HUP0401665A1 - Egy aminotiazolil-acetanilid-származék alfa- és béta-kristályalakja, alkalmazásuk és az ezeket tartalmazó gyógyszerkészítmények - Google Patents
Egy aminotiazolil-acetanilid-származék alfa- és béta-kristályalakja, alkalmazásuk és az ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0401665A1 HUP0401665A1 HU0401665A HUP0401665A HUP0401665A1 HU P0401665 A1 HUP0401665 A1 HU P0401665A1 HU 0401665 A HU0401665 A HU 0401665A HU P0401665 A HUP0401665 A HU P0401665A HU P0401665 A1 HUP0401665 A1 HU P0401665A1
- Authority
- HU
- Hungary
- Prior art keywords
- aminothiazolyl
- alfa
- beta
- pharmaceutical compositions
- compositions containing
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title abstract 5
- FJZCVRBXEZZTBP-UHFFFAOYSA-N 2-amino-n-phenyl-2-(1,3-thiazol-2-yl)acetamide Chemical class N=1C=CSC=1C(N)C(=O)NC1=CC=CC=C1 FJZCVRBXEZZTBP-UHFFFAOYSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000003814 drug Substances 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 239000004480 active ingredient Substances 0.000 abstract 1
- 230000003178 anti-diabetic effect Effects 0.000 abstract 1
- 239000003472 antidiabetic agent Substances 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 238000009776 industrial production Methods 0.000 abstract 1
- PBAPPPCECJKMCM-IBGZPJMESA-N mirabegron Chemical compound S1C(N)=NC(CC(=O)NC=2C=CC(CCNC[C@H](O)C=3C=CC=CC=3)=CC=2)=C1 PBAPPPCECJKMCM-IBGZPJMESA-N 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- 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
- C07D277/40—Unsubstituted amino or imino radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Hematology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Obesity (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Steroid Compounds (AREA)
Abstract
%-5> A találmány tárgyát képezi az (R)-2-(2-amino-tiazol-4-il)-4'-[2-[(2-hidroxi-2-fenil-etil)-amino]-etil]-acetanilid a- és b-kristályalakja, és hatóanyagként való alkalmazásuk diabétesz ellenigyógyszer előállítására. Az a-kristályalak nem mutat higroszkóposságotés stabil, így alkalmazható gyógyszerként és felhasználható az iparitermelés tömegszintézisére. A b-kristályalak viszonylag kishigroszkóposságot mutat és szintén felhasználható az a-kristályalakelőállítási intermediereként. Ó
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2001-332914 | 2001-10-30 | ||
JP2001332914 | 2001-10-30 | ||
PCT/JP2002/011217 WO2003037881A1 (fr) | 2001-10-30 | 2002-10-29 | Cristal a forme $g(a) ou $g(b) d'un derive acetanilinide |
Publications (3)
Publication Number | Publication Date |
---|---|
HUP0401665A1 true HUP0401665A1 (hu) | 2004-11-29 |
HUP0401665A3 HUP0401665A3 (en) | 2008-05-28 |
HU230481B1 HU230481B1 (hu) | 2016-07-28 |
Family
ID=19148268
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0401665A HU230481B1 (hu) | 2001-10-30 | 2002-10-29 | Egy acetanilid-származék alfa kristályalakja |
Country Status (17)
Country | Link |
---|---|
US (2) | US7342117B2 (hu) |
EP (3) | EP1932838A3 (hu) |
JP (1) | JP3800220B2 (hu) |
KR (1) | KR100908796B1 (hu) |
CN (1) | CN1243740C (hu) |
AU (1) | AU2002344419C1 (hu) |
BR (1) | BRPI0213570B8 (hu) |
CA (1) | CA2464068C (hu) |
ES (1) | ES2404071T3 (hu) |
HU (1) | HU230481B1 (hu) |
MX (1) | MXPA04003936A (hu) |
NO (1) | NO326965B1 (hu) |
PL (1) | PL218982B1 (hu) |
RU (1) | RU2303033C2 (hu) |
TW (1) | TW200300020A (hu) |
WO (1) | WO2003037881A1 (hu) |
ZA (1) | ZA200403044B (hu) |
Families Citing this family (72)
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US7342117B2 (en) * | 2001-10-30 | 2008-03-11 | Astellas Pharma Inc. | α-form or β-form crystal of acetanilide derivative |
MXPA05004925A (es) * | 2002-11-07 | 2005-08-18 | Yamanouchi Pharma Co Ltd | Remedio para vejiga hiperactiva que incluye derivado de anilida de acido acetico como el ingrediente activo. |
US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
US20080125403A1 (en) | 2004-04-02 | 2008-05-29 | Merck & Co., Inc. | Method of Treating Men with Metabolic and Anthropometric Disorders |
US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
CA2688161C (en) | 2007-06-04 | 2020-10-20 | Kunwar Shailubhai | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
WO2009057685A1 (ja) * | 2007-11-02 | 2009-05-07 | Astellas Pharma Inc. | 過活動膀胱治療用医薬組成物 |
CA2726917C (en) | 2008-06-04 | 2018-06-26 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
JP2011528375A (ja) | 2008-07-16 | 2011-11-17 | シナジー ファーマシューティカルズ インコーポレイテッド | 胃腸障害、炎症、癌、およびその他の障害の治療のために有用なグアニル酸シクラーゼのアゴニスト |
TWI478712B (zh) * | 2008-09-30 | 2015-04-01 | Astellas Pharma Inc | 釋控性醫藥組成物 |
MX2011004258A (es) | 2008-10-22 | 2011-06-01 | Merck Sharp & Dohme | Derivados de bencimidazol ciclicos novedosos utiles como agentes anti-diabeticos. |
JP5557845B2 (ja) | 2008-10-31 | 2014-07-23 | メルク・シャープ・アンド・ドーム・コーポレーション | 糖尿病用剤として有用な新規環状ベンゾイミダゾール誘導体 |
WO2010147830A2 (en) * | 2009-06-15 | 2010-12-23 | Auspex Pharmaceuticals, Inc. | Aminothiazole modulators of beta-3-adrenoreceptor |
AU2011218830B2 (en) | 2010-02-25 | 2014-07-24 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
US20120070465A1 (en) | 2010-03-29 | 2012-03-22 | Astellas Pharma Inc. | Pharmaceutical composition for modified release |
EP2583967B1 (en) * | 2010-06-16 | 2014-10-01 | Takeda Pharmaceutical Company Limited | Crystal of amide compound |
US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
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US9655885B2 (en) | 2011-05-18 | 2017-05-23 | Dr. Reddy's Laboratories Ltd. | Amorphous mirabegron and processes for crystal forms of mirabegron |
WO2013147134A1 (ja) | 2012-03-30 | 2013-10-03 | アステラス製薬株式会社 | ミラベグロン含有医薬組成物 |
CN103387500A (zh) * | 2012-05-11 | 2013-11-13 | 上海医药工业研究院 | 一种米拉贝隆及其中间体的制备方法 |
AU2013296470B2 (en) | 2012-08-02 | 2016-03-17 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
EP2891493A4 (en) | 2012-08-31 | 2016-05-18 | Astellas Pharma Inc | MEDICAL COMPOSITION ADMINISTERED ORALLY |
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WO2014132270A2 (en) * | 2013-02-27 | 2014-09-04 | Msn Laboratories Limited | Process for the preparation of 2-(2-aminothiazol-4-yl)-n-[4-(2-{[(2r)-2-hydroxy-2-phenyl ethyl]amino}ethyl)phenyl]acetamide monohydrochloride, its intermediates and polymorph thereof |
US9650375B2 (en) | 2013-03-14 | 2017-05-16 | Merck Sharp & Dohme Corp. | Indole derivatives useful as anti-diabetic agents |
CA2905435A1 (en) | 2013-03-15 | 2014-09-25 | Synergy Pharmaceuticals Inc. | Compositions useful for the treatment of gastrointestinal disorders |
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WO2015040605A1 (en) | 2013-09-23 | 2015-03-26 | Ranbaxy Laboratories Limited | Crystalline form of mirabegron |
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ITMI20131653A1 (it) | 2013-10-07 | 2015-04-08 | Dipharma Francis Srl | Forme cristalline di un agonista adrenergico |
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CN103641792B (zh) * | 2013-12-27 | 2015-07-22 | 国药集团国瑞药业有限公司 | 一种米拉贝隆有关物质或其盐、其制备方法和用途 |
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CN103896872A (zh) * | 2014-04-29 | 2014-07-02 | 黑龙江大学 | 米拉贝隆的合成方法 |
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EP3177589B1 (en) | 2014-08-06 | 2018-06-20 | Interquim, S.A. | Method for the synthesis of mirabegron and its derivatives |
WO2016024284A2 (en) | 2014-08-07 | 2016-02-18 | Wanbury Ltd. | A process for the preparation of mirabegron and its intermediates |
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JP2018090490A (ja) | 2015-03-31 | 2018-06-14 | アステラス製薬株式会社 | ミラベグロン含有医薬組成物 |
FR3043555B1 (fr) * | 2015-11-17 | 2019-10-25 | Centre National De La Recherche Scientifique (Cnrs) | Mirabegron pour le traitement de maladies retiniennes |
EP3184516A1 (en) | 2015-12-23 | 2017-06-28 | Enantia, S.L. | Crystalline inclusion complexes of mirabegron with beta-cyclodextrin |
CN105801438A (zh) * | 2016-04-12 | 2016-07-27 | 济南大学 | 一种米拉贝隆中间体的合成方法 |
CN107963976A (zh) * | 2016-10-20 | 2018-04-27 | 中国动物疫病预防控制中心 | 一种苯乙醇胺类化合物中间体的制备方法 |
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US10968232B2 (en) | 2016-12-20 | 2021-04-06 | Merck Sharp & Dohme Corp. | Antidiabetic spirochroman compounds |
EP3360866B1 (en) | 2017-02-14 | 2019-01-02 | Alfred E. Tiefenbacher (GmbH & Co. KG) | Mirabegron prodrugs |
KR101868438B1 (ko) | 2017-04-13 | 2018-06-20 | (주) 성운파마코피아 | 아미드 유도체의 제조방법 |
KR102398639B1 (ko) | 2017-06-20 | 2022-05-17 | (주) 성운파마코피아 | 아미드 유도체의 염 및 그 제조방법 |
CN108658797A (zh) * | 2018-06-19 | 2018-10-16 | 安徽德信佳生物医药有限公司 | 一种米拉贝隆中间体(r)-2-(4-硝基苯乙基氨基)-1-苯基乙醇盐酸盐的合成 |
CN108947853A (zh) * | 2018-06-29 | 2018-12-07 | 黑龙江鑫创生物科技开发有限公司 | 一种微通道反应器合成米拉贝隆中间体的方法 |
KR101928987B1 (ko) * | 2018-08-28 | 2018-12-13 | (주) 성운파마코피아 | 신규한 고순도 미라베그론의 결정질 일수화물, 이의 제조방법 또는 용도 |
KR20200117091A (ko) | 2019-04-02 | 2020-10-14 | 제이투에이치바이오텍 (주) | 미라베그론 전구체 약물 화합물 및 이의 과민성 방광 질환의 치료 또는 개선을 위한 의약 용도 |
CN110590699B (zh) * | 2019-09-29 | 2022-11-15 | 广东先强药业有限公司 | 一种米拉贝隆的精制方法 |
EP3722285B1 (en) | 2020-04-08 | 2022-03-30 | Alfred E. Tiefenbacher (GmbH & Co. KG) | Process for preparing mirabegron enacarbil |
CN113816864B (zh) * | 2020-06-18 | 2024-03-29 | 南京正大天晴制药有限公司 | 一种(r)-2-羟基-n-[2-(4-氨基苯基)乙基]-2-苯乙胺的制备方法 |
CN114539182A (zh) * | 2020-11-24 | 2022-05-27 | 威智医药有限公司 | 转晶溶剂及其应用和米拉贝隆α晶型的制备方法 |
CN114539084B (zh) * | 2020-11-24 | 2024-04-02 | 威智医药股份有限公司 | 米拉贝隆及其中间体的制备方法 |
KR20220081033A (ko) | 2020-12-08 | 2022-06-15 | 주식회사 한서켐 | 미라베그론 α형 결정의 제조방법 |
CN112574137A (zh) * | 2021-01-19 | 2021-03-30 | 南京美瑞制药有限公司 | 一种α晶型米拉贝隆的制备方法 |
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DE1921577B2 (de) * | 1969-04-28 | 1972-04-06 | Nixdorf Computer Ag, 4790 Paderborn | Trommelartige vorrichtung zn buchungs- und schreibautomaten mit greifeinrichtung zum erfassen und einziehen von kontokarten o dgl |
JPH02279685A (ja) | 1989-04-18 | 1990-11-15 | Yoshitomi Pharmaceut Ind Ltd | 新規な結晶構造を有するチアジアジン化合物およびその製造法 |
EP1028111B1 (en) * | 1997-10-17 | 2004-05-12 | Yamanouchi Pharmaceutical Co. Ltd. | Amide derivatives or salts thereof |
JP3901832B2 (ja) | 1998-03-13 | 2007-04-04 | 大日本インキ化学工業株式会社 | キノリノン誘導体製剤、及びその製造法 |
JP2000212168A (ja) | 1999-01-22 | 2000-08-02 | Yamanouchi Pharmaceut Co Ltd | ヘキサヒドロ―1,4―ジアゼピン誘導体塩水和物の新規結晶 |
EP1129712A4 (en) * | 1999-09-10 | 2002-11-05 | Dainippon Ink & Chemicals | PREPARATIONS OF QUINOLINONE DERIVATIVES AND THEIR PRODUCTION METHOD |
US6706733B2 (en) * | 2001-05-08 | 2004-03-16 | Dainippon Ink And Chemicals, Inc. | Quinolinone derivative formulation and its production method |
US7342117B2 (en) * | 2001-10-30 | 2008-03-11 | Astellas Pharma Inc. | α-form or β-form crystal of acetanilide derivative |
-
2002
- 2002-10-20 US US10/494,018 patent/US7342117B2/en not_active Expired - Lifetime
- 2002-10-28 TW TW091132011A patent/TW200300020A/zh not_active IP Right Cessation
- 2002-10-29 HU HU0401665A patent/HU230481B1/hu unknown
- 2002-10-29 EP EP08004921A patent/EP1932838A3/en not_active Withdrawn
- 2002-10-29 EP EP10075435A patent/EP2298752B1/en not_active Expired - Lifetime
- 2002-10-29 WO PCT/JP2002/011217 patent/WO2003037881A1/ja active Application Filing
- 2002-10-29 AU AU2002344419A patent/AU2002344419C1/en active Active
- 2002-10-29 CA CA002464068A patent/CA2464068C/en not_active Expired - Lifetime
- 2002-10-29 KR KR1020047006428A patent/KR100908796B1/ko active IP Right Review Request
- 2002-10-29 JP JP2003540162A patent/JP3800220B2/ja not_active Expired - Lifetime
- 2002-10-29 EP EP02779929A patent/EP1440969A4/en not_active Withdrawn
- 2002-10-29 CN CNB02821370XA patent/CN1243740C/zh not_active Expired - Lifetime
- 2002-10-29 PL PL369874A patent/PL218982B1/pl unknown
- 2002-10-29 RU RU2004116313/04A patent/RU2303033C2/ru active
- 2002-10-29 MX MXPA04003936A patent/MXPA04003936A/es active IP Right Grant
- 2002-10-29 ES ES10075435T patent/ES2404071T3/es not_active Expired - Lifetime
- 2002-10-29 BR BRPI0213570A patent/BRPI0213570B8/pt active IP Right Grant
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2004
- 2004-04-21 ZA ZA2004/03044A patent/ZA200403044B/en unknown
- 2004-05-28 NO NO20042227A patent/NO326965B1/no not_active IP Right Cessation
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2008
- 2008-01-14 US US12/007,653 patent/US7982049B2/en active Active
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