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1. 发明申请

US20060111303A1 Diketohydrazine derivative compounds and drugs contaiing the compounds as the active ingredient 失效
标题翻译：二酮肼衍生物化合物和化合物作为活性成分的药物
公开(公告)号：US20060111303A1
公开(公告)日：2006-05-25
申请号：US10512348
申请日：2003-04-24
申请人： Akira Hatayama , Hitoshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
发明人： Akira Hatayama , Hitoshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
IPC分类号： A61K38/04 , C07K5/04
CPC分类号： C07D209/48 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/4152 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/429 , C07C243/34 , C07C251/76 , C07C251/84 , C07C251/86 , C07C2601/08 , C07C2601/14 , C07D207/22 , C07D207/50 , C07D209/46 , C07D211/28 , C07D211/72 , C07D211/86 , C07D211/98 , C07D213/70 , C07D213/76 , C07D213/77 , C07D213/78 , C07D233/38 , C07D233/52 , C07D233/80 , C07D239/10 , C07D239/18 , C07D239/36 , C07D241/08 , C07D241/18 , C07D263/26 , C07D263/28 , C07D265/08 , C07D265/10 , C07D265/33 , C07D275/02 , C07D275/03 , C07D275/06 , C07D277/18 , C07D277/36 , C07D277/50 , C07D277/54 , C07D277/60 , C07D277/82 , C07D279/02 , C07D279/06 , C07D279/12 , C07D285/10 , C07D285/16 , C07D309/04 , C07D309/28 , C07D335/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D513/10 , C07F9/59 , C07F9/65583 , Y02A50/411
摘要： The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
摘要翻译：本发明涉及式（I）的二酮肼衍生物及其药学上可接受的盐（式中的符号具有与说明书中所述相同的含义）。式（I）化合物对半胱氨酸蛋白酶具有抑制活性，可用于治疗炎性疾病，免疫疾病，缺血性疾病，呼吸系统疾病，循环系统疾病，血液病，神经元疾病，肝或胆道疾病，骨质或关节疾病，代谢疾病等。该化合物对弹性蛋白酶具有抑制活性，也可用于治疗慢性阻塞性肺疾病（慢性障碍性肺疾病）。

2. 发明授权

US07655804B2 Diketohydrazine derivative compounds and drugs containing the compounds as the active ingredient 失效
标题翻译：二酮肼衍生物化合物和含有这些化合物作为活性成分的药物
公开(公告)号：US07655804B2
公开(公告)日：2010-02-02
申请号：US10512348
申请日：2003-04-24
申请人： Akira Hatayama , Hiroshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
发明人： Akira Hatayama , Hiroshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
IPC分类号： C07D417/12
CPC分类号： C07D209/48 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/4152 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/429 , C07C243/34 , C07C251/76 , C07C251/84 , C07C251/86 , C07C2601/08 , C07C2601/14 , C07D207/22 , C07D207/50 , C07D209/46 , C07D211/28 , C07D211/72 , C07D211/86 , C07D211/98 , C07D213/70 , C07D213/76 , C07D213/77 , C07D213/78 , C07D233/38 , C07D233/52 , C07D233/80 , C07D239/10 , C07D239/18 , C07D239/36 , C07D241/08 , C07D241/18 , C07D263/26 , C07D263/28 , C07D265/08 , C07D265/10 , C07D265/33 , C07D275/02 , C07D275/03 , C07D275/06 , C07D277/18 , C07D277/36 , C07D277/50 , C07D277/54 , C07D277/60 , C07D277/82 , C07D279/02 , C07D279/06 , C07D279/12 , C07D285/10 , C07D285/16 , C07D309/04 , C07D309/28 , C07D335/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D513/10 , C07F9/59 , C07F9/65583 , Y02A50/411
摘要： The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
摘要翻译：本发明涉及式（I）的二酮肼衍生物及其药学上可接受的盐（式中的符号具有与说明书中所述相同的含义）。式（I）化合物对半胱氨酸蛋白酶具有抑制活性，可用于治疗炎性疾病，免疫疾病，缺血性疾病，呼吸系统疾病，循环系统疾病，血液病，神经元疾病，肝或胆道疾病，骨质或关节疾病，代谢疾病等。该化合物对弹性蛋白酶具有抑制活性，也可用于治疗慢性阻塞性肺疾病（慢性障碍性肺疾病）。

3. 发明授权

US08138182B2 Diketohydrazine derivative compounds and drugs containing the compounds as the active ingredient 失效
标题翻译：二酮肼衍生物化合物和含有这些化合物作为活性成分的药物
公开(公告)号：US08138182B2
公开(公告)日：2012-03-20
申请号：US12566416
申请日：2009-09-24
申请人： Akira Hatayama , Hiroshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
发明人： Akira Hatayama , Hiroshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
IPC分类号： C07D207/22 , C07D233/32 , C07D263/20 , C07D265/33 , C07D403/12 , C07D413/12 , C07D417/12
CPC分类号： C07D209/48 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/4152 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/429 , C07C243/34 , C07C251/76 , C07C251/84 , C07C251/86 , C07C2601/08 , C07C2601/14 , C07D207/22 , C07D207/50 , C07D209/46 , C07D211/28 , C07D211/72 , C07D211/86 , C07D211/98 , C07D213/70 , C07D213/76 , C07D213/77 , C07D213/78 , C07D233/38 , C07D233/52 , C07D233/80 , C07D239/10 , C07D239/18 , C07D239/36 , C07D241/08 , C07D241/18 , C07D263/26 , C07D263/28 , C07D265/08 , C07D265/10 , C07D265/33 , C07D275/02 , C07D275/03 , C07D275/06 , C07D277/18 , C07D277/36 , C07D277/50 , C07D277/54 , C07D277/60 , C07D277/82 , C07D279/02 , C07D279/06 , C07D279/12 , C07D285/10 , C07D285/16 , C07D309/04 , C07D309/28 , C07D335/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D513/10 , C07F9/59 , C07F9/65583 , Y02A50/411
摘要： The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
摘要翻译：本发明涉及式（I）的二酮肼衍生物及其药学上可接受的盐（式中的符号具有与说明书中所述相同的含义）。式（I）化合物对半胱氨酸蛋白酶具有抑制活性，可用于治疗炎性疾病，免疫疾病，缺血性疾病，呼吸系统疾病，循环系统疾病，血液病，神经元疾病，肝或胆道疾病，骨质或关节疾病，代谢疾病等。该化合物对弹性蛋白酶具有抑制活性，也可用于治疗慢性阻塞性肺疾病（慢性障碍性肺疾病）。

4. 发明申请

US20100087442A1 DIKETOHYDRAZINE DERIVATIVE COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS AS THE ACTIVE INGREDIENT 失效
标题翻译：化合物衍生化合物和含有化合物作为活性成分的药物
公开(公告)号：US20100087442A1
公开(公告)日：2010-04-08
申请号：US12566416
申请日：2009-09-24
申请人： Akira Hatayama , Hiroshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
发明人： Akira Hatayama , Hiroshi Tsuruta , Yasuo Ochi , Haruo Imawaka , Kazuyuki Ohmoto
IPC分类号： A61K31/501 , C07D417/12 , C07D277/18 , C07D413/12 , C07D233/32 , C07D275/02 , C07D405/06 , A61K31/427 , A61K31/421 , A61K31/4164 , A61K31/425 , A61P35/00 , A61P19/00
CPC分类号： C07D209/48 , A61K31/16 , A61K31/165 , A61K31/341 , A61K31/351 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/4152 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/429 , C07C243/34 , C07C251/76 , C07C251/84 , C07C251/86 , C07C2601/08 , C07C2601/14 , C07D207/22 , C07D207/50 , C07D209/46 , C07D211/28 , C07D211/72 , C07D211/86 , C07D211/98 , C07D213/70 , C07D213/76 , C07D213/77 , C07D213/78 , C07D233/38 , C07D233/52 , C07D233/80 , C07D239/10 , C07D239/18 , C07D239/36 , C07D241/08 , C07D241/18 , C07D263/26 , C07D263/28 , C07D265/08 , C07D265/10 , C07D265/33 , C07D275/02 , C07D275/03 , C07D275/06 , C07D277/18 , C07D277/36 , C07D277/50 , C07D277/54 , C07D277/60 , C07D277/82 , C07D279/02 , C07D279/06 , C07D279/12 , C07D285/10 , C07D285/16 , C07D309/04 , C07D309/28 , C07D335/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D513/10 , C07F9/59 , C07F9/65583 , Y02A50/411
摘要： The present invention relates to a diketohydrazine derivative of formula (I) and a pharmaceutically acceptable salt thereof (the symbols in the formula have the same meaning as described in the specification). The compound of formula (I) has an inhibitory activity against cysteine protease, and it is useful for the treatment of inflammatory diseases, immune diseases, ischemic diseases, respiratory diseases, circulatory diseases, blood diseases, neuronal diseases, hepatic or biliary diseases, osseous or articular diseases, metabolic diseases, etc. And the compound has inhibitory activity against elastase and it is also useful for the treatment of COPD (chronic obstacle pulmonary diseases).
摘要翻译：本发明涉及式（I）的二酮肼衍生物及其药学上可接受的盐（式中的符号具有与说明书中所述相同的含义）。式（I）化合物对半胱氨酸蛋白酶具有抑制活性，可用于治疗炎性疾病，免疫疾病，缺血性疾病，呼吸系统疾病，循环系统疾病，血液病，神经元疾病，肝或胆道疾病，骨质或关节疾病，代谢疾病等。该化合物对弹性蛋白酶具有抑制活性，也可用于治疗慢性阻塞性肺疾病（慢性障碍性肺疾病）。

5. 发明申请

US20070232586A1 Hydrazino-Substituted Heterocyclic Nitrile Compounds and Use Thereof 审中-公开
标题翻译：肼基取代的杂环腈化合物及其用途
公开(公告)号：US20070232586A1
公开(公告)日：2007-10-04
申请号：US11587309
申请日：2005-04-20
申请人： Kazuyuki Ohmoto , Akira Hatayama , Katsuya Hisaichi , Makoto Tanaka , Hiroyuki Yamada
发明人： Kazuyuki Ohmoto , Akira Hatayama , Katsuya Hisaichi , Makoto Tanaka , Hiroyuki Yamada
IPC分类号： A61K31/421 , A61K31/426 , A61K31/505 , A61K31/506 , A61K31/53 , C07D239/48 , C07D263/48 , C07D277/20
CPC分类号： C07D487/04 , A61K31/421 , A61K31/426 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/53 , C07D239/42 , C07D239/48 , C07D239/70 , C07D491/048 , Y02A50/411
摘要： A compound having an inhibitory activity against cysteine protease, represented by formula (I): (wherein ring X is a heterocyclic group which may contain 1 to 4 hetero atoms selected from an nitrogen atom(s), a oxygen atom(s) and a sulfur atom(s) which may be oxidized, in addition to said nitrogen atom in the ring; J is a bond or a spacer having from 1 to 8 atoms; R, R1, R2 and R3 is each independently hydrogen atom or a substituent; n is 0 or an integer of 1 to 10), a salt thereof, a solvate thereof, or an N-oxide thereof, or a prodrug thereof; and an agent for prevention and/or treatment for a cysteine protease-related disease, such as osteoporosis, comprising it as an active ingredient are provided.
摘要翻译：由式（I）表示的具有对半胱氨酸蛋白酶的抑制活性的化合物：其中，环X是可以含有1〜4个选自氮原子，氧原子和除了环中的所述氮原子之外，可以被氧化的硫原子; J是具有1至8个原子的键或间隔基; R 1，R 1，R 2， 2和R 3各自独立地为氢原子或取代基; n为0或1〜10的整数），其盐，其溶剂合物或其N-氧化物，或其前药; 并提供了包含其作为活性成分的半胱氨酸蛋白酶相关疾病如骨质疏松症的预防和/或治疗药剂。

6. 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。

7. 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）。

8. 发明授权

US07964726B2 Tricyclic compound and use thereof 有权
标题翻译：三环化合物及其用途
公开(公告)号：US07964726B2
公开(公告)日：2011-06-21
申请号：US11722623
申请日：2005-12-21
申请人： Kazuyuki Ohmoto , Masashi Kato , Yoshifumi Kagamiishi , Junichiro Manako
发明人： Kazuyuki Ohmoto , Masashi Kato , Yoshifumi Kagamiishi , Junichiro Manako
IPC分类号： C07D401/04 , C07D221/06 , C07D221/20 , A61K31/4355 , A61K31/438
CPC分类号： C07D471/14 , A61K31/4375 , A61K31/438 , A61K45/06 , C07D471/04 , C07D471/10
摘要： The present invention relates to the compound represented by formula (I): (wherein, all the symbols has the same meanings as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.
摘要翻译：本发明涉及由式（I）表示的化合物：其中所有符号与说明书的含义相同），其盐，其溶剂合物或其前药。由于本发明的化合物具有抗应激作用，因此可用于由应激引起的疾病的预防和/或治疗剂，特别是由应激引起的消化系统疾病，优于口服吸收。

9. 发明申请

US20070060595A1 Novel fused heterocyclic compound and use thereof 审中-公开
标题翻译：新型稠合杂环化合物及其用途
公开(公告)号：US20070060595A1
公开(公告)日：2007-03-15
申请号：US10575350
申请日：2004-10-08
申请人： Toshio Yoshizawa , Koji Ogawa , Setsuko Fujita , Takeo Inohara , Kazuyuki Ohmoto
发明人： Toshio Yoshizawa , Koji Ogawa , Setsuko Fujita , Takeo Inohara , Kazuyuki Ohmoto
IPC分类号： A61K31/519 , A61K31/47 , A61K31/366 , C07D487/04 , C07D311/02 , C07D215/38
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： The compound represented by the general formula (I): wherein, a fused ring AB represents a 5- to 10-membered fused heterocyclic ring; R1 represents (1) a hydrogen atom, (2) a halogen atom, (3) a cyano group, (4) an oxo group, (5) an optionally protected hydroxyl group, (6) an optionally protected carboxyl group, (7) an optionally protected amino group, (8) a cyclic group which may have a substituent (s), (9) an aliphatic hydrocarbon group which may have a substituent (s), or (10) an optionally protected thiol group; n represents 0 or an integer of 1 to 8; provided that n represents an integer of not less than 2, plural R1 are the same or different; a salt thereof, a solvate thereof or a prodrug thereof has a kinase (especially c-Jun N-terminal kinase) inhibitory activity and an inhibitory activity of a function of AP-1 as a transcription factor, it is useful as a preventive and/or therapeutic agent for a for example, a diabetes of metabolic disease, etc., a rheumatoid arthritis of inflammatory, etc.
摘要翻译：由通式（I）表示的化合物：其中稠环AB表示5-至10-元稠合杂环; R 1表示（1）氢原子，（2）卤素原子，（3）氰基，（4）氧代基，（5）任意保护的羟基，（6）任选保护的羧基，（7）任选保护的氨基，（8）可具有取代基的环状基团，（9）可具有取代基的脂族烃基，或（10）任选保护的硫醇基; n表示0或1〜8的整数，条件是n表示不小于2的整数，多个R 1相同或不同; 其盐，其溶剂合物或其前药具有激酶（特别是c-Jun N-末端激酶）抑制活性和AP-1作为转录因子的功能的抑制活性，可用作预防和/ 或治疗剂，例如代谢疾病的糖尿病等，炎症的类风湿性关节炎等

10. 发明授权

US08476293B2 Tricyclic compound and use thereof 失效
公开(公告)号：US08476293B2
公开(公告)日：2013-07-02
申请号：US13097741
申请日：2011-04-29
申请人： Kazuyuki Ohmoto , Masashi Kato , Yoshifumi Kagamiishi , Junichiro Manako
发明人： Kazuyuki Ohmoto , Masashi Kato , Yoshifumi Kagamiishi , Junichiro Manako
IPC分类号： A61K31/438 , C07D401/04
CPC分类号： C07D471/14 , A61K31/4375 , A61K31/438 , A61K45/06 , C07D471/04 , C07D471/10
摘要： The present invention relates to the compound represented by formula (I): (wherein, all the symbols have the same meaning as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.

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