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1. 发明授权

US06689777B2 Anti-malarial compounds, compositions and methods 失效
标题翻译：抗疟疾化合物，组合物和方法
公开(公告)号：US06689777B2
公开(公告)日：2004-02-10
申请号：US10278729
申请日：2002-10-23
申请人： Peter C. Ulrich , Anthony Cerami
发明人： Peter C. Ulrich , Anthony Cerami
IPC分类号： C07D27760
CPC分类号： A61K31/5377 , A61K31/155 , A61K31/352 , A61K31/428 , A61K31/436 , A61K31/44 , A61K31/47 , A61K31/496 , A61K31/505 , Y02A50/411
摘要： The present invention is directed to substituted naphthothiazolium, aromatic guanylhydrazones, and other compounds and compositions with anti-malarial activity useful for the treatment and prophylaxis of malaria. The compounds are provided for the treatment of malaria or the sequelae of malarial infection, for depolymerizing malaria pigment (hemozoin), and for ameliorating the adverse effects of hemozoin on host cells.
摘要翻译：本发明涉及取代的萘并噻唑鎓，芳香脒腙和其它具有抗疟疾活性的化合物和组合物，其可用于治疗和预防疟疾。提供这些化合物用于治疗疟疾或疟疾感染的后遗症，用于解聚疟疾色素（hemozoin），以及改善血红素对宿主细胞的不利影响。

2. 发明授权

US06335450B1 Efficient cyclic-bridged cyanine dyes 失效
标题翻译：高效的环状花青染料
公开(公告)号：US06335450B1
公开(公告)日：2002-01-01
申请号：US09710574
申请日：2000-11-09
申请人： Firdous Farooqui , Maged A. Michael , M. Parameswara Reddy
发明人： Firdous Farooqui , Maged A. Michael , M. Parameswara Reddy
IPC分类号： C07D27760
CPC分类号： G01N33/533 , C07D209/60 , C09B23/0016 , C09B23/0066 , C09B23/086
摘要： This invention provides cyclic-bridged dyes, particularly cyclic-bridged cyanine dyes, of the general formula: In this formula, each dotted line represents carbon atoms necessary to form a fused substituted or unsubstituted aromatic ring; n=1-18; m=1-18, selected independently from n. X and Y are selected independently from the group consisting of S, O, N, CH2 and C(CH3)2; at least one of said R1 and R2 comprises a sulfonic acid or sulfonate group attached to the aromatic ring; and R3 and R4 are independently selected from the group consisting of carboxyl, activated carboxyl and methyl, wherein at least one of said R3 and R4 groups is carboxylate or activated carboxylate. Methods of making and using the cyclic-bridged dyes are also provided.
摘要翻译：本发明提供了具有以下通式的环状桥联染料，特别是环状花青染料：在该式中，每个虚线表示形成稠合取代或未取代的芳环所需的碳原子; n = 1-18; m = 1-18，独立于n。 X和Y独立地选自S，O，N，CH 2和C（CH 3）2; 所述R 1和R 2中的至少一个包含连接到所述芳香环上的磺酸基或磺酸基; 并且R 3和R 4独立地选自羧基，活化的羧基和甲基，其中所述R 3和R 4基团中的至少一个是羧酸酯或活化的羧酸酯。还提供了制备和使用环状桥连染料的方法。

3. 发明授权

US06331632B1 Cyanine dye phosphoramidites 有权
标题翻译：花青染料亚磷酰胺
公开(公告)号：US06331632B1
公开(公告)日：2001-12-18
申请号：US09710575
申请日：2000-11-09
申请人： M. Parameswara Reedy , Firdous Farooqui , Maged A. Michael
发明人： M. Parameswara Reedy , Firdous Farooqui , Maged A. Michael
IPC分类号： C07D27760
CPC分类号： C07D209/14 , C07D209/60 , C07F9/5728 , C09B23/0066 , C09B23/08 , C12Q2563/149
摘要： This invention provides dye phosphoramidites, particularly phosphoramidites of cyanine and related dyes, of the general formula: In this formula, each dotted line represents carbon atoms necessary to form a fused substituted or unsubstituted aromatic ring; m is an integer from 1 to 18; Y and Z are independently selected from the group consisting of S, O, N, CH2 and C(CH3)2; R1 is an alkyl; (PAM) is a phosphoramidite group; X⊖ is a negative ion; and Q is or wherein n is 1, 2 or 3. Methods of making and using the dye phosphoramidites are also provided.
摘要翻译：本发明提供了以下通式的染料亚磷酰胺，特别是花青和相关染料的亚磷酰胺：在该式中，每个虚线表示形成稠合取代或未取代的芳环所需的碳原子; m为1〜18的整数， Y和Z独立地选自S，O，N，CH 2和C（CH 3）2; R1是烷基; （PAM）是亚磷酰胺基团; X⊖是负离子; 而Q是其中n为1,2或3.还提供了制备和使用染料亚磷酰胺的方法。

4. 发明授权

US06225330B1 Selective NPY (Y5) antagonists (tricyclics) 失效
公开(公告)号：US06225330B1
公开(公告)日：2001-05-01
申请号：US09343635
申请日：1999-06-30
申请人： Mohammad R. Marzabadi , Wai C. Wong , Walter Schilling , Stewart A. Noble
发明人： Mohammad R. Marzabadi , Wai C. Wong , Walter Schilling , Stewart A. Noble
IPC分类号： C07D27760
CPC分类号： C07D277/60 , C07D277/42 , C07D417/12 , C07D513/04
摘要： This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.

5. 发明授权

US06410577B1 Substituted 8,8a-dihydro-3ah-indeno[1,2-d]thiazoles, processes for their preparation and their use as medicaments 有权
公开(公告)号：US06410577B1
公开(公告)日：2002-06-25
申请号：US09790905
申请日：2001-02-23
申请人： Gerhard Jaehne , Hans-Jochen Lang , Matthias Gossel , Martin Bickel
发明人： Gerhard Jaehne , Hans-Jochen Lang , Matthias Gossel , Martin Bickel
IPC分类号： C07D27760
摘要： The invention relates to substituted 8,8a-dihydro-3aH-indeno[1,2-d]thiazoles and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of formula I, in which the radicals are as defined above, and their physiologically acceptable salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.

6. 发明授权

US06274738B1 Carboxamide derivatives having aryl and thiazole rings 失效
标题翻译：具有芳基和噻唑环的羧酰胺衍生物
公开(公告)号：US06274738B1
公开(公告)日：2001-08-14
申请号：US08977651
申请日：1997-11-24
申请人： Michael R. Kozlowski , Junko Aimi , Ryan Holcomb
发明人： Michael R. Kozlowski , Junko Aimi , Ryan Holcomb
IPC分类号： C07D27760
CPC分类号： C07D277/40 , C07D311/36 , C07D471/04 , C07D493/04 , C12Q1/68
摘要： The invention provides DNA primase assays suitable for identifying DN primase modulating agents, methods of modulating DNA primase activity, compounds for modulating DNA primase activity, and compositions which modulate DNA primase.
摘要翻译：本发明提供适用于鉴定DN启动子调节剂的DNA启动子测定，调节DNA引物酶活性的方法，调节DNA引物酶活性的化合物和调节DNA引物酶的组合物。

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