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AR042630A1 - Derivados de tetrahidroquinolina, composiciones farmaceuticas que los incluyen y su uso como medicamento. - Google Patents

Derivados de tetrahidroquinolina, composiciones farmaceuticas que los incluyen y su uso como medicamento.

Info

Publication number
AR042630A1
AR042630A1 ARP030104729A ARP030104729A AR042630A1 AR 042630 A1 AR042630 A1 AR 042630A1 AR P030104729 A ARP030104729 A AR P030104729A AR P030104729 A ARP030104729 A AR P030104729A AR 042630 A1 AR042630 A1 AR 042630A1
Authority
AR
Argentina
Prior art keywords
alkoxy
derivatives
alkylamino
pharmaceutical compositions
tetrahydroquinoline
Prior art date
Application number
ARP030104729A
Other languages
English (en)
Inventor
Cornelis Marius Timmers
Willem Frederik Johan Kartens
Original Assignee
Akzo 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 Akzo Nv filed Critical Akzo Nv
Publication of AR042630A1 publication Critical patent/AR042630A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A61P5/08Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/38Nitrogen atoms
    • C07D215/42Nitrogen atoms attached in position 4
    • C07D215/44Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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

La presente se relaciona con composiciones farmacéuticas que comprenden estos derivados y con la utilización de estos derivados para regular la fertilidad. Reivindicación 1: Un derivado de tetrahidroquinolina, de acuerdo con la fórmula (1), o una sal farmacéuticamente aceptable de él, caracterizado porque R1 y R2 son H o Me; R3 es H, hidroxi, alcoxi (C1-4), (di)alquilamino(C1-4)-alcoxi(C2-4) o heterocicloalquil(C2-6)-alcoxi(C2-4); R4 es H, OH, alcoxi (C1-4) o R7; R5 es H, OH, alcoxi (C1-4) o R7; con la condición de que si R4 es H, R5 no es H, OH o alcoxi (C1-4) y de que si R5 es H, R4 no es H, OH o alcoxi (C1-4); R6 es heteroaril (C2-5), aril(C6), cicloalquil (C3-8), heterocicloalquil C2-6) o alquil (C1-6); R7 es amino, (di)alquilamino (C1-4), arilcarbonilamino(C6), arilcarboniloxi(C6), heteroarilcarbonilamino (C2-5), heteroarilcarboniloxi (C2-5), R8-alquilamino (C2-4), R8-alcoxi (C2-4), R9-metilamino o R9-metoxi; R8 es hidroxi, amino, alcoxi (C1-4), (di)alquilamino (C1-4), heterocicloalquil (C2-6), heterocicloalquilcarbonilamino (C2-6), (di)alquilaminocarbonilamino (C1-4), alcoxicarbonilamino (C1-4) y R9 es aminocarbonil, (di)alquilaminocarbonil (C1-4), heteroaril (C2-5) o aril(C6).
ARP030104729A 2002-12-20 2003-12-19 Derivados de tetrahidroquinolina, composiciones farmaceuticas que los incluyen y su uso como medicamento. AR042630A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
AR042630A1 true AR042630A1 (es) 2005-06-29

Family

ID=39311811

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030104729A AR042630A1 (es) 2002-12-20 2003-12-19 Derivados de tetrahidroquinolina, composiciones farmaceuticas que los incluyen y su uso como medicamento.

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
HRP20031080A2 (en) * 2001-07-02 2004-04-30 Akzo Nobel Nv Tetrahydroquinoline derivatives
TWI306855B (en) 2002-12-20 2009-03-01 Organon Nv Tetrahydroquinoline derivatives
TWI322012B (en) * 2002-12-20 2010-03-21 Organon Nv Tetrahydroquinoline derivatives
US7691848B2 (en) 2005-03-02 2010-04-06 Wyeth Pyrrolobenzodiazepine arylcarboxamides and derivatives thereof as follicle-stimulating hormone receptor antagonists
AU2006247601A1 (en) 2005-05-12 2006-11-23 Wyeth Pyrrolobenzodiazepines and heterocyclic carboxamide derivatives as follicle stimulating hormone receptor (FSH-R) antagonists
BRPI0611720A2 (pt) 2005-06-09 2016-11-22 Wyeth Corp "composto, composição, e, métodos de inibir a fertilidade,de evitar a concepção, e de bloquear o desenvolvimento folicular mediado por fsh em um mamífero"
CN101312720A (zh) * 2005-11-30 2008-11-26 安斯泰来制药有限公司 2-氨基苯甲酰胺衍生物
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
EP0303306B1 (en) 1987-08-08 1993-03-10 Akzo N.V. Contraceptive implant
CZ285937B6 (cs) * 1992-01-16 1999-12-15 Hoechst Aktiengesellschaft Arylcykloalkylové deriváty, způsob přípravy těchto derivátů a jejich použití
NZ300739A (en) * 1994-12-22 2000-05-26 Ligand Pharm Inc Steroid receptor modulator compounds
DE69931975T2 (de) * 1998-08-07 2006-10-05 Applied Research Systems Ars Holding N.V. FSH Mimetika zur Behandlung von Infertilität
US6200963B1 (en) * 1999-03-31 2001-03-13 American Home Products Corporation Aryl sulfonic acids as FSH antagonists
HRP20031080A2 (en) * 2001-07-02 2004-04-30 Akzo Nobel Nv Tetrahydroquinoline derivatives
TWI306855B (en) 2002-12-20 2009-03-01 Organon Nv Tetrahydroquinoline derivatives
TWI322012B (en) * 2002-12-20 2010-03-21 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
UA81442C2 (en) 2008-01-10
CL2003002685A1 (es) 2005-04-08
PL377318A1 (pl) 2006-01-23
TWI306855B (en) 2009-03-01
WO2004056780A2 (en) 2004-07-08
JP4545001B2 (ja) 2010-09-15
RS20050457A (sr) 2007-08-03
WO2004056780A3 (en) 2004-08-05
PE20040928A1 (es) 2004-12-25
AU2003298363A1 (en) 2004-07-14
AU2003298363B2 (en) 2009-09-24
US7858794B2 (en) 2010-12-28
ES2321830T3 (es) 2009-06-12
RU2328488C2 (ru) 2008-07-10
TW200418800A (en) 2004-10-01
NZ540578A (en) 2006-12-22
ATE423771T1 (de) 2009-03-15
EP1578726A2 (en) 2005-09-28
BR0317518A (pt) 2005-11-16
RS51293B (sr) 2010-12-31
RU2005122946A (ru) 2005-12-20
JP2006512347A (ja) 2006-04-13
CA2508952C (en) 2011-09-13
US20060142334A1 (en) 2006-06-29
EP1578726B1 (en) 2009-02-25
CA2508952A1 (en) 2004-07-08

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