JP2017503000A5 - - Google Patents
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- JP2017503000A5 JP2017503000A5 JP2016547026A JP2016547026A JP2017503000A5 JP 2017503000 A5 JP2017503000 A5 JP 2017503000A5 JP 2016547026 A JP2016547026 A JP 2016547026A JP 2016547026 A JP2016547026 A JP 2016547026A JP 2017503000 A5 JP2017503000 A5 JP 2017503000A5
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- JP
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- Prior art keywords
- alkyl
- amino
- substituted
- hydrogen
- halo
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims description 50
- 229910052739 hydrogen Inorganic materials 0.000 claims description 34
- 239000001257 hydrogen Substances 0.000 claims description 34
- 125000005843 halogen group Chemical group 0.000 claims description 30
- 125000003545 alkoxy group Chemical group 0.000 claims description 25
- -1 amino, hydroxy Chemical group 0.000 claims description 22
- 150000003839 salts Chemical class 0.000 claims description 22
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 14
- 150000001875 compounds Chemical class 0.000 claims description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 14
- 125000003282 alkyl amino group Chemical group 0.000 claims description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 125000003118 aryl group Chemical group 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 8
- 125000003277 amino group Chemical group 0.000 claims description 6
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 6
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims description 6
- 125000001624 naphthyl group Chemical group 0.000 claims description 6
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims description 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 4
- 206010029260 Neuroblastoma Diseases 0.000 claims description 4
- 102100033019 Tyrosine-protein phosphatase non-receptor type 11 Human genes 0.000 claims description 4
- 101710116241 Tyrosine-protein phosphatase non-receptor type 11 Proteins 0.000 claims description 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 208000005101 LEOPARD Syndrome Diseases 0.000 claims description 2
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010062901 Multiple lentigines syndrome Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims description 2
- 206010029748 Noonan syndrome Diseases 0.000 claims description 2
- 208000010708 Noonan syndrome with multiple lentigines Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 2
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 17
- 150000002431 hydrogen Chemical class 0.000 description 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461928738P | 2014-01-17 | 2014-01-17 | |
| US61/928,738 | 2014-01-17 | ||
| PCT/IB2015/050343 WO2015107493A1 (en) | 2014-01-17 | 2015-01-16 | 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017503000A JP2017503000A (ja) | 2017-01-26 |
| JP2017503000A5 true JP2017503000A5 (OSRAM) | 2018-02-22 |
| JP6523303B2 JP6523303B2 (ja) | 2019-05-29 |
Family
ID=52462361
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016547026A Active JP6523303B2 (ja) | 2014-01-17 | 2015-01-16 | Ｓｈｐ２の活性を阻害するための１−ピリダジン／トリアジン−３−イル−ピペラジン／ピペリジン／ピロリジン誘導体およびその組成物 |
Country Status (6)
| Country | Link |
|---|---|
| US (4) | US10093646B2 (OSRAM) |
| EP (1) | EP3094627B1 (OSRAM) |
| JP (1) | JP6523303B2 (OSRAM) |
| CN (1) | CN105899491B (OSRAM) |
| ES (1) | ES2699351T3 (OSRAM) |
| WO (1) | WO2015107493A1 (OSRAM) |
Families Citing this family (119)
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| US11466017B2 (en) | 2011-03-10 | 2022-10-11 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of PTPN11 |
| WO2015092819A2 (en) | 2013-12-21 | 2015-06-25 | Nektar Therapeutics (India) Pvt. Ltd. | Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5- amine |
| CN105899493B (zh) | 2014-01-17 | 2019-03-29 | 诺华股份有限公司 | 用于抑制shp2活性的1-(三嗪-3-基/哒嗪-3-基)-哌(-嗪)啶衍生物及其组合物 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| CN112625028B (zh) | 2015-06-19 | 2024-10-29 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物 |
| EP3310771B1 (en) * | 2015-06-19 | 2020-07-22 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| EP3310779B1 (en) | 2015-06-19 | 2019-05-08 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| CN108473442B (zh) | 2015-11-05 | 2022-03-25 | 赛尔基因昆蒂赛尔研究公司 | 包含赖氨酸特异性脱甲基酶-1的抑制剂的组合物 |
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-
2015
- 2015-01-16 CN CN201580004216.8A patent/CN105899491B/zh active Active
- 2015-01-16 US US15/110,498 patent/US10093646B2/en active Active
- 2015-01-16 EP EP15703105.5A patent/EP3094627B1/en active Active
- 2015-01-16 ES ES15703105T patent/ES2699351T3/es active Active
- 2015-01-16 JP JP2016547026A patent/JP6523303B2/ja active Active
- 2015-01-16 WO PCT/IB2015/050343 patent/WO2015107493A1/en not_active Ceased
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2018
- 2018-08-30 US US16/117,674 patent/US10774065B2/en active Active
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2020
- 2020-08-06 US US16/987,322 patent/US11401259B2/en active Active
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2022
- 2022-06-24 US US17/808,895 patent/US20220348553A1/en not_active Abandoned
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