[go: up one dir, main page]

WO2010092591A3 - Crystalline polymorphs of 5-[[(2r,3s)-2-[(1r)-1-[3,5- bis(trifluoromethyl) phenyl] ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2- dihydro-3h-1,2,4-triazol-3-one and process for preparation thereof - Google Patents

Crystalline polymorphs of 5-[[(2r,3s)-2-[(1r)-1-[3,5- bis(trifluoromethyl) phenyl] ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2- dihydro-3h-1,2,4-triazol-3-one and process for preparation thereof Download PDF

Info

Publication number
WO2010092591A3
WO2010092591A3 PCT/IN2009/000370 IN2009000370W WO2010092591A3 WO 2010092591 A3 WO2010092591 A3 WO 2010092591A3 IN 2009000370 W IN2009000370 W IN 2009000370W WO 2010092591 A3 WO2010092591 A3 WO 2010092591A3
Authority
WO
WIPO (PCT)
Prior art keywords
preparation
triazol
morpholinyl
fluorophenyl
dihydro
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.)
Ceased
Application number
PCT/IN2009/000370
Other languages
French (fr)
Other versions
WO2010092591A2 (en
Inventor
Dhananjay Govind Sathe
Nandu Baban Bhise
Kamlesh Digambar Sawant
Anand Vinod Shindikar
Sachin Shivaji Patil
Tushar Anil Naik
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
USV Pvt Ltd
Original Assignee
USV Pvt Ltd
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 USV Pvt Ltd filed Critical USV Pvt Ltd
Publication of WO2010092591A2 publication Critical patent/WO2010092591A2/en
Publication of WO2010092591A3 publication Critical patent/WO2010092591A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Disclosed herein is novel polymorph of 5-[[(2R,3S)-2-[(1R)-1-[3,5- bis(trifluoromethyl) phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2- dihydro-3H-1,2,4- triazol-3-one, commonly known as Aprepitant or pharmaceutically acceptable salts thereof and process for preparation thereof. The present invention further relates to highly pure polymorph, Form II of Aprepitant. The present invention further relates to improved process for preparation of Aprepitant.
PCT/IN2009/000370 2008-06-30 2009-06-29 Novel crystalline polymorphs of 5-[[(2r,3s)-2-[(1r)-1-[3,5- bis(trifluoromethyl) phenyl] ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2- dihydro-3h-1,2,4-triazol-3-one and process for preparation thereof Ceased WO2010092591A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1358/MUM/2008 2008-06-30
IN1358MU2008 2008-06-30

Publications (2)

Publication Number Publication Date
WO2010092591A2 WO2010092591A2 (en) 2010-08-19
WO2010092591A3 true WO2010092591A3 (en) 2010-12-16

Family

ID=42562136

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2009/000370 Ceased WO2010092591A2 (en) 2008-06-30 2009-06-29 Novel crystalline polymorphs of 5-[[(2r,3s)-2-[(1r)-1-[3,5- bis(trifluoromethyl) phenyl] ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2- dihydro-3h-1,2,4-triazol-3-one and process for preparation thereof

Country Status (1)

Country Link
WO (1) WO2010092591A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102939285B (en) * 2010-05-24 2014-12-24 成都地奥制药集团有限公司 Preparation method of 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazole-3-one
HUP1000325A2 (en) 2010-06-18 2012-01-30 Druggability Technologies Ip Holdco Jersey Ltd Nanostructured aprepitant compositions and process for their preparation
CZ304770B6 (en) * 2012-03-13 2014-10-08 Zentiva, K.S. Process for preparing 3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorfenyl)morpholino)methyl)-1H-1,2,4-triazol-5(4H)-one (aprepitant) in polymorphous form II
CZ304982B6 (en) * 2012-04-30 2015-03-11 Zentiva, K.S. Process for preparing and purifying novel polymorphs of fosaprepitant intermediate
CN103193725A (en) * 2013-04-12 2013-07-10 上海医药工业研究院 Preparation method of (2R, 3R)-2-((1R)-1-(3, 5-bis (trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl) morpholine
CN104119325B (en) * 2014-07-15 2017-03-22 中山奕安泰医药科技有限公司 Preparation method of aprepitant polymorphic substance
CN110776502B (en) * 2019-12-06 2021-04-20 广州白云山汉方现代药业有限公司 Refining method of aprepitant

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5719147A (en) * 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
US6096742A (en) * 1997-07-02 2000-08-01 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
WO2007044829A2 (en) * 2005-10-06 2007-04-19 Dr. Reddy's Laboratories Ltd. Preparation of aprepitant
WO2007088483A1 (en) * 2006-02-03 2007-08-09 Glenmark Pahrmaceuticals Limited Amorphous and crystalline forms of aprepitant and processes for the preparation thereof
WO2007112457A2 (en) * 2006-03-29 2007-10-04 Dr. Reddy's Labortories, Ltd. Aprepitant polymorph mixtures
WO2008026216A2 (en) * 2006-08-28 2008-03-06 Hetero Drugs Limited Process for purification of aprepitant
WO2008044102A1 (en) * 2006-10-13 2008-04-17 Glenmark Pharmaceuticals Limited Polymorph form of aprepitant and process for the preparation thereof
WO2008104512A2 (en) * 2007-02-27 2008-09-04 Sandoz Ag Novel polymorphs of aprepitant and processes for preparation

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5719147A (en) * 1992-06-29 1998-02-17 Merck & Co., Inc. Morpholine and thiomorpholine tachykinin receptor antagonists
US6096742A (en) * 1997-07-02 2000-08-01 Merck & Co., Inc. Polymorphic form of a tachykinin receptor antagonist
WO2007044829A2 (en) * 2005-10-06 2007-04-19 Dr. Reddy's Laboratories Ltd. Preparation of aprepitant
WO2007088483A1 (en) * 2006-02-03 2007-08-09 Glenmark Pahrmaceuticals Limited Amorphous and crystalline forms of aprepitant and processes for the preparation thereof
WO2007112457A2 (en) * 2006-03-29 2007-10-04 Dr. Reddy's Labortories, Ltd. Aprepitant polymorph mixtures
WO2008026216A2 (en) * 2006-08-28 2008-03-06 Hetero Drugs Limited Process for purification of aprepitant
WO2008044102A1 (en) * 2006-10-13 2008-04-17 Glenmark Pharmaceuticals Limited Polymorph form of aprepitant and process for the preparation thereof
WO2008104512A2 (en) * 2007-02-27 2008-09-04 Sandoz Ag Novel polymorphs of aprepitant and processes for preparation

Also Published As

Publication number Publication date
WO2010092591A2 (en) 2010-08-19

Similar Documents

Publication Publication Date Title
WO2010092591A3 (en) Crystalline polymorphs of 5-[[(2r,3s)-2-[(1r)-1-[3,5- bis(trifluoromethyl) phenyl] ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2- dihydro-3h-1,2,4-triazol-3-one and process for preparation thereof
WO2009055721A3 (en) 5-lipoxygenase activating protein (flap) inhibitor
WO2008027542A3 (en) 5-substituted isoindoline compounds
WO2007096151A3 (en) Inhibitors of p38-kinase for treatment of pulmonary hypertension
WO2012147107A3 (en) Novel & improved processes for preparing indoline derivatives and its pharmaceutical composition
WO2007017135A3 (en) Process for the preparation of olmesartan medoxomil
PL2559689T3 (en) Preparation process for crystalline forms of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]benzoic acid
NZ599008A (en) 2-amino-5, 5-difluoro-5, 6-dihydro-4h-oxazines as bace 1 and/or bace 2 inhibitors
EA200501075A1 (en) DRUG FOR PREVENTION AND TREATMENT OF ARTERIOCLEROSIS AND HYPERTENSION
CO6150139A2 (en) TARTRATE SALT OF 1- [2- FLUORIDE-4- (TRIFLUOROMETIL) PHENYL] -3- (3 - {[4-METHYL-5- (4-METHYL-1,3 OXAZOL-5-IL) -4H-1 , 2,4-TRIAZOL-3 IL] UNCLE} PROPIL) -3-AZABICICLO [3.1.0] -HEXAN AND ITS SOLVATES, PHARMACEUTICAL FORMULATIONS, PROCEDURES FOR THEIR PREPARATION AND THEIR
MX2009006636A (en) Novel intermediate and process useful in the preparation of {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1h-[1,2,3 ]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone.
WO2007099553A3 (en) 1,3-dioxane carboxylic acids
WO2009125434A3 (en) Oxime derivatives, process for their preparation, pharmaceutical composition containing the same and medicinal use thereof
WO2001090081A1 (en) Substituted 1-aminoalkyl-lactams and their use as muscarinic receptor antagonists
WO2010084514A3 (en) A process for the preparation of (5s)-(n)-[[3-[3-fluoro-4-(4-morpholinyl) phenyl]-2-oxo-5-oxazolidinyl] methyl] acetamide
NZ596820A (en) Trans-4-[[(5s)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl] (2-methyl-2h-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid
WO2008038092A3 (en) Substituted piperidinophenyl oxazolidinones
NZ597866A (en) Therapeutic lactams
TW201300382A (en) Polymorph form of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid
TWI341313B (en) Process for the synthesis of 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazol-3-one
WO2007039883A3 (en) Process for preparation of aprepitant
WO2008126106A3 (en) Novel and improved processes for the preparation of intermediates of darifenacin, darifenacin and its pharmaceutically acceptable salts
UA96575C2 (en) Process for the preparation of olmesartan medoxomil
TW200833323A (en) Prophylactic or therapeutic agent for alopecia
WO2009021943A3 (en) Novel preparation process

Legal Events

Date Code Title Description
NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 09839937

Country of ref document: EP

Kind code of ref document: A2