MX2018011627A - Profarmacos de farmacos citotoxicos que tienen grupos enzimaticamente escindibles. - Google Patents
Profarmacos de farmacos citotoxicos que tienen grupos enzimaticamente escindibles.Info
- Publication number
- MX2018011627A MX2018011627A MX2018011627A MX2018011627A MX2018011627A MX 2018011627 A MX2018011627 A MX 2018011627A MX 2018011627 A MX2018011627 A MX 2018011627A MX 2018011627 A MX2018011627 A MX 2018011627A MX 2018011627 A MX2018011627 A MX 2018011627A
- Authority
- MX
- Mexico
- Prior art keywords
- prodrugs
- active agents
- conjugates
- cleavable groups
- enzymatically cleavable
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/335—Radicals substituted by nitrogen atoms not forming part of a nitro radical
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- 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
- A61K47/62—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 a protein, peptide or polyamino acid
- A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
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- 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
- A61K47/6845—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 cytokine, e.g. growth factors, VEGF, TNF, a lymphokine or an interferon
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- 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
- A61K47/6849—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 receptor, a cell surface antigen or a cell surface determinant
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- 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
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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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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- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
Abstract
La invención se refiere a novedosos profármacos o conjugados de la fórmula general (la) (ver Fórmula) en los cuales los fármacos citotóxicos, por ejemplo los inhibidores de la proteína fusiforme de la quinesina, están enmascarados con los grupos escindibles con legumina y por lo tanto liberan el fármaco, y al uso de estos profármacos o conjugados para el tratamiento y/o la prevención de enfermedades, y al uso de estos conjugados o profármacos para la producción de medicamentos para el tratamiento y/o la prevención de enfermedades, especialmente de trastornos hiperproliferativos y/o angiogénicos, por ejemplo cánceres.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP16162400 | 2016-03-24 | ||
EP16205988 | 2016-12-21 | ||
PCT/EP2017/056684 WO2017162663A1 (de) | 2016-03-24 | 2017-03-21 | Prodrugs von cytotoxischen wirkstoffen mit enzymatisch spaltbaren gruppen |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2018011627A true MX2018011627A (es) | 2019-01-10 |
Family
ID=58361030
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2018011627A MX2018011627A (es) | 2016-03-24 | 2017-03-21 | Profarmacos de farmacos citotoxicos que tienen grupos enzimaticamente escindibles. |
Country Status (18)
Country | Link |
---|---|
US (2) | US11685714B2 (es) |
EP (1) | EP3432934B1 (es) |
JP (1) | JP7251981B2 (es) |
KR (1) | KR20180123047A (es) |
CN (2) | CN108883195A (es) |
AU (1) | AU2017236431A1 (es) |
BR (1) | BR112018069483A2 (es) |
CA (1) | CA3018630A1 (es) |
CL (1) | CL2018002699A1 (es) |
CO (1) | CO2018010026A2 (es) |
IL (1) | IL261758A (es) |
MX (1) | MX2018011627A (es) |
PE (1) | PE20181852A1 (es) |
RU (1) | RU2018136778A (es) |
SG (2) | SG10202008909VA (es) |
TW (1) | TW201735954A (es) |
UY (1) | UY37168A (es) |
WO (1) | WO2017162663A1 (es) |
Families Citing this family (15)
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EP3310440A1 (de) | 2015-06-22 | 2018-04-25 | Bayer Pharma Aktiengesellschaft | Binder-wirkstoff-konjugate (adcs) und binder-prodrug-konjugate (apdcs) mit enzymatisch spaltbaren gruppen |
EP3313524A1 (de) | 2015-06-23 | 2018-05-02 | Bayer Pharma Aktiengesellschaft | Antikörper-wirkstoff-konjugate (adcs) von ksp-inhibitoren mit anti-cd123-antikörpern |
EP3313523A2 (en) | 2015-06-23 | 2018-05-02 | Bayer Pharma Aktiengesellschaft | Targeted conjugates of ksp inhibitors |
RU2018136778A (ru) | 2016-03-24 | 2020-04-24 | Байер Фарма Акциенгезельшафт | Пролекарства цитотоксических лекарственных средств, содержащие ферментативно расщепляемые группы |
WO2017216028A1 (en) | 2016-06-15 | 2017-12-21 | Bayer Pharma Aktiengesellschaft | Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies |
CN110312533B (zh) * | 2016-12-21 | 2023-11-03 | 拜耳公司 | 具有酶促可裂解的基团的细胞毒性活性剂的前药 |
JP7066714B2 (ja) * | 2016-12-21 | 2022-05-13 | バイエル・ファルマ・アクティエンゲゼルシャフト | 酵素的に切断可能な基を有する抗体薬物コンジュゲート(adc) |
US11433140B2 (en) | 2016-12-21 | 2022-09-06 | Bayer Pharma Aktiengesellschaft | Specific antibody drug conjugates (ADCs) having KSP inhibitors |
CN112601553A (zh) * | 2018-06-18 | 2021-04-02 | 拜耳股份有限公司 | 具有可酶切的接头和改善的活性谱的针对cxcr5的结合剂-药物缀合物 |
WO2020113094A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
CN110428870B (zh) * | 2019-08-08 | 2023-03-21 | 苏州泓迅生物科技股份有限公司 | 一种预测抗体重链轻链配对概率的方法及其应用 |
CN113754541A (zh) * | 2020-06-02 | 2021-12-07 | 深圳湾实验室 | 靶向eb病毒核抗原蛋白的小分子抑制剂、制备方法及其应用 |
WO2022167052A1 (en) * | 2021-02-08 | 2022-08-11 | Y-Mabs Therapeutics, Inc. | Use of ascorbic acid as stabilizing agent for anti b7-h3 antibodies |
JP2024506590A (ja) * | 2021-02-16 | 2024-02-14 | グリコス・フィンランド・オーワイ | リンカー-ペイロードおよびそのコンジュゲート |
CN112979491B (zh) * | 2021-02-24 | 2022-04-15 | 中国药科大学 | 一种包含过氧化氢/组织蛋白酶l响应性保护基的化合物及其应用 |
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2017
- 2017-03-21 RU RU2018136778A patent/RU2018136778A/ru not_active Application Discontinuation
- 2017-03-21 CN CN201780019957.2A patent/CN108883195A/zh active Pending
- 2017-03-21 PE PE2018001862A patent/PE20181852A1/es not_active Application Discontinuation
- 2017-03-21 WO PCT/EP2017/056684 patent/WO2017162663A1/de active Application Filing
- 2017-03-21 MX MX2018011627A patent/MX2018011627A/es unknown
- 2017-03-21 AU AU2017236431A patent/AU2017236431A1/en not_active Abandoned
- 2017-03-21 EP EP17712140.7A patent/EP3432934B1/de active Active
- 2017-03-21 CN CN202211097986.XA patent/CN116059390A/zh active Pending
- 2017-03-21 BR BR112018069483A patent/BR112018069483A2/pt not_active Application Discontinuation
- 2017-03-21 US US16/087,928 patent/US11685714B2/en active Active
- 2017-03-21 KR KR1020187027099A patent/KR20180123047A/ko not_active Application Discontinuation
- 2017-03-21 CA CA3018630A patent/CA3018630A1/en active Pending
- 2017-03-21 SG SG10202008909VA patent/SG10202008909VA/en unknown
- 2017-03-21 SG SG11201808167VA patent/SG11201808167VA/en unknown
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- 2017-03-24 TW TW106109896A patent/TW201735954A/zh unknown
- 2017-03-24 UY UY0001037168A patent/UY37168A/es not_active Application Discontinuation
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2018
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- 2018-09-24 CO CONC2018/0010026A patent/CO2018010026A2/es unknown
- 2018-09-24 CL CL2018002699A patent/CL2018002699A1/es unknown
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2023
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Also Published As
Publication number | Publication date |
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CN116059390A (zh) | 2023-05-05 |
JP7251981B2 (ja) | 2023-04-04 |
PE20181852A1 (es) | 2018-12-03 |
SG10202008909VA (en) | 2020-10-29 |
AU2017236431A1 (en) | 2018-09-27 |
EP3432934B1 (de) | 2022-02-23 |
US11685714B2 (en) | 2023-06-27 |
UY37168A (es) | 2017-10-31 |
WO2017162663A1 (de) | 2017-09-28 |
SG11201808167VA (en) | 2018-10-30 |
CA3018630A1 (en) | 2017-09-28 |
JP2019512517A (ja) | 2019-05-16 |
US20240043379A1 (en) | 2024-02-08 |
AU2017236431A2 (en) | 2018-11-08 |
KR20180123047A (ko) | 2018-11-14 |
TW201735954A (zh) | 2017-10-16 |
CO2018010026A2 (es) | 2018-09-28 |
RU2018136778A (ru) | 2020-04-24 |
CL2018002699A1 (es) | 2019-01-18 |
US20190077752A1 (en) | 2019-03-14 |
BR112018069483A2 (pt) | 2019-07-30 |
IL261758A (en) | 2018-10-31 |
EP3432934A1 (de) | 2019-01-30 |
CN108883195A (zh) | 2018-11-23 |
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