KR970010744A - N-메틸-n-[(1s)-1-페닐-2-((3s)-3-하이드록시피롤리딘-1-일)에틸]-2,2-디페닐아세트아미드 - Google Patents

N-메틸-n-[(1s)-1-페닐-2-((3s)-3-하이드록시피롤리딘-1-일)에틸]-2,2-디페닐아세트아미드 Download PDF

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KR970010744A
KR970010744A KR1019960035289A KR19960035289A KR970010744A KR 970010744 A KR970010744 A KR 970010744A KR 1019960035289 A KR1019960035289 A KR 1019960035289A KR 19960035289 A KR19960035289 A KR 19960035289A KR 970010744 A KR970010744 A KR 970010744A
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hydroxypyrrolidin
pain
pharmaceutical formulation
medicament according
treatment
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KR100436254B1 (ko
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잉게 스타인
홀거 베에레스
클라우스 베슈만
스테펜 노이엔펠트
앤드류 바버
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슈틀러, 하르트만
메르크 파텐트 게젤샤프트 미트 베쉬랭크터 하프퉁
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    • 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
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  • Health & Medical Sciences (AREA)
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Abstract

본 발명은 신규한 열-안정성 형태의 N-메틸-N-[(1S)-1-페닐-2-((3S)-3-하이드록시 피롤리딘-1-일)에틸]-2,2-디페닐아세트아미드, 상기 화합물을 상기 신규한 형태로 제조 및 단리하는 방법, 및 상기 화합물 및/또는 그의 생리학적으로 허용가능한 염들 중 하나를 함유하는 약제의 제조를 위한 용도에 관한 것이다.

Description

N-메틸-N-[(1S)-1-페닐-2-((3S)-3-하이드록시 피롤리딘-1-일)에틸]-2,2-디페닐아세트아미드
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 열-안정성 결정 변형물을 갖는 N-메틸-N-[(1S)-1-페닐-2-((3S)-3-하이드록시 피롤리딘-1-일)에틸]-2,2-디페닐아세트아미드 하이드로클로라이드.
  2. 제1항에 있어서, 220 내지 225℃의 융점을 갖는 화합물.
  3. 청구항 1에 따른 화합물을 함유하는 약제.
  4. 카파-아편제 작용물질로서 약리 작용을 갖는 약학 제형의 제조를 위한 청구항 3에 따른 약제의 용도.
  5. 염증성 장 질환 치료용 약학 제형의 제조를 위한 청구항 3에 따른 약제의 용도.
  6. 등 질환에서 발생하는 통증 및 통증 과민증 치료용 약학 제형의 제조를 위한 청구항 3에 따른 약제의 용도.
  7. 류마티스성 질환, 화상 손상, 일광화상 또는 신경피부염의 통증, 통증 과민증 및 염증 반응 치료용 약학 제형의 제조를 위한 청구항 3에 따른 약제의 용도.
  8. 수술후 통증, 통증 과민증 및 수술후 장폐색 치료용 약학 제형의 제조를 위한 청구항 3에 따른 약제의 용도.
  9. 청구항 3에 따른 약제를 함유함을 특징으로 하는 약학 제제.
  10. a) 1-[(1S)-3-하이드록시피롤리딘-1-일]-(2S)-2-메틸아미노-2-페닐에탄 및 디페닐아세틸 클로라이드를 저온, 특히 -5 내지 10℃에서, b) 용매중에 용해된 디페닐아세틸 클로라이드를, 상기 온도를 유지시키면서 동일한 용매중에 용해되고 초기에 장치내로 도입된 1-[(1S)-3-하이드록시피롤리딘-1-일]-(2S)-1-메틸아미노-2-페닐에탄에 서서히 가함으로써 서로 반응시키고, c) 상기 반응에 이어서 고온 용매로부터 수득된 조 생성물을 재결정시킴을 특징으로 하는, N-메틸-N-[(1S)-1-페닐-2-((3S)-3-하이드록시피롤리딘-1-일)에틸]-2,2-디페닐아세트아미드 하이드로클로라이드의 제조 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019960035289A 1995-08-26 1996-08-24 N-메틸-n[(1s)-1-페닐-2-((3s)-3-하이드록시피롤리딘-1-일)에틸]-2,2-디페닐아세트아미드 KR100436254B1 (ko)

Applications Claiming Priority (2)

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DE19531464.6 1995-08-26
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

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KR100436254B1 KR100436254B1 (ko) 2005-01-25

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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
CN100411618C (zh) * 2002-05-17 2008-08-20 迪欧加药品公司 有效的选择性阿片受体调制剂化合物的用途
DE10259245A1 (de) * 2002-12-17 2004-07-01 Merck Patent Gmbh Derivate des Asimadolins mit kovalent gebundenen Säuren
US20080090859A1 (en) * 2003-10-30 2008-04-17 Tioga Pharmaceuticals, Inc. Use of Selective Opiate Receptor Modulators In the Treatment Of Neuropathy
PL2136801T3 (pl) 2007-03-30 2013-01-31 Tioga Pharmaceuticals Inc Agoniści kappa-opioidów do leczenia zespołu jelita drażliwego w postaci zmiennej i z dominującą biegunką
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
KR20130094185A (ko) * 2010-04-07 2013-08-23 오닉스 세라퓨틱스, 인크. 결정성 펩티드 에폭시케톤 면역프로테아좀 저해제
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

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DE4215213A1 (de) * 1992-05-09 1993-11-11 Merck Patent Gmbh Arylacetamide

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PL187691B1 (pl) 2004-09-30
ZA967200B (en) 1997-03-03
AU6214996A (en) 1997-03-06
DE59608050D1 (de) 2001-12-06
EP0761650A1 (de) 1997-03-12
SI0761650T1 (en) 2002-04-30
TW513407B (en) 2002-12-11
MX9603606A (es) 1997-03-29
ES2165948T3 (es) 2002-04-01
NO963526D0 (no) 1996-08-23
CA2184049A1 (en) 1997-02-27
ATE207895T1 (de) 2001-11-15
UA41978C2 (uk) 2001-10-15
KR100436254B1 (ko) 2005-01-25
BR9603540A (pt) 1998-05-12
CZ287783B6 (en) 2001-02-14
PT761650E (pt) 2002-04-29
HUP9602346A3 (en) 1998-01-28
HU226667B1 (en) 2009-06-29
HU9602346D0 (en) 1996-10-28
JP5023273B2 (ja) 2012-09-12
AU716615B2 (en) 2000-03-02
CN1081631C (zh) 2002-03-27
DK0761650T3 (da) 2002-02-18
EP0761650B1 (de) 2001-10-31
JPH09110830A (ja) 1997-04-28
SK108996A3 (en) 1997-06-04
JP2012246321A (ja) 2012-12-13
CZ243496A3 (en) 1997-03-12
HUP9602346A2 (en) 1997-09-29
JP2009046501A (ja) 2009-03-05
AR004679A1 (es) 1999-03-10
NO307048B1 (no) 2000-01-31
CA2184049C (en) 2007-10-02
SK282437B6 (sk) 2002-02-05
CN1151986A (zh) 1997-06-18
NO963526L (no) 1997-02-27
PL315799A1 (en) 1997-03-03
US6060504A (en) 2000-05-09
DE19531464A1 (de) 1997-02-27
RU2174976C2 (ru) 2001-10-20

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