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1. 发明授权

US4709022A Pheophorbide derivatives and alkaline salts thereof 失效
标题翻译：偏硼酸衍生物及其碱式盐
公开(公告)号：US4709022A
公开(公告)日：1987-11-24
申请号：US746386
申请日：1985-06-19
申请人： Isao Sakata , Susumu Nakajima , Koichi Koshimuzi , Natsuki Samejima , Kazumi Inohara , Hiroyuki Takata
发明人： Isao Sakata , Susumu Nakajima , Koichi Koshimuzi , Natsuki Samejima , Kazumi Inohara , Hiroyuki Takata
IPC分类号： A61K31/40 , A61P35/00 , C07D487/22 , C07D519/00
CPC分类号： C07D487/22 , C07D519/00
摘要： Pheophorbide derivatives and alkaline salts thereof having the general formula (A): ##STR1## wherein R.sub.1 represents --CH.dbd.CH.sub.2, --CH(OH)CH.sub.3, --CH(OCH.sub.2 CH.sub.2 OH)CH.sub.3 or --CH(OCOCH.sub.3)CH.sub.3R.sub.2 represents --CH.sub.3, --CHO or --CH.sub.2 OHR.sub.3 represents .dbd.O, --OH or --OCOCH.sub.3R.sub.4 represents --H, --COOCH.sub.3, --COOCH.sub.2 CH.sub.2 OH, --COOCH.sub.2 CH.sub.2 OCOCH.sub.3, or a --CONH-- containing residue of an amino acid andR.sub.5 represents --COOH, --COONa or --COOCH.sub.3 ; provided, however, said derivatives and alkaline salts exclude pheophorbide, 9-desoxo-9-hydroxy-pheophorbide and pyropheophorbide.Dimeric pheophorbide derivatives and alkaline salts thereof represented by the general formula (B): ##STR2## wherein R.sub.1 through R.sub.5 are the same as in general formula (A), are useful for treating cancer having a strong preferential affinity for cancer cells over normal cells and exerting upon irradiation a destructive effect on such cancer cells.
摘要翻译：（A）的焦磷酸衍生物及其碱金属盐：其中R 1表示-CH = CH 2，-CH（OH）CH 3，-CH（OCH 2 CH 2 OH）CH 3或-CH（OCOCH 3） -CH 3，-CHO或-CH 2 OH R 3表示= O，-OH或-OCOCH 3 R 4表示-H，-COOCH 3，-COOCH 2 CH 2 OH，-COOCH 2 CH 2 OCOCH 3或含-CONH-的氨基酸残基，R 5表示-COOH， COONa或-COOCH3; 但是，所述衍生物和碱性盐不包括偏硼酸，9-脱氧-9-羟基 - 脱镁叶绿素和焦脱镁叶绿素。由通式（B）表示的二聚偏硼酸衍生物及其碱式盐：其中R 1至R 5与通式（A）中相同）可用于治疗对癌细胞具有强的优先亲和力的癌症超过正常细胞，并在照射下施加对这种癌细胞的破坏作用。

2. 发明授权

US4849207A Porphyrin derivatives 失效
标题翻译：卟啉衍生物
公开(公告)号：US4849207A
公开(公告)日：1989-07-18
申请号：US922492
申请日：1986-10-23
申请人： Isao Sakata , Susumu Nakajima , Koichi Koshimizu , Natsuki Samejima , Kazumi Inohara , Hiroyuki Takata , Hirohiko Yamauchi , Nobuo Ueda , Masaaki Hazue
发明人： Isao Sakata , Susumu Nakajima , Koichi Koshimizu , Natsuki Samejima , Kazumi Inohara , Hiroyuki Takata , Hirohiko Yamauchi , Nobuo Ueda , Masaaki Hazue
IPC分类号： A61K31/40 , A61K31/43 , C07B59/00 , C07D487/22
CPC分类号： C07D487/22
摘要： A porphyrin compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each --CH.dbd.CH.sub.2, --CH.sub.2 CH.sub.3, --CH(O-lower alkanoyl)CH.sub.3, --CH(OR)CH.sub.3 or --CH(O-lower alkylene-OR)CH.sub.3 ; R.sub.3 is --H, --COOH, --COO-lower alkyl, --COO-lower alkylene-OR or --COO-lower alkylene-OOC-Z; R.sub.4 is --H, -lower alkyl or -lower alkylene-OR; R is --H, -lower alkyl or a residue of a polyfunctional carboxyl compound excluding a hydrogen atom therefrom; Z is a residue of the compound of the formula (I) excluding R.sub.3 therefrom; A is --CH.sub.2 -- or --CO--; and the dotted line from the gamma-position indicates no bonding or a single direct bond; and the dotted line between the 7- and 8-positions indicates the presence of a single bond or a double bond; and its complexes with a metal(s) in the porphine skeleton and/or at the residue of the polyfuntional carboxyl compound, at least one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 being a group containing R which represents the residue of the polyfunctional carboxyl compound and R.sub.1 being capable of representing 1-iodoethyl in addition to said meanings when R.sub.3 is --COO-lower alkylene-OOC-Z, which shows a high accumulation in the locus of cancer with quick excretion from normal tissues.
摘要翻译：一种下式的卟啉化合物：其中R 1和R 2各自为-CH = CH 2，-CH 2 CH 3，-CH（O-低级烷酰基）CH 3，-CH（OR）CH 3或-CH（O-低级）亚烷基-OR）CH 3; R3是-H，-COOH，-COO-低级烷基，-COO-低级亚烷基-OR或-COO-低级亚烷基-OOC-Z; R4是-H-低级烷基或 - 低级亚烷基-OR; R是-H，低级烷基或除了氢原子以外的多官能羧基化合物的残基; Z是除了R3之外的式（I）化合物的残基; A是-CH2-或-CO-; 并且来自γ位置的虚线表示没有键合或单个直接键合; 7位和8位之间的虚线表示存在单键或双键; 其与卟啉骨架中的金属和/或多官能羧基化合物的残基的络合物，R 1，R 2，R 3和R 4中的至少一个为含有R的基团，其表示多官能羧基化合物的残基当R 3为-COO-低级亚烷基-OOC-Z时，R 1除了所述含义之外，还能够表示1-碘乙基，其在正常组织中快速排出的癌症基因座中表现出高度的积累。

3. 发明授权

US4996312A Porphyrin derivatives, and their production and use 失效
标题翻译：卟啉衍生物及其生产和使用
公开(公告)号：US4996312A
公开(公告)日：1991-02-26
申请号：US340549
申请日：1989-04-19
申请人： Isao Sakata , Susumu Nakajima , Koichi Koshimizu , Natsuki Samejima , Kazumi Inohara , Hiroyuki Takata , Hirohiko Yamauchi , Nobuo Ueda , Masaaki Hazue
发明人： Isao Sakata , Susumu Nakajima , Koichi Koshimizu , Natsuki Samejima , Kazumi Inohara , Hiroyuki Takata , Hirohiko Yamauchi , Nobuo Ueda , Masaaki Hazue
IPC分类号： A61K31/40 , A61K31/43 , C07B59/00 , C07D487/22
CPC分类号： C07D487/22
摘要： A porphyrin compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each --CH.dbd.CH.sub.2, --CH.sub.2 CHJ.sub.3, --CH(O-lower alkanoyl)CH.sub.3, --CH(OR)CH.sub.3 or --CH(O-lower alkylene-OR)CH.sub.3 ; R.sub.3 is --H, --COOH, --COO-lower alkyl, --COO-lower alkylene-OR or --COO-lower alkylene-OOC-Z; R.sub.4 is --H, -lower alkyl or -lower alkylene-OR; R is --H, -lower alkyl or a residue of a polyfunctional carboxyl compound excluding a hydrogen atom therefrom; Z is a residue of the compound of the formula (I) excluding R.sub.3 therefrom; A is --CH.sub.2 -- or --CO--; and the dotted line from the gamma-position indicates no bonding or a single direct bond; and the dotted line between the 7- and 8-positions indicates the presence of a single bond or a double bond; and its complexes with a metal(s) in the porphine skeleton and/or at the residue of the polyfunctional carboxyl compound, at least one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 being a group containing R which represents the residue of the polyfunctional carboxyl compound and R.sub.1 being capable of representing 1-iodoethyl in addition to said meanings when R.sub.3 is --COO-lower alkylene-OOC-Z, which shows a high accumulation in the locus of cancer with quick excretion from normal tissues.

4. 发明授权

US4604241A 9-desoxo-9-hydroxy-pheophorbide derivatives and alkaline salts thereof 失效
标题翻译： 9-脱氧-9-羟基 - 脱镁叶绿酸衍生物及其碱式盐
公开(公告)号：US4604241A
公开(公告)日：1986-08-05
申请号：US664375
申请日：1984-10-24
申请人： Isao Sakata , Susumu Nakajima , Koichi Koshimizu , Natsuki Samejima , Kazumi Inohara , Hiroyuki Takata
发明人： Isao Sakata , Susumu Nakajima , Koichi Koshimizu , Natsuki Samejima , Kazumi Inohara , Hiroyuki Takata
IPC分类号： A61K31/40 , A61P35/00 , C07D487/22 , C07D519/00
CPC分类号： C07D487/22 , C07D519/00
摘要： Nine-desoxo-hydroxy-pheophorbide derivatives and alkaline salts thereof represented by the general formula: ##STR1## wherein R.sub.1 represents CH.sub.3 or CH.sub.2 OH,R.sub.2 represents H or Ac, andR.sub.3 represents H or alkali metal,are useful for treating cancer having a strong preferential affinity for cancer cells over normal cells and exerting upon irradiation a destructive effect on such cancer cells.
摘要翻译：其中R 1表示CH 3或CH 2 OH，R 2表示H或Ac，R 3表示H或碱金属，可用于治疗具有强烈的癌症的九种脱氧 - 羟基 - 脱镁叶绿酸衍生物及其碱盐对癌细胞优于正常细胞的优先亲和力并且在照射下施加对这种癌细胞的破坏作用。

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