DK0761650T3 - Termostabil og holdbar krystalmodifikation af N-methyl-N-((1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)-ethyl)-2,2-diphenyl-acetamid og fremgangsmåde til dets fremstilling - Google Patents

Termostabil og holdbar krystalmodifikation af N-methyl-N-((1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)-ethyl)-2,2-diphenyl-acetamid og fremgangsmåde til dets fremstilling

Info

Publication number: DK0761650T3
Authority: DK; Denmark
Prior art keywords: hydroxypyrrolidin; thermostable; acetamide; diphenyl; phenyl
Prior art date: 1995-08-26

Application number

DK96112489T

Other languages

Danish (da)

English (en)

Inventor

Inge Dr Stein

Holger Beeres

Klaus Dr Beschmann

Steffen Dr Neuenfeld

Andrew Dr Barber

Original Assignee

Merck Patent Gmbh

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.)

1995-08-26

Filing date

1996-08-02

Publication date

2002-02-18

1996-08-02 Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh

2002-02-18 Application granted granted Critical

2002-02-18 Publication of DK0761650T3 publication Critical patent/DK0761650T3/da

Links

JHLHNYVMZCADTC-LOSJGSFVSA-N asimadoline Chemical compound C([C@@H](N(C)C(=O)C(C=1C=CC=CC=1)C=1C=CC=CC=1)C=1C=CC=CC=1)N1CC[C@H](O)C1 JHLHNYVMZCADTC-LOSJGSFVSA-N 0.000 title 1
239000013078 crystal Substances 0.000 title 1
238000000034 method Methods 0.000 title 1
230000004048 modification Effects 0.000 title 1
238000012986 modification Methods 0.000 title 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D207/12—Oxygen or sulfur atoms
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
- 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

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Pain & Pain Management (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Biomedical Technology (AREA)
Epidemiology (AREA)
Dermatology (AREA)
Rheumatology (AREA)
Urology & Nephrology (AREA)
Pulmonology (AREA)
Immunology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Pyrrole Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Medicinal Preparation (AREA)

DK96112489T 1995-08-26 1996-08-02 Termostabil og holdbar krystalmodifikation af N-methyl-N-((1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)-ethyl)-2,2-diphenyl-acetamid og fremgangsmåde til dets fremstilling DK0761650T3 (da)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
DE19531464A DE19531464A1 (de)	1995-08-26	1995-08-26	N-Methyl-N-[(1S-)-1-phenyl-2-((3S)-3-hydroxypyrrolidin 1-yl-)-ethyl]-2,2-diphenyl-acetamid

Publications (1)

Publication Number	Publication Date
DK0761650T3 true DK0761650T3 (da)	2002-02-18

Family

ID=7770485

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
DK96112489T DK0761650T3 (da)	1995-08-26	1996-08-02	Termostabil og holdbar krystalmodifikation af N-methyl-N-((1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)-ethyl)-2,2-diphenyl-acetamid og fremgangsmåde til dets fremstilling

Country Status (25)

Country	Link
US (1)	US6060504A (cs)
EP (1)	EP0761650B1 (cs)
JP (3)	JP5023273B2 (cs)
KR (1)	KR100436254B1 (cs)
CN (1)	CN1081631C (cs)
AR (1)	AR004679A1 (cs)
AT (1)	ATE207895T1 (cs)
AU (1)	AU716615B2 (cs)
BR (1)	BR9603540A (cs)
CA (1)	CA2184049C (cs)
CZ (1)	CZ287783B6 (cs)
DE (2)	DE19531464A1 (cs)
DK (1)	DK0761650T3 (cs)
ES (1)	ES2165948T3 (cs)
HU (1)	HU226667B1 (cs)
MX (1)	MX9603606A (cs)
NO (1)	NO307048B1 (cs)
PL (1)	PL187691B1 (cs)
PT (1)	PT761650E (cs)
RU (1)	RU2174976C2 (cs)
SI (1)	SI0761650T1 (cs)
SK (1)	SK282437B6 (cs)
TW (1)	TW513407B (cs)
UA (1)	UA41978C2 (cs)
ZA (1)	ZA967200B (cs)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
AU1828399A (en) *	1997-12-22	1999-07-12	Alza Corporation	Novel formulations for the transdermal administration of asimadoline
DE19827633A1 (de) *	1998-04-20	1999-10-21	Merck Patent Gmbh	Verfahren zur Herstellung von enantiomerenreinem N-Methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamid
US6174878B1 (en) *	1999-08-31	2001-01-16	Alcon Laboratories, Inc.	Topical use of kappa opioid agonists to treat otic pain
DE10116978A1 (de) *	2001-04-05	2002-10-10	Merck Patent Gmbh	Kappa-Opiatagonisten für die Behandlung von Erkrankungen der Blase
WO2003097051A2 (en) *	2002-05-17	2003-11-27	Merck Patent Gmbh	Use of compounds that are effective as selective opiate receptor modulators
DE10259245A1 (de) *	2002-12-17	2004-07-01	Merck Patent Gmbh	Derivate des Asimadolins mit kovalent gebundenen Säuren
EP1680115A1 (en) *	2003-10-30	2006-07-19	Tioga Pharmaceuticals, Inc.	Use of selective opiate receptor modulators in the treatment of neuropathy
CA2682608A1 (en)	2007-03-30	2008-10-09	Tioga Pharmaceuticals, Inc.	Kappa-opiate agonists for the treatment of diarrhea-predominant and alternating irritable bowel syndrome
EP2284987B1 (en) *	2009-08-12	2019-02-06	Braun GmbH	Method and device for adjusting the frequency of a drive current of an electric motor
NZ602872A (en) *	2010-04-07	2014-05-30	Onyx Therapeutics Inc	Crystalline peptide epoxyketone immunoproteasome inhibitor
US9675587B2 (en)	2013-03-14	2017-06-13	Allergan Holdings Unlimited Company	Opioid receptor modulator dosage formulations
CN103664727A (zh) *	2013-12-19	2014-03-26	无锡万全医药技术有限公司	一种一锅法制备1-[(3s)-3-羟基吡咯烷-1-基]-(2s)-2-甲氨基-2-苯基乙烷的工艺
ES2906979T3 (es)	2016-12-21	2022-04-21	Tioga Pharmaceuticals Inc	Formulaciones farmacéuticas sólidas de asimadolina
EP3932390A1 (en)	2020-07-02	2022-01-05	Dr. August Wolff GmbH & Co. KG Arzneimittel	Topical gel formulation containing asimadoline

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
SE8205135D0 (sv) *	1982-09-09	1982-09-09	Astra Laekemedel Ab	Benzamido-derivatives
DE4034785A1 (de) *	1990-11-02	1992-05-07	Merck Patent Gmbh	1-(2-arylethyl)-pyrrolidine
DE4215213A1 (de) *	1992-05-09	1993-11-11	Merck Patent Gmbh	Arylacetamide

1995
- 1995-08-26 DE DE19531464A patent/DE19531464A1/de not_active Withdrawn
1996
- 1996-08-02 EP EP96112489A patent/EP0761650B1/de not_active Expired - Lifetime
- 1996-08-02 SI SI9630392T patent/SI0761650T1/xx unknown
- 1996-08-02 DK DK96112489T patent/DK0761650T3/da active
- 1996-08-02 PT PT96112489T patent/PT761650E/pt unknown
- 1996-08-02 ES ES96112489T patent/ES2165948T3/es not_active Expired - Lifetime
- 1996-08-02 AT AT96112489T patent/ATE207895T1/de active
- 1996-08-02 DE DE59608050T patent/DE59608050D1/de not_active Expired - Lifetime
- 1996-08-16 CZ CZ19962434A patent/CZ287783B6/cs not_active IP Right Cessation
- 1996-08-19 AU AU62149/96A patent/AU716615B2/en not_active Ceased
- 1996-08-21 UA UA96083322A patent/UA41978C2/uk unknown
- 1996-08-22 JP JP22129696A patent/JP5023273B2/ja not_active Expired - Fee Related
- 1996-08-22 SK SK1089-96A patent/SK282437B6/sk not_active IP Right Cessation
- 1996-08-23 TW TW085110305A patent/TW513407B/zh not_active IP Right Cessation
- 1996-08-23 CA CA002184049A patent/CA2184049C/en not_active Expired - Fee Related
- 1996-08-23 CN CN96111404A patent/CN1081631C/zh not_active Expired - Fee Related
- 1996-08-23 AR ARP960104088A patent/AR004679A1/es not_active Application Discontinuation
- 1996-08-23 RU RU96116925/04A patent/RU2174976C2/ru not_active IP Right Cessation
- 1996-08-23 NO NO963526A patent/NO307048B1/no not_active IP Right Cessation
- 1996-08-23 PL PL96315799A patent/PL187691B1/pl not_active IP Right Cessation
- 1996-08-23 MX MX9603606A patent/MX9603606A/es unknown
- 1996-08-23 ZA ZA967200A patent/ZA967200B/xx unknown
- 1996-08-23 BR BR9603540A patent/BR9603540A/pt active Search and Examination
- 1996-08-24 KR KR1019960035289A patent/KR100436254B1/ko not_active Expired - Fee Related
- 1996-08-26 HU HU9602346A patent/HU226667B1/hu not_active IP Right Cessation
- 1996-08-26 US US08/703,350 patent/US6060504A/en not_active Expired - Lifetime
2008
- 2008-10-02 JP JP2008257423A patent/JP2009046501A/ja active Pending
2012
- 2012-09-18 JP JP2012204622A patent/JP2012246321A/ja active Pending

Also Published As

Publication number	Publication date
DE19531464A1 (de)	1997-02-27
NO307048B1 (no)	2000-01-31
TW513407B (en)	2002-12-11
NO963526D0 (no)	1996-08-23
SK108996A3 (en)	1997-06-04
CZ243496A3 (en)	1997-03-12
NO963526L (no)	1997-02-27
PL315799A1 (en)	1997-03-03
HUP9602346A3 (en)	1998-01-28
JP2009046501A (ja)	2009-03-05
CZ287783B6 (en)	2001-02-14
JP5023273B2 (ja)	2012-09-12
SI0761650T1 (en)	2002-04-30
MX9603606A (es)	1997-03-29
EP0761650A1 (de)	1997-03-12
EP0761650B1 (de)	2001-10-31
AU716615B2 (en)	2000-03-02
HUP9602346A2 (en)	1997-09-29
ATE207895T1 (de)	2001-11-15
AR004679A1 (es)	1999-03-10
AU6214996A (en)	1997-03-06
HU226667B1 (en)	2009-06-29
JP2012246321A (ja)	2012-12-13
KR100436254B1 (ko)	2005-01-25
CN1151986A (zh)	1997-06-18
JPH09110830A (ja)	1997-04-28
UA41978C2 (uk)	2001-10-15
CN1081631C (zh)	2002-03-27
BR9603540A (pt)	1998-05-12
ZA967200B (en)	1997-03-03
HU9602346D0 (en)	1996-10-28
PT761650E (pt)	2002-04-29
PL187691B1 (pl)	2004-09-30
US6060504A (en)	2000-05-09
SK282437B6 (sk)	2002-02-05
KR970010744A (ko)	1997-03-27
ES2165948T3 (es)	2002-04-01
CA2184049A1 (en)	1997-02-27
CA2184049C (en)	2007-10-02
DE59608050D1 (de)	2001-12-06
RU2174976C2 (ru)	2001-10-20

Publication	Publication Date	Title
DK0761650T3 (da)	2002-02-18	Termostabil og holdbar krystalmodifikation af N-methyl-N-((1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)-ethyl)-2,2-diphenyl-acetamid og fremgangsmåde til dets fremstilling
EE03921B1 (et)	2002-12-16	N-(3-bensofuranüül)karbamiidderivaadid, nende valmistamismeetod ja kasutamine
BR9810654B1 (pt)	2013-01-08	mÉtodo de preparaÇço de um polipeptÍdeo, molÉculas de anticorpo e composiÇço.
NO982055L (no)	1998-05-06	2-alkylpyrrolidiner
BR9508262A (pt)	1997-12-23	Processo de estruturar um quadro de dados e receptor
KR950701085A (ko)	1995-02-20	내부 고정 스페이서를 이용하는 액정광 밸브 및 이의 사용 방법(Improved Liquid Crystal Light Valves Using Internal, Fixed Spacers and Method of Incorporating Same)
DK0839132T3 (da)	2001-04-09	Fremgangsmåde til fremstilling af amorft [R-(R,R)]-2-(4-fluorphenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[
NO983387L (no)	1998-09-22	Oksygeneringsapparat, fremgangsmåte ved oksygenering av vann og anvendelse derav
DE69618661D1 (de)	2002-02-28	Flüssigkristalline (meth)acrylat-verbindungen, zusammensetzung und verfahren dafür
ATE214275T1 (de)	2002-03-15	Verwendung von n-methyl-n-((1s)-1-phenyl-2-((3s)- 3-hydroxypyrrolidin-1-yl)-ethyl)-2,2-diphenyl- acetamid hydrochlorid zur herstellung von arzneimitteln zur behandlung von entzündlichen darmerkrankungen
DK0773984T3 (da)	2000-04-10	Enzymholdig granuleret substans og fremgangsmåde til fremstilling heraf
BR9600690A (pt)	1997-12-30	Catalisadores suportes de catalisador e processo de preparação dos mesmos
EE9600187A (et)	1997-06-16	Filter jookide, peamiselt kohvi jaoks ja meetod selle tootmiseks
NO981403D0 (no)	1998-03-27	Fremgangsmåte og blanding for kontrollering av begroing ved bruk av amider
EE200300153A (et)	2003-06-16	Östrogeeni retseptori modulaatorid, farmatseutiline kompositsioon ja selle valmistamismeetod
NO20021423D0 (no)	2002-03-21	Beströket, optisk lysnet trykkpapir og fremgangsmåte for fremstilling derav
DK0727416T3 (da)	2000-06-13	Substituerede benzensulfonylurinstoffer og -thiourinstoffer, og fremgangsmåde til deres fremstilling, deres anvendelse som
AU6801596A (en)	1997-04-10	Method and apparatus for treatment of neurogenic diabetes mellitus, and other conditions
DE69819867D1 (de)	2003-12-24	Linsenrasterfilm, seine herstellungsmethode, und transmissionsartiger schirm
FI953532L (fi)	1995-07-21	Nitroglyserolia sisältävä laastari, menetelmä sen valmistamiseksi ja sen käyttö
ATE303361T1 (de)	2005-09-15	Verfahren zur herstellung von enantiomerenreinem n-methyl- n- (1s)- 1-phenyl- 2-((3s)-3- hydroxypyrrolidin- 1-yl)ethyl)- 2,2- diphenylacetamid
NO972118L (no)	1997-11-10	Varmeherdende blandinger med bedret latens, fremgangsmåte for fremstilling og anvendelse derav
FI971081L (fi)	1997-05-06	Triatsolopyridatsiinit, menetelmä ja välituotteet niiden valmistamiseksi sekä niiden käyttö lääkeaineina
AU4034699A (en)	2000-06-05	Method for racemization of optically active amines
EE200100219A (et)	2002-08-15	(+)-alfa-(2,3-dimetoksüfenüül)-1-[2-(4-fluorofenüül)etüül]-4-piperidiinmetanooli estrid, nende valmistamismeetod, kasutamine ja farmatseutiline kompositsioon