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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CN103842359A (zh
Inventor
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)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (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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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) KR20170055565A (enExample)
CN (2) CN103842359B (enExample)
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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
GEP20207128B (en) * 2016-04-06 2020-07-10 Molecules Gm Innovative Aminothiazole derivatives useful as antiviral agents
JP6978501B2 (ja) * 2016-11-28 2021-12-08 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］−アセトアミド遊離塩基半水和物、製造方法およびその用途
UY37498A (es) 2016-11-28 2018-06-29 Aicuris Anti Infective Cures Gmbh Una sal maleato de la base libre de n-[5-(aminosulfonil)-4-20 metil-1,3-tiazol-2-il]-n-metil-2-[4-(2-piridinil)-fenil]-acetamida, formulaciones farmacéuticas, métodos de fabricación y usos de la misma
WO2018095576A1 (en) * 2016-11-28 2018-05-31 Aicuris Anti-Infective Cures Gmbh Topical pharmaceutical formulation comprising n-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-n-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide
KR102335327B1 (ko) 2017-04-28 2021-12-03 현대자동차 주식회사 수냉식 이지알 쿨러
CN110831577B (zh) * 2017-06-28 2023-11-28 艾库里斯有限及两合公司 包含抗病毒化合物的阴道内施用型装置
KR102708082B1 (ko) 2017-10-05 2024-09-19 이노베이티브 몰리큘스 게엠베하 항바이러스 화합물로서 치환된 티아졸의 거울상 이성질체
US11964969B2 (en) 2018-07-06 2024-04-23 Phaeno Therapeutics Co., Ltd Crystal forms of thiazole compound and application thereof
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CA3168721A1 (en) * 2020-03-26 2021-09-30 Jessica Redmer 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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CA2791142C (en) 2017-08-01
AU2015260762A1 (en) 2016-02-04
EP2598501B1 (en) 2014-03-12
CL2014000149A1 (es) 2014-09-05
NZ718867A (en) 2016-05-27
PH12014500567A1 (en) 2014-04-14
JO3037B1 (ar) 2016-09-05
JO3734B1 (ar) 2021-01-31
KR101768295B1 (ko) 2017-08-14
ES2466221T8 (es) 2016-09-13
JP6161614B2 (ja) 2017-07-12
EP2602258B1 (en) 2014-03-19
CN105541829A (zh) 2016-05-04
ES2466221T3 (es) 2014-06-09
TWI532739B (zh) 2016-05-11
US20140221433A1 (en) 2014-08-07
UA119574C2 (uk) 2019-07-10
WO2013045479A1 (en) 2013-04-04
HK1220978A1 (zh) 2017-05-19
AU2012314536B2 (en) 2016-01-14
EP2573086A1 (en) 2013-03-27
UA115317C2 (uk) 2017-10-25
PE20141148A1 (es) 2014-09-15
PH12015502801A1 (en) 2016-10-03
CN103842359A (zh) 2014-06-04
MY185063A (en) 2021-04-30
RU2620604C2 (ru) 2017-05-29
EP2602258B8 (en) 2016-09-28
AR088043A1 (es) 2014-05-07
DK2602258T3 (da) 2014-04-22
MY190878A (en) 2022-05-13
BR112014003245A2 (pt) 2017-03-01
IL230152A (en) 2015-04-30
DK2598501T3 (da) 2014-04-22
PT2598501E (pt) 2014-06-25
RU2014107430A (ru) 2015-11-10
CA2791142A1 (en) 2013-03-26
ES2462492T3 (es) 2014-05-23
MX2014003389A (es) 2014-07-09
PH12015502801B1 (en) 2016-10-03
EP2602258A1 (en) 2013-06-12
KR20180088530A (ko) 2018-08-03
AR116394A2 (es) 2021-05-05
KR20170055565A (ko) 2017-05-19
AU2015260762B2 (en) 2016-06-09
PL2598501T3 (pl) 2014-08-29
TW201625603A (zh) 2016-07-16
AR120291A2 (es) 2022-02-09
AU2012314536A1 (en) 2014-02-06
KR20140066704A (ko) 2014-06-02
RU2669388C1 (ru) 2018-10-11
IL234405A (en) 2015-04-30
ZA201408734B (en) 2016-08-31
US9340535B2 (en) 2016-05-17
IN2014DN01993A (enExample) 2015-05-15
BR112014003245B1 (pt) 2021-11-09
NZ621615A (en) 2016-04-29
HRP20140351T1 (hr) 2014-07-04
JP2017114859A (ja) 2017-06-29
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MX371088B (es) 2020-01-16
TWI567070B (zh) 2017-01-21
KR20190104249A (ko) 2019-09-06
MX338736B (es) 2016-04-29
TW201317234A (zh) 2013-05-01
ZA201401773B (en) 2015-12-23
JP6353022B2 (ja) 2018-07-04
EP2598501A1 (en) 2013-06-05
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