CN113164761A - α-1抗胰蛋白酶的调节剂 - Google Patents

α-1抗胰蛋白酶的调节剂 Download PDF

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Publication number
CN113164761A
CN113164761A CN201980078980.8A CN201980078980A CN113164761A CN 113164761 A CN113164761 A CN 113164761A CN 201980078980 A CN201980078980 A CN 201980078980A CN 113164761 A CN113164761 A CN 113164761A
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branched
linear
cyclic
group
compound
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CN201980078980.8A
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Chinese (zh)
Inventor
C·M·布利
M·A·布罗尼
M·E·埃克莱斯
K·J·加农
S·C·胡德
J·K·赫西
A·卢克
J·P·梅克西维尔
A·梅德克
M·纳瓦马尔
S·罗代
S·雷珀
R·萨万特
Y·施
Q·唐
M·瓦尔多
U·K·班达拉奇
D·M·布彻尔
M·J·博伊德
V·达马内斯
L·T·德维芬宁
R·F·小菲莫纳里
P·M·加西亚巴兰特斯
S·吉鲁
R·L·小格雷
A·B·霍尔
D·J·赫利
M·A·小约翰逊
P·琼斯
S·克萨文
P·M·努汉特
R·J·斯维特
T·L·塔普利
S·A·汤普森
J·徐
B·D·梅克西维尔
K·M·科特雷尔
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication of CN113164761A publication Critical patent/CN113164761A/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)
CN201980078980.8A 2018-10-05 2019-10-04 α-1抗胰蛋白酶的调节剂 Pending CN113164761A (zh)

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
CN113164761A true CN113164761A (zh) 2021-07-23

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CN201980078980.8A Pending CN113164761A (zh) 2018-10-05 2019-10-04 α-1抗胰蛋白酶的调节剂

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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=)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114096542A (zh) * 2019-05-14 2022-02-25 弗特克斯药品有限公司 作为α-1抗胰蛋白酶调节剂的缩合三环吡咯
CN114605385A (zh) * 2022-03-25 2022-06-10 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
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
US12502376B2 (en) 2020-04-03 2025-12-23 Vertex Pharmaceuticals Incorporated Pyrano[4,3-b]indole derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (AATD)

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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
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)
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
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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AU2021246104A1 (en) 2020-04-03 2022-10-20 Vertex Pharmaceuticals Incorporated Modulators of alpha-1 antitrypsin
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
IL296920A (en) 2020-04-03 2022-12-01 Vertex Pharma Indole derivatives as alpha-1-antitrypsin modulators for the treatment of alpha-1-antitrypsin deficiency (aatd)
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

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114096542A (zh) * 2019-05-14 2022-02-25 弗特克斯药品有限公司 作为α-1抗胰蛋白酶调节剂的缩合三环吡咯
CN114096542B (zh) * 2019-05-14 2024-09-10 弗特克斯药品有限公司 作为α-1抗胰蛋白酶调节剂的缩合三环吡咯
US12502376B2 (en) 2020-04-03 2025-12-23 Vertex Pharmaceuticals Incorporated Pyrano[4,3-b]indole derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (AATD)
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
CN114605385A (zh) * 2022-03-25 2022-06-10 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
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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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
CA3114672A1 (en) 2020-04-23
BR112021006392A2 (pt) 2021-07-06

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