JP2018529633A5 - - Google Patents
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- JP2018529633A5 JP2018529633A5 JP2018500582A JP2018500582A JP2018529633A5 JP 2018529633 A5 JP2018529633 A5 JP 2018529633A5 JP 2018500582 A JP2018500582 A JP 2018500582A JP 2018500582 A JP2018500582 A JP 2018500582A JP 2018529633 A5 JP2018529633 A5 JP 2018529633A5
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- Prior art keywords
- compound
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- cancer
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- 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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- 150000001875 compounds Chemical class 0.000 claims 53
- 125000003088 (fluoren-9-ylmethoxy)carbonyl group Chemical group 0.000 claims 27
- 125000000649 benzylidene group Chemical group [H]C(=[*])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 27
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 claims 27
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 27
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 27
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 238000000634 powder X-ray diffraction Methods 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 239000003153 chemical reaction reagent Substances 0.000 claims 6
- 239000013078 crystal Substances 0.000 claims 5
- 238000004519 manufacturing process Methods 0.000 claims 5
- XYFCBTPGUUZFHI-UHFFFAOYSA-N Phosphine Chemical compound P XYFCBTPGUUZFHI-UHFFFAOYSA-N 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 239000002585 base Substances 0.000 claims 3
- 239000003638 chemical reducing agent Substances 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 150000007529 inorganic bases Chemical class 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- USVVENVKYJZFMW-ONEGZZNKSA-N (e)-carboxyiminocarbamic acid Chemical compound OC(=O)\N=N\C(O)=O USVVENVKYJZFMW-ONEGZZNKSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 229910000073 phosphorus hydride Inorganic materials 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- CESUXLKAADQNTB-SSDOTTSWSA-N 2-methylpropane-2-sulfinamide Chemical compound CC(C)(C)[S@](N)=O CESUXLKAADQNTB-SSDOTTSWSA-N 0.000 claims 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- 206010000830 Acute leukaemia Diseases 0.000 claims 1
- 206010061424 Anal cancer Diseases 0.000 claims 1
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims 1
- 208000007860 Anus Neoplasms Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 206010006143 Brain stem glioma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010007953 Central nervous system lymphoma Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 201000001342 Fallopian tube cancer Diseases 0.000 claims 1
- 208000013452 Fallopian tube neoplasm Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010061252 Intraocular melanoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000032271 Malignant tumor of penis Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000000821 Parathyroid Neoplasms Diseases 0.000 claims 1
- 206010061336 Pelvic neoplasm Diseases 0.000 claims 1
- 208000002471 Penile Neoplasms Diseases 0.000 claims 1
- 206010034299 Penile cancer Diseases 0.000 claims 1
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims 1
- 201000005746 Pituitary adenoma Diseases 0.000 claims 1
- 206010061538 Pituitary tumour benign 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
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000023915 Ureteral Neoplasms Diseases 0.000 claims 1
- 206010046392 Ureteric cancer Diseases 0.000 claims 1
- 206010046431 Urethral cancer Diseases 0.000 claims 1
- 206010046458 Urethral neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 201000005969 Uveal melanoma Diseases 0.000 claims 1
- 206010047741 Vulval cancer Diseases 0.000 claims 1
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 201000005188 adrenal gland cancer Diseases 0.000 claims 1
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims 1
- 201000011165 anus cancer Diseases 0.000 claims 1
- 208000025997 central nervous system neoplasm Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000024207 chronic leukemia Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000030381 cutaneous melanoma Diseases 0.000 claims 1
- 239000012458 free base Substances 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
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000029559 malignant endocrine neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 208000026045 malignant tumor of parathyroid gland Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 210000000651 myofibroblast Anatomy 0.000 claims 1
- 201000002575 ocular melanoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical compound [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 claims 1
- 208000021310 pituitary gland adenoma Diseases 0.000 claims 1
- 239000000843 powder Substances 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
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000003708 skin melanoma Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 201000002510 thyroid cancer Diseases 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
- 201000005102 vulva cancer Diseases 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021069649A JP7212713B2 (ja) | 2015-07-06 | 2021-04-16 | ジアリール大環状多形 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562188846P | 2015-07-06 | 2015-07-06 | |
| US62/188,846 | 2015-07-06 | ||
| US201562218672P | 2015-09-15 | 2015-09-15 | |
| US62/218,672 | 2015-09-15 | ||
| PCT/US2016/040972 WO2017007759A1 (en) | 2015-07-06 | 2016-07-05 | Diaryl macrocycle polymorph |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021069649A Division JP7212713B2 (ja) | 2015-07-06 | 2021-04-16 | ジアリール大環状多形 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018529633A JP2018529633A (ja) | 2018-10-11 |
| JP2018529633A5 true JP2018529633A5 (enExample) | 2019-08-15 |
| JP6917974B2 JP6917974B2 (ja) | 2021-08-11 |
Family
ID=57685592
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018500582A Active JP6917974B2 (ja) | 2015-07-06 | 2016-07-05 | ジアリール大環状多形 |
| JP2021069649A Active JP7212713B2 (ja) | 2015-07-06 | 2021-04-16 | ジアリール大環状多形 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021069649A Active JP7212713B2 (ja) | 2015-07-06 | 2021-04-16 | ジアリール大環状多形 |
Country Status (24)
| Country | Link |
|---|---|
| US (5) | US10294242B2 (enExample) |
| EP (2) | EP3319969B1 (enExample) |
| JP (2) | JP6917974B2 (enExample) |
| KR (1) | KR102623734B1 (enExample) |
| CN (2) | CN108026108B (enExample) |
| AU (1) | AU2016289454B2 (enExample) |
| BR (1) | BR112018000297A2 (enExample) |
| CA (1) | CA2990020C (enExample) |
| DK (1) | DK3319969T3 (enExample) |
| ES (1) | ES2979111T3 (enExample) |
| FI (1) | FI3319969T3 (enExample) |
| HR (1) | HRP20240780T1 (enExample) |
| HU (1) | HUE067352T2 (enExample) |
| IL (2) | IL256443B (enExample) |
| LT (1) | LT3319969T (enExample) |
| MX (2) | MX386680B (enExample) |
| PL (1) | PL3319969T3 (enExample) |
| PT (1) | PT3319969T (enExample) |
| RS (1) | RS65593B1 (enExample) |
| RU (1) | RU2765181C2 (enExample) |
| SI (1) | SI3319969T1 (enExample) |
| SM (1) | SMT202400213T1 (enExample) |
| WO (1) | WO2017007759A1 (enExample) |
| ZA (1) | ZA201708436B (enExample) |
Families Citing this family (19)
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| AU2015209239C1 (en) | 2014-01-24 | 2026-05-07 | Turning Point Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| MX2017017097A (es) | 2015-07-02 | 2018-05-23 | Tp Therapeutics Inc | Macrociclos diarílicos quirales como moduladores de proteínas quinasas. |
| PL3319969T3 (pl) * | 2015-07-06 | 2024-06-24 | Turning Point Therapeutics, Inc. | Diarylowe polimorfy makrocykliczne |
| LT3733187T (lt) * | 2015-07-21 | 2024-12-10 | Turning Point Therapeutics, Inc. | Chiralinis diarilo makrociklas ir jo panaudojimas vėžio gydymui |
| RU2019105587A (ru) | 2016-07-28 | 2020-08-28 | Тёрнинг Поинт Терапьютикс, Инк. | Макроциклические ингибиторы киназ |
| TWI808958B (zh) * | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| CN107586796B (zh) * | 2017-07-20 | 2021-08-06 | 暨明医药科技（苏州）有限公司 | (r)-2-(1-氨基乙基)-4-氟苯酚的合成方法 |
| CA3069232A1 (en) | 2017-07-28 | 2019-01-31 | Turning Point Therapeutics, Inc. | Macrocyclic compounds and uses thereof |
| HUE060711T2 (hu) | 2017-12-19 | 2023-04-28 | Turning Point Therapeutics Inc | Makrociklusos vegyületek betegségek kezelésére |
| CN110386944B (zh) * | 2018-04-16 | 2021-10-29 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白激酶活性的二(杂)芳基大环化合物 |
| HRP20250048T1 (hr) | 2018-10-22 | 2025-03-28 | Alumis Inc. | Inhibitori tyk2 i njihova uporaba |
| WO2020233645A1 (zh) | 2019-05-21 | 2020-11-26 | 浙江海正药业股份有限公司 | 大环类衍生物、及其制备方法和用途 |
| US20220411439A1 (en) * | 2019-06-19 | 2022-12-29 | Turning Point Therapeutics, Inc. | Polymorphs of a macrocyclic kinase inhibitor |
| TW202133856A (zh) * | 2019-11-27 | 2021-09-16 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| JP7670711B2 (ja) * | 2019-11-27 | 2025-04-30 | ターニング・ポイント・セラピューティクス・インコーポレイテッド | ジアリール大環状化合物を含む併用療法 |
| BR112022017425A2 (pt) * | 2020-03-02 | 2022-11-29 | Turning Point Therapeutics Inc | Usos terapêuticos de compostos macrocíclicos |
| CN113620974B (zh) * | 2020-05-08 | 2023-01-31 | 山东轩竹医药科技有限公司 | 大环类酪氨酸激酶抑制剂的晶型及其制备方法 |
| CN112174982A (zh) * | 2020-09-10 | 2021-01-05 | 上海希迈医药科技有限公司 | 一种洛普替尼晶型及其制备方法 |
| WO2025217347A2 (en) | 2024-04-11 | 2025-10-16 | Bristol-Myers Squibb Company | Process of preparing repotrectinib |
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2016
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