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1. 发明授权

US5639867A TTTr as protective group in nucleotide synthesis 失效
标题翻译： TTTr作为核苷酸合成中的保护基
公开(公告)号：US5639867A
公开(公告)日：1997-06-17
申请号：US304456
申请日：1994-09-12
申请人： Wolfgang K.-D. Brill
发明人： Wolfgang K.-D. Brill
IPC分类号： C07H19/04 , C07H19/06 , C07H19/16 , C07H21/00 , C07H21/04 , C07H1/00
CPC分类号： C07H19/06 , C07H19/04 , C07H19/16 , C07H21/00 , Y02P20/55
摘要： The invention relates to nucleosides, nucleotides and oligonucleotides carrying in their basic structure a primary hydroxyl group protected by tris-4,4',4"-tert-butylphenylmethyl, to processes for the preparation of said nucleosides and nucleotides, to a process for the preparation of oligonucleotides, and to the use of said protected nucleosides, nucleotides and oligonucleotides.
摘要翻译：本发明涉及核苷，核苷酸和寡核苷酸，其基本结构是由三-4,4'，4“ - 叔丁基苯基甲基保护的伯羟基，用于制备所述核苷和核苷酸的方法，寡核苷酸的制备，以及使用所述被保护的核苷，核苷酸和寡核苷酸。

2. 发明授权

US5686457A Pyrrolopyrimidine derivatives having pharmacological activity 失效
标题翻译：具有药理活性的吡咯并嘧啶衍生物
公开(公告)号：US5686457A
公开(公告)日：1997-11-11
申请号：US434419
申请日：1995-05-03
申请人： Peter Traxler , Pascal Furet , Wolfgang K.-D. Brill
发明人： Peter Traxler , Pascal Furet , Wolfgang K.-D. Brill
IPC分类号： C07D498/02 , A61K31/495 , A61K31/505 , A61K31/519 , A61P17/06 , A61P35/00 , A61P37/02 , A61P43/00 , C07D20060101 , C07D207/18 , C07D239/42 , C07D487/04 , C07D403/02
CPC分类号： C07D487/04
摘要： The invention relates to the use of the compounds mentioned below in the therapeutic treatment of tumour diseases and other proliferative diseases, such as psoriasis, and to novel compounds of that type. The compounds are compounds of formula I ##STR1## wherein n is from 0 to 5 and, when n is not 0, R is one or more substituents selected from halogen, alkyl, trifluoromethyl and alkoxy; and R.sub.1 and R.sub.2 are each independently of the other alkyl, or phenyl that is unsubstituted or substituted by halogen, trifluoromethyl, alkyl or by alkoxy, it also being possible for one of the two radicals R.sub.1 and R.sub.2 to be hydrogen, or R.sub.1 and R.sub.2 together form an alkylene chain having from 2 to 5 carbon atoms that is unsubstituted or substituted by alkyl; or salts thereof. Compounds of formula I inhibit protein kinases, for example the tyrosine protein kinase of the receptor for the epidermal growth factor, EGF.
摘要翻译：本发明涉及下述化合物在肿瘤疾病和其它增殖性疾病如牛皮癣的治疗性治疗中的用途，以及该类型的新型化合物。化合物是式I化合物，其中n为0至5，当n不为0时，R为一个或多个选自卤素，烷基，三氟甲基和烷氧基的取代基; 并且R 1和R 2各自独立地为未被取代或被卤素，三氟甲基，烷基或烷氧基取代的苯基，也可以是两个基团R 1和R 2中的一个为氢，或者R 1和R 2 一起形成未被取代或被烷基取代的具有2至5个碳原子的亚烷基链; 或其盐。式I的化合物抑制蛋白激酶，例如表皮生长因子受体的酪氨酸蛋白激酶EGF。

3. 发明授权

US6096749A Pyrrolopyrimidine derivatives having pharmacological activity 失效
标题翻译：具有药理活性的吡咯并嘧啶衍生物
公开(公告)号：US6096749A
公开(公告)日：2000-08-01
申请号：US53266
申请日：1998-04-01
申请人： Peter Traxler , Pascal Furet , Wolfgang K.-D. Brill
发明人： Peter Traxler , Pascal Furet , Wolfgang K.-D. Brill
IPC分类号： C07D498/02 , A61K31/495 , A61K31/505 , A61K31/519 , A61P17/06 , A61P35/00 , A61P37/02 , A61P43/00 , C07D20060101 , C07D207/18 , C07D239/42 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to the use of the compounds mentioned below in the therapeutic treatment of tumor diseases and other proliferative diseases, such as psoriasis, and to novel compounds of that type. The compounds are compounds of formula I ##STR1## wherein n is from 0 to 5 and, when n is not 0,R is one or more substituents selected from halogen, alkyl, trifluoromethyl and alkoxy; andR.sub.1 and R.sub.2 are each independently of the other alkyl, or phenyl that is unsubstituted or substituted by halogen, trifluoromethyl, alkyl or by alkoxy, it also being possible for one of the two radicals R.sub.1 and R.sub.2 to be hydrogen, or R.sub.1 and R.sub.2 together form an alkylene chain having from 2 to 5 carbon atoms that is unsubstituted or substituted by alkyl;or salts thereof. Compounds of formula I inhibit protein kinases, for example the tyrosine protein kinase of the receptor for the epidermal growth factor, EGF.
摘要翻译：本发明涉及下述化合物在肿瘤疾病和其它增殖性疾病如牛皮癣的治疗性治疗中的用途，以及该类型的新型化合物。化合物是其中n为0至5的式I化合物，当n不为0时，R为一个或多个选自卤素，烷基，三氟甲基和烷氧基的取代基; 并且R 1和R 2各自独立地为未被取代或被卤素，三氟甲基，烷基或烷氧基取代的苯基，也可以是两个基团R 1和R 2中的一个为氢，或者R 1和R 2 一起形成未被取代或被烷基取代的具有2至5个碳原子的亚烷基链; 或其盐。式I的化合物抑制蛋白激酶，例如表皮生长因子受体的酪氨酸蛋白激酶EGF。

4. 发明授权

US5750666A Polynucleotide phosphorodithioate compounds 失效
标题翻译：多核苷酸二硫代磷酸酯化合物
公开(公告)号：US5750666A
公开(公告)日：1998-05-12
申请号：US332829
申请日：1994-10-31
申请人： Marvin H. Caruthers , Wolfgang K.-D Brill , Eric Yau , Michael Ma , John Nielsen
发明人： Marvin H. Caruthers , Wolfgang K.-D Brill , Eric Yau , Michael Ma , John Nielsen
IPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04 , C12N5/10 , C12N9/99 , C12Q1/68
CPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04
摘要： The present invention relates to new and useful nucleoside thiophosphoroamidites and polynucleotide phosphorodithioate compounds as well as the processes whereby these compounds may be used for synthesizing new mononucleotides and polynucleotides having phosphorothioate and phosphorodithioate internucleotide linkages.
摘要翻译：本发明涉及新的和有用的核苷硫代亚磷酰胺和多核苷酸二硫代磷酸酯化合物以及这些化合物可用于合成新的单核苷酸和具有硫代磷酸酯和二硫代磷酸酯核苷酸间键的多核苷酸的方法。

5. 发明授权

US5268464A Process for the preparation of nucleosides 失效
标题翻译：制备核苷的方法
公开(公告)号：US5268464A
公开(公告)日：1993-12-07
申请号：US31455
申请日：1993-03-15
申请人： Wolfgang K. D. Brill
发明人： Wolfgang K. D. Brill
IPC分类号： C07H1/00 , C07H19/04 , C07H19/073 , C07H19/173 , C07H21/00 , C07H19/056 , C07H21/02
CPC分类号： C07H19/04 , C07H21/00 , Y02P20/55
摘要： A process for the preparation of natural or synthetic nucleosides, nucleoside analogs or oligonucleotides from at least two such nucleosides and/or nucleoside analogs whose basic molecule contains an unsubstituted or substituted radical of a nucleic base B and a protected hydroxyl group of formula R.sub.1 --O--, wherein R.sub.1 is a protective group, or which are linked to the oxygen atom of a hydroxyl group direct or to a solid support through a linking group, from nucleoside monomers or from oligonucleotides to the basic molecule of which, in addition to said radicals, a group of formula I, Ia or Ib ##STR1## is attached, by converting the group of formula I, Ia or Ib into a hydroxyl group --OH by reacting the nucleosides or oligonucleotides, in the absence or presence of an inert organic solvent, with an excess of an aliphatic, cycloaliphatic araliphatic or aromatic alcohol containing 1 to 30 carbon atoms, a polyol containing 2 to 50 carbon atoms or a polymeric polyol, in the presence of at least a catalytic amount of an inorganic base or of an organic nitrogen base, which base has a pK value of 4 to 10.
摘要翻译：从至少两种这样的核苷和/或核苷类似物制备天然或合成核苷，核苷类似物或寡核苷酸的方法，其碱基分子含有核酸B的未取代或取代的基团和式R1-O的被保护的羟基 - 其中R 1是保护基，或者通过连接基团直接连接到羟基的氧原子或连接到固体支持物上，从核苷单体或从寡核苷酸到除了所述基团之外的碱基分子通过将式I，Ia或Ib的基团通过将式I，Ia或Ib的基团转化为羟基-OH而通过将式I，Ia或Ib的基团转化成羟基-OH 在不存在或存在惰性有机溶剂的条件下使过量的含有1至30个碳原子的脂肪族，脂环族芳脂族或芳族醇，含有2-50个碳原子的多元醇或聚合物聚在至少一种催化量的无机碱或有机氮碱的存在下，该碱的pK值为4-10。

6. 发明授权

US5602244A Polynucleotide phosphorodithioate compounds 失效
标题翻译：多核苷酸二硫代磷酸酯化合物
公开(公告)号：US5602244A
公开(公告)日：1997-02-11
申请号：US436714
申请日：1995-05-08
申请人： Marvin H. Caruthers , Wolfgang K.-D. Brill , Eric Yau , Michael Ma , John Nielsen
发明人： Marvin H. Caruthers , Wolfgang K.-D. Brill , Eric Yau , Michael Ma , John Nielsen
IPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04
摘要： Dinucleoside phosphorodithioate phosphoramidite precursors useful in the synthesis of oligonucleotide phosphorodithioate which can be used as antisense inhibitors of translation.
摘要翻译：用于合成寡核苷酸二硫代磷酸酯的二核苷酸二硫代磷酸亚磷酸酯前体，其可用作翻译的反义抑制剂。

7. 发明授权

US5684148A Nucleoside thiophosphoramidites 失效
标题翻译：核苷硫代亚磷酰胺
公开(公告)号：US5684148A
公开(公告)日：1997-11-04
申请号：US442705
申请日：1995-05-17
申请人： Marvin H. Caruthers , Wolfgang K. D. Brill , Eric Yau , Michael Ma , John Nielsen
发明人： Marvin H. Caruthers , Wolfgang K. D. Brill , Eric Yau , Michael Ma , John Nielsen
IPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04
摘要： The present invention relates to new and useful nucleoside thiophosphoroamidites and polynucleotide phosphorodithioate compounds as well as the processes whereby these compounds may be used for synthesizing new mononucleotides and polynucleotides having phosphorothioate and phosphorodithioate internucleotide linkages.
摘要翻译：本发明涉及新的和有用的核苷硫代亚磷酰胺和多核苷酸二硫代磷酸酯化合物以及这些化合物可用于合成新的单核苷酸和具有硫代磷酸酯和二硫代磷酸酯核苷酸间键的多核苷酸的方法。

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