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30 条记录 (耗时 0.029 秒)

    Pyridomorphinans, pyridazinomorphinans and use thereof
    2.
    发明授权
    Pyridomorphinans, pyridazinomorphinans and use thereof 有权
    吡哆醇，哒嗪吗啡喃及其用途

    公开(公告)号：US07541364B2

    公开(公告)日：2009-06-02

    申请号：US11718565

    申请日：2004-08-27

    申请人： Subramaniam Ananthan ,  Richard B. Rothman ,  Edward J. Bilsky ,  Frank Porreca

    发明人： Subramaniam Ananthan ,  Richard B. Rothman ,  Edward J. Bilsky ,  Frank Porreca

    IPC分类号： A61K31/4748 ,  C07D491/12

    CPC分类号： C07D491/18

    摘要： Compounds represented by the formula: wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R′ is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence to μ agonists.

    摘要翻译： 由下式表示的化合物：其中R是C 1-6烷基; C4-6环烷基烷基; 或C 3-6烯基; R'是H或C 1-6烷基; X是H或OH; Y是烷基，环烷基，芳基，杂芳基，芳基烷基或芳酰基; Z为CH或N; 条件是X为H，当Z为CH且R为C 4环烷基烷基或C 4链烯基时; 其前药; 及其药学上可接受的盐。 上述化合物可用作治疗疼痛的止痛剂; 作为免疫调节剂，调节滥用药物的行为效应，调节对mu激动剂的耐受性和依赖性的发展。

    PYRIDOMORPHINANS, PYRIDAZINOMORPHINANS AND USE THEREOF
    3.
    发明申请
    PYRIDOMORPHINANS, PYRIDAZINOMORPHINANS AND USE THEREOF 有权
    吡咯烷酮，吡咯烷酮和其用途

    公开(公告)号：US20090239892A1

    公开(公告)日：2009-09-24

    申请号：US12407000

    申请日：2009-03-19

    申请人： Subramaniam Ananthan ,  Richard B. Rothman ,  Edward J. Bilsky ,  Frank Porreca

    发明人： Subramaniam Ananthan ,  Richard B. Rothman ,  Edward J. Bilsky ,  Frank Porreca

    IPC分类号： A61K31/485 ,  C07D491/18 ,  A61P25/00

    CPC分类号： C07D491/18

    摘要： Compounds represented by the formula:wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R′ is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence to μ agonists.

    摘要翻译： 由下式表示的化合物：其中R是C 1-6烷基; C4-6环烷基烷基; 或C 3-6烯基; R'是H或C 1-6烷基; X是H或OH; Y是烷基，环烷基，芳基，杂芳基，芳基烷基或芳酰基; Z为CH或N; 条件是X为H，当Z为CH且R为C 4环烷基烷基或C 4链烯基时; 其前药; 及其药学上可接受的盐。 上述化合物可用作治疗疼痛的止痛剂; 作为免疫调节剂，调节滥用药物的行为效应，调节对mu激动剂的耐受性和依赖性的发展。

    Quinazolines as biogenic amine transport modulators
    4.
    发明授权
    Quinazolines as biogenic amine transport modulators 有权

    公开(公告)号：US10087148B2

    公开(公告)日：2018-10-02

    申请号：US14960023

    申请日：2015-12-04

    申请人： Subramaniam Ananthan ,  Richard B. Rothman

    发明人： Subramaniam Ananthan ,  Richard B. Rothman

    IPC分类号： C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

    摘要： The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

    Pyridomorphinans, Pyridazinomorphinans and Use Thereof
    5.
    发明申请
    Pyridomorphinans, Pyridazinomorphinans and Use Thereof 有权
    吡哆醇，哒嗪类吗啡及其用途

    公开(公告)号：US20080194568A1

    公开(公告)日：2008-08-14

    申请号：US11718565

    申请日：2004-08-27

    申请人： Subramaniam Ananthan ,  Richard B. Rothman ,  Edward J. Bilsky ,  Frank Porreca

    发明人： Subramaniam Ananthan ,  Richard B. Rothman ,  Edward J. Bilsky ,  Frank Porreca

    IPC分类号： A61K31/485 ,  A61K31/5025 ,  C07D489/02 ,  A61P29/00 ,  A61P25/30

    CPC分类号： C07D491/18

    摘要： Compounds represented by formula (I) wherein R is C1-6cycloalkylalkyl; or C3-6 alkenyl; R′ is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence of μ agonists.

    摘要翻译： 由式（I）表示的化合物，其中R是C 1-6环烷基烷基; 或C 3-6烯基; R'是H或C 1-6烷基; X是H或OH; Y是烷基，环烷基，芳基，杂芳基或芳酰基; Z为CH或N; 条件是X是H，当Z是CH且R是C 4环烷基烷基或C 1-4链烯基时; 其前药; 及其药学上可接受的盐。 上述化合物可用作治疗疼痛的止痛剂; 作为免疫调节剂，调节滥用药物的行为效应，并调节mu激动剂的耐受性和依赖性的发展。

    Pyridomorphinans, pyridazinomorphinans and use thereof
    6.
    发明授权
    Pyridomorphinans, pyridazinomorphinans and use thereof 有权
    吡哆醇，哒嗪吗啡喃及其用途

    公开(公告)号：US07951817B2

    公开(公告)日：2011-05-31

    申请号：US12407000

    申请日：2009-03-19

    申请人： Subramaniam Ananthan ,  Richard B. Rothman ,  Edward J. Bilsky ,  Frank Porreca

    发明人： Subramaniam Ananthan ,  Richard B. Rothman ,  Edward J. Bilsky ,  Frank Porreca

    IPC分类号： A61K31/4748 ,  C07D491/12

    CPC分类号： C07D491/18

    摘要： Compounds represented by the formula:wherein R is C1-6 alkyl; C4-6 cycloalkylalkyl; or C3-6 alkenyl; R′ is H or C1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or aroyl; and Z is CH or N; provided that X is H, when Z is CH and R is C4 cycloalkylalkyl or C4 alkenyl; prodrugs thereof; and pharmaceutically acceptable salts thereof are provided. Compounds of the above formula are useful as analgesics for treating pain; as immunomodulators, to modulate the behavioral effects of drugs of abuse and to modulate the development of tolerance and dependence to μ agonists.

    摘要翻译： 由下式表示的化合物：其中R是C 1-6烷基; C4-6环烷基烷基; 或C 3-6烯基; R'是H或C 1-6烷基; X是H或OH; Y是烷基，环烷基，芳基，杂芳基，芳基烷基或芳酰基; Z为CH或N; 条件是X为H，当Z为CH且R为C 4环烷基烷基或C 4链烯基时; 其前药; 及其药学上可接受的盐。 上述化合物可用作治疗疼痛的止痛剂; 作为免疫调节剂，调节滥用药物的行为效应，并调节对μ激动剂的耐受性和依赖性的发展。

    Nonpeptide Inhibitors of Matrix Metalloproteinases
    10.
    发明申请
    Nonpeptide Inhibitors of Matrix Metalloproteinases 失效
    基质金属蛋白酶的非肽抑制剂

    公开(公告)号：US20080312329A1

    公开(公告)日：2008-12-18

    申请号：US10593748

    申请日：2005-03-21

    申请人： Subramaniam Ananthan

    发明人： Subramaniam Ananthan

    IPC分类号： A61K31/165 ,  C07C323/63 ,  C12N5/02 ,  C12N5/08 ,  A61P35/04

    CPC分类号： C07C311/20 ,  C07C311/29 ,  C07C311/43 ,  C07C2601/14

    摘要： Disclosed are selective inhibitors of matrix metalloproteinases represented by the following formula (I). wherein X is (CH2)nO, (CH2)nS, (CH2)nNR1, (CH2)n(CH2), or CH═CH, wherein n=0, 1, or 2; R and R1 are, independently, a substituted or unsubstitued alkyl, alkenyl, alkynyl, aryl, heteroaryl group, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl; and Z is NH or CH2; or a pharmaceutically acceptable salt thereof. Also disclosed are methods of making such compounds and methods of using such compounds to inhibit tumor progression and to treat diseases such as arthritis.

    摘要翻译： 公开了由下式（I）表示的基质金属蛋白酶的选择性抑制剂。 其中X是（CH 2）n O，（CH 2）n S，（CH 2）n NR1，（CH 2）n（CH 2）或CH-CH，其中n = 0,1或2; R和R 1独立地是取代或未取代的烷基，烯基，炔基，芳基，杂芳基，环烷基，杂环烷基，环烯基或杂环烯基; Z为NH或CH 2; 或其药学上可接受的盐。 还公开了制备这些化合物的方法和使用这些化合物抑制肿瘤进展和治疗疾病如关节炎的方法。