JP2019011375A5 - - Google Patents
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- JP2019011375A5 JP2019011375A5 JP2018201775A JP2018201775A JP2019011375A5 JP 2019011375 A5 JP2019011375 A5 JP 2019011375A5 JP 2018201775 A JP2018201775 A JP 2018201775A JP 2018201775 A JP2018201775 A JP 2018201775A JP 2019011375 A5 JP2019011375 A5 JP 2019011375A5
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- Prior art keywords
- alkyl
- pharmaceutically acceptable
- acceptable salt
- methyl
- pharmaceutical composition
- Prior art date
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- 125000000217 alkyl group Chemical group 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 26
- 150000003839 salts Chemical class 0.000 claims 24
- 239000011780 sodium chloride Substances 0.000 claims 24
- 239000008194 pharmaceutical composition Substances 0.000 claims 22
- 125000005843 halogen group Chemical group 0.000 claims 20
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 13
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 12
- 108040005185 1-phosphatidylinositol-3-kinase activity proteins Proteins 0.000 claims 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 11
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 11
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 9
- -1 -OH Chemical group 0.000 claims 8
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 7
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 7
- 125000006601 (C1-C3) alkylcarbamyl group Chemical group 0.000 claims 6
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 5
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 5
- 239000003937 drug carrier Substances 0.000 claims 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 3
- 125000006698 (C1-C3) dialkylamino group Chemical group 0.000 claims 3
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 206010069351 Acute lung injury Diseases 0.000 claims 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000009856 Lung Disease Diseases 0.000 claims 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 125000005842 heteroatoms Chemical group 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000006599 (C1-C3) alkylaminocarbonylamino group Chemical group 0.000 claims 1
- 125000006597 (C1-C3) alkylcarbonylamino group Chemical group 0.000 claims 1
- 125000006595 (C1-C3) alkylsulfinyl group Chemical group 0.000 claims 1
- 125000006594 (C1-C3) alkylsulfony group Chemical group 0.000 claims 1
- 125000006602 (C1-C3) alkylsulfonylamino group Chemical group 0.000 claims 1
- 125000004455 (C1-C3) alkylthio group Chemical group 0.000 claims 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- VZUKFCYWZYFFIL-UHFFFAOYSA-N 1-[1-[5-chloro-2-methoxy-4-methyl-3-[1-(1-methylpiperidin-4-yl)pyrazol-4-yl]phenyl]ethyl]-3-methylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C(=C1)C=NN1C1CCN(C)CC1 VZUKFCYWZYFFIL-UHFFFAOYSA-N 0.000 claims 1
- YPLUJLSBEXFVAU-UHFFFAOYSA-N 1-[1-[5-chloro-3-[1-[2-(dimethylamino)ethyl]pyrazol-4-yl]-2-methoxy-4-methylphenyl]ethyl]-3-methylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C=1C=NN(CCN(C)C)C=1 YPLUJLSBEXFVAU-UHFFFAOYSA-N 0.000 claims 1
- WPJDICFYMRHROM-UHFFFAOYSA-N 1-[4-[4-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]pyrazol-1-yl]piperidin-1-yl]ethanone Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C(=C1)C=NN1C1CCN(C(C)=O)CC1 WPJDICFYMRHROM-UHFFFAOYSA-N 0.000 claims 1
- JBDVKCGETSVNRB-UHFFFAOYSA-N 2-[4-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-methylphenyl]pyrazol-1-yl]-N,N-dimethylacetamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C=1C=NN(CC(=O)N(C)C)C=1 JBDVKCGETSVNRB-UHFFFAOYSA-N 0.000 claims 1
- XOCBICZFWUYTBH-UHFFFAOYSA-N 2-[4-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-ethoxy-6-methylphenyl]pyrazol-1-yl]-N-methylacetamide Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C=1C=NN(CC(=O)NC)C=1 XOCBICZFWUYTBH-UHFFFAOYSA-N 0.000 claims 1
- CLDPAHDXVKDZMW-UHFFFAOYSA-N 2-[4-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]pyrazol-1-yl]-N,N-dimethylacetamide Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C=1C=NN(CC(=O)N(C)C)C=1 CLDPAHDXVKDZMW-UHFFFAOYSA-N 0.000 claims 1
- BXONZXFPKQOFNN-UHFFFAOYSA-N 2-[4-[3-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-5-chloro-2-methoxy-6-methylphenyl]pyrazol-1-yl]ethanol Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(Cl)C(C)=C1C=1C=NN(CCO)C=1 BXONZXFPKQOFNN-UHFFFAOYSA-N 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- NLHXYFCSZPHVIO-UHFFFAOYSA-N 5-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-4-ethoxy-2-methyl-3-(1-methylpyrazol-4-yl)benzonitrile Chemical compound CCOC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(C#N)C(C)=C1C=1C=NN(C)C=1 NLHXYFCSZPHVIO-UHFFFAOYSA-N 0.000 claims 1
- PFWHUFUHASEOFP-UHFFFAOYSA-N 5-[1-(4-amino-3-methylpyrazolo[3,4-d]pyrimidin-1-yl)ethyl]-4-methoxy-2-methyl-3-(1-methylpyrazol-4-yl)benzonitrile Chemical compound COC1=C(C(C)N2C3=NC=NC(N)=C3C(C)=N2)C=C(C#N)C(C)=C1C=1C=NN(C)C=1 PFWHUFUHASEOFP-UHFFFAOYSA-N 0.000 claims 1
- 206010000880 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 206010003246 Arthritis Diseases 0.000 claims 1
- 208000006673 Asthma Diseases 0.000 claims 1
- 208000003950 B-Cell Lymphoma Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003432 Bone Disease Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010012818 Diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010017758 Gastric cancer Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010021972 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000001083 Kidney Disease Diseases 0.000 claims 1
- 208000008456 Leukemia, Myelogenous, Chronic, BCR-ABL Positive Diseases 0.000 claims 1
- 208000007046 Leukemia, Myeloid, Acute Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025135 Lupus erythematosus Diseases 0.000 claims 1
- 206010028372 Muscular weakness Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 102000030951 Phosphotransferases Human genes 0.000 claims 1
- 108091000081 Phosphotransferases Proteins 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims 1
- 206010040767 Sjogren's syndrome Diseases 0.000 claims 1
- 206010046766 Uterine cancer Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 201000005794 allergic hypersensitivity disease Diseases 0.000 claims 1
- 125000006598 aminocarbonylamino group Chemical group 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 201000001320 atherosclerosis Diseases 0.000 claims 1
- 201000005216 brain cancer Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 201000006934 chronic myeloid leukemia Diseases 0.000 claims 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 230000003053 immunization Effects 0.000 claims 1
- 238000002649 immunization Methods 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 239000000178 monomer Substances 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 230000036473 myasthenia Effects 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 201000004681 psoriasis Diseases 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 200000000008 restenosis Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Claims (35)
- 下記式:
XはCR9またはNであり;
WはCR7またはNであり;
YはCR8、CR8a、またはNであり;
Zは結合またはC(=O)であり;
但し、−W=Y−Z−が、−CR7=CR8−、−N=CR8−、−CR7=CR8a−C(=O)−、−N=CR8a−C(=O)−、または−CR7=N−C(=O)−であることを条件とし;
R1はC1−3アルキルであり;
R2はハロ、C1−6アルキル、C1−6アルコキシ、C1−6ハロアルキル、C1−6ハロアルコキシ、フェニル、または5〜6員ヘテロアリールであり;ここで前記フェニルおよび5〜6員ヘテロアリールは、それぞれ、ハロ、OH、CN、C1−4アルキル、C1−4アルコキシ、およびC1−4ハロアルコキシから独立して選択される、1個、2個、3個または4個の置換基により置換されていてもよく;
R4はH、ハロ、OH、CN、C1−4アルキル、C1−4ハロアルキル、C1−4アルコキシ、またはC1−4ハロアルコキシであり;
R5はハロ、OH、CN、C1−4アルキル、C1−4ハロアルキル、C1−4アルコキシ、C1−4ハロアルコキシ、またはシクロプロピルであり;
R6はH、ハロ、OH、CN、C1−4アルキル、C1−4ハロアルキル、C1−4アルコキシ、またはC1−4ハロアルコキシであり;
R7はHまたはC1−4アルキルであり;
R8はH、ハロ、−OH、−CN、C1−6アルキル、C2−6アルケニル、C2−6アルキニル、C1−6ハロアルキル、Cy2、−(C1−3アルキレン)−Cy2、ORa2、SRa2、C(=O)Rb2、C(=O)NRc2Rd2、C(=O)ORa2、OC(=O)Rb2、OC(=O)NRc2Rd2、NRc2Rd2、NRc2C(=O)Rb2、NRc2C(=O)ORb2、NRc2C(=O)NRc2Rd2、C(=NRe)Rb2、C(=NRe)NRc2Rd2、NRc2C(=NRe)NRc2Rd2、NRc2S(=O)Rb2、NRc2S(=O)2NRc2Rd2、S(=O)Rb2、S(=O)2Rb2、またはS(=O)2NRc2Rd2であり;ここで前記C1−6アルキル、C2−6アルケニル、C2−6アルキニルは、それぞれ、1個、2個、3個または4個の独立して選択されるR11基により置換されていてもよく;
R8aはH、ハロ、−CN、C1−6アルキル、C2−6アルケニル、C2−6アルキニル、C1−6ハロアルキル、Cy2、−(C1−3アルキレン)−Cy2、C(=O)Rb2、C(=O)NRc2Rd2、C(=O)ORa2、NRc2Rd2、NRc2C(=O)Rb2、NRc2C(=O)ORb2、NRc2C(=O)NRc2Rd2、NRc2S(=O)Rb2、NRc2S(=O)2NRc2Rd2、S(=O)Rb2、S(=O)2Rb2、またはS(=O)2NRc2Rd2であり;ここで前記C1−6アルキル、C2−6アルケニル、C2−6アルキニルは、それぞれ、1個、2個、3個または4個の独立して選択されるR11基により置換されていてもよく;
R9はH、ハロ、OH、CN、C1−4アルキル、C1−4ハロアルキル、C1−4アルコキシ、またはC1−4ハロアルコキシであり;
R10はHまたはC1−4アルキルであり;
各ReはH、CN、OH、C1−4アルキル、およびC1−4アルコキシから独立して選択され;
各R3bは、Cy1、−(C1−3アルキレン)−Cy1、ハロ、CN、NO2、C1−6アルキル、C2−6アルケニル、C2−6アルキニル、C1−6ハロアルキル、ORa1、SRa1、C(=O)Rb1、C(=O)NRc1Rd1、C(=O)ORa1、OC(=O)Rb1、OC(=O)NRc1Rd1、NRc1Rd1、NRc1C(=O)Rb1、NRc1C(=O)ORb1、NRc1C(=O)NRc1Rd1、C(=NRe)Rb1、C(=NRe)NRc1Rd1、NRc1C(=NRe)NRc1Rd1、NRc1S(=O)Rb1、NRc1S(=O)2NRc1Rd1、S(=O)Rb1、S(=O)2Rb1、およびS(=O)2NRc1Rd1から独立して選択され;ここで前記C1−6アルキル、C2−6アルケニル、C2−6アルキニルは、それぞれ、1個、2個または3個の独立して選択されるR11基で置換されていてもよく;
各Cy1は、それぞれが1個、2個、3個または4個の独立して選択されるR11基で置換されていてもよい、C3−7シクロアルキル、4〜7員ヘテロシクロアルキル、フェニル、および5〜6員ヘテロアリールから独立して選択され;
各Ra1、Rb1、Rc1、およびRd1は、H、C1−6アルキル、C1−6ハロアルキル、C2−6アルケニル、C2−6アルキニル、C3−7シクロアルキル、4〜7員ヘテロシクロアルキル、フェニル、および5〜6員ヘテロアリールから独立して選択され;ここで前記C1−6アルキル、C2−6アルケニル、C2−6アルキニル、C3−7シクロアルキル、4〜7員ヘテロシクロアルキル、フェニルおよび5〜6員ヘテロアリールは、それぞれ、1個、2個もしくは3個の独立して選択されるR11基で置換されていてもよいか;
またはRc1およびRd1は、それらが結合しているN原子と一緒になって、−OHもしくはC1−3アルキルで置換されていてもよい、4員、5員、6員もしくは7員ヘテロシクロアルキル基を形成し;
各Cy2は、それぞれが1個、2個、3個または4個の独立して選択されるR11基で置換されていてもよい、C3−7シクロアルキル、4〜7員ヘテロシクロアルキル、フェニル、5〜6員ヘテロアリール、または9〜10員二環式ヘテロアリールから独立して選択され;
各Ra2、Rb2、Rc2、およびRd2は、H、C1−6アルキル、C1−6ハロアルキル、C2−6アルケニル、C2−6アルキニル、C3−7シクロアルキル、4〜7員ヘテロシクロアルキル、フェニル、および5〜6員ヘテロアリールから独立して選択され;ここで前記C1−6アルキル、C2−6アルケニル、C2−6アルキニル、C3−7シクロアルキル、4〜7員ヘテロシクロアルキル、フェニルおよび5〜6員ヘテロアリールは、それぞれ、1個、2個もしくは3個の独立して選択されるR11基で置換されていてもよいか;
またはRc2およびRd2は、それらが結合しているN原子と一緒になって、−OHもしくはC1−3アルキルで置換されていてもよい、4員、5員、6員もしくは7員ヘテロシクロアルキル基を形成し;
各R11は、OH、NO2、CN、ハロ、C1−3アルキル、C2−3アルケニル、C2−3アルキニル、C1−3ハロアルキル、シアノ−C1−3アルキル、HO−C1−3アルキル、C1−3アルコキシ−C1−3アルキル、C3−7シクロアルキル、C1−3アルコキシ、C1−3ハロアルコキシ、アミノ、C1−3アルキルアミノ、ジ(C1−3アルキル)アミノ、チオ、C1−3アルキルチオ、C1−3アルキルスルフィニル、C1−3アルキルスルホニル、カルバミル、C1−3アルキルカルバミル、ジ(C1−3アルキル)カルバミル、カルボキシ、C1−3アルキルカルボニル、C1−4アルコキシカルボニル、C1−3アルキルカルボニルアミノ、C1−3アルキルスルホニルアミノ、アミノスルホニル、C1−3アルキルアミノスルホニル、ジ(C1−3アルキル)アミノスルホニル、アミノスルホニルアミノ、C1−3アルキルアミノスルホニルアミノ、ジ(C1−3アルキル)アミノスルホニルアミノ、アミノカルボニルアミノ、C1−3アルキルアミノカルボニルアミノ、およびジ(C1−3アルキル)アミノカルボニルアミノから独立して選択される]
で示される化合物、またはその薬剤的に許容される塩。 -
- R1がメチルである、請求項1または2に記載の化合物、またはその薬剤的に許容される塩。
- R2がC1−6アルキル、C1−3アルコキシ、またはフェニルであり;ここで前記フェニルが、ハロから独立して選択される1個、2個、3個または4個の置換基で置換されていてもよい、請求項1〜3のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- R4がハロ、CN、またはC1−4アルキルである、請求項1〜4のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- R5がハロまたはCNである、請求項1〜5のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- R6がHである、請求項1〜6のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- R7がHである、請求項1〜7のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- R8がH、ハロ、CN、C1−6アルキル、またはCy2であり;ここでCy2が、それぞれが1個または2個の独立して選択されるR11基により置換されていてもよい、C3−6シクロアルキル、フェニル、5〜6員ヘテロアリール、および4〜7員ヘテロシクロアルキルから選択される、請求項1〜8のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- R8がH、ハロ、CN、C1−6アルキル、またはCy2であり;ここでCy2が、それぞれがOH、CN、ハロ、C1−3アルキル、C1−3ハロアルキル、HO−C1−3アルキル、C1−3アルコキシ−C1−3アルキル、C1−3アルコキシ、C1−3ハロアルコキシ、アミノ、C1−3アルキルアミノ、ジ(C1−3アルキル)アミノ、カルバミル、C1−3アルキルカルバミル、およびジ(C1−3アルキル)カルバミルから選択される1個のR11で置換されていてもよい、C3−6シクロアルキル、フェニル、5〜6員ヘテロアリール、または4〜7員ヘテロシクロアルキルから選択される、請求項1〜8のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- R8がH、ハロ、CN、メチル、またはCy2であり;ここでCy2が、それぞれがOH、CN、フルオロ、メチル、2−ヒドロキシエチル、ジメチルカルバミル、アミノ、メチルカルバミル、およびジメチルカルバミルから選択される1個のR11で置換されていてもよい、シクロプロピル、フェニル、ピラゾール環、ピリジン環、またはピリミジン環から選択される、請求項1〜8のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- R8aがH、ハロ、−CN、C1−6アルキル、C2−6アルケニル、C2−6アルキニル、C1−6ハロアルキル、またはCy2である、請求項1〜8のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- R8aがHまたはハロである、請求項1〜8のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- R9がHである、請求項1〜13のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- R10がHである、請求項1〜14のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- 各R11が独立して、OH、CN、ハロ、C1−3アルキル、C1−3ハロアルキル、HO−C1−3アルキル、C1−3アルコキシ−C1−3アルキル、C1−3アルコキシ、C1−3ハロアルコキシ、アミノ、C1−3アルキルアミノ、ジ(C1−3アルキル)アミノ、カルバミル、C1−3アルキルカルバミル、またはジ(C1−3アルキル)カルバミルである、請求項1〜15のいずれか1項に記載の化合物、またはその薬剤的に許容される塩。
- 化合物が、下記式:
- 2−(4−(3−(1−(4−アミノ−3−メチル−1H−ピラゾロ[3,4−d]ピリミジン−1−イル)エチル)−5−クロロ−2−メトキシ−6−メチルフェニル)−1H−ピラゾール−1−イル)エタノール;
1−(1−(5−クロロ−2−メトキシ−4−メチル−3−(1−(1−メチルピペリジン−4−イル)−1H−ピラゾール−4−イル)フェニル)エチル)−3−メチル−1H−ピラゾロ[3,4−d]ピリミジン−4−アミン;
1−(1−{3−[1−(1−アセチルピペリジン−4−イル)−1H−ピラゾール−4−イル]−5−クロロ−2−メトキシ−4−メチルフェニル}エチル)−3−メチル−1H−ピラゾロ[3,4−d]ピリミジン−4−アミン;
1−[1−(5−クロロ−3−{1−[2−(ジメチルアミノ)エチル]−1H−ピラゾール−4−イル}−2−メトキシ−4−メチルフェニル)エチル]−3−メチル−1H−ピラゾロ[3,4−d]ピリミジン−4−アミン;
2−(4−(3−(1−(4−アミノ−3−メチル−1H−ピラゾロ[3,4−d]ピリミジン−1−イル)エチル)−5−クロロ−2−エトキシ−6−メチルフェニル)−1H−ピラゾール−1−イル)アセトアミド;
5−[1−(4−アミノ−3−メチル−1H−ピラゾロ[3,4−d]ピリミジン−1−イル)エチル]−4−メトキシ−2−メチル−3−(1−メチル−1H−ピラゾール−4−イル)ベンゾニトリル;
5−[1−(4−アミノ−3−メチル−1H−ピラゾロ[3,4−d]ピリミジン−1−イル)エチル]−4−エトキシ−2−メチル−3−(1−メチル−1H−ピラゾール−4−イル)ベンゾニトリル;
2−(4−(3−(1−(4−アミノ−3−メチル−1H−ピラゾロ[3,4−d]ピリミジン−1−イル)エチル)−5−クロロ−2−エトキシ−6−メチルフェニル)−1H−ピラゾール−1−イル)−N−メチルアセトアミド;
2−(4−(3−(1−(4−アミノ−3−メチル−1H−ピラゾロ[3,4−d]ピリミジン−1−イル)エチル)−5−クロロ−2−エトキシ−6−メチルフェニル)−1H−ピラゾール−1−イル)−N,N−ジメチルアセトアミド;および
2−(4−(3−(1−(4−アミノ−3−メチル−1H−ピラゾロ[3,4−d]ピリミジン−1−イル)エチル)−5−クロロ−2−メトキシ−6−メチルフェニル)−1H−ピラゾール−1−イル)−N,N−ジメチルアセトアミド;
から選択される、請求項1に記載の化合物、または前述のもののいずれかの薬剤的に許容される塩。 - 請求項1〜18のいずれか1項に記載の化合物またはその薬剤的に許容される塩、および少なくとも1つの薬剤的に許容される担体を含む、医薬組成物。
- PI3Kキナーゼの活性の阻害に用いるための医薬組成物であって、請求項1〜18のいずれか1項に記載の化合物またはその薬剤的に許容される塩、および薬剤的に許容される担体を含む、医薬組成物。
- 前記PI3Kが、PI3Kα、PI3Kβ、PI3Kδ、およびPI3Kγから成る群から選択される、請求項20に記載の医薬組成物。
- 前記PI3Kが変異を含む、請求項20に記載の医薬組成物。
- 前記化合物が、PI3Kα、PI3Kβ、およびPI3Kγのうちの1つまたは複数よりも、PI3Kδに対する選択的阻害剤である、請求項20〜22のいずれか1項に記載の医薬組成物。
- 患者の疾患の治療に用いるための医薬組成物であって、請求項1〜18のいずれか1項に記載の化合物またはその薬剤的に許容される塩、および薬剤的に許容される担体を含む、医薬組成物。
- 前記疾患が、変形性関節症、再狭窄、アテローム性動脈硬化症、骨障害、関節炎、糖尿病性網膜症、乾癬、良性前立腺肥大、炎症、血管新生、膵炎、腎疾患、炎症性腸疾患、重症筋無力症、多発性硬化症、またはシェーグレン症候群である、請求項24に記載の医薬組成物。
- 前記化合物のうちの2つ以上が投与されるように用いられる、請求項24または25に記載の医薬組成物。
- 前記化合物がPI3Kキナーゼ以外のキナーゼを阻害するキナーゼ阻害剤と組み合わせて投与されるように用いられる、請求項25に記載の医薬組成物。
- 患者の免疫に基づく疾患の治療に用いるための医薬組成物であって、請求項1〜18のいずれか1項に記載の化合物またはその薬剤的に許容される塩、および薬剤的に許容される担体を含む、医薬組成物。
- 前記免疫に基づく疾患が、関節リウマチ、アレルギー、喘息、糸球体腎炎、ループス、または前述のもののいずれかに関連する炎症である、請求項28に記載の医薬組成物。
- 患者の癌の治療に用いるための医薬組成物であって、請求項1〜18のいずれか1項に記載の化合物またはその薬剤的に許容される塩、および薬剤的に許容される担体を含む、医薬組成物。
- 前記がんが、乳がん、前立腺がん、結腸がん、子宮内膜がん、脳がん、膀胱がん、皮膚がん、子宮がん、卵巣がん、肺がん、膵臓がん、腎臓がん、胃がん、または血液がんである、請求項30に記載の医薬組成物。
- 前記血液がんが、急性骨髄芽球性白血病、慢性骨髄性白血病、またはB細胞リンパ腫である、請求項31に記載の医薬組成物。
- 前記がんが、びまん性大細胞型B細胞リンパ腫である、請求項30に記載の医薬組成物。
- 患者の肺疾患の治療に用いるための医薬組成物であって、請求項1〜18のいずれか1項に記載の化合物またはその薬剤的に許容される塩、および薬剤的に許容される担体を含む、医薬組成物。
- 前記肺疾患が、急性肺傷害(ALI)または成人呼吸窮迫症候群(ARDS)である、請求項34に記載の医薬組成物。
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