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    Novel pyridyl cyanoguanidine compounds
    141.
    发明申请
    Novel pyridyl cyanoguanidine compounds 有权
    新型吡啶氰腈化合物

    公开(公告)号：US20080090842A1

    公开(公告)日：2008-04-17

    申请号：US11998575

    申请日：2007-11-30

    Applicant: Fredrik Bjorkling

    Inventor： Fredrik Bjorkling

    IPC: A61K31/4709 ,  A61K31/44 ,  A61K31/4439 ,  A61P35/00 ,  A61K31/444

    CPC classification number: C07D213/89 ,  A61K31/4439 ,  A61K45/06 ,  C07D401/12

    Abstract: Compounds according to formula I wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated C1-6 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; X represents a straight or branched, saturated or unsaturated C1-12 hydrocarbon diradical, optionaly substituted with halogen, hydroxy, cyano, nitro, carboxy, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, amino, aminoalkyl, aminocarbonyl, alkylcarbonylamino, sulfo, aminosulfonyl, alkylsulfonylamino, hydroxysulfonyloxy, dihydroxyphosphinoyloxy or phosphono; Y represents a bond, 0, C(O), S, S(O), S(0)2, C(O)O, NH, C(O)NH, OC(O) or NHC(O); Z represents an aromatic or non-aromatic heterocyclic radical with 5-12 ring atoms, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl, aminoalkyl or straight or branched, saturated or unsaturated C1-4 hydrocarbon radical, optionally substituted with halogen, hydroxy, cyano, nitro, alkoxy, alkoxycarbonyl, alkylcarbonyl, formyl or aminoalkyl; provided that R1 is not attached to the nitrogen-atom in the pyridyl ring; and pharmaceutically acceptable salts, solvates, hydrates, N-oxides and prodrugs thereof are disclosed. The compounds are useful in therapy.

    Abstract translation: 根据式I的化合物，其中R 1表示氢，卤素或一个或多个直链或支链，饱和或不饱和的C 1-6 - 烃基，任选被卤素，羟基，氰基，硝基，羧基，烷氧基 烷氧基羰基，烷基羰基，甲酰基，氨基，氨基烷基，氨基羰基，烷基羰基氨基，磺基，氨基磺酰基，烷基磺酰基氨基，羟基磺酰氧基，二羟基磷酰氧基或膦酰基; X代表直链或支链饱和或不饱和的C 1-12烃二价基，任选被卤素，羟基，氰基，硝基，羧基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，氨基，氨基烷基，氨基羰基 烷基羰基氨基，磺基，氨基磺酰基，烷基磺酰基氨基，羟基磺酰氧基，二羟基亚磷酰氧基或膦酰基; Y表示0，C（O），S，S（O），S（O）2，C（O）O，NH，C（O）NH，OC（O） 或NHC（O）; Z代表具有5-12个环原子的芳族或非芳族杂环基团，任选被卤素，羟基，氰基，硝基，烷氧基，烷氧基羰基，烷基羰基，甲酰基，氨基烷基或直链或支链，饱和或不饱和的C 1 羟基，氰基，硝基，烷氧基，烷氧基羰基，烷基羰基，甲酰基或氨基烷基; 条件是R1不连接在吡啶环中的氮原子上; 及其药学上可接受的盐，溶剂化物，水合物，N-氧化物和前体药物。 这些化合物可用于治疗。

    Isomerisation of pharmaceutical intermediates
    142.
    发明申请
    Isomerisation of pharmaceutical intermediates 审中-公开
    药物中间体异构化

    公开(公告)号：US20070215455A1

    公开(公告)日：2007-09-20

    申请号：US11431672

    申请日：2006-05-11

    Applicant: Michael Folkmann ,  Erik Hansen

    Inventor： Michael Folkmann ,  Erik Hansen

    IPC: C07C401/00

    CPC classification number: C07B37/08 ,  C07C401/00 ,  C07C2601/02 ,  C07F7/1892

    Abstract: The present invention relates to an isomerisation method of vitamin D analogues, such as compounds useful for the synthesis of calcipotriol, and to and to the use of a flow-through photoreactor or continuous flow photoreactor reactor for making said vitamin D analogues. The present invention relates further to the use of intermediates produced with said method for making calcipotriol or calcipotriol monohydrate, or pharmaceutical formulations thereof.

    Abstract translation: 本发明涉及维生素D类似物的异构化方法，例如可用于合成卡泊三醇的化合物，以及使用流通光反应器或连续流动光反应器来制备所述维生素D类似物。 本发明还涉及使用所述制备卡泊三醇或卡泊​​三醇一水合物的方法制备的中间体或其药物制剂。

    Vitamin d analogues, compositions comprising said analogues and their use
    146.
    发明申请
    Vitamin d analogues, compositions comprising said analogues and their use 有权

    公开(公告)号：US20060166949A1

    公开(公告)日：2006-07-27

    申请号：US10532019

    申请日：2003-10-23

    Applicant: Ernst Binderup ,  Holst Kai ,  Aage Svensgaard Claus ,  John Martin

    Inventor： Ernst Binderup ,  Holst Kai ,  Aage Svensgaard Claus ,  John Martin

    IPC: A61K31/59 ,  C07C401/00

    CPC classification number: C07C401/00

    Abstract: Compounds according to formula I in which formula R1 and R2, which may be the same or different, represent halogen, (C1-C6)hydrocarbyl, optionally substituted with one or two hydroxyl group or one or more fluorine atoms, or, together with the carbon atom to which they are both attached, R1 and R2 form a (C3-C6)carbocyclic ring, or one of R1 and R2 taken together with R3 forms a direct bond, such that a triple bond is constituted, or R1 and R2 represent both hydrogen; R3 when not forming a direct bond with one of R1 and R2 represents hydrogen or (C1-C3)hydrocarbyl; X represents (E)-ethylene, (Z)-ethylene, ethynylene, or a bond; Y and Z independently represent hydrogen or methyl; the bond between C#16 and C#17 is depicted with a dotted line to illustrate that said bond may be either a single bond, in which case the projection of the ring substituent is beta, or a double bond; A represents hydroxyl, fluorine or hydrogen; B represents CH2 or H2; the configuration in the 3-position corresponds to the same configuration as in natural vitamin D3 (normal), or the configuration in the 3-position is opposite to that of natural vitamin D3 (epi); with the proviso that when X represents (E)-ethylene or (Z)-ethylene, one of R1 and R2 taken together with R3 may not form a direct bond, such that a triple bond is constituted; with the further proviso that when X represents a bond R1 and R2 are not hydrogen; with the further proviso that the compound of formula I is not 3(S)-hydroxy-9,10-secocholesta-5(Z),7(E),10(19),22(E),24-penta-ene; and prodrugs and stereo isomeric forms thereof are provided together with their use in therapy, and their use in the manufacture of medicaments.

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