Title:
17α-アルキル-17β-オキシ-エストラトリエン類及びそれらの生成のための中間生成物、医薬剤及び医薬製剤の生成のためへの17α-アルキル-17β-オキシ-エストラトリエンの使用
Document Type and Number:
Japanese Patent JP4335820
Kind Code:
B2
Abstract:
17alpha -Alkyl-11beta -halo-17beta -oxy-estratriene derivatives (I), having a 7alpha -side-chain, are new. 17alpha -Alkyl-11beta -halo-17beta -oxy-estratriene derivatives of formula (I), their acid addition salts and esters are new. [Image] Hal : F or Cl; R 3>H, 1-4C alkyl, 1-4C alkanoyl or 3-7C cyclic ether residue; R 1>7>'>H, 1-4C alkyl or 1-4C alkanoyl; R 1>7>''>1-4C alkyl (optionally partially fluorinated) or 2-4C alkynyl; Q : -U-V-W-X-Y-Z-E; U : 1-13C alkylene, 2-13C alkenylene, 2-13C alkynylene, -A-B- or -A-O-B-; A : benzylidene (bonded to the steroid structure via CH 2), phenyl or (1-3C) alkyl-aryl (bonded to the steroid structure via alkyl); B : 1-13C alkylene, 2-13C alkenylene or 2-13C alkynylene; V : CH 2or CO; W : N(R 6>) or N +>(O ->)(R 6>); or an azolidinylene or azolidinylene-N-oxide ring (where X is incorporated into the ring); R 6>H, CH 2R 7>or COR 7>; R 7>H; 1-14C alkylene, 2-14C alkenylene or 2-14C alkynylene (all optionally at least partially fluorinated, optionally mono- or polyhydroxylated and optionally interrupted by 1-3 of O, S, NH or N(1-3C alkyl)); or aryl, heteroaryl, 3-10C cycloalkyl, 4-15C cycloalkylalkyl, 7-20C aralkyl, heteroaryl-(1-6C) alkyl, aminoalkyl or biphenylyl (all optionally substituted); X : 1-12C alkylene, 2-12C alkenylene or 2-12C alkynylene; Y : direct bond, R 1>1>, OR 1>1>, CH=CF or NHCONHR 1>2>; R 1>0>direct bond, 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; R 1>1>1-5C alkylene, 2-5C alkenylene or 2-5C alkynylene; or aryl, heteroaryl, 3-10C cycloalkyl, 4-15C cycloalkylalkyl or 7-20C aralkyl (all optionally substituted); R 1>2>optionally substituted arylene (bonded to Z); Z : direct bond; or 1-9C alkylene, 2-9C alkenylene or 2-9C alkynylene (all optionally partially or completely fluorinated); and E : CF 3or at least partially fluorinated aryl. Provided that if Y is SR 1>0>, SOR 1>0>or SO 2R 1>0>if W is N +>(O ->)(R 6>) or azolidinylene-N-oxide ring. Independent claims are also included for: (1) 17beta -oxy-estratriene and 17-oxo-estratriene derivatives of formula (II); and (2) 17beta -oxy-estratriene and 17-oxo-estratriene derivatives of formula (III). [Image] W : N +>(O ->)(R 6>) or azolidinylene-N-oxide. ACTIVITY : Cytostatic; Antiinfertility; Gynecological; Antialopecia; Depilatory. MECHANISM OF ACTION : Estrogen antagonist. In antiuterotrophic tests in rats, (5-(11beta -fluoro-3,17beta -dihydroxy-17alpha -methyl-estra-1,3,5(10)-trien-7alpha -yl)-pentyl)-(methyl)-(7,7,8,8,9,9,9-heptafluorononyl)-amine (Ia) at a dose of 0.03 mg/kg s.c. gave 94% of the uterotrophic effect of estradiol benzoate.
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Inventors:
Ballman, Rolf
Heinrich, Nikolaus
Yauterat, Rolf
Crawl, Yoruk
Petrov, Orrin
Reichel, Andreas
Hoffman, Jens
Richterner, Rosemary
Heinrich, Nikolaus
Yauterat, Rolf
Crawl, Yoruk
Petrov, Orrin
Reichel, Andreas
Hoffman, Jens
Richterner, Rosemary
Application Number:
JP2005013016A
Publication Date:
September 30, 2009
Filing Date:
January 20, 2005
Export Citation:
Assignee:
Bayer Schering Pharma Aktiengesellschaft
International Classes:
A61K31/567; C07J1/00; A61K31/5685; A61K31/569; A61K31/58; A61P5/32; A61P13/08; A61P15/08; A61P15/16; A61P15/18; A61P17/14; A61P35/00; C07J41/00; C07J43/00
Domestic Patent References:
| JP2001503024A | ||||
| JP2000510861A | ||||
| JP2001527088A | ||||
| JP60097995A |
Attorney, Agent or Firm:
Atsushi Aoki
Takashi Ishida
Fukumoto product
Tetsuji Koga
Kazuhiro Nakamura
Masaya Nishiyama
Takashi Ishida
Fukumoto product
Tetsuji Koga
Kazuhiro Nakamura
Masaya Nishiyama