AU2019362753A1 - Modulators of alpha-1 antitrypsin - Google Patents

Modulators of alpha-1 antitrypsin Download PDF

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Publication number
AU2019362753A1
AU2019362753A1 AU2019362753A AU2019362753A AU2019362753A1 AU 2019362753 A1 AU2019362753 A1 AU 2019362753A1 AU 2019362753 A AU2019362753 A AU 2019362753A AU 2019362753 A AU2019362753 A AU 2019362753A AU 2019362753 A1 AU2019362753 A1 AU 2019362753A1
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AU
Australia
Prior art keywords
branched
linear
groups
cyclic
chosen
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Abandoned
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AU2019362753A
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English (en)
Inventor
Upul Keerthi Bandarage
Cavan Mckeon Bligh
Diane M. BOUCHER
Michael John BOYD
Michael Aaron Brodney
Kevin Michael Cottrell
Veronique Damagnez
Lev Tyler Dewey Fanning
Mary Elizabeth ECCLES
Robert Francis FIMOGNARI Jr.
Kevin James GAGNON
Pedro M. GARCIA BARRANTES
Simon Giroux
Ronald Lee GREY Jr.
Amy Beth HALL
Sarah Carol HOOD
Dennis James Hurley
Joshua Kennedy HUSSEY
Mac Arthur Johnson Jr.
Peter Jones
Sarathy Kesavan
Adam Looker
Brad D. MAXWELL
John Patrick Maxwell
Ales Medek
Mettachit Navamal
Philippe Marcel Nuhant
Setu Roday
Stefanie Roeper
Rupa SAWANT
Yi Shi
Rebecca Jane Swett
Qing Tang
Timothy Lewis TAPLEY
Stephen A. Thomson
Michael Waldo
Jinwang Xu
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Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals 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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of AU2019362753A1 publication Critical patent/AU2019362753A1/en
Abandoned legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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
    • C07D487/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
AU2019362753A 2018-10-05 2019-10-04 Modulators of alpha-1 antitrypsin Abandoned AU2019362753A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862742148P 2018-10-05 2018-10-05
US62/742,148 2018-10-05
US201862768662P 2018-11-16 2018-11-16
US62/768,662 2018-11-16
PCT/US2019/054681 WO2020081257A1 (en) 2018-10-05 2019-10-04 Modulators of alpha-1 antitrypsin

Publications (1)

Publication Number Publication Date
AU2019362753A1 true AU2019362753A1 (en) 2021-05-20

Family

ID=69467663

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2019362753A Abandoned AU2019362753A1 (en) 2018-10-05 2019-10-04 Modulators of alpha-1 antitrypsin

Country Status (16)

Country Link
US (2) US11623924B2 (https=)
EP (1) EP3860712A1 (https=)
JP (1) JP2022512588A (https=)
KR (1) KR20210089656A (https=)
CN (1) CN113164761A (https=)
AU (1) AU2019362753A1 (https=)
BR (1) BR112021006392A2 (https=)
CA (1) CA3114672A1 (https=)
CO (1) CO2021005884A2 (https=)
IL (1) IL281884A (https=)
JO (1) JOP20210060A1 (https=)
MA (1) MA53827A (https=)
MX (1) MX2021003819A (https=)
TW (1) TW202024091A (https=)
UY (1) UY38403A (https=)
WO (1) WO2020081257A1 (https=)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3114672A1 (en) 2018-10-05 2020-04-23 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin
GB201820450D0 (en) 2018-12-14 2019-01-30 Z Factor Ltd Compound and its use for the treatment of alpha1-antitryspin deficiency
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
GB201918404D0 (en) 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of aplha1-antitrypsin deficiency
GB201918410D0 (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
GB201918413D0 (en) 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of alpha1-antitrypsin deficiency
CN115776984A (zh) * 2020-04-03 2023-03-10 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吡咯并[2,3-f]吲唑和2,4,5,10-四氮杂三环[7.3.0.03,7]十二碳-1,3(7),5,8,11-五烯衍生物
WO2021203025A1 (en) * 2020-04-03 2021-10-07 Vertex Pharmaceuticals Incorporated 1 h-pyrazolo[4,3-g]isoquinoline and 1 h-pyrazolo[4,3-g]quinoline derivatives as alpha-1 -antitrypsin modulators for treating alpha-1 -antitrypsin deficiency (aatd)
JP7732999B2 (ja) 2020-04-03 2025-09-02 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
GB202009074D0 (en) 2020-06-15 2020-07-29 Z Factor Ltd Compound
WO2022026372A2 (en) 2020-07-27 2022-02-03 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
CN116813623A (zh) * 2022-03-21 2023-09-29 东南大学 一种吡咯并[2,3-f]吲唑类化合物的制备方法
CN114605385B (zh) * 2022-03-25 2023-09-08 河南大学 吲哚哌啶脲类trpv1拮抗/faah抑制双靶点药物及制备方法和应用
WO2025090827A1 (en) 2023-10-27 2025-05-01 Sub21, Inc. A1at modulators
WO2026014456A1 (ja) * 2024-07-10 2026-01-15 株式会社アークメディスン 化合物、補体d因子阻害剤、及び医薬組成物

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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
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CN115697969A (zh) 2020-04-03 2023-02-03 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7-或8-羟基-异喹啉和7-或8-羟基-喹啉衍生物
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CN115776984A (zh) 2020-04-03 2023-03-10 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吡咯并[2,3-f]吲唑和2,4,5,10-四氮杂三环[7.3.0.03,7]十二碳-1,3(7),5,8,11-五烯衍生物
WO2021203025A1 (en) 2020-04-03 2021-10-07 Vertex Pharmaceuticals Incorporated 1 h-pyrazolo[4,3-g]isoquinoline and 1 h-pyrazolo[4,3-g]quinoline derivatives as alpha-1 -antitrypsin modulators for treating alpha-1 -antitrypsin deficiency (aatd)
JP7732999B2 (ja) 2020-04-03 2025-09-02 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
WO2022026372A2 (en) 2020-07-27 2022-02-03 Vertex Pharmaceuticals Incorporated Processes for preparing modulators of alpha-1 antitrypsin

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Publication number Publication date
MX2021003819A (es) 2021-06-23
KR20210089656A (ko) 2021-07-16
JP2022512588A (ja) 2022-02-07
EP3860712A1 (en) 2021-08-11
CO2021005884A2 (es) 2021-05-20
US20230265080A1 (en) 2023-08-24
US20210179587A1 (en) 2021-06-17
US11623924B2 (en) 2023-04-11
JOP20210060A1 (ar) 2023-01-30
UY38403A (es) 2020-04-30
IL281884A (en) 2021-05-31
WO2020081257A1 (en) 2020-04-23
MA53827A (fr) 2021-09-15
TW202024091A (zh) 2020-07-01
CN113164761A (zh) 2021-07-23
CA3114672A1 (en) 2020-04-23
BR112021006392A2 (pt) 2021-07-06

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