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51. 发明授权

US06174891B1 Antipruritic agent 有权
标题翻译：止痒剂
公开(公告)号：US06174891B1
公开(公告)日：2001-01-16
申请号：US09117052
申请日：1998-08-24
申请人： Hiroshi Nagase , Jun Utsumi , Takashi Endoh , Toshiaki Tanaka , Junzo Kamei , Kuniaki Kawamura
发明人： Hiroshi Nagase , Jun Utsumi , Takashi Endoh , Toshiaki Tanaka , Junzo Kamei , Kuniaki Kawamura
IPC分类号： A61K31485
CPC分类号： A61K31/541 , A61K31/40 , A61K31/4025 , A61K31/435 , A61K31/485 , A61K31/5377 , C07D489/00 , C07D489/08
摘要： This invention provides an antipruritic comprising an opiate &kgr; receptor agonist as an effective component, a new morphinan quaternary ammonium salt derivative and a new morphinan-N-oxide derivative which are useful in treating pruritus complicated with some diseases.
摘要翻译：本发明提供了含有鸦片类κ受体激动剂作为有效成分的止痒剂，新的吗啡喃季铵盐衍生物和新的吗啡喃-N-氧化物衍生物，其可用于治疗与某些疾病并发的瘙痒。

52. 发明授权

US6156762A Indolomorphinan derivative and agent for curing and preventing cerebral disorder 失效
标题翻译：吲哚并吗啡喃衍生物和治疗和预防脑病的药剂
公开(公告)号：US6156762A
公开(公告)日：2000-12-05
申请号：US142794
申请日：1998-09-24
申请人： Hiroshi Nagase , Yoshifumi Imamura , Junichi Hirokawa , Susumu Matsuda , Yasushi Miyauchi
发明人： Hiroshi Nagase , Yoshifumi Imamura , Junichi Hirokawa , Susumu Matsuda , Yasushi Miyauchi
IPC分类号： C07D489/00 , C07D491/18 , C07D491/20 , A61K31/485 , C07D489/10
CPC分类号： C07D489/00
摘要： The present invention provides an indolomorphinan derivative or a pharmacologically acceptable acid addition salt thereof, and an agent for curing and preventing cerebral disorders composed of the derivative and salt thereof, which is represented by the following formula (I): ##STR1## [wherein R.sup.1 represents cyclopropylmethyl or the like; R.sup.2 and R.sup.3 each represent hydroxy methoxy, or the like; R.sup.4 represents hydrogen, methyl, benzyl, 3-isothiocyanatopropyl, or the like; and (R.sup.5).sub.m represents hydrogen, substituted benzo, or the like]. The compounds of the present invention have the excellent effect of preventing damage of the cerebral nerve cells. Therefore, the compounds of the present invention are useful as medicines used for curing and preventing various cerebral diseases such as cerebral stroke, traumatic cerebral diseases, cerebral edema, and cerebral neurodegenerative diseases, ameliorating aftereffects thereof, and preventing the recurrence thereof by inhibiting various ischemic, hemorrhagic or traumatic cerebral disorders, and damages of the cerebral nerve cells caused by various nerve degenerations.
摘要翻译： PCT No.PCT / JP98 / 00092 Sec。 371日期：1998年9月24日 102（e）1998年9月24日PCT PCT 1998年1月13日PCT公布。公开号WO98 / 31684 日期：1998年7月23日本发明提供吲哚并吗啡衍生物或其药理学上可接受的酸加成盐，以及由下式（I）表示的由其衍生物和盐组成的脑病的治疗和预防剂：其中R1表示环丙基甲基等; R2和R3各自表示羟基甲氧基等; R4代表氢，甲基，苄基，3-异硫氰基丙基等; 和（R 5）m表示氢，取代的苯并或类似物]。本发明的化合物具有防止脑神经细胞损伤的优异效果。因此，本发明的化合物可用作治疗和预防各种脑疾病如脑中风，创伤性脑病，脑水肿和脑神经变性疾病的药物，改善其后遗症，并通过抑制各种缺血性疾病预防其复发，出血性或创伤性脑病，以及由各种神经变性引起的脑神经细胞损伤。

53. 发明授权

US6087369A Indole derivatives, process for producing the same and medicinal uses of the same 失效
标题翻译：吲哚衍生物，其制备方法和药物用途
公开(公告)号：US6087369A
公开(公告)日：2000-07-11
申请号：US135580
申请日：1998-08-18
申请人： Hiroshi Nagase , Akira Mizusuna , Koji Kawai , Izumi Nakatani
发明人： Hiroshi Nagase , Akira Mizusuna , Koji Kawai , Izumi Nakatani
IPC分类号： A61K31/44 , A61K31/485 , C07D489/10 , C07D491/20 , C07D491/22
CPC分类号： C07D491/20 , C07D491/22
摘要： A novel compound which is a .delta.-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof. The present invention also provides an immunosuppressive agent, antiallergic agent, anti-inflammatory agent and brain cell-protecting agent comprising the derivative or the salt as an effective ingredient.
摘要翻译：公开了具有高选择性和活性的具有免疫抑制作用，抗过敏作用，抗炎作用和脑细胞保护作用的具有高选择性和活性的δ-阿片拮抗剂的新型化合物。根据本发明的化合物是由式（I）表示的吲哚衍生物：及其药学上可接受的酸加成盐。本发明还提供了包含该衍生物或盐作为有效成分的免疫抑制剂，抗过敏剂，抗炎剂和脑细胞保护剂。

54. 发明授权

US5852030A Indole derivatives, process for producing the same and medicinal uses of the same 失效
标题翻译：吲哚衍生物，其制备方法和药物用途
公开(公告)号：US5852030A
公开(公告)日：1998-12-22
申请号：US709835
申请日：1996-09-10
申请人： Hiroshi Nagase , Akira Mizusuna , Koji Kawai , Izumi Nakatani
发明人： Hiroshi Nagase , Akira Mizusuna , Koji Kawai , Izumi Nakatani
IPC分类号： C07D491/20 , C07D491/22 , C07D489/10 , A61K31/485
CPC分类号： C07D491/20 , C07D491/22
摘要： A novel compound which is a .delta.-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof. The present invention also provides an immunosuppressive agent, antiallergic agent, anti-inflammatory agent and brain cell-protecting agent comprising the derivative or the salt as an effective ingredient.
摘要翻译：公开了具有高选择性和活性的具有免疫抑制作用，抗过敏作用，抗炎作用和脑细胞保护作用的具有高选择性和活性的δ-阿片拮抗剂的新型化合物。根据本发明的化合物是由式（I）表示的吲哚衍生物：其药学上可接受的酸加成盐。本发明还提供了包含该衍生物或盐作为有效成分的免疫抑制剂，抗过敏剂，抗炎剂和脑细胞保护剂。

55. 发明授权

US5776945A 4A-aryldecahydroisoquinoline compound and medicinal use of the same 失效
标题翻译： 4A-芳基十氢异喹啉化合物及其药用
公开(公告)号：US5776945A
公开(公告)日：1998-07-07
申请号：US809226
申请日：1997-05-08
申请人： Hiroshi Nagase , Yoshifumi Imamura , Hiroshi Ohno , Takashi Endo
发明人： Hiroshi Nagase , Yoshifumi Imamura , Hiroshi Ohno , Takashi Endo
IPC分类号： C07D217/16 , C07D405/12 , C07D217/04 , A61K31/46
CPC分类号： C07D405/12 , C07D217/16
摘要： The present invention relates to a 4a-aryldecahydroisoquinoline compound, which is represented by a compound 1, or a pharmacologically acceptable salt thereof. ##STR1## As the results of in vitro and in vivo pharmacological evaluations, it was found that the compounds of the present invention had excellent preventive effects on ischemic death of cerebral neurocytes, suppressive effects on development of cerebral infarction, and strong analgesic and antitussive effects; therefore the compounds of the present invention can be utilized in the medicinal field as a useful cerebral cytoprotective agent, which is aimed at preventing and treating cerebrovascular disorder, ischemic cerebral disorder, cerebral neurocyte disorder, and dementia, an analgesic, and an antitussive.
摘要翻译： PCT No.PCT / JP96 / 02030 Sec。 371日期：1997年5月8日 102（e）日期1997年5月8日PCT PCT 1996年7月19日PCT公布。公开号WO97 / 03968 日期：1997年2月6日本发明涉及由化合物1表示的4a-芳基十氢异喹啉化合物或其药理学上可接受的盐。作为体外和体内药理学评价的结果，发现本发明的化合物对脑神经细胞的缺血性死亡具有优异的预防作用，对脑梗死发展的抑制作用以及强镇痛和镇咳药效果; 因此，本发明的化合物可用作药用领域，作为有用的脑细胞保护剂，其旨在预防和治疗脑血管障碍，缺血性脑病，脑神经细胞病和痴呆，镇痛药和镇咳药。

56. 发明授权

US5420310A Conversion of 15-beta to 15-alpha 5,6,7-trinor-4,8-inter-m-phenylene PGI2 derivatives 失效
标题翻译： 15-β至15-α5,6,7-三硝基-4,8-间 - 间 - 亚苯基PGI 2衍生物的转化
公开(公告)号：US5420310A
公开(公告)日：1995-05-30
申请号：US957357
申请日：1992-11-20
申请人： Kiyotaka Ohno , Hiroshi Nagase , Yutaka Hosono , Hisanori Wakita , Koji Kawai , Hideo Yoshiwara
发明人： Kiyotaka Ohno , Hiroshi Nagase , Yutaka Hosono , Hisanori Wakita , Koji Kawai , Hideo Yoshiwara
IPC分类号： C07D307/93 , A61K31/557 , A61P7/02 , C07C41/16 , C07C43/247 , C07D20060101 , C07D307/92
CPC分类号： C07C43/247 , C07D307/93 , C07C2101/10
摘要： The present invention provides a process for preparing 5,6,7-trinor-4,8-inter-m-phenylene PGI.sub.2 derivative using 3a,8b-cis-dihydro-3H-5,7-dibromocyclopenta[b]benzofuran as a starting material, as well as compounds which are intermediates.
摘要翻译：本发明提供了使用3a，8b-顺 - 二氢-3H-5,7-二溴环戊二烯并[b]苯并呋喃作为起始物制备5,6,7-三硝基-4,8-间 - 间 - 亚苯基PGI 2衍生物的方法材料，以及作为中间体的化合物。

57. 发明授权

US5202447A Process of producing 5,6,7-trinor-4,8-inter-m-phenylene PGI2 derivatives 失效
标题翻译：生产5,6,7-三硝基-4,8-间 - 间苯二酚PGI2衍生物的方法
公开(公告)号：US5202447A
公开(公告)日：1993-04-13
申请号：US601783
申请日：1991-01-02
申请人： Kiyotaka Ohno , Hiroshi Nagase , Yutaka Hosono , Hisanori Wakita , Koji Kawai , Hideo Yoshiwara
发明人： Kiyotaka Ohno , Hiroshi Nagase , Yutaka Hosono , Hisanori Wakita , Koji Kawai , Hideo Yoshiwara
IPC分类号： C07D307/93 , A61K31/557 , A61P7/02 , C07C41/16 , C07C43/247 , C07D20060101
CPC分类号： C07C43/247 , C07D307/93 , C07C2101/10
摘要： The present invention provides a process for preparing 5,6,7-trinor-4,8-inter-m-phenylene PGI.sub.2 derivative [VII] using 3a,8b-cis-dihydro-3H-5,7-dibromocyclopenta[b]benzofuran (1) as a starting material, as well as compounds of the formulae (8) and (11) which are intermediates for the preparation of the compound of the formula (1). ##STR1##
摘要翻译： PCT No.PCT / JP90 / 00237 Sec。 371日期1991年1月2日 102（e）日期1991年1月2日PCT提交1990年2月27日PCT公布。 WO90 / 10003 PCT出版物 1990年9月7日，本发明提供了使用3a，8b-顺式 - 二氢-3H-5，制备5,6,7-三硝基-4,8-间 - 间 - 亚苯基PGI 2衍生物[Ⅶ] 作为原料的7-二溴环戊并[b]苯并呋喃（1），以及作为制备式（1）化合物的中间体的式（8）和（11）的化合物。 + TR

58. 发明授权

US5085806A Conductive material and process for preparing the same 失效
标题翻译：导电材料及其制备方法
公开(公告)号：US5085806A
公开(公告)日：1992-02-04
申请号：US319307
申请日：1989-03-06
申请人： Yoshiyuki Yasutomi , Tadahiko Miyoshi , Masahisa Sobue , Nobuyuki Yamashita , Hiroshi Nagase , Kiyohiko Tanno , Shoji Arimoto , Fumio Jooraku
发明人： Yoshiyuki Yasutomi , Tadahiko Miyoshi , Masahisa Sobue , Nobuyuki Yamashita , Hiroshi Nagase , Kiyohiko Tanno , Shoji Arimoto , Fumio Jooraku
IPC分类号： C04B35/584 , C04B35/58 , C04B35/581 , C04B35/65
CPC分类号： C04B35/58042 , C04B35/5156 , C04B35/5158 , C04B35/58 , C04B35/58007 , C04B35/58014 , C04B35/58028 , C04B35/581 , C04B35/584 , C04B35/6303 , C04B35/632 , C04B35/63408 , C04B35/645 , C04B35/65 , C04B35/806
摘要： The invention provides a conductor comprising a reaction-sintered body of a conductive nitride produced from a powder of at least one metal selected from Ti, Zr, V, Nb, Ta, Cr, Ce, Co, Mn, Hf, W, Mo, Fe, Pr, Nd, Sm, Eu, Gd, Tb, Dy, Ho, Yb, Lu, Th and Ni, and a process for producing such conductor by heating a molding containing a metal powder in a nitriding gaseous atmosphere containing no CO gas.

59. 发明授权

US4965504A Control apparatus for inverter for driving AC motor 失效
标题翻译：用于驱动交流电动机的逆变器控制装置
公开(公告)号：US4965504A
公开(公告)日：1990-10-23
申请号：US406516
申请日：1989-09-13
申请人： Shigeta Ueda , Kazuo Honda , Takashi Ikimi , Toshihiko Matsuda , Hiroshi Nagase , Nobuyoshi Mutoh
发明人： Shigeta Ueda , Kazuo Honda , Takashi Ikimi , Toshihiko Matsuda , Hiroshi Nagase , Nobuyoshi Mutoh
IPC分类号： H02M7/5387
CPC分类号： H02M7/53873 , H02M2007/53876
摘要： A control apparatus for controlling a PWM inverter, the PWM inverter receiving AC power and generating an AC output having a controlled frequency to be supplied to an AC motor, comprises a circuit for generating, on the basis of a given running command, a PWM signal controlling the inverter with a given sampling period, and a circuit for controlling the PWM signal generating circuit, whereby the AC motor generates an electromagnetic tone preselected so as to correspond to desired information when the AC motor is driven by output of the inverter controlled by the PWM signal. The above described desired information may be information representing the running state of the motor or selected music.

60. 发明授权

US4524186A Process for producing water-absorbing resins 失效
标题翻译：生产吸水树脂的方法
公开(公告)号：US4524186A
公开(公告)日：1985-06-18
申请号：US517838
申请日：1983-07-27
申请人： Hiroshi Nagase
发明人： Hiroshi Nagase
IPC分类号： C08J3/00 , C08F8/12 , C08F220/10
CPC分类号： C08F8/12
摘要： A process for producing an absorbent resin, which comprises polymerizing 1 mole of a lower alkyl acrylate and 0.07 to 0.5 mole of a polyhydric alcohol ester of a monoethylenically unsaturated carboxylic acid in an aqueous medium in the absence of an emulsifying agent, saponifying the resulting polymer with a basic substance in a water-lower alcohol medium, and then neutalizing the saponification product with an acid.
摘要翻译：一种制造吸收性树脂的方法，其包括在不存在乳化剂的情况下，在水性介质中聚合1摩尔丙烯酸低级烷基酯和0.07至0.5摩尔单烯属不饱和羧酸的多元醇酯，将所得聚合物皂化在水 - 低级醇介质中使用碱性物质，然后用酸中和皂化产物。

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