Abstract: Couplers for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1):
wherein X is selected from halogen and R2SO4; R3 is selected from C1 to C2 alkyl or hydroxyethyl; R2 is selected from C1 to C22 alkyl and C1 to C22 mono and dihydroxyalkyl; and R is selected from of C1 to C16 alkyl, C1 to C10 hydroxyalkyl, C1 to C6 alkoxyalkyl and benzyl.
Abstract: There are disclosed compounds of the formula 1
Type:
Application
Filed:
February 6, 2002
Publication date:
May 22, 2003
Applicant:
Schering Corporation
Inventors:
Joseph A. Kozlowski, Neng-Yang Shih, Brian J. Lavey, Razia K. Rizvi, Bandarpalle B. Shankar, James M. Spitler, Ling Tong, Ronald L. Wolin, Michael K. Wong
Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII:
wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
September 12, 2002
Date of Patent:
May 20, 2003
Assignee:
3-Dimensional Pharmaceuticals, Inc.
Inventors:
Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
Abstract: Heterocyclically substituted amides of the general formula I
wherein the variables as defined in the specification are useful in pharmaceuticals for the treatment of diseases in which increased interleuken-1 levels occur.
Abstract: This invention relates to novel dihydropyridine soft drugs of the formula &PHgr;OOR1, where &PHgr; is a dihydropyridine moiety. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibroncho-constriction activity. Use of such soft drug analogs permits the administration of greater doses of the claimed dihydropyridine compounds without intolerable systemic effects. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasim, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders, while avoiding unwanted systemic effects.
Type:
Grant
Filed:
May 2, 2001
Date of Patent:
May 13, 2003
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
John H. Dodd, James L. Bullington, Daniel A. Hall, James R. Henry, Kenneth C. Rupert
Abstract: The present invention relates to compounds of Formula (I) which may be useful in the treatment of diseases, such as, metabolic disorders, dyslipidemia and/or hyperchloesterolemia: 1
Type:
Application
Filed:
August 19, 2002
Publication date:
May 1, 2003
Inventors:
Magnus Pfahl, Catherine Tachdjian, Hussien A. Al-Shamma
Inventors:
Karl-Heinz Altmann, Guido Bold, Pascal Furet, Paul William Manley, Jeanette Marjorie Wood, Stefano Ferrari, Francesco Hofmann, Jurgen Mestan, Andreas Huth, Martin Kruger, Dieter Seidelmann, Andreas Menrad, Martin Haberey, Karl-Heinz Thierauch
Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I.
Type:
Application
Filed:
October 30, 2001
Publication date:
April 3, 2003
Applicant:
Merck Frosst Canada & Co.
Inventors:
Daniel Dube, Rejean Fortin, Richard Friesen, Zhaoyin Wang, Jacques Yves Gauthier
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: This invention relates to the novel use of diphenyl sulfamido in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
Type:
Application
Filed:
August 30, 2002
Publication date:
March 20, 2003
Inventors:
Michael R. Palovich, Joseph Weinstock, Katherine L. Widdowson
Abstract: Peptido and peptidomimetic compounds of the formula:
wherein the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also provided.
Type:
Grant
Filed:
April 29, 1999
Date of Patent:
March 11, 2003
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Peter Scott Dragovich, Stephen Evan Webber, Thomas Jay Prins, Ru Zhou, Joseph Timothy Marakovits, Theodore O. Johnson, Jr.
Abstract: Patients susceptible to or suffering from central nervous system disorders (e.g., Alzheimer's disease, Parkinson's disease, Tourette's syndrome, attention deficit disorder or schizophrenia) are treated by administering an effective amount of an aryl substituted olefinic amine compound. Exemplary compounds include (E)-N-methyl-4-[3-(5-benzyloxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-phenoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-isopropoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-methoxymethylpyridin)yl]-3-buten-1-amine, and (E)-N-methyl-4-[3-(5-phenylpyridin)yl]-3-buten-1-amine.
Type:
Grant
Filed:
February 21, 1997
Date of Patent:
March 11, 2003
Assignee:
Targacept, Inc.
Inventors:
Gary Maurice Dull, William Scott Caldwell, Grayland Page Dobson, Craig Harrison Miller
Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstitutedpropanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.
Abstract: Disclosed are substituted phenoxyacetic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds, alone or in combination with other therapeutic agents, and methods of treatment employing the compounds and pharmaceutical compositions, as well as methods for their synthesis.
Type:
Application
Filed:
July 16, 2002
Publication date:
February 20, 2003
Applicant:
The Institutes of Pharmaceutical Discovery LLC.
Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.
Inventors:
Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more fluoro-substituted benzenesulfonyl compounds corresponding to Formula I: 1
Type:
Application
Filed:
April 16, 2002
Publication date:
February 13, 2003
Applicant:
Pharmacia Corporation
Inventors:
David L. Brown, Matthew J. Graneto, Cindy L. Ludwig, John M. Molyneaux, John J. Talley
Abstract: This invention relates to the novel use of dianilino squarates in the treatment of disease states mediated by the chemokine, Interteukin-8 (IL-8).
Type:
Application
Filed:
August 30, 2002
Publication date:
February 13, 2003
Inventors:
Michael R. Palovich, Joseph Weinstock, Katherine L. Widdowson
Abstract: This invention provides an amido ligand and its synthesis. Use of the amide ligand in a variety of metal complexes, and transition metals in particular, is also provided.
Type:
Application
Filed:
April 2, 2002
Publication date:
February 13, 2003
Inventors:
Jonas C. Peters, Steven D. Brown, Seth B. Harkins
Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the formula 1
Type:
Application
Filed:
June 18, 2001
Publication date:
February 6, 2003
Inventors:
Michael A. Walker, Timothy D. Johnson, Nicholas A. Meanwell, Jacque Banville
Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: 1
Type:
Application
Filed:
August 6, 2001
Publication date:
January 9, 2003
Applicant:
Aventis CropScience S.A.
Inventors:
Vincent Gerusz, Darren James Mansfield, Jose Perez, David Tickle, Jean-Pierre Vors, Derek Baldwin, Thomas Lawley Hough, Dale Robert Mitchell
Abstract: A novel process is provided for the preparation of optionally protected 2,5-di-(3′-aminopropyl)-pyridines which are useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
Type:
Application
Filed:
June 5, 2002
Publication date:
January 2, 2003
Inventors:
Nobuyoshi Yasuda, Michael Palucki, Yi Xiao, Frederick W. Hartner, Lushi Tan
Abstract: The present invention provides methods of synthesizing and screening inhibitors of bacterial NAD synthetase enzyme, compounds thereof, and methods of treating bacterial and microbial infections with inhibitors of bacterial NAD synthetase enzyme.
Type:
Grant
Filed:
July 14, 2000
Date of Patent:
December 31, 2002
Assignee:
University of Alabama Research Foundation
Inventors:
Wayne J. Brouillette, Donald Muccio, Mark J. Jedrzejas, Christie G. Brouillette, Yancho Devedjiev, Walter Cristofoli, Lawrence J. DeLucas, Jose Gabriel Garcia, Laurent Schmitt, Sadanandan E. Velu
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: Novel polydentate asymmetric nitrogen-oxygen-containing binaphthyl derivatives of the formulae (I) and (II), and metal complexes of these compounds may be used as catalysts for enantioselective transformations.
Type:
Application
Filed:
May 2, 2002
Publication date:
December 12, 2002
Applicant:
DEGUSSA AG
Inventors:
Axel Monsees, Carsten A. Schneider, Thomas Riermeier, Uwe Dingerdissen
Abstract: A method for making an indole compound includes transition metal-catalyzed arylation of a hydrazone to form an aryl hydrazone, hydrolysis of the aryl hydrazone to form an aryl hydrazine, and acid catalyzed cyclization of the aryl hydrazine to form the indole compound.
Type:
Grant
Filed:
June 21, 2002
Date of Patent:
December 3, 2002
Assignee:
Rhodia Chirex Inc.
Inventors:
Frederick Hicks, Da-Ming Gou, Salvatore Anthony Marchese, Lawrence J. Martel, Atena Necula, Richard E. Benetti, Richard A. Silva
Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine 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.
Type:
Application
Filed:
November 14, 2001
Publication date:
November 7, 2002
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine 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.
Type:
Application
Filed:
November 14, 2001
Publication date:
November 7, 2002
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: A method for producing an aromatic primary amine, characterized by hydrogenating an aromatic nitrile at a low partial pressure of hydrogen in a heterogeneous system comprising a non-reductive polar solvent and a nickel-immobilized catalyst suspended therein was proposed. By such method, an aromatic primary amine which is industrially useful as a medicine, agricultural chemical, dye surfactant, chemical agent, etc. can be produced in a high yield.
Abstract: The compounds represented by the formula (I), and pharmacologically acceptable salts and solvates thereof are disclosed. The compound is hydrolyzed in organisms into a compound represented by the formula in which W represents a hydrogen atom, and D represents the group —V—(CH2)p—COOR, wherein R represents a hydrogen atom. The compound inhibits the aggregation of platelets via the inhibition of the linkage of the platelet membrane protein GPIIb/IIIa to fibrinogen.
wherein A represents CH2 or CO, B represents the group —(CH2)k— or —(CH2)m—CO—, X and Y are different from each other and represent N or CH, W represents an ester moiety which can be removed under the physiological condition, and Z represents the groups (II) or (III):
wherein D represents the group —V—(CH2)p—COOR.
Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof:
wherein R1, R2 and R3 are various substituent groups; and
one of X1 and X2 is N or CR′, and the other is NR′ or CHR′ wherein R′ is hydrogen, OH, C1-6alkyl, or C3-7cycloalkyl; or when one of X1 and X2 is N or CR′ then the other may be S or O;
and their use as pharmaceuticals.
Abstract: New p-diaminobenzene derivative compounds of formula (I), or their physiologically compatible salts, are disclosed:
Compositions for oxidatively dyeing keratin fibers, especially human hair, that contain the p-diaminobenzene derivative compounds of formula (I), as well as a suitable coupler substance, are also disclosed.
Inventors:
Chunjian Liu, T.G. Murali Dhar, Henry H. Gu, Edwin J. Iwanowicz, Katerina Leftheris, William J. Pitts, Timothy F. Herpin, Zulan Pi, Gregory S. Bisacchi
Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine 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. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
Type:
Grant
Filed:
November 23, 2001
Date of Patent:
October 1, 2002
Assignee:
G.D. Searle & Co.
Inventors:
James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
Abstract: Amidomethyl esters, carbonylmercaptomethyl esters, keto-containing esters, amidomethyl thioesters, amidomethyl amides, and methylene dithioesters are disclosed. The novel compounds have two carbonyl groups connected by a linking moiety having an oxygen, sulfur or nitrogen attached to a methylene group, to which is further attached a sulfur, nitrogen or CH2 group. Methods of treating illnesses and conditions, such as cancer, hemological disorders, inherited metabolic disorders and others, using these compounds are also disclosed.
Type:
Application
Filed:
May 17, 2001
Publication date:
September 26, 2002
Inventors:
Hsuan-Yin Lan-Hargest, Norbert L. Wiech
Abstract: Pharmaceutical compositions incorporate aryl substituted olefinic amine compounds. Representative compounds are (2S)-(4E)-N-methyl-5-[3-(5-isopropoxy-1-oxopyridin)yl)]-4-penten-2-amine, (4E)-N-methyl-5-(3-(1-oxopyridin)yl)-4-penten-2-amine, (4E)-N-methyl-5-(3-(5-((carboxymethyl)oxy)pyridin)yl)-4-penten-2-amine and (4E)-N-methyl-5-(3-(1-oxopyridin)yl)-4-penten-2-amine.
Type:
Grant
Filed:
May 12, 2000
Date of Patent:
September 24, 2002
Assignee:
Targacept, Inc.
Inventors:
Gary Maurice Dull, Craig Harrison Miller, William Scott Caldwell, Dwo Lynm, Balwinder Singh Bhatti, Jeffrey Daniel Schmitt, Gary Dwight Byrd
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: Described are compounds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is S02; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y=SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g.
Inventors:
Karl-Heinz Altmann, Guido Bold, Pascal Furet, Paul William Manley, Jeanette Marjorie Wood, Stefano Ferrari, Francesco Hofmann, Jürgen Mestan, Andreas Huth, Martin Krüger, Dieter Seidelmann, Andreas Menrad, Martin Haberey, Karl-Heinz Thierauch
Abstract: Oxime compounds of formula (1)
wherein R1, R2, and R3 are independently halogen, C1-C3 alkyl, C1-C3 halolalkyl, C1-C3 alkoxy, C1-C3 haloalkoxy, nitro, or cyano; R4 is 3,3-dihalogeno-2-propenyl; a is an integer of 0 to 2; Y is oxygen, sulfur, or NH; Z is oxygen, sulfur, or NR5 wherein R5 is hydrogen, acetyl, or C1-C3 alkyl; and X is of formula (2)
insecticidal/acaricidal agents containing them as active ingredients; and intermediates for their production.