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1. 发明专利

AU5058472A ALKYL-2,3,3-TRIIODOALLYL ETHERS 未知
公开(公告)号：AU5058472A
公开(公告)日：1974-07-04
申请号：AU5058472
申请日：1972-12-28
申请人： YASUHARU SEKIZAWA , BUNZO NOMIYA , TAKEMI KOEDA , FUMIO KAI , NAOTOSHI AKAI , YASUSHI YUSA , FUGUAKI FUKUYASU
发明人： SEKIZAWA YASUHARU , NOMIYA BUNZO , KOEDA TAKEMI , KAI FUMIO , AKAI NAOTOSHI , YUSA YASUSHI , FUKUYASU FUGUAKI
IPC分类号： A23K1/16 , A23K1/18 , A01N9/24 , C07C43/14
摘要： Cpds. of formula (I): (I)2C=CICH2OR (where R is Me, Et, n-Pr), are pref. prepd. by (a) reacting propargyl alcohol (II) with a 1-3 C alkyl sulphate or sulphonate in the presence of a base to give HC triple bond CCH2OR, reacting this (or its Cu salt) with iodine and then with >=1 equiv. of iodine; or (b) reacting (II) with iodine in the presence of an alkali metal hydroxide in an inert solvent to give 2,3,3-triiodoallyl alcohol, and treating this with an alkylating agent in a polar aprotic solvent or converting it into a reactive deriv. and reacting with ROM (where M is alkali metal) or with ROH in the presence of a base.

2. 发明授权

US4474764A 3-Amino-2-hydroxy-4-phenylbutanoic acid derivatives and pharmaceutical composition containing the same 失效
标题翻译： 3-氨基-2-羟基-4-苯基丁酸衍生物和含有它们的药物组合物
公开(公告)号：US4474764A
公开(公告)日：1984-10-02
申请号：US425875
申请日：1982-09-28
申请人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Mitsugu Hachisu , Kenji Kawamura , Shunzo Fukatsu , Yasuharu Sekizawa
发明人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Mitsugu Hachisu , Kenji Kawamura , Shunzo Fukatsu , Yasuharu Sekizawa
IPC分类号： C07K5/04 , A61K31/16 , A61K38/00 , A61P25/04 , C07C237/12 , C07C237/20 , C07C237/22 , C07K5/02 , C07K14/81 , A61K37/00 , C07C101/00 , C07C101/30 , C07C101/32 , C07C101/72 , C07C103/52 , C07C123/00 , C07C149/40 , C07C149/43
CPC分类号： C07K5/0202 , Y02P20/55
摘要： New 3-N-acyl derivatives of 3-amino-2-hydroxy-4-phenylbutanoic acid are provided, which exhibit analgesic activity and are affective to enhance the morphine analgesia.
摘要翻译：提供3-氨基-2-羟基-4-苯基丁酸的新的3-N-酰基衍生物，其具有止痛活性并且有助于增强吗啡镇痛。

3. 发明授权

US4395402A Analgesic agent 失效
标题翻译：止痛药
公开(公告)号：US4395402A
公开(公告)日：1983-07-26
申请号：US303938
申请日：1981-09-21
申请人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Mitsugu Hachisu , Kenji Kawamura , Shunzo Fukatsu , Yasuharu Sekizawa
发明人： Hamao Umezawa , Tomio Takeuchi , Takaaki Aoyagi , Mitsugu Hachisu , Kenji Kawamura , Shunzo Fukatsu , Yasuharu Sekizawa
IPC分类号： A61K31/135 , A61K31/165 , A61K31/195 , A61K31/215 , A61K38/00 , A61P25/04 , C07C229/36 , C07C237/20 , C07C279/14 , C07C323/60 , C07K5/06 , A61K37/00
CPC分类号： A61K31/195 , C07K5/06043 , A61K38/00
摘要： A new analgesic agent is now provided, which comprises as the active ingredient 3-amino-2-hydroxy-4-phenylbutanoic acid and some related compounds thereof. These compounds have now found to be effective as inhibitor against enkephalinase and as an agent for enhancing analgesic activity of morphine.
摘要翻译：现在提供一种新的止痛剂，其包含作为活性成分的3-氨基-2-羟基-4-苯基丁酸及其一些相关化合物。现在发现这些化合物作为抑制脑啡肽酶和作为增强吗啡镇痛作用的药剂是有效的。

4. 发明授权

US4264532A Process for preparing D,L-2-amino-4-methylphosphinobutyric acid 失效
标题翻译：制备D，L-2-氨基-4-甲基膦酰基丁酸的方法
公开(公告)号：US4264532A
公开(公告)日：1981-04-28
申请号：US140198
申请日：1979-06-15
申请人： Takashi Tsuruoka , Akira Suzuki , Kunitaka Tachibana , Kazuko Mizutani , Yasuharu Sekizawa , Shigeharu Inouye , Tetsuo Takematsu
发明人： Takashi Tsuruoka , Akira Suzuki , Kunitaka Tachibana , Kazuko Mizutani , Yasuharu Sekizawa , Shigeharu Inouye , Tetsuo Takematsu
IPC分类号： A01N57/20 , C07F9/30 , C07F9/32
CPC分类号： C07F9/3211 , A01N57/20 , C07F9/301
摘要： PCT No. PCT/JP78/00058 Sec. 371 Date June 15, 1979 Sec. 102(e) Date June 15, 1979 PCT Field Dec. 18, 1978 PCT Pub. No. WO79/00405 PCT Pub. Date July 12, 1979This invention relates to a novel process for preparing D,L-2-amino-4-methylphosphinobutyric acid having herbicidal and antifungicidal activities which comprises subjecting acrolein to reaction with a dialkyl phosphonite to synthesize an acetal of an ester of 3-oxopropylmethylphosphinic acid; treating the thus obtained compound with an acid for deacetalization to obtain an ester of 3-oxopropylmethylphosphinic acid and then applying the Strecker's process used for amino synthesis to the thus obtained ester.
摘要翻译： PCT No.PCT / JP78 / 00058 Sec。 371日期1979年6月15日 102（e）日期1979年6月15日PCT领域1978年12月18日PCT公布。公开号WO79 / 00405 日期1979年7月12日本发明涉及一种具有除草和杀真菌活性的D，L-2-氨基-4-甲基膦酰基丁酸的新方法，该方法包括使丙烯醛与二烷基亚膦酸酯反应，合成3 - 氧代丙基甲基次膦酸用酸脱乙酰化处理得到的化合物，得到3-氧代丙基甲基次膦酸的酯，然后将用于氨基合成的斯特雷克氏法用于得到的酯。

5. 发明授权

US4189489A 5-Alkoxy-picolinic acid calcium salts and anti-hypertensive composition containing 5-alkoxy-picolinic acid calcium salts and anti-hypertensive composition thereof 失效
标题翻译：含有5-烷氧基 - 吡啶甲酸钙盐及其抗高血压组合物的5-烷氧基 - 吡啶甲酸钙盐和抗高血压组合物
公开(公告)号：US4189489A
公开(公告)日：1980-02-19
申请号：US838180
申请日：1977-09-30
申请人： Takemi Koeda , Takashi Tsuruoka , Uichi Shibata , Hiroyasu Asaoka , Mitsugu Hachisu , Osamu Itoh , Yasuharu Sekizawa , Shigeharu Inouye , Taro Niida
发明人： Takemi Koeda , Takashi Tsuruoka , Uichi Shibata , Hiroyasu Asaoka , Mitsugu Hachisu , Osamu Itoh , Yasuharu Sekizawa , Shigeharu Inouye , Taro Niida
IPC分类号： A61K31/44 , A61P9/12 , C07D213/65 , C07D213/79 , A61K31/445 , C07D213/89
CPC分类号： C07D213/79 , C07D213/65
摘要： 5-Alkoxy-picolinic acids and the salts and the esters thereof represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and M represents a hydrogen atom; a calcium atom; a sodium atom; a potassium atom; an aluminum atom; an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom); a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic acids and the salts and the esters thereof, and anti-hypertensive compositions containing the 5-alkoxy-picolinic acids and the salts and the esters thereof.
摘要翻译： 5-烷氧基 - 吡啶甲酸及其由式（I）表示的盐及其酯：其中R表示具有1至6个碳原子的烷基，M表示氢原子; 钙原子; 一个钠原子; 钾原子; 铝原子; 未取代的苯基; 被一个或多个具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基或卤素原子（例如氯，溴，碘等）原子取代的苯基; 苯酞基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷基; 或具有式“IMAGE”的酰氧基烷基，其中R 2表示氢原子或甲基，R 3表示具有1至5个碳原子的烷基（例如甲基，正丙基，异丁基，叔丁基等），基团），具有1至4个碳原子的烷氧基，苯基，被一个或多个具有1至4个碳原子的烷基取代的苯基，具有1至4个碳原子的烷氧基或卤素原子（例如氯，溴，碘等原子）或其中烷基部分具有1至3个碳原子的芳烷基，其可用作抗高血压剂，制备5-烷氧基 - 吡啶甲酸的方法和其盐和酯，以及含有5-烷氧基 - 吡啶甲酸及其盐及其酯的抗高血压组合物。

6. 发明授权

US4216226A Antiviral agent and treatment of viral infections 失效
标题翻译：抗病毒药物和病毒感染的治疗
公开(公告)号：US4216226A
公开(公告)日：1980-08-05
申请号：US910627
申请日：1978-05-30
申请人： Harumi Fukuyasu , Zenichiro Ohya , Katsuo Kawakami , Takahiko Kikuchi , Takashi Shomura , Takashi Tsuruoka , Tetsuro Watanabe , Yuzo Kazuno , Shigeharu Inouye , Yasuharu Sekizawa
发明人： Harumi Fukuyasu , Zenichiro Ohya , Katsuo Kawakami , Takahiko Kikuchi , Takashi Shomura , Takashi Tsuruoka , Tetsuro Watanabe , Yuzo Kazuno , Shigeharu Inouye , Yasuharu Sekizawa
IPC分类号： A61K31/195 , A61K31/22 , A61K31/395 , A61K31/44 , A61K31/66 , A61P31/12 , A61P31/16 , A61P31/22 , C07D213/65 , C07F9/38
CPC分类号： C07F9/3808 , A61K31/195 , A61K31/22 , A61K31/44 , A61K31/66
摘要： A new antiviral agent is now provided, which contains as the active ingredient at least one known glycine derivative of the formula: ##STR1## wherein R is a hydrogen atom, R' is a group --CH.sub.2 NH.sub.2, --CH.sub.2 NHCONH.sub.2, --CH.sub.2 NHCONHOH, --CH.sub.2 CH.sub.2 PO(OH).sub.2, ##STR2## or R and R' taken together form a group ##STR3## and R" is a hydrogen atom or a lower alkyl group, or a pharmaceutically acceptable salt of said glycine derivative. This antiviral agent is useful for therapeutic prevention and treatment of diseases caused by various kinds of viruses.
摘要翻译：现在提供一种新的抗病毒剂，其包含作为活性成分的至少一种下列通式的甘氨酸衍生物：其中R是氢原子，R'是基团-CH2NH2，-CH2NHCONH2，-CH2NHCONHOH，-CH2CH2PO （OH）2，或R和R'一起形成基团，R“是氢原子或低级烷基，或所述甘氨酸衍生物的药学上可接受的盐。该抗病毒剂可用于各种病毒引起的疾病的治疗性预防和治疗。

7. 发明授权

US4198416A 5-Alkoxy-picolinic esters and anti-hypertensive composition containing 5-alkoxy-picolinic esters 失效
标题翻译： 5-烷氧基 - 吡啶甲酸酯和含有5-烷氧基 - 吡啶甲酸酯的抗高血压组合物
公开(公告)号：US4198416A
公开(公告)日：1980-04-15
申请号：US944683
申请日：1978-09-22
申请人： Takemi Koeda , Takashi Tsuruoka , Uichi Shibata , Hiroyasu Asaoka , Mitsugu Hachisu , Osamu Itoh , Yasuharu Sekizawa , Shigeharu Inouye , Taro Niida
发明人： Takemi Koeda , Takashi Tsuruoka , Uichi Shibata , Hiroyasu Asaoka , Mitsugu Hachisu , Osamu Itoh , Yasuharu Sekizawa , Shigeharu Inouye , Taro Niida
IPC分类号： C07D213/65 , C07D213/79 , A61K31/44
CPC分类号： C07D213/79 , C07D213/65
摘要： 5-Alkoxy-picolinic esters represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and R.sub.1 represents an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms or an acetyl group; a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an alkoxyalkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an indanyl group; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic esters, and anti-hypertensive compositions containing the 5-alkoxy-picolinic esters.
摘要翻译：由式（I）表示的5-烷氧基 - 吡啶甲酸酯：其中R表示具有1至6个碳原子的烷基，R 1表示未取代的苯基; 被一个或多个具有1至4个碳原子的烷基或乙酰基取代的苯基; 苯酞基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷氧基烷基; 茚满基; 或具有式“IMAGE”的酰氧基烷基，其中R 2表示氢原子或甲基，R 3表示具有1至5个碳原子的烷基（例如甲基，正丙基，异丁基，叔丁基等），基团），具有1至4个碳原子的烷氧基，苯基，被一个或多个具有1至4个碳原子的烷基取代的苯基，具有1至4个碳原子的烷氧基或卤素原子（例如氯，溴，碘等原子）或其中烷基部分具有1〜3个碳原子的芳烷基，其可用作抗高血压剂，制备5-烷氧基 - 吡啶甲酸酯的方法和含有5-烷氧基 - 吡啶甲酸酯的抗高血压组合物。

8. 发明授权

US4229448A 5-Substituted picolinic acid derivatives and an anti-hypertensive composition containing the same 失效
标题翻译： 5-取代的吡啶甲酸衍生物和含有它们的抗高血压组合物
公开(公告)号：US4229448A
公开(公告)日：1980-10-21
申请号：US23504
申请日：1979-03-23
申请人： Yasuharu Sekizawa , Takashi Tsuruoka , Mitsugu Hachisu , Masaji Sezaki , Masashi Miyamoto , Uichi Shibata , Kazuko Mizutani , Shigeharu Inouye , Takemi Koeda , Keizo Shimomura , Taro Niida
发明人： Yasuharu Sekizawa , Takashi Tsuruoka , Mitsugu Hachisu , Masaji Sezaki , Masashi Miyamoto , Uichi Shibata , Kazuko Mizutani , Shigeharu Inouye , Takemi Koeda , Keizo Shimomura , Taro Niida
IPC分类号： C07D213/65 , C07D213/79 , C07D213/81 , A61K31/455
CPC分类号： C07D213/79 , C07D213/65 , C07D213/81
摘要： 5-Substituted picolinic acid derivatives represented by the formula (I): ##STR1## wherein R.sub.1 represents a straight or branched chain halogen-substituted alkyl group having 2 to 6 carbon atoms or a substituted phenyl group having the formula ##STR2## wherein R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, an N-alkyl-substituted amino group, an acylamino group, an acetyl group, an acyloxy group, a hydroxy group or a halogen-substituted alkyl group or R.sub.3 and R.sub.4, when taken together, represent a polymethylene chain; and R.sub.2 represents an --OM group wherein M represents a hydrogen, sodium, potassium, calcium, aluminium or magnesium atom, a straight or branched chain or cyclic alkoxy group having 1 to 6 carbon atoms, an aminoalkoxy group, a phenoxy group, a substituted phenoxy group, a 5-indanyloxy group, an acyloxyalkyloxy group having the formula ##STR3## wherein R.sub.5 represents a hydrogen atom or a methyl group and R.sub.6 represents a lower alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group, or an amino group represented by the formula ##STR4## wherein R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a phenyl group which are useful as anti-hypertensive agents, a process for preparing the above 5-substituted picolinic acid derivatives, and anti-hypertensive compositions containing the same.
摘要翻译：由式（I）表示的5-取代的吡啶甲酸衍生物：其中R 1表示具有2至6个碳原子的直链或支链卤素取代的烷基或具有下式的取代苯基：其中可以相同或不同的R 3和R 4各自表示氢原子，卤素原子，低级烷基，低级烷氧基，硝基，氨基，N-烷基取代的氨基，酰氨基，乙酰基，酰氧基，羟基或卤素取代的烷基，或者R 3和R 4一起表示聚亚甲基链; R 2表示-OM基，其中M表示氢，钠，钾，钙，铝或镁原子，具有1至6个碳原子的直链或支链或环状烷氧基，氨基烷氧基，苯氧基，取代的苯氧基，5-茚满氧基，具有式“IMAGE”的酰氧基烷氧基，其中R5表示氢原子或甲基，R6表示碳原子数1〜6的低级烷基，苯基或取代苯基或由式“IMAGE”表示的氨基，其中R7和R8可以相同或不同，表示可用作抗高血压剂的氢原子，低级烷基或苯基，制备上述5-取代的吡啶甲酸衍生物的方法和含有它们的抗高血压组合物。

9. 发明授权

US4418070A Cardiotonic agents 失效
标题翻译：强心剂
公开(公告)号：US4418070A
公开(公告)日：1983-11-29
申请号：US345672
申请日：1982-02-04
申请人： Tsuneo Okonogi , Shunzo Fukatsu , Mitsugu Hachisu , Hiroko Kawashima , Keiko Shitoh , Yasuharu Sekizawa
发明人： Tsuneo Okonogi , Shunzo Fukatsu , Mitsugu Hachisu , Hiroko Kawashima , Keiko Shitoh , Yasuharu Sekizawa
IPC分类号： A61K31/425 , A61K31/426 , A61P9/04 , C07D277/20 , C07D277/22 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40
CPC分类号： A61K31/425 , C07D277/34
摘要： A 5-phenylthiazole derivative represented by the formula: ##STR1## wherein R represents a hydrogen atom, a lower alkyl group, a hydroxyl group, an amino group or a mercapto group, or a pharmaceutically acceptable salt thereof shows a cardiac effect and a low toxicity to a human or animal with little influence on atrium rhythms.
摘要翻译：其中R表示氢原子，低级烷基，羟基，氨基或巯基的5-苯基噻唑衍生物或其药学上可接受的盐显示心脏效应和低对人或动物的毒性，对心房节律几乎没有影响。

10. 发明授权

US3932668A Composition for treating swine scour 失效
标题翻译：猪冲洗用组合物
公开(公告)号：US3932668A
公开(公告)日：1976-01-13
申请号：US531415
申请日：1974-12-10
申请人： Yasuharu Sekizawa , Shigeo Seki , Bunzo Nomiya , Takemi Koeda , Fumio Kai , Naotoshi Akai , Yasushi Yusa , Fuguaki Fukuyasu
发明人： Yasuharu Sekizawa , Shigeo Seki , Bunzo Nomiya , Takemi Koeda , Fumio Kai , Naotoshi Akai , Yasushi Yusa , Fuguaki Fukuyasu
IPC分类号： A23K1/16 , A23K1/18 , A61K31/08
CPC分类号： A23K50/30 , A23K20/105
摘要： Novel alkyl 2,3,3-triiodoallyl ethers useful as disinfectants are provided by an addition reaction of alkyl-3-iodo-2-propinyl ethers with iodine. The starting alkyl-3-iodo-2-propinyl ethers can be prepared by a new process comprising an alkylation of propargyl alcohol with an alkyl sulfate or alkyl sulfonate in the presence of an alkali, followed by monoiodization of the resulting alkyl-2-propinyl ether. This invention also provides a composition comprising alkyl 2,3,3-triiodoalkyl ethers useful as a poultry feed additive having growth increasing effects and for treating swine scours.
摘要翻译：用作消毒剂的新型烷基2,3,3-三碘代烯丙基醚通过烷基-3-碘-2-丙炔基醚与碘的加成反应来提供。起始的烷基-3-碘-2-丙炔基醚可以通过一种新方法制备，该方法包括在碱存在下用炔丙醇与烷基硫酸盐或烷基磺酸盐烷基化，然后将所得的烷基-2-丙炔基醚。本发明还提供一种组合物，其包含可用作具有生长增加作用的禽饲料添加剂的烷基2,3,3-三碘烷基醚和用于治疗猪冲洗液的组合物。

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