JP2016528179A5 - - Google Patents
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- JP2016528179A5 JP2016528179A5 JP2016519576A JP2016519576A JP2016528179A5 JP 2016528179 A5 JP2016528179 A5 JP 2016528179A5 JP 2016519576 A JP2016519576 A JP 2016519576A JP 2016519576 A JP2016519576 A JP 2016519576A JP 2016528179 A5 JP2016528179 A5 JP 2016528179A5
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- Prior art keywords
- crystal
- diffraction pattern
- ray diffraction
- compound
- formula
- Prior art date
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- 239000013078 crystal Substances 0.000 claims 71
- 150000001875 compounds Chemical class 0.000 claims 35
- 238000002441 X-ray diffraction Methods 0.000 claims 28
- 238000000034 method Methods 0.000 claims 17
- 238000000634 powder X-ray diffraction Methods 0.000 claims 17
- 206010028980 Neoplasm Diseases 0.000 claims 13
- 201000011510 cancer Diseases 0.000 claims 11
- 238000000113 differential scanning calorimetry Methods 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 5
- 238000004519 manufacturing process Methods 0.000 claims 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- 238000002844 melting Methods 0.000 claims 4
- 230000008018 melting Effects 0.000 claims 4
- 239000007909 solid dosage form Substances 0.000 claims 4
- OISVCGZHLKNMSJ-UHFFFAOYSA-N 2,6-dimethylpyridine Chemical group CC1=CC=CC(C)=N1 OISVCGZHLKNMSJ-UHFFFAOYSA-N 0.000 claims 3
- 206010039491 Sarcoma Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 239000002904 solvent Substances 0.000 claims 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 159000000007 calcium salts Chemical class 0.000 claims 2
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical group [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 208000019691 hematopoietic and lymphoid cell neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 230000001590 oxidative effect Effects 0.000 claims 2
- 239000000843 powder Substances 0.000 claims 2
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 2
- 238000001959 radiotherapy Methods 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 239000003826 tablet Substances 0.000 claims 2
- WJKHJLXJJJATHN-UHFFFAOYSA-N triflic anhydride Chemical compound FC(F)(F)S(=O)(=O)OS(=O)(=O)C(F)(F)F WJKHJLXJJJATHN-UHFFFAOYSA-N 0.000 claims 2
- PDVFSPNIEOYOQL-UHFFFAOYSA-N (4-methylphenyl)sulfonyl 4-methylbenzenesulfonate Chemical compound C1=CC(C)=CC=C1S(=O)(=O)OS(=O)(=O)C1=CC=C(C)C=C1 PDVFSPNIEOYOQL-UHFFFAOYSA-N 0.000 claims 1
- XWKFPIODWVPXLX-UHFFFAOYSA-N 2-methyl-5-methylpyridine Natural products CC1=CC=C(C)N=C1 XWKFPIODWVPXLX-UHFFFAOYSA-N 0.000 claims 1
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000004463 Follicular Adenocarcinoma Diseases 0.000 claims 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 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
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010025538 Malignant ascites Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- CBENFWSGALASAD-UHFFFAOYSA-N Ozone Chemical compound [O-][O+]=O CBENFWSGALASAD-UHFFFAOYSA-N 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms 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
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 206010006007 bone sarcoma Diseases 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 230000018044 dehydration Effects 0.000 claims 1
- 238000006297 dehydration reaction Methods 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 239000008187 granular material Substances 0.000 claims 1
- 210000002768 hair cell Anatomy 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
- 230000002489 hematologic effect Effects 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- NWYYWIJOWOLJNR-RXMQYKEDSA-N l-valinol Chemical compound CC(C)[C@H](N)CO NWYYWIJOWOLJNR-RXMQYKEDSA-N 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000001926 lymphatic effect Effects 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 230000003647 oxidation Effects 0.000 claims 1
- 238000007254 oxidation reaction Methods 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 201000005528 peripheral nervous system neoplasm Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- AQAAVCJTEANSGJ-UHFFFAOYSA-N propane-2-sulfinic acid Chemical compound CC(C)S(O)=O AQAAVCJTEANSGJ-UHFFFAOYSA-N 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 210000000664 rectum Anatomy 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 210000004116 schwann cell Anatomy 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 210000004872 soft tissue Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 125000003944 tolyl group Chemical group 0.000 claims 1
- IMNIMPAHZVJRPE-UHFFFAOYSA-N triethylenediamine Chemical compound C1CN2CCN1CC2 IMNIMPAHZVJRPE-UHFFFAOYSA-N 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 0 CC(C)C(CS(C(C)*)(=O)=O)N([C@@]([C@](C[C@]1(C)C*)c2cc(*)ccc2)c(cc2)ccc2Cl)C1=O Chemical compound CC(C)C(CS(C(C)*)(=O)=O)N([C@@]([C@](C[C@]1(C)C*)c2cc(*)ccc2)c(cc2)ccc2Cl)C1=O 0.000 description 2
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020084989A JP6891322B2 (ja) | 2013-06-10 | 2020-05-14 | 製造方法及びｍｄｍ２阻害剤の結晶形 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361833196P | 2013-06-10 | 2013-06-10 | |
| US61/833,196 | 2013-06-10 | ||
| PCT/US2014/041594 WO2014200937A1 (en) | 2013-06-10 | 2014-06-09 | Processes of making and crystalline forms of a mdm2 inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020084989A Division JP6891322B2 (ja) | 2013-06-10 | 2020-05-14 | 製造方法及びｍｄｍ２阻害剤の結晶形 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016528179A JP2016528179A (ja) | 2016-09-15 |
| JP2016528179A5 true JP2016528179A5 (enExample) | 2017-07-20 |
| JP6998655B2 JP6998655B2 (ja) | 2022-02-04 |
Family
ID=51063849
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016519576A Active JP6998655B2 (ja) | 2013-06-10 | 2014-06-09 | 製造方法及びｍｄｍ２阻害剤の結晶形 |
| JP2020084989A Active JP6891322B2 (ja) | 2013-06-10 | 2020-05-14 | 製造方法及びｍｄｍ２阻害剤の結晶形 |
| JP2021087378A Active JP7263439B2 (ja) | 2013-06-10 | 2021-05-25 | 製造方法及びｍｄｍ２阻害剤の結晶形 |
| JP2023064715A Pending JP2023089126A (ja) | 2013-06-10 | 2023-04-12 | 製造方法及びｍｄｍ２阻害剤の結晶形 |
| JP2025029906A Pending JP2025084856A (ja) | 2013-06-10 | 2025-02-27 | 製造方法及びｍｄｍ２阻害剤の結晶形 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020084989A Active JP6891322B2 (ja) | 2013-06-10 | 2020-05-14 | 製造方法及びｍｄｍ２阻害剤の結晶形 |
| JP2021087378A Active JP7263439B2 (ja) | 2013-06-10 | 2021-05-25 | 製造方法及びｍｄｍ２阻害剤の結晶形 |
| JP2023064715A Pending JP2023089126A (ja) | 2013-06-10 | 2023-04-12 | 製造方法及びｍｄｍ２阻害剤の結晶形 |
| JP2025029906A Pending JP2025084856A (ja) | 2013-06-10 | 2025-02-27 | 製造方法及びｍｄｍ２阻害剤の結晶形 |
Country Status (38)
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2998B1 (ar) | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
| WO2013049250A1 (en) | 2011-09-27 | 2013-04-04 | Amgen Inc. | Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer |
| US11407721B2 (en) | 2013-02-19 | 2022-08-09 | Amgen Inc. | CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer |
| MX374513B (es) | 2013-03-14 | 2025-03-06 | Amgen Inc | Compuestos de morfolinona de ácido heteroarilo como inhibidores mdm2 para el tratamiento de cáncer. |
| JOP20200296A1 (ar) * | 2013-06-10 | 2017-06-16 | Amgen Inc | عمليات صنع وأشكال بلورية من mdm2 مثبط |
| KR102305351B1 (ko) | 2013-11-11 | 2021-09-24 | 암젠 인크 | 암의 치료를 위한, mdm2 억제제 및 하나 이상의 추가적 약제학적 활성 제제를 포함하는 조합 요법 |
| CN118436801A (zh) | 2016-05-20 | 2024-08-06 | 豪夫迈·罗氏有限公司 | Protac抗体缀合物及其使用方法 |
| IL319432A (en) * | 2018-04-30 | 2025-05-01 | Kartos Therapeutics Inc | Methods of treating cancer |
| EP3801476A4 (en) * | 2018-05-25 | 2022-07-06 | Kartos Therapeutics, Inc. | METHODS OF TREATING MYELOPROLIFERATIVE NEOPLASMS |
| AU2019327555B2 (en) * | 2018-08-31 | 2025-01-16 | Amgen, Inc. | Processes for preparing a MDM2 inhibitor |
| CN110963958B (zh) * | 2018-09-30 | 2025-10-10 | 上海长森药业有限公司 | 一种mdm2抑制剂，及其制备方法、药物组合物和应用 |
| GB201919219D0 (en) | 2019-12-23 | 2020-02-05 | Otsuka Pharma Co Ltd | Cancer biomarkers |
| WO2021236474A1 (en) * | 2020-05-22 | 2021-11-25 | Merck Sharp & Dohme Corp. | Novel processes for preparing conjugates of the il-2 protein |
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| GB202103080D0 (en) | 2021-03-04 | 2021-04-21 | Otsuka Pharma Co Ltd | Cancer biomarkers |
| US12054449B2 (en) | 2021-08-05 | 2024-08-06 | Bio-Pharm Solutions Co., Ltd. | Phenylcarbamate crystalline form and method for manufacturing the same |
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| WO2023039161A1 (en) * | 2021-09-09 | 2023-03-16 | Kartos Therapeutics | Methods of treating cancer dependent on myc gene expresssion |
| WO2023056069A1 (en) | 2021-09-30 | 2023-04-06 | Angiex, Inc. | Degrader-antibody conjugates and methods of using same |
| CN115925589A (zh) * | 2022-12-26 | 2023-04-07 | 诚达药业股份有限公司 | 一种脂肪族亚磺酸钙盐及其制备方法 |
| WO2024240858A1 (en) | 2023-05-23 | 2024-11-28 | Valerio Therapeutics | Protac molecules directed against dna damage repair system and uses thereof |
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