HRP20120961T1 - Spojevi tiazolilpirazolopirimidina kao sintetski međuprodukti i odgovarajući postupci sinteze - Google Patents
Spojevi tiazolilpirazolopirimidina kao sintetski međuprodukti i odgovarajući postupci sinteze Download PDFInfo
- Publication number
- HRP20120961T1 HRP20120961T1 HRP20120961AT HRP20120961T HRP20120961T1 HR P20120961 T1 HRP20120961 T1 HR P20120961T1 HR P20120961A T HRP20120961A T HR P20120961AT HR P20120961 T HRP20120961 T HR P20120961T HR P20120961 T1 HRP20120961 T1 HR P20120961T1
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- Croatia
- Prior art keywords
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- formula
- salt
- ethyl
- solvent
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Classifications
-
- 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
-
- 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
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (18)
1. Spoj formule
[image]
naznačen time što:
R1 i R2 su neovisno etil ili n-propil;
ili njegova sol.
2. Spoj u skladu s patentnim zahtjevom 1, ili njegova sol, naznačen time što svaki od R1 i R2 je etil.
3. Postupak sinteze u dobivanju spoja formule
[image]
gdje su R1 i R2 neovisno etil ili n-propil, naznačen time što se sastoji u koracima
i) reakcije spoja formule
[image]
ili njegove soli, s 2,4-diklortiazolom, ili njegovom solju, u prisutnosti bakrenog halogenida kao katalizatora, liganda, kojeg se bira između 1,10-fenantrolina i bipiridina, i baze, koju se bira između K3PO4 i Cs2CO3, kako bi se dobilo spoj formule
[image]
;
i
ii) reakcije produkta iz koraka i) s morfolinom, ili njegovom solju, u prisutnosti pogodne anorganske baze.
4. Postupak u skladu s patentnim zahtjevom 3, naznačen time što svaki od R1 i R2 je etil.
5. Postupak u skladu s patentnim zahtjevom 3 ili patentnim zahtjevom 4, naznačen time što bakreni halogenid je CuCl.
6. Postupak u skladu s bilo kojim od patentnih zahtjeva 3 do 5, naznačen time što ligand je 1,10-fenantrolin.
7. Postupak u skladu s bilo kojim od patentnih zahtjeva 3 do 6, naznačen time što baza u koraku i) je Cs2CO3.
8. Postupak u skladu s bilo kojim od patentnih zahtjeva 3 do 7, naznačen time što baza u koraku ii) je K2CO3.
9. Postupak u skladu s patentnim zahtjevom 3, naznačen time što svaki od R1 i R2 je etil, bakreni halogenid je CuCl, ligand je 1,10-fenantrolin, baza u koraku i) je Cs2CO3, a baza u koraku ii) je K2CO3.
10. Postupak u skladu s patentnim zahtjevom 9, naznačen time što otapalo za korak i) je 1,4-dioksan ili 2-metiltetrahidrofuran/N,N-dimetilacetamid, a otapalo za korak ii) je morfolinom, 2-metiltetrahidrofuran ili 2-propanol.
11. Postupak sinteze u dobivanju spoja formule
[image]
gdje su R1 i R2 neovisno etil ili n-propil, naznačen time što se sastoji u koracima
i) reakcije spoja formule
[image]
;
ili njegove soli, s morfolinom u suvišku, ili njegovom solju, u prisutnosti pogodnog otapala.
12. Postupak u skladu s patentnim zahtjevom 11, naznačen time što otapalo je 2-metiltetrahidrofuran.
13. Postupak u skladu s patentnim zahtjevom 11, naznačen time što otapalo je 2-propanol.
14. Postupak u skladu s bilo kojim od patentnih zahtjeva 11 do 13, naznačen time što svaki od R1 i R2 je etil.
15. Postupak sinteze u dobivanju spoja formule
[image]
gdje su R1 i R2 neovisno etil ili n-propil, naznačen time što se sastoji u koracima
i) reakcije spoja formule
[image]
ili njegove soli, s 2,4-diklortiazolom, ili njegovom solju, u prisutnosti bakrenog halogenida kao katalizatora, liganda, kojeg se bira između 1,10-fenantrolina i bipiridina, i baze, koju se bira između K3PO4 i Cs2CO3, kako bi se dobilo spoj formule
[image]
;
i
ii) reakcije produkta iz koraka i) s morfolinom u suvišku, ili njegovom solju, u pogodnom otapalu.
16. Postupak u skladu s patentnim zahtjevom 15, naznačen time što otapalo je 2-metiltetrahidrofuran.
17. Postupak u skladu s patentnim zahtjevom 15, naznačen time što otapalo je 2-propanol.
18. Postupak u skladu s bilo kojim od patentnih zahtjeva 15 do 17, naznačen time što svaki od R1 i R2 je etil.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10215308P | 2008-10-02 | 2008-10-02 | |
| PCT/US2009/058722 WO2010039678A1 (en) | 2008-10-02 | 2009-09-29 | Thiazolyl-pyrazolopyrimidine compounds as synthetic intermediates and related synthetic processes |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120961T1 true HRP20120961T1 (hr) | 2012-12-31 |
Family
ID=41507435
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120961AT HRP20120961T1 (hr) | 2008-10-02 | 2009-09-29 | Spojevi tiazolilpirazolopirimidina kao sintetski međuprodukti i odgovarajući postupci sinteze |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8563718B2 (hr) |
| EP (1) | EP2350079B1 (hr) |
| JP (1) | JP5524221B2 (hr) |
| KR (1) | KR101357392B1 (hr) |
| CN (1) | CN102171212A (hr) |
| AR (1) | AR073708A1 (hr) |
| AU (1) | AU2009298757B2 (hr) |
| BR (1) | BRPI0920838A2 (hr) |
| CA (1) | CA2739422C (hr) |
| CY (1) | CY1113499T1 (hr) |
| DK (1) | DK2350079T3 (hr) |
| EA (1) | EA018807B1 (hr) |
| ES (1) | ES2397509T3 (hr) |
| HR (1) | HRP20120961T1 (hr) |
| IL (1) | IL211292A (hr) |
| MX (1) | MX2011003529A (hr) |
| PL (1) | PL2350079T3 (hr) |
| PT (1) | PT2350079E (hr) |
| SI (1) | SI2350079T1 (hr) |
| TW (1) | TWI432435B (hr) |
| WO (1) | WO2010039678A1 (hr) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR112471A1 (es) * | 2017-08-14 | 2019-10-30 | Spruce Biosciences Inc | Antagonistas del receptor del factor liberador de corticotropina |
| CN118845788A (zh) | 2017-08-14 | 2024-10-29 | 云杉生物科学公司 | 促肾上腺皮质激素释放因子受体拮抗剂 |
| BR112023002497A2 (pt) | 2020-08-12 | 2023-05-02 | Spruce Biosciences Inc | Métodos e composições para tratamento da síndrome dos ovários policísticos |
| US11708372B2 (en) | 2021-11-19 | 2023-07-25 | Spruce Biosciences, Inc. | Crystalline composition of tildacerfont and methods of use and preparation thereof |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE161178T1 (de) * | 1992-06-10 | 1998-01-15 | Fujisawa Pharmaceutical Co | Pyrazolpyridine für die behandlung der anämie |
| AU2007297421B2 (en) * | 2006-09-20 | 2012-03-08 | Eli Lilly And Company | Thiazole pyrazolopyrimidines as CRF1 receptor antagonists |
| US8952207B2 (en) * | 2007-09-11 | 2015-02-10 | The University Of Houston System | Copper-catalyzed C—H bond arylation |
-
2009
- 2009-09-29 TW TW098132999A patent/TWI432435B/zh not_active IP Right Cessation
- 2009-09-29 WO PCT/US2009/058722 patent/WO2010039678A1/en active Application Filing
- 2009-09-29 CN CN2009801388897A patent/CN102171212A/zh active Pending
- 2009-09-29 BR BRPI0920838A patent/BRPI0920838A2/pt not_active IP Right Cessation
- 2009-09-29 EP EP09736733A patent/EP2350079B1/en active Active
- 2009-09-29 US US13/063,226 patent/US8563718B2/en active Active
- 2009-09-29 PL PL09736733T patent/PL2350079T3/pl unknown
- 2009-09-29 HR HRP20120961AT patent/HRP20120961T1/hr unknown
- 2009-09-29 MX MX2011003529A patent/MX2011003529A/es active IP Right Grant
- 2009-09-29 CA CA2739422A patent/CA2739422C/en active Active
- 2009-09-29 ES ES09736733T patent/ES2397509T3/es active Active
- 2009-09-29 KR KR1020117007555A patent/KR101357392B1/ko not_active Expired - Fee Related
- 2009-09-29 SI SI200930463T patent/SI2350079T1/sl unknown
- 2009-09-29 AU AU2009298757A patent/AU2009298757B2/en not_active Ceased
- 2009-09-29 DK DK09736733.8T patent/DK2350079T3/da active
- 2009-09-29 AR ARP090103753A patent/AR073708A1/es not_active Application Discontinuation
- 2009-09-29 JP JP2011530133A patent/JP5524221B2/ja active Active
- 2009-09-29 EA EA201170526A patent/EA018807B1/ru not_active IP Right Cessation
- 2009-09-29 PT PT97367338T patent/PT2350079E/pt unknown
-
2011
- 2011-02-17 IL IL211292A patent/IL211292A/en not_active IP Right Cessation
-
2012
- 2012-12-27 CY CY20121101263T patent/CY1113499T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2739422C (en) | 2013-03-12 |
| KR20110063513A (ko) | 2011-06-10 |
| DK2350079T3 (da) | 2012-12-17 |
| JP2012504626A (ja) | 2012-02-23 |
| CN102171212A (zh) | 2011-08-31 |
| US8563718B2 (en) | 2013-10-22 |
| MX2011003529A (es) | 2011-04-21 |
| EP2350079A1 (en) | 2011-08-03 |
| CY1113499T1 (el) | 2016-06-22 |
| ES2397509T3 (es) | 2013-03-07 |
| PT2350079E (pt) | 2012-12-20 |
| BRPI0920838A2 (pt) | 2018-10-16 |
| AR073708A1 (es) | 2010-11-24 |
| TWI432435B (zh) | 2014-04-01 |
| SI2350079T1 (sl) | 2013-02-28 |
| TW201018692A (en) | 2010-05-16 |
| IL211292A0 (en) | 2011-04-28 |
| JP5524221B2 (ja) | 2014-06-18 |
| KR101357392B1 (ko) | 2014-02-03 |
| AU2009298757A1 (en) | 2010-04-08 |
| EA018807B1 (ru) | 2013-10-30 |
| EA201170526A1 (ru) | 2011-10-31 |
| EP2350079B1 (en) | 2012-11-14 |
| CA2739422A1 (en) | 2010-04-08 |
| IL211292A (en) | 2013-06-27 |
| PL2350079T3 (pl) | 2013-03-29 |
| WO2010039678A1 (en) | 2010-04-08 |
| US20110166345A1 (en) | 2011-07-07 |
| AU2009298757B2 (en) | 2013-08-01 |
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