公开(公告)号：US06288041B1

公开(公告)日：2001-09-11

申请号：US08981240

申请日：1997-12-19

申请人： Haruyuki Chaki ,  Naoko Ando ,  Tetsuo Jikihara ,  Ken-ichi Saito ,  Tomoko Yugami

发明人： Haruyuki Chaki ,  Naoko Ando ,  Tetsuo Jikihara ,  Ken-ichi Saito ,  Tomoko Yugami

IPC分类号： A61K3170

CPC分类号： C07H15/12 ,  C07H15/04 ,  C07J41/0005 ,  G01N33/50

摘要： Sialic acid derivatives represented by the following general formula: wherein R1 represents a residue of a steroid compound excluding cholestane and cholestene residues, R2 represents hydrogen or methyl group, R3 represents a C1-C6 alkyl group and other, R4 represents hydrogen or acyl group, R5 represents a group of R15O— (R15 represents a C2-C7 acyl group and other), and X represents oxygen or sulfur atom, and their derivatives. These derivatives have activating effect on choline acetyltransferase activity in the chlonergic neurons, and are useful for preventive and therapeutic treatment of dementia, memory disorder, peripheral nervous disorder and so forth.

摘要翻译： 由以下通式表示的唾液酸衍生物：其中R1表示除胆甾烷和胆固醇残基之外的类固醇化合物的残基，R 2表示氢或甲基，R 3表示C 1 -C 6烷基等，R 4表示氢或酰基， R5表示R15O-（R15表示C2-C7酰基等），X表示氧或硫原子的基团及其衍生物。 这些衍生物对胆碱能神经元中的胆碱乙酰转移酶活性具有活化作用，并且可用于预防和治疗痴呆，记忆障碍，周围神经障碍等。

公开(公告)号：US5783564A

公开(公告)日：1998-07-21

申请号：US669219

申请日：1996-06-24

申请人： Haruyuki Chaki ,  Naoko Ando ,  Yasuhiro Morinaka ,  Ken-ichi Saito ,  Tomoko Yugami ,  Rie Yoshida

发明人： Haruyuki Chaki ,  Naoko Ando ,  Yasuhiro Morinaka ,  Ken-ichi Saito ,  Tomoko Yugami ,  Rie Yoshida

IPC分类号： C07J17/00 ,  C07J41/00 ,  A61K31/70 ,  A61K31/58

CPC分类号： C07J41/0005 ,  C07J17/005

摘要： Sialic acid derivatives represented by the general formula (I): wherein R.sup.1 is a steroidal compound residue; R.sup.2 is H or alkyl; R.sup.3 is alkyl; ##STR1## wherein each of R.sup.6 and R.sup.7 is H, alkyl or the like and I is an integer of 0 to 6; or the like; X is O or S; R.sup.4 is H or acyl; and R.sup.5 is R.sup.14 O--(R.sup.14 is H or acyl) or R.sup.15 NH--(R.sup.15 is acyl or the like); their salts, hydrates or solvates are provided. Sialic acid derivatives of the present invention are expected to be effective medicines for the prevention and therapy of senile dementia including Alzheimer's disease and the like, because they increase ChAT activity in cholinergic neurons.

摘要翻译： 由通式（I）表示的唾液酸衍生物：其中R1是甾族化合物残基; R2是H或烷基; R3是烷基; 其中R6和R7各自为H，烷基等，I为0-6的整数; 或类似物; X是O或S; R4是H或酰基; R5为R14O-（R14为H或酰基）或R15NH-（R15为酰基等）; 提供它们的盐，水合物或溶剂合物。 预期本发明的唾液酸衍生物是预防和治疗老年性痴呆（包括阿尔茨海默氏病等）的有效药物，因为它们增加胆碱能神经元中的ChAT活性。

公开(公告)号：US5712254A

公开(公告)日：1998-01-27

申请号：US362947

申请日：1994-12-23

申请人： Haruyuki Chaki ,  Naoko Ando ,  Yasuhiro Morinaka ,  Ken-Ichi Saito ,  Tomoko Yugami ,  Rie Yoshida

发明人： Haruyuki Chaki ,  Naoko Ando ,  Yasuhiro Morinaka ,  Ken-Ichi Saito ,  Tomoko Yugami ,  Rie Yoshida

IPC分类号： C07J17/00 ,  C07J41/00 ,  A61K31/70 ,  A61K31/58 ,  C07D315/00

CPC分类号： C07J41/0005 ,  C07J17/005

摘要： Sialic acid derivatives represented by the general formula (I): ##STR1## wherein R.sup.1 is a steroidal compound residue; R.sup.2 is H or alkyl; R.sup.3 is alkyl; ##STR2## wherein each of R.sup.6 and R.sup.7 is H, alkyl or the like and I is an integer of 0 to 6; or the like; X is O or S; R.sup.4 is H or acyl; and R.sup.5 is R.sup.14 O-- (R.sup.14 is H or acyl) or R.sup.15 NH--(R.sup.15 is acyl or the like); their salts, hydrates or solvates are provided. Sialic acid derivatives of the present invention are expected to be effective medicines for the prevention and therapy of senile dementia including Alzheimer's disease and the like, because they increase ChAT activity in cholinergic neurons.

摘要翻译： 由通式（I）表示的唾液酸衍生物：其中R1是甾族化合物残基; R2是H或烷基; R3是烷基; 其中R6和R7各自为H，烷基等，I为0-6的整数; 或类似物; X是O或S; R4是H或酰基; R5为R14O-（R14为H或酰基）或R15NH-（R15为酰基等）; 提供它们的盐，水合物或溶剂合物。 预期本发明的唾液酸衍生物是预防和治疗老年性痴呆（包括阿尔茨海默氏病等）的有效药物，因为它们增加胆碱能神经元中的ChAT活性。