The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Aug. 23, 1994
Filed:
Jun. 17, 1992
Monroe E Wall, Chapel Hill, NC (US);
Mansukh C Wani, Durham, NC (US);
Allan W Nicholas, Raleigh, NC (US);
Govindarajan Manikumar, Raleigh, NC (US);
Research Triangle Institute, Research Triangle Park, NC (US);
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.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; CONR.sup.2 -(CH.sub.2).sub.n -NR.sup.2 R.sup.3, where n=1-10 and R.sup.2 and R.sup.3 are as defined above; NHCO-B-(CH.sub.2).sub.n-NR.sup.2 R.sup.3, where B=oxygen or NH, or ##STR2## where m+y=3-6, and salts thereof. The campothecin compounds inhibit the enzyme topisomerase I and are useful in treating tumors and leukemia.