TW202024091A - α-1 抗胰蛋白酶之調節劑 - Google Patents

α-1 抗胰蛋白酶之調節劑 Download PDF

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Publication number
TW202024091A
TW202024091A TW108136173A TW108136173A TW202024091A TW 202024091 A TW202024091 A TW 202024091A TW 108136173 A TW108136173 A TW 108136173A TW 108136173 A TW108136173 A TW 108136173A TW 202024091 A TW202024091 A TW 202024091A
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branched
linear
groups
cyclic
compound
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TW108136173A
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Chinese (zh)
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烏珀爾 基爾斯 班達瑞格
凱文 麥克肯翁 布萊
麥可 約翰 波伊德
黛安 Ｍ 保查爾
麥可 艾倫 布魯德尼
維洛尼克 德瑪格尼茲
法寧 雷夫 泰勒 德威
馬利 伊麗莎白 艾可斯
羅伯特 法蘭西斯 二世 費摩格納里
凱文 詹姆士 葛儂
巴倫特 沛德洛 Ｍ 葛西亞
賽門 吉羅克斯
羅納德 李 二世 葛雷
艾美 貝絲 荷爾
莎拉 卡洛 胡德
丹尼斯 詹姆士 赫里
喬許華 肯迪 赫西
麥克 阿瑟 二世 強森
彼得 瓊斯
薩拉希 凱薩凡
亞當 路克
布雷德 Ｄ 麥克斯威爾
約翰 派翠克 麥可斯威爾
亞歷斯 麥迪克
麥特奇特 納法莫爾
飛利 努漢特
賽圖 羅戴
史黛芬妮 洛普
魯帕 薩萬特
誼 施
莉貝卡 珍 史維特
唐青
提摩西 路易斯 塔普立
史蒂芬 Ａ 湯姆森
麥克 華道
金旺 徐
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美商維泰克斯製藥公司
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Publication of TW202024091A publication Critical patent/TW202024091A/zh

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • 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
    • 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
    • A61K31/495—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 or sparfloxacin
    • 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
    • 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
    • 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
    • C07D487/12—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
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • 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

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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)
TW108136173A 2018-10-05 2019-10-05 α-1 抗胰蛋白酶之調節劑 TW202024091A (zh)

Applications Claiming Priority (4)

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

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TW202024091A true TW202024091A (zh) 2020-07-01

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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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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
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GB201918414D0 (en) 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of Alpha1-Antitrypsin deficiency
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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
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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
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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
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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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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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AU2019362753A1 (en) 2021-05-20
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
CN113164761A (zh) 2021-07-23
CA3114672A1 (en) 2020-04-23
BR112021006392A2 (pt) 2021-07-06

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