JP2015529194A5 - - Google Patents
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- JP2015529194A5 JP2015529194A5 JP2015527558A JP2015527558A JP2015529194A5 JP 2015529194 A5 JP2015529194 A5 JP 2015529194A5 JP 2015527558 A JP2015527558 A JP 2015527558A JP 2015527558 A JP2015527558 A JP 2015527558A JP 2015529194 A5 JP2015529194 A5 JP 2015529194A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- group
- alkyl
- methyl
- 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 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 17
- 230000002062 proliferating effect Effects 0.000 claims 17
- 201000010099 disease Diseases 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 206010039491 Sarcoma Diseases 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 201000011510 cancer Diseases 0.000 claims 9
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 229910052805 deuterium Inorganic materials 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 125000001153 fluoro group Chemical group F* 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- -1 cyano, imidazolyl Chemical group 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 208000005017 glioblastoma Diseases 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 3
- 208000009746 Adult T-Cell Leukemia-Lymphoma Diseases 0.000 claims 3
- 208000016683 Adult T-cell leukemia/lymphoma Diseases 0.000 claims 3
- 206010003571 Astrocytoma Diseases 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 3
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 3
- 206010025323 Lymphomas Diseases 0.000 claims 3
- 206010027406 Mesothelioma Diseases 0.000 claims 3
- 208000034578 Multiple myelomas Diseases 0.000 claims 3
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 3
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 3
- CXQHYVUVSFXTMY-UHFFFAOYSA-N N1'-[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide Chemical compound C1=CN=C2C=C(OCCCN3CCOCC3)C(OC)=CC2=C1OC(C(=C1)F)=CC=C1NC(=O)C1(C(=O)NC=2C=CC(F)=CC=2)CC1 CXQHYVUVSFXTMY-UHFFFAOYSA-N 0.000 claims 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 3
- 102000008022 Proto-Oncogene Proteins c-met Human genes 0.000 claims 3
- 108010089836 Proto-Oncogene Proteins c-met Proteins 0.000 claims 3
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 3
- 208000008383 Wilms tumor Diseases 0.000 claims 3
- 201000006966 adult T-cell leukemia Diseases 0.000 claims 3
- 210000000481 breast Anatomy 0.000 claims 3
- 210000003679 cervix uteri Anatomy 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 3
- 230000001419 dependent effect Effects 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 210000004696 endometrium Anatomy 0.000 claims 3
- 210000003238 esophagus Anatomy 0.000 claims 3
- 210000003128 head Anatomy 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 210000003734 kidney Anatomy 0.000 claims 3
- 210000004185 liver Anatomy 0.000 claims 3
- 210000004072 lung Anatomy 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 210000001989 nasopharynx Anatomy 0.000 claims 3
- 210000003739 neck Anatomy 0.000 claims 3
- 201000008026 nephroblastoma Diseases 0.000 claims 3
- 125000000449 nitro group Chemical class [O-][N+](*)=O 0.000 claims 3
- 210000001672 ovary Anatomy 0.000 claims 3
- 210000000496 pancreas Anatomy 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 claims 3
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims 3
- 210000002307 prostate Anatomy 0.000 claims 3
- 210000002784 stomach Anatomy 0.000 claims 3
- 210000001685 thyroid gland Anatomy 0.000 claims 3
- 210000003932 urinary bladder Anatomy 0.000 claims 3
- OAWXZFGKDDFTGS-BYPYZUCNSA-N (2s)-pyrrolidine-1,2-dicarboxylic acid Chemical compound OC(=O)[C@@H]1CCCN1C(O)=O OAWXZFGKDDFTGS-BYPYZUCNSA-N 0.000 claims 2
- CWHUFRVAEUJCEF-UHFFFAOYSA-N BKM120 Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(N2CCOCC2)=NC(N2CCOCC2)=N1 CWHUFRVAEUJCEF-UHFFFAOYSA-N 0.000 claims 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 201000007450 intrahepatic cholangiocarcinoma Diseases 0.000 claims 2
- LVTJOONKWUXEFR-FZRMHRINSA-N protoneodioscin Natural products O(C[C@@H](CC[C@]1(O)[C@H](C)[C@@H]2[C@]3(C)[C@H]([C@H]4[C@@H]([C@]5(C)C(=CC4)C[C@@H](O[C@@H]4[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@@H](O)[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@H](CO)O4)CC5)CC3)C[C@@H]2O1)C)[C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1 LVTJOONKWUXEFR-FZRMHRINSA-N 0.000 claims 2
- 229940124617 receptor tyrosine kinase inhibitor Drugs 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- GLBZSOQDAOLMGC-UHFFFAOYSA-N 1-(2-hydroxy-2-methylpropyl)-n-[5-(7-methoxyquinolin-4-yl)oxypyridin-2-yl]-5-methyl-3-oxo-2-phenylpyrazole-4-carboxamide Chemical compound C=1C=NC2=CC(OC)=CC=C2C=1OC(C=N1)=CC=C1NC(=O)C(C1=O)=C(C)N(CC(C)(C)O)N1C1=CC=CC=C1 GLBZSOQDAOLMGC-UHFFFAOYSA-N 0.000 claims 1
- 229940126062 Compound A Drugs 0.000 claims 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 1
- 239000002146 L01XE16 - Crizotinib Substances 0.000 claims 1
- UCEQXRCJXIVODC-PMACEKPBSA-N LSM-1131 Chemical compound C1CCC2=CC=CC3=C2N1C=C3[C@@H]1C(=O)NC(=O)[C@H]1C1=CNC2=CC=CC=C12 UCEQXRCJXIVODC-PMACEKPBSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 229940127361 Receptor Tyrosine Kinase Inhibitors Drugs 0.000 claims 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- KTEIFNKAUNYNJU-GFCCVEGCSA-N crizotinib Chemical compound O([C@H](C)C=1C(=C(F)C=CC=1Cl)Cl)C(C(=NC=1)N)=CC=1C(=C1)C=NN1C1CCNCC1 KTEIFNKAUNYNJU-GFCCVEGCSA-N 0.000 claims 1
- 229960005061 crizotinib Drugs 0.000 claims 1
- JOGKUKXHTYWRGZ-UHFFFAOYSA-N dactolisib Chemical group O=C1N(C)C2=CN=C3C=CC(C=4C=C5C=CC=CC5=NC=4)=CC3=C2N1C1=CC=C(C(C)(C)C#N)C=C1 JOGKUKXHTYWRGZ-UHFFFAOYSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229950008692 foretinib Drugs 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000014899 intrahepatic bile duct cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000005476 oxopyrrolidinyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 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
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 150000003254 radicals Chemical class 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261683790P | 2012-08-16 | 2012-08-16 | |
| US61/683,790 | 2012-08-16 | ||
| PCT/US2013/054848 WO2014028566A1 (en) | 2012-08-16 | 2013-08-14 | Combination of pi3k inhibitor and c-met inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017201774A Division JP6644042B2 (ja) | 2012-08-16 | 2017-10-18 | ＰＩ３Ｋインヒビターとｃ−Ｍｅｔインヒビターの組み合わせ |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015529194A JP2015529194A (ja) | 2015-10-05 |
| JP2015529194A5 true JP2015529194A5 (enExample) | 2016-09-29 |
Family
ID=49004065
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015527558A Withdrawn JP2015529194A (ja) | 2012-08-16 | 2013-08-14 | ＰＩ３Ｋインヒビターとｃ−Ｍｅｔインヒビターの組み合わせ |
| JP2017201774A Expired - Fee Related JP6644042B2 (ja) | 2012-08-16 | 2017-10-18 | ＰＩ３Ｋインヒビターとｃ−Ｍｅｔインヒビターの組み合わせ |
| JP2020000928A Expired - Fee Related JP6970217B2 (ja) | 2012-08-16 | 2020-01-07 | ＰＩ３Ｋインヒビターとｃ−Ｍｅｔインヒビターの組み合わせ |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017201774A Expired - Fee Related JP6644042B2 (ja) | 2012-08-16 | 2017-10-18 | ＰＩ３Ｋインヒビターとｃ−Ｍｅｔインヒビターの組み合わせ |
| JP2020000928A Expired - Fee Related JP6970217B2 (ja) | 2012-08-16 | 2020-01-07 | ＰＩ３Ｋインヒビターとｃ−Ｍｅｔインヒビターの組み合わせ |
Country Status (14)
| Country | Link |
|---|---|
| US (5) | US20150216870A1 (enExample) |
| EP (1) | EP2885003B1 (enExample) |
| JP (3) | JP2015529194A (enExample) |
| KR (2) | KR20210049187A (enExample) |
| CN (1) | CN105050623B (enExample) |
| AU (4) | AU2013302702A1 (enExample) |
| BR (1) | BR112015002528A2 (enExample) |
| CA (1) | CA2879704A1 (enExample) |
| ES (1) | ES2901712T3 (enExample) |
| HK (1) | HK1211476A1 (enExample) |
| IN (1) | IN2015DN00528A (enExample) |
| MX (1) | MX369518B (enExample) |
| RU (1) | RU2705095C2 (enExample) |
| WO (1) | WO2014028566A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6026544B2 (ja) | 2011-09-27 | 2016-11-16 | ノバルティス アーゲー | 変異体ｉｄｈの阻害剤としての３−ピリミジン−４−イル−オキサゾリジン−２−オン類 |
| UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
| KR102115047B1 (ko) | 2012-04-03 | 2020-05-26 | 노파르티스 아게 | 티로신 키나제 억제제들을 갖는 조합 제품 및 그의 용도 |
| US9296733B2 (en) | 2012-11-12 | 2016-03-29 | Novartis Ag | Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases |
| GEP201706699B (en) | 2013-03-14 | 2017-07-10 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| CA2914310A1 (en) * | 2013-06-18 | 2014-12-24 | Novartis Ag | Pharmaceutical combinations |
| MX2016000750A (es) | 2013-08-02 | 2016-08-05 | Aduro Biotech Holdings Europe B V | Combinacion de agonistas de cd27 e inhibicion del punto de control inmunologico para estimulacion del sistema inmunologico. |
| CA2954840A1 (en) | 2014-07-25 | 2016-01-28 | Novartis Ag | Tablet formulation of 2-fluoro-n-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide |
| US10689459B2 (en) | 2014-12-12 | 2020-06-23 | Novartis Ag | Treatment of breast cancer brain metastases |
| GB201516504D0 (en) | 2015-09-17 | 2015-11-04 | Astrazeneca Ab | Imadazo(4,5-c)quinolin-2-one Compounds and their use in treating cancer |
| IL294081A (en) * | 2019-12-20 | 2022-08-01 | Recurium Ip Holdings Llc | Combinations |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0211649D0 (en) * | 2002-05-21 | 2002-07-03 | Novartis Ag | Organic compounds |
| GB0510390D0 (en) * | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| CA2669991C (en) * | 2006-11-22 | 2016-01-26 | Incyte Corporation | Imidazotriazines and imidazopyrimidines as kinase inhibitors |
| CN101616672A (zh) * | 2007-02-20 | 2009-12-30 | 诺瓦提斯公司 | 作为脂质激酶和mTOR双重抑制剂的咪唑并喹啉类 |
| US20110033453A1 (en) * | 2008-03-05 | 2011-02-10 | Carlos Garcia-Echeverria | Use of pyrimidine derivatives for the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members |
| CA2724742C (en) * | 2008-05-21 | 2016-07-19 | Incyte Corporation | Salts of 2-fluoro-n-methyl-4-[7-(quinolin-6-yl-methyl)- imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same |
| MX2011000440A (es) * | 2008-07-11 | 2011-02-24 | Novartis Ag | Combinacion de (a) un inhibidor de fosfoinositido 3-cinasa y (b) un modulador de la ruta de ras/raf/mek. |
| UA104147C2 (uk) * | 2008-09-10 | 2014-01-10 | Новартис Аг | Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань |
| US20100267742A1 (en) * | 2009-04-17 | 2010-10-21 | Rush University Medical Center | Combination targeted therapy for lung cancer |
| AR083267A1 (es) * | 2010-10-04 | 2013-02-13 | Novartis Ag | Combinaciones farmaceuticas |
| CN103200943A (zh) * | 2010-11-08 | 2013-07-10 | 诺华有限公司 | 2-甲酰胺环氨基尿素衍生物在治疗egfr依赖性疾病或对靶向egfr家族成员的药剂有获得性耐受性的疾病中的应用 |
-
2013
- 2013-08-14 AU AU2013302702A patent/AU2013302702A1/en not_active Abandoned
- 2013-08-14 HK HK15112283.4A patent/HK1211476A1/xx unknown
- 2013-08-14 MX MX2015002005A patent/MX369518B/es active IP Right Grant
- 2013-08-14 ES ES13751058T patent/ES2901712T3/es active Active
- 2013-08-14 BR BR112015002528-5A patent/BR112015002528A2/pt not_active Application Discontinuation
- 2013-08-14 WO PCT/US2013/054848 patent/WO2014028566A1/en not_active Ceased
- 2013-08-14 CN CN201380043882.3A patent/CN105050623B/zh not_active Expired - Fee Related
- 2013-08-14 IN IN528DEN2015 patent/IN2015DN00528A/en unknown
- 2013-08-14 EP EP13751058.2A patent/EP2885003B1/en not_active Not-in-force
- 2013-08-14 JP JP2015527558A patent/JP2015529194A/ja not_active Withdrawn
- 2013-08-14 KR KR1020217012172A patent/KR20210049187A/ko not_active Ceased
- 2013-08-14 CA CA2879704A patent/CA2879704A1/en not_active Abandoned
- 2013-08-14 RU RU2015108755A patent/RU2705095C2/ru active
- 2013-08-14 KR KR1020157003716A patent/KR102245985B1/ko not_active Expired - Fee Related
- 2013-08-14 US US14/420,792 patent/US20150216870A1/en not_active Abandoned
-
2016
- 2016-10-06 AU AU2016238903A patent/AU2016238903A1/en not_active Abandoned
-
2017
- 2017-10-18 JP JP2017201774A patent/JP6644042B2/ja not_active Expired - Fee Related
-
2018
- 2018-03-09 AU AU2018201725A patent/AU2018201725A1/en not_active Abandoned
- 2018-10-11 US US16/157,333 patent/US20190083500A1/en not_active Abandoned
-
2019
- 2019-07-30 US US16/526,027 patent/US20190350935A1/en not_active Abandoned
- 2019-09-05 AU AU2019226212A patent/AU2019226212B2/en not_active Ceased
-
2020
- 2020-01-07 JP JP2020000928A patent/JP6970217B2/ja not_active Expired - Fee Related
- 2020-03-17 US US16/820,886 patent/US20200253980A1/en not_active Abandoned
-
2021
- 2021-12-15 US US17/644,491 patent/US20220280523A1/en not_active Abandoned
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