JPWO2021133748A5 - - Google Patents
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- Publication number
- JPWO2021133748A5 JPWO2021133748A5 JP2022538818A JP2022538818A JPWO2021133748A5 JP WO2021133748 A5 JPWO2021133748 A5 JP WO2021133748A5 JP 2022538818 A JP2022538818 A JP 2022538818A JP 2022538818 A JP2022538818 A JP 2022538818A JP WO2021133748 A5 JPWO2021133748 A5 JP WO2021133748A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- cycloalkyl
- och
- 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.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims 51
- 229910052799 carbon Inorganic materials 0.000 claims 20
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 14
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 13
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 13
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 11
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 9
- -1 cyanocyclopropyl Chemical group 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- COXKNKHXVAHVPA-UHFFFAOYSA-N 6-fluoro-4-[4-[(3-fluoro-5-methylphenyl)methyl]piperazin-1-yl]-1-methyl-3-pyridin-4-ylquinolin-2-one Chemical compound FC=1C=C2C(=C(C(N(C2=CC=1)C)=O)C1=CC=NC=C1)N1CCN(CC1)CC1=CC(=CC(=C1)C)F COXKNKHXVAHVPA-UHFFFAOYSA-N 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000002757 morpholinyl group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- PBZCKZMEAGILKI-UHFFFAOYSA-N 4-(4-benzyl-3-oxopiperazin-1-yl)-6-fluoro-1-methyl-3-nitroquinolin-2-one Chemical compound C(C1=CC=CC=C1)N1C(CN(CC1)C1=C(C(N(C2=CC=C(C=C12)F)C)=O)[N+](=O)[O-])=O PBZCKZMEAGILKI-UHFFFAOYSA-N 0.000 claims 2
- ZILATJQHQQWRGD-UHFFFAOYSA-N 4-[4-[(1-ethylindol-4-yl)methyl]piperazin-1-yl]-6-fluoro-1-methyl-3-nitroquinolin-2-one Chemical compound C(C)N1C=CC2=C(C=CC=C12)CN1CCN(CC1)C1=C(C(N(C2=CC=C(C=C12)F)C)=O)[N+](=O)[O-] ZILATJQHQQWRGD-UHFFFAOYSA-N 0.000 claims 2
- LCHWEYIQKVIGRW-UHFFFAOYSA-N 6-fluoro-4-[4-(1H-indol-4-ylmethyl)piperazin-1-yl]-1-methyl-3-nitroquinolin-2-one Chemical compound N1C=CC2=C(C=CC=C12)CN1CCN(CC1)C1=C(C(N(C2=CC=C(C=C12)F)C)=O)[N+](=O)[O-] LCHWEYIQKVIGRW-UHFFFAOYSA-N 0.000 claims 2
- VVHHHEXDEZQKLX-UHFFFAOYSA-N 6-fluoro-4-[4-[(3-fluorophenyl)methyl]piperazin-1-yl]-1-methyl-3-nitroquinolin-2-one Chemical compound FC=1C=C2C(=C(C(N(C2=CC=1)C)=O)[N+](=O)[O-])N1CCN(CC1)CC1=CC(=CC=C1)F VVHHHEXDEZQKLX-UHFFFAOYSA-N 0.000 claims 2
- HDBNFDAZVBIFPD-UHFFFAOYSA-N 6-methoxy-1-methyl-4-[4-(naphthalen-1-ylmethyl)piperazin-1-yl]-3-nitroquinolin-2-one Chemical compound COC=1C=C2C(=C(C(N(C2=CC=1)C)=O)[N+](=O)[O-])N1CCN(CC1)CC1=CC=CC2=CC=CC=C12 HDBNFDAZVBIFPD-UHFFFAOYSA-N 0.000 claims 2
- INJUAESEVFTURL-UXHICEINSA-N FC1=CC=C(C=C1)C(N1C[C@@H](N(C[C@H]1C)C1=C(C(N(C2=CC=CC=C12)C)=O)C#N)C)C1=CC=C(C=C1)F Chemical compound FC1=CC=C(C=C1)C(N1C[C@@H](N(C[C@H]1C)C1=C(C(N(C2=CC=CC=C12)C)=O)C#N)C)C1=CC=C(C=C1)F INJUAESEVFTURL-UXHICEINSA-N 0.000 claims 2
- MODTVAKVRSSEKI-VQTJNVASSA-N FC1=CC=C(C=C1)C(N1C[C@@H](N(C[C@H]1C)C1=CC(N(C2=CC=C(C=C12)C#N)C)=O)C)C1=CC=C(C=C1)F Chemical compound FC1=CC=C(C=C1)C(N1C[C@@H](N(C[C@H]1C)C1=CC(N(C2=CC=C(C=C12)C#N)C)=O)C)C1=CC=C(C=C1)F MODTVAKVRSSEKI-VQTJNVASSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000006555 (C3-C5) cycloalkyl group Chemical group 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
- 102000011107 Diacylglycerol Kinase Human genes 0.000 claims 1
- 108010062677 Diacylglycerol Kinase Proteins 0.000 claims 1
- 102100022735 Diacylglycerol kinase alpha Human genes 0.000 claims 1
- 101710181033 Diacylglycerol kinase alpha Proteins 0.000 claims 1
- 102100030220 Diacylglycerol kinase zeta Human genes 0.000 claims 1
- 101710192015 Diacylglycerol kinase zeta Proteins 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 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
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000005348 fluorocycloalkyl group Chemical group 0.000 claims 1
- 125000001207 fluorophenyl group Chemical group 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 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
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN201911053557 | 2019-12-23 | ||
| IN201911053557 | 2019-12-23 | ||
| PCT/US2020/066503 WO2021133748A1 (fr) | 2019-12-23 | 2020-12-22 | Composés de quinolinonyle pipérazine substitués utiles en tant qu'activateurs de lymphocytes t |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023508055A JP2023508055A (ja) | 2023-02-28 |
| JPWO2021133748A5 true JPWO2021133748A5 (fr) | 2023-12-07 |
Family
ID=74195153
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022538818A Pending JP2023508055A (ja) | 2019-12-23 | 2020-12-22 | Ｔ細胞アクティベーターとして有用な置換キノリノニルピペラジン化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20230061608A1 (fr) |
| EP (1) | EP4081513A1 (fr) |
| JP (1) | JP2023508055A (fr) |
| KR (1) | KR20220119456A (fr) |
| CN (1) | CN115103841A (fr) |
| AU (1) | AU2020414688A1 (fr) |
| BR (1) | BR112022012220A2 (fr) |
| CA (1) | CA3162992A1 (fr) |
| IL (1) | IL294269A (fr) |
| MX (1) | MX2022007369A (fr) |
| WO (1) | WO2021133748A1 (fr) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021130638A1 (fr) | 2019-12-24 | 2021-07-01 | Carna Biosciences, Inc. | Composés modulant la diacylglycérol kinase |
| CA3222277A1 (fr) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Composes modulant les diacylglycerol kinases |
| KR20240005901A (ko) | 2021-06-23 | 2024-01-12 | 길리애드 사이언시즈, 인코포레이티드 | 디아실글리세롤 키나제 조절 화합물 |
| CA3222439A1 (fr) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Composes modulant les diacylglycerol kinases |
| EP4359389A1 (fr) | 2021-06-23 | 2024-05-01 | Gilead Sciences, Inc. | Composés de modulation de la diacylglycérol kinase |
| WO2023122772A1 (fr) * | 2021-12-22 | 2023-06-29 | Gossamer Bio Services, Inc. | Dérivés d'oxime utiles comme activateurs de lymphocytes t |
| WO2023122777A1 (fr) * | 2021-12-22 | 2023-06-29 | Gossamer Bio Services, Inc. | Dérivés d'oxime utiles en tant qu'activateurs de lymphocytes t |
| WO2023150186A1 (fr) * | 2022-02-01 | 2023-08-10 | Arvinas Operations, Inc. | Composés de ciblage de dgk et utilisations associées |
| CN115124464B (zh) * | 2022-07-04 | 2023-06-06 | 新乡学院 | 一种喹啉二酮磺酰哌嗪杂合体及其制备方法和应用 |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200418829A (en) * | 2003-02-14 | 2004-10-01 | Avanir Pharmaceutics | Inhibitors of macrophage migration inhibitory factor and methods for identifying the same |
| TWI380996B (zh) | 2004-09-17 | 2013-01-01 | Hoffmann La Roche | 抗ｏｘ４０ｌ抗體 |
| PT1866339E (pt) | 2005-03-25 | 2013-09-03 | Gitr Inc | Moléculas de ligação a gitr e suas utilizações |
| SG10201809390QA (en) | 2005-05-10 | 2018-11-29 | Incyte Holdings Corp | Modulators of indoleamine 2,3-dioxygenase and methods of using the same |
| KR101411165B1 (ko) | 2005-07-01 | 2014-06-25 | 메다렉스, 엘.엘.시. | 예정 사멸 리간드 1 (피디-엘1)에 대한 인간 모노클로날항체 |
| EP1971583B1 (fr) | 2005-12-20 | 2015-03-25 | Incyte Corporation | N-hydroxyamidinoheterocycles en tant que modulateurs d'indoleamine 2,3-dioxygenase |
| 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. |
| JP5319532B2 (ja) | 2006-09-19 | 2013-10-16 | インサイト・コーポレイション | インドールアミン２，３−ジオキシゲナーゼのモジュレーターとしてのｎ−ヒドロキシアミジノヘテロサイクル |
| EP1987839A1 (fr) | 2007-04-30 | 2008-11-05 | I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale | Anticorps monoclonal cytotoxique anti-LAG-3 et son utilisation pour le traitement ou la prévention d'un rejet de greffe d'organe et de maladies auto-immunes |
| JP5932217B2 (ja) | 2007-07-12 | 2016-06-08 | ジーアイティーアール， インコーポレイテッド | Ｇｉｔｒ結合分子を使用する併用療法 |
| EP2044949A1 (fr) | 2007-10-05 | 2009-04-08 | Immutep | Utilisation de lag-3 recombinant ou ses dérivatifs pour déclencher la réponse immune des monocytes |
| CA2932121A1 (fr) | 2007-11-30 | 2009-06-11 | Newlink Genetics Corporation | Inhibiteurs de l'ido |
| WO2009156652A1 (fr) | 2008-05-29 | 2009-12-30 | Saint-Gobain Centre De Recherches Et D'etudes Europeen | Structure en nid d'abeille a base de titanate d'aluminium |
| AR072999A1 (es) | 2008-08-11 | 2010-10-06 | Medarex Inc | Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos |
| PE20120341A1 (es) | 2008-12-09 | 2012-04-24 | Genentech Inc | Anticuerpos anti-pd-l1 y su uso para mejorar la funcion de celulas t |
| WO2011028683A1 (fr) | 2009-09-03 | 2011-03-10 | Schering Corporation | Anticorps anti-gitr |
| EP2493862B1 (fr) | 2009-10-28 | 2016-10-05 | Newlink Genetics Corporation | Dérivés imidazole comme inhibiteurs de l'ido |
| CN102791738B (zh) | 2009-12-10 | 2015-10-07 | 霍夫曼-拉罗奇有限公司 | 优先结合人csf1r胞外域4的抗体及其用途 |
| NZ701539A (en) | 2010-03-04 | 2015-04-24 | Macrogenics Inc | Antibodies reactive with b7-h3, immunologically active fragments thereof and uses thereof |
| WO2011131407A1 (fr) | 2010-03-05 | 2011-10-27 | F. Hoffmann-La Roche Ag | Anticorps contre le csf-1r humain et leurs utilisations |
| KR101656548B1 (ko) | 2010-03-05 | 2016-09-09 | 에프. 호프만-라 로슈 아게 | 인간 ｃｓｆ-1ｒ에 대한 항체 및 이의 용도 |
| JP6008842B2 (ja) | 2010-05-04 | 2016-10-19 | ファイブ プライム セラピューティックス インコーポレイテッド | Ｃｓｆ１ｒに結合する抗体 |
| NZ729044A (en) | 2010-09-09 | 2020-07-31 | Pfizer | 4-1bb binding molecules |
| NO2694640T3 (fr) | 2011-04-15 | 2018-03-17 | ||
| SI2699264T1 (en) | 2011-04-20 | 2018-08-31 | Medimmune Llc | Antibodies and other molecules that bind B7-H1 and PD-1 |
| RS61033B1 (sr) | 2011-11-28 | 2020-12-31 | Merck Patent Gmbh | Antitela na pd-l1 i njihova upotreba |
| US10023643B2 (en) | 2011-12-15 | 2018-07-17 | Hoffmann-La Roche Inc. | Antibodies against human CSF-1R and uses thereof |
| CN104093740B (zh) | 2012-02-06 | 2018-01-09 | 弗·哈夫曼-拉罗切有限公司 | 使用csf1r抑制剂的组合物和方法 |
| AR090263A1 (es) | 2012-03-08 | 2014-10-29 | Hoffmann La Roche | Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma |
| RU2670743C9 (ru) | 2012-05-11 | 2018-12-19 | Файв Прайм Терапьютикс, Инк. | Способы лечения состояний антителами, которые связывают рецептор колониестимулирующего фактора 1 (csf1r) |
| 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 |
| SG10201906328RA (en) | 2012-08-31 | 2019-08-27 | Five Prime Therapeutics Inc | Methods of treating conditions with antibodies that bind colony stimulating factor 1 receptor (csf1r) |
-
2020
- 2020-12-22 CA CA3162992A patent/CA3162992A1/fr active Pending
- 2020-12-22 KR KR1020227025288A patent/KR20220119456A/ko unknown
- 2020-12-22 AU AU2020414688A patent/AU2020414688A1/en active Pending
- 2020-12-22 EP EP20845303.5A patent/EP4081513A1/fr active Pending
- 2020-12-22 WO PCT/US2020/066503 patent/WO2021133748A1/fr unknown
- 2020-12-22 IL IL294269A patent/IL294269A/en unknown
- 2020-12-22 MX MX2022007369A patent/MX2022007369A/es unknown
- 2020-12-22 BR BR112022012220A patent/BR112022012220A2/pt unknown
- 2020-12-22 JP JP2022538818A patent/JP2023508055A/ja active Pending
- 2020-12-22 CN CN202080096443.9A patent/CN115103841A/zh active Pending
- 2020-12-22 US US17/786,239 patent/US20230061608A1/en active Pending
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