HUP0001172A2 - Amorf benzotiofének, eljárás ezek előállítására, valamint amorf benzotioféneket tartalmazó gyógyászati készítmények - Google Patents
Amorf benzotiofének, eljárás ezek előállítására, valamint amorf benzotioféneket tartalmazó gyógyászati készítményekInfo
- Publication number
- HUP0001172A2 HUP0001172A2 HU0001172A HUP0001172A HUP0001172A2 HU P0001172 A2 HUP0001172 A2 HU P0001172A2 HU 0001172 A HU0001172 A HU 0001172A HU P0001172 A HUP0001172 A HU P0001172A HU P0001172 A2 HUP0001172 A2 HU P0001172A2
- Authority
- HU
- Hungary
- Prior art keywords
- general formula
- compounds
- amorphous
- amorphous forms
- methods
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 4
- 238000002360 preparation method Methods 0.000 title abstract 3
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical class C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 6
- 208000006386 Bone Resorption Diseases 0.000 abstract 1
- 206010065687 Bone loss Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 208000031226 Hyperlipidaemia Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 230000024279 bone resorption Effects 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 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 1
- 230000001419 dependent effect Effects 0.000 abstract 1
- 229940011871 estrogen Drugs 0.000 abstract 1
- 239000000262 estrogen Substances 0.000 abstract 1
- -1 hexamethyleneimino Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 238000001694 spray drying Methods 0.000 abstract 1
- 208000024891 symptom Diseases 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
- C07D333/56—Radicals substituted by oxygen atoms
-
- 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
- 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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
A találmány tárgyát képezik az (I) általános képletű vegyületek ésezek gyógyászatilag megfelelő sói vagy szolvátjai amorf alakjai éseljárás ezek előállítására, az (I) általános képletben R1 és R3jelentése egymástól függetlenül hidrogénatom, -CH3, -CO-(1-6szénatomos alkil)- vagy -COAr csoport, ahol Ar jelentése adott esetbenszubsztituált fenilcsoport; R2 jelentése pirrolidinil-, hexametilén-imino- vagy piperidinilcsoport; és a találmány szerinti eljárást olymódon végzik, hogy az (I) általános képletű vegyület kristályosalakját megfelelő oldószerben feloldják, majd az oldatot porlasztásosszárításnak vetik alá, amikoris az (I) általános képletű vegyületamorf alakját kapják. A találmány tárgyához tartoznak az evegyületeket tartalmazó gyógyászati készítmények is. Az (I) általánosképletű vegyületek amorf alakjait tartalmazó gyógyászatikészítményekkel eredményesen kezelhetők a klimax nyomán fellépőosteoporosis, a csontveszteség vagy csontreszorpció; az (I) általánosképletű vegyületek amorf alakjai eredményesen adhatók a szérumkoleszterinszint csökkentésére, a klimax tünetegyüttes tüneteinekenyhítésére, a különböző szív- és érrendszeri betegségek, minthiperlipidémia, továbbá az ösztrogéntől függő rák kezelésére. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2483196P | 1996-08-28 | 1996-08-28 | |
| PCT/US1997/014768 WO1998008513A1 (en) | 1996-08-28 | 1997-08-22 | Amorphous benzothiophenes, methods of preparation, and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0001172A2 true HUP0001172A2 (hu) | 2001-06-28 |
| HUP0001172A3 HUP0001172A3 (en) | 2002-01-28 |
Family
ID=21822611
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0001172A HUP0001172A3 (en) | 1996-08-28 | 1997-08-22 | Amorphous benzothiophenes, methods of preparation, and methods of use |
Country Status (25)
| Country | Link |
|---|---|
| EP (1) | EP0826682B1 (hu) |
| JP (1) | JP2002514174A (hu) |
| KR (1) | KR20000035941A (hu) |
| CN (1) | CN1244124A (hu) |
| AR (2) | AR009333A1 (hu) |
| AT (1) | ATE234295T1 (hu) |
| AU (1) | AU723987B2 (hu) |
| BR (1) | BR9713176A (hu) |
| CA (1) | CA2263175A1 (hu) |
| CO (1) | CO4650039A1 (hu) |
| CZ (1) | CZ64399A3 (hu) |
| DE (1) | DE69719640T2 (hu) |
| EA (1) | EA002022B1 (hu) |
| ES (1) | ES2195089T3 (hu) |
| HU (1) | HUP0001172A3 (hu) |
| IL (1) | IL128641A (hu) |
| IN (1) | IN182940B (hu) |
| NO (1) | NO990914L (hu) |
| NZ (1) | NZ333839A (hu) |
| PE (1) | PE108598A1 (hu) |
| PL (1) | PL333356A1 (hu) |
| TR (1) | TR199900403T2 (hu) |
| WO (1) | WO1998008513A1 (hu) |
| YU (1) | YU10599A (hu) |
| ZA (1) | ZA977617B (hu) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR19980033284A (ko) * | 1996-10-30 | 1998-07-25 | 피터지.스트링거 | 개선된 유방암 예방법 |
| US7005428B1 (en) | 1998-06-11 | 2006-02-28 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
| US6465445B1 (en) | 1998-06-11 | 2002-10-15 | Endorecherche, Inc. | Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors |
| FI982733A (fi) * | 1998-12-17 | 2000-06-18 | Orion Yhtymae Oyj | Trifenyylietyleeniantiestrogeenien liukoisia koostumuksia |
| EP1832583A1 (en) * | 2002-09-30 | 2007-09-12 | A/S GEA Farmaceutisk Fabrik | Novel raloxifene sulphuric acid addition salts and/or solvates thereof, and pharmaceutical compositions comprising these |
| US20050008704A1 (en) * | 2003-07-11 | 2005-01-13 | Ray Anup Kumar | Pharmaceutical composition for solubility enhancement of hydrophobic drugs |
| JPWO2007072869A1 (ja) * | 2005-12-21 | 2009-06-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | １，２−ジヒドロピリジン化合物の非晶質体 |
| WO2008047105A1 (en) | 2006-10-17 | 2008-04-24 | Cipla Limited | Crystalline form of benzothiophene compound and process for preparation thereof |
| EP2448562B1 (en) | 2009-07-02 | 2013-11-06 | Synthon B.V. | Raloxifene composition |
| WO2011099942A1 (en) | 2010-02-09 | 2011-08-18 | Silverstone Pharma | New addition salts of raloxifene, process for the preparation thereof and use thereof in therapy |
| ITMI20121821A1 (it) * | 2012-10-25 | 2014-04-26 | Erregierre Spa | Composizione farmaceutica solubile in acqua a base di un sale di raloxifene |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4230862A (en) * | 1975-10-28 | 1980-10-28 | Eli Lilly And Company | Antifertility compounds |
| JP3157882B2 (ja) * | 1991-11-15 | 2001-04-16 | 帝国臓器製薬株式会社 | 新規なベンゾチオフエン誘導体 |
| TW366342B (en) * | 1992-07-28 | 1999-08-11 | Lilly Co Eli | The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss |
| US5482949A (en) * | 1993-03-19 | 1996-01-09 | Eli Lilly And Company | Sulfonate derivatives of 3-aroylbenzo[b]thiophenes |
| US6756388B1 (en) * | 1993-10-12 | 2004-06-29 | Pfizer Inc. | Benzothiophenes and related compounds as estrogen agonists |
| US5631369A (en) * | 1994-08-31 | 1997-05-20 | Eli Lilly And Company | Process for preparing benzoic acid derivative intermediates and benzothiophene pharmaceutical agents |
-
1997
- 1997-08-22 DE DE69719640T patent/DE69719640T2/de not_active Expired - Fee Related
- 1997-08-22 BR BR9713176-8A patent/BR9713176A/pt unknown
- 1997-08-22 PE PE1997000750A patent/PE108598A1/es not_active Application Discontinuation
- 1997-08-22 PL PL97333356A patent/PL333356A1/xx unknown
- 1997-08-22 AU AU42335/97A patent/AU723987B2/en not_active Ceased
- 1997-08-22 EP EP97306426A patent/EP0826682B1/en not_active Expired - Lifetime
- 1997-08-22 TR TR1999/00403T patent/TR199900403T2/xx unknown
- 1997-08-22 NZ NZ333839A patent/NZ333839A/en unknown
- 1997-08-22 IN IN1549CA1997 patent/IN182940B/en unknown
- 1997-08-22 AT AT97306426T patent/ATE234295T1/de not_active IP Right Cessation
- 1997-08-22 WO PCT/US1997/014768 patent/WO1998008513A1/en not_active Application Discontinuation
- 1997-08-22 JP JP51174498A patent/JP2002514174A/ja active Pending
- 1997-08-22 CA CA002263175A patent/CA2263175A1/en not_active Abandoned
- 1997-08-22 HU HU0001172A patent/HUP0001172A3/hu unknown
- 1997-08-22 CZ CZ99643A patent/CZ64399A3/cs unknown
- 1997-08-22 EA EA199900235A patent/EA002022B1/ru not_active IP Right Cessation
- 1997-08-22 KR KR1019997001682A patent/KR20000035941A/ko not_active Application Discontinuation
- 1997-08-22 IL IL12864197A patent/IL128641A/en not_active IP Right Cessation
- 1997-08-22 ES ES97306426T patent/ES2195089T3/es not_active Expired - Lifetime
- 1997-08-22 YU YU10599A patent/YU10599A/sh unknown
- 1997-08-22 CN CN97197434A patent/CN1244124A/zh active Pending
- 1997-08-25 ZA ZA977617A patent/ZA977617B/xx unknown
- 1997-08-26 CO CO97049147A patent/CO4650039A1/es unknown
- 1997-08-26 AR ARP970103869A patent/AR009333A1/es not_active Application Discontinuation
- 1997-08-26 AR ARP970103870A patent/AR009334A1/es unknown
-
1999
- 1999-02-25 NO NO990914A patent/NO990914L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| HUP0001172A3 (en) | 2002-01-28 |
| DE69719640D1 (de) | 2003-04-17 |
| TR199900403T2 (xx) | 2002-01-21 |
| YU10599A (sh) | 2001-07-10 |
| AR009333A1 (es) | 2000-04-12 |
| NZ333839A (en) | 2001-06-29 |
| PE108598A1 (es) | 1999-01-13 |
| IL128641A0 (en) | 2000-01-31 |
| EP0826682A1 (en) | 1998-03-04 |
| IL128641A (en) | 2001-10-31 |
| CO4650039A1 (es) | 1998-09-03 |
| NO990914D0 (no) | 1999-02-25 |
| KR20000035941A (ko) | 2000-06-26 |
| ZA977617B (en) | 1999-02-25 |
| CZ64399A3 (cs) | 1999-05-12 |
| BR9713176A (pt) | 2000-02-08 |
| EA002022B1 (ru) | 2001-12-24 |
| EA199900235A1 (ru) | 1999-08-26 |
| ATE234295T1 (de) | 2003-03-15 |
| PL333356A1 (en) | 1999-12-06 |
| CN1244124A (zh) | 2000-02-09 |
| EP0826682B1 (en) | 2003-03-12 |
| AU723987B2 (en) | 2000-09-07 |
| WO1998008513A1 (en) | 1998-03-05 |
| DE69719640T2 (de) | 2003-11-06 |
| IN182940B (hu) | 1999-08-14 |
| NO990914L (no) | 1999-02-25 |
| AR009334A1 (es) | 2000-04-12 |
| ES2195089T3 (es) | 2003-12-01 |
| CA2263175A1 (en) | 1998-03-05 |
| AU4233597A (en) | 1998-03-19 |
| JP2002514174A (ja) | 2002-05-14 |
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