AR054000A1 - Compuesto de n-(fenilpropil)-sulfonamida, composicion farmaceutica que lo comprende, su uso para la fabricacion de un medicamento, producto de combinacion que comprende dicho compuesto y metodo para prepararlo - Google Patents

Compuesto de n-(fenilpropil)-sulfonamida, composicion farmaceutica que lo comprende, su uso para la fabricacion de un medicamento, producto de combinacion que comprende dicho compuesto y metodo para prepararlo

Info

Publication number
AR054000A1
AR054000A1 ARP060100542A ARP060100542A AR054000A1 AR 054000 A1 AR054000 A1 AR 054000A1 AR P060100542 A ARP060100542 A AR P060100542A AR P060100542 A ARP060100542 A AR P060100542A AR 054000 A1 AR054000 A1 AR 054000A1
Authority
AR
Argentina
Prior art keywords
compound
alkyl
halogen
formula
alkoxy
Prior art date
Application number
ARP060100542A
Other languages
English (en)
Original Assignee
Glaxo Group Ltd
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
Priority claimed from GB0503155A external-priority patent/GB0503155D0/en
Priority claimed from GB0601612A external-priority patent/GB0601612D0/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of AR054000A1 publication Critical patent/AR054000A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • 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
    • A61P25/18—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
    • A61P25/28—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/42—Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/65—One oxygen atom attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/58—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20—Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms

Abstract

Un compuesto de N-(fenilpropil)-sulfonamida que tiene la formula (1), o una de sus sales o solvatos en la que, R1 se selecciona de alquilo C1-6, halogeno-alquilo C1-6, alquenilo C2-6, amino, mono-alquil(C1-4)amino y di-alquil(C1-4)amino; R2, R3 y R6, que puede ser iguales o diferentes, se selecciona cada uno independientemente de H, halogeno, alquilo C1-6, halogenoalquilo C1-6 y alcoxi C1-4; cada R4, que pueden ser iguales o diferentes, se selecciona de alquilo C1-6, halogeno, halogenoalquilo C1-6, alcoxi C1-4, halogeno-alcoxi C1-4 y ciano; p se selecciona de 0, 1 y 2; y R5 es fenilo o un heterociclilo aromático, cualquiera de los cuales está opcionalmente sustituido con uno o más grupos Y; cada grupo Y se selecciona independientemente del grupo que consiste en: alquilo C1-6, halogeno, halogenoalquilo C1-6, alcoxi C1-4, halogenoalcoxi C1-4, ciano, -(CH2)qNR5aSO2R5b, -(CH2)qNR5a(C=O)R5d, -(CH2)qNR5a(C=O)N(R5c)2, -(CH2)q(C=O)R5d, -(CH2)qSO2R5b; donde R5a y cada R5c, que pueden ser iguales o diferentes, se selecciona de H y alquilo C1-6; R5b se selecciona de alquilo C1-6 y halogenoalquilo C1-6; R5d se selecciona de alquiloc1-*6, alcoxi C1-4 y halogenoalquilo C1-6; o R5a y R5b, R5a y R5c, o R5a y R5d, cuando sea adecuado, junto con los átomos conectores pueden formar un anillo de 5 o 6 miembros; y q es 0, 1 o 2; en el caso en el que hay dos o más grupos Y presentes, dos de ellos juntos pueden formar un grupo cíclico seleccionado de -(CH2)rOR5eO(CH2)s- y -(CH2)tOR5e- donde R5e es un grupo seleccionado de alquileno C1-4 o halogenoalquileno C1-4; r y s son cada uno independientemente 0, 1 o 2, y t es 2 o 3. Composicion farmacéutica que comprende un compuesto de formula (1), y al menos un vehículo o diluyente farmacéuticamente aceptables. Uso del compuesto para la fabricacion de un medicamento para tratar o prevenir una enfermedad o una afeccion causadas por una reduccion o desequilibrio en la funcion del receptor de glutamato. Producto de combinacion que comprende un compuesto de formula (1), o una de sus sales o solvatos, con un antipsicotico. Método para prepara dicho compuesto. Reivindicacion 22: Un método para preparar un compuesto de acuerdo con una cualquiera de las reivindicaciones 1 a 13, caracterizado porque comprende: a) acoplar un compuesto de formula (2) donde X es un grupo lábil tal como halogeno (por ejemplo Cl, Br o I) con un derivado de ácido boronico de formula (3); o b) acoplar un compuesto de boronato de formula (4) con un compuesto R5-X donde X es un grupo lábil tal como halogeno (por ejemplo Br o I) y después opcionalmente preparar una sal o solvato del producto. Reivindicacion 24: Un método para preparar un compuesto segun una cualquiera de las reivindicaciones 1 a 13 en forma quiral, caracterizado porque comprende la etapa de epoxidar estereoselectivamente un estireno (X) adecuado, donde X es un grupo lábil tal como halogeno (por ejemplo Cl, Br o I),seguido de la transformacion del producto de la epoxidacion en un compuesto de la presente.
ARP060100542A 2005-02-15 2006-02-15 Compuesto de n-(fenilpropil)-sulfonamida, composicion farmaceutica que lo comprende, su uso para la fabricacion de un medicamento, producto de combinacion que comprende dicho compuesto y metodo para prepararlo AR054000A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0503155A GB0503155D0 (en) 2005-02-15 2005-02-15 Novel compounds
GB0601612A GB0601612D0 (en) 2006-01-26 2006-01-26 Compounds

Publications (1)

Publication Number Publication Date
AR054000A1 true AR054000A1 (es) 2007-05-30

Family

ID=36253489

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060100542A AR054000A1 (es) 2005-02-15 2006-02-15 Compuesto de n-(fenilpropil)-sulfonamida, composicion farmaceutica que lo comprende, su uso para la fabricacion de un medicamento, producto de combinacion que comprende dicho compuesto y metodo para prepararlo

Country Status (8)

Country Link
US (1) US7790758B2 (es)
EP (1) EP1848695B1 (es)
JP (1) JP2008530162A (es)
AR (1) AR054000A1 (es)
AT (1) ATE517867T1 (es)
PE (1) PE20061127A1 (es)
TW (1) TW200640863A (es)
WO (1) WO2006087169A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4691669B2 (ja) 2007-08-22 2011-06-01 アストラゼネカ・アクチエボラーグ シクロプロピルアミド誘導体
TW201039825A (en) 2009-02-20 2010-11-16 Astrazeneca Ab Cyclopropyl amide derivatives 983
TWI520945B (zh) * 2010-02-18 2016-02-11 阿斯特捷利康公司 環丙基苯甲醯胺衍生物之新穎結晶形式
WO2013055386A2 (en) 2011-10-03 2013-04-18 The University Of Utah Research Foundation Application of 5-ht6 receptor antagonists for the alleviation of cognitive deficits of down syndrome
SG11201406274VA (en) * 2012-04-27 2014-11-27 Glaxo Group Ltd Novel compounds
US8633182B2 (en) 2012-05-30 2014-01-21 Boehringer Ingelheim International Gmbh Indanyloxyphenylcyclopropanecarboxylic acids
EP3311842A1 (en) 2013-06-13 2018-04-25 VeroScience LLC Compositions and methods for treating metabolic disorders
US10538490B2 (en) 2016-10-25 2020-01-21 Boehringer Ingelheim International Gmbh Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
WO2018095877A1 (en) 2016-11-28 2018-05-31 Boehringer Ingelheim International Gmbh Indanylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
WO2018138029A1 (en) 2017-01-26 2018-08-02 Boehringer Ingelheim International Gmbh Benzyloxypyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
US10919859B2 (en) 2017-01-26 2021-02-16 Boehringer Ingelheim International Gmbh Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
EP3573965B1 (en) 2017-01-26 2021-06-23 Boehringer Ingelheim International GmbH Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
WO2018138028A1 (en) 2017-01-26 2018-08-02 Boehringer Ingelheim International Gmbh Benzylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
US10603317B2 (en) 2017-01-26 2020-03-31 Boehringer Ingelheim International Gmbh Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1276153B1 (it) * 1995-11-17 1997-10-27 Roberto Pellicciari Derivati di glicina ad attivita' antagonista dei recettori metabotropi del glutammato
GB9702194D0 (en) * 1997-02-04 1997-03-26 Lilly Co Eli Sulphonide derivatives
ZA200605247B (en) * 2003-12-15 2007-10-31 Japan Tobacco Inc N-substituted-n-sulfonylaminocyclopropane compounds and pharmaceutical use thereof
AU2004299455A1 (en) * 2003-12-15 2005-06-30 Japan Tobacco Inc. Cyclopropane compounds and pharmaceutical use thereof
EP1786769A1 (en) * 2004-08-09 2007-05-23 Glaxo Group Limited Compounds which potentiate glutamate receptor and uses thereof in medicine

Also Published As

Publication number Publication date
ATE517867T1 (de) 2011-08-15
US20080167351A1 (en) 2008-07-10
EP1848695A1 (en) 2007-10-31
TW200640863A (en) 2006-12-01
WO2006087169A1 (en) 2006-08-24
PE20061127A1 (es) 2006-10-21
US7790758B2 (en) 2010-09-07
EP1848695B1 (en) 2011-07-27
JP2008530162A (ja) 2008-08-07

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