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    AMINOBENZOPHENONES AS INHIBITORS OF IL-1BETA AND TNF-ALPHA
    2.
    发明授权
    AMINOBENZOPHENONES AS INHIBITORS OF IL-1BETA AND TNF-ALPHA 有权
    氨基丁酸ALS抑制剂TNF-α

    公开(公告)号：EP1210325B1

    公开(公告)日：2004-10-06

    申请号：EP00943701.3

    申请日：2000-07-11

    申请人： LEO PHARMA A/S

    发明人： OTTOSEN, Erik, Rytter

    IPC分类号： C07C275/40 ,  A61K31/17

    CPC分类号： C07C311/60 ,  C07C275/40 ,  C07C2601/14

    摘要： The present invention relates to compounds of formula (I) wherein R1 and R2 independently represent 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)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl, and nitro; R2 further being represented by hydrogen; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, phenyl, cyano, carboxy, or carbamoyl; R4 represents hydrogen, (C1-C3)alkyl or allyl; Q represents a bond, -SO2-, or -C(R6)(R7)(-O-C=O)-, in which formula R6 and R7 independently represent hydrogen, trifluoromethyl, or (C1-C4)alkyl; Y represents (C1-C15)alkyl, (C2-C15)olefinic group, (C3-C10)carbocyclic group, or phenyl, any of which is optionally substituted by one or more, same or different substituents represnet by the formula R5; or Y represents a group of formula -(Z-O)n-Z, where Z is a (C1-C3)alkyl, and n is an integer >1, and no continuous linear sequence of atoms in the group Y exceeds 15; R5 represents halogen, hydroxy, mercapto, trifluoromethyl, (C1-C4)alkyl, amino, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, azido, nitro, -COOH, -CONH2, -CONHR' or -CONRR' wherein R et R' stands for (C1-C3)alkyl; X represents oxygen or sulfur, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate threof. The compounds are valuable in the human and veterinary therapy.

    摘要翻译： 本发明涉及式（Ⅳ）的化合物独立地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）烯基的取代基 ，（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，氨基甲酰基，苯基和硝基，条件是当R1表示一个取代基时， 当R1表示多于一个取代基时，至少一个R 1取代基处于邻位; R2是一个位于邻位的取代基，所述取代基选自氢，卤素，羟基，巯基，三氟甲基，氨基，（C1-C3）烷基，（C2-C3）烯基，（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，氨基甲酰基，苯基和硝基; R3代表氢，卤素，羟基，巯基，三氟甲基，氨基，（C1-C3）烷基，（C2-C3）烯基，（C1-C3）烷氧基，（C1-C3）烷硫基，（C1-C6）烷基氨基， （C 1 -C 3）烷氧基羰基，苯基，氰基，羧基或氨基甲酰基; R4表示氢，（C1-C3）烷基或烯丙基。 这些化合物在人类和兽医治疗中是有价值的。

    AMINOBENZOPHENONES AS INHIBITORS OF INTERLEUKIN AND TNF
    3.
    发明授权
    AMINOBENZOPHENONES AS INHIBITORS OF INTERLEUKIN AND TNF 失效
    AMINOBENZOPHENONES白细胞介素及TNF抑制剂

    公开(公告)号：EP0966424B1

    公开(公告)日：2004-06-23

    申请号：EP98900270.4

    申请日：1998-01-08

    申请人： LEO PHARMA A/S (with secondary name: LEO PHARMACEUTICAL PRODUCTS LTD. A/S)

    发明人： OTTOSEN, Erik, Rytter ,  RACHLIN, Schneur

    IPC分类号： C07C225/22 ,  A61K31/135

    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.

    AMINOBENZOPHENONES AS INHIBITORS OF IL-1BETA AND TNF-ALPHA
    4.
    发明授权
    AMINOBENZOPHENONES AS INHIBITORS OF IL-1BETA AND TNF-ALPHA 有权
    Aminobenzophenones AS IL-1β的抑制剂，TNF-α

    公开(公告)号：EP1237845B1

    公开(公告)日：2007-05-23

    申请号：EP00979457.9

    申请日：2000-11-29

    申请人： LEO PHARMA A/S

    发明人： OTTOSEN, Erik, Rytter

    IPC分类号： C07C225/22 ,  C07C251/48 ,  C07C325/02 ,  A61P29/00 ,  A61K31/135 ,  A61K31/15 ,  A61K31/095 ,  A61P17/00

    CPC分类号： C07C325/02 ,  A61K31/135 ,  A61K31/136 ,  A61K45/06 ,  C07C225/22 ,  C07C251/48 ,  A61K2300/00

    摘要： A compound of general formula (I), wherein R1 represents a substituent selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, -CONH2, phenyl, and nitro; R2 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, -CONH2, phenyl, and nitro; R3 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, cyano, carboxy, carbamoyl, (C1-C10)alkyl, (C2-C10)olefinic group, (C3-C8)monocyclic hydrocarbon group, (C1-C10)alkoxy, (C1-C10) alkylthio, (C1-C10)alkoxycarbonyl, and phenyl; R4 represents hydrogen, (C1-C6)alkyl, (C2-C6)olefinic group, or (C3-C6)monocyclic hydrocarbon group; R5 represents one or more, same or different substituents selected from the group consisting of hydrogen and R1; X represents oxygen, sulphur, or N-OH; and salts thereof with pharmaceutically acceptable acids, hydrates and solvates, may be used in the prophylaxis or treatment of inflammatory diseases.

    NOVEL AMINOBENZOPHENONES
    5.
    发明授权
    NOVEL AMINOBENZOPHENONES 有权
    新aminobenzophenones

    公开(公告)号：EP1202954B1

    公开(公告)日：2003-10-01

    申请号：EP00943698.1

    申请日：2000-07-11

    申请人： Leo Pharma A/S

    发明人： OTTOSEN, Erik, Rytter ,  BJÖRKLING, Fredrik

    IPC分类号： C07C225/22 ,  A61K31/136 ,  A61P17/10

    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 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, trifluorormethyl, 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. The compounds of the invention are useful in the human and veterinary practice.

    AMINOBENZOPHENONES AS INHIBITORS OF IL-1BETA AND TNF-ALPHA
    10.
    发明授权
    AMINOBENZOPHENONES AS INHIBITORS OF IL-1BETA AND TNF-ALPHA 有权

    公开(公告)号：EP1210320B1

    公开(公告)日：2004-09-29

    申请号：EP00943699.9

    申请日：2000-07-11

    申请人： LEO PHARMA A/S

    发明人： OTTOSEN, Erik, Rytter

    IPC分类号： C07C235/04 ,  C07C237/04 ,  C07C229/18 ,  A61K31/165 ,  A61K31/222

    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)alkylthio, (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.