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1. 发明申请

US20040265885A1 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：US20040265885A1
公开(公告)日：2004-12-30
申请号：US10863999
申请日：2004-06-09
申请人： Aventis Pharma Deutschland GmbH
发明人： Eugen Uhlmann , Gerhard Breipohl , David William Will
IPC分类号： C12Q001/68 , C07K014/00 , A61K048/00
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.

2. 发明申请

US20040248900A1 Triaza- and tetraaza-anthracenedione derivatives, their preparation and their use as pharmaceuticals 有权
标题翻译：三氮杂和四氮杂蒽醌二酮衍生物，其制备及其作为药物的用途
公开(公告)号：US20040248900A1
公开(公告)日：2004-12-09
申请号：US10829064
申请日：2004-04-21
申请人： Aventis Pharma Deutschland GmbH
发明人： Andreas Weichert , Hartmut Strobel , Paulus Wohlfart , Marcel Patek , Martin Smrcina , Aleksandra Weichsel
IPC分类号： A61K031/519 , C07D487/14
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to triaza- and tetraaza-anthracenedione derivatives of the formula I, 1 wherein A, B and R1 to R5 are as defined herein. The compounds of formula I are valuable pharmacologically active compounds. They are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (NO) synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式I的三氮杂和四氮杂蒽并二酮衍生物，其中A，B和R 1至R 5如本文所定义。式I的化合物是有价值的药理活性化合物。它们可用于治疗各种疾病状态，包括心血管疾病如动脉粥样硬化，血栓形成，冠状动脉疾病，高血压和心功能不全。它们上调酶内皮一氧化氮（NO）合酶的表达，并且可以在需要所述酶的增加的表达或增加的NO水平或降低的NO水平的归一化的条件下应用。本发明还涉及式I化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

3. 发明申请

US20040248809A1 Use of antagonists of the bradykinin B2 receptor for the treatment of osteoarthrosis 审中-公开
标题翻译：使用缓激肽B2受体拮抗剂治疗骨关节病
公开(公告)号：US20040248809A1
公开(公告)日：2004-12-09
申请号：US10773772
申请日：2004-02-06
申请人： Aventis Pharma Deutschland GmbH
发明人： Martin Michaelis , Karl Rudolphi
IPC分类号： A61K038/08
CPC分类号： A61K38/08
摘要： Peptides having bradykinin-antagonistic action are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases in whose course an increased activity of matrix metalloproteinases is involved. These include diseases such as degenerative joint diseases, for example osteoarthrosis, spondylosis and chondroporosis after joint trauma or relatively long immobilization of a joint after meniscus or patella injuries or torn ligaments. The invention therefore relates to the use of a compound of the formula I, A-B-X-E-F-K-(D)-TIC-G-M-Fnull-Inullnull(I) for the production of pharmaceuticals for the treatment of degenerative joint diseases, wherein A, B, X, E, F, K, (D)-TIC, G, M, Fnull and I are as defined herein.
摘要翻译：具有缓激肽拮抗作用的肽适用于生产用于预防和治疗涉及基质金属蛋白酶活性升高的疾病的药物。这些疾病包括诸如退行性关节疾病之类的疾病，例如在关节创伤之后的关节骨关节病，脊椎软骨病和软骨病，或者在弯液面或髌骨损伤或撕裂的韧带之后关节相对较长的固定。因此，本发明涉及式I化合物ABXEFK-（D）-TIC-GM-F'-I（I）用于制备用于治疗退行性关节病的药物，其中A，B， X，E，F，K，（D）-TIC，G，M，F'和I如本文所定义。

4. 发明申请

US20040242560A1 Process for synthesizing heterocyclic compounds 审中-公开
标题翻译：杂环化合物合成方法
公开(公告)号：US20040242560A1
公开(公告)日：2004-12-02
申请号：US10840105
申请日：2004-05-06
申请人： Aventis Pharma Deutschland GmbH
发明人： Uwe Heinelt , Hans-Jochen Lang
IPC分类号： A61K031/553 , A61K031/554 , A61K031/551
CPC分类号： C07D413/12 , C07D233/50 , C07D235/30 , C07D263/28 , C07D263/58 , C07D265/08 , C07D265/12 , C07D265/18 , C07D277/18 , C07D409/12 , C07D495/04
摘要： The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. 1 In the process, an isothiocyanate of formula II is initially reacted with a primary amine of formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.
摘要翻译：本发明提供了用于合成式I的杂环化合物的方案1中所示的方法。在该方法中，式II的异硫氰酸酯最初与式III的伯胺反应，得到式IV的硫脲。随后，使用碱和磺酰氯将式IV的硫脲转化成相应的式I的杂环。

5. 发明申请

US20040235824A1 Indazole-derivatives as factor Xa inhibitors 有权
标题翻译：吲唑衍生物作为因子Xa抑制剂
公开(公告)号：US20040235824A1
公开(公告)日：2004-11-25
申请号：US10849088
申请日：2004-05-19
申请人： Aventis Pharma Deutschland GmbH
发明人： Marc Nazare , Volkmar Wehner , Volker Laux , Matthias Urmann , Armin Bauer , Hans Matter
IPC分类号： A61K031/55 , A61K031/541 , A61K031/5377 , A61K031/501
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14
摘要： The present invention relates to a compound of the formula I 1 wherein J1, J2, R0, R1, R2, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式I化合物，其中J 1，J 2，R 0，R 1，R 2，Q，V，G和M如本文所定义。式I的化合物是有价值的药理活性化合物。它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望活性或用于治愈或预防因子Xa和/或因子VIIa的抑制。本发明还涉及制备式I化合物的方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物制剂。

6. 发明申请

US20040220191A1 Substituted N-aryl heterocycles, process for their preparation and their use as medicaments 有权
标题翻译：取代的N-芳基杂环，其制备方法及其用作药物
公开(公告)号：US20040220191A1
公开(公告)日：2004-11-04
申请号：US10779853
申请日：2004-02-17
申请人： Aventis Pharma Deutschland GmbH
发明人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Thomas Boehme , Gerhard Hessler , Petra Stahl , Dirk Gretzke
IPC分类号： A61K031/501 , A61K031/506 , A61K031/497 , A61K031/4747 , A61K031/4439
CPC分类号： C07D207/26 , C07D205/04 , C07D207/14 , C07D207/16 , C07D207/34 , C07D211/58 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to substituted N-aryl heterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I 1 in which the radicals have the stated meanings, the N-oxides and the physiologically tolerated salts thereof and process for the preparation thereof are described. The compounds are suitable for example as anorectic agents.
摘要翻译：本发明涉及取代的N-芳基杂环及其生理上耐受的盐和生理功能衍生物。描述了其中基团具有所述含义的式I化合物，其N-氧化物及其生理学上可接受的盐及其制备方法。该化合物适合于例如厌食剂。

7. 发明申请

US20040210061A1 Novel processes for the preparation of (R)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl) ethyl]-4-piperidinemethanol 审中-公开
标题翻译：制备（R）-α-（2,3-二甲氧基苯基）-1- [2-（4-氟苯基）乙基] -4-哌啶甲醇的新方法
公开(公告)号：US20040210061A1
公开(公告)日：2004-10-21
申请号：US10838843
申请日：2004-05-04
申请人： Aventis Pharmaceuticals Inc. , Aventis Pharma Deutschland GmbH
发明人： Thomas Heinz Eduard Hilpert , Hans-Wolfram Flemming , Sandra K. Stolz-Dunn , Jonathan C. Evans , Ian A. Tomlinson
IPC分类号： C07D213/28
CPC分类号： C07D211/32 , C07D211/22
摘要： The present invention provides various processes for the preparation of (R)-null-(2,3-dimethoxyphenyl)-1-null2-(4-fluorophenyl)ethylnull-4-piperidinemethanol. These processes may be characterized by the following scheme: 1
摘要翻译：本发明提供制备（R）-α-（2,3-二甲氧基苯基）-1- [2-（4-氟苯基）乙基] -4-哌啶甲醇的各种方法。这些过程可以通过以下方案来表征：

8. 发明申请

US20040209932A1 1,3-substitued cycloalkyl derivatives having acidic, mostly heterocyclic groups; processes for their preparation and their use as pharmaceuticals 审中-公开
标题翻译：具有酸性，主要是杂环基团的1,3-取代的环烷基衍生物; 其制备方法及其作为药物的用途
公开(公告)号：US20040209932A1
公开(公告)日：2004-10-21
申请号：US10789281
申请日：2004-02-27
申请人： Aventis Pharma Deutschland GmbH
发明人： Jochen Goerlitzer , Heiner Glombik , Eugen Falk , Dirk Gretzke , Stefanie Keil , Hans-Ludwig Schaefer , Christian Stapper , Wolfgang Wendler
IPC分类号： C07D263/02 , A61K031/421
CPC分类号： C07D263/32 , C07D413/12 , C07D471/04 , C07F5/025
摘要： The invention relates to 1,3-substituted cycloalkyl derivatives having acidic, mostly heterocyclic groups and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, 1 in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistence is involved.
摘要翻译：本发明涉及具有酸性，主要是杂环基团的1,3-取代的环烷基衍生物及其生理上可接受的盐和生理功能衍生物。描述的是式I化合物，其中基团如所定义，以及它们的生理上可接受的盐及其制备方法。所述化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及涉及胰岛素抵抗的疾病。

9. 发明申请

US20040209931A1 Process for preparing the enantiomeric forms of cis-configured 1,3-cyclohexanediol derivatives 失效
标题翻译：制备顺式构型的1,3-环己二醇衍生物的对映体形式的方法
公开(公告)号：US20040209931A1
公开(公告)日：2004-10-21
申请号：US10789053
申请日：2004-02-27
申请人： Aventis Pharma Deutschland GmbH
发明人： Wolfgang Holla , Stefanie Keil
IPC分类号： C07D263/02 , A61K031/422
CPC分类号： C07D263/32 , C07B2200/07 , C07C41/16 , C07C41/18 , C07C41/26 , C07C41/36 , C07C67/08 , C07C67/31 , C07C67/56 , C07C2601/14 , C12P41/004 , C07C69/76 , C07C69/42 , C07C43/196 , C07C43/1788
摘要： Process for preparing the enantiomeric forms of cis-configured 1,3-cyclohexanediol derivatives A process is described for preparing chiral, nonracemic, cis-configured 1,3-disubstituted cyclohexanols of the formula (I) 1 where the radicals are as defined, by means of enzymatic optical resolution.
摘要翻译：用于制备顺式构型的1,3-环己二醇衍生物的对映体形式的方法描述了制备式（I）的手性，非水性，顺式构型的1,3-二取代的环己醇的方法，其中基团通过方法的酶学光学分辨率。

10. 发明申请

US20040192738A1 2-(Butyl-1-sulfonylamino)-N-[1(R)-(6-methoxypyridin-3-yl)propyl] benzamide, its use as a medicament, and pharmaceutical preparations comprising it 审中-公开
标题翻译： 2-（丁基-1-磺酰基氨基）-N- [1（R） - （6-甲氧基吡啶-3-基）丙基]苯甲酰胺，其作为药物的用途，以及包含它的药物制剂
公开(公告)号：US20040192738A1
公开(公告)日：2004-09-30
申请号：US10796466
申请日：2004-03-09
申请人： Aventis Pharma Deutschland GmbH
发明人： Joachim Brendel , Heinz Goegelein , Klaus Wirth , Gert Ulrich Kuerzel
IPC分类号： C07D213/70 , A61K031/44
CPC分类号： C07C311/08 , C07D213/64
摘要： The invention relates to 2-(butyl-1-sulfonylamino)-N-null1(R)-(6-methoxy-pyridin-3-yl)propylnullbenzamide of the formula I 1 and to its pharmaceutically acceptable salts, their preparation and use, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation or atrial flutters.
摘要翻译：本发明涉及式I的2-（丁基-1-磺酰基氨基）-N- [1（R） - （6-甲氧基 - 吡啶-3-基）丙基]苯甲酰胺及其药学上可接受的盐，其制备和特别用于治疗和预防房性心律失常，例如房颤或心房扑动。

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