AR076703A1 - (dihidro)imidazoiso[5,1-a]quinolina y composiciones farmaceuticas que los contienen - Google Patents

(dihidro)imidazoiso[5,1-a]quinolina y composiciones farmaceuticas que los contienen

Info

Publication number
AR076703A1
AR076703A1 ARP100101803A ARP100101803A AR076703A1 AR 076703 A1 AR076703 A1 AR 076703A1 AR P100101803 A ARP100101803 A AR P100101803A AR P100101803 A ARP100101803 A AR P100101803A AR 076703 A1 AR076703 A1 AR 076703A1
Authority
AR
Argentina
Prior art keywords
alkyl
amino
hydroxy
optionally substituted
heterocycloalkyl
Prior art date
Application number
ARP100101803A
Other languages
English (en)
Inventor
C M Timmers
Hubert Jan Jozef Loozen
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 AR076703A1 publication Critical patent/AR076703A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Reproductive Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gynecology & Obstetrics (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pregnancy & Childbirth (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Los compuestos pueden ser usados para el tratamiento de la infertilidad. Reivindicacion 1: Un compuesto de (dihidro)imidazoiso[5,1-alfa]quinolina de acuerdo con la formula (1) o una sal farmacéuticamente aceptable de ellos; caracterizado porque el enlace C5-6 puede ser tanto saturado como insaturado; R1 es fenilo o (2-5C)heteroarilo, ambos opcionalmente sustituido por uno o más sustituyentes seleccionados entre R13 o R1 es (1-6C)alquilo, halogeno, ciano, (2-6C)alquenilo, (2-6C)alquinilo, (3-6C)cicloalquilo, (5-6C)cicloalquenilo, (2-5C)heterocicloalquilo o (2-5C)-heterocicloalquenilo; R3 es (di)[(1-6C)alquil]amino, opcionalmente sustituido por hidroxi o es un grupo seleccionado entre (2), (3), (4); o (5) o R3 es (1-6C)alquilo, (3-6C)cicloalquilo, (di)[(1-4C)alquil]amino(1-4C)alquilo o R3 es (2-6C)heterocicloalquilo (2-6C)heterocicloalquil(1-4C)alquilo, la mitad (2-6C)heterocicloalquilo de la cual opcionalmente puede ser sustituido por (1-4C)alquilcarbonilo o (3-6C)cicloalquilcarbonilo, R3 es pirrolidin-1-ilo, azepin-1-ilo, 1,4-oxazepin-1-ilo, todos opcionalmente sustituidos por uno o más sustituyentes (1-4C)alquilo, R8 es H, (1-4C)alquilo, (1-4C)alcoxi, (1-4C)alcoxi(1-4C)alquilo, hidroxi o (2-4C)alquenilo; R9 es H, halogeno, hidroxi, amino, (2-6C)alquinilo, (2-5C)heterocicloalquilo, (3-6C)cicloalcoxi, (2-5C)heterocicloalcoxi, (di)[(1-4C)alquil]aminocarbonilo, (2-5C)heterocicloalquilcarbonilo, (2-5C)heteroarilaminocarbonilo, (2-5C)heterocicloalquilcarbonilamino, (2-5C)heteroarilcarbonilamino, formilo, ciano, nitro, (di)[(1-4C)alquil]aminocarboxi, (1-6C)alquilcarbonilo, (1-4C)alcoxicarbonilo, (di)[(1-4C)alquil]amino, (di)[(1-4C)alquil]aminocarbonilamino, (1-4C)alcoxicarbonilamino, (di)[(1-4C)alquil]aminosulfonilamino, (1-6C)alquiltio o (1-4C)alquilsulfonilamino o R9 es (1-6C)alquilo, (1-6C)alcoxi o (2-6C)alquenilo, todos opcionalmente sustituidos por uno o más sustituyentes seleccionados entre halogeno, hidroxi, amina, azida, (1-4C)alcoxi, (1-4C)alcoxicarbonilamino o (1-4C)alquilcarbonilamino o R9 es (1-5C)heteroarilo, fenilo, (2-5C)heteroariloxi o fenoxi, todos opcionalmente sustituidos por uno o más sustituyentes seleccionados entre R14 o R9 es (1-6C)alquilcarbonilamino, opcionalmente sustituido por hidroxi, amino, (2-5C)heterocicloalquilo o (di)[(1-4C)alquil]amino o R9 es fenilo sustituido en dos posiciones adyacentes representando juntos un anillo O-(CH2)m-O fundido donde m es 1 o 2; R10 es H, metoxi, halogeno o metilo; R11 es H, (1-4C)alquilo o (2-4C)alquenilo; R12 es (1-4C)alquilcarbonilo o (3-6C)cicloalquilcarbonilo, ambos opcionalmente sustituidos por uno o más sustituyentes seleccionados entre R15; R13 es hidroxi, amino, halogeno, nitro, trifluorometilo, ciano, (1-4C)alquilo, (1-4C)alcoxi, (1-4C)alquiltio o (di)[(1-4C)alquil]amino; R14 es hidroxi, amino, halogeno, nitro, trifluorometilo, ciano, (1-4C)alquilo, (1-4C)alcoxi, (1-4C)alquiltio, (di)[(1-4C)alquil]amino, (2-5C)heteroarilo, (di)[(1-4C)alquilaminocarbonilo, (1-4C)alquilcarbonilamino o (1-4C)alquilsulfonilo o R14 es (2-5C)heterocicloalquilo opcionalmente sustituido por (1-4C)alquilo o (1-4C)alcoxicarbonilo; y R15 es hidroxi, amino, halogeno, nitro, trifluorometilo, ciano, (1-4C)alquilo, (1-4C)alcoxi, (1-4C)alquiltio o (di)[(1-4C)alquil]amino.
ARP100101803A 2009-05-27 2010-05-26 (dihidro)imidazoiso[5,1-a]quinolina y composiciones farmaceuticas que los contienen AR076703A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09161274 2009-05-27

Publications (1)

Publication Number Publication Date
AR076703A1 true AR076703A1 (es) 2011-06-29

Family

ID=42315817

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101803A AR076703A1 (es) 2009-05-27 2010-05-26 (dihidro)imidazoiso[5,1-a]quinolina y composiciones farmaceuticas que los contienen

Country Status (8)

Country Link
EP (1) EP2435433B1 (es)
JP (1) JP5647675B2 (es)
CN (1) CN102448961B (es)
AR (1) AR076703A1 (es)
AU (1) AU2010252007B2 (es)
CA (1) CA2763118A1 (es)
TW (1) TWI461426B (es)
WO (1) WO2010136438A1 (es)

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AU2012279416B2 (en) 2011-07-01 2017-04-06 Merck Patent Gmbh Dihydropyrazoles, pharmaceutical compositions thereof and their use for the treatment of fertility disorders
WO2013012848A1 (en) 2011-07-18 2013-01-24 Merck Patent Gmbh Benzamides
WO2013106409A1 (en) 2012-01-10 2013-07-18 Merck Patent Gmbh Benzamide derivatives as modulators of the follicle stimulating hormone
MX2014009416A (es) * 2012-02-08 2014-11-10 Merck Patent Gmbh Analogos de tiazolidinona deuterados como agonistas para el receptor de la hormana foliculo estimulante.
WO2014209978A1 (en) 2013-06-24 2014-12-31 Merck Patent Gmbh Imidazole compounds as modulators of fshr and uses thereof
RU2663898C2 (ru) 2013-06-24 2018-08-13 Мерк Патент Гмбх Пиразольные соединения в качестве модуляторов fshr и их применение
US9493442B2 (en) 2014-02-13 2016-11-15 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP3105226B1 (en) 2014-02-13 2019-09-04 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
CR20200199A (es) 2014-02-13 2020-06-19 Incyte Corp CICLOPROPILAMINA COMO INHIBIDOR DE LA LSD1 (Divisional 2016-0396)
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
WO2015196335A1 (en) 2014-06-23 2015-12-30 Tocopherx, Inc. Pyrazole compounds as modulators of fshr and uses thereof
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
AU2016243939B2 (en) 2015-04-03 2020-09-03 Incyte Holdings Corporation Heterocyclic compounds as LSD1 inhibitors
TWI765860B (zh) 2015-08-12 2022-06-01 美商英塞特公司 Lsd1抑制劑之鹽
JP6999574B2 (ja) 2016-04-22 2022-01-18 インサイト・コーポレイション Lsd1阻害剤の製剤
CN106866692A (zh) * 2017-03-30 2017-06-20 毛阿龙 具有苯并1,4‑二氧杂环己二烯酮结构的fshr拮抗剂的制备方法
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
WO2024077006A1 (en) * 2022-10-05 2024-04-11 Radionetics Oncology, Inc. Follicle-stimulating hormone receptor (fshr) targeted therapeutics and uses thereof

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RO66801A (fr) * 1973-05-25 1979-08-15 Lepetit Spa Procede pour obtenir des derives des triazoloizoquinolines
PH15001A (en) * 1977-07-25 1982-03-22 Sandoz Ag Prolactin secretion inhibitors
IL141063A (en) * 1998-08-07 2005-06-19 Applied Research Systems Derivatives of pyrrolidine-2-carboxylic acid and piperidine-2-carboxylic acids and pharmaceutical compositions comprising said derivatives for treating infertility
CA2452606C (en) * 2001-07-02 2011-09-13 Akzo Nobel N.V. Tetrahydroquinoline derivatives
AU2004226353A1 (en) * 2003-04-01 2004-10-14 Laboratoires Serono Sa Inhibitors of phosphodiesterases in infertility
RS20050945A (en) * 2003-06-30 2008-06-05 Altana Pharma Ag., Novel pyrrolodihydroisoquinolines useful in the treatment of cancer
TW200944523A (en) * 2008-02-08 2009-11-01 Organon Nv (Dihydro)pyrrolo[2,1-a]isoquinolines

Also Published As

Publication number Publication date
AU2010252007A1 (en) 2011-12-22
CN102448961B (zh) 2016-01-06
TW201107322A (en) 2011-03-01
EP2435433B1 (en) 2013-08-28
WO2010136438A1 (en) 2010-12-02
EP2435433A1 (en) 2012-04-04
JP2012528105A (ja) 2012-11-12
AU2010252007B2 (en) 2014-06-05
CN102448961A (zh) 2012-05-09
TWI461426B (zh) 2014-11-21
JP5647675B2 (ja) 2015-01-07
CA2763118A1 (en) 2010-12-02

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