MX378486B - Derivados de 2-oxa-5-azabiciclo[2.2.1]heptan-3-ilo. - Google Patents

Derivados de 2-oxa-5-azabiciclo[2.2.1]heptan-3-ilo.

Info

Publication number
MX378486B
MX378486B MX2017001096A MX2017001096A MX378486B MX 378486 B MX378486 B MX 378486B MX 2017001096 A MX2017001096 A MX 2017001096A MX 2017001096 A MX2017001096 A MX 2017001096A MX 378486 B MX378486 B MX 378486B
Authority
MX
Mexico
Prior art keywords
disorders
sub
halogen
lower alkoxy
lower alkyl
Prior art date
Application number
MX2017001096A
Other languages
English (en)
Other versions
MX2017001096A (es
Inventor
Giuseppe Cecere
Guido Galley
Hong Shen
Philippe Pflieger
Roger Norcross
Yimin Hu
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MX2017001096A publication Critical patent/MX2017001096A/es
Publication of MX378486B publication Critical patent/MX378486B/es

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    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen 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
    • A61K31/40—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
    • 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
    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • 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
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • 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
    • 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
    • C07D491/06—Peri-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

La presente invención se refiere a compuestos de fórmula (ver Fórmula) en la que L es un enlace, -C(O)NH-, -NHC(O)-, -CH2NHC(O)-, CH2C(O)NH-, -CH2NH-, -NH- o -NHC (O) NH-; R1 es hidrógeno, alquilo inferior, halógeno, alcoxi inferior-alquilo, alcoxi inferior sustituido con halógeno, alquilo inferior sustituido con halógeno o es fenilo o heteroarilo seleccionado entre el grupo que consiste en piridinilo, pirimidinilo, pirazinilo o pirazolilo, y en el que el fenilo y el heteroarilo están opcionalmente sustituidos con uno, dos o tres sustituyentes seleccionados entre el grupo que consiste en halógeno, alquilo inferior, alcoxi inferior, alquilo inferior sustituido con halógeno, alcoxi inferior sustituido con halógeno, cicloalquilo o O-CH2- cicloalquilo; o a una sal de adición de ácidos farmacéuticamente aceptable de los mismos, a todas las mezclas racémicas, a todos sus enantiómeros correspondientes y/o isómeros ópticos, que puede usarse para el tratamiento de la depresión, trastornos de ansiedad, trastorno bipolar, trastorno de déficit de atención e hiperactividad (TDAH), trastornos relacionados con el estrés, trastornos psicóticos, esquizofrenia, enfermedades neurológicas, enfermedad de Parkinson, trastornos neurodegenerativos, enfermedad de Alzheimer, epilepsia, migraña, hipertensión, abuso de sustancias, trastornos metabólicos, trastornos alimentarios, diabetes, complicaciones diabéticas, obesidad, dislipidemia, trastornos de consumo y asimilación de energía, trastornos de mal funcionamiento de la homeostasis de la temperatura corporal, trastornos del sueño y del ritmo circadiano, y trastornos cardiovasculares.
MX2017001096A 2014-08-01 2015-07-29 Derivados de 2-oxa-5-azabiciclo[2.2.1]heptan-3-ilo. MX378486B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
PCT/CN2014/083549 WO2016015333A1 (en) 2014-08-01 2014-08-01 2-oxa-5-azabicyclo [2.2.1] heptan-3-yl derivatives
PCT/EP2015/067353 WO2016016292A1 (en) 2014-08-01 2015-07-29 2-oxa-5-azabicyclo[2.2.1]heptan-3-yl derivatives

Publications (2)

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MX2017001096A MX2017001096A (es) 2017-04-27
MX378486B true MX378486B (es) 2025-03-11

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Country Status (11)

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US (1) US9790230B2 (es)
EP (1) EP3174886B1 (es)
JP (1) JP6364121B2 (es)
KR (1) KR101911651B1 (es)
CN (1) CN106661043B (es)
AR (1) AR101359A1 (es)
CA (1) CA2954209C (es)
MX (1) MX378486B (es)
RU (1) RU2697651C2 (es)
TW (1) TWI583687B (es)
WO (2) WO2016015333A1 (es)

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MY195528A (en) * 2016-03-17 2023-01-30 Hoffmann La Roche 5-Ethyl-4-Methyl-Pyrazole-3-Carboxamide Derivative Having Activity as Agonist of Taar
EP3463359A4 (en) * 2016-06-02 2020-08-26 Purdue Pharma LP TRACE AMINE RECEPTOR 1 AGONISTS AND PARTIAL PAIN AGONISTS
CN106187911A (zh) * 2016-07-04 2016-12-07 烟台凯博医药科技有限公司 2‑三氟甲基嘧啶‑4‑羧酸及其衍生物和制备方法
EP3621951A4 (en) * 2017-05-12 2021-01-27 Research Triangle Institute DIARYL URINE AS CB1 ALLOSTERIC MODULATORS
WO2022087630A1 (en) * 2020-10-23 2022-04-28 Icahn School Of Medicine At Mount Sinai Inhibitors of amino acid transport
CN114874143A (zh) * 2021-02-05 2022-08-09 上海翰森生物医药科技有限公司 含吡唑类衍生物调节剂、其制备方法和应用
WO2023033681A1 (en) 2021-09-01 2023-03-09 Limited Liability Company «Excellena Research And Development» (Llc «Excellena») Substituted 2-(5-aryl-4 h-1,2,4-triazol-3-yl)ethanamines as modulators of trace amine-associated receptor 1 (taar1)
WO2023033679A1 (en) * 2021-09-01 2023-03-09 Limited Liability Company «Excellena Research And Development» (Llc «Excellena») (azacycloalkyl)methoxy-substituted benzamides as modulators of trace amine-associated receptor 1 (taar1)
WO2023033680A1 (en) 2021-09-01 2023-03-09 Limited Liability Company «Excellena Research And Development» (Llc «Excellena») Substituted 2,3,4,5-tetrahydrobenzo[ f][1,4]oxazepines as modulators of trace amine-associated receptor 1 (taar1)
EP4428128A4 (en) * 2021-11-04 2026-01-07 Shanghai Hansoh Biomedical Co Ltd 2-(ARYL-2-YL)MORPHOLINE AND DEUTERATED DERIVATIVE THEREOF, ITS PREPARATION PROCESS AND ITS APPLICATION
EP4479404A1 (en) 2022-02-16 2024-12-25 Awakn Ls Europe Holdings Limited Bridged ring compounds and their therapeutic use as cns agents

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DE3431257A1 (de) * 1984-08-24 1986-03-06 Bayer Ag, 5090 Leverkusen Neue (delta)-butyrolactame, pharmakologisch aktive zusammensetzungen derselben, verfahren zu ihrer herstellung und ihre medizinische verwendung
CN1012172B (zh) * 1984-08-24 1991-03-27 北京医学科学院药物研究所 新型黄皮酰胺类化合物的分离和提取方法
DE3927369A1 (de) * 1989-08-19 1991-02-21 Bayer Ag Substituierte n-(chinolin-2-yl-methoxy)benzyl-sulfonyl-harnstoffe
FR2912404B1 (fr) * 2007-02-09 2009-04-10 Sanofi Aventis Sa Derives d'azabicycloalkane,leur preparation et leur application en therapeutique.
US9452980B2 (en) * 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
WO2014072257A1 (en) * 2012-11-07 2014-05-15 F. Hoffmann-La Roche Ag Pyrazine derivatives
KR101880841B1 (ko) * 2014-05-28 2018-07-20 에프. 호프만-라 로슈 아게 미량 아민 결합 수용체 1(taar1) 조절제로서 5-옥사-2-아자바이사이클로[2.2.2]옥탄-4-일 및 5-옥사-2-아자바이사이클로[2.2.1]헵탄-4-일 유도체

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TWI583687B (zh) 2017-05-21
BR112016028714A2 (pt) 2017-08-22
RU2017104264A (ru) 2018-09-04
CA2954209C (en) 2022-08-30
RU2017104264A3 (es) 2019-02-27
WO2016015333A1 (en) 2016-02-04
EP3174886A1 (en) 2017-06-07
CN106661043B (zh) 2020-01-17
AR101359A1 (es) 2016-12-14
CA2954209A1 (en) 2016-02-04
WO2016016292A1 (en) 2016-02-04
US20170137435A1 (en) 2017-05-18
EP3174886B1 (en) 2021-02-17
KR101911651B1 (ko) 2018-10-24
CN106661043A (zh) 2017-05-10
JP2017522353A (ja) 2017-08-10
US9790230B2 (en) 2017-10-17
JP6364121B2 (ja) 2018-07-25
RU2697651C2 (ru) 2019-08-16
MX2017001096A (es) 2017-04-27
KR20170021352A (ko) 2017-02-27
TW201617349A (zh) 2016-05-16

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