Chalcogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding [e.g., 1-(2-hydroxyethyl)-3-amino-4(para-chlorophenyl)-pyrazole, Etc.] Patents (Class 548/372.5)
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. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral heteroaryl aminoalcohols.
Type:
Grant
Filed:
December 12, 2001
Date of Patent:
January 13, 2004
Assignee:
Pharmacia Corporation
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: There is provided compounds of formula IA and of formula IB,
wherein R1, R2, R3, R4 and A have meanings given in the description, which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
Type:
Grant
Filed:
October 22, 1999
Date of Patent:
December 30, 2003
Assignee:
Pfizer Inc
Inventors:
Mark Edward Bunnage, John Paul Mathias, Stephen Derek Albert Street, Anthony Wood
Abstract: The invention concerns novel pyrazole derivatives comprising at least a cationic group Z, Z being selected among the quaternized aliphatic chains, aliphatic chains comprising at least a saturated quaternized cycle, and aliphatic chains comprising at least an unsaturated quaternized cycle, their use as oxidation base for dyeing keratin fibres, dyeing compositions containing them, and dyeing methods using them.
Abstract: The invention relates to novel compositions for the oxidation dyeing of keratin fibers, comprising at least one specific diaminopyrazole derivative, to the dyeing process using this composition, to novel diaminopyrazole derivatives and to a process for their preparation.
Type:
Grant
Filed:
October 18, 2001
Date of Patent:
November 11, 2003
Assignee:
L'Oreal, S.A.
Inventors:
Laurent Vidal, Agnès Burande, Gérard Malle, Michel Hocquaux
Abstract: Compounds of the formula
where the variables have the meaning defined in the specification, which bind specifically or selectively to to RAR&agr; retinoid receptors.
Type:
Grant
Filed:
September 19, 2002
Date of Patent:
September 16, 2003
Assignee:
Allergan, Inc.
Inventors:
Tien T. Duong, Richard Beard, Roshantha A. Chandraratna
Abstract: Disclosed is a process for forming an N-acylamino pyrazole comprising contacting a N-acyl-3-oxo-imino ether compound either with a salt of hydrazine in the presence of a base or with hydrazine.
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-heteroaryl-N-phenyl aminoalcohols.
Type:
Grant
Filed:
November 14, 2001
Date of Patent:
July 1, 2003
Assignee:
Pharmacia Corporation
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: This invention relates to compounds which are IP receptor antagonists and which are represented by Formula (I):
wherein G2 is a heteroaryl group containing one or two nitrogen atoms substituted with a carboxylic acid group, said heteroaryl ring containing one or two nitrogen atoms, and G1 is as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
Type:
Grant
Filed:
March 1, 2002
Date of Patent:
May 27, 2003
Assignee:
Roćhe Palo Alto LLC
Inventors:
Francisco Javier Lopez-Tapia, Dov Nitzan, Counde O'Yang
Abstract: Amino pyrazole derivatives of the formula:
which are ligands for the neuropeptide Y, subtype 5 receptor and pharmaceutical compositions containing an amino pyrazole derivative as the active ingredient are described. The amino pyrazole derivatives are useful in the treatment of disorders and diseases associated with the NPY receptor subtype Y5.
Type:
Grant
Filed:
February 22, 2001
Date of Patent:
March 11, 2003
Inventors:
Cheryl P. Kordik, Scott L. Dax, Chi Luo, Allen B. Reitz, James J. McNally, Timothy W. Lovenberg
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: Disclosed is an improved process for the preparation of 4,5-diamino-1-(2′-hydroxyethyl)pyrazole and acid addition salts thereof such as the addition salt from sulfuric acid. The process comprises a novel combination of steps beginning with an alkyl(alkoxymethylene)cyanoacetate and 2-hydroxyethylhydrazine and the formation of intermediate compounds 5-amino-4-alkoxycarbonyl-1-(2′-hydroxyethyl)pyrazole (I), 5-amino-4-carboxyl-1-(2′-hydroxyethyl)pyrazole (II), 5-amino-1-(2′-hydroxyethyl)pyrazole (III), 5-amino-1-(2′-hydroxyethyl)4-nitrosopyrazole (IV).
Abstract: A method of controlling a plant disease caused by a fungus comprising applying a 5-amino-pyrazole of the formula
wherein,
R1, R2, R3, R4, R5 and Y are as defined in the specification.
Type:
Grant
Filed:
February 20, 2001
Date of Patent:
September 3, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Markus Heil, Thomas Bretschneider, Hans-Christian Militzer, Astrid Mauler-Machnik, Klaus Stenzel
Abstract: The present invention provides compounds having useful antibacterial activity and pharmaceutical compositions comprising one or more of these compounds. The invention further relates to a method of treating a bacterial infection in a patient, comprising administering to the patient an effective mount of one or more of the antibacterial compounds of the invention.
Type:
Grant
Filed:
February 10, 2000
Date of Patent:
June 25, 2002
Assignee:
Genzyme Corporation
Inventors:
Bradford H. Hirth, Andrew Janjigian, Fred Vinick
Abstract: The present invention relates to certain pyrazole derivatives of Formula (I):
that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
Type:
Grant
Filed:
May 5, 1999
Date of Patent:
April 23, 2002
Assignee:
Syntex (U.S.A.) LLC
Inventors:
David Michael Goldstein, Sharada Shenvi Labadie, David Mark Rotstein, Eric Brian Sjogren, Francisco Xavier Talamas
Abstract: N-Phenylpyrazole derivatives of the formula:
wherein
R1 represents optionally halogenated alkyl;
R2 represents halogen, cyano, nitro, cycloalkyl, alkenyl, thiocyanato, optionally alkyl substituted sulphamoyl, optionally alkyl substituted carbamoyl, alkoxycarbonyl, alkanoyl or optionally halogenated alkyl; and R3 represents a hydrogen atom or a group N″R′″ or a variety of other groupings. These compounds possess arthropodicidal, plant nematocidal, anthelmintic and anti-protozoal properties; their preparation, compositions containing them and their use are described.
Type:
Grant
Filed:
July 16, 1999
Date of Patent:
April 16, 2002
Assignee:
Rhone-Poulenc Agriculture Ltd.
Inventors:
Leslie Roy Hatton, Ian George Buntain, David William Hawkins, Edgar William Parnell, Christopher John Pearson, David Alan Roberts
Abstract: Parasiticidal pyrazole derivatives of formula (I) wherein: R1 represents CN, C1-6 alkoxycarbonyl, NO2, CHO, C1-6 alkanoyl, phenyl optionally substituted by one or more halogen, or C1-6 alkyl optionally substituted by one or more halogen; R2 represents a group of formula (II), (III) or (IV) in which: R7 represents H, halogen, carbamoyl, cyano, tri(C1-6 alkyl)silyl, C1-6 alkyl (optionally substituted by one or more halogen, OH or C1-6 alkoxy), C1-6 alkoxycarbonyl, phenyl, or a 5- or 6-membered ring heterocycle which is saturated or partially or fully unsaturated and contains up to 4 hetero-atoms independently selected from up to 4 N atoms, up to 2 O atoms and up to 2 S atoms and which is attached to the alkynyl moiety by an available C, S or N atom where the valence allows; and R8, R9 and R10 each independently represents H, halogen, phenyl optionally substituted by one or more halogen, CN or C1-6 alkyl optionally substituted by one or more halogen; R3 represents H, C1-6 alkyl, halogen, NH2, NH(C1-6 alkanoyl),
Abstract: A 5-aminopyrazole-4-carboxylate derivative represented by the formula (1) is prepared by reacting a compound represented by the formula (2) with a hydrazine compound represented by the formula (3) or hydrate, hydrochloride, hydrobromide or sulfate of the same according to the reaction formula (C):
wherein R1 is a straight or branched C1 to C4 alkyl group which can be substituted with a halogen atom, R2 is a hydrogen atom, straight or branched C1 to C4 alkyl group or an unsubstituted or substituted phenyl group, and R3 is a straight or branched C1 to C4 alkyl group, and M is an alkali metal.
The 5-aminopyrazole-4-carboxylate derivative obtained by the preparation process of the invention is useful for an intermediate of agricultural chemicals and medicines, fungicides in particular.
Abstract: Compounds which are 3-amino-pyrazole derivatives represented by formula (I):
where
R is a C3-C6 cycloalkyl group, which may optionally be substituted by a straight or branched C1-C6 alkyl group, and
R1 is a straight or branched C1-C6 alkyl group or a C2-C4 alkenyl, cycloalkyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl and arylalkenyl, which may be optionally substituted; or a pharmaceutically acceptable salt thereof.
The compounds are useful for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
Inventors:
Paolo Pevarello, Paolo Orsini, Gabriella Traquandi, Mario Varasi, Edward L. Fritzen, Martha A. Warpehoski, Betsy S. Pierce, Maria Gabriella Brasca
Abstract: The present invention relates to a compound represented by the general formula [I]:
wherein Ar1 represents an aryl or heteroaryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino, acyl and aryl groups; Ar2 represents an aryl or heteroaryl group which may have a substituent selected from the group consisting of a halogen atom and lower alkyl, lower alkenyl, lower haloalkyl, lower alkoxy, lower alkylthio, lower alkylamino, lower dialkylamino and aryl groups; n is zero, 1 or 2; and R1 and R2 may be the same or different and each represents a hydrogen atom or a lower alkyl group, or its salt, a method for its preparation as well as an agent for the treatment of bulimia, obesity or diabetes comprising it as an active ingredient.