Additional Hetero Ring Which Is Unsaturated Patents (Class 544/310)
  • 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: 6127376
    Abstract: This invention is directed to aryl and heterocyclyl substituted pyrimidine derivatives selected from the following formulae: ##STR1## wherein Z.sup.1, Z.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined herein. These compounds are useful as anti-coagulants.
    Type: Grant
    Filed: December 4, 1998
    Date of Patent: October 3, 2000
    Assignee: Berlex Laboratories, Inc.
    Inventors: David D. Davey, Gary B. Phillips
  • 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: 6107297
    Abstract: The invention relates to new pharmaceutically active compounds which are P2-purinoceptor 7-transmembrane (TM) G-protein coupled receptor antagonists, compositions containing them and processes for their preparation.
    Type: Grant
    Filed: September 30, 1998
    Date of Patent: August 22, 2000
    Assignee: Astra Pharmaceuticals Limited
    Inventors: Nicholas Kindon, Premji Meghani, Stephen Thom
  • 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: 6100252
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: August 8, 2000
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takehiko Naka, Yoshiyuki Inada
  • Patent number: 6080702
    Abstract: Disclosed are herbicidal heterocyclic benzisoxazoles and benzisoxazolidinones of formula (I): ##STR1## wherein A is (a), (b) or (c); U is N or NR; X is CO or CR.sup.2 ; and R, R.sup.1, R.sup.2, R.sup.3, Y and Z are as disclosed in the disclosure.
    Type: Grant
    Filed: September 14, 1998
    Date of Patent: June 27, 2000
    Assignee: FMC Corporation
    Inventors: George Theodoridis, Lester L. Maravetz, Scott D. Crawford
  • 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: 6074989
    Abstract: The invention relates to novel substituted azolylsulphonylphenyluracils of the general formula (I) ##STR1## in which Az represents optionally substituted azolyl,R.sup.1 represents hydrogen, cyano or halogen,R.sup.2 represents cyano, nitro, halogen or a respectively optionally substituted radical of the group consisting of alkyl and alkoxy,R.sup.3 represents hydrogen, halogen, alkyl or halogenoalkyl,R.sup.4 represents hydrogen, alkyl or halogenoalkyl, andR.sup.5 represents hydrogen, amino, formyl or a respectively optionally substituted radical from the group consisting of alkyl, alkenyl or alkinyl,a process for their preparation and their use as herbicides.
    Type: Grant
    Filed: April 25, 1997
    Date of Patent: June 13, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6066641
    Abstract: The present invention relates to novel compounds of the formula (I): ##STR1## wherein Q.sub.3 R.sub.3 and Q.sub.8 R.sub.8 are described herein. The compounds possess PDE-IV inhibitory activity and improved selectivity with regard to PDE-III inhibition. Also disclosed are pharmaceutical compositions and methods of treatment utilizing the disclosed compounds.
    Type: Grant
    Filed: June 11, 1997
    Date of Patent: May 23, 2000
    Assignee: Euro-Celtique S.A.
    Inventors: David Cavalla, Peter Hofer, Mark Chasin
  • Patent number: 6057269
    Abstract: Benzylhydroxylamines I ##STR1## (X=--N(R.sup.7)--O--; Y=O, S; R.sup.1 =halogen, CN, NO.sub.2, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3 =H, NH.sub.2, CH.sub.3 ;R.sup.4 =H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl;R.sup.5 =H, halogen, C.sub.1 -C.sub.6 -alkyl;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl;R.sup.7 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.2 -C.sub.8 -alkenyloxycarbonyl, C.sub.2 -C.sub.6 -alkynyloxycarbonyl, C.sub.1 -C.sub.6 -alkylthiocarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: May 2, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Cyrill Zagar, Karl-Otto Westphalen, Helmut Walter, Ulf Misslitz, Olaf Menke, Markus Menges
  • Patent number: 6054590
    Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of phenyl derivatives of imidazolone compounds of Formula I. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
    Type: Grant
    Filed: March 3, 1999
    Date of Patent: April 25, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Graham S. Poindexter, Ildiko Antal, Leah M. Giupponi, Robert H. Stoffel, Kevin Gillman, Mendi Higgins
  • 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: 6020348
    Abstract: Novel pyridines, pyrimidines, pyrazines, pyridazines and triazines, pharmaceutical compositions containing these compounds and their use as endothelin receptor antagonists are described.
    Type: Grant
    Filed: July 31, 1998
    Date of Patent: February 1, 2000
    Assignee: SmithKline Beecham Corporation
    Inventor: John Duncan Elliott
  • Patent number: 5998456
    Abstract: Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N--R.sup.4 ; R.sup.1 and R.sup.2 independently represent hydrogen, a halogen atom, alkyl group or other; R.sup.1 and R.sup.4 independently represent hydrogen, alkyl group, acyl group or other; n and m independently represent an integer of 1, 2, or 3; and L represents a linking group such as C.sub.2-12 alkylene group or an alkylene group containing one or more phenylene groups or ether groups. The compounds are useful as an active ingredient of a medicament such as a preventive and therapeutic medicament for hyperlipemia or arterial sclerosis.
    Type: Grant
    Filed: January 16, 1998
    Date of Patent: December 7, 1999
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Kozo Aoki, Kazuhiro Aikawa
  • Patent number: 5981436
    Abstract: The invention relates to new substituted diazacyclohexanedi(thi)ones of the general formula (I) ##STR1## in which Q.sup.1, Q.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in the description,a process for their preparation, new intermediate products and their use as herbicides.
    Type: Grant
    Filed: April 29, 1998
    Date of Patent: November 9, 1999
    Assignee: Bayer Aktiengesellschaft
    Inventors: Mark-Wilhelm Drewes, Roland Andree, Otto Schallner, Hans-Joachim Santel, Markus Dollinger
  • Patent number: 5977363
    Abstract: There is provided a process for the preparation of unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds. The unsymmetrical 4,6-bis(aryloxy)pyrimidine compounds are useful as pesticidal agents.
    Type: Grant
    Filed: May 12, 1998
    Date of Patent: November 2, 1999
    Assignee: American Cyanamid Company
    Inventors: William Wakefield Wood, Salvatore John Cuccia, Robert Brigance
  • Patent number: 5977367
    Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'.sub.m, or --NR'.sub.m where m is 0, 1 or 2 and R' is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group,which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.
    Type: Grant
    Filed: January 9, 1998
    Date of Patent: November 2, 1999
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Xi Chen
  • Patent number: 5962479
    Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: October 5, 1999
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng Liang Chen
  • Patent number: 5962685
    Abstract: The present invention is directed to oxazole derivatives represented by the formula ?I!; ##STR1## wherein A represents a nitrogen atom or a R.sub.3 -substituted carbon atom; B represents a nitrogen atom, or an unsubstituted or X-substituted carbon atom; Z represents an oxygen atom, sulfinyl or sulfonyl; R.sub.1 and R.sub.2 represent each independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 haloalkoxy, C.sub.1 -C.sub.6 haloalkyl or the like; R.sub.3 represents hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, formyl or acyl; X represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 haloalkyl or the like; Y represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.sub.6 haloalkyl or the like; m represents an integar of 1 or 2, and n represents an integar of 1, 2, 3 or 4, and the salts thereof.
    Type: Grant
    Filed: January 28, 1997
    Date of Patent: October 5, 1999
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Akiyoshi Ueda, Yasuyuki Miyazawa, Yoshihiko Hara, Masami Koguchi, Akihiro Takahashi, Takashi Kawana
  • 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: 5929046
    Abstract: The present invention provides certain 6-hetarylalkyloxy pyrimidine derivatives of formula II ##STR1## wherein R is (i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hetero atom chosen from O, N, or S, or a substituted derivative thereof; or (ii) phenyl or a substituted derivative thereof,R.sup.2 is selected from H, C.sub.1 -C.sub.5 alkyl, halogen or NH.sub.2,R.sup.4 and R.sup.5 which are the same or different are selected fromH, NH.sub.2 or NO.sub.n where n=1 or 2, or R.sup.4 and R.sup.5 together with the pyrimidine ring form a 5-or 6-membered ring structure containing one or more heterocyclic atoms, and pharmaceutically acceptable salts thereof, exhibit the ability to deplete O.sup.6 -alkylguanine-DNA alkyltransferase (ATase) activity.
    Type: Grant
    Filed: December 15, 1995
    Date of Patent: July 27, 1999
    Assignee: Cancer Research Campaign Technology Limited
    Inventors: Thomas Brian Hamilton McMurry, Robert Stanley McElhinney, Dorothy Josephine Donnelly, Paul Murray, Christophe Carola, Rhoderick Hugh Elder, Jane Kelly, Geoffrey Paul Margison, Joseph Anthony Rafferty, Amanda Jean Watson, Mark Andrew Willington
  • Patent number: 5919732
    Abstract: There are described novel substituted 3-arylamino-6-trifluoromethyluracils of the formula I, processes for their preparation, and methods of controlling monocotyledonous and dicotyledonous harmful plants in agricultural and silvicultural crops. ##STR1## In formula I, the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are not only hydrogen, alkyl and haloalkyl, but can also have further meanings, R.sup.5 is alkyl or amino, and X is CH or N.
    Type: Grant
    Filed: February 9, 1998
    Date of Patent: July 6, 1999
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Reinhold Puttner, Jurgen Bohner, Hansjorg Krahmer
  • 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: 5912346
    Abstract: Methods and compositions for the prevention and/or inhibition of primary and secondary metastatic neoplasms are described. Individuals at a high risk of developing neoplasia and/or cancer patients undergoing conventional therapies may be treated with an effective dose of a salt of aminoimidazole carboxamide and/or of 5-amino or substituted amino 1,2,3-traizoles.
    Type: Grant
    Filed: November 10, 1997
    Date of Patent: June 15, 1999
    Assignee: Constantia Gruppe
    Inventor: Felix Wehrmann
  • Patent number: 5905070
    Abstract: A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a ?5-carboxamido or 5-fluoro!-2',3'-dideoxy-2',3'-didehydro-pyrimidine nucleoside or a ?5-carboxamido or 5-fluoro!-3'-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5' or N.sup.4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 30, 1997
    Date of Patent: May 18, 1999
    Assignee: Emory University
    Inventors: Raymond F. Schinazi, Dennis C. Liotta
  • Patent number: 5892025
    Abstract: A process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that referentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (-)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.
    Type: Grant
    Filed: July 14, 1998
    Date of Patent: April 6, 1999
    Assignee: Emory University
    Inventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
  • 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: 5883111
    Type: Grant
    Filed: July 22, 1996
    Date of Patent: March 16, 1999
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takehiko Naka, Yoshiyuki Inada
  • Patent number: 5877318
    Abstract: Disclosed is a hydroquinone derivative or a pharmaceutically acceptable salt thereof, the hydroquinone derivative being represented by formula (I): ##STR1## wherein R.sup.1 is a phenyl group which is unsubstituted or substituted with a substituent or substituents each independently selected from the group consisting of a halogen atom, a C1-4 alkyl group and a C1-4 alkoxy group;R.sup.2 is a hydrogen atom or a C1-4 alkyl group;each of R.sup.3 and R.sup.4 is independently a hydrogen atom or a C1-4 alkyl group;R.sup.5 is a hydrogen atom or a C1-4 alkyl group;each of R.sup.6, R.sup.7 and R.sup.8 is independently a hydrogen atom or a C1-4 alkyl group;P is a hydroxyl group;Q is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group;P may form together with Q an ether bond;R is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group, provided that when one of said Q and said R is an oxo group, the other is also an oxo group;X is a single bond, an --NR.sup.
    Type: Grant
    Filed: July 10, 1998
    Date of Patent: March 2, 1999
    Assignee: Japan Energy Corporation
    Inventors: Yoshiaki Isobe, Yuso Goto, Masanori Tobe, Osamu Takahashi
  • Patent number: 5869476
    Abstract: The invention relates to pyrimidinone derivatives and the pharmaceutically acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, and thus useful in treating cardiovascular diseases caused by angiotensin II.
    Type: Grant
    Filed: April 25, 1997
    Date of Patent: February 9, 1999
    Assignee: Boryung Pharmaceutical Co., Ltd.
    Inventors: Woo Hyun Paik, Ji Han Kim, Jae Hyoung Lee, Kyung Jin Jang, Kwang Jae Cho, Jae Seog Kang, Byoung Wug Yoo, Je Bum Park, Kyung Jin Kim, Kun Ja Lee
  • Patent number: 5861395
    Abstract: Novel compounds of the formula: ##STR1## are disclosed. Compounds of Formula 1.0 are represented by the compounds of formulas: ##STR2## wherein R.sup.1, R.sup.3 and R.sup.4 are each independently selected from halo. Also disclosed are methods of inhibiting farnesyl protein transferase and the growth of abnormal cells, such as tumor cells.
    Type: Grant
    Filed: September 11, 1997
    Date of Patent: January 19, 1999
    Assignee: Schering Corporation
    Inventors: Arthur G. Taveras, Alan K. Mallams, Adriano Afonso, Stacy W. Remiszewski, F. George Njoroge, Ronald Doll, Tarik Lalwani, Carmen Alvarez
  • Patent number: 5861406
    Abstract: Methods and compositions for the prevention and/or inhibition of primary and secondary metastatic neoplasms are described. Individuals at a high risk of developing neoplasia and/or cancer patients undergoing conventional therapies may be treated with an effective dose of a salt of aminoimidazole carboxamide and/or of 5-amino or substituted amino 1,2,3-traizoles.
    Type: Grant
    Filed: July 18, 1996
    Date of Patent: January 19, 1999
    Assignee: Constantia Gruppe
    Inventor: Felix Wehrmann
  • Patent number: 5849216
    Abstract: Compounds of the formula (I)R.sup.1 --(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.g --H(I)in which the symbols and indices have the following meanings:R.sup.1 is B or a straight-chain or branched alkyl radical having 1 to 22 carbon atoms (with or without an asymmetrical carbon atom) in which, in addition, it is possible for one or two non-adjacent --CH.sub.2 -- groups to be replaced by --O--, --S--, --CO--, --CO--O--, --O--CO--, --CO--S--, --S--CO--, --O--CO--O--, --CH.dbd.CH--, --C.tbd.C--, .DELTA. or --Si(CH.sub.3).sub.2 --, and in which, in addition, one or more hydrogen atoms of the alkyl radical may be substituted by F, Cl, Br or CN, or is a chiral group, for example an epoxide, a dioxolane or a cyclic lactone,--(A.sup.1).sub.a (--M.sup.1).sub.b --(--A.sup.2).sub.c (--M.sup.2).sub.d (--A.sup.3).sub.e (--M.sup.3).sub.f (--A.sup.4).sub.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: December 15, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerd Illian, Anke Kaltbeitzel, Rainer Wingen, Hubert Schlosser
  • Patent number: 5849751
    Abstract: Amides and sulphonamides of benzylamines having heterocyclic substituents are prepared by first converting the corresponding carboxylic acids into the corresponding amines and then substituting these on the amine nitrogen in a corresponding manner. The new amides and sulphonamides of benzylamines having heterocyclic substituents can be used as active compounds in medicaments, in particular in antiatherosclerotic medicaments.
    Type: Grant
    Filed: July 3, 1996
    Date of Patent: December 15, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Muller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Stefan Lohmer, Stefan Wohlfeil, Rudi Grutzmann
  • 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: 5821366
    Abstract: 1,3-Disubstituted-zanthines have therapeutic utility via TNF or phosphodiesterase inhibition.
    Type: Grant
    Filed: May 20, 1996
    Date of Patent: October 13, 1998
    Assignee: Chiroscience Limited
    Inventor: John Gary Montana
  • Patent number: 5807862
    Abstract: Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula:CORE MOIETY--(R).sub.jwherein j is an integer from one to three. The core moiety is non-cyclic or cyclic (carbocyclic or heterocyclic). R may be selected from among hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, carbocyclic or heterocyclic groups and at least one R has the formula I: ##STR1## wherein: one or two p are the integer one, otherwise p is two; and n is an integer from three to twenty; R.sub.1 is selected from the group consisting of substituted and unsubstituted CH.sub.2 ; NR.sub.3, R.sub.3 being hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or C.sub.(1-20) hydroxyalkyl, or carbocyclic or heterocyclic group; O; --CHR.sub.4 O--, R.sub.4 being substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, or R.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 15, 1998
    Assignee: Cell Therapeutics, Inc.
    Inventors: J. Peter Klein, Alistair J. Leigh, Gail E. Underiner, Anil M. Kumar
  • Patent number: 5807863
    Abstract: This invention relates to novel 2-(4-pyrazolyloxy-pyrimidin-5-yl) acetic acid derivatives of formula I ##STR1## wherein R.sub.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.3-6 cycloalkyl, or di-C.sub.1-4 alkylamino,R.sub.2 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, or di-C.sub.1-4 alkyl-amino,R.sub.3 is hydrogen or methyl,R.sub.4 is aryl, aryl-C.sub.1-4 alkyl, heteroaryl, or heteroaryl-C.sub.1-4 alkyl, wherein each of the aromatic rings may be optionally substituted; andX is CH or nitrogen;the use of such compounds for the control of phytopathogens, compositions for facilitating such use, and the preparation of the compounds of formula I.
    Type: Grant
    Filed: September 19, 1996
    Date of Patent: September 15, 1998
    Assignee: Novartis Corporation
    Inventors: Martin Eberle, Clemens Lamberth, Fritz Schaub
  • Patent number: 5801182
    Abstract: Compounds and pharmaceutical compositions, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, have the formula:CORE MOIETY --(R).sub.jIn these compounds, j is an integer from one to three; the core moiety is a cyclic core, the cyclic core being non-cyclic or at least one five- to seven-member non-heterocyclic ring or heterocycle; and R is selected from the group consisting of amine, hydrogen, halogen, hydroxyl, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, cyclic or heterocyclic group or formula I. At least one R having formula I: ##STR1## In formula I, n is an integer from four to twenty; and each R.sub.1 or R.sub.2 is independently hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or cyclic or heterocyclic group.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 1, 1998
    Assignee: Cell Therapeutics, Inc.
    Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar, Lance H. Ridgers
  • Patent number: 5783576
    Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: July 21, 1998
    Assignee: Boehringer Ingelheim KG
    Inventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
  • Patent number: 5783521
    Abstract: Substituted pyridylsalicylaldehyde and --salicylic acid derivatives of the formula I ##STR1## where R is a formyl group, a CO.sub.2 H group or a radical which can be hydrolyzed to CO.sub.2 H and the other substituents have the following meanings:R.sup.2 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.13, R.sup.13 being hydrogen or halogen or together with R.sup.3 forming a 3- to 4-membered alkylene or alkenylene chain in which at least one methylene group is replaced by oxygen;R.sup.3 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio, or R.sup.3 is linked with R.sup.13 as indicated above to give a 5- or 6-membered ring;Y is oxygen or sulfur;Py is a substituted pyridine ring, are described.
    Type: Grant
    Filed: November 1, 1994
    Date of Patent: July 21, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim Rheinheimer, Uwe Josef Vogelbacher, Ernst Baumann, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 5780473
    Abstract: Compounds of the formula ##STR1## inhibit the activity of endothelin.
    Type: Grant
    Filed: July 25, 1996
    Date of Patent: July 14, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: Natesan Murugesan, Joel C. Barrish, Philip D. Stein
  • Patent number: 5776932
    Abstract: 1,3,5-trisubstituted indazole derivatives of the formula ##STR1## wherein R1 is H, (b) a C.sub.1-6 straight or branched, substituted or unsubstituted alkyl residue, (c) a C.sub.3-7 cycloalkyl residue, (d) an unsustituted or substituted phenyl, naphthyl, anthranyl, or fluorenyl residue, (e) a quinolin-2-ylmethoxy, or pyridin-2-ylmethoxy residue; X is O, or a --NH, --NH--(C.dbd.O)--NH--, --NH--(C.dbd.O)--O--, --NH--(C.dbd.O)--, or --NH--CH.sub.2 --(C.dbd.O)-- residue; Y is O, or S; R.sub.2 is H; Z is a SO, SO.sub.2, --(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --O--, --O--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--, --(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--NH--, --NH--(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CHOH--, --CHOH--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CH.dbd.CH--, or --CH.dbd.CH--(CH.sub.2).sub.
    Type: Grant
    Filed: March 20, 1997
    Date of Patent: July 7, 1998
    Assignee: Arzneimittelwerk Dresden G.m.b.H.
    Inventors: Rudolf Schindler, Ilona Fleischhauer, Istvan Szelenyi
  • Patent number: 5777118
    Abstract: Cyclic acetals of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 and R.sup.2 are hydrogen, unsubstituted or substituted alkyl or phenyl; additionally R.sup.1 and R.sup.2 together are an unsubstituted or substituted C.sub.2 -C.sub.6 -alkylene chain;Y is oxygen or sulfur;A has the meaning as given in claim 1;a process for preparing the acetals I and their use for the production of crop protection compositions are described.
    Type: Grant
    Filed: July 12, 1996
    Date of Patent: July 7, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Joachim Rheinheimer, Uwe Josef Vogelbacher, Ernst Baumann, Hartmann Konig, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
  • Patent number: 5760038
    Abstract: Compounds of the formula ##STR1## in which the symbols are as defined herein, inhibit the activity of endothelin.
    Type: Grant
    Filed: February 6, 1995
    Date of Patent: June 2, 1998
    Assignee: Bristol-Myers Squibb Company
    Inventors: Natesan Murugesan, Joel C. Barrish, Philip D. Stein
  • Patent number: 5753595
    Abstract: Herbicidal 3-(substituted benzoxazol-7-yl) and 3-(substituted benzothiazol-7-yl)-1 -substituted-6-trifluoromethyl-2,4-(1H,3H)pyrimidinediones, compositions containing them, and methods of using them to control undesired plant growth are disclosed, as are novel intermediates used in the preparation of these compounds. The herbicidal compounds of the present invention are defined by the following generic structure: ##STR1## in which R is selected from a variety of substituents, including halogen, alkyl, alkenyl, alkynyl, phenyl, phenylalkyl, alkylphenylalkyl, haloalkyl, hydroxy, alkoxy, hydroxyalkyl, halophenyl, halophenylalkyl, alkoxyphenyl, sulfhydryl, alkylthio, piperidinyl, alkylamino, alkoxyalkyl, phenoxy, amino, alkylsulfonylamino, phenylsulfonylamino, and carboxy; R.sup.1 is alkyl or amino; R.sup.
    Type: Grant
    Filed: July 31, 1996
    Date of Patent: May 19, 1998
    Assignee: FMC Corporation
    Inventors: Scott D. Crawford, Lester L. Maravetz, George Theodoridis
  • Patent number: 5750469
    Abstract: Substituted lactic acid derivatives having an N-organic radical in the .beta.-position, of the formula I ##STR1## where substituents R to R.sup.5, X and Y have the meanings mentioned in the description and N is one of the radicals:a) --N.sub.3, --NC, --NCS or --NCOb) ##STR2## where R.sup.14 and R.sup.15 have the meanings described in the descriptionc) ##STR3## in which R.sup.16 is hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl or unsubstituted or substituted phenyl; andB is a group ##STR4## OR.sup.19 or --NR.sup.14 R.sup.15, where R.sup.14, R.sup.15, R.sup.17 and R.sup.19 have the meanings described in the description, or ##STR5## where R.sup.14 and R.sup.15.sub.1, have the abovementioned meanings; or ##STR6## where R.sup.20 and R.sup.21, which can be identical or different, are: hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or phenyl, where the organic radicals can in each case be substituted;or R.sup.20 and R.sup.21 together form an unsubstituted or substituted C.sub.4 -C.sub.
    Type: Grant
    Filed: March 1, 1996
    Date of Patent: May 12, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Matthias Gerber, Wilhelm Rademacher, Helmut Walter, Karl-Otto Westphalen
  • Patent number: 5747423
    Abstract: The novel 6-thienyl pyridines and 4-thienyl pyrimidines of formula I: ##STR1## (A, R.sub.1 to R.sub.5 and Z are defined in the specification) show selective herbicidal activity.The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.
    Type: Grant
    Filed: July 15, 1996
    Date of Patent: May 5, 1998
    Assignee: American Cyanamid Company
    Inventors: Stefan Scheiblich, Thomas Maier, Helmut Siegfried Baltruschat, Joseph Luke Pont
  • Patent number: 5747500
    Abstract: Novel 2,4-pyrimidinedione compounds, and pharmaceutically acceptable salts thereof which possess good antiviral activities, and specifically represented by the following formula(I): ##STR1## wherein: R.sup.1 represents an unsubstituted or substituted allyl group represented by CH.sub.2 CH.dbd.CR.sup.5 R.sup.6 or an unsubstituted or substituted propargyl group represented by CH.sub.2 C.tbd.CR.sup.7 wherein R.sup.5, R.sup.6 and R.sup.7 are each independently a hydrogen atom; a methyl group optionally substituted with a halogen atom, or a C.sub.1-10 carbonyloxy, hydroxy, azido, cyano, optionally substituted amino, optionally substituted phosphonyl, optionally substituted phenyl, C.sub.3-10 heteroaryl, C.sub.1-3 alkoxy or benzyloxy radical; a C.sub.2-10 alkyl or alkenyl group; a cyclopropyl group; an optionally substituted phenyl group; a C.sub.3-10 heteroaryl group; a C.sub.1-10 ester group; or an optionally substituted C.sub.1-10 alkylamide group;R.sup.2 represents a halogen atom, an optionally substituted C.
    Type: Grant
    Filed: June 18, 1996
    Date of Patent: May 5, 1998
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jong-Chan Son, III-Young Lee, Byung-II Bae, Jeong-Sik Han, Joong-Kwon Choi, Yung-Bok Chae