CN114929345B - 作为toll受体抑制剂的经取代的吡唑化合物 - Google Patents

作为toll受体抑制剂的经取代的吡唑化合物 Download PDF

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Publication number
CN114929345B
CN114929345B CN202080091908.1A CN202080091908A CN114929345B CN 114929345 B CN114929345 B CN 114929345B CN 202080091908 A CN202080091908 A CN 202080091908A CN 114929345 B CN114929345 B CN 114929345B
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triazolo
pyridin
isopropyl
pyrazol
methyl
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CN202080091908.1A
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Chinese (zh)
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CN114929345A (zh
Inventor
L·帕苏诺里
S·R·库马尔
P·V·V·斯里尼瓦斯
V·博加迪
S·K·杜赖萨米
A·K·拉玛钱德拉·雷迪
R·K·纳姆努拉
A·J·迪克曼
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 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
    • 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
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
    • A61K31/535—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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • 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

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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)
CN202080091908.1A 2019-11-01 2020-10-30 作为toll受体抑制剂的经取代的吡唑化合物 Active CN114929345B (zh)

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 (2)

Publication Number Publication Date
CN114929345A CN114929345A (zh) 2022-08-19
CN114929345B true CN114929345B (zh) 2024-07-23

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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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102224142A (zh) * 2008-11-21 2011-10-19 拉夸里亚创药株式会社 具有5-ht2b受体拮抗活性的新型吡唑-3-羧酰胺衍生物
CN104428300A (zh) * 2012-07-12 2015-03-18 奇斯药制品公司 酶的抑制

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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
JP2012102018A (ja) * 2009-03-03 2012-05-31 Astellas Pharma Inc アミド化合物
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102224142A (zh) * 2008-11-21 2011-10-19 拉夸里亚创药株式会社 具有5-ht2b受体拮抗活性的新型吡唑-3-羧酰胺衍生物
CN104428300A (zh) * 2012-07-12 2015-03-18 奇斯药制品公司 酶的抑制

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WO2021087181A1 (en) 2021-05-06
EP4051388A1 (en) 2022-09-07
KR20220097434A (ko) 2022-07-07
CN114929345A (zh) 2022-08-19
US20230117470A1 (en) 2023-04-20
JP7652772B2 (ja) 2025-03-27
JP2023501956A (ja) 2023-01-20

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