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1. 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。

2. 发明授权

US4369178A Glucosamine peptide derivatives, their production and use 失效
标题翻译：葡萄糖胺衍生物，其生产和使用
公开(公告)号：US4369178A
公开(公告)日：1983-01-18
申请号：US123401
申请日：1980-02-21
申请人： Yuichi Yamamura , Ichiro Azuma , Shigeru Kobayashi
发明人： Yuichi Yamamura , Ichiro Azuma , Shigeru Kobayashi
IPC分类号： A61K31/70 , A61K31/7024 , A61K31/7028 , A61K38/00 , A61K39/39 , A61P35/00 , A61P37/00 , A61P37/04 , C07H13/04 , C07H13/08 , C07H15/04 , C07H15/18 , C07K1/113 , C07K9/00 , A61K37/00 , C07C103/52
CPC分类号： C07K9/005
摘要： Novel glucosamine-peptide derivatives of the formula: ##STR1## wherein m is 0 or 1;n is 0 or an integer of 1 to 9;R is lower alkyl which may be substituted with hydroxyl, or aryl;R.sup.1 is hydrogen or acyl having an acyclic hydrocarbon group, the terminal of which may be substituted with a cyclic hydrocarbon group directly, via a carbonyl group or via an oxygen atom;provided that when R.sup.1 is hydrogen m is 1;R.sup.2 is hydrogen or lower alkyl which may form a ring by connecting its terminal with the .alpha.-nitrogen atom whenn is 0, or hydrogen when n is an integer of 1 to 9;R.sup.3 is hydrogen or lower alkyl;R.sup.4 and R.sup.5 are each hydrogen or lower alkyl which may be substituted with hydroxyl or benzyloxyl;R.sup.6 is hydrogen or lower alkyl;R.sup.7 is alkyl which may be substituted with lower alkoxyl or aralkyl;R.sup.8 and R.sup.9 are each hydrogen, lower alkyl or aralkyl; and(D) and (L) each indicate configurations if their respective carbon atoms are asymmetric;or an acid addition salt thereof, have immunostimulatory activity.
摘要翻译：下式的新型葡糖胺肽衍生物：其中m为0或1; n为0或1〜9的整数。 R是可被羟基或芳基取代的低级烷基; R1是氢或具有非环状烃基的酰基，其末端可以被环状烃基直接经由羰基或氧原子取代; 条件是当R1为氢时m为1; R2为氢或低级烷基，当n为0时，可通过将其末端与α-氮原子连接而形成环，或当n为1〜9的整数时为氢; R3是氢或低级烷基; R4和R5各自为氢或可被羟基或苄氧基取代的低级烷基; R6是氢或低级烷基; R7是可被低级烷氧基或芳烷基取代的烷基; R8和R9各自为氢，低级烷基或芳烷基; 和（D）和（L）各自表示构型，如果它们各自的碳原子是不对称的; 或其酸加成盐具有免疫刺激活性。

3. 发明授权

US4191778A Aqueous immunoregulatory agent 失效
标题翻译：水性免疫调节剂
公开(公告)号：US4191778A
公开(公告)日：1980-03-04
申请号：US766505
申请日：1977-02-07
申请人： Yuichi Yamamura , Ichiro Azuma , Kazuhisa Sugimura , Hiroshi Morimoto , Isuke Imada , Masazumi Watanabe
发明人： Yuichi Yamamura , Ichiro Azuma , Kazuhisa Sugimura , Hiroshi Morimoto , Isuke Imada , Masazumi Watanabe
IPC分类号： A61K31/12 , A61K31/122 , A61K31/19 , A61K39/39 , A61P37/00 , A61P37/04
CPC分类号： A61K31/19 , Y10S514/869 , Y10S514/87
摘要： The aqueous preparation such as an aqueous solution, a water-in-oil emulsion, in which a water-soluble salt of the quinonyl acid derivative of the formula: ##STR1## [wherein each R is a lower alkoxy group having 1 to 4 carbon atoms or the two R's, taken together, represent a group of --CH.dbd.CH--CH.dbd.CH--; --A--COOH means ##STR2## when both R's are lower alkoxy groups, or --(CH.sub.2).sub.n COOH (wherein n is an integer from 1 to 8) when two R's, taken together, represent a group of --CH.dbd.CH--CH.dbd.CH--] is dissolved in aqueous phase, shows an excellent immunoregulatory activity in animals including human being.
摘要翻译：水性制剂如水溶液，油包水乳液，其中下式的醌基酸衍生物的水溶性盐：其中每个R是具有1-4个碳原子的低级烷氧基原子或两个R一起表示-CH = CH-CH = CH-的基团; 当两个R一起表示-CH = CH-CH的基团时，-A-COOH表示两个R均为低级烷氧基或 - （CH 2）n COOH（其中n为1至8的整数） = CH-]溶解在水相中，在包括人的动物中显示出优异的免疫调节活性。

4. 发明授权

US4606857A Muramyldipeptide derivatives 失效
标题翻译：胞壁酰二肽衍生物
公开(公告)号：US4606857A
公开(公告)日：1986-08-19
申请号：US517551
申请日：1983-07-27
申请人： Akira Hasegawa , Ichiro Azuma , Yuichi Yamamura
发明人： Akira Hasegawa , Ichiro Azuma , Yuichi Yamamura
IPC分类号： A61K38/00 , A61K39/39 , A61P37/04 , C07H15/04 , C07H15/14 , C07K9/00
CPC分类号： C07K9/005
摘要： Muramyldipeptide derivatives represented by the formula: ##STR1## wherein Ala represents alanine; Acyl represents an acyl group; R.sub.1 and R.sub.2 each represents a hydrogen atom or, when taken together, may form an alkylidene group; R.sub.3 represents a hydrogen atom, an acyl group or an alkyl group; and R.sub.4 represents a hydrogen atom or an alkyl group. These compounds have excellent immunoadjuvant activity, prophylactic and therapeutic effects against microbial infections, and antitumor activity.
摘要翻译：由下式表示的乳糖基二肽衍生物：其中Ala表示丙氨酸; 酰基表示酰基; R 1和R 2各自表示氢原子，或者一起可以形成亚烷基; R3表示氢原子，酰基或烷基; R4表示氢原子或烷基。这些化合物具有优异的免疫佐剂活性，对微生物感染的预防和治疗作用以及抗肿瘤活性。

5. 发明授权

US4543253A Solidified pharmaceutical composition comprising cell wall skeleton 失效
标题翻译：包含细胞壁骨架的凝固药物组合物
公开(公告)号：US4543253A
公开(公告)日：1985-09-24
申请号：US930409
申请日：1978-08-02
申请人： Yuichi Yamamura , Ichiro Azuma , Katsusuke Ennyu , Osamu Aoki
发明人： Yuichi Yamamura , Ichiro Azuma , Katsusuke Ennyu , Osamu Aoki
IPC分类号： A61K39/39 , A61K9/00 , A61K9/14 , A61K9/19 , A61K35/74 , A61K47/00 , A61K47/14 , A61K47/26 , A61P35/00 , A61K37/00
CPC分类号： A61K35/74 , A61K47/14 , A61K47/26 , A61K9/0019 , A61K2039/55566 , A61K2039/55583 , A61K2039/55594 , A61K9/19
摘要： A stable, storable pharmaceutical composition is provided which comprises a dehydrated solid mixture of microbial cell wall skeleton, vehicle oil, suspending agent and dispersing agent; wherein said microbial cell wall skeleton has adjuvant and antitumor activity. The composition is easily prepared, stable to long term storage, and easily reconstituted to form a homogeneous suspension which retains high potency.
摘要翻译：提供了一种稳定的，可储存的药物组合物，其包含微生物细胞壁骨架，载体油，悬浮剂和分散剂的脱水固体混合物; 其中所述微生物细胞壁骨架具有佐剂和抗肿瘤活性。组合物容易制备，长期保存稳定，并易于重构以形成保持高效力的均匀悬浮液。

6. 发明授权

US4314998A 6-Deoxyglucosamine-peptide derivatives, their production and use 失效
标题翻译： 6-脱氧葡糖胺肽衍生物，其生产和使用
公开(公告)号：US4314998A
公开(公告)日：1982-02-09
申请号：US123812
申请日：1980-02-22
申请人： Yuichi Yamamura , Akira Hasegawa , Ichiro Azuma , Shigeru Kobayashi
发明人： Yuichi Yamamura , Akira Hasegawa , Ichiro Azuma , Shigeru Kobayashi
IPC分类号： C07H15/04 , C07K9/00 , A61K37/00 , A61K37/02 , C07C103/52
CPC分类号： C07H15/04 , C07K9/005
摘要： Novel 6-deoxyglucosamine-peptide derivatives of the formula ##STR1## wherein R is hydrogen or an organic acid residue or alkoxycarbonyl;R.sup.1 is hydrogen or acyl;R.sup.2 is hydrogen or lower alkyl;R.sup.3 and R.sup.4 are each hydrogen or lower alkyl which may be substituted with hydroxyl;R.sup.5 and R.sup.6 are each carboxyl which may be esterified or amidated;R.sup.7 is hydrogen or aralkyl; and(D) and (L) each indicate configurations if theirrespective carbon atoms are asymmetric or a salt thereof having immunostimulatory activity.
摘要翻译：新颖的6-脱氧葡糖胺肽衍生物，其中R为氢或有机酸残基或烷氧基羰基; R1是氢或酰基; R2是氢或低级烷基; R3和R4各自为氢或可被羟基取代的低级烷基; R5和R6各自为可被酯化或酰胺化的羧基; R7是氢或芳烷基; 和（D）和（L）各自表示各自的碳原子不对称的构型或其具有免疫刺激活性的盐。

7. 发明授权

US4243663A Glycolipid compositions for transplanted tumor immunotherapy 失效
标题翻译：用于移植肿瘤免疫治疗的糖脂组合物
公开(公告)号：US4243663A
公开(公告)日：1981-01-06
申请号：US931050
申请日：1978-08-04
申请人： Ichiro Azuma , Yuichi Yamamura
发明人： Ichiro Azuma , Yuichi Yamamura
IPC分类号： A61K31/70 , A61K35/74 , A61K39/00 , A61K39/39 , C07H13/06 , C12P19/00 , C07H13/02 , A61K31/71 , A61K31/72
CPC分类号： C07H13/06 , A61K31/70 , A61K35/74 , A61K39/39 , C12P19/00 , A61K2039/55511 , A61K2039/55572
摘要： A composition which is capable of specifically inducing an immunity when administered into the body of a host in association with a tumor antigen, or which is capable of non-specifically enhancing an immunizing function when administered into the body of a tumor-carrying host, comprising a glycolipid as active ingredient in association with a pharmaceutically acceptable carrier, wherein the saccharide moiety of the glycolipid is selected from the group consisting of fructose, glucose and sucrose.
摘要翻译：当与肿瘤抗原结合施用于宿主体内时能够特异性诱导免疫的组合物，或当被施用于携带肿瘤的宿主的体内能够非特异性增强免疫功能的组合物，其包含糖脂作为活性成分与药学上可接受的载体结合，其中糖脂的糖部分选自果糖，葡萄糖和蔗糖。

8. 发明授权

US07534443B1 Preparations for immunotherapy for cancer having bacterial somatic constituent as the active ingredient 失效
标题翻译：用于具有细菌体细胞成分作为活性成分的癌症的免疫治疗的制剂
公开(公告)号：US07534443B1
公开(公告)日：2009-05-19
申请号：US09743750
申请日：1999-07-16
申请人： Ichiro Azuma , Norio Hamamatsu , Toshio Fujinaga
发明人： Ichiro Azuma , Norio Hamamatsu , Toshio Fujinaga
IPC分类号： A61K39/04 , A61K45/00 , A61K39/38 , A61K39/02
CPC分类号： A61K47/183 , A61K9/0019 , A61K9/107 , A61K9/19 , A61K35/74 , A61K39/0011 , A61K39/39 , A61K2039/52 , A61K2039/55505 , A61K2039/55566 , A61K2039/55577 , A61K2039/55583 , A61K2039/55594
摘要： An oil-in-water emulsion that comprise a bacterial component as an active ingredient as well as essentially an oil, surfactant, and a stabilizer, and that can be used as an agent for immunotherapy, and the preparation therefor are provided.
摘要翻译：提供了包含作为活性成分的细菌成分以及基本上油，表面活性剂和稳定剂并且可以用作免疫治疗剂的水包油型乳剂及其制备方法。

9. 发明申请

US20050002951A1 Novel method of inducing antigen-specific t cells 审中-公开
标题翻译：诱导抗原特异性T细胞的新方法
公开(公告)号：US20050002951A1
公开(公告)日：2005-01-06
申请号：US10490865
申请日：2002-09-27
申请人： Haruo Sugiyama , Ichiro Azuma
发明人： Haruo Sugiyama , Ichiro Azuma
IPC分类号： A61K39/00 , A61P35/00 , A61K39/02
CPC分类号： A61K39/0011 , A61K2039/545 , A61K2039/55594
摘要： The present invention provides a novel method for inducing antigen-specific T cells. A method for inducing antigen-specific T cells in a patient comprising administering to said patient in need thereof composition (a) which comprises a therapeutically effective amount of an antigen protein or an antigen peptide as an active ingredient, and composition (b) which comprises a therapeutically effective amount of a cell wall skeleton integrant of the BCG strain of Mycobacterium bovis as an active ingredient, wherein composition (b) is administered in advance and then composition (a) is administered, and related pharmaceutical compositions are provided.
摘要翻译：本发明提供了诱导抗原特异性T细胞的新方法。一种用于在患者中诱导抗原特异性T细胞的方法，包括向所述需要的患者施用组合物（a），其包含治疗有效量的作为活性成分的抗原蛋白或抗原肽，以及组合物（b），其包含治疗有效量的牛分枝杆菌BCG菌株的细胞壁骨架组合物作为活性成分，其中组合物（b）预先施用，然后施用组合物（a），并提供相关的药物组合物。

10. 发明授权

US5945483A High solids content resin composition, high solids content type paint, and painting process using the same 失效
标题翻译：高固含量树脂组合物，高固含量型油漆，以及使用其的涂装工艺
公开(公告)号：US5945483A
公开(公告)日：1999-08-31
申请号：US921573
申请日：1997-09-29
申请人： Goro Iwamura , Shigeki Matsui , Ichiro Azuma , Yoshiaki Marutani , Hiroyuki Uemura , Shinji Sasaki , Kazuhi Koga
发明人： Goro Iwamura , Shigeki Matsui , Ichiro Azuma , Yoshiaki Marutani , Hiroyuki Uemura , Shinji Sasaki , Kazuhi Koga
IPC分类号： C08G18/40 , C08G18/62 , C08L33/14 , C08L43/04 , C08L61/28 , C08L75/04 , C09D133/14 , C09D143/04 , C09D161/20 , C09D167/00 , C09D175/04
CPC分类号： C09D133/14 , C08G18/4063 , C08G18/62 , C08G18/6225 , C08L33/14 , C08L43/04 , C09D143/04 , C08L61/28 , C08L75/04
摘要： There are disclosed a high solids content resin composition excellent in solubility in an organic solvent, comprising an acrylic oligomer having a blocked hydroxyl group, a curing agent having a reactivity with a hydroxyl group and a dissociation or curing catalyst, and a high solids content type paint using the resin composition. There are also disclosed a coating process and a baking process comprising coating and baking the resin composition or the paint while rotating a material to be coated at an appropriate speed. The resin composition and the paint of the present invention have substantially no sagging and solvent popping. Further, the thus obtained paint film have improved smoothness, solvent resistance, weather resistance and resistance to scratching.
摘要翻译：公开了一种在有机溶剂中溶解性优异的高固含量树脂组合物，其包含具有封端羟基的丙烯酸低聚物，与羟基具有反应性的固化剂和解离或固化催化剂，以及高固含量型油漆使用树脂组合物。还公开了一种涂覆方法和烘烤方法，包括在以适当的速度旋转待涂覆的材料的同时涂覆和烘烤树脂组合物或涂料。本发明的树脂组合物和涂料基本上没有下垂和溶剂挥发。此外，由此获得的涂膜具有改善的平滑性，耐溶剂性，耐候性和耐擦伤性。

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