CA3090272A1 - Novel small molecule drug conjugates of gemcitabine derivatives - Google Patents
Novel small molecule drug conjugates of gemcitabine derivatives Download PDFInfo
- Publication number
- CA3090272A1 CA3090272A1 CA3090272A CA3090272A CA3090272A1 CA 3090272 A1 CA3090272 A1 CA 3090272A1 CA 3090272 A CA3090272 A CA 3090272A CA 3090272 A CA3090272 A CA 3090272A CA 3090272 A1 CA3090272 A1 CA 3090272A1
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- effector
- compound
- halo
- int
- 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.)
- Pending
Links
Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
- A61K49/0004—Screening or testing of compounds for diagnosis of disorders, assessment of conditions, e.g. renal clearance, gastric emptying, testing for diabetes, allergy, rheuma, pancreas functions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
- G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
- G01N33/5758—Immunoassay; Biospecific binding assay; Materials therefor for cancer involving compounds serving as markers for tumours, cancers or neoplasias, e.g. cellular determinants, receptors, heat shock/stress proteins, A-protein, oligosaccharides or metabolites
-
- 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
- G01N2333/90—Enzymes; Proenzymes
- G01N2333/902—Oxidoreductases (1.)
- G01N2333/90245—Oxidoreductases (1.) acting on paired donors with incorporation of molecular oxygen (1.14)
-
- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2440/00—Post-translational modifications [PTMs] in chemical analysis of biological material
- G01N2440/24—Post-translational modifications [PTMs] in chemical analysis of biological material hydroxylation
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Genetics & Genomics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pathology (AREA)
- Hematology (AREA)
- Toxicology (AREA)
- Rheumatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Endocrinology (AREA)
- Cell Biology (AREA)
- Diabetes (AREA)
- Microbiology (AREA)
- Food Science & Technology (AREA)
- Physics & Mathematics (AREA)
- Analytical Chemistry (AREA)
- General Physics & Mathematics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicinal Preparation (AREA)
- Investigating Or Analysing Biological Materials (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862625779P | 2018-02-02 | 2018-02-02 | |
| US62/625,779 | 2018-02-02 | ||
| PCT/US2019/016477 WO2019152911A1 (en) | 2018-02-02 | 2019-02-04 | Novel small molecule drug conjugates of gemcitabine derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3090272A1 true CA3090272A1 (en) | 2019-08-08 |
Family
ID=65494546
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3090272A Pending CA3090272A1 (en) | 2018-02-02 | 2019-02-04 | Novel small molecule drug conjugates of gemcitabine derivatives |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20210380626A1 (https=) |
| EP (1) | EP3746133A1 (https=) |
| JP (2) | JP2021512951A (https=) |
| KR (1) | KR20200118828A (https=) |
| CN (1) | CN112135635A (https=) |
| AU (1) | AU2019216514A1 (https=) |
| BR (1) | BR112020015747A2 (https=) |
| CA (1) | CA3090272A1 (https=) |
| EA (1) | EA202091857A1 (https=) |
| IL (1) | IL276442A (https=) |
| PH (1) | PH12020551178A1 (https=) |
| SG (1) | SG11202007381YA (https=) |
| WO (1) | WO2019152911A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20210367A1 (es) * | 2018-02-02 | 2021-02-26 | Maverix Oncology Inc | Conjugados de farmacos de molecula pequena de monofosfato de gemcitabina |
| CN114349816B (zh) * | 2021-11-30 | 2024-08-30 | 潍坊博创国际生物医药研究院 | 一种基于氨肽酶n/cd13的小分子偶联分子及其制备方法和应用 |
| WO2026009986A1 (ja) * | 2024-07-05 | 2026-01-08 | 学校法人東京理科大学 | 化合物の製造方法及び化合物 |
| WO2026009987A1 (ja) * | 2024-07-05 | 2026-01-08 | 学校法人東京理科大学 | 化合物の製造方法、化合物、及びヌクレオチドプロドラッグ前駆体 |
| CN119708099B (zh) * | 2024-12-23 | 2025-10-24 | 中国药科大学 | 吉西他滨前药及其医药用途 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2531599A (en) | 1998-02-12 | 1999-08-30 | De Montfort University | Hydroxylation activated drug release |
| US7148226B2 (en) | 2003-02-21 | 2006-12-12 | Agouron Pharmaceuticals, Inc. | Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same |
| GB0317009D0 (en) * | 2003-07-21 | 2003-08-27 | Univ Cardiff | Chemical compounds |
| GB0907551D0 (en) * | 2009-05-01 | 2009-06-10 | Univ Dundee | Treatment or prophylaxis of proliferative conditions |
| JP6212831B2 (ja) * | 2013-12-04 | 2017-10-18 | 杭州源昶医薬科技有限公司 | ゲムシタビン誘導体、該誘導体を含む組成物及び該誘導体の製薬用途 |
| WO2015134334A1 (en) * | 2014-03-03 | 2015-09-11 | Suo Zucai | Gemcitabine analogs |
| CN105001291B (zh) * | 2014-04-15 | 2018-12-04 | 上海知萌生物医药科技有限公司 | 吉西他滨化学传递前药及其制备方法和应用 |
| US20180044368A1 (en) * | 2015-02-25 | 2018-02-15 | Ligand Pharmaceuticals, Inc. | Gemcitabine derivatives |
-
2019
- 2019-02-04 US US16/967,086 patent/US20210380626A1/en not_active Abandoned
- 2019-02-04 KR KR1020207025177A patent/KR20200118828A/ko not_active Ceased
- 2019-02-04 SG SG11202007381YA patent/SG11202007381YA/en unknown
- 2019-02-04 EA EA202091857A patent/EA202091857A1/ru unknown
- 2019-02-04 EP EP19706106.2A patent/EP3746133A1/en not_active Withdrawn
- 2019-02-04 CN CN201980024089.6A patent/CN112135635A/zh active Pending
- 2019-02-04 AU AU2019216514A patent/AU2019216514A1/en not_active Abandoned
- 2019-02-04 WO PCT/US2019/016477 patent/WO2019152911A1/en not_active Ceased
- 2019-02-04 BR BR112020015747-3A patent/BR112020015747A2/pt not_active IP Right Cessation
- 2019-02-04 CA CA3090272A patent/CA3090272A1/en active Pending
- 2019-02-04 JP JP2020564033A patent/JP2021512951A/ja active Pending
-
2020
- 2020-08-02 IL IL276442A patent/IL276442A/en unknown
- 2020-08-03 PH PH12020551178A patent/PH12020551178A1/en unknown
-
2024
- 2024-02-13 JP JP2024019158A patent/JP2024073414A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| KR20200118828A (ko) | 2020-10-16 |
| US20210380626A1 (en) | 2021-12-09 |
| SG11202007381YA (en) | 2020-08-28 |
| EP3746133A1 (en) | 2020-12-09 |
| EA202091857A1 (ru) | 2020-12-04 |
| PH12020551178A1 (en) | 2021-06-07 |
| AU2019216514A1 (en) | 2020-09-24 |
| JP2024073414A (ja) | 2024-05-29 |
| JP2021512951A (ja) | 2021-05-20 |
| BR112020015747A2 (pt) | 2020-12-08 |
| IL276442A (en) | 2020-09-30 |
| CN112135635A (zh) | 2020-12-25 |
| WO2019152911A1 (en) | 2019-08-08 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA3090272A1 (en) | Novel small molecule drug conjugates of gemcitabine derivatives | |
| EP3816163A1 (en) | Cell necrosis inhibitor, preparation method therefor and use thereof | |
| EP2419430A2 (en) | Novel compounds of reverse-turn mimetics, method for manufacturing the same and use thereof | |
| AU2005306458A1 (en) | Kinase inhibitors | |
| US20090075945A1 (en) | Phosphate-bearing prodrugs of sulfonyl hydrazines as hypoxia-selective antineoplastic agents | |
| US9481678B2 (en) | Substituted pyrrolo[2,3-D]dipyrimidines for selectively targeting tumor cells with FR-alpha and FR-beta type receptors | |
| CN104292125B (zh) | 萘衍生物及其在药物上的应用 | |
| TW202116734A (zh) | 乙醯輔酶a合成酶短鏈2(acss2)之小分子抑制劑 | |
| EP4273150A1 (en) | Tricyclic compound, and preparation method therefor and medical use thereof | |
| CN113896721B (zh) | 具有肿瘤靶向的烟酰胺磷酸核糖转移酶抑制剂 | |
| JP2024054873A (ja) | ゲムシタビンモノホスフェートの小分子薬物コンジュゲート | |
| CN104230742A (zh) | 萘衍生物及其在药物上的应用 | |
| CN107141287B (zh) | 2-亚胺-5-酮基-2,5-二氢-1-h-二吡啶并嘧啶类化合物 | |
| US9175001B2 (en) | [1,3] dioxolo [4,5-g] [1,2,4] triazolo [1,5-a] quinoline derivatives as inhibitors of the late SV40 factor (LSF) for use in treating cancer | |
| KR20080008407A (ko) | 항신생물의 화합물 및 이를 포함하는 약학적 조성물 | |
| CN109206435B (zh) | 噻吩并[3,2-d]嘧啶类化合物及其制备方法和医药用途 | |
| CN115141169A (zh) | 一种萜内酯衍生物及其在医药上的应用 | |
| KR100983318B1 (ko) | 메조-비스(오쏘-하이드록시페닐)비스(오쏘-하이드록시)살렌의 항암제로서의 용도 | |
| CA3209234A1 (en) | Heteroaromatic phosphonium salts and their use treating cancer | |
| WO2022115753A1 (en) | Merged scaffold taf1 inhibitors | |
| CN104292126A (zh) | 萘衍生物及其在药物上的应用 | |
| CN101022798A (zh) | 作为低氧选择性抗肿瘤剂的磺酰肼类 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20240202 |
|
| D15 | Examination report completed |
Free format text: ST27 STATUS EVENT CODE: A-2-2-D10-D15-D126 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: EXAMINER'S REPORT Effective date: 20250207 |
|
| P11 | Amendment of application requested |
Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - RESPONSE TO EXAMINER'S REQUISITION Effective date: 20250606 |
|
| W00 | Other event occurred |
Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT Effective date: 20250609 |
|
| P11 | Amendment of application requested |
Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT Effective date: 20250724 |
|
| P13 | Application amended |
Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED Effective date: 20250724 |
|
| MFA | Maintenance fee for application paid |
Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 6TH ANNIV.) - STANDARD Year of fee payment: 6 |
|
| U00 | Fee paid |
Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED Effective date: 20250725 |
|
| U11 | Full renewal or maintenance fee paid |
Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL Effective date: 20250725 |
|
| W00 | Other event occurred |
Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT Effective date: 20251127 |
|
| W00 | Other event occurred |
Free format text: ST27 STATUS EVENT CODE: A-2-2-W10-W00-W100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: LETTER SENT Effective date: 20260318 |