AR075090A1 - Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden. - Google Patents

Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.

Info

Publication number
AR075090A1
AR075090A1 ARP090103760A ARP090103760A AR075090A1 AR 075090 A1 AR075090 A1 AR 075090A1 AR P090103760 A ARP090103760 A AR P090103760A AR P090103760 A ARP090103760 A AR P090103760A AR 075090 A1 AR075090 A1 AR 075090A1
Authority
AR
Argentina
Prior art keywords
aliphatic
independently
substituted
unsubstituted
con
Prior art date
Application number
ARP090103760A
Other languages
English (en)
Inventor
Paul E Fleming
Jing Li
Original Assignee
Millennium Pharm Inc
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 Millennium Pharm Inc filed Critical Millennium Pharm Inc
Publication of AR075090A1 publication Critical patent/AR075090A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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
    • A61K31/69—Boron 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02—Boron compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02—Boron compounds
    • C07F5/04—Esters of boric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides

Abstract

Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1): o una sal farmacéuticamente aceptable o un anhídrido de ácido boronico del mismo, donde: A es 0, 1 o 2; P es hidrogeno o una porcion bloqueante del grupo amino: Ra1 es C1-6 alifático, C1-6 fluoroalifático, -(CH2)m-CH2-Rb, (CH2)m-CH2-NHC(=NR4)NH-Y, -(CH2)m-CH2-CON(R4)2, -(CH2)m-CH2-N(R4)CON(R4)2, -(CH2)m-CH(R6)N(R4)2, -(CH2)m-CH(R5)-OR5, o -(CH2)m-CH(R5)-SR5; cada Ra2 es en forma independiente hidrogeno, C1-6 alifático, C1-6 fluoroalifático, (CH2)m-CH2-Rb, -(CH2)m-CH2-NHC(=NR4)NH-Y, -(CH2)m-CH2-CON(R4)2, -(CH2)m-CH2-N(R4)CON(R4)2, -(CH2)m-CH(R6)N(R4)2, -(CH2)m-CH(R5)-OR5, o -(CH2)m-CH(R5)-SR5; cada Y es en forma independiente hidrogeno, -CN, -NO2, o -S(O)2-R10; cada Rb es en forma independiente un sistema de anillos monocíclico o bicíclico sustituido o no sustituido; cada R4 es en forma independiente hidrogeno o un grupo alifático, arilo, heteroarilo, o heterocíclilo sustituido o no sustituido: o dos R4 sobre el mismo átomo de nitrogeno, tomados junto con el átomo de nitrogeno, forman un anillo heterocíclilo de 4 a 8 miembros sustituido o no sustituido que tiene, además del átomo de nitrogeno, entre 0 y 2 heteroátomos del anillo seleccionados en forma independiente entre N, O, y S, cada R5 es en forma independiente hidrogeno o un grupo alifático, arilo, heteroarilo, o heterocíclilo sustituido o no sustituido: cada R6 es en forma independiente un grupo alifático, arilo, o heteroarilo sustituido o no sustituido: cada R10 es en forma independiente C1-6 alifático, C6-10 arilo, o -N(R4)2; m es 0, 1, o 2; Z1 y Z2 son cada uno en forma independiente hidroxi, alcoxi, ariloxi, o aralcoxi: o Z1 y Z2 juntos forman una porcion derivada de un agente de complexion de ácido boronico.
ARP090103760A 2008-09-29 2009-09-12 Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden. AR075090A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19461408P 2008-09-29 2008-09-29

Publications (1)

Publication Number Publication Date
AR075090A1 true AR075090A1 (es) 2011-03-09

Family

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ARP090103760A AR075090A1 (es) 2008-09-29 2009-09-12 Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.

Country Status (25)

Country Link
US (3) US8664200B2 (es)
EP (1) EP2346882B1 (es)
JP (3) JP5736314B2 (es)
KR (1) KR101739470B1 (es)
CN (2) CN102203103A (es)
AR (1) AR075090A1 (es)
AU (1) AU2009297113B2 (es)
BR (1) BRPI0919447B8 (es)
CA (1) CA2739375C (es)
CL (1) CL2011000653A1 (es)
CO (1) CO6362015A2 (es)
CR (2) CR20160475A (es)
DO (1) DOP2011000086A (es)
EA (1) EA030539B1 (es)
EC (1) ECSP11011011A (es)
IL (1) IL211983A0 (es)
MA (1) MA32729B1 (es)
MX (1) MX2011003317A (es)
MY (1) MY166653A (es)
NZ (2) NZ606001A (es)
SG (1) SG194388A1 (es)
TW (2) TWI598352B (es)
UA (1) UA105503C2 (es)
WO (1) WO2010036357A1 (es)
ZA (1) ZA201203615B (es)

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EA030539B1 (ru) 2018-08-31
JP2015143264A (ja) 2015-08-06
SG194388A1 (en) 2013-11-29
ZA201203615B (en) 2015-03-25
CA2739375A1 (en) 2010-04-01
JP2012504122A (ja) 2012-02-16
US20170349611A1 (en) 2017-12-07
CO6362015A2 (es) 2012-01-20
EP2346882A1 (en) 2011-07-27
UA105503C2 (uk) 2014-05-26
US8664200B2 (en) 2014-03-04
EA201170508A1 (ru) 2011-10-31
NZ606001A (en) 2014-08-29
AU2009297113A1 (en) 2010-04-01
CN103554143A (zh) 2014-02-05
KR20110082534A (ko) 2011-07-19
US10035811B2 (en) 2018-07-31
CL2011000653A1 (es) 2011-09-30
MY166653A (en) 2018-07-18
IL211983A0 (en) 2011-06-30
US20100081633A1 (en) 2010-04-01
CA2739375C (en) 2019-03-12
KR101739470B1 (ko) 2017-05-24
JP5736314B2 (ja) 2015-06-17
BRPI0919447B8 (pt) 2021-05-25
MX2011003317A (es) 2011-04-26
EP2346882B1 (en) 2017-09-20
WO2010036357A1 (en) 2010-04-01
TWI598352B (zh) 2017-09-11
NZ592497A (en) 2013-02-22
JP2017025091A (ja) 2017-02-02
US9771381B2 (en) 2017-09-26
CR20160475A (es) 2016-12-19
BRPI0919447A2 (pt) 2015-12-15
DOP2011000086A (es) 2011-04-15
BRPI0919447B1 (pt) 2021-03-30
TW201641504A (zh) 2016-12-01
CR20110216A (es) 2011-07-14
TW201024313A (en) 2010-07-01
MA32729B1 (fr) 2011-10-02
CN102203103A (zh) 2011-09-28
US20140194387A1 (en) 2014-07-10
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ECSP11011011A (es) 2011-07-29
CN103554143B (zh) 2018-02-23

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