Patents by Inventor Adriano Afonso

Adriano Afonso has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20070213340
    Abstract: Disclosed are compounds of the formula: wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group, and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.
    Type: Application
    Filed: January 17, 2007
    Publication date: September 13, 2007
    Inventors: Joseph Kelly, Adriano Afonso
  • Patent number: 6740661
    Abstract: Disclosed are compounds of the formula: wherein R13 represents an imidazole ring; R14 represents a carbamate, urea, amide or sulfonamide group; R8 represents H when the alkyl chain between the amide group and the R13 imidazole group is substituted, or R8 represents a substituent such as arylalkyl, heteroarylalkyl or cycloalkyl; and the remaining substituents are as defined herein. Also disclosed are compounds wherein R8 is H, and the alkyl chain between the amide group and the R13 imidazole group is unsubstituted. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: May 25, 2004
    Assignee: Schering Corporation
    Inventors: Arthur G. Taveras, Ronald J. Doll, Alan B. Cooper, Johan A. Ferreira, Timothy Guzi, Alan K. Mallams, Dinanath F. Rane, Viyyoor M. Girijavallabhan, Adriano Afonso, Cynthia J. Aki, Jianping Chao, Carmen Alvarez, Joseph M. Kelly, Tarik Lalwani, Jagdish A. Desai, James J-S Wang, Jay Weinstein
  • Patent number: 6528522
    Abstract: The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist activity or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, congestion, inflammatory and CNS-related diseases and others.
    Type: Grant
    Filed: September 18, 2001
    Date of Patent: March 4, 2003
    Assignee: Schering Corporation
    Inventors: Neng-Yang Shih, Robert G. Aslanian, John J. Piwinski, Andrew T. Lupo, Jr., Adriano Afonso
  • Patent number: 6440989
    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: February 13, 2001
    Date of Patent: August 27, 2002
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, Joseph M. Kelly, Jay Weinstein, Ronald L. Wolin, Stuart B. Rosenblum
  • Publication number: 20020103207
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: December 20, 2001
    Publication date: August 1, 2002
    Inventors: Arthur G. Taveras, Ronald J. Doll, Alan B. Cooper, Johan A. Ferreira, Timothy Guzi, Alan K. Mallams, Dinanath F. Rane, Viyyoor M. Girijavallabhan, Adriano Afonso, Cynthia J. Aki, Jianping Chao, Carmen Alvarez, Joseph M. Kelly, Tarik Lalwani, Jagdish A. Desai, James J-S Wang, Jay Weinstein
  • Publication number: 20020082272
    Abstract: The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist activity or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, congestion, inflammatory and CNS-related diseases and others.
    Type: Application
    Filed: September 18, 2001
    Publication date: June 27, 2002
    Inventors: Neng-Yang Shih, Robert G. Aslanian, John J. Piwinski, Andrew T. Lupo, Adriano Afonso
  • Publication number: 20010016585
    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: Application
    Filed: February 13, 2001
    Publication date: August 23, 2001
    Inventors: Adriano Afonso, Joseph M. Kelly, Jay Weinstein, Ronald L. Wolin, Stuart B. Rosenblum
  • 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: 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: 6133291
    Abstract: The present invention discloses novel N(imidazolylalkyl)-substituted cyclic amine compounds which have excellent histamine-H.sub.3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such cyclic amines as well as methods of using them to treat allergy, inflammatory and CNS-related diseases.
    Type: Grant
    Filed: October 16, 1998
    Date of Patent: October 17, 2000
    Assignee: Schering Corporation
    Inventors: Ronald Wolin, Stuart B. Rosenblum, Adriano Afonso
  • 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: 5985879
    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: November 16, 1999
    Assignee: Schering Corporation
    Inventors: Arthur G. Taveras, Alan K. Mallams, Adriano Afonso
  • Patent number: 5958939
    Abstract: A method of inhibiting Ras function and therefore inhibiting cellular growth is disclosed. The method comprises the administration of a novel compound of the formula (Ia), (Ib) or (Ic) ##STR1## wherein: R and R.sup.1 are H, alkyl, halogeno, OH, alkoxy, NH.sub.2, alkylamino, dialkylamino, CF.sub.3, SO.sub.3 H, CO.sub.2 R.sup.3, NO.sub.2, SO.sub.2 NH.sub.2, or CONHR.sup.4 ;n is 0 or 1;R.sup.2 is a group of the formula R.sup.5 C(O)--, R.sup.5 CH.sub.2 C(O)--, R.sup.5 C(R.sup.6).sub.2 C(O)--, R.sup.5 SO.sub.2 --, R.sup.5 CH.sub.2 SO.sub.2 --, R.sup.5 SCH.sub.2 C(O)--, R.sup.5 OC(O)--, R.sup.5 NHC(O)--, R.sup.5 C(O)C(O)-- or R.sup.5 SC(O)--;R.sup.5 is alkyl, aryl, arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl or heterocycloalkyl; andR.sup.6 is alkyl or C(R.sup.6).sub.2 is a carbocyclic ring;or pharmaceutically aceptable salts thereof.
    Type: Grant
    Filed: July 10, 1997
    Date of Patent: September 28, 1999
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, Joseph M. Kelly, Ronald L. Wolin
  • Patent number: 5945429
    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: August 31, 1999
    Assignee: Schering Corporation
    Inventors: Arthur G. Taveras, Alan K. Mallams, Adriano Afonso, Ronald J. Doll
  • Patent number: 5942522
    Abstract: Compounds useful as antihypertensive agents and useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension using compounds of Formula 1.0 wherein R is selected from the group consisting of H, halogen and --C(O)OR.sup.6 ; and R.sup.1 is selected from the group consisting of --OR.sup.14, --O(CH.sub.2).sub.a C(H).sub.3-i Z.sub.i and --O(CH.sub.2).sub.h N(R.sup.15).sub.2.
    Type: Grant
    Filed: February 26, 1997
    Date of Patent: August 24, 1999
    Assignee: Schering Corporation
    Inventors: Adriano Afonso, Jay Weinstein, Margaret Jevnik Gentles
  • Patent number: 5891872
    Abstract: Novel compounds of Formula ##STR1## 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 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: May 22, 1995
    Date of Patent: April 6, 1999
    Assignee: Schering Corporation
    Inventors: Ronald J. Doll, Alan K. Mallams, Adriano Afonso, Dinanath F. Rane, F. George Njoroge, Randall R. Rossman
  • Patent number: 5880128
    Abstract: Novel carbonyl piperazinyl and piperidinyl compounds and pharmaceutical compositions are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel carbonyl piperazinyl or piperidinyl compound 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: May 8, 1996
    Date of Patent: March 9, 1999
    Assignees: Schering Corporation, Pharmacopeia Inc.
    Inventors: Ronald J. Doll, Alan K. Mallams, Adriano Afonso, Dinanth F. Rane, George F. Njoroge, Randall R. Rossman, John J. Baldwin, Ge Li, John C. Reader
  • 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: 5801175
    Abstract: Novel compounds of Formula ##STR1## 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: September 13, 1996
    Date of Patent: September 1, 1998
    Assignees: Schering Corporation, Pharmacopeia, Inc.
    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