Patents Represented by Attorney Henry C. Jeanette
  • Patent number: 6228856
    Abstract: Novel compounds of the formula: are disclosed. Compounds of Formula 1.0 are represented by the compounds of formulas: wherein R1, R3 and R4 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: October 14, 1999
    Date of Patent: May 8, 2001
    Assignee: Schering Corporation
    Inventors: F George Njoroge, Arthur G. Taveras, Ronald J. Doll, Tarik Lalwani, Carmen Alvarez, Stacy W. Remiszewski
  • 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: 6218401
    Abstract: Novel phenyl-substituted tricyclic compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel halo-N-substituted urea compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammals such as a human.
    Type: Grant
    Filed: August 13, 1999
    Date of Patent: April 17, 2001
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, Joseph M. Kelly, Jay Weinstein, Ronald L. Wolin, Stuart B. Rosenblum
  • 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: 6211193
    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 R represents a cycloalkyl or a heterocycloalkyl ring that is substitued. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
    Type: Grant
    Filed: June 15, 1998
    Date of Patent: April 3, 2001
    Assignee: Schering Corporation
    Inventors: Stacy W. Remiszewski, Ronald J. Doll, Carmen Alvarez, Tarik Lalwani
  • Patent number: 6159984
    Abstract: Novel compounds of the formula: ##STR1## wherein a represents N or NO, R.sup.1 and R.sup.3 are halo, R.sup.2 and R.sup.4 are independently H or halo provided that at least one is H, X is C, CH or N, and T represents ##STR2## wherein R.sub.5 is H (C.sub.1 -C.sub.6)alkyl or a bond; b and c are independently 0 to 3 and Y is a three, four, five or six membered cycloalkyl ring, pyridyl, pyrazinyl or phenyl are disclosed. Pharmaceutical Compositions containing such compounds, methods of inhibiting farnesyl protein transferase and methods for treating tumor cells using such compounds or compositions are also disclosed.
    Type: Grant
    Filed: June 15, 1998
    Date of Patent: December 12, 2000
    Assignee: Schering Corporation
    Inventors: Timothy J. Guzi, Dinanath F. Rane
  • Patent number: 6143758
    Abstract: Novel compounds, such as: ##STR1## 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: November 7, 2000
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Joseph M. Kelly, Alan K. Mallams, F. George Njoroge, Stacy W. Remiszewski, Arthur G. Taveras
  • Patent number: 6130229
    Abstract: Compounds of Formula I: ##STR1## wherein: X.sup.1 is hydrogen, halogen, CF.sub.3, nitro, NH.sub.2 or lower alkyl;each X.sup.2 is independently selected from the group consisting of hydrogen, halogen, lower alkoxy and lower alkyl;n is 1 or 2;Y is selected from the group consisting of S(O).sub.p, O, and NR.sup.5, wherein p is 0, 1 or 2, and R.sup.5 is hydrogen, alkyl, aryl, cycloalkyl, loweralkoxycarbonyl, aminocarbonyl or acyl;R.sup.1 and R.sup.2, which may be the same or different, are selected from the group consisting of hydrogen and lower alkyl groups, or taken together can form an oxygen atom when Y is NR.sup.5 ;A . . . is C=, CH-- or N--;R is --CZ--Y.sup.1 --Y.sup.2 --R.sup.3, wherein:Z is O, =CH--CN, or =N--CN;one of Y.sup.1 and Y.sup.2 is a bond, --CO--, O, S, or --NR.sup.4 --, and the other is (CH.sub.2).sub.m, where m is 0 or an integer of 1 to 4, and R.sup.4 is H or alkyl, with the proviso that when Z is O and m is 0 then Y.sup.1 or Y.sup.2 is selected from --CO--, O, S, or --NR.sup.4 ;R.sup.
    Type: Grant
    Filed: October 7, 1997
    Date of Patent: October 10, 2000
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, Joseph M. Kelly, Stuart B. Rosenblum, Ronald L. Wolin, Jay Weinstein
  • Patent number: 6124295
    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: April 27, 1999
    Date of Patent: September 26, 2000
    Assignee: Schering Corporation
    Inventors: Arthur G. Taveras, Alan K. Mallams, Adriano Afonso, Ronald J. Doll
  • Patent number: 6100279
    Abstract: Disclosed are compounds of Formula I ##STR1## or pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula I. Further disclosed is a method of treating allergy (for example asthma), inflammation, hypotension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimer's, schizophrenia, obesity and migraine) comprising administering an effective amount of a compound of Formula I to a patient in need of such treatment.
    Type: Grant
    Filed: November 5, 1998
    Date of Patent: August 8, 2000
    Assignee: Schering Corporation
    Inventors: Wayne D. Vaccaro, Ronald L. Wolin, Daniel M. Solomon, Robert G. Aslanian, John J. Piwinski, Stuart B. Rosenblum
  • Patent number: 6096757
    Abstract: Methods are provided for treating proliferative diseases, especially cancers, comprising administering (1) a farnesyl protein transferase inhibitor in conjunction with (2) an antineoplastic agent and/or radiation therapy.
    Type: Grant
    Filed: December 21, 1998
    Date of Patent: August 1, 2000
    Assignee: Schering Corporation
    Inventors: Walter R. Bishop, Joseph J. Catino, Ronald J. Doll, Ashit Ganguly, Viyyoor M. Girijavallabhan, Paul Kirschimeier, Ming Liu, Loretta L. Nielsen, David L. Cutler
  • Patent number: 6075025
    Abstract: A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a compound of Formula 1.0 ##STR1## Also disclosed are novel compounds of the formulas: ##STR2## Also disclosed are processes for making 3-substituted compounds of the Formulas 1.1, 1.2 and 1.3.Further disclosed are novel compounds which are intermediates in the processes for making the 3-substituted compounds of Formulas 1.1, 1.2, and 1.3.
    Type: Grant
    Filed: March 11, 1998
    Date of Patent: June 13, 2000
    Assignee: Schering Corporation
    Inventors: W. Robert Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski
  • Patent number: 6071907
    Abstract: Novel tricyclic compounds and pharmaceutical compositions are disclosed which are inhibitors of the enzyme, farnesyl protein transferase. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel tricyclic compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammals such as a human.
    Type: Grant
    Filed: September 11, 1997
    Date of Patent: June 6, 2000
    Assignee: Schering Corporation
    Inventors: F. George Njoroge, Yi-Tsung Liu, Arthur G. Taveras
  • Patent number: 6051582
    Abstract: Novel compounds of the formula: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: a represents N or NO.sup.- ;R.sup.1 and R.sup.3 are the same or different and each represents halo;R.sup.2 and R.sup.4 are each independently selected from H and halo, provided that at least one of R.sup.2 and R.sup.4 is H;each dotted line (---) represents an optional bond;X is N, C when the optional bond to X is present, or CH when the optional bond to X is absent;T is a substituent selected from: ##STR2## Z represents O or S; R represents --SO.sub.2 R.sup.10 ;R.sup.5 represents alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, OR.sup.12, NR.sup.12 H, SH, SR.sup.12, SOR.sup.12 (where R.sup.12 is not H), or SO.sub.2 R.sup.12 (where R.sup.12 is not H); andeach R.sup.10 independently represents H, alkyl, aryl, or aralkyl;R.sup.11 is alkyl, aryl, aralkyl, heteroaryl or heterocycloalkyl;R.sup.12 is selected from H, alkyl, aryl, aralkyl, heteroaryl, heteroarylalkyl, or heterocycloalkyl.
    Type: Grant
    Filed: June 15, 1998
    Date of Patent: April 18, 2000
    Assignee: Schering Corporation
    Inventor: Arthur G. Taveras
  • Patent number: 6040305
    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: March 21, 2000
    Assignee: Schering Corporation
    Inventors: Arthur G. Taveras, George F. Njoroge
  • Patent number: 6034251
    Abstract: Disclosed are novel phenyl-alkyl-imidazoles of the formula ##STR1## wherein R.sup.1, R.sup.7, m, n, p, q, X, Y, Z, R and R.sup.15 are as defined in the specification.Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Further disclosed are methods of treating allergy, inflammation, hypotension, glaucoma, sleeping disorders, states of hyper and hypo motility of the gastrointestinal tract, hypo and hyperactivity of the central nervous system, Alzheimer's, schizophrenia, obesity and migraines by administering compounds of formula I.Also disclosed are methods for treatment of upper airway allergic responses comprising administering a compound, or salt or solvate thereof, of formula I in combination or admixture with a histamine H.sub.1 receptor antagonist.
    Type: Grant
    Filed: November 5, 1998
    Date of Patent: March 7, 2000
    Assignee: Schering Corporation
    Inventors: Robert G. Aslanian, Kevin D. McCormick, John J. Piwinski
  • Patent number: 6030982
    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: February 29, 2000
    Assignee: Schering Corporationm
    Inventors: F George Njoroge, Arthur G. Taveras, Ronald J. Doll, Tarik Lalwani, Carmen Alvarez, Stacy W. Remiszewski
  • Patent number: 5994364
    Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, Y, A, B, X, a, b, c, d, v, and w are as described herein. The compounds of formula (1.0) are useful for inhibiting tumor growth.
    Type: Grant
    Filed: September 11, 1997
    Date of Patent: November 30, 1999
    Assignee: Schering Corporation
    Inventors: F. George Njoroge, Ronald J. Doll, Stacy W. Remiszewski
  • Patent number: 5990147
    Abstract: Disclosed are novel phenyl-alkyl-imidazoles of the formula ##STR1## or pharmaceutically acceptable salts or solvates thereof, wherein A and R, are as defined in the specification.Also disclosed are methods of treating allergy, inflammation, hypotension, glaucoma, sleeping disorders, states of hyper and hypo motility of the gastrointestinal tract, hypo and hyperactivity of the central nervous system, Alzheimer's, schizophrenia, obesity and migraines, comprising administering an effective amount of a compound of formula I (or a salt or solvate thereof) to a patient in need of such treatment.Also disclosed are methods for treatment of upper airway allergic responses comprising administering a compound, or salt or solvate thereof, of formula I in combination or admixture with a histamine H.sub.1 receptor antagonist.
    Type: Grant
    Filed: November 5, 1998
    Date of Patent: November 23, 1999
    Assignee: Schering Corporation
    Inventor: Robert G. Aslanian