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72 条记录 (耗时 0.019 秒)

    MALONAMIDE DERIVATIVES BLOCKING THE ACTIVTIY OF GAMMA-SECRETASE
    33.
    发明授权
    MALONAMIDE DERIVATIVES BLOCKING THE ACTIVTIY OF GAMMA-SECRETASE 有权
    γ-分泌BLOCKING MALONAMIDDERIVATE的活动

    公开(公告)号：EP1711470B1

    公开(公告)日：2009-04-15

    申请号：EP04764665.8

    申请日：2004-08-31

    申请人： F. Hoffmann-La Roche AG

    发明人： FLOHR, Alexander ,  GALLEY, Guido ,  JAKOB-ROETNE, Roland ,  KITAS, Eric, Argirios ,  PETERS, Jens-Uwe ,  WOSTL, Wolfgang

    IPC分类号： C07D223/18 ,  C07D223/16 ,  C07D243/14 ,  C07D313/14 ,  A61K31/5513 ,  A61K31/55

    CPC分类号： C07D223/16 ,  A61K31/335 ,  A61K31/55 ,  A61K31/5513 ,  C07D223/20 ,  C07D243/24 ,  C07D273/00 ,  C07D313/14

    摘要： The invention relates to malonamide derivatives of formula (I), wherein: R1 is one of the following groups (Formulae a), b), c), d)); R2 is lower alkyl, lower alkinyl, -(CH2)n-O-lower alkyl, -(CH2)n-S-lower alkyl, -(CH2)n-CN, -(CR'R')n-CF3, -(CR'R')n-CHF2, -(CR'R')n-CH2F, -(CH2)n-C(O)O-lower alkyl, -(CH2)n-halogen, or is -(CH2)n-cycloalkyl, optionally substituted by one or more substituents, selected from the group consisting of phenyl, halogen or CF3; R',R' are independently from n and from each other hydrogen, lower alkyl, lower alkoxy, halogen or hydroxy; R3, R4 are independently from each other hydrogen, lower alkyl, lower alkoxy, phenyl or halogen; R5 is hydrogen, lower alkyl, -(CH2)n-CF3 or -(CH2)n-cycloalkyl; R6 is hydrogen or halogen; R7 is hydrogen or lower alkyl; R8 is hydrogen, lower alkyl, lower alkinyl, -(CH2)n-CF3,-(CH2)n-cycloalkyl or -(CH2)n-phenyl, optionally substituted by halogen; R9 is hydrogen, lower alkyl, -C(O)H, -C(O)-lower alkyl, -C(O)-CF3,-C(O)-CH2F,-C(O)-CHF2,-C(O)-cycloalkyl,-C(O)-(CH2)n-O-lower alkyl,-C(O)O-(CH2)n-cycloalkyl, -C(O)-phenyl, optionally substituted by one or more substituents selected from the group consisting of halogen or -C(O)O-lower alkyl, or is -S(O)2-lower alkyl, -S(O)2-CF3,-(CH2)n-cycloalkyl or is -(CH2)n-phenyl, optionally substituted by halogen; n is 0, 1, 2, 3 or 4; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixture thereof. These compounds may be used for the treatment of Alzheimer's disease.

    METHOD FOR PRODUCING BENZAZEPINONE
    34.
    发明公开
    METHOD FOR PRODUCING BENZAZEPINONE 审中-公开
    VERFAHREN ZUR HERSTELLUNG VON BENZAZEPINON

    公开(公告)号：EP1985615A1

    公开(公告)日：2008-10-29

    申请号：EP07707779.0

    申请日：2007-01-31

    申请人： API Corporation

    发明人： UEHARA, Hisatoshi

    IPC分类号： C07D223/16 ,  C07C249/04 ,  C07C251/48 ,  C07D217/26 ,  C07D223/18

    CPC分类号： C07C249/12 ,  C07C249/02 ,  C07D217/26 ,  C07D221/12 ,  C07D223/16 ,  C07D223/18 ,  C07C251/24 ,  C07C251/48

    摘要： It is an object of the present invention to provide 2-iminocarboxylic acid derivatives, and a practically suitable industrial method for producing benzazepinones in a short process under mild conditions. The present invention provides a method for producing a benzazepinone or a salt thereof, which comprises opening a ring of an isoquinoline derivative and subsequently converting the thus generated amine into a benzazepinone through lactamization reaction.

    摘要翻译： 本发明的目的是提供2-亚氨基羧酸衍生物，以及在温和条件下在短时间内生产苯并氮杂酮的实际合适的工业方法。 本发明提供一种苯并氮杂酮或其盐的制备方法，其包括打开异喹啉衍生物的环，随后通过内酰胺化反应将由此产生的胺转化为苯并氮杂酮。

    OPTICALLY ACTIVE AMMONIUM SALT COMPOUND, PRODUCTION INTERMEDIATE THEREOF AND METHOD FOR PRODUCING SAME
    35.
    发明公开
    OPTICALLY ACTIVE AMMONIUM SALT COMPOUND, PRODUCTION INTERMEDIATE THEREOF AND METHOD FOR PRODUCING SAME 有权
    光有源铵盐化合物，中间体，其制造的生产和方法

    公开(公告)号：EP1854796A1

    公开(公告)日：2007-11-14

    申请号：EP06715174.6

    申请日：2006-03-03

    申请人： Kyoto University ,  NIPPON SODA CO., LTD.

    发明人： MARUOKA, Keiji c/o Kyoto Univ. Graduate School ,  KUBOTA, Yasushi

    IPC分类号： C07D487/10 ,  C07D223/18 ,  C07C25/18 ,  C07C43/225 ,  C07B53/00

    CPC分类号： B01J31/0271 ,  C07B53/00 ,  C07B2200/07 ,  C07C22/04 ,  C07C25/18 ,  C07C33/46 ,  C07C43/225 ,  C07D223/18 ,  C07D487/10

    摘要： An optically active quaternary ammonium salt compound represented by formula (1),

    wherein R 1 represents a halogen, a C 1-8 alkyl which is optionally substituted and which is linear, branched, or cyclic, a C 2-8 alkenyl which is optionally substituted, a C 2-8 alkynyl which is optionally substituted, a C 6-14 aryl which is optionally substituted, a C 3-8 heteroaryl which is optionally substituted, a C 1-8 alkoxy which is optionally substituted and which is linear, branched, or cyclic, or a C 7-16 aralkyl which is optionally substituted;
    R 2 and R 21 each independently represents hydrogen, halogen, nitro, a C 1-8 alkyl which is optionally substituted and which is linear, branched, or cyclic, a C 2-8 alkenyl which is optionally substituted, a C 2-8 alkynyl which is optionally substituted, a C 6-14 aryl which is optionally substituted, a C 1-8 alkoxy which is optionally substituted and which is linear, branched, or cyclic, or a C 7-16 aralkyl which is optionally substituted;
    one of combinations of R 1 and R 21 , and R 2 and R 21 , may bond to form a C 1-6 alkylene which is optionally substituted, a C 1-6 alkylenemonooxy which is optionally substituted, or a C 1-6 alkylenedioxy which is optionally substituted;
    R 3 and R 4 each independently represents hydrogen, a C 6-14 aryl which is optionally substituted, a C 3-8 heteroaryl which is optionally substituted, or a C 7-16 aralkyl which is optionally substituted, with a proviso that R 3 and R 4 are not hydrogen at the same time;
    R 5 represents hydrogen, halogen, a C 1-8 alkyl which is optionally substituted and which is linear, branched, or cyclic, a C 1-8 alkoxy which is optionally substituted and which is linear, branched, or cyclic, a C 2-8 alkenyl which is optionally substituted, or a C 2-8 alkynyl which is optionally substituted;
    R 6 represents halogen, a C 1-8 alkyl which is optionally substituted and which is linear, branched, or cyclic, a C 1-8 alkoxy which is optionally substituted and which is linear, branched, or cyclic, a C 2-8 alkenyl which is optionally substituted, or a C 2-8 alkynyl which is optionally substituted, and R 5 and R 6 may bond to form an aromatic ring which is optionally substituted;
    ring A and ring B do not have a same substituent at the same time;
    symbols * and ** represent an optical activity having an axial chirality; and
    X - represents an anion.

    摘要翻译： 由式表示的光学活性季铵盐化合物（1），worin R 1代表卤素，C 1-8烷基，其任选substituiertem和其是直链，支链，或环状的，一个C 2-8链烯基，其任选 取代的，一个C 2-8炔基，其任选substituiertem，一个C 6-14芳基，其是任选substituiertem，一个C 3-8杂芳基，其任选substituiertem，一个C 1-8烷氧基，其任选substituiertem并且是线性的， 支链的，或环状的，或C 7-16芳烷基，其任选substituiertem; R 2和R 21各自独立地darstellt氢，卤素，硝基，C 1-8烷基，其任选substituiertem和其是直链，支链，或环状的，一个C 2-8链烯基，其任选substituiertem，一个C 2-8 炔基，其任选substituiertem，一个C 6-14芳基，其是任选substituiertem，一个C 1-8烷氧基，其任选substituiertem和其是直链，支链，或环状的，或C 7-16芳烷基，其任选substituiertem; R 1和R 21的组合中的一个，和R 2和R 21可以键合形成C 1-6亚烷基，其任选substituiertem，一个C 1-6 alkylenemonooxy其任选substituiertem，或C 1-6亚烷基二 所有这一切都为任选substituiertem; R 3和R 4各自独立地darstellt氢，C 6-14芳基，其任选substituiertem，一个C 3-8杂芳基，其任选substituiertem，或C 7-16芳烷基，其任选substituiertem，具有做，R 3一条件 和R 4不同时为氢; 的R 5为氢darstellt，卤素，C 1-8烷基，其任选substituiertem和其是直链，支链，或环状的，一个C 1-8烷氧基，其任选substituiertem和其是直链，支链，或环状的，C 2至 -8链烯基，其任选substituiertem，或C 2-8炔基，其任选substituiertem; -R 6 darstellt卤素，C 1-8烷基，其任选substituiertem和其是直链，支链，或环状的，一个C 1-8烷氧基，其任选substituiertem和其是直链，支链，或环状的，一个C 2-8 链烯基，其任选substituiertem，或C 2-8炔基，其任选substituiertem，和R 5和R 6可以键合形成在芳香环，其任选substituiertem; 环A和环B不具有在在Sametime一个相同的取代基; 符号*和**表示在具有在轴向手性光学活性; 和X - 阴离子的darstellt。

    NEW CRYSTAL FORMS OF OXCARBAZEPINE AND PROCESSES FOR THEIR PREPARATION
    36.
    发明公开
    NEW CRYSTAL FORMS OF OXCARBAZEPINE AND PROCESSES FOR THEIR PREPARATION 审中-公开
    奥卡西平与方法新的晶体形态及其

    公开(公告)号：EP1368322A2

    公开(公告)日：2003-12-10

    申请号：EP02718948.9

    申请日：2002-02-12

    申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD.

    发明人： ARONHIME, Judith ,  DOLITZKY, Ben-Zion ,  BERKOVICH, Yana ,  GARTH, Nissim

    IPC分类号： C07D223/18 ,  A61K31/55 ,  A61P25/08

    CPC分类号： C07D223/22

    摘要： The present invention provides for new crystal forms of oxcarbazepine, more particularly oxcarbazepine Forms B, C, D and E. The present invention further provides processes for preparation of these forms. Form B is prepared by evaporating the solvents from a solution of oxcarbazepine in toluene and dichloromethane. Form B is also obtained by immediately cooling the solution of oxcarbazepine and toluene. Cooling the same solution at a slower rate, but still fairly rapidly, results in oxcarbazepine Form C. Cooling th same solution at even a slower rate results in another Form, oxcarbazepine Form D. Oxcarbazepine Form E, a solvate of chloroform, is obtained by precipitating a solution of oxcarbazepine and chloroform. The present invention also provides processes for converting one of the newly discovered crystal forms of oxcarbazepine into another crystal form, including Form A, which is in the prior art. These conversions may occur by storage at ambient temperature, by heating one particular Form or treatment with a protic solvent.

    New amidino tricycle derivatives
    38.
    发明公开
    New amidino tricycle derivatives 失效
    新的脒三环衍生物

    公开(公告)号：EP0309422A3

    公开(公告)日：1990-01-10

    申请号：EP88830374.0

    申请日：1988-09-19

    申请人： ISTITUTO DE ANGELI S.p.A.

    发明人： Turconi, Marco ,  Donetti, Arturo ,  Cereda, Enzo ,  Quintero, Myrna Gil ,  Schiavi, Giovanni Battista ,  Micheletti, Rosamaria

    IPC分类号： C07D471/04 ,  C07D223/26 ,  C07D223/18 ,  C07D243/38 ,  C07D495/04 ,  C07D403/06 ,  C07D401/06 ,  C07D451/00 ,  C07D519/00 ,  C07D405/06 ,  C07D403/12

    CPC分类号： C07D451/02 ,  C07D223/20 ,  C07D223/26 ,  C07D223/28 ,  C07D243/38 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D471/04 ,  C07D495/04

    摘要： New pharmacologically active amidino tricycle derivatives as muscarinic receptor blocking agents, useful for the treatment of gastrointestinal disorders of the following formula:
    wherein
    R represents a hydrogen atom or a halogen atom
    X represents nitrogen or -CH-group
    W represents a -NH-CO-, -CH=CH-, -CH₂-CH₂- group, oxygen or sulfur
    R₁ represents a hydrogen atom or a C₁₋₄ alkyl group
    n is 0 or 1
    Y represents sulfur or a -CH- group
    A represents carbon or nitrogen
    B represents a -CH- group (provided that A is different from nitrogen), -COO-, -CO-, or -CH₂- group
    m is 0 or an integer from 1 to 3
    Z represents -NH-, -CO-, -COO- or -CH- group, or it is absent
    p is 0 or 1
    Het represents piperazinyl, homopiperazinyl, piperidinyl, tropyl or tetrahydropirimidinyl group, each group being optionally substituted by a C₁₋₄ alkyl group or an amino group
    q is 0 or 1
    R₂ represents a hydrogen atom, a C₁₋₄ alkyl group or an amino group optionally substituted by a linear or branched C₁₋₄ alkyl group or phenyl group
    R₃ represents a linear or branched C₁₋₈alkyl group or a hydrogen atom (provided that the bond between Het and the group
    is a carbon- carbon bond or A=C and B=CH), or
    R₂ and R₃ may join together to form a heterocyclic 5-membered ring, tautomers thereof and acid addition salts of the aforesaid compounds. The process for the preparation of the compounds of formula (I) as well as pharmaceuticals compositions containing them are also described.

    摘要翻译： 作为毒蕈碱受体阻断剂的新药理活性脒基三环衍生物，可用于治疗下式的胃肠道病症：其中R表示氢原子或卤素原子，X表示氮或-CH-基，W表示-NH-CO- ，-CH = CH-，-CH 2 -CH 2 - 基，氧或硫R 1代表氢原子或C 1-4烷基，n是0或1，Y代表硫或-CH-基团，A代表碳或氮，B代表 -CH-基团（条件是A与氮不同），-COO - ， - CO-或-CH 2 - 基团m为0或1至3的整数Z表示-NH - ， - CO - ， - COO - 或-CH-基团，或不存在p是0或1 Het代表哌嗪基，高哌嗪基，哌啶基，tropyl或四氢嘧啶基，每个基团任选被C 1-4烷基或氨基取代，q为0或1 R 2代表氢原子，C 1-4烷基或任选被直链或支链取代的氨基 C 1 -C 4烷基或苯基R 3代表直链或支链C 1-8烷基或氢原子（条件是Het和该基团之间的键是碳 - 碳键或A = C和B = CH），或 R 2和R 3可以连接在一起形成杂环5元环，其互变异构体和前述化合物的酸加成盐。 还描述了制备式（I）化合物的方法以及含有它们的药物组合物。