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    Amines that inhibit a mammalian anandamide transporter, and methods of use thereof
    67.
    发明授权
    Amines that inhibit a mammalian anandamide transporter, and methods of use thereof 有权
    抑制哺乳动物anandamide转运蛋白的胺及其使用方法

    公开(公告)号：US07511073B2

    公开(公告)日：2009-03-31

    申请号：US11439529

    申请日：2006-05-23

    Applicant: Brian M. Aquila ,  Seth C. Hopkins ,  Curtis A. Lockshin ,  Fengjiang Wang

    Inventor： Brian M. Aquila ,  Seth C. Hopkins ,  Curtis A. Lockshin ,  Fengjiang Wang

    IPC: A61K31/34 ,  A61K31/135 ,  C07D307/04 ,  C07C211/03

    CPC classification number: C40B40/04 ,  C07C217/58 ,  C07C2601/02 ,  C07D307/14 ,  C40B20/08 ,  C40B30/04 ,  C40B40/00 ,  C40B50/14

    Abstract: One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke. Another aspect of the present invention relates to combinatorial libraries of amines, and methods for preparing the libraries.

    Abstract translation: 本发明的一个方面涉及胺。 本发明的第二方面涉及胺作为哺乳动物安非他明转运蛋白的抑制剂的用途。 本发明的化合物还可用于治疗影响哺乳动物的许多疾病，病症和疾病，包括但不限于哮喘，神经性疼痛，持续性疼痛，炎性疼痛，多动症，高血压，脑缺血，帕金森病， 痉挛性，Tourette综合征，精神分裂症，出血性休克，败血性休克，心脏休克，偏头痛，霍顿头痛，多发性硬化症，厌食症，艾滋病综合征，器官排斥反应，自身免疫性疾病，变态反应，关节炎，克罗恩病，恶性胶质瘤，神经变性疾病，亨廷顿病 舞蹈病，青光眼，恶心，焦虑，精神病，注意力缺陷多动障碍，早泄和中风。 本发明的另一方面涉及胺的组合文库，以及制备文库的方法。

    Pyrrole and pyrazole DAAO inhibitors
    68.
    发明授权
    Pyrrole and pyrazole DAAO inhibitors 有权

    公开(公告)号：US07488747B2

    公开(公告)日：2009-02-10

    申请号：US11023924

    申请日：2004-12-28

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

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

    IPC: A61K31/416 ,  A61K31/405 ,  C07D231/56

    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.

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