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1. 发明授权

US06376664B1 Cyclic bis-benzimidazole ligands and metal complexes thereof 有权
标题翻译：环状双苯并咪唑配体及其金属络合物
公开(公告)号：US06376664B1
公开(公告)日：2002-04-23
申请号：US09528273
申请日：2000-03-17
申请人： Michael K. Chan , Wai H. Kwok , Huichang Zhang , Maosheng Duan
发明人： Michael K. Chan , Wai H. Kwok , Huichang Zhang , Maosheng Duan
IPC分类号： C07D22500
CPC分类号： C07D487/18
摘要： Cyclic bis benzimidazole ligands of the following formula are formed by contacting a (2-aminophenyl)-benzimidazole-4-carboxaldehyde ethylene acetal or a (2-nitrophenyl)-benzimidazole-4-benzaldehyde with an acid optionally in the presence of a metal or a metal salt. wherein R1 and R2 may be the same or different and are selected from H, an alkyl having 1 to 10 carbon atoms, a benzyl group, a substituted 2-ethylphenyl group, a carbonyl group, a phenyl substituent, a tosyl group, and an alkylsulfonate group; R3 and R4 may be the same or different and are selected from H, methyl, and ethyl; and R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, and R18 may be the same or different and are selected from H, alkyl having 1 to 10 carbon atoms, fluoride, chloride, bromide, iodide, nitro, amino, a carboxylate, an ester, and a phenyl group.
摘要翻译：通过使（2-氨基苯基） - 苯并咪唑-4-甲醛乙醛缩醛或（2-硝基苯基） - 苯并咪唑-4-苯甲醛与酸任选地在金属存在下接触而形成下式的环状双苯并咪唑配体，或其中R1和R2可以相同或不同，选自H，具有1-10个碳原子的烷基，苄基，取代的2-乙基苯基，羰基，苯基取代基，甲苯磺酰基和烷基磺酸酯基; R 3和R 4可以相同或不同，并且选自H，甲基和乙基; 和R 5，R 6，R 7，R 8，R 9，R 10，R 11，R 12，R 13，R 14，R 15，R 16，R 17和R 18可以相同或不同，选自H，具有1-10个碳原子的烷基，氯化物，溴化物，碘化物，硝基，氨基，羧酸酯，酯和苯基。

2. 发明授权

US06200967B1 Anticoagulant agents 失效
标题翻译：抗凝剂
公开(公告)号：US06200967B1
公开(公告)日：2001-03-13
申请号：US09202626
申请日：1998-12-17
申请人： Valentine J Klimkowski , Aaron L Schacht , Michael R Wiley
发明人： Valentine J Klimkowski , Aaron L Schacht , Michael R Wiley
IPC分类号： C07D22500
CPC分类号： C07D401/06 , A61K38/00 , C07C311/06 , C07D205/04 , C07D207/16 , C07D209/42 , C07D217/26 , C07K5/0222 , C07K5/06078 , C07K5/06139 , C07K5/06191
摘要： This invention relates to a compound of the Formula I X—C(O)—Y—G—R I (wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof, processes and intermediates for the preparation of such a compound or salt, pharmaceutical compositions comprising such a compound or salt and methods of their use as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.
摘要翻译：本发明涉及式I化合物（其中X，Y，G和R具有说明书中定义的值）或其药学上可接受的盐，用于制备这种化合物或盐的方法和中间体，药物组合物包括这种化合物或盐以及它们用作凝血酶抑制剂，凝血抑制剂和治疗血栓栓塞障碍的药物的方法。

3. 发明授权

US06469162B1 Compounds with chelation affinity and selectivity for first transition series elements: use in medical therapy and diagnosis 失效
标题翻译：具有螯合亲和性和对第一过渡系列元素选择性的化合物：用于医学治疗和诊断
公开(公告)号：US06469162B1
公开(公告)日：2002-10-22
申请号：US09664952
申请日：2000-09-19
申请人： Harry S. Winchell , Joseph Y. Klein , Elliot D. Simhon , Rosa L. Cyjon , Ofer Klein , Haim Zaklad
发明人： Harry S. Winchell , Joseph Y. Klein , Elliot D. Simhon , Rosa L. Cyjon , Ofer Klein , Haim Zaklad
IPC分类号： C07D22500
CPC分类号： C07D405/14 , A61K31/13 , A61K31/131 , A61K31/135 , A61K31/136 , A61K31/137 , A61K31/395 , A61K31/4025 , A61K31/415 , A61K31/44 , A61K31/675 , A61K47/54 , A61K47/547 , A61K49/0002 , A61K49/04 , A61K49/06 , A61K51/0478 , A61K51/0482 , C07D255/02 , C07D255/04 , C07D257/00 , C07D403/14 , C07D487/08 , C07D487/10 , C07F9/6515 , C07F9/6524 , C07F9/6561 , Y10S514/836
摘要： This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or physiological salts of the free or conjugated compound, results in decrease in the in vivo bioavailability of first transition series elements and/or removal from the body of first transition series elements and elements with similar chemical properties. These characteristics make such compounds useful in the management of diseases associated with a bodily excess of first transition series elements and elements with similar chemical properties. This invention demonstrates that such compounds inhibit mammalian, bacterial, and fungal cell replication and are therefore useful in the treatment of neoplasia, infection, inflammation, immune reponse, and in termination of pregnancy. Since these compounds are capable of descreasing the in vivo availability of tissue iron they are useful in management of free radical mediated tissue damage, and oxidation mediated tissue damage. When combined with radioisotopic or paramagnetic cations of first transition series elements, or elements with chemical properties similar to those of first transition series elements, prior to their administration, the resulting complexes are useful as diagnostic agents in nuclear medicine and magnetic resonance imaging (MRI).
摘要翻译：本发明涉及合成和使用具有螯合亲和性和对第一转变序列元件的选择性的一类化合物。施用游离或缀合的化合物或游离或共轭化合物的生理盐导致第一过渡系列元件的体内生物利用度降低和/或从具有相似化学性质的第一过渡系列元件和元件的体内移除。这些特征使得这些化合物可用于治疗与具有相似化学性质的第一过渡系列元件和元件的身体过剩相关的疾病。本发明证明这些化合物抑制哺乳动物，细菌和真菌细胞复制，因此可用于治疗肿瘤形成，感染，炎症，免疫反应和终止妊娠。由于这些化合物能够降低组织铁的体内可利用性，因此它们可用于管理自由基介导的组织损伤和氧化介导的组织损伤。当与第一过渡系列元件的放射性同位素或顺磁性阳离子或具有与第一过渡系列元件类似的化学特性的元素组合时，在其给药之前，所得复合物可用作核医学和磁共振成像（MRI）中的诊断剂，。

4. 发明授权

US06441164B2 Wurster's crown ligands 失效
标题翻译： Wurster的冠配体
公开(公告)号：US06441164B2
公开(公告)日：2002-08-27
申请号：US09904332
申请日：2001-07-12
申请人： John W. Sibert
发明人： John W. Sibert
IPC分类号： C07D22500
CPC分类号： C07D273/00
摘要： Wurster's crown ligands comprise a macrocyclic ligand such as a crown ether in which a hetero atom is substituted with a 1,4-phenylenediamine group. The phenylenediamine group is covalently bound to the macrocyclic ligand by one or both of the amine nitrogens, the amine nitrogen thereby substituting for the hetero atom of the macrocyclic ligand. The resulting compounds are redox active. Methods of making and using the compounds are also disclosed.
摘要翻译： Wurster的冠配体包括大环配体，例如其中杂原子被1,4-苯二胺基团取代的冠醚。苯二胺基团通过一个或两个胺氮共价结合到大环配体，胺氮由此代替大环配体的杂原子。所得化合物是氧化还原活性的。还公开了制备和使用化合物的方法。

5. 发明授权

US06444808B1 Methods of making cross-bridged macropolycycles 有权
公开(公告)号：US06444808B1
公开(公告)日：2002-09-03
申请号：US09832579
申请日：2001-04-11
申请人： George Douglas Hiler, II , Christopher Mark Perkins
发明人： George Douglas Hiler, II , Christopher Mark Perkins
IPC分类号： C07D22500
摘要： Improved synthesis of a macropolycycle, more particularly, of a cross-bridged tetraazamacrocycle.

6. 发明授权

US06262258B1 Wurster's crown ligands 失效
标题翻译： Wurster的冠配体
公开(公告)号：US06262258B1
公开(公告)日：2001-07-17
申请号：US09390444
申请日：1999-09-07
申请人： John W. Sibert
发明人： John W. Sibert
IPC分类号： C07D22500
CPC分类号： C07D273/00
摘要： Wurster's crown ligands comprise a macrocyclic ligand such as a crown ether in which a hetero atom is substituted with a 1,4-phenylenediamine group. The phenylenediamine group is covalently bound to the macrocyclic ligand by one or both of the amine nitrogens, the amine nitrogen thereby substituting for the hetero atom of the macrocyclic ligand. The resulting compounds are redox active. Methods of making and using the compounds are also disclosed.
摘要翻译： Wurster的冠配体包括大环配体，例如其中杂原子被1,4-苯二胺基团取代的冠醚。苯二胺基团通过一个或两个胺氮共价结合到大环配体，胺氮由此代替大环配体的杂原子。所得化合物是氧化还原活性的。还公开了制备和使用化合物的方法。

7. 发明授权

US06482944B2 Processes for preparing tertiary aminoalkylorganometallic compounds 失效
标题翻译：制备叔氨基烷基有机金属化合物的方法
公开(公告)号：US06482944B2
公开(公告)日：2002-11-19
申请号：US09817994
申请日：2001-03-27
申请人： James Anthony Schwindeman , Randy W. Hall , Sonia S. Stryker
发明人： James Anthony Schwindeman , Randy W. Hall , Sonia S. Stryker
IPC分类号： C07D22500
CPC分类号： C07D295/067 , C07C209/08 , C07D243/08 , C07F1/02 , C07C211/15
摘要： Processes for the preparation of haloalkylamines and tertiary aminoalkylorganometallic compounds are disclosed. The haloalkylamines can be prepared by direct reaction of an amine with an &agr;, &ohgr;-dihaloalkane or an &agr;, &ohgr;-dihaloalkene. Tertiary aminoalkylorganometallic compounds can be prepared by reacting selected tertiary haloalkylamines with an alkali metal at a temperature greater than 45° C. in hydrocarbon solvents.
摘要翻译：公开了制备卤代烷基胺和叔氨基烷基有机金属化合物的方法。卤代烷基胺可以通过胺与α，ω-二卤代烷或α，ω-二卤代烯的直接反应来制备。叔氨基烷基有机金属化合物可以通过在烃溶剂中在大于45℃的温度下使选择的叔卤代烷基胺与碱金属反应来制备。

8. 发明授权

US06352981B1 Substituted AZA- and diazacycloheptane and -cyclooctane 有权
标题翻译：取代的AZA-和二氮杂环庚烷和 - 环辛烷
公开(公告)号：US06352981B1
公开(公告)日：2002-03-05
申请号：US09696941
申请日：2000-10-27
申请人： Hans-Jörg Treiber , Stefan Blank , Dorothea Starck , Liliane Unger , Hans-Jürgen Teschendorf , Karsten Wicke
发明人： Hans-Jörg Treiber , Stefan Blank , Dorothea Starck , Liliane Unger , Hans-Jürgen Teschendorf , Karsten Wicke
IPC分类号： C07D22500
CPC分类号： C07D403/04 , C07D403/12 , C07D403/14 , C07D417/14
摘要： Aza- and diazacyclohexane and -cyclooctane compounds of the following formula: Ar1—A—B—Ar2 (I) where Ar1, A, B and Ar2 have the meanings stated in the description have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.
摘要翻译：下式的氮杂 - 和二氮杂环己烷和 - 环辛烷化合物：其中Ar1，A，B和Ar2具有说明书中所述的含义，对多巴胺D3受体具有高亲和力，因此可用于治疗对多巴胺D3 配体。

9. 发明授权

US06191272B1 Process for the preparation of endo-nortropine using 8-benzyl-nortropan-3-one perchlorate as the intermediate, as well as the latter salt 有权
标题翻译：使用8-苄基 - 异丙肾上腺素-3-酮高氯酸盐作为中间体，以及后者的盐制备内切托品的方法
公开(公告)号：US06191272B1
公开(公告)日：2001-02-20
申请号：US09487051
申请日：2000-01-19
申请人： Rolf Sachse , Albert Schaupp
发明人： Rolf Sachse , Albert Schaupp
IPC分类号： C07D22500
CPC分类号： C07D451/06
摘要： The invention relates to a process for the preparation of endo-nortropine using 8-benzyl-nortropan-3-one perchlorate, as well as the latter product. Endo-nortropine is the key product for the production of important azonia-spironortropanol esters, which are used as pharmaceuticals, particularly spasmolytics. There are three different synthesis methods for the preparation of said intermediate, which lead to different disadvantages. These problems are obviated by the present invention through the two-stage treatment of 8-benzyl-nortropan-3-one perchlorate with catalytically activated hydrogen, the starting product initially being prehydrogenated in aqueous suspension and at atmospheric pressure and ambient pressure with a palladium catalyst, at the end of the reaction the catalyst is recovered by filtration, the filtrate is passed over an anion exchanger and the now alkaline reacting solution is rendered turbulent at 1000 to 1500 r.p.m. with hydrogen activated by Raney nickel at atmospheric pressure and ambient temperature. This new synthesis method using the novel perchlorate salt as an intermediate is extremely economic and environmentally friendly and supplies substantially completely stereoselectively the desired endo-form of nortropine.
摘要翻译：本发明涉及使用8-苄基 - 异丙肾上腺素-3-酮高氯酸盐以及后一种产品制备内给妥他汀的方法。内啡诺是生产重要的氮氧化物 - 螺螺甾醇酯的关键产物，其用作药物，特别是解痉药。制备所述中间体有三种不同的合成方法，这导致不同的缺点。通过用催化活化氢对8-苄基 - 异丙醇-3-酮高氯酸盐进行两级处理，本发明消除了这些问题，起始产物最初在含水悬浮液中预先氢化，并在大气压和环境压力下用钯催化剂在反应结束时，通过过滤回收催化剂，将滤液通过阴离子交换剂，并将现在的碱性反应溶液在1000至1500rpm下变成湍流在大气压和环境温度下由阮内镍活化的氢。使用新型高氯酸盐作为中间体的这种新的合成方法是非常经济和环境友好的，并且基本上完全立体选择性地提供了所需的内质酸内生型。

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