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">1.发明公开Processes for the preparation of (R)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol" 审中-公开（A） - （2,3-二甲氧基苯基）-1- [2-（4-氟苯基）乙基] -4-哌啶甲醇
公开(公告)号：EP1734037A2
公开(公告)日：2006-12-20
申请号：EP06016486.0
申请日：1999-03-11
发明人： Bina, Alan G. , Daugs, Edward D. , Evans, Jonathan C. , Flemming, Hans-Wolfram , Guilamot, Gerard , Hawtorne, Robert A. , Hilpert, Thomas H.E. , Hitt, James E. , King, Chi-Hsin R. , Koek, Johannes N. , Laskovics, Frederick M. , Lefler, John M. , Margolin, Alexey L. , Minish, Sharon K. , Ortyl, Thomas T. , Rajewski, Lian G. , Sack, Marvin J. , Skultety, Paul F. , Stoltz-Dunn, Sandra K. , Tigner, Alonzo L. , Tomlinson, Ian A.
IPC分类号： C07D211/32
CPC分类号： C07D211/32 , C07D211/22
摘要： The present invention provides various processes for the preparation of (R)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol. These processes may be characterized by the following scheme:
摘要翻译： 本发明提供制备（R） - （2,3-二甲氧基苯基）-1- [2-（4-氟苯基）乙基] -4-哌啶甲醇的各种方法。 这些过程可以通过以下方案来表征：
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2.发明公开NOVEL PROTEIN AND PROCESS FOR PRODUCING THE SAME 无效NEUES PROTEIN UND VERFAHREN ZU DESSEN HERSTELLUNG
公开(公告)号：EP0955313A4
公开(公告)日：2001-11-07
申请号：EP96910198
申请日：1996-04-19
发明人： MAKISHIMA FUSAO , TAKAMATSU HIROYUKI , MIKI HIDEO , KAWAI SHINJI , KIMURA MICHIO , MATSUMOTO TOMOAKI , KATSUURA MIEKO , ENOMOTO KOICHI , SATOH YUSUKE
CPC分类号： C07K14/51 , A61K38/00 , Y10S514/801
摘要： A protein comprising an amino acid sequence represented by SEQ ID NO: 1 in the Sequence Listing and originating in human MP52 and the dimer of this protein. This dimer protein can be obtained by constructing a plasmid containing a DNA wherein a codon encoding methionine is added to the 5' end of a DNA sequence encoding the above-mentioned aminoacid sequence, transforming Escherichia coli by this plasmid, incubating the E. coli transformant, solubilizing and purifying the obtained inclusion body to thereby give a monomer protein, and then renaturing the obtained monomer protein into the dimer followed by purification. This dimer protein is useful in the treatment of cartilage and bone diseases.
摘要翻译： 一种蛋白质，其包含序列表中SEQ ID NO：1所示的氨基酸序列，并且源自人MP52和该蛋白质的二聚体。 该二聚体蛋白质可通过构建含有DNA的质粒来获得，其中在编码上述氨基酸序列的DNA序列的5'末端添加编码甲硫氨酸的密码子，用该质粒转化大肠杆菌，将大肠杆菌转化体 ，将得到的包涵体溶解并纯化，由此得到单体蛋白质，然后将获得的单体蛋白质复性成二聚体，然后纯化。 该二聚体蛋白质可用于治疗软骨和骨骼疾病。
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公开(公告)号：EP0866125A4
公开(公告)日：2001-10-10
申请号：EP96925064
申请日：1996-07-24
IPC分类号： C12N15/09 , A61K38/00 , A61P3/00 , A61P19/10 , A61P43/00 , C07K14/47 , C07K14/51 , C12N5/10 , C12N15/12 , C12P21/02 , C12R1/91 , A61K38/17
摘要： A protein named HMW human MP52 which is produced in CHO cells and has the amino acid sequence represented by SEQ ID NO:1 in the Sequence Listing; a process for producing HMW human MP52; and a medicinal composition comprising HMW human MP52 as the active ingredient. Because of having the effect of promoting bone induction, HMW human MP52 is usable in the treatment or prevention of bone diseases, etc.
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4.发明授权
公开(公告)号：EP0580459B1
公开(公告)日：2001-03-28
申请号：EP93401361.6
申请日：1993-05-28
IPC分类号： C07D233/86 , C07D235/02 , C07D233/88 , C07D233/84 , C07D233/74
CPC分类号： C07D233/84 , C07D233/76 , C07D233/86 , C07D233/88
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5.发明公开HUMAN BMP-2 PROMOTER AND METHOD FOR EXPLORING BONE-RELATED SUBSTANCE BY USING THE SAME 审中-公开人BMP-2子及其用途在过程中骨样物质
公开(公告)号：EP1082421A2
公开(公告)日：2001-03-14
申请号：EP99913529.6
申请日：1999-04-22
发明人： SUGIURA, Takeyuki
CPC分类号： C07K14/51
摘要： The present invention provides a method for exploring low molecular weight compounds which regulate positively or negatively the expression of the human BMP-2 with reference to a reporter activity by using 5' upstream region gene containing the human BMP-2 promoter and an animal cell introduced with a recombinant expression vector which has been connected to an appropriate reporter gene. The low molecular weight susbtances and their derivatives obtained by the present method have morphogenetic activity and inhibiting activity for bone and cartilage through the expression of human BMP-2 and are useful as preventive or therapeutic agents for bone and cartilage diseases.
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6.发明公开METHOD FOR SCREENING ANTIMYCOTIC SUBSTANCES USING ESSENTIAL GENES FROM S. CEREVISIAE 审中-公开用于筛选抗真菌物质来自酿酒酵母的使用必需基因
公开(公告)号：EP1073768A2
公开(公告)日：2001-02-07
申请号：EP99920745.9
申请日：1999-04-22
CPC分类号： C12Q1/6897 , C12Q1/18
摘要： The present invention concerns a method for the screening of antimycotic substances wherein an essential gene from mycetes or a functionally similar mycete gene, or the corresponding encoded protein, is used as target and wherein the essential gene is selected from the group consisting in YML114c, YLR186w, YLR215c, YLR222c, YLR243w, YLR272c, YLR275w, YLR276c, YLR317w, YLR359w, YLR373c, YLR424w, YLR437c, YLR440c, YML023c, YML049c, YML077w, YML093w, YML127w, YMR032w, YMR093w, YMR131c, YMR185w, YMR212c, YMR213w, YMR218c, YMR281w, YMR288w, YMR290c, YMR211w, YMR049c, YMR134w, YDR196c, YDR299w, YDR365c, YDR396w, YDR407c, YDR416w, YDR449c, YDR472w, YDR499w, YDR141c, YDR324c, YDR325w, YDR398w, YDR246w, YDR236c, YDR361c, YDR367w, YDR339c, YDR413c, YDR429c, YDR468c, YDR489w, YDR527w, YDR288w, YDR201w, YDR434w, YDR181c, YDR531w, YPL126w, YPL093w, YPL063w, YPL024w, YPL020c, YPL012w, YPL007c, YPL233w, YPL146c, YIL091c, YIL083c, YIL019w, YIL109c, YIL104c, YFL024c, YFR003c, YFR027w, YFR042w, YIR010w, YIR015w, YPR048w, YPR072w, YPR082c, YPR085c, YPR105c, YPR112c, YPR137w, YPR143w, YPR144c and YPR169w.
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7.发明公开Moenomycin A Derivatives, their preparation, and use as antibacterial products 有权霉菌素A衍生物，我的Herstellung和我的Verwendung als Antibakterielle-Arzneimittel
公开(公告)号：EP1069130A1
公开(公告)日：2001-01-17
申请号：EP99401772.1
申请日：1999-07-15
发明人： Lampilas, Maxime , Vogel, Stefan
CPC分类号： C07H13/12
摘要： New derivatives of moenomycin A, their process of preparation, and their use as antibacterial products.
wherein
R is a radical
Ra being an hydrogen atom or an alkyl radical up to 8 carbon atoms, R1 being an hydrogen atom, an optionally substituted alkyl radical linear or branched up to 30 carbon atoms, saturated or unsaturated or an optionally substituted aryl radical up to 14 carbon atoms, or R is a radical
R2 being an hydrogen atom or an alkyl radical linear or branched, saturated or unsaturated, up to 30 carbonatoms R3 being an hydrogen atom or an alkyl radical up to 12 carbon atoms.
The compounds of formula have antibacterial properties.摘要翻译： 新霉素A的新衍生物，其制备方法及其作为抗菌产品的用途。 其中R为基团，CH 2为氢原子或至多8个碳原子的烷基，R 1为氢原子，任选取代的直链或支链直至30个碳原子的烷基，饱和或不饱和的或 任选取代的至多14个碳原子的芳基，或R是基团CH 2 R 2是氢原子或直链或支链，饱和或不饱和的烷基，多至30个碳原子R3是氢原子或烷基自由基 至12个碳原子。 该化合物具有抗菌特性。
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8.发明公开BARBITURIC ACID DERIVATIVE AND PREVENTIVE AND THERAPEUTIC AGENT FOR BONE AND CARTILAGE CONTAINING THE SAME 审中-公开巴比土酸衍生物与该含，预防及治疗剂用于作用骨骼和软骨
公开(公告)号：EP1064269A1
公开(公告)日：2001-01-03
申请号：EP99919495.4
申请日：1999-03-23
发明人： SAKAI, Kunikazu , SATOH, Yusuke
IPC分类号： C07D239/62 , A61K31/515
CPC分类号： C07D409/06 , C07D239/62
摘要： The present invention relates to a barbituric acid derivative shown in formula (I) (wherein R or R1 independently represents a hydrogen atom, a susbstituted or not substituted alkyl group or alkenyl group of C¿1? - C15, a substituted or not substituted arylmethyl group, and substituted or not substituted aryl group, and R?2¿ represents substituted or not substituted alkyl group or alkenyl group of C¿1? - C15, a substituted or not substituted arylmethyl group, and substituted or not substituted aryl group). The barbituric acid derivative of the present invention has a strong inhibiting activity to bone resorption and is useful as a preventive and therapeutic agent for diseases affecting bone and cartilage.
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公开(公告)号：EP1062358A1
公开(公告)日：2000-12-27
申请号：EP99909036.8
申请日：1999-03-18
IPC分类号： C12P17/12 , C07F9/38 , C07D211/70
CPC分类号： C07D211/70 , C07F9/591 , C12P17/12
摘要： The invention concerns a method for preparing Fexofenadine from Terfenadine by a bioconversion process using Absidia corymbifera LCP 63-1800 or Steptomyces platensis NRRL 2364 strain.
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10.发明公开DERIVES D'HYDRAZONO-BENZAZULENE, COMPOSITIONS PHARMACEUTIQUES ET INTERMEDIAIRES 有权肼基benzazulene衍生物，药物组合物和中间产品
公开(公告)号：EP1017681A1
公开(公告)日：2000-07-12
申请号：EP98945363.4
申请日：1998-09-23
发明人： CARNIATO, Denis , GADEK, Thomas, R. , GOUBET, François , GOURVEST, Jean-François , KNOLLE, Jochen , MCDOWELL, Robert , SCHEUNEMANN, Karl-Heinz
IPC分类号： C07D233/52 , A61K31/415 , C07C49/747 , C07C333/04 , C07C323/22
CPC分类号： C07C333/04 , C07C49/747 , C07C323/22 , C07D233/52
摘要： The invention concerns products of formula (I) in which R1 represents S(O)X-[A]-[B]-COR6, x being equal to 0, 1 or 2; [A]- representing a bivalent radical derived from an aliphatic hydrocarbon, linear or branched, saturated or unsaturated, comprising 1 to 12 carbon atoms; [B] representing a phenyl radical, a CH(Z) radical or a single bond; G represents, either a radical of formula (G1) in which (Het') is a heterocycle of general formula (a), in which (H) forms, with the structural unit N=C-NH-, the residue of an aromatic or non-aromatic heterocycle, monocyclic or bicyclic, saturated or unsaturated, comprising 1 to 9 carbon atoms and 2 to 5 heteroatoms selected among oxygen, nitrogen or sulphur atoms, or a NRaRb radical (radical G2), or a (Het) radical (radical G3), or a -NRh-C(=X)-NHRc radical (radical G4), in which X is a sulphur, oxygen or NH atom, or a -NRh-SO2Rc radical (radical G5), and their additive salts with acids, bases and esters, the method for preparing them and the intermediates of said method, their application as medicines and the pharmaceutical compositions containing them.
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