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59 条记录 (耗时 0.045 秒)

    Retinoid antagonists and use thereof
    24.
    发明授权
    Retinoid antagonists and use thereof 有权
    类视黄醇拮抗剂及其用途

    公开(公告)号：US06326397B1

    公开(公告)日：2001-12-04

    申请号：US09307009

    申请日：1999-05-07

    申请人： Werner Bollag ,  Michael Klaus ,  Peter Mohr ,  Paola Panina-Bordignon ,  Michael Rosenberger ,  Francesco Sinigaglia

    发明人： Werner Bollag ,  Michael Klaus ,  Peter Mohr ,  Paola Panina-Bordignon ,  Michael Rosenberger ,  Francesco Sinigaglia

    IPC分类号： A01N5300

    CPC分类号： C07C57/48 ,  C07C57/42

    摘要： The present invention relates to novel retinoid antagonists of the formula I wherein the dotted bond can be either hydrogenated or form a double bond; and, when the dotted bond forms a double bond, R1 is lower alkyl and R2 is hydrogen; and, when the dotted bond is hydrogenated, R1 and R2 taken together are methylene to form a cis-substituted cyclopropyl ring; R3 is hydroxy or lower alkoxy; R4 is alkyl or alkoxy; and R5 and R6 are, independently, a C4-12 alkyl or a 5-12 cycloalkyl substituent containing from 1-3 rings which are either unsubstituted or substituted with from 1-3 lower alkyl groups, with the carbon atom of R5 and R6 being linked to the remainder of the molecule to form a quaternary carbon atom pharmaceutically acceptable salts of carbocylic acids of the formula I; as well as method for the treatment of osteoporosis and preneoplastic and neoplastic diseases, and a method for reducing or abolishing adverse events in subjects receiving retinoid agonist treatment by administering a retinoid antagonist.

    摘要翻译： 本发明涉及式I的新型类视黄醇拮抗剂，其中虚线键可以被氢化或形成双键; 并且当虚线键形成双键时，R 1为低级烷基且R 2为氢; 并且当点键被氢化时，R 1和R 2一起为亚甲基以形成顺式取代的环丙基环; R3是羟基或低级烷氧基; R4是烷基或烷氧基; 并且R 5和R 6独立地是C 1-4烷基或含有1-3个环的5-12个环烷基取代基，它们是未取代的或被1-3个低级烷基取代，R5和R6的碳原子是 与分子的其余部分连接以形成式I的碳酸的药学上可接受的盐的季碳原子; 以及用于治疗骨质疏松症和肿瘤前和肿瘤性疾病的方法，以及通过施用类视黄醇拮抗剂减少或消除接受类视黄醇激动剂治疗的受试者的不良事件的方法。

    Alkyl or alkoxy substituted S-heterocyclic retinoids
    26.
    发明授权
    Alkyl or alkoxy substituted S-heterocyclic retinoids 失效
    烷基或烷氧基取代的S-杂环类视黄醇

    公开(公告)号：US5512683A

    公开(公告)日：1996-04-30

    申请号：US324836

    申请日：1994-10-18

    申请人： Michael Klaus ,  Peter Mohr

    发明人： Michael Klaus ,  Peter Mohr

    IPC分类号： A61K31/38 ,  A61K31/381 ,  A61K31/382 ,  A61P17/00 ,  A61P37/06 ,  C07D333/54 ,  C07D335/06 ,  C07D337/08 ,  C07D337/04

    CPC分类号： C07D333/54 ,  C07D335/06 ,  C07D337/08

    摘要： Compounds of the formula ##STR1## in which X is --S--, --SO-- or --SO.sub.2 --; R.sup.1 is C.sub.7-10 -alkyl or C.sub.7-10 -alkoxy; R.sup.2 is a residue of the formula ##STR2## R.sup.3 is carboxy or lower-alkoxycarbonyl; and n is an integer of 1, 2 or 3; and salts of carboxylic acids of formula I can be used for the treatment of autoimmune diseases and diseases having a strong immunological component, such as psoriasis.

    摘要翻译： 其中X是-S-，-SO-或-SO 2 - 的式I的化合物; R1是C7-10-烷基或C7-10-烷氧基; R 2是下式的残基：R 3是羧基或低级烷氧基羰基; n为1,2或3的整数; 式I的羧酸盐可用于治疗具有强免疫组分的自身免疫性疾病和疾病，例如牛皮癣。

    Tetrahydronaphthalene and indane derivatives
    28.
    发明授权
    Tetrahydronaphthalene and indane derivatives 失效
    四氢萘和茚满衍生物

    公开(公告)号：US5084476A

    公开(公告)日：1992-01-28

    申请号：US395005

    申请日：1989-08-17

    申请人： Michael Klaus ,  Ekkehard Weiss

    发明人： Michael Klaus ,  Ekkehard Weiss

    IPC分类号： C07D213/16 ,  C07D239/26 ,  C07D307/36 ,  C07D333/08

    CPC分类号： C07D213/16 ,  C07D239/26 ,  C07D307/36 ,  C07D333/08

    摘要： The compounds of the formula ##STR1## wherein X and Y are independently --CH.sub.2 -- or >C(CH.sub.3).sub.2 ; Z is --CHR.sup.8 --, >CO, >CR.sup.8 OR.sup.7, --CHR.sup.8 --CHR.sup.8 --, --CHOR.sup.7 --CH.sub.2 --, --CO--CHOR.sup.7 or --CHOR.sup.7 --CHOR.sup.7 --; R.sup.1 is a 5- or 6-membered, monocyclic heterocyclic group which optionally can be C-substituted by halogen, lower-alkyl, lower-alkoxy, acyloxy, nitro, hydroxy, amino, lower-alkylamino or di-lower-alkylamino and/or which can be substituted on a ring --NH-- group by lower-alkyl; R.sup.2 and R.sup.3 are independently hydrogen, lower-alkyl, trifluoromethyl or halogen and one of R.sup.2 and R.sup.3 always is trifluoromethyl or lower-alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkoxy or halogen; R.sup.6 is hydrogen, lower-alkyl or --OR.sup.7 ; R.sup.7 is hydrogen, lower-alkyl or acyl; R.sup.8 is hydrogen or lower-alkyl; and R.sup.7 and R.sup.8 can be the same or different from one another,are useful for the treatment of neoplasms and dermatoses in mammals. The compounds can be manufactured from a corresponding bicyclic component and a heterocyclic component containing the residue R.sup.1 by a Wittig, Horner or Grignard reaction and the optional subsequent transformation of reactive groups.

    摘要翻译： 下式的化合物其中X和Y独立地是-CH 2 - 或> C（CH 3）2; Z是-CHR8-，> CO，> CR8OR7，-CHR8-CHR8-，-CHOR7-CH2-，-CO-CHOR7或-CHOR7-CHOR7-; R 1是任选地可以被卤素，低级烷基，低级烷氧基，酰氧基，硝基，羟基，氨基，低级烷基氨基或二低级烷基氨基和/或低级烷基氨基取代的5-或6-元单环杂环基， 或者可以被低级烷基取代在环-NH-基上; R2和R3独立地是氢，低级烷基，三氟甲基或卤素，R2和R3之一总是三氟甲基或低级烷基; R4和R5独立地是氢，烷基，烷氧基或卤素; R6是氢，低级烷基或-OR7; R7是氢，低级烷基或酰基; R8是氢或低级烷基; 并且R7和R8可以相同或不同，可用于治疗哺乳动物的肿瘤和皮肤病。 化合物可以由对应的双环组分和含有残基R1的杂环组分通过Wittig，Horner或Grignard反应和任选的随后的反应性基团的转化来制备。