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    NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION
    22.
    发明申请
    NOVEL AMINOPYRIDINE DERIVATIVES HAVING AURORA A SELECTIVE INHIBITORY ACTION 审中-公开
    具有选择性抑制作用的新型氨基吡啶衍生物

    公开(公告)号：WO2010111056A1

    公开(公告)日：2010-09-30

    申请号：PCT/US2010/027279

    申请日：2010-03-15

    Applicant: BANYU PHARMACEUTICAL CO., LTD. ,  VERTEX PHARMACEUTICALS INCORPORATED ,  BINCH, Hayley ,  HASHIMOTO, Masaya ,  MORTIMORE, Michael ,  OHKUBO, Mitsuru ,  SUNAMI, Tomoko

    Inventor： BINCH, Hayley ,  HASHIMOTO, Masaya ,  MORTIMORE, Michael ,  OHKUBO, Mitsuru ,  SUNAMI, Tomoko

    IPC: A61K31/535 ,  C07D401/04

    CPC classification number: A61K31/535 ,  C07D401/14 ,  C07D417/14

    Abstract: The present invention relates to a compound of Formula (I): wherein: R 1 is H, -NHCOOR 1a , C 5-6 cycloalkyl, or phenyl; where the cycloalkyl and phenyl each independently may be substituted with one to three of the same or different substituents selected from R 10 ; R 1a is C 1-3 alkyl which may be substituted with one to three of the same or different substituents selected from F and Cl; R 2 is H, -COOH, -CH 2 COOH, -COOR 2a , or -CH 2 COOR 2a ; R 2a is C 1-2 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from halogen atoms; R 3 is H, C 1-6 alkyl, where the alkyl may be substituted with one to three of the same or different substituents selected from R 11 ; R 10 is F, Cl, CF 3 , or C 1-2 alkyl; R 11 is halogen atom, hydroxy, or cyano; W is selected from: W 2a is H, halogen atom, cyano, C 1-2 alkyl, or C 3-5 cycloalkyl, or a pharmaceutically acceptable salt or ester thereof.

    Abstract translation: 本发明涉及式（I）的化合物：其中：R1是H，-NHCOOR1a，C5-6环烷基或苯基; 其中环烷基和苯基各自独立地可以被一至三个相同或不同的选自R 10的取代基取代; R 1a是可以被一至三个相同或不同的选自F和Cl的取代基取代的C 1-3烷基; R2是H，-COOH，-CH2COOH，-COOR2a或-CH2COOR2a; R2a是C1-2烷基，其中烷基可以被一至三个相同或不同的选自卤素原子的取代基取代; R3是H，C1-6烷基，其中烷基可以被一至三个相同或不同的选自R11的取代基取代; R 10是F，Cl，CF 3或C 1-2烷基; R11是卤素原子，羟基或氰基; W选自：W2a是H，卤素原子，氰基，C1-2烷基或C3-5环烷基，或其药学上可接受的盐或酯。

    PYRIMIDOPYRIMIDOINDAZOLE DERIVATIVE
    23.
    发明申请
    PYRIMIDOPYRIMIDOINDAZOLE DERIVATIVE 审中-公开
    吡咯并吡啶衍生物衍生物

    公开(公告)号：WO2010098367A1

    公开(公告)日：2010-09-02

    申请号：PCT/JP2010/052910

    申请日：2010-02-18

    Applicant: BANYU PHARMACEUTICAL CO.,LTD. ,  GOTO, Yasuhiro ,  NIIYAMA, Kenji ,  SUNAMI, Satoshi ,  TAKAHASHI, Keiji

    Inventor： GOTO, Yasuhiro ,  NIIYAMA, Kenji ,  SUNAMI, Satoshi ,  TAKAHASHI, Keiji

    IPC: C07D487/14 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/551 ,  A61P35/00 ,  A61P43/00 ,  C07D519/00

    CPC classification number: C07D487/14 ,  C07D519/00

    Abstract: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a):; R 1 means a -(C=O) a O b (C1-C6)alkyl group, a -(C=O) a O b (C2-C6)alkenyl group, a -(C=O) a O b (C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R 2 and R 3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a -(C=O) a O b (C1-C6)alkyl group or a group of -(C=O) a N(R 1e )R 2e ; R 4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.

    Abstract translation: 本发明提供一种用于癌症化疗或放射治疗的新型抗癌剂或敏化剂。 通式（I）的化合物：其中A表示芳基或杂芳基，或式（a）的基团：。 R1表示 - （C = O）aOb（C1-C6）烷基， - （C = O）aOb（C2-C6）烯基， - （C = O）aOb（C3-C6） 芳基或杂芳基; R2和R3各自表示氢原子，卤素原子，羟基，羧基，α-（C = O）aOb（C1-C6）烷基或 - （C = O）aN（R1e） R2E; R4表示氢原子或（C1-C6）烷基等具有优异的Wee1激酶抑制作用，因此可用于医学领域，特别是在各种癌症治疗领域。

    SUBSTITUTED SPIROCHROMANONE DERIVATIVES AS ACC INHIBITORS
    27.
    发明申请
    SUBSTITUTED SPIROCHROMANONE DERIVATIVES AS ACC INHIBITORS 审中-公开
    作为ACC抑制剂的替代螺吡喃酮衍生物

    公开(公告)号：WO2008088689A1

    公开(公告)日：2008-07-24

    申请号：PCT/US2008/000223

    申请日：2008-01-08

    Applicant: MERCK & CO., INC. ,  BANYU PHARMACEUTICAL CO., LTD. ,  IINO, Tomoharu ,  JONA, Hideki ,  SHIBATA, Jun ,  SHIMAMURA, Tadashi ,  YAMAKAWA, Takeru ,  YANG, Lihu

    Inventor： IINO, Tomoharu ,  JONA, Hideki ,  SHIBATA, Jun ,  SHIMAMURA, Tadashi ,  YAMAKAWA, Takeru ,  YANG, Lihu

    IPC: C07D491/10 ,  A61K31/438 ,  A61P3/00

    CPC classification number: C07D519/00 ,  C07D491/10

    Abstract: The invention relates to a compound of a general formula (I): wherein Ar 1 represents a group formed from an aromatic ring selected from a group consisting of indole, benzimidazole and 1,2-benzisoxazole, having R 3 and R 4 , and optionally having a substituent selected from a group consisting of a halogen atom, a hydroxyl group, a C1-C6 alkyl group, a halo-C1-C6 alkyl group, a hydroxy-C1-C6 alkyl group, a cyclo-C3-C6 alkyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group and carbamoyl group; R 1 represents a phenyl group optionally substituted with a carboxyl group, a tetrazolyl group optionally substituted with a C2-C7 alkanoyloxy-C1-C6 alkyl group, a pyridyl group optionally substituted with a C1-C6 alkyl group or a carboxyl group, a dihydro-1,2,4-triazolyl group optionally substituted with an oxo group, or a dihydro-1,2,4-oxadiazolyl group optionally substituted with an oxo group; R 2 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group, or a C1-C6 alkoxy group; and R 3 and R 4 each independently represent a hydrogen atom, a halogen atom, nitro group, a cyclo-C3-C6 alkyl group, a carbamoyl group optionally substituted with a C1-C6 alkyl or cyclo-C3-C6 alkyl group, a C1-C6 alkoxy group optionally substituted with a hydroxyl group, or a C1-C6 alkyl group optionally substituted with a hydroxyl group. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.

    Abstract translation: 本发明涉及通式（I）的化合物：其中Ar 1表示由选自吲哚，苯并咪唑和1,2-苯并异恶唑的芳环形成的基团，其中R 并且任选地具有选自卤素原子，羟基，C 1 -C 6烷基，卤代C 1 -C 6烷基的取代基， C 1 -C 6烷基，羟基-C 1 -C 6烷基，环-C 3 -C 6烷基，C 1 -C 6烷氧基，卤代-C 1 -C 6烷氧基和氨基甲酰基; R 1表示任选被羧基取代的苯基，任选被C 2 -C 7烷酰氧基-C 1 -C 6烷基取代的四唑基，任选被C 1 -C 6烷基取代的吡啶基 或任选被氧代基取代的羧基，二氢-1,2,4-三唑基或任选被氧代基取代的二氢-1,2,4-恶二唑基; R 2表示氢原子，卤素原子，C 1 -C 6烷基或C 1 -C 6烷氧基; R 3和R 4各自独立地表示氢原子，卤原子，硝基，环-C 3 -C 6烷基，任选被 C 1 -C 6烷基或环-C 3 -C 6烷基，任选被羟基取代的C 1 -C 6烷氧基或任选被羟基取代的C 1 -C 6烷基。 本发明的化合物可用作各种ACC相关疾病的治疗剂。

    SUBSTITUTED SPIROCHROMANONE DERIVATIVES AS ACC INHIBITORS
    28.
    发明申请
    SUBSTITUTED SPIROCHROMANONE DERIVATIVES AS ACC INHIBITORS 审中-公开
    作为ACC抑制剂的替代螺吡喃酮衍生物

    公开(公告)号：WO2008088688A1

    公开(公告)日：2008-07-24

    申请号：PCT/US2008/000221

    申请日：2008-01-08

    Applicant: MERCK & CO., INC. ,  BANYU PHARMACEUTICAL CO., LTD. ,  IINO, Tomoharu ,  JONA, Hideki ,  SHIBATA, Jun ,  SHIMAMURA, Tadashi ,  YAMAKAWA, Takeru ,  YANG, Lihu

    Inventor： IINO, Tomoharu ,  JONA, Hideki ,  SHIBATA, Jun ,  SHIMAMURA, Tadashi ,  YAMAKAWA, Takeru ,  YANG, Lihu

    IPC: C07D491/10 ,  A61K31/438 ,  A61P3/00 ,  C07D495/04

    CPC classification number: C07D519/00 ,  C07D491/10

    Abstract: The invention relates to a compound of a general formula (I): (I) wherein Ar 1 represents a group formed from an aromatic ring selected from a group consisting of indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R 1 and R 2 each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(R a )-Q2-R b ; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R 3 and R 4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-C6 alkyl group, a carbamoyl group optionally substituted with a C1-C6 alkyl or cyclo-C3-C6 alkyl group, or a group of -N(R e )R f ; an optionally-substituted C2-C7 alkanoyl, C1-C6 alkoxy, C2-C7 alkoxycarbonyl, cyclo-C3-C6 alkyloxycarbonyl, C1-C6 alkylsulfonyl, C1-C6 alkylthio, cyclo-C3-C6 alkyloxy, cyclo-C3-C6 alkyl-C1-C6 alkoxy, cyclo-C3-C6 alkylsulfonyl, cyclo-C3-C6 alkylthio or cyclo-C3-C6 alkyl-C1-C6 alkylthio group; or an optionally-substituted C1-C6 alkyl group; T and U each represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.

    Abstract translation: 本发明涉及通式（I）的化合物：（I）其中Ar 1表示由选自吲哚，1H-吲唑，2H-吲唑的芳环形成的基团 ，1H-噻吩并[2,3-c]吡唑，1H-吡唑并[3,4-b]吡啶，苯并[b]呋喃，苯并咪唑，苯并恶唑，1,2-苯并异恶唑和咪唑并[1,2-a] ; R 1和R 2各自表示氢原子，卤素原子，氰基，C 2 -C 6烯基，C 1 -C 6烷氧基，卤代 C1-C6烷氧基，环-C3-C6烷氧基，C2-C7烷酰基，卤代-C2-C7烷酰基，C2-C7烷氧基羰基，卤代-C2-C7烷氧基羰基， C 3 -C 6烷氧基羰基，芳烷氧基羰基，氨基甲酰基-C 1 -C 6烷氧基，羧基-C 2 -C 6烯基或-Q 1 -N（R a a O） [R b'/ SUP>; 任选取代的C 1 -C 6烷基，芳基或杂环基; 或具有芳基或杂环基的C 1 -C 6烷基或C 2 -C 6烯基; R 3和R 4各自表示氢原子，卤素原子，硝基，环-C 3 -C 6烷基，任选被C1取代的氨基甲酰基 -C 6烷基或环-C 3 -C 6烷基，或-N（R e）O的基团。 任选取代的C 2 -C 7烷酰基，C 1 -C 6烷氧基，C 2 -C 7烷氧基羰基，环C 3 -C 6烷氧基羰基，C 1 -C 6烷基磺酰基，C 1 -C 6烷硫基，环C 3 -C 6烷氧基，环C 3 -C 6烷基 - C 1 -C 6烷氧基，环-C 3 -C 6烷基磺酰基，环-C 3 -C 6烷硫基或环-C 3 -C 6烷基-C 1 -C 6烷硫基; 或任选取代的C 1 -C 6烷基; T和U各自表示氮原子或次甲基; V表示氧原子或硫原子。 本发明的化合物可用作各种ACC相关疾病的治疗剂。

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