公开(公告)号：US3984401A

公开(公告)日：1976-10-05

申请号：US422748

申请日：1973-12-07

申请人： Shinji Terao ,  Mitsuru Shiraishi ,  Toshio Miyawaki ,  Isao Minamida ,  Masayoshi Yamaoka ,  Yoshio Imashiro ,  Mitsuo Numata

发明人： Shinji Terao ,  Mitsuru Shiraishi ,  Toshio Miyawaki ,  Isao Minamida ,  Masayoshi Yamaoka ,  Yoshio Imashiro ,  Mitsuo Numata

IPC分类号： A61K31/545 ,  C07D501/04 ,  C07D501/16 ,  C07D501/26 ,  C07D501/60 ,  C07D513/14 ,  C07D515/14

CPC分类号： C07D501/04 ,  C07D501/26

摘要： A 3-hydroxymethylcephalosporin which is not protected at the carboxyl group can be directly oxidized with a hexavalent chromium compound to give in good yield a lactol type cephalosporin represented by the general formula: ##SPC1##Wherein R.sup.1 is hydrogen or an alkoxy group and R.sup.2 is an acylamino, or imido group. The resulting compounds are very useful and important as intermediates for preparing, e.g. 3-alkoxyiminomethyl cephalosporins.

摘要翻译： 在羧基上未被保护的3-羟甲基头孢菌素可以用六价铬化合物直接氧化，得到良好的产率，由通式表示的乳糖型头孢菌素：

公开(公告)号：US4011214A

公开(公告)日：1977-03-08

申请号：US534787

申请日：1974-12-20

申请人： Shinji Terao ,  Mitsuru Shiraishi ,  Toshio Miyawaki ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuo Numata

发明人： Shinji Terao ,  Mitsuru Shiraishi ,  Toshio Miyawaki ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuo Numata

IPC分类号： C07D501/24 ,  A61K31/43 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/04 ,  C07D501/38 ,  C07D501/50 ,  C07D501/52 ,  C07D501/54 ,  C07D501/60

CPC分类号： C07D501/38

摘要： Novel cephalosporin compounds of the formula ##STR1## wherein R.sup.1 is an acyl group and R.sup.2 is an alkylene group which may be substituted with a lower alkoxyl group, or pharmaceutically acceptable salt thereof, have strong inhibitory actions on broad spectra of gram-positive and gram-negative bacteria and, particularly against Esherichia coli and Klebsiella pneumoniae. Thus, the compounds are useful as therapeutic agent for various bacterial infections of animals including human beings.

公开(公告)号：US4517361A

公开(公告)日：1985-05-14

申请号：US480791

申请日：1983-03-31

申请人： Mitsuo Numata ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

发明人： Mitsuo Numata ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

IPC分类号： C07D277/34 ,  C07D277/36 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/28

CPC分类号： C07D501/24 ,  C07D277/34 ,  C07D277/36

摘要： A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula -NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula -SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.

摘要翻译： 下式的化合物：其中R 1表示氢或烷基，X表示氧或硫或式-NR 2基团（其中R 2是氢或烷基，在烷基的情况下可以形成 环与R 1连接），Y表示乙酰氧基或式-SR 3（其中R 3为含氮杂环基）基团或其药学上可接受的盐具有宽的抗菌谱，特别是， 对革兰氏阴性菌有效，包括大肠杆菌，肺炎克雷伯杆菌，普通变形杆菌，变形杆菌，以及革兰氏阳性菌。 因此，这些化合物可用于治疗目的的抗微生物剂。

公开(公告)号：US4080498A

公开(公告)日：1978-03-21

申请号：US534782

申请日：1974-12-20

申请人： Mitsuo Numata ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

发明人： Mitsuo Numata ,  Isao Minamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

IPC分类号： C07D277/34 ,  C07D277/36 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/60

CPC分类号： C07D501/24 ,  C07D277/34 ,  C07D277/36

摘要： A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula --NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula --SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.

摘要翻译： 下式的化合物：其中R 1表示氢或烷基，X表示氧或硫或式-NR 2基团（其中R 2是氢或烷基，在烷基的情况下可以形成 环与R 1连接），Y表示乙酰氧基或式-SR 3（其中R 3为含氮杂环基）基团或其药学上可接受的盐具有宽的抗菌谱，特别是， 对革兰氏阴性菌有效，包括大肠杆菌，肺炎克雷伯杆菌，普通变形杆菌，变形杆菌，以及革兰氏阳性菌。 因此，这些化合物可用于治疗目的的抗微生物剂。

公开(公告)号：US4421912A

公开(公告)日：1983-12-20

申请号：US235609

申请日：1981-02-18

申请人： Mitsuo Numata ,  Isao Mimamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

发明人： Mitsuo Numata ,  Isao Mimamida ,  Masayoshi Yamaoka ,  Mitsuru Shiraishi ,  Toshio Miyawaki

IPC分类号： C07D277/34 ,  C07D277/36 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36

CPC分类号： C07D501/24 ,  C07D277/34 ,  C07D277/36

摘要： A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula --NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula --SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.

公开(公告)号：US4379924A

公开(公告)日：1983-04-12

申请号：US863719

申请日：1977-12-23

申请人： Mitsuo Numata ,  Isao Mimamida ,  Masayoshi Yamaoka ,  Mitsura Shiraishi ,  Toshio Miyawaki

发明人： Mitsuo Numata ,  Isao Mimamida ,  Masayoshi Yamaoka ,  Mitsura Shiraishi ,  Toshio Miyawaki

IPC分类号： C07D277/34 ,  C07D277/36 ,  C07D501/36 ,  A61K31/545

CPC分类号： C07D501/24 ,  C07D277/34 ,  C07D277/36

摘要： A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula --NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula --SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.

公开(公告)号：US20060106067A1

公开(公告)日：2006-05-18

申请号：US10524452

申请日：2003-08-11

申请人： Mitsuru Shiraishi ,  Takahito Hara ,  Masami Kusaka ,  Naoyuki Kanzaki ,  Satoshi Yamamoto ,  Toshio Miyawaki

发明人： Mitsuru Shiraishi ,  Takahito Hara ,  Masami Kusaka ,  Naoyuki Kanzaki ,  Satoshi Yamamoto ,  Toshio Miyawaki

IPC分类号： A61K31/454 ,  C07D409/02

CPC分类号： C07C255/52 ,  C07C35/52 ,  C07C217/04 ,  C07C255/53 ,  C07C255/54 ,  C07C255/56 ,  C07C2601/08 ,  C07C2601/10 ,  C07D207/06 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D207/22 ,  C07D207/24 ,  C07D209/46 ,  C07D211/22 ,  C07D211/28 ,  C07D211/34 ,  C07D211/42 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D211/74 ,  C07D231/08 ,  C07D261/04 ,  C07D265/02 ,  C07D267/10 ,  C07D295/073 ,  C07D295/112 ,  C07D295/155 ,  C07D303/46 ,  C07D307/79 ,  C07D333/54 ,  C07D405/04 ,  C07D409/04 ,  C07D491/10

摘要： The present invention provides a compound represented by the general formula: [wherein Ring A represents an optionally substituted 5- to 8-membered ring, Ring B represents a further optionally substituted 4- to 10-membered ring, Ring C represents a further optionally substituted benzene ring, X1 represents carbon atom, X2 represents a carbon atom, an oxygen atom, etc., W represents a nitrogen atom, etc., Y11 represents a group represented by the formula CR2R3′ (wherein R2 represents a hydrogen atom, a cyano group, a nitro group, etc., and R3′ represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), Y21 represents a group represented by the formula CR4R5′ (wherein R4 represents a hydrogen atom, a cyano group, a nitro group, etc., and R5′ represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), etc., and R1 represents an electron-withdrawing group, respectively. The formula represents a single bond or a double bond] or a salt thereof, which is useful as an androgen receptor modulator.

摘要翻译： 本发明提供由以下通式表示的化合物：其中环A表示任选取代的5-至8-元环，环B表示另外任选取代的4-至10-元环，环C表示另外任选取代的 苯环，X 1表示碳原子，X 2表示碳原子，氧原子等，W表示氮原子等，Y表示碳原子， 11表示由式CR 2表示的基团R 3（其中R 2表示氢原子，氰基） ，硝基等，R 3'分别表示氢原子，氰基，硝基等），Y 21表示基团 由式CR 4 S 5 H 5（其中R 4表示氢原子，氰基，硝基等）表示， 和R 5'分别表示氢原子，氰基，硝基等）等，R 1， SUP>分别表示吸电子基团。 公式<？in-line-formula description =“In-line Formulas”end =“lead”？> <？in-line-formula description =”In-line Formulas“end =”tail“ α“表示单键或双键]或其盐，其可用作雄激素受体调节剂。

公开(公告)号：US07649001B2

公开(公告)日：2010-01-19

申请号：US10524452

申请日：2003-08-11

申请人： Mitsuru Shiraishi ,  Takahito Hara ,  Masami Kusaka ,  Naoyuki Kanzaki ,  Satoshi Yamamoto ,  Toshio Miyawaki

发明人： Mitsuru Shiraishi ,  Takahito Hara ,  Masami Kusaka ,  Naoyuki Kanzaki ,  Satoshi Yamamoto ,  Toshio Miyawaki

IPC分类号： A61K31/454 ,  C07D409/02

CPC分类号： C07C255/52 ,  C07C35/52 ,  C07C217/04 ,  C07C255/53 ,  C07C255/54 ,  C07C255/56 ,  C07C2601/08 ,  C07C2601/10 ,  C07D207/06 ,  C07D207/08 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D207/22 ,  C07D207/24 ,  C07D209/46 ,  C07D211/22 ,  C07D211/28 ,  C07D211/34 ,  C07D211/42 ,  C07D211/46 ,  C07D211/60 ,  C07D211/62 ,  C07D211/74 ,  C07D231/08 ,  C07D261/04 ,  C07D265/02 ,  C07D267/10 ,  C07D295/073 ,  C07D295/112 ,  C07D295/155 ,  C07D303/46 ,  C07D307/79 ,  C07D333/54 ,  C07D405/04 ,  C07D409/04 ,  C07D491/10

摘要： The present invention provides a compound represented by the general formula: [wherein Ring A represents an optionally substituted 5- to 8-membered ring, Ring B represents a further optionally substituted 4- to 10-membered ring, Ring C represents a further optionally substituted benzene ring, X1 represents carbon atom, X2 represents a carbon atom, an oxygen atom, etc., W represents a nitrogen atom, etc., Y11 represents a group represented by the formula CR2R3′ (wherein R2 represents a hydrogen atom, a cyano group, a nitro group, etc., and R3′ represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), Y21 represents a group represented by the formula CR4R5′ (wherein R4 represents a hydrogen atom, a cyano group, a nitro group, etc., and R5′ represents a hydrogen atom, a cyano group, a nitro group, etc., respectively), etc., and R1 represents an electron-withdrawing group, respectively. The formula represents a single bond or a double bond] or a salt thereof, which is useful as an androgen receptor modulator.

摘要翻译： 本发明提供由以下通式表示的化合物：其中环A表示任选取代的5-至8-元环，环B表示另外任选取代的4-至10-元环，环C表示另外任选取代的 苯环，X1表示碳原子，X2表示碳原子，氧原子等，W表示氮原子等，Y11表示由式CR2R3'表示的基团（其中R2表示氢原子，氰基 基，硝基等，R3'分别表示氢原子，氰基，硝基等），Y21表示由式CR4R5'表示的基团（其中R4表示氢原子， 氰基，硝基等，R5'分别表示氢原子，氰基，硝基等），R1表示吸电子基团。 公式表示单键或双键]或其盐，其可用作雄激素受体调节剂。

公开(公告)号：US5344928A

公开(公告)日：1994-09-06

申请号：US868100

申请日：1992-04-14

申请人： Hirotomo Masuya ,  Hiroshi Shimadzu ,  Toshio Miyawaki ,  Marvin A. Motsenbocker

发明人： Hirotomo Masuya ,  Hiroshi Shimadzu ,  Toshio Miyawaki ,  Marvin A. Motsenbocker

IPC分类号： C07C381/02 ,  C07D207/40 ,  C07D207/404 ,  C07D279/18 ,  C07D417/12 ,  C07D417/14 ,  G01N33/533 ,  C07D279/28

CPC分类号： C07D207/404 ,  C07C381/02 ,  C07D279/18 ,  C07D417/12 ,  C07D417/14 ,  G01N33/533 ,  Y10S436/811

摘要： There is disclosed a novel phenothiazine derivative of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are a C.sub.1-6 alkyl group and at least one of them has as a substituent a group which can react with amino group, thiol group or carboxyl group, and X.sup.- is a counter ion of the phenazathionium. Their production and the intermediates used in the production are also disclosed. The compound (I) is a derivative of methylene blue and is applicable to photodynamic therapy of cancer or immunoassays utilizing chemiluminescence.

摘要翻译： 公开了通式（I）的新型吩噻嗪衍生物：其中R 1，R 2，R 3和R 4相同或不同，为C 1-6烷基，并且其中至少一个具有 可以与氨基，硫醇基或羧基反应的基团的取代基，X-是对硝基苯甲酸的抗衡离子。 他们的生产和生产中使用的中间体也被披露。 化合物（I）是亚甲蓝的衍生物，适用于利用化学发光的癌症或免疫测定的光动力学治疗。

公开(公告)号：US09108986B2

公开(公告)日：2015-08-18

申请号：US14232589

申请日：2012-07-13

申请人： Sadayuki Maeda ,  Tatsunori Sato ,  Yasuhiko Kawano ,  Toshio Miyawaki

发明人： Sadayuki Maeda ,  Tatsunori Sato ,  Yasuhiko Kawano ,  Toshio Miyawaki

IPC分类号： C07D215/00 ,  C07F5/00 ,  C07D215/04 ,  C07B53/00 ,  C07F17/02 ,  C07D215/06 ,  C07D215/18 ,  C07D215/20 ,  C07D215/22 ,  C07D215/227 ,  C07D215/14

CPC分类号： C07F5/00 ,  B01J31/181 ,  B01J31/2295 ,  B01J2231/643 ,  B01J2531/0275 ,  B01J2531/827 ,  C07B53/00 ,  C07D215/04 ,  C07D215/06 ,  C07D215/14 ,  C07D215/18 ,  C07D215/20 ,  C07D215/22 ,  C07D215/227 ,  C07F17/02

摘要： Provided are a novel chiral iridium(III) complex; and a method for producing optically active 2-substituted-1,2,3,4-tetrahydroquinolines from 2-substituted-quinolines with the use of the chiral iridium(III) complex through a more economical and easy production process. The disclosed method for producing optically active 2-substituted-1,2,3,4-tetrahydroquinolines comprises reducing a quinoline compound represented by formula [I]: in the presence of a hydrogen donor compound and an iridium (III) complex having a chiral prolinamide compound as a ligand to give an optically active 2-substituted-1,2,3,4-tetrahydroquinoline represented by formula [II]:

摘要翻译： 提供了一种新型的手性铱（III）络合物; 以及通过更经济和容易的制备方法，通过使用手性铱（III）络合物从2-取代的喹啉生产光学活性的2-取代-1,2,3,4-四氢喹啉的方法。 所公开的光学活性2-取代-1,2,3,4-四氢喹啉的制备方法包括还原由式[I]表示的喹啉化合物：在氢供体化合物和具有手性的铱（III）络合物存在下， 脯氨酰胺化合物作为配体，得到式[II]表示的光学活性2-取代-1,2,3,4-四氢喹啉：