JP6144627B2 - アミノ酸１および３で修飾されたシクロスポリン類似体分子 - Google Patents

アミノ酸１および３で修飾されたシクロスポリン類似体分子 Download PDF

Info

Publication number
JP6144627B2
JP6144627B2 JP2013543478A JP2013543478A JP6144627B2 JP 6144627 B2 JP6144627 B2 JP 6144627B2 JP 2013543478 A JP2013543478 A JP 2013543478A JP 2013543478 A JP2013543478 A JP 2013543478A JP 6144627 B2 JP6144627 B2 JP 6144627B2
Authority
JP
Japan
Prior art keywords
compound
disease
group
injury
reaction
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
JP2013543478A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014505035A5 (enExample
JP2014505035A (ja
Inventor
ヘグマンズ、アレキサンダー
フェンスキ、ブルース、ダブリュー．
トレパニアー、ダン、ジェイ．
アベル、マーク、ディー．
スギヤマ、シン
アール． ウレ、ダレン
アール． ウレ、ダレン
Original Assignee
コントラヴィア ファーマシューティカルズ、インク．
コントラヴィア ファーマシューティカルズ、インク．
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
Application filed by コントラヴィア ファーマシューティカルズ、インク．, コントラヴィア ファーマシューティカルズ、インク． filed Critical コントラヴィア ファーマシューティカルズ、インク．
Publication of JP2014505035A publication Critical patent/JP2014505035A/ja
Publication of JP2014505035A5 publication Critical patent/JP2014505035A5/ja
Application granted granted Critical
Publication of JP6144627B2 publication Critical patent/JP6144627B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/06—Free radical scavengers or antioxidants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
JP2013543478A 2010-12-15 2011-12-14 アミノ酸１および３で修飾されたシクロスポリン類似体分子 Active JP6144627B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US42357610P 2010-12-15 2010-12-15
US61/423,576 2010-12-15
PCT/CA2011/050773 WO2012079172A1 (en) 2010-12-15 2011-12-14 Cyclosporine analogue molecules modified at amino acid 1 and 3

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2017024484A Division JP6831259B2 (ja) 2010-12-15 2017-02-13 アミノ酸１および３で修飾されたシクロスポリン類似体分子

Publications (3)

Publication Number Publication Date
JP2014505035A JP2014505035A (ja) 2014-02-27
JP2014505035A5 JP2014505035A5 (enExample) 2015-07-09
JP6144627B2 true JP6144627B2 (ja) 2017-06-07

Family

ID=46243924

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2013543478A Active JP6144627B2 (ja) 2010-12-15 2011-12-14 アミノ酸１および３で修飾されたシクロスポリン類似体分子
JP2017024484A Active JP6831259B2 (ja) 2010-12-15 2017-02-13 アミノ酸１および３で修飾されたシクロスポリン類似体分子
JP2019018182A Pending JP2019123712A (ja) 2010-12-15 2019-02-04 アミノ酸１および３で修飾されたシクロスポリン類似体分子

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2017024484A Active JP6831259B2 (ja) 2010-12-15 2017-02-13 アミノ酸１および３で修飾されたシクロスポリン類似体分子
JP2019018182A Pending JP2019123712A (ja) 2010-12-15 2019-02-04 アミノ酸１および３で修飾されたシクロスポリン類似体分子

Country Status (25)

Country Link
US (2) US9200038B2 (enExample)
EP (2) EP2651965B1 (enExample)
JP (3) JP6144627B2 (enExample)
KR (3) KR20190002731A (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)
MX (1) MX353720B (enExample)
MY (2) MY192981A (enExample)
NZ (1) NZ611620A (enExample)
PH (1) PH12013501213A1 (enExample)
PL (1) PL2651965T3 (enExample)
PT (1) PT2651965T (enExample)
RU (1) RU2630690C9 (enExample)
SG (2) SG10201510236XA (enExample)
SI (1) SI2651965T1 (enExample)
TR (1) TR201900128T4 (enExample)
WO (1) WO2012079172A1 (enExample)

Families Citing this family (24)

* 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
AU2013267435B2 (en) * 2012-06-01 2017-11-09 Allergan, Inc. Cyclosporin A analogs
US20160002299A1 (en) * 2013-03-01 2016-01-07 Ucl Business Plc Non-immunosuppressive cyclosporin derivatives as antiviral agents
US9221878B2 (en) * 2013-08-26 2015-12-29 Enanta Pharmaceuticals, Inc. Cyclosporin analogues for preventing or treating hepatitis C infection
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
CN110087530A (zh) 2016-12-07 2019-08-02 普罗根尼蒂公司 胃肠道检测方法、装置和系统
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
CA3046023A1 (en) 2016-12-14 2018-06-21 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with an immunosuppressant
WO2018191579A1 (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
CA3110250A1 (en) * 2018-08-22 2020-02-27 Bacainn Therapeutics, Ltd. Cyclosporine compositions and methods of use
AU2021224676A1 (en) 2020-02-19 2022-09-08 Hepion Pharmaceuticals, Inc. Use of cyclosporine analogues for treating fibrosis
US20210269479A1 (en) * 2020-02-25 2021-09-02 Hepion Pharmaceuticals, Inc. Use of cyclosporine analogues for treating cancer
WO2021190603A1 (en) * 2020-03-26 2021-09-30 Farsight Medical Technology (Shanghai) Co., Ltd. Cyclophilin inhibitors and uses thereof
BR112022018929A2 (pt) 2020-03-26 2022-12-06 Farsight Medical Tech Shanghai Co Ltd Inibidores da ciclofilina e seus usos
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
WO2024254480A2 (en) * 2023-06-08 2024-12-12 Hepion Pharmaceuticals, Inc. Solid state forms of rencofilstat

Family Cites Families (100)

* 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
US4160452A (en) 1977-04-07 1979-07-10 Alza Corporation Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
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
EP0098456B1 (en) 1980-02-14 1989-05-24 Sandoz Ag Peptides comprising a (1s,2r,3r)- or (1r,2s,3s)-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptane or -hept-5-ene residue useful in the total synthesis of cyclosporins, and processes for their production
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
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"
DE3884470T2 (de) 1987-06-17 1994-03-10 Sandoz Ag Cyclosporine und deren Benutzung als Arzneimittel.
ES2056954T3 (es) 1987-06-19 1994-10-16 Sandoz Ag Peptolidos ciclicos.
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
US5236899A (en) 1987-11-16 1993-08-17 Merck & Co., Inc. 6-position cyclosporin a analogs as modifiers of cytotoxic drug resistance
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
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
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
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
DE69124459T3 (de) 1990-11-02 2001-05-31 Novartis Ag, Basel Zyklosporine
GB9204466D0 (en) 1992-03-02 1992-04-15 Sandoz Ltd Improvements in or relating to organic compounds
US5639852A (en) 1994-09-01 1997-06-17 Wisconsin Alumni Research Foundation Immunostimulatory agents
US5948693A (en) 1994-09-01 1999-09-07 Wisconsin Alumni Research Foundation Solid phase synthesis of immunosuppressive 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
DE59608274D1 (de) * 1995-07-17 2002-01-03 Chem Ag Binningen C Cyclosporin-derivate mit anti-hiv-wirkung
EP0852233A4 (en) 1995-09-21 1999-09-15 Nippon Shinyaku Co Ltd CYCLOSPORIN PHOSPHATE DERIVATIVES AND MEDICINAL COMPOSITION
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
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
WO1999010373A1 (en) 1997-08-26 1999-03-04 Wisconsin Alumni Research Foundation Non-immunosuppressive cyclosporins and their use in the prevention and treatment of hiv infection
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
CA2298572C (en) 1997-10-08 2002-04-09 Isotechnika Inc. Deuterated cyclosporine analogs and their use as immunomodulating agents
US20030220234A1 (en) 1998-11-02 2003-11-27 Selvaraj Naicker Deuterated cyclosporine analogs and their use as immunodulating agents
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
BR9911160A (pt) 1998-06-12 2001-04-03 Chem Ag C Ciclosporinas
FR2780061B1 (fr) 1998-06-22 2001-09-07 Rhone Poulenc Rorer Sa Nouveau procede de preparation de derives de cyclosporine
EP1091975B1 (fr) 1998-07-01 2005-12-14 Debiopharm S.A. Nouvelle cyclosporine ayant un profil d'activite ameliore
ATE330968T1 (de) 1999-02-05 2006-07-15 Debiopharm Sa Cyclosporin-derivate und verfahren zu deren herstellung
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
KR100360716B1 (ko) 2000-11-22 2002-11-13 주식회사 엘지생활건강 사이클로스포린 에이 7- 티오아미드 유도체를유효성분으로 하는 모발성장촉진제
KR20020039528A (ko) 2000-11-22 2002-05-27 조명재 사이클로스포린 7- 티오아미드 유도체를 유효성분으로하는 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
CN1507451A (zh) 2001-04-20 2004-06-23 �±Ȱ·�ķ�ɷ����޹�˾ 可用作前体药物的修饰环孢菌素及其应用
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
DE60233150D1 (de) 2001-10-19 2009-09-10 Isotechnika Inc Neue cyclosporin-analoge mikroemulsionsvorkonzentrate
RU2337106C2 (ru) 2001-10-19 2008-10-27 Изотехника Инк. Смесь аналогов циклоспорина и ее применение в качестве иммуномодулирующего агента
PT1436321E (pt) 2001-10-19 2006-10-31 Isotechnika Inc Sintese de analogos de ciclosporina
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
EP1603512A2 (en) 2003-03-17 2005-12-14 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
MXPA05010948A (es) * 2003-04-11 2006-05-31 Glenmark Pharmaceuticals Sa Compuestos heterociclicos novedosos utiles para el tratamiento de trastornos inflamatorios y alergicos: procedimiento para su preparacion y composiciones farmacuticas que los contienen.
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
CA2575280C (en) 2004-07-29 2012-08-14 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
US7378391B2 (en) * 2004-09-29 2008-05-27 Amr Technology, Inc. Cyclosporin alkyne analogues and their pharmaceutical uses
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
RU2399628C2 (ru) 2004-10-01 2010-09-20 Скайнексис, Инк. Производные циклоспорина, замещенные 3-эфиром и 3-тиоэфиром, для лечения и профилактики инфекционного гепатита с
JP2008515886A (ja) 2004-10-06 2008-05-15 エーエムアール テクノロジー インコーポレイテッド シクロスポリンアルキンおよびそれらの医用薬剤としての有用性
US7696167B2 (en) 2004-11-22 2010-04-13 Astellas Pharma Inc. Cyclic peptide compound
EP1828229A4 (en) 2004-12-17 2010-06-30 Isotechnika Inc METABOLITES OF CYCLOSPORINANALOGA
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
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
US7696165B2 (en) 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne analogues for preventing or treating viral-induced disorders
US20070232532A1 (en) 2006-03-28 2007-10-04 Amr Technology, Inc. Use of cyclosporin alkene analogues for preventing or treating viral-induced disorders
WO2008069917A2 (en) 2006-11-20 2008-06-12 Scynexis, Inc. Novel cyclic peptides
BRPI0915552A2 (pt) * 2008-07-10 2017-06-20 Allergan Inc derivados de ciclosporina, seu uso e sua composição farmacêutica
US20130190223A1 (en) 2008-07-30 2013-07-25 Isotechnika Pharma Inc. Nonimmunosuppressive cyclosporine analogue molecules
KR20110111321A (ko) 2009-01-30 2011-10-10 이난타 파마슈티칼스, 인코포레이티드 Ｃ형 간염을 예방하거나 치료하기 위한 사이클로스포린 유사체
WO2010138422A1 (en) 2009-05-27 2010-12-02 Allergan, Inc. Cyclosporin derivatives for enhancing the growth of hair
JP2013516424A (ja) * 2009-12-30 2013-05-13 サイネクシス，インコーポレーテッド シクロスポリン類似体
BR112013008864A2 (pt) * 2010-10-12 2016-06-28 Allergan Inc análogos d ciclosporina
RU2013120927A (ru) * 2010-10-12 2014-11-20 Аллерган, Инк. Аналоги циклоспорина
AU2011342284C1 (en) * 2010-12-15 2017-07-13 Contravir Pharmaceuticals, Inc. Cyclosporine analogue molecules modified at amino acid 1 and 3

Also Published As

Publication number Publication date
ES2705750T3 (es) 2019-03-26
PL2651965T3 (pl) 2019-04-30
RU2013127162A (ru) 2015-06-10
MX353720B (es) 2018-01-25
CN107496902A (zh) 2017-12-22
AU2011342284C1 (en) 2017-07-13
US9714271B2 (en) 2017-07-25
KR102011339B1 (ko) 2019-08-16
US9200038B2 (en) 2015-12-01
JP2019123712A (ja) 2019-07-25
IL226792A (en) 2017-10-31
BR112013014890A2 (pt) 2020-08-04
HRP20190096T1 (hr) 2019-02-22
RU2630690C9 (ru) 2017-12-28
CN107496902B (zh) 2022-01-18
AU2011342284B2 (en) 2017-02-16
JP6831259B2 (ja) 2021-02-17
AU2011342284A1 (en) 2013-07-18
SI2651965T1 (sl) 2019-03-29
NZ611620A (en) 2016-02-26
PH12013501213A1 (en) 2016-12-16
HK1243633A1 (zh) 2018-07-20
SG10201510236XA (en) 2016-01-28
EP2651965B1 (en) 2018-12-12
SG191069A1 (en) 2013-07-31
DK2651965T3 (en) 2019-02-18
KR102305423B1 (ko) 2021-09-27
JP2014505035A (ja) 2014-02-27
JP2017128577A (ja) 2017-07-27
PT2651965T (pt) 2019-01-28
EP2651965A1 (en) 2013-10-23
BR112013014890B1 (pt) 2023-10-24
MX2013006831A (es) 2014-10-14
EP2651965A4 (en) 2017-08-09
KR20130124515A (ko) 2013-11-14
CN103443119A (zh) 2013-12-11
TR201900128T4 (tr) 2019-02-21
MY192981A (en) 2022-09-20
CA2821009C (en) 2019-03-05
MY165152A (en) 2018-02-28
CN103443119B (zh) 2017-09-22
US20140142033A1 (en) 2014-05-22
US20160207961A1 (en) 2016-07-21
KR20200029639A (ko) 2020-03-18
CA2821009A1 (en) 2012-06-21
HUE042490T2 (hu) 2019-07-29
LT2651965T (lt) 2019-01-10
EP3461835A1 (en) 2019-04-03
WO2012079172A1 (en) 2012-06-21
RU2630690C2 (ru) 2017-09-12
KR20190002731A (ko) 2019-01-08

Similar Documents

Publication Publication Date Title
JP6144627B2 (ja) アミノ酸１および３で修飾されたシクロスポリン類似体分子
JP2014505035A5 (enExample)
JP5726733B2 (ja) 非免疫抑制性シクロスポリン類似体分子
HK1243633B (zh) 在氨基酸1和3位修改的环孢菌素类似分子
HK1191655A (en) Cyclosporine analogue molecules modified at amino acid 1 and 3
HK1191655B (en) Cyclosporine analogue molecules modified at amino acid 1 and 3
HK1161277A (en) Nonimmunosuppressive cyclosporine analogue molecules

Legal Events

Date Code Title Description
A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20141016

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20141016

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20141213

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20150413

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150515

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20151215

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20160314

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160615

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20161011

A711 Notification of change in applicant

Free format text: JAPANESE INTERMEDIATE CODE: A711

Effective date: 20170203

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170213

C60 Trial request (containing other claim documents, opposition documents)

Free format text: JAPANESE INTERMEDIATE CODE: C60

Effective date: 20170213

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20170203

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20170301

C21 Notice of transfer of a case for reconsideration by examiners before appeal proceedings

Free format text: JAPANESE INTERMEDIATE CODE: C21

Effective date: 20170307

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20170502

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20170511

R150 Certificate of patent or registration of utility model

Ref document number: 6144627

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250