신규한 2,4-피리미딘 유도체 및 이의 용도
    86.
    发明授权
    신규한 2,4-피리미딘 유도체 및 이의 용도 有权
    新的2,4-嘧啶衍生物及其用途

    公开(公告)号:KR101246911B1

    公开(公告)日:2013-03-25

    申请号:KR1020100108201

    申请日:2010-11-02

    CPC classification number: C07D239/60 C07D239/52 C07D401/12

    Abstract: 본 발명은 신규한 2,4-피리미딘 유도체 및 이의 용도에 관한 것으로, 보다 상세하게는 전신성 홍반성 낭창에 효과가 있는 피리미딘 유도체, 이를 유효성분으로 포함하는 전신성 홍반성 낭창 예방 및 치료용 조성물 및 이를 스크리닝하는 방법에 관한 것이다. 본 발명자들은 gp96의 세포내 거류에 대한 분자 닻(anchor)인 AIMP1의 기능을 모방하여 gp96의 표면 전좌(translocation)를 저해하는 신규 물질을 찾았고, 이들 물질이 in vitro, in vivo상에서 자가면역질환 중 SLE 형질을 완화하여 SLE를 예방 및 치료하는 효과가 있음을 확인하였다. 따라서, 본 발명은 상기 기작을 이용하여 SLE의 치료제를 스크리닝하고, SLE를 예방 또는 치료하는 새로운 방법을 제공한다.

    신규한 크로멘 유도체, 이의 약학적으로 허용가능한 염 또는 이의 이성질체, 이의 제조방법 및 이를 포함하는 PAR-1 관련 질환의 예방 또는 치료용 약학적 조성물
    87.
    发明公开
    신규한 크로멘 유도체, 이의 약학적으로 허용가능한 염 또는 이의 이성질체, 이의 제조방법 및 이를 포함하는 PAR-1 관련 질환의 예방 또는 치료용 약학적 조성물 有权
    新颖的色谱衍生物,药物接受的盐或其异构体,其制备方法和药物组合物,用于预防或治疗含有作为活性成分的PAR-1相关疾病

    公开(公告)号:KR1020120111886A

    公开(公告)日:2012-10-11

    申请号:KR1020110114754

    申请日:2011-11-04

    Abstract: PURPOSE: A pharmaceutical composition containing novel chromeme derivative, pharmaceutically acceptable salts or isomers thereof is provided to prevent or treat blood clot-related diseases or cancer. CONSTITUTION: A chromene derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing or treating PAR-1 activation-related diseases contains the chromene derivative, pharmaceutically acceptable salt, isomer as an active ingredient. A pharmaceutical composition for cardiovascular disease treatment aid contains the chromene derivative, pharmaceutically acceptable salt, or isomer as an active ingredient. A PAR-1 antagonist contains the chromene derivative, pharmaceutically acceptable salt, or isomer as an active ingredient.

    Abstract translation: 目的:提供含有新的chromeme衍生物,其药学上可接受的盐或异构体的药物组合物,用于预防或治疗血块相关疾病或癌症。 构成:色烯衍生物由化学式1表示。用于预防或治疗PAR-1活化相关疾病的药物组合物含有色烯衍生物,药学上可接受的盐,异构体作为活性成分。 用于心血管疾病治疗助剂的药物组合物含有色烯衍生物,药学上可接受的盐或异构体作为活性成分。 PAR-1拮抗剂含有色烯衍生物,药学上可接受的盐或异构体作为活性成分。

    신규한 카보니트릴 화합물, 이의 제조방법 및 이를포함하는 류마티스성 관절염, 골관절염, 파제트병,악성고칼슘혈증, 대사성골질환 및 각종 암의 치료 및예방을 위한 약제학적 조성물
    88.
    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 。

    카보니트릴 화합물을 포함하는 골다공증 및 치은 질환의치료 및 예방을 위한 약제학적 조성물
    89.
    发明授权
    카보니트릴 화합물을 포함하는 골다공증 및 치은 질환의치료 및 예방을 위한 약제학적 조성물 有权
    用于治疗或预防骨质疏松症的药物组合物和含有碳化物的化合物

    公开(公告)号:KR100877394B1

    公开(公告)日:2009-01-07

    申请号:KR1020070069467

    申请日:2007-07-11

    CPC classification number: A61K31/415 A61K31/121 A61K31/50

    Abstract: A pharmaceutical composition for treating and preventing osteoporosis is provided to improve the selectivity and inhibitory activity to cathepsin K. A pharmaceutical composition for treating and preventing osteoporosis comprises a carbonitrile compound represented by the formula 1, wherein n is 1 or 2; R1 is H, F-substituted or unsubstituted linear or branched saturated or unsaturated C1-C10 alkyl, C3-C7 cycloalkyl, C1-C10 alkoxy, C1-C10 alkylthio, C1-C10 hydroxyalkyl, C1-C10 alkylcarbonyl, C1-C10 alkylthio C1-C10 alkyl, C3-C7 cycloalkyl C1-C10 alkyl, C3-C7 cycloalkyl C1-C10 alkoxy, C1-C10 alkoxy C1-C10 alkyl, phenyl, ar-C1-C10 alkyl, or ar-C1-C10 alkoxy group; and R2 is 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 alkoxy group.

    Abstract translation: 提供了用于治疗和预防骨质疏松症的药物组合物,以提高对组织蛋白酶K的选择性和抑制活性。用于治疗和预防骨质疏松症的药物组合物包括由式1表示的腈化合物,其中n为1或2; R1是H,F-取代或未取代的直链或支链饱和或不饱和的C1-C10烷基,C3-C7环烷基,C1-C10烷氧基,C1-C10烷硫基,C1-C10羟基烷基,C1-C10烷基羰基,C1-C10烷硫基C1 -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烷氧基,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 1 -C 10烷氧基; 并且R 2是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烷氧基羰基或芳烷基-C 1 -C 10烷氧基 。

    신규한 1-[1-(3,4-디알콕시아릴)-피리딜메틸]-1H-피라졸화합물, 이의 제조방법 및 이를 포함하는 약제학적 조성물
    90.
    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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