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    • 5. 发明授权
    • Naphthyloxyacetic acid
    • 萘氧基乙酸
    • US5723493A
    • 1998-03-03
    • US768291
    • 1996-12-17
    • Yuuki NagaoTakayuki MaruyamaNobuyuki Hamanaka
    • Yuuki NagaoTakayuki MaruyamaNobuyuki Hamanaka
    • C07C311/08C07C311/13C07C311/20C07C311/27C07C311/28C07C311/29A61K31/195
    • C07C311/13C07C311/08C07C311/20C07C311/27C07C311/28C07C311/29
    • (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.
    • (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。
    • 7. 发明授权
    • Naphthyloxyacetic acid derivatives and drugs comprising the same as
active ingredients
    • 萘氧基乙酸衍生物和包含与活性成分相同的药物
    • US6018068A
    • 2000-01-25
    • US102
    • 1998-01-26
    • Yuuki NagaoKazuhiko TorisuNobuyuki Hamanaka
    • Yuuki NagaoKazuhiko TorisuNobuyuki Hamanaka
    • C07C59/68C07C69/712C07C217/60C07C233/18C07C255/16C07C317/18C07C323/16C07D257/04C07C321/12C07C317/00
    • C07D257/04C07C217/60C07C233/18C07C255/16C07C317/18C07C323/16C07C59/68C07C69/712
    • 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.
    • 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。
    • 8. 发明授权
    • Carbocyclic sulfonamides
    • 碳环磺酰胺
    • US5663417A
    • 1997-09-02
    • US187008
    • 1994-01-27
    • Nobuyuki HamanakaTsumoru Miyamoto
    • Nobuyuki HamanakaTsumoru Miyamoto
    • A61K31/557A61P43/00C07C303/38C07C303/40C07C311/07C07C311/10C07C311/11C07C311/12C07C311/13C07C311/14C07C311/19C07C311/20C07C311/27C07C311/29C07D493/08A61K31/215A61K31/18C07C69/608
    • C07C311/19C07C311/07C07C311/10C07C311/11C07C311/13C07C311/14C07C311/20C07C311/27C07C311/29
    • (1) Prostaglandin (PG) E.sub.2 antagonist or agonist containing carbocyclic sulfonamides represented by the compound of the formula (I): ##STR1## cyclodextrin clathrates thereof, non-toxic salts thereof as active ingredient, (2) carbocyclic sulfonamides represented by the compound of the formula (II): ##STR2## cyclodextrin clathrates thereof, non-toxic salts thereof, (3) process for the preparation of the compound represented by the compound of the formula (II) described hereinbefore, (4) PGE.sub.2 antagonist or agonist containing the compound represented by the compound of the formula (II) as active ingredient.The compounds represented by the compounds of the formula (I) and (II) can be adapted to medicines which possess an inhibitory effect of uterine contraction, an analgetic 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, a hypotensive activity as PGE.sub.2 agonists, because they bind onto PGE.sub.2 receptor and have an activity of antagonist or agonist against the action thereof.
    • (1)由式(I)化合物表示的前列腺素(PG)E2拮抗剂或含有碳环磺酰胺的激动剂:其作为活性成分的无毒盐,(2)代表的碳环磺酰胺 通式(II)的化合物:其中,式(II)的环糊精包合物,其无毒盐,(3)由上述式(II)的化合物表示的化合物的制备方法,( 4)含有由式(II)化合物表示的化合物作为活性成分的PGE 2拮抗剂或激动剂。 由式(I)和(II)化合物表示的化合物可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拮抗剂的药物, 因为它们结合PGE2受体并且具有针对其作用的拮抗剂或激动剂的活性,因此其作为PGE2激动剂具有低血压活性,作为消化道蠕动的促进作用,胃酸分泌的抑制作用。
    • 10. 发明授权
    • 9,11-Methano-13-aza-11a-carbathrombanoic acid analogues
    • US4389413A
    • 1983-06-21
    • US285723
    • 1981-07-22
    • Nobuyuki HamanakaShinsuke HashimotoMasaki Hayashi
    • Nobuyuki HamanakaShinsuke HashimotoMasaki Hayashi
    • C07C33/14C07C405/00C07D309/12A61K31/557C07C101/14
    • C07C33/14C07C405/0091C07D309/12Y10S514/826
    • The 9,11-methano-13-aza-11a-carbathrombanoic acid analogues of the general formula: ##STR1## [wherein A represents ##STR2## (in which m is an integer of 1 to 6, the double bond between the carbon atoms in positions 5 and 6 in (iv) is in cis or trans-configuration or a mixture thereof and the phenylene group in (iv) represents o-, m- or p-phenylene), R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group of 1 to 12 carbon atoms, two R.sup.2 both represent hydrogen atoms or methyl groups, R.sup.3 represents a hydrogen atom or a hydroxy group, R.sup.4 represents a single bond or a straight- or branched-chain alkylene group of 1 to 5 carbon atoms, R.sup.5 represents(i) a straight- or branched-chain alkyl, alkoxy or alkylthio group of 1 to 8 carbon atoms,(ii) a cycloalkyl or cycloalkyloxy group of 4 to 7 carbon atoms being unsubstituted or substituted by at least one straight- or branched-chain alkyl group of 1 to 8 carbon atoms or ##STR3## in which Z represents a single bond, an oxygen atom or a sulfur atom and R.sup.6 may occupy any of the free positions on the phenyl ring and represents a hydrogen atom, a halogen atom, a hydroxy group, a straight- or branched-chain alkyl or alkoxy group of 1 to 5 carbon atoms, a trihalomethyl group, an amino group or a mono- or dialkyl-amino group of 1 to 5 carbon atoms)and the wavy line attached to the carbon atom in position 15 represents .alpha.- or .beta.-configuration or a mixture thereof, provided that, when R.sup.3 represents a hydroxy group and R.sup.4 represents a single bond, R.sup.5 does not represent an alkoxy group, an alkylthio group, a cycloalkyloxy group, a phenoxy group and a phenylthio group],and cyclodextrin clathrates thereof, and when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, possess strong inhibitory activities on platelet aggregation and on aorta contraction, and are useful for prevention and treatment of diseases which are induced by thromboxane A.sub.2.