ME01537B - Spojevi spiropiperidona kao antagonisti receptora orl-1 - Google Patents

Spojevi spiropiperidona kao antagonisti receptora orl-1

Info

Publication number
ME01537B
ME01537B MEP-2013-118A MEP11813A ME01537B ME 01537 B ME01537 B ME 01537B ME P11813 A MEP11813 A ME P11813A ME 01537 B ME01537 B ME 01537B
Authority
ME
Montenegro
Prior art keywords
pharmaceutically acceptable
acceptable salt
methyl
compound according
ylmethyl
Prior art date
Application number
MEP-2013-118A
Other languages
English (en)
Inventor
Collado Ana Belen Benito
Buezo Nuria Diaz
Alma Maria Jimenez-Aguado
Blanco Celia Lafuente
Maria Angeles Martinez-Grau
Concepcion Pedregal-Tercero
Escribano Miguel Angel Toledo
Original Assignee
Lilly Co Eli
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of ME01537B publication Critical patent/ME01537B/me

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/20Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Child & Adolescent Psychology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Description

"(12) PATENTNI SPIS<br /> 1 <br />me<br />B 01537 ME<br />(11)<br />ME 01537B (19) Crna Gora<br />(21) Broj prijave: P-2013-118<br />(22) Datum podnošenja prijave: 10. 11. 2010<br />(43) Datum objavljivanja prijave:<br />(45) Datum objavljivanja patenta:<br />2040420<br />20. 04. 2014<br /> Glasnik : 14/2014<br /> (51) Me dunarodna klasifikacija MKP<br />C07D495/20<br />2006.01<br />A61K31/444<br />2006.01<br />A61P25/00<br />2006.01<br />(30) Me dunarodno pravo prvenstva<br />EP<br />20090382246<br />16. 11. 2009<br />US<br />20100298629P<br />27. 01. 2010<br />(73) Nosilac Patenta<br />Eli Lilly and Company<br />Lilly Corporate Center<br />Indianapolis, IN 46285<br />US<br />(74) Zastupnik:<br />attorney<br />CUPI C, Branislav<br />Dalmatinska 10<br />Podgorica<br />81000<br />ME<br /> (72) Pronalaza c<br />BENITO COLLADO, Ana Belen<br />Lilly S.A., Avendia de la Industria 30<br />28108 Alcobendas Madrid<br />ES<br />DIAZ BUEZO, Nuria<br />Lilly S.A., Avendia de la Industria 30<br />Madrid<br />ES<br />JIMENEZ-AGUADO, Alma Maria<br />Lilly S.A., Avendia de la Industria 30<br />Madrid<br />ES<br />LAFUENTE BLANCO, Celia<br />Lilly S.A., Avendia de la Industria 30<br />Madrid<br />ES<br />MARTINEZ-GRAU, Maria Angeles<br />Lilly S.A., Avendia de la Industria 30<br />Madrid<br />ES<br />PEDREGAL-TERCERO, Concepcion<br />Lilly S.A., Avendia de la Industria 30<br />Madrid<br />ES<br />TOLEDO ESCRIBANO, Miguel Angel<br />Lilly S.A., Avendia de la Industria 30<br />Madrid<br />ES<br />(54) Naziv:<br />me<br />SPOJEVI SPIROPIPERIDONA KAO ANTAGONISTI RECEPTORA ORL-l<br />en<br />SPIROPIPERIDINE COMPOUNDS AS ORL-1 RECEPTOR ANTAGONISTS<br />(57) Apstrakt:"

Claims (15)

1.Spoj formule:,naznačen time štoR1 je fluor ili klor;svaki od R2a i R2b je vodik ili fluor;R3 je vodik, metil, hidroksimetil ili (C1-C3) alkoksimetil;R4 se bira iz skupine koju čine fluor, klor, cijano, cijanometil, (C1-C3) alkil, ciklopropil, hidroksimetil, metoksi, ciklopropilmetoksi, aminokarbonilmetoksi, (C1-C3) alkoksimetil, ciklopropiloksimetil, ciklopropilmetoksimetil, 1-hidroksi-1-metiletil, aminokarboniloksimetil, metilaminokarboniloksimetil, dimetilaminokarboniloksimetil, aminokarbonil, aminokarbonilmetil, -CH2-NR5R6, hidroksiimin, metoksiimin, morfolin-4-il, morfolin-4-ilmetil, Ar1, -CH2Ar1, tetrahidrofuran-2-il, 3-oksomorfolin-4-ilmetil, 2-oksopirolidin-1-ilmetil i 2-oksopiperidin-1-ilmetil;R5 je vodik, C1-C3 alkil, cijanometil, -C(O)CH3, ili aminokarbonilmetil;R6 je vodik ili metil; iAr1 je ostatak kojeg se bira iz skupine koju čine imidizol-1-il, imidizol-2-il, 2-metilimidizol-1-il, pirazol-1-il, 1,2,3-triazol-1-il; 1,2,3-triazol-2-il; 1,2,4-triazol-1-il, isoksazol-3-il, oksazol-5-il, i 3-metil-1,2,4-oksadiazol-5-il; ilinjegova farmaceutski prihvatljiva sol.
2.Spoj u skladu s patentnim zahtjevom 1, naznačen time što R1 je klor, ili njegova farmaceutski prihvatljiva sol.
3.Spoj u skladu s bilo kojim od patentnih zahtjeva 1 ili 2, naznačen time što svaki od R2a i R2b je fluor, ili njegova farmaceutski prihvatljiva sol.
4.Spoj u skladu s patentnim zahtjevom 1, naznačen time što R1 je fluor, a svaki od R2a i R2b je vodik, ili njegova farmaceutski prihvatljiva sol.
5.Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što R3 je metil, ili njegova farmaceutski prihvatljiva sol.
6.Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što R4 je fluor, hidroksimetil, metoksimetil ili pirazol-1-ilmetil, ili njegova farmaceutski prihvatljiva sol.
7.Spoj u skladu s patentnim zahtjevom 1, naznačen time što je [2-[4-[(2-klor-4,4-difluorspiro[5H-tieno[2,3-c]piran-7,4′-piperidin]-1′-il)metil]-3-metilpirazol-1-il]-3-piridil]metanol; 2-klor-4,4-difluor-1′-[[3-metil-1-[3-(pirazol-1-ilmetil)-2-piridil]pirazol-4-il]metil]spiro[5H-tieno[2,3-c]piran-7,4′-piperidin]; ili [4-[(2-klor-4,4-difluorspiro[5H-tieno[2,3-c]piran-7,4′-piperidin]-1′-il)metil]-1-(3-fluor-2-piridil)pirazol-3-il]metanol; ili njihove farmaceutski prihvatljive soli.
8.Spoj u skladu s patentnim zahtjevom 1, naznačen time što je [2-[4-[(2-klor-4,4-difluorspiro[5H-tieno[2,3-c]piran-7,4′-piperidin]-1′-il)metil]-3-metilpirazol-1-il]-3-piridil]metanol, ili njegova farmaceutski prihvatljiva sol.
9.Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 8, ili njegovu farmaceutski prihvatljivu sol, i farmaceutski prihvatljivu podlogu, razrjeđivač ili pomoćnu tvar.
10.Farmaceutski pripravak u skladu s patentnim zahtjevom 9, naznačen time što dodatno sadrži najmanje jedan dodatni terapijski sastojak.
11.Farmaceutski pripravak u skladu s patentnim zahtjevom 10, naznačen time što je dodatni terapijski sastojak SSRI antidepresiv.
12.Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen za uporabu u terapiji.
13.Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 12, u liječenju pretilosti ili prekomjerne tjelesne težine kod čovjeka.
14.Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 12, u liječenju migrene.
15.Spoj, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u skladu s patentnim zahtjevom 12, u liječenju depresije.
MEP-2013-118A 2009-11-16 2010-11-10 Spojevi spiropiperidona kao antagonisti receptora orl-1 ME01537B (me)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP09382246 2009-11-16
US29862910P 2010-01-27 2010-01-27
EP10782482.3A EP2501703B1 (en) 2009-11-16 2010-11-10 Spiropiperidine compounds as orl-1 receptor antagonists
PCT/US2010/056180 WO2011060035A1 (en) 2009-11-16 2010-11-10 Spiropiperidine compounds as orl-1 receptor antagonists

Publications (1)

Publication Number Publication Date
ME01537B true ME01537B (me) 2014-04-20

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Country Status (34)

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US (1) US8232289B2 (me)
EP (1) EP2501703B1 (me)
JP (1) JP5680101B2 (me)
KR (1) KR101363830B1 (me)
CN (1) CN102612520B (me)
AR (1) AR078863A1 (me)
AU (1) AU2010319581C1 (me)
CA (1) CA2796161C (me)
CO (1) CO6541545A2 (me)
CR (1) CR20130087A (me)
DK (1) DK2501703T3 (me)
DO (1) DOP2012000135A (me)
EA (1) EA020848B1 (me)
EC (1) ECSP12011902A (me)
ES (1) ES2435814T3 (me)
HN (1) HN2012001011A (me)
HR (1) HRP20130967T1 (me)
IL (1) IL219370A (me)
JO (1) JO2887B1 (me)
MA (1) MA33751B1 (me)
ME (1) ME01537B (me)
MX (1) MX2012005691A (me)
MY (1) MY160665A (me)
NZ (1) NZ600006A (me)
PE (1) PE20121430A1 (me)
PH (1) PH12012500969A1 (me)
PL (1) PL2501703T3 (me)
PT (1) PT2501703E (me)
RS (1) RS53018B (me)
SI (1) SI2501703T1 (me)
TW (1) TWI465453B (me)
UA (1) UA107943C2 (me)
WO (1) WO2011060035A1 (me)
ZA (1) ZA201202967B (me)

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JP2013510859A (ja) 2013-03-28
EA020848B1 (ru) 2015-02-27
EP2501703B1 (en) 2013-09-18
IL219370A (en) 2015-01-29
MX2012005691A (es) 2012-06-13
MY160665A (en) 2017-03-15
CA2796161A1 (en) 2011-05-19
PL2501703T3 (pl) 2014-02-28
AR078863A1 (es) 2011-12-07
DK2501703T3 (da) 2013-10-14
HK1169988A1 (en) 2013-02-15
WO2011060035A1 (en) 2011-05-19
SI2501703T1 (sl) 2013-11-29
DOP2012000135A (es) 2012-08-15
CN102612520A (zh) 2012-07-25
JP5680101B2 (ja) 2015-03-04
CN102612520B (zh) 2015-04-08
EA201290352A1 (ru) 2012-10-30
UA107943C2 (xx) 2015-03-10
AU2010319581C1 (en) 2014-05-15
JO2887B1 (en) 2015-03-15
CO6541545A2 (es) 2012-10-16
AU2010319581A1 (en) 2012-06-07
NZ600006A (en) 2014-05-30
EP2501703A1 (en) 2012-09-26
RS53018B (sr) 2014-04-30
ECSP12011902A (es) 2012-07-31
HRP20130967T1 (hr) 2013-11-22
HN2012001011A (es) 2015-08-31
PH12012500969A1 (en) 2013-01-07
PT2501703E (pt) 2013-11-26
KR20130026523A (ko) 2013-03-13
TWI465453B (zh) 2014-12-21
ZA201202967B (en) 2013-09-25
PE20121430A1 (es) 2012-10-26
ES2435814T3 (es) 2013-12-23
MA33751B1 (fr) 2012-11-01
KR101363830B1 (ko) 2014-02-14
US20110118251A1 (en) 2011-05-19
TW201127841A (en) 2011-08-16
US8232289B2 (en) 2012-07-31
CR20130087A (es) 2013-04-17
AU2010319581B2 (en) 2013-12-19
IL219370A0 (en) 2012-06-28
CA2796161C (en) 2015-03-17

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