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37 条记录 (耗时 0.017 秒)

    Oxolabdanes
    3.
    发明授权
    Oxolabdanes 失效
    奥洛沙坦

    公开(公告)号：US5130332A

    公开(公告)日：1992-07-14

    申请号：US653823

    申请日：1991-02-11

    申请人： Nicholas J. Hrib

    发明人： Nicholas J. Hrib

    IPC分类号： C07D311/92 ,  C07D407/12

    CPC分类号： C07D407/12 ,  C07D311/92

    摘要： Novel oxolabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.

    摘要翻译： 公开了用于制备它们的新型奥多吡啶，其中间体和方法，以及利用化合物或其组合物降低眼内压的方法。

    Alkoxycarbonylalkylphospholipids and alkylaminocarbonylalkylphospholipids
    4.
    发明授权
    Alkoxycarbonylalkylphospholipids and alkylaminocarbonylalkylphospholipids 失效
    烷氧基羰基烷基磷脂和烷基氨基羰基烷基磷脂

    公开(公告)号：US4888328A

    公开(公告)日：1989-12-19

    申请号：US166285

    申请日：1988-03-10

    申请人： Nicholas J. Hrib ,  Kirk D. Shoger ,  John J. Tegeler

    发明人： Nicholas J. Hrib ,  Kirk D. Shoger ,  John J. Tegeler

    IPC分类号： A61K31/685 ,  A61P29/00 ,  C07F9/09 ,  C07F9/572 ,  C07F9/59 ,  C07F9/6509 ,  C07F9/6533 ,  C07F9/6544

    CPC分类号： C07F9/6544 ,  C07F9/091 ,  C07F9/5721 ,  C07F9/591 ,  C07F9/650958 ,  C07F9/6533

    摘要： Novel alkoxycarbonylalkylalkylphospholipids and alkylaminocarbonylalkylphospholipids of the formula ##STR1## wherein A.sup.1 is a bivalent radical of the formula --C.sub.m H.sub.2m --wherein m is an integer having a value from 0 to 20, inclusive; A.sup.2 is a bivalent radical of the formula --C.sub.p H.sub.2p --wherein p is an integer having a value from 2 to 6, inclusive; X is a bivalent radial of the formula --O--or --N(R)--wherein R is selected from the group consisting of hydrogen, alkyl radicals having up to 6 carbon atoms, inclusive and phenyl radicals of the formula: ##STR2## where Z and a are as difined in the specification; Y is ##STR3## wherein R.sup.1 is an anlkyl radicals having up to 6 carbon atoms, inclusive and R.sup.2 and R.sup.3 are independently alkyl radicals having up to 6 carbon atoms, inclusive, or taken together with R.sup.1 and the nitrogen atom to which they are attached form a group of the formula ##STR4## wherein r is 0 or 1, and W is oxygen, CH.sub.2, sulfur or N(R.sup.4) wherein R.sup.4 is an alkyl radical having up to 6 carbon atoms, inclusive and aryl; and n is an integer having a value of 3 or 4; processes for the preparation thereof, and methods for treating inflammation utilizing compounds or compositions thereof are disclosed.

    Method of synthesizing forskolin from 9-deoxyforskolin
    6.
    发明授权
    Method of synthesizing forskolin from 9-deoxyforskolin 失效
    从9-脱氧福斯克林合成毛喉素的方法

    公开(公告)号：US4734513A

    公开(公告)日：1988-03-29

    申请号：US846550

    申请日：1986-03-31

    申请人： Nicholas J. Hrib

    发明人： Nicholas J. Hrib

    IPC分类号： C07H15/06 ,  C07D311/92 ,  C07D493/04

    CPC分类号： C07D493/04 ,  C07D311/92

    摘要： A method of regioselectively and stereoselectively synthesizing forskolin (8,13-epoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxylabd-14-en-11-one) from 9-deoxyforskolin (8,13-epoxy-1.alpha.,6.beta.,7.beta.-trihydroxylabd-14-en-11-one) with a good yield is described. In a preferred embodiment, it comprises an enol ether formation from 8,13-epoxy-1.alpha.,6.beta.,7.beta.-trihydroxylabd-14-en-11-one-6,7-carbonate, oxidation of the enol ether with a suitable peroxy acid to obtain 11,12-dehydro-8,13-epoxy-11-methoxy-1.alpha.,6.beta.,7.beta.,9.beta.-tetrahydrolabd-14-ene-6,7-carbonate and hydrolysis of the latter under an acidic condition to obtain 8,13-epoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxylabd-14-en-11-one-6,7-carbonate. As an alternative way of protecting the two hydroxy groups at carbon-6 and carbon-7, they may also be converted to dimethyl acetal during the synthetic sequence. Four compounds produced in the synthetic scheme as intermediates, namely, 9,11-dehydro-8,13-epoxy-11-methoxy-1.alpha.,6.beta.,7.beta.-trihydroxylabd-14-ene-6,7-carbonate and 11,12-dehydro-8,13-epoxy-11-methoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxylabd-14-ene-6,7-carbonate and the corresponding dimethyl acetal compounds are believed to be novel.

    3-[4-(1-substituted-4-piperazinyl)butyl]-4-thiazolidinone and related compounds
    10.
    发明授权
    3-[4-(1-substituted-4-piperazinyl)butyl]-4-thiazolidinone and related compounds 失效
    3- [4-（1-取代-4-哌嗪基）丁基] -4-噻唑烷酮及相关化合物

    公开(公告)号：US5229388A

    公开(公告)日：1993-07-20

    申请号：US795608

    申请日：1991-11-21

    申请人： Nicholas J. Hrib ,  John G. Jurcak

    发明人： Nicholas J. Hrib ,  John G. Jurcak

    IPC分类号： A61K31/425 ,  A61K31/44 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D277/14 ,  C07D277/60 ,  C07D277/82 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10

    CPC分类号： C07D277/60 ,  C07D277/14 ,  C07D277/82 ,  C07D417/12 ,  C07D417/14

    摘要： There are disclosed compounds of the formula, ##STR1## where n is 0, 1 or 2; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R.sub.1 and R.sub.2 are independently hydrogen, loweralkyl, ##STR3## or aryl except that when R.sub.1 is ##STR4## or aryl, R.sub.2 is hydrogen, or alternatively R.sub.1 +R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, or alternatively R.sub.3 +R.sub.4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.

    摘要翻译： 公开了下式的化合物，其中n为0,1或2; A是每一次出现的X独立地是氢，卤素，低级烷基，羟基，硝基，低级烷氧基，氨基，氰基，三氟甲基或甲硫基; Y在每次出现时独立地是氢，卤素，低级烷基，羟基，硝基，低级烷氧基，氨基，氰基，三氟甲基或甲硫基; m为1或2; k为1或2; R1和R2独立地是氢，低级烷基，低级或芳基，除了当R 1是芳基或芳基时，R 2是氢，或者R 1 + R 2与它们所连接的碳原子一起形成环戊烷，环己烷 ，环庚烷，吡喃，噻喃，茚满或哌啶环; R3和R4独立地是氢或低级烷基，或者R3 + R4与它们所连接的碳原子一起形成环戊烷，环己烷，环庚烷，吡喃，噻喃，吡咯烷或哌啶环，术语表示未取代的苯基的芳基 或被1,2或3个取代基取代的苯基，各自独立地为低级烷基，低级烷氧基，羟基，卤素，低级烷硫基，氰基，氨基或三氟甲基，其可用作抗精神病药，镇痛药，抗惊厥药和抗焦虑剂。