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1. 发明申请

WO1990014347A1 INDOLE DERIVATIVES AND MEDICINE 审中-公开
标题翻译：吲哚衍生物和药物
公开(公告)号：WO1990014347A1
公开(公告)日：1990-11-29
申请号：PCT/JP1990000645
申请日：1990-05-22
申请人： NIPPON SHINYAKU CO. LTD. , KIMURA, Kiyoshi , KISE, Masahiro , KITANO, Masahiko , UKAI, Yojiro , OGAWA, Kazuhiro , FUKUI, Takako
发明人： NIPPON SHINYAKU CO. LTD.
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Indolecarboxamide derivatives of general formula (I) and a serotonin antagonist mainly comprising the same. The test on the activity of the compounds (I) in the inhibition of Bezold-Jarisch reflex has proved that the activity is 3 to 5 times as potent as those of the conventional drugs and also the duration of action is 5 to 10 times as long as those of the conventional ones. The test on the activity of the same in the inhibition of cisplatin-induced vomiting has also proved that this activity is potent. Since the compounds of the invention have only a low acute toxicity, they are very useful as a serotonin antagonist.
摘要翻译：通式（I）的吲哚酰胺衍生物和主要包含其的5-羟色胺拮抗剂。化合物（I）在抑制Bezold-Jarisch反射中的活性测试证明，其活性是常规药物的活性的3至5倍，并且作用持续时间为5至10倍如传统的那些。对抑制顺铂引起的呕吐的活性的测试也证明了这种活性是有效的。由于本发明的化合物仅具有低的急性毒性，因此它们作为5-羟色胺拮抗剂是非常有用的。

2. 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。

3. 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。

4. 发明申请

WO1998018469A1 CRANIAL NERVE CELL PROTECTIVES 审中-公开
标题翻译：急性神经细胞保护
公开(公告)号：WO1998018469A1
公开(公告)日：1998-05-07
申请号：PCT/JP1997003974
申请日：1997-10-31
申请人： NIPPON SHINYAKU CO., LTD. , AKAIKE, Akinori , UKAI, Yojiro
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： A61K31/445
CPC分类号： C07D207/28
摘要： Cranial nerve cell protectives, in particular, preventives/remedies for neuropathy caused by excitatory amino acid neurotoxins or preventives/remedies for retinal disorders, which contain as the active ingredient pyroglutamide derivatives represented by general formula (I), their pharmaceutically acceptable salts, or solvates thereof. In said formula, A represents optionally substituted, 5- to 10- membered cyclic amino optionally containing 1 to 3 heteroatoms, which may be the same or different and selected from the group consisting of nitrogen, oxygen and sulfur, in addition to the nitrogen bonded to the carbonyl.
摘要翻译：颅神经细胞保护剂，特别是由兴奋性氨基酸神经毒素引起的神经病的预防药物/治疗剂或视网膜疾病的预防药物/治疗剂，其含有作为活性成分的通式（I）表示的焦罗他他胺衍生物，其药学上可接受的盐或溶剂合物它们。在所述式中，A代表任选含有1-3个杂原子的任选取代的5-至10-元环氨基，除了氮键合之外，它们可以相同或不同，并且选自氮，氧和硫。到羰基。

5. 发明申请

WO1996007641A1 HETEROCYCLIC DERIVATIVE AND MEDICINE 审中-公开
标题翻译：杂环衍生物和药物
公开(公告)号：WO1996007641A1
公开(公告)日：1996-03-14
申请号：PCT/JP1995001792
申请日：1995-09-08
申请人： NIPPON SHINYAKU CO., LTD. , CHOKAI, Shoichi , UKAI, Yojiro , AOKI, Tomiyosi , IDEGUCHI, Kyoichi
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07D213/64
CPC分类号： C07D213/64 , C07D239/34 , C07D239/38 , C07D239/52 , C07D239/56 , C07D251/22 , C07D401/04 , C07D401/12 , C07D409/04
摘要： A medicine containing a compound represented by general formula (I) or a salt thereof as the active ingredient, having an excellent activity of inhibiting neuron necrosis, and being useful as a remedy for cerebrovascular disorder, wherein R represents aryl or heteroaryl; R represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, haloalkyl, alkoxy, alkylthio, amino, monoalkylamino, dialkylamino or phenyl; R and R represent each hydrogen or alkyl, or R and R are combined with the adjacent nitrogen atom to represent a 5- to 7-membered cyclic amino group NR R ; A represents C2-C10 alkylene; W represents O, S or (CH)n (wherein CH may be substituted by alkyl, and n represents 0, 1 or 2); and X, Y and Z represent each independently CH (wherein H may be replaced by alkyl) or N, provided the case where all of X, Y and Z are CH at the same time is excepted.
摘要翻译：含有由通式（I）表示的化合物或其盐作为活性成分的药物，具有优异的抑制神经元坏死的活性，可用作脑血管障碍的治疗剂，其中R 1表示芳基或杂芳基; R 2表示氢，烷基，烯基，环烷基，环烷基烷基，羟基烷基，卤代烷基，烷氧基，烷硫基，氨基，单烷基氨基，二烷基氨基或苯基; R 3和R 4各自代表氢或烷基，或R 3和R 4与相邻的氮原子结合，代表5-至7-元环氨基NR 3 R 4>; A表示C2-C10亚烷基; W表示O，S或（CH）n（其中CH可以被烷基取代，n表示0,1或2）。 X，Y和Z各自独立地表示CH（其中H可以被烷基取代）或N表示，只要X，Y和Z都同时为CH的情况除外。

6. 发明申请

WO1988007867A1 NOOTROPIC 审中-公开
标题翻译：促智
公开(公告)号：WO1988007867A1
公开(公告)日：1988-10-20
申请号：PCT/JP1988000347
申请日：1988-04-07
申请人： NIPPON SHINYAKU CO., LTD. , KIMURA, Kiyoshi , UKAI, Yojiro , OGASAWARA, Takashi , NAKAGAWA, Yutaka
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： A61K37/02
CPC分类号： C07K5/0821 , A61K31/54 , A61K38/06
摘要： A novel nootropic to be applicable to senile dementia is disclosed. Known nootropics such as TRH (thyrotropin releasing hormone) have the defect that they are too rapidly decomposed in the body and cannot be administered orally. The present nootropic contains as the major component a compound having chemical structural formula (I), wherein R represents a lower alkyl. Remarkable effects are observed with animals with less toxicity, so that the nootropic can be expected to be useful as a medicine. This drug has an extreme significance in the coming aged society.

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