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    • 2. 发明授权
    • Process for producing
1-(2'-deoxy-.beta.-D-erythro-pentofuranosyl)-5-trifluoromethyluracil
derivatives
    • 1-(2'-脱氧-β-D-赤型 - 呋喃戊糖基)-5-三氟甲基尿嘧啶衍生物的制备方法
    • US5532349A
    • 1996-07-02
    • US275455
    • 1994-07-15
    • Nobuya KawauchiNobuyuki FukazawaHiroki IshibashiKengo Otsuka
    • Nobuya KawauchiNobuyuki FukazawaHiroki IshibashiKengo Otsuka
    • C07H19/06C07H19/073A61K31/70
    • C07H19/06
    • A process for producing 1-(2'-deoxy-B-D-erythropentofuranosyl)-5-trifluoromethyluracil derivatives having the formula as shown below: ##STR1## wherein X.sup.1 and X.sup.2 are independently hydrogen or halogen, comprising:(a) reacting 5-trifluoromethyl-5,6-dihydrouracil with alkylsulfoxide in the presence of a halogen and and acid to obtain 5-trifluoromethyluracil;(b) reacting the obtained 5-trifluoromethyluracil with a silylating agent to obtain 5-trifluoromethyl-2,4 -bis(trimethylsilyloxy)uracil; and(c) reacting the obtained 5-trifluoromethyl-2,4-bis(trimethylsilyloxy)uracil with a protected 2-deoxyalpha-D-erthro-pentofuranosyl)halide derivative in chloroform solvent in the presence of fluoride ion and in the presence of a copper compound as a catalyst.The resulting, deblocked nucleosides are useful as antiviral and antitumor agents.
    • 一种制备具有下式的1-(2'-脱氧-β-赤式呋喃糖基)-5-三氟甲基尿嘧啶衍生物的方法:其中X1和X2独立地是氢或卤素,包括:(a)使5-三氟甲基 -5,6-二氢尿嘧啶与烷基亚砜在卤素存在下反应,得到5-三氟甲基尿嘧啶; (b)使所得5-三氟甲基尿嘧啶与甲硅烷基化试剂反应,得到5-三氟甲基-2,4-双(三甲基甲硅烷氧基)尿嘧啶; 和(c)使得到的5-三氟甲基-2,4-双(三甲基甲硅烷氧基)尿嘧啶与受保护的2-脱氧-α-D-戊硫基呋喃糖基)卤化物衍生物在氯仿溶剂中,在氟离子存在下,在 铜化合物作为催化剂。 所得到的解封核苷可用作抗病毒和抗肿瘤剂。
    • 3. 发明授权
    • Optical lens and a process for preparing the lens
    • 光学透镜和准备透镜的工艺
    • US6019915A
    • 2000-02-01
    • US233441
    • 1999-01-20
    • Kenichi FujiiNobuya KawauchiToshiyuki SuzukiSeiichi KobayashiMasao Imai
    • Kenichi FujiiNobuya KawauchiToshiyuki SuzukiSeiichi KobayashiMasao Imai
    • C08F2/50C08F283/00C08F291/18C08G18/38G02B1/04B29D11/00B29C35/08G02B3/00G02C7/02
    • C08G18/3876C08F283/006C08F291/18G02B1/041
    • Disclosed are (1) an optical resin composition comprising Component A: a thiourethane prepolymer compound prepared by reacting a polythiol compound having at least 3 functional groups and an intramolecular sulfide bond, with a polyisocyanate compound in a molar ratio of --SH to --NCO ranging from 3.0 to 7.0; Component B: at least one (meth) acrylate compound having at least 2 functional groups; and Component C: a compound radically polymerizable with Components A and B, in 10 to 50% by weight, 35 to 70% by weight, and 5 to 30% by weight, respectively; (2) a preparation process for an optical resin by photopolymerization; (3) an optical resin; and (4) a prepolymer suitable for Component A. The composition is a novel, rapidly polymerizable composition for an optical resin. Furthermore, a resin prepared by curing the composition not only has a high refractive index and a high Abbe number, but also is excellent in transparency and optical homogeneity.
    • 公开了(1)光学树脂组合物,其包含组分A:通过使具有至少3个官能团和分子内硫键的多硫醇化合物与多异氰酸酯化合物以-SH至-NCO范围的摩尔比反应制备的硫代氨基甲酸酯预聚物化合物 3.0〜7.0; 组分B:至少一种具有至少2个官能团的(甲基)丙烯酸酯化合物; 和组分C:组分A和B可自由基聚合的化合物,分别为10至50重量%,35至70重量%和5至30重量% (2)通过光聚合制备光学树脂的制备方法; (3)光学树脂; 和(4)适用于组分A的预聚物。该组合物是用于光学树脂的新型快速聚合组合物。 此外,通过固化该组合物制备的树脂不仅具有高折射率和高阿贝数,而且透明性和光学均匀性也优异。
    • 4. 发明授权
    • Composition for optical materials and use thereof
    • 用于光学材料的组合物及其用途
    • US5756766A
    • 1998-05-26
    • US822687
    • 1997-03-24
    • Nobuya KawauchiKatsuyoshi SasagawaSeiichi Kobayashi
    • Nobuya KawauchiKatsuyoshi SasagawaSeiichi Kobayashi
    • C07C323/45C07D339/08C08G18/38C08G18/77G02B1/04C07C265/00
    • C08G18/775C07C323/45C07D339/08C08G18/3876G02B1/041
    • A composition for optical materials is herein disclosed which comprises the following two components (a) and (b): (a) a component containing at least one of poly isocyanates represented by the formula (1) ##STR1## wherein A is an alkanediyl group or an alkanetetrayl group which may contain a sulfur atom, or a dithianetetrayl group, and the alkanediyl group or the alkanetetrayl group may be substituted by a phenyl group; B is a methylene chain represented by .paren open-st.CH.sub.2 .paren close-st..sub.m (m is an integer of 1 to 4) which may contain a sulfur atom, and B's may be the same or different; and n is an integer of 2 or 4, and (b) a component containing at least one of polythiols having two or more mercapto groups. The composition is useful to provide optical products such as plastic lenses, filters, substrates for recording media and optical fibers which have a very high refractive index and which are excellent in heat resistance.
    • 本文公开了一种用于光学材料的组合物,其包含以下两种组分(a)和(b):(a)含有由式(1)A(SBNCO)n(1)表示的聚异氰酸酯中的至少一种的组分,其中 A是可以含有硫原子的烷二基或烷基四
      氮杂基团,或二硫杂萘基,并且烷二基或者烷基四氮杂基可以被苯基取代; B是可以含有硫原子的+545CH2 +546μm(m为1〜4的整数)表示的亚甲基,B可以相同或不同, n为2或4的整数,(b)含有具有两个以上巯基的多硫醇中的至少一种的成分。 该组合物可用于提供诸如塑料透镜,滤光器,用于记录介质的基底和具有非常高的折射率并且耐热性优异的光纤的光学产品。
    • 5. 发明授权
    • Thiol and sulfur-containing O-(meth)acrylate compounds and use thereof
    • 硫醇和含硫O-(甲基)丙烯酸酯化合物及其用途
    • US6114485A
    • 2000-09-05
    • US157985
    • 1998-09-22
    • Seiichi KobayashiNobuya KawauchiToshiyuki SuzukiMasao ImaiKenichi Fujii
    • Seiichi KobayashiNobuya KawauchiToshiyuki SuzukiMasao ImaiKenichi Fujii
    • C07C323/12C07C327/28C07C333/04C07D333/22C08F20/38G02B1/04C08F22/24C07C327/00G02C7/02
    • C08F20/38C07C323/12C07C327/28C07C333/04C07D333/22G02B1/041
    • A sulfur-containing O-(meth)acrylate compound of the following formula (1) is useful as a starting material for a resin composition used in optical applications such as a lens; wherein R represents hydrogen atom or methyl group; l represents an integer from 1 to 3; B is ##STR1## when B is ##STR2## n is 2; m is 1 or 2; A is selected from the following groups: ##STR3## wherein m represents 1 or 2; each ring may be substituted by one or more alkyl, alkylthio or alkoxy groups having 1 or 2 carbon atoms; p and q are 0 or 1, while m is 1 when p is 1;when B is ##STR4## n is 1; m is 2 or 3; A is selected from the following groups:--(CH.sub.2).sub.r --S--(CH.sub.2).sub.r --,--(CH.sub.2).sub.r --S--S--(CH.sub.2).sub.r --,--(CH.sub.2).sub.r --S--(CH.sub.2).sub.s --S--(CH.sub.2).sub.r -- and ##STR5## wherein r and s are an integer from 1 to 3; when B is ##STR6## n is 1; m is 2; A is selected from the following groups:--(CH.sub.2).sub.r --S--(CH.sub.2).sub.r --,--(CH.sub.2).sub.r --S--S--(CH.sub.2).sub.r -- and--(CH.sub.2).sub.r --S--(CH.sub.2).sub.s --S--(CH.sub.2).sub.r --wherein r and s are an integer from 1 to 3.
    • 下式(1)的含硫O-(甲基)丙烯酸酯化合物可用作用于光学应用如透镜的树脂组合物的起始材料; 其中R表示氢原子或甲基; l表示1〜3的整数, B是当B是n是2时; m为1或2; A选自以下基团:其中m表示1或2; 每个环可以被一个或多个具有1或2个碳原子的烷基,烷硫基或烷氧基取代; p和q为0或1,而当p为1时,m为1; 当B为n时; m为2或3; A选自以下基团: - (CH 2)r -S-(CH 2)r - , - (CH 2)r SS-(CH 2)r - , - (CH 2)r S-(CH 2)s S-(CH 2) r和s为1〜3的整数; 当B为n时; m为2; A选自以下基团: - (CH 2)r -S-(CH 2)r - , - (CH 2)r SS-(CH 2)r - 和 - (CH 2)r S-(CH 2)s S-(CH 2) s为1〜3的整数。
    • 7. 发明授权
    • Composition for optical materials and use thereof
    • 用于光学材料的组合物及其用途
    • US5652321A
    • 1997-07-29
    • US550352
    • 1995-10-30
    • Nobuya KawauchiKatsuyoshi SasagawaSeiichi Kobayashi
    • Nobuya KawauchiKatsuyoshi SasagawaSeiichi Kobayashi
    • C07C323/45C07D339/08C08G18/38C08G18/77G02B1/04C08G18/48
    • C08G18/775C07C323/45C07D339/08C08G18/3876G02B1/041
    • A composition for optical materials is herein disclosed which comprises the following two components (a) and (b):(a) a component containing at least one of poly isocyanates represented by the formula (1)A.paren open-st.S--B--NCO).sub.n (1)wherein A is an alkanediyl group or an alkanetetrayl group which may contain a sulfur atom, or a dithianetetrayl group, and the alkanediyl group or the alkanetetrayl group may be substituted by a phenyl group; B is a methylene chain represented by .paren open-st.CH.sub.2 .paren close-st..sub.m (m is an integer of 1 to 4) which may contain a sulfur atom, and B's may be the same or different; and n is an integer of 2 or 4, and(b) a component containing at least one of polythiols having two or more mercapto groups. The composition is useful to provide optical products such as plastic lenses, filters, substrates for recording media and optical fibers which have a very high refractive index and which are excellent in heat resistance.
    • 本文公开了用于光学材料的组合物,其包含以下两种组分(a)和(b):(a)含有由式(1)表示的聚异氰酸酯中的至少一种的组分A + 545 SB-NCO)n( 1)其中A是可以含有硫原子的烷二基或烷基四
      氮杂基团,或二硫代氨基甲酰基,并且烷二基或烷基四氮杂基可被苯基取代; B是可以含有硫原子的+545CH2 +546μm(m为1〜4的整数)表示的亚甲基,B可以相同或不同, n为2或4的整数,(b)含有具有两个以上巯基的多硫醇中的至少一种的成分。 该组合物可用于提供诸如塑料透镜,滤光器,用于记录介质的基底和具有非常高的折射率并且耐热性优异的光纤的光学产品。
    • 8. 发明授权
    • Thiol and sulfur-containing O-(meth)acrylate compounds and use thereof
    • 硫醇和含硫O-(甲基)丙烯酸酯化合物及其用途
    • US06265510B1
    • 2001-07-24
    • US09590015
    • 2000-06-09
    • Seiichi KobayashiNobuya KawauchiToshiyuki SuzukiMasao ImaiKenichi Fujii
    • Seiichi KobayashiNobuya KawauchiToshiyuki SuzukiMasao ImaiKenichi Fujii
    • C08F12602
    • C08F20/38C07C323/12C07C327/28C07C333/04C07D333/22G02B1/041C08L33/14
    • A sulfur-containing O-(meth)acrylate compound of the following formula (1) is useful as a starting material for a resin composition used in optical applications such as a lens; wherein R represents hydrogen atom or methyl group; 1 represents an integer from 1 to 3; B is when B is  n is 2; m is 1 or 2; A is selected from the following groups: wherein m represents 1 or 2; each ring may be substituted by one or more alkyl, alkylthio or alkoxy groups having 1 or 2 carbon atoms; p and q are 0 or 1, while m is 1 when p is 1; when B is  n is 1; m is 2 or 3; A is selected from the following groups: —(CH2)r—S—(CH2)r—, —(CH2)r—S—S—(CH2)r—, —(CH2)r—S—(CH2)s—S—(CH2)r— and wherein r and s are an integer from 1 to 3; when B is  n is 1; m is 2; A is selected from the following groups: —(CH2)r—S—(CH2)r—, —(CH2)r—S—S—(CH2)r— and —(CH2)r—S—(CH2)s—S—(CH2)r— wherein r and s are an integer from 1 to 3.
    • 下式(1)的含硫O-(甲基)丙烯酸酯化合物可用作用于光学应用如透镜的树脂组合物的起始原料;其中R表示氢原子或甲基; 1表示1〜3的整数, B是当B是n是2时; m为1或2; A选自以下基团:其中m表示1或2; 每个环可以被一个或多个具有1或2个碳原子的烷基,烷硫基或烷氧基取代; p和q为0或1,而当p为1时,m为1; B为n时为1; m为2或3; A选自以下基团: - (CH 2)r -S-(CH 2)r - , - (CH 2)r SS-(CH 2)r - , - (CH 2)r S-(CH 2)s S-(CH 2)r - s为1〜3的整数; B为n时为1; m为2; A选自以下基团: - (CH 2)r -S-(CH 2)r - , - (CH 2)r SS-(CH 2)r - 和 - (CH 2)r S-(CH 2)s S-(CH 2) s为1〜3的整数。
    • 10. 发明授权
    • Pyrimidinedione derivatives and antiarrythmic agents containing the same
    • 嘧啶二酮衍生物和含有它们的抗焦虑剂
    • US5308848A
    • 1994-05-03
    • US927738
    • 1992-08-12
    • Michihiko MiyamotoTsutomu KatakamiNobuya KawauchiTadahito NoboriJoji KamiyaMasaaki Ishii
    • Michihiko MiyamotoTsutomu KatakamiNobuya KawauchiTadahito NoboriJoji KamiyaMasaaki Ishii
    • C07D239/54C07D239/545C07D401/12A61K31/505C07D239/10
    • C07D239/545C07D401/12
    • A pyrimidinedione derivative compound has a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a linking structure comprising an alkyl chain containing two nitrogen atoms. This linking structure is represented by ##STR1## [wherein A is --(CH.sub.2).sub.n --, --CO-- or --O--(CH.sub.2).sub.m --; each of R.sup.1 and R.sup.2 is independently a hydrogen atom or a lower alkyl group which may be substituted by a hydroxyl group, or R.sup.1 and R.sup.2 may be so linked with each other as to make an alkylene chain and thus form a heterocyclic structure; R.sup.5 is a halogen atom, a hydroxyl group, a lower alkyloxycarbonyl group, a lower alkyloxy group which may be substituted by a lower alkyloxy group, or a lower alkyl group which may be substituted by a hydroxyl group, or R.sup.5 may be so linked with R.sup.1 as to make an alkylene chain and thus form a heterocyclic structure; n is 0, 1, 2 or 3 (when R.sup.5 is the hydroxyl group, n.noteq.0); m is 0, 1, 2 or 3; and k is 0, 1, 2 or 3 (however, a compound in which A is --O--(CH.sub.2).sub.m -- and R.sup.5 is the hydroxyl group is excluded from the pyrimidinedione derivative)]. The pyrimidinedione derivative and its acid addition salt are useful for a medical treatment of cardiac arrhythmias.
    • 嘧啶二酮衍生物化合物具有其中苯基部分和嘧啶二酮部分通过包含含有两个氮原子的烷基链的连接结构连接的碱性主链。 该连接结构由表示,其中A是 - (CH 2)n - , - CO-或-O-(CH 2)m - ; R 1和R 2各自独立地为氢原子或可以被羟基取代的低级烷基,或者R 1和R 2可以相互连接形成亚烷基链,从而形成杂环结构; R5是卤素原子,羟基,低级烷氧基羰基,可被低级烷氧基取代的低级烷氧基或可被羟基取代的低级烷基,或R5可以与 R1形成亚烷基链,从而形成杂环结构; n是0,1,2或3(当R5是羟基时,n是等于0); m为0,1,2或3; 并且k为0,1,2或3(然而,其中A为-O-(CH 2)m - 且R 5为羟基的化合物不包括在嘧啶二酮衍生物中]]。 嘧啶二酮衍生物及其酸加成盐可用于治疗心律失常。