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AR068681A1 - Inhibidores cristalinos peptidicos de epoxi cetona proteasa y la sintesis de ceto - epoxidos de aminoacidos - Google Patents

Inhibidores cristalinos peptidicos de epoxi cetona proteasa y la sintesis de ceto - epoxidos de aminoacidos

Info

Publication number
AR068681A1
AR068681A1 ARP080104358A ARP080104358A AR068681A1 AR 068681 A1 AR068681 A1 AR 068681A1 AR P080104358 A ARP080104358 A AR P080104358A AR P080104358 A ARP080104358 A AR P080104358A AR 068681 A1 AR068681 A1 AR 068681A1
Authority
AR
Argentina
Prior art keywords
formula
compound
crystalline
crystals
solution
Prior art date
Application number
ARP080104358A
Other languages
English (en)
Inventor
William Dean Fuller
Guy J Laidig
Louis C Sehl
Pasit Phiasivongsa
Original Assignee
Proteolix 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39941499&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR068681(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Proteolix Inc filed Critical Proteolix Inc
Publication of AR068681A1 publication Critical patent/AR068681A1/es

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Classifications

    • 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
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
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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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    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P37/02—Immunomodulators
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    • A—HUMAN NECESSITIES
    • A62—LIFE-SAVING; FIRE-FIGHTING
    • A62C—FIRE-FIGHTING
    • A62C3/00—Fire prevention, containment or extinguishing specially adapted for particular objects or places
    • A62C3/002—Fire prevention, containment or extinguishing specially adapted for particular objects or places for warehouses, storage areas or other installations for storing goods
    • A62C3/004—Fire prevention, containment or extinguishing specially adapted for particular objects or places for warehouses, storage areas or other installations for storing goods for freezing warehouses and storages
    • A—HUMAN NECESSITIES
    • A62—LIFE-SAVING; FIRE-FIGHTING
    • A62C—FIRE-FIGHTING
    • A62C35/00—Permanently-installed equipment
    • A62C35/58—Pipe-line systems
    • A62C35/68—Details, e.g. of pipes or valve systems
    • A—HUMAN NECESSITIES
    • A62—LIFE-SAVING; FIRE-FIGHTING
    • A62C—FIRE-FIGHTING
    • A62C37/00—Control of fire-fighting equipment
    • A62C37/08—Control of fire-fighting equipment comprising an outlet device containing a sensor, or itself being the sensor, i.e. self-contained sprinklers
    • A62C37/10—Releasing means, e.g. electrically released
    • A62C37/11—Releasing means, e.g. electrically released heat-sensitive
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/15—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
    • C07C53/16—Halogenated acetic acids
    • C07C53/18—Halogenated acetic acids containing fluorine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D301/00—Preparation of oxiranes
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D301/00—Preparation of oxiranes
    • C07D301/02—Synthesis of the oxirane ring
    • C07D301/03—Synthesis of the oxirane ring by oxidation of unsaturated compounds, or of mixtures of unsaturated and saturated compounds
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/36—Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1075—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of amino acids or peptide residues
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14—Extraction; Separation; Purification
    • C07K1/30—Extraction; Separation; Purification by precipitation
    • C07K1/306—Extraction; Separation; Purification by precipitation by crystallization
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    • 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
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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    • C07—ORGANIC CHEMISTRY
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    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • A—HUMAN NECESSITIES
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    • A62—LIFE-SAVING; FIRE-FIGHTING
    • A62C—FIRE-FIGHTING
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    • A62C35/60—Pipe-line systems wet, i.e. containing extinguishing material even when not in use
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    • A62—LIFE-SAVING; FIRE-FIGHTING
    • A62C—FIRE-FIGHTING
    • A62C35/00—Permanently-installed equipment
    • A62C35/58—Pipe-line systems
    • A62C35/62—Pipe-line systems dry, i.e. empty of extinguishing material when not in use
    • A—HUMAN NECESSITIES
    • A62—LIFE-SAVING; FIRE-FIGHTING
    • A62C—FIRE-FIGHTING
    • A62C37/00—Control of fire-fighting equipment
    • A62C37/08—Control of fire-fighting equipment comprising an outlet device containing a sensor, or itself being the sensor, i.e. self-contained sprinklers
    • A62C37/10—Releasing means, e.g. electrically released
    • A62C37/11—Releasing means, e.g. electrically released heat-sensitive
    • A62C37/14—Releasing means, e.g. electrically released heat-sensitive with frangible vessels

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Abstract

Compuestos Cristalinos peptídicos de ceto epoxi, métodos para su preparacion y composiciones farmacéuticas relacionadas con la inclusion del proteosorne. También métodos para la preparacion de ceto-epoxidos de aminoácidos. Específicamente, las cetonas arílicas se convierten estereoselectivamente en los cetos epoxidos deseados. Reivindicacion 13: Un compuesto cristalino que tiene una estructura de Formula (1). Reivindicacion 48: Un compuesto cristalino que tiene una estructura de Formula (2) en el que X es trifluoroacetato. Reivindicacion 52: Un método para la preparacion de un compuesto cristalino de Formula (1), que comprende (i) preparar una solucion de un compuesto de Formula (3) en la que PG es un grupo protector adecuado, en un primer disolvente orgánico (ii) anadir un ácido adecuado; (iii) llevar la solucion a supersaturacion para provocar la formacion de cristales; y (iv) aislar los cristales para proporcionar un compuesto cristalino de cristalino de Formula (2) ; (v) hacer reaccionar un compuesto cristalino de la formula (2)en la que X es cualquier contraion adecuado, con un compuesto de Formula (4) en un segundo disolvente orgánico (vi) preparar una solucion de un compuesto de Formula (1) en el segundo disolvente orgánico; (vii) llevar la solucion a supersaturacion para provocar la formacion de cristales; y (viii) aislar los cristales para proporcionar un compuesto cristalino de Formula (1).
ARP080104358A 2007-10-04 2008-10-06 Inhibidores cristalinos peptidicos de epoxi cetona proteasa y la sintesis de ceto - epoxidos de aminoacidos AR068681A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US99761307P 2007-10-04 2007-10-04
US898707P 2007-12-20 2007-12-20

Publications (1)

Publication Number Publication Date
AR068681A1 true AR068681A1 (es) 2009-11-25

Family

ID=39941499

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080104358A AR068681A1 (es) 2007-10-04 2008-10-06 Inhibidores cristalinos peptidicos de epoxi cetona proteasa y la sintesis de ceto - epoxidos de aminoacidos

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Country Link
US (3) US8367617B2 (es)
EP (3) EP2612865A3 (es)
JP (2) JP5734656B2 (es)
KR (5) KR20150131405A (es)
CN (1) CN101883779B (es)
AR (1) AR068681A1 (es)
AU (1) AU2008307510A1 (es)
CA (1) CA2701778C (es)
CL (2) CL2008002966A1 (es)
CO (1) CO6270366A2 (es)
CR (1) CR11364A (es)
CY (1) CY1117710T1 (es)
DK (1) DK2207791T4 (es)
DO (1) DOP2010000095A (es)
EA (2) EA024437B1 (es)
EC (1) ECSP10010103A (es)
ES (2) ES2684340T3 (es)
HR (1) HRP20160808T4 (es)
HU (1) HUE029665T2 (es)
IL (5) IL204890A0 (es)
MA (1) MA31831B1 (es)
ME (1) ME02462B (es)
MX (1) MX2010003732A (es)
MY (2) MY173938A (es)
NZ (2) NZ584814A (es)
PH (1) PH12013501377A1 (es)
PL (1) PL2207791T5 (es)
PT (1) PT2207791T (es)
RS (1) RS54847B2 (es)
SA (1) SA08290624B1 (es)
SG (2) SG10201902704TA (es)
SI (1) SI2207791T2 (es)
TW (1) TWI501773B (es)
WO (1) WO2009045497A1 (es)
ZA (1) ZA201002770B (es)

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