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1. 发明申请

WO1989005624A1 TRI-SCORED DRUG TABLET 审中-公开
公开(公告)号：WO1989005624A1
公开(公告)日：1989-06-29
申请号：PCT/US1988004367
申请日：1988-12-12
申请人： THE UPJOHN COMPANY , NI, Phillip, F. , ODAR, Larry, F.
发明人： THE UPJOHN COMPANY
IPC分类号： A61J03/10
CPC分类号： A61J3/10 , A61K9/2072
摘要： A tri-scored drug tablet (10) having an elongated tablet body (11) with a length greater than its width. The body (11) has a bottom facing surface with a pair of concavities (23, 24) therein. Each concavity (23, 24) is equal in size and has parallel major and minor axes, each concavity (23, 24) further having a smooth and uninterrupted arcuate surface extending between the opposite longitudinal ends of said body (11) and a longitudinally central part of said tablet (10). The opposite longitudinal ends of the body (11) and the longitudinally central part are of a thicker dimension than the thickness of the body (11) measured at an apex of each of the concavities (23, 24). Aligned breaking grooves (21, 29, 31, 32) are formed in the top and bottom surfaces at both of the concavities (23, 24) and between the concavities (23, 24) at said longitudinally central part, each of breaking groove (21, 29, 31, 32) extending laterally across the width of said tablet (10) at said apex of each of said concavities (23, 24) at said longitudinally central part to divide the tablet (10) into four quarter sections (48, 49, 51, 52) of equal size.
摘要翻译：具有长度大于其宽度的细长片剂本体（11）的三片药片（10）。主体（11）具有底面朝向的表面，其中具有一对凹部（23,24）。每个凹部（23,24）的尺寸相等并且具有平行的主轴和短轴，每个凹部（23,24）还具有在所述主体（11）的相对的纵向端部之间延伸的平滑且不间断的弓形表面，并且纵向中心所述片剂（10）的一部分。主体（11）和纵向中心部分的相对的纵向端部具有比在每个凹部（23,24）的顶点处测量的主体（11）的厚度更大的尺寸。在两个凹部（23,24）的顶表面和底表面以及在所述纵向中心部分处的凹部（23,24）之间形成有分隔开的凹槽（21,29,31,32），每个断裂槽在所述纵向中心部分处，在每个所述凹部（23,24）的顶点处横向延伸穿过所述片剂（10）的宽度的横截面（21,29,31,32），以将片剂（10）分成四个四分之一部分，49,51,52）。

2. 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）。

3. 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。

4. 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。

5. 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。

6. 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）。

7. 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。

8. 发明申请

WO1995004713A1 2-AMINOINDANS AS SELECTIVE DOPAMINE D3 LIGANDS 审中-公开
标题翻译： 2-AMINOINDANS作为选择性DOPAMINE D3配体
公开(公告)号：WO1995004713A1
公开(公告)日：1995-02-16
申请号：PCT/US1994008046
申请日：1994-07-21
申请人： THE UPJOHN COMPANY , HAADSMA-SVENSSON, Susanne, R. , ANDERSSON, Bengt, R. , SONESSON, Clas, A. , LIN, Chiu-Hong , WATERS, R., Nicholas , SVENSSON, Kjell, A., I. , CARLSSON, Per, A., E. , HANSSON, Lars, Olov , STJERNLOF, Nils, Peter
发明人： THE UPJOHN COMPANY
IPC分类号： C07C211/42
CPC分类号： C07D207/325 , C07C211/42 , C07C215/42 , C07C217/52 , C07C217/74 , C07C219/26 , C07C223/04 , C07C225/20 , C07C229/50 , C07C233/43 , C07C233/44 , C07C237/48 , C07C255/54 , C07C255/58 , C07C309/65 , C07C309/66 , C07C309/73 , C07C311/08 , C07C311/21 , C07C311/39 , C07C317/36 , C07C2602/08 , C07D209/48 , C07D295/096 , C07D295/135 , C07D317/70 , C07D319/14 , C07D333/20
摘要： Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of formula (I), wherein R1 and R2 are independently chosen from hydrogen, C1-C8 alkyl, OCH3, OH, OSO2CF3, OSO2CH3, SOR5, CO2R5, CONH2, CONR5R6, COR5, CF3, CN, SR5, SO2NH2, SO2NR5R6, SO2R5, -OCO-C1-C6 alkyl, -NCO-C1-C6 alkyl, -CH2O-C1-C6 alkyl, -CH2OH, -CO-Aryl, -NHSO2-Aryl, -NHSO2-C1-C6 alkyl, phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazol, halogen (Br, Cl, F, I), R6 or R1 and R2 together form -O(CH2)mO- (where m is 1-2) or -CH2(CH2)pCH2 - (where p is 1-4); (except that only one of R1 and R2 can be hydrogen, OCH3 or OH in any such compound); R3 and R4 are independently chosen from C2-C4 alkenyl, C3-C8 alkynyl, C3-C8 cycloalkyl, -(CH2)p-thienyl (where p is 1-4), hydrogen (except that only one of R3 and R4 can be hydrogen in any such compound) or C1-C8 alkyl (except where R1 or R2 are hydrogen, OCH3 or OH); R5 is hydrogen, C1-C8 alkyl, C2-C4 alkenyl, C3-C8 cycloalkyl; and R6 is C1-C8 alkyl, C2-C4 alkenyl, C2-C8 alkynyl, C3-C8 cycloalkyl, or Aryl.
摘要翻译：化合物及其药学上可接受的盐适用于治疗与式（I）的多巴胺D3受体活性相关的中枢神经系统疾病，其中R1和R2独立地选自氢，C1-C8烷基，OCH3，OH，OSO2CF3，OSO2CH3，SOR5 ，CO 2 R 5，CONH 2，CONR 5 R 6，COR 5，CF 3，CN，SR 5，SO 2 NH 2，SO 2 NR 5 R 6，SO 2 R 5，-OCO-C 1 -C 6烷基，-NCO-C 1 -C 6烷基，-CH 2 O-C 1 -C 6烷基，-CH 2 OH，-CO 芳基，-NHSO 2 - 芳基，-NHSO 2 -C 1烷基，邻苯二甲酰亚胺，噻吩基，吡咯，吡咯啉基，恶唑，卤素（Br，Cl，F，I），R 6或R 1和R 2一起形成-O（CH 2） - （其中m为1-2）或-CH2（CH2）pCH2 - （其中p为1-4）; （除了R1和R2中只有一个可以是任何这样的化合物中的氢，OCH 3或OH）; R 3和R 4独立地选自C 2 -C 4烯基，C 3 -C 8炔基，C 3 -C 8环烷基， - （CH 2）p - 噻吩基（其中p为1-4），氢（除了R 3和R 4中只有一个可以任何这样的化合物中的氢）或C 1 -C 8烷基（除了其中R 1或R 2是氢，OCH 3或OH）; R5是氢，C1-C8烷基，C2-C4烯基，C3-C8环烷基; 并且R 6是C 1 -C 8烷基，C 2 -C 4烯基，C 2 -C 8炔基，C 3 -C 8环烷基或芳基。

9. 发明申请

WO1994026708A1 OPTICALLY ACTIVE 3-(1-(ALKYLAMINO))ALKYL PYRROLIDINES 审中-公开
标题翻译：光学活性3-（1-（亚氨基））烷基吡咯烷酮
公开(公告)号：WO1994026708A1
公开(公告)日：1994-11-24
申请号：PCT/US1994004548
申请日：1994-05-03
申请人： THE UPJOHN COMPANY , MCWHORTER, William, W. , FLECK, Thomas, J. , PEARLMAN, Bruce, A.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D207/09
CPC分类号： C07D207/26 , C07D207/09
摘要： This invention relates to processes for the synthesis of various optically active amino pyrrolidinyl stereoisomers, or enantiomers, that may be attached to quinolonecarboxylic acids or naphthyridones. Processes and essential intermediates are disclosed and claimed for the synthesis of compounds represented by the structure shown in figure BG4-1, where R , R and R are defined independently and are H, --(C1-C8)alkyl, --(C3-C8)cycloalkyl, --(C1-C8)alkyl-(C3-C8)cycloalkyl, --(C6-C12 aryl), --(C1-C8)alkyl-(C6-C12 aryl), or the aryl or alkyl is substituted with one to three of the following groups, (C6-C12 aryl), (C1-C3)alkyl, (C1-C3)alkoxy, halogen, trifluoromethyl; where R is --(C1-C8)alkyl, --(C3-C8)cycloalkyl, --(C1-C8)alkyl-(C3-C8)cycloalkyl, --(C6-C12 aryl), --(C1-C8)alkyl-(C6-C12 aryl), or the aryl or alkyl is substituted with one to three of the following groups, --(C6-C12 aryl), --(C1-C3)alkyl, --(C1-C3)alkoxy, halogen, trifluoromethyl; depending upon the starting materials used, compounds represented by the structure shown by figure BG4-1 may have one of either of the two stereochemical arrangements shown, or, if the starting materials are a racemic mixture, the reaction may produce a 1:1 ratio of the combination of products shown in figure BG4-1, i.e. a racemic mixture.
摘要翻译：本发明涉及可以连接到喹诺酮羧酸或萘啶酮的各种光学活性氨基吡咯烷基立体异构体或对映异构体的合成方法。公开和要求用于合成由图BG4-1所示结构表示的化合物的方法和必需中间体，其中R 50，R 6和R 9独立地定义并且是H， - （C 1 （C 1 -C 8）烷基 - （C 1 -C 8）烷基 - （C 1 -C 8）烷基 - （C 3 -C 8） -C 12芳基），或芳基或烷基被一至三个下列基团取代：（C 6 -C 12芳基），（C 1 -C 3）烷基，（C 1 -C 3）烷氧基，卤素，三氟甲基; 其中R 2为 - （C 1 -C 8）烷基， - （C 3 -C 8）环烷基， - （C 1 -C 8）烷基 - （C 3 -C 8）环烷基， - （C 6 -C 12芳基） - （C 1 -C 8）烷基 - （C 6 -C 12芳基），或芳基或烷基被一至三个下列基团取代： - （C 6 -C 12芳基）， - （C 1 -C 3） - （C 1 -C 3）烷氧基，卤素，三氟甲基; 取决于所使用的起始材料，由图BG4-1所示结构表示的化合物可以具有所示的两种立体化学排列中的一种，或者如果原料是外消旋混合物，则反应可以产生1:1的比例图BG4-1所示产品的组合，即外消旋混合物。

10. 发明申请

WO1994022836A2 PIPERAZINYLPYRIDINYL WATER CLATHRATES 审中-公开
标题翻译：哌嗪类黄酮水合物
公开(公告)号：WO1994022836A2
公开(公告)日：1994-10-13
申请号：PCT/US1994002548
申请日：1994-03-15
申请人： THE UPJOHN COMPANY , PEARLMAN, Bruce, Allen , KROOK, Mark, A. , PERRAULT, William, R. , DOBROWOLSKI, Paul, J.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D213/74
CPC分类号： C07D213/74
摘要： The invention is a process to produce 3-alkylamino-2-piperazinylpyridines (III), where R3 is -CH2-CH3 or -CH(CH3)2, a process to purify them and their water clathrates. The 3-alkylamino-2-piperazinylpyridines (III) are used in the production of known compounds useful for treating individuals who are HIV positive.
摘要翻译：本发明是制备3-烷基氨基-2-哌嗪基吡啶（III）的方法，其中R3是-CH2-CH3或-CH（CH3）2，一种纯化它们和它们的水包合物的方法。 3-烷基氨基-2-哌嗪基吡啶（III）用于生产用于治疗HIV阳性个体的已知化合物。

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