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1. 发明申请

WO1996015130A1 BICYCLIC OXAZINE AND THIAZINE OXAZOLIDINONE ANTIBACTERIALS 审中-公开
标题翻译：双氧化合物和噻唑烷氧基苯胺类抗生素
公开(公告)号：WO1996015130A1
公开(公告)日：1996-05-23
申请号：PCT/US1995012751
申请日：1995-10-31
申请人： THE UPJOHN COMPANY , BARBACHYN, Michael, R. , THOMAS, Richard, C. , CLEEK, Gary, J. , THOMASCO, Lisa, Marie , GADWOOD, Robert, C.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D491/048
CPC分类号： C07D491/04 , C07D491/08 , C07D495/04 , C07D495/08
摘要： Phenyloxazolidinone compounds of formula (I) or a pharmaceutically acceptable salt thereof characterized by a bicyclic thiazine or oxazine substituent. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
摘要翻译：式（I）的苯基恶唑烷酮化合物或其药学上可接受的盐，其特征在于双环噻嗪或恶嗪取代基。这些化合物是有用的抗微生物剂，对许多人类和兽医病原体有效，包括革兰氏阳性好氧细菌，如多重耐药葡萄球菌，链球菌和肠球菌，以及厌氧生物体如拟杆菌属。和梭菌属（Clostridia spp。）物种和耐酸生物如结核分枝杆菌，鸟分枝杆菌和分枝杆菌属。

2. 发明申请

WO1995013267A1 PYRIMIDINE-THIOALKYL AND ALKYLETHER COMPOUNDS 审中-公开
标题翻译：哌嗪 - 噻二醇和烷基化合物
公开(公告)号：WO1995013267A1
公开(公告)日：1995-05-18
申请号：PCT/US1994012713
申请日：1994-11-09
申请人： THE UPJOHN COMPANY , NUGENT, Richard, A. , SCHLACHTER, Stephen, T. , MURPHY, Michael, J. , MORRIS, Joel , THOMAS, Richard, C. , WISHKA, Donn, G. , REUSSER, Fritz , CLEEK, Gary, J. , ALTHAUS, Irene, Wilson
发明人： THE UPJOHN COMPANY
IPC分类号： C07D239/46
CPC分类号： C07D239/47 , A61K31/505 , C07D239/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R4 is selected from the group consisting of -H or -NR15R16 where R15 is -H and R16 is -H, C1-C6 alkyl, -NH2 or R15 and R16 taken together with the -N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R6 is selected from the group consisting of -H, or halo (preferably -Cl); with the overall proviso that R4 and R6 are not both -H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive.
摘要翻译：本发明涉及式（I）的嘧啶 - 硫代烷基和烷基醚化合物和式（IA）的嘧啶 - 硫代烷基和烷基醚，即式（I）的化合物，其中R 4选自-H或-NR 15 R 16 其中R 15为-H且R 16为-H，C 1 -C 6烷基，-NH 2或R 15和R 16与-N形式的1-吡咯烷子基，1-吗啉代或1-哌啶子基一起使用; 并且R 6选自-H或卤素（优选-Cl）; 其总体条件是R4和R6不是-H。式（IA）的化合物可用于治疗HIV阳性的个体。

3. 发明申请

WO1988006588A1 ANTIBIOTIC SULFONYLAMINOCARBONYL ACTIVATED 'beta'-LACTAMS 审中-公开
标题翻译：抗生素磺酰氨基胆碱激活（BETA）-LACTAMS
公开(公告)号：WO1988006588A1
公开(公告)日：1988-09-07
申请号：PCT/US1988000404
申请日：1988-02-19
申请人： THE UPJOHN COMPANY , BARBACHYN, Michael, R. , BRICKNER, Steven, J. , THOMAS, Richard, C.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D417/14
CPC分类号： C07D417/14
摘要： This invention presents novel 2-azetidinone compounds which are useful as antibacterial agents to eradicate or control susceptible microbes of formula (I), wherein R401 and R402 are the same or different and are a) hydrogen, b) (C1-C12) alkyl c) (C2-C8) alkenyl, d) (C2-C8) alkynyl, e) (C3-C10) cycloalkyl, f) phenyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro, (C1-C4) alkyl, and (C1-C4) alkoxy, g) benzyl optionally substituted with from one to 3 substituents selected from the group consisting of halogen, hydroxy, amino, nitro (C1-C4) alkyl, and (C1-C4) alkoxy, h) -CH2-O-CO-CH2-NHR420, i) -CH2-O-CO2-R430, j) -CH2F, or k) -CHF2; wherein R420 is a) hydrogen, b) -COH, or c) -CO-O-C(CH3)3; wherein R430 is (C1-C8) alkyl, -(CH2)2OC(O)NH2, -(CH2)2Cl, -(CH2)2OCH3 or -(CH2)2NHCOH; wherein R300 is an acyl group derived from a carboxylic acid; wherein R100 is an optionally substituted heterocyclic moiety.

4. 发明申请

WO1993005045A1 SPIROCYCLIC BENZOPYRAN IMIDAZOLINES 审中-公开
标题翻译：螺环苯并咪唑咪唑啉
公开(公告)号：WO1993005045A1
公开(公告)日：1993-03-18
申请号：PCT/US1992006291
申请日：1992-08-03
申请人： THE UPJOHN COMPANY , GADWOOD, Robert, C.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D491/107
CPC分类号： C07D491/10
摘要： Spiro-[4H-1-benzopyran-4,4'-5'H-imidazol]-5'-ones of Formula (1), wherein R is H, R , F, Cl, Br, CF3, CF3O, CN, NO2, R SO2, R NHSO2, R O, R CO, R OCO, or R NHCO. R is a C1-C10 branched or linear alkyl, a C3-8 cycloalkyl, phenyl, or benzyl. X can be S, O, or NH. Both enantiomers are included in this invention as well as salts and tautomeric forms of these compounds. The subject compounds are useful in the treatment of hypertension, alopecia, and erectile dysfunction.
摘要翻译：式（1）的螺 - [4H-1-苯并吡喃-4,4'- 5'H-咪唑] -5'-酮，其中R 1是H，R 2，F，Cl，Br， CF 3，CF 3 O，CN，NO 2，R 2 SO 2，R 2 NHSO 2，R 2 O，R 2 CO，R 2 OCO或R 2 NHCO。 R 2是C 1 -C 10支链或直链烷基，C 3-8环烷基，苯基或苄基。 X可以是S，O或NH。这两种对映异构体都包括在本发明中，以及这些化合物的盐和互变异构形式。主题化合物可用于治疗高血压，脱发和勃起功能障碍。

5. 发明申请

WO1988006156A1 NOVEL N-1 SUBSTITUTED 'beta'-LACTAMS AS ANTIBIOTICS 审中-公开
标题翻译：新型N-1替代β-RATA作为抗生素
公开(公告)号：WO1988006156A1
公开(公告)日：1988-08-25
申请号：PCT/US1988000049
申请日：1988-01-15
申请人： THE UPJOHN COMPANY , BARBACHYN, Michael, R.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D417/14
CPC分类号： C07D417/14
摘要： Novel 2-azetidinone compounds of formula (I), wherein R10 and R15 are the same or different and are a) hydrogen, b) (C1-C12) alkyl, c) (C2-C8) alkenyl, d) (C2-C8) alkynyl, e) -CH2OCO-CH2NHR4, f) -CH2OCO2R30, g) -CH2F, or h) -CHF2; wherein R4 is hydrogen or -COH; wherein R30 is (C1-C8) alkyl; wherein R20 is an acyl group derived from a carboxylic acid; wherein A is oxygen or sulfur; and wherein R70 is a) hydrogen, b) (C1-C8) alkyl, c) phenyl, d) -OH, or e) -SH; where each member of b or c may optionally be substituted by 1 to 2 substituents selected from the group consisting of halogen, hydroxy, and amino. These compounds are useful as antibacterial agents to eradicate or control susceptible microbes. Intermediates and processes for making these compounds are also disclosed.
摘要翻译：式（I）的新型2-氮杂环丁酮化合物，其中R 10和R 15相同或不同且为a）氢，b）（C 1 -C 12）烷基，c）（C 2 -C 8）烯基，d）（C 2 -C 8 ）炔基，e）-CH2OCO-CH2NHR4，f）-CH2OCO2R30，g）-CH2F或h）-CHF2; 其中R4是氢或-COH; 其中R30为（C1-C8）烷基; 其中R 20是衍生自羧酸的酰基; 其中A是氧或硫; 并且其中R 70是a）氢，b）（C 1 -C 8）烷基，c）苯基，d）-OH或e）-SH; 其中b或c的每个成员可以任选被1至2个选自卤素，羟基和氨基的取代基取代。这些化合物可用作消除或控制易感微生物的抗菌剂。还公开了制备这些化合物的中间体和方法。

6. 发明申请

WO1996013502A1 PHENYLOXAZOLIDINONE ANTIMICROBIALS 审中-公开
标题翻译：苯并噻唑酮类抗生素
公开(公告)号：WO1996013502A1
公开(公告)日：1996-05-09
申请号：PCT/US1995010992
申请日：1995-09-12
申请人： THE UPJOHN COMPANY , HUTCHINSON, Douglas, K. , BARBACHYN, Michael, R. , TANIGUCHI, Mikio , MUNESADA, Kiyotaka , YAMADA, Hiroyoshi , BRICKNER, Steven, J.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D413/10
CPC分类号： C07D413/10
摘要： A compound of structural formula (I), or pharmaceutically acceptable salts thereof wherein: Q is selected from the structures i, ii, iii, iv and v. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, particularly aerobic gram-positive bacteria, including multiply-resistant staphylococci, enterococci and streptococci, as well as anaerobic organisms such as bacteroids and clostridia species, and acid-fast bacteria such as as Mycobacterium tuberculosis and other mycobacterial species.
摘要翻译：结构式（I）的化合物或其药学上可接受的盐，其中：Q选自结构i，ii，iii，iv和v。化合物是有效的抗微生物剂，对许多人和兽医病原体有效，特别是需氧革兰氏阳性菌，包括多重耐药性葡萄球菌，肠球菌和链球菌，以及厌氧生物体如细菌和梭菌，以及耐酸细菌如结核分枝杆菌和其他分枝杆菌菌种。

7. 发明申请

WO1995007271A1 SUBSTITUTED OXAZINE AND THIAZINE OXAZOLIDINONE ANTIMICROBIALS 审中-公开
标题翻译：取代氧化氮和噻唑啉酮类抗生素
公开(公告)号：WO1995007271A1
公开(公告)日：1995-03-16
申请号：PCT/US1994008904
申请日：1994-08-16
申请人： THE UPJOHN COMPANY , BARBACHYN, Michael, R. , BRICKNER, Steven, J. , HUTCHINSON, Douglas, K.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D263/20
CPC分类号： C07D263/20 , C07D413/10 , C07D417/10
摘要： A compound of structural formula (I) or pharmaceutically acceptable salts thereof wherein: X is O, S, SO, SO2, SNR or S(O)NR ; R is (a) hydrogen, (b) C1-C8 alkyl optionally substituted with one or more of the following: F, Cl, hydroxy, C1-C8alkoxy, C1-C8acyloxy or -O-CH2-Ph, (c) C3-C6cycloalkyl, (d) amino, (e) C1-C8alkylamino, (f) C1-C8dialkylamino or (g) C1-C8alkoxy; R is H, except when X is O, then R can be H, CH3, CN, CO2H, CO2R or (CH2)mR (m is 1 or 2); R is independently H, F or Cl; R is H except when X is O and R is CH3, then R can be H or CH3; R is independently H, C1-C4alkyl (optionally substituted with chloro, fluoro, hydroxy, C1-C8alkoxy, amino, C1-C8alkylamino, or C1-C8dialkylamino) or p-toluenesulfonyl; R is hydrogen, OH, OR, OCOR, NH2, NHCOR or N(R )2; and n is 0, 1 or 2. The oxazine and thiazine oxazolidinone derivatives are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp..
摘要翻译：结构式（I）的化合物或其药学上可接受的盐，其中：X是O，S，SO，SO 2，SNR 10或S（O）NR 10; R为（a）氢，（b）任选被一个或多个以下的取代基取代的C 1 -C 8烷基：F，Cl，羟基，C 1 -C 8烷氧基，C 1 -C 8酰氧基或-O-CH 2 Ph，（c）（d）氨基，（e）C 1 -C 8烷基氨基，（f）C 1 -C 8二烷基氨基或（g）C 1 -C 8烷氧基; R 1是H，除了当X是O时，R 1可以是H，CH 3，CN，CO 2 H，CO 2 R或（CH 2）m R 11（m是1或2）; R 2独立地为H，F或Cl; R 3为H，但当X为O且R 1为CH 3时，R 3为H或CH 3; R 10独立地是H，C 1 -C 4烷基（任选被氯，氟，羟基，C 1 -C 8烷氧基，氨基，C 1 -C 8烷基氨基或C 1 -C 8二烷基氨基取代）或对甲苯磺酰基; R 11是氢，OH，OR，OCOR，NH 2，NHCOR或N（R 10）2; 并且n为0,1或2.恶嗪和噻嗪恶唑烷酮衍生物是有用的抗微生物剂，对许多人和兽医病原体有效，包括革兰氏阳性好氧细菌如耐多重耐药性葡萄球菌，链球菌和肠球菌以及厌氧生物体如拟杆菌属（Bacteroides spp。）和梭菌属（Clostridia spp。）物种和耐酸生物如结核分枝杆菌，鸟分枝杆菌和分枝杆菌属。

8. 发明申请

WO1990006307A2 ANTIBACTERIAL QUINOLONE COMPOUNDS 审中-公开
标题翻译：抗生素喹诺酮类化合物
公开(公告)号：WO1990006307A2
公开(公告)日：1990-06-14
申请号：PCT/US1989005213
申请日：1989-11-24
申请人： THE UPJOHN COMPANY , GAMMILL, Ronald, B. , BISAHA, Sharon, N. , TIMKO, Joseph, M. , JUDGE, Thomas, M. , BARBACHYN, Michael, R. , KIM, Kyoung, S.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D401/04
CPC分类号： C07D215/56 , C07D401/04 , C07D471/04
摘要： A quinolone compound of formula (I) as defined herein having antibacteria properties, pharmaceutical compositions containing the quinoline compound and method for treating bacterial infections in animals including humans.
摘要翻译：本文定义的具有抗菌特性的式（I）的喹诺酮化合物，含有喹啉化合物的药物组合物和用于治疗包括人在内的动物的细菌感染的方法。

9. 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）。

10. 发明申请

WO1986005686A2 TREATING CHLAMYDIA INFECTIONS USING SPECTINOMYCIN ANALOGS 审中-公开
标题翻译：治疗CHLAMYDIA感染使用色谱线模拟
公开(公告)号：WO1986005686A2
公开(公告)日：1986-10-09
申请号：PCT/US1986000620
申请日：1986-03-26
申请人： THE UPJOHN COMPANY , ZURENKO, Gary, E. , VAVRA, James, J. , WHITE, David, R. , THOMAS, Richard, C.
发明人： THE UPJOHN COMPANY
IPC分类号： A61K31/70
CPC分类号： C07H15/224

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