`
`
`
`
`
`
`
`
`ngml(cid:237)1 for at least two weeks
`concentration of at least 2.5
`blood plasma fulvestrant
`wherein the method achieves a
`
`
`
`four weeks
`of at least 2.5 ngml(cid:237)1 for at least
`plasma fulvestrant concentration
`therapeutically significant blood
`wherein the method achieves a
`
`(claim 1 only)
`
`(claim 1 only)
`
`least 2 weeks after injection
`least 2.5 ngml(cid:237)1 is attained for at
`fulvestrant concentration of at
`significant blood plasma
`whereby a therapeutically
`
`at least 2 weeks after injection
`least 2.5 ngml(cid:237)1 is attained for
`fulvestrant concentration of at
`significant blood plasma
`whereby a therapeutically
`
`a sufficient amount1
`
`12–18% w/v
`
`17–23% w/v combined
`
`about 15% w/v
`about 10% w/v
`about 10% w/v
`
`about 50 mgml-1 fulvestrant
`
`about 50 mgml-1 fulvestrant
`
`10–25% w/v
`
`10–30% w/v combined
`
`>45 mgml(cid:237)1 of fulvestrant
`
`(claim 2)
`
`>45 mgml(cid:237)1 of fulvestrant
`
`15% w/v
`10% w/v
`10% w/v
`(claim 5)
`
`Intramuscularly to a human
`
`A method of treating a hormonal dependent benign or malignant disease of the breast or reproductive tract
`
`Independent Claim 1 and 11
`
`8,466,139
`
`Independent Claims 1 and 9
`
`8,329,680
`
`Independent Claims 1 and 2
`
`7,456,160
`
`Independent Claims 1 and 5
`
`6,774,122
`
`Comparison of Claims Between U.S. Patent Nos. 6,774,122; 7,456,160; 8,329,680; 8,466,139
`
`PK Result
`
`Castor Oil
`
`Benzyl Benzoate
`Benzyl Alcohol
`
`Ethanol
`
`Fulvestrant
`
`Injection Type
`
`Treatment
`
`MYLAN PHARMS. INC. EXHIBIT 1056 PAGE 1
`
`
`
`- 2 -
`
`about 15% w/v benzyl benzoate
`about 10% w/v benzyl alcohol,
`about 10% w/v ethanol,
`Claims 3, 13:
`
`14–16% w/v benzyl benzoate
`alcohol,
`19–21% w/v ethanol & benzyl
`Claims 2, 12:
`
`2–3, 12–13
`
`
`
`
`
`Claims 7, 17: 5 ml
`7, 17
`8, 18
`9, 19
`
`
`
`ngml-1 for (cid:149)4 weeks
`Claims 6, 10, 16, 20: (cid:149)2.5
`(cid:149)2 weeks
`Claims 4, 14: (cid:149)8.5 ngml-1 for
`
`4, 6, 10, 14, 16, 20
`
`
`
`
`
`
`
`Claims 4, 7, 12, 15: 5 ml
`
`
`
`4, 7, 12, 15
`5, 8, 13, 16
`
`17–20
`
`Claim 10:(cid:149)2.5 ngml-1 for (cid:149)4 wks.
`Claim 2: (cid:149)8.5 ngml-1 for (cid:149)4 wks.
`
`2, 10
`
`
`
`5, 10, 15, 20
`
`3, 6, 11, 14
`
`12–18% w/v benzyl benzoate
`8.5–11.5% w/v benzyl alcohol,
`8.5–11.5% w/v ethanol,
`Claim 4:
`
`12–20% w/v benzyl benzoate
`alcohol,
`15–25% w/v ethanol & benzyl
`Claim 3:
`
`Claim 11: (cid:149)250 mg
`Claim 2,10: (cid:149)45 mgml-1
`
`10–11
`
`
`
`3–4
`
`
`
`Claims 10, 11: (cid:148)6 ml
`10–11
`
`
`
`
`
`
`
`Claim 9: (cid:149)8.5 ngml-1 for (cid:149)4 weeks
`Claim 8: (cid:149)8.5 ngml-1 for (cid:149)2 weeks
`Claim 7: (cid:149)3 ngml-1 for (cid:149)2 weeks
`Claim 6: (cid:149)2.5 ngml-1 for (cid:149)4 weeks
`Claim 5: (cid:149)2.5 ngml-1 for (cid:149)3 weeks
`
`5–9
`12
`
`
`
`
`
`Excipient %
`Narrowing
`Further
`
`Claim 8: 250mg
`Claim 7: (cid:149)250 mg
`Claims 5,6: (cid:149)45 mgml-1
`
`6–8
`Claim 8: 5–5.25 ml
`Claims 6, 7: (cid:148)6 ml
`6–8
`
`Conc. & Dose
`
`Limiting
`
`Volume
`Injection
`Limiting
`
`Claim 4: (cid:149)2.5 ngml-1 for (cid:149)2–5 wks.
`Claim 3: (cid:149)2.5 ngml-1 for (cid:149)4 weeks
`
`
`
`Plasma Conc.
`(Raising Blood
`
`PK Result
`
`Once Monthly
`Divided Dose
`Time Periods)
`
`Extending
`Levels or
`
`Breast Cancer
`
`
`
`
`
`3–4
`2, 9
`
`Independent Claim 1 and 11
`
`8,466,139
`
`Independent Claims 1 and 9
`
`8,329,680
`
`Independent Claims 1 and 2
`
`7,456,160
`
`Independent Claims 1 and 5
`
`6,774,122
`
`Dependent Claims
`
`MYLAN PHARMS. INC. EXHIBIT 1056 PAGE 2