CA3091027A1 - Small molecule drug conjugates of gemcitabine monophosphate - Google Patents
Small molecule drug conjugates of gemcitabine monophosphate Download PDFInfo
- Publication number
- CA3091027A1 CA3091027A1 CA3091027A CA3091027A CA3091027A1 CA 3091027 A1 CA3091027 A1 CA 3091027A1 CA 3091027 A CA3091027 A CA 3091027A CA 3091027 A CA3091027 A CA 3091027A CA 3091027 A1 CA3091027 A1 CA 3091027A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- int
- effector
- halo
- ester
- 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
-
- 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
- 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
- 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)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Genetics & Genomics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cell Biology (AREA)
- Food Science & Technology (AREA)
- Pathology (AREA)
- Physics & Mathematics (AREA)
- Microbiology (AREA)
- Analytical Chemistry (AREA)
- General Physics & Mathematics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Investigating Or Analysing Biological Materials (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862625820P | 2018-02-02 | 2018-02-02 | |
| US62/625,820 | 2018-02-02 | ||
| PCT/US2019/016557 WO2019152955A1 (en) | 2018-02-02 | 2019-02-04 | Small molecule drug conjugates of gemcitabine monophosphate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3091027A1 true CA3091027A1 (en) | 2019-08-08 |
Family
ID=65494554
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3091027A Pending CA3091027A1 (en) | 2018-02-02 | 2019-02-04 | Small molecule drug conjugates of gemcitabine monophosphate |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US11760773B2 (https=) |
| EP (1) | EP3746134A1 (https=) |
| JP (2) | JP2021512953A (https=) |
| KR (1) | KR20200118827A (https=) |
| CN (1) | CN112135634A (https=) |
| AU (1) | AU2019216531A1 (https=) |
| BR (1) | BR112020015745A2 (https=) |
| CA (1) | CA3091027A1 (https=) |
| CL (1) | CL2020002022A1 (https=) |
| CO (1) | CO2020010970A2 (https=) |
| EA (1) | EA202091856A1 (https=) |
| IL (1) | IL276436A (https=) |
| MX (1) | MX2020008188A (https=) |
| PE (1) | PE20210367A1 (https=) |
| PH (1) | PH12020551182A1 (https=) |
| SG (1) | SG11202007386RA (https=) |
| WO (1) | WO2019152955A1 (https=) |
Families Citing this family (1)
| 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 |
Family Cites Families (67)
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| SU389090A1 (ru) | 1971-05-17 | 1973-07-05 | Ташкентский государственный медицинский институт | Библиотека |
| US4526988A (en) | 1983-03-10 | 1985-07-02 | Eli Lilly And Company | Difluoro antivirals and intermediate therefor |
| US5229272A (en) | 1989-04-25 | 1993-07-20 | Igen, Inc. | Catalytic antibody components |
| ZA859008B (en) | 1984-12-04 | 1987-07-29 | Lilly Co Eli | The treatment of tumors in mammals |
| ATE92499T1 (de) | 1984-12-04 | 1993-08-15 | Lilly Co Eli | Tumorbehandlung bei saeugetieren. |
| DE3786834T2 (de) | 1986-04-30 | 1994-03-03 | Otsuka Pharma Co Ltd | 5-Fluoro-Uracil-Derivate. |
| US6702705B1 (en) | 1988-05-04 | 2004-03-09 | Igen International, Inc. | Prodrugs activated by targeted catalytic proteins |
| EP0418292A4 (en) | 1988-05-25 | 1991-09-25 | Research Corporation Technologies, Inc | Phosphoramides useful as antitumor agents |
| DE3834860A1 (de) | 1988-10-13 | 1990-04-19 | Basf Ag | Heterocyclisch substituierte alkoxycumarine, verfahren zu ihrer herstellung und diese enthaltende therapeutische mittel |
| DE3834861A1 (de) | 1988-10-13 | 1990-04-19 | Basf Ag | Arylalkoxycumarine, verfahren zu ihrer herstellung und diese enthaltende therapeutische mittel |
| US6258360B1 (en) | 1989-05-04 | 2001-07-10 | Igen International, Inc. | Prodrugs activated by targeted catalytic proteins |
| US6060592A (en) | 1990-01-11 | 2000-05-09 | Isis Pharmaceuticals, Inc. | Pyrimidine nucleoside compounds and oligonucleoside compounds containing same |
| US5401838A (en) | 1992-06-22 | 1995-03-28 | Eli Lilly And Company | Stereoselective fusion glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides |
| DK0702683T3 (da) | 1993-06-08 | 2004-02-02 | Cancer Rec Tech Ltd | 06-substituerede guaninderivater, fremgangsmåde til fremstilling deraf og anvendelse deraf i behandling af tumorceller |
| DK0795334T3 (da) | 1996-03-12 | 2006-06-06 | Sanofi Aventis Deutschland | Nye prodrugs til behandling af tumorer og betændelsessygdomme |
| WO1998011484A1 (fr) | 1996-09-13 | 1998-03-19 | Hitachi, Ltd. | Processeur de commande a memoire d'historique |
| ATE236188T1 (de) | 1997-01-24 | 2003-04-15 | Conpharma As | Gemcitabin-derivate |
| NZ330360A (en) | 1997-06-02 | 1999-03-29 | Hoffmann La Roche | 5'-deoxy-cytidine derivatives, their manufacture and use as antitumoral agents |
| TW434252B (en) | 1997-07-23 | 2001-05-16 | Univ Georgia Res Found | Process for the preparation of 2'-fluoro-5-methyl-β-L-arabino-furanosyluridine |
| EP1051383B1 (en) | 1998-02-06 | 2004-07-28 | De Montfort University | Hydroxylation activated prodrugs |
| AU2531599A (en) | 1998-02-12 | 1999-08-30 | De Montfort University | Hydroxylation activated drug release |
| DE19834751A1 (de) | 1998-08-01 | 2000-02-03 | Boehringer Ingelheim Pharma | Disubstituierte bicyclische Heterocyclen, ihre Herstellung und ihre Verwendung als Arzneimittel |
| US6175001B1 (en) | 1998-10-16 | 2001-01-16 | The Scripps Research Institute | Functionalized pyrimidine nucleosides and nucleotides and DNA's incorporating same |
| YU68102A (sh) | 2000-03-16 | 2006-01-16 | F. Hoffmann-La Roche Ag. | Derivati karboksilne kiseline kao ip antagonisti |
| GB0007401D0 (en) | 2000-03-27 | 2000-05-17 | Cancer Res Campaign Tech | Substituted chalcones as therapeeutic compounds |
| US6875751B2 (en) | 2000-06-15 | 2005-04-05 | Idenix Pharmaceuticals, Inc. | 3′-prodrugs of 2′-deoxy-β-L-nucleosides |
| US7115585B2 (en) | 2000-08-21 | 2006-10-03 | Inspire Pharmaceuticals, Inc. | Compositions for treating epithelial and retinal tissue diseases |
| JP3692927B2 (ja) | 2000-11-07 | 2005-09-07 | 日本電気株式会社 | ファクシミリ装置 |
| UA75622C2 (en) | 2000-12-08 | 2006-05-15 | 3M Innovative Properties Co | Aryl ether substituted imidazoquinolines, pharmaceutical composition based thereon |
| BR0207795A (pt) | 2001-03-02 | 2004-03-23 | Hoffmann La Roche | Derivados de ácido alcoxicarbonilamino benzóico ou alcoxicarbonilamino tetrazolil fenila como antagonistas de ip |
| CN1274948C (zh) | 2001-05-18 | 2006-09-13 | 赫斯工程股份有限公司 | 用于制造催化式排气净化器的方法和装置 |
| CA2459454A1 (en) | 2001-09-14 | 2003-03-27 | Bayer Pharmaceuticals Corporation | Benzofuran and dihydrobenzofuran derivatives useful as beta-3 adrenoreceptor agonists |
| EP1300403A1 (en) | 2001-10-02 | 2003-04-09 | Aventis Pharma S.A. | Process for the manufacture of hypoxyxylerone derivatives |
| GB0123777D0 (en) | 2001-10-03 | 2001-11-21 | Cancer Res Ventures Ltd | Substituted chalcones as therapeutic agents |
| GB0123780D0 (en) | 2001-10-03 | 2001-11-21 | Cancer Res Ventures Ltd | Substituted chalcones as therapeutic agents |
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| EA012844B1 (ru) | 2003-02-19 | 2009-12-30 | Йельский Университет | Аналоги противовирусных нуклеозидов и способы лечения вирусных инфекций, в частности вич-инфекций |
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| WO2005061459A1 (en) | 2003-12-04 | 2005-07-07 | Wyeth | Biaryl sulfonamides and methods for using same |
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| GB0421294D0 (en) | 2004-09-24 | 2004-10-27 | Angiogene Pharm Ltd | Bioreductively-activated prodrugs |
| KR100874052B1 (ko) | 2004-12-17 | 2008-12-12 | 일라이 릴리 앤드 캄파니 | 젬시타빈의 아미드 전구약, 그의 조성물 및 그의 용도 |
| EP1676834A1 (en) | 2004-12-30 | 2006-07-05 | Sanofi-Aventis Deutschland GmbH | Fused bicyclic carboxamide derivates for use as CXCR2 inhibitors in the treatment of inflammation |
| NO322682B1 (no) | 2005-03-18 | 2006-11-27 | Clavis Pharma Asa | Anvendelse av gemcitabinderivater for fremstilling av orale doseringsformer ved kreftbehandling, samt slike orale doseringsformer |
| CA2624726A1 (en) | 2005-10-06 | 2007-04-12 | Sanofi-Aventis | 4-oxy-n-[1 ,3,4]-thiadiazol-2-yl-benzene sulfonamides, processes for their preparation and their use as pharmaceuticals |
| WO2007117760A2 (en) | 2006-02-06 | 2007-10-18 | Dr. Reddy's Laboratories Ltd. | Preparation of gemcitabine |
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| US20070225248A1 (en) | 2006-03-21 | 2007-09-27 | Clavis Pharma As | Oral dosage forms of gemcitabine derivatives |
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| EP2136626A4 (en) | 2007-03-19 | 2011-02-23 | Oregon State | Mannich base n-oxide drugs |
| CN100475832C (zh) | 2007-05-31 | 2009-04-08 | 南京卡文迪许生物工程技术有限公司 | 一种新颖的高立体选择性合成吉西他滨工艺及中间体 |
| JO2778B1 (en) | 2007-10-16 | 2014-03-15 | ايساي انك | Certain Compounds, Compositions and Methods |
| TWI415858B (zh) | 2007-11-06 | 2013-11-21 | Pharmaessentia Corp | β－核苷之新穎合成技術 |
| GB0907551D0 (en) | 2009-05-01 | 2009-06-10 | Univ Dundee | Treatment or prophylaxis of proliferative conditions |
| US9937128B2 (en) * | 2009-08-03 | 2018-04-10 | The University Of North Carolina At Chapel Hill | Liposomes comprising a calcium phosphate-containing precipitate |
| US20130131008A1 (en) * | 2011-10-25 | 2013-05-23 | Board Of Regents, The University Of Texas System | Lipophilic monophosphorylated derivatives and nanoparticles |
| CN104955458A (zh) | 2012-11-07 | 2015-09-30 | Z·索 | 取代的吉西他滨芳基酰胺类似物和使用所述类似物的治疗方法 |
| US10000521B2 (en) * | 2013-03-15 | 2018-06-19 | Nucorion Pharmaceuticals, Inc. | Substituted gemcitabine bicyclic amide analogs and treatment methods using same |
| 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 |
| CN105001191A (zh) * | 2015-07-23 | 2015-10-28 | 广西师范学院 | 具有5,2’-二羟基-4’-甲氧基-3-香叶基黄酮骨架的衍生物及其制备方法和用途 |
| US20210380626A1 (en) * | 2018-02-02 | 2021-12-09 | Maverix Oncology, Inc. | Novel small molecule drug conjugates of gemcitabine derivatives |
| PE20210367A1 (es) * | 2018-02-02 | 2021-02-26 | Maverix Oncology Inc | Conjugados de farmacos de molecula pequena de monofosfato de gemcitabina |
-
2019
- 2019-02-04 PE PE2020001173A patent/PE20210367A1/es unknown
- 2019-02-04 MX MX2020008188A patent/MX2020008188A/es unknown
- 2019-02-04 AU AU2019216531A patent/AU2019216531A1/en not_active Abandoned
- 2019-02-04 BR BR112020015745-7A patent/BR112020015745A2/pt not_active IP Right Cessation
- 2019-02-04 SG SG11202007386RA patent/SG11202007386RA/en unknown
- 2019-02-04 JP JP2020564037A patent/JP2021512953A/ja active Pending
- 2019-02-04 CN CN201980024079.2A patent/CN112135634A/zh active Pending
- 2019-02-04 EA EA202091856A patent/EA202091856A1/ru unknown
- 2019-02-04 KR KR1020207025176A patent/KR20200118827A/ko not_active Ceased
- 2019-02-04 WO PCT/US2019/016557 patent/WO2019152955A1/en not_active Ceased
- 2019-02-04 CA CA3091027A patent/CA3091027A1/en active Pending
- 2019-02-04 US US16/967,049 patent/US11760773B2/en active Active
- 2019-02-04 EP EP19706114.6A patent/EP3746134A1/en not_active Withdrawn
-
2020
- 2020-08-02 IL IL276436A patent/IL276436A/en unknown
- 2020-08-03 CL CL2020002022A patent/CL2020002022A1/es unknown
- 2020-08-04 PH PH12020551182A patent/PH12020551182A1/en unknown
- 2020-09-01 CO CONC2020/0010970A patent/CO2020010970A2/es unknown
-
2024
- 2024-01-22 JP JP2024007282A patent/JP2024054873A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| KR20200118827A (ko) | 2020-10-16 |
| PH12020551182A1 (en) | 2021-05-10 |
| US11760773B2 (en) | 2023-09-19 |
| CN112135634A (zh) | 2020-12-25 |
| MX2020008188A (es) | 2020-11-18 |
| US20210040136A1 (en) | 2021-02-11 |
| IL276436A (en) | 2020-09-30 |
| SG11202007386RA (en) | 2020-08-28 |
| WO2019152955A9 (en) | 2020-08-13 |
| EA202091856A1 (ru) | 2020-12-07 |
| BR112020015745A2 (pt) | 2020-12-08 |
| AU2019216531A1 (en) | 2020-09-24 |
| PE20210367A1 (es) | 2021-02-26 |
| CO2020010970A2 (es) | 2020-11-20 |
| JP2024054873A (ja) | 2024-04-17 |
| WO2019152955A1 (en) | 2019-08-08 |
| EP3746134A1 (en) | 2020-12-09 |
| CL2020002022A1 (es) | 2021-02-12 |
| JP2021512953A (ja) | 2021-05-20 |
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