AR035718A1 - Derivados de quinolina, procedimientos para su preparacion, composiciones farmaceuticas que lo comprenden, y el uso de tales compuestos en la fabricacion de medicamentos - Google Patents

Derivados de quinolina, procedimientos para su preparacion, composiciones farmaceuticas que lo comprenden, y el uso de tales compuestos en la fabricacion de medicamentos

Info

Publication number
AR035718A1
AR035718A1 ARP010105516A ARP010105516A AR035718A1 AR 035718 A1 AR035718 A1 AR 035718A1 AR P010105516 A ARP010105516 A AR P010105516A AR P010105516 A ARP010105516 A AR P010105516A AR 035718 A1 AR035718 A1 AR 035718A1
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
hydroxy
compounds
halogen
Prior art date
Application number
ARP010105516A
Other languages
English (en)
Original Assignee
Glaxosmithkline Spa
Glaxosmithkline Lab
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
Application filed by Glaxosmithkline Spa, Glaxosmithkline Lab filed Critical Glaxosmithkline Spa
Publication of AR035718A1 publication Critical patent/AR035718A1/es

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    • 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
    • C07D401/06—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 only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/06—Antiasthmatics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
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    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • 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
    • C07D401/14—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 three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Addiction (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Derivados de quinolina de fórmula (1) o una de sus sales o hidratos farmacéuticamente aceptables, en la que: R1 es H o alquilo; R2 es -R8R9; R8 es un enlace sencillo o alquilo C1-3, opcionalmente sustituido una o más veces con hidroxi; R9 es arilo o cicloalquilo o heteroarilo, opcionalmente sustituido una o más veces con hidroxi, alcoxi, o alcoxialquilo; R3 es H o alquilo o cicloalquilo o cicloalquilalquilo, opcionalmente sustituido una o más veces con hidroxi o con uno o más átomos de flúor; R4 es -NR10R11; R10 y R11 se seleccionan independientemente de H o alquilo, o R10 y R11 junto con el átomo de nitrógeno al que están unidos forman un anillo de heterociclo saturado o insaturado que comprende 3-8 miembros en el anillo, cuyo anillo de heterociclo no está sustituido o está sustituido una o más veces con uno o más sustituyentes R12; R12 es oxo o -R13R14R15, donde R13 es un enlace sencillo o alquilo; R14 es OC(O) ó C(O)O; y R15 es H o alquilo; R5 es un alquilo, cicloalquilo, cicloalquilalquilo, arilo, o grupo heterociclo aromático solo o con anillo fusionado, cuyo grupo no está sustituido o está sustituido una o más veces con uno o más sustituyentes seleccionados de halógeno tal como flúor, alquilo o halógenoalquilo tal como fluoroalquilo; R6 representa H o hasta 3 sustituyentes seleccionados independientemente de la lista que consta de alquilo, alquenilo, arilo, alcoxi o uno de sus derivados hidroxilados, hidroxi, halógeno, nitro, ciano, carboxi, carboxamido, sulfonamido, alcoxicarbonilo, halógenoalquilo tal como trifluorometilo, aciloxi, amino, mono- o di-alquilamino, alcoxiamido, alcoxicarboxilato o uno de sus derivados esterificados; R7 es H o halógeno; a es 1-6; y cualquiera de R1, R3, R5, R8, R9, R10, R11 y R12 puede estar opcionalmente sustituido una o más veces con halógeno, hidroxi, amino, ciano, nitro, carboxi u oxo; con la condición de que el compuesto no sea un compuesto en el que R7 represente H, R5 represente fenilo no sustituido, y R1, R2, R3, R4, R6 y a se seleccionan de una de las combinaciones indicadas en la Tabla 1. Dichos compuestos son antagonistas no peptídicos de los receptores NK-2 y NK-3 y por lo tanto son úutiles para tratar y prevenir una amplia variedad de estados clínicos que se caracterizan por sobrestimulación de dichos receptores. También se dan a conocer procedimientos para la preparación de dichos compuestos, composiciones farmacéuticas que comprenden dichos compuestos, y el uso de los mismos en la fabricación de medicamentos.
ARP010105516A 2000-11-28 2001-11-27 Derivados de quinolina, procedimientos para su preparacion, composiciones farmaceuticas que lo comprenden, y el uso de tales compuestos en la fabricacion de medicamentos AR035718A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0028964.5A GB0028964D0 (en) 2000-11-28 2000-11-28 Novel compounds

Publications (1)

Publication Number Publication Date
AR035718A1 true AR035718A1 (es) 2004-07-07

Family

ID=9904011

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010105516A AR035718A1 (es) 2000-11-28 2001-11-27 Derivados de quinolina, procedimientos para su preparacion, composiciones farmaceuticas que lo comprenden, y el uso de tales compuestos en la fabricacion de medicamentos

Country Status (7)

Country Link
US (3) US20040102633A1 (es)
EP (1) EP1339691A1 (es)
JP (1) JP2004517079A (es)
AR (1) AR035718A1 (es)
AU (1) AU2002216060A1 (es)
GB (1) GB0028964D0 (es)
WO (1) WO2002044154A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7037922B1 (en) 2000-03-10 2006-05-02 Neurogen Corporation Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands
ITMI20031292A1 (it) * 2003-06-25 2004-12-26 Nikem Research Srl Derivati biciclici nk-2 antagonisti selettivi.
GB0515580D0 (en) 2005-07-29 2005-09-07 Merck Sharp & Dohme Therapeutic compounds
WO2009106534A1 (en) * 2008-02-26 2009-09-03 H. Lundbeck A/S Novel heterocyclic carboxamides as m1 agonists
JP5819397B2 (ja) * 2010-03-23 2015-11-24 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ Ｔｒｐｖ４拮抗薬
WO2011119693A1 (en) * 2010-03-23 2011-09-29 Glaxosmithkline Llc Trpv4 antagonists
EP3596055A1 (en) * 2017-03-15 2020-01-22 Ziylo Limited Macrocyclic compounds

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0804419T3 (da) * 1994-05-27 2003-11-24 Glaxosmithkline Spa Quinolinderivater som tachykinin NK 3-receptor-antagonister
GB9524104D0 (en) * 1995-11-24 1996-01-24 Smithkline Beecham Spa Novel compounds
AR004735A1 (es) * 1995-11-24 1999-03-10 Smithkline Beecham Spa Quinoleina 4-amido sustituida, un procedimiento para su preparacion, una composicion farmaceutica que los contiene y el uso de los mismos para lapreparacion de un medicamento.
AP9901695A0 (en) * 1997-05-23 1999-12-31 Smithkline Beecham Spa Quinoline-4-carbaoxamide derivatives as NK-2 and NK-3 receptor antagonists.
GB9825554D0 (en) * 1998-11-20 1999-01-13 Smithkline Beecham Spa Novel Compounds
US6780875B2 (en) * 1998-11-20 2004-08-24 Smithkline Beecham S.P.A. Quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists
NZ511777A (en) * 1998-11-20 2003-12-19 Smithkline Beecham S Quinoline-4-carboxamide derivatives as NK-3 and NK-2 receptor antagonists
AU4802500A (en) * 1999-04-26 2000-11-10 Neurogen Corporation 2-aminoquinolinecarboxamides: neurokinin receptor ligands

Also Published As

Publication number Publication date
GB0028964D0 (en) 2001-01-10
US20040102633A1 (en) 2004-05-27
EP1339691A1 (en) 2003-09-03
WO2002044154A1 (en) 2002-06-06
US20050070574A1 (en) 2005-03-31
US20060161004A1 (en) 2006-07-20
AU2002216060A1 (en) 2002-06-11
JP2004517079A (ja) 2004-06-10

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