JP2022084699A5 - - Google Patents
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- Publication number
- JP2022084699A5 JP2022084699A5 JP2022033419A JP2022033419A JP2022084699A5 JP 2022084699 A5 JP2022084699 A5 JP 2022084699A5 JP 2022033419 A JP2022033419 A JP 2022033419A JP 2022033419 A JP2022033419 A JP 2022033419A JP 2022084699 A5 JP2022084699 A5 JP 2022084699A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- indicates
- cycloalkyl
- ring
- substituted
- 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 description 19
- 125000000217 alkyl group Chemical group 0.000 claims 69
- 125000003118 aryl group Chemical group 0.000 claims 32
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 29
- 125000005843 halogen group Chemical group 0.000 claims 27
- 125000001424 substituent group Chemical group 0.000 claims 22
- 229910052757 nitrogen Inorganic materials 0.000 claims 20
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 19
- 125000002619 bicyclic group Chemical group 0.000 claims 19
- 125000004432 carbon atom Chemical group C* 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 19
- 239000012453 solvate Substances 0.000 claims 18
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 17
- 125000003545 alkoxy group Chemical group 0.000 claims 14
- 125000002950 monocyclic group Chemical group 0.000 claims 11
- 125000004076 pyridyl group Chemical group 0.000 claims 9
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 125000002883 imidazolyl group Chemical group 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 229910052717 sulfur Inorganic materials 0.000 claims 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000006704 (C5-C6) cycloalkyl group Chemical group 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000034486 Multi-organ failure Diseases 0.000 claims 1
- 208000010718 Multiple Organ Failure Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 208000029744 multiple organ dysfunction syndrome Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 230000019100 sperm motility Effects 0.000 claims 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims 1
- 239000007858 starting material Substances 0.000 description 2
- WZZBNLYBHUDSHF-DHLKQENFSA-N 1-[(3s,4s)-4-[8-(2-chloro-4-pyrimidin-2-yloxyphenyl)-7-fluoro-2-methylimidazo[4,5-c]quinolin-1-yl]-3-fluoropiperidin-1-yl]-2-hydroxyethanone Chemical compound CC1=NC2=CN=C3C=C(F)C(C=4C(=CC(OC=5N=CC=CN=5)=CC=4)Cl)=CC3=C2N1[C@H]1CCN(C(=O)CO)C[C@@H]1F WZZBNLYBHUDSHF-DHLKQENFSA-N 0.000 description 1
- TVTJUIAKQFIXCE-HUKYDQBMSA-N 2-amino-9-[(2R,3S,4S,5R)-4-fluoro-3-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-7-prop-2-ynyl-1H-purine-6,8-dione Chemical compound NC=1NC(C=2N(C(N(C=2N=1)[C@@H]1O[C@@H]([C@H]([C@H]1O)F)CO)=O)CC#C)=O TVTJUIAKQFIXCE-HUKYDQBMSA-N 0.000 description 1
- 229940125851 compound 27 Drugs 0.000 description 1
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662403336P | 2016-10-03 | 2016-10-03 | |
| US62/403,336 | 2016-10-03 | ||
| EP17157785 | 2017-02-24 | ||
| EP17157785.1 | 2017-02-24 | ||
| JP2019517909A JP7101171B2 (ja) | 2016-10-03 | 2017-10-02 | Ｐｒｍｔ５阻害剤として使用するための新規な単環式および二環式環系置換カルバヌクレオシド類似体 |
| PCT/EP2017/074983 WO2018065365A1 (en) | 2016-10-03 | 2017-10-02 | Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019517909A Division JP7101171B2 (ja) | 2016-10-03 | 2017-10-02 | Ｐｒｍｔ５阻害剤として使用するための新規な単環式および二環式環系置換カルバヌクレオシド類似体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022084699A JP2022084699A (ja) | 2022-06-07 |
| JP2022084699A5 true JP2022084699A5 (https=) | 2023-10-31 |
| JP7576587B2 JP7576587B2 (ja) | 2024-10-31 |
Family
ID=60043171
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019517909A Active JP7101171B2 (ja) | 2016-10-03 | 2017-10-02 | Ｐｒｍｔ５阻害剤として使用するための新規な単環式および二環式環系置換カルバヌクレオシド類似体 |
| JP2022033419A Active JP7576587B2 (ja) | 2016-10-03 | 2022-03-04 | Ｐｒｍｔ５阻害剤として使用するための新規な単環式および二環式環系置換カルバヌクレオシド類似体 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019517909A Active JP7101171B2 (ja) | 2016-10-03 | 2017-10-02 | Ｐｒｍｔ５阻害剤として使用するための新規な単環式および二環式環系置換カルバヌクレオシド類似体 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US11098062B2 (https=) |
| EP (1) | EP3519413A1 (https=) |
| JP (2) | JP7101171B2 (https=) |
| KR (1) | KR102531344B1 (https=) |
| CN (2) | CN115626935B (https=) |
| AU (1) | AU2017338269B2 (https=) |
| BR (1) | BR112019006414A2 (https=) |
| CA (1) | CA3037998A1 (https=) |
| IL (1) | IL265718B (https=) |
| MA (1) | MA46341A (https=) |
| MX (2) | MX2019003843A (https=) |
| PE (1) | PE20190706A1 (https=) |
| PH (1) | PH12019500731A1 (https=) |
| TN (1) | TN2019000087A1 (https=) |
| UA (1) | UA124074C2 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI870767B (zh) * | 2015-08-26 | 2025-01-21 | 比利時商健生藥品公司 | 使用作為prmt5抑制劑之新穎經6-6雙環芳香環取代之核苷類似物 |
| CN115626935B (zh) | 2016-10-03 | 2025-07-15 | 詹森药业有限公司 | 用作prmt5抑制剂的单环和双环系统取代的卡巴核苷类似物 |
| CN110382707A (zh) | 2017-02-27 | 2019-10-25 | 詹森药业有限公司 | 生物标志在鉴定将对用prmt5抑制剂治疗有响应的癌症患者中的用途 |
| IL275129B2 (en) | 2017-12-08 | 2023-10-01 | Janssen Pharmaceutica Nv | Novel spirobicyclic analogues |
| WO2019219805A1 (en) * | 2018-05-16 | 2019-11-21 | Ctxone Pty Ltd | Combination therapy |
| TW202112375A (zh) | 2019-06-06 | 2021-04-01 | 比利時商健生藥品公司 | 使用ｐｒｍｔ５抑制劑治療癌症之方法 |
| WO2021055797A1 (en) * | 2019-09-18 | 2021-03-25 | Prelude Therapeutics, Incorporated | Selective inhibitors of protein arginine methyltransferase 5 (prmt5) |
| US20230066014A1 (en) * | 2019-12-03 | 2023-03-02 | Lupin Limited | Substituted nucleoside analogs as prmt5 inhibitors |
| CN113186153B (zh) * | 2021-04-15 | 2023-09-08 | 南方医科大学 | Prmt5抑制剂在促进精原干细胞损伤再生和增殖中的应用 |
| CN113234079B (zh) * | 2021-04-30 | 2022-02-01 | 上海湃隆生物科技有限公司 | 用作prmt5抑制剂的核苷类似物 |
| CN114740108B (zh) * | 2022-03-28 | 2023-07-14 | 天津键凯科技有限公司 | 一种聚合物修饰抗体类药物的修饰度的测定方法 |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4224438A (en) | 1970-07-14 | 1980-09-23 | Boehringer Mannheim Gmbh | Adenosine-5'-carboxylic acid amides |
| US6143749A (en) | 1995-06-07 | 2000-11-07 | Abbott Laboratories | Heterocyclic substituted cyclopentane compounds |
| AU2002351077A1 (en) | 2001-11-05 | 2003-05-19 | Exiqon A/S | Oligonucleotides modified with novel alpha-l-rna analogues |
| US7034147B2 (en) | 2001-11-29 | 2006-04-25 | Irm Llc | Nucleoside analog libraries |
| WO2003070739A1 (en) | 2002-02-19 | 2003-08-28 | Cv Therapeutics, Inc. | Partial and full agonists of a1 adenosine receptors |
| US20040043959A1 (en) | 2002-03-04 | 2004-03-04 | Bloom Laura A. | Combination therapies for treating methylthioadenosine phosphorylase deficient cells |
| AU2002951247A0 (en) | 2002-09-06 | 2002-09-19 | Alchemia Limited | Compounds that interact with kinases |
| US20060167241A1 (en) | 2003-07-15 | 2006-07-27 | Mitsui Chemicals, Inc. | Method for synthesizing cyclic bisdinucleoside |
| AU2004311702A1 (en) | 2003-12-19 | 2005-07-21 | Koronis Pharmaceuticals, Inc. | Mutagenic heterocycles |
| WO2006078752A2 (en) | 2005-01-21 | 2006-07-27 | Methylgene, Inc. | Inhibitors of dna methyltransferase |
| WO2008001101A2 (en) | 2006-06-29 | 2008-01-03 | Astex Therapeutics Limited | Pharmaceutical combinations |
| US20080132525A1 (en) | 2006-12-04 | 2008-06-05 | Methylgene Inc. | Inhibitors of DNA Methyltransferase |
| EP2342616A2 (en) | 2008-09-23 | 2011-07-13 | Alnylam Pharmaceuticals Inc. | Chemical modifications of monomers and oligonucleotides with cycloaddition |
| AU2010330823A1 (en) | 2009-12-18 | 2012-07-05 | Joslin Diabetes Center, Inc. | Beta-cell replication promoting compounds and methods of their use |
| CA2819620A1 (en) | 2010-12-03 | 2012-06-21 | Epizyme, Inc. | Modulators of histone methyltransferase, and methods of use thereof |
| EP2646454B1 (en) | 2010-12-03 | 2015-07-08 | Epizyme, Inc. | 7-deazapurine modulators of histone methyltransferase, and methods of use thereof |
| MX2013006951A (es) | 2010-12-16 | 2013-10-03 | Abbvie Inc | Compuestos antivirales. |
| US9284343B2 (en) | 2011-04-04 | 2016-03-15 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | 2′-O-aminooxymethyl nucleoside derivatives for use in the synthesis and modification of nucleosides, nucleotides and oligonucleotides |
| JO3154B1 (ar) | 2011-06-17 | 2017-09-20 | Glaxosmithkline Llc | عوامل مضادة لـ trpv4 |
| JP2014530910A (ja) | 2011-10-24 | 2014-11-20 | グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｎｏ．２ Ｌｉｍｉｔｅｄ | 新規化合物 |
| WO2013151975A1 (en) | 2012-04-02 | 2013-10-10 | Northeastern University | Compositions and methods for the inhibition of methyltransferases |
| WO2014035140A2 (en) | 2012-08-30 | 2014-03-06 | Kainos Medicine, Inc. | Compounds and compositions for modulating histone methyltransferase activity |
| US20140100184A1 (en) | 2012-08-31 | 2014-04-10 | Baylor College Of Medicine | Selective inhibitors of histone methyltransferase dot1l |
| JP2016505000A (ja) | 2012-12-21 | 2016-02-18 | エピザイム，インコーポレイティド | Ｐｒｍｔ５阻害剤およびその使用 |
| EP3406607A1 (en) | 2012-12-21 | 2018-11-28 | Epizyme, Inc. | Prmt5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof |
| US9611257B2 (en) | 2012-12-21 | 2017-04-04 | Epizyme, Inc. | PRMT5 inhibitors and uses thereof |
| UA118548C2 (uk) | 2012-12-21 | 2019-02-11 | Епізайм, Інк. | Тетрагідро- та дигідроізохіноліни як інгібітори prmt5 та їх застосування |
| JP6510485B2 (ja) | 2013-03-15 | 2019-05-08 | オハイオ・ステイト・イノベーション・ファウンデーション | Ｐｒｍｔ５インヒビターおよびそれらの使用方法 |
| US10087151B2 (en) | 2014-01-09 | 2018-10-02 | The J. David Gladstone Institutes, A Testimentary Trust Established Under The Will Of J. David Gladstone | Substituted benzoxazine and related compounds |
| WO2015200680A2 (en) * | 2014-06-25 | 2015-12-30 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| SG11201610476VA (en) | 2014-07-01 | 2017-01-27 | Millennium Pharm Inc | Heteroaryl compounds useful as inhibitors of sumo activating enzyme |
| JP6584521B2 (ja) * | 2015-02-24 | 2019-10-02 | ファイザー・インク | 抗がん剤として有用な置換ヌクレオシド誘導体 |
| TWI870767B (zh) | 2015-08-26 | 2025-01-21 | 比利時商健生藥品公司 | 使用作為prmt5抑制劑之新穎經6-6雙環芳香環取代之核苷類似物 |
| PE20181894A1 (es) | 2016-03-10 | 2018-12-11 | Janssen Pharmaceutica Nv | Nuevos analogos de nucleosidos sustituidos para su uso como inhibidores de prmt 5 |
| CN115626935B (zh) | 2016-10-03 | 2025-07-15 | 詹森药业有限公司 | 用作prmt5抑制剂的单环和双环系统取代的卡巴核苷类似物 |
| EA201990851A1 (ru) | 2017-02-24 | 2019-09-30 | Янссен Фармацевтика Нв | Новые аналоги карбануклеозида, замещенные моноциклической и бициклической кольцевой системой, для применения в качестве ингибиторов prmt5 |
| CN110382707A (zh) | 2017-02-27 | 2019-10-25 | 詹森药业有限公司 | 生物标志在鉴定将对用prmt5抑制剂治疗有响应的癌症患者中的用途 |
| IL275129B2 (en) | 2017-12-08 | 2023-10-01 | Janssen Pharmaceutica Nv | Novel spirobicyclic analogues |
-
2017
- 2017-10-02 CN CN202211277466.7A patent/CN115626935B/zh active Active
- 2017-10-02 BR BR112019006414A patent/BR112019006414A2/pt active Search and Examination
- 2017-10-02 EP EP17781060.3A patent/EP3519413A1/en active Pending
- 2017-10-02 US US16/336,934 patent/US11098062B2/en active Active
- 2017-10-02 UA UAA201904546A patent/UA124074C2/uk unknown
- 2017-10-02 AU AU2017338269A patent/AU2017338269B2/en not_active Ceased
- 2017-10-02 MX MX2019003843A patent/MX2019003843A/es unknown
- 2017-10-02 JP JP2019517909A patent/JP7101171B2/ja active Active
- 2017-10-02 TN TNP/2019/000087A patent/TN2019000087A1/en unknown
- 2017-10-02 CA CA3037998A patent/CA3037998A1/en active Pending
- 2017-10-02 MA MA046341A patent/MA46341A/fr unknown
- 2017-10-02 CN CN201780061258.4A patent/CN109803971B/zh active Active
- 2017-10-02 KR KR1020197012099A patent/KR102531344B1/ko active Active
- 2017-10-02 PE PE2019000723A patent/PE20190706A1/es unknown
-
2019
- 2019-03-31 IL IL265718A patent/IL265718B/en unknown
- 2019-04-02 MX MX2023005574A patent/MX2023005574A/es unknown
- 2019-04-03 PH PH12019500731A patent/PH12019500731A1/en unknown
-
2021
- 2021-07-16 US US17/378,417 patent/US11993614B2/en active Active
-
2022
- 2022-03-04 JP JP2022033419A patent/JP7576587B2/ja active Active
-
2023
- 2023-10-17 US US18/488,626 patent/US20240124493A1/en not_active Abandoned
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