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(12) Patent Application Publication (10) Pub. No.: US 2006/0052594 A1 Del Soldato Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2006/0052594 A1 Del Soldato Et Al US 20060052594A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0052594 A1 Del Soldato et al. (43) Pub. Date: Mar. 9, 2006 (54) NEW CORTICOSTEROIDS (30) Foreign Application Priority Data Jan. 29, 2002 (IT) ............................... MI2OO2AOOO148 (76) Inventors: Ongini,Piero Del Segrate Soldato, (IT) Milano (IT); Ennio Publication Classification (51) Int. Cl. Correspondence Address: (52) gton (2006.01) 540/51 ARENT FOX PLLC Oa - 1 - O - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - 1050 CONNECTICUT AVENUE, N.W. (57) ABSTRACT SUTE 400 WASHINGTON, DC 20036 (US) Nity derivatives of Steroidal compounds of general OUT (21) Appl. No.: 10/501,335 B-X-NO. (I) (22) PCT Filed: Jan.e 16,- Vs 2003 or esters or Salts thereof, wherein: B is a Steroidal radical, X is a bivalent linking group (86) PCT No.: PCT/EP03/00394 comprising an aromatic or heterocyclic ring. US 2006/0052594 A1 Mar. 9, 2006 NEW CORTICOSTEROIDS nisolone, triamcinolone, paramethasone, betamethasone, dexamethasone, triamcinolone acetonide, fluocinolone 0001. The present invention relates to steroidal com acetonide, beclomethasone, acetoxypregnelone, etc. can be pounds having an improved pharmacological activity and mentioned, exerts marked pharmaco-toxicological effects on lower Side effects and an improved receptor affinity on the various organs. For Said reason the prolonged clinic use and Specific receptors of endogenous Steroids. the interruption of the pharmacological treatment cause side 0002. In particular the invention relates to steroidal com effects, Some of them very Serious. See for example Good pounds having an improved receptor affinity on the Specific man & Gilman, “The Pharmacological Basis of Therapeu receptors of the endogenous Steroids and having an tics” 9th ed., pages 1459–1465, 1996. improved pharmacological activity and lower Side effects, in particular: 0013 Among the side effects one can mention: 0003 those affecting the bony tissue, such for example 0014 those affecting the bony tissue, such as for Osteoporosis, osteonecrosis and myopathies, which in example osteoporosis, osteonecrosis and myopathies, patients affected by asthma or by COPD (Chronic which in patients affected by asthma or by COPD Obstructive Pulmunary Disease) can determine a (Chronic Obstructive Pulmunary Disease) can deter remarkable reduction of the respiratory activity; mine a marked reduction of the respiratory capabilities, 0004 those affecting the gastrointestinal apparatus. 0015 those affecting the cardiovascular system which generate hypertensive responses and/or cardiac fre 0005 The invention relates to compounds having a ste quency diseases; roidal Structure in particular having not only an improved antiinflammatory activity at peripheral level, but also an 0016 increased easyneSS to infections, improved anti-neurodegenerative activity, an improved anti arthritic activity, an improved immunodepressive activity, 0017 those affecting the gastrointestinal apparatus, an improved angiostatic/angiogenetic and antiasthmatic 0018 increase of glucose levels in the blood, which in activity; or usable in Substitutive hormonal therapies, for diabetic patients can lead to a disease worsening, or in example in the post-menopause therapy. predisposed patients it can cause the arising of hyper 0006 More specifically the present invention relates also glycaemic attacks. to Steroid compounds of the glucocorticoid class which can be used as bronchodilators in respiratory pathologies char 0019 See for example Martindale “The Extrapharmaco acterized by broncho-constrictive events. poeia", 30th ed., pages 712-723, 1993. 0007. The compounds according to the present invention 0020. According to the prior art it does not seem possible are therapeutically useful in the treatment of illnesses to Separate the Steroid therapeutic actions from their side wherein Steroidal products are generally applied, with effects, see Goodman et al, mentioned above, page 1474. increased benefit, in terms of improved tolerability as above 0021. In the prior art nitrooxy derivatives of steroids, defined and improved efficacy. which are usable also as cardiovascular agents for the 0008. This represents a totally surprising and unexpected coronary insufficiency or angina pectoris therapy, are re-Suit compared with the known Steroidal compounds. described. Indeed considering the various above therapeutic uses of a 0022. For example, German patent DE 2.222,491 Specific precursor product, the present invention products describes the preparation of pregnane derivatives having in give a combination of results, considered as improvement of position 21 the -CH-O-NO group. In said patent it is the therapeutic performance, i.e. improved pharmacothera Stated that Said derivatives have a cardiotropic activity. This peutic efficacy and improved tolerability, compared with the activity represents a drawback for Said compounds, Since prior art products. In fact, contrary to any expectations, the they modify the cardiac frequency. Furthermore in Said present invention products are characterized in that they patent no mention is made to the receptor affinity on the show an improved therapeutic profile: high activity in the Specific receptors of the endogenous Steroids. above applications combined with lower Side effects as above defined. 0023 U.S. Pat. No. 3,494,941 describes steroid deriva tives from 3-hydroxy-extrane or from extr-4 en-3 one, used 0009. As known, steroids comprise: as vasodilators in the treatment of cardiac affections Such as 0010 corticosteroids, classified in glucocorticoids coronary insufficiency and angina pectoris. In the Structure active on the glucogenesis and on the metabolism of of said compounds a ONO group is at the free end of the proteins, lipids, carbohydrates and calcium in general, alkylene chain which is linked by an ether bond to the mineralcorticoids active on the water and Saline bal Steroid in position 17. According to Said patent it is possible to have nitrate groupS also in the positions 3 and 16 of the ance, Steroidal Structure. The same drawbacks mentioned above as 0011) Sexual Steroids, including estrogens and andro regards the effects on the cardiac frequency can be repeated genS. for the compounds of this patent. Besides, in the patent no 0012. It is well known that glucocorticoids represent a mention is made to the receptor affinity on the Specific first choice pharmacological approach in the therapy of receptors of endogenous Steroids. various pathologies. Said class of drugs, among which, for 0024 U.S. Pat. No. 3,183,252 describes derivatives of example, hydrocortisone, cortisone, prednisone, predniso 16-nitrate-alkylpregnanes wherein the alkyl group is linked lone, fluidrocortisone, desoxycorticosterone, methylpred to the pregnane Structure by a carbon-carbon bond. The US 2006/0052594 A1 Mar. 9, 2006 compounds according to Said patent can be used as vasodi 0029) in position 1-2: a double bond; lators. The same drawbacks reported for the above prior art 0030) in position 2-3 the following substituent: can be repeated. 0025 WO 98/15568 in the name of the Applicant describes nitrate esters of Steroidal compounds, wherein 2 (IA-1) between the Steroidal structure and the nitrooxy group a N bivalent linking group is inserted. Said compounds show a N s good efficacy and/or good tolerability with respect to the N corresponding precursors. However in the examples and in the description no data are reported on the receptor activity. No indication is therefore reported Suggesting Steroidal compounds having an improved receptor activity and an improved pharmacological activity combined with lower side effects. 0031 in position 2: Cl, Br; 0026 Patent application WO 00/61604 in the name of the 0032) in position 3: oxo, -O-CH-CH-Cl, OH, Applicant describes nitrooxy derivatives of Steroidal com OCH; pounds with various linking groups having at one end a nitrooxy group, and covalently linked with the other end to 0033) in position 4-5: a double bond; a Steroidal compound. In Said application the uses concern 0034) in position 5-6: a double bond; the compounds usable in the treatment of patients in Oxida 0035) in position 6: Cl, F, Br, CH, -CHO; tive StreSS. Said compounds contain in the molecule also a 0036 the ring defined by the carbon atoms numbered 1, bivalent linking group which must be capable to prevent the 2, 3, 4, 5, and 10 is an aromatic ring when B is the residue free radicals production and is Selected on the basis of the of an estrogen; tests reported therein. No indication is therefore given Suggesting Steroidal compounds having an improved recep 0037 in position 7: C1, OH: torial activity and an improved pharmacological activity 0038 in position 9: Cl, F, Br; combined with lower side effects. 0039) in position 11: OH, oxo, Cl; 0027. The need was felt to have available steroidal com 0040 in position 16: CH, OH, =CH; pounds having an improved receptor affinity on the Specific 0041) in position 17: OH, CH, OCO(O)(CH2)CH receptors of the endogenous Steroids and an improved wherein ua is an integer equal to 0 or 1, Va is an integer pharmacological activity combined with lower Side effects. The Applicant has Surprisingly and unexpectedly found a from 0 to 4, ethynyl (C=CH); or Specific class of Steroidal compounds which in the above pathologies unexpectedly and Surprisingly show not only an (IA-2) improved efficacy but also an improved tolerability and O lower side effects
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