Tricyclo Ring System Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.03)
  • Patent number: 6255306
    Abstract: The present invention relates to compounds of the formula
    Type: Grant
    Filed: August 11, 1998
    Date of Patent: July 3, 2001
    Inventor: John E. Macor
  • Patent number: 6251905
    Abstract: Tricyclic compound of the formula: wherein ring A is a nitrogen-containing heterocyclic ring, having two nitrogen atoms as the hetero-atoms, which is optionally substituted with oxo or thioxo; ring Q may optionally be substituted; Y is an optionally substituted hydrocarbon group, an optionally substituted hydroxyl group or an optionally substituted mecapto group, excluding for methyl group as Y; R1 is a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group or an acyl group, or a salt thereof, having excellent PDGF-inhibiting activities, antihypertensive activities, activities of ameliorating renal diseases and activities of lowering lipid level.
    Type: Grant
    Filed: January 21, 1999
    Date of Patent: June 26, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Muneo Takatani, Yumiko Shibouta, Kiminori Tomimatsu, Tetsuji Kawamoto
  • Patent number: 6245766
    Abstract: A method for treating a psychiatic condition or disorder selected from anxiety disorders such as panic disorder, posttraumatic stress disorder and phobias, psychotic episodes of anxiety, anxiety associated with psychosis, psychotic mood disorders such as severe major depressive disorder and mood disorders associated with psychotic disorders such as acute mania or depression associated with bipolar disorder, schizophrenia, behavioral manifestations of mental retardation, conduct disorder or autistic disorder, dementias such as dementias of the Alzheimer's type, and dyskinesias such as drug induced and neurodegeneration based dyskinesias in a mammal, including a human, comprising administering to said mammal a pharmaceutically effective amount of a compound of the formula or a pharmaceutically acceptable acid addition salt thereof, wherein n, X, Y and Ar are as defined above.
    Type: Grant
    Filed: December 18, 1998
    Date of Patent: June 12, 2001
    Assignee: Pfizer Inc
    Inventor: Eric J. Watsky
  • Patent number: 6228865
    Abstract: Novel compounds of the formula: are disclosed. In Formula 1.0 a represents N or NO, R1 and R3 are halo, R2 and R4 are independently H or halo provided that at least one is H, X is C, CH or N, and T represents a five or six membered heterocycloalkyl ring having one or two heteroatoms selected from S or O. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
    Type: Grant
    Filed: November 23, 1999
    Date of Patent: May 8, 2001
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Carmen Alvarez, Tarik Lalwani, Yi-Tsung Liu
  • Patent number: 6214828
    Abstract: Novel compounds, such as: are disclosed. Also disclosed are methods for inhibiting the abnormal growth of cells, for inhibiting farnesyl protein transferase and for treating cancers using the novel compounds.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: April 10, 2001
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Joseph M. Kelly, Alan K. Mallams, F. George Njoroge, Stacy W. Remiszewski, Arthur G. Taveras
  • Patent number: 6214827
    Abstract: Novel compounds of Formula are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
    Type: Grant
    Filed: June 23, 1998
    Date of Patent: April 10, 2001
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, John J. Baldwin, Ronald J. Doll, Ge Li, Alan K. Mallams, F. George Njoroge, Dinanath F. Rane, John C. Reader, Randall R. Rossman
  • Patent number: 6214816
    Abstract: The compounds are N-substituted azaheterocyclic compounds of formula I wherein R1 and R2 independently are hydrogen, halogen, trifluoromethyl, hydroxy, C1-6-alkyl or C1-6-alkoxy; and Y is >N—CH2— wherein only the underscored atom participates in the ring system; and X is —C(R6R7)—, —CH2CH2—, —CH═CH—CH2—, —CH2—CH═CH—, —CH2—(C═O)—, —(C═O)—CH2—, —CH2CH2CH2—, —CH═CH—, CH(R10)CH2—, —CH2CH(R10) or —(C═O)— wherein R6 and R7 independently are hydrogen or C1-6-alkyl and wherein R10 is C1-6-alkyl or phenyl; and r is 0, 1 or 2; and Z is selected from wherein A is —CH2—, —O—, —S— or —N(R5)— wherein R5 is H or C1-6-alkyl; and R3 is —(CH2)pCOR4 wherein p is 1, 2, 3 or 4 and R4 is OH, NH2, NHOH or C1-6-alkoxy; or a pharmaceutically acceptable salt th
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: April 10, 2001
    Assignee: Novo Nordisk A/S
    Inventors: Rolf Hohlweg, Tine Krogh Jørgensen, Knud Erik Andersen, Uffe Bang Olsen, Zdenék Polivka, Karel Sindelar
  • Patent number: 6187775
    Abstract: The present invention relates to several novel acridone-derived compounds of of formula (I) or (II). These compounds are potent anti-viral agents, useful in the treatment of viral diseases, such as Human Immunodeficiency Virus. In addition, these compounds are anti-neoplastic agents useful in the treatment of various forms of cancer. wherein R1 and R2 are independently —H, —OH, amino, alkylamino, dialkylamino, alkoxy, alkyl, haloalkyl or halogen; n is 2 to 6, X and X′ are independently —N or —NO2; Y and Y′ are independently —N or —CH, or —H; and the double-slash represents a double bond or no bond.
    Type: Grant
    Filed: September 22, 1998
    Date of Patent: February 13, 2001
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Christopher J. Michejda, Marek W. Cholody, William G. Rice, James A. Turpin
  • Patent number: 6177423
    Abstract: Benzo[de]isoquinoline-1,3-dione of Formula or a pharmaceutically acceptable salt thereof wherein R is hydrogen or a protecting group typically used in the art for protecting alcohols and R1-R5 are each independently chosen from H, Cl, Br, F, straight or branched alkyl C1-C8 alkyl, C3-C8 cycloalkyl, heterocycle or bridged heterocycle of 4-9 atoms containing 1-3 heteroatoms, —(CR′2)nOR6, —(CR′2)nN(R6)2, —(CR′2)nNR6COR7, —(CR′2)nNR6SO2OR7, —(CR′2)nNR6SO2 N(R6)2, —(CR′2)nOSO2 N(R6)2, —(CR′2)nCN, —(CR′2)n(NOR6)R7, NO2, CF3, —(CR′2)nSOmR7, —(CR′2)nSOmR7, —(CR′2)nCO2R6, —(CR′2)nCON(R6)2, Ph, and any two of R1-R5 may form a substituted or unsubstituted ring of 5-7 total atoms having 0-2 heteroatoms are claimed which are selective inhibitors of bacterial DNA gyrase and DNA topoisomerase useful in antibacterial agents.
    Type: Grant
    Filed: March 12, 1999
    Date of Patent: January 23, 2001
    Assignee: Warner-Lambert Company
    Inventors: Albert Kudzoi Amegadzie, Maureen Elizabeth Carey, John Michael Domagala, Liren Huang, Ronald George Micetich, Joseph Peter Sanchez, Rajeshwar Singh, Michael Andrew Stier, Arkadii Vaisburg