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1. 发明授权

US5149701A C-31 methylated FR-900520 cyclic hemiketal immunosuppressant agents 失效
标题翻译： C-31甲基化FR-900520环状半乳免疫抑制剂
公开(公告)号：US5149701A
公开(公告)日：1992-09-22
申请号：US738995
申请日：1991-08-01
申请人： Ali Shafiee , Louis Kaplan , Shieh-Shung T. Chen , Byron H. Arison , Lawrence F. Colwell, Jr. , Francis Dumont
发明人： Ali Shafiee , Louis Kaplan , Shieh-Shung T. Chen , Byron H. Arison , Lawrence F. Colwell, Jr. , Francis Dumont
IPC分类号： C07D498/22
CPC分类号： C07D498/22
摘要： Described is a process for producing a new immunosuppressant, a C-31 desmethyl, C-19/C-22 cyclic hemiketal biotransformation analog (Compound I) of FR-900520, under novel fermentation conditions utilizing the novel microorganism, Streptomyces, lavendulae ATCC No. 55209. Also disclosed is the C-31 methylated devivative (Compound II) of Compound I produced by enzymatic methylation using 31-O-desmethylimmunomycin O-methyl transferase, (DIMT), a methyl transferase enzyme. The macrolide immunosuppressants are useful in preventing human host rejection of foreign organ transplants, e.g. bone marrow, liver, lung, kidney and heart transplants.
摘要翻译：描述了FR-900520的新型免疫抑制剂，C-31脱甲基，C-19 / C-22环状半缩甲基生物转化类似物（化合物I）在新型发酵条件下利用新型微生物Streptomyces，lavendulae ATCC No 55209.还公开了通过使用31-O-去甲基免疫霉素O-甲基转移酶（DIMT），甲基转移酶进行酶促甲基化产生的化合物I的C-31甲基化偏差（化合物II）。大环内酯类免疫抑制剂可用于预防异种器官移植的人宿主排斥反应。骨髓，肝，肺，肾和心脏移植。

2. 发明授权

US5302604A Cholesterol lowering compounds produced by directed biosynthesis 失效
标题翻译：通过定向生物合成产生的胆固醇降低化合物
公开(公告)号：US5302604A
公开(公告)日：1994-04-12
申请号：US957316
申请日：1992-10-06
申请人： Kevin M. Byrne , Shieh-Shung T. Chen , Louis Kaplan , John G. MacConnell , Brian R. Petuch , Raymond F. White , Byron H. Arison
发明人： Kevin M. Byrne , Shieh-Shung T. Chen , Louis Kaplan , John G. MacConnell , Brian R. Petuch , Raymond F. White , Byron H. Arison
IPC分类号： A61K45/06 , C07D493/08 , A61K31/38 , A61K31/44
CPC分类号： C07D493/08 , A61K45/06
摘要： Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthetase inhibitors and thus useful as cholesterol lowering agents, antifungal agents and cancer treatment agents.
摘要翻译：结构式（I）化合物通过定向生物合成制备。这些化合物是角鲨烯合成酶抑制剂，因此可用作胆固醇降低剂，抗真菌剂和癌症治疗剂。

3. 发明授权

US5264355A Methlating enzyme from streptomyces MA6858 失效
标题翻译：来自链霉菌MA6858的浓缩酶
公开(公告)号：US5264355A
公开(公告)日：1993-11-23
申请号：US908244
申请日：1992-07-02
申请人： Ali Shafiee , Patricia M. Cameron , David A. Boulton , Louis Kaplan , Haideh Motamedi
发明人： Ali Shafiee , Patricia M. Cameron , David A. Boulton , Louis Kaplan , Haideh Motamedi
IPC分类号： C12N9/10 , C12N9/08
CPC分类号： C12N9/1007
摘要： Described is a new enzyme, 31-O-desmethyl-FK-506 O-methyltransferase (FKMT) and its N-terminal amino acid sequence. This enzyme can specifically and preferentially methylate the C-31 hydroxy group in 31-O-desmethyl FK-506/FR-900506 and other 31-O-desmethyl analogs of FK-506/FR-900506 and related compounds such as 31-O-desmethyl immunomycin type molecules, also designated FK-520 and FR-900520 by Fujisawa. The enzyme can be isolated from a FK-506 producing microorganism Streptomyces sp. (Merck Culture Collection No. MA 6858) ATCC No. 55098. Employing the enzyme in its active form, supplemented with Mg.sup.+2 ion, in the presence of the methyl donor, S-adenosyl methionine (SAM), derivatives of 31-O-desmethyl FK-506, 31-O-desmethyl FK-520 and related 31-O-desmethyl compounds may be prepared.
摘要翻译：描述了一种新的酶，31-O-去甲基-FK-506 O-甲基转移酶（FKMT）及其N-末端氨基酸序列。该酶可以特异地和优先地甲基化31-O-脱甲基FK-506 / FR-900506中的C-31羟基和FK-506 / FR-900506的其它31-O-脱甲基类似物和相关化合物如31-O 也称为Fujisawa的FK-520和FR-900520。该酶可以从FK-506产生的微生物链霉菌（Streptomyces sp。）中分离出来。（Merck Culture Collection No.MA6858）ATCC No.55098.在甲基供体存在下使用活性形式的补充了Mg + 2离子的酶，S-腺苷甲硫氨酸（SAM），31-O的衍生物 - 甲基FK-506,31-O-去甲基FK-520和相关的31-O-脱甲基化合物。

4. 发明授权

US5093338A Lipophilic macrolide useful as an immunosuppressant 失效
标题翻译：亲脂性大环内酯可用作免疫抑制剂
公开(公告)号：US5093338A
公开(公告)日：1992-03-03
申请号：US690410
申请日：1991-04-23
申请人： Kevin Byrne , Robert T. Goegelman , Otto Hensens , Louis Kaplan , Jerrold M. Liesch
发明人： Kevin Byrne , Robert T. Goegelman , Otto Hensens , Louis Kaplan , Jerrold M. Liesch
IPC分类号： A61K31/445 , A61P31/04 , A61P37/06 , C07D498/18 , C12P17/18 , C12R1/55
CPC分类号： C07D498/18 , C12P17/188
摘要： Disclosed is a novel lipophilic macrolide of Formula I: ##STR1## The compound of assigned Formula I is an analog of rapamycin which has activity as an antifungal agent and as an immunosuppressant.

5. 发明授权

US5049546A Antibiotic agents 失效
公开(公告)号：US5049546A
公开(公告)日：1991-09-17
申请号：US495653
申请日：1990-03-19
申请人： David F. Sesin , Jerrold M. Liesch , Jimmy M. Fountoulakis , Prakash S. Masurekar , Louis Kaplan , Carol F. Wichmann
发明人： David F. Sesin , Jerrold M. Liesch , Jimmy M. Fountoulakis , Prakash S. Masurekar , Louis Kaplan , Carol F. Wichmann
IPC分类号： A61K31/40 , A61K38/00 , A61P31/04 , C07D487/14 , C07K7/56 , C07K14/195 , C07K14/41 , C12P17/18 , C12P21/04 , C12R1/01
CPC分类号： C12R1/645 , C07K7/56 , A61K38/00
摘要： A new antibiotic cyclic lipopeptide and a method of producing it are described. The agent has very high activity against human pathogens and is of very low mammalian toxicity.

6. 发明授权

US5021403A Antibiotic agents 失效
标题翻译：抗生素
公开(公告)号：US5021403A
公开(公告)日：1991-06-04
申请号：US495651
申请日：1990-03-19
申请人： David F. Sesin , Jerrold M. Liesch , Jimmy M. Fountoulakis , Prakash S. Masurekar , Louis Kaplan , Carol F. Wichmann
发明人： David F. Sesin , Jerrold M. Liesch , Jimmy M. Fountoulakis , Prakash S. Masurekar , Louis Kaplan , Carol F. Wichmann
IPC分类号： A61K38/00 , A61P31/04 , C07K7/56 , C07K14/195 , C07K14/41 , C12P17/18 , C12P21/04 , C12R1/645
CPC分类号： C07K7/56 , A61K38/00
摘要： A new antibiotic cyclic lipopeptide and a method of producing it are described. The agent has very high activity against human pathogens and is of very low mammalian toxicity.

7. 发明授权

US3942851A Indicating storage bin 失效
标题翻译：指示储物箱
公开(公告)号：US3942851A
公开(公告)日：1976-03-09
申请号：US494129
申请日：1974-08-02
申请人： Louis Kaplan
发明人： Louis Kaplan
IPC分类号： A47F5/00 , A47F3/14 , A47F5/12
CPC分类号： A47F5/0037
摘要： A storage bin is pivotly mounted relative to a housing so as to remain in a neutral position when empty and to be positioned at an angle with respect to a horizontal plane when either in a working position or in a storage position. When in the working position free access to the interior of the bin is possible since the forward end of the bin is tipped downwardly and the material in the bin is at the forward end. When in the storage position the front end of the bin is tipped upwardly with the material being at the rear of the bin. Indicating markers on the cabinet and the front end of each bin may be used when the bins are in the storage position for providing an approximation of the quantity of material in each bin. Since the bin will be horizontal and the front surface thereof will be readily visible, by providing a different color on the front surface of the bin and, optionally, on the bottom surface of each bin, means will be available for providing a rapid, visual indication of the approximate contents of each bin merely by glancing at the entire cabinet. In the alternative embodiment of this invention the bottom wall of the storage bin is stepped to provide a plurality of transversely and upwardly extending internal shoulders that permit an indication of a "low" quantity of articles therein when the articles are relatively lightweight and might not have sufficient mass to tip the bin. An external lip at the forward end of the bin may be used in cooperation with the indicator markers on the cabinet to provide a quick quantitative analysis of the inventory.The aforementioned Abstract is neither intended to define the invention of the application which, of course, is measured by the claims. Nor is it intended to be limiting as to the scope of the invention in any way.
摘要翻译：存储箱相对于壳体枢转安装，以便在空时保持在中立位置，并且当处于工作位置或在存放位置时相对于水平面定位成一定角度。当处于工作位置时，可以自由地进入垃圾箱的内部，因为垃圾桶的前端向下倾斜并且箱中的物料处于前端。当处于储存位置时，料仓的前端向上倾斜，材料位于料仓的后部。当箱体处于存储位置时，可以使用机柜和每个仓的前端上的指示标记，以便提供每个仓中材料数量的近似值。由于仓将是水平的并且其前表面将容易可见，通过在箱的前表面上以及可选地在每个箱的底表面上提供不同的颜色，装置将可用于提供快速，可视化仅通过扫视整个橱柜来指示每个仓库的大致内容。在本发明的替代实施例中，储物箱的底壁是阶梯式的，以提供多个横向和向上延伸的内部肩部，当制品相对较轻并且可能不具有足够的质量来提取垃圾箱。可以在机柜前端的外部唇缘与机柜上的指示标记配合使用，以便对库存进行快速的定量分析。

8. 发明授权

US5426038A Process for production of an antibiotic compound with Zalerion arboricola 失效
标题翻译：用Zalerion arboricola生产抗生素化合物的方法
公开(公告)号：US5426038A
公开(公告)日：1995-06-20
申请号：US195426
申请日：1994-02-14
申请人： Jimmy M. Fountoulakis , Prakash S. Masurekar , Louis Kaplan
发明人： Jimmy M. Fountoulakis , Prakash S. Masurekar , Louis Kaplan
IPC分类号： A61K38/00 , C07K7/56 , C12P21/00
CPC分类号： C07K7/56 , A61K38/00 , Y10S435/911
摘要： A process for producing an antibiotic compound which is normally a minor component in the cultivation of Z. arboricola to be the major product is described.
摘要翻译：本发明描述了一种制备抗生素化合物的方法，该抗生素化合物通常作为主要产品的培养中的次要成分。

9. 发明授权

US5318895A Aspergillus niger mutants 失效
标题翻译：黑曲霉突变体
公开(公告)号：US5318895A
公开(公告)日：1994-06-07
申请号：US956716
申请日：1992-10-05
申请人： Jennifer N. Kahn , Kevin M. Byrne , Louis Kaplan , Richard J. Monaghan
发明人： Jennifer N. Kahn , Kevin M. Byrne , Louis Kaplan , Richard J. Monaghan
IPC分类号： C12Q1/02 , C12Q1/18 , C07D498/00 , C12N1/00
CPC分类号： C12R1/685 , C12Q1/025 , Y10S435/911 , Y10S435/913 , Y10S435/917
摘要： Disclosed are new Aspergillus niger mutants which can be used for identifying active FK-506/ rapamycin type, or cyclosporin A type inununosuppressants in a broth, natural product extract, or composition exhibiting inununosuppressant activity. Specifically disclosed are the new mutants, ATCC No. 74085 (MF 5659), which is sensitive to FK-506 and rapamycin but resistant to cyclosporin A; ATCC No. 74086 (MF 5659) which is resistant to FK-506, cyclosporin A and rapamycin; and ATCC No. 74087 (MF 5661) which is resistant to FK-506 and rapamycin, but sensitive to cyclosporin A.
摘要翻译：公开了可以用于鉴定活性FK-506 /雷帕霉素类型的新型黑曲霉突变体，或在肉汤，天然产物提取物或具有抑制剂活性的组合物中的环孢菌素A型抑制剂。具体公开的是新的突变体ATCC No. 74085（MF5659），其对FK-506和雷帕霉素敏感，但对环孢菌素A具有抗性; 对抗FK-506，环孢菌素A和雷帕霉素的ATCC No.74086（MF5659）; 和对抗FK-506和雷帕霉素但对环孢菌素A敏感的ATCC No.74087（MF5661）。

10. 发明授权

US3940866A System for mounting three dimensional letters 失效
标题翻译：安装三维字母的系统
公开(公告)号：US3940866A
公开(公告)日：1976-03-02
申请号：US565497
申请日：1975-04-07
申请人： Louis Kaplan
发明人： Louis Kaplan
IPC分类号： G09F7/06
CPC分类号： G09F7/06
摘要： The present invention discloses a system for mounting three dimensional letters on a support surface wherein at least one clip is rigidly secured to the support surface proximate a bottom edge of the letter and at least one other clip is positioned on the support surface proximate a side edge of the letter. Both clips have tongues that engage the respective edges of the letter with at least the clip on the side of the letter having a deformable tongue. With the clips properly secured to the support surface the tongue of the side clip engages the letter, for example in a hole formed therein, and then the letter is forcibly moved downwardly so that the tongue of the bottom clip engages the letter and thereby the letter itself deforms the tongue of the side clip. An obtuse angle is thus generated between the two tongues. Any one of a number of different movable clamping devices, for example such as disclosed in U.S. Pat. No. 3,749,349, may be used at the top of the letter. When the letter is completely mounted, the rear plane thereof is spaced from the front plane of the support surface to permit flow of fluid to the space created in order to wash the front plane of the support surface.
摘要翻译：本发明公开了一种用于在支撑表面上安装三维字母的系统，其中至少一个夹子刚好地固定到靠近字母的底部边缘的支撑表面，并且至少一个另一个夹子位于支撑表面上，靠近侧边缘的信。两个夹具都具有与字母的各个边缘接合的舌头，至少具有可变形的舌头的字母侧上的夹子。当夹子适当地固定到支撑表面上时，侧夹子的舌部接合字母，例如在其中形成的孔中，然后将字母强制地向下移动，使得底部夹子的舌头接合字母，从而使字母接合本身使侧夹的舌头变形。因此在两个舌头之间产生钝角。许多不同的可移动夹紧装置中的任何一个，例如在美国专利No. 3,749,349号，可以在信的顶部使用。当字母完全安装时，其后平面与支撑表面的前平面间隔开，以允许流体流动到为了洗涤支撑表面的前平面而产生的空间。

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