Silyl enol ether alkylation process
    2.
    发明授权
    Silyl enol ether alkylation process 失效
    甲硅烷基烯醇醚烷基化方法

    公开(公告)号:US5719275A

    公开(公告)日:1998-02-17

    申请号:US460546

    申请日:1995-06-02

    摘要: A method for preparing compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or a hydroxy-protecting group; R.sup.2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R.sup.3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR.sup.5 R.sup.6, where Y is oxygen or sulfur, and R.sup.5 and R.sup.6 are each alkyl, aryl or aralkyl, or R.sup.5 and R.sup.6 and the nitrogen to which they are attached together form a heterocyclic group; R.sup.4 is hydrogen or an amino-protecting group; and Z is sulfur or oxygen. The process comprises reacting a compound of formula (II): ##STR2## in which R.sup.8, R.sup.9 and R.sup.10 are the same or different and each represents an alkyl group having from 1 to 4 carbon atoms or a phenyl group, with a compound of formula (III): ##STR3## in which R.sup.11 represents an acyloxy, alkylsulfonyl, arylsulfonyl, alkylsulfinyl or arylsulfinyl group.

    摘要翻译: 制备式(I)化合物的方法:其中:R1是氢或羟基保护基; R 2是烷基,烷氧基,卤素,任选取代的苯基或任选取代的苯氧基; R3是任选取代的吡啶基,任选取代的具有式-CYNR 5 R 6的取代基的喹啉基或苯基,其中Y是氧或硫,R 5和R 6各自是烷基,芳基或芳烷基,或者R 5和R 6以及它们 一起形成杂环基; R4是氢或氨基保护基; Z是硫或氧。 该方法包括使式(II)化合物:其中R 8,R 9和R 10相同或不同并且各自表示具有1至4个碳原子的烷基或苯基的式(II)化合物与 式(III)化合物:其中R 11表示酰氧基,烷基磺酰基,芳基磺酰基,烷基亚磺酰基或芳基亚磺酰基。

    Carbapenem
    3.
    发明授权
    Carbapenem 失效
    卡巴培南

    公开(公告)号:US5614624A

    公开(公告)日:1997-03-25

    申请号:US460209

    申请日:1995-06-02

    摘要: A compound of the formula ##STR1## in which: R.sup.1' is hydrogen or a carboxy-protecting group;R.sup.41' is hydrogen or a hydroxy-protecting group;R.sup.42' is a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy, a halogen, an aryl or an aryloxy; R.sup.43' is hydrogen, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy, a hydroxy, a halogen, a cyano, a nitro or a group of the formula --NR.sup.8' R.sup.9', where R.sup.8' and R.sup.9' are independently selected from the group consisting of hydrogen, amino-protecting groups, C.sub.1 -C.sub.6 alkyl groups and phenyl groups, or R.sup.8' and R.sup.9' together represent a group --(CH.sub.2).sub.q '--O.sub.r '--(CH.sub.2).sub.s '--, where q' and s' are independently 0 or an integer of from 1 to 5 and r' is 0 or 1, provided that (q'+s') is an integer of at least 2; R.sup.45' and R.sup.46' are independently selected from the group consisting of C.sub.1 -C.sub.6 alkyl groups and aryl groups, or R.sup.45' and R.sup.46' together represent a group --(CH.sub.2).sub.q '--O.sub.r '--(CH.sub.2).sub.s '--, where q' and s' are independently 0 or an integer of from 1 to 5 and r' is 0 or 1; Y' is oxygen or sulfur; and j' is 0, 1 or 2.

    摘要翻译: 式(IV')的化合物,其中:R1'是氢或羧基保护基; R 41'是氢或羟基保护基; R 42'是C 1 -C 6烷基,C 1 -C 6烷氧基,卤素,芳基或芳氧基; R 43'是氢,C 1 -C 6烷基,C 1 -C 6烷氧基,羟基,卤素,氰基,硝基或式-NR 8'R 9'基团,其中R 8'和R 9'独立地选自 由氢,氨基保护基,C 1 -C 6烷基和苯基组成的组,或者R 8'和R 9'一起表示基团 - (CH 2)q'-Or' - (CH 2)s',其中q' 和s'独立地为0或1至5的整数,r'为0或1,条件是(q'+ s')为至少2的整数; R 45'和R 46'独立地选自C 1 -C 6烷基和芳基,或者R 45'和R 46'一起表示基团 - (CH 2)q'-Or' - (CH 2)s - ,其中 q'和s'独立地为0或1至5的整数,r'为0或1; Y'是氧或硫; 并且j'为0,1或2。

    Azetidinone compounds useful in the preparation of carbapenem
antibiotics and process for preparing carbapenem and penem compounds
    4.
    发明授权
    Azetidinone compounds useful in the preparation of carbapenem antibiotics and process for preparing carbapenem and penem compounds 失效
    可用于制备碳青霉烯类抗生素的氮杂环丁酮化合物及其制备碳青霉烯和青霉烯化合物的方法

    公开(公告)号:US5541317A

    公开(公告)日:1996-07-30

    申请号:US289133

    申请日:1994-08-11

    摘要: Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or a hydroxy-protecting group; R.sup.2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R.sup.3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR.sup.5 R.sup.6, where Y is oxygen or sulfur, and R.sup.5 and R.sup.6 are each alkyl, aryl or aralkyl, or R.sup.5 and R.sup.6 and the nitrogen to which they are attached together form a heterocyclic group; is R.sup.4 hydrogen or an amino-protecting group; and Z is sulfur or oxygen; are valuable intermediates in the preparation of carbapenem compounds and retain a desirable configuration during conversion to such carbapenem compounds. Penem and carbapenem compounds having a group of formula --SA' are prepared from a corresponding compound having a substituted thio, sulfinyl or sulfonyl group at this position by reaction with a compound A'SH (where A' is an organic group) in the presence of a salt of a metal of Group II or III of the Periodic Table.

    摘要翻译: 式(I)的化合物:其中:R1是氢或羟基保护基; R 2是烷基,烷氧基,卤素,任选取代的苯基或任选取代的苯氧基; R3是任选取代的吡啶基,任选取代的具有式-CYNR 5 R 6的取代基的喹啉基或苯基,其中Y是氧或硫,R 5和R 6各自是烷基,芳基或芳烷基,或者R 5和R 6以及它们 一起形成杂环基; 是R 4氢或氨基保护基; Z为硫或氧; 是制备碳青霉烯化合物的有价值的中间体,并且在转化成这种碳青霉烯化合物期间保留期望的构型。 在具有取代的硫代,亚磺酰基或磺酰基的相应化合物的化合物A'SH(其中A'为有机基团)的存在下,通过与化合物A'SH(其中A'为有机基团)反应,由具有取代的硫代,亚磺酰基或磺酰基的相应化合物制备具有式-SA'基团的Penem和carbapenem化合物 的元素周期表II或III族金属的盐。

    P38 kinase inhibiting agents
    5.
    发明授权
    P38 kinase inhibiting agents 有权
    P38激酶抑制剂

    公开(公告)号:US08513289B2

    公开(公告)日:2013-08-20

    申请号:US13266043

    申请日:2010-04-26

    CPC分类号: C07D417/12 C07D417/14

    摘要: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.

    摘要翻译: 由化学式(I)或其药学上可接受的盐描述的化合物:式(I); 是p38的抑制剂,可用于治疗炎症,例如治疗哮喘,COPD,ARDS,类风湿性关节炎,类风湿性脊椎炎,骨关节炎,痛风性关节炎和其他关节炎病症; 发炎关节,湿疹,牛皮癣或其他炎症皮肤病如晒伤; 炎症性眼病,包括结膜炎; 皮肤炎,疼痛等与炎症有关的病症。

    P38 KINASE INHIBITING AGENTS
    6.
    发明申请
    P38 KINASE INHIBITING AGENTS 有权
    P38激酶抑制剂

    公开(公告)号:US20120040999A1

    公开(公告)日:2012-02-16

    申请号:US13266043

    申请日:2010-04-26

    CPC分类号: C07D417/12 C07D417/14

    摘要: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.

    摘要翻译: 由化学式(I)或其药学上可接受的盐描述的化合物:式(I); 是p38的抑制剂,可用于治疗炎症,例如治疗哮喘,COPD,ARDS,类风湿性关节炎,类风湿性脊椎炎,骨关节炎,痛风性关节炎和其他关节炎病症; 发炎关节,湿疹,牛皮癣或其他炎症皮肤病如晒伤; 炎症性眼病,包括结膜炎; 皮肤炎,疼痛等与炎症有关的病症。

    Image output command method for image processing system
    7.
    发明授权
    Image output command method for image processing system 失效
    图像处理系统的图像输出命令方法

    公开(公告)号:US5086497A

    公开(公告)日:1992-02-04

    申请号:US600280

    申请日:1990-10-22

    IPC分类号: G06T11/60

    CPC分类号: G06T11/60

    摘要: An image output command method, in an image processing system comprising an input controller to dot and compress density or tone data for an image read out by an input unit and for temporarily staying the compressed image data at a buffer; a work station to picture-edit not only a code information edited by an editing input unit but also the image data by the use of an input operating means and a display means; a file server connected to the input controller and the work station by bus lines and for storing the image data, code information and edited data picture-edited by the work station in the file server; and an image setter for reading out the edited data stored in the file server and subjecting the edited data to a required data processing, which comprises the steps of: reading out the stored data from the file server, separating respective image data which constitute one page and commands which edit respective images when the images are transferred to the image output unit via the image setter and are outputted, and separating the data of a unit of one page to blocks and sub-blocks thereby to control image portions by output position and processing method.