CR20160384A - Derivados de etilino - Google Patents
Derivados de etilinoInfo
- Publication number
- CR20160384A CR20160384A CR20160384A CR20160384A CR20160384A CR 20160384 A CR20160384 A CR 20160384A CR 20160384 A CR20160384 A CR 20160384A CR 20160384 A CR20160384 A CR 20160384A CR 20160384 A CR20160384 A CR 20160384A
- Authority
- CR
- Costa Rica
- Prior art keywords
- lower alkyl
- hydrogen
- halogen
- optionally substituted
- pyridinyl
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Psychology (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invención se refiere a compuestos de fórmula I en el que Y es N o C-R1¿; R1¿ es hidrógeno o F; R1 es hidrógeno, halógeno o alquilo inferior sustituido con halógeno; R2 es hidrógeno o alquilo inferior; o R2 forma junto con R4 un anillo heterocíclico de 6 miembros que contiene ¿CH2-CH2-O-CH2- o ¿CH2-CH2-NR-C(O); R es hidrógeno, alquilo inferior, fenilo o bencilo; R3 es fenilo o piridinilo, en el que el átomo de N en el grupo de piridinilo puede estar en diferentes posiciones; R4¿ es hidrógeno, alquilo inferior o alcoxialquilo inferior; R4 es hidrógeno, alquilo inferior, fenilo opcionalmente sustituido con halógeno o alcoxi inferior, o es cicloalquilo, o es piridinilo opcionalmente sustituido con halógeno, alquilo inferior, alcoxi inferior o =O, o es pirimidinilo opcionalmente sustituido con alquilo inferior, alcoxi inferior o =O, o es 1-alquilo inferior-piridinilo, o es pirazinilo, o es piridazinilo opcionalmente sustituido con alquilo inferior, alcoxi inferior o =O, o es 1-metilpirrolo[2,3-b]piridin-5-il, o es 6-imidazo[1,2-b]piridazin-6-il; o R4 forma junto con R4¿ un anillo heterocíclico de 4, 5 o 6 miembros que contiene ¿(CH2)5-, -CH2-CH2-O-CH2-CH2-, -CH2-CH2-CH2-, -CH2-CH2-CH2-CH2-, -CH2-O-CH2-CH2- o CH2-CH2-CH2-O-CH2; R5 y R5¿ son hidrógeno o alquilo inferior; o R4 forma junto con R5 un anillo saturado de 5 miembros que contiene -CH2-CH2-CH2-; o a una sal farmacéuticamente aceptable o sal de adición de ácido, a una mezcla racémica, o a su correspondiente enantiómero y/o isómero óptico y/o estereoisómeros del mismo.
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 (1)
| Publication Number | Publication Date |
|---|---|
| CR20160384A true CR20160384A (es) | 2016-11-07 |
Family
ID=50151209
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20160384A CR20160384A (es) | 2014-02-25 | 2015-02-24 | Derivados de etilino |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US9725416B2 (es) |
| EP (1) | EP3110802B1 (es) |
| JP (1) | JP6286577B2 (es) |
| KR (1) | KR101792452B1 (es) |
| CN (1) | CN106029649B (es) |
| AR (1) | AR099529A1 (es) |
| AU (1) | AU2015222303B2 (es) |
| BR (1) | BR112016017816A8 (es) |
| CA (1) | CA2938009A1 (es) |
| CL (1) | CL2016002064A1 (es) |
| CR (1) | CR20160384A (es) |
| DK (1) | DK3110802T3 (es) |
| EA (1) | EA029261B1 (es) |
| ES (1) | ES2701167T3 (es) |
| HR (1) | HRP20182016T1 (es) |
| HU (1) | HUE041392T2 (es) |
| IL (1) | IL246842B (es) |
| LT (1) | LT3110802T (es) |
| MA (1) | MA39305A3 (es) |
| MX (1) | MX369819B (es) |
| PE (1) | PE20161415A1 (es) |
| PH (1) | PH12016501481A1 (es) |
| PL (1) | PL3110802T3 (es) |
| PT (1) | PT3110802T (es) |
| RS (1) | RS58208B1 (es) |
| SG (1) | SG11201607010XA (es) |
| SI (1) | SI3110802T1 (es) |
| TW (1) | TWI576340B (es) |
| UA (1) | UA117855C2 (es) |
| WO (1) | WO2015128307A1 (es) |
| ZA (1) | ZA201605243B (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3271353B1 (en) | 2015-03-19 | 2019-11-27 | H. Hoffnabb-La Roche Ag | 3-(4-ethynylphenyl)hexahydropyrimidin-2,4-dione derivatives as modulators of mglur4 |
| MA42508B1 (fr) | 2015-06-03 | 2020-05-29 | Hoffmann La Roche | Dérivés d'éthynyle |
| LT3322701T (lt) | 2015-07-15 | 2019-07-10 | F. Hoffmann-La Roche Ag | Etinilo dariniai kaip metabotropinių glutamato receptorių moduliatoriai |
| AR105556A1 (es) * | 2015-08-03 | 2017-10-18 | Hoffmann La Roche | Derivados de etinilo |
| PL3484889T3 (pl) * | 2016-07-18 | 2020-12-28 | F. Hoffmann-La Roche Ag | Pochodne etynylu |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2012114770A (ru) * | 2009-09-04 | 2013-10-10 | Вандербилт Юниверсити | АЛЛОСТЕРИЧЕСКИЕ СРЕДСТВА ПОТЕНЦИРОВАНИЯ mGluR4, КОМПОЗИЦИИ И СПОСОБЫ ЛЕЧЕНИЯ НЕВРОЛОГИЧЕСКИХ ДИСФУНКЦИЙ |
| 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 |
| PE20160666A1 (es) * | 2013-09-25 | 2016-07-09 | Hoffmann La Roche | Derivados de etinilo |
| 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 PT PT15706788T patent/PT3110802T/pt unknown
- 2015-02-24 HU HUE15706788A patent/HUE041392T2/hu unknown
- 2015-02-24 AU AU2015222303A patent/AU2015222303B2/en not_active Ceased
- 2015-02-24 CR CR20160384A patent/CR20160384A/es unknown
- 2015-02-24 RS RS20181482A patent/RS58208B1/sr unknown
- 2015-02-24 SG SG11201607010XA patent/SG11201607010XA/en unknown
- 2015-02-24 CA CA2938009A patent/CA2938009A1/en not_active Abandoned
- 2015-02-24 SI SI201530503T patent/SI3110802T1/sl unknown
- 2015-02-24 CN CN201580010032.2A patent/CN106029649B/zh active Active
- 2015-02-24 MA MA39305A patent/MA39305A3/fr unknown
- 2015-02-24 PL PL15706788T patent/PL3110802T3/pl unknown
- 2015-02-24 UA UAA201609882A patent/UA117855C2/uk unknown
- 2015-02-24 BR BR112016017816A patent/BR112016017816A8/pt not_active Application Discontinuation
- 2015-02-24 TW TW104105911A patent/TWI576340B/zh not_active IP Right Cessation
- 2015-02-24 DK DK15706788.5T patent/DK3110802T3/en active
- 2015-02-24 ES ES15706788T patent/ES2701167T3/es active Active
- 2015-02-24 PE PE2016001503A patent/PE20161415A1/es unknown
- 2015-02-24 KR KR1020167023095A patent/KR101792452B1/ko active IP Right Grant
- 2015-02-24 EP EP15706788.5A patent/EP3110802B1/en active Active
- 2015-02-24 MX MX2016011099A patent/MX369819B/es active IP Right Grant
- 2015-02-24 AR ARP150100537A patent/AR099529A1/es unknown
- 2015-02-24 WO PCT/EP2015/053785 patent/WO2015128307A1/en active Application Filing
- 2015-02-24 JP JP2016554209A patent/JP6286577B2/ja active Active
- 2015-02-24 LT LTEP15706788.5T patent/LT3110802T/lt unknown
- 2015-02-24 EA EA201691690A patent/EA029261B1/ru not_active IP Right Cessation
-
2016
- 2016-07-19 IL IL246842A patent/IL246842B/en active IP Right Grant
- 2016-07-27 PH PH12016501481A patent/PH12016501481A1/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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