Antiangiogenic agents
OwnerGregory Agoston, Victor Pribluda +2inventors
InventorsGregory Agoston, Victor Pribluda, Anthony Treston, Shawn Green
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Abstract
Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: wherein the variables are defined in the specification.
Claims9
1-2. (canceled)
The method of claim 10, wherein:
- Rh1 and Rh2 are independently H and Et.
The method of claim 10, wherein:
- Rh1 and Rh2 are independently H and n-Pr.
The method of claim 10, wherein:
- Rh1 and Rh2 are independently H and i-Bu.
The method of claim 10, wherein:
- Rh1 and Rh2 are independently H and CH2OH.
The compound method of claim 10, wherein:
- Rh1 and Rh2 are independently H and n-Bu.
The method of claim 10, wherein:
- Rh1 and Rh2 are independently H and Me.
The method of claim 10, wherein:
- Rh1 and Rh2 are independently H and (CH2)n—C(Me)2.
A method of inhibiting angiogenesis in a human or an animal comprising administering to the human or animal an angiogenesis inhibiting amount of a compound of the formula:
- wherein:
- a) Ra is —N3, —C≡N, —C≡C—R, —C═CH—R, —R—C═CH2, —C≡CH, —O—R, —R—R1, or —O—R—R1 where R is a straight or branched alkyl with up to 10 carbons or aralkyl, and R1 is —OH, —NH2, —Cl, —Br, —I, —F or CF3;
- b) Z′ is >CH or >C—R2—OH, where R2 is an alkyl or branched alkyl with up to 10 carbons or aralkyl;
- c) >C—Rg is >CH2, >C(H)—OH, >C═O, >C═N—OH, >C(R3)OH, >C═N—OR3, >C(H)—NH2, >C(H)—NHR3, >C(H)—NR3R4, or >C(H)—C(O)—R3, where each R3 and R4 is independently an alkyl or branched alkyl with up to 10 carbons or aralkyl;
- d) Rh1 and Rh2 are independently H, or a straight or branched chain alkyl, alkenyl or alkynyl with up to 6 carbons that is unsubstituted, or substituted with one or more groups selected from a hetero functionality (O—Y, N—Y or S—Y) where Y is H, Me or an alkyl chain up to 6 carbons;
- a halo functionality (F, Cl, Br or I);
- an aromatic group optionally substituted with hetero, halo or alkyl;
- or Rh1 and Rh2 are independently an aromatic group optionally substituted with hetero, halo or alkyl, provided that both Rh1 and Rh2 are not H;
- and
- wherein all monosubstituted substituents have either an α or β configuration.
Dependencies are inferred from the claim text.