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US 2001/0044543 A1Published application
Imaging agents for diagnosis of Parkinson's disease
AssigneeBiostream Therapeutics, Inc.
InventorsJohn W. Babich, Miles P. Smith
Life of this patent
Estimating the term…
Abstract
Generally, the present invention is directed to central nervous system dopamine transporter-imaging agents and methods of use thereof. In certain embodiments, the present invention relates to radiolabeled piperidine derivatives for use as imaging agents in the diagnosis of Parkinson's disease. Another aspect of the present invention relates to piperidine monoamine transporter ligands, comprising a functional group capable of chelating a radionuclide, e.g., technetium, and methods of use thereof.
Claims164
A compound represented by A:
- 18
- wherein
- X represents O or (H)2;
- R represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- R2 represents H;
- R3 represents optionally substituted aryl or heteroaryl;
- R4 represents H;
- R5 represents independently for each occurrence H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- and
- n is 0, 1, or 2.
7 more elements
A compound represented by B:
- 19
- wherein
- X r epresents O or (H)2;
- R represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- R2 represents H;
- R3 represents H;
- R4 represents optionally substituted aryl or heteroaryl;
- R5 represents independently for each occurrence H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- and
- n is 0, 1, or 2.
7 more elements
A compound represented by C:
- 20
- wherein
- X represents O or (H)2;
- R represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- R1 represents H;
- R3 represents optionally substituted aryl or heteroaryl;
- R4represents H;
- R5 represents independently for each occurrence H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- and
- n is 0, 1, or 2.
7 more elements
A compound represented by D:
- 21
- wherein
- X represents O or (H)2;
- R represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- R1 represents H;
- R3 represents H;
- R4 represents optionally substituted aryl or heteroaryl;
- R5 represents independently for each occurrence H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- and
- n is 0, 1, or 2.
7 more elements
A compound represented by E:
- 22
- wherein
- X represents O or S;
- Y represents O or S;
- R represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- R2 represents H;
- R3 represents optionally substituted aryl or heteroaryl;
- R4 represents H;
- R5 represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- m is 1 or 2;
- and
- n is 0, 1, or 2.
9 more elements
A compound represented by F:
- 23
- wherein
- X represents O or S;
- Y represents O or S;
- R represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- R2 represents H;
- R3 represents H;
- R4 represents optionally substituted aryl or heteroaryl;
- R5 represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- m is 1 or 2;
- and
- n is 0, 1, or 2.
9 more elements
A compound represented by G:
- 24
- wherein
- X represents O or S;
- Y represents O or S;
- R represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- R1 represents H;
- R3 represents optionally substituted aryl or heteroaryl;
- R4 represents H;
- R5 represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- m is 1 or 2;
- and
- n is 0, 1, or 2.
9 more elements
A compound represented by H:
- 25
- wherein
- X represents O or S;
- Y represents O or S;
- R represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- R1 represents H;
- R3 represents H;
- R4 represents optionally substituted aryl or heteroaryl;
- R5 represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- m is 1 or 2;
- and
- n is 0, 1, or 2.
9 more elements
A compound represented by I:
- 26
- wherein
- X represents O or (H)2;
- R represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- R1 represents —C(O)OR;
- R2 represents H;
- R3 represents optionally substituted aryl or heteroaryl;
- R4 represents H;
- R5 represents independently for each occurrence H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- and
- n is 1,2, 3, 4, or 5.
8 more elements
A compound represented by J:
- 27
- wherein
- X represents O or S;
- Y represents O or S;
- R represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- R1 represents —C(O)OR;
- R2 represents H;
- R3 represents optionally substituted aryl or heteroaryl;
- R4 represents H;
- R5 represents H, alkyl, alkoxyl, alkylamino, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkoxycarbonyl, or alkylaminocarbonyl;
- m is 1 or 2;
- and
- n is 0, 1, or 2.
10 more elements
Dependencies are inferred from the claim text.