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17 条记录 (耗时 0.027 秒)

    Aminobenzophenones
    4.
    发明授权
    Aminobenzophenones 失效
    氨基二苯甲酮

    公开(公告)号：US06624199B1

    公开(公告)日：2003-09-23

    申请号：US10030965

    申请日：2002-02-22

    申请人： Erik Rytter Ottosen ,  Fredrik Björkling

    发明人： Erik Rytter Ottosen ,  Fredrik Björkling

    IPC分类号： C07C22522

    CPC分类号： C07C225/22 ,  A61K31/136 ,  A61K31/166 ,  A61K31/325 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to compounds of formula I wherein R1 represents one or more, similar or different substituents; R2 represents hydrogen, hydroxy, halogen, alkyl, alkoxy, alkylthio, or cyano; R3 represents one or more, similar or different substituents; and R6 represents hydrogen or methyl; and salts thereof with pharmaceutically acceptable acids, hydrates, and solvates, and to the use of compounds of the general formula II in which formula R1 and R2 independently represent one or more, similar or different substituents; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, phenyl, cyano, carboxy, or carbamoyl; R4, R5 and R6 represent independently hydrogen, trifluoromethyl, alkyl, carbamoyl, alkoxycarbonyl, or alkaloyl; x represents oxygen, N—OH, and N—O-alkyl, dialkoxy, cyclic dialkoxy, dialkylthio, or cyclic dialkylthio, and salts thereof with pharmaceutically acceptable, non-toxic acids.

    摘要翻译： 本发明涉及式Ⅰ化合物，其中R1代表一个或多个相似或不同的取代基; R 2表示氢，羟基，卤素，烷基，烷氧基，烷硫基或氰基; R3表示一个或多个相似或不同的取代基; R6代表氢或甲基; 以及其与药学上可接受的酸，水合物和溶剂合物的盐，以及通式IIin的化合物，其中式R 1和R 2独立地表示一个或多个相似或不同的取代基; R 3表示氢，卤素，羟基，巯基，三氟甲基，氨基，烷基，烷氧基，烷硫基，烷基氨基或烷氧基羰基，苯基，氰基，羧基或氨基甲酰基。 R4，R5和R6独立地表示氢，三氟甲基，烷基，氨基甲酰基，烷氧基羰基或烷酰基; x表示氧，N-OH和N-O-烷基，二烷氧基，环状二烷氧基，二烷基硫代或环状二烷基硫基，及其盐与药学上可接受的无毒酸。

    Aminobenzophenones as inhibitors of interleukin and TNF
    5.
    发明授权
    Aminobenzophenones as inhibitors of interleukin and TNF 失效
    氨基二苯甲酮作为白介素和TNF的抑制剂

    公开(公告)号：US06313174B1

    公开(公告)日：2001-11-06

    申请号：US09341923

    申请日：1999-07-21

    申请人： Erik Rytter Ottosen ,  Schneur Rachlin

    发明人： Erik Rytter Ottosen ,  Schneur Rachlin

    IPC分类号： C07C22522

    CPC分类号： C07C225/22

    摘要： The compounds of the present invention are represented by general formula (I) in which formula R1 and R2 stand independently for one or more, similar or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, the C-content of which can be from 1 to 5, cyano, carboxy, carbamoyl, phenyl, or nitro; R3 stands for hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, the C-content of which can be from 1 to 5, phenyl, cyano, carboxy, or carbamoyl; R4, R5 and R6 stand independently for hydrogen, trifluoromethyl, alkyl, carbamoyl, alkoxycarbonyl, or alkyloxo, the C-content of which can be from 1 to 5; X stands for oxygen, N—OH, N—O-alkyl, dialkoxy, cyclic dialkoxy, dialkylthio, or cyclic dialkylthio, the C-content of which can be from 1 to 5. The present compounds are of value in the human and veterinary practice as systemic and topical therapeutic agents for the treatment and prophylaxis of asthma, allergy, rheumatoid arthritis, spondyloarthritis, gout, atherosclerosis, chronic inflammatory bowel disease, proliferative and inflammatory skin disorders, such as psoriasis, and atopic dermatitis.

    摘要翻译： 本发明的化合物由通式（I）表示，其中式R1和R2独立地表示一个或多个相似或不同的选自氢，卤素，羟基，巯基，三氟甲基，氨基，烷基的取代基 ，烷氧基，烷硫基，烷基氨基或烷氧基羰基，其C含量可以为1至5，氰基，羧基，氨基甲酰基，苯基或硝基; R3代表氢，卤素，羟基，巯基，三氟甲基，氨基，烷基，烷氧基，烷硫基，烷基氨基或烷氧基羰基，其C含量可以为1至5，苯基，氰基，羧基或氨基甲酰基; R4，R5和R6独立地表示氢，三氟甲基，烷基，氨基甲酰基，烷氧基羰基或烷氧基，其C含量可以为1至5; X代表氧，N-OH，NO-烷基，二烷氧基，环状二烷氧基，二烷基硫代或环状二烷硫基，其C含量可以为1至5.本化合物在人和兽医学实践中是有价值的 用于治疗和预防哮喘，过敏，类风湿性关节炎，脊柱关节炎，痛风，动脉粥样硬化，慢性炎性肠病，增殖性和炎性皮肤病，如银屑病和特应性皮炎的全身和局部治疗剂。

    Cyanoamidines as cell proliferation inhibitors
    7.
    发明授权
    Cyanoamidines as cell proliferation inhibitors 失效
    氰酰胺作为细胞增殖抑制剂

    公开(公告)号：US06303641B1

    公开(公告)日：2001-10-16

    申请号：US09424581

    申请日：1999-11-26

    申请人： Erik Rytter Ottosen

    发明人： Erik Rytter Ottosen

    IPC分类号： A61K3144

    CPC分类号： C07D213/78

    摘要： Compounds of the following formula are used for inhibiting cell proliferation: wherein R, R1, Q, X are as defined in the specification.

    摘要翻译： 下式的化合物用于抑制细胞增殖：其中R，R 1，Q，X如说明书中所定义。

    Cyanoguanidines as cell proliferation inhibitors
    8.
    发明授权
    Cyanoguanidines as cell proliferation inhibitors 失效
    氰基胍类作为细胞增殖抑制剂

    公开(公告)号：US06197797B1

    公开(公告)日：2001-03-06

    申请号：US09424630

    申请日：1999-11-26

    申请人： Charlotte Schou ,  Erik Rytter Ottosen

    发明人： Charlotte Schou ,  Erik Rytter Ottosen

    IPC分类号： A61K3144

    CPC分类号： C07D213/75

    摘要： The present invention relates to hitherto unknown compounds of formula (I) or their tautomeric forms, the attachment to the pyridine being in the 3- or 4-position, in which formula R1 stands for one or more substituents which can be the same or different and are selected from the group consisting of: hydrogen, halogen, trifluoromethyl nitro, amino, cyano, carboxy, or alkyl, alkoxy, or alkoxycarbonyl, the C-content of which can be from 1 to 4; X stands for a straight or branched C9-C20 carbon chain, saturated or unsaturated or Q—Ar—R; in which formula Ar stands for phenyl, Q stands for a C5-C20 divalent hydrocarbon radical which can be straight, branched, saturated or unsaturated and R stands for hydrogen or for one or more substituents which can be the same or different and are selected from the group consisting of: hydroxy, amino, halogen, trifluoromethyl, cyano, nitro, carboxy, carbamoyl, or alkyl, alkoxy, alkylthio, alkylamino, or alkoxycarbonyl, the C-content of which can be from 1 to 4; and pharmaceutically acceptable, non-toxic salts and N-oxides thereof. The present compounds are of value in the human and veterinary practice.

    摘要翻译： 本发明涉及迄今为止未知的式（I）化合物或其互变异构形式，其中吡啶与3-或4-位的连接，式R1代表一个或多个可相同或不同的取代基 并且选自：氢，卤素，硝基三氟甲基，氨基，氰基，羧基或烷基，烷氧基或烷氧基羰基，其C含量可以为1至4; X代表饱和或不饱和的直链或支链C 9 -C 20碳链或Q-Ar-R; 其中式Ar代表苯基，Q代表可以是直链，支链，饱和或不饱和的C 5 -C 20二价烃基，R代表氢或一个或多个相同或不同的取代基，选自 由羟基，氨基，卤素，三氟甲基，氰基，硝基，羧基，氨基甲酰基或烷基，烷氧基，烷硫基，烷基氨基或烷氧基羰基组成的基团，其C含量可以为1至4; 和其药学上可接受的无毒盐和N-氧化物。 本化合物在人类和兽医实践中是有价值的。

    Aminobenzophenones as inhibitors of IL-1&bgr; and TNF-&agr;
    10.
    发明授权
    Aminobenzophenones as inhibitors of IL-1&bgr; and TNF-&agr; 失效
    氨基二苯甲酮作为IL-1β和TNF-α的抑制剂

    公开(公告)号：US06566554B1

    公开(公告)日：2003-05-20

    申请号：US10031075

    申请日：2002-02-22

    申请人： Erik Rytter Ottosen

    发明人： Erik Rytter Ottosen

    IPC分类号： C07C23305

    CPC分类号： C07C225/22 ,  C07C229/18 ,  C07C233/43 ,  C07C235/10 ,  C07C235/72 ,  C07C235/74 ,  C07C237/20

    摘要： The present invention relates to a compound of general formula (I) wherein R1, R2, and R3 represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)akylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, or nitro; further R2 can be hydrogen, and R3 can be carboxy and carbamoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulphur; Q represents —(CO)—, —(CS)—, or a bond; Y represents (C5-C15)alkyl; (C2-C15)olefinic group; (C3-C10)monocyclic hydrocarbon group; or phenyl; any of which may be optionally substituted by one or more, same or different substituents selected from the group consisting of the formula R5 defined below; (C1-C4)alkyl substituted by one or more substituents selected for the group R5; or a group of the formula —(Z—O)n—Z, wherein Z is a (C1-C3)alkyl, n is an integer >1; and no continuous linear sequence of atoms in the group Y exceeds 15; R5 represents halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, azido, nitro, —COOH, —CONH2, —CONHR′, or COONR′R′ wherein R′ represents (C1-C3)alkyl; or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof. The compounds are valuable in the human and veterinary therapy.

    摘要翻译： 本发明涉及通式（I）的化合物，其中R 1，R 2和R 3表示一个或多个相同或不同的选自卤素，羟基，巯基，三氟甲基，氨基，（C 1 -C 3） 烷基，（C 2 -C 3）烯基，（C 1 -C 3）烷氧基，（C 1 -C 3）烷硫基，（C 1 -C 6）烷基氨基，（C 1 -C 3）烷氧基羰基，氰基，-CONH 2，苯基或硝基; 另外R2可以是氢，R3可以是羧基和氨基甲酰基; R4表示氢，（C1-C3）烷基或烯丙基; X表示氧或硫; Q表示 - （CO） - ， - （CS） - 或键; Y表示（C 5 -C 15）烷基; （C 2 -C 15）烯基; （C 3 -C 10）单环烃基; 或苯基; 其中任何一个可以任选被一个或多个相同或不同的选自以下定义的式R 5的取代基取代; 被一个或多个选自基团R 5的取代基取代的（C 1 -C 4）烷基; 或式 - （Z-O）n-Z的基团，其中Z为（C 1 -C 3）烷基，n为整数> 1; Y组中原子的连续线性序列不超过15; R5表示卤素，羟基，巯基，三氟甲基，氨基，（C1-C3）烷氧基，（C1-C3）烷硫基，（C1-C6）烷基氨基，（C1-C3）烷氧基羰基，氰基，叠氮基，硝基， CONH 2，-CONHR'或COONR'R'，其中R'表示（C 1 -C 3）烷基; 或其药学上可接受的盐，或其水合物或溶剂化物。 这些化合物在人类和兽医治疗中是有价值的。