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1. 发明授权

US06747060B2 Non-natural galanin receptor ligands 失效
标题翻译：非天然甘丙肽受体配体
公开(公告)号：US06747060B2
公开(公告)日：2004-06-08
申请号：US10155376
申请日：2002-05-24
申请人： Kulliki Saar , Tamas Bartfai , Ulo Langel , Gerd Hallnemo , Sven Hellberg
发明人： Kulliki Saar , Tamas Bartfai , Ulo Langel , Gerd Hallnemo , Sven Hellberg
IPC分类号： A61K3135
CPC分类号： C07K5/06078 , A61K38/00
摘要： Compounds which are non-natural galanin receptor ligands are disclosed. The ligands are of small size, have agonist or antagonist galanin activity and may cross the blood-brain barrier to displace galanin from galanin receptors. The ligands are useful as medicaments for treatment of convulsions (e.g. in epilepsy), diseases and disorders related to endocrinology (e.g., growth hormone, insulin or prolactin release), tumors expressing galanin receptors, feeding disorders pain, allodynia, psychiatric disorders such as depression (involving e.g., noradrenaline or serotonin), cognitive disorders (e.g. Alzeimer's disease), and the like.
摘要翻译：公开了非天然甘氨酸受体配体的化合物。配体具有小尺寸，具有激动剂或拮抗剂甘丙肽活性，并且可以穿过血脑屏障以从甘丙肽受体取代甘丙肽。配体可用作治疗惊厥（例如癫痫），与内分泌学（例如生长激素，胰岛素或催乳素释放）相关的疾病和病症的药物，表达甘丙肽受体的肿瘤，进食障碍性疼痛，异常性疼痛，抑郁症等精神疾病（例如，去甲肾上腺素或5-羟色胺），认知障碍（例如Alzeimer病）等。

2. 发明授权

US06710074B2 Compound having antimalarial activity 失效
标题翻译：具有抗疟活性的化合物
公开(公告)号：US06710074B2
公开(公告)日：2004-03-23
申请号：US10220244
申请日：2002-08-30
申请人： Masataka Ihara , Kiyosei Takasu , Yusuke Wataya , Hye-Sook Kim
发明人： Masataka Ihara , Kiyosei Takasu , Yusuke Wataya , Hye-Sook Kim
IPC分类号： A61K3135
CPC分类号： C07D493/10
摘要： An object of the present invention is to provide a novel compound having antimalarial acitivity and an antimalarial agent containing the novel compound as an active component. An antimalarial agent containing 12-hidroxy-2-(1-methoxy-carbonylethyl)-5-oxo-10,11,13-trioxatricyclo[7.2.0.01,6]tridecane represented by a following formula (II) as an active agent is prepared.
摘要翻译：本发明的目的是提供具有抗疟活性的新化合物和含有新化合物作为活性成分的抗疟剂。含有由下式（II）表示的12-羟基-2-（1-甲氧基 - 乙基乙基）-5-氧代-10,11,13-三氧杂三环[7.2.0.0 1,6]十一烷的抗疟剂作为制备活性剂。

3. 发明授权

US06696484B2 Method and compositions for regulation of 5-alpha reductase activity 有权
标题翻译：用于调节5-α还原酶活性的方法和组合物
公开(公告)号：US06696484B2
公开(公告)日：2004-02-24
申请号：US10132050
申请日：2002-04-24
申请人： Shutsung Liao , Richard Hiipakka
发明人： Shutsung Liao , Richard Hiipakka
IPC分类号： A61K3135
CPC分类号： A61K31/00 , A61K31/075 , A61K31/12 , A61K31/35 , A61K31/44 , C07C49/248 , C07C49/255 , C07D311/62
摘要： Pharmaceutical compositions and methods for treating androgen related disorders. The pharmaceutical compositions may include a 5&agr;-reductase inhibitor, such as natural and synthetic flavanoids, catechols, curcumin-related substances, quinones, catechins, particularly epigallocatechin derivatives, fatty acids, and the salts, esters, analogues, pro-drugs, isomers, racemic mixtures, or derivatives of any of the foregoing. The use of testosterone (or DHT) combinations with the aforementioned 5&agr;-reductase inhibitor compounds is also contemplated.
摘要翻译：用于治疗雄激素相关疾病的药物组合物和方法。药物组合物可包括5α-还原酶抑制剂，例如天然和合成的类黄酮，儿茶酚，姜黄素相关物质，醌类，儿茶素类，尤其是表没食子儿茶素衍生物，脂肪酸，以及其盐，酯类，前药，异构体，外消旋混合物或任何前述物质的衍生物。还考虑使用与上述5α-还原酶抑制剂化合物的睾酮（或DHT）组合。

4. 发明授权

US06620842B2 Chalcones 失效
标题翻译：笛卡尔
公开(公告)号：US06620842B2
公开(公告)日：2003-09-16
申请号：US10075626
申请日：2002-02-15
申请人： Ezio Bombardelli , Piero Valenti
发明人： Ezio Bombardelli , Piero Valenti
IPC分类号： A61K3135
CPC分类号： C07D409/06 , A61K31/35 , C07D311/30 , C07D311/86 , A61K31/335 , A61K2300/00
摘要： Disclosed are novel chalcone derivatives having the formula (I) The compounds possess antiproliferative activity and are useful for the manufacture of a medicament for the treatment or prevention of neoplasms, particularly those located in the uterus, ovary or breast. The compounds of the invention may also be useful in the manufacture of a medicament for the treatment or prevention of menopausal disorders and osteoporosis.
摘要翻译：公开了具有式（I）的新型查耳酮衍生物。该化合物具有抗增殖活性，并且可用于制备用于治疗或预防赘生物，特别是位于子宫，卵巢或乳腺中的肿瘤的药物。本发明的化合物还可用于制备用于治疗或预防绝经障碍和骨质疏松症的药物。

5. 发明授权

US06545040B1 Method of lowering the blood pressure 失效
标题翻译：降低血压的方法
公开(公告)号：US06545040B1
公开(公告)日：2003-04-08
申请号：US07825488
申请日：1992-01-24
申请人： Raymond Mathieu Xhonneux , Guy Rosalia Eugène Van Lommen
发明人： Raymond Mathieu Xhonneux , Guy Rosalia Eugène Van Lommen
IPC分类号： A61K3135
CPC分类号： A61K31/35 , C07D311/58
摘要： A method of potentiating the effects of blood pressure reducing agents in warm-blooded animals, said method comprising administering to said warm-blooded animals of an effective amount of a blood pressure reducing agent and a 2,2′-iminobisethanol derivative.
摘要翻译：一种增强血液中降血压剂在温血动物中的作用的方法，所述方法包括向所述温血动物施用有效量的降血压剂和2,2'-亚氨基双酚衍生物。

6. 发明授权

US06512007B1 Use of galiella lactone 失效
标题翻译：使用galiella内酯
公开(公告)号：US06512007B1
公开(公告)日：2003-01-28
申请号：US09895685
申请日：2001-06-29
申请人： Jörg Baumgarten , Marcus Weidler , Gerhard Erkel , Heidrun Anke , Timm Anke
发明人： Jörg Baumgarten , Marcus Weidler , Gerhard Erkel , Heidrun Anke , Timm Anke
IPC分类号： A61K3135
CPC分类号： C07D307/93 , A61K31/365
摘要： The invention relates to the use of the substance known under the name of galiella lactone as pharmaceutical, in particular for the treatment of inflammatory processes.
摘要翻译：本发明涉及使用以加里内酯为名称的物质作为药物，特别是用于治疗炎症过程。

7. 发明授权

US06495593B1 Compositions for preventing or treating adverse physiological effects associated with cardiac disease 失效
标题翻译：用于预防或治疗与心脏病相关的不良生理作用的组合物
公开(公告)号：US06495593B1
公开(公告)日：2002-12-17
申请号：US09596859
申请日：2000-06-19
申请人： Debasis Bagchi , Dipak K. Das
发明人： Debasis Bagchi , Dipak K. Das
IPC分类号： A61K3135
CPC分类号： A61K36/87 , A61K31/35
摘要： A method is disclosed for preventing or treating the adverse physiological effects associated with cardiac disease by administering a purified proanthocyanidin composition to the person in an amount effective to prevent or reduce the adverse physiological effects.
摘要翻译：公开了一种通过以有效预防或减少不良生理作用的量向人施用纯化的原花色素组合物来预防或治疗与心脏病相关的不良生理作用的方法。

8. 发明授权

US06476066B1 Anti-first-pass effect compounds 有权
标题翻译：抗首过效应化合物
公开(公告)号：US06476066B1
公开(公告)日：2002-11-05
申请号：US09793416
申请日：2001-02-27
申请人： James W. Harris
发明人： James W. Harris
IPC分类号： A61K3135
CPC分类号： A61K31/37 , A23L2/06 , A23L2/39 , A23L33/105 , A61K31/352 , A61K31/366 , A61K36/752 , C07D493/10
摘要： Safe, effective first-pass inhibiting compounds and citrus-derived substances are provided. Formulations containing the compounds are also provided as are methods for their preparation and for inhibiting the first pass effect.
摘要翻译：提供安全，有效的一次通过抑制化合物和柑橘衍生物质。还提供了含有这些化合物的制剂，其制备方法和抑制第一道次效应。

9. 发明授权

US06472422B2 Analogs of cocaine 失效
标题翻译：可卡因类似物
公开(公告)号：US06472422B2
公开(公告)日：2002-10-29
申请号：US09769774
申请日：2001-01-25
申请人： Alan P. Kozikowski , Gian Luca Araldi
发明人： Alan P. Kozikowski , Gian Luca Araldi
IPC分类号： A61K3135
CPC分类号： C07D211/60 , C07B59/002 , C07B2200/07 , C07D211/12 , C07D211/14 , C07D211/20 , C07D211/22
摘要： The invention provides a compound of formula (I): wherein R1, R2, R3, and Y have any of the meanings defined in the specification; as well a pharmaceutical composition comprising a compound of formula I; intermediates and methods useful for preparing a compound of formula I; and therapeutic methods for treating drug addiction, Parkinson's disease or depression comprising administering a compound of formula I, to a mammal in need of such treatment.
摘要翻译：本发明提供式（I）化合物：其中R1，R2，R3和Y具有本说明书中定义的任何含义; 以及包含式I化合物的药物组合物; 用于制备式I化合物的中间体和方法; 以及用于治疗药物成瘾，帕金森病或抑郁症的治疗方法，包括向需要这种治疗的哺乳动物施用式I化合物。

10. 发明授权

US06451846B1 Isocoumarin derivatives inhibiting angiogenesis 失效
标题翻译：抑制血管生成的异香豆素衍生物
公开(公告)号：US06451846B1
公开(公告)日：2002-09-17
申请号：US09980904
申请日：2002-02-26
申请人： Jung Joon Lee , Hang-Sub Kim , Jeong-Hyung Lee , Young-Soo Hong , Yun Joo Park
发明人： Jung Joon Lee , Hang-Sub Kim , Jeong-Hyung Lee , Young-Soo Hong , Yun Joo Park
IPC分类号： A61K3135
CPC分类号： C07D311/76
摘要： The present invention relates to novel isocoumarin derivatves inhibiting angiogenesis, a method for preparation thereof and pharmaceutical compositions comprising the said derivatives as pharmaceutically active ingredients. More particularly, the present invention relates to novel isocoumarin derivatves represented by formula (1), especially 6,8-dihydroxy-4-acetyl-isocoumarin, a method for preparing 6,8-dihydroxy-4-acetyl-isocoumarin from fungi, and pharmaceutical compositions comprising the compounds and/or 6,8-dihydroxy-4-acetyl-isocoumarin as pharmaceutically active ingredients, which would be effective for the treatment of angiogenic diseases such as cancers, rheumatoid arthritis and diabetic retinopathy.
摘要翻译：本发明涉及抑制血管生成的新型异香豆素衍生物，其制备方法和包含所述衍生物作为药物活性成分的药物组合物。更具体地说，本发明涉及由式（1）表示的新型异香豆素衍生物，特别是6,8-二羟基-4-乙酰基异香豆素，一种从真菌中制备6,8-二羟基-4-乙酰基异香豆素的方法，以及包含化合物和/或6,8-二羟基-4-乙酰基异香豆素作为药物活性成分的药物组合物，其对于治疗血管生成疾病如癌症，类风湿性关节炎和糖尿病性视网膜病变是有效的。

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