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1. 发明授权

US5849779A Pyrazole derivatives and their pharmaceutical use 失效
标题翻译：吡唑衍生物及其药物用途
公开(公告)号：US5849779A
公开(公告)日：1998-12-15
申请号：US864076
申请日：1997-05-28
申请人： Kohsaku Hirota , Hironao Sajiki , Yoshiaki Isobe , Yoichi Ohba , Hiroyuki Morita , Haruo Takaku , Nobuyoshi Chiba
发明人： Kohsaku Hirota , Hironao Sajiki , Yoshiaki Isobe , Yoichi Ohba , Hiroyuki Morita , Haruo Takaku , Nobuyoshi Chiba
IPC分类号： A61K31/415 , C07D231/40 , C07D231/04
CPC分类号： C07D231/40 , A61K31/415
摘要： The present invention relates to a pyrazole derivative represented by formula (I) or (II) ##STR1## wherein R.sup.1 is hydrogen C2-C6 alkyl benzyl or phenyl; each of R.sup.2 and R.sup.3 is hydrogen, C1-C6 alkyl or benzyl; each of R.sup.4 and R.sup.5 is hydrogen, C1-C6 alkyl, C3-C6 alkenyl, C3-C8 cycloalkyl, benzyl or phenyl; X is oxygen or sulfur; R.sup.5 is hydrogen, C2-C6 alkyl, C3-C6 alkenyl, C3-C8 cycloalkyl or benzyl when R.sup.1 is benzyl, R.sup.2 is ethyl, R.sup.3 is hydrogen, and R.sup.4 is hydrogen, and its pharmaceutical use.
摘要翻译：本发明涉及由式（I）或（II）表示的吡唑衍生物，苄基或苯基; R2和R3各自为氢，C1-C6烷基或苄基; R 4和R 5各自为氢，C 1 -C 6烷基，C 3 -C 6烯基，C 3 -C 8环烷基，苄基或苯基; X是氧或硫; 当R1是苄基，R2是乙基，R3是氢，R4是氢时，R5是氢，C2-C6烷基，C3-C6烯基，C3-C8环烷基或苄基，以及其药物用途。

2. 发明申请

US20080045724A1 Deuterated Polyimides and Derivatives Thereof 审中-公开
公开(公告)号：US20080045724A1
公开(公告)日：2008-02-21
申请号：US11569463
申请日：2005-05-17
申请人： Kazushige Muto , Tsuneaki Maesawa , Nobuhiro Ito , Tsutomu Watahiki , Kosaku Hirota , Hironao Sajiki
发明人： Kazushige Muto , Tsuneaki Maesawa , Nobuhiro Ito , Tsutomu Watahiki , Kosaku Hirota , Hironao Sajiki
IPC分类号： C07C229/54 , C07D487/04
CPC分类号： C07D487/04 , C07D209/48 , C08G73/10 , C08G73/1007 , G02B6/1221
摘要： The object of the present invention is to provide a polyimide compound useful as a raw material of a polymer for an optical waveguide that has excellent transparency and heat resistance, low moisture absorption, a small optical transmission loss, a high refractive index and good adhesion to a base material or a substrate. The present invention is inventions of a method for producing a deuterated polyamic acid compound represented by the general formula [2]: wherein R1 indicates a tetravalent alicyclic hydrocarbon group or a tetravalent aromatic hydrocarbon group, which may have a heavy hydrogen atom; R2 indicates a divalent aromatic hydrocarbon group having a heavy hydrogen atom; and m indicates an integer not less than 1, which comprises reacting an acid anhydride represented by the general formula [3]: wherein R1 has the same meaning as above, with a deuterated diamine compound represented by the general formula [4]: H2N—R2—NH2 [4] wherein R2 has the same meaning as above; a method for producing a deuterated polyimide compound represented by the general formula [1]: wherein R1 indicates a tetravalent alicyclic hydrocarbon group or a tetravalent aromatic hydrocarbon group, which may have a heavy hydrogen atom; R2 indicates a divalent aromatic hydrocarbon group having a heavy hydrogen atom; and n indicates an integer not less than 1, which comprises subjecting thus obtained deuterated polyamic acid compound to a ring closure reaction; a method for producing a deuterated polyimide compound represented by the general formula [1] which comprises reacting an acid anhydride represented by the above general formula [3] with a deuterated diamine compound represented by the above general formula [4] and then subjecting the reaction product to a ring closure reaction; use of a deuterated polyimide compound obtained by the above production methods as a raw material polymer for an optical waveguide; a film for an optical waveguide containing said deuterated polyimide compound; a deuterated polyimide compound; and a deuterated polyamic acid compound.

3. 发明授权

US09255070B2 Method of deuteration using mixed catalyst 有权
标题翻译：使用混合催化剂的氘化方法
公开(公告)号：US09255070B2
公开(公告)日：2016-02-09
申请号：US10585629
申请日：2004-12-21
申请人： Nobuhiro Ito , Tsuneaki Maesawa , Kazushige Muto , Kosaku Hirota , Hironao Sajiki
发明人： Nobuhiro Ito , Tsuneaki Maesawa , Kazushige Muto , Kosaku Hirota , Hironao Sajiki
IPC分类号： C07D213/74 , C07B59/00 , C07C37/00 , C07C51/353 , C07C209/68 , C07D213/80
CPC分类号： C07D213/74 , C07B59/00 , C07B2200/05 , C07C37/00 , C07C51/353 , C07C209/68 , C07D213/80 , C07C57/30 , C07C63/04 , C07C39/06
摘要： The subject of the present invention is to provide a method for deuteration, which can obtain a compound having an aromatic ring and/or a heterocyclic ring at an improved deuteration ratio. The present invention relates to a method for deuteration of a compound having an aromatic ring and/or a heterocyclic ring, comprising reacting the compound having an aromatic ring and/or a heterocyclic ring with a heavy hydrogen source in the presence of an activated mixed catalyst of not less than two kinds of catalysts selected from among a palladium catalyst, a platinum catalyst, a rhodium catalyst, an iridium catalyst, a ruthenium catalyst, a nickel catalyst and a cobalt catalyst.
摘要翻译：本发明的主题是提供一种氘化方法，其可以以改善的氘化比获得具有芳环和/或杂环的化合物。本发明涉及一种具有芳环和/或杂环的化合物的氘化方法，包括在活化的混合催化剂存在下使具有芳环和/或杂环的化合物与重氢源反应选自钯催化剂，铂催化剂，铑催化剂，铱催化剂，钌催化剂，镍催化剂和钴催化剂中的不少于两种催化剂。

4. 发明授权

US07795166B2 Functional group-selective hydrogenation catalyst and functional group-selective hydrogenation method 有权
标题翻译：功能组选择性氢化催化剂和官能团选择性氢化方法
公开(公告)号：US07795166B2
公开(公告)日：2010-09-14
申请号：US11565844
申请日：2006-12-01
申请人： Hironao Sajiki , Tomohiro Maegawa , Kosaku Hirota
发明人： Hironao Sajiki , Tomohiro Maegawa , Kosaku Hirota
IPC分类号： B01J31/00 , B01J37/00 , B01J27/02 , B01J27/043 , B01J27/045 , C08F4/02 , C08F4/60 , C07C319/00 , C07C321/00 , C07C323/00 , C07C381/00 , C07C49/92 , C07C5/10 , C07C5/05 , C07C5/02 , C07C5/03 , C07F5/00 , C07F15/00 , C07F17/02
CPC分类号： B01J23/44 , B01J21/18 , B01J31/0217 , B01J31/0218 , B01J37/0203 , C07C45/62 , C07C67/303 , C07C209/48 , C07C221/00 , C07C269/06 , C07C49/04 , C07C49/784 , C07C49/215 , C07C49/233 , C07C49/83 , C07C69/007 , C07C69/24 , C07C69/612 , C07C69/76 , C07C211/27 , C07C225/22 , C07C271/12 , C07C271/22 , C07C271/28
摘要： A functional group-selective hydrogenation catalyst is provided, which is capable of selectively hydrogenating an aliphatic carbon-carbon double bond, aliphatic carbon-carbon triple bond, aromatic formyl group or aromatic nitro group contained in an organic compound. The catalyst includes a carrier, and palladium and an organic sulfur compound supported jointly thereon.
摘要翻译：提供了能够选择性氢化有机化合物中所含的脂族碳 - 碳双键，脂族碳 - 碳三键，芳族甲酰基或芳族硝基的官能团选择性氢化催化剂。催化剂包括载体，钯和与其共同负载的有机硫化合物。

5. 发明申请

US20080145303A1 Method for Producing Deuterium Gas and Catalytic Deuteration Method Using Deuterium Gas Obtained Thereby 审中-公开
标题翻译：使用由此获得的氘气生产氘气和催化氘化方法
公开(公告)号：US20080145303A1
公开(公告)日：2008-06-19
申请号：US11883193
申请日：2006-01-16
申请人： Kosaku Hirota , Hironao Sajiki , Nobuhiro Ito
发明人： Kosaku Hirota , Hironao Sajiki , Nobuhiro Ito
IPC分类号： C01B4/00 , C01B7/00 , C07D301/00 , C07C255/00 , C07C211/00 , C07C39/00 , C07C5/08 , C07C5/02
CPC分类号： C07C209/36 , B01J21/18 , B01J23/42 , B01J23/44 , B01J23/46 , B01J23/75 , B01J23/755 , C01B4/00 , C07B59/00 , C07B2200/05 , C07C57/30 , C07C209/48 , C07C211/46 , C07C211/48
摘要： [PROBLEMS] To provide a method for producing heavy hydrogen gas, which enables heavy hydrogen gas to be efficiently produced from a deuterated solvent as a reaction substrate.[MEANS FOR SOLVING PROBLEMS] (1) A method for producing heavy hydrogen gas, comprising bringing a deuterated solvent into contact with hydrogen gas under pressure in the coexistence with a catalyst selected from a palladium catalyst, a platinum catalyst, a nickel catalyst, a cobalt catalyst, an iridium catalyst, and a rhodium catalyst and a ruthenium catalyst which are not coordinated with a ligand, and (2) a catalytic deuteration method of a compound having a reducible functional group, comprising bringing the heavy hydrogen gas obtained by the above (1) into contact with the compound having a reducible functional group in the coexistence with a catalytic reduction catalyst.
摘要翻译：本发明提供一种生产重氢气的方法，其能够使重氢气从氘化溶剂作为反应基质有效地生成。（1）一种重氢气的制造方法，其特征在于，在与钯催化剂，铂催化剂，镍催化剂，镍催化剂等的催化剂共存的同时使氘化溶剂与氢气接触，钴催化剂，铱催化剂以及不与配位体配位的铑催化剂和钌催化剂，（2）具有可还原官能团的化合物的催化氘化方法，其特征在于，将上述得到的重氢气（1）在与催化还原催化剂共存的情况下与具有可还原官能团的化合物接触。

6. 发明授权

US07126023B2 Method for deuteration of an inert methylene 失效
标题翻译：稀释惰性亚甲基的方法
公开(公告)号：US07126023B2
公开(公告)日：2006-10-24
申请号：US10516638
申请日：2002-11-12
申请人： Kosaku Hirota , Hironao Sajiki
发明人： Kosaku Hirota , Hironao Sajiki
IPC分类号： C07C69/76 , C07C53/134 , C07C41/00
CPC分类号： C07B59/00 , C07B59/001 , Y10S585/941
摘要： The present invention relates to a method for deuteration of an inert alkane using activated palladium carbon. The present invention discloses“A method for deuteration of a hydrogen atom of a methyl group or a hydrogen atom bonded to a carbon atom at benzyl position and the other carbon atoms of an alkylene group having not less than 2 carbon atoms, in a compound containing the methyl group or the-alkylene group having not less than 2 carbon atoms, directly bonded to an aromatic ring which may have a substituent, which comprises placing said compound in a deuterated solvent in the presence of activated palladium carbon, under sealed reflux condition”.
摘要翻译：本发明涉及使用活性钯碳来猝灭惰性烷烃的方法。本发明公开了“含有苄基的碳原子上的甲基或与氢原子的氢原子咔嗒嗒嗒嗒嗒”的方法，其中含有碳原子数2以上的亚烷基的其它碳原子在含有直接键合到可具有取代基的芳香环上的具有不少于2个碳原子的甲基或亚烷基，其包括在活化的钯碳存在下将所述化合物置于氘化溶剂中，在密封回流条件下“ 。

7. 发明申请

US20060116535A1 Method of deuteration 审中-公开
标题翻译：氘化方法
公开(公告)号：US20060116535A1
公开(公告)日：2006-06-01
申请号：US10539188
申请日：2003-11-07
申请人： Nobuhiro Ito , Tsuneaki Maesawa , Kazushige Muto , Kosaku Hirota , Kosaku Hirota , Hironao Sajiki
发明人： Nobuhiro Ito , Tsuneaki Maesawa , Kazushige Muto , Kosaku Hirota , Kosaku Hirota , Hironao Sajiki
IPC分类号： C07C35/22
CPC分类号： C07B59/00 , C07B2200/05 , C07C29/00 , C07C45/00 , C07C2601/14 , C07C2602/42 , C07C2603/68 , C07C31/125 , C07C35/08 , C07C35/29 , C07C35/37
摘要： The present invention relates to a method for deuteration of a compound represented by the general formula [1]: R1—X—R2 [1] wherein, R1 represents an alkyl group or an aralkyl group, which may have a carbon-carbon double bond and/or triple bond; R2 represents an alkyl group which may have a carbon-carbon double bond and/or triple bond, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group or a hydroxyl group; X represents a carbonyl group or a hydroxylmethylene group, R1 and R2 may form an alicyclic ring together with a carbon atom contained in X; provided that R2 represents an alkyl group which may have a carbon-carbon double bond and/or triple bond, an aryl group or an aralkyl group when X is a hydroxylmethylene group, comprising reacting the compound represented by the general formula [1] with a heavy hydrogen source in the co-presence of an activated catalyst selected from a palladium catalyst, a platinum catalyst, a rhodium catalyst, a ruthenium catalyst, a nickel catalyst and a cobalt catalyst. The method of the present invention can significantly improve working environment because the deuteration, which has been conventionally carried out under severe conditions such as basic condition, can be carried out under neutral condition. Further, even when the compound represented by the general formula [1] is one having a carbon-carbon double bond or triple bond, the method for deuteration of the present invention enables to efficiently carry out objective deuteration without reduction of said double bond or triple bond.
摘要翻译：本发明涉及由通式[1]表示的化合物的氘化方法：<？in-line-formula description =“In-line Formulas”end =“lead”？> R＆lt; 1＆ SUP> -XR <2> <1 in-line-formula description =“In-line Formulas”end =“tail”？>其中，R 1表示烷基或芳烷基，其可以具有碳 - 碳双键和/或三键; R 2表示可以具有碳 - 碳双键和/或三键，芳基，芳烷基，烷氧基，芳氧基或羟基的烷基; X表示羰基或羟基亚甲基，R 1和R 2可以与X中包含的碳原子一起形成脂环族环; 条件是当X是羟基亚甲基时，R 2表示可以具有碳 - 碳双键和/或三键的烷基，芳基或芳烷基，包括使由在活性催化剂共催化剂中选择钯催化剂，铂催化剂，铑催化剂，钌催化剂，镍催化剂和钴催化剂，具有重氢源的通式[1]。本发明的方法可以显着地改善工作环境，因为通常在诸如碱性条件的苛刻条件下常规进行的氘化可以在中性条件下进行。此外，即使当由通式[1]表示的化合物是具有碳 - 碳双键或三键的化合物时，本发明的氘化方法能够有效地进行目标氘化而不会减少所述双键或三重键键。

8. 发明授权

US08853457B2 Polyamine and method for producing thereof 有权
标题翻译：多胺及其制造方法
公开(公告)号：US08853457B2
公开(公告)日：2014-10-07
申请号：US13520770
申请日：2010-12-17
申请人： Hiroyuki Kitayama , Hironao Sajiki , Yasunari Monguchi
发明人： Hiroyuki Kitayama , Hironao Sajiki , Yasunari Monguchi
IPC分类号： C07C209/52 , C08G73/02
CPC分类号： C08G73/0213 , C08G73/0206 , C08G73/0266
摘要： A method for producing a polyamine is described that provides excellent safety, a lot of flexibility regarding a variety of its productions, and that can produce a polyamine of high-molecular weight easily and inexpensively.The polyamine includes a combination of units of formula (1) or (2): —(NH—(CH2)m—NH—(CH2)n)— (1) (in the formula (1), independently in every unit, “m” indicates an integral number of 0 or more and “n” indicates an integral number of 3 or more.) —(NH—y—NH —Z)— (2) (in the formula (2), independently in every unit, “Y” and “Z” are the same as or different from each other, and they indicate substituted or unsubstituted groups including unsaturated aliphatic, cyclic aliphatic or aromatic hydrocarbon radicals that can include hetero atoms.).
摘要翻译：描述了一种生产多胺的方法，其提供优异的安全性，对其各种生产具有很大的灵活性，并且可以容易且廉价地生产高分子量的多胺。多胺包括式（1）或（2）的单元的组合： - （NH-（CH 2）m -NH-（CH 2）n） - （1）（在式（1） “m”表示0以上的整数，“n”表示3以上的整数。） - （NH-y-NH-Z） - （2）（式（2）中，单元“Y”和“Z”彼此相同或不同，它们表示可以包括杂原子的取代或未取代的基团，包括不饱和脂族，环状脂族或芳族烃基。

9. 发明申请

US20130150623A1 PROCESS FOR PRODUCING HYDROGEN OR HEAVY HYDROGENS, AND HYDROGENATION (PROTIATION, DEUTERATION OR TRITIATION) OF ORGANIC COMPOUNDS USING SAME 有权
标题翻译：生产氢或重氢的方法，以及使用相同方法的有机化合物的氢化（抑制，去除或检测）
公开(公告)号：US20130150623A1
公开(公告)日：2013-06-13
申请号：US13817637
申请日：2011-08-16
申请人： Hironao Sajiki , Yasunari Monguchi , Yoshinari Sawama , Shinichi Kondo
发明人： Hironao Sajiki , Yasunari Monguchi , Yoshinari Sawama , Shinichi Kondo
IPC分类号： C01B4/00
CPC分类号： C01B3/10 , C01B3/08 , C01B4/00 , C01B2203/0277 , C01B2203/1047 , C01B2203/1064 , C07B31/00 , C07B35/02 , C07B35/06 , C07B59/00 , C07B2200/05 , C07C1/26 , C07C5/09 , C07C5/10 , C07C29/143 , C07C29/17 , C07C41/20 , C07C41/24 , C07C41/26 , C07C45/61 , C07C209/36 , C07C213/02 , C07C221/00 , C07C2523/745 , C07C2601/14 , Y02E60/364 , C07C215/68 , C07C211/58 , C07C217/84 , C07C225/22 , C07C33/20 , C07C43/2055 , C07C33/22 , C07C43/205 , C07C43/23 , C07C49/807 , C07C15/18 , C07C13/28 , C07C15/24 , C07C15/52 , C07C9/15
摘要： An object is to provide a process for providing hydrogen or heavy hydrogens conveniently without the necessity of large-scale equipment and a process capable of performing hydrogenation (protiation, deuteration or tritiation) reaction conveniently without the use of an expensive reagent and a special catalyst. The production process includes a process for producing hydrogen or heavy hydrogens, containing subjecting water or heavy water to mechanochemical reaction in the presence of a catalyst metal, and a process for producing a hydrogenated (protiated, deuterated or tritiated) organic compound, containing subjecting an organic compound and water or heavy water to mechanochemical reaction in the presence of a catalyst metal.
摘要翻译：本发明的目的是提供一种方便地提供氢或重氢的方法，而不需要大规模设备和能够方便地进行氢化（促进，氘化或氚化）反应的方法，而不需要使用昂贵的试剂和特殊的催化剂。生产方法包括生产氢或重氢的方法，包括在催化剂金属存在下使水或重水进行机械化学反应，以及生产氢化（肟化或氘代或氚化）有机化合物的方法，有机化合物和水或重水在催化剂金属存在下进行机械化学反应。

10. 发明申请

US20130123542A1 POLYAMINE AND METHOD FOR PRODUCING THEREOF 有权
标题翻译：聚胺及其生产方法
公开(公告)号：US20130123542A1
公开(公告)日：2013-05-16
申请号：US13520770
申请日：2010-12-17
申请人： Hiroyuki Kitayama , Hironao Sajiki , Yasunari Monguchi
发明人： Hiroyuki Kitayama , Hironao Sajiki , Yasunari Monguchi
IPC分类号： C08G73/02
CPC分类号： C08G73/0213 , C08G73/0206 , C08G73/0266
摘要： A method for producing a polyamine is described that provides excellent safety, a lot of flexibility regarding a variety of its productions, and that can produce a polyamine of high-molecular weight easily and inexpensively.The polyamine includes a combination of units of formula (1) or (2): —(NH—(CH2)m—NH—(CH2)n)— (1) (in the formula (1), independently in every unit, “m” indicates an integral number of 0 or more and “n” indicates an integral number of 3 or more.) —(NH—Y—NH—Z)— (2) (in the formula (2), independently in every unit, “Y” and “Z” are the same as or different from each other, and they indicate substituted or unsubstituted groups including unsaturated aliphatic, cyclic aliphatic or aromatic hydrocarbon radicals that can include hetero atoms.).
摘要翻译：描述了一种生产多胺的方法，其提供优异的安全性，对其各种生产具有很大的灵活性，并且可以容易且廉价地生产高分子量的多胺。多胺包括式（1）或（2）的单元的组合： - （NH-（CH 2）m -NH-（CH 2）n） - （1）（在式（1） “m”表示0以上的整数，“n”表示3以上的整数。） - （NH-Y-NH-Z） - （2）（式（2）中，单元“Y”和“Z”彼此相同或不同，它们表示可以包括杂原子的取代或未取代的基团，包括不饱和脂族，环状脂族或芳族烃基。

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