公开(公告)号：EP1339719B1

公开(公告)日：2004-06-16

申请号：EP01997491.4

申请日：2001-11-21

申请人： SANOFI-SYNTHELABO

发明人： BARTH, Francis ,  BICHON, Daniel ,  BOLKENIUS, Frank ,  VAN DORSSELAER, Viviane

IPC分类号： C07D487/06 ,  A61K31/5517 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00

CPC分类号： C07D487/06

摘要： The invention concerns benzimidazole derivatives of general formula (I), wherein: X represents a nitrogen atom or a carbon atom; when X represents a nitrogen atom, R3 represents in particular a hydrogen atom or a C1-C4 alkyl group; R4 represents in particular a hydrogen atom, a C1-C6 alkyl, C3-C7 cycloalkyl, 4-piperidyl, -(CH2)p-NR5R6, -(CH2)p-CONR5R6, -CO-(CH2)p-NR5R6, -(CH2)p-phenyl, -(CH2)p-morpholinyl, -(CH2)p-pyrrolidinyl, -(CH2)p-tetrahydro-isoquinoline, -(CH2)p-heteoraryl, heteroarylcarbonyl, phenylcarbonyl, C1-C6 alkylcarbonyl, -(-CH2)p-COOR', or phenylsulphonyl group; and when X represents a carbon atom, R3 represents a hydrogen atom, a -NR5R6, -NHCOR7, -CONHR5, -COR7, -NHCONH2, -OH or -CH2OH; R4 represents in particular a hydrogen atom, a -(CH2)p-phenyl group optionally substituted, a -(CH2)p-heteroaryl or a (CH2)tNR7R8 group. The compounds of formula (I) of the invention can be used for preparing a medicine for treating or preventing disorders wherein the PARP enzyme is involved.

公开(公告)号：EP1309594A1

公开(公告)日：2003-05-14

申请号：EP01960871.0

申请日：2001-08-06

申请人： SANOFI-SYNTHELABO

发明人： BARTH, Francis ,  BICHON, Daniel ,  BOLKENIUS, Frank ,  VAN DORSSELAER, Viviane

IPC分类号： C07D471/06 ,  A61K31/4375 ,  A61K31/55 ,  C07D487/06 ,  A61P9/00

CPC分类号： C07D471/06 ,  C07D487/06

摘要： The invention concerns benzimidazole derivatives of general formula (I) wherein: X represents a nitrogen atom or a carbon atom, and when X represents a nitrogen atom: R3 represents a hydrogen atom or a C1-C4 alkyl group, or does not exist to produce compounds of formula (I) comprising a secondary or tertiary amine; R4 represents a hydrogen atom or a C1-C6 alkyl, C3-C7 cycloalkyl, C3-C7 heterocycloalkyl group optionally substituted, -(CH2)p-heteroaryl, heteroarylcarbonyl, phenylcarbonyl, C1-C6 alkylcarbonyl, -(CH2)pCOOR, phenylsulphonyl group optionally substituted; and when X represents a carbon atom: R3 represents a hydrogen atom or a -NR5R6, -N(R5)3+, -NHCOR7, -CONHR5, -COR7, -NHCONH¿2?, -OH or CH2OH group, R4 represents a hydrogen atom or a -(CH2)p-phenyl group optionally substituted, -(CH2)p-heteroaryl or-(CH2)tNR7R8 group. The invention is useful in therapeutics for preparing a medicine for preventing or treating disorders wherein the poly(ADP-ribose) polymerase is involved.

公开(公告)号：EP1339719A1

公开(公告)日：2003-09-03

申请号：EP01997491.4

申请日：2001-11-21

申请人： SANOFI-SYNTHELABO

发明人： BARTH, Francis ,  BICHON, Daniel ,  BOLKENIUS, Frank ,  VAN DORSSELAER, Viviane

IPC分类号： C07D487/06 ,  A61K31/5517 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00

CPC分类号： C07D487/06

摘要： The invention concerns benzimidazole derivatives of general formula (I), wherein: X represents a nitrogen atom or a carbon atom; when X represents a nitrogen atom, R3 represents in particular a hydrogen atom or a C1-C4 alkyl group; R4 represents in particular a hydrogen atom, a C1-C6 alkyl, C3-C7 cycloalkyl, 4-piperidyl, -(CH2)p-NR5R6, -(CH2)p-CONR5R6, -CO-(CH2)p-NR5R6, -(CH2)p-phenyl, -(CH2)p-morpholinyl, -(CH2)p-pyrrolidinyl, -(CH2)p-tetrahydro-isoquinoline, -(CH2)p-heteoraryl, heteroarylcarbonyl, phenylcarbonyl, C1-C6 alkylcarbonyl, -(-CH2)p-COOR', or phenylsulphonyl group; and when X represents a carbon atom, R3 represents a hydrogen atom, a -NR5R6, -NHCOR7, -CONHR5, -COR7, -NHCONH2, -OH or -CH2OH; R4 represents in particular a hydrogen atom, a -(CH2)p-phenyl group optionally substituted, a -(CH2)p-heteroaryl or a (CH2)tNR7R8 group. The compounds of formula (I) of the invention can be used for preparing a medicine for treating or preventing disorders wherein the PARP enzyme is involved.

摘要翻译： 本发明涉及通式（I）的苯并咪唑衍生物，其中：X代表氮原子或碳原子; 当X代表氮原子时，R3特别代表氢原子或C1-C4烷基; R 4特别代表氢原子，C 1 -C 6烷基，C 3 -C 7环烷基，4-哌啶基， - （CH 2）p -NR 5 R 6， - （CH 2）p -CONR 5 R 6，-CO-（CH 2）p -NR 5 R 6， - （CH2）p-苯基， - （CH2）p-吗啉基， - （CH2）p-吡咯烷基， - （CH2）p-四氢异喹啉， - （CH2）p-杂芳酰基，杂芳基羰基，苯基羰基， - （ - CH 2）p -COOR'或苯磺酰基; 当X代表碳原子时，R 3代表氢原子，-NR 5 R 6，-NHCOR 7，-CONHR 5，-COR 7，-NHCONH 2，-OH或-CH 2 OH; R4特别表示氢原子，任选取代的 - （CH2）p-苯基， - （CH2）p-杂芳基或（CH2）tNR7R8基团。 本发明的式（I）化合物可用于制备用于治疗或预防PARP酶参与的病症的药物。