RU2618523C2 - Аналоги сплицеостатина - Google Patents

Аналоги сплицеостатина Download PDF

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RU2618523C2
RU2618523C2 RU2015115954A RU2015115954A RU2618523C2 RU 2618523 C2 RU2618523 C2 RU 2618523C2 RU 2015115954 A RU2015115954 A RU 2015115954A RU 2015115954 A RU2015115954 A RU 2015115954A RU 2618523 C2 RU2618523 C2 RU 2618523C2
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Russia
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alkyl
nrr
group
independently selected
hydrogen
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RU2015115954A
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Russian (ru)
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RU2015115954A (ru
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Кеннет Джон ДИРИКО
Алессандра С. ЭУСТАКУЙО
Майкл Эрик Грин
Хайин Хэ
Мин ХЕ
Франк Эрик КОЭН
Кристофер Джон О'Доннелл
Саджит ПУТЕНВЕЕТИЛ
Анокха Саяни РАТНАЯКЕ
Чакрапани СУБРАМАНИЯМ
Джессе Александер ТЭСКЕ
Хуэй Юй ЯН
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Пфайзер Инк.
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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
    • A61K47/6851—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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    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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    • 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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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/453—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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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
    • 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
    • A61K47/6869—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 a cell of the reproductive system: ovaria, uterus, testes, prostate
    • A—HUMAN NECESSITIES
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    • 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/10—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
    • C07D493/20—Spiro-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Cell Biology (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Microbiology (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pyrane Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Mycology (AREA)
RU2015115954A 2012-11-05 2013-10-22 Аналоги сплицеостатина RU2618523C2 (ru)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201261722769P 2012-11-05 2012-11-05
US61/722,769 2012-11-05
US201261723645P 2012-11-07 2012-11-07
US61/723,645 2012-11-07
US201361829409P 2013-05-31 2013-05-31
US61/829,409 2013-05-31
PCT/IB2013/059553 WO2014068443A1 (en) 2012-11-05 2013-10-22 Spliceostatin analogs

Publications (2)

Publication Number Publication Date
RU2015115954A RU2015115954A (ru) 2016-12-20
RU2618523C2 true RU2618523C2 (ru) 2017-05-04

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RU2015115954A RU2618523C2 (ru) 2012-11-05 2013-10-22 Аналоги сплицеостатина

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US (3) US9169264B2 (enExample)
EP (1) EP2917195B9 (enExample)
JP (1) JP6355641B2 (enExample)
KR (1) KR101762047B1 (enExample)
CN (1) CN105121421B (enExample)
AR (1) AR093339A1 (enExample)
AU (1) AU2013340449B2 (enExample)
BR (1) BR112015010070B1 (enExample)
CA (1) CA2890569C (enExample)
DK (1) DK2917195T5 (enExample)
ES (1) ES2656298T3 (enExample)
HU (1) HUE036433T2 (enExample)
IL (1) IL238578B (enExample)
MX (2) MX361218B (enExample)
PL (1) PL2917195T3 (enExample)
PT (1) PT2917195T (enExample)
RU (1) RU2618523C2 (enExample)
SI (1) SI2917195T1 (enExample)
TW (1) TW201431846A (enExample)
WO (1) WO2014068443A1 (enExample)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105829299A (zh) * 2013-11-19 2016-08-03 普渡研究基金会 抗癌剂及其制备
MX385651B (es) * 2013-12-19 2025-03-18 Seagen Inc Enlazadores de carbamato de metileno para su uso en conjugados de farmacos dirigidos.
HUE060643T2 (hu) * 2013-12-19 2023-04-28 Seagen Inc Metilén-karbamát-linkerek célzott hatóanyag-konjgátumokkal közös alkalmazásra
HUE043427T2 (hu) 2014-01-27 2019-08-28 Pfizer Bifunkciós citotoxikus szerek
US9840553B2 (en) 2014-06-28 2017-12-12 Kodiak Sciences Inc. Dual PDGF/VEGF antagonists
ES2815353T3 (es) * 2014-09-03 2021-03-29 Immunogen Inc Derivados de benzodiazepina citotóxicos
GB201416960D0 (en) * 2014-09-25 2014-11-12 Antikor Biopharma Ltd Biological materials and uses thereof
KR102210104B1 (ko) 2014-10-17 2021-02-01 코디악 사이언시스 인코포레이티드 부티릴콜린에스테라제 양성이온성 중합체 컨쥬게이트
US10676773B2 (en) * 2015-03-10 2020-06-09 Bristol-Myers Squibb Company Antibodies conjugatable by transglutaminase and conjugates made therefrom
WO2016151432A1 (en) 2015-03-20 2016-09-29 Pfizer Inc. Bifunctional cytotoxic agents containing the cti pharmacophore
GB2542391A (en) * 2015-09-17 2017-03-22 Annexin Pharmaceuticals Ab Process of manufacture
MA43354A (fr) * 2015-10-16 2018-08-22 Genentech Inc Conjugués médicamenteux à pont disulfure encombré
EP3165237B1 (en) 2015-11-03 2018-12-19 Industrial Technology Research Institute Antibody-drug conjugate (adc) and method for forming the same
CA3010056A1 (en) 2015-12-30 2017-07-06 Kodiak Sciences Inc. Antibodies and conjugates thereof
SMT202100416T1 (it) 2016-03-02 2021-09-14 Eisai R&D Man Co Ltd Coniugati anticorpo-farmaco a base di eribulina e metodi di uso
WO2017156454A1 (en) * 2016-03-10 2017-09-14 The Regents Of The University Of California Anti-cancer and splce modulating compounds and methods
CA3027029A1 (en) 2016-06-08 2017-12-14 William Marsh Rice University Derivatives of thailanstatin a, methods of treatment and methods of synthesis thereof
JP2018058822A (ja) 2016-08-03 2018-04-12 ファイザー・インク ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用
DK3515492T3 (da) 2016-09-23 2023-08-28 Purdue Research Foundation Midler mod cancer og fremstilling heraf
JP7050770B2 (ja) * 2016-10-05 2022-04-08 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト 抗体薬物コンジュゲートの調製方法
TWI835714B (zh) 2016-10-18 2024-03-21 美商思進公司 菸鹼醯胺腺嘌呤二核苷酸補救合成(salvage pathway)抑制劑之靶向投遞
CN110461860A (zh) 2017-01-24 2019-11-15 辉瑞公司 卡奇霉素衍生物及其抗体药物缀合物
MX2019011003A (es) 2017-03-15 2019-12-16 Eisai R&D Man Co Ltd Mutaciones de empalmosoma y usos de las mismas.
TW201904613A (zh) 2017-04-27 2019-02-01 美商西雅圖遺傳學公司 季鹼化菸鹼醯胺腺二核苷酸補救合成抑制劑結合物
CN111246740B (zh) * 2017-09-08 2022-06-10 马罗内生物创新公司 新型除草化合物
EP3684773A1 (en) * 2017-09-20 2020-07-29 pH Pharma Co., Ltd. Thailanstatin analogs
CA3084092A1 (en) * 2017-12-06 2019-06-13 Ontario Institute For Cancer Research (Oicr) Acyl hydrazone linkers, methods and uses thereof
EP3728273A4 (en) 2017-12-22 2021-12-29 Ontario Institute for Cancer Research (OICR) Heterocyclic acyl hydrazone linkers, methods and uses thereof
CN112203679A (zh) 2018-03-02 2021-01-08 科达制药股份有限公司 Il-6抗体及其融合构建体和缀合物
IL316090A (en) 2018-06-01 2024-12-01 Eisai R&D Man Co Ltd Antibody-drug conjugates of splicing modulators and methods of use
PH12021551389A1 (en) * 2018-12-13 2022-05-16 Eisai R&D Man Co Ltd Herboxidiene antibody-drug conjugates and methods of use
CN109734627A (zh) * 2019-03-04 2019-05-10 浙江华贝药业有限责任公司 一种新的化合物n-2-烷酰基-n-6-芴甲氧羰基-l-赖氨酸
CN109761857A (zh) * 2019-03-04 2019-05-17 浙江华贝药业有限责任公司 N-2-棕榈酰基-n-6-芴甲氧羰基-l-赖氨酸的提纯方法
CN109928895A (zh) * 2019-03-04 2019-06-25 浙江华贝药业有限责任公司 一种n-2-烷酰基-n-6-芴甲氧羰基-l-赖氨酸的合成方法
CN114786731A (zh) 2019-10-10 2022-07-22 科达制药股份有限公司 治疗眼部病症的方法
KR20220166828A (ko) * 2020-04-09 2022-12-19 브리스톨-마이어스 스큅 컴퍼니 메야마이신 유사체 및 그의 사용 방법
US12257214B2 (en) * 2021-06-02 2025-03-25 The Charlotte Mecklenburg Hospital Authority Compositions and methods comprising deoxy-pentitols
AU2024257248A1 (en) * 2023-04-17 2025-11-06 Peak Bio, Inc. Antibodies and antibody-drug conjugates and methods of use and synthetic processes and intermediates

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2073681C1 (ru) * 1989-02-07 1997-02-20 Фармиталиа Карло Эрба С.Р.Л. Антрациклиновый гликозид и способы его получения
WO2011106491A2 (en) * 2010-02-25 2011-09-01 Marrone Bio Innovations, Inc. Isolated bacterial strain of the genus burkholderia and pesticidal metabolites therefrom

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2036891B (en) 1978-12-05 1983-05-05 Windsor Smith C Change speed gear
GB8308235D0 (en) 1983-03-25 1983-05-05 Celltech Ltd Polypeptides
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
JPS6147500A (ja) 1984-08-15 1986-03-07 Res Dev Corp Of Japan キメラモノクロ−ナル抗体及びその製造法
EP0173494A3 (en) 1984-08-27 1987-11-25 The Board Of Trustees Of The Leland Stanford Junior University Chimeric receptors by dna splicing and expression
GB8422238D0 (en) 1984-09-03 1984-10-10 Neuberger M S Chimeric proteins
JPS61134325A (ja) 1984-12-04 1986-06-21 Teijin Ltd ハイブリツド抗体遺伝子の発現方法
AU606320B2 (en) 1985-11-01 1991-02-07 International Genetic Engineering, Inc. Modular assembly of antibody genes, antibodies prepared thereby and use
US5225539A (en) 1986-03-27 1993-07-06 Medical Research Council Recombinant altered antibodies and methods of making altered antibodies
US5530101A (en) 1988-12-28 1996-06-25 Protein Design Labs, Inc. Humanized immunoglobulins
DE3920358A1 (de) 1989-06-22 1991-01-17 Behringwerke Ag Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung
US5633425A (en) 1990-08-29 1997-05-27 Genpharm International, Inc. Transgenic non-human animals capable of producing heterologous antibodies
US5545806A (en) 1990-08-29 1996-08-13 Genpharm International, Inc. Ransgenic non-human animals for producing heterologous antibodies
US5625126A (en) 1990-08-29 1997-04-29 Genpharm International, Inc. Transgenic non-human animals for producing heterologous antibodies
US5661016A (en) 1990-08-29 1997-08-26 Genpharm International Inc. Transgenic non-human animals capable of producing heterologous antibodies of various isotypes
CA2089661C (en) 1990-08-29 2007-04-03 Nils Lonberg Transgenic non-human animals capable of producing heterologous antibodies
EP1136556B1 (en) 1991-11-25 2005-06-08 Enzon, Inc. Method of producing multivalent antigen-binding proteins
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
AU728657B2 (en) 1996-03-18 2001-01-18 Board Of Regents, The University Of Texas System Immunoglobulin-like domains with increased half-lives
PT2357006E (pt) 2002-07-31 2016-01-22 Seattle Genetics Inc Conjugados de fármacos e sua utilização para tratamento do cancro, de uma doença autoimune ou de uma doença infeciosa
CA2479696A1 (en) * 2003-11-11 2005-05-11 Amadeo Parissenti Use of calphostin-c to treat drug-sensitive tumor cells
EP2292248A3 (en) 2005-03-03 2011-06-29 CovX Technologies Ireland Limited Anti-angiogenic compounds
NZ566982A (en) * 2005-09-26 2011-06-30 Medarex Inc Duocarmycin drug conjugates
US7825267B2 (en) * 2006-09-08 2010-11-02 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Synthesis of FR901464 and analogs with antitumor activity
US8969405B2 (en) * 2008-06-21 2015-03-03 St. Jude Children's Research Hospital Anticancer compounds and methods of making and using same
KR101671360B1 (ko) * 2010-04-15 2016-11-01 시애틀 지네틱스, 인크. 표적화된 피롤로벤조디아제핀 접합체
TWI540136B (zh) * 2010-04-15 2016-07-01 梅迪繆思有限公司 吡咯并苯并二氮呯及其共軛物
JP2012086587A (ja) 2010-10-15 2012-05-10 Hitachi Ltd 鉄道車両
WO2012059882A2 (en) 2010-11-05 2012-05-10 Rinat Neuroscience Corporation Engineered polypeptide conjugates and methods for making thereof using transglutaminase
CA2954166A1 (en) 2011-11-11 2013-05-16 Rinat Neuroscience Corp. Antibodies specific for trop-2 and their uses

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2073681C1 (ru) * 1989-02-07 1997-02-20 Фармиталиа Карло Эрба С.Р.Л. Антрациклиновый гликозид и способы его получения
WO2011106491A2 (en) * 2010-02-25 2011-09-01 Marrone Bio Innovations, Inc. Isolated bacterial strain of the genus burkholderia and pesticidal metabolites therefrom

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
C.F.Tomspson et al, "Total Synthesis, Proof Structure, and Evaluation of Synthetic Analogues",J.Am.Chem.Soc., 2001,v.123, no.41,p.9974-9983. *
Ryonei Furumai et al, "Spliceostatin A blocks angiogentsis by inhibiting global gene expression including VEGE", CANCER SCIENCE,2010,v.101,no.11,p.2483-2489. Sami Osman et al, "Evaluation of FR 901464 analogues and in vivo", MEDCHEMCOMM, 2011,v.2,no.1,p.38. Liying Fan et al, "Sudemycins, novel small molecule analogues of FR 901464, induce alternative gene splicing", ACS CHEMICAL BIOLOGY, 2011, v.6,no.6,p.582-589 (см. abstract). *

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