Carbocyclic Ring Containing Patents (Class 544/321)
  • Patent number: 6635636
    Abstract: The invention concerns novel substituted 6-benzyl-4-oxopyrimidines and pharmaceutically acceptable salts thereof. These compounds inhibit reverse transcriptase encoded by human immunodeficiency virus (HIV), and are useful to prevent and treat HIV infection and acquired immune deficiency syndrome (AIDS). Pharmaceutical compositions containing the compounds and a method of use of the present compounds and other agents for the treatment of AIDS and viral infection by HIV are also envisaged.
    Type: Grant
    Filed: May 1, 2001
    Date of Patent: October 21, 2003
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Marino Artico, Paolo La Colla
  • Patent number: 6632821
    Abstract: Pyrimidines of formula I in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or tri-alkyl-silyl, formyl or alkoxycarbonyl, wherein R1 groups are unsubstituted or substituted as defined in the specification; R2 represents phenyl, cycloalkyl or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which are unsubstituted or substituted; R3 represents hydrogen, halogen or alkyl, alkoxy, alkylthio, alkylamino or dialkylamino; which are unsubstituted or substituted; R4 represents hydrogen or alkyl, alkenyl or alkynyl; which are unsubstituted or substituted; and X represents O, S, NR5 or a single bond, wherein R5 represents hydrogen or alkyl; or R1 and R5 together with the interjacent nitrogen ato
    Type: Grant
    Filed: June 12, 2001
    Date of Patent: October 14, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus-Juergen Pees, Waldemar Pfrengle, Gavin Heffernan
  • Patent number: 6617332
    Abstract: The invention relates to novel natural product derivatives of the formula (I), to processes for their preparation, to pharmaceutical compositions comprising them and to their use in the treatment of disorders in humans or animals: in which R1, D, X, Y and Z are defined as in claim 1.
    Type: Grant
    Filed: April 11, 2001
    Date of Patent: September 9, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Brands, Mazen Es-Sayed, Dieter Häbich, Siegfried Raddatz, Joachim Krüger, Rainer Endermann, Reinhold Gahlmann, Hein-Peter Kroll, Frank-Ulrich Geschke, Armin de Meijere, Vladimir N. Belov, Victor Sokolov, Sergej Kozhushkov, Markus Kordes
  • Patent number: 6610698
    Abstract: Selected novel substituted pyrimidine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: April 3, 2002
    Date of Patent: August 26, 2003
    Assignee: Amgen, Inc.
    Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo
  • Patent number: 6596719
    Abstract: The present invention relates to novel bis-sulfonamides represented, for example, by formula I below and a pure diastereomer, a mixture of diastereomers, a diastereomeric racemate, a mixture of diastereomeric racemates and meso-forms and a pharmaceutically acceptable salt thereof, wherein R1 represents aryl; aryl-lower alkyl; aryl-lower alkenyl; heteroaryl; or heteroaryl-lower alkyl; and R2 represents lower alkyl; trifluoromethyl; lower alkoxy-lower alkyl; lower alkenyl; lower alkynyl; aryl; aryl-lower alkyl; aryl-lower alkenyl; heterocyclyl; heterocyclyl-lower alkyl; heteroaryl; heteroaryl-lower alkyl; cycloalkyl; or cycloalkyl-lower alkyl. The present invention also relates to a process for manufacturing those compounds, pharmaceutical compositions containing one or more of those compounds as endothelin antagonists, and a method of treating a subject having a disorder involving endothelin with the compounds of the invention.
    Type: Grant
    Filed: August 16, 2001
    Date of Patent: July 22, 2003
    Assignee: Actelio Pharmaceuticals Ltd.
    Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli
  • Patent number: 6586441
    Abstract: The invention relates to cyclic heteroaromatic compounds, containing at least one nitrogen atom, and to their use in the manufacture of medicaments for the treatment of diseases, related to adenosine receptor modulators, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses, hypoxia, ischaemia, seizure, substance abuse, sedation and they may be active as muscle relaxants, antipsychotics, anti epileptics, anticonvulsants and cardiaprotective agents.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: July 1, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Edilio Maurizio Borroni, Gerda Huber-Trottmann, Gavin John Kilpatrick, Roger David Norcross
  • Patent number: 6573377
    Abstract: This invention provides compounds having antitumor effect, namely a compound represented by the following formula (I) or (Ia) having various substituents in which G and G1 are condensed tricyclic heterocyclic rings or salts thereof, and a compound represented by the following formula (Ib) having various substituents or salts thereof.
    Type: Grant
    Filed: January 24, 2001
    Date of Patent: June 3, 2003
    Assignee: Daiichi Pharmaceuticals Co., Ltd.
    Inventors: Akio Ejima, Satoru Ohsuki, Hitoshi Ohki, Hiroyuki Naito, Chie Makino
  • Patent number: 6548511
    Abstract: This invention provides an insecticidal and acaricidal agent which can control various insanitary insects and insects, mites and eggs thereof which are harmful to the agricultural and horticultural products, at a low chemical concentration. The insecticidal and acaricidal agent of this invention contains an anilinopyrimidinone derivative represented by the following general formula (I) as an active ingredient.
    Type: Grant
    Filed: February 9, 2000
    Date of Patent: April 15, 2003
    Assignees: Sagami Chemical Research Center, Mitsubishi Chemical Corporation
    Inventors: Kenji Hirai, Takeshi Yoshizawa, Sachiko Itoh, Natsuko Okano, Yuriko Nagata, Chikako Ota, Toshiki Fukuchi, Keiko Yoshiya
  • Patent number: 6518425
    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: May 15, 2000
    Date of Patent: February 11, 2003
    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: 6509339
    Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-6alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R3 is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula -Alk-R4, -Alk-NR5R6, 1-R6-4-piperidinyl, Alk-X—R7, -Alk-Y—C(═O)—R9, or -Alk-Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; R4 is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Ar-, di(Ar)methyl, Ar-oxy- or Het1; R5 is hydrogen or C1-6alkyl; R6 is Het2; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, Ar or Het2; X is O, S, SO2 or NR8; said R8 being hydrog
    Type: Grant
    Filed: August 20, 2001
    Date of Patent: January 21, 2003
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Paul René Marie Bosmans, Christopher John Love, Marc Gustaaf Celine Verdonck, Joannes Adrianus Jacobus Schuurkes
  • Patent number: 6500952
    Abstract: The invention relates to the preparation of compounds (I) in which A=H or acyl and R1, R21, R3, R, n, X, Y and Z are as defined in claim 1 by halogenation and rearrangement of compounds (II) (optionally salt) to give compounds (III) a) ammonolysis of (III) to (IV), reduction of the nitro group and reaction with carbamate (salts) (VI) of the formula Ar—OCO—N(M)—Het, where Ar=phenyl, M=H or cation and Het=heterocycle from formula (I), to give compounds (I) (A=H), or b) ammonolysis of (III) to (IV), reaction with carbamate (salt) (VI) and reduction of resulting compounds (VII) at the NO2 group to give compounds (I) (A=H), or c) reaction of (III) with cyanates and amines (VIII) of the formula HNR3—Het and reduction of the resulting compound (VII) at the NO2 group to give compounds (I) (A=H) and optional acylation if A is to be other than H.
    Type: Grant
    Filed: September 18, 2000
    Date of Patent: December 31, 2002
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Jan Vermehren, Lothar Willms
  • Patent number: 6498253
    Abstract: Compounds of the formula (I) and salts thereof in which W1, W2, R, n, R1, R2, R4, X, Y and Z are as defined in claim 1 and R3 is an acyl radical, are suitable as herbicides and plant growth regulators. The herbicides can be prepared by the process variants from claim 5, the novel intermediate products (II), (IV), (VI) and (VIII)* of claims 9 and 10 being employed.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: December 24, 2002
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
  • Patent number: 6495558
    Abstract: The invention relates to inhibitors of kinases, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making kinase inhibitor compounds, methods of inhibiting kinase activity, and methods for treating disease or disease symptoms.
    Type: Grant
    Filed: March 21, 2000
    Date of Patent: December 17, 2002
    Assignee: Amgen Inc.
    Inventors: David M. Armistead, Jean E. Bemis, Daniel Elbaum, Gregory J. Habgood, Perry M. Novak, Joseph J. Nunes, Leticia M. Toledo-Sherman
  • Patent number: 6489333
    Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
    Type: Grant
    Filed: April 9, 2001
    Date of Patent: December 3, 2002
    Assignee: Bristol - Meyers Squibb Pharma Company
    Inventors: William J. Pitts, Prabhakar K. Jadhav
  • Patent number: 6448256
    Abstract: The invention relates to prodrugs of N-substituted derivatives of 6-aminouracils, 6-aminoisocytosines, guanines, and 2-aminoadenines. The N-linked substituents include an ester group that is cleaved upon administration into a subject to yield a substituent having a terminal hydroxyl group. Pharmaceutical compositions including these compounds, and methods for treating Gram-positive bacterial infections using these compounds, are also disclosed.
    Type: Grant
    Filed: May 23, 2000
    Date of Patent: September 10, 2002
    Assignee: University of Massachusetts
    Inventors: George E. Wright, Neal C. Brown, Chengxin Zhi
  • Patent number: 6440984
    Abstract: There are provided compositions and methods comprising compounds of formula I: wherein R1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.
    Type: Grant
    Filed: November 29, 2000
    Date of Patent: August 27, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: William Wakefield Wood, Linda Fleming, Salvatore John Cuccia
  • Patent number: 6440986
    Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or
    Type: Grant
    Filed: December 27, 2000
    Date of Patent: August 27, 2002
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc René De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
  • Patent number: 6432963
    Abstract: Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1CO, CONR1, C═N—OR1 or a bond, Y: a lower alkylene group which may be substituted by OR1 or —NHR1, or a bond, Z: O, NR2 or a bond, A: H, or a lower alkyl which may have a substituent, a —CO-lower alkyl which may have a substituent, an aryl which may have a substituent, a heteroaryl which may have a substituent, a cycloalkyl which may have a substituent or a nitrogen-containing saturated heterocyclic group which may have a substituent, B: an aryl which may have a substituent or a heteroaryl group which may have a substituent, R1, R2: H, a lower alkyl or a —CO-lower alkyl group].
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: August 13, 2002
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Hisamichi, Ryo Naito, Souichirou Kawazoe, Akira Toyoshima, Kazuhito Tanabe, Eiichi Nakai, Atsushi Ichikawa, Akiko Orita, Makoto Takeuchi
  • Patent number: 6423720
    Abstract: This invention discloses compounds, and pharmaceutically acceptable salts, solvates and prodrugs thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii, Toxoplasma gondii, Mycobacterium tuberculosis, and Mycobacterium avium. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed. The compounds include 5-thiapyrimidines.
    Type: Grant
    Filed: February 1, 2001
    Date of Patent: July 23, 2002
    Assignee: Duquesne University of the Holy Ghost
    Inventor: Aleem Gangjee
  • Patent number: 6417180
    Abstract: The invention relates to antimicrobial compounds which interact with zinc in a zinc finger of a bacterial DNA polymerase, methods of screening for such compounds, and methods of using such compounds to inhibit polymerase activity or bacterial growth.
    Type: Grant
    Filed: October 7, 1998
    Date of Patent: July 9, 2002
    Assignee: University of Massachusetts
    Inventors: Neal C. Brown, Marjorie H. Barnes, George E. Wright
  • Patent number: 6417141
    Abstract: The invention relates to novel aminouracils of the general formula (I) in which, Q, R1, R2, R3, R4, R5, R6 and R7 are each as defined in the description, to their use as herbicides and to novel intermediates.
    Type: Grant
    Filed: January 21, 1998
    Date of Patent: July 9, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Otto Schallner, Markus Dollinger, Hans-Joachim Santel
  • Patent number: 6410482
    Abstract: (Het)Arylsulfonylureas having an imino function, their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which A is a (hetero)aromatic or heterocyclic bridge linked to the group SO2 by a direct bond, or via O, S, NH, CH2 or via alkylated NH or alkylated methylene, B is a group having an imino-containing fragment N═C—N, N═C—S, N═C—O or N═C—C which is linked to A by one of the nitrogen atoms of the fragment, R═H or an aliphatic radical, W═O or S and X, Y and Z are as defined in claim 1 are suitable as herbicides and plant growth regulators. The preparation is carried out for example similarly to known processes via novel intermediates of the formula (XII) (cf.
    Type: Grant
    Filed: May 13, 1997
    Date of Patent: June 25, 2002
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 6410483
    Abstract: Compounds of the formula (I) and salts thereof in which R1-R9, W and A are as defined in formula (I) of claim 1 are suitable as herbicides and plant growth regulators. They can be prepared by processes according to claim 5 via intermediates according to claim 9, some of which are novel.
    Type: Grant
    Filed: January 21, 1998
    Date of Patent: June 25, 2002
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Klaus Lorenz, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 6399620
    Abstract: There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G  (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.
    Type: Grant
    Filed: June 29, 2000
    Date of Patent: June 4, 2002
    Assignee: Aventis Pharma S.A.
    Inventors: Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
  • Patent number: 6387914
    Abstract: The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.
    Type: Grant
    Filed: April 24, 2001
    Date of Patent: May 14, 2002
    Assignee: ARYx Therapeutics
    Inventors: Pascal Druzgala, Peter G. Milner
  • Publication number: 20020049321
    Abstract: Sulfonylureas of the general formula I 1
    Type: Application
    Filed: June 14, 2001
    Publication date: April 25, 2002
    Inventors: Horst Mayer, Gerhard Hamprecht, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
  • Patent number: 6365739
    Abstract: Isocyanates of the formula (I) in which X and Y are defined as in formula (I) of claim 1 can be prepared by reacting a compound of the formula (II) or its salts in which X and Y are defined as in formula (I), with 1 to 6 mol of phosgene per mole of compound of the formula (II), in the presence of 2 to 3.5 molar equivalents of a base per mole of compound of the formula (II) and in the presence of an aprotic organic solvent at a reaction temperature in the range from −30 to +60° C. to give the compound of the formula (I). The compounds (I) can be converted by reaction with nucleophiles to give addition products, such as carbamates, ureas and sulfonylureas and corresponding products, e.g. herbicidal sulfonylureas.
    Type: Grant
    Filed: July 21, 1999
    Date of Patent: April 2, 2002
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Mark James Ford, Stephen Lachhein
  • Patent number: 6352993
    Abstract: The present invention relates to novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof which possess an excellent anti-secretory activity, pharmaceutical compositions containing the same as an active ingredient, their novel intermediates, and processes for the preparation thereof wherein: when A is piperidin-1-yl or —NH—B, wherein B is C3-C4 alkyl, C3-C4 alkenyl, C3-C7 cycloalkyl, C1-C3 alkoxyethyl, phenylethl which may be substituted or unsubstituted, 3-trifluoromethylphenylmethyl, 1-naphthylmethyl, 4-methylthiazol-2-yl or 4-phenylthiazol-2-yl, R1 is hydrogen or methyl; and R2, R3, R4 and R5 are hydrogen; or when A is a group of formula (II); when R1 is hydroxymethyl or C1-C3 alkoxymethyl, R2, R3, R4, R5 and R6 are hydrogen; and R7 is hydrogen or halogen; or when R1 is hydrogen or methyl, R7 is hydrogen or halogen; and one or two of R2, R3, R4, R5 and R6 is hydroxy, methoxy, or a group of formula (III) wherein Z is C1-C4 alkyl, substituted or unsubstituted C1-C4
    Type: Grant
    Filed: September 24, 1999
    Date of Patent: March 5, 2002
    Assignee: Yuhan Corporation
    Inventors: Jong Wook Lee, Bong Yong Lee, Chang Seop Kim, Seung Kyu Lee, Keun Seog Song, Song Jin Lee, Woo Jeon Shim, Man Soon Hwang
  • Patent number: 6342504
    Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.
    Type: Grant
    Filed: December 21, 1999
    Date of Patent: January 29, 2002
    Assignee: Corvas International, Inc.
    Inventors: Terence Kevin Brunck, Susan Y. Tamura, Joseph Edward Semple, Robert John Ardecky, Yu Ge, William Charles Ripka
  • Patent number: 6337335
    Abstract: Compounds of formula (1) are described: and the salts, solvates, hydrates and N-oxides thereof, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings given in claim 1. The compounds are selective inhibitors of protein kinases, especially src-family protein kinases and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.
    Type: Grant
    Filed: October 20, 1999
    Date of Patent: January 8, 2002
    Assignee: Celltech Therapeutics Limited
    Inventors: Martin Clive Hutchings, Peter David Davis, David Festus Charles Moffat
  • Patent number: 6337306
    Abstract: Phenoxyacetic acid derivatives of the formula: wherein R1, R2, Xn and A are as defined herein, and a process for preparing the derivatives. The derivatives are used as herbicides.
    Type: Grant
    Filed: November 5, 1999
    Date of Patent: January 8, 2002
    Assignee: Rhone-Poulenc Agro
    Inventors: Norio Sasaki, Atsushi Go, Hideshi Mukaida, Yukiko Oe
  • Patent number: 6331506
    Abstract: Disubstituted methylidenehydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which R1 to R6, W, X, Y, Z are as defined in claim 1 and the group R2R3C is a carbon atom which is subsituted by at least one electron-withdrawing radical R2 or R3 are suitable as herbicides and plant growth regulators. They can be prepared in accordance with known processes via intermediates, some of which are novel.
    Type: Grant
    Filed: September 16, 1998
    Date of Patent: December 18, 2001
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
  • Patent number: 6329323
    Abstract: This invention relates to aminosulfonylureas possessing a high herbicidal activity, a process for their preparation and their application to control control weeds in agriculture. Aminosulfonylureas of this invention have the following formula (I): wherein R, R1, R2, R3, R4, R5, and R6 are described in the specification.
    Type: Grant
    Filed: October 21, 1999
    Date of Patent: December 11, 2001
    Assignee: Isagro Ricerca S.r.l.
    Inventors: Franco Bettarini, Sergio Massimini, Giovanni Meazza, Giampaolo Zanardi, Domenico Portoso, Ernesto Signorini
  • Patent number: 6323210
    Abstract: Novel derivatives of 5-thia- and 5-selenopyrimidinone are sound to inhibit the enzyme glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). Novel intermediates of these compounds are also disclosed. A novel method of preparing such compounds is also disclosed, as well as methods and compositions for employing the compounds as antiproliferative agents.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: November 27, 2001
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer, Judith G. Deal
  • 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: 6277845
    Abstract: Compounds of the formula wherein the substituents are as defined in the application and their pharmaceutically acceptable acid and base salts thereof which are useful for preventing loss of bone matrix.
    Type: Grant
    Filed: July 7, 2000
    Date of Patent: August 21, 2001
    Assignee: Aventis Pharma S.A.
    Inventors: Denis Carniato, Thomas R. Gadek, Francois Goubet, Jean-Francois Gourvest, Jochen Knolle, Robert S. McDowell, Karl-Heinz Scheunemann
  • Publication number: 20010011094
    Abstract: This invention concerns the use of the compounds of formula 1
    Type: Application
    Filed: December 27, 2000
    Publication date: August 2, 2001
    Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
  • 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: 6252076
    Abstract: The present invention relates, first to a process for preparation of 5,6-dimethyl-2-(4-fluorophenylamino)-4-(1-methyl-1,2,3,4-tetrahydroisoquinolin-2-yl)pyrimidine represented by formula (I) and its acid addition salts, second, to a process for preparation of an intermediate for preparing the compound (I), and, third, to a novel intermediate compound. More specifically, the present invention relates, first, to a process for preparation of 5,6-dimethyl-2-(4-fluorophenylamino)-4-(1-methyl,1,2,3,4-tetrahydroisoquinolin-2-yl)pyrimidine represented by formula (I), and its acid addition salts by reacting a pyrimidine derivative represented by formula (II-A), in which Hal represents a halogen, with 1-methyl-1,2,3,4-tetrahydroisoquinoline represented by formula (III), second, to a process for preparing of the pyrimidine derivative of formula (II-A) and the compound of formula (III); and, third, to a novel intermediate compound including the pyrimidine derivative of formula (II-A).
    Type: Grant
    Filed: September 21, 2000
    Date of Patent: June 26, 2001
    Assignee: Yuhan Corporation
    Inventors: You Wha Hong, Young Nam Lee, Hong Bae Kim
  • 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: 6242454
    Abstract: This invention is directed to benzamidine derivatives substituted by amino acid and 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: September 9, 1999
    Date of Patent: June 5, 2001
    Assignee: Berlex Laboratories Inc.
    Inventors: Monica Kochanny, Raju Mohan, Michael M. Morrissey, Howard P. Ng, Weiya Yun
  • Patent number: 6228808
    Abstract: Compounds of the formula (I) or salts thereof in which R1, R3=H, (subst.) hydrocarbon radical (HC) or (subst.) heterocyclyl which, including substituents, have 1-30 carbon atoms, R2=R0—Q0—, in which R0=H, (subst.) HC or (subst.) heterocyclyl radical, in each case having 1-30 carbon atoms including substituents, and Q0=a direct bond or —O—, —SO2-, —NH—, —N[(C1-C6)alkyl]-, —CO—, —CO—NH— or —O—CO—NH—; R4=H, halogen, NO2, CN, (C1-C4)alkyl, (C1-C4)alkoxy, [(C1-C4)alkyl]carbonyl or [(C1-C4)alkoxy]carbonyl, where each of the last four radicals may be halogenated; R5=H or (C1-C4)alkyl; Q=O or NR*; R*=H.
    Type: Grant
    Filed: October 30, 1998
    Date of Patent: May 8, 2001
    Assignee: Hoechst Schering AgrEvo GmbH
    Inventors: Heinz Kehne, Lothar Willms, Christian Waldraff, Hansjörg Dietrich, Hermann Bieringer, Christopher Rosinger, Thomas Auler
  • Patent number: 6225260
    Abstract: The present invention provides a compound comprising a quaternary ammonium salt of a sulfonylurea having the formula wherein R1 is a substituted or unsubstituted phenyl, heterocyclic ring, or phenoxy, or —N(CH3)(SO2CH3); R2 is H or CH3; R3 is a substituted or unsubstituted pyrimidine or a substituted or unsubstituted triazine; R4 and R5 are independently unsubstituted or hydroxy substituted linear or branched C1-C4 alkyls, —(CH2CH2O)mCH2CH2OH, or —(CH2CHCH3O)mCH2CHCH3OH where m is 1 to 10; R6 is a substituted or unsubstituted benzyl, ethylbenzyl, naphthylmethyl, or linear or branched C1-C22 alkyl; R7 is a substituted or unsubstituted, linear or branched C8-C22 alkyl or —R13(O)n(C6H5)R14 where n is 0 or 1; R13 is a substituted or unsubstituted C1-C8 alkyl or C1-C8 alkoxyalkyl; and R14 is a substituted or unsubstituted, linear or branched C1-C12 alkyl. Also, a method of preparing a quaternary ammonium salt of a sulfonylurea is provided.
    Type: Grant
    Filed: May 20, 1999
    Date of Patent: May 1, 2001
    Assignees: Lonza Inc., E. I. DuPont de Nemours and Company
    Inventors: Robert D. Wysong, Chia-Chung Chen, Chuen-Ing Tseng, Arturo A. Tirol
  • Patent number: 6221871
    Abstract: Disclosed are compounds of the formula: where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR′ where R′ is an organic or inorganic substituent; R is hydrogen or an alkyl group; R1, X, Y, Z and T are organic or inorganic substituents; and R2 and R3 represent hydrogen or organic substituents; or NR2R3 together represents a heterocyclic ring system; and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
    Type: Grant
    Filed: June 11, 1999
    Date of Patent: April 24, 2001
    Assignee: Neurogen Corporation
    Inventors: Jun Yuan, Andrew Thurkauf
  • Patent number: 6200984
    Abstract: A compound of the general formula I: is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions, processes for preparing the compounds and methods of treatment are also disclosed.
    Type: Grant
    Filed: October 5, 1998
    Date of Patent: March 13, 2001
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Allen B. Reitz, James J. McNally, Pauline Sanfilippo
  • Patent number: 6197779
    Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 or
    Type: Grant
    Filed: March 25, 1999
    Date of Patent: March 6, 2001
    Assignee: Janssen Pharmaceutica, Inc.
    Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc René De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
  • Patent number: 6174901
    Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: January 16, 2001
    Assignee: Amgen Inc.
    Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
  • Patent number: 6172005
    Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation and Q, W, X, Y, Z, and R1 through R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: January 9, 2001
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Thomas P. Selby
  • Patent number: 6172066
    Abstract: This invention is directed to dihydropyrimidine compounds 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 the 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: January 9, 2001
    Assignee: Synaptic Pharmaceutical Corporation
    Inventors: Dhanapalan Nagarathnam, Wai C. Wong, Shou Wu Miao, Michael A. Patane, Charles Gluchowski
  • Patent number: 6162925
    Abstract: The present invention is directed to anti-bacterial and anti-tumor agents and the synthesis thereof.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: December 19, 2000
    Assignee: Research Corporation Tech., Inc.
    Inventors: Robert M. Williams, Chenguang Yuan