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1. 发明申请

WO1998006724A1 METABOTROPIC GLUTAMATE RECEPTOR AGONISTS 审中-公开
标题翻译：代谢谷氨酸受体激动剂
公开(公告)号：WO1998006724A1
公开(公告)日：1998-02-19
申请号：PCT/JP1997002748
申请日：1997-08-07
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , HAYASHIBE, Satoshi , ITAHANA, Hirotsune , YAHIRO, Kiyoshi , TSUKAMOTO, Shin-ichi , OKADA, Masamichi , YAMASHITA, Hiroshi
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D513/04
CPC分类号： C07D513/04 , A61K31/00 , A61K31/429
摘要： Medicinal compositions containing compounds represented by general formula (I) or pharmaceutically acceptable salts thereof having metabotropic glutamate receptor agonism and thus being useful as remedies for various diseases which can be cured or relieved thereby, in particular, epilepsy, pain, Parkinson's syndrome, etc.; the use of these compounds for producing these compositions; methods for treating the above-mentioned diseases through the administration of these compounds in effective dosages; and novel imidazobenzothiazole derivatives (II and III) or pharmaceutically acceptable salts thereof which are useful as remedies for the above-mentioned diseases, wherein the ring A represents an optionally substituted aryl, monocyclic heterocycle or dicyclic heterocycle group; R represents H, halogeno, lower alkyl, hydroxy(lower alkyl), lower alkoxy(lower alkyl) or lower alkoxy; R to R represent each a substituent selected from among various ones such as H, halogeno, lower alkyl, CN, NO2, alkoxy, thiol, carboxylate, sulfonate, carbamoyl, amine, substituted alkyl and heterocycles; R to R represent the same substituents as those of R to R excluding specific substituents and combinations thereof; and R represents hydroxymethyl, etc.
摘要翻译：含有由通式（I）表示的化合物或其药学上可接受的盐的代谢型谷氨酸受体激动剂的药用组合物，因此可用作可由其治愈或缓解的各种疾病，特别是癫痫，疼痛，帕金森综合症等的补救措施。 ; 这些化合物用于制备这些组合物的用途; 通过以有效剂量施用这些化合物来治疗上述疾病的方法; 和其可用作上述疾病的补救剂的新型咪唑并噻唑衍生物（II和III）或其药学上可接受的盐，其中环A表示任选取代的芳基，单环杂环或二环杂环基; R 1表示H，卤代，低级烷基，羟基（低级烷基），低级烷氧基（低级烷基）或低级烷氧基; R 2至R 5各自表示选自各种如H，卤代，低级烷基，CN，NO 2，烷氧基，硫醇，羧酸酯，磺酸酯，氨基甲酰基，胺，取代的烷基和杂环的取代基。 R 11至R 14代表与R 2至R 5相同的取代基，不包括特定取代基及其组合; R 13表示羟甲基等。

2. 发明申请

WO1994018182A1 MORPHOLINE DERIVATIVE 审中-公开
标题翻译：吗啉衍生物
公开(公告)号：WO1994018182A1
公开(公告)日：1994-08-18
申请号：PCT/JP1994000186
申请日：1994-02-08
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , FUJII, Mitsuo , SUZUKI, Takayuki , HAYASHIBE, Satoshi , TSUKAMOTO, Shin-ichi , YATSUGI, Shin-ichi , YAMAGUCHI, Tokio
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D265/30
CPC分类号： C07D265/30
摘要： A morpholine derivative represented by general formula (I) or salt thereof, wherein R and R may be the same or different from each other and each represents hydrogen or lower alkyl; R represents halogen, and the broken line represents an optional double bond. The compound and salts thereof have the activities of both of a 5-HT reincorporation inhibitor and a 5-HT2 receptor antagonist and are useful as a therapeutic agent reduced in the side effects such as depression and anxiety.
摘要翻译：由通式（I）表示的吗啉衍生物或其盐，其中R 1和R 3可以相同或不同，各自表示氢或低级烷基; R 2表示卤素，虚线表示任选的双键。其化合物及其盐具有5-HT重掺入抑制剂和5-HT2受体拮抗剂的活性，可用作减少副作用如抑郁和焦虑症的治疗剂。

3. 发明申请

WO1996010023A1 1,2,3,4-TETRAHYDROQUINOXALINDIONE DERIVATIVE 审中-公开
标题翻译： 1,2,3,4-四氢喹啉酮衍生物
公开(公告)号：WO1996010023A1
公开(公告)日：1996-04-04
申请号：PCT/JP1995001922
申请日：1995-09-25
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , SHISHIKURA, Jun-ichi , INAMI, Hiroshi , SAKAMOTO, Shuichi , TSUKAMOTO, Shin-ichi , SASAMATA, Masao , OKADA, Masamichi , FUJII, Mitsuo
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D403/04
CPC分类号： C07D231/12 , C07D233/56 , C07D241/44 , C07D249/08
摘要： A 1,2,3,4-tetrahydroquinoxalindione derivative represented by general formula (I) or a salt thereof, an NMDA-glycine receptor and/or AMPA receptor antagonist and a kainate neurocytotoxicity inhibitor each containing the same, and a medicinal composition comprising the above-mentioned compound and pharmaceutically acceptable carriers: wherein X represents N or CH; R represents imidazolyl or di(lower alkyl)amino; R represents (1) halogeno, nitro, cyano, carboxy, amino, mono- or di(lower alkyl)amino, lower alkanoyl, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, or carbamoyl, (2) lower alkyl or lower alkoxy which may be substituted by halogeno, carboxy or aryl, or (3) phenyloxy which may be substituted by lower alkoxycarbonyl or carboxy; R represents hydroxy, lower alkoxy, amino, or mono- or di(lower alkyl)amino; and A represents optionally substituted alkylene or -O-B- (B being lower alkylene); provided the case wherein R represents imidazolyl, R represents cyano, A represents ethylene and R represents hydroxy is excepted.
摘要翻译：由通式（I）表示的1,2,3,4-四氢喹喔啉二酮衍生物或其盐，NMDA-甘氨酸受体和/或AMPA受体拮抗剂和各自含有它们的红藻氨酸神经细胞毒素抑制剂，以及药物组合物，上述化合物和药学上可接受的载体：其中X表示N或CH; R代表咪唑基或二（低级烷基）氨基; R 1表示（1）卤代，硝基，氰基，羧基，氨基，单或二（低级烷基）氨基，低级烷酰基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基或氨基甲酰基，（2）低级烷基或低级可被卤素，羧基或芳基取代的烷氧基，或（3）可被低级烷氧基羰基或羧基取代的苯氧基; R 2表示羟基，低级烷氧基，氨基或单或二（低级烷基）氨基; 和A表示任选取代的亚烷基或-O-B-（B是低级亚烷基）; 条件是其中R表示咪唑基，R 1表示氰基，A表示亚乙基，R 2表示羟基。

4. 发明申请

WO1997017970A1 KAINIC ACID NEURONOTOXICITY INHIBITORS AND PYRIDOTHIAZINE DERIVATIVES 审中-公开
标题翻译：碱性酸性神经毒性抑制剂和吡啶并吡啶衍生物
公开(公告)号：WO1997017970A1
公开(公告)日：1997-05-22
申请号：PCT/JP1996003339
申请日：1996-11-14
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , SHISHIKURA, Jun-ichi , INAMI, Hiroshi , YASUNAGA, Tomoyuki , HIRANO, Masaaki , SAKAMOTO, Shuichi , OHNO, Kazushige , OKADA, Masamichi , TSUKAMOTO, Shin-ichi
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/54
CPC分类号： A61K31/5415
摘要： Neuron protective agents on the basis of the inhibition of neuronotoxicity of kainic acid and compounds useful as such agents. Pyridothiazine derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof and neuronotoxicity inhibitors containing as the active ingredient these compounds or pharmaceutically acceptable salts thereof, wherein A represents a pyridine ring; formula (II) represents formula (III) or formula (IV); and R , R , R , R and R are the same or different and each represents hydrogen, optionally substituted lower alkyl, cycloalkyl, alkenyl, aryl, carboxy or lower alkoxycarbonyl or does not exist, or R and R together form a nitrogenous heterocycle optionally having a nitrogen atom as another heteroatom, being fused with a benzene ring, or being substituted by lower alkyl.
摘要翻译：神经元保护剂基于抑制红藻氨酸的神经毒性和用作此类药物的化合物。通式（I）表示的吡唑并噻嗪衍生物或其药学上可接受的盐和含有这些化合物或其药学上可接受的盐的作为活性成分的神经毒性抑制剂，其中A表示吡啶环; 式（II）表示式（III）或式（IV）; R 1，R 2，R 3，R 4和R 5相同或不同，各自表示氢，任选取代的低级烷基，环烷基，烯基，芳基，羧基或低级烷氧基羰基或不存在，或R 2和R 3一起形成任选具有氮原子作为另一杂原子的含氮杂环，与苯环稠合或被低级烷基取代。

5. 发明申请

WO1992020683A1 (-)-(S)-2,8-DIMETHYL-3-METHYLENE-1-OXA-8-AZASPIRO[4,5]DECANE L-TARTRATE 审中-公开
标题翻译：（ - ） - （S）-2,8-二甲基-3-甲基-1-氧代-8-亚氨基[4,5]癸烷L-十二烷
公开(公告)号：WO1992020683A1
公开(公告)日：1992-11-26
申请号：PCT/JP1992000548
申请日：1992-04-27
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , TSUKAMOTO, Shin-ichi , KOHINATA, Takeshi , FUJII, Mitsuo , TOMISAWA, Sakiko
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D491/107
CPC分类号： C07D491/10
摘要： (-)-(S)-2,8-Dimethyl-3-methylene-1-oxa-8-azaspiro[4,5]decane L-tartrate having a storage stability superior to that of other salts and being applicable as a medicine.
摘要翻译：（ - ） - （S）-2,8-二甲基-3-亚甲基-1-氧杂-8-氮杂螺[4,5]癸烷L-酒石酸盐，其储存稳定性优于其它盐，并且可用作药物。

6. 发明申请

WO1995029891A1 N-(3-PYRROLIDINYL)BENZAMIDE DERIVATIVE 审中-公开
标题翻译： N-（3-吡咯烷基）苯甲酰胺衍生物
公开(公告)号：WO1995029891A1
公开(公告)日：1995-11-09
申请号：PCT/JP1995000818
申请日：1995-04-26
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , OHMORI, Junya , MAENO, Kyoichi , HIDAKA, Kazuyuki , NAKATO, Kazuhiro , SAKAMOTO, Shuichi , TSUKAMOTO, Shin-ichi
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D207/14
CPC分类号： C07D207/14
摘要： An N-(3-pyrrolidinyl)benzamide derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof and a medicine containing the same, having a potent and selective antagonism against dopamine D3 and/or D4 receptors and useful as a psychotropic agent, schizophrenia remedy, and so forth. In said formula, R represents hydrogen, lower alkyl, aralkyl, or three- to eight-membered cycloalkyl or cycloalkyl-lower alkyl; R represents four- to sixteen-membered bi- or tricyclic bridged hydrocarbon group; R represents lower alkoxy, amino, or mono- or di(lower alkyl)amino; R represents hydrogen, halogen, optionally hydroxylated lower alkyl, lower alkoxy, cyano, nitro, amino, mono- or di(lower alkyl)amino, acyl or -S(O)m-R ; R represents lower alkyl, amino or mono- or di(lower alkyl)amino; m represents 0, 1 or 2; X represents a bond, -O-, -S(O)n-, -NH- or -CONH-; and n represents 0, 1 or 2; provided when R represents cycloalkyl, the case where X represents -CONH-, R represents lower alkoxy and R represents halogen is excepted.
摘要翻译：由通式（I）表示的N-（3-吡咯烷基）苯甲酰胺衍生物或其药学上可接受的盐和含有它们的药物，具有对多巴胺D3和/或D4受体的有效和选择性拮抗作用并用作精神药物，精神分裂症补救等等。在所述式中，R 1表示氢，低级烷基，芳烷基或三至八元环烷基或环烷基 - 低级烷基; R 2表示四至十六元的二环或三环桥连烃基; R 3表示低级烷氧基，氨基或单或二（低级烷基）氨基; R 4表示氢，卤素，任选羟基化的低级烷基，低级烷氧基，氰基，硝基，氨基，单或二（低级烷基）氨基，酰基或-S（O）m -R 5。 R 5表示低级烷基，氨基或一或二（低级烷基）氨基; m表示0,1或2; X表示键，-O - ， - S（O）n - ， - NH-或-CONH-; n表示0,1或2; 当R 1表示环烷基时，其中X表示-CONH-，R 3表示低级烷氧基，R 4表示卤素的情况除外。

7. 发明申请

WO1998000420A1 NOVEL THIOPHENE DERIVATIVES AND DRUG COMPOSITIONS CONTAINING THE SAME 审中-公开
标题翻译：新型噻吩衍生物和含有它们的药物组合物
公开(公告)号：WO1998000420A1
公开(公告)日：1998-01-08
申请号：PCT/JP1997002255
申请日：1997-06-30
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , KIMURA, Takenori , MURAKAMI, Takeshi , OHMORI, Junya , MORITA, Takuma , TSUKAMOTO, Shin-ichi
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D333/24
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D333/24 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Thiophene derivatives of general formula (I) and pharmaceutically acceptable salts thereof. These compounds act as an anti-PCP agonist, thus being useful as psychotropic or antischizophrenic agents and so on. In said formula R1 is -A1-X1-R3; R2 is -A2-X2-R4 or nil; B is a four- to ten-membered nitrogenous cycloalkyl or a five- or six-membered nitrogenous unsaturated heterocycle; Ar is aryl or heteroaryl; A1, A2 and A3 are each independently a bond or lower alkylene; X1 and X2 are each independently a bond, -O-, -S- or the like; and R3 and R4 are each independently hydrogen, cyclic imido, lower alkyl, cycloalkyl, aryl or aralkyl, with the provisos that when Ar is a thiazole ring, at least either of A1 and A2 is lower alkylene and that when Ar is a benzene ring, compounds wherein one of R1 and R2 is methyl or halogeno and the other thereof is hydrogen are excepted.
摘要翻译：通式（I）的噻吩衍生物及其药学上可接受的盐。这些化合物作为抗PCP激动剂，因此可用作精神药物或抗精神分裂药剂等。在所述式中，R1是-A1-X1-R3; R2是-A2-X2-R4或nil; B是4至10元含氮环烷基或5或6元含氮不饱和杂环; Ar是芳基或杂芳基; A1，A2和A3各自独立地为键或低级亚烷基; X 1和X 2各自独立地为键，-O-，-S-等; 并且R 3和R 4各自独立地为氢，环状亚氨基，低级烷基，环烷基，芳基或芳烷基，条件是当Ar为噻唑环时，A1和A2中的至少一个为低级亚烷基，当Ar为苯环时，其中R1和R2之一是甲基或卤代，另一个是氢的化合物除外。

8. 发明申请

WO1995008533A1 N-(3-PYRROLIDINYL)BENZAMIDE DERIVATIVE 审中-公开
标题翻译： N-（3-吡咯烷基）苯甲酰胺衍生物
公开(公告)号：WO1995008533A1
公开(公告)日：1995-03-30
申请号：PCT/JP1994001547
申请日：1994-09-20
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , OHMORI, Junya , MAENO, Kyoichi , HIDAKA, Kazuyuki , NAKATO, Kazuhiro , SAKAMOTO, Shuichi , TSUKAMOTO, Shin-ichi
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D207/14
CPC分类号： C07D207/335 , C07D207/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06
摘要： An N-(3-pyrrolidinyl)benzamide derivative represented by general formula (I) having a selective and potent affinity for dopamine D3 receptors and/or dopamine D4 receptors, a pharmaceutically acceptable salt thereof, and dopamine D3 receptor and/or dopamine D4 receptor antagonists, wherein R represents halogen; R represents lower alkoxy; R represents hydrogen or lower alkyl; A represents a single bond or lower alkylene; ring B represents substituted or unsubstituted: 1) saturated or unsaturated 3- to 8-membered monocyclic hydrocarbon groups or 4- to 16-membered fused bicyclic hydrocarbon groups; 2) saturated or unsaturated 3- to 8-membered heterocyclic group or 6- to 16-membered fused bicyclic heterocyclic group each containing one or two of the heteroatoms comprising nitrogen, sulfur and oxygen, 3) saturated or unsaturated 4- to 16-membered bi- or tricyclic bridged hydrocarbon group, or 4) saturated or unsaturated 6- to 16-membered bi- or tricyclic bridged heterocyclic group each containing one or two of the heteroatoms comprising nitrogen, sulfur and oxygen; and R represents 1) phenyl; 2) halogenated or nonhalogenated 3- to 8-membered monocyclic saturated hydrocarbon group; or 3) lower alkyl, halogenated lower alkyl or lower alkenyl; provided with group -A-B represents benzyl, R represents a group other than methyl. This compound is useful as a psychotropic agent having little or no side effects such as extrapyramidal syndrome.
摘要翻译：对通式（I）表示的对多巴胺D3受体和/或多巴胺D4受体具有选择性和有效亲合力的N-（3-吡咯烷基）苯甲酰胺衍生物，其药学上可接受的盐和多巴胺D3受体和/或多巴胺D4受体拮抗剂，其中R 1表示卤素; R 2表示低级烷氧基; R 3表示氢或低级烷基; A表示单键或低级亚烷基; 环B表示取代或未取代的：1）饱和或不饱和的3至8元单环烃基或4至16元稠合双环烃基; 2）饱和或不饱和的3至8元杂环基或6至16元稠合双环杂环基，每个含有一个或两个包含氮，硫和氧的杂原子，3）饱和或不饱和的4至16元双环或三环桥基烃基，或4）饱和或不饱和的6至16元双环或三环桥联杂环基，每个含有一个或两个包含氮，硫和氧的杂原子; 和R 4表示1）苯基; 2）卤代或非卤代3-至8-元单环饱和烃基; 或3）低级烷基，卤代低级烷基或低级烯基; 基团-A-B表示苄基，R 4表示甲基以外的基团。该化合物可用作具有很少或没有副作用的精神药物，例如锥体外系综合征。

9. 发明申请

WO1995002407A1 NEURON PROTECTIVE AND NOVEL OROTIC ESTER 审中-公开
标题翻译：神经保护和新型OROTIC ESTER
公开(公告)号：WO1995002407A1
公开(公告)日：1995-01-26
申请号：PCT/JP1994001134
申请日：1994-07-12
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , AKIHO, Hiraku , IWAI, Akihiko , TSUKAMOTO, Shin-ichi , KOSHIYA, Kazuo , YAMAGUCHI, Tokio
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： A61K31/505
CPC分类号： C07D239/557 , A61K31/505
摘要： A neuron protective containing a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof as the active ingredient and capable of treating disorders and diseases accompanying neuron injury and degeneration, wherein R represents hydrogen or C1-C10 linear, branched or cyclic alkyl. The protective can treat effectively various diseases accompanying neuron degeneration, such as cerebral stroke, infarction, thrombosis and hemorrhage, and subarachnoidal hemorrhage.
摘要翻译：一种含有通式（I）表示的化合物或其药学上可接受的盐作为活性成分并能够治疗伴随神经元损伤和变性的病症和疾病的神经元保护剂，其中R表示氢或C1-C10直链，支链或环状烷基。保护性可有效治疗伴随神经元变性的各种疾病，如脑卒中，梗塞，血栓形成和出血，以及蛛网膜下腔出血。

10. 发明申请

WO1995018104A1 NOVEL BENZAMIDE DERIVATIVE AND MEDICINAL COMPOSITION CONTAINING THE SAME 审中-公开
标题翻译：新颖的苯甲酸衍生物和含有它们的药物组合物
公开(公告)号：WO1995018104A1
公开(公告)日：1995-07-06
申请号：PCT/JP1994002261
申请日：1994-12-27
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD. , SUZUKI, Takeshi , IMANISHI, Naoki , ITAHANA, Hirotsune , KAMATO, Takeshi , MIYATA, Keiji , OHTA, Mitsuaki
发明人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D207/09
CPC分类号： C07D265/30 , C07D207/09 , C07D211/26 , C07D223/04 , C07D241/04 , C07D241/08 , C07D243/08 , C07D267/10 , C07D279/12 , C07D281/06 , C07D453/02 , C07D487/08
摘要： A novel benzamide derivative represented by general formula (I), or a salt, hydrate or solvate thereof. The compound is useful as a 5-HT4 receptor agonist for preventing and treating central nervous system diseases such as schizophrenia, digestive tract movement disorders such as nausea, vomiting, irritable bowel syndrome, gastric ulcer and duodenal ulcer, heart action disorders such as cardiac failure, and urologic diseases such as urinary obstruction. It is also useful as an antinociceptive agent.
摘要翻译：由通式（I）表示的新型苯甲酰胺衍生物或其盐，水合物或溶剂合物。该化合物可用作预防和治疗中枢神经系统疾病如精神分裂症，消化道运动障碍如恶心，呕吐，肠易激综合征，胃溃疡和十二指肠溃疡，心脏功能障碍如心力衰竭的5-HT4受体激动剂，泌尿系统疾病如尿路梗阻。它也可用作抗伤害感受剂。

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