Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Para-n-benzene - sulfoxy-n containing doai – and said benzene...
Patent
1987-12-28
1989-07-18
Warren, Charles F.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Para-n-benzene - sulfoxy-n containing doai, and said benzene...
514602, 514603, 514604, 514562, 562427, 562430, 564 81, 560 10, 560 12, A61K 3163, A61K 31265, A61K 3118, C07C15400
Patent
active
048495638
ABSTRACT:
Compounds of the formula: ##STR1## wherein R.sub.1 s an alkyl of 1-6 carbon atoms, benzyl, phenyl, or phenyl substituted by halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, amino, or carbonyl substituents, or --RN(R').sub.2 wherein R and R' are each independently an alkyl of 1 to 4 carbon atoms; R.sub.2 is an aromatic substituent selected from the group consisting of phenyl, benzyl, and naphthyl, and A is an aromatic substitution selected from the group consisting of hydrogen, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, halogen, --NO.sub.2, --NH.sub.2, --COOH, and --NHCOCH.sub.3. The compounds have been found to be alkylating agents having antineoplastic activity for use in inhibiting the growth of tumors.
REFERENCES:
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patent: 4684747 (1987-08-01), Sartorelli et al.
Reed, "Procarbazine", Antineoplastic and Immunosuppressive Agents, Part & ed. by Sartorelli et al, 1975, pp. 747-765.
Friedman et al, Org. Synth. Coll. vol. 5, 1055 (1973).
Shyam et al, J. Med. Chem., 1985, 28, 527-7.
Vincent T. DeVita, Jr., "Principles of Chemotherapy", Chapter 13, Cancer Principles and Practice of Oncology.
G. P. Wheeler and S. Chumley, "Alkylating Activity of 1,3-Bis(2-chloroethyl)-1-nitrosourca and Related Compounds", J. Med. Chem., 10, 259 (1967).
K. Shyam, L. A. Cosby and A. C. Sartorelli, "Synthesis and Evaluation of N,N.sup.1 -Bis(arylsulfonyl)hydrazines as Antineoplastic Agents", Am. Chem. Society 1985, pp. 525-427.
L. Friedman, R. L. Litle, and Walter R. Reichle, "p-Toluenesulfonylhydrazide*", Organic Syntheses, pp. 1055-1057 (1973).
Hrubiec Robert T.
Sartorelli Alan C.
Shyam Krishnamurthy
Greason Carolyn S.
Warren Charles F.
Yale University
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