JP2018525393A - 化合物n−(3,5−ジメチルフェニル)−n’−(2−トリフルオロメチルフェニル)グアニジンの調製方法 - Google Patents
化合物n−(3,5−ジメチルフェニル)−n’−(2−トリフルオロメチルフェニル)グアニジンの調製方法 Download PDFInfo
- Publication number
- JP2018525393A JP2018525393A JP2018506997A JP2018506997A JP2018525393A JP 2018525393 A JP2018525393 A JP 2018525393A JP 2018506997 A JP2018506997 A JP 2018506997A JP 2018506997 A JP2018506997 A JP 2018506997A JP 2018525393 A JP2018525393 A JP 2018525393A
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound
- crystalline solid
- solid form
- dimethylphenyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
Links
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C277/00—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C277/02—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups of guanidine from cyanamide, calcium cyanamide or dicyandiamides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C277/00—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C277/08—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups of substituted guanidines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C277/00—Preparation of guanidine or its derivatives, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C277/06—Purification or separation of guanidine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
- C07C279/18—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to carbon atoms of six-membered aromatic rings
-
- 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)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Analytical Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
本願の明細書中で使用する全ての用語は、特に別段の記載がない限り、当該技術分野で知られているようなそれらの通常の意味で理解すべきである。本願で用いられる場合、ある用語についての他のより具体的な定義は、以下で記載するとおりであり、明確に別に記載された定義がより広い定義を提供するのでない限り、本明細書及び特許請求の範囲全体にわたって一貫して適用されることを意図する。
Claims (13)
- 式(II)の化合物と式(II)の化合物の塩との混合物を、式(III)のシアナミド化合物と反応させることによって実施する、請求項1に記載の方法。
- 前記式(II)の化合物の塩が、前記式(II)の化合物のクロルヒドレート(chlorhydrate)塩である、請求項1又は2に記載の方法。
- 前記極性有機溶媒が(C1〜C3)アルコールである、請求項1〜3のいずれか1項に記載の方法。
- 前記(C1〜C3)アルコールがエタノールである、請求項4に記載の方法。
- 前記反応を60℃〜75℃の温度で実施する、請求項1〜5のいずれか1項に記載の方法。
- 前記式(I)の化合物を結晶化する追加の工程を更に含む、請求項1〜6のいずれか1項に記載の方法。
- 前記結晶化を(C1〜C3)アルコール及び水の混合物の存在下で実施する、請求項7に記載の方法。
- 131.5℃の融点を示す、前記式(I)の化合物N−(3,5−ジメチルフェニル)−N’−(2−トリフルオロメチルフェニル)グアニジンの結晶性固体形態A。
- 132.4℃のDSCを示す、請求項9に記載の式(I)の結晶性固体形態A。
- 請求項9又は10に記載の前記式(I)の化合物N−(3,5−ジメチルフェニル)−N’−(2−トリフルオロメチルフェニル)グアニジンの前記結晶性固体形態の治療上有効な量を、1以上の薬剤的に許容される賦形剤又は担体と併せて含む、医薬組成物。
- 薬剤として使用するための、請求項9又は10で定義する式(I)の化合物N−(3,5−ジメチルフェニル)−N’−(2−トリフルオロメチルフェニル)グアニジンの結晶性固体形態A。
- Rho−GTPase細胞タンパク質が介在する病気の治療で使用するための、請求項9又は10で定義する式(I)の化合物N−(3,5−ジメチルフェニル)−N’−(2−トリフルオロメチルフェニル)グアニジンの結晶性固体形態A。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP15382424 | 2015-08-11 | ||
EP15382424.8 | 2015-08-11 | ||
ARP20150102582 | 2015-08-11 | ||
ARP150102582A AR101498A1 (es) | 2015-08-11 | 2015-08-11 | Procedimiento para la preparación del compuesto n-(3,5-dimetilfenil)-n-(2-trifluorometilfenil)guanidina y su forma cristalina a |
PCT/EP2016/069033 WO2017025560A1 (en) | 2015-08-11 | 2016-08-10 | A process for the preparation of the compound n-(3,5-dimethylphenyl)-n'-(2-trifluoromethylphenyl) guanidine |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2018525393A true JP2018525393A (ja) | 2018-09-06 |
JP2018525393A5 JP2018525393A5 (ja) | 2019-08-15 |
JP6748188B2 JP6748188B2 (ja) | 2020-08-26 |
Family
ID=56799434
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2018506997A Active JP6748188B2 (ja) | 2015-08-11 | 2016-08-10 | 化合物n−(3,5−ジメチルフェニル)−n’−(2−トリフルオロメチルフェニル)グアニジンの調製方法 |
Country Status (21)
Country | Link |
---|---|
US (1) | US10343984B2 (ja) |
EP (1) | EP3334707B1 (ja) |
JP (1) | JP6748188B2 (ja) |
CN (1) | CN107922322B (ja) |
AR (1) | AR101498A1 (ja) |
BR (1) | BR112018002614B1 (ja) |
CA (1) | CA2994781A1 (ja) |
CY (1) | CY1122481T1 (ja) |
DK (1) | DK3334707T3 (ja) |
ES (1) | ES2756580T3 (ja) |
HK (1) | HK1256253A1 (ja) |
HR (1) | HRP20192301T1 (ja) |
HU (1) | HUE046959T2 (ja) |
LT (1) | LT3334707T (ja) |
MX (1) | MX2018001548A (ja) |
PL (1) | PL3334707T3 (ja) |
PT (1) | PT3334707T (ja) |
RS (1) | RS59759B1 (ja) |
RU (1) | RU2737430C2 (ja) |
SI (1) | SI3334707T1 (ja) |
WO (1) | WO2017025560A1 (ja) |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2014530813A (ja) * | 2011-10-11 | 2014-11-20 | ウニベルシダッド ナシオナル デ キルメス | フェニル−グアニジン誘導体 |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IN172842B (ja) * | 1990-05-17 | 1993-12-11 | Boots Pharmaceuticals Limited | |
WO1997045111A1 (en) * | 1996-05-24 | 1997-12-04 | Neurosearch A/S | Phenyl derivatives useful as blockers of chloride channels |
US8283370B2 (en) * | 2008-10-03 | 2012-10-09 | The United States Of America As Represented By The Secretary Of The Army | Imidazolidinedione derivatives as antimalarial agents, preparation thereof, and methods of use |
-
2015
- 2015-08-11 AR ARP150102582A patent/AR101498A1/es unknown
-
2016
- 2016-08-10 LT LTEP16756641.3T patent/LT3334707T/lt unknown
- 2016-08-10 RU RU2018107840A patent/RU2737430C2/ru active
- 2016-08-10 PL PL16756641T patent/PL3334707T3/pl unknown
- 2016-08-10 MX MX2018001548A patent/MX2018001548A/es unknown
- 2016-08-10 CA CA2994781A patent/CA2994781A1/en active Pending
- 2016-08-10 DK DK16756641.3T patent/DK3334707T3/da active
- 2016-08-10 WO PCT/EP2016/069033 patent/WO2017025560A1/en active Application Filing
- 2016-08-10 BR BR112018002614-0A patent/BR112018002614B1/pt active IP Right Grant
- 2016-08-10 CN CN201680045772.4A patent/CN107922322B/zh active Active
- 2016-08-10 EP EP16756641.3A patent/EP3334707B1/en active Active
- 2016-08-10 HU HUE16756641A patent/HUE046959T2/hu unknown
- 2016-08-10 JP JP2018506997A patent/JP6748188B2/ja active Active
- 2016-08-10 RS RS20191669A patent/RS59759B1/sr unknown
- 2016-08-10 PT PT167566413T patent/PT3334707T/pt unknown
- 2016-08-10 SI SI201630561T patent/SI3334707T1/sl unknown
- 2016-08-10 US US15/751,437 patent/US10343984B2/en active Active
- 2016-08-10 ES ES16756641T patent/ES2756580T3/es active Active
-
2018
- 2018-11-29 HK HK18115310.1A patent/HK1256253A1/zh unknown
-
2019
- 2019-12-20 HR HRP20192301TT patent/HRP20192301T1/hr unknown
- 2019-12-27 CY CY20191101359T patent/CY1122481T1/el unknown
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2014530813A (ja) * | 2011-10-11 | 2014-11-20 | ウニベルシダッド ナシオナル デ キルメス | フェニル−グアニジン誘導体 |
Non-Patent Citations (3)
Title |
---|
STEPHEN BYRN ET AL: "Pharmaceutical Solids: A Strategic Approach to Regulatory Considerations", PHARMACEUTICAL RESEARCH, vol. 12, no. 7, JPN6014008492, July 1995 (1995-07-01), pages 945 - 954, XP055531015, ISSN: 0004237424, DOI: 10.1023/A:1016241927429 * |
塩路雄作, 固形製剤の製造技術, vol. 普及版, JPN6011023134, 27 January 2003 (2003-01-27), pages 9 - 12, ISSN: 0004237423 * |
浅原 照三, 溶剤ハンドブック, JPN6011026738, 1985, pages 47 - 51, ISSN: 0004237425 * |
Also Published As
Publication number | Publication date |
---|---|
CA2994781A1 (en) | 2017-02-16 |
CN107922322B (zh) | 2023-11-03 |
PL3334707T3 (pl) | 2020-05-18 |
PT3334707T (pt) | 2020-01-14 |
DK3334707T3 (da) | 2020-01-06 |
SI3334707T1 (sl) | 2020-03-31 |
ES2756580T3 (es) | 2020-04-27 |
EP3334707A1 (en) | 2018-06-20 |
AR101498A1 (es) | 2016-12-21 |
BR112018002614A2 (ja) | 2018-10-02 |
CN107922322A (zh) | 2018-04-17 |
RU2018107840A (ru) | 2019-09-12 |
RS59759B1 (sr) | 2020-02-28 |
LT3334707T (lt) | 2020-01-27 |
HRP20192301T1 (hr) | 2020-03-20 |
BR112018002614B1 (pt) | 2023-04-11 |
WO2017025560A1 (en) | 2017-02-16 |
MX2018001548A (es) | 2018-06-22 |
EP3334707B1 (en) | 2019-10-09 |
HK1256253A1 (zh) | 2019-09-20 |
HUE046959T2 (hu) | 2020-04-28 |
JP6748188B2 (ja) | 2020-08-26 |
RU2737430C2 (ru) | 2020-11-30 |
CY1122481T1 (el) | 2021-01-27 |
US20180244608A1 (en) | 2018-08-30 |
US10343984B2 (en) | 2019-07-09 |
RU2018107840A3 (ja) | 2019-12-18 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP7032583B2 (ja) | アルギナーゼ活性を阻害する組成物及び方法 | |
JP7018949B2 (ja) | アルギナーゼ活性を阻害するための組成物及び方法 | |
ES2960953T3 (es) | Forma de sal de clorhidrato para la inhibición de EZH2 | |
EA037521B1 (ru) | Противогрибковые соединения и способы их получения | |
TWI597282B (zh) | 6,7-不飽合-7-胺甲醯基嗎啡喃衍生物之結晶及其製造方法 | |
BR112020007826A2 (pt) | derivado de 4-benzopiranona, composição farmacêutica, composição alimentar funcional, método para tratamento de doenças relacionadas ao tnf, composição de reagente, método para inibir uma atividade de tnf | |
JP7025555B2 (ja) | 一過性受容体電位a1イオンチャネルの阻害 | |
JP6657294B2 (ja) | ニューロトロフィン模倣化合物およびこれらの塩の結晶形態 | |
CN106478502B (zh) | 1,2,3,4-四氢异喹啉衍生物、其制备方法和应用 | |
ES2766324T3 (es) | Formas salinas de Alfa-TEA: composiciones y usos para tratar enfermedades | |
JP2023157909A (ja) | 2-(5-(4-(2-モルホリノエトキシ)フェニル)ピリジン-2-イル)-n-ベンジルアセトアミドの固体形態 | |
TWI772424B (zh) | 一種苯并呋喃類衍生物游離鹼的晶型及製備方法 | |
JP2022106788A (ja) | 脂質化ペプチドの水溶性塩、その製造方法および用途 | |
KR20180111797A (ko) | 퀴놀론 유사체의 결정형 및 그것의 염 | |
JP6178799B2 (ja) | アプレピタントl−プロリン溶媒和化合物−組成物及び共結晶 | |
JP6748188B2 (ja) | 化合物n−(3,5−ジメチルフェニル)−n’−(2−トリフルオロメチルフェニル)グアニジンの調製方法 | |
TW201922690A (zh) | 環-amp反應元素結合蛋白的抑制劑 | |
JP2020521774A (ja) | 5−ブロモ−2,6−ジ(1h−ピラゾール−1−イル)ピリミジン−4−アミン及び新たな塩の結晶形 | |
CN117203208A (zh) | 靶向活化与失活态kras g12d的抑制剂 | |
JP6317358B2 (ja) | L‐リジンを含む(3s,3s’)4,4’‐ジスルファンジイルビス(3‐アミノブタン1‐スルホン酸)の新規結晶相 | |
RU2802964C2 (ru) | Твердые формы 2-(5-(4-(2-морфолиноэтокси)фенил)пиридин-2-ил)-n-бензилацетамида | |
JP7496440B2 (ja) | Trka阻害剤 | |
WO2014182673A1 (en) | Modulators of the g protein-coupled mas receptor and the treatment of disorders related thereto | |
WO2023114861A1 (en) | Conjugates, their compositions, and their related methods | |
JP2020143085A (ja) | サクビトリルカルシウム塩 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20190703 |
|
A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20190703 |
|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20200325 |
|
A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20200319 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20200624 |
|
TRDD | Decision of grant or rejection written | ||
A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20200714 |
|
A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20200806 |
|
R150 | Certificate of patent or registration of utility model |
Ref document number: 6748188 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |