AR042656A1 - DERIVATIVES OF 1,2, 4- - TRIAMINOBENCEN USED FOR THE TREATMENT OF DISORDERS IN THE CENTRAL NERVOUS SYSTEM - Google Patents

DERIVATIVES OF 1,2, 4- - TRIAMINOBENCEN USED FOR THE TREATMENT OF DISORDERS IN THE CENTRAL NERVOUS SYSTEM

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Publication number
AR042656A1
AR042656A1 ARP030104782A ARP030104782A AR042656A1 AR 042656 A1 AR042656 A1 AR 042656A1 AR P030104782 A ARP030104782 A AR P030104782A AR P030104782 A ARP030104782 A AR P030104782A AR 042656 A1 AR042656 A1 AR 042656A1
Authority
AR
Argentina
Prior art keywords
ilo
alkyl
cycloalkyl
aryl
hydroxy
Prior art date
Application number
ARP030104782A
Other languages
Spanish (es)
Original Assignee
Lundbeck & Co As H
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=35295526&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR042656(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Lundbeck & Co As H filed Critical Lundbeck & Co As H
Publication of AR042656A1 publication Critical patent/AR042656A1/en

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Classifications

    • 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
    • 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
    • C07D333/26—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 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
    • C07D333/28—Halogen 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
    • C07D333/26—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 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
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/32—Oxygen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Reivindicación 1: Un derivado de 1,2,4-triaminobenceno de fórmula (1) donde: R1 se selecciona entre el grupo que consiste en H, alqu(en/in)ilo-C1-6, cicloalqu(en)ilo C3-8, cicloalqu(en)il C3-8-alqu(en7in)ilo C1-6, acilo, hidroxi-alqu(en/in)ilo- C1-6 e hidroxi-cicloalqu(en)ilo-C3-8; R2 y R2´ se seleccionan independientemente entre el grupo que consiste en H, alqu(en/in)ilo- C1-6, cicloalqu(en)ilo- C3-8, arilo, cicloalq(en)ilo- C3-8-alqu(en/in)ilo-C1-6, aril-alqu(en/in)ilo-C1-6, acilo, hidroxi-alqu(en/in)ilo C1-6 e hidroxi-cicloalqu(en)ilo-C3-8; R3 se selecciona entre el grupo que consiste en H, alqu(en/in)ilo C1-6, cicloalqu(en)ilo-C3-8, arilo, cicloalqu(en)il-C3-8-alqu(en/in)ilo-C1-6, aril-alqu(en/in)ilo-C1-6, hidroxi-alqu(en/in)ilo- C1-6, aril-cicloalqu(en)ilo-C3-8, NR10R10´--alqu(en/in)ilo C1-6, NR10R10´-cicloalqu(en)ilo-C3-8 e hidroxi-cicloalqu(en)ilo- C3-8; donde R10 y R10´ se seleccionan independientemente entre el grupo que consiste en H, alqu(en/in)ilo-C1-6, cicloalqu(en)ilo-C3-8, cicloalqu(en)il C3-8-alqu(en/in)ilo C1-6, hidroxi-alqu(en/in)ilo-C1-6, hidroxi-cicloalqu(en)ilo-C3-8, hidroxi-cicloalqu(en)il-C3-8-alqu(en/in)ilo-C1-6, halo-alqu(en/in)ilo-C1-6, halo-cicloalqu(en)ilo-C3-8, halo-cicloalqu(en)il-C3-8-alqu(en/in)ilo-C1-6, ciano-alqu(en/in)ilo-C1-6, ciano-cicloalqu(en)ilo-C3-8 y ciano-cicloalqu(en)il-C3-8-alqu(en/in)ilo-C1-6; o R10 y R10´ conjuntamente con el átomo de N al cual están unidos forman un anillo saturado o insaturado de 4 a 8 miembros el cual contiene, opcionalmente 1, 2 o 3 heteroátomos adicionales; X es CO o SO2; Z es O o NR4, donde R4 se selecciona entre el grupo que consiste en H, alqu(en/in)il-C1-6, cicloalqu(en)ilo-C3-8, cicloalqu(en9il-C3-8-alqu(en/in)ilo-C1-6, hidroxi-alqu(en/in)ilo-C1-6 e hidroxi-cicloalqu(en)ilo; o R3 y R4 conjuntamente con el átomo de N al cual están unidos forman un anillo saturado o insaturado de 4-8 miembros el cual contiene, opcionalmente 1, 2 o 3 heteroátomos adicionales, el anillo formado por R3 y R4 y el átomo de N es opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre alqu(en/in)ilo-C1-6, arilo y aril-alqu(en/in)ilo-C1-6; q es 0 o 1; y Y representa un heteroarilo de fórmula (2) o (3) donde W es O o S; m es 0, 1, 2, o 3; n es 0, 1, 2, 3 o 4; p es 0 o 1; y cada R5 se selecciona independientemente entre el grupo que consiste en alqu(en/in)ilo-C1-6, cicloalqu(en)ilo-C3-8, arilo, cicloalqu(en)il-C3-8-alqu(en/in)ilo-C1-6, aril-alqu(en/in)ilo-C1-6, acilo, halógeno, halo-alqu(en/in)ilo-C1-6, alqu(en/in)iloxi-C1-6, -CO-NR6R6´, ciano, nitro, NR7R7´, -S-R8, -SO2R8 y SO2OR8; donde R6 y R6´ se seleccionan independientemente entre el grupo que consiste en H, alqu(en/in)ilo-C1-6, cicloalqu(en)ilo-C3-8, cicloalqu(en)il-C3-8-alqu(en/in)ilo-C1-6 y arilo; R7 y R7´ se seleccionan independientemente entre el grupo que consiste en H, alqu(en/in)ilo-C1-6, cicloalqu(en)ilo-C3-8, cicloalqu(en)il-C3-8-alqu(en/in)ilo-C1-6, arilo y acilo; y R8 se selecciona entre el grupo que consiste en alqu(en/in)ilo-C1-6, cicloalqu(en)ilo-C3-8, cicloalqu(en)il-C3-8-alqu(en/in)ilo-c1-6, arilo y -NR9R9´; donde R9 y R9´ se seleccionan independientemente entre el grupo que consiste en H, alqu(en/in)ilo-C1-6, cicloalqu(en)ilo-C3-8 y cicloalqu(en)il-C3-8-alqu(en/in)ilo-C1-6, o sus sales farmacéuticamente aceptables.Claim 1: A 1,2,4-triaminobenzene derivative of formula (1) wherein: R1 is selected from the group consisting of H, alkyl (en / in) ilo-C1-6, cycloalkyl (en) C3- 8, cycloalkyl (en) yl C3-8-alkyl (en7in) C1-6 yl, acyl, hydroxy-alkyl (en / in) yl-C1-6 and hydroxy-cycloalkyl (en) yl-C3-8; R2 and R2 'are independently selected from the group consisting of H, alkyl (en / in) ilo-C1-6, cycloalk (en) ilo- C3-8, aryl, cycloalq (en) ilo- C3-8-alkyl (en / in) ilo-C1-6, aryl-alkyl (en / in) ilo-C1-6, acyl, hydroxy-alkyl (en / in) C1-6 yl and hydroxy-cycloalkyl (en) ilo-C3- 8; R3 is selected from the group consisting of H, alkyl (en / in) C1-6 yl, cycloalkyl (en) ilo-C3-8, aryl, cycloalkyl (en) il-C3-8-alkyl (en / in) ilo-C1-6, aryl-alkyl (en / in) ilo-C1-6, hydroxy-alkyl (en / in) ilo-C1-6, aryl-cycloalkyl (en) ilo-C3-8, NR10R10´-- C1-6 alkyl (en / in) C1-6, NR10R10'-cycloalkyl (en) Cyl- C3-8 and hydroxycycloalkyl (en) Cyl- C3-8; where R10 and R10 'are independently selected from the group consisting of H, alkyl (en / in) ilo-C1-6, cycloalkyl (en) ilo-C3-8, cycloalkyl (en) and C3-8-alkyl (en / in) C1-6 yl, hydroxy-alkyl (en / in) ilo-C1-6, hydroxy-cycloalkyl (en) ilo-C3-8, hydroxy-cycloalkyl (en) il-C3-8-alkyl (en / in) ilo-C1-6, halo-alkyl (en / in) ilo-C1-6, halo-cycloalk (en) ilo-C3-8, halo-cycloalk (en) il-C3-8-alkyl (en / in) ilo-C1-6, cyano-alkyl (en / in) ilo-C1-6, cyano-cycloalk (en) ilo-C3-8 and cyano-cycloalk (en) il-C3-8-alkyl (en / in) yl-C1-6; or R10 and R10 'together with the N atom to which they are attached form a saturated or unsaturated ring of 4 to 8 members which optionally contains 1, 2 or 3 additional heteroatoms; X is CO or SO2; Z is O or NR4, where R4 is selected from the group consisting of H, alkyl (en / in) il-C1-6, cycloalkyl (en) ilo-C3-8, cycloalkyl (en9il-C3-8-alkyl ( en / in) ilo-C1-6, hydroxy-alkyl (en / in) ilo-C1-6 and hydroxy-cycloalkyl (en) ilo; or R3 and R4 together with the N atom to which they are attached form a saturated ring or 4-8 membered unsaturated which optionally contains 1, 2 or 3 additional heteroatoms, the ring formed by R3 and R4 and the N atom is optionally substituted with one or more substituents independently selected from alky (in / in) yl -C1-6, aryl and aryl-alkyl (en / in) yl-C1-6; q is 0 or 1; and Y represents a heteroaryl of formula (2) or (3) where W is O or S; m is 0, 1, 2, or 3; n is 0, 1, 2, 3 or 4; p is 0 or 1; and each R5 is independently selected from the group consisting of alky (in / in) ilo-C1-6 , cycloalkyl (en) yl-C3-8, aryl, cycloalkyl (en) yl-C3-8-alkyl (en / in) ilo-C1-6, aryl-alkyl (en / in) ilo-C1-6, acyl , halogen, halo-alkyl (en / in) ilo-C1-6, alky (en / in) iloxy-C1-6, -CO-NR6R 6´, cyano, nitro, NR7R7´, -S-R8, -SO2R8 and SO2OR8; where R6 and R6 'are independently selected from the group consisting of H, alkyl (en / in) ilo-C1-6, cycloalkyl (en) ilo-C3-8, cycloalkyl (en) il-C3-8-alkyl ( en / in) C1-6 yl and aryl; R7 and R7 'are independently selected from the group consisting of H, alkyl (en / in) ilo-C1-6, cycloalkyl (en) ilo-C3-8, cycloalkyl (en) il-C3-8-alk (en / in) C1-6 yl, aryl and acyl; and R8 is selected from the group consisting of alkyl (en / in) ilo-C1-6, cycloalk (en) ilo-C3-8, cycloalkyl (en) il-C3-8-alkyl (en / in) ilo- C1-6, aryl and -NR9R9 '; where R9 and R9 'are independently selected from the group consisting of H, alkyl (en / in) ilo-C1-6, cycloalkyl (en) ilo-C3-8 and cycloalkyl (en) il-C3-8-alkyl ( en / in) yl-C1-6, or its pharmaceutically acceptable salts.

ARP030104782A 2002-12-27 2003-12-22 DERIVATIVES OF 1,2, 4- - TRIAMINOBENCEN USED FOR THE TREATMENT OF DISORDERS IN THE CENTRAL NERVOUS SYSTEM AR042656A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DKPA200202012 2002-12-27

Publications (1)

Publication Number Publication Date
AR042656A1 true AR042656A1 (en) 2005-06-29

Family

ID=35295526

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030104782A AR042656A1 (en) 2002-12-27 2003-12-22 DERIVATIVES OF 1,2, 4- - TRIAMINOBENCEN USED FOR THE TREATMENT OF DISORDERS IN THE CENTRAL NERVOUS SYSTEM

Country Status (17)

Country Link
KR (1) KR20050089862A (en)
CN (1) CN100448867C (en)
AR (1) AR042656A1 (en)
BR (1) BR0317748A (en)
CL (1) CL2003002748A1 (en)
EA (1) EA008589B1 (en)
HK (1) HK1088317A1 (en)
IS (1) IS2649B (en)
MY (1) MY139844A (en)
NO (1) NO20053612L (en)
PE (1) PE20041015A1 (en)
PL (1) PL377221A1 (en)
SI (1) SI1578740T1 (en)
TW (1) TWI325414B (en)
UA (1) UA79666C2 (en)
UY (1) UY28151A1 (en)
ZA (1) ZA200504565B (en)

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4200259A1 (en) * 1992-01-08 1993-07-15 Asta Medica Ag NEW 1,2,4-TRIAMINOBENZOL DERIVATIVES AND METHOD FOR THE PRODUCTION THEREOF
DE19539861A1 (en) * 1995-10-26 1997-04-30 Asta Medica Ag Use of 4-amino-4- (4-fluorobenzylamino) -1-ethoxy-carbonylaminobenzen for the prophylaxis and treatment of the consequences of acute and chronic cerebral low blood circulation and neurodegenerative diseases
GB9915414D0 (en) * 1999-07-01 1999-09-01 Glaxo Group Ltd Medical use
US6117900A (en) * 1999-09-27 2000-09-12 Asta Medica Aktiengesellschaft Use of retigabine for the treatment of neuropathic pain
US6589986B2 (en) * 2000-12-20 2003-07-08 Wyeth Methods of treating anxiety disorders

Also Published As

Publication number Publication date
NO20053612L (en) 2005-09-23
ZA200504565B (en) 2006-08-30
NO20053612D0 (en) 2005-07-25
BR0317748A (en) 2005-11-22
TW200413280A (en) 2004-08-01
KR20050089862A (en) 2005-09-08
HK1088317A1 (en) 2006-11-03
TWI325414B (en) 2010-06-01
IS7856A (en) 2005-05-23
EA008589B1 (en) 2007-06-29
CN100448867C (en) 2009-01-07
IS2649B (en) 2010-08-15
EA200501053A1 (en) 2005-12-29
MY139844A (en) 2009-11-30
CL2003002748A1 (en) 2005-04-08
PE20041015A1 (en) 2005-01-08
PL377221A1 (en) 2006-01-23
UY28151A1 (en) 2004-07-30
CN1732162A (en) 2006-02-08
SI1578740T1 (en) 2007-08-31
UA79666C2 (en) 2007-07-10

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