JOP20210301A1 - بيرولات ثلاثية الحلقة مكثفة كمُعدِّلات مضاد تريبسين ألفا-1 - Google Patents

بيرولات ثلاثية الحلقة مكثفة كمُعدِّلات مضاد تريبسين ألفا-1

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Publication number
JOP20210301A1
JOP20210301A1 JOP/2021/0301A JOP20210301A JOP20210301A1 JO P20210301 A1 JOP20210301 A1 JO P20210301A1 JO P20210301 A JOP20210301 A JO P20210301A JO P20210301 A1 JOP20210301 A1 JO P20210301A1
Authority
JO
Jordan
Prior art keywords
alpha
tryciclic
pyrroles
condensed
compounds
Prior art date
Application number
JOP/2021/0301A
Other languages
English (en)
Inventor
Yi Shi
Timothy Lewis Tapley
Rebecca Jane Swett
Jinwang Xu
John Patrick Maxwell
Muna Shrestha
Kirk Alan Overhoff
Upul Keerthi Bandarage
Michael Aaron Brodney
Cavan Mckeon Bligh
Diane Boucher
Michael John Boyd
Qing Tang
Stephen Thomson
Kevin James Gagnon
Jr Ronald Lee Grey
Peter Jones
Jr Mac Arthur Johnson
Samantha Guido
Robert Daniel Giacometti
Simon Giroux
Veronique Damagnez
Setu Roday
Steven M Ronkin
Stefanie Roeper
Mariam Zaky
Rupa Sawant
Marisa Sposato
Kathy Stavropoulos
Barrantes Pedro Manuel Garcia
Lev Tyler Dewey Fanning
Gabrielle Simone Fleming
Robert Francis Fimognari
Michael Philip Clark
Kevin Michael Cottrell
Sarathy Kesavan
Mei-Hsiu Lai
Adam Looker
Siying Liu
Brad Maxwell
Ales Medek
Philippe Marcel Nuhant
Sarah Carol Hood
Amy Beth Hall
Dennis James Hurley
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of JOP20210301A1 publication Critical patent/JOP20210301A1/ar

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    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
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    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/23—Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups C07H19/14 - C07H19/22
    • 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
    • C07B2200/07—Optical isomers
    • 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

يوفر الكشف الحالي مركبات مُفيدة لعلاج نقص مضاد تريبسين ألفا-1 (AATD)، وفقًا للصيغة (I): (I)، ومماثلات كيميائية منها، وأملاح مقبولة صيدليًا من المركبات، وأملاح مقبولة صيدليًا من المماثلات الكيميائية، ومشتقات مُعالجة بالديوتريوم من المركبات، ومشتقات معالجة بالديوتريوم من المماثلات الكيميائية، ومشتقات مُعالجة بالديوتريوم من الأملاح، والصور الصلبة من تلك المركبات وعمليات تحضير تلك المركبات.
JOP/2021/0301A 2019-05-14 2020-05-14 بيرولات ثلاثية الحلقة مكثفة كمُعدِّلات مضاد تريبسين ألفا-1 JOP20210301A1 (ar)

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