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YU11896A - Benzothiophene compounds, intermediates, compositions containing them - Google Patents

Benzothiophene compounds, intermediates, compositions containing them

Info

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
Application number
YU11896A
Other languages
Serbo-Croatian (sh)
Inventor
David Palkowitz Alan
Jeff Thrasher Kenneth
Original Assignee
Eli Lilly And Company
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US08/396,401 external-priority patent/US5510357A/en
Priority claimed from US08/552,564 external-priority patent/US5998441A/en
Priority claimed from US08/552,565 external-priority patent/US5977093A/en
Priority claimed from US08/552,679 external-priority patent/US5856339A/en
Priority claimed from US08/552,890 external-priority patent/US5919800A/en
Priority claimed from US08/554,223 external-priority patent/US5856340A/en
Application filed by Eli Lilly And Company filed Critical Eli Lilly And Company
Publication of YU11896A publication Critical patent/YU11896A/en
Publication of RS49886B publication Critical patent/RS49886B/en

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.

YUP-118/96A 1995-02-28 1996-02-27 Benzothiophene compounds, intermedia tes, compositions and methods RS49886B (en)

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
US08/552,564 US5998441A (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
US08/552,679 US5856339A (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
US08/552,636 US5723474A (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)

Also Published As

Publication number Publication date
KR960031454A (en) 1996-09-17
KR100446895B1 (en) 2006-04-10
NZ286079A (en) 1997-12-19
RS49886B (en) 2008-08-07
MY115721A (en) 2003-08-30

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