AR088765A1 - Derivados de etinilo - Google Patents
Derivados de etiniloInfo
- Publication number
- AR088765A1 AR088765A1 ARP120103715A ARP120103715A AR088765A1 AR 088765 A1 AR088765 A1 AR 088765A1 AR P120103715 A ARP120103715 A AR P120103715A AR P120103715 A ARP120103715 A AR P120103715A AR 088765 A1 AR088765 A1 AR 088765A1
- Authority
- AR
- Argentina
- Prior art keywords
- lower alkyl
- hydrogen
- lower alkoxy
- proviso
- halogen
- Prior art date
Links
Classifications
-
- 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
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
- C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/34—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
-
- 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
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
-
- 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
- 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
- A61P25/18—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
- A61P25/28—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-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
- C07D237/20—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-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
- C07D237/22—Nitrogen and oxygen atoms
-
- 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
- C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Liquid Crystal (AREA)
Abstract
La presente se refiere a derivados de etinilo de la fórmula (1) en la que: Y es N o CH; con la condición de que Y solamente puede ser CH, si por lo menos uno de U, V o W es N; U es N o C-R⁴; V y W son con independencia N o CH; con la condición de que solamente uno de U, V o W pueda ser simultáneamente nitrógeno; R⁴ es hidrógeno, metilo o halógeno; R¹ es fenilo o heteroarilo, que están opcionalmente sustituidos por halógeno, alquilo inferior o alcoxi inferior; R es hidrógeno o alquilo inferior; R² es hidrógeno, alquilo inferior, alcoxi inferior, CF₃ o S-alquilo inferior; R³/R³ son con independencia entre sí hidrógeno, alquilo inferior o alcoxi inferior; o R³ y R³ juntos forman un anillo cicloalquilo C₃₋₅, tetrahidrofurano u oxetano; o una sal de adición de ácido farmacéuticamente aceptable, una mezcla racémica, o los correspondientes enantiómeros y/o isómeros ópticos y/o estereoisómeros de los mismos. Se ha encontrado que los compuestos de la fórmula general (1) son moduladores alostéricos del receptor metabotrópico de glutamato del subtipo 5 (mGluR5).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11184257 | 2011-10-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR088765A1 true AR088765A1 (es) | 2014-07-02 |
Family
ID=47016705
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120103715A AR088765A1 (es) | 2011-10-07 | 2012-10-05 | Derivados de etinilo |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US8530472B2 (es) |
| EP (1) | EP2763969B1 (es) |
| JP (1) | JP5840794B2 (es) |
| KR (1) | KR101656966B1 (es) |
| CN (1) | CN103857658B (es) |
| AR (1) | AR088765A1 (es) |
| BR (1) | BR112014008078A2 (es) |
| CA (1) | CA2847096A1 (es) |
| CL (1) | CL2014000818A1 (es) |
| CO (1) | CO6900142A2 (es) |
| CR (1) | CR20140093A (es) |
| CY (1) | CY1117212T1 (es) |
| DK (1) | DK2763969T3 (es) |
| EA (1) | EA024993B1 (es) |
| ES (1) | ES2556796T3 (es) |
| HK (1) | HK1193596A1 (es) |
| HR (1) | HRP20160144T1 (es) |
| HU (1) | HUE026626T2 (es) |
| IL (1) | IL231439A (es) |
| IN (1) | IN2014CN02477A (es) |
| MX (1) | MX354414B (es) |
| PE (1) | PE20141555A1 (es) |
| PL (1) | PL2763969T3 (es) |
| PT (1) | PT2763969E (es) |
| RS (1) | RS54511B1 (es) |
| SG (1) | SG11201401307WA (es) |
| SI (1) | SI2763969T1 (es) |
| TW (1) | TWI458710B (es) |
| UA (1) | UA110995C2 (es) |
| WO (1) | WO2013050460A1 (es) |
| ZA (1) | ZA201402068B (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA113223C2 (xx) * | 2012-08-13 | 2016-12-26 | Арилетинілпіримідини | |
| PE20150733A1 (es) * | 2012-10-18 | 2015-05-17 | Hoffmann La Roche | Derivados de etinilo como moduladores de la actividad del receptor mglur5 |
| KR102035048B1 (ko) | 2015-06-03 | 2019-10-22 | 에프. 호프만-라 로슈 아게 | 에틴일 유도체 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002008205A1 (en) * | 2000-07-24 | 2002-01-31 | Krenitsky Pharmaceuticals, Inc. | Substituted 5-alkynyl pyrimidines having neurotrophic activity |
| GB0325956D0 (en) | 2003-11-06 | 2003-12-10 | Addex Pharmaceuticals Sa | Novel compounds |
| US7776869B2 (en) | 2004-10-18 | 2010-08-17 | Amgen Inc. | Heteroaryl-substituted alkyne compounds and method of use |
| EP1809620B1 (en) | 2004-11-04 | 2010-12-29 | Addex Pharma SA | Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors |
| PL1863818T3 (pl) * | 2005-03-23 | 2010-08-31 | Hoffmann La Roche | Pochodne acetylenylo-pirazolo-pirymidyny jako antagoniści MGLUR2 |
| GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
| SG185285A1 (en) | 2007-06-03 | 2012-11-29 | Univ Vanderbilt | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| US8853392B2 (en) | 2007-06-03 | 2014-10-07 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
| TW201010984A (en) | 2008-07-29 | 2010-03-16 | Boehringer Ingelheim Int | 5-alkynyl-pyrimidines |
| US8389536B2 (en) * | 2009-10-27 | 2013-03-05 | Hoffmann-La Roche Inc. | Positive allosteric modulators (PAM) |
-
2012
- 2012-04-10 UA UAA201404417A patent/UA110995C2/uk unknown
- 2012-09-27 US US13/628,128 patent/US8530472B2/en active Active
- 2012-10-04 PT PT127721009T patent/PT2763969E/pt unknown
- 2012-10-04 KR KR1020147011407A patent/KR101656966B1/ko active IP Right Grant
- 2012-10-04 DK DK12772100.9T patent/DK2763969T3/en active
- 2012-10-04 EA EA201490720A patent/EA024993B1/ru not_active IP Right Cessation
- 2012-10-04 IN IN2477CHN2014 patent/IN2014CN02477A/en unknown
- 2012-10-04 RS RS20160021A patent/RS54511B1/en unknown
- 2012-10-04 HU HUE12772100A patent/HUE026626T2/en unknown
- 2012-10-04 PE PE2014000497A patent/PE20141555A1/es active IP Right Grant
- 2012-10-04 EP EP12772100.9A patent/EP2763969B1/en active Active
- 2012-10-04 BR BR112014008078A patent/BR112014008078A2/pt not_active Application Discontinuation
- 2012-10-04 PL PL12772100T patent/PL2763969T3/pl unknown
- 2012-10-04 CN CN201280049441.XA patent/CN103857658B/zh active Active
- 2012-10-04 MX MX2014003636A patent/MX354414B/es active IP Right Grant
- 2012-10-04 TW TW101136751A patent/TWI458710B/zh not_active IP Right Cessation
- 2012-10-04 SG SG11201401307WA patent/SG11201401307WA/en unknown
- 2012-10-04 JP JP2014533888A patent/JP5840794B2/ja active Active
- 2012-10-04 CA CA2847096A patent/CA2847096A1/en not_active Abandoned
- 2012-10-04 ES ES12772100.9T patent/ES2556796T3/es active Active
- 2012-10-04 SI SI201230401T patent/SI2763969T1/sl unknown
- 2012-10-04 WO PCT/EP2012/069605 patent/WO2013050460A1/en active Application Filing
- 2012-10-05 AR ARP120103715A patent/AR088765A1/es unknown
-
2014
- 2014-02-26 CR CR20140093A patent/CR20140093A/es unknown
- 2014-02-28 CO CO14043441A patent/CO6900142A2/es unknown
- 2014-03-10 IL IL231439A patent/IL231439A/en active IP Right Grant
- 2014-03-20 ZA ZA2014/02068A patent/ZA201402068B/en unknown
- 2014-04-03 CL CL2014000818A patent/CL2014000818A1/es unknown
- 2014-07-08 HK HK14106901.9A patent/HK1193596A1/zh unknown
-
2016
- 2016-02-08 HR HRP20160144TT patent/HRP20160144T1/hr unknown
- 2016-02-18 CY CY20161100141T patent/CY1117212T1/el unknown
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