Abstract: Levosimendan, or (-)-[[4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl]hydrazono]propanedinitrile, which has been previously suggested for the treatment of congestive heart failure is useful in the treatment of septic shock.
Type:
Application
Filed:
March 24, 2003
Publication date:
August 21, 2003
Inventors:
Anders Oldner, Michael Wanecek, Eddie Weitzberg, Anders Rudehill
Abstract: The invention relates to 2-phenyl-2H-pyridazin-3-ones of the general formula I 1
Type:
Application
Filed:
October 10, 2002
Publication date:
July 10, 2003
Inventors:
Michael Puhl, Thorsten Volk, Gerhard Hamprecht, Robert Reinhard, Ingo Sagasser, Cyrill Zagar, Karl-Otto Westphalen, Matthias Witschel, Helmut Walter
Abstract: The present invention describes pyridazinone compounds which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti inflammatory drugs (NSAIDs).
Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Type:
Application
Filed:
May 10, 2002
Publication date:
May 22, 2003
Inventors:
Jeremy Green, Scott L. Harbeson, John E. Cochran
Abstract: Zwitterionic imide compounds are provided according to the formula: R1—SO2—N−—SO2—R2+, where R1 and R2+are any suitable groups. Typically R1 is a highly fluorinated alkane and R2+contains a quaternary ammonium group or a heteroatomic aromatic group having an cationic nitrogen, such as: pyridiniumyl, pyridaziniumyl, pyrimidiniumyl, pyraziniumyl, imidazoliumyl, pyrazoliumyl, thiazoliumyl, oxazoliumyl, or triazoliumyl. Zwitterionic liquids are provided, typically having melting points of less than 100 ° C. and typically having a solubility in water of less than 5% by weight.
Abstract: Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
Type:
Application
Filed:
April 15, 2002
Publication date:
May 8, 2003
Applicant:
Tularik Inc.
Inventors:
Jonathan B. Houze, Lawrence R. McGee, Steven Marc Rubenstein
Abstract: Hepatic cirrhosis and fibrosis and fatty liver can be prevented and treated by administering to a subject in need thereof an effective amount of at least one adenosine A2A receptor antagonist or at least one adenosine uptake promotor.
Abstract: The invention relates to novel phenylpyridazinones of the general formula (I)
in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to processes for their preparation, to their use as herbicides and to novel intermediates and processes for preparing them.
Type:
Grant
Filed:
November 26, 1997
Date of Patent:
April 22, 2003
Assignee:
Bayer Aktiengesellschaft
Inventors:
Karl-Heinz Linker, Kurt Findeisen, Wilhelm Haas, Markus Dollinger, Hans-Joachim Santel
Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women.
Type:
Application
Filed:
August 2, 2002
Publication date:
April 17, 2003
Applicant:
Neurocrine Biosciences, Inc.
Inventors:
Chen Chen, Dongpei Wu, Zhiqiang Guo, Martin Rowbottom
Abstract: A photographic processing composition for silver halide color photographic lightsensitive material, comprising at least one compound represented by the formula (I):
Abstract: There are described cycloalkyl derivatives of the formula (I)
Type:
Application
Filed:
May 10, 2002
Publication date:
March 13, 2003
Applicant:
Aventis Pharma S.A.
Inventors:
Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
Abstract: The present invention describes pyridazione compounds having the formula (I), which are cyclooxygenase (COX) inhibitors The compounds are selective inhibitors of cyclooxygenase-2-(COX-2), which is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1), which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDS).
Abstract: Corticotropin releasing factor (CRF) antagonists of formula I:
and their use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.
Type:
Grant
Filed:
August 9, 2000
Date of Patent:
February 11, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
Paul Joseph Gilligan, Rajagopal Bakthavatchalam
Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I):
(wherein R is a C2-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group or the like, B0 to B2 and B3 are hydrogen atoms, halogen atoms, cyano groups, C1-C4 haloalkyl groups or the like, n is 0, 1 or 2, and Ar is a phenyl ring, a pyridine ring, a thiophene ring, a pyrazole ring or the like), and insecticides and miticides containing the 3-arylphenyl sulfide derivatives as an active ingredient.
Type:
Grant
Filed:
October 27, 2000
Date of Patent:
January 21, 2003
Assignees:
Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
Abstract: This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of these compounds for the treatment of feeding disorders such as obesity, anorexia nervosa, bulimia nervosa, and abnormal conditions such as sexual/reproductive disorders, depression, epileptic seizure, hypertension, cerebral hemorrhage, congestive heart failure or sleep disturbances and for the treatment of any disease in which antagonism of a Y5 receptor may be useful.
Type:
Application
Filed:
April 2, 2002
Publication date:
January 16, 2003
Applicant:
Synaptic Pharmaceutical Corporation
Inventors:
Imadul Islam, Daljit S. Dhanoa, John M. Finn, Ping Du, Charles Gluchowski, Yoon T. Jeon
Abstract: This invention relates to novel sulfonyl pyridazinone compounds useful as aldose reductase inhibitors in the treatment or prevention of certain complications arising from diabetes mellitus, pharmaceutical compositions comprising the sulfonyl pyridazinone, pharmaceutical compositions comprising a combination of the sulfonyl pyridazinone together with a second pharmaceutical agent, therapeutic methods comprising the administration of the sulfonyl pyridazinone compounds, therapeutic methods comprising the administration of the sulfonyl pyridazinone compounds in combination with a second pharmaceutical agent and compounds useful as intermediates for preparing the sulfonyl pyridazinone compounds of this invention.
Abstract: A pyridazin-3-on derivative of the formula (1):
in which R2 is a hydrogen atom or a C1-C3 alkyl group, R3 is a hydrogen atom or a C1-C3 alkyl group, and Q is an optionally substituted phenyl group can be prepared at a high yield and high purity by ring closing a carboxylic acid derivative of the formula (2):
in which R2, R3 and Q are the same as defined above, or its salt in the presence of a nitrogen-containing aromatic compound and a boron compound.
Type:
Grant
Filed:
June 28, 2001
Date of Patent:
December 31, 2002
Assignee:
Sumitomo Chemical Company, Limited
Inventors:
Masao Yanagawa, Masahiko Mizuno, Yoshiaki Oda
Abstract: Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.
Type:
Grant
Filed:
November 16, 2000
Date of Patent:
December 10, 2002
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Steffen Breitfelder, Pier F. Cirillo, Ming-Hong Hao, Eugene R. Hickey, Rajiv Sharma, Sanxing Sun, Hidenori Takahashi
Abstract: A compound selected from those of formula (I):
wherein:
R1 and R2 each independently represent hydrogen or, alkyl,
T1 and T2 each independently represent alkylene,
G represents a heterocyclic group selected of formula (&agr;):
wherein:
W1 to W5 and X1 to X4 are so defined in the description.
Medicinal products containing the same are useful as serotonin-reuptake inhibitors.
Type:
Grant
Filed:
October 11, 2000
Date of Patent:
December 10, 2002
Assignee:
Les Laboratoires Servier
Inventors:
Gilbert Lavielle, Olivier Muller, Mark Millan, Didier Cussac, Anne Dekeyne
Abstract: Compounds of the formula I and their salts, as defined in claim 1, are suitable as safeners for protecting crop plants against the phytotoxic side-effects of herbicides.
Type:
Grant
Filed:
January 29, 1998
Date of Patent:
November 19, 2002
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Xenia Holdgrün, Lothar Willms, Klaus Bauer, Klaus Trinks, Hermann Bieringer
Abstract: This invention provides pyridazinone derivatives encompassed by the following the formula:
wherein, R1, R2, R3, R4, R5 and R7 represent a hydrogen atom and the like, and R6 represents a C1-C3 alkyl and the like. The pyridazinone derivatives have excellent herbicidal activity, therefore, they can be used as an active ingredient for herbicidal compositions and can be utilized in herbicidal method, which are also described.
Abstract: The invention relates to compounds represented by the following general formula (1):
wherein A is an aromatic compound which may be substituted, or the like, B is a nitrogen atom or CH, X is a lower alkylene group which may be substituted, or the like, Y is a single bond or the like; Z is a divalent residue of benzene which may be substituted, or the like, and m and n are independently an integer of 1 to 4, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.
Abstract: This invention relates to pyridazine derivatives represented by the formula (1):
wherein R1 represents a lower alkoxyl group, a lower alkylthio group or a halogen atom; R2 represents H, a lower alkoxyl group, a lower alkylthio group or a halogen atom; R3 represents a lower alkyl or lower alkenyl group, which may be substituted by one or more OHs, CNs, lower cycloalkyl groups, (substituted) aromatic groups or (substituted) carbamoyl groups; R4 represents COOH, a lower alkoxycarbonyl group, a (substituted) carbamoyl group, a (substituted) amino group, or a (substituted) ureido group; and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients.
Abstract: Aralkylpyridazinone derivatives of the formula I
and their physiologically acceptable salts in which
R1, R2, R3, R4, R5 and Q have the meanings indicated in claim 1, show inhibition of phosphodiesterase IV and can be employed for the treatment of inflammatory processes and of allergies, asthma and autoimmune disorders.
Type:
Grant
Filed:
April 19, 1996
Date of Patent:
June 4, 2002
Assignee:
Merck Patent Gesellschaft mit beschraenkter Haftung
Inventors:
Rochus Jonas, Michael Wolf, Norbert Beier
Abstract: This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
Type:
Application
Filed:
April 26, 2001
Publication date:
May 2, 2002
Inventors:
Nancy Elisabeth Krauss, Taraneh Mirzadegan, David Bernard Smith, Keith Adrian Walker
Abstract: The invention relates to a method to inhibit bacteria from adhering to a submergible surface. The method contacts the submergible surface with an effective amount of at least one sulfamic acid or salt thereof to inhibit bacterial adhesion to the submergible surface. The invention also relates to a method for controlling biofouling of an aqueous system. This method adds an effective amount of at least one sulfamic acid or salt thereof to inhibit bacteria from adhering to a submerged surface within the aqueous system. This method effectively controls biofouling without substantially killing the fouling organisms. The sulfamic acid used in the method of the invention has the formula R1R2NS(O)2(OH). In this formula, R1 and R2 are independently a hydrogen, a C4-C20 alkyl group or a cyclohexyl group. However, R1 and R 2 are not both hydrogen.
Type:
Grant
Filed:
June 12, 2000
Date of Patent:
April 30, 2002
Inventors:
Thomas E. McNeel, Marilyn S. Whittemore, Stephen D. Bryant, Graciela H. Vunk
Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
Type:
Grant
Filed:
August 29, 2000
Date of Patent:
April 9, 2002
Assignee:
Allergan Sales, Inc.
Inventors:
Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
Abstract: Compounds of formula I useful for inhibiting the pain enhancing effects of E-type prostaglandins are disclosed
wherein A is a ring system in which the —CH(R3)N(R2)B—R1 and —OR4 groups are positioned in a 1,2 relationship to one another on ring carbon atoms. B is a ring system having R1 in a 1,3 or 1,4 relationship with the —CH(R1)N(R2)— linking group. A, B, R1, R2, R3 and R4 are as defined in the specification and may be substituted. Also disclosed are pharmaceutically-acceptable salts, in vivo-hydrolysable esters and amides of compounds of formula I, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and the use of such compounds as therapeutic agents.
Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
Type:
Grant
Filed:
May 13, 1999
Date of Patent:
April 2, 2002
Inventors:
Matthew E. Voss, Carl P. Decicco, Ruth R. Wexler
Abstract: A composition for oral administration comprising a substantially pure crystalline polymorphic form (I) of levosimendan as an active ingredient together with a pharmaceutically acceptable carrier is described. Polymorphic form (I) of levosimendan is rapidly absorbed from the gastrointestinal tract and is useful in the treatment of congestive heart disease.
Type:
Grant
Filed:
June 8, 2000
Date of Patent:
March 12, 2002
Assignee:
Orion Corporation
Inventors:
Maarit Backman, Ilkka Larma, Saila Antila, Lasse Lehtonen
Abstract: The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.
Type:
Application
Filed:
April 17, 2001
Publication date:
March 7, 2002
Inventors:
Yong-Qian Wu, Wei Huang, Gregory S. Hamilton
Abstract: The present invention describes pyridazinone compounds of formula I 1
Type:
Application
Filed:
May 31, 2001
Publication date:
March 7, 2002
Inventors:
Lawrence A. Black, Anwer Basha, Teodozyj Kolasa, Michael E. Kort, Huaqing Liu, Catherine M. McCarty, Meena Patel, Jeffrey J. Rohde, Michael J. Coghlan, Andrew O. Stewart
Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
February 5, 2001
Publication date:
February 28, 2002
Inventors:
Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe