AR028776A1 - DERIVATIVES OF PYRIMIDINE AND ITS USE FOR PROFILAXIS AND THERAPY OF CEREBRAL ISCHEMIA - Google Patents

DERIVATIVES OF PYRIMIDINE AND ITS USE FOR PROFILAXIS AND THERAPY OF CEREBRAL ISCHEMIA

Info

Publication number
AR028776A1
AR028776A1 ARP010103154A ARP010103154A AR028776A1 AR 028776 A1 AR028776 A1 AR 028776A1 AR P010103154 A ARP010103154 A AR P010103154A AR P010103154 A ARP010103154 A AR P010103154A AR 028776 A1 AR028776 A1 AR 028776A1
Authority
AR
Argentina
Prior art keywords
radical
group
trifluoromethyl
nitro
amino
Prior art date
Application number
ARP010103154A
Other languages
Spanish (es)
Original Assignee
Knoll Ag
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 Knoll Ag filed Critical Knoll Ag
Publication of AR028776A1 publication Critical patent/AR028776A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems

Landscapes

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

Abstract

Un derivado de pirimidina de la formula 1 donde A es oxígeno, B es hidrogeno o metilo, D y E son juntos -CH2CH2-F-CH2-, -CH2-F-CH2- o -CH2-F-CH2-CH2-, donde un grupo CH2 puede estar reemplazado con una funcion carbonilo si F es un grupo metileno, F es un grupo metileno, oxígeno, azufre, un grupo -(O=S)-, o un radical NR1, donde R1 es un cicloalquilo C1-5 o un radical cicloalquilmetilo o un radical sulfonilo o un radical alquilsulfonilo C2-4 que lleva un radical alquilo C1-4 o un grupo fenilo, que puede estar sustituido por fluor, cloro, metilo, trifluorometilo, nitro o amino, en el átomo de azufre. X es nitrogeno, Y es CH2,CH2-CH2, CH2-CH2-CH2, o CH2-CH, Z es un nitrogeno, carbono o CH, donde el enlace entre Y y Z también puede ser un doble enlace, n es el numero 2, 3 o 4, R2 es un grupo fenilo, piridilo, pirimidinilo o pirazinilo que puede estar monosustituido o disustituido por halogeno, alquilo C1-4, trifluorometilo, trifluormetoxi, hidroxilo, alcoxi C1-4, alquiltio C1-4, amino, monometilamino, dimetilamino, ciano o nitro y puede estar fusionado con un nucleo de benceno, que puede estar monosustituido o disustituido por halogeno, alquilo C1-4, hidroxilo, trifluorometilo, alcoxi C1-4, amino, ciano o nitro y puede contener 1 átomo de nitrogeno , o con un anillo de 5 o 6 miembros que puede contener de 1 a 2 átomos de oxígeno y las sales fisiologicamente toleradas de ellos. Uso de los compuestos de formula (1) para producir drogas para la profilaxis y la terapia de la neurodegeneracion, el trauma cerebral, la isquemia cerebral, la isquemia cerebral y ataque apoplético y también las secuelas producidas por estas enfermedades.A pyrimidine derivative of formula 1 wherein A is oxygen, B is hydrogen or methyl, D and E are together -CH2CH2-F-CH2-, -CH2-F-CH2- or -CH2-F-CH2-CH2-, where a CH2 group can be replaced with a carbonyl function if F is a methylene group, F is a methylene group, oxygen, sulfur, a group - (O = S) -, or an NR1 radical, where R1 is a C1- cycloalkyl 5 or a cycloalkylmethyl radical or a sulfonyl radical or a C2-4 alkylsulfonyl radical bearing a C1-4 alkyl radical or a phenyl group, which may be substituted by fluorine, chlorine, methyl, trifluoromethyl, nitro or amino, in the atom of sulfur. X is nitrogen, Y is CH2, CH2-CH2, CH2-CH2-CH2, or CH2-CH, Z is a nitrogen, carbon or CH, where the bond between Y and Z can also be a double bond, n is the number 2, 3 or 4, R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which may be monosubstituted or substituted by halogen, C1-4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-4 alkoxy, C1-4 alkylthio, amino, monomethylamino , dimethylamino, cyano or nitro and may be fused with a benzene nucleus, which may be monosubstituted or substituted by halogen, C1-4 alkyl, hydroxyl, trifluoromethyl, C1-4 alkoxy, amino, cyano or nitro and may contain 1 atom of nitrogen, or with a 5 or 6-membered ring that may contain 1 to 2 oxygen atoms and the physiologically tolerated salts thereof. Use of the compounds of formula (1) to produce drugs for the prophylaxis and therapy of neurodegeneration, brain trauma, cerebral ischemia, cerebral ischemia and apopletic attack and also the sequelae produced by these diseases.

ARP010103154A 2000-07-03 2001-07-02 DERIVATIVES OF PYRIMIDINE AND ITS USE FOR PROFILAXIS AND THERAPY OF CEREBRAL ISCHEMIA AR028776A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10031390A DE10031390A1 (en) 2000-07-03 2000-07-03 Pyrimidine derivatives and their use for the prophylaxis and therapy of cerebral ischemia

Publications (1)

Publication Number Publication Date
AR028776A1 true AR028776A1 (en) 2003-05-21

Family

ID=7647039

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010103154A AR028776A1 (en) 2000-07-03 2001-07-02 DERIVATIVES OF PYRIMIDINE AND ITS USE FOR PROFILAXIS AND THERAPY OF CEREBRAL ISCHEMIA

Country Status (4)

Country Link
AR (1) AR028776A1 (en)
AU (1) AU2001279709A1 (en)
DE (1) DE10031390A1 (en)
WO (1) WO2002002568A1 (en)

Families Citing this family (18)

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Publication number Priority date Publication date Assignee Title
TWI417095B (en) 2006-03-15 2013-12-01 Janssen Pharmaceuticals Inc 1,4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of mglur2-receptors
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
CN101801951B (en) 2007-09-14 2013-11-13 杨森制药有限公司 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h, 1'h-[1, 4'] bipyridinyl-2'-ones
ES2439291T3 (en) 2008-09-02 2014-01-22 Janssen Pharmaceuticals, Inc. 3-Azabicyclo [3.1.0] hexyl derivatives as modulators of metabotropic glutamate receptors
US8691813B2 (en) 2008-11-28 2014-04-08 Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
AU2009329879A1 (en) 2008-12-23 2011-08-11 President And Fellows Of Harvard College Small molecule inhibitors of necroptosis
MX2011011962A (en) 2009-05-12 2012-02-28 Janssen Pharmaceuticals Inc 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors.
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
ME01573B (en) 2009-05-12 2014-09-20 Addex Pharma Sa 1,2,4-triazolo[4,3-a]pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
AU2011328195B2 (en) 2010-11-08 2015-04-02 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
US9271967B2 (en) 2010-11-08 2016-03-01 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
JP5852666B2 (en) 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-Triazolo [4,3-a] pyridine derivatives and their use as positive allosteric modulators of the mGluR2 receptor
US9725452B2 (en) 2013-03-15 2017-08-08 Presidents And Fellows Of Harvard College Substituted indoles and pyrroles as RIP kinase inhibitors
JO3368B1 (en) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
JO3367B1 (en) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv 1,2,4-TRIAZOLO[4,3-a]PYRIDINE COMPOUNDS AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
PL3096790T3 (en) 2014-01-21 2020-01-31 Janssen Pharmaceutica, N.V. Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use
KR20200036063A (en) 2014-01-21 2020-04-06 얀센 파마슈티카 엔.브이. Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8810748D0 (en) * 1988-05-06 1988-06-08 Beecham Wuelfing Gmbh & Co Kg Novel treatment
DE19636769A1 (en) * 1996-09-10 1998-03-12 Basf Ag 3-Substituted pyrido [4 ', 3': 4,5] thieno [2,3-d] pyrimidine derivatives, their preparation and use
DE19900545A1 (en) * 1999-01-11 2000-07-13 Basf Ag Use of pyrimidine derivatives for the prophylaxis and therapy of cerebral ischemia

Also Published As

Publication number Publication date
DE10031390A1 (en) 2002-01-17
AU2001279709A1 (en) 2002-01-14
WO2002002568A1 (en) 2002-01-10

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