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1. 发明授权

US5103007A Lipids 失效
标题翻译： LIPIDS
公开(公告)号：US5103007A
公开(公告)日：1992-04-07
申请号：US427339
申请日：1989-10-27
申请人： Hiroaki Nomura , Hiroshi Akimoto , Keizo Inoue
发明人： Hiroaki Nomura , Hiroshi Akimoto , Keizo Inoue
IPC分类号： C07C317/18 , C07C321/12 , C07D213/48 , C07D213/55 , C07D239/34 , C07D401/12 , C07D403/12 , C07D417/12 , C07D521/00
CPC分类号： C07D249/08 , C07C317/18 , C07C321/12 , C07D213/48 , C07D213/55 , C07D231/12 , C07D233/56 , C07D239/34 , C07D401/12 , C07D403/12 , C07D417/12
摘要： Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.

2. 发明授权

US5081245A Carboxylic acid derivatives 失效
标题翻译：羧酸衍生物
公开(公告)号：US5081245A
公开(公告)日：1992-01-14
申请号：US395524
申请日：1989-08-18
申请人： Hiroaki Nomura , Hiroshi Akimoto , Eiko Imamiya , Keizo Inoue
发明人： Hiroaki Nomura , Hiroshi Akimoto , Eiko Imamiya , Keizo Inoue
IPC分类号： C07C43/13 , C07C43/178 , C07C45/29 , C07C45/67 , C07C49/175 , C07C49/255 , C07C217/08 , C07C229/10 , C07C309/66 , C07D213/30 , C07D239/34 , C07D401/12 , C07D521/00
CPC分类号： C07D213/30 , C07C217/08 , C07C229/10 , C07C309/66 , C07C43/135 , C07C43/1785 , C07C45/29 , C07C45/673 , C07C49/175 , C07C49/255 , C07D231/12 , C07D233/56 , C07D239/34 , C07D249/08 , C07D401/12
摘要： A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p -- wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q -- wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q -- wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.r -- (wherein r represents 0, 1 or 2), and p and q are the same as defined above; Y represents a divalent group containing tertiary or quaternary nitrogen atom(s); and Z represents an alkylene group which may be substituted and/or interrupted, or a group represented by the formula:--Q--T-- or --T--W-- wherein Q and W represent an alkylene group which may be substituted, and T represents a phenhylene group, a naphthylene group, a cycloalkylene group; and a salt thereof exhibit excellent antitumor action including differentiation inducing action and are useful as pharmaceuticals.

3. 发明授权

US5008454A Propanediol derivatives, their production and use 失效
标题翻译：丙二醇衍生物，其生产和使用
公开(公告)号：US5008454A
公开(公告)日：1991-04-16
申请号：US492330
申请日：1990-03-12
申请人： Keizo Inoue , Hiroaki Nomura , Akihiro Tasaka
发明人： Keizo Inoue , Hiroaki Nomura , Akihiro Tasaka
IPC分类号： C07D213/20 , C07D213/80 , C07D277/22
CPC分类号： C07D213/20 , C07D213/80 , C07D277/22
摘要： Novel compounds having the formula:R.sup.1 --OCH.sub.2 CH.sub.2 CH.sub.2 O--(CH.sub.2).sub.n --R.sup.2wherein R.sup.1 stands for a higher alkyl group; R.sup.2 stands for a primary to tertiary amino group or a quaternary ammonium group; and n denotes an integer of 3 to 10; and salts thereof, have excellent anti-tumor action and therefore are useful as anti-tumor agents.

4. 发明授权

US4845219A Nitrogen- and sulfur-containing lipid compounds their production and use 失效
标题翻译：含氮和含硫脂质化合物的生产和使用
公开(公告)号：US4845219A
公开(公告)日：1989-07-04
申请号：US76887
申请日：1987-07-23
申请人： Keizo Inoue , Hiroaki Nomura , Tetsuya Aono
发明人： Keizo Inoue , Hiroaki Nomura , Tetsuya Aono
IPC分类号： C07D213/20 , C07D277/22
CPC分类号： C07D213/20 , C07D277/22
摘要： A compound of the general formula [I]: ##STR1## wherein R.sub.1 represents a higher alkyl group or an N-(higher alkyl)carbamoyl group, R.sub.2 represents a lower alkyl group, an acyl group having at least three carbon atoms, an N-(lower alkyl)carbamoyl group, an N-(lower alkyl)thiocarbamoyl group or a benzyl group, R represents a primary, secondary or tertiary amino group or a quaternary ammonium group, x is 1 or 2, y is a number of 0, 1 or 2, and z is an integer of 2-10, or a pharmaceutically acceptable salt thereof. The novel substances have both anti-tumor activity and platelet activating factor-inhibiting property, and they are effective as an anti-tumor agent without circulatory trouble.
摘要翻译：通式[I]的化合物：其中R 1表示高级烷基或N-（高级烷基）氨基甲酰基，R 2表示低级烷基，具有至少3个碳原子的酰基，N-（低级烷基）氨基甲酰基，N-（低级烷基）硫代氨基甲酰基或苄基，R表示伯，仲或叔氨基或季铵基，x为1或2，y为数为0,1或2，z为2-10的整数，或其药学上可接受的盐。新型物质具有抗肿瘤活性和血小板激活因子抑制特性，作为无循环障碍的抗肿瘤药物有效。

5. 发明授权

US4920134A 2-O-pyrimidinyl glycerol derivatives 失效
标题翻译： 2-O-嘧啶基甘油衍生物
公开(公告)号：US4920134A
公开(公告)日：1990-04-24
申请号：US227550
申请日：1988-08-03
申请人： Keizo Inoue , Hiroaki Nomura , Eiko Imamiya
发明人： Keizo Inoue , Hiroaki Nomura , Eiko Imamiya
IPC分类号： C07D237/14 , C07D239/34 , C07D401/12 , C07D403/12 , C07D417/12
CPC分类号： C07D403/12 , C07D237/14 , C07D239/34 , C07D401/12 , C07D417/12
摘要： Novel compounds having the formula: ##STR1## wherein ##STR2## represents a nitrogen-containing aromatic 6-membered ring; R.sup.1 represents a higher alkyl group which may be substituted; R.sup.2 represents a tertiary amino group or a quaternary ammonium group; and m represents 2 or 3; and salts thereof have superior antitumor activities including differentiation-inducing activity, and are useful as antitumor agents.

6. 发明授权

US4889953A Glycerol derivatives, their production and use 失效
标题翻译：甘油衍生物，其生产和使用
公开(公告)号：US4889953A
公开(公告)日：1989-12-26
申请号：US76527
申请日：1987-07-22
申请人： Keizo Inoue , Hiroaki Nomura , Tetsuya Okutani
发明人： Keizo Inoue , Hiroaki Nomura , Tetsuya Okutani
IPC分类号： A61K31/08 , A61K31/13 , A61K31/14 , A61K31/22 , A61K31/44 , A61K31/4425 , A61P7/02 , A61P35/00 , C07C67/00 , C07C213/00 , C07C217/08 , C07C325/00 , C07C333/04 , C07D213/20 , C07D213/30 , C07D295/088
CPC分类号： C07D213/20 , C07D295/088
摘要： Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.
摘要翻译：下式的化合物：其中R 1是可被取代的高级烷基; R2是氢，可以被取代的低级烷基，可被取代的低级烷酰基或低级烷硫基氨基甲酰基; R3是伯至叔氨基或季铵基团; n为2或3，其盐具有抗肿瘤活性和血小板活化因子抑制活性。

7. 发明授权

US4675430A 2-alkanoyloxy-3-(N-octadecylcarbamoyloxy)propyl 2-trimethylaminoethyl phosphate 失效
标题翻译： 2-烷酰氧基-3-（N-十八烷基氨基甲酰氧基）丙基2-三甲基氨基乙基磷酸酯
公开(公告)号：US4675430A
公开(公告)日：1987-06-23
申请号：US875701
申请日：1986-06-18
申请人： Keizo Inoue , Hiroaki Nomura , Tetsuya Okutani
发明人： Keizo Inoue , Hiroaki Nomura , Tetsuya Okutani
IPC分类号： A61K31/685 , A61P35/00 , C07F9/10 , C07F9/09
CPC分类号： C07F9/10
摘要： 2-Alkanoyloxy-3-(N-octadecylcarbamoyloxy)propyl trimethylammonioethyl phosphates and a salt thereof exhibit inhibitory activity against multiplication of tumor cells, and are useful as an antitumor agent.
摘要翻译： 2-烷酰氧基-3-（N-十八烷基氨基甲酰氧基）丙基三甲基铵乙基磷酸酯及其盐对肿瘤细胞增殖具有抑制活性，可用作抗肿瘤剂。

8. 发明授权

US4650868A 7-deazapurine derivatives useful as antitumor agents 失效
标题翻译：可用作抗肿瘤剂的7-脱氮嘌呤衍生物
公开(公告)号：US4650868A
公开(公告)日：1987-03-17
申请号：US729202
申请日：1985-05-01
申请人： Susumu Nishimura , Hiroaki Nomura , Hiroshi Akimoto
发明人： Susumu Nishimura , Hiroaki Nomura , Hiroshi Akimoto
IPC分类号： A61K31/505 , A61P35/00 , C07D487/04 , C07F7/10 , C07F7/18 , C07D471/02
CPC分类号： C07D487/04 , Y02P20/55
摘要： 7-Deazapurine derivatives of the formula: ##STR1## wherein R.sup.1 is phenyl which has, at the ortho position and/or para position as substituents, at least one group represented by the formula --O--R.sup.3, --S--R.sup.4 or ##STR2## (wherein R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and each is hydrogen or an alkyl or phenyl group which may be substituted, whereby R.sup.5 and R.sup.6, together with the adjacent nitrogen atom, may form a cyclic amino group which may be substituted, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each may represent a protective group), and may have a group or groups with a molecular weight of up to about 200 as a substituent at any position other than those having the said substituents introduced; R.sup.2 is an amino group which may be protected, or its salt, have a potent antitumor activity, and hence the compounds are useful as an antitumor agent.
摘要翻译：其中R 1是在取代基的邻位和/或对位具有至少一个由式-O-R 3，-S-R 4或（其中R 3，R 4，R 5和R 6相同或不同，各自为氢或可被取代的烷基或苯基，其中R 5和R 6与相邻的氮原子一起可形成环状氨基，并且R 3，R 4，R 5和R 6各自可以表示保护基），并且可以具有除了引入了所述取代基的那些以外的任何位置具有至多约200的分子量的基团作为取代基的基团; R2是可被保护的氨基或其盐具有有效的抗肿瘤活性，因此该化合物可用作抗肿瘤剂。

9. 发明授权

US4132789A 7-[2-(2-Imino-4-thiazolin-4-yl)-2-sulfoacetamido]cephalosporins and antibacterial compositions containing them 失效
标题翻译： 7- {8-（2-亚氨基-4-噻唑烷-4-基）-2-硫代乙酰胺基{9头孢菌素和含有它们的抗菌组合物
公开(公告)号：US4132789A
公开(公告)日：1979-01-02
申请号：US715495
申请日：1976-08-18
申请人： Hiroaki Nomura , Takenori Hitaka , Hiroshi Akimoto , Isao Minami , Fumio Kiriki , Tatsuichi Matsuda , Takeshi Fugono
发明人： Hiroaki Nomura , Takenori Hitaka , Hiroshi Akimoto , Isao Minami , Fumio Kiriki , Tatsuichi Matsuda , Takeshi Fugono
IPC分类号： C07D501/20 , A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46
CPC分类号： C07D277/20 , C07D501/24
摘要： Novel cephalosporins shown by the general formula: ##STR1## wherein Y is an acyloxy group, a quaternary ammonium group or a group of the formula: --S--R in which R is a nitrogen-containing heterocyclic group, and pharmaceutically acceptable salts thereof have high antibacterial properties against Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa and Serratia marcescens.
摘要翻译：新型头孢菌素，其通式如下：其中Y为酰氧基，季铵基团或其中R为含氮杂环基的-SR基团及其药学上可接受的盐具有高抗菌性对革兰氏阳性和革兰氏阴性菌（包括铜绿假单胞菌和粘质沙雷氏菌）的特性。

10. 发明授权

US5223620A Pyrido[2,3-d]pyrimidine compounds useful as intermediates 失效
标题翻译：吡啶并[2,3-d]嘧啶化合物可用作中间体
公开(公告)号：US5223620A
公开(公告)日：1993-06-29
申请号：US830884
申请日：1992-02-04
申请人： Hiroaki Nomura , Hiroshi Akimoto , Tetsuo Miwa
发明人： Hiroaki Nomura , Hiroshi Akimoto , Tetsuo Miwa
IPC分类号： C07D239/95 , C07D471/04
CPC分类号： C07D471/04 , C07D239/95
摘要： New fused pyrimidines of the general formula (I): ##STR1## wherein the ring A is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen, fluorine or a lower alkyl group, and --COOR.sup.5 and --COOR.sup.6 are independently a carboxyl group which may be esterified, and salts thereof have excellent anti-tumor effects, and they can be produced by the following reaction scheme: ##STR2## in which A is, X, R.sup.1 to R.sup.4, --COOR.sup.5 have the above meanings.
摘要翻译：通式（I）的新的稠合嘧啶：其中环+ E，crc / A /是可被氢化的吡啶环或可被氢化的苯环，X是氨基或羟基，R1，R2，R3和R4独立地是氢，氟或低级烷基，-COOR5和-COOR6独立地是可被酯化的羧基，其盐具有优异的抗肿瘤效果，并且它们可以通过以下反应方案制备：其中+ E，crc / A / is，X，R 1至R 4，-COOR 5具有上述含义的 + TR 。

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