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KR920009390A - 신규 시클로스포린 - Google Patents

신규 시클로스포린 Download PDF

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Publication number
KR920009390A
KR920009390A KR1019910019402A KR910019402A KR920009390A KR 920009390 A KR920009390 A KR 920009390A KR 1019910019402 A KR1019910019402 A KR 1019910019402A KR 910019402 A KR910019402 A KR 910019402A KR 920009390 A KR920009390 A KR 920009390A
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South Korea
Prior art keywords
meleu
ciclosporin
hydroxy
meval
mebmt
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KR1019910019402A
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KR100203556B1 (ko
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고수영
한스코벨
로젠비르스 브리지트
제바크 디터
페.트라버 레네
벵거 롤랜드
볼링거 피트로
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예안 크레이머, 한스루돌프하우스
산도즈 리미티드
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Priority claimed from GB909023859A external-priority patent/GB9023859D0/en
Priority claimed from GB909023971A external-priority patent/GB9023971D0/en
Priority claimed from GB909023970A external-priority patent/GB9023970D0/en
Priority claimed from GB909023972A external-priority patent/GB9023972D0/en
Priority claimed from GB919116836A external-priority patent/GB9116836D0/en
Application filed by 예안 크레이머, 한스루돌프하우스, 산도즈 리미티드 filed Critical 예안 크레이머, 한스루돌프하우스
Publication of KR920009390A publication Critical patent/KR920009390A/ko
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Publication of KR100203556B1 publication Critical patent/KR100203556B1/ko
Anticipated expiration legal-status Critical
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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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A61K38/13—Cyclosporins
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • C07K7/645—Cyclosporins; Related peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S435/00—Chemistry: molecular biology and microbiology
    • Y10S435/8215—Microorganisms
    • Y10S435/911—Microorganisms using fungi
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S930/00—Peptide or protein sequence
    • Y10S930/01—Peptide or protein sequence
    • Y10S930/27—Cyclic peptide or cyclic protein

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • AIDS & HIV (AREA)
  • Rheumatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Cephalosporin Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

내용 없음

Description

신규 시클로스포린
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 CH2Cl3의 IR 스택트럼 분석 결과를 나타낸 것이고,
제2도는 CDCl3의 양자 NMR 스펙트럼 분석 결과를 나타낸 것이며,
제3도는 CDCl3의 300MHz1H NMP 스펙트럼 분석결과를 나타낸 것이다.

Claims (12)

  1. AIDS 및 AIDS 관련 장애의 치료 및 예방용 약물을 제조하는데 비면역 억제성, 시클로필린 결합성 시클로스포린을 사용하는 방법.
  2. 약제로서 사용하기 위한 하기 일반식(Ⅰ)의 화합물 :
    상기식 중 W는 MeBmt, 디히드로-MeBmt 또는 8'-히드록시-MeBmt이고; X는 α Abu, 발린, Nva 또는 MeOThr 이고; R은 Sar 또는 (D)-MeAla 이고; Y는 MeLeu, γ-히드록시-MeLeu, MeIle, MeVal, MeThr, MeAla, MeIle, 또는 MeaThr 이고; Z는 발린, 류신, MeVal 또는 MeLeu 이며; Q는 MeLeu γ-히드록시-MeLeu 또는 MeAla 인데; 단, Y가 MeLeu 일 경우에는 Z는 MeVal 또는 MeLeu, 또는 W는 8'-히드록시-MeBmt이다.
  3. 제2항에 있어서, 약제로서 사용하기 위한 일반식(Ⅰ')의 화합물 :
    상기식중, W는 MeBmt 또는 디히드로-MeBmt 이고; X'는 αAbu 또는 Nva 이고; Y' 는 γ-히드록시-MeLeu, MeVal, MeThr 또는 MeIle 이며; Z'는 발린 또는 MeVal 이다.
  4. 하기 화합물로 구성된 군중에서 선택된, 약제로 사용하기 위한 화합물 :
    〔디히드로-MeBmt〕1-〔γ-히드록시-MeLeu〕4-Ciclosporin〔MeVal〕4-Ciclosporin〔MeIle〕4-Ciclosporin〔MeThr〕4-Ciclosporin 〔γ-히드록시-MeLeu〕4-Ciclosporin 〔Nva〕2-〔γ-히드록-MeLeu〕4-Ciclosporin 〔γ-히드록시-MeLeu〕4-〔γ-히드록시-MeLeu〕6-Ciclosporin 〔MeVal〕5-Ciclosporin 〔MeOThr〕2-〔(D) MeAla〕3-〔MeVal〕5-Ciclosporin 〔8'-히드록시-MeBmt〕1-Ciclosporin, 및 〔γ-히드록시-MeLeu〕9-Ciclosporin.
  5. AIDS 및 AIDS 관련 장애의 치료 및 예방용 약물을 제조하는데 제2항, 제3항, 또는 제4항의 화합물을 사용하는 방법.
  6. 하기 일반식(Ⅱ)의 화합물 :
    상기식중, W'는 MeBmt또는 디히드로-MeBmt 이고; X는 αAbu, 발린, 트레오닌, Nva 또는 MeOThr 이고; R는 Sar 또는 (D)-MeAla 이고; Y는 MeLeu, γ-히드록시-MeLeu, MeIle, MeVal, MeThr, MeAla, MeaIle 또는 MeaThr 이며; Z는 발린, 류신, MeVal 또는 MeLeu 인데; 단 1) Y가 MeLeu 또는 MeAla 일 경우에 Z는 MeVal 또는 MeLeu 이고; 2) W'가 MeBmt, R은 Sar 이고 Y가 γ-히드록시-MeLeu 일 경우에 Z는 발린이외의 것이다.
  7. 제6항에 있어서, 하기 일반식(Ⅱ')의 화합물 :
    상기식중, W'는 MeBmt 또는 디히드로-MeBmt이고; Y'는 γ-히드록시-MeLeu, MeVal, MeThr, 또는 MeaIle 이고; Z'는 발린 또는 MeVal 인데; 단, W'가 MeBmt일 경우에 Y'는 γ-히드록시-MeLeu 이외의 것이다.
  8. 하기 화합물로 구성된 군중에서 선택된 화합물 :
    〔디히드로-MeBmt〕1-〔γ-히드록시-MeLeu〕4-Ciclosporin, 〔MeVal〕4-Ciclosporin,〔MeIle〕4-Ciclosporin,〔MeThr〕4-Ciclosporin,〔Nva〕2-〔γ-히드록시-MeLeu〕4[γ-하드록시-MeLeu]4-〔γ-히드록시-MeLeu〕6-Ciclosporin, 〔MeVal〕5-Ciclosporin, 및〔MeOThr〕2-〔(D) MeAla〕3-〔MeVal〕5-Ciclosporin.
  9. 영양배지에서 균성 균주 DSM 6627을 배양하는 단계 및 발효액으로 부터 생성물을 분리하는 단계를 포함하는 〔MeIle〕4-Ciclosporin의 제조방법.
  10. 균성균주 DSM 6627의 순수 배양체.
  11. 영양 배지내에서 균성 균주 DSM 6182를 배양하는 단계, 하나 이상의 MeLeu 잔기를 가지는 시클로스포린을 첨가하는 단계, 및 발효액으로 부터 생성물을 분리하는 단계를 포함하는, 하나이상의 γ-히드록시-MeLeu 잔기를 가지는 시클로스포린의 제조방법.
  12. 균성균주 DSM 6182의 순수 배양체.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910019402A 1990-11-02 1991-11-01 신규의 사이클로스포린 Expired - Lifetime KR100203556B1 (ko)

Applications Claiming Priority (15)

Application Number Priority Date Filing Date Title
GB9023859.3 1990-11-02
GB9023859 1990-11-02
GB909023859A GB9023859D0 (en) 1990-11-02 1990-11-02 Chemical products
GB9023971.6 1990-11-05
GB9023972.4 1990-11-05
GB909023971A GB9023971D0 (en) 1990-11-05 1990-11-05 New use of a cyclosporin derivative
GB909023970A GB9023970D0 (en) 1990-11-05 1990-11-05 New use of a cyclosporin derivative
GB9023970 1990-11-05
GB9023972 1990-11-05
GB9023970.8 1990-11-05
GB9023971 1990-11-05
GB909023972A GB9023972D0 (en) 1990-11-05 1990-11-05 New use of a cyclosporin derivative
GB919116836A GB9116836D0 (en) 1991-08-05 1991-08-05 Organic compounds
GB9116836.9 1991-08-05
GB9116836 1991-08-05

Publications (2)

Publication Number Publication Date
KR920009390A true KR920009390A (ko) 1992-06-25
KR100203556B1 KR100203556B1 (ko) 1999-06-15

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KR1019910019402A Expired - Lifetime KR100203556B1 (ko) 1990-11-02 1991-11-01 신규의 사이클로스포린

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US (3) US5767069A (ko)
EP (1) EP0484281B2 (ko)
JP (1) JP2740775B2 (ko)
KR (1) KR100203556B1 (ko)
AT (1) ATE148469T1 (ko)
AU (1) AU649277B2 (ko)
CA (1) CA2054590C (ko)
CY (1) CY2159B1 (ko)
CZ (1) CZ280909B6 (ko)
DE (1) DE69124459T3 (ko)
DK (1) DK0484281T4 (ko)
ES (1) ES2095926T5 (ko)
FI (1) FI111730B (ko)
GR (2) GR3022592T3 (ko)
HK (1) HK1005741A1 (ko)
HU (1) HU212674B (ko)
IE (1) IE913824A1 (ko)
IL (1) IL99912A (ko)
MX (1) MX9101869A (ko)
MY (1) MY134806A (ko)
NZ (1) NZ240421A (ko)
PL (1) PL168609B1 (ko)
PT (1) PT99410B (ko)
SA (1) SA92120344B1 (ko)
SK (1) SK278808B6 (ko)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2128790A1 (en) * 1992-01-28 1993-08-05 Abraham Karpas Use of a compound for the manufacture of a medicament for the treatment of hiv infection
GB9204466D0 (en) * 1992-03-02 1992-04-15 Sandoz Ltd Improvements in or relating to organic compounds
ES2065273B1 (es) * 1993-05-25 1995-09-16 Biogal Gyogyszergyar Procedimiento para la purificacion de ciclosporina a.
US5948693A (en) * 1994-09-01 1999-09-07 Wisconsin Alumni Research Foundation Solid phase synthesis of immunosuppressive agents
US5639852A (en) * 1994-09-01 1997-06-17 Wisconsin Alumni Research Foundation Immunostimulatory agents
US6696413B2 (en) 1995-06-16 2004-02-24 Hexal Ag Pharmaceutical preparation with cyclosporin A
AU722858B2 (en) * 1995-07-17 2000-08-10 Scynexis, Inc. Cyclosporin derivatives having an anti-HIV effect
JP3089350B2 (ja) * 1995-11-20 2000-09-18 ギルフォード ファーマシューティカルズ インコーポレイテッド シクロフィリンロタマーゼ活性の阻害剤
EP0944394A4 (en) * 1996-03-12 2003-05-14 Picower Inst Med Res TREATING HIV INFECTION BY INFLUENCING CYCLOPHILIN RECEPTOR ACTIVITY IN THE HOST CELL
CN1130373C (zh) * 1996-09-13 2003-12-10 诺瓦蒂斯有限公司 [3'－脱氧－3'－氧代－MeBmt]'环孢菌素制备方法
FR2757522B1 (fr) * 1996-12-24 1999-01-29 Rhone Poulenc Rorer Sa Derives de cyclosporine, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2757520B1 (fr) * 1996-12-24 1999-01-29 Rhone Poulenc Rorer Sa Derive de cyclosporine, sa preparation et les compositions pharmaceutiques qui le contiennent
FR2757521B1 (fr) * 1996-12-24 1999-01-29 Rhone Poulenc Rorer Sa Nouveaux derives de cyclosporine, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2762843B1 (fr) * 1997-04-30 1999-12-10 Rhone Poulenc Rorer Sa Nouveaux derives de cyclosporine, leur preparation et les compositions pharmaceutiques qui les contiennent
DE69840586D1 (de) 1997-10-08 2009-04-02 Isotechnika Inc Deuterierte Cyclosporin-analoga und ihre Verwendung als immunmodulierende Agenzien
US20030220234A1 (en) * 1998-11-02 2003-11-27 Selvaraj Naicker Deuterated cyclosporine analogs and their use as immunodulating agents
ZA99981B (en) * 1998-02-17 2000-08-08 Du Pont Pharm Co Oral liquid formulations of benzoxazinones HIV reverse transcriptase inhibitors.
GB9811854D0 (en) * 1998-06-02 1998-07-29 Ciba Geigy Ag Organic compounds
FR2780061B1 (fr) * 1998-06-22 2001-09-07 Rhone Poulenc Rorer Sa Nouveau procede de preparation de derives de cyclosporine
PT1091975E (pt) 1998-07-01 2006-05-31 Debiopharm Sa Nova ciclosporina com um perfil de actividade melhorado
US7026290B1 (en) 1998-12-30 2006-04-11 Dexcel Ltd. Dispersible concentrate for the delivery of cyclosprin
US6521595B1 (en) * 1999-11-19 2003-02-18 Lg Chemical, Ltd. Nonimmunosuppressive [γ-hydroxy-methylleucine4] cyclosporin A, hair growth stimulator and external composition for skin using the same
US7732404B2 (en) 1999-12-30 2010-06-08 Dexcel Ltd Pro-nanodispersion for the delivery of cyclosporin
AU2002245996B8 (en) * 2001-04-20 2005-07-14 Ophthalmopharma Ag Modified cyclosporine which can be used as a pro-drug and use thereof
KR100695611B1 (ko) * 2001-05-17 2007-03-14 주식회사 엘지생활건강 [감마 히드록시 엔-메틸 엘-루신4] 사이클로스포린유도체를 유효성분으로 하는 모발 성장 촉진제
AU2002333098B2 (en) * 2001-10-19 2006-03-16 Isotechnika Pharma Inc. Novel cyclosporin analog microemulsion preconcentrates
SI1436321T1 (sl) * 2001-10-19 2006-12-31 Isotechnika Inc Sinteza analogov ciklosporina
DE20220744U1 (de) * 2001-10-25 2004-05-13 Viromics Gmbh Mittel zur Hemmung von Lentiviren
US7108988B2 (en) * 2001-11-02 2006-09-19 The J. David Gladstone Institutes Methods of identifying agents for inhibiting lentivirus replication
US7538084B2 (en) 2003-03-17 2009-05-26 Amr Technology, Inc. Cyclosporins
GB0320638D0 (en) 2003-09-03 2003-10-01 Novartis Ag Organic compounds
US20050059583A1 (en) * 2003-09-15 2005-03-17 Allergan, Inc. Methods of providing therapeutic effects using cyclosporin components
JP2007532507A (ja) * 2004-04-08 2007-11-15 ノバルティス アクチエンゲゼルシャフト 脳虚血ならびに脳および脊髄傷害の処置のためのサイクロスポリンの使用
RU2007105141A (ru) * 2004-07-13 2008-08-20 Новартис АГ (CH) Применение циклоспоринов для лечения болезни альцгеймера
CA2573207C (en) 2004-07-14 2013-04-16 Novartis Ag Use of a combination of cyclosporin and pegylated interferons for treating hepatitis c (hcv)
KR100597309B1 (ko) 2004-09-17 2006-07-05 주식회사 핸슨바이오텍 세베키아 베니하나를 이용한 [감마 히드록실메틸루신4] 사이클로스포린 a의 제조방법
US7378391B2 (en) * 2004-09-29 2008-05-27 Amr Technology, Inc. Cyclosporin alkyne analogues and their pharmaceutical uses
US7511013B2 (en) 2004-09-29 2009-03-31 Amr Technology, Inc. Cyclosporin analogues and their pharmaceutical uses
US7196161B2 (en) * 2004-10-01 2007-03-27 Scynexis Inc. 3-ether and 3-thioether substituted cyclosporin derivatives for the treatment and prevention of hepatitis C infection
CA2583494C (en) * 2004-10-01 2014-01-21 Scynexis, Inc. 3-ether and 3-thioether substituted cyclosporin derivatives for the treatment and prevention of hepatitis c infection
EP1812037A4 (en) * 2004-10-06 2009-11-11 Amr Technology Inc ALKYNES OF CYCLOSPORINE AND THEIR USEFUL AS PHARMACEUTICAL AGENTS
US7151085B2 (en) * 2004-11-15 2006-12-19 Allergan, Inc. Therapeutic methods using cyclosporine components
US7135455B2 (en) * 2004-11-15 2006-11-14 Allergan, Inc Methods for the therapeutic use of cyclosporine components
KR100777488B1 (ko) 2004-12-15 2007-11-28 주식회사 핸슨바이오텍 세베키아 베니하나 (Sebekia benihana)배양물로부터 감마-히드록실메틸루신4 사이클로스포린 A를 효과적이고 선택적으로 회수하는 방법
NZ555143A (en) 2004-12-23 2009-12-24 Novartis Ag Compositions for HCV treatment
EP1830870A1 (en) * 2004-12-23 2007-09-12 Novartis AG Compounds for flaviviridae treatment
CA2623864C (en) * 2005-09-30 2014-12-16 Scynexis, Inc. Arylalkyl and heteroarylalkyl derivatives of cyclosporine a for the treatment and prevention of viral infection
US7696165B2 (en) 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne analogues for preventing or treating viral-induced disorders
US7696166B2 (en) 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders
EP2007789B1 (en) 2006-04-11 2015-05-20 Novartis AG Spirocyclic HCV/HIV inhibitors and their uses
ES2361635T3 (es) 2006-05-19 2011-06-20 Scynexis, Inc. Ciclosporinas para el tratamiento y prevención de trastornos oculares.
JP2009539292A (ja) * 2006-06-02 2009-11-12 ぺリション、クロード、アニー 活性電子の管理
WO2008069917A2 (en) * 2006-11-20 2008-06-12 Scynexis, Inc. Novel cyclic peptides
US20080255038A1 (en) * 2007-04-11 2008-10-16 Samuel Earl Hopkins Pharmaceutical compositions
US8394763B2 (en) * 2007-09-26 2013-03-12 Oregon Health & Science University Cyclic undecapeptides and derivatives as multiple sclerosis therapies
JP5820722B2 (ja) * 2008-06-06 2015-11-24 スシネキス インク シクロスポリン類似体及びｈｃｖ感染の治療におけるその使用
US20090306033A1 (en) * 2008-06-06 2009-12-10 Keqiang Li Novel cyclic peptides
BRPI0911709A2 (pt) 2008-07-30 2017-06-20 Isotechnika Labs Inc composto, processo para a produção de um composto, composição farmacêutica e método de tratar uma doença mediada a ciclofilina em um mamífero
JP5780969B2 (ja) 2008-12-31 2015-09-16 サイネクシス，インコーポレーテッド シクロスポリンａの誘導体
US11304960B2 (en) 2009-01-08 2022-04-19 Chandrashekar Giliyar Steroidal compositions
US8481483B2 (en) * 2009-02-19 2013-07-09 Enanta Pharmaceuticals, Inc. Cyclosporin analogues
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
US20110182850A1 (en) 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
GB0909754D0 (en) * 2009-06-05 2009-07-22 Magnani Mauro Drug delivery systems
EP2516387B1 (en) 2009-12-21 2018-02-21 Institut National de la Sante et de la Recherche Medicale (INSERM) Inhibitors of cyclophilins for use in the prevention and/or the treatment of viral pathologies or infections
CA2785978A1 (en) 2009-12-30 2011-07-07 Scynexis, Inc. Cyclosporine analogues
US9217015B2 (en) 2010-07-16 2015-12-22 S&T Global Inc. Cyclosporin derivatives for the treatment and prevention of a viral infection
WO2012021796A2 (en) 2010-08-12 2012-02-16 S&T Global, Inc. Novel cyclosporin derivatives for the treatment and prevention of a viral infection
BR112013008510A2 (pt) 2010-10-08 2016-07-05 Novartis Ag vitamina e formulações de inibidores de sulfamida ns3
US20180153904A1 (en) 2010-11-30 2018-06-07 Lipocine Inc. High-strength testosterone undecanoate compositions
US9358241B2 (en) 2010-11-30 2016-06-07 Lipocine Inc. High-strength testosterone undecanoate compositions
US9034858B2 (en) 2010-11-30 2015-05-19 Lipocine Inc. High-strength testosterone undecanoate compositions
US9890198B2 (en) 2010-12-03 2018-02-13 S&T Global Inc. Cyclosporin derivatives and uses thereof
US20120148675A1 (en) 2010-12-10 2012-06-14 Basawaraj Chickmath Testosterone undecanoate compositions
CN107496902B (zh) 2010-12-15 2022-01-18 康卓维尔制药公司 在氨基酸1和3位修改的环孢菌素类似分子
US20120253007A1 (en) * 2011-03-28 2012-10-04 The Government Of The United States Of America, As Represented By The Secretary Of The Navy Synthesis of Cyclosporin H
US20140205566A1 (en) 2012-11-30 2014-07-24 Novartis Ag Cyclic nucleuoside derivatives and uses thereof
WO2016033556A1 (en) 2014-08-28 2016-03-03 Lipocine Inc. BIOAVAILABLE SOLID STATE (17-β)-HYDROXY-4-ANDROSTEN-3-ONE ESTERS
US20170246187A1 (en) 2014-08-28 2017-08-31 Lipocine Inc. (17-ß)-3-OXOANDROST-4-EN-17-YL TRIDECANOATE COMPOSITIONS AND METHODS OF THEIR PREPARATION AND USE
JP2020503269A (ja) 2016-11-28 2020-01-30 リポカイン インコーポレーテッド 経口ウンデカン酸テストステロン療法
WO2020018974A1 (en) 2018-07-20 2020-01-23 Lipocine Inc. Liver disease
CN111449050A (zh) 2019-01-20 2020-07-28 睿诺医疗科技（上海）有限公司 环孢菌素类似物及其用途
JP2023518776A (ja) 2020-03-26 2023-05-08 ファーサイト メディカル テクノロジー （シャンハイ） カンパニー リミテッド シクロスポリン誘導体の調製

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2463138C2 (de) 1973-12-06 1984-07-05 Sandoz-Patent-GmbH, 7850 Lörrach Das Antibiotikum Cyclosporin B (S 7481/F-2), seine Herstellung und Verwendung
US4304855A (en) * 1977-05-05 1981-12-08 The Upjohn Company Allylic methyl-hydroxylated novobiocins
CH667274A5 (de) * 1984-03-23 1988-09-30 Sandoz Ag Cyclosporine, ihre herstellung und diese enthaltende pharmazeutische zusammensetzungen.
EP0194972B1 (en) * 1985-03-11 1992-07-29 Sandoz Ag Novel cyclosporins
US4814323A (en) * 1986-03-25 1989-03-21 Andrieu J M Process for the treatment and the prevention of AIDS and other disorders induced by the LAV/HTLV III virus
EP0283801A3 (en) * 1987-03-27 1990-05-30 Abbott Laboratories Fluorescence polarization assay for cyclosporin a and metabolites and related immunogens and antibodies
US4798823A (en) * 1987-06-03 1989-01-17 Merck & Co., Inc. New cyclosporin analogs with modified "C-9 amino acids"
DE3888357T2 (de) * 1987-06-22 1994-09-15 Merck & Co Inc Cyclosporin-Derivate, die eine modifizierte Aminosäure auf Stellung 8 tragen.
GB8717300D0 (en) * 1987-07-22 1987-08-26 Nat Res Dev Cyclosporins
US4981799A (en) * 1987-08-21 1991-01-01 Takeda Chemical Industries, Ltd. Acylamino acid racemase, production and use thereof
US4914188A (en) † 1987-11-16 1990-04-03 Merck & Co., Inc. Novel 6-position cyclosporin analogs as non-immunosuppressive antagonists of cyclosporin binding to cyclophilin
US5081024A (en) * 1988-09-05 1992-01-14 Nissan Chemical Industries, Ltd. Process for producing optically active amino acids
GB2227244A (en) * 1989-01-19 1990-07-25 Merck & Co Inc Immunosuppressive fluorinated cyclosporin analogs
US5122511A (en) * 1990-02-27 1992-06-16 Merck & Co., Inc. Immunosuppressive cyclosporin analogs with modified amino acids at position-8

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