AU2021328577A1 - 1H-pyrrolo[3,2-c]pyridine and 1H-pyrrolo[2,3-c]pyridine derivatives as TLR9 inhibitors for the treatment of fibrosis - Google Patents

1H-pyrrolo[3,2-c]pyridine and 1H-pyrrolo[2,3-c]pyridine derivatives as TLR9 inhibitors for the treatment of fibrosis Download PDF

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Publication number
AU2021328577A1
AU2021328577A1 AU2021328577A AU2021328577A AU2021328577A1 AU 2021328577 A1 AU2021328577 A1 AU 2021328577A1 AU 2021328577 A AU2021328577 A AU 2021328577A AU 2021328577 A AU2021328577 A AU 2021328577A AU 2021328577 A1 AU2021328577 A1 AU 2021328577A1
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Prior art keywords
phenyl
pyrrolo
dimethyl
methylsulfonyl
pyridin
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Abandoned
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AU2021328577A
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English (en)
Inventor
Chunjian Liu
Alicia Regueiro-Ren
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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Publication date
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Publication of AU2021328577A1 publication Critical patent/AU2021328577A1/en
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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
    • A61K31/44—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • 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
    • C07D471/08—Bridged 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
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2021328577A 2020-08-19 2021-08-18 1H-pyrrolo[3,2-c]pyridine and 1H-pyrrolo[2,3-c]pyridine derivatives as TLR9 inhibitors for the treatment of fibrosis Abandoned AU2021328577A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063067465P 2020-08-19 2020-08-19
US63/067,465 2020-08-19
PCT/US2021/046434 WO2022040267A1 (en) 2020-08-19 2021-08-18 1h-pyrrolo[3,2-c]pyridine and 1h-pyrrolo[2,3-c]pyridine derivatives as tlr9 inhibitors for the treatment of fibrosis

Publications (1)

Publication Number Publication Date
AU2021328577A1 true AU2021328577A1 (en) 2023-03-23

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Family Applications (1)

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AU2021328577A Abandoned AU2021328577A1 (en) 2020-08-19 2021-08-18 1H-pyrrolo[3,2-c]pyridine and 1H-pyrrolo[2,3-c]pyridine derivatives as TLR9 inhibitors for the treatment of fibrosis

Country Status (14)

Country Link
US (1) US12590091B2 (https=)
EP (1) EP4200298B1 (https=)
JP (1) JP2023538608A (https=)
KR (1) KR20230053646A (https=)
CN (1) CN115867549A (https=)
AR (1) AR123285A1 (https=)
AU (1) AU2021328577A1 (https=)
BR (1) BR112023002646A2 (https=)
CA (1) CA3189826A1 (https=)
ES (1) ES3034264T3 (https=)
IL (1) IL300643A (https=)
MX (1) MX2023001929A (https=)
TW (1) TW202214233A (https=)
WO (1) WO2022040267A1 (https=)

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Publication number Priority date Publication date Assignee Title
US11807622B2 (en) 2019-01-30 2023-11-07 Insilico Medicine Ip Limited TLR 9 inhibitors
KR20240148414A (ko) * 2022-02-18 2024-10-11 브리스톨-마이어스 스큅 컴퍼니 Tlr9의 억제제로서 유용한 치환된 이미다조피리디닐 화합물
WO2024102886A1 (en) * 2022-11-10 2024-05-16 Bristol-Myers Squibb Company Substituted benzimidazole compounds useful as inhibitors of tlr9
CN120152957A (zh) * 2022-11-10 2025-06-13 百时美施贵宝公司 用作tlr9抑制剂的经取代的喹诺酮
WO2024163380A1 (en) * 2023-01-31 2024-08-08 Bristol-Myers Squibb Company Substituted benzimidazole compounds useful as inhibitors of tlr9
IL324670A (en) 2023-06-30 2026-01-01 Bristol Myers Squibb Co KRAS inhibitors
WO2026039512A1 (en) 2024-08-14 2026-02-19 Bristol-Myers Squibb Company Kras inhibitors

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WO2007115306A2 (en) 2006-04-04 2007-10-11 Myriad Genetics, Inc. Compounds for diseases and disorders
US20060235037A1 (en) 2005-04-15 2006-10-19 Purandare Ashok V Heterocyclic inhibitors of protein arginine methyl transferases
GB0602178D0 (en) 2006-02-03 2006-03-15 Merck Sharp & Dohme Therapeutic treatment
CA2738929A1 (en) 2008-10-17 2010-04-22 Boehringer Ingelheim International Gmbh Heteroaryl substituted indole compounds useful as mmp-13 inhibitors
US20130158049A1 (en) 2011-12-20 2013-06-20 Hoffmann-La Roche Inc. 7-azaindole inhibitors of crac
US20130158066A1 (en) 2011-12-20 2013-06-20 Hoffmann-La Roche Inc. 4-azaindole inhibitors of crac
WO2013156431A1 (en) 2012-04-17 2013-10-24 Syngenta Participations Ag Pesticidally active pyridyl- and pyrimidyl- substituted thiazole and thiadiazole derivatives
EP2738172A1 (en) 2012-11-28 2014-06-04 Almirall, S.A. New bicyclic compounds as crac channel modulators
EP3080124A1 (en) * 2013-12-13 2016-10-19 Takeda Pharmaceutical Company Limited Pyrrolo[3,2-c]pyridine derivatives as tlr inhibitors
AR107032A1 (es) 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores bicíclicos de pad4
US10071079B2 (en) 2016-06-29 2018-09-11 Bristol-Myers Squibb Company [1,2,4]triazolo[1,5-a]pyridinyl substituted indole compounds
MX391344B (es) 2016-07-30 2025-03-21 Bristol Myers Squibb Co Compuestos indol sustituidos con dimetoxifenilo como inhibidores de receptores tipo toll 7, 8 o 9 (tlr7, tlr8 o tlr9).
KR102519535B1 (ko) 2016-09-09 2023-04-06 브리스톨-마이어스 스큅 컴퍼니 피리딜 치환된 인돌 화합물
US11370794B2 (en) * 2016-11-11 2022-06-28 Dynavax Technologies Corporation Toll-like receptor antagonist compounds and methods of use
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ES2921020T3 (es) 2017-08-04 2022-08-16 Bristol Myers Squibb Co Compuestos de indol sustituidos con [1,2,4]triazolo[4,3-a]piridinilo
CN111448190B (zh) 2017-11-14 2023-09-26 百时美施贵宝公司 取代的吲哚化合物
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Also Published As

Publication number Publication date
US20230312565A1 (en) 2023-10-05
JP2023538608A (ja) 2023-09-08
KR20230053646A (ko) 2023-04-21
US12590091B2 (en) 2026-03-31
AR123285A1 (es) 2022-11-16
IL300643A (en) 2023-04-01
ES3034264T3 (en) 2025-08-14
TW202214233A (zh) 2022-04-16
MX2023001929A (es) 2023-03-09
EP4200298B1 (en) 2025-05-21
CN115867549A (zh) 2023-03-28
WO2022040267A1 (en) 2022-02-24
CA3189826A1 (en) 2022-02-24
BR112023002646A2 (pt) 2023-04-04
EP4200298A1 (en) 2023-06-28

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MK1 Application lapsed section 142(2)(a) - no request for examination in relevant period