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)
  • Patent number: 6677341
    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
  • Patent number: 6670366
    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
  • Patent number: 6660046
    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.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: December 9, 2003
    Assignee: L'Oreal S.A.
    Inventors: Eric Terranova, Alain Lagrange
  • Patent number: 6645258
    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
  • Patent number: 6620963
    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
  • Patent number: 6593477
    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.
    Type: Grant
    Filed: October 29, 2002
    Date of Patent: July 15, 2003
    Assignee: Eastman Kodak Company
    Inventors: Robert F. Romanet, Susan M. Fischer
  • Patent number: 6586433
    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
  • Patent number: 6569860
    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
  • Patent number: 6531478
    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
  • Patent number: 6458803
    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
  • Patent number: 6452019
    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).
    Type: Grant
    Filed: February 22, 2002
    Date of Patent: September 17, 2002
    Assignee: Eastman Chemical Company
    Inventor: Phillip Michael Cook
  • Patent number: 6444612
    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
  • Patent number: 6410533
    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
  • Patent number: 6376527
    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
  • Patent number: 6372774
    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
  • Patent number: 6255333
    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),
    Type: Grant
    Filed: February 11, 1998
    Date of Patent: July 3, 2001
    Assignee: Pfizer Inc.
    Inventor: Bernard Joseph Banks
  • Patent number: 6235911
    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.
    Type: Grant
    Filed: May 30, 2000
    Date of Patent: May 22, 2001
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Kei Yoshida, Shingo Matsuo, Toshio Kitashima, Kanji Tomiya, Kenji Kodaka
  • Patent number: 6218418
    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.
    Type: Grant
    Filed: September 22, 2000
    Date of Patent: April 17, 2001
    Assignees: Pharmacia & Upjohn S.p.A, Pharmacia & Upjohn Co.
    Inventors: Paolo Pevarello, Paolo Orsini, Gabriella Traquandi, Mario Varasi, Edward L. Fritzen, Martha A. Warpehoski, Betsy S. Pierce, Maria Gabriella Brasca
  • Patent number: 6180653
    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.
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: January 30, 2001
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takehiro Fukami, Takahiro Fukuroda, Akio Kanatani, Masaki Ihara