JP2019524660A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
- Authority
- JP
- Japan
- Prior art keywords
- compound
- cancer
- solution
- solid form
- temperature
- 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
- 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 (OSRAM) | 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)
| Country | Link |
|---|---|
| US (6) | US10189832B2 (OSRAM) |
| EP (2) | EP4234554A3 (OSRAM) |
| JP (5) | JP7096170B2 (OSRAM) |
| KR (4) | KR102643344B1 (OSRAM) |
| CN (3) | CN114369091A (OSRAM) |
| AU (3) | AU2017281286B2 (OSRAM) |
| CA (3) | CA3220975A1 (OSRAM) |
| CL (3) | CL2018003702A1 (OSRAM) |
| CO (1) | CO2018014339A2 (OSRAM) |
| CR (2) | CR20220651A (OSRAM) |
| CY (1) | CY1126092T1 (OSRAM) |
| DK (1) | DK3472157T3 (OSRAM) |
| EC (1) | ECSP19001982A (OSRAM) |
| ES (1) | ES2945063T3 (OSRAM) |
| FI (1) | FI3472157T3 (OSRAM) |
| HR (1) | HRP20230466T1 (OSRAM) |
| HU (1) | HUE062234T2 (OSRAM) |
| IL (3) | IL263824B2 (OSRAM) |
| LT (1) | LT3472157T (OSRAM) |
| MD (1) | MD3472157T2 (OSRAM) |
| MX (3) | MX389145B (OSRAM) |
| MY (2) | MY209750A (OSRAM) |
| NZ (1) | NZ749956A (OSRAM) |
| PE (2) | PE20240236A1 (OSRAM) |
| PH (3) | PH12021551887A1 (OSRAM) |
| PL (1) | PL3472157T3 (OSRAM) |
| PT (1) | PT3472157T (OSRAM) |
| RS (1) | RS64274B1 (OSRAM) |
| SG (2) | SG10201912398PA (OSRAM) |
| SI (1) | SI3472157T1 (OSRAM) |
| SM (1) | SMT202300155T1 (OSRAM) |
| TW (3) | TWI830533B (OSRAM) |
| UA (2) | UA125476C2 (OSRAM) |
| WO (1) | WO2017222977A1 (OSRAM) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2909778T3 (es) | 2013-03-15 | 2022-05-10 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de proteína BET para su uso en el tratamiento de una enfermedad proliferativa en combinación con un inhibidor de Janus quinasas |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| SG10201809353TA (en) | 2014-04-23 | 2018-11-29 | Incyte Corp | 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS |
| WO2016044130A1 (en) | 2014-09-15 | 2016-03-24 | Incyte Corporation | Tricyclic heterocycles for use as bet protein inhibitors |
| AR106520A1 (es) | 2015-10-29 | 2018-01-24 | Incyte Corp | Forma sólida amorfa de un inhibidor de proteína bet |
| TWI830533B (zh) * | 2016-06-20 | 2024-01-21 | 美商英塞特公司 | Bet抑制劑之結晶固體形式 |
| 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 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| AU2020451061A1 (en) | 2020-06-03 | 2022-12-15 | Incyte Corporation | Combination of ruxolitinib with INCB057643 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 |
| JP2024500975A (ja) * | 2020-12-23 | 2024-01-10 | カスケード プロドラッグ インコーポレイテッド | ビンカアルカロイドn-オキシドと免疫チェックポイント阻害剤との併用療法 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | 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 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
Family Cites Families (167)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS59170313A (ja) | 1983-03-14 | 1984-09-26 | Kurimoto Iron Works Ltd | スクリ−ンゲ−ト |
| JPS6085739U (ja) | 1983-11-18 | 1985-06-13 | クラリオン株式会社 | テ−プレコ−ダにおけるピンチロ−ラ装置 |
| JPS6243003U (OSRAM) | 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 |
| US5244912A (en) | 1991-03-28 | 1993-09-14 | Eli Lilly And Company | 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz(cd)indoles and pharmaceutical use thereof |
| FR2710915B1 (fr) | 1993-10-04 | 1995-11-24 | Synthelabo | Dérivés de pipéridine, leur préparation et leur utilisation en thérapeutique. |
| GB9410469D0 (en) | 1994-05-25 | 1994-07-13 | Erba Farmitalia | Imidazolylalkyl derivatives of imidazo (5,1-c) (1,4) benzoxazin-1-one and process for their preparation |
| FR2731708B1 (fr) | 1995-03-13 | 1997-04-30 | Synthelabo | Derives de piperidine, leur procede de preparation et leur application en therapeutique |
| FR2747678B1 (fr) | 1996-04-22 | 1998-05-22 | Synthelabo | Composes derives d'imidazobenzoxazine, leurs procedes de preparation et leurs utilisations en therapeutique |
| US6287693B1 (en) | 1998-02-25 | 2001-09-11 | John Claude Savoir | Stable shaped particles of crystalline organic compounds |
| ATE312608T1 (de) | 2000-04-21 | 2005-12-15 | Pharmacia & Upjohn Co Llc | Cabergolin zur behandlung von fibromyalgie und chronic-fatigue-syndrom |
| DE60105023T2 (de) | 2000-06-28 | 2005-08-18 | Smithkline Beecham P.L.C., Brentford | Nassvermahlungsverfahren |
| AU2001282267A1 (en) | 2000-08-08 | 2002-02-18 | Sanofi-Aventis | Benzimidazole derivatives, preparation and therapeutic use thereof |
| FR2816619B1 (fr) | 2000-11-15 | 2003-01-31 | Sanofi Synthelabo | Derives de benzimidazole, leur preparation et leur application en therapeutique |
| US6919334B2 (en) | 2002-09-12 | 2005-07-19 | Wyeth | Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine |
| KR100772297B1 (ko) | 2002-11-22 | 2007-11-02 | 니뽄 다바코 산교 가부시키가이샤 | 융합 비시클릭 질소-함유 헤테로사이클 |
| EP1462103A1 (en) | 2003-03-25 | 2004-09-29 | Faust Pharmaceuticals | NO donors, combination products and uses as modulators of neurotransmitter release |
| AU2005214258A1 (en) | 2004-02-23 | 2005-09-01 | Dainippon Sumitomo Pharma Co., Ltd. | Novel heterocyclic compound |
| US7897607B2 (en) | 2004-04-07 | 2011-03-01 | Takeda Pharmaceutical Company Limited | Cyclic compounds |
| US7713954B2 (en) | 2004-09-30 | 2010-05-11 | Roche Palo Alto Llc | Compositions and methods for treating cognitive disorders |
| DE102005011058A1 (de) | 2005-03-10 | 2006-09-14 | Merck Patent Gmbh | Substituierte Tetrahydro-pyrrolo-chinolinderivate |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| TWI447120B (zh) | 2005-05-30 | 2014-08-01 | Mitsubishi Tanabe Pharma Corp | 噻吩并三唑并苯二氮呯化合物、其醫藥上之用途 |
| MX2008001152A (es) | 2005-08-05 | 2008-04-02 | Astrazeneca Ab | Benzimidazoles triciclicos y su uso como moduladores del receptor de glutamato metabotropico. |
| EP2147310A4 (en) | 2007-04-27 | 2010-09-08 | Univ Rochester | COMPOSITIONS AND METHODS OF INHIBITING G-PROTEIN SIGNALING |
| US9603848B2 (en) | 2007-06-08 | 2017-03-28 | Senomyx, Inc. | Modulation of chemosensory receptors and ligands associated therewith |
| US7928111B2 (en) | 2007-06-08 | 2011-04-19 | Senomyx, Inc. | Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors |
| US8633186B2 (en) | 2007-06-08 | 2014-01-21 | Senomyx Inc. | Modulation of chemosensory receptors and ligands associated therewith |
| WO2009020559A2 (en) | 2007-08-03 | 2009-02-12 | The J. David Gladstone Institutes | Agents that inhibit p-tefb interactions and methods of use thereof |
| KR101600634B1 (ko) | 2007-12-28 | 2016-03-07 | 미쓰비시 타나베 파마 코퍼레이션 | 항암제 |
| DE102008052618A1 (de) | 2008-10-21 | 2010-04-22 | Henkel Ag & Co. Kgaa | Tricyclische Aldehyde und C,H-acide Verbindungen |
| WO2010111626A2 (en) | 2009-03-27 | 2010-09-30 | Takeda Pharmaceutical Company Limited | Poly (adp-ribose) polymerase (parp) inhibitors |
| TW201103941A (en) | 2009-06-10 | 2011-02-01 | Janssen Pharmaceutica Nv | Benzimidazole derivatives useful as TRPM8 channel modulators |
| TW201105681A (en) | 2009-06-10 | 2011-02-16 | Janssen Pharmaceutica Nv | Benzimidazole derivatives useful as TRPM8 channel modulators |
| WO2011024987A1 (ja) | 2009-08-31 | 2011-03-03 | 塩野義製薬株式会社 | 芳香族縮合へテロ環誘導体およびそれらを含有する医薬組成物 |
| GB0919431D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| US9360482B2 (en) | 2009-11-05 | 2016-06-07 | Glaxosmithkline Llc | Process for the identification of a compound which inhibits the binding of the second bromodomain of each of human BRD-2, BRD-3, and BRD-4 |
| DK2496582T3 (en) | 2009-11-05 | 2016-03-21 | Glaxosmithkline Llc | Benzodiazepine-BROMDOMAeNEINHIBITOR. |
| PH12012500894A1 (en) | 2009-11-05 | 2022-03-09 | Glaxosmithkline Llc | Benzodiazepine bromodomain inhibitor |
| BR112012026641A2 (pt) | 2010-04-23 | 2016-07-12 | Kineta Inc | compostos antivirais |
| MX354217B (es) | 2010-05-14 | 2018-02-19 | Dana Farber Cancer Inst Inc | Composiciones y metodos para el tratamiento de leucemia. |
| CA2799381A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Male contraceptive compositions and methods of use |
| EP2569429A4 (en) | 2010-05-14 | 2013-09-25 | Dana Farber Cancer Inst Inc | COMPOSITIONS AND METHODS FOR MODULATING METABOLISM |
| PL2571503T3 (pl) | 2010-05-14 | 2015-06-30 | Dana Farber Cancer Inst Inc | Kompozycje i sposoby leczenia nowotworu, choroby zapalnej i innych zaburzeń |
| WO2011161031A1 (en) | 2010-06-22 | 2011-12-29 | Glaxosmithkline Llc | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| WO2012075456A1 (en) | 2010-12-02 | 2012-06-07 | Constellation Pharmaceuticals | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| CN103476767B (zh) | 2011-02-09 | 2015-06-10 | 弗·哈夫曼-拉罗切有限公司 | 作为pi3激酶抑制剂的杂环化合物 |
| WO2012116170A1 (en) | 2011-02-23 | 2012-08-30 | Ming-Ming Zhou | Inhibitors of bromodomains as modulators of gene expression |
| CA2825966A1 (en) | 2011-03-21 | 2012-09-27 | F. Hoffmann-La Roche Ag | Benzoxazepin compounds selective for pi3k p110 delta and methods of use |
| GB201106799D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201106750D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201106743D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| GB201107325D0 (en) | 2011-05-04 | 2011-06-15 | Glaxosmithkline Llc | Novel compounds |
| WO2012151512A2 (en) | 2011-05-04 | 2012-11-08 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2012174487A2 (en) | 2011-06-17 | 2012-12-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| WO2012178208A2 (en) | 2011-06-24 | 2012-12-27 | The Trustees Of The Stevens Institute Of Technology | Selective inhibitors of histone deacetylase isoform 6 and methods thereof |
| JP2013010719A (ja) | 2011-06-30 | 2013-01-17 | Dainippon Sumitomo Pharma Co Ltd | ベンズイミダゾロンおよびオキシインドール誘導体ならびにそれらの医薬用途 |
| WO2013019710A1 (en) | 2011-07-29 | 2013-02-07 | The Children's Hospital Of Philadelphia | Compositions and methods for the treatment of hiv |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2013033268A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bivalent bromodomain ligands, and methods of using same |
| WO2013033269A1 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same |
| NO2751083T3 (OSRAM) | 2011-08-31 | 2018-05-26 | ||
| DE102011082013A1 (de) | 2011-09-01 | 2013-03-07 | Bayer Pharma AG | 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine |
| ES2632443T3 (es) | 2011-09-22 | 2017-09-13 | Viiv Healthcare Uk Limited | Compuestos de pirrolopiridinona y procedimientos de tratamiento del VIH |
| WO2013044511A1 (zh) | 2011-09-30 | 2013-04-04 | 沈阳蓝桑医药生物技术研发有限公司 | 含有瑞利格内酯的药物组合物及其应用 |
| EP2771340B1 (en) | 2011-10-25 | 2016-04-13 | Sanofi | 6-(4-hydroxy-phenyl)-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| PT2773354T (pt) | 2011-11-01 | 2019-07-17 | Resverlogix Corp | Formulações orais de libertação imediata para quinazolinonas substituídas |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| US20150133434A1 (en) | 2012-03-28 | 2015-05-14 | The J. David Gladstone Institutes | Compositions and Methods for Reactivating Latent Immunodeficiency Virus |
| US20130281398A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| US20130281397A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| US20130281399A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| US20130281396A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| CA2870931A1 (en) | 2012-04-20 | 2013-10-24 | Abbvie Inc. | Isoindolone derivatives |
| WO2013184878A1 (en) | 2012-06-06 | 2013-12-12 | Constellation Pharmaceuticals, Inc. | Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof |
| TWI602820B (zh) | 2012-06-06 | 2017-10-21 | 星宿藥物公司 | 溴域抑制劑及其用途 |
| WO2013185284A1 (en) | 2012-06-12 | 2013-12-19 | Abbott Laboratories | Pyridinone and pyridazinone derivatives |
| IN2014DN11269A (OSRAM) | 2012-06-25 | 2015-10-09 | Oncoethix Sa | |
| WO2014015175A1 (en) | 2012-07-18 | 2014-01-23 | Massachusetts Institute Of Technology | Compositions and methods for modulating brd4 bioactivity |
| ES2628005T3 (es) | 2012-08-16 | 2017-08-01 | Bayer Pharma Aktiengesellschaft | 2,3-Benzodiazepinas |
| EP2884983B1 (en) | 2012-08-16 | 2017-10-04 | GlaxoSmithKline LLC | Benzodiazepines for treating small cell lung cancer |
| RU2015115634A (ru) | 2012-09-28 | 2016-11-20 | Онкоэтикс Гмбх | Фармацевтический состав, содержащий соединения тиенотриазолодиазепина |
| US9663523B2 (en) | 2012-09-28 | 2017-05-30 | Bayer Pharma Aktiengesellschaft | BET protein-inhibiting 5-aryltriazoleazepines |
| HUE047441T2 (hu) | 2012-11-09 | 2020-04-28 | Medicines For Malaria Venture Mmv | Heteroaril-származékok és alkamazásaik |
| US9422290B2 (en) | 2012-11-13 | 2016-08-23 | Boehringer Ingelheim International Gmbh | Triazolopyridazine |
| US9663533B2 (en) | 2012-11-14 | 2017-05-30 | Glaxosmithkline Llc | Thieno[3,2-C]pyridin-4(5H)-ones as BET inhibitors |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| WO2014080290A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Cyclic amines as bromodomain inhibitors |
| JP2016509576A (ja) | 2012-12-20 | 2016-03-31 | バイエル ファーマ アクチエンゲゼルシャフト | Betタンパク質阻害性ジヒドロキノキザリノン類 |
| CN105229002A (zh) | 2012-12-20 | 2016-01-06 | 拜耳医药股份有限公司 | 抑制bet蛋白的二氢吡啶并吡嗪酮 |
| EP2935253B1 (en) | 2012-12-21 | 2018-08-01 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2014128655A1 (en) | 2013-02-25 | 2014-08-28 | Aurigene Discovery Technologies Limited | Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors |
| EP2961747B1 (en) | 2013-02-27 | 2017-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| US9492460B2 (en) | 2013-02-27 | 2016-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| EP2970285B1 (en) | 2013-03-11 | 2019-04-17 | AbbVie Inc. | Fused tetracyclic bromodomain inhibitors |
| US9675697B2 (en) | 2013-03-11 | 2017-06-13 | The Regents Of The University Of Michigan | BET bromodomain inhibitors and therapeutic methods using the same |
| JP2016512524A (ja) | 2013-03-11 | 2016-04-28 | アッヴィ・インコーポレイテッド | ブロモドメイン阻害剤 |
| SG11201507383WA (en) | 2013-03-12 | 2015-10-29 | Abbvie Inc | Dihydro-pyrrolopyridinone bromodomain inhibitors |
| KR102224992B1 (ko) | 2013-03-12 | 2021-03-10 | 애브비 인코포레이티드 | 테트라사이클릭 브로모도메인 억제제 |
| CN105164113B (zh) | 2013-03-12 | 2018-03-02 | 艾伯维公司 | 吡咯酰胺抑制剂 |
| KR20150135359A (ko) | 2013-03-14 | 2015-12-02 | 컨버진 엘엘씨 | 브로모도메인-함유 단백질의 억제를 위한 방법 및 조성물 |
| SG11201506245QA (en) | 2013-03-14 | 2015-09-29 | Glaxosmithkline Ip No 2 Ltd | 2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors |
| JP6280573B2 (ja) | 2013-03-14 | 2018-02-14 | グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited | ブロモドメイン阻害薬としてのフロピリジン |
| US9714946B2 (en) | 2013-03-14 | 2017-07-25 | Dana-Farber Cancer Institute, Inc. | Bromodomain binding reagents and uses thereof |
| ES2909778T3 (es) | 2013-03-15 | 2022-05-10 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de proteína BET para su uso en el tratamiento de una enfermedad proliferativa en combinación con un inhibidor de Janus quinasas |
| WO2014152029A2 (en) | 2013-03-15 | 2014-09-25 | Epigenetix, Inc. | Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors |
| DK2970265T3 (en) | 2013-03-15 | 2018-10-01 | Plexxikon Inc | HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF |
| US9102684B2 (en) | 2013-03-27 | 2015-08-11 | Boehringer Ingelheim International Gmbh | Indolinone analogues |
| EP2978758B1 (en) | 2013-03-27 | 2017-02-08 | Boehringer Ingelheim International GmbH | Dihydroquinazolinone analogues as brd4 inhibitors |
| TWI530499B (zh) | 2013-03-28 | 2016-04-21 | 吉李德科學股份有限公司 | 作為溴結構域(bromodomain)抑制劑之苯並咪唑酮衍生物類 |
| US10435364B2 (en) | 2013-04-17 | 2019-10-08 | Albert Ludwigs Universität Freiburg | Compounds for use as bromodomain inhibitors |
| EA027139B1 (ru) | 2013-04-26 | 2017-06-30 | Бейджин, Лтд. | Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны |
| TWI527811B (zh) | 2013-05-09 | 2016-04-01 | 吉李德科學股份有限公司 | 作爲溴結構域抑制劑的苯並咪唑衍生物 |
| EP3004109A1 (en) | 2013-05-27 | 2016-04-13 | Novartis AG | Imidazopyrrolidinone derivatives and their use in the treatment of disease |
| US8975417B2 (en) | 2013-05-27 | 2015-03-10 | Novartis Ag | Pyrazolopyrrolidine derivatives and their use in the treatment of disease |
| JP2016520118A (ja) | 2013-05-28 | 2016-07-11 | ノバルティス アーゲー | Bet阻害剤としてのピラゾロ−ピロリジン−4−オン誘導体および疾患の処置におけるその使用 |
| MX2015016425A (es) | 2013-05-28 | 2016-03-03 | Novartis Ag | Derivados de pirazolo-pirrolidin-4-ona y su uso en el tratamiento de enfermedades. |
| ITMI20130991A1 (it) | 2013-06-17 | 2014-12-18 | Industrie De Nora Spa | Sistema per la misurazione di correnti presenti sugli elettrodi in celle elettrolitiche interconnesse. |
| JP2016521722A (ja) | 2013-06-17 | 2016-07-25 | バイエル ファーマ アクチエンゲゼルシャフト | 置換フェニル−2,3−ベンゾジアゼピン |
| WO2015002754A2 (en) | 2013-06-21 | 2015-01-08 | Zenith Epigenetics Corp. | Novel bicyclic bromodomain inhibitors |
| WO2015004533A2 (en) | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| AR096758A1 (es) * | 2013-06-28 | 2016-02-03 | Abbvie Inc | Inhibidores cristalinos de bromodominios |
| BR112015032710A2 (pt) | 2013-06-28 | 2017-07-25 | Abbvie Inc | inibidores de bromodomínio |
| ES2635560T3 (es) | 2013-07-08 | 2017-10-04 | Incyte Holdings Corporation | Heterociclos tricíclicos como inhibidores de la proteína NET |
| CA2917177C (en) | 2013-07-16 | 2022-07-12 | Basf Se | Herbicidal azines |
| MX2016001037A (es) | 2013-07-25 | 2016-11-10 | Dana Farber Cancer Inst Inc | Inhibidores de factores de transcripción y usos. |
| KR101672096B1 (ko) | 2013-09-30 | 2016-11-02 | 주식회사 엘지화학 | 헤테로환 화합물 및 이를 포함하는 유기 발광 소자 |
| RS63733B1 (sr) | 2013-10-18 | 2022-12-30 | Celgene Quanticel Research Inc | Inhibitori bromodomena |
| WO2015081246A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015081203A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
| CN105939996A (zh) | 2013-12-09 | 2016-09-14 | 艾伯维公司 | 用作布罗莫结构域抑制剂的二氢吡啶酮和二氢哒嗪酮衍生物 |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| WO2015095445A1 (en) * | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors |
| MY190835A (en) | 2014-01-09 | 2022-05-12 | Orion Corp | Bicyclic heterrocyclic derivatives as bromodomain inhibitors |
| US9580430B2 (en) | 2014-02-28 | 2017-02-28 | The Regents Of The University Of Michigan | 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors |
| WO2015163485A1 (en) | 2014-04-23 | 2015-10-29 | Takeda Pharmaceutical Company Limited | Isoindoline-1-one derivatives as cholinergic muscarinic m1 receptor positive alloesteric modulator activity for the treatment of alzheimers disease |
| EP3134400B1 (en) | 2014-04-23 | 2018-10-17 | Basf Se | Diaminotriazine compounds as herbicides |
| SG10201809353TA (en) | 2014-04-23 | 2018-11-29 | Incyte Corp | 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS |
| EP3137086A4 (en) | 2014-05-02 | 2017-12-27 | Oncoethix GmbH | Method of treating resistant non-hodgkin lymphoma, medulloblastoma, and/or alk+non-small cell lung cancer using thienotriazolodiazepine compounds |
| US9956228B2 (en) | 2014-05-02 | 2018-05-01 | Oncoethix Gmbh | Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds |
| CN106852120A (zh) | 2014-05-08 | 2017-06-13 | 翁科埃斯克斯有限公司 | 利用噻吩并三唑并二氮杂*化合物治疗三阴性乳腺癌的方法 |
| WO2015169953A1 (en) | 2014-05-08 | 2015-11-12 | Oncoethix Gmbh | Method of treating glioma using thienotriazolodiazepine compounds |
| US10065951B2 (en) | 2014-05-30 | 2018-09-04 | Icahn School Of Medicine At Mount Sinai | Small molecule transcription modulators of bromodomains |
| HUE043441T2 (hu) | 2014-06-20 | 2019-08-28 | Constellation Pharmaceuticals Inc | 2-((4S)-6-(4-klórfenil)-l-metil-4H-benzo[c]izoxazolo[4,5-e]azepin-4-il)acetamid kristályos formái |
| US9861077B2 (en) | 2014-07-11 | 2018-01-09 | Jaan Aked-Hurditch | Leash accessory |
| WO2016044130A1 (en) | 2014-09-15 | 2016-03-24 | Incyte Corporation | Tricyclic heterocycles for use as bet protein inhibitors |
| DK3461821T3 (da) | 2014-10-24 | 2020-08-17 | Bristol Myers Squibb Co | Indolcarboxamidforbindelser, der er brugbar som kinasehæmmere |
| MA40943A (fr) * | 2014-11-10 | 2017-09-19 | Constellation Pharmaceuticals Inc | Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines |
| CA2974153A1 (en) | 2015-02-03 | 2016-08-11 | Trillium Therapeutics Inc. | Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins |
| WO2016186453A1 (en) | 2015-05-20 | 2016-11-24 | Kainos Medicine, Inc. | Quinoline derivatives as bromodomain inhibitors |
| SG11201709634QA (en) | 2015-05-29 | 2017-12-28 | Shionogi & Co | Nitrogen-containing tricyclic derivative having hiv replication inhibitory activity |
| CN105039258B (zh) | 2015-07-03 | 2018-04-17 | 北京大学 | 将非神经元细胞重编程为神经元样细胞的方法和组合物 |
| AR106520A1 (es) | 2015-10-29 | 2018-01-24 | Incyte Corp | Forma sólida amorfa de un inhibidor de proteína bet |
| CN105254635A (zh) | 2015-10-30 | 2016-01-20 | 中国药科大学 | 一类咪唑并吡嗪类化合物及其药物组合物和用途 |
| US20170127985A1 (en) | 2015-11-11 | 2017-05-11 | Medtronic Minimed, Inc. | Sensor set |
| CA3007168A1 (en) | 2015-12-14 | 2017-06-22 | Zenith Epigenetics Ltd. | 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors |
| US10519151B2 (en) | 2016-01-28 | 2019-12-31 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-A]pyridines, their preparation and their use as pharmaceuticals |
| JP2019508494A (ja) | 2016-02-05 | 2019-03-28 | チーア タイ ティエンチン ファーマシューティカル グループ カンパニー,リミティド | ブロモドメインタンパク質阻害剤の三環式化合物、並びにその製造、医薬組成物及び使用 |
| TWI830533B (zh) | 2016-06-20 | 2024-01-21 | 美商英塞特公司 | Bet抑制劑之結晶固體形式 |
| CN108069958A (zh) | 2016-11-10 | 2018-05-25 | 凯惠科技发展(上海)有限公司 | 一种含氮杂环类化合物、其制备方法、药物组合物及应用 |
-
2017
- 2017-06-19 TW TW111147670A patent/TWI830533B/zh active
- 2017-06-19 DK DK17734590.7T patent/DK3472157T3/da active
- 2017-06-19 NZ NZ749956A patent/NZ749956A/en unknown
- 2017-06-19 CR CR20220651A patent/CR20220651A/es unknown
- 2017-06-19 PE PE2023002468A patent/PE20240236A1/es unknown
- 2017-06-19 PH PH1/2021/551887A patent/PH12021551887A1/en unknown
- 2017-06-19 KR KR1020227036514A patent/KR102643344B1/ko active Active
- 2017-06-19 MD MDE20190507T patent/MD3472157T2/ro unknown
- 2017-06-19 SG SG10201912398PA patent/SG10201912398PA/en unknown
- 2017-06-19 PH PH1/2021/551886A patent/PH12021551886A1/en unknown
- 2017-06-19 WO PCT/US2017/038121 patent/WO2017222977A1/en not_active Ceased
- 2017-06-19 IL IL263824A patent/IL263824B2/en unknown
- 2017-06-19 EP EP23160938.9A patent/EP4234554A3/en active Pending
- 2017-06-19 TW TW113101597A patent/TWI854936B/zh active
- 2017-06-19 UA UAA202008134A patent/UA125476C2/uk unknown
- 2017-06-19 CA CA3220975A patent/CA3220975A1/en active Pending
- 2017-06-19 JP JP2018566525A patent/JP7096170B2/ja active Active
- 2017-06-19 HR HRP20230466TT patent/HRP20230466T1/hr unknown
- 2017-06-19 CA CA3028689A patent/CA3028689A1/en active Pending
- 2017-06-19 UA UAA201900524A patent/UA124106C2/uk unknown
- 2017-06-19 LT LTEPPCT/US2017/038121T patent/LT3472157T/lt unknown
- 2017-06-19 EP EP17734590.7A patent/EP3472157B1/en active Active
- 2017-06-19 CR CR20190027A patent/CR20190027A/es unknown
- 2017-06-19 KR KR1020247006758A patent/KR102888132B1/ko active Active
- 2017-06-19 SG SG11201811416VA patent/SG11201811416VA/en unknown
- 2017-06-19 CN CN202111446313.6A patent/CN114369091A/zh active Pending
- 2017-06-19 PE PE2018003269A patent/PE20190623A1/es unknown
- 2017-06-19 HU HUE17734590A patent/HUE062234T2/hu unknown
- 2017-06-19 RS RS20230430A patent/RS64274B1/sr unknown
- 2017-06-19 KR KR1020197001805A patent/KR102460046B1/ko active Active
- 2017-06-19 CN CN201780038099.6A patent/CN109715625B/zh active Active
- 2017-06-19 MY MYPI2023005532A patent/MY209750A/en unknown
- 2017-06-19 CA CA3220957A patent/CA3220957A1/en active Pending
- 2017-06-19 ES ES17734590T patent/ES2945063T3/es active Active
- 2017-06-19 AU AU2017281286A patent/AU2017281286B2/en active Active
- 2017-06-19 KR KR1020257037981A patent/KR20250163425A/ko active Pending
- 2017-06-19 TW TW106120412A patent/TWI786050B/zh active
- 2017-06-19 CN CN202111443358.8A patent/CN114366748A/zh active Pending
- 2017-06-19 MY MYPI2018002677A patent/MY198892A/en unknown
- 2017-06-19 PL PL17734590.7T patent/PL3472157T3/pl unknown
- 2017-06-19 MX MX2018016281A patent/MX389145B/es unknown
- 2017-06-19 IL IL302528A patent/IL302528A/en unknown
- 2017-06-19 PT PT177345907T patent/PT3472157T/pt unknown
- 2017-06-19 SM SM20230155T patent/SMT202300155T1/it unknown
- 2017-06-19 FI FIEP17734590.7T patent/FI3472157T3/fi active
- 2017-06-19 US US15/626,539 patent/US10189832B2/en active Active
- 2017-06-19 SI SI201731358T patent/SI3472157T1/sl unknown
-
2018
- 2018-12-07 US US16/213,202 patent/US10626114B2/en active Active
- 2018-12-19 MX MX2023009524A patent/MX2023009524A/es unknown
- 2018-12-19 CL CL2018003702A patent/CL2018003702A1/es unknown
- 2018-12-19 MX MX2021009776A patent/MX2021009776A/es unknown
- 2018-12-20 PH PH12018502709A patent/PH12018502709A1/en unknown
- 2018-12-28 CO CONC2018/0014339A patent/CO2018014339A2/es unknown
-
2019
- 2019-01-10 EC ECSENADI20191982A patent/ECSP19001982A/es unknown
-
2020
- 2020-02-19 CL CL2020000408A patent/CL2020000408A1/es unknown
- 2020-02-19 CL CL2020000407A patent/CL2020000407A1/es unknown
- 2020-03-24 US US16/828,031 patent/US11091480B2/en active Active
- 2020-12-18 US US17/127,351 patent/US11377446B2/en active Active
-
2021
- 2021-08-09 AU AU2021215112A patent/AU2021215112B2/en active Active
- 2021-08-17 IL IL285686A patent/IL285686B/en unknown
-
2022
- 2022-03-29 JP JP2022053417A patent/JP7375082B2/ja active Active
- 2022-06-02 US US17/830,494 patent/US12030882B2/en active Active
- 2022-07-01 JP JP2022107131A patent/JP7588622B2/ja active Active
-
2023
- 2023-06-15 CY CY20231100282T patent/CY1126092T1/el unknown
- 2023-09-11 AU AU2023229471A patent/AU2023229471B2/en active Active
-
2024
- 2024-05-28 US US18/675,780 patent/US12459943B2/en active Active
- 2024-06-03 JP JP2024089725A patent/JP7727794B2/ja active Active
-
2025
- 2025-07-31 JP JP2025128117A patent/JP2025176008A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2019524660A5 (OSRAM) | ||
| JP2024113019A5 (OSRAM) | ||
| HRP20230466T1 (hr) | Kristalni čvrsti oblici bet inhibitora | |
| ES2988336T3 (es) | Un agente antineoplásico 1-((4-(4-fluoro-2-metil-1H-indol-5-iloxi)-6-metoxiquinolin-7-iloxi)metil)ciclopropanamina, su forma cristalina y sus sales | |
| ES2615238T3 (es) | Derivados de tetrahidroquinolinas como inhibidores de bromodominio | |
| TWI697495B (zh) | 科帕利普(copanlisib)及其二鹽酸鹽之合成 | |
| JP2013544847A5 (OSRAM) | ||
| WO2014090692A1 (en) | Novel bi-ring phenyl-pyridines/pyrazines for the treatment of cancer | |
| JP2017526731A5 (OSRAM) | ||
| TW200418806A (en) | HDAC inhibitor | |
| CN105237510A (zh) | 埃克替尼和盐酸埃克替尼的制备方法及其中间体 | |
| WO2006046552A1 (ja) | 新規な含窒素複素環化合物およびその塩 | |
| CN104447743A (zh) | 帕博西尼的制备方法 | |
| WO2011086541A1 (en) | Novel polymorph of nilotinib monohydrochloride monohydrate | |
| WO2017025784A1 (en) | A carbon dioxide adduct of palbociclib | |
| WO2014154723A1 (en) | Novel pyrrole derivatives for the treatment of cancer | |
| CN118496300A (zh) | 一种靶向降解kras的protac化合物及其应用 | |
| WO2011033307A1 (en) | Nilotinib dihydrochloride salt | |
| ES2698959T3 (es) | Método para producir un compuesto de 1,4-benzoxazina | |
| JP2017506267A5 (OSRAM) | ||
| CN112955449B (zh) | 制备bet溴结构域抑制剂的固体形式的方法 | |
| JP2025536416A (ja) | 置換ピペラジン誘導体の結晶およびその調製方法 | |
| CN111247153A (zh) | 3-(5-氟苯并呋喃-3-基)-4-(5-甲基-5H-[1,3]间二氧杂环戊烯并[4,5-f]吲哚-7-基)吡咯-2,5-二酮的固体形式 | |
| CN114222742B (zh) | 一类2-氨基嘧啶类化合物及其药物组合物和用途 | |
| CN111315748A (zh) | 3-(5-氟苯并呋喃-3-基)-4-(5-甲基-5H-[1,3]间二氧杂环戊烯并[4,5-f]吲哚-7-基)吡咯-2,5-二酮的固体形式 |