JP2015511621A5 - - Google Patents
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- Publication number
- JP2015511621A5 JP2015511621A5 JP2015502373A JP2015502373A JP2015511621A5 JP 2015511621 A5 JP2015511621 A5 JP 2015511621A5 JP 2015502373 A JP2015502373 A JP 2015502373A JP 2015502373 A JP2015502373 A JP 2015502373A JP 2015511621 A5 JP2015511621 A5 JP 2015511621A5
- Authority
- JP
- Japan
- Prior art keywords
- phenylamino
- dimethoxy
- dichloro
- urea
- phenyl
- 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
- -1 2,6-dichloro-3,5-dimethoxy-phenyl Chemical group 0.000 claims 13
- 239000012453 solvate Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 7
- 150000001204 N-oxides Chemical class 0.000 claims 6
- 229930003316 Vitamin D Natural products 0.000 claims 6
- QYSXJUFSXHHAJI-XFEUOLMDSA-N Vitamin D3 Natural products C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C/C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-XFEUOLMDSA-N 0.000 claims 6
- 235000019166 vitamin D Nutrition 0.000 claims 6
- 239000011710 vitamin D Substances 0.000 claims 6
- 150000003710 vitamin D derivatives Chemical class 0.000 claims 6
- 229940046008 vitamin d Drugs 0.000 claims 6
- 208000005050 Familial Hypophosphatemic Rickets Diseases 0.000 claims 4
- 208000031878 X-linked hypophosphatemia Diseases 0.000 claims 4
- 208000035724 X-linked hypophosphatemic rickets Diseases 0.000 claims 4
- 201000003674 autosomal dominant hypophosphatemic rickets Diseases 0.000 claims 4
- 201000003672 autosomal recessive hypophosphatemic rickets Diseases 0.000 claims 4
- 210000000988 bone and bone Anatomy 0.000 claims 4
- WGCYRFWNGRMRJA-UHFFFAOYSA-N 1-ethylpiperazine Chemical compound CCN1CCNCC1 WGCYRFWNGRMRJA-UHFFFAOYSA-N 0.000 claims 2
- 208000028060 Albright disease Diseases 0.000 claims 2
- 208000031213 Epidermal nevus syndrome Diseases 0.000 claims 2
- 102100024802 Fibroblast growth factor 23 Human genes 0.000 claims 2
- 101001051973 Homo sapiens Fibroblast growth factor 23 Proteins 0.000 claims 2
- 208000029663 Hypophosphatemia Diseases 0.000 claims 2
- 201000001853 McCune-Albright syndrome Diseases 0.000 claims 2
- 102000004264 Osteopontin Human genes 0.000 claims 2
- 108010081689 Osteopontin Proteins 0.000 claims 2
- 102100036893 Parathyroid hormone Human genes 0.000 claims 2
- 108090000445 Parathyroid hormone Proteins 0.000 claims 2
- 230000001054 cortical effect Effects 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 208000005368 osteomalacia Diseases 0.000 claims 2
- 208000001061 polyostotic fibrous dysplasia Diseases 0.000 claims 2
- QADPYRIHXKWUSV-UHFFFAOYSA-N BGJ-398 Chemical compound C1CN(CC)CCN1C(C=C1)=CC=C1NC1=CC(N(C)C(=O)NC=2C(=C(OC)C=C(OC)C=2Cl)Cl)=NC=N1 QADPYRIHXKWUSV-UHFFFAOYSA-N 0.000 claims 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229940125829 fibroblast growth factor receptor inhibitor Drugs 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 150000004712 monophosphates Chemical class 0.000 claims 1
- 210000004409 osteocyte Anatomy 0.000 claims 1
- 239000000199 parathyroid hormone Substances 0.000 claims 1
- 229960001319 parathyroid hormone Drugs 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261617889P | 2012-03-30 | 2012-03-30 | |
| US61/617,889 | 2012-03-30 | ||
| PCT/EP2013/056811 WO2013144339A1 (en) | 2012-03-30 | 2013-03-29 | Fgfr inhibitor for use in the treatment of hypophosphatemic disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015511621A JP2015511621A (ja) | 2015-04-20 |
| JP2015511621A5 true JP2015511621A5 (https=) | 2016-05-19 |
| JP6190871B2 JP6190871B2 (ja) | 2017-08-30 |
Family
ID=47998482
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015502373A Active JP6190871B2 (ja) | 2012-03-30 | 2013-03-29 | 低リン血症性障害の処置に使用するためのｆｇｆｒ阻害剤 |
Country Status (11)
| Country | Link |
|---|---|
| US (4) | US20150072019A1 (https=) |
| EP (1) | EP2830626B1 (https=) |
| JP (1) | JP6190871B2 (https=) |
| KR (1) | KR102126092B1 (https=) |
| CN (2) | CN109718239B (https=) |
| AU (1) | AU2013241664B2 (https=) |
| CA (1) | CA2866229C (https=) |
| IN (1) | IN2014DN08969A (https=) |
| MX (1) | MX354783B (https=) |
| RU (1) | RU2643326C2 (https=) |
| WO (1) | WO2013144339A1 (https=) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| EA028614B1 (ru) * | 2014-05-22 | 2017-12-29 | Общество С Ограниченной Ответственностью "Русские Фармацевтические Технологии" | Селективные ингибиторы, нарушающие взаимодействие рецептора фактора роста фибробластов и frs2, для профилактики и лечения рака |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| WO2016189472A1 (en) * | 2015-05-28 | 2016-12-01 | Novartis Ag | Fgfr inhibitor for use in the treatment of the phosphaturic mesenchymal tumor |
| BR112018001053A2 (pt) | 2015-07-20 | 2018-09-11 | Univ Taipei Medical | compostos, composição farmacêutica e método para inibir, prevenir ou tratar um câncer em um indivíduo |
| BR112018001438A2 (en) * | 2015-07-24 | 2018-12-04 | Debiopharm International S.A. | gffr expression and susceptibility to a gffr inhibitor |
| EP3566705B1 (en) | 2017-01-06 | 2022-11-23 | Lemonex Inc. | Composition for preventing or treating metastatic ovarian cancer, endometrial cancer or breast cancer |
| WO2018128510A1 (ko) * | 2017-01-06 | 2018-07-12 | 주식회사 레모넥스 | 전이성 난소암, 자궁내막암 또는 유방암의 예방 또는 치료용 조성물 |
| US10886468B2 (en) | 2017-04-14 | 2021-01-05 | Sakai Display Products Corporation | Manufacturing method and manufacturing apparatus for organic EL display device |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CR20200590A (es) | 2018-05-04 | 2021-04-26 | Incyte Corp | Formas sólidas de un inhibidor de fgfr y procesos para prepararlas |
| MA52493A (fr) | 2018-05-04 | 2021-03-10 | Incyte Corp | Sels d'un inhibiteur de fgfr |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| TWI891666B (zh) | 2019-10-14 | 2025-08-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之雙環雜環 |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| WO2021119108A1 (en) * | 2019-12-09 | 2021-06-17 | Cedars-Sinai Medical Center | Use of fgfr inhibitors for treatment of idiopathic short stature |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPWO2002052009A1 (ja) * | 2000-12-26 | 2004-04-30 | 中外製薬株式会社 | 血中リン濃度を低下させるヒトｆｇｆ２３タンパク質変異体 |
| GB0512324D0 (en) * | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| EP1882475A1 (en) * | 2006-07-26 | 2008-01-30 | Novartis AG | Method of treating disorders mediated by the fibroblast growth factor receptor |
| CA2720888A1 (en) * | 2008-04-29 | 2009-11-05 | Novartis Ag | Methods of monitoring the modulation of the kinase activity of fibroblast growth factor receptor and uses of said methods |
| CN102596916B (zh) * | 2009-10-30 | 2015-06-17 | 诺瓦提斯公司 | 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲的n-氧化物 |
| AR079257A1 (es) * | 2009-12-07 | 2012-01-04 | Novartis Ag | Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas |
| US20120258940A1 (en) * | 2009-12-18 | 2012-10-11 | Giordano Caponigro | Method for treating haematological cancers |
| WO2013088191A1 (en) | 2011-12-12 | 2013-06-20 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Antagonist of the fibroblast growth factor receptor 3 (fgfr3) for use in the treatment or the prevention of skeletal disorders linked with abnormal activation of fgfr3 |
-
2013
- 2013-03-29 US US14/388,978 patent/US20150072019A1/en not_active Abandoned
- 2013-03-29 MX MX2014011841A patent/MX354783B/es active IP Right Grant
- 2013-03-29 RU RU2014143517A patent/RU2643326C2/ru active
- 2013-03-29 IN IN8969DEN2014 patent/IN2014DN08969A/en unknown
- 2013-03-29 KR KR1020147026889A patent/KR102126092B1/ko active Active
- 2013-03-29 CN CN201811194059.3A patent/CN109718239B/zh active Active
- 2013-03-29 EP EP13712589.4A patent/EP2830626B1/en active Active
- 2013-03-29 CN CN201380015597.0A patent/CN104321058A/zh active Pending
- 2013-03-29 CA CA2866229A patent/CA2866229C/en active Active
- 2013-03-29 WO PCT/EP2013/056811 patent/WO2013144339A1/en not_active Ceased
- 2013-03-29 JP JP2015502373A patent/JP6190871B2/ja active Active
- 2013-03-29 AU AU2013241664A patent/AU2013241664B2/en active Active
-
2016
- 2016-09-22 US US15/272,633 patent/US10028955B2/en active Active
-
2018
- 2018-06-12 US US16/005,966 patent/US20210308132A1/en not_active Abandoned
-
2024
- 2024-01-09 US US18/407,729 patent/US20240398798A1/en not_active Abandoned
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