WO2012024584A3 - Oxysterol compounds - Google Patents
Oxysterol compounds Download PDFInfo
- 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
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 208000020084 Bone disease Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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, i.e. 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, i.e. 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Zoology (AREA)
- Endocrinology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Diabetes (AREA)
- Inorganic Chemistry (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Cardiology (AREA)
- Molecular Biology (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
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.
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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US9532994B2 (en) | 2003-08-29 | 2017-01-03 | The Regents Of The University Of California | Agents and methods for enhancing bone formation by oxysterols in combination with bone morphogenic proteins |
EP1993558B1 (en) | 2006-02-27 | 2014-07-30 | The Regents of The University of California | Oxysterol compounds and the hedgehog pathway |
CA2707663C (en) | 2007-12-03 | 2017-05-30 | The Regents Of The University Of California | Oxysterols for activation of hedgehog signaling, osteoinduction, antiadipogenesis, and wnt signaling |
JP6262723B2 (en) * | 2012-05-07 | 2018-01-17 | 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The Regents Of The University Of California | Oxysterol analog OXY133 induces bone development and hedgehog signaling and inhibits adipogenesis |
US20150140059A1 (en) * | 2012-05-07 | 2015-05-21 | The Regents Of The University Of California | Novel oxysterol analogue, oxy149, induces osteogenesis and hedgehog signaling and inhibits adipogenesis |
CA2911205A1 (en) * | 2013-05-02 | 2014-11-06 | The Regents Of The University Of California | Bone-selective osteogenic oxysterol-bone targeting agents |
WO2014206414A1 (en) * | 2013-06-28 | 2014-12-31 | Region Syddanmark | Complement factor h for use in the treatment of bone diseases |
JP6530056B2 (en) * | 2014-05-02 | 2019-06-12 | ザ・リージエンツ・オブ・ザ・ユニバーシテイ・オブ・カリフオルニア | Bone selective osteogenic oxysterol bisphosphonate analogues |
EP3617217B1 (en) | 2014-12-09 | 2022-09-07 | Warsaw Orthopedic, Inc. | Process for the production of oxysterols |
US10632230B2 (en) | 2015-07-10 | 2020-04-28 | Warsaw Orthopedic, Inc. | Implants having a high drug load of an oxysterol and methods of use |
US9878070B2 (en) | 2015-06-17 | 2018-01-30 | Warsaw Orthopedic, Inc. | Malleable implants including an oxysterol and methods of use |
US9987289B2 (en) | 2015-07-10 | 2018-06-05 | Warsaw Orthopedic, Inc. | Slow release oxysterols 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 |
EP3368543B1 (en) * | 2015-10-26 | 2020-09-23 | 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 |
MX2019007890A (en) | 2016-12-30 | 2020-01-20 | 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)
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 |
-
2011
- 2011-08-19 WO PCT/US2011/048418 patent/WO2012024584A2/en active Application Filing
Patent Citations (1)
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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