KR910004647A - 마크로사이클 화합물 - Google Patents

마크로사이클 화합물 Download PDF

Info

Publication number
KR910004647A
KR910004647A KR1019900012770A KR900012770A KR910004647A KR 910004647 A KR910004647 A KR 910004647A KR 1019900012770 A KR1019900012770 A KR 1019900012770A KR 900012770 A KR900012770 A KR 900012770A KR 910004647 A KR910004647 A KR 910004647A
Authority
KR
South Korea
Prior art keywords
compound
formula
hydroxy
octacos
azatricyclo
Prior art date
Application number
KR1019900012770A
Other languages
English (en)
Inventor
케이쓰 도날드 데이비드
노르만 하던 데이비드
에드워드 쿠퍼 마틴
퍼버 마크
Original Assignee
피존스 피엘시
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
Priority claimed from GB898918929A external-priority patent/GB8918929D0/en
Priority claimed from GB898918886A external-priority patent/GB8918886D0/en
Application filed by 피존스 피엘시 filed Critical 피존스 피엘시
Publication of KR910004647A publication Critical patent/KR910004647A/ko

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/01—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing oxygen
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

Landscapes

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

Abstract

내용 없음.

Description

마크로사이클 화합물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 일반식 I의 화합물.
    식 중, R1은 H 또는 OH이고, R2은 H이며, 또 R1과 R2가 함께 이들이 결합된 탄소 원자들 간에 제2탄소-탄소 결합을 형성할 수 있고, R3는 OH 또는 OCH3이며, X는 0 또는 (H, OH)이고, Y는 0 또는 N-OR4(여기서 R4는 H 또는 C1-6알킬기임)이되, 단, R1이 OH, R2가 H이며 X가 0인 경우, Y는 0일 수 없다.
  2. 제1항에 있어서, 1,2,14-트리히드록시-12-[2-(4-히드록시-3-메톡시시클로헥실)-1-메틸비닐]-23,25-디메톡시-17-에틸-13,19,21,27-테트라메틸-11,28-디옥사-4-아자트리시클로[22,3,1,04,9]옥타코스-18-엔-3,10,16-트리온인 화합물.
  3. 제1항에 있어서, 1,14-디히드록시-12-[2-(4-히드록시-3-메톡시시클로헥실)-1-메틸비닐]-23,25-디메톡시-17-에틸-13,19,21,27-테트라메틸-11,28-디옥사-4-아자트리시클로[22,3,1,04,9]옥타 코스-18-엔-2,3,10,16-테트라인 C16-옥심인 화합물.
  4. 제1항에 있어서, 1-히드록시-12-[2-(4-히드록시-3-메톡시시클로헥실)-1-메틸비닐]-23,25-디메톡시-17-에틸-13,19,21,27-테트라메틸-11,28-디옥사-4-아자트리시클로[22,3,1,04,9]옥타코스-14,18-디엔-2,3,10,16-테트라인 화합물.
  5. 제1항에 있어서, 1-히드록시-12-[2-(4-히드록시-3-메톡시시클로헥실)-1-메틸비닐]-23,25-디메톡시-17-에틸-13,19,21,27-테트라메틸-11,28-디옥사-4-아자트리시클로[22,3,1,04,9]옥타코스-11,28-디엔-2,3,10,16-테트라인 화합물.
  6. 제1항의 일반식(I)의 화합물의 제약학적 용도.
  7. 제1항의 일반식(I)의 화합물 및 제약학적으로 허용되는 보조제, 희석제 또는 담체로 이루어짐을 특징으로 하는 제약 조성물.
  8. 면역억제제로 이용하기 위한 의약 조제에 있어서 제1항의 일반식(I)의 화합물의 용도.
  9. 제1항의 일반식(I)의 화합물을 환자에게 치료학적 유효량으로 투여하는 것으로 이루어진, 면역억제 효과를 얻는 방법.
  10. a) 다른 단서가 없는 한, 제1항의 일반식(I)중의 R1이 OH이고, R2가 H인 화합물을 탈수하여, R1과 R2가 함께 이들이 결합된 탄소 원자들간에 제2탄소-탄소 결합을 나타내는 그의 대응하는 일반식(I)의 화합물을 얻거나, b) 제1항의 일반식 (I)중의 R1과 R2가 함께 이들이 결합된 탄소 원자들간에 제2탄소-탄소 결합을 나타내는 화합물을 환원시켜서 R1및 R2가 각각 수소 원자인 그의 대응하는 일반식(I)의 화합물을 얻거나, c) 식 NH2-OR4인 화합물(여기서, R4는 제1항에 정의된 바와 같음)을 다른 단서가 없는한 제1항의 일반식(I)중의 Y가 0인 화합물과 반응시켜 Y가 N-OR4인 그의 대응하는 일반식(I)의 화합물을 얻거나, 또는 d) 다른 단서가 없는한, 제1항의 일반식(I)중의 X가 0인 화합물을 환원시켜 X가 (H, OH)인 그의 대응하는 일반식(I)의 화합물을 얻는 것으로 이루어진, 제1항의 일반식(I)의 화합물의 제조 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900012770A 1989-08-18 1990-08-18 마크로사이클 화합물 KR910004647A (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB898918929A GB8918929D0 (en) 1989-08-18 1989-08-18 Compound
GB89/18886 1989-08-18
GB898918886A GB8918886D0 (en) 1989-08-18 1989-08-18 Compound
GB89/18929 1989-08-18

Publications (1)

Publication Number Publication Date
KR910004647A true KR910004647A (ko) 1991-03-29

Family

ID=26295787

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019900012770A KR910004647A (ko) 1989-08-18 1990-08-18 마크로사이클 화합물

Country Status (9)

Country Link
US (1) US5179087A (ko)
EP (1) EP0413532A3 (ko)
JP (1) JPH03118385A (ko)
KR (1) KR910004647A (ko)
CA (1) CA2023485A1 (ko)
FI (1) FI904072A0 (ko)
IE (1) IE902994A1 (ko)
NO (1) NO903636L (ko)
PT (1) PT95038A (ko)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5064835A (en) * 1990-03-01 1991-11-12 Merck & Co., Inc. Hydroxymacrolide derivatives having immunosuppressive activity
CA2040551A1 (en) * 1990-04-30 1991-10-31 Mark T. Goulet Deoxymacrolide derivatives having immunosuppressive activity
GB2245561A (en) * 1990-07-05 1992-01-08 Fujisawa Pharmaceutical Co Tricyclo compounds, a process for their production and a pharmaceutical composition containing the same
US5143918A (en) * 1990-10-11 1992-09-01 Merck & Co., Inc. Halomacrolides and derivatives having immunosuppressive activity
US5565560A (en) * 1991-05-13 1996-10-15 Merck & Co., Inc. O-Aryl,O-alkyl,O-alkenyl and O-alkynylmacrolides having immunosuppressive activity
US5162334A (en) * 1991-05-13 1992-11-10 Merck & Co., Inc. Amino O-alkyl, O-alkenyl and O-alkynlmacrolides having immunosuppressive activity
US5250678A (en) 1991-05-13 1993-10-05 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylmacrolides having immunosuppressive activity
US5776943A (en) * 1991-05-14 1998-07-07 American Home Products Corporation Rapamycin metabolites
US5189042A (en) * 1991-08-22 1993-02-23 Merck & Co. Inc. Fluoromacrolides having immunosuppressive activity
US5208241A (en) * 1991-09-09 1993-05-04 Merck & Co., Inc. N-heteroaryl, n-alkylheteroaryl, n-alkenylheteroaryl and n-alkynylheteroarylmacrolides having immunosuppressive activity
GB9203265D0 (en) * 1992-02-15 1992-04-01 Fisons Plc Pharmaceutically active compound
HUT66531A (en) * 1992-05-07 1994-12-28 Sandoz Ag Heteroatoms-containing tricyclic compounds, pharmaceutical prepns contg. them and process for producing them
US5284877A (en) * 1992-06-12 1994-02-08 Merck & Co., Inc. Alkyl and alkenyl macrolides having immunosuppressive activity
US5284840A (en) * 1992-06-12 1994-02-08 Merck & Co., Inc. Alkylidene macrolides having immunosuppressive activity
US5693648A (en) * 1994-09-30 1997-12-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynyl-macrolides having immunosuppressive activity
US7521420B2 (en) 2003-06-18 2009-04-21 Tranzyme Pharma, Inc. Macrocyclic antagonists of the motilin receptor

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4275149A (en) * 1978-11-24 1981-06-23 Syva Company Macromolecular environment control in specific receptor assays
US4894366A (en) * 1984-12-03 1990-01-16 Fujisawa Pharmaceutical Company, Ltd. Tricyclo compounds, a process for their production and a pharmaceutical composition containing the same
DE3853477T2 (de) * 1987-12-09 1995-11-09 Fisons Plc Makrozyklische verbindungen.
EP0349061B1 (en) * 1988-06-29 1995-03-29 Merck & Co. Inc. Immunosuppressant agent
US4981792A (en) * 1988-06-29 1991-01-01 Merck & Co., Inc. Immunosuppressant compound
DE68925080T2 (de) * 1988-08-01 1996-05-15 Fujisawa Pharmaceutical Co FR-901154- und FR-901155-Derivate, Verfahren zu ihrer Herstellung
EP0356399A3 (en) * 1988-08-26 1991-03-20 Sandoz Ag Substituted 4-azatricyclo (22.3.1.04.9) octacos-18-ene derivatives, their preparation and pharmaceutical compositions containing them

Also Published As

Publication number Publication date
EP0413532A2 (en) 1991-02-20
US5179087A (en) 1993-01-12
NO903636L (no) 1991-02-19
IE902994A1 (en) 1991-02-27
JPH03118385A (ja) 1991-05-20
NO903636D0 (no) 1990-08-17
PT95038A (pt) 1991-04-18
FI904072A0 (fi) 1990-08-17
EP0413532A3 (en) 1991-05-15
CA2023485A1 (en) 1991-02-19

Similar Documents

Publication Publication Date Title
KR910004647A (ko) 마크로사이클 화합물
IL94971A0 (en) Aqueous pharmaceutical composition containing a tricyclic compound and processes for the preparation thereof
KR910016336A (ko) 용액 제제
IL100011A0 (en) Suspendible pharmaceutical composition containing a tricyclic compound and processes for the preparation thereof
KR920702219A (ko) 신규 거대환식 화합물 및 신규 치료 방법
CA2050623A1 (en) Ointments containing tricyclic compound
DK0669127T3 (da) Farmaceutisk præparat med forlænget virkning
RU99114776A (ru) Лекарственные композиции
KR920700638A (ko) 가역적 폐색성 기도 질환 치료용 매크롤라이드
NZ507345A (en) Medicinal compositions
GB8925797D0 (en) Compositions
NO950030L (no) Anvendelse av Rifamycin-derivater for fremstilling av et medikament for behandling av toxoplasmose
KR920009400A (ko) 약제학적 조성물
KR910004557A (ko) 2,4,6-치환 페놀 유도체
KR960700055A (ko) 뇌 허혈을 치료하기 위한 마크로라이드의 용도(Use of macrolides for the treatment of cerebral ischemia)
KR870011135A (ko) 시스-6-(4-아세트아닐리도)-8,9-디메톡시-2-메틸-1,2,3,4,4a,10b- 헥사이드로-벤조〔c〕〔1,6〕 나프티리딘으로 구성된 약학적 조성물 및 그것의 용도
WO1993014771A1 (en) Macrocyclic compounds in the prophylactic treatment of aids
KR890001528A (ko) 성인 t-세포 백혈병/임파종의 억제를 위한 아바론, 아바롤 및 그 유도체의 용도

Legal Events

Date Code Title Description
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid