KR20240090506A - 피페리디닐 인돌 유도체, 이의 제조 방법 및 의약적 용도 - Google Patents

피페리디닐 인돌 유도체, 이의 제조 방법 및 의약적 용도 Download PDF

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Publication number
KR20240090506A
KR20240090506A KR1020247016505A KR20247016505A KR20240090506A KR 20240090506 A KR20240090506 A KR 20240090506A KR 1020247016505 A KR1020247016505 A KR 1020247016505A KR 20247016505 A KR20247016505 A KR 20247016505A KR 20240090506 A KR20240090506 A KR 20240090506A
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South Korea
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alkyl
alkoxy
haloalkyl
halogen
hydroxyalkyl
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KR1020247016505A
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Korean (ko)
Inventor
휴 와이. 주
아비나쉬 칸나
매튜 키어
리사 에이. 드 미즈
웨이 저우
Original Assignee
한서 바이오 엘엘씨
상하이 한서 바이오메디컬 컴퍼니 리미티드
장쑤 한서 파마슈티칼 그룹 캄파니 리미티드
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Application filed by 한서 바이오 엘엘씨, 상하이 한서 바이오메디컬 컴퍼니 리미티드, 장쑤 한서 파마슈티칼 그룹 캄파니 리미티드 filed Critical 한서 바이오 엘엘씨
Publication of KR20240090506A publication Critical patent/KR20240090506A/ko
Pending legal-status Critical Current

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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
    • C07D403/10—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 linked by a carbon chain containing aromatic rings
    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • 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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or 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
    • A61K31/435—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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D487/02—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
    • C07D487/08—Bridged 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
    • C07D491/02—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 two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • C07D491/02—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 two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
KR1020247016505A 2021-10-27 2022-10-27 피페리디닐 인돌 유도체, 이의 제조 방법 및 의약적 용도 Pending KR20240090506A (ko)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US202163263108P 2021-10-27 2021-10-27
US63/263,108 2021-10-27
US202263268655P 2022-02-28 2022-02-28
US63/268,655 2022-02-28
US202263362916P 2022-04-13 2022-04-13
US63/362,916 2022-04-13
US202263365029P 2022-05-20 2022-05-20
US63/365,029 2022-05-20
US202263366101P 2022-06-09 2022-06-09
US63/366,101 2022-06-09
PCT/CN2022/127975 WO2023072197A1 (en) 2021-10-27 2022-10-27 Piperidinyl indole derivatives, preparation methods and medicinal uses thereof

Publications (1)

Publication Number Publication Date
KR20240090506A true KR20240090506A (ko) 2024-06-21

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KR1020247016505A Pending KR20240090506A (ko) 2021-10-27 2022-10-27 피페리디닐 인돌 유도체, 이의 제조 방법 및 의약적 용도

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Country Link
US (1) US20250243186A1 (https=)
EP (1) EP4423076A4 (https=)
JP (1) JP2024541929A (https=)
KR (1) KR20240090506A (https=)
AU (1) AU2022376760A1 (https=)
CA (1) CA3236104A1 (https=)
MX (1) MX2024004921A (https=)
TW (1) TW202334121A (https=)
WO (1) WO2023072197A1 (https=)

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CN120081822A (zh) * 2021-06-03 2025-06-03 诺瓦提斯药物公司 经取代的吲哚化合物及其使用方法
EP4389742A4 (en) * 2021-08-18 2026-01-14 Xizang Haisco Pharmaceutical Co Ltd HETEROAROMATIC CYCLE DERIVATIVE CONTAINING BENZO NITROGEN AND ITS USE IN MEDICINE
CA3247772A1 (en) * 2022-01-24 2023-07-27 Novartis Ag Spirocyclic piperidinyl derivatives as complement factor B inhibitors and their uses
CN119301114A (zh) * 2022-06-07 2025-01-10 正大天晴药业集团股份有限公司 双环取代的芳香羧酸类氘代化合物
WO2023246677A1 (zh) * 2022-06-20 2023-12-28 深圳信立泰药业股份有限公司 一种吲哚-苯基哌啶化合物及其制备方法与应用
TW202423426A (zh) * 2022-08-31 2024-06-16 美商奇努克醫療股份有限公司 經取代之吲哚化合物及其使用方法
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TW202506657A (zh) * 2023-04-27 2025-02-16 大陸商上海翰森生物醫藥科技有限公司 一種哌啶基吲哚化合物的鹽及其製備方法
CN121889385A (zh) 2023-07-04 2026-04-17 希塔拉生物有限公司 作为因子b抑制剂的2-(1h-吲哚-4-基)甲基)2h-吲唑衍生物
IL325760A (en) 2023-07-04 2026-03-01 Sitala Bio Ltd History of 2-(1H-indol-4-yl)methyl)-isoindoline as factor B inhibitors
WO2025008517A1 (en) 2023-07-06 2025-01-09 Sitala Bio Ltd Indole derivatives with factor b inhibitory activity
WO2025008516A2 (en) 2023-07-06 2025-01-09 Sitala Bio Ltd Novel compounds
CN119371402A (zh) * 2023-07-26 2025-01-28 上海美悦生物科技发展有限公司 螺环烯基类或氮杂烯基类化合物及其药物组合物、制备方法和用途
TW202542111A (zh) * 2023-12-27 2025-11-01 大陸商海思科醫藥集團股份有限公司 一種苯基呱啶衍生物的製備方法
WO2025148628A1 (zh) * 2024-01-10 2025-07-17 河北以岭医药研究院有限公司 哌啶基吲哚衍生物及其制备方法和应用
WO2025172535A1 (en) 2024-02-15 2025-08-21 Sitala Bio Ltd Indole and benzimidazole compounds as factor b inhibitors
TW202543599A (zh) * 2024-03-08 2025-11-16 大陸商江蘇豪森藥業集團有限公司 一種多元螺環化合物的晶型、其製備方法和醫藥用途
WO2025185734A1 (zh) * 2024-03-08 2025-09-12 江苏豪森药业集团有限公司 一种多元螺环化合物的盐及其晶型、其制备方法和医药用途
WO2025252133A1 (zh) * 2024-06-07 2025-12-11 润尔眼科药物（广州）有限公司 一种含吲哚基团的化合物及其用途
WO2025256600A1 (zh) * 2024-06-12 2025-12-18 润尔眼科药物（广州）有限公司 一种杂环化合物及其用途

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JO3425B1 (ar) * 2013-07-15 2019-10-20 Novartis Ag مشتقات البابيريدينيل-اندول واستخدامها كعامل متمم لمثبطات b
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CN120081822A (zh) * 2021-06-03 2025-06-03 诺瓦提斯药物公司 经取代的吲哚化合物及其使用方法
EP4389742A4 (en) * 2021-08-18 2026-01-14 Xizang Haisco Pharmaceutical Co Ltd HETEROAROMATIC CYCLE DERIVATIVE CONTAINING BENZO NITROGEN AND ITS USE IN MEDICINE
CA3247772A1 (en) * 2022-01-24 2023-07-27 Novartis Ag Spirocyclic piperidinyl derivatives as complement factor B inhibitors and their uses

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US20250243186A1 (en) 2025-07-31
JP2024541929A (ja) 2024-11-13
MX2024004921A (es) 2024-06-19
EP4423076A1 (en) 2024-09-04
AU2022376760A1 (en) 2024-05-02
WO2023072197A1 (en) 2023-05-04
CA3236104A1 (en) 2023-05-04
TW202334121A (zh) 2023-09-01

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