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US 6,723,858 B2Granted
Estrogenic compounds as anti-mitotic agents
AssigneeChildren's Medical Center Corporation
InventorsRobert John D'Amato, Moses Judah Folkman
Life of this patent
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Abstract
The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.
Claims15
A compound of the formula:
- wherein:
- I. Ra-Rk are defined as follows:
- A) each Ra, Rb, Rc, Rd, Rg, Rh, R1, Rk independently is —R1, —OR1, —OCOR1, —SR1, —F, —NHR2, —Br, or —I;
- and Re is —R1, —OR1, —OCOR1, —SR1, —F, —NHR2, —Br, —I or —C≡CH;
- or
- B) each Ra, Rb, Rc, Rd, Rk, independently is —R1, —OR1, OCOR1, —SR1, —F, —NHR2, —Br, or —I;
- and each Rg, Rh, Ri, independently is ═O, —R1, —OR1, —OCOR1, —SR1, —F, —Br, or —I;
- and Re is ═O, —R1, —OR1, —OCOR1, —SR1, —F, —Br, —I or —C≡CH;
- and
- II. Z′ is defined as follows:
- A) Z′ is X, where X is >COR1,
- B) Z′is
- where Rn is —R1, —OR1, —Sr1, —F, —NHR2, —Br, or —I;
- and X′ is X, as defined above;
- or X′ is >C═O;
- and
- III. Z″ is defined as follows:
- A) Z″ is —O—;
- or
- B) Z″ is
- where Rp is —R1, —Or2, —SR1, —F, —NHR2, —Br or —I;
- where, in each formula set forth above, each R1 and R2 independently is —H, or an alkyl, alkenyl or alkynyl group of up to 6 carbons.
19 more elements
A compound of the formula:
- wherein:
- I. Ra—Ro are defined as follows:
- A) each Ra, Rb, Rc, Rd, Re, Rf, Ri, Rj, Rk, RL, Rm, Ro independently is —R1, —OR1, —OCOR1, —SR1, —F, —NHR2, —Br, or —I;
- and Rg is —R1, —OR1, —OCOR1, —SR1, —F, —NHR2, —Br, —I or —C≡CH;
- or
- B) each Ra, Rb, Rc, Rf, Rk, RL, independently is —R1, —OR1, —OCOR1, —SR1, —F, —NHR2, —Br, or —I;
- and each Rd, Re, Ri, Rj, Rm, RO independently is ═O, —R1, —OR1, —OCOR1, —SR1, —F, —NHR2, —Br, —I;
- and Rg is ═O, —R1, —OR1, —OCOR1, —SR1, —F, —NHR2, —Br, —I or —C≡CH;
- and
- II. Z is defined as follows:
- A) Z is —O—;
- or B) Z is
- where Rn is —R1, —OR1, —SR1, —NHR2, —Br or —I;
- where, in each formula set forth above, each R1 and R2 independently is —H, or an alkyl, alkenyl or alkynyl group of up to 6 carbons.
11 more elements
A compound of the formula:
- wherein:
- I. Ra-Rk are defined as follows:
- A) each Ra, Rb, Rc, Rd, Rg, Rh, Ri, Rk independently is —R1, —OR1, —OCOR1, —SR1, —F, —NHR1, —Br, or —I;
- and Re is —R1, —OR1, —OCOR1, —SR1, —F, —NHR1, —Br, —I or —C≡CH;
- or
- B) each Ra, Rb, Rc, Rd, independently is —R1, —OR1, —OCOR1, —SR1, —F, —NHR1, —Br, or —I;
- and each Rg, Rh, Ri, Rk independently is ═O, —R1, OR1, —OCOR1, —SR1, —F, —NHR1, —Br or —I;
- and Re is —R1, —OR1, —OCOR1, —SR1, —F, —NHR1, —Br, —I or —C≡CH;
- and
- II. Z is defined as follows:
- A) Z is —O—;
- or B) Z is
- where Rn is —R1, —OR1, —SR1, —F, —NHR2, —Br or —I;
- where, in each formula set forth above, each R1 and R2 independently is —H, or an alkyl, alkenyl or alkynyl group of up to 6 carbons.
11 more elements
Dependencies are inferred from the claim text.