HRP20110624T1 - Supstituirani piperazinilpirazini kao antagonisti receptora 5-ht7 - Google Patents

Supstituirani piperazinilpirazini kao antagonisti receptora 5-ht7 Download PDF

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Publication number
HRP20110624T1
HRP20110624T1 HR20110624T HRP20110624T HRP20110624T1 HR P20110624 T1 HRP20110624 T1 HR P20110624T1 HR 20110624 T HR20110624 T HR 20110624T HR P20110624 T HRP20110624 T HR P20110624T HR P20110624 T1 HRP20110624 T1 HR P20110624T1
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HR
Croatia
Prior art keywords
compound according
pharmaceutically acceptable
acceptable salt
fluorine
methyl
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HR20110624T
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English (en)
Inventor
Philip Cohen Michael
Ann Filla Sandra
Lynne Hellman Sarah
Patrick Hollinshead Sean
Wade Tidwell Michael
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Eli Lilly & Company
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Publication of HRP20110624T1 publication Critical patent/HRP20110624T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D241/20Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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

Abstract

Spoj formule: naznačen time što: A je -C(H)= ili -N=,R1 se bira iz skupine koju čine fenil, izborno supstituiran s metoksi ili 1 do 3 neovisno odabrana supstituenta, klora ili fluora; pirazol-4-il, izborno supstituiran s 1 do 3 metilne ili etilne skupine; imidazolil, izborno supstituiran s 1 ili 2 metila ili etila; piridil, izborno supstituiran s fluorom ili klorom; te tienil; R2 je vodik ili metil; m je 0, 1 ili 2; R3 se bira iz skupine koju čine vodik, fluor, klor, hidroksi, metoksi, hidroksimetil, cijanometil, metoksimetil, acetil, metilkarbonilamino, metilkarbonilaminometil, pirazol-1-ilmetil i triazolilmetil, uz uvjet da kada R3 je vodik, m nije 0; svaki R4 se neovisno bira iz skupine koju čine fluor, klor, metil i metoksi; ili su, alternativno, dvije skupine R4, zajedno s fenilom na kojeg su vezane, povezane u indol-4-ilnu skupinu; ili njegova farmaceutski prihvatljiva sol. Patent sadrži još 17 patentnih zahtjeva.

Claims (18)

1. Spoj formule: [image] naznačen time što: A je -C(H)= ili -N=, R1 se bira iz skupine koju čine fenil, izborno supstituiran s metoksi ili 1 do 3 neovisno odabrana supstituenta, klora ili fluora; pirazol-4-il, izborno supstituiran s 1 do 3 metilne ili etilne skupine; imidazolil, izborno supstituiran s 1 ili 2 metila ili etila; piridil, izborno supstituiran s fluorom ili klorom; te tienil; R2 je vodik ili metil; m je 0, 1 ili 2; R3 se bira iz skupine koju čine vodik, fluor, klor, hidroksi, metoksi, hidroksimetil, cijanometil, metoksimetil, acetil, metilkarbonilamino, metilkarbonilaminometil, pirazol-1-ilmetil i triazolilmetil, uz uvjet da kada R3 je vodik, m nije 0; svaki R4 se neovisno bira iz skupine koju čine fluor, klor, metil i metoksi; ili su, alternativno, dvije skupine R4, zajedno s fenilom na kojeg su vezane, povezane u indol-4-ilnu skupinu; ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što A je -N=; ili njegova farmaceutski prihvatljiva sol.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što A je -CH=; ili njegova farmaceutski prihvatljiva sol.
4. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 3, naznačen time što R1 je fenil, izborno supstituiran s metoksi ili s 1 do 3 neovisno odabrana supstituenta, klora ili fluora; ili njegova farmaceutski prihvatljiva sol.
5. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 3, naznačen time što R1 je pirazol-4-il, izborno supstituiran s 1 do 3 metilne ili etilne skupine; ili njegova farmaceutski prihvatljiva sol.
6. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 3, naznačen time što R1 je imidazolil, izborno supstituiran s 1 ili 2 metila ili etila; ili njegova farmaceutski prihvatljiva sol.
7. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 3, naznačen time što R1 je piridil, izborno supstituiran s fluorom ili klorom; ili njegova farmaceutski prihvatljiva sol.
8. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 3, naznačen time što R1 je tienil; ili njegova farmaceutski prihvatljiva sol.
9. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 8, naznačen time što R3 je fluor, hidroksimetil, metoksimetil ili cijanometil; ili njegova farmaceutski prihvatljiva sol.
10. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 8, naznačen time što R3 je fluor ili metoksimetil; ili njegova farmaceutski prihvatljiva sol.
11. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 8, naznačen time što R3 je fluor; ili njegova farmaceutski prihvatljiva sol.
12. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 8, naznačen time što R3 je metoksimetil; ili njegova farmaceutski prihvatljiva sol.
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je {2-[3'-(4-metoksimetilfenil)-2,3,5,6-tetrahidro[1,2']bipirazinil-4-il]etil}metilamid 1-metil-1H-pirazol-4-sulfonske kiseline; ili njegova farmaceutski prihvatljiva sol.
14. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je {2-[3'-(4-hidroksimetilfenil)-2,3,5,6-tetrahidro[1,2']bipirazinil-4-il]etil}metilamid 1-metil-1H-pirazol-4-sulfonske kiseline; ili njegova farmaceutski prihvatljiva sol.
15. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo koji od patentnih zahtjeva 1 do 14 kao aktivni sastojak u smjesi s farmaceutski prihvatljivom podlogom, razrjeđivačem ili pomoćnom tvari.
16. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 14, naznačen time što je namijenjen upotrebi u terapiji.
17. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 14, naznačen time što je namijenjen upotrebi u liječenju migrene kod ljudi.
18. Spoj u skladu s bilo koji od patentnih zahtjeva 1 do 14, naznačen time što je namijenjen upotrebi u profilaktičkom liječenju migrene kod ljudi.
HR20110624T 2007-08-28 2011-08-30 Supstituirani piperazinilpirazini kao antagonisti receptora 5-ht7 HRP20110624T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US96834407P 2007-08-28 2007-08-28
US4875208P 2008-04-29 2008-04-29
PCT/US2008/073543 WO2009029439A1 (en) 2007-08-28 2008-08-19 Substituted piperazinyl pyrazines and pyridines as 5-ht7 receptor antagonists

Publications (1)

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HRP20110624T1 true HRP20110624T1 (hr) 2011-09-30

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US (1) US8048884B2 (hr)
EP (1) EP2188268B1 (hr)
JP (1) JP5290293B2 (hr)
KR (1) KR101148616B1 (hr)
CN (1) CN101790522B (hr)
AR (1) AR068111A1 (hr)
AT (1) ATE520673T1 (hr)
AU (1) AU2008293715B2 (hr)
BR (1) BRPI0816468A2 (hr)
CA (1) CA2694911C (hr)
CY (1) CY1111848T1 (hr)
DK (1) DK2188268T3 (hr)
EA (1) EA017809B1 (hr)
HR (1) HRP20110624T1 (hr)
MX (1) MX2010002352A (hr)
PE (1) PE20090629A1 (hr)
PL (1) PL2188268T3 (hr)
PT (1) PT2188268E (hr)
SI (1) SI2188268T1 (hr)
TW (1) TW200914020A (hr)
WO (1) WO2009029439A1 (hr)

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FI118473B (fi) 2006-02-17 2007-11-30 Outotec Oyj Menetelmä kuparin talteenottamiseksi kuparisulfidimalmista
CN101821257B (zh) * 2007-10-12 2013-05-22 伊莱利利公司 5-ht7受体拮抗剂
JP5826822B2 (ja) 2010-04-16 2015-12-02 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH 有害生物防除薬としての新規な複素環化合物
CN103857670B (zh) 2011-10-11 2016-03-23 Ucb医药有限公司 2-氧代-哌啶基衍生物
FR2995605B1 (fr) 2012-09-18 2014-09-19 Sanofi Sa Derives de macrolides, leur preparation et leur application therapeutique.
EP3083563A1 (en) 2013-12-20 2016-10-26 Laboratorios Del. Dr. Esteve, S.A. Piperazine derivatives having multimodal activity against pain
US11505529B2 (en) 2017-03-03 2022-11-22 National Taiwan University 8-phenyl-isoquinolines and pharmaceutical composition thereof used in the treatment of irritable bowel syndrome
KR102014335B1 (ko) * 2017-12-01 2019-08-26 한국과학기술연구원 5-ht7 수용체의 조절제로 작용하는 아릴피라졸릴피페라진 또는 아릴피라졸릴다이아제페인의 유도체 및 이를 포함하는 중추신경계 질환 치료 또는 예방용 약학 조성물

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KR20010102003A (ko) * 1999-02-10 2001-11-15 피터 지. 스트링거 5-ht1f 효능제
US20030008880A1 (en) * 2001-05-02 2003-01-09 Pfizer Inc. 4-(2-Pyridyl) piperizines having 5HT7 receptor agonist activity
US7153858B2 (en) 2003-01-31 2006-12-26 Epix Delaware, Inc. Arylpiperazinyl compounds
WO2004067703A2 (en) * 2003-01-31 2004-08-12 Pfizer Products Inc. 5ht7 antagonists and inverse agonists

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DK2188268T3 (da) 2011-10-03
BRPI0816468A2 (pt) 2015-03-24
EA017809B1 (ru) 2013-03-29
CN101790522B (zh) 2012-06-27
KR101148616B1 (ko) 2012-05-21
WO2009029439A1 (en) 2009-03-05
PE20090629A1 (es) 2009-05-16
KR20100038117A (ko) 2010-04-12
JP2010537994A (ja) 2010-12-09
PL2188268T3 (pl) 2011-12-30
PT2188268E (pt) 2011-10-03
EA201070321A1 (ru) 2010-08-30
JP5290293B2 (ja) 2013-09-18
MX2010002352A (es) 2010-08-04
EP2188268B1 (en) 2011-08-17
US20100075976A1 (en) 2010-03-25
AU2008293715B2 (en) 2013-09-19
AU2008293715A1 (en) 2009-03-05
AR068111A1 (es) 2009-11-04
ATE520673T1 (de) 2011-09-15
CY1111848T1 (el) 2015-10-07
CA2694911C (en) 2013-05-07
CN101790522A (zh) 2010-07-28
CA2694911A1 (en) 2009-03-05
EP2188268A1 (en) 2010-05-26
TW200914020A (en) 2009-04-01
SI2188268T1 (sl) 2011-11-30
US8048884B2 (en) 2011-11-01

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