公开(公告)号：US07776894B2

公开(公告)日：2010-08-17

申请号：US12192753

申请日：2008-08-15

申请人： Ze'ev A. Ronai ,  Anindita Bhoumik ,  Nicholas D. P. Cosford ,  Russell Dahl

发明人： Ze'ev A. Ronai ,  Anindita Bhoumik ,  Nicholas D. P. Cosford ,  Russell Dahl

IPC分类号： A61K31/40 ,  A61K31/4406 ,  A61K31/215 ,  A61K31/165 ,  A61K31/16

CPC分类号： C07C235/82 ,  C07C2603/52 ,  C07J63/008

摘要： There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.

摘要翻译： 提供抑制黑素瘤生长和转移的方法，使黑素瘤细胞对凋亡敏感的方法，以及使用乙酰基异烟酸，celastrol或其衍生物治疗患有黑素瘤的受试者的方法。 还提供了celastrol的衍生物和包含乙酰基异烟酸，celastrol或其衍生物的组合物。

公开(公告)号：US07253190B2

公开(公告)日：2007-08-07

申请号：US10491613

申请日：2002-10-01

申请人： Nicholas D. P. Cosford ,  Chixu Chen ,  Thomas S. Reger ,  Jeffrey R. Roppe ,  Nicholas D. Smith

发明人： Nicholas D. P. Cosford ,  Chixu Chen ,  Thomas S. Reger ,  Jeffrey R. Roppe ,  Nicholas D. Smith

IPC分类号： A61K31/4439 ,  C07D401/04

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

摘要： Tetrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

摘要翻译： 直接或桥接的杂唑基化合物与杂芳基连接点相邻的杂芳基部分是mGluR5调节剂，可用于治疗精神病和情绪障碍，例如精神分裂症，焦虑症，抑郁症， 和恐慌，以及治疗疼痛等疾病。

公开(公告)号：US06956049B1

公开(公告)日：2005-10-18

申请号：US09387135

申请日：1999-08-31

申请人： Nicholas D. P. Cosford ,  Ian A. McDonald ,  Stephen D. Hess ,  Mark A. Varney

发明人： Nicholas D. P. Cosford ,  Ian A. McDonald ,  Stephen D. Hess ,  Mark A. Varney

IPC分类号： A61K31/425 ,  C07D277/00 ,  A51K31/425

CPC分类号： C07D277/22 ,  A61K31/425

摘要： In accordance with the present invention, there are provided methods of modulating the activity of excitatory amino acid receptors using a specifically defined class of heterocyclic compounds. In one embodiment, there are provided methods of modulating metabotropic glutamate receptors. The present invention also discloses methods of treating disease using heterocyclic compounds. Diseases contemplated include cerebral ischemia, chronic neurodegeneration, psychiatric disorders, schizophrenia, mood disorders, emotion disorders, disorders of extrapyramidal motor function, obesity, disorders of respiration, motor control and function, attention deficit disorders, concentration disorders, pain disorders, neurodegenerative disorders, epilepsy, convulsive disorders, eating disorders, sleep disorders, sexual disorders, circadian disorders, drug withdrawal, drug addiction, compulsive disorders, anxiety, panic disorders, depressive disorders, skin disorders, retinal ischemia, retinal degeneration, glaucoma, disorders associated with organ transplantation, asthma, ischemia and astrocytomas. The invention further discloses methods of preventing disease conditions related to diseases of the pulmonary system, diseases of the nervous system, diseases of the cardiovascular system, diseases of the gastrointestinal system, diseases of the endocrine system, diseases of the exocrine system, diseases of the skin, cancer and diseases of the ophthalmic system. The invention also discloses pharmaceutically acceptable salt forms of heterocyclic compounds.

摘要翻译： 根据本发明，提供了使用特定限定类杂环化合物调节兴奋性氨基酸受体活性的方法。 在一个实施方案中，提供了调节代谢型谷氨酸受体的方法。 本发明还公开了使用杂环化合物治疗疾病的方法。 预期的疾病包括脑缺血，慢性神经变性，精神疾病，精神分裂症，情绪障碍，情绪障碍，锥体外系运动功能障碍，肥胖症，呼吸障碍，运动控制和功能，注意力缺陷障碍，集中症，疼痛障碍，神经变性疾病， 癫痫症，惊厥性疾病，进食障碍，睡眠障碍，性障碍，昼夜节律障碍，药物戒断，药物成瘾，强迫症，焦虑症，恐慌症，抑郁症，皮肤病症，视网膜缺血，视网膜变性，青光眼，器官移植相关疾病 ，哮喘，局部缺血和星形细胞瘤。 本发明还公开了预防与肺系统疾病，神经系统疾病，心血管系统疾病，胃肠系统疾病，内分泌系统疾病，外分泌系统疾病， 皮肤，癌症和眼科疾病。 本发明还公开了药学上可接受的杂环化合物的盐形式。