Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.
Type:
Grant
Filed:
August 11, 2000
Date of Patent:
April 1, 2008
Assignee:
Wyeth
Inventors:
Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Juo Qing Guo
Abstract: The object of the invention is to provide polyester-based fiber which maintains physical properties of usual polyester fiber, such as heat resistance, strength and elongation and is excellent in setting ability with controlled gloss of the fiber, artificial hair using the same, a method of producing polyester-based fiber, and a method of producing artificial hair by using the same. To achieve the object, a composition obtained by melt-kneading polyalkylene terephthalate or a copolymerized polyester (A) based on polyalkylene terephthalate, polyarylate (B) and a phosphite compound (C) is melt-spun to form fiber. In the case of melt-kneading, the ester exchange reaction of components (A) and (B) is prevented due to the inhibitory effect of the component (C) on the ester exchange reaction, the heat resistance and physical properties of the fiber are not deteriorated, and a matte effect is brought about by formation of protrusions on the surface of the fiber.
Abstract: A compound or a salt thereof having the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: and inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases into which over expression of AP-1 participates and as an AP-1 inhibitor.
Abstract: An apparatus and methods to produce synergistic mixtures (or combinations) of haloamines to control growth of microorganisms in aqueous systems are disclosed. The apparatus and methods to produce synergistic mixtures entails producing a batch quantity of a haloamine and converting part of the haloamine to a second haloamine species to form the synergistic mixture.
Type:
Grant
Filed:
August 24, 2006
Date of Patent:
December 25, 2007
Assignee:
Hercules Incorporated
Inventors:
Freddie L. Singleton, Michael J. Mayer, Alexander W. Breen
Abstract: Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian Factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
Type:
Grant
Filed:
April 1, 2002
Date of Patent:
December 25, 2007
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Bing-Yan Zhu, Penglie Zhang, Erick A. Goldman, Zhaozhong Jon Jia, Shawn Bauer, Wenrong Huang, John Woolfrey, Robert M. Scarborough
Abstract: A process for the preparation of a compound of formula (I) or a single enantiomer thereof, or a salt or a solvate thereof, wherein W is a chiral auxiliary or hydrogen and P1 and P2 are each independently selected from hydrogen or a protecting group, which comprises: a)treatment of a compound of formula (II), or a salt or a solvate thereof, wherein W is a chiral auxiliary and P1 and P2 are each independently chosen from a protecting group, with a compound of formula (III) to form a resulting product, b) treating the resulting product with a reducing agent to form the compound of formula (I), or a single enantiomer thereof, or a salt or a solvate thereof.
Abstract: The present invention provides compounds of formula (I): wherein each R independently represents a halogen atom or a C1-4 alkyl group; R1 represents a C1-4 alkyl group; R2 represents hydrogen or a C1-4 alkyl group; R3 represents hydrogen or C1-4 alkyl group; R4 represents a trifluoromethyl group; R5 represents hydrogen, a C1-4 alkyl group or C(O)R6; R6 represents C1-4 alkyl, C3-7 cycloalkyl, NH(C1-4 alkyl) or N(C1-4alkyl)2; m is zero or an integer from 1 to 3; n is an integer from 1 to 3; or a pharmaceutically acceptable salt or solvate thereof; compositions containing the same, processes for their preparation and methods for their use in the treatment of conditions mediated by tachykinins.
Abstract: An improved process for the manufacture of formylphosphonic acid derivatives is reported. An aminomethylphosphonic acid substrate is contacted with a reagent selected from the group consisting of water, an alcohol, a phenol compound, and mixtures thereof and an oxidizing gas in the presence of a catalyst to form a reaction product mixture containing a formylphosphonic acid derivative and the conditions under which said contacting is carried out are controlled so that no more than 50% of the formylphosphonic acid derivative formed in the reaction product mixture is consumed by reaction with the reagent.
Abstract: Compounds of formula (I): and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective ?2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).
Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
Type:
Grant
Filed:
June 25, 2004
Date of Patent:
November 6, 2007
Assignee:
Merck + Co., Inc.
Inventors:
Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca, Harold G. Selnick
Abstract: A process for making medium and long chain alkylaromatics and alkylphenols having a high level of anti-Markovnikov addition of the alkyl group. The alkylaromatics and alkylphenols made by the process of the present invention have enhanced stability and are particularly well suited to make highly stable oil additives and enhanced oil recovery surfactants.
Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
Type:
Grant
Filed:
October 25, 2002
Date of Patent:
October 9, 2007
Assignee:
Abbott Laboratories
Inventors:
Eric J. Stoner, Arthur J. Cooper, Lawrence Kolaczkowski, Ketan M. Patel, Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Daniel A. Dickman, Patricia A. Oliver, Jien-Heh J. Tien
Abstract: The invention describes a process for preparing alkoxylated, phosphorus-containing compounds, using heterogeneous catalysts based on metal oxides of aluminum, so that the product can be worked up anhydrously.
Type:
Grant
Filed:
March 15, 2006
Date of Patent:
September 25, 2007
Assignee:
LANXESS Deutschland GmbH
Inventors:
Thomas Weiss, Wolfgang Grape, Rainer Elbert, Jan- Gerd Hansel, Johannes Kaulen
Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
Type:
Grant
Filed:
April 2, 2002
Date of Patent:
August 21, 2007
Assignee:
Merck & Co., Inc.
Inventors:
Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
Type:
Grant
Filed:
March 9, 2006
Date of Patent:
August 7, 2007
Assignee:
Pfizer Inc.
Inventors:
James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: Method of preparing diaminodiphenylmethane and higher homologues thereof from aniline and formaldehyde in the presence of heterogeneous solid acid catalysts selected from (a) delaminated zeolites and/or (b) metal silicate catalysts having an ordered mesoporous pore structure and/or (c) delaminated phyllosilicates.
Type:
Grant
Filed:
September 21, 2004
Date of Patent:
July 3, 2007
Assignee:
Huntsman International LLC
Inventors:
Pablo Botella Asuncion, Joris Karel Peter Bosman, Avelino Corma, Christopher John Mitchell
Abstract: A process for preparing (S)-(?)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4-[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide(IIa) with fluoroamine (III) in the presence of triacetoxyborohydride and ethyl acetate to provide [4-[-4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxylphenyl]methanesulfonamide (I) and then converting I into the hemifumarate salt Ia. A process for preparing IIa is also claimed as well as intermediates IIa-IId.
Type:
Grant
Filed:
February 28, 2005
Date of Patent:
June 19, 2007
Assignee:
Pharmacia & Upjohn Company
Inventors:
Sonja Suzanne MacKey, Michael E. Matison, Haifeng Wu, Michael Paul Goble, Moses W. McMillan, Vikram Gurudath Kalthod
Abstract: The present invention relates to RS 1-{4-[2-(allyloxy)-ethyl]phenoxy}-3-isopropylamino propan-2-ol of the formula (1), process for preparation thereof by selective allylation of p-hydroxy phenyl ethanol and use thereof in a preparation of RS betaxolol of formula (2)
Type:
Grant
Filed:
November 1, 2004
Date of Patent:
June 5, 2007
Assignee:
Council of Scientific and Industrial Research
Abstract: Forming a 4-aminobiphenyl derivative arylamine compound, includes (i) providing a first disubstituted 4-aminobiphenyl compound; (ii) optionally formylating the first disubstituted 4-aminobiphenyl compound to form a bisformyl substituted compound where the first disubstituted 4-aminobiphenyl compound is not a bisformyl substituted compound; (iii) acidifying the bisformyl substituted compound to convert formyl functional groups into acid functional groups to form an acidified compound; and (iv) hydrogenating the acidified compound to saturate at least one unsaturated double bonds in the acidified compound.
Abstract: A compound having the following formula: wherein R3 and M are defined herein, and processes therewith.
Type:
Grant
Filed:
August 22, 2003
Date of Patent:
January 1, 2008
Assignee:
Dow AgroSciences LLC
Inventors:
Michael J. Ricks, Richard B. Rogers, William H. Dent, III, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamad M. Niyaz, Irene M. Morrison, Matthew J. Henry, Jenifer L. Adamski Butz, Robert P. Gajewski