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14 条记录 (耗时 0.026 秒)

    C11 oxymyl and hydroxylamino prostaglandins useful as FP agonists
    3.
    发明授权
    C11 oxymyl and hydroxylamino prostaglandins useful as FP agonists 失效
    C11氧基和羟基氨基前列腺素可用作FP激动剂

    公开(公告)号：US06444840B1

    公开(公告)日：2002-09-03

    申请号：US09647380

    申请日：2000-09-28

    申请人： Mitchell Anthony deLong ,  Jack Snyder Amburgey, Jr. ,  John August Wos ,  Biswanath De ,  David Lindsey Soper

    发明人： Mitchell Anthony deLong ,  Jack Snyder Amburgey, Jr. ,  John August Wos ,  Biswanath De ,  David Lindsey Soper

    IPC分类号： C07C6974

    CPC分类号： C07D257/04 ,  C07C239/12 ,  C07C251/44 ,  C07C405/0041 ,  C07D307/64 ,  C07D333/18

    摘要： The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.

    摘要翻译： 本发明提供了新的前列腺素类似物。 特别地，本发明涉及具有式（I）结构的化合物，其中R1，R2，R3，R4，R5，R6，W，X，Z，a，b，p和q定义如下。 本发明还包括式（I）的光学异构体，非对映异构体和对映体及其药学上可接受的盐，可生物水解的酰胺，酯和酰亚胺。 本发明的化合物可用于治疗各种疾病和病症，例如骨骼疾病和青光眼。 因此，本发明还提供包含这些化合物的药物组合物。 本发明还提供了使用这些化合物或含有它们的组合物治疗骨病和青光眼的方法。

    2-decarboxy-2-phosphinico Prostaglandin F analogs
    4.
    发明授权
    2-decarboxy-2-phosphinico Prostaglandin F analogs 有权
    2-decarboxy-2-phosphinico前列腺素F类似物

    公开(公告)号：US06372730B1

    公开(公告)日：2002-04-16

    申请号：US09632256

    申请日：2000-08-03

    申请人： Mitchell Anthony deLong ,  John August Wos ,  Biswanath De ,  Frank Hallock Ebetino

    发明人： Mitchell Anthony deLong ,  John August Wos ,  Biswanath De ,  Frank Hallock Ebetino

    IPC分类号： A61K3166

    CPC分类号： C07F9/303

    摘要： The invention provides novel Prostaglandin F analogs. In particular, the present invention is directed to compounds having a structure according to the following formula: wherein R1, R2, X, Y, V, a, b, W, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically—acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.

    摘要翻译： 本发明提供了新型前列腺素F类似物。 特别地，本发明涉及具有下式结构的化合物：其中R1，R2，X，Y，V，a，b，W和Z定义如下。本发明还包括光学异构体，非对映异构体 和上式的对映异构体及其药学上可接受的盐，生物可水解的酰胺，酯和酰亚胺。本发明的化合物可用于治疗多种疾病和病症，例如骨骼疾病和青光眼。 因此，本发明还提供包含这些化合物的药物组合物。 本发明还提供了使用这些化合物或含有它们的组合物治疗骨病和青光眼的方法。

    Process for making epoxide intermediates
    6.
    发明授权
    Process for making epoxide intermediates 失效
    制备环氧化物中间体的方法

    公开(公告)号：US6066751A

    公开(公告)日：2000-05-23

    申请号：US148539

    申请日：1998-09-04

    申请人： John August Wos ,  Jack Snyder Amburgey, Jr. ,  Mitchell Anthony deLong ,  Yili Wang ,  Haiyan George Dai ,  Biswanath De

    发明人： John August Wos ,  Jack Snyder Amburgey, Jr. ,  Mitchell Anthony deLong ,  Yili Wang ,  Haiyan George Dai ,  Biswanath De

    IPC分类号： C07D301/14 ,  C07C405/00 ,  C07D303/12

    CPC分类号： C07C405/00

    摘要： It has been surprisingly discovered that the disadvantages of the lengthy literature procedures to synthesize 13,14-dihydro prostaglandin A, E, and F derivatives can be overcome using a novel Methyl 7-(2-hydroxy-5-(2-(2-oxiranyl)ethyl)-4-(1,1,2,2 tetramethyl-1-silapropoxy)cyclopentyl) heptanoate intermediate, which can be synthesized from commercially available Methyl 7-[3-(R)-hydroxy-5-oxo-1-cyclopent-1-yl] heptanoate. This novel intermediate can be coupled with oxygen, carbon, sulfur, and nitrogen nucleophiles, in the presence of a base or a Lewis acid, in a ring-opening process to provide 13,14-dihydro prostaglandin A, E, and F derivatives.

    摘要翻译： 已经令人惊讶地发现，使用新的7-（2-羟基-5-（2-（2-（2-甲氧基乙氧基）苯基）甲基丙烯酸甲酯，可以克服长时间合成13,14-二氢前列腺素A，E和F衍生物的文献程序的缺点， 环氧乙烷基）乙基）-4-（1,1,2,2-四甲基-1-硅基丙氧基）环戊基）庚酸酯中间体，其可以从市售的7- [3-（R） - 羟基-5-氧代-1 环戊-1-基]庚酸乙酯。 这种新型中间体可以在碱或路易斯酸的存在下与氧，碳，硫和氮亲核试剂在开环过程中偶联，得到13,14-二氢前列腺素A，E和F衍生物。

    Aromatic C.sub.16 -C.sub.20 -substituted tetrahydro prostaglandins useful as FP agonists
    9.
    发明授权
    Aromatic C.sub.16 -C.sub.20 -substituted tetrahydro prostaglandins useful as FP agonists 有权
    用作FP激动剂的芳族C16-C20取代的四氢前列腺素

    公开(公告)号：US6107338A

    公开(公告)日：2000-08-22

    申请号：US148374

    申请日：1998-09-04

    申请人： John August Wos ,  Mitchell Anthony deLong ,  Jack S. Amburgey, Jr. ,  Haiyan George Dai ,  Cynthia Jean Miley ,  Biswanath De

    发明人： John August Wos ,  Mitchell Anthony deLong ,  Jack S. Amburgey, Jr. ,  Haiyan George Dai ,  Cynthia Jean Miley ,  Biswanath De

    IPC分类号： C07D333/24 ,  A61K31/5575 ,  A61P19/08 ,  A61P19/10 ,  A61P27/06 ,  A61P43/00 ,  C07C405/00

    CPC分类号： C07C405/00

    摘要： The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.

    摘要翻译： 本发明提供新颖的PGF类似物。 特别地，本发明涉及具有下式结构的化合物：其中R1，R2，R3，R4，X，Y和Z定义如下。 本发明还包括上式的光学异构体，非对映异构体和对映异构体及其药学上可接受的盐，可生物水解的酰胺，酯和酰亚胺。 本发明的化合物可用于治疗各种疾病和病症，例如骨骼疾病和青光眼。 因此，本发明还提供包含这些化合物的药物组合物。 本发明还提供了使用这些化合物或含有它们的组合物治疗骨疾病和青光眼的方法。