PE20240229A1 - DERIVADOS DE INDOL UTILES EN EL TRATAMIENTO DE AFECCIONES ASOCIADAS CON cGAS - Google Patents
DERIVADOS DE INDOL UTILES EN EL TRATAMIENTO DE AFECCIONES ASOCIADAS CON cGASInfo
- Publication number
- PE20240229A1 PE20240229A1 PE2023001937A PE2023001937A PE20240229A1 PE 20240229 A1 PE20240229 A1 PE 20240229A1 PE 2023001937 A PE2023001937 A PE 2023001937A PE 2023001937 A PE2023001937 A PE 2023001937A PE 20240229 A1 PE20240229 A1 PE 20240229A1
- Authority
- PE
- Peru
- Prior art keywords
- cgas
- alkylene
- treatment
- alkoxy
- halogen
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/14—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 three or more hetero rings
-
- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles 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
- A61K31/435—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
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—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
- 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invencion se refiere a un compuesto derivado de indol de formula (I), o una sal, hidrato, solvato, estereoisomero o tautomero del mismo, farmaceuticamente aceptable, donde: R1 es un anillo heteroarilo de 5 miembros que comprende 1 a 4 heteroatomos seleccionados de entre O, N y S, sustituidos optativamente; R2 es un anillo heteroarilo de 5 miembros que comprende 3 atomos N, en las posiciones 1, 2 y 4 relativas entre si, sustituidos optativamente; R3 es H, halogeno, -OH, -NR11R12, -(C1-C4)alquileno-NR13R14, entre otros; R4 es H, (C1-C4)alquilo, -(C1-C4)alquileno-OH, -(C1-C4)alquileno-(C1-C4)alcoxi, entre otros; cada uno de R5, R6, R7 y R8 es independientemente H, halogeno, OH, (C1-C4)alquilo, (C1-C4)alcoxi, entre otros. Un compuesto seleccionado es 6-cloro-7-fluoro-5-metoxi-1-metil-3-(1H-pirazol-4-il)-2-(5-(trifluorometil)-4H-1,2,4-triazol-3-il)-1H-indol. Dicho compuesto inhibe la sintasa ciclica GMP?AMP (cGAS) o ruta cGAS. Tambien se refiere a una composicion y una combinacion farmaceutica que comprende dicho compuestos, siendo utiles en el tratamiento de enfermedades inmunitarias o inflamatorias, tales como Sindrome de Aicardi-Goutières, Lupus Hereditario de Sabanones, vasculitis, entre otros.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063128949P | 2020-12-22 | 2020-12-22 | |
| PCT/IB2021/062029 WO2022137085A1 (en) | 2020-12-22 | 2021-12-20 | Indole derivatives useful in treating conditions associated with cgas |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20240229A1 true PE20240229A1 (es) | 2024-02-16 |
Family
ID=79164465
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023001937A PE20240229A1 (es) | 2020-12-22 | 2021-12-20 | DERIVADOS DE INDOL UTILES EN EL TRATAMIENTO DE AFECCIONES ASOCIADAS CON cGAS |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US12404261B2 (es) |
| EP (1) | EP4267564A1 (es) |
| JP (1) | JP2024502258A (es) |
| KR (1) | KR20230124665A (es) |
| CN (1) | CN116635382A (es) |
| AR (1) | AR124443A1 (es) |
| AU (1) | AU2021404953A1 (es) |
| CA (1) | CA3202212A1 (es) |
| CL (1) | CL2023001859A1 (es) |
| CO (1) | CO2023007954A2 (es) |
| CR (1) | CR20230282A (es) |
| DO (1) | DOP2023000129A (es) |
| EC (1) | ECSP23045506A (es) |
| IL (1) | IL303913A (es) |
| MX (1) | MX2023007467A (es) |
| PE (1) | PE20240229A1 (es) |
| SA (1) | SA523441335B1 (es) |
| TW (1) | TW202241873A (es) |
| UY (1) | UY39579A (es) |
| WO (1) | WO2022137085A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20220241A (es) | 2019-11-04 | 2022-08-03 | Revolution Medicines Inc | Inhibidores de ras |
| US11690915B2 (en) | 2020-09-15 | 2023-07-04 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2023235809A1 (en) * | 2022-06-02 | 2023-12-07 | Eli Lilly And Company | Cgas inhibitors |
| JP2025535332A (ja) | 2022-10-18 | 2025-10-24 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド | ｃＧＡＳ阻害剤としてのトリアゾール置換イミダゾ［１，２－ａ］ピリミジン |
| WO2024137752A1 (en) | 2022-12-21 | 2024-06-27 | Eli Lilly And Company | Azepino[4,5-b]indolone cgas inhibitors |
| AR132055A1 (es) * | 2023-03-06 | 2025-05-21 | Insilico Medicine Ip Ltd | Inhibidores duales de cdk8/19 y métodos de uso de los mismos |
| WO2025215082A1 (en) * | 2024-04-11 | 2025-10-16 | Glaxosmithkline Intellectual Property Development Limited | Fused azines for the treatment of inflammatory diseases |
| WO2025231011A1 (en) * | 2024-05-01 | 2025-11-06 | Omniab, Inc. | Heteroarylindole inhibitors of apol-1 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ITMI20040874A1 (it) * | 2004-04-30 | 2004-07-30 | Ist Naz Stud Cura Dei Tumori | Derivati indolici ed azaindolici con azione antitumorale |
| AR065860A1 (es) * | 2007-03-29 | 2009-07-08 | Novartis Ag | 3-imidazolil-indoles para el tratamiento de enfermedades proliferativas |
| CA2728376C (en) | 2008-06-20 | 2015-05-12 | Rottapharm S.P.A. | 6-1h-imidazo-quinazoline and quinolines derivatives/mao inhibitors for treating depression |
| US9096579B2 (en) | 2012-04-20 | 2015-08-04 | Boehringer Ingelheim International Gmbh | Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments |
| MX365661B (es) * | 2012-12-19 | 2019-06-10 | Univ Texas | Activacion farmaceutica de una senda de señalizacion de di-nucleotido ciclico de mamifero. |
| CA2908154C (en) * | 2013-04-29 | 2023-11-28 | Memorial Sloan Kettering Cancer Center | Compositions and methods for altering second messenger signaling |
| RU2021100040A (ru) | 2014-12-22 | 2021-02-02 | Акарна Терапьютикс, Лтд. | Конденсированные бициклические соединения для лечения заболевания |
| EP3573971A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| MA50256A (fr) | 2017-09-15 | 2020-07-22 | Aduro Biotech Inc | Composés de pyrazolopyrimidinone et leurs utilisations |
| MX2020008237A (es) * | 2018-02-05 | 2020-09-25 | Univ Rockefeller | Inhibidores de 2,3,4,5-tetrahidro-1h-pirido[4,3-b]indol de cgas para tratar enfermedades autoinflamatorias. |
| EP3752150A1 (en) * | 2018-02-16 | 2020-12-23 | UCB Biopharma SRL | Pharmaceutical 6,5 heterobicyclic ring derivatives |
| WO2020123422A1 (en) | 2018-12-10 | 2020-06-18 | Aduro Biotech, Inc. | Imidazopyridazinone compounds and uses thereof |
| EP3906229A4 (en) | 2019-01-04 | 2022-11-16 | Bellbrook Labs, Llc | INHIBITORS OF CGAS ACTIVITY AS THERAPEUTIC AGENT |
| CN114901279A (zh) | 2019-03-13 | 2022-08-12 | 洛克菲勒大学 | 用于治疗自身炎性疾病和癌症转移的cGAS的抑制剂 |
| CN115427402A (zh) | 2020-04-16 | 2022-12-02 | 豪夫迈·罗氏有限公司 | 氨基磺酰胺衍生物 |
| JP2023521437A (ja) | 2020-04-16 | 2023-05-24 | エフ． ホフマン－ラ ロシュ アーゲー | ベンズイミダゾール誘導体 |
| JP2023521469A (ja) | 2020-04-16 | 2023-05-24 | エフ． ホフマン－ラ ロシュ アーゲー | インダゾール誘導体 |
| US20230192631A1 (en) | 2020-04-16 | 2023-06-22 | Hoffmann-La Roche Inc. | Biphenyl Derivatives |
| WO2021209485A1 (en) | 2020-04-16 | 2021-10-21 | F. Hoffmann-La Roche Ag | Benzimidazole derivatives |
| US11873291B2 (en) | 2020-09-03 | 2024-01-16 | Immunesensor Therapeutics, Inc. | Quinoline cGAS antagonist compounds |
| WO2022066851A1 (en) | 2020-09-24 | 2022-03-31 | Ventus Therapeutics U.S., Inc. | PYRIDO[4,3-b]INDOLE DERIVATIVES AND THEIR USE AS PHARMACEUTICALS |
-
2021
- 2021-12-20 AR ARP210103590A patent/AR124443A1/es unknown
- 2021-12-20 JP JP2023537694A patent/JP2024502258A/ja active Pending
- 2021-12-20 UY UY0001039579A patent/UY39579A/es unknown
- 2021-12-20 CN CN202180079723.3A patent/CN116635382A/zh active Pending
- 2021-12-20 US US17/645,071 patent/US12404261B2/en active Active
- 2021-12-20 WO PCT/IB2021/062029 patent/WO2022137085A1/en not_active Ceased
- 2021-12-20 AU AU2021404953A patent/AU2021404953A1/en active Pending
- 2021-12-20 CA CA3202212A patent/CA3202212A1/en active Pending
- 2021-12-20 KR KR1020237024854A patent/KR20230124665A/ko active Pending
- 2021-12-20 MX MX2023007467A patent/MX2023007467A/es unknown
- 2021-12-20 IL IL303913A patent/IL303913A/en unknown
- 2021-12-20 TW TW110147655A patent/TW202241873A/zh unknown
- 2021-12-20 CR CR20230282A patent/CR20230282A/es unknown
- 2021-12-20 EP EP21834940.5A patent/EP4267564A1/en active Pending
- 2021-12-20 PE PE2023001937A patent/PE20240229A1/es unknown
-
2023
- 2023-06-20 CO CONC2023/0007954A patent/CO2023007954A2/es unknown
- 2023-06-20 CL CL2023001859A patent/CL2023001859A1/es unknown
- 2023-06-20 EC ECSENADI202345506A patent/ECSP23045506A/es unknown
- 2023-06-21 SA SA523441335A patent/SA523441335B1/ar unknown
- 2023-06-21 DO DO2023000129A patent/DOP2023000129A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DOP2023000129A (es) | 2023-07-16 |
| AR124443A1 (es) | 2023-03-29 |
| AU2021404953A1 (en) | 2023-06-22 |
| JP2024502258A (ja) | 2024-01-18 |
| IL303913A (en) | 2023-08-01 |
| UY39579A (es) | 2022-07-29 |
| CO2023007954A2 (es) | 2023-06-30 |
| KR20230124665A (ko) | 2023-08-25 |
| CL2023001859A1 (es) | 2024-02-09 |
| EP4267564A1 (en) | 2023-11-01 |
| ECSP23045506A (es) | 2023-07-31 |
| CN116635382A (zh) | 2023-08-22 |
| CR20230282A (es) | 2023-07-12 |
| SA523441335B1 (ar) | 2025-04-20 |
| WO2022137085A1 (en) | 2022-06-30 |
| AU2021404953A9 (en) | 2024-02-08 |
| US12404261B2 (en) | 2025-09-02 |
| US20230085472A1 (en) | 2023-03-16 |
| CA3202212A1 (en) | 2022-06-30 |
| MX2023007467A (es) | 2023-07-04 |
| TW202241873A (zh) | 2022-11-01 |
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