JP2018532786A5 - - Google Patents
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- JP2018532786A5 JP2018532786A5 JP2018541572A JP2018541572A JP2018532786A5 JP 2018532786 A5 JP2018532786 A5 JP 2018532786A5 JP 2018541572 A JP2018541572 A JP 2018541572A JP 2018541572 A JP2018541572 A JP 2018541572A JP 2018532786 A5 JP2018532786 A5 JP 2018532786A5
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- cancer
- compound
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- 150000001875 compounds Chemical class 0.000 claims 43
- 125000000217 alkyl group Chemical group 0.000 claims 29
- 125000005843 halogen group Chemical group 0.000 claims 27
- 239000008194 pharmaceutical composition Substances 0.000 claims 16
- 206010028980 Neoplasm Diseases 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- -1 R a1 Chemical group 0.000 claims 11
- 201000011510 cancer Diseases 0.000 claims 11
- 239000003814 drug Substances 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 229940124597 therapeutic agent Drugs 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 7
- 239000013066 combination product Substances 0.000 claims 6
- 229940127555 combination product Drugs 0.000 claims 6
- 208000036142 Viral infection Diseases 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 125000002950 monocyclic group Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 5
- 230000009385 viral infection Effects 0.000 claims 5
- 239000002671 adjuvant Substances 0.000 claims 4
- 239000000969 carrier Substances 0.000 claims 4
- 239000003085 diluting agent Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000003054 catalyst Substances 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 3
- 230000002489 hematologic effect Effects 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 239000002904 solvent Substances 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010024612 Lipoma Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- DRTQHJPVMGBUCF-XVFCMESISA-N Uridine Chemical group O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-XVFCMESISA-N 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 206010016629 fibroma Diseases 0.000 claims 2
- 201000011066 hemangioma Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 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 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 201000003076 Angiosarcoma Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma 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
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 201000005262 Chondroma Diseases 0.000 claims 1
- 208000010126 Chondromatosis Diseases 0.000 claims 1
- 208000019591 Chondromyxoid fibroma Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 201000009047 Chordoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010058314 Dysplasia Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 201000001342 Fallopian tube cancer Diseases 0.000 claims 1
- 208000013452 Fallopian tube neoplasm Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 1
- 208000007569 Giant Cell Tumors Diseases 0.000 claims 1
- 208000002927 Hamartoma Diseases 0.000 claims 1
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 1
- 206010019629 Hepatic adenoma Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000002260 Keloid Diseases 0.000 claims 1
- 206010023330 Keloid scar Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims 1
- 208000002404 Liver Cell Adenoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 229940083338 MDM2 inhibitor Drugs 0.000 claims 1
- 239000012819 MDM2-Inhibitor Substances 0.000 claims 1
- 208000006644 Malignant Fibrous Histiocytoma Diseases 0.000 claims 1
- 208000015021 Meningeal Neoplasms Diseases 0.000 claims 1
- 206010027406 Mesothelioma 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
- NEHMBGOWUSGTLI-OAHLLOKOSA-N N-[(4R)-1-(2,4-difluorophenyl)-4,5,6,7-tetrahydroindazol-4-yl]-2-pyridinecarboxamide Chemical compound FC1=CC(F)=CC=C1N1C(CCC[C@H]2NC(=O)C=3N=CC=CC=3)=C2C=N1 NEHMBGOWUSGTLI-OAHLLOKOSA-N 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000009905 Neurofibromatoses Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 208000000035 Osteochondroma 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
- 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
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000005678 Rhabdomyoma Diseases 0.000 claims 1
- 208000032383 Soft tissue cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 206010043276 Teratoma Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 208000015778 Undifferentiated pleomorphic sarcoma 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
- 206010047741 Vulval cancer Diseases 0.000 claims 1
- 208000004354 Vulvar Neoplasms Diseases 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 210000004100 adrenal gland Anatomy 0.000 claims 1
- DRTQHJPVMGBUCF-PSQAKQOGSA-N beta-L-uridine Natural products O[C@H]1[C@@H](O)[C@H](CO)O[C@@H]1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-PSQAKQOGSA-N 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 201000006491 bone marrow cancer Diseases 0.000 claims 1
- 201000002143 bronchus adenoma Diseases 0.000 claims 1
- 210000000845 cartilage Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 210000001612 chondrocyte Anatomy 0.000 claims 1
- 238000011260 co-administration Methods 0.000 claims 1
- 230000002500 effect on skin Effects 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 208000006359 hepatoblastoma Diseases 0.000 claims 1
- 201000002735 hepatocellular adenoma Diseases 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 210000001117 keloid Anatomy 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 208000022006 malignant tumor of meninges Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000009091 myxoma Diseases 0.000 claims 1
- 201000011682 nervous system cancer Diseases 0.000 claims 1
- 201000004931 neurofibromatosis Diseases 0.000 claims 1
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims 1
- 229960001346 nilotinib Drugs 0.000 claims 1
- 239000002777 nucleoside Substances 0.000 claims 1
- 125000003835 nucleoside group Chemical group 0.000 claims 1
- 239000002773 nucleotide Substances 0.000 claims 1
- 125000003729 nucleotide group Chemical group 0.000 claims 1
- 208000003388 osteoid osteoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000047 product Substances 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000001839 skull cancer Diseases 0.000 claims 1
- 201000002314 small intestine cancer Diseases 0.000 claims 1
- 201000011096 spinal cancer Diseases 0.000 claims 1
- 208000014618 spinal cord cancer Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- DRTQHJPVMGBUCF-UHFFFAOYSA-N uracil arabinoside Natural products OC1C(O)C(CO)OC1N1C(=O)NC(=O)C=C1 DRTQHJPVMGBUCF-UHFFFAOYSA-N 0.000 claims 1
- 229940045145 uridine Drugs 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
- GTDYESQZZZLIFZ-MRXNPFEDSA-N O=C(c1c(CCCC2)[n]2cn1)N[C@H](CCC1)c2c1[n](-c(cccc1)c1F)nc2 Chemical compound O=C(c1c(CCCC2)[n]2cn1)N[C@H](CCC1)c2c1[n](-c(cccc1)c1F)nc2 GTDYESQZZZLIFZ-MRXNPFEDSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE1551410 | 2015-11-02 | ||
| SE1551410-2 | 2015-11-02 | ||
| GBGB1610823.5A GB201610823D0 (en) | 2016-06-21 | 2016-06-21 | Heterocyclic compounds and medical uses |
| GB1610823.5 | 2016-06-21 | ||
| PCT/GB2016/053383 WO2017077280A1 (en) | 2015-11-02 | 2016-11-01 | Tetrahydroindazoles and medical uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018532786A JP2018532786A (ja) | 2018-11-08 |
| JP2018532786A5 true JP2018532786A5 (https=) | 2019-12-12 |
| JP6859358B2 JP6859358B2 (ja) | 2021-04-14 |
Family
ID=57482465
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018541572A Active JP6859358B2 (ja) | 2015-11-02 | 2016-11-01 | テトラヒドロインダゾール及びその医学的使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US10889564B2 (https=) |
| EP (2) | EP3974424A1 (https=) |
| JP (1) | JP6859358B2 (https=) |
| CN (1) | CN108349947B (https=) |
| ES (1) | ES2895904T3 (https=) |
| WO (1) | WO2017077280A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2895904T3 (es) | 2015-11-02 | 2022-02-23 | Genase Therapeutics B V | Tetrahidroindazoles y usos médicos de los mismos |
| JP7542538B2 (ja) | 2018-09-18 | 2024-08-30 | ニカング セラピューティクス， インコーポレイテッド | Ｓｒｃホモロジー－２ホスファターゼ阻害剤としての縮合三環式環誘導体 |
| GB202013558D0 (en) * | 2020-08-28 | 2020-10-14 | Heptares Therapeutics Ltd | GRP52 Modularor compounds |
| CN118946568A (zh) | 2022-01-27 | 2024-11-12 | 格纳赛治疗有限公司 | 用于治疗癌症和病毒感染的四氢吡喃并吡唑衍生物 |
| IL305348B2 (en) * | 2023-08-20 | 2024-08-01 | Selene Therapeutics LTD | DHODH inhibitors penetrate the blood-brain barrier and their uses |
| WO2026062223A1 (en) | 2024-09-20 | 2026-03-26 | Prinses Máxima Centrum Voor Kinderoncologie B.V. | Use of dhodh-inhibitors for the treatment of cmarcb1 -mutant associated cancer |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2651939T1 (sl) | 2010-12-13 | 2015-07-31 | Array Biopharma, Inc. | SUBSTITUIRANE N-(1H-INDAZOL-4-IL)IMIDAZO(1,2-a)PIRIDIN-3-KARBOKSAMIDNE SPOJINE KOT INHIBITORJI RECEPTORSKE TIROZINSKE KINAZE TIPA III |
| WO2013078413A1 (en) * | 2011-11-22 | 2013-05-30 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Modulators of lipid storage |
| LV14476B (lv) | 2011-12-07 | 2012-05-20 | Rīgas Tehniskā Universitāte | Bioloģiski aktīvu 4-acilamino-4,5,6,7-tetrahidroindazolu sintēze |
| EP2929883A1 (en) | 2014-04-08 | 2015-10-14 | Institut Pasteur | Pyrazole derivatives as dihydroorotate dehydrogenase (DHODH) inhibitors |
| ES2895904T3 (es) | 2015-11-02 | 2022-02-23 | Genase Therapeutics B V | Tetrahidroindazoles y usos médicos de los mismos |
-
2016
- 2016-11-01 ES ES16805882T patent/ES2895904T3/es active Active
- 2016-11-01 WO PCT/GB2016/053383 patent/WO2017077280A1/en not_active Ceased
- 2016-11-01 EP EP21203472.2A patent/EP3974424A1/en active Pending
- 2016-11-01 JP JP2018541572A patent/JP6859358B2/ja active Active
- 2016-11-01 EP EP16805882.4A patent/EP3371172B1/en active Active
- 2016-11-01 CN CN201680063929.6A patent/CN108349947B/zh active Active
- 2016-11-01 US US15/772,650 patent/US10889564B2/en active Active
-
2021
- 2021-01-08 US US17/144,673 patent/US11795157B2/en active Active
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