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    Electrocatalytic oxidation method for the production of cyclic sulfates and sulfamidates
    122.
    发明授权
    Electrocatalytic oxidation method for the production of cyclic sulfates and sulfamidates 失效
    用于生产环状硫酸盐和氨磺酸盐的电催化氧化法

    公开(公告)号：US5271812A

    公开(公告)日：1993-12-21

    申请号：US717432

    申请日：1991-06-19

    Applicant: Yun Gao ,  Charles M Zepp

    Inventor： Yun Gao ,  Charles M Zepp

    IPC: C07D291/04 ,  C07D327/10 ,  C25B3/00

    CPC classification number: C07D291/04 ,  C07D327/10 ,  C25B3/00

    Abstract: The invention relates to a process for the production of cyclic sulfates and cyclic sulfamidates from the corresponding cyclic sulfite and cyclic sulfamidite substrate, respectively. The method involves the electrolysis of a solvent mixture containing active metal species, non-metal oxidant species and substrate.

    Abstract translation: 本发明涉及分别从相应的环状亚硫酸盐和环状亚磺酰胺基质制备环状硫酸盐和环状磺酰胺酸盐的方法。 该方法涉及电解含有活性金属物质，非金属氧化剂物质和底物的溶剂混合物。

    Treating hypertension
    123.
    发明授权
    Treating hypertension 失效
    治疗高血压

    公开(公告)号：US5190962A

    公开(公告)日：1993-03-02

    申请号：US492647

    申请日：1990-03-13

    Applicant: Timothy J. Barberich ,  James W. Young

    Inventor： Timothy J. Barberich ,  James W. Young

    IPC: A61K31/44 ,  A61K45/06

    CPC classification number: A61K45/06 ,  A61K31/44

    Abstract: The optically pure isomer of nitrendipine having anti-hypertensive activity, is a potent anti-hypertensive drug for reducing blood pressure in individuals without the undesirable side effects associated with administration of a racemic mixture of nitrendipine. A method is disclosed utilizing an optically pure isomer of nitrendipine for treating hypertension while reducing undesirable side effects associated with nitrendipine.

    Abstract translation: 具有抗高血压活性的尼群地平的光学纯的异构体是用于降低个体血压的有效的抗高血压药物，而没有与施用尼群地平的外消旋混合物相关的不期望的副作用。 公开了利用尼群地平的光学纯异构体治疗高血压同时减少与尼群地平相关的不良副作用的方法。

    Methods for preparing captopril and its analogues
    125.
    发明授权
    Methods for preparing captopril and its analogues 失效
    卡托普利及其类似物的制备方法

    公开(公告)号：US5166361A

    公开(公告)日：1992-11-24

    申请号：US766958

    申请日：1991-09-25

    Applicant: Charles M. Zepp

    Inventor： Charles M. Zepp

    IPC: C07D205/04 ,  C07D207/16 ,  C07D211/60

    CPC classification number: C07D205/04 ,  C07D207/16 ,  C07D211/60

    Abstract: This invention relates to novel methods for converting a diastereomeric mixture of S-protected derivatives of an orally active inhibitor of an angiotensin-converting enzyme (ACE) and its analogues into its separate optically resolved diastereomeric components. Specifically the invention relates to methods for the preparation of optically purified captopril and its analogs from racemic precursors. This resolution process is achieved through the fractional crystallization of S-protected derivatives of captopril and its precursors, which derivatives are useful for the reason that they are (1) easily prepared from novel precursors, (2) resolvable to their optically purified stereoisomeric species and (3) convertible to non-derivatized stereoisomeric species which correspond to the pharmacologically active inhibitor and its analogues. Novel methods for preparing the derivatives and their precursors are also noted herein. In addition, the novel derivatives and their precursors are also described herein.

    Abstract translation: 本发明涉及将血管紧张素转换酶（ACE）的口服活性抑制剂的S-保护衍生物与其类似物的非对映异构体混合物转化成其单独的光学拆分的非对映体组分的新方法。 具体地说，本发明涉及从外消旋前体制备光学纯化的卡托普利及其类似物的方法。 该解决方法是通过巯基及其前体的S-保护衍生物的分级结晶来实现的，该衍生物是有用的，因为它们是（1）容易地由新型前体制备，（2）可分解成其光学纯化的立体异构物质， （3）可转化成对应于药理活性抑制剂及其类似物的非衍生化立体异构体。 本文还注意到制备衍生物及其前体的新方法。 此外，本文还描述了新的衍生物及其前体。

    Pyrrole and pyrazole DAAO inhibitors
    127.
    发明授权
    Pyrrole and pyrazole DAAO inhibitors 有权
    吡咯和吡唑DAAO抑制剂

    公开(公告)号：US07893098B2

    公开(公告)日：2011-02-22

    申请号：US12566990

    申请日：2009-09-25

    Applicant: Q. Kevin Fang ,  Seth Hopkins ,  Michele Heffernan ,  Milan Chytil

    Inventor： Q. Kevin Fang ,  Seth Hopkins ,  Michele Heffernan ,  Milan Chytil

    IPC: A61K31/415 ,  C07D231/14 ,  C07D231/54

    CPC classification number: C07D231/56 ,  C07D207/34 ,  C07D209/42 ,  C07D209/44 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D491/04

    Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5; R5 is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R6 and R7 are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R1, R2 and R4 is other than hydrogen; and at least one of X and Y is (CR6R7)n. D-serine or cycloserine may be coadministered along with the compound of formula I.

    Abstract translation: 提高D-丝氨酸浓度，降低D-丝氨酸氧化毒性浓度的方法，用于增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛，或防止神经功能特征丧失 的神经变性疾病涉及向需要治疗的受试者施用治疗有效量的式I化合物或其药学上可接受的盐或溶剂合物：其中R 1和R 2独立地选自氢，卤素，硝基，烷基，酰基， 烷基芳基和XYR5; 或R 1和R 2一起形成5,6,7或8元取代或未取代的碳环或杂环基团; X和Y独立地选自O，S，NH和（CR 6 R 7）n; R3是氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌离子或它们的混合物; Z是N或CR4; R4选自氢，卤素，硝基，烷基，烷基芳基和XYR5; R 5选自芳基，取代的芳基，杂芳基和取代的杂芳基; R6和R7独立地选自氢和烷基; n是1至6的整数; R 1，R 2和R 4中的至少一个不是氢; 并且X和Y中的至少一个是（CR 6 R 7）n。 D-丝氨酸或环丝氨酸可以与式I化合物共同给药。

    Treatment of CNS Disorders With trans 4-(3,4-Dichlorophenyl)-1,2,3,4-Tetrahydro-1-Napthalenamine
    129.
    发明申请
    Treatment of CNS Disorders With trans 4-(3,4-Dichlorophenyl)-1,2,3,4-Tetrahydro-1-Napthalenamine 有权
    用反式4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺处理中枢神经系统疾病

    公开(公告)号：US20100292340A1

    公开(公告)日：2010-11-18

    申请号：US12847270

    申请日：2010-07-30

    Applicant: Thomas P. JERUSSI ,  Qun Kevin FANG ,  Mark G. CURRIE

    Inventor： Thomas P. JERUSSI ,  Qun Kevin FANG ,  Mark G. CURRIE

    IPC: A61K31/135 ,  A61P25/18

    CPC classification number: A61K31/135 ,  C07B2200/07 ,  C07C211/42 ,  C07C2602/10

    Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

    Abstract translation: 用（1R，4S） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺处理CNS障碍; 和（1S，4R） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺。 还公开了制备4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺的方法。 该方法包括制备N- [4-（3,4-二氯苯基）-1,2,3,4-四氢萘-1-基]甲酰胺的全部四种异构体，它们也是有用的。

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