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    Comformationally rigid bicyclic and adamantane derivatives useful as .alpha..sub.2 -adrenergic blocking agents
    1.
    发明授权
    Comformationally rigid bicyclic and adamantane derivatives useful as .alpha..sub.2 -adrenergic blocking agents 失效
    用作α2肾上腺素能阻断剂的组合刚性双环和金刚烷衍生物

    公开(公告)号：US6150389A

    公开(公告)日：2000-11-21

    申请号：US3902

    申请日：1998-01-07

    申请人： Stephen A. Munk ,  Michael E. Garst ,  James A. Burke

    发明人： Stephen A. Munk ,  Michael E. Garst ,  James A. Burke

    IPC分类号： A61P3/04 ,  A61P3/10 ,  A61P15/10 ,  A61P25/24 ,  A61P27/02 ,  C07D233/50 ,  C07D233/54 ,  C07D263/28 ,  C07D277/18 ,  C07D413/12 ,  A61K31/421 ,  C07D263/08

    CPC分类号： C07D413/12 ,  C07D233/50 ,  C07D263/28 ,  C07D277/18

    摘要： A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof.These compounds have .alpha..sub.2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.

    摘要翻译： 式I化合物，其中：环A是所示的五种替代多环之一，其中与键相邻的虚线表示在该位置可能存在单键或双键; X是氮，氧或硫; R为氢，1至6个碳原子的较低直链或支链烷基，或2至6个碳原子的较低直链或支链烯基，3至6个碳原子的脂环族环，任选被一个或二个取代 羟基，卤素，1至3个碳原子的烷基或1至2个碳原子的烷氧基，或亚甲二氧基苯基; 或立体异构体或其药学上可接受的盐。 这些化合物具有α2受体阻断活性，因此可用于治疗或缓解眼内压升高，非胰岛素依赖性糖尿病，男性阳ence和肥胖症。

    Conformationally rigid bicycle and adamantane derivatives useful as .alpha. 2
    3.
    发明授权
    Conformationally rigid bicycle and adamantane derivatives useful as .alpha. 2 失效
    用作α2-肾上腺素能阻断剂的构象刚性双环和金刚烷衍生物

    公开(公告)号：US5731337A

    公开(公告)日：1998-03-24

    申请号：US538694

    申请日：1995-10-03

    申请人： Stephen A. Munk ,  Michael E. Garst ,  James A. Burke

    发明人： Stephen A. Munk ,  Michael E. Garst ,  James A. Burke

    IPC分类号： A61K31/415 ,  A61K31/42 ,  A61K31/421 ,  A61K31/425 ,  A61K31/426 ,  A61P3/06 ,  A61P3/08 ,  A61P25/00 ,  A61P25/24 ,  A61P25/26 ,  A61P37/06 ,  A61P43/00 ,  C07C211/39 ,  C07D233/50 ,  C07D263/28 ,  C07D277/18 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D493/08

    CPC分类号： C07D413/12 ,  C07D233/50 ,  C07D263/28 ,  C07D277/18

    摘要： A compound of formula I ##STR1## in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have .alpha..sub.2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.

    摘要翻译： 式I的化合物 其中：环A是所示的五种备选的多环之一，其中与键相邻的虚线表示单键或双键可以是 出席会议; X是氮，氧或硫; R为氢，1至6个碳原子的较低直链或支链烷基，或2至6个碳原子的较低直链或支链烯基，3至6个碳原子的脂环族环，任选被一个或二个取代 羟基，卤素，1至3个碳原子的烷基或1至2个碳原子的烷氧基，或亚甲二氧基苯基; 或立体异构体或其药学上可接受的盐。 这些化合物具有α2受体阻断活性，因此可用于治疗或缓解眼内压升高，非胰岛素依赖性糖尿病，男性阳ence和肥胖症。

    Conformationally rigid bicyclic and adamantane derivatives useful as &agr;2-adrenergic blocking agents
    5.
    发明授权
    Conformationally rigid bicyclic and adamantane derivatives useful as &agr;2-adrenergic blocking agents 失效
    用作α2-肾上腺素能阻断剂的构象刚性双环和金刚烷衍生物

    公开(公告)号：US06706747B2

    公开(公告)日：2004-03-16

    申请号：US10393313

    申请日：2003-03-19

    申请人： Stephen A. Munk ,  James A. Burke ,  Michael E. Garst

    发明人： Stephen A. Munk ,  James A. Burke ,  Michael E. Garst

    IPC分类号： A61K31421

    CPC分类号： C07D413/12 ,  C07D233/50 ,  C07D263/28 ,  C07D277/18

    摘要： A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have &agr;2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.

    摘要翻译： 式Iin化合物，其中：环A是所示的五个替代多环之一，其中与键相邻的虚线表示在该位置可以存在单键或双键; X是氮，氧或硫; R为氢，1至6个碳原子的较低直链或支链烷基，或2至6个碳原子的较低直链或支链烯基，3至6个碳原子的脂环族环，任选被一个或二个取代 羟基，卤素，1至3个碳原子的烷基或1至2个碳原子的烷氧基，或亚甲二氧基苯基; 或其立体异构体或其药学上可接受的盐。这些化合物具有α2受体阻断活性，因此可用于治疗或缓解升高的眼内压，非胰岛素依赖性糖尿病，男性阳ence和肥胖。

    Conformationally rigid bicyclic and adamantane derivatives useful as &agr;2-adrenergic blocking agents
    6.
    发明授权
    Conformationally rigid bicyclic and adamantane derivatives useful as &agr;2-adrenergic blocking agents 失效
    用作α2-肾上腺素能阻断剂的构象刚性双环和金刚烷衍生物

    公开(公告)号：US06569884B2

    公开(公告)日：2003-05-27

    申请号：US09846399

    申请日：2001-05-01

    申请人： Stephen A. Munk ,  James A. Burke ,  Michael E. Garst

    发明人： Stephen A. Munk ,  James A. Burke ,  Michael E. Garst

    IPC分类号： A61K31415

    CPC分类号： C07D413/12 ,  C07D233/50 ,  C07D263/28 ,  C07D277/18

    摘要： A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have &agr;2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.

    摘要翻译： 式Iin化合物，其中：环A是所示的五个替代多环之一，其中与键相邻的虚线表示在该位置可能存在单键或双键; X是氮，氧或硫; R为氢，1至6个碳原子的较低直链或支链烷基，或2至6个碳原子的较低直链或支链烯基，3至6个碳原子的脂环族环，任选被一个或二个取代 羟基，卤素，1至3个碳原子的烷基或1至2个碳原子的烷氧基，或亚甲二氧基苯基; 或其立体异构体或其药学上可接受的盐。这些化合物具有α2受体阻断活性，因此可用于治疗或缓解升高的眼内压，非胰岛素依赖性糖尿病，男性阳ence和肥胖。

    Conformationally rigid bicyclic and adamantane derivatives useful as &agr;2-adrenergic blocking agents
    7.
    发明授权
    Conformationally rigid bicyclic and adamantane derivatives useful as &agr;2-adrenergic blocking agents 有权
    用作α2-肾上腺素能阻断剂的构象刚性双环和金刚烷衍生物

    公开(公告)号：US06319935B1

    公开(公告)日：2001-11-20

    申请号：US09542216

    申请日：2000-04-04

    申请人： Stephen A. Munk ,  Michael E. Garst ,  James A. Burke

    发明人： Stephen A. Munk ,  Michael E. Garst ,  James A. Burke

    IPC分类号： A61K31425

    CPC分类号： C07D413/12 ,  C07D233/50 ,  C07D263/28 ,  C07D277/18

    摘要： A compound of formula I in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or sulfur; R is hydrogen, lower straight or branched chain alkyl of 1 to 6 carbon atoms, or lower straight or branched chain alkenyl of 2 to 6 carbon atoms, a cycloaliphatic ring of 3 to 6 carbon atoms, phenyl optionally mono- or di-substituted with hydroxy, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 2 carbon atoms, or methylenedioxyphenyl; or a stereoisomer, or a pharmaceutically acceptable salt thereof. These compounds have &agr;2 receptor blocking activity and hence find use in the treatment or palliation of elevated intraocular pressure, non insulin-dependent diabetes, male impotence and obesity.

    摘要翻译： 式Iin化合物，其中：环A是所示的五个替代多环之一，其中与键相邻的虚线表示在该位置可能存在单键或双键; X是氮，氧或硫; R为氢，1至6个碳原子的较低直链或支链烷基，或2至6个碳原子的较低直链或支链烯基，3至6个碳原子的脂环族环，任选被一个或二个取代 羟基，卤素，1至3个碳原子的烷基或1至2个碳原子的烷氧基，或亚甲二氧基苯基; 或其立体异构体或其药学上可接受的盐。这些化合物具有α2受体阻断活性，因此可用于治疗或缓解升高的眼内压，非胰岛素依赖性糖尿病，男性阳ence和肥胖。

    Aryl-imidazolines and aryl-imidazoles useful as .alpha.-2 adrenergic agonists without cardiovascular side effects
    8.
    发明授权
    Aryl-imidazolines and aryl-imidazoles useful as .alpha.-2 adrenergic agonists without cardiovascular side effects 失效
    芳基咪唑啉和芳基咪唑可用作α-2肾上腺素能激动剂，无心血管副作用

    公开(公告)号：US6087361A

    公开(公告)日：2000-07-11

    申请号：US971952

    申请日：1997-11-17

    申请人： Stephen A. Munk ,  James A. Burke ,  Ronald K. Lai

    发明人： Stephen A. Munk ,  James A. Burke ,  Ronald K. Lai

    IPC分类号： A61K31/56

    CPC分类号： A61K31/56

    摘要： Methods are disclosed for treating a mammal with a condition that responds to .alpha.2 agonist treatment without causing cardiovascular side effects using compounds of the formula ##STR1## wherein R.sub.1 is H, alkyl or 1 to 4 carbon atoms or a halogen atom, X is O or NH and A is H or an oxo group and wherein said compound does not cause a concomitant reduction in blood pressure of said mammal.

    摘要翻译： 公开了用于治疗具有响应α2激动剂治疗而不引起心血管副作用的病症的哺乳动物的方法，其中R 1为H，烷基或1至4个碳原子或卤素原子，X为O或NH， A是H或氧代基，其中所述化合物不会引起所述哺乳动物血压的伴随降低。

    Vinyl ether terminated ester oligomers
    9.
    发明授权
    Vinyl ether terminated ester oligomers 失效
    乙烯基醚封端的酯低聚物

    公开(公告)号：US4749807A

    公开(公告)日：1988-06-07

    申请号：US15256

    申请日：1987-02-17

    申请人： Stephen C. Lapin ,  Stephen A. Munk

    发明人： Stephen C. Lapin ,  Stephen A. Munk

    IPC分类号： C07C69/34 ,  C08G63/21 ,  C08G63/676 ,  C07C69/80

    CPC分类号： C07C69/34 ,  C07C69/80 ,  C07C69/82 ,  C08G63/21 ,  C08G63/676

    摘要： There are described vinyl ether terminated ester oligomers which cure or polymerize particularly rapidly, especially by cationic polymerization which is radiation induced in the presence of an onium salt. The oligomeric units arise most often from the reaction of a dicarboxylic acid with a diol, although esters with triols and higher polyhydric polyols also are useful, especially where an extensively cross-linked product is desired. The carboxyl-terminated oligomeric esters are esterified with vinyl ether terminated alcohols which can be thought of as the adducts of alkynes and polyols, especially diols.

    摘要翻译： 描述了乙烯基醚封端的酯低聚物，它们特别快速地固化或聚合，特别是通过在鎓盐存在下诱导的辐射的阳离子聚合。 尽管二羧酸与二醇的反应，低聚单元最多地出现，尽管与三醇和更高级多羟基多元醇的酯也是有用的，特别是当需要广泛交联的产物时。 羧基封端的低聚酯用乙烯基醚封端的醇酯化，可以认为是炔和多元醇，特别是二醇的加合物。

    Stain-resistant polymers derived from the itaconic acid useful as coatings for fibers
    10.
    发明授权
    Stain-resistant polymers derived from the itaconic acid useful as coatings for fibers 失效
    衍生自衣康酸的耐污染聚合物可用作纤维涂层

    公开(公告)号：US4925906A

    公开(公告)日：1990-05-15

    申请号：US292862

    申请日：1989-01-03

    申请人： George D. Green ,  Stephen A. Munk ,  Darryl K. Barnes

    发明人： George D. Green ,  Stephen A. Munk ,  Darryl K. Barnes

    IPC分类号： C08F220/22 ,  C08F222/12 ,  D06M15/263 ,  D06M15/277

    CPC分类号： D06M15/277 ,  C08F220/22 ,  C08F222/12 ,  D06M15/263

    摘要： The present invention relates to non-halogenated hydrocarbon polymeric compositions which impart durable stain resistance to fibrous substrates, particularly nylon containing articles. In addition, it relates to fluorine containing polymeric compositions which impart durable stain resistance to fibrous substrates as above. It relates also to processes in which such substrates are treated so as to impart durable stain resistance to them. It relates further to a manufacturing process for preparing the compositions of the invention.

    摘要翻译： 本发明涉及对纤维基材，特别是含尼龙制品赋予耐久耐污性的非卤代烃聚合物组合物。 此外，它涉及如上所述赋予纤维基材耐久耐污性的含氟聚合物组合物。 它还涉及处理这样的基底以赋予它们耐久性耐污性的方法。 它进一步涉及制备本发明组合物的制备方法。