CN103842359B - 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]乙酰胺甲磺酸盐一水合物 - Google Patents

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]乙酰胺甲磺酸盐一水合物 Download PDF

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Publication number
CN103842359B
CN103842359B CN201280046744.6A CN201280046744A CN103842359B CN 103842359 B CN103842359 B CN 103842359B CN 201280046744 A CN201280046744 A CN 201280046744A CN 103842359 B CN103842359 B CN 103842359B
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methyl
phenyl
thiazol
acetamide
aminosulfonyl
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Chinese (zh)
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CN103842359A (zh
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W·施瓦布
A·比克曼
K·弗格特利
D·哈格
A·伦德
A·格瓦嫩博格
B·凯尔
J·雷泽
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Aike 316 Co ltd
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Aicuris GmbH and Co KG
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    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/46—Acylated amino or imino radicals by carboxylic acids, or sulfur or nitrogen analogues thereof
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
CN201280046744.6A 2011-09-26 2012-09-26 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]乙酰胺甲磺酸盐一水合物 Active CN103842359B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201511005819.8A CN105541829A (zh) 2011-09-26 2012-09-26 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]乙酰胺甲磺酸盐一水合物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11007823.5 2011-09-26
EP11007823A EP2573086A1 (en) 2011-09-26 2011-09-26 N-[5-(Aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate
PCT/EP2012/068938 WO2013045479A1 (en) 2011-09-26 2012-09-26 N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate

Related Child Applications (1)

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CN201511005819.8A Division CN105541829A (zh) 2011-09-26 2012-09-26 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]乙酰胺甲磺酸盐一水合物

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CN103842359A CN103842359A (zh) 2014-06-04
CN103842359B true CN103842359B (zh) 2016-05-25

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CN201280046744.6A Active CN103842359B (zh) 2011-09-26 2012-09-26 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]乙酰胺甲磺酸盐一水合物
CN201511005819.8A Pending CN105541829A (zh) 2011-09-26 2012-09-26 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]乙酰胺甲磺酸盐一水合物

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US (1) US9340535B2 (enExample)
EP (3) EP2573086A1 (enExample)
JP (2) JP6161614B2 (enExample)
KR (4) KR20180088530A (enExample)
CN (2) CN103842359B (enExample)
AR (3) AR088043A1 (enExample)
AU (2) AU2012314536B2 (enExample)
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UA (2) UA115317C2 (enExample)
WO (1) WO2013045479A1 (enExample)
ZA (2) ZA201401773B (enExample)

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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
PH12018501979B1 (en) * 2016-04-06 2023-05-05 Innovative Molecules Gmbh Aminothiazole derivatives useful as antiviral agents
ES2877854T3 (es) 2016-11-28 2021-11-17 Aicuris Gmbh & Co Kg Una sal de maleato de la base libre de N-[5-(aminosulfonil)-4-metil-1,3-tiazol-2-il]-N-metil-2-[4-(2-piridinil)-fenil]-acetamida, formulaciones farmacéuticas, procedimientos de fabricación y usos de las mismas para el tratamiento de los virus del herpes
TWI811800B (zh) * 2016-11-28 2023-08-11 德商艾庫瑞斯公司 N-[5-(胺基磺醯基)-4-甲基-1,3-噻唑-2-基]-n-甲基-2-[4-(2-吡啶基)-苯基]-乙醯胺游離鹼半水合物、製造方法及其用途
TW201825095A (zh) * 2016-11-28 2018-07-16 德商艾庫里斯抗感染治療有限公司 包含n-[5-(胺基磺醯基)-4-甲基-1,3-噻唑-2-基]-n-甲基-2-[4-(2-吡啶基)-苯基]-乙醯胺之局部醫藥調配物
KR102335327B1 (ko) 2017-04-28 2021-12-03 현대자동차 주식회사 수냉식 이지알 쿨러
WO2019002486A1 (en) * 2017-06-28 2019-01-03 Aicuris Anti-Infective Cures Gmbh Intravaginally applicable devices comprising antiviral compounds
PL3692039T3 (pl) 2017-10-05 2023-04-17 Innovative Molecules Gmbh Enancjomery podstawionych tiazoli jako związki przeciwwirusowe
WO2020007355A1 (zh) * 2018-07-06 2020-01-09 南京明德新药研发有限公司 噻唑类化合物的晶型及其应用
CN112996854B (zh) * 2018-09-19 2024-08-30 摩登纳特斯有限公司 高纯度peg脂质和其用途
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
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
JP2025527942A (ja) 2022-08-29 2025-08-25 アセンブリー・バイオサイエンシーズ・インコーポレイテッド 新規な結晶形態
JP2025527943A (ja) 2022-08-29 2025-08-25 アセンブリー・バイオサイエンシーズ・インコーポレイテッド 新規な結晶形態
EP4580601A1 (en) 2022-08-29 2025-07-09 Assembly Biosciences, Inc. Pharmaceutical compositions for herpes virus

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WO2006103011A1 (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

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PH12015502801A1 (en) 2016-10-03
PT2598501E (pt) 2014-06-25
KR20140066704A (ko) 2014-06-02
EP2598501B1 (en) 2014-03-12
EP2598501A1 (en) 2013-06-05
ZA201408734B (en) 2016-08-31
ES2466221T3 (es) 2014-06-09
PH12015502801B1 (en) 2016-10-03
BR112014003245B1 (pt) 2021-11-09
HK1220978A1 (zh) 2017-05-19
MX338736B (es) 2016-04-29
IN2014DN01993A (enExample) 2015-05-15
TW201317234A (zh) 2013-05-01
DK2602258T3 (da) 2014-04-22
AR116394A2 (es) 2021-05-05
KR101768295B1 (ko) 2017-08-14
CN105541829A (zh) 2016-05-04
IL234405A (en) 2015-04-30
TW201625603A (zh) 2016-07-16
JP2014528948A (ja) 2014-10-30
JO3734B1 (ar) 2021-01-31
CA2791142C (en) 2017-08-01
AR088043A1 (es) 2014-05-07
CL2014000149A1 (es) 2014-09-05
SG10201407430TA (en) 2014-12-30
PL2602258T3 (pl) 2014-08-29
ZA201401773B (en) 2015-12-23
KR20180088530A (ko) 2018-08-03
RU2620604C2 (ru) 2017-05-29
CN103842359A (zh) 2014-06-04
JO3037B1 (ar) 2016-09-05
NZ621615A (en) 2016-04-29
PE20141148A1 (es) 2014-09-15
RU2669388C1 (ru) 2018-10-11
IL230152A (en) 2015-04-30
RU2014107430A (ru) 2015-11-10
EP2573086A1 (en) 2013-03-27
MX2014003389A (es) 2014-07-09
MY190878A (en) 2022-05-13
ES2462492T3 (es) 2014-05-23
PH12014500567A1 (en) 2014-04-14
NZ718867A (en) 2016-05-27
HRP20140351T1 (hr) 2014-07-04
KR20170055565A (ko) 2017-05-19
MY185063A (en) 2021-04-30
CA2791142A1 (en) 2013-03-26
ES2466221T8 (es) 2016-09-13
JP6161614B2 (ja) 2017-07-12
PL2598501T3 (pl) 2014-08-29
US9340535B2 (en) 2016-05-17
JP6353022B2 (ja) 2018-07-04
JP2017114859A (ja) 2017-06-29
UA115317C2 (uk) 2017-10-25
US20140221433A1 (en) 2014-08-07
TWI532739B (zh) 2016-05-11
AR120291A2 (es) 2022-02-09
AU2012314536A1 (en) 2014-02-06
EP2602258B1 (en) 2014-03-19
MX371088B (es) 2020-01-16
AU2015260762B2 (en) 2016-06-09
KR20190104249A (ko) 2019-09-06
AU2012314536B2 (en) 2016-01-14
UA119574C2 (uk) 2019-07-10
BR112014003245A2 (pt) 2017-03-01
TWI567070B (zh) 2017-01-21
AU2015260762A1 (en) 2016-02-04
DK2598501T3 (da) 2014-04-22
EP2602258A1 (en) 2013-06-12
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WO2013045479A1 (en) 2013-04-04

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