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31. 发明申请

WO1992000290A1 ANTIATHEROSCLEROTIC AND ANTITHROMBOTIC 2-AMINO-6-PHENYL-4H-PYRAN-4-ONES 审中-公开
标题翻译：抗癌药和抗癌药2-氨基-6-苯基-4H-吡喃-4-酮
公开(公告)号：WO1992000290A1
公开(公告)日：1992-01-09
申请号：PCT/US1991003659
申请日：1991-06-03
申请人： THE UPJOHN COMPANY , MORRIS, Joel
发明人： THE UPJOHN COMPANY
IPC分类号： C07D309/38
CPC分类号： C07D405/12 , C07D309/38
摘要： This invention relates to compounds of formula (I), which are useful as antiatherosclerotic agents and inhibitors of cell proliferation for the treatment of proliferative diseases. In addition, various compounds of formula (I) are useful inhibitors of platelet aggregation.
摘要翻译：本发明涉及式（I）化合物，其可用作抗动脉粥样硬化剂和用于治疗增殖性疾病的细胞增殖抑制剂。此外，式（I）的各种化合物是血小板聚集的有用的抑制剂。

32. 发明申请

WO1991015589A1 IMPROVED PROCESS OF PURIFYING RECOMBINANT PROTEINS AND COMPOUNDS USEFUL IN SUCH PROCESS 审中-公开
标题翻译：净化重组蛋白的改进方法及其在此过程中有用的化合物
公开(公告)号：WO1991015589A1
公开(公告)日：1991-10-17
申请号：PCT/US1991001543
申请日：1991-03-11
申请人： THE UPJOHN COMPANY , SHARMA, Satish, K.
发明人： THE UPJOHN COMPANY
IPC分类号： C12N15/62
CPC分类号： C07K7/06 , C07K7/08 , C07K14/005 , C07K2319/00 , C07K2319/20 , C12N9/12 , C12N15/62 , C12N2740/16322
摘要： Recombinant fusion proteins which comprise a biologically active polypeptide portion and metal chelating peptide are disclosed. The fusion proteins contain metal chelating peptides which have at least three and preferably six alternating histidine residues. Fusion proteins which contain metal chelating peptides that are substrates for dipeptidylpeptidase I are als disclosed. Additionally, a method of obtaining desired polypeptides by producing recombinant fusion proteins and purifying them with immobilized metal ions is disclosed. A kit for purifying desired polypeptides is also disclosed.
摘要翻译：公开了包含生物活性多肽部分和金属螯合肽的重组融合蛋白。融合蛋白含有金属螯合肽，其具有至少三个，优选六个交替的组氨酸残基。含有作为二肽基肽酶I底物的金属螯合肽的融合蛋白是公开的。另外，公开了通过制备重组融合蛋白并用固定的金属离子纯化所需多肽的方法。还公开了用于纯化所需多肽的试剂盒。

33. 发明申请

WO1991013146A1 RUMINAL BACTERIUM FOR PREVENTING ACUTE LACTIC ACIDOSIS 审中-公开
标题翻译：用于预防急性浸润性溃疡的肿瘤细菌
公开(公告)号：WO1991013146A1
公开(公告)日：1991-09-05
申请号：PCT/US1991000857
申请日：1991-02-13
申请人： THE UPJOHN COMPANY , LEEDLE, Jane, Alice, Zeigler , GREENING, Richard, Charles , SMOLENSKI, walter, Joseph
发明人： THE UPJOHN COMPANY
IPC分类号： C12N01/20
CPC分类号： C12R1/01 , A23K10/18 , A23K50/10 , A61K35/74
摘要： This invention relates to a bacterial culture, NRRL B-18624, method for facilitating adaptation of ruminants from roughage or normal pasture diet to a higher energy diet, and a composition therefor comprising the bacterial culture.
摘要翻译：本发明涉及一种细菌培养物NRRL B-18624，用于促进从粗饲料或正常牧草饮食向较高能量饮食适应反刍动物的方法及其组合物，其包含细菌培养物。

34. 发明申请

WO1991011523A1 STRAIN RAL-4, USEFUL FOR PRODUCTION OF SMALL PROTEINS AND PEPTIDES 审中-公开
标题翻译：应变RAL-4，有用于生产小蛋白和肽
公开(公告)号：WO1991011523A1
公开(公告)日：1991-08-08
申请号：PCT/US1991000265
申请日：1991-01-18
申请人： THE UPJOHN COMPANY , LEPLEY, Robert, Alan , OLSON, Eric, Robert
发明人： THE UPJOHN COMPANY
IPC分类号： C12N15/70
CPC分类号： C07K14/65 , A61K38/00 , C07K14/60 , C12N15/70 , C12N15/71 , C12R1/19
摘要： This invention presents a novel strain of E. coli, RAL-4, which is a tryptophan auxotroph and shows enhanced expression of proteins and peptides. In addition, this invention presents a method for achieving enhanced expression of proteins and peptides either by the use of RAL-4 or via generation of a host cell auxotrophy for an amino acid not resident in the heterologous protein to be expressed. In an embodiment of the invention, IGF-I and GRF are exprressed at levels above that found in wild type controls
摘要翻译：本发明提出了一种新型大肠杆菌菌株RAL-4，其是色氨酸营养缺陷型并且表现出增强的蛋白质和肽的表达。此外，本发明提供了通过使用RAL-4或通过产生宿主细胞营养缺陷来实现蛋白质和肽的增强表达的方法，用于不表达异源蛋白质中的氨基酸。在本发明的一个实施方案中，IGF-1和GRF以高于野生型对照中发现的水平进行表达

35. 发明申请

WO1991007430A1 PEPTIDES CONTAINING CYCLIC TRIPEPTIDES 审中-公开
标题翻译：含有环孢霉素的肽
公开(公告)号：WO1991007430A1
公开(公告)日：1991-05-30
申请号：PCT/US1990005744
申请日：1990-10-12
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit
发明人： THE UPJOHN COMPANY
IPC分类号： C07K05/02
CPC分类号： C07K7/54 , A61K38/00 , C07K5/0215
摘要： The present invention provides novel peptides. These peptides are useful as renin inhibitors and have a novel cyclic tripeptide of formula (I) at the N-terminus. Some of these peptides also have a non-cleavable transition state insert corresponding to the 10,11-position of the renin substrate (angiotensinogen). Renin inhibitors are useful for the diagnosis and control of renin-dependent hypertension, congestive heart failure, renin-dependent hyperaldosterism, other renin-dependent cardiovascular disorders and ocular disorders. These peptides are also useful as inhibitors of HIV-I protease. Inhibitors of HIV-I protease are useful for treating humain acquired immunodeficiency disease syndrome (AIDS).
摘要翻译：本发明提供新的肽。这些肽可用作肾素抑制剂，并且在N-末端具有新的式（I）的环状三肽。这些肽中的一些还具有对应于肾素底物（血管紧张素原）的10,11位的不可切割的过渡态插入物。肾素抑制剂可用于诊断和控制肾素依赖性高血压，充血性心力衰竭，肾素依赖性醛固酮增多症，其他肾素依赖型心血管疾病和眼部疾病。这些肽也可用作HIV-1蛋白酶的抑制剂。 HIV-1蛋白酶抑制剂可用于治疗人类获得性免疫缺陷综合征（AIDS）。

36. 发明申请

WO1991003721A1 SLOW STRAIN RATE SHEAR STRENGTH TESTER FOR COMPACT 审中-公开
标题翻译：低应变率剪切强度试验机
公开(公告)号：WO1991003721A1
公开(公告)日：1991-03-21
申请号：PCT/US1990004455
申请日：1990-08-14
申请人： THE UPJOHN COMPANY , HIESTAND, Everett, N. , GLEASON, David, Duane , BALOG, Stephen
发明人： THE UPJOHN COMPANY
IPC分类号： G01N03/40
CPC分类号： G01N3/42 , G01N33/15 , G01N2203/0019 , G01N2203/0098
摘要： A slow strain rate shear strength tester for a tablet of compressed pharmaceutical powders, which apparatus includes a ram assembly (25) having a reciprocal ram (28) horizontally slidably supported on a housing. The ram projects outwardly of the housing and mounts a compression member (31) on the free end thereof. A head arrangement (13) is removably mounted on a pair of brackets (36, 37) which project from the end of the housing. The head arrangement has opposed holding members (71, 72) which cooperate to define a notch (74, 78) for accommodating a compact therein in position for compression by the ram.

37. 发明申请

WO1991001884A1 COMBINED INK LASER PRINTING OF TABLETS 审中-公开
标题翻译：组合墨水激光打印片
公开(公告)号：WO1991001884A1
公开(公告)日：1991-02-21
申请号：PCT/US1990004098
申请日：1990-07-27
申请人： THE UPJOHN COMPANY , REDFORD, Chris, R. , SACKMAN, Carl, H.
发明人： THE UPJOHN COMPANY
IPC分类号： B41F17/36
CPC分类号： A61J3/007 , B41F17/36
摘要： A process and apparatus for branding tablets, including a feeder (22) defining a row of recesses (23) each being adapted to accommodate a tablet. The feeder (22) moves individual tablets into a first station whereat an offset printing device (35) prints a graphic ink symbol or geometric ink shape on an exposed face of the tablet. The feeder then moves the tablet to a second station whereat a laser marking system (41) removes portions of the offset printed ink to expose the tablet material therebeneath.
摘要翻译：一种用于品牌片剂的方法和装置，包括限定一排凹槽（23）的进料器（22），每个凹槽适于容纳片剂。馈送器（22）将各个片剂移动到第一站，其中胶版印刷设备（35）在图形输入板的曝光面上印刷图形墨水符号或几何墨水形状。进料器然后将片剂移动到第二工位，激光打标系统（41）移除胶版印刷油墨的部分以暴露其下方的片材材料。

38. 发明申请

WO1991000870A1 SOMATOTROPIN ANALOGS 审中-公开
标题翻译： SOMATOTROPIN模拟
公开(公告)号：WO1991000870A1
公开(公告)日：1991-01-24
申请号：PCT/US1990003550
申请日：1990-06-27
申请人： THE UPJOHN COMPANY , LEHRMAN, Sherwood, Russ , HAVEL, Henry, A. , TULS, Jody, L. , PLAISTED, Scott, M. , BREMS, David, N.
发明人： THE UPJOHN COMPANY
IPC分类号： C07K07/10
CPC分类号： C07K14/61
摘要： The present invention provides analogs of animal somatotropins particularly with changes in the amino acids between residue 96 to 133 which are changed to reduce hydrophobicity or helical stability.
摘要翻译：本发明提供动物生长激素的类似物，特别是残基96至133之间的氨基酸的变化，其被改变以降低疏水性或螺旋稳定性。

39. 发明申请

WO1991000856A2 (1,2N) AND (3,2N)-CARBOCYCLIC-2-AMINO TETRALIN DERIVATIVES 审中-公开
标题翻译：（1,2N）和（3,2N） - 芳基-2-氨基四氢萘衍生物
公开(公告)号：WO1991000856A2
公开(公告)日：1991-01-24
申请号：PCT/US1990003551
申请日：1990-06-27
申请人： THE UPJOHN COMPANY , LIN, Chiu-Hong
发明人： THE UPJOHN COMPANY
IPC分类号： C07D209/60
CPC分类号： C07C217/74 , C07D209/60 , C07D221/08 , C07D221/10
摘要： This invention is therapeutically useful tetralins and pharmaceutically acceptable acid addition salts thereof of formula (I) wherein R, R1 and A are as defined in claim 1. These compounds are useful to treat central nervous system disorders.
摘要翻译：本发明是治疗上有用的式（I）的四氢化萘及其药学上可接受的酸加成盐，其中R，R 1和A如权利要求1中所定义。这些化合物可用于治疗中枢神经系统疾病。

40. 发明申请

WO1990015816A1 SURAMIN TYPE COMPOUNDS AND ANGIOSTATIC STEROIDS TO INHIBIT ANGIOGENESIS 审中-公开
标题翻译： SAMAMIN型化合物和抗抑郁药物抑制血管生成
公开(公告)号：WO1990015816A1
公开(公告)日：1990-12-27
申请号：PCT/US1990002673
申请日：1990-05-17
申请人： THE UPJOHN COMPANY , ARISTOFF, Paul, A. , MITCHELL, Mark, A. , WILKS, John, W.
发明人： THE UPJOHN COMPANY
IPC分类号： C07J03/00
CPC分类号： C07J3/005 , A61K31/565 , A61K31/57 , A61K31/185 , A61K2300/00
摘要： The invention is a method of treating angiogenesis in a warm blooded mammal who is in need of such treatment which comprises administration of an angiogenic inhibiting amount of a combination of a suramin-type compound and an angiostatic steroid. Angiostatic steroids include the known 20-substituted steroids of formula (I), 21-hydroxy steroids of formula (II), C11-functionalized steroids of formula (III) as well as the novel DELTA -etianic esters of formula (IV), as well as various individual known steroids.
摘要翻译：本发明是一种治疗需要这种治疗的温血动物哺乳动物的血管发生的方法，其包括施用血管生成抑制量的苏拉明型化合物和血管抑制类固醇的组合。血管甾醇类固醇包括已知的式（I）的20-取代的类固醇，式（II）的21-羟基类固醇，式（III）的C 11官能化类固醇以及式（III）的新型DELTA <9（11）式（IV），以及各种已知的各种类固醇。

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