# US 4,393,064 A · Process and composition for treatment of leukemia and process for preparing the same

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- Number: US 4,393,064 A
- Document ID: US4393064A
- Status: Granted
- Kind: A
- Application number: 06/075,913
- Filed: 1979-09-17
- Granted: 1983-07-12
- Earliest claimed: 1976-03-05
- Assignees: SRI International; Sloan-Kettering Institute for Cancer Research
- Inventors: Joseph I. DeGraw, Jr.; Francis M. Sirotnak
- Web page: https://patentgrep.com/patent/US4393064A

## CPC

- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/02: Suppositories; Bougies; Bases therefor; {Ovules}(apparatus for making A61J3/08; devices for introducing into the body A61M31/00)
- A61K 31/505: Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- C07D 475/08: with a nitrogen atom directly attached in position 2
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

A process and composition are provided employing 10-deazaminopterin for treating leukemia and ascites tumor.

## Claims

### Claim 1

A pharmaceutical composition in tablet form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of 10-deazaminopterin per tablet therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic carrier or diluent therefor.

### Claim 2 (depends on 1)

A pharmaceutical composition according to claim 1 in which the 10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.

### Claim 3

A pharmaceutical composition in capsule form for treating leukemia or an ascites tumor comprising an amount within the range from 0.1 to about 500 mg of 10-deazaminopterin per capsule therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic inert carrier or diluent therefor.

### Claim 4 (depends on 3)

A pharmaceutical composition according to claim 3 in which the 10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.

### Claim 5

A pharmaceutical composition in suppository form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of 10-deazaminopterin per suppository therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic inert carrier or diluent therefor.

### Claim 6 (depends on 5)

A pharmaceutical composition according to claim 5 in which the 10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.

### Claim 7

A pharmaceutical composition in cachet form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of 10-deazaminopterin per cachet therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic inert carrier or diluent therefor.

### Claim 8 (depends on 7)

A pharmaceutical composition according to claim 7 in which the 10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.

### Claim 9

A pharmaceutical composition in sterile aqueous form for treating leukemia or an ascites tumor comprising an amount within the range from about 0.1 to about 500 mg of 10-deazaminopterin therapeutically effective to ameliorate leukemia or the ascites tumor, together with a pharmaceutically acceptable nontoxic sterile inert aqueous carrier or diluent therefor.

### Claim 10 (depends on 9)

A pharmaceutical composition according to claim 9 in which the 10-deazaminopterin is in the form of a pharmaceutically acceptable acid addition salt.

### Claim 11 (depends on 9)

A pharmaceutical composition according to claim 9, in aqueous solution form.

### Claim 12 (depends on 9)

A pharmaceutical composition according to claim 9, in aqueous dispersion form.

### Claim 13

A process for treating leukemia and ascites tumors which comprises administering to a warm-blooded animal having an abnormal proportion of leukocytes or other evidence of the malignancy, a therapeutic and relatively nontoxic amount of 10-deazaminopterin, to ameliorate leukemia or ascites tumors.

### Claim 14 (depends on 13)

A process according to claim 13 in which the 10-deazaminopterin is administered as a pharmaceutically acceptable salt thereof.

### Claim 15 (depends on 13)

A process according to claim 13 in which the 10-deazaminopterin is administered in an amount with the range from about 0.1 to about 500 mg per day.

### Claim 16 (depends on 13)

A process according to claim 13 in which the 10-deazaminopterin is administered with an inert diluent or carrier.

### Claim 17 (depends on 13)

A process according to claim 13 in which the 10-deazaminopterin is administered orally.

### Claim 18 (depends on 13)

A process according to claim 13 in which the 10-deazaminopterin is administered parenterally.
