This invention relates to novel fluorinated phenyl thiphenyl (also named diarylsulfide) derivatives and their use in Positron Emission Tomagraphy (PET) imaging of Serotonin Transporters (SERTS). The present invention also provides diagnostic compositions comprising the novel compounds of the present invention, and a pharmaceutically acceptable carrier or diluent. The invention further provides a method of imaging SERTS, comprising introducing into a patient a detectable quantity of a labeled compound of the present invetion, or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.

Claims

21 · 1 independent · depth 5

21 granted claims

›1.independentA compound of Formula I+20

›2.↳ 1The compound of claim 1, whereinnR1 is hydroxy(C1-4)alkyl, one of R8 and R9 is C1-4 alkyl the other of R8 and R9 is C1-4 alkyl, halo(C1-4)alkyl, halo(…d2+1

›4.↳ 1The compound of claim 1, whereinnR1 is halo, R8 and R9 are C1-4 alkyl, R3, R4 and R5 are each hydrogen, X is halo.d2

›5.↳ 1The compound of claim 1, whereinnR1 is â€”NR6R7, nR6 and R7 are independently selected from the group consisting of hydrogen, C1-4 alkyl, halo(C1-4)al…d2+6

›12.↳ 1The compound of claim 1, whereinnR1 is hydroxy(C1-4)alkyl, R8 and R9 are each C1-4 alkyl, and R3 is hydrogen or C1-4 alkyl.d2+1

›14.↳ 1The compound of claim 1, whereinnR1 is â€”NH2, one of R8 and R9 is hydrogen or C1-4 alkyl, the other of R8 and R9 is C1-4 alkyl, or halo(C1-4)alkyl, R…d2+4

›19.↳ 1A pharmaceutical composition comprising a compound of claim 1, andna pharmaceutically acceptable excipient or diluent.d2

›20.↳ 1A diagnostic composition for imaging serotonin transporters, comprising a compound of claim 1, andna pharmaceutically acceptable excipient or diluent.d2+1

Classifications

5 codes

IPC · International Patent Classification

Section C — Chemistry; metallurgy

C07K321/28

USPC · US Patent Classification

564/341514/649514/653514/612

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Pendency

2.0 y

725 days filing → grant

Office actions

non-final + final

Responses

1 RCE

Examiner

Brian Davis

art unit 1621 · TC 1600

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Citations: 132 back · 0 forward

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Priority chain

2 priority documents

Priority

14 Mar 2002

earliest claimed

›Priority documents — 2

Type	Document	Date
provisional	US 60364905 00	14 Mar 2002
related publication	US 20030236234 A1	25 Dec 2003

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