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1. 发明授权

US06627734B1 Identification and characterization of multiple splice variants of the Kappa3-related opioid receptor (KOR-3) gene 有权
标题翻译： Kappa3相关阿片受体（KOR-3）基因的多个剪接变体的鉴定和表征
公开(公告)号：US06627734B1
公开(公告)日：2003-09-30
申请号：US09743871
申请日：2001-03-13
申请人： Gavril Pasternak , Ying-Xian Pan
发明人： Gavril Pasternak , Ying-Xian Pan
IPC分类号： C07K100
CPC分类号： C07K14/705 , A01K2217/05 , G01N33/9486 , G01N2500/00
摘要： The present invention encompasses novel splice variant forms of the muopioid receptor-1 (KOR-3) and the polynucleotide sequences encoding the KOR-3 splice variants. The invention further encompasses methods of screening for compositions regulating the KOR-3 splice variant activities and the development of therapeutic modalities directed to regulating activity. Regulation of the KOR-3 splice variant activities may impact the physiologic processes of analgesia and weight management.
摘要翻译：本发明涵盖了muopioid受体-1（KOR-3）的新型剪接变体形式和编码KOR-3剪接变体的多核苷酸序列。本发明还包括筛选调节KOR-3剪接变体活性的组合物的方法，以及针对调节活性的治疗方式的开发。 KOR-3剪接变体活性的调节可能会影响镇痛和体重管理的生理过程。

2. 发明申请

US20200345715A1 Ligands of the Mu, Kappa, and Delta Opioid Receptors 审中-公开
公开(公告)号：US20200345715A1
公开(公告)日：2020-11-05
申请号：US16763522
申请日：2018-11-14
申请人： Evan N. FEINBERG , Vijay S. PANDE , Susruta MAJUMDAR , Gavril PASTERNAK , The Board of Trustees of the Leland Stanford Junior University , Memorial Sloan-Kettering Cancer Center
发明人： Evan N. Feinberg , Vijay S. Pande , Susruta Majumdar , Gavril Pasternak
IPC分类号： A61K31/4453 , A61K31/415
摘要： Ligands of the mu, kappa, and delta opioid receptors and methods of using them are disclosed. In particular, the invention relates to the discovery of new opioid receptor ligands based on molecular dynamics simulations of conformational states of the μ opioid receptor and the use of the identified opioid receptor ligands as analgesics, anti-diarrheal agents, and overdose reversal agents.

3. 发明申请

US20140255308A1 6-AMIDO DERIVATIVES OF 4, 5-a EPOXYMORPHINANS FOR THE TREATMENT OF PAIN 有权
标题翻译：用于治疗疼痛的4,5-a环氧维生素的6-AMIDO衍生物
公开(公告)号：US20140255308A1
公开(公告)日：2014-09-11
申请号：US14281237
申请日：2014-05-19
申请人： Gavril Pasternak , Susruta Majumdar
发明人： Gavril Pasternak , Susruta Majumdar
IPC分类号： C07D489/08 , G01N33/94 , A61K51/04
CPC分类号： C07D489/08 , A61K51/0455 , G01N33/9486
摘要： Compounds of formula: in which R4 is chosen from substituted phenyl, optionally substituted naphthylene, optionally substituted anthracene and optionally substituted aromatic heterocycle, are useful as analgesics.
摘要翻译：下式的化合物：其中R 4选自取代的苯基，任选取代的亚乙基，任选取代的蒽和任选取代的芳族杂环，可用作止痛剂。

4. 发明申请

US20130289060A1 6-AMIDO DERIVATIVES OF 4, 5-a EPOXYMORPHINANS FOR THE TREATMENT OF PAIN 审中-公开
标题翻译：用于治疗疼痛的4,5-a环氧维生素的6-AMIDO衍生物
公开(公告)号：US20130289060A1
公开(公告)日：2013-10-31
申请号：US13879908
申请日：2011-10-19
申请人： Gavril Pasternak , Susruta Majumdar
发明人： Gavril Pasternak , Susruta Majumdar
IPC分类号： C07D489/08
CPC分类号： C07D489/08 , A61K51/0455 , G01N33/9486
摘要： Compounds of formula: in which R4 is chosen from substituted phenyl, optionally substituted naphthylene, optionally substituted anthracene and optionally substituted aromatic heterocycle, are useful as analgesics.
摘要翻译：下式的化合物：其中R 4选自取代的苯基，任选取代的亚乙基，任选取代的蒽和任选取代的芳族杂环，可用作止痛剂。

5. 发明授权

US06790855B2 Topical anesthetic/opioid formulations and uses thereof 有权
公开(公告)号：US06790855B2
公开(公告)日：2004-09-14
申请号：US09975812
申请日：2001-10-11
申请人： Gavril Pasternak , Yuri Kolesnikov
发明人： Gavril Pasternak , Yuri Kolesnikov
IPC分类号： A61K3144
CPC分类号： A61K9/0014 , A61K31/4745 , A61K31/485 , A61K31/675 , A61K38/33 , A61K45/06 , A61K47/20 , A61K47/38 , Y10S514/817 , A61K31/165 , A61K2300/00
摘要： Many chemical and pharmaceutical compositions are known to produce antinociceptive effects that are helpful in relieving pain and inflammation. Both opioids and local anesthetics serve an important function in providing peripheral pain relief. Topical administration of pain-relieving drugs to the periphery offers important advantages over systemic or local, non-topical administration. The present invention provides topical pharmaceutical compositions, formulated with at least one local anesthetic and at least one opioid analgesic in a topical excipient. The present invention also provides methods for relieving pain in a subject through topical administration of the pharmaceutical composition in an amount and a duration sufficient to synergistically potentiate an antinociceptive response. Synergistic potentiation of analgesia through topical administration of a local anesthetic/opioid pharmaceutical composition provides a new and improved approach to peripheral pain management.

6. 发明授权

US07820688B2 Topical anesthetic/opioid formulations and uses thereof 有权
标题翻译：局部麻醉/阿片类药物及其用途
公开(公告)号：US07820688B2
公开(公告)日：2010-10-26
申请号：US10823365
申请日：2004-04-13
申请人： Gavril Pasternak , Yuri Kolesnikov
发明人： Gavril Pasternak , Yuri Kolesnikov
IPC分类号： A01N43/42 , A01N33/02 , A61K31/44 , A61K31/135 , A61K31/16
CPC分类号： A61K31/485 , A61K31/4745 , A61K31/675 , A61K38/33 , Y10S514/817 , A61K2300/00
摘要： Many chemical and pharmaceutical compositions are known to produce antinociceptive effects that are helpful in relieving pain and inflammation. Both opioids and local anesthetics serve an important function in providing peripheral pain relief. Topical administration of pain-relieving drugs to the periphery offers important advantages over systemic or local, non-topical administration. The present invention provides topical pharmaceutical compositions, formulated with at least one local anesthetic and at least one opioid analgesic in a topical excipient. The present invention also provides methods for relieving pain in a subject through topical administration of the pharmaceutical composition in an amount and a duration sufficient to synergistically potentiate an antinociceptive response. Synergistic potentiation of analgesia through topical administration of a local anesthetic/opioid pharmaceutical composition provides a new and improved approach to peripheral pain management.
摘要翻译：已知许多化学和药物组合物产生有助于缓解疼痛和炎症的抗伤害感受作用。阿片类药物和局部麻醉剂都是提供周边疼痛缓解的重要功能。局部给予止痛药物到外围，与全身或局部，非局部给药相比，具有重要的优势。本发明提供在局部赋形剂中与至少一种局部麻醉剂和至少一种阿片样镇痛剂配制的局部药物组合物。本发明还提供了通过局部施用药物组合物以足以协同增强抗伤害感受反应的量和持续时间来缓解受试者的疼痛的方法。通过局部施用局部麻醉剂/阿片类药物组合物来协同镇痛镇痛提供了一种新的改进的外周疼痛治疗方法。

7. 发明申请

US20070258988A1 Identification and Characterization of Multiple Splice Variants of the Mu Opioid Receptor Gene 失效
标题翻译： Mu Opioid受体基因的多个接头变体的鉴定和表征
公开(公告)号：US20070258988A1
公开(公告)日：2007-11-08
申请号：US10588679
申请日：2005-02-11
申请人： Gavril Pasternak , Ying-Xian Pan
发明人： Gavril Pasternak , Ying-Xian Pan
IPC分类号： A61K39/00 , A61K31/00 , A61P25/00 , C07K14/705 , G01N33/53 , C12Q1/02 , C07H21/04 , A61K31/711
CPC分类号： C07K14/705
摘要： The present invention encompasses novel splice variant forms of the mu-opioid receptor-1 (MOR-1) and the polynucleotide sequences encoding the MOR-1 splice variants. The invention further encompasses methods of screening for compositions regulating the MOR-1 splice variant activities and the development of therapeutic modalities directed to regulating activity. Regulation of the MOR-1 splice variant activities may impact the physiologic process of analgesia.
摘要翻译：本发明包括μ-阿片受体-1（MOR-1）的新型剪接变体形式和编码MOR-1剪接变体的多核苷酸序列。本发明还包括筛选调节MOR-1剪接变体活性的组合物的方法，以及开发针对调节活性的治疗方式。 MOR-1剪接变体活性的调节可能会影响镇痛的生理过程。

8. 发明授权

US06825203B2 Topical anesthetic/opioid formulations and uses thereof 有权
标题翻译：局部麻醉/阿片类药物及其用途
公开(公告)号：US06825203B2
公开(公告)日：2004-11-30
申请号：US09844111
申请日：2001-04-27
申请人： Gavril Pasternak , Yuri Kolesnikov
发明人： Gavril Pasternak , Yuri Kolesnikov
IPC分类号： A61K3144
CPC分类号： A61K9/0014 , A61K31/4745 , A61K31/485 , A61K31/675 , A61K38/33 , A61K45/06 , A61K47/20 , A61K47/38 , Y10S514/817 , A61K31/165 , A61K2300/00
摘要： Many chemical and pharmaceutical compositions are known to produce antinociceptive effects that are helpful in relieving pain and inflammation. Both opioids and local anesthetics serve an important function in providing peripheral pain relief. Topical administration of pain-relieving drugs to the periphery offers important advantages over systemic or local, non-topical administration. The present invention provides topical pharmaceutical compositions, formulated with at least one local anesthetic and at least one opioid analgesic in a topical excipient. The present invention also provides methods for relieving pain in a subject through topical administration of the pharmaceutical composition in an amount and a duration sufficient to synergistically potentiate an antinociceptive response. Synergistic potentiation of analgesia through topical administration of a local anesthetic/opioid pharmaceutical composition provides a new and improved approach to peripheral pain management.
摘要翻译：已知许多化学和药物组合物产生有助于缓解疼痛和炎症的抗伤害感受作用。阿片类药物和局部麻醉剂都是提供周边疼痛缓解的重要功能。局部给予止痛药物到外围，与全身或局部，非局部给药相比，具有重要的优势。本发明提供在局部赋形剂中与至少一种局部麻醉剂和至少一种阿片样镇痛剂配制的局部药物组合物。本发明还提供了通过局部施用药物组合物以足以协同增强抗伤害感受反应的量和持续时间来缓解受试者的疼痛的方法。通过局部施用局部麻醉剂/阿片类药物组合物来协同镇痛镇痛提供了一种新的改进的外周疼痛治疗方法。

9. 发明授权

US06500927B2 Identification and characterization of multiple splice variants of the mu-opioid receptor gene 失效
标题翻译：识别和表征mu-阿片受体基因的多个剪接变体
公开(公告)号：US06500927B2
公开(公告)日：2002-12-31
申请号：US09761962
申请日：2001-01-17
申请人： Gavril Pasternak , Ying-Xian Pan
发明人： Gavril Pasternak , Ying-Xian Pan
IPC分类号： C07K100
CPC分类号： C07K14/705 , A01K2217/05 , A61K38/00
摘要： The present invention encompasses novel splice variant forms of the mu-opioid receptor-1 (MOR-1) and the polynucleotide sequences encoding the MOR-1 splice variants. The invention further encompasses methods of screening for compositions regulating the MOR-1 splice variant activities and the development of therapeutic modalities directed to regulating activity. Regulation of the MOR-1 splice variant activities may impact the physiologic processes of analgesia and weight management.
摘要翻译：本发明包括μ-阿片受体-1（MOR-1）的新型剪接变体形式和编码MOR-1剪接变体的多核苷酸序列。本发明还包括筛选调节MOR-1剪接变体活性的组合物的方法，以及开发针对调节活性的治疗方式。 MOR-1剪接变体活性的调控可能会影响镇痛和体重管理的生理过程。

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