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21. 发明授权

US07851650B2 Compounds for treating inflammation and pain 有权
标题翻译：用于治疗炎症和疼痛的化合物
公开(公告)号：US07851650B2
公开(公告)日：2010-12-14
申请号：US12725212
申请日：2010-03-16
申请人： Joseph P. St. Laurent
发明人： Joseph P. St. Laurent
IPC分类号： C07C315/00 , A01N37/12
CPC分类号： A61K9/06 , A61K9/0014 , C07C317/48
摘要： The present invention is directed to a compound of 2-N halo-4-methylsulfonyl-butyric acid, such as 2-N chloro-4-methylsulfonyl-butyric acid, or a pharmaceutically acceptable salt or solvate thereof. The present invention is also directed to a pharmaceutical composition comprises the compound and a pharmaceutically acceptable carrier. The present invention is further directed to a method for treating inflammation or inflammatory-related disorders, bacterial infection, pain, or skin conditions, by administering 2-N halo-4-methylsulfonyl-butyric acid to a subject in need thereof.
摘要翻译：本发明涉及2-N卤代-4-甲基磺酰基 - 丁酸如2-N氯-4-甲基磺酰基 - 丁酸或其药学上可接受的盐或溶剂化物的化合物。本发明还涉及包含该化合物和药学上可接受的载体的药物组合物。本发明还涉及通过向有需要的受试者施用2-N卤代-4-甲基磺酰基 - 丁酸来治疗炎症或炎性相关疾病，细菌感染，疼痛或皮肤病症的方法。

22. 发明授权

US07834209B2 Hydrofluoroalkanesulfonic acids from fluorovinyl ethers 有权
标题翻译：来自氟乙烯基醚的氢氟烷基磺酸
公开(公告)号：US07834209B2
公开(公告)日：2010-11-16
申请号：US11447825
申请日：2006-06-06
申请人： Christopher P. Junk , Mark Andrew Harmer , Andrew Edward Feiring , Frank Leonard Schadt, III , Zoe Schnepp
发明人： Christopher P. Junk , Mark Andrew Harmer , Andrew Edward Feiring , Frank Leonard Schadt, III , Zoe Schnepp
IPC分类号： C07C309/02 , C07C315/00
CPC分类号： G03F7/0045 , C07C303/32 , C07C309/10 , C07C381/12 , G03F7/0046 , G03F7/0392 , G03F7/0397
摘要： Hydrofluoroalkanesulfonates of the general formula R—O—CXH—CX2—SO3M, where R is selected from the group consisting of alkyl groups, functionalized alkyl groups, and alkenyl groups; X is selected from the group consisting of hydrogen and fluorine with the proviso that at least one X is fluorine; and M is a cation, are made by reacting fluorovinyl ether with aqueous sulfite solution. Organic onium hydrofluoroalkanesulfonates are useful as ionic liquids and photoacid generators.
摘要翻译：通式为R-O-CXH-CX2-SO3M的氢氟烷基磺酸盐，其中R选自烷基，官能化烷基和链烯基; X选自氢和氟，条件是至少一个X是氟; 并且M是阳离子，通过使氟乙烯基醚与亚硫酸盐水溶液反应而制成。有机鎓氢氟烷基磺酸盐可用作离子液体和光酸产生剂。

23. 发明授权

US07777084B2 Cyclopropanation process 有权
标题翻译：环丙烷化方法
公开(公告)号：US07777084B2
公开(公告)日：2010-08-17
申请号：US11722121
申请日：2005-12-20
申请人： Fridtjof Schröder
发明人： Fridtjof Schröder
IPC分类号： C07C43/02 , C07C27/10 , C07C315/00 , C07D313/00
CPC分类号： C07C29/36 , C07C2/861 , C07C29/32 , C07C41/16 , C07C41/30 , C07C67/347 , C07C253/30 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07C2602/18 , C07D313/00 , C07C13/32 , C07C69/608 , C07C255/31 , C07C43/23 , C07C43/115 , C07C43/162 , C07C31/137 , C07C33/05 , C07C33/12 , C07C31/1333
摘要： A process for the cyclopropanation of a substituted alkene, comprising the reaction of the alkene with a carbenoide, generated from dibromomethane and a tri-(C2-C8)-alkyl aluminium compound, in the presence of a catalytic amount of a metal compound selected from the group consisting of Lewis acids, metallocenes and metal carbonyl complexes. The process advantageously uses transition metal compounds as catalysts and the dibromomethane can be recovered.The process is especially useful for the preparation of ingredients for the flavour and fragrance industry.
摘要翻译：在催化量的金属化合物存在下，由二溴甲烷和三（C 2 -C 8） - 烷基铝化合物产生的包含烯烃与碳氰酸酯的反应的取代烯烃的环丙烷化方法，由路易斯酸，金属茂和金属羰基络合物组成的组。该方法有利地使用过渡金属化合物作为催化剂，并且可以回收二溴甲烷。该方法对于制备风味和香料工业的成分特别有用。

24. 发明申请

US20100174104A1 COBALT-CATALYZED ASYMMETRIC CYCLOPROPANATION WITH DIAZOSULFONES 审中-公开
标题翻译：钴催化不对称环加成双歧杆菌
公开(公告)号：US20100174104A1
公开(公告)日：2010-07-08
申请号：US12404435
申请日：2009-03-16
申请人： X. Peter Zhang , Shifa Zhu
发明人： X. Peter Zhang , Shifa Zhu
IPC分类号： C07C255/46 , C07C315/00 , C07C201/06
CPC分类号： C07C315/04 , B01J31/1815 , B01J2231/325 , B01J2531/025 , B01J2531/845 , C07B2200/07 , C07C2601/02 , C07C317/12 , C07C317/14 , C07C317/20 , C07C317/24 , C07C317/44
摘要： Asymmetric cyclopropanation of olefins with diazosulfones.
摘要翻译：烯烃与重氮砜的不对称环丙烷化反应。

25. 发明申请

US20100105953A1 Human Adam-10 Inhibitors 有权
标题翻译：人类Adam-10抑制剂
公开(公告)号：US20100105953A1
公开(公告)日：2010-04-29
申请号：US12605118
申请日：2009-10-23
申请人： Lynne Canne Bannen , Erick W. Co , Vasu Jammalamadaka , John M. Nuss , Moon Hwan Kim , Donna Tra Le , Amy Lew , Morrison B. Mac , Shumeye Mamo , Zhaoyang Wen , Wei Xu , Richard George Khoury
发明人： Lynne Canne Bannen , Erick W. Co , Vasu Jammalamadaka , John M. Nuss , Moon Hwan Kim , Donna Tra Le , Amy Lew , Morrison B. Mac , Shumeye Mamo , Zhaoyang Wen , Wei Xu , Richard George Khoury
IPC分类号： C07C315/00
CPC分类号： C07D241/04 , C07C309/87 , C07D213/70 , C07D401/06 , C07D401/12 , C07D403/06 , C07D413/06
摘要： The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.
摘要翻译：本发明提供了用于抑制ADAM-10蛋白质的化合物，具有选择性对MMP-1。这些化合物可用于体外研究ADAM-10（及其抑制）在生物过程中的作用。本发明还包括药物组合物，其包含一种或多种本发明的ADAM-10抑制剂与药学上可接受的载体的组合。这样的组合物可用于治疗癌症，关节炎和与血管发生相关的疾病。相应地，本发明还包括治疗癌症，关节炎和与血管生成有关的疾病形式的方法，其中ADAM-10起关键作用。

26. 发明申请

US20100081208A1 Multirange indicator 审中-公开
标题翻译：多重指示器
公开(公告)号：US20100081208A1
公开(公告)日：2010-04-01
申请号：US12565961
申请日：2009-09-24
申请人： Klaus KEITE-TELGENBÜSCHER , Hermann NEUHAUS-STEINMETZ
发明人： Klaus KEITE-TELGENBÜSCHER , Hermann NEUHAUS-STEINMETZ
IPC分类号： G01N21/78 , C07C381/04 , C07C45/00 , C07C315/00 , C07C255/46
CPC分类号： G01T1/04 , G01J1/50 , G01N31/22 , G03C1/685 , G03C1/73 , G03F7/105
摘要： A multirange indicator is proposed which permits quantitative dose determination of high-energy actinic radiation, where the dose for different wavelength ranges can be respectively determined in parallel. To this end, the multirange indicator has two indicator systems designed with mutually corresponding properties, thus eliminating any mutual distortion of the results of the dose measurements. The first indicator system is based on a photolatent Lewis acid or photolatent Lewis base, and the second indicator system is based on a polysubstituted triphenylmethane dye. Both the multirange indicator and its use for the production of various dose-measurement devices are described. Finally, the following are proposed for the measurement of UV radiation and/or electron-beam radiation: as dose-measurement device, a dose-measurement coating material and a flat dose-measurement element, these being based on the above multirange indicator, and also the measurement method that can be implemented with the said dose-measurement devices.
摘要翻译：提出了一种多范围指示器，其允许高能量光化辐射的定量剂量测定，其中可以分别平行地确定不同波长范围的剂量。为此，多范围指示器具有两个指定系统，其设计具有相互对应的属性，从而消除了剂量测量结果的任何相互扭曲。第一指示剂系统基于光致路易斯酸或光照路易斯碱，第二指示剂体系基于多取代的三苯基甲烷染料。描述了多范围指示器及其用于生产各种剂量测量装置的用途。最后，提出了用于测量UV辐射和/或电子束辐射的以下内容：作为剂量测量装置，剂量测量涂层材料和平坦剂量测量元件，它们基于上述多范围指示器，以及也可以使用所述剂量测量装置实现的测量方法。

27. 发明申请

US20100048939A1 PROCESS FOR THE ADDITION OF THIOLATES TO ?,?-UNSATURATED CARBONYL OR SULFONYL COMPOUNDS 有权
标题翻译：将硫酸添加到α-，β-不饱和碳或亚磺酸化合物的方法
公开(公告)号：US20100048939A1
公开(公告)日：2010-02-25
申请号：US12537274
申请日：2009-08-07
申请人： James R. McConnell , Douglas C. Bland
发明人： James R. McConnell , Douglas C. Bland
IPC分类号： C07C321/14 , C07C315/00 , C07C45/61
CPC分类号： C07C319/18 , C07C2601/08 , C07C2601/14 , C07C323/22 , C07C323/56 , C07C323/65
摘要： Alkylthio substituted aldehydes, ketones, esters and sulfones are prepared by reacting α,β-unsaturated carbonyl and sulfonyl compounds with a sodium or potassium thiolate in the presence of a alkane carboxylic acid and water.
摘要翻译：在烷烃羧酸和水存在下，通过使α，b' - 不饱和羰基和磺酰基化合物与硫醇钠或钾溶液反应来制备烷硫基取代的醛，酮，酯和砜。

28. 发明授权

US07638556B2 Freeze-dried product of N-[o-(p-pivaloyloxy benzenesulfonylamino)benzoyl]glycine monosodium salt tetra-hydrate and a process for the manufacture thereof 失效
标题翻译： N- [对 - （对新戊酰氧基苯磺酰基氨基）苯甲酰基]甘氨酸一钠盐四水合物的冷冻干燥产物及其制备方法
公开(公告)号：US07638556B2
公开(公告)日：2009-12-29
申请号：US11740756
申请日：2007-04-26
申请人： Akira Takada , Masao Sudo
发明人： Akira Takada , Masao Sudo
IPC分类号： C07C315/00 , A61K31/24 , A61K31/195
CPC分类号： A61K31/198 , A61K9/14 , A61K9/19
摘要： A method for the preparation of a freeze-dried product of N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetra-hydrate dissolved in a mixed solvent of water and ethanol, and the freeze-dried product obtained by the method. According to the present invention, N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetra-hydrate is dissolved in a small amount of a mixed solvent of water and ethanol, and therefore it is possible to manufacture high-dosage product by freeze-drying.
摘要翻译：一种溶解在水和乙醇的混合溶剂中的N- [对 - （对 - 三（新戊酰氧基苯磺酰基氨基）苯甲酰基]甘氨酸一钠盐四水合物的冷冻干燥产物的方法和通过该方法获得的冷冻干燥产物。根据本发明，将N- [O-（对新戊酰氧基苯磺酰基氨基）苯甲酰基]甘氨酸一钠盐四水合物溶解在少量的水和乙醇的混合溶剂中，因此可以制造高剂量产品通过冷冻干燥。

29. 发明申请

US20090221787A1 Production Of Monomer, Oligomer And Polymer Phosphonic Acid Esters And Phosphonic And Sulphonic Acids By A Nucleophile Aromatic Substitution 审中-公开
标题翻译：通过亲核取代芳基取代单体，低聚物和聚合物膦酸酯和膦酸和磺酸的生产
公开(公告)号：US20090221787A1
公开(公告)日：2009-09-03
申请号：US11995187
申请日：2006-07-10
申请人： Thomas Haring , Jochen Kerres , Martin Hein , Frank Schonberger
发明人： Thomas Haring , Jochen Kerres , Martin Hein , Frank Schonberger
IPC分类号： C08G75/00 , C07C315/00 , C07F9/02 , C08G73/24
CPC分类号： B01D71/52 , B01D71/66 , B01D71/68 , C07C303/02 , C07C317/22 , C07F9/3834 , C07F9/404 , C08F8/36 , C08F8/40 , H01M8/1025 , H01M8/1027 , H01M8/1032 , H01M8/1039 , H01M2300/0082 , Y02P70/56
摘要： The invention relates to producing monomer, oligomer and polymer non-fluorinated, partially fluorinated or perfluorinated sulphonic acids by reacting halogenated, low-molecular weight, oligomer or macromolecular arenes with (hydrogen) sulphites, dithionites, sulphides or other reducing sulfur salts, possibly by oxidising sulphur-containing arene intermediates which are formed at a sulphur oxidation degree less than +6 by means of appropriate oxidation agents with formation of corresponding sulphonate functional groups (sulphonic acid, sulfohalogenide, sulphonamide and sulphonic acid ester groups). The invention also relates to a method for producing monomer, oligomer or polymer non-halogenated, partially halogenated or perhalogenated phosphonic acid esters and the derivatives thereof (for example, a free phosphonic acid or a phosphonic acid salt) by a nucleophile aromatic substitution (Michaelis-Becker-reaktion, complete or partial substitution of halogenide functional groups by phosphate functional groups (phosphonic acid esters, phosphonic acid amides, phosphonic acids, phosphonic acid salts, phosphonic acid halogenides). Said invention also relates to a method for producing polymer or ionomer non-halogenated, partially halogenated or perhalogenated containing (CF2)xPO(OR)2— or (CF2)xSO2Me- or (CF2)xSO3Me- side chains, (wherein x=1-20, R=any organic radical, Me=any monovalent cation). A method for carrying out a nucleophile polycondensation of said functionalised (i.e. sulphonated, sulphonated or phosphonated) monomers into oligomers or polymers is also disclosed.
摘要翻译：本发明涉及通过卤代，低分子量，低聚物或大分子芳烃与（氢）亚硫酸盐，连二亚硫酸盐，硫化物或其它还原硫盐反应制备单体，低聚物和聚合物非氟化的，部分氟化的或全氟化的磺酸，可能通过通过形成相应的磺酸盐官能团（磺酸，磺基卤化物，磺酰胺和磺酸酯基团）的合适的氧化剂，氧化含硫芳烃中间体，它们以小于+6的硫氧化度形成。本发明还涉及通过亲核试剂芳香取代产生单体，低聚物或聚合物非卤代，部分卤化或全卤代膦酸酯及其衍生物（例如游离膦酸或膦酸盐）的方法（Michaelis - 磷酸酯官能团（膦酸酯，膦酸酰胺，膦酸，膦酸盐，膦酸卤化物）完全或部分取代卤化物官能团的方法本发明还涉及聚合物或离聚物的制备方法（CF 2）x SO 2 Me-或（CF 2）x SO 3 Me侧链，（其中x = 1-20，R =任何有机基团，Me =任何还公开了将所述官能化（即磺化，磺化或膦酸化）单体进行亲核物缩聚成低聚物或聚合物的方法。

30. 发明授权

US07569711B2 Enone cancer therapeutics 失效
标题翻译： Enone癌症治疗
公开(公告)号：US07569711B2
公开(公告)日：2009-08-04
申请号：US11006132
申请日：2004-12-07
申请人： Bruce Ganem , Donald J. Creighton , Diana S. Hamilton , Zhebo Ding
发明人： Bruce Ganem , Donald J. Creighton , Diana S. Hamilton , Zhebo Ding
IPC分类号： C07C59/147 , C07C59/185 , C07C315/00 , C07C317/00
CPC分类号： A61K31/56 , A61K38/00 , C07K5/0215
摘要： Described herein are new enone derivatives and conjugates. Additionally, methods for synthesizing these new enones are also disclosed. These compounds can be employed in cancer therapy.
摘要翻译：本文描述的是新的烯酮衍生物和共轭物。此外，还公开了合成这些新的烯酮的方法。这些化合物可用于癌症治疗。

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