Claims for Patent: 7,572,776

Summary for Patent: 7,572,776

Title:	N-(phosphonoalkyl)-amino acids, derivatives thereof and compositions and methods of use
Abstract:	The present invention relates to an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof, the N-(phosphonoalkyl)-amino acid, related compound or derivative thereof being in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, other than N-(phosphonomethyl)-glycine or N,N-bis(phosphonomethyl)-glycine. Also included is a composition including an N-(phosphonoalkyl)-amino acid, a related compound or a derivative thereof in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, and a cosmetically or pharmaceutically acceptable vehicle for topical or systemic administration to a mammalian subject, as well as a method of administering an effective amount of such a composition for alleviating or improving a condition, disorder, symptom or syndrome associated with at least one of a nervous, vascular, musculoskeletal or cutaneous system.
Inventor(s):	Yu; Ruey J. (Chalfont, PA), Van Scott; Eugene J. (Abington, PA)
Assignee:
Application Number:	12/194,203
Patent Claims:	1. A method of alleviating or improving a cosmetic condition or dermatological indication of the cutaneous system, the method comprising topically administering to a mammalian subject an effective amount of a composition comprising an N-(phosphonomethyl)-amino acid, a related compound or a derivative thereof, as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomeric or non-stereoisomeric form, wherein the N-(phosphonomethyl)-amino acid, a related compound or a derivative thereof, is N-(phosphonomethyl)-proline or has the following formula: R.sub.1CH(NR.sub.2R.sub.3)(CH.sub.2).sub.mCOR.sub.4 wherein R.sub.1is H, an alkyl, aralkyl or aryl group having up to 19 carbon atoms; R.sub.1 also optionally carries OH, SH, SCH.sub.3, NH.sub.2, NR.sub.2R.sub.3, COR.sub.4, NHCONH.sub.2, NHC(=NR.sub.2)NH.sub.2, imidazole or pyrrolidine radical; m is an integer from 0 to 5; R.sub.2 is a phosphonomethyl group having a formula (HO).sub.2PO(CH.sub.2); R.sub.3 is H or a phosphonomethyl group having a formula (HO).sub.2PO(CH.sub.2); R.sub.4 is NH.sub.2or OR.sub.5, R.sub.5 is H, an alkyl, aralkyl or aryl group having up to 19 carbon atoms; and the H attached to any carbon atom can be substituted by I, F, Cl, Br, OH or an alkoxy group having up to 9 carbon atoms; wherein the cosmetic condition or dermatological indication is selected from the group consisting of deranged or disordered cutaneous or mucocutaneous tissue relevant to skin, nail and hair; oral, vaginal and anal mucosa; disturbed keratinization; inflammation; changes associated with intrinsic and extrinsic aging; acne; rosacea; age spots; blemished skin; blotches; cellulite; dermatoses; dermatitis; skin, nail and hair infections; dandruff dryness or looseness of skin, nail and hair; xerosis; eczema; elastosis; herpes; hyperkeratosis; hyperpigmented skin; ichthyosis; keratoses; lentigines; melasmas; mottled skin; pseudofolliculitis barbae; photoaging and photodamage; pruritus; psoriasis; skin lines; stretch marks; thinning of skin, nail plate and hair; warts; wrinkles; oral or gum disease; damaged or abnormal mucosa, skin, hair, nail, nostril, ear canal, anal or vaginal conditions; breakdown, defective synthesis or repair of dermal components; abnormal or diminished synthesis of collagen, glycosaminoglycans, proteoglycans and elastin, as well as diminished levels of such components in the dermis; uneven skin tone; uneven and rough surface of skin, nail and hair; loss or reduction of skin, nail and hair resiliency, elasticity and recoilability; laxity; lack of skin, nail and hair lubricants and luster; fragility and splitting of nail and hair; yellowing skin; reactive, irritating or telangiectatic skin; and dull and older-looking skin, nail and hair; cosmetic condition or dermatological indication general care of skin, nail and hair; to improve skin texture and pores and flakiness; to make skin soft, smooth, fresh, balanced, visibly clear, even-toned and brighter; to increase skin fullness and plumpness; and for skin bleach and lightening and wound healing. 2. The method of claim 1, wherein the cosmetic condition or dermatological indication is selected from the group consisting of acne; rosacea; age spots; dryness or looseness of skin, nail and hair; eczema; hyperpigmented skin; ichthyosis; keratoses; lentigines; melasmas; photoaging and photodamage; pruritus; psoriasis; skin lines; stretch mark; warts; wrinkles; defective synthesis or repair of dermal components; abnormal or diminished synthesis of collagen, glycosaminoglycans, proteoglycans and elastin, uneven skin tone; uneven and rough surface of skin, nail and hair; loss or reduction of skin, nail and hair resiliency, elasticity and recoilability; laxity; lack of skin, nail and hair lubricants and luster; fragility and splitting of nail and hair; yellowing skin; and dull and older-looking skin, nail and hair. 3. The method of claim 1, wherein the cosmetic condition or dermatological indication is selected from the group consisting of acne; rosacea; age spots; dryness or looseness of skin, nail and hair; eczema; hyperpigmented skin; ichthyosis; keratoses; lentigines; melasmas; photoaging and photodamage; pruritus; psoriasis; skin lines; stretch mark; warts and wrinkles. 4. The method of claim 1, wherein the N-(phosphonomethyl)-amino acid, in a form as a free acid, salt, partial salt, lactone, amide or ester, or in a stereoisomeric or non-stereoisomeric form, is selected from the group consisting of N-(phosphonomethyl)-alanine, N-(phosphonomethyl)-arginine, N-(phosphonomethyl)-asparagine, N-(phosphonomethyl)-aspartic acid, N-(phosphonomethyl)-cysteine, N-(phosphonomethyl)-glutamic acid, N-(phosphonomethyl)-glutamine, N-(phosphonomethyl)-glycine, N-(phosphonomethyl)-histidine, N-(phosphonomethyl)-isoleucine, N-(phosphonomethyl)-leucine, N-(phosphonomethyl)-lysine, N-(phosphonomethyl)-methionine, N-(phosphonomethyl)-phenylalanine, N-(phosphonomethyl)-proline, N-(phosphonomethyl)-serine, N-(phosphonomethyl)-threonine, N-(phosphonomethyl)-tryptophan, N-(phosphonomethyl)-tyrosine and N-(phosphonomethyl)-valine. 5. The method of claim 1, wherein the N-(phosphonoalkyl)-amino acid compound, related compound or compound derived therefrom, in a form as a free acid, salt, partial salt, lactone, amide or ester, or in stereoisomenc or non-stereoisomeric form, is selected from the group consisting of N-(phosphonomethyl)-.beta.-alanine, N-(phosphonomethyl)-.gamma.-aminobutanoic acid, N-(phosphonomethyl)-.beta.-aminoisobutanoic acid, N-(phosphonomethyl)-anserine, N-(phosphonomethyl)-aminolevulinic acid, N-(phosphonomethyl)-carnosine, N-(phosphonomethyl)-canaline, N-(phosphonomethyl)-canavanine, N-(phosphonomethyl)-citrulline, N-(phosphonomethyl)-creatine, N-(phosphonomethyl)-creatinine, N-(phosphonomethyl)-cysteine sulfinic acid, N-(phosphonomethyl)-cystine, N-(phosphonomethyl)-cycloserine, N-(phosphonomethyl)-dopa [N-(phosphonomethyl)-3,4-dihydroxyphenylalanine], N-(phosphonomethyl)-dopamine (hydroxytyramine), N-(phosphonomethyl)-ethionine, N-(phosphonomethyl)-glutathione, N-(phosphonomethyl)-guanidinoacetic acid, N-(phosphonomethyl)-3-guanidinopropanoic acid, N-(phosphonomethyl)-4-guanidinobutanoic acid, N-(phosphonomethyl)-homocamosine, N-(phosphonomethyl)-homocysteine, N-(phosphonomethyl)-homoserine, N-(phosphonomethyl)-4-hydroxyphenylglycine, N-(phosphonomethyl)-hydroxyglutamic acid, N-(phosphonomethyl)-hydroxylysine, N-(phosphonomethyl)-hydroxyproline, N-(phosphonomethyl)-hypusine, N-(phosphonomethyl)-homoarginine, N-(phosphonomethyl)-homocitrulline, N-(phosphonomethyl)-homocystine, N-(phosphonomethyl)-homophenylalanine, N-(phosphonomethyl)-homotryptophan, N-(phosphonomethyl)-hydroxylysine, N-(phosphonomethyl)-hydroxyarginine, N-(phosphonomethyl)-hydroxyhomoarginine, N-(phosphonomethyl)-hydroxycitrulline, N-(phosphonomethyl)-hydroxyomithine, N-(phosphonomethyl)-hydroxyvaline, N-(phosphonomethyl)-indospicine, N-(phosphonomethyl)-methoxinine, N-(phosphonomethyl)-methylarginine, N-(phosphonomethyl)-methylhistidine, N-(phosphonomethyl)-methyllysine, N-(phosphonomethyl)-methylornithine, N-(phosphonomethyl)-methylserine, N-(phosphonomethyl)-norvaline, N-(phosphonomethyl)-omithine, N-(phosphonomethyl)-oxalysine, N-(phosphonomethyl)-penicillamine (N-phosphonomethyl-dimethylcysteine), N-(phosphonomethyl)-phenylglycine, N-(phosphonomethyl)-3-phenylserine, N-(phosphonomethyl)-sarcosine (N-phosphonomethyl-N-methyl-glycine), N-(phosphonomethyl)-serotonin (N-phosphonomethyl-hydroxytryptamine), N-(phosphonomethyl)-taurine, N-(phosphonomethyl)-tryptamine and N-(phosphonomethyl)-tyramine. 6. The method of claim 1, wherein the composition further comprises a cosmetic, pharmaceutical or other topically active agent. 7. The method of claim 6, wherein the cosmetic, pharmaceutical or other topically active agent is selected from the group consisting of hydroxyacids, ketoacids and related compounds; phenyl alpha acyloxyalkanoic acids and derivatives; N-acyl-aldosamines, N-acylamino acids and related N-acyl compounds; local analgesics and anesthetics; anti-acne agents; anti-bacterial agents; anti-yeast agents; anti-fungal agents; anti-viral agents; anti-infective agents; anti-dandruff agents; anti-dermatitis agents; anti-eczema agents; anti-histamine agents; anti-pruritic agents; anti-emetics; anti-motion sickness agents; anti-inflammatory agents; anti-hyperkeratotic agents; antiperspirants; anti-psoriatic agents; anti-rosacea agents; anti-seborrheic agents; hair conditioners and hair treatment agents; anti-aging and anti-wrinkle agents; anti-anxiety agents; anti-convulsant agents; anti-depressant agents; sunblock and sunscreen agents; skin tightening agents; depigmenting agents; astringents; cleansing agents; corn, callus or wart removing agents; skin plumping agents; skin volumizing agents; skin firming agents; matrix metalloproteinase (MMP) inhibitors; topical cardiovascular agents; wound-healing agents; gum disease or oral care agents; amino acids; peptides; dipeptides; tripeptides; glutathione and its derivatives; oligopeptides; polypeptides; carbohydrates; aminocarbohydrates; vitamins; corticosteroids; tanning agents; hormones and retinoids. 8. The method of claim 7, wherein the cosmetic, pharmaceutical or other topically active agent is selected from the group consisting of: abacavir, abciximab, acamprosate, acarbose, acebutolol, acetaminophen, acetaminosalol, acetazolamide, acetic acid, acetohydroxamic acid, N-acetylcysteine and its esters, N-acetylglutathione and its esters, acitretin, aclometasone dipropionate, acrivastine, acthrel, actidose, actigall, acyclovir, adalimumab, adapalene, adefovir dipivoxil, adenosine, agalsidase, albendazole, albumin, albuterol, aldesleukin, alefacept, alemtuzumab, alendronate, alfuzosin, alitretinoin, allantoin, allium, allopurinol, alloxanthine, almotriptan, alosetron, alpha tocopheral, alpha.sub.1-proteinase, alprazolam, alprenolol, alprostadil, alteplase, altretamine, aluminum acetate, aluminum chloride, aluminum chlorohydroxide, aluminum hydroxide, amantadine, amifostine, amiloride, aminacrine, amino acid, aminobenzoate, p-aminobenzoic acid, aminocaproic acid, aminohippurate, aminolevulinic acid, aminosalicylic acid, amiodarone, amitriptyline, amlodipine, amocarzine, amodiaquin, amorolfine, amoxapine, amoxicillin, amphetamine, amphotericin, ampicillin, amprenavir, anagrelide, anakinra, anastrozole, anisindione, anthralin, antihemophilic, antithrombin, anti-thymocyte, antivenin, apomorphine, aprepitant, aprotinin, arbutin, argatroban, aripiprazole, arnica, ascorbic acid and its esters, ascorbyl palmitate, aspirin, atazanavir, atenolol, atomoxetine, atorvastatin, atovaquone, atropine, azathioprine, azelaic acid, azelastine, azithromycin, baclofen, bacitracin, balsalazide, balsam, basiliximab, beclomethasone dipropionate, bemegride, benazepril, bendroflumethiazide, benzocaine, benzonatate, benzophenone, benzoyl peroxide, benztropine, bepridil, beta carotene, betamethasone dipropionate, betamethasone valerate, betaxolol, bethanechol, bevacizumab, bexarotene, bicalutamide, bimatoprost, bioflavonoids, biotin, biperiden, bisacodyl, bisoprolol, bivalirudin, bortezomib, bosentan, botulinum, brimonidine, brinzolamide, bromocriptine, brompheniramine, budesonide, bumetanide, bupivacaine, buprenorphine, bupropion, burimamide, buspirone, busulfan, butabarbital, butalbital, butenafine, butoconazole, butorphanol, butyl aminobenzoate, cabergoline, caffeic acid, caffeine, calcipotriene, calcitonin-salmon, calcitriol, calfactant, camellia sinensis, camphor, candesartan cilexetil, capecitabine, capreomycin, capsaicin, captopril, carbamazepine, carbamide peroxide, carbidopa, carbinoxamine, cefditoren pivoxil, cefepime, cefpodoxime proxetil, celecoxib, cetirizine, cevimeline, chitosan, chiordiazepoxide, chlorhexidine, chloroquine, chlorothiazide, chloroxylenol, chiorpheniramine, chlorpromazine, chlorpropamide, ciclopirox, cilostazol, cimetidine, cinacalcet, ciprofloxacin, citalopram, citric acid, cladribine, clarithromycin, clemastine, clindamycin, clioquinol, clobetasol propionate, clocortolone pivalate, clomiphene, clonidine, clopidogrel, clotrimazole, clozapine, coal tar, coal tar extracts (LCD), codeine, cromolyn, crotamiton, cyclizine, cyclobenzaprine, cycloserine, cytarabine, dacarbazine, dalfopristin, dapsone, daptomycin, daunorubicin, deferoxamine, dehydroepiandrosterone, delavirdine, desipramine, desloratadine, desmopressin, desoximetasone, dexamethasone, dexmedetomidine, dexmethylphenidate, dexrazoxane, dextroamphetamine, diazepam, diclofenac, dicyclomine, didanosine, dihydrocodeine, dihydromorphine, diltiazem, 6,8-dimercaptooctanoic acid (dihydrolipoic acid), diphenhydramine, diphenoxylate, dipyridamole, disopyramide, dobutamine, dofetilide, dolasetron, donepezil, dopa esters, dopamide, dopamine, dorzolamide, doxepin, doxorubicin, doxycycline, doxylamine, doxepin, duloxetine, dyclonine, econazole, efalizumab, eflornithine, eletriptan, emtricitabine, enalapril, ephedrine, epinephrine, epinine, epirubicin, eptifibatide, ergotamine, erythromycin, escitalopram, esmolol, esomeprazole, estazolam, estradiol, etanercept, ethacrynic acid, ethinyl estradiol, etidocaine, etomidate, famciclovir, famotidine, felodipine, fentanyl, ferulic acid, fexofenadine, flecainide, fluconazole, flucytosine, fluocinolone acetonide, fluocinonide, 5-fluorouracil, fluoxetine, fluphenazine, flurazepam, fluticasone propionate, fluvoxamine, formoterol, furosemide, galactarolactone, galactonic acid, galactonolactone, galantamine, gatifloxacin, gefitinib, gemcitabine, gemifloxacin, glucarolactone, gluconic acid, gluconolactone, glucuronic acid, glucuronolactone, glycolic acid, griseofulvin, guaifenesin, guanethidine, N-guanyihistamine, haloperidol, haloprogin, hexyiresorcinol, homatropine, homosalate, hydralazine, hydrochiorothiazide, hydrocortisone, hydrocortisone 21-acetate, hydrocortisone 17-butyrate, hydrocortisone 17-valerate, hydrogen peroxide, hydromorphone, hydroquinone, hydroquinone monoether, hydroxyzine, hyoscyamine, hypoxanthine, ibuprofen, ichthammol, idarubicin, imatinib, imipramine, imiquimod, indinavir, indomethacin, infliximab, irbesartan, irinotecan, isoetharine, isoproterenol, itraconazole, kanamycin, ketamine, ketanserin, ketoconazole, ketoprofen, ketotifen, kojic acid, labetalol, lactic acid, lactobionic acid, lamivudine, lamotrigine, lansoprazole, letrozole, leuprolide, levalbuterol, levofloxacin, lidocaine, linezolid, lobeline, loratadine, loperamide, losartan, loxapine, lysergic diethylamide, mafenide, malic acid, maltobionic acid, mandelic acid, maprotiline, mebendazole, mecamylamine, meclizine, meclocycline, memantine, menthol, meperidine, mepivacaine, mequinol, mercaptopurine, mescaline, metanephrine, metaproterenol, metaraminol, metformin, methadone, methamphetamine, methotrexate, methoxamine, methyldopa esters, methyldopamide, 3,4-methylenedioxymethamphetamine, methyllactic acid, methyl nicotinate, methyiphenidate, methyl salicylate, metiamide, metolazone, metoprolol, metronidazole, mexiletine, miconazole, midazolam, midodrine, miglustat, minocycline, minoxidil, mirtazapine, mitoxantrone, moexiprilat, molindone, monobenzone, morphine, moxifloxacin, moxonidine, mupirocin, nadolol, naftifine, nalbuphine, nalmefene, naloxone, naproxen, nefazodone, nelfinavir, neomycin, nevirapine, nicardipine, nicotine, nifedipine, nimodipine, nisoldipine, nitrofurantoin, nizatidine, norepinephrine, nystatin, octopamine, octreotide, octyl methoxycinnamate, octyl salicylate, ofloxacin, olanzapine, olmesartan medoxomil, olopatadine, omeprazole, ondansetron, oxiconazole, oxotremorine, oxybenzone, oxybutynin, oxycodone, oxymetazoline, padimate O, palonosetron, pantothenic acid, pantoyl lactone, paroxetine, pemoline, penciclovir, penicillamine, penicillins, pentazocine, pentobarbital, pentostatin, pentoxifylline, pergolide, perindopril, permethrin, phencyclidine, pheneizine, pheniramine, phenmetrazine, phenobarbital, phenol, phenoxybenzamine, phentolamine, phenylephrine, phenyipropanolamine, phenytoin, physostigmine, pilocarpine, pimecrolimus, pimozide, pindolol, pioglitazone, pipamazine, piperonyl butoxide, pirenzepine, podofilox, povidone iodine, pramipexole, pramoxine, prazosin, prednisone, prenalterol, prilocaine, procainamide, procaine, procarbazine, promazine, promethazine, promethazine propionate, propafenone, propoxyphene, propranolol, propylthiouracil, protriptyline, pseudoephedrine, pyrethrin, pyrilamine, pyrimethamine, quetiapine, quinapril, quinethazone, quinidine, quinupristin, rabeprazole, reserpine, resorcinol, retinal, 13-cis retinoic acid, retinoic acid, retinol, retinyl acetate, retinyl palmitate, ribavirin, ribonic acid, ribonolactone, rifampin, rifapentine, rifaximin, riluzole, nmantadine, risedronic acid, risperidone, ritodrine, rivastigmine, rizatriptan, ropinirole, ropivacaine, salicylamide, salicylic acid, salmeterol, scopolamine, selegiline, selenium sulfide, serotonin, sertaconazole, sertindole, sertraline, shale tar, sibutramine, sildenafil, sotalol, streptomycin, strychnine, sulconazole, sulfacetamide, sulfabenz, sulfabenzamide, sulfabromomethazine, sulfacetamide (sodium sulfacetamide), sulfachiorpyridazine, sulfacytine, sulfadiazine, sulfadimethoxine, sulfadoxine, sulfaguanole, sulfalene, sulfamethizole, sulfamethoxazole, sulfanilamide, sulfapyrazine, sulfapyridine, sulfasalazine, sulfasomizole, sulfathiazole, sulfisoxazole, sulfur, tacrolimus, tadalafil, tamsulosin, tartaric acid, tazarotene, tegaserod, telithromycin, telmisartan, temozolomide, tenofovir disoproxil, terazosin, terbinafine, terbutaline, terconazole, terfenadine, tetracaine, tetracycline, tetrahydrozoline, thalidomide, theobromine, theophylline, thiabendazole, thioctic acid (lipoic acid), thioridazine, thiothixene, thymol, tiagabine, timolol, tinidazole, tioconazole, tirofiban, tizanidine, tobramycin, tocainide, tolazoline, tolbutamide, tolnaftate, tolterodine, tramadol, tranylcypromine, trazodone, triamcinolone acetonide, triamcinolone diacetate, triamcinolone hexacetonide, triamterene, triazolam, triclosan, triflupromazine, trimethoprim, trimipramine, tripelennamine, triprolidine, tromethamine, tropic acid, tyramine, undecylenic acid, urea, urocanic acid, ursodiol, valacyclovir, vardenafil, venlafaxine, verapamil, vitamin B acetate, voriconazole, warfarin, wood tar, xanthine, zafirlukast, zaleplon, zinc pyrithione, ziprasidone, zolmitriptan and zolpidem.

Details for Patent 7,572,776

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Ferring Pharmaceuticals Inc.	ACTHREL	corticorelin ovine triflutate	For Injection	020162	05/23/1996		2026-01-10
Bayer Healthcare Pharmaceuticals Inc.	TRASYLOL	aprotinin	Injection	020304	12/29/1993		2026-01-10
Ony Biotech Inc.	INFASURF	calfactant	Suspension	020521	07/01/1998		2026-01-10
Ony Biotech Inc.	INFASURF	calfactant	Suspension	020521	12/12/2002		2026-01-10