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1. 发明授权

US6143779A Benzofuranone derivatives and a method for producing them 失效
标题翻译：苯并呋喃酮衍生物及其制备方法
公开(公告)号：US6143779A
公开(公告)日：2000-11-07
申请号：US142666
申请日：1998-12-07
申请人： Makoto Yoshihama , Masamichi Nakakoshi , Junji Nakamura , Shoji Nakayama
发明人： Makoto Yoshihama , Masamichi Nakakoshi , Junji Nakamura , Shoji Nakayama
IPC分类号： A61K31/34 , A61K31/343 , A61P5/28 , A61P5/32 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07D307/83 , C07D405/06 , C07D407/06
CPC分类号： C07D405/06 , C07D307/83 , C07D407/06
摘要： The present invention provides new benzofuranone derivatives and a method for producing the derivatives useful for a therapeutic agent for preventing and/or treating hormone dependent diseases.The present invention is a new benzofuranone derivative represented by a particular general formula (I). ##STR1## In the production, a particular benzofuranone compound and a particular benzaldehyde are reacted.
摘要翻译： PCT No.PCT / JP98 / 00090 Sec。 371 1998年12月7日第 102（e）日期1998年12月7日PCT提交1998年1月13日PCT公布。第WO98 / 30556号公报日期：1998年7月16日本发明提供了新的苯并呋喃酮衍生物和用于制备用于预防和/或治疗激素依赖性疾病的治疗剂的衍生物的方法。本发明是由特定的通式（I）表示的新的苯并呋喃酮衍生物。在生产中，特定的苯并呋喃酮化合物和特定的苯甲醛反应。

2. 发明授权

US6080781A Tetralone or benzopyranone derivatives and a method for producing them 有权
标题翻译：四氢萘酮或苯并吡喃酮衍生物及其制备方法
公开(公告)号：US6080781A
公开(公告)日：2000-06-27
申请号：US155513
申请日：1999-01-19
申请人： Makoto Yoshihama , Masamichi Nakakoshi , Junji Nakamura , Shoji Nakayama
发明人： Makoto Yoshihama , Masamichi Nakakoshi , Junji Nakamura , Shoji Nakayama
IPC分类号： C07C49/643 , A61F5/24 , A61K31/12 , A61K31/35 , A61K31/352 , A61K31/353 , A61P25/04 , C07C45/74 , C07C49/697 , C07C49/747 , C07C49/755 , C07C65/40 , C07C221/00 , C07C225/22 , C07D311/22 , C07D317/54 , C07D319/18 , C07D407/06 , A61K31/122
CPC分类号： C07D407/06 , C07C225/22 , C07C45/74 , C07C49/747 , C07C49/755 , C07C65/40 , C07D311/22 , C07D317/54 , C07D319/18 , C07C2102/10
摘要： The present invention provides new tetralone or benzopyranone derivatives and a method for producing the derivatives useful for a therapeutic agent for preventing and/or treating hormone dependent diseases. The present invention is a new tetralone or benzopyranone derivative represented by a particular general formula (I). ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen, a hydroxy group, an alkyloxy group or an aralkyloxy group, respectively, R.sub.3 -R.sub.7 represent hydrogen, a hydroxy group or a straight or branched alkyl, alkyloxy or aralkyloxy group having 1-6 carbon atoms, a halogen, an amino group or an alkylene dioxy group joined at R.sub.3 and R.sub.4, R.sub.4 and R.sub.5, R.sub.5 and R.sub.6, or R.sub.6 and R.sub.7, respectively, and A represents a methylene or oxygen.In the production, a particular tetralone or benzopyranone compound and a particular benzaldehyde compound are reacted.
摘要翻译： PCT No.PCT / JP98 / 00344 Sec。 371日期1999年1月19日 102（e）1999年1月19日PCT PCT 1998年1月28日PCT公布。第WO98 / 32724号公报日期：1998年7月30日本发明提供新的四氢萘酮或苯并吡喃酮衍生物以及用于治疗激素依赖性疾病的治疗剂的衍生物的制备方法。本发明是由特定通式（I）表示的新的四氢萘酮或苯并吡喃酮衍生物。其中R1和R2分别表示氢，羟基，烷氧基或芳烷氧基，R3-R7表示氢，羟基或具有1-6个碳原子的直链或支链烷基，烷氧基或芳烷氧基，卤素，在R3和R4，R4和R5，R5和R6或R6和R7分别连接的氨基或亚烷基二氧基，A表示亚甲基或氧。在生产中，特定的四氢萘酮或苯并吡喃酮化合物和特定的苯甲醛化合物反应。

3. 发明授权

US5079377A Novel androst-4-ene-3,17-dione derivatives and method for preparing same 失效
标题翻译：新型安慰剂-4-环-3,17-二酮衍生物及其制备方法
公开(公告)号：US5079377A
公开(公告)日：1992-01-07
申请号：US555691
申请日：1990-07-23
申请人： Makoto Yoshihama , Koji Tamura , Nobuo Miyata , Shoji Nakayama , Masamichi Nakakoshi
发明人： Makoto Yoshihama , Koji Tamura , Nobuo Miyata , Shoji Nakayama , Masamichi Nakakoshi
IPC分类号： A61K31/565 , C07J1/00 , C12P33/06
CPC分类号： C07J1/0011 , C12P33/06
摘要： Novel androst-4-ene-3,17-dione derivatives are disclosed. The group of these compounds has biological activities, in particular, the inhibiting activity on human placenta-derived estrogen-synthesizing enzyme. Therefore these compounds are expected to be utilized in the field of medical care, particularly as anticancer drugs.

4. 发明授权

US4975368A Novel androst-4-ene-3,17-dione derivatives and method for preparing same 失效
标题翻译：新型雄甾-4-烯-3,17-二酮衍生物及其制备方法
公开(公告)号：US4975368A
公开(公告)日：1990-12-04
申请号：US279596
申请日：1988-09-26
申请人： Makoto Yoshihama , Koji Tamura , Nobuo Miyata , Shoji Nakayama , Masamichi Nakakoshi
发明人： Makoto Yoshihama , Koji Tamura , Nobuo Miyata , Shoji Nakayama , Masamichi Nakakoshi
IPC分类号： A61K31/565 , C07J1/00 , C12P33/06
CPC分类号： C07J1/0011 , C12P33/06
摘要： Novel androst-4-ene-3,17-dione derivatives are disclosed. The group of these compounds has biological activities, in particular, the inhibiting activity on human placenta-derived estrogen-synthesizing enzyme. Therefore these compounds are expected to be utilized in the field of medical care, particularly as anticancer drugs.

5. 发明授权

US5098535A Process for preparing 14-.alpha.-hydroxy-4-androstene-3,6,17-trione 失效
标题翻译：制备14-（ALPHA） - 羟基-4-雄甾-336,17-三烯的方法
公开(公告)号：US5098535A
公开(公告)日：1992-03-24
申请号：US475502
申请日：1990-02-06
申请人： Masamichi Nakakoshi , Kohji Tamura , Makoto Yoshihama , Nobuo Miyata
发明人： Masamichi Nakakoshi , Kohji Tamura , Makoto Yoshihama , Nobuo Miyata
IPC分类号： A61K31/565 , A61P35/00 , A61P43/00 , C07J1/00 , C07J75/00
CPC分类号： C07J1/0011
摘要： A process for the preparation in high yield of 14.alpha.-hydroxy-4-androstene-3,6,17-trione which has an aromatase inhibition activity and is useful as an antitumor agent, in which the 6.beta.-hydroxyl group of 6.beta., 14.alpha.-dihydroxy-4-androstene-3,17-dione is selectively oxidized with the aid of visible light energy.

6. 发明授权

US5164302A Method for preparing 7.beta.-hydroxy-4-pregnene-3,20-dione derivatives 失效
标题翻译：制备7β-羟基-4-孕烯-3,20-二酮衍生物的方法
公开(公告)号：US5164302A
公开(公告)日：1992-11-17
申请号：US436582
申请日：1989-11-15
申请人： Makoto Yoshihama , Koji Tamura , Nobuo Miyata , Masamichi Nakakoshi
发明人： Makoto Yoshihama , Koji Tamura , Nobuo Miyata , Masamichi Nakakoshi
IPC分类号： C07J7/00 , C12P33/06
CPC分类号： C12P33/06 , C07J7/002 , C07J7/0045 , Y10S435/911
摘要： Novel 7.beta.-hydroxy-4-pregnene-3,20-dione derivatives are disclosed.The group of these compounds has possibility of being utilized as an intermediate for the synthesis of progesterone derivatives having ovulation-inhibiting activity. These compounds themselves have also cell differentiation activity for M1 cells.
摘要翻译：公开了新型7β-羟基-4-孕烯-3,20-二酮衍生物。这些化合物的一组可能被用作合成具有排卵抑制活性的孕酮衍生物的中间体。这些化合物本身也具有M1细胞的细胞分化活性。

7. 发明授权

US5028722A Novel 7 .beta.-hydroxy-4-pregnene-3,20-dione derivatives and method for preparing same 失效
标题翻译：新型7β-羟基-4-孕烯-3,20-二酮衍生物及其制备方法
公开(公告)号：US5028722A
公开(公告)日：1991-07-02
申请号：US294567
申请日：1988-09-26
申请人： Makoto Yoshihama , Koji Tamura , Nobuo Miyata , Masamichi Nakakoshi
发明人： Makoto Yoshihama , Koji Tamura , Nobuo Miyata , Masamichi Nakakoshi
IPC分类号： C07J7/00 , C12P33/06 , C12P33/12
CPC分类号： C12P33/06 , C07J7/002 , C07J7/0045
摘要： Novel 7.beta.-hydroxy-4-pregnene-3,20-dione derivatives are disclosed.The group of these compounds has possibility of being utilized as an intermediate for the synthesis of progesterone derivatives having ovulation-inhibiting activity. These compounds themselves have also cell differentiation activity for M1 cells.

8. 发明授权

US06559157B2 Dihydronaphthalene compounds 失效
标题翻译：二氢萘化合物
公开(公告)号：US06559157B2
公开(公告)日：2003-05-06
申请号：US09866179
申请日：2001-05-25
申请人： Rolf Wolfgang Hartmann , Bertil Wachall , Makoto Yoshihama , Masamichi Nakakoshi , Shin Nomoto , Yoshikazu Ikeda
发明人： Rolf Wolfgang Hartmann , Bertil Wachall , Makoto Yoshihama , Masamichi Nakakoshi , Shin Nomoto , Yoshikazu Ikeda
IPC分类号： A61K314409
CPC分类号： C07D233/54 , C07C2602/10 , C07D213/30
摘要： Dihydronaphthalene compounds have excellent 17&agr;-hydroxylase/C17-20-lyase inhibiting activity, thromboxan A2 synthesis inhibiting activity, and aromatase inhibiting activity and are thereby are useful as preventive and/or therapeutic agents for various male sex hormone- and female sex hormone-dependent diseases such as prostate cancer, prostatomegaly, masculinization, breast cancer, mastopathy, uterine cancer, endometriosis, and ovarian cancer, as well as myocardial infarction, angina pectoris, and bronchial asthma.
摘要翻译：二氢萘化合物具有优异的17α-羟化酶/ C17-20-裂解酶抑制活性，血栓素A2合成抑制活性和芳香酶抑制活性，因此可用作各种男性性激素和雌性激素依赖性的预防和/或治疗剂诸如前列腺癌，前列腺肥大，男性化，乳腺癌，乳腺病，子宫癌，子宫内膜异位症和卵巢癌以及心肌梗塞，心绞痛和支气管哮喘的疾病。

9. 发明授权

US5914227A Method for examination of hormone-dependent tumors 失效
标题翻译：激素依赖性肿瘤检查方法
公开(公告)号：US5914227A
公开(公告)日：1999-06-22
申请号：US892291
申请日：1997-07-14
申请人： Junji Nakamura , Makoto Yoshihama
发明人： Junji Nakamura , Makoto Yoshihama
IPC分类号： C12Q1/25 , G01N33/574 , G01N33/74 , C12Q1/00 , C12Q1/02
CPC分类号： G01N33/57407 , C12Q1/25 , G01N33/743
摘要： The invention relates to an examination method of hormone-dependent tissue, more particularly to a method for examining hormone-dependent tumors by culturing a tumor tissue in (a) a control culture medium, (b) a culture medium containing a hormone synthetase substrate, and (c) a culture medium containing a hormone synthetase substrate and a hormone synthetase inhibitor, and determining the relative growth ratios of tumor cells of (b) to (a), and (c) to (a) for diagnosing a tumor as being hormone dependent.This invention provides a method for the simultaneous and easy determination of hormone dependent tumors and the presence of hormone synthetic enzymes. Further, this invention provides a new classification system for tumors and means for indicating medical treatment for a cancer patient.
摘要翻译：本发明涉及激素依赖性组织的检查方法，更具体地，涉及通过在（a）对照培养基中培养肿瘤组织来检查激素依赖性肿瘤的方法，（b）含有激素合成酶底物的培养基，和（c）含有激素合成酶底物和激素合成酶抑制剂的培养基，并确定（b）至（a）和（c）至（a）的肿瘤细胞相对于肿瘤细胞的相对生长比例为激素依赖。本发明提供了用于同时且容易地确定激素依赖性肿瘤和激素合成酶的存在的方法。此外，本发明提供了一种用于肿瘤的新分类系统和用于指示癌症患者的治疗的装置。

10. 发明授权

US5166200A Treatment of endometriosis 失效
标题翻译：治疗子宫内膜异位症
公开(公告)号：US5166200A
公开(公告)日：1992-11-24
申请号：US683647
申请日：1991-04-11
申请人： Nobuaki Fujise , Yasushi Yamashita , Hiroaki Takaoka , Nobuyoshi Honda , Makoto Yoshihama
发明人： Nobuaki Fujise , Yasushi Yamashita , Hiroaki Takaoka , Nobuyoshi Honda , Makoto Yoshihama
IPC分类号： A61K31/565 , A61K31/56 , A61P13/02 , A61P15/00 , C07J1/00
CPC分类号： C07J1/0011
摘要： A remedy for endometriosis comprising, as an active ingredient, 14.alpha.-hydroxy-4-androstene-3,6,17-trione or an ester derivative thereof, can effectively treat endometriosis by the strong aromatase-inhibitory activity without giving serious side effects.

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