The present invention relates to progesterone receptor antagonists of general formula I: [structure] in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.

Claims

28 · 7 independent · depth 4

28 granted claims

›1.independentA progesterone receptor antagonist of formula I:+19

›6.↳ 1The compound of claim 1, in isolated form.d2+1

›9.↳ 1A pharmaceutical composition comprising a progesterone receptor antagonist as claimed in claim 1, and a pharmaceutically acceptable carrier.d2+5

›16.↳ 1A method for the treatment of endometriosis, myoma or hormone-dependent tumors, comprising administering to a host in need thereof an effective amount…d2+4

›21.↳ 1A method for the treatment of endometriosis or carcinoma of the breast, comprising administering to a host in need thereof an effective amount of an a…d2

›22.↳ 1A method for the treatment of myoma, comprising administering to a host in need thereof an effective amount of an antagonist of claim 1.d2

›23.↳ 1A process for the preparation of an antagonist of claim 1, comprising employing as an intermediate 11β-(4-Ethenylphenyl)-20,20,21,21,21-pentafluoro-5,…d2

›24.↳ 1A process for the preparation of an antagonist of claim 1, comprising employing as an intermediate 11β-[4-(1,2-Dihydroxyethyl)phenyl]-20,20,21,21,21-p…d2

›25.↳ 1A process for the preparation of an antagonist of claim 1, comprising employing as an intermediate 20,20,21,21,21-Pentafluoro-17-hydroxy-5,10α-epoxy-1…d2

›26.↳ 1A process for the preparation of an antagonist of claim 1, comprising employing as an intermediate 11β-{4-[(4R)-2,2-Dimethyl-1,3-dioxolan-4-yl]phenyl}…d2

›2.independent11β-[4-(1,2-Dihydroxyethyl)phenyl]-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one.

›3.independent11 β-[4-[(1R)-1,2-Dihydroxyethyl]phenyl]-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one.+1

›4.independent11β-[4-[(1S)-1,2-Dihydroxyethyl]phenyl]-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one.+1

›5.independent20,20,21,21,21-Pentafluoro-17-hydroxy-11β-[4-(hydroxyacetyl)phenyl]-19-nor-17α-pregna-4,9-dien-3-one.

›27.independentA process for the preparation of progesterone receptor antagonist 20,20,21,21,21-Pentafluoro-17-hydroxy-11i-[4-(hydroxyacetyl)phenyl]-19-nor-17α-pregn…

›28.independentA process for the preparation of progesterone receptor antagonist 20,20,21,21,21-Pentafluoro-17-hydroxy-11i-[4-(hydroxyacetyl)phenyl]-19-nor-17α-pregn…

Classifications

4 codes

IPC · International Patent Classification

Section A — Human necessities

A61K31/565

Section C — Chemistry; metallurgy

C07J1/00

USPC · US Patent Classification

514/179552/648

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File wrapper

Pendency

3.3 y

1,209 days filing → grant

Office actions

non-final + final

Responses

2 RCE

Examiner

Barbara P Badio

art unit 1628 · TC 1600

Law firm

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Citations: 14 back · 0 forward

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Priority chain

2 priority documents

Priority

15 Nov 2006

earliest claimed

›Priority documents — 2

Type	Document	Date
provisional	US 60858955	15 Nov 2006
related publication	US 20080200440 A1	21 Aug 2008

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