AR078171A1 - Dihidrobenzocicloalquiloximetil-oxazolopirimidinonas sustituidas, preparacion y uso de las mismas - Google Patents

Dihidrobenzocicloalquiloximetil-oxazolopirimidinonas sustituidas, preparacion y uso de las mismas

Info

Publication number
AR078171A1
AR078171A1 ARP100103337A ARP100103337A AR078171A1 AR 078171 A1 AR078171 A1 AR 078171A1 AR P100103337 A ARP100103337 A AR P100103337A AR P100103337 A ARP100103337 A AR P100103337A AR 078171 A1 AR078171 A1 AR 078171A1
Authority
AR
Argentina
Prior art keywords
group
hydrogen
same
disorders
fluoroethyl
Prior art date
Application number
ARP100103337A
Other languages
English (en)
Original Assignee
Sanofi Aventis
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of AR078171A1 publication Critical patent/AR078171A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Métodos para preparar estos compuestos, incluyendo nuevos intermedios. Los compuestos son moduladores de receptores metabotropicos de glutamato (mGluR), particularmente, el receptor mGluR2. Agentes farmacéuticos, especialmente en el tratamiento y/o prevencion de una diversidad de trastornos del sistema nervioso central (SNC), incluyendo, pero sin limitacion, afecciones neurodegenerativas agudas y cronicas, psicosis, trastornos por déficits cognitivos, convulsiones, ansiedad, depresion, migrana, dolor, trastornos del sueno y emesis. Reivindicacion 1: Un compuesto de formula (1): donde: n es 1, 2 o 3; R1 se selecciona del grupo que consiste en hidrogeno, metilo, fluorometilo, etilo, 2-fluoroetilo y propilo; R2 se selecciona del grupo que consiste en hidrogeno, metilo, fluorometilo, etilo, 2-fluoroetilo, propilo, 1,1-difluoropropilo, metoximetilo y 2-fluoroetoximetilo; R3 y R4 son iguales o diferentes e independientemente entre sí seleccionados del grupo que consiste en alquilo (C1-4), fenilo y bencilo o R3 y R4 tomados junto con el átomo de carbono al que están unidos forman un anillo carbocíclico C3-7 sustituido o no sustituido y R5 y R6 son iguales o diferentes e independientemente entre sí seleccionados del grupo que consiste en hidrogeno, halogeno, alquilo (C1-4) y alcoxi (C1-4).
ARP100103337A 2009-09-15 2010-09-13 Dihidrobenzocicloalquiloximetil-oxazolopirimidinonas sustituidas, preparacion y uso de las mismas AR078171A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24258609P 2009-09-15 2009-09-15
FR1055806 2010-07-16

Publications (1)

Publication Number Publication Date
AR078171A1 true AR078171A1 (es) 2011-10-19

Family

ID=43003494

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103337A AR078171A1 (es) 2009-09-15 2010-09-13 Dihidrobenzocicloalquiloximetil-oxazolopirimidinonas sustituidas, preparacion y uso de las mismas

Country Status (22)

Country Link
US (1) US9051331B2 (es)
EP (1) EP2477994B1 (es)
JP (1) JP5628320B2 (es)
KR (1) KR101721423B1 (es)
CN (1) CN102498116B (es)
AR (1) AR078171A1 (es)
AU (1) AU2010295802B2 (es)
BR (1) BR112012005736A2 (es)
CA (1) CA2773555C (es)
CO (1) CO6511237A2 (es)
DK (1) DK2477994T3 (es)
ES (1) ES2451348T3 (es)
IL (1) IL218490A (es)
MA (1) MA33659B1 (es)
MX (1) MX2012002725A (es)
NZ (1) NZ598743A (es)
PT (1) PT2477994E (es)
RU (1) RU2543384C2 (es)
SG (1) SG178997A1 (es)
TW (1) TWI495639B (es)
UY (1) UY32888A (es)
WO (1) WO2011034830A1 (es)

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AR059898A1 (es) 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
MX2009009447A (es) 2007-03-09 2009-09-14 Sanofi Aventis Dihidro y tetrahidro oxazolopirimidinonas sustituidas, preparacion y uso de las mismas.
EP2205565B1 (en) 2007-09-14 2013-04-17 Janssen Pharmaceuticals, Inc. 1,3-disubstituted-4-phenyl-1 h-pyridin-2-ones
NZ584145A (en) 2007-09-14 2012-03-30 Ortho Mcneil Janssen Pharm 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h, 1'h-[1,4'] bipyridinyl-2'-ones
ES2439291T3 (es) 2008-09-02 2014-01-22 Janssen Pharmaceuticals, Inc. Derivados de 3-azabiciclo[3.1.0]hexilo como moduladores de receptores de glutamato metabotrópicos
US8697689B2 (en) 2008-10-16 2014-04-15 Janssen Pharmaceuticals, Inc. Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors
MX2011005242A (es) 2008-11-28 2011-09-06 Ortho Mcneil Janssen Pharm Derivados de indol y benzoxazina como moduladores de los receptores de glutamato metabotropicos.
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
MY161325A (en) 2009-05-12 2017-04-14 Janssen Pharmaceuticals Inc 1, 2, 4-triazolo[4,3-a]pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
CA2760259C (en) 2009-05-12 2018-05-01 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
JP5852664B2 (ja) 2010-11-08 2016-02-03 ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド １，２，４−トリアゾロ［４，３−ａ］ピリジン誘導体およびｍＧｌｕＲ２受容体のポジティブアロステリックモジュレーターとしてのそれらの使用
ES2536433T3 (es) 2010-11-08 2015-05-25 Janssen Pharmaceuticals, Inc. Derivados de 1,2,4-triazolo[4,3-a]piridina y su uso como moduladores alostéricos positivos de receptores mGluR2
CN103298809B (zh) 2010-11-08 2016-08-31 杨森制药公司 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途
JP2015006994A (ja) * 2011-10-28 2015-01-15 大正製薬株式会社 ジヒドロイミダゾオキサゾール誘導体
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
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
ME03518B (me) 2014-01-21 2020-04-20 Janssen Pharmaceutica Nv Kombinacije koje obuhvataju pozitivne alosterične modulatore ili ortosterične agoniste metabotropnog glutamatergičnog receptora podtipa 2 i njihova primjena
WO2015110435A1 (en) 2014-01-21 2015-07-30 Janssen Pharmaceutica Nv Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use

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Also Published As

Publication number Publication date
MA33659B1 (fr) 2012-10-01
KR20120068005A (ko) 2012-06-26
CN102498116B (zh) 2014-08-06
EP2477994A1 (en) 2012-07-25
KR101721423B1 (ko) 2017-03-30
IL218490A (en) 2015-05-31
ES2451348T3 (es) 2014-03-26
CN102498116A (zh) 2012-06-13
TW201121977A (en) 2011-07-01
US9051331B2 (en) 2015-06-09
NZ598743A (en) 2013-02-22
JP5628320B2 (ja) 2014-11-19
TWI495639B (zh) 2015-08-11
RU2543384C2 (ru) 2015-02-27
AU2010295802A1 (en) 2012-04-05
BR112012005736A2 (pt) 2016-03-08
SG178997A1 (en) 2012-04-27
AU2010295802B2 (en) 2014-09-11
WO2011034830A1 (en) 2011-03-24
IL218490A0 (en) 2012-04-30
PT2477994E (pt) 2014-03-13
US20120184566A1 (en) 2012-07-19
CA2773555C (en) 2014-01-28
JP2013504622A (ja) 2013-02-07
EP2477994B1 (en) 2013-12-11
CO6511237A2 (es) 2012-08-31
RU2012114602A (ru) 2013-10-27
MX2012002725A (es) 2013-05-28
DK2477994T3 (en) 2014-03-17
CA2773555A1 (en) 2011-03-24
UY32888A (es) 2011-04-29

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