JO3734B1 - -n[5-(أمينوسلفونيل)-4- ميثيل-3،1- ثيازول-2- يل]-n- ميثيل-2-[4-(2- بيريدينيل) فنيل] أسيتاميد ميسيلات مونوهيدرات - Google Patents

-n[5-(أمينوسلفونيل)-4- ميثيل-3،1- ثيازول-2- يل]-n- ميثيل-2-[4-(2- بيريدينيل) فنيل] أسيتاميد ميسيلات مونوهيدرات

Info

Publication number
JO3734B1
JO3734B1 JOP/2016/0114A JOP20160114A JO3734B1 JO 3734 B1 JO3734 B1 JO 3734B1 JO P20160114 A JOP20160114 A JO P20160114A JO 3734 B1 JO3734 B1 JO 3734B1
Authority
JO
Jordan
Prior art keywords
methyl
aminosulfonyl
pyridinyl
phenyl
mesylate monohydrate
Prior art date
Application number
JOP/2016/0114A
Other languages
English (en)
Inventor
Grunenberg Alfons Dr
Birkmann Alexander Dr
Rehse Joachim Dr
Schwab Wilfried Dr
Haag Dieter Dr
Lender Andreas Dr
Birgit D -I Keil
Kurt V?Gtli
Original Assignee
Aicuris Gmbh & Co Kg
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Aicuris Gmbh & Co Kg filed Critical Aicuris Gmbh & Co Kg
Application granted granted Critical
Publication of JO3734B1 publication Critical patent/JO3734B1/ar

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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

Landscapes

  • 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)

Abstract

يتعلق الاختراع الحالي بتخليق محسن وقصير من N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide وملح mesylate monohydrate منه باستخدام مشتقات boronic acid أو عوامل كاشفة borolane بينما يتم تجنب مركبات tin عضوية سامة وبملح mesylate monohydrate من N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide الذي يظهر زيادة الثبات طويل الأجل وإطلاق حركيات من التركيبات الدوائية.
JOP/2016/0114A 2011-09-26 2016-06-07 -n[5-(أمينوسلفونيل)-4- ميثيل-3،1- ثيازول-2- يل]-n- ميثيل-2-[4-(2- بيريدينيل) فنيل] أسيتاميد ميسيلات مونوهيدرات JO3734B1 (ar)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
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

Publications (1)

Publication Number Publication Date
JO3734B1 true JO3734B1 (ar) 2021-01-31

Family

ID=46889067

Family Applications (2)

Application Number Title Priority Date Filing Date
JOP/2012/0276A JO3037B1 (ar) 2011-09-26 2012-09-23 N -[5-(أمينوسلفونيل)-4- ميثيل-3،1- ثيازول-2- يل]-n- ميثيل-2-[4-(2- بيريدينيل) فنيل] أسيتاميد ميسيلات مونوهيدرات
JOP/2016/0114A JO3734B1 (ar) 2011-09-26 2016-06-07 -n[5-(أمينوسلفونيل)-4- ميثيل-3،1- ثيازول-2- يل]-n- ميثيل-2-[4-(2- بيريدينيل) فنيل] أسيتاميد ميسيلات مونوهيدرات

Family Applications Before (1)

Application Number Title Priority Date Filing Date
JOP/2012/0276A JO3037B1 (ar) 2011-09-26 2012-09-23 N -[5-(أمينوسلفونيل)-4- ميثيل-3،1- ثيازول-2- يل]-n- ميثيل-2-[4-(2- بيريدينيل) فنيل] أسيتاميد ميسيلات مونوهيدرات

Country Status (29)

Country Link
US (1) US9340535B2 (ar)
EP (3) EP2573086A1 (ar)
JP (2) JP6161614B2 (ar)
KR (4) KR20170055565A (ar)
CN (2) CN103842359B (ar)
AR (3) AR088043A1 (ar)
AU (2) AU2012314536B2 (ar)
BR (1) BR112014003245B1 (ar)
CA (1) CA2791142C (ar)
CL (1) CL2014000149A1 (ar)
DK (2) DK2598501T3 (ar)
ES (2) ES2466221T3 (ar)
HK (1) HK1220978A1 (ar)
HR (1) HRP20140351T1 (ar)
IL (2) IL230152A (ar)
IN (1) IN2014DN01993A (ar)
JO (2) JO3037B1 (ar)
MX (2) MX371088B (ar)
MY (2) MY190878A (ar)
PE (1) PE20141148A1 (ar)
PH (2) PH12014500567A1 (ar)
PL (2) PL2602258T3 (ar)
PT (1) PT2598501E (ar)
RU (2) RU2620604C2 (ar)
SG (1) SG10201407430TA (ar)
TW (2) TWI567070B (ar)
UA (2) UA115317C2 (ar)
WO (1) WO2013045479A1 (ar)
ZA (2) ZA201401773B (ar)

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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
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
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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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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

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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
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
CN103842359B (zh) 2016-05-25
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 (ar) 2015-05-15
BR112014003245B1 (pt) 2021-11-09
NZ621615A (en) 2016-04-29
HRP20140351T1 (hr) 2014-07-04
JP2017114859A (ja) 2017-06-29
JP2014528948A (ja) 2014-10-30
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
PL2602258T3 (pl) 2014-08-29
SG10201407430TA (en) 2014-12-30

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