MX368016B - Derivados de uncialamicina, métodos de sintesis y su uso como agentes antitumor. - Google Patents
Derivados de uncialamicina, métodos de sintesis y su uso como agentes antitumor.Info
- Publication number
- MX368016B MX368016B MX2016001975A MX2016001975A MX368016B MX 368016 B MX368016 B MX 368016B MX 2016001975 A MX2016001975 A MX 2016001975A MX 2016001975 A MX2016001975 A MX 2016001975A MX 368016 B MX368016 B MX 368016B
- Authority
- MX
- Mexico
- Prior art keywords
- uncialamycin
- present disclosure
- methods
- synthesis
- derivatives
- Prior art date
Links
- OBGWIHKWGGEOEV-WJPOXRCESA-N (1S,17S,20Z,24R,26R)-4,24-dihydroxy-26-[(1R)-1-hydroxyethyl]-25-oxa-16-azahexacyclo[15.7.2.01,26.02,15.05,14.07,12]hexacosa-2,4,7,9,11,14,20-heptaen-18,22-diyne-6,13-dione Chemical class O[C@@H]1C#C\C=C/C#C[C@@H]2NC(C=3C(=O)C4=CC=CC=C4C(=O)C=3C(O)=C3)=C3[C@@]31O[C@]32[C@H](O)C OBGWIHKWGGEOEV-WJPOXRCESA-N 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 2
- 239000002246 antineoplastic agent Substances 0.000 title 1
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- OBGWIHKWGGEOEV-UHFFFAOYSA-N uncialamycin Natural products OC1C#CC=CC#CC2NC(C=3C(=O)C4=CC=CC=C4C(=O)C=3C(O)=C3)=C3C31OC32C(O)C OBGWIHKWGGEOEV-UHFFFAOYSA-N 0.000 abstract 3
- 239000000611 antibody drug conjugate Substances 0.000 abstract 1
- 229940049595 antibody-drug conjugate Drugs 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000037361 pathway Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged 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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4355—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
-
- 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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
- A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
-
- 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
- A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
- A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6851—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0021—Intradermal administration, e.g. through microneedle arrays, needleless injectors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/18—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cell Biology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
En un aspecto, la presente descripción proporciona nuevos análogos de uncialamicina de las fórmulas (I) y (II): (ver Fórmulas) La presente descripción también proporciona novedosas sendas sintéticas para obtener uncialamicina y análogos de la misma. Adicionalmente, la presente descripción también describe métodos para usar la uncialamicina y los análogos de la misma. En otro aspecto, la presente descripción proporciona conjugados de anticuerpo-fármaco que comprenden los compuestos de las fórmulas (I) y (II).
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361865896P | 2013-08-14 | 2013-08-14 | |
| US201361868783P | 2013-08-22 | 2013-08-22 | |
| US201461937003P | 2014-02-07 | 2014-02-07 | |
| PCT/US2014/051127 WO2015023879A1 (en) | 2013-08-14 | 2014-08-14 | Derivatives of uncialamycin, methods of synthesis and their use as antitumor agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2016001975A MX2016001975A (es) | 2016-11-14 |
| MX368016B true MX368016B (es) | 2019-09-13 |
Family
ID=51453866
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2016001975A MX368016B (es) | 2013-08-14 | 2014-08-14 | Derivados de uncialamicina, métodos de sintesis y su uso como agentes antitumor. |
| MX2019010875A MX2019010875A (es) | 2013-08-14 | 2016-02-12 | Derivados de uncialamicina, metodos de sintesis y su uso como agentes antitumor. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2019010875A MX2019010875A (es) | 2013-08-14 | 2016-02-12 | Derivados de uncialamicina, metodos de sintesis y su uso como agentes antitumor. |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US9777013B2 (es) |
| EP (1) | EP3033346B1 (es) |
| JP (2) | JP6474404B2 (es) |
| KR (1) | KR20160068738A (es) |
| CN (1) | CN105899515B (es) |
| AU (2) | AU2014306592B2 (es) |
| CA (1) | CA2921401A1 (es) |
| EA (1) | EA201690388A1 (es) |
| ES (1) | ES2769876T3 (es) |
| IL (1) | IL244084B (es) |
| MX (2) | MX368016B (es) |
| SG (2) | SG11201601047SA (es) |
| WO (1) | WO2015023879A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX368016B (es) * | 2013-08-14 | 2019-09-13 | Univ Rice William M | Derivados de uncialamicina, métodos de sintesis y su uso como agentes antitumor. |
| CN105764491A (zh) | 2013-12-09 | 2016-07-13 | 度瑞公司 | 药物活性剂复合物、聚合物复合物,以及包括其的组合物和方法 |
| EP3353198B1 (en) * | 2015-09-23 | 2020-06-17 | Bristol-Myers Squibb Company | Glypican-3binding fibronectin based scafflold molecules |
| KR20180089433A (ko) | 2015-12-21 | 2018-08-08 | 브리스톨-마이어스 스큅 컴퍼니 | 부위-특이적 접합을 위한 변이체 항체 |
| US20190218294A1 (en) | 2016-09-09 | 2019-07-18 | Bristol-Myers Squibb Company | Use of an anti-pd-1 antibody in combination with an anti-mesothelin antibody in cancer treatment |
| US10738338B2 (en) | 2016-10-18 | 2020-08-11 | The Research Foundation for the State University | Method and composition for biocatalytic protein-oligonucleotide conjugation and protein-oligonucleotide conjugate |
| SG11202011739SA (en) | 2018-05-29 | 2020-12-30 | Bristol Myers Squibb Co | Modified self-immolating moieties for use in prodrugs and conjugates and methods of using and making |
| RS64205B1 (sr) | 2018-11-30 | 2023-06-30 | Bristol Myers Squibb Co | Antitelo koje sadrži c-terminalnu ekstenziju lakog lanca koja sadrži glutamin, njegovi konjugati, i postupci i primene |
| JP7514836B2 (ja) | 2018-12-12 | 2024-07-11 | ブリストル-マイヤーズ スクイブ カンパニー | トランスグルタミナーゼによるコンジュゲーションのための改変抗体、ならびにそのコンジュゲート、方法および用途 |
| CN109928981B (zh) * | 2019-04-19 | 2021-06-11 | 长沙天赐生物医药科技有限公司 | 洋浦霉素类似物、制备方法及其应用 |
| US20240377413A1 (en) | 2019-09-16 | 2024-11-14 | Bristol-Myers Squibb Company | Dual capture method for analysis of antibody-drug conjugates |
| US11027253B2 (en) | 2019-09-26 | 2021-06-08 | Chevron Phillips Chemical Company Lp | Systems and methods for reducing heat exchanger fouling rate |
| CN116813627B (zh) * | 2023-06-15 | 2025-08-12 | 哈药慈航制药股份有限公司 | 一种天赐霉素类似物及其制备方法和应用 |
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| MX368016B (es) | 2013-08-14 | 2019-09-13 | Univ Rice William M | Derivados de uncialamicina, métodos de sintesis y su uso como agentes antitumor. |
-
2014
- 2014-08-14 MX MX2016001975A patent/MX368016B/es active IP Right Grant
- 2014-08-14 JP JP2016534843A patent/JP6474404B2/ja not_active Expired - Fee Related
- 2014-08-14 EP EP14758223.3A patent/EP3033346B1/en active Active
- 2014-08-14 CN CN201480056718.0A patent/CN105899515B/zh active Active
- 2014-08-14 ES ES14758223T patent/ES2769876T3/es active Active
- 2014-08-14 KR KR1020167006599A patent/KR20160068738A/ko not_active Ceased
- 2014-08-14 SG SG11201601047SA patent/SG11201601047SA/en unknown
- 2014-08-14 SG SG10201810067YA patent/SG10201810067YA/en unknown
- 2014-08-14 CA CA2921401A patent/CA2921401A1/en not_active Abandoned
- 2014-08-14 US US14/911,881 patent/US9777013B2/en active Active
- 2014-08-14 EA EA201690388A patent/EA201690388A1/ru unknown
- 2014-08-14 WO PCT/US2014/051127 patent/WO2015023879A1/en not_active Ceased
- 2014-08-14 AU AU2014306592A patent/AU2014306592B2/en not_active Ceased
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2016
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2017
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2019
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- 2019-06-07 AU AU2019204034A patent/AU2019204034A1/en not_active Abandoned
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| US10233192B2 (en) | 2019-03-19 |
| ES2769876T3 (es) | 2020-06-29 |
| US20160185791A1 (en) | 2016-06-30 |
| US9777013B2 (en) | 2017-10-03 |
| CN105899515A (zh) | 2016-08-24 |
| US20180065976A1 (en) | 2018-03-08 |
| MX2019010875A (es) | 2019-12-19 |
| EP3033346B1 (en) | 2020-01-08 |
| MX2016001975A (es) | 2016-11-14 |
| US20190382412A1 (en) | 2019-12-19 |
| JP2019089804A (ja) | 2019-06-13 |
| US10889590B2 (en) | 2021-01-12 |
| CN105899515B (zh) | 2020-01-14 |
| IL244084A0 (en) | 2016-04-21 |
| AU2019204034A1 (en) | 2019-07-04 |
| SG10201810067YA (en) | 2018-12-28 |
| SG11201601047SA (en) | 2016-03-30 |
| AU2014306592B2 (en) | 2019-04-04 |
| AU2014306592A1 (en) | 2016-03-10 |
| JP2016534105A (ja) | 2016-11-04 |
| JP6474404B2 (ja) | 2019-02-27 |
| KR20160068738A (ko) | 2016-06-15 |
| CA2921401A1 (en) | 2015-02-19 |
| EP3033346A1 (en) | 2016-06-22 |
| IL244084B (en) | 2019-08-29 |
| WO2015023879A1 (en) | 2015-02-19 |
| EA201690388A1 (ru) | 2016-07-29 |
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