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  Verification of translationUSPTO Application #: 20050227951Title: Verification of translation Abstract: The invention relates to new vitamin D derivatives of general formula (I), process for their production, intermediate products of the process as well as the use for production of pharmaceutical agents. (end of abstract)
Agent: Millen, White, Zelano & Branigan, P.C. - Arlington, VA, US Inventors: Andreas Steinmeyer, Gunter Neef, Gerald Kirsch, Katica Schwarz, Herbert Wiesinger, Martin Haberey, Marianne Fahnrich, Gernot Langer USPTO Applicaton #: 20050227951 - Class: 514167000 (USPTO) Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Ortho-hydroxybenzoic Acid (i.e., Salicyclic Acid) Or Derivative Doai, 9,10-seco- Cyclopentanohydrophenanthrene Ring System (e.g., Vitamin D, Etc.) Doai The Patent Description & Claims data below is from USPTO Patent Application 20050227951. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] The invention relates to new vitamin D derivatives of general formula I 1 [0002] process for their production, intermediate products of the process as well as the use for the production of pharmaceutical agents. PRIOR ART [0003] Natural vitamins D.sub.2 and D.sub.3 are inherently biologically inactive and are converted into biologically active metabolites [1.alpha.,25-dihydroxy vitamin D.sub.3 (calcitriol) or -D.sub.2] only after hydroxylation at C-atom 25 in the liver and at C-atom 1 in the kidney. The action of the active metabolites involves the regulation of the calcium and phosphate concentration in the serum; they counteract a dropping of the calcium concentration in the serum by increasing the calcium absorption in the intestine and under certain circumstances promoting calcium mobilization from the bones. FIG. 1 shows known vitamin D derivatives together with the commonly used numbering diagram. [0004] In addition to their pronounced effect on the calcium and phosphate metabolism, the active metabolites of vitamins D.sub.2 and D.sub.3 and their synthetic derivatives have a proliferation-inhibiting and differentiation-stimulating action on tumor cells and normal cells, such as, for example, skin cells. In addition, a pronounced effect on cells of the immune system (inhibiting of proliferation and interleukin 2-synthesis of lymphocytes, increase of cytotoxicity and phagocytosis in vitro of monocytes) has been found, which manifests itself in an immunomodulatory action, and finally, because of a stimulating action on bone-forming cells, an increased formation of bone in normal and osteoporotic rats is found [R. Bouillon et al. "Short Term Course of 1,25(OH).sub.2D.sub.3 Stimulates Osteoblasts But Not Osteoclasts," Calc. Tissue Int. 49, 168 (1991)]. [0005] All actions are mediated by bonding to the vitamin D receptor. Because of the bonding, the activity of specific genes is regulated. [0006] When using biologically active metabolites of vitamins D.sub.2 and D.sub.3, a toxic effect on the calcium metabolism is produced (hypercalcemia). [0007] By structural manipulations of the side chain, therapeutically usable effectiveness can be separated from undesirable hypercalcemic activity. A suitable structural variant is the introduction of 24-hydroxy derivatives. [0008] 1.alpha.-Cholecalciferols that are hydroxylated in 24-position are already described in DE 25 26 981. They have a lower toxicity than the corresponding non-hydroxylated 1.alpha.-cholecalciferol. Further, 24-hydroxy derivatives are described in the following patent applications: DE 39 33 034, DE 40 03 854, DE 40 34 730, EP 0 421 561, EP 0 441 467, WO 87/00834, and WO 91/12238. [0009] Finally, 25-carboxylic acid derivatives of calcitriol that are hydroxylated at C-24 are described in WO 94/07853, and said derivatives exhibit a more advantageous spectrum of action than calcitriol. The equivalent is also true for new vitamin D derivatives with substituents at C-25 (WO 97/00242). While the ability to trigger a hypercalcemia is considerably weakened, proliferation-inhibiting and differentiation-stimulating actions are maintained. Generally, however, the introduction of the 24-hydroxyl group results in metabolic destabilization of the derivatives, especially if a cyclopropyl ring is in the neigboring position. For this reason, these compounds are only conditionally suitable for systemic administration. [0010] There is therefore a need for new vitamin D derivatives that have as advantageous a spectrum of action as the compounds that are described in the prior art (especially WO 94/07853 and WO 97/00242), but that are better suited for systemic administration owing to their higher metabolic stability. [0011] The object of this patent application is to make available such vitamin D derivatives. This object is achieved by the compounds that are disclosed in the claims. [0012] This invention therefore relates to vitamin D derivatives of general formula I, 2 [0013] in which [0014] Y.sub.1 means a hydrogen atom, a hydroxyl group, a fluorine, chlorine or bromine atom or a group --O(CO)R.sub.8, in which [0015] R.sub.8 is an aliphatic or aromatic radical with 1 to 12 C atoms, [0016] Y.sub.2 means a hydrogen atom or a group --(CO)R.sub.9, in which [0017] R.sub.9 is an aliphatic or aromatic radical with 1 to 12 C atoms, [0018] R.sub.1 and R.sub.2 each mean a hydrogen atom or together an exocyclic methylene group, [0019] R.sub.3 and R.sub.41 independently of one another, mean a hydrogen atom, a chlorine or fluorine atom, an alkyl group with 1 to 4 carbon atoms, together a methylene group or together with quaternary carbon atom 20 a 3- to 7-membered, saturated or unsaturated carbocyclic ring, [0020] V and W together mean an E-double bond or V means a hydroxyl group and W means a hydrogen atom, [0021] Q means a straight-chain or branched carbon unit with up to 10 carbon atoms, which at any positions can have .alpha.- or .beta.-hydroxyl groups, which in turn can be etherified or esterified, keto groups, amino groups or halogen atoms, [0022] Z means a straight-chain or branched-chain, saturated or unsaturated hydrocarbon radical with up to 12 carbon atoms, which at any positions can have keto groups, .alpha.- or .beta.-hydroxyl groups, which in turn can be etherified or esterified, amino groups, fluorine, chlorine, or bromine atoms. [0023] The invention also relates to a process for the production of the compounds according to the invention, intermediate products in the production process as well as use of the compounds according to the invention for the production of pharmaceutical agents. Continue reading... Full patent description for Verification of translation Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Verification of translation patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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