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1. 发明授权

US07855297B2 Amide derivatives and medicinal use thereof 失效
标题翻译：酰胺衍生物及其药用
公开(公告)号：US07855297B2
公开(公告)日：2010-12-21
申请号：US10380502
申请日：2001-09-14
申请人： Mitsuharu Nakamura , Takao Kamahori , Seigo Ishibuchi , Yoichi Naka , Hiroshi Sumichika , Katsuhiko Itoh
发明人： Mitsuharu Nakamura , Takao Kamahori , Seigo Ishibuchi , Yoichi Naka , Hiroshi Sumichika , Katsuhiko Itoh
IPC分类号： C07D401/00 , A61K31/44
CPC分类号： C07D213/40 , C07C233/59 , C07C233/60 , C07C233/62 , C07C235/40 , C07C255/29 , C07C255/60 , C07C317/32 , C07C317/40 , C07C323/40 , C07C327/46 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D213/64 , C07D213/65 , C07D213/69 , C07D213/74 , C07D213/75 , C07D215/50 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/28 , C07D295/13 , C07D295/135 , C07D295/185 , C07D309/12 , C07D311/04 , C07D311/66 , C07D317/58 , C07D317/66 , C07D319/18 , C07D333/20 , C07D333/36 , C07D335/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention relates to an amide derivative of the formula (1), having a C5a receptor antagonistic action wherein each symbol is as defined in the specification. The above-mentioned amide derivative, an optically active form thereof and a pharmaceutically acceptable salt thereof are promising as an agent for the treatment or prophylaxis of diseases or syndromes caused by inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis and pancreatitis and the like) due to activation of leukocytes caused by ischemia reperfusion, trauma, burn, surgical invasion and the like]. Moreover, they are useful as a therapeutic or prophylactic agent for the infectious diseases caused by bacteria and virus that invade via a C5a receptor.
摘要翻译：本发明涉及具有C5a受体拮抗作用的式（1）的酰胺衍生物，其中每个符号如说明书中所定义。上述酰胺衍生物，其光学活性形式和其药学上可接受的盐有望用作治疗或预防由C5a引起的炎症引起的疾病或综合征的药物[例如，自身免疫疾病如风湿病，系统性红斑狼疮败血症，成人呼吸窘迫综合征，慢性阻塞性肺病，哮喘等过敏性疾病，动脉粥样硬化，心肌梗死，脑梗塞，牛皮癣，阿尔茨海默病和严重器官损伤（例如肺炎，肾炎，肝炎和胰腺炎等）由于由缺血再灌注，创伤，烧伤，手术入侵等引起的白细胞的活化]。此外，它们可用作由通过C5a受体侵入的细菌和病毒引起的感染性疾病的治疗或预防剂。

2. 发明授权

US07105567B2 3-substituted urea derivatives and medicinal use thereof 失效
标题翻译： 3-取代的脲衍生物及其医药用途
公开(公告)号：US07105567B2
公开(公告)日：2006-09-12
申请号：US10343961
申请日：2001-08-10
申请人： Seigo Ishibuchi , Hiroshi Sumichika , Katsuhiko Itoh , Yoichi Naka
发明人： Seigo Ishibuchi , Hiroshi Sumichika , Katsuhiko Itoh , Yoichi Naka
IPC分类号： A61K31/36 , A61K31/17 , C07D317/44 , C07C275/28 , C07C275/30
CPC分类号： C07D213/64 , A61K31/17 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C275/42 , C07C323/43 , C07C323/44 , C07D209/14 , C07D231/12 , C07D295/135 , C07D317/58 , C07D401/06
摘要： The present invention relates to a urea derivative of the formula (1) wherein each symbol is as described in the specification, a pharmaceutically acceptable salt thereof and pharmaceutical use thereof. The compound of the present invention has a C5a receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of diseases or syndromes due to inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis, pancreatitis and the like) due to activation of leukocytes caused by ischemia, trauma, burn, surgical invasion and the like]. In addition, it is useful as an agent for the prophylaxis or treatment of infectious diseases caused by bacteria or virus that invades via a C5a receptor.
摘要翻译：本发明涉及式（1）的脲衍生物，其中每个符号如说明书中所述，其药学上可接受的盐和药物用途。本发明化合物具有C5a受体拮抗作用，可用作预防或治疗由C5a引起的炎症引起的疾病或综合征的药剂[例如，自身免疫疾病如风湿病，系统性红斑狼疮等，败血症，成人呼吸窘迫综合征，慢性阻塞性肺病，哮喘等过敏性疾病，动脉粥样硬化，心肌梗塞，脑梗塞，牛皮癣，阿尔茨海默病和严重器官损伤（例如肺炎，肾炎，肝炎，胰腺炎等）由于缺血引起的白细胞活化，创伤，烧伤，手术入侵等]。此外，作为预防或治疗由通过C5a受体侵入的细菌或病毒引起的感染性疾病的药剂是有用的。

3. 发明授权

US08198454B2 Amide derivatives and medicinal use thereof 失效
标题翻译：酰胺衍生物及其药用
公开(公告)号：US08198454B2
公开(公告)日：2012-06-12
申请号：US12458095
申请日：2009-06-30
申请人： Mitsuharu Nakamura , Takao Kamahori , Seigo Ishibuchi , Yoichi Naka , Hiroshi Sumichika , Katsuhiko Itoh
发明人： Mitsuharu Nakamura , Takao Kamahori , Seigo Ishibuchi , Yoichi Naka , Hiroshi Sumichika , Katsuhiko Itoh
IPC分类号： C07D401/00 , A61K31/44
CPC分类号： C07D213/40 , C07C233/59 , C07C233/60 , C07C233/62 , C07C235/40 , C07C255/29 , C07C255/60 , C07C317/32 , C07C317/40 , C07C323/40 , C07C327/46 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07D213/64 , C07D213/65 , C07D213/69 , C07D213/74 , C07D213/75 , C07D215/50 , C07D231/12 , C07D233/56 , C07D249/08 , C07D277/28 , C07D295/13 , C07D295/135 , C07D295/185 , C07D309/12 , C07D311/04 , C07D311/66 , C07D317/58 , C07D317/66 , C07D319/18 , C07D333/20 , C07D333/36 , C07D335/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention relates to an amide derivative of the formula (1), having a C5a receptor antagonistic action wherein each symbol is as defined in the specification. The above-mentioned amide derivative, an optically active form thereof and a pharmaceutically acceptable salt thereof are promising as an agent for the treatment or prophylaxis of diseases or syndromes caused by inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis and pancreatitis and the like) due to activation of leukocytes caused by ischemia reperfusion, trauma, burn, surgical invasion and the like]. Moreover, they are useful as a therapeutic or prophylactic agent for the infectious diseases caused by bacteria and virus that invade via a C5a receptor.
摘要翻译：本发明涉及具有C5a受体拮抗作用的式（1）的酰胺衍生物，其中每个符号如说明书中所定义。上述酰胺衍生物，其光学活性形式和其药学上可接受的盐有望用作治疗或预防由C5a引起的炎症引起的疾病或综合征的药物[例如，自身免疫疾病如风湿病，系统性红斑狼疮败血症，成人呼吸窘迫综合征，慢性阻塞性肺病，哮喘等过敏性疾病，动脉粥样硬化，心肌梗死，脑梗塞，牛皮癣，阿尔茨海默病和严重器官损伤（例如肺炎，肾炎，肝炎和胰腺炎等）由于由缺血再灌注，创伤，烧伤，手术入侵等引起的白细胞的活化]。此外，它们可用作由通过C5a受体侵入的细菌和病毒引起的感染性疾病的治疗或预防剂。

4. 发明申请

US20080194640A1 Optically Active Tetrahydronaphthalene Derivative 审中-公开
标题翻译：光学活性四氢萘衍生物
公开(公告)号：US20080194640A1
公开(公告)日：2008-08-14
申请号：US11883743
申请日：2006-02-07
申请人： Mitsuharu Nakamura , Seigo Ishibuchi , Tatsuyuki Ohtsuka , Hiroshi Sumichika , Sumie Sekiguchi , Takayuki Ishige , Naoko Ueda
发明人： Mitsuharu Nakamura , Seigo Ishibuchi , Tatsuyuki Ohtsuka , Hiroshi Sumichika , Sumie Sekiguchi , Takayuki Ishige , Naoko Ueda
IPC分类号： A61K31/4439 , C07D401/12 , A61P37/00 , A61P11/00 , A61P9/10 , A61P25/28 , A61P17/06 , A61P37/08 , A61P19/02 , A61P31/04 , C07D231/12 , C07D231/14 , A61P29/00
CPC分类号： C07D231/12 , C07D231/14 , C07D401/12
摘要： A compound represented by the following formula (I), a pharmacologically acceptable salt thereof or a hydrate thereof or a solvate thereof, which shows not only a C5a receptor antagonistic activity but also high activity in the biological availability, as compared to its racemate.
摘要翻译：与其外消旋体相比，由下式（I）表示的化合物，其药理学上可接受的盐或其水合物或其溶剂合物，其不仅显示出C5a受体拮抗活性，而且表现出高活性的生物利用度。

5. 发明授权

US6015829A 1-phenylpyrazole compounds and medicinal application thereof 有权
标题翻译： 1-苯基吡唑化合物及其药用
公开(公告)号：US6015829A
公开(公告)日：2000-01-18
申请号：US155155
申请日：1998-09-22
申请人： Seigo Ishibuchi , Hiroshi Morimoto , Atsushi Fukunari , Hiroyoshi Inoue , Yoichi Naka
发明人： Seigo Ishibuchi , Hiroshi Morimoto , Atsushi Fukunari , Hiroyoshi Inoue , Yoichi Naka
IPC分类号： C07D231/14 , A61K31/415 , C07D231/38
CPC分类号： C07D231/14
摘要： 1-Phenylpyrazole compounds of the formula (1): ##STR1## which is exemplified by 5-amino-1-(3-cyano-4-isobutoxyphenyl)pyrazole-4-carboxylic acid, an optical isomer thereof and a pharmaceutically acceptable salt thereof. These compounds have a xanthine oxidase inhibitory activity and are useful as therapeutic agents for diseases such as hyperuricacidemia and gout.
摘要翻译： PCT No.PCT / JP97 / 03840 Sec。 371日期：1998年9月22日 102（e）1998年9月22日PCT 1997年10月22日PCT公布。公开号WO98 / 18765 日期19981年5月7日 - 式（1）的苯基吡唑化合物：其示例为5-氨基-1-（3-氰基-4-异丁氧基苯基）吡唑-4-羧酸，其旋光异构体和药学上可接受的盐其中。这些化合物具有黄嘌呤氧化酶抑制活性，可用作高尿酸血症和痛风等疾病的治疗剂。

6. 发明授权

US07015218B1 Amide compounds and medicinal use thereof 失效
标题翻译：酰胺化合物及其药用
公开(公告)号：US07015218B1
公开(公告)日：2006-03-21
申请号：US09913260
申请日：2000-02-10
申请人： Hiroyuki Ushio , Seigo Ishibuchi , Youichiro Naito , Naoki Sugiyama , Takafumi Kawaguchi , Kenji Chiba , Makio Ohtsuki , Yoichi Naka
发明人： Hiroyuki Ushio , Seigo Ishibuchi , Youichiro Naito , Naoki Sugiyama , Takafumi Kawaguchi , Kenji Chiba , Makio Ohtsuki , Yoichi Naka
IPC分类号： A61K31/541 , A61K31/5375 , A61K31/496 , A61K31/454 , A61K31/4545
CPC分类号： C07D401/12 , A61K31/00 , A61K31/135 , A61K31/40 , A61K45/06 , C07D207/34 , C07D231/14 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D491/10 , A61K2300/00
摘要： The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q is N, CH and the like, W is hydrogen, alkyl, hydroxycarbonylalkyl and the like, X is halogen, cyano, nitro, amino and the like, X′ is hydrogen, halogen, cyano, nitro, and Y is alkyl, hydroxyl group, alkoxy, mercapto and the like and a salt thereof, and a medicine containing the said compound. The compound of the present invention shows a superior inhibitory effect on activated lymphocytes proliferation and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.
摘要翻译：本发明涉及下式化合物其中R 1是取代的芳基，杂芳基等，R 2和R 3是氢烷基，卤素，羟基等，Q是N，CH等，W是氢，烷基，羟基羰基烷基等，X是卤素，氰基，硝基，氨基等，X'是氢，卤素，氰基，硝基，Y是烷基，羟基，烷氧基，巯基等及其盐，以及含有所述化合物的药物。本发明的化合物对活化的淋巴细胞增殖具有优异的抑制作用，可用作预防或治疗各种自身免疫性疾病的药剂。

7. 发明申请

US20110263571A1 NOVEL AMIDE DERIVATIVE AND USE THEREOF AS MEDICINE 有权
标题翻译：新药衍生物及其作为医药使用
公开(公告)号：US20110263571A1
公开(公告)日：2011-10-27
申请号：US13126119
申请日：2009-10-27
申请人： Seigo Ishibuchi , Hidemasa Hikawa , Akiko Tarao , Jun-ichi Endoh , Kunitomo Adachi , Kazuhiro Maeda , Kaoru Tashiro
发明人： Seigo Ishibuchi , Hidemasa Hikawa , Akiko Tarao , Jun-ichi Endoh , Kunitomo Adachi , Kazuhiro Maeda , Kaoru Tashiro
IPC分类号： A61K31/496 , C07D413/10 , A61K31/454 , A61K31/4545 , A61P1/00 , A61K31/497 , C07D417/14 , A61P37/06 , A61P29/00 , C07D413/14 , A61K31/551
CPC分类号： C07D413/14 , A61K31/454 , A61K31/496 , A61K31/551 , C07D263/22 , C07D263/24 , C07D413/10 , C07D413/12
摘要： Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof.
摘要翻译：提供了抑制诱导型MMP（特别是MMP-9）的生产的新型低分子量化合物，而不是止血型MMP-2的产生，以及用于自身免疫性疾病或骨关节炎的预防/治疗药物。由下式（I）表示的酰胺衍生物，其中每个符号如说明书中所定义，其药理学上可接受的盐，或其水合物或溶剂化物。

8. 发明授权

US08354401B2 Oxazolidinone amide aromatic compounds for supressing MMP-9 production 有权
标题翻译：用于抑制MMP-9产生的恶唑烷酮酰胺芳香族化合物
公开(公告)号：US08354401B2
公开(公告)日：2013-01-15
申请号：US13126119
申请日：2009-10-27
申请人： Seigo Ishibuchi , Hidemasa Hikawa , Akiko Tarao , Jun-ichi Endoh , Kunitomo Adachi , Kazuhiro Maeda , Kaoru Tashiro
发明人： Seigo Ishibuchi , Hidemasa Hikawa , Akiko Tarao , Jun-ichi Endoh , Kunitomo Adachi , Kazuhiro Maeda , Kaoru Tashiro
IPC分类号： A01N43/62 , A61K31/55
CPC分类号： C07D413/14 , A61K31/454 , A61K31/496 , A61K31/551 , C07D263/22 , C07D263/24 , C07D413/10 , C07D413/12
摘要： Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof.
摘要翻译：提供了抑制诱导型MMP（特别是MMP-9）的生产的新型低分子量化合物，而不是止血型MMP-2的产生，以及用于自身免疫性疾病或骨关节炎的预防/治疗药物。由下式（I）表示的酰胺衍生物，其中每个符号如说明书中所定义，其药理学上可接受的盐，或其水合物或溶剂化物。

9. 发明申请

US20100041643A1 THIENOTRIAZOLODIAZEPINE COMPOUND AND MEDICINAL USE THEREOF 有权
标题翻译：苯并噻唑啉酮化合物及其药物用途
公开(公告)号：US20100041643A1
公开(公告)日：2010-02-18
申请号：US11916015
申请日：2006-05-30
申请人： Kunitomo Adachi , Hidemasa Hikawa , Maiko Hamada , Jun-ichi Endoh , Seigo Ishibuchi , Naoto Fujie , Minoru Tanaka , Kunio Sugahara , Kouichi Oshita , Meguru Murata
发明人： Kunitomo Adachi , Hidemasa Hikawa , Maiko Hamada , Jun-ichi Endoh , Seigo Ishibuchi , Naoto Fujie , Minoru Tanaka , Kunio Sugahara , Kouichi Oshita , Meguru Murata
IPC分类号： A61K31/551 , C07D495/14
CPC分类号： C07D495/14
摘要： [Solving means] A thienotriazolodiazepine compound of the following formula (I) a pharmaceutical agent containing the compound as an active ingredient, and a production intermediate and a production method of the thienotriazolodiazepine compound. [Effect]Since this compound has an inhibitory action on costimulatory signal from CD28 on T cell, it is useful for the prophylaxis or suppression of rejection reaction in transplantation of organ or bone marrow and the like, and the prophylaxis or treatment of autoimmune diseases or allergic diseases.
摘要翻译： [解决方案]下述式（I）的噻吩并三唑并氮杂化合物是含有该化合物作为有效成分的药剂，以及噻吩并三唑并氮杂化合物的制造中间体和制造方法。 [效果]由于该化合物对T细胞上的CD28的共刺激信号具有抑制作用，因此可用于预防或抑制移植器官或骨髓等中的排斥反应，以及预防或治疗自身免疫性疾病或过敏性疾病

10. 发明授权

US06187774B1 Fused heterocyclic compounds and pharmaceutical applications thereof 失效
标题翻译：稠合杂环化合物及其药物应用
公开(公告)号：US06187774B1
公开(公告)日：2001-02-13
申请号：US09142203
申请日：1998-09-03
申请人： Hiroshi Tanaka , Takanobu Kuroita , Yoshifumi Togo , Seigo Ishibuchi , Masakazu Fujio , Takashi Futamura
发明人： Hiroshi Tanaka , Takanobu Kuroita , Yoshifumi Togo , Seigo Ishibuchi , Masakazu Fujio , Takashi Futamura
IPC分类号： A61K31416
CPC分类号： C07D413/06 , C07D209/14 , C07D231/54 , C07D231/56 , C07D261/20 , C07D401/04 , C07D401/06 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to a fused heterocyclic compound of the formula (I) wherein each symbol is as defined in the specification, an optical isomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing a compound of the formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable additive, and a medicament containing a compound of the formula (I), an optical isomer thereof or a pharmaceutically acceptable salt thereof. The compound of the present invention is a useful antipsychotic agent effective not only for positive symptoms centering on hallucination and delusion characteristic of the acute stage of schizophrenia, but also negative symptoms of apathy, abulia and autism. The inventive compound is expected to make a highly safe antipsychotic agent associated with less side effects, such as extrapyramidal symptoms and endocrine disturbance, which are observed when a conventional antipsychotic agent having a D2 receptor blocking action is administered. Therefore, the inventive compound can be used as a therapeutic agent for the diseases such as schizophrenia.
摘要翻译：本发明涉及式（I）的稠合杂环化合物，其中每个符号如说明书中所定义，其光学异构体，其药学上可接受的盐，含有式（I）化合物的药物组合物，其光学异构体或其药学上可接受的盐和药学上可接受的添加剂，以及含有式（I）化合物，其光学异构体或其药学上可接受的盐的药物。本发明的化合物是一种有效的抗精神病药物，不仅有益于以精神分裂症急性期的幻觉和妄想为特征的阳性症状，而且还有冷漠，厌食和自闭症的阴性症状。预期本发明化合物可以制备与当具有D2受体阻断作用的常规抗精神病药物被施用时观察到的较少副作用（如锥体外系症状和内分泌紊乱）的抗精神病药物。因此，本发明化合物可以用作精神分裂症等疾病的治疗剂。

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