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公开(公告)号：EP2118123A1
公开(公告)日：2009-11-18
申请号：EP08728649.8
申请日：2008-01-31
IPC分类号： C07K7/54
CPC分类号： C07K14/4746 , A61K38/00 , C07K1/113
摘要： Cross-linked peptides related to human p53 and bind to HMD2 or a family member of HDM2 useful for promoting apoptosis, e.g., in the treatment of and identifying therapeutic agents that binding to HMD2 or a family member of HDM2.
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82.发明公开SEMI-SYNTHETIC DESMETHYL-VANCOMYCIN-BASED GLYCOPEPTIDES WITH ANTIBIOTIC ACTIVITY 审中-公开半人对糖去甲万古霉素碱抗生素影响
公开(公告)号：EP1868630A2
公开(公告)日：2007-12-26
申请号：EP06721134.2
申请日：2006-02-27
发明人： CHU, Daniel , NI, Zhi-Jie , WANG, John, Jian-xin , LEI, Yaohui , BAI, Yu
摘要： Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of the desmethyl- vancomycin scaffold, in particular, acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. In addition, compounds of the invention include desmethyl- vancomycin scaffolds on which the acid moiety on the macrocyclic ring is converted to certain substituted amides and the amino substituent on the amino-substituted sugar moiety is alkylated with certain alkyl groups. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.
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公开(公告)号：EP1794180A1
公开(公告)日：2007-06-13
申请号：EP05786327.6
申请日：2005-09-20
申请人： Lonza AG
IPC分类号： C07K1/06 , C07K7/54 , C07C29/10 , C07C51/09 , C07C209/62
CPC分类号： C07K1/042 , C07K7/54 , C07K14/685
摘要： A novel method for side chain cyclisation of peptides by means of lactamization is provided.
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公开(公告)号：EP1075480B1
公开(公告)日：2004-05-19
申请号：EP99911411.9
申请日：1999-03-15
IPC分类号： C07K7/54 , C07K9/00 , C07C47/55 , C07C309/24
CPC分类号： C07C309/24 , C07C45/85 , C07C47/55
摘要： The invention is directed to the process of purifying 4'-chloro-4-biphenylcarboxaldehyde.
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公开(公告)号：EP0471453A3
公开(公告)日：1993-03-10
申请号：EP91306582.7
申请日：1991-07-19
申请人： MERCK & CO. INC.
发明人： Sugg, Elizabeth E. , Dolan, Catherine A. , Bednarek, Maria A. , Tolman, Richard L. , Christensen, Burton G.
CPC分类号： C07K14/005 , A61K39/00 , C12N2740/16122
摘要： Human Immunodeficiency Virus (HIV) Principal Neutralizing Determinant (PND) peptides, or peptides immunologically equivalent therewith, having the structure :
wherein the ring system is formed by ring closure through a stable amide bond, are useful as analytical tools, as reagents in ELISA assays, or as reagents for making covalent conjugate immunogens. Conjugates containing these stable, cyclic peptides are useful for raising mammalian anti-peptide, anti-HIV, or HIV-neutralizing immune responses, and a composition containing such a conjugate may be used as a vaccine to prevent HIV-Disease, including Acquired Immune Deficiency Syndrome, (AIDS), or AIDS related complex, (ARC), or as an immunogen for treating humans afflicted with HIV-Diseases, such as AIDS or ARC.摘要翻译： 人体免疫缺陷病毒（HIV）主要中和决定簇（PND）肽或其免疫学等同的肽具有以下结构：其中环系由通过稳定的酰胺键闭环形成，可用作分析工具，作为试剂 在ELISA测定中，或作为制备共价结合免疫原的试剂。 含有这些稳定的环状肽的缀合物可用于提高哺乳动物抗肽，抗HIV或HIV中和免疫应答，并且含有此类缀合物的组合物可用作预防HIV-疾病（包括获得性免疫缺陷）的疫苗 综合征，（AIDS）或艾滋病相关复合物（ARC）或作为用于治疗患有HIV-疾病（例如艾滋病或ARC）的人的免疫原。
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公开(公告)号：EP0468714A3
公开(公告)日：1993-03-10
申请号：EP91306620.5
申请日：1991-07-19
申请人： MERCK & CO. INC.
IPC分类号： C07K7/06 , C07K7/08 , C07K7/10 , C07K7/52 , C07K7/54 , C07K17/10 , C07K15/04 , A61K47/48 , A61K39/21 , A61K37/02
CPC分类号： C07K14/005 , A61K39/00 , C12N2740/16122
摘要： Covalent conjugate immunogens, having Human Immunodeficiency Virus (HIV) Principal Neutralizing Determinant (PND) peptides covalently bound to the Outer Membrane Protein Complex (OMPC) of Neisseria through a linker which is an anionic polysaccharide (PSA), are useful for inducing anti-peptide immune responses in mammals, for inducing HIV-neutralizing antibodies in mammals, for formulating vaccines to prevent HIV infection or disease, including the Acquired Immune Deficiency Syndrome (AIDS) or for treating humans afflicted with HIV infection or HIV disease, including AIDS.
摘要翻译： 通过作为阴离子多糖（PSA）的接头共价结合奈瑟氏球菌的外膜蛋白复合物（OMPC）的人免疫缺陷病毒（HIV）的主要中和决定簇（PND）肽的共价结合免疫原可用于诱导抗肽 哺乳动物中的免疫反应，用于在哺乳动物中诱导HIV-中和抗体，用于配制预防HIV感染或疾病的疫苗，包括获得性免疫缺陷综合征（AIDS）或用于治疗患有HIV感染或HIV疾病（包括AIDS）的人。
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公开(公告)号：EP0471453A2
公开(公告)日：1992-02-19
申请号：EP91306582.7
申请日：1991-07-19
申请人： MERCK & CO. INC.
发明人： Sugg, Elizabeth E. , Dolan, Catherine A. , Bednarek, Maria A. , Tolman, Richard L. , Christensen, Burton G.
CPC分类号： C07K14/005 , A61K39/00 , C12N2740/16122
摘要： Human Immunodeficiency Virus (HIV) Principal Neutralizing Determinant (PND) peptides, or peptides
immunologically equivalent therewith, having the structure :
wherein the ring system is formed by ring closure through a stable amide bond, are useful as analytical tools, as reagents in ELISA assays, or as reagents for making covalent conjugate immunogens. Conjugates containing these stable, cyclic peptides are useful for raising mammalian anti-peptide, anti-HIV, or HIV-neutralizing immune responses, and a composition containing such a conjugate may be used as a vaccine to prevent HIV-Disease, including Acquired Immune Deficiency Syndrome, (AIDS), or AIDS related complex, (ARC), or as an immunogen for treating humans afflicted with HIV-Diseases, such as AIDS or ARC.摘要翻译： 具有以下结构的人免疫缺陷病毒（HIV）主要中和决定因子（HIV）主要中和决定因子（PND）肽或与其免疫等同的肽：其中环系通过稳定的酰胺键通过环闭合形成，可用作分析工具，作为ELISA测定中的试剂 或作为制备共价缀合物免疫原的试剂。 含有这些稳定的环肽的缀合物可用于产生哺乳动物抗肽，抗HIV或HIV中和免疫应答，含有这种缀合物的组合物可用作疫苗来预防HIV-疾病，包括获得性免疫缺陷 （艾滋病）或AIDS相关的复合物（ARC），或作为用于治疗患有艾滋病或ARC的HIV-疾病的人的免疫原。
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公开(公告)号：EP0352092A3
公开(公告)日：1990-10-31
申请号：EP89307315.5
申请日：1989-07-19
发明人： Takesako, Kazutoh , Shimanaka, Kazuo , Yamamoto, Junko , Haruna, Fumiyo , Nakamura, Teruya , Yamaguchi, Hideyo , Uchida, Katsuhisa , Ikai, Katsushige
摘要： Antibiotic compounds R106 of formula (I):
are antifungal agents. They may be produced by culture of microorganisms of the genus Aureobasidium , e.g. of new species Aureobasidium pullulans No.R106 exemplified by the type strain deposited under accession No.FERM BP-1938.-
90.发明公开Renin inhibitors containing a C-terminal amide cycle and compositions and combinations containing the same 失效Renininhibitoren mit einem C-terminalen Amidzyklus sowie Zusammensetzungen und Mehrkomponentenzusammensetzungen davon。
公开(公告)号：EP0129189A2
公开(公告)日：1984-12-27
申请号：EP84106712.7
申请日：1984-06-13
申请人： Merck & Co., Inc.
发明人： Boger, Joshua S. , Veber, Daniel F.
CPC分类号： C07K5/0227 , C07K5/1024 , Y10S530/86 , Y10S930/27
摘要： Disclosed are renin inhibitory peptides of the formula
wherein:
A is, e.g., hydrogen;
B is, e.g., absent; glycyl or sarcosyl;
D is, e.g., absent; or -S-;
E is, e.g., absent; or
where F 6 is, e.g., hydrogen; C1-4alkyl; or aryl; F is absent; or glycyl;
R 3 is, e.g., C3-6alkyl; C3-7cycloalkyl; aryl; or C3-7cycloalkyl or aryl substituted;
R 4 is hydrogen;
where R' is hydrogen; Ci-4alkyl; hydroxy; or C3-7cycloalkyl; and R 6 is as defined above;
R 5 is, e.g., hydrogen or
where R 6 and R 7 are as defined above;
m is 1 to 4;
n is 0 to 4; and
wherein all of the asymmetric carbon atoms have an S configuration, except for those in the A, B and D substituents, which may have an S or R configuration; and a pharmaceutically acceptable salt thereof. Those compounds and compositions and combinations containing the same inhibit renin and are useful for treating various forms of renin-associated hypertension and hyperaldosteronism.摘要翻译： 公开了下式的肾素抑制肽...
其中：A是例如氢; B例如不存在; 甘氨酰或肌氨酸; D是例如不存在; 或-S-; ... E例如不存在; 或... ...其中R 6为例如氢; C 1-4烷基; 或芳基; F不存在 或甘氨酰; R 3是例如C 3-6烷基; 3-7环烷基; 芳基; 或C 3-7环烷基或芳基取代; R 4是氢; 或... ...其中R 7是氢; C 1-4烷基; 羟基; 或C 3-7环烷基; 和R 6如上所定义; R 5例如是氢或...，其中R 6和R 7如上所定义; m是1至4; ... n 是0到4; 和其中所有不对称碳原子具有S构型，除了可以具有S或R构型的A，B和D取代基中的那些取代基; 及其药学上可接受的盐。 那些含有相同抑制肾素的化合物和组合物和组合物可用于治疗各种形式的肾素相关性高血压和醛固酮增多症。
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