FI112226B - Ej solvaterad, kristallin 6-hydroxi-2-(4-hydroxifenyl)-3-[4-(2-piperidinoetoxi)bensoyl]benso[b]tiofenhydroklorid - Google Patents
Ej solvaterad, kristallin 6-hydroxi-2-(4-hydroxifenyl)-3-[4-(2-piperidinoetoxi)bensoyl]benso[b]tiofenhydroklorid Download PDFInfo
- Publication number
- FI112226B FI112226B FI954402A FI954402A FI112226B FI 112226 B FI112226 B FI 112226B FI 954402 A FI954402 A FI 954402A FI 954402 A FI954402 A FI 954402A FI 112226 B FI112226 B FI 112226B
- Authority
- FI
- Finland
- Prior art keywords
- crystalline
- hydroxy
- benzoyl
- benzo
- reaction
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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- 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
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- 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
- A61P15/18—Feminine contraceptives
-
- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Claims (5)
1. Ej solvaterad, kristallin 6-hydroxi-2-(4-hyd-roxifenyl)-3-[4-(2-piperidinoetoxi)bensoyl]benso [b]tiofen-5 hydroklorid, kännetecknad av att den har väsentligen följande röntgendiffraktionsmönster, som erhällits medelst kopparstraining d-linje avständ I/I0 (Angström) (xl.OO) 13 ,3864 71,31 9,3598 33,16 8,4625 2,08 7,3888 7,57 15 6,9907 5,80 6,6346 51,04 6,1717 29,57 5,9975 5,67 5,9135 9,87 20 5,6467 38,47 . . 5,4773 10,54 :,/ 5,2994 4,74 4,8680 4,03 4,7910 5,98 ί* 25 4,6614 57,50 4,5052 5,75 4,3701 9,03 4,2516 69,99 4,2059 57,64 30 4,1740 65,07 4,0819 12,44 3,9673 22,53 : 3,9318 100,00 3,8775 9,07 ! 35 3,7096 33,38 3,6561 21,65 112226 d-linje avständ (Angstrom) (xlOO) 3,5576 3,36 3,5037 7,97 5 3,4522 18,02 3,4138 4,65 3,2738 10,23 3,1857 8,90 3,1333 6,24 10 3,0831 9,43 3,0025 12,13 2,9437 4,96 2,8642 7,70 2,7904 11,95 15 2,7246 3,05 2,6652 3,32 2,5882 7,30
2. Farmaceutisk komposition, kännetecknad av 20 att den innehäller en kristallin förening enligt patentkrav 1 samt en eller flera farmaceutiskt godtagbara bärare, ut-’· ί spädningsmedel eller utdrygningsmedel.
3. Kristallin förening enligt patentkrav 1 för an- tik’ vändning som läkemedel. ;* 25 4. Förfarande för framställning av ej solvaterad ; kristallin 6-hydroxi-2-(4-hydroxifenyl)-3-[4-(2-piperidino- » · » . etoxi)bensoyl]benso[b]tiofenhydroklorid, som har väsentli- gen följande röntgendiffraktionsmönster, som erhällits me- ..... deist koppar s training * · » * * 39 1 12226 d-linje avständ I/I0 (Angstrom) (xlOO) 5 13 ,3864 71,31 9,3598 33,16 8,4625 2,08 7,3888 7,57 6,9907 5,80 10 6,6346 51,04 6,1717 29,57 5,9975 5,67 5,9135 9,87 5,6467 38,47 15 5,4773 10,54 5,2994 4,74 4,8680 4,03 4,7910 5,98 4,6614 57,50 ! 20 4,5052 5,75 4,3701 9,03 V* 4,2516 69,99 4,2059 57,64 ·;· 4,1740 65,07 .·. 25 4,0819 12,44 "!·. 3,9673 22,53 I·; 3,9318 100,00 3 ,8775 9,07 3,7096 33 ,38 ;* 30 3 ,6561 21,65 3 ,5576 3 ,36 *: 3,5037 7,97 ·. 3,4522 18,02 3,4138 4,65 40 1 12226 d-linje avständ I/I0 (Angstrom) (χΙΟΟ) 3,2738 10,23 5 3,1857 8,90 3,1333 6,24 3,0831 9,43 3,0025 12,13 2,9437 4,96 10 2,8642 7,70 2,7904 11,95 2,7246 3,05 2,6652 3,32 2,5882 7,30 15 kännetecknat av att (a) bensotiofen med forraeln • · R ’· · II ’· ·’ 2 0 där ·· : R4 betecknar Ci^-alkoxi, och ; R5 betecknar Ci_4-alkyl, • · acyleras med ett acyleringsmedel med formeln > ♦ esAOL : och2ch2n^ -hx R2 m ,v 25 ". där • t R6 betecknar klor, brom eller hydroxyl, HX är HC1 eller HBr; och ' * R2 och R3 bildar tillsammans med den intilliggande 30 kväveatomen en piperidinogrupp; 41 112226 i närvaro av BX'3, där X' är klor eller brom; (b) fenolgrupperna av stegets (a) acyleringsprodukt dealkyleras genom att de bringas att reagera med ett över-skott av BX'3( där X1 är som ovan definierats; och 5 (c) ett kristallint soivat av en förening med föl- jande formel isoleras V" OCH2CH2n( 1 · HX I där
10 R1 betecknar hydroxyl; och HX, R2 och R3 är som ovan definierats; (d) nämnda kristallina soivat bringas att reagera i metanol eller i en blandning av metanol och vatten med cir-ka en basekvivalent; 15 (e) stegets (d) lösning utlöses eventuellt med ett alifatiskt kolvätelösningsmedel; (f) cirka en ekvivalent av klorvätesyra tillsätts stegets (d) eller (e) metanol lösning; och : : (g) den ej solvaterade, kristallina föreningen iso- ·1· 2 0 leras. k 5. Förfarande enligt patentkrav 4, känneteck- « 1 > # : ,·, nat av att R4 betecknar metoxi, R5 betecknar metyl, R6 be- ,··, tecknar klor, HX är HC1, BX' 3 är BC13, det alifatiska kolvä- * · telösningsmedlet är hexan eller heptan, och basen är natri- ,, , 2 5 umhydroxid. > < · • · » I • · » » · » 4 · • t » » · I · » I · • » 1 1 1 · · • ·
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US30832594 | 1994-09-19 | ||
US08/308,325 US5629425A (en) | 1994-09-19 | 1994-09-19 | Haloalkyl hemisolvates of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-piperidinoethoxy)-benzoyl]benzo[b]thiophene |
US42791495A | 1995-04-26 | 1995-04-26 | |
US42791495 | 1995-04-26 |
Publications (3)
Publication Number | Publication Date |
---|---|
FI954402A0 FI954402A0 (sv) | 1995-09-18 |
FI954402A FI954402A (sv) | 1996-03-20 |
FI112226B true FI112226B (sv) | 2003-11-14 |
Family
ID=26976194
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FI954402A FI112226B (sv) | 1994-09-19 | 1995-09-18 | Ej solvaterad, kristallin 6-hydroxi-2-(4-hydroxifenyl)-3-[4-(2-piperidinoetoxi)bensoyl]benso[b]tiofenhydroklorid |
FI954403A FI121424B (sv) | 1994-09-19 | 1995-09-18 | Förfarande för framställning av ett kristallint solvat av 6-hydroxi-2-(4-hydroxifenyl)-3-[4-(2-piperidinoetoxi)bensoyl]benso[b]-tiofenhydroklorid och de kristallina1,2-dikloretan- och 1,2,3-triklorpropansolvaten |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FI954403A FI121424B (sv) | 1994-09-19 | 1995-09-18 | Förfarande för framställning av ett kristallint solvat av 6-hydroxi-2-(4-hydroxifenyl)-3-[4-(2-piperidinoetoxi)bensoyl]benso[b]-tiofenhydroklorid och de kristallina1,2-dikloretan- och 1,2,3-triklorpropansolvaten |
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Families Citing this family (72)
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1995
- 1995-06-02 CO CO95023869A patent/CO4410190A1/es unknown
- 1995-06-02 CO CO95023870A patent/CO4410191A1/es unknown
- 1995-06-05 TW TW084105613A patent/TW412534B/zh not_active IP Right Cessation
- 1995-06-06 US US08/467,485 patent/US5731327A/en not_active Expired - Lifetime
- 1995-06-06 US US08/469,093 patent/US6399778B1/en not_active Expired - Fee Related
- 1995-06-06 US US08/469,961 patent/US6472531B1/en not_active Expired - Lifetime
- 1995-06-07 PE PE1995270674A patent/PE14796A1/es not_active Application Discontinuation
- 1995-06-07 PE PE1995270673A patent/PE32796A1/es not_active IP Right Cessation
- 1995-09-13 ES ES09501774A patent/ES2109882B1/es not_active Revoked
- 1995-09-13 ES ES009501775A patent/ES2129293B1/es not_active Expired - Fee Related
- 1995-09-14 UA UA95094168A patent/UA44240C2/uk unknown
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- 1995-09-14 NL NL1001196A patent/NL1001196C2/nl active Search and Examination
- 1995-09-14 NL NL1001194A patent/NL1001194C2/nl active Search and Examination
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- 1995-09-15 KR KR1019950030209A patent/KR100367376B1/ko active IP Right Grant
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- 1995-09-15 KR KR1019950030210A patent/KR100381346B1/ko active IP Right Grant
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- 1995-09-18 BE BE9500761A patent/BE1009626A3/fr active
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- 1995-09-18 JP JP7238209A patent/JPH08193081A/ja active Pending
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1997
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1998
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2002
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MM | Patent lapsed |