Patents Examined by Kahsay T. Habte
  • Patent number: 8946210
    Abstract: A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: February 3, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yuichi Suzuki, Takafumi Motoki, Toshihiko Kaneko, Mamoru Takaishi, Tasuku Ishida, Yoichi Kita, Kunitoshi Takeda, Noboru Yamamoto, Afzal Khan, Paschalis Dimopoulos
  • Patent number: 8754076
    Abstract: Disclosed is a compound represented by Formula (Im1): or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Also disclosed are pharmaceutical compositions comprising the compound of Formula (Im1) or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof and methods of inhibiting 11?-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (Im1), or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Values for the variables in Formula (Im1) are defined herein.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: June 17, 2014
    Assignees: Vitae Pharmaceuticals, Inc./Boehringer-Ingelheim, Boehringer-Ingelheim International GmbH
    Inventors: David A. Claremon, Frank Himmelsbach, Katerina Leftheris, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Linghang Zhuang
  • Patent number: 8697689
    Abstract: The present invention relates to novel compounds, in particular novel indole and benzomorpholine derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions as well as to the use of such compounds or compositions for the prevention and treatment of such diseases in which mGluR2 is involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: April 15, 2014
    Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma SA
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez
  • Patent number: 8691813
    Abstract: The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds and to the use of such compounds and compositions for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: April 8, 2014
    Assignees: Janssen Pharmaceuticals, Inc., Addex Pharma SA
    Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald
  • Patent number: 8680093
    Abstract: This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, lo1, lo2, lo5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: March 25, 2014
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbH
    Inventors: Martin Renz, Martin Schuehle, Zhenrong Xu
  • Patent number: 8629138
    Abstract: Disclosed is a compound represented by Formula (Im1): or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Also disclosed are pharmaceutical compositions comprising the compound of Formula (Im1) or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof and methods of inhibiting 11?-HSD1 activity comprising the step of administering to a mammal in need of such treatment an effective amount of a compound of Formula (Im1), or a pharmaceutically acceptable salt, monohydrate, enantiomer or diastereomer thereof. Values for the variables in Formula (Im1) are defined herein.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: January 14, 2014
    Assignee: Boehringer-Ingelheim International GmbH
    Inventor: Frank Himmelsbach
  • Patent number: 8592410
    Abstract: This invention relates to novel compounds of the Formula Il Ik, Im3, Im4, Im6-12, In3, In4, In6-12, lo3, lo4, lo6-12, Ip2, Ip4-7, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
    Type: Grant
    Filed: April 30, 2009
    Date of Patent: November 26, 2013
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International GmbH
    Inventors: David A. Claremon, Linghang Zhuang, Katerina Leftheris, Colin M. Tice, Yuanjie Ye, Suresh B. Singh, Frank Himmelsbach
  • Patent number: 8592409
    Abstract: This invention relates to novel compounds of the Formula (I), (Ia), (Ic), (Ie), (If), (Ig), (Ih), (Ii), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: November 26, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice, Salvacion Cacatian
  • Patent number: 8575157
    Abstract: This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, lo1, lo2, lo5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: November 5, 2013
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer Ingelheim International, GmbH
    Inventors: Martin Renz, Martin Schuehle, Zhenrong Xu
  • Patent number: 8546380
    Abstract: A composition having BACE 1 inhibitory activity containing a compound represented by the formula (I): wherein ring A is an optionally substituted heterocyclic group; E is lower alkylene; X is S; R1 is a hydrogen atom or lower alkyl; R2a, R2b, R3a, R3b, R4a and R4b is each independently a hydrogen atom, halogen, or hydroxy etc.; n and m are each independently an integer of 0 to 3; n+m is an integer of 0 to 3; R5 is a hydrogen atom or substituted lower alkyl; or its pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: October 1, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Naotake Kobayashi, Kazuo Ueda, Naohiro Itoh, Shinji Suzuki, Gaku Sakaguchi, Akira Kato, Akira Yukimasa, Akihiro Hori, Yuji Koriyama, Hidekazu Haraguchi, Ken Yasui, Yasuhiko Kanda
  • Patent number: 8541408
    Abstract: This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid ? protein.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: September 24, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yuusuki Tamura, Shinji Suzuki, Yukio Tada, Chiaki Fujikoshi, Sae Matsumoto, Yuuji Kooriyama
  • Patent number: 8524708
    Abstract: The present invention provides methods of use of oxadiazoanthracene derivatives of the formula (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, R, R1, R2, R3, R4 and R5 are as herein described, and wherein said methods of use include uses for the treatment and/or prevention of disorders and diseases, such as diabetes.
    Type: Grant
    Filed: August 31, 2010
    Date of Patent: September 3, 2013
    Assignee: TransTech Pharma, Inc.
    Inventors: Adnan M. M. Mjalli, Dharma Rao Polisetti, Thomas Scott Yokum, Kalpathy Santhosh, Mustafa Guzel, Christopher Behme, Stephen Thomas Davis
  • Patent number: 8518975
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: August 27, 2013
    Assignee: Merck Sharp + Dohme Corp.
    Inventors: Robert G. Aslanian, Xianhai Huang, Anandan Palani, Jun Qin, Wei Zhou, Xiaohong Zhu, Robert D. Mazzola, Jr., Pawan Dhondi, William J. Greenlee
  • Patent number: 8513265
    Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.
    Type: Grant
    Filed: October 10, 2012
    Date of Patent: August 20, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: John M. Fevig, Dean A. Wacker
  • Patent number: 8507479
    Abstract: This invention provides a compound of the formula (I): wherein the ring A is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl; R2a and R2b are each independently hydrogen, optionally substituted lower alkyl or optionally substituted acyl; R3a, R3b, R3c and R3d are each independently hydrogen, halogen, hydroxy or optionally substituted lower alkyl etc.; a pharmaceutically acceptable salt or solvate thereof, which is useful for treating diseases induced by production, secretion and/or deposition of amyloid ? protein.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: August 13, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yuusuki Tamura, Shinji Suzuki, Yukio Tada, Chiaki Fujikoshi, Sae Matsumoto, Yuuji Kooriyama
  • Patent number: 8507472
    Abstract: Bicyclic pyridinylpyrazoles of the formula (I) in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling unwanted microorganisms in crop protection and the protection of materials and for reducing mycotoxins in plants and plant parts, and also processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: April 5, 2011
    Date of Patent: August 13, 2013
    Assignee: Bayer CropScience AG
    Inventors: Amos Mattes, Hendrik Helmke, Stefan Hillebrand, Gorka Peris, Alexander Sudau, Lars Rodefeld, Stefan Gauger, Jürgen Benting, Peter Dahmen, Ruth Meissner, Ulrike Wachendorff-Neumann, Hiroyuki Hadano
  • Patent number: 8501733
    Abstract: A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof, has an A? production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? and typified by Alzheimer-type dementia.
    Type: Grant
    Filed: July 24, 2009
    Date of Patent: August 6, 2013
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Takafumi Motoki, Toshihiko Kaneko, Noboru Yamamoto, Afzal Khan
  • Patent number: 8497264
    Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
    Type: Grant
    Filed: March 14, 2011
    Date of Patent: July 30, 2013
    Assignee: Amgen Inc.
    Inventors: Jian J. Chen, Wenge Zhong, Bryant Yang, Ryan White, Matthew Weiss, Timothy Powers, Yuan Cheng
  • Patent number: 8486934
    Abstract: Novel dioxazine- and oxdiazine-substituted arylamides of the formula (I) in which A1, A2, R1, R2, R3, R4 and R5 are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: July 16, 2013
    Assignee: Bayer CropScience AG
    Inventors: Bernd-Wieland Krüger, Achim Hense, Bernd Alig, Rüdiger Fischer, Christian Funke, Ernst Rudolf Gesing, Olga Malsam, Mark Wilhelm Drewes, Christian Arnold, Peter Lümmen, Erich Sanwald
  • Patent number: 8487094
    Abstract: Disclosed are syntheses of 11?-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease (e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: July 16, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Keith R. Fandrick, Joe Ju Gao, Wenjie Li, Zhi-Hui Lu, Yongda Zhang