ME02845B - ASIMETRIČNE UREE l NJIHOVE MEDICINSKE UPOTREBE - Google Patents

ASIMETRIČNE UREE l NJIHOVE MEDICINSKE UPOTREBE

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Publication number
ME02845B
ME02845B MEP-2017-123A MEP2017123A ME02845B ME 02845 B ME02845 B ME 02845B ME P2017123 A MEP2017123 A ME P2017123A ME 02845 B ME02845 B ME 02845B
Authority
ME
Montenegro
Prior art keywords
ethyl
urea
methylpiperidin
methyl
dichlorophenyl
Prior art date
Application number
MEP-2017-123A
Other languages
English (en)
French (fr)
Inventor
Claudio Pietra
Claudio Giuliano
Rubio Silvina Garcia
Zhigang Li
Original Assignee
Helsinn Healthcare Sa
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 Helsinn Healthcare Sa filed Critical Helsinn Healthcare Sa
Publication of ME02845B publication Critical patent/ME02845B/me

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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
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    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/94—Oxygen atom, e.g. piperidine N-oxide
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    • C07D211/96—Sulfur atom
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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Addiction (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Nutrition Science (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)

Claims (22)

1. Jedinjenje formule (I) ili njegova farmaceutski prihvatljiva so ili adukt, u kome: R je aril izborno supstituisan sa jednim ili više nezavisnih R103 supstituenata; R1 je izabran iz grupe koja se sastoji od hidroksialkila, alkila, izborno supstitusanog sa jednim ili više nezavisnih R103 supstituenata; R4 je izabran iz grupe koja se sastoji od alkila, arila, arilalkila, izborno supstituisanog sa jednim ili više nezavisnih R103 supstituenata; ili R4 je OR103; R6, R7, R8, R9 su izabrani iz grupe koja se sastoji od vodonika i alkila; R103 je izabran iz grupe koja se sastoji od vodonika, cijano, -NO2, -OR104, hidroksi, amino, alkil, alkenil, cikloalkil, halogen, alkoksi, alkoksialkil, aril, arilalkil, heterocikloalkil, heterocikloalkilalkil, heteroaril, heteroarilalkil, -C(O)R104 -C(O)OR104 -C(O)NR104R105, -NR104R105, -NR104S(O)2R105,-NR104C(O)R105, -S(O)2R104 , -SR104 i -S(O)2NR104R105, svaki izborno nezavisno supstituisan sa jednim ili više nezavisnih R103 supstituenata; i R104 i R105 su svaki nezavisno izabrani iz grupe koja se sastoji od vodonika, cijano, NO2, hidroksi, hidroksialkil, amino, alkil, alkenil, cikloalkil, halogen, alkoksi, alkoksialkil, aril, arilalkil, heterocikloalkil, heterocikloalkilalkil, heteroaril i heteroarilalkil.
2. Jedinjenje prema patentnom zahtevu 1, naznačeno time što R je izabran iz grupe koja se sastoji od fenila, naftalena, tetrahidronaftalenila, indenila, izoindenila, indanila, antracenila, fenantrenila, benzonaftenil, fluorenila, pri čemu je navedeni R izborno supstituisan sa jednim ili više nezavisnih R103 supstituenata.
3. Jedinjenje prema patentnom zahtevu 1, naznačeno time što R je fenil ili naftalen koji je izborno nezavisno supstituisan sa od jednog do šest supstituenata nezavisno izabranih iz grupe koja se sastoji od hloro, fluoro, bromo, metoksi i etoksi.
4. Jedinjenje prema patentnom zahtevu 1, naznačeno time što R1 je izabran iz grupe koja se sastoji od metila, -CH2OH i -CH2-OCH2-fenila.
5. Jedinjenje prema patentnom zahtevu 1, naznačeno time što R4 je metil, etil, benzil ili benzil supstituisan sa od jednog do pet supstituenata nezavisno izabranih iz grupe koja se sastoji od metil, fluoro, hloro, trifluorometil, metoksi, cijano i hidroksi.
6. Jedinjenje prema patentnom zahtevu 1, naznačeno time što su svaki R8 i R9 nezavisno vodonik, metil ili etil.
7. Jedinjenje prema patentnom zahtevu 1: Jedinjenje br. Hemijska struktura Hemijski naziv GA1 1-metil-3-((R)-1-(naftalen-1- il)etil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA2 1-metil-3-((S)-1-(naftalen-1- il)etil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA3 1-metil-3-(1-(naftalen-1- il)etil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA4 3-(1-(4-metoksinaftalen-1- il)etil)-1-metil-1-(1,3,3- trimetilpiperidin-4-il)urea, GA5 1-benzil-3-((R)-1-(naftalen-1- il)etil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA6 3-(1-(2,3-dihlorofenil)etil)-1- (3-metoksibenzil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA7 3-(1-(2,3-dihlorofenil)etil)-1- (2-fluorobenzil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA8 3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-metil-1- (1,3,3-trimetilpiperidin-4-il)urea, GA9 3-(1-(2,3-dihlorofenil)etil)-1- metil-1-(1,3,3-trimetilpiperidin- 4-il)urea, GA10 3-((R)-1-(2,3-dihloro-4- metoksifenil)etil)-1-(1,3- dimetilpiperidin-4-il)-1-(3- metoksibenzil)urea, GA11 1-benzil-3-(1-(2,3- dihlorofenil)propil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA12 3-((S)-1-(2,3- dihlorofenil)etil)-1-metil-1- (1,3,3-trimetilpiperidin-4-il)urea, GA13 3-((R)-1-(2,3- dihlorofenil)etil)-1-metil-1- (1,3,3-trimetilpiperidin-4-il)urea, GA14 3-(1-(2,3-dihlorofenil)etil)-1- metil-1-(1,3,3-trimetilpiperidin- 4-il)urea, GA15 1-benzil-3-((S)-1-(naftalen-1- il)etil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA16 1-benzil-3-((R)-1-(naftalen-1- il)etil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA17 1-benzil-3-(1-(naphthalcn-1- il)etil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA18 3-(1-(2,3-dihlorofenil)propil)- 1-metil-1-(1,3,3- trimetilpiperidin-4-il)urea, GA19 3-(1-(2,3-difluorofenil)etil)-1- metil-1-(1,3,3-trimetilpiperidin- 4-il)urea, GA20 1-benzil-3-(1-(2,3- dihlorofenil)etil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA21 1-benzil-3-(1-(2,3- difluorofenil)etil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA22 1-benzil-3-(1-(4- metoksinaftalen-1-il)etil)-1- (1,3,3-trimetilpiperidin-4-il)urea, GA23 3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-metil-1- (l,3,3-trimetilpiperidin-4-il)urea, GA24 3-(1-(2,3-dihlorofenil)etil)-1- metil-1-(1,2,2,5,5- pentametilpiperidin-4-il)urea, GA26 3-(2-hidroksi-1-(naftalen-1- il)etil)-1-metil-1-(1,3,3- trimetilpiperidin-4-il)urea, GA27 1-(4-hlorobenzil)-3-(1-(2,3- dihlorofenil)etil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA28 1-benzil-1-(3,3-dietil-1- metilpiperidin-4-il)-3-((S)-1- (naftalen-1-il)etil)urea, GA29 1-benzil-1-(3,3-dietil-1- metilpiperidin-4-il)-3-((R)-1- (naftalen-1-il)etil)urea, GA30 1-benzil-1-(3,3-dietil-1- metilpiperidin-4-il)-3-(1- (naftalen-1-il)etil)urea, GA31 3-(2-(benziloksi)-1-(naftalen-1- il)etil)-1-metil-1-(1,3,3- trimetilpiperidin-4-il)urea, GA33 3-((R)-1-(2,3- dihlorofenil)etil)-1-(3- metoksibenzil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA34 3-(2-ciklopropil-1-(2,3- dihlorofenil)etil)-1-(3- metoksibenzil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA35 3-(1-(2,3-dihlorofenil)etil)-1- (3-hidroksibenzil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA37 1-benzil-3-(1-(2,3- dihidroksifenil)etil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA38 3-((R)-1-(2,3- dihlorofenil)etil)-1-(3-(2- hidroksietoksi)benzil)-1-(1,3,3- trimetilpiperidin-4-il)urea, GA39 3-(1-(2,3-difluoro-4- metoksifenil)etil)-1-metil-1- (1,3,3-trimetilpiperidin-4-il)urea, GA40 3-(1-(2,3-difluoro-4- hidroksifenil)etil)-1-metil-1- (1,3,3-trimetilpiperidin-4-il)urea, GA44 4-(3-(1-(2,3-dihlorofenil)etil)- 1-metilureido)-1,3,3- trimetilpiperidin 1-oksid, GA46 1-etil-1-(1-metilpiperidin-4-il)- 3-(1-(naftalen-1-il)etil)urea, GA47 3-(1-(4-metoksinaftalen-1- il)etil)-1-metil- metilpiperidin-4-il)urea, GA48 3-(2-hidroksi-1-(naftalen-1- il)etil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA49 3-(2-hidroksi-1-(4- metoksinaftalen-1-il)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA50 1-(1-metilpiperidin-4-il)-3-(1- (naftalen-1-il)etil)-1-(piridin- 3-ilmetil)urea, GA57 1-(cikloheksilmetil)-1-(1- metilpiperidin-4-il)-3-(1- (naftalen-1-il)etil)urea, GA58 1-izopropil-1-(1-metilpiperidin- 4-il)-3-(1-(naftalen-1- il)etil)urea, GA59 1-(2-metoksietil)-1-(1- metilpiperidin-4-il)-3-(1- (naftalen-1-il)etil)urea, GA62 1-(ciklopropilmetil)-1-(1- metilpiperidin-4-il)-3-(1- (naftalen-1-il)etil)urea, GA63 3-(1-(2-metoksinaftalen-1- il)etil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA67 3-(2-metoksi-1-(naftalen-1- il)etil)-1-metil- metilpiperidin-4-il)urea, GA68 3-(3-metoksi-1-(naftalen-1- il)propil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA69 1-metil-1-(1-metilpiperidin-4- il)-3-(1-(naftalen-1- il)propil)urea, GA73 (S)-1-(1-metilpiperidin-4-il)-3- (1-(naftalen-1-il)etil)-1- (piridin-3-ilmetil)urea, GA74 (R)-1-(1-metilpiperidin-4-il)-3- (1-(naftalen-1-il)etil)-1- (piridin-3-ilmetil)urea, GA75 1-izobutil-1-(1-metilpiperidin-4- il)-3-(1-(naftalen-1- il)etil)urea, GA76 1-(ciklobutilmetil)-1-(1- metilpiperidin-4-il)-3-(1- (naftalen-1-il)etil)urea, GA77 1-butil-1-(1-metilpiperidin-4-il)- 3-(1-(naftalen-1-il)etil)urea, GA79 1-(1-metilpiperidin-4-il)-3-(1- (naftalen-1-il)etil)-1-(piridin- 2-ilmetil)urea, GA80 1-(1-metilpiperidin-4-il)-3-(1- (naftalen-1-il)etil)-1-(piridin- 4-ilmetil)urea, GA82 (R)-1-etil-1-(1-metilpiperidin- 4-il)-3-(1-(naftalen-1- il)etil)urea, GA83 3-(2-hidroksi-1-(4- metoksinaftalen-1-il)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA84 3-(2-hidroksi-1-(naftalen-1- il)etil)-1-(1-metilpiperidin-4- il)-1-(piridin-3-ilmetil)urea, GA85 3-(2-metoksi-1-(4- metoksinaftalen-1-il)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA86 3-(1-(2,3-dihlorofenil)etil)-1- (3-hidroksibenzil)-1-(1- metilpiperidin-4-il)urea, GA87 1-benzil-1-(1,3-dimetilpiperidin- 4-il)-3-((R)-1-(naftalen-1- il)etil)urea, GA88 1-(1,3-dimetilpiperidin-4-il)-1- metil-3-((R)-1-(naftalen-1- il)etil)urea, GA89 3-(1-(4-metoksinaftalen-1- il)etil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA90 (R)-3-(1-(4-metoksinaftalen-1- il)etil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA91 (S)-3-(1-(4-metoksinaftalen-1- il)etil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA92 3-(1-(4,8-dimetoksinaftalen-1- il)etil)-1-metil- metilpiperidin-4-il)urea, GA93 3-(1-(4- (metoksimetoksi)naftalen-1- il)etil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA94 3-(2-(benziloksi)-1-(2,3- dihlorofenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA95 (R)-3-(2-(benziloksi)-1-(2,3- dihlorofenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA96 (S)-3-(2-(benziloksi)-1-(2,3- dihlorofenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA97 3-(1-(2,3-dihlorofenil)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA98 1-benzil-3-(1-(2,3- dihlorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA99 3-(1-(2,3-dihlorofenil)etil)-1- (3-fluorobenzil)-1-(1- metilpiperidin-4-il)urea, GA100 1-(2-hlorobenzil)-3-(1-(2,3- dihlorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA101 3-(1-(3,5-difluorofenil)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA102 3-(1-(2-hlorofenil)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA103 3-(1-(3-fluorofenil)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA104 3-(1-(4-hlorofenil)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA105 3-(1-(2,4-difluorofenil)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA106 1-metil-1-(1-metilpiperidin-4- il)-3-(1-(o-tolil)etil)urea, GA107 1-metil-1-(1-metilpiperidin-4- il)-3-(1-(4-(metilsulfonil)fenil)etil)urea, GA108 1-(cikloheksilmetil)-3-(1-(2,3- dihlorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA109 1-(ciklopropilmetil)-3-(1-(2,3- dihlorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA110 3-(1-(2,3-dihlorofenil)etil)-1- etil-1-(1-metilpiperidin-4- il)urea, GA111 3-(1-(2,3-dihlorofenil)etil)-1- (1-metilpiperidin-4-il)-1- (piridin-3-ilmetil)urea, GA112 3-(1-(3-hlorofenil)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA113 1-benzil-3-(1-(3- hlorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA114 1-(3-hlorobenzil)-3-(1-(2,3- dihlorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA115 3-(1-(2,3-dihlorofenil)etil)-1- (2-metoksibenzil)-1-(1- metilpiperidin-4-il)urea, GA116 3-(1-(2,3-dihlorofenil)etil)-1- (3-metoksibenzil)-1-(1- metilpiperidin-4-il)urea, GA117 3-(1-(2,3-dihlorofenil)etil)-1- (4-fluorobenzil)-1-(1- metilpiperidin-4-il)urea, GA118 3-(1-(2,3-dihlorofenil)etil)-1- (2-fluorobenzil)-1-(1- metilpiperidin-4-il)urea, GA119 1-(4-hlorobenzil)-3-(1-(2,3- dihlorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA120 3-(1-(3,4-dihlorofenil)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA121 3-(1-(2,3-dihlorofenil)etil)-1- (4-metoksibenzil)-1-(1- metilpiperidin-4-il)urea, GA122 3-(1-(2,3-dihlorofenil)propil)- 1-etil-1-(1-metilpiperidin-4- il)urea, GA123 1-(cikloheksilmetil)-3-(1-(2,3- dihlorofenil)propil)-1-(1- metilpiperidin-4-il)urea, GA124 3-(1-(2,3-difluorofenil)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA125 1-benzil-3-(1-(2,3- difluorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA126 1-(cikloheksilmetil)-3-(1-(2,3- difluorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA127 (R)-3-(1-(2,3- dihlorofenil)etil)-1-etil-1-(1- metilpiperidin-4-il)urea, GA128 1-benzil-3-(1-(2,3- dihlorofenil)etil)-1-(1,3- dimetilpiperidin-4-il)urea, GA129 3-(1-(2,3-dihlorofenil)etil)-1- (1,3-dimetilpiperidin-4-il)-1- metilurea, GA130 (S)-3-(1-(2,3- dihlorofenil)etil)-1-etil-1-(1- metilpiperidin-4-il)urea, GA131 (R)-3-(1-(2,3- dihlorofenil)etil)-1-etil-1-(1- metilpiperidin-4-il)urea, GA132 3-(1-(2,3-dihlorofenil)etil)-1- etil-1-(1-metilpiperidin-4- il)urea, GA133 3-((R)-1-(2,3-dihloro-4- metoksifenil)etil)-1-(1,3- dimetilpiperidin-4-il)-1-(3- metoksibenzil)urea, GA134 3-((S)-1-(2,3-dihloro-4- metoksifenil)etil)-1-(1,3- dimetilpiperidin-4-il)-1-(3- metoksibenzil)urea, GA135 3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-(1,3- dimetilpiperidin-4-il)-1-(3- metoksibenzil)urea, GA136 3-(1-(2,3-difluorofenil)etil)-1- (1,3-dimetilpiperidin-4-il)-1-(3- metoksibenzil)urea, GA137 3-(1-(2,3-dihlorofenil)etil)-1- (4-(hidroksimetil)benzil)-1-(1- metilpiperidin-4-il)urea, GA138 metil 4-((3-(1-(2,3- dihlorofenil)etil)-1-(1- metilpiperidin-4- il)ureido)metil)benzoat, GA139 3-(2-ciklopropil-1-(2,3- dihlorofenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA140 3-(1-(2,3-dihlorofenil)-2- hidroksietil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA141 (R)-1-(2-hlorobenzil)-3-(1-(2,3- dihlorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA142 (S)-1-(2-hlorobenzil)-3-(1-(2,3- dihlorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA143 1-(2-hlorobenzil)-3-(1-(2,3- dihlorofenil)etil)-1-(1- metilpiperidin-4-il)urea, GA144 3-(1-(2,3-dimetoksifenil)etil)- 1-metil-1-(1-metilpiperidin-4- il)urea, GA145 3-(1-(2,3-difluoro-4- metoksifenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA146 3-(1-(2,3-dihlorofenil)-2- metoksietil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA147 N-(2,3-dihloro-4-(1-(3-metil-3- (1-metilpiperidin-4- il)ureido)etil)fenil)acetamid, GA148 3-(1-(4-amino-2,3- dihlorofenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA149 3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA150 1-etil-1-(1-metilpiperidin-4-il)- 3-(1-(naftalen-1-il)-3-(3- (piridin-3- iloksi)fenil)propil)urea, GA151 1-metil-1-(1-metilpiperidin-4- il)-3-(1-(naftalen-1-il)-3- (piridin-3-il)propil)urea, GA152 1-metil-1-(1-metilpiperidin-4- il)-3-(3-morpholino-1-(naftalen- 1-il)propil)urea, GA153 1-etil-3-(3-(3-metoksifenil)-1- (naftalen-1-il)propil)-1-(1- metilpiperidin-4-il)urea, GA154 3-(3-(3-(benziloksi)fenil)-1- (naftalen-1-il)propil)-1-etil-1- (1-metilpiperidin-4-il)urea, GA155 1-etil-1-(1-metilpiperidin-4-il)- 3-(1-(naftalen-1-il)-3-(piridin- 3-il)propil)urea, GA156 3-(3-(3-(benziloksi)fenil)-1- (naftalen-1-il)propil)-1-(1- metilpiperidin-4-il)-1-(piridin-3- ilmetil)urea, GA157 3-(3-(3-(benziloksi)fenil)-1-(2,3- dihlorofenil)propil)-1-metil- 1-(1-metilpiperidin-4-il)urea, GA158 3-(2-(benziloksi)-1-(2,3- dihlorofenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA159 3-(2-(benzilamino)-1-(2,3- dihlorofenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA160 3-(1-(2,3-dihlorofenil)-2-((3- (hidroksimetil)benzil)oksi)etil)- 1-metil-1-(1-metilpiperidin-4- il)urea, GA161 3-(2-(benziloksi)-1-(2,3- dihlorofenil)etil)-1-(2- hlorobenzil)-1-(1- metilpiperidin-4-il)urea, GA162 3-(2-(benziloksi)-1-(2,3- dihlorofenil)etil)-1-(4- (hidroksimetil)benzil)-1-(1- metilpiperidin-4-il)urea, GA163 3-(1-(2,3-dihlorofenil)-2-((4- metoksibenzil)oksi)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA164 3-(1-(2,3-dihlorofenil)-2- (piridin-4-ilmetoksi)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA165 3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-metoksi- 1-(1-metilpiperidin-4-il)urea, GA166 (S)-3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-metoksi- 1-(1-metilpiperidin-4-il)urea, GA167 (R)-3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-metoksi- 1-(1-metilpiperidin-4-il)urea, GA168 1-hidroksi-3-(1-(4- metoksinaftalen-1-il)etil)-1- (1-metilpiperidin-4-il)urea, GA169 (R)-1-hidroksi-3-(1-(4- metoksinaftalen-1-il)etil)-1- (1-metilpiperidin-4-il)urea, GA170 (S)-1-hidroksi-3-(1-(4- metoksinaftalen-1-il)etil)-1- (1-metilpiperidin-4-il)urea, GA171 3-(1-(2,3-dihlorofenil)etil)-1- metoksi-1-(1-metilpiperidin-4- il)urea, GA172 (R)-3-(1-(2,3- dihlorofenil)etil)-1-metoksi- 1-(1-metilpiperidin-4-il)urea, GA173 (S)-3-(1-(2,3- dihlorofenil)etil)-1-metoksi- 1-(1-metilpiperidin-4-il)urea, GA174 1-metoksi-3-(1-(4- metoksinaftalen-1-il)etil)-1- (1-metilpiperidin-4-il)urea, GA175 (R)-1-metoksi-3-(1-(4- metoksinaftalen-1-il)etil)-1- (1-metilpiperidin-4-il)urea, GA176 (S)-1-metoksi-3-(1-(4- metoksinaftalen-1-il)etil)-1- (1-metilpiperidin-4-il)urea, GA177 3-(1-(2,3-dihlorofenil)etil)-1- hidroksi-1-(1-metilpiperidin-4- il)urea, GA178 (R)-3-(1-(2,3- dihlorofenil)etil)-1-hidroksi-1- (1-metilpiperidin-4-il)urea, GA179 (S)-3-(1-(2,3- dihlorofenil)etil)-1-hidroksi-1- (1-metilpiperidin-4-il)urea, GA180 3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-hidroksi- 1-(1-metilpiperidin-4-il)urea, G181 (R)-3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-hidroksi- 1-(1-metilpiperidin-4-il)urea, GA182 (S)-3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-hidroksi- 1-(1-metilpiperidin-4-il)urea, GA183 3-(1-(2,3-dihloro-4- (dimetilamino)fenil)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA184 3-(1-(4-((4- metoksibenzil)oksi)naftalen-1- il)etil)-1-metil-1-(1- metilpiperidin-4-il)urea, G185 3-(1-(4-hidroksinaftalen-1- il)etil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA186 3-(1-(4,5-dimetoksinaftalen-1- il)etil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA187 3-(1-(2,3-dihlorofenil)-2- (piridin-3-ilmetoksi)etil)-1- metil-1-(1-metilpiperidin-4- il)urea, GA189 3-(1-(2-hloro-3,4- dimetoksifenil)etil)-1-metil- 1-(1-metilpiperidin-4-il)urea, GA190 1-metil-1-(1-metilpiperidin-4- il)-3-(1-(2,3,4- trihlorofenil)etil)urea, GA191 1-metil-1-(1-metilpiperidin-4- il)-3-(1-(4-(piridin-4- ilmetoksi)naftalen-1- il)etil)urea, GA192 3-(1-(6-hloro-[1,1′-bifenil]-2- il)etil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA193 3-(1-(3-hloro-2-(piridin-4- il)fenil)etil)-1-metil-1-(1- metilpiperidin-4-il)urea, GA194 3-(1-(2,3-dihloro-4- metilfenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA195 3-(1-(3-hloro-2- metilfenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA196 3-(1-(2,3-dihlorofenil)-2-((4- (hidroksimetil)benzil)oksi)etil)- 1-metil-1-(1-metilpiperidin-4- il)urea, GA197 3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA198 (R)-3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA199 (S)-3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-metil-1- (1-metilpiperidin-4-il)urea, GA200 3-(1-(2,3-dihloro-4- metoksifenil)etil)-1-metil-1- (1,3,3-trimetilpiperidin-4-il)urea, GA201 3-((R)-1-(2,3-dihloro-4- metoksifenil)etil)-1-metil-1- (1,3,3-trimetilpiperidin-4-il)urea, GA202 3-((S)-1-(2,3-dihloro-4- metoksifenil)etil)-1-metil-1- (1,3,3-trimetilpiperidin-4-il)urea, i GA203 3-(1-(4-(2- (benziloksi)etoksi)naftalen-1- il)etil)-1-metil-1-(1- metilpiperidin-4-il)urea.
8. Jedinjenje formule (I) prema bilo kom od patentnih zahteva 1- 7, ili njegova farmaceutski prihvatljiva so ili adukt za upotrebu u postupku za prevenciju i/ili lečenje subjekta koji ima bolest koja je patofiziološki posredovana preko receptora za grelin, pri čemu je navedena bolest izabrana od gojaznosti, prekomerne težine, poremećaja ishrane, dijabetesa, metaboličkog sindroma, metaboličkog poremećaja, kaheksije koja je rezultat kancera, kongestivne srčane insuficijencije, smanjenja telesne težine kao posledice starenja ili SIDA-e, hronične insuficijencije jetre, hronične opstruktivne bolesti pluća, gastrointestinalne bolesti, poremećaja želudca ili zloupotrebe supstanci.
9. Jedinjenje za upotrebu prema patentnom zahtevu 8, naznačeno time što navedeni metabolički poremećaj je izabran iz grupe koja se sastoji od dijabetesa, dijabetesa tipa I, dijabetesa tipa II, neodgovarajuće tolerancije glukoze, insulinske rezistencije, hiperglikemije, hiperinsulinemije, hiperlipidemije, hipertrigliceridemije, hiperholesterolemije, dislipidemije, gojaznosti, starenja, sindroma X, ateroskleroze, bolesti srca, šloga, hipertenzije i periferne vaksularne bolesti.
10. Jedinjenje za upotrebu prema patentnom zahtevu 8, naznačeno time što navedeni poremećaj želudca je izabran grupe koja se sastoji od postoperativnog ileusa (POI), dijabetičke gastropareze i disfunkcije creva indukovane opioidom.
11. Jedinjenje za upotrebu prema patentnom zahtevu 8, naznačeno time što je navedena gastrointestinalna bolest izabrana iz grupe koja se sastoji od sindroma iritabilnog creva, gastritisa, bolesti refluksa kiseline, gastropareze i funkcionalne dispepsije.
12. Jedinjenje za upotrebu prema patentnom zahtevu 8, naznačeno time što, navedena zloupotreba supstanci je zloupotreba alkohola ili zloupotreba leka/droge.
13. Jedinjenje za upotrebu prema patentnom zahtevu 12, naznačeno time što je navedeni lek/droga izabran iz grupe koja se sastoji od amfetamina, barbiturata, benzodiazepina, kokaina, metakvalona i opioida.
14. Jedinjenje za upotrebu prema bilo kom od patentnih zahteva 8 do 13, naznačeno time što navedeno jedinjenje ili njegova farmaceutski prihvatljiva so ili adukt, je modulator receptora za grelin.
15. Jedinjenje za upotrebu prema bilo kom od patentnih zahteva 8 do 14, naznačeno time što navedeno jedinjenje ili njegova farmaceutski prihvatljiva so ili adukt, je primenjeno preko jednog ili više puteva izabranih iz grupe koja se sastoji od rektalne, bukalne, sublingvalne, intravenske, subkutane, intradermalne, transdermalne, intraperitonealne, oralne, preko kapi za oči, parenteralne i topikalne primene.
16. Jedinjenje za upotrebu prema bilo kom od patentnih zahteva 8 do 15, naznačeno time što navedena primena je postignuta primenom oralnog oblika navedenog jedinjenja ili njegove farmaceutski prihvatljive soli ili adukta.
17. Jedinjenje za upotrebu prema bilo kom od patentnih zahteva 8 do 16, naznačeno time što navedeno jedinjenje ili njegova farmaceutski prihvatljiva so ili adukt, je primenjeno u količini od 0.01 mikrograma po kg (μg/Kg) telesne težine na dan do 100 mg/Kg telesne težine na dan, od 0.1 μg /Kg/dan do 10 mg/Kg/dan, od 1 μg /Kg /dan do 5 mg/ Kg /dan, od 10 μg /Kg/dan do 5 mg/Kg/dan, od 100 μg /Kg/dan do 5 mg/Kg/dan, ili od 500 μg /Kg/dan do 5 mg/Kg/dan.
18. Jedinjenje za upotrebu prema bilo kom od patentnih zahteva 8 do 17, koje dalje sadrži primenu jednog ili više terapeutskih sredstava.
19. Jedinjenje za upotrebu prema bilo kom od patentnih zahteva 8 do 18, naznačeno time što subjekat je čovek.
20. Jedinjenje za upotrebu prema bilo kom od patentnih zahteva 8 do 19, naznačeno time što subjekat je identifikovan tako da mu je potreban tretman bolesti ili primena.
21. Farmaceutska kompozicija za upotrebu u prevenciji i/ili lečenju subjekta koji sadrži terapeutski efikasnu količinu jedinjenja prema bilo kom od patentnih zahteva 1-7, i jedan ili više farmaceutski prihvatljivih ekscipijenasa.
22. Farmaceutska kompozicija koja sadrži terapeutski efikasnu količinu jedinjenja prema bilo kom od patentnih zahteva 1- 7, i farmaceutski prihvatljiv nosač ili vehikulum.
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