CO4950608A1 - Nuevos derivados de piperazina y procesos para su preparacion - Google Patents

Nuevos derivados de piperazina y procesos para su preparacion

Info

Publication number
CO4950608A1
CO4950608A1 CO98021149A CO98021149A CO4950608A1 CO 4950608 A1 CO4950608 A1 CO 4950608A1 CO 98021149 A CO98021149 A CO 98021149A CO 98021149 A CO98021149 A CO 98021149A CO 4950608 A1 CO4950608 A1 CO 4950608A1
Authority
CO
Colombia
Prior art keywords
alkyl
nitrogen
oxygen
alkoxy
sulfur
Prior art date
Application number
CO98021149A
Other languages
English (en)
Inventor
Kantilal Rami Harshad
Paul Adrian Wyman
Original Assignee
Smithkline Beecham Plc
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 GBGB9707829.9A external-priority patent/GB9707829D0/en
Priority claimed from GBGB9801882.3A external-priority patent/GB9801882D0/en
Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc
Publication of CO4950608A1 publication Critical patent/CO4950608A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • 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
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • 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
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

Un compuesto de la fórmula (I) o una de sus salesen la que Ra es un grupo de la fórmula (i)en la que P1 es fenilo, arilo bicíclico, un anillo heterocíclico de 5 a 7 miembros que contiene 1 a 3 heteroátomos seleccionados entre oxígeno, nitrógeno y azufre, o un anillo heterocíclico bicíclico que contiene 1 a 3 heteroátomos seleccionados entre oxígeno, nitrógeno y azufre;R1 es hidrógeno, halógeno, alquilo C1-6 , cicloalquilo C3-6 , CO-alquilo C1-6 , alcoxi C1-6 , hidroxi, hidroxi-alquilo C1-6 , hidroxi-alcoxi C1-6 , alcoxi C1-6 -alcoxi C1-6 , alcanoilo C1-6 , nitro,trifluorometilo, ciano, SR9 , SOR9 , SO2 R9 , SO2 NR10 R11 , CO2 R10 , CONR10 R11 , CO2 NR10 R11 , CONR10 (CH2 )a CO2 R11 , (CH2 )a NR10 R11 ,(CH2 )a CONR10 R11 , (CH2 )a NR10 CONR11 , (CH2 )2 CO2 -alquilo C1-6 , CO2 (CH2 )a OR10 , NR10 R11 , NR10 CO2 R11 , NR10 CONR10 R11 , CR10 =NOR11 , NR10 COOR11 , CNR10 =NOR11 , donde R10 y R11 son independientemente hidrógeno o alquilo C1-6 y C es 1 a 4,R2 es hidrógeno, halógeno, alquilo C1-6 , cicloalquilo C3-6 , cicloalquenilo C3-6 , alcoxi C1-6 , alcanoilo C1-6 , arilo, aciloxi, hidroxi, nitro, trifluorometilo, ciano, CO2 R10 , CONR10 R11 , NR10 R11 , donde R10 y R11 son como se han definido para R1 ;a es 1, 2 ó 3; - 2 -o Ra es un grupo de la fórmula (ii)en la que P2 y P3 son independientemente fenilo, arilo bicíclico, un anillo heterocíclico de 5 a 7 miembros que contiene 1 a 3 heteroátomos seleccionados entre oxígeno, nitrógeno yazufre, o un grupo heterocíclico bicíclico que contiene 1 a 3 heteroátomos seleccionados entre oxígeno, nitrógeno o azufre;A es un enlace u oxígeno, S(O)m donde m es 0 a 2, carbonilo, CH2 , -CH2 CH2 -, o NR4 donde R4 es hidrógeno o alquilo C1-6 ; R1 es como se ha definido antes para la fórmula (I) o R1 es un anillo heterocíclico de 5 a 7 miembros que contiene 1 a 3 heteroátomos seleccionados entre oxígeno, nitrógeno o azufre, opcionalmentesustituido con alquilo C1-6 , halógeno o alcanoilo C1-6 . R2 y R3 son independientemente, hidrógeno, halógeno, alquilo C1-6 , cicloalquilo C3-6 , cicloalquenilo C3-6 , alcoxi C1-6 , alcanoilo C1-6 , arilo, aciloxi, hidroxi, nitro, trifluorometilo, ciano, CO2 R10 , CONR10 R11 , NR10 R11 , donde R10 y R11 son como se han definido para R1 ;y a y b son independientemente, 1, 2 ó 3;Y es -NH-, -NR5 - donde R5 es alquilo C1-6 , o Y es -CH2 - o -O-;V es oxígeno o azufre;D es nitrógeno, carbono o un grupo CH; W es (CR16 R17 )t donde t es 2, 3 ó 4 y R16 y R17 son independientemente hidrógeno o alquilo C1-6 , o W es (CR16 R17 )u AND#8209;J donde u es 0, 1, 2 ó 3 y J es oxígeno, azufre, CR16 =CR17 , CR16 =N, =CR16 O, =CR16 S o =CR16 -N17 ;X es nitrógeno o carbono;Rb es hidrógeno, halógeno, hidroxi, alquilo C1-6 , trifluorometilo, alcoxi C1-6 , alquenilo C2-6 , cicloalquilo C3-7 , opcionalmente sustituido con alquilo C1-4 , o arilo;Ra es hidrógeno o alquilo C1-6 ; y--- es un enlace sencillo cuando X es nitrógeno o un enlace sencillo o doble cuando X es carbono.
CO98021149A 1997-04-18 1998-04-17 Nuevos derivados de piperazina y procesos para su preparacion CO4950608A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9707829.9A GB9707829D0 (en) 1997-04-18 1997-04-18 Novel compounds
GBGB9801882.3A GB9801882D0 (en) 1998-01-29 1998-01-29 Novel compounds

Publications (1)

Publication Number Publication Date
CO4950608A1 true CO4950608A1 (es) 2000-09-01

Family

ID=26311401

Family Applications (1)

Application Number Title Priority Date Filing Date
CO98021149A CO4950608A1 (es) 1997-04-18 1998-04-17 Nuevos derivados de piperazina y procesos para su preparacion

Country Status (17)

Country Link
EP (1) EP0975593A1 (es)
JP (1) JP2001524116A (es)
KR (1) KR20010006487A (es)
CN (1) CN1260781A (es)
AR (1) AR013076A1 (es)
AU (1) AU732863B2 (es)
BR (1) BR9809092A (es)
CA (1) CA2288662A1 (es)
CO (1) CO4950608A1 (es)
HU (1) HUP0001123A3 (es)
IL (1) IL132409A0 (es)
NO (1) NO995065L (es)
NZ (1) NZ500252A (es)
PL (1) PL336317A1 (es)
TR (1) TR199902590T2 (es)
TW (1) TW509687B (es)
WO (1) WO1998050358A1 (es)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9725931D0 (en) * 1997-12-05 1998-02-04 Smithkline Beecham Plc Novel compounds
EP1101759A4 (en) 1998-07-31 2001-12-12 Nippon Soda Co PHENYLAZOLE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND MEDICATIONS FOR HYPERLIPEMY
GB9827882D0 (en) * 1998-12-17 1999-02-10 Smithkline Beecham Plc Novel compounds
UA62015C2 (en) * 1998-12-28 2003-12-15 Pfizer Prod Inc Benzoizoxazol derivatives, a pharmaceutical composition (variants) based thereon (variants) and a method for treatment (variants)
GB9912413D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
GB9912417D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
CA2378047A1 (en) * 1999-07-15 2001-01-25 Methvin Isaac Heterocyclic compounds for the treatment of migraine
HUP0202787A3 (en) 1999-09-25 2003-12-29 Smithkline Beecham Plc Piperazine derivatives as 5-ht1b antagonists, process for their preparation and pharmaceutical compositions containing them
WO2001032626A1 (en) * 1999-11-05 2001-05-10 Smithkline Beecham P.L.C. Isoquinoline and quinazoline derivatives having a combined 5ht1a, 5ht1b and 5ht1d receptor activity
GB9926303D0 (en) * 1999-11-05 2000-01-12 Smithkline Beecham Plc Novel compounds
DE10051981A1 (de) 2000-10-20 2002-05-02 Bayer Ag Substituierte Phenyluracile
GB0106419D0 (en) 2001-03-15 2001-05-02 Smithkline Beecham Plc Novel compounds
GB0106586D0 (en) * 2001-03-16 2001-05-09 Smithkline Beecham Plc Novel compounds
KR100600240B1 (ko) * 2001-06-07 2006-07-13 에프. 호프만-라 로슈 아게 5-ｈｔ6 수용체 친화도를 갖는 신규한 인돌 유도체
EP2033953A1 (en) 2002-02-15 2009-03-11 Glaxo Group Limited Vanilloid receptor modulators
ATE316523T1 (de) 2002-05-13 2006-02-15 Hoffmann La Roche Benzoxazinderivate als 5-ht6-modulatoren und deren verwendungen
AU2004299201B2 (en) 2003-12-09 2009-12-03 F. Hoffmann-La Roche Ag Benzoxazine derivatives and uses thereof
CN101896461A (zh) * 2007-12-13 2010-11-24 安姆根有限公司 γ分泌酶调节剂
CA2794153C (en) 2010-03-25 2018-01-02 Glaxosmithkline Llc Substituted indoline derivatives as perk inhibitors
GB201106817D0 (en) 2011-04-21 2011-06-01 Astex Therapeutics Ltd New compound
CN102924330A (zh) * 2012-09-03 2013-02-13 华东理工大学 一种规模化制备5-氨基-1-萘腈的方法
US9980973B2 (en) 2012-10-19 2018-05-29 Astex Therapeutics Limited Bicyclic heterocycle compounds and their uses in therapy
GB201218862D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
GB201218864D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
GB201218850D0 (en) 2012-10-19 2012-12-05 Astex Therapeutics Ltd Bicyclic heterocycle compounds and their uses in therapy
CN103467374A (zh) * 2013-08-30 2013-12-25 江苏弘和药物研发有限公司 一种8-溴-4-羧基喹啉的合成方法
CN109336883B (zh) 2013-12-20 2022-06-14 阿斯特克斯治疗有限公司 双环杂环化合物及其治疗用途
CN115197099A (zh) * 2022-05-30 2022-10-18 安徽昊帆生物有限公司 N-Boc-1，4-苯二胺的制备方法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9119920D0 (en) * 1991-09-18 1991-10-30 Glaxo Group Ltd Chemical compounds
EP0533268B1 (en) * 1991-09-18 2001-08-16 Glaxo Group Limited Benzanilide derivatives as 5-HT1D antagonists
GB9119932D0 (en) * 1991-09-18 1991-10-30 Glaxo Group Ltd Chemical compounds
EP0712397B1 (en) * 1993-08-06 1999-04-21 Smithkline Beecham Plc Amide derivatives as 5ht1d receptor antagonists
JPH09504004A (ja) * 1993-08-20 1997-04-22 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー ５ｈｔ１ｄレセプター拮抗薬用アミドおよび尿素誘導体
WO1995006637A1 (en) * 1993-09-03 1995-03-09 Smithkline Beecham Plc Indole and indoline derivatives as 5ht1d receptor antagonists

Also Published As

Publication number Publication date
AU732863B2 (en) 2001-05-03
BR9809092A (pt) 2002-01-22
AU7431098A (en) 1998-11-27
PL336317A1 (en) 2000-06-19
AR013076A1 (es) 2000-12-13
HUP0001123A3 (en) 2002-04-29
JP2001524116A (ja) 2001-11-27
HUP0001123A2 (hu) 2001-04-28
CA2288662A1 (en) 1998-11-12
TR199902590T2 (xx) 2000-06-21
WO1998050358A1 (en) 1998-11-12
NZ500252A (en) 2001-07-27
NO995065D0 (no) 1999-10-15
NO995065L (no) 1999-10-15
CN1260781A (zh) 2000-07-19
KR20010006487A (ko) 2001-01-26
TW509687B (en) 2002-11-11
EP0975593A1 (en) 2000-02-02
IL132409A0 (en) 2001-03-19

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