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1.发明公开Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin d analogs, and other compounds 失效的24羟基化的中间体立体有择制备用于Aminosterin-和维生素D类似物和其它化合物的制备
公开(公告)号：EP1389623A2
公开(公告)日：2004-02-18
申请号：EP03011093.6
申请日：1997-12-08
发明人： Kinney, William A. , Jones, Steven , Zhang, Xuehai , Rao, Meena N. , Bulliard, Michel , Meckler, Harold , Lee, Nancy
CPC分类号： C07J41/0005 , C07J9/00 , C07J31/006
摘要： A method is described for stereoselectively reducing an unsaturated alkyl ketone substituant attached to a fused ring base such as a steroid ring base or a Vitamin D3 analog ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent to stereoselectively reduce the unsaturated alkyl ketone to an unsaturated alkyl alcohol.
摘要翻译： 描述了一种方法用于立体选择性地还原到附连到的稠环基的不饱和烷基酮substituant：例如类固醇环基或维生素D3类似物环基。 在该方法中，所述不饱和烷基酮与手性恶唑硼烷试剂反应立体选择性地还原不饱和的烷基酮在不饱和的烷基醇。
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2.发明公开ASTHMA ASSOCIATED FACTORS AS TARGETS FOR TREATING ATOPIC ALLERGIES INCLUDING ASTHMA AND RELATED DISORDERS 审中-公开支气管哮喘相关因素，如特应性目标过敏的治疗包括哮喘和相关疾病
公开(公告)号：EP1067940A1
公开(公告)日：2001-01-17
申请号：EP99911092.7
申请日：1999-03-03
发明人： HOLROYD, Kenneth, J. , LEVITT, Roy, C. , MALOY, W., Lee , LOUAHED, Jamila , McLANE, Mike , NICOLAIDES, Nicholas, C. , ZHOU, Yuhong , DONG, Qu
IPC分类号： A61K31/70 , A61K39/395 , C07H21/04 , G01N33/53
CPC分类号： C07K14/705 , A61K38/00 , G01N33/6872 , G01N2500/00 , Y10S977/914 , Y10S977/927
摘要： A new gene in the calcium-activated chloride channel family has been discovered that is induced by IL-9, thereby providing a therapeutic target in IL-9 mediated development of atopic allergy, asthma-related disorders and cystic fibrosis. A method for the identification and use of small molecule inhibitors of this gene and its products to treat these disorders has also been discovered. The invention also includes a method for diagnosing susceptibility to, and assessing treatment of atopic allergy, asthma-related disorders by measuring the level of gene expression in biologic samples using antibody specific for this protein.
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3.发明授权STEROID DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE AS ANTIBIOTICS OR DISINFECTANTS 失效甾类衍生物，药物组合物含幽及其作为抗生素或消毒剂
公开(公告)号：EP0688333B1
公开(公告)日：1998-08-19
申请号：EP94911470.6
申请日：1994-03-10
CPC分类号： C07J31/006 , C07J9/00 , C07J9/005 , C07J17/00 , C07J41/0005 , C07J41/0055 , C07J41/0088 , C07J43/003 , C07J51/00
摘要： Compounds having a broad range of antimicrobial activity generally have a structure including a steroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of formula (III) preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z5 is alpha -H; one Z7 is beta -H and the other is alpha -H or alpha -OH; both substituents Z12 are hydrogen; X' is a polyamine side chain of the formula -NH-(CH2)p-NH-(CH2)q-N(R )(R ) where p and q are each independently 3 or 4, and R and R are each independently hydrogen or methyl; R' is methyl; and Y' is (C1-C10)-alkyl substituted with a group such as -CO2H or -SO3H.
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公开(公告)号：EP0579763A1
公开(公告)日：1994-01-26
申请号：EP92911044.0
申请日：1992-03-27
发明人： MALOY, W., Lee
CPC分类号： C07K14/001 , A61K38/00 , C07K14/46
摘要： Nouveaux peptides amphiphiles biologiquement actifs et/ou leurs analogues ou dérivés, utilisés comme agents pharmaceutiques. De tels peptides ont une activité antibiotique et/ou anti-virale et/ou anti-tumorale et/ou anti-parasite et/ou spermicide.
摘要翻译： 用作药物的新型生物活性两亲性肽和/或其类似物或衍生物。 这样的肽具有抗生素和/或抗病毒和/或抗肿瘤和/或抗寄生虫和/或杀精子活性。
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5.发明公开COMPOSITION AND TREATMENT WITH BIOLOGICALLY ACTIVE PEPTIDES AND ANTIBIOTICS WHICH INHIBIT DNA GYRASE 失效用生物活性肽和抗生素抑制DNAGYRASE的组成和处理
公开(公告)号：EP0559647A1
公开(公告)日：1993-09-15
申请号：EP91912701.0
申请日：1991-06-20
发明人： BERKOWITZ, Barry
CPC分类号： A61K38/04 , A61K38/17 , A61K2300/00
摘要： Composition comprenant au moins un peptide ou une protéine amphiphile biologiquement actif, ledit peptide ou ladite protéine étant un peptide ou une protéine formant des canaux d'ions et un antibiotique inhibant la gyrase d'ADN . On peut administrer le peptide amphiphile biologiquement actif et l'antibiotique inhibant la gyrase d'ADN dans des doses efficaces pour inhiber la croissance d'une cellule cible telle qu'une bactérie.
摘要翻译： 包含至少一种生物活性肽或两亲性蛋白质的组合物，其中所述肽或蛋白质是形成离子通道的肽或蛋白质和抗生素抑制DNA促旋酶。 生物活性两亲肽和DNA促旋酶抑制抗生素可以以有效抑制靶细胞如细菌生长的剂量施用。
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6.发明授权SQUALAMINE IN COMBINATION WITH OTHER ANTI-CANCER AGENTS FOR TREATING TUMORS 失效角鲨与其他抗癌治疗肿瘤MITTELEN TO组合
公开(公告)号：EP0910382B1
公开(公告)日：2003-06-11
申请号：EP97921396.4
申请日：1997-04-25
发明人： ZASLOFF, Michael , WILLIAMS, Jon
CPC分类号： A61K31/575 , A61K33/24 , A61K2300/00 , A61K31/00
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公开(公告)号：EP0749437B1
公开(公告)日：2001-12-05
申请号：EP94931274.8
申请日：1994-09-13
发明人： FRYE, Leah, L. , ZASLOFF, Michael, A. , KINNEY, William, A. , MORIARTY, Robert , COLLINS, Delwood, C.
CPC分类号： C07J51/00 , C07J9/00 , C07J9/005 , C07J17/00 , C07J31/006 , C07J41/0005 , C07J41/0055 , C07J43/003
摘要： Compounds having a broad range of antimicrobial activity generally have a structure including a steroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of formula (III), preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z5 is alpha -H; one Z7 is beta -H and the other is alpha -H or alpha -OH; both substituents Z12 are hydrogen; X' is a polyamine side chain of the formula -NH-(CH2)p-NH-(CH2)q-N(R )(R ) where p and q are each independently 3 or 4, and R and R are each independently hydrogen or methyl; R' is methyl; and Y' is (C1-C10)-alkyl substituted with a group such as -CO2H or -SO3H. Such compounds, as well as squalamine itself, have antiangiogenic activity and Na /K -ATPase-inhibiting activity.
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8.发明公开A METHOD FOR STIMULATION OF DEFENSIN PRODUCTION BY EXPOSURE TO ISOLEUCIN 审中-公开方法踱步DEFENSINPRODUKTION通过与异亮氨酸联系
公开(公告)号：EP1093364A1
公开(公告)日：2001-04-25
申请号：EP99923261.4
申请日：1999-05-21
IPC分类号： A61K31/195 , A61K31/19 , A61K31/22
CPC分类号： A61K31/19 , A61K31/198 , A61K31/22 , Y02A50/473
摘要： The subject invention relates to a method for the stimulation of defensin production in eukaryotic cells such as, for example, mammalian cells. Furthermore, the invention includes said method for the prevention and treatment of infections and other various disease states and in the stimulation of the immune system.
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公开(公告)号：EP0923377A1
公开(公告)日：1999-06-23
申请号：EP97926574.0
申请日：1997-05-16
CPC分类号： C07J41/0005 , A61K31/575
摘要： A pharmaceutical composition includes, as an active ingredient, a compound according to formula 1436, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. Various pharmaceutical products may be produced including this pharmaceutical composition. Such pharmaceutical products may be used for the treatment of cancers, such as leukemia; inflammation; arthritis; and viruses, such as HSV. Methods for using the pharmaceutical compositions also are described. In these methods, various diseases are treated or other body functions are activated or inhibited by administering an effective amount of the pharmaceutical composition. For example, inflammation, arthritis, herpes simplex virus, melanoma, and leukemia may be treated by administering an effective amount of the pharmaceutical compositions. Viral replication, weight gain, and growth factor production can be inhibited by administering an effective amount of these pharmaceutical compositions. Appetite can be suppressed by administering an effective amount of the pharmaceutical compositions, and a diuretic effect can be produced.
摘要翻译： 药物组合物包含作为活性成分的根据式1436的化合物或其药学上可接受的盐和药学上可接受的载体或赋形剂。 可以生产包括这种药物组合物的各种药物产品。 此类药物产品可用于治疗癌症，如白血病; 炎; 关节炎; 和病毒，如HSV。 还描述了使用药物组合物的方法。 在这些方法中，通过施用有效量的药物组合物治疗各种疾病或激活或抑制其他身体功能。 例如，炎症，关节炎，单纯疱疹病毒，黑素瘤和白血病可以通过施用有效量的药物组合物来治疗。 通过施用有效量的这些药物组合物可以抑制病毒复制，体重增加和生长因子产生。 通过施用有效量的药物组合物可以抑制食欲，并且可以产生利尿效果。
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10.发明公开
公开(公告)号：EP0833841A1
公开(公告)日：1998-04-08
申请号：EP96922560.0
申请日：1996-06-19
CPC分类号： C07K14/461 , A61K38/00
摘要： A new family of linear antimicrobial peptide from hagfish intestine is described. This invention relates to proteins with antimicrobial properties isolated from hagfish intestine and their corresponding chemical sequences. The antibiotics obtained include, but are not limited to, peptides having a sequence selected from the group consisting of (a); (b); and (c).
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