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公开(公告)号:US5527908A
公开(公告)日:1996-06-18
申请号:US94106
申请日:1993-08-05
申请人: Fumio Suzuki , Yoshisuke Nakasato , Kenji Ohmori , Tadafumi Tamura , Soichiro Sato , Hiroshi Tanaka
发明人: Fumio Suzuki , Yoshisuke Nakasato , Kenji Ohmori , Tadafumi Tamura , Soichiro Sato , Hiroshi Tanaka
IPC分类号: C07D513/14 , A61K31/505
CPC分类号: C07D513/14
摘要: Pyrazolothiazolopyrimidine derivatives represented by the Formula ##STR1## and pharmaceutically acceptable salts thereof are useful as anti-inflammatory, analgesic, immunomodulatory and anti-ulcer agents.
摘要翻译: PCT No.PCT / JP92 / 01595 Sec。 371日期:1993年8月5日 102(e)日期1993年8月5日PCT提交1992年12月7日PCT公布。 公开号WO93 / 12120 PCT 日期:1992年6月24日。由式< IMAGE>表示的吡唑并噻唑并嘧啶衍生物及其药学上可接受的盐可用作抗炎,镇痛,免疫调节和抗溃疡剂。
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公开(公告)号:US5371225A
公开(公告)日:1994-12-06
申请号:US170192
申请日:1993-12-22
申请人: Fumio Suzuki , Yoshisuke Nakasato , Hiroshi Tsumuki , Kenji Ohmori , Hiroshi Nakajima , Tadafumi Tamura , Soichiro Sato
发明人: Fumio Suzuki , Yoshisuke Nakasato , Hiroshi Tsumuki , Kenji Ohmori , Hiroshi Nakajima , Tadafumi Tamura , Soichiro Sato
IPC分类号: A61K31/00 , A61K31/47 , A61K31/55 , C07D221/18 , A61K31/44
CPC分类号: C07D221/18
摘要: The present invention relates to novel tetracyclic compounds represented by formula (I) ##STR1## (wherein each of X.sup.1 and X.sup.2 independently represents hydrogen or lower alkyl; n represents an integer of 1 to 4), or a pharmaceutically acceptable salt thereof, which are useful as immunosuppressive agents.
摘要翻译: PCT No.PCT / JP93 / 00527 Sec。 371日期:1993年12月22日 102(e)日期1993年12月22日PCT 1993年4月23日PCT公布。 公开号WO93 / 22286 日本公开专利文献1:日本专利公开1 9 9 3年11月11日本发明涉及式(I)表示的新型四环化合物(Ⅰ)(其中X1和X2各自独立地表示氢或低级烷基; n表示1〜4的整数) ,或其药学上可接受的盐,其可用作免疫抑制剂。
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公开(公告)号:US5646283A
公开(公告)日:1997-07-08
申请号:US436370
申请日:1995-05-22
申请人: Fumio Suzuki , Yoshisuke Nakasato , Hiroshi Tsumuki , Soichiro Sato , Tadafumi Tamura , Hiroshi Nakajima
发明人: Fumio Suzuki , Yoshisuke Nakasato , Hiroshi Tsumuki , Soichiro Sato , Tadafumi Tamura , Hiroshi Nakajima
IPC分类号: C07D221/18 , C07D401/04 , C07D409/04
CPC分类号: C07D401/04 , C07D221/18 , C07D409/04
摘要: This invention relates to a novel tetracyclic compound represented by formula (I): ##STR1## or its pharmacologically-acceptable salt. The compound of this invention has strong immunosuppressive activity, and is useful as an immunosuppressive agent and as an agent for treating autoimmune disease.
摘要翻译: PCT No.PCT / JP94 / 01591 Sec。 371日期:1995年5月22日 102(e)日期1995年5月22日PCT 1994年9月28日PCT公布。 出版物WO95 / 09153 日期1995年4月6日本发明涉及由式(I)表示的新颖的四环化合物:其IMA或其药理学上可接受的盐。 本发明的化合物具有强的免疫抑制活性,可用作免疫抑制剂和作为治疗自身免疫性疾病的药物。
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公开(公告)号:US5192768A
公开(公告)日:1993-03-09
申请号:US757988
申请日:1991-09-12
申请人: Fumio Suzuki , Yoshisuke Nakasato , Kenji Ohmori , Tadafumi Tamura , Hisashi Hosoe , Kazuhiro Kubo , Ikufumi Yoshitake
发明人: Fumio Suzuki , Yoshisuke Nakasato , Kenji Ohmori , Tadafumi Tamura , Hisashi Hosoe , Kazuhiro Kubo , Ikufumi Yoshitake
IPC分类号: C07D471/04
CPC分类号: C07D471/04
摘要: A pyrazoloquinoline derivative having the formula (I): ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 independently represent a hydrogen atom or a lower alkyl group; R.sup.4 represents a hydrogen atom, a lower alkyl group, a halogen-substituted lower alkyl group, or a lower alkoxycarbonyl group; the dotted line means that the pyrazole ring has two conjugated double bonds; and R.sup.4 is bonded to the nitrogen atom at the 1-position or 2-position, or pharmacologically acceptable salts thereof. These compounds exhibit excellent anti-inflammatory activity and hepatic insufficiency treating activity.
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公开(公告)号:US06716987B1
公开(公告)日:2004-04-06
申请号:US10023091
申请日:2001-12-20
申请人: Etsuo Ohshima , Takashi Kawakita , Koji Yanagawa , Kyoichiro Iida , Rie Koike , Yoshisuke Nakasato , Tohru Matsuzaki , Kenji Ohmori , Soichiro Sato , Hidee Ishii , Haruhiko Manabe , Michio Ichimura , Fumio Suzuki
发明人: Etsuo Ohshima , Takashi Kawakita , Koji Yanagawa , Kyoichiro Iida , Rie Koike , Yoshisuke Nakasato , Tohru Matsuzaki , Kenji Ohmori , Soichiro Sato , Hidee Ishii , Haruhiko Manabe , Michio Ichimura , Fumio Suzuki
IPC分类号: C07D41300
CPC分类号: C07D307/79 , C07D307/94 , C07D405/06 , C07D405/12 , C07D405/14
摘要: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CONH, CONHCH2, or a bond), or N], or (iii) a bond; and R5 represents aryl, an aromatic heterocyclic group, cycloalkyl, pyridine-N-oxide, cyano, or lower alkoxycarbonyl; or pharmaceutically acceptable salts thereof.
摘要翻译: 由下式(I)表示的含氧杂环化合物:其中R 1和R 2独立地表示氢,低级烷基,氰基, - (CH 2)nE 1 -CO-G 1(其中 E 1表示键,O或NH;且G 1表示氢,取代或未取代的低级烷基,OR 6或NR 7 R 8; n表示0〜 4)等; R 1和R 2相互结合形成饱和碳环和与其相邻的碳原子。 或R 2,以及下述R 11或R 13组合形成单键; R 3表示氢,苯基或卤素; R 4表示羟基,低级烷氧基等; A表示-C(R 9)(R 10) - 或O; B表示O,NR 11,-C(R 12)(R 13) - 或-C(R 14)(R 15)-C(R 16)(R 16) <17>) - ; D表示(i)-C(R 18)(R 19)-X-(其中X表示-C(R 21)(R 22) - ,S或NR 23) ,(ii)-C(R 19)= Y- [Y表示-C(R 24) - Z-(其中Z表示CONH,CONHCH 2或键)或N]或(iii) 一个债券 R 5表示芳基,芳香族杂环基,环烷基,吡啶-N-氧化物,氰基或低级烷氧基羰基; 或其药学上可接受的盐。
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公开(公告)号:US06514996B2
公开(公告)日:2003-02-04
申请号:US08974739
申请日:1997-11-19
申请人: Etsuo Ohshima , Takashi Kawakita , Koji Yanagawa , Kyoichiro Iida , Rie Koike , Yoshisuke Nakasato , Tohru Matsuzaki , Kenji Ohmori , Soichiro Sato , Hidee Ishii , Haruhiko Manabe , Michio Ichimura , Fumio Suzuki
发明人: Etsuo Ohshima , Takashi Kawakita , Koji Yanagawa , Kyoichiro Iida , Rie Koike , Yoshisuke Nakasato , Tohru Matsuzaki , Kenji Ohmori , Soichiro Sato , Hidee Ishii , Haruhiko Manabe , Michio Ichimura , Fumio Suzuki
IPC分类号: A61K3144
CPC分类号: C07D307/79 , C07D307/94 , C07D405/06 , C07D405/12 , C07D405/14
摘要: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CONH, CONHCH2, or a bond), or N], or (iii) a bond; and R5 represents aryl, an aromatic heterocyclic group, cycloalkyl, pyridine-N-oxide, cyano, or lower alkoxycarbonyl; or pharmaceutically acceptable salts thereof.
摘要翻译: 由下式(I)表示的含氧杂环化合物:其中R1和R2独立地表示氢,低级烷基,氰基, - (CH2)n-E1-CO-G1(其中E1表示键,O或NH; 并且G 1表示氢,取代或未取代的低级烷基,OR 6或NR 7 R 8; n表示0〜4的整数)等。 R 1和R 2组合在一起,与邻近的碳原子一起代表饱和碳环; 或R 2,R 11或R 13组合形成单键; R3表示氢,苯基或卤素; R4代表羟基,低级烷氧基等; A表示-C(R 9)(R 10) - 或O; B表示O,NR 11,-C(R 12)(R 13) - 或-C(R 14)(R 15)-C(R 16)(R 17) - ; D表示(i)-C(R 18)(R 19)-X-(其中X表示-C(R 21)(R 22) - ,S或NR 23),(ⅱ)-C(R 19a)= Y- [Y -C(R 24)-Z-(其中Z表示CONH,CONHCH 2或键)或N]或(iii)键; R5表示芳基,芳香族杂环基,环烷基,吡啶-N-氧化物,氰基或低级烷氧基羰基; 或其药学上可接受的盐。
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公开(公告)号:US5010084A
公开(公告)日:1991-04-23
申请号:US553551
申请日:1990-07-18
IPC分类号: A61K31/00 , A61K31/47 , A61K31/4738 , A61K31/4745 , A61P11/00 , A61P11/06 , A61P11/08 , A61P37/00 , A61P37/08 , C07D471/04
CPC分类号: C07D471/04
摘要: Novel imidazoquinolone derivative represented by formula (I); ##STR1## wherein R.sup.1 represents lower alkyl or --(CH.sub.2).sub.m CO--R.sup.3 where R.sup.3 represents hydrogen, lower alkyl, hydroxy or lower alkoxy; and m is an integer of 1 to 3; R.sup.2 represents lower alkyl; or a pharmaceutically acceptable salt thereof.
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公开(公告)号:US5126341A
公开(公告)日:1992-06-30
申请号:US684214
申请日:1991-04-12
申请人: Fumio Suzuki , Takeshi Kuroda , Kenji Ohmori , Tadafumi Tamura , Hisashi Hosoe
发明人: Fumio Suzuki , Takeshi Kuroda , Kenji Ohmori , Tadafumi Tamura , Hisashi Hosoe
IPC分类号: A61K31/435 , A61K31/00 , A61K31/4353 , A61K31/4375 , A61K31/44 , A61K31/4427 , A61K31/444 , A61K31/495 , A61K31/4965 , A61K31/497 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P29/00 , A61P37/00 , A61P37/08 , C07D471/04
CPC分类号: C07D471/04
摘要: Disclosed are naphthyridine derivatives represented by formula (I) ##STR1## wherein: X represents hydrogen; lower alkyl; aralkyl; substituted or unsubstituted aryl; substituted or unsubstituted aromatic heterocyclic group; --NR.sup.1 R.sup.2 wherein R.sup.1 and R.sup.2 independently represent hydrogen or lower alkyl; ##STR2## wherein W represents N or CH, Z represents a single bond, oxygen or NR.sup.3 (wherein R.sup.3 represents hydrogen, lower alkyl or benzyl) and n1 and n2 represent an integer of 1 to 3; or substituted or unsubstituted thiazolinyl; andY is a single bond or alkylene and pharmaceutically acceptable salts thereof. The compounds show potent anti-inflammatory activity and are expected to be useful in treating rheumarthritis.
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公开(公告)号:US5173492A
公开(公告)日:1992-12-22
申请号:US752180
申请日:1991-08-23
申请人: Fumio Suzuki , Junichi Shimada , Kenji Ohmori , Haruhiko Manabe , Kazuihiro Kubo , Akira Karasawa , Tetsuji Ohno , Shizuo Shiozaki , Akio Ishii , Katsuichi Shuto
发明人: Fumio Suzuki , Junichi Shimada , Kenji Ohmori , Haruhiko Manabe , Kazuihiro Kubo , Akira Karasawa , Tetsuji Ohno , Shizuo Shiozaki , Akio Ishii , Katsuichi Shuto
IPC分类号: C07D471/14
CPC分类号: C07D471/14
摘要: There are disclosed s-triazolo[3,4-i]purine derivatives represented by formula: ##STR1## wherein Y-Z represents ##STR2## R.sub.4 represents hydrogen, alkyl, substituted or unsubstituted aromatic heterocyclic group or substituted or unsubstituted aryl; and X.sup.2 represents oxygen, sulfur or NH; each of R.sup.1 and R.sup.2 independently represents hydrogen, alkyl, cycloalkyl, aralkyl or substituted or unsubstituted aryl; R.sup.3 represents alkyl, cycloalkyl, aralkyl or substituted or unsubstituted aryl; X.sup.1 represents oxygen or sulfur; and represents a single bond or a double bond or pharmaceutically acceptable salts thereof.
摘要翻译: 公开了由下式表示的三唑并[3,4-i]嘌呤衍生物:其中Y-Z表示R 4表示氢,烷基,取代或未取代的芳族杂环基或取代或未取代的芳基; X2表示氧,硫或NH; R 1和R 2各自独立地表示氢,烷基,环烷基,芳烷基或取代或未取代的芳基; R3表示烷基,环烷基,芳烷基或取代或未取代的芳基; X1表示氧或硫; 并且表示单键或双键或其药学上可接受的盐。
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公开(公告)号:US4994468A
公开(公告)日:1991-02-19
申请号:US489025
申请日:1990-03-05
IPC分类号: C07D471/04
CPC分类号: C07D471/04
摘要: Novel imidazoquinolone derivative represented by the formula (I); ##STR1## wherein R.sup.1 represents hydrogen, alkyl, cycloalkyl, alkenyl aralkyl, aralkenyl or substituted or unsubstituted aryl; X represents nitrogen or ##STR2## where R.sup.2 is hydrogen, hydroxyl, alkyl, cycloalkyl, alkenyl, aralkyl, aralkenyl, substituted or unsubstituted aryl, thiol, halogen, substituted or unsubstituted aromatic heterocyclic group, or --(CH.sub.2).sub.m CO.sub.2 R.sup.6 where R.sup.6 is hydrogen or lower alkyl and m is an integer of 0 to 3; Y represents oxygen or sulfur; R.sup.3 represents alkyl, cycloalkyl, alkoxyalkly, alkenyl, aralkyl, aralkenyl, --(CH.sub.2).sub.n -- Het where Het is substituted or unsubstituted aromatic heterocyclic group and n is an integer of 1 to 3 or --(CH.sub.2).sub.n CO.sub.2 R.sup.6a where n has the same meaning as defined above and R.sup.6a has the same meaning as defined as to R.sup.6 ; each of R.sup.4 and R.sup.5 independently represents hydrogen, lower alkyl, trifluoromethyl, cycloalkyl, halogen, hydroxyl, lower alkoxyl, lower alkylthio, nitro, amino, lower alkylamino, lower alkanoylamino, aroylamino, lower alkanoyl or aroyl; and a pharmaceutically acceptable salt thereof. The Compound (I) and a pharmaceutically acceptable salt thereof show bronchodilatory and antiallergic activities, and are useful for treating respiratory disorders such as bronchial asthma.
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