MA33855B1 - Dérivés de benzamide substitués - Google Patents

Dérivés de benzamide substitués

Info

Publication number
MA33855B1
MA33855B1 MA35019A MA35019A MA33855B1 MA 33855 B1 MA33855 B1 MA 33855B1 MA 35019 A MA35019 A MA 35019A MA 35019 A MA35019 A MA 35019A MA 33855 B1 MA33855 B1 MA 33855B1
Authority
MA
Morocco
Prior art keywords
lower alkyl
disorders
phenyl
optionally substituted
heterocycloalkyl
Prior art date
Application number
MA35019A
Other languages
Arabic (ar)
English (en)
Inventor
Zbinden Katrin Groebke
Roger Norcross
Philippe Pflieger
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43544985&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MA33855(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of MA33855B1 publication Critical patent/MA33855B1/fr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/06Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/4025Heterocyclic 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61P25/06Antimigraine 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
    • A61P25/14Drugs 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
    • A61P25/36Opioid-abuse
    • 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
    • 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
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/12Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D267/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02Seven-membered rings
    • C07D267/08Seven-membered rings having the hetero atoms in positions 1 and 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D267/00Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02Seven-membered rings
    • C07D267/08Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/10Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • 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

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)

Abstract

L'invention concerne des composés de formule i, dans laquelle r est l'hydrogène ou un alkyle inférieur ; r1 est -(ch2)n-(o)o-hétérocycloalkyle ou -c(o)-hétérocycloalkyle, le groupe hétérocycloalkyle étant éventuellement substitué par un alkyle inférieur, un hydroxy, un halogène ou par -(ch2)p-aryle ; n est 0, 1 ou 2 ; o est 0 ou 1 ; p est 0, 1 ou 2 ; r2 est cf3, cycloalkyle, éventuellement substitué par un alcoxy inférieur ou un halogène, ou est indan-2-yle, ou est hétérocycloalkyle, éventuellement substitué par hétéroaryle, ou est aryle ou hétéroaryle, les cycles aromatiques étant éventuellement substitués par un ou deux substituants, choisis parmi un alkyle inférieur, un halogène, un hétéroaryle, hydroxy, cf3, ocf3, och2cf3, och2-cycloalkyle, och2c(ch2oh)(ch2cl)(ch3), s-alkyle inférieur, alcoxy inférieur, ch2-alcoxy inférieur, alcynyle inférieur ou cyano, ou par -c(o)-phényle, -o-phényle, -o-ch2-phényle, phényle ou -ch2-phényle, et les cycles phényle pouvant éventuellement être substitués par un halogène, -c(o)-alkyle inférieur, -c(o)oh ou -c(o)o-alkyle inférieur, ou les cycles aromatiques étant éventuellement substitués par hétérocycloalkyle, och2-oxétan-3-yle ou o-tétrahydropyran-4-yle, éventuellement substitué par un alkyle inférieur ; x est une liaison, -nr'-, -ch2nh-, -chr''-, -(chr'')q-o-, -o-(chr'')q- ou -(ch2)2- ; y est une liaison ou -ch2-, r' l'hydrogène ou un alkyle inférieur, r'' est l'hydrogène, un alkyle inférieur, cf3, un alcoxy inférieur, q est 0, 1, 2 ou 3 ; ou un de leurs sels d'addition acide pharmaceutiquement appropriés. Il a maintenant été découvert que les composés de formule i ont une bonne affinité avec les récepteurs associés aux amines traces (taar), notamment taar1. Les composés peuvent être utilisés pour le traitement de la dépression, des troubles de l'anxiété, du trouble bipolaire, du trouble déficitaire de l'attention avec hyperactivité (tdah), des troubles associés au stress, des troubles psychotiques tels que la schizophrénie, des maladies neurologiques telles que la maladie de parkinson, des troubles neurodégénératifs tels que la maladie d'alzheimer, de l'épilepsie, de la migraine, de l'hypertension, de l'abus de substances et des troubles métaboliques tels que les troubles de l'alimentation, le diabète, les complications du diabète, l'obésité, la dyslipidémie, les troubles de la consommation et de l'assimilation d'énergie, les troubles et dysfonctionnements de l'homéostasie de la température corporelle, les troubles du sommeil et du rythme circadien, et les troubles cardiovasculaires
MA35019A 2009-12-22 2012-06-29 Dérivés de benzamide substitués MA33855B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09180504 2009-12-22
PCT/EP2010/070045 WO2011076678A1 (fr) 2009-12-22 2010-12-17 Dérivés de benzamide substitués

Publications (1)

Publication Number Publication Date
MA33855B1 true MA33855B1 (fr) 2012-12-03

Family

ID=43544985

Family Applications (1)

Application Number Title Priority Date Filing Date
MA35019A MA33855B1 (fr) 2009-12-22 2012-06-29 Dérivés de benzamide substitués

Country Status (25)

Country Link
US (4) US9452980B2 (fr)
EP (2) EP3187490B1 (fr)
JP (2) JP6109575B2 (fr)
KR (1) KR101461296B1 (fr)
CN (2) CN105254623A (fr)
AR (1) AR079542A1 (fr)
AU (1) AU2010335277B2 (fr)
BR (1) BR112012015168B1 (fr)
CA (1) CA2780161C (fr)
CL (1) CL2012001673A1 (fr)
CO (1) CO6531470A2 (fr)
CR (1) CR20120275A (fr)
EC (1) ECSP12011999A (fr)
IL (1) IL219437A (fr)
MA (1) MA33855B1 (fr)
MX (1) MX2012007409A (fr)
MY (1) MY176030A (fr)
NZ (1) NZ599577A (fr)
PE (1) PE20121395A1 (fr)
RU (1) RU2595902C2 (fr)
SG (1) SG181874A1 (fr)
TW (1) TWI409261B (fr)
UA (1) UA113141C2 (fr)
WO (1) WO2011076678A1 (fr)
ZA (1) ZA201203137B (fr)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9452980B2 (en) 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
US9132136B2 (en) * 2010-08-02 2015-09-15 Hoffmann-La Roche Inc. Pharmaceutical combination
US9073911B2 (en) * 2011-06-09 2015-07-07 Hoffmann-La Roche Inc. Pyrazole derivatives
US9029370B2 (en) * 2011-06-10 2015-05-12 Hoffmann-La Roche Inc. Substituted benzamide derivatives
WO2013104591A1 (fr) * 2012-01-12 2013-07-18 F. Hoffmann-La Roche Ag Dérivés hétérocycliques utilisés comme récepteurs associés à des amines sous forme de trace (taar)
MY178667A (en) 2012-09-14 2020-10-20 Hoffmann La Roche Pyrazole carboxamide derivatives as taar modulators for use in the treatment of several disorders, such as depression, diabetes and parkinson's disease
MX361761B (es) * 2012-09-17 2018-12-17 Hoffmann La Roche Derivados de triazol carboxamida.
CN108250128A (zh) * 2012-09-27 2018-07-06 江苏先声药业有限公司 作为钾通道调节剂的化合物
MX2015005721A (es) * 2012-11-07 2015-09-08 Hoffmann La Roche Derivados de pirazina.
US9045477B2 (en) * 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
CN103242191B (zh) * 2013-05-06 2015-05-20 暨南大学 一种防治老年痴呆症的化合物及其制备方法和用途
WO2015165085A1 (fr) 2014-04-30 2015-11-05 F.Hoffmann-La Roche Ag Dérivés de morpholine-pyridine
EP3149002B1 (fr) * 2014-05-28 2018-04-25 F.Hoffmann-La Roche Ag Dérivés 5-oxa-2-azabicyclo[2.2.2]octan-4-yliques et 5-oxa-2-azabicyclo[2.2.1]heptan-4-yliques en tant que modulateurs de taar1
WO2016015333A1 (fr) * 2014-08-01 2016-02-04 F.Hoffmann-La Roche Ag Dérivés de 2-oxa-5-azabicyclo[2.2.1]heptan-3-yl
CN104292143A (zh) * 2014-08-17 2015-01-21 湖南华腾制药有限公司 一种2-(4-溴苄基)吡咯烷的制备方法
CN104478798B (zh) * 2014-12-18 2017-01-18 武汉华纳联合药业有限公司 N‑氨基烷基磺酰基‑3‑吡啶甲酰胺衍生物及其在制备治疗心脑血管病药物中的应用
RU2731095C2 (ru) 2016-03-17 2020-08-28 Ф. Хоффманн-Ля Рош Аг Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar
WO2017210616A1 (fr) * 2016-06-02 2017-12-07 Purdue Pharma L.P. Agonistes du récepteur 1 associé à une amine à l'état de trace et agonistes partiels pour le traitement de la douleur
CN106432057A (zh) * 2016-09-17 2017-02-22 青岛云天生物技术有限公司 一种制备(3s)‑3‑(4‑氨基苯基)哌啶‑1‑甲酸叔丁酯的方法
WO2020113094A1 (fr) 2018-11-30 2020-06-04 Nuvation Bio Inc. Composés pyrrole et pyrazole et leurs procédés d'utilisation
WO2022087630A1 (fr) * 2020-10-23 2022-04-28 Icahn School Of Medicine At Mount Sinai Inhibiteurs du transport d'acides aminés
CN114478360B (zh) * 2022-02-10 2023-08-15 江苏海洋大学 一种苯甲酰胺类衍生物及其制备方法和应用
WO2023235844A2 (fr) * 2022-06-03 2023-12-07 Axsome Therapeutics Composés de carbamoyl phénylalaninol utiles en tant qu'agonistes de taar1

Family Cites Families (164)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US440195A (en) * 1890-11-11 Press for bundle-wrapping
US2731471A (en) 1956-01-17 Nxg hi
US609558A (en) * 1898-08-23 Lantern
US661266A (en) * 1899-11-27 1900-11-06 Francis T Roots Triple sign.
US2161938A (en) 1934-07-31 1939-06-13 Soc Of Chemical Ind Imidazolines
US2457047A (en) 1946-02-13 1948-12-21 Monsanto Chemicals 2-(2'-thenyl)-4, 5-dihydroimidazoles and process for making the same
DE842065C (de) 1950-07-30 1952-06-23 Bayer Ag Verfahren zur Herstellung stickstoffhaltiger heterocyclischer Verbindungen
US2778836A (en) 1954-04-02 1957-01-22 Union Chimique Belge Sa Substituted 2-methyl-delta2 imidazolines
US2744910A (en) 1955-06-27 1956-05-08 Bristol Lab Inc 2-(ortho-benzylbenzyl)-imidazoline and acid addition salts
US2744909A (en) 1955-06-27 1956-05-08 Bristol Lab Inc 2-(ortho-phenylbenzyl) imidazoline and acid addition salts
US2919274A (en) 1957-09-17 1959-12-29 Sahyun Melville Amidines
GB877306A (en) 1958-04-21 1961-09-13 Pfizer & Co C Halogenated derivatives of tetrahydro-1-naphthyl cyclic amidines
DE1083803B (de) 1958-05-30 1960-06-23 Bayer Ag Verfahren zur Herstellung von Derivaten der Anthranil-N-carbonsaeure
DE1121054B (de) 1960-11-23 1962-01-04 Merck Ag E Verfahren zur Herstellung eines neuen Imidazolinderivates und dessen Saeureadditionssalzen
US3202660A (en) 1961-10-09 1965-08-24 Boehringer Sohn Ingelheim Process for the preparation of 3-arylamino-1, 3-diazacycloalkenes
FR1355049A (fr) 1962-04-12 1964-03-13 Merck Ag E Agent pour le traitement préalable de la peau en vue du rasage
DE1150180B (de) 1962-04-12 1963-06-12 Merck Ag E Mittel zur Vorbehandlung der Haut fuer die Rasur
US3459763A (en) 1966-01-25 1969-08-05 Geigy Chem Corp Certain amino imidazole derivatives
ES323985A1 (es) 1966-02-26 1966-12-16 Blade Pique Juan Procedimiento para la obtenciën de derivados del imidazol
FI48082C (fi) 1966-08-05 1974-06-10 Boehringer Sohn Ingelheim Menetelmä uusien verenpainetta alentavien 2-aryylihydratsino-imidatsol iinien-(2) valmistamiseksi
US3377247A (en) 1967-04-28 1968-04-09 Dow Chemical Co Antidepressant method
US3586695A (en) 1968-01-26 1971-06-22 Dow Chemical Co Substituted imidazolinyl indoles
US3577415A (en) * 1968-12-23 1971-05-04 Robins Co Inc A H 1-substituted-3-substituted phenoxypyrrolidines
US3577428A (en) 1969-04-14 1971-05-04 Colgate Palmolive Co 2-amino-4-aryloxyalkyl-4-alkyl-2-oxazolines
BE754935A (fr) 1969-08-13 1971-02-17 Hoechst Ag 2-(thienyl-3'-amino)-1,3-diazacycloalcenes et leur preparation
US3818094A (en) 1969-08-28 1974-06-18 Boehringer Sohn Ingelheim Hypotensive pharmaceutical compositions containing certain 2-anilino-1,3-diazacyclopentenes-(2)
US3622579A (en) 1969-08-28 1971-11-23 Boehringer Sohn Ingelheim Derivatives of 2-anilino-1,3-diazacyclopentene-(2)
US3660423A (en) 1970-02-13 1972-05-02 Dow Chemical Co 2-(substituted benzyl)methyl-2-imidazolines
GB1333471A (en) 1971-01-27 1973-10-10 Labaz Imidazoline derivatives and process for preparing the same
DE2123246C2 (de) 1971-05-11 1982-11-25 Basf Ag, 6700 Ludwigshafen 6-[p-(β-Phenyläthylaminoacetylamino)-phenyl]-4,5-dihydropyridazon-(3)
DE2253555A1 (de) 1972-11-02 1974-05-09 Hoechst Ag Oxazolo-pyrimidine und verfahren zu ihrer herstellung
CH609558A5 (en) 1973-09-18 1979-03-15 Givaudan & Cie Sa Antibacterial composition
US3981814A (en) 1973-09-18 1976-09-21 Givaudan Corporation Bacteriostatic substituted benzanilide compositions and methods for their use
DE2446758C3 (de) 1974-10-01 1979-01-04 C.H. Boehringer Sohn, 6507 Ingelheim 2-(2-Fluor-6-trifluormethylphenylimino)-imidazolidin, dessen Säureadditionssalze, Verfahren zur Herstellung dieser Verbindungen und deren Verwendung bei der Bekämpfung der Hypertonie
US4125620A (en) 1974-10-01 1978-11-14 Boehringer Ingelheim Gmbh 2-[(2',6'-Disubstituted-phenyl)-imino]-imidazolidines and salts thereof
US3992403A (en) 1975-05-30 1976-11-16 Schering Corporation 2-Imidazolines and their use as hypoglycemic agents
GB1538097A (en) 1976-01-26 1979-01-10 Lafon Labor Substituted phenyl-amidines
DE2849537C2 (de) 1978-11-15 1983-03-17 Beiersdorf Ag, 2000 Hamburg Substituierte 5-(2-Imidazolin-2-yl)-aminopyrimidine, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
US4323570A (en) 1978-11-15 1982-04-06 Beiersdorf Aktiengesellschaft Substituted aminopyrimidines
AU518569B2 (en) 1979-08-07 1981-10-08 Farmos-Yhtyma Oy 4-benzyl- and 4-benzoyl imidazole derivatives
US4311840A (en) 1980-11-13 1982-01-19 E. R. Squibb & Sons, Inc. 2,3,6,7-Tetrahydro-2-thioxo-4H-oxazolo[3,2-a]-1,3,5 triazin-4-ones
US4735959A (en) 1981-01-10 1988-04-05 Dr. Karl Thomae Gmbh Carboxylic acid amides and pharmaceutical compositions containing them
DE3133887A1 (de) 1981-08-27 1983-03-10 Bayer Ag, 5090 Leverkusen 2-arylhydrazino-2-imidazoline, deren acylderivate, verfahren zu ihrer herstellung und ihre verwendung zur bekaempfung von endo- und ektoparasiten
ES8405770A1 (es) 1982-01-27 1984-06-16 Pfizer Un procedimiento para la preparacion de una composicion ectoparasiticida, especialmente acaricida, o antihelmintica.
DE3302021A1 (de) 1983-01-22 1984-07-26 Basf Ag, 6700 Ludwigshafen 6-aryl-4,5-dihydro-3(2h)-pyridazinone, ihre herstellung und verwendung
US4540705A (en) 1983-03-14 1985-09-10 Sterling Drug Inc. Antidepressant imidazolines and related compounds
EP0166937B1 (fr) 1984-06-06 1991-08-28 Abbott Laboratories Composés adrénergiques
DK302185A (da) 1984-07-05 1986-01-06 Rolland Sa A 2-amino-oxazoliner samt fremgangsmaade til deres fremstilling
JPS61233678A (ja) 1985-04-09 1986-10-17 Maruko Seiyaku Kk ベンジルピペラジン誘導体
US4665095A (en) 1985-12-11 1987-05-12 Abbott Laboratories Use of 2-[(3,5-dihalo-4-aminobenzyl)]imidazolines to stimulate alpha-1 adrenergic receptors and to treat nasal congestion
GB2215206B (en) 1988-02-29 1991-07-03 Farmos Oy 4-substituted imidazole derivatives useful in perioperative care
DE3830054A1 (de) 1988-09-03 1990-03-15 Boehringer Mannheim Gmbh Phenylamide - verfahren zu ihrer herstellung sowie diese verbindungen enthaltende arzneimittel
FR2645860B1 (fr) 1989-04-14 1991-07-26 Sarget Lab Nouvelles aryloxymethyl-5 amino-2 oxazolines, syntheses et applications therapeutiques
FI894911A0 (fi) 1989-10-17 1989-10-17 Farmos Oy En terapeutiskt vaerdefull foerening.
DE69127002T2 (de) 1990-01-31 1997-11-20 Fuji Photo Film Co Ltd Farbphotographisches Silberhalogenidmaterial
CA2211325C (fr) 1993-10-13 2006-08-15 H. Joseph Horacek Preparation de clonidine a liberation prolongee
EP0661266A1 (fr) 1993-12-27 1995-07-05 Toa Eiyo Ltd. Composés cycliques aminés substitués comme 5HT2 antagonistes
GB9425211D0 (en) 1994-12-14 1995-02-15 Ucb Sa Substituted 1H-imidazoles
DE19514579A1 (de) 1995-04-20 1996-10-24 Boehringer Ingelheim Kg Verwendung von alpha¶1¶¶L¶-Agonisten zur Behandlung der Harninkontinenz
US5610174A (en) 1995-06-02 1997-03-11 Synaptic Pharmaceutical Corporation Use of α1A -selective adrenoceptor agonists for the treatment of urinary incontinence
DE69612698T2 (de) * 1995-06-09 2001-12-06 Hoffmann La Roche Pyrimidindion-, Pyrimidintrion-, Triazindion-Derivate als alpha-1-adrenergische Rezeptorantagonisten
GB9520150D0 (en) 1995-10-03 1995-12-06 Orion Yhtymae Oy New imidazole derivatives
TR199900314T2 (xx) * 1996-08-15 1999-05-21 Schering Corporation Eter muskarinik antagonistleri.
US5969137A (en) 1996-09-19 1999-10-19 Virginia Commonwealth University Benzylamidine derivatives with serotonin receptor binding activity
GB9625145D0 (en) * 1996-12-03 1997-01-22 Smithkline Beecham Plc Novel compounds
NO980546L (no) 1997-02-11 1998-08-12 Lilly Co Eli Farmas°ytiske midler
US5866579A (en) 1997-04-11 1999-02-02 Synaptic Pharmaceutical Corporation Imidazole and imidazoline derivatives and uses thereof
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
US6184242B1 (en) 1997-09-04 2001-02-06 Syntex Usa (Llc) 2-(substituted-phenyl)amino-imidazoline derivatives
NZ331480A (en) * 1997-09-04 2000-02-28 F 2-(Arylphenyl)amino-imidazoline derivatives and pharmaceutical compositions
NZ504667A (en) 1997-12-04 2003-03-28 Allergan Sales Inc Substituted imidazole derivatives having agonist-like activity at alpha 2B or 2B/2C adrenergic receptors
US6841684B2 (en) 1997-12-04 2005-01-11 Allergan, Inc. Imidiazoles having reduced side effects
WO1999032112A1 (fr) 1997-12-19 1999-07-01 Eli Lilly And Company Methodes de traitement du diabete
CA2328973A1 (fr) 1998-04-23 1999-10-28 Akio Ojida Derives de naphtalene, leur production et utilisation
DE19826517B4 (de) 1998-06-15 2006-03-23 Baxter Healthcare S.A. Verfahren zur Herstellung von Filmtabletten mit Cyclophosphamid als Wirkstoff und daraus hergestellte Cyclophosphamid-Filmtablette
ES2150378B1 (es) 1998-08-07 2001-07-01 Esteve Labor Dr Empleo de derivados de aril(o heteroaril)azolilcarbinoles en la elaboracion de un medicamento para el tratamiento de los trastornos mediados por un exceso de substancia p.
CA2246027A1 (fr) 1998-08-27 2000-02-27 Virginia Commonwealth University Derives de benzylamidine avec activite de fixation provenant des recepteurs de la serotonine
AU771975B2 (en) * 1998-11-04 2004-04-08 Meiji Seika Kaisha Ltd. Picolinamide derivatives and pest controllers containing the same as the active ingredient
CN1206219C (zh) 1998-12-18 2005-06-15 布里斯托尔-迈尔斯斯奎布药品公司 作为趋化因子受体活性调节剂的n-脲基烷基-哌啶化合物
US6777428B1 (en) 1999-02-10 2004-08-17 Eli Lilly And Company 5-HT1f agonist
BR0009041A (pt) * 1999-03-17 2001-12-26 Astrazeneca Ab Derivado de amida, processo para a preparação deum derivado de amida, composição farmacêutica,uso de um derivado de amida, e, método paratratar doenças ou quadros clìnicos mediados porcitocinas
EP1177188B1 (fr) * 1999-05-12 2005-10-12 Ortho-McNeil Pharmaceutical, Inc. Carboxamides de pyrazole utiles pour le traitement de l'obesite et d'autres troubles
US6355660B1 (en) * 1999-07-20 2002-03-12 Dow Agrosciences Llc Fungicidal heterocyclic aromatic amides and their compositions, methods of use and preparation
PE20010781A1 (es) 1999-10-22 2001-08-08 Takeda Chemical Industries Ltd Compuestos 1-(1h-imidazol-4-il)-1-(naftil-2-sustituido)etanol, su produccion y utilizacion
JP2001151742A (ja) 1999-11-26 2001-06-05 Mitsui Chemicals Inc アニリド誘導体及びそれを含有する抗不整脈剤
FR2802533B1 (fr) 1999-12-17 2002-02-15 Sanofi Synthelabo Phenoxypropanolamines, leur preparation et leur application en therapeutique
JP2001302643A (ja) 2000-04-21 2001-10-31 Suntory Ltd 環状アミジン化合物
JO2654B1 (en) * 2000-09-04 2012-06-17 شركة جانسين فارماسوتيكا ان. في Multiple aryl caroxa amides are useful as lipid - lowering agents
WO2002022801A2 (fr) 2000-09-12 2002-03-21 Oregon Health & Science University Nouveaux genes de recepteurs mammaliens et leurs utilisations
HUP0303156A3 (en) 2000-11-14 2004-03-29 Hoffmann La Roche Substituted 2-phenylaminoimidazoline derivatives as ip antagonists, process for their preparation and pharmaceutical compositions containing them
US7141590B2 (en) 2000-12-29 2006-11-28 Ucb Sa Pharmaceutical uses and synthesis of nicotinanilide-N-oxides
US6656971B2 (en) 2001-01-25 2003-12-02 Guilford Pharmaceuticals Inc. Trisubstituted carbocyclic cyclophilin binding compounds and their use
US7429593B2 (en) 2001-09-14 2008-09-30 Shionogi & Co., Ltd. Utilities of amide compounds
IL147921A0 (en) 2002-01-31 2002-08-14 Abdulrazik Mohammad A method for treating central nervous system disorders by ocular dosing
MXPA04010441A (es) * 2002-04-23 2005-02-14 Shionogi & Co Derivado de pirazolo[1,5-a]pirimidina e inhibidor de nad(p)h oxidasa que contiene el mismo.
TW200930291A (en) 2002-04-29 2009-07-16 Bayer Cropscience Ag Pesticidal heterocycles
WO2003101444A1 (fr) 2002-05-29 2003-12-11 Millennium Pharmaceuticals, Inc. Composes et derives de diaryluree utilises comme inhibiteurs de chk-1 dans le traitement du cancer
UA77536C2 (en) * 2002-07-03 2006-12-15 Lundbeck & Co As H Secondary aminoaniline piperidines as mch1 antagonists and their use
KR100492252B1 (ko) 2002-08-09 2005-05-30 한국화학연구원 이미다졸을 포함하는 이차아민으로 치환된 벤조피란유도체 및 그의 제조방법
DE10250743A1 (de) 2002-10-31 2004-05-19 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Amid-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel
EP1569907B1 (fr) * 2002-12-13 2016-03-09 YM BioSciences Australia Pty Ltd Inhibiteurs de kinase a base de nicotinamide
EP1575918A2 (fr) * 2002-12-19 2005-09-21 Neurogen Corporation Analogues d'arylamide d'acide biphenyl-4-carboxylique substitues comme modulateurs du recepteur de la capsaicine
WO2004065370A1 (fr) * 2003-01-23 2004-08-05 Crystalgenomics, Inc. Inhibiteur de glycogene synthase kinase 3$g(b), composition et procede de preparation associe
US6933311B2 (en) 2003-02-11 2005-08-23 Abbott Laboratories Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
DE10306250A1 (de) 2003-02-14 2004-09-09 Aventis Pharma Deutschland Gmbh Substituierte N-Arylheterozyklen, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
CA2767153A1 (fr) 2003-02-20 2004-09-02 Encysive Pharmaceuticals Inc. Antagonistes du recepteur de l'urotensine-ii de la phenylenediamine et antagonistes du ccr-9
CN1777584A (zh) 2003-04-18 2006-05-24 伊莱利利公司 作为5-ht1f激动剂的(哌啶氧基)苯基、(哌啶氧基)吡啶基、(哌啶硫基)苯基和(哌啶硫基)吡啶基化合物
WO2005014554A1 (fr) 2003-08-08 2005-02-17 Astex Therapeutics Limited Composes 1h-indazole-3-carboxamide utilises comme modulateurs de la mapkap kinase
EP1680109A4 (fr) * 2003-10-07 2009-05-06 Renovis Inc Derives d'amide utilises comme ligands du canal ionique et compositions pharmaceutiques et methodes d'utilisation de ces derives
BRPI0415167A (pt) * 2003-10-07 2006-11-28 Renovis Inc composto de amina como ligandos de canal de ìon e usos dos mesmos
EP1678177B1 (fr) 2003-10-23 2007-11-28 F.Hoffmann-La Roche Ag Derives de triaza-spiropiperidine a utiliser comme inhibiteurs de glyt-1 dans le traitement de troubles neurologiques et neuropsychiatriques
JP4771468B2 (ja) * 2003-12-26 2011-09-14 正敏 萩原 Sr蛋白質のリン酸化制御方法、および、sr蛋白質の活性制御剤を有効成分とする抗ウイルス剤
WO2005087217A1 (fr) 2004-03-05 2005-09-22 The General Hospital Corporation Compositions et procedes pour moduler l'interaction entre des polypeptides
US7767674B2 (en) 2004-06-23 2010-08-03 Eli Lilly And Company Kinase inhibitors
CA2572874A1 (fr) 2004-07-02 2006-01-12 Sankyo Company Limited Derive d'uree
US20080261952A1 (en) 2004-08-16 2008-10-23 Jason Bloxham Aryl Urea Derivatives for Treating Obesity
DE102004039789A1 (de) * 2004-08-16 2006-03-02 Sanofi-Aventis Deutschland Gmbh Arylsubstituierte polycyclische Amine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
ZA200703383B (en) * 2004-09-29 2009-05-27 Mitsubishi Pharma Corp 6-(pyridinyl)-4-pyrimidone derivates as tau protein kinase 1 inhibitors
US20080076760A1 (en) 2004-11-10 2008-03-27 Wakamoto Pharmaceutical Co., Ltd 2,3,4,5-tetrahydro-1h-1,5-benzodiazepine derivative and medicinal composition
US20060111392A1 (en) 2004-11-23 2006-05-25 Wood Michael R Substituted biaryl-carboxylate derivatives
WO2006070878A1 (fr) 2004-12-28 2006-07-06 Astellas Pharma Inc. Derive d'acide carboxylique ou sel de ce derive
GB0611907D0 (en) 2006-06-15 2006-07-26 Glaxo Group Ltd Compounds
WO2006077425A1 (fr) 2005-01-21 2006-07-27 Astex Therapeutics Limited Combinaisons d'inhibiteurs de pyrazole kinase et d'autres agents antitumoraux
JP2008534685A (ja) 2005-04-05 2008-08-28 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 炎症性疾患の治療に有用な置換ベンジルイミダゾール
CN101212898A (zh) 2005-05-03 2008-07-02 拜尔农作物科学股份公司 杀虫的取代的氨基烷基杂环及杂芳基衍生物
WO2007003967A2 (fr) 2005-07-06 2007-01-11 Cambridge Semiconductor Limited Systemes de commande pour alimentation en mode commute
JP2007051121A (ja) 2005-07-22 2007-03-01 Taiho Yakuhin Kogyo Kk プロスタグランジンd合成酵素を阻害するピリミジン化合物
US20100152188A1 (en) 2005-08-05 2010-06-17 Akella Satya Surya Visweswara Srinivas Novel Heterocyclic Compounds
AR056043A1 (es) 2005-08-25 2007-09-12 Schering Corp Agonistas de receptores adrenergicos alfa2c funcionalmente selectivos
ATE478044T1 (de) 2005-09-16 2010-09-15 Arrow Therapeutics Ltd Biphenylderivate und ihre verwendung bei der behandlung von hepatitis c
KR20080059634A (ko) 2005-10-06 2008-06-30 유니버시티 오브 매사추세츠 Hiv 복제를 억제하기 위한 시약의 조성물 및 합성법
US20070197529A1 (en) 2005-12-01 2007-08-23 Viviana Braude Isolated desfluoro-linezolid, preparation thereof and its use as a reference marker and standard
JP2007191471A (ja) 2005-12-21 2007-08-02 Sankyo Co Ltd ウレア誘導体を含有する医薬
US20070254894A1 (en) 2006-01-10 2007-11-01 Kane John L Jr Novel small molecules with selective cytotoxicity against human microvascular endothelial cell proliferation
WO2007085556A2 (fr) 2006-01-27 2007-08-02 F. Hoffmann-La Roche Ag Utilisation de derives de 4-imidazole contre les troubles du snc
KR20090004976A (ko) 2006-04-19 2009-01-12 아스테라스 세이야쿠 가부시키가이샤 아졸카르복사미드 유도체
TW200808705A (en) * 2006-06-15 2008-02-16 Sanofi Aventis Aryl- and heteroaryl-ethyl-acylguanidine derivatives, their preparation and their application in therapeutics
DE602007006019D1 (de) * 2006-06-28 2010-06-02 Glaxo Group Ltd Für die behandlung von durch den gpr38-rezeptor vermittelten krankheiten geeignete piperazinylderivate
ES2381589T3 (es) 2006-10-19 2012-05-29 F. Hoffmann-La Roche Ag Aminometil-4-imidazoles
US9206142B2 (en) 2006-10-31 2015-12-08 Merck Sharp & Dohme Corp. Anilinopiperazine derivatives and methods of use thereof
EP2077839A2 (fr) 2006-11-03 2009-07-15 Arete Therapeutics, INC. Inhibiteurs époxyde hydrolase soluble pour le traitement de polyarthrite rhumatoïde
US8076332B2 (en) 2006-12-26 2011-12-13 Santen Pharmaceutical Co., Ltd. N- (2-aminophenyl) benzamide derivative having urea structure
US7470684B2 (en) * 2007-01-03 2008-12-30 Hoffmann-La Roche Inc. Spiropiperidine derivatives as NK3 antagonists
RU2473545C2 (ru) 2007-02-02 2013-01-27 Ф.Хоффманн-Ля Рош Аг Новые 2-аминооксазолины в качестве лигандов taar1 для заболеваний цнс
RU2460725C2 (ru) 2007-02-15 2012-09-10 Ф. Хоффманн-Ля Рош Аг Новые 2-аминооксазолины в качестве лигандов taar1
AU2008253118B2 (en) 2007-05-22 2013-11-21 Madrigal Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors
US8058299B2 (en) * 2007-05-22 2011-11-15 Via Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors
US8367686B2 (en) 2007-06-07 2013-02-05 Intra-Cellular Therapies, Inc. Heterocycle compounds and uses thereof
US8981094B2 (en) 2007-06-08 2015-03-17 Janssen Pharmaceutica N.V. Piperidine/piperazine derivatives
JO2972B1 (en) 2007-06-08 2016-03-15 جانسين فارماسوتيكا ان. في Piperidine / piperazine derivatives
BRPI0815038A2 (pt) 2007-08-02 2015-03-17 Hoffmann La Roche Uso de derivados de benzamida para o tratamento de transtornos do cns
JP5341084B2 (ja) 2007-08-03 2013-11-13 エフ.ホフマン−ラ ロシュ アーゲー Taar1リガンドとしてのピリジンカルボキシアミド及びベンズアミド誘導体
US8093428B2 (en) 2007-10-26 2012-01-10 Janssen Pharmaceutica N.V. Synthesis of quaternary salt compounds
CN101434570B (zh) 2007-11-16 2011-02-02 上海医药工业研究院 吡咯烷衍生物及其制备方法和应用
JP2011507910A (ja) 2007-12-21 2011-03-10 ユニバーシティー オブ ロチェスター 真核生物の寿命を変更するための方法
WO2010010014A1 (fr) 2008-07-24 2010-01-28 F. Hoffmann-La Roche Ag Dérivés de 4,5-dihydrooxazol-2-yle
EP2331518A1 (fr) * 2008-08-22 2011-06-15 Evotec AG Nouveaux antagonistes du récepteur de la bradykinine b1
JP5605844B2 (ja) 2008-10-17 2014-10-15 塩野義製薬株式会社 血管内皮リパーゼ阻害活性を有する酢酸アミド誘導体
US8415333B2 (en) 2009-02-24 2013-04-09 Respiratorious Ab Bronchodilating diazaheteroaryls
EP2411526A4 (fr) 2009-03-27 2012-09-19 Zacharon Pharmaceuticals Inc Modulateurs de la biosynthèse des gangliosides
JP5381257B2 (ja) 2009-04-09 2014-01-08 ユニマテック株式会社 含フッ素ボロン酸エステル化合物の製造方法
WO2010118347A2 (fr) 2009-04-10 2010-10-14 Zacharon Pharmaceuticals, Inc. Modulateurs de la biosynthèse de o-glycanes
EP2493875B1 (fr) * 2009-10-27 2014-08-06 Boehringer Ingelheim International GmbH Composés hétérocycliques utilisés en tant qu'antagonistes des récepteurs ccr1
US9452980B2 (en) 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides

Also Published As

Publication number Publication date
TWI409261B (zh) 2013-09-21
IL219437A0 (en) 2012-06-28
JP2016041740A (ja) 2016-03-31
IL219437A (en) 2015-07-30
ZA201203137B (en) 2013-01-30
KR101461296B1 (ko) 2014-11-12
TW201130828A (en) 2011-09-16
BR112012015168B1 (pt) 2021-11-03
SG181874A1 (en) 2012-07-30
AR079542A1 (es) 2012-02-01
UA113141C2 (xx) 2016-12-26
MX2012007409A (es) 2012-07-17
ECSP12011999A (es) 2012-07-31
US20200048194A1 (en) 2020-02-13
JP6109575B2 (ja) 2017-04-05
CA2780161C (fr) 2017-09-26
JP2013515026A (ja) 2013-05-02
AU2010335277A1 (en) 2012-06-07
AU2010335277B2 (en) 2016-07-07
EP3187490B1 (fr) 2022-04-06
PE20121395A1 (es) 2012-10-26
US11697636B2 (en) 2023-07-11
EP3187490A1 (fr) 2017-07-05
CN102686563A (zh) 2012-09-19
RU2012129737A (ru) 2014-01-27
RU2595902C2 (ru) 2016-08-27
KR20120110123A (ko) 2012-10-09
MY176030A (en) 2020-07-22
CL2012001673A1 (es) 2012-11-23
US9452980B2 (en) 2016-09-27
CN105254623A (zh) 2016-01-20
CR20120275A (es) 2012-07-04
BR112012015168A2 (pt) 2016-03-29
US20210061760A1 (en) 2021-03-04
WO2011076678A1 (fr) 2011-06-30
JP6567393B2 (ja) 2019-08-28
CA2780161A1 (fr) 2011-06-30
US20160264596A1 (en) 2016-09-15
CO6531470A2 (es) 2012-09-28
US20110152245A1 (en) 2011-06-23
US10501411B2 (en) 2019-12-10
EP2516392A1 (fr) 2012-10-31
NZ599577A (en) 2014-05-30

Similar Documents

Publication Publication Date Title
MA33855B1 (fr) Dérivés de benzamide substitués
MA35192B1 (fr) Derives de pyrazole
MA32486B1 (fr) Derives de 4,5- dihydrooxazol-2-yle
MA31165B1 (fr) Nouvelles 2-aminooxazolines servant de ligands du taar1 pour des troubles du snc
CN104136413B (zh) 用于预防或治疗癫痫症的苯基氨基甲酸酯化合物
CN101096348A (zh) 新萘化合物、其制备方法及其药物组合物
MA42442B1 (fr) Dérivés d'éthynyle comme modulateurs du récepteur métabotropique au glutamate
MA35062B1 (fr) Dérivés d'amines hétérocycliques
MA35194B1 (fr) Derives de benzamide substitues
EP3409658B1 (fr) Dérivé de tétrahydronaphtalène
MA38012B1 (fr) Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5
MA35133B1 (fr) Dérivés d'éthynyle comme modulateurs allostériques positifs de mglur5
NO20091936L (no) 4-imidazoliner som TAAR ligander
MX2009005920A (es) Nuevos 2-imidazoles como ligandos para receptores asociados con trazas de amina.
RU2006105779A (ru) Индол-5-ильные сульфонамидные производные, их получение и их применение в качестве модуляторов 5-нт-6
MA37944A1 (fr) Dérivés de pyrazole-carboxamide en tant que modulateurs de taar pour utilisation dans le traitement de plusieurs troubles, tels que la dépression, le diabète et la maladie de parkinson
KR20050075281A (ko) 씨엔에스 질병의 치료를 위한 도파민-디3 리간드로서헤테로아렌 카복스아미드의 용도
EP0447292A1 (fr) Dérivés de 4-(aminométhyl)pipéridine, leur préparation et leur application en thérapeutique
EP2516383A1 (fr) Nouveaux dérivés d'aminotétraline
EP2234966B1 (fr) Derives d'azetidines, leur preparation et leur application en therapeutique
MX2009004617A (es) 2-imidazoles sustituidos como moduladores de los receptores asociados con trazas de amina.
WO2016055482A1 (fr) Dérivés d'isoindoline
WO2007090720A3 (fr) Utilisation de 2-imidazoles pour le traitement de troubles du système nerveux central
EP2077837A2 (fr) Derives de pyrrolizine, indolizine et quinolizine, leur preparation et leur application en therapeutique.
BG62349B2 (bg) N-заместени производни на 3-азабицикло/3.2.0/хептан като невролептици