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11. 发明授权

US4008220A Penicillins 失效
标题翻译：青霉素
公开(公告)号：US4008220A
公开(公告)日：1977-02-15
申请号：US495914
申请日：1974-08-08
申请人： Hisao Tobiki , Hirotada Yamada , Iwao Nakatsuka , Kozo Shimago , Shigeru Okano , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Hiroshi Noguchi , Yasuko Eda
发明人： Hisao Tobiki , Hirotada Yamada , Iwao Nakatsuka , Kozo Shimago , Shigeru Okano , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Hiroshi Noguchi , Yasuko Eda
IPC分类号： C07D499/00 , C07D499/68 , C07D499/48
CPC分类号： C07D499/00 , Y02P20/55
摘要： A penicillin of the formula: ##STR1## wherein ##STR2## is a six-membered heteroaromatic ring containing 1 or 2 nitrogen atoms as the hetero atom, Y is hydrogen, lower alkanoyl or lower alkoxycarbonyl, R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkanoyl, benzoyl, lower alkylmercapto, hydroxyl, mercapto, hydroxy(lower)alkyl, halogen or cyano or R.sub.1 and R.sub.2 may link together to form a lower alkylene chain which may be substituted with an oxo group, and Z is phenyl, hydroxyphenyl, lower alkyl, cyclohexadienyl, thienyl or isothiazolyl, which is prepared by reacting a compound of the formula: ##STR3## wherein Z is as defined above or its derivative with a carboxylic acid of the formula: ##STR4## wherein ##STR5## and R.sub.2 are each as defined above or its reactive derivative, if necessary, followed by hydrolysis or acylation of the resulting product and/or elimination of any protective group and which is useful as an antimicrobial agent against various gram-positive and gram-negative bacteria including Pseudomonas.
摘要翻译：一种下式的青霉素：其中是含有1或2个氮原子作为杂原子的六元杂芳环，Y是氢，低级烷酰基或低级烷氧基羰基，R 1和R 2各自是氢，低级烷基，低级烷酰基，苯甲酰基，低级烷基巯基，羟基，巯基，羟基（低级）烷基，卤素或氰基，或者R 1和R 2可以连接在一起形成可被氧代基取代的低级亚烷基链，Z是苯基，低级烷基，环己二烯基，噻吩基或异噻唑基，其通过使下式化合物：其中Z如上所定义或其衍生物与下式的羧酸反应制备：其中和R2 各自如上所定义，或其反应性衍生物，如果需要，随后水解或酰化所得产物和/或消除任何保护基团，并且其可用作针对各种革兰氏阳性和革兰氏阴性菌的抗微生物剂，包括 uding假单胞菌

12. 发明授权

US3992371A Penicillins substituted with heterocyclic and substituted phenyl groups 失效
标题翻译：用杂环和取代的苯基取代的青霉素
公开(公告)号：US3992371A
公开(公告)日：1976-11-16
申请号：US536181
申请日：1974-12-24
申请人： Hisao Tobiki , Hirotada Yamada , Iwao Nakatsuka , Kozo Shimago , Shigeru Okano , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Hiroshi Noguchi , Yasuko Eda
发明人： Hisao Tobiki , Hirotada Yamada , Iwao Nakatsuka , Kozo Shimago , Shigeru Okano , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Hiroshi Noguchi , Yasuko Eda
IPC分类号： C07D499/10 , C07D471/04 , C07D499/00 , C07D499/04 , C07D499/64 , C07D499/68 , C07D519/06 , C07D499/70
CPC分类号： C07D471/04 , C07D499/00
摘要： Novel penicillins of the formula ##SPC1##Wherein ##EQU1## represents a substituted or unsubstituted benzene or nitrogen atom-containing heteroaromatic ring which may be substituted, ##EQU2## represents a pyridine, pyrazine or pyridazine ring, X represents an oxygen or sulfur atom, Y represents a hydrogen atom or a loer alkoxycarbonyl or lower alkanoyl group, and R.sub.1, R.sub.2 and R.sub.3 are each a hydrogen or halogen atom or a nitro, lower alkylamino, di(lower)alkylamino, aine, lower alkoxycarbonylamino, lower alkanoylamino, amino(lower)alkyl, lower alkyl, lower alkoxy, hydroxyl, sulfamoyl, trifluoromethyl, lower alkylthio or lower alkylsulfonyl group, excluding the cases where all of R.sub.1, R.sub.2 and R.sub.3 are hydrogen atoms and where R.sub.1 is a hydroxyl group and R.sub.2 and R.sub.3 are each a hydrogen or halogen atom, and their nontoxic, pharmaceutically acceptable salts, which can be prepared by reacting a carboxylic acid of the formula: ##EQU3## wherein ##EQU4## X and Y are each as defined above or its reactive derivative with a compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2 and R.sub.3 are each as defined above or its reactive derivative, and are ueful as antimicrobial agents against gram-positive and gram-negative bacteria including Pseudomonas.
摘要翻译：式+ q，10的新型青霉素其中C | A C表示可被取代的取代或未取代的含有苯或含氮原子的杂芳环，C | C | CB表示吡啶，吡嗪或哒嗪环，X表示氧或硫原子，Y表示氢原子或低级烷氧基羰基或低级烷酰基，R 1，R 2和R 3各自为氢或卤素原子或硝基，低级烷基氨基，二（低级）烷基氨基，亚氨基，低级烷氧基羰基氨基，低级烷酰基氨基，氨基（低级）烷基，低级烷基，低级烷氧基，羟基，氨磺酰基，三氟甲基，低级烷硫基或低级烷基磺酰基，不包括R1，R2和R3全部为氢原子，其中R1为羟基， R2和R3各自为氢或卤素原子，以及它们的无毒的药学上可接受的盐，其可以通过使下式的羧酸：XY | C | C-COOH A | CB反应而制备，其中CC | | CA | | C，CB，X和Y为ea ch或其反应性衍生物与下式的化合物：+ q，21，其中R1，R2和R3各自如上所定义，或其反应性衍生物，并且作为抗革兰氏阳性和革兰氏阴性细菌的抗微生物剂包括假单胞菌。

13. 发明授权

US3951955A Penicillins substituted with heterocyclic groups 失效
标题翻译：青霉素被杂环基取代
公开(公告)号：US3951955A
公开(公告)日：1976-04-20
申请号：US491693
申请日：1974-07-25
申请人： Hisao Tobiki , Kozo Shimago , Shigeru Okano , Toshiaki Komatsu , Toyozo Katsura , Yasushi Taira , Yasuko Eda
发明人： Hisao Tobiki , Kozo Shimago , Shigeru Okano , Toshiaki Komatsu , Toyozo Katsura , Yasushi Taira , Yasuko Eda
IPC分类号： C07D499/00 , C07D499/64 , C07D499/44
CPC分类号： C07D499/00
摘要： A penicillin of the formula: ##SPC1##Wherein A is a substituted or unsubstituted condensed aromatic carbocyclic or heterocyclic ring, R is hydrogen or lower alkyl, X is oxygen or sulfur, Y is hydrogen, lower alkyl, lower alkanoyl or lower alkoxycarbonyl and Z is phenyl or thienyl which can be produced by reacting 6-aminopenicillanic acid or its ester with a carboxylic acid of the formula: ##SPC2##Wherein A, R, X, Y and Z are each as defined above or its reactive derivative. The said penicillin and its non-toxic salts have a broad antimicrobial spectrum against various gram-positive and gram-negative bacteria, and they exhibit characteristically a strong antimicrobial activity against Pseudomonas.
摘要翻译：青霉素的配方：

14. 外观设计

USD456402S1 Computer 失效
公开(公告)号：USD456402S1
公开(公告)日：2002-04-30
申请号：US29138302
申请日：2001-03-12
申请人： Hideo Sue , Toshiaki Komatsu , Jun Kubokawa , Junya Ohno , Muneyoshi Nikuni
设计人： Hideo Sue , Toshiaki Komatsu , Jun Kubokawa , Junya Ohno , Muneyoshi Nikuni

15. 发明授权

US4302454A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US4302454A
公开(公告)日：1981-11-24
申请号：US105440
申请日：1979-12-19
申请人： Hirotada Yamada , Takenari Nakagome , Toshiaki Komatsu
发明人： Hirotada Yamada , Takenari Nakagome , Toshiaki Komatsu
IPC分类号： A61K31/545 , C07D501/36
CPC分类号： A61K31/545
摘要： A compound of the formula (I): ##STR1## wherein A is a monocyclic or polycyclic heteroaromatic ring containing at least one nitrogen atom as a hetero atom, which may be unsubstituted or substituted with one or more substituents;R is a phenyl group which can be unsubstituted or substituted or a thienyl group;T is (1) a --CH.sub.2 --S--Het group, where Het is a tetrazolopyridazine ring, a triazolopyridazine ring, or a triazolopyridine ring, (2) a ##STR2## group where R.sub.1 and R.sub.2, which may be the same or different, each is a hydrogen atom or a (C.sub.1 -C.sub.4) alkyl group, (3) a --CH.sub.2 N.sub.3 group or (4) a --CH.sub.2 S--D group in which D is a group selected from the group consisting of ##STR3## where m and n each is 0 to 3: with the proviso that (a) when the HO--A-- moiety is a ##STR4## group where B represents the non-metallic atoms necessary to complete a pyridine ring, a pyrimidine ring or a pyrazole ring, each of which may be unsubstituted or substituted, then T is the --CH.sub.2 SD group wherein D is as defined above, and(b) when T is the --CH.sub.2 N.sub.3 group, then R is a substituted phenyl groupand the non-toxic, pharmaceutically acceptable salts thereof, processes for preparing the same, and anti-microbial compositions containing the same.
摘要翻译：式（I）的化合物：其中A是含有至少一个氮原子作为杂原子的单环或多环杂芳族环，其可以是未取代的或被一个或多个取代基取代; R是可以是未取代的或取代的苯基或噻吩基; T是（1）-CH 2 -S-Het基团，其中Het是四唑并哒嗪环，三唑并哒嗪环或三唑并吡啶环，（2）其中R 1和R 2可以相同或不同各自为氢原子或（C1-C4）烷基，（3）-CH2N3基或（4）-CH2S-D基，其中D为选自下组的基团：图像其中m和n各自为0至3，条件是（a）当HO-A-部分为“IMAGE”基团时，B表示完成所需的非金属原子吡啶环，嘧啶环或吡唑环，其各自可以是未取代的或取代的，则T是-CH2SD基团，其中D如上所定义，和（b）当T是-CH 2 N 3基团时，R是取代的苯基及其无毒的药学上可接受的盐，及其制备方法和含有它们的抗微生物组合物。

16. 发明授权

US4247554A Method for the prevention of gastro-intestinal ulcer caused by a non-steroidal anti-inflammatory agent 失效
标题翻译：用于预防由非甾体抗炎剂引起的胃肠溃疡的方法
公开(公告)号：US4247554A
公开(公告)日：1981-01-27
申请号：US795887
申请日：1977-05-11
申请人： Hisao Yamamoto , Toshiaki Komatsu , Hiroshi Awata
发明人： Hisao Yamamoto , Toshiaki Komatsu , Hiroshi Awata
IPC分类号： A61K31/505
CPC分类号： A61K31/505 , Y10S514/926 , Y10S514/927
摘要： A method for preventing gastro-intestinal ulcer caused by a non-steroidal anti-inflammatory agent, which comprises administering an effective amount of a quinazolinone of the formula, ##STR1## wherein R.sub.1 is C.sub.1-3 alkyl, cyclopropylmethyl or 2,2,2-trifluoroethyl, R.sub.2 is halogen, C.sub.1-3 alkyl or C.sub.1-3 alkoxy, and R.sub.3 is phenyl or thienyl, or a non-toxic pharmaceutically acceptable salt thereof in combination with a pharmaceutically effective amount of the non-steroidal anti-inflammatory agent.
摘要翻译：一种用于预防由非甾体抗炎药引起的胃肠溃疡的方法，其包括给予有效量的下式的喹唑啉酮，其中R 1为C 1-3烷基，环丙基甲基或2,2,2 三氟乙基，R 2是卤素，C 1-3烷基或C 1-3烷氧基，R 3是苯基或噻吩基，或其无毒的药学上可接受的盐与药学上有效量的非甾体抗炎剂的组合。

17. 发明授权

US4156724A N-acylamino-alpha-arylacetamido cephalosporins and antibacterial compositions and methods containing them 失效
标题翻译： N-酰基氨基-α-芳基乙酰胺基头孢菌素和含有它们的抗菌组合物和方法
公开(公告)号：US4156724A
公开(公告)日：1979-05-29
申请号：US611104
申请日：1975-09-08
申请人： Hirotada Yamada , Kousaku Okamura , Hisao Tobiki , Norihiko Tanno , Kozo Shimago , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Hiroshi Noguchi , Kenji Irie , Yasuko Eda
发明人： Hirotada Yamada , Kousaku Okamura , Hisao Tobiki , Norihiko Tanno , Kozo Shimago , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Hiroshi Noguchi , Kenji Irie , Yasuko Eda
IPC分类号： A61K20060101 , A61K31/545 , C07D20060101 , C07D501/04 , C07D501/20 , C07D501/24 , C07D501/26 , C07D501/32 , C07D501/34 , C07D501/36 , C07D501/44 , C07D501/46 , C07D501/54 , C07D501/56 , C07D501/60 , C07D519/00
CPC分类号： C07D501/34 , C07D501/24
摘要： A cephalosporin derivative of the formula (I), ##STR1## wherein A is a mono- or polycyclic heteroaromatic ring, which contains at least one nitrogen atom as a hetero atom and which may be substituted with one or more substituents; R is a phenyl group substituted with at least one substituent selected from the group consisting of an amino group, a hydroxy group, a ureido group and a hydroxymethyl group; and X is an --OCOCH.sub.3 group or an --S-Het group in which Het is a 5- or 6-membered heterocyclic ring containing one to four hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur atoms which may be substituted with one or more substituents, and the non-toxic pharmaceutically acceptable salts thereof which are useful as an antimicrobial and prepared by the reaction of a compound of the formula (II),ho--a--cooh (ii)wherein A is as defined above, or a reactive derivative thereof, with a compound of the formula (III), ##STR2## wherein R and X are as defined above, or a derivative thereof.
摘要翻译：式（I）的头孢菌素衍生物，其中A是单环或多环杂芳环，其含有至少一个氮原子作为杂原子并且可以被一个或多个取代基取代; R是被至少一个选自氨基，羟基，脲基和羟甲基的取代基取代的苯基; 并且X是-OCOCH 3基团或-S-Het基团，其中Het是含有1至4个选自氮，氧和硫原子的杂原子的5或6元杂环，其可以被一种或多种取代基及其无毒的药学上可接受的盐，其可用作抗微生物剂并通过式（II）化合物，其中A如上定义的HO-A-COOH（II）或其活性衍生物与式（III）化合物，其中R和X如上所定义的其中，或其衍生物。

18. 发明授权

US4125611A 3-Heterocyclic thiomethyl 7-methoxy-7 substituted acetamido cephalosporins 失效
标题翻译： 3-杂环硫甲基7-甲氧基-7取代的乙酰氨基头孢菌素
公开(公告)号：US4125611A
公开(公告)日：1978-11-14
申请号：US745749
申请日：1976-11-29
申请人： Hirotada Yamade , Takenari Nakagome , Toshiaki Komatsu
发明人： Hirotada Yamade , Takenari Nakagome , Toshiaki Komatsu
IPC分类号： A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/04 , C07D501/06 , C07D501/20 , C07D501/24 , C07D501/28 , C07D501/32 , C07D501/34 , C07D501/36 , C07D501/40 , C07D501/44 , C07D501/46 , C07D501/56 , C07D501/57 , C07D501/60 , C07D519/06
CPC分类号： C07D501/57 , Y02P20/55
摘要： A cephalosporin of the formula (I): ##STR1## wherein A is a mono- or polycyclic heteroaromatic ring containing at least one nitrogen atom as a hetero atom, which may be unsubstituted or substituted; R is a phenyl group which may be unsubstituted or substituted, a thienyl group, a furyl group, a cyclohexadienyl group or a cyclohexenyl group; X is an acetoxy group, a pyridinium group which may be unsubstituted or substituted with a methyl or carbamoyl group, a group of the formula: ##STR2## in which R.sub.1 and R.sub.2, which may be the same or different, each is a hydrogen atom or a (C.sub.1 - C.sub.4) alkyl group, or a group of the formula:-S-Hetin which Het is a heterocyclic ring containing 1 to 5 oxygen, nitrogen and sulfur atoms as a hetero atom, in which the heterocyclic ring system may be either polycyclic or 5- or 6-membered monocyclic and may be unsubstituted or substituted; and M is a hydrogen atom or a biologically active carboxyl-protecting group, or is an anionic charge only when X is a pyridinium group; and the pharmaceutically acceptable salts thereof, which are useful as antimicrobial agents and prepared by the reaction of a compound of the formula (II):ho--a--cooh (ii)wherein A is as defined above, or a reactive derivative thereof, with a compound of the formula (III): ##STR3## wherein R, M and X are as defined above, or a derivative thereof.
摘要翻译：式（I）的头孢菌素：其中A是含有至少一个氮原子作为杂原子的单环或多环杂芳环，其可以是未取代的或取代的; R是可以是未取代或取代的苯基，噻吩基，呋喃基，环己二烯基或环己烯基; X是乙酰氧基，可以是未取代的或被甲基或氨基甲酰基取代的吡啶鎓基，下式的基团：其中R 1和R 2可以相同或不同，各自为氢原子或（C 1 -C 4）烷基，或下式的基团：

19. 发明授权

US4008237A 2,3,5,8-Tetrahydro-5-alkoxy-8-oxofuro(2,3-g)quinoline-7-carboxylic acid derivatives 失效
标题翻译： 2,3,5,8-四氢-5-烷氧基-8-氧代呋喃（2,3-g）喹啉-7-羧酸衍生物
公开(公告)号：US4008237A
公开(公告)日：1977-02-15
申请号：US626001
申请日：1975-10-28
申请人： Hideo Agui , Iwao Nakatsuka , Toru Mitani , Mitsuo Nakashita , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Yasuko Eda
发明人： Hideo Agui , Iwao Nakatsuka , Toru Mitani , Mitsuo Nakashita , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Yasuko Eda
IPC分类号： C07D215/56 , C07D491/048
CPC分类号： C07D491/048
摘要： Novel antibacterial agents consisting of a 2,3,5,8-tetrahydro-5-alkoxy-8-oxofuro(2,3-g)quinoline-7-carboxylic acid of the formula: ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl, a process for producing the derivatives and pharmaceutical compositions containing the same. The above-identified derivatives possess antibacterial activity against gram-negative bacteria at test concentration levels of about 0.0001 to 1.0 mg/cc.
摘要翻译：新型抗菌剂由下列通式的2,3,5,8-四氢-5-烷氧基-8-氧代呋喃（2,3-g）喹啉-7-羧酸组成，其中R是C 1 -C 4烷基，制备衍生物的方法和含有该衍生物的药物组合物。上述衍生物在约0.0001至1.0mg / cc的测试浓度水平下对革兰氏阴性细菌具有抗菌活性。

20. 发明授权

US3954775A Thiazolo(5,4-f)quinoline-8-carboxylic acid derivatives 失效
标题翻译：噻唑（5,4-f）喹啉-8-羧酸衍生物
公开(公告)号：US3954775A
公开(公告)日：1976-05-04
申请号：US515753
申请日：1974-10-17
申请人： Hideo Agui , Toru Mitani , Mitsuo Nakashita , Eiichi Murayama , Kousaku Okamura , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Yasuko Eda
发明人： Hideo Agui , Toru Mitani , Mitsuo Nakashita , Eiichi Murayama , Kousaku Okamura , Takenari Nakagome , Toshiaki Komatsu , Akio Izawa , Yasuko Eda
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： Thiazolo[5,4-f]quinoline-8-carboxylic acid derivatives having either the general formula (I): ##SPC1##wherein R.sub.1 is a lower alkyl group, a lower alkenyl group or a benzyl group; or the general formula (III-a): ##SPC2##Wherein R.sub.3 is a lower alkyl group and X is a halogen atom; and methods for the preparation thereof. The compounds of the general formula (I) are useful as antibacterial agents against gram-negative and gram-positive bacteria. The compounds of the general formula (III-a) are useful as antifungal agents against eumycetes and also as an intermediate in a preparation of the compounds of the general formula (I).
摘要翻译：具有通式（I）的噻唑并[5,4-f]喹啉-8-羧酸衍生物：

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