ZA200601237B - Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin D derivatives and an estrogen agonist/antagonist - Google Patents
Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin D derivatives and an estrogen agonist/antagonist Download PDFInfo
- Publication number
- ZA200601237B ZA200601237B ZA200601237A ZA200601237A ZA200601237B ZA 200601237 B ZA200601237 B ZA 200601237B ZA 200601237 A ZA200601237 A ZA 200601237A ZA 200601237 A ZA200601237 A ZA 200601237A ZA 200601237 B ZA200601237 B ZA 200601237B
- Authority
- ZA
- South Africa
- Prior art keywords
- antagonist
- prodrug
- osteoporosis
- pharmaceutically acceptable
- dihydroxyvitamin
- Prior art date
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- 125000003431 oxalo group Chemical group 0.000 description 1
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- MPQXHAGKBWFSNV-UHFFFAOYSA-N oxidophosphanium Chemical class [PH3]=O MPQXHAGKBWFSNV-UHFFFAOYSA-N 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
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- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 239000008247 solid mixture Substances 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 108010079522 solysime Proteins 0.000 description 1
- 230000002269 spontaneous effect Effects 0.000 description 1
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- 238000004448 titration Methods 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 description 1
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- 230000008733 trauma Effects 0.000 description 1
- SMYMDRJWEFCCCI-UHFFFAOYSA-N trichloro(trichloromethoxy)methane Chemical compound ClC(Cl)(Cl)OC(Cl)(Cl)Cl SMYMDRJWEFCCCI-UHFFFAOYSA-N 0.000 description 1
- WZEOZJQLTRFNCU-UHFFFAOYSA-N trifluoro(trifluoromethoxy)methane Chemical compound FC(F)(F)OC(F)(F)F WZEOZJQLTRFNCU-UHFFFAOYSA-N 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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- 239000003981 vehicle Substances 0.000 description 1
- 102000009310 vitamin D receptors Human genes 0.000 description 1
- 108050000156 vitamin D receptors Proteins 0.000 description 1
- 235000005282 vitamin D3 Nutrition 0.000 description 1
- 239000011647 vitamin D3 Substances 0.000 description 1
- QYSXJUFSXHHAJI-YRZJJWOYSA-N vitamin D3 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)CCCC(C)C)=C\C=C1\C[C@@H](O)CCC1=C QYSXJUFSXHHAJI-YRZJJWOYSA-N 0.000 description 1
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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
- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
- A61K31/593—9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- 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
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Physical Education & Sports Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Child & Adolescent Psychology (AREA)
- Neurology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US50452103P | 2003-09-19 | 2003-09-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200601237B true ZA200601237B (en) | 2007-05-30 |
Family
ID=34375516
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200601237A ZA200601237B (en) | 2003-09-19 | 2006-02-10 | Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin D derivatives and an estrogen agonist/antagonist |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20050070512A1 (zh) |
| EP (1) | EP1667692A1 (zh) |
| JP (1) | JP2007505881A (zh) |
| KR (1) | KR20060040746A (zh) |
| CN (1) | CN100496501C (zh) |
| AU (1) | AU2004273658A1 (zh) |
| BR (1) | BRPI0414448A (zh) |
| CA (1) | CA2539361A1 (zh) |
| CO (1) | CO5670328A2 (zh) |
| IL (1) | IL173621A0 (zh) |
| MX (1) | MXPA06003122A (zh) |
| NO (1) | NO20061702L (zh) |
| RU (1) | RU2331425C2 (zh) |
| TW (1) | TW200522967A (zh) |
| WO (1) | WO2005027924A1 (zh) |
| ZA (1) | ZA200601237B (zh) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7122533B2 (en) * | 1999-11-29 | 2006-10-17 | The United States Of America As Represented By The Department Of Health And Human Services | Cosalane compounds and methods for their use |
| MXPA06005887A (es) | 2003-11-25 | 2006-06-27 | Wisconsin Alumni Res Found | Analogos de vitamina d para la prevencion y el tratamiento de la obesidad. |
| WO2005051396A2 (en) * | 2003-11-25 | 2005-06-09 | Deltanoid Pharmaceuticals, Inc. | Methods for reducing body fat using vitamin d compounds |
| AU2006213722B2 (en) * | 2005-02-11 | 2011-09-22 | Wisconsin Alumni Research Foundation | 2-methylene-19-nor-(20S-24epi)-1alpha,25-dihydroxyvitamin-D2 |
| WO2006086613A2 (en) * | 2005-02-11 | 2006-08-17 | Wisconsin Alumni Research Foundation | 2-METHYLENE-19-NOR- (20S-24S) - 1α, 25-D IHYDROXYVITAMIN-D2 |
| EP1865965A4 (en) * | 2005-03-29 | 2010-06-02 | Wisconsin Alumni Res Found | 2-METHYLENE-19-NOR- (23S) -25-DEHYDRO-1-HYDROXYVITAMINE-D3-26,23-LACTONE AND 2-METHYLENE-19-NOR- (23R) -25-DEHYDRO-1-HYDROXYVITAMINE-D3- 26.23-lACTONE |
| US7803789B2 (en) * | 2006-02-02 | 2010-09-28 | Wisconsin Alumni Research Foundation | Vitamin D analog—RAK, methods and uses thereof |
| US7528122B2 (en) * | 2006-02-02 | 2009-05-05 | Wisconsin Alumni Research Foundation | Vitamin D analog—NEL, methods and uses thereof |
| US20090036429A1 (en) * | 2006-02-17 | 2009-02-05 | Ohler Norman E | Hydroxypiperidine Derivatives and Uses Thereof |
| EP2141994A4 (en) * | 2007-04-26 | 2011-05-18 | Avalon Pharmaceuticals | POLYCYCLIC COMPOUNDS AND USES THEREOF |
| US8664206B2 (en) | 2010-03-23 | 2014-03-04 | Wisconsin Alumni Research Foundation | Diastereomers of 2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin D3 |
| WO2011119610A2 (en) | 2010-03-23 | 2011-09-29 | Wisconsin Alumni Research Foundation | (20S)-2-METHYLENE-19-NOR-22-DIMETHYL-1α,25- DIHYDROXYVITAMIN D3 AND (20R)-2-METHYLENE-19-NOR-22- DIMETHYL-1α,25-HYDROXYVITAMIN D3 |
| JP5931845B2 (ja) * | 2010-03-23 | 2016-06-08 | ウイスコンシン アラムニ リサーチ ファンデーション | ２−メチレン−１９−ノル−２２−メチル−１α，２５−ジヒドロキシビタミンＤ３のジアステレオマー |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE637389A (zh) * | 1962-09-13 | |||
| US3822287A (en) * | 1969-04-17 | 1974-07-02 | Rexall Drug Chemical | Process for preparation of substituted 3,4-(diphenyl)chromans |
| DE2860900D1 (en) * | 1977-08-22 | 1981-11-05 | Ici Plc | Triphenylalkene derivatives, process for their preparation and pharmaceutical compositions containing them |
| DE3046719C2 (de) * | 1980-12-11 | 1983-02-17 | Klinge Pharma GmbH, 8000 München | 1,1,2-Triphenyl-but-1-en-Derivate, Verfahren zu ihrer Herstellung und Arzneimittel |
| US4418068A (en) * | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
| GB2126576B (en) * | 1982-06-25 | 1985-06-19 | Farmos Group Limited | Alkane and alkene derivatives |
| DE3762617D1 (de) * | 1986-09-11 | 1990-06-13 | Nat Res Dev | Tamoxifenderivate. |
| US5086191A (en) * | 1991-05-28 | 1992-02-04 | Wisconsin Alumni Research Foundation | Intermediates for the synthesis of 19-nor vitamin D compounds |
| TW366342B (en) * | 1992-07-28 | 1999-08-11 | Lilly Co Eli | The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss |
| JP2898882B2 (ja) * | 1993-04-05 | 1999-06-02 | ウイスコンシン アラムナイ リサーチ フオンデーシヨン | ２−位に置換基を有する１９−ノル−ビタミンｄ３ 化合物 |
| US5478847A (en) * | 1994-03-02 | 1995-12-26 | Eli Lilly And Company | Methods of use for inhibiting bone loss and lowering serum cholesterol |
| US7501441B1 (en) * | 1994-09-20 | 2009-03-10 | Eli Lilly And Company | Naphthyl compounds, intermediates, processes, compositions, and methods |
| US5552412A (en) * | 1995-01-09 | 1996-09-03 | Pfizer Inc | 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis |
| US5510357A (en) * | 1995-02-28 | 1996-04-23 | Eli Lilly And Company | Benzothiophene compounds as anti-estrogenic agents |
| US5998402A (en) * | 1996-04-19 | 1999-12-07 | American Home Products Corporation | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents |
| US5780497A (en) * | 1996-04-19 | 1998-07-14 | American Home Products Corporation | 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents |
| US5985910A (en) * | 1996-04-19 | 1999-11-16 | American Home Products Corporation | 3- [4- (2- Phenyl-Indole-1-ylmethyl) Phenyl]- Acrylamides as estrogenic agents |
| US5880137A (en) * | 1996-04-19 | 1999-03-09 | American Home Products Corporation | 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents |
| US6306844B1 (en) * | 1997-03-17 | 2001-10-23 | Wisconsin Alumni Research Foundation | Use of 2α-methyl-19-nor-20(S)-1α, 25-dihydroxyvitamin D3 to increase bone strength |
| US5843928A (en) * | 1997-03-17 | 1998-12-01 | Wisconsin Alumni Research Foundation | 2-alkylidene-19-nor-vitamin D compounds |
| US6392071B1 (en) * | 1997-03-17 | 2002-05-21 | Wisconsin Alumni: Research Foundation | 26,27-homologated-20-EPI-2-alkylidene-19-nor-vitamin D compounds |
| AUPO727097A0 (en) * | 1997-06-10 | 1997-07-03 | Unisearch Limited | Method of treatment of hepatoma and pharmaceutical compositions for use therein |
| DE19916419B4 (de) * | 1999-04-08 | 2005-06-16 | Schering Ag | Kombinationspräparat aus Vitamin-D-Metaboliten oder Vitamin-D-Analoga und einem Östrogenpartialagonisten zur Behandlung von Osteoporose |
| CN1217664C (zh) * | 2000-07-14 | 2005-09-07 | 威斯康星校友研究基金会 | 2－亚甲基－19－去甲－20(S)－1α，25－二羟维生素D3增加骨强度的用途 |
| JP2004530684A (ja) * | 2001-05-10 | 2004-10-07 | メルク エンド カムパニー インコーポレーテッド | エストロゲン受容体モジュレーター |
| US20030195175A1 (en) * | 2002-03-25 | 2003-10-16 | Deluca Hector F. | Use of carbon-2-modified-vitamin D analogs to induce the formation of new bone |
| US7259143B2 (en) * | 2002-09-05 | 2007-08-21 | Wisconsin Alumni Research Foundation | Method of extending the dose range of vitamin D compounds |
-
2004
- 2004-09-06 CA CA002539361A patent/CA2539361A1/en not_active Abandoned
- 2004-09-06 WO PCT/IB2004/002900 patent/WO2005027924A1/en active Application Filing
- 2004-09-06 AU AU2004273658A patent/AU2004273658A1/en not_active Abandoned
- 2004-09-06 MX MXPA06003122A patent/MXPA06003122A/es not_active Application Discontinuation
- 2004-09-06 CN CNB2004800268325A patent/CN100496501C/zh not_active Expired - Fee Related
- 2004-09-06 RU RU2006107652/15A patent/RU2331425C2/ru not_active IP Right Cessation
- 2004-09-06 KR KR1020067005416A patent/KR20060040746A/ko not_active Application Discontinuation
- 2004-09-06 JP JP2006526713A patent/JP2007505881A/ja active Pending
- 2004-09-06 BR BRPI0414448-1A patent/BRPI0414448A/pt not_active Application Discontinuation
- 2004-09-06 EP EP04769299A patent/EP1667692A1/en not_active Withdrawn
- 2004-09-16 US US10/943,568 patent/US20050070512A1/en not_active Abandoned
- 2004-09-17 TW TW093128107A patent/TW200522967A/zh unknown
-
2006
- 2006-02-08 IL IL173621A patent/IL173621A0/en unknown
- 2006-02-10 ZA ZA200601237A patent/ZA200601237B/en unknown
- 2006-03-03 CO CO06021161A patent/CO5670328A2/es not_active Application Discontinuation
- 2006-04-18 NO NO20061702A patent/NO20061702L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| CN1852720A (zh) | 2006-10-25 |
| TW200522967A (en) | 2005-07-16 |
| CO5670328A2 (es) | 2006-08-31 |
| KR20060040746A (ko) | 2006-05-10 |
| WO2005027924A1 (en) | 2005-03-31 |
| IL173621A0 (en) | 2006-07-05 |
| RU2331425C2 (ru) | 2008-08-20 |
| NO20061702L (no) | 2006-06-19 |
| US20050070512A1 (en) | 2005-03-31 |
| AU2004273658A1 (en) | 2005-03-31 |
| BRPI0414448A (pt) | 2006-11-14 |
| CN100496501C (zh) | 2009-06-10 |
| RU2006107652A (ru) | 2007-10-27 |
| JP2007505881A (ja) | 2007-03-15 |
| MXPA06003122A (es) | 2006-05-31 |
| CA2539361A1 (en) | 2005-03-31 |
| EP1667692A1 (en) | 2006-06-14 |
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