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(12) Patent Application Publication (10) Pub. No.: US 2004/0242594 A1 Peters Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2004/0242594 A1 Peters Et Al US 2004O242594A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/0242594 A1 Peters et al. (43) Pub. Date: Dec. 2, 2004 (54) PRODRUGS OF ANTIDEPRESSANTS AND (30) Foreign Application Priority Data THEIR USE FOR TREATING DEPRESSIONS Nov. 17, 2001 (DK)................................. PA2001-01713 (76) Inventors: Dan Peters, Malmo (SE); Carl-Emil Sandberg, Smorum (DK) Publication Classification Correspondence Address: (51) Int. Cl.' ....................... A61K 31/519; A61K 31/24; BRCH STEWART KOLASCH & BRCH A61K 31/205 PO BOX 747 (52) U.S. Cl. ....................... 514/258.1; 514/554; 514/540 FALLS CHURCH, VA 22040-0747 (US) (57) ABSTRACT (21) Appl. No.: 10/489,657 This invention relates to prodrugs of antidepressants and the (22) PCT Filed: Nov. 15, 2002 use of these prodrugs in a method for therapy and to pharmaceutical compositions comprising the prodrugs of the (86) PCT No.: PCT/DK02/00767 invention. US 2004/0242594 A1 Dec. 2, 2004 PRODRUGS OF ANTIDEPRESSANTS AND THEIR group, which prodrug is a covalent conjugate of the antide USE FOR TREATING DEPRESSIONS preSSant and either a carboxylic acid or an alcohol, or a pharmaceutically acceptable Salt of Said prodrug. TECHNICAL FIELD 0012. In a special embodiment, the prodrug and the 0001. This invention relates to prodrugs of antidepres carboxylic acid or the alcohol are conjugated via an ester SantS. bond, a carbamate bond, or a carbonate bond. 0002. In other aspects the invention relates to the use of 0013 In its second aspect, the invention relates to a these prodrugs in a method for therapy and to pharmaceu prodrug of an antidepressant having a hydroxy group or a tical compositions comprising the prodrugs of the invention. carboxy group, which prodrug is an ester derivative formed between BACKGROUND ART 0014) either the hydroxy group of the antidepressant and 0003) Depression is a serious illness that affects more a carboxylic acid or the carboxy group of the antidepressant than ten million people in the USA alone. One of the greatest and an alcohol, or a pharmaceutically acceptable Salt of Said problems in treating depression is non-compliance with the prodrug. treatment program. The reasons for non-compliance with taking prescription medicines vary among individuals and 0015. In one embodiment, the antidepressant having a include: Feeling too depressed or embarrassed to take the hydroxy group or a carboxy group is an antidepressant prescription, becoming discouraged because the medicine having a hydroxy group. In a Second embodiment, the may take as long as Six weeks to take effect, misinformation antidepressant having a hydroxy group or a carboxy group about how anti-depressant medicine works or unwarranted is an antidepressant having a carboxy group. In a further fear of becoming addicted to it. embodiment, the antidepressant having a hydroxy group may have one or more hydroxy groups. In a special embodi 0004 Furthermore, non-compliance-such as early dis ment, the antidepressant having a hydroxy group has one continuation of the medicine because it is working-is likely hydroxy group. In a further embodiment, the antidepressant to lead to relapse or recurrence of the depression. having a carboxy group may have one or more carboxy 0005 Thus there is a continued strong need to find groups. In a special embodiment, the antidepressant having medications that give a better compliance for patients with a carboxy group has one carboxy group. depression. 0016. The antidepressant having a hydroxy group or a carboxy group may be Selected from the group of tricyclic SUMMARY OF THE INVENTION antidepressants, the group of monoamine oxidase inhibitors 0006 Therefore, in its first aspect, the invention provides (MAOIs), the group of reversible MAO type A inhibitors a prodrug of an antidepressant having a hydroxy group or a (RIMAS), the group of tetracyclic antidepressants, the group carboxy group, which prodrug is a covalent conjugate of the of selective serotonin re-uptake inhibitors (SSRIs), the antidepressant and either a carboxylic acid or an alcohol, or group of Serotonin noradrenaline re-uptake inhibitors a pharmaceutically acceptable Salt of Said prodrug. (SNRIs), the group of noradrenaline re-uptake inhibitors 0007. In its second aspect the invention provides a phar (NARIs), the group of noradrenergic specific Serotonergic maceutical composition comprising a therapeutically effec antidepressants (NaSSAS), or any other antidepressant. tive amount of a prodrug of the invention together with at 0017. In a further embodiment, the antidepressant having least one pharmaceutically-acceptable carrier, excipient or a hydroxy group is Selected from the group of compounds diluent. consisting of opipramol (4-3-(5H-dibenzb.fazepin-5-yl )propyl)-1-piperazine-ethanol (dihydrochloride)), Venlafax 0008. In a further aspect the invention provides a method ine (venlafexine), befloxatone ((R)-5-(methoxymethyl)-3-(p of treatment, prevention or alleviation of a disease or a (R)-4,4,4-trifluoro-3-hydroxybutoxyphenyl-2- disorder or a condition of a living animal body, including a oxazolidinone), MDL-72394 ((E)-f-fluoromethylene-m- human, which disorder, disease or condition is which dis tyrosine; or (E)-2-amino-4-fluoro-3-(m-hydroxyphenyl)-3- ease, disorder or condition is related to depression, which butenoic acid), danitracen (10-(1-methyl-4-piperidylidene)- method comprises the Step of administering to Such a living 9,10-dihydro-9-anthrol), ciclazindol (10-(3-chlorophenyl)- animal body in need thereof a therapeutically effective 2,3,4,10-tetrahydro-pyrimido 1,2-alindol-10-ol), RS-8359+ amount of a compound of the invention. ((+)-6,7-dihydro-7-hydroxy-5H-cyclopentadpyrimidinyl 0009. Other objects of the invention will be apparent to 4-aminobenzonitrile), 2 hydroxyimipramine (5-3- the person skilled in the art from the following detailed (dimethylamino)propyl)-10,11-dihydro-5H-dibenzb.f description and examples. azepin-2-ol), 2-hydroxy desipramine (5-3- (methylamino)propyl)-10,11-dihydro-5H-dibenzb.f 0.010 The prodrug of the invention gives extended thera azepin-2-ol), 10-hydroxyamitriptyline (5,11-dihydro-10 peutic effectiveness and permits leSS frequent dosing com hydroxy-N,N-dimethyl-dibenzoadcycloheptene-A*- pared to the unconjugated antidepressant, thereby enhancing propylamine), 10-hydroxynortriptyline (5,11-dihydro-10 the possibility of compliance with the treatment for patients hydroxy-N-methyl-dibenzoadcycloheptene-A*- with depression. propylamine), trazium esilate (1-(p-chlorophenyl)-1,2- dihydro-1-hydroxy-as-triazino6, 1-allisoquinolin-5-ium DETAILED DISCLOSURE OF THE INVENTION ethaneSulfonate), Oxaprotiline ((+)-O-(methylamino)m- 0011. In its first aspect, the invention provides a prodrug ethyl-9,10-ethanoanthracene-9-(10H)-ethanol), levopro of an antidepressant having a hydroxy group or a carboxy tiline (the (R)-(-) enantiomer, (R)-(-)O-(methylamino)m- US 2004/0242594 A1 Dec. 2, 2004 ethyl-9,10-ethanoanthracene-9-(10H)-ethanol, or the (S)- 0025 Z is hydrogen; R is aryl optionally substituted one (+) enantiomer, (S)-(+)C-(methylamino)methyl-9,10 or more times with Substituents Selected from the group ethanoanthracene-9-(10H)-ethanol), cilobamine (cis-2-(3,4- consisting of halogen, CF, CN, alkoxy, cycloalkoxy, alkyl, dichlorophenyl)-3-isopropylamino-bicyclo2.2.2]octan-2-ol cycloalkyl, alkenyl, alkynyl, amino, alkylamino, dialky (methanesulfonate)), flesinoxan ((+)-(S)-4-fluoro-N-2-4- lamino and nitro, and n is 1, 2, 3, or 4. In a special (2-2-hydromethyl)-1,4-benzodioxan-5-yl)-1-piperarinyl embodiment thereof, R is chlorophenyl or-dichlorophenyl. ethylbenzamide), ifoxetine ((+)-cis-4-(2,3-xylyloxy)-3-pi peridinol (sulfate)), flerobuterol (C-tert-butylamino 0026. In a second special embodiment, the antidepressant methyl-o-fluorobenzyl alcohol), BRL 14342 (1-amino-3- having a hydroxy group is a compound of the general (m-chlorophenyl)-N,N-dimethyl-3-phenyl-2-propanol), formula (Ia) or (Ib) as above, wherein R is alkyl, alkenyl, bipenamol (O-(C-amino-o-tolyl)thiobenzyl alcohol), or alkynyl. cyprolidol (O.C.-diphenyl-C-2-(4-pyridyl) cyclopropyl 0027. In a further special embodiment, the antidepressant methanol), and dazadrol (C-(p-chlorophenyl)-O-(2-imida having a hydroxy group is a compound of the general Zolinyl)-2-pyridine-methanol (Z)-2-butenedionate). formula (Ia) or (Ib) as above and the carboxylic acid forming 0.018. In a special embodiment, the antidepressant having the ester derivative is a C7 so-carboxylic acid, Such as a a hydroxy group is Selected from the group of compounds C7o-carboxylic acid. consisting of opipramol, Venlafaxine, and befloxatone. 0028. In a still further special embodiment, the antide 0019. In a further special embodiment, the antidepressive preSSant having a hydroxy group is Selected from the group having a hydroxy group is Venlafaxine. of compounds consisting of: 0020 Venlafaxine (1-2-dimethylamino-1-(4-methoxy 0029 (1S,3S,4S,5R/S,8R)-3-(3,4-dichlorophenyl)-7- phenyl)-ethyl-cyclohexanol) and its preparation is i.a. azatricyclo5.3.0.0decan-5-ol; described in U.S. Pat. No. 4,535,186. Venlafaxine is a 0030 (1S,3S,4S,5S,8R)-3-(3,4-dichlorophenyl)-7- racemic mixture of (-) isomer and the (+) isomer. In a azatricyclo5.3.0.0decan-5-ol; Special embodiment the antidepressive having a hydroxy group is the racemate of Venlafaxine. In a further embodi 0031 (1S,3S,4S,5S,8R)-3-(3,4-dichlorophenyl)-7- ment the antidepressive having a hydroxy group is the (-) azatricyclo5.3.0.0decan-5-ol; isomer of Venlafaxine. In a still further embodiment the antidepressive having a hydroxy group is the (+) isomer of 0032 (1R,3R.4R,5R/S,8S)-3-(3,4-dichlorophenyl)-7- Venlafaxine. aza-tricyclo5.3.0.0-decan-5-ol; 0021. In a further embodiment, the antidepressant having 0033 (1R,3R.4R,5R,8S)-3-(3,4-dichlorophenyl)-7- a hydroxy group is a compound of the general formula (Ia) aza-tricyclo[5.3.0,0'decan-5-ol; and or (Ib), 0034) (1R,3R,4R,5S,8S)-3-(3,4-Dichlorophenyl)-7- azatricyclo-5.3.0,0'-decan-5-ol.
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