公开(公告)号：US4652638A

公开(公告)日：1987-03-24

申请号：US782591

申请日：1985-09-30

申请人： Tatsuro Fujiwara ,  Kazuyo Ohta ,  Takao Hirano

发明人： Tatsuro Fujiwara ,  Kazuyo Ohta ,  Takao Hirano

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

CPC分类号： C07H17/08 ,  Y02P20/55

摘要： Novel 3-O-acyl-4"-deoxydesmycosin derivatives of the formula ##STR1## wherein R.sub.1 is lower alkyl, phenyl, substituted phenyl, phenyl-lower alkyl or substituted phenyl-lower alkyl, R.sub.2 is hydrogen or --CHO and R.sub.3 is hydrogen or hydroxyl, or a non-toxic salt thereof, can be produced by acylating the hydroxyl group at position-3 of the corresponding intermediate while protecting the hydroxyl at position-2' or positions-2' and -4' with acetyl, and then removing the protective group or groups. These derivatives have antibiotic utility against Gram positive and Gram negative bacteria.

摘要翻译： 其中R 1为低级烷基，苯基，取代的苯基，苯基 - 低级烷基或取代的苯基 - 低级烷基，R2为氢或-CHO，R3为低级烷基，低级烷氧基， 氢或羟基或其无毒盐可以通过酰化相应中间体的3位的羟基，同时用乙酰基保护位置-2'或位置-2'和-4'的羟基来制备，和 然后取出保护基或组。 这些衍生物具有抗革兰氏阳性和革兰氏阴性菌的抗生素效用。

公开(公告)号：US5026832A

公开(公告)日：1991-06-25

申请号：US450398

申请日：1989-12-14

申请人： Tatsuro Fujiwara ,  Yuji Kogami ,  Asako Watanabe

发明人： Tatsuro Fujiwara ,  Yuji Kogami ,  Asako Watanabe

IPC分类号： C07H17/08

CPC分类号： C07H17/08

摘要： 9-Dihydro-9-O-alkyldesmycosin derivatives and their salts are disclosed. The 9-dihydro-9-O-alkyldesmycosin derivatives are represented by the following formula (I), ##STR1## --wherein X represents an --O-- mycinose or a di-lower alkylamino group, R.sup.1 represents a hydrogen atom or a lower alkanoyl group, R.sup.2 represents a lower alkyl group, a cycloalkyl-lower group, or phenyl-lower alkyl group which may have a substituent, and R.sup.3 represents a hydrogen atom or a hydroxyl group. The compounds and the salts are useful as an antimicrobial agent. Unlike known desmycosin derivatives, the compounds give a high blood concentration by oral administration.

公开(公告)号：US5200515A

公开(公告)日：1993-04-06

申请号：US701125

申请日：1991-05-16

申请人： Satoshi Shuto ,  Hiromichi Itoh ,  Takumi Obara ,  Tatsuro Fujiwara

发明人： Satoshi Shuto ,  Hiromichi Itoh ,  Takumi Obara ,  Tatsuro Fujiwara

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61P35/00 ,  C07H19/10 ,  C12P19/30

CPC分类号： C07H19/10 ,  A61K47/48053 ,  C12P19/305

摘要： Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each C.sub.16-18 long-chain aliphatic acyl and are the same or different; and pharmacologically acceptable salts thereof are disclosed. These novel compounds are effective against 5-FU-resistant tumor cells, have low toxicity, and are not inactivated by nucleoside phosphorylase in vivo.

公开(公告)号：US5187174A

公开(公告)日：1993-02-16

申请号：US673177

申请日：1991-03-18

申请人： Satoshi Shuto ,  Takumi Obara ,  Hiromichi Itoh ,  Takehiro Koshio ,  Tatsuro Fujiwara ,  Masao Yaso

发明人： Satoshi Shuto ,  Takumi Obara ,  Hiromichi Itoh ,  Takehiro Koshio ,  Tatsuro Fujiwara ,  Masao Yaso

IPC分类号： C07D473/00

CPC分类号： C07D473/00 ,  Y02P20/55

摘要： A compound of the formula ##STR1## wherein A is adenine-9-yl and X is halogen, Preferably iodine, or a pharmaceutically acceptable salt thereof. It is a novel derivative of neplanocin A and has almost the same level of cytotoxic activity. However, it is not inactivated by the action of adenosine deaminase. It is produced by replacing a hydroxyl at position-6' in neplanocin A or 2', 3'-O-protected neplanocin A with halogen by use of a halogenating agent, and when hydroxyl at position-2' or -3' is protected, removing the protective group thereof.

摘要翻译： 式IMA的化合物，其中A是腺嘌呤-9-基，X是卤素，优选碘，或其药学上可接受的盐。 它是奈曲立诺A的新型衍生物，具有几乎相同的细胞毒活性水平。 然而，它不会被腺苷脱氨酶的作用所灭活。 通过使用卤化剂用卤素取代在neplanocin A或2'，3'-O保护的neplanocin A中的6'位的羟基，并且当位置-2'或-3'的羟基被保护时， ，除去其保护基。