JP2018537486A5 - - Google Patents
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- JP2018537486A5 JP2018537486A5 JP2018530880A JP2018530880A JP2018537486A5 JP 2018537486 A5 JP2018537486 A5 JP 2018537486A5 JP 2018530880 A JP2018530880 A JP 2018530880A JP 2018530880 A JP2018530880 A JP 2018530880A JP 2018537486 A5 JP2018537486 A5 JP 2018537486A5
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- JP
- Japan
- Prior art keywords
- cancer
- diffraction pattern
- ray powder
- powder diffraction
- theta
- 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.)
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- 239000013078 crystal Substances 0.000 claims description 66
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 62
- 206010028980 Neoplasm Diseases 0.000 claims description 41
- 201000011510 cancer Diseases 0.000 claims description 41
- 210000004027 cell Anatomy 0.000 claims description 23
- 239000000203 mixture Substances 0.000 claims description 20
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 18
- 238000001757 thermogravimetry curve Methods 0.000 claims description 18
- 102000036365 BRCA1 Human genes 0.000 claims description 15
- 108700020463 BRCA1 Proteins 0.000 claims description 15
- 102000052609 BRCA2 Human genes 0.000 claims description 15
- 108700020462 BRCA2 Proteins 0.000 claims description 15
- 150000001875 compounds Chemical class 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 11
- 230000005782 double-strand break Effects 0.000 claims description 9
- 230000006801 homologous recombination Effects 0.000 claims description 9
- 238000002744 homologous recombination Methods 0.000 claims description 9
- 206010009944 Colon cancer Diseases 0.000 claims description 8
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 8
- 150000003278 haem Chemical group 0.000 claims description 8
- 230000002950 deficient Effects 0.000 claims description 7
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 7
- 230000035772 mutation Effects 0.000 claims description 6
- 230000006780 non-homologous end joining Effects 0.000 claims description 6
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 5
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims description 4
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 4
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 4
- 208000006168 Ewing Sarcoma Diseases 0.000 claims description 4
- 208000008839 Kidney Neoplasms 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
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- 206010038389 Renal cancer Diseases 0.000 claims description 4
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 4
- 201000010881 cervical cancer Diseases 0.000 claims description 4
- 208000029742 colonic neoplasm Diseases 0.000 claims description 4
- 230000007547 defect Effects 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 201000010536 head and neck cancer Diseases 0.000 claims description 4
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 4
- 201000010235 heart cancer Diseases 0.000 claims description 4
- 208000024348 heart neoplasm Diseases 0.000 claims description 4
- 201000010982 kidney cancer Diseases 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 201000007270 liver cancer Diseases 0.000 claims description 4
- 208000014018 liver neoplasm Diseases 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 201000010453 lymph node cancer Diseases 0.000 claims description 4
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 3
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 3
- 230000001419 dependent effect Effects 0.000 claims description 3
- 229940049920 malate Drugs 0.000 claims description 3
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 3
- 230000037361 pathway Effects 0.000 claims description 3
- SJJCQDRGABAVBB-UHFFFAOYSA-N 1-hydroxy-2-naphthoic acid Chemical compound C1=CC=CC2=C(O)C(C(=O)O)=CC=C21 SJJCQDRGABAVBB-UHFFFAOYSA-N 0.000 claims description 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 2
- 102100025064 Cellular tumor antigen p53 Human genes 0.000 claims description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 2
- 108091081406 G-quadruplex Proteins 0.000 claims description 2
- 229910019142 PO4 Inorganic materials 0.000 claims description 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 150000002148 esters Chemical class 0.000 claims description 2
- 150000003840 hydrochlorides Chemical class 0.000 claims description 2
- 239000002955 immunomodulating agent Substances 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 2
- 239000010452 phosphate Substances 0.000 claims description 2
- 238000001959 radiotherapy Methods 0.000 claims description 2
- 201000000849 skin cancer Diseases 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims description 2
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims description 2
- AEMOLEFTQBMNLQ-AQKNRBDQSA-N D-glucopyranuronic acid Chemical compound OC1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-AQKNRBDQSA-N 0.000 claims 1
- OFOBLEOULBTSOW-UHFFFAOYSA-L Malonate Chemical compound [O-]C(=O)CC([O-])=O OFOBLEOULBTSOW-UHFFFAOYSA-L 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- 229940077388 benzenesulfonate Drugs 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical group OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 1
- 229940097042 glucuronate Drugs 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 1
- 238000000034 method Methods 0.000 description 29
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 230000002062 proliferating effect Effects 0.000 description 2
- 239000005711 Benzoic acid Substances 0.000 description 1
- AEMOLEFTQBMNLQ-AQKNRBDQSA-M D-glucopyranuronate Chemical compound OC1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O AEMOLEFTQBMNLQ-AQKNRBDQSA-M 0.000 description 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical class OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 1
- 235000010233 benzoic acid Nutrition 0.000 description 1
- 230000004663 cell proliferation Effects 0.000 description 1
- 150000001860 citric acid derivatives Chemical class 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-N ethanesulfonic acid Chemical class CCS(O)(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-N 0.000 description 1
- 150000002690 malonic acid derivatives Chemical class 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-M methanesulfonate group Chemical class CS(=O)(=O)[O-] AFVFQIVMOAPDHO-UHFFFAOYSA-M 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 150000003890 succinate salts Chemical class 0.000 description 1
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/US2015/065443 WO2017105382A1 (en) | 2015-12-14 | 2015-12-14 | Crystalline forms of quinolone analogs and their salts |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020144658A Division JP2020189888A (ja) | 2020-08-28 | 2020-08-28 | キノロン類似体及びその塩の結晶形 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018537486A JP2018537486A (ja) | 2018-12-20 |
| JP2018537486A5 true JP2018537486A5 (https=) | 2019-02-07 |
Family
ID=59057173
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018530880A Withdrawn JP2018537486A (ja) | 2015-12-14 | 2015-12-14 | キノロン類似体及びその塩の結晶形 |
Country Status (10)
| Country | Link |
|---|---|
| EP (2) | EP4249072A3 (https=) |
| JP (1) | JP2018537486A (https=) |
| KR (1) | KR20180111797A (https=) |
| CN (1) | CN108699083A (https=) |
| AU (2) | AU2015417382A1 (https=) |
| CA (2) | CA3006502A1 (https=) |
| ES (1) | ES2959536T3 (https=) |
| IL (1) | IL260004A (https=) |
| RU (1) | RU2018124599A (https=) |
| WO (1) | WO2017105382A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112334133A (zh) * | 2018-02-15 | 2021-02-05 | 生华生物科技股份有限公司 | 喹诺酮类似物及其盐、组合物及其使用方法 |
| CA3129722A1 (en) * | 2019-02-11 | 2020-08-20 | Phoenix Molecular Designs | Crystalline forms of an rsk inhibitor |
| CA3151116A1 (en) * | 2019-08-14 | 2021-02-18 | Hshiou-Ting Liu | Crystalline forms of quinoline analogs and salts thereof, compositions, and their methods for use |
| EP4013421A4 (en) * | 2019-08-14 | 2023-08-23 | Senhwa Biosciences, Inc. | TETRACYCLIC COMPOUNDS AND THEIR SALTS, COMPOSITIONS AND METHODS OF USE |
| JP2020189888A (ja) * | 2020-08-28 | 2020-11-26 | センワ バイオサイエンシズ インコーポレイテッド | キノロン類似体及びその塩の結晶形 |
| CN118005653B (zh) * | 2023-04-23 | 2024-12-10 | 信义核新(北京)生物科技有限公司 | 喹诺酮类似物及其用途 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006034113A2 (en) * | 2004-09-17 | 2006-03-30 | Cylene Pharmaceuticals, Inc. | Quinolone analogs as cell proliferation inhibitors |
| JP2009504192A (ja) * | 2005-08-19 | 2009-02-05 | サイリーン ファーマシューティカルズ インコーポレーティッド | ヒトリボソームＤＮＡ（ｒＤＮＡ）およびリボソームＲＮＡ（ｒＲＮＡ）核酸ならびにそれらの使用 |
| US7928100B2 (en) | 2007-10-05 | 2011-04-19 | Cylene Pharmaceuticals, Inc. | Quinolone analogs and methods related thereto |
| US20140086839A1 (en) * | 2011-03-17 | 2014-03-27 | Tel Hashomer Medical Research Infrastructure And Services Ltd. | Quinolone analogs for treating autoimmune diseases |
| ES2754207T3 (es) * | 2013-11-28 | 2020-04-16 | Tel Hashomer Medical Res Infrastructure & Services Ltd | Inhibidores de la ARN polimerasa I y usos de los mismos |
-
2015
- 2015-12-14 JP JP2018530880A patent/JP2018537486A/ja not_active Withdrawn
- 2015-12-14 CN CN201580085777.5A patent/CN108699083A/zh active Pending
- 2015-12-14 CA CA3006502A patent/CA3006502A1/en active Pending
- 2015-12-14 CA CA3255938A patent/CA3255938A1/en active Pending
- 2015-12-14 EP EP23188399.2A patent/EP4249072A3/en active Pending
- 2015-12-14 KR KR1020187020110A patent/KR20180111797A/ko not_active Ceased
- 2015-12-14 AU AU2015417382A patent/AU2015417382A1/en not_active Abandoned
- 2015-12-14 WO PCT/US2015/065443 patent/WO2017105382A1/en not_active Ceased
- 2015-12-14 EP EP15910869.5A patent/EP3394070B1/en active Active
- 2015-12-14 RU RU2018124599A patent/RU2018124599A/ru unknown
- 2015-12-14 ES ES15910869T patent/ES2959536T3/es active Active
-
2018
- 2018-06-13 IL IL260004A patent/IL260004A/en unknown
-
2021
- 2021-05-14 AU AU2021203085A patent/AU2021203085B2/en active Active
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