JP2019524660A5 - - Google Patents
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- JP2019524660A5 JP2019524660A5 JP2018566525A JP2018566525A JP2019524660A5 JP 2019524660 A5 JP2019524660 A5 JP 2019524660A5 JP 2018566525 A JP2018566525 A JP 2018566525A JP 2018566525 A JP2018566525 A JP 2018566525A JP 2019524660 A5 JP2019524660 A5 JP 2019524660A5
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- Prior art keywords
- compound
- cancer
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- solid form
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- Prior art date
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- 238000000034 method Methods 0.000 claims 31
- 229940125904 compound 1 Drugs 0.000 claims 26
- 239000007787 solid Substances 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 20
- 239000003814 drug Substances 0.000 claims 15
- 239000002904 solvent Substances 0.000 claims 13
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims 9
- 239000002585 base Substances 0.000 claims 9
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 7
- 239000003054 catalyst Substances 0.000 claims 7
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 238000006243 chemical reaction Methods 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 229910052723 transition metal Inorganic materials 0.000 claims 5
- 150000003624 transition metals Chemical class 0.000 claims 5
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims 4
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 4
- IPWKHHSGDUIRAH-UHFFFAOYSA-N bis(pinacolato)diboron Chemical compound O1C(C)(C)C(C)(C)OB1B1OC(C)(C)C(C)(C)O1 IPWKHHSGDUIRAH-UHFFFAOYSA-N 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 230000002062 proliferating effect Effects 0.000 claims 4
- 238000001816 cooling Methods 0.000 claims 3
- 238000010438 heat treatment Methods 0.000 claims 3
- 238000002360 preparation method Methods 0.000 claims 3
- GLGNXYJARSMNGJ-VKTIVEEGSA-N (1s,2s,3r,4r)-3-[[5-chloro-2-[(1-ethyl-6-methoxy-2-oxo-4,5-dihydro-3h-1-benzazepin-7-yl)amino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide Chemical compound CCN1C(=O)CCCC2=C(OC)C(NC=3N=C(C(=CN=3)Cl)N[C@H]3[C@H]([C@@]4([H])C[C@@]3(C=C4)[H])C(N)=O)=CC=C21 GLGNXYJARSMNGJ-VKTIVEEGSA-N 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 229910052783 alkali metal Inorganic materials 0.000 claims 2
- -1 alkali metal bicarbonate Chemical class 0.000 claims 2
- 208000037979 autoimmune inflammatory disease Diseases 0.000 claims 2
- 229940125758 compound 15 Drugs 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229910052763 palladium Inorganic materials 0.000 claims 2
- 230000001376 precipitating effect Effects 0.000 claims 2
- 238000001556 precipitation Methods 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
- 238000001757 thermogravimetry curve Methods 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- LIDBMZYKSAXTQG-UHFFFAOYSA-N 3-[4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yl]oxy-N-(2-sulfamoylethyl)benzamide Chemical compound NCC1=CC(=NC(=C1)C(F)(F)F)OC=1C=C(C(=O)NCCS(N)(=O)=O)C=CC=1 LIDBMZYKSAXTQG-UHFFFAOYSA-N 0.000 claims 1
- ISXSUKUXUPLGTD-UHFFFAOYSA-N 3-[4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yl]oxy-N-[(5-oxopyrrolidin-2-yl)methyl]benzamide Chemical compound NCC1=CC(=NC(=C1)C(F)(F)F)OC=1C=C(C(=O)NCC2NC(CC2)=O)C=CC=1 ISXSUKUXUPLGTD-UHFFFAOYSA-N 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000008720 Bone Marrow Neoplasms Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 108091052242 Bromo- and Extra-Terminal domain (BET) family Proteins 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010007953 Central nervous system lymphoma Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 241000711549 Hepacivirus C Species 0.000 claims 1
- 241000700721 Hepatitis B virus Species 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
- 241000701044 Human gammaherpesvirus 4 Species 0.000 claims 1
- 241000725303 Human immunodeficiency virus Species 0.000 claims 1
- 241000701806 Human papillomavirus Species 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000005016 Intestinal Neoplasms Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010023825 Laryngeal cancer Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 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
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000009565 Pharyngeal Neoplasms Diseases 0.000 claims 1
- 206010034811 Pharyngeal cancer Diseases 0.000 claims 1
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010053879 Sepsis syndrome Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 206010051379 Systemic Inflammatory Response Syndrome 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
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 206010043515 Throat cancer Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 241000700605 Viruses Species 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 150000008044 alkali metal hydroxides Chemical class 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 201000000053 blastoma Diseases 0.000 claims 1
- 201000006491 bone marrow cancer Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000008184 embryoma Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 208000024519 eye neoplasm Diseases 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 208000006454 hepatitis Diseases 0.000 claims 1
- 231100000283 hepatitis Toxicity 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008106 ocular cancer Diseases 0.000 claims 1
- 208000027500 optic nerve neoplasm Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 208000010916 pituitary tumor Diseases 0.000 claims 1
- 208000016800 primary central nervous system lymphoma Diseases 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000002314 small intestine cancer Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 241000701161 unidentified adenovirus Species 0.000 claims 1
- 241001529453 unidentified herpesvirus Species 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 206010046885 vaginal cancer Diseases 0.000 claims 1
- 208000013139 vaginal neoplasm Diseases 0.000 claims 1
Priority Applications (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022053417A JP7375082B2 (ja) | 2016-06-20 | 2022-03-29 | Ｂｅｔ阻害剤の結晶固体形態 |
| JP2022107131A JP7588622B2 (ja) | 2016-06-20 | 2022-07-01 | Ｂｅｔ阻害剤の結晶固体形態 |
| JP2023183248A JP7789735B2 (ja) | 2016-06-20 | 2023-10-25 | Ｂｅｔ阻害剤の結晶固体形態 |
| JP2024089725A JP7727794B2 (ja) | 2016-06-20 | 2024-06-03 | Ｂｅｔ阻害剤の結晶固体形態 |
| JP2025128117A JP2025176008A (ja) | 2016-06-20 | 2025-07-31 | Ｂｅｔ阻害剤の結晶固体形態 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662352220P | 2016-06-20 | 2016-06-20 | |
| US62/352,220 | 2016-06-20 | ||
| US201662397575P | 2016-09-21 | 2016-09-21 | |
| US62/397,575 | 2016-09-21 | ||
| PCT/US2017/038121 WO2017222977A1 (en) | 2016-06-20 | 2017-06-19 | Crystalline solid forms of a bet inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022053417A Division JP7375082B2 (ja) | 2016-06-20 | 2022-03-29 | Ｂｅｔ阻害剤の結晶固体形態 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019524660A JP2019524660A (ja) | 2019-09-05 |
| JP2019524660A5 true JP2019524660A5 (enExample) | 2020-07-30 |
| JP7096170B2 JP7096170B2 (ja) | 2022-07-05 |
Family
ID=59258384
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018566525A Active JP7096170B2 (ja) | 2016-06-20 | 2017-06-19 | Ｂｅｔ阻害剤の結晶固体形態 |
| JP2022053417A Active JP7375082B2 (ja) | 2016-06-20 | 2022-03-29 | Ｂｅｔ阻害剤の結晶固体形態 |
| JP2022107131A Active JP7588622B2 (ja) | 2016-06-20 | 2022-07-01 | Ｂｅｔ阻害剤の結晶固体形態 |
| JP2024089725A Active JP7727794B2 (ja) | 2016-06-20 | 2024-06-03 | Ｂｅｔ阻害剤の結晶固体形態 |
| JP2025128117A Pending JP2025176008A (ja) | 2016-06-20 | 2025-07-31 | Ｂｅｔ阻害剤の結晶固体形態 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022053417A Active JP7375082B2 (ja) | 2016-06-20 | 2022-03-29 | Ｂｅｔ阻害剤の結晶固体形態 |
| JP2022107131A Active JP7588622B2 (ja) | 2016-06-20 | 2022-07-01 | Ｂｅｔ阻害剤の結晶固体形態 |
| JP2024089725A Active JP7727794B2 (ja) | 2016-06-20 | 2024-06-03 | Ｂｅｔ阻害剤の結晶固体形態 |
| JP2025128117A Pending JP2025176008A (ja) | 2016-06-20 | 2025-07-31 | Ｂｅｔ阻害剤の結晶固体形態 |
Country Status (34)
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI719464B (zh) | 2013-03-15 | 2021-02-21 | 美商英塞特控股公司 | 作為bet蛋白抑制劑之三環雜環 |
| US9309246B2 (en) | 2013-12-19 | 2016-04-12 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| KR20240134245A (ko) | 2014-04-23 | 2024-09-06 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
| US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| US20170121347A1 (en) | 2015-10-29 | 2017-05-04 | Incyte Corporation | Amorphous solid form of a bet protein inhibitor |
| EP4234554A3 (en) | 2016-06-20 | 2023-12-27 | Incyte Corporation | Crystalline solid forms of a bet inhibitor |
| TWI882964B (zh) * | 2018-09-13 | 2025-05-11 | 大陸商恒翼生物醫藥（上海）股份有限公司 | Bet 溴結構域(bromodomain)抑制劑之固體形式之製備方法 |
| WO2021217117A1 (en) * | 2020-04-24 | 2021-10-28 | Memorial Sloan Kettering Cancer Center | Targeted therapy for the treatment & prevention of life-threatening complications of infection |
| DK4161528T3 (da) | 2020-06-03 | 2025-11-24 | Incyte Corp | Kombination af ruxolitinib med incb057643 til anvendelse ved behandling af myeloproliferative neoplasmer |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CN112137961A (zh) * | 2020-09-30 | 2020-12-29 | 严鹏科 | 一种雷帕霉素组合物及其制备方法 |
| EP4267136A4 (en) * | 2020-12-23 | 2025-02-05 | Cascade Prodrug Inc. | Combination therapy with a vinca alkaloid n-oxide and an immune checkpoint inhibitor |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
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| JPS6243003U (enExample) | 1985-09-05 | 1987-03-14 | ||
| JPH0314566A (ja) | 1989-06-09 | 1991-01-23 | Sankyo Co Ltd | ベンズイミダゾール誘導体 |
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