JP2020535168A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2020535168A5 JP2020535168A5 JP2020517516A JP2020517516A JP2020535168A5 JP 2020535168 A5 JP2020535168 A5 JP 2020535168A5 JP 2020517516 A JP2020517516 A JP 2020517516A JP 2020517516 A JP2020517516 A JP 2020517516A JP 2020535168 A5 JP2020535168 A5 JP 2020535168A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- salt
- production method
- cancer
- salt according
- 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
- 150000003839 salts Chemical class 0.000 claims description 80
- -1 1-isobutyryl piperidine-4-yl Chemical group 0.000 claims description 64
- 238000004519 manufacturing process Methods 0.000 claims description 58
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 36
- 239000002904 solvent Substances 0.000 claims description 34
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims description 32
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 30
- 239000000243 solution Substances 0.000 claims description 30
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 28
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 25
- 239000002002 slurry Substances 0.000 claims description 16
- 150000001875 compounds Chemical class 0.000 claims description 14
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims description 10
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 10
- 239000011976 maleic acid Substances 0.000 claims description 10
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 10
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 10
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims description 8
- 238000010438 heat treatment Methods 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- 238000003756 stirring Methods 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 6
- WVPZJYCGPGSZHW-UHFFFAOYSA-N 2,4-dioxo-3-phenyl-1-propan-2-ylpyrimidine-5-carboxamide Chemical group C(C)(C)N1C(N(C(C(=C1)C(=O)N)=O)C1=CC=CC=C1)=O WVPZJYCGPGSZHW-UHFFFAOYSA-N 0.000 claims description 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010025323 Lymphomas Diseases 0.000 claims description 4
- 208000034578 Multiple myelomas Diseases 0.000 claims description 4
- 108091000080 Phosphotransferase Proteins 0.000 claims description 4
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 4
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 4
- 239000007864 aqueous solution Substances 0.000 claims description 4
- 239000000706 filtrate Substances 0.000 claims description 4
- 238000001914 filtration Methods 0.000 claims description 4
- 206010017758 gastric cancer Diseases 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 102000020233 phosphotransferase Human genes 0.000 claims description 4
- 201000011549 stomach cancer Diseases 0.000 claims description 4
- 239000000126 substance Substances 0.000 claims description 4
- 238000001757 thermogravimetry curve Methods 0.000 claims description 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 208000009746 Adult T-Cell Leukemia-Lymphoma Diseases 0.000 claims description 2
- 208000016683 Adult T-cell leukemia/lymphoma Diseases 0.000 claims description 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 208000017604 Hodgkin disease Diseases 0.000 claims description 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims description 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims description 2
- 206010052178 Lymphocytic lymphoma Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims description 2
- 201000006966 adult T-cell leukemia Diseases 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 230000001684 chronic effect Effects 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 238000001035 drying Methods 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 201000010536 head and neck cancer Diseases 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 201000000564 macroglobulinemia Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims description 2
- 239000000741 silica gel Substances 0.000 claims description 2
- 229910002027 silica gel Inorganic materials 0.000 claims description 2
- 201000000849 skin cancer Diseases 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 5
- 238000001816 cooling Methods 0.000 claims 1
- 210000002768 hair cell Anatomy 0.000 claims 1
- 230000001376 precipitating effect Effects 0.000 claims 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 description 2
- 108060006633 protein kinase Proteins 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024014546A JP7639195B2 (ja) | 2017-09-27 | 2024-02-02 | Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩 |
| JP2025025024A JP2025093936A (ja) | 2017-09-27 | 2025-02-19 | Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762564070P | 2017-09-27 | 2017-09-27 | |
| US62/564,070 | 2017-09-27 | ||
| US201862714196P | 2018-08-03 | 2018-08-03 | |
| US62/714,196 | 2018-08-03 | ||
| PCT/US2018/052925 WO2019067594A1 (en) | 2017-09-27 | 2018-09-26 | Salts of pyrrolotriazine derivatives useful as tam inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024014546A Division JP7639195B2 (ja) | 2017-09-27 | 2024-02-02 | Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020535168A JP2020535168A (ja) | 2020-12-03 |
| JP2020535168A5 true JP2020535168A5 (enExample) | 2021-10-28 |
| JP7504791B2 JP7504791B2 (ja) | 2024-06-24 |
Family
ID=63794769
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020517516A Active JP7504791B2 (ja) | 2017-09-27 | 2018-09-26 | Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩 |
| JP2024014546A Active JP7639195B2 (ja) | 2017-09-27 | 2024-02-02 | Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩 |
| JP2025025024A Ceased JP2025093936A (ja) | 2017-09-27 | 2025-02-19 | Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024014546A Active JP7639195B2 (ja) | 2017-09-27 | 2024-02-02 | Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩 |
| JP2025025024A Ceased JP2025093936A (ja) | 2017-09-27 | 2025-02-19 | Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩 |
Country Status (34)
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017035366A1 (en) | 2015-08-26 | 2017-03-02 | Incyte Corporation | Pyrrolopyrimidine derivatives as tam inhibitors |
| ES2821010T3 (es) | 2015-12-09 | 2021-04-23 | Cadent Therapeutics Inc | Moduladores heteroaromáticos del receptor NMDA y usos de los mismos |
| TWI828027B (zh) | 2016-03-28 | 2024-01-01 | 美商英塞特公司 | 作為tam抑制劑之吡咯并三嗪化合物 |
| AU2017382339B2 (en) | 2016-12-22 | 2024-02-15 | Novartis Ag | NMDA receptor modulators and uses thereof |
| US10633387B2 (en) | 2017-09-27 | 2020-04-28 | Incyte Corporation | Salts of TAM inhibitors |
| ES3031110T3 (en) * | 2018-06-29 | 2025-07-04 | Incyte Corp | Formulations of an axl/mer inhibitor |
| PT3830092T (pt) | 2018-08-03 | 2023-07-25 | Novartis Ag | Moduladores do recetor nmda heteroaromáticos e suas utilizações |
| CR20250050A (es) | 2018-09-05 | 2025-03-19 | Incyte Corp | Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165) |
| PH12022552347A1 (en) * | 2020-03-06 | 2024-01-29 | Incyte Corp | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| US12534479B2 (en) | 2020-07-10 | 2026-01-27 | Findcure Biosciences (Zhongshan) Co., Ltd. | Triazine compound and composition and use thereof |
| CN115028648B (zh) * | 2021-03-03 | 2024-08-30 | 武汉誉祥医药科技有限公司 | 三并环化合物及其药物组合物和应用 |
| WO2023286719A1 (ja) * | 2021-07-13 | 2023-01-19 | 日本曹達株式会社 | ウラシル化合物の製造方法 |
Family Cites Families (137)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4399216A (en) | 1980-02-25 | 1983-08-16 | The Trustees Of Columbia University | Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials |
| US5179017A (en) | 1980-02-25 | 1993-01-12 | The Trustees Of Columbia University In The City Of New York | Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials |
| US4634665A (en) | 1980-02-25 | 1987-01-06 | The Trustees Of Columbia University In The City Of New York | Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials |
| US5156840A (en) | 1982-03-09 | 1992-10-20 | Cytogen Corporation | Amine-containing porphyrin derivatives |
| US5057313A (en) | 1986-02-25 | 1991-10-15 | The Center For Molecular Medicine And Immunology | Diagnostic and therapeutic antibody conjugates |
| JP3101690B2 (ja) | 1987-03-18 | 2000-10-23 | エス・ビィ・２・インコーポレイテッド | 変性抗体の、または変性抗体に関する改良 |
| IL162181A (en) | 1988-12-28 | 2006-04-10 | Pdl Biopharma Inc | A method of producing humanized immunoglubulin, and polynucleotides encoding the same |
| US5530101A (en) | 1988-12-28 | 1996-06-25 | Protein Design Labs, Inc. | Humanized immunoglobulins |
| DE3920358A1 (de) | 1989-06-22 | 1991-01-17 | Behringwerke Ag | Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung |
| JPH0395163A (ja) | 1989-09-08 | 1991-04-19 | Daicel Chem Ind Ltd | ２．２．４．４．６―ペンタメチル―２．３．４．５―テトラヒドロピリミジンの製造法 |
| US5859205A (en) | 1989-12-21 | 1999-01-12 | Celltech Limited | Humanised antibodies |
| EP0590058B1 (en) | 1991-06-14 | 2003-11-26 | Genentech, Inc. | HUMANIZED Heregulin ANTIBODy |
| DE69233528T2 (de) | 1991-11-25 | 2006-03-16 | Enzon, Inc. | Verfahren zur Herstellung von multivalenten antigenbindenden Proteinen |
| US5714350A (en) | 1992-03-09 | 1998-02-03 | Protein Design Labs, Inc. | Increasing antibody affinity by altering glycosylation in the immunoglobulin variable region |
| US5827690A (en) | 1993-12-20 | 1998-10-27 | Genzyme Transgenics Corporatiion | Transgenic production of antibodies in milk |
| US5731168A (en) | 1995-03-01 | 1998-03-24 | Genentech, Inc. | Method for making heteromultimeric polypeptides |
| US5869046A (en) | 1995-04-14 | 1999-02-09 | Genentech, Inc. | Altered polypeptides with increased half-life |
| EP0859841B1 (en) | 1995-08-18 | 2002-06-19 | MorphoSys AG | Protein/(poly)peptide libraries |
| US20020077461A1 (en) | 1996-04-24 | 2002-06-20 | Soren Bjorn | Pharmaceutical formulation |
| HK1053831A1 (zh) | 1999-09-17 | 2003-11-07 | Basf Aktiengesellschaft | 作为治疗药物的激酶抑制剂 |
| EP1294358B1 (en) | 2000-06-28 | 2004-08-18 | Smithkline Beecham Plc | Wet milling process |
| ATE406892T1 (de) | 2001-04-06 | 2008-09-15 | Wyeth Corp | Antineoplastische kombinationspräparate enthaltend cci-779 (rapamycin derivat) zusammen mit gemcitabin oder fluoro-uracil |
| GB0221697D0 (en) | 2002-09-18 | 2002-10-30 | Unilever Plc | Novel compouds and their uses |
| AU2003272175A1 (en) | 2002-10-21 | 2004-05-04 | Aprea Ab | Reactivation of wild type p53 in human tumour cells by a low molecular weight compound |
| US7355008B2 (en) | 2003-01-09 | 2008-04-08 | Macrogenics, Inc. | Identification and engineering of antibodies with variant Fc regions and methods of using same |
| AU2004205631A1 (en) | 2003-01-16 | 2004-08-05 | Genentech, Inc. | Synthetic antibody phage libraries |
| WO2004072266A2 (en) | 2003-02-13 | 2004-08-26 | Kalobios Inc. | Antibody affinity engineering by serial epitope-guided complementarity replacement |
| DE602004014747D1 (de) | 2003-03-26 | 2008-08-14 | Egalet As | Matrixzubereitungen für die kontrollierte darreichung von arzneistoffen |
| DK1639014T3 (da) | 2003-06-13 | 2011-01-17 | Biogen Idec Inc | Aglycosyl-anti-CD154 (CD40-ligand)-antistoffer og anvendelser deraf |
| AU2004266159A1 (en) | 2003-08-22 | 2005-03-03 | Biogen Idec Ma Inc. | Improved antibodies having altered effector function and methods for making the same |
| WO2005025515A2 (en) | 2003-09-12 | 2005-03-24 | California Institute Of Technology | Proteasome pathway inhibitors and related methods |
| MXPA06011423A (es) | 2004-04-02 | 2007-01-23 | Osi Pharm Inc | Inhibidores de proteina cinasa heterobiciclica sustituida en el anillo 6,6-biciclico. |
| UY28931A1 (es) | 2004-06-03 | 2005-12-30 | Bayer Pharmaceuticals Corp | Derivados de pirrolotriazina utiles para tratar trastornos hiper-proliferativos y enfermedades asociadas con angiogenesis |
| MY139689A (en) | 2004-07-20 | 2009-10-30 | Osi Pharm Inc | Imidazotriazines as protein kinase inhibitors |
| UY29177A1 (es) | 2004-10-25 | 2006-05-31 | Astex Therapeutics Ltd | Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos |
| RU2007123675A (ru) | 2004-11-24 | 2008-12-27 | Новартис АГ (CH) | Комбинации ингибиторов jak |
| CA2630271C (en) | 2005-11-17 | 2014-04-08 | Osi Pharmaceuticals, Inc. | Fused bicyclic mtor inhibitors |
| BRPI0619146A2 (pt) | 2005-12-02 | 2011-09-13 | Bayer Pharmaceuticals Corp | derivados de 4-amino-pirroltriazina substituìda úteis no tratamento de disordens e doenças hiperproliferativas associadas com angiogênesis |
| PE20070855A1 (es) | 2005-12-02 | 2007-10-14 | Bayer Pharmaceuticals Corp | Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas |
| HUE028588T2 (hu) | 2005-12-13 | 2016-12-28 | Incyte Holdings Corp | Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok |
| EP1960372B1 (en) | 2005-12-15 | 2015-12-09 | Rigel Pharmaceuticals, Inc. | Kinase inhibitors and their uses |
| EP2010542B1 (en) | 2006-04-12 | 2012-01-25 | Vertex Pharmaceuticals Incorporated | 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridines as plk1 protein kinase inhibitors for the treatment of proliferative disorders |
| KR101464385B1 (ko) | 2006-04-19 | 2014-11-21 | 노파르티스 아게 | ６-ｏ-치환된 벤즈옥사졸 및 벤조티아졸 화합물, 및 ｃｓｆ-１ｒ 신호전달의 억제 방법 |
| US20090253718A1 (en) | 2006-04-25 | 2009-10-08 | Astex Therapeutics Limited | Pharmaceutical Compounds |
| EP2023926B1 (en) | 2006-05-19 | 2011-10-12 | Bayer Pharma Aktiengesellschaft | Pyridonecarboxamide derivatives useful in treating hyper-proliferative and angiogenesis disorders |
| US8097630B2 (en) | 2006-10-10 | 2012-01-17 | Rigel Pharmaceuticals, Inc. | Pinane-substituted pyrimidinediamine derivatives useful as Axl inhibitors |
| GEP20125658B (en) | 2006-11-22 | 2012-10-10 | Incyte Corp | Imidazotriazines and imidazo pyrimidines as kinase inhibitors |
| US8129387B2 (en) | 2006-12-14 | 2012-03-06 | Vertex Pharmaceuticals Incorporated | Substituted 5,6-dihydroimidazo[1,5-F]pteridines useful as protein kinase inhibitors |
| RS53281B (sr) | 2006-12-29 | 2014-08-29 | Rigel Pharmaceuticals Inc. | Policiklični heteroaril supstituisani triazoli koji su korisni kao axl inhibitori |
| ES2406930T3 (es) | 2006-12-29 | 2013-06-10 | Rigel Pharmaceuticals, Inc. | Triazoles sustituidos con arilo bicíclico y heteroarilo bicíclico útiles como inhibidores de AXL |
| CN101622248B (zh) | 2006-12-29 | 2013-04-17 | 里格尔制药公司 | 用作axl抑制剂的n3-杂芳基取代的三唑和n5-杂芳基取代的三唑 |
| EP2114983B8 (en) | 2007-02-07 | 2015-02-18 | The Regents of the University of Colorado, A Body Corporate | Axl tyrosine kinase inhibitors and methods of making and using the same |
| AU2008288105A1 (en) | 2007-03-29 | 2009-02-19 | Panacea Biotec Limited. | Modified dosage forms of tacrolimus |
| MX2009013565A (es) | 2007-06-12 | 2010-06-02 | Concert Pharmaceuticals Inc | Derivados de azapeptidos. |
| AU2008287339A1 (en) | 2007-08-15 | 2009-02-19 | Vertex Pharmaceuticals Incorporated | 4-(9-(3, 3-difluorocyclopentyl) -5, 7, 7-trimethyl-6-oxo-6, 7, 8, 9-tetrahydro-5H-pyrimido [4, 5-b][1, 4] diazepin-2-ylamino)-3-methoxybenzamide Derivatives as Inhibitors of the Human Protein Kinases PLK1 to PLK4 for the Treatment of Proliferative Diseases |
| GB0719803D0 (en) | 2007-10-10 | 2007-11-21 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| EP2215085B1 (en) | 2007-10-25 | 2011-09-07 | AstraZeneca AB | Pyridine and pyrazine derivatives useful in the treatment of cell proliferative disorders |
| CA2704052C (en) | 2007-10-26 | 2015-04-21 | Rigel Pharmaceuticals, Inc. | Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| AU2008343932B2 (en) | 2007-12-19 | 2013-08-15 | Amgen Inc. | Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors |
| AR070127A1 (es) | 2008-01-11 | 2010-03-17 | Novartis Ag | Pirrolo - pirimidinas y pirrolo -piridinas |
| JP5746015B2 (ja) | 2008-04-16 | 2015-07-08 | マックス プランク ゲゼルシャフト ツゥアー フェデルゥン デル ヴィッセンシャフテン エー フォー | Ａｘｌキナーゼ阻害剤としてのキノリン誘導体 |
| TWI539953B (zh) | 2008-04-28 | 2016-07-01 | 瑞波若斯治療學公司 | 用於治療乳癌之組成物和方法 |
| CA2728729C (en) | 2008-06-23 | 2016-09-27 | Vertex Pharmaceuticals Incorporated | Protein kinase inhibitors |
| CA2730231C (en) | 2008-07-09 | 2016-10-18 | Rigel Pharmaceuticals, Inc. | Polycyclic heteroaryl substituted triazoles useful as axl inhibitors |
| CA2730251C (en) | 2008-07-09 | 2016-08-09 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| WO2010014755A1 (en) | 2008-07-29 | 2010-02-04 | The Regents Of The University Of Colorado | Methods and compounds for enhancing anti-cancer therapy |
| EP2158913A1 (en) | 2008-08-25 | 2010-03-03 | Ratiopharm GmbH | Pharmaceutical composition comprising N-[3-chhloro-4-[(3-fluorophenyl)methoxy]phenyl]6-(5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine |
| WO2010025073A1 (en) | 2008-08-28 | 2010-03-04 | Takeda Pharmaceutical Company Limited | Dihydroimidazo [ 1, 5-f] pteridines as polo-like kinase inhibitors |
| WO2010071885A1 (en) | 2008-12-19 | 2010-06-24 | Cephalon, Inc. | Pyrrolotriazines as alk and jak2 inhibitors |
| SG172857A1 (en) | 2009-02-09 | 2011-08-29 | Supergen Inc | Pyrrolopyrimidinyl axl kinase inhibitors |
| US8765754B2 (en) | 2009-04-29 | 2014-07-01 | Locus Pharmaceuticals, Inc. | Pyrrolotriazine compounds |
| NZ596479A (en) | 2009-05-22 | 2014-01-31 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| EP2448938B9 (en) | 2009-06-29 | 2015-06-10 | Incyte Corporation | Pyrimidinones as pi3k inhibitors |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| SG179207A1 (en) | 2009-09-25 | 2012-04-27 | Vertex Pharma | Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors |
| EP2311809A1 (en) | 2009-10-16 | 2011-04-20 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Quinolinyloxyphenylsulfonamides |
| US8604217B2 (en) | 2009-11-12 | 2013-12-10 | Selvita S.A. | Compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent |
| WO2011075630A1 (en) | 2009-12-18 | 2011-06-23 | Incyte Corporation | Substituted fused aryl and heteroaryl derivatives as pi3k inhibitors |
| CA2792508C (en) | 2010-03-10 | 2018-01-16 | Incyte Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| EP2552922A1 (en) | 2010-03-31 | 2013-02-06 | Bristol-Myers Squibb Company | Substituted pyrrolotriazines as protein kinase inhibitors |
| AU2010352577A1 (en) | 2010-05-05 | 2012-01-19 | Vertex Pharmaceuticals Incorporated | 4 substituted pyrazolopyrimidines useful as PKC-theta inhibitors |
| EP2571361A4 (en) | 2010-05-19 | 2013-11-13 | Univ North Carolina | PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| EP2423208A1 (en) | 2010-08-28 | 2012-02-29 | Lead Discovery Center GmbH | Pharmaceutically active compounds as Axl inhibitors |
| BR112013008526A2 (pt) | 2010-10-08 | 2016-07-12 | Elan Pharm Inc | inibidores de quinase do tipo polo |
| ITRM20100537A1 (it) | 2010-10-12 | 2012-04-12 | Consiglio Nazionale Ricerche | Aptamero inibitore del recettore tirosina chinasi axl per uso in terapia |
| ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| JP5961187B2 (ja) | 2010-12-20 | 2016-08-02 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉ３ｋ阻害剤としてのｎ−（１−（置換フェニル）エチル）−９ｈ−プリン−６−アミン |
| MX352844B (es) | 2011-02-28 | 2017-12-11 | Calitor Sciences Llc | Compuestos de quinolina sustituidos y metodos de uso. |
| KR101606250B1 (ko) | 2011-03-23 | 2016-03-24 | 암젠 인크 | Cdk 4/6 및 flt3의 융합된 트리사이클릭 이중 저해제 |
| EP3628665B1 (en) | 2011-04-01 | 2022-11-02 | University of Utah Research Foundation | Substituted n-phenylpyrimidin-2-amine analogs as inhibitors of the axl kinase |
| AR086913A1 (es) | 2011-06-14 | 2014-01-29 | Novartis Ag | 4-metil-3-[[4-(3-piridinil)-2-pirimidinil]-amino]-n-[5-(4-metil-1h-imidazol-1-il)-3-(trifluoro-metil)-fenil]-benzamida amorfa, forma de dosificacion que la contiene y metodo para prepararlas |
| US8691807B2 (en) | 2011-06-20 | 2014-04-08 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
| WO2013004551A1 (en) | 2011-07-01 | 2013-01-10 | Bayer Intellectual Property Gmbh | Hydroxymethylaryl-substituted pyrrolotriazines as alk1 inhibitors |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| MX389479B (es) | 2011-09-02 | 2025-03-20 | Incyte Holdings Corp | Heterociclilaminas como inhibidores de fosfoinositida 3-cinasas (pi3k) |
| EP2758052B9 (en) | 2011-09-18 | 2019-03-27 | Euro-Celtique S.A. | Pharmaceutical composition comprising an HDAC inhibitor and a cyclopolysaccharide |
| CN102408411B (zh) | 2011-09-19 | 2014-10-22 | 北京康辰药业股份有限公司 | 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用 |
| BR112014007788A2 (pt) | 2011-10-03 | 2017-04-18 | Univ North Carolina Chapel Hill | compostos de pirrolopirimidina para tratamento do câncer |
| EA023521B1 (ru) | 2011-11-14 | 2016-06-30 | Сефалон, Инк. | ПРОИЗВОДНЫЕ УРАЦИЛА В КАЧЕСТВЕ ИНГИБИТОРОВ AXL И c-MET КИНАЗЫ |
| RS54738B1 (sr) | 2011-11-29 | 2016-10-31 | Perosphere Inc | Agensi koji vrše reverziju antikoagulanta |
| EP2788000B1 (en) | 2011-12-06 | 2018-05-30 | Merck Sharp & Dohme Corp. | Pyrrolopyrimidines as janus kinase inhibitors |
| UY34484A (es) | 2011-12-15 | 2013-07-31 | Bayer Ip Gmbh | Benzotienilo-pirrolotriazinas disustituidas y sus usos |
| SG11201404505PA (en) | 2012-01-31 | 2014-10-30 | Daiichi Sankyo Co Ltd | Pyridone derivative |
| CA2865021C (en) | 2012-02-23 | 2020-06-30 | Bayer Intellectual Property Gmbh | Substituted benzothienyl-pyrrolotriazines and uses thereof |
| WO2013162061A1 (ja) | 2012-04-26 | 2013-10-31 | 第一三共株式会社 | 二環性ピリミジン化合物 |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| JP6318156B2 (ja) | 2012-09-06 | 2018-04-25 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | キナーゼをモジュレートするための化合物および方法、ならびにその指標 |
| CA2886240A1 (en) | 2012-09-26 | 2014-04-03 | The Regents Of The University Of California | Modulation of ire1 |
| WO2014062774A1 (en) | 2012-10-17 | 2014-04-24 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
| CA2888816A1 (en) | 2012-11-01 | 2014-05-08 | Incyte Corporation | Tricyclic fused thiophene derivatives as jak inhibitors |
| US9925193B2 (en) | 2012-11-20 | 2018-03-27 | Proqinase Gmbh | Thioether derivatives as protein kinase inhibitors |
| US20150353542A1 (en) | 2013-01-14 | 2015-12-10 | Amgen Inc. | Methods of using cell-cycle inhibitors to modulate one or more properties of a cell culture |
| TW201522337A (zh) | 2013-03-12 | 2015-06-16 | Arqule Inc | 經取代之三環吡唑並－嘧啶化合物類 |
| TWI649308B (zh) | 2013-07-24 | 2019-02-01 | 小野藥品工業股份有限公司 | 喹啉衍生物 |
| EP3067356B1 (en) | 2013-11-08 | 2018-07-04 | ONO Pharmaceutical Co., Ltd. | Pyrrolo pyrimidine derivative |
| WO2015081783A1 (zh) | 2013-12-06 | 2015-06-11 | 江苏奥赛康药业股份有限公司 | 吡咯并[2,1-f][1,2,4]三嗪类衍生物及其制备方法和用途 |
| SG11201605417QA (en) | 2014-02-03 | 2016-08-30 | Cadila Healthcare Ltd | Heterocyclic compounds |
| GB201420285D0 (en) | 2014-11-14 | 2014-12-31 | Bergenbio As | Process |
| WO2016097918A1 (en) | 2014-12-18 | 2016-06-23 | Pfizer Inc. | Pyrimidine and triazine derivatives and their use as axl inhibitors |
| US9840503B2 (en) | 2015-05-11 | 2017-12-12 | Incyte Corporation | Heterocyclic compounds and uses thereof |
| PE20231958A1 (es) | 2015-07-30 | 2023-12-06 | Macrogenics Inc | Moleculas de union a pd-1 y metodos de uso de las mismas |
| WO2017027717A1 (en) * | 2015-08-12 | 2017-02-16 | Incyte Corporation | Bicyclic fused pyrimidine compounds as tam inhibitors |
| WO2017035366A1 (en) | 2015-08-26 | 2017-03-02 | Incyte Corporation | Pyrrolopyrimidine derivatives as tam inhibitors |
| WO2017062797A1 (en) | 2015-10-07 | 2017-04-13 | The University Of North Carolina At Chapel Hill | The methods for treatment of tumors |
| KR102073779B1 (ko) | 2015-10-13 | 2020-02-05 | 니혼노야쿠가부시키가이샤 | 옥심기를 가지는 축합복소환 화합물 또는 그의 염류 및 상기 화합물을 함유하는 농원예용 살충제 및 그 사용 방법 |
| WO2017083789A1 (en) | 2015-11-14 | 2017-05-18 | Sunshine Lake Pharma Co., Ltd. | Crystalline form of a substituted quinoline compound and pharmaceutical compositions thereof |
| US9920033B2 (en) | 2015-11-14 | 2018-03-20 | Calitor Sciences, Llc | Crystalline form of a substituted quinoline compound and pharmaceutical compositions thereof |
| TWI828027B (zh) | 2016-03-28 | 2024-01-01 | 美商英塞特公司 | 作為tam抑制劑之吡咯并三嗪化合物 |
| CA3021678A1 (en) | 2016-04-22 | 2017-10-26 | Incyte Corporation | Formulations of an lsd1 inhibitor |
| TW201803871A (zh) * | 2016-06-24 | 2018-02-01 | 英塞特公司 | 作為ＰＩ３Ｋ-γ抑制劑之雜環化合物 |
| JOP20170153A1 (ar) | 2016-07-15 | 2019-01-30 | Lilly Co Eli | نظائر urocortin-2 جديدة معدلة بحمض دهني لعلاج داء السكري وأمراض الكلى المزمنة |
| PL3484524T3 (pl) | 2016-07-15 | 2023-03-20 | Ionis Pharmaceuticals, Inc. | Związki i sposoby modulacji smn2 |
| JOP20190257A1 (ar) | 2017-04-28 | 2019-10-28 | Novartis Ag | مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats |
| US10633387B2 (en) * | 2017-09-27 | 2020-04-28 | Incyte Corporation | Salts of TAM inhibitors |
| ES3031110T3 (en) * | 2018-06-29 | 2025-07-04 | Incyte Corp | Formulations of an axl/mer inhibitor |
| PH12022552347A1 (en) | 2020-03-06 | 2024-01-29 | Incyte Corp | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
-
2018
- 2018-09-26 US US16/142,514 patent/US10633387B2/en active Active
- 2018-09-26 HU HUE18783341A patent/HUE057190T2/hu unknown
- 2018-09-26 KR KR1020207012225A patent/KR102739325B1/ko active Active
- 2018-09-26 CR CR20200179A patent/CR20200179A/es unknown
- 2018-09-26 EP EP21196789.8A patent/EP3988552A1/en active Pending
- 2018-09-26 MX MX2020003375A patent/MX2020003375A/es unknown
- 2018-09-26 PL PL18783341T patent/PL3687996T3/pl unknown
- 2018-09-26 JP JP2020517516A patent/JP7504791B2/ja active Active
- 2018-09-26 MY MYPI2020001589A patent/MY208007A/en unknown
- 2018-09-26 ES ES18783341T patent/ES2904458T3/es active Active
- 2018-09-26 PT PT187833413T patent/PT3687996T/pt unknown
- 2018-09-26 SM SM20220011T patent/SMT202200011T1/it unknown
- 2018-09-26 CA CA3077308A patent/CA3077308A1/en active Pending
- 2018-09-26 SG SG11202002821UA patent/SG11202002821UA/en unknown
- 2018-09-26 RS RS20220048A patent/RS62872B1/sr unknown
- 2018-09-26 MA MA50655A patent/MA50655B1/fr unknown
- 2018-09-26 CN CN202410706110.3A patent/CN118930549A/zh active Pending
- 2018-09-26 PE PE2020000404A patent/PE20210002A1/es unknown
- 2018-09-26 MD MDE20200803T patent/MD3687996T2/ro unknown
- 2018-09-26 CN CN201880073539.6A patent/CN111386273B/zh active Active
- 2018-09-26 DK DK18783341.3T patent/DK3687996T3/da active
- 2018-09-26 IL IL273579A patent/IL273579B2/en unknown
- 2018-09-26 WO PCT/US2018/052925 patent/WO2019067594A1/en not_active Ceased
- 2018-09-26 GE GEAP202215322A patent/GEAP202215322A/en unknown
- 2018-09-26 EP EP18783341.3A patent/EP3687996B1/en active Active
- 2018-09-26 LT LTEPPCT/US2018/052925T patent/LT3687996T/lt unknown
- 2018-09-26 GE GEAP201815322A patent/GEP20227429B/en unknown
- 2018-09-26 AU AU2018342471A patent/AU2018342471B2/en active Active
- 2018-09-26 TW TW107133765A patent/TWI821200B/zh active
- 2018-09-26 SI SI201830551T patent/SI3687996T1/sl unknown
-
2020
- 2020-03-19 US US16/823,751 patent/US11104682B2/en active Active
- 2020-03-26 PH PH12020550143A patent/PH12020550143A1/en unknown
- 2020-03-26 CL CL2020000791A patent/CL2020000791A1/es unknown
- 2020-03-27 SA SA520411638A patent/SA520411638B1/ar unknown
- 2020-04-08 EC ECSENADI202021655A patent/ECSP20021655A/es unknown
- 2020-04-23 CO CONC2020/0005009A patent/CO2020005009A2/es unknown
- 2020-04-30 JO JOJO/P/2020/0081A patent/JOP20200081B1/ar active
-
2021
- 2021-08-13 US US17/401,570 patent/US12187730B2/en active Active
-
2022
- 2022-01-17 CY CY20221100036T patent/CY1124952T1/el unknown
- 2022-04-21 CL CL2022001014A patent/CL2022001014A1/es unknown
-
2023
- 2023-11-20 AU AU2023270198A patent/AU2023270198B2/en active Active
-
2024
- 2024-02-02 JP JP2024014546A patent/JP7639195B2/ja active Active
- 2024-11-26 US US18/960,485 patent/US20250188086A1/en active Pending
-
2025
- 2025-02-19 JP JP2025025024A patent/JP2025093936A/ja not_active Ceased
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2013203283B2 (en) | Processes for the preparation of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethylamine | |
| JP2010526056A (ja) | イマチニブの製造方法 | |
| JP2007521340A5 (enExample) | ||
| BR122021022703B1 (pt) | Processos para preparação de dimetilamida do ácido 7-ciclopentil-2-(5-piperazin-1-ilpiridin-2-ilamo)-7h-pirrol [2,3-d]pirimidino-6-carboxílico e seus sais, e de seus intermediários | |
| CA2971872A1 (en) | Mutant idh1 inhibitors useful for treating cancer | |
| JP2014524476A5 (enExample) | ||
| JP2010539237A5 (enExample) | ||
| JP7749857B2 (ja) | キナゾリン化合物を合成するための方法 | |
| KR20160095161A (ko) | 포스파티딜이노시톨 3-키나제 억제제의 가공 방법 | |
| KR20150072408A (ko) | 5-(2,6-디-4-모르폴리닐-4-피리미디닐)-4-트리플루오로메틸피리딘-2-아민의 개선된 제조 방법 | |
| JP2018532713A5 (enExample) | ||
| CN105408321A (zh) | 新的吲哚和吡咯衍生物、它们的制备方法和含有它们的药物组合物 | |
| WO2018191815A1 (en) | Processes for the preparation of acalabrutinib and intermediates thereof | |
| AU2024201119A1 (en) | Methods of preparing cytotoxic benzodiazepine derivatives | |
| CN121925420A (zh) | 作为tnf活性的调节剂的桥联五环咪唑衍生物的制备、中间体及其制备 | |
| WO2014024950A1 (ja) | １，４－ベンゾオキサジン化合物の製法 | |
| CN112955449B (zh) | 制备bet溴结构域抑制剂的固体形式的方法 | |
| CN101921260B (zh) | 一种伊马替尼的制备方法 | |
| TWI833800B (zh) | 用於製造3-[(1S)-1-咪唑并[1,2-a]吡啶-6-基乙基]-5-(1-甲基吡唑-4-基)三唑并[4,5-b]吡嗪的改進方法及其多晶型形式 | |
| KR20130056887A (ko) | 시클로펜타퀴나졸린의 합성 | |
| WO2016139773A1 (ja) | シロドシン合成中間体の新規合成方法 | |
| EP3773584A1 (en) | Methods for preparing substituted pyridinone-containing tricyclic compounds | |
| KR20240125858A (ko) | 신규 화합물 및 이를 포함하는 약학 조성물 | |
| TH2001001805A (th) | เกลือของอนุพันธ์ไพร์โรโลไตรอะซินที่ใช้ประโยชน์เป็นสารยับยั้ง tam | |
| AU2020278162A1 (en) | Processes and intermediates for preparing a BTK inhibitor |