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81. 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。

82. 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。

83. 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。

84. 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。

85. 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。

86. 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。

87. 发明申请

WO1993017100A1 SPECIFIC ADSORBENT AND PURIFICATION METHOD 审中-公开
标题翻译：特殊吸附和纯化方法
公开(公告)号：WO1993017100A1
公开(公告)日：1993-09-02
申请号：PCT/JP1993000202
申请日：1993-02-19
申请人： NIPPON SHINYAKU CO., LTD. , MARUO, Shigeaki , OGAWA, Hirotsugu , EZURE, Yohji
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C12N09/00
CPC分类号： C07K1/22 , C12N9/2414 , C12N9/2445 , C12Y302/01001 , C12Y302/01021
摘要： A specific adsorbent for affinity chromatography using glucosylmoranoline or the like as a ligand. Various sugar-related enzymes such as amylase and glucosidase can be purified effectively and highly by the affinity chromatography.
摘要翻译：用于使用葡糖基吗啉醇等作为配体的亲和层析的特定吸附剂。通过亲和层析可以有效和高效地纯化各种与糖相关的酶如淀粉酶和葡糖苷酶。

88. 发明申请

WO1993015098A1 LEWIS-TYPE SUGAR CHAIN DERIVATIVE 审中-公开
标题翻译： LEWIS型糖链衍生物
公开(公告)号：WO1993015098A1
公开(公告)日：1993-08-05
申请号：PCT/JP1993000106
申请日：1993-01-29
申请人： NIPPON SHINYAKU CO., LTD. , HASEGAWA, Akira , KISO, Makoto , YOSHIKUNI, Yoshiaki
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07H17/02
CPC分类号： C07H17/02 , C07H3/06
摘要： A novel SLe-type sugar chain derivative represented by general formula [I], which is useful as a medicine and has a novel structure containing moranoline, wherein R represents hydrogen, lower alkyl, lower alkenyl or lower alkynyl; R and R represent each independently galactosyl, sialylgalactosyl or fucosyl; and R represents hydroxy or acetamido. This compound has the activity of inhibiting cell adhesion and inhibits secretin antagonistically, thus being useful for treating inflammation and its accompanying thrombosis, asthma and rheumatism, and for preventing and treating immunopathy and cancer.
摘要翻译：由通式[I]表示的新型SLe型糖链衍生物，其可用作药物并具有含有山梨醇的新结构，其中R 1表示氢，低级烷基，低级烯基或低级炔基; R 2和R 3各自独立地表示半乳糖基，唾液酸半乳糖基或岩藻糖基; 且R 4表示羟基或乙酰氨基。该化合物具有抑制细胞粘附的作用，并且拮抗拮抗促胰液素，因此可用于治疗炎症及其伴随的血栓形成，哮喘和风湿病，以及预防和治疗免疫病和癌症。

89. 发明申请

WO1993001180A1 BENZOFURAN DERIVATIVE AND PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：苯并呋喃衍生物和药物组合物
公开(公告)号：WO1993001180A1
公开(公告)日：1993-01-21
申请号：PCT/JP1992000875
申请日：1992-07-08
申请人： NIPPON SHINYAKU CO., LTD. , CHOKAI, Shoichi , OHMACHI, Shinji , TAIRA, Masafumi
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07D307/80
CPC分类号： C07D307/80
摘要： A compound represented by general formula (I), a pharmacologically acceptable salt thereof, and a pharmaceutical composition containing the same as the active ingredient, wherein R represents hydrogen, halogen or alkyl; R represents alkoxycarbonyl, aralkyloxycarbonyl, carboxyl, hydroxyalkyl or acyloxyalkyl; Y represents CHOH, CHOZ, CH2 or C=O; and Z represents acyl. The composition is effective in preventing and treating arteriosclerosis, ischemic heart diseases, cerebral infarction, and restenosis after PTCA.
摘要翻译：由通式（I）表示的化合物，其药学上可接受的盐和含有该化合物的药物组合物，其中R 1表示氢，卤素或烷基; R 2表示烷氧基羰基，芳烷氧基羰基，羧基，羟基烷基或酰氧基烷基; CH2表示CHOH，符号CHOZ，符号CH2或标记C = O; Z表示酰基。该组合物有效预防和治疗PTCA后的动脉硬化，缺血性心脏病，脑梗死和再狭窄。

90. 发明申请

WO1992004347A1 INDOLE DERIVATIVE AND MEDICINE 审中-公开
标题翻译： INDOLE DIVIVATIVE和MEDICINE
公开(公告)号：WO1992004347A1
公开(公告)日：1992-03-19
申请号：PCT/JP1991001148
申请日：1991-08-29
申请人： NIPPON SHINYAKU CO., LTD. , CHOKAI, Shoichi , AOKI, Tomiyoshi , UKAI, Yojiro
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： A novel serotonin-antagonistic indolecarboxamide derivative represented by general formula (I) and a serotonin antagonist containing the same as the active ingredient wherein R represents lower alkyl and R hydrogen, halogen, lower alkyl or lower alkoxy. It is efficacious as a regulatory agent for gastrointestinal motility, a therapeutic agent for migraine, an antipsychotic drug, an antianxiety drug, etc., and also as an antidemential drug and a therapeutic agent for orthostatic hypotension.
摘要翻译：由通式（I）表示的新型5-羟色胺拮抗性吲哚克酰胺衍生物和含有与活性成分相同的5-羟色胺拮抗剂，其中R 1表示低级烷基和R 2氢，卤素，低级烷基或低级烷氧基。作为胃肠蠕动的调节剂，偏头痛治疗剂，抗精神病药，抗焦虑药等，作为抗静脉药物和直立性低血压的治疗剂是有效的。

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