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AR120404A1 - CARBOXAMIDAS HETEROCÍCLICAS SUSTITUIDAS COMO ANTAGONISTAS DE LOS RECEPTORES a₂C ADRENÉRGICOS - Google Patents

CARBOXAMIDAS HETEROCÍCLICAS SUSTITUIDAS COMO ANTAGONISTAS DE LOS RECEPTORES a₂C ADRENÉRGICOS

Info

Publication number
AR120404A1
AR120404A1 ARP200103077A ARP200103077A AR120404A1 AR 120404 A1 AR120404 A1 AR 120404A1 AR P200103077 A ARP200103077 A AR P200103077A AR P200103077 A ARP200103077 A AR P200103077A AR 120404 A1 AR120404 A1 AR 120404A1
Authority
AR
Argentina
Prior art keywords
halogen
substituted
alkyl
alkoxy
cycloalkyl
Prior art date
Application number
ARP200103077A
Other languages
English (en)
Inventor
Martina Delbeck
Michael Hahn
Thomas Mller
Lisa Dietz
Magdalena Platzk
Daniel Meibom
Original Assignee
Bayer Ag
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Filing date
Publication date
Application filed by Bayer Ag filed Critical Bayer Ag
Publication of AR120404A1 publication Critical patent/AR120404A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P25/08—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
    • 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
    • A61P25/24—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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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 three or more hetero rings
    • 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Carboxamidas heterocíclicas que poseen actividad antagonista de los receptores a₂C adrenérgicos, medicamentos que los contienen y el uso de los mismos en el tratamiento o prevención de trastornos respiratorios, de enfermedades vasculares y de desórdenes del sistema nervioso central o periférico. Reivindicación 1: Compuestos de la fórmula general (1) en donde X representa S, N u O; Y representa N, S u O, en donde, cuando X es igual a S, entonces Y es igual a N; en donde, cuando X es igual a O, entonces Y es igual a N; Z representa CR⁴, O ó NR⁴, en donde, cuando X es igual a N e Y es igual a N, entonces Z es igual a O; en donde, cuando X es igual a S, entonces Z es igual a CR⁴ o NR⁴, R¹ representa heteroarilo de 5 ó 6 miembros, fenilo, en donde heteroarilo de 5 a 6 miembros puede estar sustituido con 1 a 2 sustituyentes independientemente entre sí seleccionados del grupo alquilo C₁₋₄, alcoxi C₁₋₄, halógeno; en donde alquilo C₁₋₄ puede estar sustituido hasta tres veces con halógeno, en donde alcoxi C₁₋₄ puede estar sustituido hasta tres veces con halógeno, en donde fenilo puede estar sustituido con 1 a 2 sustituyentes independientemente entre sí seleccionados del grupo alquilo C₁₋₄, cicloalquilo C₃₋₅, alcoxi C₁₋₄, ciano, hidroxi, halógeno; en donde alquilo C₁₋₄ puede estar sustituido hasta tres veces con halógeno, R² representa hidrógeno, alquilo C₁₋₄; en donde alquilo C₁₋₄ puede estar sustituido hasta tres veces con halógeno, o junto al átomo de carbono al que está unido R², forma un anillo cicloalquilo C₃₋₄, R³ representa hidrógeno, alquilo C₁₋₄, en donde alquilo C₁₋₄ puede estar sustituido hasta tres veces con halógeno, R⁴ en CR⁴ representa hidrógeno, alquilo C₁₋₄, cicloalquilo C₃₋₄, fenilo, halógeno; en donde alquilo C₁₋₄ puede estar sustituido hasta tres veces con halógeno y fenilo con halógeno, en NR⁴ representa hidrógeno, alquilo C₁₋₄, cicloalquilo C₃₋₄, fenilo; en donde alquilo C₁₋₄ puede estar sustituido hasta tres veces con halógeno y fenilo con halógeno, R⁵ representa hidrógeno, alquilo C₁₋₄, alcoxi C₁₋₄, halógeno, R⁶ representa uno de los grupos de las fórmulas a), b), c), d), e), f) o g) del grupo de fórmulas (2) en donde *** marca la unión con el anillo de piperidina adyacente, en donde R⁷ representa hidrógeno, alquilo C₁₋₄, cicloalquilo C₃₋₄, alcoxi C₁₋₄, cicloalcoxi C₃₋₄, fenilo, en donde alquilo C₁₋₄ puede estar sustituido con cicloalquilo C₃₋₄, alcoxi C₁₋₄, cicloalcoxi C₃₋₄ y puede estar sustituido hasta tres veces con halógeno, en donde alcoxi C₁₋₄ puede estar sustituido con cicloalquilo C₃₋₄ y puede estar sustituido hasta tres veces con halógeno, en donde cicloalquilo C₃₋₄ puede estar sustituido con monofluorometilo, difluorometilo o trifluorometilo y puede estar sustituido hasta dos veces con halógeno, en donde alcoxi C₁₋₄ puede estar sustituido con cicloalquilo C₃₋₄ y puede estar sustituido hasta tres veces con halógeno, en donde cicloalquilo C₃₋₄ puede estar sustituido una vez o dos veces con halógeno, en donde cicloalcoxi C₃₋₄ puede estar sustituido hasta dos veces con halógeno, en donde R⁸ representa hidrógeno o flúor, en donde R⁹ representa hidrógeno, alquilo C₁₋₄, alcoxi C₁₋₄, halógeno; en donde alquilo C₁₋₄ puede estar sustituido con alcoxi C₁₋₄, n representa 0 ó 1, m representa 0, 1 ó 2, p representa 0, 1 ó 2 y q representa 0, 1 ó 2, así como sus sales, solvatos y solvatos de las sales.
ARP200103077A 2019-11-06 2020-11-05 CARBOXAMIDAS HETEROCÍCLICAS SUSTITUIDAS COMO ANTAGONISTAS DE LOS RECEPTORES a₂C ADRENÉRGICOS AR120404A1 (es)

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EP19207536 2019-11-06

Publications (1)

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AR120404A1 true AR120404A1 (es) 2022-02-09

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EP (1) EP4021905A1 (es)
JP (1) JP7748938B2 (es)
KR (1) KR20220098160A (es)
CN (4) CN114929694B (es)
AR (1) AR120404A1 (es)
AU (1) AU2020377470A1 (es)
BR (1) BR112022008146A2 (es)
CA (1) CA3160035A1 (es)
CO (1) CO2022005783A2 (es)
CR (1) CR20220195A (es)
DO (1) DOP2022000093A (es)
EC (1) ECSP22035103A (es)
GE (2) GEP20247644B (es)
IL (1) IL292656A (es)
JO (1) JOP20220102A1 (es)
MX (1) MX2022005414A (es)
PE (1) PE20221025A1 (es)
PH (1) PH12022551097A1 (es)
SA (1) SA522432419B1 (es)
TW (1) TWI867088B (es)
WO (1) WO2021089683A1 (es)

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CN118434414A (zh) 2021-12-22 2024-08-02 拜耳公司 用于治疗睡眠呼吸暂停的α2-肾上腺素受体亚型C（α-2C）拮抗剂与毒蕈碱受体拮抗剂的结合物
KR20240124995A (ko) 2021-12-22 2024-08-19 바이엘 악티엔게젤샤프트 수면 무호흡의 치료를 위한 a2-아드레날린수용체 하위유형 c (알파-2c) 길항제와 노르에피네프린 재흡수 억제제의 조합물
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JOP20190284A1 (ar) 2017-06-14 2019-12-11 Bayer Pharma AG مركبات إيميدازوبيريميدين مستبدلة بديازا ثنائي الحلقة واستخدامها للمعالجة من اضطرابات التنفس
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