KR20230053646A - 섬유증의 치료를 위한 tlr9 억제제로서의 1h-피롤로[3,2-c]피리딘 및 1h-피롤로[2,3-c]피리딘 유도체 - Google Patents
섬유증의 치료를 위한 tlr9 억제제로서의 1h-피롤로[3,2-c]피리딘 및 1h-피롤로[2,3-c]피리딘 유도체 Download PDFInfo
- Publication number
- KR20230053646A KR20230053646A KR1020237009022A KR20237009022A KR20230053646A KR 20230053646 A KR20230053646 A KR 20230053646A KR 1020237009022 A KR1020237009022 A KR 1020237009022A KR 20237009022 A KR20237009022 A KR 20237009022A KR 20230053646 A KR20230053646 A KR 20230053646A
- Authority
- KR
- South Korea
- Prior art keywords
- phenyl
- pyrrolo
- dimethyl
- methylsulfonyl
- pyridin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- 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
Landscapes
- 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)
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 |
|---|---|
| KR20230053646A true KR20230053646A (ko) | 2023-04-21 |
Family
ID=77711459
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020237009022A Pending KR20230053646A (ko) | 2020-08-19 | 2021-08-18 | 섬유증의 치료를 위한 tlr9 억제제로서의 1h-피롤로[3,2-c]피리딘 및 1h-피롤로[2,3-c]피리딘 유도체 |
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=) |
Families Citing this family (7)
| 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 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN110891949B (zh) | 2017-07-05 | 2023-05-23 | 先正达参股股份有限公司 | 具有含硫取代基的杀有害生物活性杂环衍生物 |
| CN110997656B (zh) | 2017-08-04 | 2023-04-14 | 百时美施贵宝公司 | 用作tlr7/8/9抑制剂的取代的吲哚化合物 |
| 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 |
| BR112020011668A2 (pt) | 2017-12-15 | 2020-11-17 | Bristol-Myers Squibb Company | compostos de éter de indol substituído |
| 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 |
| WO2019126082A1 (en) | 2017-12-19 | 2019-06-27 | Bristol-Myers Squibb Company | 6-azaindole compounds |
| BR112020012084A2 (pt) | 2017-12-19 | 2020-11-24 | Bristol-Myers Squibb Company | compostos de indol substituído úteis como inibidores de tlr |
| CA3085942A1 (en) | 2017-12-20 | 2019-06-27 | Bristol-Myers Squibb Company | Aryl and heteroaryl substituted indole compounds |
| US11299501B2 (en) | 2017-12-20 | 2022-04-12 | Bristol-Myers Squibb Company | Diazaindole compounds |
| BR112020011984A2 (pt) | 2017-12-20 | 2020-11-17 | Bristol-Myers Squibb Company | compostos de amino indol úteis como inibidores de tlr |
| MX2021001565A (es) | 2018-08-08 | 2021-04-19 | Bristol Myers Squibb Co | Inhibidores tipo indol y azaindol de enzimas peptidil arginina deiminasas (pad). |
-
2021
- 2021-08-18 AU AU2021328577A patent/AU2021328577A1/en not_active Abandoned
- 2021-08-18 KR KR1020237009022A patent/KR20230053646A/ko active Pending
- 2021-08-18 BR BR112023002646A patent/BR112023002646A2/pt not_active Application Discontinuation
- 2021-08-18 CN CN202180050340.3A patent/CN115867549A/zh active Pending
- 2021-08-18 MX MX2023001929A patent/MX2023001929A/es unknown
- 2021-08-18 TW TW110130428A patent/TW202214233A/zh unknown
- 2021-08-18 WO PCT/US2021/046434 patent/WO2022040267A1/en not_active Ceased
- 2021-08-18 AR ARP210102329A patent/AR123285A1/es not_active Application Discontinuation
- 2021-08-18 US US18/042,069 patent/US12590091B2/en active Active
- 2021-08-18 ES ES21769261T patent/ES3034264T3/es active Active
- 2021-08-18 IL IL300643A patent/IL300643A/en unknown
- 2021-08-18 EP EP21769261.5A patent/EP4200298B1/en active Active
- 2021-08-18 JP JP2023512162A patent/JP2023538608A/ja active Pending
- 2021-08-18 CA CA3189826A patent/CA3189826A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US20230312565A1 (en) | 2023-10-05 |
| AU2021328577A1 (en) | 2023-03-23 |
| JP2023538608A (ja) | 2023-09-08 |
| 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 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EP4200298B1 (en) | 1h-pyrrolo[3,2-c]pyridine and 1h-pyrrolo[2,3-c]pyridine derivatives as tlr9 inhibitors for the treatment of fibrosis | |
| EP4200015B1 (en) | Substituted heteroaryl compounds useful as inhibitors of tlr9 | |
| US12492188B2 (en) | 1H-benzo[D]imidazole derivatives as TLR9 inhibitors for the treatment of fibrosis | |
| JP7813775B2 (ja) | 線維症の処置のためのｔｌｒ９の阻害剤としてのイミダゾ［１，２－ａ］ピリジンおよび［１，２，４］トリアゾロ［１，５－ａ］ピリジン誘導体 | |
| EA050843B1 (ru) | Замещенные гетероарильные соединения, пригодные для применения в качестве ингибиторов tlr9 | |
| KR20240148413A (ko) | Tlr9의 억제제로서 유용한 치환된 비시클릭 헤테로아릴 화합물 | |
| KR20240148414A (ko) | Tlr9의 억제제로서 유용한 치환된 이미다조피리디닐 화합물 | |
| EA047759B1 (ru) | Замещенные гетероарильные соединения, пригодные для применения в качестве ингибиторов tlr9 | |
| WO2024102884A1 (en) | Substituted quinolone compounds useful as inhibitors of tlr9 | |
| KR20250109202A (ko) | Tlr9의 억제제로서 유용한 치환된 벤즈이미다졸 화합물 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
St.27 status event code: A-0-1-A10-A15-nap-PA0105 |
|
| PG1501 | Laying open of application |
St.27 status event code: A-1-1-Q10-Q12-nap-PG1501 |
|
| A201 | Request for examination | ||
| E13-X000 | Pre-grant limitation requested |
St.27 status event code: A-2-3-E10-E13-lim-X000 |
|
| P11-X000 | Amendment of application requested |
St.27 status event code: A-2-2-P10-P11-nap-X000 |
|
| P13-X000 | Application amended |
St.27 status event code: A-2-2-P10-P13-nap-X000 |
|
| PA0201 | Request for examination |
St.27 status event code: A-1-2-D10-D11-exm-PA0201 |
|
| D21 | Rejection of application intended |
Free format text: ST27 STATUS EVENT CODE: A-1-2-D10-D21-EXM-PE0902 (AS PROVIDED BY THE NATIONAL OFFICE) |
|
| PE0902 | Notice of grounds for rejection |
St.27 status event code: A-1-2-D10-D21-exm-PE0902 |