MX2016012624A - Derivados de 5-oxa-2-azabiciclo[2.2.2]octan-4-ilo y 5-oxa-2-azabiciclo[2.2.1]heptan-4-ilo como modularores de los receptores asociados a la amina de trazas 1 (taar1). - Google Patents

Derivados de 5-oxa-2-azabiciclo[2.2.2]octan-4-ilo y 5-oxa-2-azabiciclo[2.2.1]heptan-4-ilo como modularores de los receptores asociados a la amina de trazas 1 (taar1).

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Publication number
MX2016012624A
MX2016012624A MX2016012624A MX2016012624A MX2016012624A MX 2016012624 A MX2016012624 A MX 2016012624A MX 2016012624 A MX2016012624 A MX 2016012624A MX 2016012624 A MX2016012624 A MX 2016012624A MX 2016012624 A MX2016012624 A MX 2016012624A
Authority
MX
Mexico
Prior art keywords
disorders
halogen
azabicyclo
oxa
lower alkoxy
Prior art date
Application number
MX2016012624A
Other languages
English (en)
Inventor
Galley Guido
Norcross Roger
Pflieger Philippe
Shen Hong
Hu Yimin
Cecere Giuseppe
Original Assignee
F Hoffman-La Roche 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
Application filed by F Hoffman-La Roche Ag filed Critical F Hoffman-La Roche Ag
Publication of MX2016012624A publication Critical patent/MX2016012624A/es

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    • 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
    • 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

Abstract

La presente invención se refiere a los compuestos de la fórmula (I) en donde ----C----- es -CH2- o -CH2-CH2-; X es -NH-, -C(O)NH- o -NHC(O)NH-; Ar es fenilo o un grupo heteroarilo de 5 o 6 elementos que contiene uno o dos átomos de N; R1 es halógeno, alquilo inferior, alquilo inferior sustituido por halógeno, alcoxi inferior, alcoxi inferior sustituido por cicloalquilo, alcoxi inferior sustituido por halógeno o es cicloalquilo; -( )- es -CH2-; n es 0 o 1; m es 0, 1 o 2; o una sal de adición ácida farmacéuticamente adecuada del mismo, todas las mezclas racémicas, todos sus enantiómeros y/o isómeros ópticos correspondientes, tales compuestos pueden ser utilizados para el tratamiento de la depresión, trastornos de ansiedad, trastorno bipolar, trastorno de déficit de atención con hiperactividad (ADHD), trastornos relacionados con el estrés, trastornos psicóticos, esquizofrenia, enfermedades neurológicas, enfermedad de Parkinson, enfermedades neurodegenerativas, enfermedad de Alzheimer, epilepsia, migraña, hipertensión, abuso de sustancias, trastornos metabólicos, trastornos de la alimentación, diabetes, complicaciones de la diabetes, obesidad, dislipidemia, trastornos de consumo y asimilación de energía, trastornos y el mal funcionamiento de la homeostasis de la temperatura corporal, trastornos del sueño y del ritmo circadiano, y trastornos cardiovasculares.
MX2016012624A 2014-05-28 2015-05-22 Derivados de 5-oxa-2-azabiciclo[2.2.2]octan-4-ilo y 5-oxa-2-azabiciclo[2.2.1]heptan-4-ilo como modularores de los receptores asociados a la amina de trazas 1 (taar1). MX2016012624A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2014078644 2014-05-28
PCT/EP2015/061348 WO2015181061A1 (en) 2014-05-28 2015-05-22 5-oxa-2-azabicyclo[2.2.2]octan-4-yl and 5-oxa-2-azabicyclo[2.2.1]heptan-4-yl derivatives as taar1 modulators

Publications (1)

Publication Number Publication Date
MX2016012624A true MX2016012624A (es) 2016-12-14

Family

ID=53267355

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016012624A MX2016012624A (es) 2014-05-28 2015-05-22 Derivados de 5-oxa-2-azabiciclo[2.2.2]octan-4-ilo y 5-oxa-2-azabiciclo[2.2.1]heptan-4-ilo como modularores de los receptores asociados a la amina de trazas 1 (taar1).

Country Status (19)

Country Link
US (1) US9663530B2 (es)
EP (1) EP3149002B1 (es)
JP (1) JP6275870B2 (es)
KR (1) KR101880841B1 (es)
CN (1) CN106459073B (es)
CA (1) CA2943889A1 (es)
DK (1) DK3149002T3 (es)
ES (1) ES2674800T3 (es)
HR (1) HRP20180933T1 (es)
HU (1) HUE039262T2 (es)
LT (1) LT3149002T (es)
MX (1) MX2016012624A (es)
PL (1) PL3149002T3 (es)
PT (1) PT3149002T (es)
RS (1) RS57341B1 (es)
RU (1) RU2016149984A (es)
SI (1) SI3149002T1 (es)
TR (1) TR201808506T4 (es)
WO (1) WO2015181061A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016015333A1 (en) * 2014-08-01 2016-02-04 F.Hoffmann-La Roche Ag 2-oxa-5-azabicyclo [2.2.1] heptan-3-yl derivatives
MA53755A (fr) 2016-03-17 2021-08-04 Hoffmann La Roche Dérivé de 5-éthyl-4-méthyl-pyrazole-3-carboxamide ayant une activité comme agonist de taar
EP3463359A4 (en) * 2016-06-02 2020-08-26 Purdue Pharma LP SPURENAMINE-ASSOCIATED RECEPTOR-1 AGONISTS AND PARTIAL AGONISTS FOR PAIN MANAGEMENT

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0206033D0 (en) * 2002-03-14 2002-04-24 Pfizer Ltd Compounds useful in therapy
WO2009019149A1 (en) * 2007-08-03 2009-02-12 F. Hoffmann-La Roche Ag Pyridinecarboxamide and benzamide derivatives as taar1 ligands
US9452980B2 (en) * 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
US8802673B2 (en) * 2011-03-24 2014-08-12 Hoffmann-La Roche Inc Heterocyclic amine derivatives
US9029370B2 (en) * 2011-06-10 2015-05-12 Hoffmann-La Roche Inc. Substituted benzamide derivatives
US20130310340A1 (en) * 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
EP2917211A1 (en) * 2012-11-07 2015-09-16 F. Hoffmann-La Roche AG Pyrazine derivatives

Also Published As

Publication number Publication date
PT3149002T (pt) 2018-06-18
EP3149002B1 (en) 2018-04-25
RS57341B1 (sr) 2018-08-31
HUE039262T2 (hu) 2018-12-28
WO2015181061A1 (en) 2015-12-03
KR101880841B1 (ko) 2018-07-20
US9663530B2 (en) 2017-05-30
JP2017511345A (ja) 2017-04-20
HRP20180933T1 (hr) 2018-07-27
CN106459073A (zh) 2017-02-22
RU2016149984A3 (es) 2018-11-12
CN106459073B (zh) 2018-11-13
ES2674800T3 (es) 2018-07-04
JP6275870B2 (ja) 2018-02-07
RU2016149984A (ru) 2018-07-02
DK3149002T3 (en) 2018-07-02
PL3149002T3 (pl) 2018-08-31
TR201808506T4 (tr) 2018-07-23
LT3149002T (lt) 2018-07-10
US20170066775A1 (en) 2017-03-09
KR20160146985A (ko) 2016-12-21
CA2943889A1 (en) 2015-12-03
SI3149002T1 (en) 2018-08-31
EP3149002A1 (en) 2017-04-05

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