Abstract: The invention concerns novel lipoic acid derivatives, which have an inhibiting action with respect to NO-synthase enzymes producing nitrogen monoxide NO and/or are agents enabling the regeneration of antioxidants or entities trapping reactive oxygen species (ROS) and intervening in a more general manner in the redox status of thiol groups. The invention also concerns methods for preparing them, pharmaceutical compositions containing them and their use for therapeutic purposes, particularly their use as NO-synthase inhibitors and/or as agents acting more generally in the redox status of thiol groups.
Type:
Application
Filed:
April 21, 2003
Publication date:
January 29, 2004
Applicant:
SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATION SCIENTIFIQUES (S.C.R.A.S)
Inventors:
Jeremiah Harnett, Michel Auguet, Pierre-Etienne Chabrier de Lassauhyere
Abstract: Provided herein are novel heteroaromatic substituted cyclopropanes of the Formula (I): 1
Type:
Application
Filed:
September 5, 2002
Publication date:
December 11, 2003
Inventors:
Andreas Termin, Peter D.J. Grootenhuis, Dean M. Wilson, Valentina Molteni, Long Mao, Angelo Castellino, Zhicai Yang, Anthony Pechulis, Mark Suto
Abstract: The present invention refers to a process for preparing indolinone derivatives of the general formula (VI) as defined in the specification and intermediates of that process.
Type:
Application
Filed:
February 14, 2003
Publication date:
December 11, 2003
Inventors:
Qingwu Jin, Michael A. Mauragis, Paul D. May
Abstract: The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of neurodegenerative disorders, diseases associated with polygultamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders renal hypoxia, hepatitis and AIDS. Said pyrrolidine derivatives display a modulatory and most notably a down-regulating-up to an inhibitory-activity with respect to the cellular death agonist Bax and/or the activation pathways leading to Bax and allows therefore to block the release of cytochrome (c).
Type:
Application
Filed:
April 28, 2003
Publication date:
September 11, 2003
Inventors:
Serge Halazy, Anna Quattropani, Agnes Bombrun, Mattias Schwarz, Russel Thomas, Anthony Baxter
Abstract: The invention relates to nitrofuran-containing compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making the compounds, and methods for identifying compounds with desired biological activity.
Type:
Application
Filed:
June 25, 2002
Publication date:
September 4, 2003
Inventors:
Paul J. Ala, Jacob J. Clement, Andrew S. Magee, Scott T. Moe, Manuel A. Navia, Aloka Roy
Abstract: Triazole compounds having a 2,6-disubstituted-phenyl group in the 3-position, arylthien-2- or -3-yl in the 5-position and an alkyl group in the 1-position are effective in controlling lepidoptera, coleoptera, mites and other sucking pests.
Type:
Application
Filed:
September 13, 2002
Publication date:
July 17, 2003
Inventors:
Vidyadhar Babu Hegde, Scott Jerome Bis, Maurice Chee Hoong Yap, Denise Marie Perreault, Francis Eugene Tisdell, Leonard Paul Dintenfass, James Edwin Dripps, James Michael Gifford, Katherine Anne Guenthenspberger, Laura Lee Karr, Joe Raymond Schoonover
Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives.
Type:
Application
Filed:
August 30, 2002
Publication date:
June 19, 2003
Inventors:
Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
Abstract: The invention relates to complexes of ruthenium of the structural formula I
where
X is an anionic ligand,
Z is a monodentate to tridentate ligand which contains a metal and is nonionically bound to the ruthenium center,
R1 and R2 are identical or different and are each hydrogen or/and a hydrocarbon group, but may also form a ring, and
Ligand L is an N-heterocyclic carbene, and also to a process for preparing acyclic olefins having two or more carbon atoms or/and cyclic olefins having three or more carbon atoms and the use of at least one complex of the formula I in olefin metathesis.
Type:
Grant
Filed:
January 20, 2000
Date of Patent:
April 22, 2003
Assignee:
Degussa AG
Inventors:
Wolfgang Anton Herrmann, Florian J. Kohl, Thomas Weskamp
Abstract: Novel compounds are provided having the structural formula R[—N(NO2)—L—R1]n wherein R, L, R1 and n are defined herein. The compounds are useful in a variety of contexts, but are primarily to be used as high energy oxidizing agents in explosive compositions, propellant formulations, gas-generating compositions and the like. The compounds are also useful as pharmaceutical agents. Compositions containing the compounds are also provided, including energetic compositions, as are methods for using the novel compounds and compositions.
Type:
Grant
Filed:
June 7, 2001
Date of Patent:
April 22, 2003
Assignee:
SRI International
Inventors:
Jeffrey C. Bottaro, Robert J. Schmitt, Mark A. Petrie, Paul E. Penwell
Abstract: The invention provides compounds of Formula I: compounds of the Formula I: 1
Type:
Application
Filed:
August 14, 2002
Publication date:
April 10, 2003
Inventors:
Donn G. Wishka, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, David W. Piotrowski, Jeffrey W. Corbett, Alice L. Bodnar, Vincent E. Groppi,
Abstract: The invention relates to novel thienylsulphonylamino(thio)carbonyl compounds of the formula (I), 1
Type:
Application
Filed:
November 9, 2001
Publication date:
January 2, 2003
Inventors:
Klaus-Helmut Muller, Ernst Rudolf F. Gesing, Mark Wilhelm Drewes, Johannes Rudolf Jansen, Rolf Kirsten, Joachim kluth, Klaus Konig, Ulrich Philipp, Markus Dollinger
Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.
Type:
Application
Filed:
June 29, 2001
Publication date:
December 12, 2002
Inventors:
Peng Cho Tang, Chung Chen Wei, Ping Huang, Jingrong Cui
Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula
wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and n, R1 and R2 are as defined in the specification.
Type:
Grant
Filed:
February 21, 2001
Date of Patent:
November 26, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Thomas W. Hudyma, Oak K. Kim, Xiaofan Zheng
Abstract: The present invention relates to compounds of the formula (I):
wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.
Type:
Grant
Filed:
September 10, 2001
Date of Patent:
October 1, 2002
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Simon Neil Owen, Eileen Mary Seward, Christopher John Swain, Brian John Williams
Abstract: Benzoylcyclohexanediones and benzoylpyrazoles, their preparation and their use as herbicides and plant growth regulators.
There are described benzoyl compounds of the formula (I), their preparation and their use as herbicides and plant growth regulators.
In this formula (I), R1, R2, R3 and R4 are various radicals, X is an alkylene chain which may contain a hetero atom and Het is a heterocycle or heteroaromatic ring.
Type:
Grant
Filed:
November 2, 2000
Date of Patent:
September 10, 2002
Assignee:
Aventis CropScience GmbH
Inventors:
Thomas Seitz, Lothar Willms, Thomas Auler, Hermann Bieringer, Felix Thürwächter
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:
Grant
Filed:
April 13, 2001
Date of Patent:
July 9, 2002
Assignee:
Dow AgroSciences LLC
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: 3-(Substituted phenyl)-5-(substituted heterocyclyl)-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:
Grant
Filed:
October 22, 1999
Date of Patent:
July 2, 2002
Assignee:
Dow AgroSciences LLC
Inventors:
Francis E. Tisdell, Peter L. Johnson, James T. Pechacek, Robert G. Suhr, Donald H. DeVries, Carl P. Denny, Mary L. Ash
Abstract: An antifungal compound of formula (I):
or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of either entity, wherein X is CH or N; R1 is phenyl subsituted with 1 to 3 substituents each independently selected from halo and CF3; R2 is (hydroxy)C1-C4 alkyl, CONH2, S(O)m(C1-C4 alkyl), Ar or Het; m is 1 or 2; Ar is phenyl optionally monosubstituted with halo or CF3; and Het is a C-linked 6-membered nitrogen-containing aromatic heterocyclic group containing 1 or 2 nitrogen atoms, or a C- or N-linked 5-membered nitrogen-containing aromatic heterocyclic group containing from 2 to 4 nitrogen atoms, wherein either of said heterocyclic groups is optionally substituted with C1-C4 alkyl or (C1-C4 alkoxy)methyl.
Type:
Grant
Filed:
December 1, 1999
Date of Patent:
April 23, 2002
Assignee:
Pfizer Inc.
Inventors:
Andrew Simon Bell, Peter Thomas Stephenson
Abstract: An antifungal compound of formula (I) or a pharmaceutically acceptable salt thereof:
wherein:
X is CH or N;
Y is O,
R1 and R2 are each independently F or Cl;
R3 is a thiophenyl, naphthyl, or phenyl group, the phenyl group being optionally substituted with one or more substituents selected from the group consisting of C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, methylenedioxy and halogen; and
R4 is H or trifluoromethyl.
Type:
Grant
Filed:
July 6, 2001
Date of Patent:
April 23, 2002
Assignee:
Korea Research Institute of Chemical Technology
Inventors:
Bum-Tae Kim, Sun-Young Han, Chwang-Siek Pak
Abstract: Compounds including 1-(biphenyl-4-yl)methyl-1H-1,2,4-triazoles and 1-(biphenyl-4-yl)methyl-4H-1,2,4-triazoles each having a (2,4-dioxopyrrolidine-5-ylidene) methyl or (2,4-dioxo-tetrahydrofuran-5-ylidene)methyl group as the substituent at the 2′-position and salts thereof are lowly toxic and highly safe and are useful as an angiotensin II antagonist. Thus, these compounds can be used in medicines, which contain these compounds as an active ingredient.
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: 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: The invention discloses ruthenium alkylidene complexes of the type (PCy3)(L)Cl2Ru(CHPh), where L is a triazolylidene ligand of the general formula: 1
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: Block copolymers containing a fluorinated hydrocarbon unit, a hydrocarbon unit, and a poly(oxyethylene) unit are useful in fluid formulations of pharmaceutical agents. A typical embodiment is:
C11H23—CONHC2H4NHCO—C8F16—CONHC2H4NHCOO—(C2H4O)34—H.
Type:
Grant
Filed:
August 5, 1999
Date of Patent:
November 13, 2001
Assignee:
Supratek Pharma, Inc.
Inventors:
Alexander V. Kabanov, Serguei V. Vinogradov
Abstract: A triazole compound having the formula:
wherein Ar1 represents a phenyl group which may be substituted, Ar2 represents a heterocyclic group which may be substituted, R0 represents a hydrogen atom or a lower alkyl; R1 represents a lower alkyl; R2 to R5 each represent a hydrogen atom or an unsubstituted or halo substituted alkyl; n represents 0 to 2; p represents 0 or 1; q, r and s each represent 0 to 2; A represents a 4- to 7-membered carbon ring or a 4- to 7-membered heterocyclic group. The compound of the present invention exhibits an excellent antifungal activity.
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: 3-(Substituted phenyl)-5-(thienyl)-1,2,4-triazole compounds are useful as insecticides and acaricides.
Type:
Grant
Filed:
October 22, 1999
Date of Patent:
July 24, 2001
Assignee:
Dow AgroSciences LLC
Inventors:
Francis E. Tisdell, James T. Pechacek, Vidyadhar B. Hegde, Joe R. Schoonover, Jr., Leonard P. Dintenfass, James M. Gifford, Maurice C. Yap, Donald H. DeVries, Christopher T. Hamilton, Norman R. Pearson, Mary L. Ash
Abstract: The present invention relates to triazole and imidazole derivatives of formula I and to their pharmaceutically acceptable acid addition salts. These compounds are NMDA receptor subtype blockers and are useful for the treatment of diseases related to the NMDA receptor.
Type:
Grant
Filed:
July 19, 2000
Date of Patent:
July 24, 2001
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Alexander Alanine, Bernd Büttelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, René Wyler
Abstract: Compounds including 1-(biphenyl-4-yl)methyl-1H-1,2,4-triazoles and 1-(biphenyl-4-yl)methyl-4H-1,2,4-triazoles each having a (2,4-dioxopyrrolidine-5-ylidene)methyl or (2,4-dioxo-tetrahydrofiuran-5-ylidene)methyl group as the substituent at the 2′-position and salts thereof are lowly toxic and highly safe and are useful as an angiotensin II antagonist. Thus, these compounds can be used in medicines, which contain these compounds as an active ingredient.
Abstract: The invention provides compositions electron-deficient nitrogen heterocycle-substituted fluorescein dyes and methods in which the dyes are conjugated to substrates and used as detection labels in molecular biology experiments. The electron-deficient nitrogen heterocycles include pyridine, quinoline, pyrazine, and the like. Substrates include polynucleotides, nucleosides, nucleotides, peptides, proteins, carbohydrates, and ligands.
Type:
Grant
Filed:
February 7, 2000
Date of Patent:
April 24, 2001
Assignee:
PE Corporation
Inventors:
Krishna G. Upadhya, Steven M. Menchen, Weiguo Zhen
Abstract: This invention relates to novel 3-substituted-2-oxindole derivatives of the formula
and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
January 16, 2001
Assignee:
Pfizer Inc.
Inventors:
Frederick J. Ehrgott, Carl J. Goddard, Gary R. Schulte