RU2006132352A - Кристаллическая полиморфная форма базедоксифен ацетата - Google Patents
Кристаллическая полиморфная форма базедоксифен ацетата Download PDFInfo
- Publication number
- RU2006132352A RU2006132352A RU2006132352/04A RU2006132352A RU2006132352A RU 2006132352 A RU2006132352 A RU 2006132352A RU 2006132352/04 A RU2006132352/04 A RU 2006132352/04A RU 2006132352 A RU2006132352 A RU 2006132352A RU 2006132352 A RU2006132352 A RU 2006132352A
- Authority
- RU
- Russia
- Prior art keywords
- approximately
- polymorphic form
- mixture
- bazedoxifene acetate
- composition
- Prior art date
Links
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 title 1
- 239000013078 crystal Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 claims 45
- OMZAMQFQZMUNTP-UHFFFAOYSA-N acetic acid;1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol Chemical compound CC(O)=O.C=1C=C(OCCN2CCCCCC2)C=CC=1CN1C2=CC=C(O)C=C2C(C)=C1C1=CC=C(O)C=C1 OMZAMQFQZMUNTP-UHFFFAOYSA-N 0.000 claims 24
- 229960003713 bazedoxifene acetate Drugs 0.000 claims 24
- 238000000034 method Methods 0.000 claims 22
- 241000124008 Mammalia Species 0.000 claims 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 6
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 6
- 238000001228 spectrum Methods 0.000 claims 6
- 239000002904 solvent Substances 0.000 claims 5
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 229940011871 estrogen Drugs 0.000 claims 4
- 239000000262 estrogen Substances 0.000 claims 4
- 238000002441 X-ray diffraction Methods 0.000 claims 3
- 239000000843 powder Substances 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 230000001457 vasomotor Effects 0.000 claims 3
- 206010065687 Bone loss Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 235000012000 cholesterol Nutrition 0.000 claims 2
- 230000007812 deficiency Effects 0.000 claims 2
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 2
- 230000002357 endometrial effect Effects 0.000 claims 2
- 238000002329 infrared spectrum Methods 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 230000035755 proliferation Effects 0.000 claims 2
- 210000001519 tissue Anatomy 0.000 claims 2
- 229940035811 conjugated estrogen Drugs 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 1
- 230000003637 steroidlike Effects 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/12—Radicals substituted by oxygen atoms
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/32—Antioestrogens
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Dermatology (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Indole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US56058404P | 2004-04-07 | 2004-04-07 | |
| US60/560,584 | 2004-04-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2006132352A true RU2006132352A (ru) | 2008-05-20 |
Family
ID=34965585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2006132352/04A RU2006132352A (ru) | 2004-04-07 | 2005-04-06 | Кристаллическая полиморфная форма базедоксифен ацетата |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US7683052B2 (https=) |
| EP (1) | EP1732889A1 (https=) |
| JP (2) | JP2007532548A (https=) |
| KR (1) | KR20070004815A (https=) |
| CN (1) | CN1938271A (https=) |
| AR (1) | AR048683A1 (https=) |
| AU (1) | AU2005233114A1 (https=) |
| BR (1) | BRPI0509257A (https=) |
| CA (1) | CA2561296A1 (https=) |
| EC (1) | ECSP066910A (https=) |
| GT (1) | GT200500080A (https=) |
| IL (1) | IL178101A0 (https=) |
| NO (1) | NO20065046L (https=) |
| PA (1) | PA8629201A1 (https=) |
| PE (1) | PE20060173A1 (https=) |
| RU (1) | RU2006132352A (https=) |
| TW (1) | TW200536845A (https=) |
| UA (1) | UA86055C2 (https=) |
| WO (1) | WO2005100314A1 (https=) |
| ZA (1) | ZA200608361B (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20070188A1 (es) * | 2005-06-29 | 2007-03-16 | Wyeth Corp | Formulaciones de estrogenos conjugados y bazedoxifeno |
| AU2006283121A1 (en) * | 2005-08-24 | 2007-03-01 | Wyeth | Bazedoxifene acetate formulations and manufacturing process thereof |
| PE20090100A1 (es) * | 2007-03-30 | 2009-02-26 | Wyeth Corp | Metodos de separacion y deteccion de acetato de bacedoxifeno en composiciones farmaceuticas |
| CZ302358B6 (cs) * | 2007-07-25 | 2011-03-30 | Zentiva, A. S. | Nové soli bazedoxifenu |
| CN101977897A (zh) * | 2008-02-11 | 2011-02-16 | 惠氏有限责任公司 | 制备乙酸巴多昔芬的多晶型a的方法 |
| WO2009102778A1 (en) * | 2008-02-11 | 2009-08-20 | Wyeth | Amorphous polymorph of bazedoxifene acetate |
| ITMI20091109A1 (it) * | 2009-06-23 | 2010-12-24 | Wyeth Corp | Forma polimorfa d di bazedoxifene acetato e metodi per la sua preparazione |
| AR078785A1 (es) | 2009-10-27 | 2011-11-30 | Wyeth Llc | Formulaciones de bazedoxifeno con antioxidantes |
| EP2407467A1 (de) | 2010-07-14 | 2012-01-18 | Sandoz Ag | Kristalline Verbindung von 1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol und Milchsäure |
| WO2012007453A1 (en) | 2010-07-14 | 2012-01-19 | Sandoz Ag | Crystalline compound of 1-[4-(2-azepan-1-ylethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1h-indol-5-ol |
| EP2616463A4 (en) | 2010-09-14 | 2014-01-08 | Reddys Lab Ltd Dr | PREPARATION OF CRYSTALLINE BAZEDOXIFES AND THEIR SALTS |
| EP2471770A1 (en) | 2010-12-28 | 2012-07-04 | Sandoz Ag | Method of preparing polymorphic pure form A of bazedoxifene acetate |
| CN103864664A (zh) * | 2012-12-18 | 2014-06-18 | 江苏柯菲平医药有限公司 | 巴多昔芬乙酸盐新晶型及其制备方法 |
| US9751835B2 (en) | 2013-05-15 | 2017-09-05 | Indiana University Research And Technology Corporation | Processes and intermediates for preparing indole pharmaceuticals |
| CN103864665B (zh) * | 2014-03-04 | 2016-03-02 | 苏州特瑞药业有限公司 | 醋酸巴多昔芬的制备方法 |
| CN104030963A (zh) * | 2014-06-30 | 2014-09-10 | 四川大学 | 一种巴多昔芬醋酸盐晶型a的制备方法 |
| CN111004165A (zh) * | 2019-12-03 | 2020-04-14 | 南京正济医药研究有限公司 | 一种醋酸巴多昔芬晶型a的制备方法 |
| US11246874B1 (en) | 2021-04-20 | 2022-02-15 | Oxygen Biotech LLC | Treatment of COVID-19 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| DE69707189T2 (de) | 1996-04-19 | 2002-06-20 | American Home Products Corp., Madison | Östrogene Verbindungen |
| TW397821B (en) | 1996-04-19 | 2000-07-11 | American Home Produits Corp | 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof |
| 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 |
| US5998402A (en) | 1996-04-19 | 1999-12-07 | American Home Products Corporation | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents |
| NZ503793A (en) * | 1997-10-15 | 2002-10-25 | Wyeth Corp | Novel aryloxy-alkyl-dialkylamines and processes for preparing these compounds |
| US6005102A (en) | 1997-10-15 | 1999-12-21 | American Home Products Corporation | Aryloxy-alkyl-dialkylamines |
| US6479535B1 (en) | 1998-05-15 | 2002-11-12 | Wyeth | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indole and estrogen formulations |
| AR029538A1 (es) | 2000-07-06 | 2003-07-02 | Wyeth Corp | Composiciones farmaceuticas de agentes estrogenicos |
| EP1336602A1 (en) | 2002-02-13 | 2003-08-20 | Giovanni Scaramuzzino | Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases |
| IL165395A0 (en) | 2002-06-25 | 2006-01-15 | Wyeth Corp | Use of thio-oxubdile derivatives in treatment of hormone-related conditions |
| PE20060676A1 (es) | 2004-04-07 | 2006-07-24 | Wyeth Corp | Polimorfo cristalino de acetato de bazedoxifeno |
-
2005
- 2005-04-06 GT GT200500080A patent/GT200500080A/es unknown
- 2005-04-06 CA CA002561296A patent/CA2561296A1/en not_active Abandoned
- 2005-04-06 CN CNA2005800103454A patent/CN1938271A/zh not_active Withdrawn
- 2005-04-06 WO PCT/US2005/011423 patent/WO2005100314A1/en not_active Ceased
- 2005-04-06 BR BRPI0509257-4A patent/BRPI0509257A/pt not_active IP Right Cessation
- 2005-04-06 US US11/100,998 patent/US7683052B2/en active Active
- 2005-04-06 AR ARP050101366A patent/AR048683A1/es unknown
- 2005-04-06 TW TW094110849A patent/TW200536845A/zh unknown
- 2005-04-06 AU AU2005233114A patent/AU2005233114A1/en not_active Withdrawn
- 2005-04-06 JP JP2007507417A patent/JP2007532548A/ja not_active Abandoned
- 2005-04-06 PE PE2005000385A patent/PE20060173A1/es not_active Application Discontinuation
- 2005-04-06 EP EP05735042A patent/EP1732889A1/en not_active Withdrawn
- 2005-04-06 RU RU2006132352/04A patent/RU2006132352A/ru not_active Application Discontinuation
- 2005-04-06 UA UAA200610608A patent/UA86055C2/ru unknown
- 2005-04-06 KR KR1020067020645A patent/KR20070004815A/ko not_active Withdrawn
- 2005-04-06 PA PA20058629201A patent/PA8629201A1/es unknown
-
2006
- 2006-09-14 IL IL178101A patent/IL178101A0/en unknown
- 2006-10-06 ZA ZA200608361A patent/ZA200608361B/xx unknown
- 2006-10-06 EC EC2006006910A patent/ECSP066910A/es unknown
- 2006-11-02 NO NO20065046A patent/NO20065046L/no not_active Application Discontinuation
-
2008
- 2008-06-30 JP JP2008171116A patent/JP2009007361A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| NO20065046L (no) | 2006-11-06 |
| GT200500080A (es) | 2005-10-31 |
| US20050250762A1 (en) | 2005-11-10 |
| JP2007532548A (ja) | 2007-11-15 |
| PE20060173A1 (es) | 2006-04-12 |
| JP2009007361A (ja) | 2009-01-15 |
| BRPI0509257A (pt) | 2007-09-11 |
| CA2561296A1 (en) | 2005-10-27 |
| TW200536845A (en) | 2005-11-16 |
| EP1732889A1 (en) | 2006-12-20 |
| US7683052B2 (en) | 2010-03-23 |
| AR048683A1 (es) | 2006-05-17 |
| ZA200608361B (en) | 2010-03-31 |
| PA8629201A1 (es) | 2005-11-25 |
| WO2005100314A1 (en) | 2005-10-27 |
| IL178101A0 (en) | 2006-12-31 |
| ECSP066910A (es) | 2006-12-20 |
| KR20070004815A (ko) | 2007-01-09 |
| UA86055C2 (ru) | 2009-03-25 |
| AU2005233114A1 (en) | 2005-10-27 |
| CN1938271A (zh) | 2007-03-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20091102 |