Abstract: The present invention relates to 5-Aryltetrazole Compounds, compositions comprising an effective amount of a a 5-Aryltetrazole Compound, and methods for treating an inflammation disease, a reperfusion disease, or hyperuricemia in an animal in need thereof comprising administering to the animal an effective amount of a 5-Aryltetrazole compound.
Type:
Application
Filed:
July 17, 2003
Publication date:
June 17, 2004
Inventors:
Alex Nivorozhkin, John Van Duzer, Andrew Salzman, Garry Southan, Siya Ram, Qi Zeng, Csaba Szabo
Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.
Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I
in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.
Abstract: The present invention relates to 5-Aryltetrazole compounds, compositions comprising a 5-Aryltetrazole compound, and methods for treating an inflammation disease, a reperfusion disease, hyperuricemia, gout, or tumor-lysis syndrome in an animal in need thereof comprising administering to the animal an effective amount of a 5-Aryltetrazole compound.
Type:
Application
Filed:
July 18, 2002
Publication date:
January 29, 2004
Inventors:
Alex Nivorozhkin, John Van Duzer, Andrew Salzman, Garry Southan, Siya Ram, Qi Zeng, Csaba Szabo
Abstract: The present invention provides an agent for inhibiting cytokine production or cell adhesion, comprising at least one compound selected from the group consisting of thiazole derivatives represented by the following general formula: 1
Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R represents hydrogen, C1-10alkyl, haloC1-10alkyl or aryl; which are useful intermediates in the preparation of morpholine derivatives of formula (A). Compounds of formula (A) are useful as therapeutic agents.
Abstract: Substituted heterocycles of the general structural formula:
are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
Type:
Grant
Filed:
April 17, 2001
Date of Patent:
October 28, 2003
Assignee:
Merck & Co. Inc.
Inventors:
Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
Abstract: The present application describes disubstituted pyrazolines and triazolines of formulae I and II:
or pharmaceutically acceptable salt forms thereof, wherein one of M1 and M2 maybe N and D may be a variety of N-containing groups, which are useful as inhibitors of factor Xa.
Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
Abstract: The present invention discloses disubstiuted 4-oxo-1,4-dihydro-3-quinolinecarboxamide derivatives. The compounds are useful as antiviral agents, in particular, as agents against viruses of the herpes family.
Type:
Grant
Filed:
February 27, 2002
Date of Patent:
April 8, 2003
Assignee:
Pharmacia & Upjohn Company
Inventors:
Valerie A. Vaillancourt, Joseph Walter Strohbach, Audris Huang
Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3- (S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
Abstract: 1-(4-aminophenyl)pyrazoles optionally substituted on the 3- and 5-positions of the pyrazole ring and on the amino group at the 4-position of the phenyl ring are disclosed and described, which pyrazoles inhibit IL-2 production in T-lymphocytes.
Type:
Grant
Filed:
June 3, 1999
Date of Patent:
January 14, 2003
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Rajashekhar Betageri, Charles L. Cywin, Karl Hargrave, Mary Ann Hoermann, Thomas M. Kirrane, Thomas M. Parks, Usha R. Patel, John R. Proudfoot, Rajiv Sharma, Sanxing Sun, Xiao-Jun Wang
Abstract: A silver halide color photographic lightsensitive material contains a coupler represented by formula (I) below in at least one layer on a support (in this formula, X represents a hydrogen atom or a group which can split off by a coupling reaction with an oxidized form of an aromatic primary amine color developing agent, each of R1 and R2 represents an electron-attracting group having a Hammett's substituent constant p value of 0.20 or more, and the sum of the p values of R1 and R2 is 0.65 or more, and each of G1 and G2 represents a nitrogen atom or a substituent). A pyrrolotriazole compound represented by formula (I) below is also provided.
Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.
Type:
Application
Filed:
November 16, 2001
Publication date:
December 12, 2002
Inventors:
Carsten Behrens, Jesper Lau, Peter Madsen
Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.
Type:
Application
Filed:
March 27, 2002
Publication date:
November 28, 2002
Inventors:
Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, David Lee Varie
Abstract: The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacylic compounds. The present invention relates in particular to five-membered heteroaromatic olefinic azacyclic compounds and five-membered heteroaromatic acetylenic azacylic compounds, including isoxazolyl olefinic cycloalkylamines and isoxazolyl acetylenic cycloalkylamines.
Abstract: The use is described of 3,5-diphenyl-1,2,4-triazoles of the formula I
in which R1-R5 are as defined in the description. The compounds have useful pharmaceutical properties and are particularly active as iron chelators. They can be used for the treatment of iron overload in warm-blooded animals.
Abstract: This invention is concerned with a novel polymorphic forms of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethyl-amino)methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic forms have advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethylamino)methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
Abstract: The invention provides certain 1,2,4-triazole-3-thione compounds, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Application
Filed:
December 10, 2001
Publication date:
July 4, 2002
Applicant:
AstraZeneca AB
Inventors:
Andrew Baxter, Colin Bennion, Peter Cage, Nicholas Kindon, Michael Mortimore, Bryan Roberts
Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.
Abstract: The present invention provides compounds of formula (I): 1
Type:
Application
Filed:
June 22, 2001
Publication date:
May 23, 2002
Inventors:
Christopher John Urch, Terence Lewis, Raymond Leo Sunley, Roger Salmon, Christopher Richard Ayles Godfrey, Christopher Ian Brightwell, Matthew Brian Hotson
Abstract: There is disclosed a 1H-pyrrolo-[1,2-b][1,2,4]triazole compound represented by formula (I):
wherein R is an alkyl group; R1, R2, R3, R1′, R2′, and R3′ each are a hydrogen atom or an alkyl group; R1 and R2, and R1′ and R2′ may bond together to form a ring, respectively; R4 is a hydrogen atom or an alkyl group, and X is heterocyclic group, a substituted amino group, or an aryl group. The compound is useful as a photographic cyan coupler. There is also disclosed synthetic intermediates of the compound and a production method of the intermediates.
Abstract: Compounds of formula I
are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NF&kgr;B is involved.
Type:
Grant
Filed:
June 22, 2000
Date of Patent:
March 19, 2002
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Olaf Ritzeler, Hans Ulrich Stilz, Bernhard Neises, William Jerome Bock, Jr., Armin Walser, Gary A. Flynn, Jörg Habermann, Gerhard Jähne
Abstract: 3-(Substituted aryl)-5-{substituted aryl-(alkynyl-aryl)}-[1,2,4]- triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.
Type:
Application
Filed:
April 13, 2001
Publication date:
February 14, 2002
Inventors:
Vidyadhar Babu Hegde, Scott Jerome Bis, Emilie Chassat Heo, Christopher Thomas Hamilton, Peter Lee Johnson, Laura Lee Karr, Timothy Patrick Martin, Paul Allen Neese, Nailah Orr, Francis Eugene Tisdell, Maurice Chee Hoong Yap, Yuanming Zhu
Abstract: Asymmetrical bisbenzotriazoles of the formula I
where G2′ is perfluoroalkyl of 1 to 12 carbon atoms, preferably CF3, and where G2 does not contain said group are red-shifted and due to the asymmetry are particularly soluble and useful in a host of applications including automotive coatings, thermoplastics and especially in adhesive compositions, themselves useful in solar panels and other laminate structures.
Abstract: New synthetic procedures for preparing insecticidal 3-(substituted phenyl)-5-(thienyl or furyl)-1,2,4-triazoles utilizing thioimidate intermediate.
Type:
Grant
Filed:
October 22, 1999
Date of Patent:
December 11, 2001
Assignee:
Dow AgroSciences LLC
Inventors:
Mary L. Ash, Mark W. Zettler, Norman R. Pearson, Duane R. Romer, John W. Hull, Jr., David E. Podhorez
Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,1-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
Abstract: The present invention relates to benzimidazole derivatives and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to the preparation of the benzimidazole derivatives and pharmaceutical formulations containing them.
Type:
Grant
Filed:
January 21, 2000
Date of Patent:
October 23, 2001
Assignee:
Glaxo Wellcome Inc.
Inventors:
Stanley Dawes Chamberlain, Jeffrey H. Tidwell
Abstract:
The present invention relates to a process for the preparation of mopholine derivatives of formula (I) which are useful as a therapeutic agents.
Type:
Grant
Filed:
December 15, 2000
Date of Patent:
October 2, 2001
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Ian Frank Cottrell, Ulf H Dolling, David Hands, Robert Darrin Wilson
Abstract: Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Abstract: Asymmetrical bis benzotriazoles of the formula I
where G2′ is perfluoroalkyl of 1 to 12 carbon atoms, preferably CF3, and where G2 does not contain said group are red-shifted and due to the asymmetry are particularly soluble and useful in a host of applications including automotive coatings, thermoplastics and especially in adhesive compositions, themselves useful in solar panels and other laminate structures.
Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.
Abstract: Benzotriazole UV absorbers which are substituted at the 5-position of the benzo ring by an electron withdrawing group exhibit enhanced durability and very low loss rates when incorporated into automotive coatings. This is particularly the case when the 3-position of the phenyl ring is also substituted by phenyl or phenylalkyl such as .alpha.-cumyl. Compounds where the 5-position of the benzo ring are substituted by perfluoroalkyl such as trifluoromethyl are particularly of interest for both their enhanced durability and for their excellent solubility and excellent color properties in some thermoplastic compositions when the phenyl ring is substituted at the 3-position by hydrogen or tert-alkyl.
Type:
Grant
Filed:
January 21, 1999
Date of Patent:
December 26, 2000
Assignee:
Ciba Specialty Chemicals Corporation
Inventors:
Ramanathan Ravichandran, Joseph Suhadolnik, Mervin G. Wood, Anthony Debellis, Robert E. Detlefsen, Revathi Iyengar, Jean-Pierre Wolf
Abstract: This invention is concerned with a novel polymorphic form of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)-phenyl)-ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic form has advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoro-methyl)-phenyl)ethoxy)-3-(S)-(4-fluoro)phe nyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.