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 contienenInfo
- 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
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic 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.
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) |
Families Citing this family (21)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
-
2010
- 2010-05-06 TW TW099114528A patent/TWI461426B/zh not_active IP Right Cessation
- 2010-05-25 JP JP2012512338A patent/JP5647675B2/ja not_active Expired - Fee Related
- 2010-05-25 AU AU2010252007A patent/AU2010252007B2/en not_active Ceased
- 2010-05-25 CA CA2763118A patent/CA2763118A1/en not_active Abandoned
- 2010-05-25 EP EP10723991.5A patent/EP2435433B1/en not_active Not-in-force
- 2010-05-25 WO PCT/EP2010/057134 patent/WO2010136438A1/en active Application Filing
- 2010-05-25 CN CN201080023361.8A patent/CN102448961B/zh not_active Expired - Fee Related
- 2010-05-26 AR ARP100101803A patent/AR076703A1/es unknown
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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Legal Events
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FB | Suspension of granting procedure |