PE20040928A1 - Derivados de tetrahidroquinolinas como moduladores del receptor fsh - Google Patents
Derivados de tetrahidroquinolinas como moduladores del receptor fshInfo
- Publication number
- PE20040928A1 PE20040928A1 PE2004000023A PE2004000023A PE20040928A1 PE 20040928 A1 PE20040928 A1 PE 20040928A1 PE 2004000023 A PE2004000023 A PE 2004000023A PE 2004000023 A PE2004000023 A PE 2004000023A PE 20040928 A1 PE20040928 A1 PE 20040928A1
- Authority
- PE
- Peru
- Prior art keywords
- alcoxy
- dimetoxy
- trimethyl
- phenyl
- fsh receptor
- Prior art date
Links
- 150000003530 tetrahydroquinolines Chemical class 0.000 title abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- 150000003973 alkyl amines Chemical class 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- -1 AMINO Chemical group 0.000 abstract 1
- 201000009273 Endometriosis Diseases 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical class [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- 208000000509 infertility Diseases 0.000 abstract 1
- 230000036512 infertility Effects 0.000 abstract 1
- 231100000535 infertility Toxicity 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 210000002307 prostate Anatomy 0.000 abstract 1
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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
-
- 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
- A61P15/18—Feminine contraceptives
-
- 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
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
-
- 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
- C07D215/42—Nitrogen atoms attached in position 4
- C07D215/44—Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen atoms
-
- 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
-
- 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
- C07D409/14—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic 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
- C07D413/12—Heterocyclic 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (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
SE REFIERE DERIVADOS DE TETRAHIDROQUINOLINA DE FORMULA I, DONDE R1 Y R2 SON H O Me; R3 ES H, HIDROXI, ALCOXI(C1-C4), (DI)ALQUILAMINO(C1-C4)-ALCOXI(C2-C4) O HETEROCICLOALQUIL(C2-C6)-ALCOXI(C2-C4); R4 Y R5 SON H, OH, ALCOXI(C1-C4) O R7; CON LA CONDICION DE QUE SI R4 ES H, R5 NO ES H, OH O ALCOXI(C1-C4) Y DE QUE SI R5 ES H, R4 NO ES H, OH o ALCOXI(C1-C4); R6 ES HETEROARIL(C2-C5), ARIL(C6), CICLOALQUILO(C3-C8), HETEROCICLOALQUIL(C2-C6) O ALQUIL(C1-C6), R7 ES AMINO, (DI)ALQUILAMINO(C1-C4), ARILCARBONILAMINO(C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N-[1-ACETIL-5,7-DIMETOXI-4-(4-METOXI-FENIL)-2,2,4-TRIMETIL-1,2,3,4-TETRAHIDRO-QUINOLINA-6-IL]-3-CLORO-2,6-DIMETOXI-BENZAMIDA, 4,5-DIMETIL-FURAN-2-ACIDO CARBOXILICO [1-ACETIL-5,7-DIMETOXI-4-(4-METOXI-FENIL)-2,2,4-TRIMETIL-1,2,3,4-TETRAHIDRO-QUINOLINA-6-IL]-AMIDA, 5-BROMO-TIOFENO-2-ACIDO ACRBOXILICO [1-ACETIL5,7-DIMETOXI-4-(4-METOXI-FENIL)-2,2,4-TRIMETIL-1,2,3,4-TETRAHIDRO-QUINOLINA-6-IL]-AMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA QUE LOS CONTIENE. ESTOS COMPUESTOS SON MODULARES DEL RECEPTOR DE FSH YA QUE PUEDEN UTILIZARSE COMO AGONISTAS(PARCIALES) O ANTAGONISTAS(PARCIALES) DEL RECEPTOR FSH, Y PUEDEN UTILIZARSE PARA TRATAR LA INFERTILIDAD, PARA LA ANTICONCEPCION Y PARA EL TRATAMIENTO DE DESORDENES HORMONO-DEPENDIENTES COMO CANCER DE MAMAS, DE PROSTATA Y ENDOMETRIOSIS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02102866 | 2002-12-20 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20040928A1 true PE20040928A1 (es) | 2004-12-25 |
Family
ID=39311811
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2004000023A PE20040928A1 (es) | 2002-12-20 | 2004-01-05 | Derivados de tetrahidroquinolinas como moduladores del receptor fsh |
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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4523273B2 (ja) * | 2001-07-02 | 2010-08-11 | ナームローゼ・フエンノートチヤツプ・オルガノン | テトラヒドロキノリン誘導体 |
| 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 |
| JP2008540567A (ja) | 2005-05-12 | 2008-11-20 | ワイス | 卵胞刺激ホルモン受容体（ｆｓｈ−ｒ）アンタゴニストとしてのピロロベンゾジアゼピンおよびヘテロ環状カルボキサミド誘導体 |
| US7678787B2 (en) | 2005-06-09 | 2010-03-16 | Wyeth | Pyrrolobenzodiazepine pyridine carboxamides and derivatives as follicle-stimulating hormone receptor antagonists |
| EP1955697B1 (en) * | 2005-11-30 | 2012-05-02 | Astellas Pharma Inc. | 2-aminobenzamide derivatives as vanilloid receptor 1 (vr1) inhibitors useful for the treatment of pain or bladder function disorder |
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2686182A (en) * | 1950-12-07 | 1954-08-10 | Basf Ag | O-hydroxy-dihydro-quinoline carboxylic acids |
| ES2054784T3 (es) | 1987-08-08 | 1994-08-16 | Akzo Nv | Un metodo para la fabricacion de un implante. |
| CZ285937B6 (cs) * | 1992-01-16 | 1999-12-15 | Hoechst Aktiengesellschaft | Arylcykloalkylové deriváty, způsob přípravy těchto derivátů a jejich použití |
| HUT78117A (hu) | 1994-12-22 | 1999-11-29 | Ligand Pharmaceuticals Incorporated | Szteroid receptor modulátor kinolin- és kondenzált kinolinszármazékok, eljárás előállításukra és az ezeket tartalmazó gyógyszerkészítmények |
| 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 |
| US6200963B1 (en) * | 1999-03-31 | 2001-03-13 | American Home Products Corporation | Aryl sulfonic acids as FSH antagonists |
| JP4523273B2 (ja) * | 2001-07-02 | 2010-08-11 | ナームローゼ・フエンノートチヤツプ・オルガノン | テトラヒドロキノリン誘導体 |
| 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 |
-
2003
- 2003-12-15 TW TW092135447A patent/TWI306855B/zh not_active IP Right Cessation
- 2003-12-16 AT AT03796105T patent/ATE423771T1/de not_active IP Right Cessation
- 2003-12-16 RS YUP-2005/0457A patent/RS51293B/sr unknown
- 2003-12-16 NZ NZ540578A patent/NZ540578A/en not_active IP Right Cessation
- 2003-12-16 WO PCT/EP2003/051025 patent/WO2004056780A2/en not_active Ceased
- 2003-12-16 PL PL377318A patent/PL377318A1/pl not_active Application Discontinuation
- 2003-12-16 EP EP03796105A patent/EP1578726B1/en not_active Expired - Lifetime
- 2003-12-16 ES ES03796105T patent/ES2321830T3/es not_active Expired - Lifetime
- 2003-12-16 UA UAA200505288A patent/UA81442C2/xx unknown
- 2003-12-16 US US10/540,336 patent/US7858794B2/en not_active Expired - Lifetime
- 2003-12-16 JP JP2004561499A patent/JP4545001B2/ja not_active Expired - Fee Related
- 2003-12-16 CA CA2508952A patent/CA2508952C/en not_active Expired - Lifetime
- 2003-12-16 BR BR0317518-9A patent/BR0317518A/pt active Search and Examination
- 2003-12-16 RU RU2005122946/04A patent/RU2328488C2/ru not_active IP Right Cessation
- 2003-12-16 AU AU2003298363A patent/AU2003298363B2/en not_active Ceased
- 2003-12-18 CL CL200302685A patent/CL2003002685A1/es unknown
- 2003-12-19 AR ARP030104729A patent/AR042630A1/es unknown
-
2004
- 2004-01-05 PE PE2004000023A patent/PE20040928A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| PL377318A1 (pl) | 2006-01-23 |
| TW200418800A (en) | 2004-10-01 |
| JP2006512347A (ja) | 2006-04-13 |
| AU2003298363A1 (en) | 2004-07-14 |
| EP1578726A2 (en) | 2005-09-28 |
| AU2003298363B2 (en) | 2009-09-24 |
| CA2508952A1 (en) | 2004-07-08 |
| RS20050457A (sr) | 2007-08-03 |
| WO2004056780A2 (en) | 2004-07-08 |
| AR042630A1 (es) | 2005-06-29 |
| TWI306855B (en) | 2009-03-01 |
| CL2003002685A1 (es) | 2005-04-08 |
| RU2328488C2 (ru) | 2008-07-10 |
| CA2508952C (en) | 2011-09-13 |
| UA81442C2 (en) | 2008-01-10 |
| JP4545001B2 (ja) | 2010-09-15 |
| US20060142334A1 (en) | 2006-06-29 |
| ES2321830T3 (es) | 2009-06-12 |
| NZ540578A (en) | 2006-12-22 |
| EP1578726B1 (en) | 2009-02-25 |
| ATE423771T1 (de) | 2009-03-15 |
| US7858794B2 (en) | 2010-12-28 |
| BR0317518A (pt) | 2005-11-16 |
| RS51293B (sr) | 2010-12-31 |
| WO2004056780A3 (en) | 2004-08-05 |
| RU2005122946A (ru) | 2005-12-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |