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1. 发明授权

US5556861A 1,8 benzonaphthyridine derivatives and antimicrobial compositions 失效
标题翻译： 1,8苯并萘啶衍生物和抗微生物组合物
公开(公告)号：US5556861A
公开(公告)日：1996-09-17
申请号：US472766
申请日：1995-06-07
申请人： Eric Bacque , Michel Barreau , Jean-Francois Desconclois , Philippe Girard , Michel Kryvenko , Marc P. Lavergne , Jean-Marc Paris , Guy Picaut
发明人： Eric Bacque , Michel Barreau , Jean-Francois Desconclois , Philippe Girard , Michel Kryvenko , Marc P. Lavergne , Jean-Marc Paris , Guy Picaut
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： This invention relates to a novel 1,8 benzo[b]naphythyridine derivative of general formula (I), ##STR1## wherein R is H or a hydroxy, amino or alkylamino radical optionally substituted by amino or hydroxy, or R is dialkylamino of which the alkyl portions may form, with the nitrogen atom, a 5- or 6-membered heterocyclic ring which optionally contains a further heteroatom chosen from nitrogen, oxygen or sulphur, or R is C.sub.3-6 cycloalkylamino or an alkanylamino, N-alkyl N-alkanylamino or aminoalkylphenylamino radical; R.sub.1 and R.sub.2, which are the same or different, are in positions 2 and 3 and represent H, alkyl, C.sub.2-4 alkenyl, phenyl, or substituted phenyl, or R.sub.1 and R.sub.2 are in position 2 and represent alkyl; R.sub.3 is H or alkyl, fluoroalkyl, carboxyalkyl, C.sub.3-6 cycloalkyl, fluorophenyl, difluorophenyl, alkyloxy or alkylamino; and R.sub.4 is H or F, wherein the C.sub.1-4 alkanyl and alkyl radicals are linear or branched; stereoisomeric forms thereof or mixtures of these; and salts and hydrated forms thereof. These novel derivatives are useful as antimicrobials.
摘要翻译：本发明涉及通式（I）的新颖的1,8-苯并[b]萘啶衍生物，其中R是H或羟基，任选被氨基或羟基取代的氨基或烷基氨基，或R是烷基部分可以与氮原子形成的二烷基氨基，其任选地含有选自氮，氧或硫的另外的杂原子的5-或6-元杂环，或R是C 3-6环烷基氨基或烷基氨基，烷基N-烷基氨基或氨基烷基苯基氨基; R1和R2相同或不同，位于2和3位，代表H，烷基，C2-4烯基，苯基或取代苯基，或R1和R2位于2位，代表烷基; R3是H或烷基，氟代烷基，羧基烷基，C3-6环烷基，氟苯基，二氟苯基，烷氧基或烷基氨基; R4是H或F，其中C1-4烷基和烷基是直链或支链的; 其立体异构形式或它们的混合物; 及其盐和水合形式。这些新型衍生物可用作抗微生物剂。

2. 发明授权

US5053509A Benzo[1,8]naphthyridine derivatives, their preparation and compositions containing them 失效
标题翻译：苯并[1,8]萘啶衍生物，其制备方法和含有它们的组合物
公开(公告)号：US5053509A
公开(公告)日：1991-10-01
申请号：US605340
申请日：1990-10-30
申请人： Michel Antoine , Michel Barreau , Jean-Francois Desconclois , Philippe Girard , Guy Picaut
发明人： Michel Antoine , Michel Barreau , Jean-Francois Desconclois , Philippe Girard , Guy Picaut
IPC分类号： C07D401/14 , A61K31/4375 , A61K31/44 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/54 , A61P31/04 , A61P31/12 , C07D471/04
CPC分类号： C07D471/04
摘要： New benzo[b][1,8]naphthyridine derivatives of general formula (I), in which R.sub.1 is a hydrogen atom or a hydroxyl or alkyl radical, R.sub.2 is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkyloxy or alkylamino radical, R.sub.3 is a phenyl or phenylalkyl radical substituted with one or more halogen atoms or alkyl, cycloalkyl (3 to 6 C), alkyloxy, cyano, amino, alkylamino, dialkylamino, alkyloxyalkyl, hydroxyalkyl, hydroxyalkyloxy, methylenedioxy, aminoalkyl, alkylaminoalkyl or dialkylaminoalkyl radicals, or R.sub.3 is a heterocyclic radical, and R.sub.4 is a hydrogen atom or a fluorine atom, the alkyl radicals (1 to 4 C) being linear or branched, their salts, their preparation and compositions containing them.These new products are useful as antimicrobials, or in the treatment of AIDS. ##STR1##
摘要翻译：其中R1是氢原子或羟基或烷基的新的苯并[b] [1,8]萘啶衍生物，其中R 2是氢原子或烷基，氟烷基，环烷基（3至6个碳原子），烷氧基或烷基氨基，R3是被一个或多个卤素原子或烷基，环烷基（3至6个C），烷氧基，氰基，氨基，烷基氨基，二烷基氨基，烷氧基烷基，羟基烷基，羟基烷氧基，亚甲二氧基，氨基烷基，烷基氨基烷基或二烷基氨基烷基，或R3是杂环基，R4是氢原子或氟原子，烷基（1-4C）是直链或支链的，它们的盐，它们的制备和含有它们的组合物。这些新产品可用作抗菌药物或用于治疗艾滋病。（一）

3. 发明授权

US4513001A .beta.-Adrenergic 1-[1-benzimidazolyl]-N-[2-(4-hydroxy-3-methoxy-phenyl)-2-hydroxy-ethyl]- 3-amino butane and salts and hydrates thereof 失效
标题翻译： β-肾上腺素能1- [1-苯并咪唑基] -N- [2-（4-羟基-3-甲氧基 - 苯基）-2-羟基 - 乙基] -3-氨基丁烷及其盐和水合物
公开(公告)号：US4513001A
公开(公告)日：1985-04-23
申请号：US477680
申请日：1983-03-22
申请人： Michel Joannic , Francoise Roquet , Marcel Pesson
发明人： Michel Joannic , Francoise Roquet , Marcel Pesson
IPC分类号： C07D235/08 , A61K31/415 , A61K31/4184 , A61P11/00 , A61P13/02 , A61P15/00 , C07C45/28 , C07C45/63 , C07C45/71 , C07C49/84 , C07C49/86 , C07D235/04 , C07D235/06
CPC分类号： C07D235/06 , C07C45/28 , C07C45/63 , C07C45/71 , C07C49/84 , C07C49/86 , Y10S514/826
摘要： Novel compounds with .beta.-adrenergic properties comprising 1-[1-benzimidazolyl] N-[2-(4-hydroxy 3-methoxy phenyl) 2-hydroxy ethyl]3-amino butane, corresponding to the following formula ##STR1## as well as its addition salts with pharmaceutically acceptable non-toxic inorganic or organic acids, and the hydrates of said salts. These compounds are particularly useful for the treatment of asthma and in the case of premature labor.
摘要翻译：具有β-肾上腺素能性质的新型化合物包含1- [1-苯并咪唑基] -N- [2-（4-羟基-3-甲氧基苯基）-2-羟基乙基] 3-氨基丁烷，对应于下列化学式以及其与药学上可接受的无毒或无机酸的加成盐和所述盐的水合物。这些化合物特别适用于治疗哮喘和早产的情况。

4. 发明授权

US4442101A Sesquihydrate of naphthyridine derivative, and process for the preparation thereof 失效
标题翻译：萘啶衍生物的倍半水合物及其制备方法
公开(公告)号：US4442101A
公开(公告)日：1984-04-10
申请号：US345916
申请日：1982-02-04
申请人： Hitoshi Ichihashi , Terukazu Tanaka , Yu Imasato
发明人： Hitoshi Ichihashi , Terukazu Tanaka , Yu Imasato
IPC分类号： C07D487/04 , A61K31/495 , A61P31/04 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04
CPC分类号： C07D213/73 , C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04
摘要： Novel 1-ethyl-6-fluoro-1,4-dihyono-4-oxo -7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid.sesquihydrate (ATT-2266.sesquihydrate). The aforesaid compound can be prepared by heating 1-ethyl-6-fluoro-1,4-dihydro-4-oxo -7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid at a temperature above about 60.degree. C. in the presence of water in an amount sufficient to form the sesquihydrate. This sesquihydrate is much more stable than the anhydrate and the trihydrate and is superior to the anhydrate in the rate of dissolution and transference into the body through the intestines. Thus, it is especially useful as a pharmaceutical compound.
摘要翻译：新的1-乙基-6-氟-1,4-二氢化-4-氧代-7-（1-哌嗪基）-1,8-萘啶-3-羧酸二水合物（ATT-2266，水合二水合物）。上述化合物可以通过在高于约60℃的温度下加热1-乙基-6-氟-1,4-二氢-4-氧代-7-（1-哌嗪基）-1,8-二氮杂萘-3-羧酸来制备在水存在下，其量足以形成倍半水合物。这种倍半水合物比无水物和三水合物更稳定，并且在溶解速率和通过肠中转移到体内优于无水物质。因此，作为药物化合物是特别有用的。

5. 发明授权

US4359578A Naphthyridine derivatives and salts thereof useful as antibacterial agents 失效
标题翻译：萘吡啶衍生物及其盐可用作抗菌剂
公开(公告)号：US4359578A
公开(公告)日：1982-11-16
申请号：US68966
申请日：1979-08-23
申请人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
发明人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
IPC分类号： C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04 , A61K31/495
CPC分类号： C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04 , Y10S514/96 , Y10S514/962
摘要： This invention relates to 1,8-naphthyridine compounds of the formula ##STR1## wherein X is a halogen atom especially fluorine atom,R.sub.1 is an ethyl group or a vinyl group, andR.sub.2 is a hydrogen atom or a lower alkyl group, their salts and processes for the preparation of them.The 1,8-naphthyridine compounds and their salts are useful as antibacterial agents and intermediates thereof.

6. 发明授权

US5225207A Complexes derived from platinum, their preparation and the pharmaceutical compositions which contain them 失效
标题翻译：衍生自铂的复合物，其制备物和含有它们的药物组合物
公开(公告)号：US5225207A
公开(公告)日：1993-07-06
申请号：US775410
申请日：1991-10-15
申请人： Michel Barreau , Jean-Claude Chottard , Jean-Bernard Le Peco , Patrick Mailliet
发明人： Michel Barreau , Jean-Claude Chottard , Jean-Bernard Le Peco , Patrick Mailliet
IPC分类号： C07F15/00
CPC分类号： C07F15/0093
摘要： New complexes of general formula (I) in whichR.sub.1 and R.sub.2 together form a saturated or unsaturated polycyclic carbocyclic radical containing 7 to 12 carbon atoms, or a saturated or partially saturated mono-, bi- or tricyclic heterocyclic radical containing 5 to 11 chain members and a hetero-atom chosen from oxygen, sulphur or nitrogen, which latter atom can optionally be substituted by an alkoxycarbonyl radical, and,X.sub.1 and X.sub.2 represent chlorine atoms or together formeither a radical of structure: ##STR1## in which n is 0 to 2 and R.sub.6 and R.sub.7, which are identical or different, are hydrogen atoms or, when n=1, can be alkyl radicals or form, together with the carbon atom to which they are attached, a cyclobutyl radical,or a radical of structure: ##STR2## in which n, R.sub.6 and R.sub.7 are defined as above, or their salts where such exist, and their hydrates, their preparation and the pharmaceutical compositions which contain them. ##STR3##
摘要翻译：通式（I）的新络合物，其中R 1和R 2一起形成含有7至12个碳原子的饱和或不饱和多环碳环基团，或含有5至11个链成员的饱和或部分饱和的单，双或三环杂环基团和选自氧，硫或氮的杂原子，其后一个原子可任选被烷氧基羰基取代，并且，X 1和X 2表示氯原子或一起形成结构式如下的基团：其中 n为0〜2，R6和R7为相同或不同的氢原子，n = 1时，可以为烷基，也可以与它们所连接的碳原子一起形成环丁基或结构基团：其中n，R6和R7如上所定义，或其盐，如此存在，以及它们的水合物，它们的制备和含有它们的药物组合物。（一）

7. 发明授权

US4496566A Naphthyridine derivatives 失效
标题翻译：萘啶衍生物
公开(公告)号：US4496566A
公开(公告)日：1985-01-29
申请号：US333181
申请日：1981-12-21
申请人： Jun-ichi Matsumoto , Shinichi Nakamura
发明人： Jun-ichi Matsumoto , Shinichi Nakamura
IPC分类号： A01N43/90 , A23L3/3544 , A61K31/495 , A61P31/04 , C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04 , A61K31/47 , C07D401/04
CPC分类号： C07D213/75 , C07D213/74 , C07D213/77 , C07D471/04
摘要： A 1,8-naphthyridine compound of the formula ##STR1## wherein R.sub.1 is a lower alkyl group, and the esters and salts thereof. The 1,8-naphthyridine compound of the formula (I) in which R.sub.1 is a methyl group is useful as an antibacterial agent.
摘要翻译：其中R1是低级烷基的式“IMAGE”的1,8-萘啶化合物及其酯和盐。其中R 1为甲基的式（I）的1,8-萘啶化合物可用作抗菌剂。

8. 发明授权

US4352803A Novel naphthyridine derivatives, intermediates thereof, processes for preparation thereof, and use thereof 失效
标题翻译：新型萘啶衍生物，其中间体，其制备方法及其用途
公开(公告)号：US4352803A
公开(公告)日：1982-10-05
申请号：US264824
申请日：1981-05-18
申请人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
发明人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
IPC分类号： C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04 , A61K31/495
CPC分类号： C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04 , Y10S514/96 , Y10S514/962
摘要： This invention relates to 1,8-naphthyridine compounds of the formula ##STR1## wherein X is a halogen atom especially fluorine atom,R.sub.1 is an ethyl group or a vinyl group, andR.sub.2 is a hydrogen atom or a lower alkyl group, their salts and processes for the preparation of them.The 1,8-naphthyridine compounds and their salts are useful as antibacterial agents and intermediates thereof.
摘要翻译：本发明涉及下式的1,8-萘啶化合物，其中X是卤原子，特别是氟原子，R 1是乙基或乙烯基，R 2是氢原子或低级烷基，它们的盐以及它们的制备过程。 1,8-萘啶化合物及其盐可用作抗菌剂及其中间体。

9. 发明授权

US4341784A Naphthyridine derivatives 失效
标题翻译：萘啶衍生物
公开(公告)号：US4341784A
公开(公告)日：1982-07-27
申请号：US187081
申请日：1980-09-15
申请人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
发明人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
IPC分类号： C07D487/02 , A61K31/435 , A61P31/04 , C07D471/04 , A61K31/44
CPC分类号： C07D471/04 , Y02P20/55
摘要： The present invention provides a 1,8-naphthyridine compound of the formula ##STR1## wherein R is hydrogen, methyl, ethyl or propyl, and a nontoxic pharmaceutically acceptable salt thereof, and a process for preparing a 1,8-naphthyridine compound of the above formula which comprises(A) reacting a compound of the formula ##STR2## wherein Y is halogen, lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower alkylsulfonyloxy or arylsulfonyloxy, and R.sub.1 is hydrogen or lower alkyl,with a compound of the formula ##STR3## wherein R.sub.2 is hydrogen or a protective group for the amino group, and R is as defined above,and when a reaction product in which R.sub.1 is lower alkyl and/or R.sub.2 is the amino protective group is obtained, treating it with an acid or base, and/or reductively cleaving it,(B) decomposing a compound of the formula ##STR4## wherein A .crclbar. is a fluorine-containing anion, and R.sub.1 and R.sub.2 are as defined above,and when a reaction product in which R.sub.1 is lower alkyl and/or R.sub.2 is the amino protective group is obtained, treating it with an acid or base, and/or reductively cleaving it,(C) treating a compound of the formula ##STR5## wherein R'.sub.1 is hydrogen or lower alkyl, R'.sub.2 is hydrogen or a protective group for the amino group, provided that R'.sub.1 and R'.sub.2 are not hydrogen atoms at the same time, and R is as defined above,with an acid or base, and/or reductively cleaving it, and optionally converting the resulting compound to a nontoxic pharmaceutically acceptable salt thereof.The 1,8-naphthyridine compound is useful as an antibacterial agent.
摘要翻译：本发明提供式IMA图示的1,8-萘啶化合物，其中R是氢，甲基，乙基或丙基，及其无毒的药学上可接受的盐，以及制备1,8-萘啶化合物的方法其包含（A）使式（I）的化合物其中Y为卤素，低级烷氧基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷基磺酰氧基或芳基磺酰氧基，R 1为氢或低级烷基，其中R2是氢或氨基保护基的式“IMAGE”，R的定义同上，当R1是低级烷基和/或R2是氨基保护基的反应产物得到时，将其处理（B）分解其中A（ - ）为含氟阴离子的式“IMAGE”的化合物，并且R 1和R 2如上所定义，当反应其中R1是低级烷基和/或 r R2是得到的氨基保护基团，用酸或碱处理，和/或还原性地裂解它;（C）处理下式化合物其中R'1是氢或低级烷基，R'2 是氢或氨基的保护基团，条件是R 1和R 2不同时为氢原子，R为如上所定义，与酸或碱反应，和/或还原性地裂解，和任选地将所得化合物转化为无毒的药学上可接受的盐。 1,8-萘啶化合物可用作抗菌剂。

10. 发明授权

US4015002A 1-Aryl-2-oxo-2,4,5,6,7,7a-hexahydro-indoles, salts, pharmaceutical compositions and methods of use 失效
标题翻译： 1-芳基-2-氧代-2,4,5,6,7,7a-六氢 - 吲哚，盐，药物组合物和使用方法
公开(公告)号：US4015002A
公开(公告)日：1977-03-29
申请号：US600937
申请日：1975-08-01
申请人： Marcel Pesson , Henri Techer
发明人： Marcel Pesson , Henri Techer
IPC分类号： C07D209/12 , A61K31/404 , C07D209/34 , C07D413/12
CPC分类号： C07D209/34 , Y10S514/929
摘要： This invention relates to 1-aryl-2-oxo-2,4,5,6,7,7a-hexahydro-indoles, and acid addition salts thereof. In particular, the compounds have (.beta.-aminoethoxy- or .gamma.-amino-propoxy)-phenyl substituents, the amino groups in each case either being joined to two C.sub.1.sub.-5 alkyl groups or forming part of a heterocyclic group such as a pyrolidino, piperidino or morpholino group. Compounds in accordance with the invention have been found to exhibit interesting actions on the cardiovascular system in particular as vasodilators.
摘要翻译：本发明涉及1-芳基-2-氧代-2,4,5,6,7,7a-六氢 - 吲哚及其酸加成盐。特别地，化合物具有（β-氨基乙氧基 - 或γ-氨基 - 丙氧基） - 苯基取代基，每种情况下的氨基都被连接到两个C 1-5烷基或形成杂环基的一部分，例如吡咯烷基，哌啶子基或吗啉代基团。已经发现根据本发明的化合物对心血管系统，特别是作为血管舒张剂表现出有趣的作用。

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