Additional Chalcogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/314)
  • Patent number: 6281219
    Abstract: The present invention provides compounds of Formula I methods for their preparation and their use as acaricidal and insecticidal agents.
    Type: Grant
    Filed: July 12, 1999
    Date of Patent: August 28, 2001
    Assignee: American Cyanamid Co.
    Inventors: Salvatore John Cuccia, William Wakefield Wood, Brian Lee Buckwalter, John Francis Chiarello, Linda Barbara Fleming
  • Patent number: 6277789
    Abstract: The invention relates to substituted phenyluracils of the general formula (I) in which the radicals R1 to R5, Q and n are each as defined in the description, and to processes for their preparation and to their use as herbicides.
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: August 21, 2001
    Inventors: Roland Andree, Otto Schallner, Katharina Voigt, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6274732
    Abstract: A process for the preparation of the compound of the formula (I) by reacting a compound of the formula (IV) with a compound of the formula (III).
    Type: Grant
    Filed: December 28, 1999
    Date of Patent: August 14, 2001
    Assignee: Samjin Pharmaceutical Co., Ltd.
    Inventors: Eui-Hwan Cho, Sun-Gan Chung, Sun-Hwan Lee, Ho-Seok Kwon, Jae-Eung Lee, Dong-Wook Kang
  • Patent number: 6262051
    Abstract: The invention relates to novel methoximinomethyldioxazines, to a plurality of processes for their preparation and to their use as fungicides, and also to novel intermediates and to a process for their preparation.
    Type: Grant
    Filed: September 28, 1999
    Date of Patent: July 17, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Bernd-Wieland Krüger, Robert Markert, Thomas Seitz, Bernd Gallenkamp, Uwe Stelzer, Ralf Tiemann, Astrid Mauler-Machnik, Stefan Dutzmann, Klaus Stenzel, Gerd Hänssler
  • Patent number: 6254669
    Abstract: A compound of the Formula (1) and salts thereof: wherein: Ar, Ar1, J, J1, X, X1 W, W1, L and m are as defined in the description. The compounds of Formula (1) are useful as additives in inks, especially ink jet printing inks, for reducing color bleed between adjacent printed regions. Also claimed are inks containing a compound of the Formula (1), a method of ink jet printing using the inks, a substrate printed with the ink and an ink jet printer cartridge containing the ink.
    Type: Grant
    Filed: August 5, 1999
    Date of Patent: July 3, 2001
    Assignee: Zeneca Limited
    Inventors: Aidan Joseph Lavery, Prahalad Manibhai Mistry, Ronald Wynford Kenyon
  • Patent number: 6251828
    Abstract: The invention relates to novel substituted phenyluracils 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 novel intermediates and to their use as herbicides.
    Type: Grant
    Filed: January 23, 1998
    Date of Patent: June 26, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6251829
    Abstract: This invention relates to herbicidal alpha-(2,4,5-trisubstituted)- and alpha-(2,5-disubstituted)-benzoyloxy-alpha-beta-, and/or beta-gamma-unsaturated-carboxylates and their derivatives, to compositions which contain these compounds, and to methods of use of these compounds.
    Type: Grant
    Filed: April 18, 2000
    Date of Patent: June 26, 2001
    Assignee: Rohm and Haas Company
    Inventors: Bin Li, Ying Man, Zongjian Zhang, Longhe Xu, Adam Chi-Tung Hsu
  • Patent number: 6245773
    Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: June 12, 2001
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Wai C. Wong, Bharat Lagu, Dhanapalan Nagarathnam, Mohammad R. Marzabadi, Charles Gluchowski
  • Patent number: 6242601
    Abstract: The compounds of formula (I) wherein R1, R2 and X have the significance as given in the description, are inhibitors of endothelin receptors and can therefore be used for the treatment of disorders which are associated with abnormal vascular tone and endothelial dysfunction.
    Type: Grant
    Filed: January 13, 2000
    Date of Patent: June 5, 2001
    Assignee: Hoffman-La Roche Inc.
    Inventors: Volker Breu, Philippe Coassolo, Rolf Huber, Werner Neidhart, Henri Ramuz, Sébastien Roux, Hans Peter Wessel
  • Patent number: 6239074
    Abstract: A substituted 3-phenyluracil of the formula I where X1 and X2 are each oxygen; W is —C(R8)=X5, where X5 is oxygen, sulfur, or a radical —NR14; R14 is hydroxyl, alkoxy, alkenyloxy, alkynyloxy, cycloalkoxy, cycloalkenyloxy, haloalkoxy, haloalkenyloxy, hydroxyalkoxy, cyanoalkoxy, cycloalkylalkoxy, alkoxyalkoxy, alkoxyalkenyloxy, alkylcarbonyloxy, haloalkylcarbonyloxy, alkylcarbamoyloxy, haloalkylcarbamoyloxy, alkoxycarbonylalkoxy, alkylthioalkoxy, dialkylaminoalkoxy, R8 is hydrogen, cyano or alkyl; R1 is halogen or cyano; R2 is hydrogen or halogen; R3 is hydrogen or alkyl; R4 is cyano, alkyl or haloalkyl; R5 is hydrogen, halogen or alkyl; or a salt or enol ether of a compound I wherein R3 is hydrogen, or its tautomeric forms, for the desiccation and defoliation of plants or as an insecticide or herbicide.
    Type: Grant
    Filed: January 3, 1997
    Date of Patent: May 29, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Ralf Klintz, Peter Schaefer, Gerhard Hamprecht, Elisabeth Heistracher, Hans-Josef Wolf, Karl-Otto Westphalen, Matthias Gerber, Uwe Kardorff, Helmut Walter, Klaus Grossmann
  • Patent number: 6232318
    Abstract: Novel pyrimidinedione compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: May 15, 2001
    Assignee: Merck & Co., Ltd.
    Inventors: Jennie B. Nerenberg, Mark G. Bock
  • Patent number: 6232325
    Abstract: This invention is directed to benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: May 15, 2001
    Assignee: Berlex Laboratories, Inc.
    Inventors: Monica Kochanny, Michael M. Morrissey, Howard P. Ng
  • Patent number: 6225470
    Abstract: The invention relates to a process for preparing ar(alk)yluracils of the general formula (I) in which A represents a single bond or represents alkanediyl, Ar represents optionally substituted aryl, R1 represents optionally substituted alkyl and R2 represents hydrogen, halogen or alkyl, and to novel intermediates for this purpose and to processes for their preparation.
    Type: Grant
    Filed: May 8, 2000
    Date of Patent: May 1, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Gallenkamp, Reinhard Lantzsch, Lothar Rohe, Lubbertus Mulder
  • Patent number: 6218376
    Abstract: Compounds of formula I or salts thereof where for example Y is a group of the formula (i) and R1 is a group of formula (ii) are provided along with compositions containing them and processes for their preparation. The compounds are P2-purinoreceptor 7-transmembrane G-protein coupled receptor antagonists, and are useful in the treatment of inflammatory conditions.
    Type: Grant
    Filed: December 9, 1998
    Date of Patent: April 17, 2001
    Assignee: AstraZeneca UK Limited
    Inventors: Nicholas Kindon, Premji Meghani, Stephen Thom
  • Patent number: 6215004
    Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.
    Type: Grant
    Filed: August 12, 1999
    Date of Patent: April 10, 2001
    Assignees: Emory University, Triangle Pharmaceuticals, Inc.
    Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
  • Patent number: 6191070
    Abstract: Pyrimidinone derivatives of the general formula: wherein R1 is hydrogen or alkyl; R2 is haloalkyl; R3 is nitrogen or CH; G is optionally substituted ethylene, trimethylene, or vinylene; and Q is selected from several optionally substituted or heterocyclic-condensed phenyl groups, are useful as the active ingredients of herbicides because of their excellent herbicidal activity.
    Type: Grant
    Filed: September 4, 1998
    Date of Patent: February 20, 2001
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takashi Komori, Hisayuki Hoshi
  • Patent number: 6177437
    Abstract: The invention is directed to novel 6-aromatic substituted uracil compounds of formula I therapeutic compositions comprising the compounds, and methods of treating Herpes simplex virus Type I and Type II recurrent infections and Herpes simplex virus Type I and Type II encephalitis in humans using the compounds and/or therapeutic compositions.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: January 23, 2001
    Assignee: University of Massachusetts Medical Center
    Inventor: George E. Wright
  • Patent number: 6175008
    Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S═O or SO2. The invention also relates to intermediates of use in the preparation of these compounds.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 16, 2001
    Assignee: BioChem Pharma Inc.
    Inventors: Bernard Belleau, Tarek Mansour, Allan Tse, Colleen A. Evans, Haolun Jin, Boulos Zacharie, Nghe Nguyen-Ba
  • Patent number: 6169182
    Abstract: The invention relates to a novel process for preparing substituted cyanophenyluracils of the general formula (I) in which R1, R2, R3 and R4 are each as defined in the description, said compounds being known as herbicidally active compounds, to novel substituted N-(cyanophenyl)aminoalkenamides as intermediates therefor and to an inventive process for their preparation.
    Type: Grant
    Filed: July 30, 1998
    Date of Patent: January 2, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Reinhard Lantzsch, Heinz-J{umlaut over (u)}rgen Wroblowsky
  • Patent number: 6159995
    Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.
    Type: Grant
    Filed: May 8, 1998
    Date of Patent: December 12, 2000
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
  • Patent number: 6156759
    Abstract: Novel compounds that are potent inhibitors of HIV reverse transcriptase (RT) are described in the invention. Thes novel compounds also inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The novel compounds of the invention include analogs and derivatives of phenethylthiazolylthiourea (PETT), of dihydroalkoxybenzyloxopyrimidine (DABO), and of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT).The invention additionally provides a composite HIV reverse-transcriptase (RT) nonnucleoside inhibitor (NNI) binding pocket constructed from a composite of multiple NNI-RT complexes The composite RT-NNI binding pocket provides a unique and useful tool for designing and identifying novel, potent inhibitors of reverse transcriptase.
    Type: Grant
    Filed: December 4, 1998
    Date of Patent: December 5, 2000
    Assignee: Parker Hughes Institute
    Inventors: Rakesh Vig, Chen Mao, Fatih A. Uckun
  • Patent number: 6153619
    Abstract: There are provided compositions and methods comprising compounds of formula I: ##STR1## wherein R.sup.1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.
    Type: Grant
    Filed: March 22, 1999
    Date of Patent: November 28, 2000
    Assignee: American Cyanamid Company
    Inventors: William Wakefield Wood, Linda Fleming, Salvatore John Cuccia
  • Patent number: 6136815
    Abstract: 6-aryloxy and 6-arylcarbonyl 2,4-pyrimidinedione derivatives of the formula(I) having high antiviral activity against HIV-1 and low toxicity are useful for treating AIDS: ##STR1## wherein: R.sup.1 is hydrogen or a C.sub.1-10 alkyl group optionally having a substituent selected from the group consisting of aryl, hydroxy, C.sub.1-10 alkoxy and C.sub.2-5 alkylcarbonyloxy groups;R.sup.2 is hydrogen or a C.sub.1-10 alkyl group optionally having an aryl substituent;R.sup.3 and R.sup.4 are each hydrogen or a C.sub.1-3 alkyl group; andA is oxygen or a carbonyl group.
    Type: Grant
    Filed: November 10, 1998
    Date of Patent: October 24, 2000
    Assignees: Korea Research Inst. of Chem. Tech., Samjin Pharmaceutical Co., Ltd.
    Inventors: Jong-Chan Son, Iii Young Lee, Hyun-Sook Kim, Jin-Chel Kim, Eui-Hwan Cho, Sun-Gan Chung, Joung-Young Kim, Soon-Hwan Lee, Ho-Seok Kwon, Jae-Weung Lee
  • Patent number: 6136976
    Abstract: Perylene-3,4-dicarboximides I ##STR1## (R.sup.1 is hydrogen; C.sub.1 -C.sub.8 -alkyl; C.sub.5 -C.sub.8 -cycloalkyl; substituted or unsubstituted phenyl or naphthyl;R.sup.2 independently at each occurrence is hydrogen; C.sub.1 -C.sub.18 -alkyl, substituted or unsubstituted aryloxy, arylthio, hetaryloxy or hetarylthio)are prepared by reacting the corresponding perylene-3,4,9,10-tetracarboxylic acid or its anhydride (II) with an amide IIIR.sup.3 --CO--NHR.sup.1 III(R.sup.3 : C.sub.1 -C.sub.4 -alkyl or --NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 independently are hydrogen or one of the R.sup.1 alkyls, cycloalkyls, phenyls or naphthyls and where if two or more of R.sup.1, R.sup.4 and R.sup.5 are other than hydrogen they are identical)under superatmospheric pressure in the presence of an inert diluent and a transition metal catalyst.
    Type: Grant
    Filed: December 7, 1998
    Date of Patent: October 24, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Arno Boehm, Harald Arms, Willi Helfer, Georg Henning
  • Patent number: 6130225
    Abstract: The invention relates to novel substituted p-trifluoromethylphenyluracils of the general formula (I) in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each as defined in the description, to a process for their preparation and to their use as herbicides.
    Type: Grant
    Filed: February 2, 1999
    Date of Patent: October 10, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Mark-Wilhelm Drewes, Roland Andree, Markus Dollinger
  • Patent number: 6127355
    Abstract: The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of a biologically active moiety;X is an electron withdrawing group;Y and Y' are independently O or S;(n) is zero (0) or a positive integer, preferably from 1 to about 12;R.sub.1 and R.sub.2 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls and substituted C.sub.1-6 alkyls;R.sub.3 is a substantially non-antigenic polymer, C.sub.1-12 straight or branched alkyl or substituted alkyl, C.sub.5-8 cycloalkyl or substituted cycloalkyl, carboxyalkyl, carboalkoxy alkyl, dialkylaminoalkyl, phenylalkyl, phenylaryl or ##STR2## R.sub.4 and R.sub.5 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls, and substituted C.sub.1-6 alkyls or jointly form a cyclic C.sub.5 -C.sub.7 ring.
    Type: Grant
    Filed: March 26, 1999
    Date of Patent: October 3, 2000
    Assignee: Enzon, Inc.
    Inventors: Richard B. Greenwald, Annapurna Pendri, Hong Zhao
  • Patent number: 6124307
    Abstract: Novel compounds that are potent inhibitors of HIV reverse transcriptase (RT) are described in the invention. Thes novel compounds also inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The novel compounds of the invention include analogs and derivatives of phenethylthiazolylthiourea (PETT), of dihydroalkoxybenzyloxopyrimidine (DABO), and of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT).The invention additionally provides a composite HIV reverse-transcriptase (RT) nonnucleoside inhibitor (NNI) binding pocket constructed from a composite of multiple NNI-RT complexes The composite RT-NNI binding pocket provides a unique and useful tool for designing and identifying novel, potent inhibitors of reverse transcriptase.
    Type: Grant
    Filed: December 4, 1998
    Date of Patent: September 26, 2000
    Assignee: Wayne Hughes Institute
    Inventors: Rakesh Vig, Chen Mao, Faith A. Uckun
  • Patent number: 6110870
    Abstract: The invention relates to new N-cyanoaryl-nitrogen hetero-cycles of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Z have the meanings given in the description,to a plurality of processes for their preparation, to their use as herbicides and to novel intermediates.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: August 29, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark-Wilhelm Drewes, Albrecht Marhold, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 6103898
    Abstract: Cyclic urea derivatives of the formula I ##STR1## in which X, X', Y, Y' and Z can have various meanings, are prepared by a) reacting a urea derivative of the formula II ##STR2## with a diketone of the formula III ##STR3## and b) hydrogenating the product from step a) in the presence of a metal-containing catalyst.
    Type: Grant
    Filed: September 28, 1998
    Date of Patent: August 15, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Andreas Kramer, Wolfgang Siegel
  • Patent number: 6103732
    Abstract: Carboxylic acid derivatives of the formula I ##STR1## where the radicals have the meanings stated in the description, and the preparation of these agreements [sic] and their use as drugs are described.
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: August 15, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Wilhelm Amberg, Andreas Kling, Dagmar Klinge, Hartmut Riechers, Ernst Baumann, Liliane Unger, Manfred Raschack, Stefan Hergenroder, Sabine Schult
  • Patent number: 6077812
    Abstract: Novel herbicidal compounds, compositions containing them, and methods for their use in controlling weeds are disclosed. The novel herbicidal compounds are represented by formula I: ##STR1## where J is a 1-substituted-6-trifluoromethyl-2,4-pyrimidinedione-3-yl, a 1-substituted-6-trifluoromethyl-1,3,5-triazine-2,4-dion-1-yl, a 3,4,5,6-tetrahydrophthalimid-1-yl, a 4-difluoromethyl-4,5-dihydro-3-methyl-1,2,4-triazol-5(1H)-on-1-yl, a 5,6,7,8-tetrahydro-1H,3H-[1,3,4]thiadiazolo[3,5-a]pyridazineimin-1-yl, or a 1,6,8-triazabicyclo[4.3.0]-nonane-7,9-dion-8-yl ring attached at the 7 position of a benzofuran, benzoxazole, indole, 2,3-dihydrobenzimidazole or benzimidazole, and X is selected from hydrogen, halogen, cyano, nitro, and amino. Preferred R groups are optionally substituted alkyl groups.
    Type: Grant
    Filed: February 24, 1998
    Date of Patent: June 20, 2000
    Assignee: FMC Corporation
    Inventors: Scott D. Crawford, Lester L. Maravetz, George Theodoridis, Benjamin Dugan
  • Patent number: 6066733
    Abstract: 4-Ethoxy-pyrimidines useful as intermediates in preparing antiviral 1,3-oxathiolane nucleosides are described.
    Type: Grant
    Filed: June 28, 1999
    Date of Patent: May 23, 2000
    Assignee: Glaxo Wellcome Inc.
    Inventors: Mirna C. Samano, Vicente Samano
  • Patent number: 6057445
    Abstract: The present invention comprises methods of synthesizing compounds having the formula I: ##STR1## wherein: Y.sub.1, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.8 are as described herein, which comprises the steps of(a) reacting a compound of the formula III ##STR2## with a base to cause cyclization to compound IV ##STR3## (b) transforming said hydroxy group of said compound IV to an amine by successive halogenation by a halogenating agent and displacement of the resultant halogen with an amide to form compound V ##STR4## (c) reacting said compound V with an effective amount of compound VI ##STR5## to form the compound of formula 1.
    Type: Grant
    Filed: December 10, 1998
    Date of Patent: May 2, 2000
    Assignee: Euro-Celtique S.A.
    Inventors: David J. Cavalla, Mark Chasin, Peter Hofer
  • Patent number: 6051709
    Abstract: The invention relates to a diastereoselective process for the preparation of compounds of formula (I), wherein W is S, S.dbd.O, SO.sub.2 or O; X is S, S.dbd.O, SO.sub.2 or O; R.sub.1 is hydrogen or acyl, and R.sub.2 is a purine or pyrimidine base or an analogue or derivative thereof.
    Type: Grant
    Filed: December 24, 1996
    Date of Patent: April 18, 2000
    Assignee: Glaxo Group Limited
    Inventors: Michael David Goodyear, P. Owen Dwyer, Malcolm Leithead Hill, Andrew Jonathan Whitehead, Roy Hornby, Peter Hallett
  • Patent number: 6043248
    Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R.sub.4 is selected from the group consisitng of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R.sub.6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R.sub.4 and R.sub.6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive being inhibitors of viral reverse transcriptase.
    Type: Grant
    Filed: October 17, 1997
    Date of Patent: March 28, 2000
    Assignee: Pharmacia & Upjohn Company
    Inventors: Richard A. Nugent, Stephen T. Schlachter, Michael J. Murphy, Joel Morris, Richard C. Thomas, Donn G. Wishka, Gary J. Cleek, David R. Graber
  • Patent number: 6017923
    Type: Grant
    Filed: May 31, 1996
    Date of Patent: January 25, 2000
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Jeffrey S. Sabol, Sai P. Sunkara, Shawn C. Miller
  • Patent number: 5962460
    Abstract: The present invention provides antineoplastic .alpha.-methylene-.gamma.-butyrolactones represented by the general formula ?I! wherein R.sub.1 is a phenyl group optionally substituted with one or two groups selected from the group consisting of halide, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, phenyl, nitro and amino;.sub.2 R represents hydrogen, halide, (C.sub.1 -C.sub.4)alkyl or benzyl; X represents N; or wherein R.sub.1 is a phenyl group optionally substituted with one or two groups selected from the group consisting of halide, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4) alkoxy, nitro and amino; R.sub.2 represents Cl, F, or benzyl; X represents CH. These .alpha.-methylene-.gamma.-butyrolactones may be administered with an inert diluent or with a pharmaceutically acceptable carrier in controlling the growth of a neoplasm in a patient afflicted with a neoplasm disease.
    Type: Grant
    Filed: June 27, 1995
    Date of Patent: October 5, 1999
    Assignee: National Science Council (Taiwan)
    Inventors: Cherng-Chyi Tzeng, Kuan-Han Lee, Yeh-Long Chen, Bor-Ruey Huang
  • Patent number: 5935965
    Abstract: 2-?(2-Alkoxy-6-trifluoromethylpyrimidin-4-yl)oxymethylene!-phenylacetic acid derivatives of the formula I ##STR1## where the index and the substituents have the following meanings: U is CH or N;V is O or NH;R is alkyl;R.sup.1 is cyano, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or phenyl;n is 0 or an integer from 1 to 4,processes and intermediates for their preparation, and their use are described.
    Type: Grant
    Filed: May 6, 1997
    Date of Patent: August 10, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Kirstgen, Klaus Oberdorf, Franz Schutz, Hans Theobald, Volker Harries
  • Patent number: 5935907
    Abstract: The invention is related to a novel phenylacetylene derivates of formula: ##STR1## wherein X represents hydrogen, halogen, optionally substituted C.sub.1-6 alkyl; Y represents hydrogen, halogen, cyano, nitro, optionally substituted C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.3-8 cycloalkoxy, optionally substituted C.sub.1-6 alkylthio, C.sub.3-8 cycloalkylthio, C.sub.1-6 alkylsulfinyl, optionally substituted C.sub.1-6 alkylsulfonyl, C.sub.3-8 cycloalkylsulfonyl, C.sub.1-6 alkylsulfonyloxy, optionally substituted sulfonamide, optionally substituted carboxamide, etc., or Y may form together with Z which is bonded to the vicinal carbon atom a 5- or 6-membered ring; n is 0 or 1; Z represents hydrogen or halogen; m is 1 or 2; R represents hydrogen, halogen, C.sub.1-6 alkyl, tri(C.sub.1-6 alkyl)silyl, COOR.sup.c or CONR.sup.d R.sup.e ; Q represents a heterocyclic group, and their use as herbicid.
    Type: Grant
    Filed: March 24, 1998
    Date of Patent: August 10, 1999
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Akihiko Yanagi, Shin-ichi Narabu, Toshio Goto, Seishi Ito, Natsuko Minegishi, Tatsuya Yamaoka, Chieko Ueno
  • Patent number: 5932730
    Abstract: Carboxylic acid derivatives ##STR1## where R-R.sup.6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: August 3, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
  • Patent number: 5922727
    Abstract: The present invention relates to novel compound of general formula (I) and pharmaceutically acceptable salts thereof, and process for the preparation of such derivatives and to pharmaceutical compositions containing the same as active ingredients. ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 represents independently hydrogen atom, halogen atom, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 thioalkyl, C.sub.3 -C.sub.8 optionally substituted cyclicalkyl, unsaturated alkyl, substituted alkyl hydroxyl or aryl hydroxyl, C.sub.1 -C.sub.10 alkylamine, nitro, C.sub.1 -C.sub.4 lower ester, C.sub.1 -C.sub.4 lower alkoxy, C.sub.1 -C.sub.4 lower thioalkoxy; Z represents oxygen atom, sulfur atom, carbon atom and carbonyl group; X represents oxygen atom, sulfur atom; n represents an integer of 1-3; and (sub)cycloalk(en)yl represents ##STR2## in which R.sub.4 and R.sub.
    Type: Grant
    Filed: January 21, 1998
    Date of Patent: July 13, 1999
    Assignee: Samjin Pharmaceutical Co., Ltd
    Inventors: Eui-Hwan Cho, Sun-Gan Chung, Joong-Young Kim, Sun-Hwan Lee, Ho-Seok Kwon, Jae-Eung Lee, Jeong-Ho Joo, Byung-Chul Kim, Dong-Wook Kang
  • Patent number: 5919792
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.
    Type: Grant
    Filed: October 28, 1997
    Date of Patent: July 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
  • Patent number: 5914400
    Abstract: The present invention relates to a method of preparing BCH-189 and various analogs of BCH-189 from inexpensive precursors with the option of introducing functionality as needed. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds, .beta.-BCH-189 and related compounds. Furthermore, the steochemistry at the nucleoside 4' position can be controlled to produce enantiomerically-enriched .beta.-BCH-189 and its analogs.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 22, 1999
    Assignee: Emory University
    Inventors: Dennis C. Liotta, Woo-Baeg Choi
  • Patent number: 5912261
    Abstract: Carboxyalkyl heterocyclic derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component are useful pharmaceuticals for the treatment of diabetic complications such as diabetic neuropathy, diabetic cataracts and retinopathy, diabetic nephropathy, diabetic dermopathy, and other diabetic microangiopathy. The compounds of the present invention are represented by the following general formula (A): ##STR1## The compounds of the present invention exhibit excellent inhibitory action towards aldose reductase with a high enzyme selectivity. Accordingly, they are useful as drugs for the therapy and prevention of various types of diabetic complications without substantially inhibiting aldehyde reductase.
    Type: Grant
    Filed: December 19, 1995
    Date of Patent: June 15, 1999
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Takayuki Kotani, Kaoru Okamoto, Yasuhiro Nagaki
  • Patent number: 5888940
    Abstract: Substituted benzothiazoles I and their salts ##STR1## used as herbicides and for the desiccation/abscission of plants.
    Type: Grant
    Filed: February 17, 1998
    Date of Patent: March 30, 1999
    Assignee: BASF Aktiengesellschaft
    Inventors: Elisabeth Heistracher, Gerhard Hamprecht, Olaf Menke, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter
  • Patent number: 5889013
    Abstract: The present invention relates to novel pyrimidine acyclonucleoside derivatives represented by the following general formula (I), antiviral agents containing the derivatives as the active ingredients and processes of preparation thereof. ##STR1## wherein R.sup.1 is ethyl or isopropyl; R.sup.2 is (3,5 dimethylphenyl)selenenyl; R.sup.3 is phenyl or methyl; X is oxygen; and Y is oxygen.
    Type: Grant
    Filed: January 4, 1996
    Date of Patent: March 30, 1999
    Assignee: Sunkyong Industries Co., Inc.
    Inventors: Dae-Kee Kim, Jongsik Gam, Ganghyeok Kim, Young-Woo Kim, Namkyu Lee, Jinsoo Lim, Hun-Taek Kim, Key Hyup Kim
  • Patent number: 5869666
    Abstract: Conformationally locked 4',6'-cyclopropane-fused carboxylic nucleoside analogues. The compounds are prepared by condensing a cyclopropane-fused carbocyclic allylic alcohol with substituted purine or pyrimidine bases. The condensation products are then modified to produce the adenosine, guanosine, cytidine, thymidine, and uracil nucleoside analogues. The compounds are therapeutically useful as antimetabolites, or in the preparation of anti-metabolic agents.
    Type: Grant
    Filed: March 14, 1997
    Date of Patent: February 9, 1999
    Assignee: The United States of America as represented by the Secretary of the Department of Health and Human Services
    Inventors: Victor E. Marquez, Juan B. Rodriguez, Marc C. Nicklaus, Joseph J. Barchi, Jr., Maqbool A. Siddiqui
  • Patent number: 5840892
    Abstract: A novel process for the preparation of substituted pyrimidine derivatives of the general formula: ##STR1## in which a halopyrimidine is reacted in the presence of a sulfinate with a compound selected from the series: ##STR2## The compounds of the general formula I are precursors of, for example, compounds with herbicidal activity.
    Type: Grant
    Filed: April 8, 1997
    Date of Patent: November 24, 1998
    Assignee: Lonza AG
    Inventors: Yves Bessard, Gerhard Stucky
  • Patent number: 5817814
    Abstract: This invention describes a method for preparing benzyluracils using methyl benzylcarbamates as intermediates. The method comprises the steps of contacting an alkali metal salt of an ester of 3-amino-4,4,4-trifluoro-2-butenoic acid with a methyl benzylcarbamate I to provide a benzyluracil II. ##STR1## where R, W, V, X and Y are as described in the specification.
    Type: Grant
    Filed: May 1, 1997
    Date of Patent: October 6, 1998
    Assignee: FMC Corporation
    Inventors: Marvin J. Konz, Harvey R. Wendt
  • Patent number: H1951
    Abstract: It has now been found that certain novel benzofuranyl derived uracils have provided unexpected pre-emergent and post-emergent herbicidal efficacy. These compounds are represented by formula I Preferred are those of formula I where R is fluoroalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonylhaloalkyl, alkenoxycarbonylalkyl, or mono- or dialkylaminocarbonylalkyl; X is halogen; Y is hydrogen or halogen; and, Z is methyl or amino. Novel intermediates to the compounds of formula I are also disclosed.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: March 6, 2001
    Inventors: George Theodoridis, Scott D. Crawford