WO2009114010A1 - Composés de lactone macrocycliques et leurs procédés d’utilisation - Google Patents

Composés de lactone macrocycliques et leurs procédés d’utilisation Download PDF

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Publication number
WO2009114010A1
WO2009114010A1 PCT/US2008/056501 US2008056501W WO2009114010A1 WO 2009114010 A1 WO2009114010 A1 WO 2009114010A1 US 2008056501 W US2008056501 W US 2008056501W WO 2009114010 A1 WO2009114010 A1 WO 2009114010A1
Authority
WO
WIPO (PCT)
Prior art keywords
compound
group
independently
poly
member selected
Prior art date
Application number
PCT/US2008/056501
Other languages
English (en)
Inventor
John Yan
Xiaoxia Zheng
Vinayak D. Bhat
Original Assignee
Elixir Medical Corporation
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 Elixir Medical Corporation filed Critical Elixir Medical Corporation
Priority to CN200880128027.1A priority Critical patent/CN102215682A/zh
Priority to PCT/US2008/056501 priority patent/WO2009114010A1/fr
Priority to JP2010550655A priority patent/JP2011525890A/ja
Priority to BRPI0822405A priority patent/BRPI0822405A8/pt
Priority to EP08731883A priority patent/EP2254412A4/fr
Publication of WO2009114010A1 publication Critical patent/WO2009114010A1/fr
Priority to IL208026A priority patent/IL208026A0/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/10—Ophthalmic agents for accommodation disorders, e.g. myopia
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system

Abstract

La présente invention a trait à une composition pharmaceutique comprenant un excipient acceptable d’un point de vue pharmaceutique et un composé de formule (I) où R1, R2, R3, R5, R6, R8, M1, M2, M3, M4, M5, M6 et M7 sont chacun indépendamment un élément sélectionné dans le groupe comprenant H, C1-6 alkyle, OH et C1-6 hydroxyalkyle; R, R7 et R9 sont chacun indépendamment sélectionnés dans le groupe comprenant C1-6 alkoxy et OH; R10 est un élément sélectionné dans le groupe comprenant H, -OH, -OP(O)Me2, (II), (III), -O-(CH2)n-OH et -O-(CH2)m-O-(CH2)o-CH3, où les indices n et m sont chacun indépendamment des nombres entiers allant de 2 à 8 et l’indice o est un nombre entier allant de 1 à 6; chacun des éléments L1 et L4 est indépendamment sélectionné dans le groupe comprenant (IV) et (V) où chaque élément M8 est indépendamment un élément sélectionné dans le groupe comprenant C1-6 alkyle, OH et C1-6 hydroxyalkyle; les éléments L2 et L3 sont chacun indépendamment sélectionnés dans le groupe comprenant (VI), (VII) et (VIII); la présente invention a également trait à des sels, des hydrates, des isomères, des métabolites, des N-oxydes et des promédicaments de ladite composition pharmaceutique.
PCT/US2008/056501 2008-03-11 2008-03-11 Composés de lactone macrocycliques et leurs procédés d’utilisation WO2009114010A1 (fr)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CN200880128027.1A CN102215682A (zh) 2008-03-11 2008-03-11 大环内酯化合物及它们的使用方法
PCT/US2008/056501 WO2009114010A1 (fr) 2008-03-11 2008-03-11 Composés de lactone macrocycliques et leurs procédés d’utilisation
JP2010550655A JP2011525890A (ja) 2008-03-11 2008-03-11 大環状ラクトン化合物およびそれらの使用方法
BRPI0822405A BRPI0822405A8 (pt) 2008-03-11 2008-03-11 Método para tratar uma condição ou doença oftálmica, composição farmacêutica, dispositivo para o uso intracorporal, método para inibir a proliferação celular, composto, e, método para fabricar um composto
EP08731883A EP2254412A4 (fr) 2008-03-11 2008-03-11 Composés de lactone macrocycliques et leurs procédés d utilisation
IL208026A IL208026A0 (en) 2008-03-11 2010-09-06 Macrocyclic lactone compounds and methods for their use

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US2008/056501 WO2009114010A1 (fr) 2008-03-11 2008-03-11 Composés de lactone macrocycliques et leurs procédés d’utilisation

Publications (1)

Publication Number Publication Date
WO2009114010A1 true WO2009114010A1 (fr) 2009-09-17

Family

ID=41065507

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/056501 WO2009114010A1 (fr) 2008-03-11 2008-03-11 Composés de lactone macrocycliques et leurs procédés d’utilisation

Country Status (6)

Country Link
EP (1) EP2254412A4 (fr)
JP (1) JP2011525890A (fr)
CN (1) CN102215682A (fr)
BR (1) BRPI0822405A8 (fr)
IL (1) IL208026A0 (fr)
WO (1) WO2009114010A1 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10123996B2 (en) 2006-09-13 2018-11-13 Elixir Medical Corporation Macrocyclic lactone compounds and methods for their use
US10307292B2 (en) 2011-07-18 2019-06-04 Mor Research Applications Ltd Device for adjusting the intraocular pressure
US10695327B2 (en) 2006-09-13 2020-06-30 Elixir Medical Corporation Macrocyclic lactone compounds and methods for their use
US11654036B2 (en) 2020-05-26 2023-05-23 Elixir Medical Corporation Anticoagulant compounds and methods and devices for their use

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103387572B (zh) * 2013-07-17 2015-09-30 成都雅途生物技术有限公司 依维莫司杂质检测用参比标示物及其制备方法
CN107759616B (zh) * 2016-08-23 2020-11-17 上海微创医疗器械（集团）有限公司 一种化合物及其制备方法和用途
CN113801104B (zh) * 2020-06-15 2023-12-08 鲁南制药集团股份有限公司 一种依维莫司大环内酯水解杂质的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5665772A (en) * 1992-10-09 1997-09-09 Sandoz Ltd. O-alkylated rapamycin derivatives and their use, particularly as immunosuppressants
US20060229711A1 (en) * 2005-04-05 2006-10-12 Elixir Medical Corporation Degradable implantable medical devices
US20070015697A1 (en) * 2005-07-18 2007-01-18 Peyman Gholam A Enhanced ocular neuroprotection and neurostimulation
US20070059336A1 (en) * 2004-04-30 2007-03-15 Allergan, Inc. Anti-angiogenic sustained release intraocular implants and related methods

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA935112B (en) * 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
WO1994012655A1 (fr) * 1992-11-20 1994-06-09 Smithkline Beecham Corporation Procede de production de derives de rapamycine
WO2007011880A2 (fr) * 2005-07-18 2007-01-25 Minu, L.L.C. Neuro-protection/neuro-stimulation oculaire amelioree
CN101557814B (zh) * 2006-09-13 2015-05-20 万能医药公司 大环内酯化合物及它们的使用方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5665772A (en) * 1992-10-09 1997-09-09 Sandoz Ltd. O-alkylated rapamycin derivatives and their use, particularly as immunosuppressants
US20070059336A1 (en) * 2004-04-30 2007-03-15 Allergan, Inc. Anti-angiogenic sustained release intraocular implants and related methods
US20060229711A1 (en) * 2005-04-05 2006-10-12 Elixir Medical Corporation Degradable implantable medical devices
US20070015697A1 (en) * 2005-07-18 2007-01-18 Peyman Gholam A Enhanced ocular neuroprotection and neurostimulation

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
See also references of EP2254412A4 *
VIGNOT ET AL.: "mTOR-targeted therapy of cancer with rapamycin derivatives.", ANNALS OF ONCOLOGY ADVANCE ACCESS, 22 February 2005 (2005-02-22), pages 5,7,9, XP008145753 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10123996B2 (en) 2006-09-13 2018-11-13 Elixir Medical Corporation Macrocyclic lactone compounds and methods for their use
US10695327B2 (en) 2006-09-13 2020-06-30 Elixir Medical Corporation Macrocyclic lactone compounds and methods for their use
US10307292B2 (en) 2011-07-18 2019-06-04 Mor Research Applications Ltd Device for adjusting the intraocular pressure
US11654036B2 (en) 2020-05-26 2023-05-23 Elixir Medical Corporation Anticoagulant compounds and methods and devices for their use

Also Published As

Publication number Publication date
EP2254412A4 (fr) 2012-05-09
JP2011525890A (ja) 2011-09-29
BRPI0822405A8 (pt) 2018-06-05
IL208026A0 (en) 2010-12-30
EP2254412A1 (fr) 2010-12-01
BRPI0822405A2 (pt) 2018-05-15
CN102215682A (zh) 2011-10-12

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