Patents by Inventor Allan W. Nicholas

Allan W. Nicholas 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).

  • Alkyl camptothecin compounds as potent inhibitors of human colorectal cancer
    Patent number: 5401747
    Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase. I and show antileukemic and anti-tumor activity.
    Type: Grant
    Filed: May 31, 1994
    Date of Patent: March 28, 1995
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
  • Camptothecin analogs as potent inhibitors of topoisomerase I
    Patent number: 5364858
    Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase.I and show antileukemic and anti-tumor activity.
    Type: Grant
    Filed: December 8, 1992
    Date of Patent: November 15, 1994
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
  • Method of treating tumors with anti-tumor effective camptothecin compounds
    Patent number: 5340817
    Abstract: A camptothecin analog having the structure shown below: ##STR1## where Z is H or C.sub.1-8 alkyl and R is NO.sub.2, NH.sub.2, N.sub.3, hydrogen, halogen, COOH, OH, O-C.sub.1-3 alkyl, SH, S-C.sub.1-3 alkyl, CN, CH.sub.2 NH.sub.2, NH-C.sub.1-3 alkyl, CH.sub.2 -NH-C.sub.1-3 alkyl, N(C.sub.1-3 alkyl).sub.2, CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O-, NH- or S-CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O-, NH- or S- CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O-, NH- or S-CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH).sub.2, O-, NH- or S-CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH.sub.2).sub.2, O-, NH- or S-CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O-, NH- or S-CH.sub.2 CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, CHO, C.sub.1-3 alkyl or NHCOCHR.sup.1 NR.sup.2 R.sup.3, where R.sup.1 is the side-chain of an .alpha.-amino acid and R.sup.2 and R.sup.3, independently are hydrogen or a lower alkyl group or R.sup.
    Type: Grant
    Filed: June 17, 1992
    Date of Patent: August 23, 1994
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
  • Camptothecin analogs as potent inhibitors of topoisomerase I
    Patent number: 5244903
    Abstract: A method for synthesizing camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase.
    Type: Grant
    Filed: October 22, 1990
    Date of Patent: September 14, 1993
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
  • Pharmaceutical compositions and methods employing camptothecins
    Patent number: 5227380
    Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show antileukemic and anti-tumor activity.
    Type: Grant
    Filed: December 31, 1990
    Date of Patent: July 13, 1993
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
  • 10,11-methylenedioxy-20(RS)-camptothecin and 10,11-methylenedioxy-20(S)-camptothecin analogs
    Patent number: 5180722
    Abstract: A camptothecin analog having the structure shown below: ##STR1## where Z is H or C.sub.1-8 alkyl and R is NO.sub.2, NH.sub.2, N.sub.3, hydrogen, halogen, COOH, OH, O--C.sub.1-3 alkyl, SH, S--C.sub.1-3 alkyl, CN, CH.sub.2 NH.sub.2, NH--C.sub.1-3 alkyl, CH.sub.2 --NH--C.sub.1-3 alkyl, N(C.sub.1-3 alkyl).sub.2, CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O--, NH--, or S--CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S-- CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 CH.sub.2 N(CH.sub.2 CH.sub.2 CH.sub.2 OH.sub.2).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, O--, NH-- or S--CH.sub.2 CH.sub.2 CH.sub.2 N(C.sub.1-3 alkyl).sub.2, CHO, C.sub.1-3 alkyl or NHCOCHR.sup.1 NR.sup.2 R.sup.3, where R.sup.1 is the side-chain of an .alpha.-amino acid and R.sup.2 and R.sup.3, independently are hydrogen or a lower alkyl group or R.sup.
    Type: Grant
    Filed: September 13, 1990
    Date of Patent: January 19, 1993
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
  • Camptothecin and analogs thereof and pharmaceutical compositions and method using them
    Patent number: 5122526
    Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show anti-leukemic and anit-tumor activity.
    Type: Grant
    Filed: December 31, 1990
    Date of Patent: June 16, 1992
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
  • 10,11-methylenedioxy camptothecins
    Patent number: 5122606
    Abstract: The invention relates to a method of producing 20(S)-camptothecin, 20(R)-camptothecin and analogs thereof. The method involves the resolution of an mixture of enantiomers of an intermediate lactone.
    Type: Grant
    Filed: March 7, 1991
    Date of Patent: June 16, 1992
    Assignee: Research Triangle Institute
    Inventors: Mansukh C. Wani, Allan W. Nicholas, Monroe E. Wall
  • Total synthesis of 20(S) and 20(R)-camptothecin and compthothecin derivatives
    Patent number: 5053512
    Abstract: The invention relates to a method of producing 20(S)-comptothecin, 20(R)-camptothecin and analogs thereof. The method involves the resolution of an mixture of enantiomers of an intermediate lactone.
    Type: Grant
    Filed: April 17, 1990
    Date of Patent: October 1, 1991
    Assignee: Research Triangle Institute
    Inventors: Mansukh C. Wani, Allan W. Nicholas, Monroe E. Wall
  • 10,11-methylenedioxy-20(RS)-camptothecin analogs
    Patent number: 5049668
    Abstract: A camptothecin analog having the structure shown below: ##STR1## wherein R is NO.sub.2, NH.sub.2, NHCOCHR.sup.1 NR.sup.2 R.sup.3, where R.sup.1 is the side-chain of an .alpha.-amino acid and R.sup.2 and R.sup.3, independently are hydrogen or a lower alkyl group or R.sup.3 is a peptide unit containing 1-3 amino acid units bonded to the nitrogen through a peptide bond, NHCO--C.sub.2-8 -alkylene-X or NHCO--C.sub.2-8 -alkenylene-X, where X is COOH or CONR.sup.2 --(CH.sub.2).sub.n --NR.sup.2 R.sup.3, n=1-10 and R.sup.2 and R.sup.3 are as defined above, NHCO--Z--(CH.sub.2).sub.n --NR.sup.2 R.sup.3, where z=oxygen or NH, or ##STR2## where m+y=3-6 and salts thereof.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: September 17, 1991
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
  • Synthesis of camptothecin and analogs thereof
    Patent number: 4981968
    Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show anti-leukemic and anti-tumor activity.
    Type: Grant
    Filed: September 28, 1988
    Date of Patent: January 1, 1991
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar
  • Synthesis of camptothecin and analogs thereof
    Patent number: 4894456
    Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show anti-leukemic and anti-tumor activity.
    Type: Grant
    Filed: March 31, 1987
    Date of Patent: January 16, 1990
    Assignee: Research Triangle Institute
    Inventors: Monroe E. Wall, Mansukh C. Wani, Allan W. Nicholas, Govindarajan Manikumar