PE20180610A1 - CONJUGADOS DE LIGADOR-PRINCIPIO ACTIVO (ADCs) Y CONJUGADOS DE LIGADOR-PROFARMACO (APDCs) CON GRUPOS ENZIMATICAMENTE ESCINDIBLES - Google Patents
CONJUGADOS DE LIGADOR-PRINCIPIO ACTIVO (ADCs) Y CONJUGADOS DE LIGADOR-PROFARMACO (APDCs) CON GRUPOS ENZIMATICAMENTE ESCINDIBLESInfo
- Publication number
- PE20180610A1 PE20180610A1 PE2017002810A PE2017002810A PE20180610A1 PE 20180610 A1 PE20180610 A1 PE 20180610A1 PE 2017002810 A PE2017002810 A PE 2017002810A PE 2017002810 A PE2017002810 A PE 2017002810A PE 20180610 A1 PE20180610 A1 PE 20180610A1
- Authority
- PE
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- Prior art keywords
- conjugates
- binder
- linker
- alkyl
- active principle
- Prior art date
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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
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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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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- A—HUMAN NECESSITIES
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- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- 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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- 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
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- 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
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- 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
- A61K47/6855—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 the tumour determinant being from breast cancer cell
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- A61K47/6857—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 the tumour determinant being from lung cancer cell
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- 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
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- 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
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Abstract
Referido a un conjugado de formula I, en donde el LIGADOR es ligador o su derivado, preferentemente anticuerpo; L es un enlazador; kn es un numero entero de 1 a 50; KSP es un inhibidor de la proteina de huso de la quinesina o de su profarmaco, de formula IIa, en donde en donde X1 es N, X2 es N y X3 es C, entre otros; R1 es H, halogeno, entre otros; R2 es -L-#1, H, -MOD, entre otros; R4 es -L-#1, H, entre otros; R3 es -L-#1, MOD, alquilo, entre otros; R5 es H, NH2, NO2, entre otros; R6 y R7 son, de modo independiente entre si, N, ciano, alquilo C1-10, entre otros; R8 es alquilo C1-10 (eventualmente fluorado), alquenilo C2-10 (eventualmente fluorado), entre otros; R9 es H, F, CH3, entre otros; A es CO, SO, SO2, SO2NH o CNNH; en donde -L#1 es el enlace con el ligador o su derivado; -MOD es -(NR10)n-(G1)o-G2-H; n es 0 o 1; o es 0 o 1; R10 es H o alquilo C1-3; G1 es -NH-C(=O), entre otros; G2 es un hidrocarburo de cadena recta y/o ramificada que tiene 1 a 10 atomos de carbono, entre otros. Tambien se refiere a procedimientos para preparar estos conjugados. Estos conjugados de ligador-profarmaco (APDC) o ligador-principio activo (ADC), son utiles en tratamientos de enfermedades proliferativas como el cancer.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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EP15173102 | 2015-06-22 | ||
EP16160738 | 2016-03-16 |
Publications (1)
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PE20180610A1 true PE20180610A1 (es) | 2018-04-09 |
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PE2017002810A PE20180610A1 (es) | 2015-06-22 | 2016-06-20 | CONJUGADOS DE LIGADOR-PRINCIPIO ACTIVO (ADCs) Y CONJUGADOS DE LIGADOR-PROFARMACO (APDCs) CON GRUPOS ENZIMATICAMENTE ESCINDIBLES |
Country Status (16)
Country | Link |
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US (2) | US11123439B2 (es) |
EP (1) | EP3310440A1 (es) |
JP (2) | JP6971858B2 (es) |
KR (1) | KR20180018808A (es) |
CN (2) | CN108025084A (es) |
AU (2) | AU2016282723B2 (es) |
BR (1) | BR112017027813A2 (es) |
CA (1) | CA2990076A1 (es) |
IL (2) | IL256394B (es) |
MX (1) | MX2017017172A (es) |
PE (1) | PE20180610A1 (es) |
RU (1) | RU2751512C2 (es) |
SG (2) | SG11201710639YA (es) |
TW (2) | TWI735448B (es) |
WO (1) | WO2016207089A1 (es) |
ZA (1) | ZA201800395B (es) |
Families Citing this family (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP5851842B2 (ja) * | 2009-01-12 | 2016-02-03 | サイトムエックス セラピューティクス, インク.CytomX Therapeutics, Inc. | 改変した抗体組成物、それを作製および使用する方法 |
AU2016282723B2 (en) | 2015-06-22 | 2021-09-23 | Bayer Pharma Aktiengesellschaft | Antibody drug conjugates (ADCs) and antibody prodrug conjugates (APDCs) with enzymatically cleavable groups |
WO2016207098A1 (de) | 2015-06-23 | 2016-12-29 | Bayer Pharma Aktiengesellschaft | Antikörper-wirkstoff-konjugate (adcs) von ksp-inhibitoren mit anti-cd123-antikörpern |
PE20180452A1 (es) | 2015-06-23 | 2018-03-05 | Bayer Pharma AG | Conjugados homogeneos especificos de sitio con inhibidores de ksp |
JP7251981B2 (ja) * | 2016-03-24 | 2023-04-04 | バイエル ファーマ アクチエンゲゼルシャフト | 酵素開裂基を有する細胞毒性活性剤のプロドラッグ |
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TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Hdac抑制劑與pd-l1抑制劑之組合治療 |
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RU2751512C2 (ru) | 2021-07-14 |
KR20180018808A (ko) | 2018-02-21 |
MX2017017172A (es) | 2018-02-23 |
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JP7394103B2 (ja) | 2023-12-07 |
CN108025084A (zh) | 2018-05-11 |
TW202216213A (zh) | 2022-05-01 |
JP2022025122A (ja) | 2022-02-09 |
ZA201800395B (en) | 2021-07-28 |
AU2016282723A1 (en) | 2018-01-18 |
US20230039341A1 (en) | 2023-02-09 |
US20180169256A1 (en) | 2018-06-21 |
AU2016282723B2 (en) | 2021-09-23 |
SG11201710639YA (en) | 2018-01-30 |
JP2018524321A (ja) | 2018-08-30 |
RU2018102153A (ru) | 2019-07-25 |
JP6971858B2 (ja) | 2021-11-24 |
US11123439B2 (en) | 2021-09-21 |
RU2018102153A3 (es) | 2019-12-03 |
CN114917361A (zh) | 2022-08-19 |
BR112017027813A2 (pt) | 2018-08-28 |
CA2990076A1 (en) | 2016-12-29 |
IL291160A (en) | 2022-05-01 |
AU2021290341A1 (en) | 2022-02-03 |
WO2016207089A1 (de) | 2016-12-29 |
EP3310440A1 (de) | 2018-04-25 |
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