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11. 发明授权

US06548543B1 Remedies or preventives containing cyclopentenone compounds as the active ingredient 失效
标题翻译：含环戊烯酮化合物作为活性成分的补救措施或预防措施
公开(公告)号：US06548543B1
公开(公告)日：2003-04-15
申请号：US09763244
申请日：2001-02-20
申请人： Eiji Kobayashi , Hiromu Ohnogi , Hiroaki Sagawa , Takanari Tominaga , Eiji Nishiyama , Nobuto Koyama , Katsushige Ikai , Ikunoshin Kato
发明人： Eiji Kobayashi , Hiromu Ohnogi , Hiroaki Sagawa , Takanari Tominaga , Eiji Nishiyama , Nobuto Koyama , Katsushige Ikai , Ikunoshin Kato
IPC分类号： A61K31215
CPC分类号： A61K31/215 , A61K31/22 , C07C69/013 , C07C2601/10 , Y02A50/411
摘要： Remedies or preventives for diseases with a need for immunoregulation, diseases with a need for inhibition of inflammation, diseases with a need for regulation of tumor necrosis factor production, diseases with a need for regulation of fungal growth, diseases with a need for regulation of cell adhesion or disease with a deed for induction of heat-shock protein, which contain as the active ingredient at least one compound selected from among cyclopentenone derivatives represented by general formula [I], optically active isomers and salts thereof, wherein R1 and R2 are the same or different and each represents hydrogen, an aliphatic group, an aromatic group or an aromatic aliphatic group.
摘要翻译：需要免疫调节的疾病的治疗或预防措施，需要抑制炎症的疾病，需要调节肿瘤坏死因子产生的疾病，需要调节真菌生长的疾病，需要调节细胞的疾病含有作为活性成分的至少一种选自通式[I]表示的环戊烯酮衍生物的化合物，其光学活性异构体和盐，其中R 1和R 2为相同或不同，各自表示氢，脂族基，芳基或芳族脂族基。

12. 发明授权

US06342524B1 Use of non-steroidal anti-inflammatory agents in combination with compounds that have FP prostaglandin agonist activity to treat glaucoma and ocular hypertension 失效
标题翻译：使用非甾体抗炎药与具有FP前列腺素激动剂活性的化合物联合用于治疗青光眼和高眼压症
公开(公告)号：US06342524B1
公开(公告)日：2002-01-29
申请号：US09575833
申请日：2000-05-22
申请人： Mark R. Hellberg , Jon C. Nixon
发明人： Mark R. Hellberg , Jon C. Nixon
IPC分类号： A61K31215
CPC分类号： A61K31/215 , Y10S514/913
摘要： Disclosed are methods and compositions for the treatment of glaucoma and ocular hypertension, comprising the administration of a prostaglandin analog and a prostaglandin synthesis inhibitor.
摘要翻译：公开了用于治疗青光眼和高眼压症的方法和组合物，包括施用前列腺素类似物和前列腺素合成抑制剂。

13. 发明授权

US06306881B1 Anti-inflammatory agents 失效
标题翻译：抗炎剂
公开(公告)号：US06306881B1
公开(公告)日：2001-10-23
申请号：US09341929
申请日：1999-07-21
申请人： Andrew Paul Ayscough , Mark Whittaker
发明人： Andrew Paul Ayscough , Mark Whittaker
IPC分类号： A61K31215
CPC分类号： A61K31/215 , A61K31/216 , A61K31/223 , A61K31/341 , A61K31/381 , A61K31/4406 , A61K31/445
摘要： Compounds of general formula (I) wherein R4 is an ester or thioester group and R, R1, R2, and R3 are as specified in the description, inhibit intracellular Leukotriene A4 hydrolase activity and are therefore of value for the treatment of inflammatory disease.
摘要翻译：通式（I）的化合物，其中R 4是酯或硫酯基，R 1，R 2，R 2和R 3如说明书中所述，抑制细胞内白细胞三烯A4水解酶活性，因此具有治疗炎性疾病的价值。

14. 发明授权

US06303569B1 Trialkyl-lock-facilitated polymeric prodrugs of amino-containing bioactive agents 失效
标题翻译：含氨基的生物活性剂的三烷基锁定促进的聚合物前药
公开(公告)号：US06303569B1
公开(公告)日：2001-10-16
申请号：US09137430
申请日：1998-08-21
申请人： Richard B. Greenwald , Yun H. Choe , Annapurna Pendri
发明人： Richard B. Greenwald , Yun H. Choe , Annapurna Pendri
IPC分类号： A61K31215
CPC分类号： C07C237/22 , A61K47/60 , C07B2200/11 , C07C271/16 , C07C271/22
摘要： The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric compounds comprise the formula: wherein: B is H, OH, OSiR13, a residue of an amine-containing target moiety or a residue of a hydroxyl-containing moiety; L1 and L2 are bifunctional linking moieties; Y2is O or S; R2 is selected from the group consisting of C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy, and C1-6 heteroalkoxy; R9, R10, R13 are independently one of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3 S substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy, and C1-6 heteroalkoxy; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or one; and R11 is a polymer residue. The first prodrug is generated when the polymeric portion of the double prodrug is cleaved and the parent molecule is generated rapidly thereafter in vivo, as a result of a trialkyl lock type lactonization-type reaction.
摘要翻译：本发明涉及含有基于聚合物的输送形式的双重前药。这些聚合化合物包括下式：其中：B是H，OH，OSiR13，含胺目标部分的残基或含羟基部分的残基; L1和L2是双官能连接部分; Y 2是O或S; R 2 选自C1-6烷基，C3-12支链烷基，C3-8环烷基，C1-6取代烷基，C3-8取代环烷基，芳基，取代芳基，芳烷基，C1-6杂烷基，取代C1- 6个杂烷基，C 1-6烷氧基，苯氧基和C 1-6杂烷氧基; R 9，R 10，R 13独立地为氢，C 1-6烷基，C 3-12支链烷基，C 3-8环烷基，C 1-6取代的烷基，C 3 S取代的环烷基，芳基，取代的芳基，芳烷基，C 1-6杂烷基，取代的C 1-6杂烷基，C 1-6烷氧基，苯氧基和C 1-6杂烷氧基; Ar是当式（I）中包括时，取代的芳族烃或多取代的杂环基;（m）为0或1; 并且R11是聚合物残基。当双前体药物的聚合部分被切割并且其后在体内快速产生母体分子时，由于三烷基锁定型内酯化反应的结果产生第一种前体药物。

15. 发明授权

US06284791B1 Guanidinomethyl cyclohexane carboxylic acid ester derivatives 失效
标题翻译：胍基甲基环己烷羧酸酯衍生物
公开(公告)号：US06284791B1
公开(公告)日：2001-09-04
申请号：US08793728
申请日：1997-02-28
申请人： Osamu Kamoda , Hiromichi Fujiwara , Toshiharu Yanagi
发明人： Osamu Kamoda , Hiromichi Fujiwara , Toshiharu Yanagi
IPC分类号： A61K31215
CPC分类号： C07C279/14 , A61K31/215 , A61K31/24 , C07C69/94 , C07C2601/14
摘要： A compound represented by general formula (I-2) or a pharmaceutically acceptable acid-addition salt thereof, useful as an anti-microbial against Helicobacter pylori and as a medicinal composition for treating Helicobacter pylori infection, wherein Ar represents phenyl, biphenyl or naphthyl each having a at least one substituent selected from the group consisting of halogen, cyano, nitro, carboxy, C1-C18 alkyl, C1-C18 alkoxy, C3-C18 cycloalkyl, C7-C18 aralkyl, C8-C18 arylalkenyl, C7-C18 aralkyloxy, optionally substituted phenoxy, optionally substituted C2-C19 alkoxycarbonyl, and optionally substituted C8-C19 aralkyloxycarbonyl, provided the case where Ar represents phenyl substituted by halogen, cyano, nitro, carboxy, C1-C18 alkyl, optionally substituted C2-C19 alkoxycarbonyl or C8-C19 aralkyloxycarbonyl is expected.
摘要翻译：由通式（I-2）表示的化合物或其药学上可接受的酸加成盐可用作幽门螺杆菌的抗微生物剂和用作治疗幽门螺杆菌感染的药用组合物，其中Ar表示苯基，联苯基或萘基具有至少一个选自卤素，氰基，硝基，羧基，C 1 -C 18烷基，C 1 -C 18烷氧基，C 3 -C 18环烷基，C 7 -C 18芳烷基，C 8 -C 18芳基烯基，C 7 -C 18芳烷氧基，氰基，硝基，羧基，C 1 -C 18烷基，任意取代的C 2 -C 19烷氧基羰基或C 8 -C 19烷氧基羰基取代的苯基，任意取代的苯氧基，任意取代的C 2 -C 19烷氧羰基和任选取代的C 8 -C 19芳烷氧基羰基， C19芳烷氧基羰基是预期的。

16. 发明授权

US06251939B1 Carbamate-based cationic lipids 失效
标题翻译：基于氨基甲酸酯的阳离子脂质
公开(公告)号：US06251939B1
公开(公告)日：2001-06-26
申请号：US08665057
申请日：1996-06-05
申请人： David Aaron Schwartz , Bob Dale Brown , Brian Patrick Dwyer
发明人： David Aaron Schwartz , Bob Dale Brown , Brian Patrick Dwyer
IPC分类号： A61K31215
CPC分类号： A61K9/1272 , C07C271/20 , C07J41/0055 , C07J43/003 , C07J51/00 , C07K5/0205
摘要： The present invention provides novel carbamate-based cationic lipids of the general structure: or a salt, or solvate, or enantiomers thereof, wherein (a) R1 is a lipophilic moiety; (b) R2 is a positively charged moiety; (c) n is an integer from 1 to 8; (d) X is an anion or polyanion; and (e) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid. The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions, and a kit for preparing the same.
摘要翻译：本发明提供了一般结构的新的氨基甲酸酯基阳离子脂质：或其盐或溶剂化物或其对映异构体，其中（a）R 1是亲脂性部分; （b）R2是带正电的部分; （c）n为1〜8的整数，（d）X是阴离子或聚阴离子; 和（e）m是0至等于脂质上存在的正电荷的数的整数。本发明还提供了这些脂质与聚阴离子大分子的组合物，利用这些组合物干扰细胞中的蛋白质表达的方法，以及用于制备该组合物的试剂盒。

17. 发明授权

US06235780B1 &ohgr;-cycloalkyl-prostaglandin E1 derivatives 失效
标题翻译： ω-环烷基 - 前列腺素E1衍生物
公开(公告)号：US06235780B1
公开(公告)日：2001-05-22
申请号：US09356674
申请日：1999-07-19
申请人： Shuichi Ohuchida , Kousuke Tani
发明人： Shuichi Ohuchida , Kousuke Tani
IPC分类号： A61K31215
CPC分类号： A61K31/557
摘要： (wherein R1 is OH etc.; X is Cl, F; R2 is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl which may be substituted; n is 0-4.), non-toxic salts thereof or cyclodextrin clathrates thereof can strongly bind on EP2 subtype receptor. Therefore, they are useful for the prevention and/or treatment of immunological diseases (autoimmune diseases, post-transplantation graft rejection etc.), asthma, abnormal bone formation, neuronal cell death, hepatopathy, abortion, premature birth or retina neuropathy (e.g. glaucoma) etc.
摘要翻译：（其中R1为OH等; X为Cl，F; R2为H，C1-8烷基，C2-8烯基，可被取代的C2-8炔基; n为0-4），无毒性盐或其环糊精包合物可以强烈结合EP2亚型受体。因此，它们可用于预防和/或治疗免疫疾病（自身免疫疾病，移植后移植排斥反应等），哮喘，异常骨形成，神经元细胞死亡，肝病，流产，早产或视网膜神经病变（例如青光眼）等

18. 发明授权

US06831101B2 Tricyclic rantes receptor ligands 失效
标题翻译：三环兰受体配体
公开(公告)号：US06831101B2
公开(公告)日：2004-12-14
申请号：US09992550
申请日：2001-11-13
申请人： Geeta Saxena , Christopher R. Tudan , Ahmed Merzouk , Hassan Salari
发明人： Geeta Saxena , Christopher R. Tudan , Ahmed Merzouk , Hassan Salari
IPC分类号： A61K31215
CPC分类号： A61K31/19
摘要： In various aspects, the invention provides compounds that bind to one or more RANTES receptors for the treatment of chemokine mediated disease states, such as compounds of formula (I):
摘要翻译：在各个方面，本发明提供了结合一种或多种RANTES受体以治疗趋化因子介导的疾病状态的化合物，例如式（I）的化合物：

19. 发明授权

US06806261B2 Methods for treating certain diseases using naaladase inhibitors 失效
标题翻译：使用奈拉替酶抑制剂治疗某些疾病的方法
公开(公告)号：US06806261B2
公开(公告)日：2004-10-19
申请号：US10209011
申请日：2002-08-01
申请人： Barbara S. Slusher , Xi-Chun May Lu , Krystyna Wozniak
发明人： Barbara S. Slusher , Xi-Chun May Lu , Krystyna Wozniak
IPC分类号： A61K31215
CPC分类号： A61K31/66 , A61K31/00
摘要： The present invention relates to methods for regulating the release of TGF-&bgr; from living cells in vitro or in vivo, comprising bringing the cells into contact with an effective amount of a NAALADase inhibitor. Such methods are believed to be useful for affecting neuroregeneration, cell proliferation, cell differentiation, extracellular matrix formation, myelination, inflammation, immune function, liver function, pancreatic function, angiogenesis, or wound healing; and/or for preventing or treating diabetes.
摘要翻译：本发明涉及用于在体外或体内调节TGF-β从活细胞释放的方法，包括使细胞与有效量的NAALADase抑制剂接触。据信这些方法可用于影响神经再生，细胞增殖，细胞分化，细胞外基质形成，髓鞘形成，炎症，免疫功能，肝功能，胰腺功能，血管生成或伤口愈合。和/或用于预防或治疗糖尿病。

20. 发明授权

US06794409B2 Use of ER&bgr;-selective ligands for regulating fertility and compounds useful therefor 失效
标题翻译：使用ERbeta选择性配体调节生育力和有用的化合物
公开(公告)号：US06794409B2
公开(公告)日：2004-09-21
申请号：US10083685
申请日：2002-02-27
申请人： Christa Hegele-Hartung , Karl-Heinrich Fritzemeier , Hiroshi Yamanouchi , Olaf Peters , Dirk Kosemund , Gerd Mueller , Ingo Tornus , Gerd Schubert , Sven Ring
发明人： Christa Hegele-Hartung , Karl-Heinrich Fritzemeier , Hiroshi Yamanouchi , Olaf Peters , Dirk Kosemund , Gerd Mueller , Ingo Tornus , Gerd Schubert , Sven Ring
IPC分类号： A61K31215
CPC分类号： A61K45/06 , A61K31/00 , A61K31/05 , A61K31/122
摘要： The present invention discloses the use of ER&bgr;-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ER&bgr;-agonists are used for treatment of infertility and ER&bgr;-antagonists for contraception.
摘要翻译：本发明公开了ERbeta选择性配体用于生产用于调节生育力的药物的用途，而不需要额外使用孕激素.Ebeta激动剂用于治疗不育症和用于避孕的ERbeta拮抗剂。

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