JP2020105211A5 - - Google Patents
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- Publication number
- JP2020105211A5 JP2020105211A5 JP2020038089A JP2020038089A JP2020105211A5 JP 2020105211 A5 JP2020105211 A5 JP 2020105211A5 JP 2020038089 A JP2020038089 A JP 2020038089A JP 2020038089 A JP2020038089 A JP 2020038089A JP 2020105211 A5 JP2020105211 A5 JP 2020105211A5
- Authority
- JP
- Japan
- Prior art keywords
- benzo
- substituted
- cycloheptane
- pyridazine
- triazole
- 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
- DMEGYFMYUHOHGS-UHFFFAOYSA-N cycloheptane Chemical compound C1CCCCCC1 DMEGYFMYUHOHGS-UHFFFAOYSA-N 0.000 claims 120
- -1 pyridazine-3-yl Chemical group 0.000 claims 82
- 108091008036 Immune checkpoint proteins Proteins 0.000 claims 18
- 102000037982 Immune checkpoint proteins Human genes 0.000 claims 18
- 230000000694 effects Effects 0.000 claims 18
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 229940045513 CTLA4 antagonist Drugs 0.000 claims 7
- 125000003710 aryl alkyl group Chemical group 0.000 claims 7
- 125000003107 substituted aryl group Chemical group 0.000 claims 7
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 7
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 6
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000004449 heterocyclylalkenyl group Chemical group 0.000 claims 6
- 125000004450 alkenylene group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 5
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000000262 haloalkenyl group Chemical group 0.000 claims 4
- 125000000232 haloalkynyl group Chemical group 0.000 claims 4
- 125000004447 heteroarylalkenyl group Chemical group 0.000 claims 4
- 125000005312 heteroarylalkynyl group Chemical group 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000006413 ring segment Chemical group 0.000 claims 4
- 125000005357 cycloalkylalkynyl group Chemical group 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000000464 thioxo group Chemical group S=* 0.000 claims 3
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 2
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 claims 2
- 102000037984 Inhibitory immune checkpoint proteins Human genes 0.000 claims 2
- 108091008026 Inhibitory immune checkpoint proteins Proteins 0.000 claims 2
- 210000001744 T-lymphocyte Anatomy 0.000 claims 2
- 125000004419 alkynylene group Chemical group 0.000 claims 2
- 125000005018 aryl alkenyl group Chemical group 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 108091008034 costimulatory receptors Proteins 0.000 claims 2
- 125000005356 cycloalkylalkenyl group Chemical group 0.000 claims 2
- 125000006311 cyclobutyl amino group Chemical group [H]N(*)C1([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000006312 cyclopentyl amino group Chemical group [H]N(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 2
- 125000004914 dipropylamino group Chemical group C(CC)N(CCC)* 0.000 claims 2
- 239000012274 immune-checkpoint protein inhibitor Substances 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229960002621 pembrolizumab Drugs 0.000 claims 2
- 239000000018 receptor agonist Substances 0.000 claims 2
- 229940044601 receptor agonist Drugs 0.000 claims 2
- 125000004913 2-ethylbutylamino group Chemical group C(C)C(CN*)CC 0.000 claims 1
- NLTFNEOTIGWQDZ-UHFFFAOYSA-N 3-[3-fluoro-4-(4-pyrrolidin-1-ylpiperidin-1-yl)phenyl]-1,2-dihydro-1,2,4-triazole-3,5-diamine Chemical compound N1NC(N)=NC1(N)C(C=C1F)=CC=C1N1CCC(N2CCCC2)CC1 NLTFNEOTIGWQDZ-UHFFFAOYSA-N 0.000 claims 1
- 125000004897 3-methylbutylamino group Chemical group CC(CCN*)C 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 210000004443 dendritic cell Anatomy 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 230000005965 immune activity Effects 0.000 claims 1
- 229960005386 ipilimumab Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229960003301 nivolumab Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003367 polycyclic group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229950007217 tremelimumab Drugs 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022114274A JP7549627B2 (ja) | 2015-05-29 | 2022-07-15 | Ａｘｌインヒビタおよび免疫チェックポイントモジュレータまたは腫瘍溶解性ウィルスによる併用療法 |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1509338.8 | 2015-05-29 | ||
| GBGB1509338.8A GB201509338D0 (en) | 2015-05-29 | 2015-05-29 | Combination therapy |
| GB1516442.9 | 2015-09-16 | ||
| GBGB1516442.9A GB201516442D0 (en) | 2015-05-29 | 2015-09-16 | Combination therapy |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018513923A Division JP6795585B2 (ja) | 2015-05-29 | 2016-05-27 | Ａｘｌインヒビタおよび免疫チェックポイントモジュレータまたは腫瘍溶解性ウィルスによる併用療法 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022114274A Division JP7549627B2 (ja) | 2015-05-29 | 2022-07-15 | Ａｘｌインヒビタおよび免疫チェックポイントモジュレータまたは腫瘍溶解性ウィルスによる併用療法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020105211A JP2020105211A (ja) | 2020-07-09 |
| JP2020105211A5 true JP2020105211A5 (enExample) | 2021-05-06 |
| JP7229194B2 JP7229194B2 (ja) | 2023-02-27 |
Family
ID=53677482
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018513923A Active JP6795585B2 (ja) | 2015-05-29 | 2016-05-27 | Ａｘｌインヒビタおよび免疫チェックポイントモジュレータまたは腫瘍溶解性ウィルスによる併用療法 |
| JP2020038089A Active JP7229194B2 (ja) | 2015-05-29 | 2020-03-05 | Ａｘｌインヒビタおよび免疫チェックポイントモジュレータまたは腫瘍溶解性ウィルスによる併用療法 |
| JP2022114274A Active JP7549627B2 (ja) | 2015-05-29 | 2022-07-15 | Ａｘｌインヒビタおよび免疫チェックポイントモジュレータまたは腫瘍溶解性ウィルスによる併用療法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018513923A Active JP6795585B2 (ja) | 2015-05-29 | 2016-05-27 | Ａｘｌインヒビタおよび免疫チェックポイントモジュレータまたは腫瘍溶解性ウィルスによる併用療法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022114274A Active JP7549627B2 (ja) | 2015-05-29 | 2022-07-15 | Ａｘｌインヒビタおよび免疫チェックポイントモジュレータまたは腫瘍溶解性ウィルスによる併用療法 |
Country Status (5)
| Country | Link |
|---|---|
| US (4) | US20180153888A1 (enExample) |
| EP (2) | EP3302481A1 (enExample) |
| JP (3) | JP6795585B2 (enExample) |
| GB (2) | GB201509338D0 (enExample) |
| WO (1) | WO2016193680A1 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201509338D0 (en) * | 2015-05-29 | 2015-07-15 | Bergenbio As | Combination therapy |
| JP6885390B2 (ja) * | 2016-02-26 | 2021-06-16 | 小野薬品工業株式会社 | Ａｘｌ阻害剤と免疫チェックポイント阻害剤とを組み合わせて投与することを特徴とする癌治療のための医薬 |
| US10639368B2 (en) | 2016-05-27 | 2020-05-05 | Agenus Inc. | Anti-TIM-3 antibodies and methods of use thereof |
| IL265800B2 (en) | 2016-10-11 | 2023-10-01 | Agenus Inc | Anti-LAG-3 antibodies and methods of using them |
| US11576873B2 (en) | 2017-03-31 | 2023-02-14 | The Curators Of The University Of Missouri | Compositions for the treatment of drug-resistant tumors and methods of use thereof |
| WO2019039525A1 (ja) * | 2017-08-23 | 2019-02-28 | 小野薬品工業株式会社 | Ａｘｌ阻害剤を有効成分として含むがん治療剤 |
| WO2019074116A1 (ja) | 2017-10-13 | 2019-04-18 | 小野薬品工業株式会社 | Ａｘｌ阻害剤を有効成分として含む固形がん治療剤 |
| BR112020026641A2 (pt) * | 2018-06-27 | 2021-03-30 | Oscotec Inc. | Derivados de piridopirimidinona para o uso como inibidores de axl |
| UY38349A (es) | 2018-08-30 | 2020-03-31 | Array Biopharma Inc | Compuestos de pirazolo[3,4-b]piridina como inhibidores de cinasas tam y met |
| GB201912059D0 (en) | 2019-08-22 | 2019-10-09 | Bergenbio As | Combaination therapy of a patient subgroup |
| GB202004189D0 (en) | 2020-03-23 | 2020-05-06 | Bergenbio As | Combination therapy |
| GB202006072D0 (en) * | 2020-04-24 | 2020-06-10 | Bergenbio Asa | Method of selecting patients for treatment with cmbination therapy |
| GB202104037D0 (en) | 2021-03-23 | 2021-05-05 | Bergenbio Asa | Combination therapy |
| EP4359439A1 (en) | 2021-06-24 | 2024-05-01 | Yeda Research and Development Co. Ltd | Combination therapy for the treatment of cancer comprising an anti-egfr antibody and an axl-inhibitor |
| GB202209285D0 (en) | 2022-06-24 | 2022-08-10 | Bergenbio Asa | Dosage regimen for AXL inhibitor |
| AR129722A1 (es) | 2022-06-28 | 2024-09-18 | Arcus Biosciences Inc | Compuestos inhibidores de axl |
| KR20240156104A (ko) * | 2023-04-21 | 2024-10-29 | 아주대학교산학협력단 | 면역 관문 억제제 저항성 극복을 위한 암의 예방 또는 치료용 약학적 조성물 |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2226211A1 (de) | 1972-05-30 | 1973-12-13 | Basf Ag | N-substituierte iminocumarinfarbstoffe |
| AU2905199A (en) * | 1999-03-15 | 2000-10-04 | Trustees Of The University Of Pennsylvania, The | Combined therapy with a chemotherapeutic agent and an oncolytic virus for killing tumor cells in a subject |
| US6149495A (en) | 1999-03-15 | 2000-11-21 | Austin; Joseph James | Confetti and theatrical snow delivery device |
| EP1382969A1 (en) | 2002-07-17 | 2004-01-21 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Diagnosis and prevention of cancer cell invasion |
| AU2003286746A1 (en) | 2002-10-29 | 2004-05-25 | Rigel Pharmaceuticals, Inc. | Modulators of angiogenesis and tumorigenesis |
| WO2007030680A2 (en) | 2005-09-07 | 2007-03-15 | Rigel Pharmaceuticals, Inc. | Triazole derivatives useful as axl inhibitors |
| CA2647282A1 (en) * | 2006-04-05 | 2007-10-11 | Pfizer Products Inc. | Ctla4 antibody combination therapy |
| AU2007307652A1 (en) | 2006-10-10 | 2008-04-17 | Squicor | Compositions and methods for treating and diagnosing cancers |
| US8097630B2 (en) | 2006-10-10 | 2012-01-17 | Rigel Pharmaceuticals, Inc. | Pinane-substituted pyrimidinediamine derivatives useful as Axl inhibitors |
| JP2008130120A (ja) | 2006-11-17 | 2008-06-05 | Sharp Corp | 光ピックアップ装置 |
| WO2008080134A2 (en) | 2006-12-22 | 2008-07-03 | Rigel Pharmaceuticals, Inc. | 4-amin0-2- (hetero) arylamino-5- (hetero) arylthiazoles useful as axl inhibitors |
| US9650391B2 (en) | 2006-12-29 | 2017-05-16 | Rigel Pharmaceuticals Inc. | N3-heteroaryl substituted triazoles and N5-heteroaryl substituted triazoles useful as Axl inhibitors |
| CA2710230C (en) | 2006-12-29 | 2016-02-23 | Rigel Pharmaceuticals, Inc. | Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors |
| PL2078010T3 (pl) * | 2006-12-29 | 2014-07-31 | Rigel Pharmaceuticals Inc | Triazole podstawione policyklicznym heteroarylem użyteczne jako inhibitory Axl |
| ES2558477T3 (es) | 2006-12-29 | 2016-02-04 | Rigel Pharmaceuticals, Inc. | Triazoles sustituidos útiles como inhibidores de AXL |
| ES2406930T3 (es) | 2006-12-29 | 2013-06-10 | Rigel Pharmaceuticals, Inc. | Triazoles sustituidos con arilo bicíclico y heteroarilo bicíclico útiles como inhibidores de AXL |
| EP2102356A2 (en) | 2007-01-09 | 2009-09-23 | Brystol-Myers Squibb Company | Identification of polynucleotides for predicting activity of compounds that interact with and/or modulate protein tyrosine kinases and/or protein tyrosine kinase pathways in prostate cells |
| JP2010523712A (ja) * | 2007-04-13 | 2010-07-15 | スーパージェン， インコーポレイテッド | 癌または過剰増殖の治療に有用なａｘｌキナーゼ阻害剤 |
| EP2137535B1 (en) | 2007-04-13 | 2015-06-03 | Dana-Farber Cancer Institute, Inc. | Receptor tyrosine kinase profiling |
| SI2205592T1 (sl) | 2007-10-26 | 2013-09-30 | Rigel Pharmaceuticals, Inc. | Triazoli substituirani s policikličnim arilom in triazoli substituirani s policikličnim heteroarilom uporabni kot Axl inhibitorji |
| NZ599628A (en) | 2007-11-12 | 2013-11-29 | U3 Pharma Gmbh | Axl antibodies |
| PE20091024A1 (es) | 2007-11-15 | 2009-08-12 | Chugai Pharmaceutical Co Ltd | Anticuerpos monoclonales que se unen a anexelekto y sus usos |
| SI2851374T1 (sl) | 2007-12-14 | 2017-08-31 | Bristol-Myers Squibb Company | Vezavne molekule k humanemu ox40 receptorju |
| US8735064B2 (en) | 2007-12-24 | 2014-05-27 | Bergenbio As | Methods for creating and identifying functional RNA interference elements |
| US8546433B2 (en) * | 2009-01-16 | 2013-10-01 | Rigel Pharmaceuticals, Inc. | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
| KR20120035145A (ko) | 2009-05-11 | 2012-04-13 | 우드라이 파마 게엠베하 | 인간화 ａｘｌ 항체 |
| JP5669732B2 (ja) | 2009-05-15 | 2015-02-12 | 中外製薬株式会社 | 抗ａｘｌ抗体 |
| AU2010303149B2 (en) * | 2009-09-30 | 2016-08-04 | Board Of Regents, The University Of Texas System | Combination immunotherapy for the treatment of cancer |
| US20130064831A1 (en) | 2010-05-17 | 2013-03-14 | Bristol-Myers Squibb Company | Immunotherapeutic dosing regimens and combinations thereof |
| BR112012027995A2 (pt) * | 2010-06-18 | 2017-01-10 | Genentech Inc | anticorpo e ácido nucleíco isolado, célula hospedeira, método de produção de um anticorpo, imunoconjugado, formulação farmacêutica, uso do anticorpo, método de tratamento de um indivíduo com câncer, de um indivíduo possuíndo um distúrbio imune, de inibição da angiogênese e para inibir a ativação constitutiva de axl |
| NZ714128A (en) | 2010-09-09 | 2017-10-27 | Pfizer | 4-1bb binding molecules |
| KR20140104944A (ko) | 2011-06-22 | 2014-08-29 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 항-ａｘｌ 항체 및 그의 용도 |
| EP2723377B1 (en) | 2011-06-22 | 2018-06-13 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Anti-axl antibodies and uses thereof |
| WO2013180949A1 (en) * | 2012-05-27 | 2013-12-05 | Ning Xi | Substituted quinoline compounds and methods of use |
| NZ711946A (en) | 2013-03-14 | 2020-05-29 | Icahn School Med Mount Sinai | Newcastle disease viruses and uses thereof |
| TWI649308B (zh) * | 2013-07-24 | 2019-02-01 | 小野藥品工業股份有限公司 | 喹啉衍生物 |
| GB201410826D0 (en) * | 2014-06-18 | 2014-07-30 | Bergenbio As | Anti-axl antibodies |
| GB201410825D0 (en) * | 2014-06-18 | 2014-07-30 | Bergenbio As | Anti-axl antibodies |
| EP3226856A4 (en) | 2014-12-02 | 2018-07-11 | Celgene Corporation | Combination therapies |
| US10208121B2 (en) * | 2014-12-18 | 2019-02-19 | Bergen Teknologioverforing As | Anti-Axl antagonistic antibodies |
| GB201509338D0 (en) | 2015-05-29 | 2015-07-15 | Bergenbio As | Combination therapy |
-
2015
- 2015-05-29 GB GBGB1509338.8A patent/GB201509338D0/en not_active Ceased
- 2015-09-16 GB GBGB1516442.9A patent/GB201516442D0/en not_active Ceased
-
2016
- 2016-05-27 EP EP16726396.1A patent/EP3302481A1/en active Pending
- 2016-05-27 WO PCT/GB2016/051542 patent/WO2016193680A1/en not_active Ceased
- 2016-05-27 JP JP2018513923A patent/JP6795585B2/ja active Active
- 2016-05-27 EP EP20211207.4A patent/EP3804723A1/en active Pending
- 2016-05-27 US US15/577,804 patent/US20180153888A1/en not_active Abandoned
-
2020
- 2020-01-09 US US16/738,103 patent/US11534440B2/en active Active
- 2020-03-05 JP JP2020038089A patent/JP7229194B2/ja active Active
-
2022
- 2022-07-15 JP JP2022114274A patent/JP7549627B2/ja active Active
- 2022-12-16 US US18/067,408 patent/US20230149397A1/en active Pending
-
2024
- 2024-03-26 US US18/616,625 patent/US20240277707A1/en active Pending
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