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

아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자 Download PDF

Info

Publication number
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
Authority
KR
South Korea
Prior art keywords
compound
formula
group
disease
saturated
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
KR1020207007384A
Other languages
English (en)
Korean (ko)
Other versions
KR20200029639A (ko
Inventor
알렉산더 헤그먼스
브루스 더블유. 펜스크
댄 제이. 트리패니어
마크 디. 아벨
신 스기야마
대런 알. 유레
Original Assignee
콘트라빌 파마슈티컬스, 인코퍼레이티드
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 콘트라빌 파마슈티컬스, 인코퍼레이티드 filed Critical 콘트라빌 파마슈티컬스, 인코퍼레이티드
Publication of KR20200029639A publication Critical patent/KR20200029639A/ko
Application granted granted Critical
Publication of KR102305423B1 publication Critical patent/KR102305423B1/ko
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)
  • Virology (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Transplantation (AREA)
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
PCT/CA2011/050773 WO2012079172A1 (en) 2010-12-15 2011-12-14 Cyclosporine analogue molecules modified at amino acid 1 and 3
KR1020187037529A KR20190002731A (ko) 2010-12-15 2011-12-14 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020187037529A Division KR20190002731A (ko) 2010-12-15 2011-12-14 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자

Publications (2)

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

Family

ID=46243924

Family Applications (3)

Application Number Title Priority Date Filing Date
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

Family Applications After (2)

Application Number Title Priority Date Filing Date
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

Country Status (25)

Country Link
US (2) US9200038B2 (https=)
EP (2) EP2651965B1 (https=)
JP (3) JP6144627B2 (https=)
KR (3) KR102305423B1 (https=)
CN (2) CN103443119B (https=)
AU (1) AU2011342284C1 (https=)
BR (1) BR112013014890B1 (https=)
CA (1) CA2821009C (https=)
DK (1) DK2651965T3 (https=)
ES (1) ES2705750T3 (https=)
HR (1) HRP20190096T1 (https=)
HU (1) HUE042490T2 (https=)
IL (1) IL226792A (https=)
LT (1) LT2651965T (https=)
MX (1) MX353720B (https=)
MY (2) MY165152A (https=)
NZ (1) NZ611620A (https=)
PH (1) PH12013501213A1 (https=)
PL (1) PL2651965T3 (https=)
PT (1) PT2651965T (https=)
RU (1) RU2630690C9 (https=)
SG (2) SG10201510236XA (https=)
SI (1) SI2651965T1 (https=)
TR (1) TR201900128T4 (https=)
WO (1) WO2012079172A1 (https=)

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
WO2012079172A1 (en) * 2010-12-15 2012-06-21 Isotechnika Pharma Inc. Cyclosporine analogue molecules modified at amino acid 1 and 3
JP2015519368A (ja) * 2012-06-01 2015-07-09 アラーガン インコーポレイテッドＡｌｌｅｒｇａｎ，Ｉｎｃｏｒｐｏｒａｔｅｄ シクロスポリンａ類似体
EP2961767B1 (en) * 2013-03-01 2018-09-26 UCL Business PLC Non-immunosuppressive cyclosporin derivatives as antiviral agents
WO2015031381A1 (en) * 2013-08-26 2015-03-05 Enanta Pharmaceuticals, Inc. Cyclosporin analogues for preventing or treating hepatitis c
US9914755B2 (en) 2015-01-08 2018-03-13 Allergan, Inc. Cyclosporin derivatives wherein the MeBmt sidechain has been cyclized
CN109476705B (zh) * 2016-05-17 2024-02-27 美国科技环球有限公司 新型环孢菌素衍生物及其用途
US10610104B2 (en) 2016-12-07 2020-04-07 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
EP3554346B1 (en) 2016-12-14 2024-01-31 Biora Therapeutics, Inc. Treatment of a disease of the gastrointestinal tract with an immunosuppressant
TW201902507A (zh) 2017-04-14 2019-01-16 美商康特維爾製藥公司 治療病毒感染之組合療法
EP3612540A1 (en) 2017-04-20 2020-02-26 Rising Tide Foundation Triphenylphosphonium-tethered tetracycyclines for use in treating cancer
WO2019246312A1 (en) 2018-06-20 2019-12-26 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with an immunomodulator
ES2990218T3 (es) * 2018-08-22 2024-11-29 Bacainn Biotherapeutics Ltd Composiciones de ciclosporina y métodos de uso
WO2020163594A1 (en) 2019-02-07 2020-08-13 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
IL295498A (en) * 2020-02-25 2022-10-01 Hepion Pharmaceuticals Inc Use of cyclosporine analogues for treating cancer
IL296586B1 (en) 2020-03-26 2026-04-01 Farsight Medical Tech Shanghai Co Ltd Cyclophilin inhibitors and their uses
CA3172689A1 (en) * 2020-03-26 2021-09-30 Ching-Pong Mak Cyclophilin inhibitors and uses thereof
AU2021388171A1 (en) * 2020-11-29 2023-06-22 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
KR20260018851A (ko) * 2023-06-02 2026-02-09 파사이트 메디컬 테크놀로지 (상하이) 컴퍼니 리미티드 사이클로필린 저해제 및 그 용도
EP4724081A2 (en) * 2023-06-08 2026-04-15 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
US4210581A (en) 1975-11-04 1980-07-01 Sandoz Ltd. Organic compounds
CH614931A5 (https=) 1975-11-04 1979-12-28 Sandoz Ag
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
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
EP0034567B1 (en) 1980-02-14 1984-11-07 Sandoz Ag A method for the total synthesis of cyclosporins and novel cyclosporins
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
US4885276A (en) 1987-06-03 1989-12-05 Merck & Co., Inc. Cyclosporin analogs with modified "C-9 amino acids"
US4798823A (en) 1987-06-03 1989-01-17 Merck & Co., Inc. New cyclosporin analogs with modified "C-9 amino acids"
ES2059558T3 (es) 1987-06-17 1994-11-16 Sandoz Ag Ciclosporins y su uso como productos farmaceuticos.
EP0296123B1 (en) 1987-06-19 1994-08-31 Sandoz Ag Cyclic peptolides
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
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
CA2004626A1 (en) 1988-12-05 1990-06-05 Bernard F. Erlanger 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
US5122511A (en) 1990-02-27 1992-06-16 Merck & Co., Inc. Immunosuppressive cyclosporin analogs with modified amino acids at position-8
US5214130A (en) 1990-02-27 1993-05-25 Merck & Co., Inc. Synthesis of novel 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
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
ATE209216T1 (de) * 1995-07-17 2001-12-15 Chem Ag 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
EP0991660B8 (en) 1997-10-08 2006-04-05 Isotechnika,Inc. DEUTERATED and undeuterated 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
PT1086124E (pt) 1998-06-12 2004-04-30 Chem Ag C Ciclosporinas novas
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
US6790935B1 (en) 1999-02-05 2004-09-14 Debiopharm S.A. Cyclosporin derivatives and method for the production of said derivatives
WO2001035914A1 (en) 1999-11-19 2001-05-25 Lg Household & Health Care Ltd Use of nonimmunosuppressive cyclosporin derivatives for hair growth
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
HRP20040354B1 (en) 2001-10-19 2012-10-31 Isotechnika Inc. Novel cyclosporin analog microemulsion preconcentrates
EP1816138A1 (en) 2001-10-19 2007-08-08 Isotechnika,Inc. Cyclosporine analogue mixtures and their use as immunomodulating agents
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
OA13154A (en) * 2003-04-11 2006-12-13 Glenmark Pharmaceuticals Sa Novel heterocyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them.
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
US7378391B2 (en) 2004-09-29 2008-05-27 Amr Technology, Inc. Cyclosporin alkyne analogues and their pharmaceutical uses
WO2006039164A2 (en) 2004-09-29 2006-04-13 Amr Technology, Inc. Novel cyclosporin analogues and their pharmaceutical uses
KR101309409B1 (ko) 2004-10-01 2013-09-23 싸이넥시스, 인크. Ｃ형 간염 바이러스 감염의 치료 및 예방을 위한 ３-에테르및 ３-티오에테르 치환된 시클로스포린 유도체
WO2006041631A2 (en) 2004-10-06 2006-04-20 Amr Technology, Inc. Novel cyclosporin alkynes and their utility as pharmaceutical agents
US7696167B2 (en) 2004-11-22 2010-04-13 Astellas Pharma Inc. Cyclic peptide compound
JP2008524122A (ja) * 2004-12-17 2008-07-10 イソテクニカ インコーポレーテッド シクロスポリン類似体の代謝体
DE602006020152D1 (de) 2005-09-30 2011-03-31 Scynexis Inc Arylalkyl- und heteroarylalkyl-derivate von cyclosporin a bei der behandlung und vorbeugung einer virusinfektion
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
KR20110031973A (ko) * 2008-07-10 2011-03-29 알러간, 인코포레이티드 눈 및 피부의 질환 및 상태를 치료하기 위한 사이클로스포린 유도체
WO2010088573A1 (en) 2009-01-30 2010-08-05 Enanta Pharmaceuticals, Inc. Cyclosporin analogues for preventing or treating hepatitis c infection
WO2010138422A1 (en) * 2009-05-27 2010-12-02 Allergan, Inc. Cyclosporin derivatives for enhancing the growth of hair
KR20120125610A (ko) * 2009-12-30 2012-11-16 싸이넥시스, 인크. 시클로스포린 유사체
MX2013004062A (es) * 2010-10-12 2013-07-22 Allergan Inc Analogos de ciclosporina.
BR112013008864A2 (pt) * 2010-10-12 2016-06-28 Allergan Inc análogos d ciclosporina
WO2012079172A1 (en) * 2010-12-15 2012-06-21 Isotechnika Pharma 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

Also Published As

Publication number Publication date
BR112013014890B1 (pt) 2023-10-24
US9200038B2 (en) 2015-12-01
DK2651965T3 (en) 2019-02-18
CN103443119A (zh) 2013-12-11
MY192981A (en) 2022-09-20
LT2651965T (lt) 2019-01-10
RU2630690C2 (ru) 2017-09-12
JP2014505035A (ja) 2014-02-27
JP6831259B2 (ja) 2021-02-17
MX353720B (es) 2018-01-25
SG10201510236XA (en) 2016-01-28
WO2012079172A1 (en) 2012-06-21
SG191069A1 (en) 2013-07-31
ES2705750T3 (es) 2019-03-26
RU2630690C9 (ru) 2017-12-28
RU2013127162A (ru) 2015-06-10
TR201900128T4 (tr) 2019-02-21
KR20190002731A (ko) 2019-01-08
HK1243633A1 (zh) 2018-07-20
KR102011339B1 (ko) 2019-08-16
AU2011342284B2 (en) 2017-02-16
EP2651965A4 (en) 2017-08-09
KR20130124515A (ko) 2013-11-14
PH12013501213A1 (en) 2016-12-16
IL226792A (en) 2017-10-31
PL2651965T3 (pl) 2019-04-30
CN107496902B (zh) 2022-01-18
AU2011342284C1 (en) 2017-07-13
EP2651965B1 (en) 2018-12-12
KR20200029639A (ko) 2020-03-18
NZ611620A (en) 2016-02-26
US20140142033A1 (en) 2014-05-22
EP2651965A1 (en) 2013-10-23
JP6144627B2 (ja) 2017-06-07
CN107496902A (zh) 2017-12-22
HRP20190096T1 (hr) 2019-02-22
SI2651965T1 (sl) 2019-03-29
JP2017128577A (ja) 2017-07-27
HUE042490T2 (hu) 2019-07-29
MX2013006831A (es) 2014-10-14
AU2011342284A1 (en) 2013-07-18
US20160207961A1 (en) 2016-07-21
CA2821009A1 (en) 2012-06-21
EP3461835A1 (en) 2019-04-03
US9714271B2 (en) 2017-07-25
MY165152A (en) 2018-02-28
JP2019123712A (ja) 2019-07-25
BR112013014890A2 (pt) 2020-08-04
PT2651965T (pt) 2019-01-28
CN103443119B (zh) 2017-09-22
CA2821009C (en) 2019-03-05

Similar Documents

Publication Publication Date Title
KR102305423B1 (ko) 아미노산 1 및 3에서 변형된 사이클로스포린 유사체 분자
JP2014505035A5 (https=)
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
A107 Divisional application of patent
A302 Request for accelerated examination
PA0104 Divisional application for international application

Comment text: Divisional Application for International Patent

Patent event code: PA01041R01D

Patent event date: 20200312

Application number text: 1020187037529

Filing date: 20181224

PA0201 Request for examination
PA0302 Request for accelerated examination

Patent event date: 20200312

Patent event code: PA03022R01D

Comment text: Request for Accelerated Examination

PG1501 Laying open of application
E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20200504

Patent event code: PE09021S01D

AMND Amendment
E601 Decision to refuse application
PE0601 Decision on rejection of patent

Patent event date: 20210119

Comment text: Decision to Refuse Application

Patent event code: PE06012S01D

Patent event date: 20200504

Comment text: Notification of reason for refusal

Patent event code: PE06011S01I

X091 Application refused [patent]
AMND Amendment
PX0901 Re-examination

Patent event code: PX09011S01I

Patent event date: 20210119

Comment text: Decision to Refuse Application

Patent event code: PX09012R01I

Patent event date: 20201104

Comment text: Amendment to Specification, etc.

E90F Notification of reason for final refusal
PE0902 Notice of grounds for rejection

Comment text: Final Notice of Reason for Refusal

Patent event date: 20210427

Patent event code: PE09021S02D

AMND Amendment
PX0701 Decision of registration after re-examination

Patent event date: 20210817

Comment text: Decision to Grant Registration

Patent event code: PX07013S01D

Patent event date: 20210624

Comment text: Amendment to Specification, etc.

Patent event code: PX07012R01I

Patent event date: 20210416

Comment text: Amendment to Specification, etc.

Patent event code: PX07012R01I

Patent event date: 20210119

Comment text: Decision to Refuse Application

Patent event code: PX07011S01I

Patent event date: 20201104

Comment text: Amendment to Specification, etc.

Patent event code: PX07012R01I

X701 Decision to grant (after re-examination)
GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20210916

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20210917

End annual number: 3

Start annual number: 1

PG1601 Publication of registration
PR1001 Payment of annual fee

Payment date: 20240903

Start annual number: 4

End annual number: 4