JP2015524472A5 - - Google Patents
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- Publication number
- JP2015524472A5 JP2015524472A5 JP2015526606A JP2015526606A JP2015524472A5 JP 2015524472 A5 JP2015524472 A5 JP 2015524472A5 JP 2015526606 A JP2015526606 A JP 2015526606A JP 2015526606 A JP2015526606 A JP 2015526606A JP 2015524472 A5 JP2015524472 A5 JP 2015524472A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- deuterium
- inhibitor
- combination
- 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
- 239000003814 drug Substances 0.000 claims 14
- 125000001424 substituent group Chemical group 0.000 claims 10
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 8
- 229910052805 deuterium Inorganic materials 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 230000002062 proliferating effect Effects 0.000 claims 7
- KKVYYGGCHJGEFJ-UHFFFAOYSA-N 1-n-(4-chlorophenyl)-6-methyl-5-n-[3-(7h-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine Chemical compound N=1C=CC2=C(NC=3C(=CC=CN=3)C=3C=4N=CNC=4N=CN=3)C(C)=CC=C2C=1NC1=CC=C(Cl)C=C1 KKVYYGGCHJGEFJ-UHFFFAOYSA-N 0.000 claims 6
- 101100381978 Mus musculus Braf gene Proteins 0.000 claims 6
- 229940121647 egfr inhibitor Drugs 0.000 claims 6
- 230000035772 mutation Effects 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 229960005395 cetuximab Drugs 0.000 claims 3
- -1 cyano, aminocarbonyl Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 239000012828 PI3K inhibitor Substances 0.000 claims 2
- 229940124607 PI3Kα inhibitor Drugs 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims 2
- OAWXZFGKDDFTGS-BYPYZUCNSA-N (2s)-pyrrolidine-1,2-dicarboxylic acid Chemical compound OC(=O)[C@@H]1CCCN1C(O)=O OAWXZFGKDDFTGS-BYPYZUCNSA-N 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 229940000425 combination drug Drugs 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229960001433 erlotinib Drugs 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 229960001972 panitumumab Drugs 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261680473P | 2012-08-07 | 2012-08-07 | |
| US61/680,473 | 2012-08-07 | ||
| PCT/US2013/053619 WO2014025688A1 (en) | 2012-08-07 | 2013-08-05 | Pharmaceutical combinations comprising a b-raf inhibitor, an egfr inhibitor and optionally a pi3k-alpha inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018022248A Division JP6595024B2 (ja) | 2012-08-07 | 2018-02-09 | Ｂ−Ｒａｆ阻害薬、ＥＧＦＲ阻害薬及び場合によってはＰＩ３Ｋ−α阻害薬を含む組合せ医薬 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015524472A JP2015524472A (ja) | 2015-08-24 |
| JP2015524472A5 true JP2015524472A5 (enExample) | 2016-09-15 |
| JP6342396B2 JP6342396B2 (ja) | 2018-06-13 |
Family
ID=48980368
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015526606A Active JP6342396B2 (ja) | 2012-08-07 | 2013-08-05 | Ｂ−Ｒａｆ阻害薬、ＥＧＦＲ阻害薬及び場合によってはＰＩ３Ｋ−α阻害薬を含む組合せ医薬 |
| JP2018022248A Active JP6595024B2 (ja) | 2012-08-07 | 2018-02-09 | Ｂ−Ｒａｆ阻害薬、ＥＧＦＲ阻害薬及び場合によってはＰＩ３Ｋ−α阻害薬を含む組合せ医薬 |
| JP2019174353A Active JP6974669B2 (ja) | 2012-08-07 | 2019-09-25 | Ｂ−Ｒａｆ阻害薬、ＥＧＦＲ阻害薬及び場合によってはＰＩ３Ｋ−α阻害薬を含む組合せ医薬 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018022248A Active JP6595024B2 (ja) | 2012-08-07 | 2018-02-09 | Ｂ−Ｒａｆ阻害薬、ＥＧＦＲ阻害薬及び場合によってはＰＩ３Ｋ−α阻害薬を含む組合せ医薬 |
| JP2019174353A Active JP6974669B2 (ja) | 2012-08-07 | 2019-09-25 | Ｂ−Ｒａｆ阻害薬、ＥＧＦＲ阻害薬及び場合によってはＰＩ３Ｋ−α阻害薬を含む組合せ医薬 |
Country Status (39)
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA028420B1 (ru) * | 2012-08-07 | 2017-11-30 | Новартис Аг | Фармацевтические комбинации, содержащие ингибитор b-raf, ингибитор egfr и, необязательно, ингибитор pi3k-альфа |
| PL2976106T3 (pl) | 2013-03-21 | 2021-10-25 | Array Biopharma Inc. | Terapia kombinowana obejmująca inhibitor B-Raf i drugi inhibitor |
| WO2015145388A2 (en) * | 2014-03-27 | 2015-10-01 | Novartis Ag | Methods of treating colorectal cancers harboring upstream wnt pathway mutations |
| DK3155126T3 (en) * | 2014-06-16 | 2018-09-03 | Worldwide Innovative Network | METHOD OF CHOOSING PERSONAL TRIAL TREATMENT FOR CANCER TREATMENT |
| WO2016193955A1 (en) * | 2015-06-04 | 2016-12-08 | Giorgio Stassi | Combinations of kinase inhibitors for treating colorectal cancer |
| EP3355886A1 (en) * | 2015-08-28 | 2018-08-08 | Novartis AG | Pharmaceutical combination comprising the pi3k inhibitor alpelisib and the b-raf inhibitor dabrafenib; the use of such combination in the treatment or prevention of cancer |
| JP2018526375A (ja) * | 2015-08-28 | 2018-09-13 | ノバルティス アーゲー | 組み合わせ療法 |
| WO2017066664A1 (en) * | 2015-10-16 | 2017-04-20 | Millennium Pharmaceuticals, Inc. | Combination therapy including a raf inhibitor for the treatment of colorectal cancer |
| MX387795B (es) | 2016-06-03 | 2025-03-19 | Array Biopharma Inc | Combinaciones farmaceuticas. |
| AU2017329090B9 (en) * | 2016-09-19 | 2019-09-05 | Novartis Ag | Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor |
| MX393855B (es) | 2017-05-02 | 2025-03-21 | Novartis Ag | Terapia de combinación que comprende un inhibidor de raf y trametinib |
| EP3661516A1 (en) * | 2017-08-03 | 2020-06-10 | Novartis AG | Therapeutic combination of a third-generation egfr tyrosine kinase inhibitor and a raf inhibitor |
| SI3860998T1 (sl) | 2018-10-05 | 2024-06-28 | Annapurna Bio Inc. | Spojine in sestavki za zdravljenje stanj, povezanih z aktivnostjo apj-receptorja |
| TWI849043B (zh) * | 2019-01-25 | 2024-07-21 | 英屬開曼群島商百濟神州有限公司 | B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途 |
| WO2020164997A1 (en) * | 2019-02-12 | 2020-08-20 | Bayer Aktiengesellschaft | Combination of pi3k-inhibitors |
| AU2020276695B2 (en) | 2019-05-13 | 2025-12-18 | Novartis Ag | New crystalline forms of N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as RAF inhibitors for the treatment of cancer |
| JPWO2023145530A1 (enExample) * | 2022-01-27 | 2023-08-03 | ||
| WO2023230554A1 (en) | 2022-05-25 | 2023-11-30 | Pfizer Inc. | Combination of a braf inhibitor, an egfr inhibitor, and a pd-1 antagonist for the treatment of braf v600e-mutant, msi-h/dmmr colorectal cancer |
| WO2024073364A1 (en) * | 2022-09-26 | 2024-04-04 | Beigene, Ltd. | Combinations of a b-raf inhibitor, and an anti-egfr antibody for the treatment of cancer |
| WO2025003956A1 (en) | 2023-06-30 | 2025-01-02 | Pfizer Inc. | High drug loading formulations of encorafenib |
| WO2025262686A1 (en) * | 2024-06-20 | 2025-12-26 | Ilan Paz | Devices, systems and methods for optimized, personalized administration of oral dosage forms |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU4128089A (en) | 1988-09-15 | 1990-03-22 | Rorer International (Overseas) Inc. | Monoclonal antibodies specific to human epidermal growth factor receptor and therapeutic methods employing same |
| US6235883B1 (en) | 1997-05-05 | 2001-05-22 | Abgenix, Inc. | Human monoclonal antibodies to epidermal growth factor receptor |
| RS52939B (sr) | 2007-04-10 | 2014-02-28 | Exelixis Inc. | Postupci za lečenje kancera upotrebom piridopirimidinonskih inhibitora pi3k alfa |
| UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| BR112012003926A2 (pt) * | 2009-08-24 | 2020-08-11 | Genentech Inc | método para identificar um paciente não responsivo ao tratamento com um inibidor de b-raf, método para determinar se um tumor irá responder ao tratamento com um inibidor de b-raf, método para predizer se um paciente será não responsivo ao tratamento com um inibidor de braf específico, kit, método para classificar um tumor de mama, pulmão, cólon, ovário, tiroide, melanoma, ou pancreático e método para identificar um tumor não responsivo ao tratamento com um inibidor de b-raf |
| AR077975A1 (es) * | 2009-08-28 | 2011-10-05 | Irm Llc | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
| CN102665720A (zh) * | 2009-10-12 | 2012-09-12 | 葛兰素史密斯克莱有限责任公司 | 组合 |
| US20120045433A1 (en) | 2010-08-17 | 2012-02-23 | Kapil Dhingra | Combination therapy |
| MX360157B (es) * | 2010-11-08 | 2018-10-24 | Novartis Ag | Uso de derivados de 2-carboxamida-cicloamino-urea en el tratamiento de enfermedades dependientes de egfr o de enfermedades que han adquirido resistencia a los agentes que tienen como objetivo los miembros de la familia egfr. |
| CA2855245A1 (en) | 2011-11-10 | 2013-05-16 | Memorial Sloan-Kettering Cancer Center | Treatment of ovarian cancer with 2-amino-4h-naphtho[1,2-b]pyran-3-carbonitriles |
| AU2012335663B2 (en) * | 2011-11-11 | 2015-12-24 | Array Biopharma Inc. | Method of treating a proliferative disease |
| EA028420B1 (ru) * | 2012-08-07 | 2017-11-30 | Новартис Аг | Фармацевтические комбинации, содержащие ингибитор b-raf, ингибитор egfr и, необязательно, ингибитор pi3k-альфа |
-
2013
- 2013-08-05 EA EA201590332A patent/EA028420B1/ru not_active IP Right Cessation
- 2013-08-05 US US14/419,256 patent/US9474754B2/en active Active
- 2013-08-05 PT PT13748243T patent/PT2882440T/pt unknown
- 2013-08-05 MX MX2015001732A patent/MX359403B/es active IP Right Grant
- 2013-08-05 RS RS20190351A patent/RS58734B1/sr unknown
- 2013-08-05 DK DK13748243.6T patent/DK2882440T3/da active
- 2013-08-05 CN CN201380042229.5A patent/CN104519887B/zh active Active
- 2013-08-05 ES ES13748243T patent/ES2717911T3/es active Active
- 2013-08-05 HU HUE13748243A patent/HUE042877T2/hu unknown
- 2013-08-05 PE PE2015000130A patent/PE20150673A1/es not_active Application Discontinuation
- 2013-08-05 CA CA2879548A patent/CA2879548C/en active Active
- 2013-08-05 AR ARP130102776A patent/AR092045A1/es not_active Application Discontinuation
- 2013-08-05 EP EP19159506.5A patent/EP3574904A1/en active Pending
- 2013-08-05 HR HRP20190537TT patent/HRP20190537T1/hr unknown
- 2013-08-05 TR TR2019/04980T patent/TR201904980T4/tr unknown
- 2013-08-05 SG SG11201500321YA patent/SG11201500321YA/en unknown
- 2013-08-05 EP EP13748243.6A patent/EP2882440B1/en active Active
- 2013-08-05 NZ NZ703940A patent/NZ703940A/en unknown
- 2013-08-05 SI SI201331387T patent/SI2882440T1/sl unknown
- 2013-08-05 UA UAA201500424A patent/UA115786C2/uk unknown
- 2013-08-05 JP JP2015526606A patent/JP6342396B2/ja active Active
- 2013-08-05 AU AU2013299841A patent/AU2013299841B8/en active Active
- 2013-08-05 WO PCT/US2013/053619 patent/WO2014025688A1/en not_active Ceased
- 2013-08-05 HK HK15110834.2A patent/HK1211831A1/xx unknown
- 2013-08-05 PL PL13748243T patent/PL2882440T3/pl unknown
- 2013-08-05 LT LTEP13748243.6T patent/LT2882440T/lt unknown
- 2013-08-05 MY MYPI2015000102A patent/MY176031A/en unknown
- 2013-08-05 PE PE2019001539A patent/PE20191655A1/es unknown
- 2013-08-05 KR KR1020157002982A patent/KR102112885B1/ko active Active
- 2013-08-05 IN IN450DEN2015 patent/IN2015DN00450A/en unknown
- 2013-08-06 TW TW102128165A patent/TWI607754B/zh active
- 2013-08-06 JO JOP/2013/0236A patent/JOP20130236B1/ar active
-
2015
- 2015-01-19 TN TNP2015000027A patent/TN2015000027A1/fr unknown
- 2015-01-26 IL IL236934A patent/IL236934B/en active IP Right Grant
- 2015-02-04 PH PH12015500246A patent/PH12015500246A1/en unknown
- 2015-02-04 MA MA37829A patent/MA37829A1/fr unknown
- 2015-02-06 CO CO15024921A patent/CO7200273A2/es unknown
- 2015-02-06 CL CL2015000294A patent/CL2015000294A1/es unknown
- 2015-02-06 GT GT201500025A patent/GT201500025A/es unknown
- 2015-03-06 EC ECIEPI20158695A patent/ECSP15008695A/es unknown
-
2018
- 2018-02-09 JP JP2018022248A patent/JP6595024B2/ja active Active
-
2019
- 2019-04-30 CY CY20191100461T patent/CY1122143T1/el unknown
- 2019-09-25 JP JP2019174353A patent/JP6974669B2/ja active Active
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