AR063979A1 - Antagonistas de receptor de orexina de diazepam sustituidos - Google Patents

Antagonistas de receptor de orexina de diazepam sustituidos

Info

Publication number
AR063979A1
AR063979A1 ARP070105246A ARP070105246A AR063979A1 AR 063979 A1 AR063979 A1 AR 063979A1 AR P070105246 A ARP070105246 A AR P070105246A AR P070105246 A ARP070105246 A AR P070105246A AR 063979 A1 AR063979 A1 AR 063979A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
substituents selected
alkyl
cycloalkyl
Prior art date
Application number
ARP070105246A
Other languages
English (en)
Original Assignee
Merck & Co Inc
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=39284173&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR063979(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR063979A1 publication Critical patent/AR063979A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/16Central respiratory analeptics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • A61P25/10Antiepileptics; Anticonvulsants for petit-mal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • A61P25/12Antiepileptics; Anticonvulsants for grand-mal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/052Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Otolaryngology (AREA)
  • Child & Adolescent Psychology (AREA)

Abstract

La presente está dirigida a compuestos de diazepam sustituidos que son antagonistas de receptores de orexina, y que son utiles en el tratamiento o la prevencion de trastornos o enfermedades neurologicas y psiquiátricas en los que están implicados los receptores de orexina. También está dirigida a composiciones farmacéuticas que comprenden estos compuestos y al uso de estos compuestos y composiciones en la prevencion o el tratamiento de dichas enfermedades en las que están implicados receptores de orexina. Reivindicacion 1: Un compuesto de formula 1, en la que R1 es fenilo que está sustituido con R1a, R1b y R1c; R2 es heteroarilo que está sustituido con R2a, R2b y R2c; R1a, R1b, R1c, R2a, R2b y R2c se seleccionan independientemente del grupo constituido por: (1) hidrogeno, (2) halogeno, (3) hidroxilo, (4) -(C=O)m-On-alquilo C1-6, en el que m es 0 o 1, n es 0 o 1 (en el que si rn es 0 o n es 0, está presente un enlace), en la que los R2a y R2b o R2b y R2c adyacentes pueden estar unidos conjuntamente formando un anillo cicloalquilo o cicloalcoxi, y en los que el alquilo está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13, (5) -(C=O)rn-On-cicloalquilo C3-6, en el que el cicloalquilo está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13, (6) -(C=O)rn-alquenilo C2-4, en el que el alquenilo está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13, (7) -(C=O)m- alquinilo C2-4, en el que el alquinilo está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13, (8) -(C=O)m-On-fenilo o -(C=O)m-On-naftilo, en los que el fenilo o naftilo está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13, (9) -(C=O)m-On-heterociclo, en el que el heterociclo está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13, (10) -(C=O)m-NR10R11, en el que R10 y R11 se seleccionan independientemente del grupo constituido por: (a) hidrogeno, (b) alquilo C1-6, que está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13, (c) alquenilo C3-6, que está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13, (d) cicloalquilo, que está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13, (e) fenilo, que está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13, y (f) heterociclo, que está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13, (11) -S(O)2-NR10R11, (12) -S(O)q-R12, en el que q es 0, 1 o 2 y en el que R12 se selecciona de las definiciones de R10 y R11, (13) -CO2H, (14) -CN, (15) -NO2, (16) =O, y (17) -B(OH)2, con la condicion de que al menos uno de R2a, R2b o R2c sea halogeno o alquilo C1-6, o en la que los R2a y R2b o R2b y R2c adyacentes están unidos conjuntamente formando un anillo cicloalquilo o cicloalcoxi, en el que el alquilo, cicloalquilo o cicloalcoxi está no sustituido o sustituido con uno o más sustituyentes seleccionados de R13; R3 es -alquilo C1-6 o -cicloalquilo C3-6, que están no sustituidos o sustituidos con uno o más sustituyentes seleccionados de R13; R13 se selecciona del grupo constituido por: (1) halogeno, (2) hidroxilo, (3) -(C=O)m-On-alquilo C1-6, en el que el alquilo está no sustituido o sustituido con uno o más sustituyentes seleccionados de R14, (4) -On-perfluoroalquilo C1-3, (5) -(C=O)m-On-cicloalquilo C3-6, en el que el cicloalquilo está no sustituido o sustituido con uno o más sustituyentes seleccionados de R14, (6) -(C=O)m-alquenilo C2-4, en el que el alquenilo está no sustituido o sustituido con uno o más sustituyentes seleccionados de R14, (7) - (C=O)m-On-fenilo o -(C=O)m-On-naftilo, en los que el fenilo o naftilo está no sustituido o sustituido con uno o más sustituyentes seleccionados de R14, (8) -(C=O)m-On-heterociclo, en el que el heterociclo está no sustituido o sustituido con uno o más sustituyentes seleccionados de R14, (9) -(C=O)m-NR10R11, (10) -S(O)2-NR10R11, (11) -S(O)q-R12, (12) -CO2H, (13) -CN, (14) =O, y (15) -NO2; R14 se selecciona del grupo constituido por: (1) hidroxilo, (2) halogeno, (3) alquilo C1-6, (4) - cicloalquilo C3-6, (5) -O-alquilo C1-6, (6) -O(C=O)-alquilo C1-6, (7) -NH-alquilo C1-6, (8) fenilo, (9) heterociclo, (10) -CO2H, y (11) -CN; o una sal farmacéuticamente aceptable del mismo.
ARP070105246A 2006-12-01 2007-11-27 Antagonistas de receptor de orexina de diazepam sustituidos AR063979A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US87239306P 2006-12-01 2006-12-01
US95974207P 2007-07-16 2007-07-16

Publications (1)

Publication Number Publication Date
AR063979A1 true AR063979A1 (es) 2009-03-04

Family

ID=39284173

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP070105246A AR063979A1 (es) 2006-12-01 2007-11-27 Antagonistas de receptor de orexina de diazepam sustituidos
ARP120104304A AR088881A2 (es) 2006-12-01 2012-11-15 Una composicion farmaceutica que comprende 5-cloro-2-{(5r)-5-metil-4-[5-metil-2-(2h-1,2,3-triazol-2-il)benzoil]-1,4-diazepan-1-il}-1,3-benzoxazol; o una sal farmaceuticamente aceptable del mismo y su uso en la preparacion de medicamentos

Family Applications After (1)

Application Number Title Priority Date Filing Date
ARP120104304A AR088881A2 (es) 2006-12-01 2012-11-15 Una composicion farmaceutica que comprende 5-cloro-2-{(5r)-5-metil-4-[5-metil-2-(2h-1,2,3-triazol-2-il)benzoil]-1,4-diazepan-1-il}-1,3-benzoxazol; o una sal farmaceuticamente aceptable del mismo y su uso en la preparacion de medicamentos

Country Status (35)

Country Link
US (2) US7951797B2 (es)
EP (2) EP2392572B1 (es)
JP (3) JP4675427B2 (es)
KR (2) KR101217057B1 (es)
CN (1) CN101880276B (es)
AR (2) AR063979A1 (es)
AU (2) AU2007328267B2 (es)
BR (1) BRPI0719361B8 (es)
CA (1) CA2670892C (es)
CL (2) CL2007003441A1 (es)
CO (1) CO6190524A2 (es)
CR (1) CR10859A (es)
CY (1) CY1113798T1 (es)
DK (1) DK2089382T3 (es)
DO (1) DOP2009000126A (es)
EC (1) ECSP099374A (es)
ES (1) ES2397188T3 (es)
HK (1) HK1128691A1 (es)
HR (1) HRP20130002T1 (es)
IL (1) IL198825A0 (es)
MA (1) MA31016B1 (es)
MX (1) MX2009005712A (es)
MY (1) MY161834A (es)
NI (1) NI200900100A (es)
NO (1) NO342586B1 (es)
NZ (1) NZ577334A (es)
PE (1) PE20081229A1 (es)
PL (1) PL2089382T3 (es)
PT (1) PT2089382E (es)
RS (1) RS52617B (es)
RU (2) RU2458924C3 (es)
SI (1) SI2089382T1 (es)
SV (1) SV2009003276A (es)
TW (2) TWI515188B (es)
WO (1) WO2008069997A1 (es)

Families Citing this family (106)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2049529T3 (pl) * 2006-07-14 2011-01-31 Merck Sharp & Dohme Podstawione związki diazepanowe - antagoniści receptora oreksyny
EP2049110B1 (en) * 2006-07-14 2014-08-20 Merck Sharp & Dohme Corp. Bridged diazepan orexin receptor antagonists
PE20081229A1 (es) * 2006-12-01 2008-08-28 Merck & Co Inc Antagonistas de receptor de orexina de diazepam sustituido
AU2008255005B2 (en) 2007-05-18 2013-05-02 Merck Sharp & Dohme Corp. OXO bridged diazepan orexin receptor antagonists
PL2152690T3 (pl) * 2007-05-23 2012-06-29 Merck Sharp & Dohme Pirydylo piperydynowi antagoniści receptora oreksyny
EP2214676B1 (en) 2007-10-29 2012-11-21 Merck Sharp & Dohme Corp. Substituted diazepan orexin receptor antagonists
WO2009097995A1 (de) * 2008-02-07 2009-08-13 Sanofi-Aventis Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
US8785491B2 (en) * 2008-06-19 2014-07-22 Takeda Pharmaceuticals U.S.A., Inc. Pharmaceutical compositions and methods for treating age-related macular degeneration with melatonin analogues
CA2739927A1 (en) * 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. Disubstituted azepan orexin receptor antagonists
CA2739917A1 (en) 2008-10-21 2010-04-29 Merck Sharp & Dohme Corp. 2,5-disubstituted morpholine orexin receptor antagonists
US8853202B2 (en) 2008-11-04 2014-10-07 Chemocentryx, Inc. Modulators of CXCR7
BRPI0921496A2 (pt) * 2008-11-04 2016-01-19 Chemocentryx Inc composto, composição farmacêutica, e, métodos para tratar doença ou distúrbio, para inibir ligação de quimiocinas a um receptor, para formar imagem de um dito tumor, orgão ou tecido, e para detectar níveis elevados de cxcr7 em uma amostra
US20110046047A1 (en) * 2009-05-20 2011-02-24 Joslin Diabets Center, Inc. Bone Morphogenetic Proteins for Appetite Control
KR101350845B1 (ko) 2009-09-15 2014-01-14 주식회사 만도 전자 브레이크의 간극 조정 장치 및 그 방법
WO2011050202A1 (en) 2009-10-23 2011-04-28 Janssen Pharmaceutica Nv Fused heterocyclic compounds as orexin receptor modulators
JP5847087B2 (ja) * 2009-10-23 2016-01-20 ヤンセン ファーマシューティカ エヌ.ベー. オレキシン受容体調節因子としての縮合複素環式化合物
DK2491038T3 (da) 2009-10-23 2016-07-18 Janssen Pharmaceutica Nv Disubstituerede octahydropyrrolo [3,4-c]pyrroler som orexin receptormodulatorer
CA2778613C (en) 2009-10-24 2018-11-27 Indiana University Research And Technology Corporation Methods and compositions for panic disorders
US9096558B2 (en) 2010-07-09 2015-08-04 Pfizer Limited N-sulfonylbenzamide compounds
SI2626350T1 (sl) 2010-09-22 2015-09-30 Eisai R&D Management Co., Ltd. Spojina ciklopropana
WO2012085852A1 (en) 2010-12-22 2012-06-28 Actelion Pharmaceuticals Ltd 3,8-diaza-bicyclo[4.2.0]oct-8-yl amides
EP2680697B1 (en) 2011-03-03 2018-01-10 Merck Sharp & Dohme Corp. Process for the preparation of an orexin receptor antagonist
WO2012145581A1 (en) 2011-04-20 2012-10-26 Janssen Pharmaceutica Nv Disubstituted octahy-dropyrrolo [3,4-c] pyrroles as orexin receptor modulators
US9617517B2 (en) 2011-05-02 2017-04-11 National University Corporation Kumamoto University Small chemical compound which promotes induction of differentiation of stem cells into insulin-producing cells and method for inducing differentiation of stem cells into insulin-producing cells using said small chemical compound
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
WO2013050938A1 (en) 2011-10-04 2013-04-11 Actelion Pharmaceuticals Ltd 3,7-diazabicyclo[3.3.1]nonane and 9-oxa-3,7-diazabicyclo[3.3.1]nonane derivatives
AR088352A1 (es) 2011-10-19 2014-05-28 Merck Sharp & Dohme Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina
AR088692A1 (es) 2011-11-08 2014-06-25 Actelion Pharmaceuticals Ltd Derivados de 2-(1,2,3-triazol-2-il)benzamina y 3-(1,2,3-triazol-2-il)picolinamida
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
SG11201404738QA (en) 2012-02-07 2014-10-30 Eolas Therapeutics Inc Substituted prolines / piperidines as orexin receptor antagonists
US9440982B2 (en) 2012-02-07 2016-09-13 Eolas Therapeutics, Inc. Substituted prolines/piperidines as orexin receptor antagonists
EP2847343A4 (en) 2012-05-09 2016-04-06 Merck Sharp & Dohme METHOD FOR PREPARING AN INTERMEDIATE FOR AN OREXIN RECEPTOR ANTAGONIST
EP2854816B1 (en) * 2012-05-31 2020-07-08 Merck Sharp & Dohme Corp. Solid dosage formulations of an orexin receptor antagonist
NZ703448A (en) 2012-06-04 2017-07-28 Actelion Pharmaceuticals Ltd Benzimidazole-proline derivatives
CN104703980B (zh) 2012-10-10 2017-09-22 埃科特莱茵药品有限公司 属于[邻双(杂)芳基]‑[2‑(间双(杂)芳基)吡咯烷‑1‑基]甲酮衍生物的食欲素受体拮抗剂
US20160272627A1 (en) * 2012-11-12 2016-09-22 Dr. Reddy's Laboratories Limited Polymorphic forms of suvoroxant
CN105189484B (zh) 2012-11-29 2018-05-04 凯莫森特里克斯股份有限公司 Cxcr7拮抗剂
US8999393B1 (en) * 2013-01-09 2015-04-07 Edgemont Pharmaceuticals Llc Sustained release formulations of lorazepam
EP2970241A1 (en) 2013-03-12 2016-01-20 Actelion Pharmaceuticals Ltd. Azetidine amide derivatives as orexin receptor antagonists
WO2015003355A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
US9579324B2 (en) 2013-07-11 2017-02-28 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
WO2015003360A2 (en) 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
CN105593215B (zh) 2013-07-11 2019-01-15 安吉奥斯医药品有限公司 用于治疗癌症的作为idh2突变体抑制剂的2,4-或4,6-二氨基嘧啶化合物
CA2918451A1 (en) * 2013-07-15 2015-01-22 Dr. Reddy's Laboratories Limited Process for the preparation of suvorexant and intermediates useful in the synthesis of suvorexant
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
UA119151C2 (uk) 2013-12-03 2019-05-10 Ідорсія Фармасьютікалз Лтд КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА
CA2929423C (en) 2013-12-03 2021-12-07 Actelion Pharmaceuticals Ltd Crystalline form of (s)-(2-(6-chloro-7-methyl-1h-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1 -yl)(5-methoxy-2-(2h-1 ,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists
AU2014358766B2 (en) 2013-12-04 2019-01-17 Idorsia Pharmaceuticals Ltd Use of benzimidazole-proline derivatives
US9732077B2 (en) 2013-12-18 2017-08-15 Merck Sharp & Dohme Corp. Diazepane orexin receptor antagonists
WO2015095442A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Piperidinyloxy lactone orexin receptor antagonists
KR20220070066A (ko) 2014-03-14 2022-05-27 아지오스 파마슈티컬스 아이엔씨. 치료적으로 활성인 화합물의 약제학적 조성물
WO2015158910A2 (en) 2014-04-17 2015-10-22 Sandoz Ag Solid dispersion comprising an orexin receptor antagonist
WO2015164160A1 (en) 2014-04-21 2015-10-29 Merck Sharp & Dohme Corp. Pharmaceutical salts of an orexin receptor antagonist
WO2015180060A1 (zh) * 2014-05-28 2015-12-03 杭州普晒医药科技有限公司 一种二氮杂环庚烷化合物的盐及其晶型与无定型物
WO2016020404A1 (en) * 2014-08-04 2016-02-11 Sandoz Ag Process for the resolution of (r,s)-diazepane and diazepanone derivatives
CN106573882B (zh) * 2014-08-04 2020-09-01 桑多斯股份公司 制备苏沃雷生的合成途径
WO2016020403A1 (en) * 2014-08-04 2016-02-11 Sandoz Ag Preparation of a benzoic acid derivative and its use for the preparation of suvorexant
EP3178814B1 (en) 2014-08-06 2019-04-10 Eisai R&D Management Co., Ltd. Method for producing pyrimidin-1-ol compound, and intermediate thereof
EP3180332B1 (en) 2014-08-13 2021-10-27 Eolas Therapeutics Inc. Difluoropyrrolidines as orexin receptor modulators
AU2015336463B2 (en) 2014-10-23 2020-06-18 Eisai R&D Management Co., Ltd. Compositions and methods for treating insomnia
WO2016065586A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Pyrazole, triazole and tetrazole orexin receptor antagonists
WO2016065585A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Piperidine isoxazole and isothiazole orexin receptor antagonists
WO2016065587A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Pyrazole orexin receptor antagonists
WO2016065584A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Piperidine oxadiazole and thiadiazole orexin receptor antagonists
WO2016065583A1 (en) 2014-10-30 2016-05-06 Merck Sharp & Dohme Corp. Oxazole orexin receptor antagonists
WO2016085784A1 (en) * 2014-11-26 2016-06-02 Merck Sharp & Dohme Corp. Methyl diazepane orexin receptor antagonists
US9994570B2 (en) 2014-11-26 2018-06-12 Merck Sharp & Dohme Corp. Bridged diazepane orexin receptor antagonists
WO2016086357A1 (en) 2014-12-02 2016-06-09 Merck Sharp & Dohme Corp. Methyl oxazole orexin receptor antagonists
WO2016086358A1 (en) 2014-12-02 2016-06-09 Merck Sharp & Dohme Corp. Hydroxymethyl piperidine orexin receptor antagonists
US9987255B2 (en) 2014-12-19 2018-06-05 Merck Sharp & Dohme Corp. 5,5-bicyclic oxazole orexin receptor antagonists
WO2016095204A1 (en) 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Pyrrolidine orexin receptor antagonists
WO2016100157A2 (en) 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. 6,5-bicyclic octahydropyrrolopyridine orexin receptor antagonists
WO2016100161A1 (en) 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Ethyldiamine orexin receptor antagonists
WO2016095205A1 (en) 2014-12-19 2016-06-23 Merck Sharp & Dohme Corp. Heteroaryl orexin receptor antagonists
WO2016101119A1 (en) 2014-12-23 2016-06-30 Merck Sharp & Dohme Corp. Fused heteroaryl derivatives as orexin receptor antagonists
WO2016101118A1 (en) 2014-12-23 2016-06-30 Merck Sharp & Dohme Corp. Amidoethyl azole orexin receptor antagonists
CZ201587A3 (cs) 2015-02-10 2016-08-17 Zentiva, K.S. Amorfní pevná forma suvorexantu s kyselinou sírovou
WO2016149628A1 (en) * 2015-03-19 2016-09-22 Chembridge Corporation Tgr5 agonists
US10131653B2 (en) 2015-04-24 2018-11-20 Takeda Pharmaceutical Company Limited Heterocyclic compound
AR105025A1 (es) * 2015-06-19 2017-08-30 Astellas Pharma Inc Compuesto de imidazodiazepina
WO2017001499A1 (en) 2015-06-30 2017-01-05 Hexal Ag Liquid composition comprising suvorexant
WO2017012502A1 (en) 2015-07-17 2017-01-26 Sunshine Lake Pharma Co., Ltd. Substituted quinazoline compounds and preparation and uses thereof
HRP20211790T1 (hr) 2015-10-15 2022-03-04 Les Laboratoires Servier Kombinirana terapija za liječenje maligniteta
PL3362065T3 (pl) 2015-10-15 2024-09-16 Les Laboratoires Servier Terapia skojarzona zawierająca iwosidenib, cytarabinę i daunorubicynę lub idarubicynę do leczenia ostrej białaczki szpikowej
SG11201803191VA (en) 2015-10-29 2018-05-30 Univ Tsukuba Morphinan derivative and medical usage thereof
WO2017072264A1 (en) 2015-10-29 2017-05-04 Hexal Ag Solid composition comprising suvorexant
US10370380B2 (en) 2015-11-23 2019-08-06 Sunshine Lake Pharma Co., Ltd. Octahydropyrrolo[3,4-c]pyrrole derivatives and uses thereof
CN107021955B (zh) * 2016-02-01 2021-03-30 上海奥博生物医药股份有限公司 苏沃雷生中间体化合物及其制备方法
CN109219606B (zh) 2016-02-12 2021-10-01 阿斯利康(瑞典)有限公司 食欲素受体调节剂的卤素取代的哌啶
CA3016706A1 (en) 2016-03-10 2017-09-14 Janssen Pharmaceutica Nv Methods of treating depression using orexin-2 receptor antagonists
CN107179356B (zh) * 2016-03-11 2021-07-16 广东东阳光药业有限公司 一种用hplc法测定苏沃雷生有关物质的方法
CN107304204B (zh) * 2016-04-18 2020-12-22 广东东阳光药业有限公司 一种制备n-杂环化合物的方法
WO2017194548A1 (en) 2016-05-10 2017-11-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of autoimmune inflammatory diseases
CN109195954A (zh) 2016-06-06 2019-01-11 南迪亚公司 沃雷生的中间体的手性拆分及其共晶
EP3554508A4 (en) * 2016-12-19 2020-08-05 Druggability Technologies IP Holdco Limited SUVOREXANT PHARMACEUTICAL FORMULATIONS
GB201702174D0 (en) 2017-02-09 2017-03-29 Benevolentai Bio Ltd Orexin receptor antagonists
MX2019012902A (es) * 2017-05-03 2019-12-16 Idorsia Pharmaceuticals Ltd Preparacion de derivados de acido 2-([1,2,3]triazol-2-il)-benzoico .
GB201707499D0 (en) 2017-05-10 2017-06-21 Benevolentai Bio Ltd Orexin receptor antagonists
GB201707504D0 (en) 2017-05-10 2017-06-21 Benevolentai Bio Ltd Orexin receptor antagonists
CN115710250A (zh) * 2017-08-01 2023-02-24 博健制药有限责任公司 一种食欲素受体拮抗剂的晶型及其制备方法和用途
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
WO2020007977A1 (en) * 2018-07-06 2020-01-09 Idorsia Pharmaceuticals Ltd 7-trifluoromethyl-[1,4]diazepan derivatives
MX2021006915A (es) 2018-12-12 2021-08-24 Chemocentryx Inc Inhibidores de cxcr7 para el tratamiento de cancer.
CZ310035B6 (cs) * 2019-12-09 2024-05-29 Univerzita PalackĂ©ho v Olomouci N-(furan-2-ylmethyl)-7H-purin-6-amin pro modulaci cirkadiánních rytmů
MX2023001688A (es) 2020-08-12 2023-02-22 Spruce Biosciences Inc Metodos y composiciones para tratar el sindrome de ovario poliquistico.
CN111943945B (zh) * 2020-09-03 2022-07-12 上海应用技术大学 一种苏沃雷生中间体及其制备方法

Family Cites Families (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS536156B2 (es) * 1972-10-30 1978-03-04
GB2068961B (en) * 1980-02-13 1983-11-30 Sankyo Co Quinazoline derivatives
JPH0747574B2 (ja) * 1989-03-03 1995-05-24 大日本製薬株式会社 ピリジン誘導体及びそれを有効成分とする向精神剤
EP0794178A4 (en) * 1994-11-25 1998-02-25 Nippon Chemiphar Co CHINAZOLIN DERIVATIVES
GB9606805D0 (en) 1996-03-30 1996-06-05 Glaxo Wellcome Inc Medicaments
AR016817A1 (es) 1997-08-14 2001-08-01 Smithkline Beecham Plc Derivados de fenilurea o feniltiourea, procedimiento para su preparacion, coleccion de compuestos, compuestos intermediarios, composicion farmaceutica,metodo de tratamiento y uso de dichos compuestos para la manufactura de un medicamento
ES2196806T3 (es) 1998-05-08 2003-12-16 Smithkline Beecham Plc Derivados de fenilurea y de feniltiourea.
WO2000047576A1 (en) 1999-02-12 2000-08-17 Smithkline Beecham Plc Cinnamide derivatives as orexin-1 receptors antagonists
JP2002536447A (ja) 1999-02-12 2002-10-29 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー フェニル尿素およびフェニルチオ尿素誘導体
JP2002536445A (ja) 1999-02-12 2002-10-29 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー オレキシン受容体アンタゴニストとしてのフェニル尿素およびフェニルチオ尿素誘導体
US6414002B1 (en) 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
MXPA02008797A (es) 2000-03-14 2005-09-08 Actelion Pharmaceuticals Ltd Derivados de 1,2,3,4-tetrahidroisoquinolina.
CA2408343A1 (en) * 2000-05-11 2002-11-07 Banyu Pharmaceutical Co., Ltd. N-acyltetrahydroisoquinoline derivatives
PT1289955E (pt) 2000-06-16 2005-08-31 Smithkline Beecham Plc Piperidinas para utilizacao como antagonistas dos receptores da orexina
DE10036818A1 (de) * 2000-07-28 2002-02-07 Solvay Pharm Gmbh Neue N-Triazolylmethyl-Piperazinderivate als Neurokininrezeptor-Antagonisten
EP1353918B1 (en) 2000-11-28 2005-01-12 Smithkline Beecham Plc Morpholine derivatives as antagonists of orexin receptors
WO2002051232A2 (en) 2000-12-27 2002-07-04 Actelion Pharmaceuticals Ltd. Novel benzazepines and related heterocyclic derivatives
US7432270B2 (en) 2001-05-05 2008-10-07 Smithkline Beecham P.L.C. N-aroyl cyclic amines
US20040192673A1 (en) 2001-05-05 2004-09-30 Pascale Gaillard N-aroyl cyclic amine derivatives as orexin receptor antagonists
GB0115862D0 (en) 2001-06-28 2001-08-22 Smithkline Beecham Plc Compounds
EP1399441B1 (en) 2001-06-28 2006-07-05 Smithkline Beecham Plc N-aroyl cyclic amine derivatives as orexin receptor antagonists
GB0124463D0 (en) 2001-10-11 2001-12-05 Smithkline Beecham Plc Compounds
GB0126292D0 (en) 2001-11-01 2002-01-02 Smithkline Beecham Plc Compounds
GB0127145D0 (en) 2001-11-10 2002-01-02 Smithkline Beecham Compounds
GB0130335D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
GB0130393D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
GB0130341D0 (en) 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
WO2004004733A1 (en) 2002-07-09 2004-01-15 Actelion Pharmaceuticals Ltd. 7,8,9,10-tetrahydro-6h-azepino, 6,7,8,9-tetrahydro-pyrido and 2,3-dihydro-2h-pyrrolo[2,1-b]-quinazolinone derivatives
EP1539747B1 (en) 2002-09-18 2006-11-02 Glaxo Group Limited N-aroyl cyclic amines as orexin receptor antagonists
CN1332942C (zh) 2002-10-11 2007-08-22 埃科特莱茵药品有限公司 磺酰基氨基-乙酸衍生物及其作为阿立新受体拮抗剂的应用
GB0225938D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
GB0225884D0 (en) 2002-11-06 2002-12-11 Glaxo Group Ltd Novel compounds
AU2003299648A1 (en) 2002-12-12 2004-06-30 Janssen Pharmaceutica, N.V. Substituted 4-phenyl-(1,3)-dioxanes
PL1633724T3 (pl) * 2003-03-12 2011-10-31 Kudos Pharm Ltd Pochodne ftalazynonu
CL2004000553A1 (es) 2003-03-20 2005-02-04 Actelion Pharmaceuticals Ltd Uso de compuestos derivados de guanidina como antagonistas del receptor de neuropeptido ff; compuestos derivados de guanidina; procedimientos de preparacion; y composicion farmaceutica que los comprende.
EP1611104B1 (en) 2003-03-26 2009-07-01 Actelion Pharmaceuticals Ltd. Tetrahydroisoquinolyl acetamide derivatives for use as orexin receptor antagonists
CN1780820A (zh) 2003-04-28 2006-05-31 埃科特莱茵药品有限公司 作为阿立新受体拮抗剂的喹喔啉-3-酮衍生物
ES2322651T3 (es) * 2003-09-09 2009-06-24 F. Hoffmann-La Roche Ag Derivados de 1-benzoil-piperazina como inhibidores de absorcion de glicina para el tratamiento de psicosis.
HUP0304101A3 (en) 2003-12-22 2008-10-28 Sanofi Aventis Pyrazole derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates
HUP0400405A3 (en) 2004-02-10 2009-03-30 Sanofi Synthelabo Pyrimidine derivatives, process for producing them, their use, pharmaceutical compositions containing them and their intermediates
AU2005250077B2 (en) 2004-03-01 2011-06-09 Idorsia Pharmaceuticals Ltd Substituted 1,2,3,4-tetrahydroisoquinoline derivatives
WO2006067224A2 (en) 2004-12-23 2006-06-29 Biovitrum Ab (Publ) Spiro-benzodioxole and spiro-benzodioxane compounds as orexin receptor antagonists
AU2006235302A1 (en) 2005-04-12 2006-10-19 Merck & Co., Inc. Amidopropoxyphenyl orexin receptor antagonists
WO2006124748A2 (en) * 2005-05-13 2006-11-23 Lexicon Genetics Incorporated Multicyclic compounds and methods of their use
US20060258762A1 (en) * 2005-05-13 2006-11-16 Dobransky Michael A Hydrocarbon or hydrofluorocarbon blown ASTM E-84 class I rigid polyurethane foams
CA2609203A1 (en) 2005-05-23 2006-11-30 Merck & Co., Inc Proline bis-amide orexin receptor antagonists
JP2009503106A (ja) 2005-08-04 2009-01-29 メルク エンド カムパニー インコーポレーテッド アミノエタンスルホンアミドオレキシン受容体アンタゴニスト
WO2007025069A2 (en) 2005-08-26 2007-03-01 Merck & Co., Inc. Diazaspirodecane orexin receptor antagonists
US8685961B2 (en) 2006-03-29 2014-04-01 Merck Sharp & Dohme Corp. Diazepan orexin receptor antagonists
EP2049110B1 (en) 2006-07-14 2014-08-20 Merck Sharp & Dohme Corp. Bridged diazepan orexin receptor antagonists
PL2049529T3 (pl) 2006-07-14 2011-01-31 Merck Sharp & Dohme Podstawione związki diazepanowe - antagoniści receptora oreksyny
PE20081229A1 (es) * 2006-12-01 2008-08-28 Merck & Co Inc Antagonistas de receptor de orexina de diazepam sustituido
EP2214676B1 (en) * 2007-10-29 2012-11-21 Merck Sharp & Dohme Corp. Substituted diazepan orexin receptor antagonists

Also Published As

Publication number Publication date
TWI513696B (zh) 2015-12-21
BRPI0719361A2 (pt) 2014-02-04
SV2009003276A (es) 2009-11-09
JP2011079848A (ja) 2011-04-21
CY1113798T1 (el) 2016-07-27
US7951797B2 (en) 2011-05-31
IL198825A0 (en) 2010-02-17
CA2670892A1 (en) 2008-06-12
DOP2009000126A (es) 2009-08-15
DK2089382T3 (da) 2013-02-04
JP4675427B2 (ja) 2011-04-20
CO6190524A2 (es) 2010-08-19
EP2089382A1 (en) 2009-08-19
NO342586B1 (no) 2018-06-18
EP2089382B1 (en) 2012-10-24
TW200831494A (en) 2008-08-01
JP5335758B2 (ja) 2013-11-06
ECSP099374A (es) 2009-07-31
KR101217057B1 (ko) 2013-01-02
JP2010511621A (ja) 2010-04-15
JP2011068665A (ja) 2011-04-07
AR088881A2 (es) 2014-07-16
NI200900100A (es) 2010-02-11
MX2009005712A (es) 2009-06-08
CL2010001173A1 (es) 2011-03-25
BRPI0719361B1 (pt) 2020-10-06
TW201109318A (en) 2011-03-16
CL2007003441A1 (es) 2008-05-30
CN101880276B (zh) 2013-06-19
RS52617B (en) 2013-06-28
RU2458924C3 (ru) 2017-11-16
AU2007328267B2 (en) 2011-03-24
SI2089382T1 (sl) 2013-02-28
MA31016B1 (fr) 2009-12-01
CR10859A (es) 2009-06-25
ES2397188T3 (es) 2013-03-05
PT2089382E (pt) 2013-01-24
RU2561727C2 (ru) 2015-09-10
CA2670892C (en) 2013-08-13
KR20100031767A (ko) 2010-03-24
CN101880276A (zh) 2010-11-10
EP2392572B1 (en) 2014-05-14
HK1128691A1 (en) 2009-11-06
RU2458924C2 (ru) 2012-08-20
KR20090087110A (ko) 2009-08-14
RU2009125024A (ru) 2011-01-10
WO2008069997A1 (en) 2008-06-12
NO20092470L (no) 2009-08-27
US20080132490A1 (en) 2008-06-05
NZ577334A (en) 2011-09-30
JP5767803B2 (ja) 2015-08-19
EP2392572A1 (en) 2011-12-07
HRP20130002T1 (hr) 2013-01-31
AU2007328267A1 (en) 2008-06-12
US20110195957A1 (en) 2011-08-11
BRPI0719361B8 (pt) 2021-05-25
TWI515188B (zh) 2016-01-01
KR101299426B1 (ko) 2013-08-30
PE20081229A1 (es) 2008-08-28
MY161834A (en) 2017-05-15
RU2010150818A (ru) 2012-06-20
AU2010249269B2 (en) 2012-02-02
PL2089382T3 (pl) 2013-03-29
AU2010249269A1 (en) 2011-01-06

Similar Documents

Publication Publication Date Title
AR063979A1 (es) Antagonistas de receptor de orexina de diazepam sustituidos
AR072899A1 (es) Derivados de terpiridina-carboxamida antagonistas de receptores de orexina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del insomnio y la obesidad.
CO6170356A2 (es) Derivados de piridazina
AR087288A1 (es) Compuestos de tetrahidropirido-piridina y tetrahidropirido-pirimidina y su uso como moduladores de receptores de c5a
GT200500185A (es) Moduladores del receptor de progesterona que comprenden derivados de pirrol-oxindol y sus usos
GT200500292A (es) Derivados de 2-amido-4-feniltiazol, su preparacion y su aplicacion en terapeutica
GT200400161A (es) Piridinonas sustituidas
AR061923A1 (es) Compuestos derivados de benzofuran-piperidina
TW200718422A (en) 1,6-Dihydro-1,3,5,6-tetraaza-as-indacene based tricyclic compounds and pharmaceutical compositions comprising same
GT200400092A (es) Preparacion y uso de derivados de alquilarilo para el tratamiento de la obesidad
GT200800258A (es) Compuestos de pirrolo-pirimidina y sus usos
MX2009007077A (es) Analogos de ciclopamina.
CL2004000917A1 (es) Compuestos derivados de tiazol; procedimiento de preparacion; composicion farmaceutica; y su uso para el tratamiento de enfermedades mediadas por 3-cinasa de dosfatidilnositol tal como enfermedades respiratorias, alergias, artritis reumatoide, osteoa
BRPI0520870B8 (pt) compostos intermediários para a preparação de alfa-mercaptoacetanilidas de s-triazolila
AR056979A1 (es) Derivados de dihidrobenzofuranos y usos de los mismos
CO6160307A2 (es) Compuestos de pirazolina y su uso y composiciones farmaceuticas
PE20130155A1 (es) Derivados de ariletinilo
ES2603931T3 (es) Compuestos de triazolo
CO5700829A2 (es) Derivados triciclicos de indol y su uso en eltratamiento de la enfermedad de alzheimer
AR060535A1 (es) Pirido-piridazinonas y ftalazinonas como antagonistas duales de los receptores h1 y h3 de histamina
AR050167A1 (es) Compuesto piperidina y procedimiento para preparar el mismo
AR056470A1 (es) Sulfonamidos n- ciclicos puenteados inhibidores de gamma secretasa
GT200600030A (es) 2-fenil-indoles como antagonistas del receptor de la prostaglandina d2
CO6801736A2 (es) Derivados heterocíclicos de amina
AR073774A1 (es) Compuestos antibioticos oxazolidinona triciclicos

Legal Events

Date Code Title Description
FG Grant, registration