One Of The Two Rings Which Form The Spiro Is Part Of A Polycyclo Ring System Patents (Class 548/301.1)
  • Patent number: 10231967
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods 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: Grant
    Filed: January 31, 2018
    Date of Patent: March 19, 2019
    Assignee: AstraZeneca AB
    Inventors: Gabor Csjernyik, Sofia Karlstrom, Annika Kers, Karin Kolmodin, Martin Nylof, Liselotte Ohberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Soderman, Britt-Marie Swahn, Stefan Von Berg
  • Patent number: 9526727
    Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: December 27, 2016
    Assignee: Vitae Pharmaceutical, Inc.
    Inventors: Yuri Bukhtiyarov, Salvacion Cacatian, Lawrence Wayne Dillard, Cornelia Dorner-Ciossek, Klaus Fuchs, Lanqi Jia, Deepak S. Lala, Angel Morales-Ramos, Jonathan Reeves, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Jing Yuan, Yi Zhao, Yajun Zheng, Georg Rast
  • Patent number: 9290477
    Abstract: The present invention relates to spirocyclic indane imidazole 4-amines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Grant
    Filed: September 25, 2013
    Date of Patent: March 22, 2016
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Shankar Venkatraman, Jing Yuan, Yajun Zheng
  • Patent number: 9248129
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods 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: Grant
    Filed: September 15, 2014
    Date of Patent: February 2, 2016
    Assignee: ASTRAZENECA AB
    Inventors: Gabor Csjernyik, Sofia Karlstrom, Annika Kers, Karin Kolmodin, Martin Nylof, Liselotte Ohberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Soderman, Britt-Marie Swahn, Stefan Von Berg
  • Patent number: 9018391
    Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: April 28, 2015
    Assignees: Boehringer Ingelheim International GmbH, Vitae Pharmaceuticals, Inc.
    Inventors: Yuri Bukhtiyarov, Salvacion Cacatian, Lawrence Wayne Dillard, Klaus Fuchs, Lanqi Jia, Deepak S. Lala, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Jing Yuan, Yi Zhao, Yajun Zheng, Cornelia Dorner-Ciossek, Ulrike Gross, Niklas Heine, Achim Sauer
  • Publication number: 20150111882
    Abstract: The present invention provide compounds of Formula (I) used as BACE inhibitors for the treatment of neurodegenerative diseases.
    Type: Application
    Filed: May 10, 2013
    Publication date: April 23, 2015
    Applicant: Ares Trading S.A.
    Inventors: Anna Quattropani, Dominique Swinnen
  • Publication number: 20150105354
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLC
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Patent number: 9000184
    Abstract: Cyclohexane-1,2?-naphthalene-1?,2?-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, 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, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: April 7, 2015
    Assignee: AstraZeneca AB
    Inventors: Sofia Karlstrom, Lars Sandberg, Peter Soderman, Karin Kolmodin, Liselotte Ohberg
  • Patent number: 9000183
    Abstract: Cyclohexane-1,2?-indene-1?,2?-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, 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, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: April 7, 2015
    Assignee: Astrazeneca AB
    Inventors: Sofia Karlstrom, Peter Soderman, Laszlo Rakos, Liselotte Ohberg, Karin Kolmodin, Lars Sandberg
  • Patent number: 9000185
    Abstract: Cycloalkyl ether compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, 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 and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: April 7, 2015
    Assignee: AstraZeneca AB
    Inventors: Sofia Karlstrom, Peter Soderman, Britt-Marie Swahn, Laszlo Rakos, Liselotte Ohberg
  • Patent number: 9000182
    Abstract: 2H-imidazol-4-amine compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, 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. methods of therapy, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: April 7, 2015
    Assignee: AstraZeneca AB
    Inventors: Sofia Karlstrom, Gabor Csjernyik, Britt-Marie Swahn, Lars Sandberg, Karin Kolmodin, Peter Soderman, Liselotte Ohberg
  • Patent number: 8981112
    Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: March 17, 2015
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer-Ingelheim International GmbH
    Inventors: Yuri Bukhtiyarov, Salvacion Cacatian, Lawrence Wayne Dillard, Cornelia Dorner-Ciossek, Klaus Fuchs, Lanqi Jia, Deepak S. Lala, Angel Morales-Ramos, Jonathan Reeves, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Jing Yuan, Yi Zhao, Yajun Zheng, Georg Rast
  • Patent number: 8962859
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A1, A3, A5, A6, A8, R2, R7, X, Y and Z of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.
    Type: Grant
    Filed: February 13, 2012
    Date of Patent: February 24, 2015
    Assignee: Amgen Inc.
    Inventors: Oleg Epstein, Ryan White, Vinod F. Patel, Jason Brooks Human
  • Patent number: 8957083
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A1, A3, A4, A5, A6, A8, L, R2, R7, R9, W and Y of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, sub-Formula embodiments of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulae I-III.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: February 17, 2015
    Assignee: Amgen Inc.
    Inventors: Ana Elena Minatti, Oleg Epstein, Ryan White, Matthew Weiss, Wenge Zhong, Jonathan D. Low
  • Publication number: 20140312311
    Abstract: An optoelectronic materials for OLED is represented by formula (I): wherein R1 is selected from a group consisting of formulas (II)-(VI): wherein R2 and R3 are identical and selected from a group consisting of formula (VII) and formula (VIII): The optoelectronic materials possesses superior luminescent performance and thermal stability and is suitable to be a new type of ambipolar materials for OLED elements.
    Type: Application
    Filed: July 11, 2013
    Publication date: October 23, 2014
    Inventors: Chien-Tien CHEN, Wei-Shan CHAO, Hao-Wei LIU, Wei-Sheng SU
  • Patent number: 8865911
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods 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: Grant
    Filed: March 15, 2013
    Date of Patent: October 21, 2014
    Assignee: Astrazeneca AB
    Inventors: Gabor Csjernyik, Sofia Karlstrom, Annika Kers, Karin Kolmodin, Martin Nylof, Liselotte Ohberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Soderman, Britt-Marie Swahn, Stefan Von Berg
  • Publication number: 20140308282
    Abstract: Benzimidazoles of formula (I): wherein: A is 5- to 12-membered aryl or 5- to 12-membered heteroaryl, each of which is unsubstituted or substituted; Y is a single bond, —(CH2)p—, —X—, —CH2—X—, or —X—CH2—; X is —O—, —S—, —N(R2)—, >C?O, >S(?O), >S(?O)2, —O—C(?O)—, —C(?O)—O—, N(R2)—C(?O)—, or —C(?O)—N(R2)—; each L is independently a single bond, C1-3alkylene, C2-3alkenylene or C2-3alkynylene; R1 is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, each of which is unsubstituted or substituted; each Z is independently —N(R2)2, —OR2, —SR2, —S(?O)R2, —S(?O)2R2; each R2 is independently hydrogen, C1-6alkyl, C2-6alkenyl or C2-6 alkynyl, wherein said alkyl, alkenyl and alkynyl groups are unsubstituted or substituted; m is 0, 1, 2, or 3; n is 1, 2, or 3; and p is 1, 2, or 3; and the pharmaceutically acceptable salt thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
    Type: Application
    Filed: November 12, 2012
    Publication date: October 16, 2014
    Applicant: re: Viral Ltd
    Inventors: Stuart Cockerill, Christopher Pilkington, James Lumley, Richard Angell, Neil Mathews
  • Publication number: 20140225040
    Abstract: The present invention relates to compounds for use in electronic devices, preferably organic electroluminescent devices. The invention furthermore relates to processes for the preparation of these compounds and to electronic devices comprising these compounds, preferably in a function as matrix materials and/or as electron-transport materials.
    Type: Application
    Filed: July 3, 2012
    Publication date: August 14, 2014
    Applicant: Merck Patent GmbH Patents & Scientific Information
    Inventors: Amir Hossain Parham, Christof Pflumm, Anja Jatsch
  • Publication number: 20140200223
    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: Application
    Filed: December 18, 2013
    Publication date: July 17, 2014
    Inventors: Salvacion Cacatian, David A. Claremon, Lawrence Wayne 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
  • 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
  • Patent number: 8748629
    Abstract: The present invention is a photochromic material formed of a biimidazole compound represented by general formula (1-1): (where, R4 and R5 respectively and independently represent a halogen atom or alkyl group, R1 to R3 and R6 to R8 respectively and independently represent a hydrogen atom, halogen atom, alkyl group, fluoroalkyl group, hydroxyl group, alkoxyl group, amino group, alkylamino group, carbonyl group, alkylcarbonyl group, nitro group, cyano group or aryl group, Ar1 to Ar4 respectively and independently represent a substituted or unsubstituted aryl group, R4 may form a condensed, substituted or unsubstituted aryl ring with R3, and R5 may form a condensed, substituted or unsubstituted aryl ring with R6).
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: June 10, 2014
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Takeru Horino, Atsuhiro Tokita, Toyoji Oshima
  • Publication number: 20140147412
    Abstract: Disclosed are spiro compounds of formula (I), or stereomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof. The compounds can be used to treat hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore disclosed are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions in the treatment of HCV infection or hepatitis C disease.
    Type: Application
    Filed: July 9, 2012
    Publication date: May 29, 2014
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Jiancun Zhang, Yingjun Zhang, Hongming Xie, Qingyun Ren, Huichao Luo, Tianzhu Yu, Yumei Tan
  • Publication number: 20140094613
    Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.
    Type: Application
    Filed: December 5, 2013
    Publication date: April 3, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Noriaki MURASE, Toshihito KUMAGAI, Hisaya WADA, Hisahide TANIMOTO, Koumei OHTA, Yoshihiro KIMURA
  • Publication number: 20140057927
    Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Application
    Filed: August 27, 2013
    Publication date: February 27, 2014
    Inventors: Yuri Bukhtiyarov, Salvacion Cacatian, Lawrence Wayne Dillard, Klaus Fuchs, Lanqi Jia, Deepak S. Lala, Angel Morales-Ramos, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Jing Yuan, Yi Zhao, Yajun Zheng, Cornelia Dorner-Ciossek, Ulrike Gross, Niklas Heine, Achim Sauer
  • Publication number: 20140057910
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.
    Type: Application
    Filed: February 22, 2012
    Publication date: February 27, 2014
    Applicant: Schering Corporation
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
  • Publication number: 20140034924
    Abstract: Provided is a compound having an indolo[3,2,1-jk]carbazole skeleton and a heterocyclic skeleton which are bonded to each other through an arylene group. The heterocyclic skeleton contains an imidazole skeleton, a pyrazine skeleton, a pyrimidine skeleton, a triazole skeleton, or a condensed heteroaromatic ring including any of these heterocycles. The high carrier-transport property and the large band gap of the compound allows the used as a host material of a phosphorescent dopant, leading to the formation of a green to blue emissive phosphorescent light-emitting element having high emission efficiency, low driving voltage, and reduced power consumption.
    Type: Application
    Filed: July 30, 2013
    Publication date: February 6, 2014
    Applicant: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Yuko Kawata, Hiroshi Kadoma, Satoko Shitagaki, Satoshi Seo
  • Patent number: 8642777
    Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.
    Type: Grant
    Filed: November 18, 2010
    Date of Patent: February 4, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Noriaki Murase, Toshihito Kumagai, Hisaya Wada, Hisahide Tanimoto, Koumei Ohta, Yoshihiro Kimura
  • Publication number: 20140031341
    Abstract: An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology.
    Type: Application
    Filed: December 19, 2011
    Publication date: January 30, 2014
    Applicants: UNIVERSITAT MUNSTER, GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Jerome Aubert, Martin Steinhoff
  • 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: 20130345246
    Abstract: 2H-imidazol-4-amine compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, 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. methods of therapy, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: June 13, 2013
    Publication date: December 26, 2013
    Applicant: ASTRAZENECA AB
    Inventors: Sofia Karlstrom, Gabor Csjernyik, Britt-Marie Swahn, Lars Sandberg, Karin Kolmodin, Peter Soderman, Liselotte Ohberg
  • Publication number: 20130345247
    Abstract: Cyclohexane-1,2?-indene-1?,2?-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, 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, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: June 13, 2013
    Publication date: December 26, 2013
    Applicant: ASTRAZENECA AB
    Inventors: Sofia Karlstrom, Peter Soderman, Laszlo Rakos, Liselotte Ohberg, Karin Kolmodin, Lars Sandberg
  • Publication number: 20130345272
    Abstract: Cycloalkyl ether compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, 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 and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: June 13, 2013
    Publication date: December 26, 2013
    Applicant: AstraZeneca AB
    Inventors: Sofia Karlstrom, Peter Soderman, Britt-Marie Swahn, Laszlo Rakos, Liselotte Ohberg
  • Publication number: 20130345248
    Abstract: Cyclohexane-1,2?-naphthalene-1?,2?-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy, 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, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: June 13, 2013
    Publication date: December 26, 2013
    Applicant: AstraZeneca AB
    Inventors: Sofia Karlstrom, Lars Sandberg, Peter Soderman, Karin Kolmodin, Liselotte Ohberg
  • Publication number: 20130338177
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I), wherein variables A1, A3, A4, A5, A6, A8, L, R2, R7, R9, W and Y of Formula (I) are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas (II) and (III), sub-Formula embodiments of Formulas (I), (II) and (III), intermediates and processes and methods useful for the preparation of compounds of Formulae (I-III).
    Type: Application
    Filed: November 18, 2011
    Publication date: December 19, 2013
    Applicant: AMGEN INC.
    Inventors: Ana Elena Minatti, Oleg Epstein, Ryan White, Matthew Weiss, Wenge Zhong, Jonathan D. Low
  • Publication number: 20130289050
    Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Application
    Filed: March 4, 2013
    Publication date: October 31, 2013
    Applicants: VITAE PHARMACEUTICALS, INC., BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Boehringer Ingelheim International GmbH, Vitae Pharmaceuticals, Inc.
  • Publication number: 20130287789
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Application
    Filed: June 26, 2013
    Publication date: October 31, 2013
    Applicant: Novartis AG
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • Patent number: 8569312
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: April 4, 2013
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
  • Publication number: 20130274212
    Abstract: The present invention relates to sesterterpene compounds, to the precursors thereof that are hydrolysable in a living body, or to the pharmaceutically acceptable salts thereof, and also relates to the prevention and treatment efficacy of the sesterterpene compounds with respect to non-insulin dependent diabetes mellitus, diabetic complications (renal failure and foot ulcers caused by diabetes), alcoholic, non-alcoholic, and viral fatty liver diseases, obesity, hyperlipidemia, atherosclerosis, cardiovascular diseases such as atherosclerotic stroke, and cerebropathies (Parkinsonism, schizophrenia and Alzheimer's disease). In addition, the present invention relates to compositions for functional foods, functional beverages, functional cosmetics, and functional feed.
    Type: Application
    Filed: September 7, 2011
    Publication date: October 17, 2013
    Applicant: SNU R&DB FOUNDATION
    Inventors: Heon Joong Kang, Dong Hwan Won, In Ho Yang, Eun Oh Kim, Jung Ah Kim, Awadut Gajendra Giri, Venkat Reddy Mallepally
  • Patent number: 8552023
    Abstract: The present invention is directed to novel non-amidic linkers with branched termini derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: October 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael R. Wood, June J. Kim, Harold G. Selnick, Shawn J. Stachel
  • Publication number: 20130210837
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods 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: March 15, 2013
    Publication date: August 15, 2013
    Applicant: ASTRAZENECA INTELLECTUAL PROPERTY
    Inventors: Gabor Csjernyik, Sofia Karlstrom, Annika Kers, Karin Kolmodin, Martin Nylof, Liselotte Ohberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Soderman, Britt-Marie Swahn, Stefan Von Berg
  • Patent number: 8450308
    Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: May 28, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
  • Publication number: 20130123215
    Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: November 9, 2012
    Publication date: May 16, 2013
    Applicant: ALLERGAN, INC.
    Inventor: Allergan, Inc.
  • Publication number: 20130102775
    Abstract: The present invention is a photochromic material formed of a biimidazole compound represented by general formula (1-1): (where, R4 and R5 respectively and independently represent a halogen atom or alkyl group, R1 to R3 and R6 to R8 respectively and independently represent a hydrogen atom, halogen atom, alkyl group, fluoroalkyl group, hydroxyl group, alkoxyl group, amino group, alkylamino group, carbonyl group, alkylcarbonyl group, nitro group, cyano group or aryl group, Ar1 to Ar4 respectively and independently represent a substituted or unsubstituted aryl group, R4 may form a condensed, substituted or unsubstituted aryl ring with R3, and R5 may form a condensed, substituted or unsubstituted aryl ring with R6).
    Type: Application
    Filed: July 8, 2011
    Publication date: April 25, 2013
    Applicant: MITSUBISHI GAS CHEMICAL COMPANY, INC.
    Inventors: Takeru Horino, Atsuhiro Tokita, Toyoji Oshima
  • Patent number: 8415483
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods 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: Grant
    Filed: December 20, 2011
    Date of Patent: April 9, 2013
    Assignee: AstraZeneca AB
    Inventors: Gabor Csjernyik, Sofia Karlström, Annika Kers, Karin Kolmodin, Martin Nylöf, Liselotte Öhberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Söderman, Britt-Marie Swahn, Stefan Von Berg
  • Publication number: 20130037752
    Abstract: OLED compounds of the general structure: B—S-A-S—B in which rod-like nuclei A includes a condensed aromatic ring structure in turn having fluorene ring structures condensed with at least one additional fluorene ring structures wherein the fluorene ring systems provided by the condensed aromatic structure are substituted at the 9-position, and in which the 9-positions of the fluorenes are not susceptible to oxidation.
    Type: Application
    Filed: September 29, 2010
    Publication date: February 14, 2013
    Applicant: LOMOX LIMITED
    Inventor: Gene Carl Koch
  • Patent number: 8324235
    Abstract: The patent application relates to new heterocyclic compounds of the general formula (I), in which R, R1, R2, Q, T, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: December 4, 2012
    Assignee: Novartis AG
    Inventors: Peter Herold, Robert Mah, Stefan Stutz, Vincenzo Tschinke, Aleksandar Stojanovic, Nathalie Jotterand, Bibia Bennacer
  • Patent number: 8314097
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Grant
    Filed: August 23, 2006
    Date of Patent: November 20, 2012
    Assignee: Novartis AG
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • Publication number: 20120277215
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Application
    Filed: July 2, 2012
    Publication date: November 1, 2012
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • Publication number: 20120270071
    Abstract: A chromene compound having a skeleton represented by the following formula (1) and exhibiting double peak characteristic: wherein Z is a group represented by any one of the following formulas: n is an integer of 1 to 3, when n is 2 or 3, Z? s may be the same or different, with the proviso that when n is 1, Z cannot be —CH2—, and when n is 2 or 3, Z's cannot be —CH2— at the same time; R1 is an electron absorbing group having a Hammett constant ?p of more than 0, with the proviso that when there are a plurality of R1's, R1's may be the same or different; and X and Y are each independently an oxygen atom or ?NR2, with the proviso that X and Y cannot be oxygen atoms at the same time.
    Type: Application
    Filed: July 21, 2010
    Publication date: October 25, 2012
    Inventors: Toshiaki Takahashi, Junji Takenaka
  • Publication number: 20120238763
    Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.
    Type: Application
    Filed: November 18, 2010
    Publication date: September 20, 2012
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Noriaki Murase, Toshihito Kumagai, Hisaya Wada, Hisahide Tanimoto, Koumei Ohta, Yoshihiro Kimura