AR086554A1 - Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina - Google Patents

Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina

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Publication number
AR086554A1
AR086554A1 ARP120101842A ARP120101842A AR086554A1 AR 086554 A1 AR086554 A1 AR 086554A1 AR P120101842 A ARP120101842 A AR P120101842A AR P120101842 A ARP120101842 A AR P120101842A AR 086554 A1 AR086554 A1 AR 086554A1
Authority
AR
Argentina
Prior art keywords
alkyl
cra1ra2
membered
hydrogen
independently selected
Prior art date
Application number
ARP120101842A
Other languages
English (en)
Inventor
Ameer Vijay Ambarkhane
Gurdip Bhalay
Martin Beckett
James Dale
Ahmed Hamadi
Alessandro Mazzacani
Jeffrey Mkenna
Christopher Thompson
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46317469&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR086554(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR086554A1 publication Critical patent/AR086554A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/435—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
    • 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
    • A61K31/435—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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • C07D487/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nutrition Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Procedimientos para la preparación de tales derivados, composiciones farmacéuticas que comprenden tales derivados, tales derivados como un medicamento, tales derivados para el tratamiento de un trastorno o una enfermedad mediada por el receptor de la ghrelina.Reivindicación 1: Un compuesto de la fórmula (1), en donde - - - - - es un enlace sencillo o un enlace doble; X1 es (CRx1H)n y X2 es (CH); ó X1 es (CRx1H)n y X2 es N; ó X1 es NRx1 y X2 es (CH); ó X1 es NRx1 y X2 es N; ó X1 es N y X2 es C; en donde el enlace entre X1 y X2 es un enlace doble si X1 es N y X2 es C; n es 0 ó 1; Rx1 se selecciona a partir de hidrógeno y alquilo C1-6; m es 1 y p es 0; ó m es 1 y p es 1;ó m es 2 y p es 1; Y es NR1 u O; R1 se selecciona a partir de hidrógeno, alquilo C1-6, -alquil C1-4C(O)NR1aR1b, -alquil C1-4C(O)O-alquilo C1-4, -alquil C1-4C(O)O-haloalquilo C1-4, haloalquilo C1-6, cicloalquilo C3-6, -alquil C1-4-heteroarilo de 5 - 6 miembros, hidroxialquilo C1-6, alcoxilo C1-6 y alcoxi C1-4-alquilo C1-4; en donde el heteroarilo de 5 - 6 miembros es sustituido o no sustituido por 1 a 3 sustituyentes independientemente seleccionados a partir de halógeno y alquilo C1-6; R1a y R1b son independientemente seleccionados a partir de hidrógeno, alquilo C1-6 y haloalquilo C1-6; ó R1a y R1b junto con el nitrógeno al cual se fijan forman un anillo heterocíclico de 4 - 6 miembros que contiene 0, 1 ó 2 heteroátomos adicionales seleccionados a partir de oxígeno, nitrógeno y azufre; R2a se selecciona a partir de (i) -A-fenilo; (ii) -A-heteroarilo de 5 - 6 miembros; (iii) -A-heterociclilo de 4 - 6 miembros; (iv) -A-cicloalquilo C5-6; (v) -D-sistema de anillo bicíclico condensado de 8 - 10 miembros; en donde el fenilo, heteroarilo de 5 - 6 miembros, heterociclilo de 4 - 6 miembros, cicloalquilo C5-6 y sistema de anillo bicíclico condensado de 8 - 10 miembros son sustituidos o no sustituidos por 1 a 3 sustituyentes independientemente seleccionados a partir de halógeno, hidroxilo, alquilo C1-6, alcoxilo C1-6 y haloalquilo C1-6; A se selecciona a partir de un enlace, -(CRA1RA2), -(CRA1RA2)(CRA1RA2), -(CRA1RA2)-O-, -O-(CRA1RA2), -(CRA1RA2)-S-, -(CRA1RA2)-S(O)-, -(CRA1RA2)-S(O)2-, -S-(CRA1RA2)-, -S(O)-(CRA1RA2)-, -S(O)2-(CRA1RA2)-, -NRA3-(CRA1RA2), -(CRA1RA2)-NRA3- y -(CRA1)=(CRA1)-; D es un enlace, -O- ó -(CRD1RD2)-; RA1, RA2 y RA3 son independientemente seleccionados a partir de hidrógeno, alquilo C1-6 y halógeno; RD1 y RD2 son independientemente seleccionados a partir de hidrógeno, alquilo C1-6 y halógeno; R2b es hidrógeno ó alquilo C1-4; R3 y R4 son independientemente seleccionados a partir de hidrógeno, alquilo C1-6 y cicloalquilo C3-6; ó R3 y R4 junto con el nitrógeno al cual se fijan forman un anillo heterocíclico de 4 - 6 miembros que contiene 0, 1 ó 2 heteroátomos adicionales seleccionados a partir de oxígeno, nitrógeno y azufre; tal anillo heterocíclico de 4 - 6 miembros es sustituido o no sustituido por 1 ó 2 sustituyentes de halógeno; R6 y R7 son independientemente seleccionados a partir de hidrógeno, alquilo C1-6, hidroxialquilo C1-6 y haloalquilo C1-6; R5 se selecciona a partir de fenilo, un heteroarilo de 5 - 6 miembros, cicloalquilo C3-6 y heterociclilo de 4 - 6 miembros; tal fenilo, heteroarilo de 5 - 6 miembros, cicloalquilo C3-6 y heterociclilo de 4 - 6 miembros es sustituido o no sustituido por 1 a 3 sustituyentes independientemente seleccionados a partir de halógeno, alquilo C1-6, alcoxilo C1-6 y haloalquilo C1-6; o una sal farmacéuticamente aceptable de los mismos.
ARP120101842A 2011-05-27 2012-05-24 Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina AR086554A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161490848P 2011-05-27 2011-05-27
US201161560960P 2011-11-17 2011-11-17
US201261642116P 2012-05-03 2012-05-03

Publications (1)

Publication Number Publication Date
AR086554A1 true AR086554A1 (es) 2014-01-08

Family

ID=46317469

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120101842A AR086554A1 (es) 2011-05-27 2012-05-24 Derivados de la piperidina 3-espirociclica como agonistas de receptores de la ghrelina

Country Status (21)

Country Link
US (2) US8546416B2 (es)
EP (1) EP2714690A1 (es)
JP (1) JP2014515369A (es)
KR (1) KR20140023399A (es)
CN (1) CN103562206A (es)
AP (1) AP2013007234A0 (es)
AR (1) AR086554A1 (es)
AU (1) AU2012264305A1 (es)
BR (1) BR112013030391A2 (es)
CA (1) CA2835916A1 (es)
CL (1) CL2013003211A1 (es)
CO (1) CO6811856A2 (es)
CR (1) CR20130625A (es)
EA (1) EA201391797A1 (es)
IL (1) IL229320A0 (es)
MX (1) MX355072B (es)
PE (1) PE20140610A1 (es)
SG (1) SG194616A1 (es)
TW (1) TW201302749A (es)
UY (1) UY34094A (es)
WO (1) WO2012164473A1 (es)

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UY34094A (es) 2013-01-03
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US20130331369A1 (en) 2013-12-12
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