JP2015529248A5 - - Google Patents
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- Publication number
- JP2015529248A5 JP2015529248A5 JP2015533126A JP2015533126A JP2015529248A5 JP 2015529248 A5 JP2015529248 A5 JP 2015529248A5 JP 2015533126 A JP2015533126 A JP 2015533126A JP 2015533126 A JP2015533126 A JP 2015533126A JP 2015529248 A5 JP2015529248 A5 JP 2015529248A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- membered
- cycloalkyl
- optionally substituted
- cancer
- 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
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 87
- 125000000623 heterocyclic group Chemical group 0.000 claims description 50
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 33
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 26
- 150000001875 compounds Chemical class 0.000 claims description 22
- 125000005843 halogen group Chemical group 0.000 claims description 22
- 125000003282 alkyl amino group Chemical group 0.000 claims description 18
- 150000003839 salts Chemical class 0.000 claims description 17
- 125000001424 substituent group Chemical group 0.000 claims description 17
- 125000003545 alkoxy group Chemical group 0.000 claims description 16
- 125000004429 atom Chemical group 0.000 claims description 16
- -1 hydroxy, methoxy, oxo, amino, methylamino Chemical group 0.000 claims description 15
- 229910052760 oxygen Inorganic materials 0.000 claims description 14
- 229910052717 sulfur Inorganic materials 0.000 claims description 13
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 11
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 125000005842 heteroatom Chemical group 0.000 claims description 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 10
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 9
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 9
- 125000004442 acylamino group Chemical group 0.000 claims description 9
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims description 8
- 125000003342 alkenyl group Chemical group 0.000 claims description 8
- 125000000304 alkynyl group Chemical group 0.000 claims description 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims description 6
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims description 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 4
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims description 3
- 125000001188 haloalkyl group Chemical group 0.000 claims description 3
- 125000003107 substituted aryl group Chemical group 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
- 206010001233 Adenoma benign Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 230000003325 follicular Effects 0.000 claims 1
- 210000004907 gland Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 230000000527 lymphocytic effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 238000007363 ring formation reaction Methods 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 208000037964 urogenital cancer Diseases 0.000 claims 1
- 108091054455 MAP kinase family Proteins 0.000 description 3
- 102000043136 MAP kinase family Human genes 0.000 description 3
- 108040008097 MAP kinase activity proteins Proteins 0.000 description 2
- 102000019149 MAP kinase activity proteins Human genes 0.000 description 2
- 102100024193 Mitogen-activated protein kinase 1 Human genes 0.000 description 2
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- 239000012636 effector Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 230000037361 pathway Effects 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- 101000876610 Dictyostelium discoideum Extracellular signal-regulated kinase 2 Proteins 0.000 description 1
- 108010007457 Extracellular Signal-Regulated MAP Kinases Proteins 0.000 description 1
- 101001052493 Homo sapiens Mitogen-activated protein kinase 1 Proteins 0.000 description 1
- 101000944909 Homo sapiens Ribosomal protein S6 kinase alpha-1 Proteins 0.000 description 1
- 101000944921 Homo sapiens Ribosomal protein S6 kinase alpha-2 Proteins 0.000 description 1
- 101000945090 Homo sapiens Ribosomal protein S6 kinase alpha-3 Proteins 0.000 description 1
- 108010034782 Ribosomal Protein S6 Kinases Proteins 0.000 description 1
- 102000009738 Ribosomal Protein S6 Kinases Human genes 0.000 description 1
- 102100033536 Ribosomal protein S6 kinase alpha-1 Human genes 0.000 description 1
- 102100033534 Ribosomal protein S6 kinase alpha-2 Human genes 0.000 description 1
- 102100033643 Ribosomal protein S6 kinase alpha-3 Human genes 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 230000009977 dual effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 description 1
- 210000003705 ribosome Anatomy 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261702981P | 2012-09-19 | 2012-09-19 | |
| US61/702,981 | 2012-09-19 | ||
| PCT/US2013/060032 WO2014047020A1 (en) | 2012-09-19 | 2013-09-17 | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015529248A JP2015529248A (ja) | 2015-10-05 |
| JP2015529248A5 true JP2015529248A5 (https=) | 2017-08-17 |
| JP6186440B2 JP6186440B2 (ja) | 2017-08-23 |
Family
ID=49274870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015533126A Active JP6186440B2 (ja) | 2012-09-19 | 2013-09-17 | キナーゼ阻害剤としてのジヒドロピロリジノピリミジン |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9546173B2 (https=) |
| EP (1) | EP2897961B1 (https=) |
| JP (1) | JP6186440B2 (https=) |
| KR (1) | KR20150056550A (https=) |
| CN (1) | CN104640865B (https=) |
| AU (1) | AU2013318283A1 (https=) |
| BR (1) | BR112015005982A2 (https=) |
| CA (1) | CA2882410A1 (https=) |
| EA (1) | EA201590600A1 (https=) |
| ES (1) | ES2612885T3 (https=) |
| IN (1) | IN2015DN01328A (https=) |
| MX (1) | MX2015003535A (https=) |
| WO (1) | WO2014047020A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2013318283A1 (en) * | 2012-09-19 | 2015-03-05 | Novartis Ag | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
| EP3820567A1 (en) * | 2018-07-12 | 2021-05-19 | UCB Biopharma SRL | Spirocyclic indane analogues as il-17 modulators |
| WO2020243457A1 (en) * | 2019-05-29 | 2020-12-03 | Viogen Biosciences, Llc | Compounds and therapeutic uses thereof |
| AU2020319888A1 (en) * | 2019-08-01 | 2022-02-24 | Praetego, Inc. | Inhibitors of advanced glycation end products |
| AU2020403082A1 (en) * | 2019-12-10 | 2022-05-12 | F. Hoffmann-La Roche Ag | New BRAF inhibitors as paradox breakers |
| PH12022551119A1 (en) | 2019-12-10 | 2023-08-23 | Hoffmann La Roche | New methylquinazolinone derivatives |
| CN115443274B (zh) * | 2020-04-30 | 2025-04-25 | 勤浩医药（苏州）有限公司 | 含苯基并内磺酰胺的化合物 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7208498B2 (en) * | 2002-07-15 | 2007-04-24 | Merck & Co., Inc. | Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes |
| JP2007524596A (ja) | 2003-02-28 | 2007-08-30 | トランスフォーム・ファーマシューティカルズ・インコーポレイテッド | 共結晶医薬組成物 |
| CA2547080A1 (en) * | 2003-12-02 | 2005-07-28 | Vertex Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors and uses thereof |
| PE20060426A1 (es) | 2004-06-02 | 2006-06-28 | Schering Corp | DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa |
| AU2005323797B2 (en) | 2005-01-10 | 2009-07-09 | Pfizer Inc. | Pyrrolopyrazoles, potent kinase inhibitors |
| KR101417136B1 (ko) | 2005-12-13 | 2014-08-07 | 머크 샤프 앤드 돔 코포레이션 | Ｅｒｋ 억제제인 폴리사이클릭 인다졸 유도체 및 이를 포함하는 약제학적 조성물 |
| MY148609A (en) | 2007-06-05 | 2013-05-15 | Merck Sharp & Dohme | Polycyclic indazole derivatives and their use as erk inhibitors for the treatment of cancer |
| EP2613782B1 (en) | 2010-09-01 | 2016-11-02 | Merck Sharp & Dohme Corp. | Indazole derivatives useful as erk inhibitors |
| US9242981B2 (en) * | 2010-09-16 | 2016-01-26 | Merck Sharp & Dohme Corp. | Fused pyrazole derivatives as novel ERK inhibitors |
| WO2012065935A1 (en) | 2010-11-17 | 2012-05-24 | F. Hoffmann-La Roche Ag | Methods of treating tumors |
| EP2681215B1 (en) * | 2011-02-28 | 2015-04-22 | Array Biopharma, Inc. | Serine/threonine kinase inhibitors |
| JP2015508785A (ja) | 2012-03-02 | 2015-03-23 | ジェネンテック， インコーポレイテッド | ピリジニル及びピリミジニルスルホキシド及びスルホン誘導体 |
| AU2013318283A1 (en) * | 2012-09-19 | 2015-03-05 | Novartis Ag | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
-
2013
- 2013-09-17 AU AU2013318283A patent/AU2013318283A1/en not_active Abandoned
- 2013-09-17 EP EP13771007.5A patent/EP2897961B1/en active Active
- 2013-09-17 BR BR112015005982A patent/BR112015005982A2/pt not_active IP Right Cessation
- 2013-09-17 MX MX2015003535A patent/MX2015003535A/es unknown
- 2013-09-17 KR KR1020157006602A patent/KR20150056550A/ko not_active Withdrawn
- 2013-09-17 CN CN201380048493.XA patent/CN104640865B/zh active Active
- 2013-09-17 ES ES13771007.5T patent/ES2612885T3/es active Active
- 2013-09-17 US US14/428,546 patent/US9546173B2/en active Active
- 2013-09-17 EA EA201590600A patent/EA201590600A1/ru unknown
- 2013-09-17 JP JP2015533126A patent/JP6186440B2/ja active Active
- 2013-09-17 IN IN1328DEN2015 patent/IN2015DN01328A/en unknown
- 2013-09-17 CA CA2882410A patent/CA2882410A1/en not_active Abandoned
- 2013-09-17 WO PCT/US2013/060032 patent/WO2014047020A1/en not_active Ceased
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