YU11896A - Benzothiophene compounds, intermediates, compositions containing them - Google Patents
Benzothiophene compounds, intermediates, compositions containing themInfo
- Publication number
- YU11896A YU11896A YU11896A YU11896A YU11896A YU 11896 A YU11896 A YU 11896A YU 11896 A YU11896 A YU 11896A YU 11896 A YU11896 A YU 11896A YU 11896 A YU11896 A YU 11896A
- Authority
- YU
- Yugoslavia
- Prior art keywords
- alkyl
- compounds
- formula
- pyrrolidinyl
- protecting group
- Prior art date
Links
Classifications
-
- 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
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
-
- 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
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- 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
- A61K31/4025—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 not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
-
- 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
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
- C07D333/64—Oxygen atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Dati pronalazak daje farmaceutski aktivna jedinjenja formule I u kojoj, R1 je -H, -OH, -O(C1-C4 alkil), -OCOC6H5, -OCO(C1-C6 alkil), ili -OSO(C2-C6 alkil); R2 je -H, -OH, -O(C1-C4 alkil), -OCOC6H5, -OCO(C1-C6 alkil), ili -OSO(C2-C6 alkil) ili halogen; R3 je 1-piperidinil, 1-pirolidinil, metil-1-pirolidinil, dimetil-1-pirolidinil, 4-morfolino, dimetilamino, dietilamino, diizopropilamino, ili 1-heksametilenaimino; n je 2 ili 3; i z je -O- ili -S-; ili njihovu farmaceutski prihvatljivu so. Takođe su data jedinjnja formule II R1a je -H ili -OR7a, pri čemu R7a je -H ili hidroksi zaštitna grupa; R2a je -H, halogen, ili -OR8a u kojem R8a je -H ili hidroksi zaštitna grupa; R6 je -H, ili hidroksi zaštitna grupa koji se može selektivno ukloniti; Z je -O- ili -S-; ili njihova farmaceutski prihvatljiva so, koji su korisni intermedijari za dobijanje jedinjenja formule I. Dalje su obezbeđene farmaceutske kompozicije jedinjenja formule I i postupci upotrebe jedinjenja formule I, za, inter alia, ublažavanje simptoma post menopauznog sindroma i hormonalno zavisnog kancera, posebno kancera dojki.The present invention provides pharmaceutically active compounds of formula I wherein, R 1 is -H, -OH, -O (C 1 -C 4 alkyl), -OCOC 6 H 5, -OCO (C 1 -C 6 alkyl), or -OSO (C 2 -C 6 alkyl); R 2 is -H, -OH, -O (C 1 -C 4 alkyl), -OCOC 6 H 5, -OCO (C 1 -C 6 alkyl), or -OSO (C 2 -C 6 alkyl) or halogen; R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and z is -O- or -S-; or a pharmaceutically acceptable salt thereof. Also provided are compounds of formula II R 1a is -H or -OR 7a, wherein R 7a is -H or a hydroxy protecting group; R 2a is -H, halogen, or -OR 8a wherein R 8a is -H or a hydroxy protecting group; R6 is -H, or a selectively removable hydroxy protecting group; Z is -O- or -S-; or a pharmaceutically acceptable salt thereof, which are useful intermediates for the preparation of compounds of formula I. Further provided are pharmaceutical compositions of compounds of formula I and methods of using compounds of formula I, inter alia, to alleviate symptoms of post menopausal syndrome and hormone-dependent cancer, especially breast cancer.
Applications Claiming Priority (8)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/396,401 US5510357A (en) | 1995-02-28 | 1995-02-28 | Benzothiophene compounds as anti-estrogenic agents |
US55276095A | 1995-11-03 | 1995-11-03 | |
US08/552,636 US5723474A (en) | 1995-02-28 | 1995-11-03 | Benzothiophene compounds, intermediates, compositions, and methods |
US08/552,564 US5998441A (en) | 1995-02-28 | 1995-11-03 | Benzothiophene compounds, intermediates, compositions, and methods |
US08/552,890 US5919800A (en) | 1995-02-28 | 1995-11-03 | Benzothiophene compounds, intermediates, compositions, and methods |
US08/554,223 US5856340A (en) | 1995-02-28 | 1995-11-03 | Method of treating estrogen dependent cancers |
US08/552,679 US5856339A (en) | 1995-02-28 | 1995-11-03 | Benzothiophene compounds, intermediates, compositions, and methods |
US08/552,565 US5977093A (en) | 1995-02-28 | 1995-11-03 | Benzothiophene compounds, intermediates, compositions, and methods |
Publications (2)
Publication Number | Publication Date |
---|---|
YU11896A true YU11896A (en) | 1998-12-23 |
RS49886B RS49886B (en) | 2008-08-07 |
Family
ID=27569747
Country Status (4)
Country | Link |
---|---|
KR (1) | KR100446895B1 (en) |
MY (1) | MY115721A (en) |
NZ (1) | NZ286079A (en) |
RS (1) | RS49886B (en) |
-
1996
- 1996-02-27 NZ NZ286079A patent/NZ286079A/en not_active IP Right Cessation
- 1996-02-27 RS YUP-118/96A patent/RS49886B/en unknown
- 1996-02-27 KR KR1019960004749A patent/KR100446895B1/en not_active IP Right Cessation
- 1996-02-28 MY MYPI96000722A patent/MY115721A/en unknown
Also Published As
Publication number | Publication date |
---|---|
RS49886B (en) | 2008-08-07 |
MY115721A (en) | 2003-08-30 |
KR960031454A (en) | 1996-09-17 |
KR100446895B1 (en) | 2006-04-10 |
NZ286079A (en) | 1997-12-19 |
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