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220 条记录 (耗时 0.021 秒)

    INDOLE DERIVATIVES
    54.
    发明公开
    INDOLE DERIVATIVES 有权
    吲哚衍生物

    公开(公告)号：EP2125795A1

    公开(公告)日：2009-12-02

    申请号：EP08709170.8

    申请日：2008-02-21

    申请人： N.V. Organon

    发明人： ADAM, Julia

    IPC分类号： C07D413/04 ,  C07D417/04 ,  A61K31/425 ,  A61K31/433 ,  A61K31/4245 ,  A61P29/00

    CPC分类号： C07D417/04 ,  C07D413/04

    摘要： The invention relates to indole derivative having the general Formula (I) wherein A represents a 5-membered aromatic heterocyclic ring, wherein X1, X2 and X3 are independently selected from N, O, S and CH;Y represents CH2, O, S or SO2;R1 is H, (C1-4)-alkyl, (C1-4)alkyloxy, CN orhalogen;R2, R2 ', R3, R3 ', R4,R4 ', R5 and R5 ' are independently hydrogen, (C1-4)alkyl (optionally substituted with OH) or CO-OR8; orone pair of geminal substituents R3 and R3 ' or R5 and R5 ' together represent a keto group, and the others are all hydrogen or (C1-4)alkyl; or R2and R5 together represent a methylene or an ethylene bridge, and R2 '2, R3, R3 ', R4, R4 ' and R5 ' are hydrogen; n is 1 or 2; R6 is H, (C1-4)alkyl (optionally substituted with OH, (C1-4)alkyloxy, CO-NR9R10, CO-OR11or 1,2,4-oxadiazol-3-yl), SO2NR12R13or COOR14; R7 is H or halogen; R 8 is (C1-4)alkyl; R9and R10are independently hydrogen, (C1-4)alkyl or (C 3-7)cycloalkyl, the alkyl groups being optionally substituted with OH or (C1-4)alkyloxy; R11is H or (C1-4)alkyl; R12 and R13 are independently H or (C1-4)alkyl; R14is (C1-6)alkyl; or a pharmaceutically acceptable salt thereof,as agonists of the cannabinoid CB1 receptor, which can be used in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.

    ORAL CONTRACEPTIVE SPRAY
    55.
    发明公开
    ORAL CONTRACEPTIVE SPRAY 审中-公开
    口腔喷雾防治

    公开(公告)号：EP2120874A2

    公开(公告)日：2009-11-25

    申请号：EP07856699.9

    申请日：2007-12-11

    申请人： N.V. Organon

    发明人： VAN DER VOORT MAARSCHALK, Kees

    IPC分类号： A61K9/12

    CPC分类号： A61K9/006 ,  A61K9/12

    摘要： The subject invention provides a liquid contraceptive formulation for oral transmucosal administration. The formulation comprises etonogestrel, optionally together with ethinyl estradiol but does not contain a matrix former or a percutaneous absorption promoter, which is a hydroxy acid or a salt thereof.

    DELIVERY SYSTEM FOR RISPERIDONE
    57.
    发明公开
    DELIVERY SYSTEM FOR RISPERIDONE 审中-公开
    供应系统利培酮

    公开(公告)号：EP2094270A1

    公开(公告)日：2009-09-02

    申请号：EP07822774.1

    申请日：2007-11-21

    申请人： N.V. Organon

    发明人： DE GRAAFF, Wouter ,  SZEGEDI, Armin

    IPC分类号： A61K31/517 ,  A61K9/02

    CPC分类号： A61K31/517 ,  A61K9/0036

    摘要： This invention relates to an extended release formulation comprising solid risperidone, which formulation is a vaginal device having a skin and which device comprises an inner compartment made of a thermoplastic polymer, which polymer is containing risperidone. The polymer is preferably made of ethylene-vinyl acetate copolymer.

    ISOQUINOLINE DERIVATIVES
    58.
    发明授权
    ISOQUINOLINE DERIVATIVES 有权
    异喹啉

    公开(公告)号：EP1963304B1

    公开(公告)日：2009-06-24

    申请号：EP06830425.2

    申请日：2006-12-06

    申请人： N.V. Organon

    发明人： RAY, Peter, Christopher

    IPC分类号： C07D401/12

    CPC分类号： C07D401/12

    摘要： The invention relates to isoquinoline derivatives having the general Formula (I) wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 1 or 2; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R is H or (C1-6)alkyl, optionally substituted with OH, (C1-4)- alkyloxy, (C1-4)alkyloxycarbonyl, (C3-7)cycloalkyl, which may optionally comprise a heteroatom selected from O and S, (C6-10)aryl, (C6-10)aryloxy or a 5- or 6-membered heteroaryl group comprising 1-3 heteroatoms independently selected from O, N and S, each aryl or heteroaryl group being optionally substituted with 1-3 substituents independently selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkylsulfonyl and halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of the isoquinoline derivatives in the treatment of ROCK-I related disorders such as hypertension, atherosclerosis and glaucoma.

    Intrauterine deposit
    59.
    发明公开
    Intrauterine deposit 审中-公开
    宫内Vorrichtung

    公开(公告)号：EP2057972A1

    公开(公告)日：2009-05-13

    申请号：EP07120191.7

    申请日：2007-11-07

    申请人： N.V. Organon

    发明人： The designation of the inventor has not yet been filed

    IPC分类号： A61F6/14 ,  A61F6/18 ,  A61K9/00

    CPC分类号： A61F6/142 ,  A61F6/14 ,  A61F6/144 ,  A61F6/18 ,  A61K9/0039 ,  Y10T29/4998 ,  Y10T29/49982

    摘要： An intrauterine system (1) for the retention of a biologically active compound within the uterus of a female mammal is formed by a frame (16) defining an interior space (20) for receipt of a deposit of the compound (22). The frame has an open structure (18) allowing access to a substantial part of an outer surface of the deposit and the deposit has a rate controlling structure that controls a rate of release of the compound within the uterus. Retention elements (6) are provided on the frame for retaining the frame within the uterus.

    摘要翻译： 通过限定用于接收化合物（22）的沉积物的内部空间（20）的框架（16）形成用于将生物活性化合物保留在雌性哺乳动物子宫内的子宫内系统（1）。 框架具有允许进入沉积物的外表面的大部分的开放结构（18），沉积物具有速率控制结构，其控制化合物在子宫内的释放速率。 保持元件（6）设置在框架上，用于将框架保持在子宫内。

    REMOVAL OF LIPOPOLYSACCHARIDES FROM PROTEIN- LIPOPOLYSACCHARIDE COMPLEXES BY NONFLAMMABLE SOLVENTS
    60.
    发明授权
    REMOVAL OF LIPOPOLYSACCHARIDES FROM PROTEIN- LIPOPOLYSACCHARIDE COMPLEXES BY NONFLAMMABLE SOLVENTS 有权
    脂多糖OFF LIPOPOLYSACCHARIDKOMPLEXEN分离使用非易燃溶剂

    公开(公告)号：EP1638990B1

    公开(公告)日：2009-04-08

    申请号：EP04755271.6

    申请日：2004-06-15

    申请人： N.V. Organon

    发明人： ROPP, Philip, Alfred ,  MURRAY, Michael, Van, Alen

    IPC分类号： C07K1/18

    CPC分类号： C07K1/22 ,  B01D15/362 ,  B01D15/363 ,  B01D15/3804 ,  B01D15/426 ,  C07K1/18

    摘要： During the production of recombinant proteins from gram negative bacteria, lipopolysaccharides (LPS, endotoxin) are released along with the protein of interest. In many instances, LPS will copurify with the target protein due to specific or non­specific protein-ILPS interactions. We have investigated the ability of alkanediols to effect the separation of LPS from protein-LPS complexes while the complexes are immobilized on anion or cation exchange chromatographic media. Alkanediols provide a safer alternative to the use of other organics such as alcohols or acetonitrile due to their lower toxicity and decreased flammability. In addition, they are less costly than many of the detergents that have been used for such purposes. LPS removal efficiency increased with increasing alkane chain length. 1,2-alkanediols were more effective than terminal alkanediols in the separation of LPS from protein­LPS complexes.