ME02402B - Derivati azola - Google Patents

Derivati azola

Info

Publication number
ME02402B
ME02402B MEP-2016-102A MEP2016102A ME02402B ME 02402 B ME02402 B ME 02402B ME P2016102 A MEP2016102 A ME P2016102A ME 02402 B ME02402 B ME 02402B
Authority
ME
Montenegro
Prior art keywords
ethyl
phenyl
acetamide
propan
triazol
Prior art date
Application number
MEP-2016-102A
Other languages
German (de)
English (en)
French (fr)
Inventor
Mitsukane Yoshinaga
Takeshi Kuwada
Naoki Miyakoshi
Tomoko Ishizaka
Daisuke Wakasugi
Shin-Ichi Shirokawa
Nobutaka Hattori
Youichi Shimazaki
Original Assignee
Taisho Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Taisho Pharmaceutical Co Ltd filed Critical Taisho Pharmaceutical Co Ltd
Publication of ME02402B publication Critical patent/ME02402B/me

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/44—Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members
    • C07D207/444—Heterocyclic 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 three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/70—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/12—Oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic 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
    • C07D263/32—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/10—Heterocyclic 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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/10—Heterocyclic 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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Psychology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Predmetni pronalazak se odnosi na jedinjenje saskeletom azola koje ima antagonističko dejstvo prema arginin-vazopresinskom(AVP) receptoru V1b, kao i na farmaceutske preparate koji sadrže navedenojedinjenje kao aktivni sastojak, posebno na sredstva za lečenje ili prevencijubolesti kao što su poremećaji raspoloženja (uključujući depresiju), anksiozni poremećaj,šizofrenija, Alchajmerova bolest, Parkinsonova bolest, Hantingtonova horeja,poremećaj ishrane, hipertenzija, gastrointestinalna bolest, zavisnost odnarkotika, epilepsija, cerebralni infarkt, cerebralna ishemija, cerebralniedem, povreda glave, zapaljenje, bolesti u vezi sa imunim sistemom i alopecija.

Claims (12)

1. Derivat azola predstavljen formulom (I): naznačen time što u formuli I R1 predstavlja atom vodonika, C1-5 alkil grupu (gde je navedena C1-5 alkil grupa opciono supstituisana jednom do trima grupama izabranim iz grupe koja se sastoji od hidroksi grupe, halogenih atoma, cijano, C3-7 cikloalkil i C1-5 alkoksi grupa), C3-7 cikloalkil grupu ili 4- do 8-člani zasićeni heterociklični prsten; R2 predstavlja atom vodonika ili C1-5 alkil grupu; R3 predstavlja aril ili heteroaril grupu (gde je navedena aril ili heteroaril grupa opciono supstituisana jednom ili dvema grupama izabranim iz grupe koja se sastoji od C1-5 alkoksi, C1-5 alkil grupe, halogenih atoma, trifluormetil, trifluormetoksi, cijano, hidroksi, difluormetoksi i C1-5 alkilsulfonil grupa); R4 i R5, koji mogu da budu isti ili različiti, predstavljaju, svaki za sebe, vodonikov atom, C1-5 alkil grupu (gde je navedena C1-5 alkil grupa opciono supstituisana jednom do trima grupama izabranim iz grupe koja se sastoji od hidroksi grupe, halogenih atoma, cijano, C3-7 cikloalkil i C1-5 alkoksi grupa), C3-7 cikloalkil grupu ili 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten koji sadrži jedan ili više azotovih, kiseonikovih ili sumporovih atoma u prstenu (navedeni 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten opciono je supstituisan jednom ili dvema grupama izabranim iz grupe koja se sastoji od hidroksi, C1-5 alkil, C1-5 alkoksi grupa, halogenih atoma, cijano, C2-5 alkanoil i trifluormetil grupa); ili R4 i R5, zajedno sa susednim atomom azota, grade 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten koji opciono sadrži jedan ili veći broj azotovih, kiseonikovih ili sumporovih atoma u prstenu uz navedeni susedni azotov atom (navedeni 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten opciono je supstituisan jednom ili dvema grupama izabranim iz grupe koja se sastoji od hidroksi, C1-5 alkil (gde je navedena C1-5 alkil grupa opciono supstituisana jednom ili dvema hidroksilnim grupama), C1-5 alkoksi grupa, halogenih atoma, cijano, C2-5 alkanoil, okso, aminokarbonil, mono-C1-5 alkilaminokarbonil, di-C1-5 alkilaminokarbonil, trifluormetil, amino, mono-C1-5 alkilamino, di-C1-5 alkilamino i C2-5 alkanoilamino grupa, a navedeni 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten opciono sadrži C1-5 alkilensku grupu koja unakrsno povezuje dva različita ugljenikova atoma u prstenu), ili grade 2-oksa-6-azaspiro[3.3]hept-6-il ili 7-oksa-2-azaspiro[3.5]non-2-il; opciono supstituisani azolov prsten koji je predstavljen sledećom formulom (�): ima bilo koju od struktura iz sledeće grupe formula (II): gde Ry predstavlja atom vodonika ili C1-5 alkil grupu; X1 i X2 su takvi da i) kada je X1 prosta veza ili formula -CO-, X2 predstavlja -C1-5 alkilen ili -O-C1-5 alkilen grupu; i ii) kada je X1 formula -CONRx1, X2 predstavlja prostu vezu; Rx1 predstavlja atom vodonika ili C1-5 alkil grupu; i prsten A predstavlja benzenov prsten, 6-člani aromatični heterociklični prsten (gde su navedeni benzenov i 6-člani aromatični heterociklični prsten opciono supstituisani jednom ili dvema grupama izabranim iz grupe koja se sastoji od halogenih atoma i C1-5 alkoksi grupe), 4- do 8-člani zasićeni ili delimično nezasićeni heterociklični prsten koji sadrži jedan ili dva azotova atoma (gde je navedeni 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten opciono supstituisan jednom okso grupom) ili C3-7 cikloalkan], ili farmaceutski prihvatljiva so navedenog derivata azola.
2. Derivat azola ili njegova farmaceutski prihvatljiva so prema prema patentnom zahtevu 1, naznačena time što u prethodnoj formuli (I), R4 i R5, koji mogu da budu isti ili različiti, predstavljaju, svaki za sebe, vodonikov atom, C1-5 alkil grupu (gde je navedena C1-5 alkil grupa opciono supstituisana jednom do trima grupama izabranim iz grupe koja se sastoji od hidroksi grupe, halogenih atoma, cijano, C3-7 cikloalkil i C1-5 alkoksi grupa), C3-7 cikloalkil grupu ili 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten koji sadrži jedan ili više azotovih, kiseonikovih ili sumporovih atoma u prstenu (navedeni 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten opciono je supstituisan jednom ili dvema grupama izabranim iz grupe koja se sastoji od hidroksi, C1-5 alkil, C1-5 alkoksi grupa, halogenih atoma, cijano, C2-5 alkanoil i trifluormetil grupa); ili R4 i R5, zajedno sa susednim atomom azota, grade 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten koji opciono sadrži jedan ili veći broj azotovih, kiseonikovih ili sumporovih atoma u prstenu uz navedeni susedni azotov atom (navedeni 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten opciono je supstituisan jednom ili dvema grupama izabranim iz grupe koja se sastoji od hidroksi, C1-5 alkil (gde je navedena C1-5 alkil grupa opciono supstituisana jednom ili dvema hidroksilnim grupama), C1-5 alkoksi grupa, halogenih atoma, cijano, C2-5 alkanoil, okso, aminokarbonil, mono-C1-5 alkilaminokarbonil, di-C1-5 alkilaminokarbonil i trifluormetil grupa, a navedeni 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten opciono sadrži C1-5 alkilensku grupu koja unakrsno povezuje dva različita ugljenikova atoma u prstenu), ili grade 2-oksa-6-azaspiro[3.3]hept-6-il ili 7-oksa-2-azaspiro[3.5]non-2-il.
3. Derivat azola ili njegova farmaceutski prihvatljiva so prema prema patentnim zahtevima 1 ili 2, naznačena time što u prethodnoj formuli (I), X1 predstavlja prostu vezu; X2 predstavlja -C1-5 alkilen ili -O-C1-5 alkilen grupu; i prsten A predstavlja benzenov prsten, 6-člani aromatični heterociklični prsten (gde su navedeni benzenov i 6-člani aromatični heterociklični prsten opciono supstituisani jednom ili dvema grupama izabranim iz grupe koja se sastoji od halogenih atoma i C1-5 alkoksi grupe) ili 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten koji sadrži jedan ili dva azotova atoma (gde je navedeni 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten opciono supstituisan jednom okso grupom).
4. Derivat azola ili njegova farmaceutski prihvatljiva so prema prema bilo kom od patentnih zahteva 1 do 3, naznačena time što u prethodnoj formuli (I), prsten A predstavlja benzenov prsten ili 6-člani aromatični heterociklični prsten (gde su navedeni benzenov i 6-člani aromatični heterociklični prsten opciono supstituisani jednom ili dvema grupama izabranim iz grupe koja se sastoji od halogenih atoma i C1-5 alkoksi grupe).
5. Derivat azola ili njegova farmaceutski prihvatljiva so prema prema bilo kom od patentnih zahteva 1 do 4, naznačena time što u prethodnoj formuli (I), prsten A predstavlja benzenov prsten ili piridinski prsten (gde su navedeni benzenov prsten i piridinski prsten opciono supstituisani jednom ili dvema grupama izabranim iz grupe koja se sastoji od halogenih atoma i C1-5 alkoksi grupe).
6. Derivat azola ili njegova farmaceutski prihvatljiva so prema prema bilo kom od patentnih zahteva 1 do 5, naznačena time što u prethodnoj formuli (I), R1 predstavlja C1-5 alkil grupu; R2 je atom vodonika; i R3 predstavlja fenil ili piridil grupu (gde je navedena fenil ili piridil grupa opciono supstituisana jednom ili dvema grupama izabranim iz grupe koja se sastoji od C1-5 alkil, C1-5 alkoksi grupe, halogenih atoma, cijano, trifluormetil, difluormetoksi, trifluormetoksi i C1-5 alkilsulfonil grupa);
7. Derivat azola ili njegova farmaceutski prihvatljiva so prema prema bilo kom od patentnih zahteva 1 do 6, naznačena time što u prethodnoj formuli (I), opciono supstituisani azolov prsten koji je predstavljen sledećom formulom (�): ima bilo koju od struktura iz sledeće grupe formula (III): gde Ry predstavlja atom vodonika ili metil grupu.
8. Derivat azola ili njegova farmaceutski prihvatljiva so prema prema bilo kom od patentnih zahteva 1 do 7, naznačena time što u prethodnoj formuli (I), X1 predstavlja prostu vezu; X2 je etilen ili metilen grupa; i R4 i R5, zajedno sa susednim atomom azota, grade 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten koji opciono sadrži jedan ili veći broj azotovih, kiseonikovih ili sumporovih atoma u prstenu uz navedeni susedni azotov atom (navedeni 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten opciono je supstituisan jednom ili dvema grupama izabranim iz grupe koja se sastoji od hidroksi, C1-5 alkil (gde je navedena C1-5 alkil grupa opciono supstituisana jednom ili dvema hidroksilnim grupama), C1-5 alkoksi grupa, halogenih atoma, cijano, C2-5 alkanoil, i trifluormetil grupa, a navedeni 4- do 8-člani zasićeni ili nezasićeni heterociklični prsten opciono sadrži C1-5 alkilensku grupu koja unakrsno povezuje dva različita ugljenikova atoma u prstenu), ili grade 2-oksa-6-azaspiro[3.3]hept-6-il.
9. Derivat azola ili njegova farmaceutski prihvatljiva so prema prema bilo kom od patentnih zahteva 1 do 8, naznačena time što u prethodnoj formuli (I), R4 i R5, zajedno sa susednim atomom azota, grade 5- ili 6-člani zasićeni heterociklični prsten koji opciono sadrži jedan ili veći broj kiseonikovih atoma u prstenu uz navedeni susedni azotov atom (navedeni 6-člani zasićeni heterociklični prsten opciono je supstituisan jednom ili dvema grupama izabranim iz grupe koja se sastoji od hidroksilne i C1-5 alkil grupe, i navedeni 6-člani zasićeni heterociklični prsten opciono sadrži C1-5 alkilensku grupu koja unakrsno povezuje dva različita ugljenikova atoma u prstenu), ili grade 2-oksa-6-azaspiro[3.3]hept-6-il.
10. Derivat azola ili njegova farmaceutski prihvatljiva so prema prema patentnom zahtevu 1, naznačena time što je derivat azola predstavljen formulom (I) izabran iz grupe koja se sastoji od: 2-[2-(3-hlorfenil)-4-{4-[2-(piperidin-1-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(3-hlorfenil)-4-{4-[2-(morfolin-4-il)etil]fernil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(3-hlorfenil)-4-(4-{2-[3-(hidroksimetil)pirolidin-1-il]etil}fenil)-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(3-hlorfenil)-4-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(4-fluor-3-metoksifenil)-4-{4-[2-(piperidin-1-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(4-fluor-3-metoksifenil)-4-{4-[2-(morfolin-4-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(4-fluor-3-metoksifenil)-4-{4-(2-(pirolidin-1-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(4-fluor-3-metoksifenil)-4-(4-{2-[(2R)-2-metilpirolidin-1-il]etil}fenil)-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(4-fluor-3-metoksifenil)-4-{4-[2-(3-hidroksi-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(4-fluor-3-metoksifenil)-4-{4-[2-(3-metoksipiperidin-1-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[4-{4-[2-(2,6-dimetilmorfolin-4-il)etil]fenil}-2-(4-fluor-3-metoksifenil)-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(4-fluor-3-metoksifenil)-4-{4-[2-(3-metilpirolidin-1-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(4-fluor-3-metoksifenil)-4-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(4-fluor-3-metoksifenil)-4-{4-[2-(1,4-oksazepan-4-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[4-{4-[2-(3,5-dimetilmorfolin-4-il)etil]fenil}-2-(4-fluor-3-metoksifenil)-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(3-hlorfenil)-4-{5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(3-hlorfenil)-4-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(3-hlorfenil)-4-{6-[2-(morfolin-4-il)etil]piridin-3-il}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(3-metoksifenil)-5-metil-4-{4-[2-(morfolin-4-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(3-metoksifenil)-4-{4-[2-(morfolin-4-il)etil)fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-(2-(3-hlor-4-fluorfenil)-4-{4-[2-(morfolin-4-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(3-metoksifenil)-4-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(3-hlorfenil)-4-{2-fluor-4-[2-(morfolin-4-il)etil)fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[2-(3-hlorfenil)-4-{4-[2-(morfolin-4-il)propil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[5-(3-hlorfenil)-3-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[5-(3-hlorfenil)-3-{4-[2-(morfolin-4-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[5-(3-hlorfenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[5-(3-metoksifenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[5-(4-fluor-3-metoksifenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; N-terc-butil-2-[5-(3-metoksifenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]acetamida; 2-[5-(3-hlor-4-fluorfenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; N-terc-butil-2-[5-(3-hlorfenil)-3-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]acetamida; 2-[5-(3-hlorfenil)-3-{5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; N-terc-butil-2-[5-(3-hlorfenil)-3-{5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]acetamida; 2-[5-(3-hlor-4-fluorfenil)-3-{5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[5-(4-fluor-3-metoksifenil)-3-{5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; N-terc-butil-2-[5-(3-metoksifenil)-3-{5-[2-(morfolin-4-il)etil]piridin-2-il}-1H-1,2,4-triazol-1-il]acetamida; 2-[5-(3-metoksifenil)-3-{4-[2-(morfolin-4-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[5-(3-metoksifenil)-3-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[3-(2-fluor-4-[2-(morfolin-4-il)etil]fenil}-5-(3-metoksifenil)-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[3-{3-fluor-4-[2-(morfolin-4-il)etil]fenil}-5-(3-metoksifenil)-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[5-(3-metoksifenil)-3-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[5-(3-metoksifenil)-3-{4-[2-(7-oksa-2-azaspiro[3.5]non-2-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[5-(3-metoksifenil)-3-{4-[2-(2-oksa-6-azaspiro[3.3]hept-6-il)etil]fenil}-1H-1,2,4-triazol-1-il]-N-(propan-2-il)acetamida; 2-[1-(3-hlorfenil)-3-{4-[2-(morfolin-4-il)etil]fenil}-1H-1,2,4-triazol-5-il]-N-(propan-2-il)acetamida; 2-[1-(3-hlorfenil)-3-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-1H-1,2,4-triazol-5-il]-N-(propan-2-il)acetamida; 2-[5-(3-hlorfenil)-3-{4-[2-(morfolin-4-il)etil]fenil}-2-okso-2,3-dihidro-1H-imidazol-1-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlorfenil)-2-{4-[2-(piperidin-1-il)etil]fenil}-1,3-oksazol-5-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlorfenil)-2-{4-[2-(morfolin-4-il)etil]fenil}-1,3-oksazol-5-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlorfenil)-2-{4-[2-(2-oksa-6-azaspiro[3.3]hept-6-il)etil]fenil}-1,3-oksazol-5-il]-N-(propan-2-il)acetamida; 2-[5-(3-hlorfenil)-2-{4-[2-(piperidin-1-il)etil]fenil}-1,3-tiazol-4-il]-N-(propan-2-il)acetamida; 2-[5-(3-hlorfenil)-2-{4-[2-(morfolin-4-il)etil]fenil}-1,3-tiazol-4-il]-N-(propan-2-il)acetamida; 2-[3-(3-hlorfenil)-1-{4-[2-(piperidin-1-il)etil]fenil}-1H-pirazol-4-il]-N-(propan-2-il)acetamida; 2-[3-(3-hlorfenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-1H-pirazol-4-il]-N-(propan-2-il)acetamida; 2-[5-(3-hlorfenil)-3-{4-[2-(morfolin-4-il)etil]fenil}-1H-pirazol-1-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlorfeni])-1-{4-[2-(morfolin-4-il)etil]fenil}-2,5-diokso-2,5-dihidro-1H-pirol-3-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlorfenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlorfenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; N-terc-butil-2-[4-(4-fluor-3-metoksifenil)-1-{4-[2-(morfolin-4-it)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamida; N-terc-butil-2-[4-(3-metoksifenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamida; N-terc-butil-2-[4-(3-metoksifenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamida; N-terc-butil-2-[4-(4-fluor-3-metoksifenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamida; N-terc-butil-2-[4-(4-fluor-3-metoksifenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamida; N-terc-butil-2-[4-(3-hlorfenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamida; N-terc-butil-2-[4-(3-hlorfenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamida; 2-[4-(3-hlorfenil)-1-{4-[2-(morfolin-4-il)propil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlorfenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlorfenil)-1-{3-fluor-4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlorfenil)-1-{3-fluor-4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlorfenil)-1-{3-metoksi-4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlorfenil)-1-{3-metoksi-4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlor-4-fluorfenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlor-4-fluorfenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; N-terc-butil-2-[4-(3-hlor-4-fluorfenil)-1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamida; N-terc-butil-2-[4-(3-hlor-4-fluorfenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamida; N-terc-butil-2-[4-(3-hlor-4-fluorfenil)-1-{5-[2-(morfolin-4-il)etil]piridin-2-il}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamida; N-terc-butil-2-[4-(3-hlor-4-fluorfenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]piridin-2-il}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]acetamida; 2-[4-(3-hlorfenil)-1-{5-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]piridin-2-il}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-(1-{4-[2-(morfolin-4-il)etil]fenil}-5-okso-4-[3-(trifluormetil)fenil]-4,5-dihidro-1H-1,2,4-triazol-3-il)-N-(propan-2-il)acetamida; 2-[4-(3-hlor-4-fluorfenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)propil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(4-fluor-3-metoksifenil)-1-{4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil)-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(4-fluor-3-metoksifenil)-1-{3-metoksi-4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[1-{3-metoksi-4-[2-(3-oksa-8-azabiciklo[3.2.1]okt-8-il)etil]fenil}-4-(3-metoksifenil)-5-okso-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlor-4-fluorfenil)-5-okso-1-{4-[2-(pirolidin-1-il)etil]fenil}-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; 2-[4-(3-hlor-4-fluorfenil)-5-okso-1-{4-[2-(piperidin-1-il)etil]fenil}-4,5-dihidro-1H-1,2,4-triazol-3-il]-N-(propan-2-il)acetamida; i 2-[2-(3-hlorfenil)-4-{4-[2-(2-oksa-6-azaspiro[3.3]hept-6-il)etil]fenil}-1H-imidazol-1-il]-N-(propan-2-il)acetamida.
11. Farmaceutski preparat naznačen time što sadrži navedeni derivat azola ili njegovu farmaceutski prihvatljivu so iz bilo kog od patentnih zahteva 1 do 10 kao aktivni sastojak.
12. Sredstvo za lečenje ili prevenciju bolesti kao što su poremećaj raspoloženja, anksiozni poremećaj, šizofrenija, Alchajmerova bolest, Parkinsonova bolest, Hantingtonova horeja, poremećaj ishrane, hipertenzija, gastrointestinalna bolest, zavisnost od narkotika, epilepsija, cerebralni infarkt, cerebralna ishemija, cerebralni edem, povreda glave, zapaljenje, bolesti u vezi sa imunim sistemom i alopecija, naznačeno time što sadrži derivat azola ili njegovu farmaceutski prihvatljivu iz bilo kog od patentnih zahteva 1 do 10 kao aktivni sastojak.
MEP-2016-102A 2011-10-27 2012-10-25 Derivati azola ME02402B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2011236487 2011-10-27
EP12843663.1A EP2772482B1 (en) 2011-10-27 2012-10-25 Azole derivative
PCT/JP2012/077541 WO2013062027A1 (ja) 2011-10-27 2012-10-25 アゾール誘導体

Publications (1)

Publication Number Publication Date
ME02402B true ME02402B (me) 2016-09-20

Family

ID=48167853

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2016-102A ME02402B (me) 2011-10-27 2012-10-25 Derivati azola

Country Status (28)

Country Link
US (1) US9522914B2 (me)
EP (1) EP2772482B1 (me)
JP (1) JP6025066B2 (me)
KR (1) KR101998442B1 (me)
CN (1) CN103889951B (me)
AU (1) AU2012329965B2 (me)
BR (1) BR112014009927B1 (me)
CA (1) CA2853227C (me)
CY (1) CY1118021T1 (me)
DK (1) DK2772482T3 (me)
ES (1) ES2568882T3 (me)
HR (1) HRP20160421T1 (me)
HU (1) HUE028799T2 (me)
IL (1) IL232217A (me)
ME (1) ME02402B (me)
MX (1) MX339763B (me)
MY (1) MY168930A (me)
PH (1) PH12014500921A1 (me)
PL (1) PL2772482T3 (me)
PT (1) PT2772482E (me)
RS (1) RS54825B1 (me)
RU (1) RU2622639C2 (me)
SG (1) SG11201401766UA (me)
SI (1) SI2772482T1 (me)
SM (1) SMT201600153B (me)
TW (1) TWI543971B (me)
WO (1) WO2013062027A1 (me)
ZA (1) ZA201403000B (me)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2011308403B2 (en) * 2010-10-01 2014-08-21 Taisho Pharmaceutical Co., Ltd. 1,2,4-triazolone derivative
JP6387669B2 (ja) * 2013-04-26 2018-09-12 大正製薬株式会社 アゾール誘導体を含有する医薬
US9663457B2 (en) * 2014-04-09 2017-05-30 Allergan, Inc. Carbamoyl hydrazine derivatives as formyl peptide modulators
CN109879859B (zh) 2015-07-06 2022-01-25 吉利德科学公司 Cot调节剂及其使用方法
US20190297887A1 (en) 2016-07-12 2019-10-03 Bayer Cropscience Aktiengesellschaft Bicyclic compounds as pesticides
CN106831713B (zh) * 2017-01-13 2019-04-02 深圳大学 一种多靶点Aβ寡聚化抑制剂的合成方法及应用
CN106831712B (zh) * 2017-01-13 2019-04-02 深圳大学 一种多靶点Aβ寡聚化抑制剂
CN107434778A (zh) * 2017-05-23 2017-12-05 重庆文理学院 一种4‑羟基‑2h‑吡咯‑2‑酮衍生物的制备方法
CN107857729B (zh) * 2017-12-25 2019-10-15 福州大学 一种4-碘化-n-芳基化的吡唑类化合物的合成方法
US10039749B1 (en) 2018-01-15 2018-08-07 King Saud University Substituted pyrazole derivatives
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
TWI770527B (zh) 2019-06-14 2022-07-11 美商基利科學股份有限公司 Cot 調節劑及其使用方法
RU2730492C1 (ru) * 2019-12-27 2020-08-24 Федеральное государственное бюджетное образовательное учреждение высшего образования "Российский химико-технологический университет имени Д.И. Менделеева" Способ получения алкил 2-[([1,1'-бифенил]-4-карбонил)амино]-3-(1н-азол-1-ил) пропаноатов
WO2021187486A1 (ja) * 2020-03-17 2021-09-23 大日本住友製薬株式会社 オキサジアゾール誘導体
EP4126231A1 (en) 2020-03-30 2023-02-08 Gilead Sciences, Inc. Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound
CN115397824B (zh) 2020-04-02 2024-10-22 吉利德科学公司 用于制备cot抑制剂化合物的方法

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000063363A (ja) * 1998-08-12 2000-02-29 Yamanouchi Pharmaceut Co Ltd 新規なトリアゾール誘導体
FR2804114B1 (fr) 2000-01-25 2002-03-08 Sanofi Synthelabo Nouveaux derives de 1,3-dihydro-2h-indol-2-one, un procede pour leur preparation et les compositions pharmaceutiques en contenant
EP1659121A4 (en) 2003-08-28 2008-11-26 Taisho Pharmaceutical Co Ltd 1,3-dihydro-2H-indol-2-one derivative
US20050070718A1 (en) 2003-09-30 2005-03-31 Abbott Gmbh & Co. Kg Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them
MX2007001986A (es) 2004-08-26 2007-05-10 Pfizer Compuestos de aminoheteroarilo como inhibidores de proteina quinasa.
AR052342A1 (es) * 2004-12-21 2007-03-14 Janssen Pharmaceutica Nv Derivados sustituidos de triazolona,tetrazolona e imidazolona con actividad selectiva antagonista de alfa2c-adenoreceptores
TW200643015A (en) 2005-03-11 2006-12-16 Akzo Nobel Nv 2-(4-oxo-4H-quinazolin-3-yl)acetamide derivatives
AU2006227199A1 (en) 2005-03-22 2006-09-28 Azevan Pharmaceuticals, Inc. Beta-lactamylalkanoic acids for treating premenstrual disorders
JP5002592B2 (ja) 2005-06-07 2012-08-15 フアーマコペイア・インコーポレイテツド うつ病およびストレス疾患のためのアジノンおよびジアジノンｖ３阻害剤
WO2007109098A2 (en) 2006-03-16 2007-09-27 Azevan Pharmaceuticals, Inc. HYDROXY AND KETO-SUBSTITUTED β-LACTAMYL ALKANEDIOIC ACIDS
DE102006024024A1 (de) 2006-05-23 2007-11-29 Bayer Healthcare Aktiengesellschaft Substituierte Arylimidazolone und -triazolone sowie ihre Verwendung
EP2061769A1 (en) 2006-08-26 2009-05-27 Abbott GmbH & Co. KG Substituted benzimidazolone derivatives, medicaments comprising them and their use
US7820649B2 (en) 2006-09-11 2010-10-26 N.V. Organon Quinazolinone and isoquinolinone acetamide derivatives
ATE523493T1 (de) 2006-09-11 2011-09-15 Organon Nv 2-(1-oxo-1h-isochinolin-2-yl) acetamid-derivate
JP2010229035A (ja) * 2007-08-01 2010-10-14 Taisho Pharmaceutical Co Ltd ピリドピリミジン−４−オン誘導体
WO2009130232A1 (en) * 2008-04-24 2009-10-29 Glaxo Group Limited Pyrazolo [1, 5 -a] pyrazine derivatives as antagonists of v1b receptors
WO2009130231A1 (en) 2008-04-24 2009-10-29 Glaxo Group Limited Pyrrolo [1, 2-a] pyrazine derivatives as vasopressin vib receptor antagonists
JP5369721B2 (ja) * 2009-01-30 2013-12-18 大正製薬株式会社 ピリドピリミジン−４−オン誘導体
DE102009013642A1 (de) * 2009-03-18 2010-09-23 Bayer Schering Pharma Aktiengesellschaft Substituierte Phenylalaninderivate und deren Verwendung
JP2013075830A (ja) 2010-02-03 2013-04-25 Taisho Pharmaceutical Co Ltd キノリン誘導体
CA2791100C (en) * 2010-02-27 2018-01-30 Bayer Intellectual Property Gmbh Bisaryl-bonded aryltriazolones and use thereof
AU2011308403B2 (en) 2010-10-01 2014-08-21 Taisho Pharmaceutical Co., Ltd. 1,2,4-triazolone derivative

Also Published As

Publication number Publication date
RU2622639C2 (ru) 2017-06-19
HRP20160421T1 (hr) 2016-05-20
CA2853227C (en) 2019-05-14
ZA201403000B (en) 2015-08-26
AU2012329965A1 (en) 2014-05-08
KR20140081824A (ko) 2014-07-01
PL2772482T3 (pl) 2016-08-31
CN103889951A (zh) 2014-06-25
TWI543971B (zh) 2016-08-01
PT2772482E (pt) 2016-06-03
RS54825B1 (sr) 2016-10-31
HUE028799T2 (en) 2017-01-30
IL232217A (en) 2017-02-28
RU2014121205A (ru) 2015-12-10
EP2772482B1 (en) 2016-03-09
SMT201600153B (it) 2016-07-01
CN103889951B (zh) 2016-12-14
BR112014009927B1 (pt) 2022-07-05
ES2568882T3 (es) 2016-05-05
MX339763B (es) 2016-06-07
EP2772482A4 (en) 2015-02-18
BR112014009927A2 (pt) 2017-04-25
CA2853227A1 (en) 2013-05-02
US9522914B2 (en) 2016-12-20
MY168930A (en) 2019-01-09
MX2014005140A (es) 2014-05-27
WO2013062027A1 (ja) 2013-05-02
PH12014500921A1 (en) 2014-06-09
JPWO2013062027A1 (ja) 2015-04-02
IL232217A0 (en) 2014-06-30
AU2012329965B2 (en) 2016-10-13
SI2772482T1 (sl) 2016-06-30
TW201332977A (zh) 2013-08-16
SG11201401766UA (en) 2014-10-30
NZ623918A (en) 2015-07-31
KR101998442B1 (ko) 2019-07-09
US20140275006A1 (en) 2014-09-18
EP2772482A1 (en) 2014-09-03
JP6025066B2 (ja) 2016-11-16
DK2772482T3 (en) 2016-06-06
CY1118021T1 (el) 2017-05-17

Similar Documents

Publication Publication Date Title
ME02402B (me) Derivati azola
AU2020274011B2 (en) Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
CA2930324C (en) Aminopyridine derivatives as tam family kinase inhibitors
IL300402A (en) Oxadiazole fungicides
HRP20180382T1 (hr) Inhibitori protein kinaze
JPWO2020231808A5 (me)
RU2425826C2 (ru) СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ ITPKb
HRP20201746T1 (hr) Aromatski derivati sulfonamida
RU2016141646A (ru) Ингибиторы trka киназы, основанные на них композиции и способы
ES2557478T3 (es) Compuestos de pirazol y triazol como inhibidores de KSP
RU2016133684A (ru) Бициклические азот-содержащие соединения как агонисты М1 мускариновых рецепторов
US12233065B2 (en) Inhibitors of RNA helicase DHX9 and uses thereof
JP2013532713A5 (me)
ES2550201T3 (es) Moduladores de la PDE10
JP2016519096A5 (me)
JP2016528212A (ja) 複素芳香環−ベンジル−アミド−サイクルコアを含むオートタキシン阻害剤
CA2671744A1 (en) Compounds and compositions as protein kinase inhibitors
KR20130105914A (ko) Ｈ-ｐｇｄｓ 억제제로서 다중헤테로아릴 화합물 및 프로스타글란딘 ｄ2 매개된 질병의 치료를 위한 그의 용도
HRP20230789T1 (hr) Derivati benzhidroksamske kiseline kao selektivni inhibitori hdac6
HRP20120969T1 (hr) Spoj azola
HRP20200440T1 (hr) 1h-pirazolo[4,3-b]piridini kao pde1 inhibitori
KR102655318B1 (ko) 치환된 질소 함유 화합물
RU2015101102A (ru) Гетероароматическое метильное производное циклического амина
RU2011103789A (ru) Производное триазола или его соль
JP2016540811A5 (me)