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    • 71. 发明授权
    • Vitamin D analogues having a halogen-or azido- substituted side chain
    • 维生素D类似物具有卤素或叠氮基取代的侧链
    • US5612325A
    • 1997-03-18
    • US367206
    • 1995-01-03
    • Kai HansenHenrik Pedersen
    • Kai HansenHenrik Pedersen
    • A61K31/59A61K31/593A61P3/08A61P9/12A61P11/00A61P17/00A61P29/00A61P35/00A61P37/00A61P43/00C07C401/00
    • C07C401/00
    • A compound of formula I ##STR1## wherein R stands for a straight or branched, saturated or unsaturated alkyl group containing from 4 to 12 carbon atoms optionally substituted with a hydroxy group, and possibly containing a ring structure, and in which at least one of the carbon atoms not bearing hydroxyl group is substituted with one or more halogen atoms or an azido group; and prodrugs of I in which one or more of the hydroxy groups are masked as groups which can be reconverted to hydroxy groups in vivo, in pure form or in mixtures. The compounds show antiinflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells. The compounds are prepared by oxidizing 1(S),3(R)-bis-(tert-butyldimethylsilyloxy)-20(S)formyl-9,10-seco-pregna-5(E),7(E),10(19)-triene, reducing the resulting product; alkylating the reduction product and then subjecting the alkylated product to triplet-sensitized photoisomerization.
    • PCT No.PCT / DK95 / 00305 Sec。 371日期1995年1月3日 102(e)日期1995年1月3日PCT 1993年9月23日PCT公布。 第WO94 / 07851号公报 日期1994年04月14日一种式I化合物其中R代表任选被羟基取代的含有4至12个碳原子的直链或支链饱和或不饱和烷基,并且可能含有环结构, 其中至少一个不含羟基的碳原子被一个或多个卤素原子或叠氮基取代; 和其中一个或多个羟基被掩蔽为可以在体内,纯形式或混合物中再转化为羟基的基团的I前药。 这些化合物显示出抗炎和免疫调节作用,以及在诱导分化和抑制某些细胞的不期望的增殖方面具有很强的活性。 通过氧化1(S),3(R) - 双 - (叔丁基二甲基甲硅烷氧基)-20(S)甲酰基-9,10-仲孕-5(E),7(E),10( 19) - 三烯,还原所得产物; 烷基化还原产物,然后使烷基化产物进行三重敏感的光异构化。
    • 74. 发明授权
    • 1,2,3-Triazole and tetrazole substituted piperidine or
tetrahydropyridine compounds useful as acetylcholine agonists
    • 可用作乙酰胆碱激动剂的1,2,3-三唑和四唑取代的哌啶或四氢吡啶化合物
    • US4866077A
    • 1989-09-12
    • US209994
    • 1988-06-22
    • Klaus P. BogesoKlaus G. JensenEjner K. MoltzenHenrik Pedersen
    • Klaus P. BogesoKlaus G. JensenEjner K. MoltzenHenrik Pedersen
    • A61K31/4427A61K31/445A61P21/00A61P25/02A61P25/28C07D401/04C07D413/04C07D417/04
    • C07D401/04C07D413/04C07D417/04
    • The present invention relates to novel compounds of the following formula, where the dotted line designates an optional bond: ##STR1## wherein "het" designates a five membered heterocyclic ring which may include 1 or 2 double bonds and 1-4 heteroatoms selected from nitrogen, oxygen or sulphur, provided that "het" may not designate a 1,2,4- or 1,3,4-oxadiazole;R.sup.1 is selected from hydrogen, lower alkyl, optionally substituted with phenyl which may be substituted with halogen, lower alkyl, or lower alkoxy, or a group R.sup.6 --CO--NH--CH.sub.2 -- or R.sup.6 --O--CO--, wherein R.sup.6 is lower alkyl, branched or unbranched, or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy, lower alkoxy, or lower acyloxy;R.sup.2 and R.sup.3 are the same or different, each representing hydrogen, lower alkyl, cycloalkyl (3-6 C-atoms), lower alkenyl, lower alkadienyl, lower alkynyl, optionally substituted with hydroxy, halogen or phenyl, in which the phenyl group may be substituted with halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy; R.sup.2 and R.sup.3 may further, respectively, be selected from trifluoromethyl or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy, lower alkoxy or lower acyloxy, or R.sup.2 and R.sup.3 may, respectively, be a group OR.sup.7 or SR.sup.7 wherein R.sup.7 is defined as R.sup.2 or R.sup.3, andif "het" includes 2 or more carbon atoms, R.sup.4 and R.sup.5 are the same or different, and each is defined as R.sup.2 or R.sup.3, and if "het" includes only one carbon atom, there is only one substituent, R.sup.4, on the heterocyclic ring, and R.sup.4 is defined as R.sup.2 or R.sup.3,as well as individual stereo isomers and pharmaceutically acceptable acid addition salts thereof.The invention moreover relates to methods for the preparation of the compounds of formula I, to novel intermediates, to pharmaceutical compositions containing same and to methods for the treatment of disorders, caused by malfunction of the acetylcholine (AcCh) or muscarinic system, by administering a non-toxic effective amount of a compound of formula I.
    • 79. 发明申请
    • AUTOMATED ROOT CAUSE ANALYSIS
    • 自动原因分析
    • US20140163926A1
    • 2014-06-12
    • US14233744
    • 2011-12-09
    • Henrik Pedersen
    • Henrik Pedersen
    • G05B23/02
    • G05B23/02F01D17/02F01D21/00F01D21/003F02C9/00G05B23/0278G06Q10/0631G07C3/00
    • A method for performing computerized automated root cause analysis for a complex product, such as a turbine, and computer-readable medium encoded with programming instructions for performing such a root cause analysis are provided. The method may include: monitoring the product; detecting a product misbehavior; forming a misbehavior pattern with timeslots of normal operation and timeslots of misbehavior operation; comparing timeslots of the misbehavior pattern to corresponding timeslots of channels of information in at least one database relating to the product; measuring how close the misbehavior pattern numerically fits to the information; and automatically identifying a best numerical fit.
    • 提供了一种用于对复杂产品(例如涡轮机)执行计算机化的自动根本原因分析的方法以及用编程指令编码的用于执行这种根本原因分析的计算机可读介质。 该方法可以包括:监控产品; 检测产品的不当行为; 形成了正常运作时间和不当行为时间的不正当行为模式; 将不正当行为模式的时间间隔与至少一个与产品相关的数据库中的信息通道的相应时隙进行比较; 衡量不正当行为模式在数字上与信息的接近程度; 并自动识别最佳数值拟合。