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公开(公告)号:US4839351A
公开(公告)日:1989-06-13
申请号:US941069
申请日:1986-12-12
IPC分类号: C07D519/06 , A61K31/545 , A61P31/04 , C07D463/00 , C07D501/36 , C07D505/00 , C07D519/00
CPC分类号: C07D505/00 , C07D463/22 , Y02P20/55
摘要: A compound of the general formula: ##STR1## wherein R.sup.0 is hydrogen, a nitrogen-containing heterocyclic group, an acyl group or an amino-protective group; A is S, S.fwdarw.O, O or CH.sub.2 ; R.sup.4 is hydrogen, methoxy group or formamido group; R.sup.13 is hydrogen, methyl, hydroxyl or a halogen; and A is an optionally substituted condensed cyclic group formed by combining an imidazole or pyrazole ring with 5- or 6-membered nitrogen-containing aromatic heterocyclic ring to share a C-N bond with each other,or a salt or ester thereof.and a process for preparing the same and a pharmaceutical composition thereof are disclosed.
摘要翻译: 通式为:其中R 0为氢,含氮杂环基,酰基或氨基保护基的化合物。 A是S,S-> O,O或CH 2; R4是氢,甲氧基或甲酰氨基; R 13是氢,甲基,羟基或卤素; A是通过将咪唑或吡唑环与5-或6-元含氮芳族杂环相结合而形成的任选取代的稠合环状基团,以共价C-N键或其盐或酯。 并公开了其制备方法及其药物组合物。
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公开(公告)号:US4921851A
公开(公告)日:1990-05-01
申请号:US396758
申请日:1989-08-22
IPC分类号: C07D501/00 , C07D501/46 , C07D519/00
CPC分类号: C07D501/46 , C07D501/00 , C07D519/00
摘要: This invention relates to a compound of the formula: ##STR1## wherein Q is nitrogen or CH; R.sup.1 is hydrogen or a lower alkyl group which may be substituted; and ring A is a pyridine or pyridazine ring which is substituted at the ring-constituting carbon atom by a group of the formula:--E--(CH.sub.2).sub.n --R.sup.2in which E is sulfur or NH; R.sup.2 is an amino, carbamoylamino, formylamino, acetylamino, N-formimidoylamino, N-acetimidoylamino, lower alkylamino, hydroxyl or carbamoyloxy group; and n is an integer of 2 to 4, or a pharmaceutically acceptable salt thereof. The compound (I) or a pharmaceutically acceptable sale thereof has excellent antibacterial activity and is used as antibiotics.
摘要翻译: 本发明涉及下式的化合物:其中Q是氮或CH; R1是氢或可被取代的低级烷基; 环A为吡啶或哒嗪环,其在环的构成碳原子上被下列基团取代:其中E为硫或NH的-E-(CH2)n-R2; R2是氨基,氨基甲酰基氨基,甲酰氨基,乙酰氨基,N-甲脒基氨基,N-亚氨代乙酰氨基,低级烷基氨基,羟基或氨基甲酰氧基; n为2〜4的整数,或其药学上可接受的盐。 化合物(I)或其药学上可接受的销售具有优异的抗菌活性并用作抗生素。
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公开(公告)号:US4797395A
公开(公告)日:1989-01-10
申请号:US886814
申请日:1986-07-18
申请人: Akio Miyake , Yoshinobu Yoshimura , Mitsuo Numata
发明人: Akio Miyake , Yoshinobu Yoshimura , Mitsuo Numata
IPC分类号: A61K31/545 , C07D501/36 , C07D501/56
CPC分类号: C07D501/36
摘要: A compound of the formula ##STR1## wherein (1) R.sub.1 is a lower alkyl group of 2 to 6 carbon atoms or a cycloalkyl group of 5 to 7 carbon atoms and R.sub.2 is a cycloalkyl group of 5 to 7 carbon atoms or a lower alkyl group of 1 to 3 carbon atoms which is substituted by a cycloalkyl group of 5 to 7 carbon atoms or by a phenyl group, or (2) R.sub.1 is a cycloalkyl group of 5 to 7 carbon atoms and R.sub.2 is a lower alkyl group of 1 to 5 carbon atoms, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.
摘要翻译: 式(Ⅰ)化合物其中(1)R 1为2〜6个碳原子的低级烷基或5〜7个碳原子的环烷基,R 2为5〜7个碳原子的环烷基 原子或碳原子数为5〜7的环烷基取代的1〜3个碳原子的低级烷基或苯基,或(2)R 1为5〜7个碳原子的环烷基,R 2为 提供1〜5个碳原子的低级烷基或其药学上可接受的盐,其制备方法及其药物组合物。 该化合物可口服施用,具有改善生物利用度的抗生素。
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公开(公告)号:US5519024A
公开(公告)日:1996-05-21
申请号:US207091
申请日:1994-03-08
申请人: Akio Miyake , Masahira Nakamura , Hideto Fukushi
发明人: Akio Miyake , Masahira Nakamura , Hideto Fukushi
IPC分类号: C07D215/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/06 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D513/04 , C07D519/00 , C07D417/04 , A61K31/495
CPC分类号: C07D401/04 , C07D215/56 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/06 , C07D417/14 , C07D471/04 , C07D471/06 , C07D487/04 , C07D513/04
摘要: A composition comprises a 1,7-disubstituted-4-oxo-3-quinolinecarboxylic acid or 1,7-disubstituted-4-oxo-3-naphthyridinecarboxylic acid derivative which is useful as a prophylactic and/or therapeutic agent for peripheral arterial obstruction, acute myocardial infarction, an antitumor agent, and as a prophylactic and/or therapeutic agent for osteoporosis.
摘要翻译: 组合物包含可用作外周动脉阻塞的预防和/或治疗剂的1,7-二取代-4-氧代-3-喹啉羧酸或1,7-二取代-4-氧代-3-萘啶羧酸衍生物, 急性心肌梗死,抗肿瘤剂,以及作为骨质疏松症的预防和/或治疗剂。
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公开(公告)号:US5145850A
公开(公告)日:1992-09-08
申请号:US659704
申请日:1991-02-25
申请人: Akio Miyake , Yasuko Ashida
发明人: Akio Miyake , Yasuko Ashida
IPC分类号: A61K31/50 , A61K31/5025 , A61P11/00 , A61P11/06 , A61P11/08 , A61P29/00 , A61P37/08 , C07D487/04
CPC分类号: C07D487/04
摘要: An imidazo [1,2-b]pyridazine compound of the formula (I): ##STR1## wherein R.sub.1 is a halogen atom or a lower alkyl group optionally having substituent(s), R.sub.2 and R.sub.3 are, independently, a hydrogen atom, a lower alkyl group optionally having substituent(s), a cycloalkyl group or a phenyl group optionally having substituent(s) or R.sub.2 and R.sub.3 together with the adjacent nitrogen atom to which they bond may form a heterolcyclic ring optionally having substituent(s), X is an oxygen atom or S(O).sub.k (k is zero to two), a group --.circle.A-- is a bivalent three to seven membered homocyclic or heterocyclic group optionally having substituent(s), m.sup.1 and m.sup.2 each is an integer of 0 to 4 and n is an integer of 0 or 1; or its salt, which is useful as antiasthmatics.
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公开(公告)号:US4864022A
公开(公告)日:1989-09-05
申请号:US834969
申请日:1986-02-28
申请人: Akio Miyake , Masahiro Kondo , Masahiko Fujino
发明人: Akio Miyake , Masahiro Kondo , Masahiko Fujino
IPC分类号: C07D501/06 , A61K31/545 , A61K31/546 , C07D277/20 , C07D285/08 , C07D463/00 , C07D471/04 , C07D487/04 , C07D498/04 , C07D501/46 , C07D505/00 , C07D519/00
CPC分类号: C07D277/587 , C07D285/08 , C07D463/20 , C07D463/22 , C07D471/04 , C07D487/04 , C07D505/00
摘要: A compound of the formula; ##STR1## wherein R.sup.1 is an amino group which may be protected, R.sup.3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S.fwdarw.O, O or CH.sub.2, R.sup.4 is a hydrogen atom, methoxy group or formamido group, R.sup.13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A.sym. is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.
摘要翻译: 式的化合物; 其中R 1为可被保护的氨基,R 3为氢原子或任选取代的烃残基; Z是S,S-> O,O或CH2,R4是氢原子,甲氧基或甲酰氨基,R13是氢原子,甲基,羟基或卤素原子,A(+)是任选取代的咪唑鎓 - 在2,3-或3,4-位上形成稠合环或其药学上可接受的盐或酯是新的,具有优异的抗菌活性。
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公开(公告)号:US5948774A
公开(公告)日:1999-09-07
申请号:US836424
申请日:1997-07-29
申请人: Keiji Kamiyama , Kenji Okonogi , Akio Miyake
发明人: Keiji Kamiyama , Kenji Okonogi , Akio Miyake
IPC分类号: C07D501/00 , C07D501/24 , A61K31/545
CPC分类号: C07D501/00
摘要: Cephem compounds of the formula: ##STR1## wherein R.sup.1 is an optionally protected amino group; R.sup.2 is a fluoro-lower alkyl group; and the ring A may have further substituent(s), or their esters or salts, show broad and excellent antibacterial activities and are useful as antibacterial agents.
摘要翻译: PCT No.PCT / JP96 / 01436 Sec。 371日期1997年7月29日第 102(e)日期1997年7月29日PCT提交1996年5月28日PCT公布。 WO96 / 34851 PCT出版物 日期:1996年12月5日化学式:其中R1为任选保护的氨基; R2是氟代低级烷基; 并且环A可以具有其它取代基或其酯或盐,显示出广泛和优异的抗菌活性并且可用作抗菌剂。
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公开(公告)号:US5492909A
公开(公告)日:1996-02-20
申请号:US225981
申请日:1994-04-12
申请人: Akio Miyake , Masahiro Kajino , Yasuko Ashida
发明人: Akio Miyake , Masahiro Kajino , Yasuko Ashida
IPC分类号: C07D487/04 , A61K31/50 , A61K31/535 , C07D487/14
CPC分类号: C07D487/04
摘要: A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 are a hydrogen atom, a lower alkyl group or a 5- to 7-membered cyclic group formed together with the adjacent --C.dbd.C--; X is an oxygen atom, a sulfur atom or a methylene group; Y is an optionally substituted methylene group, a divalent 3- to 7-membered homo- or heterocyclic group; R.sup.6 and R.sup.7 are a hydrogen atom, a lower alkyl group, a cycloalkyl group, an aryl group, or a nitrogen-containing heterocyclic group formed together With the adjacent nitrogen atom; m is an integer of 0 to 4; and n is an integer of 0 to 4, or a salt thereof. Said compound has an excellent anti-PAF activity, antiallergic action, etc., thus is useful as an antiasthmatic agent.
摘要翻译: 下式的化合物:其中R 1是氢原子,低级烷基或卤素原子; R2和R3是与相邻的-C = C-一起形成的氢原子,低级烷基或5-至7-元环基; X是氧原子,硫原子或亚甲基; Y是任选取代的亚甲基,二价3-至7-元同 - 或杂环基; R6和R7是与相邻的氮原子一起形成的氢原子,低级烷基,环烷基,芳基或含氮杂环基; m为0〜4的整数。 n为0〜4的整数,或其盐。 所述化合物具有优异的抗PAF活性,抗过敏作用等,因此可用作抗哮喘药。
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公开(公告)号:US4962100A
公开(公告)日:1990-10-09
申请号:US331192
申请日:1989-03-28
申请人: Akio Miyake , Masahiro Kondo , Masahiko Fujino
发明人: Akio Miyake , Masahiro Kondo , Masahiko Fujino
IPC分类号: C07D501/06 , A61K31/545 , A61K31/546 , C07D277/20 , C07D285/08 , C07D463/00 , C07D471/04 , C07D487/04 , C07D498/04 , C07D501/46 , C07D505/00 , C07D519/00
CPC分类号: C07D277/587 , C07D285/08 , C07D463/20 , C07D463/22 , C07D471/04 , C07D487/04 , C07D505/00
摘要: A compound of the formula: ##STR1## wherein R.sup.1 is an amino group which may be protected, R.sup.3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S.fwdarw.O, O or CH.sub.2, R.sup.4 is a hydrogen atom, methoxy group or formamido group, R.sup.13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A.sup..sym. is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.
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公开(公告)号:US4725592A
公开(公告)日:1988-02-16
申请号:US637138
申请日:1984-08-03
申请人: Akio Miyake , Masayoshi Yamaoka , Mitsuo Numata
发明人: Akio Miyake , Masayoshi Yamaoka , Mitsuo Numata
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36 , C07D501/56
CPC分类号: C07D501/36
摘要: A compound of the formula: ##STR1## wherein R.sub.1 stands for n-propyl or isopropyl; and R.sub.2 stands for n-butyl, isobutyl, n-pentyl, n-hexyl or 2-ethylbutyl, or a pharmaceutically acceptable salt thereof, processes for preparing the same and a pharmaceutical composition thereof are provided. The compound can orally be applied as antibiotics having improved bioavailability.
摘要翻译: 下式的化合物:其中R 1代表正丙基或异丙基; R2代表正丁基,异丁基,正戊基,正己基或2-乙基丁基,或其药学上可接受的盐,其制备方法及其药物组合物。 该化合物可口服施用,具有改善生物利用度的抗生素。
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