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28 条记录 (耗时 0.018 秒)

    Antidepressant arylpiperazine derivatives of heterocycle-fused benzodioxans
    12.
    发明申请
    Antidepressant arylpiperazine derivatives of heterocycle-fused benzodioxans 审中-公开
    杂环稠合苯并二恶烷的抗抑郁芳基哌嗪衍生物

    公开(公告)号：US20060276481A1

    公开(公告)日：2006-12-07

    申请号：US11505663

    申请日：2006-08-16

    申请人： Deborah Evrard ,  Dahui Zhou ,  Gary Stack ,  Aranapakam Venkatesan ,  Amedeo Failli ,  Susan Croce

    发明人： Deborah Evrard ,  Dahui Zhou ,  Gary Stack ,  Aranapakam Venkatesan ,  Amedeo Failli ,  Susan Croce

    IPC分类号： A61K31/496 ,  C07D491/02

    CPC分类号： C07D491/04 ,  Y02P20/582

    摘要： Compounds of the formula I: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive-compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

    摘要翻译： 式I化合物可用于治疗抑郁症（包括但不限于重度抑郁症，儿童抑郁症和抑郁症），焦虑症，恐慌症，创伤后应激障碍，经前期焦虑症（也称为月经前） 综合征），注意缺陷障碍（伴有和不伴有多动症），强迫症，社会焦虑症，广泛性焦虑症，肥胖症，进食障碍如神经性厌食症和神经性贪食症，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍及相关 疾病

    Rapamycin 42-sulfonates and 42-(N-carbalkoxy) sulfamates useful as immunosuppressive agents
    13.
    发明授权
    Rapamycin 42-sulfonates and 42-(N-carbalkoxy) sulfamates useful as immunosuppressive agents 失效
    雷帕霉素42-磺酸盐和42-（N-烷烃氧基）氨基磺酸盐可用作免疫抑制剂

    公开(公告)号：US5346893A

    公开(公告)日：1994-09-13

    申请号：US65107

    申请日：1993-05-19

    申请人： Amedeo Failli ,  Wenling Kao ,  Robert J. Steffan ,  Robert L. Vogel

    发明人： Amedeo Failli ,  Wenling Kao ,  Robert J. Steffan ,  Robert L. Vogel

    IPC分类号： C07D498/18 ,  A61K31/395 ,  C07D491/06

    CPC分类号： C07D498/18

    摘要： The invention concerns compounds of formula (I) ##STR1## where R.sup.1 is alkyl, haloalkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from phenyl, naphthyl and 4-(phenylaza) phenyl wherein said aromatic group is optionally substituted by one or more substituents selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, amino, mono- or di-(C.sub.1 -C.sub.6)alkylamino, carboxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.2 -C.sub.7 alkanoyl, (C.sub.1 -C.sub.6) thioalkyl, halo, cyano, nitro, trifuluoromethyl, trifluoromethoxy or R.sup.1 is a heteroaromatic group of 5 to 10 ring atoms containing oxygen, nitrogen and/or sulfur as heteroatom(s) wherein said heteroaromatic group is optionally substituted by one or more substituents selected form C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, amino, mono- or di-(C.sub.1 -C.sub.6)alkylamino, carboxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.2 -C.sub.7 alkanoyl, (C.sub.1 -C.sub.6) thioalkyl, halo, cyano, nitro, trifluoromethyl, trifluoromethoxy or R.sup.1 is NHCO.sub.2 R.sup.2 wherein R.sup.2 is lower alkyl containing 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof, which compounds are useful in the treatment of transplantation rejection, host versus graft disease, autoimmune diseases and diseases of inflammation.

    摘要翻译： 本发明涉及式（I）的化合物：其中R 1是含有1至6个碳原子的烷基，卤代烷基，烯基或炔基; 或选自苯基，萘基和4-（苯基苯基）苯基的芳族部分，其中所述芳族基团任选被一个或多个选自C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，氨基，单 - 或二 - C1-C6）烷基氨基，羧基，（C1-C6烷氧基）羰基，C2-C7烷酰基，（C1-C6）硫代烷基，卤素，氰基，硝基，三氟甲基，三氟甲氧基或R1是含有5-10个环原子的杂芳族基团 氧，氮和/或硫作为杂原子，其中所述杂芳基任选被一个或多个选自C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，氨基，单 - 或二 - （C 1 -C 6） 烷基氨基，羧基，（C1-C6烷氧基）羰基，C2-C7烷酰基，（C1-C6）硫代烷基，卤素，氰基，硝基，三氟甲基，三氟甲氧基或R1是NHCO2R2，其中R2是含有1至6个碳原子的低级烷基; 或其药学上可接受的盐，该化合物可用于治疗移植排斥反应，宿主与移植物疾病，自身免疫疾病和炎症疾病。

    N-Substituted dimeric cyclopeptide derivatives
    14.
    发明授权
    N-Substituted dimeric cyclopeptide derivatives 失效
    N-取代的二聚环肽衍生物

    公开(公告)号：US4401656A

    公开(公告)日：1983-08-30

    申请号：US189458

    申请日：1980-09-22

    申请人： Amedeo Failli ,  Hans U. Immer ,  Manfred K. Gotz

    发明人： Amedeo Failli ,  Hans U. Immer ,  Manfred K. Gotz

    IPC分类号： C07K5/12 ,  C07K7/64 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K7/64 ,  C07K5/12 ,  Y10S930/19 ,  Y10S930/27

    摘要： The N-substituted dimeric cyclopeptide derivatives of formula ##STR1## in which A is a peptide residue having one to four amino acid residues; R.sup.1 is lower alkyl, phenyl or phenyl(lower)alkylene; R.sup.2 is lower alkyl, cyclo(lower)alkyl or lower alkoxycarbonyl(lower)alkylene; and R.sup.3 is a neutral amino acid side chain and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful for treating microbial infections. Pharmaceutical compositions also are disclosed.

    摘要翻译： 式（I）的N-取代二聚环肽衍生物，其中A是具有1-4个氨基酸残基的肽残基; R1是低级烷基，苯基或苯基（低级）亚烷基; R2是低级烷基，环（低级）烷基或低级烷氧基羰基（低级）亚烷基; 并且R3是中性氨基酸侧链，并且公开了制备式I化合物的方法。 式I化合物可用于治疗微生物感染。 也公开了药物组合物。

    N-substituted cyclopeptide derivatives and preparation thereof
    15.
    发明授权
    N-substituted cyclopeptide derivatives and preparation thereof 失效
    N-取代的环肽衍生物及其制备

    公开(公告)号：US4237045A

    公开(公告)日：1980-12-02

    申请号：US941827

    申请日：1978-09-11

    申请人： Amedeo Failli ,  Hans U. Immer ,  Manfred K. Gotz

    发明人： Amedeo Failli ,  Hans U. Immer ,  Manfred K. Gotz

    IPC分类号： A61K38/00 ,  C07K7/64 ,  C07C103/52 ,  A61K37/00

    CPC分类号： C07K7/64 ,  A61K38/00 ,  Y10S930/19 ,  Y10S930/27 ,  Y10S930/29

    摘要： The N-substituted cyclopeptide derivatives of formula I ##STR1## in which R.sup.1 is lower alkyl, R.sup.2 is lower alkyl or cyclo(lower)alkyl, R.sup.3 is a neutral amino acid side chain and Y is a peptide residue having three to nine amino acid residues and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful antibacterial and antifungal agents. Pharmaceutical compositions also are disclosed.

    摘要翻译： 式I的N-取代的环肽衍生物，其中R 1为低级烷基，R 2为低级烷基或环（低级）烷基，R 3为中性氨基酸侧链，Y为具有3至9个氨基酸的肽残基 公开了制备式I化合物的残基和方法。 式I的化合物是有用的抗菌和抗真菌剂。 也公开了药物组合物。

    Novel hydrazinocarboxamide derivatives and preparation thereof
    16.
    发明授权
    Novel hydrazinocarboxamide derivatives and preparation thereof 失效
    新型氢氯氰菊酯衍生物及其制备方法

    公开(公告)号：US4000122A

    公开(公告)日：1976-12-28

    申请号：US565332

    申请日：1975-04-07

    申请人： Amedeo Failli ,  Verner R. Nelson ,  Hans U. Immer ,  Manfred K. Gotz

    发明人： Amedeo Failli ,  Verner R. Nelson ,  Hans U. Immer ,  Manfred K. Gotz

    IPC分类号： C07D207/40 ,  C07K5/04 ,  C07C103/52 ,  A61K37/00

    CPC分类号： C07C243/00 ,  C07D207/40

    摘要： .alpha.-Hydrazinocarboxamide and .alpha.-(.alpha.'-acylhydrazino)-carboxamide derivatives of formula I ##STR1## in which R.sup.1 and R.sup.2 each are lower alkyl or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are joined form a piperidino or morpholino radical; R.sup.3 is hydrogen, lower alkanoyl, benzoyl, p-nitrobenzoyl, p-aminobenzoyl, p-chlorobenzoyl, isocyanoacetyl, or protected amino acyl radicals, for example, N-formylglycyl or ##STR2## (N-carbobenzoxyglycylglycyl); R.sup.4 is lower alkyl, CHR.sup.7 COOR.sup.8 or CH.sub.2 CH.sub.2 COOR.sup.8 wherein R.sup.7 is hydrogen or phenyl and R.sup.8 is hydrogen or lower alkyl; R.sup.5 is hydrogen or lower alkyl; or R.sup.4 and R.sup.5 together with the carbon atom to which they are joined form a cyclohexylidene radical; and R.sup.6 is a cyclohexyl or CHR.sup.9 COY wherein R.sup.9 is hydrogen or benzyl and Y is hydroxyl, lower alkoxy or amine, with the provisos that when Y is hydroxyl then R.sup.8 is hydrogen, that when Y is lower alkoxy than R.sup.8 is lower alkyl and that when Y is amino R.sup.4 is lower alkyl, are disclosed herein along with the related .alpha.-hydrazino-carboxamide and .alpha.-(.alpha.'-acylhydrazino)carboxamide compounds of formula III ##STR3## in which R.sup.1, R.sup.2, R.sup.3 , R.sup.5 and R.sup.7 are as defind above and Y is lower alkoxy. These compounds possess antibacterial activity. Methods for their preparation and use are disclosed also.

    Cyclohexylphenyl vasopressin agonists
    19.
    发明申请
    Cyclohexylphenyl vasopressin agonists 失效
    环己基苯基加压素激动剂

    公开(公告)号：US20060183734A1

    公开(公告)日：2006-08-17

    申请号：US11403072

    申请日：2006-04-11

    申请人： Amedeo Failli ,  Jay Shumsky ,  Thomas Caggiano ,  John Dusza ,  Kevin Memoli

    发明人： Amedeo Failli ,  Jay Shumsky ,  Thomas Caggiano ,  John Dusza ,  Kevin Memoli

    IPC分类号： A61K31/55 ,  C07D498/02

    CPC分类号： C07D471/04 ,  C07D243/14 ,  C07D471/14 ,  C07D487/04 ,  C07D495/04

    摘要： The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.

    摘要翻译： 本发明提供下列通式的化合物：其中Y是NR或 - （CH 2 CH 2）n。 R是H或烷基; “Z”表示任选取代的苯基或具有一个氮原子的6元芳环; “W”表示具有一个氮原子的任选取代的苯基或5元芳环; “X”表示具有一个硫原子的任选取代的5元芳环; 以及利用这些化合物诱导临时延迟排尿或治疗由加压素激动剂活性（包括尿崩症，夜间遗尿症，夜尿症，尿失禁或出血和凝血障碍）补救的病症的方法和药物组合物。

    Thiadiazolediamine derivative with histamine H-2 receptor inhibiting properties
    20.
    发明授权
    Thiadiazolediamine derivative with histamine H-2 receptor inhibiting properties 失效
    噻二唑二胺衍生物与组胺H-2受体的抑制性质

    公开(公告)号：US4529731A

    公开(公告)日：1985-07-16

    申请号：US534953

    申请日：1983-09-22

    申请人： Amedeo Failli ,  Luis Borella

    发明人： Amedeo Failli ,  Luis Borella

    IPC分类号： C07D285/10 ,  A61K31/445 ,  C07D417/12

    CPC分类号： C07D285/10

    摘要： N-[2-(dimethylamino)ethyl]-N'-[3-[3-[(1-piperidinyl)methyl]phenoxy]-propyl]-1,2,5-thiadiazole-3,4-diamine, 1-oxide is a long acting histamine H-2 receptor antagonist. The compound inhibits gastric acid secretion, and prevents and alleviates ulcers.

    摘要翻译： N- [2-（二甲基氨基）乙基] -N' - [3- [3 - [（1-哌啶基）甲基]苯氧基] - 吡喃基] -1,2,5-噻二唑-3,4-二胺，1 氧化物是长效组胺H-2受体拮抗剂。 该化合物可抑制胃酸分泌，并预防和缓解溃疡。