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1. 发明授权

US08017809B2 Bisboron compound 有权
标题翻译： Bisboron化合物
公开(公告)号：US08017809B2
公开(公告)日：2011-09-13
申请号：US12094968
申请日：2006-11-24
申请人： Katsuhiko Mikoshiba , Shoichiro Ozaki , Akinobu Suzuki , Takeshi Nakamura , Kyoko Nakamura, legal representative , Aiko Nakamura, legal representative
发明人： Katsuhiko Mikoshiba , Shoichiro Ozaki , Akinobu Suzuki , Takeshi Nakamura
IPC分类号： C07F5/02 , A61K31/69
CPC分类号： C07F5/025
摘要： A bisboron compound represented by the general formula (I): wherein B represents a boron atom, Y represents an oxygen or sulfur atom, R1 and R2 independently represent a monocyclic aromatic group, a polycyclic aromatic group, or a heterocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur atoms, R3 represents a hydrogen atom; —(CH2)m—NR4R5; —CO—(CH2)m—NR4R5; —COCH(NH2)R6; —CHR7R8; —CH2CH(NH2)—R9; quinolyl substituted with C1-C4 alkyl group; or C1-C4 alkyl substituted with pyridyl, piperidino or pyrrolidinyl group, and X represents a monocyclic aromatic group, a polycyclic aromatic group or a heterocyclic group, which may be the same as or different from R1 and R2, or a bifunctional group having a monocyclic aromatic group, polycyclic aromatic group or heterocyclic group bonded to each side of a group selected from the group consisting of a single bond, O, CH2, S, SO2, CH2OCH2, OCH2, OCH2CH2OCH2, OCH2OCH2CH2 and CH2OCH2CH2, or a salt thereof, and a composition for controlling the intracellular calcium concentration, which comprises the compound or salt thereof as an active ingredient.
摘要翻译：由通式（I）表示的双硼化合物：其中B表示硼原子，Y表示氧或硫原子，R1和R2独立地表示单环芳基，多环芳基或含有至少一个选自氧，氮和硫原子的杂原子，R 3表示氢原子; - （CH 2）m -NR 4 R 5; -CO-（CH 2）m -NR 4 R 5; -COCH（NH 2）R 6; -CHR7R8; -CH 2 CH（NH 2）-R 9; 被C1-C4烷基取代的喹啉基; 或被吡啶基，哌啶子基或吡咯烷基取代的C1-C4烷基，X表示可以与R1和R2相同或不同的单环芳基，多环芳基或杂环基，或具有或选自由单键，O，CH2，S，SO2，CH2OCH2，OCH2，OCH2CH2OCH2，OCH2OCH2CH2和CH2OCH2CH2组成的组中的一个基团键合的单环芳基，多环芳基或杂环基，或其盐，以及用于控制细胞内钙浓度的组合物，其包含其化合物或其盐作为活性成分。

2. 发明申请

US20100087645A1 NOVEL BISBORON COMPOUND 有权
标题翻译：新颖的BISBONON化合物
公开(公告)号：US20100087645A1
公开(公告)日：2010-04-08
申请号：US12094968
申请日：2006-11-24
申请人： Katsuhiko Mikoshiba , Shoichiro Ozaki , Akinobu Suzuki , Takeshi Nakamura
发明人： Katsuhiko Mikoshiba , Shoichiro Ozaki , Akinobu Suzuki , Takeshi Nakamura
IPC分类号： C07F5/02
CPC分类号： C07F5/025
摘要： A bisboron compound represented by the general formula (I): wherein B represents a boron atom, Y represents an oxygen or sulfur atom, R1 and R2 independently represent a monocyclic aromatic group, a polycyclic aromatic group, or a heterocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur atoms, R3 represents a hydrogen atom; —(CH2)m—NR4R5; —CO—(CH2)m—NR4R5; —COCH(NH2)R6; —CHR7R8; —CH2CH(NH2)—R9; quinolyl substituted with C1-C4 alkyl group; or C1-C4 alkyl substituted with pyridyl, piperidino or pyrrolidinyl group, and X represents a monocyclic aromatic group, a polycyclic aromatic group or a heterocyclic group, which may be the same as or different from R1 and R2, or a bifunctional group having a monocyclic aromatic group, polycyclic aromatic group or heterocyclic group bonded to each side of a group selected from the group consisting of a single bond, O, CH2, S, SO2, CH2OCH2, OCH2, OCH2CH2OCH2, OCH2OCH2CH2 and CH2OCH2CH2, or a salt thereof, and a composition for controlling the intracellular calcium concentration, which comprises the compound or salt thereof as an active ingredient.
摘要翻译：由通式（I）表示的双硼化合物：其中B表示硼原子，Y表示氧或硫原子，R1和R2独立地表示单环芳基，多环芳基或含有至少一个选自氧，氮和硫原子的杂原子，R 3表示氢原子; - （CH 2）m -NR 4 R 5; -CO-（CH 2）m -NR 4 R 5; -COCH（NH 2）R 6; -CHR7R8; -CH 2 CH（NH 2）-R 9; 被C1-C4烷基取代的喹啉基; 或被吡啶基，哌啶子基或吡咯烷基取代的C1-C4烷基，X表示可以与R1和R2相同或不同的单环芳基，多环芳基或杂环基，或具有或选自由单键，O，CH2，S，SO2，CH2OCH2，OCH2，OCH2CH2OCH2，OCH2OCH2CH2和CH2OCH2CH2组成的组中的一个基团键合的单环芳基，多环芳基或杂环基，或其盐，以及用于控制细胞内钙浓度的组合物，其包含其化合物或其盐作为活性成分。

3. 发明授权

US08853424B2 Protein cross-linking inhibitor 有权
标题翻译：蛋白质交联抑制剂
公开(公告)号：US08853424B2
公开(公告)日：2014-10-07
申请号：US13058647
申请日：2009-08-11
申请人： Katsuhiko Mikoshiba , Nobuyuki Nukina , Shoichiro Ozaki , Kouzo Hamada , Jun-Ichi Goto , Akinobu Suzuki , Etsuko Ebisui , Akiko Terauchi
发明人： Katsuhiko Mikoshiba , Nobuyuki Nukina , Shoichiro Ozaki , Kouzo Hamada , Jun-Ichi Goto , Akinobu Suzuki , Etsuko Ebisui , Akiko Terauchi
IPC分类号： C07D333/00 , A61K31/67 , C07F5/02 , A61K31/69
CPC分类号： C07F5/025 , A61K31/69
摘要： The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof: R3—[—X—B(ZR1)—Y—B(ZR2)—W—]n—R4, (1) R3—[—X—B(ZR1)—Y—]n—R4, (2) R3—[—B(ZR1)—Y—B(ZR2)—W—]n—R4, (3) R3—[—X—B(ZR1)—]n—R4, (4) R3—[—B(ZR2)—W—]n—R4, (5) R3—X—B(ZR1)-T[B(ZR2)—W—R4]2, (6) R3—B(OH)2, (7) R3—B(ZR1)—X—B(ZR2)—R4, (8) R3—B(R1)—O—B(R2)—R4, (9) R3—[—X—B(ZR1)—Y—B(ZR2)—]n—R4, (10) R3—[—X—B(ZR1)—Y—B(ZR2)—W-Q-]n—R4, (11) R3—[—P—X—B(ZR1)—Y—B(ZR2)—W—]n—R4, (12) [R3—X—B(ZR1)—Y]2B(ZR2), (13) wherein each symbol is as defined in the DESCRIPTION.
摘要翻译：本发明提供一种蛋白质交联抑制剂，其含有下述式（1） - （13）中任一项所示的化合物或其药学上可接受的盐：R3 - [ - X-B（ZR1）-Y-B ZR2）-W-] n-R4，（1）R3 - [ - X-B（ZR1）-Y-] n-R4，（2）R3 - [ - B（ZR1）-Y-B（ZR2） - W - ] n-R4，（3）R3 - [ - X-B（ZR1） - ] n-R4，（4）R3 - [ - B（ZR2）-W-] n-R4，（5） X-B（ZR1）-T [B（ZR2）-W-R4] 2，（6）R3-B（OH）2，（7）R3-B（ZR1）-X-B（ZR2）-R4，（8）R3-B（R1）-O-B（R2）-R4，（9）R3 - [ - X-B（ZR1）-Y-B（ZR2） - ] n-R4，（10） [-X-B（ZR1）-Y-B（ZR2）-WQ-] n-R4，（11）R3 - [ - P-X-B（ZR1）-Y-B（ZR2）-W-] n -R4，（12）[R3-X-B（ZR1）-Y] 2B（ZR2），（13）其中每个符号如说明书中所定义。

4. 发明申请

US20110212919A1 PROTEIN CROSS-LINKING INHIBITOR 有权
标题翻译：蛋白交联抑制剂
公开(公告)号：US20110212919A1
公开(公告)日：2011-09-01
申请号：US13058647
申请日：2009-08-11
申请人： Katsuhiko Mikoshiba , Nobuyuki Nukina , Shoichiro Ozaki , Kouzo Hamada , Jun-Ichi Goto , Akinobu Suzuki , Etsuko Ebisui , Akiko Terauchi
发明人： Katsuhiko Mikoshiba , Nobuyuki Nukina , Shoichiro Ozaki , Kouzo Hamada , Jun-Ichi Goto , Akinobu Suzuki , Etsuko Ebisui , Akiko Terauchi
IPC分类号： A61K31/69 , C07F5/02 , C07F5/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P27/12 , A61P3/00 , A61P17/00 , A61P7/00
CPC分类号： C07F5/025 , A61K31/69
摘要： The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas (1)-(13), or a pharmaceutically acceptable salt thereof: R3—[—X—B(ZR1)—Y—B(ZR2)—W—]n—R4, (1) R3—[—X—B(ZR1)—Y—]n—R4, (2) R3—[—B(ZR1)—Y—B(ZR2)—W—]n—R4, (3) R3—[—X—B(ZR1)—]n—R4, (4) R3—[—B(ZR2)—W—]n—R4, (5) R3—X—B(ZR1)-T[B(ZR2)—W—R4]2, (6) R3—B(OH)2, (7) R3—B(ZR1)—X—B(ZR2)—R4, (8) R3—B(R1)—O—B(R2)—R4, (9) R3—[—X—B(ZR1)—Y—B(ZR2)—]n—R4, (10) R3—[—X—B(ZR1)—Y—B(ZR2)—W-Q-]n—R4, (11) R3—[—P—X—B(ZR1)—Y—B(ZR2)—W—]n—R4, (12) [R3—X—B(ZR1)—Y]2B(ZR2), (13) wherein each symbol is as defined in the DESCRIPTION.
摘要翻译：本发明提供一种蛋白质交联抑制剂，其含有下述式（1） - （13）中任一项所示的化合物或其药学上可接受的盐：R3 - [ - X-B（ZR1）-Y-B ZR2）-W-] n-R4，（1）R3 - [ - X-B（ZR1）-Y-] n-R4，（2）R3 - [ - B（ZR1）-Y-B（ZR2） - W - ] n-R4，（3）R3 - [ - X-B（ZR1） - ] n-R4，（4）R3 - [ - B（ZR2）-W-] n-R4，（5） X-B（ZR1）-T [B（ZR2）-W-R4] 2，（6）R3-B（OH）2，（7）R3-B（ZR1）-X-B（ZR2）-R4，（8）R3-B（R1）-O-B（R2）-R4，（9）R3 - [ - X-B（ZR1）-Y-B（ZR2） - ] n-R4，（10） [-X-B（ZR1）-Y-B（ZR2）-WQ-] n-R4，（11）R3 - [ - P-X-B（ZR1）-Y-B（ZR2）-W-] n -R4，（12）[R3-X-B（ZR1）-Y] 2B（ZR2），（13）其中每个符号如说明书中所定义。

5. 发明授权

US4952717A Myoinositol derivatives and preparation process thereof 失效
标题翻译：肌醇衍生物及其制备方法
公开(公告)号：US4952717A
公开(公告)日：1990-08-28
申请号：US131049
申请日：1987-10-20
申请人： Shoichiro Ozaki , Yutaka Watanabe , Akira Awaya , Yusaku Ishizuka
发明人： Shoichiro Ozaki , Yutaka Watanabe , Akira Awaya , Yusaku Ishizuka
IPC分类号： C07C29/00 , C07C35/16 , C07C43/18 , C07C43/188 , C07C43/196 , C07C43/235 , C07D317/46 , C07D317/72 , C07D493/04 , C07F9/117 , C07F9/24
CPC分类号： C07C43/196 , C07C43/188 , C07F9/117
摘要： Disclosed herein are phosphoric acid esters of myoinositol, which are represented by the following general formula (I): ##STR1## and their salts, as well as a preparation process thereof. The myoinositol derivatives can each be obtained by causing a phosphorylating agent to act on a myoinositol derivative substituted with catalytic reduction removable substituent groups at the positions other than those desired to be substituted by phosphoric acid residual groups and then catalytically reducing the thus-phosphorylated myoinositol.

6. 发明授权

US4376768A Benzothiazine derivative 失效
标题翻译：苯并噻嗪衍生物
公开(公告)号：US4376768A
公开(公告)日：1983-03-15
申请号：US274229
申请日：1981-06-16
申请人： Shoichiro Ozaki , Hideya Kobayashi , Haruki Mori , Takafumi Kitano , Hiroshi Kawazura , Yutaka Okazaki
发明人： Shoichiro Ozaki , Hideya Kobayashi , Haruki Mori , Takafumi Kitano , Hiroshi Kawazura , Yutaka Okazaki
IPC分类号： C07D417/12 , A61K31/54 , A61P29/00 , C07D213/73
CPC分类号： C07D213/73
摘要： N-(6-chloro-2-pyridyl)-3,4-dihydro-2-methyl-4-oxo-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide that is a novel benzothiazine derivative. The compound is characterized by a low degree of toxicity and a low incidence of gastric disorders and useful as an anti-inflammatory agent.
摘要翻译：作为新的苯并噻嗪衍生物的N-（6-氯-2-吡啶基）-3,4-二氢-2-甲基-4-氧代-2H-1,2-苯并噻嗪-3-甲酰胺1,1-二氧化物。该化合物的特征在于毒性低，胃疾病发生率低，可用作抗炎剂。

7. 发明授权

US5091549A Synthesis of D-myoinositol-1-phosphate 失效
标题翻译： D-木糖醇-1-磷酸酯的合成
公开(公告)号：US5091549A
公开(公告)日：1992-02-25
申请号：US575615
申请日：1990-08-31
申请人： Shoichiro Ozaki , Takahiko Akiyama , Naoto Takechi , Kunio Kageyama , Morihisa Machida
发明人： Shoichiro Ozaki , Takahiko Akiyama , Naoto Takechi , Kunio Kageyama , Morihisa Machida
IPC分类号： C07F7/18 , C07F9/117 , C07F9/6574
CPC分类号： C07F9/117 , Y02P20/55
摘要： A method of synthesizing D-myoinositol-1-phosphate from 1,2-(R.sup.1)-3-R.sup.2 -myoinositol compounds of the formula ##STR1## wherein R.sup.1 is a bridging type protective group bonded to two oxygen atoms at the 1- and 2-position, and R.sup.2 is a protective group coupled to the oxygen atom at the 3-position. D-Myoinositol-1-phosphate is useful as an intermediate for the production of inositol-1,4,5-triphosphate.
摘要翻译：由式（IMA）的1,2-（R1）-3-R2-肌醇化合物合成D-肌醇-1-磷酸的方法，其中R 1是在1位上与两个氧原子键合的桥连型保护基， 2位，R2是与3位上的氧原子连接的保护基。 D-肌醇-1-磷酸可用作生产肌醇-1,4,5-三磷酸的中间体。

8. 发明授权

US4032524A 1-Carbamoyl-5-fluorouracil derivatives 失效
标题翻译： 1-CARBAMOYL-5-FLUOROURACIL DORIVATIVES
公开(公告)号：US4032524A
公开(公告)日：1977-06-28
申请号：US726196
申请日：1976-09-24
申请人： Shoichiro Ozaki , Haruki Mori
发明人： Shoichiro Ozaki , Haruki Mori
IPC分类号： A61K31/505 , C07D239/54 , C07D239/553 , C07D239/10
CPC分类号： C07D239/553 , A61K31/505 , C07D239/54 , Y10S514/908
摘要： 1-Carbamoyl-5-fluorouracil derivatives represented by the formula ##STR1## wherein R.sub.1 represents methyl, ethyl, phenyl or cyclohexyl and R.sub.2 represents hydrogen or is the same as R.sub.1 are effective anti-metabolites useful in treating lymphatic leukemia L1210, sarcoma 180A and Ehrlich ascites carcinoma in mice.

9. 发明授权

US4376119A Benzothiazine derivative 失效
标题翻译：苯并噻嗪衍生物
公开(公告)号：US4376119A
公开(公告)日：1983-03-08
申请号：US274209
申请日：1981-06-16
申请人： Shoichiro Ozaki , Hideya Kobayashi , Haruki Mori , Hiroshi Kawazura , Yutaka Okazaki , Takafumi Kitano , Mikio Kumakura , Takuo Nakano
发明人： Shoichiro Ozaki , Hideya Kobayashi , Haruki Mori , Hiroshi Kawazura , Yutaka Okazaki , Takafumi Kitano , Mikio Kumakura , Takuo Nakano
IPC分类号： C07D417/12 , A61K31/54 , A61P29/00 , C07D213/73
CPC分类号： C07D213/73
摘要： N-(6-fluoro-2-pyridyl)-3,4-dihydro-2-methyl-4-oxo-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide that is a novel benzothiazine derivative. The compound is characterized by a low degree of toxicity and a low incidence of gastric disorders and useful as an anti-inflammatory agent.
摘要翻译：作为新的苯并噻嗪衍生物的N-（6-氟-2-吡啶基）-3,4-二氢-2-甲基-4-氧代-2H-1,2-苯并噻嗪-3-甲酰胺1,1-二氧化物。该化合物的特征在于毒性低，胃疾病发生率低，可用作抗炎剂。

10. 发明授权

US4267326A Uracil derivatives 失效
标题翻译：尿嘧啶衍生物
公开(公告)号：US4267326A
公开(公告)日：1981-05-12
申请号：US15149
申请日：1979-02-26
申请人： Shoichiro Ozaki , Yoshimasa Ike , Katsutoshi Ishikawa , Haruki Mori
发明人： Shoichiro Ozaki , Yoshimasa Ike , Katsutoshi Ishikawa , Haruki Mori
IPC分类号： C07D239/545 , A61K31/495 , A61K31/505 , A61K31/513 , A61P35/00 , C07D239/54 , C07D239/553
CPC分类号： C07D239/553
摘要： New uracil derivatives of the general formula: ##STR1## wherein R.sup.1 stands for a hydrogen atom or a grouping of the formula: ##STR2## R.sup.2 for a hydrogen atom, an alkyl group or a phenyl group and R.sup.3 for an alkyl group or a phenyl group, with the proviso that when both R.sup.1 and R.sup.2 stand for a hydrogen atom, R.sup.3 stands for a phenyl group or a straight chain alkyl group with 3.about.11 carbon atoms, that when R.sup.1 stands for a hydrogen atom and R.sup.2 for methyl group, R.sup.3 stands for an alkyl group with at least 2 carbon atoms or a phenyl group, and that when R.sup.1 stands for a hydrogen atom and R.sup.3 for methyl group, R.sup.2 stands for an alkyl group with at least 2 carbon atoms or a phenyl group. These uracil derivatives are prepared by reacting 5-fluorouracil with an .alpha.-haloalkyl carboxylate or with an aldehyde diacylate or by hydrolyzing a 1,3-bis(acyloxymethyl)-5-fluorouracil with an acid or alkali. These uracil derivatives are useful as improved anti-tumor agents especially for oral administration and injection.
摘要翻译：其中R1代表氢原子的新的尿嘧啶衍生物或氢原子，烷基或苯基基团的下式的分子式：R 2，烷基或苯基的R 3 基团，条件是当R1和R2均表示氢原子时，R3表示具有3个碳原子的苯基或直链烷基，当R1表示氢原子且R2表示甲基时， R3表示具有至少2个碳原子的烷基或苯基，当R1表示氢原子且R3表示甲基时，R2表示具有至少2个碳原子的烷基或苯基。这些尿嘧啶衍生物通过5-氟尿嘧啶与α-卤代烷基羧酸酯或二醛酸醛反应或通过用酸或碱水解1,3-双（酰氧基甲基）-5-氟尿嘧啶来制备。这些尿嘧啶衍生物可用作改进的抗肿瘤剂，特别是用于口服给药和注射。

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