JP2018516994A5 - - Google Patents
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- Publication number
- JP2018516994A5 JP2018516994A5 JP2018516405A JP2018516405A JP2018516994A5 JP 2018516994 A5 JP2018516994 A5 JP 2018516994A5 JP 2018516405 A JP2018516405 A JP 2018516405A JP 2018516405 A JP2018516405 A JP 2018516405A JP 2018516994 A5 JP2018516994 A5 JP 2018516994A5
- Authority
- JP
- Japan
- Prior art keywords
- salt
- cancer
- alkyl
- halo
- alkoxy
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims 46
- 150000003839 salts Chemical class 0.000 claims 43
- 125000003545 alkoxy group Chemical group 0.000 claims 26
- 125000005843 halogen group Chemical group 0.000 claims 26
- 125000000217 alkyl group Chemical group 0.000 claims 25
- 125000001188 haloalkyl group Chemical group 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 16
- -1 cyano, hydroxy Chemical group 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 125000003282 alkyl amino group Chemical group 0.000 claims 14
- 125000004438 haloalkoxy group Chemical group 0.000 claims 14
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 13
- 239000008194 pharmaceutical composition Substances 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 125000003342 alkenyl group Chemical group 0.000 claims 10
- 101000577126 Homo sapiens Monocarboxylate transporter 4 Proteins 0.000 claims 9
- 101000577129 Homo sapiens Monocarboxylate transporter 5 Proteins 0.000 claims 9
- 102100025276 Monocarboxylate transporter 4 Human genes 0.000 claims 9
- 102000000562 Monocarboxylic Acid Transporters Human genes 0.000 claims 9
- 101710204259 Monocarboxylic acid transporter Proteins 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 208000035475 disorder Diseases 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 6
- 230000001404 mediated effect Effects 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 230000002062 proliferating effect Effects 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- 101000937642 Homo sapiens Malonyl-CoA-acyl carrier protein transacylase, mitochondrial Proteins 0.000 claims 2
- 101000590830 Homo sapiens Monocarboxylate transporter 1 Proteins 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 102100034068 Monocarboxylate transporter 1 Human genes 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 125000003368 amide group Chemical group 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 229940124530 sulfonamide Drugs 0.000 claims 2
- 150000003456 sulfonamides Chemical class 0.000 claims 2
- 208000016683 Adult T-cell leukemia/lymphoma 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
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 201000010915 Glioblastoma multiforme 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
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 208000005615 Interstitial Cystitis Diseases 0.000 claims 1
- 208000005016 Intestinal Neoplasms Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010023825 Laryngeal cancer Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 1
- 208000034578 Multiple myelomas 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
- 208000009565 Pharyngeal Neoplasms Diseases 0.000 claims 1
- 206010034811 Pharyngeal cancer Diseases 0.000 claims 1
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma 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
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis 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
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 206010043515 Throat cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 201000006966 adult T-cell leukemia Diseases 0.000 claims 1
- 125000006323 alkenyl amino group Chemical group 0.000 claims 1
- 125000005021 aminoalkenyl group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 201000000053 blastoma Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000008184 embryoma Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 208000024519 eye neoplasm Diseases 0.000 claims 1
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 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
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 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
- 239000000203 mixture Substances 0.000 claims 1
- 201000006938 muscular dystrophy Diseases 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 210000000653 nervous system Anatomy 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008106 ocular cancer Diseases 0.000 claims 1
- 208000027500 optic nerve neoplasm Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000010916 pituitary tumor 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
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000002314 small intestine cancer Diseases 0.000 claims 1
- 206010062261 spinal cord neoplasm Diseases 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 206010044412 transitional cell carcinoma Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 208000037964 urogenital 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
- 0 CC*C1**(CCN)*(C)N(*)CC1 Chemical compound CC*C1**(CCN)*(C)N(*)CC1 0.000 description 4
- DSCSGSGYDAITAF-UHFFFAOYSA-N CC(C)(C(O)=O)OCc1n[n](Cc(cccc2)c2Cl)c(-c2cc(F)ccc2)c1 Chemical compound CC(C)(C(O)=O)OCc1n[n](Cc(cccc2)c2Cl)c(-c2cc(F)ccc2)c1 DSCSGSGYDAITAF-UHFFFAOYSA-N 0.000 description 1
- FZEGIMRSYFQOHT-UHFFFAOYSA-N CC(C)(C(O)O)OCc1n[n](Cc(cccc2)c2Cl)c(-c2cc(C)ccc2)c1 Chemical compound CC(C)(C(O)O)OCc1n[n](Cc(cccc2)c2Cl)c(-c2cc(C)ccc2)c1 FZEGIMRSYFQOHT-UHFFFAOYSA-N 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021102860A JP2021152056A (ja) | 2015-06-12 | 2021-06-22 | 疾患を治療するためのｍｃｔ４阻害剤 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562174685P | 2015-06-12 | 2015-06-12 | |
| US62/174,685 | 2015-06-12 | ||
| PCT/US2016/037213 WO2016201426A1 (en) | 2015-06-12 | 2016-06-13 | Mct4 inhibitors for treating disease |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021102860A Division JP2021152056A (ja) | 2015-06-12 | 2021-06-22 | 疾患を治療するためのｍｃｔ４阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018516994A JP2018516994A (ja) | 2018-06-28 |
| JP2018516994A5 true JP2018516994A5 (enExample) | 2019-07-18 |
| JP6944442B2 JP6944442B2 (ja) | 2021-10-06 |
Family
ID=57504734
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018516405A Active JP6944442B2 (ja) | 2015-06-12 | 2016-06-13 | 疾患を治療するためのｍｃｔ４阻害剤 |
| JP2021102860A Pending JP2021152056A (ja) | 2015-06-12 | 2021-06-22 | 疾患を治療するためのｍｃｔ４阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021102860A Pending JP2021152056A (ja) | 2015-06-12 | 2021-06-22 | 疾患を治療するためのｍｃｔ４阻害剤 |
Country Status (11)
| Country | Link |
|---|---|
| US (6) | US10202350B2 (enExample) |
| EP (2) | EP3307068B1 (enExample) |
| JP (2) | JP6944442B2 (enExample) |
| KR (1) | KR102653599B1 (enExample) |
| CN (1) | CN107635404B (enExample) |
| AU (2) | AU2016277126A1 (enExample) |
| BR (1) | BR112017026535B1 (enExample) |
| CA (1) | CA2988983A1 (enExample) |
| ES (1) | ES2894919T3 (enExample) |
| IL (2) | IL256206A (enExample) |
| WO (1) | WO2016201426A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2016277126A1 (en) | 2015-06-12 | 2017-12-14 | Vettore, LLC | MCT4 inhibitors for treating disease |
| CN110114351B (zh) | 2016-12-12 | 2022-09-20 | 维托尔股份有限公司 | Mct4的杂环抑制剂 |
| AU2019317518B2 (en) | 2018-04-25 | 2023-05-25 | Charles R. Drew University Of Medicine And Science | Novel MCT4 inhibitors and uses thereof |
| TWI823932B (zh) * | 2018-05-11 | 2023-12-01 | 中國大陸商迪哲（江蘇）醫藥有限公司 | 三唑并嘧啶化合物及其在治療癌症中之用途 |
| WO2020127960A1 (en) | 2018-12-21 | 2020-06-25 | Merck Patent Gmbh | Disubstituted alkyne derivatives |
| WO2020234454A1 (en) | 2019-05-23 | 2020-11-26 | Deutsches Krebsforschungszentrum | Combination treatment of cancer targeting energy metabolism and intracellular ph |
| US20210214731A1 (en) * | 2019-10-25 | 2021-07-15 | President And Fellows Of Harvard College | Methods for treating cancer |
| 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 |
| CN113929627A (zh) * | 2021-10-19 | 2022-01-14 | 吕梁学院 | 一种宾达利的合成方法 |
| CN113845476B (zh) * | 2021-11-08 | 2024-04-30 | 中国药科大学 | 一种喹诺酮衍生物及其制备方法和用途 |
| JP2025526689A (ja) * | 2022-08-10 | 2025-08-15 | ベットーレ リミテッド ライアビリティー カンパニー | Ｍｃｔ４阻害剤を調製する方法及びプロセス |
Family Cites Families (21)
| 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 |
| DE3775527D1 (de) | 1986-10-22 | 1992-02-06 | Ciba Geigy Ag | 1,5-diphenylpyrazol-3-carbonsaeurederivate zum schuetzen von kulturpflanzen. |
| 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 |
| WO2005054852A1 (en) | 2003-11-21 | 2005-06-16 | Astrazeneca Ab | Screening method |
| JP5503874B2 (ja) | 2006-02-28 | 2014-05-28 | ダート ニューロサイエンス （ケイマン） エルティーディー | 治療化合物 |
| TWI339205B (en) | 2006-10-02 | 2011-03-21 | Nat Health Research Institutes | Pyrazole compounds and pharmaceutical composition |
| KR101581828B1 (ko) | 2008-03-07 | 2015-12-31 | 아지엔드 키미쉐 리유나이트 안젤리니 프란체스코 에이.씨.알.에이.에프. 에스.피.에이 | 신규한 1-벤질-3-하이드록시메틸인다졸 유도체들 및 ｍｃｐ-1, ｃｘ3ｃｒ1 및 ｐ40의 발현을 기초로 한 질환들의 치료에서 이의 용도 |
| 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 |
| WO2012024543A1 (en) * | 2010-08-18 | 2012-02-23 | Caris Life Sciences Luxembourg Holdings | Circulating biomarkers for disease |
| 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 |
| JP6257596B2 (ja) * | 2012-05-18 | 2018-01-10 | サノフイ | ピラゾール誘導体およびｌｐａｒ５アンタゴニストとしてのその使用 |
| MX2015002038A (es) | 2012-08-16 | 2016-01-22 | Janssen Pharmaceutica Nv | Pirazoles sustituidos como bloqueadores del canal de calcio tipo n. |
| WO2014195507A1 (en) * | 2013-06-07 | 2014-12-11 | 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 |
| DE202015003905U1 (de) | 2015-06-05 | 2016-09-12 | Rudolf King | Methode zur Übermittlung und Differenzierung von Verfassungszuständen während und nach Auslösen eines persönlichen Notfallsystems oder Systems zur Mitteilung an ein soziales Notfallsystem oder Systems zur Mitteilung an ein soziales Notfall-Netzwerk |
| WO2016201416A1 (en) | 2015-06-11 | 2016-12-15 | Cequent Performance Products Inc. | Roof rack crossbar assembly |
| AU2016277126A1 (en) * | 2015-06-12 | 2017-12-14 | Vettore, LLC | MCT4 inhibitors for treating disease |
| CN110114351B (zh) | 2016-12-12 | 2022-09-20 | 维托尔股份有限公司 | Mct4的杂环抑制剂 |
-
2016
- 2016-06-13 AU AU2016277126A patent/AU2016277126A1/en not_active Abandoned
- 2016-06-13 EP EP16808515.7A patent/EP3307068B1/en active Active
- 2016-06-13 JP JP2018516405A patent/JP6944442B2/ja active Active
- 2016-06-13 US US15/180,623 patent/US10202350B2/en active Active
- 2016-06-13 ES ES16808515T patent/ES2894919T3/es active Active
- 2016-06-13 KR KR1020187000674A patent/KR102653599B1/ko active Active
- 2016-06-13 CN CN201680034104.1A patent/CN107635404B/zh active Active
- 2016-06-13 EP EP21191357.9A patent/EP3942934A1/en active Pending
- 2016-06-13 BR BR112017026535-4A patent/BR112017026535B1/pt active IP Right Grant
- 2016-06-13 WO PCT/US2016/037213 patent/WO2016201426A1/en not_active Ceased
- 2016-06-13 CA CA2988983A patent/CA2988983A1/en active Pending
-
2017
- 2017-12-10 IL IL256206A patent/IL256206A/en unknown
-
2018
- 2018-12-17 US US16/222,964 patent/US20190112274A1/en not_active Abandoned
-
2020
- 2020-09-23 US US17/030,243 patent/US11155522B2/en active Active
- 2020-10-22 IL IL278247A patent/IL278247B/en unknown
-
2021
- 2021-02-12 AU AU2021200919A patent/AU2021200919B2/en active Active
- 2021-06-22 JP JP2021102860A patent/JP2021152056A/ja active Pending
- 2021-09-22 US US17/481,660 patent/US11724989B2/en active Active
-
2023
- 2023-06-19 US US18/337,313 patent/US12187682B2/en active Active
-
2024
- 2024-11-25 US US18/958,610 patent/US20250257039A1/en active Pending