CN115003659B - 用于治疗由cftr活性缺乏介导的疾患的5元杂芳基氨基磺酰胺 - Google Patents

用于治疗由cftr活性缺乏介导的疾患的5元杂芳基氨基磺酰胺

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Publication number
CN115003659B
CN115003659B CN202080092755.2A CN202080092755A CN115003659B CN 115003659 B CN115003659 B CN 115003659B CN 202080092755 A CN202080092755 A CN 202080092755A CN 115003659 B CN115003659 B CN 115003659B
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compound
alkyl
substituted
mmol
cycloalkyl
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Chinese (zh)
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CN115003659A (zh
Inventor
J·廖
M·蒙森
Z·高
G·赫尔巴特
S·巴尔策尔
B·魏伟特
B·弗里德
H·P·内斯特勒
H·耶奥曼
I·马琴
M·斯姆尔奇纳
N·马
S·莱布雷顿
R·哈通
W·维尔
S·图赖拉特纳姆
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Genzyme Corp
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Genzyme Corp
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    • 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
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/427—Thiazoles 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
    • A61K31/435—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
    • A61K31/535—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/50—Nitrogen atoms bound to hetero atoms
    • C07D277/52—Nitrogen atoms bound to hetero atoms to sulfur atoms, e.g. sulfonamides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • C07D498/02—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 two hetero rings
    • C07D498/10—Spiro-condensed systems
    • 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 Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/22—Amides of acids of phosphorus
    • C07F9/222—Amides of phosphoric acids
    • 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 Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6536—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539—Five-membered rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Saccharide Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN202080092755.2A 2019-11-12 2020-11-12 用于治疗由cftr活性缺乏介导的疾患的5元杂芳基氨基磺酰胺 Active CN115003659B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962934293P 2019-11-12 2019-11-12
US62/934293 2019-11-12
PCT/US2020/060180 WO2021097057A1 (en) 2019-11-12 2020-11-12 5-membered heteroarylaminosulfonamides for treating conditions mediated by deficient cftr activity

Publications (2)

Publication Number Publication Date
CN115003659A CN115003659A (zh) 2022-09-02
CN115003659B true CN115003659B (zh) 2026-04-21

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Country Status (17)

Country Link
US (1) US20240002374A1 (https=)
EP (1) EP4058439A1 (https=)
JP (2) JP7721517B2 (https=)
KR (1) KR20220115829A (https=)
CN (1) CN115003659B (https=)
AU (1) AU2020384279A1 (https=)
BR (1) BR112022009185A2 (https=)
CA (1) CA3158057A1 (https=)
CL (1) CL2022001245A1 (https=)
CO (1) CO2022007953A2 (https=)
EC (1) ECSP22046050A (https=)
IL (1) IL292966A (https=)
JO (1) JOP20220105A1 (https=)
MX (1) MX2022005809A (https=)
PE (1) PE20221461A1 (https=)
PH (1) PH12022551139A1 (https=)
WO (1) WO2021097057A1 (https=)

Families Citing this family (14)

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Publication number Priority date Publication date Assignee Title
AU2019222758B2 (en) 2018-02-15 2022-07-07 Vertex Pharmaceuticals Incorporated Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cystic fibrosis, and process for making them
TWI848092B (zh) 2019-04-03 2024-07-11 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白調節劑
TWI867024B (zh) 2019-08-14 2024-12-21 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白之調節劑
CA3150162A1 (en) 2019-08-14 2021-02-18 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
TWI899097B (zh) 2019-08-14 2025-10-01 美商維泰克斯製藥公司 製備cftr調節劑之方法
EP4058434A1 (en) 2019-11-12 2022-09-21 Genzyme Corporation 6-membered heteroarylaminosulfonamides for treating diseases and conditions mediated by deficient cftr activity
WO2022076628A1 (en) * 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
AU2021397294A1 (en) 2020-12-10 2023-07-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
CN113480416B (zh) * 2021-07-12 2023-03-21 重庆大学 一种芳基酮的制备方法
KR20240168370A (ko) 2022-03-30 2024-11-29 이시하라 산교 가부시끼가이샤 피리다지논계 화합물 또는 그의 염 및 그들을 함유하는 유해 생물 방제제
CN114835655A (zh) * 2022-04-14 2022-08-02 河南师范大学 一种合成光学活性三氟甲基丙烯酸酯类化合物的方法
EP4611742A1 (en) 2022-10-31 2025-09-10 Sionna Therapeutics Inc. Methods of treating cftr-mediated diseases or disorders
WO2025017207A1 (en) * 2023-07-20 2025-01-23 Cemm - Forschungszentrum Für Molekulare Medizin Gmbh Inhibitors of smndc1 and their therapeutic use
WO2025076235A1 (en) 2023-10-04 2025-04-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator

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US5449783A (en) * 1991-03-07 1995-09-12 Hisamitsu Pharmaceutical Co., Inc. Diphenylthiazole derivative
WO1996016650A1 (en) * 1994-11-29 1996-06-06 Hisamitsu Pharmaceutical Co., Inc. Antibacterial or bactericide comprising 2-aminothiazole derivative and salts thereof
WO2003039451A2 (en) * 2001-11-08 2003-05-15 Fujisawa Pharmaceutical Co., Ltd. Thiazole pyridazinones as adenosine antagonists
WO2016183173A1 (en) * 2015-05-12 2016-11-17 Avista Pharma Solutions Antiparasitic compounds

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US10138227B2 (en) * 2016-06-03 2018-11-27 Abbvie S.Á.R.L. Heteroaryl substituted pyridines and methods of use
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US5449783A (en) * 1991-03-07 1995-09-12 Hisamitsu Pharmaceutical Co., Inc. Diphenylthiazole derivative
WO1996016650A1 (en) * 1994-11-29 1996-06-06 Hisamitsu Pharmaceutical Co., Inc. Antibacterial or bactericide comprising 2-aminothiazole derivative and salts thereof
WO2003039451A2 (en) * 2001-11-08 2003-05-15 Fujisawa Pharmaceutical Co., Ltd. Thiazole pyridazinones as adenosine antagonists
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MX2022005809A (es) 2022-06-08
WO2021097057A1 (en) 2021-05-20
PE20221461A1 (es) 2022-09-21
JP2025160375A (ja) 2025-10-22
EP4058439A1 (en) 2022-09-21
KR20220115829A (ko) 2022-08-18
JOP20220105A1 (ar) 2023-01-30
AU2020384279A1 (en) 2022-05-26
IL292966A (en) 2022-07-01
CL2022001245A1 (es) 2023-03-10
CN115003659A (zh) 2022-09-02
BR112022009185A2 (pt) 2022-07-26
JP7721517B2 (ja) 2025-08-12
CO2022007953A2 (es) 2022-09-09
US20240002374A1 (en) 2024-01-04
ECSP22046050A (es) 2022-08-31
CA3158057A1 (en) 2021-05-20
PH12022551139A1 (en) 2023-07-17
JP2023500408A (ja) 2023-01-05

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