The Additional Hetero Ring Is Bonded Directly To A Ring Carbon Of The Bicyclo Ring System Patents (Class 548/466)
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Publication number: 20110124668Abstract: The present invention relates to synthetic studies on novel indole derivatives having a carbamoyl group, a ureido group and a substituted oxy group or a salt thereof, and pharmaceutical actions of the derivatives. The compound and a salt thereof represented by the general formula (1) has an IKK? inhibitory activity and is useful as a preventive and/or therapeutic agent for diseases considered to be associated with IKK?.Type: ApplicationFiled: July 14, 2009Publication date: May 26, 2011Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Kenji Kawashima, Hiroshi Enomoto, Minoru Yamamoto, Masaaki Murai
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Patent number: 7947713Abstract: 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: GrantFiled: October 30, 2007Date of Patent: May 24, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Henry Joseph Breslin, Hans Louis Jos De Winter, Michael Joseph Kukla
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Publication number: 20110098483Abstract: 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: ApplicationFiled: March 27, 2009Publication date: April 28, 2011Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Nicos A. Petasis, Malgorzata Myslinska
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Patent number: 7915260Abstract: 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: GrantFiled: January 10, 2007Date of Patent: March 29, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Publication number: 20110071132Abstract: 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: ApplicationFiled: July 30, 2010Publication date: March 24, 2011Applicant: Abbott GmbH & Co. KGInventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Andrea Hager-Wernet, Wilfried Hornberger, Liliane Unger
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Patent number: 7902379Abstract: 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: GrantFiled: September 30, 2004Date of Patent: March 8, 2011Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Wilfried Hornberger, Thorsten K. Oost, Daryl Richard Sauer, Liliane Unger, Wolfgang Wernet, Hervé Geneste
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Patent number: 7897601Abstract: 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: GrantFiled: January 16, 2007Date of Patent: March 1, 2011Assignees: 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
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Publication number: 20110046367Abstract: 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: ApplicationFiled: November 1, 2010Publication date: February 24, 2011Applicant: President and Fellows of Harvard CollegeInventors: José A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
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Publication number: 20110028519Abstract: 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: ApplicationFiled: October 11, 2010Publication date: February 3, 2011Inventor: Michael C. Pirrung
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Publication number: 20110021556Abstract: 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: ApplicationFiled: March 10, 2009Publication date: January 27, 2011Applicant: Hoffman-La Roche, Inc.Inventors: Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
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Publication number: 20110021785Abstract: 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: ApplicationFiled: January 20, 2010Publication date: January 27, 2011Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
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Publication number: 20100317100Abstract: 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: ApplicationFiled: June 11, 2010Publication date: December 16, 2010Inventors: Soumen Paul, Debasree Dutta, Soma Ray, Jeffrey Aube, Frank John Schoenen
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Patent number: 7825155Abstract: 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: GrantFiled: September 13, 2006Date of Patent: November 2, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Publication number: 20100273774Abstract: 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: ApplicationFiled: July 9, 2010Publication date: October 28, 2010Inventors: Jürgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
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Publication number: 20100273824Abstract: 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: ApplicationFiled: January 18, 2008Publication date: October 28, 2010Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
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Patent number: 7820672Abstract: 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: GrantFiled: February 12, 2004Date of Patent: October 26, 2010Assignee: Novartis AGInventors: Peter Von Matt, Jürgen Wagner
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Patent number: 7812017Abstract: 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: GrantFiled: July 3, 2007Date of Patent: October 12, 2010Assignee: Biovitrum AB (publ.)Inventors: Johan Angbrant, Rune Ringom, Kristin Hammer, Erik Ringberg, Bengt Lindqvist, Gary Johansson, Peter Brandt, Katarina Beierlein, Björn M Nilsson
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Publication number: 20100252112Abstract: 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: ApplicationFiled: April 6, 2010Publication date: October 7, 2010Inventor: Mark D. Watson
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Publication number: 20100240650Abstract: 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: ApplicationFiled: May 25, 2010Publication date: September 23, 2010Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly White, Hong Ye, Leonard R. Hecker, Bruce Conway, Keith Demarest
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Publication number: 20100234422Abstract: 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: ApplicationFiled: May 26, 2010Publication date: September 16, 2010Applicant: Wyeth LLCInventors: Casey Cameron McComas, Andrew Fensome
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Patent number: 7786104Abstract: 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: GrantFiled: January 26, 2009Date of Patent: August 31, 2010Assignee: Sanofi-AventisInventors: Laurent DuBois, Yannick Evanno, Andre Malanda, David Machnik, Catherine Gille
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Patent number: 7781438Abstract: 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: GrantFiled: July 10, 2006Date of Patent: August 24, 2010Assignee: Novartis AGInventors: Jürgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
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Patent number: 7776999Abstract: 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: GrantFiled: April 12, 2007Date of Patent: August 17, 2010Assignee: Battelle Memorial InstituteInventors: M. Uljana Mayer-Cumblidge, Haishi Cao
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Patent number: 7759380Abstract: 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: GrantFiled: May 8, 2007Date of Patent: July 20, 2010Assignee: Janssen Pharmaceutica, NVInventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly White, Hong Ye, Leonard R. Hecker
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Patent number: 7750038Abstract: 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: GrantFiled: March 4, 2008Date of Patent: July 6, 2010Assignee: Wyeth LLCInventors: Casey Cameron McComas, Andrew Fensome
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Patent number: 7745435Abstract: 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: GrantFiled: July 18, 2008Date of Patent: June 29, 2010Assignee: Gemix X Pharmaceuticals Canada Inc.Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrence W. Doyle
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Patent number: 7737166Abstract: 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: GrantFiled: August 16, 2006Date of Patent: June 15, 2010Assignee: Daiichi Sankyo Company, LimitedInventors: Katsuhiro Kawakami, Kazuo Kanai, Takao Horiuchi, Hiroshi Takeshita, Syozo Kobayashi, Yuichi Sugimoto, Issei Achiwa, Junichi Kuroyanagi
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Publication number: 20100137280Abstract: 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: ApplicationFiled: March 20, 2008Publication date: June 3, 2010Applicant: ABBOTT GMBH & CO. KGInventors: Thomas Schultz, SR., Wilfried Braje, Sean Colm Turner, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Matthias Mayrer
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Publication number: 20100130468Abstract: 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: ApplicationFiled: March 20, 2008Publication date: May 27, 2010Inventors: Jeffrey Charles Boehm, Jakob Busch-Petersen, Wei Fu, Qi Jin, Jeffrey K. Kerns, Huijie Li, Guoliang Lin, Xichen Lin, Christopher E. Neipp
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Publication number: 20100111862Abstract: 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: ApplicationFiled: October 28, 2009Publication date: May 6, 2010Inventors: Daniela Alberati, Edilio Maurizio Borroni, Thomas Hartung, Roger Norcross, Emmanuel Pinard
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Patent number: 7709477Abstract: 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: GrantFiled: July 18, 2008Date of Patent: May 4, 2010Assignee: Gemin X Pharmaceuticals Canada Inc.Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrence W. Doyle
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Patent number: 7691861Abstract: 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: GrantFiled: January 19, 2005Date of Patent: April 6, 2010Assignee: Novartis AGInventors: Maurice Van Eis, Peter Von Matt, Jürgen Wagner, Jean-Pierre Evenou
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Publication number: 20100041628Abstract: 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: ApplicationFiled: January 15, 2008Publication date: February 18, 2010Inventors: Hiroshi Enomoto, Kenji Kawashima, Kazuhiro Kudou, Minoru Yamamoto, Masaaki Murai, Takaaki Inaba, Noriko Ishizaka
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Patent number: 7648989Abstract: 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: GrantFiled: January 19, 2005Date of Patent: January 19, 2010Assignee: Novartis AGInventors: Maurice Van Eis, Peter Von Matt, Jürgen Wagner, Jean-Pierre Evenou, Walter Schuler
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Patent number: 7576082Abstract: 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: GrantFiled: June 20, 2006Date of Patent: August 18, 2009Assignee: Hoffman-La Roche Inc.Inventors: Kin-Chun Luk, Sung-Sau So, Jing Zhang, Zhuming Zhang
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Patent number: 7572824Abstract: 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: GrantFiled: November 16, 2007Date of Patent: August 11, 2009Assignee: WyethInventor: Bogdan K. Wilk
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Publication number: 20090192157Abstract: 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: ApplicationFiled: November 17, 2008Publication date: July 30, 2009Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi, John S. Andrews, Gabriela Mladenova
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Patent number: 7553836Abstract: 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: GrantFiled: February 5, 2007Date of Patent: June 30, 2009Assignee: Bristol-Myers Squibb CompanyInventor: Guohua Zhao
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Publication number: 20090163518Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.Type: ApplicationFiled: March 4, 2009Publication date: June 25, 2009Inventors: Roger Bonnert, Rukhsana Rasul
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Patent number: 7528124Abstract: 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: GrantFiled: August 27, 2004Date of Patent: May 5, 2009Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Toshihito Kumagai, Takeshi Kuwada, Tsuyoshi Shibata, Masato Hayashi, Yuri Fujisawa, Yoshinori Sekiguchi
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Patent number: 7514452Abstract: 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: GrantFiled: January 30, 2003Date of Patent: April 7, 2009Assignee: Dainippon Pharmaceutical Co., LtdInventors: Akihito Fujii, Toshiyuki Negoro, Chiaki Migihashi, Makoto Murata, Keiji Nakamura, Takashi Nukuda, Takafumi Matsumoto, Kiyomi Imano
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Patent number: 7511071Abstract: 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: GrantFiled: March 7, 2008Date of Patent: March 31, 2009Assignee: WyethInventor: Bogdan Kazimierz Wilk
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Patent number: 7491788Abstract: 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: GrantFiled: June 29, 2006Date of Patent: February 17, 2009Assignee: SABIC Innovative Plastics IP B.V.Inventors: Chiel Albertus Leenders, Brian Mullen, Adam S Zerda
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Publication number: 20080318902Abstract: 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: ApplicationFiled: July 18, 2008Publication date: December 25, 2008Applicant: Gemin X Pharmaceuticals Canada Inc.Inventors: Giorgio Attardo, Jean-Francois Lavallee, Elise Rioux, Sasmita Tripathy, Terrence W. Doyle
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Publication number: 20080318923Abstract: 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: ApplicationFiled: January 30, 2006Publication date: December 25, 2008Applicant: 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
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Publication number: 20080318975Abstract: 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: ApplicationFiled: July 10, 2006Publication date: December 25, 2008Inventors: Jurgen Wagner, Maurice Van Eis, Peter Von Matt, Jean-Pierre Evenou, Walter Schuler
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Patent number: 7456183Abstract: 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: GrantFiled: April 8, 2002Date of Patent: November 25, 2008Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Daniel Chu, Rustum Boyce, David Duhl, Bryan Chang
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Patent number: 7452881Abstract: 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: GrantFiled: February 16, 2007Date of Patent: November 18, 2008Assignee: Laboratories Del Dr. Esteve, S.A.Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
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Patent number: 7449459Abstract: The invention relates to compounds of general formula I as well as the production and use thereof as a medication.Type: GrantFiled: March 23, 2007Date of Patent: November 11, 2008Assignee: Bayer Schering Pharma AGInventors: Bernd Buchmann, Dirk Kosemund, Bernd Menzenbach, Martin Fritsch
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Publication number: 20080269200Abstract: 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: ApplicationFiled: January 13, 2005Publication date: October 30, 2008Applicant: SmithKline Beecham CorporationInventors: Ian Robert Baldwin, Paul Bamborough, John Andrew Christopher, Jeffrey K Kerns, Timothy Longstaff, David Drysdale Miller