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1. 发明授权

US07109245B2 Vasoconstrictor cannabinoid analogs 有权
标题翻译：血管收缩大麻素类似物
公开(公告)号：US07109245B2
公开(公告)日：2006-09-19
申请号：US10486810
申请日：2002-08-14
申请人： George Kunos , Raj K. Razdan
发明人： George Kunos , Raj K. Razdan
IPC分类号： A61K31/075 , C07C43/205
CPC分类号： C07C43/215 , A61K31/047 , A61K31/09 , C07C43/225 , C07C2601/16
摘要： Methods and compounds for reversing pathological vasodilation of blood vessels, for example vasodilation caused by activation of CB1-like receptors, by administering to a subject a therapeutically effective amount of a compound sufficient to induce vasoconstriction, the compound comprising: wherein dashed lines independently represent either a single or a double bond, R1 is a lower alkyl, R2 is a lower alkyl, R3 is a lower alkyl or halogen, R4 is a lower alkyl or hydrogen, R5 is a lower alkyl or hydrogen, R6 is a hydrogen, lower alkyl or halogen, and R7 is a hydrogen, lower alkyl or halogen. The vasoconstrictor can be used for a variety of purposes, including hemostasis or the treatment of shock, for example vasodilatory shock syndromes such as septic shock.
摘要翻译：用于逆转血管病理性血管舒张的方法和化合物，例如通过活化CB1样受体引起的血管舒张，通过向受试者施用治疗有效量的足以引起血管收缩的化合物，所述化合物包括：其中虚线独立地表示单键或双键，R 1是低级烷基，R 2是低级烷基，R 3是低级烷基或卤素 R 4是低级烷基或氢，R 5是低级烷基或氢，R 6是氢，低级烷基或卤素 R 7是氢，低级烷基或卤素。血管收缩剂可用于各种目的，包括止血或治疗休克，例如血管舒张性休克综合征，如脓毒性休克。

2. 发明授权

US06563009B1 Vasodilator cannabinoid analogs 失效
标题翻译：血管扩张剂大麻素类似物
公开(公告)号：US06563009B1
公开(公告)日：2003-05-13
申请号：US10009813
申请日：2002-03-08
申请人： George Kunos , Billy Martin , Raj Razdan
发明人： George Kunos , Billy Martin , Raj Razdan
IPC分类号： C07C3917
CPC分类号： C07C39/23 , A61K31/05 , A61K31/055 , C07C39/42 , C07C2601/16
摘要： Cannabinoids have been found to have antioxidant properties, unrelated to NMDA receptor antagonism. This new found property makes the cannabinoids useful in the treatment and prophylaxis of wide variety of oxidation associated diseases, such as ischemic, age-related, inflammatory and autoimmune diseases. The cannabinoids are found to have particular application as neuroprotuctants, for example in limiting neurological damage following ischemic insults, such as stroke and trauma, or in the treatment of neurodegenerative diseases, such as Alzheimer's disease, Parkinson's disease and HIV dementia. Nonpsychoactive cannabinoids, such as cannabidoil, are particularly advantageous to use because they avoid toxicity that is encountered with psychoactive cannabinoids at high doses useful in the method of the present invention. A particular disclosed class of cannabinoids useful as neuroprotective antioxidants is formula (I) wherein the R group is independently selected from the group consisting of H, CH3, and COCH3
摘要翻译：已经发现大麻素具有与NMDA受体拮抗作用无关的抗氧化性质。这种新发现的属性使得大麻素可用于治疗和预防各种氧化相关疾病，例如缺血性，年龄相关性，炎性和自身免疫性疾病。发现大麻素具有作为神经保护剂的特殊应用，例如限制缺血性损伤（例如中风和创伤）或治疗神经变性疾病如阿尔茨海默病，帕金森病和HIV痴呆中的神经损伤。非精神活性大麻素，如大麻素，特别有利于使用，因为它们避免了在本发明方法中有用的高剂量的精神活性大麻素遇到的毒性。可用作神经保护性抗氧化剂的特定公开类型的大麻素是式（I），其中R基团独立地选自H，CH 3和COCH 3

3. 发明申请

US20130041037A1 THERAPEUTIC APPLICATIONS OF FATTY ACID AMIDE HYDROLASE INHIBITORS 审中-公开
标题翻译：脂肪酸酰胺水解酶抑制剂的治疗应用
公开(公告)号：US20130041037A1
公开(公告)日：2013-02-14
申请号：US13652324
申请日：2012-10-15
申请人： George Kunos , Alexandros Makriyannis
发明人： George Kunos , Alexandros Makriyannis
IPC分类号： A61K31/185 , A61P25/22
CPC分类号： C07C309/82
摘要： Fatty acid amide hydrolase (FAAH) is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors). Disclosed herein are potent inhibitors of FAAH and methods for their use for treating a variety of disorder, including hypertension and cardiac hypertrophy.
摘要翻译：脂肪酸酰胺水解酶（FAAH）是负责降解油酰胺（内源性睡眠诱导性脂质）和anandamide（大麻素受体的内源性配体）的酶。本文公开了FAAH的有效抑制剂及其用于治疗多种障碍（包括高血压和心脏肥大）的方法。

4. 发明授权

US08293724B2 Therapeutic applications of fatty acid amide hydrolase inhibitors 失效
标题翻译：脂肪酸酰胺水解酶抑制剂的治疗应用
公开(公告)号：US08293724B2
公开(公告)日：2012-10-23
申请号：US12755227
申请日：2010-04-06
申请人： George Kunos , Alexandros Makriyannis
发明人： George Kunos , Alexandros Makriyannis
IPC分类号： A61K31/69 , A61K31/10 , A61K317/06 , C07F5/02 , C07F9/02
CPC分类号： C07C309/82
摘要： Fatty acid amide hydrolase (FAAH) is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors). Disclosed herein are potent inhibitors of FAAH and methods for their use for treating a variety of disorder, including hypertension and cardiac hypertrophy.
摘要翻译：脂肪酸酰胺水解酶（FAAH）是负责降解油酰胺（内源性睡眠诱导性脂质）和anandamide（大麻素受体的内源性配体）的酶。本文公开了FAAH的有效抑制剂及其用于治疗多种障碍（包括高血压和心脏肥大）的方法。

5. 发明申请

US20100261674A1 THERAPEUTIC APPLICATIONS OF FATTY ACID AMIDE HYDROLASE INHIBITORS 失效
标题翻译：脂肪酸酰胺水解酶抑制剂的治疗应用
公开(公告)号：US20100261674A1
公开(公告)日：2010-10-14
申请号：US12755227
申请日：2010-04-06
申请人： George Kunos , Alexandros Makriyannis
发明人： George Kunos , Alexandros Makriyannis
IPC分类号： A61K31/69 , C07C317/06 , A61K31/10 , C07F9/02 , A61K31/66 , C07C49/167 , A61K31/12 , C07F5/02 , C07F5/04 , A61P9/12 , A61P25/24 , A61P25/22
CPC分类号： C07C309/82
摘要： Fatty acid amide hydrolase (FAAH) is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors). Disclosed herein are potent inhibitors of FAAH and methods for their use for treating a variety of disorder, including hypertension and cardiac hypertrophy.
摘要翻译：脂肪酸酰胺水解酶（FAAH）是负责降解油酰胺（内源性睡眠诱导性脂质）和anandamide（大麻素受体的内源性配体）的酶。本文公开了FAAH的有效抑制剂及其用于治疗多种障碍（包括高血压和心脏肥大）的方法。

6. 发明授权

US5939429A Cardiovascular uses of cannabinoid compounds 失效
标题翻译：大麻素化合物的心血管用途
公开(公告)号：US5939429A
公开(公告)日：1999-08-17
申请号：US161751
申请日：1998-09-29
申请人： George Kunos , Karoly Varga , Jens Wagner , Earl F. Ellis , Aron Sanyal
发明人： George Kunos , Karoly Varga , Jens Wagner , Earl F. Ellis , Aron Sanyal
IPC分类号： A61K31/00 , A61K31/05 , A61K31/352 , A61K31/454 , A61K31/44 , A61K31/38 , A61K31/40 , A61K31/405 , A61K31/535
CPC分类号： A61K31/454 , A61K31/00 , A61K31/05 , A61K31/352
摘要： Hemorrhagic shock and in other conditions associated with excessive vasoconstriction, such as hypertension, peripheral vascular disease, cirrhosis of the liver, or certain forms of angina pectoris can be treated by using agonists of CB1 receptors as well as other cannabinoid receptors. In addition, it has been determined that in septic shock and cirrhosis of the liver when hypotension is due to activation of macrophages by bacterial endotoxin, the use of a drug that selectively blocks CB1 receptors or other cannabinoid receptors may be of therapeutic value by preventing or attenuating the endotoxin-induced hypotension.
摘要翻译：出血性休克和与过度血管收缩相关的其他病症如高血压，外周血管疾病，肝硬化或某些形式的心绞痛可以通过使用CB1受体的激动剂以及其他大麻素受体来治疗。此外，已经确定，当低血压是由细菌内毒素激活巨噬细胞时，在脓毒性休克和肝硬化中，选择性阻断CB1受体或其他大麻素受体的药物的使用可以通过预防或减轻内毒素引起的低血压。

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