JP2020507569A5 - - Google Patents
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- JP2020507569A5 JP2020507569A5 JP2019542717A JP2019542717A JP2020507569A5 JP 2020507569 A5 JP2020507569 A5 JP 2020507569A5 JP 2019542717 A JP2019542717 A JP 2019542717A JP 2019542717 A JP2019542717 A JP 2019542717A JP 2020507569 A5 JP2020507569 A5 JP 2020507569A5
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- 125000003275 alpha amino acid group Chemical group 0.000 claims description 103
- 238000000034 method Methods 0.000 claims description 21
- 239000002955 immunomodulating agent Substances 0.000 claims description 19
- 206010028980 Neoplasm Diseases 0.000 claims description 12
- 150000001875 compounds Chemical class 0.000 claims description 12
- -1 1H-pyrazole-1-yl Chemical group 0.000 claims description 11
- 201000011510 cancer Diseases 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 206010061424 Anal cancer Diseases 0.000 claims description 2
- 208000007860 Anus Neoplasms Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 201000009030 Carcinoma Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 206010062878 Gastrooesophageal cancer Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims description 2
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 201000011165 anus cancer Diseases 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 229950009791 durvalumab Drugs 0.000 claims description 2
- 201000006974 gastroesophageal cancer Diseases 0.000 claims description 2
- 201000010536 head and neck cancer Diseases 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 201000005787 hematologic cancer Diseases 0.000 claims description 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims description 2
- 229960005386 ipilimumab Drugs 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 210000004698 lymphocyte Anatomy 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 2
- 229960003301 nivolumab Drugs 0.000 claims description 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 229960002621 pembrolizumab Drugs 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 229950007217 tremelimumab Drugs 0.000 claims description 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 2
- XSLJSHJSFPBCAB-UHFFFAOYSA-N 1-(4-amino-5-bromo-6-pyrazol-1-ylpyrimidin-2-yl)pyrazol-4-ol Chemical compound NC1=NC(=NC(=C1Br)N1N=CC=C1)N1N=CC(=C1)O XSLJSHJSFPBCAB-UHFFFAOYSA-N 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 230000001413 cellular effect Effects 0.000 claims 1
- ATFXVNUWQOXRRU-UHFFFAOYSA-N taminadenant Chemical class BrC=1C(N)=NC(N2N=CC=C2)=NC=1N1C=CC=N1 ATFXVNUWQOXRRU-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 description 12
- 150000001413 amino acids Chemical class 0.000 description 5
- 241001024304 Mino Species 0.000 description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 3
- 102000007471 Adenosine A2A receptor Human genes 0.000 description 1
- 108010085277 Adenosine A2A receptor Proteins 0.000 description 1
- 208000003950 B-cell lymphoma Diseases 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762457219P | 2017-02-10 | 2017-02-10 | |
| US62/457,219 | 2017-02-10 | ||
| PCT/IB2018/050783 WO2018146612A1 (en) | 2017-02-10 | 2018-02-08 | 1-(4-amino-5-bromo-6-(1 h-pyrazol-1-yl)pyrimidin-2-yl)-1 h-pyrazol-4-ol and use thereof in the treatment of cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020507569A JP2020507569A (ja) | 2020-03-12 |
| JP2020507569A5 true JP2020507569A5 (enExample) | 2021-03-18 |
| JP7161481B2 JP7161481B2 (ja) | 2022-10-26 |
Family
ID=61274309
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019542717A Active JP7161481B2 (ja) | 2017-02-10 | 2018-02-08 | １－（４－アミノ－５－ブロモ－６－（１ｈ－ピラゾール－１－イル）ピリミジン－２－イル）－１ｈ－ピラゾール－４－オール及びがんの治療におけるその使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US11078191B2 (enExample) |
| EP (1) | EP3579874B1 (enExample) |
| JP (1) | JP7161481B2 (enExample) |
| KR (1) | KR20190115053A (enExample) |
| CN (1) | CN110290808B (enExample) |
| AU (2) | AU2018217963B2 (enExample) |
| CA (1) | CA3051986A1 (enExample) |
| DK (1) | DK3579874T3 (enExample) |
| ES (1) | ES2893006T3 (enExample) |
| HU (1) | HUE057337T2 (enExample) |
| IL (1) | IL268549B (enExample) |
| PL (1) | PL3579874T3 (enExample) |
| PT (1) | PT3579874T (enExample) |
| SI (1) | SI3579874T1 (enExample) |
| WO (1) | WO2018146612A1 (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3389712B1 (en) * | 2015-12-17 | 2024-04-10 | Novartis AG | Antibody molecules to pd-1 and uses thereof |
| JOP20190279A1 (ar) * | 2017-05-31 | 2019-11-28 | Novartis Ag | الصور البلورية من 5-برومو -2، 6-داي (1h-بيرازول -1-يل) بيريميدين -4- أمين وأملاح جديدة |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
| IL129299A0 (en) | 1999-03-31 | 2000-02-17 | Mor Research Applic Ltd | Monoclonal antibodies antigens and diagnosis of malignant diseases |
| IL149820A0 (en) | 2002-05-23 | 2002-11-10 | Curetech Ltd | Humanized immunomodulatory monoclonal antibodies for the treatment of neoplastic disease or immunodeficiency |
| US7119200B2 (en) * | 2002-09-04 | 2006-10-10 | Schering Corporation | Pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| CN101899114A (zh) | 2002-12-23 | 2010-12-01 | 惠氏公司 | 抗pd-1抗体及其用途 |
| CN109485727A (zh) | 2005-05-09 | 2019-03-19 | 小野药品工业株式会社 | 程序性死亡-1(pd-1)的人单克隆抗体及使用抗pd-1抗体来治疗癌症的方法 |
| KR101411165B1 (ko) | 2005-07-01 | 2014-06-25 | 메다렉스, 엘.엘.시. | 예정 사멸 리간드 1 (피디-엘1)에 대한 인간 모노클로날항체 |
| NZ600758A (en) | 2007-06-18 | 2013-09-27 | Merck Sharp & Dohme | Antibodies to human programmed death receptor pd-1 |
| EP2262837A4 (en) | 2008-03-12 | 2011-04-06 | Merck Sharp & Dohme | PD-1 BINDING PROTEINS |
| CA2735006A1 (en) | 2008-08-25 | 2010-03-11 | Amplimmune, Inc. | Pd-1 antagonists and methods of use thereof |
| EP2342229A1 (en) | 2008-09-12 | 2011-07-13 | ISIS Innovation Limited | Pd-1 specific antibodies and uses thereof |
| ES2592216T3 (es) | 2008-09-26 | 2016-11-28 | Dana-Farber Cancer Institute, Inc. | Anticuerpos anti-PD-1, PD-L1 y PD-L2 humanos y sus usos |
| WO2010077634A1 (en) | 2008-12-09 | 2010-07-08 | Genentech, Inc. | Anti-pd-l1 antibodies and their use to enhance t-cell function |
| US8741295B2 (en) | 2009-02-09 | 2014-06-03 | Universite De La Mediterranee | PD-1 antibodies and PD-L1 antibodies and uses thereof |
| US20130017199A1 (en) | 2009-11-24 | 2013-01-17 | AMPLIMMUNE ,Inc. a corporation | Simultaneous inhibition of pd-l1/pd-l2 |
| EP2545078A1 (en) | 2010-03-11 | 2013-01-16 | UCB Pharma, S.A. | Pd-1 antibody |
| ES2365960B1 (es) | 2010-03-31 | 2012-06-04 | Palobiofarma, S.L | Nuevos antagonistas de los receptores de adenosina. |
| US8907053B2 (en) | 2010-06-25 | 2014-12-09 | Aurigene Discovery Technologies Limited | Immunosuppression modulating compounds |
| PL2699264T3 (pl) | 2011-04-20 | 2018-08-31 | Medimmune, Llc | Przeciwciała i inne cząsteczki wiążące B7-H1 i PD-1 |
| LT2734551T (lt) | 2011-07-24 | 2018-04-10 | Cure Tech Ltd. | Humanizuotų imunomoduliuojančių monokloninių antikūnų variantai |
| EP2785375B1 (en) | 2011-11-28 | 2020-07-22 | Merck Patent GmbH | Anti-pd-l1 antibodies and uses thereof |
| HRP20210122T1 (hr) | 2013-05-02 | 2021-04-16 | Anaptysbio, Inc. | Protutijela usmjerena protiv programirane smrti-1 (pd-1) |
| CN111423511B (zh) | 2013-05-31 | 2024-02-23 | 索伦托药业有限公司 | 与pd-1结合的抗原结合蛋白 |
| KR20160013049A (ko) * | 2013-06-03 | 2016-02-03 | 노파르티스 아게 | 항-pd-l1 항체 및 mek 억제제 및/또는 braf 억제제의 조합물 |
| WO2014209804A1 (en) | 2013-06-24 | 2014-12-31 | Biomed Valley Discoveries, Inc. | Bispecific antibodies |
| ES2792183T3 (es) | 2013-09-13 | 2020-11-10 | Beigene Switzerland Gmbh | Anticuerpos anti-PD1 y su uso como productos terapéuticos y de diagnóstico |
| GB201320729D0 (en) * | 2013-11-25 | 2014-01-08 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| PE20160953A1 (es) | 2013-12-12 | 2016-09-26 | Shanghai hengrui pharmaceutical co ltd | Anticuerpo pd-1, fragmento de union al antigeno de este y uso medico de este |
| TWI681969B (zh) | 2014-01-23 | 2020-01-11 | 美商再生元醫藥公司 | 針對ｐｄ-１的人類抗體 |
| JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
| TWI693232B (zh) | 2014-06-26 | 2020-05-11 | 美商宏觀基因股份有限公司 | 與pd-1和lag-3具有免疫反應性的共價結合的雙抗體和其使用方法 |
| MX389663B (es) | 2014-10-14 | 2025-03-20 | Novartis Ag | Moleculas de anticuerpo que se unen a pd-l1 y usos de las mismas. |
| TWI595006B (zh) | 2014-12-09 | 2017-08-11 | 禮納特神經系統科學公司 | 抗ｐｄ－１抗體類和使用彼等之方法 |
| SG10202111808WA (en) * | 2015-08-11 | 2021-11-29 | Novartis Ag | 5-bromo-2,6-di-(1h-pyrazol-1-yl)pyrimidin-4-amine for use in the treatment of cancer |
-
2018
- 2018-02-08 CA CA3051986A patent/CA3051986A1/en active Pending
- 2018-02-08 KR KR1020197025984A patent/KR20190115053A/ko not_active Abandoned
- 2018-02-08 HU HUE18707151A patent/HUE057337T2/hu unknown
- 2018-02-08 EP EP18707151.9A patent/EP3579874B1/en active Active
- 2018-02-08 WO PCT/IB2018/050783 patent/WO2018146612A1/en not_active Ceased
- 2018-02-08 CN CN201880011779.3A patent/CN110290808B/zh active Active
- 2018-02-08 SI SI201830420T patent/SI3579874T1/sl unknown
- 2018-02-08 PT PT18707151T patent/PT3579874T/pt unknown
- 2018-02-08 ES ES18707151T patent/ES2893006T3/es active Active
- 2018-02-08 PL PL18707151T patent/PL3579874T3/pl unknown
- 2018-02-08 US US16/484,183 patent/US11078191B2/en not_active Expired - Fee Related
- 2018-02-08 DK DK18707151.9T patent/DK3579874T3/da active
- 2018-02-08 AU AU2018217963A patent/AU2018217963B2/en not_active Ceased
- 2018-02-08 JP JP2019542717A patent/JP7161481B2/ja active Active
-
2019
- 2019-08-06 IL IL268549A patent/IL268549B/en unknown
-
2020
- 2020-10-19 AU AU2020256467A patent/AU2020256467B2/en not_active Ceased
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