Abstract: This invention relates generally to bis-amino acid sulfonamides containing substituted benzyl amines of formula I:
or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as assay standards or reagents, and intermediates and processes for making the same.
Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.
Type:
Grant
Filed:
June 30, 2000
Date of Patent:
April 1, 2003
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
William P. Dankulich, Daniel G. McGarry, Christopher Burns, Timothy F. Gallagher, Francis A. Volz
Abstract: The invention relates to a process for the preparation of carbonyl compounds by the oxidation of alcohols in the presence of osmium compounds as catalysts in water or a solvent mixture containing water.
Type:
Application
Filed:
July 23, 2002
Publication date:
March 20, 2003
Inventors:
Markus Eckert, Hans-Christian Militzer, Matthias Beller, Christian Dobler, Gerald Mehltretter, Uta Sundermeier
Abstract: Phenylalkanoic acid derivatives of formula (1) are described:
wherein
Ar1 is an aromatic or heteroaromatic group;
L1 is a covalent bond or a linker atom or group;
A is an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group;
R is a carboxylic acid (—CO2H) or a derivative thereof;
and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha 4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
Type:
Grant
Filed:
September 29, 1999
Date of Patent:
March 18, 2003
Assignee:
Celltech R&D Limited
Inventors:
John Robert Porter, Graham John Warrellow, Sarah Catherine Archibald, John Clifford Head
Abstract: A compound of formula (I) wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NOS(nitric oxide synthasey)-mediated diseases such as adult respiratory distress syndrome, myocarditis, synovitis, septic shock, insulin-ependent diabetes mellitus, ulcerative colitis, cerebral infarction, rheumatoid arthritis, osteoarthritis, osteoporosis, systemic lupus erythematosus, rejection by organ transplantation, asthma, pain, ulcer, and the like in human being and animals.
Abstract: Novel compounds of the pyridinium series useful for the management of diabetes and aging-related vascular and neurovascular complications, including kidney disease, nerve damage, atherosclerosis, retinopathy, inflammatory disorders, immunological disorders, oxidative stress, dermatological disorders and discoloration of teeth, by breaking preformed AGE, of the general formula I, or pharmaceutically acceptable salts thereof, 1
Abstract: The present invention provides the compound having the formula:
wherein each of R1 and R2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH2—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
Type:
Grant
Filed:
August 24, 2000
Date of Patent:
January 28, 2003
Assignees:
Sloan-Kettering Institute for Cancer Research, The Trustees of Columbia University in the City of New
York
Inventors:
Ronald Breslow, Sandro Belvedere, Leland Gershell, Thomas A. Miller, Paul A. Marks, Victoria M. Richon, Richard A. Rifkind
Abstract: The instant invention provides compositions and methods for modeling post-Amadori AGE formation and the identification and characterization of effective inhibitors of post-Amadori AGE formation, and such identified inhibitor compositions.
Type:
Application
Filed:
August 8, 2002
Publication date:
January 16, 2003
Applicant:
University of Kansas Medical Center.
Inventors:
Billy G. Hudson, Parvin Todd, Raja Gabriel Khalifah, Aaron Ashley Booth
Abstract: Disclosed are nicotinanilide-N-oxide compounds, methods for their production, pharmaceutical compositions which include these compounds, and methods for their use in various therapies.
Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.
Abstract: The present invention provides methods for the asymmetric synthesis of (S,S,R)-(−)-actinonin and its analogs and the compounds thereby synthesized having a structural formula: 1
Type:
Application
Filed:
March 19, 2002
Publication date:
December 26, 2002
Inventors:
William G. Bornmann, Francis Sirotnak, Howard Scher, Ephraim Vidal, Christopher Borella, David Scheinberg
Abstract: There is disclosed a genus of compounds and pharmaceutical compositions that are protective for mitigating damage associated with tissue ischemia, particularly stroke (CNS ischemia), and ischemia of the myocardium. The present invention further provides a method for treating tissue damage caused by ischemia. Lastly, the present invention provides a method for treating tissue damage caused by providing a compound that inhibits the cytotoxic activity of 3-aminopropanal.
Type:
Application
Filed:
May 7, 2002
Publication date:
December 19, 2002
Inventors:
Kevin J. Tracey, Yousef Al-Abed, Svetlana Ivanova, Richard J. Bucala
Abstract: Propanolamine derivatives represented by the following formula (I):
These derivatives may be &bgr;3 agonists and exert sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-urinary incontinence and anti-pollakiuria activities. Pharmaceutical compositions containing such propanolamine derivatives, methods for the prevention and/or treatment diseases using these propanolamine derivatives, and processes for their preparation are also described.
Abstract: An efficient and selective process, capable of scale-up, to make itaconate derivatives of formula (IV), and/or succinate derivatives of formula (V) and/or (VI) by asymmetric hydrogenation of the itaconate derivatives.
Type:
Application
Filed:
July 18, 2002
Publication date:
December 12, 2002
Inventors:
Andrew Michael Derrick, Nicholas Murray Thomson
Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.
Abstract:
The present invention is concerned with new pyridine double esters of formula (I), their acids, and pharmaceutically acceptable salts. These compounds can be obtained by oxydation of the corresponding 1,4-dihydropyridines, and they are useful as cardioprotective agents in pharmaceutical compositions.
Abstract: The present invention relates to a novel antifungal antibacterial compound 2-methylheptylisonicotinate of formula 1 below obtained from natural sources and to a process for the isolation thereof.
Type:
Application
Filed:
December 20, 2001
Publication date:
October 31, 2002
Applicant:
Council of Scientific and Industrial Research
Inventors:
Gojendra Nath Bordoloi, Babita Kumari, Nabibjyoti Bordoloi, Monoj Kanti Roy, Tarun Chandra Bora
Abstract: HIV protease inhibitors inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds can be prepared by the novel methods of the present invention using the novel inventive compounds and intermediates.
Abstract: Compositions comprising TRH and a compound of the general formula A—B—C—D(—E)p are used for treating the catabolic state of prolonged critical illness.
Abstract: The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, and, optionally, 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 vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, 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 vasoactive agent.
Abstract: Compounds of formula (I)
are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
Type:
Grant
Filed:
May 8, 1998
Date of Patent:
September 17, 2002
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
Abstract: There is provided a process for preparing a heteroaromatic aldehyde by catalytic reaction of alkyl-substituted heteroaromatic compound with molecular oxygen in a gaseous phase in the presence of a catalyst, which comprises employing an oxide containing vanadium, phosphorus, aluminium and silicon as a catalyst, and diluting a part or all of the oxide present as a catalyst layer in a reactor with a solid inert to the reaction.
Abstract: The present invention provides compounds, pharmaceutical compositions and methods that are useful in modulating the farnesoid X receptor (FXR). As FXR is involved in negatively controlling the expression level of cholesterol 7&agr;-hydroxylase (cyp7a), the rate-limiting enzyme involved in the oxidative metabolism of cholesterol into bile acids, the compounds described herein find utility in treating diseases associated with abnormally high or low cholesterol levels. In certain aspects, the FXR modulators (e.g., antagonists) described herein block the negative feed-back downregulation of cyp7a expression produced by certain cholic acids, the endogenous ligands for FXR. Moreover, as FXR forms heterodimers with the retinoid X receptor (RXR) in some cell types, modulation of the level of FXR activity in cells has a wide range of effects on a variety of biological processes which are mediated by RXR or other RXR-interacting proteins such as PPAR&ggr; and PPAR&agr;.
Type:
Application
Filed:
August 31, 2001
Publication date:
August 29, 2002
Applicant:
Tularik Inc.
Inventors:
Jonathan Houze, Sharon McKendry, Joshua P. Gergely, Yi Xia, Bei Shan, Frank Kayser
Abstract: The invention provides peptide derivatives designed to deliver peptides having growth factor inhibitory activity, especially somatostatin analogs, to the retina by sequential metabolism. The peptide derivatives, which comprise a dihydropyridinepyridinium salt-type redox targetor moiety, a bulky lipophilic function and an amino acid/dipeptide/tripeptide spacer, are used in the prevention and treatment of diabetic retinopathy.
Type:
Grant
Filed:
September 1, 1998
Date of Patent:
August 27, 2002
Assignee:
University of Florida
Inventors:
Nicholas Stephen Bodor, Maria Bartolomeo Grant
Abstract: Tertiary amines of the formula
wherein
A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.
Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.
Type:
Grant
Filed:
September 5, 2000
Date of Patent:
August 6, 2002
Assignee:
Eli Lilly and Company
Inventors:
Sean P. Hollinshead, Michael A. Staszak, John S. Ward, Joseph W. Wilson, Bret E. Huff, Philip F. Hughes, Jose S. Mendoza, Charles H. Mitch
Abstract: 2-lithio-5-halopyridine is formed as a predominant component of a reaction mixture by reacting BuLi with 2,5-dihalopyridine in a non-coordinating solvent.
Type:
Grant
Filed:
February 27, 2001
Date of Patent:
July 16, 2002
Assignees:
Merck & Co., Inc., Merck Frosst Canada & Co
Abstract: The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, and, optionally, 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 vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, 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 vasoactive agent.
Abstract: Compounds of the formula:
wherein the substituents are defined herein which are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.
Type:
Grant
Filed:
December 29, 2000
Date of Patent:
June 25, 2002
Assignee:
American Home Products Corporation
Inventors:
Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Thomas Jones, Stanley Lang, Adma Ross, Eugene A. Terefenko, Bryan O'Hara
Abstract: A biological response modifying metal ion chelating agent such as picolinic acid, analogs or derivatives thereof, and methods of using the same. The agents chelate metals in metal containing protein complexes and enzymes required for growth, replication or inflammatory response. The preparations can be administered systemically or topically. The products can be used to reduce systemic levels of metals in disease states such as Wilson's disease, iron or lead toxicity. The preparations have antineoplastic, antiviral, antiinflammatory, analgesic antiangiogenic, antiproliferative as well as hematopoetic and immune stimulant, effects and are used in the treatment of warts, psoriasis, acne, cancers, sunburn, inflammatory responses, untoward angiogenesis, immune depression and other diseases and in the prevention of sexually transmitted diseases such as genital warts, herpes and AIDS.
Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.
Type:
Application
Filed:
December 6, 2001
Publication date:
June 6, 2002
Inventors:
Jinhua J. Song, Nathan K. Yee, Suresh R. Kapadia
Abstract: Neuroprotective agents are disclosed having the following structure:
wherein R1, R2, R3, R4 and R5 are as defined herein. Such compounds have utility in the treatment of conditions which benefit from administration of neuroprotective agents generally, including treatment of central and peripheral nervous condition as well as for promoting nerve cell differentiation. Methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more of the compounds of this invention.
Type:
Grant
Filed:
November 27, 2000
Date of Patent:
June 4, 2002
Assignee:
Nippon Kayaku Co., Ltd.
Inventors:
Moorthy S. S. Palanki, Shripad S. Bhagwat, Hiroshi Sato, Paul E. Erdman, Mary Doubleday
Abstract: Disclosed is a photographic element comprising a light-sensitive silver halide emulsion layer having associated therewith a cyan “NB coupler” having the formula (I): 1
Type:
Application
Filed:
October 18, 2001
Publication date:
May 2, 2002
Inventors:
William J. Begley, Frank D. Coms, Gary M. Russo
Abstract: Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.
Abstract: A compound having the following formula:
wherein R3 and M are defined herein, and processes therewith.
Type:
Grant
Filed:
August 4, 2000
Date of Patent:
March 12, 2002
Assignee:
Dow AgroSciences LLC
Inventors:
Michael J. Ricks, Richard B. Rogers, William H. Dent, III, Chenglin Yao, Bassam S. Nader, Gina M. Fitzpatrick, Noormohamed M. Niyaz, Matthew J. Henry, Robert P. Gajewski, John L. Miesel, Kevin G. Meyer, Irene M. Morrison, Jenifer L. Adamski Butz
Abstract:
The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine ring being in the 3- or 4-position, in which formula R1 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl, carboxy, C1-C4 alkyl, alkoxy or alkoxycarbonyl, nitro, amino or cyano and Q stands for C4-C20 divalent hydrocarbon radical which can be straight, branched, cyclic, saturated or unsaturated and X stands for carbonyl, carbonylamino, aminocarbonyl, oxycarbonyloxy, oxycarbonyl, carbonyloxy, aminocarbonyloxy, aminothiocarbonyloxy, oxycarbonylamino or oxythiocarbonylamino and Y stands for benzylene or phenylene and R2 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, C1-C4 alkyl, hydroxyalkyl or alkoxy, hydroxy, halogen, trifluoromethyl, cyano, carboxamido, sulfamoyl, nitro, amino, ca
Abstract: This invention relates to a ligandless process wherein heterogeneous Pd catalysts are used to activate aryl and heteroaryl chlorides for cross coupling aryl and heteroaryl chlorides and boronic acids. The process provides for use with either electron-withdrawing or electron-donating substituents, for cross coupling with boronic acids.
Type:
Application
Filed:
July 16, 2001
Publication date:
February 7, 2002
Inventors:
Yongkui Sun, Carl LeBlond, John R. Sowa
Abstract: The invention relates to novel biaromatic compounds having general formula I
and their use in pharmaceutical compositions for use in human and veterinary medicine, in particular for treating dermatological, rheumatic, respiratory, cardiovascular, and ophthalmological disorders, and for use in cosmetic compositions.
Type:
Grant
Filed:
January 8, 1999
Date of Patent:
December 4, 2001
Assignee:
Centre International de Recherches Dermatologiques