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18 条记录 (耗时 0.036 秒)

    Cyclic peptide LHRH antagonists
    5.
    发明授权
    Cyclic peptide LHRH antagonists 失效
    环肽LHRH拮抗剂

    公开(公告)号：US5508383A

    公开(公告)日：1996-04-16

    申请号：US208544

    申请日：1994-03-09

    申请人： Daryl R. Sauer ,  Fortuna Haviv

    发明人： Daryl R. Sauer ,  Fortuna Haviv

    IPC分类号： A61K38/00 ,  C07K7/23 ,  C07K14/59 ,  C07K7/64

    CPC分类号： C07K7/23 ,  A61K38/00

    摘要： A class of cyclic peptides are effective inhibitors of LHRH and are useful in the treatment of disease conditions which are mediated by sex hormones including prostate cancer, endometriosis, uterine fibroids, and precocious puberty.

    摘要翻译： 一类环肽是LHRH的有效抑制剂，可用于治疗由性激素（包括前列腺癌，子宫内膜异位症，子宫肌瘤和早熟性青春期）介导的疾病状况。

    N-[PIPERAZINYL HETARYL]ARYLSUFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR
    8.
    发明申请
    N-[PIPERAZINYL HETARYL]ARYLSUFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR 失效
    具有多巴胺D3受体亲和性的N- [哌嗪基]维生素A亚磺酰胺化合物

    公开(公告)号：US20110294817A1

    公开(公告)日：2011-12-01

    申请号：US13117269

    申请日：2011-05-27

    申请人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer ,  Sean C. Turner

    发明人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer ,  Sean C. Turner

    IPC分类号： A61K31/496 ,  A61P13/12 ,  A61P25/00 ,  C07D401/04 ,  A61K31/4995

    CPC分类号： C07D213/74 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D403/04 ,  C07D403/14 ,  C07D487/08

    摘要： The invention related to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula (I) in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Ra which is/are selected, independently of each other, from halogen, CN, NO2, CO2R4, COR5, C1-C4-alkyl and C1-C4-haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Rb, which is/are selected from halogen, NO2, CN, CO2R4, COR5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl and C1-C4-haloalkyl, with it also being possible for two radicals Rb which are bonded to adjacent C atoms of Ar to be together C3-C4-alkylene; R1 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; with the radicals n, R1, R2, R3, R4 and R5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropriate together with physiologically acceptable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.

    摘要翻译： 本发明涉及通式（I）的N - [（哌嗪基）杂芳基]芳基磺酰胺化合物，其中Q是具有1或2个N原子作为环成员的二价，6元杂芳族基团，并且任选地带有一个或两个 被卤素，CN，NO 2，CO 2 R 4，COR 5，C 1 -C 4 - 烷基和C 1 -C 4卤代烷基独立地选择的取代基R a; Ar是苯基或6元杂芳族基，其具有1或2个N原子作为环成员，并且任选地带有一个或两个选自卤素，NO 2，CN，CO 2 R 4，COR 5，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基-C 1 -C 4 - 烷基和C 1 -C 4卤代烷基， 与Ar的相邻C原子一起C3-C4-亚烷基; R 1是氢，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 3 -C 6环烷基，C 3 -C 6环烷基-C 1 -C 4烷基，C 1 -C 4羟烷基，C 1 -C 4烷氧基-C 1 -C 4 - 烷基，C 3 -C 4 - 烯基或C 3 -C 4 - 炔基; 具有如专利权利要求中给出的含义的基团n，R 1，R 2，R 3，R 4和R 5与这些化合物的N-氧化物和生理上耐受的酸加成盐以及包含至少一种N- 和/或至少一种I的生理学耐受的酸加成盐和/或I的N-氧化物，其中适宜地与生理上可接受的载体和/或 用于治疗对多巴胺D3受体拮抗剂或激动剂影响的疾病的辅助物质，特别是用于治疗中枢神经系统疾病和肾功能障碍。

    Tetrahydrobenzazepines and their use in the modulation of the dopamine d3 receptor
    9.
    发明申请
    Tetrahydrobenzazepines and their use in the modulation of the dopamine d3 receptor 失效
    四氢苯并吖嗪及其在调节多巴胺d3受体中的用途

    公开(公告)号：US20090105224A1

    公开(公告)日：2009-04-23

    申请号：US10583590

    申请日：2004-12-17

    申请人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer

    发明人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer

    IPC分类号： C07D223/16 ,  A61K31/55 ,  A61P25/00

    CPC分类号： C07D223/16 ,  C07D409/12

    摘要： The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides.The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.

    摘要翻译： 本发明涉及通式Ⅰ的四氢苯并吖庚因，其中变量Ar，A，B，Y，R 1和R 2具有权利要求1所示的含义，以及这些化合物的N-氧化物，生理上耐受的酸加成盐 的这些化合物和N-氧化物的生理上耐受的酸加成盐。 本发明还涉及药物组合物，其包含至少一种式I的四氢苯并氮杂化合物，I的物理耐受的酸加成盐，式I化合物的N-氧化物和/或其物理上耐受的酸加成盐 I的N-氧化物，并且进一步使用根据本发明的化合物用于治疗有益于多巴胺D3受体拮抗剂或多巴胺D3激动剂的病症。 根据本发明的化合物优选可用于治疗中枢神经系统疾病如精神分裂症和抑郁症以及治疗肾功能障碍。

    SYNTHESIS OF NOVEL KETONE BODY ANALOGS FOR USE AS A NUTRITIONAL SUPPLEMENT
    10.
    发明公开
    SYNTHESIS OF NOVEL KETONE BODY ANALOGS FOR USE AS A NUTRITIONAL SUPPLEMENT 审中-公开

    公开(公告)号：US20230150913A1

    公开(公告)日：2023-05-18

    申请号：US17525663

    申请日：2021-11-12

    申请人： Samuel J. Rozzoni ,  Daryl R. Sauer

    发明人： Samuel J. Rozzoni ,  Daryl R. Sauer

    IPC分类号： C07C69/18 ,  C07C69/21 ,  A23L33/10

    CPC分类号： C07C69/18 ,  C07C69/21 ,  A23L33/10

    摘要： When a healthy and balanced diet is not achieved, nutritional supplements are used to help deal with the resulting health issues and enhance the body's performance. Two compounds of interest in this research, ketone bodies and β-Hydroxy β-Methylbutyrate (HMB) have been used for dealing with the side effects of various health conditions including muscle mass loss and insufficient food intake. Although these molecules have been used extensively as supplements, no supplement was found which combined the properties of both ketone bodies and HMB. This project was conceived to create a novel category of molecules that combine the properties of both ketone bodies and HMB that can be used as supplements for treating a wide range of health-related issues. Acetoacetate and isopentyldiol were used as the sources of ketone bodies and HMB, respectively. Six novel compounds were synthesized using transesterification of acetoacetate and isopentyldiol. Some of the developed reaction procedures were versatile as they could be performed under a variety of parameters such as solventless, catalyst-free, and mild conditions. Immobilized enzymes and chemicals were used to generate new compounds under greener parameters. The compounds that were isolated were characterized using GCMS, H NMR, and FTIR instrumentation. In summary, the goal of this research project was to design and synthesize novel ketone body analogs.