公开(公告)号：US20080312253A1

公开(公告)日：2008-12-18

申请号：US12213067

申请日：2008-06-13

申请人： Ghil Soo Nam ,  Hye Whon Rhim ,  Ae Nim Pae ,  Kyung II Choi ,  Hyun Ah Choo ,  Seung Yeol Nah

发明人： Ghil Soo Nam ,  Hye Whon Rhim ,  Ae Nim Pae ,  Kyung II Choi ,  Hyun Ah Choo ,  Seung Yeol Nah

IPC分类号： A61K31/496 ,  A61P25/16 ,  A61P25/28 ,  A61P25/18

CPC分类号： A61K31/496

摘要： The present invention relates to a pharmaceutical composition containing a pyrazole derivative as an active ingredient, which has antagonistic activity against serotonin 5-HT3A and is effective for the prevention and treatment of central nervous system (CNS) diseases, including emesis, nausea, alcoholism, drug abuse, depression, compulsive neurosis, anxiety, seizure, Alzheimer's disease, Parkinson's disease, Huntington's chorea, psychosis, schizophrenia, suicidal tendency, sleep disorder, appetite disorder and migraine.

摘要翻译： 本发明涉及含有吡唑衍生物作为活性成分的药物组合物，其对5-羟色胺5-HT3A具有拮抗作用，对预防和治疗中枢神经系统（CNS）疾病有效，包括呕吐，恶心，酒精中毒， 药物滥用，抑郁症，强迫性神经症，焦虑症，癫痫发作，阿尔茨海默病，帕金森病，亨廷顿舞蹈病，精神病，精神分裂症，自杀倾向，睡眠障碍，食欲障碍和偏头痛。

公开(公告)号：US08748422B2

公开(公告)日：2014-06-10

申请号：US12195951

申请日：2008-08-21

申请人： Ghil Soo Nam ,  Hye Whon Rhim ,  Ae Nim Pae ,  Hyun Ah Choo ,  Kyung Il Choi ,  Seung Yeol Nah

发明人： Ghil Soo Nam ,  Hye Whon Rhim ,  Ae Nim Pae ,  Hyun Ah Choo ,  Kyung Il Choi ,  Seung Yeol Nah

IPC分类号： A61K31/5377 ,  A61K31/517 ,  A61P25/00

CPC分类号： A61K31/517 ,  A61K31/5377

摘要： The present invention relates to a pharmaceutical composition containing one or more quinazoline compounds as an active ingredient, which has antagonistic activity against serotonin 5-HT3A and is effective for the prevention and treatment of central nervous system (CNS) diseases, including emesis, nausea, alcoholism, drug abuse, depression, compulsive neurosis, anxiety, seizure, Alzheimer's disease, Parkinson's disease, Huntington's chorea, psychosis, schizophrenia, suicidal tendency, sleep disorder, appetite disorder and migraine.

摘要翻译： 本发明涉及一种含有一种或多种喹唑啉化合物作为活性成分的药物组合物，其对5-羟色胺5-HT3A具有拮抗作用，对预防和治疗中枢神经系统（CNS）疾病有效，包括呕吐，恶心， 酒精中毒，药物滥用，抑郁症，强迫性神经症，焦虑症，癫痫发作，阿尔茨海默病，帕金森病，亨廷顿舞蹈病，精神病，精神分裂症，自杀倾向，睡眠障碍，食欲障碍和偏头痛。

公开(公告)号：US08673856B2

公开(公告)日：2014-03-18

申请号：US12513182

申请日：2007-11-02

申请人： Jae II Kim ,  Hye Whon Rhim ,  Hyun Jeong Kim ,  Hong Won Suh ,  Soung Hun Roh ,  Jung A Yun ,  Seung Kyu Lee ,  Young Jae Eu ,  Heung Sik Na

发明人： Jae II Kim ,  Hye Whon Rhim ,  Hyun Jeong Kim ,  Hong Won Suh ,  Soung Hun Roh ,  Jung A Yun ,  Seung Kyu Lee ,  Young Jae Eu ,  Heung Sik Na

IPC分类号： A61K38/16 ,  A61K38/00 ,  C07K14/00

CPC分类号： C07K14/43504 ,  A61K38/00

摘要： The present invention relates to a method for increasing the binding reversibility of a ω-conotoxin to a N-type calcium channel, which comprises preparing a ω-conotoxin having a Ile and/or Ala residue at a position of amino acid (11 and/or 12), respectively in the second loop between cysteine residues (2 and 3) of the ω-conotoxin represented by the formula I, such that the prepared ω-conotoxin has the increased binding reversibility to N-type calcium channel. In addition, the present invention relates to a novel ω-conotoxin and a pharmaceutical composition having plausible properties in view of blocking activity to and specificity to N-type calcium channel, and dramatically improved binding reversibility to N-type calcium channel.

摘要翻译： 本发明涉及一种增加ω-芋螺毒素与N型钙通道的结合可逆性的方法，其包括在氨基酸（11和/或其氨基酸）的位置制备具有Ile和/或Ala残基的ω-芋螺毒素， 或12）分别在由式I表示的ω-芋螺毒素的半胱氨酸残基（2和3）之间的第二环中，使得所制备的ω-芋螺毒素具有增加的对N-型钙通道的结合可逆性。 此外，本发明涉及一种新型的ω-芋螺毒素和具有似乎合理的性质的药物组合物，其特征在于阻断N-型钙通道的活性和特异性，并显着提高了对N-型钙通道的结合可逆性。

公开(公告)号：US20100056456A1

公开(公告)日：2010-03-04

申请号：US12513182

申请日：2007-11-02

申请人： Jae Il Kim ,  Hye Whon Rhim ,  Hyun Jeong Kim ,  Hong Won Suh ,  Soung Hun Roh ,  Jung A. Yun ,  Seung Kyu Lee ,  Young Jae Eu ,  Heung Sik Na

发明人： Jae Il Kim ,  Hye Whon Rhim ,  Hyun Jeong Kim ,  Hong Won Suh ,  Soung Hun Roh ,  Jung A. Yun ,  Seung Kyu Lee ,  Young Jae Eu ,  Heung Sik Na

IPC分类号： A61K38/10 ,  C07K7/08 ,  C07H21/00 ,  A61P25/00

CPC分类号： C07K14/43504 ,  A61K38/00

摘要： The present invention relates to a method for increasing the binding reversibility of a ω-conotoxin to a N-type calcium channel, which comprises preparing a ω-conotoxin having a Ile and/or Ala residue at a position of amino acid (11 and/or 12), respectively in the second loop between cysteine residues (2 and 3) of the ω-conotoxin represented by the formula I, such that the prepared ω-conotoxin has the increased binding reversibility to N-type calcium channel. In addition, the present invention relates to a novel ω-conotoxin and a pharmaceutical composition having plausible properties in view of blocking activity to and specificity to N-type calcium channel, and dramatically improved binding reversibility to N-type calcium channel.

摘要翻译： 本发明涉及一种增加ω-芋螺毒素与N-型钙通道的结合可逆性的方法，其包括在氨基酸（11和/或其氨基酸）的位置制备具有Ile和/或Ala残基的ω-芋螺毒素， 或12）分别在由式I表示的ω-芋螺毒素的半胱氨酸残基（2和3）之间的第二环中，使得制备的ω-芋螺毒素对N-型钙通道具有增加的结合可逆性。 此外，本发明涉及一种新型的ω-芋螺毒素和具有似乎合理的性质的药物组合物，其特征在于阻断N-型钙通道的活性和特异性，并显着提高了与N-型钙通道的结合可逆性。