발생일자 2014.12.09 

사건번호 1:14-cv-01028 

법원국가 UNITED STATES OF AMERICA 

관할법원명 D.C.M.D.NorthCarolina(지방법원) 

침해권리 특허 

원고명 Duke University/ Allergan, Inc ( 미국 / 외국기업 )  

피고명 Apotex, Inc./ Apotex Corp. ( 캐나다 / 외국기업 )  

소송유형 침해금지 

[Duke University et al v. Apotex, Inc. et al] 사건번호 1:14-cv-01028에 따르면 원고 Duke University/ Allergan, Inc는 피고 Apotex, Inc./ Apotex Corp.을 상대로 특허 US8906962를 침해하였다는 이유로 미국 노스캐롤라이나 중부 지방법원에 소를 제기하였다. 

분쟁결과 분쟁중 

산업분류 화학∙바이오 > 의약품 

계쟁제품 Bimatoprost Topical Solution, 0.03%, generic version of Latisse

지재권번호/명칭

US8906962   Compositions and methods for treating hair loss using non-naturally occurring prostaglandins 

Abstract

A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth. 

What is claimed is: 

 1. A method of growing hair, wherein the method comprises topically applying to mammalian skin a safe and effective amount of a composition comprising: A) an active ingredient selected from the group consisting of a prostaglandin F analog of the following structure: ##STR00111## and pharmaceutically acceptable salts thereof; wherein R.sup.1 is selected from the group consisting of C(O)NHOH, CH.sub.2OH, S(O).sub.2R.sup.3, C(O)NHR.sup.3, C(O)NHS(O).sub.2R.sup.4, and tetrazole; R.sup.2 is selected from the group consisting of a hydrogen atom, a lower heterogeneous group, and a lower monovalent hydrocarbon group; R.sup.3 is selected from the group consisting of a monovalent hydrocarbon group, a heterogeneous group, a carbocyclic group, a heterocyclic group, an aromatic group, a heteroaromatic group, a substituted monovalent hydrocarbon group, a substituted heterogeneous group, a substituted carbocyclic group, a substituted heterocyclic group, a substituted aromatic group, and a substituted heteroaromatic group; R.sup.4 is selected from the group consisting of a monovalent hydrocarbon group, a heterogeneous group, a carbocyclic group, a heterocyclic group, an aromatic group, a heteroaromatic group, a substituted monovalent hydrocarbon group, a substituted heterogeneous group, a substituted carbocyclic group, a substituted heterocyclic group, a substituted aromatic group, and a substituted heteroaromatic group; X is selected from the group consisting of --CC--, a covalent bond, --CH.dbd.C.dbd.CH--, --CH.dbd.CH--, --CH.dbd.N--, --C(O)--, --C(O)Y--, --(CH.sub.2).sub.n--, wherein n is 2 to 4, --CH.sub.2NH--, --CH.sub.2S--, and --CH.sub.2O--; Y is selected from the group consisting of a sulfur atom, an oxygen atom, and NH; and Z is selected from the group consisting of a carbocyclic group, a heterocyclic group, an aromatic group, a heteroaromatic group, a substituted carbocyclic group, a substituted heterocyclic group, a substituted aromatic group, and a substituted heteroaromatic group. 

 2. The method of claim 1, wherein R.sup.1 is selected from the group consisting of C(O)NHOH, C(O)NHR.sup.3, and C(O)NHS(O).sub.2R.sup.4, and tetrazole. 

 3. The method of claim 1, wherein R.sup.2 is a hydrogen atom. 

 4. The method of claim 1, wherein R.sup.3 is selected from the group consisting of methyl, ethyl, and isopropyl. 

 5. The method of claim 1, wherein Z is an aromatic ring. 

 6. The method of claim 1, wherein the composition is a topical composition in a form selected from the group consisting of solutions, oils, creams, ointments, gels, lotions, shampoos, leave-on and rinse-out hair conditioners, milks, cleansers, moisturizers, sprays, and skin patches. 

 7. The method of claim 1, wherein the composition is a topical composition further comprising B) a carrier, wherein the carrier is selected from the group consisting of water, alcohols, aloe vera gel, allantoin, glycerin, vitamin A and E oils, mineral oil, propylene glycol, dimethyl isosorbide, polypropylene glycol, 2 myristyl propionate, and combinations thereof. 

 8. The method of claim 1, wherein the composition further comprises C) an activity enhancer selected from the group consisting of i) a hair growth stimulant, ii) a penetration enhancer, and combinations thereof. 

 9. The method of claim 8, wherein component i) is selected from the group vasodilator, an antiandrogen, a cyclosporin, a cyclosporin analog, an antimicrobial, an anti-inflammatory, a thyroid hormone, a thyroid hormone derivative, and a thyroid hormone analog, a non-selective prostaglandin agonist, a non-selective prostaglandin antagonist, a retinoid, a triterpene, and combinations thereof. 

 10. The method of claim 8, wherein component ii) is selected from the group consisting of 2-methyl propan-2-ol, propan-2-ol, ethyl-2-hydroxypropanoate, hexan-2,5-diol, polyoxyethylene(2) ethyl ether, di(2-hydroxypropyl) ether, pentan-2,4-diol, acetone, polyoxyethylene(2) methyl ether, 2-hydroxypropionic acid, 2-hydroxyoctanoic acid, propan-1-ol, 1,4-dioxane, tetrahydrofuran, butan-1,4-diol, propylene glycol dipelargonate, polyoxypropylene 15 stearyl ether, octyl alcohol, polyoxyethylene ester of oleyl alcohol, oleyl alcohol, lauryl alcohol, dioctyl adipate, dicapryl adipate, di-isopropyl adipate, di-isopropyl sebacate, dibutyl sebacate, diethyl sebacate, dimethyl sebacate, dioctyl sebacate, dibutyl suberate, dioctyl azelate, dibenzyl sebacate, dibutyl phthalate, dibutyl azelate, ethyl myristate, dimethyl azelate, butyl myristate, dibutyl succinate, didecyl phthalate, decyl oleate, ethyl caproate, ethyl salicylate, isopropyl palmitate, ethyl laurate, 2-ethyl-hexyl pelargonate, isopropyl isostearate, butyl laurate, benzyl benzoate, butyl benzoate, hexyl laurate, ethyl caprate, ethyl caprylate, butyl stearate, benzyl salicylate, 2-hydroxypropanoic acid, 2-hydroxyoctanoic acid, dimethyl sulphoxide, N,N-dimethyl acetamide, N,N-dimethyl formamide, 2-pyrrolidone, 1-methyl-2-pyrrolidone, 5-methyl-2-pyrrolidone, 1,5-dimethyl-2-pyrrolidone, 1-ethyl-2-pyrrolidone, phosphine oxides, sugar esters, tetrahydrofurfural alcohol, urea, diethyl-m-toluamide, 1-dodecylazacyloheptan-2-one, and combinations thereof. 

 11. The method of claim 1, wherein the composition is a topical composition locally administered on the skin once per day. 

 12. The method of claim 11, wherein the composition is administered once per day for 6 to 12 weeks. 

 13. The method of claim 1, wherein the composition is topically applied directly to the locus of desired hair growth. 

 14. The method of claim 1, wherein the prostaglandin F analog is selective for an FP receptor over an excitatory prostaglandin receptor in a ratio of at least 1:10. 

 15. The method of claim 1, wherein the prostaglandin F analog is selective for an FP receptor over an excitatory prostaglandin receptor in a ratio of at least 1:20. 

 16. The method of claim 1, wherein the prostaglandin F analog is selective for an FP receptor over an excitatory prostaglandin receptor in a ratio of at least 1:50. 

 17. A method of growing hair, wherein the method comprises topically applying to mammalian skin a safe and effective amount of a composition comprising: A) an active ingredient selected from the group consisting of a prostaglandin F analog of the following structure: ##STR00112## and pharmaceutically acceptable salts thereof; wherein R.sup.1 is selected from the group consisting of C(O)NHOH, C(O)NHR.sup.3, C(O)NHS(O).sub.2R.sup.4 and tetrazole; R.sup.2 is a hydrogen atom; R.sup.3 is methyl, ethyl or isopropyl; R.sup.4 is phenyl; X is selected from the group consisting of --C.ident.C--, a covalent bond, --CH.dbd.C.dbd.CH--, --CH.dbd.CH--, --CH.dbd.N--, --C(O)--, --C(O)Y--, and --(CH.sub.2).sub.n--, wherein n is 2 to 4; Y is selected from the group consisting of a sulfur atom, an oxygen atom, and NH; and Z is selected from the group consisting of a carbocyclic group, a heterocyclic group, an aromatic group, a heteroaromatic group, a substituted carbocyclic group, a substituted heterocyclic group, a substituted aromatic group, and a substituted heteroaromatic group. 

 18. The method of claim 17, wherein Z is an aromatic ring. 

 19. The method of claim 17, wherein the composition is a topical composition in a form selected from the group consisting of solutions, oils, creams, ointments, gels, lotions, shampoos, leave-on and rinse-out hair conditioners, milks, cleansers, moisturizers, sprays, and skin patches. 

 20. The method of claim 17, wherein the composition is a topical composition further comprising B) a carrier, wherein the carrier is selected from the group consisting of water, alcohols, aloe vera gel, allantoin, glycerin, vitamin A and E oils, mineral oil, propylene glycol, dimethyl isosorbide, polypropylene glycol, 2 myristyl propionate, and combinations thereof. 

 21. The method of claim 17, wherein the composition further comprises C) an activity enhancer selected from the group consisting of i) a hair growth stimulant, ii) a penetration enhancer, and combinations thereof. 

 22. The method of claim 21, wherein component i) is selected from the group vasodilator, an antiandrogen, a cyclosporin, a cyclosporin analog, an antimicrobial, an anti-inflammatory, a thyroid hormone, a thyroid hormone derivative, and a thyroid hormone analog, a non-selective prostaglandin agonist, a non-selective prostaglandin antagonist, a retinoid, a triterpene, and combinations thereof. 

 23. The method of claim 21, wherein component ii) is selected from the group consisting of 2-methyl propan-2-ol, propan-2-ol, ethyl-2-hydroxypropanoate, hexan-2,5-diol, polyoxyethylene(2) ethyl ether, di(2-hydroxypropyl) ether, pentan-2,4-diol, acetone, polyoxyethylene(2) methyl ether, 2-hydroxypropionic acid, 2-hydroxyoctanoic acid, propan-1-ol, 1,4-dioxane, tetrahydrofuran, butan-1,4-diol, propylene glycol dipelargonate, polyoxypropylene 15 stearyl ether, octyl alcohol, polyoxyethylene ester of oleyl alcohol, oleyl alcohol, lauryl alcohol, dioctyl adipate, dicapryl adipate, di-isopropyl adipate, di-isopropyl sebacate, dibutyl sebacate, diethyl sebacate, dimethyl sebacate, dioctyl sebacate, dibutyl suberate, dioctyl azelate, dibenzyl sebacate, dibutyl phthalate, dibutyl azelate, ethyl myristate, dimethyl azelate, butyl myristate, dibutyl succinate, didecyl phthalate, decyl oleate, ethyl caproate, ethyl salicylate, isopropyl palmitate, ethyl laurate, 2-ethyl-hexyl pelargonate, isopropyl isostearate, butyl laurate, benzyl benzoate, butyl benzoate, hexyl laurate, ethyl caprate, ethyl caprylate, butyl stearate, benzyl salicylate, 2-hydroxypropanoic acid, 2-hydroxyoctanoic acid, dimethyl sulphoxide, N,N-dimethyl acetamide, N,N-dimethyl formamide, 2-pyrrolidone, 1-methyl-2-pyrrolidone, 5-methyl-2-pyrrolidone, 1,5-dimethyl-2-pyrrolidone, 1-ethyl-2-pyrrolidone, phosphine oxides, sugar esters, tetrahydrofurfural alcohol, urea, diethyl-m-toluamide, 1-dodecylazacyloheptan-2-one, and combinations thereof. 

 24. The method of claim 17, wherein the composition is a topical composition locally administered on the skin once per day. 

 25. The method of claim 24, wherein the composition is administered once per day for 6 to 12 weeks. 

 26. The method of claim 17, wherein the composition is topically applied directly to the locus of desired hair growth. 

 27. The method of claim 17, wherein the prostaglandin F analog is selective for an FP receptor over an excitatory prostaglandin receptor in a ratio of at least 1:10. 

 28. The method of claim 17, wherein the prostaglandin F analog is selective for an FP receptor over an excitatory prostaglandin receptor in a ratio of at least 1:20. 

 29. The method of claim 17, wherein the prostaglandin F analog is selective for an FP receptor over an excitatory prostaglandin receptor in a ratio of at least 1:50.