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1. 发明申请

WO1993023384A1 OXAZOLIDINONES CONTAINING A SUBSTITUTED DIAZINE MOIETY AND THEIR USE AS ANTIMICROBIALS 审中-公开
标题翻译：含有取代的DIAZINE MOIETY的OXAZOLIDONON及其作为抗微生物剂的用途
公开(公告)号：WO1993023384A1
公开(公告)日：1993-11-25
申请号：PCT/US1993003570
申请日：1993-04-21
申请人： THE UPJOHN COMPANY , HUTCHINSON, Douglas, K. , BRICKNER, Steven, Joseph , BARBACHYN, Michael, Robert , GAMMILL, Ronald, B. , PATEL, Mahest, V.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D263/20
CPC分类号： C07D263/20 , C07D413/10 , C07D413/12
摘要： A compound of structural formula (I) or pharmaceutically acceptable salts thereof wherein: Y is chosen from a-n as defined herein; wherein each occurrence of said C1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR , CO2R , CN, SR , or R (where R is a hydrogen or C1-4 alkyl); X and Z are independently C1-6 alkyl, C3-12 cycloalkyl or hydrogen, or X and Z form a C0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C1-6 alkyl, F, Cl, Br, hydrogen or a C1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C1-12 alkyl, C3-12 cycloalkyl, C1-6 alkoxy, C1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.
摘要翻译：结构式（I）的化合物或其药学上可接受的盐，其中：Y选自如本文所定义的a-n; 其中所述C 1-6烷基的每次出现可以被一个或多个F，Cl，Br，I，OR 1，CO 2 R 1，CN，SR 1或R 1取代（其中R 1， 1是氢或C 1-4烷基）; X和Z独立地是C 1-6烷基，C 3-12环烷基或氢，或X和Z形成C0-3桥连基，优选X和Z是氢; U，V和W独立地是C 1-6烷基，F，Cl，Br，氢或被F，Cl，Br或I中的一个或多个取代的C 1-6烷基，优选U和V是F，W是氢; R是氢，C 1-12烷基，C 3-12环烷基，C 1-6烷氧基，被一个或多个F，Cl，Br，I或OH取代的C 1-6烷基; q为0〜4。具有与N-芳基环结合的取代的二嗪部分的恶唑烷酮衍生物是有效的抗微生物剂，其对许多人类和兽医病原体有效，包括多重耐药性葡萄球菌和链球菌，以及厌氧生物体如杀菌剂和梭菌属物种，以及耐酸生物如结核分枝杆菌和鸟分枝杆菌。

2. 发明申请

WO1993009103A1 SUBSTITUTED ARYL- AND HETEROARYLPHENYLOXAZOLIDINONES USEFUL AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：用作抗菌剂的取代的芳基和异环戊二烯并咪唑啉酮
公开(公告)号：WO1993009103A1
公开(公告)日：1993-05-13
申请号：PCT/US1992008267
申请日：1992-10-05
申请人： THE UPJOHN COMPANY , BARBACHYN, Michael, Robert , BRICKNER, Steven, Joseph
发明人： THE UPJOHN COMPANY
IPC分类号： C07D263/20
CPC分类号： C07D263/20 , C07D413/10
摘要： The present invention discloses novel substituted aryl- and heteroarylphenyloxazolidinones which are useful as antibacterial agents. More specifically, the substituted aryl- and heteroarylphenyloxazolidinones of the invention are characterized by oxazolidinones having an aryl or heteroaryl group at the p-position of the 3-phenyl ring and additional substitutions at the m-position(s) of the 3-phenyl ring. A compound representative of this new class of oxazolidinones is (+/-)-5-(acetamidomethyl)-3-[4-(3-pyridyl)-3,5-difluorophenyl]-2-oxazo lidinone.
摘要翻译：本发明公开了可用作抗菌剂的新型取代的芳基 - 和杂芳基苯基恶唑烷酮。更具体地，本发明的取代的芳基 - 和杂芳基苯基恶唑烷酮的特征在于在3-苯基环的对位具有芳基或杂芳基的恶唑烷酮和在3-苯基环的m位的另外的取代。代表这种新一类恶唑烷酮的化合物是（+/-） - 5-（乙酰氨基甲基）-3- [4-（3-吡啶基）-3,5-二氟苯基] -2-恶唑烷酮。

3. 发明申请

WO1994001110A1 5'-INDOLINYL OXAZOLIDINONES USEFUL AGAINST MYCOBACTERIUM TUBERCULOSIS 审中-公开
标题翻译： 5-INDOLINYL OXAZOLIDINONESES有效应对MYCOBACTERIUM TUBERCULOSIS
公开(公告)号：WO1994001110A1
公开(公告)日：1994-01-20
申请号：PCT/US1993004850
申请日：1993-05-26
申请人： THE UPJOHN COMPANY , BRICKNER, Steven, Joseph , ZURENKO, Gary, Edward
发明人： THE UPJOHN COMPANY
IPC分类号： A61K31/42
CPC分类号： A61K31/42
摘要： 5-(S)-N-(1'-Hydroxyacetyl-5'-indolinyl)-5-(acetamidomethyl)-2-oxazolid inone and 5-(S)-N-(1'-(2-thiophenecarbonyl)-5'-indolinyl)-5-(acetamidomethyl)-2- oxazolidinone are useful in treating tuberculosis caused by M. Tuberculosis.
摘要翻译： 5-（S）-N-（1'-羟基乙酰基-5'-二氢吲哚基）-5-（乙酰胺基甲基）-2-恶唑烷酮和5-（S）-N-（1' - （2-噻吩羰基）-5 ' - 吲哚啉基）-5-（乙酰氨基甲基）-2-恶唑烷酮可用于治疗由结核分枝杆菌引起的结核病。

4. 发明申请

WO1991007409A1 TRICYCLIC [6,5,5]/[6,6,5]-FUSED OXAZOLIDINONE ANTIBACTERIAL AGENTS 审中-公开
标题翻译： TRICYCLIC [6,5,5] / [6,6,5] - 氟氧化物抗菌剂
公开(公告)号：WO1991007409A1
公开(公告)日：1991-05-30
申请号：PCT/US1990006220
申请日：1990-11-02
申请人： THE UPJOHN COMPANY , BRICKNER, Steven, Joseph
发明人： THE UPJOHN COMPANY
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： The present invention involves tricyclic-fused 6-member ring oxazolidinones (6-A) and (6-B) and tricyclic-fused 5-member ring oxazolidinones (5) which are useful as antibacterial agents.
摘要翻译：本发明涉及可用作抗菌剂的三环稠合的6-元环恶唑烷酮（6-A）和（6-B）和三环稠合的5-元环恶唑烷酮（5）。

5. 发明申请

WO1994013649A1 TROPONE-SUBSTITUTED PHENYLOXAZOLIDINONE ANTIBACTERIAL AGENTS 审中-公开
标题翻译： TROPONE-取代的苯基吖唑烷酮抗菌剂
公开(公告)号：WO1994013649A1
公开(公告)日：1994-06-23
申请号：PCT/US1993009589
申请日：1993-10-14
申请人： THE UPJOHN COMPANY , BARBACHYN, Michael, Robert
发明人： THE UPJOHN COMPANY
IPC分类号： C07D263/20
CPC分类号： C07D263/20
摘要： A novel class of phenyloxazolidinone antibacterial agents which have, as their salient structural feature, an appended substituted tropone moiety, are described. Intermediates and processes for the preparation of these antibiotics are also disclosed. These compounds are useful antibacterial agents to eradicate or control suceptible organisms. In formula (I), R , R and R are the same as in claim 1 and R is selected from the group consisting of (a), (b), (c) and (d), wherein R and Ra are the same or different and are selected from the group consisting of (C1-C8) alkyl optionally substituted with chloro, fluoro, hydroxy, (C1-C8) alkoxy, amino, (C1-C8) alkylamino, (C1-C8) dialkylamino.
摘要翻译：描述了一类新的苯基恶唑烷酮抗菌剂，它们的显着结构特征是附加的取代的环丙烯酮部分。还公开了制备这些抗生素的中间体和方法。这些化合物是消除或控制易感生物体的有用的抗菌剂。在式（I）中，R 1，R 2和R 3与权利要求1中相同，R 4选自（a），（b），（c）和（d），其中R和R a相同或不同，并且选自任选被氯，氟，羟基，（C 1 -C 8）烷氧基，氨基，（C 1 -C 8））烷基氨基，（C1-C8）二烷基氨基。

6. 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）。

7. 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。

8. 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。

9. 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。

10. 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）。

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