Abstract: The invention relates to a method for obtaining pure tetrahydrocannabinol from reaction mixtures containing tetrahydrocannabinol compounds or from raw products containing tetrahydrocannabinol compounds. According to said method, the tetrahydrocannabinol compounds in the reaction mixture or in the raw product are converted into crystallisable derivatives, preferably using a suitable solvent, said derivatives are then crystallised and isolated, and the pure tetrahydrocannabinol compounds are then obtained from the crystallised derivatives. The invention also related to the use of compounds produced in this way for the production of a medicament for human therapy, and to the medicaments thus produced.
Abstract: A process for preparing at least one partial oxidation and/or ammoxidation product of a hydrocarbon by partially dehydrogenating at least one saturated hydrocarbon H under heterogeneous catalysis and using the resulting product gas mixture A, which comprises the partially dehydrogenated hydrocarbon H, as such or in modified form for heterogeneously catalyzed partial oxidation and/or ammoxidation of the partially dehydrogenated hydrocarbon present in the product gas mixture A, said process including at least one mechanical separating operation inserted between the product gas mixture A and the heterogeneously catalyzed partial oxidation and/or ammoxidation.
Type:
Grant
Filed:
March 31, 2004
Date of Patent:
March 22, 2011
Assignee:
BASF Aktiengesellschaft
Inventors:
Goetz-Peter Schindler, Otto Machhammer, Klaus Joachim Mueller-Engel, Claus Hechler, Jochen Petzoldt, Christoph Adami, Klaus Harth
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 relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.
Type:
Grant
Filed:
November 12, 2007
Date of Patent:
March 1, 2011
Assignee:
King Pharmaceuticals Research & Development, Inc.
Inventors:
Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli
Abstract: The present invention relates to active bactericidal, antibacterial, anti-infective, antimicrobial, sporicidal, disinfectant, antifungal and antiviral compounds and compositions and to new uses of these compositions in therapy. This specification also describes methods of use for the new compounds and compositions. The specification further describes methods for preparing these compounds.
Type:
Grant
Filed:
September 11, 2008
Date of Patent:
February 22, 2011
Assignee:
Novabay Pharmaceuticals, Inc.
Inventors:
Mansour Bassiri, Ramin Najafi, Lu Wang, Jane Yang
Abstract: Racemic mixtures and enantiomerically pure forms of novel 1-[(2?-substituted)-piperazin-1?-yl]-isoquinolines are norepinephrine (NE) transporter (NET) inhibitor compounds. Compounds of the invention are considered therapeutic agents for central nervous system (CNS) diseases and disorders, without limitation, including neurodegeneration, anxiety, depression, attention deficit disorders, drug dependency, and post traumatic stress disorder. Examples of the chemical syntheses of the compounds of the invention are provided. The isoquinoline compounds of the invention competitively bind at NET at nanomolar concentrations. The isoquinoline agents of the invention bind selectively to NET over other competitive transporter targets and receptor binding sites, including those of serotonin and dopamine, amongst others. The chemical syntheses of the invention are suitable for labeling with radionuclide atoms.
Type:
Grant
Filed:
March 21, 2008
Date of Patent:
February 15, 2011
Assignee:
University of Montana
Inventors:
John M. Gerdes, David B. Bolstad, Michael R. Braden, August W. Barany
Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.
Type:
Grant
Filed:
December 11, 2009
Date of Patent:
February 8, 2011
Assignee:
NicOx S.A.
Inventors:
Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
Abstract: The present invention relates to acid addition salts of aripiprazole, a process for preparing said acid addition salts and their use to prepare or purify aripiprazole in the form of a free base or in the form of a pharmaceutically acceptable salt.
Abstract: A series of new chemical agents that demonstrate anti-tumor activity are described. The new chemical agents combine two major mechanisms of anti-tumor action. In an embodiment, the agents are capable of both inhibiting EGFR and damaging DNA while also, upon degradation, degrading to an inhibitor of EGFR and to an agent capable of damaging DNA. Moreover, a novel series of molecules capable of releasing two moles of EGFR inhibitor and a potent bi-functional alkylating agent are also described.
Abstract: A method for dispersing polymerization by-products and maintaining said by-products in suspension in a hydrocarbon processing system during acrylic acid and acrylate monomer formation is disclosed, which includes adding to the monomer an effective inhibiting amount of an N-alkyl polyalkenyl succinimide dispersant.
Abstract: The iron-containing catalyst suitable for use as a catalyst contains a) iron or a mixture containing iron and an iron-based compound. The iron has an average crystallite size ranging from 1-35 nm measured by X-ray diffraction.
Type:
Grant
Filed:
October 18, 2002
Date of Patent:
January 25, 2011
Assignee:
BASF Aktiengesellschaft
Inventors:
Andreas Ansmann, Christoph Benisch, Peter Baβler, Rolf-Hartmuth Fischer, Stefan Maixner, Johann-Peter Melder, Hermann Luyken
Abstract: An improved process for the preparation of aripiprazole (1) which comprises (i) reacting 6-hydroxy-l-indanone (11) with 1,4-dihalobutane (12) in the presence of a base and a solvent at a temperature in the range of 90 to 110 deg C to form the novel intermediate 6-(4-halo butoxy)-indan-1-one (3), (ii) reacting the novel intermediate with 1-(2,3-clichlorophenyl)-piperazine (9) to get another novel intermediate 6-[4-[4-(2,3-dichlorophenyl)-l-piperazinyl]butoxy]-indan-l-one (2) and (iii) reacting the resulting novel compound with sodium azide. The invention also relates to the novel intermediates of the formulae (2) & (3) and processes for their preparation. The invention also includes intermediate compounds useful for the preparation of aripiprazole.
Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
Type:
Grant
Filed:
June 6, 2008
Date of Patent:
January 18, 2011
Assignee:
Helicon Therapeutics, Inc.
Inventors:
Alan P. Kaplan, Varsha Gupta, Jan W. F. Wasley
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:
May 3, 2005
Date of Patent:
January 4, 2011
Assignee:
Trustees of Dartmouth College
Inventors:
Gordon W. Gribble, Tadashi Honda, Michael B. Sporn, Nanjoo Suh
Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
Abstract: Salt forms of potent modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
Type:
Grant
Filed:
October 23, 2006
Date of Patent:
January 4, 2011
Assignee:
KALYPSYS, Inc
Inventors:
Dennis A. Bennett, Stephan D. Parent, David T. Jonaitis
Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
Type:
Grant
Filed:
June 6, 2008
Date of Patent:
December 28, 2010
Assignee:
Helicon Therapeutics, Inc.
Inventors:
Alan P. Kaplan, Varsha Gupta, Jan W.F. Wasley
Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4 and Q have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric modulators of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain; cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke; neurological disease or injury; sleep disorder; epilepsy; and depression.
Type:
Grant
Filed:
November 12, 2007
Date of Patent:
December 21, 2010
Assignee:
King Pharmaceuticals Research and Development, Inc.
Inventors:
Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli