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1. 发明授权

US07718705B1 Methods of using rapid-onset selective serotonin reuptake inhibitors for treating sexual dysfunction 有权
标题翻译：使用快速发作的选择性5-羟色胺再摄取抑制剂治疗性功能障碍的方法
公开(公告)号：US07718705B1
公开(公告)日：2010-05-18
申请号：US10049427
申请日：2000-08-22
申请人： Karl Bruce Thor
发明人： Karl Bruce Thor
IPC分类号： A01N33/02 , A61K31/135 , A61K31/13
CPC分类号： A61K31/138 , A61K31/135 , A61K45/06 , A61K31/557 , A61K31/505 , A61K2300/00
摘要： Methods for the prevention, treatment, or management of sexual dysfunction, such as premature ejaculation, by administering to a patient in need of therapy a therapeutically effective amount of a rapid-onset selective serotonin reuptake inhibitor on an as-needed basis shortly before sexual activity.
摘要翻译：预防，治疗或管理性功能障碍（例如早泄）的方法是通过在需要治疗的情况下，在需要治疗的基础上，在需要治疗的基础上，根据需要，向需要治疗的患者施用治疗有效量的快速发作的选择性5-羟色胺再摄取抑制剂。

2. 发明申请

US20130059837A1 BENZAZEPINE COMPOUND 有权
公开(公告)号：US20130059837A1
公开(公告)日：2013-03-07
申请号：US13613948
申请日：2012-09-13
申请人： Hiroyuki KOSHIO , Norio ASAI , Taisuke TAKAHASHI , Takafumi SHIMIZU , Yasuhito NAGAI , Keiko KAWABATA , Karl Bruce THOR
发明人： Hiroyuki KOSHIO , Norio ASAI , Taisuke TAKAHASHI , Takafumi SHIMIZU , Yasuhito NAGAI , Keiko KAWABATA , Karl Bruce THOR
IPC分类号： C07D471/04 , A61K31/55 , A61P13/00 , C07D498/04
CPC分类号： C07D498/04 , A61K31/55 , C07D471/04 , C07D487/04
摘要： Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. The present inventors have investigated compounds having a 5-HT2C receptor agonist activity and have found that the benzazepine compounds of the present invention have an excellent 5-HT2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.

3. 发明申请

US20110269744A1 Benzazepine Compound 审中-公开
标题翻译：苯扎西平化合物
公开(公告)号：US20110269744A1
公开(公告)日：2011-11-03
申请号：US13044080
申请日：2011-03-09
申请人： Hiroyuki KOSHIO , Norio ASAI , Taisuke TAKAHASHI , Takafumi SHIMIZU , Yasuhito NAGAI , Keiko KAWABATA , Karl Bruce THOR
发明人： Hiroyuki KOSHIO , Norio ASAI , Taisuke TAKAHASHI , Takafumi SHIMIZU , Yasuhito NAGAI , Keiko KAWABATA , Karl Bruce THOR
IPC分类号： A61K31/55 , C07D487/04 , A61P13/00 , C07D498/04
CPC分类号： C07D498/04 , A61K31/55 , C07D471/04 , C07D487/04
摘要： [Problem] Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.[Means for Solution] The present inventors have investigated compounds having a 5-HT2C receptor agonist activity, which is promising as an active ingredient of a pharmaceutical composition for treating or preventing incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like, and have found that the benzazepine compounds of the present invention have an excellent 5-HT2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.
摘要翻译： [问题]提供可用作治疗或预防5-HT 2C受体相关疾病，特别是尿失禁，尿失禁尿，尿失禁等尿失禁的药物的化合物，勃起功能障碍功能障碍综合征等，肥胖等。 [解决方案]本发明人研究了具有5-HT 2C受体激动剂活性的化合物，其有希望作为用于治疗或预防失禁的药物组合物的活性成分，例如压力性尿失禁，敦促性尿失禁，混合性尿失禁，性功能障碍如勃起功能障碍综合征等，肥胖等，并且发现本发明的苯并氮杂化合物具有优异的5-HT 2C受体激动剂活性，从而完成了本发明。也就是说，本发明的苯并氮杂化合物具有5-HT 2C受体激动剂活性，可用作治疗或预防5-HT 2C受体相关疾病的药剂，特别是尿失禁，压力性尿失禁，压力性尿失禁，混合型尿失禁等，性功能障碍如勃起功能障碍综合征等，肥胖等。

4. 发明授权

US09108977B2 Benzazepine compound 有权
标题翻译：苯扎西平化合物
公开(公告)号：US09108977B2
公开(公告)日：2015-08-18
申请号：US13613948
申请日：2012-09-13
申请人： Hiroyuki Koshio , Norio Asai , Taisuke Takahashi , Takafumi Shimizu , Yasuhito Nagai , Keiko Kawabata , Karl Bruce Thor
发明人： Hiroyuki Koshio , Norio Asai , Taisuke Takahashi , Takafumi Shimizu , Yasuhito Nagai , Keiko Kawabata , Karl Bruce Thor
IPC分类号： A61K31/55 , C07D471/04 , C07D498/04 , C07D487/04
CPC分类号： C07D498/04 , A61K31/55 , C07D471/04 , C07D487/04
摘要： Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. The present inventors have investigated compounds having a 5-HT2C receptor agonist activity and have found that the benzazepine compounds of the present invention have an excellent 5-HT2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.
摘要翻译：本发明提供可用作治疗或预防5-HT 2C受体相关疾病，特别是尿失禁，尿失禁尿，尿失禁等尿失禁的药物的化合物，勃起功能障碍综合征等性功能障碍，类似物，肥胖症等。本发明人研究了具有5-HT 2C受体激动剂活性的化合物，并且发现本发明的苯并氮杂化合物具有优异的5-HT 2C受体激动剂活性，从而完成了本发明。也就是说，本发明的苯并氮杂化合物具有5-HT 2C受体激动剂活性，可用作治疗或预防5-HT 2C受体相关疾病的药剂，特别是尿失禁，压力性尿失禁，压力性尿失禁，混合型尿失禁等，性功能障碍如勃起功能障碍综合征等，肥胖等。

5. 发明申请

US20110294881A1 METHODS FOR TREATING LOWER URINARY TRACT DISORDERS USING alpha2delta SUBUNIT CALCIUM CHANNEL MODULATORS WITH SMOOTH MUSCLE MODULATORS 审中-公开
标题翻译：使用具有平滑肌肉调节剂的α2δ亚基钙通道调节剂治疗下尿路感染性疾病的方法
公开(公告)号：US20110294881A1
公开(公告)日：2011-12-01
申请号：US13206216
申请日：2011-08-09
申请人： Matthew Oliver Fraser , Karl Bruce Thor , Edward C. Burgard , Lee R. Brettman , Steven B. Landau , Daniel J. Ricca
发明人： Matthew Oliver Fraser , Karl Bruce Thor , Edward C. Burgard , Lee R. Brettman , Steven B. Landau , Daniel J. Ricca
IPC分类号： A61K31/216 , A61P13/02 , A61K31/195
CPC分类号： A61K45/06 , A61K31/195 , A61K31/197 , A61K31/216 , A61K2300/00
摘要： A method is provided for using α2δ subunit calcium channel modulators or other compounds that interact with the α2δ calcium channel subunit in combination with one or more compounds with smooth muscle modulatory effects to treat and/or alleviate the symptoms associated with painful and non-painful lower urinary tract disorders in normal and spinal cord injured patients. According to the present invention, α2δ subunit calcium channel modulators include GABA analogs (e.g. gabapentin and pregabalin), fused bicyclic or tricyclic amino acid analogs of gabapentin, and amino acid compounds. Compounds with smooth muscle modulatory effects include antimuscarinics, β3 adrenergic agonists, spasmolytics, neurokinin receptor antagonists, bradykinin receptor antagonists, and nitric oxide donors.
摘要翻译：提供了一种使用α2δ亚基钙通道调节剂或与α2δ钙通道亚基相互作用的其它化合物与一种或多种具有平滑肌调节作用的化合物组合以治疗和/或缓解与疼痛和非痛苦性较低的症状相关的症状的方法正常和脊髓损伤患者尿路疾病。根据本发明，α2δ亚基钙通道调节剂包括GABA类似物（例如加巴喷丁和普瑞巴林），加巴喷丁的稠合双环或三环氨基酸类似物和氨基酸化合物。具有平滑肌调节作用的化合物包括抗毒蕈碱，3肾上腺素能激动剂，解痉药，神经激肽受体拮抗剂，缓激肽受体拮抗剂和一氧化氮供体。

6. 发明申请

US20090203792A1 METHODS OF TREATING NON-PAINFUL BLADDER DISORDERS USING ALPHA2DELTA SUBUNIT CALCIUM CHANNEL MODULATORS 审中-公开
标题翻译：使用ALPHA2DELTA亚音频通道调制器处理非阻塞性疾病的方法
公开(公告)号：US20090203792A1
公开(公告)日：2009-08-13
申请号：US12425674
申请日：2009-04-17
申请人： Karl Bruce Thor , Edward C. Burgard , Mathew Oliver Fraser
发明人： Karl Bruce Thor , Edward C. Burgard , Mathew Oliver Fraser
IPC分类号： A61K31/197 , A61P13/00
CPC分类号： A61K31/195 , A61K31/197
摘要： A method is provided for treatment of non-painful bladder disorders, particularly non-painful overactive bladder without loss of urine. The method comprises administration of an α2δ subunit calcium channel modulator, including gabapentin, pregabalin, GABA analogs, fused bicyclic or tricyclic amino acid analogs of gabapentin, amino acid compounds, and other compounds that interact with the α2δ calcium channel subunit.
摘要翻译：提供了一种用于治疗非痛性膀胱疾病，特别是非疼痛的膀胱过度活动症而不损失尿液的方法。该方法包括施用α2delta亚基钙通道调节剂，其包括加巴喷丁，加巴喷丁，GABA类似物，加巴喷丁的稠合双环或三环氨基酸类似物，氨基酸化合物和与α2dtata钙通道亚基相互作用的其它化合物。

7. 发明授权

US07459430B2 Methods of using ziconotide to treat overactive bladder 失效
标题翻译：使用齐考诺肽治疗膀胱过动症的方法
公开(公告)号：US07459430B2
公开(公告)日：2008-12-02
申请号：US11449489
申请日：2006-06-08
申请人： Matthew Oliver Fraser , Karl Bruce Thor , Edward C. Burgard
发明人： Matthew Oliver Fraser , Karl Bruce Thor , Edward C. Burgard
IPC分类号： A61K38/12
CPC分类号： A61K31/455 , A61K31/00
摘要： The invention relates to methods of using Cav2.2 subunit calcium channel modulators to treat painful and non-painful lower urinary tract disorders and the related genitourinary tract disorders vulvodynia and vulvar vestibulitis in normal and spinal cord injured patients.
摘要翻译：本发明涉及使用Cav2.2亚基钙通道调节剂治疗正常和脊髓损伤患者的疼痛和非痛苦的下尿路疾病以及相关的泌尿生殖道疾病外阴和外阴前庭炎的方法。

8. 发明授权

US07223754B2 Thiazolidinone, oxazolidinone, and imidazolone derivatives for treating lower urinary tract and related disorders 失效
公开(公告)号：US07223754B2
公开(公告)日：2007-05-29
申请号：US10990843
申请日：2004-11-17
申请人： Matthew Oliver Fraser , Karl Bruce Thor , Edward C. Burgard
发明人： Matthew Oliver Fraser , Karl Bruce Thor , Edward C. Burgard
IPC分类号： A61K31/54
CPC分类号： A61K31/426
摘要： The invention relates to methods of using Cav2.2 subunit calcium channel modulators, particularly thiazolidinone, oxazolidinone, and imidazolone derivatives, to treat lower urinary tract and related disorders.

9. 发明授权

US06864262B2 1-(2-m-methanesulfonamidophenylethyl)-4-(m-trifluoromethylphenyl) piperazine and pharmaceutically acceptable salts and solvents thereof 失效
标题翻译： 1-（2-间甲磺酰氨基苯乙基）-4-（间 - 三氟甲基苯基）哌嗪及其药学上可接受的盐和溶剂
公开(公告)号：US06864262B2
公开(公告)日：2005-03-08
申请号：US10432413
申请日：2001-11-16
申请人： John Mehnert Schaus , Dennis Charles Thompson , Karl Bruce Thor
发明人： John Mehnert Schaus , Dennis Charles Thompson , Karl Bruce Thor
IPC分类号： C07D295/12 , A61K31/495 , A61K45/06 , A61P13/10 , C07D295/135
CPC分类号： C07D295/135 , A61K31/495 , A61K45/06 , A61K2300/00
摘要： The present invention provides a compound of the formula (I) and the pharmaceutically acceptable salts and solvates thereof, which is useful for treating bladder over-activity or urinary incontinence.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐和溶剂合物，其可用于治疗膀胱过度活动或尿失禁。

10. 发明申请

US20110236318A1 ANIMAL MODEL OF AN EJACULATION-LIKE REFLEX 审中-公开
标题翻译：类似反射的动物模型
公开(公告)号：US20110236318A1
公开(公告)日：2011-09-29
申请号：US13069595
申请日：2011-03-23
申请人： Masayuki TANAHASHI , Karl Bruce THOR , Venkateswarlu KARICHETI
发明人： Masayuki TANAHASHI , Karl Bruce THOR , Venkateswarlu KARICHETI
IPC分类号： A01K67/027 , A61K49/00
CPC分类号： A61K49/0008 , A01K67/027 , A01K2227/105 , A01K2267/03
摘要： An animal model of an ejaculation-like reflex, wherein the ejaculation-like reflex is induced by continuous infusion of saline through a catheter extending into the proximal urethra of a non-human male animal, and wherein the urethra of the animal is occluded by extending and bending the penis at the base; and a method of screening a test substance for effectiveness in prevention or treatment of male ejaculatory dysfunction using the animal model.
摘要翻译：射精样反射的动物模型，其中通过连续输注生理盐水通过延伸到非人雄性动物的近端尿道的导管诱导射精样反射，并且其中动物的尿道通过延伸并将阴茎弯曲在基部; 以及使用动物模型筛选测试物质以预防或治疗男性射精功能障碍的有效性的方法。

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