MX2014008373A - Conjugados antagonistas de integrina para suministro dirigido a celulas que expresan alfa-v-beta-3. - Google Patents

Conjugados antagonistas de integrina para suministro dirigido a celulas que expresan alfa-v-beta-3.

Info

Publication number
MX2014008373A
MX2014008373A MX2014008373A MX2014008373A MX2014008373A MX 2014008373 A MX2014008373 A MX 2014008373A MX 2014008373 A MX2014008373 A MX 2014008373A MX 2014008373 A MX2014008373 A MX 2014008373A MX 2014008373 A MX2014008373 A MX 2014008373A
Authority
MX
Mexico
Prior art keywords
beta
cells expressing
targeted delivery
integrin antagonist
expressing alpha
Prior art date
Application number
MX2014008373A
Other languages
English (en)
Inventor
Matthew Michael Hamilton
Achyutharao Sidduri
Robert Alan Goodnow Jr
Agnieszka Kowalczyk
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MX2014008373A publication Critical patent/MX2014008373A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/587—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with aliphatic hydrocarbon radicals substituted by 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, said aliphatic radicals being substituted in the alpha-position to the ring by a hetero atom, e.g. with m >= 0, Z being a singly or a doubly bound hetero atom
    • C07D277/593—Z being doubly bound oxygen or doubly bound nitrogen, which nitrogen is part of a possibly substituted oximino radical
    • 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
    • C07D207/44—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
    • 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
    • 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
    • A61K47/54—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
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/52—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the nitrogen atom of at least one of the carboxamide groups further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/20—Esters of monothiocarboxylic acids
    • C07C327/32—Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • 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
    • C07D207/44—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
    • C07D239/12—Nitrogen atoms not forming part of a nitro radical
    • C07D239/14—Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

La invención se refiere a compuestos de fórmula (I): en la que R1, R2, y n se definen en la descripción detallada y las reivindicaciones. En particular, la presente invención se refiere a los compuestos de fórmula (I) para uso en la fabricación y suministros de restos conjugados tales como pequeñas moléculas, péptidos, ácidos nucleicos, restos fluorescentes, y polímeros que están ligados a antagonistas de integrina alfa-V-beta-3 a las células objetivo que expresan alfa-V-beta-3.
MX2014008373A 2012-01-27 2013-01-22 Conjugados antagonistas de integrina para suministro dirigido a celulas que expresan alfa-v-beta-3. MX2014008373A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261591299P 2012-01-27 2012-01-27
US201261678669P 2012-08-02 2012-08-02
PCT/EP2013/051082 WO2013110578A1 (en) 2012-01-27 2013-01-22 Integrin antagonist conjugates for targeted delivery to cells expressing alpha-v-beta-3

Publications (1)

Publication Number Publication Date
MX2014008373A true MX2014008373A (es) 2014-09-26

Family

ID=47628132

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014008373A MX2014008373A (es) 2012-01-27 2013-01-22 Conjugados antagonistas de integrina para suministro dirigido a celulas que expresan alfa-v-beta-3.

Country Status (12)

Country Link
US (1) US9586916B2 (es)
EP (1) EP2806899B1 (es)
JP (1) JP6316209B2 (es)
KR (1) KR20150009952A (es)
CN (1) CN104144706B (es)
BR (1) BR112014016736A8 (es)
CA (1) CA2856619A1 (es)
ES (1) ES2605939T3 (es)
HK (1) HK1202426A1 (es)
MX (1) MX2014008373A (es)
RU (1) RU2623441C2 (es)
WO (1) WO2013110578A1 (es)

Families Citing this family (8)

* 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
MX2014008590A (es) * 2012-01-27 2015-03-03 Hoffmann La Roche Conjugados de antagonista de la integrina para suministro dirigido a celulas que expresan el antigeno 1 asociado a la funcion de linfocitos (lfa-1).
CN104023751B (zh) * 2012-01-27 2016-11-09 弗·哈夫曼-拉罗切有限公司 靶向递送至表达vla-4的细胞的整联蛋白拮抗剂结合物
CA2919088A1 (en) * 2013-08-07 2015-02-12 Arrowhead Research Corporation Polyconjugates for delivery of rnai triggers to tumor cells in vivo
JP7035044B2 (ja) 2016-11-11 2022-03-14 ジーランド ファーマ エー／エス α４β７インテグリンを標的とする環状ペプチド多量体
CN110283223B (zh) * 2018-03-19 2022-01-04 广州市锐博生物科技有限公司 一种阳离子脂质分子及其在核酸递送中的应用
EP3784269A4 (en) * 2018-04-27 2022-03-23 Arrowhead Pharmaceuticals, Inc. ANTI-INTEGRIN LIGANDS AND USES THEREOF
US20200085979A1 (en) * 2018-09-11 2020-03-19 Stanley Satz Precision medicine theranostics and diagnostics a combination thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69716900T2 (de) * 1996-04-10 2003-07-03 Merck & Co Inc Alpha v Beta 3 ANTAGONISTEN
AU4551500A (en) * 1999-04-28 2000-11-17 Basf Aktiengesellschaft Integrin receptor antagonists
ITRM20040241A1 (it) * 2004-05-13 2004-08-13 Ist Naz Stud Cura Dei Tumori Camptotecine coniugate in posizione 20 con antagonisti delle integrine.
US7300940B2 (en) * 2004-08-04 2007-11-27 The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services Integrin α-v β-3 antagonists for use in imaging and therapy
AU2005314392B2 (en) * 2004-12-09 2011-04-14 Centocor, Inc. Anti-integrin immunoconjugates, methods and uses
US8686044B2 (en) 2008-08-13 2014-04-01 Mitsui Chemicals Agro, Inc. Amide derivative, pest control agent containing the amide derivative, and use of the amide derivative
CA2740000C (en) 2008-10-09 2017-12-12 Tekmira Pharmaceuticals Corporation Improved amino lipids and methods for the delivery of nucleic acids

Also Published As

Publication number Publication date
EP2806899A1 (en) 2014-12-03
JP6316209B2 (ja) 2018-04-25
HK1202426A1 (en) 2015-10-02
CA2856619A1 (en) 2013-08-01
RU2623441C2 (ru) 2017-06-26
US9586916B2 (en) 2017-03-07
EP2806899B1 (en) 2016-10-19
CN104144706A (zh) 2014-11-12
WO2013110578A1 (en) 2013-08-01
BR112014016736A8 (pt) 2017-07-04
BR112014016736A2 (pt) 2017-06-13
CN104144706B (zh) 2017-03-29
RU2014132565A (ru) 2016-03-20
US20150038523A1 (en) 2015-02-05
ES2605939T3 (es) 2017-03-17
KR20150009952A (ko) 2015-01-27
JP2015506946A (ja) 2015-03-05

Similar Documents

Publication Publication Date Title
MX2014008373A (es) Conjugados antagonistas de integrina para suministro dirigido a celulas que expresan alfa-v-beta-3.
CY1124924T1 (el) Φαρμακευτικη συνθεση καρβετοκινης
CY1121299T1 (el) Υποκατεστημενες τρικυκλικες ενωσεις ως αναστολεις fgfr
CY1120560T1 (el) Βελτιστοποιημενο συστημα παραδοσης in vivo me ενδοσωματολυτικους παραγοντες για συζευγματα νουκλεϊνικου οξεος
MX356625B (es) Oligonucleotidos para elaborar un cambio en la secuencia de una molécula de ácido ribonucleico objetivo presente en una célula viva.
EA201390145A1 (ru) Конъюгаты, частицы, композиции и связанные с ними способы
EP4253395A3 (en) Processes for the preparation of carbohydrate conjugated rna agents
EA201070421A1 (ru) Микрорибонуклеиновые кислоты
CY1121466T1 (el) Αντισωματα εναντι προσδεματων υποδοχεα β1 βραδυκινινης
MX344009B (es) Conjugados de amatoxinas con enlaces mejorados.
NZ710729A (en) Amatoxin derivatives
HK1189031A1 (zh) 用於細胞內遞送核酸的小分子綴合物
EA201590783A1 (ru) Конъюгаты для доставки лекарственных средств и способы лечения заболеваний, вызванных клетками, экспрессирующими psma
EP3698631A3 (en) Methods of delivering oligonucleotides to immune cells
EA201200617A1 (ru) Полимеры на основе циклодекстрина для доставки лекарственных средств
MX2012000575A (es) Conjugados de epsilon-polilisina y uso de los mismos.
EP3065758A4 (en) Peptide containing conjugates for dual molecular delivery of oligonucleotides
MA33937B1 (fr) Composes pyrazole comme antagonistes du recepteur crth2
EA201491613A1 (ru) Катионные полимеры на основе гликогена
MX351015B (es) Conjugados de antagonista de la integrina para su suministro dirigido a celulas que expresan vla-4.
MY165075A (en) Pharmaceutical composition comprising fimasartan and hydrochlorothiazide
LT2013016A (lt) Aktyvuotos-potencijuotos formos antikūno poveikio padidinimo būdas
MX2014008590A (es) Conjugados de antagonista de la integrina para suministro dirigido a celulas que expresan el antigeno 1 asociado a la funcion de linfocitos (lfa-1).
EA201290243A1 (ru) Хиназолиновые соединения
EA201391643A1 (ru) Составы с замедленным высвобождением парацетамола