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    Malonic acid derivatives, processes for their preparation their use and pharmaceutical compositions containing them
    4.
    发明授权
    Malonic acid derivatives, processes for their preparation their use and pharmaceutical compositions containing them 有权
    丙二酸衍生物，其制备方法，其用途和含有它们的药物组合物

    公开(公告)号：US06794365B2

    公开(公告)日：2004-09-21

    申请号：US09790641

    申请日：2001-02-23

    申请人： Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    发明人： Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    IPC分类号： C07K506

    CPC分类号： C07D213/56 ,  A61K38/00 ,  C07C257/18 ,  C07C279/14 ,  C07C2601/14 ,  C07K5/0202 ,  C07K5/06026 ,  C07K5/06034

    摘要： The present invention relates to new malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula I, to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to the use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

    摘要翻译： 本发明涉及式I的新型丙二酸衍生物，其中R（1），R（2），R（3），R（4），R（5）和R（6） 索赔。 式I化合物是凝血酶因子Xa的抑制剂。 本发明还涉及制备式I化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，使用式I化合物治疗和预防可治疗的疾病 或通过抑制诸如血栓栓塞性疾病的因子Xa活性来防止，以及式I化合物在制备用于这些疾病的药物中的用途。 本发明还涉及含有式I化合物的组合物，其与惰性载体混合或以其它方式结合，特别是含有式I化合物与药学上可接受的载体物质和辅助物质的药物组合物。

    Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them
    5.
    发明授权
    Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them 有权
    丙二酸衍生物，其制备方法，用途及含有它们的药物组合物

    公开(公告)号：US06395737B1

    公开(公告)日：2002-05-28

    申请号：US09473053

    申请日：1999-12-28

    申请人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Hans Matter ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    发明人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Hans Matter ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    IPC分类号： A61K31165

    CPC分类号： C07C257/18 ,  C07C279/14

    摘要： New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. Compositions containing a compound of formula I in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula I together with pharmaceutically acceptable carrier substances and auxiliary substances.

    摘要翻译： 用于抑制血液凝固蛋白质的新化合物，更具体地，涉及式I的丙二酸衍生物，其中R（1），R（2），R（3），R（4），R（5）和 R（6）具有权利要求中所示的含义。 式I化合物是凝血酶因子Xa的抑制剂。 用于制备式I化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，式I化合物在治疗和预防疾病中的用途，其可以通过抑制因子Xa来治疗或预防 活性如血栓栓塞性疾病，以及式I化合物在制备用于这些疾病的药物中的应用。 含有式I化合物的组合物与惰性载体混合或以其它方式结合，特别是含有式I化合物的药物组合物以及药学上可接受的载体物质和辅助物质。

    Pharmacologically active chromanes
    6.
    发明授权
    Pharmacologically active chromanes 失效

    公开(公告)号：US5132310A

    公开(公告)日：1992-07-21

    申请号：US627523

    申请日：1990-12-14

    申请人： Armin Walser

    发明人： Armin Walser

    IPC分类号： C07D311/72 ,  C07D405/06 ,  C07D405/10 ,  C07D407/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D491/04 ,  C07D491/048

    CPC分类号： C07D405/06 ,  C07D311/72 ,  C07D405/10 ,  C07D407/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D491/04

    摘要： Racemic Compounds of the formula ##STR1## A is --C.tbd.C--R.sub.6, --CH.sub.2 --CH.sub.2 --R.sub.7 or ##STR2## R.sub.1 is hydrogen or lower alkanoyl, R.sub.2, R.sub.3, and R.sub.4 independently are hydrogen or lower alkyl,R.sub.5 is lower alkyl,R.sub.6 is a heteroaromatic radical or an aromatic radical selected from phenyl, naphthyl or phenanthryl, which aromatic radical may optionally be substituted by one or more substituents selected from chlorine, fluorine, lower alkyl, lower alkoxy, phenyl lower alkoxy, lower alkanoyl, lower alkanoyloxy, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, hydroxyimino lower alkyl, amino, amino lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylamino-lower alkyl, lower alkanoylamino, aminocarbonyl, lower alkylaminocarbonyl, lower dialkylaminocarbonyl, trifluoroacetylamino, trifluoromethyl, hydroxy, pyridyl, or on adjacent carbons can be ##STR3## wherein R' is hydrogen, lower alkanoyl, trifluoroacetyl and R" hydrogen or lower alkyl,R.sub.7 is a heteroaromatic radical or an aromatic radical selected from phenyl, naphthyl or phenanthryl, which aromatic radical may optionally be substituted by one or more substituents selected from chlorine, fluorine, lower alkyl, lower alkoxy, phenyl-lower alkoxy of 2-7 carbon atoms, lower alkanoyl, lower alkanoyloxy, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, amino, amino-lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylamino-lower alkyl, lower alkanoylamino, aminocarbonyl, lower alkylaminocarbonyl, lower dialkylaminocarbonyl, trifluoroacetylamino, trifluoromethyl, hydroxy or pyridyl, or on adjacent carbons can be ##STR4## wherein R' is hydrogen, lower alkanoyl, trifluoroacetyl and R" hydrogen or lower alkyl,R.sub.8, R.sub.9, and R.sub.10, independently, are hydrogen, hydroxy, lower alkyl, lower alkoxy, hydroxy lower alkyl, fluorine, chlorine or lower alkanoyl provided that no more than one of R.sub.8, R.sub.9, and R.sub.10 is hydroxy, lower alkoxy, lower hydroxyalkyl, fluorine, chlorine or lower alkanoyl, and Y is CH or N,and their enantiomer and salts thereof are described.The compounds of formula I exhibit activity as inhibitors of 5-lipoxygenase and inhibit lipid peroxidation. They are, therefore, useful in the treatment of diseases caused or aggravated by excess oxidative metabolism of arachidonic acid via the 5-lipoxygenase pathway and in the treatment of inflammation, arthritis, allergies, asthma and psoriasis. The compounds of formula I can also be used to prevent peroxidation of lipids and thus protect lipid membranes from oxidative stress.

    Imidazodiazepines and processes therefor
    7.
    发明授权
    Imidazodiazepines and processes therefor 失效
    咪唑二氮类及其制备方法

    公开(公告)号：US4440685A

    公开(公告)日：1984-04-03

    申请号：US504999

    申请日：1983-06-16

    申请人： Armin Walser ,  Rodney I. Fryer

    发明人： Armin Walser ,  Rodney I. Fryer

    IPC分类号： C07D233/54 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D498/14 ,  C07F9/645 ,  C07F9/6561 ,  A61K31/55

    CPC分类号： C07D233/64 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/645 ,  C07F9/6561

    摘要： Novel Imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a] [1,4] diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included with the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl, preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro or halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof; R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety; and R.sub.2 is hydrogen and lower alkyl.

    摘要翻译： 新型咪唑并二氮杂类及其类似物可用作抗惊厥药，肌肉松弛剂，抗焦虑药和镇静剂。 该类的优选化合物属于可能具有非常多种有机取代基的咪唑并[1,5-a] [1,4]二氮杂类。 包括在本发明的范围内的特别优选的类包括式IMA的化合物，其中R 1是氢和低级烷基，优选甲基; R3和R5是氢; R4是氢，硝基或卤素，最优选氯，而在最优选的实施方案中，当位于咪唑并二氮杂的稠合的苯并部分位于其8-位时; R6是苯基或卤素，硝基或低级烷基取代的苯基，优选卤素，氟是优选的卤素，取代的氟位于苯基部分的2-位; 并且R 2是氢和低级烷基。

    Imidazodiazepines and processes therefor
    8.
    发明授权
    Imidazodiazepines and processes therefor 失效
    咪唑二氮类及其制备方法

    公开(公告)号：US4376074A

    公开(公告)日：1983-03-08

    申请号：US242851

    申请日：1981-03-12

    申请人： Armin Walser ,  Rodney I. Fryer

    发明人： Armin Walser ,  Rodney I. Fryer

    IPC分类号： C07D243/16 ,  C07D243/20 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561 ,  C07D487/22 ,  A61K31/55

    CPC分类号： C07D487/04 ,  C07D243/16 ,  C07D243/20 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

    摘要： Novel Imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included within the purview of the invention encompasses a compound of the formula ##STR1## wherein R.sub.1 is hydrogen and lower alkyl preferably methyl; R.sub.3 and R.sub.5 are hydrogen; R.sub.4 is hydrogen, nitro and halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof, R.sub.6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety and R.sub.2 is hydrogen and lower alkyl.

    摘要翻译： 新型咪唑并二氮卓类及其类似物可用作抗惊厥药，肌肉松弛剂，抗焦虑药和镇静剂。 该类的优选化合物属于可能具有非常多种有机取代基的咪唑并[1,5-a] [1,4]二氮杂类。 包括在本发明的范围内的特别优选的类包括式IMA的化合物，其中R 1是氢，低级烷基优选是甲基; R3和R5是氢; R4是氢，硝基和卤素，最优选氯，最优选的实施方案中，当位于咪唑并二氮杂的稠合苯并部分位于其8-位时，R 6是苯基或卤素，硝基或低级烷基取代的 苯基，优选卤素，氟是优选的卤素，取代的氟位于苯基部分的2-位和R2

    Imidazodiazepines
    9.
    发明授权
    Imidazodiazepines 失效

    公开(公告)号：US4347365A

    公开(公告)日：1982-08-31

    申请号：US242861

    申请日：1981-03-12

    申请人： Armin Walser ,  Rodney I. Fryer

    发明人： Armin Walser ,  Rodney I. Fryer

    IPC分类号： C07D233/66 ,  C07D243/16 ,  C07D243/20 ,  C07D487/04 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561 ,  C07D403/04 ,  C07D409/04

    CPC分类号： C07D487/04 ,  C07D243/16 ,  C07D243/20 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07F9/6561

    摘要： This invention is directed toward pharmacologically active compound of the formula ##STR1## R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, phenyl, alkoxy lower alkyl, halo lower alkyl, amino lower alkyl, substituted amino lower alkyl, substituted phenyl, pyridyl, aralkyl and the groups ##STR2## wherein R is hydrogen or lower alkyl and ROOC where R is lower alkyl; R.sub.2 is selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, acyloxy lower alkyl, alkoxy lower alkyl, halo lower alkyl, amino or substituted amino lower alkyl, amino, cyano, cyano lower alkyl, substituted amino, chloro, bromo and iodo, the group --COOR where R is hydrogen or lower alkyl, the group ##STR3## where R is hydrogen or lower alkyl, or derivatives thereof, e.g., the group R--C.dbd.N--R' wherein R' is hydrogen, lower alkyl, hydroxy, phenyl, alkoxy, amino, mono or di-alkylamino and arylamino and R is hydrogen or lower alkyl, the group ##STR4## (where R and R' are individually hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl, aryl or together R and R' form a part of a heterocyclic ring and the group (CH.sub.2).sub.n NRR' where R and R' are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or together R and R' form a part of a heterocyclic ring and n is 1 to 4); the group ##STR5## where R.sup.10, R.sup.11, R.sup.12 are hydrogen or lower alkyl and the group (CH.sub.2).sub.n NR.sup.13 R.sup.14 where n is 1 to 4 and R.sup.13, R.sup.14 are hydrogen, lower alkyl, hydroxy lower alkyl, lower alkenyl or R.sup.13 and R.sup.14 together form part of a heterocyclic ring, with the limitation that where R.sup.10, R.sup.11 or R.sup.12 is a basic side chain, then the remaining substituents are hydrogen or lower alkyl; R.sub.3 is selected from group consisting of hydrogen and lower alkyl; R.sub.4 is selected from the group consisting of hydrogen, halogen, nitro, cyano, trifluoromethyl, lower alkyl, substituted amino, amino, hydroxy lower alkyl and lower alkanoyl; R.sub.6 is selected from the group consisting of phenyl, mono-substituted phenyl, di-substituted phenyl, pyridyl and mono-substituted pyridyl; and ##STR6## is selected from the group consisting of ##STR7## and the pharmaceutically acceptable salts thereof. Also provided are methods for the preparation of these compounds as well as pharmaceutical formulations which contain the active compounds of this invention. The compounds of the formulas illustrated above and their analogs are useful as anticonvulsants, muscle relaxants, anxiolytic and sedative agents.