JP2020500916A5 - - Google Patents
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- Publication number
- JP2020500916A5 JP2020500916A5 JP2019531149A JP2019531149A JP2020500916A5 JP 2020500916 A5 JP2020500916 A5 JP 2020500916A5 JP 2019531149 A JP2019531149 A JP 2019531149A JP 2019531149 A JP2019531149 A JP 2019531149A JP 2020500916 A5 JP2020500916 A5 JP 2020500916A5
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- JP
- Japan
- Prior art keywords
- compound according
- alkoxy
- alkyl
- bond
- salt
- 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
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- 150000001875 compounds Chemical class 0.000 claims 31
- 125000003545 alkoxy group Chemical group 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 19
- -1 azetidine-1-yl Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 239000011780 sodium chloride Substances 0.000 claims 10
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 5
- 125000004429 atoms Chemical group 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 5
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 239000005977 Ethylene Substances 0.000 claims 2
- 102000000562 Monocarboxylic Acid Transporters Human genes 0.000 claims 2
- 101710032195 SLC16A3 Proteins 0.000 claims 2
- 102100007163 SLC16A3 Human genes 0.000 claims 2
- 101710032196 SLC16A4 Proteins 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 101700050207 mctC Proteins 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 230000000240 adjuvant Effects 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000002609 media Substances 0.000 claims 1
- 0 CC(CC1)CN1c1c(CCN(C(*)C2)NC2C=C)cccc1 Chemical compound CC(CC1)CN1c1c(CCN(C(*)C2)NC2C=C)cccc1 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662433113P | 2016-12-12 | 2016-12-12 | |
| US62/433,113 | 2016-12-12 | ||
| PCT/US2017/065864 WO2018111904A1 (en) | 2016-12-12 | 2017-12-12 | Heterocyclic inhibitors of mct4 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020500916A JP2020500916A (ja) | 2020-01-16 |
| JP2020500916A5 true JP2020500916A5 (US07794700-20100914-C00152.png) | 2021-01-28 |
| JP7123929B2 JP7123929B2 (ja) | 2022-08-23 |
Family
ID=62488735
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019531149A Active JP7123929B2 (ja) | 2016-12-12 | 2017-12-12 | Ｍｃｔ４の複素環阻害剤 |
Country Status (13)
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10202350B2 (en) | 2015-06-12 | 2019-02-12 | Vettore, LLC | MCT4 inhibitors for treating disease |
| BR112019011825A2 (pt) | 2016-12-12 | 2019-10-22 | Vettore Llc | composto, enantiômero isolado, composição farmacêutica, método para inibir a atividade do transportador de monocarboxilato mct4, ou um mutante do mesmo, em uma amostra biológica, método para inibir a atividade do transportador de monocarboxilato mct4, ou um mutante do mesmo, em relação ao transportador de monocarboxilato mct1, ou um mutante do mesmo, em um paciente, método para tratar um distúrbio mediado por transportador de monocarboxilato mct4 em um sujeito que necessite do mesmo, uso de um composto e método para obter um efeito em um paciente |
| JPWO2019188456A1 (ja) * | 2018-03-26 | 2021-03-18 | 学校法人 川崎学園 | 新規抗腫瘍剤 |
| CN111423377B (zh) * | 2020-05-12 | 2021-06-01 | 中国药科大学 | 5-氨基-1h-吡唑衍生物、制备方法及医药用途 |
| WO2021249969A1 (en) * | 2020-06-10 | 2021-12-16 | Merck Patent Gmbh | Combination product for the treatment of cancer diseases |
| WO2022243573A1 (en) | 2021-05-21 | 2022-11-24 | Cemm - Forschungszentrum Für Molekulare Medizin Gmbh | 1,2,4-triazolo[1,5-a]pyrimidine-based slc16a3 inhibitors and their therapeutic use |
| WO2022243574A1 (en) | 2021-05-21 | 2022-11-24 | Cemm - Forschungszentrum Für Molekulare Medizin Gmbh | 3-(phthalazin-1-yl)benzenesulfonamide-based slc16a3 inhibitors and their therapeutic use |
| WO2023211938A1 (en) * | 2022-04-25 | 2023-11-02 | Cyteir Therapeutics, Inc. | Methods of using a (thiazolyl)benzenesulfonamide derivative |
| WO2024036243A2 (en) * | 2022-08-10 | 2024-02-15 | Vettore, LLC | Salts of heterocyclic inhibitors of monocarboxylate transporter 4 for the treatment of disease |
| WO2024031445A1 (en) * | 2022-08-10 | 2024-02-15 | Vettore, LLC | Methods and processes for the preparation of mct4 inhibitors |
| CN118001272A (zh) * | 2022-11-08 | 2024-05-10 | 中山大学 | 吲唑类化合物在治疗炎症小体激活介导的疾病中的应用 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1052111B (it) | 1972-02-29 | 1981-06-20 | Acraf | Acidi i benzil i h indazol 3 carbossilici sostituiti e loro derivati |
| ES2037739T3 (es) * | 1986-10-22 | 1993-07-01 | Ciba-Geigy Ag | Derivados del acido 1,5-difenilpirazol-3-carboxilico para la proteccion de plantas de cultivo. |
| FR2742148B1 (fr) | 1995-12-08 | 1999-10-22 | Sanofi Sa | Nouveaux derives du pyrazole-3-carboxamide, procede pour leur preparation et compositions pharmaceutiques les contenant |
| IT1293795B1 (it) | 1997-07-28 | 1999-03-10 | Angelini Ricerche Spa | Farmaco attivo nel ridurre la produzione di proteina mcp-1 |
| EP1697744A1 (en) | 2003-11-21 | 2006-09-06 | AstraZeneca AB | Screening method |
| ES2425578T3 (es) | 2006-02-28 | 2013-10-16 | Dart Neuroscience (Cayman) Ltd | Compuestos terapéuticos |
| TWI339205B (en) * | 2006-10-02 | 2011-03-21 | Nat Health Research Institutes | Pyrazole compounds and pharmaceutical composition |
| WO2009109618A2 (en) * | 2008-03-07 | 2009-09-11 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | Novel 1-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of mcp-1, cx3cr1 and p40 |
| CN102093341B (zh) | 2009-12-10 | 2013-07-24 | 天津药物研究院 | 吲哚环取代的吡唑羧酸类内皮素受体拮抗剂及其制备方法和用途 |
| US20130190324A1 (en) * | 2011-12-23 | 2013-07-25 | The Regents Of The University Of Colorado, A Body Corporate | Topical ocular drug delivery |
| EP2804852A2 (en) * | 2012-01-20 | 2014-11-26 | Regents Of The University Of Minnesota | Therapeutic compounds |
| US10085987B2 (en) * | 2012-01-27 | 2018-10-02 | Thomas Jefferson University | MCT protein inhibitor-related prognostic and therapeutic methods |
| PT2882715T (pt) | 2012-05-18 | 2016-12-30 | Sanofi Sa | Derivados de pirazol e seu uso como antagonistas de lpar5 |
| WO2014028803A1 (en) * | 2012-08-16 | 2014-02-20 | Janssen Pharmaceutica Nv | Substituted pyrazoles as n-type calcium channel blockers |
| US20160115146A1 (en) * | 2013-06-07 | 2016-04-28 | Universite Catholique De Louvain | 3-carboxy substituted coumarin derivatives with a potential utility for the treatment of cancer diseases |
| AU2015273934B2 (en) * | 2014-06-10 | 2020-08-20 | 3B Pharmaceuticals Gmbh | Conjugate comprising a neurotensin receptor ligand and use thereof |
| US10202350B2 (en) * | 2015-06-12 | 2019-02-12 | Vettore, LLC | MCT4 inhibitors for treating disease |
| BR112019011825A2 (pt) | 2016-12-12 | 2019-10-22 | Vettore Llc | composto, enantiômero isolado, composição farmacêutica, método para inibir a atividade do transportador de monocarboxilato mct4, ou um mutante do mesmo, em uma amostra biológica, método para inibir a atividade do transportador de monocarboxilato mct4, ou um mutante do mesmo, em relação ao transportador de monocarboxilato mct1, ou um mutante do mesmo, em um paciente, método para tratar um distúrbio mediado por transportador de monocarboxilato mct4 em um sujeito que necessite do mesmo, uso de um composto e método para obter um efeito em um paciente |
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2017
- 2017-12-12 BR BR112019011825A patent/BR112019011825A2/pt unknown
- 2017-12-12 US US15/839,539 patent/US10214492B2/en active Active
- 2017-12-12 CA CA3046212A patent/CA3046212A1/en active Pending
- 2017-12-12 MX MX2019006893A patent/MX2019006893A/es unknown
- 2017-12-12 EP EP17880801.0A patent/EP3551625B1/en active Active
- 2017-12-12 JP JP2019531149A patent/JP7123929B2/ja active Active
- 2017-12-12 KR KR1020197019870A patent/KR102615828B1/ko active IP Right Grant
- 2017-12-12 WO PCT/US2017/065864 patent/WO2018111904A1/en active Application Filing
- 2017-12-12 AU AU2017375960A patent/AU2017375960B2/en active Active
- 2017-12-12 CN CN201780081025.0A patent/CN110114351B/zh active Active
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2018
- 2018-12-17 US US16/222,949 patent/US11292767B2/en active Active
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2019
- 2019-06-06 PH PH12019501261A patent/PH12019501261A1/en unknown
- 2019-06-10 IL IL267183A patent/IL267183A/en unknown
- 2019-07-10 ZA ZA2019/04522A patent/ZA201904522B/en unknown
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2021
- 2021-01-04 IL IL279949A patent/IL279949A/en unknown
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2022
- 2022-02-22 US US17/652,022 patent/US20220251047A1/en active Pending
