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1. 发明申请

US20050080113A1 Medicinal compositions 审中-公开
标题翻译：药用成分
公开(公告)号：US20050080113A1
公开(公告)日：2005-04-14
申请号：US10480551
申请日：2002-06-10
申请人： Shigenori Ohkawa , Ken-ichi Naruo , Shigeru Morimoto , Seiji Miwatashi
发明人： Shigenori Ohkawa , Ken-ichi Naruo , Shigeru Morimoto , Seiji Miwatashi
IPC分类号： A61K31/00 , A61P29/00 , A61P43/00 , C07D417/04 , C07D417/14 , A61K31/426 , A61K31/4439
CPC分类号： C07D417/04 , A61K31/00 , C07D417/14
摘要： The present invention relates to an agent for the prophylaxis or treatment of pain, an agent for suppressing activation of osteoclast, and an inhibitor of osteoclast formation, which contains a p38 MAP kinase inhibitor and/or a TNF-α production inhibitor.
摘要翻译：本发明涉及含有p38 MAP激酶抑制剂和/或TNF-α产生抑制剂的用于预防或治疗疼痛的药剂，用于抑制破骨细胞活化的药剂和破骨细胞形成抑制剂。

2. 发明授权

US07495018B2 Substituted 1,3-thiazole compounds, their production and use 失效
标题翻译：取代的1,3-噻唑化合物，其生产和使用
公开(公告)号：US07495018B2
公开(公告)日：2009-02-24
申请号：US10239692
申请日：2001-03-29
申请人： Shigenori Ohkawa , Ken-ichi Naruo , Seiji Miwatashi , Hiroyuki Kimura
发明人： Shigenori Ohkawa , Ken-ichi Naruo , Seiji Miwatashi , Hiroyuki Kimura
IPC分类号： A61K31/4436 , C07D417/04
CPC分类号： C07D417/04
摘要： (1) A 1,3-thiazole compound of which the 5-position is substituted with a 4-pyridyl group having a substituent including no aromatic group or (2) a 1,3-thiazole compound of which the 5-position is substituted with a pyridyl group having at the position adjacent to a nitrogen atom of the pyridyl group a substituent including no aromatic group has an excellent p38 MAP kinase inhibitory activity.
摘要翻译：（1）5-取代的不具有芳香族基团的取代基的4-吡啶基的1,3-噻唑化合物或（2）取代有5位的1,3-噻唑化合物在与吡啶基的氮原子相邻的位置具有吡啶基的情况下，不含芳香族基团的取代基具有优异的p38MAP激酶抑制活性。

3. 发明申请

US20090048307A1 5-pyridyl-1, 3-azole compounds, process for producing the same and use there of 审中-公开
标题翻译： 5-吡啶基-1,3-唑化合物，其制备方法和用途
公开(公告)号：US20090048307A1
公开(公告)日：2009-02-19
申请号：US11896072
申请日：2007-08-29
申请人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
发明人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
IPC分类号： A61K31/4439 , C07D413/04 , C07D417/04
CPC分类号： C07D417/14 , C07D417/04
摘要： An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.
摘要翻译：由下式表示的任选的N-氧化化合物：其中R1表示氢，烃，杂环，氨基，酰基，R2表示芳族基团，R3表示氢，吡啶基，芳香烃，X表示氧，任选氧化的硫，Y表示键，氧，任选氧化的硫，由式NR4表示的基团（R4表示氢，烃或酰基），Z表示键或二价无环烃或其盐具有优异的腺苷A3受体拮抗活性，并且为用作预防或治疗与腺苷A3受体有关的疾病的药剂。此外，化合物（I）或其盐具有p38 MAP激酶抑制活性和TNF-α抑制活性，并且用作预防或治疗与p38 MAP激酶相关的疾病和与TNF-α相关的疾病的药剂。

4. 发明授权

US06583146B1 Thiazolopyrimidine compounds, its production and use 失效
标题翻译：噻唑并嘧啶化合物，其生产和使用
公开(公告)号：US06583146B1
公开(公告)日：2003-06-24
申请号：US09889139
申请日：2001-07-12
申请人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
发明人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
IPC分类号： A61K31519
CPC分类号： C07D513/04 , A61K31/519
摘要： Compounds represented by general formula (I): and salts thereof, exhibiting excellent adenosine A3 receptor antagonism: wherein A is an optionally substituted benzene ring; B may be further substituted; and R1 is an optionally substituted cyclic group.
摘要翻译：由通式（I）表示的化合物及其盐，显示出优异的腺苷A3受体拮抗作用：其中A为任选取代的苯环; B可以进一步被取代; 并且R 1是任选取代的环状基团。

5. 发明授权

US07276527B2 5-pyridyl-1,3-azole compounds, process for producing the same and use thereof 失效
标题翻译： 5-吡啶基-1,3-唑化合物，其制备方法及其用途
公开(公告)号：US07276527B2
公开(公告)日：2007-10-02
申请号：US11354897
申请日：2006-02-16
申请人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
发明人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
IPC分类号： A61K31/4436 , C07D417/04
CPC分类号： C07D417/14 , C07D417/04
摘要： An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.
摘要翻译：由下式表示的任选的N-氧化化合物：其中R 1表示氢，烃，杂环，氨基，酰基，R 2表示芳族基团， 3表示氢，吡啶基，芳香烃，X表示氧，任选氧化的硫，Y表示键，氧，任选氧化的硫，由式NR 4表示的基团（R 4代表氢，烃或酰基），Z表示键或二价无环烃，或其盐具有优异的腺苷A 3受体拮抗活性，并用作用于预防或治疗与腺苷A 3受体相关的疾病的药剂。此外，化合物（I）或其盐具有p38 MAP激酶抑制活性和TNF-α抑制活性，并且用作预防或治疗与p38 MAP激酶相关的疾病和与TNF-α相关的疾病的药剂。

6. 发明申请

US20060135566A1 5-pyridyl-1,3-azole compounds, process for producing the same and use thereof 失效
标题翻译： 5-吡啶基-1,3-唑化合物，其制备方法及其用途
公开(公告)号：US20060135566A1
公开(公告)日：2006-06-22
申请号：US11354897
申请日：2006-02-16
申请人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
发明人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
IPC分类号： A61K31/4439 , C07D417/04 , C07D413/04
CPC分类号： C07D417/14 , C07D417/04
摘要： An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.
摘要翻译：由下式表示的任选的N-氧化化合物：其中R 1表示氢，烃，杂环，氨基，酰基，R 2表示芳族基团， 3表示氢，吡啶基，芳香烃，X表示氧，任选氧化的硫，Y表示键，氧，任选氧化的硫，由式NR 4表示的基团（R 4代表氢，烃或酰基），Z表示键或二价无环烃，或其盐具有优异的腺苷A 3受体拮抗活性，并用作用于预防或治疗与腺苷A 3受体相关的疾病的药剂。此外，化合物（I）或其盐具有p38 MAP激酶抑制活性和TNF-α抑制活性，并且用作预防或治疗与p38 MAP激酶相关的疾病和与TNF-α相关的疾病的药剂。

7. 发明授权

US07199124B2 JNK inhibitor 失效
标题翻译： JNK抑制剂
公开(公告)号：US07199124B2
公开(公告)日：2007-04-03
申请号：US10470751
申请日：2002-02-01
申请人： Shigenori Ohkawa , Kenichi Naruo , Seiji Miwatashi , Hiroyuki Kimura , Tomohiro Kawamoto
发明人： Shigenori Ohkawa , Kenichi Naruo , Seiji Miwatashi , Hiroyuki Kimura , Tomohiro Kawamoto
IPC分类号： C07D403/04 , A61K31/506 , C07D401/04 , C07D401/14 , A61K31/4439
CPC分类号： C07D417/04 , C07D403/14 , C07D417/14
摘要： The present invention relates to a c-Jun N-terminal kinase inhibitor containing an azole compound (I) substituted by a nitrogen-containing aromatic group having substituent(s)(except a compound represented by the formula: ) or a salt thereof or a prodrug thereof.
摘要翻译：本发明涉及含有被具有取代基的含氮芳香族基团取代的唑类化合物（I）的c-Jun N-末端激酶抑制剂（除了下式所示的化合物：

8. 发明授权

US07101899B1 5-pyridyl-1,3-azole compounds, process for producing the same and use thereof 失效
公开(公告)号：US07101899B1
公开(公告)日：2006-09-05
申请号：US09959356
申请日：2000-04-20
申请人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
发明人： Shigenori Ohkawa , Naoyuki Kanzaki , Seiji Miwatashi
IPC分类号： A61K31/445 , C07D417/04
CPC分类号： C07D417/14 , C07D417/04
摘要： An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.

9. 发明授权

US06962933B1 Method for inhibiting p38 MAP kinase or TNF-α production using a 1,3-thiazole 失效
标题翻译：使用1,3-噻唑抑制p38 MAP激酶或TNF-α产生的方法
公开(公告)号：US06962933B1
公开(公告)日：2005-11-08
申请号：US10048937
申请日：2000-08-03
申请人： Shigenori Ohkawa , Kenichi Naruo , Hiroyuki Kimura , Seiji Miwatashi
发明人： Shigenori Ohkawa , Kenichi Naruo , Hiroyuki Kimura , Seiji Miwatashi
IPC分类号： A61K31/4439 , A61K31/444 , A61P1/04 , A61P3/10 , A61P7/06 , A61P7/08 , A61P9/10 , A61P11/00 , A61P11/06 , A61P19/02 , A61P19/10 , A61P21/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/06 , A61P37/08 , A61P39/02 , A61P43/00 , C07D417/04 , C07D417/14 , A61K31/4421 , A61K31/4436
CPC分类号： C07D417/04 , A61K31/4439 , A61K31/444 , C07D417/14
摘要： A 1,3-thiazole compound substituted at the 5-position by a pyridyl group optionally having substituent(s) has a superior p38 MAP kinase inhibitory activity and TNF-α production inhibitory activity.
摘要翻译：通过任选具有取代基的吡啶基在5位上取代的1,3-噻唑化合物具有优异的p38 MAP激酶抑制活性和TNF-α产生抑制活性。

10. 发明授权

US07750037B2 Antidepressant 失效
标题翻译：抗抑郁药
公开(公告)号：US07750037B2
公开(公告)日：2010-07-06
申请号：US11475539
申请日：2006-06-27
申请人： Shigenori Ohkawa , Masaomi Miyamoto
发明人： Shigenori Ohkawa , Masaomi Miyamoto
IPC分类号： A61K31/4035 , C07D405/02
CPC分类号： C07D405/04 , C07D307/79 , C07D405/12 , C07D409/12 , C07D491/04 , C07D491/10
摘要： A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X: O or S; Y: O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.
摘要翻译：一种PKB（Akt）活化剂，其包含由式（I）表示的化合物：其中R1和R2：H，烃基或杂环基或R1和R2与相邻碳原子一起形成环; R3：H，烃基或杂环基; W：表示由下式表示的基团：其中环A：任选取代的苯环; 环B：任选取代的5-至7-元含氮杂环; R4：被芳基取代并进一步任选取代的脂族烃基或含芳基的酰基; R5：H，C1-6烷基或酰基; R4c：芳基，脂族烃基或酰基; 和X：O或S; Y：O，S或NH; 和环C：任选取代的苯环，或其盐或前药，并且提供了用于预防或治疗抑郁，焦虑，躁狂抑郁性精神病或PTSD的活化剂。

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