AR101392A1 - COMPUESTOS DE 6,7-DIHIDROPIRAZOLO[1,5-A]PIRAZIN-4(5H)-ONA Y SU USO COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE RECEPTORES mGluR2 - Google Patents
COMPUESTOS DE 6,7-DIHIDROPIRAZOLO[1,5-A]PIRAZIN-4(5H)-ONA Y SU USO COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE RECEPTORES mGluR2Info
- Publication number
- AR101392A1 AR101392A1 ARP150102461A ARP150102461A AR101392A1 AR 101392 A1 AR101392 A1 AR 101392A1 AR P150102461 A ARP150102461 A AR P150102461A AR P150102461 A ARP150102461 A AR P150102461A AR 101392 A1 AR101392 A1 AR 101392A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- monohalo
- polyhalo
- nrr
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 102100036837 Metabotropic glutamate receptor 2 Human genes 0.000 title 1
- 108010038421 metabotropic glutamate receptor 2 Proteins 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 42
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000001475 halogen functional group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 3
- -1 2-pyridinyl Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 125000003566 oxetanyl group Chemical group 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
Classifications
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- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- 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
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring 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
- A61K31/495—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
- A61P25/24—Antidepressants
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- 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
- C07D487/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic 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)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1) o una forma estereoisomérica del mismo, en donde R¹ es fenilo o 2-piridinilo, cada uno opcionalmente sustituido por uno o más sustituyentes seleccionados cada uno independientemente del grupo que consiste en halo, alquilo C₁₋₄, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -alquil C₁₋₄-OH, -CN, -alquil C₁₋₄-O-alquilo C₁₋₄, cicloalquilo C₁₋₄, -O-alquilo C₁₋₄, monohalo-alquil C₁₋₄oxi, polihalo-alquil C₁₋₄oxi, SF₅, alquil C₁₋₄tio, monohalo-alquil C₁₋₄tio y polihalo-alquil C₁₋₄tio; R² se selecciona del grupo que consiste en hidrógeno; alquilo C₁₋₄; cicloalquilo C₃₋₇; Het¹; arilo; -C(O)R⁵; -C(O)Het²; Het²; y alquilo C₁₋₄ sustituido por uno o más sustituyentes seleccionados cada uno independientemente del grupo que consiste en halo, cicloalquilo C₃₋₇, arilo, Het¹ y Het²; en donde R⁵ se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₄ y cicloalquilo C₃₋₇; arilo es fenilo opcionalmente sustituido por uno o más sustituyentes seleccionados cada uno independientemente del grupo que consiste en halo, alquilo C₁₋₄, -alquil C₁₋₄-OH, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -CN, -O-alquilo C₁₋₄, -OH, alquil C₁₋₄-O-alquilo C₁₋₄, -NRR, -NHC(O)alquilo C₁₋₄, -C(O)NRR, -C(O)NH[C(O)alquil C₁₋₄], -S(O)₂NRR, -S(O)₂NH[C(O)alquil C₁₋₄] y -SO₂-alquilo C₁₋₄; Het¹ se selecciona del grupo que consiste en oxetanilo, tetrahidrofuranilo y tetrahidropiranilo; Het² es (a) un sustituyente heterociclilo aromático de 6 miembros que se selecciona del grupo que consiste en piridinilo, pirimidinilo, pirazinilo y piridazinilo, cada uno de los cuales puede sustituirse opcionalmente con uno o más sustituyentes seleccionados cada uno independientemente del grupo que consiste en halo, alquilo C₁₋₄, -alquil C₁₋₄-OH, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -CN, -O-alquilo C₁₋₄, -OH, -alquil C₁₋₄-O-alquilo C₁₋₄, -NRR, -NHC(O)alquilo C₁₋₄, -C(O)NRR, -C(O)NH[C(O)alquil C₁₋₄], -S(O)₂NRR, -S(O)₂NH[C(O)alquil C₁₋₄] y -SO₂-alquilo C₁₋₄; o (b) un heterociclilo aromático de 5 miembros que se selecciona del grupo que consiste en tiazolilo, oxazolilo, 1H-pirazolilo y 1H-imidazolilo, cada uno de los cuales puede sustituirse opcionalmente con uno o más sustituyentes seleccionados cada una independientemente del grupo que consiste en halo, alquilo C₁₋₄, -alquil C₁₋₄-OH, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -CN, -O-alquilo C₁₋₄, -OH, -alquil C₁₋₄-O-alquilo C₁₋₄, -NRR, -NHC(O)alquilo C₁₋₄, -C(O)NRR, -C(O)NH[C(O)alquil C₁₋₄], -S(O)₂NRR, -S(O)₂NH[C(O)alquil C₁₋₄] y -SO₂-alquilo C₁₋₄; cada R y R se selecciona independientemente de hidrógeno y alquilo C₁₋₄; y R³ se selecciona de hidrógeno y alquilo C₁₋₄; R⁴ se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₄, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -alquil C₁₋₄-O-alquilo C₁₋₄ y -alquil C₁₋₄-OH; o un N-óxido, o una sal farmacéuticamente aceptable o un solvato del mismo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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EP14179598 | 2014-08-01 |
Publications (1)
Publication Number | Publication Date |
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AR101392A1 true AR101392A1 (es) | 2016-12-14 |
Family
ID=51257437
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP150102461A AR101392A1 (es) | 2014-08-01 | 2015-07-31 | COMPUESTOS DE 6,7-DIHIDROPIRAZOLO[1,5-A]PIRAZIN-4(5H)-ONA Y SU USO COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE RECEPTORES mGluR2 |
Country Status (33)
Country | Link |
---|---|
US (3) | US10005786B2 (es) |
EP (1) | EP3177623B1 (es) |
JP (1) | JP6662846B2 (es) |
KR (1) | KR102531689B1 (es) |
CN (1) | CN106573936B (es) |
AR (1) | AR101392A1 (es) |
AU (1) | AU2015295298B2 (es) |
BR (1) | BR112017001726A2 (es) |
CA (1) | CA2954093C (es) |
CL (1) | CL2017000192A1 (es) |
CY (1) | CY1121649T1 (es) |
DK (1) | DK3177623T3 (es) |
EA (1) | EA031087B1 (es) |
ES (1) | ES2708215T3 (es) |
HR (1) | HRP20181997T1 (es) |
HU (1) | HUE042871T2 (es) |
IL (1) | IL250298A0 (es) |
JO (1) | JOP20150179B1 (es) |
LT (1) | LT3177623T (es) |
MA (1) | MA39582B1 (es) |
ME (1) | ME03320B (es) |
MX (1) | MX2017001452A (es) |
NZ (1) | NZ728122A (es) |
PH (1) | PH12017500161A1 (es) |
PL (1) | PL3177623T3 (es) |
PT (1) | PT3177623T (es) |
RS (1) | RS58279B1 (es) |
SG (1) | SG11201700638YA (es) |
SI (1) | SI3177623T1 (es) |
TR (1) | TR201901074T4 (es) |
TW (1) | TWI696624B (es) |
WO (1) | WO2016016380A1 (es) |
ZA (1) | ZA201700759B (es) |
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CN109999033B (zh) | 2014-01-21 | 2022-12-23 | 詹森药业有限公司 | 包括代谢型谷氨酸能受体亚型2的正别构调节物或正位激动剂的组合及其用途 |
KR20200126026A (ko) | 2014-01-21 | 2020-11-05 | 얀센 파마슈티카 엔.브이. | 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도 |
JOP20150177B1 (ar) * | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
JOP20150179B1 (ar) * | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
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JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
JO3601B1 (ar) | 2014-08-01 | 2020-07-05 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
JOP20150177B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
WO2016016383A1 (en) | 2014-08-01 | 2016-02-04 | Janssen Pharmaceutica Nv | 6,7-DIHYDROPYRAZOLO[1,5-α]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
WO2016016382A1 (en) | 2014-08-01 | 2016-02-04 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors |
JOP20150179B1 (ar) * | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
US10967078B2 (en) | 2014-12-03 | 2021-04-06 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2 PET ligands |
US10072014B2 (en) | 2014-12-03 | 2018-09-11 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of MGLUR2 receptors |
EA037941B1 (ru) | 2015-12-18 | 2021-06-09 | Янссен Фармацевтика Нв | ЛИГАНДЫ mGluR2/3 ДЛЯ PET, МЕЧЕННЫЕ РАДИОАКТИВНЫМИ ИЗОТОПАМИ |
PL3389727T3 (pl) | 2015-12-18 | 2021-02-08 | Janssen Pharmaceutica Nv | RADIOZNAKOWANE LIGANDY mGluR2/3 DO PET |
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