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    • 专利摘要:
    AMINOPIRAZOL DERIVATIVE, ITS USE, PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS IT, AGENTS TO INHIBIT FGFR ACTIVITY AND TO PREVENT OR TREAT CANCERThe present invention relates to a compound represented by formula (I)(I)or a pharmacologically acceptable salt thereof, which can inhibit a kinase of the fibroblast growth factor receptor (FGFR) family in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C 6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, N02, a C1-4 haloalkyl group, a C1- group 6 alkyl, or similar <r1 e = "" r2 = "" together = "" form = "" uma = "" heterocyclyl = "" (substituted) = "" de = "" 3 = "" a = "" 10 = "" members = "" group = "" or = "" heteroaryl = "" 5 = "">; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group, and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.). </r1>
    公开号:BR112012008094A2
    申请号:R112012008094-6
    申请日:2010-08-05
    公开日:2020-08-18
    发明作者:Naoki Taka；Yoshito Nakanishi；Toshiyuki Mio；Lisha Wang；Weili Zhao；Masayuki Ohmori；Kyoko Takami；Masayuki Matsushita；Tadakatsu Hayase；Ikumi Hyodo；Masami Kochi；Hiroki Nishii；Hirosato Ebiike
    申请人:Chugai Seiyaku Kabushiki Kaisha；F. Hoffmann-La Roche Ag；
    IPC主号:
    专利说明:

    : 1/314 Invention Patent Descriptive Report for "AMINOPYRAZOL DERIVATIVE, ITS USE, PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS, AGENTS TO INHIBIT FGFR ACTIVITY AND TO PREVENT OR TREAT CANCER". 5 Technical Field The present invention relates to aminopyrazole derivatives and their uses.
    Background of the Invention Most of the currently promising molecularly targeted drugs against cancer are receptor tyrosine kinase inhibitors such as erlotinib and lapatinib.
    Many of them are highly effective against cancers with mutation, amplification, or overexpression of target genes.
    However, such molecular targeting agents cannot be effective against cancers in which genes that are not their targets are altered.
    Thus, there is still no established therapeutic method that is effective against such cancers.
    Inhibitors against new altered genes in cancer are supposed to make a major contribution to the treatment of cancer patients over whom conventional drugs have no effect.
    Fibroblast growth factor receptors (FGFRs) are kinases that belong to the receptor tyrosine kinase family.
    FGFR1, FGFR2, FGFR3, and FGFRA4 constitute the FGFR family.
    The ligand is a fibroblast growth factor (FGF), and 22 types of structurally similar proteins form the family.
    Each FGFR is known to be activated in overexpression, gene amplification, mutation, or translocation, and serves as a cause of cancer.
    The FGFR signal follows the MAPK track or PISK / YAKT track.
    In cancer, the signal is known to be involved in cell growth, angiogenesis, cell migration, invasion, metastasis, and the like (Non-patent document 1). The FGFR1 gene is known to be amplified in breast cancer and non-small cell lung cancer (Non-Patent Documents 2 and 3); mutated in glioblastoma (Non-patent document 4); translocated to generate a fusion protein in acute myelocytic leukemia (Document of
    权利要求:
    Claims (11)
    [1]
    1. Compound, characterized by the fact that it is represented by the following general formula (I), or a pharmaceutically acceptable salt thereof: R24Y A di, o | E | Xe. NH, R1 T
    N NA ON [[| Mrs.
    RN R4 to (1) where R1, R2, Ra, and Ra each independently represent the group listed below: R1 represents hydrogen, hydroxy, halogen, cyan, nitro, C14 haloalkyl, C1.6 alkyl, Ca.6 alkenyl, Ca.6 alkynyl, Ca; cycloalkyl, Ce19 aryl C14 alkyl, -OR5, -NReR7, - (CRgR9) nZ1, -C (OINR1i2R13, -SRi, -SOR15, - SO2R16, -NR17SO2R18, COOH, Ce-109 arila which is optionally substituted by one or more groups independently selected from group P, 5- to 10-membered heteroaryl or 3- to 10-membered heterocyclyl which is optionally substituted by one or more groups independently selected from group Q, -COR19, -COOR29, -OC (O ) R21, -NR22C (O) R23, -NR24C (S) Roa5, “C (S) NR26R27, -SO2NR28R29, -OSO2R30, -SO3R31, or -Si (R32) 3; R2 represents hydrogen, hydroxy, halogen, cyano , nitro, C14 haloalkyl, C1.6 alkyl, Ca.6 alkenyl, Ca.6 alkynyl, Ca; cycloalkyl, Ce19 aryl C14 alkyl, -OR5, -NReR7, - (CRR9) nZ1, -C (OINR12R13, - SRia4, -SOR15, - SO2R16, -NR17SO2R18, COOH, Cge-10 aryl which is optionally substituted by one or more groups independently selected from group P, 5 to 10 membered heteroaryl or 3 to 10 membered heterocyclyl finally replaced by one or more groups i independently selected from the group Q, -COR19, -COOR20, -OC (O) R21, -NR22C (O) R23, -NR24C (S) Ras, -C (S) INR26R27, -SO2NR28R29, -OSO2R30, -SO3R31 , or -Si (R32) 3; or R1 and R2, together with an atom attached to them, form 3 to 10 membered heterocyclic or 5 to 10 membered heteroaryl, wherein the heterocyclyl or heteroaryl is optionally substituted by halogen;
    R3 represents hydrogen, C1.5 alkyl, Ce10 aryl Cie alkyl, or C14 haloalkyl;
    Ra represents hydrogen, halogen, C1.3 alkyl, C1-3 perfluoroalkyl, cyano, methanesulfonyl, hydroxyl, alkoxy or amino;
    Are an indole or pyrrole;
    Rs represents C1.5 alkyl, Ca-7 cycloalkyl, C3-7 cycloalkyl C1.3 alkyl, Ca. alkenyl, Ca.6 alkynyl, Cia haloalkyl, C1.3 alkoxy C1.4 alkyl, C13 alkoxy C14 alkoxy C14 alkyl, Cia aminoalkyl, C14 alkylamino C14 alkyl, di (C14 alkyl) amino C1.4 alkyl, Ce-109 aryl, Ce-10 aryl C1.3 alkyl, or he-
    terocyclyl C1.3 alkyl of 3 to 10 members, heterocyclyl of 3 to 10 members, heteroaryl of 5 to 10 members, heteroaryl of 5 to 10 members C1.3 alkyl, C1-.6 monohydroxy alkyl, C1.6 di- hydroxy alkyl, or C1 + trihydroxy hydroxy which is optionally substituted by one or more groups independently selected from the group Q;
    Rs: and R7, which are the same or different, each representing hydrogen, C1.4 alkyl, C2.6 alkenyl, C2.6 alkynyl, C1.4 haloalkyl, C1.3 alkoxy C1.4 alkyl, Ce 109 aryl C1.3 alkyl, C1.3 heterocyclyl 3 to 10 membered alkyl, 5 to 10 membered heteroaryl C13 alkyl, Ci. Monohydroxy alkyl, C1-6 dihydroxy alkyl, C1.6 trihydroxy alkyl, 3 to 10 membered heterocyclyl,
    Cia aminoalkyl, C1, C14 alkylamino alkyl, di (C14 alkyl) amino C1.4 alkyl, or cyano (C1-3 alkyl); or Rg and R7, together with a nitrogen atom attached to them, form 3 to 10 membered heterocyclyl or 5 to 10 membered heteroaryl;
    n represents 1 to 3;
    Rg and Ro, which are the same or different, each representing hydrogen, C14 alkyl, or halogen; or alternatively, Rg and Ra, together with a carbon atom attached to them, form a cycloaliphatic ring;
    Z, represents hydrogen, NR1oR11, -OH, or 3 to 10 membered heterocyclyl or 5 to 10 membered heteroaryl which is optionally substituted
    replaced by one or more groups independently selected from group Q;
    Ra1o and Ru, which are the same or different, each representing C1.- 4 alkyl, Ca.6 alkenyl, C2.6 alkynyl, C1.4 haloalkyl, C1.3 alkoxy C14 alkyl,
    cyano (C13 alkyl), or C13 alkylsulfonyl C1-6 alkyl; or alternatively, Rio and Ru, together with a nitrogen atom attached to them, form 3 to 10 membered heterocyclyl or 5 to 10 membered heteroaryl; R12 € R13, which are the same or different, each representing hydrogen, Ci, alkyl, C2.6 alkenyl, C2.6 alkynyl, C1.4 haloalkyl, C1.3 alkoxy C14 alkyl, Ce-10 aryl, 5 to 10 membered heteroaryl, 3 to membered heterocyclyl, Ce-10 aryl Cia alkyl, 3 to 10 membered C1-3 heterocyclyl, 5 to 10 membered heteroaryl C1.3 alkyl, cyano (C1.3 alkyl ), C13 alkylsulfonyl, C14 alkyl, 3 to 10 membered cycloaliphatic ring, heteroaryl of
    10 5 to 10 members, or 3 to 10 member heterocyclyl; or alternatively, R12 and R13, together with a nitrogen atom attached to them, form 3 to 10 membered heterocyclyl or 5 to 10 membered heteroaryl which is optionally substituted by one or more groups independently selected from the group Q;
    Ra1a represents Ci, alkyl, C2.6 alkenyl, Ca.6 alkynyl, C1.4 haloalkyl, Ce.109 aryl which is optionally substituted by one or more groups independently selected from the group P, or 5 to 10 membered heteroaryl. bros or 3 to 10 membered heterocyclyl which is optionally substituted by one or more groups independently selected from group Q;
    R15 represents C1.4 alkyl, Ca.6 alkenyl, Ca.6 alkynyl, C14 haloalkyl, Ceg-19 aryl which is optionally substituted by one or more groups independently selected from the group P, or heteroaryl of 5 to 10 members or 3 to 10 membered heterocyclyl which is optionally substituted by one or more groups independently selected from group Q;
    Ra16 represents C1., Alkyl, C2.6 alkenyl, C2.6 alkynyl, C1.4 haloalkyl, Ce.10 aryl which is optionally substituted by one or more groups independently selected from the group P, or 5 to 10 mem heteroaryl - bros or 3 to 10 membered heterocyclyl which is optionally substituted by one or more groups independently selected from group Q;
    R17 represents hydrogen or C14 alkyl;
    R13 represents C1., Alkyl, C2.6 alkenyl, C2.6 alkynyl, C1.4 haloalkyl, Ce.109 aryl which is optionally substituted by one or more groups independently selected from the group P, or 5 to 10 mem heteroaryl - bros or 3 to 10 membered heterocyclyl which is optionally substituted by one or more groups independently selected from group Q; R19 represents hydrogen, C1.4 alkyl, Ca .; cycloalkyl, C1.4 haloalkyl, Ce.109 aryl, or 5 to 10 membered heteroaryl or 3 to membered heterocyclyl which is optionally substituted by one or more groups independently selected from group Q; R2o represents C1.4 alkyl, Ca, 7 cycloalkyl, C14 haloalkyl, Ce. 10 aryl, 5 to 10 membered heteroaryl, or 3 to 10 membered heterocyclyl; 10 R2, represents C1.4 alkyl, C3.7 cycloalkyl, C14 haloalkyl, Ce-10 aryl, 5 to 10 membered heteroaryl, or 3 to 10 membered heterocyclyl; R22 represents hydrogen, C14 alkyl, or C1.4 haloalkyl; R> 23 represents hydrogen, C1.4 alkyl, C3.7 cycloalkyl, C1.4 haloalkyl, Ce.105 aryl, 5 to 10 membered heteroaryl, or 3 to 10 membered heterocyclyl; R24 represents hydrogen, C14 alkyl, or C1.4 haloalkyl; R25 represents C1.4 alkyl, Ca, 7 cycloalkyl, C14 haloalkyl, Ce. 10 aryl, 5 to 10 membered heteroaryl, or 3 to 10 membered heterocyclyl; R26 € R27, which are the same or different, each representing hydrogen, Ci alkyl, Ca.6 alkenyl, Ca.6 alkynyl, C14 haloalkyl, C13 alkoxy C14 alkyl, Ce-109 aryl, heteroaryl from 5 to 10 members, heterocyclyl from 3 to 10 members, Cçe.10 aryl C1.4 alkyl, heterocyclyl C1.3 alkyl from 3 to 10 members, heteroaryl from 5 to 10 members C1-3 alkyl, cyan (C1-3 alkyl), C1-3 alkylsulfonyl C14 alkyl, or 3 to 10 membered cycloaliphatic ring; or alternatively, Rax6 and R27, together with a nitrogen atom attached to them, form 3 to 10 membered heterocyclyl or 5 to 10 membered heteroaryl; R28 AND R29, which are the same or different, each representing hydrogen, C14 alkyl, C2.6 alkenyl, Ca.6 alkynyl, C14 haloalkyl, C1.3 alkoxy C14 alkyl, Ce-10 aryl, 5-heteroaryl to 10 members, heterocyclyl of 3 to 10 members, Ce.10 aryl C1.4 alkyl, heterocyclyl C1.3 alkyl of 3 to 10 members, heteroaryl of 5 to 10 members C1.3 alkyl, cyan (C1.3 alkyl), C1.3 alkylsulfonyl C14 alkyl, or 3 to 10 membered cycloaliphatic ring; or alternately
    tively, R28 and R29, together with a nitrogen atom attached to them, form 3 to 10 membered heterocyclyl or 5 to 10 membered heteroaryl; R3o represents C1.4 alkyl, C3.7 cycloalkyl, C14 haloalkyl, Ce 10 aryl, 5 to 10 membered heteroaryl, or 3 to 10 membered heterocyclyl; R31 represents C14 alkyl, C3.7 cycloalkyl, C1.4 haloalkyl, Ce-10 aryl, 5 to 10 membered heteroaryl, or 3 to 10 membered heterocyclyl; R32 represents C14 alkyl or Cç.10 aryl; <group P> halogen, C1.4 alkyl, C14 haloalkyl, -OH, C1-3 alkoxy, C1.3 haloalkoxy, 3- to 10-membered heterocyclylamino, -SO2R16, -CN, -NO ;, and heterocyclyl from 3 to 10 members; <group Q> halogen, Cia alkyl, Ci, haloalkyl, -OH, C1.3 alkoxy, C1-6 monohydroxy alkyl, C1.6 dihydroxy alkyl, C1.6 trihydroxy alkyl, heterocyclyl amine 3 to 10 members, -SO2R16, -CN, -NO>, C3-7 cycloalkyl, -COR 19, and 3 to 10 membered heterocyclyl which is optionally substituted by Ci alkyl, with the proviso that said compound represented by the general formula ( 1) exclude [5-amino-1- (2-methyl-1H-benzimidazo | -5-1) -1H-pyrazol-4-iI) - [5- (4-trifluoromethyl-phenyl) -1H-indole- 2-yl] -methanone; and wherein the cycloalkyl refers to a saturated or partially saturated cyclic monovalent aliphatic hydrocarbon group.
    [2]
    2. Compound according to claim 1, or a pharmaceutically acceptable salt thereof, characterized by the fact that R; 3 represents hydrogen, C1.4 alkyl, Ce.109 aryl C14 alkyl, or C1.3 perfluoroalkyl .
    [3]
    A compound according to claim 1 or 2, or a pharmaceutically acceptable salt thereof, characterized by the fact that it is represented by the following formula:
    CA N P & NAN
    SW TU
    [4]
    4. Compound, characterized by the fact that it is selected from the group consisting of: [5-amino-1- (2-methyl-3H-benzimidazo] -5-yl) -1H-pyrazol-4-i1] - (1H - indol-2-yl) -netanone L-malate; [5-amino-1- (2-methyl-1 H-benzimidazo | -5-i1) -1H-pyrazol-4-i1] - (1H-indol-2-yl) -netanone hydrochloride; and [5-amino-1- (2-methyl-1 H-benzimidazol-5-yl) -1 H-pyrazol-4-11) - (1H-indol-2-yl) -methanone 1-methanesulfonate monohydrate.
    [5]
    A compound according to any one of claims 1 to 3, or a pharmaceutically acceptable salt thereof, characterized in that the pharmaceutically acceptable salt is selected from the group consisting of acetate, succinate, fumarate, maleate, tartrate, citrate, lactate , malate, stearate, benzoate, methanesulfonate and p-toluenesulfonate.
    [6]
    6. Pharmaceutical composition, characterized by the fact that it comprises the compound, as defined in any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof; and a vehicle.
    [7]
    7. Agent for use in a method to prevent or treat cancer, characterized in that it comprises the compound as defined in any one of claims 1 to 5 as an active ingredient or a pharmaceutically acceptable form thereof.
    [8]
    8. Agent for use in a method to prevent or treat cancer according to claim 7, characterized by the fact that the cancer is at least one selected from the group consisting of: breast cancer, acute myelocytic leukemia, pancreatic cancer , bladder cancer, prostate cancer, esophageal cancer, angiogenesis, stomach cancer, uterine body cancer, ovarian cancer, brain tumor, colon cancer, multiple myeloma, hepatocarcinoma, lung cancer, and thyroid cancer.
    [9]
    9. Composition, characterized by the fact that it comprises the compound, as defined in any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof for use in a method to prevent or treat cancer, comprising administering a pharmaceutical amount
    maceutically effective use of said composition to a patient in need of cancer prevention or treatment.
    [10]
    10. Use of the compound, as defined in any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, characterized by the fact that it is in the production of an agent to prevent or treat cancer.
    [11]
    A compound according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, characterized in that it is for use in a method for preventing or treating cancer
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    法律状态:
    2020-09-01| B06F| Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]|
    2020-09-15| B07D| Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]|Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS. |
    2021-03-16| B07E| Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]|
    2021-03-23| B06U| Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]|
    2021-07-06| B11B| Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements|
    2021-11-03| B350| Update of information on the portal [chapter 15.35 patent gazette]|
    优先权:
    申请号 | 申请日 | 专利标题
    JP2009-184822|2009-08-07|
    JP2009184822|2009-08-07|
    PCT/JP2010/063315|WO2011016528A1|2009-08-07|2010-08-05|Aminopyrazole derivative|
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