US2004198722A1PendingUtilityA1

Collections of compounds

52
Assignee: SPIROGEN LTDPriority: Aug 27, 1998Filed: Apr 15, 2004Published: Oct 7, 2004
Est. expiryAug 27, 2018(expired)· nominal 20-yr term from priority
A61P 43/00A61P 31/00C07D 487/04
52
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Claims

Abstract

A compound of formula (I), wherein: R 2 and R 3 are independently selected from H, R, OH, OR, ═O, ═CH—R, ═CH 2 , CH 2 —CO 2 R, CH 2 —CO 2 H, CH 2 —SO 2 R, O—SO 2 R, CO 2 R, COR and CN, and there is optionally a double bond between C1 and C2 or C2 and C3; R 6 , R 7 , R 8 and R 9 are independently selected from H, R, OH, OR, halo, nitro, amino, Me 3 Sn; R 11 is either H or R; Q is S, O or NH; L is a linking group, or a single bond; O is a solid support; or where one or more of R 2 , R 3 , R 6 , R 7 and R 8 are independently: H—(T) n —X—Y—A— where: X is CO, NH, S or O; T is a combinatorial unit; Y is a divalent group such that HY═R; A is O, S, NH, or a single bond and n is a positive integer.

Claims

exact text as granted — not AI-modified
1 - 25 . Cancelled.  
     
     
         26 . A compound of formula (I):  
       
         
           
           
               
               
           
         
       
       wherein: 
 one of R 2 , R 3 , R 6 , R 7  and R 8  is X—Y—A—, where X is selected from —COZ′, NHZ, SH, or OH, where Z is either H or an nitrogen protecting group, Z′ is either OH or an acid protecting group, Y is a divalent group such that HY═R, and A is O, S, NH, or a single bond;  
 R 2  and R 3  (if not X—Y—A—) are independently selected from: H, R, OH, OR, ═O, ═CH—R, ═CH 2 , CH 2 —CO 2 R, CH 2 —CO 2 H, CH 2 —SO 2 R, O—SO 2 R, CO 2 R, COR and CN, and there is optionally a double bond between C1 and C2 or C2 and C3;  
 R 6 , R 7 , R 8  and R 9  (if not X—Y—A—) are independently selected from H, R, OH, OR, halo, nitro, amino, Me 3 Sn; or R 7  and R 8  together form a group —O—(CH 2 ) p —O—, where p is 1 or 2;  
 R 11  is either H or R;  
 Q is S, O or NH;  
 L is a linking group, or a single bond;  
 O is a solid support;  
 where R is a lower alkyl group having 1 to 10 carbon atoms, or an aralkyl group of up to 12 carbon atoms, whereof the alkyl group optionally contains one or more carbon-carbon double or triple bonds, which may form part of a conjugated system, or an aryl group of up to 12 carbon atoms; and is optionally substituted by one or more halo, hydroxy, amino, or nitro groups, and optionally contains one or more hetero atoms, which may form part of, or be, a functional group.  
 
     
     
         27 . A compound according to  claim 26 , wherein it is either R 2  and/or R 8  that is X—Y—A—.  
     
     
         28 . A compound according to  claim 26 , wherein R, and HY if Y is present, are independently selected from lower alkyl group having 1 to 10 carbon atoms, or an alkaryl group of up to 12 carbon atoms, or an aryl group of up to 12 carbon atoms, optionally substituted by one or more halo, hydroxy, amino, or nitro groups.  
     
     
         29 . A compound according to  claim 28 , wherein R, and HY, if Y is present, are independently selected from lower alkyl group having 1 to 10 carbon atoms optionally substituted by one or more halo, hydroxy, amino, or nitro groups.  
     
     
         30 . A compound according to  claim 29 , wherein R, and HY, if Y is present, are unsubstituted straight or branched chain alkyl groups, having 1 to 10 carbon atoms.  
     
     
         31 . A compound according to  claim 26 , wherein Q is O.  
     
     
         32 . A compound according to  claim 26 , wherein R 11  is H.  
     
     
         33 . A compound according to  claim 26 , wherein R 6  and R 9  are H.  
     
     
         34 . A compound according to  claim 26 , wherein R 7  is an alkoxy group.  
     
     
         35 . A compound according to  claim 26 , wherein R 2  and R 3  are H.  
     
     
         36 . A collection of compounds all of which are represented by formula (I):  
       
         
           
           
               
               
           
         
       
       wherein one of R 2 , R 3 , R 6 , R 7  and R 8  is H—(T) n —X′—Y—A—, where: 
 X′ is CO, NH, S or O,;  
 Y is a divalent group such that HY═R;  
 A is O, S, NH or a single bond;  
 T is a combinatorial unit;  
 and n is a positive integer.  
 R 2  and R 3  (if not H—(T) n —X′—Y—A—) are independently selected from: H, R, OH, OR, ═O, ═CH—R, ═CH 2 , CH 2 —CO 2 R, CH 2 —CO 2 H, CH 2 —SO 2 R, O—SO 2 R, CO 2 R, COR and CN, and there is optionally a double bond between C1 and C2 or C2 and C3;  
 R 6 , R 7 , R 8  and R 9  (if not H—(T) n —X′—Y—A—) are independently selected from H, R, OH, OR, halo, nitro, amino, Me 3 Sn; or R 7  and R 8  together form a group —O—(CH 2 ) p —O—, where p is 1 or 2;  
 R 11  is either H or R;  
 Q is S, O or NH;  
 L is a linking group, or a single bond;  
 O is a solid support;  
 where R is a lower alkyl group having I to 10 carbon atoms, or an aralkyl group of up to 12 carbon atoms, whereof the alkyl group optionally contains one or more carbon-carbon double or triple bonds, which may form part of a conjugated system, or an aryl group of up to 12 carbon atoms; and is optionally substituted by one or more halo, hydroxy, amino, or nitro groups, and optionally contains one or more hetero atoms, which may form part of, or be, a functional group.  
 
     
     
         37 . A collection of compounds according to  claim 36 , wherein it is R 2  and/or R 8  that are independently: 
       H—(T) n —X′—Y—A—. 
     
     
         38 . A collection of compounds according to  claim 36 , wherein X′ is either CO or NH.  
     
     
         39 . A collection of compounds according to  claim 36 , wherein n is from 1 to 16.  
     
     
         40 . A collection of compounds according to  claim 39 , wherein n is from 3 to 14.  
     
     
         41 . A collection of compounds all of which are represented by formula (II):  
       
         
           
           
               
               
           
         
       
       wherein one of R 2 , R 3 , R 6 , R 7  and R 8  is H—(T) n —X′—Y—A—, where: 
 X′ is CO, NH, S or O,;  
 Y is a divalent group such that HY═R;  
 A is O, S, NH or a single bond;  
 T is a combinatorial unit;  
 and n is a positive integer.  
 R 2  and R 3  (if not H—(T) n —X′—Y—A—) are independently selected from: H, R, OH, OR, ═O, ═CH—R, ═CH 2 , CH 2 —CO 2 R, CH 2 —CO 2 H, CH 2 —SO 2 R, O—SO 2 R, CO 2 R, COR and CN, and there is optionally a double bond between C1 and C2 or C2 and C3;  
 R 6 , R 7 , R 8  and R 9  (if not H—(T) n —X′—Y—A—) are independently selected from H, R, OH, OR, halo, nitro, amino, Me 3 Sn; or R 7  and R 8  together form a group —O—(CH 2 ) p —O—, where p is 1 or 2;  
 where R is a lower alkyl group having 1 to 10 carbon atoms, or an aralkyl group of up to 12 carbon atoms, whereof the alkyl group optionally contains one or more carbon-carbon double or triple bonds, which may form part of a conjugated system, or an aryl group of up to 12 carbon atoms; and is optionally substituted by one or more halo, hydroxy, amino, or nitro groups, and optionally contains one or more hetero atoms, which may form part of, or be, a functional group.  
 
     
     
         42 . A collection of compounds according to  claim 41 , wherein it is R 2  and/or R 8  that are independently: 
       H—(T) n —X′—Y—A—. 
     
     
         43 . A collection of compounds according to  claim 41 , wherein X′ is either CO or NH.  
     
     
         44 . A collection of compounds according to  claim 41 , wherein n is from 1 to 16.  
     
     
         45 . A collection of compounds according to  claim 44 , wherein n is from 3 to 14.  
     
     
         46 . A method of screening a collection of compounds according to  claim 41  to discover biologically active compounds.

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