Polycyclo Ring System Having One Of The Two Rings Which Form The Spiro As One Of The Cyclos Patents (Class 548/411)
  • Patent number: 10858322
    Abstract: Disclosed are a method for preparing an imidazole derivative and crystal form A and crystal form B thereof, and also disclosed is a method for preparing a compound of formula (I) and an intermediate thereof.
    Type: Grant
    Filed: March 20, 2020
    Date of Patent: December 8, 2020
    Assignee: SHANDONG DANHONG PHARMACEUTICAL CO., LTD.
    Inventors: Weihua Shi, Feng Xu, Zheng Wang, Weidong Li, Linghui Wu, Hongwei Li, Minggao Zeng, Kunmin Lai, Zhigan Jiang, Haiying He
  • Patent number: 10835514
    Abstract: Pharmaceutical compositions of muscarinic acetylcholine receptor antagonists suitable for administration via a dry powdered inhaler and methods of using the compositions for treating respiratory disease are provided.
    Type: Grant
    Filed: January 7, 2017
    Date of Patent: November 17, 2020
    Assignee: THERON PHARMACEUTICALS, INC.
    Inventors: Meenakshi S. Venkatraman, Xiaoming Zhang, Phillip Haywood
  • Publication number: 20150031691
    Abstract: The present invention relates to compounds represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
    Type: Application
    Filed: October 8, 2014
    Publication date: January 29, 2015
    Inventors: Lawrence Wayne Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh B. Singh, Yajun Zheng
  • Patent number: 8889703
    Abstract: The present invention relates to compounds represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
    Type: Grant
    Filed: February 23, 2011
    Date of Patent: November 18, 2014
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Lawrence W. Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh Singh, Yajun Zheng
  • Patent number: 8889897
    Abstract: The present invention relates to a process for obtaining a compound of formula (1), (2) or (3) by means of a electrocarboxylation with CO2. The present invention also relates to the new intermediates (1) and (2). The present invention further relates to the use of intermediates (1) and (2) as starting materials for the synthesis of SPAN derivatives.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: November 18, 2014
    Assignee: Air Products and Chemicals, Inc.
    Inventors: J Oriol Osso, Lourdes F. Vega, Illuminado Gallardo, Gonzalo Guirado, Ana Belen Gomez, Francisca Irene Reche
  • Patent number: 8877796
    Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: November 4, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Shanghai Yu, Wei Sun, Sanjeev Kumar, Duxin Sun, Peng Zou, Donna McEachern, Yujun Zhao
  • Patent number: 8877797
    Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.
    Type: Grant
    Filed: February 19, 2013
    Date of Patent: November 4, 2014
    Assignee: Board of Regents of The University of Texas System
    Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
  • Publication number: 20140309434
    Abstract: The patent discloses novel 2,2-disubstituted 1,2-dihydro-3H-indol-3-one derivatives and their preparation thereof.
    Type: Application
    Filed: April 4, 2014
    Publication date: October 16, 2014
    Applicant: Council of Scientific & Industrial Research
    Inventors: Venkata Ramana Chepuri, Yogesh Mansukhabhai Goriya
  • Publication number: 20140288091
    Abstract: Beta-secretase inhibitors, of formula (I) as described in the specification, pharmaceutical compositions comprising them and therapeutic methods using them for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's Disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
    Type: Application
    Filed: October 10, 2012
    Publication date: September 25, 2014
    Applicants: ASTRAZENECA AB, ASTRAZENECA AB
    Inventors: Anna Minidis, Fredrik Rahm, Jenny Viklund
  • Patent number: 8772288
    Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: July 8, 2014
    Assignee: Almirall, S.A.
    Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
  • Publication number: 20140163175
    Abstract: Conventional cross-linked cyclic olefin polymers do not have a sufficiently low linear expansion coefficient. A compound having a structure represented by the following formula (a).
    Type: Application
    Filed: July 25, 2012
    Publication date: June 12, 2014
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Seiji Okada, Ryo Ogawa
  • Patent number: 8742131
    Abstract: Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetyl-choline receptor-mediated diseases, such as pulmonary diseases, are provided.
    Type: Grant
    Filed: January 27, 2011
    Date of Patent: June 3, 2014
    Assignee: Theron Pharmaceuticals, Inc.
    Inventors: Jürg R. Pfister, Gwenaella Rescourio, Meenakshi S. Venkatraman, Xiaoming Zhang
  • Patent number: 8633212
    Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: January 21, 2014
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbH
    Inventors: Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Klaus Fuchs, Niklas Heine, Lanqi Jia, Katerina Leftheris, Brian McKeever, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Guosheng Wu, Zhongren Wu, Zhenrong Xu, Jing Yuan, Yajun Zheng
  • Publication number: 20130231604
    Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Application
    Filed: March 3, 2012
    Publication date: September 5, 2013
    Applicant: NANOQUANTUM SCIENCES, INC.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Patent number: 8497295
    Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: July 30, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Lewis R. Makings, Miguel Garcia-Guzman Blanco, Dennis J. Hurley, Ioana Drutu, Gabriel Raffai, Daniele M. Bergeron, Akiko Nakatani, Andreas P. Termin, Alina Silina
  • Patent number: 8431407
    Abstract: Temperature and/or irradiation and/or polymerization indicators comprise at least one 1,3-dipole and at least one dipolarophile, the dipole preferably being an ylide from the group of azomethines (sydnones), azomethinylides (munchnones), carbonylylides (isomunchnones), thiocarbonylylides (thioisomunchnones), or 1,3-dithiolylium-4-olates.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: April 30, 2013
    Assignee: Heraeus Kulzer GmbH
    Inventor: Andreas Grundler
  • Publication number: 20130102604
    Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1. The compound may be used, for example, for the treatment or prophylaxis of obesity, hyperglycemia, dyslipidemia, and type 1 or type 2 diabetes.
    Type: Application
    Filed: December 10, 2012
    Publication date: April 25, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130053377
    Abstract: The present invention relates to compounds represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Definitions for the variables are provided herein.
    Type: Application
    Filed: February 23, 2011
    Publication date: February 28, 2013
    Applicant: Vitae Pharmaceuticals, Inc.
    Inventors: Lawrence W. Dillard, Jing Yuan, Katerina Leftheris, Shankar Venkatraman, Guosheng Wu, Lanqi Jia, Zhenrong Xu, Salvacion Cacatian, Angel Morales-Ramos, Suresh Singh, Yajun Zheng
  • Publication number: 20130040935
    Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders.
    Type: Application
    Filed: February 8, 2011
    Publication date: February 14, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ningshu Liu, Kai Thede, Philip Lienau, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Maher Najjar, Knut Eis, Reiner Fischer, Wahed Ahmed Moradi
  • Patent number: 8354443
    Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1. The compound may be used, for example, for the treatment or prophylaxis of obesity, hyperglycemia, dyslipidemia, and type 1 or type 2 diabetes.
    Type: Grant
    Filed: December 3, 2010
    Date of Patent: January 15, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Lichun Feng, Yun He, Mengwei Huang, Hongying Yun
  • Publication number: 20130012702
    Abstract: Methods for purifying a compound of formula I are provided, wherein A, B, X, Q, and R1 are defined herein. The methods include mixing the compound of formula I and a solvent; adding a base to the solvent; and precipitating purified compound of formula I.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicant: Wyeth LLC
    Inventors: Bogdan Kazimierz Wilk, Arkadiy Zinoviy Rubezhov, Anthony Francis Hadfield, Jean Louise Helom
  • Patent number: 8334317
    Abstract: The present invention relates generally to novel calcimimetic compounds and pharmaceutical compositions comprising them. The invention also relates to methods of treating of diseases or disorders related to the function of the calcium sensing receptor using the compounds represented in Formula I.
    Type: Grant
    Filed: October 15, 2008
    Date of Patent: December 18, 2012
    Assignee: Amgen Inc.
    Inventors: Thomas S. Coulter, Christopher H. Fotsch, Chiara Ghiron, Paul E. Harrington, Michael G. Kelly, Philip Miller, Gilbert M. Rishton, David J. St. Jean, Jr., David J. Semin
  • Patent number: 8288430
    Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: October 16, 2012
    Assignee: Grunenthal GmbH
    Inventors: Saskia Zemolka, Stefan Schunk, Klaus Linz, Wolfgang Schröder, Werner Englberger, Fritz Theil, Birgit Roloff
  • Publication number: 20120225873
    Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Application
    Filed: April 13, 2012
    Publication date: September 6, 2012
    Applicant: Myrexis, Inc.
    Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
  • Patent number: 8088931
    Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: January 3, 2012
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
  • Publication number: 20110294783
    Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.
    Type: Application
    Filed: August 10, 2011
    Publication date: December 1, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
  • Publication number: 20110224334
    Abstract: A near-infrared-ray absorbing material which contains a cyanine compound represented by general formula (I), shows a narrow peak of light absorption in the range of wavelengths of 800-1,000 nm, and has excellent light resistance. In formula (I), R1 to R4, Y1, and Y2 each represents a hydrogen atom, a group of formula (II) or (II?), etc., and Anq? represents a q-valent anion, provided that at least R1 is a group of formula (II) or (II') or Anq? is an ion of formula (III); R11 to R13 each represents a hydrogen atom, hydroxy, etc.; and Z1 and Z2 each represents a C1-10 alkyl, etc. In formula (II?), the bond between G? and T? is a double bond or a conjugated double bond; G? represents a carbon atom; T? represents a carbon atom or a nitrogen atom; the ring including G? and T? represents a 6-membered ring, etc.; w? is 0-4; and R01? represents a hydrogen atom, hydroxy, etc. In formula (III), R5 and R6 each represents a C1-8 haloalkyl.
    Type: Application
    Filed: November 18, 2009
    Publication date: September 15, 2011
    Applicant: ADEKA CORPORATION
    Inventors: Yosuke Maeda, Ryoya Otsuki, Koichi Shigeno
  • Publication number: 20110178311
    Abstract: Processes are provided for purifying a compound of the structure (I): wherein, A, B, T, Q and R1 are defined herein, and wherein the process includes dissolving the compound of formula I in a solution containing acetone, water and a base at about 30° C.; filtering the solution containing the compound of formula I at about 30° C.; and precipitating the purified compound of formula I by adjusting the filtered solution to an acidic pH. Desirably, the compound of formula I is 5-(2-thioxospiro[cyclohexane-1,3-[3H]indol]-5-yl)-1-methylpyrrole-2-carbonitrile or tanaproget.
    Type: Application
    Filed: April 1, 2011
    Publication date: July 21, 2011
    Applicant: Wyeth LLC
    Inventors: Mahmut Levent, Panolil Raveendranath, Bogdan Wilk, Donald Carl Boop, Marinus Cornelis Hofman
  • Publication number: 20110150757
    Abstract: The present invention relates to compounds of Formula (I), below, (wherein R1, R2, R3, R27, R28, R29, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.
    Type: Application
    Filed: October 16, 2008
    Publication date: June 23, 2011
    Inventors: M. Arshad Siddiqui, Chaoyang Dai, Umar Faruk Mansoor, Liping Yang, Lalalnthi Dilrukshi Vitharana, Angie R. Angeles
  • Publication number: 20110144106
    Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1.
    Type: Application
    Filed: December 3, 2010
    Publication date: June 16, 2011
    Inventors: Li Chen, Lichun Feng, Yun He, Mengwei Huang, Hongying Yun
  • Publication number: 20110124622
    Abstract: The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Application
    Filed: July 1, 2009
    Publication date: May 26, 2011
    Applicant: Genentech, Inc.
    Inventors: Emanuela Gancia, Robert Andrew Heald, Philip Jackson, Stephen Price
  • Patent number: 7935721
    Abstract: This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.
    Type: Grant
    Filed: December 30, 2009
    Date of Patent: May 3, 2011
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Jianyu Sun, Shifeng Liu, Jianmin Fu
  • Publication number: 20110053936
    Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: April 3, 2009
    Publication date: March 3, 2011
    Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernat Vidal Juan, Nuria Aguilar Izquierdo
  • Patent number: 7776874
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
    Type: Grant
    Filed: June 10, 2008
    Date of Patent: August 17, 2010
    Assignee: Incyte Corporation
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
  • Patent number: 7723372
    Abstract: There are provided compounds of the general formulas wherein W, X, Y, R1, R2, R3, and R4 are as described herein. The compounds exhibit anticancer activity.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: May 25, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventor: Jin-Jun Liu
  • Publication number: 20100113791
    Abstract: Precursors of carbenes of CAAC type (Cyclic)(Alkyl)(Amino)(Carbenes) are prepared and carbenes are produced therefrom; novel synthesis intermediates are provided for preparing the precursors of CAAC-type carbenes.
    Type: Application
    Filed: April 9, 2008
    Publication date: May 6, 2010
    Inventor: Gérard Mignani
  • Publication number: 20090239889
    Abstract: There are provided compounds of the general formulas wherein W, X, Y, R1, R2, R3, and R4 are as described herein. The compounds exhibit anticancer activity.
    Type: Application
    Filed: February 18, 2009
    Publication date: September 24, 2009
    Inventor: Jin-Jun Liu
  • Publication number: 20090098410
    Abstract: Disclosed is a trimethine dimer compound represented by the following general formula (I) and optical recording medium containing such a compound in a recording layer. (I)(In the formula, symbols are as in the description. When both Xa2 and Xb2 are imino groups, one of Xa1, Xb1, Xa3 and Xb3 is necessarily a 1-alkyl-1-benzylmethylene group which may have a substituent, a 1,1-dibenzylmethylene group which may have a substituent or a cycloalkane-1,1-diyl group having 3 to 6 carbon atoms which may have a substituent.
    Type: Application
    Filed: May 16, 2006
    Publication date: April 16, 2009
    Applicant: Mitsui Chemicals, Inc.
    Inventors: Taizo Nishimoto, Eiichi Takahashi, Shunsuke Murayama, Yoshiaki Aso, Akira Ogiso, Akihiro Kohsaka, Takafumi Yoshida, Hiroyuki Sasaki, Kenichi Kato, Hiroshi Terao, Yojiro Kumagae
  • Publication number: 20090093469
    Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
    Type: Application
    Filed: December 15, 2008
    Publication date: April 9, 2009
    Applicant: WYETH
    Inventors: Callain Younghee Kim, Paige Erin Mahaney, Eugene John Trybulski, Puwen Zhang, Eugene Anthony Terefenko, Casey Cameron McComas, Michael Anthony Marella, Richard Dale Coghlan, Gavin David Heffernan, Stephen Todd Cohn, An Thien Vu, Joseph Peter Sabatucci, Fei Ye
  • Publication number: 20090076278
    Abstract: The present invention provides novel organic compounds, which absorb the light in the ultra violet and the infrared regions, have improved light tolerance and solubility in solvents, and have thermal tolerance suitable for uses to which the organic compounds are applied, and provides uses of the same. The above objects are solved by providing indolenine compounds and methine dyes, which have a bis-indolenine skeleton composed of two indolenine rings linked together at their respective C-3 positions via a divalent linking group, and by providing optical recording media containing the methine dyes.
    Type: Application
    Filed: November 7, 2006
    Publication date: March 19, 2009
    Applicant: KABUSHIKI KAISHA HAYASHIBARA SEIBUTSU KAGAKU KENKYUJO
    Inventors: Yasufumi Dan-Oh, Masahiko Toki, Kentaro Yano, Yasushi Aizawa
  • Patent number: 7498338
    Abstract: The invention provides compounds of formula (I) wherein m, R1, n, R2, q, X, Y, Z, t, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: November 15, 2004
    Date of Patent: March 3, 2009
    Assignee: AstraZeneca AB
    Inventors: Andrew Baxter, Nafizal Hossain, Svetlana Ivanova, Marguerite Mensonides-Harsema, Austen Pimm, James Reuberson
  • Publication number: 20080319204
    Abstract: Processes for preparing substituted oxindole-2-ones, and specifically the following, are described, wherein R1-R4, R6, and n are defined herein. The processes include reacting a first alkali metal hydroxide, a tetraalkyl ammonium salt, a benzonitrile, and R6X or XCH2(CH2)nX?, wherein R6 is C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, or substituted heterocyclic, X and X? are, independently, leaving groups, and n is 1 to 5; (ii) reacting the product of step (i) with a second alkali metal hydroxide at a temperature of at least about 60° C.; (iii) reacting the product of step (ii) with an alkali alkoxide at a temperature of at least about 140° C. to form an oxindol-2-one; (iv) brominating the oxindol-2-one; and (v) coupling the brominated oxindol-2-one with a coupling reagent.
    Type: Application
    Filed: May 15, 2008
    Publication date: December 25, 2008
    Applicant: Wyeth
    Inventors: Yanzhong Wu, Karen Sutherland, John Leo Considine, Bogdan Kazimierz Wilk, Pierre Giguere, Michael MacEwan, Archana Sharma, Alexander Gontcharov
  • Publication number: 20080312306
    Abstract: Novel polymorph Form II and III, solvate Forms I, II, III, and IV, and the hydrate of 5-(4?-fluoro-2?-oxo-1?,2?-dihydrospiro[cyclopropane-1,3?-indol]-5?-yl)-1-methyl-1H-pyrrole-2-carbonitrile are provided, as are methods for preparing the same. Pharmaceutical compositions and kits containing these novel polymorphs, solvates, and hydrate, and combinations thereof are further provided, as are methods of contraception; treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, hormone-dependent carcinomas; treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; or treating symptoms of premenstrual syndrome using one or more of these polymorphs, solvates, or hydrate.
    Type: Application
    Filed: June 13, 2008
    Publication date: December 18, 2008
    Applicant: Wyeth
    Inventors: Mahmoud Mirmehrabi, John Leo Considine, Yuping Niu, Abdolsamad Tadayon, Subodh Deshmukh, Jennifer Q. Liang, Yanzhong Wu
  • Publication number: 20080293685
    Abstract: This invention relates to diamondoid derivatives which exhibit therapeutic activity. Specifically, the diamondoid derivatives herein exhibit therapeutic effects in the treatment of viral disorders. Also provided are methods of treatment, prevention and inhibition of viral disorders in a subject in need.
    Type: Application
    Filed: May 22, 2008
    Publication date: November 27, 2008
    Applicant: Chevron U.S.A. Inc.
    Inventors: Deyuan Kong, Frederick W. Lam, Steven F. Sciamanna, Earl Shelton, Shenggao Liu, Robert M. Carlson
  • Patent number: 7390798
    Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.
    Type: Grant
    Filed: February 9, 2005
    Date of Patent: June 24, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
  • Publication number: 20080114013
    Abstract: There are provided compounds of the general formulas wherein X, Y, R1, R2, R3 and R4 are as described herein. The compounds exhibit anticancer activity.
    Type: Application
    Filed: October 4, 2007
    Publication date: May 15, 2008
    Inventors: Jin-Jun Liu, Zhuming Zhang
  • Patent number: 7317037
    Abstract: Pyrrole-oxindole derivatives useful as progesterone receptor antagonists, and methods for preparing the same, are provided. Pharmaceutical compositions containing these derivatives are described, as is the use thereof in contraception and hormone-related conditions.
    Type: Grant
    Filed: July 6, 2005
    Date of Patent: January 8, 2008
    Assignee: Wyeth
    Inventors: Andrew Fensome, Casey Cameron McComas, Edward George Melenski, Michael Anthony Marella, Jay Edward Wrobel, Gary Sondermann Grubb
  • Patent number: 7314932
    Abstract: Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrite groups, are provided.
    Type: Grant
    Filed: April 7, 2005
    Date of Patent: January 1, 2008
    Assignee: Wyeth
    Inventor: Bogdan Kazimierz Wilk
  • Patent number: 7309787
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: July 6, 2006
    Date of Patent: December 18, 2007
    Assignee: Allergan, Inc.
    Inventor: Julie A. Wurster
  • Patent number: 7205328
    Abstract: The present invention relates to inhibition of viruses, e.g., HIV using oxindoles and compounds related to oxindoles. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.
    Type: Grant
    Filed: October 21, 2003
    Date of Patent: April 17, 2007
    Assignee: IRM LLC
    Inventors: Yun He, Tao Jiang, Kelli L. Kuhen, David Archer Ellis, Baogen Wu, Tom Yao-Hsiang Wu, Badry Bursulaya