Two Double Bonds Between Ring Members Of The Diazole Ring (i.e., Imidazole) Patents (Class 548/335.1)
  • Publication number: 20020025965
    Abstract: 1
    Type: Application
    Filed: June 29, 2001
    Publication date: February 28, 2002
    Inventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
  • Publication number: 20020013356
    Abstract: A compound of formula I 1
    Type: Application
    Filed: May 7, 2001
    Publication date: January 31, 2002
    Inventors: Jari Ratilainen, Paavo Huhtala, Arto Karjalainen, Arja Karjalainen, Antti Haapalinna, Raimo Virtanen, Jyrki Lehtimaki
  • Publication number: 20010056109
    Abstract: An imidazole derivative of formula (I) 1
    Type: Application
    Filed: January 12, 2001
    Publication date: December 27, 2001
    Inventors: Paavo Huhtala, Arto Karjalainen, Antti Haapalinna, Jyrki Lehtimaki, Arja Karjalainen, Raimo Virtanen
  • Patent number: 6326500
    Abstract: Compounds of formula (I) and salts thereof, wherein R1 is hydrogen, halo, cyano, cyanoalkyl, alkyl, alkoxy, phenoxy, phenyl, alkoxycarbonyl, —NR13R14, —N(R15)SO2R16, haloalkoxy, haloalkyl, arylalkoxy, hydroxy, phenylalkyl, alkoxycarbonylvinyl, —SOnR7, alkoxycarbonylalkyl, carboxylalkyl, —CONR11R12, carbamoylvinyl, —O—SO2R21, 4,5-dihydrothiazol-2-yl, 4,4-dimethyl-2-oxazolin-2-yl, —NR60R61 or —(O)z—L3—G (G=−NR22R23, —SOmR26, CONR27R28 or —OR29); R2 and R3 are independently hydrogen halo, alkyl, alkoxy, —NR13R14, haloalkoxy, haloalkyl, hydroxy, —SOnR7 or —NR60R61; L1 is a bond, alkylene, cycloalkylene or cycloalkylidene; T is a bond, O, S, SO, SO2, CO or 1,3-dioxolan-2-ylidene; L2 is alkylene, cycloalkylene or cycloalkylidene; R6 is hydrogen or alkyl; Q is alkylene; and Y is imidazolyl, which are antiinflammatory, antiallergic and immunodulant agents.
    Type: Grant
    Filed: December 27, 2000
    Date of Patent: December 4, 2001
    Assignee: Abbott Laboratories
    Inventors: David John Calderwood, Adrian John Fisher, James Edward Jeffery, Colin Gerhart Pryce Jones, Paul Rafferty
  • Patent number: 6316620
    Abstract: A new class of chiral bidentate ligands to transition metals is disclosed which compounds have the following structure: wherein the substituents are as defined herein.
    Type: Grant
    Filed: September 5, 2000
    Date of Patent: November 13, 2001
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventor: Carl A. Busacca
  • Patent number: 6316380
    Abstract: This invention provides a catalyst system useful in many coupling reactions, such as Suzuki, Kumada, Heck, and amination reactions. The catalyst system of the present invention makes use of N-heterocyclic carbenes or their protonated salts. The composition of the catalyst system comprises at least one transition metal compound and at least one N-heterocyclic carbene or its protonated salt. This invention further provides novel N-heterocyclic carbenes and their protonated salts. One type of N-heterocyclic carbene used in this invention is an imidazolinc-2-ylidene wherein the 1 and 3 positions are each, independently, substituted by an aromatic group in which each ortho position is, independently, substituted by a secondary or tertiary group which has at least three atoms.
    Type: Grant
    Filed: February 22, 2000
    Date of Patent: November 13, 2001
    Assignee: University of New Orleans Research & Technology Foundation
    Inventors: Steven P. Nolan, Jinkun Huang, Mark L. Trudell, Chunming Zhang
  • Patent number: 6310067
    Abstract: Urocanic acid derivatives useful as antiallergic agents represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R2 denotes hydrogen or lower alkyl, R3 denotes nitro, amino, cyano or COOR2, wherein R2 in said COOR2 is as defined above, and Q denotes carbon or nitrogen.
    Type: Grant
    Filed: August 3, 2000
    Date of Patent: October 30, 2001
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Kazuhiko Ito, Takahiro Sakaue, Sachiko Inoue, Shinya Ogino
  • Patent number: 6297239
    Abstract: The present invention is directed to compounds which inhibit a prenyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting a prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: October 6, 1998
    Date of Patent: October 2, 2001
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, John H. Hutchinson, Anthony W. Shaw, Samuel L. Graham, Terrence M. Ciccarone
  • Patent number: 6288071
    Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.
    Type: Grant
    Filed: December 10, 1998
    Date of Patent: September 11, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
  • Publication number: 20010018526
    Abstract: The present invention provides a method for preparation of a quaternary ammonium salt comprising reacting an alkyl halide with 2 equimolar amount or more per the alkyl halide of a pyridine compound or an N-lower alkyl imidazole at 120° C. to 350°C., and a method for the continuous production of a quatemary ammonium salt comprises introducing continuously an alkyl halide and 2 equimolar amount or more per the alkyl halide of a pyridine compound or an N-lower alkyl imidazole into a pipe reactor from the one end thereof under heating at 120 to 350° C. to pass through the pipe reactor wherein a reaction is allowed to take place, and taking out continuously the resulting quaternary ammonium salt from the other end of the reactor.
    Type: Application
    Filed: February 9, 2001
    Publication date: August 30, 2001
    Applicant: WAKO PURE CHEMICAL INDUSTRIES, LTD.
    Inventors: Kimihiko Sano, Yoji Urano, Takuhiro Kimura, Atsunori Sano
  • Patent number: 6274584
    Abstract: Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (1): wherein a, b, A, R1, L1, D, R3, R4, R2, L2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.
    Type: Grant
    Filed: July 19, 2000
    Date of Patent: August 14, 2001
    Assignee: Novo Nordisk A/S
    Inventors: Bernd Peschke, Michael Ankersen, Thomas Kruse Hansen, Henning Thøgersen
  • Patent number: 6268313
    Abstract: The dihalopropene compounds of the general formula [I] have excellent insecticidal/acaricidal activity, so that they are satisfactorily effective for the control of noxious insects, mites and ticks.
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: July 31, 2001
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Noriyasu Sakamoto, Sanshiro Matsuo, Masaya Suzuki, Taro Hirose, Kazunori Tsushima, Kimitoshi Umeda
  • Patent number: 6265428
    Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1): where X and Y are selected from groups that include O, S, and NH; and Ar1, Ar2 and Ar3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteroaryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.
    Type: Grant
    Filed: June 8, 1999
    Date of Patent: July 24, 2001
    Assignee: Texas Biotechnology Corporation
    Inventors: Ming Fai Chan, Vitukudi Narayanaiyengar Balaji, Rosario Silvestre Castillo, Adam Kois, Bore Gowda Raju, Chengde Wu
  • Patent number: 6258851
    Abstract: Compounds of formula (I), wherein A, B, X, R1, R2, R3, R4, R5, R6 are as defined in the specification, are matrix metalloproteinase inhibitors.
    Type: Grant
    Filed: October 8, 1999
    Date of Patent: July 10, 2001
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Christopher David Floyd, Sanjay Ratilal Patel, Mark Whittaker
  • Patent number: 6245918
    Abstract: Process for the preparation of an ionic compound, Q+A− liquid at less than 150° C., wherein a trialkyloxonium of the anion is reacted with an amine in a hydrocarbon solvent. The aforesaid ionic compound can be used as a solvent in numerous catalytic reactions.
    Type: Grant
    Filed: June 1, 1999
    Date of Patent: June 12, 2001
    Assignee: Institut Francais du Petrole
    Inventors: Hélène Olivier, Frédéric Favre
  • Patent number: 6245804
    Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.
    Type: Grant
    Filed: May 29, 1998
    Date of Patent: June 12, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
  • Patent number: 6242474
    Abstract: Novel aromatic ring derivatives represented by formula (I) or their pharmaceutical acceptable salts are provided. wherein Nu represents a 5- or 6-membered aromatic ring; ch1 and ch2 each represents a cross-linking group; and A represents an aromatic ring. These compounds have blood sugar-depressing activity or PDE 5 inhibitory activity and are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin-resistance, polycystic ovary syndrome, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, hypertension, stenocardia, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, autoimmune diseases, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, nephritis, cachexia, pancreatitis, restenosis after PTCA, etc.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: June 5, 2001
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Noritsugu Yamasaki, Takafumi Imoto, Takahiro Hiramura, Osamu Onomura, Masahiro Nishikawa, Hiroshi Kayakiri, Yoshito Abe, Hitoshi Hamashima, Hitoshi Sawada
  • Patent number: 6211366
    Abstract: Disclosed are compounds encompassed by general formula (I), wherein, A represents ethenylene, or A represents —X—CH2—; where X is CH2 or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring; R1, R2, R3 and R4 are inorganic or organic substituents; and R5 and R6 are optionally substituted organic substituents; or NR5R6 represents a carbocyclic or heterocyclic six-membered ring optionally substituted with various organic or inorganic groups, which compounds can be used in treatment of neuropsychological disorders.
    Type: Grant
    Filed: August 9, 1999
    Date of Patent: April 3, 2001
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 6201001
    Abstract: Compounds of formula I inhibit celluar proliferation. Processes for the preparation of the compounds, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds are disclosed.
    Type: Grant
    Filed: August 2, 1999
    Date of Patent: March 13, 2001
    Assignee: Abbott Laboratories
    Inventors: Le Wang, Qun Li, Hing L. Sham, Keith W. Woods
  • Patent number: 6191157
    Abstract: The hetero-linked phenylglycinolamides are prepared by reaction of the corresponding hetero-linked phenylacetic acids with appropriate phenylglycinols. The hetero-linked phenylglycinolamides are suitable as active compounds in medicaments.
    Type: Grant
    Filed: December 4, 1998
    Date of Patent: February 20, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Ulrich Müller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Rudi Grützmann, Martin Beuck
  • Patent number: 6187928
    Abstract: Novel imidazolium compounds of the formula wherein A represents the atomic group necessary to form a heteroaromatic ring, which may be optionally substituted by one or more R substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substitutents; B is an optional substituent which represents the atomic group necessary to form a heteroaromatic ring or a double or triple carbon-nitrogen bond, which may optionally be substituted by one or more R′ substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substitutents; C is an optional substituent which represents the atomic group necessary to form an aromatic or heteroaromatic ring, which may optionally be substituted by one or more R″″ substituents selected from the group consisting of aryl, heteroaryl, lower alkyl, hydroxy, halide, or carboxy substituents; R″ and R′″ are each independently a lower alk
    Type: Grant
    Filed: March 7, 2000
    Date of Patent: February 13, 2001
    Assignee: The Rockefeller University
    Inventors: Robert J. Donovan, Robert J. Morgan
  • Patent number: 6177575
    Abstract: Imidazoles may be manufactured by reacting a glyoxal, ammonia, an aldehyde, and optionally a primary amine, in the presence of a Bronsted acid whose pKa is approximately equal to the pKa of the ammonium cation of the primary amine, or if the primary amine is not present, to the pKa of the ammonium (NH4+) cation. The reaction may be used to make in relatively high yields a wide variety of imidazoles using relatively inexpensive starting materials. The imidazoles are useful as chemical intermediates.
    Type: Grant
    Filed: November 17, 1998
    Date of Patent: January 23, 2001
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Anthony J. Arduengo, III, Frederick P. Gentry, Jr., Prakash K. Taverkere, Howard E. Simmons, III
  • 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