KR102305423B1 - 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자 - Google Patents

아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자 Download PDF

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KR102305423B1
KR102305423B1 KR1020207007384A KR20207007384A KR102305423B1 KR 102305423 B1 KR102305423 B1 KR 102305423B1 KR 1020207007384 A KR1020207007384 A KR 1020207007384A KR 20207007384 A KR20207007384 A KR 20207007384A KR 102305423 B1 KR102305423 B1 KR 102305423B1
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group
disease
saturated
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KR20200029639A (ko
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알렉산더 헤그먼스
브루스 더블유. 펜스크
댄 제이. 트리패니어
마크 디. 아벨
신 스기야마
대런 알. 유레
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콘트라빌 파마슈티컬스, 인코퍼레이티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
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    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
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KR1020207007384A 2010-12-15 2011-12-14 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자 Active KR102305423B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US42357610P 2010-12-15 2010-12-15
US61/423,576 2010-12-15
KR1020187037529A KR20190002731A (ko) 2010-12-15 2011-12-14 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자
PCT/CA2011/050773 WO2012079172A1 (en) 2010-12-15 2011-12-14 Cyclosporine analogue molecules modified at amino acid 1 and 3

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KR1020187037529A Division KR20190002731A (ko) 2010-12-15 2011-12-14 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자

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KR20200029639A KR20200029639A (ko) 2020-03-18
KR102305423B1 true KR102305423B1 (ko) 2021-09-27

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KR1020207007384A Active KR102305423B1 (ko) 2010-12-15 2011-12-14 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자
KR1020187037529A Ceased KR20190002731A (ko) 2010-12-15 2011-12-14 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자
KR1020137016342A Active KR102011339B1 (ko) 2010-12-15 2011-12-14 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자

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KR1020187037529A Ceased KR20190002731A (ko) 2010-12-15 2011-12-14 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자
KR1020137016342A Active KR102011339B1 (ko) 2010-12-15 2011-12-14 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자

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US (2) US9200038B2 (enExample)
EP (2) EP2651965B1 (enExample)
JP (3) JP6144627B2 (enExample)
KR (3) KR102305423B1 (enExample)
CN (2) CN103443119B (enExample)
AU (1) AU2011342284C1 (enExample)
BR (1) BR112013014890B1 (enExample)
CA (1) CA2821009C (enExample)
DK (1) DK2651965T3 (enExample)
ES (1) ES2705750T3 (enExample)
HR (1) HRP20190096T1 (enExample)
HU (1) HUE042490T2 (enExample)
IL (1) IL226792A (enExample)
LT (1) LT2651965T (enExample)
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PT (1) PT2651965T (enExample)
RU (1) RU2630690C9 (enExample)
SG (2) SG191069A1 (enExample)
SI (1) SI2651965T1 (enExample)
TR (1) TR201900128T4 (enExample)
WO (1) WO2012079172A1 (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9890198B2 (en) 2010-12-03 2018-02-13 S&T Global Inc. Cyclosporin derivatives and uses thereof
AU2011342284C1 (en) * 2010-12-15 2017-07-13 Contravir Pharmaceuticals, Inc. Cyclosporine analogue molecules modified at amino acid 1 and 3
WO2013181339A2 (en) * 2012-06-01 2013-12-05 Allergan, Inc. Cyclosporin a analogs
US20160002299A1 (en) * 2013-03-01 2016-01-07 Ucl Business Plc Non-immunosuppressive cyclosporin derivatives as antiviral agents
HK1223843A1 (zh) * 2013-08-26 2017-08-11 Enanta Pharmaceuticals, Inc. 用於預防或治療丙型肝炎的環孢菌素類似物
TW201639873A (zh) 2015-01-08 2016-11-16 歐樂根公司 Mebmt側鏈已環化之環孢菌素衍生物
AU2017267560B2 (en) 2016-05-17 2022-03-24 S&T Global Inc. Novel cyclosporin derivatives and uses thereof
CA3045944A1 (en) 2016-12-07 2018-06-14 Progenity, Inc. Gastrointestinal tract detection methods, devices and systems
WO2018106928A1 (en) 2016-12-08 2018-06-14 Contravir Pharmaceuticals, Inc. Treatment and prevention of hbv diseases by cyclosporine analogue molecules modified at amino acides 1 and 3
US11523772B2 (en) 2016-12-14 2022-12-13 Biora Therapeutics, Inc. Treatment of a disease of the gastrointestinal tract with an immunosuppressant
US20180296588A1 (en) 2017-04-14 2018-10-18 Contravir Pharmaceuticals, Inc. Combination therapy for treating viral infections
WO2018193114A1 (en) 2017-04-20 2018-10-25 Novintum Biotechnology Gmbh Triphenylphosphonium-tethered tetracycyclines for use in treating cancer
US20230041197A1 (en) 2018-06-20 2023-02-09 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with an immunomodulator
CN121554542A (zh) 2018-08-22 2026-02-24 贝凯恩生物医疗技术有限公司 环孢菌素组合物及使用方法
US12594275B2 (en) 2019-02-07 2026-04-07 The Regents Of The University Of California Immunophilin binding agents and uses thereof
TW202143994A (zh) 2020-02-19 2021-12-01 美商希皮恩製藥公司 環孢素類似物於治療纖維化之用途
CN115484961A (zh) * 2020-02-25 2022-12-16 海必恩制药公司 环孢菌素类似物用于治疗癌症的用途
CA3172535A1 (en) 2020-03-26 2021-09-30 Ching-Pong Mak Cyclophilin inhibitors and uses thereof
WO2021190603A1 (en) * 2020-03-26 2021-09-30 Farsight Medical Technology (Shanghai) Co., Ltd. Cyclophilin inhibitors and uses thereof
EP4251189A1 (en) * 2020-11-29 2023-10-04 Hepion Pharmaceuticals, Inc. Use of cyclosporine analogues as antithrombotic agents
CN113173974B (zh) 2021-03-18 2024-09-06 北京大学深圳研究生院 环孢素衍生物的合成方法
CN115677533B (zh) * 2021-07-30 2023-12-05 沈阳化工研究院有限公司 一种4-庚基苯甲腈的制备方法
IT202300001116A1 (it) * 2023-01-25 2024-07-25 Indena Spa Processo per la preparazione di un intermedio utile per la sintesi di voclosporina
WO2024245384A1 (en) * 2023-06-02 2024-12-05 Farsight Medical Technology (Shanghai) Co., Ltd. Cyclophilin inhibitors and uses thereof
AU2024285817A1 (en) * 2023-06-08 2026-01-08 Hepion Pharmaceuticals, Inc. Solid state forms of rencofilstat

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030212249A1 (en) 2001-10-19 2003-11-13 Isotechnika, Inc. Synthesis of cyclosporin analogs
US20070232531A1 (en) * 2006-03-28 2007-10-04 Amr Technology, Inc. Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders
WO2010012073A1 (en) 2008-07-30 2010-02-04 Isotechnika Labs Inc. Nonimmunosuppressive cyclosporine analogue molecules

Family Cites Families (97)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH614931A5 (enExample) 1975-11-04 1979-12-28 Sandoz Ag
US4210581A (en) 1975-11-04 1980-07-01 Sandoz Ltd. Organic compounds
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4160452A (en) 1977-04-07 1979-07-10 Alza Corporation Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina
DE2819094A1 (de) 1977-05-10 1978-11-23 Sandoz Ag Cyclosporin-derivate, ihre verwendung und herstellung
SE448386B (sv) 1978-10-18 1987-02-16 Sandoz Ag Nya cyklosporinderivat, forfarande for framstellning av dem samt farmaceutisk komposition innehallande dem
US4396542A (en) 1980-02-14 1983-08-02 Sandoz Ltd. Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
EP0098457B1 (en) 1980-02-14 1987-08-05 Sandoz Ag (1s,2r,3r)- and (1r,2s,3s)-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes useful in the total synthesis of cyclosporins and processes for their production
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
DE3260468D1 (en) 1981-01-09 1984-09-06 Sandoz Ag Novel cyclosporins
CH667274A5 (de) 1984-03-23 1988-09-30 Sandoz Ag Cyclosporine, ihre herstellung und diese enthaltende pharmazeutische zusammensetzungen.
JPS6182786A (ja) 1984-09-28 1986-04-26 ブラザー工業株式会社 ミシン
EP0194972B1 (en) 1985-03-11 1992-07-29 Sandoz Ag Novel cyclosporins
US4764503A (en) 1986-11-19 1988-08-16 Sandoz Ltd. Novel cyclosporins
US4798823A (en) 1987-06-03 1989-01-17 Merck & Co., Inc. New cyclosporin analogs with modified "C-9 amino acids"
US4885276A (en) 1987-06-03 1989-12-05 Merck & Co., Inc. Cyclosporin analogs with modified "C-9 amino acids"
ATE95193T1 (de) 1987-06-17 1993-10-15 Sandoz Ag Cyclosporine und deren benutzung als arzneimittel.
ATE110784T1 (de) 1987-06-19 1994-09-15 Sandoz Ag Zyklische peptolide.
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
US5227467A (en) 1987-08-03 1993-07-13 Merck & Co., Inc. Immunosuppressive fluorinated cyclosporin analogs
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
US5236899A (en) 1987-11-16 1993-08-17 Merck & Co., Inc. 6-position cyclosporin a analogs as modifiers of cytotoxic drug resistance
US5604092A (en) 1988-12-05 1997-02-18 The Trustees Of Columbia University In The City Of New York Method for the detection of HIV-1 using a cyclosporine-specific monoclonal antibody that reacts with the P24 Gag protein
WO1990006763A1 (en) 1988-12-05 1990-06-28 The Trustees Of Columbia University In The City Of New York Novel derivatives of cyclosporine a, antibodies directed thereto and uses thereof
US5284826A (en) 1989-07-24 1994-02-08 Sandoz Ltd. 0-hydroxyethyl and acyloxyethyl derivatives of [ser]8 cyclosporins
US5214130A (en) 1990-02-27 1993-05-25 Merck & Co., Inc. Synthesis of novel immunosuppressive cyclosporin analogs with modified amino acids at position-8
US5122511A (en) 1990-02-27 1992-06-16 Merck & Co., Inc. Immunosuppressive cyclosporin analogs with modified amino acids at position-8
FI111730B (fi) 1990-11-02 2003-09-15 Novartis Ag Menetelmä ei-immunosuppressiivisen syklosporiinin valmistamiseksi
GB9204466D0 (en) 1992-03-02 1992-04-15 Sandoz Ltd Improvements in or relating to organic compounds
WO1997011092A1 (en) 1994-04-07 1997-03-27 Nippon Shinyaku Co., Ltd. Cyclosporin phosphate derivatives and medicinal composition
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
JPH08148407A (ja) 1994-11-21 1996-06-07 Nikon Corp 照明光学装置
SE520730C2 (sv) 1995-01-20 2003-08-19 Eskil Elmer Behandling av hjärnischemi och hjärnskador med ett neuroprotektivt läkemedel
KR100241643B1 (ko) 1995-06-06 2000-03-02 디. 제이. 우드 당뇨병치료제인 치환된 N-(인돌-2-카르보닐)-β-알라님아미드 및 그의 유도체
CN1141317C (zh) 1995-07-17 2004-03-10 碳化学公司 有抗人体免疫缺损病毒作用的环孢菌素衍生物
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
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
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
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
US6270957B1 (en) 1997-08-26 2001-08-07 Wisconsin Alumni Research Foundation Non-Imuunosuppressive cyclosporins and their use in the prevention and treatment of HIV infection
WO1999010374A1 (en) 1997-08-26 1999-03-04 Wisconsin Alumni Research Foundation Cyclosporin a conjugates and uses therefor
US20030220234A1 (en) 1998-11-02 2003-11-27 Selvaraj Naicker Deuterated cyclosporine analogs and their use as immunodulating agents
DE69832984T2 (de) 1997-10-08 2006-09-21 Isotechnika, Inc., Edmonton DEUTERIERtE und undeuterierte CYCLOSPORIN-ANALOGA UND IHRE VERWENDUNG ALS IMMUNMODULIERENDE AGENtIEN
US5990274A (en) 1997-11-25 1999-11-23 Dade Behring Inc. Cyclosporine derivatives and uses thereof
FR2772768B1 (fr) 1997-12-19 2000-01-14 Rhone Poulenc Rorer Sa Nouveau procede de preparation de derives de cyclosporine
ATE254630T1 (de) 1998-06-12 2003-12-15 Chem Ag C Cyclosporine
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
PT1150999E (pt) 1999-02-05 2006-10-31 Debiopharm Sa Derivados da ciclosporina em que a sequencia peptidica contem pelo menos um aminoacido nao natural do tipo pseudo-prolina e metodo para preparacao dos mesmos
CN1391458A (zh) 1999-11-19 2003-01-15 Lg生活健康株式会社 非免疫抑制性环孢菌素衍生物在促进毛发生长中的应用
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
KR20020039528A (ko) 2000-11-22 2002-05-27 조명재 사이클로스포린 7- 티오아미드 유도체를 유효성분으로하는 모발성장촉진제
KR100360716B1 (ko) 2000-11-22 2002-11-13 주식회사 엘지생활건강 사이클로스포린 에이 7- 티오아미드 유도체를유효성분으로 하는 모발성장촉진제
KR100681670B1 (ko) 2001-02-14 2007-02-09 주식회사 엘지생활건강 [감마 히드록시 엔- 메틸-엘-루신9]사이클로스포린 에이를유효성분으로 하는 모발 성장 촉진제
US6784156B2 (en) 2001-03-05 2004-08-31 Enanta Pharmaceuticals, Inc. Cyclosporins for the treatment of respiratory diseases
JP4588979B2 (ja) 2001-04-20 2010-12-01 オプタルモファーマ アクチェンゲゼルシャフト プロドラッグとして使用されうる修飾型シクロスポリン及びその使用
KR100465012B1 (ko) 2001-05-11 2005-01-13 주식회사 엘지생활건강 모발 성장 효과를 갖는 사이클로스포린 3 위치 유도체를유효성분으로 하는 모발 성장 촉진제
KR100695611B1 (ko) 2001-05-17 2007-03-14 주식회사 엘지생활건강 [감마 히드록시 엔-메틸 엘-루신4] 사이클로스포린유도체를 유효성분으로 하는 모발 성장 촉진제
US6809077B2 (en) 2001-10-12 2004-10-26 Enanta Pharmaceuticals, Inc. Cyclosporin analogs for the treatment of autoimmune diseases
US20030087813A1 (en) 2001-10-12 2003-05-08 Or Yat Sun Cyclosporin analogs for the treatment of lung diseases
EP1435910B9 (en) 2001-10-19 2010-02-03 Isotechnika Inc. Novel cyclosporin analog microemulsion preconcentrates
DK1436322T3 (da) 2001-10-19 2008-11-03 Isotechnika Inc Blandinger af cyclosporinanaloger og deres anvendelse som immunmodulerende midler
US6987090B2 (en) 2002-05-09 2006-01-17 Lg Household & Health Care Ltd. Use of 3-position cyclosporin derivatives for hair growth
KR100641295B1 (ko) * 2002-11-11 2006-10-31 김성수 사이클로필린의 항산화제로서의 용도 및 사이클로필린의과발현에 의해 세포이식에서 사이클로스포린 a에 의해유발되는 세포독성의 방지
US20040110666A1 (en) 2002-12-04 2004-06-10 Or Yat Sun Cyclosporins for the treatment of immune disorders
US7012065B2 (en) 2003-02-07 2006-03-14 Enanta Pharmaceuticals, Inc. Cyclosporins for the treatment of immune disorders
CA2518265A1 (en) 2003-03-17 2004-09-30 Albany Molecular Research, Inc. Novel cyclosporins
ITMI20030627A1 (it) 2003-03-31 2004-10-01 Polimeri Europa Spa Polimeri vinilaromatici espandibili e procedimento per la loro preparazione.
TW200505946A (en) 2003-04-08 2005-02-16 Hoffmann La Roche Process for preparation of cyclosporin a analog
SI1620429T1 (sl) * 2003-04-11 2009-08-31 Glenmark Pharmaceuticals Sa Nove heterociklične spojine, uporabne za zdravljenje vnetnih in alergijskih motenj: postopek za njihovo pripravo in farmacevtski sestavki, ki jih vsebujejo
US20040266669A1 (en) 2003-06-20 2004-12-30 Wu Frank X. H. Cyclosporin derivatives for the treatment of immune disorders
GB0320638D0 (en) 2003-09-03 2003-10-01 Novartis Ag Organic compounds
DE102004011988A1 (de) 2004-03-11 2005-09-22 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Cyclosporinderivate und diese enthaltende pharmazeutische Zusammensetzungen
US20060015374A1 (en) 2004-07-19 2006-01-19 Yanhong Ochs Risk management on the application of crop inputs
WO2006014872A2 (en) 2004-07-29 2006-02-09 Amr Technology, Inc. Novel processes for stereoselective synthesis of trans isatx 247
US20060035821A1 (en) 2004-08-16 2006-02-16 Hunt Kevin W Cyclosporin analogs for the treatment of immunoregulatory disorders and respiratory diseases
US7226906B2 (en) 2004-08-16 2007-06-05 Array Biopharma, Inc. Cyclosporin analogs for the treatment of immunoregulatory disorders and respiratory diseases
JP2008514702A (ja) * 2004-09-29 2008-05-08 エーエムアール テクノロジー インコーポレイテッド 新規シクロスポリン類似体およびそれらの薬学的使用
US7378391B2 (en) * 2004-09-29 2008-05-27 Amr Technology, Inc. Cyclosporin alkyne analogues and their pharmaceutical uses
PT1802650E (pt) 2004-10-01 2011-12-30 Scynexis Inc Derivados da ciclosporina 3-éter e 3-tioéter substituída para o tratamento e prevenção da infecção de hepatite c
WO2006041631A2 (en) 2004-10-06 2006-04-20 Amr Technology, Inc. Novel cyclosporin alkynes and their utility as pharmaceutical agents
ES2314731T3 (es) 2004-11-22 2009-03-16 Astellas Pharma Inc. Analogo de ciclosporina.
TW200635954A (en) * 2004-12-17 2006-10-16 Isotechnika Inc Metabolites of cyclosporin analogs
WO2007041631A1 (en) 2005-09-30 2007-04-12 Scynexis, Inc. ARYIiALKYL AND HETEROARYLALKYL DERIVATIVES OF CYCLOSPORINE A FOR THE TREATMENT AND PREVENTION OF VIRAL INFECTION
US20070232532A1 (en) 2006-03-28 2007-10-04 Amr Technology, Inc. Use of cyclosporin alkene analogues for preventing or treating viral-induced disorders
US7696165B2 (en) 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne analogues for preventing or treating viral-induced disorders
WO2008069917A2 (en) 2006-11-20 2008-06-12 Scynexis, Inc. Novel cyclic peptides
US8716238B2 (en) * 2008-07-10 2014-05-06 Allergan, Inc. Cyclosporin derivatives for treating ocular and dermal diseases and conditions
RU2492181C2 (ru) 2009-01-30 2013-09-10 Энанта Фармасьютикалс, Инк. Аналоги циклоспорина для предупреждения или лечения инфекции гепатита с
US20100305047A1 (en) * 2009-05-27 2010-12-02 Allergan, Inc. Cyclosporin derivatives for enhancing the growth of hair
CA2785978A1 (en) * 2009-12-30 2011-07-07 Scynexis, Inc. Cyclosporine analogues
AU2011316690C1 (en) * 2010-10-12 2017-01-19 Allergan, Inc. Cyclosporin analogs
EP2627663B1 (en) * 2010-10-12 2018-02-21 Allergan, Inc. Cyclosporin analogs
AU2011342284C1 (en) * 2010-12-15 2017-07-13 Contravir Pharmaceuticals, Inc. Cyclosporine analogue molecules modified at amino acid 1 and 3

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030212249A1 (en) 2001-10-19 2003-11-13 Isotechnika, Inc. Synthesis of cyclosporin analogs
US20070232531A1 (en) * 2006-03-28 2007-10-04 Amr Technology, Inc. Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders
WO2010012073A1 (en) 2008-07-30 2010-02-04 Isotechnika Labs Inc. Nonimmunosuppressive cyclosporine analogue molecules

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