BG64703B1 - Полиморфна форма на 2-(r)-(1-(r)-(3,5-бис(трифлуорометил) фенил)етокси)-3-(s)-(4-флуоро)-фенил-4-(3-(5-оксо-1н,4н- 1,2,4-триазоло)метилморфолин, метод за нейното получаване и фармацевтични състави, които я съдържат - Google Patents

Полиморфна форма на 2-(r)-(1-(r)-(3,5-бис(трифлуорометил) фенил)етокси)-3-(s)-(4-флуоро)-фенил-4-(3-(5-оксо-1н,4н- 1,2,4-триазоло)метилморфолин, метод за нейното получаване и фармацевтични състави, които я съдържат Download PDF

Info

Publication number: BG64703B1
Authority: BG; Bulgaria
Prior art keywords: phenyl; ethoxy; bis; fluoro; methyl
Prior art date: 1997-07-02

Application number

BG104010A

Other languages

Bulgarian (bg)

English (en)

Other versions

BG104010A (en

Inventor

Louis Crocker

James Mccauley

Original Assignee

Merck & Co. Inc.

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.)

1997-07-02

Filing date

1999-12-14

Publication date

2005-12-30

1998-01-07 Priority claimed from GBGB9800216.5A external-priority patent/GB9800216D0/en

1999-12-14 Application filed by Merck & Co. Inc. filed Critical Merck & Co. Inc.

2001-08-31 Publication of BG104010A publication Critical patent/BG104010A/xx

2005-12-30 Publication of BG64703B1 publication Critical patent/BG64703B1/bg

Links

238000000034 method Methods 0.000 title claims abstract description 26
239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 12
SJRJJKPEHAURKC-UHFFFAOYSA-N N-Methylmorpholine Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 title claims description 63
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 title claims description 8
150000001875 compounds Chemical class 0.000 claims abstract description 108
238000002360 preparation method Methods 0.000 claims abstract description 19
OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 105
-1 1- (R) - (3,5-bis (tri-fluoromethyl) phenyl) ethoxy Chemical group 0.000 claims description 97
239000000203 mixture Substances 0.000 claims description 96
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LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 62
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125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 6
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Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
- C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- 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

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Health & Medical Sciences (AREA)
Organic Chemistry (AREA)
Chemical & Material Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Pharmacology & Pharmacy (AREA)
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Animal Behavior & Ethology (AREA)
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Neurology (AREA)
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Pain & Pain Management (AREA)
Hospice & Palliative Care (AREA)
Otolaryngology (AREA)
Rheumatology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Polyamides (AREA)
Polyurethanes Or Polyureas (AREA)
Plural Heterocyclic Compounds (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

BG104010A 1997-07-02 1999-12-14 Полиморфна форма на 2-(r)-(1-(r)-(3,5-бис(трифлуорометил) фенил)етокси)-3-(s)-(4-флуоро)-фенил-4-(3-(5-оксо-1н,4н- 1,2,4-триазоло)метилморфолин, метод за нейното получаване и фармацевтични състави, които я съдържат BG64703B1 (bg)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
US5160097P	1997-07-02	1997-07-02
GBGB9800216.5A GB9800216D0 (en)	1998-01-07	1998-01-07	Polymorphic form of a tachykinin receptor antagonist

Publications (2)

Publication Number	Publication Date
BG104010A BG104010A (en)	2001-08-31
BG64703B1 true BG64703B1 (bg)	2005-12-30

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Application Number	Title	Priority Date	Filing Date
BG104010A BG64703B1 (bg)	1997-07-02	1999-12-14	Полиморфна форма на 2-(r)-(1-(r)-(3,5-бис(трифлуорометил) фенил)етокси)-3-(s)-(4-флуоро)-фенил-4-(3-(5-оксо-1н,4н- 1,2,4-триазоло)метилморфолин, метод за нейното получаване и фармацевтични състави, които я съдържат

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EP (1)	EP0994867B1 (is)
JP (1)	JP2000513383A (is)
KR (1)	KR20010020593A (is)
CN (1)	CN1106390C (is)
AT (1)	ATE372991T1 (is)
AU (1)	AU735230B2 (is)
BG (1)	BG64703B1 (is)
CA (1)	CA2293836C (is)
CZ (1)	CZ295410B6 (is)
DE (1)	DE69838421D1 (is)
DZ (1)	DZ2551A1 (is)
EA (1)	EA002405B1 (is)
EE (1)	EE04152B1 (is)
HR (1)	HRP980370B1 (is)
HU (1)	HU228003B1 (is)
ID (1)	ID23191A (is)
IL (1)	IL133357A (is)
IS (1)	IS2617B (is)
NO (1)	NO316893B1 (is)
NZ (1)	NZ501589A (is)
PE (1)	PE86499A1 (is)
PL (1)	PL191496B1 (is)
SK (1)	SK285644B6 (is)
TR (1)	TR199903299T2 (is)
TW (1)	TW577887B (is)
WO (1)	WO1999001444A1 (is)

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JP2003513095A (ja)	1999-10-29	2003-04-08	メルクエンドカムパニーインコーポレーテッド	タキキニン受容体アンタゴニストの多形
GB0203061D0 (en) *	2002-02-08	2002-03-27	Novartis Ag	Organic compounds
US7192962B2 (en) *	2002-05-31	2007-03-20	Schering Corporation	Xanthine phosphodiesterase V inhibitor polymorphs
GB0417702D0 (en) *	2004-08-09	2004-09-08	Merck Sharp & Dohme	New uses
EP2266980A1 (en) *	2005-10-05	2010-12-29	Ranbaxy Laboratories Limited	Polymorphic form of aprepitant intermediate
EP1984359A1 (en)	2006-02-03	2008-10-29	Glenmark Pharmaceuticals Limited	Amorphous and crystalline forms of aprepitant and processes for the preparation thereof
EP2662374A1 (en)	2006-04-05	2013-11-13	OPKO Health, Inc.	Salts of 8-[{1-(3,5-bis-(trifluoromethyl) phenyl) -ethoxy}-methyl]-8-phenyl-1,7 -diaza-spiro[4.5]decan-2-one and preparation process therefor
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Also Published As

Publication number	Publication date
SK285644B6 (sk)	2007-05-03
TR199903299T2 (xx)	2000-07-21
NO996549L (no)	2000-03-01
EE9900603A (et)	2000-08-15
CA2293836A1 (en)	1999-01-14
SK187299A3 (en)	2000-07-11
NO316893B1 (no)	2004-06-14
WO1999001444A1 (en)	1999-01-14
KR20010020593A (ko)	2001-03-15
HUP0004008A3 (en)	2002-03-28
AU735230B2 (en)	2001-07-05
CA2293836C (en)	2007-06-05
EE04152B1 (et)	2003-10-15
IS5293A (is)	1999-12-10
IS2617B (is)	2010-04-15
EP0994867A1 (en)	2000-04-26
IL133357A (en)	2003-12-10
HRP980370A2 (en)	1999-04-30
ATE372991T1 (de)	2007-09-15
PE86499A1 (es)	1999-10-25
HUP0004008A2 (hu)	2002-02-28
JP2000513383A (ja)	2000-10-10
HK1029345A1 (en)	2001-03-30
DE69838421D1 (en)	2007-10-25
ID23191A (id)	2000-03-23
PL191496B1 (pl)	2006-05-31
CZ477799A3 (cs)	2000-09-13
EP0994867B1 (en)	2007-09-12
EA002405B1 (ru)	2002-04-25
HRP980370B1 (en)	2002-10-31
PL337579A1 (en)	2000-08-28
CN1261882A (zh)	2000-08-02
CN1106390C (zh)	2003-04-23
IL133357A0 (en)	2001-04-30
HU228003B1 (en)	2012-08-28
EA199901114A1 (ru)	2000-08-28
TW577887B (en)	2004-03-01
NO996549D0 (no)	1999-12-29
NZ501589A (en)	2001-10-26
BG104010A (en)	2001-08-31
CZ295410B6 (cs)	2005-08-17
DZ2551A1 (fr)	2003-08-15
AU8283398A (en)	1999-01-25

Publication	Publication Date	Title
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AU735230B2 (en)	2001-07-05	Polymorphic form of the tachykinin receptor antagonist 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl) phenyl)ethoxy)-3-(S)-(4-fluoro) phenyl-4-(3-5 (-oxo-1H,4H-1,2,4,-triazolo) methylmorpholine
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US5457107A (en)	1995-10-10	Polymorphic form of a tachykinin receptor antagonist
US6096766A (en)	2000-08-01	3-benzylaminopiperidines as tachykinin receptor antagonists
US5919803A (en)	1999-07-06	3-benzylamino-2-phenylpiperidines as neurokinin antagonists
JP3245424B2 (ja)	2002-01-15	モルホリンおよびチオモルホリン系のタキキニン受容体拮抗薬
HU217428B (hu)	2000-01-28	3-(5-Tetrazolil-benzil)-amino-piperidin-származékok, eljárás előállításukra és ezeket a vegyületeket tartalmazó gyógyászati készítmények
US6432952B1 (en)	2002-08-13	Polymorphic form of a tachykinin receptor antagonist
MXPA99012067A (en)	2001-12-04	Polymorphic form of the tachykinin receptor antagonist 2-(r)-(1-(r) -(3,5-bis(trifluoromethyl) phenyl)ethoxy)-3-(s)-(4-fluoro) phenyl-4-(3-5 (-oxo-1h,4h-1,2,4,-triazolo) methylmorpholine
UA57089C2 (uk)	2003-06-16	Поліморфна форма 2-(r)-(1(r)-(3,5-біс(трифторметил)феніл)етокси)-3-(s)-(4-фтор)феніл-4-(3-(5-оксо-1h,4h-1,2,4-триазоло)метил)морфоліну як антагоніст рецептора тахікініну
HK1029345B (en)	2004-02-06	Polymorphic form of the tachykinin receptor antagonist 2-(r)-(1-(r)-(3,5-bis(trifluoromethyl) phenyl)ethoxy)-3(s)-(4-fluoro) phenyl-4-(3-5(-oxo-1h,4h-1,2,4,-triazolo) methylmorpholine
JPH05239037A (ja)	1993-09-17	セロトニン神経系関連疾患治療剤