Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers.
Type:
Grant
Filed:
July 12, 2007
Date of Patent:
April 14, 2015
Assignee:
Acumen Pharmaceuticals, Inc.
Inventors:
Grant A. Krafft, Todd Pray, William F. Goure
Abstract: PROBLEM Provided is a novel cyanine dye derivative with a pyrazole skeleton and an indole skeleton, having high sensitivity performance in a shorter wavelength region as compared with a conventional optical system, and showing high water solubility.
Abstract: A method of treating insulin resistance, obesity and metabolic syndrome by administering an indazolemethoxyalkanoic acid as described herein.
Type:
Grant
Filed:
May 8, 2012
Date of Patent:
September 30, 2014
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: The present invention is concerned with novel substituted indazole and aza-indazole derivatives of Formula (I) wherein R1, R2, R3, R4, Y, A1, A2, A3, A4, X1, X2, X3 and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Abstract: The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor.
Type:
Grant
Filed:
August 27, 2010
Date of Patent:
July 15, 2014
Assignee:
Arena Pharmaceuticals, Inc.
Inventors:
Robert M. Jones, Sangdon Han, Lars Thoresen, Jae-Kyu Jung, Sonja Strah-Pleynet, Xiuwen Zhu, Yifeng Xiong, Dawei Yue
Abstract: Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
Abstract: Provided herein are hydrobromide salts of a pyrazolylaminoquinazoline, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating a proliferative disease.
Type:
Grant
Filed:
August 31, 2011
Date of Patent:
January 21, 2014
Assignee:
Ambit Biosciences Corporation
Inventors:
Timothy David Gross, Patrick B. O'Donnell
Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.
Abstract: The present invention relates to a method for regioselectively reducing the maleimide compounds of formula (I). The invention also relates to C7 hydroxy lactam regioisomers of formula (II) obtainable by this method and their use for the preparation of lactams of formula (III) which are particularly useful as intermediate for the synthesis of fused pyrrolocarbazoles.
Abstract: A heterocyclic compound represented by one of Formulae 1-4 below and an organic light-emitting device including an organic layer that includes the heterocyclic compound. The heterocyclic compounds have excellent light-emitting characteristics and excellent electron transporting characteristics, and thus may be used as electron injecting materials or electron transporting materials suitable for all-color fluorescent and phosphorescent devices, such as red, green, blue, and white fluorescent and phosphorescent devices. In particular, the heterocyclic compounds are efficiently used as light-emitting materials of green, blue, and while fluorescent devices. By using the heterocyclic compounds, organic light-emitting devices having high efficiency, low driving voltage, high brightness, and long lifespan may be prepared.
Abstract: Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.
Type:
Grant
Filed:
July 22, 2011
Date of Patent:
December 4, 2012
Assignee:
Sequoia Sciences, Inc.
Inventors:
Gary R. Eldridge, Ronald Neil Buckle, Michael Ellis, Zhongping Huang, John Edward Reilly
Abstract: The present invention relates to novel aryloazol-2-yl-cyanoethylamino derivatives of formula (I): wherein R3, R4, R5, R6, R7, P, Q, V, W, X, Y, Z and a are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.
Type:
Grant
Filed:
December 14, 2011
Date of Patent:
October 9, 2012
Assignees:
Merial Limited, Aventis Agriculture
Inventors:
Mark David Soll, Loïc Patrick Le Hir de Fallois, Scot Kevin Huber, Hyoung Ik Lee, Douglas Edward Wilkinson, Robert Toms Jacobs
Abstract: Compounds corresponding to the formula (I) as defined in the disclosure, as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.
Type:
Grant
Filed:
January 11, 2012
Date of Patent:
September 4, 2012
Assignee:
Sanofi
Inventors:
Laurent Dubois, Yannick Evanno, Christian Maloizel, Mireille Sevrin
Abstract: Use of a compound of formula (I) in which R, R? and R? have the meanings given in the description, optionally in the form of a salt thereof with a pharmaceutically acceptable organic or mineral base, to prepare a pharmaceutical composition for reducing the blood triglyceride, cholesterol and glucose levels.
Type:
Grant
Filed:
November 13, 2007
Date of Patent:
June 12, 2012
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F.S.p.A.
Abstract: The present invention discloses an inverted organic photovoltaic cell comprising a polymerizable fullerene interlayer adapted to enhance the device performance and lifetime. The polymerizable fullerene derivative comprises a fullerene core, a bridging functional group and a polymerizable functional group. The fullerene core can be either C60 or C70, and the bridging functional group comprises a cyclic hydrocarbon or a heterocyclic ring. The polymerizable functional group comprises a thermally polymerizable functional group or a photochemically polymerizable functional group.
Type:
Application
Filed:
March 11, 2011
Publication date:
March 15, 2012
Applicant:
NATIONAL CHIAO TUNG UNIVERSITY
Inventors:
CHAIN-SHU HSU, YEN-JU CHENG, CHAO-HSIANG HSIEH, PEI-JUNG LI
Abstract: The novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1 and R2 are as defined in the description, and the active compound groups (2) and (3) listed in the description have very good fungicidal properties.
Type:
Grant
Filed:
March 27, 2006
Date of Patent:
March 13, 2012
Assignee:
Bayer Cropscience AG
Inventors:
Anne Suty-Heinze, Burkhard Schütz, Gerhard-Johann Feurer, Hans-Ludwig Elbe
Abstract: The present invention relates to a method for regioselectively reducing the maleimide compounds of formula (I). The invention also relates to C7 hydroxy lactam regioisomers of formula (II) obtainable by this method and their use for the preparation of lactams of formula (III) which are particularly useful as intermediate for the synthesis of fused pyrrolocarbazoles.
Abstract: The invention provides non-steroidal ligands for the glucocorticoid receptor, methods for making non-steroidal ligands of the glucocorticoid receptor, compositions of non-steroidal ligands of the glucocorticoid receptor and methods of using non-steroidal ligands and compositions of non-steroidal ligands of the glucocorticoid receptor for treating or preventing diseases (e.g., obesity, diabetes, depression, neurodegeneration or an inflammatory disease) associated with glucocorticoid binding to the glucocorticoid receptor.
Type:
Grant
Filed:
February 3, 2009
Date of Patent:
May 24, 2011
Assignee:
The Regents of the University of California
Abstract: The invention relates to fungicide and insecticide, especifically to the substituted azole compounds and its preparation method and use thereof. The azole compounds of the invention having general formula (I): The compounds of present invention, having broad spectrum fungicidal activity, applied for controlling various disease in plants. For example they have good activity against the diseases such as cucumber downy mildew, cucumber grey mold, cucumber powdery mildew, tomato early blight, tomato late blight, phytophthora blight of pepper, grape downy mildew, grape white rot, apple ring rot, apple alternaria leaf spot, rice sheath blight, rice blast, wheat leaf rust, wheat leaf blotch, wheat powdery mildew, rapesclerotiniose, corn southern leaf blight. Some compounds have good insecticidal or acaricidal activity and can be used to control insects and acacids of various crops. For example they are used to control army worm, diamond backmoth and aphid, and culex mosquito.
Type:
Grant
Filed:
February 17, 2005
Date of Patent:
September 14, 2010
Assignee:
Shenyang Research Institute of Chemical Industry
Inventors:
Changling Liu, Miao Li, Hong Zhang, Lin Li, Mingxing Zhang, Aiying Guan, Chunqing Hou, Zhinian Li, Yonggang Jia
Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments.
Inventors:
Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrecher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.
Type:
Grant
Filed:
June 29, 2006
Date of Patent:
March 2, 2010
Assignee:
Cephalon, Inc.
Inventors:
Robert L. Hudkins, Allison L. Zulli, Dandu R. Reddy, Diane E. Gingrich, Ming Tao, Nadine C. Becknell, James L. Diebold, Theodore L. Underiner
Abstract: The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Application
Filed:
October 3, 2008
Publication date:
November 19, 2009
Applicant:
AstraZeneca AB
Inventors:
Hakan BLADH, Frank Burkamp, Balint Gabos, Peter Hansen, Svetlana Ivanova, Karolina Lawitz
Abstract: The present invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles of formula (I): wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and their use for the treatment of pathological conditions, in particular as anticancer agents.
Abstract: The present invention relates to tricyclic pyrazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Type:
Grant
Filed:
February 6, 2006
Date of Patent:
September 29, 2009
Assignee:
Merck & Co. Inc.
Inventors:
Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Lou Anne Neilson, David B. Whitman
Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
Abstract: Compounds corresponding to the formula (I) as defined in the disclosure as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions containing the compounds of the invention, and methods of treatment using them.
Type:
Grant
Filed:
October 13, 2006
Date of Patent:
March 10, 2009
Assignee:
Sanofi-Aventis
Inventors:
Laurent DuBois, Yannick Evanno, Christian Maloizel, Mireille Sevrin
Abstract: The invention provides non-steroidal ligands for the glucocorticoid receptor, methods for making non-steroidal ligands of the glucocorticoid receptor, compositions of non-steroidal ligands of the glucocorticoid receptor and methods of using non-steroidal ligands and compositions of non-steroidal ligands of the glucocorticoid receptor for treating or preventing diseases (e.g., obesity, diabetes, depression, neurodegeneration or an inflammatory disease) associated with glucocorticoid binding to the glucocorticoid receptor.
Type:
Grant
Filed:
October 22, 2004
Date of Patent:
February 3, 2009
Assignee:
The Regents of the University of California
Abstract: The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents a
Abstract: Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Type:
Grant
Filed:
March 24, 2005
Date of Patent:
December 23, 2008
Assignee:
Abbott Laboratories Inc.
Inventors:
Lee D. Arnold, Jürgen Dinges, Richard W. Dixon, Stevan W. Djuric, Anna M. Ericsson, Kimba Fischer, Alan F. Gasiecki, Vijaya J. Gracias, James H. Holms, Makoto Takeshita, Michael R. Michaelides, Melanie A. Muckey, Paul Rafferty, Douglas H. Steinman, Carol K. Wada, Zhiren Xia, Irini Akritopoulou-Zanze, Henry Q. Zhang
Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.
Type:
Grant
Filed:
October 6, 2005
Date of Patent:
November 11, 2008
Assignee:
Schering Corporation
Inventors:
Kamil Paruch, Timothy J. Guzi, Michael P. Dwyer, Gerald W. Shipps, Jr.
Abstract: The invention relates to novel processes for the preparation of small molecule antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”) and intermediates thereof.
Type:
Grant
Filed:
December 1, 2005
Date of Patent:
November 11, 2008
Assignee:
Bristol-Myers Squibb Company
Inventors:
Prasad V. Chaturvedula, Xiaojan Han, Xiang-Jun J. Jiang
Abstract: The present invention is directed to novel compounds of Formula I: and forms and pharmaceutical compositions thereof, and the use thereof as inhibitors of Factor Xa.
Type:
Grant
Filed:
October 24, 2005
Date of Patent:
November 4, 2008
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Tianbao Lu, Tho V. Thieu, Yu-Kai Lee, Daniel J. Parks, Thomas P. Markotan, Wenxi Pan, Karen L. Milkiewicz, Mark R. Player
Abstract: Novel dioxinoindazole compounds and dioxoloindazole compounds are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions of one or more of the compounds of the present invention.
Abstract: This invention relates to potent potassium channel blocker compounds of Formula (I) or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans, or a pharmaceutically acceptable salt, in vivo hydrolysable ester, enantiomer, diastereomer or mixture thereof: formula (II) represents C6-10 aryl or C3-10 heterocyclyl, said aryl or heterocyclyl optionally substituted with 1-3 groups selected from Ra; Z represents (CH2)nPO(OR)(OR*).
Type:
Grant
Filed:
August 31, 2004
Date of Patent:
August 12, 2008
Assignee:
Merck & Co. Inc.
Inventors:
Meng Hsin Chen, James B. Doherty, Luping Liu, Swaminathan Natarajan, Robert M. Tynebor
Abstract: The present invention provides a novel fused indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Z11 and Z12 each independently represent a carbonyl group, a methylene group, etc.; represents a double bond or a single bond; R1a represents a hydrogen atom, etc.; the ring A represents a benzene ring, a naphthalene ring or a 5- to 10-membered aromatic heterocyclic ring, etc.; and R2a, R2b and R2c each independently represent (1) a hydrogen atom, (2) a halogen atom, (3) a nitro group, etc.
Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.
Type:
Grant
Filed:
December 22, 2004
Date of Patent:
July 10, 2007
Assignee:
Cephalon, Inc.
Inventors:
Robert L. Hudkins, Allison L. Zulli, Dandu R. Reddy, Ming Tao, Theodore L. Underiner
Abstract: The invention relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.
Type:
Grant
Filed:
June 2, 2003
Date of Patent:
March 27, 2007
Assignee:
Schering Corporation
Inventors:
Gerald W. Shipps, Kristin E. Rosner, Janet Popovici-Muller, Yongqi Deng, Tong Wang, Patrick J. Curran
Abstract: The present invention relates generally to selected fused pyrrolocarbazoles, including pharmaceutical compositions thereof and methods of treating diseases therewith. The present invention is also directed to intermediates and processes for making these fused pyrrolocarbazoles.
Type:
Grant
Filed:
December 22, 2004
Date of Patent:
January 30, 2007
Assignee:
Cephalon, Inc.
Inventors:
Robert L. Hudkins, Allison L. Zulli, Dandu R. Reddy, Diane E. Gingrich, Ming Tao, Nadine C. Becknell, James L. Diebold, Theodore L. Underiner
Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, V1, V2, and V3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT, PKA, PDK1, p70S6K, or ROCK kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.
Type:
Grant
Filed:
January 23, 2003
Date of Patent:
May 9, 2006
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Hayley Binch, Guy Brenchley, Julian M. C. Golec, Ronald Knegtel, Michael Mortimore, Sanjay Patel, Alistair Rutherford