The Additional Hetero Ring Is Bonded Directly To A Ring Carbon Of The Bicyclo Ring System Patents (Class 548/466)
  • Patent number: 7947713
    Abstract: The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: May 24, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Henry Joseph Breslin, Hans Louis Jos De Winter, Michael Joseph Kukla
  • Publication number: 20110098483
    Abstract: The invention relates to a nitrogen heterocycle compound of formula 1: Also disclosed are a method of synthesizing the compound and use of the compound for treating various diseases and conditions.
    Type: Application
    Filed: March 27, 2009
    Publication date: April 28, 2011
    Applicant: UNIVERSITY OF SOUTHERN CALIFORNIA
    Inventors: Nicos A. Petasis, Malgorzata Myslinska
  • Patent number: 7915260
    Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.
    Type: Grant
    Filed: January 10, 2007
    Date of Patent: March 29, 2011
    Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
  • Publication number: 20110071132
    Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress- and/or oxytocin-dependent-diseases are also disclosed.
    Type: Application
    Filed: July 30, 2010
    Publication date: March 24, 2011
    Applicant: Abbott GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Andrea Hager-Wernet, Wilfried Hornberger, Liliane Unger
  • Patent number: 7902379
    Abstract: The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5 R6 and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.
    Type: Grant
    Filed: September 30, 2004
    Date of Patent: March 8, 2011
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Wilfried Hornberger, Thorsten K. Oost, Daryl Richard Sauer, Liliane Unger, Wolfgang Wernet, Hervé Geneste
  • Patent number: 7897601
    Abstract: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: March 1, 2011
    Assignees: Intervet, Inc., Intervet International B.V.
    Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Martin C. Clasby, Keith A. Eagen, Jack D. Scott, Yuguang Wang, Yan Xia, William J. Greenlee
  • Publication number: 20110046367
    Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.
    Type: Application
    Filed: November 1, 2010
    Publication date: February 24, 2011
    Applicant: President and Fellows of Harvard College
    Inventors: José A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
  • Publication number: 20110028519
    Abstract: Compounds of Formula I are described along with pharmaceutical formulations thereof, and methods of treating disorders such as diabetes and neurodegenerative diseases with such compounds.
    Type: Application
    Filed: October 11, 2010
    Publication date: February 3, 2011
    Inventor: Michael C. Pirrung
  • Publication number: 20110021556
    Abstract: The invention relates to 3,3 disubstituted pyrrole derivatives useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Application
    Filed: March 10, 2009
    Publication date: January 27, 2011
    Applicant: Hoffman-La Roche, Inc.
    Inventors: Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
  • Publication number: 20110021785
    Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Application
    Filed: January 20, 2010
    Publication date: January 27, 2011
    Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
  • Publication number: 20100317100
    Abstract: The present invention embraces compositions and methods for establishing and maintaining stem cells and inhibiting stem cell differentiation using a selective Protein Kinase C (PKC) inhibitor.
    Type: Application
    Filed: June 11, 2010
    Publication date: December 16, 2010
    Inventors: Soumen Paul, Debasree Dutta, Soma Ray, Jeffrey Aube, Frank John Schoenen
  • Patent number: 7825155
    Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.
    Type: Grant
    Filed: September 13, 2006
    Date of Patent: November 2, 2010
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
  • Publication number: 20100273774
    Abstract: A compound of formula (I), wherein R, R1, R2, ring A, which ring contains one or two nitrogen atoms, and ring B are as defined in the Specification, pharmaceutical compositions containing these compounds, and uses for these compounds and compositions, in particular, in transplantation.
    Type: Application
    Filed: July 9, 2010
    Publication date: October 28, 2010
    Inventors: Jürgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
  • Publication number: 20100273824
    Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.
    Type: Application
    Filed: January 18, 2008
    Publication date: October 28, 2010
    Applicant: EVOLVA SA
    Inventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
  • Patent number: 7820672
    Abstract: The compounds are indolylmaleimide derivatives comprising either a substituted pyridyl or indolyl residue. The compounds have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, or acute or chronic transplant rejection.
    Type: Grant
    Filed: February 12, 2004
    Date of Patent: October 26, 2010
    Assignee: Novartis AG
    Inventors: Peter Von Matt, Jürgen Wagner
  • Patent number: 7812017
    Abstract: The present invention relates to novel compounds of formula (I): wherein m, n, R0, R1, R2, R3 and R4 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: October 12, 2010
    Assignee: Biovitrum AB (publ.)
    Inventors: Johan Angbrant, Rune Ringom, Kristin Hammer, Erik Ringberg, Bengt Lindqvist, Gary Johansson, Peter Brandt, Katarina Beierlein, Björn M Nilsson
  • Publication number: 20100252112
    Abstract: Disclosed are semiconducting compounds having one or more phthalimide units and/or one or more head-to-head (H-H) substituted biheteroaryl units. Such compounds can be monomeric, oligomeric, or polymeric, and can exhibit desirable electronic properties and possess processing advantages including solution-processability and/or good stability at ambient conditions.
    Type: Application
    Filed: April 6, 2010
    Publication date: October 7, 2010
    Inventor: Mark D. Watson
  • Publication number: 20100240650
    Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
    Type: Application
    Filed: May 25, 2010
    Publication date: September 23, 2010
    Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly White, Hong Ye, Leonard R. Hecker, Bruce Conway, Keith Demarest
  • Publication number: 20100234422
    Abstract: Compounds of the following structure are provided, wherein n, R1-R3 and R6-R9 are defined below, as are methods of preparing and using these compounds for contraception; treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms.
    Type: Application
    Filed: May 26, 2010
    Publication date: September 16, 2010
    Applicant: Wyeth LLC
    Inventors: Casey Cameron McComas, Andrew Fensome
  • Patent number: 7786104
    Abstract: The invention concerns compounds of general formula (I): Wherein n, X1, X2, X3, X4, Y, Z, Z1, Z2, Z3 and Z4 are as defined herein. The invention also concerns a process for the preparation of compounds of formula (I) and their therapeutic use.
    Type: Grant
    Filed: January 26, 2009
    Date of Patent: August 31, 2010
    Assignee: Sanofi-Aventis
    Inventors: Laurent DuBois, Yannick Evanno, Andre Malanda, David Machnik, Catherine Gille
  • Patent number: 7781438
    Abstract: A compound of formula (I) wherein R, R1, and R2, ring A and ring B are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 10, 2006
    Date of Patent: August 24, 2010
    Assignee: Novartis AG
    Inventors: Jürgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
  • Patent number: 7776999
    Abstract: A molecular probe comprises two arsenic atoms and at least one cyanine based moiety. A method of producing a molecular probe includes providing a molecule having a first formula, treating the molecule with HgOAc, and subsequently transmetallizing with AsCl3. The As is liganded to ethanedithiol to produce a probe having a second formula. A method of labeling a peptide includes providing a peptide comprising a tag sequence and contacting the peptide with a biarsenical molecular probe. A complex is formed comprising the tag sequence and the molecular probe. A method of studying a peptide includes providing a mixture containing a peptide comprising a peptide tag sequence, adding a biarsenical probe to the mixture, and monitoring the fluorescence of the mixture.
    Type: Grant
    Filed: April 12, 2007
    Date of Patent: August 17, 2010
    Assignee: Battelle Memorial Institute
    Inventors: M. Uljana Mayer-Cumblidge, Haishi Cao
  • Patent number: 7759380
    Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
    Type: Grant
    Filed: May 8, 2007
    Date of Patent: July 20, 2010
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly White, Hong Ye, Leonard R. Hecker
  • Patent number: 7750038
    Abstract: Compounds of the following structure are provided, wherein n, R1-R3 and R6-R9 are defined below, as are methods of preparing and using these compounds for contraception; treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms.
    Type: Grant
    Filed: March 4, 2008
    Date of Patent: July 6, 2010
    Assignee: Wyeth LLC
    Inventors: Casey Cameron McComas, Andrew Fensome
  • Patent number: 7745435
    Abstract: The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: June 29, 2010
    Assignee: Gemix X Pharmaceuticals Canada Inc.
    Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrence W. Doyle
  • Patent number: 7737166
    Abstract: A 1,6-?-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-?-glucan synthesis inhibition. Also provided is a drug, a salt or hydrate thereof, especially an antifungal that contains the compound.
    Type: Grant
    Filed: August 16, 2006
    Date of Patent: June 15, 2010
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Katsuhiro Kawakami, Kazuo Kanai, Takao Horiuchi, Hiroshi Takeshita, Syozo Kobayashi, Yuichi Sugimoto, Issei Achiwa, Junichi Kuroyanagi
  • Publication number: 20100137280
    Abstract: The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl, is a single or double bond; X1 and X2 are N, CRx1, NRx2, or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.
    Type: Application
    Filed: March 20, 2008
    Publication date: June 3, 2010
    Applicant: ABBOTT GMBH & CO. KG
    Inventors: Thomas Schultz, SR., Wilfried Braje, Sean Colm Turner, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Matthias Mayrer
  • Publication number: 20100130468
    Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula (I): wherein R1, R2, R3, R4, and m are as defined herein. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, rhinitis, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: March 20, 2008
    Publication date: May 27, 2010
    Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
  • Publication number: 20100111862
    Abstract: The present invention relates to novel radiolabelled inhibitors of formula I for the Glycine 1 transporter (GlyT1), useful for the labelling and diagnostic imaging of the glycine 1 transporter functionality. wherein R1 is isopropoxy or 2,2,2-trifluoro-1-methyl-ethoxy; and R2 is a radiolabelled group CH3, wherein the radionuclide is 3H or 11C. The radiolabelled compounds of formula I may be used as PET (Positron Emission Tomography) radiotracer for the labelling and diagnostic molecular imaging of the glycine 1 transporter functionality.
    Type: Application
    Filed: October 28, 2009
    Publication date: May 6, 2010
    Inventors: Daniela Alberati, Edilio Maurizio Borroni, Thomas Hartung, Roger Norcross, Emmanuel Pinard
  • Patent number: 7709477
    Abstract: The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: May 4, 2010
    Assignee: Gemin X Pharmaceuticals Canada Inc.
    Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrence W. Doyle
  • Patent number: 7691861
    Abstract: A compound of formula I wherein R, Ra, Rb, Rc, Rd and Re are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: January 19, 2005
    Date of Patent: April 6, 2010
    Assignee: Novartis AG
    Inventors: Maurice Van Eis, Peter Von Matt, Jürgen Wagner, Jean-Pierre Evenou
  • Publication number: 20100041628
    Abstract: Disclosed is a compound represented by the general formula (1) or a salt thereof. The compound or a salt thereof has an inhibitory activity on IKK? and is therefore useful as preventive and/or therapeutic agent for a disease associated with IKK?. In the formula, R1 represents a hydrogen atom, a lower alkyl group, an aryl group, a hydroxy group, or the like; R2 represents a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or the like; and m represents 0, 1, 2, or the like.
    Type: Application
    Filed: January 15, 2008
    Publication date: February 18, 2010
    Inventors: Hiroshi Enomoto, Kenji Kawashima, Kazuhiro Kudou, Minoru Yamamoto, Masaaki Murai, Takaaki Inaba, Noriko Ishizaka
  • Patent number: 7648989
    Abstract: This invention relates to PKC inhibitors which are able to selectively inhibit e.g. the and optionally 0, isoforms of PKC, and their use in particular in transplantation.
    Type: Grant
    Filed: January 19, 2005
    Date of Patent: January 19, 2010
    Assignee: Novartis AG
    Inventors: Maurice Van Eis, Peter Von Matt, Jürgen Wagner, Jean-Pierre Evenou, Walter Schuler
  • Patent number: 7576082
    Abstract: The invention describes compounds of the general formula I or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are herein described, a process for their manufacture, medicaments containing them as well as the use of these compounds as pharmaceutically active agents. The compounds show activity as antiproliferative agents and may be especially useful for the treatment of cancer.
    Type: Grant
    Filed: June 20, 2006
    Date of Patent: August 18, 2009
    Assignee: Hoffman-La Roche Inc.
    Inventors: Kin-Chun Luk, Sung-Sau So, Jing Zhang, Zhuming Zhang
  • Patent number: 7572824
    Abstract: Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrile groups, and the products thereby are provided.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: August 11, 2009
    Assignee: Wyeth
    Inventor: Bogdan K. Wilk
  • Publication number: 20090192157
    Abstract: The invention features methods of treating visceral pain or a condition in a mammal caused by the action of nitric oxide synthase (NOS) or by the action of serotonin 5HT1D/1B receptors, by administering to a patient in need thereof a therapeutically effective amount of an indole compound of Formula (I), or a pharmaceutically acceptable salt or prodrug thereof. The methods of the invention may further comprise the administration of additional therapeutic agent. The invention also features new compounds of Formula (I), pharmaceutical compositions thereof, and methods of resolving enantiomeric mixtures.
    Type: Application
    Filed: November 17, 2008
    Publication date: July 30, 2009
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi, John S. Andrews, Gabriela Mladenova
  • Patent number: 7553836
    Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1a, R1b, R1c, Q, A, R3, W, D and R2 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: February 5, 2007
    Date of Patent: June 30, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventor: Guohua Zhao
  • Publication number: 20090163518
    Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.
    Type: Application
    Filed: March 4, 2009
    Publication date: June 25, 2009
    Inventors: Roger Bonnert, Rukhsana Rasul
  • Patent number: 7528124
    Abstract: A 1,3-dihydro-2H-indol-2-one derivative expressed by Formula 1 (wherein R1 is a halogen atom, a C1 to C4 alkyl group, etc., and R2 is a hydrogen atom, a halogen atom, etc., or R2 is in the 6-position of the indol-2-one and R1 and R2 join together to form a C3 to C6 alkylene group, R3 is a halogen atom, a hydroxyl group, etc., and R4 is a hydrogen atom, a halogen atom, a C1 to C4 alkyl group, etc., or R4 is in the 3-position of the phenyl and R3 and R4 join together to form a methylenedioxy group, R5 is a hydrogen atom or a fluorine atom, R6 is an ethylamino group, a dimethylamino group, etc., R7 is a C1 to C4 alkoxy group, and R8 is a C1 to C4 alkoxy group), or a pharmaceutically acceptable salt of this derivative. This is a novel compound that has antagonistic activity against an aruginine-vasopressin V1b receptor.
    Type: Grant
    Filed: August 27, 2004
    Date of Patent: May 5, 2009
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Toshihito Kumagai, Takeshi Kuwada, Tsuyoshi Shibata, Masato Hayashi, Yuri Fujisawa, Yoshinori Sekiguchi
  • Patent number: 7514452
    Abstract: The present invention provides 2-furancarboxylic acid hydrazide compounds represented by General Formula (I) below, and prodrugs, physiologically acceptable salts, hydrates, solvates thereof: wherein A is a group represented by Formula (a) or the like: (wherein either R4 or R5 represents cyano, nitro or the like, and the other represents a hydrogen atom or the like); either R1 or R2 represents a group: -D-(X)m-R6 or the like, and the other represents a group: -E-(Y)n-R7, hydrogen atom, aryl or the like; R3 is a hydrogen atom or the like; D and E independently represent aryl; X and Y independently represent O or the like; R6 and R7 independently represent alkyl, aryl, arylalkyl or the like; and m and n are independently 0 or 1, provided that the aryl is optionally substituted.
    Type: Grant
    Filed: January 30, 2003
    Date of Patent: April 7, 2009
    Assignee: Dainippon Pharmaceutical Co., Ltd
    Inventors: Akihito Fujii, Toshiyuki Negoro, Chiaki Migihashi, Makoto Murata, Keiji Nakamura, Takashi Nukuda, Takafumi Matsumoto, Kiyomi Imano
  • Patent number: 7511071
    Abstract: Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies.
    Type: Grant
    Filed: March 7, 2008
    Date of Patent: March 31, 2009
    Assignee: Wyeth
    Inventor: Bogdan Kazimierz Wilk
  • Patent number: 7491788
    Abstract: Melt blended compositions, comprising up to 20 wt % of an optional additive, and 80-100 wt % of a copolycarbonate having a Tg of 200° C. or more of (1) wherein the mole ratio of x:y is 35:65 to 90:10, R1 is derived from a dihydroxy compound (2) wherein R3 and R5 are each independently a halogen or a C1-6 alkyl group, R4 is a C1-6 alkyl, phenyl, or phenyl substituted with up to five halogens or C1-6 alkyl groups, and each c is independently 0 to 4; R2 is derived from a dihydroxy compound (6): wherein Ra and Rb are each independently a halogen atom or a monovalent C1-6 alkyl group; p and q are each independently integers of 0 to 4; and Xa is a divalent group; and 95 to 5 wt % of a polycarbonate having a Tg of less than 200° C. of formula (9) wherein R9 derived from a dihydroxy compound of formula (6); and 0.001 to 0.1 wt % of a transesterification catalyst.
    Type: Grant
    Filed: June 29, 2006
    Date of Patent: February 17, 2009
    Assignee: SABIC Innovative Plastics IP B.V.
    Inventors: Chiel Albertus Leenders, Brian Mullen, Adam S Zerda
  • Publication number: 20080318975
    Abstract: A compound of formula (I) wherein R, R1, and R2, ring A and ring B are as defined in the specification, processes for their production, their uses, in particular in transplantation, and pharmaceutical compositions containing them.
    Type: Application
    Filed: July 10, 2006
    Publication date: December 25, 2008
    Inventors: Jurgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
  • Publication number: 20080318923
    Abstract: It is intended to provide a drug which is efficacious against pathological conditions relating to arginine-vasopressin V1b receptor. More particularly speaking, it is intended to provide a drug which has a therapeutic or preventive effect on depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorders, hypertension, digestive diseases, drug addiction, epilepsy, brain infarction, brain ischemia, brain edema, head injury, inflammation, immune diseases, alopecia and so on. As the results of intensive studies, a novel 1,3-dihydro-2H-indol-2-one compound and a pyrrolidin-2-one compound fused with a heteroaromatic ring, which are highly selective antagonists of arginine-vasopressin V1b receptor, have high metabolic stabilities and show favorable brain penetration and high plasma concentrations, are found, thereby achieving the above objective.
    Type: Application
    Filed: January 30, 2006
    Publication date: December 25, 2008
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Yoshinori Sekiguchi, Takeshi Kuwada, Masato Hayashi, Dai Nozawa, Yuri Amada, Tsuyoshi Shibata, Shuji Yamamoto, Hiroshi Ohta, Taketoshi Okubo, Takeshi Koami
  • Publication number: 20080318902
    Abstract: The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.
    Type: Application
    Filed: July 18, 2008
    Publication date: December 25, 2008
    Applicant: Gemin X Pharmaceuticals Canada Inc.
    Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrence W. Doyle
  • Patent number: 7456183
    Abstract: Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C?O, C?S, S?O, SO2, S, O, (CR6R7)n, C(?O)—(CR6R7)n, and C(?S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of (formula I) and L is selected from the group consisting of N, O, S?O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r2) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.
    Type: Grant
    Filed: April 8, 2002
    Date of Patent: November 25, 2008
    Assignee: Novartis Vaccines and Diagnostics, Inc.
    Inventors: Daniel Chu, Rustum Boyce, David Duhl, Bryan Chang
  • Patent number: 7452881
    Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: November 18, 2008
    Assignee: Laboratories Del Dr. Esteve, S.A.
    Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
  • Patent number: 7449459
    Abstract: The invention relates to compounds of general formula I as well as the production and use thereof as a medication.
    Type: Grant
    Filed: March 23, 2007
    Date of Patent: November 11, 2008
    Assignee: Bayer Schering Pharma AG
    Inventors: Bernd Buchmann, Dirk Kosemund, Bernd Menzenbach, Martin Fritsch
  • Publication number: 20080269200
    Abstract: Indole carboxamide compounds of Formula (I): are provided as inhibitors of kinase activity, in particular IKK2 activity as well as compositions and medicaments containing them, for use in inflammatory and tissue repair disorders.
    Type: Application
    Filed: January 13, 2005
    Publication date: October 30, 2008
    Applicant: SmithKline Beecham Corporation
    Inventors: Ian Robert Baldwin, Paul Bamborough, John Andrew Christopher, Jeffrey K Kerns, Timothy Longstaff, David Drysdale Miller
  • Publication number: 20080242675
    Abstract: This invention relates to PKC inhibitors which are able to selectively inhibit e.g. the and optionally 0, isoforms of PKC, and their use in particular in transplantation.
    Type: Application
    Filed: January 19, 2005
    Publication date: October 2, 2008
    Inventors: Maurice Van Eis, Peter Von Matt, Jurgen Wagner, Jean-Pierre Evenou, Walter Schuler