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1. 发明授权

US4064351A 9-OXO-15 .xi.-HYDROXY-20-ALKYLIDENEPROST-13(TRANS)-ENOIC ACID DERIVATIVES 失效
标题翻译： 9-OXO-15 {86-羟基-20-烷基硫代-13（反式） - 酸性衍生物
公开(公告)号：US4064351A
公开(公告)日：1977-12-20
申请号：US753277
申请日：1976-12-22
申请人： Kiyoshi Sakai , Koichi Kojima , Junya Ide , Shinsaku Kobayashi
发明人： Kiyoshi Sakai , Koichi Kojima , Junya Ide , Shinsaku Kobayashi
IPC分类号： C07C405/00 , C07F9/40 , C07C177/00
CPC分类号： C07C405/00 , C07F9/4015
摘要： Prostanoic acid derivatives having the formula ##STR1## wherein A represents ethylene group or cis-vinylene group, R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen atom or an alkyl group having 1-3 carbon atoms, R.sup.3 and R.sup.4 may be the same or different and each represents an alkyl group having 1-3 carbon atoms and R.sup.5 represents hydrogen atom or hydroxyl group and the pharmaceutically acceptable salts thereof and a process for the preparation thereof.The compounds are useful as anti-ulcerogenic or bronchodilating agents and may be prepared by oxidizing 9.xi.-hydroxy-15.xi.-protected-hydroxy-20-alkylideneprost-13(trans)-enoic acid derivatives.
摘要翻译：具有式“IMAGE”的前列腺酸衍生物，其中A表示亚乙基或顺式亚乙烯基，R 1和R 2可以相同或不同，各自表示氢原子或具有1-3个碳原子的烷基，R 3和R 4可以是相同或不同，各自表示具有1-3个碳原子的烷基，R 5表示氢原子或羟基及其药学上可接受的盐及其制备方法。

2. 发明授权

US3996263A 9-Oxo-11.alpha.-methyl-15.EPSILON.-hyroxyprost-13(trans)-enoic acid derivatives and process for the preparaion thereof 失效
标题翻译： 9-氧代-11 {60-甲基-15 {69-羟基霜霉素-13（反） - 烯酸衍生物及其制备方法
公开(公告)号：US3996263A
公开(公告)日：1976-12-07
申请号：US574376
申请日：1975-05-05
申请人： Kiyoshi Sakai , Takashi Yusa , Junya Ide , Mitsuo Yamazaki , Shinsaku Kobayashi
发明人： Kiyoshi Sakai , Takashi Yusa , Junya Ide , Mitsuo Yamazaki , Shinsaku Kobayashi
IPC分类号： C07C405/00 , C07D307/93 , C07D307/935 , C07D317/72 , C07C177/00
CPC分类号： C07D307/935 , C07C405/00 , C07D307/93 , C07D317/72
摘要： Prostanoic acid derivatives having the formula ##STR1## wherein A represents an alkylene group having from 4 to 8 carbon atoms, R.sup.1 represents an alkyl group having from one to 5 carbon atoms, R.sup.2 and R.sup.3 may be the same or different and each represents hydrogen atom or an alkyl group having from one to 4 carbon atoms and R.sup.4 represents hydrogen atom or an alkyl group having from one to 4 carbon atoms and the pharmaceutically acceptable salts thereof and also relates to a process for the preparation thereof.The compounds are useful as anti-ulcerogenic agents and may be prepared by reducing a compound having the formula ##STR2## wherein A, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same above and Z represents a carbonyl-protecting group to give a compound having the formula ##STR3## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Z are the same as above and removing the carbonyl-protecting group from the latter compound.
摘要翻译：具有式的前列生酸衍生物，其中A表示具有4至8个碳原子的亚烷基，R 1表示具有1至5个碳原子的烷基，R 2和R 3可以相同或不同，各自表示氢原子或具有1至4个碳原子的烷基和R 4表示氢原子或具有1至4个碳原子的烷基及其药学上可接受的盐，并且涉及其制备方法。

3. 发明授权

US4322435A Prostacyclin compounds 失效
标题翻译：前列环素化合物
公开(公告)号：US4322435A
公开(公告)日：1982-03-30
申请号：US153825
申请日：1980-05-27
申请人： Koichi Kojima , Kiyoshi Sakai , Shinsaku Kobayashi
发明人： Koichi Kojima , Kiyoshi Sakai , Shinsaku Kobayashi
IPC分类号： C07C69/732 , A61K31/19 , A61K31/20 , A61K31/215 , A61K31/23 , A61K31/557 , A61P7/02 , C07C29/147 , C07C47/198 , C07C49/633 , C07C49/743 , C07C51/00 , C07C51/353 , C07C59/46 , C07C62/38 , C07C67/00 , C07C69/73 , C07C69/757 , C07C405/00 , C07D309/12 , C07D317/72 , C07D407/12 , C07C177/00
CPC分类号： C07D317/72 , C07C29/147 , C07C309/00 , C07C405/00 , C07C405/0083 , C07C49/633 , C07C49/743 , C07C62/38 , C07D309/12 , C07C2101/16 , Y02P20/55
摘要： Prostacyclin derivatives of formula (I): ##STR1## (wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents an alkenyl group having from 8 to 12 carbon atoms; and n represents an integer of from 1 to 8, inclusive) and pharmaceutically acceptable salts thereof, are valuable pharmaceuticals, showing excellent thrombocyte agglutination inhibitory, coronary blood vessel dilatory and bronchodilatory effects, and may be prepared by introducing the .dbd.CH(CH.sub.2).sub.n COOR.sup.1 side chain onto an appropriate compound by means of a Wittig reaction.
摘要翻译：式（I）的前列环素衍生物：其中，R1表示氢原子或低级烷基，R2表示碳原子数为8〜12的烯基，n表示1〜8的整数，包括）和其药学上可接受的盐是有价值的药物，显示优异的凝血细胞凝集抑制，冠状动脉血管扩张和支气管扩张作用，并且可以通过将= CH（CH 2）n COOR 1侧链通过维蒂希反应。

4. 发明授权

US4757087A Carbacyclin derivatives 失效
标题翻译：卡巴环素衍生物
公开(公告)号：US4757087A
公开(公告)日：1988-07-12
申请号：US840920
申请日：1986-03-18
申请人： Koichi Kojima , Shinsaku Kobayashi
发明人： Koichi Kojima , Shinsaku Kobayashi
IPC分类号： A61K31/557 , A61P1/04 , C07C59/46 , C07C69/732 , C07C405/00 , C07H15/00 , C07C62/32 , A61K31/21
CPC分类号： C07C405/0083 , Y02P20/55
摘要： Carbacyclin derivatives with anti-ulcer activity comprise compounds of the general formula (I): ##STR1## (wherein R.sup.1 is selected from the group consisting of a hydrogen atom and an alkyl group having from 1 to 10 carbon atoms; R.sup.2 is selected from the group consisting of a hydrogen atom and a methyl group; and R.sup.3 is selected from the group consisting of a 3-butenyl group, a 4-pentenyl group and a 5-methyl-4-hexenyl group), and pharmaceutically acceptable salts thereof.
摘要翻译：具有抗溃疡活性的卡巴环素衍生物包括通式（I）的化合物：其中R 1选自氢原子和具有1至10个碳原子的烷基; R 2是选自氢原子和甲基; R3选自3-丁烯基，4-戊烯基和5-甲基-4-己烯基）和药学上可接受的盐其中。

5. 发明授权

US5489613A Carbacyclin derivatives, process for their preparation and compositions containing them 失效
标题翻译：卡巴环素衍生物，其制备方法和含有它们的组合物
公开(公告)号：US5489613A
公开(公告)日：1996-02-06
申请号：US824696
申请日：1992-01-21
申请人： Kazuo Koyama , Shigeo Amemiya , Koichi Kojima , Shinsaku Kobayashi
发明人： Kazuo Koyama , Shigeo Amemiya , Koichi Kojima , Shinsaku Kobayashi
IPC分类号： C07C405/00 , C07D317/72 , A61K31/557
CPC分类号： C07D317/72 , C07C405/0083 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## have valuable platelet-aggregation inhibitory activities and may be used for the prophylaxis and treatment of such diseases as thrombosis.
摘要翻译：式（I）化合物：（I）具有有价值的血小板聚集抑制活性，可用于预防和治疗诸如血栓形成之类的疾病。

6. 发明授权

US5405870A Carbacyclin compounds; pharmaceutical compositions and method of use 失效
标题翻译：卡巴环素化合物; 药物组合物和使用方法
公开(公告)号：US5405870A
公开(公告)日：1995-04-11
申请号：US147892
申请日：1993-11-04
申请人： Kazuo Koyama , Shigeo Amemiya , Koichi Kojima , Shinsaku Kobayashi
发明人： Kazuo Koyama , Shigeo Amemiya , Koichi Kojima , Shinsaku Kobayashi
IPC分类号： C07C405/00 , C07D317/72 , A61K31/557 , C07C69/732
CPC分类号： C07D317/72 , C07C405/0083 , Y02P20/55
摘要： Compounds of formula (Ic): ##STR1## having valuable platelet-aggregation inhibitory activities useful for the prophylaxis and treatment of such diseases as thrombosis and pharmaceutical compositions containing said compounds.
摘要翻译：式（Ic）化合物：具有有用的预防和治疗诸如血栓形成的疾病和含有所述化合物的药物组合物的有价值的血小板聚集抑制活性的图像（Ic）。

7. 发明授权

US4260551A Polyprenyl derivatives 失效
标题翻译：聚丙烯衍生物
公开(公告)号：US4260551A
公开(公告)日：1981-04-07
申请号：US11514
申请日：1979-02-12
申请人： Hiroshi Mishima , Akira Ogiso , Shinsaku Kobayashi
发明人： Hiroshi Mishima , Akira Ogiso , Shinsaku Kobayashi
IPC分类号： C07C43/00 , C07C69/007 , C07C69/767 , C09F5/08 , C07C69/76
CPC分类号： C07C69/618 , C07C45/68 , C07C69/007 , C07C69/16 , C07C69/18 , C07C69/28 , C07C69/56 , C07C69/76 , C07C69/78
摘要： Polyprenyl derivatives having the formula ##STR1## in which R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen atom, hydroxyl group, an alkoxy group having 1-8 carbon atoms, an aliphatic acyloxy group having 2-18 carbon atoms, an aromatic acyloxy group or an araliphatic acyloxy group having 2-3 carbon atoms in the aliphatic acyl moiety, R.sup.3 represents hydrogen atom, an alkyl group having 1-8 carbon atoms, an aliphatic acyl group having 2-18 carbon atoms, an aromatic acyl group or an araliphatic acyl group having 2-3 carbon atoms in the aliphatic acyl moiety, n is an integer of 1-4 and, when n is an integer of 2-4, R.sup.2 's may be the same or different; provided that, when n is 1 or 2, at least one of R.sup.1 and R.sup.2 's is hydroxyl group, an alkoxy group, an aliphatic acyloxy group, an aromatic acyloxy group or an araliphatic acyloxy group. These derivatives are useful as medicines for treating peptic ulcer.
摘要翻译：其中R 1和R 2可以相同或不同并且各自表示氢原子，羟基，具有1-8个碳原子的烷氧基，具有2-羟基的脂肪族酰氧基， 18个碳原子，芳香族酰氧基或脂肪族酰基部分中具有2-3个碳原子的芳脂肪酰氧基，R3表示氢原子，具有1-8个碳原子的烷基，具有2-18个碳原子的脂族酰基芳香族酰基或脂肪族酰基部分具有2-3个碳原子的芳脂酰基，n为1-4的整数，当n为2-4的整数时，R 2可以相同或不同，条件是当n为1或2时，R 1和R 2中的至少一个为羟基，烷氧基，脂族酰氧基，芳香族酰氧基或芳脂族酰氧基。这些衍生物可用作治疗消化性溃疡的药物。

8. 发明授权

US4192953A Polyprenyl derivatives 失效
标题翻译：聚丙烯衍生物
公开(公告)号：US4192953A
公开(公告)日：1980-03-11
申请号：US1162
申请日：1979-01-04
申请人： Hiroshi Mishima , Akira Ogiso , Shinsaku Kobayashi
发明人： Hiroshi Mishima , Akira Ogiso , Shinsaku Kobayashi
IPC分类号： C07C43/00 , C07C69/007 , A61K31/07 , A61K31/08 , C07C43/02
CPC分类号： C07C41/16 , C07C33/02 , C07C43/15 , C07C45/68 , C07C69/007 , C07C69/16 , C07C69/28 , C07C69/56 , C07C69/618 , C07C69/78 , Y10S514/926 , Y10S514/927
摘要： Polyprenyl derivatives having the formula ##STR1## in which R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen atom, hydroxyl group, an alkoxy group having 1-8 carbon atoms, an aliphatic acyloxy group having 2-18 carbon atoms, an aromatic acyloxy group or an araliphatic acyloxy group having 2-3 carbon atoms in the aliphatic acyl moiety, R.sup.3 represents hydrogen atom, an alkyl group having 1-8 carbon atoms, an aliphatic acyl group having 2-18 carbon atoms, an aromatic acyl group or an araliphatic acyl group having 2-3 carbon atoms in the aliphatic acyl moiety, n is an integer of 1-4 and, when n is an interger of 2-4, R.sup.2 's may be the same or different; provided that, when n is 1 or 2, at least one of R.sup.2 and R.sup.2 's is hydroxyl group, an alkoxy group, an aliphatic acyloxy group, an aromatic acyloxy group or an araliphatic acyloxy group. These derivatives are useful as medicines for treating peptic ulcer.
摘要翻译：其中R 1和R 2可以相同或不同并且各自表示氢原子，羟基，具有1-8个碳原子的烷氧基，具有2-羟基的脂肪族酰氧基， 18个碳原子，芳香族酰氧基或脂肪族酰基部分中具有2-3个碳原子的芳脂肪酰氧基，R3表示氢原子，具有1-8个碳原子的烷基，具有2-18个碳原子的脂族酰基芳香酰基或脂肪族酰基部分具有2-3个碳原子的芳脂酰基，n为1-4的整数，当n为2-4的整数时，R 2可以相同或不同; 条件是当n为1或2时，R 2和R 2中的至少一个为羟基，烷氧基，脂族酰氧基，芳香族酰氧基或芳脂族酰氧基。这些衍生物可用作治疗消化性溃疡的药物。

9. 发明授权

US4059641A Polyprenyl derivatives 失效
标题翻译：聚丙烯衍生物
公开(公告)号：US4059641A
公开(公告)日：1977-11-22
申请号：US633097
申请日：1975-11-18
申请人： Hiroshi Mishima , Akira Ogiso , Shinsaku Kobayashi
发明人： Hiroshi Mishima , Akira Ogiso , Shinsaku Kobayashi
IPC分类号： C07C69/025 , A61K31/045 , A61K31/075 , A61K31/215 , A61P1/04 , C07C27/00 , C07C33/02 , C07C41/00 , C07C43/00 , C07C43/14 , C07C43/178 , C07C67/00 , C07C69/007
CPC分类号： C07C45/64 , C07C33/02 , C07C41/16 , C07C43/15 , C07C45/68 , C07C69/007 , C07C69/16 , C07C69/18 , C07C69/28 , C07C69/56 , C07C69/614 , C07C69/618 , C07C69/76 , C07C69/78 , C07C69/92 , Y10S514/927
摘要： Polyprenyl derivatives having the formula ##STR1## in which R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen atom, hydroxyl group, an alkoxy group having 1-8 carbon atoms, an aliphatic acyloxy group having 2-18 carbon atoms, an aromatic acyloxy group or an araliphatic acyloxy group having 2-3 carbon atoms in the aliphatic acyl moiety, R.sup.3 represents hydrogen atom, an alkyl group having 1-8 carbon atoms, an aliphatic acyl group having 2-18 carbon atoms, an aromatic acyl group or an araliphatic acyl group having 2-3 carbon atoms in the aliphatic acyl moiety, n is an integer of 1-4 and, when n is an integer of 2-4, R.sup.2 's may be the same or different; provided that, when n is 1 or 2, at least one of R.sup.1 and R.sup.2 's is hydroxyl group, an alkoxy group, an aliphatic acyloxy group, an aromatic acyloxy group or an araliphatic acyloxy group. These derivatives are useful as medicines for treating peptic ulcer.
摘要翻译：其中R 1和R 2可以相同或不同并且各自代表氢原子，羟基，具有1-8个碳原子的烷氧基，具有2-取代基的脂肪族酰氧基的具有式 + tr 的聚丙烯基衍生物， 18个碳原子，芳香族酰氧基或脂肪族酰基部分中具有2-3个碳原子的芳脂肪酰氧基，R3表示氢原子，具有1-8个碳原子的烷基，具有2-18个碳原子的脂族酰基芳香族酰基或脂肪族酰基部分具有2-3个碳原子的芳脂酰基，n为1-4的整数，当n为2-4的整数时，R 2可以相同或不同，条件是当n为1或2时，R 1和R 2中的至少一个为羟基，烷氧基，脂族酰氧基，芳香族酰氧基或芳脂族酰氧基。这些衍生物可用作治疗消化性溃疡的药物。

10. 发明授权

US4914093A Pyridazinone derivatives, their preparation and use 失效
标题翻译：哒嗪酮衍生物，其制备和用途
公开(公告)号：US4914093A
公开(公告)日：1990-04-03
申请号：US325112
申请日：1989-03-16
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Seiji Kumakura , Hiroyuki Koike , Shinsaku Kobayashi
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Seiji Kumakura , Hiroyuki Koike , Shinsaku Kobayashi
IPC分类号： A61K31/50 , A61P1/04 , A61P7/02 , A61P9/04 , A61P9/12 , C07D237/00 , C07D237/04 , C07D237/14 , C07D401/12 , C07D403/12 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D237/04 , C07D237/14 , C07D249/08 , C07D401/12 , C07D403/12
摘要： Compounds of formula (I): ##STR1## (wherein Q is oxygen or sulfur, the dotted line is a single or double bond, A is alkylene, and R.sup.1 -R.sup.5 are a variety of atoms or organic groups)have excellent ability to potentiate myocardial contractivity and a variety of other properties, and can be used to treat cardiac disorders.
摘要翻译：式（I）化合物：其中Q为氧或硫，虚线为单键或双键，A为亚烷基，R1-R5为多种原子或有机基团）具有优异的增强心肌收缩力和多种其他特性的能力，可用于治疗心脏疾病。

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