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34 条记录 (耗时 0.044 秒)

    Process for the preparation of clausenamide
    12.
    发明授权
    Process for the preparation of clausenamide 失效
    制备克劳森酰胺的方法

    公开(公告)号：US4731456A

    公开(公告)日：1988-03-15

    申请号：US915309

    申请日：1986-10-03

    申请人： Wolfgang Hartwig

    发明人： Wolfgang Hartwig

    IPC分类号： C07D207/26 ,  C07D207/267 ,  C07D207/273 ,  C07D207/28 ,  C07D207/12

    CPC分类号： C07D207/26 ,  C07D207/273 ,  C07D207/28

    摘要： A new synthetic route to clausenamide having the formula ##STR1## has been found. It has been found that a compound of the formula ##STR2## can be oxidized to provide the stereochemically correctly configured product, clasuenamide. A number of new compounds useful in the total synthesis of clausenamide have also been found. These compounds have the general formula ##STR3## wherein R is ##STR4## and CH.sub.2 OH.

    摘要翻译： 已经找到了具有式“IMAGE”的新的克劳森酰胺的合成路线。 已经发现，式“化合物”的化合物可以被氧化以提供立体化学正确构型的产物巴拉那胺。 还发现了许多用于全合成克劳森酰胺的新化合物。 这些化合物具有通式“IMAGE”，其中R是＆lt; IMAGE＆gt;和CH2OH。

    Process for the preparation of 7-acylamino-3-hydroxy-cephem-4-carboxylic acids and 7-acylamino-3-hydroxy-1-dethia-1-oxacephem-4-carboxylic acids
    13.
    发明授权
    Process for the preparation of 7-acylamino-3-hydroxy-cephem-4-carboxylic acids and 7-acylamino-3-hydroxy-1-dethia-1-oxacephem-4-carboxylic acids 失效
    制备7-酰基氨基-3-羟基 - 头孢烯-4-羧酸和7-酰基氨基-3-羟基-1-脱硫-1-氧代四氢-4-羧酸的方法

    公开(公告)号：US4616084A

    公开(公告)日：1986-10-07

    申请号：US636470

    申请日：1984-07-31

    申请人： Dieter Habich ,  Wolfgang Hartwig

    发明人： Dieter Habich ,  Wolfgang Hartwig

    IPC分类号： C07C205/42 ,  C07D205/085 ,  C07D501/02 ,  C07D501/59 ,  C07D503/00 ,  C07D505/00 ,  A61K31/545

    CPC分类号： C07D505/00 ,  C07C201/12 ,  C07D205/085 ,  C07D503/00 ,  Y02P20/55

    摘要： A process for the preparation of a 7-acylamino-3-hydroxy-2-cephem-4-carboxylic acid, 7-acylamino-3-hydroxy-1-dethia-1-oxa-3-cephem-4-carboxylic acid or derivative thereof of the general formula ##STR1## in which R.sup.1 is hydrogen or optionally substituted alkyl, alkenyl, alkinyl, aralkyl, aryl, heteroaryl, heteroaralkyl, aryloxyalkyl, heteroaryloxyalkyl, alkoxyalkyl, arylthioalkyl, heteroarylthioalkyl, alkylthioalkyl, alkoxy, aryloxy, alkylthio or arylthio,R.sup.2 is hydrogen, a carboxy-protective group or a pharmaceutically useful ester radical, andX is sulphur or oxygen,which comprises:(a) reacting a compound of the formula ##STR2## with (i) a compound of the formula ##STR3## in which R.sup.2 and X have the abovementioned meaning and Y represents diazo (N.sub.2) or hydrogen (H.sub.2) in an inert solvent in the presence of a Lewis acid or proton acid catalyst, or(ii) a compound of the formulaHX--CH.sub.2 --C.tbd.C--COOR.sup.2 to form an intemediate compound having a triple bond, and hydrating the triple bond, the compounds thus obtained, for Y being hydrogen (H.sub.2)--(in case of Y=diazo (N.sub.2) directly the compounds of general formula (2) are obtained) thereby to produce a compound of the formula ##STR4## (b) reacting such compound with an azide in a solvent in the presence of a base to give a compound of the formula ##STR5## (c) converting said compound to the desired product by (i) irradiation in an inert solvent, or(ii) warming in the presence of a catalyst.The end products are, or can be converted to, known .beta.-lactam antibiotics.

    摘要翻译： 制备7-酰基氨基-3-羟基-2-头孢烯-4-羧酸，7-酰基氨基-3-羟基-1-脱硫-1-氧杂-3-头孢烯-4-羧酸或其衍生物的方法 烯基，炔基，芳烷基，芳基，杂芳基，杂芳烷基，芳氧基烷基，杂芳基氧基烷基，烷氧基烷基，芳硫基烷基，杂芳硫基烷基，烷硫基烷基，烷氧基，芳氧基，烷硫基或芳硫基，其中R 1为氢或任选取代的烷基， R2是氢，羧基保护基或药学上有用的酯基，X是硫或氧，其包括：（a）使式（IMAGE）的化合物与（i）下式化合物 其中R2和X具有上述含义，Y代表重氮（N 2）或氢（H 2）在惰性溶剂中，在路易斯酸或质子酸催化剂存在下，或（ii）式HX-CH2- C 3 C COR CO 2，以形成具有三键的中间体化合物，并且使三键水合，该共聚物 （H）在（Y =重氮（N 2）的情况下直接得到通式（2）的化合物），得到下式的化合物：（b）使此 在碱的存在下在溶剂中与叠氮化合物反应，得到下式的化合物：（c）通过（i）在惰性溶剂中照射将所述化合物转化为所需产物，或（ii）在 存在催化剂。 最终产品是或可以转化为已知的β-内酰胺抗生素。

    Method and device for providing automatic load alleviation to a high lift surface system, in particular to a landing flap system, of an aircraft
    14.
    发明授权
    Method and device for providing automatic load alleviation to a high lift surface system, in particular to a landing flap system, of an aircraft 有权
    一种提供自动负载减轻的方法和装置，用于飞机的高升力面系统，特别是降落翼系统

    公开(公告)号：US08256718B2

    公开(公告)日：2012-09-04

    申请号：US12086467

    申请日：2006-12-08

    申请人： Andreas Fleddermann ,  Wolfgang Hartwig ,  Alexandre Darbois ,  Martin Richter

    发明人： Andreas Fleddermann ,  Wolfgang Hartwig ,  Alexandre Darbois ,  Martin Richter

    IPC分类号： B64C13/00 ,  G05D1/00

    CPC分类号： B64C13/16

    摘要： A method and a device for providing automatic load alleviation to a high lift surface system, in particular to a landing flap system, of an aircraft when a blockage occurs, wherein in response to a control signal emitted by a control device at least one high lift surface, which is actuated by means of a local mechanical final control element, is brought to a predetermined position by a central drive unit that is connected by way of a rotary shaft arrangement to the local final control element by generating a torque transmitted by the central drive unit to the rotary shaft arrangement. If a signal is registered that indicates that there is a blockage within the high lift surface system, the torque transmitted by the central drive unit to the rotary shaft arrangement is automatically reduced to a predetermined low torque value, and the position of the high lift surface system is fixed.

    摘要翻译： 一种方法和装置，用于在发生堵塞时向飞行器的高升力表面系统（特别是着陆翼片系统）提供自动负载减轻，其中响应于由控制装置发射的控制信号，至少一个高升程 通过局部机械终控制元件致动的表面通过中心驱动单元被带到预定位置，该中心驱动单元通过旋转轴装置连接到局部最终控制元件，通过产生由中心传递的扭矩 驱动单元到旋转轴装置。 如果登记指示高升力面系统内存在阻塞的信号，则由中央驱动单元传递给旋转轴装置的扭矩自动降低到预定的低扭矩值，并且高升程面的位置 系统固定。

    Peptides and peptidomimetics with structural similarity to human p53 that activate p53 function
    15.
    发明授权
    Peptides and peptidomimetics with structural similarity to human p53 that activate p53 function 有权
    肽和肽模拟物与人p53的结构相似性激活p53功能

    公开(公告)号：US07189801B2

    公开(公告)日：2007-03-13

    申请号：US10160290

    申请日：2002-06-04

    申请人： Thanos Halazonetis ,  Wolfgang Hartwig

    发明人： Thanos Halazonetis ,  Wolfgang Hartwig

    IPC分类号： C07K5/00

    CPC分类号： A61K38/1709 ,  C07K14/4746 ,  C07K14/82

    摘要： The present invention provides peptides and peptidomimetics corresponding to part or to the entirety of the region encompassed by residues 360–386 of human p53, said peptides and peptidomimetics characterized by the ability to activate DNA binding of wild-type p53 and of select tumor-derived p53 mutants. Pharmaceutical compositions of the compounds of the invention and methods of using these compositions therapeutically are also provided.

    摘要翻译： 本发明提供了对应于人p53的残基360-386所包含的部分或整个区域的肽和肽模拟物，所述肽和肽模拟物的特征在于活化野生型p53和选择性肿瘤衍生物的DNA结合的能力 p53突变体。 还提供了本发明化合物的药物组合物和治疗性使用这些组合物的方法。

    Peptides and peptidomimetics with structural similarity to human P53 that activate P53 function
    16.
    发明授权
    Peptides and peptidomimetics with structural similarity to human P53 that activate P53 function 失效
    肽和肽模拟物与人类P53的结构相似性激活P53功能

    公开(公告)号：US06245886B1

    公开(公告)日：2001-06-12

    申请号：US08894327

    申请日：1997-12-04

    申请人： Thanos Halazonetis ,  Wolfgang Hartwig

    发明人： Thanos Halazonetis ,  Wolfgang Hartwig

    IPC分类号： A61K3800

    CPC分类号： A61K38/1709 ,  C07K14/4746 ,  C07K14/82

    摘要： The present invention provides peptides and peptidomimetics corresponding to part or to the entirety of the region encompassed by residues 360-386 of human p53, said peptides and peptidomimetics characterized by the ability to activate DNA binding of wild-type p53 and to select tumor-derived p53 mutants. Pharmaceutical compositions of the compounds of the invention and methods of using these compositions therapeutically are also provided.

    摘要翻译： 本发明提供了对应于人p53的残基360-386所包含的部分或全部区域的肽和肽模拟物，所述肽和肽模拟物的特征在于活化野生型p53的DNA结合的能力，并选择肿瘤衍生的 p53突变体。 还提供本发明化合物的药物组合物和治疗性使用这些组合物的方法。

    Peptides and peptidomimetics with structural similarity to human p53 that activate p53 function
    17.
    发明授权
    Peptides and peptidomimetics with structural similarity to human p53 that activate p53 function 失效
    肽和肽模拟物与人p53的结构相似性激活p53功能

    公开(公告)号：US06169073A

    公开(公告)日：2001-01-02

    申请号：US08392542

    申请日：1995-02-16

    申请人： Thanos Halazonetis ,  Wolfgang Hartwig

    发明人： Thanos Halazonetis ,  Wolfgang Hartwig

    IPC分类号： A61K3800

    CPC分类号： A61K38/1709 ,  C07K14/4746 ,  C07K14/82

    摘要： The present invention provides peptides and peptidomimetics corresponding to part or to the entirety of the region encompassed by residues 360-386 of human p53, said peptides and peptidomimetics characterized by the ability to activate DNA binding of wild-type p53 and of select tumor-derived p53 mutants. Pharmaceutical compositions of the compounds of the invention and methods of using these compositions therapeutically are also provided.

    摘要翻译： 本发明提供了对应于人p53的残基360-386所包含的部分或整个区域的肽和肽模拟物，所述肽和肽模拟物的特征在于活化野生型p53和选择性肿瘤衍生物的DNA结合的能力 p53突变体。 还提供本发明化合物的药物组合物和治疗性使用这些组合物的方法。

    Process for the preparation of 2,3-epoxyamides
    19.
    发明授权
    Process for the preparation of 2,3-epoxyamides 失效
    2,3-环氧酰胺的制备方法

    公开(公告)号：US4849531A

    公开(公告)日：1989-07-18

    申请号：US043664

    申请日：1987-04-28

    申请人： Dieter Habich ,  Wolfgang Hartwig

    发明人： Dieter Habich ,  Wolfgang Hartwig

    IPC分类号： C07B61/00 ,  B01J31/00 ,  C07D303/48

    CPC分类号： C07D303/48 ,  Y02P20/55

    摘要： A process for the preparation of a 2,3-epoxyamide of the formula ##STR1## in which R.sup.1 represents hydrogen or straight-chain or branched C.sub.1 -C.sub.8 -alkyl, which may be substituted by phenyl or halogen, or represents C.sub.3 -C.sub.7 -cycloalkyl, phenyl, C.sub.1 -C.sub.8 -alkoxycarbonyl, or a group of the formula ##STR2## in which R.sup.4 and R.sup.5 are identical or different and denote hydrogen, phenyl, benzyl, acetyl or C.sub.1 -C.sub.8 -alkyl which is optionally substituted by phenyl or halogen,R.sup.2 represents hydrogen or an amino protecting group andR.sup.3 represents a radical which activates the methylene group,comprising reacting a 2-halogeno-3-hydroxyamide of the formula ##STR3## in which X represents fluorine, chlorine, bromine or iodine,with an alkali metal hydroxide in an inert solvent.

    摘要翻译： 制备式“IMAGE”的2,3-环氧酰胺的方法，其中R 1表示氢或可被苯基或卤素取代的直链或支链C 1 -C 8 - 烷基，或代表C 3 -C 7 - 环烷基，苯基，C 1 -C 8 - 烷氧基羰基或其中R 4和R 5相同或不同并表示氢，苯基，苄基，乙酰基或任选被苯基取代的C 1 -C 8 - 烷基的式 卤素，R 2表示氢或氨基保护基，R 3表示活化亚甲基的基团，包括将其中X表示氟，氯，溴或碘的式“IMAGE”的2-卤代-3-羟基酰胺与 在惰性溶剂中的碱金属氢氧化物。

    Peptides and Peptidomimetics with Structural Similarity to Human p53 that Activate p53 Function
    20.
    发明申请
    Peptides and Peptidomimetics with Structural Similarity to Human p53 that Activate p53 Function 失效
    肽和肽模拟物与人p53的结构相似性激活p53功能

    公开(公告)号：US20070167611A1

    公开(公告)日：2007-07-19

    申请号：US11684285

    申请日：2007-03-09

    申请人： Thanos Halazonetis ,  Wolfgang Hartwig

    发明人： Thanos Halazonetis ,  Wolfgang Hartwig

    IPC分类号： C07K14/705

    CPC分类号： A61K38/1709 ,  C07K14/4746 ,  C07K14/82

    摘要： The present invention provides peptides and peptidomimetics corresponding to part or to the entirety of the region encompassed by residues 360-386 of human p53, said peptides and peptidomimetics characterized by the ability to activate DNA binding of wild-type p53 and of select tumor-derived p53 mutants. Pharmaceutical compositions of the compounds of the invention and methods of using these compositions therapeutically are also provided.

    摘要翻译： 本发明提供了对应于人p53的残基360-386所包含的部分或整个区域的肽和肽模拟物，所述肽和肽模拟物的特征在于活化野生型p53和选择性肿瘤衍生物的DNA结合的能力 p53突变体。 还提供了本发明化合物的药物组合物和治疗性使用这些组合物的方法。