WO2012024584A3 - Oxysterol compounds - Google Patents

Oxysterol compounds Download PDF

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Publication number
WO2012024584A3
WO2012024584A3 PCT/US2011/048418 US2011048418W WO2012024584A3 WO 2012024584 A3 WO2012024584 A3 WO 2012024584A3 US 2011048418 W US2011048418 W US 2011048418W WO 2012024584 A3 WO2012024584 A3 WO 2012024584A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
disclosed
disorders
oxysterol compounds
oxysterol
Prior art date
Application number
PCT/US2011/048418
Other languages
French (fr)
Other versions
WO2012024584A2 (en
Inventor
Wei Xiao
Matt Epperson
Francine Farouz
Frank Stappenbeck
Eugene Thorsett
Original Assignee
Fate Therapeutics, Inc.
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 Fate Therapeutics, Inc. filed Critical Fate Therapeutics, Inc.
Publication of WO2012024584A2 publication Critical patent/WO2012024584A2/en
Publication of WO2012024584A3 publication Critical patent/WO2012024584A3/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/16—Fluorine compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/18—Growth factors; Growth regulators
    • A61K38/1841—Transforming growth factor [TGF]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/29—Parathyroid hormone (parathormone); Parathyroid hormone-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
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/30—Insulin-like growth factors (Somatomedins), e.g. IGF-1, IGF-2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0066—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by a carbon atom forming part of an amide group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group

Abstract

Compounds for use in the treatment of bone disorders, obesity, cardiovascular disorders and neurological disorders are disclosed. The compounds have the following structure (I), including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X and R1 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
PCT/US2011/048418 2010-08-20 2011-08-19 Oxysterol compounds WO2012024584A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37554910P 2010-08-20 2010-08-20
US61/375,549 2010-08-20

Publications (2)

Publication Number Publication Date
WO2012024584A2 WO2012024584A2 (en) 2012-02-23
WO2012024584A3 true WO2012024584A3 (en) 2012-04-12

Family

ID=44543861

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2011/048418 WO2012024584A2 (en) 2010-08-20 2011-08-19 Oxysterol compounds

Country Status (1)

Country Link
WO (1) WO2012024584A2 (en)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005020928A2 (en) 2003-08-29 2005-03-10 The Regents Of The University Of California Agents and methods for enhancing bone formation by oxysterols in combination with bone morphogenic proteins
WO2007098281A2 (en) 2006-02-27 2007-08-30 Regents Of The University Of California Oxysterol compounds and the hedgehog pathway
EP2231164A1 (en) 2007-12-03 2010-09-29 The Regents of the University of California Oxysterols for activation of hedgehog signaling, osteoinduction, antiadipogenesis, and wnt signaling
RU2014149153A (en) * 2012-05-07 2016-06-27 Те Риджентс Оф Те Юниверсити Оф Калифорния THE NEW ANALOGUE OF OXISTEROL, OXY149, INDUCES OSTEOGENESIS AND THE HEDGEHOG SIGNAL WAY AND INHIBITS LIPOGENESIS
RU2632191C2 (en) * 2012-05-07 2017-10-03 Те Риджентс Оф Те Юниверсити Оф Калифорния Oxy133 OXYSTEROL ANALOGUE INDUCTS OSTEOGENESIS AND SIGNAL WAY HEDGEHOG AND INHIBITED LIPOGENESIS
JP2016517888A (en) * 2013-05-02 2016-06-20 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Oxysterol bone targeting drug for osteoselective bone formation
WO2014206414A1 (en) * 2013-06-28 2014-12-31 Region Syddanmark Complement factor h for use in the treatment of bone diseases
WO2015168636A1 (en) * 2014-05-02 2015-11-05 The Regents Of The University Of California Bone-selective osteogenic oxysterol bisphosphonate analogs
EP3229809B1 (en) 2014-12-09 2019-11-27 Warsaw Orthopedic, Inc. Compounds and methods involving sterols
US10632230B2 (en) 2015-07-10 2020-04-28 Warsaw Orthopedic, Inc. Implants having a high drug load of an oxysterol and methods of use
US9987289B2 (en) * 2015-07-10 2018-06-05 Warsaw Orthopedic, Inc. Slow release oxysterols and methods of use
US9878070B2 (en) 2015-06-17 2018-01-30 Warsaw Orthopedic, Inc. Malleable implants including an oxysterol and methods of use
US9877836B2 (en) 2015-07-10 2018-01-30 Warsaw Orthopedic, Inc. Compression resistant implants including an oxysterol and methods of use
US9637514B1 (en) 2015-10-26 2017-05-02 MAX BioPharma, Inc. Oxysterols and hedgehog signaling
WO2017074957A1 (en) * 2015-10-26 2017-05-04 MAX BioPharma, Inc. Oxysterols and hedgehog signaling
US20170275330A1 (en) * 2016-03-28 2017-09-28 Warsaw Orthopedic, Inc. Polymorphic forms of an oxysterol and methods of making them
US10688222B2 (en) 2016-11-21 2020-06-23 Warsaw Orthopedic, Inc. Lyophilized moldable implants containing an oxysterol
US11384114B2 (en) 2016-12-09 2022-07-12 Warsaw Orthopedic, Inc. Polymorphic forms of an oxysterol and methods of making them
EP3562827A1 (en) 2016-12-30 2019-11-06 Frequency Therapeutics, Inc. 1h-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells
US10434106B2 (en) 2017-05-19 2019-10-08 Warsaw Orthopedic, Inc. Oxysterol-statin compounds for bone growth
US11464888B2 (en) * 2017-06-12 2022-10-11 Warsaw Orthopedic, Inc. Moldable formulations containing an oxysterol in an acellular tissue matrix
CN111269291B (en) * 2020-03-20 2023-11-21 三峡大学 Synthesis of oligopeptide and application of oligopeptide in medicines for inhibiting citrus saprophytic bacteria penicillium digitatum

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009073186A1 (en) * 2007-12-03 2009-06-11 The Regents Of The University Of California Oxsterols for activation of hedgehog signaling, osteoinduction, antiadipogenesis, and wnt signaling

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009073186A1 (en) * 2007-12-03 2009-06-11 The Regents Of The University Of California Oxsterols for activation of hedgehog signaling, osteoinduction, antiadipogenesis, and wnt signaling

Also Published As

Publication number Publication date
WO2012024584A2 (en) 2012-02-23

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