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    MACROCYCLIC LACTONE DRUG DELIVERY SYSTEM
    44.
    发明公开
    MACROCYCLIC LACTONE DRUG DELIVERY SYSTEM 审中-公开
    系统给药的大环LACTONARZNEIMITTELS的

    公开(公告)号：EP2408432A1

    公开(公告)日：2012-01-25

    申请号：EP10709491.4

    申请日：2010-03-16

    申请人： Intervet International B.V. ,  N.V. Organon

    发明人： GRAAFF DE, Wouter ,  ZEEMAN, Raymond ,  HONCOOP, Niels

    IPC分类号： A61K9/20 ,  A61K31/365

    CPC分类号： A61K31/365 ,  A61K9/0024 ,  A61K9/2027 ,  A61K9/209

    摘要： Disclosed is a drug delivery system from which a macrocyclic lactone can be released with a desirable zero order release profile. The system is based on the use of thermoplastic polymers, and particularly of polyethylene vinyl acetate copolymers (EVA). The drug delivery system of the invention comprises a solid non-porous reservoir in which the macrocyclic lactone is contained, preferably in a concentration well above the saturation concentration, and a non-porous skin covering the reservoir not initially loaded with the drug. The system is preferably in the form of a rod, wherein the core and the skin are concentric, and the end surfaces of the rod are not skin-covered.

    1-(4-(PYRIDIN-2-YL)BENZYL)IMIDAZOLIDINE-2,4-DIONE DERIVATIVES
    45.
    发明公开
    1-(4-(PYRIDIN-2-YL)BENZYL)IMIDAZOLIDINE-2,4-DIONE DERIVATIVES 审中-公开
    1-（4-（吡啶-2-基）苄基）咪唑啉-2,4-二酮衍生物

    公开(公告)号：EP2373639A1

    公开(公告)日：2011-10-12

    申请号：EP09764238.3

    申请日：2009-11-30

    申请人： N.V. Organon

    发明人： VAN DER STELT, Marcelis ,  CALS, Joseph, Maria, Gerardus, Barbara ,  KLOMP, Johannes, Petrus, Gerardus

    IPC分类号： C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/445 ,  A61K31/541 ,  A61K31/4439 ,  A61K31/5375 ,  A61P25/04

    CPC分类号： C07D401/10 ,  C07D401/14 ,  C07D405/14

    摘要： The invention relates to 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivative having the general Formula I wherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, (C1-3)alkyloxy, (C1-3)alkyloxycarbonyl, halogen or CN), (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each cycloalkyl ring optionally comprising a heteroatom selected from O and S; R2 and R3 are independently H or (C1-3)alkyl; or R2 and R3 form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R4 is H or 1 to 3 F substituents; R5 is H or 1 to 4 F substituents; R6 and R7 are independently H or F; X represents R8, OR8, NR8R9, R8 is (C5-7)cycloalkyl optionally comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; R10 represents 1-3 substituents independently selected from H, (C1-3)alkyl, halogen, oxo, CN and CF3; Y is CF2, O, S, SO or SO2; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives 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.

    1-(4-UREIDOBENZOYL)PIPERAZINE DERIVATIVES
    47.
    发明公开
    1-(4-UREIDOBENZOYL)PIPERAZINE DERIVATIVES 有权
    1-（4-脲基苯甲酰基）哌嗪衍生物

    公开(公告)号：EP2318368A1

    公开(公告)日：2011-05-11

    申请号：EP09791938.5

    申请日：2009-08-26

    申请人： N.V. Organon ,  Pharmacopeia, LLC

    发明人： COOKE, Andrew, John ,  BENNETT, David, Jonathan ,  EDWARDS, Andrew Stanley ,  ROUGHTON, Andrew Laird ,  NEAGU, Irina ,  CHAN, Jui-Hsiang ,  HO, Koc-Kan ,  ANSARI, Nasrin ,  MORRIS, Michelle Lee ,  RONG, Yajing ,  OHLMEYER, Michael

    IPC分类号： C07D213/56 ,  C07D263/34 ,  C07D307/68 ,  C07D333/38 ,  A61P9/10 ,  A61K31/496

    CPC分类号： C07D263/34 ,  C07D213/56 ,  C07D277/56 ,  C07D307/68 ,  C07D333/38

    摘要： The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R
    1 is (C
    1-8 )alkyl, (C
    3-8 )cycloalkyl or (C
    3-8 )cycloalkyl(C
    1-3 )alkyl, each of which may be substituted by hydroxy, cyano or halogen; R
    2 represents 1 or 2 optional halogens; R
    3 is (C
    1-6 )alkyl, (C
    3-6 )cycloalkyl or (C
    3-6 )cycloalkyl(C
    1-3 )alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5-or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.

    摘要翻译： 本发明涉及具有通式I的1-（4-脲基苯甲酰基）哌嗪衍生物（我们引起您的注意，在该电子版中没有提供式I，因为它在该论文摘要中提供）其中R 1 是各自可被羟基，氰基或卤素取代的（C 1-8）烷基，（C 3-8）环烷基或（C 3-8）环烷基（C 1-3）烷基; R 2代表1或2个任选的卤素; R 3是可以被一个或多个卤素取代的（C 1-6）烷基，（C 3-6）环烷基或（C 3-6）环烷基（C 1-3）烷基; A表示包含1-3个选自N，O和S的杂原子的杂芳基环系统，当X是C时，该环系统是5-或6-元，并且当X是N时是5-元; n是1或2; 或其药学上可接受的盐; 涉及包含它们的药物组合物，并涉及这些1-（4-脲基苯甲酰基）哌嗪衍生物在制备用于治疗或预防与胆固醇和胆汁酸转运和代谢相关的动脉粥样硬化和相关病症的药物中的用途。

    6-PHENYL-1H-IMIDAZO[4,5-C]PYRIDINE-4-CARBONITRILE DERIVATIVES AS CATHEPSIN INHIBITORS
    48.
    发明授权
    6-PHENYL-1H-IMIDAZO[4,5-C]PYRIDINE-4-CARBONITRILE DERIVATIVES AS CATHEPSIN INHIBITORS 有权
    作为钙调蛋白抑制剂的6-苯基-1H-咪唑并[4,5-C]吡啶-4-碳腈衍生物

    公开(公告)号：EP2178873B1

    公开(公告)日：2010-12-22

    申请号：EP08786128.2

    申请日：2008-07-14

    申请人： N.V. Organon

    发明人： CAI, Jiaqiang ,  RANKOVIC, Zoran ,  JONES, Philip, Stephen ,  BENNETT, David, Jonathan ,  FRADERA, Xavier

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P19/00 ,  A61P17/00 ,  A61P29/00

    CPC分类号： C07D471/04 ,  C07D519/00

    摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula (I), to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such asatherosclerosis,obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer,and chronic pain, such as neuropathic pain.

    摘要翻译： 本发明涉及具有通式（I）的6-苯基-1H-咪唑并[4,5-c]吡啶-4-腈衍生物，包含其的药物组合物，以及涉及这些衍生物用于 制备用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖症，炎症和免疫紊乱如类风湿性关节炎，牛皮癣，癌症和慢性疼痛如神经性疼痛的药物。

    INTRAUTERINE DEPOSIT
    49.
    发明公开
    INTRAUTERINE DEPOSIT 有权
    宫内节育器

    公开(公告)号：EP2211794A2

    公开(公告)日：2010-08-04

    申请号：EP08848433.2

    申请日：2008-11-07

    申请人： N.V. Organon

    发明人： DE GRAAFF, Wouter ,  VEENSTRA, Harm ,  MULDERS, Titia

    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 compoun 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.

    Use of glucocorticoid receptor antagonists for treatment of infectious conditions
    50.
    发明公开
    Use of glucocorticoid receptor antagonists for treatment of infectious conditions 审中-公开
    Verwendung von Glucocorticoid-Rezeptorantagonisten zur Behandlung voninfektiösenZuständen

    公开(公告)号：EP2204171A1

    公开(公告)日：2010-07-07

    申请号：EP10159050.3

    申请日：2007-08-06

    申请人： N.V. Organon

    发明人： Peeters, B.W.M.M., Bernardus

    IPC分类号： A61K31/00 ,  A61K31/569 ,  A61P37/04

    CPC分类号： A61K31/00 ,  A61K31/569

    摘要： The invention provides the use of a glucocorticoid receptor antagonist for the manufacture of a medicament for immune stimulation, such as prevention or treatment of infections or infectious conditions, in an aging mammalian subject, a mammalian subject with low serum DHEAS values, a mammalian subject with a high serum cortisol/DHEAS ratio or a mammalian subject with high neutrophil counts.
    In particular, the glucocorticoid receptor antagonist can be chosen from the group consisting of a dibenzopyranyl derivative defined and/or exemplified in US6329534 and WO200116128, mifepristone, and (11β,17β)-11-(1,3-benzodioxol-5-yl)-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one.

    摘要翻译： 本发明提供糖皮质激素受体拮抗剂在老化哺乳动物受试者，具有低血清DHEAS值的哺乳动物受试者中的制备用于免疫刺激的药物，例如预防或治疗感染或感染性病症的用途，哺乳动物受试者具有 高血清皮质醇/ DHEAS比例或具有高嗜中性粒细胞计数的哺乳动物受试者。 特别地，糖皮质激素受体拮抗剂可以选自US6329534和WO200116128中定义和/或例举的二苯并吡喃基衍生物，米非司酮和（11,2,172）-11-（1,3-苯并间二氧杂环戊烯-5-基） -17-羟基-17-（1-丙炔基）雌甾-4,9-二烯-3-酮。