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1. 发明授权

US3991045A N.sup.4 -acylarabinonucleosides 失效
标题翻译： N {HU 4 {B-酰基阿糖胞苷
公开(公告)号：US3991045A
公开(公告)日：1976-11-09
申请号：US540294
申请日：1975-01-10
申请人： Torao Ishida , Kageyasu Akashi , Koichi Yoshida , Minoru Akiyama , Yoshio Sakurai , Shigeru Tsukagoshi
发明人： Torao Ishida , Kageyasu Akashi , Koichi Yoshida , Minoru Akiyama , Yoshio Sakurai , Shigeru Tsukagoshi
IPC分类号： C07H19/06
CPC分类号： C07H19/06
摘要： An N.sup.4 -acyl-1-.beta.-D-arabinofuranosylcytosine having the following formula ##SPC1##Wherein R is an aliphatic acyl group having 3 to 35 carbon atoms. The compounds of this invention are useful as a cancer chemotherapeutic agent for controlling tumors, e.g., in mice, an insecticide, and a fungicidal surface active agent.
摘要翻译：具有下式的N 4 - 酰基-1-β-D-阿拉伯呋喃糖基胞嘧啶R是具有3至35个碳原子的脂族酰基。本发明的化合物可用作控制肿瘤的癌症化学治疗剂，例如在小鼠，杀虫剂和杀真菌剂表面活性剂中。

2. 发明授权

US4086417A Cytidine nucleotide derivatives 失效
标题翻译：胞苷核苷酸衍生物
公开(公告)号：US4086417A
公开(公告)日：1978-04-25
申请号：US622794
申请日：1975-10-15
申请人： Torao Ishida , Minoru Akiyama , Yoshio Sakurai , Shigeru Tsukagoshi
发明人： Torao Ishida , Minoru Akiyama , Yoshio Sakurai , Shigeru Tsukagoshi
IPC分类号： C07H19/10
CPC分类号： C07H19/10
摘要： A nucleotide derivative represented by the general formula: ##STR1## wherein R represents an acyl group having 14 - 22 carbon atoms and having an aliphatic acyl moiety; X represents a hydrogen atom, a halogen atom, an alkyl group having 1 - 4 carbon atoms, or a trifluoromethyl group; and at least one, but not all, of Y.sub.1, Y.sub.2, and Y.sub.3 represents a phosphate, a pyrophosphate, a triphosphate, or a salt thereof, the balance of Y.sub.1, Y.sub.2 and Y.sub.3 representing a hydroxyl group; or in case of ribosyl, Y.sub.1 and Y.sub.3, or Y.sub.2 and Y.sub.3 represent, at the same time, the aforesaid phosphate, pyrophosphate, triphosphate or salt thereof and the remaining group of Y.sub.1, Y.sub.2 or Y.sub.3 represents a hydroxyl group; or in case of arabinosyl, Y.sub.1 and Y.sub.2, or Y.sub.2 and Y.sub.3 represent, at the same time, the aforesaid phosphate, pyrophosphate, triphosphate or salt therof and the remaining group of Y.sub.1, Y.sub.2 or Y.sub.3 represents a hydroxyl group. The nontoxic salts of these phosphates are useful as an antileukemialagent for mice which is soluble in water and has high stability.
摘要翻译：由以下通式表示的核苷酸衍生物：其中R表示具有14-22个碳原子且具有脂族酰基部分的酰基; X表示氢原子，卤素原子，具有1-4个碳原子的烷基或三氟甲基; Y1，Y2和Y3中的至少一个但不是全部表示磷酸酯，焦磷酸酯，三磷酸酯或其盐，余量的Y1，Y2和Y3表示羟基; 或在核糖基，Y1和Y3的情况下，或Y2和Y3同时表示上述磷酸盐，焦磷酸盐，三磷酸盐或其盐，剩余的Y 1，Y 2或Y 3基团表示羟基; 或在阿糖基，Y1和Y2的情况下，或Y2和Y3同时表示上述磷酸盐，焦磷酸盐，三磷酸盐或盐，而剩余的Y1，Y2或Y3基团表示羟基。这些磷酸盐的无毒盐可用作可溶于水并具有高稳定性的小鼠的抗白血病细胞。

3. 发明授权

US4097665A Diacylnucleosides and process for preparing the same 失效
标题翻译：二酰基核苷及其制备方法
公开(公告)号：US4097665A
公开(公告)日：1978-06-27
申请号：US634706
申请日：1975-11-24
申请人： Torao Ishida , Minoru Akiyama , Daikichi Nishimura , Hiroshi Hayashi , Yoshio Sakurai , Shigeru Tsukagoshi
发明人： Torao Ishida , Minoru Akiyama , Daikichi Nishimura , Hiroshi Hayashi , Yoshio Sakurai , Shigeru Tsukagoshi
IPC分类号： C07H19/09 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7076 , A61P35/02 , C07H19/06 , C07H19/20 , C07H19/08
CPC分类号： C07H19/06 , Y02P20/55 , Y10S514/908
摘要： Compounds represented by formula (I) ##STR1## wherein one of Z.sub.1 ', Z.sub.2 ', Z.sub.3 ' and Z.sub.4 ' represents R, another one of Z.sub.1 ', Z.sub.2 ', Z.sub.3 ' and Z.sub.4 ' represents Z, and the remaining two moieties of Z.sub.1 ', Z.sub.2 ', Z.sub.3 ' and Z.sub.4 ' represents a hydrogen atom and/or a protective group, one of R and Z represents A.sub.1 and the other represents A.sub.2, A.sub.1 being an acyl group having 14 to 22 carbon atoms which does not contain a carboxylic group and A.sub.2 being an acyl group having 2 to 14 carbon atoms and having one carboxyl group, X represents a hydrogen atom or a halogen atom (hereinafter referred to as Compound Ia); a 2,2'-anhydro product of Compound Ia wherein Z.sub.2 ' represents a hydrogen atom (hereinafter referred to as Compound Ib); an arabinosylation product of Compound Ia (hereinafter referred to as Compound Ic); a deamination product of Compound Ia (hereinafter referred to as Compound Id); a 2'-deoxy product of Compound Id wherein Z.sub.2 ' represents a hydrogen atom (hereinafter referred to as Compound Ie); a salt of Compound Ia, Ib, Ic, or Id or Ie having an A.sub.2 group with a base (hereinafter referred to as Compound If); and a salt of Compound Ia, Ib or Ic wherein Z.sub.1 ' represents a hydrogen atom with an acid (hereinafter referred to as Compound Ih); and processes for preparing the same.
摘要翻译：由式（I）表示的化合物其中Z1'，Z2'，Z3'和Z4'之一表示R，Z1'，Z2'，Z3'和Z4'中的另一个表示Z，剩余的 Z1'，Z2'，Z3'和Z4'的两个部分表示氢原子和/或保护基，R和Z之一表示A1，另一个表示A2，A1表示具有14-22个碳原子的酰基，不含羧基，A2为碳原子数2〜14的酰基，具有1个羧基，X表示氢原子或卤素原子（以下称为化合物Ia）。化合物Ia的2,2'-脱水产物，其中Z2'表示氢原子（以下称为化合物Ib）; 化合物Ia的阿拉伯糖基化产物（以下称为化合物Ic）; 化合物Ia的脱氨产物（以下称为化合物Id）; 化合物Id的2'-脱氧产物，其中Z2'表示氢原子（以下称为化合物Ie）; 具有A2基团的化合物Ia，Ib，Ic或Id或Ie的盐（以下称为化合物If）; 和化合物Ia，Ib或Ic的盐，其中Z1'表示氢原子与酸（以下称为化合物Ih）; 及其制备方法。

4. 发明授权

US4055716A N.sup.4 Acyl-1-arabinofuranosylcytosine-5'-esters 失效
标题翻译： N {HU 4 {B酰基-1-阿拉伯呋喃糖基胞嘧啶-5 {40-酯
公开(公告)号：US4055716A
公开(公告)日：1977-10-25
申请号：US675050
申请日：1976-04-08
申请人： Torao Ishida , Takashi Shirai , Minoru Akiyama
发明人： Torao Ishida , Takashi Shirai , Minoru Akiyama
IPC分类号： C07H19/06
CPC分类号： C07H19/06 , Y10S514/908
摘要： N.sup.4 -Acyl-1-.beta.-D-arabinofuranosylcytosine-5'-esters represented by the formula ##STR1## wherein R.sup.1 represents an acyl group having 3 to 28 carbon atoms and R.sup.2 represents an XCH.sub.2, XCH.sub.2 CH.sub.2 or CH.sub.3 CHX group, wherein X represents a halogen atom, a (CH.sub.3).sub.2 N or (C.sub.2 H.sub.5).sub.2 N group.
摘要翻译：由式“IMAGE”表示的N4-酰基-β-D-阿拉伯呋喃糖基胞嘧啶-5'-酯，其中R1表示具有3至28个碳原子的酰基，R2表示XCH2，XCH2CH2或CH3CHX基团，其中X表示卤素原子，（CH 3）2 N或（C 2 H 5）2 N基团。

5. 再颁专利

USRE32637E Physiologically active peptide 失效
标题翻译：生理活性肽
公开(公告)号：USRE32637E
公开(公告)日：1988-04-05
申请号：US881759
申请日：1986-07-03
申请人： Torao Ishida
发明人： Torao Ishida
IPC分类号： C12N15/09 , A61K38/00 , C07K14/52 , C07K14/555 , C07K14/57 , C12N15/00 , C12N15/81 , C12P21/02
CPC分类号： C12N15/81 , C07K14/57 , A61K38/00 , Y02P20/55 , Y10S930/142
摘要： A novel physiologically active peptide represented by the following formula:BCysX.sub.1 CysX.sub.2 CysX.sub.3(wherein B stands for a hydrogen atom or a methionyl group, Cys a cysteine residue, X.sub.1 .[.5 to 9 amino acid residues.]. .Iadd.an isoleucylvalylleucylglycylserylleucylglycine residue, .Iaddend.X.sub.2 .[.one amino acid residue.]. .Iadd.a tyrosine residue.Iaddend., and X.sub.3 .[.138 to 148 amino acid residues.]. .Iadd.a specific sequence of 143 amino acid residues as defined herein.Iaddend.), which is excellent in physiological activities such as antiviral action, cell proliferation inhibitive action and NK (natural killer) cell activity enhancing action.Iadd., and a short sequence peptide represented by the above-mentioned X.sub.3 .Iaddend..

6. 发明授权

US4667017A Method for producing an active protein 失效
标题翻译：生产活性蛋白的方法
公开(公告)号：US4667017A
公开(公告)日：1987-05-19
申请号：US640819
申请日：1984-08-15
申请人： Torao Ishida
发明人： Torao Ishida
IPC分类号： C12N15/09 , C07K1/00 , C07K1/107 , C07K14/52 , C07K14/54 , C07K14/55 , C07K14/555 , C07K14/57 , C12N9/72 , C12P21/00 , C07K1/02
CPC分类号： C12N9/6459 , C07K1/1075 , C07K14/55 , C07K14/57 , C12Y304/21069 , Y02P20/55 , Y10S930/141 , Y10S930/142
摘要： An active protein can be easily, safely produced by a method comprising providing a first peptide fragment having a first amino acid sequence corresponding to part of an active protein and a second peptide fragment having a second amino acid sequence corresponding to the remaining part of the active protein, at least one of said first peptide fragment and said second peptide fragment being one which has been obtained by recombinant DNA technique or has been obtained by a method comprising producing a predetermined peptide fragment by recombinant DNA technique and deleting from or adding to said predetermined peptide fragment at its N-terminus at least one amino acid residue; and linking said first peptide fragment at its C-terminus to said second peptide fragment at its N-terminus. The method of the present invention may be practiced, with further advantages, by predeterming said first peptide fragment and said second peptide fragment so that a first occurring methionine residue subsequent to the N-terminal amino acid residue of the active protein constitutes the N-terminal amino acid of the amino acid sequence of said second peptide fragment, or so that an amino acid residue positioned near the first occurring methionine residue subsequent to the N-terminal amino acid residue of the desired protein on the side of the N-terminus of the desired protein constitutes the N-terminal amino acid residue of said second peptide fragment.
摘要翻译：通过包括提供具有对应于活性蛋白的一部分的第一氨基酸序列的第一肽片段和具有对应于活性成分的剩余部分的第二氨基酸序列的第二肽片段的方法可以容易地，安全地产生活性蛋白质蛋白质，所述第一肽片段和所述第二肽片段中的至少一个是通过重组DNA技术获得的或通过包括通过重组DNA技术产生预定肽片段并从所述预定肽片段在其N末端至少有一个氨基酸残基; 以及在其N-末端将所述第一肽片段在其C末端与所述第二肽片段连接。本发明的方法可以通过预先使用所述第一肽片段和所述第二肽片段进一步实现，使得活性蛋白质的N-末端氨基酸残基之后的第一个出现的甲硫氨酸残基构成N-末端或所述第二肽片段的氨基酸序列的氨基酸，或者使得位于所述第二肽片段的N末端侧的所需蛋白质的N-末端氨基酸残基之后的第一产生的甲硫氨酸残基附近的氨基酸残基所需蛋白质构成所述第二肽片段的N-末端氨基酸残基。

7. 发明授权

US4393225A AI-77 Compounds and pharmaceutically acceptable salts thereof 失效
标题翻译： AI-77其化合物及其药学上可接受的盐
公开(公告)号：US4393225A
公开(公告)日：1983-07-12
申请号：US167581
申请日：1980-07-11
申请人： Hiroshi Hayashi , Yukiji Shimojima , Takashi Shirai , Torao Ishida , Mitsuru Shibukawa
发明人： Hiroshi Hayashi , Yukiji Shimojima , Takashi Shirai , Torao Ishida , Mitsuru Shibukawa
IPC分类号： C07D311/76 , C12P13/02 , C12P17/06 , C12P17/16
CPC分类号： C12R1/07 , C07D311/76 , C12P13/02 , C12P17/06 , C12P17/162
摘要： AI-77 compounds, pharmaceutically acceptable salts thereof, and a process for the preparation thereof are described, said compounds having the formulae ##STR1## wherein: X is NR.sub.6 or O; Y is NHR.sub.5 or combine with Z to provide a link for bonding C and C; Z is H or combines with Y to provide a link for bonding C and C; R.sub.1, R.sub.3 and R.sub.5 are each H, R', --CH.sub.2 R, or --COR; R.sub.6 is H or R; R.sub.7 is H, R or CH.sub.2 R; R is a hydrocarbon group consisting of a saturated or unsaturated straight or branched aliphatic group of C.sub.1 to C.sub.17, an aromatic group of C.sub.6 to C.sub.10, a cage type group of C.sub.7 to C.sub.10, a monocyclic aliphatic group of C.sub.3 to C.sub.8, an aromatic-aliphatic group of C.sub.7 to C.sub.15, a heterocyclic hydrocarbon of C.sub.1 to C.sub.9, wherein the above hydrocarbons can be substituted with one or more groups selected from halogen, oxo, carboxyl, hydroxyl, a saturated or unsaturated straight or branched aliphatic group of C.sub.1 to C.sub.5, an aromatic group of C.sub.6 to C.sub.10, a monocyclic aliphatic group of C.sub.3 to C.sub.8, an aromatic-aliphatic group of C.sub.7 to C.sub.11, alkoxy of C.sub.1 to C.sub.5, thioalkoxyl of C.sub.1 to C.sub.5, carboalkoxyl of C.sub.1 to C.sub.6, acyl of C.sub.1 to C.sub.5, acyloxy of C.sub.2 to C.sub.6 and a heterocyclic group of C.sub.1 to C.sub.9 ; R' is the same as R exclusive of those groups wherein unsaturated carbon or tertiary carbon is directly bonded to O or N; R.sub.2 is H, or combines with T.sub.1 to provide a link for bonding C and O in a lactone ring; T.sub.1 is OH or combines with R.sub.2 to provide a link for bonding C and O in a lactone ring; R.sub.4 is H or combines with T.sub.2 to provide a link for bonding C and O in a lactone ring; and T.sub.2 is OH or combines with R.sub.4 to provide a link for bonding C and O in a lactone ring; and pharmaceutically acceptable salts thereof.
摘要翻译：描述了具有下式的化合物：其中：X为NR6或O;其中：X为NR6或O; Y是NHR5或与Z结合以提供用于键合C和C的连接; Z是H或与Y结合以提供用于键合C和C的连接; R1，R3和R5各自为H，R'，-CH2R或-COR; R6是H或R; R7是H，R或CH2R; R是由C 1〜C 17的饱和或不饱和直链或支链脂族基团，C6〜C10的芳香族基团，C7〜C10的保持基团，C3〜C8的单环式脂肪族基团，芳香族 - C 7〜C 15的脂族基团，C 1〜C 9的杂环烃，其中上述烃可以被一个或多个选自卤素，氧代，羧基，羟基，C1至C5的饱和或不饱和直链或支链脂族基团的基团取代，C 6〜C 10的芳基，C 3〜C 8的单环脂族基，C 7〜C 11的芳香族 - 脂肪族基，C 1〜C 5的烷氧基，C 1〜C 5的烷氧基，C 1〜C 6的碳烷氧基， C5，C2〜C6的酰氧基和C1〜C9的杂环基; R'与R不同，其中不饱和碳或叔碳直接与O或N键合; R2是H或与T1结合以提供用于在内酯环中键合C和O的连接; T1是OH或与R2结合以提供用于在内酯环中键合C和O的连接; R4是H或与T2结合以提供用于在内酯环中键合C和O的连接; 并且T2是OH或与R4结合以提供用于在内酯环中键合C和O的连接; 及其药学上可接受的盐。

8. 发明授权

US4314059A Process for preparing cephalosporin compounds 失效
标题翻译：制备头孢菌素化合物的方法
公开(公告)号：US4314059A
公开(公告)日：1982-02-02
申请号：US172553
申请日：1980-07-28
申请人： Chisei Shibuya , Kunihiko Ishii , Takumi Sano , Torao Ishida
发明人： Chisei Shibuya , Kunihiko Ishii , Takumi Sano , Torao Ishida
IPC分类号： A01N43/90 , C07D417/12 , C07D501/36 , C07D501/06
CPC分类号： C07D501/36 , A01N43/90 , C07D417/12 , Y10S514/923
摘要： An 1,3,4-thiadiazole-5-thiol ester of the formula, ##STR1## wherein R is a hydrogen atom or a methyl group, a process for their preparation and a process for preparing a cephalosporin compound of the formula, ##STR2## wherein R is the same as defined above, using the above described 1,3,4-thiadiazole-5-thiol ester.
摘要翻译：下式的1,3,4-噻二唑-5-硫醇酯，其中R是氢原子或甲基，其制备方法和制备下式的头孢菌素化合物的方法其中R与上述相同，使用上述1,3,4-噻二唑-5-硫醇酯。

9. 发明授权

US4457867A Physiologically active peptide 失效
标题翻译：生理活性肽
公开(公告)号：US4457867A
公开(公告)日：1984-07-03
申请号：US450721
申请日：1982-12-17
申请人： Torao Ishida
发明人： Torao Ishida
IPC分类号： C12N15/09 , A61K38/00 , C07K14/52 , C07K14/555 , C07K14/57 , C12N15/00 , C12N15/81 , C12P21/02 , C07C103/52
CPC分类号： C12N15/81 , C07K14/57 , A61K38/00 , Y02P20/55 , Y10S930/142
摘要： A novel physiologically active peptide represented by the following formula:BCysX.sub.1 CysX.sub.2 CysX.sub.3(wherein B stands for a hydrogen atom or a methionyl group, Cys a cysteine residue, X.sub.1 5 to 9 amino acid residues, X.sub.2 one amino acid residue, and X.sub.3 138 to 148 amino acid residues), which is excellent in physiological activities such as antiviral action, cell proliferation inhibitive action and NK (natural killer) cell activity enhancing action.
摘要翻译：由下式表示的新型生理活性肽：BCysX1CysX2CysX3（其中B表示氢原子或甲硫氨酰基，Cys a半胱氨酸残基，X1-59个氨基酸残基，X2一个氨基酸残基，X3 138〜148氨基酸残基），其具有优异的生理活性，如抗病毒作用，细胞增殖抑制作用和NK（自然杀伤）细胞活性增强作用。

10. 发明授权

US4258195A Novel thiol esters and process for preparing cephalosporin compounds using same 失效
标题翻译：新型巯基酯和使用其制备头孢菌素化合物的方法
公开(公告)号：US4258195A
公开(公告)日：1981-03-24
申请号：US18755
申请日：1979-03-08
申请人： Chisei Shibuya , Kunihiko Ishii , Takumi Sano , Torao Ishida
发明人： Chisei Shibuya , Kunihiko Ishii , Takumi Sano , Torao Ishida
IPC分类号： C07D501/06 , A01N43/90 , C07D417/12 , C07D501/36 , A01N43/82 , A61K31/425 , C07D501/56
CPC分类号： C07D501/36 , A01N43/90 , C07D417/12
摘要： An 1,3,4-thiadiazole-5-thiol ester of the formula, ##STR1## wherein R is a hydrogen atom or a methyl group, a process for their preparation and a process for preparing a cephalosporin compound of the formula, ##STR2## wherein R is the same as defined above, using the above described 1,3,4-thiadiazole-5-thiol ester.
摘要翻译：下式的1,3,4-噻二唑-5-硫醇酯，其中R是氢原子或甲基，其制备方法和制备下式的头孢菌素化合物的方法 + TR 其中R与上述相同，使用上述1,3,4-噻二唑-5-硫醇酯。

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