JP7313354B2 - 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 - Google Patents

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 Download PDF

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JP7313354B2
JP7313354B2 JP2020534509A JP2020534509A JP7313354B2 JP 7313354 B2 JP7313354 B2 JP 7313354B2 JP 2020534509 A JP2020534509 A JP 2020534509A JP 2020534509 A JP2020534509 A JP 2020534509A JP 7313354 B2 JP7313354 B2 JP 7313354B2
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isopropyl
indol
methylpyridin
indole
ethyl
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JP2021506923A5 (enExample
JP2021506923A (ja
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アラリック・ジェイ・ディックマン
ダームパル・エス・ドッド
クリストファー・ピー・マッサリ
トレバー・シー・シャーウッド
タシル・シャムスル・ハーク
ショシャナ・エル・ポージー
スリーカンタ・ラトナ・クマール
ラクスマン・パスヌーリ
スブラマニア・ヘグデ
ルシト・クマール・アヌムラ
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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
    • 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
    • A61K31/40—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
    • A61K31/407—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 other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
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    • 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
    • A61K31/4995—Pyrazines or piperazines forming part of bridged 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
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    • 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
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    • 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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
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    • 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
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
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    • 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
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    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D471/10—Spiro-condensed systems
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    • 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
    • C07D491/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
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  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2020534509A 2017-12-19 2018-12-18 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 Active JP7313354B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762607388P 2017-12-19 2017-12-19
US62/607,388 2017-12-19
PCT/US2018/066106 WO2019126081A1 (en) 2017-12-19 2018-12-18 Amide substituted indole compounds useful as tlr inhibitors

Publications (3)

Publication Number Publication Date
JP2021506923A JP2021506923A (ja) 2021-02-22
JP2021506923A5 JP2021506923A5 (enExample) 2022-01-11
JP7313354B2 true JP7313354B2 (ja) 2023-07-24

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Country Link
US (1) US11420973B2 (enExample)
EP (1) EP3728221B1 (enExample)
JP (1) JP7313354B2 (enExample)
KR (1) KR102755258B1 (enExample)
CN (1) CN111511730B (enExample)
AU (1) AU2018392316B2 (enExample)
BR (1) BR112020011979A2 (enExample)
CA (1) CA3085346A1 (enExample)
EA (1) EA202091483A1 (enExample)
ES (1) ES2922174T3 (enExample)
IL (1) IL275353A (enExample)
MX (1) MX2020005515A (enExample)
SG (1) SG11202005700SA (enExample)
WO (1) WO2019126081A1 (enExample)

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* Cited by examiner, † Cited by third party
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US10071079B2 (en) 2016-06-29 2018-09-11 Bristol-Myers Squibb Company [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds
HUE067314T2 (hu) 2017-09-22 2024-10-28 Jubilant Epipad LLC Heterociklusos vegyületek mint PAD gátlók
KR102782563B1 (ko) 2017-10-18 2025-03-14 주빌런트 에피파드 엘엘씨 Pad 억제제로서의 이미다조-피리딘 화합물
KR20200085836A (ko) 2017-11-06 2020-07-15 주빌런트 프로델 엘엘씨 Pd1/pd-l1 활성화 억제제로서의 피리미딘 유도체
BR112020010322A2 (pt) 2017-11-24 2020-11-17 Jubilant Episcribe Llc composto da fórmula i; composto da fórmula ia; composto da fórmula ib; processo de preparação de compostos da fórmula i; composição farmacêutica; método para o tratamento e/ou prevenção de várias doenças; uso dos compostos; método para o tratamento de câncer; e método para o tratamento e/ou prevenção de uma afecção mediada por prmt5 ou um distúrbio proliferativo ou câncer
BR112020011984A2 (pt) * 2017-12-20 2020-11-17 Bristol-Myers Squibb Company compostos de amino indol úteis como inibidores de tlr
ES2965182T3 (es) * 2017-12-20 2024-04-11 Bristol Myers Squibb Co Compuestos de indol sustituidos con arilo y heteroarilo
SG11202008950PA (en) 2018-03-13 2020-10-29 Jubilant Prodel LLC Bicyclic compounds as inhibitors of pd1/pd-l1 interaction/activation
SG11202011137SA (en) 2018-06-05 2020-12-30 Hoffmann La Roche Tetrahydro-1 h-pyrazino[2,1 -ajisoindolylquinoline compounds for the treatment of autoimmune disease
JP7434186B2 (ja) 2018-06-12 2024-02-20 エフ． ホフマン－ラ ロシュ アーゲー 自己免疫疾患の処置のための新規のヘテロアリールヘテロシクリル化合物
CN112584903B (zh) 2018-07-23 2025-12-23 豪夫迈·罗氏有限公司 用于自身免疫性疾病治疗的哌嗪化合物
CN112638908A (zh) 2018-09-04 2021-04-09 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的苯并噻唑类化合物
CN112654618A (zh) 2018-09-06 2021-04-13 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的新型环脒化合物
WO2020048596A1 (en) 2018-09-06 2020-03-12 F. Hoffmann-La Roche Ag Novel pyrazolopyridine compounds for the treatment of autoimmune disease
EP4051387B1 (en) 2019-10-31 2025-02-19 F. Hoffmann-La Roche AG Hydropyrazino[1,2-d][1,4]diazepine compounds for the treatment of autoimmune disease
US20230117470A1 (en) * 2019-11-01 2023-04-20 Bristol-Myers Squibb Company Substituted pyrazole compounds as toll receptor inhibitors
WO2021099284A1 (en) 2019-11-19 2021-05-27 F. Hoffmann-La Roche Ag Hydro-1h-pyrrolo[1,2-a]pyrazine compounds for the treatment of autoimmune disease
US12421252B2 (en) 2019-11-20 2025-09-23 Hoffmann-La Roche Inc. Spiro (isobenzofuranazetidine) compounds for the treatment of autoimmune disease
CA3161049A1 (en) * 2020-01-30 2021-08-05 David William Sheppard Collagen 1 translation inhibitors and methods of use thereof
JP2023537280A (ja) * 2020-08-04 2023-08-31 エフ． ホフマン－ラ ロシュ アーゲー 自己免疫疾患の処置のためのイミダゾ［１，２－ａ］ピリジン化合物
KR20230053644A (ko) 2020-08-19 2023-04-21 브리스톨-마이어스 스큅 컴퍼니 섬유증의 치료를 위한 tlr9 억제제로서의 이미다조[1,2-a]피리딘 및 [1,2,4]트리아졸로[1,5-a]피리딘 유도체
CA3189873A1 (en) 2020-08-19 2022-02-24 David S. Yoon 1h-benzo[d]imidazole derivatives as tlr9 inhibitors for the treatment of fibrosis
TWI861488B (zh) 2021-04-16 2024-11-11 美商基利科學股份有限公司 噻吩并吡咯化合物
AU2022341114A1 (en) 2021-09-10 2024-02-29 Gilead Sciences, Inc. Thienopyrrole compounds
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KR20240066957A (ko) 2022-10-31 2024-05-16 아주대학교산학협력단 자기염증질환 치료 및 예방 조성물

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