公开(公告)号：US07589068B2

公开(公告)日：2009-09-15

申请号：US11795156

申请日：2006-02-10

申请人： Nicholas D. P. Cosford ,  Mark E. Layton ,  Jun Liang ,  Craig W. Lindsley ,  Philip E. Sanderson ,  Zhijian Zhao

发明人： Nicholas D. P. Cosford ,  Mark E. Layton ,  Jun Liang ,  Craig W. Lindsley ,  Philip E. Sanderson ,  Zhijian Zhao

IPC分类号： A01N43/04 ,  A01N43/58 ,  A01N43/42 ,  A61K31/70 ,  A61K31/50 ,  A61K31/495 ,  A61K31/52 ,  A61K31/47 ,  C07D487/00 ,  C07D491/00 ,  C07H15/00 ,  C07H17/00 ,  C07H17/02 ,  C09B25/00

CPC分类号： C07D471/04

摘要： The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

摘要翻译： 本发明提供抑制Akt活性的化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。

公开(公告)号：US07544677B2

公开(公告)日：2009-06-09

申请号：US11659606

申请日：2005-08-19

申请人： Mark T. Bilodeau ,  Nicholas D. P. Cosford ,  John C. Hartnett ,  Yiwei Li ,  Jun Liang ,  Peter J. Manley ,  Lou Anne Neilson ,  Tony Siu ,  Zhicai Wu

发明人： Mark T. Bilodeau ,  Nicholas D. P. Cosford ,  John C. Hartnett ,  Yiwei Li ,  Jun Liang ,  Peter J. Manley ,  Lou Anne Neilson ,  Tony Siu ,  Zhicai Wu

IPC分类号： A61K31/541 ,  A61K31/5355 ,  A61K31/519 ,  C07D471/04 ,  C07D519/00 ,  A61P35/00

CPC分类号： C07D471/04

摘要： The present invention is directed to compounds which contain substituted 5-deazapteridine moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

摘要翻译： 本发明涉及含有抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代的5-取代哌啶部分的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。

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。