# US 8,569,332 B2 · O-methylated rapamycin derivatives for alleviation and inhibition of lymphoproliferative disorders

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- Number: US 8,569,332 B2
- Document ID: US8569332B2
- Status: Granted
- Kind: B2
- Application number: 12/795,335
- Filed: 2010-06-07
- Published: 2010-11-18
- Granted: 2013-10-29
- Earliest claimed: 2000-01-14
- Assignees: The Trustees of the University of Pennsylvania
- Applicants: Mariusz A. Wasik; Leslie M. Shaw
- Inventors: Mariusz A. Wasik; Leslie M. Shaw
- Web page: https://patentgrep.com/patent/US8569332B2

## CPC

- G01N 33/5052: {involving B-cells}
- A61K 31/436: the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61K 31/4745: condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48)
- A61P 31/22: for herpes viruses
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 35/04: specific for metastasis
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- G01N 33/5011: {for testing antineoplastic activity}
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)
- 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

## Abstract

The present invention relates to methods of alleviating and inhibiting a lymphoproliferative disorder in a mammal, the method comprising administering one or more rapamycin derivatives (including rapamycin) to the mammal. Further, the invention provides a method for identifying agents which are useful for alleviating and inhibiting a lymphoproliferative disorders, as well as a method for identifying agents which are capable of inhibiting metastasis of lymphatic tumors in a mammal.

## Claims

### Claim 1

A method of inhibiting metastasis of a lymphatic tumor in a human patient afflicted with a lymphatic cancer, the method comprising administering to the patient, in an amount sufficient to inhibit lymphocyte proliferation, a rapamycin derivative having the chemical structure
wherein
X is (H, H) or O;
Y is (H, OH) or O;
each of R1 and R2 independently ndependently selected from the group consisting of —H, alkyl, thioalkyl, arylalkyl, hydroxyalkyl, dihydroxyalkyl, hydroxyalkylarylalkyl, dihydroxyalkylarylalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, arylsulfonamidoalkyl, allyl, dihydroxyalkylallyl, dioxolanylallyl, carbalkoxyalkyl, and (R3)3 Si;
each R3 is independently selected from the group consisting of —H, methyl, ethyl, isopropyl, tert-butyl, and phenyl; and
either R4 is methyl or R4 and R1 together form a C2-5 alkylene moiety.

### Claim 2 (depends on 1)

The method of claim 1, wherein the rapamycin derivative is 40-O-(2-hydroxy)ethyl-rapamycin.