Additional Unsaturated Hetero Ring Attached Directly Or Indirectly To The Triazole Ring By Nonionic Bonding Patents (Class 548/266.2)
  • Publication number: 20040019084
    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
  • Publication number: 20030229091
    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
  • Publication number: 20030229076
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: September 16, 2002
    Publication date: December 11, 2003
    Inventors: Stanislaw Rachwal, Alan Hutchison, Kenneth Shaw, George D. Maynard, Xiao-Shu He, Robert DeSimone, Kevin Hodgetts
  • Publication number: 20030229229
    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
  • Publication number: 20030212012
    Abstract: The present invention is related to pyrrolidine derivatives of formula (I).
    Type: Application
    Filed: February 10, 2003
    Publication date: November 13, 2003
    Inventors: Serge Halazy, Anna Quattropani, Alexander Scheer, Mattias Schwarz, Russell Thomas, Antony Baxter
  • Publication number: 20030176480
    Abstract: A compound of formula (I) or a pharmacologically acceptable prodrug or salt thereof which exhibits excellent antifungal activity: 1
    Type: Application
    Filed: September 27, 2002
    Publication date: September 18, 2003
    Applicant: SANKYO COMPANY, LIMITED
    Inventors: Takuya Uchida, Toshiyuki Konosu
  • Publication number: 20030171309
    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
  • Publication number: 20030166645
    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
  • Publication number: 20030134801
    Abstract: The present invention relates to a compound having formula I: 1
    Type: Application
    Filed: November 1, 2002
    Publication date: July 17, 2003
    Applicant: LG Life Sciences, Ltd.
    Inventors: Koo Lee, Won Hyuk Jung, Cheol Won Park, Sang Koo Lee, Sun Hwa Lee, Hee Dong Park
  • Publication number: 20030134748
    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
  • Publication number: 20030130281
    Abstract: The present invention relates to compounds of formula (I) 1
    Type: Application
    Filed: October 14, 2002
    Publication date: July 10, 2003
    Inventors: Markus Boehringer, Daniel Hunziker, Holger Kuehne, Bernd M. Loeffler, Ramakanth Sarabu, Hans P. Wessel
  • Publication number: 20030125368
    Abstract: The present invention relates to compounds of the formula 1
    Type: Application
    Filed: July 2, 2002
    Publication date: July 3, 2003
    Inventors: Subas M. Sakya, Andrei Shavnya, Bryson Rast
  • Publication number: 20030114681
    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
  • Publication number: 20030096814
    Abstract: Isoxazolone compounds having the generic structure: 1
    Type: Application
    Filed: May 7, 2002
    Publication date: May 22, 2003
    Inventors: Michael Philip Clark, Jane Far-Jine Djung, Steven Karl Laughlin, Joshua Spector Tullis, Michael George Natchus, Biswanath De
  • Patent number: 6552139
    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
  • Patent number: 6552051
    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
  • Publication number: 20030069290
    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,
  • Publication number: 20030065190
    Abstract: The present invention relates to novel spiro compounds of the formula (I) 1
    Type: Application
    Filed: September 13, 2002
    Publication date: April 3, 2003
    Inventors: Hubert Spreitzer, Josef Salbeck, Frank Weissortel
  • Publication number: 20030004354
    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
  • Publication number: 20020187978
    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
  • Patent number: 6486159
    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
  • Publication number: 20020151574
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: 1
    Type: Application
    Filed: October 5, 2001
    Publication date: October 17, 2002
    Inventors: Michael Hale, James Janetka, Francois Maltais, Jingrong Cao
  • Patent number: 6458830
    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
  • Patent number: 6451833
    Abstract: A class of N-substituted (&agr;-imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: September 17, 2002
    Assignee: Pharmacia Corporation
    Inventors: Philippe R. Bovy, Joe T. Collins, Robert E. Manning
  • Patent number: 6448201
    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
  • Patent number: 6417187
    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
  • Patent number: 6413997
    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
  • Patent number: 6376526
    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
  • Patent number: 6376497
    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
  • Publication number: 20020037912
    Abstract: The present invention provides novel compounds of Formula I: 1
    Type: Application
    Filed: August 10, 2001
    Publication date: March 28, 2002
    Inventor: Ellen M. Leahy
  • Publication number: 20020038028
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: November 21, 2001
    Publication date: March 28, 2002
    Inventors: Daniel Yohannes, Mark W. Bundesmann
  • Publication number: 20020035262
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: November 21, 2001
    Publication date: March 21, 2002
    Inventors: Daniel Yohannes, Mark W. Bundesmann
  • Patent number: 6358984
    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.
    Type: Grant
    Filed: August 11, 2000
    Date of Patent: March 19, 2002
    Assignee: Lead Chemical Co., Ltd.
    Inventors: Eiichi Yoshii, Masao Mori
  • Publication number: 20020028814
    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
  • Publication number: 20020019370
    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
  • Publication number: 20020013473
    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
    Type: Application
    Filed: January 25, 2001
    Publication date: January 31, 2002
    Applicant: CALIFORNIA INSTITUTE OF TECHNOLOGY
    Inventors: Robert H. Grubbs, Tina M. Trnka
  • Patent number: 6329528
    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
  • Patent number: 6316505
    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
  • Patent number: 6300357
    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.
    Type: Grant
    Filed: February 1, 1999
    Date of Patent: October 9, 2001
    Assignee: Sankyo Company, Limited
    Inventors: Sadao Oida, Teruo Tanaka, Yawara Tajima, Toshiyuki Konosu, Atsushi Somada, Takeo Miyaoka, Hiroshi Yasuda
  • Patent number: 6294561
    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.
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: September 25, 2001
    Assignee: ICOS Corporation
    Inventors: Kerry W. Fowler, Joshua Odingo
  • Patent number: 6265424
    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
  • Patent number: 6265426
    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
  • Patent number: 6232335
    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.
    Type: Grant
    Filed: March 17, 1999
    Date of Patent: May 15, 2001
    Assignee: Lead Chemical Co., Ltd.
    Inventors: Eiichi Yoshii, Masao Mori
  • Patent number: 6221604
    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
  • Patent number: 6174883
    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