Abstract: Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Grant
Filed:
September 17, 2010
Date of Patent:
December 3, 2013
Assignee:
Vanderbilt University
Inventors:
P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Charles David Weaver, Alice L. Rodriguez, Andrew S. Felts, Carrie K. Jones, Brittney S. Bates
Abstract: Provided herein are novel iso-ergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT1D and/or the 5-HT1Breceptor, without agonizing the 5-HT2B receptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing or inhibiting activity at receptors such as, for example, the adrenergic alpha2A and/or the alpha2Breceptors using the compounds and compositions disclosed herein.
Abstract: The present invention provides a method for producing a pyrimidinylpyrazole compound (1), wherein aminoguanidine (2) or its salt is reacted with a ?-diketone compound (3) to produce the pyrimidinylpyrazole compound: wherein R1 and R3 are each independently an alkyl group having 1 to 4 carbon atoms, and R2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms. The method is excellent in the environmental compatibility and economic efficiency.
Abstract: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
Type:
Grant
Filed:
August 24, 2011
Date of Patent:
November 19, 2013
Assignee:
Trustees of Dartmouth College
Inventors:
Gordon W. Gribble, Tadashi Honda, Michael B. Sporn, Nanjoo Suh
Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds and/or their pharmaceutically acceptable salts may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition/cognitive disorders.
Type:
Grant
Filed:
June 15, 2010
Date of Patent:
November 19, 2013
Assignee:
Cephalon, Inc.
Inventors:
Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J. S. Knutsen, Ming Tao, Allison L. Zulli
Abstract: A synergistically effective combination of an anti-cancer agent and a therapeutic compound, such as an mTOR-Rictor complex inhibitor, a Serine 473 phosphorylation inhibitor, an AKT2 inhibitor, or a combination thereof, for use in the treatment of cancer, and methods and uses thereof. Also included are methods and uses of a thiosemicarbazone for treating a cancer in a mammal in need thereof characterized by over-expression of RAS, by an EGFR mutation, and/or by over-expression of AKT2.
Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
Type:
Grant
Filed:
April 29, 2008
Date of Patent:
November 12, 2013
Assignee:
Merck Patent GmbH
Inventors:
Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
Abstract: The disclosure relates to (heterocycle-fused piperidine)-(piperazinyl)-1-alkanone derivatives and (heterocycle-fused pyrrolidine)-(piperazinyl)-1-alkanone derivatives of formula (I): wherein A, W, R2 and n are as defined in the disclosure, to the method of preparation thereof and the therapeutic use thereof.
Type:
Grant
Filed:
June 7, 2012
Date of Patent:
November 12, 2013
Assignee:
Sanofi
Inventors:
Marco Baroni, Francoise Bono, Sandrine Delbary-Gossart, Valentina Vercesi
Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Type:
Grant
Filed:
August 23, 2011
Date of Patent:
November 12, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Alessandra Bartolozzi, Todd Bosanac, Zhidong Chen, Stephane De Lombaert, Jonathon Alan Dines, John D. Huber, Weimin Liu, Ho Yin Lo, Pui Leng Loke, Tina Marie Morwick, Peter Allen Nemoto, Alan Olague, Doris Riether, Heather Tye, Lifen Wu, Renee M. Zindell
Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Type:
Grant
Filed:
September 20, 2011
Date of Patent:
November 12, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Alessandra Bartolozzi, Todd Bosanac, Zhidong Chen, Stephane De Lombaert, John D. Huber, Weimin Liu, Ho Yin Lo, Pui Leng Loke, Doris Riether, Heather Tye, Lifen Wu, Renee M. Zindell
Abstract: Novel acid addition salts of 6-{2-[1-(6-methyl-3-pyridazinyl)-4-piperidinyl]ethoxy}-3-ethoxy-1,2-benzisoxazole of following formula are disclosed, particularly a crystalline form of a bis-dihydrogenphosphate salt: Such compounds have particular advantages with regard to treatment of picornaviruses. Related pharmaceutical compositions and methods of treating a picornavirus infection are also disclosed.
Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.
Abstract: The present invention aims to provide a novel SCD inhibitor. The present invention relate to SCD inhibitor comprising A compound represented by the formula (I) wherein R is an optionally substituted cyclic group or an optionally substituted carbamoyl group, provided that R is not an optionally substituted 7-pyrido[2,3-d]pyrimidyl group; ring A is an optionally further substituted pyridazine ring; R1, R2, R3, R4, R11, R12, R13 and R14 are each independently a hydrogen atom or a substituent, or R1 and R11 in combination, R2 and R12 in combination, R3 and R13 in combination, or R4 and R14 in combination optionally form an oxo group, or R2 and R4 in combination optionally form a bond or an alkylene cross-linkage; m and n are each independently an integer of 0 to 2; ring B is an optionally substituted ring, provided that the two atoms constituting ring B, which are adjacent to the spiro carbon atom, are not oxygen atoms at the same time, or a salt thereof, or a prodrug thereof.
Abstract: This invention relates to novel compounds and hydrochloric acid salts thereof. More specifically, this invention relates to novel compounds and hydrochloric acid salts thereof derived from erlotinib. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an epidermal growth factor receptor tyrosine kinase (EGFR) inhibitor, such as erlotinib.
Abstract: The present invention relates to compounds of formula (I) and (IA): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Type:
Grant
Filed:
September 20, 2011
Date of Patent:
November 5, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Alessandra Bartolozzi, Todd Bosanac, Zhidong Chen, Stephane De Lombaert, Jonathon Alan Dines, John D. Huber, Weimin W. Liu, Pui Leng Loke, Tina Marie Morwick, Alan Olague, Doris Riether, Heather Tye, Lifen Wu, Renee M. Zindell
Abstract: Compounds represented by Structural Formula (I): are useful, for example, in the effective killing or reducing the rate of proliferation of cancer cells, such as in patients suffering from cancer. In addition to the compounds themselves, the invention provides pharmaceutical compositions of the compounds and method of treatment using the compounds.
Type:
Grant
Filed:
December 22, 2006
Date of Patent:
November 5, 2013
Assignee:
Prolexys Pharmaceuticals, Inc.
Inventors:
Longwu Qi, Raj Gopal Venkat, Michael Pierce, Paul B. Robbins, Sudhir R. Sahasrabudhe, Robert Selliah
Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
Abstract: The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.
Type:
Grant
Filed:
October 26, 2011
Date of Patent:
November 26, 2013
Assignee:
GlaxoSmithKline LLC
Inventors:
Kevin J. Duffy, William Henry Miller, Andrea K. Myers, Antony N. Shaw, Michael N. Zimmerman