JP2012500785A5 - - Google Patents
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- Publication number
- JP2012500785A5 JP2012500785A5 JP2011523425A JP2011523425A JP2012500785A5 JP 2012500785 A5 JP2012500785 A5 JP 2012500785A5 JP 2011523425 A JP2011523425 A JP 2011523425A JP 2011523425 A JP2011523425 A JP 2011523425A JP 2012500785 A5 JP2012500785 A5 JP 2012500785A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- cyclopentyl
- ylamino
- pyrrolo
- pyrimidine
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- RHXHGRAEPCAFML-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[(5-piperazin-1-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCNCC1 RHXHGRAEPCAFML-UHFFFAOYSA-N 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims 37
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 15
- 201000011510 cancer Diseases 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 13
- 239000011780 sodium chloride Substances 0.000 claims 13
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 206010006187 Breast cancer Diseases 0.000 claims 8
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims 6
- 201000005787 hematologic cancer Diseases 0.000 claims 6
- 201000002528 pancreatic cancer Diseases 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 150000001408 amides Chemical class 0.000 claims 5
- 206010009944 Colon cancer Diseases 0.000 claims 4
- 206010018338 Glioma Diseases 0.000 claims 4
- 206010024324 Leukaemias Diseases 0.000 claims 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 4
- 206010025650 Malignant melanoma Diseases 0.000 claims 4
- 206010061311 Nervous system neoplasm Diseases 0.000 claims 4
- 208000002154 Non-Small-Cell Lung Carcinoma Diseases 0.000 claims 4
- 108009000071 Non-small cell lung cancer Proteins 0.000 claims 4
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 4
- 206010033128 Ovarian cancer Diseases 0.000 claims 4
- 206010060862 Prostate cancer Diseases 0.000 claims 4
- 201000004101 esophageal cancer Diseases 0.000 claims 4
- 201000005202 lung cancer Diseases 0.000 claims 4
- 201000001441 melanoma Diseases 0.000 claims 4
- 210000004027 cells Anatomy 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims 2
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims 2
- 206010003571 Astrocytoma Diseases 0.000 claims 2
- 208000003950 B-Cell Lymphoma Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 208000009899 Burkitt Lymphoma Diseases 0.000 claims 2
- 125000005915 C6-C14 aryl group Chemical group 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 206010008958 Chronic lymphocytic leukaemia Diseases 0.000 claims 2
- 208000002416 Cutaneous Malignant Melanoma Diseases 0.000 claims 2
- 210000002615 Epidermis Anatomy 0.000 claims 2
- 208000007276 Esophageal Squamous Cell Carcinoma Diseases 0.000 claims 2
- 208000004463 Follicular Adenocarcinoma Diseases 0.000 claims 2
- 206010017758 Gastric cancer Diseases 0.000 claims 2
- 206010020243 Hodgkin's disease Diseases 0.000 claims 2
- 201000006743 Hodgkin's lymphoma Diseases 0.000 claims 2
- 208000007766 Kaposi Sarcoma Diseases 0.000 claims 2
- 208000000429 Leukemia, Lymphocytic, Chronic, B-Cell Diseases 0.000 claims 2
- 210000004324 Lymphatic System Anatomy 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010026798 Mantle cell lymphomas Diseases 0.000 claims 2
- 208000007538 Neurilemmoma Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 206010029592 Non-Hodgkin's lymphomas Diseases 0.000 claims 2
- 206010061534 Oesophageal squamous cell carcinoma Diseases 0.000 claims 2
- 206010025310 Other lymphomas Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 206010039667 Schwannoma Diseases 0.000 claims 2
- 208000000587 Small Cell Lung Carcinoma Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims 2
- 206010043276 Teratoma Diseases 0.000 claims 2
- 201000005510 acute lymphocytic leukemia Diseases 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 201000011231 colorectal cancer Diseases 0.000 claims 2
- 125000004966 cyanoalkyl group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 229940079593 drugs Drugs 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 201000000497 familial melanoma Diseases 0.000 claims 2
- 201000005160 follicular thyroid carcinoma Diseases 0.000 claims 2
- 201000010175 gallbladder cancer Diseases 0.000 claims 2
- 201000010915 glioblastoma multiforme Diseases 0.000 claims 2
- 210000002768 hair cell Anatomy 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 201000008806 mesenchymal cell neoplasm Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 201000009251 multiple myeloma Diseases 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 201000010208 seminoma Diseases 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 201000006083 xeroderma pigmentosum Diseases 0.000 claims 2
- -1 2,3-dihydroxypropyl Chemical group 0.000 claims 1
- PKNZXGSXXRQHQY-UHFFFAOYSA-N 2-[4-[6-[[7-cyclopentyl-6-(dimethylcarbamoyl)pyrrolo[2,3-d]pyrimidin-2-yl]amino]pyridin-3-yl]piperazin-1-yl]acetic acid Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCN(CC(O)=O)CC1 PKNZXGSXXRQHQY-UHFFFAOYSA-N 0.000 claims 1
- ZBRMBWWZBMELPR-UHFFFAOYSA-N 2-[4-[6-[[7-cyclopentyl-6-(dimethylcarbamoyl)pyrrolo[2,3-d]pyrimidin-2-yl]amino]pyridin-3-yl]piperazin-1-yl]propanoic acid Chemical compound C1CN(C(C)C(O)=O)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 ZBRMBWWZBMELPR-UHFFFAOYSA-N 0.000 claims 1
- PDMWDVSSTBDYJL-UHFFFAOYSA-N 2-[[5-(3-aminopyrrolidin-1-yl)pyridin-2-yl]amino]-7-cyclopentyl-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCC(N)C1 PDMWDVSSTBDYJL-UHFFFAOYSA-N 0.000 claims 1
- UFZLZSPDJSRERW-UHFFFAOYSA-N 2-[[5-[4-(2-amino-2-oxoethyl)piperazin-1-yl]pyridin-2-yl]amino]-7-cyclopentyl-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCN(CC(N)=O)CC1 UFZLZSPDJSRERW-UHFFFAOYSA-N 0.000 claims 1
- UOCBBZYWTNUHBC-UHFFFAOYSA-N 2-[[5-[4-(2-aminoacetyl)piperazin-1-yl]pyridin-2-yl]amino]-7-cyclopentyl-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCN(C(=O)CN)CC1 UOCBBZYWTNUHBC-UHFFFAOYSA-N 0.000 claims 1
- UERYQFAYBUYBDW-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(3,3-dimethylpiperazin-1-yl)pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCNC(C)(C)C1 UERYQFAYBUYBDW-UHFFFAOYSA-N 0.000 claims 1
- OLHGFHRURCFMRB-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(3,8-diazabicyclo[3.2.1]octan-3-ylmethyl)pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(CN4CC5CCC(N5)C4)=CC=3)N=C2N1C1CCCC1 OLHGFHRURCFMRB-UHFFFAOYSA-N 0.000 claims 1
- ACJGJMCIFMQOSA-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(4-cyclopentylpiperazin-1-yl)pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N(CC1)CCN1C1CCCC1 ACJGJMCIFMQOSA-UHFFFAOYSA-N 0.000 claims 1
- NGOLAYUXEIFEMV-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(4-ethylpiperazin-1-yl)pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(CC)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 NGOLAYUXEIFEMV-UHFFFAOYSA-N 0.000 claims 1
- CKXSVXWMVJCCSR-GOSISDBHSA-N 7-cyclopentyl-2-[[5-[(3R)-4-(2-hydroxyethyl)-3-methylpiperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(CCO)[C@H](C)CN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 CKXSVXWMVJCCSR-GOSISDBHSA-N 0.000 claims 1
- CKXSVXWMVJCCSR-SFHVURJKSA-N 7-cyclopentyl-2-[[5-[(3S)-4-(2-hydroxyethyl)-3-methylpiperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(CCO)[C@@H](C)CN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 CKXSVXWMVJCCSR-SFHVURJKSA-N 0.000 claims 1
- QGMQUAZBMWEJAS-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[1-(2-hydroxyethyl)piperidin-4-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1C1CCN(CCO)CC1 QGMQUAZBMWEJAS-UHFFFAOYSA-N 0.000 claims 1
- WAQVNITUBIANSO-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[4-(1-hydroxypropan-2-yl)piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(C(CO)C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 WAQVNITUBIANSO-UHFFFAOYSA-N 0.000 claims 1
- CLIQXKGGFSZHEF-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[4-(2-fluoroethyl)piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCN(CCF)CC1 CLIQXKGGFSZHEF-UHFFFAOYSA-N 0.000 claims 1
- MELBWWJCOAUKFK-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[4-(2-hydroxy-2-methylpropyl)piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCN(CC(C)(C)O)CC1 MELBWWJCOAUKFK-UHFFFAOYSA-N 0.000 claims 1
- BCCZLUXDWZUOBK-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[4-(2-hydroxyethyl)piperazin-1-yl]pyrazin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CN=C1N1CCN(CCO)CC1 BCCZLUXDWZUOBK-UHFFFAOYSA-N 0.000 claims 1
- NAXBGVSFGBQHDO-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[4-(2-hydroxyethyl)piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCN(CCO)CC1 NAXBGVSFGBQHDO-UHFFFAOYSA-N 0.000 claims 1
- OPHHLWCBNAKAGG-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[4-(2-methoxyethyl)piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(CCOC)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 OPHHLWCBNAKAGG-UHFFFAOYSA-N 0.000 claims 1
- BKIYMWJZWFUKEM-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[4-(3-cyclopentylpropanoyl)piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N(CC1)CCN1C(=O)CCC1CCCC1 BKIYMWJZWFUKEM-UHFFFAOYSA-N 0.000 claims 1
- SGBLGMZZKLPXCW-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[4-(dimethylamino)piperidin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CC(N(C)C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 SGBLGMZZKLPXCW-UHFFFAOYSA-N 0.000 claims 1
- WPTNHXKUYYITBY-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[4-(dimethylamino)piperidine-1-carbonyl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CC(N(C)C)CCN1C(=O)C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 WPTNHXKUYYITBY-UHFFFAOYSA-N 0.000 claims 1
- WCCRZTMTXBWQTH-OAQYLSRUSA-N 7-cyclopentyl-2-[[5-[4-[(2R)-2,3-dihydroxypropyl]piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCN(C[C@@H](O)CO)CC1 WCCRZTMTXBWQTH-OAQYLSRUSA-N 0.000 claims 1
- MLGDDYSNCUJCIK-GOSISDBHSA-N 7-cyclopentyl-2-[[5-[4-[(2R)-2-hydroxypropyl]piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(C[C@H](O)C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 MLGDDYSNCUJCIK-GOSISDBHSA-N 0.000 claims 1
- WCCRZTMTXBWQTH-NRFANRHFSA-N 7-cyclopentyl-2-[[5-[4-[(2S)-2,3-dihydroxypropyl]piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCN(C[C@H](O)CO)CC1 WCCRZTMTXBWQTH-NRFANRHFSA-N 0.000 claims 1
- MLGDDYSNCUJCIK-SFHVURJKSA-N 7-cyclopentyl-2-[[5-[4-[(2S)-2-hydroxypropyl]piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(C[C@@H](O)C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 MLGDDYSNCUJCIK-SFHVURJKSA-N 0.000 claims 1
- JPDFBVOEACJMHS-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N1CCN(CCOCCO)CC1 JPDFBVOEACJMHS-UHFFFAOYSA-N 0.000 claims 1
- GIHYRSIEPFPUKX-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-[4-[2-(dimethylamino)acetyl]piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(C(=O)CN(C)C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 GIHYRSIEPFPUKX-UHFFFAOYSA-N 0.000 claims 1
- YKWPDJQXUDYJND-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[(5-piperidin-4-ylpyridin-2-yl)amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1C1CCNCC1 YKWPDJQXUDYJND-UHFFFAOYSA-N 0.000 claims 1
- IQUDLJFGRYAYDQ-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-(1-propan-2-ylpiperidin-4-yl)pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(C(C)C)CCC1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 IQUDLJFGRYAYDQ-UHFFFAOYSA-N 0.000 claims 1
- IMQBGJIBVDHUCE-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-(3-methylpiperazin-1-yl)pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CNC(C)CN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 IMQBGJIBVDHUCE-UHFFFAOYSA-N 0.000 claims 1
- XVVBHKGQHJECBA-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-(4-propan-2-ylpiperazin-1-yl)pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(C(C)C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 XVVBHKGQHJECBA-UHFFFAOYSA-N 0.000 claims 1
- BKQDDJOUNQSRRA-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-(4-propan-2-ylpiperazine-1-carbonyl)pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(C(C)C)CCN1C(=O)C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 BKQDDJOUNQSRRA-UHFFFAOYSA-N 0.000 claims 1
- IXLOPBXFESKDHV-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-(piperazine-1-carbonyl)pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1C(=O)N1CCNCC1 IXLOPBXFESKDHV-UHFFFAOYSA-N 0.000 claims 1
- IMQBGJIBVDHUCE-MRXNPFEDSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-[(3R)-3-methylpiperazin-1-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN[C@H](C)CN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 IMQBGJIBVDHUCE-MRXNPFEDSA-N 0.000 claims 1
- IMQBGJIBVDHUCE-INIZCTEOSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-[(3S)-3-methylpiperazin-1-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN[C@@H](C)CN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 IMQBGJIBVDHUCE-INIZCTEOSA-N 0.000 claims 1
- SRKLUGHVHDHQGA-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-[4-(2-methylpropyl)piperazin-1-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(CC(C)C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 SRKLUGHVHDHQGA-UHFFFAOYSA-N 0.000 claims 1
- CTFLYIFHIVSZQN-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-[4-(2-propan-2-yloxyethyl)piperazin-1-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(CCOC(C)C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 CTFLYIFHIVSZQN-UHFFFAOYSA-N 0.000 claims 1
- BJCUXTCYGYAAED-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-[4-(4-methylpentyl)piperazin-1-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN(CCCC(C)C)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 BJCUXTCYGYAAED-UHFFFAOYSA-N 0.000 claims 1
- JXPGGWJYNZMXNB-UHFFFAOYSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-[4-(pyrrolidine-1-carbonyl)piperazin-1-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1N(CC1)CCN1C(=O)N1CCCC1 JXPGGWJYNZMXNB-UHFFFAOYSA-N 0.000 claims 1
- BPEQUIQBCWEGBU-KRWDZBQOSA-N 7-cyclopentyl-N,N-dimethyl-2-[[5-[[(3S)-3-methylpiperazin-1-yl]methyl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C1CN[C@@H](C)CN1CC(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 BPEQUIQBCWEGBU-KRWDZBQOSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010034800 Phaeochromocytoma Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 238000004132 cross linking Methods 0.000 claims 1
- QKIUAMUSENSFQQ-UHFFFAOYSA-N dimethylazanide Chemical compound C[N-]C QKIUAMUSENSFQQ-UHFFFAOYSA-N 0.000 claims 1
- ASDWVTGHLAHFKI-UHFFFAOYSA-N ethyl 2-[4-[6-[[7-cyclopentyl-6-(dimethylcarbamoyl)pyrrolo[2,3-d]pyrimidin-2-yl]amino]pyridin-3-yl]piperazin-1-yl]acetate Chemical compound C1CN(CC(=O)OCC)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 ASDWVTGHLAHFKI-UHFFFAOYSA-N 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- MIGQOVZXJXABMW-UHFFFAOYSA-N methyl 2-[4-[6-[[7-cyclopentyl-6-(dimethylcarbamoyl)pyrrolo[2,3-d]pyrimidin-2-yl]amino]pyridin-3-yl]piperazin-1-yl]acetate Chemical compound C1CN(CC(=O)OC)CCN1C(C=N1)=CC=C1NC1=NC=C(C=C(C(=O)N(C)C)N2C3CCCC3)C2=N1 MIGQOVZXJXABMW-UHFFFAOYSA-N 0.000 claims 1
Claims (31)
- 式I:
Xは、CR 9 であり;
R1は、CONR5R 6 であり、R 5 およびR 6 はC 1−8 アルキルであり;
R2は、C 3−14シクロアルキルであり、R2は、1個以上のC1−8アルキルまたはOHで置換されていてもよく;
Lは、結合、C1−8アルキレン、C(O)またはC(O)NHであり、Lは、置換されていても非置換であってもよく;
Yは、H、R11、NR12R13、OHであるか、あるいは、Yは下記の基:
ここで、Yは、CR9またはNであり;
0〜3個のR8が存在でき、そしてR8は、C1−8アルキル、オキソ、ハロゲンであるか、あるいは、2個以上のR8は架橋アルキル基を形成してもよく;
Wは、CR9またはNであり;
R3は、H、C1−8アルキル、C1−8アルキルR14、C3−14シクロアルキル、C(O)C1−8アルキル、C1−8ハロアルキル、C1−8アルキルOH、C(O)NR14R15、C1−8シアノアルキル、C(O)R14、C0−8アルキルC(O)C0−8アルキルNR14R15、C0−8アルキルC(O)OR14、NR14R15、SO2C1−8アルキル、C1−8アルキルC3−14シクロアルキル、C(O)C1−8アルキルC3−14シクロアルキル、C1−8アルコキシまたはOHであり、R3がHではないとき、該基は、置換されていても非置換であってもよく;
R9は、Hまたはハロゲンであり;
R 11、R12、R13、R14およびR15はそれぞれ、H、C1−8アルキル、C3−14シクロアルキル、3〜14員のシクロヘテロアルキル基、C6−14アリール基、5〜14員のヘテロアリール基、アルコキシ、C(O)H、C(N)OH、C(N)OCH3、C(O)C1−3アルキル、C1−8アルキルNH2、C1−6アルキルOHから独立して選択され、かつ、R 11、R12、R13、R14およびR15は、Hではない場合、置換されていても非置換であってもよく;
mおよびnは、独立して、0〜2であり;
ここで、L、R3 、R 11、R12、R13、R14およびR15は、1個以上のC1−8アルキル、C2−8アルケニル、C2−8アルキニル、C3−14シクロアルキル、5〜14員のヘテロアリール基、C6−14アリール基、3〜14員のシクロヘテロアルキル基、OH、(O)、CN、アルコキシ、ハロゲンまたはNH2で置換されていてもよい。]
の化合物またはその薬学的に許容される塩。 - R3が、H、C1−8アルキル、C3−14シクロアルキル、C(O)C1−8アルキル、C1−8アルキルOH、C1−8シアノアルキル、C0−8アルキルC(O)C0−8アルキルNR14R15、C0−8アルキルC(O)OR14、NR14R15、C1−8アルキルC3−14シクロアルキル、C(O)C1−8アルキルC3−14シクロアルキル、C0−8アルコキシ、C1−8アルキルR14、C1−8ハロアルキルまたはC(O)R14であり、これらは、1個以上のOH、CN、FまたはNH2で置換されていてもよく、ここで、R14およびR15がそれぞれ、H、C1−8アルキル、C3−14シクロアルキル、アルコキシ、C(O)C1−3アルキル、C1−8アルキルNH2またはC1−6アルキルOHから独立して選択される、請求項1に記載された式Iの化合物またはその薬学的に許容される塩。
- R3が、H、C1−8アルキルまたはC1−8アルキルOHである、請求項1〜2の何れか1項に記載された式Iの化合物またはその薬学的に許容される塩。
- R 3 が、H、メチル、エチル、プロピル、イソプロピル、CH 2 OHまたはCH 2 CH 2 OHである、請求項3に記載された式Iの化合物またはその薬学的に許容される塩。
- R2がシクロペンチルである、請求項1〜5の何れか1項に記載された式Iの化合物。
- mが2であり、nが1である、請求項5に記載された化合物またはその薬学的に許容される塩。
- R 8 が、メチル、エチル、プロピル、ブチル、またはオキソであるか、あるいは、2個のR 8 が架橋基を形成してもよい、請求項1〜8の何れか1項に記載された化合物またはその薬学的に許容される塩。
- 次に示すものから選択される、請求項1に記載された化合物:
7−シクロペンチル−2−{5−[4−(2−フルオロ−エチル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−(4−ジメチルアミノ−3,4,5,6−テトラヒドロ−2H−[1,3']ビピリジニル−6'−イルアミノ)−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
2−[5−(4−カルバモイルメチル−ピペラジン−1−イル)−ピリジン−2−イルアミノ]−7−シクロペンチル−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
2−{5−[4−(2−アミノ−アセチル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7−シクロペンチル−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
2−[5−(3−アミノ−ピロリジン−1−イル)−ピリジン−2−イルアミノ]−7−シクロペンチル−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(2−メトキシ−エチル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[4−(2−ヒドロキシエチル)−3,4,5,6−テトラヒドロ−2H−[1,2']ビピラジニル−5'−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−((R)−3−メチル−ピペラジン−1−イル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−((S)−3−メチルピペラジン−1−イル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−(3−メチルピペラジン−1−イル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(3−ヒドロキシプロピル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(ピロリジン−1−カルボニル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(2−ヒドロキシ−エチル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−((S)−2,3−ジヒドロキシプロピル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−(5−{4−[2−(2−ヒドロキシエトキシ)−エチル]−ピペラジン−1−イル}−ピリジン−2−イルアミノ)−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(2−ヒドロキシ−1−メチルエチル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(2,3−ジヒドロキシプロピル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−((R)−2,3−ジヒドロキシプロピル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−(ピペラジン−1−カルボニル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−(4−ジメチルアミノピペリジン−1−カルボニル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−(1',2',3',4',5',6'−ヘキサヒドロ−[3,4']ビピリジニル−6−イルアミノ)−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−((S)−3−メチルピペラジン−1−イルメチル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−((S)−2−ヒドロキシプロピル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−((R)−2−ヒドロキシプロピル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−(4−イソプロピル−ピペラジン−1−イル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−(4−イソプロピル−ピペラジン−1−カルボニル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(4−メチル−ペンチル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(2−ヒドロキシ−2−メチルプロピル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−(3,3−ジメチル−ピペラジン−1−イル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−(3,8−ジアザ−ビシクロ[3.2.1]オクタ−3−イルメチル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−(5−ピペラジン−1−イル−ピリジン−2−イルアミノ)−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−(4−エチル−ピペラジン−1−イル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−(4−シクロペンチル−ピペラジン−1−イル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−(1'−イソプロピル−1',2',3',4',5',6'−ヘキサヒドロ−[3,4']ビピリジニル−6−イルアミノ)−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[(R)−4−(2−ヒドロキシエチル)−3−メチル−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[(S)−4−(2−ヒドロキシエチル)−3−メチル−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(2−ヒドロキシエチル)−ピペラジン−1−イルメチル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(2−ジメチルアミノアセチル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(2−エチル−ブチル)ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
2−{5−[4−(2−シクロヘキシル−アセチル)ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7−シクロペンチル−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−{5−[4−(3−シクロペンチル−プロピオニル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[5−(4−イソブチルピペラジン−1−イル)−ピリジン−2−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
{4−[6−(7−シクロペンチル−6−ジメチルカルバモイル−7H−ピロロ[2,3−d]ピリミジン−2−イルアミノ)ピリジン−3−イル]−ピペラジン−1−イル}−酢酸メチルエステル;
7−シクロペンチル−2−{5−[4−(2−イソプロポキシエチル)−ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
{4−[6−(7−シクロペンチル−6−ジメチルカルバモイル−7H−ピロロ[2,3−d]ピリミジン−2−イルアミノ)ピリジン−3−イル]−ピペラジン−1−イル}−酢酸エチルエステル;
7−シクロペンチル−2−{5−[4−(2−メチル−ブチル)ピペラジン−1−イル]−ピリジン−2−イルアミノ}−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
7−シクロペンチル−2−[1'−(2−ヒドロキシ−エチル)−1',2',3',4',5',6'−ヘキサヒドロ−[3,4']ビピリジニル−6−イルアミノ]−7H−ピロロ[2,3−d]ピリミジン−6−カルボン酸 ジメチルアミド;
{4−[6−(7−シクロペンチル−6−ジメチルカルバモイル−7H−ピロロ[2,3−d]ピリミジン−2−イルアミノ)−ピリジン−3−イル]ピペラジン−1−イル}−酢酸;および
2−{4−[6−(7−シクロペンチル−6−ジメチルカルバモイル−7H−ピロロ[2,3−d]ピリミジン−2−イルアミノ)−ピリジン−3−イル]−ピペラジン−1−イル}−プロピオン酸;
またはそれらの薬学的に許容される塩。 - 請求項1〜12の何れか1項に記載された化合物またはその薬学的に許容される塩および薬学的に許容される担体を含む医薬組成物。
- 他の薬物と共に請求項1〜12の何れか1項に記載された化合物またはその薬学的に許容される塩を含む、組み合わせ剤。
- 癌の処置に使用される、請求項14に記載された医薬組成物。
- 癌が、乳癌、膵臓癌、結腸直腸癌、肺癌、肉腫、白血病、神経膠腫、家族性黒色腫および黒色腫からなる群から選択される、請求項16に記載された医薬組成物。
- 癌が、膀胱癌、乳癌、大腸癌、腎臓癌、表皮癌、肝臓癌、肺癌、食道癌、胆嚢癌、卵巣癌、膵臓癌、胃癌、子宮頚癌、甲状腺癌、鼻の癌、頭頚部癌、前立腺癌、または皮膚癌;リンパ系の造血器腫瘍;骨髄系の造血器腫瘍;間葉系由来の腫瘍;中枢または末端神経系の腫瘍;黒色腫;精上皮腫;奇形腫;骨肉腫;色素性乾皮症;角化棘細胞腫;甲状腺濾胞癌;またはカポジ肉腫である、請求項16に記載された医薬組成物。
- リンパ系の造血器腫瘍が、白血病、急性リンパ性白血病、慢性リンパ性白血病、B細胞リンパ腫、T細胞リンパ腫、多発性骨髄腫、ホジキンリンパ腫、非ホジキンリンパ腫、有毛細胞リンパ腫またはバーキットリンパ腫である、請求項18に記載された医薬組成物。
- 癌が、乳癌、卵巣癌、大腸癌、前立腺癌、食道癌、扁平上皮癌、または非小細胞肺癌である、請求項18に記載された医薬組成物。
- 中枢または末端神経系の腫瘍が、星状細胞腫、神経芽腫、神経膠腫、またはシュワン腫である、請求項18に記載された医薬組成物。
- 癌が、小細胞肺癌、非小細胞肺癌、膵臓癌、乳癌、多形神経膠芽腫、T細胞ALL、または、マントル細胞リンパ腫である、請求項16に記載された医薬組成物。
- 請求項13に記載された化合物および薬学的に許容される担体を含む医薬組成物。
- 他の薬物と共に請求項13に記載された化合物を含む、組み合わせ剤。
- 癌の処置に使用される、請求項23に記載された医薬組成物。
- 癌が、乳癌、膵臓癌、結腸直腸癌、肺癌、肉腫、白血病、神経膠腫、家族性黒色腫および黒色腫からなる群から選択される、請求項25に記載された医薬組成物。
- 癌が、膀胱癌、乳癌、大腸癌、腎臓癌、表皮癌、肝臓癌、肺癌、食道癌、胆嚢癌、卵巣癌、膵臓癌、胃癌、子宮頚癌、甲状腺癌、鼻の癌、頭頚部癌、前立腺癌、または皮膚癌;リンパ系の造血器腫瘍;骨髄系の造血器腫瘍;間葉系由来の腫瘍;中枢または末端神経系の腫瘍;黒色腫;精上皮腫;奇形腫;骨肉腫;色素性乾皮症;角化棘細胞腫;甲状腺濾胞癌;またはカポジ肉腫である、請求項25に記載された医薬組成物。
- リンパ系の造血器腫瘍が、白血病、急性リンパ性白血病、慢性リンパ性白血病、B細胞リンパ腫、T細胞リンパ腫、多発性骨髄腫、ホジキンリンパ腫、非ホジキンリンパ腫、有毛細胞リンパ腫またはバーキットリンパ腫である、請求項27に記載された医薬組成物。
- 癌が、乳癌、卵巣癌、大腸癌、前立腺癌、食道癌、扁平上皮癌、または非小細胞肺癌である、請求項25に記載された医薬組成物。
- 中枢または末端神経系の腫瘍が、星状細胞腫、神経芽腫、神経膠腫、またはシュワン腫である、請求項27に記載された医薬組成物。
- 癌が、小細胞肺癌、非小細胞肺癌、膵臓癌、乳癌、多形神経膠芽腫、T細胞ALL、または、マントル細胞リンパ腫である、請求項25に記載された医薬組成物。
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