Cyclopentane heptan(ene)oic acid, 2-heteroarylalk(en)yl derivatives as therapeutic agents
    71.
    发明授权
    Cyclopentane heptan(ene)oic acid, 2-heteroarylalk(en)yl derivatives as therapeutic agents 有权
    环戊烷庚(烯)酸,2-杂芳基烷基(烯)基衍生物作为治疗剂

    公开(公告)号:US06248773B1

    公开(公告)日:2001-06-19

    申请号:US09643330

    申请日:2000-08-22

    申请人: Robert M. Burk

    发明人: Robert M. Burk

    IPC分类号: A61K3138

    摘要: The invention relates to the use of cyclopentane heptan(ene)oic acid, 2-heteroarylalk(en)yl derivatives as ocular hypotensives. The compounds used in accordance with the invention are represented by the following formula I: wherein the hatched segments represent &agr; bonds, the solid triangle represents a &bgr; bond, wavy line attachments indicate either the alpha (&agr;) or beta (&bgr;) configuration; dashed bonds represent a double bond or a single bond, R is a substituted hetero aryl radical having at least two pendant substituents selected from the group consisting of C1 to C6 alkyl; halogen; trifluoromethyl; COR1; COCF3; SO2NR1; NO2 and CN or at least one cyano group; R1 is hydrogen or a lower alkyl radical having up to six carbon atoms; X is selected from the group consisting of —OR1 and —N(R1)2; Y is ═O or represents 2 hydrogen radicals, and the 9, 11, or 15 alkyl esters thereof; provided, however, when said heteroaryl radical is a dichlorothienyl radical, said compound is not a 1-carboxylic acid or amide thereof.

    摘要翻译: 本发明涉及环戊烷庚烷(烯)酸,2-杂芳基烷基(烯)基衍生物作为眼睛低渗剂的用途。 根据本发明使用的化合物由下式I表示:其中阴影链段表示α键,实心三角形表示β键,波浪线附着物表示α(α)或β(β)构型; 虚键表示双键或单键,R是具有至少两个选自C1-C6烷基的侧链取代基的取代杂芳基; 卤素; 三氟甲基 COR1; COCF3; SO2NR1; NO 2和CN或至少一个氰基; R1是氢或具有至多6个碳原子的低级烷基; X选自-OR1和-N(R1)2; Y为= O或表示2个氢原子,及其9,11或15个烷基酯; 但是,当所述杂芳基为二氯噻吩基时,所述化合物不是其1-羧酸或酰胺。

    Ocular depressor
    72.
    发明授权
    Ocular depressor 失效
    眼压抑制剂

    公开(公告)号:US6127413A

    公开(公告)日:2000-10-03

    申请号:US875022

    申请日:1997-10-15

    摘要: This invention relates to an agent for decreasing ocular tension comprising as an effective ingredient a 4,8-inter-m-phenylene PGI.sub.2 derivative represented by the formula: ##STR1## or a pharmaceutically acceptable salt thereof. The agent for decreasing ocular tension according to the present invention is useful as a therapeutic agent for treating various high ocular tension states such as glaucoma, ocular hypertension and high ocular tension which occurs after surgery.

    摘要翻译: PCT No.PCT / JP96 / 03351 Sec。 371日期:1997年10月15日 102(e)日期1997年10月15日PCT 1996年11月14日PCT PCT。 第WO97 / 17974号公报 日期:2005年5月22日本发明涉及一种用于降低眼睛张力的药剂,其包含作为有效成分的由下式表示的4,8-间 - 间 - 亚苯基PGI 2衍生物或其药学上可接受的盐。 根据本发明的用于降低眼睛张力的药剂可用作治疗在手术后发生的各种高眼部张力状态如青光眼,高眼压和高眼压的治疗剂。

    Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as
therapeutic agents
    73.
    发明授权
    Cyclopentane heptan(ene)oic acid, 2-heteroarylalkenyl derivatives as therapeutic agents 失效
    环戊烷庚(烯)酸,2-杂芳基烯基衍生物作为治疗剂

    公开(公告)号:US6124344A

    公开(公告)日:2000-09-26

    申请号:US974067

    申请日:1997-11-19

    申请人: Robert M. Burk

    发明人: Robert M. Burk

    摘要: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The compounds used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate a configuration; the solid triangle is used to indicate .beta. configuration; dashed bonds represent a double bond, or a single bond; R is a substituted heteroaryl radical having at least two pendant substituents selected from the group consisting of C.sub.1 to C.sub.6 alkyl; halogen; trifluoromethyl; COR.sup.1 ; COCF.sub.3 ; SO.sub.2 NR.sup.1 ; NO.sub.2 and CN or at least one cyano group; R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2 ; Y is .dbd.O or represents 2 hydrogen radicals and the 9, 11 or 15 lower alkyl esters thereof; provided, however, when said heteroaryl radical is a dichlorothienyl radical, the compound is not a 1-carboxylic add or amide thereof. Certain of the compounds represented by Formula I are novel and comprise another aspect of the present invention.

    摘要翻译: 本发明涉及使用F型前列腺素衍生物作为眼部低血压。 根据本发明使用的化合物由下式I表示:其中波浪线附着物指示α(α)或β(β)构型; 阴影线段表示一个配置; 实心三角形用于指示beta配置; 虚线键代表双键或单键; R是具有至少两个选自C 1至C 6烷基的侧基取代基的取代的杂芳基; 卤素; 三氟甲基 COR1; COCF3; SO2NR1; NO 2和CN或至少一个氰基; R 1是氢或具有至多6个碳原子的低级烷基,X选自-OR 1和-N(R 1)2; Y为= O或代表2个氢原子及其9,11或15个低级烷基酯; 但是,当所述杂芳基为二氯噻吩基时,该化合物不是其1-羧酸添加物或酰胺。 某些由式I表示的化合物是新的并且包括本发明的另一方面。

    Cyclopentane heptan(ENE)OIC acid, 2-heteroarylalkenyl derivatives as
therapeutic agents
    74.
    发明授权
    Cyclopentane heptan(ENE)OIC acid, 2-heteroarylalkenyl derivatives as therapeutic agents 失效
    环戊烷庚烷(ENE)OIC酸,2-杂芳基烯基衍生物作为治疗剂

    公开(公告)号:US6096902A

    公开(公告)日:2000-08-01

    申请号:US994810

    申请日:1997-12-19

    申请人: Robert M. Burk

    发明人: Robert M. Burk

    CPC分类号: A61K31/559 A61K31/5585

    摘要: The present invention provides cyclopentane heptanoic acid, 2 heteroaryl alkyl or alkenyl derivatives which may be substituted in the 1-position with hydroxyl, alkyloxy, amino and amido groups, e.g. 1-OH cyclopentane heptanoic acid, 2 heteroarylalkenyl derivatives. In particular, these derivatives are 7-[5-hydroxy-2-(heteroatom-substituted hydroxyhydrocarbyl)-3-hydroxycyclopentyl] heptanoic or heptenoic acids and amine, amide, ether, ester and alchohol derivatives of said acids wherein one or more of said hydroxy groups are replaced with an ether group. These compounds are potent ocular hypotensive and are particularly suited for the management of glaucoma. Moreover, the compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; with additional application in gastrointestinal disease, reproduction, fertility, incontinence, shock, inflammation, immune regulation, disorder of bone metabolism, renal dysfunction, cancer and other hypoproliferative diseases.

    摘要翻译: 本发明提供环戊烷庚酸,2个可被羟基,烷氧基,氨基和酰氨基取代的杂芳基烷基或烯基衍生物,例如。 1-OH环戊烷庚酸,2个杂芳基烯基衍生物。 特别地,这些衍生物是所述酸的7- [5-羟基-2-(杂原子取代的羟基烃基)-3-羟基环戊基]庚酸或庚烯酸和胺,酰胺,醚,酯和醇醇衍生物,其中一个或多个所述 羟基被醚基取代。 这些化合物是有效的眼低血压并且特别适用于治疗青光眼。 此外,本发明的化合物是广泛应用于全身高血压和肺部疾病的平滑肌松弛剂; 在胃肠道疾病,繁殖,生育能力,失禁,休克,炎症,免疫调节,骨代谢紊乱,肾功能障碍,癌症和其他低增殖性疾病中的应用。

    Agents containing prostacyclin derivatives for topical application
    77.
    发明授权
    Agents containing prostacyclin derivatives for topical application 失效
    含有前列环素衍生物的药物用于局部应用

    公开(公告)号:US5663203A

    公开(公告)日:1997-09-02

    申请号:US350171

    申请日:1994-11-30

    IPC分类号: A61K31/557

    CPC分类号: A61K31/5585

    摘要: The invention relates to a dermal application form of prostacyclin derivatives of Formula I ##STR1## wherein R.sub.1 means hydrogen or alkyl of 1-10 carbon atoms,A is a --CH.sub.2 --CH.sub.2 --, trans-CH.dbd.CH-- or --C.ident.C-group,W represents a hydroxymethyl group which is free or functionally modified at the hydroxy group, the OH-group being in the .alpha.- or .beta.-position,X is a CH.sub.2 -group or an oxygen atom,Z is hydrogen or a cyano group,D means a straight-chain or branched, saturated alkylene group of 1-5 carbon atoms,E is a --C.ident.C-linkage or a direct bond,R.sub.2 is a straight- or branched-chain, saturated alkyl group of 1-7 carbon atoms,R.sub.3 is a free or functionally modified hydroxy group,and, if R.sub.1 means a hydrogen atom, containing the salts thereof with physiologically compatible bases, for the treatment of ulcerations caused by arterial occlusive diseases, and other skin disorders.

    摘要翻译: 本发明涉及式I的前列环素衍生物(I)的真皮施用形式,其中R 1表示氢或1-10个碳原子的烷基,A是-CH 2 -CH 2 - ,反式-CH = CH-或 - C = C - 基,W表示在羟基上游离或官能改性的羟甲基,OH-位于α位或β位,X为CH 2基或氧原子,Z为氢 或氰基,D表示1-5个碳原子的直链或支链饱和亚烷基,E是-C = C-键或直接键,R2是直链或支链饱和烷基 1-7个碳原子的基团,R3是游离或官能改性的羟基,并且如果R 1表示含有其与生理相容性碱的盐的氢原子,用于治疗由动脉闭塞性疾病引起的溃疡和其它皮肤 疾病