Abstract: The present teachings provide a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
Type:
Application
Filed:
June 21, 2013
Publication date:
January 2, 2014
Applicant:
UNIVERSITY HEALTH NETWORKS
Inventors:
Heinz W. Pauls, Radoslaw Laufer, Sze-Wan Li, Grace Ng
Abstract: Compounds of Formula I: in which R1, R2, R3, R4 and R10 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.
Type:
Application
Filed:
February 24, 2012
Publication date:
January 2, 2014
Applicant:
ARRAY BIOPHARMA INC.
Inventors:
James F. Blake, Robert Kirk Delisle, Lisa A. De Meese, James M. Graham, Yvan Le Huerou, Michael Lyon, John E. Robinson, Eli M. Wallace, Bin Wang, Rui Xu
Abstract: The present invention is directed to piperidinone carboxamide spirohydantoin derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the 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:
Application
Filed:
March 14, 2012
Publication date:
January 2, 2014
Inventors:
Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Helen J. Mitchell, Cheng Wang
Abstract: Remote marker systems are disclosed for marking a target using optical markers, including systems that allow a target to be marked using a remote optical marking device, as well as photochromic solutions and methods of their preparation.
Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
Type:
Grant
Filed:
June 10, 2013
Date of Patent:
December 31, 2013
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.
Type:
Application
Filed:
August 27, 2013
Publication date:
December 26, 2013
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
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
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
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
Abstract: An optically active spirolactone compound is highly enantioselectively produced by using an iodoarene derivative which can be synthesized easily and which is not racemized easily. A hypervalent iodine compound precursor (iodoarene derivative) which was able to be designed flexibly was synthesized from 2,6-dihydroxyiodoarene by using 1,2-aminoalcohol as a chiral source in short steps, a hypervalent iodine compound was prepared in a reaction system (in situ) by using a catalyst quantity of the resulting precursor in the presence of a stoichiometric quantity of m-CPBA, and a spirolactonization reaction of 3-(1-hydroxy-2-naphthyl)propionic acid was induced. As a result, a corresponding spirolactone compound was obtained at a high enantiomeric excess.
Type:
Application
Filed:
March 6, 2012
Publication date:
December 19, 2013
Applicant:
NATIONAL UNIVERSITY CORPORATION NAGOYA UNIVERSITY
Inventors:
Kazuaki Ishihara, Muhammet Uyanik, Takeshi Yasui
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
Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
Type:
Application
Filed:
May 20, 2013
Publication date:
December 19, 2013
Applicant:
Novartis AG
Inventors:
Matthew Burger, Joseph E. Drumm, III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
Abstract: The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).
Type:
Application
Filed:
November 30, 2011
Publication date:
December 12, 2013
Inventors:
David C. Tully, Paul Vincent Rucker, Phillip B. Alper, Daniel Mutnick, Donatella Chianelli
Abstract: This application describes compounds that can act as opioid receptor ligands, which compounds can be used in the treatment of, for example, pain and pain related disorders.
Type:
Application
Filed:
August 12, 2013
Publication date:
December 12, 2013
Applicant:
Trevena, Inc.
Inventors:
Dennis Yamashita, Dimitar Gotchev, Philip Pitis, Xiao-Tao Chen, Guodong Liu, Catherine C.K. Yuan
Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
Type:
Grant
Filed:
September 25, 2009
Date of Patent:
December 3, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer
Abstract: The present invention provides a compound of formula (II): where R1 is a substituted alkyl, heterocyclic, or cycloalkyl, group, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof, and pharmaceutical compositions comprising these compounds. Also provided are methods of using these compounds to treat a disease or condition mediated by CDK9, such as cancers and other conditions described herein.
Type:
Application
Filed:
January 20, 2012
Publication date:
November 14, 2013
Applicant:
Novartis AG
Inventors:
William R. Antonios-McCrea, Paul A. Barsanti, Cheng Hu, Xianming Jin, Eric Martin, Yue Pan, Xiaodong Lin, Keith B. Pfister, Paul A. Renhowe, Martin Sendzik, James Sutton, Lifeng Wan
Abstract: The invention is directed to methods of using antagonists selective for the metabotropic mGlu5 receptor to treat conditions of neuromuscular dysfunction of the lower urinary tract in a mammal. Provided are methods of treating a mammal suffering from a condition of neuromuscular dysfunction of the lower urinary tract by administering a selective mGlu5 antagonist. The selective mGlu5 antagonist may be administered alone or in combination with one or more additional therapeutic agents for treating such a condition. Also provided are methods of identifying selective mGlu5 antagonists that are useful for treating neuromuscular dysfunction of the lower urinary tract in a mammal. Methods for treating migraine and gastroesophageal reflux disease (GERD) using selective mGlu5 antagonists are also disclosed.
Type:
Grant
Filed:
July 11, 2011
Date of Patent:
November 12, 2013
Assignee:
Recordati Ireland Ltd.
Inventors:
Amedeo Leonardi, Gianni Motta, Carlo Riva, Luciano Guarneri, Davide Graziani, Carlo De Toma, Katia Dimitrova Karamfilova
Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.
Type:
Grant
Filed:
August 29, 2012
Date of Patent:
October 29, 2013
Inventors:
Valentina Molteni, Hank Michael James Petrassi, Xiaolin Li, Xiaodong Liu, Jon Loren, Juliet Nabakka, Bao Nguyen, Vince Yeh
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
Abstract: The present invention relates to morphinan derivatives and preparation methods thereof, especially to ketal hydroxyl protected compounds of morphinan derivatives and preparation method thereof, and to a method for preparing corresponding alkylated morphinan derivatives by using the ketal hydroxyl protected compounds as intermediates, and more especially to a ketal hydroxyl protected compound of methylnaltrexone as intermediate for preparing methylnaltrexone and a method for preparing methylnaltrexone through said intermediate.
Type:
Grant
Filed:
June 19, 2009
Date of Patent:
October 22, 2013
Assignee:
Chongqing Pharmaceutical Research Institute Co., Ltd.
Inventors:
Huafu Sun, Jie Luo, Wenrun Ye, Jie Deng, Bo Lin, Chunyan Dan, Bin Fan
Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
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
Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal.
Type:
Application
Filed:
December 13, 2011
Publication date:
October 17, 2013
Inventors:
Mark Laurence Boys, Robert Kirk Delisle, Erik James Hicken, April L. Kennedy, David A. Mareska, Fredrik P. Marmsater, Mark C. Munson, Brad Newhouse, Bryson Rast, James P. Rizzi, Martha E. Rodriguez, George T. Topalov, Qian Zhao
Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
Type:
Application
Filed:
June 10, 2013
Publication date:
October 17, 2013
Inventors:
Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
Abstract: The present invention is directed to fused heterocyclic azaindane carboxamide derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the 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:
Application
Filed:
December 16, 2011
Publication date:
October 10, 2013
Inventors:
Christopher S. Burgey, Anthony Ginnetti, Ashley Nomland, Daniel V. Paone
Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
Type:
Application
Filed:
December 6, 2011
Publication date:
October 10, 2013
Applicant:
AUTIFONY THERAPEUTICS LIMITED
Inventors:
Giuseppe Alvaro, Paolo Dambruoso, Simona Tommasi, Anne Decor, Charles Large
Abstract: The present invention provides compounds of formula M-L-M? (where M and M? are each independently a monomeric moiety of Formula (I), (II), (III) or (IV) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.
Type:
Application
Filed:
December 13, 2011
Publication date:
October 10, 2013
Applicant:
NOVARTIS AG
Inventors:
Christopher Sean Straub, Zhuoliang Chen
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
Abstract: The present invention is directed to fused heterocyclic indane carboxamide derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the 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:
Application
Filed:
December 16, 2011
Publication date:
October 3, 2013
Inventors:
Christopher S. Burgey, Anthony Ginnetti, Daniel V. Paone
Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
Type:
Grant
Filed:
May 24, 2012
Date of Patent:
October 1, 2013
Assignee:
Novartis AG
Inventors:
Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
Type:
Application
Filed:
March 6, 2013
Publication date:
September 26, 2013
Inventors:
Mikhail CHAFEEV, Sultan CHOWDHURY, Lauren FRASER, Jianmin FU, Jonathan LANGILLE, Shifeng LIU, Jianyu SUN, Shaoyi SUN, Serguei SVIRIDOV, Mark WOOD, Alla Yurevna ZENOVA, Qi JIA, Jean-Jacques Alexandre CADIEUX, Simon J. GAUTHIER, Amy Frances DOUGLAS, Tom HSIEH, Nagasree CHAKKA, Zoran CIKOJEVIC
Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
Type:
Application
Filed:
February 26, 2013
Publication date:
September 12, 2013
Applicant:
Bristol-Myers Squibb Company
Inventors:
Vivekananda M. Vrudhula, Senliang Pan, Ramkumar Rajamani, John E. Macor, Joanne J. Bronson, Carolyn Diane Dzierba, Susheel Jethanand Nara, Maheswaran Sivasamban Karatholuvhu
Abstract: Substituted spiro-amide compounds corresponding to formula I in which R5 through R8, D, X, Y and Z have defined meanings, processes for preparing such spiro-amide compounds, pharmaceutical compositions containing such compounds, and methods of using such spiro-amide compounds for treating and/or inhibiting disorders or disease states mediated at least in part by the bradykinin 1 receptor.
Abstract: The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.
Type:
Application
Filed:
April 16, 2013
Publication date:
September 5, 2013
Applicant:
H. LUNDBECK A/S
Inventors:
Mathivanan Packiarajan, Allen Hopper, Anette Graven Sams, Gitte Kobberoee Mikkelsen, Michel Grenon
Abstract: The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the 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:
Application
Filed:
November 10, 2011
Publication date:
September 5, 2013
Inventors:
Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, Blair C. Zartman, Heather E. Stevenson
Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
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.
Abstract: Heterobicyclic compounds of Formula (I): or a pharmaceutically-acceptable salt, tautomer, or stereoisomer thereof, as defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, Huntington's Disease, and the like.
Abstract: A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.
Type:
Application
Filed:
March 21, 2013
Publication date:
August 29, 2013
Applicant:
Sloan-Kettering Institute for Cancer Research
Inventors:
Ouathek Ouerfelli, Anna Dilhas, Guangbin Yang, Hong Zhao
Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
Type:
Grant
Filed:
February 10, 2011
Date of Patent:
August 27, 2013
Assignee:
Celgene Corporation
Inventors:
Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
Abstract: Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. Wherein R1, L1, R3, R4, Cy, L2 and R5 are as defined herein.
Type:
Application
Filed:
February 7, 2013
Publication date:
August 22, 2013
Inventors:
Christel Jeanne Marie MENET, Benoit Antoine SCHMITT, Raphael Jean Joel GENEY, Kevin James DOYLE, Joanne PEACH, Nicholas John PALMER, Graham Peter JONES, David HARDY, James Edward Stewart DUFFY
Abstract: The present invention relates to compounds defined by formula I wherein the variables R1-R8 are defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this protein.
Type:
Application
Filed:
August 16, 2012
Publication date:
August 15, 2013
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Thomas TRIESELMANN, Dieter HAMPRECHT, Holger WAGNER
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
Abstract: The present invention relates to a novel amide derivative. More specifically, the present invention provides a medicinal agent useful as a prophylactic or therapeutic agent for diseases, which relies on the production of cytokines from T cells, and which comprises an amide derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or the pharmacologically acceptable salt as an active ingredient. Provided is an amide derivative represented by general formula (I) [wherein each symbol is as defined in the description] or a pharmacologically acceptable salt thereof, or a solvate of the derivative or the pharmacologically acceptable salt.
Abstract: The present invention relates to crystalline forms of (3R,9S)-4-isopropyl-7,7-dimethyl-3-(4-(trifluoromethyl)phenyl)-2?,3?,5?,6,6?,7,8,9-octahydro-3H-spiro[furo[3,4-c]quinoline-1,4?-pyran]-9-ol and its hydrochloride or hydrobromide salts, to a process for the manufacture thereof, and to the use thereof in pharmaceutical compositions.
Type:
Application
Filed:
August 17, 2012
Publication date:
August 15, 2013
Applicant:
Boehringer Ingelheim International GmbH
Inventors:
Markus OSTERMEIER, Kai GERLACH, Peter SIEGER
Abstract: Provided herein are improved fluorogenic compounds and probes that can be used as reagents for measuring, detecting and/or screening peroxynitrite. The fluorogenic compounds of the invention can produce fluorescence colors, such as green, yellow, red, or far-red. Also provided herein are fluorogenic compounds for selectively staining peroxynitrite in the mitochondria of living cells. Provided also herein are methods that can be used to measure, directly or indirectly, the presence and/or amount of peroxynitrite in chemical samples and biological samples such as cells and tissues in living organisms. Also provided are high-throughput screening methods for detecting or screening peroxynitrite or compounds that can increase or decrease the level of peroxynitrite in chemical and biological samples.