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1. 发明授权

US5106868A Epoxycyclohexenone amides with antibacterial activity 失效
标题翻译：具有抗菌活性的环氧环己烯酮
公开(公告)号：US5106868A
公开(公告)日：1992-04-21
申请号：US696610
申请日：1991-05-07
申请人： Hirofumi Nakano , Mitsunobu Hara , Yutaka Saito , Yoji Ikuina , Toshimitsu Takiguchi , Masami Okabe
发明人： Hirofumi Nakano , Mitsunobu Hara , Yutaka Saito , Yoji Ikuina , Toshimitsu Takiguchi , Masami Okabe
IPC分类号： C07D303/36 , C07D303/46 , C12P17/02
CPC分类号： C12R1/465 , C07D303/36 , C07D303/46 , C12P17/02
摘要： Compounds UCF1 and derivatives thereof exhibit anti-bacterial and anti-tumor activities and may be used for the preparation of anti-bacterial and anti-tumor agents.Compounds UCF1 may be produced by fermentation of a microorganism of the genus Streptomyces capable of producing compounds UCF1, preferably Streptomyces sp. UOF1 (FERM BP-2844) and recovering the desired compounds from the cultured broth.The compounds UCF1 have the formula ##STR1## wherein R represents either ##STR2## The compounds may be oxidized to obtain derivatives of formula ##STR3## which exhibit similar pharmacological activities.

2. 发明授权

US5103018A Mitomycin derivatives 失效
标题翻译：麻醉药物衍生物
公开(公告)号：US5103018A
公开(公告)日：1992-04-07
申请号：US204429
申请日：1988-10-31
申请人： Kono Motomichi , Saito Yutaka , Kanda Yutaka , Kasai Masaji , Sato Akira , Morimoto Makoto , Ashizawa Tadashi
发明人： Kono Motomichi , Saito Yutaka , Kanda Yutaka , Kasai Masaji , Sato Akira , Morimoto Makoto , Ashizawa Tadashi
IPC分类号： C07D487/14 , C07D487/22 , C07H19/06 , C07J43/00
CPC分类号： C07D487/14 , C07H19/06 , C07J43/003
摘要： Mitomycin derivatives containing substituted dithioethylamino groups at the 7th position are provided. The mitomycin derivatives according to the present invention are superior to mitomycin C with respect to their improved anti-tumour activity and toxicity. More particularly, they exhibit a wider tolerance of dosage against Sarcoma 180A solid tumour as well as a better survival time and weaker bone marrow supression against P388.Furthermore, certain compounds exhibit a high water-solubility which is advantageous for pharmaceutical purposes. Excellent anti-tumour agents may readily be prepared by using the derivatives of the present invention.
摘要翻译： PCT No.PCT / JP87 / 00640 Sec。 371日期1988年10月31日第 102（e）日期1988年10月31日PCT PCT 1987年8月28日PCT公布。第WO88 / 01622号公报日期为1988年3月10日。在第七位置含有取代二硫代乙基氨基的霉素衍生物。关于其改善的抗肿瘤活性和毒性，根据本发明的丝裂霉素衍生物优于丝裂霉素C. 更具体地，它们对肉瘤180A实体瘤具有更宽的剂量耐受性，并且对P388具有更好的存活时间和更弱的骨髓抑制。此外，某些化合物表现出高水溶性，这对于药物目的是有利的。通过使用本发明的衍生物可以容易地制备出优异的抗肿瘤剂。

3. 发明授权

US4952576A UCY1003 derivatives 失效
标题翻译： UCY1003衍生物
公开(公告)号：US4952576A
公开(公告)日：1990-08-28
申请号：US223193
申请日：1988-07-22
申请人： Toru Yasuzawa , Hiroshi Sano , Hirofumi Nakano , Shunji Ichikawa , Katsuichi Shuto
发明人： Toru Yasuzawa , Hiroshi Sano , Hirofumi Nakano , Shunji Ichikawa , Katsuichi Shuto
IPC分类号： A61K31/58 , A61P25/04 , C07D493/02 , C07D493/08 , C07D493/10 , C07J71/00
CPC分类号： C07D493/10 , C07J71/0005
摘要： Compounds having analgesic activity which have the formula ##STR1## wherein R.sub.1 -R.sub.6 represent hydrogen or a substituent and X and Y together represent inter alia as epoxyethylene, ethylene halohydrin, haloethylene or a --CH.dbd.CH-group.

4. 发明授权

US4880825A Mitomycin derivatives 失效
标题翻译：丝裂霉素衍生物
公开(公告)号：US4880825A
公开(公告)日：1989-11-14
申请号：US173219
申请日：1988-03-25
申请人： Masaji Kasai , Yutaka Kanda , Motomichi Kono , Yutaka Saito , Makoto Morimoto , Tadashi Ashizawa
发明人： Masaji Kasai , Yutaka Kanda , Motomichi Kono , Yutaka Saito , Makoto Morimoto , Tadashi Ashizawa
IPC分类号： C07D491/22
CPC分类号： C07D491/22
摘要： Mitomycin derivatives having potent anti-tumor activity having the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 represents carbamoyloxymethyl and the other represents hydrogen or R.sub.1 and R.sub.2 are bonded together to form methylene;X is hydrogen or halogen;Y is hydrogen or methyl;Z is hydrogen, methyl or acyl; andn is an integer of 2 or 3.

5. 发明授权

US4338745A Process for mass propagation of plantlets 失效
标题翻译：植物大规模繁殖的过程
公开(公告)号：US4338745A
公开(公告)日：1982-07-13
申请号：US127276
申请日：1980-03-05
申请人： Masanaru Misawa , Shinsaku Takayama , Yoshiki Takashige , Hiroshi Tsumori
发明人： Masanaru Misawa , Shinsaku Takayama , Yoshiki Takashige , Hiroshi Tsumori
IPC分类号： A01H4/00 , A01G1/00
CPC分类号： A01H4/005
摘要： A process for mass propagation of plantlets, which comprises cultivating in vitro a piece of a plant in a medium to obtain an aggregate with stems, leaves, buds, roots, flowers and/or bulbs and cultivating said aggregate in a liquid medium with shaking to obtain plantlets. This process may be applied to a wide variety of plants from Gymnospermae to Angiospermae.
摘要翻译：一种植物的大规模繁殖的方法，其包括在培养基中体外培养一片植物以获得具有茎，叶，芽，根，花和/或灯泡的骨料，并在摇动到液体培养基中培养所述骨料获得小植株。这个过程可以应用于从Gymnosperma到Angiospermae的各种植物。

6. 发明授权

US4322345A 2-Azetidinone 4-carboxy derivatives and a process for producing the same 失效
标题翻译： 2-氮杂环丁酮-4-羧基衍生物及其制备方法
公开(公告)号：US4322345A
公开(公告)日：1982-03-30
申请号：US142542
申请日：1980-04-21
申请人： Tadashi Hirata , Akira Sato , Nobuhiro Nakamizo
发明人： Tadashi Hirata , Akira Sato , Nobuhiro Nakamizo
IPC分类号： C07D205/08 , C07D403/06
CPC分类号： C07D205/08
摘要： A 2-azetidinone of formula (I): ##STR1## wherein R.sub.1 represents an aralkoxy, acyloxy, sulphonyloxy or amino group any of which may be substituted, or hydrogen, hydroxy, alkoxy or azido;R.sub.2 represents an alkyl or aralkyl group either of which may be substituted, or hydrogen;R.sub.3 represents an alkyl, aryl, aralkyl, alkenyl, aralkenyl, alkynyl, aralkynyl, acyl or heterocyclic group any of groups may be substituted;andR.sub.4 represents an alkyl, alkenyl, aryl or aralkyl group any of which may be substituted;or formula (I'): ##STR2## wherein R.sub.1 ' is the same as R.sub.1 above;R.sub.2 ' represents an alkyl, aralkyl or trialkylsilyl group any of which may be substituted, or hydrogen;R.sub.3 ' is the same as R.sub.3 above;andR.sub.4 ' represents an alkyl, aralkyl or trialkylsilyl group any of which may be substituted, or hydrogen; provided that when R.sub.1 ' represents azido or optionally substituted amino, R.sub.2 ' represents hydrogen or CH.sub.2 CCl.sub.3 and R.sub.4 ' represents ##STR3## R.sub.3 ' represents other than ##STR4## or a pharmaceutically acceptable salt thereof is disclosed. The derivatives exhibit .beta.-lactamase inhibiting activity and are thus of interest as anti-bacterial agents, used alone or together with known antibiotic subtances.
摘要翻译：式（I）的2-氮杂环丁酮：其中R 1表示可以被取代的芳烷氧基，酰氧基，磺酰氧基或氨基，或氢，羟基，烷氧基或叠氮基; R2表示可以被取代的烷基或芳烷基，或氢; R 3表示烷基，芳基，芳烷基，烯基，芳烯基，炔基，芳炔基，酰基或杂环基，任何基团可以被取代; 并且R 4表示任何可以被取代的烷基，烯基，芳基或芳烷基; 或式（I'）：其中R 1'与上述R 1相同; R 2'表示任何可以被取代的烷基，芳烷基或三烷基甲硅烷基，或氢; R3'与上述R3相同; 和R 4'表示任何可以被取代的烷基，芳烷基或三烷基甲硅烷基，或氢; 条件是当R 1'表示叠氮基或任选被取代的氨基时，R 2'表示氢或CH 2 ClCl 3，并且R 4'表示除了“IMAGE”以外的R 3'或其药学上可接受的盐。衍生物表现出β-内酰胺酶抑制活性，因此作为抗菌剂是有意义的，单独使用或与已知的抗生素偶联使用。

7. 发明授权

US4126625A Certain 5-substituted-3-methyl-2-benzofuran acetic acids 失效
标题翻译：某些5-取代的3-取代的3-甲基-2-苯并呋喃乙酸
公开(公告)号：US4126625A
公开(公告)日：1978-11-21
申请号：US704604
申请日：1976-07-12
申请人： Shigetaka Yoshina, deceased , by Teruko Yoshina, legal heir , Tsutomu Kameyama , Yoshimasa Oiji , Akira Kiyohara
发明人： Shigetaka Yoshina, deceased , by Teruko Yoshina, legal heir , Tsutomu Kameyama , Yoshimasa Oiji , Akira Kiyohara
IPC分类号： C07D307/79 , C07D307/80
CPC分类号： C07D307/79
摘要： This invention relates to certain derivatives of benzo (b) furylacetic acid, namely, 5-substituted-3-methyl-2-benzo(b)furylacetic acids having interesting pharmacological properties, in particular an antiphlogistic and analgesic activity.

8. 发明授权

US4019957A Process for producing (2'-amino-2'-deoxypentofuranosyl) guanine 失效
标题翻译：制备（2 {40-氨基-2 {40-脱氧呋喃糖基）鸟嘌呤的方法
公开(公告)号：US4019957A
公开(公告)日：1977-04-26
申请号：US706865
申请日：1976-07-19
申请人： Takeo Suzuki , Toshihide Nakanishi
发明人： Takeo Suzuki , Toshihide Nakanishi
IPC分类号： C07H19/16 , C12P19/40 , C12D13/06
CPC分类号： C07H19/16 , C12P19/40 , Y10S435/803 , Y10S435/822
摘要： The present invention relates to the production of a new compound (2'-amino-2'-deoxypentofuranosyl) guanine by a fermantation process using a microorganism belonging to the genus Aerobacter.
摘要翻译：本发明涉及通过使用属于Aerobacter属的微生物的发明方法生产新化合物（2'-氨基-2'-脱氧呋喃糖基）鸟嘌呤。

9. 发明授权

US5212079A Process for the preparation of ascorbic acid-2-phosphate 失效
标题翻译：制备抗坏血酸-2-磷酸的方法
公开(公告)号：US5212079A
公开(公告)日：1993-05-18
申请号：US758528
申请日：1991-09-06
申请人： Tatsuro Fujio , Akihiko Maruyama , Satoshi Koizumi
发明人： Tatsuro Fujio , Akihiko Maruyama , Satoshi Koizumi
IPC分类号： C12P17/04
CPC分类号： C12R1/01 , C12P17/04
摘要： A process for the preparation of ascorbic acid-2-phosphate, which comprises reacting ascorbic acid or araboascorbic acid with a phosphate donor other than ATP in an aqueous medium in the presence of an effective amount of an enzyme derived and capable of preferentially catalyzing the enzymatic phosphorylation in the 2-position of ascorbic acid or araboascorbic acid by said phosphate donor, and recovering the resultant ascorbic acid-2-phosphate from the reaction solution.
摘要翻译：一种用于制备抗坏血酸-2-磷酸酯的方法，该方法包括在水性介质中，在有效量的酶存在下能够使抗坏血酸或阿拉伯糖酸与除ATP以外的磷酸盐供体反应，并能够优先催化酶由所述磷酸盐供体在抗坏血酸或阿拉伯糖酸的2-位上磷酸化，并从反应溶液中回收得到的抗坏血酸-2-磷酸。

10. 发明授权

US5080917A Oral compositions for ruminants 失效
标题翻译：口服组合物
公开(公告)号：US5080917A
公开(公告)日：1992-01-14
申请号：US333170
申请日：1989-04-03
申请人： Kunio Itoh , Kiyoshi Sugiyama , Motohiro Ohta
发明人： Kunio Itoh , Kiyoshi Sugiyama , Motohiro Ohta
IPC分类号： A23K1/00 , A61K9/50 , A61K9/52
CPC分类号： A61K9/5047 , A23K40/35 , A61K9/5015 , A61K9/5026 , Y10S426/807
摘要： A coating agent for delaying the release of a physiologically active substance to be administered per os to ruminants, said coating comprising a veterinary acceptable water-soluble, synthetic high molecular compound and ethylcellulose, said coating agent being stable in the first stomach or rumen of ruminants and capable of being effectively disintegrated for subsequent absorption in the 4th stomach of ruminants, characterized in that said coating agent further comprises at least one substance which is miscible with both of said high molecular weight compound and ethylcellulose and is insoluble in water.Said coating agent forms a coat which protects the active substance from degradation in the first stomach of a ruminant at a pH of about 5.5 and rapidly breaks down in the 4th stomach at a pH of about 3, thereby releasing the active ingredient for absorption by the animal.The coating agent and the actives coated therewith and their preparation are described.

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