US2015051180A9PendingUtilityA9

Progesterone Antagonist and Selective Progesterone Modulator in the Treatment of Excessive Uterine Bleeding

Assignee: PREGLEM SAPriority: Apr 20, 2007Filed: Oct 7, 2013Published: Feb 19, 2015

Est. expiryApr 20, 2027(~0.8 yrs left)· nominal 20-yr term from priority

Inventors:Bartholomeus C.J.M. Fauser Ernest Loumaye

A61P 5/00A61P 7/04A61P 5/36A61P 7/00A61P 7/02A61P 15/00A61K 31/57A61K 31/573A61K 31/567

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Claims

Abstract

Progesterone antagonists and SPRM are useful to prepare a medication for the treatment or the prophylaxis of excessive uterine bleeding in women with spontaneous or iatrogenic coagulation disorders such as thrombopenia, coagulation factor deficiency or anti-coagulant therapy. Treatment will last from 1 day to 180 days.

Claims

exact text as granted — not AI-modified

1 - 28 . (canceled) 
     
     
         29 . A kit comprising a composition that comprises a therapeutically effective amount of a progesterone antagonist, a selective progesterone receptor modulator (SPRM), or an active metabolite thereof, wherein
 the progesterone antagonist or SPRM is selected from the group consisting of CDB-2914, mifepristone, asoprisnil, CDB-4124, onapristone, org33628, tanaproget, tanaproget-combo, 11 beta-((4-N,N-dimethylamino)-phenyl)-17 beta-hydroxy-18-methyl-17 alpha-propinyl-4,9(10)-estradien-3-one, 11 beta-((4-N,N-dimethylamino)-phenyl)-17 a beta-hydroxy-17a alpha-propinyl-D-homo-4,9(10),16-estratrien-3-one, 11 beta-4-methoxyphenyl-17 beta-hydroxy-17 alpha-ethinyl-4,9(10)-estradien-3-one, 11 beta-(4-acetylphenyl)-17 beta-hydroxy-17 alpha-(prop-1-inyl)-4,9(10)estradien-3-one, 11 beta-(4-dimethylaminophenyl)-17 alpha-hydroxy-17 beta-(3-hydroxy-propyl)-13 alpha-methyl-4,9-gonadien-3-one, (Z)-11 beta-[4-(dimethylamino)phenyl]-17beta-hydroxy-17alpha-(3-hydroxy-1-propenyl)-estr-4-en-3-one-5, 11 beta-(4-acetylphenyl)-17 beta-hydroxy-17 alpha-(3-hydroxyprop-1-(Z)-enyl)-4, 9(10)-estradien-3-one, 11 beta-(4-cyanophenyl)-17 beta-hydroxy-17 alpha-(3-hydroxyprop-1-(Z)-enyl)-4-androsten-3-one, 11 beta, 19-(4- (3-pyridinyl)-o-phenylene)-17 beta-hydroxy-17 alpha-(3-hydroxyprop- 1-(Z)-enyl)-4-androsten-3-one, and a pharmaceutically acceptable salt of any of the progesterone antagonists or SPRMs, and   wherein the therapeutically effective amount of the progesterone antagonist, the SPRM, an active metabolite thereof, or a pharmaceutically acceptable salt thereof can treat excessive uterine bleeding resulting from a coagulation disorder.   
     
     
         30 . The kit of  claim 29 , wherein the active metabolite of asoprisnil is J912 or J956. 
     
     
         31 . The kit of  claim 29 , wherein the active metabolite of CDB-4124 is CDB-4453. 
     
     
         32 . The kit of  claim 29 , wherein the active metabolite of CDB-2914 is selected from the group consisting of CBD-3877, CDB-3963, CDB-3236, and CDB-4183. 
     
     
         33 . The kit of  claim 29 , wherein the coagulation disorder is hemophilia, von Willebrand&#39;s disease, hepatic function impairment, thrombocytopenia, leukemia, disseminated intravascular coagulation, bone marrow aplasia, or inadequate anticoagulation treatment. 
     
     
         34 . The kit of  claim 29 , wherein the progesterone antagonist, the SPRM, or active metabolite of the progesterone antagonist or the SPRM is selected from the group consisting of CDB-2914, mifepristone, CDB-4124, onapristone, org33628, 11 beta-((4-N,N-dimethylamino)-phenyl)-17 beta-hydroxy-18-methyl-17 alpha-propinyl -4,9(10)-estradien-3-one, 11 beta-((4-N,N-dimethylamino)-phenyl)-17 a beta-hydroxy-17a alpha-propinyl-D-homo-4,9(10),16-estratrien-3-one, 11 beta-4-methoxyphenyl-17 beta-hydroxy-17 alpha-ethinyl-4,9(10)-estradien-3-one, 11 beta-(4- acetylphenyl)-17 beta-hydroxy-17 alpha-(prop-1-inyl)-4,9(10)estradien-3-one, 11 beta-(4-dimethylaminophenyl)-17 alpha-hydroxy-17 beta-(3-hydroxy-propyl)-13 alpha-methyl-4,9-gonadien-3-one, (Z)-11 beta-[4-(dimethylamino)phenyl]-17beta-hydroxy-17alpha-(3-hydroxy-1-propenyl)-estr-4-en-3-one-5, 11 beta-(4-acetylphenyl)-17 beta-hydroxy-17 alpha-(3 -hydroxyprop-1 -(Z)-enyl)-4, 9(10)-estradien-3 -one, 11 beta-(4- cyanophenyl)-17 beta-hydroxy-17 alpha-(3-hydroxyprop-1-(Z)-enyl)-4-androsten-3-one, 11 beta, 19-(4-(3 -pyridinyl)-o-phenylene)-17 beta-hydroxy-17 alpha-(3-hydroxyprop-1 -(Z)-enyl)-4-androsten-3-one, and a pharmaceutically acceptable salt of any of the progesterone antagonists or SPRMs. 
     
     
         35 . The kit of  claim 29 , wherein the composition is for daily administration, every other day administration, once a week administration, once every month administration, or a one-time administration. 
     
     
         36 . The kit of  claim 35 , wherein the composition is for daily administration. 
     
     
         37 . The kit of  claim 29 , wherein the composition can be administered over a period of 1 to 180 days. 
     
     
         38 . The kit of  claim 29 , wherein the composition is for administration during bleeding peaks or during menstruation. 
     
     
         39 . The kit of  claim 29 , wherein the therapeutically effective amount is between 0.1 to 1000 mg. 
     
     
         40 . A kit comprising a composition that comprises a therapeutically effective amount of CDB-2914, an active metabolite of CDB-2914, or a pharmaceutically acceptable salt of CDB-2914, wherein the therapeutically effective amount can treat excessive uterine bleeding resulting from a coagulation disorder, and wherein the active metabolite of CDB-2914 is selected from the group consisting of CBD-3877, CDB-3963, CDB-3236, and CDB-4183. 
     
     
         41 . The kit of  claim 40 , wherein the therapeutically effective amount is between 1 to 15 mg CDB-2914 or an amount of the pharmaceutically acceptable salt of CDB-2914 equivalent to 1 to 15 mg CDB-2914. 
     
     
         42 . The kit of  claim 40 , wherein the therapeutically effective amount is 10 mg CDB-2914, or an amount of the pharmaceutically acceptable salt of CDB-2914 equivalent to 1 mg CDB-2914. 
     
     
         43 . The kit of  claim 40 , wherein the composition is for oral administration. 
     
     
         44 . The kit of  claim 40 , wherein the coagulation disorder is hemophilia, von Willebrand&#39;s disease, hepatic function impairment, thrombocytopenia, leukemia, disseminated intravascular coagulation, bone marrow aplasia, or inadequate anticoagulation treatment 
     
     
         45 . The kit of  claim 40 , wherein the coagulation disorder is bone marrow aplasia. 
     
     
         46 . The kit of  claim 40 , wherein the composition is administered over a period of 1 to 180 days. 
     
     
         47 . A kit comprising a composition that comprises a therapeutically effective amount of CDB-4124, CDB-4453, or a pharmaceutically acceptable salt of CDB-4124 or CDB-4453, wherein the therapeutically effective amount can treat excessive uterine bleeding resulting from a coagulation disorder. 
     
     
         48 . The kit of  claim 47 , wherein the therapeutically effective amount is 25 mg CDB-4124 or an amount of a pharmaceutically acceptable salt thereof equivalent to 25 mg CDB-4124. 
     
     
         49 . The kit of claim  19 , wherein the composition is an oral dosage form. 
     
     
         50 . The kit of claim  19  further comprises an instruction for use.

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