JP2018505880A5 - - Google Patents
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- JP2018505880A5 JP2018505880A5 JP2017540856A JP2017540856A JP2018505880A5 JP 2018505880 A5 JP2018505880 A5 JP 2018505880A5 JP 2017540856 A JP2017540856 A JP 2017540856A JP 2017540856 A JP2017540856 A JP 2017540856A JP 2018505880 A5 JP2018505880 A5 JP 2018505880A5
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- Prior art keywords
- cancer
- hydroxy
- methyl
- alkoxy
- alkyl
- 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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- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 14
- 206010028980 Neoplasm Diseases 0.000 claims description 12
- 125000003545 alkoxy group Chemical group 0.000 claims description 12
- 150000001875 compounds Chemical class 0.000 claims description 11
- 125000000217 alkyl group Chemical group 0.000 claims description 10
- 201000011510 cancer Diseases 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 230000002265 prevention Effects 0.000 claims description 9
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 5
- 229910052736 halogen Inorganic materials 0.000 claims description 5
- 150000002367 halogens Chemical class 0.000 claims description 5
- 125000003282 alkyl amino group Chemical group 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 239000001257 hydrogen Substances 0.000 claims description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 2
- 125000004171 alkoxy aryl group Chemical group 0.000 claims description 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 2
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims 15
- 125000001424 substituent group Chemical group 0.000 claims 8
- -1 2-hydroxy-phenyl Chemical group 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 6
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- XSBJQWNBBMWICJ-UHFFFAOYSA-N 2-[6-[methyl-(2,2,6,6-tetramethylpiperidin-4-yl)amino]pyridazin-3-yl]-5-(1H-pyrazol-4-yl)phenol Chemical compound C=1C=C(C=2C(=CC(=CC=2)C2=CNN=C2)O)N=NC=1N(C)C1CC(C)(C)NC(C)(C)C1 XSBJQWNBBMWICJ-UHFFFAOYSA-N 0.000 claims 1
- ZWVAEWAYWBRRLZ-UHFFFAOYSA-N 3-[6-(2,2,6,6-tetramethylpiperidin-4-yl)oxypyridazin-3-yl]naphthalene-2,7-diol Chemical compound C1C(C)(C)NC(C)(C)CC1OC1=CC=C(C=2C(=CC3=CC(O)=CC=C3C=2)O)N=N1 ZWVAEWAYWBRRLZ-UHFFFAOYSA-N 0.000 claims 1
- IUIYZTQPJTUDPK-UHFFFAOYSA-N 3-[6-[methyl-(2,2,6,6-tetramethylpiperidin-4-yl)amino]pyridazin-3-yl]naphthalen-2-ol Chemical compound C=1C=C(C=2C(=CC3=CC=CC=C3C=2)O)N=NC=1N(C)C1CC(C)(C)NC(C)(C)C1 IUIYZTQPJTUDPK-UHFFFAOYSA-N 0.000 claims 1
- ANRDBHZBYHYNDL-UHFFFAOYSA-N 3-[6-[methyl-(2,2,6,6-tetramethylpiperidin-4-yl)amino]pyridazin-3-yl]naphthalene-2,7-diol Chemical compound C=1C=C(C=2C(=CC3=CC(O)=CC=C3C=2)O)N=NC=1N(C)C1CC(C)(C)NC(C)(C)C1 ANRDBHZBYHYNDL-UHFFFAOYSA-N 0.000 claims 1
- QTUJFHJUHDTZFB-UHFFFAOYSA-N 3-hydroxy-4-[6-[methyl-(2,2,6,6-tetramethylpiperidin-4-yl)amino]pyridazin-3-yl]benzonitrile Chemical compound C=1C=C(C=2C(=CC(=CC=2)C#N)O)N=NC=1N(C)C1CC(C)(C)NC(C)(C)C1 QTUJFHJUHDTZFB-UHFFFAOYSA-N 0.000 claims 1
- AUAALGSREBBOGE-UHFFFAOYSA-N 5-(1-methylpyrazol-4-yl)-2-[6-[methyl-(2,2,6,6-tetramethylpiperidin-4-yl)amino]pyridazin-3-yl]phenol Chemical compound C=1C=C(C=2C(=CC(=CC=2)C2=CN(C)N=C2)O)N=NC=1N(C)C1CC(C)(C)NC(C)(C)C1 AUAALGSREBBOGE-UHFFFAOYSA-N 0.000 claims 1
- STWTUEAWRAIWJG-UHFFFAOYSA-N 5-(1H-pyrazol-4-yl)-2-[6-(2,2,6,6-tetramethylpiperidin-4-yl)oxypyridazin-3-yl]phenol Chemical compound C1C(C)(C)NC(C)(C)CC1OC1=CC=C(C=2C(=CC(=CC=2)C2=CNN=C2)O)N=N1 STWTUEAWRAIWJG-UHFFFAOYSA-N 0.000 claims 1
- BCRSNYZJXWMFBJ-UHFFFAOYSA-N 7-methoxy-3-[6-[methyl-(2,2,6,6-tetramethylpiperidin-4-yl)amino]pyridazin-3-yl]naphthalen-2-ol Chemical compound OC1=CC2=CC(OC)=CC=C2C=C1C(N=N1)=CC=C1N(C)C1CC(C)(C)NC(C)(C)C1 BCRSNYZJXWMFBJ-UHFFFAOYSA-N 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 206010000871 Acute monocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis 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
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000035489 Monocytic Acute Leukemia Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia 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
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma 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
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 208000002517 adenoid cystic carcinoma Diseases 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 229940126523 co-drug Drugs 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 230000000112 colonic effect Effects 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 208000030381 cutaneous melanoma Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 210000000214 mouth Anatomy 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 210000000653 nervous system Anatomy 0.000 claims 1
- 238000011275 oncology therapy Methods 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 201000005825 prostate adenocarcinoma Diseases 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 201000006845 reticulosarcoma Diseases 0.000 claims 1
- 208000029922 reticulum cell sarcoma Diseases 0.000 claims 1
- 201000007416 salivary gland adenoid cystic carcinoma Diseases 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 201000003708 skin melanoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- OVNPTSMJFITONH-UHFFFAOYSA-N Bc1ccc(-c2cc3ccc(C)cc3cc2O)nn1 Chemical compound Bc1ccc(-c2cc3ccc(C)cc3cc2O)nn1 OVNPTSMJFITONH-UHFFFAOYSA-N 0.000 description 1
- 150000002431 hydrogen Chemical class 0.000 description 1
- 239000003607 modifier Substances 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15154342.8A EP3053577A1 (en) | 2015-02-09 | 2015-02-09 | Compounds for the treatment of cancer |
| EP15154342.8 | 2015-02-09 | ||
| EP15155286.6 | 2015-02-16 | ||
| EP15155286 | 2015-02-16 | ||
| PCT/EP2016/052597 WO2016128343A1 (en) | 2015-02-09 | 2016-02-08 | Compounds for the treatment of cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018505880A JP2018505880A (ja) | 2018-03-01 |
| JP2018505880A5 true JP2018505880A5 (enExample) | 2021-04-08 |
| JP6884102B2 JP6884102B2 (ja) | 2021-06-09 |
Family
ID=55305013
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017540856A Active JP6884102B2 (ja) | 2015-02-09 | 2016-02-08 | がんの治療のための化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US20170001995A1 (enExample) |
| EP (1) | EP3256126B1 (enExample) |
| JP (1) | JP6884102B2 (enExample) |
| CN (1) | CN107428729B (enExample) |
| WO (1) | WO2016128343A1 (enExample) |
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| CN105392790B (zh) | 2013-08-19 | 2019-04-19 | 豪夫迈·罗氏有限公司 | 4H-吡啶并[1,2-a]嘧啶-4-酮化合物制备用于预防或治疗癌症的药物的用途 |
| GB201410693D0 (en) | 2014-06-16 | 2014-07-30 | Univ Southampton | Splicing modulation |
| AU2015327836B2 (en) | 2014-10-03 | 2021-07-01 | Cold Spring Harbor Laboratory | Targeted augmentation of nuclear gene output |
| US10668171B2 (en) | 2015-05-30 | 2020-06-02 | Ptc Therapeutics, Inc. | Methods for modulating RNA splicing |
| EP3359685A1 (en) | 2015-10-09 | 2018-08-15 | University Of Southampton | Modulation of gene expression and screening for deregulated protein expression |
| CN113750101A (zh) * | 2015-12-10 | 2021-12-07 | Ptc医疗公司 | 用于治疗亨廷顿病的方法 |
| ES2882500T3 (es) | 2015-12-14 | 2021-12-02 | Cold Spring Harbor Laboratory | Oligómeros antisentido para el tratamiento del síndrome de Dravet |
| US11096956B2 (en) | 2015-12-14 | 2021-08-24 | Stoke Therapeutics, Inc. | Antisense oligomers and uses thereof |
| EA201991309A1 (ru) | 2016-11-28 | 2019-11-29 | Способы модуляции сплайсинга рнк | |
| US11407753B2 (en) | 2017-06-05 | 2022-08-09 | Ptc Therapeutics, Inc. | Compounds for treating Huntington's disease |
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| KR20210135239A (ko) * | 2019-02-05 | 2021-11-12 | 스카이호크 테라퓨틱스, 인코포레이티드 | 스플라이싱을 조절하는 방법 및 조성물 |
| WO2020163541A1 (en) * | 2019-02-05 | 2020-08-13 | Skyhawk Therapeutics, Inc. | Methods and compositions for modulating splicing |
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| JP7603594B2 (ja) * | 2019-02-06 | 2024-12-20 | スカイホーク・セラピューティクス・インコーポレーテッド | スプライシングを調節するための方法および組成物 |
| KR20210135507A (ko) | 2019-02-06 | 2021-11-15 | 스카이호크 테라퓨틱스, 인코포레이티드 | 스플라이싱을 조절하는 방법 및 조성물 |
| UY38687A (es) * | 2019-05-17 | 2023-05-15 | Novartis Ag | Inhibidores del inflamasoma nlrp3, composiciones, combinaciones de los mismos y métodos para su uso |
| US11129829B2 (en) | 2019-06-17 | 2021-09-28 | Skyhawk Therapeutics, Inc. | Methods for modulating splicing |
| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
| US20230148184A1 (en) | 2020-02-28 | 2023-05-11 | Remix Therapeutics Inc. | Compounds and methods for modulating splicing |
| WO2021174176A1 (en) * | 2020-02-28 | 2021-09-02 | Remix Therapeutics Inc. | Pyridazine dervatives for modulating nucleic acid splicing |
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| AU2021270720A1 (en) | 2020-05-11 | 2022-12-08 | Stoke Therapeutics, Inc. | OPA1 antisense oligomers for treatment of conditions and diseases |
| TW202216710A (zh) | 2020-07-02 | 2022-05-01 | 美商雷密克斯醫療公司 | 調節剪接之化合物及方法 |
| JP2023532331A (ja) | 2020-07-02 | 2023-07-27 | リミックス セラピューティクス インコーポレイテッド | 核酸をスプライシングするため及び増殖性疾患を処置するための修飾因子としての５－［５－（ピペリジン－４－イル）チエノ［３，２－ｃ］ピラゾール－２－イル］インダゾール誘導体及び関連する化合物並びにスプライシングを調節するための化合物及び方法 |
| CN112716946B (zh) * | 2021-01-22 | 2022-02-08 | 中国人民解放军陆军军医大学 | 磺内酰胺-环己酮螺环衍生物1-3-51在制备治疗胃癌药物中的应用 |
| EP4396177A1 (en) | 2021-08-30 | 2024-07-10 | Remix Therapeutics Inc. | Compounds and methods for modulating splicing |
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| KR20240096913A (ko) | 2021-08-30 | 2024-06-26 | 레믹스 테라퓨틱스 인크. | 스플라이싱 조절을 위한 화합물 및 방법 |
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| EP4416156A1 (en) | 2021-10-13 | 2024-08-21 | Remix Therapeutics Inc. | Compounds and methods for modulating nucleic acid splicing |
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| US8729263B2 (en) * | 2012-08-13 | 2014-05-20 | Novartis Ag | 1,4-disubstituted pyridazine analogs there of and methods for treating SMN-deficiency-related conditions |
| HK1213909A1 (zh) * | 2013-01-11 | 2016-07-15 | Novartis Ag | 通過調節melk治療乳腺癌 |
| US9040712B2 (en) * | 2013-01-23 | 2015-05-26 | Novartis Ag | Thiadiazole analogs thereof and methods for treating SMN-deficiency-related-conditions |
| MX2020011652A (es) * | 2013-07-31 | 2022-09-27 | Novartis Ag | Derivados de piridazina 1,4-disustituida, y su uso para el tratamiento de afecciones relacionadas con la deficiencia de smn. |
| CN103965169A (zh) * | 2014-05-30 | 2014-08-06 | 彭正中 | 一种化合物及其制备方法与用途 |
-
2016
- 2016-02-08 CN CN201680019434.3A patent/CN107428729B/zh active Active
- 2016-02-08 WO PCT/EP2016/052597 patent/WO2016128343A1/en not_active Ceased
- 2016-02-08 EP EP16703164.0A patent/EP3256126B1/en active Active
- 2016-02-08 JP JP2017540856A patent/JP6884102B2/ja active Active
- 2016-02-09 US US15/019,135 patent/US20170001995A1/en not_active Abandoned
-
2017
- 2017-12-21 US US15/851,188 patent/US11066400B2/en active Active
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