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1. 发明授权

US5733927A Salts of glucopyranose derivative and solutions of the same 失效
标题翻译：吡喃葡萄糖衍生物的盐及其溶液
公开(公告)号：US5733927A
公开(公告)日：1998-03-31
申请号：US465470
申请日：1995-06-05
申请人： Katsuhiro Imaki , Shinsuke Hashimoto , Hirohisa Wakatsuka
发明人： Katsuhiro Imaki , Shinsuke Hashimoto , Hirohisa Wakatsuka
IPC分类号： A61K31/715 , A61K9/08 , A61K31/00 , A61K31/70 , A61K31/7024 , A61P7/00 , A61P35/00 , A61P37/00 , A61P37/04 , C07H13/02 , C07H13/04 , C07H13/06 , C07H15/18 , A61K31/35 , C07D309/10
CPC分类号： C07H13/06 , C07H15/18 , Y02P20/55
摘要： A method for improving the solubility of a salt of a glucopyranose derivative of formula (I) ##STR1## wherein R.sup.2, R.sup.3 and Y.sup.+ are as defined herein. The compound of formula (I) possesses enhanced activity for cellular immunity, and therefore is useful as an enhancing agent for immunity. It also possesses inducing activity for TNF, IL-1, and IFN, and therefore is useful as an anti-tumor agent.
摘要翻译：一种改善式（I）的吡喃葡萄糖衍生物（I）的盐的溶解度的方法，其中R2，R3和Y +如本文所定义。式（I）化合物具有增强的细胞免疫活性，因此可用作免疫增强剂。它还具有TNF，IL-1和IFN的诱导活性，因此可用作抗肿瘤剂。

2. 发明授权

US5294723A Salts of glucopyranose derivatives and its intermediate 失效
标题翻译：吡喃葡萄糖衍生物及其中间体的盐
公开(公告)号：US5294723A
公开(公告)日：1994-03-15
申请号：US010163
申请日：1993-01-28
申请人： Katsuhiro Imaki , Shinsuke Hashimoto , Hirohisa Wakatsuka
发明人： Katsuhiro Imaki , Shinsuke Hashimoto , Hirohisa Wakatsuka
IPC分类号： A61K31/715 , A61K9/08 , A61K31/00 , A61K31/70 , A61K31/7024 , A61P7/00 , A61P35/00 , A61P37/00 , A61P37/04 , C07H13/02 , C07H13/04 , C07H13/06 , C07H15/18 , C07D309/10
CPC分类号： C07H13/06 , C07H15/18 , Y02P20/55
摘要： A salt of glucopyranose derivative of the formula (I) ##STR1## wherein R.sup.2 is ##STR2## R.sup.3 is ##STR3## Y.sup.+ is sodium ion or tris(hydroxymethyl)methylammonium ion; and a glucopyranose derivative of the formula (II) ##STR4## wherein all the symbols are the same meaning as hereinbefore defined, is an important intermediate for the preparation of compound of the formula (I).
摘要翻译：式（I）的吡喃葡萄糖衍生物（*化学结构*）（I）其中R2是（*化学结构*）R3是（*化学结构*）Y +是钠离子或三（羟甲基）甲基铵离子; 和式（II）的吡喃葡萄糖衍生物（*化学结构*）（II），其中所有符号与上述定义相同，是制备式（I）化合物的重要中间体。

3. 发明授权

US5359121A Glycine derivative monosodium salt tetrahydrate 失效
标题翻译：甘氨酸衍生物单钠盐四水合物
公开(公告)号：US5359121A
公开(公告)日：1994-10-25
申请号：US182366
申请日：1994-01-18
申请人： Katsuhiro Imaki , Hirohisa Wakatsuka
发明人： Katsuhiro Imaki , Hirohisa Wakatsuka
IPC分类号： C07C311/29 , C07C311/15
CPC分类号： C07C311/29
摘要： N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetrahydrate of the formula (I): ##STR1## is non-hygroscopic, homogeneous and stable compound, and has an inhibitory effect on elastase. Accordingly, the compound may be useful for the treatment and/or prevention of diseases induced by the abnormal enhancing of degradation of elastin, collagen fiber and/or proteoglican by the action of elastase, e.g., pulmonary emphysema, atherosclerosis, rheumatoid arthritis, etc.
摘要翻译：式（I）的N- [对 - （对 - 新戊酰氧基苯磺酰基氨基）苯甲酰基]甘氨酸四钠水合物：（I）是不吸湿，均相和稳定的化合物，对弹性蛋白酶具有抑制作用。因此，该化合物可用于治疗和/或预防由弹性蛋白酶（例如肺气肿，动脉粥样硬化，类风湿性关节炎等）的弹性蛋白，胶原纤维和/或蛋白多糖的异常增强引起的疾病的治疗和/或预防。

4. 发明授权

US4888351A 3-phenoxy (or phenylthia) cyclopentanecarbonylamino acid analogues 失效
标题翻译： 3-苯氧基（或苯基硫）环戊烷羰基氨基酸类似物
公开(公告)号：US4888351A
公开(公告)日：1989-12-19
申请号：US268623
申请日：1988-11-07
申请人： Katsuhiro Imaki , Tadao Okegawa , Yoshinobu Arai
发明人： Katsuhiro Imaki , Tadao Okegawa , Yoshinobu Arai
IPC分类号： A61K31/195 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61P7/10 , A61P25/00 , C07C67/00 , C07C235/40 , C07C313/00 , C07C323/61 , C07D307/46 , C07D307/80 , C07D333/22
CPC分类号： C07D333/22
摘要： This invention relates to compounds presented by the general formula: ##STR1## [wherein R.sup.1 and R.sup.2 are: (i) R.sup.1, R.sup.2 and carbon atoms to which R.sup.1 and R.sup.2 are linked, together represent the group of the general formula: ##STR2## (wherein R.sup.5 and R.sup.6 represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl or phenyl, independently, with the proviso that R.sup.5 and R.sup.6 is not hydrogen atoms at the same time), or(ii) R.sup.1 represents hydrogen and R.sup.2 represents the group of the formula: --COR.sup.7 (wherein R.sup.7 represents the group of the formula: ##STR3## (wherein Y represents a single-bond, alkylene, alkenylene, W represents oxygen or sulfur, m represents 1 to 3, R.sup.8 represents hydrogen, halogen, nitro, hydroxy, alkyl or alkoxy, with the proviso that when m represents two or more, plural R.sup.8 s may be different each, and R.sup.9 represents hydrogen, alkyl or phenyl group, with the proviso that two of R.sup.9 may be different each)), R.sup.3 represents hydrogen, halogen, alkyl group or two of R.sup.3 and phenyl to which two of R.sup.3 are linked, together represent naphthyl of the formula: ##STR4## (wherein R.sup.10 represents hydrogen, halogen or alkyl), with the proviso that when R.sup.1 represents hydrogen, the atom may be replaced by R.sup.3, and n represents 1 to 3, with the proviso that when n represents two or more, plural R.sup.3 s may be different each, X represents oxygen or sulfur and R.sup.4 represents amino acid-residue], or a non-toxic salt thereof, and methods for their preparation and treating agents for cerebral edema containing them as active ingredients.

5. 发明授权

US4640931A 3-(indian-5-yloxy (or thio)) cyclopentanecarboxylic acid analogues 失效
标题翻译： 3-（印indian -5-基氧基（或硫代））环戊烷羧酸类似物
公开(公告)号：US4640931A
公开(公告)日：1987-02-03
申请号：US792399
申请日：1985-10-29
申请人： Katsuhiro Imaki , Tadao Okegawa , Yoshinobu Arai
发明人： Katsuhiro Imaki , Tadao Okegawa , Yoshinobu Arai
IPC分类号： C07C62/08 , A61K31/19 , A61K31/215 , A61P7/10 , C07C51/00 , C07C51/09 , C07C62/26 , C07C62/38 , C07C67/00 , C07C69/757 , C07C313/00 , C07C323/61 , C07C149/40
CPC分类号： C07C323/00 , C07C309/00 , C07C327/00 , C07C62/26
摘要： The present invention relates to novel compounds of the general formula: ##STR1## wherein X represent an oxygen atom or a sulfur atom and R represents a hydrogen atom or an alkyl group of 1-4 carbon atoms, and non-toxic salts thereof when R represents a hydrogen atom, possessing an inhibitory effect on cerebral edema.
摘要翻译：本发明涉及以下通式的新化合物：其中X表示氧原子或硫原子，R表示氢原子或1-4个碳原子的烷基，和无毒盐当R表示氢原子时，具有对脑水肿的抑制作用。

6. 发明授权

US4473587A Prostaglandin E.sub.1 analogues 失效
标题翻译：前列腺素E1类似物
公开(公告)号：US4473587A
公开(公告)日：1984-09-25
申请号：US515909
申请日：1983-07-21
申请人： Takashi Muryobayashi , Katsuhiro Imaki , Yoshiki Sakai
发明人： Takashi Muryobayashi , Katsuhiro Imaki , Yoshiki Sakai
IPC分类号： A61K31/557 , A61K31/5575 , A61P1/16 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/937 , C08B37/00 , C07C177/00 , C07C49/653
CPC分类号： C07D307/937 , C07C405/0025 , C08B37/0015
摘要： Prostaglandin E.sub.1 analogues of the general formula: ##STR1## (wherein R.sup.1 represents a single bond or a straight- or branched-chain alkylene group of from 1 to 5 carbon atom(s), R.sup.2 represents a cycloalkyl group of from 4 to 7 carbon atoms either unsubstituted or substituted by at least one straight- or branched-chain alkyl group of from 1 to 8 carbon(s), and the double bond between C.sub.13 and C.sub.14 is trans) and cyclodextrin clathrate thereof, are useful in the prevention or treatment of cytodamage associated with digestive system disease, especially liver damage.
摘要翻译：前列腺素E1类似物，通式如下：＆lt; IMAGE＆gt;（其中R 1表示单键或1〜5个碳原子的直链或支链亚烷基，R 2表示4〜7个碳原子的环烷基原子是未取代的或被至少一个1至8个碳原子的直链或支链烷基取代，C13和C14之间的双键是反式）和环糊精包合物可用于预防或治疗与消化系统疾病相关的细胞损伤，特别是肝损伤。

7. 发明授权

US5221689A Prostaglandin analogues, processes for their preparation and pharmaceutical compositions containing them 失效
标题翻译：前列腺素类似物，其制备方法和含有它们的药物组合物
公开(公告)号：US5221689A
公开(公告)日：1993-06-22
申请号：US824543
申请日：1992-01-23
申请人： Katsuhiro Imaki , Hajimi Miyake , Tadao Okegawa
发明人： Katsuhiro Imaki , Hajimi Miyake , Tadao Okegawa
IPC分类号： C07C405/00 , C07D209/52 , C07D307/937 , C08B37/00
CPC分类号： C07D307/937 , C07C405/00 , C07C405/0083 , C07D209/52 , C08B37/0015
摘要： The present invention relates to novel isomers of 6,9.alpha.-nitrilo-PGI.sub.1 s having a specific steric configuration, which are replaced by an alkyl (C.sub.1 to C.sub.8)-substituted cycloalkyl (C.sub.4 to C.sub.7) group in (1S,S) form, in (1S,R) form or in cis form at the 15-, 16- or 17-position of the PG skeleton, and, alkyl esters thereof, non-toxic salts thereof, non-toxic acid addition salts thereof and cyclodextrin clathrates thereof, possessing more potent PG-like pharmacological activity than other isomers.
摘要翻译：本发明涉及具有特定立体构型的6,9个α-亚硝基-PGI1的新异构体，其被（1S，S）形式的（C1-C8） - 取代的环烷基（C4至C7）烷基取代，（1S，R）形式或顺式，在PG骨架的15-，16-或17-位，及其烷基酯，其无毒盐，其无毒酸加成盐和环糊精包合物，具有比其他异构体更强大的PG样药理活性。

8. 发明授权

US5017610A Derivatives of p-substituted phenyl ester of pivalic acid 失效
标题翻译：新戊酸对取代苯基酯的衍生物
公开(公告)号：US5017610A
公开(公告)日：1991-05-21
申请号：US364994
申请日：1989-06-12
申请人： Katsuhiro Imaki , Yoshinobu Arai , Tadao Okegawa
发明人： Katsuhiro Imaki , Yoshinobu Arai , Tadao Okegawa
IPC分类号： C07C235/56 , C07C235/64 , C07C311/29 , C07C323/59 , C07C323/63 , C07D207/16 , C07D209/20 , C07D211/62 , C07D211/96 , C07D213/42 , C07D213/75 , C07D213/76 , C07D295/26 , C07D319/20 , C07D521/00
CPC分类号： C07D213/42 , C07C235/56 , C07C235/64 , C07C311/29 , C07C323/59 , C07C323/63 , C07D207/16 , C07D209/20 , C07D211/62 , C07D211/96 , C07D213/75 , C07D213/76 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/26 , C07D319/20
摘要： A derivative of general formula: ##STR1## wherein Y is --SO.sub.2 -- or ##STR2## (i) R.sup.1 and R.sup.2, which may be the same or different, each represent, (1) --H, (2) C1-16 alkyl or (3) the formula: --X-- .circle.A --(R.sup.4).sub.n wherein X is a single-bond, --SO.sub.2 --, C1-4 alkylene, C1-4 alkylene substituted by ##STR3## -- .circle.A -- is carbocyclic or heterocyclic ring, n is 1.about.5, R.sup.4 is (1) --H or C1-8 alkyl, (2) C1-14 alkoxy, (3) C1-6 alkylthio, (4) --OH, halogen, --NO.sub.2 or trihalomethyl, (5) the formula: --NR.sup.41 R.sup.42 wherein R.sup.41 and R.sup.42 each represents halogen or C1-4 alkyl, (6) tetrazole, (7) --SO.sub.3 H or --CH.sub.2 OH, (8) the formula: --SO.sub.2 NR.sup.41 R.sup.42 (9) the formula: --Z.sup.41 --COOR.sup.43 wherein Z.sup.41 is single-bond, C1-4 alkylene or C2-4 alkenylene, R.sup.43 is --H, C1-4 alkyl or benzyl, (10) the formula: --CONR.sup.41 R.sup.42 (11) the formula: --COO--Z.sup.42 --COOR.sup.43 wherein Z.sup.42 is C1-4 alkylene, R.sup.43 is --H, C1-4 alkyl or benzyl, (12) the formula: --COO--Z.sup.42 --CONR.sup.41 R.sup.42 (13) the formula: --OCO--R.sup.45 wherein R.sup.45 is C1-8 alkyl or p-guanidinophenyl, (14) the formula: --CO--R.sup.46 wherein R.sup.46 is C1-4 alkyl, (15) the formula: --O--Z.sup.43 --COOR.sup.450 wherein Z.sup.43 is C1-6 alkylene, R.sup.450 represents a hydrogen, C1-8 alkyl or p-guanidinophenyl, (16) the formula: ##STR4## wherein ##STR5## is an amino acid residue, R.sup.47 is bond, C1-4 alkyl, R.sup.48 is --H or C1-4 alkyl, R.sup.49 is --OH, C1-4 alkoxy, --NH.sub.2, amino substituted by one or two C1-4 alkyl, carbamoylmethoxy or carbamoylmethoxy substituted by one or two C1-4 alkyl at N atom of carbamoyl, wherein ##STR6## is C3-6 heterocyclic ring, (ii) R.sup.1, R.sup.2 and N atom bonded to R.sup.1 and R.sup.2 together represents heterocyclic ring containing at least a N atom(s) and substituted by --COOH or unsubstituted heterocyclic ring containing at least a N atom(s), R.sup.3 is (1) --H, (2) --OH, (3) C1-6 alkyl, (4) halogen, (5) C1-4 alkoxy or (6) C2-5 acyloxy, m is 1-4.or non-toxic salt or an acid addition salt thereof possess inhibitory activity on elastase, and therefore is useful for treating and/or preventing agent for pulmonary emphysema, atherosclerosis and rheumatoid arthritis and the like.

9. 发明授权

US4464388A Use of prostaglandin analogues to treat cytodamage 失效
标题翻译：使用前列腺素类似物治疗细胞损伤
公开(公告)号：US4464388A
公开(公告)日：1984-08-07
申请号：US478031
申请日：1983-03-23
申请人： Yoshiki Sakai , Katsuhiro Imaki , Takashi Muryobayashi
发明人： Yoshiki Sakai , Katsuhiro Imaki , Takashi Muryobayashi
IPC分类号： A61K31/34 , A61K31/38 , A61K31/40 , A61K31/557 , A61K31/5575 , A61P1/16 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C08B37/00 , A61K31/215 , A61K31/19
CPC分类号： C08B37/0015 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/557
摘要： Prostaglandin analogue of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atom(s), R.sup.2 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 6 carbon atom(s), the symbols------X--Y--Z-- in formula VB represent one of the groups: ##STR2## wherein in formulae (ii) and (iv), the configuration on C.sub.6 is S- or R-configuration or a mixture thereof and in formulae (iii) and (v) the double bond between C.sub.5 and C.sub.6 is in E- or Z-configuration or a mixture thereof) and n represents an integer of from 3 to 5 non-toxic salts thereof when R.sup.1 represents a hydrogen atom and cyclodextrin clathrates thereof are useful in the prevention or treatment of cytodamage associated with many diseases, especially liver damage.
摘要翻译：具有下式的前列腺素类似物：其中R 1表示氢原子或含有1至12个碳原子的直链或支链烷基，R 2表示氢原子原子或含有1至6个碳原子的直链或支链烷基，式VB中的符号--- XYZ-表示下列组之一：（i）（ii）（iv）其中在式（ii）和（iv）中，C6上的构型是S-或R-构型或其混合物，在式（ⅲ）中，和（v）C 5和C 6之间的双键为E-或Z-构型或其混合物），当R 1表示氢原子时，n表示3至5个无毒盐的整数，并且其环糊精包合物为可用于预防或治疗与许多疾病相关的细胞损伤，特别是肝损伤。

10. 发明授权

US4975464A Treatment of diseases caused by abnormal action of elastase 失效
标题翻译：治疗由弹性蛋白酶异常作用引起的疾病
公开(公告)号：US4975464A
公开(公告)日：1990-12-04
申请号：US337812
申请日：1989-04-14
申请人： Katsuhiro Imaki , Yoshinobu Arai , Hiroyuki Ohno
发明人： Katsuhiro Imaki , Yoshinobu Arai , Hiroyuki Ohno
IPC分类号： A61K31/255 , C07C279/18 , C07C309/63 , C07C309/65 , C07C309/66 , C07C311/00 , C07C311/08 , C07C311/29 , C07C311/46 , C07C327/16 , C07C329/10 , C07D213/65 , C07D213/75 , C07D277/04 , C07D277/22 , C07D295/26 , C07D521/00 , A61K31/24
CPC分类号： C07D213/75 , C07C279/18 , C07C309/65 , C07C309/66 , C07C311/08 , C07C311/29 , C07C311/46 , C07C329/10 , C07D213/65 , C07D277/04 , C07D277/22 , C07D295/26
摘要： Compounds presented by the general formula: ##STR1## wherein Y is oxygen, R.sup.2 is H, alkyl, alkoxy, alkoxymethyl, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --CH.dbd.CH--COOR.sup.3, halogen, --CF.sub.3, --COR.sup.4, --OCOR.sup.4, --CH.sub.2 OCOR.sup.4, --SO.sub.2 R.sup.4, --OSO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --OCONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --COHN-- SO.sub.2 NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, --NO.sub.2, --OH, --CH.sub.2 OH, guanidino, benzyloxy, guanidinophenylthiomethyl, morpholinosulfonylphenoxymethyl, pyridyloxymethyl, or (1,1-dioxothiazol-3-yl)carbonyl, or when Y is sulfur, R.sup.2 is H, alkyl, alkoxy, halogen, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --NO.sub.2, or --SO.sub.2 NR.sup.5 R.sup.6, and n represents an integer of one to five, and when n represents more than two, each or R.sup.2 may be the same group or the different group and acid addition salts thereof have inhibitory effect on elastase, and, therefore, are useful for the treatment and/or prevention of diseases induced by abnormal enhancing of degradation of proteins such as elastin and the like, by the action of elastase in mammals, especially in human beings.
摘要翻译：由以下通式表示的化合物：其中Y是氧，R2是H，烷基，烷氧基，烷氧基甲基，-COOR3，-CH2COOR3，-CH = CH-COOR3，卤素，-CF3，-COR4， - OCOR4，-CH2OCOR4，-SO2R4，-OSO2R4，-CONR5R6，-OCONR5R6，-SO2NR5R6，-COHN-SO2NR5R6，-NHSO2R7，-NO2，-OH，-CH2OH，胍基，苄氧基，胍基苯硫基甲基，吗啉代磺酰基苯氧基甲基，吡啶氧基甲基或（1 ，1-二氧代噻唑-3-基）羰基，或当Y为硫时，R 2为H，烷基，烷氧基，卤素，-COOR 3，-CH 2 COOR 3，-NO 2或-SO 2 NR 5 R 6，n为1至5的整数，当n表示2以上时，各个或R2可以是相同的基团，也可以是不同的基团，其酸加成盐对弹性蛋白酶具有抑制作用，因此可用于治疗和/或预防由异常增强引起的疾病蛋白质如弹性蛋白等的降解，通过弹性蛋白酶在哺乳动物，特别是人类中的作用。

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