USE OF (HALOBENZYLOXY) BENZYLAMINO-PROPANAMIDES FOR THE MANUFACTURE OF MEDICAMENTS ACTIVE AS SODIUM AND/OR CALCIUM CHANNEL SELECTIVE MODULATORS
    1.
    发明申请
    USE OF (HALOBENZYLOXY) BENZYLAMINO-PROPANAMIDES FOR THE MANUFACTURE OF MEDICAMENTS ACTIVE AS SODIUM AND/OR CALCIUM CHANNEL SELECTIVE MODULATORS 审中-公开
    (HALOBENZYLOXY)苯甲酰胺丙酰胺用于制备作为钠和/或钙通道选择性调节剂活性的药物的用途

    公开(公告)号:US20110184068A1

    公开(公告)日:2011-07-28

    申请号:US12939726

    申请日:2010-11-04

    IPC分类号: A61K31/167 A61P25/04

    摘要: The invention relates to the use of selected (R)-2-[(halobenzyloxy)benzylamino]-propanamides and the pharmaceutically acceptable salts thereof for the manufacture of medicament, that are selectively active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, pain, migraine, periferal diseases, cardiovascular diseases, inflammatory processes affecting all body systems, disorders affecting skin and related tissues, disorders of the respiratory system, disorders of the immune and endocrinological systems, gastrointestinal, urogenital, metabolic and seizure disorders, where the above mechanisms have been described as playing a pathological role.

    摘要翻译: 本发明涉及选择的(R)-2 - [(卤代苄氧基)苄基氨基] - 丙酰胺及其药学上可接受的盐在制备药物中的用途,其作为钠和/或钙通道调节剂选择性活性, 预防,缓解和治愈各种病症,包括疼痛,偏头痛,周围疾病,心血管疾病,影响所有身体系统的炎症过程,影响皮肤和相关组织的疾病,呼吸系统疾病,免疫和内分泌系统疾病 ,胃肠道,泌尿生殖,代谢和发作障碍,其中上述机制被描述为发挥病理作用。

    ALPHA-AMINOAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF PSYCHIATRIC DISORDERS
    2.
    发明申请
    ALPHA-AMINOAMIDE DERIVATIVES USEFUL IN THE TREATMENT OF PSYCHIATRIC DISORDERS 有权
    用于治疗心理疾病的ALPHA-氨基腺苷衍生物

    公开(公告)号:US20110014304A1

    公开(公告)日:2011-01-20

    申请号:US12816143

    申请日:2010-06-15

    CPC分类号: A61K31/165

    摘要: The disclosure relates to pharmacotherapy of a psychiatric disorder which is schizophrenia and/or anxiety, wherein schizophrenia includes schizophrenia related disorders such as brief psychotic disorders, delusional disorders, schizoaffective disorders, and schizophreniform disorders, and anxiety includes panic disorders, obsessive-compulsive disorders (OCD), post-traumatic stress disorders (PTSD), social phobia or social anxiety disorders, specific phobia, and generalized anxiety disorders (GAD). The compounds of the disclosure are useful for the treatment of the above psychiatric disorders alone or in combination with other therapeutical agents effective in the treatment of schizophrenia and/or anxiety disorders.

    摘要翻译: 本公开涉及精神障碍和/或焦虑症的精神障碍的药物治疗,其中精神分裂症包括精神分裂症相关的疾病,例如短暂性精神病,妄想障碍,分裂情感障碍和精神分裂症样症状,焦虑包括恐慌症,强迫症(强迫症) OCD),创伤后应激障碍(PTSD),社交恐惧症或社会焦虑症,特定恐惧症和广泛性焦虑症(GAD)。 本公开的化合物可用于单独或与治​​疗精神分裂症和/或焦虑症有效的其它治疗剂组合治疗上述精神障碍。

    N-acyl-N′-benzyl-alkylendiamino derivatives

    公开(公告)号:US07411091B2

    公开(公告)日:2008-08-12

    申请号:US10580367

    申请日:2004-11-12

    CPC分类号: C07D207/27 C07C233/36

    摘要: This invention is related to compounds and use of N-Acyl-N′-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C2-C8 alkyl chain; X is a methylene, oxygen, sulphur or a NR7 group; R1 is a straight or branched C1-C8 alkyl or C3-C8 alkenylene or C3-C8 alkynylene chain, optionally substituted with CF3, phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C1-C4 alkyl, halogens, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R2, R3 are independently hydrogen, a C1-C3 alkyl chain, halogen, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R4, R5 are independently hydrogen or C1-C6 alkyl; R6 is a hydrogen or a straight or branched C1-C8 alkyl or linked to R5 can form a five to seven membered lactam; R7 is hydrogen or C1-C6 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to, neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role

    Azabicycloalkyl derivatives of imidazo[1,5-a]indol-3-one and process for
their preparation
    8.
    发明授权
    Azabicycloalkyl derivatives of imidazo[1,5-a]indol-3-one and process for their preparation 失效
    咪唑并[1,5-a]吲哚-3-酮的氮杂双环烷基衍生物及其制备方法

    公开(公告)号:US5637596A

    公开(公告)日:1997-06-10

    申请号:US578548

    申请日:1996-01-24

    摘要: Novel 5-HT.sub.3 receptor antagonist compounds having the general formula (I) ##STR1## wherein each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, are provided.

    摘要翻译: PCT No.PCT / EP95 / 01652 Sec。 371日期:1996年1月24日 102(e)日期1996年1月24日PCT 1995年5月2日PCT PCT。 公开号WO95 / 32209 日期1995年11月30日具有通式(I)的图像的新型5-HT 3受体拮抗剂化合物(I)其中R,R 1和R 2可以相同或不同,为氢,卤素,羟基,氰基 ,C 1 -C 6烷基,CF 3,C 1 -C 6烷氧基,C 1 -C 6烷硫基,甲酰基,C 2 -C 6烷酰基,羧基,C 1 -C 6烷氧羰基,硝基,-N(R 4 R 5) 是氢,C 1 -C 6烷基,甲酰基或C 2 -C 6烷酰基; 或(R6R7)N-SO2基团,其中R6和R7各自独立地为氢或C1-C6烷基; R3是a,a)或b)其中n是1或2的整数,R8是氢,未被取代或被苯基取代的C1-C6烷基,C2-C4烯基,C2-C4炔基, 或C 2 -C 6烷酰基; 及其药学上可接受的盐。

    N-imidazolyl derivatives of substituted alkoxyimino
tetrahydronaphthalenes and chromans having antithromboxane A.sub.2
activity
    9.
    发明授权
    N-imidazolyl derivatives of substituted alkoxyimino tetrahydronaphthalenes and chromans having antithromboxane A.sub.2 activity 失效
    取代的烷氧基亚氨基四氢萘酮的N-咪唑衍生物和具有抗恶唑酮A2活性的色素

    公开(公告)号:US5246956A

    公开(公告)日:1993-09-21

    申请号:US830876

    申请日:1992-02-04

    摘要: The invention provides new imidazole containing alkoxyimino derivatives of tetrahydronaphthalene and chroman of general formula (I) ##STR1## wherein Z is --CH.sub.2 --or--O--;m is an integer of 1 to 4;n is zero of 1;T is a straight or branched saturated C.sub.1 -C.sub.6 hydrocarbon chain or C.sub.2 -C.sub.5 alkenylene chain;A is a bond or a divalent group consisting of --Si(R'R")--; --O--CH.sub.2 --,--CF.sub.2 --,C(R'R")--,vinylene or isopropenylene, wherein each of R' and R" being the same or different is hydrogen or C.sub.1 -C.sub.4 alkyl;R is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, being the same, are hydrogen or methyl, or one of R.sub.1 and R.sub.2 is hydrogen and the other isa) a C.sub.1 -C.sub.8 alkyl group;b) a C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkyl-C.sub.1 C.sub.4 alkyl group, wherein the cycloalkyl group or moiety is unsubstituted or substituted by 1 to 4 C.sub.1 -C.sub.4 alkyl groups; orc) an aryl or aryl-C.sub.1 -C.sub.4 alkyl group, wherein the aryl group or the aryl moiety is unsubstituted or substituted by 1 to 4 substituents independently chosen from halogen, hydroxy, C.sub.1 -C.sub.4 alkyl, trihalo-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio and C.sub.1 -C.sub.4 alkylsulfonyl;R.sub.3 is hydrogen or a substituent chosen from halogen, hydroxy, C.sub.1 -C.sub.4 alkyl, trihalo-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio and C.sub.1 -C.sub.4 alkylsulfonyl;R.sub.4 is an --OR.sub.5 or --N(R.sub.5 R.sub.6) group, wherein each of R.sub.5 and R.sub.6 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl;and the pharmaceutically acceptable salts thereof, which are useful in the treatment of a disease state in which an enhancement of TxA.sub.2 synthesis exerts a pathogenic effect.