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CY1108281T1 - 17-α-υποκατασταθεισα-11-β-υποκατασταθεισα-4-αρυλ και 21-υποκατασταθεισα 19-νορπρεγναδιενοδιονη ως νεοι αντι-προεμμηνορροϊκοι παραγοντες. - Google Patents

17-α-υποκατασταθεισα-11-β-υποκατασταθεισα-4-αρυλ και 21-υποκατασταθεισα 19-νορπρεγναδιενοδιονη ως νεοι αντι-προεμμηνορροϊκοι παραγοντες.

Info

Publication number
CY1108281T1
CY1108281T1 CY20081100895T CY081100895T CY1108281T1 CY 1108281 T1 CY1108281 T1 CY 1108281T1 CY 20081100895 T CY20081100895 T CY 20081100895T CY 081100895 T CY081100895 T CY 081100895T CY 1108281 T1 CY1108281 T1 CY 1108281T1
Authority
CY
Cyprus
Prior art keywords
substitutes
aryl
norpregnadienedionion
principle
new anti
Prior art date
Application number
CY20081100895T
Other languages
English (en)
Inventor
Hyun K Kim
Richard P Blye
Pemmaraju N Rao
James W Cessac
Carmie K Acosta
Anne Marie Simmons
Original Assignee
The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services
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 US09/526,855 external-priority patent/US6900193B1/en
Application filed by The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services filed Critical The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services
Publication of CY1108281T1 publication Critical patent/CY1108281T1/el

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • 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
    • A61P15/04—Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P5/36—Antigestagens
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C07J41/0016—Oximes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
    • C07J5/0053—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/004—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
    • C07J7/0045—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/0085—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by an halogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Η παρούσα εφεύρεση αναφέρεται, μεταξύ άλλων, σε ενώσεις έχουσες το γενικό τύπο (I) στον οποίο: το R1 είναι ένα μέλος επιλεγόμενο από την ομάδα την αποτελούμενη από -OCH3, -SCH3, -N(CH3)2, -NHCH3, -NC4H8, -NC5H10, -NC4H8O, -CHO, -CH(OH)CH3, -C(O)CH3, -O(CH2)2N(CH3)2 και -O(CH2)2NC5H10- το R2 είναι ένα μέλος επιλεγόμενο από την ομάδα την αποτελούμενη από υδρογόνο, αλογόνο, αλκύλιο, ακύλιο, υδροξύλιο, αλκο-ξύλιο (π.χ. μεθοξύλιο, αιθοξύλιο, βινυλοξύλιο, αιθυνυλοξύλιο, κυκλοπροπυλοξύλιο, κλπ.), ακυλοξύλιο (π.χ. ακετοξύλιο, γλυκινικό, κλπ.), αλκυλανθρακικό, κυπιονυλοξύλιο, S-αλκύλιο, -SCN, S-ακύλιο και -OC(O)R6, όπου το R6 είναι μία χαρακτηριστική ομάδα περιλαμβάνου­σα, αλλά μη περιοριζόμενη σε αυτά, τα αλκύλιο (π.χ. μεθύλιο, αιθύλιο, κλπ.), αλκοξυεστέρα (π.χ. -CH2OCH3) και αλκοξύλιο (-OCH3)- το R3 είναι ένα μέλος επιλεγόμενο από την ομάδα την αποτελούμενη από αλκύλιο, υδροξύλιο, αλκοξύλιο και ακυλοξύλιο- το R4 είναι ένα μέλος επιλεγόμενο από την ομάδα την αποτελούμενη από υδρογόνο και αλκύλιο· και το Χ είναι ένα μέλος επιλεγόμενο από την ομάδα την αποτελούμενη από =O και =N-OR5, όπου το R5 είναι ένα μέλος επιλεγόμενο από την ομάδα την αποτελούμενη από υδρογόνο και αλκύλιο. Επί πλέον της παροχής των ενώσεων Τύπου I, η παρούσα εφεύρεση παρέχει μεθόδους στις οποίες χρησιμοποιούνται πλεονεκτικά οι ενώσεις Τύπου I, μεταξύ άλλων για τον ανταγωνισμό της ενδογενούς προγεστερόνης· για την επαγωγή εμμήνων- για την αγω­γή της ενδομητριώσεως- για την αγωγή της δυσμηνόρροιας- για την αγωγή εξαρτώμενων από ενδοκρινείς ορμόνες όγκων- για την αγωγή μηνιγγιωμάτων- για την αγωγή λειομυωμάτων της μήτρας- για την αγωγή ινομυωμάτων της μήτρας- για την αγωγή του ενδομήτριου πολλαπλασιασμού- για την επαγωγή της ωριμάνσεως του τραχήλου της μήτρας- για την επαγωγή τοκετού- και για αντισύλληψη.
CY20081100895T 2000-03-17 2008-08-21 17-α-υποκατασταθεισα-11-β-υποκατασταθεισα-4-αρυλ και 21-υποκατασταθεισα 19-νορπρεγναδιενοδιονη ως νεοι αντι-προεμμηνορροϊκοι παραγοντες. CY1108281T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/526,855 US6900193B1 (en) 1996-05-01 2000-03-17 Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
EP01918812A EP1265911B1 (en) 2000-03-17 2001-03-16 17-alpha-substituted-11-beta-substituted-4-aryl and 21-substituted 19-norpregnadienedione as antiprogestational agents

Publications (1)

Publication Number Publication Date
CY1108281T1 true CY1108281T1 (el) 2014-02-12

Family

ID=24099075

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20081100895T CY1108281T1 (el) 2000-03-17 2008-08-21 17-α-υποκατασταθεισα-11-β-υποκατασταθεισα-4-αρυλ και 21-υποκατασταθεισα 19-νορπρεγναδιενοδιονη ως νεοι αντι-προεμμηνορροϊκοι παραγοντες.

Country Status (11)

Country Link
EP (4) EP1265911B1 (el)
JP (2) JP5417562B2 (el)
AT (1) ATE396197T1 (el)
AU (2) AU2001245849B2 (el)
CA (1) CA2403756C (el)
CY (1) CY1108281T1 (el)
DE (1) DE60134126D1 (el)
DK (1) DK1265911T3 (el)
ES (3) ES2546336T3 (el)
PT (1) PT1265911E (el)
WO (1) WO2001074840A2 (el)

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ES2212912B1 (es) * 2003-01-22 2005-10-01 Crystal Pharma, S.A. Procedimiento para la obtencion de 17alfa-acetoxi-11beta-(4-n,n-dimetilaminofenil)-19-norpregna-4,9-dien-3,20-diona.
US8173626B2 (en) * 2006-03-08 2012-05-08 Danco Laboratories Llc Methods, dosing regimens and medications using anti-progestational agents for the treatment of disorders
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HU228636B1 (en) * 2007-06-27 2013-04-29 Richter Gedeon Nyrt Industrial method for the synthesis of 17-acetoxy-11betha-4[-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione and the key intermediates of the process
TWI477276B (zh) * 2008-04-28 2015-03-21 Repros Therapeutics Inc 抗黃體素給藥方案
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TWI539953B (zh) * 2008-04-28 2016-07-01 瑞波若斯治療學公司 用於治療乳癌之組成物和方法
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CN102942612A (zh) * 2012-10-30 2013-02-27 四川大学 一种合成醋酸乌利司他的新方法
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CN103073612B (zh) * 2013-02-04 2015-11-04 山东大学 醋酸乌利司他关键中间体的制备方法
HU230319B1 (hu) 2013-10-01 2016-01-28 Richter Gedeon Nyrt. Ipari eljárás szteroid hatóanyagok előállítására
CN104774231A (zh) * 2014-01-13 2015-07-15 上海医药工业研究院 17α-羟基-19-去甲孕甾-4,9-二烯-3,20-二酮的制备工艺
HU230381B1 (hu) 2014-02-17 2016-03-29 Richter Gedeon Nyrt Ipari eljárás szteroid intermedier előállítására
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CA2403756A1 (en) 2001-10-11
EP1265911B1 (en) 2008-05-21
CA2403756C (en) 2010-02-09
EP2348030B1 (en) 2015-05-06
JP2012051935A (ja) 2012-03-15
EP2033965A3 (en) 2012-09-19
WO2001074840A2 (en) 2001-10-11
PT1265911E (pt) 2008-10-09
JP2003529604A (ja) 2003-10-07
JP5417562B2 (ja) 2014-02-19
EP2348031A3 (en) 2012-05-09
EP2348030A3 (en) 2012-05-09
DK1265911T3 (da) 2008-09-29
EP2348031A2 (en) 2011-07-27
EP2348030A2 (en) 2011-07-27
WO2001074840A3 (en) 2002-05-02
EP1265911A2 (en) 2002-12-18
EP2033965A2 (en) 2009-03-11
AU2001245849B2 (en) 2007-01-04
ES2546291T3 (es) 2015-09-22
ES2307604T3 (es) 2008-12-01
EP2348031B1 (en) 2015-06-17
ATE396197T1 (de) 2008-06-15
DE60134126D1 (de) 2008-07-03
ES2546336T3 (es) 2015-09-22
EP2348031B9 (en) 2016-08-10
AU4584901A (en) 2001-10-15

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