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1. 发明授权

US5432267A Amino sugar derivatives 失效
标题翻译：氨基糖衍生物
公开(公告)号：US5432267A
公开(公告)日：1995-07-11
申请号：US40987
申请日：1993-03-31
申请人： Tsuneo Kusama , Tsunehiko Soga , Akiko Tohgo
发明人： Tsuneo Kusama , Tsunehiko Soga , Akiko Tohgo
IPC分类号： C07H15/04 , C07H5/04 , C07H11/04 , C07H13/02
CPC分类号： C07H15/04
摘要： A compound represented by formula (I): ##STR1## wherein R.sup.1 represents --CO--Z.sup.1 --N(Z.sup.11)--CO--Z.sup.2 --H or --CO--Z.sup.3 --H, wherein Z.sup.1, Z.sup.2, and Z.sup.3 each represent an alkylene group having from 1 to 20 carbon atoms, a phenylene group, or a combination thereof, and Z.sup.11 represents a hydrogen atom, an alkyl group having from 1 to 20 carbon atoms which may be substituted with a phenyl group, a phenyl group which may be substituted with an alkyl group having from 1 to 20 carbon atoms, or an alkylene group having from 1 to 20 carbon atoms which may contain therein a phenylene group; R.sup.2 represents --CO--Z.sup.4 --N(Z.sup.12)--CO--Z.sup.5 --H, --CO--Z.sup.6 --H or a hydrogen atom, wherein Z.sup.4, Z.sup.5, and Z.sup.6 each have the same meaning as Z.sup.1, and Z.sup.12 has the same meaning as Z.sup.11 ; Q.sup.1 and Q.sup.2 each represent a carboxyl group or a phosphonoxy group; Q.sup.3 represents a hydrogen atom, a carboxyl group or a phosphonoxy group; m represents 0 or an integer of from 1 to 20; n represents 0 or an integer of from 1 to 20; Y.sup.1 represents an alkylene group having from 1 to 10 carbon atoms which may contain one or more substituents selected from --OCOR.sup.11 and --NHCOR.sup.12, wherein R.sup.11 represents --Z.sup.13 or --Z.sup.7 --N (Z.sup.14)--CO--Z.sup.8 --H (wherein Z.sup.7 and Z.sup.8 each have the same meaning as Z.sup.1, and Z.sup.13 and Z.sup.14 each have the same meaning as Z.sup.11) and R.sup.12 represents --Z.sup.15 or --Z.sup.9 --N(Z.sup.16)--CO--Z.sup.10 --H (wherein Z.sup.9 and Z.sup.10 each have the same meaning as Z.sup.1, and Z.sup.15 and Z.sup.16 each have the same meaning as Z.sup.11), and a salt thereof. The compound inhibits TNF derivation by endotoxin and is therefore useful for the treatment of multiorganic insufficiencies.
摘要翻译：由式（I）表示的化合物：其中Z 1，Z 2和Z 3各自表示具有1至20个碳原子的亚烷基，亚苯基或其组合，和 Z 11表示氢原子，可以被苯基取代的碳原子数1〜20的烷基，可以被碳原子数1〜20的烷基取代的苯基或具有碳原子数1〜20的亚烷基可含有亚苯基的1至20个碳原子; R2表示-CO-Z4-N（Z12）-CO-Z5-H，-CO-Z6-H或氢原子，其中Z4，Z5和Z6各自与Z1相同，Z12具有相同的含义如Z11; Q1和Q2各自表示羧基或膦酰氧基; Q3表示氢原子，羧基或膦氧基; m表示0或1〜20的整数， n表示0或1〜20的整数， Y1表示可含有一个或多个选自-OCOR 11和-NHCOR 12的取代基的具有1至10个碳原子的亚烷基，其中R11表示-Z13或-Z7-N（Z14）-CO-Z8-H（其中Z7和 Z 8各自具有与Z1相同的含义，Z 13和Z 14各自具有与Z 11相同的含义，R 12表示-Z 15或-Z 9 -N（Z 16）-CO-Z 10 -H（其中Z 9和Z 10各自具有相同的含义 Z1，Z15和Z16各自具有与Z11相同的含义）及其盐。该化合物通过内毒素抑制TNF衍生，因此可用于治疗多机能不足。

2. 发明授权

US5006647A Phosphorus containing disaccharide derivatives 失效
标题翻译：含磷二糖衍生物
公开(公告)号：US5006647A
公开(公告)日：1991-04-09
申请号：US162932
申请日：1988-03-02
申请人： Tsuneo Kusama , Tsunehiko Soga , Tetsuo Shiba
发明人： Tsuneo Kusama , Tsunehiko Soga , Tetsuo Shiba
IPC分类号： A61K31/70 , C07H13/06 , C07H15/04
CPC分类号： C07H13/06 , C07H15/04
摘要： A disaccharide compound represented by formula (I): ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as defined in the specification and a salt thereof are disclosed. The compound exhibits excellent antitumor activity and low toxicity and is useful as an antitumor agent.

3. 发明授权

US5134230A 2-Deoxy-2-aminoglucopyranoside derivatives 失效
标题翻译： 2-脱氧-2-氨基吡喃糖苷衍生物
公开(公告)号：US5134230A
公开(公告)日：1992-07-28
申请号：US614417
申请日：1991-01-18
申请人： Tsuneo Kusama , Tsunehiko Soga , Tetsuo Shiba
发明人： Tsuneo Kusama , Tsunehiko Soga , Tetsuo Shiba
IPC分类号： C07H13/06 , C07H15/04
CPC分类号： C07H13/06 , C07H15/04
摘要： A disaccharide compound represented by formula (I): ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as defined in the specification and a salt thereof are disclosed. The compound exhibits excellent antitumor activity and low toxicity and is useful as an antitumor agent.
摘要翻译：由式（I）表示的二糖化合物：其中R，R 1，R 2，R 3，R 4和R 5如本说明书中所定义，及其盐。该化合物具有优异的抗肿瘤活性和低毒性，可用作抗肿瘤剂。

4. 发明授权

US4681856A Muramyldipeptide active ester derivatives 失效
标题翻译：胞间二肽活性酯衍生物
公开(公告)号：US4681856A
公开(公告)日：1987-07-21
申请号：US641905
申请日：1984-08-20
申请人： Toshiyuki Hamaoka , Hiromi Fujiwara , Tsuneo Kusama
发明人： Toshiyuki Hamaoka , Hiromi Fujiwara , Tsuneo Kusama
IPC分类号： A61K38/00 , A61K39/385 , A61P35/00 , A61P37/00 , A61P37/04 , C07K9/00 , C08B37/00
CPC分类号： C07K9/005
摘要： Muramyldipeptide active ester derivatives represented by the formula: ##STR1## wherein R.sub.1 represents a straight or branched chain fatty acid residue having 2 to 30 carbon atoms; R.sub.2 represents an active ester residue; and "Acyl" represents an acyl group having 2 to 6 carbon atoms. These compounds are applicable as haptens for the immunotherapy and exhibit antitumor activity.
摘要翻译：由下式表示的杀脒基多肽活性酯衍生物：其中R 1表示具有2-30个碳原子的直链或支链脂肪酸残基; R2代表活性酯残基; “酰基”表示碳原子数2〜6的酰基。这些化合物适用于免疫治疗的半抗原，并表现出抗肿瘤活性。

5. 发明授权

US4672106A Muramylpeptide active ester derivatives 失效
标题翻译： Muramylpeptide活性酯衍生物
公开(公告)号：US4672106A
公开(公告)日：1987-06-09
申请号：US770471
申请日：1985-08-29
申请人： Toshiyuki Hamaoka , Hiromi Fujiwara , Tsuneo Kusama , Masahiro Komiya
发明人： Toshiyuki Hamaoka , Hiromi Fujiwara , Tsuneo Kusama , Masahiro Komiya
IPC分类号： A61K38/00 , A61P9/12 , A61P37/04 , C07K1/113 , C07K9/00 , A61K37/00 , A61K37/02
CPC分类号： C07K9/005
摘要： Muramylpeptide active ester derivatives represented by the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a fatty acid residue having from 2 to 10 carbon atoms; --COR.sub.2 represents an active ester group; R.sub.3 represents a fatty acid residue having from 1 to 10 carbon atoms; X represents an alanine, N-methylalanine or valine residue; "Acyl" represents a fatty acid residue having from 2 to 6 carbon atoms; and n represents an integer of from 1 to 6. These compounds are applicable as haptens for the immunotherapy and exhibit antitumor activity.
摘要翻译：由下式表示的Muramylpeptide活性酯衍生物：其中R1代表氢原子或具有2-10个碳原子的脂肪酸残基; -COR 2表示活性酯基; R3表示具有1至10个碳原子的脂肪酸残基; X表示丙氨酸，N-甲基丙氨酸或缬氨酸残基; “酰基”表示具有2至6个碳原子的脂肪酸残基; 并且n表示1〜6的整数。这些化合物适用于半抗原用于免疫治疗，并表现出抗肿瘤活性。

6. 发明授权

US4101536A Muramyldipeptide derivatives and process for the preparation thereof 失效
标题翻译：胞壁酰二肽衍生物及其制备方法
公开(公告)号：US4101536A
公开(公告)日：1978-07-18
申请号：US809245
申请日：1977-06-23
申请人： Yuichi Yamamura , Tetsuo Shiba , Ichiro Azuma , Shoichi Kusumoto , Tadamasa Hirayama , Tsuneo Kusama
发明人： Yuichi Yamamura , Tetsuo Shiba , Ichiro Azuma , Shoichi Kusumoto , Tadamasa Hirayama , Tsuneo Kusama
IPC分类号： A61K38/14 , C07K9/00 , A61K37/00 , C07G7/00
CPC分类号： C07K9/005
摘要： Muramyldipeptide derivatives of the formula: ##STR1## wherein Y represents a mycoloyl group or a synthetic higher acyl group having total carbon number of C30-C90 and having at least a branched chain of long alkyl group on the .alpha.-position thereof,Q represents an -L-alanyl-D-isoglutamine group, a -glycyl-D-isoglutamine group or an -L-seryl-D-isoglutamine group;Salts of such derivatives; the method of preparing such derivatives and their salts; the derivatives and their salts having potent immunoadjuvant activities and antitumor activity and being applicable as the agent for the immunotherapy of cancer for humans and animals.
摘要翻译：其中Y表示总碳数为C30-C90并且在其α-位上具有至少一个长烷基的支链的合成的较高级酰基，其中Y代表一个或多个烷基， -L-丙氨酰-D-异谷氨酰胺基，α-甘氨酰-D-异谷氨酸胺基或-L-丝氨酰-D-异谷氨酰胺基; 这些衍生物的销售; 制备这些衍生物及其盐的方法; 衍生物及其具有免疫功能活动和抗肿瘤活性的药物，适用于人类和动物免疫球蛋白的代理。

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