[go: up one dir, main page]

KR920002608A - 라파마이신 유도체 - Google Patents

라파마이신 유도체 Download PDF

Info

Publication number
KR920002608A
KR920002608A KR1019910012015A KR910012015A KR920002608A KR 920002608 A KR920002608 A KR 920002608A KR 1019910012015 A KR1019910012015 A KR 1019910012015A KR 910012015 A KR910012015 A KR 910012015A KR 920002608 A KR920002608 A KR 920002608A
Authority
KR
South Korea
Prior art keywords
carbon atoms
pharmaceutically acceptable
hydrogen
rapamycin
acceptable salt
Prior art date
Application number
KR1019910012015A
Other languages
English (en)
Inventor
유진 커필드 크레이그
아르투로 페일리 아메데오
죤 스테판 로버트
Original Assignee
에곤 이. 버그
아메리칸 홈 프로덕츠 코포레이션
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 US07/667,684 external-priority patent/US5120726A/en
Application filed by 에곤 이. 버그, 아메리칸 홈 프로덕츠 코포레이션 filed Critical 에곤 이. 버그
Publication of KR920002608A publication Critical patent/KR920002608A/ko

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

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

Abstract

내용 없음

Description

라파마이신 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 일반식(Ⅰ)의 화합물 및 이의 약학적으로 허용가능한 염.
    상기식에서, R은 NR1R2또는 -OR3이고, R1은 수소, 탄소수 1내지 6의 알킬 또는 탄소수 7내지 10의 아르알킬이며, R2는 수소, 탄소수 1내지 6의 알킬, 탄소수 3내지 10의 사이클로알킬,탄소수 7내지 10의 아르알킬, -COR4, -CO2R4, -SO2R4, -CONR5R6, -CSNR5R6, -COCONR5R6또는 Ar이고, R3는 수소, 탄소수 1내지 6의 알킬 또는 -CH2Ar이며, R4는 탄소수 1내지 6의 알킬, 탄소수 7내지 10의 아르알킬 또는 Ar이고, R5및 R6는 각각,독립적으로, 수소, 탄소수, 1내지 6의 알킬, 탄소수 3내지 10의 사이클로알킬, 알릴, 탄소수 7내지 10의 아르알킬 또는 Ar이며,
    R7,R8,R9는 각각 독립적으로, 수소, 탄소수 1내지 6의 알킬, 탄소수 1내지 6의 알콕시, 하이드록시, 시아노, 할로, 니트로, 탄소수 2내지 7의 카브알콕시, 트리플루오로메틸, 트리플루오로메톡시, 아미노 또는 카복실산이며, X는 CH 또는 N이고 Y는 NH, O 또는 S이다.
  2. 제1항에 있어서, R이 -NR1R2이고 R1이 수소인 화합물 및 이의 약학적으로 허용가능한 염.
  3. 제1항에 있어서, R이 -NR1R2이고 R1이 수소이며, R2가 -CONR5R6인 화합물 및 이의 약학적으로 허용가능한 염.
  4. 제1항에 있어서, R이 -NR1R2이고 R1이 수소이며, R2가 -CONR4인 화합물 및 이의 약학적으로 허용가능한 염.
  5. 제1항에 있어서, R이 -NR1R2이고 R1이 수소이며, R2가 Ar인 화합물 및 이의 약학적으로 허용가능한 염.
  6. 제1항에 있어서, R이 -OR3이고 R3가 탄소수 1내지 6의 알킬인 화합물 및 이의 약학적으로 허용가능한 염.
  7. 제1항에 있어서, R이 -OR3이고 R3가 -CH2Ar이며
    인 화합물 및 이의 약학적으로 허용가능한 염.
  8. 제1항에 있어서, 라파마이신 27-(메틸카보닐하이드라존) 및 이의 약학적으로 허용가능한 염.
  9. 제1항에 있어서, 라파마이신 27-(4-페닐세미카브아존) 및 이의 약학적으로 허용가능한 염.
  10. 제1항에 있어서, 라파마이신 27-(2-피리디닐하이드리존) 및 이의 약학적으로 허용가능한 염.
  11. 제1항에 있어서, 라파마이신 27-세미키보아존 및 이의 약학적으로 허용가능한 염.
  12. 제1항에 있어서, 라파마이신 27-하이드라존 및 이의 약학적으로 허용가능한 염.
  13. 제1항에 있어서, 라파마이신 27-옥심 및 이의 약학적으로 허용가능한 염.
  14. 제1항에 있어서, 라파마이신-O-벤질-27-옥심 및 이의 약학적으로 허용가능한 염.
  15. 제1항에 있어서, 라파마이신-O-메틸-27-옥심 및 이의 약학적으로 허용가능한 염.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910012015A 1990-07-16 1991-07-15 라파마이신 유도체 KR920002608A (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US55272090A 1990-07-16 1990-07-16
US07/552,720 1990-07-16
US07/667,684 1991-03-08
US07/667,684 US5120726A (en) 1991-03-08 1991-03-08 Rapamycin hydrazones

Publications (1)

Publication Number Publication Date
KR920002608A true KR920002608A (ko) 1992-02-28

Family

ID=27070117

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019910012015A KR920002608A (ko) 1990-07-16 1991-07-15 라파마이신 유도체

Country Status (8)

Country Link
EP (1) EP0467606A1 (ko)
JP (1) JPH04230389A (ko)
KR (1) KR920002608A (ko)
AU (1) AU641785B2 (ko)
GB (1) GB2247017B (ko)
HU (1) HUT58745A (ko)
IE (1) IE912468A1 (ko)
PT (1) PT98303A (ko)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT98990A (pt) * 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5078999A (en) * 1991-02-22 1992-01-07 American Home Products Corporation Method of treating systemic lupus erythematosus
US5118677A (en) * 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
MX9304868A (es) * 1992-08-13 1994-05-31 American Home Prod 27-hidroxirapamicina, derivados de la misma y composicion farmaceutica que la contiene.
US7279561B1 (en) 1993-04-23 2007-10-09 Wyeth Anti-rapamycin monoclonal antibodies
WO1995014023A1 (en) * 1993-11-19 1995-05-26 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
US5527907A (en) * 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
US5849730A (en) * 1994-08-31 1998-12-15 Pfizer Inc. Process for preparing demethylrapamycins
TW427904B (en) * 1995-12-07 2001-04-01 American Home Prod Neuroprotective agents
AU735648B2 (en) 1996-07-12 2001-07-12 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
US6890546B2 (en) 1998-09-24 2005-05-10 Abbott Laboratories Medical devices containing rapamycin analogs
US7399480B2 (en) 1997-09-26 2008-07-15 Abbott Laboratories Methods of administering tetrazole-containing rapamycin analogs with other therapeutic substances using medical devices
US6015815A (en) 1997-09-26 2000-01-18 Abbott Laboratories Tetrazole-containing rapamycin analogs with shortened half-lives
US20030129215A1 (en) 1998-09-24 2003-07-10 T-Ram, Inc. Medical devices containing rapamycin analogs
US8257726B2 (en) 1997-09-26 2012-09-04 Abbott Laboratories Compositions, systems, kits, and methods of administering rapamycin analogs with paclitaxel using medical devices
US8057816B2 (en) 1997-09-26 2011-11-15 Abbott Laboratories Compositions and methods of administering paclitaxel with other drugs using medical devices
US7357942B2 (en) 1997-09-26 2008-04-15 Abbott Laboratories Compositions, systems, and kits for administering zotarolimus and paclitaxel to blood vessel lumens
US7378105B2 (en) 1997-09-26 2008-05-27 Abbott Laboratories Drug delivery systems, kits, and methods for administering zotarolimus and paclitaxel to blood vessel lumens
US8257725B2 (en) 1997-09-26 2012-09-04 Abbott Laboratories Delivery of highly lipophilic agents via medical devices
US8394398B2 (en) 1997-09-26 2013-03-12 Abbott Laboratories Methods of administering rapamycin analogs with anti-inflammatories using medical devices
US8257724B2 (en) 1998-09-24 2012-09-04 Abbott Laboratories Delivery of highly lipophilic agents via medical devices
US7455853B2 (en) 1998-09-24 2008-11-25 Abbott Cardiovascular Systems Inc. Medical devices containing rapamycin analogs
US7960405B2 (en) 1998-09-24 2011-06-14 Abbott Laboratories Compounds and methods for treatment and prevention of diseases
GB9826882D0 (en) 1998-12-07 1999-01-27 Novartis Ag Organic compounds
KR101012605B1 (ko) 2002-09-06 2011-02-10 아보트 러보러터리즈 수화 억제제를 포함하는 의료용 장치
KR20060085246A (ko) 2003-09-18 2006-07-26 마커사이트, 인코포레이티드 경공막 전달
JP4540704B2 (ja) * 2004-03-10 2010-09-08 セラディン インコーポレイテッド エベロリムスの測定方法および測定キット
ATE534424T1 (de) 2004-03-19 2011-12-15 Abbott Lab Mehrfache arzneiabgabe aus einem ballon und eine prothese
US8431145B2 (en) 2004-03-19 2013-04-30 Abbott Laboratories Multiple drug delivery from a balloon and a prosthesis
US8021849B2 (en) 2004-11-05 2011-09-20 Siemens Healthcare Diagnostics Inc. Methods and kits for the determination of sirolimus in a sample
GB2438544A (en) 2005-02-09 2007-11-28 Cooper Internat Corp Liquid formulations for treatment of diseases or conditions
US8663639B2 (en) 2005-02-09 2014-03-04 Santen Pharmaceutical Co., Ltd. Formulations for treating ocular diseases and conditions
EP1868663B1 (en) 2005-03-23 2011-11-16 Abbott Laboratories Delivery of highly lipophilic agents via medical devices
EP1877004A4 (en) 2005-03-23 2012-01-25 Abbott Lab COMPOSITIONS AND METHODS FOR THE ADMINISTRATION OF RAPAMYCIN ANALOGUES WITH MEDICAL DEVICES FOR LONG-TERM EFFECT
US7189582B2 (en) 2005-04-27 2007-03-13 Dade Behring Inc. Compositions and methods for detection of sirolimus
US7700614B2 (en) 2005-12-14 2010-04-20 Abbott Laboratories One pot synthesis of tetrazole derivatives of rapamycin
EP2001438A2 (en) 2006-02-09 2008-12-17 Macusight, Inc. Stable formulations, and methods of their preparation and use
US7622477B2 (en) 2006-02-28 2009-11-24 Cordis Corporation Isomers and 42-epimers of rapamycin alkyl ether analogs, methods of making and using the same
US7678901B2 (en) 2006-02-28 2010-03-16 Wyeth Rapamycin analogs containing an antioxidant moiety
PL2001466T3 (pl) 2006-03-23 2016-06-30 Santen Pharmaceutical Co Ltd Rapamycyna w małej dawce do leczenia chorób związanych z przepuszczalnością naczyń
US7883855B2 (en) 2006-07-21 2011-02-08 Abbott Laboratories Immunosuppressant drug extraction reagent for immunoassays
CA2709272C (en) 2007-12-19 2015-03-10 Abbott Laboratories Immunosuppressant drug extraction reagent for immunoassays
US8951595B2 (en) 2009-12-11 2015-02-10 Abbott Cardiovascular Systems Inc. Coatings with tunable molecular architecture for drug-coated balloon
US8480620B2 (en) 2009-12-11 2013-07-09 Abbott Cardiovascular Systems Inc. Coatings with tunable solubility profile for drug-coated balloon
EP3556774B1 (en) 2011-03-11 2024-01-03 Beth Israel Deaconess Medical Center Inc. Anti-cd40 antibodies and uses thereof
EP2589383A1 (en) 2011-11-06 2013-05-08 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Berlin FKBP subtype-specific rapamycin analogue for use in treatment of diseases
EP3307322B1 (en) 2015-09-04 2021-02-17 Primatope Therapeutics Inc. Humanized anti-cd40 antibodies and uses thereof
US10682340B2 (en) 2016-06-30 2020-06-16 Durect Corporation Depot formulations
US10668011B2 (en) 2016-06-30 2020-06-02 Durect Corporation Depot formulations
EA201990127A1 (ru) 2016-12-30 2020-08-18 Дьюрект Корпорейшн Депо-препарат
IL303660A (en) * 2017-05-02 2023-08-01 Revolution Medicines Inc Rapamycin analogs as mtor inhibitors
SG11202010560QA (en) 2018-05-01 2020-11-27 Revolution Medicines Inc C26-linked rapamycin analogs as mtor inhibitors
PE20212112A1 (es) 2018-05-01 2021-11-04 Revolution Medicines Inc Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor
EP4531859A1 (en) 2022-05-25 2025-04-09 Revolution Medicines, Inc. Methods of treating cancer with an mtor inhibitor

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4316885A (en) * 1980-08-25 1982-02-23 Ayerst, Mckenna And Harrison, Inc. Acyl derivatives of rapamycin
US4650803A (en) * 1985-12-06 1987-03-17 University Of Kansas Prodrugs of rapamycin
US5100899A (en) * 1989-06-06 1992-03-31 Roy Calne Methods of inhibiting transplant rejection in mammals using rapamycin and derivatives and prodrugs thereof

Also Published As

Publication number Publication date
GB2247017B (en) 1994-04-20
EP0467606A1 (en) 1992-01-22
IE912468A1 (en) 1992-01-29
GB9115205D0 (en) 1991-08-28
GB2247017A (en) 1992-02-19
JPH04230389A (ja) 1992-08-19
HUT58745A (en) 1992-03-30
AU8045091A (en) 1992-01-16
AU641785B2 (en) 1993-09-30
HU912356D0 (en) 1991-12-30
PT98303A (pt) 1992-05-29

Similar Documents

Publication Publication Date Title
KR920002608A (ko) 라파마이신 유도체
ES8300112A1 (es) Un procedimiento para preparar compuestos de cefem .
AR241528A1 (es) Un procedimiento para la preparacion de n-(3- o 4-((alquilamino)alquil)-fenil)alcansulfonamidas y sus sales.
ES414279A1 (es) Procedimiento para la preparacion de 1,4-benzodiazepinas.
NO903438D0 (no) Fremgangsmaate for fremstilling av tiazolderivater.
PT976748E (pt) Derivados de pirrolidina com actividade inibidora de fosfolipase a2
ATE68473T1 (de) 1-phenyl-3-naphthalenyloxy-propanamine.
KR930703303A (ko) 1, 4-벤조티아제핀 유도체
MY123083A (en) Acyclic nucleoside derivatives
KR960007592A (ko) 신규한 피롤로카바졸
KR930021628A (ko) 심장 혈관계 활성을 갖는 벤족사지논 및 벤조티아지논 유도체
KR900014388A (ko) 에세롤린의 카보네이트 유도체, 이의 제조방법 및 약제로서의 용도
KR890005088A (ko) 4- 아미노피리딘 유도체 및 그의 산 부가염
EP0357089A3 (en) Novel cephem compound as an antimicrobial agent and its preparation
KR930021641A (ko) 7-옥소-7H-피리도[1,2,3-d,e][1,4]벤족사진-6-카르복실산 및 에스테르
IE831923L (en) Thieno-thiazole derivatives
KR890008148A (ko) 새로운 세파로스포린 화합물 및 항균제
KR850000455A (ko) 세팔로스포린 에스테르 유도체의 제조방법
DE3788149D1 (de) Prostazyklin-(PGI2)-Analoge.
ES2092470T3 (es) Derivados de pirrolidina.
ES8401761A1 (es) Un procedimiento para la preparacion de derivados de 1-(3,4,5-trimetoxicinamoil)-4-aminocarboniletil-piperazina sustituidos.
ES8503199A1 (es) Procedimiento para la preparacion de nuevos agentes antihelminticos derivados de imidiazoles.
DK0417746T3 (da) N-Azabicyclo(3.3.0)octanamider af aromatiske syrer
ATE105565T1 (de) Pradimicinderivate.
IE44999L (en) Hydrazinopyridazine derivatives.

Legal Events

Date Code Title Description
PA0109 Patent application

Patent event code: PA01091R01D

Comment text: Patent Application

Patent event date: 19910715

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid