JP2018516917A5 - - Google Patents
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- JP2018516917A5 JP2018516917A5 JP2017561810A JP2017561810A JP2018516917A5 JP 2018516917 A5 JP2018516917 A5 JP 2018516917A5 JP 2017561810 A JP2017561810 A JP 2017561810A JP 2017561810 A JP2017561810 A JP 2017561810A JP 2018516917 A5 JP2018516917 A5 JP 2018516917A5
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- JP
- Japan
- Prior art keywords
- compound
- cancer
- pharmaceutically acceptable
- stereoisomer
- acceptable salt
- 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
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- 150000001875 compounds Chemical class 0.000 claims 28
- 150000003839 salts Chemical class 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 206010028980 Neoplasm Diseases 0.000 claims 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 239000001257 hydrogen Substances 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 206010025323 Lymphomas Diseases 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000011594 Autoinflammatory disease Diseases 0.000 claims 2
- 208000035473 Communicable disease Diseases 0.000 claims 2
- 102100038111 Cyclin-dependent kinase 12 Human genes 0.000 claims 2
- 102100038114 Cyclin-dependent kinase 13 Human genes 0.000 claims 2
- 102100033144 Cyclin-dependent kinase 18 Human genes 0.000 claims 2
- 102100026810 Cyclin-dependent kinase 7 Human genes 0.000 claims 2
- 102100024457 Cyclin-dependent kinase 9 Human genes 0.000 claims 2
- 101000884345 Homo sapiens Cyclin-dependent kinase 12 Proteins 0.000 claims 2
- 101000884348 Homo sapiens Cyclin-dependent kinase 13 Proteins 0.000 claims 2
- 101000911952 Homo sapiens Cyclin-dependent kinase 7 Proteins 0.000 claims 2
- 101000980930 Homo sapiens Cyclin-dependent kinase 9 Proteins 0.000 claims 2
- 108010039798 PCTAIRE-3 protein kinase Proteins 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 230000002103 transcriptional effect Effects 0.000 claims 2
- GHYOCDFICYLMRF-UTIIJYGPSA-N (2S,3R)-N-[(2S)-3-(cyclopenten-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]propanoyl]amino]propanamide Chemical compound C1(=CCCC1)C[C@@H](C(=O)[C@@]1(OC1)C)NC([C@H]([C@@H](C1=CC=C(C=C1)OC)O)NC([C@H](C)NC(CN1CCOCC1)=O)=O)=O GHYOCDFICYLMRF-UTIIJYGPSA-N 0.000 claims 1
- WWTBZEKOSBFBEM-SPWPXUSOSA-N (2s)-2-[[2-benzyl-3-[hydroxy-[(1r)-2-phenyl-1-(phenylmethoxycarbonylamino)ethyl]phosphoryl]propanoyl]amino]-3-(1h-indol-3-yl)propanoic acid Chemical compound N([C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)O)C(=O)C(CP(O)(=O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1C=CC=CC=1)CC1=CC=CC=C1 WWTBZEKOSBFBEM-SPWPXUSOSA-N 0.000 claims 1
- HUWSZNZAROKDRZ-RRLWZMAJSA-N (3r,4r)-3-azaniumyl-5-[[(2s,3r)-1-[(2s)-2,3-dicarboxypyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-5-oxo-4-sulfanylpentane-1-sulfonate Chemical compound OS(=O)(=O)CC[C@@H](N)[C@@H](S)C(=O)N[C@@H]([C@H](C)CC)C(=O)N1CCC(C(O)=O)[C@H]1C(O)=O HUWSZNZAROKDRZ-RRLWZMAJSA-N 0.000 claims 1
- PYRKKGOKRMZEIT-UHFFFAOYSA-N 2-[6-(2-cyclopropylethoxy)-9-(2-hydroxy-2-methylpropyl)-1h-phenanthro[9,10-d]imidazol-2-yl]-5-fluorobenzene-1,3-dicarbonitrile Chemical compound C1=C2C3=CC(CC(C)(O)C)=CC=C3C=3NC(C=4C(=CC(F)=CC=4C#N)C#N)=NC=3C2=CC=C1OCCC1CC1 PYRKKGOKRMZEIT-UHFFFAOYSA-N 0.000 claims 1
- FMKGJQHNYMWDFJ-CVEARBPZSA-N 2-[[4-(2,2-difluoropropoxy)pyrimidin-5-yl]methylamino]-4-[[(1R,4S)-4-hydroxy-3,3-dimethylcyclohexyl]amino]pyrimidine-5-carbonitrile Chemical compound FC(COC1=NC=NC=C1CNC1=NC=C(C(=N1)N[C@H]1CC([C@H](CC1)O)(C)C)C#N)(C)F FMKGJQHNYMWDFJ-CVEARBPZSA-N 0.000 claims 1
- LFOIDLOIBZFWDO-UHFFFAOYSA-N 2-methoxy-6-[6-methoxy-4-[(3-phenylmethoxyphenyl)methoxy]-1-benzofuran-2-yl]imidazo[2,1-b][1,3,4]thiadiazole Chemical compound N1=C2SC(OC)=NN2C=C1C(OC1=CC(OC)=C2)=CC1=C2OCC(C=1)=CC=CC=1OCC1=CC=CC=C1 LFOIDLOIBZFWDO-UHFFFAOYSA-N 0.000 claims 1
- BGAJNPLDJJBRHK-UHFFFAOYSA-N 3-[2-[5-(3-chloro-4-propan-2-yloxyphenyl)-1,3,4-thiadiazol-2-yl]-3-methyl-6,7-dihydro-4h-pyrazolo[4,3-c]pyridin-5-yl]propanoic acid Chemical compound C1=C(Cl)C(OC(C)C)=CC=C1C1=NN=C(N2C(=C3CN(CCC(O)=O)CCC3=N2)C)S1 BGAJNPLDJJBRHK-UHFFFAOYSA-N 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000004463 Follicular Adenocarcinoma Diseases 0.000 claims 1
- 208000022072 Gallbladder Neoplasms Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas 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
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms 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
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 1
- 230000001594 aberrant effect Effects 0.000 claims 1
- 229940035676 analgesics Drugs 0.000 claims 1
- 239000000730 antalgic agent Substances 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 229940125797 compound 12 Drugs 0.000 claims 1
- 229940126208 compound 22 Drugs 0.000 claims 1
- 229940127113 compound 57 Drugs 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000004966 cyanoalkyl group Chemical group 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 201000010175 gallbladder cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- IOMMMLWIABWRKL-WUTDNEBXSA-N nazartinib Chemical compound C1N(C(=O)/C=C/CN(C)C)CCCC[C@H]1N1C2=C(Cl)C=CC=C2N=C1NC(=O)C1=CC=NC(C)=C1 IOMMMLWIABWRKL-WUTDNEBXSA-N 0.000 claims 1
- 230000009826 neoplastic cell growth Effects 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 208000017572 squamous cell neoplasm Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 208000013077 thyroid gland carcinoma Diseases 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 230000035897 transcription Effects 0.000 claims 1
- 238000013518 transcription Methods 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 (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN2803CH2015 | 2015-06-04 | ||
| IN2803/CHE/2015 | 2015-06-04 | ||
| IN6214/CHE/2015 | 2015-11-18 | ||
| IN6214CH2015 | 2015-11-18 | ||
| PCT/IB2016/053267 WO2016193939A1 (en) | 2015-06-04 | 2016-06-03 | Substituted heterocyclyl derivatives as cdk inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020131775A Division JP7033764B2 (ja) | 2015-06-04 | 2020-08-03 | Ｃｄｋ阻害剤としての置換型ヘテロシクリル誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018516917A JP2018516917A (ja) | 2018-06-28 |
| JP2018516917A5 true JP2018516917A5 (https=) | 2019-07-04 |
| JP6750806B2 JP6750806B2 (ja) | 2020-09-02 |
Family
ID=57440798
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017561810A Active JP6750806B2 (ja) | 2015-06-04 | 2016-06-03 | Ｃｄｋ阻害剤としての置換型ヘテロシクリル誘導体 |
| JP2020131775A Expired - Fee Related JP7033764B2 (ja) | 2015-06-04 | 2020-08-03 | Ｃｄｋ阻害剤としての置換型ヘテロシクリル誘導体 |
| JP2022024039A Active JP7482918B2 (ja) | 2015-06-04 | 2022-02-18 | Ｃｄｋ阻害剤としての置換型ヘテロシクリル誘導体 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020131775A Expired - Fee Related JP7033764B2 (ja) | 2015-06-04 | 2020-08-03 | Ｃｄｋ阻害剤としての置換型ヘテロシクリル誘導体 |
| JP2022024039A Active JP7482918B2 (ja) | 2015-06-04 | 2022-02-18 | Ｃｄｋ阻害剤としての置換型ヘテロシクリル誘導体 |
Country Status (20)
| Country | Link |
|---|---|
| US (3) | US10689347B2 (https=) |
| EP (2) | EP4342540A3 (https=) |
| JP (3) | JP6750806B2 (https=) |
| KR (1) | KR102691467B1 (https=) |
| CN (2) | CN113773257A (https=) |
| AU (3) | AU2016272908B2 (https=) |
| CA (1) | CA2987552A1 (https=) |
| CU (1) | CU24496B1 (https=) |
| DK (1) | DK3302448T3 (https=) |
| EA (1) | EA037236B1 (https=) |
| FI (1) | FI3302448T3 (https=) |
| HR (1) | HRP20240101T1 (https=) |
| IL (2) | IL255960B (https=) |
| LT (1) | LT3302448T (https=) |
| MX (2) | MX375639B (https=) |
| MY (2) | MY190459A (https=) |
| PH (1) | PH12017502179B1 (https=) |
| SI (1) | SI3302448T1 (https=) |
| WO (1) | WO2016193939A1 (https=) |
| ZA (1) | ZA201800022B (https=) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6854762B2 (ja) | 2014-12-23 | 2021-04-07 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | サイクリン依存性キナーゼ７（ｃｄｋ７）の阻害剤 |
| ES2899196T3 (es) * | 2015-03-09 | 2022-03-10 | Aurigene Discovery Tech Ltd | Derivados de pirazolo[1,5-a][1,3,5]triazina y de pirazolo[1,5-a]pirimidina como inhibidores de CDK |
| USRE50776E1 (en) | 2015-03-27 | 2026-02-03 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| SI3302448T1 (sl) * | 2015-06-04 | 2024-03-29 | Aurigene Oncology Limited | Substituirani heterociklični derivati kot inhibitorji cdk |
| GB201617548D0 (en) | 2016-10-17 | 2016-11-30 | Linnane Pharma Ab | Novel biological factor |
| TWI703149B (zh) | 2017-11-16 | 2020-09-01 | 美商美國禮來大藥廠 | 用於抑制cdk7之化合物 |
| EP3720436A4 (en) | 2017-12-06 | 2021-06-02 | Lin Bioscience, Pty Ltd. | TUBULIN INHIBITORS |
| AU2019215799B2 (en) * | 2018-02-01 | 2022-04-14 | The University Of Sydney | Anti-cancer compounds |
| US11584737B2 (en) | 2018-03-29 | 2023-02-21 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| AU2019247885B2 (en) * | 2018-04-04 | 2023-09-07 | Aurigene Oncology Limited | Substituted pyrazole derivatives as selective CDK12/13 inhibitors |
| US11447493B2 (en) | 2018-05-02 | 2022-09-20 | Kinnate Biopharma Inc. | Inhibitors of cyclin-dependent kinases |
| CN110590747B (zh) * | 2018-06-12 | 2022-03-22 | 隆泰申医药科技(南京)有限公司 | 一种化合物、其制备方法、药物组合物和应用 |
| EP3810132A4 (en) * | 2018-06-25 | 2022-06-22 | Dana-Farber Cancer Institute, Inc. | TAIRE FAMILY KINASE INHIBITORS AND RELATED USES |
| EP3813819A4 (en) | 2018-06-29 | 2022-08-17 | Kinnate Biopharma Inc. | CYCLIN-DEPENDENT KINASE INHIBITORS |
| JP7235859B2 (ja) * | 2018-09-17 | 2023-03-08 | ユンジン ファーム．カンパニー、リミテッド | 新規なチアゾール誘導体及びその薬学的に許容される塩 |
| US12281126B2 (en) | 2018-12-28 | 2025-04-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 and uses thereof |
| CN113727707A (zh) * | 2019-04-01 | 2021-11-30 | 奥里吉恩发现科技有限公司 | 作为选择性cdk12/13抑制剂的取代5-环丙基-1h-吡唑-3-基-胺衍生物 |
| CN110845474B (zh) * | 2019-11-07 | 2021-01-12 | 四川大学 | 一种靶向i型prmt的化合物及其制备方法和应用 |
| EP4119556A1 (en) * | 2020-03-13 | 2023-01-18 | Yungjin Pharm. Co., Ltd. | Pharmaceutical composition for preventing or treating cancer comprising azole derivatives or pharmaceutically acceptable salt thereof |
| WO2021182914A1 (ko) * | 2020-03-13 | 2021-09-16 | 영진약품 주식회사 | 신규한 cdk7 억제 화합물 및 이의 약제학적으로 허용가능한 염 |
| TWI783480B (zh) * | 2020-05-27 | 2022-11-11 | 美商美國禮來大藥廠 | 用於抑制cdk7之化合物 |
| WO2022084930A2 (en) * | 2020-10-22 | 2022-04-28 | Aurigene Discovery Technologies Limited | Cancer therapy using a combination of cdk7 inhibitor with an anti-microtubule agent |
| PE20231441A1 (es) | 2020-12-18 | 2023-09-14 | Aurigene Oncology Ltd | Cocristal de un inhibidor de cdk |
| AU2022267889A1 (en) * | 2021-04-27 | 2023-11-09 | Aurigene Oncology Limited | Process for preparing a cdk inhibitor |
| US20240277722A1 (en) * | 2021-05-28 | 2024-08-22 | Aurigene Oncology Limited | Cancer therapy using a combination of cdk7 inhibitor with an anti-cancer agent |
| MX2023015245A (es) * | 2021-06-16 | 2024-01-19 | Blueprint Medicines Corp | Pirimidinil-pirazoles sustituidos como inhibidores de cdk2. |
| US11932648B2 (en) | 2021-06-28 | 2024-03-19 | Blueprint Medicines Corporation | CDK2 inhibitors |
| TW202327583A (zh) * | 2021-12-06 | 2023-07-16 | 美商艾克塞里克斯公司 | 使用ｃｄｋ７抑制劑治療癌症之方法 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
| TWI835645B (zh) | 2022-05-11 | 2024-03-11 | 日商前川製作所股份有限公司 | 切削裝置以及工件的切削方法 |
| WO2023224961A1 (en) | 2022-05-16 | 2023-11-23 | Exelixis, Inc. | Cancer therapy using a combination of a cdk7 inhibitor with an oral serd |
| CN115093397B (zh) * | 2022-06-07 | 2023-09-05 | 自贡市第三人民医院 | 一种用于治疗肿瘤的化合物、合成方法及应用 |
| CN119790056A (zh) * | 2022-09-30 | 2025-04-08 | 楚浦创制（武汉）医药科技有限公司 | 三并环类衍生物、药物组合物以及应用 |
| WO2024140653A1 (zh) * | 2022-12-27 | 2024-07-04 | 南京圣和药业股份有限公司 | 选择性cdk12/13抑制剂及其应用 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025217307A1 (en) | 2024-04-09 | 2025-10-16 | Revolution Medicines, Inc. | Methods for predicting response to a ras(on) inhibitor and combination therapies |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS57169465A (en) * | 1981-04-13 | 1982-10-19 | Showa Denko Kk | Pyrazole derivative, its preparation and herbicide |
| WO2000047553A2 (en) | 1999-02-11 | 2000-08-17 | Cor Therapeutics Inc. | ALKENYL AND ALKYNYL COMPOUNDS AS INHIBITORS OF FACTOR Xa |
| WO2001012189A1 (en) | 1999-08-12 | 2001-02-22 | Pharmacia Italia S.P.A. | 3(5)-amino-pyrazole derivatives, process for their preparation and their use as antitumor agents |
| KR100423899B1 (ko) | 2000-05-10 | 2004-03-24 | 주식회사 엘지생명과학 | 세포 증식 억제제로 유용한 1,1-디옥소이소티아졸리딘을갖는 인다졸 |
| DK1320531T3 (da) * | 2000-08-10 | 2011-01-03 | Pfizer Italia Srl | Bicyclo-pyrazoler, der er aktive som kinase inhibitorer, fremgangsmåde til fremstilling deraf og farmaceutiske sammensætninger, der indeholder disse |
| AU2002215053A1 (en) | 2000-11-27 | 2002-06-24 | Pharmacia Italia S.P.A. | Phenylacetamido- pyrazole derivatives and their use as antitumor agents |
| US6455559B1 (en) | 2001-07-19 | 2002-09-24 | Pharmacia Italia S.P.A. | Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents |
| DE10148618B4 (de) * | 2001-09-25 | 2007-05-03 | Schering Ag | Substituierte N-(1,4,5,6-Tetrahydro-cyclopentapyrazol-3-yl)-Derivate, deren Herstellung und Verwendung als Arzneimittel |
| CN1839114A (zh) | 2003-08-21 | 2006-09-27 | 默克弗罗斯特加拿大有限公司 | 组织蛋白酶半胱氨酸蛋白酶抑制剂 |
| WO2006070198A1 (en) * | 2004-12-30 | 2006-07-06 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
| MX2007008008A (es) * | 2004-12-30 | 2007-11-12 | Astex Therapeutics Ltd | Compuestos de pirazol que modulan la actividad de las cinasas cdk, gsk y aurora. |
| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
| EP1845975A1 (en) | 2005-01-21 | 2007-10-24 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors and further antitumor agents |
| GT200600457A (es) | 2005-10-13 | 2007-04-27 | Aventis Pharma Inc | Sal de fosfato dihidrogeno como antagonistas del receptor de prostaglandina d2 |
| WO2008043745A1 (en) | 2006-10-11 | 2008-04-17 | Nerviano Medical Sciences S.R.L. | Substituted pyrrolo-pyrazole derivatives as kinase inhibitors |
| WO2010002472A1 (en) * | 2008-07-02 | 2010-01-07 | Ambit Biosciences Corporation | Jak kinase modulating compounds and methods of use thereof |
| ATE544063T1 (de) | 2008-07-17 | 2012-02-15 | Koninkl Philips Electronics Nv | Nanoporenvorrichtung und verfahren zur nukleinsäureanalyse |
| SG172352A1 (en) | 2008-12-23 | 2011-07-28 | Abbott Lab | Anti-viral compounds |
| FR2943058B1 (fr) | 2009-03-11 | 2011-06-03 | Centre Nat Rech Scient | Derives de pyrazolo°1,5-a!-1,3,5-triazines, leur preparation et leur application en therapeutique. |
| EP2241619A1 (en) * | 2009-04-17 | 2010-10-20 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Development of fluorescently P-loop labeled kinases for screening of inhibitors |
| US9382239B2 (en) * | 2011-11-17 | 2016-07-05 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-Jun-N-terminal kinase (JNK) |
| EP2909194A1 (en) | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| EP3008052A1 (en) | 2013-06-13 | 2016-04-20 | Bristol-Myers Squibb Company | Macrocyclic factor viia inhibitors |
| KR20160055170A (ko) | 2013-08-30 | 2016-05-17 | 암비트 바이오사이언시즈 코포레이션 | 바이아릴 아세트아미드 화합물 및 이의 사용 방법 |
| BR112016008632A8 (pt) | 2013-10-21 | 2020-03-17 | Merck Patent Gmbh | compostos de heteroarila como inibidores de btk, seus usos, e composição farmacêutica |
| EP3129371B1 (en) | 2014-04-05 | 2020-07-29 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| FR3025075A1 (fr) * | 2014-08-28 | 2016-03-04 | Oreal | Nouveau dispositif de soin et/ou maquillage comprenant une composition d’architecture gel/gel |
| JP6854762B2 (ja) | 2014-12-23 | 2021-04-07 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | サイクリン依存性キナーゼ７（ｃｄｋ７）の阻害剤 |
| SI3302448T1 (sl) | 2015-06-04 | 2024-03-29 | Aurigene Oncology Limited | Substituirani heterociklični derivati kot inhibitorji cdk |
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2016
- 2016-06-03 SI SI201631797T patent/SI3302448T1/sl unknown
- 2016-06-03 CN CN202111184551.4A patent/CN113773257A/zh active Pending
- 2016-06-03 EP EP23203356.3A patent/EP4342540A3/en not_active Withdrawn
- 2016-06-03 PH PH1/2017/502179A patent/PH12017502179B1/en unknown
- 2016-06-03 FI FIEP16802673.0T patent/FI3302448T3/fi active
- 2016-06-03 CN CN201680045348.XA patent/CN108024970B/zh active Active
- 2016-06-03 DK DK16802673.0T patent/DK3302448T3/da active
- 2016-06-03 EA EA201890001A patent/EA037236B1/ru unknown
- 2016-06-03 MY MYPI2017001787A patent/MY190459A/en unknown
- 2016-06-03 LT LTEPPCT/IB2016/053267T patent/LT3302448T/lt unknown
- 2016-06-03 CA CA2987552A patent/CA2987552A1/en active Pending
- 2016-06-03 WO PCT/IB2016/053267 patent/WO2016193939A1/en not_active Ceased
- 2016-06-03 US US15/579,246 patent/US10689347B2/en active Active
- 2016-06-03 MX MX2017015521A patent/MX375639B/es active IP Right Grant
- 2016-06-03 HR HRP20240101TT patent/HRP20240101T1/hr unknown
- 2016-06-03 MY MYPI2021007215A patent/MY198769A/en unknown
- 2016-06-03 KR KR1020187000333A patent/KR102691467B1/ko active Active
- 2016-06-03 EP EP16802673.0A patent/EP3302448B1/en active Active
- 2016-06-03 AU AU2016272908A patent/AU2016272908B2/en active Active
- 2016-06-03 JP JP2017561810A patent/JP6750806B2/ja active Active
- 2016-06-03 CU CU2017000154A patent/CU24496B1/es unknown
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2017
- 2017-11-28 IL IL255960A patent/IL255960B/en unknown
- 2017-12-01 MX MX2020010484A patent/MX2020010484A/es unknown
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2018
- 2018-01-03 ZA ZA2018/00022A patent/ZA201800022B/en unknown
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2020
- 2020-05-06 US US16/867,761 patent/US11174232B2/en active Active
- 2020-08-03 JP JP2020131775A patent/JP7033764B2/ja not_active Expired - Fee Related
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2021
- 2021-08-04 AU AU2021212016A patent/AU2021212016B2/en not_active Ceased
- 2021-09-14 IL IL286428A patent/IL286428A/en unknown
- 2021-10-07 US US17/496,452 patent/US12331023B2/en active Active
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2022
- 2022-02-18 JP JP2022024039A patent/JP7482918B2/ja active Active
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2023
- 2023-06-06 AU AU2023203524A patent/AU2023203524A1/en not_active Abandoned
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