AR126244A2 - HETEROARYL SUBSTITUTED PYRIMIDINES LRRK2 INHIBITORS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS - Google Patents
HETEROARYL SUBSTITUTED PYRIMIDINES LRRK2 INHIBITORS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERSInfo
- Publication number
- AR126244A2 AR126244A2 ARP220101670A ARP220101670A AR126244A2 AR 126244 A2 AR126244 A2 AR 126244A2 AR P220101670 A ARP220101670 A AR P220101670A AR P220101670 A ARP220101670 A AR P220101670A AR 126244 A2 AR126244 A2 AR 126244A2
- Authority
- AR
- Argentina
- Prior art keywords
- optionally substituted
- alkyl
- stereoisomers
- treatment
- alkoxy
- Prior art date
Links
- 229940124786 LRRK2 inhibitor Drugs 0.000 title abstract 2
- 208000015122 neurodegenerative disease Diseases 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 229940002612 prodrug Drugs 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000005338 substituted cycloalkoxy group Chemical group 0.000 abstract 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente revelación se refiere en general a inhibidores de LRRK2 o una de sus sales, análogos deuterados, profármacos, tautómeros, estereoisómeros farmacéuticamente aceptables o mezcla de sus estereoisómeros y sus métodos de preparación y de uso. Reivindicación 1: Un compuesto de la fórmula (1) o una de sus sales, análogos deuterados, profármacos, estereoisómeros farmacéuticamente aceptables o una mezcla de sus estereoisómeros, caracterizado porque: R¹ es cicloalquilo opcionalmente sustituido; R² es halo, ciano, alquilo C₁₋₆ opcionalmente sustituido, alquenilo C₂₋₆ opcionalmente sustituido, alquinilo C₂₋₆ opcionalmente sustituido, cicloalquilo opcionalmente sustituido, alcoxi C₁₋₆ opcionalmente sustituido, cicloalcoxi opcionalmente sustituido, alquiltio C₁₋₆ opcionalmente sustituido, alquilsulfonilo C₁₋₆ opcionalmente sustituido, -C(O)R¹⁰ o -C(O)N(R¹¹)(R¹²); R³ es alcoxi C₁₋₆ opcionalmente sustituido, cicloalquilo opcionalmente sustituido, cicloalcoxi opcionalmente sustituido, alquiltio C₁₋₆ opcionalmente sustituido, alquil C₁₋₆-sulfonilo opcionalmente sustituido o -N(R¹¹)(R¹²); R⁴ es hidrógeno o halo; R⁵ es heterociclilo opcionalmente sustituido; cada R¹⁰ es independientemente un alquilo C₁₋₆ opcionalmente sustituido o un alcoxi C₁₋₆ opcionalmente sustituido; y R¹¹ y R¹² son cada uno independientemente hidrógeno, alquilo C₁₋₆ opcionalmente sustituido, o cicloalquilo opcionalmente sustituido.The present disclosure relates generally to LRRK2 inhibitors or one of its salts, deuterated analogues, prodrugs, tautomers, pharmaceutically acceptable stereoisomers or mixtures of stereoisomers thereof and their methods of preparation and use. Claim 1: A compound of formula (1) or one of its salts, deuterated analogues, prodrugs, pharmaceutically acceptable stereoisomers or a mixture of stereoisomers thereof, characterized in that: R¹ is optionally substituted cycloalkyl; R² is halo, cyano, optionally substituted C₁₋₆ alkyl, optionally substituted C₂₋₆ alkenyl, optionally substituted C₂₋₆ alkynyl, optionally substituted cycloalkyl, optionally substituted C₁₋₆ alkoxy, optionally substituted cycloalkoxy, optionally substituted C₁₋₆ alkylthio, alkylsulf onyl optionally substituted C₁₋₆, -C(O)R¹⁰ or -C(O)N(R¹¹)(R¹²); R³ is optionally substituted C₁₋₆ alkoxy, optionally substituted cycloalkyl, optionally substituted cycloalkoxy, optionally substituted C₁₋₆ alkylthio, optionally substituted C₁₋₆ alkyl-sulfonyl or -N(R¹¹)(R¹²); R⁴ is hydrogen or halo; R⁵ is optionally substituted heterocyclyl; each R¹⁰ is independently an optionally substituted C₁₋₆ alkyl or an optionally substituted C₁₋₆ alkoxy; and R¹¹ and R¹² are each independently hydrogen, optionally substituted C₁₋₆ alkyl, or optionally substituted cycloalkyl.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662350876P | 2016-06-16 | 2016-06-16 | |
| US202062476581P | 2020-03-24 | 2020-03-24 | |
| US202062510711P | 2020-05-24 | 2020-05-24 | |
| US202062417151P | 2020-11-03 | 2020-11-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR126244A2 true AR126244A2 (en) | 2023-10-04 |
Family
ID=88679249
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP220101667A AR126241A2 (en) | 2016-06-16 | 2022-06-24 | COMPOUNDS, COMPOSITIONS AND METHODS |
| ARP220101670A AR126244A2 (en) | 2016-06-16 | 2022-06-24 | HETEROARYL SUBSTITUTED PYRIMIDINES LRRK2 INHIBITORS FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP220101667A AR126241A2 (en) | 2016-06-16 | 2022-06-24 | COMPOUNDS, COMPOSITIONS AND METHODS |
Country Status (1)
| Country | Link |
|---|---|
| AR (2) | AR126241A2 (en) |
-
2022
- 2022-06-24 AR ARP220101667A patent/AR126241A2/en unknown
- 2022-06-24 AR ARP220101670A patent/AR126244A2/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AR126241A2 (en) | 2023-10-04 |
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