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

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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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Quinoline Compounds (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
US8058441B2 (en) * 2001-07-02 2011-11-15 N.V. Organon Tetrahydroquinoline derivatives
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
WO2006124581A2 (en) 2005-05-12 2006-11-23 Wyeth Pyrrolobenzodiazepines and heterocyclic carboxamide derivatives as follicle stimulating hormone receptor (fsh-r) antagonists
JP2008543765A (ja) 2005-06-09 2008-12-04 ワイス 卵胞刺激ホルモンレセプターアンタゴニストとしてのピロロベンゾジアゼピンピリジンカルボキサミドおよび誘導体
AU2006319916A1 (en) 2005-11-30 2007-06-07 Astellas Pharma Inc. 2-aminobenzamide derivative
WO2008071455A1 (en) * 2006-12-15 2008-06-19 Bayer Schering Pharma Aktiengesellschaft Bicyclic acyltryptophanols
EP1956016A1 (en) * 2006-12-15 2008-08-13 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
US8431564B2 (en) 2009-07-29 2013-04-30 Merck Sharp & Dohme B.V. Ring-annulated dihydropyrrolo[2,1-α]isoquinolines
TW201116531A (en) * 2009-07-29 2011-05-16 Organon Nv Ring-annulated dihydropyrrolo[2,1-a]isoquinolines
WO2017192847A1 (en) * 2016-05-04 2017-11-09 University Of Cincinnati Female fertility therapies

Family Cites Families (9)

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Publication number Priority date Publication date Assignee Title
US2686182A (en) * 1950-12-07 1954-08-10 Basf Ag O-hydroxy-dihydro-quinoline carboxylic acids
DE19975054I2 (de) 1987-08-08 2000-04-13 Akzo Nobel Nv Kontrazeptives Implantat
DE69533180T2 (de) 1994-12-22 2005-07-14 Ligand Pharmaceuticals, Inc., San Diego 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
US8058441B2 (en) * 2001-07-02 2011-11-15 N.V. Organon Tetrahydroquinoline derivatives
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
RS20050457A (en) 2007-08-03
JP2006512347A (ja) 2006-04-13
EP1578726A2 (en) 2005-09-28
AU2003298363B2 (en) 2009-09-24
AR042630A1 (es) 2005-06-29
RU2005122946A (ru) 2005-12-20
RU2328488C2 (ru) 2008-07-10
US20060142334A1 (en) 2006-06-29
JP4545001B2 (ja) 2010-09-15
PL377318A1 (pl) 2006-01-23
CL2003002685A1 (es) 2005-04-08
AU2003298363A1 (en) 2004-07-14
EP1578726B1 (en) 2009-02-25
US7858794B2 (en) 2010-12-28
ES2321830T3 (es) 2009-06-12
BR0317518A (pt) 2005-11-16
TWI306855B (en) 2009-03-01
RS51293B (sr) 2010-12-31
CA2508952A1 (en) 2004-07-08
ATE423771T1 (de) 2009-03-15
CA2508952C (en) 2011-09-13
UA81442C2 (en) 2008-01-10
WO2004056780A3 (en) 2004-08-05
WO2004056780A2 (en) 2004-07-08
NZ540578A (en) 2006-12-22
TW200418800A (en) 2004-10-01

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