CY1116119T1 - Παραγωγα ισοξαζολο-πυριδινης - Google Patents
Παραγωγα ισοξαζολο-πυριδινηςInfo
- Publication number
- CY1116119T1 CY1116119T1 CY20151100262T CY151100262T CY1116119T1 CY 1116119 T1 CY1116119 T1 CY 1116119T1 CY 20151100262 T CY20151100262 T CY 20151100262T CY 151100262 T CY151100262 T CY 151100262T CY 1116119 T1 CY1116119 T1 CY 1116119T1
- Authority
- CY
- Cyprus
- Prior art keywords
- optionally substituted
- group
- 7alkyl
- isoxazolo
- halo
- Prior art date
Links
- NABZXASCLFSKLF-UHFFFAOYSA-N [1,2]oxazolo[4,3-b]pyridine Chemical compound C1=CC=NC2=CON=C21 NABZXASCLFSKLF-UHFFFAOYSA-N 0.000 title abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229960003692 gamma aminobutyric acid Drugs 0.000 abstract 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- A61P25/28—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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- C07D491/08—Bridged 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
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)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Η παρούσα εφεύρεση αναφέρεται σε παράγωγα ισοξαζολο-πυριδίνης του τύπου (I) όπου: το Χ είναι Ο ή ΝΗ, το R1 είναι φαινυλο ομάδα, πυριδινυλο ομάδα ή πυριμιδινυλο ομάδα, κάθε μία προαιρετικώς υποκατεστημένη με 1, 2 ή 3 αλο ομάδες, το R2 είναι Η ή CH3 ή CF3, τα R3, R4, R5 και R6 ανεξαρτήτως το καθένα είναι Η, προαιρετικώς υποκατεστημένη C1-7αλκυλο ομάδα, προαιρετικώς υποκατεστημένη C1-7αλκοξυ ομάδα, CN, αλο ομάδα, ΝΟ2, S-C1-7αλκυλο ομάδα, S(O)-C1-7αλκυλο ομάδα, προαιρετικώς υποκατεστημένη βενζυλοξυ ομάδα, -C(O)-Ra, -C(O)-NRbRc ή ένα φαρμακευτικώς αποδεκτό άλας αυτών. Οι ενώσεις είναι ενεργές στη θέση δέσμευσης του υποδοχέα GABA Α α5 και χρήσιμες για τη θεραπευτική αντιμετώπιση γνωστικών διαταραχών, όπως η νόσος του Alzheimer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07122240 | 2007-12-04 | ||
| EP08857137.7A EP2227467B1 (en) | 2007-12-04 | 2008-11-26 | Isoxazolo-pyridine derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1116119T1 true CY1116119T1 (el) | 2017-02-08 |
Family
ID=40329314
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20151100262T CY1116119T1 (el) | 2007-12-04 | 2015-03-16 | Παραγωγα ισοξαζολο-πυριδινης |
| CY20151100999T CY1116902T1 (el) | 2007-12-04 | 2015-11-09 | Παραγωγα ισοξαζολο-πυριδινης |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20151100999T CY1116902T1 (el) | 2007-12-04 | 2015-11-09 | Παραγωγα ισοξαζολο-πυριδινης |
Country Status (33)
| Country | Link |
|---|---|
| US (6) | US20090143371A1 (el) |
| EP (2) | EP2227467B1 (el) |
| JP (1) | JP5301557B2 (el) |
| KR (2) | KR101237576B1 (el) |
| CN (1) | CN101889010B (el) |
| AR (1) | AR069523A1 (el) |
| AU (1) | AU2008333326B2 (el) |
| BR (1) | BRPI0820112B8 (el) |
| CA (1) | CA2707648C (el) |
| CL (1) | CL2008003591A1 (el) |
| CO (1) | CO6351788A2 (el) |
| CR (1) | CR11454A (el) |
| CY (2) | CY1116119T1 (el) |
| DK (2) | DK2227467T3 (el) |
| EC (1) | ECSP10010230A (el) |
| ES (2) | ES2550994T3 (el) |
| HR (2) | HRP20150348T1 (el) |
| HU (1) | HUE025545T2 (el) |
| IL (1) | IL205759A (el) |
| MA (1) | MA31865B1 (el) |
| MX (1) | MX2010005717A (el) |
| MY (1) | MY156747A (el) |
| NZ (1) | NZ585308A (el) |
| PE (2) | PE20091073A1 (el) |
| PL (2) | PL2767536T3 (el) |
| PT (2) | PT2227467E (el) |
| RS (2) | RS53877B1 (el) |
| RU (1) | RU2484091C2 (el) |
| SI (2) | SI2227467T1 (el) |
| TW (1) | TWI363624B (el) |
| UA (1) | UA100132C2 (el) |
| WO (1) | WO2009071476A1 (el) |
| ZA (1) | ZA201003631B (el) |
Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2227467E (pt) | 2007-12-04 | 2015-03-02 | Hoffmann La Roche | Derivados de isoxazol-piridina |
| NZ592603A (en) * | 2008-10-21 | 2013-02-22 | Metabolex Inc | Aryl gpr120 receptor agonists and uses thereof |
| EP2942346B1 (en) | 2009-02-17 | 2020-05-06 | Syntrix Biosystems, Inc. | Pyridinecarboxamides as cxcr2 modulators |
| US8389550B2 (en) * | 2009-02-25 | 2013-03-05 | Hoffmann-La Roche Inc. | Isoxazoles / O-pyridines with ethyl and ethenyl linker |
| US8222246B2 (en) * | 2009-04-02 | 2012-07-17 | Hoffmann-La Roche Inc. | Substituted isoxazoles |
| US20100280019A1 (en) * | 2009-04-30 | 2010-11-04 | Roland Jakob-Roetne | Isoxazoles |
| MX2011011273A (es) * | 2009-05-05 | 2011-11-04 | Hoffmann La Roche | Derivados de isoxazol-pirazol. |
| CA2759598C (en) * | 2009-05-05 | 2017-09-12 | F. Hoffmann-La Roche Ag | Isoxazole-thiazole derivatives as gaba a receptor inverse agonists for use in the treatment of cognitive disorders |
| AU2010244553A1 (en) * | 2009-05-05 | 2011-12-01 | F. Hoffmann-La Roche Ag | Isoxazole-pyridine derivatives |
| ES2430223T3 (es) * | 2009-05-07 | 2013-11-19 | F. Hoffmann-La Roche Ag | Derivados de isoxazol-piridina como moduladores de GABA |
| EP2482657A4 (en) * | 2009-09-21 | 2013-05-15 | Univ Vanderbilt | O-BENZYL-NICOTINAMIDANALOGA AS POSITIVE ALLOSTERIC MGLUR5 MODULATORS |
| KR20120117905A (ko) | 2010-01-28 | 2012-10-24 | 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 | 프로테아좀 활성을 향상시키는 조성물 및 방법 |
| BR112013001237A2 (pt) | 2010-07-19 | 2016-05-17 | Syngenta Participations Ag | compostos de isoxazola, isoatiazola, furano e tiofeno como microbicidas |
| CN103003265A (zh) | 2010-07-19 | 2013-03-27 | 先正达参股股份有限公司 | 杀微生物剂 |
| WO2012027289A1 (en) | 2010-08-23 | 2012-03-01 | Syntrix Biosystems Inc. | Aminopyridine- and aminopyrimidinecarboxamides as cxcr2 modulators |
| EP2635277B1 (en) * | 2010-11-05 | 2018-12-19 | F.Hoffmann-La Roche Ag | Use of active pharmaceutical compounds for the treatment of central nervous system conditions |
| EP2457569A1 (en) | 2010-11-05 | 2012-05-30 | F. Hoffmann-La Roche AG | Use of active pharmaceutical compounds for the treatment of central nervous system conditions |
| PT2707101T (pt) | 2011-05-12 | 2019-05-30 | Proteostasis Therapeutics Inc | Reguladores da proteostase |
| US8604062B2 (en) * | 2011-10-20 | 2013-12-10 | Hoffman-La Roche Inc. | Process for the preparation of isoxazolyl-methoxy nicotinic acids |
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| JP6242810B2 (ja) | 2011-12-28 | 2017-12-06 | グローバル・ブラッド・セラピューティクス・インコーポレイテッドGlobal Blood Therapeutics,Inc. | 置換ベンズアルデヒド化合物および組織酸素化の増加におけるそれらの使用方法 |
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| MX379228B (es) | 2013-03-15 | 2025-03-10 | Global Blood Therapeutics Inc | Compuestos y usos de estos para la modulación de la hemoglobina. |
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| US8969365B2 (en) | 2013-08-02 | 2015-03-03 | Syntrix Biosystems, Inc. | Thiopyrimidinecarboxamides as CXCR1/2 modulators |
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| MA41841A (fr) | 2015-03-30 | 2018-02-06 | Global Blood Therapeutics Inc | Composés aldéhyde pour le traitement de la fibrose pulmonaire, de l'hypoxie, et de maladies auto-immunes et des tissus conjonctifs |
| CN106810542B (zh) * | 2015-11-30 | 2021-03-09 | 苏州开拓药业股份有限公司 | 一种硫代咪唑烷酮化合物的晶型、盐型及其制备方法 |
| FI3383392T3 (fi) | 2015-12-04 | 2025-09-11 | Global Blood Therapeutics Inc | Annosteluohjelmat 2-hydroksi-6-((2-(1-isopropyyli-1h-pyratsol-5-yyli)pyridin-3-yyli)metoksi)bentsaldehydille |
| TWI752307B (zh) | 2016-05-12 | 2022-01-11 | 美商全球血液治療公司 | 新穎化合物及製造化合物之方法 |
| TWI778983B (zh) | 2016-10-12 | 2022-10-01 | 美商全球血液治療公司 | 包含2-羥基-6-((2-(1-異丙基-1h-吡唑-5-基)吡啶-3-基)甲氧基)-苯甲醛之片劑 |
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| BR112020004116A2 (pt) * | 2017-08-28 | 2020-09-01 | University Of Maryland, Baltimore | novos moduladores do receptor de ácido gama aminobutírico tipo a para distúrbios de humor |
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| WO2021191837A1 (en) | 2020-03-26 | 2021-09-30 | Richter Gedeon Nyrt. | 1,3-dihydro-2h-pyrrolo[3,4-c]pyridine derivatives as gabaa α5 receptor modulators |
| CA3216863A1 (en) | 2021-05-05 | 2022-11-10 | University College Cardiff Consultants Limited | Heteroaryl compounds useful in the treatment of cognitive disorders |
| CN116854680A (zh) * | 2022-03-28 | 2023-10-10 | 上海赛默罗生物科技有限公司 | 异噁唑-杂环类衍生物、药物组合物和用途 |
| CN115286636A (zh) * | 2022-10-08 | 2022-11-04 | 上海赛默罗生物科技有限公司 | 烟酰胺晶型及其制备方法和用途 |
| TW202448433A (zh) * | 2023-06-05 | 2024-12-16 | 大陸商武漢人福創新藥物研發中心有限公司 | 作為α5-GABAA受體調節劑的雜環化合物及其用途 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3812225A1 (de) * | 1988-04-13 | 1989-10-26 | Basf Ag | Isoxazol(isothiazol)-5-carbonsaeureamide |
| ATE315033T1 (de) | 1998-08-07 | 2006-02-15 | Chiron Corp | Subtituierte isoxazole derivate als estrogen rezeptor modulatore |
| DE19920791A1 (de) * | 1999-05-06 | 2000-11-09 | Bayer Ag | Substituierte Benzoylisoxazole |
| GB0125086D0 (en) | 2001-10-18 | 2001-12-12 | Merck Sharp & Dohme | Novel compounds |
| WO2003099793A1 (en) | 2002-05-24 | 2003-12-04 | Takeda Pharmaceutical Company Limited | 1,2-azole derivatives with hypoglycemic and hypolipidemic activity |
| GB0221443D0 (en) * | 2002-09-16 | 2002-10-23 | Glaxo Group Ltd | Pyridine derivates |
| MXPA06013196A (es) * | 2004-05-14 | 2007-02-14 | Irm Llc | Compuestos y composiciones como moduladores del receptor activado por proliferador de peroxisoma (ppar). |
| ES2315912T3 (es) * | 2004-10-01 | 2009-04-01 | F. Hoffmann-La Roche Ag | Derivados de eter sustituido por hexafluorisopropanol. |
| US7700620B2 (en) * | 2005-06-27 | 2010-04-20 | Bristol-Myers Squibb Company | C-linked cyclic antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions |
| AU2006298867A1 (en) * | 2005-09-19 | 2007-04-12 | F. Hoffmann-La Roche Ag | Isoxazolo derivatives as GABA A alpha5 inverse agonists |
| CA2625301A1 (en) * | 2005-10-11 | 2007-04-19 | F. Hoffmann-La Roche Ag | Isoxazole derivatives |
| EP1968972B1 (en) * | 2005-12-23 | 2012-11-28 | F. Hoffmann-La Roche AG | Aryl-isoxazolo-4-yl-oxadiazole derivatives |
| BRPI0620760A2 (pt) | 2005-12-27 | 2011-11-22 | Hoffmann La Roche | derivados de aril-isoxazol-4-il-imidazo[1,5]piridina |
| WO2007074078A2 (en) | 2005-12-27 | 2007-07-05 | F. Hoffmann-La Roche Ag | Aryl-isoxazol-4-yl-imidazole derivatives |
| AU2007207053B2 (en) | 2006-01-17 | 2012-05-24 | F. Hoffmann-La Roche Ag | Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine useful for the treatment of Alzheimer's disease via GABA receptors |
| CA2706990C (en) | 2007-12-04 | 2016-05-10 | F. Hoffmann-La Roche Ag | Isoxazolo-pyrazine derivatives |
| US7943619B2 (en) | 2007-12-04 | 2011-05-17 | Hoffmann-La Roche Inc. | Isoxazolo-pyridazine derivatives |
| PT2227467E (pt) | 2007-12-04 | 2015-03-02 | Hoffmann La Roche | Derivados de isoxazol-piridina |
| US20100280019A1 (en) * | 2009-04-30 | 2010-11-04 | Roland Jakob-Roetne | Isoxazoles |
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2008
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