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81. 发明申请

US20090252773A1 EMULSION COMPOSITION 有权
标题翻译：乳化组合物
公开(公告)号：US20090252773A1
公开(公告)日：2009-10-08
申请号：US12307166
申请日：2007-07-03
申请人： Tadashi Yoneda , Naoko Ito , Kazuo Furuya
发明人： Tadashi Yoneda , Naoko Ito , Kazuo Furuya
IPC分类号： A61K9/107 , A61K31/665
CPC分类号： A61K8/06 , A61K8/31 , A61K8/39 , A61K8/676 , A61Q19/00
摘要： An emulsion composition of the present invention includes (A) a salt of a higher fatty acid ester of ascorbic acid-2-phosphoric acid ester, (B) a polyglycerin fatty acid monoester including polyglycerin having a mean polymerization degree of 8 to 12 and an unsaturated fatty acid residual group of 14 to 22 carbon atoms, (C) a polyglycerin fatty acid monoester comprising polyglycerin having a mean polymerization degree of 2 to 6 and an unsaturated fatty acid residual group of 14 to 22 carbon atoms, and (D) a hydrocarbon oil, wherein the blending ratio by mass between the component (B) and the component (C) is in the range of 1:1 to 3:1, and the blending ratio by mass between the total of the components (B) and (C) and the component (D) is in the range of 10:1 to 1:4. By the use of the emulsion composition of the present invention, a skin external preparation can be provided which is prevented from decrease of a salt of a higher fatty acid ester of ascorbic acid-2-phosphoric acid ester attributable to decomposition of the salt, is excellent in retention of moisture, and has a beautiful appearance.
摘要翻译：本发明的乳液组合物包含（A）抗坏血酸-2-磷酸酯的高级脂肪酸酯的盐，（B）包含平均聚合度为8〜12的聚甘油的聚甘油脂肪酸单酯和 14个碳原子的不饱和脂肪酸残基，（C）包含平均聚合度为2〜6的聚甘油和14〜22个碳原子的不饱和脂肪酸残基的聚甘油脂肪酸单酯，（D）烃类油，其中组分（B）和组分（C）之间的混合重量比在1:1至3:1的范围内，并且组分（B）和（C）和成分（D）的比例在10:1至1:4的范围内。通过使用本发明的乳液组合物，可以提供防止由于盐分解引起的抗坏血酸-2-磷酸酯的高级脂肪酸酯的盐的降低的皮肤外用剂，是优良的保湿性，外观美观。

82. 发明申请

US20090227543A1 PHOSPHONATE COMPOUNDS HAVING IMMUNO-MODULATORY ACTIVITY 审中-公开
标题翻译：具有免疫调节活性的磷酸盐化合物
公开(公告)号：US20090227543A1
公开(公告)日：2009-09-10
申请号：US12166145
申请日：2008-07-01
申请人： Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Manoj Desai , Maria Fardis , Alan X. Huang , Thorsten Kirschberg , Christopher P. Lee , Richard L. Mackman , Peter H. Nelson , Hyung-Jung Pyun , Adrian S. Ray , William J. Watkins , Jennifer R. Zhang , Sundaramoorthi Swaminathan
发明人： Carina Cannizzaro , James M. Chen , Xiaowu Chen , Aesop Cho , Lee S. Chong , Manoj Desai , Maria Fardis , Alan X. Huang , Thorsten Kirschberg , Christopher P. Lee , Richard L. Mackman , Peter H. Nelson , Hyung-Jung Pyun , Adrian S. Ray , William J. Watkins , Jennifer R. Zhang , Sundaramoorthi Swaminathan
IPC分类号： A61K31/665 , C07F9/655
CPC分类号： A61K47/548 , A61K47/542
摘要： The invention is related to phosphonate substituted compounds having immuno-modulatory activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译：本发明涉及具有免疫调节活性的膦酸酯取代的化合物，含有这些化合物的组合物，以及包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。

83. 发明申请

US20090221530A1 Relaxase Modulators and Methods of Using Same 审中-公开
标题翻译：松弛调节剂及其使用方法
公开(公告)号：US20090221530A1
公开(公告)日：2009-09-03
申请号：US12084843
申请日：2006-11-08
申请人： Matthew R. Redinbo , Scott Lujan , Steven W. Matson
发明人： Matthew R. Redinbo , Scott Lujan , Steven W. Matson
IPC分类号： A61K31/665 , C12Q1/68
CPC分类号： C12Q1/533 , C07K2299/00 , C12N9/22
摘要： Methods of treating a microbial infection in a subject by administering to the subject an effective amount of a compound that modulates an enzymatic activity of a relaxase polypeptide is provided. Methods of inhibiting bacterial conjugation by modulating activity of a relaxase polypeptide in a bacterium are also provided. Novel compounds that modulate relaxase enzymes and assays for measuring kinetics of relaxase enzymes and selecting for modulators of relaxase enzyme activity are further provided.
摘要翻译：提供了通过向受试者施用有效量的调节松弛酶多肽的酶活性的化合物来治疗受试者的微生物感染的方法。还提供了通过调节细菌中松弛酶多肽的活性来抑制细菌共轭的方法。还提供了调节松弛酶的新型化合物和用于测量松弛酶的动力学和选择松弛酶酶活性调节剂的测定。

84. 发明申请

US20090005348A1 Compounds Having Cytokine Modulating Properties 审中-公开
标题翻译：具有细胞因子调节性质的化合物
公开(公告)号：US20090005348A1
公开(公告)日：2009-01-01
申请号：US12158932
申请日：2006-12-22
申请人： Esra Ogru , Roksan Libinaki , Robert Gianello
发明人： Esra Ogru , Roksan Libinaki , Robert Gianello
IPC分类号： A61K31/665 , A61P37/02
CPC分类号： A61K31/665 , Y02A50/422
摘要： A method of modulating one or more immuno-regulatory cytokines, such as pro-inflammatory and/or anti-inflammatory cytokines, comprising administering to a subject a therapeutically effective amount of one or more phosphate derivatives of one or more hydroxy chromans, or complexes thereof.
摘要翻译：调节一种或多种免疫调节细胞因子（例如促炎和/或抗炎细胞因子）的方法，包括向受试者施用治疗有效量的一种或多种一种或多种羟基色满酸的磷酸酯衍生物或其复合物。

85. 发明申请

US20080275005A1 MITOCHONDRIALLY TARGETED ANTIOXIDANTS 审中-公开
标题翻译：微量定向抗氧化剂
公开(公告)号：US20080275005A1
公开(公告)日：2008-11-06
申请号：US12109170
申请日：2008-04-24
申请人： Michael P. Murphy , Robin A.J. Smith
发明人： Michael P. Murphy , Robin A.J. Smith
IPC分类号： A61K31/665 , A61P35/00 , A61P3/10
CPC分类号： A61K31/35 , A61K31/66 , C07F9/5449 , C07F9/65522
摘要： The invention provides mitochondrially targeted antioxidant compounds. A compound of the invention comprises a lipophilic cation covalently coupled to an antioxidant moiety. In preferred embodiments, the lipophilic cation is the triphenyl phosphonium cation, and the compound is of the formula P(Ph3)+XR.Z- where X is a linking group, Z is an anion and R is an antioxidant moiety. Also provided are pharmaceutical compositions containing the mitochondrially targeted antioxidant compounds, and methods of therapy or prophylaxis of patients who would benefit from reduced oxidative stress, which comprise the step of administering the compounds of the invention.
摘要翻译：本发明提供线粒体靶向的抗氧化剂化合物。本发明的化合物包含与抗氧化剂部分共价偶联的亲脂性阳离子。在优选的实施方案中，亲脂性阳离子是三苯基鏻阳离子，化合物具有式P（Ph 3/3）+ XR.Z-，其中X是连接基团，Z是阴离子，R 是抗氧化剂部分。还提供了含有线粒体靶向抗氧化剂化合物的药物组合物，以及治疗或预防受益于减少氧化应激的患者的方法，其包括施用本发明化合物的步骤。

86. 发明申请

US20080221070A1 METHODS AND COMPOUNDS FOR THE TARGETED DELIVERY OF AGENTS TO BONE FOR INTERACTION THEREWITH 审中-公开
标题翻译：方法和化合物用于交付代理交付骨代谢
公开(公告)号：US20080221070A1
公开(公告)日：2008-09-11
申请号：US12043904
申请日：2008-03-06
申请人： William M. Pierce , K. Grant Taylor , Leonard C. Waite
发明人： William M. Pierce , K. Grant Taylor , Leonard C. Waite
IPC分类号： A61K31/665 , C07J41/00 , A61K31/661 , A61P19/10 , A61P19/08 , C07F9/08
CPC分类号： C07F9/65522 , C07F9/12 , C07J51/00
摘要： Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion. The Bone Active Portion is derived from an estrogenic agent. Compounds can also include a Blocking Group (RP) that reduces or eliminates the estrogenic activity of the Bone Active Portion.
摘要翻译：提供骨靶化合物和方法。化合物可以包括对骨具有亲和性的骨靶向部分（RTA）; 用于与骨骼相互作用并影响骨骼的骨活动部分（R A A A）; 连接骨骼目标部分和骨骼活动部分的连接部分（R L L L）。骨活性部分来自雌激素剂。化合物还可以包括减少或消除骨活性部分的雌激素活性的阻断组（R）。

87. 发明申请

US20080145450A1 Delivery or removal of metals from biological systems 有权
标题翻译：从生物系统中提取或清除金属
公开(公告)号：US20080145450A1
公开(公告)日：2008-06-19
申请号：US11639105
申请日：2006-12-14
申请人： David T. Hobbs , John C. Wataha , Jill Lewis , Regina L. W. Messer
发明人： David T. Hobbs , John C. Wataha , Jill Lewis , Regina L. W. Messer
IPC分类号： A61K33/24 , A61K47/02 , A61K31/665 , A61P1/00 , A61P11/00 , A61P19/00 , A61P35/00
CPC分类号： A61K31/665 , A61K33/24 , A61K47/6923
摘要： A process for delivering and/or removing metal from a biological system by loading a titanate sorbent with a biometal either before introduction into the system for delivery to a site within the system or after introduction into the system for delivery to a site where there is an excess accumulation of metal and thereafter the sorbent is loaded at the site with the excess metal and is removed from the system.
摘要翻译：一种用于通过在引入系统之前装载具有生物金属的钛酸盐吸附剂以递送到系统内的部位或者在引入到系统中以递送到具有金属的过量积累，此后吸附剂在该位置装载多余的金属，并从系统中取出。

88. 发明申请

US20080096844A1 Novel inhibitors of chymase 有权
标题翻译：糜酶的新型抑制剂
公开(公告)号：US20080096844A1
公开(公告)日：2008-04-24
申请号：US11975235
申请日：2007-10-18
申请人： Michael Greco , Michael Hawkins , Lawrence De Garavilla , Eugene Powell , Bruce Maryanoff
发明人： Michael Greco , Michael Hawkins , Lawrence De Garavilla , Eugene Powell , Bruce Maryanoff
IPC分类号： A61K31/665 , A61P11/00 , C07F9/02
CPC分类号： C07F9/65517
摘要： The present invention is directed to a compound of Formula (I): or an enantiomer, diastereomer, polymorph or pharmaceutically acceptable salt thereof and methods for preparing said compounds and compositions, intermediates and derivatives thereof, and methods for treating inflammatory or serine protease mediated disorders.
摘要翻译：本发明涉及式（I）的化合物或其对映体，非对映异构体，多晶型物或其药学上可接受的盐以及制备所述化合物及其组合物，中间体及其衍生物的方法，以及用于治疗炎性或丝氨酸蛋白酶介导的病症的方法。

89. 发明申请

US20080095866A1 Topical Compositions Containing Phosphorylated Polyphenols 审中-公开
标题翻译：含有磷酸化多酚的局部组合物
公开(公告)号：US20080095866A1
公开(公告)日：2008-04-24
申请号：US11574252
申请日：2004-09-14
申请人： Lieve Declercq , Hugo Corstjens , Daniel Maes , Willy Van Brussel , Geert Schelkens
发明人： Lieve Declercq , Hugo Corstjens , Daniel Maes , Willy Van Brussel , Geert Schelkens
IPC分类号： A61K31/665 , A61K31/661 , A61K36/61 , A61K36/752 , A61K36/87 , A61P17/00
CPC分类号： A61K36/00 , A61K31/66 , A61K36/87 , A61K2300/00
摘要： The present invention provides topical compositions containing phosphorylated polyphenols in combination with a topically acceptable carrier. The compositions of the invention provide a means for delayed delivery of the polyphenol to keratinous tissues, such as skin, hair and nails, with enzymes of the keratinous tissue dephosphorylating the polyphenol, and returning it to its native active form. The compositions are particularly useful in the regulation of skin conditions.
摘要翻译：本发明提供含有磷酸化多酚与局部可接受的载体组合的局部组合物。本发明的组合物提供了将多酚延迟递送到角质组织如皮肤，毛发和指甲的手段，其中角质组织的酶使多酚脱磷化并将其返回到其天然活性形式。组合物特别可用于调节皮肤状况。

90. 发明申请

US20070155704A1 Ketone compounds and compositions for cholesterol management and related uses 有权
公开(公告)号：US20070155704A1
公开(公告)日：2007-07-05
申请号：US10596047
申请日：2003-12-24
申请人： Jean-Louis Dasseux , Daniela Oniciu
发明人： Jean-Louis Dasseux , Daniela Oniciu
IPC分类号： A61K31/665 , A61K31/4743 , A61K31/4166 , A61K31/4178 , A61K31/42 , A61K31/366
CPC分类号： C07C59/353 , C07C49/17 , C07C49/185 , C07C49/215 , C07C49/245 , C07C49/258 , C07C49/507 , C07C49/723 , C07C49/743 , C07C49/747 , C07C49/784 , C07C49/82 , C07C49/86 , C07C50/30 , C07C59/347 , C07C59/82 , C07C59/84 , C07C59/90 , C07C69/716 , C07C69/738 , C07C235/74 , C07C261/04 , C07C309/07 , C07C309/24 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07D233/72 , C07D233/84 , C07D233/86 , C07D257/04 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/12 , C07D309/30 , C07D309/40 , C07F9/093 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

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