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1. 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。

2. 发明授权

US4160830A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US4160830A
公开(公告)日：1979-07-10
申请号：US842153
申请日：1977-10-14
申请人： Shiro Morimoto , Hiroaki Nomura , Takeshi Fugono , Isao Minami
发明人： Shiro Morimoto , Hiroaki Nomura , Takeshi Fugono , Isao Minami
IPC分类号： A61K31/54
CPC分类号： C07D501/38
摘要： A method of combating bacterial infections in humans involves the administration of an antibacterially effective amount of a compound of the formula: ##STR1## wherein R is phenyl or thienyl group, and R' is a group which constitutes together with the adjacent nitrogen atom a pyridinium group that is unsubstituted or substituted by carbamoyl, or a 4'-methyl-5'-(.beta.-hydroxyethyl)-thiazolium or a pharmaceutically acceptable salt thereof, to a patient. This method is effective particularly against Pseudomonas aeruginosa as well as against other Gram negative and positive microorganisms.
摘要翻译：一种抗人类细菌感染的方法包括施用抗菌有效量的下式化合物：其中R是苯基或噻吩基，R'是与相邻氮原子一起构成的一个吡啶鎓未取代或被氨基甲酰基取代的基团，或4'-甲基-5' - （β-羟乙基） - 噻唑鎓或其药学上可接受的盐。该方法特别针对铜绿假单胞菌以及其他革兰氏阴性和阳性微生物有效。

3. 发明授权

US4065619A 7-(.alpha.-Sulfoacylamido)cephalosporins 失效
标题翻译： 7 - （{60-磺酰基氨基）头孢菌素
公开(公告)号：US4065619A
公开(公告)日：1977-12-27
申请号：US719704
申请日：1976-09-02
申请人： Shiro Morimoto , Hiroaki Nomura , Takeshi Fugono , Isao Minami
发明人： Shiro Morimoto , Hiroaki Nomura , Takeshi Fugono , Isao Minami
IPC分类号： A61K31/545 , C07D501/38 , C07D501/44 , C07D501/46
CPC分类号： C07D501/38
摘要： Novel cephalosporins of the formula, ##STR1## wherein R is a hydrogen atom or an alkyl, aryl or thienyl group, and R' is a group which constitutes together with the adjacent nitrogen atom a 5- or 6-membered ring containing 1 or 2 nitrogen atoms, which are effective particularly against Pseudomonas aeruginosa as well as against other Gram negative and positive microorganisms, for example, N-[7-(.alpha.-sulfophenylacetamido)ceph-3-em-3-ylmethyl] pyridinium 4-carboxylate, N-[7-(.alpha.-sulfo-3'-thienylacetamido)ceph-3-em-3-ylmethyl] pyridinium-4-carboxylate, and their pharmaceutically acceptable salts thereof. Sodium salt of the former is prepared by, e.g. reacting sodium 7-(.alpha.-sulfophenylacetamido) cephalosporanate with pyridine in water.
摘要翻译：新颖的下式头孢菌素其中R是氢原子或烷基，芳基或噻吩基，R'是与相邻氮原子一起构成含有1或2的5-或6-元环的基团氮原子，其特别对绿脓假单胞菌以及其他革兰氏阴性和阳性微生物有效，例如N- [7-（α-磺基苯基乙酰氨基）头孢-3-烯-3-基甲基]吡啶鎓4-羧酸盐，N - [7-（α-磺基-3'-噻吩基乙酰胺基）头孢-3-烯-3-基甲基]吡啶鎓-4-羧酸盐及其药学上可接受的盐。前者的钠盐通过例如使7-（α-磺基苯基乙酰氨基）头孢菌素钠与吡啶在水中反应。

4. 发明授权

US4029656A 7-(.alpha.-SULFOACYLAMIDO) CEPHALOSPORANIC ACIDS 失效
标题翻译： 7 - （{60 -SULFOACYLAMIDO）CEPHALOSPORANIC酸
公开(公告)号：US4029656A
公开(公告)日：1977-06-14
申请号：US711565
申请日：1976-08-04
申请人： Toshihiro Ishiguro , Takeshi Fugono , Hiroaki Nomura
发明人： Toshihiro Ishiguro , Takeshi Fugono , Hiroaki Nomura
IPC分类号： C07D501/36 , C07D501/50 , C07D501/54
CPC分类号： C07D501/36 , C07D501/24 , C07D501/26
摘要： Novel cephalosporanic acid derivatives which are active against both Gram positive and Gram negative pathogenic bacteria, particularly Pseudomonas, and which have .alpha.-sulfoacylamino group at 7-position. A few examples of the compounds are 7-(.alpha.-sulfophenylacetamido)-cephalosporanic acid, 7-(.alpha.-sulfopropionamido)-cephalosporanic acid, 7-(.alpha.-sulfocapronamido)-cephalosporanic acid. They are prepared by condensing 7-aminocephalosporanic acid or salts thereof with .alpha.-sulfocarboxylic acid or functional derivatives thereof in the presence of a solvent at -2.degree. - 10.degree. C.
摘要翻译：新型头孢菌素酸衍生物，其对革兰氏阳性和革兰氏阴性致病菌特别是假单胞菌具有活性，并且在7-位具有α-磺酰氨基。化合物的一些实例是7-（α-磺基苯基乙酰胺基） - 头孢烷酸，7-（α-亚磺基丙酰氨基） - 头孢烷酸，7-（α-磺基己内酰胺基） - 头孢烷酸。它们通过将7-氨基头孢烷酸或其盐与α-磺基羧酸或其官能衍生物在溶剂存在下在-2°-10℃下进行缩合来制备。

5. 发明授权

US3988327A 7-(.alpha.-SULFOACYLAMIDO)CEPHALOSPORANIC ACIDS 失效
标题翻译： 7 - （{60 -SULFOACYLAMIDO）CEPHALOSPORANIC酸
公开(公告)号：US3988327A
公开(公告)日：1976-10-26
申请号：US547169
申请日：1975-02-05
申请人： Toshihiro Ishiguro , Takeshi Fugono , Hiroaki Nomura
发明人： Toshihiro Ishiguro , Takeshi Fugono , Hiroaki Nomura
IPC分类号： C07D501/26 , C07D501/28 , C07D501/32
CPC分类号： C07D501/36 , C07D501/24 , C07D501/26
摘要： Novel cephalosporanic acid derivatives which are active against both Gram positive and Gram negative pathogenic bacteria, particularly Pseudomonas, and which have an .alpha.-sulfoacylamino group at 7-position. A few examples of the compounds are 7-(.alpha.-sulfophenylacetamido)-cephalosporanic acid, 7-(.alpha.-sulfopropionamido)-cephalosporanic acid, 7-(.alpha.-sulfocapronamido)-cephalosporanic acid. They are prepared by condensing 7-aminocephalosporanic acid or salts thereof with .alpha.-sulfocarboxylic acid or functional derivatives thereof in the presence of a solvent at -2.degree. - 10.degree. C.
摘要翻译：新型的头孢菌素酸衍生物，其对革兰氏阳性和革兰氏阴性致病菌，特别是假单胞菌属均具有活性，在7-位具有α-磺酰氨基。化合物的一些实例是7-（α-磺基苯基乙酰胺基） - 头孢烷酸，7-（α-亚磺基丙酰氨基） - 头孢烷酸，7-（α-磺基己内酰胺基） - 头孢烷酸。它们通过将7-氨基头孢烷酸或其盐与α-磺基羧酸或其官能衍生物在溶剂存在下在-2°-10℃下进行缩合来制备。

6. 发明授权

US4249006A Method of producing 5-fluorouracil derivatives 失效
标题翻译：生产5-氟尿嘧啶衍生物的方法
公开(公告)号：US4249006A
公开(公告)日：1981-02-03
申请号：US744929
申请日：1976-11-24
申请人： Isao Minami , Yoshio Yoshioka , Hiroaki Nomura
发明人： Isao Minami , Yoshio Yoshioka , Hiroaki Nomura
IPC分类号： C07D405/14 , C07D405/04
CPC分类号： C07D405/14
摘要： A new and industrially useful method of producing 1(or 1,3-bis)-(tetrahydro-2-furyl)-5-fluorouracil or a mixture thereof by reacting 5-fluorouracil with 2,3-dihydrofuran at elevated temperature in a closed vessel. Depending upon reaction conditions, each of the above 5-fluorouracil derivatives or a mixture of them is produced.1,3-Bis-(tetrahydro-2-furyl)-5-fluorouracil thus formed can be converted to 1-(tetrahydro-2-furyl)-5-fluorouracil by solvolysis under non-acidic conditions.
摘要翻译：一种新的和工业上有用的方法，通过在高温下将5-氟尿嘧啶与2,3-二氢呋喃在封闭的环境中反应生产1（或1,3-双） - （四氢-2-呋喃基）-5-氟尿嘧啶或其混合物船只。根据反应条件，制备上述5-氟尿嘧啶衍生物或它们的混合物。如此形成的1,3-双 - （四氢-2-呋喃基）-5-氟尿嘧啶可以在非酸性条件下通过溶剂分解转化成1-（四氢-2-呋喃基）-5-氟尿嘧啶。

7. 发明授权

US4110537A Method of producing N.sup.1 -(2-tetrahydrofuryl)-5-fluorouracil 失效
标题翻译：生产N“1” - （2-四氢呋喃）-5-氟尿嘧啶的方法
公开(公告)号：US4110537A
公开(公告)日：1978-08-29
申请号：US751541
申请日：1976-12-16
申请人： Isao Minami , Yoshio Yoshioka , Hiroaki Nomura
发明人： Isao Minami , Yoshio Yoshioka , Hiroaki Nomura
IPC分类号： C07D405/04 , A61K31/505 , C07C20060101 , C07D20060101 , C07D239/22 , C07D239/54 , C07D307/04 , C07D307/22 , C07D407/04
摘要： N.sup.1 -(2-tetrahydrofuryl)-5-fluorouracil is produced in high yield by reacting 5-fluorouracil with 2,3-dihydrofuran in the presence of trimethylsilyl chloride and a tertiary amine and treating the resultant mixture with an aqueous alkaline solution.

8. 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.

9. 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。

10. 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.

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