5-Pyrrolidinylsulfonyl Isatin Derivatives
First Claim
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1. 5-Pyrrolidinylsulfonyl isatin derivatives of the formula 1, wherein, X is —
- O—
, —
S—
or —
NH— and
Y is —
CH2—
or —
C(O)—
;
R1 is an alkyl, substituted alkyl, aryl, heteroarylalkyl group, and optionally additionally comprises a spacer or linker selected from PEG1-200, an oligopeptide, polyamide, polysaccharide, —
NHC(O)—
((CH2)n—
NH—
C(O))m—
, —
O—
((CH2)n-0)m—
, succinyl and 1,4-disubstituted 1,2,3-triazole units, wherein n=0-6 and m=1-200;
R2 is an optionally substituted alkyl, heteroalkyl, aralkyl, heteroarylalkyl, carboxymethyl or methyloxycarbonylmethyl group, wherein the substituents are selected from F, I, Br, OH, NH2, methylamino, methoxy, fluoroethyloxy, fluoropropyloxy, trimethylamino, nitro, tosylate, triflate, mesylate, diazonium N2+, 3-fluorobenzoyl, 4-fluorobenzoyl, 4-fluorophenyl, tributylstannyl, trimethylstannyl, trimethylsilyl, 2-hydrazino-pyridin-5-carbonyl;
or a metal-chelator or a metal-chelator bound to an aralkyl, aminoalkyl, hydroxyalkyl or piperazin-1-carbonylmethyl group;
and optionally additionally comprises a spacer, linker or molecular transporter selected from Annexin V, PEG1-200, an oligopeptide, polyamide, polysaccharide, —
NHC(O)—
((CH2)n—
NH—
C(O))m—
, —
O—
((CH2)n—
O)m—
, succinyl and 1,4-disubstituted 1,2,3-triazole units, wherein n=0-6 and m=1-200 and wherein R2 can also contain an amino acid selected from histidine, lysine, tyrosine, cysteine, arginine and aspartic acid.
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Abstract
The present invention relates to novel 5-pyrrolidinylsulfonyl isatin derivatives, non-peptidyl Caspase binding Radioligands (CbRs) and CbR-transporter conjugates derived from said isatin derivatives, diagnostic compositions comprising said compounds of the invention and their use for non-invasive diagnostic imaging.
7 Citations
13 Claims
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1. 5-Pyrrolidinylsulfonyl isatin derivatives of the formula 1,
wherein, X is — - O—
, —
S—
or —
NH— and
Y is —
CH2—
or —
C(O)—
;
R1 is an alkyl, substituted alkyl, aryl, heteroarylalkyl group, and optionally additionally comprises a spacer or linker selected from PEG1-200, an oligopeptide, polyamide, polysaccharide, —
NHC(O)—
((CH2)n—
NH—
C(O))m—
, —
O—
((CH2)n-0)m—
, succinyl and 1,4-disubstituted 1,2,3-triazole units, wherein n=0-6 and m=1-200;R2 is an optionally substituted alkyl, heteroalkyl, aralkyl, heteroarylalkyl, carboxymethyl or methyloxycarbonylmethyl group, wherein the substituents are selected from F, I, Br, OH, NH2, methylamino, methoxy, fluoroethyloxy, fluoropropyloxy, trimethylamino, nitro, tosylate, triflate, mesylate, diazonium N2+, 3-fluorobenzoyl, 4-fluorobenzoyl, 4-fluorophenyl, tributylstannyl, trimethylstannyl, trimethylsilyl, 2-hydrazino-pyridin-5-carbonyl; or a metal-chelator or a metal-chelator bound to an aralkyl, aminoalkyl, hydroxyalkyl or piperazin-1-carbonylmethyl group; and optionally additionally comprises a spacer, linker or molecular transporter selected from Annexin V, PEG1-200, an oligopeptide, polyamide, polysaccharide, —
NHC(O)—
((CH2)n—
NH—
C(O))m—
, —
O—
((CH2)n—
O)m—
, succinyl and 1,4-disubstituted 1,2,3-triazole units, wherein n=0-6 and m=1-200 andwherein R2 can also contain an amino acid selected from histidine, lysine, tyrosine, cysteine, arginine and aspartic acid. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13)
- O—
Specification