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11. 发明授权

US08168826B2 Method of producing highly functionalized 1,3-diamino-propan-2-ols from solid support 有权
标题翻译：从固体支持物制备高度官能化的1,3-二氨基 - 丙-2-醇的方法
公开(公告)号：US08168826B2
公开(公告)日：2012-05-01
申请号：US12630042
申请日：2009-12-03
申请人： Steve J. Coats , Dennis J. Hlasta , Mark J. Schulz
发明人： Steve J. Coats , Dennis J. Hlasta , Mark J. Schulz
IPC分类号： C07C233/00 , C07D303/00 , C07D303/08 , C08F8/30
CPC分类号： C07C315/04 , C07B2200/11 , C07C233/37 , C07C233/40 , C07C233/62 , C07C233/78 , C07C235/50 , C07C235/84 , C07C237/20 , C07C237/22 , C07C237/34 , C07C271/20 , C07C303/40 , C07C319/20 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/50 , C07D213/38 , C07D215/54 , C07D295/13 , C07D307/22 , C07D333/20 , C40B40/04 , C40B50/14 , C07C317/44 , C07C323/60 , C07C311/37
摘要： The invention is directed to compounds and methods of synthesizing hydroxyethylamino amides and their use in treatment of aspartyl protease mediated diseases and conditions.
摘要翻译：本发明涉及合成羟乙基氨基酰胺的化合物和方法及其在治疗天冬氨酰蛋白酶介导的疾病和病症中的用途。

12. 发明授权

US07838695B2 Neuroactive substance and uses of one such substance 失效
标题翻译：神经活性物质和一种此类物质的用途
公开(公告)号：US07838695B2
公开(公告)日：2010-11-23
申请号：US10581226
申请日：2004-11-25
申请人： Karina-Ethel Petit , Jean-Francois Biard , Bruno Lapied , Francoise Grolleau , Alain Hamon
发明人： Karina-Ethel Petit , Jean-Francois Biard , Bruno Lapied , Francoise Grolleau , Alain Hamon
IPC分类号： C07D303/00 , A01N43/20
CPC分类号： A01N43/20 , A61K31/336 , C07D303/16
摘要： The invention relates to a neuroactive substance which is characterised in that it has formula (O), wherein R1, R2, R3 and R4 are identical or different and are methyl or ethyl radicals. Preferably, the neuroactive substance comprises 6S-acetyl-4R,5R-dimethyl-1R(10S)-epoxy-2R-hy-droxy-7R-acetoxydecahydro naphthalene which can be isolated from Rhytisma fulvum cnidaria. The inventive neuroactive substance can be used as a pharmacological reagent in research work and is also suitable for use in the fields of industry (insecticides) and health.
摘要翻译：本发明涉及神经活性物质，其特征在于其具有式（O），其中R 1，R 2，R 3和R 4相同或不同，为甲基或乙基。优选地，神经活性物质包含可从Rh be中分离的6S-乙酰基-4R，5R-二甲基-1R（10S） - 环氧-2R-羟基-7R-乙酰氧基十氢萘。本发明的神经活性物质可用作研究工作中的药物试剂，并且也适用于工业（杀虫剂）和健康领域。

13. 发明申请

US20100041905A1 Process for the Preparation of Substituted 2-Acetylamino-Alkoxyphenyl 审中-公开
标题翻译：制备取代的2-乙酰氨基 - 烷氧基苯基的方法
公开(公告)号：US20100041905A1
公开(公告)日：2010-02-18
申请号：US12374230
申请日：2007-07-17
申请人： Debra Ainge , Philip Cornwall , Duncan Michael Gill , Luis Manuel Vaz
发明人： Debra Ainge , Philip Cornwall , Duncan Michael Gill , Luis Manuel Vaz
IPC分类号： C07D303/00 , C07C233/00 , C07C43/00
CPC分类号： C07C205/37 , C07B2200/07 , C07C201/08 , C07C201/12 , C07C213/02 , C07C217/84 , C07C231/02 , C07C231/18 , C07C233/25 , C07D303/22 , C07C205/26
摘要： The present invention relates to a novel process for the preparation of compounds of formula (V) wherein X, Q, R1, R1a and R2 are as defined in the specification, the compounds being useful in the preparation of therapeutic agents.
摘要翻译：本发明涉及制备式（V）化合物的新方法，其中X，Q，R 1，R 1a和R 2如本说明书中所定义，该化合物可用于制备治疗剂。

14. 发明授权

US07501535B2 Chemical synthons and intermediates 有权
标题翻译：化学合成物和中间体
公开(公告)号：US07501535B2
公开(公告)日：2009-03-10
申请号：US10662781
申请日：2003-09-15
申请人： Philip L. Fuchs , David J. Meyers , Eduardo Torres , Taesik Park , In C. Kim , Yuzhong Chen , Douglas Lantrip , Jerry B. Evarts, Jr.
发明人： Philip L. Fuchs , David J. Meyers , Eduardo Torres , Taesik Park , In C. Kim , Yuzhong Chen , Douglas Lantrip , Jerry B. Evarts, Jr.
IPC分类号： C07F556/482 , C07C315/00 , C07D303/00
CPC分类号： C07C323/30 , C07C317/20 , C07C317/24 , C07C323/17 , C07C323/65 , C07C2601/18 , C07F7/1804 , Y02P20/582
摘要： The invention provides novel six and seven-carbon termini-differentiated polypropionate stereotetrads and stereopentads useful in syntheses of natural products. The invention also provides a novel alkylative sulfenylation-desulfonylation process that efficiently transforms enantiopure epoxyvinyl sulfones to syn and anti dienylsulfides in two operations.
摘要翻译：本发明提供了可用于合成天然产物的新颖的六碳和七碳末端分解的丙酸酯立体三
唑和立体孔。本发明还提供了一种新的烷基化亚磺酰化 - 脱磺酰化方法，其在两次操作中有效地将对映异构体环氧乙烯基砜转化成顺式和反式二烯基硫化物。

15. 发明授权

US07351825B2 Cyclopropane compounds and pharmaceutical use thereof 失效
标题翻译：环丙烷化合物及其药物用途
公开(公告)号：US07351825B2
公开(公告)日：2008-04-01
申请号：US11011773
申请日：2004-12-15
申请人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
发明人： Takashi Inaba , Julia Haas , Makoto Shiozaki , Nicole M. Littmann , Katsutaka Yasue , Steven W. Andrews , Atushi Sakai , Andrew M. Fryer , Takafumi Matsuo , Ellen R. Laird , Akira Suma , Yuichi Shinozaki , Yoshikazu Hori , Hiroto Imai , Tamotsu Negoro
IPC分类号： C07D265/00 , C07D295/00 , C07D237/00 , C07D409/00 , C07D411/00 , C07D217/00 , C07D211/00 , C07D213/00 , C07D271/00 , C07D413/00 , C07D498/00 , C07D277/00 , C07D257/00 , C07D233/00 , C07D231/00 , C07D207/00 , C07D333/00 , C07D307/00 , C07D303/00 , C07D309/00 , C07D311/00
CPC分类号： C07C311/29 , C07C311/13 , C07C311/20 , C07C311/22 , C07C311/46 , C07C2601/02 , C07C2601/14 , C07C2603/08 , C07C2603/18 , C07C2603/30 , C07D205/04 , C07D207/48 , C07D209/44 , C07D211/58 , C07D211/96 , C07D213/18 , C07D213/65 , C07D213/71 , C07D213/74 , C07D213/81 , C07D213/82 , C07D217/08 , C07D231/12 , C07D233/64 , C07D237/12 , C07D239/22 , C07D243/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/107 , C07D277/26 , C07D277/36 , C07D277/82 , C07D295/26 , C07D307/79 , C07D307/91 , C07D333/18 , C07D333/34 , C07D333/36 , C07D333/38 , C07D333/62 , C07D401/04 , C07D409/04 , C07D409/12 , C07D413/04 , C07D417/04 , C07D417/12 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有聚集蛋白聚糖蛋白聚糖酶抑制活性和MMP-13抑制活性的化合物，可用作骨关节炎，类风湿性关节炎等的治疗剂，更具体而言，可以使用式（1）的环丙烷化合物：其中R 1 是 - （CH 2）2 -X-（CH 2）n - SUP> 1等，其中m和n相同或不同，并且各自为0至6，X为单键等，而A 1为取代的C _{3-14个烃环基等; R 2和R 3相同或不同，并且各自为氢原子， - （CH 2）2 N 其中p和q为 - （CH 2）2 - - - - CH 2 - 相同或不同，并且各自为0至6，X 1为单键等，而A 2为任选取代的C 3-14烷基，烃环等; R 4是-CO 2 R 9等，其中R 9是氢原子等。 ; 和R 20和R 21相同或不同，各自为氢原子， - （CH 2 CH 2）m 12 其中m12和m12（其中m12和m12）相同或不同，各自为0至6，X 12为单键等，R 30为氢原子等; 或其前药或其药学上可接受的盐。}

16. 发明授权

US07223882B2 Process for producing triterpene derivative 失效
标题翻译：三萜衍生物的制备方法
公开(公告)号：US07223882B2
公开(公告)日：2007-05-29
申请号：US10508476
申请日：2003-03-18
申请人： Haruo Koike , Katsuo Oda , Yutaka Nishino , Makoto Kakinuma
发明人： Haruo Koike , Katsuo Oda , Yutaka Nishino , Makoto Kakinuma
IPC分类号： C07C261/00 , C07C69/74 , C07C229/00 , C07C61/12 , C07D303/00
CPC分类号： A61K31/56 , C07C231/02 , C07J63/00 , C07J75/00 , C07C233/33
摘要： A process for a preparation of Compound (V), a pharmaceutically acceptable salt or a solvate thereof, said process comprising the steps represented by the following formula: wherein R1 and R2 are each independently C1–C8 alkyl.
摘要翻译：一种制备化合物（V），其药学上可接受的盐或溶剂合物的方法，所述方法包括由下式表示的步骤：其中R 1和R 2 2 >各自独立地为C 1 -C 8烷基。

17. 发明授权

US06846938B2 Water-compatible epoxy compounds containing sulfonate or thiosulfate moieties 失效
标题翻译：含有磺酸盐或硫代硫酸盐部分的水溶性环氧化合物
公开(公告)号：US06846938B2
公开(公告)日：2005-01-25
申请号：US10207297
申请日：2002-07-29
申请人： Jeffrey W. Leon , Robert E. McCovick
发明人： Jeffrey W. Leon , Robert E. McCovick
IPC分类号： G03F7/038 , B41C1/10 , B41N1/14 , C07D303/34 , C08G59/14 , C08G59/30 , C07D303/00
CPC分类号： B41C1/1041 , C07D303/34 , C08G59/1411 , C08G59/1483
摘要： Water-compatible branched or unbranched epoxy compounds comprise a backbone having covalently attached two or more epoxy moieties and one or more of the same or different sulfonate or thiosulfate moieties.
摘要翻译：水相溶的支链或非支链环氧化合物包括具有共价连接的两个或多个环氧部分和一个或多个相同或不同的磺酸盐或硫代硫酸盐部分的主链。

18. 发明授权

US6166075A Antiestrogens, process for their production and their pharmaceutical use 失效
标题翻译：抗雌激素，其生产过程及其药物用途
公开(公告)号：US6166075A
公开(公告)日：2000-12-26
申请号：US328451
申请日：1999-06-09
申请人： Ulrich Klar , Rolf Bohlmann , Karsten Parczyk , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner
发明人： Ulrich Klar , Rolf Bohlmann , Karsten Parczyk , Karl-Heinrich Fritzemeier , Monika Lessl , Rosemarie Lichtner
IPC分类号： C07D295/08 , A61K9/127 , A61K31/085 , A61K31/10 , A61K31/135 , A61K31/336 , A61K31/40 , A61K31/4465 , A61K31/45 , A61P5/32 , A61P35/00 , C07C43/23 , C07C217/14 , C07C275/08 , C07C317/18 , C07C323/12 , C07D303/16 , C07D303/22 , C07D303/26 , C07D303/34 , A61K31/22 , A61K31/045 , A61K31/075 , C07D303/00
CPC分类号： C07D303/22 , C07C43/23 , C07C217/14 , C07C317/18 , C07C323/12 , C07C2602/24
摘要： This invention relates to new antiestrogens of the general formula ##STR1## in which the substituents have the meanings that are explained in more detail in the description.The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens).Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.
摘要翻译：本发明涉及通式的新抗雌激素，其中取代基具有在说明书中更详细解释的含义。新化合物是a）纯抗雌激素或b）具有部分雌激素作用的抗雌激素（组织选择性雌激素）。基于这些性质，新化合物适用于生产药剂：a）例如用于治疗乳腺癌的情况; 在b）的情况下，例如用于激素替代疗法。

19. 发明授权

US6139781A Chemiluminescent electron-rich aryl-substituted 1,2-dioxetanes 失效
标题翻译：化学发光富电子的芳基取代的1,2-二氧杂环丁烷
公开(公告)号：US6139781A
公开(公告)日：2000-10-31
申请号：US885445
申请日：1997-06-30
申请人： Nai-Yi Wang , Roger C. Hu
发明人： Nai-Yi Wang , Roger C. Hu
IPC分类号： C07D321/00 , C07D493/04 , C07F7/18 , C07F9/655 , C07F9/6561 , C12Q1/34 , C12Q1/42 , C12Q1/68 , C12Q1/70 , G01N33/533 , G01N33/58 , C09K3/00 , C07D303/00
CPC分类号： G01N33/582 , C07F7/1856 , C07F9/65512 , C12Q1/34 , C12Q1/42 , G01N33/533 , C12Q2334/00 , Y10S435/968
摘要： Chemiluminescent electron-rich aryl-substituted 1,2-dioxetane compounds are disclosed in which the aryl group is poly-substituted with suitable electron-donating groups such that the light-emitting pattern of the molecule results in a very high luminescent count, thus providing for a sensitive and precise assay for haptens, analytes, polynucleotides and the like. These substituted aryl-containing 1,2-dioxetane compounds can be used as direct labels in an immunoassay or when derivatized with an appropriate leaving group, can be used as a substrate for a enzyme immunoassay. The unusual chemiluminescence of the compounds allows the timing of the luminescent reaction to be exactly controlled.
摘要翻译：公开了化学发光富电子的芳基取代的1,2-二氧杂环丁烷化合物，其中芳基被合适的给电子基团多取代，使得分子的发光图案导致非常高的发光计数，从而提供对于半抗原，分析物，多核苷酸等的敏感和精确的测定。这些取代的含芳基的1,2-二氧杂环丁烷化合物可以在免疫测定中用作直接标记，或者当用合适的离去基团衍生化时，可用作酶免疫测定的底物。化合物的不寻常的化学发光使得准确控制发光反应的时间。

20. 发明授权

US6107433A Process for the preparation of vegetable oil-based polyols and electroninsulating casting compounds created from vegetable oil-based polyols 有权
标题翻译：由植物油基多元醇制备的植物油基多元醇和电子注射铸造化合物的制备方法
公开(公告)号：US6107433A
公开(公告)日：2000-08-22
申请号：US187992
申请日：1998-11-06
申请人： Zoran Petrovic , Andrew Guo , Ivan Javni
发明人： Zoran Petrovic , Andrew Guo , Ivan Javni
IPC分类号： C07D303/42 , C08G18/36 , C08G83/00 , C07D301/00 , C07D301/14 , C07D301/19 , C07D303/00
CPC分类号： C08G18/36 , C07D303/42 , C08G2190/00
摘要： A vegetable oil-based polyol is made by adding a peroxyacid to vegetable oil wherein said peroxyacid reacts with said vegetable oil to form epoxidized vegetable oil and adding said epoxidized vegetable oil to a mixture of an alcohol, water, and a catalytic amount of fluoboric acid so as to form a vegetable oil-based polyol. A further embodiment of the present invention involves making a vegetable oil-based polyol using an epoxidized vegetable oil as the starting material. The epoxidized vegetable oil undergoes hydroxylation by the same process as outlined above. According to another aspect of the present invention, the vegetable oil-based polyol formed by the novel methods of this invention may be reacted with an isocyanate to form a polyurethane. Alternatively, a filler such as silica may be combined with the vegetable oil-based polyol before it is reacted with the isocyanate. These polyurethanes made from vegetable oil-based polyols may be used to form electroinsulating casting resins.
摘要翻译：通过向植物油中加入过氧酸而制备植物油性多元醇，其中所述过氧酸与所述植物油反应形成环氧化植物油，并将所述环氧化植物油加入到醇，水和催化量的氟硼酸的混合物中以形成植物油基多元醇。本发明的另一个实施方案涉及使用环氧化植物油作为原料制备植物油基多元醇。环氧化植物油通过与上述相同的方法进行羟基化。根据本发明的另一方面，通过本发明的新方法形成的植物油基多元醇可以与异氰酸酯反应形成聚氨酯。或者，诸如二氧化硅的填料可以在与异氰酸酯反应之前与植物油基多元醇组合。这些由植物油基多元醇制成的聚氨酯可用于形成电绝缘铸塑树脂。

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