Abstract: The present invention relates to a novel process for the manufacture of blood-platelet aggregation inhibiting agent. In particular, the present invention is directed to a process for the manufacture of Methyl-(+)-(S)-?-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-S-(4H)acetate bisulfate Form-I.
Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula 1: wherein Q is an optionally substituted azetidinyl, pyrrolidinyl, piperidyl, and indolinyl; or Q is NR25R26; and A, R5, R6, R7, R8, R9, R25, R26 and Ar are substituents.
Type:
Application
Filed:
April 21, 2010
Publication date:
August 12, 2010
Applicant:
IRM LLC
Inventors:
Hong Liu, Arnab Chatterjee, David C. Tully, Phillip Alper, Badry Bursulaya, Jianhua Guo, David H. Woodmansee, Daniel Mutnick, Donald S. Karanewsky, Yun He
Abstract: A method of preparation of (S)—N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine of formula (I) or its pharmaceutically acceptable salt, in which (RS)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine of formula (III) is reacted with an optically active acid, after which a crystallization is made of that diastereoisomer which yields, by reaction with an inorganic or organic base, (S)—N,N-dimethyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine of formula (S)-III, which is then demethylated using alkylchloroformates, followed by a hydrolysis and optional conversion of the compound of formula (I) to its salt.
Type:
Application
Filed:
October 21, 2005
Publication date:
June 4, 2009
Applicant:
ZENTIVA, A.S.
Inventors:
Ludek Ridvan, Petr Hruby, Lukas Placek, Miroslav Kuchar
Abstract: Catalyst systems, methods to improve a catalyst system, and dimerization processes therewith are provided. Catalyst systems which comprise at least one elemental alkali metal supported on an alkali metal carbonate catalyst support, are contacted with a liquid organic solvent in order to improve the isomer ratio of the desired reaction product(s) to undesired product(s).
Abstract: The compound of formula (III), optionally its alkaline salt, is reacted with a compound of formula VII, wherein X is a leaving group, resulting in (S)-rivastigmine of formula II, which is then optionally converted into (S)-rivastigmine hydrogentartrade of formula I.
Type:
Grant
Filed:
October 21, 2003
Date of Patent:
June 9, 2009
Assignee:
Zentiva, a.s.
Inventors:
Hana Stepankova, Josef Hajicek, Stanislav Simek
Abstract: The present invention, relates to a shaft or handle wherein the palm or upper side of the shaft has corner edges whose radius of curvature, at least in the grip area(s), is greater than the radius of curvature in the corresponding finger area(s); a hockey stick provided with such a handle may provide a sense of a better or more comfortable feel on the gripped portion of the handle and/or a sense of a more comfortable and precise control of a blade which may be fixed to the end of such a handle.
Abstract: The present invention relates to novel microparticles formed of amphiphilic polyamino acids which transport active principle(s), AP(s), in particular protein and peptide active principle(s), and to novel modified-release pharmaceutical formulations comprising said AP microparticles. Microparticles of amphiphilic polyamino acid (PO) may include at least one AP (associated noncovalently) which spontaneously form a colloidal suspension of nanoparticles in water, at pH 7.0, under isotonic conditions. The microparticles may be obtained by atomization of a solution or colloidal suspension of PO comprising at least one AP, may have a size of between 0.5 and 100 microns, and may be dispersible in colloidal suspension.
Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
Abstract: A stable, low viscosity bimodal oil in water emulsion having an emulsifier, a continuous water phase and a discontinuous oil phase having an oil:water ratio of from about 70:30 to about 85:15 by weight, the discontinuous oil phase being characterized by two distinct oil droplet sizes D.sub.L and D.sub.S wherein D.sub.L is about 10 to 40 microns and D.sub.S is less than or equal to 5 microns, the ratio of D.sub.L /D.sub.S is greater than or equal to 4 and about 45 to 85% by weight of the oil is in oil droplet size D.sub.L.
Abstract: For the therapy of neurological complications in AIDS sufferers, the use of pharmaceutical compositions containing as an active principle at least one compound selected from the group consisting of S-adenosyl-L-methionine salt, 5-methyl-tetrahydro-folic acid, 5-formyltetrahydro-folic acid, when the active principle consists of S-adenosyl-L-methionine and of a derivative of tetrahydro folic acid, the weight ratio between the S-adenosyl-L-methionine salt and 5-methyltetrahydrofolic acid or 5-formyl-tetrahydrofolic acid is comprised between 10/1 and 4/1, in pharmaceutical form, suitable for oral or parenteral administration.
Abstract: The present invention relates to the finding that receptors for the neurotransmitter 5-HT of the 5-HT2B class are located on the human colon, and that their activation potentiates neuronally-mediated responses, and are thus causative in the abnormal motility and pain associated with IBS. The invention provides a method of treatment of IBS which comprises providing to a patient in need of treatment an effective amount of a 5HT2B receptor antagonist which acts on 5HT2B receptors located in the colon of said patient. Such antagonists may be administered in the form of compositions adapted to be delivered to the colon, such as depot formulations and suppositories. Assay methods for the development of compounds for the treatment of IBS are also provided.
Type:
Grant
Filed:
November 28, 2000
Date of Patent:
September 3, 2002
Assignee:
Pharmagene Laboratories Limited
Inventors:
Richard A. Borman, Nicholas S. Tilford, Gordon S. Baxter
Abstract: Triggered sensor data capture in a mobile device environment. A method monitors primary sensor data obtained from first wearable sensor device(s) to determine whether trigger condition(s) are met for triggering supplemental sensor data capture. Based on recognizing a health event, the method obtains health status input from a user, configures second wearable sensor device(s) to obtain supplemental sensor data that includes additional data in addition to the primary sensor data, and obtains the supplemental sensor data. The method provides the health status input and the obtained supplemental sensor data as correlated health event data of the health event for analysis. Based on the analysis, the method tunes at least one trigger condition of the trigger condition(s) to adjust a scope of supplemental sensor data capture.
Type:
Grant
Filed:
November 18, 2016
Date of Patent:
December 29, 2020
Assignee:
INTERNATIONAL BUSINESS MACHINES CORPORATION
Inventors:
Kathleen Chalas, Jonathan R. Fry, Michael Gschwind, John S. Houston, Alexander C. Leventhal, Cameron E. Tidd, Lahiruka S. Winter