SG11202112414UA - Condensed tricyclic pyrroles as alpha-1 antitrypsin modulators - Google Patents

Condensed tricyclic pyrroles as alpha-1 antitrypsin modulators

Info

Publication number
SG11202112414UA
SG11202112414UA SG11202112414UA SG11202112414UA SG11202112414UA SG 11202112414U A SG11202112414U A SG 11202112414UA SG 11202112414U A SG11202112414U A SG 11202112414UA SG 11202112414U A SG11202112414U A SG 11202112414UA SG 11202112414U A SG11202112414U A SG 11202112414UA
Authority
SG
Singapore
Prior art keywords
alpha
condensed tricyclic
antitrypsin
modulators
tricyclic pyrroles
Prior art date
Application number
SG11202112414UA
Other languages
English (en)
Inventor
Upul Keerthi Bandarage
Cavan Mckeon Bligh
Diane Boucher
Michael John Boyd
Michael Aaron Brodney
Michael Philip Clark
Veronique Damagnez
Lev Tyler Dewey Fanning
Robert Francis Fimognari
Gabrielle Simone Fleming
Kevin James Gagnon
Barrantes Pedro Manuel Garcia
Robert Daniel Giacometti
Simon Giroux
Jr Ronald Lee Grey
Samantha Guido
Amy Beth Hall
Sarah Carol Hood
Dennis James Hurley
Johnson, Jr
Peter Jones
Sarathy Kesavan
Mei-Hsiu Lai
Siying Liu
Adam Looker
Brad Maxwell
John Patrick Maxwell
Ales Medek
Philippe Marcel Nuhant
Kirk Alan Overhoff
Setu Roday
Stefanie Roeper
Steven M Ronkin
Rupa Sawant
Yi Shi
Muna Shrestha
Marisa Sposato
Kathy Stavropoulos
Rebecca Jane Swett
Qing Tang
Timothy Lewis Tapley
Stephen Thomson
Jinwang Xu
Mariam Zaky
Kevin Michael Cottrell
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 SG11202112414UA publication Critical patent/SG11202112414UA/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • 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
    • 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
    • A61K31/41—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
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring 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
    • A61K31/41—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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41—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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/41—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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/41—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
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring 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
    • A61K31/41—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
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • 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
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/14—Ortho-condensed systems
    • 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
    • C07D491/12—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 three hetero rings
    • C07D491/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C07H13/08—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Pyrrole Compounds (AREA)
SG11202112414UA 2019-05-14 2020-05-14 Condensed tricyclic pyrroles as alpha-1 antitrypsin modulators SG11202112414UA (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962847562P 2019-05-14 2019-05-14
US202063004813P 2020-04-03 2020-04-03
PCT/US2020/032832 WO2020247160A1 (en) 2019-05-14 2020-05-14 Condensed tryciclic pyrroles as alpha-1 antitrypsin modulators

Publications (1)

Publication Number Publication Date
SG11202112414UA true SG11202112414UA (en) 2021-12-30

Family

ID=72644864

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11202112414UA SG11202112414UA (en) 2019-05-14 2020-05-14 Condensed tricyclic pyrroles as alpha-1 antitrypsin modulators

Country Status (22)

Country Link
US (1) US11884672B2 (es)
EP (1) EP3969440A1 (es)
JP (1) JP2022532340A (es)
KR (1) KR20220023987A (es)
CN (1) CN114096542A (es)
AU (1) AU2020286424A1 (es)
BR (1) BR112021022832A2 (es)
CA (1) CA3140039A1 (es)
CL (1) CL2021002964A1 (es)
CO (1) CO2021016594A2 (es)
CR (1) CR20210608A (es)
DO (1) DOP2021000234A (es)
EC (1) ECSP21085481A (es)
IL (1) IL287878A (es)
JO (1) JOP20210301A1 (es)
MA (1) MA55971A (es)
MX (1) MX2021013993A (es)
PE (1) PE20220905A1 (es)
SG (1) SG11202112414UA (es)
TW (1) TW202108588A (es)
UY (1) UY38696A (es)
WO (1) WO2020247160A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2021003819A (es) 2018-10-05 2021-06-23 Vertex Pharma Moduladores de alfa-1 antitripsina.
US11884672B2 (en) 2019-05-14 2024-01-30 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin
GB201918413D0 (en) 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of alpha1-antitrypsin deficiency
GB201918416D0 (en) 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of Alpha1-Antitrypsin deficiency
GB201918414D0 (en) 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of Alpha1-Antitrypsin deficiency
GB201918410D0 (en) 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of alpha1-antitrypsin deficiency
GB201918404D0 (en) 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of aplha1-antitrypsin deficiency
WO2021155087A1 (en) * 2020-01-30 2021-08-05 Vertex Pharmaceuticals Incorporated Methods of treatment for alpha-1 antitrypsin deficiency
IL296750A (en) * 2020-04-03 2022-11-01 Vertex Pharma Pyrrolo[2,3-f]indazole and 2,4,5,10-tetrazatricyclo[7.3.0.03.7]dodeca-1,3(7),5,8,11-pentane derivatives as alpha-1 modulators -antitrypsin for the treatment of alpha-1-antitrypsin deficiency (aatd)
AU2021318940A1 (en) 2020-07-27 2023-03-16 Vertex Pharmaceuticals Incorporated Processes for preparing modulators of alpha-1 antitrypsin
WO2022104353A1 (en) 2020-11-12 2022-05-19 Vertex Pharmaceuticals Incorporated Methods of monitoring alpha-1 antitrypsin (aat) deficiency by measuring polymerised aat
AU2021381509A1 (en) 2020-11-17 2023-06-22 Vertex Pharmaceuticals Incorporated Solid forms of 4-(5-(4-fluorophenyl)-6-tetrahydro-2h-pyran-4-yl)- 1,5-dihydropyrrolo[2,3-f]indazol-7-yl)benzoic acid
GB202108523D0 (en) 2021-06-15 2021-07-28 Z Factor Ltd Compositions and their use for the treatment of alpha1-antitrypsin deficiency
WO2024054624A1 (en) 2022-09-09 2024-03-14 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK158590D0 (da) 1990-07-02 1990-07-02 Lundbeck & Co As H Indolderivater
US20020017295A1 (en) 2000-07-07 2002-02-14 Weers Jeffry G. Phospholipid-based powders for inhalation
JP2000072751A (ja) 1998-08-26 2000-03-07 Tanabe Seiyaku Co Ltd イソキノリノン誘導体
JP2000281654A (ja) 1999-03-26 2000-10-10 Tanabe Seiyaku Co Ltd イソキノリン誘導体
GB9913083D0 (en) 1999-06-04 1999-08-04 Novartis Ag Organic compounds
FR2802532A1 (fr) 1999-12-17 2001-06-22 Sanofi Synthelabo Derives de 2-phenyl-quinoleine, leur preparation et leur application en therapeutique
US6638929B2 (en) 1999-12-29 2003-10-28 Wyeth Tricyclic protein kinase inhibitors
CZ2003243A3 (cs) 2000-07-26 2003-09-17 Smithkline Beecham P. L. C. Aminopiperidinové chinoliny a jejich azaisosterické analogy s antibakteriální aktivitou
US6777400B2 (en) 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
WO2002094790A1 (fr) 2001-05-23 2002-11-28 Mitsubishi Pharma Corporation Compose heterocyclique condense et son utilisation medicale
CA2672549A1 (en) 2001-11-14 2003-06-12 Ben-Zion Dolitzky Amorphous and crystalline forms of losartan potassium and process for their preparation
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
DE102008022521A1 (de) * 2008-05-07 2009-11-12 Bayer Schering Pharma Aktiengesellschaft 1,4-Diaryl-pyrimidopyridazin-2,5-dione und ihre Verwendung
WO2011056222A1 (en) 2009-11-05 2011-05-12 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Methods of treating disorders associated with protein aggregation
WO2011110852A1 (en) 2010-03-10 2011-09-15 Astrazeneca Ab Polymorphic forms of 6- [2- (4 -cyanophenyl) - 2h - pyrazol - 3 - yl] - 5 -methyl - 3 - oxo - 4 - (trifluoromethyl - phenyl) 3,4-dihydropyrazine-2-carboxylic acid ethylamide
RU2711481C2 (ru) 2010-03-25 2020-01-17 Вертекс Фармасьютикалз Инкорпорейтед ТВЕРДЫЕ ФОРМЫ (R)-1-(2, 2-ДИФТОРБЕНЗО[d][1, 3]ДИОКСОЛ-5-ИЛ)-N-(1-(2, 3-ДИГИДРОКСИПРОПИЛ)-6-ФТОР-2-(1-ГИДРОКСИ-2-МЕТИЛПРОПАН-2-ИЛ)-1H-ИНДОЛ-5-ИЛ)ЦИКЛОПРОПАНКАРБОКСАМИДА
HUE025584T2 (en) 2010-09-24 2016-04-28 Grifols Therapeutics Inc Immunochromatographic instruments, procedures and kits
US9572794B2 (en) 2014-08-06 2017-02-21 Vanderbilt University Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists
WO2016154051A1 (en) 2015-03-20 2016-09-29 University Of Florida Research Foundation, Inc. Combination therapy for treating infections diseases
ES2910787T3 (es) 2016-05-12 2022-05-13 Univ Michigan Regents Inhibidores de ASH1L y métodos de tratamiento con los mismos
JOP20180008A1 (ar) * 2017-02-02 2019-01-30 Gilead Sciences Inc مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b
JP2020537669A (ja) 2017-10-19 2020-12-24 江▲蘇▼豪森▲薬▼▲業▼集▲団▼有限公司 ピラゾリル基を含む三環式誘導体、その製造方法及び用途
EP3704113B1 (en) 2017-11-01 2023-10-11 Bristol-Myers Squibb Company Bridged bicyclic compounds as farnesoid x receptor modulators
CN107698505A (zh) 2017-11-20 2018-02-16 孙婷婷 一种诺得司他的制备方法
PE20211444A1 (es) 2017-12-13 2021-08-05 Lupin Ltd Componentes heterociclicos biciclicos sustituidos como inhibidores de prmt5
CA3088766A1 (en) 2018-01-31 2019-08-08 Merck Patent Gmbh Quinoline compounds as irak inhibitors and uses thereof
MX2020013853A (es) 2018-06-22 2021-05-27 Ucl Business Ltd Compuestos innovadores.
CA3108388A1 (en) 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
MX2021003819A (es) 2018-10-05 2021-06-23 Vertex Pharma Moduladores de alfa-1 antitripsina.
CN110776459B (zh) 2019-03-19 2023-01-24 江苏知原药业股份有限公司 7-羟基-2-喹诺酮-二硫代氨基甲酸酯类胆碱酯酶抑制剂
US11884672B2 (en) 2019-05-14 2024-01-30 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin
TW202116303A (zh) 2019-10-02 2021-05-01 美商維泰克斯製藥公司 α—１抗胰蛋白酶缺乏症之治療方法
WO2021155087A1 (en) 2020-01-30 2021-08-05 Vertex Pharmaceuticals Incorporated Methods of treatment for alpha-1 antitrypsin deficiency
WO2021203028A1 (en) 2020-04-03 2021-10-07 Vertex Pharmaceuticals Incorporated 7- or 8-hydroxy-isoquinoline and 7- or 8-hydroxy-quinoline derivatives as alpha-1 -antitrypsin modulators for treating alpha-1 -antitrypsin deficiency (aatd)
JP2023520396A (ja) 2020-04-03 2023-05-17 バーテックス ファーマシューティカルズ インコーポレイテッド アルファ１－アンチトリプシンのモジュレーター
CN115715292A (zh) 2020-04-03 2023-02-24 弗特克斯药品有限公司 作为用于治疗α-1-抗胰蛋白酶缺乏症(AATD)的α-1-抗胰蛋白酶调节剂的1H-吡唑并[4,3-g]异喹啉和1H-吡唑并[4,3-g]喹啉衍生物
IL296750A (en) 2020-04-03 2022-11-01 Vertex Pharma Pyrrolo[2,3-f]indazole and 2,4,5,10-tetrazatricyclo[7.3.0.03.7]dodeca-1,3(7),5,8,11-pentane derivatives as alpha-1 modulators -antitrypsin for the treatment of alpha-1-antitrypsin deficiency (aatd)
EP4132908A1 (en) 2020-04-03 2023-02-15 Vertex Pharmaceuticals Incorporated Indole derivatives as alpha-1 -antitrypsin modulators for treating alpha-1 -antitrypsin deficiency (aatd)
WO2022104353A1 (en) 2020-11-12 2022-05-19 Vertex Pharmaceuticals Incorporated Methods of monitoring alpha-1 antitrypsin (aat) deficiency by measuring polymerised aat
AU2021381509A1 (en) 2020-11-17 2023-06-22 Vertex Pharmaceuticals Incorporated Solid forms of 4-(5-(4-fluorophenyl)-6-tetrahydro-2h-pyran-4-yl)- 1,5-dihydropyrrolo[2,3-f]indazol-7-yl)benzoic acid

Also Published As

Publication number Publication date
WO2020247160A1 (en) 2020-12-10
ECSP21085481A (es) 2022-01-31
US11884672B2 (en) 2024-01-30
JOP20210301A1 (ar) 2023-01-30
AU2020286424A1 (en) 2022-01-06
CR20210608A (es) 2022-02-11
DOP2021000234A (es) 2022-03-15
TW202108588A (zh) 2021-03-01
CO2021016594A2 (es) 2022-04-29
JP2022532340A (ja) 2022-07-14
US20200361939A1 (en) 2020-11-19
MX2021013993A (es) 2021-12-10
CA3140039A1 (en) 2020-12-10
BR112021022832A2 (pt) 2022-01-18
MA55971A (fr) 2022-03-23
KR20220023987A (ko) 2022-03-03
UY38696A (es) 2020-11-30
CN114096542A (zh) 2022-02-25
EP3969440A1 (en) 2022-03-23
PE20220905A1 (es) 2022-05-30
CL2021002964A1 (es) 2022-08-05
IL287878A (en) 2022-01-01

Similar Documents

Publication Publication Date Title
IL287878A (en) Concentrated tricyclic pyrroles as alpha-1 antitrypsin modulators
ZA202207722B (en) Substituted tricyclic compounds
ZA202206253B (en) Substituted tricyclic compounds
ZA202106192B (en) Fused tricyclic compounds useful as anticancer agents
EP3510999A4 (en) PREVENTION OR REMEDY COMPOSITION AGAINST DEMENTIA OR DEPRESSION
EP3588499A4 (en) PHOTOPOLYMER COMPOSITION
EP3867219A4 (en) POLYCYCLIC COMPOUNDS
EP3508190A4 (en) PHOTOSETTING COMPOSITION
EP3656821A4 (en) ASPHALT COMPOSITION
EP3514627A4 (en) PHOTO POLYMER COMPOSITION
IL286902A (en) Pyrrole compounds
ZA202303688B (en) Substituted tricyclic compounds
EP3595691A4 (en) PLANT-BASED COMPOSITION
EP3543260A4 (en) PHOTO POLYMER COMPOSITION
ZA202100237B (en) Tricyclic compounds
EP3978501A4 (en) TETRACYCLIC COMPOUNDS AS CDC7 INHIBITORS
EP3898839A4 (en) MODIFIED ASPHALT COMPOSITION
EP3641756A4 (en) TRICYCLIC COMPOUNDS AS CYP1 INHIBITORS
IL287813A (en) tricyclic compounds
EP4005833A4 (en) TIRE COMPOSITION
EP3880190A4 (en) ANTICANCER COMPOSITION
EP3953615A4 (en) SHIFT LOCK GUARD
EP3640296A4 (en) NEUTRAL LAYER COMPOSITION
EP3640298A4 (en) NEUTRAL LAYER COMPOSITION
EP3773577A4 (en) TRICYCLIC ASK1 INHIBITORS