HRP20110344T1 - Derivati dihidropiridina - Google Patents

Derivati dihidropiridina Download PDF

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Publication number
HRP20110344T1
HRP20110344T1 HR20110344T HRP20110344T HRP20110344T1 HR P20110344 T1 HRP20110344 T1 HR P20110344T1 HR 20110344 T HR20110344 T HR 20110344T HR P20110344 T HRP20110344 T HR P20110344T HR P20110344 T1 HRP20110344 T1 HR P20110344T1
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Croatia
Prior art keywords
alkyl
alkynyl
alkenyl
compound according
heteroaryl
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HR20110344T
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English (en)
Inventor
Corine Renee Van Straten Nicole
Geziena Gerritsma Gerritdina
Anders Van Der Veen Lars
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N.V. Organon
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Publication of HRP20110344T1 publication Critical patent/HRP20110344T1/hr

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    • 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • 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
    • 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

Abstract

Derivat dihidropiridina Formule 1, ili njegova farmaceutski prihvatljiva sol, naznačen time štoR1 je (1-6C)alkil, (2-6C)alkenil, (2-6C)alkinil ili fenil i (1-5C)heteroaril, od kojih su oba izborno supstituirani s jednim ili više supstituenata, koje se bira između hidroksi, amino, halogena, nitro, trifluormetila, cijano, (1-4C)alkila, (2-4C)alkenila, (2-4C)alkinila, (1-4C)alkoksi, (1-4C)(di)alkilamino; R2 i R3 su neovisno (1-4C)alkil, (2-4C)alkenil, (2-4C)alkinil, (1-4C)alkoksi, (2-4C)alkeniloksi, (3-4C)alkiniloksi, halogen; R4 je (1-6C)alkil, (2-6C)alkenil, (2-6C)alkinil, (3-6C)cikloalkil, (3-6C)cikloalkenil, (3-6C)cikloalkil(1-4C)alkil, (2-6C)heterocikloalkil, (2-6C)heterocikloalkil(1-4C)alkil ili (6-10C)aril, (6-10C)aril(1-4C)alkil, (1-9C)heteroaril, (1-9C)heteroaril(1-4C)alkil, gdje je (hetero)arilna skupina izborno supstituirana s jednim ili više supstituenata, koje se bira između hidroksi, amino, halogena, nitro, trifluormetila, cijano, (1-4C)alkila, (2-4C)alkenila, (2-4C)alkinila, (1-4C)alkoksi, (1-4C)(di)alkilamino, a ako R4 je fenil, uz (1-4C)alkiltio, (1-4C)alilsulfonil, R5-oksikarbonil, R5-karbonil ili R5,R6-aminokarbonil; X je SO2 CH2, C(O), ili X je odsutan, gdje ako X je CH2, R4 može dodatno biti R5-oksikarbonil ili R5-karbonil; R5 i R6 su neovisno H, (1-4C)alkil, (2-4C)alkenil, (2-4C)alkinil, (3-6C)cikloalkil, (3-6C)cikloalkil(1-4C)alkil, (2-6C)heterocikloalkil, (2-6C)heterocikloalkil(1-4C)alkil, (1-4C)alkoksikarbonil(1-4C)alkil, (1-4C)(di)alkilaminokarbonil(1-4C)alkil ili (6-10C)arilaminokarbonil(1-4C)alkil, (1-9C)heteroarilaminokarbonil(1-4C)alkil, (6-10C)aril, (1-9C)heteroaril, (6-10C)aril(1-4C)alkil, (1-9C)heteroaril(1-4C)alkil, gdje je (hetero)arilna skupina izborno supstituirana s jednim ili više supstituenata, koje se bira između hidroksi, amino, halogena, nitro, trifluormetila, cijano, (1-4C)alkila, (2-4C)alkenila, (2-4C)alkinila, (1-4C)alkoksi, (1-4C)(di)alkilamino; iliR5 i R6 u R5,R6-aminokarbonilu mogu biti vezani u (2-6C)heterocikloalkilni prsten; uz uvjet da spoj nije 2-metil-5-okso-7-fenil-4-(3,4,5-trlmetoksifenil)-1,4,5,6,7,8-heksahidrokinolin-3-karbonitril. Patent sadrži još 11 patentnih zahtjeva.

Claims (12)

1. Derivat dihidropiridina Formule 1, [image] ili njegova farmaceutski prihvatljiva sol, naznačen time što R1 je (1-6C)alkil, (2-6C)alkenil, (2-6C)alkinil ili fenil i (1-5C)heteroaril, od kojih su oba izborno supstituirani s jednim ili više supstituenata, koje se bira između hidroksi, amino, halogena, nitro, trifluormetila, cijano, (1-4C)alkila, (2-4C)alkenila, (2-4C)alkinila, (1-4C)alkoksi, (1-4C)(di)alkilamino; R2 i R3 su neovisno (1-4C)alkil, (2-4C)alkenil, (2-4C)alkinil, (1-4C)alkoksi, (2-4C)alkeniloksi, (3-4C)alkiniloksi, halogen; R4 je (1-6C)alkil, (2-6C)alkenil, (2-6C)alkinil, (3-6C)cikloalkil, (3-6C)cikloalkenil, (3-6C)cikloalkil(1-4C)alkil, (2-6C)heterocikloalkil, (2-6C)heterocikloalkil(1-4C)alkil ili (6-10C)aril, (6-10C)aril(1-4C)alkil, (1-9C)heteroaril, (1-9C)heteroaril(1-4C)alkil, gdje je (hetero)arilna skupina izborno supstituirana s jednim ili više supstituenata, koje se bira između hidroksi, amino, halogena, nitro, trifluormetila, cijano, (1-4C)alkila, (2-4C)alkenila, (2-4C)alkinila, (1-4C)alkoksi, (1-4C)(di)alkilamino, a ako R4 je fenil, uz (1-4C)alkiltio, (1-4C)alilsulfonil, R5-oksikarbonil, R5-karbonil ili R5,R6-aminokarbonil; X je SO2 CH2, C(O), ili X je odsutan, gdje ako X je CH2, R4 može dodatno biti R5-oksikarbonil ili R5-karbonil; R5 i R6 su neovisno H, (1-4C)alkil, (2-4C)alkenil, (2-4C)alkinil, (3-6C)cikloalkil, (3-6C)cikloalkil(1-4C)alkil, (2-6C)heterocikloalkil, (2-6C)heterocikloalkil(1-4C)alkil, (1-4C)alkoksikarbonil(1-4C)alkil, (1-4C)(di)alkilaminokarbonil(1-4C)alkil ili (6-10C)arilaminokarbonil(1-4C)alkil, (1-9C)heteroarilaminokarbonil(1-4C)alkil, (6-10C)aril, (1-9C)heteroaril, (6-10C)aril(1-4C)alkil, (1-9C)heteroaril(1-4C)alkil, gdje je (hetero)arilna skupina izborno supstituirana s jednim ili više supstituenata, koje se bira između hidroksi, amino, halogena, nitro, trifluormetila, cijano, (1-4C)alkila, (2-4C)alkenila, (2-4C)alkinila, (1-4C)alkoksi, (1-4C)(di)alkilamino; ili R5 i R6 u R5,R6-aminokarbonilu mogu biti vezani u (2-6C)heterocikloalkilni prsten; uz uvjet da spoj nije 2-metil-5-okso-7-fenil-4-(3,4,5-trlmetoksifenil)-1,4,5,6,7,8-heksahidrokinolin-3-karbonitril.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R4 je fenil, izborno supstituiran s jednim ili više supstituenata, koje se bira između hidroksi, amino, halogena, nitro, trifluormetila, cijano, (1-4C)alkila, (2-4C)alkenila, (2-4C)alkinila, (1-4C)alkoksi, (1-4C)(di)alkilamino, (1-4C)alkiltio, (1-4C)alkilsulfonila, R5-oksikarbonila, R5-karbonila ili R5,R6-aminokarbonila.
3. Spoj u skladu s patentnim zahtjevom 2, naznačen time što supstituent fenila na položaju R4 je R5,R6-aminokarbonil, (1-4C)alkoksi i/ili halogen.
4. Spoj u skladu s patentnim zahtjevom 3, naznačen time što R5,R6 u R5,R6-aminokarbonilu je (1-4C)(di)alkilamino.
5. Spoj u skladu s patentnim zahtjevom 3, naznačen time što R5 u R5,R6-aminokarbonilu je (1-4C)alkoksikarbonil(1-4C)alkil, a R6 je H.
6. Spoj u skladu s patentnim zahtjevom 3, naznačen time što R5 u R5,R6-aminokarbonilu je (1-9C)heteroaril(1-4C)alkil, gdje je (hetero)arilna skupina izborno supstituirana s jednim ili više supstituenata, koje se bira između hidroksi, amino, halogena, nitro, trifluormetila, cijano, (1-4C)alkila, (2-4C)alkenila, (2-4C)alkinila, (1-4C)alkoksi, (1-4C)(di)alkilamino ili (1-4C)alkoksikarbonil(1-4C)alkila, a R6 je H.
7. Spoj u skladu s patentnim zahtjevima 1-6, naznačen time što X je CH2.
8. Spoj u skladu s patentnim zahtjevima 1-7, naznačen time što R1 je (1-6C)alkil, fenil ili (1-5C)heteroaril.
9. Spoj u skladu s patentnim zahtjevima 1-8, naznačen time što R2 i R3 su halogen i/ili (1-4C)alkoksi.
10. Spoj u skladu s patentnim zahtjevima 1-9, naznačen time što je namijenjen upotrebi u terapiji.
11. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1-9, uključujući 2-metil-5-okso-7-fenil-4-(3,4,5-trimetoksifenil)-1,4,5,6,7,8-heksahidrokinolin-3-karbonitril i farmaceutski prikladne pomoćne tvari.
12. Upotreba spoja u skladu s bilo kojim od patentnih zahtjeva 1-9, uključujući 2-metil-5-okso-7-fenil-4-(3,4,5-trimetoksifenil)-1,4,5,6,7,8-heksahidrokinolin-3-karbonitril, ili njegove farmaceutski prihvatljive soli ili solvata, naznačena time što je navedeni spoj namijenjen proizvodnji medikamenta za liječenje poremećaja plodnosti.
HR20110344T 2005-05-04 2011-05-10 Derivati dihidropiridina HRP20110344T1 (hr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP2005/052042 WO2006117023A1 (en) 2005-05-04 2005-05-04 Dihydropyridine derivatives

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HRP20110344T1 true HRP20110344T1 (hr) 2011-06-30

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US (1) US7994189B2 (hr)
EP (1) EP1879866B1 (hr)
JP (1) JP4869336B2 (hr)
CN (1) CN101171234B (hr)
AT (1) ATE502014T1 (hr)
AU (1) AU2005331482B2 (hr)
BR (1) BRPI0520259A2 (hr)
CA (1) CA2606521C (hr)
CY (1) CY1111642T1 (hr)
DE (1) DE602005027002D1 (hr)
DK (1) DK1879866T3 (hr)
ES (1) ES2361674T3 (hr)
HK (1) HK1110855A1 (hr)
HR (1) HRP20110344T1 (hr)
IL (1) IL186660A0 (hr)
MX (1) MX2007013745A (hr)
NO (1) NO20075579L (hr)
NZ (1) NZ562541A (hr)
PL (1) PL1879866T3 (hr)
PT (1) PT1879866E (hr)
RS (1) RS51784B (hr)
SI (1) SI1879866T1 (hr)
WO (1) WO2006117023A1 (hr)

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UA92007C2 (ru) * 2005-05-04 2010-09-27 Н.В. Органон Производные 4-фенил-5-оксо-1,4,5,6,7,8-гексагидрохинолина для лечения бесплодности
TW200944523A (en) 2008-02-08 2009-11-01 Organon Nv (Dihydro)pyrrolo[2,1-a]isoquinolines
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
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EP2925739A4 (en) * 2012-11-28 2016-07-27 Stichting Dienst Landbouwkundi SUBSTITUTED DIHYDROPYRTOINS FOR PLANTS WITH SOMATIC EMBRYOGENESIS I
CN110357993B (zh) * 2019-07-09 2020-05-05 清华大学 一种可作为抑菌添加剂的含1,4-二氢吡啶结构的新型高分子

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HK1110855A1 (en) 2008-07-25
DK1879866T3 (da) 2011-06-06
CA2606521C (en) 2012-09-18
BRPI0520259A2 (pt) 2009-09-15
ATE502014T1 (de) 2011-04-15
US20090215773A1 (en) 2009-08-27
WO2006117023A1 (en) 2006-11-09
US7994189B2 (en) 2011-08-09
IL186660A0 (en) 2008-01-20
JP2008540349A (ja) 2008-11-20
EP1879866A1 (en) 2008-01-23
CA2606521A1 (en) 2006-11-09
DE602005027002D1 (en) 2011-04-28
MX2007013745A (es) 2008-01-24
SI1879866T1 (sl) 2011-06-30
JP4869336B2 (ja) 2012-02-08
CN101171234A (zh) 2008-04-30
NO20075579L (no) 2008-01-18
RS51784B (en) 2011-12-31
PT1879866E (pt) 2011-06-01
ES2361674T3 (es) 2011-06-21
CN101171234B (zh) 2011-11-16
AU2005331482B2 (en) 2011-06-02
AU2005331482A1 (en) 2006-11-09
CY1111642T1 (el) 2015-10-07
EP1879866B1 (en) 2011-03-16
NZ562541A (en) 2009-02-28
PL1879866T3 (pl) 2011-07-29

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