PE20010956A1 - Derivados de isoquinolina y quinazolina con afinidad por los receptores de serotonina combinados 5-ht1a, 5-ht1b, 5-ht1d - Google Patents

Derivados de isoquinolina y quinazolina con afinidad por los receptores de serotonina combinados 5-ht1a, 5-ht1b, 5-ht1d

Info

Publication number
PE20010956A1
PE20010956A1 PE2000001176A PE0011762000A PE20010956A1 PE 20010956 A1 PE20010956 A1 PE 20010956A1 PE 2000001176 A PE2000001176 A PE 2000001176A PE 0011762000 A PE0011762000 A PE 0011762000A PE 20010956 A1 PE20010956 A1 PE 20010956A1
Authority
PE
Peru
Prior art keywords
isoquinoline
quinazoline
derivatives
ht1d
ht1b
Prior art date
Application number
PE2000001176A
Other languages
English (en)
Inventor
Laramie Mary Gaster
Thomas Daniel Heightman
Jean-Pierre Pilleux
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 GBGB9926304.8A external-priority patent/GB9926304D0/en
Priority claimed from GB0017880A external-priority patent/GB0017880D0/en
Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc
Publication of PE20010956A1 publication Critical patent/PE20010956A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms

Landscapes

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

Abstract

SE REFIERE A DERIVADOS DE ISOQUINOLINA Y QUINAZOLINA DE FORMULA I DONDE R1 ES UN GRUPO i, ii; P1 P2, P3 SON FENILO, NAFTILO, HETEROARILO DE 5-6 MIEMBROS, HETEROCICLO CONDENSADO CON BENCENO, HETEROCICLO CONDENSADO CON PIRIDINA; Ra, Rb, Rc SON HALOGENO, ALQUILO C1-C6, CICLOALQUILO C3-C6, CF3, ALCOXI C1-C6, CO2R5, NR5R6, ENTRE OTROS; R5 Y R6 SON H, ALQUILO C1-C6; n, p, q SON 0-3; L ES UN ENLACE, NH; R2 ES H, O JUNTO CON R3 FORMAN CH=CH, -(CR7CR8)2-; R7 Y R8 SON H, ALQUILO C1-C6; R3 ES H; Y, X SON N, CH; R4 ES H, ALQUILO C1-C6. SON COMPUESTOS PREFERIDOS 2,3-DIHIDRO-1-(5-METIL-1-FENILPIRAZOL-4-ILCARBONIL)-8-(4-METILPIPERAZIN-1-IL)-PIRROLO[3,2-g]ISOQUINOLINA; 1-(2-FLUOROBENZOIL)-2,3-DIHIDRO-8-(4-METILPIPERAZIN-1-IL)PIRROLO[3,2-g]ISOQUINOLINA, 1-[1-(4-CIANOFENIL)-5-METILPIRAZOL-4-ILCARBONIL]-2,3DIHIDRO-8-(4-METILPIPERAZIN-1-IL)PIRROLO[3,2-g]ISOQUINOLINA, ENTRE OTROS; TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I ES UN LIGANDO CON AFINIDAD POR LOS RECEPTORES DE SEROTONINA 5-HT1A, 5-HT1B, 5-HT1D UTIL PARA EL TRATAMIENTO DE LA DEPRESION
PE2000001176A 1999-11-05 2000-11-03 Derivados de isoquinolina y quinazolina con afinidad por los receptores de serotonina combinados 5-ht1a, 5-ht1b, 5-ht1d PE20010956A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9926304.8A GB9926304D0 (en) 1999-11-05 1999-11-05 Novel compounds
GB0017880A GB0017880D0 (en) 2000-07-20 2000-07-20 Novel compounds

Publications (1)

Publication Number Publication Date
PE20010956A1 true PE20010956A1 (es) 2001-09-15

Family

ID=26244692

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001176A PE20010956A1 (es) 1999-11-05 2000-11-03 Derivados de isoquinolina y quinazolina con afinidad por los receptores de serotonina combinados 5-ht1a, 5-ht1b, 5-ht1d

Country Status (10)

Country Link
US (1) US20050239797A1 (es)
EP (1) EP1228043B1 (es)
JP (1) JP2003513075A (es)
AT (1) ATE286883T1 (es)
AU (1) AU1028601A (es)
DE (1) DE60017446T2 (es)
ES (1) ES2234683T3 (es)
PE (1) PE20010956A1 (es)
UY (1) UY26426A1 (es)
WO (1) WO2001032626A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001256733A1 (en) * 2000-05-16 2001-11-26 Takeda Chemical Industries Ltd. Melanin-concentrating hormone antagonist
DE10315569A1 (de) 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazolverbindungen
DE10315573A1 (de) 2003-04-05 2004-10-14 Merck Patent Gmbh Substituierte Pyrazole
DE10315571A1 (de) * 2003-04-05 2004-10-14 Merck Patent Gmbh Pyrazolverbindungen
GB0316915D0 (en) * 2003-07-18 2003-08-20 Glaxo Group Ltd Compounds
EP1651612B9 (en) 2003-07-22 2012-09-05 Astex Therapeutics Limited 3,4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinases (cdk) and glycogen synthase kinase-3 (gsk-3) modulators
RU2006129464A (ru) * 2004-01-16 2008-02-27 Ф.Хоффманн-Ля Рош Аг (Ch) Производные 1-бензил-5-пиперазин-1-ил-3, 4-дигидро-1н-хиназолин-2-она и соответствующие производные 1н-бензо (1, 2, 6) тиадиазин-2, 2-диоксида и 1, 4-дигидробензо (1, 3)оксазин-2-она в качестве модуляторов рецептора 5-гидрокситриптамина (5нт) для лечения заболевания центральной нервной системы
US9066903B2 (en) * 2006-02-28 2015-06-30 The United States Of America As Represented By The Department Of Veterans Affairs Pharmacological treatment of Parkinson's disease
US20090099175A1 (en) * 2006-03-01 2009-04-16 Arrington Mark P Phosphodiesterase 10 inhibitors
EP2139481B1 (en) 2007-03-21 2013-08-21 The University Of Montana 1-[(2'-substituted)-piperazin-1'-yl]-isoquinolines as norepinephrine transporter inhibitor therapeutics and positron emission tomography imaging agents
WO2012102405A1 (ja) 2011-01-28 2012-08-02 佐藤製薬株式会社 縮環化合物
US10092574B2 (en) 2012-09-26 2018-10-09 Valorisation-Recherche, Limited Partnership Inhibitors of polynucleotide repeat-associated RNA foci and uses thereof
KR101709127B1 (ko) * 2015-06-16 2017-02-22 경동제약 주식회사 Dpp-iv 억제제의 제조를 위한 신규 중간체, 이의 제조방법 및 이를 이용한 dpp-iv 억제제의 제조방법
CN112480007B (zh) * 2020-12-08 2022-11-18 宿迁市科莱博生物化学有限公司 一种1,3-二甲基-1h-吡唑-4-羧酸的合成方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3778440A (en) * 1970-12-07 1973-12-11 Sandoz Ag 1-substituted amino-isoquinolines and nitrates thereof
US3932412A (en) * 1970-12-07 1976-01-13 Sandoz, Inc. 1-(4-Hydroxyalkylpiperazino)-isoquinoline nitrates
IL112248A0 (en) * 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
WO1998047868A1 (en) * 1997-04-18 1998-10-29 Smithkline Beecham Plc Heterocycle-containing urea derivatives as 5ht1a, 5ht1b and 5ht1d receptor antagonists
PL336317A1 (en) * 1997-04-18 2000-06-19 Smithkline Beecham Plc Derivatives of indole exhibiting combined activity of receptor 5ht 1a, 5ht and 5ht 1d antagonist
EP1020445B1 (en) * 1997-10-02 2008-08-13 Eisai R&D Management Co., Ltd. Fused pyridine derivatives
EP1047691A1 (en) * 1997-12-12 2000-11-02 Smithkline Beecham Plc Quinolinepiperazine and quinolinepiperidine derivatives, their preparation and their use as combined 5-ht1a, 5-ht1b and 5-ht1d receptor antagonists
WO2000006575A2 (en) * 1998-07-28 2000-02-10 Smithkline Beecham Plc Azabicyclic compounds

Also Published As

Publication number Publication date
WO2001032626A1 (en) 2001-05-10
EP1228043B1 (en) 2005-01-12
DE60017446D1 (de) 2005-02-17
ES2234683T3 (es) 2005-07-01
AU1028601A (en) 2001-05-14
UY26426A1 (es) 2001-05-31
JP2003513075A (ja) 2003-04-08
ATE286883T1 (de) 2005-01-15
EP1228043A1 (en) 2002-08-07
US20050239797A1 (en) 2005-10-27
DE60017446T2 (de) 2006-03-02

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