싸이아졸 유도체, 이의 제조 방법 및 이를 포함하는 약학적조성물
    13.
    发明公开
    싸이아졸 유도체, 이의 제조 방법 및 이를 포함하는 약학적조성물 失效
    噻唑衍生物,其制备方法及包括其的药物组合物

    公开(公告)号:KR1020080016249A

    公开(公告)日:2008-02-21

    申请号:KR1020060078095

    申请日:2006-08-18

    Abstract: A novel thiazole derivative is provided to inhibit effectively the enzymatic activity of 5-lipoxygenase(5-LO) acting when an arachidonic acid is converted into a leukotriene metabolite, thereby being used as a prophylactic and therapeutic agent of various inflammatory diseases and cancers. A thiazole derivative is represented by the formula(1), wherein each R1 and R2 is independently H, OR7, NO2, halogen or C1-4 linear, branched, or cyclic alkyl; each R3, R4, R5 and R6 is independently H, CF3, OR7, CO2R7, NR7R8, NO2, NHCOR7, C(=O)R7, SR7, halogen, C1-4 linear, branched or cyclic alkyl(in which each R7 and R8 is independently H, unsubstituted or F-substituted C1-6 linear, branched, or cyclic alkyl, or aryl); X is NH, O, S or SO2; Y is C or N. A method for preparing a thiazole derivative represented by the formula(1a) comprises a step of reacting an acetophenone derivative represented by the formula(2) with an aniline derivative represented by the formula(2) and a thiocyanate salt, wherein the R1 to R6, and Y are same as defined above. A pharmaceutical composition for preventing or treating asthma, chronic obstructive lung disease, arthritis, psoriasis, atopic dermatitis, allergy, enteritis, and cancer comprises the thiazole derivative, or a pharmaceutically acceptable salt thereof, a hydrate, solvate or isomer thereof as an effective ingredient.

    Abstract translation: 提供了一种新的噻唑衍生物,用于有效地抑制花生四烯酸转化为白三烯代谢物时作用的5-脂氧合酶(5-LO)的酶活性,从而用作各种炎性疾病和癌症的预防和治疗剂。 噻唑衍生物由式(1)表示,其中每个R 1和R 2独立地为H,OR 7,NO 2,卤素或C 1-4直链,支链或环状烷基; 每个R 3,R 4,R 5和R 6独立地是H,CF 3,OR 7,CO 2 R 7,NR 7 R 8,NO 2,NHCOR 7,C(= O)R 7,SR 7,卤素,C 1-4直链,支链或环状烷基(其中每个R 7和 R8独立地是H,未取代的或F-取代的C 1-6直链,支链或环状烷基或芳基); X是NH,O,S或SO 2; Y为C或N.由式(1a)表示的噻唑衍生物的制备方法包括使式(2)表示的苯乙酮衍生物与式(2)表示的苯胺衍生物和硫氰酸盐 ,其中R1至R6和Y与上述定义相同。 用于预防或治疗哮喘,慢性阻塞性肺病,关节炎,牛皮癣,特应性皮炎,过敏,肠炎和癌症的药物组合物包含噻唑衍生物或其药学上可接受的盐,其水合物,溶剂化物或异构体作为有效成分 。

    신규한 카보니트릴 화합물, 이의 제조방법 및 이를포함하는 류마티스성 관절염, 골관절염, 파제트병,악성고칼슘혈증, 대사성골질환 및 각종 암의 치료 및예방을 위한 약제학적 조성물
    15.
    发明公开
    신규한 카보니트릴 화합물, 이의 제조방법 및 이를포함하는 류마티스성 관절염, 골관절염, 파제트병,악성고칼슘혈증, 대사성골질환 및 각종 암의 치료 및예방을 위한 약제학적 조성물 失效
    新型碳青霉烯类化合物,其制备方法以及用于治疗或预防特发性恶病质,糖皮质激素,帕格病,恶性高血压,代谢性骨髓疾病和包含其中的癌症的药物组合物

    公开(公告)号:KR1020090005842A

    公开(公告)日:2009-01-14

    申请号:KR1020070069210

    申请日:2007-07-10

    Abstract: A novel carbonitrile compound or its pharmaceutically acceptable salt, a method for preparing the compound, and a pharmaceutical composition containing compound are provided to prevent and treat osteoarthritis and various cancer without side effect. A carbonitrile compound is represented by the formula 1, wherein n is 1 or 2; R1 is H, halogen-substituted or unsubstituted linear or branched saturated or unsaturated C1-C10 alkyl, C3-C7 cycloalkyl, C1-C10 alkoxy, C1-C10 alkylthio, hydroxy-C1-C10 alkyl, C1-C10 alkylcarbonyl, C1-C10 alkylthio-C1-C10 alkyl, C3-C7 cycloalkyl-C1-C10 alkyl, C3-C7 cycloalkyl-C1-C10 alkyl, C1-C10 alkoxy-C1-C10 alkyl, phenyl, ar-C1-C10 alkyl, or ar-C1-C10 alkoxy group; and R2 linear or branched saturated or unsaturated C1-C10 alkyl, C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C10 alkyl, phenyl, ar-C1-C10 alkyl, C1-C10 alkoxycarbonyl, or ar-C1-C10 alkoxycarbonyl group.

    Abstract translation: 提供新的腈化合物或其药学上可接受的盐,制备该化合物的方法和含有药物组合物的化合物以预防和治疗骨关节炎和各种癌症而没有副作用。 腈化合物由式1表示,其中n为1或2; R1是H,卤素取代或未取代的直链或支链饱和或不饱和C 1 -C 10烷基,C 3 -C 7环烷基,C 1 -C 10烷氧基,C 1 -C 10烷硫基,羟基-C 1 -C 10烷基,C 1 -C 10烷基羰基,C 1 -C 10 烷硫基-C 1 -C 10烷基,C 3 -C 7环烷基-C 1 -C 10烷基,C 3 -C 7环烷基-C 1 -C 10烷基,C 1 -C 10烷氧基-C 1 -C 10烷基,苯基,芳基-C 1 -C 10烷基或芳烷基 -C 10烷氧基 和R 2直链或支链饱和或不饱和的C 1 -C 10烷基,C 3 -C 7环烷基,C 3 -C 7环烷基-C 1 -C 10烷基,苯基,芳基-C 1 -C 10烷基,C 1 -C 10烷氧基羰基或芳基-C 1 -C 10烷氧基羰基 。

    신규한 1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1H-피라졸화합물, 이의 제조방법 및 이를 포함하는 약제학적 조성물
    16.
    发明授权
    신규한 1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1H-피라졸화합물, 이의 제조방법 및 이를 포함하는 약제학적 조성물 失效
    1- [1-(3,4-二甲氧基乙基) - 吡咯烷基] -1H-吡唑化合物,其制备方法和包含该化合物的药物组合物

    公开(公告)号:KR100833799B1

    公开(公告)日:2008-05-30

    申请号:KR1020070002725

    申请日:2007-01-10

    Abstract: 1-[1-(3,4-Dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compounds are provided to inhibit activity of PDE-4(phosphodiesterase-4) with high activity and selectivity without side effects, so that the compounds are useful for treating inflammation diseases, neurodegenerative disease and cancers. 1-[1-(3,4-Dialkoxyaryl)-pyridylmethyl]-1H-pyrazole compounds represented by the formula(1) are provided, wherein A is N or CH; R1 is linear or branched, saturated or unsaturated (C1-C7)alkyl or halogen-substituted linear or branched, saturated or unsaturated (C1-C7)alkyl; R2 is hydrogen atom, (C3-C7)cycloalkyl or (C3-C8)cycloalkylmethyl; R3, R4 and R5 are each independently hydrogen atom, phenyl, pyridinyl, N-oxypyridinyl, linear or branched, saturated or unsaturated (C1-C7)alkyl, (C3-C7)cycloalkyl, (C3-C10)cycloalkyl(C1-C7)alkyl, halogen atom, cyano, nitro, amino, mono- or di(C1-C7)alkylamino, mono- or di(C1-C7)alkylaminocarbonyl, (C3-C7)cycloalkylamino, 3- to 7-membered saturated or unsaturated hetero ring containing oxygen, nitrogen or sulfur in hetero ring, guanidinyl, ureido, benzyl, benzyloxy, formyl, (C1-C7)alkanoyl, (C1-C7)alkoxy, (C1-C7)alkoxy(C1-C7)alkyl, hydroxy(C1-C7)alkyl, carboxyl or (C1-C7)alkoxycarbonyl; and R6 is pyridinyl or N-oxypyridinyl group.

    Abstract translation: 提供1- [1-(3,4-二烷氧基芳基) - 吡啶基甲基] -1H-吡唑化合物以抑制具有高活性和选择性的PDE-4(磷酸二酯酶-4)的活性而没有副作用,使得该化合物可用于 治疗炎症疾病,神经退行性疾病和癌症。 提供由式(1)表示的1- [1-(3,4-二烷氧基芳基) - 吡啶基甲基] -1H-吡唑化合物,其中A是N或CH; R1是直链或支链饱和或不饱和(C1-C7)烷基或卤素取代的直链或支链饱和或不饱和(C1-C7)烷基; R2是氢原子,(C3-C7)环烷基或(C3-C8)环烷基甲基; R 3,R 4和R 5各自独立地为氢原子,苯基,吡啶基,N-氧代吡啶基,直链或支链,饱和或不饱和的(C1-C7)烷基,(C3-C7)环烷基,(C3-C10)环烷基 )(C 1 -C 7)烷基氨基羰基,(C 3 -C 7)环烷基氨基,3至7元饱和或不饱和的(C 1 -C 7)烷基氨基, 杂环中含氧,氮或硫的杂环,胍基,脲基,苄基,苄氧基,甲酰基,(C1-C7)烷酰基,(C1-C7)烷氧基,(C1-C7)烷氧基(C1-C7) (C 1 -C 7)烷基,羧基或(C 1 -C 7)烷氧基羰基; R6是吡啶基或N-氧代吡啶基。

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