PYRROLE AND PYRAZOLE DAAO INHIBITORS
    175.
    发明申请
    PYRROLE AND PYRAZOLE DAAO INHIBITORS 审中-公开
    吡咯和吡唑多糖抑制剂

    公开(公告)号:US20110092559A1

    公开(公告)日:2011-04-21

    申请号:US12965175

    申请日:2010-12-10

    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。

    Nonracemic mixtures and uses thereof

    公开(公告)号:US12161623B2

    公开(公告)日:2024-12-10

    申请号:US17977920

    申请日:2022-10-31

    Abstract: Provided are compositions comprising unequal mixtures of (R)-amisulpride and (S)-amisulpride, or pharmaceutically acceptable salts thereof, where the amount of (R)-amisulpride is greater than the amount of (S)-amisulpride, compositions and medicaments comprising the same used for the treatment of various diseases and disorders, and methods of using same for the treatment of various diseases and disorders, including, but not limited to, dosage regimens. In addition, provided are various formulations thereof, including, but not limited to, formulations employing polymorphs of enantiomeric amisulpride.

    Computational Model and Methods for Selecting Clinical Trial Subjects to Reduce Heterogeneity

    公开(公告)号:US20240185965A1

    公开(公告)日:2024-06-06

    申请号:US18284130

    申请日:2022-03-30

    CPC classification number: G16H10/20 G16H20/70 G16H50/20

    Abstract: Clinical study populations require reduced heterogeneity to properly determine effectiveness of treatments. In an embodiment, a method of verifying eligibility of a subject for a treatment includes representing the subject's symptoms in a rating scale as a vector. The method computes an anomaly score based on the vector of the subject and multiple vectors representing rating scales of other subjects. The method ranks, based on the anomaly score, the subject with a likelihood of contributing to a subgroup of patients having a common element structure of the rating scale. The method enriches a study population in a clinical trial prior to randomization, the enriched study population having a reduced heterogeneity. Therefore, the method can verify diseases or conditions or diagnoses of subjects for eligibility for a clinical trial or for other purposes.

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