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1. 发明授权

US4290954A Tetrahydroxanthone derivatives 失效
标题翻译：四氢呫吨酮衍生物
公开(公告)号：US4290954A
公开(公告)日：1981-09-22
申请号：US89403
申请日：1979-10-30
申请人： Kazuhiro Onogi , Hisashi Kunieda , Kiyoshi Kawamura , Masami Shiratsuchi , Masahiko Nagakura , Naoki Machida, deceased , by Takayasu Miwa, heir
发明人： Kazuhiro Onogi , Hisashi Kunieda , Kiyoshi Kawamura , Masami Shiratsuchi , Masahiko Nagakura , Naoki Machida, deceased , by Takayasu Miwa, heir
IPC分类号： A61K31/35 , A61K31/352 , A61K31/41 , A61K31/495 , A61K31/535 , A61P25/04 , A61P29/00 , A61P37/08 , C07D311/86 , C07D405/04 , C07D405/12 , C07D405/10 , C07D413/10
CPC分类号： C07D311/86
摘要： A tetrahydroxanthone derivative represented by the general formula: ##STR1## wherein R is a hydrogen atom, a hydroxyl, cyano, lower alkyl, lower alkoxy, lower acyloxy, benzoyloxy or tetrazolyl group, or ##STR2## (R.sub.3 is a hydrogen atom, R.sub.4 is a hydrogen atom, a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.3 and R.sub.4 commonly form a ring together with the adjacent nitrogen atom and another nitrogen atom or an oxygen atom); R.sub.1 is a hydrogen or halogen atom, a lower alkyl, cyano, carboxyl or tetrazolyl group, or ##STR3## (R.sub.5 is a hydrogen atom, R.sub.6 is a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.5 and R.sub.6 commonly form a ring together with the adjacent nitrogen atom and an oxygen atom); and R.sub.2 is a hydrogen or halogen atom, or a lower alkyl group; with the proviso that neither R nor R.sub.1 is a hydrogen atom; when R is --CONH.sub.2, R.sub.1 and R.sub.2 are not respectively a hydrogen atom nor a hydrogen or halogen atom, or a lower alkyl group; and R.sub.2 and R.sub.1 are not respectively a hydrogen atom nor a halogen atom or a lower alkyl group. Exhibits anti-allergic, anti-inflammatory, analgesic, inhibitory and asthma-treating activities.
摘要翻译：其中R是氢原子，羟基，氰基，低级烷基，低级烷氧基，低级酰氧基，苯甲酰氧基或四唑基，或者是（R 3是氢原子，R 4 是氢原子，可以被任意取代的苯基或四唑基;或者R3和R4通常与相邻的氮原子和另一个氮原子或氧原子一起形成环）; R 1是氢或卤素原子，低级烷基，氰基，羧基或四唑基，或者R 5是氢原子，R 6是任选被取代的苯基或四唑基;或R 5和R 6 通常与相邻的氮原子和氧原子一起形成环）; 并且R 2是氢或卤原子或低级烷基; 条件是R和R1都不是氢原子; 当R为-CONH 2时，R 1和R 2不分别为氢原子或氢或卤素原子或低级烷基; R2和R1不分别为氢原子或卤素原子或低级烷基。展示抗过敏，抗炎，镇痛，抑制和哮喘治疗活动。

2. 发明授权

US4216225A Methylmethioninesulfonium compounds, process for their preparation, and pharmaceutical compositions containing them 失效
标题翻译：甲基亚氨基锍化合物，其制备方法和含有它们的药物组合物
公开(公告)号：US4216225A
公开(公告)日：1980-08-05
申请号：US906567
申请日：1978-05-16
申请人： Masami Shiratsuchi , Kiyoshi Kawamura , Hisashi Kunieda , Naoki Machida , Toshihiro Akashi , Masahiko Nagakura
发明人： Masami Shiratsuchi , Kiyoshi Kawamura , Hisashi Kunieda , Naoki Machida , Toshihiro Akashi , Masahiko Nagakura
IPC分类号： A61K31/195 , A61K31/16 , A61K31/22 , A61P1/04 , C07C67/00 , C07C325/00 , C07C381/12 , C07D213/82 , A61K31/55 , A61K31/215
CPC分类号： C07D213/82
摘要： Methylmethioninesulfonium compounds of the formula ##STR1## wherein X.crclbar. represents an anion;R.sup.1 represents a hydrogen atom or an acyl group of the formula -COR.sup.3 in which R.sup.3 represents an alkyl group with 1 to 20 carbon atoms, the group --CH.sub.2).sub.2 COOH or the group ##STR2## in which Z represents a direct bond or a methylene or vinylene linkage, Y represents C or N, R.sup.4 represents a member selected from the class consisting of a hydrogen atom, lower alkyl groups, lower alkoxy groups, di-lower-alkylamino groups and a sulfamoyl group, n is a number of 1 to 3, and two or more R.sup.4 groups may be identical or different; andR.sup.2 represents the group --COOR.sup.5 in which R.sup.5 represents a hydrogen atom, an alkyl group with 1 to 5 carbon atoms or a metal- or metal complex-forming moiety, or the group ##STR3## in which R.sup.6 groups may be identical or different, and each represent a hydrogen atom or an alkyl group with 1 to 5 carbon atoms, with the proviso that when R.sup.1 represents a hydrogen atom, R.sup.2 is not --COOH; when R.sup.1 represents a hydrogen atom and R.sup.2 represents --CONH.sub.2, X.crclbar. is not Cl.crclbar.; and when R.sup.1 is --COCH.sub.3 and R.sup.2 is --COOCH.sub.3, X.crclbar. is not I.crclbar..The compounds can be easily prepared from methionine as a starting material by a combination of known unit reactions such as methylsulfonium-forming reaction, acylation, amidation, esterification and metal salt-forming reaction. These compounds are especially useful for treating ulcers.
摘要翻译：其中X（ - ）表示阴离子的式“IMAGE”的甲基甲硫氨onium化合物; R 1表示氢原子或式-COR 3的酰基，其中R 3表示具有1至20个碳原子的烷基，基团-CH 2）2 COOH或其中Z表示直接键或基团亚甲基或亚乙烯基，Y表示C或N，R4表示选自氢原子，低级烷基，低级烷氧基，二低级烷基氨基和氨磺酰基的成员，n为1 至3个，并且两个或更多个R 4基团可以相同或不同; 并且R 2表示其中R 5表示氢原子，具有1至5个碳原子的烷基或金属或金属络合物形成部分的基团-COOR 5或其中R6基团可以相同或不同的基团并且各自表示氢原子或具有1至5个碳原子的烷基，条件是当R 1表示氢原子时，R 2不是-COOH; 当R 1表示氢原子且R 2表示-CONH 2时，X（ - ）不是Cl（ - ）; 当R1是-COCH3且R2是-COOCH3时，X（ - ）不是I（ - ）。通过已知的单元反应如甲基锍形成反应，酰化，酰胺化，酯化和金属盐形成反应的组合，可以容易地从甲硫氨酸作为原料制备化合物。这些化合物特别适用于治疗溃疡。

3. 发明授权

US4394382A Dihydrobenzopyran compounds and pharmaceutical composition comprising said compounds 失效
标题翻译：二氢苯并吡喃化合物和包含所述化合物的药物组合物
公开(公告)号：US4394382A
公开(公告)日：1983-07-19
申请号：US271927
申请日：1981-06-09
申请人： Masami Shiratsuchi , Noboru Shimizu , Hiromichi Shigyo , Yoshinori Kyotani , Hisashi Kunieda , Kiyoshi Kawamura , Seiichi Sato , Toshihiro Akashi , Masahiko Nagakura , Naotoshi Sawada , Yasumi Uchida
发明人： Masami Shiratsuchi , Noboru Shimizu , Hiromichi Shigyo , Yoshinori Kyotani , Hisashi Kunieda , Kiyoshi Kawamura , Seiichi Sato , Toshihiro Akashi , Masahiko Nagakura , Naotoshi Sawada , Yasumi Uchida
IPC分类号： C07D311/04 , A61K31/353 , A61P9/02 , A61P9/04 , A61P21/02 , C07D311/22 , C07D311/58 , C07D311/64 , C07D311/66 , A61K31/35
CPC分类号： C07D311/22 , C07D311/58 , C07D311/64 , C07D311/66 , Y10S514/821
摘要： A benzopyran compound represented by the following ##STR1## wherein A represents a direct bond or the bond --CH.sub.2 --O--,R.sub.1 represents a member selected from the group consisting of a C.sub.3 -C.sub.5 alkyl group, a hydroxy-(C.sub.3 -C.sub.5 alkyl) group, a lower alkylamino-lower alkyl group, a nitrato-(C.sub.3 -C.sub.5 alkyl) group and a phenyl-(C.sub.1 -C.sub.5) alkyl group, provided that the phenyl may be substituted by a lower alkoxy group, R.sub.2 represents a member selected from the group consisting of hydrogen, halogen, OH, NO.sub.2, a carbamoyl group, a lower alkyl group, a lower alkoxy group, a lower alkyleneoxy group and acetyl group,R.sub.3 represents hydrogen or NO.sub.2,B represents a direct bond, a C.sub.1 -C.sub.7 alkylene group, a --O-lower alkylene group or a --CONH-lower alkylene group, andn represents 1 or 2;and an acid addition salt thereof and a pharmaceutical composition comprising aforesaid compound.
摘要翻译：由下式（I）表示的苯并吡喃化合物，其中A表示直接键或键-CH2-O-，R1表示选自C3-C5烷基，羟基 - （C3 -C 5烷基）基，低级烷基氨基 - 低级烷基，硝基 - （C 3 -C 5烷基）基和苯基 - （C 1 -C 5）烷基，条件是苯基可以被低级烷氧基取代，R 2 表示选自氢，卤素，OH，NO 2，氨基甲酰基，低级烷基，低级烷氧基，低级亚烷基氧基和乙酰基的成员，R 3表示氢或NO 2，B表示直接键，C 1 -C 7亚烷基，-O-低级亚烷基或-CONH-低级亚烷基，n表示1或2; 及其酸加成盐和包含上述化合物的药物组合物。

4. 发明授权

US4482562A Aromatic aminoethanol compounds, and utilization thereof as cardiovascular agents 失效
标题翻译：芳香族氨基乙醇化合物及其作为心血管药物的用途
公开(公告)号：US4482562A
公开(公告)日：1984-11-13
申请号：US414819
申请日：1982-09-03
申请人： Masami Shiratsuchi , Noboru Shimizu , Hiromichi Shigyo , Yoshinori Kyotani , Hisashi Kunieda , Kiyoshi Kawamura , Seiichi Sato , Toshihiro Akashi , Masahiko Nagakura , Naotoshi Sawada , Yasumi Uchida
发明人： Masami Shiratsuchi , Noboru Shimizu , Hiromichi Shigyo , Yoshinori Kyotani , Hisashi Kunieda , Kiyoshi Kawamura , Seiichi Sato , Toshihiro Akashi , Masahiko Nagakura , Naotoshi Sawada , Yasumi Uchida
IPC分类号： A61K31/21 , A61K31/135 , A61K31/165 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61P9/00 , A61P9/12 , A61P25/02 , A61P25/28 , C07C67/00 , C07C203/04 , C07C213/00 , C07C217/32 , C07C217/70 , C07C219/16 , C07C219/34 , C07C225/16 , C07C231/00 , C07C231/12 , C07C235/42 , C07C235/46 , C07C237/30 , C07C301/00 , C07C303/40 , C07C311/17 , C07C311/29 , C07C313/00 , C07C315/04 , C07C317/22 , C07C317/24 , C07C317/32 , C07C319/20 , C07C323/25 , C07D213/30 , C07D213/60 , C07D213/64 , C07D213/69 , C07D303/24 , C07D303/26 , C07D309/12 , C07D213/74
CPC分类号： C07D213/64 , C07C203/04 , C07D213/69 , C07D303/24 , C07D303/26 , C07D309/12
摘要： A compound represented by the following formula ##STR1## wherein A represents a direct bond or the bond --O--CH.sub.2 --,B represents a C.sub.1 -C.sub.11 alkylene group bonded to a carbon atom of the aromatic ring D either directly or through --O--, --S--, --SO-- or --NH--,W represents a carbon or nitrogen atom,R.sub.1 represents a C.sub.3 -C.sub.7 alkyl group, a hydroxy-C.sub.1 -C.sub.6 alkyl group, or a phenyl- or diphenyl-alkyl group with the alkyl group having 1 to 4 carbon atoms,R.sub.2 represents a member selected from the group consisting of hydrogen, halogen, OH, C.sub.1 -C.sub.4 alkyl, NO.sub.2, C.sub.1 -C.sub.4 alkoxy, acetyl, allyloxy, carbamoyl and sulfamoyl, and when two or more R.sub.2 groups exist, they may be identical or different, andn represents 1, 2 or 3 and m represents 1 or 2, provided that n+m.gtoreq.4;and an acid addition salt thereof; a process for producing the same; and a pharmaceutical composition comprising aforesaid compound.

5. 发明授权

US4374840A Certain phenyl or pyridyl-propanol-amines containing alkyl-nitrate moieties 失效
标题翻译：含有烷基 - 硝酸盐部分的某些苯基或吡啶基 - 丙醇 - 胺
公开(公告)号：US4374840A
公开(公告)日：1983-02-22
申请号：US233643
申请日：1981-02-11
申请人： Masami Shiratsuchi , Noboru Shimizu , Hiromichi Shigyo , Yoshinori Kyotani , Hisashi Kunieda , Kiyoshi Kawamura , Seiichi Sato , Toshihiro Akashi , Masahiko Nagakura , Naotoshi Sawada , Yasumi Uchida
发明人： Masami Shiratsuchi , Noboru Shimizu , Hiromichi Shigyo , Yoshinori Kyotani , Hisashi Kunieda , Kiyoshi Kawamura , Seiichi Sato , Toshihiro Akashi , Masahiko Nagakura , Naotoshi Sawada , Yasumi Uchida
IPC分类号： A61K31/21 , A61K31/135 , A61K31/165 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61P9/00 , A61P9/12 , A61P25/02 , A61P25/28 , C07C67/00 , C07C203/04 , C07C213/00 , C07C217/32 , C07C217/70 , C07C219/16 , C07C219/34 , C07C225/16 , C07C231/00 , C07C231/12 , C07C235/42 , C07C235/46 , C07C237/30 , C07C301/00 , C07C303/40 , C07C311/17 , C07C311/29 , C07C313/00 , C07C315/04 , C07C317/22 , C07C317/24 , C07C317/32 , C07C319/20 , C07C323/25 , C07D213/30 , C07D213/60 , C07D213/64 , C07D213/69 , C07D303/24 , C07D303/26 , C07D309/12 , C07D213/74
CPC分类号： C07D213/64 , C07C203/04 , C07D213/69 , C07D303/24 , C07D303/26 , C07D309/12
摘要： A compound represented by the following formula ##STR1## wherein A represents a direct bond or the bond --0--CH.sub.2--,B represents a C.sub.1 -C.sub.11 alkylene group bonded to a carbon atom of the aromatic ring D either directly or through --O--, --S--, --SO-- or --NH--,W represents a carbon or nitrogen atom,R.sub.1 represents a C.sub.3 -C.sub.7 alkyl group, a hydroxy-C.sub.1 -C.sub.6 alkyl group, or a phenyl- or diphenyl-alkyl group with the alkyl group having 1 to 4 carbon atoms,R.sub.2 represents a member selected from the group consisting of hydrogen, halogen, OH, C.sub.1 -C.sub.4 alkyl, NO.sub.2, C.sub.1 -C.sub.4 alkoxy, acetyl, allyloxy, carbamoyl and sulfamoyl, and when two or more R.sub.2 groups exist, they may be identical or different, andn represents 1, 2 or 3 and m represents 1 or 2, provided that n+m.gtoreq.4;and an acid addition salt thereof; a process for producing the same; and a pharmaceutical composition comprising aforesaid compound.
摘要翻译：由下式表示的化合物：其中A表示直接键或-O-CH 2 - 键，B表示与芳环D的碳原子键合的C1-C11亚烷基直接或-O- ，-S-，-SO-或-NH-，W表示碳原子或氮原子，R1表示C3-C7烷基，羟基-C1-C6烷基或苯基或二苯基 - 烷基，其中具有1至4个碳原子的烷基，R 2表示选自氢，卤素，OH，C 1 -C 4烷基，NO 2，C 1 -C 4烷氧基，乙酰基，烯丙氧基，氨基甲酰基和氨磺酰基的成员，当两个或更多个 R2基团存在，它们可以相同或不同，n表示1,2或3，m表示1或2，条件是n + m> = 4; 及其酸加成盐; 其制造方法; 和包含上述化合物的药物组合物。

6. 发明授权

US4678803A Optical isomers, processes for production thereof and pharmaceutical composition thereof 失效
标题翻译：光学异构体，其制备方法及其药物组合物
公开(公告)号：US4678803A
公开(公告)日：1987-07-07
申请号：US716462
申请日：1985-03-27
申请人： Masami Shiratsuchi , Kiyoshi Kawamura , Toshihiro Akashi , Hiroshi Ishihama , Yasumi Uchida
发明人： Masami Shiratsuchi , Kiyoshi Kawamura , Toshihiro Akashi , Hiroshi Ishihama , Yasumi Uchida
IPC分类号： A61K31/35 , A61K31/352 , A61P9/08 , A61P9/12 , A61P25/02 , C07D303/16 , C07D311/64 , C07D407/12
CPC分类号： C07D407/12 , C07D303/16 , C07D311/64
摘要： An optical isomer selected from the group consisting of (2'R),(3R)-3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2H-1-benzopyran, (2'S),(3R)-3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2H-1-benzopyran and acid addition salts of these isomers, process for producing these isomers and a pharmaceutical composition thereof useful for the treatment of cardiovascular diseases.
摘要翻译：选自（2'R），（3R）-3,4-二氢-8-（2'-羟基-3'-异丙基氨基）丙氧基-3-硝基苯基-2H-1-苯并吡喃的旋光异构体，（2'S），（3R）-3,4-二氢-8-（2'-羟基-3'-异丙氨基）丙氧基-3-硝基xy-2H-1-苯并吡喃和这些异构体的酸加成盐，方法制备这些异构体及其用于治疗心血管疾病的药物组合物。

7. 发明授权

US4727085A Racemates of 3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2H-1-benzo pyran, process for converting them and pharmaceutical compositions thereof 失效
标题翻译： 3,4-二氢-8-（2'-羟基-3'-异丙基氨基）丙氧基-3-硝基氧基-2H-1-苯并吡喃的外消旋体，其转化方法及其药物组合物
公开(公告)号：US4727085A
公开(公告)日：1988-02-23
申请号：US706748
申请日：1985-02-28
申请人： Masami Shiratsuchi , Kiyoshi Kawamura , Toshihiro Akashi , Hiroshi Ishihama , Yasumi Uchida
发明人： Masami Shiratsuchi , Kiyoshi Kawamura , Toshihiro Akashi , Hiroshi Ishihama , Yasumi Uchida
IPC分类号： A61K31/35 , C07D311/64
CPC分类号： A61K31/35 , C07D311/64
摘要： A novel racemate K-351A composed of an optical isomer (2'S),(3S)K-351 [3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2H-1-benzopyran] and (2'R),(3R)K-351, a novel racemate K-351B composed of an optical isomer (2'R),(3S)K-351 and (2'S),(3R)K351 and an acid addition salt of these two novel racemates; a process for converting the two racemates to each other; and also to a pharmaceutical composition comprising each of the two racemates useful for the treatment of cardiovascular diseases.
摘要翻译：由旋光异构体（2'S），（3S）K-351 [3,4-二氢-8-（2'-羟基-3'-异丙氨基）丙氧基-3-硝酰氧基-2H-1 （3S）K-351和（2'S），（3R）K351组成的新型外消旋体K-351B，（3R）K-351 和这两种新型外消旋体的酸加成盐; 将两种消旋体相互转化的过程; 并且还涉及包含用于治疗心血管疾病的两种外消旋体中的每一种的药物组合物。

8. 发明申请

US20140336377A1 ARYLAMIDE DERIVATIVES AS TTX-S BLOCKERS 有权
标题翻译： ARYLAMIDE衍生物作为TTX-S阻挡剂
公开(公告)号：US20140336377A1
公开(公告)日：2014-11-13
申请号：US13879673
申请日：2011-10-18
申请人： Tatsuya Yamagishi , Kiyoshi Kawamura , Yoshimasa Arano , Mikio Morita
发明人： Tatsuya Yamagishi , Kiyoshi Kawamura , Yoshimasa Arano , Mikio Morita
IPC分类号： C07D213/64 , C07D213/75 , C07D239/42 , C07D471/04 , C07D413/12 , C07D413/14 , C07D401/12 , C07D401/14
CPC分类号： C07D213/64 , A61K31/44 , A61K31/4427 , A61K31/444 , A61K31/506 , C07D213/75 , C07D213/81 , C07D239/42 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention relates to arylamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
摘要翻译：本发明涉及具有电压门控钠通道作为TTX-S通道的阻断活性的芳基酰胺衍生物，其可用于治疗或预防涉及电压门控钠通道的疾病和疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及电压门控钠通道的疾病中的用途。

9. 发明申请

US20120094964A1 SULFAMOYL BENZOIC ACID DERIVATIVES AS TRPM8 ANTAGONISTS 审中-公开
标题翻译：磺酰胆碱衍生物作为TRPM8拮抗剂
公开(公告)号：US20120094964A1
公开(公告)日：2012-04-19
申请号：US13318212
申请日：2010-05-06
申请人： Tadashi Inoue , Masashi Ohmi , Kiyoshi Kawamura , Kazuo Ando , Yuji Shishido
发明人： Tadashi Inoue , Masashi Ohmi , Kiyoshi Kawamura , Kazuo Ando , Yuji Shishido
IPC分类号： A61K31/635 , A61K31/18 , A61K31/495 , A61K31/4453 , A61K31/5377 , A61K31/444 , A61K31/4439 , C07D213/76 , C07C311/21 , C07D295/192 , C07D413/12 , C07D401/12 , A61P29/00 , A61P13/00 , A61P19/08 , A61P25/00 , A61P25/06 , A61P9/10 , A61P1/00 , A61P25/22 , A61P25/24 , A61P11/06 , A61P11/00 , A61P9/12 , A61P13/10 , A61P35/00 , A61P13/02 , A61K31/44
CPC分类号： C07C311/21 , A61K31/18 , A61K31/196 , A61K31/44 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4453 , A61K31/4709 , A61K31/495 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07D213/42 , C07D213/75 , C07D295/13 , C07D295/185 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12 , A61K2300/00
摘要： The present invention relates to sulfamoyl benzoic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.
摘要翻译：本发明涉及式（I）的氨磺酰苯甲酸衍生物或其药学上可接受的盐，其制备方法，含有它们的药物组合物及其用于治疗通过TRPM8受体介导的各种病症的用途。

10. 发明授权

US07964727B2 Quinolonecarboxylic acid compounds having 5-HT4 receptor agonistic activity 失效
标题翻译：具有5-HT 4受体激动活性的喹诺酮羧酸化合物
公开(公告)号：US07964727B2
公开(公告)日：2011-06-21
申请号：US10595948
申请日：2004-11-10
申请人： Tomoki Kato , Kiyoshi Kawamura , Mikio Morita , Chikara Uchida
发明人： Tomoki Kato , Kiyoshi Kawamura , Mikio Morita , Chikara Uchida
IPC分类号： C07D221/02 , C07D215/00 , C07D413/00 , A01N43/40 , A01N43/42 , A61K31/435 , A61K31/44
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14 , C07D405/14
摘要： This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α1; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; R1 represents an isopropyl group, a n-propyl group or a cyclopentyl group; R2 represents a methyl group, a fluorine atom or a chlorine atom; R3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1, 2 or 3, or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
摘要翻译：本发明提供式（I）化合物：其中Het表示具有一个氮原子的杂环基团，B直接与该碳原子结合，并且具有4至7个碳原子，所述杂环基团未被取代或被1至4个取代基取代独立地选自取代基α1; A表示具有1至4个碳原子的亚烷基; B表示共价键或具有1至5个碳原子的亚烷基; R1表示异丙基，正丙基或环戊基; R2表示甲基，氟原子或氯原子; R3独立地表示（i）氧代基，羟基，氨基，烷基氨基或羧基; （ii）具有3至8个碳原子的环烷基，所述环烷基被1至5个取代基取代，或（iii）具有3至8个原子的杂环基，所述杂环基未被取代或被1 至5个取代基，n为1,2或3，或其药学上可接受的盐。这些化合物具有5-HT 4受体激动活性，因此可用于治疗哺乳动物特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。

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