JP2020517598A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2020517598A5 JP2020517598A5 JP2019555918A JP2019555918A JP2020517598A5 JP 2020517598 A5 JP2020517598 A5 JP 2020517598A5 JP 2019555918 A JP2019555918 A JP 2019555918A JP 2019555918 A JP2019555918 A JP 2019555918A JP 2020517598 A5 JP2020517598 A5 JP 2020517598A5
- Authority
- JP
- Japan
- Prior art keywords
- isoindole
- methoxyphenyl
- dihydro
- oxo
- fluoro
- 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 oxan-4-yl Chemical group 0.000 claims 34
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 22
- 230000002265 prevention Effects 0.000 claims 16
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 15
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 13
- 206010028980 Neoplasm Diseases 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 206010009944 Colon cancer Diseases 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 5
- 238000000634 powder X-ray diffraction Methods 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide Chemical compound CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 claims 4
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims 4
- 206010025323 Lymphomas Diseases 0.000 claims 4
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical group CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 claims 4
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims 4
- 239000007900 aqueous suspension Substances 0.000 claims 4
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 4
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 4
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 4
- 230000003211 malignant effect Effects 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000011580 syndromic disease Diseases 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 3
- 208000019838 Blood disease Diseases 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 3
- 239000002253 acid Substances 0.000 claims 3
- 208000014951 hematologic disease Diseases 0.000 claims 3
- 208000018706 hematopoietic system disease Diseases 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 2
- 101150073096 NRAS gene Proteins 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 2
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 2
- 238000000113 differential scanning calorimetry Methods 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 150000004668 long chain fatty acids Chemical class 0.000 claims 2
- 230000036210 malignancy Effects 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 230000002071 myeloproliferative effect Effects 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 239000002245 particle Substances 0.000 claims 2
- 150000003512 tertiary amines Chemical class 0.000 claims 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 2
- QKRMFCXDTFLKKT-UHFFFAOYSA-N 2-hydroxyethanesulfonic acid Chemical compound OCCS(O)(=O)=O.OCCS(O)(=O)=O QKRMFCXDTFLKKT-UHFFFAOYSA-N 0.000 claims 1
- 229940080296 2-naphthalenesulfonate Drugs 0.000 claims 1
- GIZKBEAJKWOWLS-UHFFFAOYSA-N 6-[5-chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]-2,3-dihydroisoindol-1-one Chemical compound ClC=1C(=NC(=NC=1)NC1CCOCC1)C1=CC=C2CNC(C2=C1)=O GIZKBEAJKWOWLS-UHFFFAOYSA-N 0.000 claims 1
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010010356 Congenital anomaly Diseases 0.000 claims 1
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 claims 1
- 206010014950 Eosinophilia Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 239000007821 HATU Substances 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 102000019149 MAP kinase activity proteins Human genes 0.000 claims 1
- 108040008097 MAP kinase activity proteins Proteins 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- LKJPYSCBVHEWIU-UHFFFAOYSA-N N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide Chemical compound C=1C=C(C#N)C(C(F)(F)F)=CC=1NC(=O)C(O)(C)CS(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-UHFFFAOYSA-N 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 239000004721 Polyphenylene oxide Substances 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000000389 T-cell leukemia Diseases 0.000 claims 1
- 208000028530 T-cell lymphoblastic leukemia/lymphoma Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 239000000010 aprotic solvent Substances 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 claims 1
- 229940077388 benzenesulfonate Drugs 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 claims 1
- 229950004221 besilate Drugs 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 210000002798 bone marrow cell Anatomy 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 238000007323 disproportionation reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 210000002308 embryonic cell Anatomy 0.000 claims 1
- 201000011523 endocrine gland cancer Diseases 0.000 claims 1
- 210000000981 epithelium Anatomy 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- AFAXGSQYZLGZPG-UHFFFAOYSA-L ethane-1,2-disulfonate Chemical compound [O-]S(=O)(=O)CCS([O-])(=O)=O AFAXGSQYZLGZPG-UHFFFAOYSA-L 0.000 claims 1
- 230000001605 fetal effect Effects 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 230000002489 hematologic effect Effects 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
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 1
- 230000000527 lymphocytic effect Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- XTEGVFVZDVNBPF-UHFFFAOYSA-N naphthalene-1,5-disulfonic acid Chemical compound C1=CC=C2C(S(=O)(=O)O)=CC=CC2=C1S(O)(=O)=O XTEGVFVZDVNBPF-UHFFFAOYSA-N 0.000 claims 1
- KVBGVZZKJNLNJU-UHFFFAOYSA-M naphthalene-2-sulfonate Chemical compound C1=CC=CC2=CC(S(=O)(=O)[O-])=CC=C21 KVBGVZZKJNLNJU-UHFFFAOYSA-M 0.000 claims 1
- 229950006327 napsilate Drugs 0.000 claims 1
- 239000002736 nonionic surfactant Substances 0.000 claims 1
- 230000007170 pathology Effects 0.000 claims 1
- 201000005528 peripheral nervous system neoplasm Diseases 0.000 claims 1
- 229920000570 polyether Polymers 0.000 claims 1
- 208000003476 primary myelofibrosis Diseases 0.000 claims 1
- 208000012201 sexual and gender identity disease Diseases 0.000 claims 1
- 208000015891 sexual disease Diseases 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 238000003756 stirring Methods 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000002411 thermogravimetry Methods 0.000 claims 1
- 150000003626 triacylglycerols Chemical class 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 125000005500 uronium group Chemical group 0.000 claims 1
- 230000004580 weight loss Effects 0.000 claims 1
- NAZAQFAQNOECEK-SECBINFHSA-N COc1cc(F)cc([C@@H](CO)N)c1 Chemical compound COc1cc(F)cc([C@@H](CO)N)c1 NAZAQFAQNOECEK-SECBINFHSA-N 0.000 description 2
- QAPPIHUULOISOQ-LLVKDONJSA-N C[C@H](C(O)=O)N(Cc(cc1)c2cc1-c(nc(NC1CCOCC1)nc1)c1Cl)C2=O Chemical compound C[C@H](C(O)=O)N(Cc(cc1)c2cc1-c(nc(NC1CCOCC1)nc1)c1Cl)C2=O QAPPIHUULOISOQ-LLVKDONJSA-N 0.000 description 1
- DEXRGKNMLMWKQQ-SSDOTTSWSA-N C[C@H](C(O)=O)N(Cc(cc1)c2cc1-c(nc(nc1)Cl)c1Cl)C2=O Chemical compound C[C@H](C(O)=O)N(Cc(cc1)c2cc1-c(nc(nc1)Cl)c1Cl)C2=O DEXRGKNMLMWKQQ-SSDOTTSWSA-N 0.000 description 1
- 0 C[C@](*(O)=O)N(Cc(cc1)c2cc1-c(nc(NC1CCOCC1)nc1)c1Cl)C2=O Chemical compound C[C@](*(O)=O)N(Cc(cc1)c2cc1-c(nc(NC1CCOCC1)nc1)c1Cl)C2=O 0.000 description 1
- AHVQYHFYQWKUKB-UHFFFAOYSA-N NC1CCOCC1 Chemical compound NC1CCOCC1 AHVQYHFYQWKUKB-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1706327.2 | 2017-04-20 | ||
| GBGB1706327.2A GB201706327D0 (en) | 2017-04-20 | 2017-04-20 | A pharmaceutical compound |
| PCT/IB2018/052745 WO2018193410A1 (en) | 2017-04-20 | 2018-04-20 | 6-pyrimidin-isoindole derivative as erk1/2 inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020517598A JP2020517598A (ja) | 2020-06-18 |
| JP2020517598A5 true JP2020517598A5 (https=) | 2021-05-27 |
| JP7113846B2 JP7113846B2 (ja) | 2022-08-05 |
Family
ID=58795788
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019555918A Active JP7113846B2 (ja) | 2017-04-20 | 2018-04-20 | Ｅｒｋ１／２阻害剤としての６－ピリミジン－イソインドール誘導体 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US11142518B2 (https=) |
| EP (1) | EP3612524B1 (https=) |
| JP (1) | JP7113846B2 (https=) |
| KR (1) | KR102652193B1 (https=) |
| CN (1) | CN110831939B (https=) |
| AU (1) | AU2018255935B2 (https=) |
| CA (1) | CA3059674A1 (https=) |
| DK (1) | DK3612524T3 (https=) |
| ES (1) | ES2994283T3 (https=) |
| FI (1) | FI3612524T3 (https=) |
| GB (1) | GB201706327D0 (https=) |
| IL (1) | IL269803B (https=) |
| MA (1) | MA52123A (https=) |
| MX (1) | MX2019012471A (https=) |
| MY (1) | MY203722A (https=) |
| PH (1) | PH12019502154A1 (https=) |
| SA (1) | SA519410253B1 (https=) |
| SG (1) | SG11201909189QA (https=) |
| TW (1) | TWI813566B (https=) |
| WO (1) | WO2018193410A1 (https=) |
| ZA (1) | ZA201907484B (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE068392T2 (hu) * | 2015-10-21 | 2024-12-28 | Otsuka Pharma Co Ltd | Benzolaktám vegyületek mint fehérje kináz gátlók |
| GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
| IL276232B2 (en) | 2018-03-02 | 2024-04-01 | Otsuka Pharma Co Ltd | Pyrazine derivatives, pharmaceutical compositions comprising them and their use for treating diseases |
| MX2021000795A (es) | 2018-07-24 | 2021-04-12 | Taiho Pharmaceutical Co Ltd | Compuestos heterociclicos para inhibir la actividad de shp2. |
| CN109608444B (zh) * | 2018-11-27 | 2022-02-11 | 中国药科大学 | 含异吲哚啉酮的erk抑制剂及其制备方法与用途 |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| TW202140024A (zh) * | 2020-01-24 | 2021-11-01 | 日商大鵬藥品工業股份有限公司 | Shp2抑制劑嘧啶酮與新穎癌症醫藥併用於癌症之抗腫瘤活性之增強 |
| 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 |
| CN113967198A (zh) * | 2020-07-24 | 2022-01-25 | 鲁南制药集团股份有限公司 | 一种甾体cyp17抑制剂胶囊及其制备方法 |
| US20230312564A1 (en) * | 2020-08-21 | 2023-10-05 | Shanghai Ringene Biopharma Co., Ltd. | Aromatic ring-lactam compound, preparation method therefor and use thereof |
| KR20240021198A (ko) * | 2021-06-11 | 2024-02-16 | 오츠카 세이야쿠 가부시키가이샤 | Erk 억제제의 제조 방법 |
| US11931370B2 (en) * | 2021-10-08 | 2024-03-19 | Slayback Pharma Llc | Stable pharmaceutical compositions of cyclophosphamide |
| US20240415835A1 (en) * | 2021-10-26 | 2024-12-19 | Otsuka Pharmaceutical Co., Ltd. | Compositions comprising an erk inhibitor |
| CN114085213B (zh) * | 2022-01-20 | 2022-03-25 | 苏州国匡医药科技有限公司 | 一种arv-471的制备方法 |
Family Cites Families (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5629327A (en) | 1993-03-01 | 1997-05-13 | Childrens Hospital Medical Center Corp. | Methods and compositions for inhibition of angiogenesis |
| US5463063A (en) | 1993-07-02 | 1995-10-31 | Celgene Corporation | Ring closure of N-phthaloylglutamines |
| US5958934A (en) | 1996-05-23 | 1999-09-28 | Syntex (U.S.A.) Inc. | Aryl pyrimidine derivatives and uses thereof |
| JP2003504301A (ja) | 1998-04-01 | 2003-02-04 | ブリストル−マイヤーズ スクイブ ファーマ カンパニー | インテグリンアンタゴニスト |
| CA2450934A1 (en) | 2001-06-19 | 2002-12-27 | Marco Dodier | Pyrimidine inhibitors of phosphodiesterase (pde) 7 |
| MXPA05011523A (es) | 2003-04-30 | 2006-01-23 | Inst For Pharm Discovery Inc | Heteroarilos sustituidos como inhibidores de proteinas de tirosina fosfatasas. |
| US7504401B2 (en) | 2003-08-29 | 2009-03-17 | Locus Pharmaceuticals, Inc. | Anti-cancer agents and uses thereof |
| EP1663204B1 (en) | 2003-08-29 | 2014-05-07 | Exelixis, Inc. | C-kit modulators and methods of use |
| UA84930C2 (ru) | 2004-05-14 | 2008-12-10 | Вертекс Фармасьютикалс Инкорпорейтед | Пиррольные соединения как ингибиторы протеинкиназ erk, их синтез и соответствующие промежуточные соединения |
| WO2006113769A1 (en) | 2005-04-15 | 2006-10-26 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
| KR101417136B1 (ko) | 2005-12-13 | 2014-08-07 | 머크 샤프 앤드 돔 코포레이션 | Ｅｒｋ 억제제인 폴리사이클릭 인다졸 유도체 및 이를 포함하는 약제학적 조성물 |
| US20080280891A1 (en) | 2006-06-27 | 2008-11-13 | Locus Pharmaceuticals, Inc. | Anti-cancer agents and uses thereof |
| CA2654670A1 (en) | 2006-07-06 | 2008-01-10 | Boehringer Ingelheim International Gmbh | New compounds |
| WO2008008059A1 (en) | 2006-07-12 | 2008-01-17 | Locus Pharmaceuticals, Inc. | Anti-cancer agents ans uses thereof |
| WO2008124085A2 (en) | 2007-04-03 | 2008-10-16 | Exelixis, Inc. | Methods of using combinations of mek and jak-2 inhibitors |
| WO2009017838A2 (en) | 2007-08-01 | 2009-02-05 | Exelixis, Inc. | Combinations of jak-2 inhibitors and other agents |
| WO2009039635A1 (en) | 2007-09-24 | 2009-04-02 | Painceptor Pharma Corporation | Methods of modulating neurotrophin-mediated activity |
| EP2215074B1 (en) | 2007-09-27 | 2014-02-19 | The United States of America, as Represented by the Secretary, Department of Health and Human Services | Isoindoline compounds for the treatment of spinal muscular atrophy and other uses |
| WO2009092432A1 (en) | 2008-01-24 | 2009-07-30 | Merck Patent Gmbh | Beta-amino acid derivatives for treatment of diabetes |
| NZ603525A (en) | 2008-06-27 | 2015-02-27 | Celgene Avilomics Res Inc | Pyrimidine based compound and uses thereof |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| GB0815369D0 (en) | 2008-08-22 | 2008-10-01 | Summit Corp Plc | Compounds for treatment of duchenne muscular dystrophy |
| TWI453207B (zh) | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基三唑并吡啶，其組合物及使用其之治療方法 |
| GB0821307D0 (en) | 2008-11-21 | 2008-12-31 | Summit Corp Plc | Compounds for treatment of duchenne muscular dystrophy |
| US8084620B2 (en) | 2008-12-19 | 2011-12-27 | Bristol-Myers Squibb Company | Carbazole carboxamide compounds useful as kinase inhibitors |
| EP2429987A4 (en) | 2009-05-15 | 2012-10-03 | Korea Res Inst Chem Tech | AMIDE COMPOUND, PROCESS FOR PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME |
| WO2010151747A1 (en) | 2009-06-26 | 2010-12-29 | Cystic Fibrosis Foundation Therapeutics, Inc. | Pyrimine compounds and methods of making and using same |
| WO2011008931A2 (en) | 2009-07-15 | 2011-01-20 | Cystic Fibrosis Foundation Therapeutics, Inc. | Arylpyrimidine compounds and combination therapy comprising same for treating cystic fibrosis & related disorders |
| KR101758046B1 (ko) | 2009-12-22 | 2017-07-14 | 버텍스 파마슈티칼스 인코포레이티드 | 포스파티딜이노시톨 3-키나제의 이소인돌리논 억제제 |
| AU2010336027A1 (en) | 2009-12-23 | 2012-07-19 | Auckland Uniservices Limited | Compounds, preparations and uses thereof |
| NZ601526A (en) | 2009-12-31 | 2014-07-25 | Piramal Entpr Ltd | Inhibitors of diacylglycerol acyl transferase |
| WO2012002527A1 (ja) | 2010-07-02 | 2012-01-05 | あすか製薬株式会社 | 複素環化合物及びｐ２７Ｋｉｐ１分解阻害剤 |
| PE20130774A1 (es) | 2010-07-29 | 2013-06-26 | Rigel Pharmaceuticals Inc | Compuestos heterociclicos activadores de ampk y metodos para emplearlos |
| US9938269B2 (en) | 2011-06-30 | 2018-04-10 | Abbvie Inc. | Inhibitor compounds of phosphodiesterase type 10A |
| DK2820009T3 (en) | 2012-03-01 | 2018-04-16 | Array Biopharma Inc | Serine / threonine kinase inhibitors |
| CN104583195B (zh) | 2012-09-12 | 2018-08-17 | 山东亨利医药科技有限责任公司 | 作为酪氨酸激酶抑制剂的含氮杂芳环衍生物 |
| US20150272939A1 (en) | 2012-10-02 | 2015-10-01 | Yale University | Identification of Small Molecule Inhibitors of Jumonji AT-Rich Interactive Domain 1A (JARID1A) and 1B (JARID1B) Histone Demethylase |
| AU2013337717B2 (en) | 2012-11-01 | 2018-10-25 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using PI3 kinase isoform modulators |
| MX2015009952A (es) | 2013-02-08 | 2015-10-05 | Celgene Avilomics Res Inc | Inhibidores de cinasas reguladas por señales extracelulares (erk) y sus usos. |
| US20140357636A1 (en) | 2013-02-21 | 2014-12-04 | Wayne Rothbaum | Treatment of Skeletal-Related Disorders |
| EA034866B1 (ru) | 2013-08-30 | 2020-03-31 | ПиТиСи ТЕРАПЬЮТИКС, ИНК. | Замещенные пиримидиновые ингибиторы bmi-1 |
| US20150087673A1 (en) | 2013-09-26 | 2015-03-26 | Rigel Pharmaceuticals, Inc. | Methods for using and biomarkers for ampk-activating compounds |
| WO2015108861A1 (en) * | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| CN110229142A (zh) | 2014-04-04 | 2019-09-13 | 希洛斯医药品股份有限公司 | 细胞周期蛋白依赖性激酶7(cdk7)的抑制剂 |
| WO2015157556A1 (en) | 2014-04-09 | 2015-10-15 | Kadmon Corporation, Llc | Treatment of gvhd |
| WO2016025649A1 (en) | 2014-08-13 | 2016-02-18 | Celgene Avilomics Research, Inc. | Combinations of an erk inhibitor and a dot1l inhibitor and related methods |
| TWI704151B (zh) | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
| WO2016162325A1 (en) | 2015-04-07 | 2016-10-13 | Astrazeneca Ab | Substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1 (2h)-one derivatives as kinase inhibitors |
| BR112017026159A2 (pt) | 2015-06-15 | 2018-08-14 | Asana Biosciences, Llc | inibidores heterocíclicos de erk1 e erk2 e seu uso no tratamento de câncer |
| HUE068392T2 (hu) | 2015-10-21 | 2024-12-28 | Otsuka Pharma Co Ltd | Benzolaktám vegyületek mint fehérje kináz gátlók |
| LT3374359T (lt) | 2015-11-09 | 2020-03-25 | Astrazeneca Ab | Dihidroimidazopirazinono deriniai, tinkami panaudoti vėžio gydymui |
| EP3492462B1 (en) | 2016-07-26 | 2023-08-30 | Shenzhen TargetRx, Inc. | Amino pyrimidine compound for inhibiting protein tyrosine kinase activity |
| GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
-
2017
- 2017-04-20 GB GBGB1706327.2A patent/GB201706327D0/en not_active Ceased
-
2018
- 2018-04-20 CA CA3059674A patent/CA3059674A1/en active Pending
- 2018-04-20 AU AU2018255935A patent/AU2018255935B2/en active Active
- 2018-04-20 ES ES18722731T patent/ES2994283T3/es active Active
- 2018-04-20 IL IL269803A patent/IL269803B/en unknown
- 2018-04-20 WO PCT/IB2018/052745 patent/WO2018193410A1/en not_active Ceased
- 2018-04-20 SG SG11201909189Q patent/SG11201909189QA/en unknown
- 2018-04-20 DK DK18722731.9T patent/DK3612524T3/da active
- 2018-04-20 KR KR1020197033128A patent/KR102652193B1/ko active Active
- 2018-04-20 CN CN201880024602.7A patent/CN110831939B/zh active Active
- 2018-04-20 MX MX2019012471A patent/MX2019012471A/es unknown
- 2018-04-20 MA MA052123A patent/MA52123A/fr unknown
- 2018-04-20 US US16/604,002 patent/US11142518B2/en active Active
- 2018-04-20 MY MYPI2019005656A patent/MY203722A/en unknown
- 2018-04-20 TW TW107113537A patent/TWI813566B/zh active
- 2018-04-20 JP JP2019555918A patent/JP7113846B2/ja active Active
- 2018-04-20 FI FIEP18722731.9T patent/FI3612524T3/fi active
- 2018-04-20 EP EP18722731.9A patent/EP3612524B1/en active Active
-
2019
- 2019-09-20 PH PH12019502154A patent/PH12019502154A1/en unknown
- 2019-10-03 SA SA519410253A patent/SA519410253B1/ar unknown
- 2019-11-12 ZA ZA2019/07484A patent/ZA201907484B/en unknown
-
2021
- 2021-09-01 US US17/464,166 patent/US12030873B2/en active Active
-
2024
- 2024-05-31 US US18/679,934 patent/US20250002481A1/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2020517598A5 (https=) | ||
| JP7519416B2 (ja) | Ｃ－ｋｉｔ阻害剤としてのアミノチアゾール化合物 | |
| TWI851542B (zh) | Ｓｈｐ２之八氫環戊烷并[c]吡咯別構抑制劑 | |
| KR102613409B1 (ko) | 항암제인 l-((4-(4-플루오로-2-메틸-lH-인돌-5-일옥시)-6-메톡시퀴놀린-7-일옥시)메틸)시클로프로판아민, 이의 결정형 및 이의 염의 제조방법 | |
| JP2024023295A (ja) | Ｓｈｐ２の活性を阻害するための化合物の製造方法 | |
| JP2023179513A (ja) | ケモカイン受容体調節剤及びその使用 | |
| JP6530313B2 (ja) | ヒストン脱メチル化酵素の阻害剤 | |
| JP7328323B2 (ja) | ＳＭＡＲＣＡ２／ＢＲＭ ＡＴＰａｓｅ阻害剤としての尿素化合物及び組成物 | |
| JP6903635B2 (ja) | 抗増殖活性を有するピペリジノベンゾジアゼピン化合物 | |
| JP2022520448A5 (https=) | ||
| JP2019525962A (ja) | ケモカイン受容体調節剤及びそれの使用 | |
| CN111132972A (zh) | 人sting的小分子调节剂 | |
| JP2016523973A5 (https=) | ||
| TWI690506B (zh) | 阻斷疾病之泛素化－蛋白酶體系統之胺萘醌化合物及醫藥組合物 | |
| FI3612524T3 (fi) | 6-pyrimidiini-isoindolijohdannainen erk1/2:n estäjänä | |
| JP2020506951A5 (https=) | ||
| CA2901022A1 (en) | Substituted pyridine compounds as inhibitors of histone demethylases | |
| JP2014513704A5 (https=) | ||
| TW202114985A (zh) | Ｅｐ拮抗劑 | |
| JP2017520538A5 (https=) | ||
| TW202515853A (zh) | 㗁唑化合物晶體 | |
| JP6976248B2 (ja) | （ｒ）−１−（４−（６−（２−（４−（３，３−ジフルオロシクロブトキシ）−６−メチルピリジン−２−イル）アセトアミド）ピリダジン−３−イル）−２−フルオロブチル）−ｎ−メチル−１ｈ−１，２，３−トリアゾール−４−カルボキサミドの塩形態および多形体 | |
| JP2009502921A5 (https=) | ||
| JP2018520167A (ja) | ＰＩ３Ｋ／ｍＴＯＲ阻害剤としての溶融キノリン化合物 | |
| RU2011101661A (ru) | Пиримидилсульфонамидное производное и его применение для лечения хемокин-опосредованных заболеваний |