JP2017530959A5 - - Google Patents
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- JP2017530959A5 JP2017530959A5 JP2017514627A JP2017514627A JP2017530959A5 JP 2017530959 A5 JP2017530959 A5 JP 2017530959A5 JP 2017514627 A JP2017514627 A JP 2017514627A JP 2017514627 A JP2017514627 A JP 2017514627A JP 2017530959 A5 JP2017530959 A5 JP 2017530959A5
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- JP
- Japan
- Prior art keywords
- unsubstituted
- substituted
- alkyl
- haloalkyl
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 66
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 41
- 229910052739 hydrogen Inorganic materials 0.000 claims 35
- 239000001257 hydrogen Substances 0.000 claims 35
- 125000000623 heterocyclic group Chemical group 0.000 claims 33
- 229910052736 halogen Inorganic materials 0.000 claims 27
- 150000002367 halogens Chemical group 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 25
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 19
- 125000004093 cyano group Chemical group *C#N 0.000 claims 16
- 150000002431 hydrogen Chemical group 0.000 claims 15
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 11
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 102100025210 Histone-arginine methyltransferase CARM1 Human genes 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 108010030886 coactivator-associated arginine methyltransferase 1 Proteins 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 102000015735 Beta-catenin Human genes 0.000 claims 1
- 108060000903 Beta-catenin Proteins 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 101000904152 Homo sapiens Transcription factor E2F1 Proteins 0.000 claims 1
- 102100024026 Transcription factor E2F1 Human genes 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000004419 alkynylene group Chemical group 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 230000008482 dysregulation Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000011664 signaling Effects 0.000 claims 1
- 230000003827 upregulation Effects 0.000 claims 1
- 0 C*(**)C1CCOCC1 Chemical compound C*(**)C1CCOCC1 0.000 description 11
- LQVZUXUQGFIYEK-UHFFFAOYSA-N CNC1COCC1 Chemical compound CNC1COCC1 LQVZUXUQGFIYEK-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462051872P | 2014-09-17 | 2014-09-17 | |
| US62/051,872 | 2014-09-17 | ||
| PCT/US2015/050712 WO2016044604A1 (en) | 2014-09-17 | 2015-09-17 | Carm1 inhibitors and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017530959A JP2017530959A (ja) | 2017-10-19 |
| JP2017530959A5 true JP2017530959A5 (US06780888-20040824-C00057.png) | 2018-11-01 |
Family
ID=55533856
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017514627A Withdrawn JP2017530959A (ja) | 2014-09-17 | 2015-09-17 | Ｃａｒｍ１阻害剤およびその使用 |
Country Status (4)
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2935222T3 (en) | 2012-12-21 | 2019-01-07 | Epizyme Inc | PRMT5 INHIBITORS AND APPLICATIONS THEREOF |
| 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 |
| WO2014100734A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| CA2899363A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| US9745291B2 (en) | 2012-12-21 | 2017-08-29 | Epizyme, Inc. | PRMT5 inhibitors containing a dihydro- or tetrahydroisoquinoline and uses thereof |
| US9776972B2 (en) | 2013-03-14 | 2017-10-03 | Epizyme Inc. | Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof |
| EP2970135B1 (en) | 2013-03-14 | 2018-07-18 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| WO2014153214A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyl transferase inhibtors and uses thereof |
| US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014153208A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| RS61231B1 (sr) | 2013-03-14 | 2021-01-29 | Epizyme Inc | Inhibitori arginin-metiltransferaze i njihove upotrebe |
| US9718816B2 (en) | 2013-03-15 | 2017-08-01 | Epizyme, Inc. | 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as CARM1 inhibitors and uses thereof |
| KR20160003647A (ko) | 2013-03-15 | 2016-01-11 | 에피자임, 인코포레이티드 | Carm1 억제제 및 이의 용도 |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| EP3177288A4 (en) | 2014-08-04 | 2018-04-04 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| TW201718581A (zh) | 2015-10-19 | 2017-06-01 | 英塞特公司 | 作為免疫調節劑之雜環化合物 |
| LT3377488T (lt) | 2015-11-19 | 2023-01-10 | Incyte Corporation | Heterocikliniai junginiai, kaip imunomoduliatoriai |
| SI3394033T1 (sl) | 2015-12-22 | 2021-03-31 | Incyte Corporation | Heterociklične spojine kot imunomodulatorji |
| MA44860A (fr) | 2016-05-06 | 2019-03-13 | Incyte Holdings Corp | Composés hétérocycliques utilisés comme immunomodulateurs |
| WO2017205464A1 (en) | 2016-05-26 | 2017-11-30 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| EP4137489A1 (en) | 2016-06-20 | 2023-02-22 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| WO2018013789A1 (en) | 2016-07-14 | 2018-01-18 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| EP3504198B1 (en) | 2016-08-29 | 2023-01-25 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| EP3535588A4 (en) | 2016-11-07 | 2020-09-16 | University of Massachusetts | THERAPEUTIC TARGET MOLECULES FOR FACIO-CAPULOHUMERAL MUSCLE DYSTROPHY |
| TWI798192B (zh) | 2016-12-22 | 2023-04-11 | 美商英塞特公司 | 免疫調節劑化合物及使用方法 |
| ES2874756T3 (es) | 2016-12-22 | 2021-11-05 | Incyte Corp | Derivados de triazolo[1,5-A]piridina como inmunomoduladores |
| MX2019007416A (es) | 2016-12-22 | 2019-12-11 | Incyte Corp | Derivados de benzooxazol como inmunomoduladores. |
| US20180179179A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| WO2018140512A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| US11358959B2 (en) | 2017-01-26 | 2022-06-14 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| EP3573970A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer |
| US11279689B2 (en) | 2017-01-26 | 2022-03-22 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1 yl)prop-2-en-1-one derivatives and similar compounds as KRAS G12C modulators for treating cancer |
| CN110382482A (zh) | 2017-01-26 | 2019-10-25 | 亚瑞克西斯制药公司 | 稠合的杂-杂二环化合物及其使用方法 |
| MD3483164T2 (ro) | 2017-03-20 | 2020-07-31 | Forma Therapeutics Inc | Compoziții pirolopirolice ca activatori ai piruvat kinazei (PKR) |
| EP3630747A1 (en) | 2017-05-25 | 2020-04-08 | Araxes Pharma LLC | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| CN110869358A (zh) | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | Kras的共价抑制剂 |
| ES2940750T3 (es) | 2018-03-30 | 2023-05-11 | Incyte Corp | Compuestos heterocíclicos como inmunomoduladores |
| HRP20230306T1 (hr) | 2018-05-11 | 2023-05-12 | Incyte Corporation | Derivati tetrahidro-imidazo[4,5-c]piridina kao pd-l1 imunomodulatori |
| KR20210045998A (ko) * | 2018-08-01 | 2021-04-27 | 아락세스 파마 엘엘씨 | 헤테로사이클릭 스피로 화합물 및 암 치료를 위한 그의 사용 방법 |
| US20200129485A1 (en) | 2018-09-19 | 2020-04-30 | Forma Therapeutics, Inc. | Treating sickle cell disease with a pyruvate kinase r activating compound |
| WO2020061255A1 (en) | 2018-09-19 | 2020-03-26 | Forma Therapeutics, Inc. | Activating pyruvate kinase r |
| KR20220027216A (ko) | 2019-06-28 | 2022-03-07 | 에이엘에스 테라피 디벨럽먼트 인스티튜트 | 디펩타이드 반복 단백질의 억제 |
| CA3150434A1 (en) | 2019-08-09 | 2021-02-18 | Incyte Corporation | Salts of a pd-1/pd-l1 inhibitor |
| TW202126652A (zh) | 2019-09-30 | 2021-07-16 | 美商英塞特公司 | 作為免疫調節劑之吡啶并［３，２—ｄ］嘧啶化合物 |
| KR20220101664A (ko) | 2019-11-11 | 2022-07-19 | 인사이트 코포레이션 | Pd-1/pd-l1 억제제의 염 및 결정질 형태 |
| WO2021188828A1 (en) * | 2020-03-18 | 2021-09-23 | Dana-Farber Cancer Institute, Inc. | Methods for treating cancer by inhibiting carm1 |
| US11760756B2 (en) | 2020-11-06 | 2023-09-19 | Incyte Corporation | Crystalline form of a PD-1/PD-L1 inhibitor |
| WO2022099018A1 (en) | 2020-11-06 | 2022-05-12 | Incyte Corporation | Process of preparing a pd-1/pd-l1 inhibitor |
| US11866434B2 (en) | 2020-11-06 | 2024-01-09 | Incyte Corporation | Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0004886D0 (en) * | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| EP2137158A4 (en) * | 2007-02-28 | 2012-04-18 | Methylgene Inc | LOW-MOLECULAR INHIBITORS OF PROTEINARGININE METHYLTRANSFERASES (PRMTS) |
| WO2010028179A1 (en) * | 2008-09-03 | 2010-03-11 | Dr. Reddy's Laboratories Ltd. | Heterocyclic compounds as gata modulators |
| WO2014100734A1 (en) * | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| KR20160003647A (ko) * | 2013-03-15 | 2016-01-11 | 에피자임, 인코포레이티드 | Carm1 억제제 및 이의 용도 |
| WO2016044641A2 (en) * | 2014-09-17 | 2016-03-24 | Epizyme, Inc. | Carm1 inhibitors and uses thereof |
-
2015
- 2015-09-17 WO PCT/US2015/050712 patent/WO2016044604A1/en active Application Filing
- 2015-09-17 US US15/511,503 patent/US20170305922A1/en not_active Abandoned
- 2015-09-17 EP EP15842456.4A patent/EP3193608A4/en not_active Withdrawn
- 2015-09-17 JP JP2017514627A patent/JP2017530959A/ja not_active Withdrawn
