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公开(公告)号:US06826033B2
公开(公告)日:2004-11-30
申请号:US10380627
申请日:2003-03-21
申请人: Minoru Sakurai , Kenichi Washizuka , Hitoshi Hamashima , Yasuyo Tomishima , Masashi Imanishi , Yutaka Nakajima , Hiroaki Ohtake , Satoru Kuroda , Masayoshi Murata , Hiroshi Kayakiri , Naoaki Fujii , Kiyoshi Taniguchi
发明人: Minoru Sakurai , Kenichi Washizuka , Hitoshi Hamashima , Yasuyo Tomishima , Masashi Imanishi , Yutaka Nakajima , Hiroaki Ohtake , Satoru Kuroda , Masayoshi Murata , Hiroshi Kayakiri , Naoaki Fujii , Kiyoshi Taniguchi
IPC分类号: H01G902
CPC分类号: C07D207/416 , C07C233/43 , C07C233/62 , C07C233/80 , C07C235/56 , C07C275/40 , C07C275/42 , C07C275/54 , C07C311/08 , C07C2601/10 , C07C2601/14 , C07C2602/10 , C07D207/34 , C07D209/08 , C07D209/18 , C07D209/40 , C07D209/42 , C07D209/88 , C07D213/40 , C07D213/56 , C07D213/75 , C07D213/81 , C07D213/82 , C07D215/38 , C07D215/40 , C07D215/48 , C07D215/50 , C07D217/22 , C07D217/26 , C07D231/14 , C07D231/56 , C07D233/90 , C07D235/06 , C07D235/08 , C07D235/16 , C07D237/28 , C07D241/20 , C07D241/42 , C07D241/44 , C07D249/08 , C07D261/14 , C07D261/18 , C07D261/20 , C07D263/34 , C07D277/28 , C07D277/56 , C07D295/215 , C07D307/54 , C07D307/66 , C07D307/68 , C07D307/82 , C07D333/36 , C07D333/38 , C07D333/66 , C07D333/70 , C07D487/04 , Y02P20/55
摘要: The present invention relates to a compound formula (I) wherein X1 is bond or —O—CH2—, (II) or (III) R1 is hydrogen or an amino protective group, a is phenyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s), and B is hydrogen; halogen; lower alkyl; lower alkoxycarbonyl; cyclo(lower)alkyl; or a heterocyclic group, naphthyl, 1,2,3,4-tetrahydronaphthyl, benzyl or phenyl, each of which may be substituted with one or two substituent(s), or a salt thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiures or urinary incontinence.
摘要翻译: 本发明涉及其中X 1为键或-O-CH 2 - ,(II)或(III)R 1为氢或氨基保护基的化合物式(I),a为苯基,吲哚基或咔唑基,各自为 可以被一个或两个取代基取代,B是氢; 卤素; 低级烷基 低级烷氧基羰基; 环(低级)烷基; 或杂环基,萘基,1,2,3,4-四氢萘基,苄基或苯基,其各自可以被一个或两个取代基取代,或其盐。 本发明的化合物(I)及其药学上可接受的盐可用于预防和/或治疗感染或尿失禁。
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公开(公告)号:US06348474B1
公开(公告)日:2002-02-19
申请号:US09446110
申请日:2000-02-14
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: A61K31435
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—R2 (I) wherein R1 is alkyl, alkenyl, alkynyl and the like; A is an optionally substituted heteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyl and 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:其中R1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,4,7-二氢苯并咪唑基和2,3-二氢苯并恶嗪基; X是亚烷基,氧杂,氧杂(低级)亚烷基等; 并且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:US06242474B1
公开(公告)日:2001-06-05
申请号:US09446619
申请日:2000-03-21
申请人: Noritsugu Yamasaki , Takafumi Imoto , Takahiro Hiramura , Osamu Onomura , Masahiro Nishikawa , Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada
发明人: Noritsugu Yamasaki , Takafumi Imoto , Takahiro Hiramura , Osamu Onomura , Masahiro Nishikawa , Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada
IPC分类号: A61K314164
CPC分类号: C07D213/78 , C07C311/51 , C07D213/81 , C07D233/64 , C07D233/68 , C07D409/06
摘要: Novel aromatic ring derivatives represented by formula (I) or their pharmaceutical acceptable salts are provided. wherein Nu represents a 5- or 6-membered aromatic ring; ch1 and ch2 each represents a cross-linking group; and A represents an aromatic ring. These compounds have blood sugar-depressing activity or PDE 5 inhibitory activity and are useful as medicines for treating impaired glucose tolerance, diabetes, diabetic complications, syndrome of insulin-resistance, polycystic ovary syndrome, hyperlipidemia, atherosclerosis, cardiovascular disorders, hyperglycemia, hypertension, stenocardia, pulmonary hypertension, congestive heart failure, glomerulopathy, tubulointerstitial disorders, renal failure, angiostenosis, distal angiopathy, cerebral apoplexy, chronic reversible obstructions, autoimmune diseases, allergic rhinitis, urticaria, glaucoma, diseases characterized by enteromotility disorders, impotence, nephritis, cachexia, pancreatitis, restenosis after PTCA, etc.
摘要翻译: 提供由式(I)表示的新颖芳环衍生物或其药学上可接受的盐。其中Nu表示5-或6-元芳环; ch1和ch2各自表示交联基团; 并且A代表芳香环。这些化合物具有抑制血糖的活性或PDE 5抑制活性,可用作治疗糖耐量异常,糖尿病,糖尿病并发症,胰岛素抵抗综合征,多囊卵巢综合症,高脂血症,动脉粥样硬化, 心血管疾病,高血糖症,高血压,心律失常,肺动脉高压,充血性心力衰竭,肾小球病,肾小管间质性疾病,肾衰竭,血管狭窄,远端血管病,脑中风,慢性可逆障碍,自身免疫性疾病,过敏性鼻炎,荨麻疹,青光眼,以肠蠕动为特征的疾病 疾病,阳ence,肾炎,恶病质,胰腺炎,PTCA后再狭窄等。
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公开(公告)号:US06787565B2
公开(公告)日:2004-09-07
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: A61K3134
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: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:US06573274B1
公开(公告)日:2003-06-03
申请号:US09856172
申请日:2001-09-12
申请人: Teruo Oku , Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada , Naoki Ishibashi , Hiroyuki Setoi , Noritsugu Yamasaki , Takafumi Imoto , Takahiro Hiramura
发明人: Teruo Oku , Hiroshi Kayakiri , Yoshito Abe , Hitoshi Hamashima , Hitoshi Sawada , Naoki Ishibashi , Hiroyuki Setoi , Noritsugu Yamasaki , Takafumi Imoto , Takahiro Hiramura
IPC分类号: A61K31437
CPC分类号: C07D471/04
摘要: The present invention relates to a sulfonamide compound of the formula (I): wherein each symbol is as defined in the specification, a salt thereof, and a pharmaceutical composition containing same. This compound can be an effective agent for the prophylaxis and treatment of the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy suppressing action.
摘要翻译: 本发明涉及式(I)的磺酰胺化合物:其中每个符号如说明书中所定义,其盐和含有其的药物组合物。 该化合物可以是用于预防和治疗基于降血糖作用的可治疗疾病的有效试剂,以及基于cGMP-PDE抑制作用,平滑肌松弛作用,支气管扩张作用,血管舒张作用, 平滑肌细胞抑制作用和过敏抑制作用。
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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:US20050171185A1
公开(公告)日:2005-08-04
申请号:US11092398
申请日:2005-03-29
申请人: Noritsugu Yamasaki , Takafumi Imoto , Teruo Oku , Noriko Oku , Chikako Oku , Tomohito Oku , Hiroshi Kayakiri , Osamu Onomura , Takahiro Hiramura
发明人: Noritsugu Yamasaki , Takafumi Imoto , Teruo Oku , Noriko Oku , Chikako Oku , Tomohito Oku , Hiroshi Kayakiri , Osamu Onomura , Takahiro Hiramura
IPC分类号: C07D209/10 , C07D209/12 , C07D405/10 , C07D409/10 , C07D409/12 , A61K31/405 , C07D209/02 , C07D43/02
CPC分类号: C07D405/10 , C07D209/10 , C07D209/12 , C07D409/10 , C07D409/12
摘要: A novel indole derivative or a salt thereof is provided, which is represented by the formula: wherein R1 represents an aryl lower alkyl group, said aryl group may be substituted with one or more groups selected from the group consisting of a halogen atom, an aryl group, a heterocyclic group, an aryl lower alkyl group, an aryl lower alkenyl group, a halo-lower alkyl group, a lower cycloalkyl-lower alkoxy group, a lower cycloalkoxy-lower alkyl group, an aryl lower alkynyl group, an aryloxy lower alkyl group, an aryl lower alkoxy group, a lower alkylthio group, a lower alkoxy group, and an alkenyl group; and R2 represents a lower alkyl group, a lower alkenyl group, an aryl group, or a heterocyclic group, each of which may be substituted with a hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aryl group. The compound of the present invention has blood sugar level-depressing activity and PDE5-inhibiting activity, and is useful as medicine.
摘要翻译: 提供了一种新的吲哚衍生物或其盐,其由下式表示:其中R 1表示芳基低级烷基,所述芳基可以被一个或多个选自下组的基团取代: 由卤素原子,芳基,杂环基,芳基低级烷基,芳基低级烯基,卤代低级烷基,低级环烷基 - 低级烷氧基,低级环烷氧基 - 低级烷基, 芳基低级炔基,芳氧基低级烷基,芳基低级烷氧基,低级烷硫基,低级烷氧基和烯基; R 2表示低级烷基,低级烯基,芳基或杂环基,它们各自可以被氢原子,低级烷基,低级烯基 ,或芳基。 本发明的化合物具有血糖降低活性和PDE5抑制活性,作为药物有用。
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公开(公告)号:US06194396B1
公开(公告)日:2001-02-27
申请号:US09425207
申请日:1999-10-22
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: A61K314184
CPC分类号: C07D209/48 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/16 , C07D235/26 , C07D235/28 , C07D235/30 , C07D263/56 , C07D277/64 , C07D307/79 , C07D307/80 , C07D307/84 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07F7/1804
摘要: This invention relates to a heterocyclic compound of the formula wherein a group of the formula: is a group of the formula X is O, S or N-R5, R1 is lower alkyl, etc., R5 is hydrogen, lower alkyl, etc., R2 is hydrogen, halogen, lower alkyl, etc., R3 is halogen, lower alkyl, etc., R4 is amino optionally having suitable substituent(s), and A is lower alkylene, and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
摘要翻译: 本发明涉及下式的下式的杂环化合物:式X的基团是O,S或N-R 5,R 1是低级烷基等,R 5是氢,低级烷基等,R 2是 氢,卤素,低级烷基等,R 3为卤素,低级烷基等,R 4为任选具有合适取代基的氨基,A为低级亚烷基及其盐,其制备方法为 包含其用于预防和/或治疗缓激肽或其类似物介导的人或动物疾病的药物组合物。
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公开(公告)号:US6083961A
公开(公告)日:2000-07-04
申请号:US776518
申请日:1997-02-03
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: C07D209/48 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/16 , C07D235/26 , C07D235/28 , C07D235/30 , C07D263/56 , C07D277/64 , C07D307/79 , C07D307/80 , C07D307/84 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D498/04 , C07F7/18 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/34 , C07D405/12
CPC分类号: C07D209/48 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/16 , C07D235/26 , C07D235/28 , C07D235/30 , C07D263/56 , C07D277/64 , C07D307/79 , C07D307/80 , C07D307/84 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07F7/1856
摘要: This invention relates to a heterocyclic compound of the formula: ##STR1## wherein a group of the formula: ##STR2## is a group of the formula: ##STR3## etc., X is O, S or N--R.sup.5,R.sup.1 is lower alkyl, etc.,R.sup.5 is hydrogen, lower alkyl, etc.,R.sup.2 is hydrogen, halogen, lower alkyl, etc.,R.sup.3 is halogen, lower alkyl, etc.,R.sup.4 is amino optionally having suitable substituent(s), andA is lower alkylene,and a salt thereof, to processes for preparation thereof, and to a pharmaceutical composition comprising the same for the prevention and/or the treatment of bradykinin or its analogues mediated diseases in human being or animals.
摘要翻译: PCT No.PCT / JP95 / 01478 Sec。 371日期1997年2月3日 102(e)日期1997年2月3日PCT提交1995年7月25日PCT公布。 公开号WO96 / 04251 日本特开1996年2月15日本发明涉及下式的杂环化合物:其中式为下式的基团:X为O,S或N-R 5,R 1为低级烷基等。 R 5为氢,低级烷基等,R 2为氢,卤素,低级烷基等,R 3为卤素,低级烷基等,R 4为任选具有适当取代基的氨基,A为低级亚烷基, 及其盐,其制备方法,以及包含其的药物组合物,用于预防和/或治疗人类或动物中缓激肽或其类似物介导的疾病。
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公开(公告)号:US06420409B1
公开(公告)日:2002-07-16
申请号:US09446749
申请日:2000-03-24
申请人: Noritsugu Yamasaki , Takafumi Imoto , Teruo Oku , Akira Katayama , Hiroshi Kayakiri , Osamu Onomura , Takahiro Hiramura , Masahiro Nishikawa , Hitoshi Sawada
发明人: Noritsugu Yamasaki , Takafumi Imoto , Teruo Oku , Akira Katayama , Hiroshi Kayakiri , Osamu Onomura , Takahiro Hiramura , Masahiro Nishikawa , Hitoshi Sawada
IPC分类号: A61K31415
CPC分类号: C07D401/06 , C07D235/08 , C07D405/10 , C07D409/10 , C07D409/12
摘要: A novel benzimidazole derivative or a salt thereof is provided, which is represented by the formula: wherein R1 represents an alkyl group, etc., R2 represents a substituted or unsubstituted aromatic lower alkyl group, R3 represents an alkyl group, etc., and -X- is represented by the following formula (V): etc. This derivative or a salt thereof is useful as medicine.
摘要翻译: 提供了一种新的苯并咪唑衍生物或其盐,其由下式表示:其中R1表示烷基等,R2表示取代或未取代的芳族低级烷基,R3表示烷基等, X-由下式(V)表示:等。 该衍生物或其盐可用作药物。
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