CY1117212T1 - Εθυνυλο παραγωγα ως μεταβοτροπικοι ρυθμιστες του υποδοχεα γλουταμινικου - Google Patents
Εθυνυλο παραγωγα ως μεταβοτροπικοι ρυθμιστες του υποδοχεα γλουταμινικουInfo
- Publication number
- CY1117212T1 CY1117212T1 CY20161100141T CY161100141T CY1117212T1 CY 1117212 T1 CY1117212 T1 CY 1117212T1 CY 20161100141 T CY20161100141 T CY 20161100141T CY 161100141 T CY161100141 T CY 161100141T CY 1117212 T1 CY1117212 T1 CY 1117212T1
- Authority
- CY
- Cyprus
- Prior art keywords
- hydrogen
- lower alkyl
- alkyl
- derivators
- glutaminic
- Prior art date
Links
Classifications
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- 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
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- 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
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- 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
- 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
- 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
Η παρούσα εφεύρεση σχετίζεται με παράγωγα αιθυνυλίου του τύπου Ι όπου η Υ είναι Ν ή CH· με τον όρο ότι η Υ μπορεί να είναι μόνο CH, αν τουλάχιστον μία των U, V ή W είναι Ν· η U είναι Ν ή C-R4· οι V και W είναι ανεξαρτήτως Ν ή CH· με τον όρο ότι μόνο μία των U, V ή W μπορεί να είναι ταυτόχρονα άζωτο· η R4 είναι υδρογόνο, μεθύλιο ή αλογόνο· η R1 είναι φαινύλιο ή ετεροαρύλιο, τα οποία προαιρετικώς είναι υποκατεστημένα με αλογόνο, κατώτερο αλκύλιο ή κατώτερο άλκοξυ· η R είναι υδρογόνο ή κατώτερο αλκύλιο· η R2 είναι υδρογόνο, κατώτερο αλκύλιο, κατώτερο άλκοξυ, CF3 ή S-κατώτερο αλκύλιο· είναι ανεξαρτήτως μεταξύ των υδρογόνο, κατώτερο αλκύλιο ή κατώτερο άλκοξυ· ή οι R3 και R3 σχηματίζουν μαζί δακτύλιο C3-5-κυκλοαλκυλίου, τετραϋδροφουρανίου ή οξετανίου· ή με άλας προσθήκης οξέος φαρμακευτικώς αποδεκτό, με ρακεμικό μίγμα, ή με το αντίστοιχο εναντιομερές και/ή οπτικό ισομερές και/ή στερεοϊσομερές αυτού. Βρέθηκε ότι οι ενώσεις του γενικού τύπου I είναι αλλοστερικοί ρυθμιστές του μεταβοτροπικού υποδοχέα γλουταμινικού υποτύπου 5 (mGluR5).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11184257 | 2011-10-07 | ||
| EP12772100.9A EP2763969B1 (en) | 2011-10-07 | 2012-10-04 | Ethynyl derivatives as metabotropic glutamate receptor modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1117212T1 true CY1117212T1 (el) | 2017-04-05 |
Family
ID=47016705
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20161100141T CY1117212T1 (el) | 2011-10-07 | 2016-02-18 | Εθυνυλο παραγωγα ως μεταβοτροπικοι ρυθμιστες του υποδοχεα γλουταμινικου |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US8530472B2 (el) |
| EP (1) | EP2763969B1 (el) |
| JP (1) | JP5840794B2 (el) |
| KR (1) | KR101656966B1 (el) |
| CN (1) | CN103857658B (el) |
| AR (1) | AR088765A1 (el) |
| BR (1) | BR112014008078A2 (el) |
| CA (1) | CA2847096A1 (el) |
| CL (1) | CL2014000818A1 (el) |
| CO (1) | CO6900142A2 (el) |
| CR (1) | CR20140093A (el) |
| CY (1) | CY1117212T1 (el) |
| DK (1) | DK2763969T3 (el) |
| EA (1) | EA024993B1 (el) |
| ES (1) | ES2556796T3 (el) |
| HK (1) | HK1193596A1 (el) |
| HR (1) | HRP20160144T1 (el) |
| HU (1) | HUE026626T2 (el) |
| IL (1) | IL231439A (el) |
| IN (1) | IN2014CN02477A (el) |
| MX (1) | MX354414B (el) |
| PE (1) | PE20141555A1 (el) |
| PL (1) | PL2763969T3 (el) |
| PT (1) | PT2763969E (el) |
| RS (1) | RS54511B1 (el) |
| SG (1) | SG11201401307WA (el) |
| SI (1) | SI2763969T1 (el) |
| TW (1) | TWI458710B (el) |
| UA (1) | UA110995C2 (el) |
| WO (1) | WO2013050460A1 (el) |
| ZA (1) | ZA201402068B (el) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA113223C2 (xx) * | 2012-08-13 | 2016-12-26 | Арилетинілпіримідини | |
| NZ703537A (en) * | 2012-10-18 | 2018-06-29 | Hoffmann La Roche | Ethynyl derivatives |
| CN107849006B (zh) | 2015-06-03 | 2020-11-13 | 豪夫迈·罗氏有限公司 | 乙炔基衍生物 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7205297B2 (en) * | 2000-07-24 | 2007-04-17 | 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 |
| RU2412943C2 (ru) | 2005-03-23 | 2011-02-27 | Ф. Хоффманн-Ля Рош Аг | ПРОИЗВОДНЫЕ АЦЕТИЛЕНИЛ-ПИРАЗОЛО-ПИРИМИДИНА В КАЧЕСТВЕ АНТАГОНИСТОВ mGluR2 |
| GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
| US8853392B2 (en) | 2007-06-03 | 2014-10-07 | Vanderbilt University | Benzamide mGluR5 positive allosteric modulators and methods of making and using same |
| WO2008151184A1 (en) | 2007-06-03 | 2008-12-11 | Vanderbilt University | Benzamide mglur5 positive allosteric modulators and methods of making and using same |
| PL2323992T3 (pl) | 2008-07-29 | 2017-01-31 | Boehringer Ingelheim International Gmbh | 5-alkinylo-pirymidyny |
| 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 PE PE2014000497A patent/PE20141555A1/es active IP Right Grant
- 2012-10-04 PL PL12772100T patent/PL2763969T3/pl unknown
- 2012-10-04 BR BR112014008078A patent/BR112014008078A2/pt not_active Application Discontinuation
- 2012-10-04 DK DK12772100.9T patent/DK2763969T3/en active
- 2012-10-04 HU HUE12772100A patent/HUE026626T2/en unknown
- 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 CN CN201280049441.XA patent/CN103857658B/zh active Active
- 2012-10-04 WO PCT/EP2012/069605 patent/WO2013050460A1/en active Application Filing
- 2012-10-04 ES ES12772100.9T patent/ES2556796T3/es active Active
- 2012-10-04 SG SG11201401307WA patent/SG11201401307WA/en unknown
- 2012-10-04 TW TW101136751A patent/TWI458710B/zh not_active IP Right Cessation
- 2012-10-04 JP JP2014533888A patent/JP5840794B2/ja active Active
- 2012-10-04 EP EP12772100.9A patent/EP2763969B1/en active Active
- 2012-10-04 MX MX2014003636A patent/MX354414B/es active IP Right Grant
- 2012-10-04 PT PT127721009T patent/PT2763969E/pt unknown
- 2012-10-04 CA CA2847096A patent/CA2847096A1/en not_active Abandoned
- 2012-10-04 KR KR1020147011407A patent/KR101656966B1/ko active IP Right Grant
- 2012-10-04 SI SI201230401T patent/SI2763969T1/sl unknown
- 2012-10-04 RS RS20160021A patent/RS54511B1/en unknown
- 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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