-
公开(公告)号:EP0698607A1
公开(公告)日:1996-02-28
申请号:EP95909968.0
申请日:1995-02-23
发明人: SUZUKI, Fumio , KOIKE, Nobuaki , SHIMADA, Junichi , NAKAMURA, Joji , SHIOZAKI, Shizuo , KITAMURA, Shigeto , ICHIKAWA, Shunji , KASE, Hiroshi , NONAKA, Hiromi
IPC分类号: C07D473/06 , A61K31/52
CPC分类号: C07D473/06
摘要: A xanthine derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R¹, R² and R³ are the same or different from one another and each represents hydrogen, lower alkyl, lower alkenyl or lower alkynyl; R⁴ represents lower alkyl or (un)substituted aryl; R⁵ and R⁶ are the same or different from each other and each represents hydrogen, lower alkyl or lower alkoxy, or R⁵ and R⁶ 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,各自表示氢,低级烷基,低级烯基 或低级炔基; R 4表示低级烷基或(取代)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,或者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。
-
公开(公告)号:EP0603399B1
公开(公告)日:2002-09-11
申请号:EP93900411.5
申请日:1992-12-28
发明人: TANAKA, Takeo , MORISHITA, Yoshikazu , NOZAWA, Mika , CHIBA, Shigeru , KAWAMOTO, Isao , TSUKUDA, Eiji , YOSHIDA, Mayumi , SHIMAZAKI, Chieko , YAMAGUCHI, Kazuo , MATSUDA, Yuzuru , KITAMURA, Shigeto , IKEMURA, Toshihide , OGAWA, Tatsuhiro , YANO, Keiichi , SUZAWA, Toshiyuki , SHIBATA, Kenji , YAMASAKI, Motoo
CPC分类号: C07K7/06 , A61K38/00 , C07K5/1021 , C07K5/1024 , C07K7/08 , C07K14/36 , C07K14/57536
-
公开(公告)号:EP0667349B1
公开(公告)日:2001-01-24
申请号:EP94925620.0
申请日:1994-09-02
发明人: SUZUKI, Fumio , KOIKE, Nobuaki , SHIMADA, Junichi , KITAMURA, Shigeto , ICHIKAWA, Shunji , NAKAMURA, Joji , SHIOZAKI, Shizuo
IPC分类号: C07D487/04 , A61K31/53
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 R1 represents hydrogen, (un)substituted lower alkyl or (un)substituted lower alkanoyl; R2 represents hydrogen, (un)substituted lower alkyl, (un)substituted lower alkenyl, (un)substituted cycloalkyl, (un)substituted aryl, (un)substituted aralkyl or (un)substituted heterocycle; R3 represents (un)substituted heterocycle; X represents a single bond, O, S, S(O), S(O)¿2? or NR?4¿, wherein R4 represents hydrogen or (un)substituted lower alkyl or R?2 and NR4¿ are combined with each other to form a 4- to 6-membered (un)substituted nitrogeneous saturated heterocyclic group; and A represents N or CR5, wherein R5 represents hydrogen or (un)substituted lower alkyl.
-
公开(公告)号:EP0698607B1
公开(公告)日:2002-05-29
申请号:EP95909968.0
申请日:1995-02-23
发明人: SUZUKI, Fumio , KOIKE, Nobuaki , SHIMADA, Junichi , NAKAMURA, Joji , SHIOZAKI, Shizuo , KITAMURA, Shigeto , ICHIKAWA, Shunji , KASE, Hiroshi , NONAKA, Hiromi
IPC分类号: C07D473/06 , A61K31/52
CPC分类号: C07D473/06
-
公开(公告)号:EP0667349A1
公开(公告)日:1995-08-16
申请号:EP94925620.0
申请日:1994-09-02
发明人: SUZUKI, Fumio , KOIKE, Nobuaki , SHIMADA, Junichi , KITAMURA, Shigeto , ICHIKAWA, Shunji , NAKAMURA, Joji , SHIOZAKI, Shizuo
IPC分类号: C07D487/04 , A61K31/53
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 1 represents hydrogen, (un)substituted lower alkyl or (un)substituted lower alkanoyl; R 2 represents hydrogen, (un)substituted lower alkyl, (un)substituted lower alkenyl, (un)substituted cycloalkyl, (un)substituted aryl, (un)substituted aralkyl or (un)substituted heterocycle; R 3 represents (un)substituted heterocycle; X represents a single bond, O, S, S(O), S(O) 2 or NR 4 , wherein R 4 represents hydrogen or (un)substituted lower alkyl or R 2 and NR 4 are combined with each other to form a 4- to 6-membered (un)substituted nitrogeneous saturated heterocyclic group; and A represents N or CR 5 , wherein R 5 represents hydrogen or (un)substituted lower alkyl.
摘要翻译: (I)表示的三嗪衍生物或其药理学上可接受的盐作为有效成分的抑郁症药物,其中R1表示氢,(未)取代的低级烷基或(未)取代的低级烷酰基; (未)取代的低级链烯基,(未)取代的环烷基,(未)取代的芳基,(未)取代的芳烷基或(未)取代的杂环; R3代表(未)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彼此结合形成4-6 (未)取代的氮杂饱和杂环基; A代表N或CR5,其中R5代表氢或(未)取代的低级烷基。
-
公开(公告)号:EP0603399A1
公开(公告)日:1994-06-29
申请号:EP93900411.5
申请日:1992-12-28
发明人: TANAKA, Takeo , MORISHITA, Yoshikazu , NOZAWA, Mika , CHIBA, Shigeru , KAWAMOTO, Isao , TSUKUDA, Eiji , YOSHIDA, Mayumi , SHIMAZAKI, Chieko , YAMAGUCHI, Kazuo , MATSUDA, Yuzuru , KITAMURA, Shigeto , IKEMURA, Toshihide , OGAWA, Tatsuhiro , YANO, Keiichi , SUZAWA, Toshiyuki , SHIBATA, Kenji , YAMASAKI, Motoo
IPC分类号: C12P21/00
CPC分类号: C07K7/06 , A61K38/00 , C07K5/1021 , C07K5/1024 , C07K7/08 , C07K14/36 , C07K14/57536
摘要: A novel peptide represented by the following general formula and a process for producing the same: X-A-Trp-B-Gly-Thr-E-G-Y wherein, A represents Asn or Asp; B represents His or Lys; E represents Ala or Ser; G represents Ala or Pro; X represents X¹-Gly or X³-Cys-X²; and Y represents hydroxy, lower alkoxy, amino, Y¹-Asp-Z or Y²-Cys-Z. The peptide is isolated from the product of culture of a streptomyces and has an endothelin antagonism and an activity of suppressing the rise of an intracellular calcium or cyclic guanosine-3,5-phosphate concentration caused by endothelin.
摘要翻译: 由以下通式表示的新肽及其制备方法:X-A-Trp-B-Gly-Thr-E-G-Y其中A表示Asn或Asp; B代表His或Lys; E表示Ala或Ser; G代表Ala或Pro; X表示X 1 -Gly或X 3 -Cys-X 2; Y表示羟基,低级烷氧基,氨基,Y 1 -Asp-Z或Y 2 -Cys-Z。 该肽从链霉菌培养物的产物中分离,具有内皮素拮抗作用和抑制由内皮素引起的细胞内钙或环鸟苷-3磷酸盐浓度升高的活性。
-
-
-
-
-