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1. 发明申请

US20080103178A1 N-dihydroxyalkyl-substituted 2-oxo-imidazole derivatives 审中-公开
标题翻译： N-二羟基烷基取代的2-氧代 - 咪唑衍生物
公开(公告)号：US20080103178A1
公开(公告)日：2008-05-01
申请号：US11974130
申请日：2007-10-11
申请人： Masaya Hashimoto , Yoshikazu Iwasawa , Hiroshi Kawamoto , Hisashi Ohta , Satoshi Ozaki , Takeshi Sagara , Hiroki Sakoh , Atsushi Satoh
发明人： Masaya Hashimoto , Yoshikazu Iwasawa , Hiroshi Kawamoto , Hisashi Ohta , Satoshi Ozaki , Takeshi Sagara , Hiroki Sakoh , Atsushi Satoh
IPC分类号： A61K31/454 , A61P25/00
CPC分类号： C07D403/04
摘要： The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.
摘要翻译：本发明提供由式（I）表示的化合物，其中R代表二羟基取代的C 1 -C 6烷基，Cy代表任选地取代的C 6 -C 10 - 二环或三环脂族碳环基团。这些化合物作为伤害感受肽受体拮抗剂起作用，例如可用作对麻醉止痛药的耐受性，对麻醉性镇痛药或成瘾的依赖; 镇痛增强剂; 抗生素或食欲抑制剂; 认知障碍和痴呆/遗忘症的治疗或预防剂; 治疗发育性认知异常的药剂; 精神分裂症补救措施治疗神经变性疾病的药剂; 用于情感障碍的抗抑郁药或治疗剂; 尿崩症的治疗或预防剂; 多尿症的治疗或预防剂; 并补救低血压等。

2. 发明授权

US07300947B2 N-dihydroxyalkyl-substituted 2-oxo-imidazole derivatives 有权
公开(公告)号：US07300947B2
公开(公告)日：2007-11-27
申请号：US11484203
申请日：2006-07-11
申请人： Masaya Hashimoto , Yoshikazu Iwasawa , Hiroshi Kawamoto , Hisashi Ohta , Satoshi Ozaki , Takeshi Sagara , Hiroki Sakoh , Atsushi Satoh
发明人： Masaya Hashimoto , Yoshikazu Iwasawa , Hiroshi Kawamoto , Hisashi Ohta , Satoshi Ozaki , Takeshi Sagara , Hiroki Sakoh , Atsushi Satoh
IPC分类号： A01N43/40 , A01N43/52 , A61K31/445 , A61K31/415 , C07D211/32 , C07D403/02
CPC分类号： C07D403/04
摘要： The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.

3. 发明申请

US20070015792A1 N-dihydroxyalkyl-substituted 2-oxo-imidazole derivatives 有权
标题翻译： N-二羟基烷基取代的2-氧代 - 咪唑衍生物
公开(公告)号：US20070015792A1
公开(公告)日：2007-01-18
申请号：US11484203
申请日：2006-07-11
申请人： Masaya Hashimoto , Yoshikazu Iwasawa , Hiroshi Kawamoto , Hisashi Ohta , Satoshi Ozaki , Takeshi Sagara , Hiroki Sakoh , Atsushi Satoh
发明人： Masaya Hashimoto , Yoshikazu Iwasawa , Hiroshi Kawamoto , Hisashi Ohta , Satoshi Ozaki , Takeshi Sagara , Hiroki Sakoh , Atsushi Satoh
IPC分类号： A61K31/454 , C07D403/04
CPC分类号： C07D403/04
摘要： The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.
摘要翻译：本发明提供由式（I）表示的化合物，其中R代表二羟基取代的C 1 -C 6烷基，Cy代表任选地取代的C 6 -C 10 - 二环或三环脂族碳环基团。这些化合物作为伤害感受肽受体拮抗剂起作用，例如可用作对麻醉止痛药的耐受性，对麻醉性镇痛药或成瘾的依赖; 镇痛增强剂; 抗生素或食欲抑制剂; 认知障碍和痴呆/遗忘症的治疗或预防剂; 治疗发育性认知异常的药剂; 精神分裂症补救措施治疗神经变性疾病的药剂; 用于情感障碍的抗抑郁药或治疗剂; 尿崩症的治疗或预防剂; 多尿症的治疗或预防剂; 并补救低血压等。

4. 发明授权

US06258825B1 2-oxoimidazole derivatives 有权
标题翻译： 2-氧代咪唑衍生物
公开(公告)号：US06258825B1
公开(公告)日：2001-07-10
申请号：US09424114
申请日：1999-11-19
申请人： Satoshi Ozaki , Hiroshi Kawamoto , Yoshiki Ito , Kaori Hirano , Kyoko Hayashi , Yoshikazu Iwasawa
发明人： Satoshi Ozaki , Hiroshi Kawamoto , Yoshiki Ito , Kaori Hirano , Kyoko Hayashi , Yoshikazu Iwasawa
IPC分类号： A61K31454
CPC分类号： C07D401/04 , C07D403/04 , C07D451/06
摘要： The present invention relates to a compound represented by Formula [I] wherein represents an aromatic carbo- or heterocyclic ring which may have a substituent; Cy represents a mono-, bi- or tricyclic aliphatic carbocyclic group having 3 to 20 carbon atoms, which may have a substituent; represents a mono- or bicyclic aliphatic nitrogen-containing heterocyclic group having 3 to 14 carbon atoms, which may have a substituent; R1 represents a hydrogen atom, a lower alkenyl group, a lower alkynyl group, a cyclo(lower alkyl) group, an amino group, a lower alkylamino group, a di(lower alkyl)-amino group, a hydroxyl group, a lower alkoxy group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group or a di(lower alkyl)carbamoyl group, or a lower alkyl group which may have a substituent; and R2 represents a hydrogen atom or a lower alkyl group, a salt or ester thereof, a production process for the same, and an analgesic, a reliever against tolerance to a narcotic analgesic represented by morphine, a reliever against dependence on a narcotic analgesic represented by morphine, an analgesic enhancer, an antiobestic, a drug for ameliorating brain function, a remedy for schizophrenia, a remedy for Parkinsonism, a remedy for chorea, an antidepressant, a remedy for diabetes insipidus, a remedy for polyuria, or a remedy for hypotension, comprising an effective ingredient of the same.
摘要翻译：本发明涉及由式[I]表示的化合物，其表示可具有取代基的芳族碳 - 或杂环; Cy表示可具有取代基的碳原子数为3〜20的单环，二环或三环脂肪族碳环基，表示可具有取代基的碳原子数为3〜14的单环或二环脂族含氮杂环基， ; R1表示氢原子，低级烯基，低级炔基，环（低级烷基），氨基，低级烷基氨基，二（低级烷基） - 氨基，羟基，低级烷氧基羧基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基或二（低级烷基）氨基甲酰基或可以具有取代基的低级烷基; 并且R 2表示氢原子或低级烷基，其盐或酯，其制备方法，以及止痛剂，对由吗啡代表的麻醉止痛剂的耐受性的缓解剂，对依赖麻醉止痛剂的缓解剂吗啡，镇痛增强剂，抗胆碱药，用于改善脑功能的药物，精神分裂症的治疗方法，帕金森综合征的补救措施，舞蹈病的补救措施，抗抑郁药，尿崩症的治疗方法，多尿症的治疗方法或治疗方法低血压，包括其有效成分。

5. 发明申请

US20070078153A1 4-Oxoimidazolidine-2-spiropiperidine derivatives 失效
标题翻译： 4-氧代咪唑烷-2-螺哌啶衍生物
公开(公告)号：US20070078153A1
公开(公告)日：2007-04-05
申请号：US11603147
申请日：2006-11-22
申请人： Masaya Hashimoto , Osamu Okamoto , Satoshi Ozaki , Hisashi Ohta
发明人： Masaya Hashimoto , Osamu Okamoto , Satoshi Ozaki , Hisashi Ohta
IPC分类号： A61K31/4747 , C07D471/10
CPC分类号： C07D471/10
摘要： The invention relates to 4-oxoimidazolidine-2-spiropiperidine derivatives represented by a general formula [I] [in which A1, A2, A3, A4 and A5 stand for optionally halogen-substituted methine, or nitrogen atom; R1 and R2 stand for lower alkyl or the like; R3 stands for hydrogen or lower alkyl; R4 and R5 stand for hydrogen, or lower alkyl which is optionally substituted with hydroxy, or the like]or salts thereof These compounds act as nociceptin receptor agonist, and are useful as analgesic, reliever from tolerance to narcotic analgesic, reliever from dependence on narcotic analgesic, analgesic enhancer, antiobestic, drug for ameliorating brain function, remedy for schizophrenia, drug for treating regressive neurodegenerative diseases, antianxiety agent or antidepressant and remedy for diabetes insipidus and polyuria; and the like.
摘要翻译：本发明涉及由通式[I]表示的4-氧代咪唑烷-2-螺哌啶衍生物[其中A 1，A 2，A 3，任选地，卤素取代的次甲基或氮原子的烷基，亚氨基， R 1和R 2代表低级烷基等; R 3代表氢或低级烷基; R 4和R 5代表氢，或任选被羟基取代的低级烷基等）或其盐这些化合物作为伤害感受肽受体激动剂起作用，并且是可用作止痛剂，缓解药物对麻醉止痛药的缓解，依赖麻醉止痛药缓解，镇痛增强剂，抗胆碱药物，改善脑功能的药物，精神分裂症治疗药物，治疗退行性神经退行性疾病药物，抗焦虑剂或抗抑郁药物及对尿崩症的治疗多尿等等。

6. 发明授权

US07557117B2 4-oxoimidazolidine-2-spiropiperidine derivatives 失效
标题翻译： 4-氧代咪唑烷-2-螺哌啶衍生物
公开(公告)号：US07557117B2
公开(公告)日：2009-07-07
申请号：US11603147
申请日：2006-11-22
申请人： Masaya Hashimoto , Osamu Okamoto , Satoshi Ozaki , Hisashi Ohta
发明人： Masaya Hashimoto , Osamu Okamoto , Satoshi Ozaki , Hisashi Ohta
IPC分类号： A61K31/438 , C07D401/04
CPC分类号： C07D471/10
摘要： The invention relates to 4-oxoimidazolidine-2-spiropiperidine derivatives represented by a general formula [I] [in which A1, A2, A3, A4 and A5 stand for optionally halogen-substituted methine, or nitrogen atom; R1 and R2 stand for lower alkyl or the like; R3 stands for hydrogen or lower alkyl; R4 and R5 stand for hydrogen, or lower alkyl which is optionally substituted with hydroxy, or the like]or salts thereof. These compounds act as nociceptin receptor agonist, and are useful as analgesic, reliever from tolerance to narcotic analgesic, reliever from dependence on narcotic analgesic, analgesic enhancer, antiobestic, drug for ameliorating brain function, remedy for schizophrenia, drug for treating regressive neurodegenerative diseases, antianxiety agent or antidepressant and remedy for diabetes insipidus and polyuria; and the like.
摘要翻译：本发明涉及由通式[I]表示的4-氧代咪唑烷-2-螺哌啶衍生物[其中A1，A2，A3，A4和A5代表任选卤素取代的次甲基或氮原子; R1和R2代表低级烷基等; R3代表氢或低级烷基; R4和R5代表氢，或任选被羟基取代的低级烷基，或其盐。这些化合物作为伤害感受肽受体激动剂起作用，可用作镇痛药，缓解麻醉止痛药耐受性，缓解依赖麻醉止痛药，镇痛增强剂，抗胆固醇药，改善脑功能药物，精神分裂症药物治疗，治疗退行性神经退行性疾病药物，抗焦虑药或抗抑郁药及其治疗尿崩症及多尿症; 等等。

7. 发明授权

US07829586B2 Aryl-substituted nitrogen-containing heterocyclic compounds 有权
标题翻译：芳基取代的含氮杂环化合物
公开(公告)号：US07829586B2
公开(公告)日：2010-11-09
申请号：US11992817
申请日：2006-09-28
申请人： Hirokatsu Ito , Kensuke Kobayashi , Hisashi Ohta , Osamu Okamoto , Satoshi Ozaki , Tomohiro Tsujita
发明人： Hirokatsu Ito , Kensuke Kobayashi , Hisashi Ohta , Osamu Okamoto , Satoshi Ozaki , Tomohiro Tsujita
IPC分类号： A61K31/4439 , A61K31/415 , A61K31/4184 , C07D401/02 , C07D235/02 , C07D231/10
CPC分类号： C07D405/12 , C07D207/335 , C07D231/12 , C07D233/64 , C07D401/04
摘要： Disclosed is an aryl-substituted nitrogen-containing heterocyclic compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof. This compound serves as nociceptin receptor antagonist and is useful as a pharmaceutical agent for treating diseases associated with a nociceptin receptor. (I) [in the formula, A1, A2 and A3 independently represent a carbon atom or a nitrogen atom, and one or two of A1, A2 and A3 represent a carbon atom; R1 represents a lower alkyl group or the like; R2 represents a phenyl group which may be substituted with a halogen atom or the like; R3 represents a hydrogen atom, a lower alkyl group or the like; and R4 represents a lower alkyl group or the like.]
摘要翻译：公开了由下式（I）表示的芳基取代的含氮杂环化合物或其药学上可接受的盐。该化合物用作伤害感受肽受体拮抗剂，可用作治疗与伤害感受肽受体相关疾病的药剂。（I）[式中，A1，A2和A3独立地表示碳原子或氮原子，A1，A2和A3中的一个或二个表示碳原子; R1表示低级烷基等; R 2表示可以被卤素原子等取代的苯基; R3表示氢原子，低级烷基等; R4表示低级烷基等。]

8. 发明申请

US20090025095A1 Method for Evaluating Compound Using Barlp and Substance for Regulating Eating and Body Weight 审中-公开
标题翻译：使用Barlp和物质评价化合物调节饮食和体重的方法
公开(公告)号：US20090025095A1
公开(公告)日：2009-01-22
申请号：US11918099
申请日：2006-04-25
申请人： Hirohide Nambu , Satoshi Ozaki , Takeshi Tanaka , Hisashi Ohta
发明人： Hirohide Nambu , Satoshi Ozaki , Takeshi Tanaka , Hisashi Ohta
IPC分类号： G01N33/53 , G01N33/00 , C07K16/00 , C07H21/04 , C07H21/02 , C07K14/00 , C07K2/00
CPC分类号： G01N33/74 , C12Q1/6883 , C12Q2600/136 , C12Q2600/158 , G01N2333/72 , G01N2500/10 , G01N2800/303
摘要： It is intended to provide a method for evaluating a compound which regulates eating or body weight characterized by comprising the steps of introducing a BARLP gene and preparing a cell expressing BARLP; bringing a test compound into contact with the cell; and detecting a specific binding of the test compound to the BARLP and a method for evaluating a compound further comprising the step of evaluating a test compound using a nonhuman genetically-engineered animal in which the BARLP gene is inactivated. According to this invention, knowledge about a relationship between BARLP and biological functions is obtained and a method for evaluating a compound targeting BARLP and a BARLP ligand obtained by the evaluation can be provided.
摘要翻译：旨在提供一种评估调节进食或体重的化合物的方法，其特征在于包括引入BARLP基因并制备表达BARLP的细胞的步骤; 使测试化合物与细胞接触; 以及检测所述测试化合物与所述BARLP的特异性结合，以及评价化合物的方法，其还包括使用其中所述BARLP基因失活的非人基因工程动物评估测试化合物的步骤。根据本发明，可以获得关于BARLP与生物功能之间的关系的知识，并且可以提供通过评价获得的靶向BARLP和BARLP配体的化合物的评价方法。

9. 发明申请

US20070275379A1 Simian Orl1 Gene and Method of Assessing Compound 审中-公开
标题翻译：猿猴Orl1基因及其鉴定方法
公开(公告)号：US20070275379A1
公开(公告)日：2007-11-29
申请号：US10577827
申请日：2004-11-08
申请人： Kazumi Koga , Satoshi Ozaki , Daisuke Ichikawa , Hirohide Nambu , Tomoko Azuma , Naoko Sakai , Hiroko Kawagoe , Hisashi Ohta
发明人： Kazumi Koga , Satoshi Ozaki , Daisuke Ichikawa , Hirohide Nambu , Tomoko Azuma , Naoko Sakai , Hiroko Kawagoe , Hisashi Ohta
IPC分类号： C12Q1/68 , C07H21/02 , C07K14/705 , C12N5/06
CPC分类号： C07K14/705
摘要： A nucleic acid having a base sequence of SEQ ID NO. 1; a protein having an amino acid sequence of SEQ ID NO. 2; a recombinant vector comprising a gene constituted of the above nucleic acid; and a transformant cell comprising the recombinant vector. By the use of these, it is feasible to provide ORL1 gene of non-human primates, etc. and to perform assessment, screening, etc. of compounds acting on the ORL1.
摘要翻译：具有SEQ ID NO：1的碱基序列的核酸。 1; 具有SEQ ID NO：1的氨基酸序列的蛋白质。 2; 包含由上述核酸构成的基因的重组载体; 和包含重组载体的转化体细胞。通过使用这些，可以提供非人灵长类动物的ORL1基因等，并对作用于ORL1的化合物进行评估，筛选等。

10. 发明申请

US20090275617A1 Aryl-Substituted Nitrogen-Containing Heterocyclic Compounds 有权
标题翻译：芳基取代的含氮杂环化合物
公开(公告)号：US20090275617A1
公开(公告)日：2009-11-05
申请号：US11992817
申请日：2006-09-28
申请人： Hirokatsu Ito , Kensuke Kobayashi , Hisashi Ohta , Osamu Okamoto , Satoshi Ozaki , Tomohiro Tsujita
发明人： Hirokatsu Ito , Kensuke Kobayashi , Hisashi Ohta , Osamu Okamoto , Satoshi Ozaki , Tomohiro Tsujita
IPC分类号： A61K31/4439 , A61K31/4164 , A61K31/415 , C07D401/02 , C07D233/64 , C07D231/12 , C07D207/335 , A61P25/00
CPC分类号： C07D405/12 , C07D207/335 , C07D231/12 , C07D233/64 , C07D401/04
摘要： Disclosed is an aryl-substituted nitrogen-containing heterocyclic compound represented by the formula (I) below or a pharmaceutically acceptable salt thereof. This compound serves as nociceptin receptor antagonist and is useful as a pharmaceutical agent for treating diseases associated with a nociceptin receptor. (I) [in the formula, A1, A2 and A3 independently represent a carbon atom or a nitrogen atom, and one or two of A1, A2 and A3 represent a carbon atom; R1 represents a lower alkyl group or the like; R2 represents a phenyl group which may be substituted with a halogen atom or the like; R3 represents a hydrogen atom, a lower alkyl group or the like; and R4 represents a lower alkyl group or the like.]
摘要翻译：公开了由下式（I）表示的芳基取代的含氮杂环化合物或其药学上可接受的盐。该化合物用作伤害感受肽受体拮抗剂，可用作治疗与伤害感受肽受体相关疾病的药剂。（I）[式中，A1，A2和A3独立地表示碳原子或氮原子，A1，A2和A3中的一个或二个表示碳原子; R1表示低级烷基等; R 2表示可以被卤素原子等取代的苯基; R3表示氢原子，低级烷基等; R4表示低级烷基等。]

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