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    2-HYDROXYMETHYL-SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS
    2.
    发明申请
    2-HYDROXYMETHYL-SUBSTITUTED OREXIN RECEPTOR ANTAGONISTS 审中-公开
    2-羟甲基取代的OREXIN受体拮抗剂

    公开(公告)号：WO2014176144A1

    公开(公告)日：2014-10-30

    申请号：PCT/US2014/034748

    申请日：2014-04-21

    Applicant: MERCK SHARP & DOHME CORP. ,  KUDUK, Scott, D. ,  SKUDLAREK, Jason, W.

    Inventor： KUDUK, Scott, D. ,  SKUDLAREK, Jason, W.

    IPC: A61K31/4709

    CPC classification number: C07D401/12 ,  C07D401/00 ,  C07D401/14 ,  C07D409/14

    Abstract: The present invention is directed to 2-hydroxymethyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

    Abstract translation: 本发明涉及作为食欲肽受体拮抗剂的2-羟甲基化合物。 本发明还涉及本文所述的化合物在涉及食欲素受体的神经和精神病症和疾病的潜在治疗或预防中的用途。 本发明还涉及包含这些化合物的药物组合物。 本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

    ISOINDOLO[2,1-A]QUINAZOLINE DERIVATIVES FOR STABILIZATION OF ORGANIC MATERIALS
    3.
    发明申请
    ISOINDOLO[2,1-A]QUINAZOLINE DERIVATIVES FOR STABILIZATION OF ORGANIC MATERIALS 审中-公开
    用于稳定有机材料的ISOINDOLO [2,1-A]喹唑啉衍生物

    公开(公告)号：WO2013139799A1

    公开(公告)日：2013-09-26

    申请号：PCT/EP2013/055713

    申请日：2013-03-19

    Applicant: BASF SE

    Inventor： HÖLZL, Werner ,  ROTZINGER, Bruno

    IPC: C09K15/30 ,  C07D403/04 ,  C07D401/00

    CPC classification number: C08K5/3465 ,  C07D401/00 ,  C07D403/04 ,  C07D487/04 ,  C08K5/101 ,  C08K5/52 ,  C09K15/30

    Abstract: The present invention relates to a composition, which comprises a) an organic material susceptible to oxidative, thermal or light-induced degradation, which is a polymer, an oligohydroxy compound, a wax, a fat or a mineral oil, with the proviso that the polymer is not a polypeptide, agar-agar or a component of agar-agar and the oligohydroxy compound is not glucose or a component of agar-agar; and b) a compound of formula (I) n is 1, 2, 3 or 4; when n is 1, R 5 is H, C 1 -C 30 -alkyl, C 3 -C 10 -cycloalkyl, C 6 -C 10 -aryl, which is unsubstituted or substituted by C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, halogen or one phenyl, C 7 -C 13 -aralkyl, C 2 -C 22 -alkenyl, C 3 -C 12 -alkinyl, OH, C 1 -C 30 -alkyloxy, C 3 -C 10 -cycloalkyloxy, C 6 -C 12 -aryloxy, C 7 -C 13 -aralkyloxy, hydroxy-C 1 -C 8 -alkyl, carboxy-C 1 -C 12 -alkyl, C 1 -C 12 -alkoxycarbonyl-C 1 -C 12 -alkyl, C 2 -C 30 -alkyl, which is interrupted by one or more oxygen atoms, C 2 -C 16 -alkyl, which is interrupted by one sulfur atom, or NR' 1 R' 2 ; when n is 2, R 5 is C 1 -C 12 -alkane-diyl, C 6 -C 14 -arylene, C 4 -C 8 -cycloalkane-bis-(C 1 -C 4 -alkylene), C 6 -C 14 -arene-bis-(C 1 -C 4 -alkylene), C 4 -C 24 -alkane-diyl, which is interrupted by one or more oxygen atoms, C 4 -C 20 -alkane-diyl, which is interrupted by one or more -NH-, -N(C 1 -C 8 -alkyl)- or -N(hydroxy-C 1 -C 8 -alkyl)-, piperazine-N,N'-bis-(C 1 -C 4 -alkylene) or C 2 -C 10 -alkane-diyl, which is interrupted by one sulfur atom; R 1 to R 4 and R 6 to R 9 are each independently from each other H, C 1 -C 12 -alkyl, C 3 -C 10 -cycloalkyl, C 3 -C 22 -alkenyl, C 1 -C 12 -alkoxy, C 1 -C 12 -alkylsulfanyl, hydroxy-C 1 -C 8 -alkyl, halogen, NR" 1 R" 2 , NO 2 , CN, phenyl, phenyloxy or R 1 and R 2 or R 2 and R 3 or R 3 and R 4 or R 6 and R 7 or R 7 and R 8 or R 8 and R 9 are linked together to form a five- or 6-membered alicylic, aromatic or heterocyclic ring together with their 2 corresponding carbons atoms, to which they are attached.

    Abstract translation: 本发明涉及一种组合物，其包含a）易于氧化，热或光诱导降解的有机材料，其是聚合物，低聚羟基化合物，蜡，脂肪或矿物油，条件是 聚合物不是多肽，琼脂或琼脂的组分，并且寡羟基化合物不是葡萄糖或琼脂的组分; 和b）式（I）的化合物n为1,2,3或4; 当n为1时，R 5为H，C 1 -C 30 - 烷基，C 3 -C 10 - 环烷基，未被取代或被C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基，卤素或1个苯基取代的C 6 -C 10 - C 7 -C 13 - 芳烷基，C 2 -C 22 - 烯基，C 3 -C 12 - 炔基，OH，C 1 -C 30 - 烷氧基，C 3 -C 10 - 环烷氧基，C 6 -C 12 - 芳氧基，C 7 -C 13 - 芳烷氧基，羟基-C 1 -C 8 - 烷基，羧基-C 1 -C 12烷基，C 1 -C 12烷氧基羰基-C 1 -C 12烷基，被一个或多个氧原子间隔的C 2 -C 30 - 烷基，被一个硫中断的C 2 -C 16 - 烷基 原子或NR'1R'2; 当n为2时，R 5为C 1 -C 12烷烃二基，C 6 -C 14亚芳基，C 4 -C 8环烷基 - 双 - （C 1 -C 4亚烷基），C 6 -C 14 - 芳 - 双 - （C 1 -C 4 - 亚烷基），被一个或多个氧原子中断的C 4 -C 24 - 烷烃二基，被一个或多个-NH-， - C 1 -C 8 - 烷基 - 或被一个硫原子中断的-N（羟基-C 1 -C 8烷基） - ，哌嗪-N，N'-双 - （C 1 -C 4 - 亚烷基）或C 2 -C 10 - 烷烃二基， R 1至R 4和R 6至R 9各自独立地为H，C 1 -C 12 - 烷基，C 3 -C 10 - 环烷基，C 3 -C 22 - 烯基，C 1 -C 12 - 烷氧基，C 1 -C 12烷基硫烷基，羟基-C 1 -C 8 - 烷基，卤素，NR“1R”2，NO 2，CN，苯基，苯氧基或R 1，R 2或R 2，R 3或R 3和R 4或R 6或R 7或R 7和R 8或R 8和R 9连接在一起， 或6元芳基，芳族或杂环以及它们所连接的2个相应的碳原子。

    (20R)-23,23-DIFLUORO-2-METHYLENE-19-NOR-BISHOMOPREGNACALCIFEROL-VITAMIN D ANALOGS
    5.
    发明申请
    (20R)-23,23-DIFLUORO-2-METHYLENE-19-NOR-BISHOMOPREGNACALCIFEROL-VITAMIN D ANALOGS 审中-公开
    （20R）-23,23-二氟-2-甲基-19-异 - 双异噻唑烷基 - 维生素D类似物

    公开(公告)号：WO2009086437A1

    公开(公告)日：2009-07-09

    申请号：PCT/US2008/088272

    申请日：2008-12-24

    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION ,  DELUCA, Hector, F. ,  CLAGETT-DAME, Margaret ,  PLUM, Lori, A. ,  BARYCKI, Rafal

    Inventor： DELUCA, Hector, F. ,  CLAGETT-DAME, Margaret ,  PLUM, Lori, A. ,  BARYCKI, Rafal

    IPC: A61P17/00 ,  A61K31/593 ,  C07C401/00

    CPC classification number: C07D401/00

    Abstract: This invention discloses (20R)-23,23-difluoro-2-methylene-19-nor-bishomopregnacalciferol-vitamin D analogs, and specifically (20R)-23,23-difluoro-lα-hydroxy-2-methylene-19-nor-bishomopregnacalciferol, and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has little, if any, calcemic activity and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.

    Abstract translation: 本发明公开了（20R）-23,23-二氟-2-亚甲基-19-去氧胆固醇酯 - 维生素D类似物，特别是（20R）-23,23-二氟-1a-羟基-2-亚甲基-19-不 双代孕代孕甾醇及其药物用途。 该化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面表现出显着的活性，从而证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，松弛皮肤， 皮肤干燥，皮脂分泌不足。 该化合物也具有很少（如果有的话）钙活性，因此可用于治疗人体中的自身免疫性疾病或炎性疾病以及肾性骨营养不良。 该化合物也可用于治疗或预防肥胖症。

    VITAMIN D3 ANALOGS WITH BIS C-20 SIDE CHAINS
    6.
    发明申请
    VITAMIN D3 ANALOGS WITH BIS C-20 SIDE CHAINS 审中-公开
    维他命D3模拟与BIS C-20侧链

    公开(公告)号：WO98049138A2

    公开(公告)日：1998-11-05

    申请号：PCT/EP1998/002390

    申请日：1998-04-22

    IPC: A61K31/593 ,  A61K20060101 ,  A61K31/59 ,  A61K31/695 ,  A61P19/10 ,  A61P35/00 ,  A61P37/06 ,  C07C401/00 ,  C07D20060101 ,  C07D401/00 ,  C07F20060101 ,  C07F7/18

    CPC classification number: A61K31/59 ,  A61K31/593 ,  A61K31/695 ,  C07C401/00 ,  C07D401/00 ,  C07F1/00 ,  C07F7/18

    Abstract: This invention provides Vitamin D3 analogs of the Formula (I) wherein: X is H2 or CH2; Y is hydrogen, hydroxy or fluorine; Z is hydroxy; R1 and R2 are a (C1-C4) alkyl or fluoroalkyl, or R1 and R2 together with C25 form a (C3-C6) cycloalkyl or cyclofluoroalkyl; R3 and R4 are a (C1-C4) alkyl or fluoroalkyl, or R3 and R4 together with C25' form a (C3-C6) cycloalkyl or cyclofluoroalkyl; A is a single bond or a double bond; B1 is a single bond, an E-double bond, a Z-double bond or a triple bond; and B2 is a single bond, an E-double bond, a Z-double bond or a triple bond; and prodrugs thereof; intermediates and methods for preparation of these analogs, pharmaceutical compositions containing such analogs and methods for treatment of osteoporosis, hyperparathyroidism autoimmune diseases and for the treatment and prevention of neoplastic diseases.

    Abstract translation: 本发明提供式（I）的维生素D3类似物，其中：X是H 2或CH 2; Y是氢，羟基或氟; Z是羟基; R1和R2是（C1-C4）烷基或氟烷基，或R1和R2与C25一起形成（C 3 -C 6）环烷基或环氟烷基; R3和R4是（C1-C4）烷基或氟代烷基，或R3和R4与C25'一起形成（C 3 -C 6）环烷基或环氟烷基; A是单键或双键; B1是单键，E-双键，Z-双键或三键; B2是单键，E-双键，Z-双键或三键; 和前药; 用于制备这些类似物的中间体和方法，含有这种类似物的药物组合物和用于治疗骨质疏松症，甲状旁腺功能亢进症自身免疫性疾病以及用于治疗和预防肿瘤性疾病的方法。

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