AU2017348322B8 - Compositions and methods for treating EZH2-mediated cancer - Google Patents
Compositions and methods for treating EZH2-mediated cancer Download PDFInfo
- Publication number
- AU2017348322B8 AU2017348322B8 AU2017348322A AU2017348322A AU2017348322B8 AU 2017348322 B8 AU2017348322 B8 AU 2017348322B8 AU 2017348322 A AU2017348322 A AU 2017348322A AU 2017348322 A AU2017348322 A AU 2017348322A AU 2017348322 B8 AU2017348322 B8 AU 2017348322B8
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- AU
- Australia
- Prior art keywords
- mmol
- ezh2
- cancer
- alkyl
- methyl
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- 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.)
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- 0 CCN(CCNNC(CCOCCOCCC(NC(N(C(CC(C)C)C(C1)O)[C@@]1C(NCc(cc1)ccc1-c1c(C)nc[s]1)=O)=O)=O)=O)C(N)=CC=C(*)c1cc(C(NCC(C2)=C(C)C=C(C)[N+]2[O-])=O)c([C@@](C)N)c(NC(C)C)c1 Chemical compound CCN(CCNNC(CCOCCOCCC(NC(N(C(CC(C)C)C(C1)O)[C@@]1C(NCc(cc1)ccc1-c1c(C)nc[s]1)=O)=O)=O)=O)C(N)=CC=C(*)c1cc(C(NCC(C2)=C(C)C=C(C)[N+]2[O-])=O)c([C@@](C)N)c(NC(C)C)c1 0.000 description 2
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- GBZGMCCZDOBVMJ-PGWNOLSTSA-N CC(C)Nc1cc(/C(/C)=C/C=C(\N)/N2CCN(CCNC(COOCCOCCOOC/C=[O]/CC(C)(C)[C@@H](C(N(CC(C3)O)C3C(NCc(cc3)ccc3C3=C(C)NCS3)=O)=O)N)=O)CC2)cc(C(NCC2=C(C)C=C(C)NC2=O)=O)c1C=N Chemical compound CC(C)Nc1cc(/C(/C)=C/C=C(\N)/N2CCN(CCNC(COOCCOCCOOC/C=[O]/CC(C)(C)[C@@H](C(N(CC(C3)O)C3C(NCc(cc3)ccc3C3=C(C)NCS3)=O)=O)N)=O)CC2)cc(C(NCC2=C(C)C=C(C)NC2=O)=O)c1C=N GBZGMCCZDOBVMJ-PGWNOLSTSA-N 0.000 description 1
- FBXQUGOIWPRMSH-UHFFFAOYSA-N CC1=C(c2ccc(CN)cc2)SCN1 Chemical compound CC1=C(c2ccc(CN)cc2)SCN1 FBXQUGOIWPRMSH-UHFFFAOYSA-N 0.000 description 1
- AUFKVQVMVLSEAG-QYLXDIQESA-N CCN(CCNNC(COCCOCCOCCOCCC(N[C@@H](C(C)(C)C)C(N(CC(C1)O)[C@@H]1C(NCc(cc1)ccc1-c1c(C)nc[s]1)=O)=O)=O)=O)c(nc1)ccc1-c1cc(C(NCC2=C(C)C=C(C)NC2=O)=O)c(C=N)c(NC(C)C)c1 Chemical compound CCN(CCNNC(COCCOCCOCCOCCC(N[C@@H](C(C)(C)C)C(N(CC(C1)O)[C@@H]1C(NCc(cc1)ccc1-c1c(C)nc[s]1)=O)=O)=O)=O)c(nc1)ccc1-c1cc(C(NCC2=C(C)C=C(C)NC2=O)=O)c(C=N)c(NC(C)C)c1 AUFKVQVMVLSEAG-QYLXDIQESA-N 0.000 description 1
- PCZXZPOWHWJXDZ-UHFFFAOYSA-N Cc1c(-c2ccc(CN)cc2)[s]cn1 Chemical compound Cc1c(-c2ccc(CN)cc2)[s]cn1 PCZXZPOWHWJXDZ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2022201488A AU2022201488A1 (en) | 2016-10-28 | 2022-03-03 | Compositions and methods for treating EZH2-mediated cancer |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662414195P | 2016-10-28 | 2016-10-28 | |
| US62/414,195 | 2016-10-28 | ||
| PCT/US2017/058718 WO2018081530A1 (en) | 2016-10-28 | 2017-10-27 | Compositions and methods for treating ezh2-mediated cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2022201488A Division AU2022201488A1 (en) | 2016-10-28 | 2022-03-03 | Compositions and methods for treating EZH2-mediated cancer |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| AU2017348322A1 AU2017348322A1 (en) | 2019-06-13 |
| AU2017348322B2 AU2017348322B2 (en) | 2021-12-09 |
| AU2017348322B8 true AU2017348322B8 (en) | 2021-12-23 |
| AU2017348322A8 AU2017348322A8 (en) | 2021-12-23 |
Family
ID=62024052
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017348322A Ceased AU2017348322B8 (en) | 2016-10-28 | 2017-10-27 | Compositions and methods for treating EZH2-mediated cancer |
| AU2022201488A Abandoned AU2022201488A1 (en) | 2016-10-28 | 2022-03-03 | Compositions and methods for treating EZH2-mediated cancer |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2022201488A Abandoned AU2022201488A1 (en) | 2016-10-28 | 2022-03-03 | Compositions and methods for treating EZH2-mediated cancer |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US20190255041A1 (enExample) |
| EP (1) | EP3532464A4 (enExample) |
| JP (1) | JP2019537585A (enExample) |
| KR (1) | KR20190084063A (enExample) |
| CN (1) | CN110167924A (enExample) |
| AU (2) | AU2017348322B8 (enExample) |
| CA (1) | CA3041840A1 (enExample) |
| EA (1) | EA201991071A1 (enExample) |
| IL (1) | IL266053A (enExample) |
| MX (1) | MX2019004950A (enExample) |
| SG (2) | SG10202104386UA (enExample) |
| WO (1) | WO2018081530A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102667413B1 (ko) * | 2016-10-27 | 2024-05-21 | 삼성전자주식회사 | 음성 명령에 기초하여 애플리케이션을 실행하는 방법 및 장치 |
| MX2019004950A (es) | 2016-10-28 | 2019-09-26 | Icahn School Med Mount Sinai | Composiciones y metodos para tratar el cancer mediado por el potenciador del homologo zeste 2. |
| CA3045037A1 (en) | 2016-12-08 | 2018-06-14 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating cdk4/6-mediated cancer |
| US11191741B2 (en) * | 2016-12-24 | 2021-12-07 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide |
| JP2021515013A (ja) | 2018-03-06 | 2021-06-17 | アイカーン スクール オブ メディスン アット マウント シナイ | セリンスレオニンキナーゼ(akt)分解/破壊化合物および使用方法 |
| CN118344338A (zh) | 2018-04-23 | 2024-07-16 | 细胞基因公司 | 取代的4-氨基异吲哚啉-1,3-二酮化合物以及它们用于治疗淋巴瘤的用途 |
| JP2021527666A (ja) | 2018-06-21 | 2021-10-14 | アイカーン スクール オブ メディスン アット マウント シナイ | Wd40反復ドメインタンパク質5(wdr5)分解/破壊化合物および使用の方法 |
| WO2020010204A1 (en) | 2018-07-05 | 2020-01-09 | Icahn School Of Medicine At Mount Sinai | Protein tyrosine kinase 6 (ptk6) degradation / disruption compounds and methods of use |
| AU2019371400B2 (en) * | 2018-11-02 | 2024-10-17 | Dana-Farber Cancer Institute, Inc. | Acetylation writer inhibitor development and uses thereof |
| CN114423463B (zh) | 2019-05-06 | 2025-09-26 | 西奈山伊坎医学院 | 作为hpk1的降解剂的异双功能化合物 |
| CN112457365B (zh) | 2019-09-09 | 2023-06-09 | 中国医学科学院药物研究所 | 一类靶向蛋白质水解通路的功能分子及其制备和应用 |
| DK4034535T3 (da) | 2019-09-26 | 2026-04-07 | Novartis Ag | Aza-quinolinforbindelser og anvendelser deraf |
| CN110862434B (zh) * | 2019-10-28 | 2021-07-06 | 中山大学 | 一种可促进TGF-β1蛋白靶向降解的化合物及其制备方法与应用 |
| US12502434B2 (en) * | 2019-10-31 | 2025-12-23 | Daegu-Gyeongbuk Medical Innovation Foundation | Compound comprising EZH2 inhibitor and E3 ligase binder and pharmaceutical composition for preventing or treating EZH2-associated disease comprising same as active ingredient |
| CN111303133A (zh) * | 2020-03-25 | 2020-06-19 | 清华大学 | 降解ezh2蛋白的小分子化合物 |
| CN112920176B (zh) * | 2020-05-25 | 2022-11-04 | 四川大学华西医院 | 可诱导prc2蛋白复合物核心亚基降解的双功能化合物和药物组合物及应用 |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| KR102386403B1 (ko) * | 2020-08-13 | 2022-04-15 | 한미약품 주식회사 | 신규한 디옥솔로이소퀴놀린온 유도체 화합물 및 이의 용도 |
| CN113214203A (zh) * | 2020-12-16 | 2021-08-06 | 中山大学肿瘤防治中心(中山大学附属肿瘤医院、中山大学肿瘤研究所) | 基于ezh2蛋白降解的小分子化合物及其应用 |
| WO2022159650A1 (en) * | 2021-01-22 | 2022-07-28 | Icahn School Of Medicine At Mount Sinai | HETEROBIFUNCTIONAL COMPOUNDS AS DEGRADERS OF eEF1A2 |
| US12042543B2 (en) | 2021-04-30 | 2024-07-23 | Northwestern University | Substituted 3-amino-5-phenylbenzamide compounds as covalent inhibitors of enhancer zeste homolog 2 (EZH2) and proteolysis-targeting chimeric derivatives thereof (PROTACs) that induce degradation of EZH2 |
| EP4511128A1 (en) | 2022-04-20 | 2025-02-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| WO2024243441A1 (en) | 2023-05-24 | 2024-11-28 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| EP4735451A1 (en) | 2023-06-30 | 2026-05-06 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
| CN122228262A (zh) | 2023-11-02 | 2026-06-16 | 金橘生物科技公司 | 降解剂及其用途 |
| KR20250088371A (ko) * | 2023-12-08 | 2025-06-17 | 인제대학교 산학협력단 | Ezh2 저해제 및 jak3 억제제를 포함하는 암의 예방 또는 치료용 약학적 조성물 |
| WO2025121807A1 (ko) * | 2023-12-08 | 2025-06-12 | 인제대학교 산학협력단 | Ezh2 저해제 및 mettl3 억제제를 포함하는 암의 예방 또는 치료용 약제학적 조성물 |
| CN118420604A (zh) * | 2024-03-29 | 2024-08-02 | 中国药科大学 | 一种以降冰片烯为疏水基团修饰的ezh2蛋白降解剂及其制备方法和应用 |
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| WO2017011371A1 (en) * | 2015-07-10 | 2017-01-19 | Arvinas, Inc | Mdm2-based modulators of proteolysis and associated methods of use |
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| US5691147A (en) | 1994-06-02 | 1997-11-25 | Mitotix, Inc. | CDK4 binding assay |
| US6486214B1 (en) | 1997-09-10 | 2002-11-26 | Rutgers, The State University Of New Jersey | Polyanhydride linkers for production of drug polymers and drug polymer compositions produced thereby |
| HRP20020751B1 (hr) | 2000-02-15 | 2011-01-31 | Sugen | Pirolom supstituirani 2-indolinoni kao inhibitori protein kinaze |
| AU2004293026B2 (en) | 2003-11-21 | 2012-01-19 | Array Biopharma Inc. | AKT protein kinase inhibitors |
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| US11510920B2 (en) | 2022-11-29 |
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| US20190255041A1 (en) | 2019-08-22 |
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