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1. 发明授权

US4618613A Preventive and healing composition for diseases due to lipoxygenase metabolic products 失效
标题翻译：由于脂氧合酶代谢产物引起的疾病的预防和治疗组合物
公开(公告)号：US4618613A
公开(公告)日：1986-10-21
申请号：US749716
申请日：1985-06-28
申请人： Kazuko Hashizume , Hiroshi Kase , Shigeto Kitamura , Takao Iida , Kunikatsu Shirahata , Kenji Omori , Katsuichi Shuto
发明人： Kazuko Hashizume , Hiroshi Kase , Shigeto Kitamura , Takao Iida , Kunikatsu Shirahata , Kenji Omori , Katsuichi Shuto
IPC分类号： C07D215/60 , A61K31/47 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P29/00 , A61P37/08
CPC分类号： A61K31/47 , Y10S514/826
摘要： A preventive and healing composition for diseases due to lipoxygenase metabolic products, which comprises an effective amount of a compound represented by the formula: ##STR1## wherein R is an alkyl group having 1 to 15 carbon atoms and at least one pharmaceutically acceptable carrier.
摘要翻译：一种用于由脂氧合酶代谢产物引起的疾病的预防和治疗组合物，其包含有效量的由下式表示的化合物：其中R是具有1至15个碳原子的烷基和至少一种药学上可接受的载体。

2. 发明授权

US4555402A Physiologically active substance K-252, process for producing same and pharmaceutical composition containing same 失效
标题翻译：生理活性物质K-252，其生产方法和含有其的药物组合物
公开(公告)号：US4555402A
公开(公告)日：1985-11-26
申请号：US640159
申请日：1984-08-10
申请人： Yuzuru Matsuda , Kazuyuki Iwahashi , Takao Iida , Noriaki Hirayama , Kozo Asano , Katsuichi Shuto , Koji Yamada , Kunikatsu Shirahata , Hiroshi Kase
发明人： Yuzuru Matsuda , Kazuyuki Iwahashi , Takao Iida , Noriaki Hirayama , Kozo Asano , Katsuichi Shuto , Koji Yamada , Kunikatsu Shirahata , Hiroshi Kase
IPC分类号： C07G99/00 , A61K31/55 , A61K35/74 , A61P37/08 , C07D498/22 , C12P1/04 , C12P1/06 , C12P17/18 , C12R1/01
CPC分类号： C12P1/06
摘要： A novel physiologically active substance K-252 having an antiallergic action is produced by culturing a microorganism of the genus Nocardiopsis.
摘要翻译：具有抗过敏作用的新型生理活性物质K-252通过培养诺卡氏菌属的微生物而产生。

3. 发明授权

US4657916A Quinoline-N-oxide derivative and pharmaceutical composition 失效
标题翻译：喹啉-N-氧化物衍生物和药物组合物
公开(公告)号：US4657916A
公开(公告)日：1987-04-14
申请号：US772693
申请日：1985-09-05
申请人： Masayuki Teranishi , Koji Suzuki , Hiroshi Kase , Shigeto Kitamura , Katsuichi Shuto , Kenji Omori
发明人： Masayuki Teranishi , Koji Suzuki , Hiroshi Kase , Shigeto Kitamura , Katsuichi Shuto , Kenji Omori
IPC分类号： A61K31/47 , A61P43/00 , C07D215/60 , C07D405/12 , C07F7/18
CPC分类号： C07D405/12 , C07D215/60
摘要： A quinoline-N-oxide derivative represented by the formula: ##STR1## wherein X is hydroxy, lower alkoxy, lower alkylthio, unsubstituted or substituted aralkyloxy, or unsubstituted or substituted aralkylthio; Y is a hydrogen atom or halogen atom; R.sub.1 is alkylene or alkenylene having 3 to 15 carbon atom; Z is hydroxymethyl, lower alkoxymethyl, unsubstituted or substituted aryloxymethyl, tetrahydropyranyloxymethyl, tetrahydrofuranyloxymethyl, unsubstituted or substituted arylsulfonyloxymethyl, lower alkylthiomethyl, unsubstituted or substituted arylthiomethyl, lower alkylsulfinylmethyl, unsubstituted or substituted arylsulfinylmethyl, lower alkylsulfonylmethyl, unsubstituted or substituted arylsulfonylmethyl, aminomethyl, --CH.sub.2 NHR.sub.2 (wherein R.sub.2 is lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), --CH.sub.2 NR.sub.3 R.sub.4 (wherein R.sub.3 and R.sub.4 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), --CH.sub.2 N.sup.+ R.sub.5 R.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl, where the counterion is an anion of acid or a hydroxyl ion), --COR.sub.8 (wherein R.sub.8 is a hydrogen atom, lower alkyl or hydroxy), --CH(OR.sub.9).sub.2 (wherein R.sub.9 is lower alkyl), iminomethyl, hydroxyiminomethyl, or a halogen atom and its salts, can very strongly inhibit the lipoxygenase and considerably suppress production and release of its metabolites, and thus are useful as preventive and healing agents for the diseases caused by the lipoxygenase metabolites.
摘要翻译：由下式表示的喹啉-N-氧化物衍生物：其中X为羟基，低级烷氧基，低级烷硫基，未取代或取代的芳烷氧基，或未取代或取代的芳烷硫基; Y是氢原子或卤素原子; R1是具有3至15个碳原子的亚烷基或亚烯基; Z是羟甲基，低级烷氧基甲基，未取代或取代的芳氧基甲基，四氢吡喃氧基甲基，四氢呋喃氧基甲基，未取代或取代的芳基磺酰氧基甲基，低级烷硫基甲基，未取代或取代的芳基硫代甲基，低级烷基亚磺酰基甲基，未取代或取代的芳基亚磺酰基甲基，低级烷基磺酰基甲基，未取代或取代的芳基磺酰基甲基，氨基甲基，-CH2NHR2（其中R 2是低级烷基，未取代或取代的芳烷基或未取代或取代的芳基），-CH 2 NR 3 R 4（其中R 3和R 4是低级烷基，未取代或取代的芳烷基，或未取代或取代的芳基），-CH 2 N + R 5 R 6 R 7（其中R 5，R 6 ，R 7为低级烷基，未取代或取代的芳烷基或未取代或取代的芳基，其中抗衡离子为酸或羟基离子的阴离子），-COR8（其中R8为氢原子，低级烷基或羟基），-CH （OR 9）2（其中R 9为低级烷基），亚氨基甲基，羟基亚氨基甲基或卤素原子及其盐可以非常强烈地抑制脂氧合酶，并显着抑制其代谢物的产生和释放，因此可用作由脂氧合酶代谢物引起的疾病的预防和治疗剂。

4. 发明授权

US4683220A Novel physiologically active substances K-26, a process for preparation thereof and a pharmaceutical composition containing the same 失效
标题翻译：新型生理活性物质K-26，其制备方法和含有它的药物组合物
公开(公告)号：US4683220A
公开(公告)日：1987-07-28
申请号：US912685
申请日：1986-09-26
申请人： Masayuki Yamato , Hiroshi Kase , Isao Kawamoto , Masaji Kasai , Kunikatsu Shirahata , Takashi Deguchi , Katsuichi Shuto , Akira Karasawa , Ryo Okachi , Kiyoshi Nakayama
发明人： Masayuki Yamato , Hiroshi Kase , Isao Kawamoto , Masaji Kasai , Kunikatsu Shirahata , Takashi Deguchi , Katsuichi Shuto , Akira Karasawa , Ryo Okachi , Kiyoshi Nakayama
IPC分类号： C12P21/00 , A61K35/74 , A61K38/00 , A61P9/12 , C07F9/38 , C07F9/40 , C07K5/06 , C07K14/005 , C07K14/195 , C07K14/41 , C12P21/02 , C12R1/01 , A61K37/64
CPC分类号： C07F9/3808 , C07F9/3882 , C07F9/4006 , C07F9/4056 , C07K5/06191 , A61K38/00
摘要： Disclosed is a novel physiologically active substance, K-26, a process for preparation thereof and a pharmaceutical composition containing the same. The composition of matter, K-26, is useful as a hypotensive agent.
摘要翻译：公开了一种新的生理活性物质K-26，其制备方法和含有该生物活性物质的药物组合物。物质的组成，K-26，作为一种降压剂是有用的。

5. 发明授权

US5011854A Hydroxamic acid derivatives and use thereof in combatting lipoxygenase-mediated diseases 失效
标题翻译：羟肟酸衍生物及其在抗氧化酶介导的疾病中的应用
公开(公告)号：US5011854A
公开(公告)日：1991-04-30
申请号：US281050
申请日：1989-12-07
申请人： Mitsuru Takahashi , Shigeto Kitamura , Hiroshi Kase , Masaji Kasai , Isao Kawamoto , Takao Iida , Hiroshi Sano , Hiromitsu Saito , Koji Yamada , Chikara Murakata
发明人： Mitsuru Takahashi , Shigeto Kitamura , Hiroshi Kase , Masaji Kasai , Isao Kawamoto , Takao Iida , Hiroshi Sano , Hiromitsu Saito , Koji Yamada , Chikara Murakata
IPC分类号： C07C239/16 , C07C259/06
CPC分类号： C07C239/16 , C07C259/06
摘要： A hydroxamic acid compound represented by the general formula (I) or a salt thereof; ##STR1## wherein R.sup.1 represents a hydrogen atom, or a substituted or unsubstituted alkanoyl group, R.sup.2 represents an unsubstituted alkanoyl, substituted lower alkanoyl or substituted lower alkyl group, and m represents an integer of 3 to 7, which are useful for the prevention and/or treatment of diseases caused by lipoxygenase-mediated metablites.

6. 发明授权

US4522812A Novel physiologically active substance K-4, a process for preparation thereof and a pharmaceutical composition containing the same 失效
标题翻译：新型生理活性物质K-4，其制备方法和含有它的药物组合物
公开(公告)号：US4522812A
公开(公告)日：1985-06-11
申请号：US407082
申请日：1982-08-11
申请人： Toshiro Koguchi , Hiroshi Kase , Isao Kawamoto , Masaji Kasai , Kunikatsu Shirahata , Ryo Okachi , Kiyoshi Nakayama
发明人： Toshiro Koguchi , Hiroshi Kase , Isao Kawamoto , Masaji Kasai , Kunikatsu Shirahata , Ryo Okachi , Kiyoshi Nakayama
IPC分类号： C12N1/20 , A61K35/74 , A61K38/00 , A61P9/12 , C07F9/38 , C07F9/40 , C07G99/00 , C12P1/06 , C12R1/03 , C07C103/52 , A61K37/02
CPC分类号： C07F9/4056 , C07F9/3808 , C07F9/3882 , C07F9/4006 , A61K38/00
摘要： Disclosed is a novel physiologically active substance K-4 which has a hypotensive activity, a process production thereof and a pharmaceutical composition containing the same.
摘要翻译：公开了一种具有低血压活性的新型生理活性物质K-4，其制备方法和含有它们的药物组合物。

7. 发明授权

US4962125A Novel substance KS-619-1, preparation process and pharmaceutical composition 失效
标题翻译：新型物质KS-619-1，制备方法和药物组成
公开(公告)号：US4962125A
公开(公告)日：1990-10-09
申请号：US235654
申请日：1988-08-24
申请人： Hiroshi Kase , Yuzuru Matauda , Kunikatsu Shirahata , Toru Yasuzawa , Koji Yamada
发明人： Hiroshi Kase , Yuzuru Matauda , Kunikatsu Shirahata , Toru Yasuzawa , Koji Yamada
IPC分类号： C07G99/00 , A61K31/19 , A61K35/74 , A61P9/08 , C12P1/06 , C12P29/00 , C12R1/465
CPC分类号： C12P1/06
摘要： A novel physiologically active substance KS-619-1 having a vasodilative activity is produced by culturing Streptomyces californicus ATCC 3312.
摘要翻译：具有血管扩张活性的新型生理活性物质KS-619-1是通过培养加利福尼亚镰刀菌（Streptomyces californicus）ATCC 3312产生的。

8. 发明授权

US4692310A Substance K-259-2 and a process for producing the same 失效
标题翻译：物质K-259-2及其制备方法
公开(公告)号：US4692310A
公开(公告)日：1987-09-08
申请号：US852590
申请日：1986-04-16
申请人： Hiroshi Kase , Yuzuru Matsuda , Isao Kawamoto , Kozo Asano , Kunikatsu Shirahata , Tohru Yasuzawa , Koji Yamada
发明人： Hiroshi Kase , Yuzuru Matsuda , Isao Kawamoto , Kozo Asano , Kunikatsu Shirahata , Tohru Yasuzawa , Koji Yamada
IPC分类号： C07G11/00 , A61K35/74 , A61P9/08 , C07C66/02 , C12P1/06 , C12P15/00 , C12R1/29
CPC分类号： C12P1/06
摘要： A new substance K-259-2 having a molecular formula of C.sub.21 H.sub.18 O.sub.7, a molecular weight of 382 and an elemental analysis (%) of H: 4.50, C: 65.53 and N: 0. This substance is of interest in providing a new vasodilating agent in view of its ability to dilate the blood vessel, particularly the artery, of mammals. This substance may be obtained by fermentation of a microorganism Micromonospora sp. K-259 (FERM BP 569).
摘要翻译：分子式为C 21 H 18 O 7，分子量382，元素分析（％）H：4.50，C：65.53和N：0的新物质K-259-2。提供新的血管扩张剂鉴于其能够扩大哺乳动物的血管，特别是动脉的能力。该物质可以通过微生物微单孢菌发酵获得。 K-259（FERM BP 569）。

9. 发明授权

US4677125A Phosphorus-containing peptide derivatives 失效
标题翻译：含磷肽衍生物
公开(公告)号：US4677125A
公开(公告)日：1987-06-30
申请号：US902109
申请日：1986-08-29
申请人： Masayuki Teranishi , Mitsuru Takahashi , Hisayo Nomoto , Hiroshi Kase , Katsuichi Shuto , Kazuhiro Kubo , Akira Karasawa
发明人： Masayuki Teranishi , Mitsuru Takahashi , Hisayo Nomoto , Hiroshi Kase , Katsuichi Shuto , Kazuhiro Kubo , Akira Karasawa
IPC分类号： A61K38/00 , C07C59/68 , C07F9/38 , C07F9/40 , C07K5/06 , A61K37/02 , C07K5/08
CPC分类号： C07F9/3808 , C07C59/68 , C07F9/4006 , C07F9/4065 , C07K5/06191 , A61K38/00
摘要： Phosphorus-containing oligopeptide derivatives are prepared by synthetic methods. The compounds exhibit angiotensin converting enzyme-inhibiting action and are, therefore, useful as anti-hypertensive agents.
摘要翻译：通过合成方法制备含磷寡肽衍生物。化合物表现出血管紧张素转化酶抑制作用，因此可用作抗高血压药。

10. 发明授权

US5703085A Xanthine derivatives 失效
标题翻译：黄嘌呤衍生物
公开(公告)号：US5703085A
公开(公告)日：1997-12-30
申请号：US537770
申请日：1995-10-20
申请人： Fumio Suzuki , Nobuaki Koike , Junichi Shimada , Joji Nakamura , Shizuo Shiozaki , Shigeto Kitamura , Shunji Ichikawa , Hiroshi Kase , Hiromi Nonaka
发明人： Fumio Suzuki , Nobuaki Koike , Junichi Shimada , Joji Nakamura , Shizuo Shiozaki , Shigeto Kitamura , Shunji Ichikawa , Hiroshi Kase , Hiromi Nonaka
IPC分类号： C07D473/06 , A61K31/52 , C07D473/10 , C07D473/12
CPC分类号： C07D473/06
摘要： The present invention relates to novel xanthine derivatives and pharmaceutically acceptable salts thereof, represented by Formula (I): ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, R.sup.4 represents lower alkyl, or substituted or unsubstituted aryl, R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, and lower alkoxy, or R.sup.5 and R.sup.6 are combined together to represent --O--(CH.sub.2)p--O-- (p is an integer of 1 to 3), n represents 0, 1, or 2, and m represents 1 or 2. The compounds of the present invention have an adenosine A.sub.2 receptor antagonistic activity, and are useful for the treatment or prevention of various kinds of diseases caused by hyperergasia of adenosine A.sub.2 receptors (for example, Parkinson's disease, senile dementia, depression, asthma, and osteoporosis).
摘要翻译： PCT No.PCT / JP95 / 00267 Sec。 371 1995年10月20日第 102（e）1995年10月20日日期PCT提交1995年2月23日PCT公布。公开号WO95 / 23148 日期：1995年8月31日本发明涉及由式（I）表示的新颖的黄嘌呤衍生物及其药学上可接受的盐：其中R1，R2和R3独立地表示氢，低级烷基，低级链烯基或低级炔基，R 4表示低级烷基或取代或未取代的芳基，R 5和R 6独立地表示氢，低级烷基和低级烷氧基，或者R 5和R 6结合在一起代表-O-（CH 2）p O-（p是整数 1〜3），n表示0,1或2，m表示1或2.本发明化合物具有腺苷A2受体拮抗活性，可用于治疗或预防各种疾病腺苷A2受体（例如帕金森病，老年性痴呆，抑郁症，哮喘和骨质疏松症）的过度高血症。

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