JP2020534259A5 - - Google Patents
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- Publication number
- JP2020534259A5 JP2020534259A5 JP2020513700A JP2020513700A JP2020534259A5 JP 2020534259 A5 JP2020534259 A5 JP 2020534259A5 JP 2020513700 A JP2020513700 A JP 2020513700A JP 2020513700 A JP2020513700 A JP 2020513700A JP 2020534259 A5 JP2020534259 A5 JP 2020534259A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- heterocyclyl
- cycloalkyl
- aryl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 40
- 125000000623 heterocyclic group Chemical group 0.000 claims 26
- 125000000753 cycloalkyl group Chemical group 0.000 claims 24
- 125000003118 aryl group Chemical group 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 22
- 239000001257 hydrogen Substances 0.000 claims 22
- 125000001424 substituent group Chemical group 0.000 claims 21
- 229910052736 halogen Inorganic materials 0.000 claims 19
- 150000002367 halogens Chemical class 0.000 claims 19
- 125000001072 heteroaryl group Chemical group 0.000 claims 18
- 150000002431 hydrogen Chemical class 0.000 claims 14
- 125000005842 heteroatom Chemical group 0.000 claims 10
- 229920006395 saturated elastomer Polymers 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000005843 halogen group Chemical group 0.000 claims 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- -1 halo C 2-6 alkynyl Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 3
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 3
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 3
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 3
- 125000002619 bicyclic group Chemical group 0.000 claims 3
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 201000006417 multiple sclerosis Diseases 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 208000003950 B-cell lymphoma Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 201000003444 follicular lymphoma Diseases 0.000 claims 2
- 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 230000009885 systemic effect Effects 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 206010018372 Glomerulonephritis membranous Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010028372 Muscular weakness Diseases 0.000 claims 1
- 206010028980 Neoplasm 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
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 208000002552 acute disseminated encephalomyelitis Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 125000006193 alkinyl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 210000003719 b-lymphocyte Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 230000000112 colonic effect Effects 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 150000002366 halogen compounds 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
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000003445 large cell neuroendocrine carcinoma 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
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 201000007919 lymphoplasmacytic lymphoma Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000008350 membranous glomerulonephritis Diseases 0.000 claims 1
- 231100000855 membranous nephropathy Toxicity 0.000 claims 1
- 230000036473 myasthenia Effects 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2017/101058 | 2017-09-08 | ||
| CN2017101058 | 2017-09-08 | ||
| CN2017119373 | 2017-12-28 | ||
| CNPCT/CN2017/119373 | 2017-12-28 | ||
| CN2018086555 | 2018-05-11 | ||
| CNPCT/CN2018/086555 | 2018-05-11 | ||
| PCT/CN2018/104559 WO2019047915A1 (en) | 2017-09-08 | 2018-09-07 | IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3KDELTA INHIBITORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020534259A JP2020534259A (ja) | 2020-11-26 |
| JP2020534259A5 true JP2020534259A5 (https=) | 2021-09-24 |
| JP7128264B2 JP7128264B2 (ja) | 2022-08-30 |
Family
ID=65633578
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020513700A Active JP7128264B2 (ja) | 2017-09-08 | 2018-09-07 | ＰＩ３Ｋδ阻害剤としてのイミダゾ［１，５－ａ］ピラジン誘導体 |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US11220506B2 (https=) |
| EP (2) | EP3679042B1 (https=) |
| JP (1) | JP7128264B2 (https=) |
| KR (1) | KR20200052297A (https=) |
| CN (2) | CN111704615B (https=) |
| AU (2) | AU2018328569B2 (https=) |
| BR (1) | BR112020004500A2 (https=) |
| CA (1) | CA3072842A1 (https=) |
| DK (1) | DK3679042T3 (https=) |
| ES (1) | ES2944658T3 (https=) |
| FI (1) | FI3679042T3 (https=) |
| HU (1) | HUE061898T2 (https=) |
| IL (1) | IL272988B (https=) |
| MX (1) | MX2020002630A (https=) |
| NZ (1) | NZ761680A (https=) |
| PL (1) | PL3679042T3 (https=) |
| PT (1) | PT3679042T (https=) |
| SG (1) | SG11202001286SA (https=) |
| TW (2) | TWI817956B (https=) |
| WO (1) | WO2019047915A1 (https=) |
| ZA (1) | ZA202000875B (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3045959A1 (en) | 2016-12-07 | 2018-06-14 | Beigene, Ltd. | Imidazo [1,5-a] pyrazine derivatives as pi3kdelta inhibitors |
| BR112020004500A2 (pt) | 2017-09-08 | 2020-12-01 | Beigene, Ltd. | derivados de imidazo [1,5-a] pirazina como inibidores de pi3kdelta |
| US20230011916A1 (en) * | 2019-11-21 | 2023-01-12 | Beigene, Ltd. | Methods of cancer treatment using anti-ox40 antibodies in combination with pi3 kinase delta inhibitors |
| AU2022280905A1 (en) * | 2021-05-27 | 2024-01-18 | Beigene Switzerland Gmbh | SALTS OF A PI3Kdelta INHIBITOR, CRYSTALLINE FORMS, METHODS OF PREPARATION, AND USES THEREFORE |
| WO2023040810A1 (en) * | 2021-09-14 | 2023-03-23 | Beigene, Ltd. | Methods of cancer treatment using a combination of btk inhibitors and pi3 kinase inhibitors |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005089352A (ja) * | 2003-09-16 | 2005-04-07 | Kissei Pharmaceut Co Ltd | 新規なイミダゾ［１，５−ａ］ピラジン誘導体、それを含有する医薬組成物およびそれらの用途 |
| UA83509C2 (en) * | 2003-10-15 | 2008-07-25 | Оси Фармасьютикалз, Инк. | Imidazopyrazines as tyrosine kinase inhibitors |
| TW200738725A (en) * | 2006-01-25 | 2007-10-16 | Osi Pharm Inc | Unsaturated mTOR inhibitors |
| US20120077813A1 (en) * | 2009-04-15 | 2012-03-29 | Astrazeneca Ab | Imidazole Substituted Pyrimidines Useful in the Treatment of Glycogen Synthase Kinase-3 Related Disorders such as Alzheimer's Disease |
| BRPI1014572B8 (pt) | 2009-04-16 | 2022-07-19 | Fundacion Centro Nac De Investigaciones Oncologicas Carlos Iii | Imidazopirazinas para uso como inibidores de cinase |
| RU2013138835A (ru) * | 2011-02-09 | 2015-03-20 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения в качестве ингибиторов pi3 киназы |
| ES2588186T3 (es) | 2012-01-10 | 2016-10-31 | Bayer Intellectual Property Gmbh | Imidazopirazinas sustituidas como inhibidores de la quinasa Akt |
| AU2013337717B2 (en) | 2012-11-01 | 2018-10-25 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using PI3 kinase isoform modulators |
| TWI687220B (zh) * | 2013-03-01 | 2020-03-11 | 美商英塞特控股公司 | 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途 |
| CA2914284A1 (en) | 2013-05-30 | 2014-12-04 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| CA2922058A1 (en) * | 2013-10-18 | 2015-04-23 | Medivation Technologies, Inc. | Heterocyclic compounds and methods of use |
| PL3179991T3 (pl) * | 2014-08-11 | 2022-02-14 | Acerta Pharma B.V. | Kombinacje terapeutyczne inhibitora btk i inhibitora bcl-2 |
| AR102220A1 (es) * | 2015-10-08 | 2017-02-15 | Incyte Corp | Imidazopiridinas e imidazopirazinas como inhibidores de lsd1 |
| HRP20210508T1 (hr) * | 2016-06-16 | 2021-05-28 | Janssen Pharmaceutica Nv | Biciklički derivati piridina, pirazina i pirimidina kao inhibitori pi3k beta |
| CA3045959A1 (en) * | 2016-12-07 | 2018-06-14 | Beigene, Ltd. | Imidazo [1,5-a] pyrazine derivatives as pi3kdelta inhibitors |
| BR112020004500A2 (pt) | 2017-09-08 | 2020-12-01 | Beigene, Ltd. | derivados de imidazo [1,5-a] pirazina como inibidores de pi3kdelta |
-
2018
- 2018-09-07 BR BR112020004500-4A patent/BR112020004500A2/pt not_active Application Discontinuation
- 2018-09-07 KR KR1020207007386A patent/KR20200052297A/ko active Pending
- 2018-09-07 FI FIEP18853233.7T patent/FI3679042T3/fi active
- 2018-09-07 TW TW107131522A patent/TWI817956B/zh not_active IP Right Cessation
- 2018-09-07 DK DK18853233.7T patent/DK3679042T3/da active
- 2018-09-07 JP JP2020513700A patent/JP7128264B2/ja active Active
- 2018-09-07 SG SG11202001286SA patent/SG11202001286SA/en unknown
- 2018-09-07 AU AU2018328569A patent/AU2018328569B2/en not_active Ceased
- 2018-09-07 CN CN202010273331.8A patent/CN111704615B/zh active Active
- 2018-09-07 WO PCT/CN2018/104559 patent/WO2019047915A1/en not_active Ceased
- 2018-09-07 PL PL18853233.7T patent/PL3679042T3/pl unknown
- 2018-09-07 NZ NZ761680A patent/NZ761680A/en not_active IP Right Cessation
- 2018-09-07 ES ES18853233T patent/ES2944658T3/es active Active
- 2018-09-07 CA CA3072842A patent/CA3072842A1/en active Pending
- 2018-09-07 CN CN201880057835.7A patent/CN111051312A/zh active Pending
- 2018-09-07 MX MX2020002630A patent/MX2020002630A/es unknown
- 2018-09-07 PT PT188532337T patent/PT3679042T/pt unknown
- 2018-09-07 IL IL272988A patent/IL272988B/en unknown
- 2018-09-07 EP EP18853233.7A patent/EP3679042B1/en active Active
- 2018-09-07 HU HUE18853233A patent/HUE061898T2/hu unknown
- 2018-09-07 US US16/643,040 patent/US11220506B2/en active Active
- 2018-09-07 TW TW111147323A patent/TW202336010A/zh unknown
- 2018-09-07 EP EP23152036.2A patent/EP4219502A1/en not_active Withdrawn
-
2020
- 2020-02-11 ZA ZA2020/00875A patent/ZA202000875B/en unknown
-
2021
- 2021-11-23 US US17/533,442 patent/US11905294B2/en active Active
-
2023
- 2023-10-25 AU AU2023254925A patent/AU2023254925A1/en not_active Abandoned
-
2024
- 2024-01-11 US US18/410,925 patent/US20240150361A1/en not_active Abandoned
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