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1. 发明授权

US4160784A Process for the production of o-aminophenyl ketone derivatives 失效
标题翻译：制备邻氨基苯基酮衍生物的方法
公开(公告)号：US4160784A
公开(公告)日：1979-07-10
申请号：US770037
申请日：1977-02-18
申请人： Tsutomu Sugasawa , Tatsuo Toyoda , Makoto Adachi , Kazuyuki Sasakura
发明人： Tsutomu Sugasawa , Tatsuo Toyoda , Makoto Adachi , Kazuyuki Sasakura
IPC分类号： C07C225/22 , C07C67/00 , C07C241/00 , C07C251/24 , C07F5/02 , C07C85/18
CPC分类号： C07F5/022
摘要： O-Aminophenyl ketone derivatives are regio-specifically prepared by reacting an aniline unsubstituted in at least one ortho position with a nitrile in the presence of boron trihalogenide to introduce a substituted iminomethyl into the ortho position of said aniline and hydrolyzing the resulting iminomethyl compound.
摘要翻译：通过在三卤代硼存在下使至少一个邻位未取代的苯胺与腈反应来引入O-氨基苯基酮衍生物，以将取代的亚氨基甲基引入所述苯胺的邻位并水解所得的亚氨基甲基化合物。

2. 发明授权

US4186144A Process for the production of cyanopinacolone 失效
标题翻译：氰考酚酸的生产工艺
公开(公告)号：US4186144A
公开(公告)日：1980-01-29
申请号：US897001
申请日：1978-04-17
申请人： Tsutomu Sugasawa , Tatsuo Toyoda , Kazuyuki Sasakura , Shiro Ueda , Akira Takase , Katsuto Okuno , Ichiro Ishizuka , Shinzaburo Sumimoto
发明人： Tsutomu Sugasawa , Tatsuo Toyoda , Kazuyuki Sasakura , Shiro Ueda , Akira Takase , Katsuto Okuno , Ichiro Ishizuka , Shinzaburo Sumimoto
IPC分类号： C07D261/14 , A01N43/80 , C07C45/00 , C07C45/63 , C07C49/16 , C07C67/00 , C07C253/00 , C07C253/16 , C07C255/17 , C07C121/34
CPC分类号： C07C255/00 , C07C45/63
摘要： Cyanopinacolone is produced by reacting pinacolone with about 1.0 to about 1.2 molar equivalents of chlorine in methanol and further reacting the resulting monochloropinacolone with about 1.0 to about 1.2 molar equivalents of an alkali metal cyanide in methanol.
摘要翻译：通过频哪酮与约1.0至约1.2摩尔当量的甲醇中的氯反应制备亚氨基乐康酮，并使所得一氯一可乐酮与约1.0至约1.2摩尔当量的碱金属氰化物在甲醇中反应。

3. 发明授权

US4551554A Process for production of 2-haloacetylphenols 失效
标题翻译： 2-卤代乙酰苯酚的制备方法
公开(公告)号：US4551554A
公开(公告)日：1985-11-05
申请号：US305621
申请日：1981-09-23
申请人： Tsutomu Sugasawa , Tatsuo Toyoda , Kazuyuki Sasakura
发明人： Tsutomu Sugasawa , Tatsuo Toyoda , Kazuyuki Sasakura
IPC分类号： C07C49/825 , B01J27/00 , B01J27/08 , C07C45/00 , C07C45/42 , C07C45/46 , C07C49/84 , C07C67/00
CPC分类号： C07C45/42 , C07C45/00 , C07C45/008
摘要： A new process for production of 2-haloacetylphenols having the general formula ##STR1## (wherein, Y is halogen atom;m is an integer of 0-2,X and n have the same meaning as mentioned below),which comprises reacting phenols having the general formula ##STR2## (wherein, X is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.5 alkoxy or halogen atom;n is an integer of 0-2)with haloacetonitriles and boron halide compounds in the presence of condensing coagents.
摘要翻译： PCT No.PCT / JP81 / 00012 Sec。 371日期1981年9月23日 102（e）1981年9月23日PCT PCT 1月16日PCT PCT。公开号WO81 / 02157 日本1981年8月6日。具有通式为“IMAGE”的2-卤代乙酰基苯酚的新方法（其中，Y为卤素原子; m为0-2的整数，X和n具有与下述相同的含义）），其包括使具有通式“IMAGE”（其中X是氢，C 1 -C 5烷基，C 3 -C 6环烷基，C 1 -C 5烷氧基或卤原子; n是0-2的整数）的酚与卤代乙腈和卤化硼化合物反应在冷凝助剂的存在下。

4. 发明授权

US5223615A Dipeptide derivatives 失效
标题翻译：二肽衍生物
公开(公告)号：US5223615A
公开(公告)日：1993-06-29
申请号：US974212
申请日：1992-11-10
申请人： Tatsuo Toyoda , Toshihiro Fujioka , Kunio Hayashi , Masuhisa Nakamura , Naofumi Hashimoto
发明人： Tatsuo Toyoda , Toshihiro Fujioka , Kunio Hayashi , Masuhisa Nakamura , Naofumi Hashimoto
IPC分类号： A61K38/00 , C07D213/56 , C07D233/54 , C07D263/06 , C07D277/30 , C07D277/46 , C07D295/26 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/06 , C07D417/12 , C07K5/02 , C07K5/065
CPC分类号： C07D233/64 , C07D213/56 , C07D263/06 , C07D277/30 , C07D277/46 , C07D295/26 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/06 , C07D417/12 , C07K5/0205 , C07K5/06078 , A61K38/00
摘要： A dipeptide derivative of the formula (I) is provided, which is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure, provided. ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, aryl, or heterocyclic radical;R.sup.2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C.sub.1 -C.sub.12 alkyl-S--, C.sub.1 -C.sub.12 alkyl-S--CH.sub.2 -, or C.sub.3 -C.sub.10 cycloalkyl-S-;R.sup.3 is aryl or 5- or 6-membered heterocyclic radical;R.sup.4 is R.sup.4' --SO.sub.2 or R.sup.4' --CO;R.sup.4' is aryl, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl; C.sub.3 -C.sub.10 cycloalkyl, or heterocyclic radical;X is CH.sub.2, NH, O, or S; andY is CO or NHSO.sub.2, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4' each may be substituted with one to three substituents.
摘要翻译：提供式（I）的二肽衍生物，其能够抑制肾素的酶活性，从而抑制肾素 - 血管紧张素系统并降低血压。（I）其中：R1是C1-C12烷基，C2-C6烯基，C2-C6炔基，C3-C10环烷基，芳基或杂环基; R2是氨基甲酰基，芳基，5-或6-元杂环基，C1-C12烷基-S-，C1-C12烷基-S-CH2-或C3-C10环烷基-S-; R3是芳基或5-或6-元杂环基; R4是R4'-SO2或R4'-CO; R 4'是芳基，C 1 -C 12烷基，C 2 -C 6烯基，C 2 -C 6炔基; C3-C10环烷基或杂环基; X是CH 2，NH，O或S; 并且Y是CO或NHSO 2，其中R 1，R 2，R 3和R 4'各自可被一至三个取代基取代。

5. 发明授权

US4814127A Method of producing a reinforced ceramic 失效
标题翻译：生产增强陶瓷的方法
公开(公告)号：US4814127A
公开(公告)日：1989-03-21
申请号：US32250
申请日：1987-03-31
申请人： Tatsuo Toyoda
发明人： Tatsuo Toyoda
IPC分类号： B28B1/26 , C04B35/111 , C04B35/80 , C04B38/00 , C04B33/28
CPC分类号： C04B35/111 , C04B35/80
摘要： A method of producing a reinforced ceramic which includes a step of aggregating ceramic fibrous material of 0.5 .mu.m or more in diameter; a composite step in which the fiber aggregate obtained is placed on a filter and a dispersion liquid in which ceramic powder having a particle size of not more than one-tenth of the diameter of the ceramic fibrous material is dispersed in a dispersion medium is transferred through the fiber aggregate from a side opposite to the filter to the other side, for passing the dispersion medium through said filter and introducing the ceramic powder in a gap between the fibrous material of the fiber aggregate to form a composite of the fibrous material and the ceramic powder; and a step of sintering the composite.
摘要翻译：一种增强陶瓷的制造方法，其特征在于，包括直径为0.5μm以上的陶瓷纤维材料的聚集工序。将获得的纤维聚集体放置在过滤器上的复合步骤和其中具有不超过陶瓷纤维材料直径的十分之一的陶瓷粉末分散在分散介质中的分散液转移通过纤维聚集体从与过滤器相反的一侧到另一侧，用于使分散介质通过所述过滤器并将陶瓷粉末引入纤维聚集体的纤维材料之间的间隙中以形成纤维材料和陶瓷的复合材料粉末; 以及烧结复合材料的步骤。

6. 发明授权

US5272268A Dipeptide derivatives 失效
标题翻译：二肽衍生物
公开(公告)号：US5272268A
公开(公告)日：1993-12-21
申请号：US974211
申请日：1992-11-10
申请人： Tatsuo Toyoda , Toshihiro Fujioka , Kunio Hayashi , Masuhisa Nakamura , Naofumi Hashimoto
发明人： Tatsuo Toyoda , Toshihiro Fujioka , Kunio Hayashi , Masuhisa Nakamura , Naofumi Hashimoto
IPC分类号： A61K38/00 , C07D213/56 , C07D233/54 , C07D263/06 , C07D277/30 , C07D277/46 , C07D295/26 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/06 , C07D417/12 , C07K5/02 , C07K5/065 , C07D401/06 , C07D249/14 , C07D277/18
CPC分类号： C07D233/64 , C07D213/56 , C07D263/06 , C07D277/30 , C07D277/46 , C07D295/26 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/06 , C07D417/12 , C07K5/0205 , C07K5/06078 , A61K38/00
摘要： A following dipeptide derivative of the following formula (I) is provided, which is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure. ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, aryl, or heterocyclic radical;R.sup.2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C.sub.1 -C.sub.12 alkyl-S--, C.sub.1 -C.sub.12 alkyl-S--CH.sub.2 --, or C.sub.3 -C.sub.10 cycloalkyl-S--;R.sup.3 is aryl or 5- or 6-membered heterocyclic radical;R.sup.4 is R.sup.4' --SO.sub.2 or R.sup.4' --CO;R.sup.4' is aryl, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl; C.sub.3 -C.sub.10 cycloaklyl, or heterocyclic radical;X is CH.sub.2, NH, O, or S; andY is CO or NHSO.sub.2, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4' each may be substituted with one to three substituents.
摘要翻译：提供下述式（I）的二肽衍生物，其能够抑制肾素的酶活性，从而抑制肾素 - 血管紧张素系统并降低血压。（I）其中：R1是C1-C12烷基，C2-C6烯基，C2-C6炔基，C3-C10环烷基，芳基或杂环基; R2是氨基甲酰基，芳基，5-或6-元杂环基，C1-C12烷基-S-，C1-C12烷基-S-CH2-或C3-C10环烷基-S-; R3是芳基或5-或6-元杂环基; R4是R4'-SO2或R4'-CO; R 4'是芳基，C 1 -C 12烷基，C 2 -C 6烯基，C 2 -C 6炔基; C 3 -C 10环烷基或杂环基; X是CH 2，NH，O或S; 并且Y是CO或NHSO 2，其中R 1，R 2，R 3和R 4'各自可被一至三个取代基取代。

7. 发明授权

US5194608A Dipeptide derivatives 失效
标题翻译：替代衍生物
公开(公告)号：US5194608A
公开(公告)日：1993-03-16
申请号：US719492
申请日：1991-06-24
申请人： Tatsuo Toyoda , Toshihiro Fujioka , Kunio Hayashi , Masuhisa Nakamura , Naofumi Hashimoto
发明人： Tatsuo Toyoda , Toshihiro Fujioka , Kunio Hayashi , Masuhisa Nakamura , Naofumi Hashimoto
IPC分类号： A61K38/00 , C07D213/56 , C07D233/54 , C07D233/64 , C07D263/06 , C07D277/30 , C07D277/46 , C07D277/56 , C07D295/26 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/06 , C07D417/12 , C07K5/02 , C07K5/065
CPC分类号： C07D233/64 , C07D213/56 , C07D263/06 , C07D277/30 , C07D277/46 , C07D295/26 , C07D401/12 , C07D405/12 , C07D413/06 , C07D417/06 , C07D417/12 , C07K5/0205 , C07K5/06078 , A61K38/00
摘要： A dipeptide derivative of formula (I) is provided, which is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure. ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.10 cycloalkyl, aryl, or heterocyclic radical;R.sup.2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C.sub.1 -C.sub.12 alkyl-S--, C.sub.1 -C.sub.12 alkyl-S--CH.sub.2 --, or C.sub.3 -C.sub.10 cycloalkyl-S--;R.sup.3 is aryl or 5- or 6-membered heterocyclic radical;R.sup.4 is R.sup.4' --SO.sub.2 or R.sup.4' --CO;R.sup.4' is aryl, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl; C.sub.3 -C.sub.10 cycloalkyl, or heterocyclic radical;X is CH.sub.2, NH, O, or S; andY is CO or NHSO.sub.2, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4' each may be substituted with one to three substituents.

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