AR081252A1 - COMPOUNDS FOR THE TREATMENT OF METABOLIC SYNDROME - Google Patents
COMPOUNDS FOR THE TREATMENT OF METABOLIC SYNDROMEInfo
- Publication number
- AR081252A1 AR081252A1 ARP110101820A ARP110101820A AR081252A1 AR 081252 A1 AR081252 A1 AR 081252A1 AR P110101820 A ARP110101820 A AR P110101820A AR P110101820 A ARP110101820 A AR P110101820A AR 081252 A1 AR081252 A1 AR 081252A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- optionally substituted
- cycloalkyl
- heteroaryl
- Prior art date
Links
Classifications
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61P3/06—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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/08—Bridged systems
Abstract
Composición farmacéutica y usos como agonistas de GPR119. Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde A es un fenilo para sustituido o un anillo heteroarilo de 6 miembros para sustituido que contienen uno a tres átomos de nitrógeno; R1 es hidrógeno, halo, ciano, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4 o alcoxialquilo C2-6; R2 es: un resto de fórmula (2), fenilo opcionalmente sustituido con uno o más grupos halo, metilo, halometilo o metoxi, o piridilo, N-piridonilo o N-pirazolilo, opcionalmente sustituido con uno o más grupos halo, alquilo C1-2 o halometilo; R3 es independientemente halo, metilo o halometilo; Z es -C(O)OR4, -C(O)R4, -S(O)2R4, -S(O)2N(alquil C1-3)R4, heteroarilo o -CH2-heteroarilo, y cuando p y q son ambos 0, Z también puede ser -CH2-fenilo, dicho fenilo está opcionalmente sustituido con uno o dos grupos independientemente seleccionados de alquilo C1-4, haloalquilo C1-4 y halo; R4 es arilo, heteroarilo, alquilo C2-6, cicloalquilo C3-6, heterociclilo C4-6, heterociclilalquilo C1-4, alcoxialquilo C2-6, arilalquilo C1-4, heteroarilalquilo C1-4 o cicloalquil C4-6alquilo C1-4, dicho cicloalquilalquilo C1-4 está opcionalmente sustituido con alquilo C1-4; en donde cuando Z es o incluye heteroarilo o cuando R4 es o incluye arilo o heteroarilo, dicho arilo o heteroarilo puede estar opcionalmente sustituido con uno o dos grupos seleccionados de halo, ciano, SF5, alquilo C1-4, haloalquilo C1-4, hidroxialquilo C1-5, alcoxi C1-4, alcoxialquilo C2-4, heterociclilo, heterociclilalquilo C1-4, heteroarilalquilo C1-4, alquilamino C1-4, alquilamino C1-4alquilo C1-4, cicloalquilo C3-6 y -(alquil C1-3)-(cicloalquilo C3-6), en donde los grupos cicloalquilo y alquilo están cada uno opcionalmente sustituidos con uno o dos grupos independientemente seleccionados de alquilo C1-4, hidroxi o halo; X se selecciona de CR5H, O, y NR6 en los cuales R5 y R6 son independientemente hidrógeno o alquilo C1-2; Y es Y1 o W-Y1, donde W es un anillo heteroarilo de 5 miembros que contiene uno o más heteroátomos seleccionados de N, O y S, e Y1 se seleccione de CR7H, O y NR8, en los cuales R7 es hidrógeno, alquilo C1-2, alcoxialquilo C2-6 o heterociclilo; en donde dicho alquilo C1-2 puede estar opcionalmente sustituido con ciano, hidroxi o halo y R8 es alquilo C1-4 o cicloalquilo C1-4, siempre que cuando Y es W-Y1, X es O y Y1 es CR7H, cuando Y1 es O ó NR8, X es CR5H y cuando X es O ó NR6, Y1 es CR7H; cada uno de R9 y R10 es independientemente H, halo, alquilo C1-2, haloalquilo C1-2, alcoxi C1-3 o hidroxi; o R9 y R10 se unen para formar un azabiciclo[3.3.1]nonano, un 3-oxa-7-azabiciclo[3.3.1]nonano o un azabiciclo[3.2.1]octano; R11 es H, halo, alquilo C1-2, haloalquilo C1-2 o alcoxi C1-3; m es 0, 1 ó 2; n es 0 ó 1; p y q son cada uno 0, 1 ó 2, siempre que 0 L p + q L 2; y r es 1 ó 2.Pharmaceutical composition and uses as agonists of GPR119. Claim 1: A compound of the formula (1) or a pharmaceutically acceptable salt thereof, wherein A is a substituted phenyl or a 6-membered heteroaryl ring containing one to three nitrogen atoms; R1 is hydrogen, halo, cyano, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy or C2-6 alkoxyalkyl; R2 is: a moiety of formula (2), phenyl optionally substituted with one or more halo, methyl, halomethyl or methoxy groups, or pyridyl, N-pyridonyl or N-pyrazolyl, optionally substituted with one or more halo groups, C1- alkyl 2 or halomethyl; R3 is independently halo, methyl or halomethyl; Z is -C (O) OR4, -C (O) R4, -S (O) 2R4, -S (O) 2N (C1-3 alkyl) R4, heteroaryl or -CH2-heteroaryl, and when p and q are both 0 , Z may also be -CH2-phenyl, said phenyl is optionally substituted with one or two groups independently selected from C1-4 alkyl, C1-4 haloalkyl and halo; R 4 is aryl, heteroaryl, C 2-6 alkyl, C 3-6 cycloalkyl, C 4-6 heterocyclyl, C 1-4 heterocyclylalkyl, C 2-6 alkoxyalkyl, C 1-4 arylalkyl, C 1-4 heteroarylalkyl or C 1-4 alkyl cycloalkyl, said C1-4 cycloalkylalkyl is optionally substituted with C1-4 alkyl; wherein when Z is or includes heteroaryl or when R4 is or includes aryl or heteroaryl, said aryl or heteroaryl may be optionally substituted with one or two groups selected from halo, cyano, SF5, C1-4 alkyl, C1-4 haloalkyl, hydroxyalkyl C1-5, C1-4 alkoxy, C2-4 alkoxyalkyl, heterocyclyl, C1-4 heterocyclylalkyl, C1-4 heteroarylalkyl, C1-4 alkylamino, C1-4 alkylamino C1-4 alkyl, C3-6 cycloalkyl and - (C1-3 alkyl ) - (C3-6 cycloalkyl), wherein the cycloalkyl and alkyl groups are each optionally substituted with one or two groups independently selected from C1-4 alkyl, hydroxy or halo; X is selected from CR5H, O, and NR6 in which R5 and R6 are independently hydrogen or C1-2 alkyl; Y is Y1 or W-Y1, where W is a 5-membered heteroaryl ring containing one or more heteroatoms selected from N, O and S, and Y1 is selected from CR7H, O and NR8, in which R7 is hydrogen, alkyl C1-2, C2-6 alkoxyalkyl or heterocyclyl; wherein said C1-2 alkyl may be optionally substituted with cyano, hydroxy or halo and R8 is C1-4 alkyl or C1-4 cycloalkyl, provided that when Y is W-Y1, X is O and Y1 is CR7H, when Y1 is O or NR8, X is CR5H and when X is O or NR6, Y1 is CR7H; each of R9 and R10 is independently H, halo, C1-2 alkyl, C1-2 haloalkyl, C1-3 alkoxy or hydroxy; or R9 and R10 join to form an azabicyclo [3.3.1] nonane, a 3-oxa-7-azabicyclo [3.3.1] nonane or an azabicyclo [3.2.1] octane; R11 is H, halo, C1-2 alkyl, C1-2 haloalkyl or C1-3 alkoxy; m is 0, 1 or 2; n is 0 or 1; p and q are each 0, 1 or 2, provided that 0 L p + q L 2; and r is 1 or 2.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1008985.2A GB201008985D0 (en) | 2010-05-28 | 2010-05-28 | Novel compounds |
| GBGB1019547.7A GB201019547D0 (en) | 2010-11-19 | 2010-11-19 | Novel compounds |
| GB1103283.6A GB2488360A (en) | 2011-02-25 | 2011-02-25 | Heterocyclic GPCR agonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR081252A1 true AR081252A1 (en) | 2012-07-18 |
Family
ID=44227954
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110101820A AR081252A1 (en) | 2010-05-28 | 2011-05-27 | COMPOUNDS FOR THE TREATMENT OF METABOLIC SYNDROME |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR081252A1 (en) |
| TW (1) | TW201209054A (en) |
| WO (1) | WO2011147951A1 (en) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2602813T3 (en) | 2011-06-09 | 2017-02-22 | Rhizen Pharmaceuticals S.A. | New compounds as modulators of GPR-119 |
| JP6030752B2 (en) | 2012-05-09 | 2016-11-24 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Method for producing oxetane-3-ylmethanamine |
| EP2872127A1 (en) | 2012-07-11 | 2015-05-20 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| RU2017129757A (en) | 2015-01-23 | 2019-02-25 | ДжиВиКей БИОСАЕНСЕЗ ПРАЙВИТ ЛИМИТЕД | TRKA KINASE INHIBITORS |
| WO2016131198A1 (en) * | 2015-02-18 | 2016-08-25 | Eli Lilly And Company | Pyrazole compounds |
| CN104788386A (en) * | 2015-04-24 | 2015-07-22 | 湖南华腾制药有限公司 | Preparation method of fluorine-containing pyrimidine compound |
| CN111989327A (en) | 2018-02-05 | 2020-11-24 | 奥克梅斯公司 | Compounds for the treatment of pain |
| CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| AU2021275038A1 (en) | 2020-05-19 | 2022-12-22 | Kallyope, Inc. | AMPK activators |
| CN116390925A (en) | 2020-06-26 | 2023-07-04 | 卡尔优普公司 | AMPK activator |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6221660B1 (en) | 1999-02-22 | 2001-04-24 | Synaptic Pharmaceutical Corporation | DNA encoding SNORF25 receptor |
| GB0230045D0 (en) | 2002-12-23 | 2003-01-29 | Glaxo Group Ltd | Compounds |
| NZ547965A (en) | 2003-12-24 | 2009-12-24 | Prosidion Ltd | 1,2,4-Oxadiazole derivatives as GPCR receptor agonists |
| CN101084191A (en) | 2004-12-22 | 2007-12-05 | 默克公司 | Process for making substituted piperidines |
| US8193359B2 (en) | 2004-12-24 | 2012-06-05 | Prosidion Limited | G-protein coupled receptor agonists |
| EP1838311A1 (en) | 2004-12-24 | 2007-10-03 | Prosidion Limited | G-protein coupled receptor (gpr116) agonists and use thereof for treating obesity and diabetes |
| GB0428514D0 (en) | 2004-12-31 | 2005-02-09 | Prosidion Ltd | Compounds |
| US20090325924A1 (en) | 2005-06-30 | 2009-12-31 | Stuart Edward | GPCR Agonists |
| MX2007016545A (en) | 2005-06-30 | 2008-02-21 | Prosidion Ltd | G-protein coupled receptor agonists. |
| EP1907384A2 (en) | 2005-06-30 | 2008-04-09 | Prosidion Limited | Gpcr agonists |
| US20100063081A1 (en) | 2005-06-30 | 2010-03-11 | Stuart Edward Bradly | CPCR Agonists |
| US20090221639A1 (en) | 2006-04-06 | 2009-09-03 | Lisa Sarah Bertram | Heterocyclic GPCR Agonists |
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| JP2010501629A (en) * | 2006-08-30 | 2010-01-21 | ビオヴィトルム・アクチボラゲット（プブリクト） | Pyridine compounds for treating GPR119 related disorders |
| TWI387585B (en) | 2006-09-01 | 2013-03-01 | Dow Agrosciences Llc | Insecticidal n-substituted (heteroaryl)alkyl sulfilimines |
| GB0619343D0 (en) | 2006-09-30 | 2006-11-08 | Vernalis R&D Ltd | New chemical compounds |
| CN101657471B (en) | 2006-12-06 | 2013-07-03 | 史密丝克莱恩比彻姆公司 | Bicyclic compounds and use as antidiabetics |
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| CL2008000018A1 (en) | 2007-01-04 | 2008-08-01 | Prosidion Ltd | COMPOUNDS DERIVED FROM NITROGEN AND OXYGEN HETEROCICLES, GPCR AGONISTS; PHARMACEUTICAL COMPOSITION THAT INCLUDES SUCH COMPOUND; AND USE OF THE COMPOUND FOR THE TREATMENT OF OBESITY, DIABETES, METABOLIC SYNDROME, HYPERLIPIDEMIA, TOLERANCE |
| PE20081849A1 (en) | 2007-01-04 | 2009-01-26 | Prosidion Ltd | PIPERIDIN-4-IL-PROPOXY-BENZAMIDE DERIVATIVES AS GPCR AGONISTS |
| CA2674360A1 (en) | 2007-01-04 | 2008-07-10 | Prosidion Limited | Piperidine gpcr agonists |
| GB0700122D0 (en) | 2007-01-04 | 2007-02-14 | Prosidion Ltd | GPCR agonists |
| US20100048632A1 (en) | 2007-01-04 | 2010-02-25 | Matthew Colin Thor Fyfe | Piperidine GPCR Agonists |
| EP2200609A1 (en) | 2007-09-10 | 2010-06-30 | Prosidion Limited | Compounds for the treatment of metabolic disorders |
| GB0720390D0 (en) | 2007-10-18 | 2007-11-28 | Prosidion Ltd | G-Protein coupled receptor agonists |
| GB0720389D0 (en) | 2007-10-18 | 2008-11-12 | Prosidion Ltd | G-Protein Coupled Receptor Agonists |
| WO2009117421A2 (en) | 2008-03-17 | 2009-09-24 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| AU2009231906A1 (en) | 2008-03-31 | 2009-10-08 | Metabolex, Inc. | Oxymethylene aryl compounds and uses thereof |
| GB0811304D0 (en) | 2008-06-19 | 2008-07-30 | Ucb Pharma Sa | Therapeutic agents |
| GB0812031D0 (en) | 2008-07-01 | 2008-08-06 | 7Tm Pharma As | Thiazole derivatives |
| GB0812649D0 (en) | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| GB0812648D0 (en) | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| GB0812641D0 (en) | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| AU2009269772A1 (en) | 2008-07-10 | 2010-01-14 | Prosidion Limited | Piperidinyl GPCR agonists |
| ATE557024T1 (en) | 2008-07-10 | 2012-05-15 | Prosidion Ltd | PIPERIDINE COMPOUNDS AS GPCR AGONISTS |
| GB0812642D0 (en) | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| WO2010095663A1 (en) | 2009-02-18 | 2010-08-26 | 武田薬品工業株式会社 | Fused heterocyclic ring compound |
-
2011
- 2011-05-24 TW TW100118140A patent/TW201209054A/en unknown
- 2011-05-27 AR ARP110101820A patent/AR081252A1/en unknown
- 2011-05-27 WO PCT/EP2011/058703 patent/WO2011147951A1/en active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011147951A1 (en) | 2011-12-01 |
| WO2011147951A8 (en) | 2012-03-15 |
| TW201209054A (en) | 2012-03-01 |
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