AR082844A1 - Derivados de piperidina y su uso para el tratamiento de desordenes metabolicos - Google Patents

Derivados de piperidina y su uso para el tratamiento de desordenes metabolicos

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Publication number
AR082844A1
AR082844A1 ARP110102362A ARP110102362A AR082844A1 AR 082844 A1 AR082844 A1 AR 082844A1 AR P110102362 A ARP110102362 A AR P110102362A AR P110102362 A ARP110102362 A AR P110102362A AR 082844 A1 AR082844 A1 AR 082844A1
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Argentina
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alkyl
carbocyclyl
group
optionally substituted
heterocyclyl
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ARP110102362A
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English (en)
Inventor
Martin Fleck
Thorsten Lehmann-Lintz
Heike Neubauer
Bernd Nosse
Gerald Juergen Roth
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Boehringer Ingelheim Int
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Publication of AR082844A1 publication Critical patent/AR082844A1/es

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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4465Non condensed piperidines, e.g. piperocaine only substituted in position 4
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D498/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Obesity (AREA)
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  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Su uso como medicamentos, métodos para su uso terapéutico y composiciones farmacéuticas que los contienen.Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula general (1) en la que Ar1 se selecciona del grupo Ar1-G1 que consiste en arilo y heteroarilo, todos los cuales pueden estar opcionalmente sustituidos con uno o más sustituyentes RA, en donde dos sustituyentes RA enlazados a átomos de C adyacentes de Ar1 pueden estar conectados uno con otro y juntos forman un grupo de puenteo de alquileno C3-5, en el que 1, 2 ó 3 grupos CH2 pueden estar reemplazados por O, C(=O), S, S(=O), S(=O)2, NH o N(alquilo C1-4)-, en donde el puente de alquileno puede estar opcionalmente sustituido con uno o dos grupos alquilo C1-3; y RA se selecciona del grupo RA-G1 que consiste en H, F, Cl, Br, I, CN, OH, -NO2, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo C3-10, carbociclil C3-10-alquilo C1-3, alquil C1-6-O-, alquenil C3-6-O-, alquinil C3-6-O-, carbociclil C3-10-O-, carbociclil C3-10-alquil C1-3-O-, alquil C1-6-S-, alquil C1-6-S(=O)-, alquil C1-6-S(=O)2-, carbociclil C3-10-S-, carbociclil C3-10-alquil C1-3-S-, alquil C1-4-C(=O)-, carbociclil C3-10-C(=O)-, RN1RN2N-, RN1RN2N-alquil C2-3-O-, RN1RN2N-C(=O)-, RN1RN2N-S(=O)2-, alquil C1-6-C(=O)-NRN1-, alquil C1-6-S(=O)2-NRN1-, alquil C1-6-C(=O)NRN1-alquil C1-3-, HO-C(=O)-, alquil C1-6-O-C(=O)-, heterociclilo, heterociclil-O-, heterociclil-alquilo C1-3, heterociclil-alquil C1-3-O-, heterociclil-C(=O)-, arilo, aril-alquilo C1-3, aril-O-, aril-alquil C1-3-O-, heteroarilo, heteroaril-alquilo C1-3, heteroaril-O-, heteroaril-alquil C1-3-O- y heteroaril-C(=O), en donde en cada uno de carbociclilo y heterociclilo un grupo CH2 puede estar opcionalmente reemplazado por -C(=O)- o -C(=CRAlk2)-, y en donde cada uno de carbociclilo y heterociclilo puede estar opcionalmente sustituido con uno o más alquilo C1-4 que pueden estar opcionalmente sustituidos con uno o más sustituyentes RC, y en donde cada uno de alquilo, carbociclilo y heterociclilo puede estar opcionalmente sustituido con uno o más sustituyentes RC, y en donde cada heterociclilo puede estar opcionalmente sustituido con arilo o heteroarilo, y en donde cada grupo arilo y heteroarilo puede estar opcionalmente sustituido con uno o más sustituyentes L; RC se selecciona del grupo RC-G1 que consiste en F, Cl, Br, CN, OH, alquil C1-4-O-, cicloalquil C3-7-O-, cicloalquil C3-7-alquil C1-3-O-, H2N-, (alquil C1-4)NH-, (alquil C1-4)2N-, H2N-C(=O)-, (alquil C1-4)NH-C(=O)-, (alquil C1-4)2N-C(=O)-, alquil C1-4-C(=O)-, alquil C1-4-S(=O)2-, HO-C(=O)- y alquil C1-4-O-C(=O)-, en donde cada uno de alquilo y cicloalquilo puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados de F y OH; y RN1 se selecciona del grupo RN1-G1 que consiste en H, alquilo C1-6, carbociclilo C3-10, carbociclil C3-10-alquilo C1-3, alquenilo C3-6, alquinilo C3-6, heterociclilo, heterociclil-alquilo C1-3, arilo, aril-alquilo C1-3, heteroarilo y heteroaril-alquilo C1-3, en donde cada uno de carbociclilo y heterociclilo puede estar opcionalmente sustituido con uno o más alquilo C1-4, arilo o aril-alquil C1-3-, y en donde en cada uno de carbociclilo y heterociclilo un grupo CH2 puede estar opcionalmente reemplazado por -C(=O)-, y en donde cada uno de alquilo, carbociclilo y heterociclilo puede estar opcionalmente sustituido con uno o más sustituyentes RC, y en donde cada grupo arilo y heteroarilo puede estar opcionalmente sustituido con uno o más sustituyentes L; RN2 se selecciona entre el grupo RN2-G1 que consiste en H y alquilo C1-6; y RAlk se selecciona entre el grupo RAlk-G1 que consiste en H y alquilo C1-6, que puede estar sustituido con uno o más átomos de F; y Ar2 se selecciona del grupo Ar2-G1 que consiste en fenilo y un sistema de anillos carbocíclico monocíclico aromático de 5 ó 6 miembros, que contiene 1, 2 ó 3 heteroátomos seleccionados de N, O ó S, en donde la totalidad de los grupos antes mencionados puede estar opcionalmente sustituido con uno o más sustituyentes L; y L se selecciona del grupo L-G1 que consiste en F, Cl, Br, CN, OH, alquilo C1-4-, alquil C1-4-O-, alquil C1-4-S-, alquil C1-4-S(=O)2-, alquil C1-4-NRN2-S(=O)2, H2N-, (alquil C1-4)NH-, (alquil C1-4)2N-, H2N-alquil C1-4, (alquil C1-4)NH-alquil C1-4-, (alquil C1-4-)2N-alquil C1-4-, cicloalquil C3-7-, cicloalquil C3-7-alquil C1-3-O- y heterociclilo, en donde cada uno de alquilo puede estar opcionalmente sustituido con uno o más átomos de F y/o con un sustituyente seleccionado de OH, alquil C1-3-O- y CN; y en donde dos sustituyentes L fijados a un grupo arilo o heteroarilo pueden estar enlazados uno con otro y forman un grupo de puenteo de alquileno C2-5, en el que 1 ó 2 grupos -CH2 pueden estar reemplazados por un grupo seleccionado, independientemente uno de otro, de O, S, NH y N(alquilo C1-4)-, en donde el grupo de puenteo de alquileno C2-5 está opcionalmente sustituido con 1 ó 2 grupos alquilo C1-3; X se selecciona del grupo X-G1 que consiste en un grupo alquileno C1-3 de cadena lineal que puede estar sustituido opcionalmente con uno o más alquilo C1-3 y alquil C1-3-O-alquilo C1-3, y en donde dos sustituyentes alquilo pueden estar conectados uno con otro y juntos forman un grupo de puenteo de alquileno C1-5 en el que 1 ó 2 grupos -CH2 pueden estar reemplazados por un grupo seleccionado, independientemente uno de otro, de O, S, NH o N(alquilo C1-4)-, en donde el grupo de puenteo de alquileno C1-5 está opcionalmente sustituido con 1 ó 2 grupos alquilo C1-3; e Y se selecciona del grupo Y-G1 que consiste en -C(=O)-, -C(=S)- y S(=O)2-; RN se selecciona entre el grupo RN-G1 que consiste en H y alquilo C1-3; T se selecciona del grupo T-G1 que consiste en alquilo C1-6, alquenilo C2-6, alquinilo C2-6, carbociclilo C3-10, carbociclil C3-10-alquil C1-3-, alquil C1-6-O-, carbociclil C3-10-O-, carbociclil C3-10-alquil C1-3-O-, alquil C1-6-S-, carbociclil C3-10-S-, carbociclil C3-10-alquil C1-3-S-, alquil C1-4-C(=O)-, alquil C1-4-S(=O)2-, RN1RN2-N, RN1RN2-N-alquil C1-3-, RN1RN2-N-CO, alquil C1-4-C(=O)-RN2N-alquil C1-3-, alquil C1-3-O-N=CH-, alquil C1-4-OC(=O)-RN2N-alquil C1-3-, heterociclilo, arilo, heteroarilo y heteroaril-alquil C1-3-, en donde en cada carbociclilo y heterociclilo un grupo CH2 puede estar opcionalmente reemplazado por -C(=O)-, y en donde cada carbociclilo y heterociclilo puede estar opcionalmente sustituido con uno o más alquilo C1-4 que puede estar opcionalmente sustituido con uno o más sustituyentes RC, y en donde cada uno de alquilo, carbociclilo y heterociclilo puede estar opcionalmente sustituido con uno o más sustituyentes RC, y en donde cada grupo arilo y heteroarilo puede estar opcionalmente sustituido con uno o más sustituyentes L, o los grupos T y RN pueden estar conectados uno con otro y juntos forman un grupo que se selecciona del grupo (T-RN)-G1 que consiste en alquileno C2-5 que puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados de F, Cl, Br, OH, CN, alquilo C1-4, carbociclilo C3-10, carbociclil C3-10-alquilo C1-3, alquil C1-4-O-, cicloalquil C3-7-O-, carbociclil C3-10-alquil C1-3-O-, H2N-, (alquil C1-4)NH-, (alquil C1-4)2N-, alquil C1-4-C(=O)-, alquil C1-4-S(=O)2-, HO-C(=O)-, alquil C1-4-O-C(=O)-, en donde cada uno de alquilo o carbociclilo puede estar opcionalmente sustituido con uno o más sustituyentes seleccionados de RC; incluyendo cualquier tautómero y estereoisómero de los mismos, o una sal de los mismos.
ARP110102362A 2010-07-01 2011-06-30 Derivados de piperidina y su uso para el tratamiento de desordenes metabolicos AR082844A1 (es)

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KR (1) KR20130113352A (es)
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US20120157425A1 (en) 2012-06-21
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