddutorri
  • Publication number: 20130310254
    Abstract: The present application relates to novel alpha, beta-unsaturated imines, to processes for their preparation, to their use for controlling animal pests including arthropods and in particular insects and to their use in the control of vectors.
    Type: Application
    Filed: November 24, 2011
    Publication date: November 21, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Stefan Werner, Ulrich Ebbinghaus-Kintscher, Sebastian Horstmann, Michael Maue, Hans-Georg Schwarz, Robert Velten, Arnd Voerste, Ulrich Görgens, Andreas Turberg
  • Patent number: 8586743
    Abstract: The present disclosure is directed to a reactive ester agent capable of conjugating a reporter molecule to a carrier molecule or solid support. The reactive ester agent has the general formula: wherein the variables are described throughout the application.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: November 19, 2013
    Assignee: Life Technologies Corporation
    Inventors: Kyle Gee, Aleksey Rukavishnikov, Diane M. Witczak
  • Publication number: 20130248835
    Abstract: There is provided an electroactive material having Formula I wherein: Q is the same or different at each occurrence and can be O, S, Se, Te, NR, SO, SO2, P, PO, PO2, and SiR2; R is the same or different at each occurrence and can be hydrogen, alkyl, aryl, alkenyl, or alkynyl; R1 through R10 are the same or different and can be hydrogen, alkyl, aryl, halogen, hydroxyl, aryloxy, alkoxy, alkenyl, alkynyl, amino, alkylthio, phosphino, silyl, —COR, —COOR, —PO3R2, —OPO3R2, or CN.
    Type: Application
    Filed: May 13, 2013
    Publication date: September 26, 2013
    Applicant: E I Du Pont De Nemours And Company
    Inventors: HONG MENG, Dengfu Wang
  • Publication number: 20130253183
    Abstract: Provided are: an aromatic amine derivative in which a terminal substituent such as a dibenzofuran ring or a dibenzothiophene ring is bonded to a nitrogen atom directly or through an arylene group or the like; an organic electroluminescence device including an organic thin film layer formed of one or more layers including a light emitting layer and interposed between a cathode and an anode in which a layer of the organic thin film layer contains the aromatic amine derivative by itself or as a component of a mixture, and the device has a long lifetime and high luminous efficiency; and an aromatic amine derivative for realizing the device.
    Type: Application
    Filed: May 24, 2013
    Publication date: September 26, 2013
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Yumiko MIZUKI, Masakazu Funahashi, Mitsunori Ito, Masahiro Kawamura
  • Patent number: 8497372
    Abstract: Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder with one of these compounds.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: July 30, 2013
    Assignee: Hutchison Medipharma Enterprises Limited
    Inventors: Wei-Guo Su, Weihan Zhang, Xiaoqiang Yan, Yumin Cui, Yongxin Ren, Jifeng Duan
  • Publication number: 20130175510
    Abstract: Triphenylene containing benzo-fused thiophene compounds are provided. Additionally, triphenylene containing benzo-fused furan compounds are provided. The compounds may be useful in organic light emitting devices, particularly as hosts in the emissive layer of such devices, or as materials for enhancement layers in such devices, or both.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 11, 2013
    Applicant: UNIVERSAL DISPLAY CORPORTION
    Inventor: Universal Display Corportion
  • Patent number: 8470878
    Abstract: The present invention relates to compounds: and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases like cancer and inflammation.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: June 25, 2013
    Assignee: Novartis AG
    Inventors: Ramulu Poddutoori, Can Wang, Xianglin Zhao
  • Publication number: 20130131358
    Abstract: The subject of the invention is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-di-n-butylamino)-propoxy]benzoyl}benzofuran-5-yl]-methanesulfonamide of formula I: and pharmaceutically acceptable salts thereof wherein the acyl group of the benzofuran derivative of the general formula II: where R represents C1-4 alkyl-, C1-4 alkoxy- or aryl group, is selectively cleaved and if desired, the resulting compound of formula I is transformed into its salt.
    Type: Application
    Filed: January 14, 2013
    Publication date: May 23, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Publication number: 20130131351
    Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
    Type: Application
    Filed: October 5, 2012
    Publication date: May 23, 2013
    Applicant: Metabolex, Inc.
    Inventor: Metabolex, Inc.
  • Publication number: 20130096209
    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 18, 2013
    Applicants: Kraft Foods Global Brands LLC, Chromocell Corporation
    Inventors: David Hayashi, William P. Jones, Jane V. Leland, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Louise Slade, Kambiz Shekdar, Jessica Langer
  • Publication number: 20130085284
    Abstract: Hafnium complexes of heterocyclic organic ligands having improved solubility in aliphatic hydrocarbon solvents and their use as components of olefin polymerization catalysts as well as novel syntheses of component parts thereof are disclosed.
    Type: Application
    Filed: November 26, 2012
    Publication date: April 4, 2013
    Applicant: Dow Global Technologies LLC
    Inventor: Dow Global Technologies LLC
  • Publication number: 20130046103
    Abstract: The present invention provides several synthetic methods for preparing N-(2-butylbenzofuran-5-yl)-N-(methylsulfonyl)methanesulfonamide, a compound of formula (3), an intermediate in the preparation of Dronedarone. The present invention further provides a process for preparing Dronedarone, comprising the steps of converting 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) to Dronedarone, wherein the 2-butyl-5-bis(methanesulfon)-amidobenzofuran of formula (3) is prepared by the processes of the present invention.
    Type: Application
    Filed: February 10, 2011
    Publication date: February 21, 2013
    Applicant: MAPI PHARMA LIMITED
    Inventors: Ehud Marom, Michael Mizhiritskii, Shai Rubnov
  • Patent number: 8372991
    Abstract: Described herein are compounds of Formula (I): wherein A, J, Z, X, R1 and R4 are defined herein, 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 or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: February 12, 2013
    Assignee: Calcimedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20130023678
    Abstract: The invention relates to a process for preparing 5-sulfonamido-benzofuran derivatives of general formula: formula (I) in which R represents an alkyl or aryl group and R1 and R2 represent hydrogen or an alkyl or aryl group. According to the invention, the compounds of formula I are prepared by coupling a benzofuran derivative of general formula II, where X represents chlorine, bromine or iodine or a sulfonate group: formula (II) with a sulfonamide derivative of formula R—SO2—NH2, in the presence of a basic agent and of a catalyst system formed from a complex between a palladium compound and a ligand.
    Type: Application
    Filed: March 30, 2011
    Publication date: January 24, 2013
    Applicant: SANOFI
    Inventors: Thomas Priem, Philippe Paul Vayron
  • Publication number: 20130005767
    Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 3, 2013
    Applicant: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Publication number: 20120330036
    Abstract: The subject of the present disclosure is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide of formula I: and the new intermediates of the preparation process.
    Type: Application
    Filed: June 29, 2012
    Publication date: December 27, 2012
    Applicant: SANOFI
    Inventors: Antal FRIESZ, Mariann CSATARINE NAGY
  • Publication number: 20120316149
    Abstract: The present invention relates to compounds: and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases like cancer and inflammation.
    Type: Application
    Filed: June 7, 2012
    Publication date: December 13, 2012
    Inventors: Ramulu PODDUTOORI, Can WANG, Xianglin ZHAO
  • Publication number: 20120302566
    Abstract: The present invention relates to compounds defined by formula (I) wherein the variables R1, R2, R3, m, and n are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are activators of the receptor GPR40 and thus are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: November 30, 2011
    Publication date: November 29, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank Himmelsbach, Remko Bakker, Matthias Eckhardt, Dieter Hamprecht, Elke Langkopf, Holger Wagner
  • Publication number: 20120302752
    Abstract: Methods are described for efficient and regioselective reactions that are Ru-catalyzed and either (i) amide-directed C—H, C—N, C—O activation/C—C bond forming reactions, (ii) ester-directed C—O and C—N activation/C—C bond forming reactions, or (iii) amide-directed C—O activation/hydrodemethoxylation reactions. All of these reactions of directed C—H, C—N, C—O activation/coupling reactions establish a catalytic base-free DoM-cross coupling process at non-cryogenic temperature. High regioselectivity, yields, operational simplicity, low cost, and convenient scale-up make these reactions suitable for industrial applications. Many previously unknown amide-substituted or ester-substituted aryl and heteroaryl compounds are presented with synthetic details also provided.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 29, 2012
    Inventors: Yigang Zhao, Victor A. Snieckus
  • Patent number: 8309545
    Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.
    Type: Grant
    Filed: October 4, 2007
    Date of Patent: November 13, 2012
    Assignee: Bionomics Limited
    Inventors: Bernard Luke Flynn, Jonathan B. Baell, Andrew J. Harvey, Jason Hugh Chaplin, Dharam Paul, Jorgen Alvar Mould
  • Publication number: 20120245209
    Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds have been demonstrated as inhibitors of MEK and therefore may be useful in the treatment of hyperproliferative diseases (e.g., cancer and inflammation).
    Type: Application
    Filed: December 7, 2010
    Publication date: September 27, 2012
    Applicant: NOVARTIS AG
    Inventors: Dinesh Chikkanna, Mark Gary Bock, Clive McCarthy, Henrik Moebitz, Chetan Pandit, Ramulu Poddutorri
  • Publication number: 20120190639
    Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
    Type: Application
    Filed: April 30, 2010
    Publication date: July 26, 2012
    Applicant: UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • Patent number: 8212033
    Abstract: Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder with one of these compounds.
    Type: Grant
    Filed: September 29, 2010
    Date of Patent: July 3, 2012
    Assignee: Hutchison Medipharma Enterprises Limited
    Inventors: Wei-Guo Su, Weihan Zhang, Xiaoqiang Yan, Yumin Cui, Yongxin Ren, Jifeng Duan
  • Patent number: 8198466
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: June 12, 2012
    Assignee: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn, Gabriel Kremmidiotis
  • Publication number: 20120065064
    Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Application
    Filed: December 12, 2009
    Publication date: March 15, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: John Benjamin Taylor, Jeffrey Steven Wailes, Stephane André Marie Jeanmart, Mangala Govenkar
  • Patent number: 8129570
    Abstract: The present invention relates to a process for the preparation of compounds of a 1,4-dialkyl-2,3-diol-1,4-butanedione by a acidic aldol condensation between an alkyl glyoxal and an ?-hydroxy ketone.
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: March 6, 2012
    Assignee: Firmenich SA
    Inventor: Olivier Andrey
  • Publication number: 20120053173
    Abstract: Provision of a prophylactic or therapeutic agent for diabetes, which has superior efficacy. A compound represented by the formula: wherein each symbol is as described in the specification, or a salt thereof.
    Type: Application
    Filed: March 4, 2009
    Publication date: March 1, 2012
    Inventors: Yoshihiro Banno, Ryoma Hara, Ryosuke Tokunoh
  • Publication number: 20120053132
    Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.
    Type: Application
    Filed: November 1, 2011
    Publication date: March 1, 2012
    Applicant: Sequoia Pharmaceuticals, Inc.
    Inventors: Michael Eissenstat, Dehui Duan
  • Publication number: 20120034270
    Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
    Type: Application
    Filed: October 16, 2009
    Publication date: February 9, 2012
    Applicant: Akaal Pharma Pty Ltd
    Inventors: Damian W. Grobelny, Gurmit S. Gill
  • Patent number: 8012984
    Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
    Type: Grant
    Filed: September 14, 2010
    Date of Patent: September 6, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Philip D. Stein, Sharon N. Bisaha, Saleem Ahmad, Khehyong Ngu, William N. Washburn