JP2018515525A5 - - Google Patents
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- Publication number
- JP2018515525A5 JP2018515525A5 JP2017559003A JP2017559003A JP2018515525A5 JP 2018515525 A5 JP2018515525 A5 JP 2018515525A5 JP 2017559003 A JP2017559003 A JP 2017559003A JP 2017559003 A JP2017559003 A JP 2017559003A JP 2018515525 A5 JP2018515525 A5 JP 2018515525A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- substituted
- cycloalkyl
- hydrogen
- 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
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 129
- 229910052739 hydrogen Inorganic materials 0.000 claims 78
- 239000001257 hydrogen Substances 0.000 claims 78
- 150000002431 hydrogen Chemical class 0.000 claims 67
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 51
- -1 CD 3 Chemical class 0.000 claims 43
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 37
- 229910052736 halogen Inorganic materials 0.000 claims 36
- 150000002367 halogens Chemical class 0.000 claims 36
- 125000001072 heteroaryl group Chemical group 0.000 claims 34
- 125000003107 substituted aryl group Chemical group 0.000 claims 30
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 25
- 125000000623 heterocyclic group Chemical group 0.000 claims 24
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 23
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 19
- 125000004093 cyano group Chemical group *C#N 0.000 claims 18
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 9
- 238000006243 chemical reaction Methods 0.000 claims 9
- 229920001577 copolymer Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 125000001188 haloalkyl group Chemical group 0.000 claims 8
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 8
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 6
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 4
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 4
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 4
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 4
- 206010009944 Colon cancer Diseases 0.000 claims 4
- 208000034578 Multiple myelomas Diseases 0.000 claims 4
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 4
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 4
- 206010041067 Small cell lung cancer Diseases 0.000 claims 4
- 208000029742 colonic neoplasm Diseases 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 4
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 3
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims 1
- 102000001805 Bromodomains Human genes 0.000 claims 1
- 108050009021 Bromodomains Proteins 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 229940125763 bromodomain inhibitor Drugs 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- WMSPXQIQBQAWLL-UHFFFAOYSA-N cyclopropanesulfonamide Chemical compound NS(=O)(=O)C1CC1 WMSPXQIQBQAWLL-UHFFFAOYSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 0 CC(C)c1c(*)nn[n]1 Chemical compound CC(C)c1c(*)nn[n]1 0.000 description 25
- JPDPRXXLFYTTRV-UHFFFAOYSA-N CC(C)c1c(C)[o]nc1C Chemical compound CC(C)c1c(C)[o]nc1C JPDPRXXLFYTTRV-UHFFFAOYSA-N 0.000 description 4
- VTYLNNZBVOSGTA-UHFFFAOYSA-N CC(C)c([n](C)nn1)c1OC Chemical compound CC(C)c([n](C)nn1)c1OC VTYLNNZBVOSGTA-UHFFFAOYSA-N 0.000 description 3
- DWVFSQVBDSMYJA-UHFFFAOYSA-N CC(C)c([nH]nn1)c1OC Chemical compound CC(C)c([nH]nn1)c1OC DWVFSQVBDSMYJA-UHFFFAOYSA-N 0.000 description 2
- FMSYGTJKIDOBPH-UHFFFAOYSA-N CCc1c(C(C)C)[nH]nn1 Chemical compound CCc1c(C(C)C)[nH]nn1 FMSYGTJKIDOBPH-UHFFFAOYSA-N 0.000 description 2
- MRFNWSQNINZIIA-UHFFFAOYSA-O CC(C)C1=C(C)N(C)N[NH2+]1 Chemical compound CC(C)C1=C(C)N(C)N[NH2+]1 MRFNWSQNINZIIA-UHFFFAOYSA-O 0.000 description 1
- VSNWPYLQRCUJJC-UHFFFAOYSA-O CC(C)C1=C(C)N=N[NH2+]1 Chemical compound CC(C)C1=C(C)N=N[NH2+]1 VSNWPYLQRCUJJC-UHFFFAOYSA-O 0.000 description 1
- MMTJVWTXKUNWCZ-UHFFFAOYSA-N CC(C)c1c(C)nn[n]1C Chemical compound CC(C)c1c(C)nn[n]1C MMTJVWTXKUNWCZ-UHFFFAOYSA-N 0.000 description 1
- UJKAFNFFPBCHLA-UHFFFAOYSA-N CCC1=C(C(C)C)NNN1C Chemical compound CCC1=C(C(C)C)NNN1C UJKAFNFFPBCHLA-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562159991P | 2015-05-12 | 2015-05-12 | |
| US62/159,991 | 2015-05-12 | ||
| US15/150,492 US9725449B2 (en) | 2015-05-12 | 2016-05-10 | Tricyclic compounds as anticancer agents |
| US15/150,492 | 2016-05-10 | ||
| PCT/US2016/031707 WO2016183118A1 (en) | 2015-05-12 | 2016-05-11 | Tricyclic compounds as anticancer agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018515525A JP2018515525A (ja) | 2018-06-14 |
| JP2018515525A5 true JP2018515525A5 (enExample) | 2019-06-13 |
| JP6843767B2 JP6843767B2 (ja) | 2021-03-17 |
Family
ID=56117957
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017559003A Active JP6843767B2 (ja) | 2015-05-12 | 2016-05-11 | 抗がん剤としての三環式化合物 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US9725449B2 (enExample) |
| EP (1) | EP3294739B1 (enExample) |
| JP (1) | JP6843767B2 (enExample) |
| CN (1) | CN107709322B (enExample) |
| ES (1) | ES2746131T3 (enExample) |
| TW (1) | TW201713657A (enExample) |
| UY (1) | UY36677A (enExample) |
| WO (1) | WO2016183118A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102238012B1 (ko) * | 2016-01-20 | 2021-04-09 | 닝보 웬다 파르마 테크놀로지 엘티디 | 브로모도메인 억제제인 카르볼린 유도체 |
| US20190040063A1 (en) * | 2016-02-05 | 2019-02-07 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Tricyclic compound for bromodomain-containing protein inhibitor and preparation pharmaceutical composition, and application thereof |
| WO2019080941A1 (en) * | 2017-10-27 | 2019-05-02 | Jacobio-Beta Pharmaceuticals Co., Ltd. | NEW TRICYCLIC COMPOUNDS |
| EP4227302A1 (en) | 2018-02-13 | 2023-08-16 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| MX2020014111A (es) * | 2018-06-25 | 2021-06-15 | Jacobio Pharmaceuticals Co Ltd | Compuestos triciclicos. |
| UA126421C2 (uk) | 2018-07-13 | 2022-09-28 | Гіліад Сайєнсіз, Інк. | Інгібітори pd-1/pd-l1 |
| WO2020200284A1 (zh) * | 2019-04-04 | 2020-10-08 | 上海华汇拓医药科技有限公司 | 三环类化合物制备方法及其在医药领域的应用 |
| US10947253B2 (en) | 2019-08-05 | 2021-03-16 | Ankh Life Sciences Limited | Fused polycyclic dimers |
| JP2023500213A (ja) * | 2019-10-30 | 2023-01-05 | ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー | ３－ニトロ－ｎ－（２，２，２－トリフルオロエチル）－４－ピリジンアミンの合成 |
| US12129265B2 (en) | 2020-07-21 | 2024-10-29 | Ankh Life Sciences Limited | Therapeutic agents and uses thereof |
| JP2024506260A (ja) * | 2021-01-22 | 2024-02-13 | ジンルイ バイオファーマ カンパニー リミテッド | 抗がん剤としての三環式化合物 |
| WO2024099441A1 (en) * | 2022-11-11 | 2024-05-16 | Jingrui Biopharma (Shandong) Co., Ltd. | Bromodomain and extra-terminal (bet) protein degrader |
| US12173005B1 (en) | 2023-12-21 | 2024-12-24 | King Faisal University | Pyrimido[1′,6′:1,5]pyrazolo[4,3-b][1,7]naphthyridine compounds as CK2 inhibitors |
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| SE504828C2 (sv) | 1990-04-11 | 1997-05-12 | Sandvik Ab | Hammaranordning där kolv och borrkrona har omvänd design relativt varandra vad gäller impedans |
| TWI309240B (en) | 2004-09-17 | 2009-05-01 | Hoffmann La Roche | Anti-ox40l antibodies |
| ES2432091T5 (es) | 2005-03-25 | 2022-03-18 | Gitr Inc | Moléculas de unión GITR y usos de las mismas |
| EP2559690B1 (en) | 2005-05-10 | 2016-03-30 | Incyte Holdings Corporation | Modulators of indoleamine 2,3-dioxygenase and methods of using the same |
| EA019344B1 (ru) | 2005-07-01 | 2014-03-31 | МЕДАРЕКС, Эл.Эл.Си. | Человеческие моноклональные антитела против лиганда-1 запрограммированной гибели клеток (pd-l1) и их применения |
| TWI382974B (zh) | 2005-12-20 | 2013-01-21 | 英塞特公司 | 作為吲哚胺２，３-二氧化酶調節劑之ｎ-羥基甲脒基雜環化物 |
| US7696166B2 (en) | 2006-03-28 | 2010-04-13 | Albany Molecular Research, Inc. | Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders |
| CL2007002650A1 (es) | 2006-09-19 | 2008-02-08 | Incyte Corp | Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras. |
| WO2008036642A2 (en) | 2006-09-19 | 2008-03-27 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
| EP1987839A1 (en) | 2007-04-30 | 2008-11-05 | I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale | Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease |
| PT2175884T (pt) | 2007-07-12 | 2016-09-21 | Gitr Inc | Terapias de combinação empregando moléculas de ligação a gitr |
| EP2044949A1 (en) | 2007-10-05 | 2009-04-08 | Immutep | Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response |
| EP2227233B1 (en) | 2007-11-30 | 2013-02-13 | Newlink Genetics | Ido inhibitors |
| BRPI0821209A2 (pt) * | 2007-12-19 | 2019-09-24 | Amgen Inc | composto, composição farmacêutica, métodos de tratar câncer, para reduzir o tamanho de tumor, para tratar distúrbios, e para reduzir metástase em um tumor. |
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| EP2358825A1 (en) | 2008-12-18 | 2011-08-24 | E. I. du Pont de Nemours and Company | Powder coating composition with new pigment |
| RU2595409C2 (ru) | 2009-09-03 | 2016-08-27 | Мерк Шарп И Доум Корп., | Анти-gitr-антитела |
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| SI2510010T1 (sl) | 2009-12-10 | 2016-02-29 | F. Hoffmann-La Roche Ag | Protitelesa, vezavna na ekstracelično domeno 4 humanega csf1r in njihova uporaba |
| PE20170779A1 (es) | 2010-03-04 | 2017-07-04 | Macrogenics Inc | Anticuerpos reactivos con b7-h3, fragmentos inmunologicamente activos de los mismos y usos de los mismos |
| JP2013521765A (ja) | 2010-03-05 | 2013-06-13 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | ヒトｃｓｆ−１ｒに対する抗体及びその使用 |
| RU2617966C2 (ru) | 2010-03-05 | 2017-04-28 | Ф.Хоффманн-Ля Рош Аг | Антитела против csf-1r человека и их применение |
| HRP20190047T1 (hr) | 2010-05-04 | 2019-02-22 | Five Prime Therapeutics, Inc. | Protutijela koja se vežu na csf1r |
| PH12013500395B1 (en) | 2010-09-09 | 2020-10-16 | Pfizer | 4-1bb binding molecules |
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| NO2694640T3 (enExample) | 2011-04-15 | 2018-03-17 | ||
| RS57324B1 (sr) | 2011-04-20 | 2018-08-31 | Medimmune Llc | Antitela i drugi molekuli koji vezuju b7-h1 i pd-1 |
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| AR091649A1 (es) | 2012-07-02 | 2015-02-18 | Bristol Myers Squibb Co | Optimizacion de anticuerpos que se fijan al gen de activacion de linfocitos 3 (lag-3) y sus usos |
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| UA115576C2 (uk) | 2012-12-06 | 2017-11-27 | Байєр Фарма Акцієнгезелльшафт | Похідні бензимідазолу як антагоністи ер4 |
| US9492460B2 (en) | 2013-02-27 | 2016-11-15 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
| CN105189488B (zh) | 2013-02-27 | 2018-07-24 | 百时美施贵宝公司 | 用作溴区结构域抑制剂的咔唑化合物 |
| JP6401773B2 (ja) | 2013-03-11 | 2018-10-10 | ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン | Ｂｅｔブロモドメイン阻害剤およびこれを用いる治療方法 |
| SI3466949T1 (sl) | 2013-12-24 | 2021-03-31 | Bristol-Myers Squibb Company | Triciklična spojina kot sredstvo proti raku |
| US9458156B2 (en) | 2014-12-23 | 2016-10-04 | Bristol-Myers Squibb Company | Tricyclic compounds as anticancer agents |
| US10662193B2 (en) | 2014-01-21 | 2020-05-26 | Ac Immune Sa | Carbazole and carboline compounds for use in the diagnosis, treatment, alleviation or prevention of disorders associated with amyloid or amyloid-like proteins |
| EP3110818B1 (en) | 2014-02-28 | 2019-10-23 | The Regents of The University of Michigan | 9h-pyrimido[4,5-b]indoles and related analogs as bet bromodomain inhibitors |
-
2016
- 2016-05-10 US US15/150,492 patent/US9725449B2/en active Active
- 2016-05-11 CN CN201680039269.8A patent/CN107709322B/zh active Active
- 2016-05-11 UY UY0001036677A patent/UY36677A/es unknown
- 2016-05-11 TW TW105114608A patent/TW201713657A/zh unknown
- 2016-05-11 WO PCT/US2016/031707 patent/WO2016183118A1/en not_active Ceased
- 2016-05-11 EP EP16728765.5A patent/EP3294739B1/en active Active
- 2016-05-11 JP JP2017559003A patent/JP6843767B2/ja active Active
- 2016-05-11 ES ES16728765T patent/ES2746131T3/es active Active