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81. 发明申请

WO1996004914A1 TRIAZINE DERIVATIVE AND MEDICINE 审中-公开
公开(公告)号：WO1996004914A1
公开(公告)日：1996-02-22
申请号：PCT/JP1995001577
申请日：1995-08-08
申请人： NIPPON SHINYAKU CO., LTD. , UEDA, Fusao , OZAKI, Takayuki , NAKAMURA, Ken-ichi
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： A61K31/53
CPC分类号： A61K31/541 , A61K31/53 , A61K31/5377 , A61K31/55
摘要： A medicine containing as the active ingredient a triazine derivative represented by general formula (I), a solvate thereof, or a salt thereof and being useful as a hepatitis remedy, wherein R and R represent each independently hydrogen or (un)substituted alkyl, aralkyl or alkenyl, or NR R represents a cyclic amino group which may bear, in addition to the pertinent nitrogen atom, nitrogen, oxygen or sulfur as the ring atom and may be substituted, provided the case where NR R represents NH2 is excluded.
摘要翻译：含有作为活性成分的由通式（I）表示的三嗪衍生物，其溶剂化物或其盐，可用作肝炎药物的药物，其中R 1和R 2各自独立地表示氢或（未取代的烷基，芳烷基或链烯基，或NR 1 R 2表示除了相关的氮原子外还可以含有氮，氧或硫作为环原子并且可被取代的环状氨基，排除NR 1 R 2表示NH 2的情况。

82. 发明申请

WO1996004371A1 TISSUE PLASMINOGEN ACTIVATOR DIMER 审中-公开
标题翻译：组织等离子激活剂二聚体
公开(公告)号：WO1996004371A1
公开(公告)日：1996-02-15
申请号：PCT/JP1995001541
申请日：1995-08-03
申请人： NIPPON SHINYAKU CO., LTD. , MORI, Kazuya
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C12N09/64
CPC分类号： C12N9/6459 , C12Y304/21069
摘要： A novel tissue plasminogen activator dimer having a high fibrinolytic activity and a remarkably lowered antigenicity.
摘要翻译：具有高纤维蛋白溶解活性和显着降低的抗原性的新型组织纤溶酶原激活物二聚体。

83. 发明申请

WO1996000236A1 TRITERPENE DERIVATIVE AND MEDICINAL COMPOSITION 审中-公开
标题翻译： TRITERPENE衍生物和药物组合物
公开(公告)号：WO1996000236A1
公开(公告)日：1996-01-04
申请号：PCT/JP1995001249
申请日：1995-06-22
申请人： NIPPON SHINYAKU CO., LTD. , OHGI, Tadaaki , YOSHIFUSA, Hiroto , KANDORI, Kazuhisa
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07J63/00
CPC分类号： C07J63/008 , C07J71/0005
摘要： Hederagenin derivatives represented by general formula (1) and pharmaceutically acceptable salts thereof, and a medicinal composition containing the same as the active ingredient and being efficacious in treating nephritis, wherein R represents OR or NR R , and R and R represent each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl or optionally substituted heteroaryl; R and R represent each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted acyl, optionally substituted monoalkylcarbamoyl, optionally substituted dialkylcarbamoyl or optionally substituted alkoxycarbonyl, or alternatively R and R are combined together to represent carbonyl.
摘要翻译：由通式（1）表示的上皮原素衍生物及其药学上可接受的盐，以及含有与活性成分相同的有效治疗肾炎的药物组合物，其中R 1表示OR 11或NR 11 R R 11和R 12各自独立地表示氢，任选取代的烷基，任选取代的环烷基，任选取代的烯基，任选取代的炔基，任选取代的芳基或任选取代的杂芳基; R 2和R 3各自独立地表示氢，任选取代的烷基，任选取代的环烷基，任选取代的烯基，任选取代的炔基，任选取代的酰基，任选取代的单烷基氨基甲酰基，任选取代的二烷基氨基甲酰基或任选取代的烷氧羰基， 2>和R 3结合在一起代表羰基。

84. 发明申请

WO1995027699A1 AMINOSTILBAZOLE DERIVATIVE AND MEDICINE 审中-公开
标题翻译：氨基噻唑衍生物和药物
公开(公告)号：WO1995027699A1
公开(公告)日：1995-10-19
申请号：PCT/JP1995000658
申请日：1995-04-05
申请人： NIPPON SHINYAKU CO., LTD. , HIDAKA, Hiroyoshi , MATSUURA, Akira , MATSUDA, Masato
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07D213/42
CPC分类号： C07D213/42 , A61K31/44 , C07D213/76 , C07D213/89 , C07D239/26 , C07D241/12 , C07D405/06
摘要： An aminostilbazole derivative represented by general formula (I) or a hydrate and a salt thereof, useful for treating various types of malignant tumor. In said formula R and R represent each hydrogen, etc.; R , R , R and R represent each hydrogen, C1-C3 acyl, halogen, hydroxy, etc.; R represents hydrogen, hydroxylated C1-C3 alkyl, etc.; R represents C1-C3-alkoxy-substituted benzenesulfonyl, etc.; ring Y represents phenyl, etc.; and ring Z represents 4-pyridyl, and oxide thereof, etc.
摘要翻译：由通式（I）表示的氨基芪衍生物或其水合物及其盐，可用于治疗各种恶性肿瘤。在所述式中，R 1和R 2代表每个氢等; R 3，R 4，R 13和R 14各自代表氢，C 1 -C 3酰基，卤素，羟基等; R 5表示氢，羟基化的C 1 -C 3烷基等; R 6表示C 1 -C 3烷氧基取代的苯磺酰基等。环Y表示苯基等; 环Z表示4-吡啶基及其氧化物等

85. 发明申请

WO1995013794A1 PROCESS FOR PRODUCING STABLE MEDICINAL COMPOSITION, AND PHARMACEUTICAL PREPARATION 审中-公开
标题翻译：生产稳定的药物组合物的方法和药物制备
公开(公告)号：WO1995013794A1
公开(公告)日：1995-05-26
申请号：PCT/JP1994001936
申请日：1994-11-17
申请人： NIPPON SHINYAKU CO., LTD. , NAKAMICHI, Kouichi , IZUMI, Shougo , YASUURA, Hiroyuki
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： A61K09/00
CPC分类号： A61K9/2095 , A61K9/1694
摘要： An object of the invention is to provide a technique whereby medicines and pharmaceutical preparations can readily be stabilized by a more practicable and economical process than before. The process comprises processing 1 part by weight of a physiologically inactive powdery additive, 0.001-1 part by weight of a high-molecular-weight additive and, for example, a sublimable medicine as the essential starting materials in one batch on a multi-screw extruder. This process enables a physicochemically stable medicinal composition to be produced readily and rapidly in a large quantity and in a fundamentally continuous manner.
摘要翻译：本发明的目的是提供一种技术，其中药物和药物制剂可以通过比以前更可行和经济的方法容易地稳定。该方法包括将1重量份的生理惰性粉末状添加剂，0.001-1重量份的高分子量添加剂和例如作为主要原料的可升华药物一批次加入多螺杆挤出机。该方法使得物理化学稳定的药物组合物能够以大量和基本上连续的方式容易且快速地生产。

86. 发明申请

WO1995003801A1 ANTIDEPRESSANT 审中-公开
标题翻译：抗抑郁
公开(公告)号：WO1995003801A1
公开(公告)日：1995-02-09
申请号：PCT/JP1994001235
申请日：1994-07-27
申请人： NIPPON SHINYAKU CO., LTD. , KIMURA, Kiyoshi , UKAI, Yojiro
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： A61K31/445
CPC分类号： C07D207/28 , A61K31/454 , A61K31/496
摘要： An antidepressant containing a pyroglutamamide derivative represented by general formula (I) and a pharmaceutically acceptable salt thereof as the active ingredient, wherein Y represents CH2 or N-R; and R represents alkoxycarbonyl, (un)substituted aralkyl or morpholinocarbonylalkyl. This compound is useful for preventing or treating the depressive condition or depression.
摘要翻译：一种抗抑郁药，其含有通式（I）所示的焦谷氨酰胺衍生物及其药学上可接受的盐作为活性成分，其中Y表示CH 2或N-R; 和R表示烷氧基羰基，（取代的）取代的芳烷基或吗啉代羰基烷基。该化合物可用于预防或治疗抑郁症或抑郁症。

87. 发明申请

WO1994014819A1 QUINOLINECARBOXYLIC ACID DERIVATIVE AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：喹啉酮羧酸衍生物及其制备方法
公开(公告)号：WO1994014819A1
公开(公告)日：1994-07-07
申请号：PCT/JP1993001897
申请日：1993-12-27
申请人： NIPPON SHINYAKU CO., LTD. , SEGAWA, Jun , MATSUOKA, Masato , TOMII, Yoshifumi
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07D513/04
CPC分类号： C07D513/04 , C07D215/56
摘要： A quinolinecarboxylic acid derivative represented by general formula (I) and a pharmaceutically acceptable salt thereof, wherein z represents (un)substituted cyclic amino or phenyl; A represents > C = CH2 or > CHR , R representing fluoroalkyl; R represents hydrogen, alkyl, alkoxy, amino or halogen; and R represents hydrogen or alkyl. The invention compound is useful for treating various infectious diseases, in particular, those caused by Gram-positive bacteria including methicillin resistant Staphylococcus aureus and new quinolone and methicillin resistant Staphylococcus aureus.
摘要翻译：由通式（I）表示的喹啉羧酸衍生物及其药学上可接受的盐，其中z表示（未）取代的环状氨基或苯基; A表示> C = CH 2或> CHR 1，R 1表示氟代烷基; R 2表示氢，烷基，烷氧基，氨基或卤素; R 3表示氢或烷基。本发明化合物可用于治疗各种感染性疾病，特别是由革兰氏阳性菌（包括耐甲氧西林金黄色葡萄球菌和新喹诺酮和耐甲氧西林金黄色葡萄球菌）引起的感染性疾病。

88. 发明申请

WO1994008561A1 CRYSTALLINE CONDITION DISLOCATING METHOD 审中-公开
标题翻译：晶体条件分离方法
公开(公告)号：WO1994008561A1
公开(公告)日：1994-04-28
申请号：PCT/JP1993001469
申请日：1993-10-13
申请人： NIPPON SHINYAKU CO., LTD. , NAKAMICHI, Kouichi , IZUMI, Shougo , OKA, Masaaki
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： A61K09/00
CPC分类号： A61K9/14
摘要： An object of this invention is to provide a method of dislocating the crystalline condition of crystalline medicine simply, speedily and homogeneously, and, moreover, in large quantities at once. This invention is directed to a method using an extruder when crystalline medicine in a certain crystalline condition ( DELTA is dislocated to another crystalline condition ( omicron ), i.e., when the dislocation of crystalline condition ( DELTA -> omicron ) is carried out.
摘要翻译：本发明的一个目的是提供一种简单，快速和均匀的脱色结晶状态的方法，此外大量地提供一种方法。本发明涉及一种使用挤出机的方法，该结晶药物在某种结晶状态（DELTA被脱位至另一结晶状态（微米））时，即当结晶状态（DELTA - >微米）脱位时。

89. 发明申请

WO1993025532A1 CARBOXYLIC ACID DERIVATIVE AND PRODUCTION THEREOF 审中-公开
标题翻译：羧酸衍生物及其生产方法
公开(公告)号：WO1993025532A1
公开(公告)日：1993-12-23
申请号：PCT/JP1993000795
申请日：1993-06-15
申请人： NIPPON SHINYAKU CO., LTD. , SEGAWA, Jun , MAKITA, Yoshihiko
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07D215/56
CPC分类号： C07D513/04 , C07D215/56
摘要： A compound represented by general formula (I), a compound represented by general formula (II), and a process for producing a compound represented by general formula (Ia) by the ring closure reaction of a compound represented by general formula (IIa) wherein R represents hydrogen or alkyl; R represents alkyl; R represents hydrogen or acyl; R represents -NH2 or -SCH2R ; and X represents hydrogen or chlorine. The invention process, using these compounds as the intermediates, can provide an alkyl 6,7-difluoro-1-methyl-4-oxo-4H-[1,3]thiazeto[3,2-a]quinolinecarboxylate in fewer steps than the conventional processes efficiently and economically.
摘要翻译：由通式（I）表示的化合物，通式（II）表示的化合物以及通式（IIa）表示的化合物的闭环反应制备由通式（Ia）表示的化合物的方法，其中 R 1表示氢或烷基; R 2表示烷基; R 3表示氢或酰基; R 4表示-NH 2或-SCH 2 R 1; X表示氢或氯。使用这些化合物作为中间体的本发明方法可以以较少的步骤提供6,7-二氟-1-甲基-4-氧代-4H- [1,3]噻唑并[3,2-a]喹啉羧酸烷基酯常规方法有效和经济。

90. 发明申请

WO1993024512A1 NUCLEIC ACID HOMOLOGUE 审中-公开
标题翻译：核酸同种异体
公开(公告)号：WO1993024512A1
公开(公告)日：1993-12-09
申请号：PCT/JP1993000684
申请日：1993-05-24
申请人： NIPPON SHINYAKU CO., LTD. , YANO, Junichi , OHGI, Tadaaki , ISHIYAMA, Kouichi
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07H21/04
CPC分类号： C07H21/00
摘要： An object of the invention is to provide a novel antisense molecule utilizable as a medicine which suppresses infection with herpesvirus, influenza virus, human immunodeficiency virus or the like and the action of cancer genes. The nucleic acid homologue of the invention is one represented by general formula (I), wherein X and Y may be the same or different from each other and each represents S or O; B , B , B and B may be the same or different from one another and each represents adenine, guanine, hypoxanthine, cytosine, thymine or uracil; and n represents an integer of 1 or above, provided that B and B need not necessarily be one and the same base when n is 2 or above.
摘要翻译：本发明的目的是提供一种可用作药物的新型反义分子，其可抑制疱疹病毒，流感病毒，人类免疫缺陷病毒等的感染和癌基因的作用。本发明的核酸同源物是通式（I）所示的核酸同系物，其中X和Y可以相同或不同，各自表示S或O; B 1，B 2，B 3和B 4可以彼此相同或不同，并且各自表示腺嘌呤，鸟嘌呤，次黄嘌呤，胞嘧啶，胸腺嘧啶或尿嘧啶; n表示1以上的整数，条件是当n为2以上时，B 2和B 3不一定是同一个碱基。

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