KR20220097434A - 톨 수용체 억제제로서의 치환된 피라졸 화합물 - Google Patents

톨 수용체 억제제로서의 치환된 피라졸 화합물 Download PDF

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Publication number
KR20220097434A
KR20220097434A KR1020227018003A KR20227018003A KR20220097434A KR 20220097434 A KR20220097434 A KR 20220097434A KR 1020227018003 A KR1020227018003 A KR 1020227018003A KR 20227018003 A KR20227018003 A KR 20227018003A KR 20220097434 A KR20220097434 A KR 20220097434A
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South Korea
Prior art keywords
triazolo
pyridin
isopropyl
methyl
pyrazol
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Pending
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KR1020227018003A
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English (en)
Korean (ko)
Inventor
락스만 파수누리
스리칸타 라트나 쿠마르
피타니 비라 벤카타 스리니바스
비크람 보가디
스리니바산 쿤치타파탐 두라이사미
아누파마 칸디 라마찬드라 레디
루시트 쿠마르 아누물라
알라릭 제이. 딕맨
Original Assignee
브리스톨-마이어스 스큅 컴퍼니
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Publication of KR20220097434A publication Critical patent/KR20220097434A/ko
Pending legal-status Critical Current

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    • 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
    • C07D471/02Heterocyclic 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 two hetero rings
    • C07D471/04Ortho-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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020227018003A 2019-11-01 2020-10-30 톨 수용체 억제제로서의 치환된 피라졸 화합물 Pending KR20220097434A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962929299P 2019-11-01 2019-11-01
US62/929,299 2019-11-01
PCT/US2020/058081 WO2021087181A1 (en) 2019-11-01 2020-10-30 Substituted pyrazole compounds as toll receptor inhibitors

Publications (1)

Publication Number Publication Date
KR20220097434A true KR20220097434A (ko) 2022-07-07

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020227018003A Pending KR20220097434A (ko) 2019-11-01 2020-10-30 톨 수용체 억제제로서의 치환된 피라졸 화합물

Country Status (6)

Country Link
US (1) US20230117470A1 (enExample)
EP (1) EP4051388A1 (enExample)
JP (1) JP7652772B2 (enExample)
KR (1) KR20220097434A (enExample)
CN (1) CN114929345B (enExample)
WO (1) WO2021087181A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230171469A (ko) 2021-04-16 2023-12-20 길리애드 사이언시즈, 인코포레이티드 티에노피롤 화합물
EP4398989A1 (en) 2021-09-10 2024-07-17 Gilead Sciences, Inc. Thienopyrrole compounds
EP4436975A1 (en) * 2021-11-23 2024-10-02 Genentech, Inc. Spirocyclic cyclic modulators of cholesterol biosynthesis and their use for promoting remyelination
WO2025261449A1 (zh) * 2024-06-19 2025-12-26 浙江扬厉医药技术有限公司 一种parp1抑制剂吡啶酰胺类化合物、中间体及其制备方法
WO2026002036A1 (zh) * 2024-06-26 2026-01-02 北京双鹤润创科技有限公司 一种化合物及其用途
CN119684287A (zh) * 2024-12-18 2025-03-25 烟台新药创制山东省实验室 4-(3-(哌啶-4-基)-1H-吡唑-5-基)-1H-吡咯[2,3-b]吡啶衍生物及其制备方法与应用

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1971594A2 (en) * 2005-11-21 2008-09-24 Biogen Idec MA Inc. Substituted pyrazalones
EP2304366A2 (en) * 2008-05-30 2011-04-06 Foster Wheeler Energia Oy Method of and system for generating power by oxyfuel combustion
CA2738929A1 (en) * 2008-10-17 2010-04-22 Boehringer Ingelheim International Gmbh Heteroaryl substituted indole compounds useful as mmp-13 inhibitors
MX2011005221A (es) * 2008-11-21 2011-08-03 Raqualia Pharma Inc Nuevo derivado de la pirazol-3-carboxamida que tiene actividad de antagonista del receptor de 5-ht2b.
JP2012102018A (ja) * 2009-03-03 2012-05-31 Astellas Pharma Inc アミド化合物
CA2878792A1 (en) * 2012-07-12 2014-01-16 Chiesi Farmaceutici S.P.A. Inhibition of enzymes
US9550778B2 (en) * 2014-10-03 2017-01-24 Vanderbilt University Substituted 6-aryl-imidazopyridine and 6-aryl-triazolopyridine carboxamide analogs as negative allosteric modulators of mGluR5
KR102434226B1 (ko) * 2016-06-30 2022-08-19 한미약품 주식회사 Alk5 억제제로서의 신규 피라졸 유도체 및 이의 용도
CN110869360B (zh) * 2017-07-12 2023-12-15 百时美施贵宝公司 作为rock抑制剂的苯乙酰胺类
FI3728252T3 (fi) * 2017-12-18 2023-10-18 Bristol Myers Squibb Co 4-atsaindoliyhdisteitä
JP7313354B2 (ja) * 2017-12-19 2023-07-24 ブリストル-マイヤーズ スクイブ カンパニー Tlr阻害剤として有用なアミド置換されたインドール化合物
WO2019136147A1 (en) * 2018-01-03 2019-07-11 The Board Of Trustees Of The University Of Illinois Toll-like receptor signaling inhibitors

Also Published As

Publication number Publication date
WO2021087181A1 (en) 2021-05-06
EP4051388A1 (en) 2022-09-07
CN114929345A (zh) 2022-08-19
CN114929345B (zh) 2024-07-23
US20230117470A1 (en) 2023-04-20
JP7652772B2 (ja) 2025-03-27
JP2023501956A (ja) 2023-01-20

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