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    TETRAHYDROQUINOLINE DERIVATIVES AND THEIR USE AS FSH RECEPTOR MODULATORS
    31.
    发明授权
    TETRAHYDROQUINOLINE DERIVATIVES AND THEIR USE AS FSH RECEPTOR MODULATORS 有权
    啉及其作为FSH受体的调节剂

    公开(公告)号：EP1578727B1

    公开(公告)日：2008-04-16

    申请号：EP03808299.6

    申请日：2003-12-16

    申请人： N.V. Organon

    发明人： TIMMERS, Cornelis Marius, N.V. Organon ,  KARSTENS, Willem Frederik Johan, N.V. Organon

    IPC分类号： C07D215/38 ,  A61K31/47 ,  A61P5/08 ,  C07D401/12 ,  C07D409/12

    CPC分类号： C07D215/38 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

    摘要： The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R and R are H, Me; R is (2-6C)heterocycloalkyl(1-­4C)alkyl, (2-5C)heteroaryl(1-4C)alkyl, (6C)aryl (1-4C)alkyl, (1-4C)(di)alkylaminocarbonylamino(2-4C)alkyl, (2-­6C) heterocycloalkylcarbonylamino(2-4C)alkyl, R -(2-4C)alkyl or R -carbonyl(1-4C)alkyl; R is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2-6C)heterocycloalkyl or (1-6C) alkyl and R is (di)(1-4C)alkylamino, (1-4C)alkoxy, amino, hydroxy, (6C)arylamino, (di)(3-4C)alkenylamino, (2-5C)heteroaryl(1-4C)alkylamino, (6C)aryl(1-4C) alkylamino, (di)[(1­-4C)alkoxy(2-4C)alkyl]amino, (di)[(1-4C)alkylamino(2-4C) alkyl]amino, (di)[amino(2-4C)alkyl]amino or (di)[hydroxy(2­-4C)alkyl]amino. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility.

    Use of Mirtazapine for improving the therapeutic response of humans having major depression and carrying the gene for apolipoprotein E4
    33.
    发明授权
    Use of Mirtazapine for improving the therapeutic response of humans having major depression and carrying the gene for apolipoprotein E4 有权
    使用米氮平用于改善抑郁症谁是基因载脂蛋白E4携带者的人的治疗。

    公开(公告)号：EP1442133B1

    公开(公告)日：2007-12-12

    申请号：EP02704147.4

    申请日：2002-02-12

    申请人： N.V. Organon

    发明人： MURPHY, Greer, M. ,  SCHATZBERG, Alan, F.

    IPC分类号： C12Q1/68

    CPC分类号： A61K31/00 ,  A61K31/55 ,  A61K31/551 ,  C12Q1/6883 ,  C12Q2600/156

    摘要： This invention relates to methods for improving the treatment of major depression in a human patient by genotyping the patient for the gene for apolipoprotein E4 and adapting the further treatment of the patient accordingly depending on the presence or absence of the gene in the patient. The invention also relates to methods for improving the therapeutic response of human patients with major depression by determining the apolipoprotein E genotype of a human patient and administering a noradrenergic transmission enhancing anti-depressant drug, such as mirtazapine, in an amount effective to treat major depression, to those patients who are found to carry the gene for apolipoprotein E4. Also disclosed are methods for improving the therapeutic response of a human patient with major depression comprising administering mirtazapine, in an amount effective to treat major depression, to a human patient who is a carrier of the gene for apolipoprotein E4.

    APPLICATOR FOR INSERTING AN IMPLANT
    35.
    发明公开
    APPLICATOR FOR INSERTING AN IMPLANT 有权
    VORRICHTUNG ZUM IMPLANTIEREN EINES IMPLANTATS

    公开(公告)号：EP1841493A1

    公开(公告)日：2007-10-10

    申请号：EP06707783.4

    申请日：2006-01-20

    申请人： N.V. Organon

    发明人： JANSEN, Willem ,  TAK, Maurice Petrus Wilhelmus ,  VERTEGAAL, Hendricus Johannes ,  VAN DER GRAAF, Iris Epkjen Hobo

    IPC分类号： A61M37/00

    CPC分类号： A61M37/0069 ,  A61M31/007

    摘要： The invention pertains to an applicator (1) for inserting an implant, in particular a rod-like implant (2) containing an active substance, under the skin of a human or animal, comprising a housing (3), a cannula (6), a cannula holder (9), an implant (2) accommodated inside the cannula (6) and/or the cannula holder (9), a protective cover (7) for the cannula (6), and a mechanism (22, 23, 7) which, at least after the cover (7) has been removed from the cannula (6), secures the implant (2) inside the cannula (6) and/or cannula holder (9). The mechanism (22, 23, 7) disengages the implant (2) during insertion of the cannula (6) or after the cannula (6) has been inserted. Substantially no lateral force will be exerted during the expelling of the implant from the cannula.

    摘要翻译： 本发明涉及一种用于在人或动物的皮肤下插入植入物，特别是包含活性物质的棒状植入物（2）的施用器（1），包括壳体（3），插管（6） ，套管保持器（9），容纳在套管（6）和/或套管保持器（9）内部的植入物（2），用于插管（6）的保护盖（7），以及机构 ，7），其至少在从所述套管（6）移除所述盖（7）之后，将所述植入物（2）固定在所述套管（6）和/或套管保持器（9）内。 在套管（6）的插入过程中或套管（6）插入后，机构（22,23,7）脱离植入物（2）。 在将植入物从插管中排出时，基本上不会施加横向力。

    PROGESTERONE RECEPTOR MODULATORS
    39.
    发明公开
    PROGESTERONE RECEPTOR MODULATORS 有权
    PROGESTERONREZEPTORMODULATOREN

    公开(公告)号：EP1735330A1

    公开(公告)日：2006-12-27

    申请号：EP05733590.3

    申请日：2005-03-18

    申请人： N.V. Organon

    发明人： HAMERSMA, Johannes Antonius Maria ,  REWINKEL, Johannes Bernardus Maria

    IPC分类号： C07J43/00 ,  C07J53/00 ,  A61K31/58 ,  A61P15/18

    CPC分类号： C07J43/003 ,  C07J5/00 ,  C07J43/00 ,  C07J53/001

    摘要： The subject invention provides a compound according to Formula I, wherein Formula (1) is O, NOH, NO(1-4C)alkyl, NO(1-4C)acyl; Al-A5 are C, substituted with RI, or N, provided that at least one and not more than three of Al-A5 are N; or one or two of Al, A2 and A5 are N, and the others are C, substituted with Rl, and A3 and A4 together represent a fused benzo ring or a fused five- or six-membered nitrogen-containing aromatic ring, both optionally substituted with one or more halogen and/or (1-4C)alkyl; RI is H, halogen, (1 -4C)alkyl, (1 -4C)alkoxy; R2 is H, (1-4C)alkyl or (1-6C)alkenyl, both optionally substituted with an (6-10)aryl group, which is optionally substituted with one or more halogen and/or (1-4C)alkyl; and R3 is H or (1-4C)alkyl, optionally substituted with one or more halogen atoms; and R4 is cyclopropyl or cyclopropenyl, both optionally substituted with one or more halogen and/or (1-4C)alkyl; or R2 together with R3 forms a 3-, 4-, 5- or 6-membered carbocyclic ring; and R4 is cyclopropyl or cyclopropenyl, both optionally substituted with one or more halogen and/or (1-4C)alkyl); or R2 is H or (1-4C)alkyl; and R3 together with R4 forms a 5-, 6- or 7-membered saturated or unsaturated carbocyclic ring; R5 is H or (1-4C)alkyl; or a pharmaceutically acceptable salt and/or hydrate form and/or prodrug thereof.