[go: up one dir, main page]

PE20040928A1 - Derivados de tetrahidroquinolinas como moduladores del receptor fsh - Google Patents

Derivados de tetrahidroquinolinas como moduladores del receptor fsh

Info

Publication number
PE20040928A1
PE20040928A1 PE2004000023A PE2004000023A PE20040928A1 PE 20040928 A1 PE20040928 A1 PE 20040928A1 PE 2004000023 A PE2004000023 A PE 2004000023A PE 2004000023 A PE2004000023 A PE 2004000023A PE 20040928 A1 PE20040928 A1 PE 20040928A1
Authority
PE
Peru
Prior art keywords
alcoxy
dimetoxy
trimethyl
phenyl
fsh receptor
Prior art date
Application number
PE2004000023A
Other languages
English (en)
Inventor
Willem Frederik Johan Karstens
Cornelis Marius Timmers
Original Assignee
Organon Nv
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 Organon Nv filed Critical Organon Nv
Publication of PE20040928A1 publication Critical patent/PE20040928A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/38—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A61P5/08—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C07D215/44—Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
    • 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
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

SE REFIERE DERIVADOS DE TETRAHIDROQUINOLINA DE FORMULA I, DONDE R1 Y R2 SON H O Me; R3 ES H, HIDROXI, ALCOXI(C1-C4), (DI)ALQUILAMINO(C1-C4)-ALCOXI(C2-C4) O HETEROCICLOALQUIL(C2-C6)-ALCOXI(C2-C4); R4 Y R5 SON H, OH, ALCOXI(C1-C4) O R7; CON LA CONDICION DE QUE SI R4 ES H, R5 NO ES H, OH O ALCOXI(C1-C4) Y DE QUE SI R5 ES H, R4 NO ES H, OH o ALCOXI(C1-C4); R6 ES HETEROARIL(C2-C5), ARIL(C6), CICLOALQUILO(C3-C8), HETEROCICLOALQUIL(C2-C6) O ALQUIL(C1-C6), R7 ES AMINO, (DI)ALQUILAMINO(C1-C4), ARILCARBONILAMINO(C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-[1-ACETIL-5,7-DIMETOXI-4-(4-METOXI-FENIL)-2,2,4-TRIMETIL-1,2,3,4-TETRAHIDRO-QUINOLINA-6-IL]-3-CLORO-2,6-DIMETOXI-BENZAMIDA, 4,5-DIMETIL-FURAN-2-ACIDO CARBOXILICO [1-ACETIL-5,7-DIMETOXI-4-(4-METOXI-FENIL)-2,2,4-TRIMETIL-1,2,3,4-TETRAHIDRO-QUINOLINA-6-IL]-AMIDA, 5-BROMO-TIOFENO-2-ACIDO ACRBOXILICO [1-ACETIL5,7-DIMETOXI-4-(4-METOXI-FENIL)-2,2,4-TRIMETIL-1,2,3,4-TETRAHIDRO-QUINOLINA-6-IL]-AMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA QUE LOS CONTIENE. ESTOS COMPUESTOS SON MODULARES DEL RECEPTOR DE FSH YA QUE PUEDEN UTILIZARSE COMO AGONISTAS(PARCIALES) O ANTAGONISTAS(PARCIALES) DEL RECEPTOR FSH, Y PUEDEN UTILIZARSE PARA TRATAR LA INFERTILIDAD, PARA LA ANTICONCEPCION Y PARA EL TRATAMIENTO DE DESORDENES HORMONO-DEPENDIENTES COMO CANCER DE MAMAS, DE PROSTATA Y ENDOMETRIOSIS
PE2004000023A 2002-12-20 2004-01-05 Derivados de tetrahidroquinolinas como moduladores del receptor fsh PE20040928A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP02102866 2002-12-20

Publications (1)

Publication Number Publication Date
PE20040928A1 true PE20040928A1 (es) 2004-12-25

Family

ID=39311811

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000023A PE20040928A1 (es) 2002-12-20 2004-01-05 Derivados de tetrahidroquinolinas como moduladores del receptor fsh

Country Status (18)

Country Link
US (1) US7858794B2 (es)
EP (1) EP1578726B1 (es)
JP (1) JP4545001B2 (es)
AR (1) AR042630A1 (es)
AT (1) ATE423771T1 (es)
AU (1) AU2003298363B2 (es)
BR (1) BR0317518A (es)
CA (1) CA2508952C (es)
CL (1) CL2003002685A1 (es)
ES (1) ES2321830T3 (es)
NZ (1) NZ540578A (es)
PE (1) PE20040928A1 (es)
PL (1) PL377318A1 (es)
RS (1) RS51293B (es)
RU (1) RU2328488C2 (es)
TW (1) TWI306855B (es)
UA (1) UA81442C2 (es)
WO (1) WO2004056780A2 (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1406628E (pt) * 2001-07-02 2006-06-30 Akzo Nobel Nv Derivados de tera-hidroquinolina
TWI322012B (en) * 2002-12-20 2010-03-21 Organon Nv Tetrahydroquinoline derivatives
TWI306855B (en) 2002-12-20 2009-03-01 Organon Nv Tetrahydroquinoline derivatives
US7691848B2 (en) 2005-03-02 2010-04-06 Wyeth Pyrrolobenzodiazepine arylcarboxamides and derivatives thereof as follicle-stimulating hormone receptor antagonists
CA2607882A1 (en) 2005-05-12 2006-11-23 Wyeth Pyrrolobenzodiazepines and heterocyclic carboxamide derivatives as follicle stimulating hormone receptor (fsh-r) antagonists
EP1893615A1 (en) * 2005-06-09 2008-03-05 Wyeth a Corporation of the State of Delaware Pyrrolobenzodiazepine pyridine carboxamides and derivatives as follicle-stimulating hormone receptor antagonists
ES2384643T3 (es) * 2005-11-30 2012-07-10 Astellas Pharma Inc. Derivados de 2-aminobenzamida como inhibidores del receptor vainilloide 1 (VR1) útiles para el tratamiento del dolor o el trastorno de la función de la vejiga
EP1956016A1 (en) * 2006-12-15 2008-08-13 Bayer Schering Pharma Aktiengesellschaft Bicyclic acyltryptophanols
WO2008071455A1 (en) * 2006-12-15 2008-06-19 Bayer Schering Pharma Aktiengesellschaft Bicyclic acyltryptophanols
GB0705656D0 (en) * 2007-03-23 2007-05-02 Addex Pharmaceuticals Sa Novel compounds E1
TW200918058A (en) * 2007-08-31 2009-05-01 Organon Nv TSH receptor antagonizing tetrahydroquinoline compounds
US8071587B2 (en) * 2009-05-27 2011-12-06 N. V. Organon (Dihydro)imidazoiso[5,1-A]quinolines
TW201116531A (en) * 2009-07-29 2011-05-16 Organon Nv Ring-annulated dihydropyrrolo[2,1-a]isoquinolines
US8431564B2 (en) 2009-07-29 2013-04-30 Merck Sharp & Dohme B.V. Ring-annulated dihydropyrrolo[2,1-α]isoquinolines
US11185569B2 (en) * 2016-05-04 2021-11-30 University Of Cincinnati ActRIIB:Fc to treat infertility in females

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2686182A (en) 1950-12-07 1954-08-10 Basf Ag O-hydroxy-dihydro-quinoline carboxylic acids
DE3879031T2 (de) 1987-08-08 1993-06-24 Akzo Nv Kontrazeptives implantat.
SK280617B6 (sk) * 1992-01-16 2000-05-16 Hoechst Aktiengesellschaft Arylcykloalkylové deriváty, spôsob ich prípravy, f
ATE269336T1 (de) * 1994-12-22 2004-07-15 Ligand Pharm Inc Steroidrezeptor-modulator verbindungen und methoden
CA2339018A1 (en) 1998-08-07 2000-02-17 Applied Research Systems Ars Holding N.V. Fsh mimetics for the treatment of infertility
US6200963B1 (en) * 1999-03-31 2001-03-13 American Home Products Corporation Aryl sulfonic acids as FSH antagonists
PT1406628E (pt) * 2001-07-02 2006-06-30 Akzo Nobel Nv Derivados de tera-hidroquinolina
TWI322012B (en) * 2002-12-20 2010-03-21 Organon Nv Tetrahydroquinoline derivatives
TWI306855B (en) 2002-12-20 2009-03-01 Organon Nv Tetrahydroquinoline derivatives
TW592127U (en) * 2003-05-19 2004-06-11 Tatung Co Network-type physiology monitoring device

Also Published As

Publication number Publication date
JP4545001B2 (ja) 2010-09-15
JP2006512347A (ja) 2006-04-13
CA2508952A1 (en) 2004-07-08
WO2004056780A3 (en) 2004-08-05
EP1578726B1 (en) 2009-02-25
TWI306855B (en) 2009-03-01
CL2003002685A1 (es) 2005-04-08
AU2003298363B2 (en) 2009-09-24
UA81442C2 (en) 2008-01-10
RS51293B (sr) 2010-12-31
AU2003298363A1 (en) 2004-07-14
ATE423771T1 (de) 2009-03-15
RS20050457A (sr) 2007-08-03
ES2321830T3 (es) 2009-06-12
RU2328488C2 (ru) 2008-07-10
TW200418800A (en) 2004-10-01
RU2005122946A (ru) 2005-12-20
CA2508952C (en) 2011-09-13
PL377318A1 (pl) 2006-01-23
AR042630A1 (es) 2005-06-29
EP1578726A2 (en) 2005-09-28
BR0317518A (pt) 2005-11-16
US7858794B2 (en) 2010-12-28
US20060142334A1 (en) 2006-06-29
WO2004056780A2 (en) 2004-07-08
NZ540578A (en) 2006-12-22

Similar Documents

Publication Publication Date Title
PE20040928A1 (es) Derivados de tetrahidroquinolinas como moduladores del receptor fsh
ATE496620T1 (de) 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
AR055592A1 (es) Derivados de 2-amino-5-cicloalquil-hidantoina como moduladores y/o inhibidores de la beta-secretasa(bace)
CO5721006A2 (es) Derivados de pirazolo-quinazolina, proceso para su preparacion y su uso como inhibidores de quinasa
PE20190326A1 (es) Isoquinolin-3-il-carboxamidas y preparacion y uso de las mismas
UY28150A1 (es) Agentes terapeuticos
ES2182535T3 (es) Derivados de benzo(b)tiepina-1,-dioxido, procedimiento para su preparacion, medicamentos que contienen estos compuestos y su utilizacion.
BR0214024A (pt) Derivados de 1,2,4-tiadiazol como moduladores de receptor de melanocortina
PE20011030A1 (es) Combinaciones farmaceuticas que comprenden tegaserod y omeprazol
ATE297910T1 (de) Retinoid x rezeptormodulatoren
TW200505903A (en) CGRP receptor antagonists
BR0311541A (pt) indol, azaindol e 4-aquenil piperidina amidas heterocìclicas relacionadas
MY146494A (en) Indole sulfonamide modulators of progesterone receptors
PE20050420A1 (es) Fenacilo 2-hidroxi-3-diaminoalcanos
BR0312069A (pt) Compostos de benzimidazol e seu uso como agonistas/antagonistas de estrogênio
CO5680438A2 (es) Uso de derivados de ciclotiocarbamato en tratamiento de condiciones relacionadas con hormonas
AR037907A1 (es) Derivados de azaindolilalquilamina como ligandos de 5-hidroxitriptamina-6
AR036327A1 (es) Compuestos derivados del cromano para uso terapeutico, composicion farmaceutica, uso de estos compuestos para la preparacion de medicamentos para tratar migrana, compuestos relacionados, y procesos para preparar esos compuestos relacionados
CY1106973T1 (el) Παραγωγα θειαζολινης ως εκλεκτικοι διαμορφωται υποδοχεως ανδρογονου (sarms)
ES2038678T3 (es) Procedimiento para la preparacion de n-(2-alquil-3-mercapto-glutaril)-alfamino-acidos.
DE60221425D1 (de) Substituierte tetrazyklische pyprolochinolonderivate als phosphodiesterase-inhibitoren
AR041786A1 (es) Derivados de azetidina como antagonistas del receptor ccr-3, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la elaboracion de un medicamento
EA200400896A1 (ru) Терапевтические акридоновые и акридиновые соединения
AR068381A1 (es) Compuestos de quinolina apropiados para tratar trastornos que responden a la modulacion del receptor de serotonina 5-ht6
BRPI0508404A (pt) derivado de (indol-3-il)-heterociclo, composição farmacêutica, uso de um derivado de (indol-3-il)-heterociclo, e método de tratamento da dor

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed