MX2009013334A - Derivados de piperidina/piperazina. - Google Patents
Derivados de piperidina/piperazina.Info
- Publication number
- MX2009013334A MX2009013334A MX2009013334A MX2009013334A MX2009013334A MX 2009013334 A MX2009013334 A MX 2009013334A MX 2009013334 A MX2009013334 A MX 2009013334A MX 2009013334 A MX2009013334 A MX 2009013334A MX 2009013334 A MX2009013334 A MX 2009013334A
- Authority
- MX
- Mexico
- Prior art keywords
- sup
- compounds
- optionally
- substituted
- naphtalenyl
- Prior art date
Links
- 150000003053 piperidines Chemical class 0.000 title 1
- -1 adamantanyl Chemical group 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000005871 1,3-benzodioxolyl group Chemical group 0.000 abstract 2
- 102100036869 Diacylglycerol O-acyltransferase 1 Human genes 0.000 abstract 2
- 108050004099 Diacylglycerol O-acyltransferase 1 Proteins 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
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- 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
- A61K31/435—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
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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Abstract
La invención se refiere a un inhibidor de DGAT de fórmula (I) (ver fórmula I) que incluye cualquier forma estereoquímicamente isomérica del mismo, donde A representa CH o N; la línea punteada representa un enlace opcional en el caso en que A represente un átomo de carbono; X representa -O-C(=O).-; - C(=O)-C(=O)-; NRxC(=O) -Z-C(=O)-; ZNRxC(O) -C(=O)-Z-; NRx C(0)-Z-; -C(=S)-; NRxC(=S) -Z-C(S)-; Z.NRxC(S) -C(=S)--Z-; NRx C(=S)-Z-; Z representa un radical bivalente seleccionado de alcandillo C16, alquendiilo C26 o alquindiilo C26 donde cada alcandiilo C1, alquendiilo C2..6 o alquindillo C2..6 puede estar opcionalmente sustituido; y donde dos átomos de hidrógeno unidos al mismo carbono en el alcandiilo C16 pueden estar opcionalmente reemplazados por alcandiilo C1 Y representa _C(=O)NRx o _NRxC(O) R1 representa adamantanilo, cicloalquilo C36 arilo1 o Het1 R2 representa cicloalquilo C3.6, fenilo, naftalenilo, 2,3-dihidro-1 ,4-benzodioxinilo, 1,3-benzodioxolilo, 2,3-dihidrobenzofuranilo o un heterociclo aromático de 6 miembros que contiene 1 o 2 átomos de N, donde dicho cicloalquilo C3.6, fenilo, naftalenilo, 2, 3-dihidro- 1 ,4-benzodioxinilo, 1, 3-benzodioxolilo, o heterociclo pueden estar opcionalmente sustituidos; R7 representa hidrógeno, halo, alquilo C14, alquilo C1..4 sustituido con hidroxilo; con la salvedad de que se excluyen los siguientes compuestos (ver fórmulas A, B) un N-óxido de los mismos, una sal aceptable farmacéuticamente de los mismos o un solvato de los mismos; además, la invención se refiere además a métodos para preparar tales compuestos, composiciones farmacéuticas que comprenden dichos compuestos así como al uso como medicamento, como inhibidor de DGAT, de dichos compuestos.
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MX2009013334A MX2009013334A (es) | 2007-06-08 | 2008-06-05 | Derivados de piperidina/piperazina. |
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- 2008-06-05 JP JP2010510806A patent/JP5443343B2/ja active Active
- 2008-06-05 CA CA2687243A patent/CA2687243C/en active Active
- 2008-06-05 ES ES08760584.6T patent/ES2522617T3/es active Active
- 2008-06-05 WO PCT/EP2008/057008 patent/WO2008148849A2/en active Application Filing
- 2008-06-05 AU AU2008258558A patent/AU2008258558B2/en not_active Ceased
- 2008-06-05 MX MX2009013334A patent/MX2009013334A/es active IP Right Grant
- 2008-06-05 CN CN200880018624.9A patent/CN101678013B/zh active Active
- 2008-06-05 RU RU2009148796/04A patent/RU2478628C2/ru not_active IP Right Cessation
- 2008-06-05 BR BRPI0812923-1A2A patent/BRPI0812923A2/pt not_active Application Discontinuation
- 2008-06-05 EP EP08760584.6A patent/EP2155198B1/en active Active
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- 2008-06-06 PE PE2008000974A patent/PE20090820A1/es not_active Application Discontinuation
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- 2008-06-06 AR ARP080102426A patent/AR066153A1/es unknown
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PE20090820A1 (es) | 2009-06-27 |
US8946228B2 (en) | 2015-02-03 |
JP2010529085A (ja) | 2010-08-26 |
WO2008148849A2 (en) | 2008-12-11 |
RU2009148796A (ru) | 2011-07-20 |
BRPI0812923A2 (pt) | 2014-12-09 |
JO2972B1 (en) | 2016-03-15 |
US20100210618A1 (en) | 2010-08-19 |
US20160081997A1 (en) | 2016-03-24 |
JP5443343B2 (ja) | 2014-03-19 |
EP2155198A2 (en) | 2010-02-24 |
AR066153A1 (es) | 2009-07-29 |
RU2478628C2 (ru) | 2013-04-10 |
CN101678013B (zh) | 2014-05-07 |
CA2687243A1 (en) | 2008-12-11 |
EP2155198B1 (en) | 2014-08-13 |
CL2008001668A1 (es) | 2009-07-17 |
WO2008148849A8 (en) | 2009-07-09 |
AU2008258558A1 (en) | 2008-12-11 |
ES2522617T3 (es) | 2014-11-17 |
UY31134A1 (es) | 2009-03-02 |
TW200916449A (en) | 2009-04-16 |
PA8783401A1 (es) | 2009-01-23 |
TWI438197B (zh) | 2014-05-21 |
CN101678013A (zh) | 2010-03-24 |
CA2687243C (en) | 2016-07-12 |
US20150087629A1 (en) | 2015-03-26 |
WO2008148849A3 (en) | 2009-04-16 |
AU2008258558B2 (en) | 2013-11-07 |
US9227935B2 (en) | 2016-01-05 |
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