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1. 发明申请

WO1994004499A1 CYANOGUANIDINES AS POTASSIUM CHANNEL BLOCKERS 审中-公开
标题翻译： CYANOGUANIDINES作为钾通道阻塞剂
公开(公告)号：WO1994004499A1
公开(公告)日：1994-03-03
申请号：PCT/US1993005458
申请日：1993-06-11
申请人： THE UPJOHN COMPANY , HUMPHREY, Stephen, J. , MEISHERI, Kaushik, D. , LUDENS, James, H. , HESTER, Jackson, B., Jr.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , C07D239/42
摘要： Cyanoguanidine compounds of formula (I) and its pharmaceutically acceptable acid addition salts wherein X is CH or N; R1 is hydrogen or methyl; R2 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C5 cycloalkyl, hydroxy-C1-C5 alkyl, methoxy-C1-C5 alkyl, or R1 and R2 are combined to form a C3-C6 carbocyclic ring; R3 and R4 are each independently selected to be hydrogen, C1-C4 alkyl, F, Cl, Br or CF3; R5 is hydrogen, F or Cl. The compounds of formula (I) are potassium channel blockers useful in the treatment of cardiovascular disorders such as congestive heart failure and hypertension.
摘要翻译：式（I）的氰基胍化合物及其药学上可接受的酸加成盐，其中X是CH或N; R1是氢或甲基; R 2是C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 3 -C 5环烷基，羟基-C 1 -C 5烷基，甲氧基-C 1 -C 5烷基或R 1和R 2结合形成C 3 -C 6碳环 ; R 3和R 4各自独立地选自氢，C 1 -C 4烷基，F，Cl，Br或CF 3; R5是氢，F或Cl。式（I）化合物是可用于治疗心血管疾病如充血性心力衰竭和高血压的钾通道阻滞剂。

2. 发明申请

WO1995020579A1 CYANOGUANIDINES AS K-CHANNEL BLOCKERS 审中-公开
标题翻译： CYANOGUANIDINES作为K-通道阻塞剂
公开(公告)号：WO1995020579A1
公开(公告)日：1995-08-03
申请号：PCT/US1995000024
申请日：1995-01-09
申请人： THE UPJOHN COMPANY , HUMPHREY, Stephen, J. , MEISHERI, Kaushik, D. , LUDENS, James, H. , HESTER, Jackson, B., Jr.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , Y10S514/869
摘要： Cyanoguanidine compounds of Formula (I) and their pharmaceutically acceptable acid addition salts where R1 is hydrogen or methyl; R2 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl C3-C5 cycloalkyl, C3-C5 cycloalkenyl, hydroxymethyl, methoxy C1-C5 alkyl, or R1 and R2 are combined to form a C3-C6 carboxyclic ring; R3 and R4 are each independently selected to be hydrogen, C1-C4 alkyl, F, Cl, Br, I or CF3; R5 is hydrogen, F or Cl; R6 is hydrogen, NH2, NHCH3, NHC2H5, NHCH(CH3)2, N(CH3)2, N(C2H5)2, NH(CH2)mOC1-C3 alkyl, NHC(O)C1-C3 alkyl, F, Cl, Br, C1-C3 alkyl, NH(CH2)mF, 1-imidazolyl, NHOC1-C3 alkyl, NHOH, NHSO2C1-C3 alkyl, SH, SC1-C3 alkyl, NHC(O)OC1-C3 alkyl, NHC(O)NHC1-C3 alkyl, NHSO2NHC1-C3 alkyl, NHSO2N(C1-C3 alkyl)2 or amino acid amide; R7 is C1-C7 alkyl, NH2, NHC1-C3 alkyl, N(C1-C3 alkyl)2, CF3, F, Cl, Br, I, OC1-C3 alkyl, OH, COOH, C(O)OC1-C3 alkyl, C(O)NH2, C(O)NHC1-C3 alkyl, C(O)C1-C3 alkyl, C(O)N(C1-C3 alkyl)2, SO2NH2, SO2NHC1-C3 alkyl, CN, SO2N(C1-C3 alkyl)2, NHC(O)C1-C3 alkyl, NHC(O)NHC1-C3 alkyl, NHC(O)N(C1-C3 alkyl)2, NHSO2NHC1-C3 alkyl, NHSO2N(C1-C3 alkyl)2, SH, SC1-C3 alkyl, NO2, SO2C1-C3 alkyl, NHC(O)OC1-C3 alkyl, amino acid amide or hydrogen; R8 is hydrogen, C1-C6 alkyl, NH2, NHC1-C3 alkyl, N(CH3)2, N(C2H5)2, F, Cl, Br, OC1-C3 alkyl or OH; and where m is 2 or 3 and n is 0 or 1 (except for those compounds where R8 is hydrogen and R6 is hydrogen, NH2, NHCH3, NHC2H5, NHCH(CH3)2, N(CH3)2, N(C2H5)2, NH(CH2)m-OC1-C3 alkyl, NHC(O)C1-C3 alkyl, Cl or Br). The compounds of Formula (I) are potassium channel blockers useful in the treatment of cardiovascular disorders such as congestive heart failure and hypertension and as a diuretic.
摘要翻译：式（I）的氰基胍化合物及其药学上可接受的酸加成盐，其中R 1是氢或甲基; R 2是C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基C 3 -C 5环烷基，C 3 -C 5环烯基，羟甲基，甲氧基C 1 -C 5烷基或R 1和R 2结合形成C 3 -C 6羧基环; R 3和R 4各自独立地选自氢，C 1 -C 4烷基，F，Cl，Br，I或CF 3; R5是氢，F或Cl; R6是氢，NH2，NHCH3，NHC2H5，NHCH（CH3）2，N（CH3）2，N（C2H5）2，NH（CH2）mOC1-C3烷基，NHC（O）C1-C3烷基， Br，C1-C3烷基，NH（CH2）mF，1-咪唑基，NHOC1-C3烷基，NHOH，NHSO2C1-C3烷基，SH，SC1-C3烷基，NHC（O）OC1-C3烷基，NHC（O） -C 3烷基，NHSO 2 NHC 1 -C 3烷基，NHSO 2 N（C 1 -C 3烷基）2或氨基酸酰胺; R 7是C 1 -C 7烷基，NH 2，NHC 1 -C 3烷基，N（C 1 -C 3烷基）2，CF 3，F，Cl，Br，I，OC 1 -C 3烷基，OH，COOH，C（O），C（O）NH2，C（O）NHCl-C3烷基，C（O）C1-C3烷基，C（O）N（C1-C3烷基）2，SO2NH2，SO2NHC1-C3烷基，CN，SO2N C 1 -C 3烷基）2，NHC（O）C 1 -C 3烷基，NHC（O）NHCl 3 C 3烷基，NHC（O）N（C 1 -C 3烷基）2，NHSO 2 NHC 1 -C 3烷基，NHSO 2 N ，SH，SC1-C3烷基，NO2，SO2C1-C3烷基，NHC（O）OC1-C3烷基，氨基酰胺或氢; R 8是氢，C 1 -C 6烷基，NH 2，NHCl-C 3烷基，N（CH 3）2，N（C 2 H 5）2，F，Cl，Br，OC 1 -C 3烷基或OH; 并且其中m为2或3且n为0或1（除了那些其中R 8为氢且R 6为氢，NH 2，NHCH 3，NHC 2 H 5，NHCH（CH 3）2，N（CH 3）2，N（C 2 H 5）2 ，NH（CH 2）m -OC 1 -C 3烷基，NHC（O）C 1 -C 3烷基，Cl或Br）。式（I）的化合物是可用于治疗心血管疾病如充血性心力衰竭和高血压以及作为利尿剂的钾通道阻滞剂。

3. 发明申请

WO1994004500A1 CYANOGUANIDINES AS POTASSIUM CHANNEL BLOCKERS 审中-公开
标题翻译： CYANOGUANIDINES作为钾通道阻塞剂
公开(公告)号：WO1994004500A1
公开(公告)日：1994-03-03
申请号：PCT/US1993006752
申请日：1993-07-21
申请人： THE UPJOHN COMPANY , HUMPHREY, Stephen, J. , MEISHERI, Kaushik, D. , LUDENS, James, H. , HESTER, Jackson, B., Jr.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , C07D239/42
摘要： Cyanoguanidine compounds of formula (I) and its pharmaceutically acceptable acid addition salts wherein R1 is hydrogen or methyl; R2 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C5 cycloalkyl, C3-C5 cycloalkenyl hydroxy methyl, methoxy-C1-C5 alkyl, or R1 and R2 are combined to form a C3-C6 carbocyclic ring; R3 and R4 are each independently selected to be hydrogen, C1-C4 alkyl, F, Cl, Br, I or CF3; R5 is hydrogen, F or Cl; R6 is hydrogen, -NH2, -NHCH3-, -NHC2H5, -NHCH(CH3)2, -N(CH3)2, -N(C2H5)2, NH(CH2)m, -OC1-C3 alkyl (where m is 2 or 3), -NHC(O)C1-C3 alkyl, Cl or Br; and n is 0 or 1. The compounds of formula (I) are potassium channel blockers useful in the treatment of cardiovascular disorders such as congestive heart failure and hypertension and as a diuretic.
摘要翻译：式（I）的氰基胍化合物及其药学上可接受的酸加成盐，其中R 1是氢或甲基; R 2是C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 3 -C 5环烷基，C 3 -C 5环烯基羟基甲基，甲氧基-C 1 -C 5烷基或R 1和R 2结合形成C 3 -C 6碳环 ; R 3和R 4各自独立地选自氢，C 1 -C 4烷基，F，Cl，Br，I或CF 3; R5是氢，F或Cl; R6是氢，-NH2，-NHCH3-，-NHC2H5，-NHCH（CH3）2，-N（CH3）2，-N（C2H5）2，NH（CH2）m，-OC1-C3烷基（其中m是 2或3），-NHC（O）C 1 -C 3烷基，Cl或Br; 并且n为0或1.式（I）化合物是可用于治疗心血管疾病如充血性心力衰竭和高血压以及作为利尿剂的钾通道阻滞剂。

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