KR900016220A - 매크로리드 조성물 - Google Patents

매크로리드 조성물 Download PDF

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Publication number
KR900016220A
KR900016220A KR1019890005088A KR890005088A KR900016220A KR 900016220 A KR900016220 A KR 900016220A KR 1019890005088 A KR1019890005088 A KR 1019890005088A KR 890005088 A KR890005088 A KR 890005088A KR 900016220 A KR900016220 A KR 900016220A
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KR
South Korea
Prior art keywords
compound
formula
alkyl
bond
preparing
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KR1019890005088A
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English (en)
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KR970009580B1 (en
Inventor
싱 기다 재스왠트
앤드류 키르스트 허버트
웨인 로버트슨 데이비드
Original Assignee
매리 앤 터커
일라이 릴리 앤드 캄파니
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Publication of KR900016220A publication Critical patent/KR900016220A/ko
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Publication of KR970009580B1 publication Critical patent/KR970009580B1/ko

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    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Nutrition Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

내용 없음.

Description

매크로리드 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (6)

  1. 활성성분으로서의 하기 일반식(I)의 화합물 또는 이의 약제학적 허용가능한 염(R1이 -N(CH3)2인 경우), 및 하나이상의 약제학적 허용가능한 담체를 포함하는 약제학적 조성물.
    상기식에서, R1은 -N(CH3)2또는 -[N(CH3)2R]+X-이고; R은 C1-C6-알킬 C2-C6-알케닐, C2-C6-알케닐, C2-C6-알키닐, 벤질, 또는 플루오로, 클로로, C1-C4-알킬, C1-C4-알콕시, 니트로, C1-C4-알콕시카보닐, -N(C1-C4-알킬)2및 시아노로 부터 선택된 1내지 3개의 치환제로 치환된 벤질이고;R2및 R3각각 H이거나 함께 결합을 형성하며;R4및 R5는 독립적으로 H 또는 C1-C4-아실이거나 카보닐 그룹과 함께 5-원의 사이클릭 탄산염을 형성하고; R6는 H 또는 C1-C4-아실이며; X-는 할로겐화물, 하디드록사이드, 카복실레이트, 설페이트, 포스페이트, 니트레이트, C1-C3-알킬설포네이트 또는 아릴설포네이트 이다.
  2. 제1항에 있어서, 상기 화합물이 R1이 -N(CH3)2이고, R2및 R3가 함께 결합을 형성하고, R4, R5및 R6가 H인 조성물.
  3. R1아 -[N(CH3)2R]+X-인 제1항 또는 2항에서 정의한 상기 일반식(I)의 화합물.
  4. 제3항에 있어서, R이 C1-C6-알킬이고, R2및 R3가 함께 결합을 형성하고, R4, R5및 R6가 H인 화합물.
  5. (A) (i) 하기 일반식(II)의 매크로리드와 알킬화제를 반응시켜 R1이 -[N(CH3)2R]+X-인 상기 일반식(I)의 화합물을 제조하고; 임의로 (ii) 단계 (A) (i)의 화합물을 환원시켜 R1이 -[N(CH3)2R]+X-이고 R2및 R3가 각각 H인 상기 일반식(I)의 화합물을 제조하거나; 또는 (B) (i) 하기 일반식(II)의 매크로리드를 환원시켜 R1이 -N(CH3)2이고, R2및 R3가 각각 H인 상기 일반식(I)의 화합물을 제조하고/ 하거나; 화합물이 염 형태가 아닌 경우화합물을 임의로 염화시키고; 임의로 (ⅱ)단계 (B)(i)화합물과 알킬화제를 반응시켜 R1이 -[N(CH3)2R]+X-이고 R2및 R3가 각각 H인 상기 일반식(I)의 화합물을 제조함을 포함하는 제3항 또는 제4항에서 정의한 일반식(I) 화합물의 제조방법.
  6. 제5항에 다른 제조방법에 따라 각각 제조된 상기 일반식(I)의 화합물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR89005088A 1988-04-18 1989-04-18 Macrolide compositions for treating gastro-intestinal motility disorders KR970009580B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/182,645 US4920102A (en) 1988-04-18 1988-04-18 Method for treating gastrointestinal disorders
US07/182.645 1988-04-18

Publications (2)

Publication Number Publication Date
KR900016220A true KR900016220A (ko) 1990-11-12
KR970009580B1 KR970009580B1 (en) 1997-06-14

Family

ID=22669415

Family Applications (1)

Application Number Title Priority Date Filing Date
KR89005088A KR970009580B1 (en) 1988-04-18 1989-04-18 Macrolide compositions for treating gastro-intestinal motility disorders

Country Status (22)

Country Link
US (1) US4920102A (ko)
EP (1) EP0349100B1 (ko)
JP (1) JPH0825882B2 (ko)
KR (1) KR970009580B1 (ko)
CN (1) CN1023017C (ko)
AR (1) AR244699A1 (ko)
AT (1) ATE139782T1 (ko)
AU (1) AU616746B2 (ko)
CA (1) CA1328257C (ko)
DE (1) DE68926728T2 (ko)
DK (1) DK183589A (ko)
ES (1) ES2088388T3 (ko)
GR (1) GR3020604T3 (ko)
HU (1) HU206365B (ko)
IE (1) IE72969B1 (ko)
IL (1) IL89996A (ko)
MX (1) MX15701A (ko)
NZ (1) NZ228768A (ko)
PH (1) PH26391A (ko)
PT (1) PT90293B (ko)
RU (1) RU2086560C1 (ko)
ZA (1) ZA892801B (ko)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5106961A (en) * 1987-05-26 1992-04-21 Eli Lilly And Company Erythromycin ring-contracted derivatives
US5068221A (en) * 1989-05-09 1991-11-26 Mathias John R Treatment of motility disorders with a gnrh analog
US5434136A (en) * 1990-12-14 1995-07-18 Mathias; John R. Treatment of motility disorders with a GNRH analog
KR100222014B1 (ko) * 1991-04-09 1999-10-01 스티븐 에프. 웨인스톡 거대환식 락탐 유도체, 이의 제조방법 및 이를 포함하는 약제학적 조성물
US5554605A (en) * 1991-04-09 1996-09-10 Abbott Laboratories Macrocyclic lactam prokinetic agents
DE4200145A1 (de) * 1992-01-07 1993-07-08 Kali Chemie Pharma Gmbh 7,10-epoxy-oxacyclododecan-derivate, verfahren und zwischenprodukte zu ihrer herstellung und diese verbindungen enthaltende arzneimittel
ES2115760T3 (es) * 1992-01-21 1998-07-01 Abbott Lab Derivados de 4''-desoxieritromicina.
US5470961A (en) * 1992-03-19 1995-11-28 Takeda Chemical Ind., Ltd. 14 and/or 15-hydroxy 6,9 hemiacetal erythromycin derivatives
FR2697524B1 (fr) * 1992-11-05 1994-12-23 Roussel Uclaf Nouveaux dérivés de l'érythromycine, leur procédé de préparation et leur application comme médicaments.
US5712253A (en) * 1996-06-18 1998-01-27 Abbott Laboratories Macrocyclic 13-membered ring derivatives of erythromycins A and B
DE19644195A1 (de) * 1996-10-24 1998-04-30 Solvay Pharm Gmbh 10,13,15-Trioxatricyclo[9.2.1.1.·9·.·6·]-pentadecanon-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
US6165985A (en) * 1998-02-13 2000-12-26 Solvay Pharmaceuticals Gmbh 11-acetyl-12,13-dioxabicyclo[8.2.1]-tridecenone derivatives, processes for their preparation and pharmaceutical compositions comprising them
DE19805822B4 (de) * 1998-02-13 2009-02-05 Solvay Pharmaceuticals Gmbh 11-Acetyl-12,13-dioxabicyclo[8.2.1]tridecenon-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
US5972898A (en) * 1998-03-27 1999-10-26 Abbott Laboratories 3',3-N-bis-substituted macrolide LHRH antagonists
US5955440A (en) * 1998-03-27 1999-09-21 Abbott Laboratories Macrolide LHRH antagonists
US6020521A (en) * 1998-08-26 2000-02-01 Abbott Laboratories Macrolide LHRH antagonists
US6387885B1 (en) 1998-08-26 2002-05-14 Abbott Laboratories 3′,3′-N-bis-desmethyl-3′-N-cycloalkyl erythromycin derivatives as LHRH antagonists
US6451806B2 (en) 1999-09-29 2002-09-17 Adolor Corporation Methods and compositions involving opioids and antagonists thereof
US6469030B2 (en) 1999-11-29 2002-10-22 Adolor Corporation Methods for the treatment and prevention of ileus
ATE321770T1 (de) * 2000-08-17 2006-04-15 Kitasato Inst Pseudoerythromycin-derivate
GB0123400D0 (en) 2001-09-28 2001-11-21 Novartis Ag Organic compounds
US20040067896A1 (en) * 2002-07-25 2004-04-08 The Kitasato Institute Novel pseudoerythromycin derivatives
EP1559719A4 (en) * 2002-10-29 2006-12-20 Kitasato Inst NEW ANTIMYCOTIC ACTIVITY REINFORCING MAKROLIDE DERIVATIVES
EP1633774B1 (en) 2003-06-18 2010-02-17 Tranzyme Pharma Inc. Macrocyclic antagonists of the motilin receptor
NZ568763A (en) * 2005-12-08 2010-04-30 Pfizer Method for demethylating the 3'-dimethylamino group of erythromycin compounds
CN101528765B (zh) 2006-09-11 2015-04-22 欧塞拉治疗有限公司 用于治疗胃肠动力障碍病症的促胃动素受体的大环拮抗剂
US20080287371A1 (en) * 2007-05-17 2008-11-20 Tranzyme Pharma Inc. Macrocyclic antagonists of the motilin receptor for modulation of the migrating motor complex
FR2995605B1 (fr) * 2012-09-18 2014-09-19 Sanofi Sa Derives de macrolides, leur preparation et leur application therapeutique.

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US4547491A (en) * 1984-07-18 1985-10-15 Merck & Co., Inc. C-8A-Oxo-avermectin and milbemycin derivatives, pharmaceutical compositions and method of use
JPS6187625A (ja) * 1984-10-05 1986-05-06 Satoshi Omura 消化管収縮運動促進剤
DE3689758T2 (de) * 1985-08-31 1994-08-18 Kitasato Inst Erythromycinderivat und Verfahren zu dessen Herstellung.
CA1321581C (en) * 1987-05-26 1993-08-24 Herbert A. Kirst Ring-contracted macrolides

Also Published As

Publication number Publication date
JPH0825882B2 (ja) 1996-03-13
DE68926728T2 (de) 1996-11-28
AU3310789A (en) 1989-10-19
US4920102A (en) 1990-04-24
RU2086560C1 (ru) 1997-08-10
KR970009580B1 (en) 1997-06-14
MX15701A (es) 1993-11-01
ES2088388T3 (es) 1996-08-16
DK183589A (da) 1989-10-19
IL89996A (en) 1994-08-26
EP0349100A2 (en) 1990-01-03
ATE139782T1 (de) 1996-07-15
AR244699A1 (es) 1993-11-30
HU206365B (en) 1992-10-28
IL89996A0 (en) 1989-12-15
CN1023017C (zh) 1993-12-08
DE68926728D1 (de) 1996-08-01
DK183589D0 (da) 1989-04-17
PT90293B (pt) 1994-07-29
IE891224L (en) 1989-10-18
PH26391A (en) 1992-07-02
EP0349100B1 (en) 1996-06-26
ZA892801B (en) 1990-12-28
JPH01311096A (ja) 1989-12-15
CN1037517A (zh) 1989-11-29
AU616746B2 (en) 1991-11-07
PT90293A (pt) 1989-11-10
HUT49625A (en) 1989-10-30
CA1328257C (en) 1994-04-05
NZ228768A (en) 1990-10-26
IE72969B1 (en) 1997-05-07
GR3020604T3 (en) 1996-10-31
EP0349100A3 (en) 1991-11-13

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