JP2020506895A5 - - Google Patents
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- JP2020506895A5 JP2020506895A5 JP2019538180A JP2019538180A JP2020506895A5 JP 2020506895 A5 JP2020506895 A5 JP 2020506895A5 JP 2019538180 A JP2019538180 A JP 2019538180A JP 2019538180 A JP2019538180 A JP 2019538180A JP 2020506895 A5 JP2020506895 A5 JP 2020506895A5
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- Prior art keywords
- alkyl
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- membered
- compound according
- cancer
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- 150000001875 compounds Chemical class 0.000 claims 30
- 125000005842 heteroatom Chemical group 0.000 claims 26
- 229910052760 oxygen Inorganic materials 0.000 claims 25
- 229910052757 nitrogen Inorganic materials 0.000 claims 23
- 229910052717 sulfur Inorganic materials 0.000 claims 23
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 19
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 16
- 239000000651 prodrug Substances 0.000 claims 15
- 229940002612 prodrug Drugs 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- 125000000081 (C5-C8) cycloalkenyl group Chemical group 0.000 claims 4
- 101001037256 Homo sapiens Indoleamine 2,3-dioxygenase 1 Proteins 0.000 claims 4
- 102100040061 Indoleamine 2,3-dioxygenase 1 Human genes 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000006584 (C3-C10) heterocycloalkyl group Chemical group 0.000 claims 3
- 101001037261 Homo sapiens Indoleamine 2,3-dioxygenase 2 Proteins 0.000 claims 3
- 102100040062 Indoleamine 2,3-dioxygenase 2 Human genes 0.000 claims 3
- 102100040653 Tryptophan 2,3-dioxygenase Human genes 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 206010055113 Breast cancer metastatic Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 201000009036 biliary tract cancer Diseases 0.000 claims 1
- 208000020790 biliary tract neoplasm Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 1
- 230000001413 cellular effect Effects 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer 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
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 230000001394 metastastic effect Effects 0.000 claims 1
- 206010061289 metastatic neoplasm Diseases 0.000 claims 1
- 208000010658 metastatic prostate carcinoma Diseases 0.000 claims 1
- 201000002628 peritoneum cancer Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 0 C*C(*)([C@@]1C2*)[C@@]1C(*)C2*(*)=S Chemical compound C*C(*)([C@@]1C2*)[C@@]1C(*)C2*(*)=S 0.000 description 7
- RIKMMFOAQPJVMX-UHFFFAOYSA-N Cc1c[nH]nc1 Chemical compound Cc1c[nH]nc1 RIKMMFOAQPJVMX-UHFFFAOYSA-N 0.000 description 2
- NDLWRNDHOJPLTE-UHFFFAOYSA-N CC(C)Oc1ncc(C)cn1 Chemical compound CC(C)Oc1ncc(C)cn1 NDLWRNDHOJPLTE-UHFFFAOYSA-N 0.000 description 1
- QYOFIWQGXQGNMB-UHFFFAOYSA-N CCCOc1ncc(C)cn1 Chemical compound CCCOc1ncc(C)cn1 QYOFIWQGXQGNMB-UHFFFAOYSA-N 0.000 description 1
- NDLQVGMDCZDJQP-ORQPDHAQSA-O CCOC(/C=C\C(C)=N)=[NH2+] Chemical compound CCOC(/C=C\C(C)=N)=[NH2+] NDLQVGMDCZDJQP-ORQPDHAQSA-O 0.000 description 1
- KUQQONVKIURIQU-UHFFFAOYSA-N Cc(c(F)c1)ccc1C#N Chemical compound Cc(c(F)c1)ccc1C#N KUQQONVKIURIQU-UHFFFAOYSA-N 0.000 description 1
- MKFCYQTVSDCXAQ-UHFFFAOYSA-N Cc(c(F)c1)ccc1Cl Chemical compound Cc(c(F)c1)ccc1Cl MKFCYQTVSDCXAQ-UHFFFAOYSA-N 0.000 description 1
- MPXDAIBTYWGBSL-UHFFFAOYSA-N Cc(c(F)c1)ccc1F Chemical compound Cc(c(F)c1)ccc1F MPXDAIBTYWGBSL-UHFFFAOYSA-N 0.000 description 1
- WQOHEWKWIJOAHQ-UHFFFAOYSA-N Cc(c(F)c1)ccc1OC Chemical compound Cc(c(F)c1)ccc1OC WQOHEWKWIJOAHQ-UHFFFAOYSA-N 0.000 description 1
- YSNVKDGEALPJGC-UHFFFAOYSA-N Cc(cc(cc1)F)c1F Chemical compound Cc(cc(cc1)F)c1F YSNVKDGEALPJGC-UHFFFAOYSA-N 0.000 description 1
- XPUXIETZGSTMEX-UHFFFAOYSA-N Cc(cc1)cc(OCC(F)F)c1Cl Chemical compound Cc(cc1)cc(OCC(F)F)c1Cl XPUXIETZGSTMEX-UHFFFAOYSA-N 0.000 description 1
- JUXFXYQUXNXVAA-UHFFFAOYSA-N Cc(cc1)ccc1OC(F)(F)F Chemical compound Cc(cc1)ccc1OC(F)(F)F JUXFXYQUXNXVAA-UHFFFAOYSA-N 0.000 description 1
- DJDQNISEJVPQCS-UHFFFAOYSA-N Cc(cc1)ccc1OC(F)F Chemical compound Cc(cc1)ccc1OC(F)F DJDQNISEJVPQCS-UHFFFAOYSA-N 0.000 description 1
- NFQGQMBFMIIIOR-UHFFFAOYSA-N Cc(cc1)cnc1OC Chemical compound Cc(cc1)cnc1OC NFQGQMBFMIIIOR-UHFFFAOYSA-N 0.000 description 1
- WCGNLBCJPBKXCN-UHFFFAOYSA-N Cc(cc1F)ccc1C#N Chemical compound Cc(cc1F)ccc1C#N WCGNLBCJPBKXCN-UHFFFAOYSA-N 0.000 description 1
- MHXNHUSVBYUTJL-UHFFFAOYSA-N Cc(cc1F)ccc1Cl Chemical compound Cc(cc1F)ccc1Cl MHXNHUSVBYUTJL-UHFFFAOYSA-N 0.000 description 1
- FZMPLKVGINKUJZ-UHFFFAOYSA-N Cc(cc1F)ccc1F Chemical compound Cc(cc1F)ccc1F FZMPLKVGINKUJZ-UHFFFAOYSA-N 0.000 description 1
- MSQWWFRWHKYEAU-UHFFFAOYSA-N Cc(cc1OC(F)F)ccc1Cl Chemical compound Cc(cc1OC(F)F)ccc1Cl MSQWWFRWHKYEAU-UHFFFAOYSA-N 0.000 description 1
- KBRLTYHUJDMMLI-UHFFFAOYSA-N Cc(cc1OC)ccc1Cl Chemical compound Cc(cc1OC)ccc1Cl KBRLTYHUJDMMLI-UHFFFAOYSA-N 0.000 description 1
- LPVVVCBDJJRLHT-UHFFFAOYSA-N Cc(nc1)ccc1OC Chemical compound Cc(nc1)ccc1OC LPVVVCBDJJRLHT-UHFFFAOYSA-N 0.000 description 1
- LRLRAYMYEXQKID-UHFFFAOYSA-N Cc1ccc(C(F)(F)F)cc1 Chemical compound Cc1ccc(C(F)(F)F)cc1 LRLRAYMYEXQKID-UHFFFAOYSA-N 0.000 description 1
- CSDACMXHCXPONB-UHFFFAOYSA-N Cc1ccc(C)c(OCC(F)(F)F)c1 Chemical compound Cc1ccc(C)c(OCC(F)(F)F)c1 CSDACMXHCXPONB-UHFFFAOYSA-N 0.000 description 1
- TWGNOYAGHYUFFR-UHFFFAOYSA-N Cc1cncnc1 Chemical compound Cc1cncnc1 TWGNOYAGHYUFFR-UHFFFAOYSA-N 0.000 description 1
- FICAQKBMCKEFDI-UHFFFAOYSA-N Cc1n[o]c(C)c1 Chemical compound Cc1n[o]c(C)c1 FICAQKBMCKEFDI-UHFFFAOYSA-N 0.000 description 1
- XHANCLXYCNTZMM-UHFFFAOYSA-N Cc1nc2cc(C)ccc2[s]1 Chemical compound Cc1nc2cc(C)ccc2[s]1 XHANCLXYCNTZMM-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762447368P | 2017-01-17 | 2017-01-17 | |
| US62/447,368 | 2017-01-17 | ||
| US201762458777P | 2017-02-14 | 2017-02-14 | |
| US62/458,777 | 2017-02-14 | ||
| US201762528366P | 2017-07-03 | 2017-07-03 | |
| US62/528,366 | 2017-07-03 | ||
| PCT/US2018/013914 WO2018136437A2 (en) | 2017-01-17 | 2018-01-16 | Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020506895A JP2020506895A (ja) | 2020-03-05 |
| JP2020506895A5 true JP2020506895A5 (enExample) | 2021-02-25 |
Family
ID=62908947
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019538180A Pending JP2020506895A (ja) | 2017-01-17 | 2018-01-16 | インドールアミン２，３−ジオキシゲナーゼおよび／またはトリプトファンジオキシゲナーゼの阻害剤として有用な化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US11173145B2 (enExample) |
| EP (1) | EP3570832A4 (enExample) |
| JP (1) | JP2020506895A (enExample) |
| CN (1) | CN110191709A (enExample) |
| CA (1) | CA3047002A1 (enExample) |
| WO (1) | WO2018136437A2 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018136437A2 (en) | 2017-01-17 | 2018-07-26 | Tesaro, Inc. | Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase |
| EP3823604A4 (en) * | 2018-07-17 | 2022-03-16 | Board of Regents, The University of Texas System | COMPOUNDS AS INHIBITORS OF INDOLAMINE-2,3-DIOXYGENASE AND/OR TRYPTOPHANE DIOXYGENASE |
| TWI731420B (zh) | 2018-09-27 | 2021-06-21 | 大陸商深圳微芯生物科技股份有限公司 | 具有吲哚胺-2,3-雙加氧酶抑制活性的喹啉衍生物及其製備方法、藥物組合物、聯合用藥物與用途 |
| US12091405B2 (en) | 2018-11-01 | 2024-09-17 | Merck Sharp & Dohme Llc | Substituted pyrazole compounds as indoleamine 2,3-dioxygenase inhibitors |
| EP3886845B1 (en) * | 2018-11-28 | 2024-09-04 | Merck Sharp & Dohme LLC | Novel substituted piperazine amide compounds as indoleamine 2, 3-dioxygenase (ido) inhibitors |
| US11458149B1 (en) * | 2019-05-31 | 2022-10-04 | Ikena Oncology, Inc. | TEAD inhibitors and uses thereof |
| BR112021024108A2 (pt) | 2019-05-31 | 2022-03-22 | Ikena Oncology Inc | Inibidores de tead e usos dos mesmos |
| CN112107685A (zh) * | 2020-07-17 | 2020-12-22 | 深圳市第二人民医院 | 一种基于ido1酶抑制剂设计的治疗骨关节炎的方法 |
| CN115215780B (zh) * | 2022-04-22 | 2023-08-08 | 上海格苓凯生物科技有限公司 | 一种利用n,n-二琥珀酰亚胺基碳酸酯制备异双功能交联剂smcc的方法 |
| AU2023260353A1 (en) * | 2022-04-26 | 2024-11-28 | Viscient Bio, Inc. | Tryptanthrin derivatives and uses thereof |
| WO2023229024A1 (ja) * | 2022-05-27 | 2023-11-30 | 富士フイルム株式会社 | 血液腫瘍の診断を補助する方法、血液腫瘍の診断を行うためのデータを得る方法、及びこれらの方法のためのキット |
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2018
- 2018-01-16 WO PCT/US2018/013914 patent/WO2018136437A2/en not_active Ceased
- 2018-01-16 EP EP18741114.5A patent/EP3570832A4/en not_active Withdrawn
- 2018-01-16 US US16/478,076 patent/US11173145B2/en active Active
- 2018-01-16 CA CA3047002A patent/CA3047002A1/en not_active Abandoned
- 2018-01-16 JP JP2019538180A patent/JP2020506895A/ja active Pending
- 2018-01-16 CN CN201880006825.0A patent/CN110191709A/zh active Pending