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11. 发明授权

US4939145A Phenothiazone derivatives and analogs 失效
标题翻译：吩噻嗪衍生物和类似物
公开(公告)号：US4939145A
公开(公告)日：1990-07-03
申请号：US298716
申请日：1989-01-19
申请人： Cheuk K. Lau , Joshua Rokach , Christiane Yoakim , Rejean Fortin , Yvan Guindon
发明人： Cheuk K. Lau , Joshua Rokach , Christiane Yoakim , Rejean Fortin , Yvan Guindon
IPC分类号： A61K31/495 , A61K31/535 , A61K31/54 , C07C46/06 , C07D241/46 , C07D265/34 , C07D265/38 , C07D279/18 , C07D279/34 , C07D279/36 , C07D293/10
CPC分类号： C07D293/10 , A61K31/495 , A61K31/535 , A61K31/54 , C07C46/06 , C07D241/46 , C07D265/34 , C07D265/38 , C07D279/18 , C07D279/34 , C07D279/36
摘要： Phenothiazone derivatives and analogs thereof, pharmaceutical compositions and methods of treatment are disclosed. These compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.
摘要翻译：苯并噻唑衍生物及其类似物，药物组合物和治疗方法。这些化合物可用作哺乳动物白细胞三烯生物合成的抑制剂。因此，这些化合物是治疗过敏性疾病，哮喘，心血管疾病和炎症的有用的治疗剂。

12. 发明授权

US4818441A Quinine derivatines 失效
标题翻译：奎宁衍生物
公开(公告)号：US4818441A
公开(公告)日：1989-04-04
申请号：US165009
申请日：1980-07-01
申请人： Isuke Imada , Shinji Terao , Mitsuru Kawada , Mitsuru Shiraishi
发明人： Isuke Imada , Shinji Terao , Mitsuru Kawada , Mitsuru Shiraishi
IPC分类号： A61K31/12 , A61K31/20 , A61P3/02 , A61P9/00 , A61P9/12 , A61P11/08 , C07C41/26 , C07C43/23 , C07C45/00 , C07C45/71 , C07C46/02 , C07C46/06 , C07C46/10 , C07C47/277 , C07C50/14 , C07C50/26 , C07C50/28 , C07C50/32 , C07C50/38 , C07C51/00 , C07C66/00 , C07C67/00 , C07C50/02
CPC分类号： C07C66/00 , C07C41/26 , C07C41/48 , C07C45/71 , C07C46/02 , C07C46/06 , C07C46/10 , C07C47/277 , C07C50/28 , C07C50/32 , C07C50/38
摘要： A compound of the general formul: ##STR1## wherein .alpha. .beta. means a saturated bond or a double bond; each R independently of one another is a methyl group or a methoxy group, or two R's taken together represent a group of --CH.dbd.CH--CH.dbd.CH--; n is zero or an integer of 1 through 9; when .alpha. .beta. is a saturated bond, R.sub.2 is a hydrogen atom or hydroxyl group, and when .alpha. .beta. is a double bond, R.sub.2 is a hydrogen atom; when .alpha. .beta. is a double bond or when R.sub.2 is a hydroxyl group, R.sub.1 is a carboxyl group, a group of CH.sub.2.sub.2m OH (wherein m is an integer of 1 through 3) or a group of ##STR2## (wherein m is an integer of 1 through 3); when .alpha. .beta. is a saturated bond and R.sup.2 is a hydrogen atom, R.sub.1 is a hydroxymethyl group or a group of ##STR3## (wherein m is an integer of 1 through 3) has pharmacological actions such as membrane stabilizing activity (e.g. lysosomal membrane stabilizing activity), mitochondrial electron transport activity, hypotensive activity, activity to inhibit cardiac hypertrophy, tracheal muscle relaxant activity, cerebral circulation improving activity and cerebral ischemia preventive activity and is of value in the prophylaxis and treatment of hypertension, cardiac failure, asthma, cerebral apoplexy and other diseases, as a cardiac failure remedy, bronchodilator, cerebral circulation improving agent or the like.
摘要翻译：一般化合物的化合物：其中αβ表示饱和键或双键; 每个R彼此独立地是甲基或甲氧基，或两个R一起表示-CH = CH-CH = CH-的基团; n为0或1〜9的整数; 当αβ是饱和键时，R2是氢原子或羟基，当αβ是双键时，R2是氢原子; 当αβ是双键时，或当R2是羟基时，R1是羧基，CH22mOH（其中m是1至3的整数）或一组（其中m是 1〜3）; 当αβ为饱和键且R 2为氢原子时，R 1为羟甲基或一组（其中m为1至3的整数）具有药物作用如膜稳定活性（例如溶酶体膜稳定活性），线粒体电子传递活性，降血压活性，抑制心脏肥大的活性，气管肌松弛剂活性，脑循环改善活性和脑缺血预防活性，并且在预防和治疗高血压，心力衰竭，哮喘，脑中风中具有价值和其他疾病，作为心力衰竭治疗，支气管扩张剂，脑循环改善剂等。

13. 发明授权

US4393075A Quinone compounds and their use in suppressing the production of SRS-A in mammals 失效
标题翻译：喹诺酮类化合物及其在抑制哺乳动物SRS-A生产中的应用
公开(公告)号：US4393075A
公开(公告)日：1983-07-12
申请号：US248042
申请日：1981-03-26
申请人： Shinji Terao , Mitsuru Shiraishi , Yoshitaka Maki
发明人： Shinji Terao , Mitsuru Shiraishi , Yoshitaka Maki
IPC分类号： C07C43/225 , C07C43/23 , C07C45/29 , C07C46/00 , C07C46/02 , C07C46/06 , C07C47/277 , C07C50/06 , C07C50/14 , C07C50/28 , C07C50/32 , C07C59/64 , C07C59/82 , C07C66/00 , C07D295/18 , C07D295/185 , C07D307/12 , C07D309/12 , A61K31/12 , A61K31/275 , C07C50/00
CPC分类号： C07D295/185 , C07C43/225 , C07C43/23 , C07C45/29 , C07C46/00 , C07C46/02 , C07C46/06 , C07C47/277 , C07C50/06 , C07C50/14 , C07C50/28 , C07C50/32 , C07C59/64 , C07C66/00 , C07D307/12 , C07D309/12 , Y10S514/826
摘要： New quinone compounds of the formula: ##STR1## wherein R.sup.1 is methyl or methoxy, or the two R.sup.1 groups jointly represent --CH.dbd.CH--CH.dbd.CH--; X is --CH.dbd.CH-- or --C.dbd.C--; Y.sup.1 is hydrogen, hydroxyl, carboxyl, cyano, acyloxy or --COZ in which Z is amino which may be substituted; m is zero or an integer of 1 to 3; n is zero or an integer of 1 to 10; n' is an integer of 1 to 5; k is an integer of 1 to 3; and when k is 2 or 3, n' is optionally variable within the range of 1 to 5 in each occurrence of the --X--(CH.sub.2).sub.n' group; and their hydroquinone forms and salts, have useful physiological activities such as antiasthmatic, antiallergic and bloodpressure decreasing activities.
摘要翻译：下式的新醌化合物：其中R 1是甲基或甲氧基，或两个R 1基团共同表示-CH = CH-CH = CH-; X是-CH = CH-或-C = C-; Y1是氢，羟基，羧基，氰基，酰氧基或-COZ，其中Z是可以被取代的氨基; m为0或1〜3的整数; n为0或1〜10的整数， n'为1〜5的整数， k为1〜3的整数，并且当k为2或3时，n'任选地在-X-（CH 2）n'基团的每次出现中在1至5的范围内可变; 和它们的氢醌形式和盐具有有用的生理活性，如抗哮喘，抗过敏和减压活性。

14. 发明授权

US4208340A Substituted ortho-quinones and derivatives 失效
标题翻译：取代的邻醌和衍生物
公开(公告)号：US4208340A
公开(公告)日：1980-06-17
申请号：US955930
申请日：1978-10-30
申请人： Richard J. Lee
发明人： Richard J. Lee
IPC分类号： A01N35/06 , C07C46/00 , C07C46/06 , C07C50/02 , C07C50/08 , C07C50/24 , C07F9/6571 , C08F8/06 , C09K15/06 , C07C49/62 , C07C49/73 , C07C49/735
CPC分类号： C09K15/06 , A01N35/06 , C07C46/00 , C07C46/06 , C07C50/02 , C07C50/08 , C07C50/24 , C07F9/657127 , C08G65/34 , C08G65/38
摘要： Ortho-quinones with alkyl, olefin polymer, or halogen substituents and a process for the preparation of these compounds comprising a base catalyzed halogen oxidation of alkylated phenol.
摘要翻译：具有烷基，烯烃聚合物或卤素取代基的正 - 醌和用于制备这些化合物的方法包括烷基化苯酚的碱催化卤素氧化。

15. 发明授权

US4199531A Intermediates for the production of quinones 失效
标题翻译：用于生产醌的中间体
公开(公告)号：US4199531A
公开(公告)日：1980-04-22
申请号：US840806
申请日：1977-10-11
申请人： Shinji Terao , Kaneyoshi Kato
发明人： Shinji Terao , Kaneyoshi Kato
IPC分类号： C07C37/055 , C07C39/19 , C07C39/225 , C07C46/00 , C07C46/02 , C07C46/06 , C07C46/10 , C07C50/28 , C07C317/18 , C07D303/22 , C07D303/24 , C07D303/32 , C07C147/06 , C07C43/22 , C07C147/14
CPC分类号： C07D303/22 , C07C317/18 , C07C37/055 , C07C46/00 , C07C46/02 , C07C46/06 , C07C46/10 , C07C50/28 , C07D303/24 , C07D303/32
摘要： A novel method for producing hydroquinone and quinone derivatives by a regio- and stereo-specific coupling reaction of hydroquinone derivative having a terminal activated (poly)prenyl side chain with a prenyl derivative. This method can provide in good yield various hydroquinone and quinone derivatives having any prenyl length of the side chain.
摘要翻译：一种通过具有末端活化（聚）异戊烯基侧链与异戊烯基衍生物的氢醌衍生物的区域和立体特异性偶合反应制备氢醌和醌衍生物的新方法。该方法可以很好地提供具有侧链的任何异戊烯基长度的各种氢醌和醌衍生物。

16. 发明授权

US4151177A Synthesis of optically active vitamin E 失效
公开(公告)号：US4151177A
公开(公告)日：1979-04-24
申请号：US895424
申请日：1978-04-12
申请人： Noal Cohen , Gabriel Saucy
发明人： Noal Cohen , Gabriel Saucy
IPC分类号： C07C37/00 , C07C37/07 , C07C39/11 , C07C46/06 , C07C50/28 , C07D307/33 , C07D311/58 , C07D311/72 , C07D317/20 , C07D317/26 , C07D317/30 , C07D493/08 , C07D493/10 , C07D317/10
CPC分类号： C07D307/33 , C07C37/07 , C07C37/50 , C07C46/06 , C07D311/58 , C07D311/72 , C07D317/20 , C07D317/26 , C07D317/30 , C07D493/08 , C07D493/10 , C07B2200/07
摘要： Synthesis of optically active vitamin E from 2-methyl-5-oxotetrahydro-2-furoic acid including intermediates in this synthesis.

17. 发明授权

US4139545A Aralkyl carboxylic acid compounds 失效
标题翻译：芳烷基羧酸化合物
公开(公告)号：US4139545A
公开(公告)日：1979-02-13
申请号：US573158
申请日：1975-04-30
申请人： Hiroshi Morimoto , Isuke Imada , Masazumi Watanabe , Mitsuru Kawada
发明人： Hiroshi Morimoto , Isuke Imada , Masazumi Watanabe , Mitsuru Kawada
IPC分类号： C07C69/95 , A61K31/19 , A61K31/215 , A61P37/02 , A61P37/04 , A61P37/06 , C07C37/00 , C07C37/07 , C07C37/50 , C07C39/11 , C07C45/54 , C07C45/67 , C07C46/00 , C07C46/06 , C07C49/82 , C07C49/84 , C07C50/28 , C07C50/38 , C07C51/00 , C07C59/52 , C07C59/64 , C07C59/90 , C07C65/40 , C07C66/00 , C07C67/00 , C07C301/00 , C07C303/22 , C07C309/42
CPC分类号： C07C66/00 , C07C37/002 , C07C37/50 , C07C39/11 , C07C45/54 , C07C45/673 , C07C46/00 , C07C46/06 , C07C49/82 , C07C49/84 , C07C50/28 , C07C50/38 , C07C59/52 , C07C59/64 , C07C59/90 , C07C65/40 , Y10S514/885
摘要： Novel compounds of the formulae ##STR1## wherein R represents lower alkyl or lower alkoxy, A represents --CH.sub.2 --, --CO-- or ##STR2## n represents an integer of 1 to 8, X represents hydrogen or hydroxyl which may be protected and Y represents hydroxyl which may be protected, and their esters show an excellent action on the lysosomal membranes of cells, and exhibit excellent pharmacological activities such as physiologic host defense control activity, especially immuno-potentiating activity.
摘要翻译：式中，R表示低级烷基或低级烷氧基，A表示-CH 2 - ， - CO-或者n表示1〜8的整数，X表示可以被保护的氢或羟基，Y表示可被保护的羟基，它们的酯对细胞的溶酶体膜表现出优异的作用，并表现出优异的药理活性，例如生理宿主防御控制活性，特别是免疫增强活性。

18. 发明授权

US4070382A Intermediates for polycyclic quinoid antibiotics 失效
标题翻译：多环喹诺酮类抗生素中间体
公开(公告)号：US4070382A
公开(公告)日：1978-01-24
申请号：US632939
申请日：1975-11-18
申请人： Andrew S. Kende , John E. Mills , Yuh-Geng Tsay
发明人： Andrew S. Kende , John E. Mills , Yuh-Geng Tsay
IPC分类号： C07C69/013 , A61K31/12 , A61K31/215 , A61K31/22 , A61P35/00 , C07C45/00 , C07C46/00 , C07C46/02 , C07C46/06 , C07C50/26 , C07C50/36 , C07C50/38 , C07C67/00 , C07C69/017 , C07C87/10
CPC分类号： C07C46/02 , C07C46/00 , C07C46/06
摘要： There is provided a novel method of synthesizing certain tetracyclic quinones. In particular, there is provided a novel route to the synthesis of (.+-.)-7-deoxydaunomycinone and analogs thereof, which includes the provision of novel tri- and tetracyclic quinone intermediates. The -7-deoxydaunomycinone derived from naturally occurring daunomycin is a known compound, which is itself an intermediate in the preparation of the clinically accepted anti-tumor antibiotics daunomycine and its derivative adriamycin.
摘要翻译：提供合成某些四环醌的新方法。特别地，提供了（+/-） - 7-脱氧果多霉素酮及其类似物的合成的新途径，其包括提供新的三环和四环醌中间体。衍生自天然道诺霉素的7-脱氧菌多霉素是已知的化合物，其本身是制备临床接受的抗肿瘤抗生素柔红霉素及其衍生物阿霉素的中间体。

19. 发明授权

US4062879A Process for synthesis of coenzyme Q compounds 失效
标题翻译：合成辅酶Q化合物的方法
公开(公告)号：US4062879A
公开(公告)日：1977-12-13
申请号：US725447
申请日：1976-09-22
申请人： Shizumasa Kijima , Isao Yamatsu , Norio Minami , Yuichi Inai
发明人： Shizumasa Kijima , Isao Yamatsu , Norio Minami , Yuichi Inai
IPC分类号： C07C45/00 , C07C46/06 , C07C50/28 , C07C67/00 , C07F5/04 , C07C49/73
CPC分类号： C07F5/04 , C07C46/06 , C07C50/28
摘要： A process for synthesizing 2,3-dimethoxy-5-methyl-6-substituted-1,4-benzoquinones having the formula: ##STR1## wherein R is ##STR2## in which n is an integer of 0 to 9, and A and B are hydrogens or taken together form a valence bond,In which 2-methyl-4,5,6-trimethoxyphenol is reacted with boric acid or a reactive derivative thereof to obtain a 2-methyl-4,5,6-trimethoxyphenol ester of boric acid, reacting the resulting ester with an n-prenol or iso-prenol having the formula: ##STR3## wherein R is as defined above, OR A REACTIVE DERIVATIVE OF SAID N- OR ISO-PRENOL, IN THE PRESENCE OF A SILICA-ALUMINA COMPOUND, TO OBTAIN A 2-METHYL-3-SUBSTITUTED-4,5,6-TRIMETHOXYPHENOL ESTER OF BORIC ACID, AND HYDROLYZING THE THUS-OBTAINED ESTER AND TREATING THE RESULTING 2-METHYL-3-SUBSTITUTED 4,5,6-TRIMETHOXYPHENOL HAVING THE FORMULA: ##STR4## wherein R is as defined above, with an oxidant.
摘要翻译：具有下式的合成2,3-二甲氧基-5-甲基-6-取代-1,4-苯醌的方法：其中R是，其中n是0-9的整数，A和 B是氢或一起形成价键，其中2-甲基-4,5,6-三甲氧基苯酚与硼酸或其反应性衍生物反应，得到2-甲基-4,5,6-三甲氧基苯酚酯硼酸，用具有本公式的N-丙烯酸酯或ISO-PRENOL反应所述酯类：其中R如上所定义，或者是在SILICA存在下的反应性衍生物，氧化铝化合物，得到2-甲基-3-取代的4,5,6-三甲氧基苯甲酸酯，并将所得的酯水解并处理结晶的2-甲基-3-取代的4,5,6- 具有公式的三甲苯酚：其中R如上所定义，其中R 1与氧化剂一起形成。

20. 发明授权

US4061660A Process for synthesis of coenzyme Q compounds 失效
标题翻译：合成辅酶Q化合物的方法
公开(公告)号：US4061660A
公开(公告)日：1977-12-06
申请号：US725510
申请日：1976-09-22
申请人： Shizumasa Kijima , Isao Yamatsu , Norio Minami , Yuichi Inai
发明人： Shizumasa Kijima , Isao Yamatsu , Norio Minami , Yuichi Inai
IPC分类号： C07C45/00 , C07C46/06 , C07C50/28 , C07C67/00 , C07F5/04 , C07C49/73
CPC分类号： C07F5/04 , C07C46/06 , C07C50/28
摘要： A process for the synthesis of 2,3-dimethoxy-5-methyl-6-substituted-1,4-benzoquinones having the formula: ##STR1## wherein R is ##STR2## in which n is an integer of 0 to 9, and A and B are hydrogens or A--B is a direct valence bond between the carbon atoms to which they are attached,Characterized by reacting 2-methyl-4,5,6-trimethoxyphenol with an aryl boronic acid, a lower alkyl boronic acid or an acid anhydride thereof to obtain a 2-methyl-4,5,6-trimethoxyphenol ester of boric acid, reacting the resulting ester with an n-prenol or iso-prenol having the formula: ##STR3## wherein R is as defined above, OR A REACTIVE DERIVATIVE OF SAID N- OR ISO-PRENOL, IN THE PRESENCE OF A SILICA-ALUMINA COMPOUND, TO OBTAIN A 2-METHYL-3-SUBSTITUTED-4,5,6-TRIMETHOXYPHENOL ESTER OF BORIC ACID, AND HYDROLYZING THE THUS-OBTAINED ESTER AND TREATING THE RESULTING 2-METHYL-3-SUBSTITUTED-4,5,6-TRIMETHOXYPHENOL HAVING THE FORMULA: ##STR4## wherein R is as defined above, WITH AN OXIDIZING AGENT.
摘要翻译：一种用于合成具有下式的2,3-二甲氧基-5-甲基-6-取代-1,4-苯醌的方法，其中R是其中n是0-9的整数，以及 A和B是氢原子，或AB是它们所连接的碳原子之间的直接键合键，其特征在于通过使具有亚芳基酸的2-甲基-4,5,6-三甲氧基苯酚，低级碱金属硼酸或酸获得硼酸的2-甲基-4,5,6-三甲氧基苯酚的无水物，用具有下式的N-PRENOL或ISO-PRENOL反应结果的酯：其中R如上所定义，OR A 在二氧化硅铝化合物存在下，得到N-或ISO-PRENOL的反应性衍生物，得到2-甲基-3-取代的4,5,6-三甲氧基苯甲酸酯，并将所得的酯化和处理具有该化合物的结构式2-甲基-3-取代的4,5,6-三甲氧基苯酚：其中R如上定义，其中R是氧化剂。

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