MX2014008590A - Conjugados de antagonista de la integrina para suministro dirigido a celulas que expresan el antigeno 1 asociado a la funcion de linfocitos (lfa-1). - Google Patents

Conjugados de antagonista de la integrina para suministro dirigido a celulas que expresan el antigeno 1 asociado a la funcion de linfocitos (lfa-1).

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Publication number
MX2014008590A
MX2014008590A MX2014008590A MX2014008590A MX2014008590A MX 2014008590 A MX2014008590 A MX 2014008590A MX 2014008590 A MX2014008590 A MX 2014008590A MX 2014008590 A MX2014008590 A MX 2014008590A MX 2014008590 A MX2014008590 A MX 2014008590A
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Mexico
Prior art keywords
cells expressing
targeted delivery
integrin antagonist
lfa
expressing lfa
Prior art date
Application number
MX2014008590A
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English (en)
Inventor
Matthew Michael Hamilton
Achyutharao Sidduri
Agnieszka Kowalczyk
Robert Alan Goodnow Jr
Original Assignee
Hoffmann La Roche
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Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MX2014008590A publication Critical patent/MX2014008590A/es

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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • 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
    • 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
    • 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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
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    • C07C327/04—Monothiocarboxylic acids having carbon atoms of thiocarboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
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    • 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
    • C07D207/34—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 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
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    • 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
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • C09B11/10—Amino derivatives of triarylmethanes
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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
    • C07D207/44—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 three double bonds between ring members or between ring members and non-ring members
    • C07D207/444—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 three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C07D207/448—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 three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide
    • C07D207/452—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 three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

La presente invención se refiere a compuestos de la fórmula I: en donde R1, R2, y n se definen en la descripción detallada y las reivindicaciones. En particular, la presente invención se refiere a los compuestos de la fórmula I para uso en la fabricación y suministro de porciones conjugadas tales como moléculas pequeñas, péptidos, ácidos nucleicos, porciones fluorescentes, y polímeros las cuales se enlazan a antagonistas de la integrina LFA-1 a las células objetivo que expresan LFA-1.
MX2014008590A 2012-01-27 2013-01-24 Conjugados de antagonista de la integrina para suministro dirigido a celulas que expresan el antigeno 1 asociado a la funcion de linfocitos (lfa-1). MX2014008590A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261591297P 2012-01-27 2012-01-27
US201261678673P 2012-08-02 2012-08-02
PCT/EP2013/051273 WO2013110679A1 (en) 2012-01-27 2013-01-24 Integrin antagonist conjugates for targeted delivery to cells expressing lfa-1

Publications (1)

Publication Number Publication Date
MX2014008590A true MX2014008590A (es) 2015-03-03

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MX2014008590A MX2014008590A (es) 2012-01-27 2013-01-24 Conjugados de antagonista de la integrina para suministro dirigido a celulas que expresan el antigeno 1 asociado a la funcion de linfocitos (lfa-1).

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US (2) US9650363B2 (es)
EP (1) EP2806897B1 (es)
JP (1) JP6182542B2 (es)
KR (1) KR20140121453A (es)
CN (1) CN104185478B (es)
BR (1) BR112014017517A2 (es)
CA (1) CA2857127A1 (es)
DK (1) DK2806897T3 (es)
HK (1) HK1202425A1 (es)
MX (1) MX2014008590A (es)
RU (1) RU2624732C2 (es)
WO (1) WO2013110679A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9447035B2 (en) * 2012-01-27 2016-09-20 Hoffmann-La Roche Inc. Integrin antagonist conjugates for targeted delivery to cells expressing VLA-4
US9650363B2 (en) * 2012-01-27 2017-05-16 Hoffmann-La Roche Inc. Integrin antagonist conjugates for targeted delivery to cells expressing LFA-1
CN111825622A (zh) * 2020-07-10 2020-10-27 西华大学 一种氧化脱氢芳构化制备2-嘧啶酮衍生物的方法
CN115028828B (zh) * 2022-07-19 2023-09-15 西安超磁纳米生物科技有限公司 一种可靶向肝细胞的聚乙二醇衍生物及其制备方法

Family Cites Families (12)

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Publication number Priority date Publication date Assignee Title
US6229011B1 (en) * 1997-08-22 2001-05-08 Hoffman-La Roche Inc. N-aroylphenylalanine derivative VCAM-1 inhibitors
HU229362B1 (en) * 1997-08-22 2013-11-28 Hoffmann La Roche N-alkanoylphenylalanine derivatives
SI1005445T1 (en) * 1997-08-22 2004-12-31 F. Hoffmann-La Roche Ag N-alkanoylphenylalanine derivatives
US6331640B1 (en) * 1998-10-13 2001-12-18 Hoffmann-La Roche Inc. Diaminopropionic acid derivatives
US6515124B2 (en) 2000-02-09 2003-02-04 Hoffman-La Roche Inc. Dehydroamino acids
US6774116B2 (en) * 2001-04-17 2004-08-10 Cryolife, Inc. Prodrugs via acylation with cinnamate
PT1881823E (pt) * 2005-05-17 2015-03-02 Sarcode Bioscience Inc Composições e métodos para o tratamento de transtornos oculares
EP2350043B9 (en) 2008-10-09 2014-08-20 TEKMIRA Pharmaceuticals Corporation Improved amino lipids and methods for the delivery of nucleic acids
US9447455B2 (en) * 2011-02-16 2016-09-20 Headway Technologies, Inc. Methods and compositions for the target-localized anchoring of detectable label
US20120270875A1 (en) * 2011-03-16 2012-10-25 Paul Gillespie Pyrimidine amide compounds
JP6316209B2 (ja) * 2012-01-27 2018-04-25 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ αＶβ３を発現する細胞への標的化送達のためのインテグリンアンタゴニスト結合体
US9650363B2 (en) * 2012-01-27 2017-05-16 Hoffmann-La Roche Inc. Integrin antagonist conjugates for targeted delivery to cells expressing LFA-1

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Publication number Publication date
CN104185478B (zh) 2016-10-12
CN104185478A (zh) 2014-12-03
WO2013110679A1 (en) 2013-08-01
JP2015508055A (ja) 2015-03-16
BR112014017517A2 (pt) 2017-06-13
EP2806897A1 (en) 2014-12-03
JP6182542B2 (ja) 2017-08-16
US20130197059A1 (en) 2013-08-01
CA2857127A1 (en) 2013-08-01
DK2806897T3 (en) 2017-10-16
US20150065534A1 (en) 2015-03-05
RU2014132837A (ru) 2016-03-20
KR20140121453A (ko) 2014-10-15
HK1202425A1 (en) 2015-10-02
EP2806897B1 (en) 2017-08-02
RU2624732C2 (ru) 2017-07-06
US9650363B2 (en) 2017-05-16

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