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ES2195049T3 - Analogos de vitamina d3 fluorados. - Google Patents

Analogos de vitamina d3 fluorados.

Info

Publication number
ES2195049T3
ES2195049T3 ES97107868T ES97107868T ES2195049T3 ES 2195049 T3 ES2195049 T3 ES 2195049T3 ES 97107868 T ES97107868 T ES 97107868T ES 97107868 T ES97107868 T ES 97107868T ES 2195049 T3 ES2195049 T3 ES 2195049T3
Authority
ES
Spain
Prior art keywords
sub
link
hydrogen
double link
fluoroalquilo
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES97107868T
Other languages
English (en)
Inventor
Percy Sarwood Manchand
Jr John Joseph Nestor
Milan Radoje Uskokovic
Brian Henry Vickery
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
HOFFMANN LA ROCHE
F Hoffmann La Roche AG
Original Assignee
HOFFMANN LA ROCHE
F Hoffmann La Roche AG
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 HOFFMANN LA ROCHE, F Hoffmann La Roche AG filed Critical HOFFMANN LA ROCHE
Application granted granted Critical
Publication of ES2195049T3 publication Critical patent/ES2195049T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C401/00Irradiation products of cholesterol or its derivatives; Vitamin D derivatives, 9,10-seco cyclopenta[a]phenanthrene or analogues obtained by chemical preparation without irradiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/59Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Nutrition Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

LOS NUEVOS ANALOGOS DE VITAMINA D3 DE FORMULA I DONDE: X ES (H,H) O = CH{SUB,2}; R{SUB,1} Y R{SUB,2} SON, INDEPENDIENTEMENTE ENTRE SI, HIDROGENO, (C{SUB,1} OROALQUILO, O R{SUB,1} Y R{SUB,2} JUNTO CON C C{SUB,3} B,1} Y R{SUB,2} JUNTOS FORMAN = CH{SUB,2}; R{SUB,3} Y R{SUB,4} SON, INDEPENDIENTEMENTE ENTRE SI, (C{SUB,1} C{SUB,4}) ALQUILO O FLUOROALQUILO, O R{SUB,3} Y R{SUB,4} JUNTO CON C UN (C{SUB,3} ES UN ENLACE SENCILLO O UN DOBLE ENLACE; Y B ES UN DOBLE ENLACE O UN TRIPLE ENLACE; EXCEPTO QUE: (I) CUANDO X ES = CH{SUB,2}, R{SUB,3} Y R{SUB,4} SON CADA UNO DE ELLOS CF{SUB,3}, A ES UN DOBLE ENLACE Y UNO DE R{SUB,1} O R{SUB,2} ES HIDROGENO, ENTONCES EL OTRO R{SUB,1} O R{SUB,2} NO PUEDE SER CH{SUB,3}; (II) CUANDO X ES = CH{SUB,2}, R{SUB,3} Y R{SUB,4} SON CADA UNO DE ELLOS UN (C{SUB,1} ,2} ES HIDROGENO, ENTONCES R{SUB,1} NO PUEDE SER CH{SUB,3}; (III) CUANDO X ES = CH{SUB,2}, R{SUB,3} Y R{SUB,4} SON CADA UNO DE ELLOS UN (C{SUB,1} B,3}; (IV) CUANDO X ES = CH{SUB,2}, UNO DE R{SUB,3} O R{SUB,4} ES UN CF{SUB,3}, A ES UN DOBLE ENLACE, R{SUB,1} ES CH{SUB,3} Y R{SUB,2} ES HIDROGENO, ENTONCES EL OTRO R{SUB,3} O R{SUB,4} NO PUEDE SER CH{SUB,3}; Y (V) CUANDO X ES (H,H), R{SUB,3} Y R{SUB,4} SON CADA UNO DE ELLOS CF{SUB,3}, A ES UN DOBLE ENLACE, B ES UN TRIPLE ENLACE Y R{SUB,2} ES HIDROGENO, ENTONCES R{SUB,1} NO PUEDE SER CH{SUB,3}, Y LOS COMPUESTOS DE LA FORMULA I ANTERIOR DONDE: X ES (H,H) O = CH{SUB,2}; R{SUB,1} Y R{SUB,2} SON, INDEPENDIENTEMENTE ENTRE SI, HIDROGENO, (C{SUB,1} UILO O FLUOROALQUILO, O R{SUB,1} Y R{SUB,2} JUNTO CON C ORMAN UN (C{SUB,3} LO, O R{SUB,1} Y R{SUB,2} JUNTOS FORMAN = CH{SUB,2}; R{SUB,3} Y R{SUB,4} SON, INDEPENDIENTEMENTE ENTRE SI, UN (C{SUB,1} SUB,4}) ALQUILO O FLUOROALQUILO, O R{SUB,3} Y R{SUB,4} JUNTO CON C FLUOROALQUILO; A ES UN ENLACE SENCILLO O UN DOBLE ENLACE; Y B ES UN DOBLE ENLACE O UN TRIPLE ENLACE; EXCEPTO QUE DONDE R{SUB,3} Y R{SUB,4} SON CADA UNO DE ELLOS CF{SUB,3} Y A ES UN DOBLE ENLACE Y B ES UN TRIPLE ENLACE Y R{SUB,2} ES HIDROGENO, ENTONCES R{SUB,1} NOPUEDE SER CH{SUB,3}, SON UTILES EN EL TRATAMIENTO DE LA OSTEOPOROSIS.
ES97107868T 1996-05-23 1997-05-14 Analogos de vitamina d3 fluorados. Expired - Lifetime ES2195049T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US1821996P 1996-05-23 1996-05-23
US3990197P 1997-03-19 1997-03-19

Publications (1)

Publication Number Publication Date
ES2195049T3 true ES2195049T3 (es) 2003-12-01

Family

ID=26690870

Family Applications (1)

Application Number Title Priority Date Filing Date
ES97107868T Expired - Lifetime ES2195049T3 (es) 1996-05-23 1997-05-14 Analogos de vitamina d3 fluorados.

Country Status (26)

Country Link
EP (1) EP0808832B1 (es)
JP (1) JP2859248B2 (es)
KR (1) KR100253961B1 (es)
CN (1) CN100402497C (es)
AR (1) AR007776A1 (es)
AT (1) ATE238278T1 (es)
AU (1) AU733970B2 (es)
BR (1) BR9703385A (es)
CA (1) CA2205315C (es)
CO (1) CO4940503A1 (es)
CZ (1) CZ157797A3 (es)
DE (1) DE69721123T2 (es)
DK (1) DK0808832T3 (es)
ES (1) ES2195049T3 (es)
HR (1) HRP970272A2 (es)
HU (1) HUP9700928A3 (es)
IL (1) IL120844A0 (es)
MA (1) MA24250A1 (es)
NO (1) NO972278L (es)
NZ (1) NZ314840A (es)
PE (1) PE66798A1 (es)
PL (1) PL320130A1 (es)
PT (1) PT808832E (es)
SG (1) SG70010A1 (es)
TR (1) TR199700416A2 (es)
YU (1) YU20097A (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6008209A (en) * 1997-04-28 1999-12-28 Hoffmann-La Roche Inc. Method of using vitamin D3 analogs with bis C-20 side chains
DE19935771A1 (de) 1999-07-23 2001-02-01 Schering Ag Neue Vitamin D-Derivate mit cyclischen Substrukturen in den Seitenketten, Verfahren und Zwischenprodukte zu ihrer Herstellung und die Verwendung zur Herstellung von Arzneimitteln
WO2002013832A1 (fr) * 2000-08-17 2002-02-21 Chugai Seiyaku Kabushiki Kaisha Agent therapeutique destine au traitement de l'osteoporose
CA2459789A1 (en) * 2001-09-21 2003-04-03 F. Hoffmann-La Roche Ag 3-desoxy-vitamin d3 analog esters
PT103177A (pt) 2003-09-24 2005-03-31 Bioxell Spa 1-alfa-fluoro-25-hidroxi-16,23e-dieno-26,27-bis-homo-20-epi-colecalciferol, seus sais ou esteres e sua utilizacao no fabrico de medicamentos
WO2006036813A2 (en) * 2004-09-24 2006-04-06 Bioxell S.P.A. 20-cycloalkyl,26,27-alkyl/haloalkyl vitamin d3 compounds and methods of use thereof
CA2601914A1 (en) * 2005-03-23 2006-09-28 Bioxell S.P.A. 20-alkyl, gemini vitamin d3 compounds and methods of use thereof
CN104829510B (zh) 2010-10-25 2016-05-04 帝人制药株式会社 23-炔-维生素d3衍生物

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4141746A1 (de) * 1991-12-13 1993-06-17 Schering Ag 20-methyl-substituierte vitamin d-derivate
DE4220757A1 (de) * 1992-06-24 1994-01-05 Schering Ag Derivate in der Vitamin D-Reihe mit Modifikationen in der 20-Position, Verfahren zu ihrer Herstellung, Zwischenprodukte für dieses Verfahren, diese Derivate enthaltende pharmazeutische Präparate sowie deren Verwendung zur Herstellung von Arzneimitteln
US5428029A (en) * 1993-11-24 1995-06-27 Hoffmann-La Roche Inc. Vitamin D3 fluorinated analogs
US5384314B1 (en) * 1994-03-11 1997-08-05 Hoffmann La Roche 1alpha-fluoro-25-hydroxy-16-ene-23-yne-cholecalciferol
AU7295696A (en) * 1995-10-27 1997-05-22 F. Hoffmann-La Roche Ag Pharmaceutical composition for treating osteoporosis

Also Published As

Publication number Publication date
EP0808832B1 (en) 2003-04-23
HRP970272A2 (en) 1998-04-30
JP2859248B2 (ja) 1999-02-17
KR100253961B1 (ko) 2000-04-15
SG70010A1 (en) 2000-01-25
MX9703775A (es) 1998-06-30
CN100402497C (zh) 2008-07-16
PE66798A1 (es) 1998-10-22
CO4940503A1 (es) 2000-07-24
TR199700416A2 (xx) 1997-12-21
EP0808832A2 (en) 1997-11-26
CZ157797A3 (en) 1997-12-17
NZ314840A (en) 1998-11-25
NO972278L (no) 1997-11-24
AR007776A1 (es) 1999-11-24
IL120844A0 (en) 1997-09-30
HUP9700928A3 (en) 1999-07-28
PL320130A1 (en) 1997-11-24
EP0808832A3 (en) 1999-02-03
HU9700928D0 (en) 1997-07-28
CN1172801A (zh) 1998-02-11
MA24250A1 (fr) 1998-04-01
ATE238278T1 (de) 2003-05-15
DE69721123D1 (de) 2003-05-28
DK0808832T3 (da) 2003-08-11
NO972278D0 (no) 1997-05-20
AU2357697A (en) 1997-11-27
PT808832E (pt) 2003-07-31
HUP9700928A2 (hu) 1998-01-28
JPH1045714A (ja) 1998-02-17
CA2205315A1 (en) 1997-11-23
DE69721123T2 (de) 2004-01-08
KR970074764A (ko) 1997-12-10
BR9703385A (pt) 1998-09-15
AU733970B2 (en) 2001-05-31
CA2205315C (en) 2006-10-24
YU20097A (sh) 1999-09-27

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