JP2018525441A5 - - Google Patents
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- Publication number
- JP2018525441A5 JP2018525441A5 JP2018525826A JP2018525826A JP2018525441A5 JP 2018525441 A5 JP2018525441 A5 JP 2018525441A5 JP 2018525826 A JP2018525826 A JP 2018525826A JP 2018525826 A JP2018525826 A JP 2018525826A JP 2018525441 A5 JP2018525441 A5 JP 2018525441A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- branched
- linear
- halide
- compound according
- 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 70
- 125000000217 alkyl group Chemical group 0.000 claims description 44
- 150000004820 halides Chemical class 0.000 claims description 28
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 25
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 20
- 125000003118 aryl group Chemical group 0.000 claims description 19
- 229910052799 carbon Inorganic materials 0.000 claims description 18
- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
- 125000000623 heterocyclic group Chemical group 0.000 claims description 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 17
- 201000010099 disease Diseases 0.000 claims description 15
- GJVFBWCTGUSGDD-UHFFFAOYSA-L pentamethonium bromide Chemical compound [Br-].[Br-].C[N+](C)(C)CCCCC[N+](C)(C)C GJVFBWCTGUSGDD-UHFFFAOYSA-L 0.000 claims description 15
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 14
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- 229920006395 saturated elastomer Polymers 0.000 claims description 14
- 206010028980 Neoplasm Diseases 0.000 claims description 12
- 201000011510 cancer Diseases 0.000 claims description 12
- 150000001408 amides Chemical class 0.000 claims description 10
- 150000002148 esters Chemical class 0.000 claims description 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 10
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims description 9
- 230000003211 malignant effect Effects 0.000 claims description 9
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims description 7
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 6
- 206010006187 Breast cancer Diseases 0.000 claims description 6
- 208000026310 Breast neoplasm Diseases 0.000 claims description 6
- 208000034578 Multiple myelomas Diseases 0.000 claims description 6
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 6
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 6
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims description 6
- 201000001441 melanoma Diseases 0.000 claims description 6
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 5
- 208000035475 disorder Diseases 0.000 claims description 5
- 208000032839 leukemia Diseases 0.000 claims description 5
- 230000004044 response Effects 0.000 claims description 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 4
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 4
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
- 238000002619 cancer immunotherapy Methods 0.000 claims description 4
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 3
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 3
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims description 3
- 206010060862 Prostate cancer Diseases 0.000 claims description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
- 239000000090 biomarker Substances 0.000 claims description 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 3
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims description 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 3
- 201000010536 head and neck cancer Diseases 0.000 claims description 3
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 3
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 description 14
- 102000008122 Casein Kinase I Human genes 0.000 description 9
- 108010049812 Casein Kinase I Proteins 0.000 description 9
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 9
- 102000006940 Interleukin-1 Receptor-Associated Kinases Human genes 0.000 description 6
- 108010072621 Interleukin-1 Receptor-Associated Kinases Proteins 0.000 description 6
- 230000002401 inhibitory effect Effects 0.000 description 6
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 5
- 210000004027 cell Anatomy 0.000 description 5
- 230000001939 inductive effect Effects 0.000 description 4
- 239000003112 inhibitor Substances 0.000 description 4
- 150000001350 alkyl halides Chemical class 0.000 description 3
- 208000024891 symptom Diseases 0.000 description 3
- 102000008096 B7-H1 Antigen Human genes 0.000 description 2
- 108010074708 B7-H1 Antigen Proteins 0.000 description 2
- 102000045959 Interleukin-1 Receptor-Like 1 Human genes 0.000 description 2
- 108700003107 Interleukin-1 Receptor-Like 1 Proteins 0.000 description 2
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- 125000002252 acyl group Chemical group 0.000 description 2
- 230000006023 anti-tumor response Effects 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- -1 hydroxyl compound Chemical class 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 1
- 210000001185 bone marrow Anatomy 0.000 description 1
- 238000000684 flow cytometry Methods 0.000 description 1
- 238000009169 immunotherapy Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562200846P | 2015-08-04 | 2015-08-04 | |
| US62/200,846 | 2015-08-04 | ||
| US201562268750P | 2015-12-17 | 2015-12-17 | |
| US62/268,750 | 2015-12-17 | ||
| PCT/IL2016/050852 WO2017021969A1 (en) | 2015-08-04 | 2016-08-04 | Pyrazole pyrimidine derivative and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018525441A JP2018525441A (ja) | 2018-09-06 |
| JP2018525441A5 true JP2018525441A5 (enExample) | 2019-09-19 |
| JP7083309B2 JP7083309B2 (ja) | 2022-06-10 |
Family
ID=56738143
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018525826A Active JP7083309B2 (ja) | 2015-08-04 | 2016-08-04 | ピラゾールピリミジン誘導体及びその使用 |
Country Status (23)
| Country | Link |
|---|---|
| US (4) | US10376511B2 (enExample) |
| EP (1) | EP3331877B1 (enExample) |
| JP (1) | JP7083309B2 (enExample) |
| KR (1) | KR102698366B1 (enExample) |
| CN (1) | CN108137562B (enExample) |
| AU (2) | AU2016304464B2 (enExample) |
| CA (1) | CA2994644A1 (enExample) |
| CY (1) | CY1124898T1 (enExample) |
| DK (1) | DK3331877T3 (enExample) |
| ES (1) | ES2901349T3 (enExample) |
| HR (1) | HRP20211949T1 (enExample) |
| HU (1) | HUE057607T2 (enExample) |
| IL (1) | IL257282B (enExample) |
| LT (1) | LT3331877T (enExample) |
| MX (1) | MX384172B (enExample) |
| PL (1) | PL3331877T3 (enExample) |
| PT (1) | PT3331877T (enExample) |
| RS (1) | RS62728B1 (enExample) |
| RU (1) | RU2735522C2 (enExample) |
| SI (1) | SI3331877T1 (enExample) |
| SM (1) | SMT202100720T1 (enExample) |
| WO (1) | WO2017021969A1 (enExample) |
| ZA (1) | ZA201800671B (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10376511B2 (en) * | 2015-08-04 | 2019-08-13 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Pyrazole pyrimidine derivative and uses thereof |
| MX394556B (es) * | 2017-02-01 | 2025-03-24 | Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd | Derivados de n1-(4-(5-(ciclopropilmetil)-1-metil-1h-pirazol-4-il) piridin-2-il) ciclohexano-1,4-diamina y compuestos relacionados como inhibidores de ck1 y/o irak1 para tratar cáncer. |
| TW202340194A (zh) | 2017-02-16 | 2023-10-16 | 美商基利科學股份有限公司 | 吡咯并[1,2-b]嗒𠯤衍生物 |
| EP3749666A1 (en) * | 2018-02-08 | 2020-12-16 | Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. | Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use |
| TWI842978B (zh) | 2018-07-13 | 2024-05-21 | 美商基利科學股份有限公司 | 衍生物 |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| US11384083B2 (en) | 2019-02-15 | 2022-07-12 | Incyte Corporation | Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors |
| TW202100520A (zh) | 2019-03-05 | 2021-01-01 | 美商英塞特公司 | 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物 |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| WO2020223469A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer |
| BR112021024330A2 (pt) * | 2019-06-03 | 2022-01-11 | Biotheryx Inc | Sais cristalinos não higroscópicos de um composto de pirazol, e composições farmacêuticas e uso dos mesmos |
| WO2021000957A1 (zh) * | 2019-07-04 | 2021-01-07 | 北京国鸿生物医药科技有限公司 | 一种杂环化合物、其药物组合物及用途 |
| CA3150681A1 (en) | 2019-08-14 | 2021-02-18 | Incyte Corporation | Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| US11851426B2 (en) | 2019-10-11 | 2023-12-26 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| EP4090159A4 (en) * | 2020-01-13 | 2024-01-24 | Yissum Research Development Company of the Hebrew University of Jerusalem Ltd | PYRAZOLYLPYRIMIDINES AND THEIR USE |
| WO2021155050A1 (en) * | 2020-01-29 | 2021-08-05 | Biotheryx, Inc. | Kinase modulators, pharmaceutical compositions, and therapeutic applications |
| CN115362151B (zh) * | 2020-03-26 | 2025-02-11 | 詹森药业有限公司 | 作为单酰基甘油脂肪酶调节剂的芳基哌啶 |
| EP4313053A4 (en) * | 2021-03-24 | 2025-03-05 | Yissum Research Development Company of the Hebrew University of Jerusalem, Ltd. | Pyrazolylpyrimidines for treating malignant solid tumor |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US11752151B2 (en) * | 2021-07-12 | 2023-09-12 | Buddhist Tzu Chi Medical Foundation | Method for enhancing hair growth |
| US20230053307A1 (en) * | 2021-07-19 | 2023-02-16 | Buddhist Tzu Chi Medical Foundation | Method for preventing or treating skin disorders and conditions |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| WO2025199434A1 (en) * | 2024-03-21 | 2025-09-25 | Edgewood Oncology | Methods of treating breast cancer using a pyrazole compound |
| WO2025199440A1 (en) * | 2024-03-21 | 2025-09-25 | Edgewood Oncology | Methods of treating liposarcoma using a pyrazole compound |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE407132T1 (de) * | 2000-12-05 | 2008-09-15 | Vertex Pharma | Inhibitoren von c-jun n-terminalen kinasen (jnk) und anderen proteinkinasen |
| WO2002092573A2 (en) * | 2001-05-16 | 2002-11-21 | Vertex Pharmaceuticals Incorporated | Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases |
| GB0215844D0 (en) * | 2002-07-09 | 2002-08-14 | Novartis Ag | Organic compounds |
| CN101693695A (zh) | 2004-03-30 | 2010-04-14 | 大正制药株式会社 | 嘧啶衍生物以及与其应用有关的治疗方法 |
| JP2007145819A (ja) * | 2005-10-28 | 2007-06-14 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
| WO2007129195A2 (en) * | 2006-05-04 | 2007-11-15 | Pfizer Products Inc. | 4-pyrimidine-5-amino-pyrazole compounds |
| US20100063049A1 (en) * | 2006-05-26 | 2010-03-11 | Clifford Jones | 2-carbocycloamino-4-imidazolylpyrimidines as agents for the inhbition of cell proliferation |
| CA2707989A1 (en) * | 2007-12-07 | 2009-06-11 | Novartis Ag | Pyrazole derivatives and use thereof as inhibitors of cyclin dependent kinases |
| KR101990605B1 (ko) * | 2011-11-04 | 2019-06-18 | 자스코 파머수티컬스, 엘엘씨 | 아미노피리미딘 키나아제 억제제 |
| CN106232122A (zh) * | 2013-09-27 | 2016-12-14 | 林伯士艾瑞斯公司 | Irak抑制剂和其用途 |
| EP3057956B1 (en) * | 2013-10-18 | 2021-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7) |
| US10376511B2 (en) | 2015-08-04 | 2019-08-13 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Pyrazole pyrimidine derivative and uses thereof |
| MX394556B (es) * | 2017-02-01 | 2025-03-24 | Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd | Derivados de n1-(4-(5-(ciclopropilmetil)-1-metil-1h-pirazol-4-il) piridin-2-il) ciclohexano-1,4-diamina y compuestos relacionados como inhibidores de ck1 y/o irak1 para tratar cáncer. |
| EP3749666A1 (en) | 2018-02-08 | 2020-12-16 | Yissum Research Development Company of the Hebrew University of Jerusalem Ltd. | Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use |
-
2016
- 2016-08-04 US US15/748,536 patent/US10376511B2/en active Active
- 2016-08-04 WO PCT/IL2016/050852 patent/WO2017021969A1/en not_active Ceased
- 2016-08-04 SM SM20210720T patent/SMT202100720T1/it unknown
- 2016-08-04 HU HUE16753709A patent/HUE057607T2/hu unknown
- 2016-08-04 PL PL16753709T patent/PL3331877T3/pl unknown
- 2016-08-04 RS RS20211558A patent/RS62728B1/sr unknown
- 2016-08-04 AU AU2016304464A patent/AU2016304464B2/en active Active
- 2016-08-04 LT LTEPPCT/IL2016/050852T patent/LT3331877T/lt unknown
- 2016-08-04 PT PT167537091T patent/PT3331877T/pt unknown
- 2016-08-04 DK DK16753709.1T patent/DK3331877T3/da active
- 2016-08-04 KR KR1020187006128A patent/KR102698366B1/ko active Active
- 2016-08-04 EP EP16753709.1A patent/EP3331877B1/en active Active
- 2016-08-04 HR HRP20211949TT patent/HRP20211949T1/hr unknown
- 2016-08-04 MX MX2018001395A patent/MX384172B/es unknown
- 2016-08-04 RU RU2018107668A patent/RU2735522C2/ru active
- 2016-08-04 ES ES16753709T patent/ES2901349T3/es active Active
- 2016-08-04 JP JP2018525826A patent/JP7083309B2/ja active Active
- 2016-08-04 SI SI201631426T patent/SI3331877T1/sl unknown
- 2016-08-04 CN CN201680059148.XA patent/CN108137562B/zh active Active
- 2016-08-04 CA CA2994644A patent/CA2994644A1/en active Pending
-
2018
- 2018-01-31 IL IL257282A patent/IL257282B/en active IP Right Grant
- 2018-01-31 ZA ZA2018/00671A patent/ZA201800671B/en unknown
-
2019
- 2019-08-12 US US16/538,550 patent/US10960003B2/en active Active
-
2021
- 2021-02-10 AU AU2021200839A patent/AU2021200839A1/en not_active Abandoned
- 2021-03-29 US US17/215,959 patent/US11925641B2/en active Active
- 2021-12-21 CY CY20211101124T patent/CY1124898T1/el unknown
-
2024
- 2024-02-05 US US18/432,931 patent/US12514859B2/en active Active
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