Derivatives of (1-hydroxy-2-piperidylalkyl-indol-2-ones, 2-quinolinones,
2-benzo(B)azapinones, benzimidazol-2-ones, and quinazolin-2-ones, their
preparation and their application in therapeutics
    5.
    发明授权
    Derivatives of (1-hydroxy-2-piperidylalkyl-indol-2-ones, 2-quinolinones, 2-benzo(B)azapinones, benzimidazol-2-ones, and quinazolin-2-ones, their preparation and their application in therapeutics 失效
    (1-羟基-2-哌啶基烷基 - 吲哚-2-酮,2-喹啉酮,2-苯并(B)吖庚因酮,苯并咪唑-2-酮和喹唑啉-2-酮的衍生物,其制备及其在治疗中的应用

    公开(公告)号:US5034401A

    公开(公告)日:1991-07-23

    申请号:US378094

    申请日:1989-07-11

    CPC分类号: C07D401/06 C07D401/14

    摘要: A compound, in the form of a pure optical isomer or a mixture thereof, of formula (I): ##STR1## in which: Z represents a group of formula --CH.sub.2 --, --C(CH.sub.3).sub.2 --, --CH.dbd.CH--, --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --NH-- or --N(CH.sub.3)CH.sub.2 --, in which the nitrogen is bonded to the carbonyl group;R1 represents hydrogen or a C.sub.1 -C.sub.4 alkyl group;R2 represents hydrogen or a methyl group; andR3 represents:a phenoxy group which is unsubstituted or substituted by a halogen or a methyl group,a naphthyloxy group,a phenylmethyl group substituted by a halogen or a methyl group,an unsubstituted phenylmethyl group when Z does not representa group of formula --CH.dbd.CH-- or --(CH.sub.2).sub.2 --,a bis (4-fluorophenyl)-methyl group,a phenylmethoxy group which is unsubstituted or substituted by a halogen or a methyl group,a (2-naphthyl)methoxy group,a phenoxymethyl group which is unsubstituted or substituted by a halogen or a methyl group, ora pyridinyloxy group, andR4 represents hydrogen; orR3 and R4 form, together and with the piperidine ring to which they are attached, a spiro (2,3-dihydrobenzofuran-2,4'-piperid-1-yl) group; or a pharmacologically acceptable acid addition salt thereof.

    摘要翻译: 式(I)的纯旋光异构体或其混合物形式的化合物:其中:Z表示式-CH 2 - , - C(CH 3)2 - , - CH = CH - , - (CH 2)2 - , - (CH 2)3 - , - NH-或-N(CH 3)CH 2 - ,其中氮键合到羰基上; R1表示氢或C1-C4烷基; R2表示氢或甲基; R3表示:未被取代或被卤素或甲基取代的苯氧基,萘氧基,被卤素或甲基取代的苯基甲基,当Z不表示式 - CH = CH-或 - (CH 2)2 - ,双(4-氟苯基) - 甲基,未被取代或被卤素或甲基取代的苯基甲氧基,(2-萘基)甲氧基,苯氧基甲基 未取代或被卤素或甲基取代的基团,或吡啶氧基,R4表示氢; 或者R 3和R 4与它们所连接的哌​​啶环一起形成螺(2,3-二氢苯并呋喃-2,4'-哌啶-1-基)基团; 或其药理学上可接受的酸加成盐。

    Process for the preparation of pyridinyl and pyrimidinyl mono-fluorinated beta keto-esters
    7.
    发明授权
    Process for the preparation of pyridinyl and pyrimidinyl mono-fluorinated beta keto-esters 有权
    制备吡啶基和嘧啶基单氟化β-酮酯的方法

    公开(公告)号:US07135569B2

    公开(公告)日:2006-11-14

    申请号:US11221023

    申请日:2005-09-07

    申请人: Jonathan Frost

    发明人: Jonathan Frost

    IPC分类号: C07D239/26 C07D213/127

    CPC分类号: C07D239/26 C07D213/55

    摘要: The present invention relates to a process for preparing pyridinyl and pyrimidinyl mono-fluorinated beta keto esters of formula (I): wherein: R1 represents a pyridine ring or a pyrimidine ring, the rings being optionally substituted by a C3-6 cycloalkyl group, a C1-4 alkyl group, a C1-4 alkoxy group, a benzyl group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group or ahalogenatom; and R3 represents a C1-6 alkyl group; by reacting with fluorine a compound of formula (II) wherein R1, R2 and R3 have the same meaning as defined above.

    摘要翻译: 本发明涉及制备式(I)的吡啶基和嘧啶基单氟化β-酮酯的方法:其中:R1表示吡啶环或嘧啶环,该环任选被C 3-6 C 1-4烷基,C 1-4烷氧基,苄基或卤素原子; C 1-4烷基,C 1-4烷基,C 1-4烷基, R 2表示氢原子,C 1-6烷基或卤素原子; 并且R 3表示C 1-6烷基; 通过与氟反应,其中R 1,R 2和R 3具有与上述相同的含义的式(Ⅱ)化合物。

    Quinolinone derivatives and their preparation in therapy
    8.
    发明授权
    Quinolinone derivatives and their preparation in therapy 失效
    喹啉酮衍生物及其在治疗中的应用

    公开(公告)号:US4983607A

    公开(公告)日:1991-01-08

    申请号:US417970

    申请日:1989-10-10

    CPC分类号: C07D215/227 C07D401/12

    摘要: A quinolinone derivative which is a compound of formula (I): ##STR1## in which: R.sub.1 and R.sub.2 are each, independently of one another, a hydrogen or halogen atom or a (C.sub.1-4)alkyl radical;R.sub.3 is a hydrogen atom or a (C.sub.1-4)alkyl radical;R.sub.4 is an unsubstituted or substituted naphthyl, tetrahydronaphthyl, benzyl, phenyl, pyridyl, isoquinolyl or benzoyl radical; and X and Y are each a hydrogen atom or together form a bond; or a pharmaceutically acceptable acid addition salt thereof and, when X and Y are each a hydrogen atom, the diastereoisomers and enantiomers thereof.

    摘要翻译: 作为式(I)化合物的喹啉酮衍生物:其中:R 1和R 2各自独立地为氢或卤素原子或(C 1-4)烷基; R3是氢原子或(C1-4)烷基; R4是未取代或取代的萘基,四氢萘基,苄基,苯基,吡啶基,异喹啉基或苯甲酰基; X和Y各自为氢原子或一起形成键; 或其药学上可接受的酸加成盐,当X和Y各自为氢原子时,其非对映异构体和对映异构体。

    Ensuring accurate measurements for soft proofing system
    10.
    发明申请
    Ensuring accurate measurements for soft proofing system 审中-公开
    确保软打样系统的准确测量

    公开(公告)号:US20050036162A1

    公开(公告)日:2005-02-17

    申请号:US10815096

    申请日:2004-03-31

    CPC分类号: H04N1/6011

    摘要: Techniques for providing accurate output measurement and calibration in soft proofing systems incorporate one or more features to promote controlled viewing conditions. For example, a soft proofing system is described in which an administrator can control the proofing process by limiting or restricting the ability to view an image until acceptable viewing conditions have been met. For example, the ability to view the image can be restricted until the viewing station has been calibrated using a calibration device known to support calibration of the viewing station to less than or equal to a maximum magnitude of error. With controlled viewing conditions and, more particularly, controlled calibration conditions, the soft proof reviewers obtain more uniform output. In this manner, the system can provide safeguards to ensure that the images viewed at the viewing station have acceptable color accuracy.

    摘要翻译: 用于在软打样系统中提供精确的输出测量和校准的技术包含一个或多个特征以促进受控的观察条件。 例如,描述了一种软打样系统,其中管理员可以通过限制或限制在满足可接受的观看条件之前查看图像的能力来控制打样过程。 例如,可以限制观看图像的能力,直到观察站已经使用已知支持观察站的校准的校准装置校准为小于或等于最大误差大小。 具有受控的观察条件,更具体地,控制的校准条件,软证明审查者获得更均匀的输出。 以这种方式,系统可以提供保护以确保在观察站观看的图像具有可接受的颜色精度。