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    • 1. 发明申请
    • COMPOUNDS WHICH BIND TO THE ACTIVE SITE OF PROTEIN KINASE ENZYMES
    • 与蛋白激酶酶活性位点结合的化合物
    • WO2006072792A2
    • 2006-07-13
    • PCT/GB2006/000034
    • 2006-01-06
    • BIOFOCUS DISCOVERY LIMITEDBIRAULT, VeroniqueHARRIS, Clifford, JohnCROSSLEY, Roger
    • BIRAULT, VeroniqueHARRIS, Clifford, JohnCROSSLEY, Roger
    • A61K31/44A61K31/4418A61K31/4433A61K31/4965A61K31/497A61P25/00A61P25/16A61P25/28A61P27/02A61P29/00
    • A61K31/44A61K31/4418A61K31/4433A61K31/4965A61K31/497
    • One or more compounds that are inhibitors of a serine/ threonine kinase, more particularly Rho kinase (ROK, ROCK) can be used in the manufacture of a medicament for treatment or prophylaxis of a condition selected from: an ocular condition including age related macular degeneration, lacrimal gland disease or diabetic retinopathy, or suppression of neurite growth and hence a condition requiring nerve cell extension and connectivity, neuronal regeneration, inducing new axonal growth and promotion of axonal (re)wiring, repairing damage to neurons in the CNS caused by trauma (eg stroke, traumatic brain injury etc.) or neurodegeneration (eg Alzheimer's, Parkinson's etc), repair and recovery from and treatment of disorders such as spinal cord injury and in reducing the subsequent effects thereof, or pain caused by nerve cell damage such as following trauma or amputation for example in the treatment of neuropathic pain. The compounds are selected from the specific group of compounds that comprises or consists of compounds of formula (I) or (II) wherein R1, R2, R3, R4, R5 and R6 are defined herein.
    • 作为丝氨酸/苏氨酸激酶抑制剂,尤其是Rho激酶(ROK,ROCK)的一种或多种化合物可用于制备用于治疗或预防选自以下的病症的药物:包括年龄相关性黄斑变性 ,泪腺疾病或糖尿病性视网膜病变或抑制神经突生长,因此需要神经细胞延伸和连接,神经元再生,诱导新的轴突生长和促进轴突(重新)接线,修复由创伤引起的CNS中的神经元损伤的病症 (例如中风,创伤性脑损伤等)或神经变性(例如阿尔茨海默氏症,帕金森病等),修复和恢复并治疗诸如脊髓损伤和减轻其后续作用的疾病或由神经细胞损伤引起的疼痛,例如 在创伤或截肢后,例如治疗神经性疼痛。 化合物选自包含式I或II的化合物或其组成的特定组的化合物,其中R 1,R 2,R 3,R 4,R 5和R 6在本文中定义。
    • 7. 发明申请
    • COMPOUNDS WHICH BIND TO THE ACTIVE SITE OF PROTEIN KINASE ENZYMES
    • 与蛋白激酶酶活性位点结合的化合物
    • WO2006072792A3
    • 2007-01-11
    • PCT/GB2006000034
    • 2006-01-06
    • GALAPAGOS NVBIRAULT VERONIQUEHARRIS CLIFFORD JOHNCROSSLEY ROGER
    • BIRAULT VERONIQUEHARRIS CLIFFORD JOHNCROSSLEY ROGER
    • A61K31/44A61K31/4418A61K31/4433A61K31/4965A61K31/497A61P25/00A61P25/16A61P25/28A61P27/02A61P29/00
    • A61K31/44A61K31/4418A61K31/4433A61K31/4965A61K31/497
    • One or more compounds that are inhibitors of a serine/ threonine kinase, more particularly Rho kinase (ROK, ROCK) can be used in the manufacture of a medicament for treatment or prophylaxis of a condition selected from: an ocular condition including age related macular degeneration, lacrimal gland disease or diabetic retinopathy, or suppression of neurite growth and hence a condition requiring nerve cell extension and connectivity, neuronal regeneration, inducing new axonal growth and promotion of axonal (re)wiring, repairing damage to neurons in the CNS caused by trauma (eg stroke, traumatic brain injury etc.) or neurodegeneration (eg Alzheimer's, Parkinson's etc), repair and recovery from and treatment of disorders such as spinal cord injury and in reducing the subsequent effects thereof, or pain caused by nerve cell damage such as following trauma or amputation for example in the treatment of neuropathic pain. The compounds are selected from the specific group of compounds that comprises or consists of compounds of formula (I) or (II) wherein R1, R2, R3, R4, R5 and R6 are defined herein.
    • 作为丝氨酸/苏氨酸激酶抑制剂,尤其是Rho激酶(ROK,ROCK)的一种或多种化合物可用于制备用于治疗或预防选自以下的病症的药物:包括年龄相关性黄斑变性 ,泪腺疾病或糖尿病性视网膜病变或抑制神经突生长,因此需要神经细胞延伸和连接,神经元再生,诱导新的轴突生长和促进轴突(重新)接线,修复由创伤引起的CNS中的神经元损伤的病症 (例如中风,创伤性脑损伤等)或神经变性(例如阿尔茨海默氏症,帕金森病等),修复和恢复并治疗诸如脊髓损伤和减轻其后续作用的疾病或由神经细胞损伤引起的疼痛,例如 在创伤或截肢后,例如治疗神经性疼痛。 化合物选自包含式I或II的化合物或其组成的特定组的化合物,其中R 1,R 2,R 3,R 4,R 5和R 6在本文中定义。