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

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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16—Drugs 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
    • 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
    • C07D401/10—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 aromatic rings
    • 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

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)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (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
PL2753928T3 (pl) * 2011-09-09 2018-07-31 Quidel Corporation Kompozycje i sposoby wykrywania autoprzeciwciał
KR102394518B1 (ko) * 2014-01-09 2022-05-06 오리온 코포레이션 브로모도메인 억제제로서의 비사이클릭 헤테로사이클릭 유도체
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
CA2452606C (en) * 2001-07-02 2011-09-13 Akzo Nobel N.V. 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
US7560528B2 (en) 2003-06-20 2009-07-14 Efthimios Ippikoglou Method of producing recombinant DNA molecules

Also Published As

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

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