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  • Administration of 6 - (3 - (1-Adamantyl) - 4-Methoxyphenyl) - 2-Naphthoic Acid For The Treatment of Dermatological Disorders (US Patent 7579377)

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    U.S. patent 7579377: Administration of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid for the treatment of dermatological disorders. Granted to Graeber et. al. (2 total) on 2009-08-25 (filed 2004-09-10) and assigned to Galderma Research & Development. Currently involved in at least 1 patent litigation: Galderma Laboratories LP et. al. v. Actavis Mid Atlantic LLC (Delaware). See http://news.priorsmart.com for more info.

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    Administration of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid for the treatment of dermatological disorders (US patent 7579377)

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    U.S. patent 7579377: Administration of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid for the treatment of dermatological disorders. Granted to Graeber et. al. (2 total) on 2009-08-25 (filed 2004-09-10) and assigned to Galderma Research & Development. Currently involved in at least 1 patent litigation: Galderma Laboratories LP et. al. v. Actavis Mid Atlantic LLC (Delaware). See http://news.priorsmart.com for more info.

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    120 tayangan7 halaman

    Administration of 6 - (3 - (1-Adamantyl) - 4-Methoxyphenyl) - 2-Naphthoic Acid For The Treatment of Dermatological Disorders (US Patent 7579377)

    Diunggah oleh

    PriorSmart
    U.S. patent 7579377: Administration of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid for the treatment of dermatological disorders. Granted to Graeber et. al. (2 total) on 2009-08-25 (filed 2004-09-10) and assigned to Galderma Research & Development. Currently involved in at least 1 patent litigation: Galderma Laboratories LP et. al. v. Actavis Mid Atlantic LLC (Delaware). See http://news.priorsmart.com for more info.

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    w sy as) 7) ° 21) 2 6) @) @) 60) United States Patent Graeber et al. ADMINISTRATION OF 6[34(1-ADAMANTYL)-4-METHOXYPHENYL|- -NAPHITHOIC ACID FOR THE TREATMENT. (OF DERMATOLOGICAL DISORDERS. Inventors: Michael Graeber, Lawrenceville, NJ (US); Janusz, Czernielowskd, Biot (FR) Assignee: Galderma Research & Development, Biot (FR) Notice: Subject to any disclaimer, the term ofthis patent is extended or adjusted under 35 USC. 1544b) by T4 days Appl. No. 10997,612 Filed: Sep. 10,2004 a US 200810059740.A1 Mar, 17,2005 Publication Data Related US. Application Data Continuation of application No, PCTEPO303246, filed on Max, 12, 2003, Provisional application No, 60370.223 filed on Ape 8, 2002, Foreign Application Priority Data Mar, 12,2002 (FR) 0203070 1) 658) (56) Tat. CL AOIN 3710 (2006.01) AOIN 37700 (2006.01) AOIK 31/19 (2006.01) AGIK 31/188 (2006.01) 461K 82 (2006.01) us.c. 514/809; 514/577; 5141859; 424/401 s1ais6o, S14/577, 839; 4244401 ‘Se application file for complete serch istry References Cited U.S, PATENT DOCUMENTS, T1720 A I98E Shoot S00 y1S79371B2 10) Patent No. US 7,579,377 B2 (4s) Date of Patent: Aug. 25, 2009 7088.79 BL $2006 Giscomoni FOREIGN PATENT DOCUMENTS. Bp 0199636 1011986, FR 2730930 811996, WO WOOL28SS2 AZ 42001 OTHER PUBLICATIONS Healy tal. ts Motil Juma, 1994, vl. 308, 6732 pp. (Czemiclewski et al. Joural of Euopean Academy of Dermatology snd Vererlogy Dec. 200, vl. 15, Sopplement 3.99. 12." Difxn Get Data Shot avilable a of Nox. 1998 pp. 1-5 Alle «tal. “Skin Dstibtion and Pharmaceical Aspects of Adaplene Ge, Journal ofthe American Academy of Demitogy Inc 1997, pp, SLIS-S125, v0, 36, No. 6 Pat 2. ‘Shroot et "A new Concept of Drig Delivery fr Aene” Dera tology, 1998, pp. 165-17, vo. 196, No, IS Kargor AG Bass Rolland tal Sit-Spcie Drug Delivery to Plschaceous Su ‘ure Using Polymeric Microsphsres” Pharmaccuieal Research 1093, pp. 1738-174, vl 10, No. 12, Plenum Pblsing Comp. Jamoalle sal, "FllislarPentation and Distribution of Topical Applic CD 271, a New Naphihoic Acid Derwaive Intended or Topic Aene Treatment” Joural of Investigation Dermatology. 1990, pp 731-732. v.94, No.5 Alireza etal, “ude comparative delicate ela tolerance de ssdndapalenead, e003 p. 100 e¢@ungel detrtneine 10.025 100 dans letrtemen de acne” Ana. Demat. Venerol, 196, Pp. 165-170, vo. 123, No 3 (Extensive Summary in Els Huropea Search Rept for comesponding European Application EP (0500 3144 in English). International Seach Report for PCTIEPOS 03246) (in English. * cited by examiner Primary EsaminerSreeni Padmanabhan Assistant ExaminerSamira Jean-Louis (74) tonnes, Agent, or Firm—Buchanan, Ingersoll & Rooney PC 6 ABSTRACT Denmatologcal disorders having an inflammatory or prolif cative component are treated with pharmaceutical eomposi- ‘ions containing on the order of 0.3% by weight of 6.[341- adamanty)-4-methoxypbeny]]-2-naphthanoic id (dgpatene) or salt thereof, formulated into pharmaceutically acceptable mesa therefor, advantageously topically appli- cable gels, ereams or lotions, 3 Claims, 3 Drawing Sheets US. Patent Aug. 25,2009 Sheet 1 of 3 US 7,579,377 B2 Figure 1 Regression of total lesions mean US. Patent Aug. 25,2009 Sheet 2 of 3 US 7,579,377 B2 Figure 2 Regression of inflammatory lesions mean US. Patent Aug. 25,2009 Sheet 3 of 3 US 7,579,377 B2 Figure 3 Regression of non-inflammatory lesions mean US 7,579,377 B2 1 ADMINISTRATION OF 6{34(1-ADAMANTYL)-4-METHONYPHENYL}2- NAPHTHOIC ACID FOR THE TREATMENT ‘OF DERMATOLOGICAL DISORDERS. CROSS-REFERENCE TO PRIORITY:PCTPROVISIONAL APPLICATIONS ‘This application claims peoeity undee 35 USC. § 119 of FR02/03070, fled Mur. 12, 2002, and of provisional app cation Set. No. 60'370,223, filed Ape. 8, 2002, and is eon- ‘inuation of PCT/EP 03/03246 filed Mar. 12, 2003 and des- inating the United States (published in English on Sep. 18, 2008 as WO 031075908 A1), each hereby expressly incorpo- ‘ated by reference and each assigned tothe assignee hereo, BACKGROUND OF THE INVENTION |. Technical Field ofthe Invention ‘The present invention relates to the administration oindi- viduals in need of sueh treatment of 6-[3-(1-adamantyl) 4 smethoxyphenyl]-2-naphthanoic acid, the chemical stricture of which isa follows cooit 0° 8 inpharmaceotical compositions in particular dermatological ‘compositions, forthe tretmeat of dermatological slments! aflitions having an inflammatory oF proliferative compo nent 2, Description of Background andor Related andor Peo An 6-(341-Adamantyl)-4-methoxypheny]]-2-naphthanoic avid (hereinafter referred tas adapalene is aretinoid derived from naphthoic acid, having ant-inllammtory properties ‘This molecule has been the subject of development forthe topical teatment of common acne and dermatoses sensitive to retinoids Adapalene is deserbed in EP-0,199,636, and a process for synthesizing same is. described in’ EP-0;358,574, both assigned tothe assignee hereo. ‘The assignee hereof markets adapalene formulated st 3 ‘weight concentration of 0.1% inthe form of an alcoholic lotion, an aqueous gel and a cream, These compositions are suited forthe treatment of acne. Finally, adspalene is described as having a beneficial ‘ction on photo-damaged skin (Photographie assessment of the effets of adapalene 0.1% and 0.3% gels and vehicle on photo-damaged skin. M, Goldlxb et al, Clinical Dermatol ‘oy, Vienna, Austria, May 2000), SUMMARY OF THE INVENTION « "Novel pharmaceutical compositions have now been devel- oped contsising apalene ata weight concentration of 0.3% 2 formulated into pharmaceutically acceptable media therefor, ‘sefl forthe treatment (epime or regimen) of dermatologi- cal ailments, conditions oraillicdonshaving an inflammatory ‘or proliferative component. Specifically, i has now surpris- ingly boen shown tat, in adsition to exhibiting better thera- peutic elicacy compared to known compositions, the com positions according othe invention exhibits pond tolerance, ‘comparable to those of the known compositions witha lower cconcentation of ative principle ‘The results regarding tolerance observed in als relating to photo-damaged skin (indication “photodamago"), obiained on individuals on average 65 years old, could not be exploited inthe context ofthe present invention. Specifically, asregands use of adapalene on young individuals (in particu lar regarding aene with populations of teenagers of young, dul), the skin exhibits very different physiopathoiogical charctristcs (presence of many lesions, in particular inflammatory lesions, modifying skin permeability. hyper- comification of he follicular channel, immuno response, bac ‘eral colonization ofthe skin (2 aenes), sebaceous hyperpla- sia with hyperseborthea). DETAILED DESCRIPTION OF BEST MODE AND SPECIFIC/PREFERRED EMBODIMENTS ‘OP THE INVENTION ‘Thus, the present invention features formulating 6-[3-(1- adamantyl)-4-methoxyphenyl-2-naphthanoic acid (alae palene), ort sts, into pharmaceutical eompositons wsef forthe treatment of dermatological ailments, conditions or afictions having an inflammatory or prokferaive campo ‘nent, such phamaceatical eompositios comprising 0.3% by ‘weigh of adapalene relative tothe total weight ofthe com postion “The tenn “odapolene sul” is intended to mean the salts formed witha pharmaceutically acceptable bse, in particular organi bass such as sodium hydroxide, potassium hydrox {de and aqueous ammonia, or organic bases such a Isine, angnine or N-methyglocamine. “The term “adapalene salts” is also intended to mean the salts formed with fatty amines such as dioetylamine and stearylamine The administration of the compositions according to the ‘vention may be erred out enteral parenterally topically oroceulary ‘The pharmaceutical compositions according tothe inven- tion are preferably aainisered topically Enteral, the pharmaceutical composition may be inthe form of tablets, gelatin capsules, dragées, syrups, suspen- sions, solutions, powders, grannles, emulsions, oF suspen sions of mirospheres or nanospheres or of lipidor polymeric ‘vesicles for controled eeease, Parenteral, the phamaceu tical composition may be inthe fom of solutions or suspen sions for infsion or for injection. ‘Topically, the pharmaceutical compositions accoring 0 the invention are more particulary suited fr treatment ofthe skin andthe mucous membranes, and may be in the form of cinments,ersams, milks, pomades, powders, impregnated pads, solution, gels, sprays, lotions or suspensions. They ‘may also bein the form of suspensions of microspheres or inanosperesorflipidor polymeric vesics orof polymeric patches and hydrogels for controlled eease. These compo sitions for topical application may be in anhydrous fom, in aqueoss form o inthe form ofan emulsion Ina prefered embodiment of the invention, the pharma

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