PE20060173A1 - Polimorfo cristalino de acetato de bazedoxifeno - Google Patents
Polimorfo cristalino de acetato de bazedoxifenoInfo
- Publication number
- PE20060173A1 PE20060173A1 PE2005000385A PE2005000385A PE20060173A1 PE 20060173 A1 PE20060173 A1 PE 20060173A1 PE 2005000385 A PE2005000385 A PE 2005000385A PE 2005000385 A PE2005000385 A PE 2005000385A PE 20060173 A1 PE20060173 A1 PE 20060173A1
- Authority
- PE
- Peru
- Prior art keywords
- crystalline polymorph
- deficiency
- refers
- polymorph
- syndrome
- Prior art date
Links
- 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 title 1
- 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 abstract 2
- 230000007812 deficiency Effects 0.000 abstract 2
- 208000011580 syndromic disease Diseases 0.000 abstract 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 abstract 1
- 206010006187 Breast cancer Diseases 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 238000002441 X-ray diffraction Methods 0.000 abstract 1
- 235000012000 cholesterol Nutrition 0.000 abstract 1
- 238000000113 differential scanning calorimetry Methods 0.000 abstract 1
- 102000015694 estrogen receptors Human genes 0.000 abstract 1
- 108010038795 estrogen receptors Proteins 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000843 powder Substances 0.000 abstract 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)
- 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)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Hematology (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)
Abstract
SE REFIERE A UN POLIMORFO CRISTALINO (FORMA B) DE ACETATO DE BASEDOXIFENO (1-[4-(2-AZEPAN-1-IL-ETOXI)-BENCIL]-2-(4-HIDROXI-FENIL)-3-METIL-1H-INDOL-5-OL ACETICO, CARACTERIZADO POR UN PATRON DE DIFRACCION DE RAYOS X EN POLVO QUE COMPRENDE PICOS CARACTERISTICOS , EN TERMINOS DE 2 THETA, A ALREDEDOR DE 13,3 Y 20,8° Y TIENE UN TRAZADO DE CALORIMETRIA DIFERENCIAL DE BARRIDO QUE MUESTRA UN MAXIMO ALREDEDOR DE 181°C. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHO POLIMORFO ES MODULADOR SELECTIVO DEL RECEPTOR DE ESTROGENO UTILES EN EL TRATAMIENTO DE SINDROME ASOCIADO CON DEFICIENCIA O EXCESO DE ESTROGENO, DESARROLLO ANORMAL DE TEJIDOS ENDOMETRIALES, DISMINUCION DE COLESTEROL, CANCER MAMARIO, ENTRE OTROS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US56058404P | 2004-04-07 | 2004-04-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20060173A1 true PE20060173A1 (es) | 2006-04-12 |
Family
ID=34965585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2005000385A PE20060173A1 (es) | 2004-04-07 | 2005-04-06 | Polimorfo cristalino de acetato de bazedoxifeno |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US7683052B2 (es) |
| EP (1) | EP1732889A1 (es) |
| JP (2) | JP2007532548A (es) |
| KR (1) | KR20070004815A (es) |
| CN (1) | CN1938271A (es) |
| AR (1) | AR048683A1 (es) |
| AU (1) | AU2005233114A1 (es) |
| BR (1) | BRPI0509257A (es) |
| CA (1) | CA2561296A1 (es) |
| EC (1) | ECSP066910A (es) |
| GT (1) | GT200500080A (es) |
| IL (1) | IL178101A0 (es) |
| NO (1) | NO20065046L (es) |
| PA (1) | PA8629201A1 (es) |
| PE (1) | PE20060173A1 (es) |
| RU (1) | RU2006132352A (es) |
| TW (1) | TW200536845A (es) |
| UA (1) | UA86055C2 (es) |
| WO (1) | WO2005100314A1 (es) |
| ZA (1) | ZA200608361B (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20080031037A (ko) * | 2005-06-29 | 2008-04-07 | 와이어쓰 | 결합형 에스트로겐과 바제독시펜의 제형 |
| RU2417084C2 (ru) | 2005-08-24 | 2011-04-27 | Вайет | Составы, содержащие базедоксифен ацетат |
| 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 |
| WO2009102778A1 (en) * | 2008-02-11 | 2009-08-20 | Wyeth | Amorphous polymorph of bazedoxifene acetate |
| JP5199395B2 (ja) * | 2008-02-11 | 2013-05-15 | ワイス・エルエルシー | バゼドキシフェン酢酸塩の多形体aの調製方法 |
| 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 |
| 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 |
| 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 |
| WO2012037187A2 (en) | 2010-09-14 | 2012-03-22 | Dr. Reddy's Laboratories Ltd. | Preparation of crystalline bazedoxifene and its 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 |
| WO2014186325A1 (en) | 2013-05-15 | 2014-11-20 | 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 |
|---|---|---|---|---|
| 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 |
| ATE206701T1 (de) | 1996-04-19 | 2001-10-15 | American Home Prod | Östrogene verbindungen |
| 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 |
| 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 |
| US6005102A (en) * | 1997-10-15 | 1999-12-21 | American Home Products Corporation | Aryloxy-alkyl-dialkylamines |
| AR015183A1 (es) * | 1997-10-15 | 2001-04-18 | Wyeth Corp | Ariloxi-alquil-dialquilaminas y procesos para su produccion |
| 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 |
| MXPA04012419A (es) * | 2002-06-25 | 2005-04-19 | Wyeth Corp | Uso de derivados de tio-oxindol en el tratamiento de condiciones relacionadas con la hormona. |
| US7683051B2 (en) | 2004-04-07 | 2010-03-23 | Wyeth | Crystalline polymorph of bazedoxifene acetate |
-
2005
- 2005-04-06 PA PA20058629201A patent/PA8629201A1/es unknown
- 2005-04-06 CN CNA2005800103454A patent/CN1938271A/zh not_active Withdrawn
- 2005-04-06 JP JP2007507417A patent/JP2007532548A/ja not_active Abandoned
- 2005-04-06 GT GT200500080A patent/GT200500080A/es unknown
- 2005-04-06 EP EP05735042A patent/EP1732889A1/en not_active Withdrawn
- 2005-04-06 PE PE2005000385A patent/PE20060173A1/es not_active Application Discontinuation
- 2005-04-06 WO PCT/US2005/011423 patent/WO2005100314A1/en not_active Ceased
- 2005-04-06 CA CA002561296A patent/CA2561296A1/en not_active Abandoned
- 2005-04-06 AU AU2005233114A patent/AU2005233114A1/en not_active Withdrawn
- 2005-04-06 KR KR1020067020645A patent/KR20070004815A/ko not_active Withdrawn
- 2005-04-06 TW TW094110849A patent/TW200536845A/zh unknown
- 2005-04-06 AR ARP050101366A patent/AR048683A1/es unknown
- 2005-04-06 UA UAA200610608A patent/UA86055C2/ru unknown
- 2005-04-06 RU RU2006132352/04A patent/RU2006132352A/ru not_active Application Discontinuation
- 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
-
2006
- 2006-09-14 IL IL178101A patent/IL178101A0/en unknown
- 2006-10-06 EC EC2006006910A patent/ECSP066910A/es unknown
- 2006-10-06 ZA ZA200608361A patent/ZA200608361B/xx 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 |
|---|---|
| AR048683A1 (es) | 2006-05-17 |
| WO2005100314A1 (en) | 2005-10-27 |
| JP2007532548A (ja) | 2007-11-15 |
| JP2009007361A (ja) | 2009-01-15 |
| US20050250762A1 (en) | 2005-11-10 |
| IL178101A0 (en) | 2006-12-31 |
| CA2561296A1 (en) | 2005-10-27 |
| GT200500080A (es) | 2005-10-31 |
| UA86055C2 (ru) | 2009-03-25 |
| NO20065046L (no) | 2006-11-06 |
| ZA200608361B (en) | 2010-03-31 |
| ECSP066910A (es) | 2006-12-20 |
| CN1938271A (zh) | 2007-03-28 |
| TW200536845A (en) | 2005-11-16 |
| BRPI0509257A (pt) | 2007-09-11 |
| PA8629201A1 (es) | 2005-11-25 |
| EP1732889A1 (en) | 2006-12-20 |
| RU2006132352A (ru) | 2008-05-20 |
| AU2005233114A1 (en) | 2005-10-27 |
| US7683052B2 (en) | 2010-03-23 |
| KR20070004815A (ko) | 2007-01-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |