WO2002069902A3 - Cyclosporins for the treatment of respiratory diseases - Google Patents

Cyclosporins for the treatment of respiratory diseases Download PDF

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Publication number
WO2002069902A3
WO2002069902A3 PCT/US2002/006541 US0206541W WO02069902A3 WO 2002069902 A3 WO2002069902 A3 WO 2002069902A3 US 0206541 W US0206541 W US 0206541W WO 02069902 A3 WO02069902 A3 WO 02069902A3
Authority
WO
WIPO (PCT)
Prior art keywords
halogen
ser
alkylthio
alkoxy
alkyl
Prior art date
Application number
PCT/US2002/006541
Other languages
French (fr)
Other versions
WO2002069902A2 (en
Inventor
Yat Sun Or
Tsvetelina Lazarova
Blake Christopher Hamann
Original Assignee
Enanta Pharm Inc
Yat Sun Or
Tsvetelina Lazarova
Blake Christopher Hamann
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 Enanta Pharm Inc, Yat Sun Or, Tsvetelina Lazarova, Blake Christopher Hamann filed Critical Enanta Pharm Inc
Priority to CA002439832A priority Critical patent/CA2439832A1/en
Priority to EP02713733A priority patent/EP1365791A2/en
Priority to JP2002569080A priority patent/JP2004526719A/en
Publication of WO2002069902A2 publication Critical patent/WO2002069902A2/en
Publication of WO2002069902A3 publication Critical patent/WO2002069902A3/en

Links

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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

The present invention relates to novel semisynthetic cyclosporin analogs of formula (I), wherein A is (II), X is absent, -C1-C6 alkyl-, or -C3-C6 cycloalkyl- Y is selected from the group consisting of: (i) C(O)-O-R1, where R1 is hydrogen, C1-C6-alkyl, optionally substituted with halogen, heterocyclic, aryl, C1-C6-alkoxy, C1-C6-alkylthio, halogen-substituted C1-C6-alkoxy, or halogen-substituted C1-C6-alkylthio; (ii) C(O)-S-R1 , where R1 is as previously defined; (iii) C(O)-OCH2-OC(O)R2, where R2 is C1-C6-alkyl, optionally substituted with halogen, C1-C6-alkoxy; C1-C6-alkylthio, heterocyclic or aryl; (iv) C(S)-O-R1 , where R1 is as previously defined; and (v) C(S)-S-R1 , where R1 is as previously defined; B is -αAbu-, -Val-, -Thr- or -Nva- ;U and is -(D)Ala-, -(D)Ser-, -[O-(2 -hydroxyethyl)(D)Ser]-, -[O-acyl(D)Ser]- or -[O-(2-acyloxyethyl) (D )Ser]-.
PCT/US2002/006541 2001-03-05 2002-03-05 Cyclosporins for the treatment of respiratory diseases WO2002069902A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CA002439832A CA2439832A1 (en) 2001-03-05 2002-03-05 Cyclosporins for the treatment of respiratory diseases
EP02713733A EP1365791A2 (en) 2001-03-05 2002-03-05 Cyclosporins for the treatment of respiratory diseases
JP2002569080A JP2004526719A (en) 2001-03-05 2002-03-05 Cyclosporine for the treatment of respiratory diseases

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/800,856 2001-03-05
US09/800,856 US6784156B2 (en) 2001-03-05 2001-03-05 Cyclosporins for the treatment of respiratory diseases

Publications (2)

Publication Number Publication Date
WO2002069902A2 WO2002069902A2 (en) 2002-09-12
WO2002069902A3 true WO2002069902A3 (en) 2003-04-17

Family

ID=25179553

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/006541 WO2002069902A2 (en) 2001-03-05 2002-03-05 Cyclosporins for the treatment of respiratory diseases

Country Status (5)

Country Link
US (3) US6784156B2 (en)
EP (1) EP1365791A2 (en)
JP (1) JP2004526719A (en)
CA (1) CA2439832A1 (en)
WO (1) WO2002069902A2 (en)

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US20030087813A1 (en) * 2001-10-12 2003-05-08 Or Yat Sun Cyclosporin analogs for the treatment of lung diseases
AU2003280867A1 (en) * 2002-11-04 2004-06-07 Charite-Universitatsme Dizin Berlin Specific haplotypes of the mdr1 gene and their use in diagnosis and therapy
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
US20040261140A1 (en) * 2003-03-07 2004-12-23 Benson John D. Transgenic mice expressing human formyl peptide receptor
JP2006524232A (en) * 2003-03-17 2006-10-26 アルバニー モレキュラー リサーチ インコーポレーティッド New cyclosporine
US20050059583A1 (en) 2003-09-15 2005-03-17 Allergan, Inc. Methods of providing therapeutic effects using cyclosporin components
US20060014677A1 (en) * 2004-07-19 2006-01-19 Isotechnika International Inc. Method for maximizing efficacy and predicting and minimizing toxicity of calcineurin inhibitor compounds
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 (en) * 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 Novel cyclosporine analogues and their pharmaceutical use
JP2008514701A (en) * 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 Cyclosporine alkyne analogs and their pharmaceutical use
EP1812037A4 (en) * 2004-10-06 2009-11-11 Amr Technology Inc Novel cyclosporin alkynes and their utility as pharmaceutical agents
US7135455B2 (en) * 2004-11-15 2006-11-14 Allergan, Inc Methods for the therapeutic use of cyclosporine components
US7151085B2 (en) * 2004-11-15 2006-12-19 Allergan, Inc. Therapeutic methods using cyclosporine components
TW200635954A (en) * 2004-12-17 2006-10-16 Isotechnika Inc Metabolites of cyclosporin analogs
TW200711649A (en) * 2005-06-17 2007-04-01 Combinatorx Inc Combination therapy for the treatment of immunoinflammatory disorders
US7696166B2 (en) * 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders
US7696165B2 (en) * 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne analogues for preventing or treating viral-induced disorders
WO2009018424A2 (en) * 2007-08-01 2009-02-05 Emory University Methods for determination of protein phosphatase activity, and uses in predicting therapeutic outcomes
CN101918019B (en) * 2007-10-08 2014-11-26 奥里尼亚制药有限公司 Ophthalmic compositions comprising calcineurin inhibitors or mTOR inhibitors
US20130190223A1 (en) * 2008-07-30 2013-07-25 Isotechnika Pharma Inc. Nonimmunosuppressive cyclosporine analogue molecules
KR101476626B1 (en) 2009-01-30 2014-12-26 이난타 파마슈티칼스, 인코포레이티드 Cyclosporin analogues for preventing or treating hepatitis c infection
US8481483B2 (en) * 2009-02-19 2013-07-09 Enanta Pharmaceuticals, Inc. Cyclosporin analogues
RU2012126681A (en) * 2009-06-02 2014-01-10 НИКАН ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи HUMAN FORMIL PEPTIDE RECEPTOR ANTAGONISM FOR THE TREATMENT OF DISEASES
MX338355B (en) * 2009-06-09 2016-04-13 Aurinia Pharmaceuticals Inc Topical drug delivery systems for ophthalmic use.
US8367053B2 (en) * 2009-07-09 2013-02-05 Enanta Pharmaceuticals, Inc. Cyclosporin analogues
US8349312B2 (en) * 2009-07-09 2013-01-08 Enanta Pharmaceuticals, Inc. Proline substituted cyclosporin analogues
US8685917B2 (en) * 2009-07-09 2014-04-01 Enanta Pharmaceuticals, Inc. Cyclosporin analogues
US8623814B2 (en) * 2010-02-23 2014-01-07 Enanta Pharmaceuticals, Inc. Antiviral agents
MY165152A (en) 2010-12-15 2018-02-28 Contravir Pharmaceuticals Inc Cyclosporine analogue molecules modified at amino acid 1 and 3
WO2012145427A1 (en) 2011-04-18 2012-10-26 The Trustees Of Columbia University In The City Of New York Methods to treat cancer using cyclosporine and cyclosporine derivatives
DE102011111991A1 (en) * 2011-08-30 2013-02-28 Lead Discovery Center Gmbh New cyclosporin derivatives
US9266927B2 (en) 2012-06-01 2016-02-23 Allergan, Inc. Cyclosporin A analogs
US8906853B2 (en) 2012-11-28 2014-12-09 Enanta Pharmaceuticals, Inc. [N-Me-4-hydroxyleucine]-9-cyclosporin analogues for treatment and prevention of hepatitis C infection
RU2015146211A (en) 2013-04-01 2017-05-19 Аллерган, Инк. MICROSPHERIC MEDICINAL DELIVERY SYSTEM FOR SLOW-IN-ORGANIC DISCHARGE
JP2016538317A (en) 2013-08-26 2016-12-08 エナンタ ファーマシューティカルズ インコーポレイテッド Novel cyclosporine analogues for preventing or treating hepatitis C
US9669095B2 (en) 2014-11-03 2017-06-06 Enanta Pharmaceuticals, Inc. Cyclosporin analogues for preventing or treating hepatitis C infection
WO2016112321A1 (en) 2015-01-08 2016-07-14 Allergan, Inc. Cyclosporin derivatives wherein the mebmt sidechain has been cyclized
US20190224275A1 (en) 2017-05-12 2019-07-25 Aurinia Pharmaceuticals Inc. Protocol for treatment of lupus nephritis

Citations (2)

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Publication number Priority date Publication date Assignee Title
US4554351A (en) * 1980-02-14 1985-11-19 Sandoz Ltd. Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
US4798823A (en) * 1987-06-03 1989-01-17 Merck & Co., Inc. New cyclosporin analogs with modified "C-9 amino acids"

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US5239057A (en) * 1987-03-27 1993-08-24 Abbott Laboratories Fluorescence polarization assay for cyclosporin a and metabolites and related immunogens and antibodies
US5427960A (en) * 1987-03-27 1995-06-27 Abbott Laboratories Fluorescence polarization assay for cyclosporin A and metabolites and related immunogens and antibodies
EP0296122B1 (en) 1987-06-17 1993-09-29 Sandoz Ag Cyclosporins and their use as pharmaceuticals
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WO1999018120A1 (en) 1997-10-08 1999-04-15 Isotechnika Inc. Deuterated cyclosporine analogs and their use as immunomodulating agents
JP4477777B2 (en) 1998-06-12 2010-06-09 シネクシス・インコーポレイテツド New cyclosporine

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4554351A (en) * 1980-02-14 1985-11-19 Sandoz Ltd. Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
US4798823A (en) * 1987-06-03 1989-01-17 Merck & Co., Inc. New cyclosporin analogs with modified "C-9 amino acids"

Also Published As

Publication number Publication date
US20020142946A1 (en) 2002-10-03
US6784156B2 (en) 2004-08-31
CA2439832A1 (en) 2002-09-12
US20030109426A1 (en) 2003-06-12
JP2004526719A (en) 2004-09-02
US20030186855A1 (en) 2003-10-02
WO2002069902A2 (en) 2002-09-12
US7012064B2 (en) 2006-03-14
EP1365791A2 (en) 2003-12-03

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