AR081252A1 - Compuestos para el tratamiento del sindrome metabolico - Google Patents
Compuestos para el tratamiento del sindrome metabolicoInfo
- 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
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 208000001145 Metabolic Syndrome Diseases 0.000 title 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 title 1
- 125000005843 halogen group Chemical group 0.000 abstract 9
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 abstract 6
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 4
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000004970 halomethyl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 2
- -1 N-pyrazolyl Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001188 haloalkyl group Chemical group 0.000 abstract 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- HCMJWOGOISXSDL-UHFFFAOYSA-N (2-isothiocyanato-1-phenylethyl)benzene Chemical compound C=1C=CC=CC=1C(CN=C=S)C1=CC=CC=C1 HCMJWOGOISXSDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- STHHLVCQSLRQNI-UHFFFAOYSA-N 1-azabicyclo[3.2.1]octane Chemical compound C1C2CCN1CCC2 STHHLVCQSLRQNI-UHFFFAOYSA-N 0.000 abstract 1
- FMEHIMDNLRASDU-UHFFFAOYSA-N 1-azabicyclo[3.3.1]nonane Chemical compound C1CCN2CCCC1C2 FMEHIMDNLRASDU-UHFFFAOYSA-N 0.000 abstract 1
- DTGDMYHJFTVULL-UHFFFAOYSA-N 3-oxa-7-azabicyclo[3.3.1]nonane Chemical compound C1OCC2CNCC1C2 DTGDMYHJFTVULL-UHFFFAOYSA-N 0.000 abstract 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 1
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 abstract 1
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000000556 agonist Substances 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Hematology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Obesity (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
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.
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 (es) | 2012-07-18 |
Family
ID=44227954
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110101820A AR081252A1 (es) | 2010-05-28 | 2011-05-27 | Compuestos para el tratamiento del sindrome metabolico |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR081252A1 (es) |
| TW (1) | TW201209054A (es) |
| WO (1) | WO2011147951A1 (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2602813T3 (es) | 2011-06-09 | 2017-02-22 | Rhizen Pharmaceuticals S.A. | Nuevos compuestos como moduladores de GPR-119 |
| WO2013169531A1 (en) | 2012-05-09 | 2013-11-14 | Boehringer Ingelheim International Gmbh | Methods for making oxetan-3-ylmethanamines |
| CA2878625A1 (en) | 2012-07-11 | 2014-01-16 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| CN107531589A (zh) | 2015-01-23 | 2018-01-02 | Gvk生物科技私人有限公司 | TrkA激酶抑制剂 |
| WO2016131198A1 (en) * | 2015-02-18 | 2016-08-25 | Eli Lilly And Company | Pyrazole compounds |
| CN104788386A (zh) * | 2015-04-24 | 2015-07-22 | 湖南华腾制药有限公司 | 一种含氟嘧啶化合物的制备方法 |
| EA202091881A1 (ru) | 2018-02-05 | 2020-11-10 | Алкермес, Инк. | Соединения для лечения боли |
| CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CA3173731A1 (en) | 2020-02-28 | 2021-09-02 | Kallyope, Inc. | Gpr40 agonists |
| KR20230012597A (ko) | 2020-05-19 | 2023-01-26 | 칼리오페, 인크. | Ampk 활성화제 |
| AU2021297323A1 (en) | 2020-06-26 | 2023-02-16 | Kallyope, Inc. | AMPK activators |
| IL291418B2 (en) | 2022-03-16 | 2024-05-01 | Anima Biotech Inc | Substances that function as modulators of cMYC-mRNA translation and their uses for cancer treatment |
| WO2025037212A1 (en) * | 2023-08-11 | 2025-02-20 | Mankind Pharma Ltd. | Processes for the preparation and purification of a gpr119 agonist compound |
Family Cites Families (38)
| 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 |
| AU2004303604B2 (en) | 2003-12-24 | 2011-03-24 | Prosidion Limited | Heterocyclic derivatives as GPCR receptor agonists |
| CA2591738A1 (en) | 2004-12-22 | 2006-06-29 | Merck & Co., Inc. | Process for making substituted piperidines |
| KR20070091038A (ko) | 2004-12-24 | 2007-09-06 | 프로시디온 리미티드 | Ｇ-단백질 결합 수용체(ｇｐｒ116) 효능제 및 비만 및당뇨병을 치료하기 위한 이의 용도 |
| EP1838706A1 (en) | 2004-12-24 | 2007-10-03 | Prosidion Limited | G-protein coupled receptor agonists |
| GB0428514D0 (en) | 2004-12-31 | 2005-02-09 | Prosidion Ltd | Compounds |
| US20090325924A1 (en) | 2005-06-30 | 2009-12-31 | Stuart Edward | GPCR Agonists |
| MX2007016508A (es) | 2005-06-30 | 2008-03-04 | Prosidion Ltd | Agonistas del receptor acoplado a la proteina g. |
| BRPI0612599A2 (pt) | 2005-06-30 | 2010-11-23 | Prosidion Ltd | composto, composição farmacêutica compreendendo o mesmo, método de tratamento e uso do mesmo |
| US20090221644A1 (en) | 2005-06-30 | 2009-09-03 | Stuart Edward Bradley | Gpcr Agonists |
| US20090221639A1 (en) | 2006-04-06 | 2009-09-03 | Lisa Sarah Bertram | Heterocyclic GPCR Agonists |
| GB0607196D0 (en) | 2006-04-11 | 2006-05-17 | Prosidion Ltd | G-protein coupled receptor agonists |
| WO2007148185A2 (en) | 2006-06-21 | 2007-12-27 | Pfizer Products Inc. | Substituted 3 -amino- pyrrolidino-4 -lactams as dpp inhibitors |
| CA2661371A1 (en) * | 2006-08-30 | 2008-03-06 | Biovitrum Ab (Publ) | Pyrimidine compounds for treating gpr119 related disorders |
| TWI387585B (zh) | 2006-09-01 | 2013-03-01 | Dow Agrosciences Llc | 殺蟲性之ｎ-取代（雜芳基）烷基烴基硫亞胺 |
| GB0619343D0 (en) | 2006-09-30 | 2006-11-08 | Vernalis R&D Ltd | New chemical compounds |
| JP5330260B2 (ja) | 2006-12-06 | 2013-10-30 | スミスクライン ビーチャム コーポレーション | 二環式化合物ならびに抗糖尿病薬としての使用 |
| US7638541B2 (en) | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| BRPI0806312A2 (pt) | 2007-01-04 | 2011-09-06 | Prosidion Ltd | agonistas cgpr piperidina |
| JP2010514828A (ja) | 2007-01-04 | 2010-05-06 | プロシディオン・リミテッド | ピペリジンｇｐｃｒアゴニスト |
| CL2008000017A1 (es) | 2007-01-04 | 2008-08-01 | Prosidion Ltd | Compuestos derivados de heterociclos de nitrogeno y oxigeno, agonistas de gpcr; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento de la obesidad, diabetes, sindrome metabolico, hiperlipidemia, toleranci |
| GB0700122D0 (en) | 2007-01-04 | 2007-02-14 | Prosidion Ltd | GPCR agonists |
| AR064735A1 (es) | 2007-01-04 | 2009-04-22 | Prosidion Ltd | Agonistas de gpcr y composicion farmaceutica en base al compuesto |
| 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 |
| BRPI0909469A2 (pt) | 2008-03-31 | 2015-12-29 | Metabolex Inc | compostos de oximetileno de arila e usos dos mesmos |
| 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 |
| GB0812641D0 (en) | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| GB0812648D0 (en) | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| ATE557024T1 (de) | 2008-07-10 | 2012-05-15 | Prosidion Ltd | Piperidinverbindungen als gpcr-agonisten |
| GB0812642D0 (en) | 2008-07-10 | 2008-08-20 | Prosidion Ltd | Compounds |
| MX2011000060A (es) | 2008-07-10 | 2011-02-22 | Prosidion Ltd | Agonistas del receptor acoplado a la proteina g piperidinilo. |
| JP5657518B2 (ja) | 2009-02-18 | 2015-01-21 | 武田薬品工業株式会社 | 縮合複素環化合物 |
-
2011
- 2011-05-24 TW TW100118140A patent/TW201209054A/zh unknown
- 2011-05-27 AR ARP110101820A patent/AR081252A1/es unknown
- 2011-05-27 WO PCT/EP2011/058703 patent/WO2011147951A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| WO2011147951A1 (en) | 2011-12-01 |
| TW201209054A (en) | 2012-03-01 |
| WO2011147951A8 (en) | 2012-03-15 |
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