AR083813A1 - Derivados de pirazol aminopirimidina como moduladores de lrrk2 - Google Patents
Derivados de pirazol aminopirimidina como moduladores de lrrk2Info
- Publication number
- AR083813A1 AR083813A1 ARP110104181A ARP110104181A AR083813A1 AR 083813 A1 AR083813 A1 AR 083813A1 AR P110104181 A ARP110104181 A AR P110104181A AR P110104181 A ARP110104181 A AR P110104181A AR 083813 A1 AR083813 A1 AR 083813A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- optionally substituted
- halo
- alkoxy
- Prior art date
Links
- 102000009784 Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 Human genes 0.000 title abstract 2
- 108010020246 Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 Proteins 0.000 title abstract 2
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 35
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 19
- 125000000217 alkyl group Chemical group 0.000 abstract 13
- 125000000623 heterocyclic group Chemical group 0.000 abstract 8
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 7
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 5
- 125000001475 halogen functional group Chemical group 0.000 abstract 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 2
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
-
- 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
- C07D403/02—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 two hetero rings
- C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/14—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 three or more hetero rings
-
- 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
Abstract
También se describen usos de los compuestos para el tratamiento de enfermedades relacionadas con el receptor de LRRK2, tales como la enfermedad de Parkinson.Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en el cual: X es: -NRa- u -O- donde Ra es hidrógeno o alquilo C1-6; R1 es: alquilo C1-6; alquenilo C2-6; alquinilo C2-6; halo-alquilo C1-6; alcoxi C1-6-alquilo C1-6; hidroxi-alquilo C1-6; amino-alquilo C1-6; alquilsulfonilo C1-6-alquilo C1-6; cicloalquilo C3-6, opcionalmente sustituido una o más veces con alquilo C1-6; cicloalquilo C3-6-alquilo C1-6, donde la parte de cicloalquilo C3-6 se sustituye opcionalmente una o más veces con alquilo C1-6; heterociclilo, opcionalmente sustituido una o más veces con R7 o heterociclil-alquilo C1-6, opcionalmente sustituido una o más veces con R7; o X y R1 forman juntos alquilo C1-6; alcoxi C1-6-alquilo C1-6 cicloalquilo C3-6, opcionalmente sustituido una o más veces con R6 o cicloalquilo C3-6-alquilo C1-6, donde la parte de cicloalquilo C3-6 se sustituye opcionalmente una o más veces con R6; o R1 y Ra junto con los átomos a los cuales están unidos pueden formar un anillo heterocíclico de tres a seis miembros, opcionalmente sustituido una o más veces con R7; R2 es: alquilo C1-6; halo; alcoxi C1-6; ciano; alquinilo C2-6; alquenilo C2-6; halo-alquilo C1-6; halo-alcoxi C1-6; cicloalquilo C3-6, opcionalmente sustituido una o más veces con R6; cicloalquilo C3-6-alquilo C1-6, donde la parte de cicloalquilo C3-6 se sustituye opcionalmente una o más veces con R6; -ORb donde Rb es alquilo C1-6, cicloalquilo C3-6, opcionalmente sustituido una o más veces con R6, o cicloalquilo C3-6-alquilo C1-6, donde la parte de cicloalquilo C3-6 se sustituye opcionalmente una o más veces con R6 o -C(O)-Rc donde Rc es alquilo C1-6, alcoxi C1-6, amino, o heterociclilo, opcionalmente sustituido una o más veces con R7; R3 es: hidrógeno; alquilo C1-6; halo-alquilo C1-6; alquenilo C2-6; alquinilo C2-6; hidroxi-alquilo C1-6; alcoxi C1-6-alquilo C1-6; ciano-alquilo C1-6; alquilsulfonilo C1-6; alquilsulfonilo C1-6-alquilo C1-6; amino-alquilo C1-6; cicloalquilo C3-6, opcionalmente sustituido una o más veces con R6; cicloalquilo C3-6-alquilo C1-6, donde la parte de cicloalquilo C3-6 se sustituye opcionalmente una o más veces con R6; cicloalquilo C3-6-sulfonilo, donde la parte de cicloalquilo C3-6 se sustituye opcionalmente una o más veces con R6; heterociclilo, opcionalmente sustituido una o más veces con R7; heterociclil-alquilo C1-6, donde la parte de heterociclilo se sustituye opcionalmente una o más veces con R7; arilo, opcionalmente sustituido una o más veces con R8; aril-alquilo C1-6, donde la parte de arilo se sustituye opcionalmente una o más veces con R8; heteroarilo, opcionalmente sustituido una o más veces con heteroaril-alquilo C1-6, donde la parte de heteroarilo se sustituye opcionalmente una o más veces con R8 o -Y-C(O)-Rd; Y es alquileno C2-6 o una unión; Rd es alquilo C1-6, alcoxi C1-6, amino, alquilo C1-6-amino, di-alquilo C1-6-amino, halo-alquilo C1-6-amino, di-halo-alquilo C1-6-amino, halo-alquilo C1-6, hidroxi-alquilo C1-6, hidroxi, alcoxi C1-6-alquilo C1-6, ciano-alquilo C1-6, alquilsulfonilo C1-6-alquilo C1-6, amino-alquilo C1-6, cicloalquilo C3-6, opcionalmente sustituido una o más veces con R6, cicloalquilo C3-6-alquilo C1-6, donde la parte de cicloalquilo C3-6 se sustituye opcionalmente una o más veces con R6, -heterociclilo, opcionalmente sustituido una o más veces con R7, o heterociclil-alquilo C1-6, donde la parte de heterociclilo se sustituye opcionalmente una o más veces con R7; R4 es: hidrógeno; alquilo C1-6; halo; ciano; halo-alquilo C1-6; alquenilo C2-6; alquinilo C2-6; alcoxi C1-6; alcoxi C1-6-alquilo C1-6; hidroxi-alquilo C1-6; cicloalquilo C3-6, opcionalmente sustituido una o más veces con R6; cicloalquilo C3-6-alquilo C1-6, donde la parte de cicloalquilo C3-6 se sustituye opcionalmente una o más veces con R6 o -Y-C(O)-Rd; R5 es: hidrógeno o alquilo C1-6; cada R6 es, independientemente: alquilo C1-6; halo-alquilo C1-6; alcoxi C1-6; oxo; ciano; halo o Y-C(O)-Rd; cada R7 es, independientemente: alquilo C1-6; halo-alquilo C1-6; halo; oxo; alcoxi C1-6; alquilsulfonilo C1-6; alcoxi C1-6-alquilo C1-6; ciano; -Y-C(O)-Rd; heterociclilo; heterociclil-alquilo C1-6; cicloalquilo C3-6; cicloalquilo C3-6-alquilo C1-6 o cicloalquilo C3-6sulfonilo y cada R8 es independientemente: oxo; alquilo C1-6; halo-alquilo C1-6; halo; alquilo C1-6-sulfonilo; alcoxi C1-6; alcoxi C1-6-alquilo C1-6; ciano; heterociclilo; heterociclil-alquilo C1-6; -Y-C(O)-Rd; cicloalquilo C3-6, cicloalquilo C3-6-alquilo C1-6, o cicloalquilo C3-6-sulfonilo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41227310P | 2010-11-10 | 2010-11-10 | |
| US201161546613P | 2011-10-13 | 2011-10-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR083813A1 true AR083813A1 (es) | 2013-03-27 |
Family
ID=44983512
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110104181A AR083813A1 (es) | 2010-11-10 | 2011-11-09 | Derivados de pirazol aminopirimidina como moduladores de lrrk2 |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US8815882B2 (es) |
| EP (3) | EP2638031B9 (es) |
| JP (3) | JP5986094B2 (es) |
| KR (1) | KR101566091B1 (es) |
| CN (1) | CN103313978B (es) |
| AR (1) | AR083813A1 (es) |
| AU (1) | AU2011328139A1 (es) |
| BR (1) | BR112013011600B1 (es) |
| CA (2) | CA2812669C (es) |
| CY (1) | CY1120073T1 (es) |
| DK (2) | DK3124483T3 (es) |
| EC (1) | ECSP13012611A (es) |
| ES (2) | ES2653967T3 (es) |
| HK (1) | HK1187605A1 (es) |
| HR (2) | HRP20172006T1 (es) |
| HU (2) | HUE046617T2 (es) |
| IL (1) | IL225234A0 (es) |
| LT (2) | LT2638031T (es) |
| MA (1) | MA34644B1 (es) |
| MX (1) | MX2013005199A (es) |
| NO (1) | NO2638031T3 (es) |
| PL (2) | PL2638031T3 (es) |
| PT (2) | PT2638031T (es) |
| RS (2) | RS56583B1 (es) |
| SG (1) | SG189043A1 (es) |
| SI (2) | SI3124483T1 (es) |
| TW (1) | TW201302733A (es) |
| WO (1) | WO2012062783A1 (es) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2837199A1 (en) | 2011-05-23 | 2012-11-29 | Elan Pharmaceuticals, Inc. | Cinnoline compounds as inhibitor of lrrk2 kinase activity |
| US20140228384A1 (en) * | 2011-11-29 | 2014-08-14 | Genentech, Inc. | Assays and biomarkers for lrrk2 |
| WO2013079493A1 (en) | 2011-11-29 | 2013-06-06 | F. Hoffmann-La Roche Ag | Aminopyrimidine derivatives as lrrk2 modulators |
| AR089182A1 (es) | 2011-11-29 | 2014-08-06 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| PL2785711T3 (pl) * | 2011-11-29 | 2017-01-31 | F.Hoffmann-La Roche Ag | Pochodne 2-(fenylo lub piryd-3-ylo)aminopirymidyny jako modulatory kinazy lrrk2 do leczenia choroby parkinsona |
| CN103958498B (zh) * | 2011-11-29 | 2016-09-07 | 霍夫曼-拉罗奇有限公司 | 作为lrrk2调节剂的氨基嘧啶衍生物 |
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| CA2871375C (en) * | 2012-05-03 | 2020-10-27 | F. Hoffmann-La Roche Ag | Pyrazole aminopyrimidine derivatives as lrrk2 modulators for use in the treatment of parkinson's disease |
| KR102091894B1 (ko) * | 2012-05-03 | 2020-03-20 | 제넨테크, 인크. | Lrrk2 조절제로서의 피라졸 아미노피리미딘 유도체 |
| WO2014001973A1 (en) | 2012-06-29 | 2014-01-03 | Pfizer Inc. | NOVEL 4-(SUBSTITUTED-AMINO)-7H-PYRROLO[2,3-d]PYRIMIDINES AS LRRK2 INHIBITORS |
| WO2014060381A1 (de) | 2012-10-18 | 2014-04-24 | Bayer Cropscience Ag | Heterocyclische verbindungen als schädlingsbekämpfungsmittel |
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| US10058559B2 (en) | 2014-05-15 | 2018-08-28 | The United States Of America, As Represented By The Secretary, Department Of Health & Human Services | Treatment or prevention of an intestinal disease or disorder |
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- 2011-11-09 EP EP16180927.2A patent/EP3124483B1/en active Active
- 2011-11-09 WO PCT/EP2011/069696 patent/WO2012062783A1/en active Application Filing
- 2011-11-09 AU AU2011328139A patent/AU2011328139A1/en not_active Abandoned
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- 2011-11-09 CA CA3017869A patent/CA3017869C/en active Active
- 2011-11-09 ES ES16180927T patent/ES2746134T3/es active Active
- 2011-11-09 PL PL16180927T patent/PL3124483T3/pl unknown
- 2011-11-09 TW TW100140970A patent/TW201302733A/zh unknown
- 2011-11-09 SI SI201131772T patent/SI3124483T1/sl unknown
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2013
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2014
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2016
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2017
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2018
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2019
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