CN106232612B - 骨选择性成骨性氧固醇双膦酸盐类似物 - Google Patents

骨选择性成骨性氧固醇双膦酸盐类似物 Download PDF

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Publication number
CN106232612B
CN106232612B CN201580021530.7A CN201580021530A CN106232612B CN 106232612 B CN106232612 B CN 106232612B CN 201580021530 A CN201580021530 A CN 201580021530A CN 106232612 B CN106232612 B CN 106232612B
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Prior art keywords
compound
oxy133
bone
pharmaceutically acceptable
acceptable salt
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Expired - Fee Related
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CN201580021530.7A
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English (en)
Chinese (zh)
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CN106232612A (zh
Inventor
F·帕勒米
F·斯塔彭贝克
B·T·张伯伦
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University of California San Diego UCSD
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University of California San Diego UCSD
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/12Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/32Bones; Osteocytes; Osteoblasts; Tendons; Tenocytes; Teeth; Odontoblasts; Cartilage; Chondrocytes; Synovial membrane
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001Normal 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
    • C07J7/0015Normal 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 not substituted in position 17 alfa
    • C07J7/002Normal 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 not substituted in position 17 alfa not substituted in position 16

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Public Health (AREA)
  • Rheumatology (AREA)
  • Medicinal Chemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cell Biology (AREA)
  • Biotechnology (AREA)
  • Biomedical Technology (AREA)
  • Developmental Biology & Embryology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Zoology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
CN201580021530.7A 2014-05-02 2015-05-01 骨选择性成骨性氧固醇双膦酸盐类似物 Expired - Fee Related CN106232612B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461987739P 2014-05-02 2014-05-02
US61/987,739 2014-05-02
PCT/US2015/028917 WO2015168636A1 (en) 2014-05-02 2015-05-01 Bone-selective osteogenic oxysterol bisphosphonate analogs

Publications (2)

Publication Number Publication Date
CN106232612A CN106232612A (zh) 2016-12-14
CN106232612B true CN106232612B (zh) 2019-01-29

Family

ID=54359404

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CN201580021530.7A Expired - Fee Related CN106232612B (zh) 2014-05-02 2015-05-01 骨选择性成骨性氧固醇双膦酸盐类似物

Country Status (7)

Country Link
US (1) US10421773B2 (enExample)
EP (1) EP3137480A4 (enExample)
JP (1) JP6530056B2 (enExample)
CN (1) CN106232612B (enExample)
AU (1) AU2015252859B2 (enExample)
CA (1) CA2945404A1 (enExample)
WO (1) WO2015168636A1 (enExample)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009528291A (ja) 2006-02-27 2009-08-06 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 オキシステロール化合物及びヘッジホッグ経路
KR20150013232A (ko) 2012-05-07 2015-02-04 더 리전트 오브 더 유니버시티 오브 캘리포니아 골형성 및 헤지호그 신호전달을 유도하고 지방생성을 억제하는 옥시스테롤 유사체 oxy133
CN105263500A (zh) 2013-05-02 2016-01-20 加利福尼亚大学董事会 骨选择性成骨性氧固醇-骨靶向剂
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
US9877836B2 (en) 2015-07-10 2018-01-30 Warsaw Orthopedic, Inc. Compression resistant 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
US12171909B2 (en) 2015-07-10 2024-12-24 Warsaw Orthopedic, Inc. Implants having a drug load of an oxysterol and methods of use
US9637514B1 (en) 2015-10-26 2017-05-02 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
US10294264B2 (en) * 2017-04-21 2019-05-21 Warsaw Orthopedic, Inc. Oxysterol-therapeutic agent derivative for bone healing
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
US12049475B2 (en) * 2018-07-23 2024-07-30 Brise Pharmaceuticals Co., Ltd. Bisphosphonate drug conjugates
CN114585316A (zh) * 2019-07-24 2022-06-03 布莱阿姆青年大学 骨结合化合物

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5183815A (en) * 1991-01-22 1993-02-02 Merck & Co., Inc. Bone acting agents
EP0555845A2 (en) * 1992-02-14 1993-08-18 Mitsubishi Kasei Corporation Steroid derivatives
CN101951915A (zh) * 2007-12-03 2011-01-19 加利福尼亚大学董事会 用于刺猬蛋白信号、骨诱导、抗脂肪形成和wnt信号的激活的氧固醇
WO2013169397A1 (en) * 2012-05-07 2013-11-14 The Regents Of The University Of California Novel oxysterol analogue, oxy149, induces osteogenesis and hedgehog signaling and inhibits adipogenesis

Family Cites Families (11)

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Publication number Priority date Publication date Assignee Title
US4559157A (en) 1983-04-21 1985-12-17 Creative Products Resource Associates, Ltd. Cosmetic applicator useful for skin moisturizing
LU84979A1 (fr) 1983-08-30 1985-04-24 Oreal Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux
US4820508A (en) 1987-06-23 1989-04-11 Neutrogena Corporation Skin protective composition
US4992478A (en) 1988-04-04 1991-02-12 Warner-Lambert Company Antiinflammatory skin moisturizing composition and method of preparing same
EP0496520A1 (en) 1991-01-22 1992-07-29 Merck & Co. Inc. Novel bone acting agents
JPH06329697A (ja) * 1993-03-25 1994-11-29 Kowa Co 骨疾患治療剤
DE102004032781A1 (de) 2004-01-23 2005-08-11 Mcs Micro Carrier Systems Gmbh Bisphosphonsäurederivate
JP2009528291A (ja) * 2006-02-27 2009-08-06 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 オキシステロール化合物及びヘッジホッグ経路
AU2008218188B2 (en) * 2007-02-23 2014-03-06 University Of Louisville Research Foundation, Inc Methods and compounds for the targeted delivery of agents to bone for interaction therewith
WO2012024584A2 (en) * 2010-08-20 2012-02-23 Fate Therapeutics, Inc. Oxysterol compounds
KR20150013232A (ko) * 2012-05-07 2015-02-04 더 리전트 오브 더 유니버시티 오브 캘리포니아 골형성 및 헤지호그 신호전달을 유도하고 지방생성을 억제하는 옥시스테롤 유사체 oxy133

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5183815A (en) * 1991-01-22 1993-02-02 Merck & Co., Inc. Bone acting agents
EP0555845A2 (en) * 1992-02-14 1993-08-18 Mitsubishi Kasei Corporation Steroid derivatives
CN101951915A (zh) * 2007-12-03 2011-01-19 加利福尼亚大学董事会 用于刺猬蛋白信号、骨诱导、抗脂肪形成和wnt信号的激活的氧固醇
WO2013169397A1 (en) * 2012-05-07 2013-11-14 The Regents Of The University Of California Novel oxysterol analogue, oxy149, induces osteogenesis and hedgehog signaling and inhibits adipogenesis

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Publication number Publication date
AU2015252859B2 (en) 2019-11-07
EP3137480A4 (en) 2017-11-29
CA2945404A1 (en) 2015-11-05
JP6530056B2 (ja) 2019-06-12
JP2017514910A (ja) 2017-06-08
US20170022244A1 (en) 2017-01-26
CN106232612A (zh) 2016-12-14
WO2015168636A1 (en) 2015-11-05
EP3137480A1 (en) 2017-03-08
AU2015252859A1 (en) 2016-10-20
US10421773B2 (en) 2019-09-24

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