HRP20210385T1 - Postupak proizvodnje derivata tiazola - Google Patents
Postupak proizvodnje derivata tiazola Download PDFInfo
- Publication number
- HRP20210385T1 HRP20210385T1 HRP20210385TT HRP20210385T HRP20210385T1 HR P20210385 T1 HRP20210385 T1 HR P20210385T1 HR P20210385T T HRP20210385T T HR P20210385TT HR P20210385 T HRP20210385 T HR P20210385T HR P20210385 T1 HRP20210385 T1 HR P20210385T1
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- Prior art keywords
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- 238000004519 manufacturing process Methods 0.000 title claims 10
- 150000007979 thiazole derivatives Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 9
- PFKFTWBEEFSNDU-UHFFFAOYSA-N 1,1'-Carbonyldiimidazole Substances C1=CN=CN1C(=O)N1C=CN=C1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- PAQZWJGSJMLPMG-UHFFFAOYSA-N 2,4,6-tripropyl-1,3,5,2$l^{5},4$l^{5},6$l^{5}-trioxatriphosphinane 2,4,6-trioxide Chemical compound CCCP1(=O)OP(=O)(CCC)OP(=O)(CCC)O1 PAQZWJGSJMLPMG-UHFFFAOYSA-N 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- -1 tetrahydropyranyloxy Chemical group 0.000 claims 2
- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide Substances CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 claims 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- FPQQSJJWHUJYPU-UHFFFAOYSA-N 3-(dimethylamino)propyliminomethylidene-ethylazanium;chloride Chemical compound Cl.CCN=C=NCCCN(C)C FPQQSJJWHUJYPU-UHFFFAOYSA-N 0.000 claims 1
- 125000004487 4-tetrahydropyranyl group Chemical group [H]C1([H])OC([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- QOSSAOTZNIDXMA-UHFFFAOYSA-N Dicylcohexylcarbodiimide Chemical compound C1CCCCC1N=C=NC1CCCCC1 QOSSAOTZNIDXMA-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 238000010306 acid treatment Methods 0.000 claims 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
Classifications
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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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
-
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Anesthesiology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Cephalosporin Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Claims (7)
1. Postupak proizvodnje spoja koji je predstavljen formulom (C), naznačen time, da obuhvaća (i) fazu reakcije spoja koji je predstavljen formulom (A) i spoja koji je predstavljen formulom (B):
[image]
pri čemu R1 predstavlja furil, R4, R5 i R6 su isti ili različiti i svaki od njih predstavlja niži alkil ili aril, R2 predstavlja piridil ili tetrahidropiranil, i
X1 predstavlja halogen.
2. Postupak proizvodnje prema patentnom zahtjevu 1, naznačen time, da nadalje obuhvaća proizvodnju spoja koji je predstavljen formulom (I):
[image]
pri čemu je svaki od R1 i R2 isti kao što je gore definirano, R3 predstavlja aril, aralkil, aromatsku heterocikličku skupinu, aromatski heterociklilalkil, alifatski heterociklilalkil ili tetrahidropiraniloksi, ili su te skupine supstituirane s jednim do tri supstituenta odabrana iz skupine koja se sastoji od sljedećih: halogen; niži alkil opcionalno supstituiran s nižim alkoksi ili morfolino; niži alkoksi; niži alkanoil; i vinil, pri čemu postupak proizvodnje nadalje obuhvaća (ii) fazu dobivanja spoja koji je predstavljen formulom (D) pomoću kiselinske obrade spoja koji je predstavljen formulom (C):
[image]
gdje je svaki od R1, R2, R4, R5 i R6 isti kao što je gore definirano, i (iii) fazu dobivanja spoja koji je predstavljen formulom (I) pomoću reakcije spoja koji je predstavljen formulom (D) i spoja koji je predstavljen formulom (E):
[image]
pri čemu Y predstavlja halogen ili hidroksi, i gdje je svaki od R1, R2 i R3 isti kao što je gore definirano.
3. Postupak proizvodnje prema patentnom zahtjevu 2, naznačen time, da se kod kiseline u fazi (ii) radi o klorovodičnoj kiselini ili trifluoroctenoj kiselini.
4. Postupak proizvodnje prema patentnom zahtjevu 2 ili 3, naznačen time, da Y je hidroksi.
5. Postupak proizvodnje prema patentnom zahtjevu 4, naznačen time, da se reakcija u fazi (iii) provodi u prisutnosti 1,3-dicikloheksilkarbodiimida, 1-etil-3-(3-dimetilaminopropil)karbodiimid-hidroklorida, 1,1'-karbonildiimidazola (CDI) ili propilfosfonskog anhidrida.
6. Postupak proizvodnje prema patentnom zahtjevu 4, naznačen time, da se reakcija u fazi (iii) provodi u prisutnosti CDI.
7. Postupak proizvodnje prema bilo kojem od patentnih zahtjeva 2 do 6, naznačen time, da R1 je 2-furil, R2 je 4-tetrahidropiranil, i R3 je 2-metilpiridin-5-il.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2015002964 | 2015-01-09 | ||
PCT/JP2016/051197 WO2016111381A1 (en) | 2015-01-09 | 2016-01-08 | Production method of thiazole derivative |
EP16735119.6A EP3242877B1 (en) | 2015-01-09 | 2016-01-08 | Production method of thiazole derivative |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20210385T1 true HRP20210385T1 (hr) | 2021-04-16 |
Family
ID=56356063
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20210385TT HRP20210385T1 (hr) | 2015-01-09 | 2021-03-04 | Postupak proizvodnje derivata tiazola |
Country Status (24)
Country | Link |
---|---|
US (3) | US10214523B2 (hr) |
EP (2) | EP3822269A1 (hr) |
JP (2) | JP6770962B2 (hr) |
CN (1) | CN107108602B (hr) |
AR (1) | AR103380A1 (hr) |
AU (1) | AU2016205657B2 (hr) |
BR (1) | BR112017014179A2 (hr) |
CA (2) | CA2972746C (hr) |
CL (1) | CL2017001695A1 (hr) |
CO (1) | CO2017006204A2 (hr) |
DK (1) | DK3242877T3 (hr) |
ES (1) | ES2861050T3 (hr) |
HR (1) | HRP20210385T1 (hr) |
HU (1) | HUE053567T2 (hr) |
IL (2) | IL252906B (hr) |
JO (2) | JOP20200093A1 (hr) |
MX (2) | MX2017009008A (hr) |
PL (1) | PL3242877T3 (hr) |
PT (1) | PT3242877T (hr) |
RS (1) | RS61570B1 (hr) |
RU (2) | RU2020141085A (hr) |
SI (1) | SI3242877T1 (hr) |
TW (2) | TWI729810B (hr) |
WO (1) | WO2016111381A1 (hr) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JOP20200093A1 (ar) * | 2015-01-09 | 2017-06-16 | Kyowa Kirin Co Ltd | طريقة لإنتاج مشتق ثيازول |
CN109293652B (zh) * | 2017-07-24 | 2021-10-22 | 四川科伦博泰生物医药股份有限公司 | 一种取代的噻唑衍生物及其用途 |
Family Cites Families (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SE445350B (sv) * | 1978-04-14 | 1986-06-16 | Roussel Uclaf | Oximderivat av 3-azidometyl-7-amino-tiazolyl-acetamido-cefalosporansyra och dess anvendning som antibiotika |
EA013249B1 (ru) * | 2003-12-26 | 2010-04-30 | Киова Хакко Кирин Ко., Лтд. | Производные тиазола |
ES2324922T3 (es) | 2004-07-27 | 2009-08-19 | Astellas Pharma Inc. | Derivados de tiazol que tienen actividad inhibidora de vap-1. |
US20100280023A1 (en) | 2005-06-23 | 2010-11-04 | Kyowa Hakko Kogyo Co., Ltd. | Thiazole derivatives |
WO2007015528A1 (ja) | 2005-08-02 | 2007-02-08 | Kyowa Hakko Kogyo Co., Ltd. | 睡眠障害の治療および/または予防剤 |
BRPI0615046C1 (pt) | 2005-08-22 | 2021-05-25 | Melior Discovery Inc | uso de um composto |
BRPI0615236A2 (pt) * | 2005-08-31 | 2011-05-10 | Astellas Pharma Inc | derivado de tiazol |
ZA200801857B (en) * | 2005-08-31 | 2009-07-29 | Astellas Pharma Inc | Thiazole derivative |
TWI473614B (zh) | 2008-05-29 | 2015-02-21 | Kyowa Hakko Kirin Co Ltd | Anti-analgesic inhibitors |
CN102105168A (zh) | 2008-07-23 | 2011-06-22 | 协和发酵麒麟株式会社 | 偏头痛治疗剂 |
TWI548411B (zh) | 2009-04-28 | 2016-09-11 | Kyowa Hakko Kirin Co Ltd | Exercise disorder treatment |
UA110097C2 (uk) | 2009-09-02 | 2015-11-25 | Терапевтичний агент для лікування розладів настрою | |
UA113383C2 (xx) | 2009-09-02 | 2017-01-25 | Терапевтичний агент для лікування тривожних розладів | |
WO2012027965A1 (en) * | 2010-09-01 | 2012-03-08 | Glaxo Group Limited | Novel compounds |
JP6266270B2 (ja) | 2013-05-20 | 2018-01-24 | セイコーインスツル株式会社 | 運動フォーム解析装置および運動フォーム解析方法 |
JOP20200093A1 (ar) | 2015-01-09 | 2017-06-16 | Kyowa Kirin Co Ltd | طريقة لإنتاج مشتق ثيازول |
-
2015
- 2015-01-09 JO JOP/2020/0093A patent/JOP20200093A1/ar unknown
-
2016
- 2016-01-07 JO JOP/2016/0004A patent/JO3546B1/ar active
- 2016-01-08 TW TW109116071A patent/TWI729810B/zh not_active IP Right Cessation
- 2016-01-08 JP JP2017535938A patent/JP6770962B2/ja not_active Expired - Fee Related
- 2016-01-08 MX MX2017009008A patent/MX2017009008A/es unknown
- 2016-01-08 RS RS20210278A patent/RS61570B1/sr unknown
- 2016-01-08 AU AU2016205657A patent/AU2016205657B2/en not_active Ceased
- 2016-01-08 CN CN201680005378.8A patent/CN107108602B/zh active Active
- 2016-01-08 EP EP20207877.0A patent/EP3822269A1/en not_active Withdrawn
- 2016-01-08 SI SI201631113T patent/SI3242877T1/sl unknown
- 2016-01-08 US US15/541,857 patent/US10214523B2/en active Active
- 2016-01-08 EP EP16735119.6A patent/EP3242877B1/en active Active
- 2016-01-08 AR ARP160100039A patent/AR103380A1/es unknown
- 2016-01-08 PT PT167351196T patent/PT3242877T/pt unknown
- 2016-01-08 ES ES16735119T patent/ES2861050T3/es active Active
- 2016-01-08 WO PCT/JP2016/051197 patent/WO2016111381A1/en active Application Filing
- 2016-01-08 RU RU2020141085A patent/RU2020141085A/ru unknown
- 2016-01-08 CA CA2972746A patent/CA2972746C/en active Active
- 2016-01-08 CA CA3080031A patent/CA3080031C/en active Active
- 2016-01-08 PL PL16735119T patent/PL3242877T3/pl unknown
- 2016-01-08 DK DK16735119.6T patent/DK3242877T3/da active
- 2016-01-08 BR BR112017014179-5A patent/BR112017014179A2/pt not_active IP Right Cessation
- 2016-01-08 RU RU2017128217A patent/RU2738937C2/ru active
- 2016-01-08 TW TW105100553A patent/TWI732748B/zh not_active IP Right Cessation
- 2016-01-08 HU HUE16735119A patent/HUE053567T2/hu unknown
-
2017
- 2017-06-14 IL IL252906A patent/IL252906B/en active IP Right Grant
- 2017-06-22 CO CONC2017/0006204A patent/CO2017006204A2/es unknown
- 2017-06-23 CL CL2017001695A patent/CL2017001695A1/es unknown
- 2017-07-07 MX MX2021000711A patent/MX2021000711A/es unknown
-
2019
- 2019-01-14 US US16/246,988 patent/US10618894B2/en not_active Expired - Fee Related
-
2020
- 2020-02-20 IL IL272811A patent/IL272811A/en unknown
- 2020-03-18 US US16/822,626 patent/US10894790B2/en active Active
- 2020-08-18 JP JP2020138297A patent/JP7068402B2/ja active Active
-
2021
- 2021-03-04 HR HRP20210385TT patent/HRP20210385T1/hr unknown
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