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51. 发明申请

WO1990006761A1 TRANSDERMAL AND INTRANASAL ADMINISTRATION OF RENIN INHIBITORY PEPTIDES 审中-公开
标题翻译：瑞恩抑制肽的转移和内毒素治疗
公开(公告)号：WO1990006761A1
公开(公告)日：1990-06-28
申请号：PCT/US1989005343
申请日：1989-12-01
申请人： THE UPJOHN COMPANY , PALS, Donald, Theodore , OLANOFF, Lawrence, S. , LAWSON, Judy, Ann , GIBSON, Richard, Earle
发明人： THE UPJOHN COMPANY
IPC分类号： A61K37/02
CPC分类号： A61K9/0043 , A61K9/7023 , A61K38/553
摘要： The present invention provides transdermal and intranasal means to administer renin inhibitory peptides and compositions adapted therefor.
摘要翻译：本发明提供用于施用肾素抑制肽的经皮和鼻内装置以及适于其的组合物。

52. 发明申请

WO1990006367A1 TRANSGENIC MICE FOR THE ANALYSIS OF HAIR GROWTH 审中-公开
标题翻译：用于分析头发生长的转基因小鼠
公开(公告)号：WO1990006367A1
公开(公告)日：1990-06-14
申请号：PCT/US1989005055
申请日：1989-11-17
申请人： THE UPJOHN COMPANY , MCNAB, Alistair, R. , WOOD, Linda, S. , VOGELI, Gabriel , KAYTES, Paul, S.
发明人： THE UPJOHN COMPANY
IPC分类号： C12N15/85
CPC分类号： C12N15/8509 , A01K67/0275 , A01K2217/05 , A01K2227/103 , A01K2227/105 , A01K2267/0393 , C07K14/4741 , C12N15/85 , C12N2830/008
摘要： This invention is a transgenic, non-human mammal having a recombinant transgene comprising a promoter sequence from a gene which codes for a hair specific protein and a reporter gene. This recombinant gene is introduced into the animal, or an ancestor of the animal, at an embryonic stage. Hair specific proteins are expressed by skin cells during the hair growth cycle. Reporter genes are genes for which expression is detectable. The transgenic animal of the present invention will express the reporter gene when induced under the control of the regulatory mechanisms for hair growth present in the animal. Consequently, the transgenic animal of the present invention provides a system to study regulation of genes related to hair growth and a system which provides tissue specific, time specific limits on expression of structural transgenes.
摘要翻译：本发明是具有重组转基因的转基因非人哺乳动物，其包含编码毛发特异性蛋白质和报道基因的基因的启动子序列。在胚胎期将该重组基因导入动物或动物祖先。毛发生长周期中，毛发特异性蛋白质由皮肤细胞表达。报告基因是可检测表达的基因。当在动物中存在的毛发生长的调控机制的控制下诱导时，本发明的转基因动物将表达报道基因。因此，本发明的转基因动物提供了一种研究与毛发生长有关的基因调节的系统，以及提供结构转基因表达的组织特异性，时间特异性限制的系统。

53. 发明申请

WO1990003725A1 TRANSFORMATION OF CUCUMBER BY AGROBACTERIUM TUMEFACIENS AND THE REGENERATION OF TRANSFORMED CUCUMBER PLANTS 审中-公开
标题翻译：农杆菌转化玉米和转化后的植物的再生
公开(公告)号：WO1990003725A1
公开(公告)日：1990-04-19
申请号：PCT/US1989003891
申请日：1989-09-14
申请人： THE UPJOHN COMPANY , CHEE, Paula, P.
发明人： THE UPJOHN COMPANY
IPC分类号： A01H04/00
CPC分类号： A01H4/00 , C12N15/8205
摘要： A method for the transfer and integration of genetic materials into the genome of Cucumis plants using explants from the cotyledons and hypocotyl to produce transformed embryoids and the regeneration of transformed plants from the embryoids.
摘要翻译：使用来自子叶和下胚轴的外植体将遗传物质转移并整合到黄瓜植物的基因组中的方法，以产生转化的胚状体以及从胚状体再生转化的植物。

54. 发明申请

WO1990002137A1 RENIN INHIBITORY PEPTIDES CONTAINING SULEPTANIC ACID OR DERIVATIVES THEREOF 审中-公开
标题翻译：含有亚油酸或其衍生物的RENIN抑制肽
公开(公告)号：WO1990002137A1
公开(公告)日：1990-03-08
申请号：PCT/US1989003093
申请日：1989-07-20
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit
发明人： THE UPJOHN COMPANY
IPC分类号： C07K05/02
CPC分类号： C07K5/0227
摘要： The present invention provides novel renin-inhibiting peptides having a non-cleavable transition state insert corresponding to the 10,11-position of the renin substrate (angiotensinogen) and having a suleptanic acid moiety or derivatives thereof of formula L1 at the N-terminus of the peptide. Such 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.

55. 发明申请

WO1989012452A1 FINE-MILLED COLESTIPOL HYDROCHLORIDE 审中-公开
标题翻译：精细磨砂盐酸盐
公开(公告)号：WO1989012452A1
公开(公告)日：1989-12-28
申请号：PCT/US1989002187
申请日：1989-05-24
申请人： THE UPJOHN COMPANY , MCCURDY, Vincent, E. , SPILMAN, Charles, H.
发明人： THE UPJOHN COMPANY
IPC分类号： A61K31/785
CPC分类号： A61K31/785 , A61K9/14 , A61K31/19 , A61K2300/00
摘要： The present invention provides a novel fine milled form of a known pharmaceutical composition, colestipol hydrochloride. This fine milled form of colestipol hydrochloride yields pharmaceutically elegant dosage forms exhibiting increased potency, including non-gritty oral powders and high dose oral tablets (e.g., 1000 mg tablets). Conventional colestipol hydrochloride was heretoforth available in spherical granules which produced less elegant (gritty) oral suspensions and oral tablets with substantially lower doses of drug (e.g., ca 500 mg).
摘要翻译：本发明提供了一种已知药物组合物的新型精细研磨形式，盐酸考来替泊。盐酸考来替泊的这种精细研磨形式产生显示出增加的效力的药学上优雅的剂型，包括非致密口服粉剂和高剂量口服片剂（例如1000mg片剂）。常规的盐酸考来昔泊可以以球形颗粒形式提供，其产生较不优雅（粗砂）的口服悬浮液和具有基本较低剂量的药物（例如约500mg）的口服片剂。

56. 发明申请

WO1989007651A2 METHODS FOR CONTROLLING NORLEUCINE CONTENT IN POLYPEPTIDES 审中-公开
标题翻译：控制多糖含量的方法
公开(公告)号：WO1989007651A2
公开(公告)日：1989-08-24
申请号：PCT/US1989000425
申请日：1989-02-07
申请人： THE UPJOHN COMPANY , BRUNNER, David, P. , HARBOUR, Gary, C. , KIRSCHNER, Richard, J. , PINNER, James, F. , GARLICK, Robert, L.
发明人： THE UPJOHN COMPANY
IPC分类号： C12P21/00
CPC分类号： C12P21/02 , C07K14/61 , C12P1/00 , C12P13/04
摘要： The present invention provides an inexpensive fermentation medium for growing microorganisms. Also provided are fermentation media and methods for producing norleucine by growing E. coli thereon, fermentation media and methods for incorporating norleucine into polypeptides expressed by microorganisms grown thereon, and fermentation media and methods for preventing the incorporation of norleucine into polypeptides expressed by microorganisms grown thereon. Also provided are bovine somatotropin analogs.
摘要翻译：本发明提供了用于生长微生物的廉价的发酵培养基。还提供了发酵培养基和通过在其上生长大肠杆菌来生产正亮氨酸的方法，发酵培养基和将正亮氨酸掺入由其上生长的微生物表达的多肽的方法，以及发酵培养基和用于防止将正亮氨酸掺入由其上生长的微生物表达的多肽的方法。还提供了牛生长激素类似物。

57. 发明申请

WO1989007113A1 GRF ANALOGS 审中-公开
标题翻译： GRF模拟
公开(公告)号：WO1989007113A1
公开(公告)日：1989-08-10
申请号：PCT/US1989000245
申请日：1989-01-27
申请人： THE UPJOHN COMPANY , FRIEDMAN, Alan, R.
发明人： THE UPJOHN COMPANY
IPC分类号： C07K07/10
CPC分类号： C07K14/60 , A61K38/00
摘要： GRF peptides wherein a cysteic acid residue (Cya) is substituted for the amino acid in position R3 and/or R25.

58. 发明申请

WO1989004672A1 DERIVATIVES OF LINCOSAMINIDE ANTIBIOTICS 审中-公开
标题翻译：林酰胺抗生素的衍生物
公开(公告)号：WO1989004672A1
公开(公告)日：1989-06-01
申请号：PCT/US1988003865
申请日：1988-11-07
申请人： THE UPJOHN COMPANY , BRISON, Jean , TULKENS, Paul, M. , BOTTCHER, Patrick , ZENEBERGH, Andree
发明人： THE UPJOHN COMPANY
IPC分类号： A61K47/00
CPC分类号： C07H15/16 , A61K47/643 , A61K47/6809 , A61K47/6889
摘要： The invention relates to a new pharmaceutical form of a medicament of the formula: Lincosaminide-Radical-Carrier in which ''Lincosaminide'' represents an antibiotic lincosaminide; ''Radical'' represents a radical bound through a carboxylic function to the hydroxyl group of the antibiotic with another functional group susceptible to allow the attachment of the ''Lincosaminide-Radical'' complex to a carrier; and ''Carrier'' represents a peptide, a protein, or another macromolecule with free amino or carboxyl group(s) which allows the ''Lincosaminide-Radical-Carrier'' complex to specifically bind to cells. The ''Lincosaminide-Radical-Carrier'' complex is useful to treat bacterial infections and is particularly useful to treat bovine mastitis.
摘要翻译：本发明涉及新的药物形式的下式的药物：氯化钠 - 自由基 - 载体，其中“氯菌胺”代表抗生素长春碱; “自由基”表示通过羧基官能团与抗生素的羟基结合的自由基，另一个官能团易于将“氯霉素 - 自由基”复合物附着到载体上; 和“载体”表示肽，蛋白质或具有游离氨基或羧基的另一个大分子，其允许“氯氰菊酯 - 自由基 - 载体”复合物特异性结合细胞。 “氯氰菊酯 - 自由基 - 载体”复合物可用于治疗细菌感染，特别适用于治疗牛乳腺炎。

59. 发明申请

WO1989001936A1 PROCESS FOR PRODUCTION OF PROSTAGLANDIN INTERMEDIATES 审中-公开
标题翻译：生产PROSTAGLANDIN中间体的方法
公开(公告)号：WO1989001936A1
公开(公告)日：1989-03-09
申请号：PCT/US1988002293
申请日：1988-07-11
申请人： THE UPJOHN COMPANY , SADDLER, John, C. , SYMONDS, John, H.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D307/935
CPC分类号： C07D307/935
摘要： The present invention is a process for the production of a ketolactone of formula (III) which comprises contacting and aldehyde lactone of formula (I) with a beta -ketophosphonate (X1-O-)2-PO-CH2-CO-X15 (II). The ketolactone (III) is a useful intermediate in the synthesis of prostaglandins.
摘要翻译：本发明是制备式（III）的酮内酯的方法，其包括使式（I）的醛内酯与β-酮膦酸酯（X1-O-）2-PO-CH2-CO-X15（II ）。酮内酯（III）是合成前列腺素的有用中间体。

60. 发明申请

WO1989000558A1 AMINE SALTS OF ALKANE-1,n-DICARBOXYLIC ACID MONO-(2-SULFATO-ETHYL)AMIDES 审中-公开
标题翻译： ALKANE-1，正二羧酸单 - （2-硫代 - 乙基）胺的胺盐
公开(公告)号：WO1989000558A1
公开(公告)日：1989-01-26
申请号：PCT/US1988002181
申请日：1988-07-01
申请人： THE UPJOHN COMPANY , PEARLMAN, Bruce, A.
发明人： THE UPJOHN COMPANY
IPC分类号： C07C143/155
CPC分类号： C07J41/005
摘要： Amine salts of alkane-1,n-dicarboxylic acid mono-(2-sulfato-ethyl)amides of the formula (I): HOC(O)-(CH2)n-C(O)-N(R1)-CH2CH2SO3 HN(R2)3, wherein R1 is selected from the group consisting of hydrogen, C1-C8 alkyl and phenyl, R2 is C1-C8 alkyl or (R2)3 when taken together with the nitrogen atom is pyridinyl; and n is an integer from 4 to 20, their preparation and use to prepare water-soluble esters of corticosteroids.
摘要翻译：式（I）的烷烃-1正 - 二羧酸单 - （2-磺酸基 - 乙基）酰胺的盐：HOC（O） - （CH2）nC（O）-N（R1）-CH2CH2SO3 - 其中R 1选自氢，C 1 -C 8烷基和苯基，R 2为C 1 -C 8烷基或（R 2）3，当与氮原子一起为吡啶基时; 并且n为4-20的整数，它们的制备和用途是制备皮质类固醇的水溶性酯。

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