公开(公告)号：US20130079376A1

公开(公告)日：2013-03-28

申请号：US13543760

申请日：2012-07-06

Applicant: Bijan Almassian ,  Martin J. Sadowski ,  Xu Kevin Lin

Inventor： Bijan Almassian ,  Martin J. Sadowski ,  Xu Kevin Lin

IPC: C07D235/30 ,  C07D213/53 ,  C07D213/38

CPC classification number: C07D235/30 ,  C07D213/38 ,  C07D213/53

Abstract: Compounds are provided according to formula I: where R, R′, R3, R4, R5, and R6 are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, Alzheimer' s Disease, Down's syndrome, Parkinson's Disease, and others.

Abstract translation: 根据式I提供化合物：其中R，R'，R 3，R 4，R 5和R 6如本文所定义。 提供的化合物及其药物组合物可用于预防和治疗包括人在内的哺乳动物中的各种病症，包括非限制性实例，阿尔茨海默病，唐氏综合症，帕金森病等。

公开(公告)号：US20060194810A1

公开(公告)日：2006-08-31

申请号：US11282314

申请日：2005-11-18

Applicant: Bijan Almassian ,  Zhi-Gang Jiang ,  Michael Lebowitz ,  Weiying Pan ,  Hossein Ghanbari

Inventor： Bijan Almassian ,  Zhi-Gang Jiang ,  Michael Lebowitz ,  Weiying Pan ,  Hossein Ghanbari

IPC: A61K31/4965 ,  A61K31/44 ,  A61K31/426 ,  A61K31/4172

CPC classification number: A61K31/44 ,  A61K31/175 ,  A61K31/4172 ,  A61K31/426 ,  A61K31/4402 ,  A61K31/4965 ,  C07D213/53 ,  C07D213/73 ,  C07D233/64 ,  C07D241/12 ,  C07D277/28

Abstract: The present invention relates to methods of treating or preventing ischemia-related (i.e., neural cell hypoxia and/or hypoglycemic) conditions by administering to a patient in need thereof certain thiosemicarbazone compounds. More particularly, the present invention relates to methods of preventing or treating certain ischemia-related conditions, which may include Alzheimer's disease, Parkinson's disease, and ischemic states that are due to or result from such conditions as: coronary artery bypass graft surgery; global cerebral ischemia due to cardiac arrest; focal cerebral infarction; cerebral hemorrhage; hemorrhage infarction; hypertensive hemorrhage; hemorrhage due to rupture of intracranial vascular abnormalities; subarachnoid hemorrhage due to rupture of intracranial arterial aneurysms; hypertensive encephalopathy; carotid stenosis or occlusion leading to cerebral ischemia; cardiogenic thromboembolism; spinal stroke and spinal cord injury; diseases of cerebral blood vessels, e.g., atherosclerosis, vasculitis; macular degeneration; myocardial infarction; cardiac ischemia; and superaventicular tachyarrhytmia.

Abstract translation: 本发明涉及通过向有需要的患者施用某些缩氨基硫脲化合物来治疗或预防缺血相关（即，神经细胞缺氧和/或降血糖）病症的方法。 更具体地，本发明涉及预防或治疗某些局部缺血相关病症的方法，其可能包括由冠状动脉旁路移植手术引起的或由其导致的阿尔茨海默氏病，帕金森病和缺血状态; 心脏骤停引起的全球脑缺血; 局灶性脑梗死; 脑出血; 出血性梗死; 高血压性出血 出血由于颅内血管异常破裂; 蛛网膜下腔出血由于颅内动脉瘤破裂; 高血压性脑病 颈动脉狭窄或闭塞导致脑缺血; 心源性血栓栓塞 脊髓中风和脊髓损伤; 脑血管疾病，例如动脉粥样硬化，血管炎; 黄斑变性; 心肌梗死; 心脏缺血; 和超表型性快速性心律失常。

公开(公告)号：US5338867A

公开(公告)日：1994-08-16

申请号：US872282

申请日：1992-04-24

Applicant: William Choy ,  Jen Chen ,  Bijan Almassian

Inventor： William Choy ,  Jen Chen ,  Bijan Almassian

IPC: C07D493/04 ,  C07D307/77

CPC classification number: C07D493/04

Abstract: A method of preparing a 4'-0-demethy-4.beta.-NHR podophyllotoxin, where R is an aryl or dialkyl amino alkyl group, is disclosed. The method includes reacting H.sub.2 NR under basic conditions with a mixture of .alpha. and .beta. epimers of 4'-0-demethyl-4-bromo-podophyllotoxin, to form an epimeric mixture of the 4'-0-demethyl-4-NHR-podophyllotoxin compounds, removing acidic impurities which bind to silica gel in a dichloromethane solvent, and crystallizing 4'-0-demethyl-4.beta.-NHR-podophyllotoxin from its .alpha. epimer.

Abstract translation: 公开了一种制备其中R为芳基或二烷基氨基烷基的4'-O-脱甲基-4β-NHR鬼臼毒素的方法。 该方法包括使碱性条件下的H 2 N R与4'-O-去甲基-4-溴鬼臼毒素的α和β差向异构体的混合物反应，形成4'-O-去甲基-4-NHR-鬼臼毒素化合物的差向异构体混合物 去除在二氯甲烷溶剂中与硅胶结合的酸性杂质，并从其α差向异构体中结晶出4'-O-脱甲基-4β-NHR-鬼臼毒素。

公开(公告)号：US08658677B2

公开(公告)日：2014-02-25

申请号：US13543760

申请日：2012-07-06

Applicant: Bijan Almassian ,  Martin J. Sadowski ,  Xu Kevin Lin

Inventor： Bijan Almassian ,  Martin J. Sadowski ,  Xu Kevin Lin

IPC: A61K31/44

CPC classification number: C07D235/30 ,  C07D213/38 ,  C07D213/53

Abstract: Compounds are provided according to formula I: where R, R′, R3, R4, R5, and R6 are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, Alzheimer's Disease, Down's syndrome, Parkinson's Disease, and others.

Abstract translation: 根据式I提供化合物：其中R，R'，R 3，R 4，R 5和R 6如本文所定义。 提供的化合物及其药物组合物可用于预防和治疗包括人在内的哺乳动物中的多种病症，包括作为非限制性实例，阿尔茨海默病，唐氏综合征，帕金森病等。

公开(公告)号：US20090275587A1

公开(公告)日：2009-11-05

申请号：US12276456

申请日：2008-11-24

Applicant: Bijan Almassian ,  Hossein A. Ghanbari ,  Michael Lebowitz ,  Weiying Pan ,  Zhi-Gang Jiang

Inventor： Bijan Almassian ,  Hossein A. Ghanbari ,  Michael Lebowitz ,  Weiying Pan ,  Zhi-Gang Jiang

IPC: A61K31/44 ,  A61P25/00 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/40 ,  A61K31/4164 ,  A61K31/42

CPC classification number: A61K31/44 ,  A61K31/4166 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4965 ,  A61K31/505

Abstract: The present invention relates to methods of treating ischemia-related conditions by administering to a patient in need of such methods certain thiosemicarbazone compounds. Preferred embodiments of the present invention relates to methods of treating specific ischemia-related conditions, including but not limited to Alzheimer's disease, Parkinson's disease, Coronary artery bypass graft surgery, Global cerebral ischemia due to cardiac arrest, focal cerebral infarction, cerebral hemorrhage, hemorrhage infarction, hypertensive hemorrhage. hemorrhage due to rupture of intracranial vascular abnormalities, subarachnoid hemorrhage due to rupture of intracranial arterial aneurysms, hypertensive encephalopathy, carotid stenosis or occlusion leading to cerebral ischemia, cardiogenic thromboembolism, spinal stroke and spinal cord injury, diseases of cerebral blood vessels: e.g., atherosclerosis, vasculitis, Macular degeneration, myocardial infarction, cardiac ischemia and superaventicular tachyarrhytmia.

Abstract translation: 本发明涉及通过向需要这种方法的患者施用某些缩氨基硫脲化合物来治疗缺血相关病症的方法。 本发明的优选实施方案涉及治疗特定缺血相关病症的方法，包括但不限于阿尔茨海默氏病，帕金森病，冠状动脉旁路移植手术，由于心脏停搏引起的全球性脑缺血，局灶性脑梗死，脑出血，出血 梗死，高血压性出血。 由于颅内血管异常破裂引起的出血，颅内动脉瘤破裂引起的蛛网膜下腔出血，高血压性脑病，颈动脉狭窄或闭塞，导致脑缺血，心源性血栓栓塞，脊髓卒中和脊髓损伤，脑血管疾病：动脉粥样硬化 ，血管炎，黄斑变性，心肌梗死，心脏缺血和超表型性快速性心律失常。

公开(公告)号：US07456179B2

公开(公告)日：2008-11-25

申请号：US10835668

申请日：2004-04-30

Applicant: Bijan Almassian ,  Hossein A. Ghanbari ,  Michael Lebowitz ,  Weiying Pan ,  Zhi-Gang Jiang

Inventor： Bijan Almassian ,  Hossein A. Ghanbari ,  Michael Lebowitz ,  Weiying Pan ,  Zhi-Gang Jiang

IPC: A61K31/4965 ,  A61K31/44 ,  A61K31/426 ,  A61K31/4172

CPC classification number: A61K31/44 ,  A61K31/4166 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4965 ,  A61K31/505

Abstract: The present invention relates to methods of treating ischemia-related conditions by administering to a patient in need of such methods certain thiosemicarbazone compounds. Preferred embodiments of the present invention relates to methods of treating specific ischemia-related conditions, including but not limited to Alzheimer's disease, Parkinson's disease, Coronary artery bypass graft surgery, Global cerebral ischemia due to cardiac arrest, focal cerebral infarction, cerebral hemorrhage, hemorrhage infarction, hypertensive hemorrhage. hemorrhage due to rupture of intracranial vascular abnormalities, subarachnoid hemorrhage due to rupture of intracranial arterial aneurysms, hypertensive encephalopathy, carotid stenosis or occlusion leading to cerebral ischemia, cardiogenic thromboembolism, spinal stroke and spinal cord injury, diseases of cerebral blood vessels: e.g., atherosclerosis, vasculitis, Macular degeneration, myocardial infarction, cardiac ischemia and superaventicular tachyarrhytmia.

Abstract translation: 本发明涉及通过向需要这种方法的患者施用某些缩氨基硫脲化合物来治疗缺血相关病症的方法。 本发明的优选实施方案涉及治疗特定缺血相关病症的方法，包括但不限于阿尔茨海默氏病，帕金森病，冠状动脉旁路移植手术，由于心脏停搏引起的全球性脑缺血，局灶性脑梗死，脑出血，出血 梗死，高血压性出血。 由于颅内血管异常破裂引起的出血，颅内动脉瘤破裂引起的蛛网膜下腔出血，高血压性脑病，颈动脉狭窄或闭塞，导致脑缺血，心源性血栓栓塞，脊髓卒中和脊髓损伤，脑血管疾病：动脉粥样硬化 ，血管炎，黄斑变性，心肌梗死，心脏缺血和超表型性快速性心律失常。