Abstract: The present invention relates to tetrahydroprotoberberines of the formula (I) and the physiologically acceptable salts thereof. The invention also relates to the use of the compounds of the formula (I) or pharmaceutically acceptable salts thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with dopamine receptor ligand, such as schizophrenia.
Type:
Grant
Filed:
July 7, 2006
Date of Patent:
August 6, 2013
Assignees:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Topharman Shanghai Co., Ltd.
Abstract: The present invention relates to an improved process for the preparation of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide—Sunitinib base of formula (I) and its pharmaceutically acceptable malate salt of formula (I(a)).
Abstract: The invention provides a composition comprising (S)2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, wherein the composition is either substantially free of (R)2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol or the composition contains a mixture of the (S) and (R) enantiomers in which the (S) enantiomer predominates. Also provided are processes for the preparation of the (S)2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, novel process intermediates and methods for making the novel process intermediates.
Type:
Grant
Filed:
July 11, 2011
Date of Patent:
July 30, 2013
Assignees:
Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology Limtied
Inventors:
Steven John Woodhead, David Charles Rees, Kyla Merriom Grimshaw
Abstract: A process for carrying out at least two unit operations in series, the process comprising the step of: (a) directing a feed stream into an integrated assembly which comprises a first microchannel unit operation upon at least one chemical of the feed stream to generate a distributed output stream that exits the first microchannel unit operation in a first set of discrete microchannels isolating flow through the discrete microchannels; and (b) directing the distributed output stream of the first microchannel unit operation into a second microchannel unit operation as a distributed input stream, to continue isolating flow between the first set of discrete microchannels, and conducting at least one operation upon at least one chemical of the input stream to generate a product stream that exits the second microchannel unit operation, where the first microchannel unit operation and the second unit operation share a housing.
Type:
Grant
Filed:
September 5, 2007
Date of Patent:
July 30, 2013
Assignee:
Velocys, Inc.
Inventors:
Anna Lee Y. Tonkovich, Robert D. Litt, Timothy M. Werner, Bin Yang
Abstract: The invention relates to the use of compounds of formula (I) and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
Type:
Grant
Filed:
April 20, 2011
Date of Patent:
July 23, 2013
Assignee:
AstraZeneca AB
Inventors:
Elaine S E Stokes, Darren Mckerrecher, Laurent F A Hennequin, Patrick Ple
Abstract: The present invention relates to processes for the preparation of oxindoles and ortho-substituted anilines and their use as intermediates for syntheses. The invention further relates to a process for the preparation of compounds of formula (4): where a mixture of an aniline (compound of formula Q) is reacted with a thioether (compound of formula W): in the presence of a chlorinating agent and an organic solvent at a reaction temperature in the range above ?65° C.
Abstract: The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
Type:
Grant
Filed:
October 14, 2005
Date of Patent:
July 16, 2013
Assignee:
Abbott GmbH & Co., KG
Inventors:
Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
Abstract: The present invention, in one or more embodiments, comprises water-soluble derivatives of 3-n-pentadecylcatechol (poison ivy urushiol saturated congener) and/or 3-n-heptadecylcatechol (poison oak urushiol saturated congener) as compositions for the prevention and/or prophylactic treatment of contact dermatitis caused by poison ivy and poison oak. The present invention is also directed towards processes for making such compounds. Disclosed are compounds which are effective for tolerizing and desensitizing a subject against allergens contained in plants of the Anacardiaceae and Ginkgoaceae families comprising water soluble urushiol esters of general formula (I) Tolerizing and desensitizing mammals, including humans, to allergens contained in plants of the Anacardiaceae and Ginkgoaceae families is attained by administering a composition containing at least one water soluble urushiol ester compound.
Type:
Grant
Filed:
April 3, 2009
Date of Patent:
July 16, 2013
Assignee:
The University of Mississippi
Inventors:
Mahmoud A. Elsohly, Waseem Gul, Mohammad Khalid Ashfaq, Susan P. Manly
Abstract: The present invention relates to novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, to novel antiviral active ingredients, pharmaceutical compositions, antiviral medicaments, methods for prophylaxis and treatment of viral diseases particularly caused by influenza viruses and infectious hepatisis C (HCV) viruses.
Type:
Grant
Filed:
November 27, 2009
Date of Patent:
July 9, 2013
Inventors:
Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko, Pavel Mikhailovich Yamanushkin, Oleg Dmitrievich Mitkin, Vladimir Yurievich Vvedensky, Vadim Vasilievich Bichko
Abstract: The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 2 (polymorphic form I) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.
Type:
Grant
Filed:
June 7, 2012
Date of Patent:
July 9, 2013
Assignee:
Apotex Technologies Inc.
Inventors:
Tim Fat Tam, Blaise N'Zemba, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao, Lily Yu
Abstract: Thieno[2,3-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
Abstract: Disclosed is a process for preparing a molybdated succinimide complex, the process comprising: (a) reacting an alkyl or alkenyl succinimide of a polyamine of formula I or formula II or mixtures thereof: wherein R is an about C12 to C30 alkyl or alkenyl group, R? is a straight or branched-chain alkylene group having 2 to 3 carbon atoms, x is 1 to 11, and y is 1 to 10, with an ?,?-unsaturated mono-carboxylic acid or carboxylic acid ester, in a charge mole ratio of the ?,?-unsaturated mono-carboxylic acid or carboxylic acid ester to the succinimide of formula I or formula II or mixtures thereof of about 0.1:1 to about 6:1, and wherein the reaction temperature is no greater than about 135° C.; and (b) reacting the succinimide product of step (a) with an acidic molybdenum compound to provide the molybdated succinimide complex, wherein the molybdated succinimide complex prepared is a liquid at room temperature.
Type:
Grant
Filed:
January 21, 2011
Date of Patent:
July 2, 2013
Assignee:
Chevron Oronite Company LLC
Inventors:
Kenneth D. Nelson, James J. Harrison, Paula Rogers, Mitra Hosseini
Abstract: Processes for the preparation of Silodosin and its intermediates comprising reductive amination of compound of Formula (VIII) with a compound of Formula (VII) or a compound of Formula (XV) in a suitable solvent using a reducing agent.
Abstract: The present invention relates to new salts of perindopril, particularly to a new calcium salt and new amine salts of perindopril, to a process for their preparation and to a pharmaceutical formulations containing the new salts.
Type:
Grant
Filed:
June 27, 2008
Date of Patent:
June 25, 2013
Assignee:
KRKA, Tovarna Zdravil D.D. Novo Mesto
Inventors:
Marjo Merslavic, Sergeja Bombek, Urska Gojak, Matej Smrkolj, Rok Zupet
Abstract: Cyanine dye compounds having a substituted methine moiety that are nucleic acid stains, particularly for fluorescent staining of RNA, including compounds having the formula where R1 is a C1-C6 alkyl, sulfoalkyl, carboxyalkyl or C1-C6 alkoxy; each R2 is independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, fused benzo, trifluoromethyl, amino, sulfo, carboxy and halogen, that is optionally further substituted; at least one of R3, R4, and R5 is an alkyl, aryl, heteroaryl, cyclic, or heterocyclic moiety that is optionally substituted by alkyl, amino, aminoalkyl, carboxy, nitro, or halogen; and the remaining R3, R4 or R5 are hydrogen; X is S, O, or Se; and D is a substituted or unsubstituted pyridinium, quinolinium or benzazolium moiety.
Type:
Grant
Filed:
August 5, 2010
Date of Patent:
June 25, 2013
Assignee:
Life Technologies Corporation
Inventors:
Jason Dallwig, David Hagen, Ching-Ying Cheung, Gerald Thomas, Stephen Yue
Abstract: The present invention relates to novel polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl-2,4-dimethyl-1H-pyrrole-3-carboxamide-Sunitinib base (I). The present invention also relates to methods of preparing such polymorphic crystals.
Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.
Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.