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ME01988B - Hidroksimetil pirolidini kao agonisti beta 3 adrenergičkog receptora - Google Patents

Hidroksimetil pirolidini kao agonisti beta 3 adrenergičkog receptora

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Publication number
ME01988B
ME01988B MEP-2012-549A MEP54912A ME01988B ME 01988 B ME01988 B ME 01988B ME P54912 A MEP54912 A ME P54912A ME 01988 B ME01988 B ME 01988B
Authority
ME
Montenegro
Prior art keywords
pharmaceutically acceptable
group
stereoisomer
acceptable salt
optionally substituted
Prior art date
Application number
MEP-2012-549A
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English (en)
French (fr)
Inventor
Scott D Edmondson
Gregori J Morriello
Chris R Moyes
Dong-Ming Shen
Liping Wang
Cheng Zhu
Richard Berger
Lehua Chang
Stephen D Goble
Sookhee Nicole Ha
Nam Fung Kar
Ihor E Kopka
Bing Li
Original Assignee
Merck Sharp & Dohme
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Filing date
Publication date
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of ME01988B publication Critical patent/ME01988B/me

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/06—Anti-spasmodics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

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  • Chemical & Material Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pyridine Compounds (AREA)

Claims (22)

1.Jedinjenje formule I, ili njegova farmaceutski prihvatljiva so, ili njegov stereoizmer, ili farmaceutski prihvatljiva so njegovog stereoizomera: u kome m je 0, 1, 2, 3 ili 4; nje 0, 1, 2, 3, 4 ili 5, p je 0, 1 ili 2; q je 0, 1, 2, 3 ili 4; t je 0, 1, 2, 3, 4 ili 5; X je -CO- ili -SO2-; Y je izabran iz grupe koju čine: (1)    C1-C5 alkandiil, C2-C5 alkendiil i C2-C5 alkindiil, gde je svaki od alkandiil, alkendiil i alkindiil izborno supstituisan sa jednom do tri grupe nezavisno izabrane od halogena, -ORa, -S(0)p-C1-C3 alkila; (2)    -(CRaRa)j-Q-(CRaRa)k, gde su j i k celi brojevi nezavisno izabrani od 0, 1 i 2, (3)    veza, i (4)    fenilen izborno supstituisan sa jednom do tri grupe nezavisno izabrane od R1; Z je izabran iz grupe koju čine: (1)    fenil, (2)    5- ili 6-člani heterociklični prsten sa od 1 do 4 heteroatoma izabrana od kiseonika, sumpora i azota, (3)    benzenov prsten fuzionisan za C5-C10 karbocikličan prsten, (4)    5- ili 6-člani heterociklični prsten sa od 1 do 4 heteroatoma izabrana od kiseonika, sumpora i azota, fuzionisan za 5- ili 6-člani heterociklični prsten sa od 1 do 4 heteroatoma izabrana od kiseonika, sumpora i azota, i (5) 5- ili 6-člani heterociklični prsten sa od 1 do 4 heteroatoma izabrana od kiseonika, sumpora i azota fuzionisan za C5-C10 karbocikličan prsten; R1 je izabran iz grupe koju čine: (1)    C1-C5 alkil izborno supstituisan sa 1 do 5 atoma halogena, (2)    C3-C6 cikloalkil, (3)    halogen, (4)    nitro, (5)    cijano, (6)    -C(O)Ra, (7)    -C(O)2Ra, (8)    -C(O)NRaRb, i (9)    -QRb; R2 je izabran iz grupe koju čine halogen i C1-C5 alkil; R3 je izabran iz grupe koju čine: (1) C1-C6 alkil izborno supstituisan sa 1 do 5 grupa nezavisno izabranih od halogena, -ORa, -CO2Ra i -CONRaRb, (2)    -(CH2)t-fenil ili -(CH2)t-O-fenil, i gde je navedeni fenil u svakom izborno supstituisan sa 1 do 3 grupe nezavisno izabrane od halogena, C1-C5 alkila izborno supstituisanog sa 1 do 5 atoma halogena, i -ORa, (3)    okso, (4)    tiokso, (5)    halogen, (6)    -CN, (7)    C3-C6 cikloalkil, (8)    -(CH2)t-heterocikličan prsten ili -(CH2)t-0-heterocikličan prsten, i gde je svaki heterocikličan prsten u svakom 5- ili 6-člani prsten sa od 1 do 4 heteroatoma izabrana od kiseonika, sumpora i azota, i gde je navedeni heterociklični prsten izborno orto-fuzionisan za benzenov prsten, i izborno supstituisan sa 1 do 3 grupe nezavisno izabrane od halogena, C1-C5 alkila izborno supstituisanog sa 1 do 5 atoma halogena, i -ORa, (9)    -ORa, (10)    -C(0)0Ra, (11)    -C(0)Ra, (12)    -C(0)NRaRb, (12) -NRaRb (13)    -NRaC(0)Rb, (14)    -NRaC(0)ORb, i (15)    -NRaC(0)NRaRb; Ra je izabran iz grupe koju čine vodonik i C1-C6 alkil izborno supstituisan sa 1 do 5 atoma halogena; Rb je izabran iz grupe koju čine: (1)    vodonik, (2)    C1-C6 alkil izborno supstituisan sa 1 do 5 grupa izabranih iz grupe koju čine: (a)    hidroksi, (b)    halogen, (c)    -C02Ra (d)    -S(0)p-C, -C3 alkil; (e)    C3-C8 cikloalkil, (f)    C1-C6 alkoksi izborno supstituisan sa 1 do 5 halogena, i (g)    fenil izborno supstituisan sa 1 do 5 grupa nezavisno izabranih iz grupe koju čine halogen, nitro, -NRaRa, trifluorometil, trifluorometltoksi, C1-C5 alkil i -ORa, (3)    C3-C8 cikloalkil, i (4)    fenil izborno supstituisan sa 1 do 5 grupa izabranih iz grupe koju čine: (a)    halogen, (b)    nitro, (c)    -NRaRa, (d)    -OH, (e)    C1-C6 alkoksi izborno supstituisan sa 1 do 5 halogena, (f)    -S(0)p-C1-C6 alkil; i (g)    C1-C6 alkil izborno supstituisan sa do 5 grupa izabranih od hidroksi, halogen, trifluorometil, cijano, -C02R3, C3-C8 cikloalkil i -QRC; Rc je izabran iz grupe koju čine (1)    Z izborno supstituisan sa do 5 grupa izabranih od halogena, trifluorometil, cijano, C1-C5 alkil i C1-C5 alkoksi, i (2)    C1-C6 alkil; i Q je izabran iz grupe koju čine: (1) N(Ra)-, (2)    -O-, i (3)    -S(O)p-.
2. Jedinjenje prema patentnom zahtevu 1 koje ima formulu Ia, ili njegova farmaceutski prihvatljiva so, ili njegov stereoizomer, ili farmaceutski prihvatljiva so njegovog stereoizomera: u kome, Y, Z, R3 i n su kao što su definisani u patentnom zahtevu 1.
3. Jedinjenje prema patentnom zahtevu 1 ili 2, gde, Y je metilen, -CH(CH3)- ili veza.
4. Jedinjenje prema patentnom zahtevu 1, 2 ili 3, gde, Z je 5-člani heterocikličan prsten koji ima jedan atom azota i 0 do 3 dodatna heteroatoma nezavisno izabrana od N, O i S, ili 6-člani heterociklus koji ima 1, 2 ili 3 atoma azota, ili 1 atom azota i jedan atom kiseonika ili sumpora, ili Z je 5- ili 6-člani heterociklični prsten sa od 1 do 4 heteroatoma izabrana od kiseonika, sumpora i azota fuzionisan za C5-C6karbocikličan prsten, i gde, navedeni heterociklični prstenje 5-člani heterociklus koji ima jedan atom azota u prstenu i 0 do 3 dodatna heteroatoma nezavisno izabrana od N, O i S, ili 6-člani heterociklus koji ima 1, 2 ili 3 atoma zota u prstenu, ili 1 atom azota u prstenu i atom kiseonika ili sumpora u prstenu, ili Z je 5- ili 6-člani heterociklični prsten sa od 1 do 4 heteroatoma izabrana od kiseonika, sumpora i azota, fuzionisan za 5- ili 6-člani heterociklični prsten sa od 1 do 4 heteroatoma izabrana od kiseonika, sumpora i azota, pri čemu navedeni fuzionisani prsten ima 2 do 5 heteroatoma, od kojih je najmanje jedan azot.
5. Jedinjenje prema patentnom zahtevu 4, gde, Z je 5-člani heterociklični prsten koji ima jedan atom azota i 0 do 3 dodatna heteroatoma nezavisno izabrana od N, O i S.
6. Jedinjenje prema patentnom zahtevu 4, gde, Z je izabran iz grupe koju čine tiazolil, oksazolil, piridil, dihidropiridil, 1, 2, 4-triazolil, 1, 2, 3-triazolil, tetrazolil, pirimidinil, dihidropirimidinil, tetrahidropirimidinil, pirazinil, dihidropirazinil, piridazinil, dihidropiridazinil, pirolidinil, imidazolil, pirazolil, 1, 2, 4-oksadiazolil i 1, 2, 5-oksadiazolil.
7. Jedinjenje prema patentnom zahtevu 4, gde, Z je 5- ili 6-člani heterociklični prsten sa od 1 do 4 heteroatoma izabrana od kiseonika, sumpora i azota, fuzionisan za 5- ili 6-člani heterociklični prsten sa od 1 do 4 heteroatoma izabrana od kiseonika, sumpora i azota, i gde, fuzionisani prsten ima 2 do 4 atoma azota i nema više drugih heteroatoma.
8. Jedinjenje prema patentnom zahtevu 4, gde, Z je izabran iz grupe koju čine: gde, r je 1 ili 2.
9. Jedinjenje prema bilo kom prethodnom patentnom zahtevu gde je R3 izabran iz grupe koju čine: (1)    C1-C6 alkil izborno supstituisan sa halogenom ili -ORa, (2)    okso, (3)    halogen, (4)    -ORa, (5)    -C(0)NRaRa, i (6)    -NRaRa; gde je Ra kao što je definisan u patentnom zahetvu 6.
10. Jedinjenje prema patentnom zahtevu 1 ili Formuli Ia, ili njegova farmaceutski prihvatljiva so, ili njegov stereoizomer, ili farmaceutski prihvatljiva so njegovog stereoizomera: u kome n je 0, 1 ili 2; Y je izabran iz grupe koju čine metilen, -CH(CH3)- i veza; Z je izabran iz grupe koju čine tiazolil, piridil, dihidropiridil, 1, 2, 4-triazolil, pirimidinil, dihidropirimidinil, piridazinil, dihidropiridazinil, pirazolil, i R3 je izabran iz grupe koju čine: (1)    metil, (2)    okso, i (3) -NHz.
11. Jedinjenje prema patentnom zahtevu 10, gde je Z izabran iz grupe koju čine:
12. Jedinjenje prema patentnom zahtevu 18, gde, n je 1; Y je veza; Z je i R3 je okso.
13. Jedinjenje prema patentnom zahtevu 10, gde, Z je izabran iz grupe koju čine tiazolil, piridil, dihidropiridil, 1, 2, 4-triazolil, pirimidinil, dihidropirimidinil, piridazinil, dihidropiridazinil i pirazolil.
14. Jedinjenje prema patentnom zahtevu 13, gde, n je 1; Y je -CH(CH3)-; Z je 1, 2, 4-triazolil; i R3 je metil.
15. Jedinjenje prema patentnom zahtevu 1 izabrano iz grupe koju čine: ili njegova farmaceutski prihvatljiva so, ili njegov farmaceutski prihvatljiv stereoizomer, ili farmaceutski prihvatljiva so njegovog stereoizomera.
16. Jedinjenje prema patentnom zahtevu 15, gde je jedinjenje izabrano iz grupe koju čine: ili njegova farmaceutski prihvatljiva so, ili njegov farmaceutski prihvatljiv stereoizomer, ili farmaceutski prihvatljiva so njegovog stereoizomera.
17. Farmaceutska kompozicija koja sadrži jedinjenje prema bilo kom prethodnom patentnom zahtevu ili njegovu farmaceutski prihvatljivu so, ili njegov farmaceutski prihvatljiv stereoizomer, ili farmaceutski prihvatljivu so njegovog stereoizomera i farmaceutski prihvatljiv nosač.
18. Jedinjenje prema bilo kom od patentnih zahteva 1 do 16 ili njegova farmaceutski prihvatljiva so, ili njegov farmaceutski prihvatljiv stereoizmer, ili farmaceutski prihvatljiva so njegovog stereoizomera za upotrebu u postupku za lečenje ljudskog tela terapijom.
19. Jedinjenje za upotrebu prema patentnom zahtevu 18, gde je terapija - lečenje bolesti ili poremećaja izabranog od (1) preterano aktivne bešike, (2) uriname inkontinencije, (3) nagonske uriname inkotinencije i (4) uriname urgencije.
20. Upotreba jedinjenja prema bilo kom od patentnih zahteva 1 do 16 ili njegove farmaceutski prihvatljive soli, ili njegovog farmaceutski prihvatljivog stereoizomera, ili farmaceutski prihvatljive soli njegovog stereoizomera u proizvodnji leka za lečenje ili prevenciju bolesti ili poremećaja koji je izabran od (1) preterano aktivne bešike, (2) uriname inkontinencije, (3) nagonske uriname inkotinencije i (4) uriname urgencije.
21. Kombinacija jedinjenja prema bilo kom od patentnih zahteva 1 do 16 ili njegove farmaceutski prihvatljive soli, ili njegovog farmaceutski prihvatljivog stereoizomera ili farmaceutski prihvatljive soli njegovog stereoizomera i drugog aktivnog sredstva.
22. Kombinacija prema patentnom zahtevu 21, gde je drugo aktivno sredstvo antagonist muskarinskog receptora.
MEP-2012-549A 2008-04-04 2009-04-02 Hidroksimetil pirolidini kao agonisti beta 3 adrenergičkog receptora ME01988B (me)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US12306308P 2008-04-04 2008-04-04
US20604309P 2009-01-27 2009-01-27
EP09726601A EP2276756B9 (en) 2008-04-04 2009-04-02 Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists
PCT/US2009/039253 WO2009124167A1 (en) 2008-04-04 2009-04-02 Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists

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PE20091825A1 (es) * 2008-04-04 2009-12-04 Merck & Co Inc Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3
BR112012004333A2 (pt) * 2009-08-27 2015-09-08 Merck Sharp & Dohme composto, composição farmacêutica, e, método para o tratamento ou a prevenção de uma doença ou um distúrbio.
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