PE20090955A1 - Compuestos de tetrahidroquinolina como antagonistas del receptor de tsh - Google Patents

Compuestos de tetrahidroquinolina como antagonistas del receptor de tsh

Info

Publication number
PE20090955A1
PE20090955A1 PE2008001465A PE2008001465A PE20090955A1 PE 20090955 A1 PE20090955 A1 PE 20090955A1 PE 2008001465 A PE2008001465 A PE 2008001465A PE 2008001465 A PE2008001465 A PE 2008001465A PE 20090955 A1 PE20090955 A1 PE 20090955A1
Authority
PE
Peru
Prior art keywords
alkyl
phenyl
quinolin
tetrahydro
trimethyl
Prior art date
Application number
PE2008001465A
Other languages
English (en)
Inventor
Willem Frederik Johan Karstens
Paolo Giovanni Martino Conti
Cornelis Marius Timmers
Ralf Plate
Koppen Christianus Johannes Van
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 PE20090955A1 publication Critical patent/PE20090955A1/es

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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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • 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
    • 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
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
    • 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
    • C07D401/10Heterocyclic 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 aromatic rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

REFERIDA A UN DERIVADO DE TETRAHIDROQUINOLINA DE FORMULA (I), DONDE R1 ES H O METILO; X ES UN ENLACE, O, NH, N(ALQUILO C1-C4); R2 ES ALQUILO C1-C4, R5(ALQUILO C1-C4), R9(ALQUILO C2-C4); X ES UN ENLACE O NH; Y ES UN ENLACE, O, NH; R3 ES R6(ALQUILO C1-C6), R6(CICLOALQUILO C3-C6), FENILO, ENTRE OTROS; R4 ES H, ALCOXI C1-C3, (DI)[ALQUIL C1-C3]AMINO; R5 ES CN O PIRIDILO; R6 ES H, CICLOALQUILO C3-C5, FENILO, ENTRE OTROS; R9 ES (DI)[ALQUIL C1-C4]AMINO, HETEROCICLOALQUILO C2-C6. SON COMPUESTOS PREFERIDOS: ACIDO HEXANOICO (1-ACETIL-2,2,4-TRIMETIL-4-FENIL-1,2,3,4-TETRAHIDRO-QUINOLIN-6-IL)-AMIDA, ACIDO 1-METIL-1H-PIRROL-2-CARBOXILICO(1-ACETIL-2,2,4-TRIMETIL-4-FENIL-1,2,3,4-TETRAHIDRO-QUINOLIN-6-IL)-AMIDA, N-(1-ACETIL-2,2,4-TRIMETIL-4-FENIL-1,2,3,4-TETRAHIDRO-QUINOLIN-6-IL)-5-BROMO-2-METILAMINO-BENZAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD ANTAGONISTA DEL RECEPTOR DE LA HORMONA ESTIMULANTE DE LA TIROIDES (TSH) Y SON UTILES EN EL TRATAMIENTO DE HIPERTIROIDISMO, ENFERMEDAD DE GRAVES, BOCIO NODULAR, ENTRE OTRAS
PE2008001465A 2007-08-31 2008-08-29 Compuestos de tetrahidroquinolina como antagonistas del receptor de tsh PE20090955A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07115368 2007-08-31
EP08150398 2008-01-18

Publications (1)

Publication Number Publication Date
PE20090955A1 true PE20090955A1 (es) 2009-07-23

Family

ID=40387927

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008001465A PE20090955A1 (es) 2007-08-31 2008-08-29 Compuestos de tetrahidroquinolina como antagonistas del receptor de tsh

Country Status (13)

Country Link
US (1) US9174940B2 (es)
EP (1) EP2197445B1 (es)
JP (1) JP5467044B2 (es)
KR (1) KR20100063105A (es)
CN (1) CN101790376B (es)
AR (1) AR068065A1 (es)
AU (1) AU2008292134B2 (es)
CA (1) CA2695503A1 (es)
CL (1) CL2008002566A1 (es)
MX (1) MX2010002192A (es)
PE (1) PE20090955A1 (es)
TW (1) TW200918058A (es)
WO (1) WO2009027482A2 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090124651A1 (en) 2007-08-31 2009-05-14 H. Lundbeck A/S Catecholamine derivatives and prodrugs thereof
JP5908590B2 (ja) * 2011-09-09 2016-04-26 クイデル コーポレーション 自己抗体を検出するための組成物および方法
RS57586B1 (sr) * 2014-01-09 2018-11-30 Orion Corp Biciklični heterociklični derivati kao inhibitori bromodomena
KR101686881B1 (ko) * 2014-07-25 2016-12-20 연세대학교 산학협력단 스타틴을 포함하는 갑상선 안병증의 예방 또는 치료용 약제학적 조성물
TW202408996A (zh) * 2022-06-30 2024-03-01 日商橘生藥品工業股份有限公司 3,4-二氫喹啉-2(1h)-酮化合物

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4237430C1 (de) * 1992-11-05 1994-03-17 Henning Berlin Gmbh Aufgereinigtes TSH-Präparat, Verfahren zu seiner Herstellung und seine Verwendung zur Herstellung von TSH-Tracern für TSH-Rezeptorassays und in TSH-Rezeptorassays
JPH0789991A (ja) * 1993-09-28 1995-04-04 Mitsubishi Chem Corp 新規なポリペプチドおよびそれを用いるtsh受容体抗体の測定法
JPH09140386A (ja) * 1995-11-22 1997-06-03 Eiken Chem Co Ltd 甲状腺機能を刺激する活性を持つ抗体
EP1406628B1 (en) * 2001-07-02 2006-03-08 Akzo Nobel N.V. 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
DK1594991T3 (da) * 2003-06-20 2007-01-29 Serum Biomedical Inst Fremgangsmåde til fremstilling af DNA-molekyler

Also Published As

Publication number Publication date
AU2008292134A1 (en) 2009-03-05
US20110172267A1 (en) 2011-07-14
JP5467044B2 (ja) 2014-04-09
CL2008002566A1 (es) 2009-01-02
WO2009027482A2 (en) 2009-03-05
CN101790376B (zh) 2013-06-12
WO2009027482A3 (en) 2009-05-28
TW200918058A (en) 2009-05-01
AU2008292134B2 (en) 2013-06-13
US9174940B2 (en) 2015-11-03
EP2197445A2 (en) 2010-06-23
MX2010002192A (es) 2010-03-17
JP2010536934A (ja) 2010-12-02
EP2197445B1 (en) 2017-04-19
KR20100063105A (ko) 2010-06-10
CN101790376A (zh) 2010-07-28
CA2695503A1 (en) 2009-03-05
AR068065A1 (es) 2009-11-04

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