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公开(公告)号：WO1996040686A1
公开(公告)日：1996-12-19
申请号：PCT/US1996009042
申请日：1996-06-06
Applicant: ABBOTT LABORATORIES
Inventor： ABBOTT LABORATORIES , BHAGWAT, Shripad, S. , COWART, Marlon, Daniel
IPC: C07D487/04
CPC classification number: C07D473/00 , C07D471/04 , C07F9/6561 , Y02P20/55
Abstract: The present invention provides new heterocyclic substituted cyclopentane compounds of formula (I), wherein X is -N or -CR7, where R7 is hydrogen, halogen, loweralkyl, loweralkoxy or -S-loweralkyl; Y is -N or -CH; R1 and R2 are each independently hydrogen, hydroxy, alkoxy, or acyloxy or R1 and R2 are both hydroxy protected with an individual hydroxy protecting group or with a single dihydroxy-protecting group or R1 and R2 are absent and there is a double bond between the carbon atoms to which R1 and R2 are attached; R3 is hydrogen, hydroxy, loweralkyl or alkoxy; R4 is (a) hydrogen, (b) amino, (c) halogen, (d) hydroxy, (e) sulfonamido, (f) -P(O)(OH)2, (g) -P(O)-R8R9, wherein R8 and R9 are each independently hydrogen, hydroxy, loweralkyl, aryl or arylalkyl, (h) -NHR10, wherein R10 is hydrogen or an amino protecting group, (i) -NHC(O)NHR11, where R11 is hydrogen or loweralkyl, or (j) -A-R12 wherein A is O, S(O)n or -N(R13)- wherein R13 is hydrogen or loweralkyl, n is zero, one or two, and R12 is hydrogen, loweralkyl, alkylsulfonyl, acyl, alkoxycarbonyl, aryl, heteroaryl, arylalkyl, arylsulfonyl, haloalkyl, heteroarylalkyl, heteroarylsulfonyl, aminoalkyl or heterocyclic or (k) R4 is a ring N-member of a heteroaryl or heterocycle; or R3 and R4 taken together are =O, or taken together with the carbon atom to which they are attached, form a spirocyclic ring; R5 is hydrogen, loweralkyl, aryl, arylalkyl, heteroaryl, amino, alkylamino, alkoxy, acylamino, arylalkynyl, arylamino, arylmercapto, alkylmercapto, halogen, heterocyclic, hydrazino, -NHC(O)NH2, or -NR14R15 wherein R14 and R15 are each independently hydrogen or an amino protecting group or -NR14R15 is a nitrogen containing heterocycle of 5 to 7 members; and R6 is loweralkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkoxycarbonyl, carboxy, aryl, heteroaryl, heteroarylalkyl, arylalkyl, arylalkenyl, arylalkynyl, cyano, halogen, heteroarylalkynyl, or -C(O)NHR16, wherein R16 is alkyl, aryl, or heterocyclic. The present invention also provides pharmaceutical compositions containing such compounds and methods of using such compounds for inhibiting adenosine kinase.
Abstract translation: 本发明提供新的式（I）的杂环取代的环戊烷化合物，其中X是-N或-CR 7，其中R 7是氢，卤素，低级烷基，低级烷氧基或-S-低级烷基; Y是-N或-CH; R 1和R 2各自独立地为氢，羟基，烷氧基或酰氧基，或者R 1和R 2均用单独的羟基保护基或单个二羟基保护基进行羟基保护，或者R1和R2不存在，并且在 R1和R2所连接的碳原子; R3是氢，羟基，低级烷基或烷氧基; R4是（a）氢，（b）氨基，（c）卤素，（d）羟基，（e）亚磺酰氨基，（f）-P（O）（OH）2，（g）-P（O）-R8R9 其中R 8和R 9各自独立地是氢，羟基，低级烷基，芳基或芳基烷基，（h）-NHR 10，其中R 10是氢或氨基保护基，（i）-NHC（O）NHR 11，其中R 11是氢或低级烷基 ，或（j）-A-R12，其中A是O，S（O）n或-N（R13） - ，其中R13是氢或低级烷基，n是0,1或2，R12是氢，低级烷基，烷基磺酰基， 酰基，烷氧基羰基，芳基，杂芳基，芳基烷基，芳基磺酰基，卤代烷基，杂芳基烷基，杂芳基磺酰基，氨基烷基或杂环或（k）R4是杂芳基或杂环的环N-成员; 或R 3和R 4一起为= O，或与它们所连接的碳原子一起形成螺环; R5是氢，低级烷基，芳基，芳基烷基，杂芳基，氨基，烷基氨基，烷氧基，酰基氨基，芳基炔基，芳基氨基，芳基巯基，烷基巯基，卤素，杂环，肼基，-NHC（O）NH2或-NR14R15，其中R14和R15各自 独立地是氢或氨基保护基或-NR14R15是5-7个成员的含氮杂环; 芳基，芳基烯基，芳基炔基，氰基，卤素，杂芳基炔基或-C（O）NHR 16，其中R 16是烷基，芳基，杂芳基， 或杂环。 本发明还提供含有这些化合物的药物组合物和使用这些化合物抑制腺苷激酶的方法。
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公开(公告)号：EP0873340A1
公开(公告)日：1998-10-28
申请号：EP96918151.0
申请日：1996-06-06
Applicant: Abbott Laboratories
Inventor： BHAGWAT, Shripad, S. , COWART, Marlon, Daniel
CPC classification number: C07D473/00 , C07D471/04 , C07F9/6561 , Y02P20/55
Abstract: The present invention provides new heterocyclic substituted cyclopentane compounds of formula (I), wherein X is -N or -CR7, where R7 is hydrogen, halogen, loweralkyl, loweralkoxy or -S-loweralkyl; Y is -N or -CH; R1 and R2 are each independently hydrogen, hydroxy, alkoxy, or acyloxy or R1 and R2 are both hydroxy protected with an individual hydroxy protecting group or with a single dihydroxy-protecting group or R1 and R2 are absent and there is a double bond between the carbon atoms to which R1 and R2 are attached; R3 is hydrogen, hydroxy, loweralkyl or alkoxy; R4 is (a) hydrogen, (b) amino, (c) halogen, (d) hydroxy, (e) sulfonamido, (f) -P(O)(OH)2, (g) -P(O)-R8R9, wherein R8 and R9 are each independently hydrogen, hydroxy, loweralkyl, aryl or arylalkyl, (h) -NHR10, wherein R10 is hydrogen or an amino protecting group, (i) -NHC(O)NHR11, where R11 is hydrogen or loweralkyl, or (j) -A-R12 wherein A is O, S(O)n or -N(R13)- wherein R13 is hydrogen or loweralkyl, n is zero, one or two, and R12 is hydrogen, loweralkyl, alkylsulfonyl, acyl, alkoxycarbonyl, aryl, heteroaryl, arylalkyl, arylsulfonyl, haloalkyl, heteroarylalkyl, heteroarylsulfonyl, aminoalkyl or heterocyclic or (k) R4 is a ring N-member of a heteroaryl or heterocycle; or R3 and R4 taken together are =O, or taken together with the carbon atom to which they are attached, form a spirocyclic ring; R5 is hydrogen, loweralkyl, aryl, arylalkyl, heteroaryl, amino, alkylamino, alkoxy, acylamino, arylalkynyl, arylamino, arylmercapto, alkylmercapto, halogen, heterocyclic, hydrazino, -NHC(O)NH2, or -NR14R15 wherein R14 and R15 are each independently hydrogen or an amino protecting group or -NR14R15 is a nitrogen containing heterocycle of 5 to 7 members; and R6 is loweralkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkoxycarbonyl, carboxy, aryl, heteroaryl, heteroarylalkyl, arylalkyl, arylalkenyl, arylalkynyl, cyano, halogen, heteroarylalkynyl, or -C(O)NHR16, wherein R16 is alkyl, aryl, or heterocyclic. The present invention also provides pharmaceutical compositions containing such compounds and methods of using such compounds for inhibiting adenosine kinase.
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公开(公告)号：EP0873340B1
公开(公告)日：2001-11-21
申请号：EP96918151.0
申请日：1996-06-06
Applicant: Abbott Laboratories
Inventor： BHAGWAT, Shripad, S. , COWART, Marlon, Daniel
IPC: C07D487/04
CPC classification number: C07D473/00 , C07D471/04 , C07F9/6561 , Y02P20/55
Abstract: The present invention provides new heterocyclic substituted cyclopentane compounds of formula (I), wherein X is -N or -CR7, where R7 is hydrogen, halogen, loweralkyl, loweralkoxy or -S-loweralkyl; Y is -N or -CH; R1 and R2 are each independently hydrogen, hydroxy, alkoxy, or acyloxy or R1 and R2 are both hydroxy protected with an individual hydroxy protecting group or with a single dihydroxy-protecting group or R1 and R2 are absent and there is a double bond between the carbon atoms to which R1 and R2 are attached; R3 is hydrogen, hydroxy, loweralkyl or alkoxy; R4 is (a) hydrogen, (b) amino, (c) halogen, (d) hydroxy, (e) sulfonamido, (f) -P(O)(OH)2, (g) -P(O)-R8R9, wherein R8 and R9 are each independently hydrogen, hydroxy, loweralkyl, aryl or arylalkyl, (h) -NHR10, wherein R10 is hydrogen or an amino protecting group, (i) -NHC(O)NHR11, where R11 is hydrogen or loweralkyl, or (j) -A-R12 wherein A is O, S(O)n or -N(R13)- wherein R13 is hydrogen or loweralkyl, n is zero, one or two, and R12 is hydrogen, loweralkyl, alkylsulfonyl, acyl, alkoxycarbonyl, aryl, heteroaryl, arylalkyl, arylsulfonyl, haloalkyl, heteroarylalkyl, heteroarylsulfonyl, aminoalkyl or heterocyclic or (k) R4 is a ring N-member of a heteroaryl or heterocycle; or R3 and R4 taken together are =O, or taken together with the carbon atom to which they are attached, form a spirocyclic ring; R5 is hydrogen, loweralkyl, aryl, arylalkyl, heteroaryl, amino, alkylamino, alkoxy, acylamino, arylalkynyl, arylamino, arylmercapto, alkylmercapto, halogen, heterocyclic, hydrazino, -NHC(O)NH2, or -NR14R15 wherein R14 and R15 are each independently hydrogen or an amino protecting group or -NR14R15 is a nitrogen containing heterocycle of 5 to 7 members; and R6 is loweralkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkoxycarbonyl, carboxy, aryl, heteroaryl, heteroarylalkyl, arylalkyl, arylalkenyl, arylalkynyl, cyano, halogen, heteroarylalkynyl, or -C(O)NHR16, wherein R16 is alkyl, aryl, or heterocyclic. The present invention also provides pharmaceutical compositions containing such compounds and methods of using such compounds for inhibiting adenosine kinase.
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