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9 条记录 (耗时 0.034 秒)

    Nitro-sulfobenzamides
    2.
    发明申请
    Nitro-sulfobenzamides 有权
    硝基磺基苯甲酰胺

    公开(公告)号：US20010020092A1

    公开(公告)日：2001-09-06

    申请号：US09732006

    申请日：2000-12-07

    发明人： Mark James Ford ,  Jan Vermehren

    IPC分类号： C07D211/38 ,  C07D27/12 ,  C07D25/04 ,  C07D23/06

    CPC分类号： C07C303/38 ,  C07C303/22 ,  C07C309/59 ,  C07C311/65 ,  C07D239/52 ,  C07D327/04 ,  C07C311/16 ,  C07C309/89

    摘要： The present invention relates to a compound of the formula (I) 1 wherein R1 is an unsubstituted or substituted hydrocarbon radical having a total of 1 to 10 carbon atoms, preferably 1 to 6 carbon atoms, R2 is an unsubstituted or substituted hydrocarbon radical having a total of 1 to 10 carbon atoms, preferably 1 to 6 carbon atoms, or the group NR1R2 is a heterocyclic ring having 3 to 8 ring atoms which is unsubstituted or substituted and contains the nitrogen atom of the group NR1R2 as ring heteroatom and may also contain one or two further ring heteroatoms from the group consisting of N, O and S, and Q is H or a cation. The compounds of the present invention can advantageously be used for the preparation of sulfonylureas and their precursors such as sulfochlorides or sulfonamides.

    摘要翻译： 本发明涉及式（I）化合物，其中R 1是总共具有1至10个碳原子，优选1至6个碳原子的未取代或取代的烃基，R 2是未取代或取代的烃基，其具有总计 1〜10个碳原子，优选1〜6个碳原子，或者NR1R2是具有3〜8个环原子的杂环，其未被取代或取代，并且含有NR1R2基团的氮原子作为环杂原子，并且还可以含有一个 或另外两个来自N，O和S的环杂原子，Q是H或阳离子。 本发明的化合物可以有利地用于制备磺酰脲类及其前体如磺酰氯或磺酰胺

    New amidino derivatives and their use as thormbin inhibitors
    3.
    发明申请
    New amidino derivatives and their use as thormbin inhibitors 失效
    新的脒基衍生物及其作为酪氨酸抑制剂的用途

    公开(公告)号：US20020068730A1

    公开(公告)日：2002-06-06

    申请号：US09900903

    申请日：2001-07-10

    发明人： Tord Inghardt ,  Arne N. Svensson

    IPC分类号： A61K031/4015 ,  A61K031/397 ,  C07D27/12 ,  C07D25/04

    CPC分类号： C07D401/12 ,  C07C229/42 ,  C07C233/54 ,  C07D205/04 ,  C07D413/12 ,  C07D417/12

    摘要： There is provided compounds of formula I, 1 wherein Y and R1 have meanings given in the description, and pharmaceutically acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

    摘要翻译： 提供式I化合物，其中Y和R 1具有本说明书中给出的含义及其药学上可接受的衍生物（包括前药），该化合物和衍生物可用作或用作胰蛋白酶样竞争性抑制剂的前药 蛋白酶，如凝血酶，特别是治疗需要凝血酶抑制（如血栓形成）或作为抗凝剂的条件。

    New crystalline forms
    4.
    发明申请
    New crystalline forms 失效
    新的结晶形式

    公开(公告)号：US20010023244A1

    公开(公告)日：2001-09-20

    申请号：US09753655

    申请日：2001-01-04

    申请人： Astra Aktiebolag

    发明人： Daniel Edvardsson ,  Lena Hedstrom ,  Anita Lundblad ,  Ursula Pettersson

    IPC分类号： A61K038/05 ,  C07D25/04

    CPC分类号： C07K5/06026 ,  A61K38/00 ,  C07K5/0222

    摘要： There is provided EtO2CnullCH2null(R)CglnullAzenullPabnullOH, or a pharmaceutically-acceptable salt thereof, in a form which is substantially crystalline. It has been found that crystalline forms of EtO2CnullCH2null(R)CglnullAzenullPabnullOH have a high chemical and solid state stability when compared to amorphous forms of the compound.

    摘要翻译： 提供了基本上是结晶形式的EtO 2 C-CH 2 - （R）Cgl-Aze-Pab-OH或其药学上可接受的盐。 已经发现，与化合物的无定形形式相比，EtO 2 C-CH 2 - （R）Cgl-Aze-Pab-OH的结晶形式具有高的化学和固态稳定性。

    Ester derivatives
    6.
    发明申请
    Ester derivatives 失效
    酯衍生物

    公开(公告)号：US20030191316A1

    公开(公告)日：2003-10-09

    申请号：US10332617

    申请日：2003-01-10

    发明人： Yoshio Ogino ,  Hideki Kurihara ,  Kenji Matsuda ,  Tomoshige Numazawa ,  Norikazu Otake ,  Kazuhito Noguchi

    IPC分类号： C07D211/14 ,  C07D29/02 ,  C07D27/09 ,  C07D25/04

    CPC分类号： C07D207/08 ,  C07C219/10 ,  C07C219/14 ,  C07D205/04 ,  C07D207/12 ,  C07D209/52 ,  C07D211/22 ,  C07D211/42 ,  C07D211/46 ,  C07D211/70 ,  C07D239/06 ,  C07D451/02 ,  C07D451/06 ,  C07D471/08 ,  C07D471/10 ,  C07D487/10

    摘要： This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); 1 nullin which A signifies a group expressed by a formula (a0) or (b0); 2 Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as nullN(R8)R9; and Xnull signifies an anionnull.

    摘要翻译： 本发明涉及具有选择性毒蕈碱M3受体拮抗作用，副作用小，适用于吸入治疗的化合物，并且可用作通式（I）的呼吸系统疾病的治疗剂; [其中A表示由式（a0）或（b0）表示的组; Ar表示可选取代的芳基或杂芳基; B 1和B 2表示脂族烃; R 1表示氟取代的环烷基; R 2，R 3和R 4表示低级烷基，单键或与B 1键合的亚烷基，或R 2和R 3一起表示亚烷基; R 5和R 7表示氢，低级烷基或与B 2键合的单键或亚烷基; R 6表示氢，低级烷基或以-N（R 8）R 9表示的基团; 而X - 表示阴离子]。

    Orally available peptidic thrombin inhibitors
    8.
    发明申请
    Orally available peptidic thrombin inhibitors 失效
    口服可利用的肽凝血酶抑制剂

    公开(公告)号：US20020169113A1

    公开(公告)日：2002-11-14

    申请号：US09810243

    申请日：2001-03-19

    发明人： Koo Lee ,  Cheol-Won Park ,  Won-Hyuk Jung ,  Sang-Koo Lee

    IPC分类号： A61K038/05 ,  C07D27/16 ,  C07D25/04

    CPC分类号： C07D401/12 ,  C07D207/16 ,  C07D403/12

    摘要： The present invention relates to novel thrombin inhibitors that are useful as anticoagulants. More particularly, the present invention is directed to peptide derivatives having high antithrombotic activity and high oral bioavailability.

    摘要翻译： 本发明涉及可用作抗凝血剂的新型凝血酶抑制剂。 更具体地，本发明涉及具有高抗血栓活性和高口服生物利用度的肽衍生物。