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1. 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.

2. 发明申请

WO1989010257A1 TABLET PRESS 审中-公开
标题翻译：平板印刷机
公开(公告)号：WO1989010257A1
公开(公告)日：1989-11-02
申请号：PCT/US1989001565
申请日：1989-04-19
申请人： THE UPJOHN COMPANY , HIESTAND, Everett, N. , BALOG, Stephen
发明人： THE UPJOHN COMPANY
IPC分类号： B30B11/14
CPC分类号： B29C43/04 , B29C2043/046 , B29C2043/3615 , B29C2043/3618 , B30B11/02 , B30B11/14 , B30B15/022
摘要： A press (10) particularly for forming a blocklike tablet or compact from powder. A die (45) is split into opposed halves (54, 55) for defining a die opening (78) vertically therethrough. The die (45) is supported within a carrier (41) having an openable front door (48). The carrier (41) is mounted on a carriage (12) which is horizontally rollable on a base frame (23) between compacting and loading positions. The carrier (41) preferably has limited resilient floating movement relative to the carriage (12) in the vertical direction. A first pressure cylinder (61) has its housing (62) carried by the carrier (41) so that its piston rod (63) extends horizontally for direct compression against a rear side of the die (45). A second pressure cylinder (65) has its housing (66) mounted on the frame (11) and its piston rod (67) extending vertically downwardly for compression against a punch (74) which projects downwardly into the die opening (78) to compress the powders therein against a lower punch (72). The die (45) is vertically aligned with the piston rod (67) of this second cylinder (65) only when the carriage (12) is in the compacting position.
摘要翻译：一种压制机（10），特别用于从粉末形成块状片剂或压块。模具（45）被分成相对的两半（54,55），用于垂直地限定模具开口（78）。模具（45）支撑在具有可打开的前门（48）的托架（41）内。托架（41）安装在可在压实和装载位置之间在基架（23）上水平滚动的托架（12）上。载体（41）优选地在垂直方向上相对于滑架（12）具有有限的弹性浮动运动。第一压力缸（61）具有由托架（41）承载的壳体（62），使得其活塞杆（63）水平延伸，以抵抗模具（45）的后侧直接压缩。第二压力缸（65）具有安装在框架（11）上的壳体（66），并且其活塞杆（67）垂直向下延伸，以抵抗向下突出到模具开口（78）中的冲头（74）压缩其中的粉末相对于下冲头（72）。只有当滑架（12）处于压实位置时，模具45与第二气缸65的活塞杆67垂直对准。

3. 发明申请

WO1989011642A1 HARDNESS IMPACT TESTER 审中-公开
标题翻译：硬度冲击试验机
公开(公告)号：WO1989011642A1
公开(公告)日：1989-11-30
申请号：PCT/US1989001640
申请日：1989-04-21
申请人： THE UPJOHN COMPANY , HIESTAND, Everett, N. , BALOG, Stephen
发明人： THE UPJOHN COMPANY
IPC分类号： G01N03/52
CPC分类号： G01N3/52
摘要： A tester for testing hardness of a tablet formed from a compact of pharmaceutical powders. The tester has a spherical indenter (17) suspended from a wire (16) to impact the tablet to evaluate the hardness thereof. The tablet (27) is contained in a split die holder (26) which can regulate the die wall pressure. The indenter is supported against an electromagnet (20) and, when released, swings through a controlled arc and impacts the tablet. The indenter passes three photocells (41, 42, 45) in its downward arc toward the tablet, and the last photocell (41) activates both a timing device (46) connected to the first two photocells (42, 45) and a shutter plate (47) to prevent reimpact of the indenter with the tablet face. After impact with the tablet face, the indenter is timed as it rebounds past the first two photocells (42, 45). Since the distance between the first two photocells is known, the time it takes the indenter to travel between the first two photocells is sent to a computer and the velocity is calculated. The velocity is converted into rebound height of the indenter, and from this information, a calculation of the indentation hardness and the strain index is made.

4. 发明申请

WO1991011526A1 GAS DRIVEN MICROPROJECTILE ACCELERATOR 审中-公开
标题翻译：气体驱动微型加速器
公开(公告)号：WO1991011526A1
公开(公告)日：1991-08-08
申请号：PCT/US1990007264
申请日：1990-12-17
申请人： THE UPJOHN COMPANY , JONES, Lawrence, Duane , FREY, Paul, Timothy , GLEASON, David, Duane , CHEE, Paul, P. , SLIGHTOM, Jerry, L.
发明人： THE UPJOHN COMPANY
IPC分类号： C12N15/87
CPC分类号： C12N15/87 , C12M35/00 , C12M35/04 , C12N15/8207
摘要： A foreign substance, such as DNA, is injected into plant cells or tissue by means of a biological ballistical insertion technique. High pressure propellant gas is employed to accelerate the macroprojectile (86) containing microprojectiles coated with the foreign substance. A movable macroprojectile stop mechanism is provided between an upper injection chamber (13) and a lower sample-holding chamber (14) so that multiple shots of macroprojectiles can be made without disrupting the vacuum in the lower chamber (14). The stop mechanism includes removable stopper plugs (52) for stopping the macroprojectile. A vacuum seal (37, 43) is provided between the stop mechanism and the lower chamber.

5. 发明申请

WO1996018628A1 ALKYL SUBSTITUTED PIPERADINYL AND PIPERAZINYL ANTI-AIDS COMPOUNDS 审中-公开
标题翻译：烷基取代的哌嗪和哌嗪类抗艾滋病化合物
公开(公告)号：WO1996018628A1
公开(公告)日：1996-06-20
申请号：PCT/US1995014558
申请日：1995-11-28
申请人： THE UPJOHN COMPANY , ROMERO, Donna, L. , THOMAS, Richard, C. , MAY, Paul, D. , POEL, Toni-Jo
发明人： THE UPJOHN COMPANY
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D401/14
摘要： Anti-AIDS compounds of formula (I), where the aromatic/heteroaromatic ring is bonded to a carbon atom of the R8 substituent are disclosed as well as specific Anti-AIDS pyridines (V).
摘要翻译：公开了芳族/杂芳环与R 8取代基的碳原子键合的式（I）的抗艾滋病化合物以及具体的抗艾滋病吡啶（V）。

6. 发明申请

WO1996018395A1 USE OF PRAMIPEXOLE AS A NEUROPROTECTIVE AGENT 审中-公开
标题翻译：使用作为神经保护剂的PRAMIPEXOLE
公开(公告)号：WO1996018395A1
公开(公告)日：1996-06-20
申请号：PCT/US1995015613
申请日：1995-12-12
申请人： THE UPJOHN COMPANY , BOEHRINGER INGELHEIM KG , HALL, Edward, Dallas , VON VOIGTLANDER, Philip, F. , ROHDE, Frank, A.
发明人： THE UPJOHN COMPANY , BOEHRINGER INGELHEIM KG
IPC分类号： A61K31/425
CPC分类号： A61K31/428 , Y10S514/879
摘要： The present invention provides the use of pramipexole as a neuroprotective agent.
摘要翻译：本发明提供了普拉克索作为神经保护剂的用途。

7. 发明申请

WO1996015258A1 A SCINTILLATION PROXIMITY ASSAY FOR N-ACETYLGALACTOSAMINYLTRANSFERASE ACTIVITY 审中-公开
标题翻译： N-乙酰胆碱酯酶基因活性的SCINTILLATION近似性测定
公开(公告)号：WO1996015258A1
公开(公告)日：1996-05-23
申请号：PCT/US1995013483
申请日：1995-11-08
申请人： THE UPJOHN COMPANY , ELHAMMER, Ake, P.
发明人： THE UPJOHN COMPANY
IPC分类号： C12Q01/48
CPC分类号： C07K7/06 , C12Q1/48
摘要： This invention comprises a scintillation proximity assay designed to assay for the presence of N-acetylgalactosaminyltransferase, also known as GalNAc-transferase. The assay is most conveniently carried out on 96-well microtiterplates. The assay is especially suitable for large volume screens for compounds affecting GalNAc-transferase activity.
摘要翻译：本发明包括设计用于测定N-乙酰半乳糖胺基转移酶（也称为GalNAc-转移酶）的存在的闪烁亲近测定。该测定最方便地在96孔微量滴定板上进行。该测定特别适用于影响GalNAc转移酶活性的化合物的大体积筛选。

8. 发明申请

WO1996009309A1 THE OLIGOSACCHARIDE STRUCTURE OF A LIGAND FOR E AND P SELECTIN 审中-公开
标题翻译：用于E和P选择素的配体的低聚物结构
公开(公告)号：WO1996009309A1
公开(公告)日：1996-03-28
申请号：PCT/US1995011401
申请日：1995-09-15
申请人： THE UPJOHN COMPANY , ELHAMMER, Ake, P. , GENG, Jian-Guo
发明人： THE UPJOHN COMPANY
IPC分类号： C07H03/06
CPC分类号： C07H3/06
摘要： A specific ligand for E- and P-selectin was isolated from in vivo[ H]-glucosamine labeled HL-60 cells by a combination of weat germ agglutinin agarose and E- or P-selectin rIg-agarose chromatography. The total O-linked oligosaccharides on the purified molecule were released by alkaline hydrolysis in the presence of NaBH4 and analyzed by ion-exchange, size-exclusion and paper chromatography in combination with specific exoglycosidase digestions. Various derived ligands and carbohydrates are claimed.
摘要翻译：通过组合病毒凝集素琼脂糖和E-或P-选择素rIg-琼脂糖层析从体内[3 H] - 葡萄糖胺标记的HL-60细胞中分离出E-和P-选择蛋白的特异性配体。在NaBH4存在下，通过碱水解释放纯化分子上的O链寡糖，并通过离子交换，大小排阻和纸层析与特异性去糖基酶消化结合进行分析。要求各种衍生的配体和碳水化合物。

9. 发明申请

WO1995029922A1 METHANOL DERIVATIVES FOR TREATMENT OF RETROVIRAL INFECTIONS ESPECIALLY HIV INFECTIONS 审中-公开
标题翻译：用于治疗特发性感染的甲醇衍生物特别是艾滋病毒感染
公开(公告)号：WO1995029922A1
公开(公告)日：1995-11-09
申请号：PCT/US1995004444
申请日：1995-04-20
申请人： THE UPJOHN COMPANY , SMITH, Herman, W.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： The present invention relates to compounds of formula (I) which are imidazo[2,1-b]benzothiazole-3-methanol and imidazo[2,1-b]thiazole-5-methanol derivatives useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R1 is -H or -CH3; wherein R2 is -H or -CH3; or wherein R1 and R2 taken together are (a) formula (II), or (b) formula (III).
摘要翻译：本发明涉及用于抑制哺乳动物细胞中的逆转录病毒的咪唑并[2,1-b]苯并噻唑-3-甲醇和咪唑并[2,1-b]噻唑-5-甲醇衍生物的式（I）化合物感染所述逆转录病毒，其中R1是-H或-CH3; 其中R2是-H或-CH3; 或其中R 1和R 2一起是（a）式（II）或（b）式（III）。

10. 发明申请

WO1995020582A1 'DELTA'12,13-ISO-TAXOL ANALOGS, ANTINEOPLASTIC USE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译： DELTA <12,13> -ISO-TAXOL ANALOGS，ANTINEOPLASTIC USE AND PHARMACEUTICAL COMPOSITIONS CONTEMING THE THEM
公开(公告)号：WO1995020582A1
公开(公告)日：1995-08-03
申请号：PCT/US1995000551
申请日：1995-01-26
申请人： THE UPJOHN COMPANY , KELLY, Robert, C. , WUTS, Peter, G., M. , WICNIENSKI, Nancy, Anne
发明人： THE UPJOHN COMPANY
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： This invention provides 7-deoxy- DELTA -iso-taxol analogs of formula (I). The compounds of formula (I) are useful for the treatment of the same cancers for which taxol has been shown active, including human ovarian cancer, breast cancer, and malignant melanoma as well as lung cancer, gastric cancer, colon cancer, head and neck cancer, and leukemia.
摘要翻译：本发明提供了式（I）的7-脱氧-ΔTA-13-异紫杉醇类似物。式（I）化合物可用于治疗已经显示紫杉醇活性的相同癌症，包括人卵巢癌，乳腺癌和恶性黑素瘤以及肺癌，胃癌，结肠癌，头颈部癌症和白血病。

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