HRP20210720T1 - Osnovni hemihidrat bez acetamida n-[5-(aminosulfonil)-4-metil-1,3-tiazol-2-il]-n-metil-2-[4-(2-piridinil)-fenil], postupci proizvodnje i njegove uporabe - Google Patents

Osnovni hemihidrat bez acetamida n-[5-(aminosulfonil)-4-metil-1,3-tiazol-2-il]-n-metil-2-[4-(2-piridinil)-fenil], postupci proizvodnje i njegove uporabe Download PDF

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HRP20210720T1
HRP20210720T1 HRP20210720TT HRP20210720T HRP20210720T1 HR P20210720 T1 HRP20210720 T1 HR P20210720T1 HR P20210720T T HRP20210720T T HR P20210720TT HR P20210720 T HRP20210720 T HR P20210720T HR P20210720 T1 HRP20210720 T1 HR P20210720T1
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Croatia
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methyl
phenyl
thiazol
pyridinyl
acetamide
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HRP20210720TT
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English (en)
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Yogeshwar BACHHAV
Wilfried Schwab
Alexander Birkmann
Kurt Voegtli
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Aicuris Gmbh & Co. Kg
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Application filed by Aicuris Gmbh & Co. Kg filed Critical Aicuris Gmbh & Co. Kg
Publication of HRP20210720T1 publication Critical patent/HRP20210720T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Biotechnology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (11)

1. Osnovni hemihidrat bez acetamida N-[5-(amino-sulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)fenil] s molekularnom formulom C18H18N4O3S2 x 0.5 H2O.
2. Osnovni hemihidrat bez acetamida N-[5-(amino-sulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)fenil] prema zahtjevu 1, koji sadrži vrhove XRPD na 5.9, 11.7, 15.5 i 18.7.
3. Farmaceutski pripravak koji sadrži osnovni hemihidrat bez acetamida N-[5-(amino-sulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)fenil] prema bilo kojem od prethodnih zahtjeva, naznačen time što navedeni pripravak nadalje sadrži najmanje jedan farmaceutski prihvatljiv ekscipijent.
4. Farmaceutski pripravak koji se može dobiti formuliranjem osnovnog hemihidrata bez acetamida N-[5-(amino-sulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)fenil] kako je definiran u bilo kojem od prethodnih zahtjeva 1 i 2 s najmanje jednim farmaceutski prihvatljivim ekscipijentom.
5. Farmaceutski pripravak kako je definiran u bilo kojem od zahtjeva 3 i 4, naznačen time što je osnovni hemihidrat bez acetamida N-[5-(amino-sulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)fenil] prisutan u količini od oko 0.1 do oko 10% m/m.
6. Osnovni hemihidrat bez acetamida N-[5-(amino-sulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)fenil] prema bilo kojem od zahtjeva 1 i 2 za uporabu kao lijek.
7. Osnovni hemihidrat bez acetamida N-[5-(amino-sulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)fenil] kako je definirano u bilo kojem od zahtjeva 1 i 2 za uporabu u liječenju i/ili prevenciji infekcija virusom herpes.
8. Osnovni hemihidrat bez acetamida N-[5-(amino-sulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)fenil] kako je definirano u bilo kojem od zahtjeva 1 i 2 za uporabu u liječenju i/ili prevenciji infekcija virusom herpes, pri čemu su navedeni virusi herpesa odabrani iz redova simplex virusa.
9. Osnovni hemihidrat bez acetamida N-[5-(amino-sulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)fenil] kako je definirano u bilo kojem od zahtjeva 1 i 2 za uporabu u liječenju i/ili prevenciji infekcije virusom herpes prema zahtjevu 8 odabran je iz skupine koja obuhvaća ponavljajući herpes labialis, herpes genitalis, herpes keratitis, herpes meningitis i/ili encefalitis, i herpes infekcije kod novorođenčeta.
10. Postupak za proizvodnju osnovnog hemihidrata bez acetamida N-[5-(amino-sulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)fenil] kao što je definirano u bilo kojem od zahtjeva 1 do 2, naznačen time što navedeni postupak sadrži sljedeće korake: a) Miješanje amida (4-piridin-2-il-fenil) -octene kiseline i aminotiazola sulfonske kiseline u N-metilpirolidonu (NMP); b) Hlađenje mješavine dobivene u koraku a); c) Dodavanje N-etil-N’-(3-dimetilaminopropil)-karbodiimid hidroklorida (EDC x HCl) u navedenu mješavinu dobivenu u koraku b); d) Miješanje otopine dobivene u koraku c) i dodavanje pročišćenoj H2O; e) Filtriranje otopine dobivene u koraku d); f) Pranje proizvoda u formi kolača dobivenog u koraku e); g) Sušenje proizvoda dobivenog u koraku f); h) Dodavanje H2O otopini dobivenoj u koraku g); i) Miješanje suspenzije dobivene u koraku h); j) Hlađenje suspenzije dobivene u koraku i); k) Miješanje suspenzije dobivene u koraku j); l) Izoliranje proizvoda filtracijom suspenzije dobivene u koraku k); m) Pranje proizvoda dobivenog u koraku l) s H2O; n) Sušenje proizvoda dobivenog u koraku m).
11. Farmaceutski pripravak koji sadrži osnovni hemihidrat bez acetamida N-[5-(amino-sulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)fenil] dobiven postupkom prema zahtjevu 10.
HRP20210720TT 2016-11-28 2021-05-07 Osnovni hemihidrat bez acetamida n-[5-(aminosulfonil)-4-metil-1,3-tiazol-2-il]-n-metil-2-[4-(2-piridinil)-fenil], postupci proizvodnje i njegove uporabe HRP20210720T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16200967 2016-11-28
EP17811883.2A EP3544976B1 (en) 2016-11-28 2017-11-28 N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide free base hemihydrate, methods of manufacture and uses thereof
PCT/EP2017/080653 WO2018096170A1 (en) 2016-11-28 2017-11-28 N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide free base hemihydrate, methods of manufacture and uses thereof

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HRP20210720T1 true HRP20210720T1 (hr) 2021-09-03

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HRP20210720TT HRP20210720T1 (hr) 2016-11-28 2021-05-07 Osnovni hemihidrat bez acetamida n-[5-(aminosulfonil)-4-metil-1,3-tiazol-2-il]-n-metil-2-[4-(2-piridinil)-fenil], postupci proizvodnje i njegove uporabe

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US (2) US11021474B2 (hr)
EP (3) EP4201934A1 (hr)
JP (2) JP6978501B2 (hr)
KR (2) KR102622289B1 (hr)
CN (2) CN109996798B (hr)
AR (1) AR110249A1 (hr)
AU (3) AU2017365632B2 (hr)
CA (1) CA3045059A1 (hr)
CY (1) CY1124523T1 (hr)
DK (2) DK3848369T3 (hr)
ES (2) ES2941390T3 (hr)
HR (1) HRP20210720T1 (hr)
HU (1) HUE054703T2 (hr)
LT (1) LT3544976T (hr)
PL (1) PL3544976T3 (hr)
PT (2) PT3544976T (hr)
RS (1) RS61905B1 (hr)
SI (2) SI3848369T1 (hr)
TW (2) TWI811800B (hr)
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2573085A1 (en) 2011-09-26 2013-03-27 AiCuris GmbH & Co. KG N-[5-(aminosulfonyl)-4methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl] acetamide mesylate monohydrate having a specific particle size distribution range and a specific surface area range
CN109996798B (zh) * 2016-11-28 2023-05-05 艾库里斯有限及两合公司 N-[5-(氨基磺酰基)-4-甲基-1,3-噻唑-2-基]-n-甲基-2-[4-(2-吡啶基)-苯基]-乙酰胺游离碱半水合物、其制造方法和用途
JP7316214B2 (ja) * 2016-11-28 2023-07-27 アイクリス ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト N-[5-(アミノスルホニル)-4-メチル-1,3-チアゾール-2-イル]-n-メチル-2-[4-(2-ピリジニル)-フェニル]-アセトアミドの遊離塩基形のマレイン酸塩、医薬製剤、製造方法およびヘルペスウイルスの処置のためのその使用
AR113344A1 (es) 2017-10-05 2020-04-22 Innovative Molecules Gmbh Enantiómeros de una serie de compuestos antivirales
TW202038947A (zh) 2018-11-28 2020-11-01 德商創新分子有限責任公司 在與溶瘤病毒之組合療法中治療癌症的解旋酶引子酶抑制劑
EP3925595A1 (en) * 2020-06-17 2021-12-22 AiCuris GmbH & Co. KG Ophthalmic formulation comprising n-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)phenyl] acetamide hemihydrate
EP4096632A1 (en) * 2020-03-26 2022-12-07 AiCuris GmbH & Co. KG Ophthalmic formulation comprising n-[5-(aminosulfonyl)-4-methyl-1,3- thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)phenyl]acetamide hemihydrate
WO2024047507A1 (en) 2022-08-29 2024-03-07 Assembly Biosciences, Inc. A novel crystalline form of pritelivir
WO2024047506A1 (en) 2022-08-29 2024-03-07 Assembly Biosciences, Inc. A novel crystalline form of pritelivir

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US5496820A (en) * 1988-10-20 1996-03-05 Peraelampi; Markku Ophthalmic use of S-timolol hemihydrate
DOP2000000109A (es) * 1999-12-23 2002-08-30 Gerald Kleymann Derivados de tiazolilamida
DE10129714A1 (de) 2001-06-22 2003-01-02 Bayer Ag Topische Anwendung von Thiazolylamiden
DE102005014248A1 (de) * 2005-03-30 2006-10-05 Aicuris Gmbh & Co. Kg Pharmazeutische Zubereitung von N-[5-(Aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamid
EP2573085A1 (en) * 2011-09-26 2013-03-27 AiCuris GmbH & Co. KG N-[5-(aminosulfonyl)-4methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl] acetamide mesylate monohydrate having a specific particle size distribution range and a specific surface area range
EP2573086A1 (en) * 2011-09-26 2013-03-27 AiCuris GmbH & Co. KG N-[5-(Aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate
CN109996798B (zh) 2016-11-28 2023-05-05 艾库里斯有限及两合公司 N-[5-(氨基磺酰基)-4-甲基-1,3-噻唑-2-基]-n-甲基-2-[4-(2-吡啶基)-苯基]-乙酰胺游离碱半水合物、其制造方法和用途
JP7316214B2 (ja) * 2016-11-28 2023-07-27 アイクリス ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト N-[5-(アミノスルホニル)-4-メチル-1,3-チアゾール-2-イル]-n-メチル-2-[4-(2-ピリジニル)-フェニル]-アセトアミドの遊離塩基形のマレイン酸塩、医薬製剤、製造方法およびヘルペスウイルスの処置のためのその使用
EP4096632A1 (en) * 2020-03-26 2022-12-07 AiCuris GmbH & Co. KG Ophthalmic formulation comprising n-[5-(aminosulfonyl)-4-methyl-1,3- thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)phenyl]acetamide hemihydrate

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CN109996798B (zh) 2023-05-05
JP6978501B2 (ja) 2021-12-08
TWI737861B (zh) 2021-09-01
CN109996798A (zh) 2019-07-09
SI3544976T1 (sl) 2021-08-31
AU2017365632B2 (en) 2021-07-15
US20200123145A1 (en) 2020-04-23
KR20190085115A (ko) 2019-07-17
TW201825483A (zh) 2018-07-16
SI3848369T1 (sl) 2023-07-31
EP3848369A1 (en) 2021-07-14
US20210269429A1 (en) 2021-09-02
EP4201934A1 (en) 2023-06-28
RS61905B1 (sr) 2021-06-30
JP2022024043A (ja) 2022-02-08
AR110249A1 (es) 2019-03-13
TWI811800B (zh) 2023-08-11
CN116804007A (zh) 2023-09-26
HUE054703T2 (hu) 2021-09-28
CY1124523T1 (el) 2022-07-22
PL3544976T3 (pl) 2021-11-02
AU2021221901A1 (en) 2021-09-23
TW202207924A (zh) 2022-03-01
KR102536156B1 (ko) 2023-05-25
ES2941390T3 (es) 2023-05-22
KR20230075524A (ko) 2023-05-31
CA3045059A1 (en) 2018-05-31
ES2870614T3 (es) 2021-10-27
EP3544976A1 (en) 2019-10-02
EP3544976B1 (en) 2021-02-17
LT3544976T (lt) 2021-08-10
KR102622289B1 (ko) 2024-01-05
WO2018096170A9 (en) 2019-12-19
JP7289891B2 (ja) 2023-06-12
JP2020509991A (ja) 2020-04-02
DK3544976T3 (da) 2021-05-10
DK3848369T3 (da) 2023-03-27
AU2017365632A1 (en) 2019-06-13
AU2021221901B2 (en) 2022-08-11
PT3848369T (pt) 2023-04-10
UY37496A (es) 2018-06-29
US11021474B2 (en) 2021-06-01
PT3544976T (pt) 2021-05-18
WO2018096170A1 (en) 2018-05-31
AU2022263540A1 (en) 2022-12-08
EP3848369B1 (en) 2023-01-11

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