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1. WO2016016292 - 2-OXA-5-AZABICYCLO[2.2.1]HEPTAN-3-YL DERIVATIVES

Publication Number WO/2016/016292
Publication Date 04.02.2016
International Application No. PCT/EP2015/067353
International Filing Date 29.07.2015
IPC
C07D 491/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic 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/-C07D459/290
02in which the condensed system contains two hetero rings
06Peri-condensed systems
A61K 31/35 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
35having six-membered rings with one oxygen as the only ring hetero atom
A61K 31/407 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
407condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61P 25/28 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for 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
CPC
A61K 31/35
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
35having six-membered rings with one oxygen as the only ring hetero atom
A61K 31/407
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
407condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/46
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
468-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
A61K 31/5386
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5386spiro-condensed or forming part of bridged ring systems
A61P 1/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH]/[CH] (AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BE, BF, BG, BH, BJ, BN, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CL, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IR, IS, IT, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, ME, MG, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SI, SK, SL, SM, SN, ST, SV, SY, SZ, TD, TG, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, ZA, ZM, ZW)
  • HOFFMANN-LA ROCHE INC. [US]/[US] (US)
Inventors
  • CECERE, Giuseppe
  • GALLEY, Guido
  • HU, Yimin
  • NORCROSS, Roger
  • PFLIEGER, Philippe
  • SHEN, Hong
Agents
  • POPPE, Regina
Priority Data
PCT/CN2014/08354901.08.2014CN
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 2-OXA-5-AZABICYCLO[2.2.1]HEPTAN-3-YL DERIVATIVES
(FR) DÉRIVÉS DU 2-OXA -5-AZABICYCLO [2.2.1] HEPTAN -3-YL
Abstract
(EN)
The present invention relates to compounds of formula (I), wherein L is a bond, -C(O)NH-, -NHC(O)-, -CH2NHC(O)-, CH2C(O)NH-, -CH2NH-, -NH- or -NHC(O)NH-; R1 is hydrogen, lower alkyl, halogen, lower alkoxy-alkyl, lower alkoxy substituted by halogen, lower alkyl substituted by halogen or is phenyl or heteroaryl selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl or pyrazolyl, and wherein phenyl and heteroaryl are optionally substituted by one, two or three substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cycloalkyl or O-CH2-cycloalkyl; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
(FR)
La présente invention concerne des composés de formule (I), dans laquelle L est une liaison, -C (O) NH -, -NHC (O) -, -CH2NHC(O)-, CH2C(O)NH-, -CH2NH-, -NH-ou-NHC (O) NH -; R1 est hydrogène, alkyle inférieur, halogène, alcoxy-alkyle inférieur, alcoxy inférieur substitué par halogène, alkyle inférieur substitué par halogène ou est un groupe phényle ou hétéroaryle choisi dans le groupe constitué par pyridinyle, pyrimidinyle, pyrazinyle ou pyrazolyle, et dans laquelle le phényle et l'hétéroaryle sont éventuellement substitués par un, deux ou trois substituants choisis dans le groupe constitué par un atome d'halogène, alkyle inférieur, alcoxy inférieur, alkyle inférieur substitué par halogène, alcoxy inférieur substitué par halogène, cycloalkyle ou O-CH2-cycloalkyle ; ou son sel d'addition d'acide pharmaceutiquement approprié, tous les mélanges racémiques, tous leurs énantiomères et/ou isomères optiques correspondants, qui peuvent être utilisés pour le traitement de la dépression, des troubles de l'anxiété, du trouble bipolaire, du trouble d'hyperactivité avec déficit de l'attention (ADHD), des troubles liés au stress, des troubles psychotiques, de la schizophrénie, des maladies neurologiques, de la maladie de Parkinson, des troubles neurodégénératifs, de la maladie d'Alzheimer, de l'épilepsie, de la migraine, de l'hypertension, de l'abus de substances psychoactives, des troubles métaboliques, des troubles de l'alimentation, du diabète, des complications diabétiques, de l'obésité, de la dyslipidémie, des troubles de consommation et d'assimilation d'énergie, des troubles et dysfonctionnements de l'homéostasie de la température corporelle, des troubles du sommeil et du rythme circadien et des troubles cardiovasculaires.
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