AR037682A1 - Derivados de acetileno que tienen actividad antagonista para receptores glutamato metabotropico humanos, composicion farmaceutica, una combinacion y el uso de dichos derivados para la fabricacion de composiciones farmaceuticas - Google Patents

Derivados de acetileno que tienen actividad antagonista para receptores glutamato metabotropico humanos, composicion farmaceutica, una combinacion y el uso de dichos derivados para la fabricacion de composiciones farmaceuticas

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Publication number
AR037682A1
AR037682A1 ARP020104641A ARP020104641A AR037682A1 AR 037682 A1 AR037682 A1 AR 037682A1 AR P020104641 A ARP020104641 A AR P020104641A AR P020104641 A ARP020104641 A AR P020104641A AR 037682 A1 AR037682 A1 AR 037682A1
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Argentina
Prior art keywords
hydrogen
alkyl
derivatives
pharmaceutical composition
manufacture
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ARP020104641A
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English (en)
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Novartis Ag
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Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR037682A1 publication Critical patent/AR037682A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
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    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • 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
    • A61P25/24—Antidepressants
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    • 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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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/23—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
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    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Derivados de acetileno que comprenden un compuesto de la fórmula general (1) en la que: m es 0 o 1; n es 0 o 1; y A es hidroxi; X es hidrógeno y Y es hidrógeno o A forma una ligadura simple con X o con Y; R0 es hidrógeno, alquilo de C1-4. Alcoxi de C1-4, trifluorometilo, halógeno, ciano, nitro, -COOR1; donde R1 es alquilo de C1-4, o -COR2, donde R2 es hidrógeno o alquilo C1-4; y R es -COR3, COOR3, -CONR4R5 o -SO2R6; donde R3 es alquilo de C1-4, cicloalquilo de C3-7 o fenilo opcionalmente sustituido, 2-piridilo o 2-tienilo; R4 y R5, independientemente son hidrógeno o alquilo de C1-4 y R6 es alquilo de C1-4, cicloalquilo de C3-7 o fenilo opcionalmente sustituido; R´ es hidrógeno o alquilo de C1-4 y R´´ es hidrógeno o alquilo de C1-4; o R´ y R´´ forman juntos Un grupo -CH2(CH2)p-; donde p es 0, 1, o 2; en cuyo caso uno de n y p es diferente de 0; a condición de que R0 sea diferente de hidrógeno, trifluorometilo y metoxi cuando m es 1, n es 0, A es hidroxi, X e Y son ambos hidrógeno, R es COOEt y R´ y R´´ forman un grupo -(CH2)2-; en forma de base libre o de una sal de adición de ácido. Los compuestos de la fórmula (1) son útiles como productos farmacéuticos. Un proceso para su preparación, una composición farmacéutica y el uso de dicho compuesto para la fabricación de una composición farmacéutica destinada al tratamiento de trastornos del sistema nervioso, asociados con irregularidades de la transmisión de la senal glutamatérgica y trastornos mediados total o parcialmente por mGluR5 y una combinación.
ARP020104641A 2001-12-04 2002-12-02 Derivados de acetileno que tienen actividad antagonista para receptores glutamato metabotropico humanos, composicion farmaceutica, una combinacion y el uso de dichos derivados para la fabricacion de composiciones farmaceuticas AR037682A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0128996.6A GB0128996D0 (en) 2001-12-04 2001-12-04 Organic compounds

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AR037682A1 true AR037682A1 (es) 2004-12-01

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ID=9926969

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP020104641A AR037682A1 (es) 2001-12-04 2002-12-02 Derivados de acetileno que tienen actividad antagonista para receptores glutamato metabotropico humanos, composicion farmaceutica, una combinacion y el uso de dichos derivados para la fabricacion de composiciones farmaceuticas
ARP120104356A AR088921A2 (es) 2001-12-04 2012-11-20 PROCESO PARA LA PREPARACION DE DERIVADOS DE ACETILENO QUE TIENEN ACTIVIDAD ANTAGONISTA mGluR5, COMPOSICIONES Y USO DE LOS COMPUESTOS

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ARP120104356A AR088921A2 (es) 2001-12-04 2012-11-20 PROCESO PARA LA PREPARACION DE DERIVADOS DE ACETILENO QUE TIENEN ACTIVIDAD ANTAGONISTA mGluR5, COMPOSICIONES Y USO DE LOS COMPUESTOS

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US (4) US7348353B2 (es)
EP (1) EP1453512B8 (es)
JP (2) JP4176020B2 (es)
KR (2) KR100980901B1 (es)
CN (2) CN100430059C (es)
AR (2) AR037682A1 (es)
AT (1) ATE327755T1 (es)
AU (1) AU2002358585B2 (es)
BR (1) BR0214666A (es)
CA (1) CA2466560C (es)
CO (1) CO5590929A2 (es)
CY (1) CY1105460T1 (es)
DE (1) DE60211944T2 (es)
DK (1) DK1453512T3 (es)
EC (1) ECSP045139A (es)
EG (1) EG24936A (es)
ES (1) ES2263842T3 (es)
GB (1) GB0128996D0 (es)
HK (1) HK1071510A1 (es)
HU (1) HU229429B1 (es)
IL (1) IL161990A0 (es)
MX (1) MXPA04005456A (es)
MY (1) MY137774A (es)
NO (1) NO327005B1 (es)
NZ (1) NZ533266A (es)
PE (1) PE20030640A1 (es)
PL (1) PL212996B1 (es)
PT (1) PT1453512E (es)
RU (1) RU2341515C2 (es)
TW (1) TWI328578B (es)
WO (1) WO2003047581A1 (es)
ZA (1) ZA200403713B (es)

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