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1. 发明授权

US4605645A 5-fluoro-2'-deoxyuridine derivatives and a process for the preparation thereof 失效
标题翻译： 5-氟-2'-脱氧尿苷衍生物及其制备方法
公开(公告)号：US4605645A
公开(公告)日：1986-08-12
申请号：US448087
申请日：1982-12-09
申请人： Kenzo Watanabe , Yoshinori Kato , Masahiko Saito , Takeo Oba , Hisashi Fukushima , Takeshi Hara
发明人： Kenzo Watanabe , Yoshinori Kato , Masahiko Saito , Takeo Oba , Hisashi Fukushima , Takeshi Hara
IPC分类号： C07H19/10 , C07H15/12 , C07H17/00
CPC分类号： C07H19/10 , Y02P20/55
摘要： 5-fluoro-2'-deoxyuridine derivatives expressed by general formula (1) and their pharmacologically permissible salts ##STR1## wherein A indicates a saturated or unsaturated divalent aliphatic hydrocarbon group having 1 to 30 carbon atoms; the letter n indicates 0 or 1, and when n is 0, it indicates that Y is directly bound to an oxygen atom; Y represents a hydrogen atom, phenyl group, or substituted phenyl group; however, when Y is a hydrogen atom, n is 1; R indicates a hydrogen atom or alcohol-protecting group.These compounds have a very strong antitumor activity.
摘要翻译：由通式（1）表示的5-氟-2'-脱氧尿苷衍生物及其药理学允许的盐（1）其中A表示具有1至30个碳原子的饱和或不饱和的二价脂族烃基; 字母n表示0或1，当n为0时，表示Y与氧原子直接结合; Y表示氢原子，苯基或取代的苯基; 然而，当Y为氢原子时，n为1; R表示氢原子或醇保护基。这些化合物具有非常强的抗肿瘤活性。

2. 发明授权

US4421914A Thiazolo[3,2-a]pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof 失效
公开(公告)号：US4421914A
公开(公告)日：1983-12-20
申请号：US311329
申请日：1981-10-14
申请人： Noriaki Okamura , Takeshi Toru , Takeo Oba , Toshio Tanaka , Kiyoshi Bannai , Kenzo Watanabe , Seizi Kurozumi , Tatsuyuki Naruchi , Keiji Komoriya
发明人： Noriaki Okamura , Takeshi Toru , Takeo Oba , Toshio Tanaka , Kiyoshi Bannai , Kenzo Watanabe , Seizi Kurozumi , Tatsuyuki Naruchi , Keiji Komoriya
IPC分类号： C07D513/04 , C07D513/14 , A61K31/505
CPC分类号： C07D513/04
摘要： A compound selected from thiazolo[3,2-a]pyrimidines or their enolate derivatives represented by the following general formula ##STR1## wherein R.sup.1 and R.sup.2 are identical or different, and each represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 3 to 10 carbon atoms, a substituted or unsubstituted phenyl group, a substituted or unsubstituted cycloaliphatic group having 3 to 8 carbon atoms, a substituted or unsubstituted phenylalkyl group or a substituted or unsubstituted acyl group having 2 to 7 carbon atoms, provided that R.sup.1 and R.sup.2 are not simultaneously hydrogen atoms or substituted or unsubstituted acyl groups having 2 to 7 carbon atoms; and R.sup.1 and R.sup.2, when taken together, may form, with the nitrogen atom to which they are bonded, a 5- or 6-membered ring which may further contain one or more hetero atoms;and acid addition salts of these compounds.The thiazolo[3,2-a]pyrimidines may be prepared by a process comprising (a) reacting a malonic acid derivative of the following general formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined with regard to formula (I), and R.sup.4 and R.sup.5 are identical or different and each represents an alkyl group having 1 to 6 carbon atoms,with 2-aminothiazoline under heat, if desired in the presence of an inert organic solvent, to induce cyclocondensation, or (b) performing said condensation reaction in the presence of an alkali metal alkoxide, if desired in the presence of an inert organic solvent, and neutralizing the resulting enolate with an acid; and if desired, reacting the reaction product of (a) or (b) with an acid.The present invention provides also several processes for preparing enolate derivatives thereof.The thiazolo[3,2-a]pyrimidines, their enolate derivatives and acid addition compounds thereof are useful for regulating the immune function of a warm-blooded animal.

3. 发明授权

US4466980A Thiaprostaglandin E.sub.1 derivatives, process for production thereof, and pharmaceutical use thereof 失效
标题翻译： Thiaprostaglandin E1衍生物，其制备方法及其药物用途
公开(公告)号：US4466980A
公开(公告)日：1984-08-21
申请号：US316902
申请日：1981-10-30
申请人： Toshio Tanaka , Takeshi Toru , Takeo Oba , Noriaki Okamura , Kenzo Watanabe , Kiyoshi Bannai , Atsuo Hazato , Seizi Kurozumi , Fukuyoshi Kamimoto , Akira Ohtsu
发明人： Toshio Tanaka , Takeshi Toru , Takeo Oba , Noriaki Okamura , Kenzo Watanabe , Kiyoshi Bannai , Atsuo Hazato , Seizi Kurozumi , Fukuyoshi Kamimoto , Akira Ohtsu
IPC分类号： C07C405/00 , C07D309/12 , C07C177/00 , A61K31/557
CPC分类号： C07C405/0033 , C07D309/12
摘要： A novel compound selected from the group consisting of 7-(or 6- or 4-)thiaprostaglandin E.sub.1 derivatives of the formula (I). ##STR1## wherein A represents --CH.sub.2 -- or ##STR2## in which n is 0, 1 or 2, provided that only one A cut of three is ##STR3## R.sup.1 -R.sup.7 and G are as defined in the specification, the 15-epimers of said thiaprostaglandin E.sub.1 derivatives, the enatiomers of said thiaprostaglandin E.sub.1 derivatives or their 15-epimers, and mixtures of these compounds.A 7-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by reacting a 2-organo-2-cyclopentenone (II) with an organic copper-lithium compound (III) to effect conjugation reaction. A 6-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by subjecting an .alpha.,.beta.-unsaturated ketone (IV) and a thiol (V) to the Michael addition reaction. And, 4-thiaprostaglandin derivative and/or its optical isomer may also be prepared by the Michael addition reaction from a 2-allyl substituted cyclopentanone (VI) and a thiol (VIII).Some compounds ((I)-1) amongst the compounds of the formula (I) and/or their optical isomer are useful for controlling vascular actions such as angina pectoris, vasodilation etc.
摘要翻译：选自式（I）的7-（或6-或4-）赖氨酸前列腺素E1衍生物的新化合物。（I）其中A表示-CH 2 - 或，其中n为0,1或2，条件是三个只有一个A切割是R 1 -R 7，G如说明书中所定义，所述thiaprostaglandin E1衍生物的15-差向异构体，所述thiaprostaglandin E1衍生物或它们的15-差向异构体的对映体，以及这些化合物的混合物。 7-硫代前列腺素E1衍生物和/或其旋光异构体可以通过2-有机-2-环戊烯酮（II）与有机铜 - 锂化合物（III）反应来制备共轭反应。 6-硫代前列腺素E1衍生物和/或其旋光异构体可以通过使α，β-不饱和酮（IV）和硫醇（V）进行迈克尔加成反应来制备。并且，也可以通过从2-烯丙基取代的环戊酮（VI）和硫醇（VIII）的迈克尔加成反应制备4-硫代前列腺素衍生物和/或其旋光异构体。式（I）化合物和/或其旋光异构体中的一些化合物（（I）-1）可用于控制血管作用，例如心绞痛，血管舒张等。

4. 发明授权

US4383996A Derivative of thiazolo[3,2-a]pyrimidine and a process for the preparation thereof and a drug containing it 失效
标题翻译：噻唑并[3,2-a]嘧啶的衍生物及其制备方法和含有它的药物
公开(公告)号：US4383996A
公开(公告)日：1983-05-17
申请号：US339460
申请日：1981-12-28
申请人： Takeo Oba , Kiyoshi Bannai , Toshio Tanaka , Kenzo Watanabe , Tatsuyuki Naruchi , Keiji Komoriya , Seizi Kurozumi , Kenji Hoshina
发明人： Takeo Oba , Kiyoshi Bannai , Toshio Tanaka , Kenzo Watanabe , Tatsuyuki Naruchi , Keiji Komoriya , Seizi Kurozumi , Kenji Hoshina
IPC分类号： C07D513/04 , A61K31/505
CPC分类号： C07D513/04 , Y10S514/825 , Y10S514/885
摘要： A derivative of thiazolo [3,2-a] pyrimidine expressed by formula (I) ##STR1## (where R indicates a phenyl group or a benzyl group which has a halogen atom, a lower alkyl or lower alkyloxy group as a substituent group, an alicyclic group or an arylethyl group), and a process for the preparation of a compound of formula (I) comprising cyclizing a compound expressed by formula (II) by application of heat ##STR2## (where a definition of R is as same as that given in case of formula (I) and R' indicates a halogen atom or lower alkyloxy group). A drug which contains this compound as active ingredient is useful for curing autoimmune diseases such as rheumatoid arthritis, nephritis, etc.
摘要翻译： PCT No.PCT / JP80 / 00090 Sec。 371日期：1981年12月28日 102（e）日期1981年12月28日PCT提交1980年4月28日PCT公布。公开号WO81 / 03174 1981年11月12日，由式（I）表示的噻唑并[3,2-a]嘧啶衍生物（I）（其中R表示苯基或具有卤素原子的苄基，较低烷基或低级烷氧基作为取代基，脂环基或芳乙基），以及制备式（I）化合物的方法，其包括使式（II）表示的化合物通过加热（II）（其中R的定义与式（I）的情况相同，R'表示卤素原子或低级烷氧基）。含有该化合物作为活性成分的药物可用于治疗自身免疫性疾病如类风湿性关节炎，肾炎等。

5. 发明授权

US4138553A 3-Methylene cephalosporanic acid derivatives and process for preparation thereof 失效
标题翻译： 3-亚甲基头孢菌酸衍生物及其制备方法
公开(公告)号：US4138553A
公开(公告)日：1979-02-06
申请号：US841321
申请日：1977-10-11
申请人： Sachio Ishimoto , Hisao Yamaguchi , Yoshinori Kato , Takeo Oba , Kenji Ozawa , Yataro Ichikawa , Koji Nakagawa , Hideki Tsuruta
发明人： Sachio Ishimoto , Hisao Yamaguchi , Yoshinori Kato , Takeo Oba , Kenji Ozawa , Yataro Ichikawa , Koji Nakagawa , Hideki Tsuruta
IPC分类号： C07D499/00 , C07D501/10 , C07D501/02
CPC分类号： C07D499/00 , Y02P20/55
摘要： Novel substituted hydrazide derivatives of 7-(substituted)amino-3-methylene-cepham-4-carboxylic acids expressed by the formula ##STR1## wherein R.sub.1 represents alkyl containing at least 3 carbon atoms, cycloalkyl, or optionally substituted aryl, and one of R.sub.2 and R.sub.3 represents hydrogen with the other being hydrogen or the same as R.sub.1 ; or R.sub.1 and R.sub.2 form a heterocyclic ring optionally through a hetero atom together with the attached nitrogen and R.sub.3 represents hydrogen atom; and Z.sub.1 represents amino or protected amino; and acid addition salts thereof, which are useful as intermediates for synthesizing cephalosporin antibiotics. These compounds can be prepared in high yields from the corresponding substituted hydrazide derivatives of 6-substituted amino-1-oxide-2, 2-dimethyl-penam-3-carboxylic acids, which are readily available at low costs, by heating them in the presence of a thermal rearrangement promotor such as organic sulfonic acids and optionally in the further presence of a tertiary nitrogen-containing cyclic compound, followed if desired by splitting off the amino-protecting group and converting the product to acid addition salts.
摘要翻译：由式“IMAGE”表示的7-（取代的）氨基-3-亚甲基 - 头孢烯-4-羧酸的新型取代的酰肼衍生物，其中R 1表示含有至少3个碳原子的烷基，环烷基或任选取代的芳基， R2和R3代表氢，另一个是氢或与R1相同; 或R 1和R 2与所连接的氮一起任选地通过杂原子形成杂环，并且R 3表示氢原子; Z1表示氨基或被保护的氨基; 其酸加成盐，其可用作合成头孢菌素抗生素的中间体。这些化合物可以以相当于6-取代的氨基-1-氧化物-2,2-二甲基 - 对甲苯磺酸的取代的酰肼衍生物的高收率制备，它们以低成本容易获得，通过在存在热重排促进剂如有机磺酸，并且任选地在另外存在叔氮气环状化合物的情况下，如果需要的话，分解氨基保护基并将产物转化成酸加成盐。

6. 发明授权

US4472428A Halogenated prostacyclins pharmaceutical use thereof and hydroxy intermediates therefore 失效
标题翻译：因此，其卤化前列环素及其羟基中间体
公开(公告)号：US4472428A
公开(公告)日：1984-09-18
申请号：US327741
申请日：1981-12-04
申请人： Takeshi Toru , Kiyoshi Bannai , Takeo Oba , Toshio Tanaka , Noriaki Okamura , Kenzo Wantanabe , Seizi Kurozumi , Akira Ohtsu , Tatsuyuki Naruchi
发明人： Takeshi Toru , Kiyoshi Bannai , Takeo Oba , Toshio Tanaka , Noriaki Okamura , Kenzo Wantanabe , Seizi Kurozumi , Akira Ohtsu , Tatsuyuki Naruchi
IPC分类号： C07D307/937 , A61K31/557 , C07D307/935
CPC分类号： C07D307/937
摘要： Novel 5- or 7-monohalogenated or 5,7-dihalogenated .sup.6 -PGI.sub.1 and 5- or 7-monohalogenated or dihalogenated PGI.sub.2 (except 5-monofluorinated PGI.sub.2). The novel halogenated prostacyclins are useful for controlling vascular actions and also in organ transplantation, extra-corporeal circulation and the like. The present invention also provides processes for preparing the novel halogenated prostacyclins.
摘要翻译： 5-或7-单卤代或5,7-二卤代6-PGI1和5-或7-单卤代或二卤代PGI2（5-单氟化PGI2除外）。新型卤代前列环素可用于控制血管作用，还可用于器官移植，体外循环等。本发明还提供了制备新型卤代前列环素的方法。

7. 发明授权

US4918558A Magnetic tape cassette having reel locks controlled by an optical tape end detecting element 失效
标题翻译：具有由光带末端检测元件控制的卷轴锁的磁带盒
公开(公告)号：US4918558A
公开(公告)日：1990-04-17
申请号：US287155
申请日：1988-12-21
申请人： Tadao Igarashi , Takashi Ota , Takeo Oba
发明人： Tadao Igarashi , Takashi Ota , Takeo Oba
IPC分类号： G11B23/087
CPC分类号： G11B23/08714 , G11B23/08721
摘要： A magnetic tape cassette comprises a compact reel lock mechanism which includes a pair of reel lock arms engaging with outer peripheries of a pair of tape reels, a sliding member serving as a cover for a single opening through which an end of an optical tape end detecting element is inserted into the cassette casing, a cam member which provided on the sliding member for rotating the pair of reel lock arms, and a guide member guiding said sliding member. When the tape cassette is out of a recording and/or reproducing apparatus, the single opening is closed by the sliding member and the reel lock arms restrict rotation of reels. Conversely, when the tape cassette is inserted into the recording and/or reproducing apparatus, the sliding member is pushed up by the end of the optical detecting element and as a result the cam member moves upward along with said sliding member. The opening, therefore, becomes open, and simultaneously the cam member releases engagement between the reel lock arms and the peripheries of tape reels.
摘要翻译：一种磁带盒包括一个紧凑的卷轴锁定机构，该机构包括与一对磁带盘的外周啮合的一对卷轴锁定臂，用作单个开口的盖子的滑动部件，通过该滑动部件检测光带端部的一端元件插入盒壳体中，设置在用于使一对卷轴锁定臂旋转的滑动构件上的凸轮构件和引导所述滑动构件的引导构件。当磁带盒离开记录和/或再现装置时，单个开口由滑动构件封闭，并且卷轴锁定臂限制卷轴的旋转。相反，当磁带盒插入记录和/或重放装置时，滑动件被光学检测元件的一端向上推，结果凸轮件随着滑动件向上移动。因此，开口变得开放，同时凸轮构件释放卷轴锁定臂与磁带卷轴的周边之间的接合。

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