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1. 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。

2. 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。

3. 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.

4. 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。

5. 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。

6. 发明申请

WO1997048712A1 ASIALOTRISACCHARIDE MORANOLINE DERIVATIVES AND DRUGS 审中-公开
标题翻译： ASIALOTRISACCHARIDE MORANOLINE DORIVATIVES AND DRUGS
公开(公告)号：WO1997048712A1
公开(公告)日：1997-12-24
申请号：PCT/JP1997002069
申请日：1997-06-16
申请人： NIPPON SHINYAKU CO., LTD. , OHGI, Tadaaki , ISHIYAMA, Kouichi , MORI, Kazuya
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07H17/02
CPC分类号： C07H17/02
摘要： Novel asialotrisaccharide moranoline derivatives represented by general formula (I) which inhibit selectins and thus are useful in the treatment of diseases such as inflammation wherein R represents (a) or (b); one of R and R represents galactopyranosyl optionally substituted at all or some of the hydroxyl groups by -SO3H, -CH2COOH or (c) while another represents fucopyranosyl; A represents -(CH2)m-NR -CO-O-, -CO-O-, -(CH2)n-CO-O-, -C2H4(OC2H4)z-NR -CO-O-, -C2H4(OC2H4)y-OCH2-CO-O- or -(CH2)n-O-; R and R are the same or different and each represents a saturated or unsaturated hydrocarbon group or a saturated or unsaturated fatty acid residue; R and R are the same or different and each represents hydroxy, alkyl or alkoxy; and R represents H or alkyl.
摘要翻译：抑制选择素的由通式（I）表示的新型脱二羟基山梨醇衍生物衍生物，因此可用于治疗诸如炎症的疾病，其中R代表（a）或（b）; R 1和R 2中的一个表示通过-SO 3 H，-CH 2 COOH或（c）任选地在所有或一些羟基上被取代的吡喃半乳糖基，而另一个代表fucopyranosyl; A表示 - （CH 2）m -NR 6 -CO-O-，-CO-O-， - （CH 2）n -CO-O-，-C 2 H 4（OC 2 H 4）z -NR NR -CO-O - ， - C 2 H 4（OC 2 H 4）y -OCH 2 -CO-O-或 - （CH 2）n O-; R a和R b相同或不同，各自表示饱和或不饱和烃基或饱和或不饱和脂肪酸残基; R c和R d相同或不同，各自表示羟基，烷基或烷氧基; R e表示H或烷基。

7. 发明申请

WO1997025987A1 ISCHEMIC HEART MUSCLE PROTECTIVE AGENTS 审中-公开
标题翻译： ISCHEMIC HEART MUSCLE保护剂
公开(公告)号：WO1997025987A1
公开(公告)日：1997-07-24
申请号：PCT/JP1997000071
申请日：1997-01-17
申请人： NIPPON SHINYAKU CO., LTD. , FUJIWARA, Hisayoshi , YOSHIKUNI, Yoshiaki , OCHI, Seishi
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： A61K31/445
CPC分类号： C07D471/04 , A61K31/437 , C07C215/42 , C07C2601/14 , C07D211/46
摘要： Ischemic heart muscle protecting agents and remedies for angina pectoris containing as the active ingredient compounds represented by general formula (I), wherein R , R and R are the same or different and each represents hydrogen, acyl, cyclohexanecarbonyl, alkoxyacetyl, naphthylcarbonyl, phenylalkanoyl, cinnamoyl, pyridinecarbonyl, dihydropyridinecarbonyl, thiophenecarbonyl, furylcarbonyl or benzyl; and A represents CH or N; provided that when A represents CH, then R represents hydroxy, R represents alkylamino and R represents hydroxymethyl or acyloxymethyl; while when A represents N, then R represents hydrogen, R represents hydroxymethyl or acyloxy, R represents alkyl, aryloxyalkyl or arylalkenyl, or R and R are combined together so that general formula (I) is represented by general formula (II).
摘要翻译：缺血性心肌保护剂和含有作为由通式（I）表示的活性成分化合物的心绞痛的治疗剂，其中R 1，R 2和R 3相同或不同，各自表示氢，酰基环己烷羰基，烷氧基乙酰基，萘基羰基，苯基烷酰基，肉桂酰基，吡啶羰基，二氢吡啶羰基，噻吩羰基，呋喃基羰基或苄基; A表示CH或N; 条件是当A表示CH时，R 4表示羟基，R 5表示烷基氨基，R 6表示羟甲基或酰氧基甲基; 而当A表示N时，R 6表示氢，R 4表示羟甲基或酰氧基，R 5表示烷基，芳氧基烷基或芳基烯基，或R 4和R 5组合在一起，式（I）由通式（II）表示。

8. 发明申请

WO1996022276A1 ETHYLAMINE DERIVATIVES AND DRUGS 审中-公开
标题翻译：乙酰胺衍生物和药物
公开(公告)号：WO1996022276A1
公开(公告)日：1996-07-25
申请号：PCT/JP1996000086
申请日：1996-01-19
申请人： NIPPON SHINYAKU CO., LTD. , MURASE, Masao , HAMADA, Kozo , ASAKI, Tetsuo
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07C215/50
CPC分类号： C07C219/28 , C07C215/50 , C07C271/44
摘要： A compound of general formula (I) or a pharmaceutically acceptable salt thereof or its hydrate, wherein R and R are each independently alkyl or alkenyl; R is optionally substituted aryl or an optionally substituted aromatic heterocyclic group having at least one heteroatom selected from the group consisting of nitrogen, oxygen and sulfur in the aromatic heterocycle; R is hydrogen, acyl, alkoxycarbonyl or optionally mono- or di-alkyl substituted carbamoyl; and R is hydrogen, halogeno or alkyl.
摘要翻译：通式（I）的化合物或其药学上可接受的盐或其水合物，其中R 1和R 2各自独立地为烷基或烯基; R 3是在芳族杂环中具有至少一个选自氮，氧和硫的杂原子的任选取代的芳基或任选取代的芳族杂环基; R 4是氢，酰基，烷氧基羰基或任选的单或二烷基取代的氨基甲酰基; R 5为氢，卤代或烷基。

9. 发明申请

WO1996000217A1 OPTICALLY ACTIVE QUINOLINECARBOXYLIC ACID DERIVATIVE AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：光活性喹啉羧酸衍生物及其制备方法
公开(公告)号：WO1996000217A1
公开(公告)日：1996-01-04
申请号：PCT/JP1995001255
申请日：1995-06-23
申请人： NIPPON SHINYAKU CO., LTD. , SEGAWA, Jun , MATSUOKA, Masato , AMIMOTO, Isao
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： C07D215/56
CPC分类号： C07D215/56
摘要： Diastereomers (Ia) and (Ib) obtained by reacting a compound (III) with a chiral carboxylic or amino acid or a reactive derivative thereof, chlorinating the reaction product (II), and separating the obtained diastereomeric mixture (I), wherein R represents hydrogen, halogeno, etc.; R represents hydrogen, etc.; R represents alkyl, etc.; R represents a chiral acyl or amino acid residue; and X represents halogen, or (un)substituted cyclic amino or phenyl.
摘要翻译：通过使化合物（III）与手性羧酸或氨基酸或其活性衍生物反应获得的非对映体（Ia）和（Ib），氯化反应产物（II），并分离得到的非对映体混合物（I） 1>表示氢，卤素等; R 2表示氢等; R 3表示烷基等; R 4表示手性酰基或氨基酸残基; X表示卤素，或（un）取代的环状氨基或苯基。

10. 发明申请

WO1995028835A1 PROCESS FOR PRODUCING PESTICIDE-CONTAINING WAX MATRIX AND AGRICULTURAL PREPARATION 审中-公开
标题翻译：生产含农药的WAX矩阵和农业准备的方法
公开(公告)号：WO1995028835A1
公开(公告)日：1995-11-02
申请号：PCT/JP1995000780
申请日：1995-04-20
申请人： NIPPON SHINYAKU CO., LTD. , NAKAMICHI, Kouichi , IZUMI, Shougo , YASUURA, Hiroyuki
发明人： NIPPON SHINYAKU CO., LTD.
IPC分类号： A01N25/10
CPC分类号： A01N25/08
摘要： A process for producing a pesticide-containing wax matrix capable of coping with environmental changes, which comprises treating a number of waxes having different properties and a pesticide as the essential ingredient in one batch on a multi-screw extruder. As the waxes having different properties can be mixed with one another sufficiently homogeneously, the pesticide can be released in a highly controlled manner.
摘要翻译：一种能够应对环境变化的含农药蜡基质的方法，其包括在多螺杆挤出机上一批处理许多具有不同性质的蜡和作为必需成分的农药的蜡。由于具有不同性质的蜡可以彼此充分地相互混合，因此可以以高度可控的方式释放农药。

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