ME00681B - Jedinjenje indola - Google Patents
Jedinjenje indolaInfo
- Publication number
- ME00681B ME00681B MEP-2009-118A MEP11809A ME00681B ME 00681 B ME00681 B ME 00681B ME P11809 A MEP11809 A ME P11809A ME 00681 B ME00681 B ME 00681B
- Authority
- ME
- Montenegro
- Prior art keywords
- optionally substituted
- group
- hydrogen atom
- compound according
- methyl
- Prior art date
Links
- -1 Indole compound Chemical class 0.000 title 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 title 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 title 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 22
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 19
- 125000005843 halogen group Chemical group 0.000 claims abstract 8
- 229940002612 prodrug Drugs 0.000 claims abstract 6
- 239000000651 prodrug Substances 0.000 claims abstract 6
- 229940124828 glucokinase activator Drugs 0.000 claims abstract 4
- 208000008589 Obesity Diseases 0.000 claims abstract 3
- 239000003795 chemical substances by application Substances 0.000 claims abstract 3
- 206010012601 diabetes mellitus Diseases 0.000 claims abstract 3
- 235000020824 obesity Nutrition 0.000 claims abstract 3
- 239000008177 pharmaceutical agent Substances 0.000 claims abstract 3
- 150000003839 salts Chemical class 0.000 claims abstract 3
- 238000011282 treatment Methods 0.000 claims abstract 3
- 238000011321 prophylaxis Methods 0.000 claims abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- DLFVBJFMPXGRIB-UHFFFAOYSA-N thioacetamide Natural products CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 5
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 3
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 2
- KTFDYVNEGTXQCV-UHFFFAOYSA-N 2-Thiophenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CS1 KTFDYVNEGTXQCV-UHFFFAOYSA-N 0.000 claims 1
- 125000005915 C6-C14 aryl group Chemical group 0.000 claims 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
Classifications
-
- 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
- C07D417/14—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 three or more hetero rings
-
- 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
- A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/433—Thidiazoles
-
- 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
- A61P3/08—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Indole Compounds (AREA)
Abstract
Svrha ovog pronalaska je da obezbedi aktivator glukokinaze koristan kao farmaceutsko sredstvo kao što je sredstvo za profilaksu ili tretman dijabetesa, gojaznosti i slično. Ovaj pronalazak obezbeđuje aktivator glukokinaze koji sadrži jedinjenje predstavljeno formulom (I): gde R 1 je atom vodonika ili atom halogena; R 2 je grupa predstavljena sa gde je svaki simbol definisan u specifikaciji, ili njegovu so ili njegov prolek.
Claims (18)
1.Jedinjenje predstavljeno formulom (I): gde R1 je atom vodonika ili atom halogena; R2 je grupa predstavljena sa ili gde je A je CH ili N; R4 iR5 su svaki nezavisno opciono supstituisana C1-6 alkil grupa ili opciono supstituisana C3-10 cikloalkil grupa, ili R4 i R5 u kombinaciji formiraju opciono supstituisani prsten pri čemu prsten ne bi trebalo da bude morfolin; i R6, R7, R21 i R22 su svaki nezavisno atom vodonika, opciono supstituisana ugljovodonična grupa, cijano grupa ili acil grupa, ili R6 i R7 u kombinaciji formiraju opciono supstituisani prsten; W je O ili NR8, gde je R8 atom vodonika, opciono supstituisana C1-6 alkil grupa ili opciono supstituisana C3-10 cikloalkil grupa; R3 je opciono supstituisana heterociklična grupa ili opciono supstituisana C6-14 aril grupa; i R9, R10 i R11 su svaki nezavisno atom vodonika, atom halogena, opciono supstituisana C1-6 alkil grupa ili opciono supstituisana C1-6 alkoksi grupa, pod uslovom da je isključeno jedinjenje gde je R21 atom vodonika ili C1-6 alkoksi-karbonil grupa, R22 je atom vodonika, a R6 i R7 su oba atomi vodonika, i jedinjenje gde je R21 atom vodonika ili C1-6 alkoksi-karbonil grupa, R22 je atom vodonika, a R6 i R7 su oba metil grupe, ili njegova so.
2.Jedinjenje u skladu sa patentim zahtevom 1, naznačeno time što je to jedinjenje predstavljeno formulom (I): R1 atom vodonika ili atom halogena; R je grupa predstavljena sa ili pri čemu A je CH ili N; R4 i R5 su svaki nezavisno opciono supstituisana C1-6 alkil grupa ili opciono supstituisana C3-10 cikloalkil grupa, ili R4 i R5 u kombinaciji formiraju opciono supstituisani prsten, pri čemu prsten ne bi trebalo da bude morfolin; i R6 i R7 su svaki nezavisno atom vodonika, opciono supstituisana ugljovodonična grupa, cijano grupa ili acil grupa, ili R6 i R7 u kombinaciji formiraju opciono supstituisani prsten; W je O ili NR8, gde je R8 atom vodonika ili opciono supstituisana C1-6 alkil grupa; R3 je opciono supstituisana heterociklična grupa; 1 R9, R10 i R11 su svaki nezavisno atom vodonika, atom halogena, opciono supstituisana C1-6 alkil grupa ili opciono supstituisana C1-6 alkoksi grupa, pod uslovom daje isključeno jedinjenje gde su i R6 i R7 atomi vodonika, i jedinjenje gde su i R6 i R7 metil grupa, ili njegova so.
3.Jedinjenje u skladu sa patentnim zahtevom 1, naznačeno time što je R grupa predstavljena sa gde su R6 i R7 kako je definisano u patetnom zahtevu 1.
4. Jedinjenje u skladu sa patentim zahtevom 3, naznačeno time što je R6 = C1-6 alkil grupa supstituisana sa opciono supstituisanom heterocikličnom grupom.
5. Jedinjenje u skladu sa patentim zahtevom 3, naznačeno time što je R7 atom vodonika.
6. Jedinjenje u skladu sa patentim zahtevom 3, naznačeno time što R6 i R7 u kombinaciji formiraju opciono supstituisani prsten.
7. Jedinjenje u skladu sa patentim zahtevom 3, naznačeno time što je W = NR8, pri čemu je R8 kako je definisano u patentnom zahtevu 1.
8. Jedinjenje u skladu sa patentim zahtevom 3, naznačeno time što je R3 5- ili 6-člana monociklična aromatična heterociklična grupa.
9. Jedinjenje u skladu sa patentim zahtevom 3, naznačeno time što je R9 atom vodonika ili atom halogena.
10. Jedinjenje u skladu sa patentim zahtevom 3, naznačeno time što je R10 atom vodonika, atom halogena, C1-6 alkil grupa ili opciono supstituisana C1-6 alkoksi grupa.
11. Jedinjenje u skladu sa patentim zahtevom 3, naznačeno time što je R11 atom vodonika, atom halogena ili C1-6 alkil grupa.
12. N, N-dimetil-2-{4-[(2-{7-[metil(2-tienilsulfonil)amino]-lH-indol-2-il}-l, 3-tiazol-5-iljmetiljpiperazin-1 -il} acetamid; N-metil-N-[2-(8-oksa-l-tia-3-azaspiro[4. 5]dec-2-en-2-il)-lH-indol-7-il]tiofen-2-sulfonamid; N-[2-[4-(hidroksimetil)-4, 5-dihidro-l, 3-tiazol-2-il]-5-(2-metoksietoksi)-lH-indol-7-il]-N-metilpiridin-2- sulfonamid; N-metil-N-{2-[5-(morfolinometil)-4, 5-dihidro-l, 3-tiazol-2-il]-lH-indol-7-il}tiofen-2-sulfonamid; 2-(2-{7-[metil(piridin-2-ilsulfonil)amino]-lH-indol-2-il}-4. 5-dihidro-l, 3-tiazol-5-il)acetamid; N-(difluorometil)-N-{2-[5-(morfolinometil)-4, 5-dihidro-l, 3-tiazol-2-il]-lH-indol-7-il}tiofen-2-sulfonamid; 2-{2-[7-[metil(2-tiemlsulfoml)amino]-5-(trifluorometoksi)-lH-mdol-2-il]-4, 5-diWdro-l, 3-tiazol-5- iljacetamid; N-(5-(2-metoksietoksi)-2- {5-[( 1 -oksidotiomorfolino)metil]-4, 5-dihidro-1, 3 -tiazol-2-il} -1 H-indol-7-il)-N-metilpiridin-2-sulfonamid; 2-(2-{7-[metil(2-tienilsulfonil)amino]-lH-indol-2-il}-l-tia-3, 8-diazaspiro[4. 5]dec-2-en-8-il)acetamid; ili N-[2-{5-[(l, l-dioksidotiomorfolino)metil]-4, 5-dihidro-l, 3-tiazol-2-il}-5-(2-metoksietoksi)-lH-indol-7-il]-N-metilpiridin-2-sulfonamid; ili njegova so.
13. Prolek jedinjenja u skladu sa patentim zahtevom 1.
14. Aktivator glukokinaze koji uključuje jedinjenje u skladu sa patentim zahtevom 1 ili njegov prolek.
15. Farmaceutsko sredstvo koji uključuje jedinjenje u skladu sa patentim zahtevom 1 ili njegov prolek.
16. Farmaceutsko sredstvo u skladu sa patentim zahtevom 15, naznačeno time što je to sredstvo za profilaksu ili tretman dijabetesa ili gojaznosti.
17. Upotreba jedinjenja u skladu sa patentim zahtevom 1 ili njegovog proleka za produkciju aktivatora glukokinaze.
18. Upotreba jedinjenja u skladu sa patentim zahtevom 1 ili njegovog proleka za produkciju sredstva za profilaksu ili tretman dijabetesa ili gojaznosti.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2006285551 | 2006-10-19 | ||
| PCT/JP2007/070772 WO2008050821A1 (en) | 2006-10-19 | 2007-10-18 | Indole compound |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ME00681B true ME00681B (me) | 2011-12-20 |
| MEP11809A MEP11809A (en) | 2011-12-20 |
Family
ID=39010108
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-118/09A MEP11809A (en) | 2006-10-19 | 2007-10-18 | Indole compound |
Country Status (26)
| Country | Link |
|---|---|
| US (4) | US8410087B2 (me) |
| EP (2) | EP2074119A1 (me) |
| JP (1) | JP5260507B2 (me) |
| KR (1) | KR101444486B1 (me) |
| CN (1) | CN101573357B (me) |
| AU (1) | AU2007310064B2 (me) |
| BR (1) | BRPI0717722A2 (me) |
| CA (1) | CA2666973C (me) |
| CL (1) | CL2008001017A1 (me) |
| CR (1) | CR10748A (me) |
| EC (1) | ECSP099330A (me) |
| GE (1) | GEP20115241B (me) |
| IL (1) | IL198154A (me) |
| MA (1) | MA30890B1 (me) |
| ME (1) | MEP11809A (me) |
| MX (1) | MX2009003972A (me) |
| MY (1) | MY158052A (me) |
| NO (1) | NO20091948L (me) |
| NZ (1) | NZ576570A (me) |
| PE (1) | PE20090884A1 (me) |
| RU (1) | RU2454415C9 (me) |
| TN (1) | TN2009000129A1 (me) |
| TW (1) | TWI460176B (me) |
| UA (1) | UA97257C2 (me) |
| WO (1) | WO2008050821A1 (me) |
| ZA (1) | ZA200902585B (me) |
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| WO2009082152A2 (en) | 2007-12-20 | 2009-07-02 | Lg Life Sciences Ltd. | Glucokinase activators and pharmaceutical compositions containing the same as an active ingredient |
| EP2230238B1 (en) * | 2008-01-04 | 2013-12-11 | LG Life Sciences Ltd. | Indole and indazole derivatives having a cell-, tissue- and organ-preserving effect |
| EP2242745A1 (de) * | 2008-02-07 | 2010-10-27 | Sanofi-Aventis | Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung |
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