[go: up one dir, main page]

RU2015116112A - Производные n-(2-(циклический амин)этил)бензамида в качестве ингибиторов р2х7 - Google Patents

Производные n-(2-(циклический амин)этил)бензамида в качестве ингибиторов р2х7 Download PDF

Info

Publication number
RU2015116112A
RU2015116112A RU2015116112A RU2015116112A RU2015116112A RU 2015116112 A RU2015116112 A RU 2015116112A RU 2015116112 A RU2015116112 A RU 2015116112A RU 2015116112 A RU2015116112 A RU 2015116112A RU 2015116112 A RU2015116112 A RU 2015116112A
Authority
RU
Russia
Prior art keywords
optionally substituted
compound according
paragraphs
nitrogen
combined
Prior art date
Application number
RU2015116112A
Other languages
English (en)
Inventor
Джон Пол Килбурн
Ларс Кин Расмуссен
Миккель Джэссинг
Эман Мохаммед Элдеменки
Бин ЧЕН
Ию Джианг
Original Assignee
Х. Лундбекк А/С
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=49546380&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RU2015116112(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Х. Лундбекк А/С filed Critical Х. Лундбекк А/С
Publication of RU2015116112A publication Critical patent/RU2015116112A/ru

Links

Classifications

    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • 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
    • A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
    • 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61K31/535—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
    • 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
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A61K31/625—Salicylic acid; Derivatives thereof having heterocyclic substituents, e.g. 4-salicycloylmorpholine
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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 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
    • C07D211/38—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/10—Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/12—Heterocyclic 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
    • C07D295/125—Heterocyclic 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 attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic 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 attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • C07D401/06—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 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
    • C07D403/06—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
    • 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
    • C07D413/06—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 only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

1. Соединение формулы Iгде Rпредставляет собой фенил, пиридил, пиразинил, пиридазинил, пиримидил, 5-членный гетероарил, каждый из которых необязательно замещен одним или несколькими Салкилами, галогенами, гидрокси, Сфторалкилами, Сциклоалкилами, Салкокси, Cфторалкокси, циано или -SOR;где Rи Rобъединяются с азотом, к которому они присоединены, образуя пиперазинил, пиперидинил, морфолинил, пирролидинил, пирроло, имидазо, азетидинил, 6-10-членный спиро(гетороциклил), гомоморфолинил, гомопиперидинил или гомопиперазинил, каждый из которых необязательно замещен одним или несколькими Салкилами, Салкенилами, С-циклоалкилами, Салкокси, оксо, -NRRили атомами фтора;где Rпредставляет собой галоген, Сфторалкил, циано, циклопропил, Cалкилокси, Сфторалкилокси, -SOR, -NRRили Cалкил;где Rпредставляет собой галоген, Салкил, Сфторалкил, циано, -SOR, -NRR, Салкокси, Сфторалкокси или С-циклоалкил;где Rи Rнезависимо друг от друга представляют собой водород или Cалкил;где Rпредставляет собой Салкил, Сциклоалкил, Сфторалкил и где n равно 0-3; или его фармацевтически приемлемая соль.2. Соединение по п. 1, где Rпредставляет собой необязательно замещенный фенил.3. Соединение по п. 1, где Rпредставляет собой необязательно замещенный пиридил.4. Соединение по п. 1, где Rпредставляет собой необязательно замещенный пиразинил.5. Соединение по п. 1, где Rпредставляет собой необязательно замещенный пиримидил.6. Соединение по п. 1, где Rпредставляет собой необязательно замещенный 5-членный гетероарил.7. Соединение по любому из пп. 1-6, где Rи Rобъединяются с азотом, к которому они присоединены, образуя необязательно замещенный пиперазинил.8. Соединение по любому из пп. 1-6, где Rи Rобъединяются с азотом, к которому они присоединены, образуя

Claims (24)

1. Соединение формулы I
Figure 00000001
где R1 представляет собой фенил, пиридил, пиразинил, пиридазинил, пиримидил, 5-членный гетероарил, каждый из которых необязательно замещен одним или несколькими С1-6алкилами, галогенами, гидрокси, С1-4фторалкилами, С3-6циклоалкилами, С1-6алкокси, C1-6фторалкокси, циано или -SO2R7;
где R2a и R2b объединяются с азотом, к которому они присоединены, образуя пиперазинил, пиперидинил, морфолинил, пирролидинил, пирроло, имидазо, азетидинил, 6-10-членный спиро(гетороциклил), гомоморфолинил, гомопиперидинил или гомопиперазинил, каждый из которых необязательно замещен одним или несколькими С1-6алкилами, С1-6алкенилами, С3-6-циклоалкилами, С1-6алкокси, оксо, -NR5R6 или атомами фтора;
где R3 представляет собой галоген, С1-4фторалкил, циано, циклопропил, C1-4алкилокси, С1-4фторалкилокси, -SO2R7, -NR5R6 или C1-6алкил;
где R4 представляет собой галоген, С1-6алкил, С1-4фторалкил, циано, -SO2R8, -NR5R6, С1-6алкокси, С1-4фторалкокси или С3-6-циклоалкил;
где R5 и R6 независимо друг от друга представляют собой водород или C1-6алкил;
где R7 представляет собой С1-6алкил, С3-6циклоалкил, С1-4фторалкил и где n равно 0-3; или его фармацевтически приемлемая соль.
2. Соединение по п. 1, где R1 представляет собой необязательно замещенный фенил.
3. Соединение по п. 1, где R1 представляет собой необязательно замещенный пиридил.
4. Соединение по п. 1, где R1 представляет собой необязательно замещенный пиразинил.
5. Соединение по п. 1, где R1 представляет собой необязательно замещенный пиримидил.
6. Соединение по п. 1, где R1 представляет собой необязательно замещенный 5-членный гетероарил.
7. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пиперазинил.
8. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пиперидинил.
9. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный морфолинил.
10. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пирролидинил.
11. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный пирроло.
12. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный имидазо.
13. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный 6-10-членный спиро(гетероциклил).
14. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный гомоморфолинил.
15. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный гомопиперидинил.
16. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный гомопиперазинил.
17. Соединение по любому из пп. 1-6, где R2a и R2b объединяются с азотом, к которому они присоединены, образуя необязательно замещенный азетидинил.
18. Соединение по любому из пп. 1-6, где R3 представляет собой хлор, метил или трифторметил.
19. Соединение по любому из пп. 1-6, где n равно 0.
20. Соединение по любому из пп. 1-6, где n равно 1.
21. Соединение по любому из пп. 1-6, где n равно 2.
22. Соединение по любому из пп. 1-6, где R4 представляет собой фтор, хлор, С1-3алкил, С1-4фторалкил, циано-, C1-3алкокси- или С1-4фторалкокси.
23. Соединение, представленное в Таблице 1.
24. Фармацевтическая композиция, содержащая соединение по любому из пп. 1-23.
RU2015116112A 2012-10-12 2013-10-11 Производные n-(2-(циклический амин)этил)бензамида в качестве ингибиторов р2х7 RU2015116112A (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261713099P 2012-10-12 2012-10-12
US61/713,099 2012-10-12
PCT/EP2013/071253 WO2014057080A2 (en) 2012-10-12 2013-10-11 Cyclic amines

Publications (1)

Publication Number Publication Date
RU2015116112A true RU2015116112A (ru) 2016-12-10

Family

ID=49546380

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2015116112A RU2015116112A (ru) 2012-10-12 2013-10-11 Производные n-(2-(циклический амин)этил)бензамида в качестве ингибиторов р2х7

Country Status (29)

Country Link
US (6) US9108938B2 (ru)
EP (2) EP3536689A1 (ru)
JP (2) JP6333827B2 (ru)
KR (1) KR20150067189A (ru)
CN (1) CN104955819B (ru)
AP (1) AP2015008407A0 (ru)
AR (1) AR092975A1 (ru)
AU (1) AU2013328586B2 (ru)
BR (1) BR112015008123A2 (ru)
CA (1) CA2886559A1 (ru)
CL (1) CL2015000879A1 (ru)
CR (1) CR20150184A (ru)
DO (1) DOP2015000078A (ru)
EA (1) EA201590669A1 (ru)
EC (1) ECSP15014177A (ru)
HK (1) HK1213880A1 (ru)
IL (1) IL238011A0 (ru)
MA (1) MA37989A1 (ru)
MX (1) MX2015004414A (ru)
NI (1) NI201500052A (ru)
NZ (1) NZ630816A (ru)
PE (1) PE20150638A1 (ru)
PH (2) PH12015500795B1 (ru)
RU (1) RU2015116112A (ru)
SG (1) SG11201502684YA (ru)
TN (1) TN2015000114A1 (ru)
TW (1) TW201427947A (ru)
WO (1) WO2014057080A2 (ru)
ZA (1) ZA201503246B (ru)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI598325B (zh) * 2012-10-12 2017-09-11 Ｈ 朗德貝克公司 苯甲醯胺類
TW201427947A (zh) 2012-10-12 2014-07-16 Lundbeck & Co As H 環狀胺
EP2931717B1 (en) 2012-12-12 2016-12-07 Actelion Pharmaceuticals Ltd. Indole carboxamide derivatives as p2x7 receptor antagonists
CA2891499C (en) 2012-12-18 2021-07-06 Actelion Pharmaceuticals Ltd Indole carboxamide derivatives as p2x7 receptor antagonists
CN104918617B (zh) 2013-01-22 2017-05-10 埃科特莱茵药品有限公司 作为p2x7受体拮抗剂的杂环酰胺衍生物
JP6282017B2 (ja) 2013-01-22 2018-02-21 イドーシア ファーマシューティカルズ リミテッドＩｄｏｒｓｉａ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ Ｐ２ｘ７受容体アンタゴニストとしての複素環アミド誘導体
MA55805A (fr) 2019-05-03 2022-03-09 Flagship Pioneering Innovations V Inc Métodes de modulation de l'activité immunitaire

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1445707A1 (de) 1962-05-05 1969-03-13 Hoechst Ag Piperidinverbindungen und Verfahren zu ihrer Herstellung
US3435038A (en) 1965-06-01 1969-03-25 Sandoz Ag 5,6,7,9,10,14b-hexahydroisoquinolo (2,1-d) benzo (1,4) diazepines
US6303637B1 (en) 1998-10-30 2001-10-16 Merck & Co., Inc. Heterocyclic potassium channel inhibitors
US6632836B1 (en) 1998-10-30 2003-10-14 Merck & Co., Inc. Carbocyclic potassium channel inhibitors
US6194458B1 (en) 1998-10-30 2001-02-27 Merck & Co., Inc. Benzamide potassium channel inhibitors
SE9904738D0 (sv) 1999-12-22 1999-12-22 Astra Pharma Prod Novel compounds
SE0003476D0 (sv) 2000-09-28 2000-09-28 Astrazeneca Ab Compounds
ES2314096T3 (es) 2001-07-17 2009-03-16 N.V. Organon Derivados de n-((1-dimetilaminocicloalquil) metil) benzamida.
PA8557501A1 (es) 2001-11-12 2003-06-30 Pfizer Prod Inc Benzamida, heteroarilamida y amidas inversas
TW200300083A (en) 2001-11-12 2003-05-16 Pfizer Prod Inc Benzamide, heteroarylamide and reverse amides
TW200403058A (en) 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
PA8591801A1 (es) 2002-12-31 2004-07-26 Pfizer Prod Inc Inhibidores benzamidicos del receptor p2x7.
JP4731468B2 (ja) 2003-05-12 2011-07-27 ファイザー・プロダクツ・インク Ｐ２ｘ７受容体のベンズアミド阻害剤
EP1500651A1 (en) 2003-07-25 2005-01-26 Bayer CropScience S.A. N-[2-(2-Pyridinyl)ethyl]benzamide compounds and their use as fungicides
TW200524888A (en) 2003-08-08 2005-08-01 Vertex Pharma Compositions useful as inhibitors of voltage-gated ion channels
TWI368482B (en) 2003-12-19 2012-07-21 Bayer Sas New 2-pyridinylethylbenzamide derivatives
AU2005228133B2 (en) 2004-03-24 2011-09-08 Merck Sharp & Dohme Corp. Heteroaryl piperidine glycine transporter inhibitors
EP1773776A1 (en) 2004-07-23 2007-04-18 Bayer Cropscience Sa 3-pyridinylethylbenzamide derivatives as fungicides
JP5055493B2 (ja) 2004-12-21 2012-10-24 メルク シャープ エンド ドーム リミテッド Ｇｌｙｔ１阻害薬としてのピペリジンおよびアゼチジン誘導体
PE20061156A1 (es) 2004-12-23 2006-12-16 Glaxo Group Ltd Derivados de benzamida como agentes inhibidores del transportador de glicina
WO2006134341A1 (en) 2005-06-13 2006-12-21 Merck Sharp & Dohme Limited Therapeutic agents
EP1940782B1 (en) 2005-10-19 2009-03-11 F.Hoffmann-La Roche Ag N-phenyl phenylacetamide non-nucleoside reverse transcriptase inhibitors
JP2009057282A (ja) 2005-12-19 2009-03-19 Astellas Pharma Inc カルボン酸誘導体又はその塩
TWI435863B (zh) 2006-03-20 2014-05-01 Nihon Nohyaku Co Ltd Ｎ-２-（雜）芳基乙基甲醯胺衍生物及含該衍生物之蟲害防治劑
CN101687836A (zh) 2007-07-02 2010-03-31 先正达参股股份有限公司 新型杀微生物剂
ITMC20070152A1 (it) 2007-07-26 2009-01-27 Faggiolati Pumps Spa Miscelatore sommerso in particolare miscelatore sommerso per vasche di trattamento delle acque reflue.
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
ES2376092T3 (es) * 2008-04-22 2012-03-08 Janssen Pharmaceutica, N.V. Antagonistas de p2x7 sustituidos con quinolina o isoquinolina.
ES2345527B1 (es) 2008-10-08 2011-09-08 Hospital Clinic I Provincial De Barcelona Sustancias bloqueadoras de los canales kv 1.3 para el tratamiento de enfermedades asociadas a hiperplasia de la intima.
JP2013532185A (ja) 2010-07-12 2013-08-15 ファイザー・リミテッド 化合物
EP2682115B1 (en) 2011-03-02 2017-04-19 The University of Tokyo Endoparasite control agent
RU2608217C2 (ru) 2011-11-02 2017-01-17 Байер Интеллектуэль Проперти Гмбх Соединения с нематоцидной активностью
TW201427947A (zh) 2012-10-12 2014-07-16 Lundbeck & Co As H 環狀胺
TWI598325B (zh) 2012-10-12 2017-09-11 Ｈ 朗德貝克公司 苯甲醯胺類

Also Published As

Publication number Publication date
EA201590669A1 (ru) 2015-10-30
EP2906549B1 (en) 2019-04-17
HK1213880A1 (zh) 2016-07-15
AP2015008407A0 (en) 2015-04-30
CL2015000879A1 (es) 2015-11-06
AU2013328586A1 (en) 2015-04-16
EP2906549A2 (en) 2015-08-19
DOP2015000078A (es) 2015-09-15
US10124010B2 (en) 2018-11-13
PH12017500351A1 (en) 2017-12-11
JP6333827B2 (ja) 2018-05-30
TN2015000114A1 (en) 2016-06-29
IL238011A0 (en) 2015-05-31
US20150306114A1 (en) 2015-10-29
ZA201503246B (en) 2016-11-30
AU2013328586B2 (en) 2017-07-13
WO2014057080A3 (en) 2014-07-10
US9593105B2 (en) 2017-03-14
JP2018140995A (ja) 2018-09-13
CN104955819A (zh) 2015-09-30
PH12015500795A1 (en) 2015-06-08
WO2014057080A2 (en) 2014-04-17
SG11201502684YA (en) 2015-05-28
US20170128460A1 (en) 2017-05-11
CA2886559A1 (en) 2014-04-17
EP3536689A1 (en) 2019-09-11
US20170008898A1 (en) 2017-01-12
MX2015004414A (es) 2015-06-24
BR112015008123A2 (pt) 2017-07-04
US9861639B2 (en) 2018-01-09
US20180177793A1 (en) 2018-06-28
CN104955819B (zh) 2018-06-19
US9415055B2 (en) 2016-08-16
US20140107335A1 (en) 2014-04-17
AR092975A1 (es) 2015-05-13
TW201427947A (zh) 2014-07-16
US20190307766A1 (en) 2019-10-10
US9108938B2 (en) 2015-08-18
MA37989A1 (fr) 2016-02-29
ECSP15014177A (es) 2015-12-31
NI201500052A (es) 2016-02-16
PH12015500795B1 (en) 2015-06-08
NZ630816A (en) 2017-03-31
JP2015533143A (ja) 2015-11-19
KR20150067189A (ko) 2015-06-17
PE20150638A1 (es) 2015-05-13
CR20150184A (es) 2015-07-21

Similar Documents

Publication Publication Date Title
RU2015113320A (ru) Бензамиды
RU2015116112A (ru) Производные n-(2-(циклический амин)этил)бензамида в качестве ингибиторов р2х7
IL277341B2 (en) Antifibrotic pyridinones
EA201391239A1 (ru) Пирроло[2,3-d]пиримидиновые производные в качестве ингибиторов тропомиозин-связанных киназ
AR082153A1 (es) N-sulfonilbenzamidas utiles como inhibidor del canal de sodio
AR086546A1 (es) Derivados de 7h-purin-8(9h)-ona como inhibidores de jak
AR076435A1 (es) Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos
HRP20251220T1 (hr) Derivati bipirazola kao jak inhibitori
AR075332A1 (es) Dionas ciclicas como herbicidas
AR073687A1 (es) Agonistas de receptores cb2, derivados de oxazoles y/o triazoles, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento del dolor, enfermedades autoinmunes y alergicas, entre otras.
PH12015502232A1 (en) Naphthyridine derivatives useful as alpha-v-beta-6 integrin antagonists
EA201390199A1 (ru) 2-замещенные-8-алкил-7-оксо-7,8-дигидропиридо[2,3-d]пиримидин-6-карбонитрилы и их применение
EA200970656A1 (ru) Вич-ингибирующие 5,6-замещенные пиримидины
EA201170099A1 (ru) Замещенные пиримидин-4-оновые производные
AR091271A1 (es) Pirrolopirimidona y pirrolopiridona, inhibidores de tanquirasa
AR073286A1 (es) Compuestos de imidazol y de triazol, su uso, asi como productos que los contienen
PE20150194A1 (es) Novedosas n-piridinil amidas ciclicas sustituidas como inhibidores de quinasa
EA201391558A1 (ru) Тетрагидропиразоло[1,5-а]пиримидины как противотуберкулезные соединения
AR081252A1 (es) Compuestos para el tratamiento del sindrome metabolico
MX336247B (es) Derivados de amida heterociclicos como antagonistas del receptor p2x7.
EA201070817A1 (ru) ПРОИЗВОДНЫЕ ИМИДАЗО[1,2-α]ПИРИДИН-2-КАРБОКСАМИДОВ, ИХ ПОЛУЧЕНИЕ И ИХ ПРИМЕНЕНИЕ В ТЕРАПИИ
MY194004A (en) 4 -substituted benzoxaborole compounds and uses thereof
JP2015500842A5 (ru)
EA201591904A1 (ru) НОВЫЕ ПРОИЗВОДНЫЕ N-(2,3-ДИГИДРО-1H-ПИРРОЛО[2,3-b]ПИРИДИН-5-ИЛ)-4-ХИНАЗОЛИНАМИНА И N-(2,3-ДИГИДРО-1H-ИНДОЛ-5-ИЛ)-4-ХИНАЗОЛИНАМИНА В КАЧЕСТВЕ ИНГИБИТОРОВ PERK
EA201590828A1 (ru) Насыщенные азотсодержащие и n-ацилированные гетероциклы, усиливающие действие активного антибиотика против микобактерий

Legal Events

Date Code Title Description
FA92 Acknowledgement of application withdrawn (lack of supplementary materials submitted)

Effective date: 20181107