Chalcogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 548/182)
  • Patent number: 9380782
    Abstract: The present invention provides a compound having an excellent efficacy for controlling pests. A tetrazolinone compound of a formula (1): [wherein, R1 represents an C6-C16 aryl group, an C1-C12 alkyl group, a C3-C12 cycloalkyl group or an adamantyl group, etc., which each optionally be substituted; R2 represents a hydrogen atom, an C1-C12 alkyl group, or a halogen atom, etc.; R4 and R5 represent independently of each other a hydrogen atom or an C1-C3 alkyl group, etc.; R6, R7, R8 and R9 represent independently of each other a hydrogen atom, a halogen atom, an C1-C12 alkyl group, a C1-C12 haloalkyl group, an C2-C12 alkenyl group, a C3-C12 cycloalkyl group, an C1-C12 alkoxy group or a C1-C12 haloalkoxy group, etc.; X and Y represent independently of each other a sulfur atom or an oxygen atom; Q represents an oxygen atom or a sulfur atom; and R10 represents an C1-C6 alkyl group, etc.] shows an excellent controlling efficacy on pests.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: July 5, 2016
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yuya Yoshimoto, Teruki Takahashi, Daisuke Oohira, Shuhei Azuma
  • Patent number: 8933107
    Abstract: The present invention relates to aryloxy substituted phenylamidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions (I).
    Type: Grant
    Filed: September 12, 2006
    Date of Patent: January 13, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Klaus Kunz, Jörg Greul, Oliver Guth, Benoît Hartmann, Kerstin Ilg, Wahed Ahmed Moradi, Thomas Seitz, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Ralf Dunkel, Ronald Ebbert, Eva-Maria Franken, Olga Malsam
  • Patent number: 8901311
    Abstract: The present invention relates to a process for preparing heterocyclic fluoroalkenyl sulfones and fluoroalkenyl sulfoxides by allowing the corresponding fluoroalkenyl thioethers to react with a salt of peroxomonosulfuric acid (H2SO5), optionally in the presence of a reaction assistant and optionally in the presence of a diluent.
    Type: Grant
    Filed: June 20, 2003
    Date of Patent: December 2, 2014
    Assignee: Makhteshim Chemical Works, Ltd.
    Inventor: Alexander Straub
  • Patent number: 8901306
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: December 2, 2014
    Assignee: StemSynergy Therapeutics, Inc.
    Inventor: Darren Orton
  • Publication number: 20140235867
    Abstract: The present invention relates to a specific thiazolium salt used for producing an ?-hydroxy ketone compound, and a method for producing an ?-hydroxy ketone compound by carrying out a coupling reaction of an aldehyde compound in the presence of a base compound and the specific thiazolium salt.
    Type: Application
    Filed: August 27, 2012
    Publication date: August 21, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Koji Hagiya, Akio Tanaka, Toshihiro Hodai
  • Patent number: 8748627
    Abstract: The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
    Type: Grant
    Filed: February 15, 2007
    Date of Patent: June 10, 2014
    Assignee: AbbVie Inc.
    Inventors: Yu Gui Gu, Moshe Weitzberg, Xiangdong Xu, Richard F. Clark, Tianyuan Zhang, Qun Li, Todd M. Hansen, Hing Sham, Bruce A. Beutel, Heidi S. Camp, Xiaojun Wang
  • Patent number: 8735595
    Abstract: The present invention relates to compounds of formula (I) which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
    Type: Grant
    Filed: February 15, 2007
    Date of Patent: May 27, 2014
    Assignee: AbbVie Inc.
    Inventors: Yu Gui Gu, Xiangdong Xu, Moshe Weitzberg, Hing L. Sham
  • Patent number: 8653278
    Abstract: One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising an HDAC inhibitor of the invention.
    Type: Grant
    Filed: August 2, 2007
    Date of Patent: February 18, 2014
    Assignees: Georgetown University, The Board of Trustees of the University of Illinois
    Inventors: Alan P. Kozikowski, Mira Jung, Anatoly Dritschilo, Arsen Gaysin, Pavel A. Petukhov, Werner Tueckmantel, Hongbin Yuan, Yufeng Chen
  • Patent number: 8637558
    Abstract: The present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and the uses thereof. More specifically, the present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and a pharmaceutical composition comprising the same. The novel thiazolidinedione derivatives of formula (I) according to the present invention can be effectively used for the prevention or treatment of cardiovascular disease, gastrointestinal disease and renal disease by inhibiting the activity of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) that decomposes prostaglandins as well as useful for the prevention of hair loss and the stimulation of hair growth, and osteogenic stimulation and wound healing.
    Type: Grant
    Filed: December 30, 2009
    Date of Patent: January 28, 2014
    Assignee: Industry-Academic Cooperation Foundation, Chosun University
    Inventors: Hoon Cho, Ying Wu, Cheol-Hee Choi
  • Patent number: 8497381
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: February 25, 2009
    Date of Patent: July 30, 2013
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Brian Andrew Stearns, Thomas Jonathan Seiders, Jill Melissa Scott, Jeannie M. Arruda, Bowei Wang
  • Patent number: 8426605
    Abstract: Disclosed are novel active substance combinations comprising specific heterocyclic trifluorobutenyls and previously known fungicidal agents. Said active substance combinations have a very good synergistic fungicidal, nematicidal, insecticidal, and/or acaricidal effect.
    Type: Grant
    Filed: April 20, 2004
    Date of Patent: April 23, 2013
    Assignee: Makhteshim Chemical Works, Ltd.
    Inventors: Wolfram Andersch, Ulrike Wachendorff-Neumann, Anton Kraus
  • Patent number: 8344009
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: October 7, 2010
    Date of Patent: January 1, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Michael Gaul, Alexander Kim, Lily Lee Searle, Raymond Patch, Dionisois Rentzeperis, Guozhang Xu, Xizhen Zhu
  • Patent number: 8338466
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: January 18, 2010
    Date of Patent: December 25, 2012
    Assignee: Abbott Laboratories
    Inventors: Aaron R. Kunzer, Steven W. Elmore, Laura A. Hexamer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Gary T. Wang, Xilu Wang, Michael D. Wendt
  • Patent number: 8222285
    Abstract: Compounds are provided which are glucokinase activators and thus are useful in treating diabetes and related diseases and have the structure wherein in the ring represents one or two double bonds; R1 is alkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; R2 is alkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; R5 is as defined herein; Z is O, S, S(O), S(O)2, or NR5a; X is S, O, N, NR3, or CR3; Y is NCR4 or NR4; R3, R4, and R5 are as defined herein; R8 is aryl, heteroaryl, —PO(OR9)(OR10), —PO(OR9)R10 or —P(O)(R9)R10 (wherein R9 and R10 are as defined herein)/R6 and R7 are independently H, halogen, or alkyl; m is 0 or 1; and n is 0 to 3, or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.
    Type: Grant
    Filed: June 11, 2008
    Date of Patent: July 17, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Sean Chen, Peter T. W. Cheng, Rebecca A. Smirk
  • Patent number: 8143296
    Abstract: The present invention relates to novel thiazole-based compounds and T-type calcium channel inhibitors containing the compound. The T-type calcium channel inhibitor of the present invention is useful as a treating agent for disease associated with overexpression of T-type calcium channel.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: March 27, 2012
    Assignee: Korea Institute of Science and Technology
    Inventors: Hoh-Gyu Hahn, Dong-Yun Shin, Kee-Dal Nam
  • Patent number: 8034954
    Abstract: The present invention provides novel calcium channel antagonists, and methods of treating disease sates using the novel antagonists.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: October 11, 2011
    Assignee: Icagen, Inc.
    Inventors: Gregory J. Pacofsky, Mark J. Suto, Paul Christopher Fritch
  • Publication number: 20110046177
    Abstract: Disclosed herein is a stable compound having a structure formula (I): therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: August 21, 2008
    Publication date: February 24, 2011
    Applicant: ALLERGAN, INC.
    Inventors: Richard L. Beard, Hiaqing Yuan, John E. Donello, Michael E. Garst
  • Patent number: 7879892
    Abstract: Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.
    Type: Grant
    Filed: May 21, 2008
    Date of Patent: February 1, 2011
    Assignee: Nereus Pharmaceuticals, Inc.
    Inventors: Venkata Rami Reddy Macherla, Benjamin Nicholson, Kin Sing Lam
  • Patent number: 7872027
    Abstract: Compounds and compositions for interfering with the association of Myc and Max are described herein. These compounds and compositions are useful in methods inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell are provided, comprising contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: January 18, 2011
    Assignees: University of Pittsburgh - Of the Commonwealth System of Higher Education, Georgetown University
    Inventors: Steven J. Metallo, Edward V. Prochownik
  • Publication number: 20110009398
    Abstract: The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G1, G2, G3 and G8 are each independently selected from —N? etc., Ring G6 is selected from divalent aryl etc., A is selected from amino etc., G4 is selected from oxygen etc., G5 is selected from oxygen etc., G7 is selected from —CH2— etc., and R2 is selected from C1-6 alkyl etc.
    Type: Application
    Filed: July 18, 2008
    Publication date: January 13, 2011
    Inventors: Toshiyuki Sakai, Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
  • Patent number: 7846953
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: December 7, 2010
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Michael Gaul, Alexander Kim, Lily Lee Searle, Raymond Patch, Dionisois Rentzeperis, Guozhang Xu, Xizhen Zhu
  • Publication number: 20100286032
    Abstract: A compound of the formula is disclosed as a prodrug of an HIV protease inhibitor. Methods and compositions for inhibiting HIV protease activity and treating HIV infection are also disclosed.
    Type: Application
    Filed: April 7, 2010
    Publication date: November 11, 2010
    Applicant: Abbott Laboratories
    Inventors: David A. DeGoey, William J. Flosi, David J. Grampovnik, Larry L. Klein, Dale J. Kempf, Xiu C. Wang
  • Patent number: 7812043
    Abstract: This invention relates to compounds that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. The compounds are of the general formula (I) wherein A and B are further defined in the application.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: October 12, 2010
    Assignee: TransTech Pharma, Inc.
    Inventors: Jesper F Lau, Per Vedsø, János Tibor Kodra, Anthony Murray, Lone Jeppesen, Michael Ankersen, Govindan Subramanian, Adnan M. M. Mjalli, Robert Carl Andrews, Dharma Rao Polisetti, Daniel Peter Christen
  • Patent number: 7803797
    Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein G, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: April 22, 2009
    Date of Patent: September 28, 2010
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Patent number: 7795442
    Abstract: A process is provided for preparing compounds having the general formula I wherein R is a range of organic groups and X is a leaving group. The process comprises reacting a compound of formula II with a water-removing reagent. When X is halogen or a sulfonate, the compound of formula I may be prepared by reacting a compound of the formula III with a halogenating agent or a sulfonylating agent. Alternatively, when X is halogen, the compound of formula I can be prepared by reacting a compound of the formula IV where R2 and R2 are defined organic groups, with a compound of the formula halogen-C(—O)—O—C1-C8alkyl, halogen-C(—O)—O-aryl or halogen-C(—O)—O-benzyl.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: September 14, 2010
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Thomas Pitterna, Henry Szczepanski, Peter Mainenfisch, Ottmar Franz Huter, Thomas Rapold, Marcel Senn, Thomas Gobel, Anthony Cornelius O'Sullivan
  • Patent number: 7786119
    Abstract: This invention is directed to drug conjugates of certain ion channel modulating compounds having the following formula: wherein A, X, R1, R2, R3, R4, R5, LB, L and DM are defined herein, including isolated enantiomeric and diastereomeric isomers thereof, and mixtures thereof. Pharmaceutical compositions and methods of use are also disclosed.
    Type: Grant
    Filed: March 31, 2005
    Date of Patent: August 31, 2010
    Assignee: Cardiome Pharma Corp.
    Inventors: Elizabeth L. S. Cheu, Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Alan M. Ezrin, Grace Jung, Bertrand M. C. Plouvier, Aregahegn S. Yifru
  • Patent number: 7786150
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: August 31, 2010
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 7781465
    Abstract: Disclosed herein is a compound represented by a formula Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: August 24, 2010
    Assignee: Allergan, Inc.
    Inventor: David W. Old
  • Patent number: 7781594
    Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt, prodrug and/or solvate thereof, and to a method for the treatment an acute or chronic inflammatory disease by inhibiting the production of at least one pro-inflammatory cytokine selected from TNF-alpha, IFN-gamma, IL-8 and IL-10, which comprises administering to a patient who needs such treatment a therapeutically effective amount of a compound of formula (I) as defined above.
    Type: Grant
    Filed: June 16, 2008
    Date of Patent: August 24, 2010
    Assignee: Faes Farma, S.A.
    Inventors: Victor Rubio Royo, Antonio De La Hera Martinez, Melchor Alvarez De Mon Soto, Ana Munoz Munoz
  • Patent number: 7758861
    Abstract: The present invention discloses dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and free radicals at the lesion of interest.
    Type: Grant
    Filed: March 21, 2006
    Date of Patent: July 20, 2010
    Assignee: Mallinckrodt Inc.
    Inventors: Raghavan Rajagopalan, Samuel I. Achilefu, Joseph E. Bugaj, Richard D. Dorshow
  • Publication number: 20100145063
    Abstract: 2-Ethenylthio-type carbapenem derivatives of formula (I) or pharmaceutically acceptable salts thereof are provided. The compounds according to the present invention have potent antimicrobial activity and a wide antimicrobial spectrum against pneumococci including penicillin resistant Streptococcus pneumoniae (PRSP), Haemophilus influenzae including ?-lactamase-negative, ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis.
    Type: Application
    Filed: February 4, 2010
    Publication date: June 10, 2010
    Inventors: Takahisa Maruyama, Yuko Kano, Takashi Ando, Toshiro Sasaki, Kazuhiro Aihara, Toshiki Fujita
  • Publication number: 20100081610
    Abstract: The present invention relates to ?-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.
    Type: Application
    Filed: August 21, 2007
    Publication date: April 1, 2010
    Inventors: Viswajanani J. Sattigeri, Venkata P. Palle, Manoj Kumar Khera, Ranaheer Reddy, Manoj Kumar Tiwari, Ajay Soni, Abdul Rehman Abdul Rauf, Sony Joseph, Arpita Musib, Sunanda G. Dastidar, Punit Kumar Srivastava
  • Patent number: 7666861
    Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: February 23, 2010
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: John W. Lampe, Robert Plourde, Jr., Jin She, Jason L. Vittitow, Paul S. Watson, Michael T. Crimmins, David J. Slade
  • Patent number: 7662842
    Abstract: Substituted thiazolidinone carboxylic acid amides and substituted thiazolidine carboxylic acid amides according to formulae (I) and (II) are disclosed where the various substituent groups are as defined in the specification. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.
    Type: Grant
    Filed: July 19, 2006
    Date of Patent: February 16, 2010
    Assignees: Ohio State Univesity Research Foundation, The University of Tennessee Research Foundation
    Inventors: Duane D. Miller, James T. Dalton, Veeresa Gududuru, Eunju Hurh
  • Publication number: 20090326011
    Abstract: Disclosed herein are compounds of formula (I) where G and Q are heteroaromatic groups. These compounds are useful for treating psychosis or a psychotic condition, substance abuse, premature ejaculation or cognition impairment.
    Type: Application
    Filed: June 13, 2006
    Publication date: December 31, 2009
    Inventors: Luca Arista, Francesca Cardullo, Anna Checchia, Dieter Hamprecht, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
  • Patent number: 7612059
    Abstract: N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, salts or prodrugs thereof have interesting properties, e.g., in the treatment or prevention of disorders amenable to treatment by PDF inhibitors, such as treatment of bacterial infections.
    Type: Grant
    Filed: June 13, 2005
    Date of Patent: November 3, 2009
    Assignee: Vicuron Pharmaceuticals, Inc.
    Inventors: Jeffrey Jacobs, Rakesh K Patel, Jason G Lewis, Dinesh V Patel, Zhengyu Yuan
  • Patent number: 7598391
    Abstract: This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: October 6, 2009
    Assignee: Novo Nordisk A/S
    Inventors: Anthony Murray, Jesper Lau, Lone Jeppesen, Per Vedsø, Michael Ankersen, Jane Marie Lundbeck, Marit Kristiansen, Maria Carmen Valcarce-Lopez, Dharma Rao Polisetti, Govindan Subramanian, Robert Carl Andrews, Daniel P. Christen, Jeremy T. Cooper, Kalpathy Chidambareswaran Santhosh
  • Patent number: 7598423
    Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.
    Type: Grant
    Filed: November 15, 2005
    Date of Patent: October 6, 2009
    Assignee: Eli Lilly and Company
    Inventors: Thomas Daniel Aicher, Guillermo S. Cortez, Todd Michael Groendyke, Albert Khilevich, James Allen Knobelsdorf, Fredrik Pehr Marmsater, Jeffrey Michael Schkeryantz, Tony Pisal Tang, Nicholas Andrew Magnus
  • Patent number: 7572816
    Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.
    Type: Grant
    Filed: July 21, 2004
    Date of Patent: August 11, 2009
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Bruno Tse, Sepehr Sarshar
  • Patent number: 7563813
    Abstract: Compounds of Formula 1, or pharmaceutically acceptable salts thereof, are provided: which are inhibitors of secreted frizzled related protein-1. The compounds, and compositions containing the compounds, can be used to treat a variety of disorders, including osteoporosis.
    Type: Grant
    Filed: May 10, 2006
    Date of Patent: July 21, 2009
    Assignee: Wyeth
    Inventors: Ariamala Gopalsamy, Mengxiao Shi
  • Patent number: 7557095
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: May 7, 2007
    Date of Patent: July 7, 2009
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, David W. Old, Todd Gac
  • Patent number: 7550448
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: June 23, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Publication number: 20090156644
    Abstract: There is provided a use of a compound of formula (I), wherein X, Y, T, W, A1, A2R1, R5 and R6 have meanings given in the description for the manufacture of a medicament for the treatment of cancer.
    Type: Application
    Filed: July 21, 2006
    Publication date: June 18, 2009
    Inventors: Jacob Westman, Guido Kurz, Bjorn Eriksson, Christian Hedberg
  • Publication number: 20090136472
    Abstract: There is provided a use of a compound of formula I, wherein X, T, Y, W, A1, A2, R1, R5 and R6 have meanings given in the description, for the manufacture of a medicament for the treatment of a disorder or condition caused by, linked to, or contributed to by, free fatty acids, such as hyperinsulinemia and associated conditions, including type 2 diabetes and the like.
    Type: Application
    Filed: July 21, 2006
    Publication date: May 28, 2009
    Inventors: Jacob Westman, Guido Kurz, Bjorn Eriksson, Christian Hdberg
  • Publication number: 20090137817
    Abstract: Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.
    Type: Application
    Filed: August 25, 2008
    Publication date: May 28, 2009
    Inventors: Pierre Deslongchamps, Yves Dory, Kamel Benakli, Eric Marsault, Luc Ouellet, Mahesh Ramaseshan, Martin Vezina, Daniel Fortin, Ruoxi Lan, Shigui Li, Gerald Villeneuve, Hamid R. Hoveyda, Sylvie Beaubien, Mark L. Peterson
  • Patent number: 7521466
    Abstract: Novel dipeptide ethers are effective for lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyceride levels. The dipeptide ethers are also useful for the treatment and/or prophylaxis of diabetes, obesity, inflammation and autoimmune diseases such as multiple sclerosis and rheumatoid arthritis.
    Type: Grant
    Filed: May 4, 2006
    Date of Patent: April 21, 2009
    Assignee: Bexel Pharmaceuticals, Inc.
    Inventors: Bishwajit Nag, Abhijeet Nag, Debendranath Dey, Partha Neogi, Shiv Kumar Agarwal, Surendra Kumar Pandey
  • Publication number: 20080274892
    Abstract: A haloalkylsulfonanilide derivative represented by the formula (I): {wherein R1 represents haloalkyl; R2 represents H, alkylcarbonyl, optionally substituted phenylcarbonyl, alkoxycarbonyl, optionally substituted phenoxycarbonyl, optionally substituted phenylsulfonyl, etc.; R3 and R4 each represents H, alkyl, cycloalkyl, halogeno, CN, etc.; R5, R6, R7, and R8 each represents H, halogeno, alkyl, cycloalkyl, optionally substituted phenyl(C1-6 alkyl), an optionally substituted heterocycle, etc.; A and W each represents O or S; and X represents one to four substituents selected among H, halogeno, alkyl, alkenyl, optionally substituted phenyl, optionally substituted phenylalkylaminocarbonyl, OH, CN, etc.} and a salt thereof; and a herbicide containing any of these compounds as an active ingredient. The herbicide is excellent in wide applicability, persistency, and selectivity for crops and effectiveness against weeds. It is excellent especially as a herbicide for rice fields.
    Type: Application
    Filed: February 23, 2006
    Publication date: November 6, 2008
    Inventors: Tomokazu Hino, Toshihiko Shigenari, Takahiro Kiyokawa, Koki Mametsuka, Yasuko Yamada
  • Patent number: 7439260
    Abstract: The instant invention provides compounds of Formula (I) which are leukotriene biosynthesis inhibitors. Compounds of formula (I) are useful as anti-asthmatic, anti-allergic, anti-inflammatory, cytoprotective and anti-artherosclerotic agents.
    Type: Grant
    Filed: June 8, 2004
    Date of Patent: October 21, 2008
    Assignee: Merck Forsst Canada & Co.
    Inventors: Yves Gareau, Helene Juteau, D. Bruce MacKay, Richard Friesen, Erich L. Grimm, Marc Blouin, Sebastien Laliberte
  • Patent number: 7378530
    Abstract: Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity.
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: May 27, 2008
    Assignee: Nereus Pharmaceuticals, Inc.
    Inventors: Venkata Rami Reddy Macherla, Benjamin Nicholson, Kin Sing Lam
  • Patent number: 7358266
    Abstract: The invention relates to cis- and trans-12, 13-cyclopropyl and 12,13-cyclobutyl epothilones of formula I to IV wherein Ar is a radical represented by the following structure: and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.
    Type: Grant
    Filed: August 23, 2002
    Date of Patent: April 15, 2008
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Kenji Namoto, Andreas Ritzen, Mitsuru Shoji, Trond Ulven, Karl-Heinz Altmann