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1. 发明授权

US07084250B2 Process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides 有权
标题翻译：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
申请人： Gerhard Breipohl , Wolfgang Holla , Heiner Jendralla , Gerhard Beck
发明人： Gerhard Breipohl , Wolfgang Holla , Heiner Jendralla , Gerhard Beck
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。

2. 发明申请

US20080070258A1 POLYAMIDE NUCLEIC ACID DERIVATIVES AND AGENTS, AND PROCESSES FOR PREPARING THEM 失效
标题翻译：聚酰胺核酸衍生物和药剂及其制备方法
公开(公告)号：US20080070258A1
公开(公告)日：2008-03-20
申请号：US11855443
申请日：2007-09-14
申请人： Eugen UHLMANN , Gerhard Breipohl , David Will
发明人： Eugen UHLMANN , Gerhard Breipohl , David Will
IPC分类号： C12Q1/68 , C07H21/00
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。

3. 发明授权

US06905820B2 Polyamide nucleic acid derivatives, and agents and processes for preparing them 失效
标题翻译：聚酰胺核酸衍生物，以及制备它们的试剂和方法
公开(公告)号：US06905820B2
公开(公告)日：2005-06-14
申请号：US09835371
申请日：2001-04-17
申请人： Eugen Uhlmann , Gerhard Breipohl , David William Will
发明人： Eugen Uhlmann , Gerhard Breipohl , David William Will
IPC分类号： G01N33/53 , A61K38/00 , A61K48/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P31/16 , A61P31/18 , A61P35/00 , C07K14/00 , C08G69/48 , C12Q1/04 , C12Q1/68 , G01N21/78 , G01N33/566 , G01N33/58 , C07H21/02 , C12M1/34 , C12P19/34 , C07H21/64
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。

4. 发明授权

US06492356B1 Acylguanidine derivatives as inhibitors of bone resorption and as vitronectin receptor antagonists 失效
标题翻译：酰基胍衍生物作为骨吸收抑制剂和玻连蛋白受体拮抗剂
公开(公告)号：US06492356B1
公开(公告)日：2002-12-10
申请号：US09581915
申请日：2000-11-02
申请人： Anuschirwan Peyman , Jochen Knolle , Gerhard Breipohl , Karl-Heinz Scheunemann , Denis Carniato , Jean-Francois Gourvest , Thomas Gadek , Robert McDowell , Sarah Catherine Bodary , Robert Andrew Cuthbertson , Napoleane Ferrara
发明人： Anuschirwan Peyman , Jochen Knolle , Gerhard Breipohl , Karl-Heinz Scheunemann , Denis Carniato , Jean-Francois Gourvest , Thomas Gadek , Robert McDowell , Sarah Catherine Bodary , Robert Andrew Cuthbertson , Napoleane Ferrara
IPC分类号： A61K3155
CPC分类号： C07C279/20 , C07D239/16
摘要： The present invention relates to acylguanidine derivatives of formula (I) in which R1, R2, R4, R5, R6, A, m and n have the meanings indicated in the patent claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmaceutical active ingredients. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts and are suitable, for example, for the therapy or prophylaxis of diseases which are caused at least partially by an undesired extend of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式（I）的酰基胍衍生物，其中R 1，R 2，R 4，R 5，R 6，A，m和n具有专利权利要求中指出的含义，其生理上可耐受的盐及其前药。式（I）化合物是有价值的药物活性成分。它们是玻连蛋白受体拮抗剂和破骨细胞骨吸收的抑制剂，并且适合于例如治疗或预防由至少部分由不期望的骨吸收扩展（例如骨质疏松症）引起的疾病。本发明还涉及式（I）化合物的制备方法，其用途，特别是作为药物活性成分，以及包含它们的药物制剂。

5. 发明授权

US6046306A PNA synthesis using an amino protecting group which is labile to weak acids 失效
标题翻译：使用对弱酸不稳定的氨基保护基的PNA合成
公开(公告)号：US6046306A
公开(公告)日：2000-04-04
申请号：US927178
申请日：1997-09-11
申请人： Gerhard Breipohl , Eugen Uhlmann
发明人： Gerhard Breipohl , Eugen Uhlmann
IPC分类号： C07K1/04 , C07D473/18 , C07D473/34 , C07K1/06 , C07K1/10 , C07K14/00 , C08G69/10 , C07N21/00
CPC分类号： C07D473/18 , C07D473/34 , C07K14/003 , C08G69/10 , Y02P20/55
摘要： PNA synthesis using an amino protective group which is labile to weak acids.
摘要翻译：使用对弱酸不稳定的氨基保护基的PNA合成。

6. 发明授权

US5863901A Use of bradykinin antagonists for the production of pharmaceuticals for the treatment of chronic fibrogenetic liver disorders and acute liver disorders 失效
标题翻译：缓激肽拮抗剂用于制备用于治疗慢性纤维化肝病和急性肝脏疾病的药物的用途
公开(公告)号：US5863901A
公开(公告)日：1999-01-26
申请号：US810012
申请日：1997-03-04
申请人： Gerhard Breipohl , Stephan Henke , Jochen Knolle , Klaus Wirth , Max Hropot , Martin Bickel
发明人： Gerhard Breipohl , Stephan Henke , Jochen Knolle , Klaus Wirth , Max Hropot , Martin Bickel
IPC分类号： A61K38/00 , A61K38/04 , A61K38/08 , A61K45/00 , A61P1/16 , A61P43/00 , C07K7/18
CPC分类号： A61K38/043 , Y10S514/893
摘要： This invention relates to a method of treating a chronic fibrogenetic liver disorder and/or an acute liver disorder and/or complications associated therewith, comprising administering to a patient a therapeutically effective amount of a bradykinin antagonist. Particular complications associated with said liver disorders include portal hypertension, decompensation phenomena such as ascites, edema formation, hepatorenal syndrome, hypertensive gastropathy and colopathy, splenomegaly and hemorrhagic complications in the gastrointestinal tract due to portal hypertension, collateral circulation and hyperemia and a cardiopathy as a result of a chronically hyperdynamic circulatory situation and its consequences.
摘要翻译：本发明涉及一种治疗慢性纤维化肝病和/或急性肝病和/或与其相关的并发症的方法，包括向患者施用治疗有效量的缓激肽拮抗剂。与所述肝脏疾病相关的特异性并发症包括门静脉高压，诸如腹水，水肿形成，肝肾综合征，高血压性胃病和病变的代偿失调现象，由于门静脉高压，侧支循环和充血引起的胃肠道中的脾肿大和出血并发症以及心脏病长期超动力循环状况及其后果的结果。

7. 发明授权

US07550582B2 Polyamide nucleic acid derivatives and agents, and processes for preparing them 失效
标题翻译：聚酰胺核酸衍生物和试剂，及其制备方法
公开(公告)号：US07550582B2
公开(公告)日：2009-06-23
申请号：US11855443
申请日：2007-09-14
申请人： Eugen Uhlmann , Gerhard Breipohl , David William Will
发明人： Eugen Uhlmann , Gerhard Breipohl , David William Will
IPC分类号： C07H21/00 , C07H21/02 , C07H21/04 , C12Q1/68
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。

8. 发明授权

US07485421B2 Polyamide-oligonucleotide derivatives, their preparation and use 失效
标题翻译：聚酰胺 - 寡核苷酸衍生物，其制备和用途
公开(公告)号：US07485421B2
公开(公告)日：2009-02-03
申请号：US10939214
申请日：2004-09-10
申请人： Eugen Uhlmann , Gerhard Breipohl
发明人： Eugen Uhlmann , Gerhard Breipohl
IPC分类号： C12Q1/68 , C07H21/04
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： F [（DNA-Li）q（PNA-Li）r（DNA-Li）s（（N-1））其中q，r，s，t彼此独立地为0或1，其中总共为两个或更多个相邻的q，r，s和t> = 2; 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。

9. 发明授权

US07241882B2 Polyamide nucleic acid derivatives, and agents, and processes for preparing them 有权
标题翻译：聚酰胺核酸衍生物和试剂，及其制备方法
公开(公告)号：US07241882B2
公开(公告)日：2007-07-10
申请号：US10863999
申请日：2004-06-09
申请人： Eugen Uhlmann , Gerhard Breipohl , David William Will
发明人： Eugen Uhlmann , Gerhard Breipohl , David William Will
IPC分类号： C07H21/00 , C07H21/02 , C07H21/04 , C12Q1/68
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。

10. 发明授权

US06777544B2 Polyamide nucleic acid derivatives and agents and processes for preparing them 有权
标题翻译：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
申请人： Eugen Uhlmann , Gerhard Breipohl , David William Will
发明人： Eugen Uhlmann , Gerhard Breipohl , David William Will
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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