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公开(公告)号:US06911469B2
公开(公告)日:2005-06-28
申请号:US10047093
申请日:2002-01-17
申请人: Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada , Tsuyoshi Mizutani , Teruo Oku , Noritsugu Yamasaki , Osamu Onomura , Masahiro Nishikawa , Takahiro Hiramura , Takafumi Imoto
发明人: Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada , Tsuyoshi Mizutani , Teruo Oku , Noritsugu Yamasaki , Osamu Onomura , Masahiro Nishikawa , Takahiro Hiramura , Takafumi Imoto
IPC分类号: G06Q50/10 , A61K20060101 , A61K31/381 , A63B69/36 , C07D20060101 , C07D215/48 , C07D231/56 , C07D239/96 , C07D241/52 , C07D249/18 , C07D307/79 , C07D333/54 , C07D333/56 , C07D333/62 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04 , C07F20060101 , A61K31/34
CPC分类号: C07D241/52 , C07D215/48 , C07D231/56 , C07D239/96 , C07D249/18 , C07D307/79 , C07D333/54 , C07D333/62 , C07D405/12 , C07D409/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2 (I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.
摘要翻译: 式(I)的磺酰胺化合物:<?in-line-formula description =“In-line Formulas”end =“lead”→> R sub> 2 SUB > NHCO-AXR 2(I)<?in-line-formula description =“In-line Formulas”end =“tail”?>其中R 1是烷基, 烯基,炔基等; A是任选取代的杂多环基团,除了苯并咪唑基,吲哚基,4,7-二氢苯并咪唑啉-2,3-二氢苯并恶嗪基; X是亚烷基,氧杂,氧杂(低级)亚烷基等; 和R 2是任选取代的芳基,取代的联苯基等,其盐和包含它们的药物组合物。 磺胺类化合物可以基于其血糖降低活性,cGMP-PDE(特别是PDE-V)抑制活性,平滑肌松弛活性,支气管扩张活性,血管舒张活性,平滑肌细胞抑制活性,以及 抗过敏活性。
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公开(公告)号:US20050075342A1
公开(公告)日:2005-04-07
申请号:US10747079
申请日:2003-12-30
申请人: Yoshito Abe , Makoto Inoue , Tsuyoshi Mizutani , Kozo Sawada , Kazuhiko Ohne , Mitsuaki Okumura , Yuki Sawada , Kenichiro Imamura
发明人: Yoshito Abe , Makoto Inoue , Tsuyoshi Mizutani , Kozo Sawada , Kazuhiko Ohne , Mitsuaki Okumura , Yuki Sawada , Kenichiro Imamura
IPC分类号: A61P31/00 , C07D487/04 , A61K31/503
CPC分类号: C07D487/04
摘要: The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-α mediated diseases.
摘要翻译: 本发明涉及式(I)化合物或其盐,其中R 1,R 2,R 3和R 4如说明书中所定义,它们作为药物的用途, 其制备和用途用于治疗PDE-IV或TNF-α介导的疾病。
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公开(公告)号:US6127389A
公开(公告)日:2000-10-03
申请号:US422075
申请日:1999-10-21
申请人: Teruo Oku , Hiroshi Kayakiri , Yoshito Abe , Yuki Sawada , Tsuyoshi Mizutani
发明人: Teruo Oku , Hiroshi Kayakiri , Yoshito Abe , Yuki Sawada , Tsuyoshi Mizutani
IPC分类号: A61K31/4439 , A61K31/4709 , A61P1/00 , A61P1/16 , A61P1/18 , A61P3/10 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P15/00 , A61P15/12 , A61P27/02 , A61P27/06 , A61P43/00 , C07D401/12 , C07D401/14 , C07D409/14 , A61K31/4184 , C07D235/04 , C07D235/06
CPC分类号: C07D401/14 , C07D401/12 , C07D409/14
摘要: This invention relates to compounds of formula: ##STR1## wherein R.sup.6, R.sup.7, R.sup.2, R.sup.2, R.sup.3 and A.sup.1 are as defined in the disclosure; and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of hypertension or the like.
摘要翻译: 本发明涉及下式化合物:其中R6,R7,R2,R2,R3和A1如本公开所定义; 及其药学上可接受的盐,其制备方法,包含其的药物组合物,以及在预防和/或治疗高血压等中治疗性地使用该方法。
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公开(公告)号:US6100284A
公开(公告)日:2000-08-08
申请号:US419684
申请日:1999-10-15
申请人: Teruo Oku , Hiroshi Kayakiri , Yoshito Abe , Yuki Sawada , Tsuyoshi Mizutani
发明人: Teruo Oku , Hiroshi Kayakiri , Yoshito Abe , Yuki Sawada , Tsuyoshi Mizutani
IPC分类号: A61K31/4025 , A61K31/4184 , A61K31/422 , A61K31/437 , A61K31/4439 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/498 , A61K31/517 , A61K31/5377 , A61P29/00 , A61P37/08 , A61P43/00 , C07D215/26 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/04 , C07D521/00 , A61K31/415 , A61K31/495 , C07D235/04 , C07D403/02 , C07D403/10
CPC分类号: C07D231/12 , C07D215/26 , C07D233/56 , C07D249/08 , C07D401/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D471/04
摘要: This invention relates to a compound of the formula: ##STR1## wherein A.sup.1 is lower alkylene,R.sup.1 is substituted quinolyl, etc.,R.sup.2 is hydrogen, halogen or lower alkyl,R.sup.3 is halogen or lower alkyl, andR.sup.4 is a group of the formula:--Q--A.sup.2 --R.sup.5, etc.,in whichR.sup.5 is amino, acylamino, etc.,A.sup.2 is lower alkylene or a single bond, andQ is a group of the formula: ##STR2## etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof, to a pharmaceutical composition comprising the same, and to methods of using the same therapeutically in the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
摘要翻译: 本发明涉及下式化合物:其中A1为低级亚烷基,R1为取代喹啉基等,R2为氢,卤素或低级烷基,R3为卤素或低级烷基,R4为下式基团: Q-A2-R5等,其中R5是氨基,酰氨基等,A2是低级亚烷基或单键,Q是下式的基团及其药学上可接受的盐,用于 制备其包含其的药物组合物,以及在预防和/或治疗缓激肽或其类似物介导的人或动物疾病中的方法。
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公开(公告)号:US5624931A
公开(公告)日:1997-04-29
申请号:US471175
申请日:1995-06-06
申请人: Teruo Oku , Yoshio Kawai , Hiroshi Marusawa , Hitoshi Yamazaki , Yoshito Abe
发明人: Teruo Oku , Yoshio Kawai , Hiroshi Marusawa , Hitoshi Yamazaki , Yoshito Abe
IPC分类号: A61K31/415 , A61K31/505 , A61K31/53 , A61P29/00 , A61P37/00 , A61P43/00 , C07D487/04
CPC分类号: C07D487/04
摘要: Pyrazole derivatives useful for inhibiting the production of Interleukin-1 (IL-1) and tumor necrosis factor (TNF) and the like, which can be represented by the following formula: ##STR1## and a pharmaceutical composition containing the same and to uses thereof.
摘要翻译: 可用于抑制白细胞介素-1(IL-1)和肿瘤坏死因子(TNF)等的产生的吡唑衍生物,其可以由下式表示:其中含有其的药物组合物和 使用它。
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公开(公告)号:US5574042A
公开(公告)日:1996-11-12
申请号:US441786
申请日:1995-05-16
申请人: Teruo Oku , Hiroshi Kayakiri , Shigeki Satoh , Yoshito Abe , Yuki Sawada , Hirokazu Tanaka
发明人: Teruo Oku , Hiroshi Kayakiri , Shigeki Satoh , Yoshito Abe , Yuki Sawada , Hirokazu Tanaka
IPC分类号: C07D471/04 , A61K31/44 , A01N43/42 , C07D471/02
CPC分类号: C07D471/04
摘要: The invention relates to novel bradykinin antagonists of the formula: ##STR1## wherein R.sup.1 is halogen,R.sup.2 and R.sup.3 are each hydrogen, lower alkyl, halo(lower)alkyl or acyl,R.sup.4 is aryl having suitable substituent(s), or a heterocyclic group optionally having suitable substituent(s),Q is O or N--R.sup.11, in which R.sup.11 is hydrogen or acyl, andA is lower alkylene,and pharmaceutically acceptable salts thereof.
摘要翻译: 本发明涉及下式的新型缓激肽拮抗剂:其中R 1为卤素,R 2和R 3各自为氢,低级烷基,卤代(低级)烷基或酰基,R 4为具有合适取代基的芳基或杂环基 基团任选具有合适的取代基,Q是O或N-R11,其中R11是氢或酰基,A是低级亚烷基,及其药学上可接受的盐。
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公开(公告)号:US5563162A
公开(公告)日:1996-10-08
申请号:US233771
申请日:1994-04-26
申请人: Teruo Oku , Hiroshi Kayakiri , Shigeki Satoh , Yoshito Abe , Yuki Sawada , Takayuki Inoue , Hirokazu Tanaka
发明人: Teruo Oku , Hiroshi Kayakiri , Shigeki Satoh , Yoshito Abe , Yuki Sawada , Takayuki Inoue , Hirokazu Tanaka
IPC分类号: A61K31/47 , A61K31/495 , A61K31/498 , A61K31/50 , A61K31/502 , A61K31/505 , A61K31/517 , A61K31/53 , A61P35/00 , A61P37/08 , A61P43/00 , C07D215/24 , C07D215/26 , C07D215/40 , C07D237/10 , C07D237/28 , C07D239/74 , C07D241/42 , C07D241/44 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D413/12 , C07F7/18 , C07D215/02
CPC分类号: C07D401/12 , C07D215/26 , C07D237/28 , C07D239/74 , C07D241/42 , C07D401/14 , C07D403/12 , C07D409/12 , C07D413/12 , C07F7/1856
摘要: This invention relates to new heterocyclic compounds and pharmaceutically acceptable salts thereof. More particularly, this invention relates to new heterocyclic compounds and salts thereof which display bradykinin antagonist activity, to processes for preparing these compounds, to a pharmaceutical composition comprising these compounds, and to methods of using same in the prevention and/or the treatment of bradykinin- or bradykinin analogue-mediated diseases such as allergy, inflammation, autoimmune disease, shock, pain, or the like, in human beings or in animals.
摘要翻译: 本发明涉及新的杂环化合物及其药学上可接受的盐。 更具体地说,本发明涉及向包含这些化合物的药物组合物中显示缓激肽拮抗剂活性的新型杂环化合物及其盐,制备这些化合物的方法,以及用于预防和/或治疗缓激肽的方法 - 或缓激肽类似物介导的疾病,如过敏,炎症,自身免疫性疾病,休克,疼痛等,在人类或动物中。
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