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67 条记录 (耗时 0.018 秒)

    C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
    1.
    发明申请
    C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases 有权
    C末端修饰（N-取代的）-2-吲哚基二肽作为ICE / ced-3家族半胱氨酸蛋白酶的抑制剂

    公开(公告)号：US20020025935A1

    公开(公告)日：2002-02-28

    申请号：US09747317

    申请日：2000-12-20

    发明人： Donald S. Karanewsky ,  Xu Bai

    IPC分类号： A61K031/675 ,  A61K031/404 ,  A61K038/05 ,  C07D29/20

    CPC分类号： C07K5/0202 ,  A61K38/00

    摘要： This invention is directed to novel (N-substituted) indole ICE/ced-3-inhibitor compounds. The invention is also directed to pharmaceutical compositions of such indole compounds, plus the use of such compositions in the treatment of patients suffering inflammatory. autoimmune and neurodegenerative diseases, for the prevention of ischemic injury.

    摘要翻译： 本发明涉及新的（N-取代的）吲哚ICE / ced-3抑制剂化合物。 本发明还涉及这种吲哚化合物的药物组合物，以及这些组合物在治疗患有炎症的患者中的用途。 自身免疫和神经退行性疾病，用于预防缺血性损伤。

    Neo-tryptophan
    2.
    发明申请
    Neo-tryptophan 审中-公开
    新色氨酸

    公开(公告)号：US20010027174A1

    公开(公告)日：2001-10-04

    申请号：US09755638

    申请日：2001-01-05

    申请人： Mayo Foundation for Medical Education and Research Minnesota corporation

    发明人： Elliott Richelson ,  Bernadette Marie Cusack ,  Yuan-Ping Pang ,  Daniel J. McCormick ,  Abdul Fauq ,  Beth Marie Tyler ,  Mona Boules

    IPC分类号： A61K038/10 ,  C07D29/20 ,  C07K014/00

    CPC分类号： C07K7/083 ,  A61K38/00 ,  C07D209/08 ,  C07K7/14 ,  C07K7/18 ,  C07K14/70 ,  C07K14/702

    摘要： The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.

    摘要翻译： 本发明提供了新的氨基酸，新色氨酸，以及含有这种新型氨基酸的多肽，如神经降压素类似物。 此外，本发明提供新色氨酸衍生物，5-羟色胺样新色氨酸衍生物和含有这些衍生物的多肽。 本发明还提供了制备新色氨酸，新色氨酸衍生物，血清素样新色氨酸衍生物和含有这些化合物的组合物的方法。 此外，本发明提供了在哺乳动物中诱导神经降压素反应的方法以及用于治疗具有5-羟色胺识别分子的哺乳动物的方法。

    3-(5,7-dimethyl-2-hydroxy-4-oxo-6,8-decadienyl)-glutarimide
    4.
    发明授权
    3-(5,7-dimethyl-2-hydroxy-4-oxo-6,8-decadienyl)-glutarimide 失效
    3-（5,7-二甲基-2-羟基-4-氧代-6,8-十二烷基） - 葡萄糖苷

    公开(公告)号：US3880858A

    公开(公告)日：1975-04-29

    申请号：US39199673

    申请日：1973-08-27

    申请人： MITSUBISHI CHEM IND

    发明人： ISHIDA NAKAO ,  OKADA TSUTOMU ,  KAMATA AKIRA

    IPC分类号： C12P1/06 ,  A61K31/445 ,  A61K35/74 ,  C07D211/88 ,  C07G11/00 ,  C12R1/465 ,  C07D29/20

    CPC分类号： A61K31/445 ,  C07D211/88 ,  Y10S435/886

    摘要： 3-(5,7-Dimethyl-2-hydroxy-4-oxo-6,8-decadienyl)-glutarimide is prepared by cultivating Streptomyces pluricolorescens var. yamashitaensis (S-885) ATCC No. 21956 in an aqueous nutrient broth containing a carbohydrate and a source of organic nitrogen until said broth achieves substantial antiviral activity, and recovering said antibiotic from said culture broth.

    摘要翻译： 3-（5,7-二甲基-2-羟基-4-氧代-6,8-十二烯基） - 戊二酰亚胺通过培养多孢菌链霉菌（Streptomyces pluricolorescens var。 在含有碳水化合物和有机氮源的含水营养肉汤中，直到所述肉汤获得显着的抗病毒活性，并从所述培养液中回收所述抗生素后，将所述抗氧化剂（S-885）ATCC号21956。

    Gamma-piperidinobutyrophenones
    5.
    发明授权
    Gamma-piperidinobutyrophenones 失效
    氨基哌啶酮

    公开(公告)号：US3799932A

    公开(公告)日：1974-03-26

    申请号：US12452271

    申请日：1971-03-15

    申请人： SUMITOMO CHEMICAL CO

    发明人： YAMAMOTO H ,  MARUYAMA I ,  KATAYAMA S ,  NAKAO M ,  SASAJIMA K

    IPC分类号： C07D211/48 ,  C07D211/52 ,  C07D401/04 ,  C07D29/20

    CPC分类号： C07D401/04 ,  C07D211/48 ,  C07D211/52

    摘要： A NOVEL PROCESS FOR PREPARING CENTRAL NERVOUS SYSTEM ACTIVE BUTYROPHENONE DERIVATIVES IN WHICH V-PIPERDINOBUTROPHENONE DERIVATIVES OF THE FORMULA

    1-((4-R3,4-R4-PIPERIDINO)-CH2-CH2-CH2-CO-),2-R1,R2-BENZENE

    WHEREIN R1 IS HYDROGEN, HALOGEN AMINO, ACYLAMINO, ALKYLAMINO OR N-ACYLALKYLAMINO; R2 IS HYDROGEN OR HALOGEN; R3 IS HYDROGEN OR HYDROXYL; AND R4 IS A GROUP HAVING THE FORMULA,

    (RA,RB-PHENYL)-(CH2)N-

    WHEREIN EACH OR RA AND RB IS HYDROGEN, HALOGEN, LOWER ALKYL, LOWER ALKOXY OR TRIFLUOROMETHYL; AND N IS 1 OR 2), OR A GROUP HAVING THE FORMULA,

    1-RC,2-(O=),RD,RE-2,3-DIHYDROBENZIMIDAZOL-3-YL

    (WHEREIN RC IS HYDROGEN OR LOWER ALKYL; AND EACH OR RD AND RE IS HYDROGEN, HALOGEN, LOWER ALKYL OR LOWER ALKOXY), CAN BE PREPARED BY REACTING AN INDOLE DERIVATIVE OF THE FORMULA

    1-R5,2-R6,3-((4,4-DI(R3-)PIPERIDINO)-CH2-CH2-CH2-),R2-

    WHEREIN R2, R3 AND R4 ARE THE SAME AS DEFINED ABOVE, AND R5 AND R6 ARE HYDROGEN OR ALKYL HAVING UP TO 4 CARBON ATOMS RESPECTIVELY, WITH AN OXIDIZING AGENT TO YIELD AN O-ACYLAMINO-Y-PIPERIDINOBUTYPROPHENONE DERIVATIVE OF THE FORMULA, 1-((4-R3,4-R4-PIPERIDINO)-(CH2)3-CO-),2-(R6-CO-N(-R5)-), WHEREIN R2, R3, R4, R5 AND R6 ARE THE SAME AS DEFINED ABOVE, AND FURTHER, IF NECESSARY, HYDROLYZING THE PRODUCT TO YIELD AN O-AMINO-Y-PIPERIDINOBUTYROPHENONE DERIVATIVE OF THE FORMULA, 1-((4-R3,4-R4-PIPERIDINO)-(CH2)3-CO-),2-(R5-NH-),R2-BENZENE INDOLE R2-BENZENE WHEREIN R2, R3, R4 AND R5 ARE THE SAME AS DEFINED ABOVE, AND FURTHER DIAZOTIZING, IF DESIRED, IN CASE R5 IS HYDROGEN, THE OBTAINED O-AMINO-Y-PIPERIDINOBUTYROPHENONE DERIVATIVE AND SUBSEQUENTLY DECOMPOSING THE RESULTANT DIAZONIUM COMPOUND TO REPLACE THE DIAZONIUM GROUP BY HYDROGEN OR HALOGEN. AMONG THE BUTYROPHENONE DERIVATIVES THUS OBTAINED, THOSE IN WHICH R1 IS HALOGEN, AMNIO, ACYLAMINO, ALKYLAMINO OR N--ACYAKYLAMINO ARE NOVEL COMPOUNDS.

    2-methylene glutarimide and process for preparing the same
    6.
    发明授权
    2-methylene glutarimide and process for preparing the same 失效
    2-甲基谷氨酰胺及其制备方法

    公开(公告)号：US3720679A

    公开(公告)日：1973-03-13

    申请号：US3720679D

    申请日：1971-01-18

    申请人： NAT DISTILLERS CHEM CORP

    发明人： FELDMAN J ,  THOMAS M

    IPC分类号： C07D211/88 ,  C07D29/20

    CPC分类号： C07D211/88

    摘要： A process is provided for the preparation of alpha-substituted unsaturated aliphatic diamides and alpha-substituted unsaturated aliphatic imides from the corresponding dinitriles, employing an amount of water within the range from about 50 mole percent to about 200 mole percent of that stoiciometrically required to hydrolyze the dinitrile to the diamide, and wherein the acid concentration is within the range of 40 percent to 82 percent, at a temperature within the range of about 0* to 150*C., in the presence of an inorganic or organic acid and in a homogeneous reaction medium. The hydrolysis is arrested, preferably by neutralization. Diamides are obtained preferentially by neutralizing the mixture at temperatures below about 30* C. Cyclic imides are obtained preferentially by neutralizing the acid hydrolysis mixture at elevated temperatures above about 60* C. The products formed by neutralization at intermediate temperatures are mixtures of the two products.

    摘要翻译： 提供了一种从相应的二腈制备α-取代的不饱和脂族二酰胺和α-取代的不饱和脂族酰亚胺的方法，其中使用一定量的水，其水解所需要的约50摩尔％至约200摩尔％ 二腈与二酰胺，并且其中酸浓度在40％至82％的范围内，在约0℃至150℃的温度范围内，在无机或有机酸存在下，并且在 均相反应介质。 水解被阻止，优选通过中和。