公开(公告)号：US5985844A

公开(公告)日：1999-11-16

申请号：US855242

申请日：1992-03-26

申请人： James V. Heck ,  William J. Leanza ,  Ronald W. Ratcliffe ,  Thomas N. Salzmann ,  Kothandaraman Shankaran ,  Michael J. Szymonifka ,  Robert R. Wilkening

发明人： James V. Heck ,  William J. Leanza ,  Ronald W. Ratcliffe ,  Thomas N. Salzmann ,  Kothandaraman Shankaran ,  Michael J. Szymonifka ,  Robert R. Wilkening

IPC分类号： C07H17/08

CPC分类号： C07H17/08

摘要： Compounds of the formula: ##STR1## where R is hydrogen, hydroxyl, alkyl or acyl, R' and R" together are oxo, hydroxyimino or alkoxyimino, and R' and R" independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.

摘要翻译： 下式的化合物：其中R是氢，羟基，烷基或酰基，R'和R“一起是氧代，羟基亚氨基或烷氧基亚氨基，R'和R”独立地是氢，羟基，酰氧基或被任何 的氢，烷基羰基，芳基羰基，芳烷基羰基，烷氧基羰基，芳烷氧基羰基，烷基磺酰基或芳基磺酰基，n为0或1，及其药学上可接受的盐。 这些化合物是大环内酯类抗生素，也可用作合成其他大环内酯抗生素的中间体。 还提供了其使用的药物组合物和方法。

公开(公告)号：US4374848A

公开(公告)日：1983-02-22

申请号：US301544

申请日：1981-09-14

申请人： Burton G. Christensen ,  James V. Heck ,  Michael J. Szymonifka

发明人： Burton G. Christensen ,  James V. Heck ,  Michael J. Szymonifka

IPC分类号： C07D477/00 ,  A61K31/40 ,  C07D487/14

CPC分类号： C07D477/00

摘要： Disclosed are 6-(1-hydroxyethyl)cyclonocardicins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics. ##STR1## Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.

摘要翻译： 公开了可用作抗生素的6-（1-羟基乙基）环心内酯（I）及其药学上可接受的盐和酯。 （I）还公开了制备这些化合物的方法; 包含这些化合物的药物组合物; 和治疗方法，包括当指出抗生素效应时施用这些化合物和组合物。

公开(公告)号：US08138219B2

公开(公告)日：2012-03-20

申请号：US12739984

申请日：2008-11-25

申请人： Alexander Pasternak ,  Michael J. Szymonifka

发明人： Alexander Pasternak ,  Michael J. Szymonifka

IPC分类号： A61K31/404 ,  C07D209/14

CPC分类号： C07D209/16

摘要： Novel compounds of the structural formula (I) are antagonists of the 5-HT6 receptor and are useful in the treatment, prevention and suppression of diseases mediated by the 5-HT6 receptor. The compounds of the present invention are useful in the treatment of obesity, diabetes, metabolic disorder, cognitive disorders, age related cognitive disorder, depression, mania, bipolar disorders, schizophrenia, anxiety, generalized anxiety disorder, panic disorder, and obsessive compulsive disorder, epilepsy, convulsions, migraine, substance withdrawal from substances including but not limited to opiates, nicotine, tobacco products, alcohol, benzodiazepines, sedatives, and the like, sleep disorders, attention deficit/hyperactivity disorder, and Alzheimer's disease.

摘要翻译： 结构式（I）的新型化合物是5-HT 6受体的拮抗剂，可用于治疗，预防和抑制由5-HT 6受体介导的疾病。 本发明的化合物可用于治疗肥胖，糖尿病，代谢紊乱，认知障碍，与年龄相关的认知障碍，抑郁症，躁狂症，双相情感障碍，精神分裂症，焦虑症，广泛性焦虑症，恐慌症和强迫症， 癫痫症，惊厥，偏头痛，物质从物质包括但不限于阿片剂，尼古丁，烟草产品，酒精，苯二氮卓类，镇静剂等，物质戒断，睡眠障碍，注意力缺陷/多动症和阿尔茨海默病。

公开(公告)号：US20100256106A1

公开(公告)日：2010-10-07

申请号：US12739984

申请日：2008-11-25

申请人： Alexander Pasternak ,  Michael J. Szymonifka

发明人： Alexander Pasternak ,  Michael J. Szymonifka

IPC分类号： A61K31/397 ,  C07D209/14 ,  A61K31/4045 ,  A61K31/44 ,  A61K31/4985 ,  A61P3/04

CPC分类号： C07D209/16

摘要： Novel compounds of the structural formula (I) are antagonists of the 5-HT6 receptor and are useful in the treatment, prevention and suppression of diseases mediated by the 5-HT6 receptor. The compounds of the present invention are useful in the treatment of obesity, diabetes, metabolic disorder, cognitive disorders, age related cognitive disorder, depression, mania, bipolar disorders, schizophrenia, anxiety, generalized anxiety disorder, panic disorder, and obsessive compulsive disorder, epilepsy, convulsions, migraine, substance withdrawal from substances including but not limited to opiates, nicotine, tobacco products, alcohol, benzodiazepines, sedatives, and the like, sleep disorders, attention deficit/hyperactivity disorder, and Alzheimer's disease.

摘要翻译： 结构式（I）的新化合物是5-HT 6受体的拮抗剂，可用于治疗，预防和抑制由5-HT 6受体介导的疾病。 本发明的化合物可用于治疗肥胖，糖尿病，代谢紊乱，认知障碍，与年龄相关的认知障碍，抑郁症，躁狂症，双相情感障碍，精神分裂症，焦虑症，广泛性焦虑症，恐慌症和强迫症， 癫痫症，惊厥，偏头痛，物质从物质包括但不限于阿片剂，尼古丁，烟草产品，酒精，苯二氮卓类，镇静剂等，物质戒断，睡眠障碍，注意力缺陷/多动症和阿尔茨海默病。

公开(公告)号：US20090258862A1

公开(公告)日：2009-10-15

申请号：US11991188

申请日：2006-08-25

申请人： Steven L. Colletti ,  Hong Shen ,  James R. Tata ,  Michael J. Szymonifka

发明人： Steven L. Colletti ,  Hong Shen ,  James R. Tata ,  Michael J. Szymonifka

IPC分类号： A61K31/55 ,  C07D403/04 ,  C07D487/08 ,  C07D401/04 ,  A61K31/495

CPC分类号： C07D403/04 ,  C07D207/09 ,  C07D211/40 ,  C07D241/04 ,  C07D413/04 ,  C07D491/10

摘要： Compounds of the formula (I): as well as pharmaceutically acceptable salts and solvates are disclosed. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels. Pharmaceutical compositions and methods of treatment are also included.

摘要翻译： 公开了式（I）的化合物以及药学上可接受的盐和溶剂合物。 该化合物可用于治疗血脂异常，特别是降低血清LDL，VLDL和甘油三酸酯，并提高HDL水平。 还包括药物组合物和治疗方法。