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1. 发明专利

CA1281720C CARBAPENEM COMPOUNDS AND PRODUCTION THEREOF 未知
公开(公告)号：CA1281720C
公开(公告)日：1991-03-19
申请号：CA494815
申请日：1985-11-07
申请人： SUNAGAWA MAKOTO , MATSUMURA HARUKI , INOUE TAKAAKI , FUKASAWA MASATOMO , KATO MASUHIRO
发明人： SUNAGAWA MAKOTO , MATSUMURA HARUKI , INOUE TAKAAKI , FUKASAWA MASATOMO , KATO MASUHIRO
IPC分类号： C07D207/12 , C07D207/16 , C07D403/06 , C07D477/20 , C07F7/18 , C07D487/04 , C07F7/10 , A61K31/40
摘要： The present invention is directed to compounds of the formula: wherein R1 is a hydrogen atom or a lower alkyl group, R2 is a hydrogen atom or a conventional protecting group for a carboxyl group, R0 is a hydrogen atom or a conventional protecting group for a hydroxyl group, X is a protected or unprotected amino group, a carboxyl group, a lower alkoxycarbonyl group, an ar(lower)alkyloxycarbonyl group, a cyano group, a hydroxyl group, a lower alkyloxy group, a lower alkylthio group, a lower alkylsulfonyl group or a group of either one of the following formulas: (1) wherein R3 and R4, which may be the same or different, each represents a hydrogen atom or a lower alkyl group, or they are taken together to represent an alkylene chain to form, in combination with the adjacent nitrogen atom, a 3- to 7-membered cyclic amino group, (2) -ZCOR5 wherein Z represents -NH- or -O- and R5 represents an amino group, a mono(lower)alkylamino group, a di(lower)alkylamino group, a lower alkyloxy group or a lower alkyl group, (3) wherein R6 represents a hydrogen atom or a lower alkyl group, (4) -CH=N-R7 wherein R7 represents a mono(lower)alkylamino group, a di (lower)alkylamino group or a lower alkyloxy group, or (5) wherein R8, R9 and R10, which may be the same or different, each represents a hydrogen atom or a lower alkyl group, Y represents a hydrogen atom, a conventional protecting group for an amino group or a group of either one of the following formulas: (6) wherein R11 and R12, which may be the same or different, each represents a hydrogen atom or a lower alkyl group or (7) wherein R6 is as defined above and n is an integer of 1 to 6, and pharmacologically acceptable salts thereof. The compounds of the present invention are useful as antimicrobial agents.

2. 发明申请

WO1998009965A1 NOVEL 'beta'-LACTAM COMPOUNDS AND PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：新型β--LACTAM化合物及其制备方法
公开(公告)号：WO1998009965A1
公开(公告)日：1998-03-12
申请号：PCT/JP1997003078
申请日：1997-09-03
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED , SUNAGAWA, Makoto , YAMAGA, Hiroshi , NOUDA, Hiroshi , SHINAGAWA, Hisatoshi
发明人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
IPC分类号： C07D487/04
CPC分类号： C07D477/20
摘要： beta -Lactam compounds represented by general formula (1) and salts and esters thereof, wherein R represents a lower alkyl or an OH-substituted lower alkyl; R represents H or a lower alkyl; X represents O, S, or NH; n is 1 to 3; and R represents -C(Ra)=NH (wherein Ra represents H, a lower alkyl, or a substituted lower alkyl). The above compounds have an excellent antimicrobial activity against Gram-positive bacteria, particularly meticillin-resistant staphylococci and meticillin-resistant and coagulase-negative staphylococci.
摘要翻译：由通式（1）表示的β-内酰胺化合物及其盐和酯，其中R 1表示低级烷基或OH-取代的低级烷基; R 2表示H或低级烷基; X表示O，S或NH; n为1〜3; 并且R 3表示-C（R a）= NH（其中R a表示H，低级烷基或取代的低级烷基）。上述化合物对革兰氏阳性菌，特别是耐甲氧西林葡萄球菌和耐甲氧西林和凝固酶阴性葡萄球菌具有优异的抗菌活性。

3. 发明申请

WO1996031488A1 NOVEL PYRIMIDINE DERIVATIVES EFFICACIOUS AS PSYCHOTROPIC DRUG AND PROCESS FOR THE PRODUCTION THEREOF 审中-公开
标题翻译：新型吡咯烷酮衍生物作为心血管药物有效，其生产方法
公开(公告)号：WO1996031488A1
公开(公告)日：1996-10-10
申请号：PCT/JP1996000895
申请日：1996-04-02
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED , IGARASHI, Jun-etsu , NISHIMURA, Tamiki , SUNAGAWA, Makoto
发明人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
IPC分类号： C07D239/47
CPC分类号： C07D239/47 , C07D239/38 , C07D239/48 , C07D401/12
摘要： Compound represented by general formula (I) or pharmacologically acceptable salts thereof: wherein A represents halogeno, optionally substituted lower alkyl or optionally substituted cycloalkyl; B and B are the same or different and each represents hydrogen or optionally substituted amino; X represents sulfur or oxygen; and Y , Y , Y , Y and Y are the same or different and each represents hydrogen, halogeno, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted aryl or optionally substituted heterocycle. The compounds have a potent interaction with central nervous system receptors such as dopamine or serotonin and are excellent in absorbability in vivo, stability, etc. Thus they are highly useful as a psychotropic drug with relieved side effects.
摘要翻译：由通式（I）表示的化合物或其药理学上可接受的盐：其中A 1表示卤代，任选取代的低级烷基或任选取代的环烷基; B 1和B 2相同或不同，各自表示氢或任选取代的氨基; X表示硫或氧; Y 1，Y 2，Y 3，Y 4和Y 5相同或不同，各自代表氢，卤代，任选取代的低级烷基，任选取代的环烷基，任选取代的低级烯基，任选取代的低级炔基，任选取代的芳基或任选取代的杂环。这些化合物与中枢神经系统受体如多巴胺或5-羟色胺具有强烈的相互作用，并且在体内的吸收性，稳定性等方面优异。因此，它们作为具有减轻副作用的精神药物是非常有用的。

4. 发明申请

WO1994029313A1 NOVEL beta-LACTAM COMPOUND AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：新型β--LACTAM化合物及其生产方法
公开(公告)号：WO1994029313A1
公开(公告)日：1994-12-22
申请号：PCT/JP1994000958
申请日：1994-06-14
申请人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED , SUNAGAWA, Makoto , YAMAGA, Hiroshi , SUMITA, Yoshihiro
发明人： SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
IPC分类号： C07D477/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D477/20
摘要： A novel beta -lactam compound represented by general formula [1] and having an excellent antibacterial activity against gram-positive bacteria, in particular, methicillin-resistant staphylococci and methicillin-resistant coagulase-negative staphylococci, a pharmaceutically acceptable salt thereof, and a process for producing the same, wherein R represents lower alkyl which may be hydroxylated; R represents hydrogen or lower alkyl; X represents oxygen, sulfur or NH; Y represents nitrogen or carbon, provided n is 0 when Y represents nitrogen and n is 1 when Y represents carbon; and Z represents (each independently when n is 1) hydrogen, R (lower alkyl, etc.), A (aryl, etc.), -OH, -OR , -OA, -SR , -SA, -NH2, -NHR , -NR R (R and R being each lower alkyl, etc.), -NHA, -NR A, -CONH2, -CONHR , -CONR R , -CONHA, -CONR A, -CONHC(NH)NH2, -COOH, -COOR , -COOA, -COR , -COA, halogen, or cyano.
摘要翻译：由通式[1]表示的新颖的β-内酰胺化合物，对革兰氏阳性细菌，特别是耐甲氧西林葡萄球菌和耐甲氧西林凝固酶阴性葡萄球菌，其药学上可接受的盐具有优异的抗菌活性，制备其中R 1表示可被羟基化的低级烷基; R 2表示氢或低级烷基; X表示氧，硫或NH; Y表示氮或碳，当Y表示氮时n为0，当Y表示碳时n为1; 并且Z代表（当n为1时各自独立地为氢），R a（低级烷基等），A（芳基等），-OH，-OR a，-OA，-SR a ，-SA，-NH 2，-NHR a，-NR R c（R b和R c各自为低级烷基等），-NHA，-NR a A ，-CONH 2，-CONHR a，-CONR b，R a，-CONHA，-CONR a，-CONHC（NH）NH 2，-COOH，-COOR a，-COOA， - COR a，-COA，卤素或氰基。

5. 发明申请

US20100210855A1 SULFONIC ACID SALT COMPOUND OF 4-CARBAMOYL-5-HYDROXY-IMIDAZOLE DERIVATIVE 有权
标题翻译： 4-卡巴酸-5-羟基咪唑衍生物的磺酸盐化合物
公开(公告)号：US20100210855A1
公开(公告)日：2010-08-19
申请号：US12733656
申请日：2008-09-16
申请人： Kato Nobuo , Higuchi Yusuke , Kondo Chihiro , Sunagawa Makoto
发明人： Kato Nobuo , Higuchi Yusuke , Kondo Chihiro , Sunagawa Makoto
IPC分类号： C07D233/38
CPC分类号： C07D233/90
摘要： The object is to provide a stable SM-108 derivative, which is effective as a carcinostatic agent, particularly an SM-108 derivative having good storage stability. An SM-108 compound having good storage stability can be produced by producing an organic sulfonic acid salt compound of SM-108. Further, a crystalline SM-108 compound containing a trace amount of an organic carboxylic acid can be produced by using an aqueous solution of the organic sulfonic acid salt of SM-108, and by adding an alkali metal salt of an organic carboxylic acid to the aqueous solution to neutralize the aqueous solution and then causing the crystal precipitation in the solution.
摘要翻译：目的是提供一种稳定的SM-108衍生物，其作为制癌剂，特别是具有良好储存稳定性的SM-108衍生物是有效的。通过制备SM-108的有机磺酸盐化合物可以制备具有良好储存稳定性的SM-108化合物。此外，通过使用SM-108的有机磺酸盐的水溶液，并且通过将有机羧酸的碱金属盐加入到所述有机羧酸的碱金属盐中，可以制备含有微量有机羧酸的结晶SM-108化合物水溶液中和水溶液，然后使溶液中的晶体析出。

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