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1. 发明申请

US20150166585A1 BISPHOSPHONATES VINYLIC MONOMERS AND POLYMERS AND USES THEREOF 有权
标题翻译：二硫代苯乙烯单体和聚合物及其用途
公开(公告)号：US20150166585A1
公开(公告)日：2015-06-18
申请号：US14401964
申请日：2013-05-20
申请人： BAR-ILAN UNIVERSITY
发明人： Shlomo Margel , Dana Mizrahi , Eran Gluz , Ravit Chen
IPC分类号： C07F9/38 , A61K31/80 , A61K49/00 , A61K45/06 , A61K9/16 , C08F220/60 , A61K31/663
CPC分类号： C07F9/3873 , A61K9/1635 , A61K31/663 , A61K31/80 , A61K45/06 , A61K47/6933 , A61K49/0034 , A61K49/0052 , A61K49/0054 , A61K49/0093 , A61K2123/00 , C07F9/386 , C07F9/3882 , C07F9/65583 , C08F220/60
摘要： The present invention provides novel bisphosphonates vinylic monomers, polymers and particles that have utility as biologically active molecule (such as drugs) carriers, medical device coatings and for imaging/radiology applications, especially in bone and dental applications. The invention also provides methods of synthesizing the monomers, polymerizing the polymers, and assembling the particles of the invention.
摘要翻译：本发明提供了新型的双膦酸盐乙烯基单体，聚合物和颗粒，其具有生物活性分子（例如药物）载体，医疗器械涂层和成像/放射学应用的用途，特别是在骨和牙科应用中。本发明还提供合成单体，聚合聚合物和组装本发明颗粒的方法。

2. 发明授权

US08969377B2 Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders 有权
标题翻译：用于抑制NHE介导的止痒剂用于治疗与流体保留或盐过载和胃肠道疾病相关的疾病的化合物和方法
公开(公告)号：US08969377B2
公开(公告)日：2015-03-03
申请号：US13804752
申请日：2013-03-14
申请人： Ardelyx, Inc.
发明人： Noah Bell , Christopher Carreras , Dominique Charmot , Jeffrey W Jacobs , Michael Robert Leadbetter , Marc Navre
IPC分类号： A61K31/18 , C07F9/60 , A61K31/472 , A61K31/4725 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , C07C311/29 , C07D217/04 , C07D217/14 , C07D401/12 , C07F9/38 , C07F9/576 , C07F9/6558 , C07D217/16 , C07D215/14
CPC分类号： A61K31/4725 , A61K31/18 , A61K31/472 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , A61K47/55 , A61P1/00 , A61P7/10 , A61P9/04 , A61P9/12 , C07C311/29 , C07D215/14 , C07D217/04 , C07D217/14 , C07D217/16 , C07D401/12 , C07F9/3808 , C07F9/3834 , C07F9/3882 , C07F9/5765 , C07F9/60 , C07F9/65583
摘要： The present disclosure is directed to compounds of the structure (X): wherein: n is 2 or 3; NHE has the structure wherein: R1 is H or —SO2—NR7R8—; R2 is selected from H, —NR7(CO)R8, —SO2—NR7R8— and —NR7R8; R3 is hydrogen; R7 is hydrogen; R8 is a bond linking to L; L is a polyalkylene glycol linker; and Core has the following structure: wherein: X is selected from the group consisting of a bond, —O—, —NH—, NHC(═O)—, —NHC(═O)NH— and —NHSO2—; and Y is selected from the group consisting of a bond, optionally substituted C1-6 alkylene, optionally substituted benzene, pyridinyl, a polyethylene glycol linker and —(CH2)1-6O(CH2)1-6—, and methods of using such compounds for the treatment of irritable bowel syndrome, chronic kidney disease and end-stage renal disease.
摘要翻译：本公开涉及结构（X）的化合物：其中：n为2或3; NHE具有以下结构：其中：R1是H或-SO2-NR7R8-; R2选自H，-NR7（CO）R8，-SO2-NR7R8-和-NR7R8; R3是氢; R7是氢; R8是连接L的键; L是聚亚烷基二醇连接体; 和Core具有以下结构：其中：X选自键，-O - ， - NH - ，NHC（= O） - ， - NHC（= O）NH-和-NHSO 2 - ; 和Y选自由以下组成的组：任选取代的C 1-6亚烷基，任选取代的苯，吡啶基，聚乙二醇连接体和 - （CH 2）1-6 O（CH 2）1-6 - 用于治疗肠易激综合征，慢性肾脏疾病和终末期肾病的化合物。

3. 发明申请

US20140235592A1 SUBSTITUTED 6-METHOXY-4-AMINO-N-PHENYL-2-NAPHTAMIDES AS SPHINGOSINE RECEPTOR MODULATORS 审中-公开
标题翻译：取代的6-甲氧基-4-氨基-N-苯基-2-二磷酸酯作为丝氨酸受体调节剂
公开(公告)号：US20140235592A1
公开(公告)日：2014-08-21
申请号：US14184224
申请日：2014-02-19
申请人： Allergan, Inc.
发明人： Janet A. Takeuchi , Ling Li , Wha Bin Im
IPC分类号： C07F9/38 , C07C237/48
CPC分类号： C07F9/3895 , A61K31/136 , C07C237/48 , C07C2601/02 , C07F9/3882
摘要： The present invention relates to substituted 6-methoxy-4-amino-N-phenyl-2-naphtamides derivatives, processes for preparing them, pharmaceutical compositions to containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
摘要翻译：本发明涉及取代的6-甲氧基-4-氨基-N-苯基-2-萘甲酰胺衍生物，其制备方法，含有它们的药物组合物及其作为药物作为鞘氨醇-1-磷酸受体调节剂的用途。

4. 发明申请

US20140235587A1 SUBSTITUTED PYRAZOLES AS SPHINGOSINE RECEPTOR MODULATORS 审中-公开
标题翻译：替代吡咯烷酮作为受体调节剂
公开(公告)号：US20140235587A1
公开(公告)日：2014-08-21
申请号：US14179693
申请日：2014-02-13
申请人： Allergan, Inc.
发明人： Janet A. Takeuchi , Ling Li , Wha Bin Im , KEN CHOW
IPC分类号： C07F9/6558 , C07D413/04
CPC分类号： C07D413/04 , C07F9/3882
摘要： The present invention relates to substituted pyrazoles, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
摘要翻译：本发明涉及取代的吡唑，其制备方法，含有它们的药物组合物及其作为药物作为鞘氨醇-1-磷酸受体调节剂的用途。

5. 发明申请

US20130289174A1 SURFACE-MODIFIED PIGMENT PREPARATIONS 有权
标题翻译：表面改性颜料制剂
公开(公告)号：US20130289174A1
公开(公告)日：2013-10-31
申请号：US13976045
申请日：2011-12-15
申请人： Philippe Bugnon , Peter Nesvadba
发明人： Philippe Bugnon , Peter Nesvadba
IPC分类号： C09D7/00 , C09D11/02
CPC分类号： C09D7/007 , C07C245/04 , C07C255/65 , C07C281/20 , C07C309/51 , C07C2601/14 , C07C2601/20 , C07F9/3808 , C07F9/3882 , C07F9/4006 , C09B67/0004 , C09B67/0034 , C09B68/26 , C09B68/4475 , C09D7/41 , C09D11/037
摘要： A pigment preparation is provided, said preparation comprises an organic pigment comprising a chromophore Q1 and a derivative thereof comprising specific organic substituents via an aliphatic carbon atom in an amount of from 0.1 to 30 mol, based on 100 mol of the organic pigment as well as a process for its preparation and to its use in coloring an organic material such as plastics, coatings or inks.
摘要翻译：提供颜料制剂，所述制剂包含有机颜料，其包含发色团Q1及其衍生物，其衍生物含有基于100mol有机颜料的0.1-30mol脂族碳原子的特定有机取代基，以及其制备方法和用于着色有机材料如塑料，涂料或油墨的方法。

6. 发明申请

US20120283221A1 NOVEL PHOSPHONIC ACID COMPOUNDS AS INHIBITORS OF SERINE PROTEASES 失效
公开(公告)号：US20120283221A1
公开(公告)日：2012-11-08
申请号：US13550963
申请日：2012-07-17
申请人： Michael N. Greco , Harold R. Almond, JR. , Lawrence de Garavilla , Michael J. Hawkins , Michael J. Humora , Yun Qian , Donald Gilmore Walker , Sergio Cesco-Cancian , Christopher Norman Nillsen , Mitul N. Patel , Kirk Leonard Sorgi , Eugene Powell
发明人： Michael N. Greco , Harold R. Almond, JR. , Lawrence de Garavilla , Michael J. Hawkins , Michael J. Humora , Yun Qian , Donald Gilmore Walker , Sergio Cesco-Cancian , Christopher Norman Nillsen , Mitul N. Patel , Kirk Leonard Sorgi , Eugene Powell
IPC分类号： A61K31/675 , C07F9/40 , C07F9/576 , A61K31/662 , C07F9/6509
CPC分类号： C07F9/65586 , C07F9/3882 , C07F9/572 , C07F9/59 , C07F9/650952 , C07F9/65517 , C07F9/65583 , C07F9/6561
摘要： The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.

7. 发明申请

US20120083471A1 Novel Compounds, Pharmaceutical Compositions Containing Same, Methods of Use for Same, and Methods for Preparing Same 审中-公开
标题翻译：新型化合物，含有其的药物组合物，其使用方法及其制备方法
公开(公告)号：US20120083471A1
公开(公告)日：2012-04-05
申请号：US13273740
申请日：2011-10-14
申请人： Craig A. Townsend , Edward Wydysh , Francis Kuhajda , Gabriele Valeria Ronnett
发明人： Craig A. Townsend , Edward Wydysh , Francis Kuhajda , Gabriele Valeria Ronnett
IPC分类号： A61K31/662 , C07D333/24 , C07D213/55 , C07C311/06 , A61K31/4418 , A61K31/505 , A61K31/381 , A61K31/196 , C07C311/08 , C07F9/38 , C07C311/21 , C07C311/13 , A61K31/195 , A61P3/04 , A61P3/00 , C07D239/26
CPC分类号： C07C311/08 , A61K31/18 , C07C311/06 , C07C311/13 , C07C311/21 , C07D213/55 , C07D333/24 , C07F9/3834 , C07F9/3882
摘要： The present invention relates to novel pharmaceutical compositions containing the same, and methods of use for a variety of therapeutically valuable uses including, but not limited to, treating obesity by inhibiting the activity of Glycerol 3-phosphate acyltransferase (GPAT).
摘要翻译：本发明涉及含有该组合物的新型药物组合物，以及用于各种治疗有价值的用途的方法，包括但不限于通过抑制甘油3-磷酸酰基转移酶（GPAT）的活性来治疗肥胖症。

8. 发明申请

US20110092457A1 NOVEL PHOSPHONIC ACID COMPOUNDS AS INHIBITORS OF SERINE PROTEASES 有权
公开(公告)号：US20110092457A1
公开(公告)日：2011-04-21
申请号：US12972891
申请日：2010-12-20
申请人： Michael N. Greco , Harold R. Almond, JR. , Michael J. Hawkins , Eugene Powell
发明人： Michael N. Greco , Harold R. Almond, JR. , Michael J. Hawkins , Eugene Powell
IPC分类号： A61K31/675 , C07F9/58 , C07F9/38 , C07F9/572 , C07F9/6561 , C07F9/6509 , A61K31/662
CPC分类号： C07F9/65586 , C07F9/3882 , C07F9/572 , C07F9/59 , C07F9/650952 , C07F9/65517 , C07F9/65583 , C07F9/6561
摘要： The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.

9. 发明授权

US07829552B2 Phosphorus-containing thyromimetics 失效
标题翻译：含磷的甲状腺素
公开(公告)号：US07829552B2
公开(公告)日：2010-11-09
申请号：US10580134
申请日：2004-11-19
申请人： Mark D. Erion , Hongjian Jiang , Serge H. Boyer
发明人： Mark D. Erion , Hongjian Jiang , Serge H. Boyer
IPC分类号： A61K31/66 , C07F9/02
CPC分类号： C07F9/4056 , C07F9/301 , C07F9/306 , C07F9/3808 , C07F9/3882 , C07F9/4006 , C07F9/4075 , C07F9/4407 , C07F9/4465 , C07F9/5728 , C07F9/58 , C07F9/65517 , C07F9/657181
摘要： The present invention relates to compounds of phosphonic acid containing T3 mimetics, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndromex and diabetes.
摘要翻译：本发明涉及含有T3模拟物的膦酸化合物，其立体异构体，药学上可接受的盐，共晶体和前体药物以及前体药学上可接受的盐和共晶体，以及它们的制备和用途，用于预防和/或治疗代谢疾病如肥胖，NASH，高胆固醇血症和高脂血症，以及相关病症如动脉粥样硬化，冠心病，糖耐量异常，代谢综合征和糖尿病。

10. 发明授权

US07691898B2 Phosphonic acid derivatives and the treating agents of diseases related hyperphosphatemia 失效
标题翻译：膦酸衍生物和疾病相关高磷血症的治疗剂
公开(公告)号：US07691898B2
公开(公告)日：2010-04-06
申请号：US11664830
申请日：2005-10-05
申请人： Hiroshi Tomiyama , Masayuki Yokota , Kazuo Tokuzaki , Ryoko Tomita
发明人： Hiroshi Tomiyama , Masayuki Yokota , Kazuo Tokuzaki , Ryoko Tomita
IPC分类号： A61K31/381 , C07D333/46 , C07F9/30
CPC分类号： C07F9/6541 , C07F9/3834 , C07F9/3882 , C07F9/3891 , C07F9/59 , C07F9/6539 , C07F9/65517 , C07F9/655345 , C07F9/655354 , C07F9/6558 , C07F9/65586
摘要： This invention related to a series of new phosphonic acid derivatives having anti-hyperphosphatemia activity. wherein: A is selected from —(CH2)n—, —CO—, —(CH2)n—CO—(CH2)m—, —(CH2)n—CS—(CH2)m— or a branched alkylene group, B ring and C ring are selected from a benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle compound, D is —(CH2)(n+1)—, —(CH2)—O—(CH2)m—, —(CH2)—S(O)o—(CH2)m—, —CF3 or —(CH2)n—NR10—(CH2)m— wherein a D ring is connected with the carbon atom composing the C ring, E is selected from an oxygen atom or a sulfur atom, P is a phosphine atom, R1˜R7, wherein R1 and R2, R4 and R5 are joined together with neighbored carbon atom to form 5˜7 membered saturated or unsaturated hydrocarbon ring, or 5˜6 membered fused heterocycle, R1, R2 and R3 are not a hydrogen atom if the B ring is a benzene ring and may be the same or different and are substituents, R8 and R9 are may be the same or different and are substituents, R10 is an alkyl group, n and m are 0-10 and o is 0-2.
摘要翻译：本发明涉及一系列具有抗高磷酸血症活性的新型膦酸衍生物。其中：A选自 - （CH 2）n - ， - CO - ， - （CH 2）n -CO-（CH 2）m - ， - （CH 2）n -C CS-（CH 2）m-或支链亚烷基， B环和C环选自苯环，萘环，薁环或杂环或稠合杂环化合物，D是 - （CH 2）（n + 1） - ， - （CH 2）-O-（CH 2）m - ， - （CH2）-S（O）o-（CH2）m-，-CF3或 - （CH2）n-NR10-（CH2）m-，其中D环与构成C环的碳原子连接，E 选自氧原子或硫原子，P为膦原子，R1〜R7，其中R1和R2，R4和R5与邻位碳原子连接在一起形成5〜7元饱和或不饱和烃环，或5 如果B环是苯环并且可以相同或不同，并且是取代基，则R 6，R 6和R 3不是氢原子，R 8和R 9可以相同或不同，并且是取代基R 10 是烷基，n和m是0-10，o是0-2。

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