CN115066235A - 包含泛素特异性加工蛋白酶1(usp1)抑制剂和多聚(adp-核糖)聚合酶(parp)抑制剂的治疗组合 - Google Patents
包含泛素特异性加工蛋白酶1(usp1)抑制剂和多聚(adp-核糖)聚合酶(parp)抑制剂的治疗组合 Download PDFInfo
- Publication number
- CN115066235A CN115066235A CN202180013564.7A CN202180013564A CN115066235A CN 115066235 A CN115066235 A CN 115066235A CN 202180013564 A CN202180013564 A CN 202180013564A CN 115066235 A CN115066235 A CN 115066235A
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- China
- Prior art keywords
- cancer
- inhibitor
- usp1
- parp
- pharmaceutically acceptable
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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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- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- 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
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
- G01N2333/46—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans from vertebrates
- G01N2333/47—Assays involving proteins of known structure or function as defined in the subgroups
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2800/00—Detection or diagnosis of diseases
- G01N2800/52—Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Enzymes And Modification Thereof (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062976864P | 2020-02-14 | 2020-02-14 | |
| US62/976,864 | 2020-02-14 | ||
| US202063032245P | 2020-05-29 | 2020-05-29 | |
| US63/032,245 | 2020-05-29 | ||
| US202163146937P | 2021-02-08 | 2021-02-08 | |
| US63/146,937 | 2021-02-08 | ||
| PCT/US2021/017912 WO2021163530A1 (en) | 2020-02-14 | 2021-02-12 | Therapeutic combinations comprising ubiquitin-specific-processing protease 1 (usp1) inhibitors and poly (adp-ribose) polymerase (parp) inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN115066235A true CN115066235A (zh) | 2022-09-16 |
Family
ID=77291879
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202180013564.7A Pending CN115066235A (zh) | 2020-02-14 | 2021-02-12 | 包含泛素特异性加工蛋白酶1(usp1)抑制剂和多聚(adp-核糖)聚合酶(parp)抑制剂的治疗组合 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20230277533A1 (enExample) |
| EP (1) | EP4103165A4 (enExample) |
| JP (1) | JP2023514568A (enExample) |
| KR (1) | KR20220140732A (enExample) |
| CN (1) | CN115066235A (enExample) |
| AU (1) | AU2021218805A1 (enExample) |
| CA (1) | CA3168009A1 (enExample) |
| IL (1) | IL295149A (enExample) |
| MX (1) | MX2022009818A (enExample) |
| TW (1) | TW202140026A (enExample) |
| WO (1) | WO2021163530A1 (enExample) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN117384187A (zh) * | 2022-09-30 | 2024-01-12 | 轩竹生物科技股份有限公司 | 泛素特异性蛋白酶1抑制剂 |
| WO2025087460A1 (zh) * | 2023-10-25 | 2025-05-01 | 海思科医药集团股份有限公司 | 一种吡啶并吡唑衍生物药物组合物及其应用 |
| WO2025153067A1 (zh) * | 2024-01-19 | 2025-07-24 | 江苏亚虹医药科技股份有限公司 | Usp1抑制剂及其医药用途 |
| WO2025180502A1 (zh) * | 2024-03-01 | 2025-09-04 | 上海齐鲁制药研究中心有限公司 | 一种联合用药物组合物及其用途 |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023514568A (ja) * | 2020-02-14 | 2023-04-06 | ケーエスキュー セラピューティクス, インコーポレイテッド | ユビキチン特異的プロセシングプロテアーゼ1(usp1)阻害剤及びポリ(adpリボース)ポリメラーゼ(parp)阻害剤を含む治療効果のある組み合わせ |
| EP4236958A4 (en) | 2020-10-30 | 2024-09-11 | KSQ Therapeutics, Inc. | SOLID STATE FORMS OF SUBSTITUTED PYRAZOLOPYRIMIDINES AND THEIR USES |
| JP2024540921A (ja) * | 2021-10-19 | 2024-11-06 | 上海瑛派▲薬▼▲業▼有限公司 | Usp1阻害剤としての置換トリアゾロヘテロアリール化合物及びその応用 |
| KR20240117556A (ko) * | 2021-11-12 | 2024-08-01 | 인실리코 메디신 아이피 리미티드 | 유비퀴틴 특이적 프로테아제 1(usp1)의 소분자 억제제 및 이의 용도 |
| CR20240190A (es) * | 2021-11-12 | 2024-09-13 | Insilico Medicine Ip Ltd | Inhibidores de moléculas pequeñas de la proteasa específica de ubiquitina 1 (usp1) y sus usos |
| JP2025503139A (ja) * | 2022-01-25 | 2025-01-30 | ケーエスキュー セラピューティクス, インコーポレイテッド | 固形腫瘍の治療のためのユビキチン特異的プロセシングプロテアーゼ1(usp1)阻害剤 |
| JP2025531133A (ja) * | 2022-09-20 | 2025-09-19 | チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッド | ユビキチン特異的プロテアーゼ阻害剤としてのカルボニル縮合複素環誘導体 |
| AU2023347293A1 (en) * | 2022-09-23 | 2025-04-10 | KSQ Therapeutics, Inc. | Therapeutic combinations comprising ubiquitin-specific-processing protease 1 (usp1) inhibitors and parp1-selective inhibitors |
| EP4605391A1 (en) | 2022-10-21 | 2025-08-27 | Exelixis, Inc. | 4,5,6,7-tetrahydro-1-pyrazolo[4,3-c]pyridine compounds and derivatives as usp1 inhibitors |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| TW202509030A (zh) | 2023-05-08 | 2025-03-01 | 美商譚格醫療公司 | 化合物及使用方法 |
| WO2024233665A1 (en) | 2023-05-08 | 2024-11-14 | Tango Therapeutics, Inc. | Compounds and their use against cancer |
| JP2026521192A (ja) * | 2023-06-16 | 2026-06-26 | コリア・インスティテュート・オブ・サイエンス・アンド・テクノロジー | BRCA特異的siRNAを有効成分として含む標的癌予防又は治療用医薬組成物 |
| EP4739397A1 (en) | 2023-07-06 | 2026-05-13 | Exelixis, Inc. | Fused pyrazole derivatives as usp1 inhibitors |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AU2024378865A1 (en) | 2023-11-10 | 2026-06-25 | Vrise Therapeutics, Inc. | Novel molecules as inhibitors of dna damage repair pathway |
| WO2025151705A1 (en) | 2024-01-10 | 2025-07-17 | Vrise Therapeutics, Inc. | Novel inhibitors of dna damage repair pathway |
| 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 |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (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 |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| 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 |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | Revolution Medicines, Inc. | Ras inhibitors |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20130253005A1 (en) * | 2010-04-30 | 2013-09-26 | The Brigham And Women's Hospital, Inc. | Small molecule inhibitors of usp1 deubiquitinating enzyme activity |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201519573D0 (en) * | 2015-11-05 | 2015-12-23 | King S College London | Combination |
| WO2018165615A1 (en) * | 2017-03-09 | 2018-09-13 | The Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College | Parp-1 and methods of use thereof |
| EP3606523A1 (en) * | 2017-03-27 | 2020-02-12 | Tesaro, Inc. | Niraparib formulations |
| WO2020132269A1 (en) * | 2018-12-20 | 2020-06-25 | KSQ Therapeutics, Inc. | Substituted pyrazolopyrimidines and substituted purines and their use as ubiquitin-specific-processing protease 1 (usp1) inhibitors |
| ES3025474T3 (en) * | 2020-01-15 | 2025-06-09 | Ksq Therapeutics Inc | Compositions of substituted pyrazolopyrimidines and uses thereof |
| JP2023514568A (ja) * | 2020-02-14 | 2023-04-06 | ケーエスキュー セラピューティクス, インコーポレイテッド | ユビキチン特異的プロセシングプロテアーゼ1(usp1)阻害剤及びポリ(adpリボース)ポリメラーゼ(parp)阻害剤を含む治療効果のある組み合わせ |
| EP4236958A4 (en) * | 2020-10-30 | 2024-09-11 | KSQ Therapeutics, Inc. | SOLID STATE FORMS OF SUBSTITUTED PYRAZOLOPYRIMIDINES AND THEIR USES |
-
2021
- 2021-02-12 JP JP2022548896A patent/JP2023514568A/ja active Pending
- 2021-02-12 AU AU2021218805A patent/AU2021218805A1/en active Pending
- 2021-02-12 CA CA3168009A patent/CA3168009A1/en active Pending
- 2021-02-12 KR KR1020227027461A patent/KR20220140732A/ko not_active Ceased
- 2021-02-12 IL IL295149A patent/IL295149A/en unknown
- 2021-02-12 EP EP21754160.6A patent/EP4103165A4/en not_active Withdrawn
- 2021-02-12 US US17/904,159 patent/US20230277533A1/en not_active Abandoned
- 2021-02-12 MX MX2022009818A patent/MX2022009818A/es unknown
- 2021-02-12 WO PCT/US2021/017912 patent/WO2021163530A1/en not_active Ceased
- 2021-02-12 CN CN202180013564.7A patent/CN115066235A/zh active Pending
- 2021-02-17 TW TW110105371A patent/TW202140026A/zh unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20130253005A1 (en) * | 2010-04-30 | 2013-09-26 | The Brigham And Women's Hospital, Inc. | Small molecule inhibitors of usp1 deubiquitinating enzyme activity |
Non-Patent Citations (2)
| Title |
|---|
| 李华明;罗彦英;史颖萍;辛芝;张艳萍;: "特异性泛素蛋白酶―22生物学功能研究现状", 中国中西医结合外科杂志, no. 03 * |
| 蒋智文;刘新光;周中军;: "组蛋白修饰调节机制的研究进展", 生物化学与生物物理进展, no. 10 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN117384187A (zh) * | 2022-09-30 | 2024-01-12 | 轩竹生物科技股份有限公司 | 泛素特异性蛋白酶1抑制剂 |
| WO2025087460A1 (zh) * | 2023-10-25 | 2025-05-01 | 海思科医药集团股份有限公司 | 一种吡啶并吡唑衍生物药物组合物及其应用 |
| WO2025153067A1 (zh) * | 2024-01-19 | 2025-07-24 | 江苏亚虹医药科技股份有限公司 | Usp1抑制剂及其医药用途 |
| WO2025180502A1 (zh) * | 2024-03-01 | 2025-09-04 | 上海齐鲁制药研究中心有限公司 | 一种联合用药物组合物及其用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| TW202140026A (zh) | 2021-11-01 |
| WO2021163530A1 (en) | 2021-08-19 |
| KR20220140732A (ko) | 2022-10-18 |
| CA3168009A1 (en) | 2021-08-19 |
| US20230277533A1 (en) | 2023-09-07 |
| EP4103165A4 (en) | 2024-02-28 |
| EP4103165A1 (en) | 2022-12-21 |
| JP2023514568A (ja) | 2023-04-06 |
| AU2021218805A1 (en) | 2022-09-01 |
| MX2022009818A (es) | 2022-09-05 |
| IL295149A (en) | 2022-09-01 |
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