US 7,803,808 B2 · Production of polyketides and other natural products

Abstract

The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. Therefore in aspect the present invention provides 17-desmethylrapamycin and analogues thereof, methods for their production, including recombinant strains, and isolation and uses of the compounds of the invention. In a further aspect the present invention provides for the use of 17-desmethylrapamycin and analogues thereof in the induction or maintenance of immunosuppression, the stimulation of neuronal regeneration or the treatment of cancer, B-cell malignancies, fungal infections, transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation vascular disease and fibrotic diseases, and in the regulation of wound healing.

Claims14

Dependent claims

A compound having the following formula:

wherein:
x represents a direct bond, —CH2—, —S—CH2—, —CH2—S— or —S(═O)—CH2—;
or —CHR5-x-CHR6— represents
R1 represents ═O or (H,H);
R2 represents OH or OMe;
R3 represents H, OH or OMe;
R4 represents a structural fragment selected from groups A, B, C, D, E and F,
in which
the wavy line indicates the position of attachment of the fragment,
R7 represents H or OH and
R8 represents H, OH, halo, thiol or C1-4 alkyl;
or R4 alternatively represents a 5- to 7-membered heterocycle containing one or more heteroatoms selected from the group consisting of O, S and N, which heterocycle is optionally substituted with one or more substituents selected from C1-4 alkyl, OH, F and Cl;
and
R5 and R6 are each independently H or OH,
or pharmaceutically acceptable salts thereof.

12 more elements

Dependencies are inferred from the claim text.

Production of polyketides and other natural products

Life of this patent

Production of polyketides and other natural products

Life of this patent

Abstract

Claims14