RU2007143507A - Производные фенилацетилена, обладающие сродством к рецептору mglur 5 - Google Patents
Производные фенилацетилена, обладающие сродством к рецептору mglur 5 Download PDFInfo
- Publication number
- RU2007143507A RU2007143507A RU2007143507/04A RU2007143507A RU2007143507A RU 2007143507 A RU2007143507 A RU 2007143507A RU 2007143507/04 A RU2007143507/04 A RU 2007143507/04A RU 2007143507 A RU2007143507 A RU 2007143507A RU 2007143507 A RU2007143507 A RU 2007143507A
- Authority
- RU
- Russia
- Prior art keywords
- compound
- formula
- alkyl
- free base
- hydrogen
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C211/00—Compounds containing amino groups bound to a carbon skeleton
- C07C211/43—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
- C07C211/44—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring
- C07C211/52—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/42—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups or hydroxy groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C215/44—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups or hydroxy groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton bound to carbon atoms of the same ring or condensed ring 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
-
- 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
- A61P1/10—Laxatives
-
- 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
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
- 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
-
- 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
- A61P25/36—Opioid-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C211/00—Compounds containing amino groups bound to a carbon skeleton
- C07C211/43—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
- C07C49/587—Unsaturated compounds containing a keto groups being part of a ring
- C07C49/703—Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups
- C07C49/747—Unsaturated compounds containing a keto groups being part of a ring containing hydroxy groups containing six-membered aromatic rings
-
- 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
- C07D213/60—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 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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/38—Nitrogen atoms
- C07D215/40—Nitrogen atoms attached in position 8
-
- 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
- C07D231/14—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 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
- C07D231/38—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- 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
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
-
- 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
- C07D239/06—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
- C07D239/12—Nitrogen atoms not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three 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
- C07D241/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
- C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
- C07D241/40—Benzopyrazines
- C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
- C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
- C07D241/40—Benzopyrazines
- C07D241/44—Benzopyrazines 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 carbon atoms of the hetero ring
-
- 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
- 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
- C07D277/32—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 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
- C07D277/38—Nitrogen atoms
- C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/14—Thiadiazoles; Hydrogenated thiadiazoles condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Addiction (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Nutrition Science (AREA)
- Rheumatology (AREA)
- Child & Adolescent Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
Abstract
1. Соединение формулы (I) ! ! в которой ! R1 обозначает водород или С1-С4алкил и ! R2 обозначает незамещенный или замещенный гетероцикл, или ! R1 обозначает водород или С1-С4алкил и ! R2 обозначает арил или замещенный арил, или ! R1 и R2 совместно с атомом азота образуют незамещенный или замещенный гетероцикл; ! R3 обозначает (С1-С4)алкил, (С1-С4)алкоксигруппу, трифторметил, галоген, цианогруппу, нитрогруппу, -СНО, -СОО(С1-С4)алкил, -СО(С1-С4)алкил; ! n равно 0, 1, 2, 3, 4 или 5; ! R4 обозначает ОН и ! R5 и R6 обозначают Н или С1-С4алкил, или ! R4 и R5 образуют связь и ! R6 обозначает Н или С1-С4алкил, или ! R4 и R6 образуют связь и ! R5 обозначает Н или С1-С4алкил, ! в форме свободного основания или соли присоединения с кислотой. ! 2. Соединение формулы (I') ! ! в которой R1, R2, R3 являются такими, как определено в п.1. ! 3. Соединение формулы (II) ! ! в которой R6, R5, R3, n являются такими, как определено в п.1. ! 4. Способ получения соединения формулы (I) по п.1 или его соли, который включает стадии ! а) получения соединения формулы (I), в которой i) R4 обозначает гидроксигруппу, ! R1 обозначает водород или С1-С4алкил и R2 обозначает незамещенный или замещенный гетероцикл или ii) R1 обозначает водород или С1-С4алкил и R2 обозначает арил или замещенный арил, с помощью восстановительного аминирования соединения формулы (II) ! ! в которой R6, R5, R3, n являются такими, как определено выше, соединением формулы (III) ! ! в которой R1 и R2 являются такими, как определено выше, или ! b) получения соединения формулы (I), в которой R4 обозначает гидроксигруппу, R1 и R2 совместно с атомом азота образуют незамещенный или замещенный гетероцикл, с помощью циклоконденсации соединения формулы (IV) ! ! или ! с) получения соединения формулы (I), в которо
Claims (10)
1. Соединение формулы (I)
в которой
R1 обозначает водород или С1-С4алкил и
R2 обозначает незамещенный или замещенный гетероцикл, или
R1 обозначает водород или С1-С4алкил и
R2 обозначает арил или замещенный арил, или
R1 и R2 совместно с атомом азота образуют незамещенный или замещенный гетероцикл;
R3 обозначает (С1-С4)алкил, (С1-С4)алкоксигруппу, трифторметил, галоген, цианогруппу, нитрогруппу, -СНО, -СОО(С1-С4)алкил, -СО(С1-С4)алкил;
n равно 0, 1, 2, 3, 4 или 5;
R4 обозначает ОН и
R5 и R6 обозначают Н или С1-С4алкил, или
R4 и R5 образуют связь и
R6 обозначает Н или С1-С4алкил, или
R4 и R6 образуют связь и
R5 обозначает Н или С1-С4алкил,
в форме свободного основания или соли присоединения с кислотой.
4. Способ получения соединения формулы (I) по п.1 или его соли, который включает стадии
а) получения соединения формулы (I), в которой i) R4 обозначает гидроксигруппу,
R1 обозначает водород или С1-С4алкил и R2 обозначает незамещенный или замещенный гетероцикл или ii) R1 обозначает водород или С1-С4алкил и R2 обозначает арил или замещенный арил, с помощью восстановительного аминирования соединения формулы (II)
в которой R6, R5, R3, n являются такими, как определено выше, соединением формулы (III)
в которой R1 и R2 являются такими, как определено выше, или
b) получения соединения формулы (I), в которой R4 обозначает гидроксигруппу, R1 и R2 совместно с атомом азота образуют незамещенный или замещенный гетероцикл, с помощью циклоконденсации соединения формулы (IV)
или
с) получения соединения формулы (I), в которой R4 обозначает гидроксигруппу, R1 и R2 совместно с атомом азота образуют незамещенный или замещенный гетероцикл, с помощью восстановительного алкилирования соединения формулы (V)
в которой R6, R5, R2, R1 являются такими, как определено выше, соединением формулы (VI)
в которой R3 и n являются такими, как определено выше, или
d) получения соединения формулы (I), в которой i) R4 и R5 образуют связь и R6 обозначает водород или С1-С4алкил или ii) в которой R4 и R6 образуют связь и R5 обозначает водород, с помощью дегидратации соединения формулы (I), в которой R4 обозначает гидроксигруппу, R5 и R6 обозначают водород или С1-С4алкил;
и выделения полученного соединения формулы (I) в форме свободного основания или соли присоединения с кислотой.
5. Соединение по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой, предназначенное для применения в качестве фармацевтического средства.
6. Соединение по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой, предназначенное для применения для предупреждения, лечения или задержки прогрессирования нарушений, связанных с нерегулярностью глутаматергической передачи сигнала, нарушений желудочно-кишечного тракта и мочевых путей, и нервной системы, полностью или частично опосредуемых mGluR5.
7. Фармацевтическая композиция, включающая соединение по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой совместно с фармацевтическим носителем или разбавителем.
8. Применение соединения по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой для предупреждения, лечения или задержки прогрессирования нарушений, связанных с нерегулярностью глутаматергической передачи сигнала, нарушений желудочно-кишечного тракта и мочевых путей, и нервной системы, полностью или частично опосредуемых mGluR5.
9. Применение соединения по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой для приготовления фармацевтической композиции, предназначенной для предупреждения, лечения или задержки прогрессирования нарушений, связанных с нерегулярностью глутаматергической передачи сигнала, нарушений желудочно-кишечного тракта и мочевых путей, и нервной системы, полностью или частично опосредуемых mGluR5.
10. Способ лечения нарушений, связанных с нерегулярностью глутаматергической передачи сигнала, и нарушений нервной системы, полностью или частично опосредуемых mGluR5, способ включает введение субъекту, нуждающемуся в таком лечении, терапевтически эффективного количества соединения по п.1 в форме свободного основания или фармацевтически приемлемой соли присоединения с кислотой.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0508318.3 | 2005-04-25 | ||
GBGB0508318.3A GB0508318D0 (en) | 2005-04-25 | 2005-04-25 | Organic compounds |
Publications (1)
Publication Number | Publication Date |
---|---|
RU2007143507A true RU2007143507A (ru) | 2009-06-10 |
Family
ID=34640066
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2007143507/04A RU2007143507A (ru) | 2005-04-25 | 2006-04-24 | Производные фенилацетилена, обладающие сродством к рецептору mglur 5 |
Country Status (17)
Country | Link |
---|---|
US (1) | US20080188490A1 (ru) |
EP (1) | EP1877364B1 (ru) |
JP (1) | JP2008538775A (ru) |
KR (1) | KR20070122224A (ru) |
CN (1) | CN101163662A (ru) |
AT (1) | ATE427927T1 (ru) |
AU (1) | AU2006239545A1 (ru) |
BR (1) | BRPI0610337A2 (ru) |
CA (1) | CA2605262A1 (ru) |
DE (1) | DE602006006170D1 (ru) |
ES (1) | ES2323288T3 (ru) |
GB (1) | GB0508318D0 (ru) |
MX (1) | MX2007013238A (ru) |
PL (1) | PL1877364T3 (ru) |
PT (1) | PT1877364E (ru) |
RU (1) | RU2007143507A (ru) |
WO (1) | WO2006114260A1 (ru) |
Families Citing this family (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN100381083C (zh) | 2003-04-29 | 2008-04-16 | 韩力 | 一种非可燃性电子喷雾香烟 |
CN2719043Y (zh) * | 2004-04-14 | 2005-08-24 | 韩力 | 雾化电子烟 |
GB0503646D0 (en) * | 2005-02-22 | 2005-03-30 | Novartis Ag | Organic compounds |
GB0508314D0 (en) * | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
GB0508319D0 (en) * | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
CN201067079Y (zh) * | 2006-05-16 | 2008-06-04 | 韩力 | 仿真气溶胶吸入器 |
US20100249136A1 (en) * | 2007-10-12 | 2010-09-30 | Daniel Umbricht | Organic compounds |
WO2009047303A2 (en) * | 2007-10-12 | 2009-04-16 | Novartis Ag | Metabotropic glutamate receptor modulators for the treatment of pervasive developmental disorder |
JPWO2009130900A1 (ja) * | 2008-04-24 | 2011-08-11 | 日本曹達株式会社 | オキシム誘導体、中間体化合物および植物病害防除剤 |
US8349852B2 (en) | 2009-01-13 | 2013-01-08 | Novartis Ag | Quinazolinone derivatives useful as vanilloid antagonists |
MX2012002842A (es) | 2009-09-08 | 2012-04-19 | Kyorin Seiyaku Kk | Metodo para fabricar derivado de acido 4-(5-metilpiridin-2.iloamin o) piperidin-1-carboxilico. |
EP2531510B1 (en) | 2010-02-01 | 2014-07-23 | Novartis AG | Pyrazolo[5,1b]oxazole derivatives as crf-1 receptor antagonists |
AR080056A1 (es) | 2010-02-01 | 2012-03-07 | Novartis Ag | Derivados de ciclohexil-amida como antagonistas de los receptores de crf |
ES2527849T3 (es) | 2010-02-02 | 2015-01-30 | Novartis Ag | Derivados de ciclohexilamida como antagonistas del receptor de CRF |
KR101862626B1 (ko) * | 2010-07-09 | 2018-05-31 | 레코르다티 아일랜드 리미티드 | Mglu5 대항체로서의 신 스피로헤테로사이클릭 화합물 |
EP2758375A1 (en) | 2011-09-23 | 2014-07-30 | Advinus Therapeutics Limited | Amide compounds, compositions and applications thereof |
CN105121424B (zh) * | 2013-02-18 | 2019-01-22 | 华领医药技术(上海)有限公司 | mGluR调节剂 |
KR20180067030A (ko) | 2016-12-12 | 2018-06-20 | 김성갑 | 금속판에 다양한 곡면을 성형하는 방법 |
KR20180067010A (ko) | 2016-12-12 | 2018-06-20 | 김선권 | 금속판에 다양한 곡면을 성형하는 방법 |
JP7456621B2 (ja) * | 2018-08-07 | 2024-03-27 | 慶應義塾 | 神経機能調節物質の動態の検出剤、及び神経機能調節物質の検出方法 |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3991064A (en) * | 1975-01-17 | 1976-11-09 | Warner-Lambert Company | Benzonaphthyridines |
US5576336A (en) * | 1993-03-18 | 1996-11-19 | Merck Sharp & Dohme Limited | Indole derivatives as dopamine D4 antagonists |
US5714498A (en) * | 1993-03-18 | 1998-02-03 | Merck, Sharp, & Dohme, Ltd. | Benzimidazole derivatives |
US5521297A (en) * | 1993-06-04 | 1996-05-28 | Salk Institute Biotechnology/Industrial Associates | Nucleic acids encoding human metabotropic glutamate receptors |
JPH09512542A (ja) * | 1994-04-28 | 1997-12-16 | メルク シヤープ エンド ドーム リミテツド | D▲下4▼リセプタ拮抗剤としてのベンゾフラン誘導体 |
WO1996005200A1 (en) * | 1994-08-10 | 1996-02-22 | Merck Sharp & Dohme Limited | TETRAHYDROPYRIDINYLMETHYL DERIVATIVES OF PYRROLO[2,3-b]PYRIDINE |
US5688798A (en) * | 1995-10-10 | 1997-11-18 | Hoffmann-La Roche Inc. | Pyrimidine compounds |
AUPR201600A0 (en) * | 2000-12-11 | 2001-01-11 | Fujisawa Pharmaceutical Co., Ltd. | Quinazolinone derivative |
GB0128996D0 (en) * | 2001-12-04 | 2002-01-23 | Novartis Ag | Organic compounds |
US6806279B2 (en) * | 2001-12-17 | 2004-10-19 | Sunesis Pharmaceuticals, Inc. | Small-molecule inhibitors of interleukin-2 |
US6995144B2 (en) * | 2002-03-14 | 2006-02-07 | Eisai Co., Ltd. | Nitrogen containing heterocyclic compounds and medicines containing the same |
GB0503646D0 (en) * | 2005-02-22 | 2005-03-30 | Novartis Ag | Organic compounds |
GB0508314D0 (en) * | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
GB0508319D0 (en) * | 2005-04-25 | 2005-06-01 | Novartis Ag | Organic compounds |
-
2005
- 2005-04-25 GB GBGB0508318.3A patent/GB0508318D0/en not_active Ceased
-
2006
- 2006-04-24 RU RU2007143507/04A patent/RU2007143507A/ru not_active Application Discontinuation
- 2006-04-24 CN CNA2006800136880A patent/CN101163662A/zh active Pending
- 2006-04-24 KR KR1020077024419A patent/KR20070122224A/ko not_active Application Discontinuation
- 2006-04-24 EP EP06724538A patent/EP1877364B1/en not_active Not-in-force
- 2006-04-24 AU AU2006239545A patent/AU2006239545A1/en not_active Abandoned
- 2006-04-24 PL PL06724538T patent/PL1877364T3/pl unknown
- 2006-04-24 ES ES06724538T patent/ES2323288T3/es active Active
- 2006-04-24 PT PT06724538T patent/PT1877364E/pt unknown
- 2006-04-24 CA CA002605262A patent/CA2605262A1/en not_active Abandoned
- 2006-04-24 MX MX2007013238A patent/MX2007013238A/es not_active Application Discontinuation
- 2006-04-24 US US11/912,624 patent/US20080188490A1/en not_active Abandoned
- 2006-04-24 WO PCT/EP2006/003764 patent/WO2006114260A1/en active Application Filing
- 2006-04-24 DE DE602006006170T patent/DE602006006170D1/de active Active
- 2006-04-24 AT AT06724538T patent/ATE427927T1/de not_active IP Right Cessation
- 2006-04-24 BR BRPI0610337-5A patent/BRPI0610337A2/pt not_active IP Right Cessation
- 2006-04-24 JP JP2008508131A patent/JP2008538775A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
KR20070122224A (ko) | 2007-12-28 |
PT1877364E (pt) | 2009-07-09 |
EP1877364B1 (en) | 2009-04-08 |
EP1877364A1 (en) | 2008-01-16 |
CA2605262A1 (en) | 2006-11-02 |
JP2008538775A (ja) | 2008-11-06 |
PL1877364T3 (pl) | 2009-09-30 |
GB0508318D0 (en) | 2005-06-01 |
US20080188490A1 (en) | 2008-08-07 |
BRPI0610337A2 (pt) | 2010-06-15 |
DE602006006170D1 (de) | 2009-05-20 |
ATE427927T1 (de) | 2009-04-15 |
CN101163662A (zh) | 2008-04-16 |
AU2006239545A1 (en) | 2006-11-02 |
ES2323288T3 (es) | 2009-07-10 |
MX2007013238A (es) | 2008-01-24 |
WO2006114260A1 (en) | 2006-11-02 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
RU2007143507A (ru) | Производные фенилацетилена, обладающие сродством к рецептору mglur 5 | |
RU2007143509A (ru) | Производные ацетилена | |
RU2405774C2 (ru) | Гетероциклические ингибиторы аспартилпротеазы | |
RU2007143505A (ru) | Производные ацетилена | |
CA2466560A1 (en) | Acetylene derivatives having mglur5 antagonistic activity | |
RU2007134970A (ru) | Производные пирролидинацетилена и пиперидинацетилена для применения в качестве антагонистов mglur5 | |
WO2018188641A1 (zh) | 一种mor激动剂与kor激动剂的药物组合物及其用途 | |
JP2013503139A5 (ru) | ||
RU2016125705A (ru) | Замещенные бензоазепины в качестве модуляторов тoll-подобных рецепторов | |
EA200700712A1 (ru) | Производные индолуксусной кислоты, способ получения таких производных (варианты), фармацевтическая композиция, набор на их основе, способ ингибирования связывания эндогенных лигандов и способ лечения заболеваний и расстройств, восприимчивых к ингибированию связывания эндогенных лигандов с рецептором crth-2 | |
RU2008119692A (ru) | Новые 1-азабициклоалкилпроизводные для лечения психических растройств | |
ATE517882T1 (de) | Chinolinderivate | |
RU2007116987A (ru) | Новые соединения | |
TW200736257A (en) | Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives | |
EA200601364A1 (ru) | Производные хинолина и их применение в качестве ингибиторов микобактерий | |
EA200700099A1 (ru) | Производные пиридина | |
JP2009521483A5 (ru) | ||
RU2007130144A (ru) | Гетероциклические соединения в качестве антагонистов cccr2b | |
RU2012123009A (ru) | Применение бензогетероциклических производных для предупреждения и лечения рака или для ингибирования метастазирования рака | |
JP2009534358A5 (ru) | ||
WO2007054444A3 (en) | 3-aryl-isoxazole-4-carbonyl-benzofuran derivatives | |
EA200801536A1 (ru) | Новые тиенопирсульфоновые производные | |
RU2007125658A (ru) | Фенилпиперазиновые производные с сочетанием свойств неполного агонизма к рецепторам дофамина-d2 и ингибирования повторного поглощения серотонина | |
RU2011112684A (ru) | АГЕНТ, СПОСОБСТВУЮЩИЙ РОСТУ ВОЛОС, СОДЕРЖАЩИЙ В КАЧЕСТВЕ АКТИВНОГО ИНГРЕДИЕНТА ПРОИЗВОДНОЕ 15,15-ДИФТОРПРОСТАГЛАНДИНА F2α | |
RU2014144883A (ru) | Новые производные фенил-тетрагидроизохинолина |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20100901 |