HRP20110852T1 - PIPERIDINSKI AGONISTI GPCR-a - Google Patents
PIPERIDINSKI AGONISTI GPCR-a Download PDFInfo
- Publication number
- HRP20110852T1 HRP20110852T1 HR20110852T HRP20110852T HRP20110852T1 HR P20110852 T1 HRP20110852 T1 HR P20110852T1 HR 20110852 T HR20110852 T HR 20110852T HR P20110852 T HRP20110852 T HR P20110852T HR P20110852 T1 HRP20110852 T1 HR P20110852T1
- Authority
- HR
- Croatia
- Prior art keywords
- piperidine
- propyl
- oxadiazol
- pharmaceutically acceptable
- acceptable salt
- Prior art date
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- 229940125633 GPCR agonist Drugs 0.000 title abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 title 2
- 150000001875 compounds Chemical class 0.000 claims abstract 26
- 150000003839 salts Chemical class 0.000 claims abstract 22
- 208000008589 Obesity Diseases 0.000 claims abstract 2
- 206010012601 diabetes mellitus Diseases 0.000 claims abstract 2
- 235000020824 obesity Nutrition 0.000 claims abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- QMSQESRBSZEVLM-OAHLLOKOSA-N 3-[4-[(2r)-4-(3-fluoro-4-methylsulfonylphenoxy)butan-2-yl]piperidin-1-yl]-5-propan-2-yl-1,2,4-oxadiazole Chemical compound O1C(C(C)C)=NC(N2CCC(CC2)[C@H](C)CCOC=2C=C(F)C(=CC=2)S(C)(=O)=O)=N1 QMSQESRBSZEVLM-OAHLLOKOSA-N 0.000 claims 1
- ICMKSFZJDNVMGL-MRXNPFEDSA-N 3-[4-[(2r)-4-(4-methylsulfonylphenoxy)butan-2-yl]piperidin-1-yl]-5-propan-2-yl-1,2,4-oxadiazole Chemical compound O1C(C(C)C)=NC(N2CCC(CC2)[C@H](C)CCOC=2C=CC(=CC=2)S(C)(=O)=O)=N1 ICMKSFZJDNVMGL-MRXNPFEDSA-N 0.000 claims 1
- WMHFRNVJYXYHMU-UHFFFAOYSA-N 3-[4-[3-(3-chloro-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-5-propan-2-yl-1,2,4-oxadiazole Chemical compound O1C(C(C)C)=NC(N2CCC(CCCOC=3C=C(Cl)C(=CC=3)S(C)(=O)=O)CC2)=N1 WMHFRNVJYXYHMU-UHFFFAOYSA-N 0.000 claims 1
- BZGNKWPKMZGCDV-UHFFFAOYSA-N 3-[4-[3-(3-fluoro-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-5-propan-2-yl-1,2,4-oxadiazole Chemical compound O1C(C(C)C)=NC(N2CCC(CCCOC=3C=C(F)C(=CC=3)S(C)(=O)=O)CC2)=N1 BZGNKWPKMZGCDV-UHFFFAOYSA-N 0.000 claims 1
- COLSBVLYLGYHNK-UHFFFAOYSA-N 3-[4-[3-(3-fluoro-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-5-propyl-1,2,4-oxadiazole Chemical compound O1C(CCC)=NC(N2CCC(CCCOC=3C=C(F)C(=CC=3)S(C)(=O)=O)CC2)=N1 COLSBVLYLGYHNK-UHFFFAOYSA-N 0.000 claims 1
- VFZLLTFPVWCIQY-UHFFFAOYSA-N 3-[4-[3-(3-methyl-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-5-propan-2-yl-1,2,4-oxadiazole Chemical compound O1C(C(C)C)=NC(N2CCC(CCCOC=3C=C(C)C(=CC=3)S(C)(=O)=O)CC2)=N1 VFZLLTFPVWCIQY-UHFFFAOYSA-N 0.000 claims 1
- KJJOJTSYGQMCTR-UHFFFAOYSA-N 3-[4-[3-(3-methyl-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-5-propyl-1,2,4-oxadiazole Chemical compound O1C(CCC)=NC(N2CCC(CCCOC=3C=C(C)C(=CC=3)S(C)(=O)=O)CC2)=N1 KJJOJTSYGQMCTR-UHFFFAOYSA-N 0.000 claims 1
- VRXGLILJFLLDGP-UHFFFAOYSA-N 3-[4-[3-(4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-5-propan-2-yl-1,2,4-oxadiazole Chemical compound O1C(C(C)C)=NC(N2CCC(CCCOC=3C=CC(=CC=3)S(C)(=O)=O)CC2)=N1 VRXGLILJFLLDGP-UHFFFAOYSA-N 0.000 claims 1
- QRTLCDQUPUHALP-UHFFFAOYSA-N 3-[4-[3-(4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-5-propyl-1,2,4-oxadiazole Chemical compound O1C(CCC)=NC(N2CCC(CCCOC=3C=CC(=CC=3)S(C)(=O)=O)CC2)=N1 QRTLCDQUPUHALP-UHFFFAOYSA-N 0.000 claims 1
- GOJZISSHNRVZTQ-UHFFFAOYSA-N 3-ethyl-5-[4-[3-(3-fluoro-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-1,2,4-oxadiazole Chemical compound CCC1=NOC(N2CCC(CCCOC=3C=C(F)C(=CC=3)S(C)(=O)=O)CC2)=N1 GOJZISSHNRVZTQ-UHFFFAOYSA-N 0.000 claims 1
- FAGWQFDQJJTQLD-UHFFFAOYSA-N 3-ethyl-5-[4-[3-(4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-1,2,4-oxadiazole Chemical compound CCC1=NOC(N2CCC(CCCOC=3C=CC(=CC=3)S(C)(=O)=O)CC2)=N1 FAGWQFDQJJTQLD-UHFFFAOYSA-N 0.000 claims 1
- OKCPZOKPEJXTKM-OAHLLOKOSA-N 3-tert-butyl-5-[4-[(2r)-4-(3-fluoro-4-methylsulfonylphenoxy)butan-2-yl]piperidin-1-yl]-1,2,4-oxadiazole Chemical compound C([C@@H](C)C1CCN(CC1)C=1ON=C(N=1)C(C)(C)C)COC1=CC=C(S(C)(=O)=O)C(F)=C1 OKCPZOKPEJXTKM-OAHLLOKOSA-N 0.000 claims 1
- DEFUWUWXBZYCTH-MRXNPFEDSA-N 3-tert-butyl-5-[4-[(2r)-4-(4-methylsulfonylphenoxy)butan-2-yl]piperidin-1-yl]-1,2,4-oxadiazole Chemical compound C([C@@H](C)C1CCN(CC1)C=1ON=C(N=1)C(C)(C)C)COC1=CC=C(S(C)(=O)=O)C=C1 DEFUWUWXBZYCTH-MRXNPFEDSA-N 0.000 claims 1
- HCLMFPSZNCSUHX-UHFFFAOYSA-N 3-tert-butyl-5-[4-[3-(3-chloro-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-1,2,4-oxadiazole Chemical compound CC(C)(C)C1=NOC(N2CCC(CCCOC=3C=C(Cl)C(=CC=3)S(C)(=O)=O)CC2)=N1 HCLMFPSZNCSUHX-UHFFFAOYSA-N 0.000 claims 1
- YUUSWHOAPSHNQT-UHFFFAOYSA-N 3-tert-butyl-5-[4-[3-(3-methyl-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-1,2,4-oxadiazole Chemical compound C1=C(S(C)(=O)=O)C(C)=CC(OCCCC2CCN(CC2)C=2ON=C(N=2)C(C)(C)C)=C1 YUUSWHOAPSHNQT-UHFFFAOYSA-N 0.000 claims 1
- HOCKOIVSHFOEFS-UHFFFAOYSA-N 3-tert-butyl-5-[4-[3-(4-ethylsulfonyl-3-fluorophenoxy)propyl]piperidin-1-yl]-1,2,4-oxadiazole Chemical compound C1=C(F)C(S(=O)(=O)CC)=CC=C1OCCCC1CCN(C=2ON=C(N=2)C(C)(C)C)CC1 HOCKOIVSHFOEFS-UHFFFAOYSA-N 0.000 claims 1
- ZXOXTFAYLUXYKJ-UHFFFAOYSA-N 3-tert-butyl-5-[4-[3-(4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-1,2,4-oxadiazole Chemical compound CC(C)(C)C1=NOC(N2CCC(CCCOC=3C=CC(=CC=3)S(C)(=O)=O)CC2)=N1 ZXOXTFAYLUXYKJ-UHFFFAOYSA-N 0.000 claims 1
- AJJISMLYIMQAKP-OAHLLOKOSA-N 5-[4-[(2r)-4-(3-fluoro-4-methylsulfonylphenoxy)butan-2-yl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole Chemical compound CC(C)C1=NOC(N2CCC(CC2)[C@H](C)CCOC=2C=C(F)C(=CC=2)S(C)(=O)=O)=N1 AJJISMLYIMQAKP-OAHLLOKOSA-N 0.000 claims 1
- UFZGQTYELYCXFZ-MRXNPFEDSA-N 5-[4-[(2r)-4-(3-methyl-4-methylsulfonylphenoxy)butan-2-yl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole Chemical compound CC(C)C1=NOC(N2CCC(CC2)[C@H](C)CCOC=2C=C(C)C(=CC=2)S(C)(=O)=O)=N1 UFZGQTYELYCXFZ-MRXNPFEDSA-N 0.000 claims 1
- WLMVBEXOSRILNA-MRXNPFEDSA-N 5-[4-[(2r)-4-(4-methylsulfonylphenoxy)butan-2-yl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole Chemical compound CC(C)C1=NOC(N2CCC(CC2)[C@H](C)CCOC=2C=CC(=CC=2)S(C)(=O)=O)=N1 WLMVBEXOSRILNA-MRXNPFEDSA-N 0.000 claims 1
- JCUIBGNUQRNNDK-MRXNPFEDSA-N 5-[4-[(2r)-4-(4-methylsulfonylphenoxy)butan-2-yl]piperidin-1-yl]-3-propyl-1,2,4-oxadiazole Chemical compound CCCC1=NOC(N2CCC(CC2)[C@H](C)CCOC=2C=CC(=CC=2)S(C)(=O)=O)=N1 JCUIBGNUQRNNDK-MRXNPFEDSA-N 0.000 claims 1
- VLACEOSUCJAWDG-UHFFFAOYSA-N 5-[4-[3-(3-chloro-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole Chemical compound CC(C)C1=NOC(N2CCC(CCCOC=3C=C(Cl)C(=CC=3)S(C)(=O)=O)CC2)=N1 VLACEOSUCJAWDG-UHFFFAOYSA-N 0.000 claims 1
- NGTLMTJXHHVFKK-UHFFFAOYSA-N 5-[4-[3-(3-fluoro-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-3-methyl-1,2,4-oxadiazole Chemical compound CC1=NOC(N2CCC(CCCOC=3C=C(F)C(=CC=3)S(C)(=O)=O)CC2)=N1 NGTLMTJXHHVFKK-UHFFFAOYSA-N 0.000 claims 1
- DPSQJTZWTDOKFO-UHFFFAOYSA-N 5-[4-[3-(3-fluoro-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole Chemical compound CC(C)C1=NOC(N2CCC(CCCOC=3C=C(F)C(=CC=3)S(C)(=O)=O)CC2)=N1 DPSQJTZWTDOKFO-UHFFFAOYSA-N 0.000 claims 1
- IATPCIBOIGPQOH-UHFFFAOYSA-N 5-[4-[3-(3-fluoro-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-3-propyl-1,2,4-oxadiazole Chemical compound CCCC1=NOC(N2CCC(CCCOC=3C=C(F)C(=CC=3)S(C)(=O)=O)CC2)=N1 IATPCIBOIGPQOH-UHFFFAOYSA-N 0.000 claims 1
- GAONLKXQODVTMM-UHFFFAOYSA-N 5-[4-[3-(3-methyl-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole Chemical compound CC(C)C1=NOC(N2CCC(CCCOC=3C=C(C)C(=CC=3)S(C)(=O)=O)CC2)=N1 GAONLKXQODVTMM-UHFFFAOYSA-N 0.000 claims 1
- XXYKDYFLCGNWMI-UHFFFAOYSA-N 5-[4-[3-(3-methyl-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-3-propyl-1,2,4-oxadiazole Chemical compound CCCC1=NOC(N2CCC(CCCOC=3C=C(C)C(=CC=3)S(C)(=O)=O)CC2)=N1 XXYKDYFLCGNWMI-UHFFFAOYSA-N 0.000 claims 1
- YMTJKYZUSASUQK-UHFFFAOYSA-N 5-[4-[3-(4-ethylsulfonyl-3-fluorophenoxy)propyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole Chemical compound C1=C(F)C(S(=O)(=O)CC)=CC=C1OCCCC1CCN(C=2ON=C(N=2)C(C)C)CC1 YMTJKYZUSASUQK-UHFFFAOYSA-N 0.000 claims 1
- SPJLGAQJXPHCIZ-UHFFFAOYSA-N 5-[4-[3-(4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole Chemical compound CC(C)C1=NOC(N2CCC(CCCOC=3C=CC(=CC=3)S(C)(=O)=O)CC2)=N1 SPJLGAQJXPHCIZ-UHFFFAOYSA-N 0.000 claims 1
- FNFRIJXKHNODKE-UHFFFAOYSA-N 5-[4-[3-(4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-3-propyl-1,2,4-oxadiazole Chemical compound CCCC1=NOC(N2CCC(CCCOC=3C=CC(=CC=3)S(C)(=O)=O)CC2)=N1 FNFRIJXKHNODKE-UHFFFAOYSA-N 0.000 claims 1
- NHLBTHMXWSUWFN-UHFFFAOYSA-N 5-ethyl-3-[4-[3-(3-fluoro-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-1,2,4-oxadiazole Chemical compound O1C(CC)=NC(N2CCC(CCCOC=3C=C(F)C(=CC=3)S(C)(=O)=O)CC2)=N1 NHLBTHMXWSUWFN-UHFFFAOYSA-N 0.000 claims 1
- CZPITONRODPQDR-UHFFFAOYSA-N 5-tert-butyl-3-[4-[3-(3-fluoro-4-methylsulfonylphenoxy)propyl]piperidin-1-yl]-1,2,4-oxadiazole Chemical compound O1C(C(C)(C)C)=NC(N2CCC(CCCOC=3C=C(F)C(=CC=3)S(C)(=O)=O)CC2)=N1 CZPITONRODPQDR-UHFFFAOYSA-N 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000002184 metal Substances 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000036186 satiety Effects 0.000 claims 1
- 235000019627 satiety Nutrition 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Peptides Or Proteins (AREA)
Abstract
Spoj formule (I), ili njegova farmaceutski prihvatljiva sol: naznačen time, da jedan između X i Y predstavlja O, a drugi predstavlja N; R1 je SO2R5;R2 je vodik, halo ili metil; R3 je vodik ili metil; R4 je C2-5 alkil; a R5 je C1-3 alkil. Patent sadrži još 21 patentni zahtjev.
Claims (22)
1. Spoj formule (I), ili njegova farmaceutski prihvatljiva sol:
[image]
naznačen time, da jedan između X i Y predstavlja O, a drugi predstavlja N;
R1 je SO2R5;
R2 je vodik, halo ili metil;
R3 je vodik ili metil;
R4 je C2-5 alkil; a
R5 je C1-3 alkil.
2. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol, naznačen time, da X je O.
3. Spoj u skladu s patentnim zahtjevom 1, ili njegova farmaceutski prihvatljiva sol naznačen time, da Y je O.
4. Spoj u skladu s bilo kojim patentnim zahtjevom 1 do 3, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R1 je so2ch3.
5. Spoj u skladu s bilo kojim patentnim zahtjevom 1 do 4, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R2 je vodik, fluoro, kloro ili metil.
6. Spoj u skladu s patentnim zahtjevom 5, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R2 je vodik ili fluoro.
7. Spoj u skladu s bilo kojim patentnim zahtjevom 1 do 6, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R3 je vodik.
8. Spoj u skladu s bilo kojim patentnim zahtjevom 1 do 6, ili njegova farmaceutski prihvatljiva sol, naznačen time, da r3 je metil.
9. Spoj u skladu s patentnim zahtjevom 8, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R3 je metal, a dobiveni stereocentar ima (R)-konfiguraciju.
10. Spoj u skladu s bilo kojim patentnim zahtjevom 1 do 9, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R4 je c3-4 alkil.
11. Spoj u skladu s patentnim zahtjevom 10, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R4je n-propil, izopropil ili tert-butil.
12. Spoj u skladu s patentnim zahtjevom 11, ili njegova farmaceutski prihvatljiva sol, naznačen time, da R4 je izopropil.
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da navedeni spoj je 4-[3-(3-Fluoro-4-metan-sulfonilfenoksi)propil]1-(3-izopropil-[1,2,4]oksadiazol-5-il)piperidin ili njegova farmaceutski prihvatljiva sol.
14. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da navedeni spoj je
1-(3-Izopropil- [1,2,4]oksadiazol-5-il)-4-[(R)-3-(4-metansulfonil-fenoksi)-1-metilpropil]-piperidin.
15. Spoj u skladu s patentnim zahtjevom 1 formule (I), naznačen time, da je odabran između sljedećih spojeva:
1-(3-Izopropil-[1,2,4]oksadiazol-5-il)-4-[3-(4metansulfonilfenoksi)-propil]piperidin;
1-(3-Izopropil-[1,2,4]oksadiazol-5-il)-4-[(R)-3-(4-metansulfonil-3metilfenoksi)-1-metilpropil]piperidin;
4-[3-(4-Etansulfonil-3-fluorofenoksi)propil]-1-(3-izopropil-[1,2,4]oksadiazol-5-il)piperidin;
1-(5-Izopropil-[1,2,4]oksadiazol-3-il)-4-[3-(4-metansulfonil-3-metil-fenoksi)propil]piperidin;
4-[(R)-3-(3-Fluoro-4-metansulfonilfenoksi)-1-metilpropil]-1-(5-izopropil-[1,2,4]oksadiazol-3il)-piperidin;
1-(5-Izopropil-[1,2,4]oksadiazol-3-il)-4-[(R)-3-(4-metansulfonil-fenoksi)-1-metilpropil]-piperidin;
4-[3-(3-Kloro-4-metansulfonilfenoksi)-propil]-1-(3-izopropil-[1,2,4]oksadiazol-5-il)-piperidin;
4-[3-(4Metansulfonil-fenoksi)propil]-1-(5-propil-[1,2,4]oksadiazol-3-il)-piperidin;
4-[3-(3-Fluoro-4-metansulfonilfenoksi)-propil]-1-(5-propil-[1,2,4]oksadiazol-3-il)-piperidin;
4-[3-(4-Metansulfonil-3-metilfenoksi)propil]1-(5-propil-[1,2,4]oksadiazol-3-il)-piperidin;
4-[3-(4-Metansulfonil-fenoksi)propil]-1-(3-propil-[1,2,4]oksadiazol-5-il)-piperidin;
4-[3-(4-Metansulfonil-3-metilfenoksi)propil]-1-(3-propil-[1,2,4]oksadiazol-5-il)-piperidin;
1-(5-Izopropil-[1,2,4]oksadiazol-3-il)-4-[3-(4-metansulfonilfenoksi)-propil]piperidin;
1-(3-Izopropil-[1,2,4]oksadiazol-5-il)-4-[3-(4-metansulfonil-3-metil-fenoksi)propil]piperidin;
4-[3-(3-Kloro-4-metansulfonilfenoksi)-propil]-1-(5-izopropil-[1,2,4]oksadiazol-3-il)-piperidin;
4-[3-(3-Fluoro-4-metansulfonilfenoksi)propil]-1-(3-propil-[1,2,4]oksadiazol-5-il)piperidin;
1-(3-Etil-[1,2,4]oksadiazol-5-il)-4-[3-(3-fluoro-4-metansulfonilfenoksi)-propil]piperidin;
4-[3-(3-Fluoro-4-metansulfonilfenoksi)-propil]-1-(3-metil-[1,2,4]oksadiazol-5il)-piperidin;
4-[(R)-3-(3-Fluoro-4-metansulfonilfenoksi)-1-metilpropil]-1-(3-izopropil-[1,2,4]oksadiazol-5il)-piperidin;
4-[(R)-3-(4-Metansulfonil-fenoksi)-1-metilpropil]-1-(3-propil-[1,2,4]oksadiazol-5-il)piperidin;
1-(3-Etil-[1,2,4]oksadiazol-5-il)-4-[3-(4-metansulfonil-fenoksi)propil]piperidin;
1-(3-tert-Butil-[1,2,4]oksadiazol-5-N)-4-[3-(3-fluoro-4-metansulfoml-fenoksi)propil]piperidin;
1-(3-tert-Butil-[1,2,4]oksadiazol-5-il)-4-[(R)3-(4-metansulfonil-fenoksi)-1-metilpropil]-piperidin;
1-(3-tert-Butil-[1,2,4]oksadiazol-5-il)-4-[(R)-3-(3-fluoro4-metansulfonil-fenoksi)-1-metilpropil]-piperidin;
1-(3-tert-Butil-[1,2,4]oksadiazol-5-il)-4-[3-(3-kloro-4-metansulfonil-fenoksi)propil]piperidin;
1-(3-tert-Butil-[1,2,4]oksadiazol-5-il)-4-[3-(4-metansulfonil-3-metilfenoksi)propil]piperidin;
1-(3-tert-Butil-[1,2,4]oksadiazol-5-il)-4-[3-(4-metansulfonilfenoksi)-propil]piperidin;
1-(3-tert-Butil-[1,2,4]oksadiazol-5-il)-4-[3-(4-etansulfonil-3-fluoro-fenoksi)propil]piperidin;
1-(5-tert-Butil-[1,2,4]oksadiazol-3-il)-4-[3-(3-fluoro-4-metansulfonil-fenoksi)propil]piperidin;
4-[3-(3-Fluoro-4-metansulfonilfenoksi)-propil]-1-(5-izopropil-[1,2,4]oksadiazol-3-il)-piperidin;
1-(5-Etil-[1,2,4]oksadiazol-3-il)-4-[3-(3fluoro-4-metansulfonilfenoksi)-propil]piperidin;
ili njegova farmaceutski prihvatljiva sol.
16. Farmaceutski pripravak, naznačen time, da sadrži spoj u skladu s bilo kojim patentnim zahtjevom 1 do 15, ili njegova farmaceutski prihvatljiva sol i farmaceutski prihvatljiv nosač.
17. Spoj u skladu s bilo kojim patentnim zahtjevom 1 do 15, ili njegova farmaceutski prihvatljiva sol, naznačen time, da se koristi za regulaciju sitosti.
18. Spoj u skladu s bilo kojim patentnim zahtjevom 1 do 15, ili njegova farmaceutski prihvatljiva sol, naznačen time, da se koristi za liječenje pretilosti.
19. Spoj u skladu s bilo kojim patentnim zahtjevom 1 do 15, ili njegova farmaceutski prihvatljiva sol, naznačen time, da se koristi za liječenje dijabetesa.
20. Spoj u skladu s bilo kojim patentnim zahtjevom 1 do 15, ili njegova farmaceutski prihvatljiva sol, naznačen time, da se koristi za liječenje metaboličkog sindroma (sindrom X), poremećene tolerancije glukoze, hiperlipidemije, hipertrigliceridemije, hiperkolesterolemije, niske razine HDL ili hipertenzije.
21. Spoj u skladu s bilo kojim patentnim zahtjevom 1 do 15, ili njegova farmaceutski prihvatljiva sol, naznačen time, da se koristi kao lijek.
22. Spoj u skladu s bilo kojim patentnim zahtjevom 1 do 15, ili njegova farmaceutski prihvatljiva sol, naznačen time, da se koristi za proizvodnju lijeka za liječenje ili sprječavanje bolesti ili stanja kako su definirani u bilo kojem od patentnih zahtjeva 17 to 20.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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GB0700123A GB0700123D0 (en) | 2007-01-04 | 2007-01-04 | GPCR agonists |
GB0719760A GB0719760D0 (en) | 2007-10-10 | 2007-10-10 | GPCR agonists |
PCT/GB2008/050010 WO2008081204A1 (en) | 2007-01-04 | 2008-01-04 | Piperidine gpcr agonists |
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HRP20110852T1 true HRP20110852T1 (hr) | 2011-12-31 |
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HR20110852T HRP20110852T1 (hr) | 2007-01-04 | 2011-11-15 | PIPERIDINSKI AGONISTI GPCR-a |
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US (1) | US20100048632A1 (hr) |
EP (2) | EP2377863A1 (hr) |
JP (1) | JP2010514828A (hr) |
AT (1) | ATE523507T1 (hr) |
BR (1) | BRPI0806498A2 (hr) |
CA (1) | CA2674348A1 (hr) |
CY (1) | CY1112483T1 (hr) |
DK (1) | DK2114933T3 (hr) |
EA (1) | EA015129B1 (hr) |
ES (1) | ES2373181T3 (hr) |
HK (1) | HK1135703A1 (hr) |
HR (1) | HRP20110852T1 (hr) |
PL (1) | PL2114933T3 (hr) |
PT (1) | PT2114933E (hr) |
RS (1) | RS52065B (hr) |
SI (1) | SI2114933T1 (hr) |
WO (1) | WO2008081204A1 (hr) |
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-
2008
- 2008-01-04 JP JP2009544447A patent/JP2010514828A/ja active Pending
- 2008-01-04 SI SI200830454T patent/SI2114933T1/sl unknown
- 2008-01-04 AT AT08702095T patent/ATE523507T1/de active
- 2008-01-04 DK DK08702095.4T patent/DK2114933T3/da active
- 2008-01-04 EP EP11174256A patent/EP2377863A1/en not_active Withdrawn
- 2008-01-04 US US12/522,015 patent/US20100048632A1/en not_active Abandoned
- 2008-01-04 EA EA200900877A patent/EA015129B1/ru not_active IP Right Cessation
- 2008-01-04 BR BRPI0806498-9A2A patent/BRPI0806498A2/pt not_active IP Right Cessation
- 2008-01-04 RS RS20110523A patent/RS52065B/en unknown
- 2008-01-04 ES ES08702095T patent/ES2373181T3/es active Active
- 2008-01-04 EP EP08702095A patent/EP2114933B1/en active Active
- 2008-01-04 PL PL08702095T patent/PL2114933T3/pl unknown
- 2008-01-04 WO PCT/GB2008/050010 patent/WO2008081204A1/en active Application Filing
- 2008-01-04 PT PT08702095T patent/PT2114933E/pt unknown
- 2008-01-04 CA CA002674348A patent/CA2674348A1/en not_active Abandoned
-
2010
- 2010-04-16 HK HK10103731.6A patent/HK1135703A1/xx not_active IP Right Cessation
-
2011
- 2011-11-15 HR HR20110852T patent/HRP20110852T1/hr unknown
- 2011-11-25 CY CY20111101161T patent/CY1112483T1/el unknown
Also Published As
Publication number | Publication date |
---|---|
SI2114933T1 (sl) | 2012-01-31 |
EA200900877A1 (ru) | 2010-02-26 |
US20100048632A1 (en) | 2010-02-25 |
ES2373181T3 (es) | 2012-02-01 |
PL2114933T3 (pl) | 2012-02-29 |
HK1135703A1 (en) | 2010-06-11 |
WO2008081204A1 (en) | 2008-07-10 |
BRPI0806498A2 (pt) | 2014-04-22 |
JP2010514828A (ja) | 2010-05-06 |
EP2377863A1 (en) | 2011-10-19 |
DK2114933T3 (da) | 2012-01-02 |
CY1112483T1 (el) | 2015-12-09 |
ATE523507T1 (de) | 2011-09-15 |
PT2114933E (pt) | 2011-12-20 |
CA2674348A1 (en) | 2008-07-10 |
EP2114933B1 (en) | 2011-09-07 |
RS52065B (en) | 2012-06-30 |
EP2114933A1 (en) | 2009-11-11 |
EA015129B1 (ru) | 2011-06-30 |
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