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1. 发明授权

US4668820A Method of preparing polyprenyl compounds or mixtures thereof 失效
标题翻译：聚异戊二烯基化合物或其混合物的制备方法
公开(公告)号：US4668820A
公开(公告)日：1987-05-26
申请号：US722173
申请日：1985-04-10
申请人： Koichi Ibata , Tetsuo Takigawa , Masafumi Okada , Masao Mizuno , Takashi Nishida
发明人： Koichi Ibata , Tetsuo Takigawa , Masafumi Okada , Masao Mizuno , Takashi Nishida
IPC分类号： C07C69/007 , C07C27/00 , C07C29/74 , C07C29/76 , C07C29/88 , C07C33/02 , C07C67/00 , C07C67/54 , C07C69/025 , C08F8/12 , C08F8/14 , C07C67/48 , C07C67/52
CPC分类号： C07C33/02 , C07C29/76
摘要： Polyprenols or esters thereof, which are similar in the trans and cis configurations to dolichol, or mixtures thereof are obtained from the leaves of plants belonging to the genus Pinus L. of the family Pinaceae by extraction, if necessary followed by hydrolysis, esterification or transesterification or a combination thereof. These polyprenyl compounds and mixtures thereof are useful as favorable starting materials for the synthesis of dolichol.
摘要翻译：通过提取，如果需要，然后进行水解，酯化或酯交换，从属于松果科属松属植物的植物的叶子获得反式和顺式构型与二醇的类似的聚螺旋体或其酯或其混合物或其组合。这些聚异戊二烯基化合物及其混合物可用作合成双氯酚的有利原料。

2. 发明授权

US4564477A Polyprenyl compounds and method of producing the same 失效
标题翻译：聚丙烯基化合物及其制备方法
公开(公告)号：US4564477A
公开(公告)日：1986-01-14
申请号：US467253
申请日：1983-02-17
申请人： Tetsuo Takigawa , Koichi Ibata , Masafumi Okada , Masao Mizuno , Takashi Nishida
发明人： Tetsuo Takigawa , Koichi Ibata , Masafumi Okada , Masao Mizuno , Takashi Nishida
IPC分类号： C07C29/14 , C07C29/147 , C07C45/29 , C07C45/30 , C07C45/59 , C07C45/67 , C07C47/21 , C07C49/203 , C07C57/03 , C07C69/587 , C07D295/02 , C07D295/03 , C07D295/185 , C09F5/00
CPC分类号： C07D295/185 , C07C255/00 , C07C29/14 , C07C29/147 , C07C45/292 , C07C45/298 , C07C45/305 , C07C45/59 , C07C45/676 , C07C47/21 , C07C49/203 , C07C57/03 , C07D295/03
摘要： There are provided polyprenyl compounds of the formula ##STR1## wherein ##STR2## represent a trans-isoprene unit and a cis-isoprene unit, respectively, n is an integer of 11-19, Z.sup.1 and Z.sup.2 combinedly represent .dbd.O, .dbd.CH--COOH,.dbd.CH--COOR.sup.1, .dbd.CH--CN, .dbd.C(CN)COOR.sup.2, .dbd.CH--CO--NH.sub.2, .dbd.CH--CO--N(R.sup.3) (R.sup.4), .dbd.CH--CO--NHR.sup.5, .dbd.CH--CH.sub.2 --N(R.sup.3) (R.sup.4), .dbd.CH--CH.sub.2 --NHR.sup.5 or .dbd.CH--CHO or Z.sup.1 is a hydrogen atom and Z.sup.2 is --CH.sub.2 COOH, --CH.sub.2 COOR.sup.6, --CH(CN)COOR.sup.2, --CH.sub.2 CN, --CH.sub.2 --CO--NH.sub.2, --CH.dbd.CH--N(R.sup.3) (R.sup.4) or --CH.sub.2 --CH.dbd.N--R.sup.5, R.sup.1, R.sup.2 and R.sup.6 each being a lower alkyl group, R.sup.3 and R.sup.4 each independently being a lower-alkyl, cycloalkyl, aryl or aralkyl group or R.sup.3 and R.sup.4 combinedly representing an alkylene group containing 2-5 carbon atoms, and R.sup.5 being a lower-alkyl, cycloalkyl, aryl or aralkyl group. These polyprenyl compounds can be synthesized starting with a polyprenol obtainable from leaves of a plant such as Ginkgo biloba or Cedrus deodara by extraction and as necessary followed by hydrolysis, or a reactive derivative thereof. The polyprenyl compounds are useful as intermediates for the synthesis of dolichol without the use of an expensive C.sub.5 chain extender.
摘要翻译：提供下式的聚异戊二烯基化合物：其中，“IMAGE”分别代表异戊二烯单元和顺式异戊二烯单元，n为11-19的整数，Z1和Z2组合表示 = CH 2 COOR 1 = CH-COOR 1 = CH-CN = C（CN）COOR 2 = CH-CO-NH 2 = CH-CO-N（R3）（R4） NHR 5，= CH-CH 2 -N（R 3）（R 4），= CH-CH 2 -NHR 5或= CH-CHO或Z 1是氢原子，Z 2是-CH 2 COOH，-CH 2 COOR 6，-CH（CN）COOR 2，-CH 2 CN ，-CH 2 -CO-NH 2，-CH = CH-N（R 3）（R 4）或-CH 2 -CH = N-R 5，R 1，R 2和R 6各自为低级烷基，R 3和R 4各自独立地为低级 - 烷基，环烷基，芳基或芳烷基或R3和R4组合表示含2-5个碳原子的亚烷基，R5为低级烷基，环烷基，芳基或芳烷基。这些聚异戊二烯基化合物可以从通过提取从植物如银杏叶或Cedrus deodara的叶获得的聚异戊二烯开始合成，并且根据需要随后进行水解或其活性衍生物合成。聚异戊二烯基化合物可用作合成Dolichol而不使用昂贵的C5扩链剂的中间体。

3. 发明授权

US4792615A Method of producing .alpha.-dihydropolyprenyl monophosphates 失效
标题翻译： α-二氢聚丙烯基单磷酸盐的制备方法
公开(公告)号：US4792615A
公开(公告)日：1988-12-20
申请号：US429
申请日：1986-12-22
申请人： Naoshi Nakagawa , Tetsuo Takigawa , Akira Kageyu , Michiya Shimamura , Masafumi Okada , Masao Mizuno
发明人： Naoshi Nakagawa , Tetsuo Takigawa , Akira Kageyu , Michiya Shimamura , Masafumi Okada , Masao Mizuno
IPC分类号： C07F9/113 , C07H11/04 , C07F9/09
CPC分类号： C07H11/04 , C07F9/113
摘要： A method of producing .alpha.-dihydropolyprenyl monophosphates from .alpha.-dihydropolyprenols through .alpha.-dihydropolyprenyl dichlorophosphates in good yield and with ease is provided. A method of producing .alpha.-dihydropolyprenyl dichlorophosphates which are intermediate compounds useful for the first-mentioned method is also provided.
摘要翻译：提供了从α-二氢聚戊二醇通过α-二氢聚丙烯基二氯磷酸盐以良好的产率和容易地制备α-二氢聚芘基单磷酸酯的方法。还提供了用于第一种方法的中间体化合物的制备α-二氢聚丙烯基二氯磷酸盐的方法。

4. 发明授权

US4603208A Certain polyprenyl intermediates 失效
标题翻译：某些聚异戊烯中间体
公开(公告)号：US4603208A
公开(公告)日：1986-07-29
申请号：US465483
申请日：1983-02-10
申请人： Takashi Onishi , Shigeaki Suzuki , Fumio Mori , Tetsuo Takigawa , Yoshiji Fujita , Masao Mizuno , Takashi Nishida
发明人： Takashi Onishi , Shigeaki Suzuki , Fumio Mori , Tetsuo Takigawa , Yoshiji Fujita , Masao Mizuno , Takashi Nishida
IPC分类号： C07C69/767 , C07C317/00 , C07C317/24 , C07D213/70 , C07D213/71 , C07D309/12 , C07D317/18 , C07D405/12 , C07D417/12 , C07F7/18 , C07C69/78 , C07C147/103
CPC分类号： C07D405/12 , C07C317/00 , C07C321/00 , C07D309/12 , C07D317/18 , C07D417/12 , C07F7/1852
摘要： Novel polyprenyl compounds have the general formula: ##STR1## represents a cis-isoprene unit, n is an integer of 11-19, Z.sup.1 is --CH.sub.2 OH or a functional precursor thereof, and either one of R.sup.1 and R.sup.2 is a hydrogen atom and the other is --S(O).sub.m R.sup.3 in which m is an integer of 0 (zero), 1 or 2 and R.sup.3 is a phenyl, naphthyl, pyridyl or thiazolinyl group or such group substituted with at least one lower alkyl and/or halogen substituent. The topic novel polyprenyl compounds can be synthesized from derivatives of the polyprenol which is obtainable from leaves of Ginkgo biloba or Cedrus deodara, among others, by extraction, if necessary followed by hydrolytic treatment. The novel polyprenyl compounds can be converted to mammalian dolichols or precursors thereof by reductive elimination of the --S(O).sub.m R.sup.3 group.
摘要翻译：新颖的聚异戊二烯化合物具有以下通式：其中n为11〜19的整数，Z 1为-CH 2 OH的整数，或其功能性前体，R 1和R 2中的任一个是氢原子，另一个是-S（O）m R 3，其中m是0（0），1或2的整数，并且R 3是苯基，萘基，吡啶基或噻唑啉基或该基团被至少一个低级烷基和/或卤素取代基取代。主题新颖的聚异戊二烯基化合物可以由聚乙二醇的衍生物合成，其可以通过提取，如果需要然后进行水解处理，可以从银杏叶或塞德斯酵母的叶获得。新的聚异戊烯基化合物可以通过-S（O）m R 3基团的还原性消除而转化为哺乳动物多烯醇或其前体。

5. 发明授权

US4703061A Gamma-aminobutyric acid derivatives, process for production thereof, and use thereof as medicaments 失效
标题翻译： γ-氨基丁酸衍生物，其制备方法及其作为药物的用途
公开(公告)号：US4703061A
公开(公告)日：1987-10-27
申请号：US753613
申请日：1985-07-09
申请人： Tsutomu Kameyama , Jiro Kitamura , Tetsuo Takigawa , Masao Mizuno
发明人： Tsutomu Kameyama , Jiro Kitamura , Tetsuo Takigawa , Masao Mizuno
IPC分类号： A61K31/195 , A61P25/28 , C07C67/00 , C07C231/00 , C07C231/10 , C07C231/12 , C07C231/14 , C07C235/12 , C07C103/48 , A61K31/22
CPC分类号： C07C235/12
摘要： A compound which is 4-(3,5-dihydroxy-3-methylpentylamide)butyric acid or its pharmaceutically acceptable salt or ester; this compound being produced by reacting a salt or an ester of gamma-aminobutyric acid with beta-hydroxy-beta-methyl-delta-valerolactone, and as required, converting the resulting compound in the form of a salt or ester to a free acid, or as required, converting the resulting compound in the form of a free acid to its pharmaceutically acceptable salt or ester; and useful as a medicament for preventing or treating an impediment in cerebral function.
摘要翻译： 4-（3,5-二羟基-3-甲基戊酰胺）丁酸或其药学上可接受的盐或酯的化合物; 该化合物通过γ-氨基丁酸的盐或酯与β-羟基-β-甲基-δ-戊内酯反应而产生，并根据需要将所得到的化合物以盐或酯的形式转化为游离酸，或根据需要，将所得化合物以游离酸的形式转化为其药学上可接受的盐或酯; 并且可用作预防或治疗脑功能障碍的药物。

6. 发明授权

US5258371A Method to reduce connective tissue destruction 失效
标题翻译：减少结缔组织破坏的方法
公开(公告)号：US5258371A
公开(公告)日：1993-11-02
申请号：US891554
申请日：1992-05-29
申请人： Lorne M. Golub , Nangavarum S. Ramamurthy , Thomas F. McNamara , Robert A. Greenwald , Tsutomu Kawai , Takashi Hamasaki , Michiya Shimamura , Goro Kobayashi , Tetsuo Takigawa , Hisashi Iwata
发明人： Lorne M. Golub , Nangavarum S. Ramamurthy , Thomas F. McNamara , Robert A. Greenwald , Tsutomu Kawai , Takashi Hamasaki , Michiya Shimamura , Goro Kobayashi , Tetsuo Takigawa , Hisashi Iwata
IPC分类号： A61K31/65 , A61P19/02 , A61P29/00 , A61P43/00 , C07C235/40 , C07C237/26
CPC分类号： A61K31/65 , Y10S514/825
摘要： Provided is a method of treating humans or animals suffering from a condition or disease characterized by excessive collagen destruction, which comprises administering to said human or animal an effective amount of a 12a-deoxytetracycline represented by the following general formula ##STR1## The method is effective in the treatment of various articular diseases characterized by excessive collagen destruction.
摘要翻译：本发明提供一种治疗患有特征在于过度胶原破坏的病症或疾病的人或动物的方法，其包括向所述人或动物施用有效量的由以下通式表示的12a-脱氧四环素：该方法是有效的用于治疗以胶原蛋白破坏过多为特征的各种关节疾病。

7. 发明授权

US5360914A Long chain carboxylic acid maleimides 失效
标题翻译：长链羧酸马来酰亚胺
公开(公告)号：US5360914A
公开(公告)日：1994-11-01
申请号：US59759
申请日：1993-05-11
申请人： Masayasu Inoue , Iwao Ebashi , Tetsuo Takigawa
发明人： Masayasu Inoue , Iwao Ebashi , Tetsuo Takigawa
IPC分类号： A61K38/44 , C12N9/02 , A61K37/50 , C07D207/452 , C07K15/12
CPC分类号： C12N9/0089
摘要： Provided are novel superoxide dismutase derivatives represented by the following general formula (I) ##STR1## wherein [SOD] is a superoxide dismutase residue derived by removal of two mercapto groups, and W is a divalent long chain hydrocarbon residue which may optionally be interrupted by one or more groups each independently selected from the group consisting of an oxygen atom, a sulfur atom and a group of -N(R)- (R being a lower alkyl group). The SOD derivatives retain most of the enzymatic activities of unmodified SOD and have much longer plasma half-life than unmodified SOD. They are effective for treating various diseases caused by active oxygen species.Also provided are chemical modifiers to prepare the above SOD derivatives.
摘要翻译：提供了由以下通式（I）表示的新型超氧化物歧化酶衍生物，其通过除去两个巯基衍生得到的酪蛋白酶残基，W是二价长链烃残基，其可以任选地被一个或多个各自独立地选自由氧原子，硫原子和-N（R） - （R为低级烷基）的基团组成。 SOD衍生物保留大部分未修饰的SOD的酶活性，并且具有比未修饰的SOD更长的血浆半衰期。它们对于治疗由活性氧引起的各种疾病是有效的。还提供了制备上述SOD衍生物的化学改性剂。

8. 发明授权

US5238837A Superoxide dismutase derivatives 失效
标题翻译：超氧化物歧化酶衍生物
公开(公告)号：US5238837A
公开(公告)日：1993-08-24
申请号：US803414
申请日：1991-12-06
申请人： Masayasu Inoue , Iwao Ebashi , Tetsuo Takigawa
发明人： Masayasu Inoue , Iwao Ebashi , Tetsuo Takigawa
IPC分类号： A61K38/44 , C12N9/02
CPC分类号： C12N9/0089
摘要： Provided are novel superoxide dismutase derivatives represented by the following general formula (I) ##STR1## wherein [SOD] is a superoxide dismutase residue derived by removal of two mercapto groups, and W is a divalent long chain hydrocarbon residue which may optionally be interrupted by one or more groups each independently selected from the group consisting of an oxygen atom, a sulfur atom and a group of --N(R)-- (R being a lower alkyl group). The SOD derivatives retain most of the enzymatic activities of unmodified SOD and have much longer plasma half-life than unmodified SOD. They are effective for treating various diseases caused by active oxygen species.Also provided are chemical modifiers to prepare the above SOD derivatives.
摘要翻译：提供了由以下通式（I）表示的新型超氧化物歧化酶衍生物：其中[SOD]是通过除去两个巯基衍生的超氧化物歧化酶残基，W是可任意选择的二价长链烃残基被一个或多个各自独立地选自氧原子，硫原子和-N（R） - （R是低级烷基）的基团的基团中断）。 SOD衍生物保留大部分未修饰的SOD的酶活性，并且具有比未修饰的SOD更长的血浆半衰期。它们对于治疗由活性氧引起的各种疾病是有效的。还提供了制备上述SOD衍生物的化学改性剂。

9. 发明授权

US5336782A Long chain carboxylic acid imide ester 失效
标题翻译：长链羧酸酰亚胺酯
公开(公告)号：US5336782A
公开(公告)日：1994-08-09
申请号：US872534
申请日：1992-04-23
申请人： Iwao Ebashi , Tetsuo Takigawa , Masayasu Inoue
发明人： Iwao Ebashi , Tetsuo Takigawa , Masayasu Inoue
IPC分类号： C07D207/46 , C07D209/48 , C07D209/76 , C07D211/94 , C07K1/00 , C07K14/00 , C07K16/00 , C07K17/00
CPC分类号： C07D209/48 , C07D207/46 , C07D209/76 , C07D211/94
摘要： Provided is a long chain carboxylic acid imide ester (I) represented by the following general formula (I) ##STR1## wherein W is a divalent long chain hydrocarbon group which may optionally be interrupted by one or more groups each independently selected from the group consisting of an oxygen atom, a sulfur atom and a group of --N(R.sup.1)-- (R.sup.1 being a lower alkyl group) and X represents a divalent hydrocarbon group which may optionally be substituted, or salts thereof. The above long chain carboxylic acid imide ester or its salts is useful for modifying enzymes or proteins having biological activities to give their derivatives which have, while retaining most of the original biological activities, an extremely prolonged plasma half-life as compared with the proteins and have no antigenecities and can be administered to animals.
摘要翻译：提供由以下通式（I）表示的长链羧酸酰亚胺酯（I）：其中W是二价长链烃基，其可任选地被一个或多个各自独立地选自由氧原子，硫原子和-N（R1） - （R1为低级烷基）组成的基团，X表示任选被取代的二价烃基或其盐。上述长链羧酸酰亚胺酯或其盐可用于修饰具有生物活性的酶或蛋白质以产生其衍生物，其与原始蛋白质相比具有极大延长的血浆半衰期，同时保留大部分原始生物活性，没有抗原性，可以给予动物。

10. 发明授权

US5112998A Pregnane derivatives and processes for production thereof 失效
标题翻译： PREGNANE衍生物及其生产方法
公开(公告)号：US5112998A
公开(公告)日：1992-05-12
申请号：US545120
申请日：1990-06-15
申请人： Jiro Tsuji , Takashi Takahashi , Masao Tsuji , Naoshi Nakagawa , Tetsuo Takigawa
发明人： Jiro Tsuji , Takashi Takahashi , Masao Tsuji , Naoshi Nakagawa , Tetsuo Takigawa
IPC分类号： C07J9/00 , C07J17/00 , C07J41/00 , C07J51/00 , C07J71/00
CPC分类号： C07J41/0055 , C07J17/00 , C07J51/00 , C07J71/001 , C07J9/00
摘要： There are provided pregnane derivatives represented by formula ##STR1## wherein A.sup.1 represents a hydrogen atom or a hydroxyl group, A.sup.2 represents a substituent such as a hydroxyl group when A.sup.1 represents a hydrogen atom, or A.sup.2 represents a hydrogen atom when A.sup.1 represents a hydroxyl group, or A.sup.1 and A.sup.2 are combined together to form an oxo group; D.sup.1 represents a substitutent such as a hydroxyl group, and D.sup.2 represents a hydrogen atom, or D.sup.1 and D.sup.2 are combined together to form an epoxy group or a single bond; D.sup.3, D.sup.5 and D.sup.7 each represents a hydrogen atom, D.sup.4 represents a hydroxyl group, and D.sup.6 represents a substitutent such as a hydroxyl group, or D.sup.3 and D.sup.4 may be combined together to form an epoxy group or a single bond, or D.sup.4 and D.sup.5 may be combined together to form a single bond, or D.sup.5 and D.sup.6 may be combined together to form an epoxy group or a single bond, or D.sup.6 and D.sup.7 may be combined together to form a singel bond; and X.sup.1 and X.sup.2 each represents a lower alkoxyl group or, when combined together, they represent a lower alkylenedioxy or oxo group, and a process for their preparation.The pregnane derivatives are useful as intermediates for synthesizing vitamin D.sub.3 derivatives having a hydroxyl group in the 1.alpha.-position.
摘要翻译： PCT No.PCT / JP88 / 00313 Sec。 371日期1987年11月30日 102（e）1987年11月30日日期PCT提交1988年3月29日PCT公布。出版物WO88 / 07545 提供了由式表示的孕烷衍生物，其中A1表示氢原子或羟基，当A1表示氢原子时，A2表示取代基如羟基，或A2表示氢当A1表示羟基时，或A1和A2组合在一起形成氧代基; D1表示取代基，例如羟基，D2表示氢原子，或D1和D2组合在一起形成环氧基或单键; D3，D5和D7各自表示氢原子，D4表示羟基，D6表示取代基如羟基，或D3和D4可以组合在一起形成环氧基或单键，或D4和D5 可以组合在一起形成单键，或者D5和D6可以组合在一起以形成环氧基或单键，或者D6和D7可以组合在一起形成单键; 并且X 1和X 2各自表示低级烷氧基，或者当它们组合在一起时，它们代表低级亚烷基二氧基或氧代基团，及其制备方法。孕烷衍生物可用作合成在1α位具有羟基的维生素D3衍生物的中间体。

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