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1. 发明授权

US5712306A Physiologically active substances PF1092A, PF1092B and PF1092C, and contraceptives and anticancer drugs containing the same as active ingredients 失效
标题翻译：生理活性物质PF1092A，PF1092B和PF1092C，以及与活性成分相同的避孕药和抗癌药
公开(公告)号：US5712306A
公开(公告)日：1998-01-27
申请号：US585411
申请日：1996-01-11
申请人： Yuji Tabata , Masahiro Hatsu , Naoko Miike , Takashi Yaguchi , Ayako Someya , Yasushi Kurata
发明人： Yuji Tabata , Masahiro Hatsu , Naoko Miike , Takashi Yaguchi , Ayako Someya , Yasushi Kurata
IPC分类号： C07D307/92 , A61K31/34 , C07D307/77
CPC分类号： C07D307/92
摘要： This invention provides novel physiologically active substances PF1092A, PF1092B and PF1092C, which can inhibit binding of progesterone to progesterone receptor. These substances were obtained by culturing a fungal microorganism belonging to the genus Penicillium using a medium containing ordinary nutrients for microorganisms and isolating the physiologically active substances PF1092A, PF1092B and PF1092C from the resulting culture mixture by means of solvent extraction, silica gel column chromatography, and the like. Molecular formulae of the novel physiologically active substances PF1092A, PF1092B and PF1092C are C.sub.17 H.sub.20 O.sub.5, C.sub.17 H.sub.20 O.sub.5 and C.sub.15 H.sub.18 O.sub.4, respectively.
摘要翻译：本发明提供新的生理活性物质PF1092A，PF1092B和PF1092C，其可以抑制孕酮与孕酮受体的结合。这些物质通过使用含有微生物的普通营养素的培养基培养属于青霉属的真菌微生物并通过溶剂萃取，硅胶柱色谱和从所得培养物中分离生理活性物质PF1092A，PF1092B和PF1092C而得到。类似。新型生理活性物质PF1092A，PF1092B和PF1092C的分子式分别为C17H20O5，C17H20O5和C15H18O4。

2. 发明授权

US5789602A Physiologically active substances PF1092A, PF1092B and PF1092C, process for the production thereof, and contraceptives and anticancer drugs containing the same as active ingredients 失效
标题翻译：生理活性物质PF1092A，PF1092B和PF1092C，其生产方法和含有与活性成分相同的避孕药和抗癌药
公开(公告)号：US5789602A
公开(公告)日：1998-08-04
申请号：US925709
申请日：1997-09-09
申请人： Yuji Tabata , Masahiro Hatsu , Naoko Miike , Takashi Yaguchi , Ayako Someya , Yasushi Kurata
发明人： Yuji Tabata , Masahiro Hatsu , Naoko Miike , Takashi Yaguchi , Ayako Someya , Yasushi Kurata
IPC分类号： C07D307/92 , C07D307/77
CPC分类号： C07D307/92
摘要： This invention provides novel physiologically active substances PF1092A, PF1092B and PF1092C, which can inhibit binding of progesterone to progesterone receptor. These substances were obtained by culturing a fungal microorganism belonging to the genus Penicillium using a medium containing ordinary nutrients for microorganisms and isolating the physiologically active substances PF1092A, PF1092B and PF1092C from the resulting culture mixture by means of solvent extraction, silica gel column chromatography, and the like. Molecular formulae of the novel physiologically active substances PF1092A, PF1092B and PF1092C are C.sub.17 H.sub.20 O.sub.5, C.sub.17 H.sub.20 O.sub.5 and C.sub.15 H.sub.18 O.sub.4, respectively.
摘要翻译：本发明提供新的生理活性物质PF1092A，PF1092B和PF1092C，其可以抑制孕酮与孕酮受体的结合。这些物质通过使用含有微生物的普通营养素的培养基培养属于青霉属的真菌微生物并通过溶剂萃取，硅胶柱色谱和从所得培养物中分离生理活性物质PF1092A，PF1092B和PF1092C而得到。类似。新型生理活性物质PF1092A，PF1092B和PF1092C的分子式分别为C17H20O5，C17H20O5和C15H18O4。

3. 发明授权

US6077840A Tetrahydrobenzindolone derivatives 有权
标题翻译：四氢苯并吲哚酮衍生物
公开(公告)号：US6077840A
公开(公告)日：2000-06-20
申请号：US331294
申请日：1999-06-18
申请人： Kenichi Kurihara , Rie Shinei , Yasushi Kurata , Yuji Tabata , Kiyoshi Tanabe , Tsuneo Okonogi
发明人： Kenichi Kurihara , Rie Shinei , Yasushi Kurata , Yuji Tabata , Kiyoshi Tanabe , Tsuneo Okonogi
IPC分类号： C07D209/60 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D521/00 , A61K31/535 , A61K31/40 , A61K31/44 , A61K31/50 , C07D233/02
CPC分类号： C07D231/12 , C07D209/60 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof and a process for producing the same are disclosed. The compounds have progesterone receptor binding inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for hysteromyoma, endometriosis, meningioma, and myeloma, abortifacients, oral contraceptive pills, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance. ##STR1## wherein R.sup.1 represents alkyl or aralkyl; R.sup.2 represents a hydrogen atom, alkylcarbonyl, cycloalkylcarbonyl, aromatic acyl, heteroaromatic acyl, saturated heterocyclic acyl, alkyl, alkenyl, aralkyl, carbamoyl, alkylcarbamoyl, aromatic carbamoyl, aralkylcarbamoyl, alkylaminocarbonyl, cycloalkylcarbamoyl, alkoxycarbonyl, aryloxycarbonyl, heteroaromatic thiocarbonyl, saturated heterocyclic thiocarbonyl, or alkyl-thiocarbamoyl: and R.sup.3 represents a hydrogen atom, a hydroxyl group, alkyloxy, alkylcarbonyloxy, alkylthio, or arylthio.
摘要翻译： PCT No.PCT / JP97 / 04683 Sec。 371日期：1999年6月18日 102（e）1999年6月18日PCT 1997年12月18日PCT公布。第WO98 / 27059号公报日期：1998年6月25日公开了由下式（I）表示的化合物或其药学上可接受的盐及其制备方法。所述化合物具有孕酮受体结合抑制活性，因此可用作孕酮相关疾病的治疗和预防剂。具体地说，它们可用作乳腺癌和卵巢癌的制癌剂，子宫肌瘤，子宫内膜异位症，脑膜瘤和骨髓瘤的治疗剂，流产者，口服避孕药以及用于骨质疏松和更年期障碍的治疗和预防剂。其中R1表示烷基或芳烷基; R 2表示氢原子，烷基羰基，环烷基羰基，芳香族酰基，杂芳基酰基，饱和杂环酰基，烷基，烯基，芳烷基，氨基甲酰基，烷基氨基甲酰基，芳香族氨基甲酰基，芳烷基氨基甲酰基，烷基氨基羰基，环烷基氨基甲酰基，烷氧基羰基，芳氧基羰基，杂芳硫基羰基，饱和杂环硫代羰基，或烷基 - 硫代氨基甲酰基：和R3表示氢原子，羟基，烷氧基，烷基羰氧基，烷硫基或芳硫基。

4. 发明授权

US6111658A Dither method and printing apparatus 失效
标题翻译：抖动方式和打印装置
公开(公告)号：US6111658A
公开(公告)日：2000-08-29
申请号：US986808
申请日：1997-12-08
申请人： Yuji Tabata
发明人： Yuji Tabata
IPC分类号： B41J2/52 , B41J2/525 , G06F3/12 , G06K15/12 , H04N1/405 , H04N1/52
CPC分类号： G06K15/128 , H04N1/4051 , G06K2215/0094
摘要： A ROM in the control circuit of a color printer stores a threshold matrix. The individual elements of the threshold matrix correspond to print dots, the number of which is X.times.Y and which form 1 pixel in the original image. Values t (x, y) which are integral numbers not less than 0 are assigned one to each of the individual elements in a predetermined order. Using the threshold matrix, the CPU of the control circuit creates mask patterns for representing halftones. A value of 1 is subtracted from the tone number allotted to the tone of color of a pixel in an image to be printed, and the resultant value is substituted for a variable G. When a gradation for image data representing the pixel is given as "g", the condition required for setting ON (transferring toner to print) the dot specified by the coordinates (x, y) in the pixel in the case of the gradation "g" is expressed by the following formula (6):t (x, y).ltoreq.g.times.X.times.Y/G (6)Based on the threshold matrix and the formula (6), the CPU of the control section creates mask patterns in the case where the gradation "g" takes values 0 to G-1 in sequence, and develops those mask patterns in a RAM.
摘要翻译：彩色打印机的控制电路中的ROM存储阈值矩阵。阈值矩阵的各个元素对应于打印点，其数量为XxY，并且在原始图像中形成1个像素。作为不小于0的整数的值t（x，y）以预定顺序分配给每个单独元件1。使用阈值矩阵，控制电路的CPU创建用于表示半色调的掩模图案。从分配给要打印的图像中的像素的色调的色调数字中减去值1，并将结果值替换为变量G.当表示像素的图像数据的灰度被给定为“ g“时，在灰度”g“的情况下，将由像素中的坐标（x，y）指定的点所指定的ON（转印墨粉打印）所需的条件用下式（6）表示：t（（6）基于阈值矩阵和公式（6），控制部分的CPU在灰度“g”取0到G-1的情况下创建掩模图案并且在RAM中开发出这些掩模图案。

5. 发明授权

US06255339B1 Tetrahydronaphthofuranone derivatives and process for producing the same 失效
标题翻译：四氢萘并呋喃酮衍生物及其制备方法
公开(公告)号：US06255339B1
公开(公告)日：2001-07-03
申请号：US09117070
申请日：1998-07-21
申请人： Kenichi Kurihara , Rie Shinei , Kiyoshi Tanabe , Yasuo Yamamoto , Keiichi Ajito , Kaori Miyajima , Yuji Tabata , Shohei Yasuda , Kuniaki Tatsuta , Tsuneo Okonogi
发明人： Kenichi Kurihara , Rie Shinei , Kiyoshi Tanabe , Yasuo Yamamoto , Keiichi Ajito , Kaori Miyajima , Yuji Tabata , Shohei Yasuda , Kuniaki Tatsuta , Tsuneo Okonogi
IPC分类号： A61K3134
CPC分类号： C07D307/92 , C07D407/12 , C07D407/14 , C07D409/12 , C07D417/12
摘要： Compounds represented by the following formula (I) and pharmaceutically acceptable salts thereof are disclosed. The compounds have progesterone receptor binding inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as abortifacients, oral contraceptive pills, carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for endometriosis, meningioma, and myeloma, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance. wherein R1 and R2 represent a hydroxyl group, alkyloxy, alkenyloxy, alkynyloxy, cycloalkyloxy, alkoxyalkyloxy, cycloalkyloxy containig one oxygen atom, aralkyloxy, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, cycloalkylcarbonyloxy, alkoxycarbonyloxy, aryloxy carbonyloxy, aralkylcarbonyloxy, aromatic acyloxy, heteroaromatic acyloxy, saturated heterocyclic carbonyloxy, alkylsulfonyloxy, aromatic sulfonyloxy, alkylcarbamoyloxy, aromatic carbamoyloxy, alkylcarbonylamino, or aromatic acylamino, provided that R1 may further represent a hydrogen atom, alkyl, alkenyl, or alkynyl; and R3, R4, and R5 each independently represent a hydrogen atom, alkyl or alkenyl.
摘要翻译：公开了由下式（I）表示的化合物及其药学上可接受的盐。所述化合物具有孕酮受体结合抑制活性，因此可用作孕酮相关疾病的治疗和预防剂。具体地说，它们可用作流产者，口服避孕药，乳腺癌和卵巢癌的制癌剂，子宫内膜异位症的治疗剂，脑膜瘤和骨髓瘤，以及骨质疏松症和更年期障碍的治疗和预防剂。其中R1和R2表示羟基，烷氧基，链烯氧基，炔氧基，环烷氧基，烷氧基烷氧基，含有一个氧原子的环烷氧基，芳烷氧基，烷基羰基氧基，链烯基羰基氧基，炔基羰氧基，环烷基羰基氧基，烷氧基羰基氧基，芳氧基羰基氧基，芳烷基羰基氧基，芳香酰氧基，杂芳基酰氧基，饱和杂环羰氧基，烷基磺酰氧基，芳香磺酰氧基，烷基氨基甲酰氧基，芳族氨基甲酰氧基，烷基羰基氨基或芳族酰氨基，条件是R 1可以进一步代表氢原子，烷基，烯基或炔基; 并且R 3，R 4和R 5各自独立地表示氢原子，烷基或链烯基。

6. 发明授权

US06713473B1 Tricyclic compounds 失效
标题翻译：三环化合物
公开(公告)号：US06713473B1
公开(公告)日：2004-03-30
申请号：US09926355
申请日：2002-02-19
申请人： Naoyuki Nishikawa , Masaharu Sugai , Kozo Aoki , Makoto Suzuki , Akihiko Ikegawa , Kazunobu Takahashi , Fukuichi Ohsawa , Naomi Masuda , Nobukazu Kakui , Jiro Tanaka , Yuji Tabata , Kenji Asai
发明人： Naoyuki Nishikawa , Masaharu Sugai , Kozo Aoki , Makoto Suzuki , Akihiko Ikegawa , Kazunobu Takahashi , Fukuichi Ohsawa , Naomi Masuda , Nobukazu Kakui , Jiro Tanaka , Yuji Tabata , Kenji Asai
IPC分类号： A61K31403
CPC分类号： C07D231/12 , A61K31/403 , A61K31/4035 , A61K31/41 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/675 , C07D209/88 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07F9/5728 , C09B57/00
摘要： A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents —NR3—CO—, —CO—NR3— and the like (R3 represents a hydrogen atom, a lower alkyl group, a lower acyl group and the like); M represents an alkylene linking group (a carbon atom constituting the carbon chain may be replaced with a nitrogen atom, an oxygen atom and the like); X represents —S—, —O—, —NR4—, —NR5—CO— and the like (R4 and R5 represent a hydrogen atom, a lower alkyl group and the like) or a single bond; Y represents an alkyl group, an aryl group, an amino group, an aromatic heterocyclic group and the like; R1 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group or a lower acyl group; and R21, R22 and R23 represent a hydrogen atom, a hydroxyl group, a lower alkyl group and the like] or a salt thereof. The compound is useful as an active ingredient of medicaments for diseases in which neuropeptide Y is involved, ingestion control for hyperphagia and the like.
摘要翻译：由式（I）表示的化合物[A表示5-至7-元烃环基团; L代表-NR 3 -CO - ， - CO-NR 3 - 等（R 3表示氢原子，低级烷基，低级酰基等）。 M表示亚烷基连接基（构成碳链的碳原子可以被氮原子，氧原子等取代）; X表示-S - ， - O - ，-NR 4 - ， - NR 5 -CO-等（R 4和R 5表示氢原子，低级烷基等））或单一债券; Y表示烷基，芳基，氨基，芳香族杂环基等; R 1表示低级烷基，低级烯基，低级炔基或低级酰基; R 21，R 22和R 23表示氢原子，羟基，低级烷基等〕或其盐。该化合物可用作其中涉及神经肽Y的疾病的药物的活性成分，用于食欲摄入的摄取控制等。

7. 发明授权

US5817816A Sesquiterpene derivatives having progesterone receptor binding inhibitory activity 失效
标题翻译：具有孕激素受体结合抑制活性的倍半萜衍生物
公开(公告)号：US5817816A
公开(公告)日：1998-10-06
申请号：US878841
申请日：1997-06-19
申请人： Kenzo Harimaya , Emiko Magome , Yuji Tabata , Toru Sasaki
发明人： Kenzo Harimaya , Emiko Magome , Yuji Tabata , Toru Sasaki
IPC分类号： C07C69/738 , C07D303/48 , C07D307/92 , A61K31/365
CPC分类号： C07D307/92 , C07C69/738 , C07D303/48
摘要： Sesquiterpene derivatives, represented by the following formulae (I) and (II), having progesterone receptor binding inhibitory activity are disclosed. They can be used as therapeutic and prophylactic agents for progesterone-related diseases, for example, as a carcinostatic agent for breast cancer or ovarian cancer, a therapeutic agent for hysteromyoma, endometriosis, meningioma, or myeloma, an abortifacient, an oral contraceptive pill, or a therapeutic or prophylactic agent for osteoporosis or climacteric disturbance. These compounds have no steroid skeleton and, hence, are considered to be advantageously free from side effect inherent in steroid such as found in conventional progesterone receptor binding inhibitors having a steroid skeleton. ##STR1## wherein R.sup.1 represents a hydrogen atom, a halogen atom, C.sub.1 -C.sub.5 alkoxy, or phenylthio; R.sup.2 represents C.sub.1 -C.sub.5 alkoxy or C.sub.2 -C.sub.5 alkanoyloxy; and ---- with letters a, b, c, d, and e attached thereto represent a double bond or a single bond; R.sup.3 has the same meaning as R.sup.2 ; and R.sup.4 represents C.sub.1 -C.sub.5 alkoxy.
摘要翻译：公开了具有孕酮受体结合抑制活性的由下式（I）和（II）表示的倍半萜衍生物。它们可以用作孕激素相关疾病的治疗和预防剂，例如作为乳腺癌或卵巢癌的制癌剂，子宫肌瘤，子宫内膜异位症，脑膜瘤或骨髓瘤的治疗剂，流产者，口服避孕药，或用于骨质疏松症或更年期障碍的治疗或预防剂。这些化合物没有类固醇骨架，因此被认为有利地不含类固醇中固有的副作用，例如在具有类固醇骨架的常规孕酮受体结合抑制剂中发现。（Ⅰ）其中R1表示氢原子，卤素原子，C1-C5烷氧基或苯硫基; R2代表C1-C5烷氧基或C2-C5烷酰氧基; 和+ E，uns ---- + EE与字母a，b，c，d和e表示双键或单键; R3与R2具有相同的含义; R4表示C1-C5烷氧基。

8. 发明授权

US09018507B2 Musical instrument that generates electronic sound, light-emission controller used in this musical instrument, and control method of musical instrument 有权
标题翻译：产生电子音乐的乐器，本乐器使用的发光控制器以及乐器的控制方法
公开(公告)号：US09018507B2
公开(公告)日：2015-04-28
申请号：US13590690
申请日：2012-08-21
申请人： Yuji Tabata
发明人： Yuji Tabata
IPC分类号： G10H3/06 , G10H1/00
CPC分类号： G10H1/0008 , G10H2220/061 , G10H2220/185 , G10H2220/201 , G10H2220/395 , G10H2220/455
摘要： A musical instrument (1) includes a stick (10) to be held by a player and provided with a marker (15) at a leading end that emits light and switches off; a camera unit (20) that captures an image of the player holding the stick (10); and a center unit (30) that generates a percussion instrument sound based on a position of the marker (15) while emitting light in image-capture space captured by the camera unit (20), in which the stick (10) causes the marker (15) to emit light under the condition of detecting start of a down swing movement by the player, and causes the marker (15) to switch off under the condition of detecting the end of this movement.
摘要翻译：乐器（1）包括由玩家保持的杆（10），并在发光并切断的前端设置有标记（15）; 拍摄保持棒（10）的玩家的图像的相机单元（20）; 以及中心单元（30），其在基于所述标记（15）的位置产生打击乐器声音，同时在由所述照相机单元（20）捕获的图像捕获空间中发射光，其中所述杆（10）使所述标记（15）在检测到游戏者的向下摆动运动的开始的状态下发光，并且在检测到该移动结束的条件下使标记（15）关闭。

9. 发明授权

US08889727B2 Topical antifungal agent 有权
标题翻译：局部抗真菌剂
公开(公告)号：US08889727B2
公开(公告)日：2014-11-18
申请号：US13982734
申请日：2012-01-30
申请人： Makoto Ohyama , Yuji Tabata , Maiko Iida , Kaori Kaneda , Sho Takahata
发明人： Makoto Ohyama , Yuji Tabata , Maiko Iida , Kaori Kaneda , Sho Takahata
IPC分类号： A61K31/415 , C07D231/10 , C07D207/32 , C07D231/12 , C07D231/14 , C07D231/22 , C07D207/34 , C07D207/36
CPC分类号： C07D207/32 , A61K31/415 , C07D207/34 , C07D207/36 , C07D231/12 , C07D231/14 , C07D231/22
摘要： An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is provided
摘要翻译：提供了一种抗真菌剂，其包含作为活性成分的具有由下式（I）或（II）表示的2-（1H-吡唑-1-基）苯酚骨架的化合物或其盐，

10. 发明申请

US20130317074A1 TOPICAL ANTIFUNGAL AGENT 有权
标题翻译：局部抗真菌药物
公开(公告)号：US20130317074A1
公开(公告)日：2013-11-28
申请号：US13982734
申请日：2012-01-30
申请人： Makoto Ohyama , Yuji Tabata , Maiko Iida , Kaori Kaneda , Sho Takahata
发明人： Makoto Ohyama , Yuji Tabata , Maiko Iida , Kaori Kaneda , Sho Takahata
IPC分类号： C07D207/32 , C07D207/34 , C07D207/36
CPC分类号： C07D207/32 , A61K31/415 , C07D207/34 , C07D207/36 , C07D231/12 , C07D231/14 , C07D231/22
摘要： An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is provided
摘要翻译：提供了一种抗真菌剂，其包含作为活性成分的具有由下式（I）或（II）表示的2-（1H-吡唑-1-基）苯酚骨架的化合物或其盐，

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