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1. 发明申请

WO1997010213A1 PHENYLPIPERIDINE DERIVATIVES 审中-公开
标题翻译：苯并吡啶衍生物
公开(公告)号：WO1997010213A1
公开(公告)日：1997-03-20
申请号：PCT/JP1996002589
申请日：1996-09-11
申请人： KYOWA HAKKO KOGYO CO., LTD. , KUMAZAWA, Toshiaki , KOSHIMURA, Hirokazu , AONO, Shigeru , ICHIKAWA, Shunji , KITAMURA, Shigeto
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D211/44
CPC分类号： C07D401/04 , C07D211/52 , C07D405/04 , C07D491/04
摘要： Phenylpiperidine derivative represented by general formula (I) or pharmacologically acceptable salts thereof and an analgetic agent containing the compound, wherein X represents CH or N: Y-Z represents CH2-O, CH2-S, CH2-CH2, CH=CH or CONR (wherein R represents hydrogen or lower alkyl); R represents hydrogen, lower alkyl, halogeno, lower alkoxy or trifluoromethyl; and R , R and R are the same or different and each represents hydrogen, lower alkyl or QR (wherein Q represents a single bond or lower alkylene; and R represents hydroxy, lower alkoxyalkoxy, lower alkoxy, lower alkylthio, nitro, halogeno, lower alkanoyloxy, lower alkoxycarbonyl, lower alkanoyl or carboxy.
摘要翻译：由通式（I）表示的苯基哌啶衍生物或其药学上可接受的盐和含有该化合物的止痛剂，其中X表示CH或N：YZ表示CH 2 -O，CH 2 -S，CH 2 -CH 2，CH = CH或CONR 5 >（其中R 5表示氢或低级烷基）; R 1表示氢，低级烷基，卤代，低级烷氧基或三氟甲基; 和R 2，R 3和R 4相同或不同，各自表示氢，低级烷基或QR 6（其中Q表示单键或低级亚烷基; R 6表示羟基低级烷氧基烷氧基，低级烷硫基，硝基，卤代，低级烷酰氧基，低级烷氧基羰基，低级烷酰基或羧基。

2. 发明申请

WO1995023148A1 XANTHINE DERIVATIVE 审中-公开
公开(公告)号：WO1995023148A1
公开(公告)日：1995-08-31
申请号：PCT/JP1995000267
申请日：1995-02-23
申请人： KYOWA HAKKO KOGYO CO., LTD. , SUZUKI, Fumio , KOIKE, Nobuaki , SHIMADA, Junichi , NAKAMURA, Joji , SHIOZAKI, Shizuo , KITAMURA, Shigeto , ICHIKAWA, Shunji , KASE, Hiroshi , NONAKA, Hiromi
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D473/06
CPC分类号： C07D473/06
摘要： A xanthine derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R , R and R are the same or different from one another and each represents hydrogen, lower alkyl, lower alkenyl or lower alkynyl; R represents lower alkyl or (un)substituted aryl; R and R are the same or different from each other and each represents hydrogen, lower alkyl or lower alkoxy, or R and R are combined together to represent -O-(CH2)p-O- (wherein p represents an integer of 1 to 3); n represents 0, 1 or 2; and m represents 1 or 2. The compound has an adenosine A2 receptor antagonism and is useful for treating or preventing various diseases caused by the hyperfunctioning of adenosine A2 receptors, such as Parkinson's disease, senile dementia, depression, asthma or osteoporosis.
摘要翻译：由通式（I）表示的黄嘌呤衍生物或其药学上可接受的盐，其中R 1，R 2和R 3彼此相同或不同，并且各自表示氢，低级烷基，低级链烯基或低级炔基; R 4表示低级烷基或（未）取代的芳基; R 5和R 6彼此相同或不同，各自表示氢，低级烷基或低级烷氧基，或R 5和R 6组合在一起，表示-O-（CH 2）p O - （其中p表示1〜3的整数）; n表示0,1或2; m表示1或2.该化合物具有腺苷A2受体拮抗作用，可用于治疗或预防由腺苷A2受体如帕金森病，老年性痴呆，抑郁症，哮喘或骨质疏松症功能障碍引起的各种疾病。

3. 发明申请

WO1992006976A1 XANTHINE DERIVATIVE 审中-公开
公开(公告)号：WO1992006976A1
公开(公告)日：1992-04-30
申请号：PCT/JP1991001420
申请日：1991-10-17
申请人： KYOWA HAKKO KOGYO CO., LTD. , SUZUKI, Fumio , SHIMADA, Junichi , ISHII, Akio , NONAKA, Hiromi , KOSAKA, Nobuo , ICHIKAWA, Shunji
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D473/06
CPC分类号： C07D473/06
摘要： A novel xanthine derivative represented by general formula (I), which selectively antagonizes adenosine receptor, and a pharmacologically acceptable salt thereof. In formula (I) R?1 and R2¿ may be the same or different from each other and each represents hydrogen, propyl, butyl or allyl; R3 represents hydrogen or lower alkyl; Y?1 and Y2¿ may be the same or different from each other and each represents hydrogen or methyl; and Z represents (un)substituted phenyl, pyridyl, imidazolyl, furyl or thienyl.

4. 发明申请

WO1998015555A1 FUSED PURINE DERIVATIVES 审中-公开
标题翻译：熔化的嘌呤衍生物
公开(公告)号：WO1998015555A1
公开(公告)日：1998-04-16
申请号：PCT/JP1997003586
申请日：1997-10-07
申请人： KYOWA HAKKO KOGYO CO., LTD. , TSUMUKI, Hiroshi , SAKI, Mayumi , NONAKA, Hiromi , ICHIMURA, Michio , SHIMADA, Junichi , SUZUKI, Fumio , ICHIKAWA, Shunji , KOSAKA, Nobuo
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/14
CPC分类号： C07D487/14
摘要： Fused purine derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, which show an adenosine A3 receptor antagonism and have, for example, antiasthmatic, bronchodilating and itch-relieving effects. In said formula, R represents optionally substituted aryl or an optionally substituted aromatic heterocyclic group; R represents hydrogen, lower alkyl, alicyclic alkyl, optionally substituted aralkyl, optionally substituted aryl, or an optionally substituted aromatic heterocyclic group; R represents hydrogen, lower alkyl or optionally substituted aralkyl; X and X are the same or different and each represents hydrogen, lower alkyl, optionally substituted aralkyl, or optionally substituted aryl; and n is an integer of 0 to 3.
摘要翻译：由通式（I）表示的稠合嘌呤衍生物或其药理学上可接受的盐，其表现出腺苷A3受体拮抗作用，并且具有例如止喘，支气管扩张和瘙痒缓解作用。在所述式中，R 1表示任选取代的芳基或任选取代的芳族杂环基; R 2表示氢，低级烷基，脂环族烷基，任选取代的芳烷基，任选取代的芳基或任选取代的芳族杂环基; R 3表示氢，低级烷基或任选取代的芳烷基; X 1和X 2相同或不同，各自表示氢，低级烷基，任选取代的芳烷基或任选取代的芳基; n为0〜3的整数。

5. 发明申请

WO1995007282A1 DEPRESSION REMEDY 审中-公开
标题翻译：拒绝救济
公开(公告)号：WO1995007282A1
公开(公告)日：1995-03-16
申请号：PCT/JP1994001455
申请日：1994-09-02
申请人： KYOWA HAKKO KOGYO CO., LTD. , SUZUKI, Fumio , KOIKE, Nobuaki , SHIMADA, Junichi , KITAMURA, Shigeto , ICHIKAWA, Shunji , NAKAMURA, Joji , SHIOZAKI, Shizuo
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/53
摘要： A depression remedy containing a triazine derivative represented by general formula (I) or a pharmacologically acceptable salt thereof as the active ingredient, wherein R represents hydrogen, (un)substituted lower alkyl or (un)substituted lower alkanoyl; R represents hydrogen, (un)substituted lower alkyl, (un)substituted lower alkenyl, (un)substituted cycloalkyl, (un)substituted aryl, (un)substituted aralkyl or (un)substituted heterocycle; R represents (un)substituted heterocycle; X represents a single bond, O, S, S(O), S(O)2 or NR , wherein R represents hydrogen or (un)substituted lower alkyl or R and NR are combined with each other to form a 4- to 6-membered (un)substituted nitrogeneous saturated heterocyclic group; and A represents N or CR , wherein R represents hydrogen or (un)substituted lower alkyl.
摘要翻译：含有由通式（I）表示的三嗪衍生物或其药理学上可接受的盐作为活性成分的抑郁症药物，其中R 1表示氢，（un）取代的低级烷基或（取代的）低级烷酰基; R 2代表氢，（未）取代的低级烷基，（未）取代的低级烯基，（未）取代的环烷基，（未）取代的芳基，（未）取代的芳烷基或（未）取代杂环; R 3表示（un）取代的杂环; X表示单键O，S，S（O），S（O）2或NR 4，其中R 4表示氢或（未）取代的低级烷基或R 2和NR 4 相互结合形成4-至6-元（取代）的取代的含氮饱和杂环基; A表示N或CR 5，其中R 5表示氢或（取代的）取代的低级烷基。

6. 发明申请

WO1995003806A1 REMEDY FOR PARKINSON'S DISEASE 审中-公开
标题翻译：补救帕金森病
公开(公告)号：WO1995003806A1
公开(公告)日：1995-02-09
申请号：PCT/JP1994001196
申请日：1994-07-20
申请人： KYOWA HAKKO KOGYO CO., LTD. , SUZUKI, Fumio , SHIMADA, Junichi , KOIKE, Nobuaki , ICHIKAWA, Shunji , NAKAMURA, Joji , KANDA, Tomoyuki , KITAMURA, Shigeto
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： A61K31/53
CPC分类号： C07D487/04 , A61K31/505 , A61K31/53
摘要： A remedy for Parkinson's disease, which contains a polycyclic compound represented by general formula (I) or (II), or a pharmacologically acceptable salt thereof as the active ingredient. In formula (I) R represents hydrogen, lower alkyl or lower alkanoyl; R represents hydrogen, lower alkyl, lower alkenyl, cycloalkyl, aryl, aralkyl or heterocycle; R represents heterocycle; X represents a single bond, O, S, S(O), S(O)2 or NR , wherein R represents hydrogen, lower alkyl, etc.; and A represents N or CR , wherein R represents hydrogen or lower alkyl. In formula (II) R represents aryl or heterocycle; Y represents O, S or NR , wherein R represents hydrogen or lower alkyl; R represents hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, aralkyl or heterocycle; and B represents together with the two neighboring groups a mono- or bicyclic carbon or hetero ring.
摘要翻译：帕金森病的补救剂，其含有通式（I）或（II）表示的多环化合物或其药理学上可接受的盐作为活性成分。在式（I）中，R 1表示氢，低级烷基或低级烷酰基; R 2表示氢，低级烷基，低级烯基，环烷基，芳基，芳烷基或杂环; R 3表示杂环; X表示单键，O，S，S（O），S（O）2或NR 4，其中R 4表示氢，低级烷基等; A表示N或CR 5，其中R 5表示氢或低级烷基。在式（II）中，R 6表示芳基或杂环; Y表示O，S或NR 7，其中R 7表示氢或低级烷基; R 8表示氢，低级烷基，低级烯基，低级炔基，环烷基，芳基，芳烷基或杂环; 并且B与两个相邻基团一起表示单环或双环碳或杂环。

7. 发明申请

WO1994001114A1 ANTIDEPRESSANT 审中-公开
标题翻译：抗抑郁
公开(公告)号：WO1994001114A1
公开(公告)日：1994-01-20
申请号：PCT/JP1993000931
申请日：1993-07-07
申请人： KYOWA HAKKO KOGYO CO., LTD. , SUZUKI, Fumio , SHIMADA, Junichi , ISHII, Akio , NAKAMURA, Joji , ICHIKAWA, Shunji , KITAMURA, Shigeto , KOIKE, Nobuaki
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： A61K31/52
CPC分类号： A61K31/52 , C07D473/06 , C07D473/08 , F16B37/048
摘要： An antidepressant containing an active ingredient comprising a xanthine derivative represented by general formule (I) or a pharmacologically acceptable salt thereof, wherein R1, R2 and R3 may be the same or different from one another and each represents hydrogen, lower alkyl, alkyl or propargyl; R4 represents cycloalkyl, -(CH2)n-R5 (wherein R5 represents optionally substituted aryl or optionally substituted heterocyclic group, and n represents an integer of 0 to 4) of group (A) wherein Y1 and Y2 may be the same or different from each other and each represents hydrogen, fluorine or methyl, and Z represents optionally substituted aryl, group (B) (wherein R6 represents hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro or amino, and m represents an integer of 1 to 3), or optionally substituted heterocyclic group; and X1 and X2 may be the same or different from each other and each represents O or S.
摘要翻译：含有由通式（I）表示的黄嘌呤衍生物或其药理学上可接受的盐的活性成分的抗抑郁药，其中R 1，R 2和R 3可以相同或不同，各自表示氢，低级烷基，烷基或炔丙基 ; R4代表环烷基， - （CH2）n-R5（其中R5表示任选取代的芳基或任选取代的杂环基，n表示0至4的整数）（A）其中Y1和Y2可以相同或不同彼此各自表示氢，氟或甲基，Z表示任选取代的芳基，（B）（其中R6表示氢，羟基，低级烷基，低级烷氧基，卤素，硝基或氨基，m表示1〜 3）或任选取代的杂环基; 并且X 1和X 2可以彼此相同或不同，并且各自表示O或S.

8. 发明申请

WO1992012150A1 QUINOLINE DERIVATIVE 审中-公开
标题翻译：喹啉衍生物
公开(公告)号：WO1992012150A1
公开(公告)日：1992-07-23
申请号：PCT/JP1991001758
申请日：1991-12-25
申请人： KYOWA HAKKO KOGYO CO., LTD. , SUZUKI, Fumio , HAYASHI, Hiroaki , MIWA, Yoshikazu , KURODA, Takeshi , ISHII, Akio , ICHIKAWA, Shunji , MIKI, Ichiro , SHUTO, Katsuichi
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D451/04
CPC分类号： C07D451/14 , C07D451/04 , C07D451/12
摘要： A quinoline derivative represented by general formula (I), which has a potent 5HT3 antagonism and is useful as an antiemetic, and a pharmacologically acceptable salt thereof. In formula (I) A-B-D represents either a group of formula -C(COO-Y)=CH-C(OR)= (wherein Y represents 8-methyl-8-azabicyclo[3.2.1]oct-3-yl and R represents alkyl) or a group of formula -C(OH)=C(COX-Y)-CH= (wherein X represents -O- or -NH- and Y is as defined above).

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