DK2922551T3 - Hidtil ukendte fobindelser som diacylglycerolacyltransferase-inhibitorer - Google Patents
Hidtil ukendte fobindelser som diacylglycerolacyltransferase-inhibitorer Download PDFInfo
- Publication number
- DK2922551T3 DK2922551T3 DK13856479.4T DK13856479T DK2922551T3 DK 2922551 T3 DK2922551 T3 DK 2922551T3 DK 13856479 T DK13856479 T DK 13856479T DK 2922551 T3 DK2922551 T3 DK 2922551T3
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- DK
- Denmark
- Prior art keywords
- amino
- indol
- dihydropyrimido
- mmol
- oxazepin
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Virology (AREA)
- Endocrinology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Epidemiology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (13)
1. Forbindelse som er: 4-amino-6-(l-(oxetan-3-yl)-lF/-indol-5-yl)-7,8-dihydropyrimido[5,4- f][l,4]oxazepin-5(6F/)-on; 4-amino-6-(l-(3-(trifluormethoxy)phenyl)-lF/-indol-5-yl)-7,8- dihydropyrimido[5,4-f][l/4]oxazepin-5(6F/)-on; 4-amino-6-(l-cyclobutyl-lF/-pyrrolo[2,3-b]pyridin-5-yl)-7,8- dihydropyrimido[5,4-f][l/4]oxazepin-5(6F/)-on; 4-amino-6-(l-(2-hydroxy-2-methylpropyl)-lF/-indol-5-yl)-7,8- dihydropyrimido[5,4-f][l/4]oxazepin-5(6F/)-on; 4-amino-6-(l-(2-(trifluormethoxy)phenyl)-lF/-indol-5-yl)-7,8- dihydropyrimido[5,4-f][l/4]oxazepin-5(6F/)-on; 4-amino-6-(l-(2-methoxy-4-(trifluormethyl)phenyl)-lF/-indol-5-yl)-7,8- dihydropyrimido[5,4-f][l/4]oxazepin-5(6F/)-on; 4-amino-6-(l-(3-(difluormethoxy)phenyl)-lF/-indol-5-yl)-7,8- dihydropyrimido[5,4-f][l/4]oxazepin-5(6F/)-on; 4-amino-6-(l-(3-isobutoxyphenyl)-lF/-indol-5-yl)-7,8-dihydropyrimido[5,4- f][l,4]oxazepin-5(6F/)-on; 4-amino-6-(l-(2- isopropoxyphenyl)-lF/-indol-5-yl)-7,8-dihydropyrimido[5,4-f][l/4]oxazepin-5(6F/)-on; 4-amino-6-(l-(3,5-dichlorphenyl)-lF/-indol-5-yl)-7,8-dihydropyrimido[5,4-f][l,4]oxazepin-5(6F/)-on; 4-amino-6-(l-(3,5-dichlorphenyl)-lF/-pyrrolo[2,3-b]pyridin-5-yl)-7,8- dihydropyrimido[5,4-f][l/4]oxazepin-5(6F/)-on; 4-amino-6-(l-(2,3-dichlorphenyl)-lF/-indol-5-yl)-7,8-dihydropyrimido[5,4- f][l,4]oxazepin-5(6F/)-on; 4-amino-6-(l-(2-methylpyrimidin-5-yl)-lF/-indol-5-yl)-7,8- dihydropyrimido[5,4-f][l/4]oxazepin-5(6F/)-on; 4-amino-6-(l-(6-methylpyridin-3-yl)-lF/-pyrrolo[2,3-b]pyridin-5-yl)-7,8- dihydropyrimido[5,4-f][l/4]oxazepin-5(6F/)-on; 4-amino-6-(l-(l-methyl-6-oxo-l,6-dihydropyridin-3-yl)-lF/-indol-5-yl)- 7,8-dihydropyrimido[5,4-n[l/4]oxazepin-5(6A7)-on; 4-amino-6-(l-(2-hydroxyphenyl)-l/7-indol-5-yl)-7,8-dihyd ropyrimido[5,4-f][l,4]oxazepin-5(6H)-on; 4-amino-6-(l-(2-(cyclopentyloxy)phenyl)-lH-indol-5-yl)-7,8- dihydropyrimido[5,4-n[l/4]oxazepin-5(6A7)-on; 4-amino-6-(l-(2-hydroxyphenyl)-l/7-pyrrolo[2,3-b]pyridin-5-yl)-7,8- dihydropyrimido[5,4-n[l/4]oxazepin-5(6A7)-on; 4-amino-6-(l-(2-(cyclopentyloxy)phenyl)-l/7-pyrrolo[2,3-b]pyridin-5-yl)- 7,8-dihydropyrimido[5,4-n[l/4]oxazepin-5(6A7)-on; 4-amino-6-(l-(2-ethoxyphenyl)-l/7-indol-5-yl)-7,8-dihydropyrimido[5,4- f][l,4]oxazepin-5(6H)-on; 4-amino-6-(l-(5-methyl-l,3,4-oxadiazol-2-yl)-lH-indol-5-yl)-7,8- dihydropyrimido[5,4-n[l/4]oxazepin-5(6A7)-on; 4-amino-6-(7-cyclopropyl-l-propyl-l/7-indol-5-yl)-7,8- dihydropyrimido[5,4-n[l/4]oxazepin-5(6A7)-on; /V-(5-(4-amino-5-oxo-7,8-dihydrOpyrimido[5,4-n[l/4]oxazepin-6(5A/)-yl)- l-(2-methoxyphenyl)-l/7-indol-7-yl)cyclopropancarboxamid; 4-amino-6-(l-isopropyl-7-morpholino-l/7-indol-5-yl)-7,8- dihydropyrimido[5,4-n[l/4]oxazepin-5(6A7)-on; eller /V-(5-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-n[l/4]oxazepin-6(5A/)-yl)- l-isopropyl-lH-indol-7-yl)cyclopropancarboxamid; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1 som er 4-amino-6-(l-(2-hydroxy-2-methylpropyl)-l/7-indol-5-yl)-7,8-dihydropyrimido[5,4_r][l/4]oxazepin-5(6F/)-on; eller et farmaceutisk acceptabelt salt deraf.
3. Forbindelse ifølge krav 1 som er 4-amino-6-(l-(2-hydroxyphenyl)-lF/-indol-5-yl)-7,8-dihydropyrimido[5,4-n[l/4]oxazepin-5(6A7)-on; eller et farmaceutisk acceptabelt salt deraf.
4. Forbindelse ifølge krav 1 som er 4-amino-6-(7-cyclopropyl-l-propyl-lF/-indol-5-yl)-7,8-dihydropyrimido[5,4-n[l/4]oxazepin-5(6A7)-on; eller et farmaceutisk acceptabelt salt deraf.
5. Den frie base af forbindelsen ifølge krav 2.
6. Den frie base af forbindelsen ifølge krav 3.
7. Den frie base af forbindelsen ifølge krav 4.
8. Farmaceutisk sammensætning omfattende forbindelsen eller det farmaceutisk acceptable salt ifølge et hvilket som helst af kravene 1-7 og en farmaceutisk acceptabel excipiens.
9. Farmaceutisk sammensætning ifølge krav 8, tilpasset topisk anvendelse.
10. Forbindelse eller farmaceutisk acceptabelt salt ifølge et hvilket som helst af kravene 1-7 til anvendelse i terapi.
11. Forbindelse eller farmaceutisk acceptabelt salt ifølge et hvilket som helst af kravene 1-7 til anvendelse til behandling af fedme.
12. Forbindelse eller farmaceutisk acceptabelt salt ifølge et hvilket som helst af kravene 1-7 til anvendelse til behandling af akne.
13. Forbindelse eller farmaceutisk acceptabelt salt ifølge et hvilket som helst af kravene 1-7 til anvendelse til behandling af ikke-alkoholisk steatohepatitis.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN3593DE2012 | 2012-11-23 | ||
IN750DE2013 | 2013-03-14 | ||
IN3172DE2013 | 2013-10-25 | ||
PCT/US2013/071376 WO2014081994A1 (en) | 2012-11-23 | 2013-11-22 | Novel compounds as diacylglycerol acyltransferase inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2922551T3 true DK2922551T3 (da) | 2019-02-18 |
Family
ID=50776577
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK13856479.4T DK2922551T3 (da) | 2012-11-23 | 2013-11-22 | Hidtil ukendte fobindelser som diacylglycerolacyltransferase-inhibitorer |
Country Status (31)
Country | Link |
---|---|
US (1) | US20150322082A1 (da) |
EP (2) | EP3492474B1 (da) |
JP (1) | JP6279600B2 (da) |
KR (1) | KR102176463B1 (da) |
CN (1) | CN104918620B (da) |
AU (1) | AU2013347843B2 (da) |
BR (1) | BR112015011982A8 (da) |
CA (1) | CA2892304C (da) |
CL (1) | CL2015001397A1 (da) |
CY (1) | CY1121426T1 (da) |
DK (1) | DK2922551T3 (da) |
EA (1) | EA031114B1 (da) |
ES (1) | ES2708626T3 (da) |
HK (1) | HK1214757A1 (da) |
HR (1) | HRP20190099T1 (da) |
HU (1) | HUE042483T2 (da) |
IL (1) | IL238835B (da) |
LT (1) | LT2922551T (da) |
ME (1) | ME03315B (da) |
MX (1) | MX363484B (da) |
NZ (1) | NZ630436A (da) |
PE (1) | PE20150967A1 (da) |
PH (1) | PH12015501109B1 (da) |
PL (1) | PL2922551T3 (da) |
PT (1) | PT2922551T (da) |
RS (1) | RS58539B1 (da) |
SG (1) | SG11201503761WA (da) |
SI (1) | SI2922551T1 (da) |
UA (1) | UA115079C2 (da) |
WO (1) | WO2014081994A1 (da) |
ZA (1) | ZA201503304B (da) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2018052818A (ja) * | 2015-01-28 | 2018-04-05 | 武田薬品工業株式会社 | スルホンアミド化合物 |
RU2019117958A (ru) | 2016-11-18 | 2020-12-18 | Мерк Шарп И Доум Корп. | Производные индола, полезные в качестве ингибиторов диацилглицерид-о-ацилтрансферазы 2 |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR100795462B1 (ko) * | 2006-09-27 | 2008-01-16 | 한국생명공학연구원 | 인돌 유도체, 이의 제조방법 및 이를 유효성분으로함유하는 대사성 질환 예방 및 치료용 약학적 조성물 |
US20090036425A1 (en) | 2007-08-02 | 2009-02-05 | Pfizer Inc | Substituted bicyclolactam compounds |
US20090076275A1 (en) * | 2007-09-19 | 2009-03-19 | David Robert Bolin | Diacylglycerol acyltransferase inhibitors |
AR066169A1 (es) * | 2007-09-28 | 2009-07-29 | Novartis Ag | Derivados de benzo-imidazoles, utiles para trastornos asociados con la actividad de dgat |
US8324385B2 (en) * | 2008-10-30 | 2012-12-04 | Madrigal Pharmaceuticals, Inc. | Diacylglycerol acyltransferase inhibitors |
WO2010086820A1 (en) * | 2009-02-02 | 2010-08-05 | Pfizer Inc. | 4-amino-5-oxo-7, 8-dihydropyrimido [5,4-f] [1,4] oxazepin-6 (5h) -yl) phenyl derivatives, pharmaceutical compositions and uses thereof |
WO2011121350A1 (en) * | 2010-04-01 | 2011-10-06 | Astrazeneca Ab | 4 -amino -7,8- dihydropyrimido [5, 4 - f] [1, 4] oxazepin- 5 ( 6h) - one based dgat1 inhibitors |
CN103703009B (zh) | 2011-05-20 | 2016-08-17 | 葛兰素史密斯克莱知识产权(第2号)有限公司 | 作为二酰基甘油酰基转移酶抑制剂的新化合物 |
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2013
- 2013-11-22 NZ NZ630436A patent/NZ630436A/en not_active IP Right Cessation
- 2013-11-22 WO PCT/US2013/071376 patent/WO2014081994A1/en active Application Filing
- 2013-11-22 PE PE2015000657A patent/PE20150967A1/es unknown
- 2013-11-22 RS RS20190081A patent/RS58539B1/sr unknown
- 2013-11-22 HU HUE13856479A patent/HUE042483T2/hu unknown
- 2013-11-22 EA EA201590982A patent/EA031114B1/ru unknown
- 2013-11-22 EP EP18203369.6A patent/EP3492474B1/en active Active
- 2013-11-22 CA CA2892304A patent/CA2892304C/en not_active Expired - Fee Related
- 2013-11-22 MX MX2015006533A patent/MX363484B/es unknown
- 2013-11-22 CN CN201380069807.4A patent/CN104918620B/zh not_active Expired - Fee Related
- 2013-11-22 AU AU2013347843A patent/AU2013347843B2/en not_active Ceased
- 2013-11-22 SG SG11201503761WA patent/SG11201503761WA/en unknown
- 2013-11-22 EP EP13856479.4A patent/EP2922551B1/en active Active
- 2013-11-22 LT LTEP13856479.4T patent/LT2922551T/lt unknown
- 2013-11-22 PT PT13856479T patent/PT2922551T/pt unknown
- 2013-11-22 PL PL13856479T patent/PL2922551T3/pl unknown
- 2013-11-22 JP JP2015544141A patent/JP6279600B2/ja not_active Expired - Fee Related
- 2013-11-22 SI SI201331321T patent/SI2922551T1/sl unknown
- 2013-11-22 ES ES13856479T patent/ES2708626T3/es active Active
- 2013-11-22 ME MEP-2019-14A patent/ME03315B/me unknown
- 2013-11-22 DK DK13856479.4T patent/DK2922551T3/da active
- 2013-11-22 BR BR112015011982A patent/BR112015011982A8/pt active Search and Examination
- 2013-11-22 KR KR1020157016270A patent/KR102176463B1/ko active IP Right Grant
- 2013-11-22 US US14/646,403 patent/US20150322082A1/en not_active Abandoned
- 2013-11-22 UA UAA201506216A patent/UA115079C2/uk unknown
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2015
- 2015-05-12 ZA ZA2015/03304A patent/ZA201503304B/en unknown
- 2015-05-14 IL IL238835A patent/IL238835B/en active IP Right Grant
- 2015-05-19 PH PH12015501109A patent/PH12015501109B1/en unknown
- 2015-05-22 CL CL2015001397A patent/CL2015001397A1/es unknown
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2016
- 2016-03-09 HK HK16102704.5A patent/HK1214757A1/zh not_active IP Right Cessation
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2019
- 2019-01-16 HR HRP20190099TT patent/HRP20190099T1/hr unknown
- 2019-01-29 CY CY20191100120T patent/CY1121426T1/el unknown
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