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31.发明授权Polyamide nucleic acid derivatives and agents and processes for preparing them 有权聚酰胺核酸衍生物及其制备方法及其制备方法公开(公告)号：US06777544B2
公开(公告)日：2004-08-17
申请号：US09835370
申请日：2001-04-17
IPC分类号： C12Q168
CPC分类号： C07H21/00
摘要： The present invention relates to PNA derivatives which carry, at the N terminus of the PNA backbone, a phosphoryl radical. The phosphoryl radical can be, for example, a phosphate radical, or a substituted phosphoryl radical, with substituted phosphoryl derivatives carrying, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the abovementioned PNA derivatives and to their use as pharmaceuticals and diagnostic agents.
摘要翻译： 本发明涉及在PNA主链的N末端携带磷酰基的PNA衍生物。 磷酰基可以是例如磷酸根或取代的磷酰基，其中取代的磷酰基衍生物在适当的情况下携带一个或多个标记基团，交联基团，促进细胞内摄取的基团或增加结合的基团 PNA衍生物对核酸的亲和力。 本发明还涉及制备上述PNA衍生物的方法及其作为药物和诊断剂的用途。
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32.发明授权Polymide nucleic acid derivatives, and agents and processes for preparing them 失效聚酰亚胺核酸衍生物，及其制备方法和制备方法公开(公告)号：US08268560B2
公开(公告)日：2012-09-18
申请号：US13012266
申请日：2011-01-24
申请人： Eugen Uhlmann , Gerhard Breipohl , David W. Will
发明人： Eugen Uhlmann , Gerhard Breipohl , David W. Will
CPC分类号： C07K14/003 , A61K38/00 , Y10T436/143333
摘要： The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.
摘要翻译： 本发明涉及在C末端或在PNA主链的C和N末端携带一个或多个磷酰基的PNA衍生物。 磷酰基在适当的情况下携带一个或多个标记基团，用于交联的基团，促进细胞内摄取的基团，或增加PNA衍生物对核酸的结合亲和力的基团。 本发明还涉及制备上述PNA衍生物的方法及其作为药物或诊断剂的用途。
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公开(公告)号：US20050026817A1
公开(公告)日：2005-02-03
申请号：US10939214
申请日：2004-09-10
申请人： Eugen Uhlmann , Gerhard Breipohl
发明人： Eugen Uhlmann , Gerhard Breipohl
CPC分类号： C07H21/00 , A61K47/59 , A61K47/595 , A61K47/60 , A61K47/605 , C07K14/003
摘要： Polyamide-oligonucleotide derivatives of the formula F[(DNA-Li)q(PNA-Li)r(DNA-Li)s(PNA)t]xF′wherein q, r, s, t are, independently of one another, zero or 1, where the total of two or more adjacent q, r, s and t≧2; x is 1 to 20; DNA is a nucleic acid such as DNA or RNA or a known derivative thereof; Li is a covalent linkage between DNA and PNA, where the covalent linkage comprises a bond or an organic radical with at least one atom from the series consisting of C, N, O or S; PNA is a polyamide structure which contains at least one nucleotide base which is different from thymine; and F and F′ are end groups and/or are linked together by a covalent bond, and the physiologically tolerated salts thereof, a process for their preparation and their use as pharmaceutical, as gene probe and as primer, are described.
摘要翻译： 式F [（DNA-Li）q（PNA-Li）r（DNA-Li）s（PNA）t] xF'的聚酰胺 - 寡核苷酸衍生物其中q，r，s，t彼此独立地为零 或1，其中两个或更多个相邻q，r，s和t> = 2的总和; x为1〜20; DNA是核酸如DNA或RNA或其已知衍生物; Li是DNA与PNA之间的共价连接，其中共价连接包含与C，N，O或S组成的系列中至少一个原子的键或有机基团; PNA是含有与胸腺嘧啶不同的至少一个核苷酸碱基的聚酰胺结构; 并且F和F'是端基和/或通过共价键连接在一起，并且描述了其生理学上耐受的盐，它们的制备方法及其作为药物的用途，作为基因探针和引物。
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34.发明授权
公开(公告)号：US5874553A
公开(公告)日：1999-02-23
申请号：US613417
申请日：1996-03-11
IPC分类号： A61K31/66 , A01N43/04 , A61K31/7088 , A61P31/16 , A61P31/18 , A61P35/00 , A61P43/00 , C07F9/38 , C07F9/40 , C07H19/00 , C07H21/00 , C07H21/02 , C07K14/00 , C12Q1/68 , C12Q1/70 , A01N61/00
CPC分类号： C07H21/00 , C07F9/4006 , C07F9/4087 , C07K14/003
摘要： Novel oligonucleotide analogs of the formula (I) are described, ##STR1## in which A, B, D, G, L, P, Q, Q', R.sup.5, R.sup.6, X, Y, Z and n are as defined in the description, which have useful physical, biological and pharmacological properties, as well as a process for their preparation. Their application relates to use as inhibitors of gene expression (antisense oligonucleotides, ribozymes, sense oligonucleotides and triplex-forming oligonucleotides), as probes for the detection of nucleic acids and as auxiliaries in molecular biology.
摘要翻译： 描述式（I）的新型寡核苷酸类似物，其中A，B，D，G，L，P，Q，Q'，R 5，R 6，X，Y，Z和n分别为 在描述中定义，其具有有用的物理，生物和药理学性质，以及它们的制备方法。 其应用涉及用作基因表达抑制剂（反义寡核苷酸，核酶，有义寡核苷酸和三重复合形成寡核苷酸），作为用于检测核酸的探针和分子生物学中的辅助物质。
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35.发明申请POLYAMIDE NUCLEIC ACID DERIVATIVES AND AGENTS, AND PROCESSES FOR PREPARING THEM 失效聚酰胺核酸衍生物和药剂及其制备方法公开(公告)号：US20100022016A1
公开(公告)日：2010-01-28
申请号：US12474532
申请日：2009-05-29
申请人： Eugen UHLMANN , Gerhard Breipohl , David W. Will
发明人： Eugen UHLMANN , Gerhard Breipohl , David W. Will
IPC分类号： G01N33/50
CPC分类号： C07K14/003 , A61K38/00 , Y10T436/143333
摘要： The present invention relates to PNA derivatives which carry, at the C terminus, or at both the C and N termini of the PNA backbone, one or more phosphoryl radicals. The phosphoryl radicals carry, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the above-mentioned PNA derivatives and to their use as pharmaceuticals or diagnostic agents.
摘要翻译： 本发明涉及在C末端或在PNA主链的C和N末端携带一个或多个磷酰基的PNA衍生物。 磷酰基在适当的情况下携带一个或多个标记基团，用于交联的基团，促进细胞内摄取的基团，或增加PNA衍生物对核酸的结合亲和力的基团。 本发明还涉及制备上述PNA衍生物的方法及其作为药物或诊断剂的用途。
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36.发明授权Process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides 有权制备乙酰基 - 脒基苯丙氨酰 - 环己基甘氨酰 - 吡啶并氨酰胺的方法公开(公告)号：US07084250B2
公开(公告)日：2006-08-01
申请号：US10869076
申请日：2004-06-17
IPC分类号： C07K5/08
CPC分类号： C07K5/0821 , C07K5/06139
摘要： The present invention relates to a process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides of the formula I, in which the anions X are physiologically acceptable anions, and their analogs, which are effective inhibitors of the blood coagulation factor Xa and which can be used, for example, for preventing thromboses. The process according to the invention comprises the coupling of 2-[2-acetylamino-3-(4-amidinophenyl)propionylamino]-2-cyclohexylacetic acid, which is obtained from 2-[2-acetylamino-3-(4-cyanophenyl)acryloylamino]-2-cyclohexylacetic acid by asymmetric hydrogenation and conversion of the cyano group into the amidine, or a salt thereof, with a 3-(2-amino-2-carbamoylethyl)-1-methylpyridinium salt or a salt thereof. The invention furthermore provides starting materials and intermediates for this process, processes for their preparation and acetyl-(S)-4-amidiniophenylalanyl-(S)-cyclohexylglycyl-(S)-(1-methyl-3-pyridinio)alaninamide as ditosylate salt.
摘要翻译： 本发明涉及一种制备式I的乙酰基 - 脒基苯脒基 - 环己基甘氨酰 - 吡啶并吡喃酰胺的方法，其中阴离子X是生理上可接受的阴离子，以及它们的类似物，它们是凝血因子Xa的有效抑制剂， 可用于例如用于预防血栓形成。 根据本发明的方法包括2- [2-乙酰氨基-3-（4-脒基苯基）丙酰基氨基] -2-环己基乙酸的偶联，其由2- [2-乙酰氨基-3-（4-氰基苯基） 丙烯酰氨基] -2-环己基乙酸，通过不对称氢化，并将氰基转化为脒或其盐与3-（2-氨基-2-氨基甲酰基乙基）-1-甲基吡啶鎓盐或其盐。 本发明还提供了该方法的起始原料和中间体，其制备方法和乙酰基 - （S）-4-脒基苯基丙氨酰 - （S） - 环己基甘氨酰 - （S） - （1-甲基-3-吡啶鎓）丙烯酰胺作为二甲苯磺酸盐 。
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37.发明授权公开(公告)号：US06437136B1
公开(公告)日：2002-08-20
申请号：US09842832
申请日：2001-04-27
IPC分类号： C07D21102
摘要： Disclosed is a method for producing (−)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine characterized in that 1-methyl-piperidine-4-one is converted into hydrobromide, subsequently transformed with bromine into 3(R,S)-bromine-1-methyl-4-oxo-piperidine-hydrobromide and reacted with 1,3,5-trimethoxybenzol to form 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide. By stirring the reaction solution into an organic solvent, 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide is initially isolated as a solid and subsequently the product is mixed with water and converted into 3(R,S)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine by means of stirring. The product thus prepared is catalytically hydrogenated into a racemic 3,4-cis-alcohol and subsequently, enantiomerically pure (−)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine is obtained by separation of racemic mixtures with chiral auxiliary reagents from racemic 3,4-cis alcohol.
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38.发明授权Method for producing (−)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine 有权（ - ）顺式-3-羟基-1-甲基-4-（2,4,6-三甲氧基苯基） - 哌啶的制备方法公开(公告)号：US06225473B1
公开(公告)日：2001-05-01
申请号：US09600775
申请日：2000-07-21
IPC分类号： C07D21102
CPC分类号： C07D405/04 , C07D211/42 , C07D211/72 , C07D211/74
摘要： Disclosed is a method for producing (−)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine characterised in that 1-methyl-piperidine-4-one is converted into hydrobromide, subsequently transformed with bromine into 3(R,S)-bromine-1-methyl-4-oxo-pyridine-hydrobromide and reacted with 1,3,5-trimethoxyphenyl to form 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide. By stirring the reaction solution into an organic solvent, 3(R,S)-bromine-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine-hydrobromide is initially isolated as a solid and subsequently the product is mixed with water and converted into 3(R,S)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine by means of stirring. The product thus prepared is catalytically hydrogenated into a racemic 3,4-cis-alcahol and subsequently, enantiomerically pure (−)cis-3-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidine is obtained by separation of recemic mixtures with chiral auxiliary reagents from recemic 3,4-cis alcohol.
摘要翻译： 公开了一种制备（ - ）顺式-3-羟基-1-甲基-4-（2,4,6-三甲氧基苯基） - 哌啶的方法，其特征在于将1-甲基 - 哌啶-4-酮转化成氢溴酸盐，随后 用溴转化成3（R，S） - 溴-1-甲基-4-氧代 - 吡啶 - 氢溴酸盐，并与1,3,5-三甲氧基苯基反应形成3（R，S） - 溴-1-甲基-4 （2,4,6-三甲氧基苯基）-1,2,3,6-四氢 - 吡啶 - 氢溴酸盐。 通过将反应溶液搅拌成有机溶剂，最初将3（R，S） - 溴-1-甲基-4-（2,4,6-三甲氧基苯基）-1,2,3,6-四氢 - 吡啶 - 氢溴酸盐 分离为固体，随后将产物与水混合并转化成3（R，S） - 羟基-1-甲基-4-（2,4,6-三甲氧基苯基）-1,2,3,6-四氢 - 吡啶通过搅拌。 将如此制备的产物催化氢化成外消旋的3,4-顺式醇，然后得到对映体纯的（ - ）顺式-3-羟基-1-甲基-4-（2,4,6-三甲氧基苯基） - 哌啶 通过从接受的3,4-顺式乙醇中分离具有手性辅助试剂的接收混合物。
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39.发明授权
公开(公告)号：US6127346A
公开(公告)日：2000-10-03
申请号：US196132
申请日：1998-11-20
IPC分类号： A61K31/66 , A01N43/04 , A61K31/7088 , A61P31/16 , A61P31/18 , A61P35/00 , A61P43/00 , C07F9/38 , C07F9/40 , C07H19/00 , C07H21/00 , C07H21/02 , C07K14/00 , C12Q1/68 , C12Q1/70
CPC分类号： C07H21/00 , C07F9/4006 , C07F9/4087 , C07K14/003
摘要： Novel oligonucleotide analogs of the formula [I] are described, ##STR1## in which A, B, D, G, L, P, Q, Q', R.sup.5, R.sup.6, X, Y, Z and n are as defined in the description, which have useful physical, biological and pharmacological properties, as well as a process for their preparation. Their application relates to use as inhibitors of gene expression (antisense oligonucleotides, ribozymes, sense oligonucleotides and triplex-forming oligonucleotides), as probes for the detection of nucleic acids and as auxiliaries in molecular biology.
摘要翻译： 描述了式[I]的新型寡核苷酸类似物，其中A，B，D，G，L，P，Q，Q'，R 5，R 6，X，Y，Z和n如说明书中所定义， 具有有用的物理，生物和药理性质，以及它们的制备方法。 其应用涉及用作基因表达抑制剂（反义寡核苷酸，核酶，有义寡核苷酸和三重复合形成寡核苷酸），作为用于检测核酸的探针和分子生物学中的辅助物质。
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公开(公告)号：US5908828A
公开(公告)日：1999-06-01
申请号：US497599
申请日：1995-06-30
摘要： The present invention provides synthetic peptide derivatives represented by the formulaP.sup.1 -R.sup.1 -P.sup.2wherein P.sup.1 is a peptide having an amino acid sequence in the SEQ ID NO.:1 of the Sequence Listing, or analogues thereof; P.sup.2 is a peptide having an amino acid sequence in the SEQ ID NO.:2 of the Sequence Listing, or analogues thereof; R.sup.1 denotes a linker with a property that does not interfere with the activity of the each peptide P.sup.1 and P.sup.2 to bind N-terminal end of the peptides P.sup.1 and P.sup.2.The present invention also provides a pharmaceutical composition for the treatment of bone related diseases comprising said peptide derivatives, or a therapeutically acceptable salt thereof, and a pharmaceutically acceptable carrier.The present invention also provides a method of treating bone related diseases in a mammal comprising administering thereto an effective amount of said peptide derivatives, or therapeutically acceptable salts thereof.
摘要翻译： 本发明提供由式P1-R1-P2表示的合成肽衍生物，其中P1是具有序列表SEQ ID NO：1中的氨基酸序列的肽或其类似物; P2是具有序列表的SEQ ID NO：2中的氨基酸序列的肽或其类似物; R1表示具有不影响各肽P1和P2与肽P1和P2的N末端结合的活性的性质的连接体。 本发明还提供了用于治疗骨相关疾病的药物组合物，其包含所述肽衍生物或其治疗上可接受的盐和药学上可接受的载体。 本发明还提供了治疗哺乳动物中骨相关疾病的方法，其包括向其施用有效量的所述肽衍生物或其可治疗可接受的盐。
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