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1. 发明授权

US08404858B2 Agent for regeneration and/or protection of nerves 有权
标题翻译：神经再生和/或保护剂
公开(公告)号：US08404858B2
公开(公告)日：2013-03-26
申请号：US12944326
申请日：2010-11-11
申请人： Kazuyuki Ohmoto , Akihiro Kinoshita , Hidekazu Matsuya
发明人： Kazuyuki Ohmoto , Akihiro Kinoshita , Hidekazu Matsuya
IPC分类号： C07D277/04
CPC分类号： A61K31/426 , A61K9/0019 , A61K31/427 , A61K45/06 , A61K47/6951 , B82Y5/00 , C07D277/20 , C07D277/56 , C07D417/12
摘要： An EP2 agonist which may have an EP3 agonistic effect has an effect of regenerating and/or protecting nerves, and is therefore useful as a therapeutic agent for a disease of the peripheral nervous system, such as a lower or upper motor neuron disease, a nerve root disease, plexopathy, thoracic outlet compression syndrome, peripheral neuropathy, neurofibromatosis and neuromuscular transmission disease. An EP2 agonist which has an EP3 agonistic effect is a safe and effective agent for the regeneration and/or protection of nerves which has little influence on the circulatory system.
摘要翻译：可能具有EP3激动作用的EP2激动剂具有再生和/或保护神经的作用，因此可用作周围神经系统疾病的治疗剂，例如下部或上部运动神经元疾病，神经根系疾病，癫痫病，胸出口压迫综合征，周围神经病变，神经纤维瘤病和神经肌肉传播疾病。具有EP3激动作用的EP2激动剂是对循环系统影响不大的神经的再生和/或保护的安全有效的药剂。

2. 发明授权

US07863263B2 Agent for regeneration and/or protection of nerves 有权
标题翻译：神经再生和/或保护剂
公开(公告)号：US07863263B2
公开(公告)日：2011-01-04
申请号：US11916374
申请日：2006-06-02
申请人： Kazuyuki Ohmoto , Akihiro Kinoshita , Hidekazu Matsuya
发明人： Kazuyuki Ohmoto , Akihiro Kinoshita , Hidekazu Matsuya
IPC分类号： A61K31/33 , C07D277/04
CPC分类号： A61K31/426 , A61K9/0019 , A61K31/427 , A61K45/06 , A61K47/6951 , B82Y5/00 , C07D277/20 , C07D277/56 , C07D417/12
摘要： An EP2 agonist which may have an EP3 agonistic effect has an effect of regenerating and/or protecting nerves, and is therefore useful as a therapeutic agent for a disease of the peripheral nervous system, such as a lower or upper motor neuron disease, a nerve root disease, plexopathy, thoracic outlet compression syndrome, peripheral neuropathy, neurofibromatosis and neuromuscular transmission disease. An EP2 agonist which has an EP3 agonistic effect is a safe and effective agent for the regeneration and/or protection of nerves which has little influence on the circulatory system.
摘要翻译：可能具有EP3激动作用的EP2激动剂具有再生和/或保护神经的作用，因此可用作周围神经系统疾病的治疗剂，例如下部或上部运动神经元疾病，神经根系疾病，癫痫病，胸出口压迫综合征，周围神经病变，神经纤维瘤病和神经肌肉传播疾病。具有EP3激动作用的EP2激动剂是对循环系统影响不大的神经的再生和/或保护的安全有效的药剂。

3. 发明授权

US08410281B2 Compound having detrusor muscle-contracting activity and urethral sphincter muscle-relaxing activity 有权
公开(公告)号：US08410281B2
公开(公告)日：2013-04-02
申请号：US13377047
申请日：2010-06-09
申请人： Kazuyuki Ohmoto , Akihiro Kinoshita , Hidekazu Matsuya , Hiroki Okada
发明人： Kazuyuki Ohmoto , Akihiro Kinoshita , Hidekazu Matsuya , Hiroki Okada
IPC分类号： A61K31/426 , C07D277/56
CPC分类号： C07D277/56 , A61K31/426 , A61K45/06 , A61K47/6951 , B82Y5/00 , C07D277/20 , C07D277/36 , C08B37/00
摘要： Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and/or ameliorating underactive bladder.

4. 发明授权

US08501793B2 Blood flow promoters for cauda equina tissues 失效
标题翻译：马尾组织血流促进剂
公开(公告)号：US08501793B2
公开(公告)日：2013-08-06
申请号：US12889731
申请日：2010-09-24
申请人： Kazuyuki Ohmoto , Akihiro Kinoshita , Yoshihisa Kamanaka , Hidekazu Matsuya
发明人： Kazuyuki Ohmoto , Akihiro Kinoshita , Yoshihisa Kamanaka , Hidekazu Matsuya
IPC分类号： A61K31/425 , A61K31/19 , A61K31/557
CPC分类号： A61K31/5575 , A61K31/427 , A61K31/429 , A61K31/559 , C07C405/00 , C07D277/56
摘要： It is intended to provide highly safe and efficacious blood flow promoters for cauda equina tissues. Among prostaglandin-like compounds having a weak hypotensive effect, compounds having an effect of promoting the blood flow in cauda equina tissues (excluding limaprost) are useful as highly safe blood flow promoters for cauda equina tissues and, therefore, are efficacious in preventing and/or treating lumbar pain, lower limb pain, lower limb palsy, intermittent claudication, vesicorectal failure, hypogonadism, etc. caused by cauda equina injuries.
摘要翻译：旨在为马尾组织提供高度安全有效的血液流动促进剂。在具有低血压降低作用的前列腺素样化合物中，具有促进马尾组织（不包括利马前列素）中的血流的作用的化合物可用作马尾组织的高度安全的血液流动促进剂，因此有效地预防和/ 或治疗由马尾损伤引起的腰痛，下肢疼痛，下肢麻痹，间歇性跛行，膀胱直肠功能衰竭，性腺机能减退等。

5. 发明授权

US07833995B2 Blood flow promoters for cauda equina tissues 有权
标题翻译：马尾组织血流促进剂
公开(公告)号：US07833995B2
公开(公告)日：2010-11-16
申请号：US10581619
申请日：2004-12-02
申请人： Kazuyuki Ohmoto , Akihiro Kinoshita , Yoshihisa Kamanaka , Hidekazu Matsuya
发明人： Kazuyuki Ohmoto , Akihiro Kinoshita , Yoshihisa Kamanaka , Hidekazu Matsuya
IPC分类号： A01N43/78 , A61K31/425
CPC分类号： A61K31/5575 , A61K31/427 , A61K31/429 , A61K31/559 , C07C405/00 , C07D277/56
摘要： It is intended to provide highly safe and efficacious blood flow promoters for cauda equina tissues. Among prostaglandin-like compounds having a weak hypotensive effect, compounds having an effect of promoting the blood flow in cauda equina tissues (excluding limaprost) are useful as highly safe blood flow promoters for cauda equina tissues and, therefore, are efficacious in preventing and/or treating lumbar pain, lower limb pain, lower limb palsy, intermittent claudication, vesicorectal failure, hypogonadism, etc. caused by cauda equina injuries.
摘要翻译：旨在为马尾组织提供高度安全有效的血液流动促进剂。在具有低血压降低作用的前列腺素样化合物中，具有促进马尾组织（不包括利马前列素）中的血流的作用的化合物可用作马尾组织的高度安全的血液流动促进剂，因此有效地预防和/ 或治疗由马尾损伤引起的腰痛，下肢疼痛，下肢麻痹，间歇性跛行，膀胱直肠功能衰竭，性腺机能减退等。

6. 发明申请

US20090227644A1 AGENT FOR REGENERATION AND/OR PROTECTION OF NERVES 有权
标题翻译：用于再生和/或保护神经的药剂
公开(公告)号：US20090227644A1
公开(公告)日：2009-09-10
申请号：US11916374
申请日：2006-06-02
申请人： Kazuyuki Ohmoto , Akihiro Kinoshita , Hidekazu Matsuya
发明人： Kazuyuki Ohmoto , Akihiro Kinoshita , Hidekazu Matsuya
IPC分类号： A61K31/425 , C07D277/56 , A61P25/00
CPC分类号： A61K31/426 , A61K9/0019 , A61K31/427 , A61K45/06 , A61K47/6951 , B82Y5/00 , C07D277/20 , C07D277/56 , C07D417/12
摘要： An EP2 agonist which may have an EP3 agonistic effect has an effect of regenerating and/or protecting nerves, and is therefore useful as a therapeutic agent for a disease of the peripheral nervous system, such as a lower or upper motor neuron disease, a nerve root disease, plexopathy, thoracic outlet compression syndrome, peripheral neuropathy, neurofibromatosis and neuromuscular transmission disease. An EP2 agonist which has an EP3 agonistic effect is a safe and effective agent for the regeneration and/or protection of nerves which has little influence on the circulatory system.
摘要翻译：可能具有EP3激动作用的EP2激动剂具有再生和/或保护神经的作用，因此可用作周围神经系统疾病的治疗剂，例如下部或上部运动神经元疾病，神经根系疾病，癫痫病，胸出口压迫综合征，周围神经病变，神经纤维瘤病和神经肌肉传播疾病。具有EP3激动作用的EP2激动剂是对循环系统影响不大的神经的再生和/或保护的安全有效的药剂。

7. 发明申请

US20070129327A1 Blood flow promoters for cauda equina tissues 有权
标题翻译：马尾组织血流促进剂
公开(公告)号：US20070129327A1
公开(公告)日：2007-06-07
申请号：US10581619
申请日：2004-12-02
申请人： Kazuyuki Ohmoto , Akihiro Kinoshita , Yoshihisa Kamanaka , Hidekazu Matsuya
发明人： Kazuyuki Ohmoto , Akihiro Kinoshita , Yoshihisa Kamanaka , Hidekazu Matsuya
IPC分类号： A61K31/724 , A61K31/558 , A61K31/557
CPC分类号： A61K31/5575 , A61K31/427 , A61K31/429 , A61K31/559 , C07C405/00 , C07D277/56
摘要： It is intended to provide highly safe and efficacious blood flow promoters for cauda equina tissues. Among prostaglandin-like compounds having a weak hypotensive effect, compounds having an effect of promoting the blood flow in cauda equina tissues (excluding limaprost) are useful as highly safe blood flow promoters for cauda equina tissues and, therefore, are efficacious in preventing and/or treating lumbar pain, lower limb pain, lower limb palsy, intermittent claudication, vesicorectal failure, hypogonadism, etc. caused by cauda equina injuries.
摘要翻译：旨在为马尾组织提供高度安全有效的血液流动促进剂。在具有低血压降低作用的前列腺素样化合物中，具有促进马尾组织（不包括利马前列素）中的血流的作用的化合物可用作马尾组织的高度安全的血液流动促进剂，因此有效地预防和/ 或治疗由马尾损伤引起的腰痛，下肢疼痛，下肢麻痹，间歇性跛行，膀胱直肠功能衰竭，性腺机能减退等。

8. 发明申请

US20110015238A1 BLOOD FLOW PROMOTERS FOR CAUDA EQUINA TISSUES 失效
标题翻译：用于CAUDA EQUINA TISSUES的血液流动促进剂
公开(公告)号：US20110015238A1
公开(公告)日：2011-01-20
申请号：US12889731
申请日：2010-09-24
申请人： Kazuyuki Ohmoto , Akihiro Kinoshita , Yoshihisa Kamanaka , Hidekazu Matsuya
发明人： Kazuyuki Ohmoto , Akihiro Kinoshita , Yoshihisa Kamanaka , Hidekazu Matsuya
IPC分类号： A61K31/429 , C07D417/12 , A61K31/427 , A61P9/12 , A61K31/5575 , C07C405/00 , C07D515/18
CPC分类号： A61K31/5575 , A61K31/427 , A61K31/429 , A61K31/559 , C07C405/00 , C07D277/56
摘要： It is intended to provide highly safe and efficacious blood flow promoters for cauda equina tissues. Among prostaglandin-like compounds having a weak hypotensive effect, compounds having an effect of promoting the blood flow in cauda equina tissues (excluding limaprost) are useful as highly safe blood flow promoters for cauda equina tissues and, therefore, are efficacious in preventing and/or treating lumbar pain, lower limb pain, lower limb palsy, intermittent claudication, vesicorectal failure, hypogonadism, etc. caused by cauda equina injuries.
摘要翻译：旨在为马尾组织提供高度安全有效的血液流动促进剂。在具有低血压降低作用的前列腺素样化合物中，具有促进马尾组织（不包括利马前列素）中的血流的作用的化合物可用作马尾组织的高度安全的血液流动促进剂，因此有效地预防和/ 或治疗由马尾损伤引起的腰痛，下肢疼痛，下肢麻痹，间歇性跛行，膀胱直肠功能衰竭，性腺机能减退等。

9. 发明申请

US20120088805A1 COMPOUND HAVING DETRUSOR MUSCLE-CONTRACTING ACTIVITY AND URETHRAL SPHINCTER MUSCLE-RELAXING ACTIVITY 有权
标题翻译：具有抑制性肌肉收缩活性的化合物和URETHRAL SPHINCTER肌肉松弛活性
公开(公告)号：US20120088805A1
公开(公告)日：2012-04-12
申请号：US13377047
申请日：2010-06-09
申请人： Kazuyuki Ohmoto , Akihiro Kinoshita , Hidekazu Matsuta , Hiroki Okada
发明人： Kazuyuki Ohmoto , Akihiro Kinoshita , Hidekazu Matsuta , Hiroki Okada
IPC分类号： A61K31/426 , A61P13/02 , A61P13/10 , C07D277/56 , C08B37/16
CPC分类号： C07D277/56 , A61K31/426 , A61K45/06 , A61K47/6951 , B82Y5/00 , C07D277/20 , C07D277/36 , C08B37/00
摘要： Since a compound represented by formula (I) wherein all of the symbols are the same as defined in the specification, a salt thereof, a solvate thereof, a prodrug thereof, a mixture with a diastereomer thereof in an arbitrary ratio, or a cyclodextrin clathrate thereof have a contracting activity of bladder detrusor and a relaxing activity of urethral sphincter, they can ameliorate bladder contraction dysfunction and/or urethral relaxation dysfunction, and for example, are effective for underactive bladder. Additionally, the compound of the present invention has little risk of side effects on the urinary system, the circulatory system and the digestive system, and exhibits excellent pharmacokinetics, such as oral absorbability etc. Therefore, the compound of the present invention is useful as a superior agent for preventing, treating and/or ameliorating underactive bladder.
摘要翻译：由于其中所有符号与说明书中所定义的相同的式（I）表示的化合物，其盐，其溶剂合物，前药，任意比例的非对映异构体的混合物或环糊精包合物其具有膀胱逼尿肌的收缩活动和尿道括约肌的放松活动，它们可以改善膀胱收缩功能障碍和/或尿道松弛功能障碍，并且例如对膀胱活动不足有效。此外，本发明的化合物对尿液系统，循环系统和消化系统几乎没有副作用的风险，并且表现出优异的药代动力学，例如口服吸收性等。因此，本发明的化合物可用作用于预防，治疗和/或改善膀胱活动不足的优良药剂。

10. 发明授权

US08115014B2 Ethynylindole compounds 有权
标题翻译：乙炔基吲哚化合物
公开(公告)号：US08115014B2
公开(公告)日：2012-02-14
申请号：US12644378
申请日：2009-12-22
申请人： Kazuyuki Ohmoto , Satoshi Itadani , Yoshisuke Nakayama , Jun Takeuchi , Manabu Fujita
发明人： Kazuyuki Ohmoto , Satoshi Itadani , Yoshisuke Nakayama , Jun Takeuchi , Manabu Fujita
IPC分类号： C07D209/04 , A61K31/405 , A61K31/40
CPC分类号： C07D209/18
摘要： As a compound having a potent oral activity and a long-lasting cysLT1/cysLT2 receptor antagonistic activity, the compound of the formula (I): which exhibits potent antagonistic activity against the cysLT1/cysLT2 receptor, and have long-lasting effects even in case of oral administration, and therefore is useful as an oral agent for preventing and/or treating a variety of diseases, for example, respiratory disease (for example, asthma (bronchial asthma, etc.), chronic obstructive pulmonary disease (COPD), pulmonary emphysema, chronic bronchitis, pneumonia (interstitial pneumonia, etc.), severe acute respiratory syndrome (SARS), acute respiratory distress syndrome (ARDS), apnea syndrome, allergic rhinitis, sinusitis (acute sinusitis, chronic sinusitis, etc.), pulmonary fibrosis, coughing (chronic coughing, etc.), and the like) was developed.
摘要翻译：作为具有有效的口服活性和持久的cysLT1 / cysLT2受体拮抗活性的化合物，式（I）化合物：其对cysLT1 / cysLT2受体具有强的拮抗活性，并且即使在例如因此可用作预防和/或治疗各种疾病的口服药物，例如呼吸系统疾病（例如哮喘（支气管哮喘等），慢性阻塞性肺病（COPD），肺部肺气肿，慢性支气管炎，肺炎（间质性肺炎等），严重急性呼吸综合征（SARS），急性呼吸窘迫综合征（ARDS），呼吸暂停综合征，过敏性鼻炎，鼻窦炎（急性鼻窦炎，慢性鼻窦炎等），肺纤维化，咳嗽（慢性咳嗽等）等）。

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