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公开(公告)号：US20190015448A1
公开(公告)日：2019-01-17
申请号：US15908365
申请日：2018-02-28
IPC分类号： A61K33/06 , A61K45/06 , A61K31/352 , A61K31/12 , A61K31/05 , A61K31/351 , A61K31/7048 , A61K31/381 , A61P19/02 , A61P19/10
摘要： The invention encompasses compositions and methods for effectively treating and/or preventing osteoporosis and related disorders such as osteoarthritis and rheumatoid arthritis, and for promoting overall bone and joint health. This is accomplished by totally addressing the multiple mechanisms that lead to such disorders. The invention includes compositions comprising a combination of agents that effectively suppress, regulate or interfere with the various biochemical processes and mechanisms that increase the risk for development of osteoporosis. The present compositions and methods simultaneously promote bone formation and reduce bone resorption by (a) stimulating osteoblast formation and osteogenesis; (b) suppressing adipocyte differentiation; (c) inhibiting osteoclast formation; and (d) increasing apoptosis of osteoclasts. The inventive compositions used for administration to human and other mammalian subjects having or at risk for development of osteoporosis comprise (1) at least one agent capable of modulating expression and/or activity of one or more of peroxisome activated protein receptor gamma (PPAR-γ), CAAT/enhancer binding protein-α (C/EBPα) and Sterol Regulatory Element-Binding Protein (SREBP-1); (2) at least one agent that activates expression and/or activity of one or more of the osteogenic transcription factors (Runx2/Cbfα1, Dlx5, Osterix, Msx2); (3) at least one agent that activates expression and/or activity of one or more of bone morphogenetic proteins (BMPs: BMP 2 and 4), alkaline phosphatase (ALP), and osteocalcin; (4) at least one agent capable of activating Wnt/β-catenin signaling pathway; (5) at least one agent that inhibits the activity of pro-oxidants including reactive nitrogen species and reactive oxygen species (ROS); (6) at least one agent that suppresses one or more of inflammatory mediators including interleukins IL-1α, IL-1β, IL-6, NF-κB, TNF-α, matrix metalloproteinases (MMPs) and prostaglandin E2 (PGE2); and (7) at least one agent that induces the expression of and/or activates one or more of adenosine monophosphate-activated protein kinase (AMPK), sirtuin (SIRT1) and adiponectin (AP).
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公开(公告)号：US20190015384A1
公开(公告)日：2019-01-17
申请号：US16050069
申请日：2018-07-31
IPC分类号： A61K31/353 , A61K31/12 , A61K31/05 , A61K31/047 , A61K31/7048 , A61K47/22 , A61K47/12 , A61K9/00 , A61P19/02
摘要： The invention encompasses compositions and methods for effectively treating and/or preventing the development and/or progression of osteoarthritis and rheumatoid arthritis and for promoting overall joint health. This is accomplished by totally addressing the key multiple biochemical processes and mechanisms that lead to such disorders. The invention includes compositions comprising a combination of natural agents that safely and effectively suppress, regulate or interfere with the various biochemical processes and mechanisms that increase the risk for or lead to the development and/or progression of OA and RA. The present compositions are holistically formulated to be effective in preventing/arresting loss of and/or damage to the articular cartilage (AC) by suppressing (a) extracellular matrix (ECM) degradation, (b) chondrocyte apoptosis, and (c) inflammation of synovium through modulation of mechanisms that involve transcription factors, growth factors, kinases, antiapoptotic/apoptotic factors and deacetylases. The active agents used herein are natural materials, in particular phytonutrients (or phytochemicals), minerals and/or vitamins.
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公开(公告)号：US20190261668A1
公开(公告)日：2019-08-29
申请号：US16410335
申请日：2019-05-13
IPC分类号： A23L33/105 , A23L33/155
摘要： The invention encompasses compositions and methods for effectively treating and/or preventing the development and/or progression of osteoporosis and related disorders such as osteoarthritis and rheumatoid arthritis, and for promoting overall bone and joint health. This is accomplished by addressing multiple key mechanisms that lead to such disorders. The invention includes compositions comprising a combination of agents having biological activities that effectively suppress, regulate or interfere with the various key biochemical processes and mechanisms that increase the risk for development and/or progression of osteoporosis. The present compositions and methods simultaneously promote bone formation and reduce bone resorption by (a) stimulating osteoblast formation and osteogenesis; (b) suppressing adipocyte differentiation; (c) inhibiting osteoclast formation; and (d) increasing apoptosis of osteoclasts. The inventive compositions used for administration to human and other mammalian subjects having or at risk for development of osteoporosis comprise (1) at least one agent capable of modulating expression and/or activity of one or more of peroxisome activated protein receptor gamma (PPAR-γ), CAAT/enhancer binding protein-α (C/EBPα) and Sterol Regulatory Element-Binding Protein (SREBP-1); (2) at least one agent that activates expression and/or activity of one or more of the osteogenic transcription factors (Runx2/Cbfα1, Dlx5, Osterix, Msx2); (3) at least one agent that activates expression and/or activity of one or more of bone morphogenetic proteins (BMPs: BMP 2 and 4), alkaline phosphatase (ALP), and osteocalcin; (4) at least one agent capable of activating Wnt/β-catenin signaling pathway; (5) at least one agent that inhibits the activity of pro-oxidants including reactive nitrogen species and reactive oxygen species (ROS); (6) at least one agent that suppresses one or more of inflammatory mediators including interleukins IL-1α, IL-1β, IL-6, NF-κB, TNF-α, matrix metalloproteinases (MMPs) and prostaglandin E2 (PGE2); and (7) at least one agent that induces the expression of and/or activates one or more of adenosine monophosphate-activated protein kinase (AMPK), sirtuin (SIRT1) and adiponectin (AP).
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公开(公告)号：US5891425A
公开(公告)日：1999-04-06
申请号：US23823
申请日：1998-02-13
申请人： Eric John Bretzler, deceased , Christine Marie Putman , Ghebre Egziabher Tzeghai , David Frederick Swaile
发明人： Eric John Bretzler, deceased , Christine Marie Putman , Ghebre Egziabher Tzeghai , David Frederick Swaile
IPC分类号： A61K8/02 , A61K8/34 , A61K8/37 , A61K8/42 , A61K8/58 , A61Q5/10 , A61Q15/00 , A61K7/32 , A61K7/00
摘要： Disclosed are anhydrous antiperspirant cream compositions that are substantially free of polymeric or inorganic thickening, and have improved product stability and spreading performance. These compositions have a rheology profile characterized by select product hardness (from about 75 gram force to about 500 gram force), delta stress (from about 300 dyne/cm.sup.2 to about 8,000 dyne/cm.sup.2) and static yield stress (at least about 1,000 dyne/cm.sup.2) values. The new rheology profile is preferably applied to antiperspirant cream compositions comprising from about 0.1% to about 20% by weight of a crystalline gellant, from about 10% to about 80% by weight of an anhydrous liquid carrier for the crystalline gellant having a solubility parameter of from about 3 to about 13 and, from about 5% to about 35% by weight of a particulate antiperspirant active. Also disclosed are methods of using and making the compositions, and packaged compositions having a shear force delivery means for applying the composition to the axlla or other area of the skin. The disclosed compositions are especially effective at minimizing or eliminating solvent syneresis during packaging, storage, transport or during extrusion through a perforated mesh cap or other shear force delivery means.
摘要翻译： 公开了基本上不含聚合物或无机增稠的无水止汗剂组合物，并具有改进的产品稳定性和扩散性能。 这些组合物具有以选择的产品硬度（约75克力至约500克力），δ应力（约300达因/厘米2至约8,000达因/平方厘米）和静态屈服应力（至少约1,000达因 / cm2）值。 新的流变学特征优选地应用于止汗剂组合物，其包含约0.1％至约20％重量的结晶胶凝剂，约10％至约80％重量的用于具有溶解度参数的结晶胶凝剂的无水液体载体 约3至约13，和约5重量％至约35重量％的颗粒止汗剂活性物质。 还公开了使用和制备组合物和包装组合物的方法，所述组合物具有剪切力递送装置，用于将组合物施用于轴突或皮肤的其它区域。 所公开的组合物在包装，储存，运输期间或通过穿孔网罩或其它剪切力递送装置的挤出期间最小化或消除溶剂脱水特别有效。
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5.发明授权Antiperspirant gel-solid stick compositions containing select nucleating agents 失效含有选择成核剂的止汗凝胶固体棒组合物
公开(公告)号：US5849276A
公开(公告)日：1998-12-15
申请号：US770392
申请日：1996-12-20
IPC分类号： A61K8/00 , A61K8/34 , A61K8/36 , A61K8/365 , A61K8/37 , A61K8/39 , A61K8/42 , A61K8/44 , A61K8/58 , A61K8/60 , A61K8/73 , A61K8/86 , A61K8/89 , A61K8/891 , A61K8/894 , A61K8/98 , A61Q15/00 , C08L83/04 , A61K7/32 , A61K7/34 , A61K7/36 , A61K7/38
CPC分类号： A61Q15/00 , A61K8/0229 , A61K8/042 , A61K8/342 , A61K8/365 , A61K8/39 , A61K8/42 , A61K8/44 , A61K8/585 , A61K8/60 , A61K8/86 , A61K8/891 , A61K8/894
摘要： Disclosed are anhydrous antiperspirant compositions comprising from about 0.5% to about 60% by weight of particulate antiperspirant active; from about 1% to about 15% by weight of a solid non-polymeric gellant; from about 10% to about 80% by weight of an anhydrous liquid carrier having an average solubility parameter of from about 3 to about 13 (cal/cm.sup.3).sup.0.5 ; and from about 0.0001% to about 5.0% by weight of a solid nucleating agent wherein the molar ratio of the solid non-polymeric gellant to the nucleating agent is from about 10:1 to about 1000:1. These antiperspirant compositions provide improved low residue performance and improved antiperspirant efficacy.
摘要翻译： 公开了无水止汗组合物，其包含约0.5重量％至约60重量％的颗粒止汗剂活性物质; 约1重量％至约15重量％的固体非聚合胶凝剂; 约10重量％至约80重量％的平均溶解度参数为约3至约13（cal / cm 3）0.5的无水液体载体; 和约0.0001重量％至约5.0重量％的固体成核剂，其中固体非聚合物胶凝剂与成核剂的摩尔比为约10:1至约1000:1。 这些止汗组合物提供改善的低残留性能和改善的止汗效力。
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公开(公告)号：US5902570A
公开(公告)日：1999-05-11
申请号：US23584
申请日：1998-02-13
申请人： Eric John Bretzler, deceased , Christine Marie Putman , Ghebre Egziabher Tzeghai , David Frederick Swaile
发明人： Eric John Bretzler, deceased , Christine Marie Putman , Ghebre Egziabher Tzeghai , David Frederick Swaile
IPC分类号： A61K8/02 , A61K8/34 , A61K8/37 , A61K8/42 , A61K8/58 , A61Q5/10 , A61Q15/00 , A61K7/32 , A61K7/00
摘要： Disclosed are anhydrous antiperspirant cream compositions that are substantially free of polymeric or inorganic thickening, and have improved product stability and spreading performance. These compositions have a rheology profile characterized by select product hardness (from about 75 gram force to about 500 gram force), delta stress (from about 300 dyne/cm.sup.2 to about 8,000 dyne/cm.sup.2) and static yield stress (at least about 1,000 dyne/cm.sup.2 ) values. The new rheology profile is preferably applied to antiperspirant cream compositions comprising from about 0.1% to about 20 % by weight of a crystalline gellant, from about 10% to about 80% by weight of an anhydrous liquid carrier for the crystalline gellant having a solubility parameter of from about 3 to about 13 and, from about 5 % to about 35% by weight of a particulate antiperspirant active. Also disclosed are methods of using and making the compositions, and packaged compositions having a shear force delivery means for applying the composition to the axilla or other area of the skin. The disclosed compositions are especially effective at minimizing or eliminating solvent syneresis during packaging, storage, transport or during extrusion through a perforated mesh cap or other shear force delivery means.
摘要翻译： 公开了基本上不含聚合物或无机增稠的无水止汗剂组合物，并具有改进的产品稳定性和扩散性能。 这些组合物具有以选择的产品硬度（约75克力至约500克力），δ应力（约300达因/厘米2至约8,000达因/平方厘米）和静态屈服应力（至少约1,000达因 / cm2）值。 新的流变学特征优选地应用于止汗剂组合物，其包含约0.1％至约20％重量的结晶胶凝剂，约10％至约80％重量的用于具有溶解度参数的结晶胶凝剂的无水液体载体 约3至约13，和约5重量％至约35重量％的颗粒止汗剂活性物质。 还公开了使用和制备组合物和包装组合物的方法，所述组合物具有用于将组合物施用于腋窝或皮肤的其它区域的剪切力递送装置。 所公开的组合物在包装，储存，运输期间或通过穿孔网罩或其它剪切力递送装置的挤出期间最小化或消除溶剂脱水特别有效。
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公开(公告)号：US5871717A
公开(公告)日：1999-02-16
申请号：US738631
申请日：1996-10-29
申请人： Eric John Bretzler, deceased , Christine Marie Putman , Ghebre Egziabher Tzeghai , David Frederick Swaile
发明人： Eric John Bretzler, deceased , Christine Marie Putman , Ghebre Egziabher Tzeghai , David Frederick Swaile
IPC分类号： A61K8/00 , A61K8/02 , A61K8/34 , A61K8/37 , A61K8/42 , A61K8/58 , A61K8/89 , A61K8/891 , A61K8/97 , A61Q5/10 , A61Q15/00 , A61K7/32 , A61K7/00
摘要： Disclosed are anhydrous antiperspirant cream compositions that are substantially free of polymeric or inorganic thickening, and have improved product stability and spreading performance. These compositions have a rheology profile characterized by select product hardness (from about 75 gram force to about 500 gram force), delta stress (from about 300 dyne/cm.sup.2 to 8,000 dyne/cm.sup.2) and static yield stress (at least about 1,000 dyne/cm.sup.2) values. The new rheology profile is preferably applied to antiperspirant cream compositions comprising from about 0.1% to about 20% by weight of a crystalline gellant, from about 10% to about 80% by weight of an anhydrous liquid carrier for the crystalline gellant having a solubility parameter of from about 3 to about 13 and, from about 5% to about 35% by weight of a particulate antiperspirant active. Also disclosed are methods of using and making the compositions, and packaged compositions having a shear force delivery means for applying the composition to the axilla or other area of the skin. The disclosed compositions are especially effective at minimizing or eliminating solvent syneresis during packaging, storage, transport or during extrusion through a perforated mesh cap or other shear force delivery means.
摘要翻译： 公开了基本上不含聚合物或无机增稠的无水止汗剂组合物，并具有改进的产品稳定性和扩散性能。 这些组合物具有以选择的产品硬度（约75克力至约500克力），δ应力（约300达因/厘米2至8,000达因/厘米2）和静态屈服应力（至少约1,000达因/ cm2）值。 新的流变学特征优选地应用于止汗剂组合物，其包含约0.1％至约20％重量的结晶胶凝剂，约10％至约80％重量的用于具有溶解度参数的结晶胶凝剂的无水液体载体 约3至约13，和约5重量％至约35重量％的颗粒止汗剂活性物质。 还公开了使用和制备组合物和包装组合物的方法，所述组合物具有用于将组合物施用于腋窝或皮肤的其它区域的剪切力递送装置。 所公开的组合物在包装，储存，运输期间或通过穿孔网罩或其它剪切力递送装置的挤出期间最小化或消除溶剂脱水特别有效。
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公开(公告)号：US5891424A
公开(公告)日：1999-04-06
申请号：US23777
申请日：1998-02-13
申请人： Eric John Bretzler, deceased , Christine Marie Putman , Ghebre Egziabher Tzeghai , David Frederick Swaile
发明人： Eric John Bretzler, deceased , Christine Marie Putman , Ghebre Egziabher Tzeghai , David Frederick Swaile
IPC分类号： A61K8/02 , A61K8/34 , A61K8/37 , A61K8/42 , A61K8/58 , A61Q5/10 , A61Q15/00 , A61K7/32 , A61K7/00
摘要： Disclosed are anhydrous antiperspirant cream compositions that are substantially free of polymeric or inorganic thickening, and have improved product stability and spreading performance. These compositions have a rheology profile characterized by select product hardness (from about 75 gram force to about 500 gram force), delta stress (from about 300 dyne/cm.sup.2 to about 8,000 dyne/cm.sup.2) and static yield stress (at least about 1,000 dyne/cm.sup.2) values. The new rheology profile is preferably applied to antiperspirant cream compositions comprising from about 0.1% to about 20% by weight of a crystalline gellant, from about 10% to about 80% by weight of an anhydrous liquid carrier for the crystalline gellant having a solubility parameter of from about 3 to about 13 and, from about 5% to about 35% by weight of a particulate antiperspirant active. Also disclosed are methods of using and making the compositions, and packaged compositions having a shear force delivery means for applying the composition to the axilla or other area of the skin. The disclosed compositions are especially effective at minimizing or eliminating solvent syneresis during packaging, storage, transport or during extrusion through a perforated mesh cap or other shear force delivery means.
摘要翻译： 公开了基本上不含聚合物或无机增稠的无水止汗剂组合物，并具有改进的产品稳定性和扩散性能。 这些组合物具有以选择的产品硬度（约75克力至约500克力），δ应力（约300达因/厘米2至约8,000达因/平方厘米）和静态屈服应力（至少约1,000达因 / cm2）值。 新的流变学特征优选地应用于止汗剂组合物，其包含约0.1％至约20％重量的结晶胶凝剂，约10％至约80％重量的用于具有溶解度参数的结晶胶凝剂的无水液体载体 约3至约13，和约5重量％至约35重量％的颗粒止汗剂活性物质。 还公开了使用和制备组合物和包装组合物的方法，所述组合物具有用于将组合物施用于腋窝或皮肤的其它区域的剪切力递送装置。 所公开的组合物在包装，储存，运输期间或通过穿孔网罩或其它剪切力递送装置的挤出期间最小化或消除溶剂脱水特别有效。
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