Naphthyloxyacetic acid derivatives
    1.
    发明授权
    Naphthyloxyacetic acid derivatives 失效
    萘氧基乙酸衍生物

    公开(公告)号:US5753700A

    公开(公告)日:1998-05-19

    申请号:US574133

    申请日:1995-12-18

    摘要: A naphthyloxyacetic acid derivative of the formula (I) ##STR1## wherein R.sup.1 is H, alkyl, alkylene-(--COOR.sup.10, --OH, --CONR.sup.4 R.sup.5, --CONR.sup.6 -alkylene-OH, --NR.sup.4 R.sup.5, -cyano or -tetrazolyl); A is single bond, alkylene, alkenylene, --S-alkylene, --O-alkylene; B is NR.sup.3 CO, CONR.sup.3 ; R.sup.2 is (1) alkyl (2) alkenyl, (3) alkyl or alkenyl substituted by 1-3 of phenyl, cycloalkyl, naphthyl and heterocyclic ring containing nitrogen atom (the said ring may be substituted by 1-3 of alkyl, alkoxy and halogen etc.), (4) NR.sup.7 R.sup.8 or (5) alkylene-NR.sup.7 R.sup.8 ; non-toxic salt thereof, non-toxic acid addition salt thereof and hydrate thereof can bind the PGE.sub.2 receptor and exhibits the activity to antagonize or agonize for PGE.sub.2, therefore, they are useful as PGE.sub.2 antagonist or PGE.sub.2 agonist.

    摘要翻译: (I)的萘氧基乙酸衍生物其中R 1为H,烷基,亚烷基 - ( - COOR 10,-OH,-CONR 4 R 5,-CONR 6 - 亚烷基-OH,-NR 4 R 5 - 氰基或四唑基 ); A是单键,亚烷基,亚烯基,-S-亚烷基,-O-亚烷基; B为NR3CO,CONR3; R2是(1)烷基(2)烯基,(3)被1-3个含氮原子的苯基,环烷基,萘基和杂环取代的烷基或链烯基(所述环可以被1-3个烷基,烷氧基和 卤素等),(4)NR7R8或(5)亚烷基-NR7R8; 其无毒盐,其无毒酸加成盐和其水合物可结合PGE2受体并表现出拮抗或激动PGE2的活性,因此它们可用作PGE2拮抗剂或PGE2激动剂。

    Naphthyloxy acetic acid derivatives and a pharmaceutical composition comprising them as an active ingredient
    2.
    发明授权
    Naphthyloxy acetic acid derivatives and a pharmaceutical composition comprising them as an active ingredient 失效
    萘氧基乙酸衍生物和包含它们作为活性成分的药物组合物

    公开(公告)号:US06335366B2

    公开(公告)日:2002-01-01

    申请号:US09765676

    申请日:2001-01-22

    IPC分类号: A61K31185

    摘要: The naphthyloxyacetic acid derivatives of the formula (I) wherein A is H, -(alkylene)COOR1, -(alkylene)CONR2R3, -(alkylene)OH, -(alkylene)tetrazole, -(alkylene)CN; E is single bond or alkylene; G is —S—, —SO—, —SO2—, —O— or —NR4—; L is alkylene, —(CH2)m—CH═CH—(CH2)n— or —(CH2)x—CH(OH)—(CH2)y—; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE2 receptor and exhibit the activity to antagonize or agonize for PGE2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.

    摘要翻译: 式(I)的萘氧基乙酸衍生物,其中A是H, - (亚烷基)COOR1, - (亚烷基)CONR2R3, - (亚烷基)OH, - (亚烷基)四唑, - (亚烷基) E是单键或亚烷基; G是-S - , - SO - , - SO 2 - , - O-或-NR 4 - 。 L是亚烷基, - (CH 2)m -CH = CH-(CH 2)n - 或 - (CH 2)x -CH(OH) - (CH 2)y - M是苯基,苯基(硫代,氧基,氨基),二苯基甲基,二苯基甲基(硫代,氧基,氨基),以及包含它们作为活性成分的药物组合物。 式(I)化合物可以组合PGE 2受体并表现出拮抗或激动PGE2受体的活性。 因此,它们可用作抗高血脂,防止流产,镇痛药,止泻药,睡眠诱导剂,利尿剂,抗糖尿病,止痛药,通气药,抗溃疡药,抗胃炎或抗高血压药等。

    Naphthyloxy acetic acid derivatives
    3.
    发明授权
    Naphthyloxy acetic acid derivatives 失效
    萘氧基乙酸衍生物

    公开(公告)号:US6013673A

    公开(公告)日:2000-01-11

    申请号:US12448

    申请日:1998-01-23

    摘要: A naphthyloxyacetic acid derivative of the formula (I) ##STR1## wherein R.sup.1 is H, alkyl, alkylene-(--COOR.sup.10, --OH, --CONR.sup.4 R.sup.5, --CONR.sup.6 -alkylene-OH, --NR.sup.4 R.sup.5, -cyano or -tetrazolyl); A is single bond, alkylene, alkenylene, --S-alkylene, --O-alkylene; B is NR.sup.3 CO, CONR.sup.3 ; R.sup.2 is (1) alkyl (2) alkenyl, (3) alkyl or alkenyl substituted by 1-3 of phenyl, cycloalkyl, naphthyl and heterocyclic ring containing nitrogen atom (the said ring may be substituted by 1-3 of alkyl, alkoxy and halogen etc.), (4) NR.sup.7 R.sup.8 or (5) alkylene-NR.sup.7 R.sup.8 ; non-toxic salt thereof, non-toxic acid addition salt thereof and hydrate thereof can bind the PGE.sub.2 receptor and exhibits the activity to antagonize or agonize for PGE.sub.2., therefore, they are useful as PGE.sub.2 antagonist or PGE.sub.2 agonist.

    摘要翻译: 其中R 1为H,烷基,亚烷基 - ( - COOR 10,-OH,-CONR 4 R 5,-CONR 6 - 亚烷基-OH,-NR 4 R 5 - 氰基或四唑基)的式(I)的萘氧基乙酸衍生物; A是单键,亚烷基,亚烯基,-S-亚烷基,-O-亚烷基; B为NR3CO,CONR3; R2是(1)烷基(2)烯基,(3)被1-3个含氮原子的苯基,环烷基,萘基和杂环取代的烷基或链烯基(所述环可以被1-3个烷基,烷氧基和 卤素等),(4)NR7R8或(5)亚烷基-NR7R8; 其无毒盐,无毒性酸加成盐和其水合物可结合PGE2受体并表现出拮抗或激动PGE2的活性,因此它们可用作PGE2拮抗剂或PGE2激动剂。

    Naphthyloxyacetic acid
    4.
    发明授权
    Naphthyloxyacetic acid 失效
    萘氧基乙酸

    公开(公告)号:US5624959A

    公开(公告)日:1997-04-29

    申请号:US355187

    申请日:1994-12-08

    摘要: (1) Naphthyloxyaetic acid represented by the compound of the formula (I): ##STR1## and non-toxic salts thereof, (2) process for the preparation of the compounds represented by the compound of the formula (I) described hereinbefore,(3) PGE.sub.2 antagonist or agonist containing the compound represented by the compound of the formula (I) as the active ingredient.The compounds represented by the compounds of the formula (I) can be adapted to medicines which possess an inhibitory effect of uterine contraction, an analgesic action, an inhibitory effect of digestive peristalsis, a sleep-inducing effect as PGE.sub.2 antagonists, and an uterine contractile activity, a promoting effect of digestive peristalsis, a suppressive effect of gastric acid secretion, hypotensive activity as PGE.sub.2 agonists. The compounds bind to PGE.sub.2 receptor and have an activity of antagonist or agonist against the action thereof.

    摘要翻译: (1)由式(I)的化合物代表的萘乙酸:其中,(I)化合物及其无毒盐,(2)由上述式(I)的化合物表示的化合物的制备方法, (3)PGE2拮抗剂或含有式(I)化合物所代表的化合物作为活性成分的激动剂。 由式(I)化合物表示的化合物可以适用于具有子宫收缩抑制作用,止痛作用,消化性蠕动抑制作用,睡眠诱导作用PGE2拮抗剂和子宫收缩的药物 活动,消化性蠕动的促进作用,胃酸分泌的抑制作用,作为PGE2激动剂的降血压活性。 该化合物与PGE2受体结合,并具有拮抗剂或激动剂抵抗其作用的活性。

    Sulfonamide and carboxamide derivatives and drugs containing the same as the active ingredient
    5.
    发明授权
    Sulfonamide and carboxamide derivatives and drugs containing the same as the active ingredient 有权
    磺酰胺和甲酰胺衍生物以及含有与活性成分相同的药物

    公开(公告)号:US06448290B1

    公开(公告)日:2002-09-10

    申请号:US09331327

    申请日:1999-06-18

    IPC分类号: A61K3144

    摘要: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.

    摘要翻译: 式(I)的磺酰胺或氨基酰胺衍生物和包含它们作为活性成分的药物组合物:其中A环,B环为碳环,杂环; Z1为-COR1,-CH = CH-COR1等。 Z2是H,烷基等; Z3是单键,亚烷基; Z4是SO2,CO; Z5是烷基,苯基,杂环等; R2是CONR8,O,S,NZ6,Z7-亚烷基,亚烷基等。 ; R3是H,烷基,卤素,CF3等; R4是H,(取代的)烷基等; n,t是1-4)。式(I)化合物可以与PGE2的受体结合, 针对其作用或激动活性的活性。 因此,它们被认为可用作抑制子宫收缩,止痛剂,止泻药,睡眠诱导剂,用于增加膀胱能力的药物或用于子宫收缩的药物,通气,抑制胃酸分泌,抗高血压药或利尿剂的药物。

    Naphthyloxyacetic acid derivatives and a pharmaceutical composition comprising them as an active ingredient
    6.
    发明授权
    Naphthyloxyacetic acid derivatives and a pharmaceutical composition comprising them as an active ingredient 失效
    萘氧基乙酸衍生物和包含它们的药物组合物作为活性成分

    公开(公告)号:US06197993B1

    公开(公告)日:2001-03-06

    申请号:US09440674

    申请日:1999-11-16

    IPC分类号: C07C25500

    摘要: The naphthyloxyacetic acid derivatives of the formula (I) wherein A is H, -(alkylene)COOR1, -(alkylene)CONR2R3, -(alkylene)OH, -(alkylene)tetrazole, -(alkylene)CN; E is single bond or alkylene; G is —S—, —SO—, —SO2—, —O— or —NR4—; L is alkylene, —(CH2)m—CH═CH—(CH2)n— or —(CH2)x—CH(OH)— (CH2)y—; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE2 receptor and exhibit the activity to antagonize or agonize for PGE2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.

    摘要翻译: 式(I)的萘氧基乙酸衍生物,其中A是H, - (亚烷基)COOR1, - (亚烷基)CONR2R3, - (亚烷基)OH, - (亚烷基)四唑, - (亚烷基) E是单键或亚烷基; G是-S - , - SO - , - SO 2 - , - O-或-NR 4 - ; L是亚烷基, - (CH 2)m -CH = CH-(CH 2)n - 或 - (CH 2)x -CH(OH) - (CH 2)y - M是苯基,苯基(硫代,氧基,氨基),二苯基甲基,二苯基甲基(硫代,氧基,氨基),以及包含它们作为活性成分的药物组合物。 式(I)化合物可以组合PGE 2受体并表现出拮抗或激动PGE2受体的活性。 因此,它们可用作抗高血脂,防止流产,镇痛药,止泻药,睡眠诱导剂,利尿剂,抗糖尿病,止痛药,通气药,抗溃疡药,抗胃炎或抗高血压药等。

    Naphthyloxyacetic acid
    7.
    发明授权
    Naphthyloxyacetic acid 失效
    萘氧基乙酸

    公开(公告)号:US5723493A

    公开(公告)日:1998-03-03

    申请号:US768291

    申请日:1996-12-17

    摘要: (1) Naphthyloxyaetic acid represented by the compound of the formula (I): ##STR1## and non-toxic salts thereof, (2) process for the preparation of the compounds represented by the compound of the formula (I) described hereinbefore, (3) PGE.sub.2 antagonist or agonist containing the compound represented by the compound of the formula (I) as the active ingredient. The compounds represented by the compounds of the formula (I) can be adapted to medicines which possess an inhibitory effect of uterine contraction, an analgesic action, an inhibitory effect of digestive peristalsis, a sleep-inducing effect as PGE.sub.2 antagonists, and an uterine contractile activity, a promoting effect of digestive peristalsis, a suppressive effect of gastric acid secretion, hypotensive activity as PGE.sub.2 agonists. The compounds bind to PGE.sub.2 receptor and have an activity of antagonist or agonist against the action thereof.

    摘要翻译: (1)由式(I)的化合物代表的萘乙酸:其中,(I)化合物及其无毒盐,(2)由上述式(I)的化合物表示的化合物的制备方法, (3)PGE2拮抗剂或含有式(I)化合物所代表的化合物作为活性成分的激动剂。 由式(I)化合物表示的化合物可以适用于具有子宫收缩抑制作用,止痛作用,消化性蠕动抑制作用,睡眠诱导作用PGE2拮抗剂和子宫收缩的药物 活动,消化性蠕动的促进作用,胃酸分泌的抑制作用,作为PGE2激动剂的降血压活性。 该化合物与PGE2受体结合,并具有拮抗剂或激动剂抵抗其作用的活性。

    Sulfonamide and carboxamide derivatives and drugs containing the same as the active ingredient
    8.
    发明授权
    Sulfonamide and carboxamide derivatives and drugs containing the same as the active ingredient 失效
    磺酰胺和甲酰胺衍生物以及含有与活性成分相同的药物

    公开(公告)号:US06790866B2

    公开(公告)日:2004-09-14

    申请号:US10207078

    申请日:2002-07-30

    IPC分类号: A61K3144

    摘要: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.

    摘要翻译: 式(I)的磺酰胺或氨基酰胺衍生物和包含它们作为活性成分的药物组合物:其中A环,B环为碳环,杂环; Z 1为-COR 1,-CH = CH-COR 1等; Z 2是H,烷基等; Z 3是单键,亚烷基; Z 4是SO 2,CO; Z 5是烷基,苯基,杂环 环等; R 2是CONR 8,O,S,NZ 6,Z 7 - 亚烷基,亚烷基等; R 3是H,烷基,卤素,CF 3等; R 式(I)化合物可以与PGE2的受体结合,对其作用或激动作用具有拮抗作用。 因此,它们被认为可用作抑制子宫收缩,止痛剂,止泻药,睡眠诱导剂,用于增加膀胱能力的药物或用于子宫收缩的药物,通气,抑制胃酸分泌,抗高血压药或利尿剂的药物。

    Benzenesulfonamide compounds
    9.
    发明授权
    Benzenesulfonamide compounds 失效
    苯磺酰胺化合物

    公开(公告)号:US06235777B1

    公开(公告)日:2001-05-22

    申请号:US09078577

    申请日:1998-05-14

    IPC分类号: A61K3121

    摘要: A benzenesulfonamide compound of the formula (I) (R1 is hydroxy, C1˜4 alkoxy, NR6R7 (each R6 and R7 is, independently, H or C1˜4 alkyl.); R2 is H, C1˜4 alkyl; R3, R4 are C1˜4 alkyl, halogen trifluoromethyl; R5 is H, C1˜4 alkyl, halogen, trifluoromethyl; Y is cis-vinylene, trans-vinylene; and the symbol (i) is single bond, double bond.), non-toxic salt thereof or cyclodextrin clathrate thereof and an antagonist of EP1 receptor which is a prostaglandin E2 receptor subtype comprising it as an active ingredient. The present invention compounds of the of the formula (I) can bind strongly to EP1 receptor which is a prostaglandin E2 receptor subtype and scarcely bind to the other receptor subtypes. Therefore, they are considered to be useful as antipyretic agents, as analgesics or as treating agent for pollakiuria having little side effect.

    摘要翻译: 式(I)的苯磺酰胺化合物(R 1是羟基,C 1-4烷氧基,NR 6 R 7(各R 6和R 7独立地是H或C 1-4烷基); R 2是H,C 1-4烷基; R 3,R 4 是C1〜4烷基,卤素三氟甲基; R5是H,C1〜4烷基,卤素,三氟甲基; Y是顺式亚乙烯基,反式亚乙烯基;符号(i)是单键,双键),无毒 其盐或环糊精包合物和作为前列腺素E2受体亚型的EP1受体的拮抗剂,其包含其作为活性成分。本发明式(I)的化合物可以强烈地与作为前列腺素E2受体的EP1受体结合 亚型,几乎不结合其他受体亚型。 因此,它们被认为可用作解热剂,作为止痛剂或作为尿酸治疗剂具有很小的副作用。

    Naphthyloxyacetic acid derivatives and drugs comprising the same as
active ingredients
    10.
    发明授权
    Naphthyloxyacetic acid derivatives and drugs comprising the same as active ingredients 失效
    萘氧基乙酸衍生物和包含与活性成分相同的药物

    公开(公告)号:US6018068A

    公开(公告)日:2000-01-25

    申请号:US102

    申请日:1998-01-26

    摘要: The naphthyloxyacetic acid derivatives of the formula (I) ##STR1## wherein A is H, --(alkylene)COOR.sup.1, --(alkylene)CONR.sup.2 R.sup., --(alkylene)OH, --(alkylene)tetrazole, --(alkylene)CN; E is single bond or alkylene; G is --S--, --SO--, --SO.sub.2 --, --O-- or --NR.sup.4 --; L is alkylene, --(CH.sub.2).sub.m --CH=CH--(CH.sub.2).sub.n -- or --(CH.sub.2).sub.x --CH(OH)--(CH.sub.2).sub.y --; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE.sub.2 receptor and exhibit the activity to antagonize or agonize for PGE.sub.2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.

    摘要翻译: PCT No.PCT / JP96 / 01833 Sec。 371日期1998年1月26日 102(e)日期1998年1月26日PCT提交1996年7月2日PCT公布。 公开号WO97 / 05091 日本时间1997年2月13日其中A为H, - (亚烷基)COOR1 - (亚烷基)CONR2R, - (亚烷基)OH, - (亚烷基)四唑, - (亚烷基)CN的式(I)的萘氧基乙酸衍生物 E是单键或亚烷基; G是-S - , - SO - , - SO 2 - , - O-或-NR 4 - ; L是亚烷基, - (CH 2)m -CH = CH-(CH 2)n - 或 - (CH 2)x -CH(OH) - (CH 2)y - M是苯基,苯基(硫代,氧基,氨基),二苯基甲基,二苯基甲基(硫代,氧基,氨基),以及包含它们作为活性成分的药物组合物。 式(I)化合物可以组合PGE 2受体并表现出拮抗或激动PGE2受体的活性。 因此,它们可用作抗高血脂,防止流产,镇痛药,止泻药,睡眠诱导剂,利尿剂,抗糖尿病,止痛药,通气药,抗溃疡药,抗胃炎或抗高血压药等。