BR112023005853A2 - Processo para preparar um composto de fórmula i, compostos, processos para preparar o composto 1, forma cristalina, composição farmacêutica, processo de preparação da forma cristalina do composto i e método para tratar uma condição neurodegenerativa - Google Patents

Processo para preparar um composto de fórmula i, compostos, processos para preparar o composto 1, forma cristalina, composição farmacêutica, processo de preparação da forma cristalina do composto i e método para tratar uma condição neurodegenerativa

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Publication number
BR112023005853A2
BR112023005853A2 BR112023005853A BR112023005853A BR112023005853A2 BR 112023005853 A2 BR112023005853 A2 BR 112023005853A2 BR 112023005853 A BR112023005853 A BR 112023005853A BR 112023005853 A BR112023005853 A BR 112023005853A BR 112023005853 A2 BR112023005853 A2 BR 112023005853A2
Authority
BR
Brazil
Prior art keywords
preparing
compound
crystalline form
processes
compounds
Prior art date
Application number
BR112023005853A
Other languages
English (en)
Inventor
Hoffmann-Emery Fabienne
Konrath Manuel
Lautz Christian
Monika Niedermann Katrin
Jonathan Orcel Ugo
Elizabeth Carrera Diane
Original Assignee
Genentech Inc
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 Genentech Inc, Hoffmann La Roche filed Critical Genentech Inc
Publication of BR112023005853A2 publication Critical patent/BR112023005853A2/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • 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
    • A61K31/537—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 spiro-condensed or forming part of bridged ring systems
    • 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
    • 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
    • C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • 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
    • C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—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 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/38—One sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Abstract

PROCESSO PARA PREPARAR UM COMPOSTO DE FÓRMULA I, COMPOSTOS, PROCESSOS PARA PREPARAR O COMPOSTO 1, FORMA CRISTALINA, COMPOSIÇÃO FARMACÊUTICA, PROCESSO DE PREPARAÇÃO DA FORMA CRISTALINA DO COMPOSTO I E MÉTODO PARA TRATAR UMA CONDIÇÃO NEURODEGENERATIVA. São fornecidos processos para a preparação de compostos bi-heteroarila, incluindo o composto bi-heteroarila 3-(difluorometóxi)-5-[2-(3,3-difluoropirrolidin-1-il)-6-[(1S,4S)-2-oxa-5- azabiciclo[2.2.1]heptan-5-il]pirimidin-4-il]piridin-2-amina. Entre outras vantagens, os processos proporcionam: o uso de solventes relativamente atóxicos e de baixo custo; uso reduzido de catalisadores de metais preciosos caros; redução da temperatura de reação em determinadas etapas; o uso de agentes de oxidação relativamente não tóxicos; o uso de catalisadores baratos de metais de transição; uma redução das razões molares de certos reactantes, melhorando assim a eficiência do processo enquanto reduz o custo e o desperdício; concentrações de reactante significativamente mais altas em certas etapas; eliminação da necessidade de múltiplas etapas de purificação cromatográfica; eliminação da necessidade de certas etapas de extração usando solvente orgânico; e proporcionar maior rendimento e pureza melhorada.
BR112023005853A 2020-10-02 2021-09-30 Processo para preparar um composto de fórmula i, compostos, processos para preparar o composto 1, forma cristalina, composição farmacêutica, processo de preparação da forma cristalina do composto i e método para tratar uma condição neurodegenerativa BR112023005853A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202063087109P 2020-10-02 2020-10-02
PCT/US2021/053005 WO2022072721A1 (en) 2020-10-02 2021-09-30 Process for the preparation of biheteroaryl compounds and crystal forms thereof

Publications (1)

Publication Number Publication Date
BR112023005853A2 true BR112023005853A2 (pt) 2023-05-02

Family

ID=78599176

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112023005853A BR112023005853A2 (pt) 2020-10-02 2021-09-30 Processo para preparar um composto de fórmula i, compostos, processos para preparar o composto 1, forma cristalina, composição farmacêutica, processo de preparação da forma cristalina do composto i e método para tratar uma condição neurodegenerativa

Country Status (14)

Country Link
US (1) US20230312473A1 (pt)
EP (1) EP4222154A1 (pt)
JP (1) JP2023544037A (pt)
KR (1) KR20230079123A (pt)
CN (1) CN116744933A (pt)
AU (1) AU2021353532A1 (pt)
BR (1) BR112023005853A2 (pt)
CA (1) CA3200566A1 (pt)
CL (1) CL2023000945A1 (pt)
CR (1) CR20230183A (pt)
IL (1) IL301266A (pt)
MX (1) MX2023003759A (pt)
PE (1) PE20230781A1 (pt)
WO (1) WO2022072721A1 (pt)

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US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
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US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
HUT35524A (en) 1983-08-02 1985-07-29 Hoechst Ag Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance
US5004697A (en) 1987-08-17 1991-04-02 Univ. Of Ca Cationized antibodies for delivery through the blood-brain barrier
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ATE191853T1 (de) 1992-07-27 2000-05-15 Us Health Zielgerichte liposome zur blut-hirne schranke
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DE10121982B4 (de) 2001-05-05 2008-01-24 Lts Lohmann Therapie-Systeme Ag Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung
DE60234057D1 (de) 2001-07-25 2009-11-26 Raptor Pharmaceutical Inc Zusammensetzungen und verfahren zur modulation des transports durch die blut-hirn-schranke
US20030162695A1 (en) 2002-02-27 2003-08-28 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
KR101186210B1 (ko) 2002-12-03 2012-10-08 블랜체트 록펠러 뉴로사이언시즈 인스티튜트 혈뇌장벽을 통과하는 물질 수송용 인공 저밀도 지단백질 운반체
EP1663239A4 (en) 2003-09-10 2008-07-23 Cedars Sinai Medical Center KALIUM CHANNEL-MEDIATED FEEDING OF MEDICINES BY THE BLOOD BRAIN BARRIER
MX2012004638A (es) 2009-10-22 2012-07-04 Genentech Inc Modulacion de degeneracion de axones.
EP2991978A4 (en) * 2013-05-01 2016-09-14 Hoffmann La Roche BIHETEROARYL COMPOUNDS AND USES THEREOF

Also Published As

Publication number Publication date
KR20230079123A (ko) 2023-06-05
CA3200566A1 (en) 2022-04-07
CN116744933A (zh) 2023-09-12
MX2023003759A (es) 2023-04-24
US20230312473A1 (en) 2023-10-05
AU2021353532A8 (en) 2023-05-04
EP4222154A1 (en) 2023-08-09
WO2022072721A1 (en) 2022-04-07
IL301266A (en) 2023-05-01
CR20230183A (es) 2023-06-14
PE20230781A1 (es) 2023-05-09
AU2021353532A1 (en) 2023-04-13
JP2023544037A (ja) 2023-10-19
CL2023000945A1 (es) 2023-09-29

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