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    Benzofuran derivatives useful in treating diabetic complications
    3.
    发明授权
    Benzofuran derivatives useful in treating diabetic complications 失效
    可用于治疗糖尿病并发症的苯并呋喃衍生物

    公开(公告)号：US4666931A

    公开(公告)日：1987-05-19

    申请号：US814135

    申请日：1985-12-27

    申请人： Yoshitaka Ohishi ,  Michiko Nagahara ,  Norio Kajikawa ,  Motoyuki Yajima ,  Katsumi Nogimori ,  Shigeki Kurokawa

    发明人： Yoshitaka Ohishi ,  Michiko Nagahara ,  Norio Kajikawa ,  Motoyuki Yajima ,  Katsumi Nogimori ,  Shigeki Kurokawa

    IPC分类号： C07D337/00 ,  A61K31/34 ,  A61K31/343 ,  A61K31/36 ,  A61K31/415 ,  A61P3/08 ,  A61P3/10 ,  A61P7/02 ,  C07D307/79 ,  C07D307/80 ,  C07D307/82 ,  C07D307/85 ,  C07D307/86 ,  C07D405/04 ,  C07D493/04

    CPC分类号： C07D307/82 ,  C07D307/80 ,  C07D307/85 ,  C07D307/86 ,  C07D405/04 ,  C07D493/04

    摘要： A benzofuran derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, a benzyl group, unsubstituted or substituted with a halogen atom or an alkyloxy group, or an alkyl group having 1 to 3 carbon atoms, R.sup.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms, R.sup.3 is acetyl group, ethyl group, carboxyl group or 4-methyl-2,5-dioxoimidazolidine-4-yl group, R.sup.4 is hydrogen atom, hydroxyl group, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 9 carbon atoms, carboxymethoxy group, nitro group, acetoamino group, a benzylozy group unsubstituted or substituted with a halogen atom, nitro group or an alkyloxy group or a group having the formula: --OR.sup.6, wherein R.sup.6 is an alkenyl group having 2 to 4 carbon atoms or an alkyl group having 2 to 3 carbon atoms having a halogen atom, cyano group or oxo group, R.sup.5 is hydrogen atom or methylenedioxy group together with R.sup.4 group, n is 1 or 2, and the unsubstituted or substituted N-carboxymethylsulfamoyl group, R.sup.4 and R.sup.5 are attached at 3-position, 4-position, 5-position, 6-position or 7-position of the benzofuran ring, or a nontoxic salt thereof, process for preparing the same and a pharmaceutical composition containing the same.The compounds of the present invention have powerful aldose reductase inhibiting activity, platelet aggregation inhibiting activity and arachidonic acid metabolism inhibiting activity and are useful for a remedy for treatment of diabetic complications.

    摘要翻译： 具有通式（I）的苯并呋喃衍生物：其中R1是氢原子，未被取代或被卤素原子或烷氧基取代的苄基或具有1至3个碳原子的烷基的苄基， R2是氢原子或碳原子数1〜3的烷基，R3是乙酰基，乙基，羧基或4-甲基-2,5-二氧代咪唑烷-4-基，R4是氢原子，羟基， 具有1至6个碳原子的烷基，具有1至9个碳原子的烷氧基，羧甲氧基，硝基，乙酰氨基，未被取代或被卤素原子取代的苄氧基，硝基或烷氧基或具有 式：-OR6，其中R6是具有2至4个碳原子的烯基或具有2至3个碳原子的具有卤素原子的烷基，氰基或氧代基，R5是氢原子或亚甲二氧基以及R4基团， n为1或2，未取代或取代的N-羧甲基氨磺酰基 基团，R4和R5连接在苯并呋喃环的3-位，4-位，5-位，6-位或7-位上，或其无毒盐，其制备方法和含有它们的药物组合物 。 本发明化合物具有强大的醛糖还原酶抑制活性，血小板聚集抑制活性和花生四烯酸代谢抑制活性，可用于治疗糖尿病并发症的治疗方法。

    Azaazulene compounds which are useful as antiallergic and antiinflammatory agents
    4.
    再颁专利
    Azaazulene compounds which are useful as antiallergic and antiinflammatory agents 失效

    公开(公告)号：USRE34918E

    公开(公告)日：1995-04-25

    申请号：US225761

    申请日：1994-04-05

    申请人： Michiko Nagahara ,  Chikara Ieda ,  Mitsuo Mimura ,  Katsuhiro Uchida ,  Soichiro Sato ,  Makoto Okumura

    发明人： Michiko Nagahara ,  Chikara Ieda ,  Mitsuo Mimura ,  Katsuhiro Uchida ,  Soichiro Sato ,  Makoto Okumura

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/41 ,  A61K31/47 ,  A61K31/495 ,  A61P29/00 ,  A61P37/08 ,  C07D209/52 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D409/06 ,  C07D409/14 ,  C07D209/02

    CPC分类号： C07D401/06 ,  C07D209/52 ,  C07D401/14 ,  C07D403/04 ,  C07D409/06 ,  C07D409/14

    摘要： An azaazulene derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom or isopropyl group; the bond C N between C at the 2-position and N at the 1-position is single bond or double bond; when the bond C N is single bond, R.sup.2 is 5-tetrazolyl group, R.sup.3 is taken together with carbon atom to form carbonyl group at the 2-position, and R.sup.4 is hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a lower alkenyl group, a lower alkyl group having oxygen atom or sulfur atom in carbon chain, a lower alkyl group having a halogen atom or cyano group, a lower alkyl group having heteroaromatic ring, a diphenyl lower alkyl group, or a lower alkyl group having hydrocarbon-aromatic ring with the general formula: ##STR2## in which W is single bond or carbonyl group, oxygen atom, sulfur atom or --CH.dbd.CH--, n is an integer of 1 to 6, and R.sup.1', R.sup.2' and R.sup.3' are the same or different and each is hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group, trifluoromethyl group, hydroxyl group, a lower alkoxycarbonyl group, carboxyl group, acetyl group or cyano group; when the bond C N is double bond, N at the 1-position has no substituent R.sup.4, R.sup.2 is cyano group, and R.sup.3 is amino group or a salt thereof, azido group, a diphenyl lower alkyl amino group, a substituted phenyl amino group, a substituted piperazinyl group, a substituted homopiperazinyl group, an amino acid residue bonded by N terminal group in which C terminal group is carboxyl group or a lower alkyl ester thereof, or a lower alkyl amino group which may have an alkyl amino group that may be cyclic one, or a salt thereof, which is useful as an active ingredient of an antiallergic agent and an antiinflammatory agent and has also an inhibitory activity against histamine release, 5-lipoxygenase inhibiting activity, relaxing activity of smooth musculus trachealis and inhibitory activity against carrageenin edema, and further, is useful as medicine for prevention and treatment of bronchial asthma, allergic coryza, allergic conjunctivitis, urticaria, atopic dermatitis, other inflammatory diseases or the like.

    Azaazulene compounds which are useful as antiallergic and antiinflammatory agents
    7.
    发明授权
    Azaazulene compounds which are useful as antiallergic and antiinflammatory agents 失效
    可用作抗过敏和抗炎剂的氮杂薁化合物

    公开(公告)号：US5013736A

    公开(公告)日：1991-05-07

    申请号：US457125

    申请日：1989-12-26

    申请人： Michiko Nagahara ,  Chikara Ieda ,  Mitsuo Mimura ,  Katsuhiro Uchida ,  Soichiro Sato ,  Makoto Okumura

    发明人： Michiko Nagahara ,  Chikara Ieda ,  Mitsuo Mimura ,  Katsuhiro Uchida ,  Soichiro Sato ,  Makoto Okumura

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/41 ,  A61K31/47 ,  A61K31/495 ,  A61P29/00 ,  A61P37/08 ,  C07D209/52 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D409/06 ,  C07D409/14

    CPC分类号： C07D401/06 ,  C07D209/52 ,  C07D401/14 ,  C07D403/04 ,  C07D409/06 ,  C07D409/14

    摘要： An azaazulene derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom or isopropyl group; the bond C N between C at the 2-position and N at the 1-position is single bond or double bond; when the bond C N is single bond, R.sup.2 is 5-tetrazolyl group, R.sup.3 is taken together with carbon atom to form carbonyl group at the 2-position, and R.sup.4 is hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a lower alkenyl group, a lower alkyl group having oxygen atom or sulfur atom in carbon chain, a lower alkyl group having a halogen atom or cyano group, a lower alkyl group having heteroaromatic ring, a diphenyl lower alkyl group, or a lower alkyl group having hydrocarbon-aromatic ring with the general formula: ##STR2## in which W is single bond or carbonyl group, oxygen atom, sulfur atom or --CH.dbd.CH--, n is an integer of 1 to 6, and R.sup.1', R.sup.2' and R.sup.3' are the same or different and each is hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group, trifluoromethyl group, hydroxyl group, a lower alkoxycarbonyl group, carboxyl group, acetyl group or cyano group; when the bond C N is double bond, N at the 1-position has no substituent R.sup.4, R.sup.2 is cyano group, and R.sup.3 is amino group or a salt thereof, azido group, a diphenyl lower alkyl amino group, a substituted phenyl amino group, a substituted piperazinyl group, a substituted homopiperazinyl group, an amino acid residue bonded by N terminal group in which C terminal group is carboxyl group or a lower alkyl ester thereof, or a lower alkyl amino group which may have an alkyl amino group that may be cyclic one, or a salt thereof, which is useful as an active ingredient of an antiallergic agent and an antiinflammatory agent and has also an inhibitory activity against histamine release, 5-lipoxygenase inhibiting activity, relaxing activity of smooth musculus trachealis and inhibitory activity against carrageenin edema, and further, is useful as medicine for prevention and treatment of bronchial asthma, allergic coryza, allergic conjunctivitis, urticaria, atopic dermatitis, other inflammatory diseases or the like.