IN2014DN01993A - - Google Patents
Info
- Publication number
- IN2014DN01993A IN2014DN01993A IN1993DEN2014A IN2014DN01993A IN 2014DN01993 A IN2014DN01993 A IN 2014DN01993A IN 1993DEN2014 A IN1993DEN2014 A IN 1993DEN2014A IN 2014DN01993 A IN2014DN01993 A IN 2014DN01993A
- Authority
- IN
- India
- Prior art keywords
- methyl
- aminosulfonyl
- thiazol
- pyridinyl
- phenyl
- Prior art date
Links
- ZZLCFHIKESPLTH-UHFFFAOYSA-N 4-Methylbiphenyl Chemical compound C1=CC(C)=CC=C1C1=CC=CC=C1 ZZLCFHIKESPLTH-UHFFFAOYSA-N 0.000 abstract 2
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 2
- OIXMUQLVDNPHNS-UHFFFAOYSA-N methanesulfonic acid;hydrate Chemical compound O.CS(O)(=O)=O OIXMUQLVDNPHNS-UHFFFAOYSA-N 0.000 abstract 2
- FCVMHSMWASHTGN-UHFFFAOYSA-N n-methyl-2-(4-pyridin-2-ylphenyl)acetamide Chemical compound C1=CC(CC(=O)NC)=CC=C1C1=CC=CC=N1 FCVMHSMWASHTGN-UHFFFAOYSA-N 0.000 abstract 2
- 125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 abstract 2
- HBXRPXYBMZDIQL-UHFFFAOYSA-N 1$l^{2}-borolane Chemical compound [B]1CCCC1 HBXRPXYBMZDIQL-UHFFFAOYSA-N 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 150000001642 boronic acid derivatives Chemical class 0.000 abstract 1
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 230000007774 longterm Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 150000003606 tin compounds Chemical class 0.000 abstract 1
- 231100000331 toxic Toxicity 0.000 abstract 1
- 230000002588 toxic effect Effects 0.000 abstract 1
Classifications
-
- 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)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Biotechnology (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
The present invention relates to an improved and shortened synthesis of N [5 (aminosulfonyl) 4 methyl 1 3 thiazol 2 yl] N methyl 2 [4 (2 pyridinyl)phenyl]acet amide and the mesylate monohydrate salt thereof by using boronic acid derivatives or borolane reagents while avoiding toxic organic tin compounds and to the mesylate monohydrate salt of N [5 (aminosulfonyl) 4 methyl 1 3 thiazol 2 yl] N methyl 2 [4 (2 pyridinyl)phenyl]acet amide which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions.
Applications Claiming Priority (2)
| 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 |
| 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IN2014DN01993A true IN2014DN01993A (en) | 2015-05-15 |
Family
ID=46889067
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IN1993DEN2014 IN2014DN01993A (en) | 2011-09-26 | 2012-09-26 |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US9340535B2 (en) |
| EP (3) | EP2573086A1 (en) |
| JP (2) | JP6161614B2 (en) |
| KR (4) | KR20180088530A (en) |
| CN (2) | CN103842359B (en) |
| AR (3) | AR088043A1 (en) |
| AU (2) | AU2012314536B2 (en) |
| BR (1) | BR112014003245B1 (en) |
| CA (1) | CA2791142C (en) |
| CL (1) | CL2014000149A1 (en) |
| DK (2) | DK2602258T3 (en) |
| ES (2) | ES2462492T3 (en) |
| HK (1) | HK1220978A1 (en) |
| HR (1) | HRP20140351T1 (en) |
| IL (2) | IL230152A (en) |
| IN (1) | IN2014DN01993A (en) |
| JO (2) | JO3037B1 (en) |
| MX (2) | MX338736B (en) |
| MY (2) | MY190878A (en) |
| PE (1) | PE20141148A1 (en) |
| PH (2) | PH12014500567A1 (en) |
| PL (2) | PL2598501T3 (en) |
| PT (1) | PT2598501E (en) |
| RU (2) | RU2620604C2 (en) |
| SG (1) | SG10201407430TA (en) |
| TW (2) | TWI567070B (en) |
| UA (2) | UA119574C2 (en) |
| WO (1) | WO2013045479A1 (en) |
| ZA (2) | ZA201401773B (en) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| MX375099B (en) * | 2016-04-06 | 2025-03-06 | Innovative Molecules Gmbh | AMINOTHIAZOLE DERIVATIVES USEFUL AS ANTIVIRAL AGENTS. |
| UY37497A (en) * | 2016-11-28 | 2018-06-29 | Aicuris Anti Infective Cures Gmbh | TOPICAL FORMULATION INCLUDING N- [5- (AMINOSULFONIL) -4-METHYL-1,3-TIAZOL-2-IL] -N-METHYL-2- [4- (2-PYRIDINYL) -PHENYL] -ACETAMIDE |
| UY37496A (en) * | 2016-11-28 | 2018-06-29 | Aicuris Anti Infective Cures Gmbh | N- [5- (AMINOSULFONYL) -4-METHYL-1,3-TIAZOL-2-IL] -N-METHYL-2- [4- (2-PYRIDINYL) -PHENYL] -ACETAMIDE FREE BASE HEMIHYDRATE MANUFACTURING METHODS AND USES OF THE SAME |
| CN117186085A (en) | 2016-11-28 | 2023-12-08 | 艾库里斯有限及两合公司 | Prime Li Wei sulfate, pharmaceutical preparation, preparation method and application thereof in treatment of herpesvirus |
| KR102335327B1 (en) | 2017-04-28 | 2021-12-03 | 현대자동차 주식회사 | Water cooled egr cooler |
| US11213516B2 (en) * | 2017-06-28 | 2022-01-04 | Aicuris Gmbh & Co. Kg | Intravaginally applicable devices comprising antiviral compounds |
| LT3692039T (en) | 2017-10-05 | 2023-03-27 | Innovative Molecules Gmbh | ENANTIOMERES OF THIAZOLE AS ANTIVIRAL COMPOUNDS |
| US11964969B2 (en) | 2018-07-06 | 2024-04-23 | Phaeno Therapeutics Co., Ltd | Crystal forms of thiazole compound and application thereof |
| AU2019345067A1 (en) * | 2018-09-19 | 2021-04-08 | Modernatx, Inc. | High-purity peg lipids and uses thereof |
| TW202038947A (en) | 2018-11-28 | 2020-11-01 | 德商創新分子有限責任公司 | Helicase primase inhibitors for treating cancer in a combination therapy with oncolytic viruses |
| US20230124969A1 (en) * | 2020-03-26 | 2023-04-20 | 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 |
| CN119731171A (en) | 2022-08-29 | 2025-03-28 | 组装生物科学股份有限公司 | New crystalline forms of primi Li Wei |
| WO2024047506A1 (en) | 2022-08-29 | 2024-03-07 | Assembly Biosciences, Inc. | A novel crystalline form of pritelivir |
| IL319024A (en) | 2022-08-29 | 2025-04-01 | Assembly Biosciences Inc | Pharmaceutical compositions for herpes virus |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DOP2000000109A (en) | 1999-12-23 | 2002-08-30 | Gerald Kleymann | THIAZOLILAMIDE DERIVATIVES |
| DE10129714A1 (en) * | 2001-06-22 | 2003-01-02 | Bayer Ag | Topical application of thiazolylamides |
| DE10129717A1 (en) * | 2001-06-22 | 2003-01-02 | Bayer Ag | Combination preparation containing nucleoside compound and 5-sulfonyl-2-phenylacetamido-thiazole derivative, useful as antiviral agent effective againts herpes viruses, especially herpes simplex |
| DE10129716A1 (en) * | 2001-06-22 | 2003-01-02 | Bayer Ag | Combination preparation useful as antiviral agent effective against herpes viruses, especially herpes simplex, contains acetylsalicylic acid and 5-sulfonyl-2-phenylacetamido-thiazole derivative |
| DE10131128A1 (en) * | 2001-06-28 | 2003-01-16 | Bayer Ag | New 5-aminosulfonyl-2-phenylacetamido-thiazole derivatives, useful as antiviral medicaments effective against herpes viruses, especially herpes simplex |
| GB0423653D0 (en) * | 2004-10-25 | 2004-11-24 | Piramed Ltd | Pharmaceutical compounds |
| DE102005014248A1 (en) * | 2005-03-30 | 2006-10-05 | Aicuris Gmbh & Co. Kg | Pharmaceutical preparation of N- [5- (aminosulfonyl) -4-methyl-1,3-thiazol-2-yl] -N-methyl-2- [4- (2-pyridinyl) phenyl] acetamide |
| JP2007314516A (en) * | 2006-04-25 | 2007-12-06 | Daiichi Sankyo Co Ltd | Pharmaceutical containing benzene compound having two or more substituents |
| EA201200423A1 (en) * | 2006-06-09 | 2012-08-30 | Икос Корпорейшн | SUBSTITUTED PHENYLACETIC ACIDS AS DP-2 ANTAGONISTS |
| AR070127A1 (en) * | 2008-01-11 | 2010-03-17 | Novartis Ag | PIRROLO - PIRIMIDINAS AND PIRROLO -PIRIDINAS |
| UA103918C2 (en) * | 2009-03-02 | 2013-12-10 | Айерем Элелси | N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators |
| 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 |
-
2011
- 2011-09-26 EP EP11007823A patent/EP2573086A1/en not_active Withdrawn
-
2012
- 2012-09-21 TW TW105109173A patent/TWI567070B/en active
- 2012-09-21 TW TW101134784A patent/TWI532739B/en active
- 2012-09-23 JO JOP/2012/0276A patent/JO3037B1/en active
- 2012-09-26 CN CN201280046744.6A patent/CN103842359B/en active Active
- 2012-09-26 SG SG10201407430TA patent/SG10201407430TA/en unknown
- 2012-09-26 HR HRP20140351AT patent/HRP20140351T1/en unknown
- 2012-09-26 KR KR1020187021891A patent/KR20180088530A/en not_active Ceased
- 2012-09-26 JP JP2014532361A patent/JP6161614B2/en active Active
- 2012-09-26 CA CA2791142A patent/CA2791142C/en active Active
- 2012-09-26 UA UAA201704493A patent/UA119574C2/en unknown
- 2012-09-26 AR ARP120103551A patent/AR088043A1/en not_active Application Discontinuation
- 2012-09-26 KR KR1020197025387A patent/KR20190104249A/en not_active Ceased
- 2012-09-26 ES ES12762300.7T patent/ES2462492T3/en active Active
- 2012-09-26 UA UAA201404411A patent/UA115317C2/en unknown
- 2012-09-26 EP EP12762300.7A patent/EP2598501B1/en active Active
- 2012-09-26 PL PL12762300T patent/PL2598501T3/en unknown
- 2012-09-26 PL PL13157396T patent/PL2602258T3/en unknown
- 2012-09-26 RU RU2014107430A patent/RU2620604C2/en active
- 2012-09-26 MY MYPI2017702805A patent/MY190878A/en unknown
- 2012-09-26 DK DK13157396.6T patent/DK2602258T3/en active
- 2012-09-26 MY MYPI2014000656A patent/MY185063A/en unknown
- 2012-09-26 BR BR112014003245-9A patent/BR112014003245B1/en active IP Right Grant
- 2012-09-26 CN CN201511005819.8A patent/CN105541829A/en active Pending
- 2012-09-26 KR KR1020177012548A patent/KR20170055565A/en not_active Ceased
- 2012-09-26 KR KR1020147004026A patent/KR101768295B1/en active Active
- 2012-09-26 ES ES13157396.6T patent/ES2466221T3/en active Active
- 2012-09-26 IN IN1993DEN2014 patent/IN2014DN01993A/en unknown
- 2012-09-26 DK DK12762300.7T patent/DK2598501T3/en active
- 2012-09-26 AU AU2012314536A patent/AU2012314536B2/en active Active
- 2012-09-26 EP EP13157396.6A patent/EP2602258B8/en active Active
- 2012-09-26 RU RU2017114501A patent/RU2669388C1/en active
- 2012-09-26 WO PCT/EP2012/068938 patent/WO2013045479A1/en active Application Filing
- 2012-09-26 PH PH1/2014/500567A patent/PH12014500567A1/en unknown
- 2012-09-26 MX MX2014003389A patent/MX338736B/en active IP Right Grant
- 2012-09-26 MX MX2015016192A patent/MX371088B/en unknown
- 2012-09-26 PE PE2014000390A patent/PE20141148A1/en active IP Right Grant
- 2012-09-26 US US14/347,287 patent/US9340535B2/en active Active
- 2012-09-26 PT PT127623007T patent/PT2598501E/en unknown
-
2013
- 2013-12-24 IL IL230152A patent/IL230152A/en active IP Right Grant
-
2014
- 2014-01-20 CL CL2014000149A patent/CL2014000149A1/en unknown
- 2014-03-11 ZA ZA2014/01773A patent/ZA201401773B/en unknown
- 2014-09-01 IL IL234405A patent/IL234405A/en active IP Right Grant
- 2014-09-02 HK HK16109165.2A patent/HK1220978A1/en unknown
- 2014-11-27 ZA ZA2014/08734A patent/ZA201408734B/en unknown
-
2015
- 2015-11-24 AU AU2015260762A patent/AU2015260762B2/en active Active
- 2015-12-16 PH PH12015502801A patent/PH12015502801A1/en unknown
-
2016
- 2016-06-07 JO JOP/2016/0114A patent/JO3734B1/en active
- 2016-12-22 JP JP2016249351A patent/JP6353022B2/en active Active
-
2019
- 2019-09-13 AR ARP190102595A patent/AR116394A2/en not_active Application Discontinuation
-
2020
- 2020-10-23 AR ARP200102938A patent/AR120291A2/en unknown
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