US2001018514A1PendingUtilityA1

Nucleic acid labeling compounds

34
Priority: Jul 31, 1998Filed: Jul 31, 1998Published: Aug 30, 2001
Est. expiryJul 31, 2018(expired)· nominal 20-yr term from priority
C07H 19/12C07H 19/06C07H 19/04C07H 19/052C07H 21/00C07H 19/10
34
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Claims

Abstract

Nucleic acid labeling compounds containing heterocyclic derivatives are disclosed. The heterocyclic derivative containing compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.

Claims

exact text as granted — not AI-modified
1 . A nucleic acid labeling compound of the following structure:  
                   
       wherein A is H or a functional group that permits the attachment of the nucleic acid labeling compound to a nucleic acid; X is O, S, NR 1  or CHR 2 , wherein R 1  and R 2  are, independently, H, alkyl or aryl; Y is H, N 3 , F, OR 1 , SR 1  or NHR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is amido alkyl; Q is a detectable moiety; and, M is a connecting group, wherein m is an integer ranging from 0 to about 3.  
     
     
         2 . A nucleic acid labeling compound according to    claim 1   , wherein A is H or H 4 O 9 P 3 —; X is O; Y is H or OR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is —C(O)NH(CH 2 ) n NH—, wherein n is an integer ranging from about 2 to about 10; Q is biotin or a carboxyfluorescein; and, M is —CO(CH 2 ) 5 NH—, wherein m is 1 or 0.  
     
     
         3 . A nucleic acid labeling compound according to    claim 2   , wherein Y is H or OH; Z is H or OH; L is —C(O)NH(CH 2 ) 4 NH—; Q is biotin; and, M is —CO(CH 2 ) 5 NH, wherein m is 1.  
     
     
         4 . A nucleic acid labeling compound according to    claim 2   , wherein Y is H or OH; Z is H or OH; L is —C(O)NH(CH 2 ) 4 NH—; Q is 5-carboxyfluorescein; and m is 0.  
     
     
         5 . A nucleic acid labeling compound of the following structure:  
                   
       wherein A is H or a functional group that permits the attachment of the nucleic acid labeling compound to a nucleic acid; X is O, S, NR 1  or CHR 2 , wherein R 1  and R 2  are, independently, H, alkyl or aryl; Y is H, N 3 , F, OR 1 , SR 1  or NHR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is amino alkyl; Q is a detectable moiety; and, M is a connecting group, wherein m is an integer ranging from 0 to about 3.  
     
     
         6 . A nucleic acid labeling compound according to    claim 5   , wherein A is H or H 4 O 9 P 3 —; X is O; Y is H or OR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is —NH(CH 2 ) n NH—, wherein n is an integer ranging from about 2 to about 10; Q is biotin or carboxyfluorescein; and, M is —CO(CH 2 ) 5 NH— or —CO(CH 2 ) 5 NHCO(CH 2 ) 5 NH—, wherein m is 1 or 0.  
     
     
         7 . A nucleic acid labeling compound according to    claim 6   , wherein Y is H or OH; Z is H or OH; L is —NH(CH 2 ) 4 NH—; Q is biotin; and, m is 0.  
     
     
         8 . A nucleic acid labeling compound according to    claim 6   , wherein Y is H or OH; Z is H or OH; L is —NH(CH 2 ) 4 NH—; Q is 5-carboxyfluorescein; and, m is 0.  
     
     
         9 . A nucleic acid labeling compound of the following structure:  
                   
       wherein A is H or a functional group that permits the attachment of the nucleic acid labeling compound to a nucleic acid; X is O, S, NR 1  or CHR 2 , wherein R 1  and R 2  are, independently, H, alkyl or aryl; Y is H, N 3 , F, OR 1 , SR 1  or NHR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is alkynyl alkyl; Q is a detectable moiety; and, M is a connecting group, wherein m is an integer ranging from 0 to about 3.  
     
     
         10 . A nucleic acid labeling compound according to    claim 9   , wherein A is H or H 4 O 9 P 3 —; X is O; Y is H or OR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is —C≡C(CH 2 ) n NH—, wherein n is an integer ranging from about 1 to about 10; Q is biotin or carboxyfluorescein; and, M is —CO(CH 2 ) 5 NH—, wherein m is 1 or 0.  
     
     
         11 . A nucleic acid labeling compound according to    claim 10   , wherein Y is H or OH; Z is H or OH; L is —C≡CCH 2 NH—; Q is biotin; and, m is 1.  
     
     
         12 . A nucleic acid labeling compound according to    claim 10   , wherein Y is H or OH; Z is H or OH; L is —C≡CCH 2 NH—; Q is 5-carboxyfluorescein; and, m is 1.  
     
     
         13 . A nucleic acid labeling compound of the following structure:  
                   
       wherein A is H or a functional group that permits the attachment of the nucleic acid labeling compound to a nucleic acid; X is O, S, NR 1  or CHR 2 , wherein R 1  and R 2  are, independently, H, alkyl or aryl; Y is H, N 3 , F, OR 1 , SR 1  or NHR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is amino alkyl; Q is a detectable moiety; and, M is a connecting group, wherein m is an integer ranging from 0 to about 3.  
     
     
         14 . A nucleic acid labeling compound according to    claim 13   , wherein A is H or H 4 O 9 P 3 —; X is O; Y is H or OR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is —NH(CH 2 ) n NH—, wherein n is an integer ranging from about 2 to about 10; Q is biotin or carboxyfluorescein; and, M is —CO(CH 2 ) 5 NH— or —CO(CH 2 ) 5 NHCO(CH 2 ) 5 NH—, wherein m is 1 or 0.  
     
     
         15 . A nucleic acid labeling compound according to    claim 14   , wherein Y is H or OH; Z is H or OH; L is —NH(CH 2 ) 4 NH—; Q is biotin; and, M is —CO(CH 2 ) 5 NH—, wherein m is 1.  
     
     
         16 . A nucleic acid labeling compound according to    claim 14   , wherein Y is H or OH; Z is H or OH; L is —NH(CH 2 ) 4 NH—; Q is 5-carboxyfluorescein; and, M is —CO(CH 2 ) 5 NH—, wherein m is 1.  
     
     
         17 . A nucleic acid labeling compound of the following structure:  
                   
       wherein A is H or a functional group that permits the attachment of the nucleic acid labeling compound to a nucleic acid; X is O, S, NR 1  or CHR 2 , wherein R 1  and R 2  are, independently, H, alkyl or aryl; Y is H, N 3 , F, OR 1 , SR 1  or NHR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is functionalized alkyl, alkenyl alkyl or alkynyl alkyl; Q is a detectable moiety; and, M is a connecting group, wherein m is an integer ranging from 0 to about 3.  
     
     
         18 . A nucleic acid labeling compound according to    claim 17   , wherein A is H or H 4 O 9 P 3 —; X is O; Y is H or OR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is —CH═CH(CH 2 ) n NH—, wherein n is an integer ranging from about 1 to about 10; Q is biotin or carboxyfluorescein; and, M is —CO(CH 2 ) 5 NH— or —CO(CH 2 ) 5 NHCO(CH 2 ) 5 NH—, wherein m is 1 or 0.  
     
     
         19 . A nucleic acid labeling compound according to    claim 18   , wherein Y is H or OH; Z is H or OH; L is —CH═CHCH 2 NH—; Q is biotin; and, m is 0.  
     
     
         20 . A nucleic acid labeling compound according to    claim 18   , wherein Y is H or OH; Z is H or OH; L is —CH═CHCH 2 NH—; Q is 5-carboxyfluorescein; and, m is 0.  
     
     
         21 . A nucleic acid labeling compound of the following structure:  
                   
       wherein A is H or a functional group that permits the attachment of the nucleic acid labeling compound to a nucleic acid; X is O, S, NR 1  or CHR 2 , wherein R 1  and R 2  are, independently, H, alkyl or aryl; Y is H, N 3 , F, OR 1 , SR 1  or NHR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is functionalized alkyl, alkenyl alkyl or alkynyl alkyl; Q is a detectable moiety; and, M is a connecting group, wherein m is an integer ranging from 0 to about 3.  
     
     
         22 . A nucleic acid labeling compound according to    claim 21   , wherein A is H or H 4 O 9 P 3 —; X is O; Y is H or OR 1 , wherein R 1  is H, alkyl or aryl; Z is H, N 3 , F or OR 1 , wherein R 1  is H, alkyl or aryl; L is —CH═CH(CH 2 ) n NH—, wherein n is an integer ranging from about 1 to about 10; Q is biotin or carboxyfluorescein; and, M is —CO(CH 2 ) 5 NH— or —CO(CH 2 ) 5 NHCO(CH 2 ) 5 NH—, wherein m is 1 or 0.  
     
     
         23 . A nucleic acid labeling compound according to    claim 22   , wherein Y is H or OH; Z is H or OH; L is —CH═CHCH 2 NH—; Q is biotin; and, m is 0.  
     
     
         24 . A nucleic acid labeling compound according to    claim 22   , wherein Y is H or OH; Z is H or OH; L is —CH═CHCH 2 NH—; Q is 5-carboxyfluorescein; and, m is 0.  
     
     
         25 . A nucleic acid derivative produced by coupling a nucleic acid labeling compound according to    claim 2    with a nucleic acid.  
     
     
         26 . A nucleic acid derivative produced by coupling a nucleic acid labeling compound according to    claim 6    with a nucleic acid.  
     
     
         27 . A nucleic acid derivative produced by coupling a nucleic acid labeling compound according to    claim 10    with a nucleic acid.  
     
     
         28 . A nucleic acid derivative produced by coupling a nucleic acid labeling compound according to    claim 14    with a nucleic acid.  
     
     
         29 . A nucleic acid derivative produced by coupling a nucleic acid labeling compound according to    claim 18    with a nucleic acid.  
     
     
         30 . A nucleic acid derivative produced by coupling a nucleic acid labeling compound according to    claim 22    with a nucleic acid.  
     
     
         31 . A hybridization product, wherein the hybridization product comprises the nucleic acid derivative according to    claim 25    bound to a complementary probe.  
     
     
         32 . The hybridization product according to    claim 31   , wherein the probe is attached to a glass chip.  
     
     
         33 . A hybridization product, wherein the hybridization product comprises the nucleic acid derivative according to    claim 26    bound to a complementary probe.  
     
     
         34 . The hybridization product according to    claim 33   , wherein the probe is attached to a glass chip.  
     
     
         35 . A hybridization product, wherein the hybridization product comprises the nucleic acid derivative according to    claim 27    bound to a complementary probe.  
     
     
         36 . The hybridization product according to    claim 35   , wherein the probe is attached to a glass chip.  
     
     
         37 . A hybridization product, wherein the hybridization product comprises the nucleic acid derivative according to    claim 28    bound to a complementary probe.  
     
     
         38 . The hybridization product according to    claim 37   , wherein the probe is attached to a glass chip.  
     
     
         39 . A hybridization product, wherein the hybridization product comprises the nucleic acid derivative according to    claim 29    bound to a complementary probe.  
     
     
         40 . The hybridization product according to    claim 39   , wherein the probe is attached to a glass chip.  
     
     
         41 . A hybridization product, wherein the hybridization product comprises the nucleic acid derivative according to    claim 30    bound to a complementary probe.  
     
     
         42 . The hybridization product according to    claim 41   , wherein the probe is attached to a glass chip.  
     
     
         43 . A method of synthesizing a labeled nucleic acid comprising attaching a nucleic acid labeling compound according to    claim 2    to a nucleic acid.  
     
     
         44 . A method of synthesizing a labeled nucleic acid comprising attaching a nucleic acid labeling compound according to    claim 6    to a nucleic acid.  
     
     
         45 . A method of synthesizing a labeled nucleic acid comprising attaching a nucleic acid labeling compound according to    claim 10    to a nucleic acid.  
     
     
         46 . A method of synthesizing a labeled nucleic acid comprising attaching a nucleic acid labeling compound according to    claim 14    to a nucleic acid.  
     
     
         47 . A method of synthesizing a labeled nucleic acid comprising attaching a nucleic acid labeling compound according to    claim 18    to a nucleic acid.  
     
     
         48 . A method of synthesizing a labeled nucleic acid comprising attaching a nucleic acid labeling compound according to    claim 22    to a nucleic acid.  
     
     
         49 . A method of detecting a nucleic acid comprising incubating a nucleic acid derivative according to    claim 25    with a probe.  
     
     
         50 . A method according to    claim 49   , wherein the probe is attached to a glass chip.  
     
     
         51 . A method of detecting a nucleic acid comprising incubating a nucleic acid derivative according to    claim 26    with a probe.  
     
     
         52 . A method according to    claim 51   , wherein the probe is attached to a glass chip.  
     
     
         53 . A method of detecting a nucleic acid comprising incubating a nucleic acid derivative according to    claim 27    with a probe.  
     
     
         54 . A method according to    claim 53   , wherein the probe is attached to a glass chip.  
     
     
         55 . A method of detecting a nucleic acid comprising incubating a nucleic acid derivative according to    claim 28    with a probe.  
     
     
         56 . A method according to    claim 55   , wherein the probe is attached to a glass chip.  
     
     
         57 . A method of detecting a nucleic acid comprising incubating a nucleic acid derivative according to    claim 29    with a probe.  
     
     
         58 . A method according to    claim 57   , wherein the probe is attached to a glass chip.  
     
     
         59 . A method of detecting a nucleic acid comprising incubating a nucleic acid derivative according to    claim 30    with a probe.  
     
     
         60 . A method according to    claim 59   , wherein the probe is attached to a glass chip.

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