EA201691690A1 - Производные этинила - Google Patents
Производные этинилаInfo
- Publication number
- EA201691690A1 EA201691690A1 EA201691690A EA201691690A EA201691690A1 EA 201691690 A1 EA201691690 A1 EA 201691690A1 EA 201691690 A EA201691690 A EA 201691690A EA 201691690 A EA201691690 A EA 201691690A EA 201691690 A1 EA201691690 A1 EA 201691690A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- lower alkyl
- hydrogen
- halogen
- pyridinyl
- phenyl
- Prior art date
Links
Classifications
-
- 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
- C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
-
- 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
-
- 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
- A61K31/495—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
- A61P25/14—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
- A61P25/22—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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
-
- 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
- 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
- C07D401/14—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 three or more hetero 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
- 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
- C07D471/04—Ortho-condensed systems
-
- 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
- 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
- C07D498/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Настоящее изобретение относится к соединениям формулы Iгде Y представляет собой N или C-R; Rпредставляет собой водород или F; Rпредставляет собой водород, галоген или низший алкил, замещенный галогеном; Rпредставляет собой водород или низший алкил; или Rобразует вместе с R6-членное гетероциклическое кольцо, содержащее -СН-СН-О-СН- или -CH-CH-NR-C(O)-; R представляет собой водород, низший алкил, фенил или бензил; Rпредставляет собой фенил или пиридинил, где N атом в пиридинильной группе может быть в различных положениях; Rпредставляет собой водород, низший алкил или низший алкоксиалкил; Rпредставляет собой водород, низший алкил, фенил, возможно замещенный галогеном или низшим алкокси, или представляет собой циклоалкил, или представляет собой пиридинил, возможно замещенный галогеном, низшим алкилом, низшим алкокси или =O, или представляет собой пиримидинил, возможно замещенный низшим алкилом, низшим алкокси или =O, или представляет собой 1-низший алкил-пиридинил, или представляет собой пиразинил, или представляет собой пиридазинил, возможно замещенный низшим алкилом, низшим алкокси или =O, или представляет собой 1-метилпирроло[2,3-b]пиридин-5-ил, или представляет собой 6-имидазо[1,2-b]пиридазин-6-ил; или Rобразует вместе с R4-, 5- или 6-членное гетероциклическое кольцо, содержащее -(СН)-, -СН-СН-О-CH-CH-, CH-CH-CH-, CH-CH-CH-CH-, CH-O-CH-CH- или CH-CH-СН-О-СН; Rи Rпредставляют собой водород или низший алкил; или Rобразует вместе с Rнасыщенное 5-членное кольцо, содержащее -CH-CH-CH-; или к их фармацевтически приемлемым солям или кислотно-аддитивным солям, рацемическим смесям или их соответствующим энантиомерам, и/или оптическим изомерам, и/или стереоизомерам. Указанные соединения могут применяться для лечения болезни Паркинсона, тревожности, рвоты,
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14156461 | 2014-02-25 | ||
| PCT/EP2015/053785 WO2015128307A1 (en) | 2014-02-25 | 2015-02-24 | Ethynyl derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201691690A1 true EA201691690A1 (ru) | 2016-12-30 |
| EA029261B1 EA029261B1 (ru) | 2018-02-28 |
Family
ID=50151209
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201691690A EA029261B1 (ru) | 2014-02-25 | 2015-02-24 | Производные этинила |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US9725416B2 (ru) |
| EP (1) | EP3110802B1 (ru) |
| JP (1) | JP6286577B2 (ru) |
| KR (1) | KR101792452B1 (ru) |
| CN (1) | CN106029649B (ru) |
| AR (1) | AR099529A1 (ru) |
| AU (1) | AU2015222303B2 (ru) |
| BR (1) | BR112016017816A8 (ru) |
| CA (1) | CA2938009A1 (ru) |
| CL (1) | CL2016002064A1 (ru) |
| CR (1) | CR20160384A (ru) |
| DK (1) | DK3110802T3 (ru) |
| EA (1) | EA029261B1 (ru) |
| ES (1) | ES2701167T3 (ru) |
| HR (1) | HRP20182016T1 (ru) |
| HU (1) | HUE041392T2 (ru) |
| IL (1) | IL246842B (ru) |
| LT (1) | LT3110802T (ru) |
| MA (1) | MA39305A3 (ru) |
| MX (1) | MX369819B (ru) |
| PE (1) | PE20161415A1 (ru) |
| PH (1) | PH12016501481B1 (ru) |
| PL (1) | PL3110802T3 (ru) |
| PT (1) | PT3110802T (ru) |
| RS (1) | RS58208B1 (ru) |
| SG (1) | SG11201607010XA (ru) |
| SI (1) | SI3110802T1 (ru) |
| TW (1) | TWI576340B (ru) |
| UA (1) | UA117855C2 (ru) |
| WO (1) | WO2015128307A1 (ru) |
| ZA (1) | ZA201605243B (ru) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6539749B2 (ja) | 2015-03-19 | 2019-07-03 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ｍＧｌｕＲ４のモジュレーターとしての３−（４−エチニルフェニル）ヘキサヒドロピリミジン−２，４−ジオン誘導体 |
| RU2712633C1 (ru) | 2015-06-03 | 2020-01-30 | Ф. Хоффманн-Ля Рош Аг | Этинильные производные |
| ES2733468T3 (es) | 2015-07-15 | 2019-11-29 | Hoffmann La Roche | Derivados de etinilo como moduladores de los receptores metabotrópicos de glutamato |
| AR105556A1 (es) * | 2015-08-03 | 2017-10-18 | Hoffmann La Roche | Derivados de etinilo |
| BR112019000314A2 (pt) * | 2016-07-18 | 2019-04-16 | F. Hoffmann-La Roche Ag | derivados de etinila |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102740699A (zh) * | 2009-09-04 | 2012-10-17 | 范德比尔特大学 | 用于治疗神经学上的功能失调的mglur4变构增效剂、组合物和方法 |
| US8759377B2 (en) * | 2009-11-23 | 2014-06-24 | Vanderbilt University | Substituted dioxopiperidines and dioxopyrrolidines as MGLUR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction |
| US8420661B2 (en) * | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
| DK3049409T3 (en) * | 2013-09-25 | 2017-07-10 | Hoffmann La Roche | ethynyl derivatives |
| TWI649310B (zh) * | 2014-01-10 | 2019-02-01 | 赫孚孟拉羅股份公司 | 乙炔基衍生物 |
-
2015
- 2015-02-24 PE PE2016001503A patent/PE20161415A1/es unknown
- 2015-02-24 AR ARP150100537A patent/AR099529A1/es unknown
- 2015-02-24 PL PL15706788T patent/PL3110802T3/pl unknown
- 2015-02-24 KR KR1020167023095A patent/KR101792452B1/ko active IP Right Grant
- 2015-02-24 SG SG11201607010XA patent/SG11201607010XA/en unknown
- 2015-02-24 ES ES15706788T patent/ES2701167T3/es active Active
- 2015-02-24 CR CR20160384A patent/CR20160384A/es unknown
- 2015-02-24 UA UAA201609882A patent/UA117855C2/uk unknown
- 2015-02-24 EA EA201691690A patent/EA029261B1/ru not_active IP Right Cessation
- 2015-02-24 AU AU2015222303A patent/AU2015222303B2/en not_active Ceased
- 2015-02-24 CN CN201580010032.2A patent/CN106029649B/zh active Active
- 2015-02-24 PT PT15706788T patent/PT3110802T/pt unknown
- 2015-02-24 JP JP2016554209A patent/JP6286577B2/ja active Active
- 2015-02-24 WO PCT/EP2015/053785 patent/WO2015128307A1/en active Application Filing
- 2015-02-24 BR BR112016017816A patent/BR112016017816A8/pt not_active Application Discontinuation
- 2015-02-24 LT LTEP15706788.5T patent/LT3110802T/lt unknown
- 2015-02-24 EP EP15706788.5A patent/EP3110802B1/en active Active
- 2015-02-24 SI SI201530503T patent/SI3110802T1/sl unknown
- 2015-02-24 HU HUE15706788A patent/HUE041392T2/hu unknown
- 2015-02-24 DK DK15706788.5T patent/DK3110802T3/en active
- 2015-02-24 MA MA39305A patent/MA39305A3/fr unknown
- 2015-02-24 CA CA2938009A patent/CA2938009A1/en not_active Abandoned
- 2015-02-24 TW TW104105911A patent/TWI576340B/zh not_active IP Right Cessation
- 2015-02-24 MX MX2016011099A patent/MX369819B/es active IP Right Grant
- 2015-02-24 RS RS20181482A patent/RS58208B1/sr unknown
-
2016
- 2016-07-19 IL IL246842A patent/IL246842B/en active IP Right Grant
- 2016-07-27 PH PH12016501481A patent/PH12016501481B1/en unknown
- 2016-07-28 ZA ZA2016/05243A patent/ZA201605243B/en unknown
- 2016-08-16 CL CL2016002064A patent/CL2016002064A1/es unknown
- 2016-08-24 US US15/245,955 patent/US9725416B2/en active Active
-
2018
- 2018-11-29 HR HRP20182016TT patent/HRP20182016T1/hr unknown
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