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1. 发明申请

WO2012006475A1 COMPOUNDS AND METHODS FOR INHIBITING PHOSPHATE TRANSPORT 审中-公开
标题翻译：抑制磷酸盐运输的化合物和方法
公开(公告)号：WO2012006475A1
公开(公告)日：2012-01-12
申请号：PCT/US2011/043263
申请日：2011-07-07
申请人： ARDELYX, INC. , LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric , DU, Xunxiang , OSLOB, Johan
发明人： LEWIS, Jason, G. , JACOBS, Jeffrey, W. , REICH, Nicholas , LEADBETTER, Michael, R. , BELL, Noah , CHANG, Han-Ting , CHEN, Tao , NAVRE, Marc , CHARMOT, Dominique , CARRERAS, Christopher , LABONTE, Eric , DU, Xunxiang , OSLOB, Johan
IPC分类号： G01N33/48 , G01N31/00 , G01G23/01 , G06G7/58
CPC分类号： A61K33/24 , A61K31/19 , A61K31/415 , A61K31/4192 , A61K31/4418 , A61K31/4433 , A61K31/4439 , A61K31/4453 , A61K31/454 , A61K31/4545 , A61K31/465 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/522 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/706 , A61K31/785 , A61K33/10 , A61K45/06 , C07D213/81 , C07D295/155 , C07D401/12 , C07D405/12 , C07D417/12
摘要： Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：具有作为磷酸盐转运抑制剂的活性的化合物，更具体地，公开了肠顶膜Na /磷酸盐共转运的抑制剂。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

2. 发明申请

WO2010078449A3 COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS 审中-公开
标题翻译：抑制NHE介导的抗生素治疗与流体滞留，盐负荷过重和胃肠道病变相关的疾病的化合物和方法
公开(公告)号：WO2010078449A3
公开(公告)日：2010-09-30
申请号：PCT/US2009069852
申请日：2009-12-30
申请人： ARDELYX INC , CHARMOT DOMINIQUE , JACOBS JEFFREY W , LEADBETTER MICHAEL ROBERT , NAVRE MARC , CARRERAS CHRIS , BELL NOAH
发明人： CHARMOT DOMINIQUE , JACOBS JEFFREY W , LEADBETTER MICHAEL ROBERT , NAVRE MARC , CARRERAS CHRIS , BELL NOAH
IPC分类号： C07C311/29 , A61K31/18 , A61K31/472 , A61K31/4725 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , C07D217/04 , C07D401/12 , C07F9/38 , C07F9/40 , C07F9/572 , C07F9/62
CPC分类号： A61K31/4725 , A61K31/18 , A61K31/472 , A61K31/517 , A61K31/662 , A61K31/675 , A61K45/06 , 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 and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract.
摘要翻译：本公开涉及用于治疗与体液潴留或盐超负荷相关的病症例如心力衰竭（特别是充血性心力衰竭），慢性肾病，终末期肾病，肝病和过氧化物酶体的化合物和方法增殖激活受体（PPAR）γ激动剂诱导的液体潴留。本公开还涉及用于治疗高血压的化合物和方法。本公开还涉及用于治疗胃肠道病症的化合物和方法，包括治疗或减轻与胃肠道病症相关的疼痛。所述方法通常包括向需要其的哺乳动物施用药物有效量的化合物或包含该化合物的药物组合物，其被设计为在胃肠（GI）道中基本上具有活性以抑制NHE介导的钠离子和氢离子。更特别地，所述方法包括向需要其的哺乳动物施用药学有效量的化合物或包含该化合物的药物组合物，其抑制NHE-3，-2和/或-8介导的钠和/或氢气离子在胃肠道中，并被设计为对上皮细胞层，或更具体而言，胃肠道的上皮层基本上不可渗透。由于该化合物基本上不可渗透，所以它不被吸收，因此基本上不具有生物可利用性，从而限制其它内部器官（例如肝脏，心脏，脑等）暴露于其中。本发明还进一步涉及一种方法，其中将哺乳动物与流体吸收聚合物一起给予这种化合物，使得所述组合如上所述起作用并进一步提供螯合存在于胃肠道中的流体和/或盐的能力。

3. 发明申请

WO2010022383A2 CROSSLINKED CATION EXCHANGE POLYMERS, COMPOSITIONS AND USE IN TREATING HYPERKALEMIA 审中-公开
标题翻译：交联剂交联聚合物，组合物和用于治疗高血压
公开(公告)号：WO2010022383A2
公开(公告)日：2010-02-25
申请号：PCT/US2009054706
申请日：2009-08-22
申请人： RELYPSA INC , MANSKY PAUL , ALBRECHT DETLEF , BURDICK MICHAEL , CHANG HAN-TING , CHARMOT DOMINIQUE , CONNOR ERIC , HALFON SHERIN , HUANG I-ZU , LIU MINGJUN , CHIDAMBARAM RAMAKRISHNAN , MILLS JONATHAN , STRUEVER WERNER
发明人： MANSKY PAUL , ALBRECHT DETLEF , BURDICK MICHAEL , CHANG HAN-TING , CHARMOT DOMINIQUE , CONNOR ERIC , HALFON SHERIN , HUANG I-ZU , LIU MINGJUN , CHIDAMBARAM RAMAKRISHNAN , MILLS JONATHAN , STRUEVER WERNER
IPC分类号： C08F4/68
CPC分类号： A61K31/78 , A61K9/14 , A61K31/7004 , A61K47/26 , B01J39/20 , C08F212/36 , C08F220/22
摘要： The present invention is directed to crosslinked cation exchange polymers comprising a fluoro group and an acid group, pharmaceutical compositions of these polymers, compositions of a linear polyol and a salt of such polymer. Crosslinked cation exchange polymers having beneficial physical properties, including combinations of particle size, particle shape, particle size distribution, viscosity, yield stress, compressibility, surface morphology, and/or swelling ratio are also described. These polymers and compositions are useful to bind potassium in the gastrointestinal tract.
摘要翻译：本发明涉及包含氟基团和酸基团的交联阳离子交换聚合物，这些聚合物的药物组合物，线型多元醇的组合物和这种聚合物的盐。还描述了具有有益物理性质的交联阳离子交换聚合物，包括粒度，颗粒形状，粒度分布，粘度，屈服应力，压缩性，表面形态和/或溶胀比的组合。这些聚合物和组合物可用于结合胃肠道中的钾。

4. 发明申请

WO2010022381A1 TREATING HYPERKALEMIA WITH CROSSLINKED CATION EXCHANGE POLYMERS OF IMPROVED PHYSICAL PROPERTIES 审中-公开
标题翻译：用改进的物理特性的交联剂交换聚合物处理高分子量
公开(公告)号：WO2010022381A1
公开(公告)日：2010-02-25
申请号：PCT/US2009/054704
申请日：2009-08-22
申请人： RELYPSA, INC. , ALBRECHT, Detlef , MANSKY, Paul , BURDICK, Michael , CHANG, Han-Ting , CHARMOT, Dominique , CONNOR, Eric , HALFON, Sherin , HUANG, I-Zu , LIU, Mingjun , STRÜVER, Werner
发明人： ALBRECHT, Detlef , MANSKY, Paul , BURDICK, Michael , CHANG, Han-Ting , CHARMOT, Dominique , CONNOR, Eric , HALFON, Sherin , HUANG, I-Zu , LIU, Mingjun , STRÜVER, Werner
IPC分类号： A61K31/74 , A61P1/00
CPC分类号： A61K31/78 , A61K31/74
摘要： The present invention is directed to methods of removing potassium or treating hyperkalemia by administering pharmaceutical compositions of crosslinked cation exchange polymers having beneficial physical properties, including combinations of particle size, particle shape, particle size distribution, viscosity, yield stress, compressibility, surface morphology, and/or swelling ratio.
摘要翻译：本发明涉及通过施用具有有益物理性质的交联阳离子交换聚合物的药物组合物来除去钾或治疗高钾血症的方法，包括粒度，颗粒形状，粒度分布，粘度，屈服应力，压缩性，表面形态，和/或溶胀比。

5. 发明申请

WO2007038801A3 MONOVALENT CATION-BINDING COMPOSITIONS COMPRISING CORE-SHELL PARTICLES HAVING CROSSLINKED POLY-VINYLIC SHELLS, AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2007038801A3
公开(公告)日：2007-04-05
申请号：PCT/US2006/038899
申请日：2006-10-02
申请人： ILYPSA, INC. , LIU, Futian , CHANG, Han-Ting , CHARMOT, Dominique , LIU, Mingjun , CONNOR, Eric
发明人： LIU, Futian , CHANG, Han-Ting , CHARMOT, Dominique , LIU, Mingjun , CONNOR, Eric
IPC分类号： A61K31/75 , A61K31/78 , A61K31/795 , A61K9/50 , A61P3/12
摘要： The present invention provides methods and compositions for the treatment of ion imbalances using core-shell composites and compositions comprising such core-shell composites. In particular, the invention provides core-shell particles and compositions comprising potassium binding polymers, and core-shell particles and compositions comprising sodium binding polymers, and in each case, pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are also disclosed. The compositions and methods of the invention offer improved approaches for treatment of hyperkalemia and other indications related to potassium ion homeostasis, and for treatment of hypertension and other indicates related to sodium ion homeostasis.

6. 发明申请

WO2005107767A2 MODULATION OF LYSOPHOSPHATIDYLCHOLINE AND TREATMENT OF DIET-INDUCED CONDITIONS 审中-公开
标题翻译：溶血磷脂酰胆碱的调节及膳食诱导条件的处理
公开(公告)号：WO2005107767A2
公开(公告)日：2005-11-17
申请号：PCT/US2005/015625
申请日：2005-05-03
申请人： ILYPSA, INC. , CHARMOT, Dominique , BUYSSE, Jerry, M. , HUY, David
发明人： CHARMOT, Dominique , BUYSSE, Jerry, M. , HUY, David
IPC分类号： A61K31/685
CPC分类号： A61K31/685 , A61K31/70
摘要： The present invention provides methods for the treatment of lysophosphatidylcholine-related conditions. In particular, the invention provides a method of treating an insulin-related condition, e.g., diabetes or diabetes type 2, and/or a weight-related-condition, e.g., unwanted weight gain or obesity, in an animal subject by reducing production, absorption and/or activity of lysophosphatidylcholine. Further, the beneficial effects of reducing lysophosphatidylcholine in terms of diabetes and weight gain are disclosed.
摘要翻译：本发明提供了治疗溶血磷脂酰胆碱相关病症的方法。具体而言，本发明提供了通过降低产量来治疗动物受试者中的胰岛素相关病症例如2型糖尿病或2型糖尿病和/或体重相关病症例如不想要的体重增加或肥胖的方法，吸收和/或溶血磷脂酰胆碱的活性。此外，公开了降低溶血磷脂酰胆碱在糖尿病和体重增加方面的有益作用。

7. 发明申请

WO2005097072A1 ION BINDING COMPOSITIONS 审中-公开
标题翻译：离子键合组合物
公开(公告)号：WO2005097072A1
公开(公告)日：2005-10-20
申请号：PCT/US2005/010747
申请日：2005-03-30
申请人： ILYPSA, INC. , CHARMOT, Dominique , FORDTRAN, John , CHANG, Han Ting , CONNOR, Eric , LIU, Mingjun , KLAERNER, Gerrit
发明人： CHARMOT, Dominique , FORDTRAN, John , CHANG, Han Ting , CONNOR, Eric , LIU, Mingjun , KLAERNER, Gerrit
IPC分类号： A61K9/14
CPC分类号： A61K31/78 , A61K9/14 , A61K9/1635 , A61K9/5026 , A61K9/5031 , A61K31/74 , A61K31/785 , A61K31/795 , A61K31/80 , A61K45/06 , C08F120/06 , C08F128/02 , Y10S514/838 , Y10S514/869 , Y10S514/87 , Y10S514/893
摘要： The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides core-shell compositions and pharmaceutical compositions thereof. Methods of use of the core-shell compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of phosphate imbalance disorders, hypertension, chronic heart failure, end stage renal disease, liver cirrhosis, chronic renal insufficiency, fluid overload, or sodium overload.
摘要翻译：本发明提供了用于治疗离子失衡的方法和组合物。特别地，本发明提供了核 - 壳组合物及其药物组合物。本文公开了用于治疗和/或预防益处的核 - 壳组合物的使用方法。这些方法的实例包括治疗磷酸盐不平衡障碍，高血压，慢性心力衰竭，终末期肾病，肝硬化，慢性肾功能不全，流体过载或钠过载。

8. 发明申请

WO2005003198A1 PHOTORESIST POLYMER COMPOSITIONS 审中-公开
标题翻译：光电聚合物组合物
公开(公告)号：WO2005003198A1
公开(公告)日：2005-01-13
申请号：PCT/US2004/020351
申请日：2004-06-25
申请人： JSR CORPORATION , BENOIT, Didier , SAFIR, Adam , CHANG, Han-Ting , CHARMOT, Dominique , NISHIMURA, Isao , SOYANO, Akimasa , OKAMOTO, Kenji , WANG, Yong
发明人： BENOIT, Didier , SAFIR, Adam , CHANG, Han-Ting , CHARMOT, Dominique , NISHIMURA, Isao , SOYANO, Akimasa , OKAMOTO, Kenji , WANG, Yong
IPC分类号： C08F220/18
CPC分类号： C08F220/18 , C08F20/18 , C08F220/28 , G03F7/0397
摘要： The present invention is directed to the preparation of photoresist polymers via living free radical polymerization techniques. Sterically bulky ester monomers are utilized as the polymerization components. Use of chain transfer agents is included in polymerization processing conditions. Cleavage of polymer terminal end groups that include a heteroatom are described.
摘要翻译：本发明涉及通过活性自由基聚合技术制备光致抗蚀剂聚合物。用作单体体积大的酯单体作为聚合组分。链转移剂的使用包括在聚合工艺条件中。描述了包含杂原子的聚合物末端基团的切割。

9. 发明申请

WO2003076922A1 COPOLYMERS FOR USE IN CAPILLARY ELECTROPHORETIC SEPARATION MEDIA 审中-公开
标题翻译：用于毛细管电泳分离介质的共聚物
公开(公告)号：WO2003076922A1
公开(公告)日：2003-09-18
申请号：PCT/US2003/006334
申请日：2003-02-26
申请人： SYMYX TECHNOLOGIES, INC. , BENOIT, Dider , CHARMOT, Dominique , HAJDUK, Damian , KLAERNER, Gerrit , NGUYEN, Son, Hoai , PIOTTI, Marcelo , LIN, Shan
发明人： BENOIT, Dider , CHARMOT, Dominique , HAJDUK, Damian , KLAERNER, Gerrit , NGUYEN, Son, Hoai , PIOTTI, Marcelo , LIN, Shan
IPC分类号： G01N27/447
CPC分类号： G01N27/44747
摘要： Graft and block copolymers are used in separation media for capillary electrophoseris separation of biological or other molecules, with the copolymers comprising one segment being made from monomers that form an effective dynamic wall coating agent and another segment being made from monomers that form an effective sieving agent. The copolymers can be used alone or with other polymers that are either sieving polymers, wall coating polymers or both.
摘要翻译：接枝和嵌段共聚物用于生物或其他分子的毛细管电泳分离的分离介质中，共聚物包含一个链段由形成有效动态壁涂剂的单体制成，另一个链段由形成有效筛分剂的单体制成。共聚物可以单独使用或与其他聚合物一起使用，这些聚合物是筛分聚合物，壁涂层聚合物或两者。

10. 发明申请

WO0109204A9 CONTROLLED-ARCHITECTURE POLYMERS AND USE THEREOF AS SEPARATION MEDIA 审中-公开
标题翻译：控制结构聚合物及其用作分离介质的用途
公开(公告)号：WO0109204A9
公开(公告)日：2002-09-26
申请号：PCT/US0020850
申请日：2000-07-31
申请人： SYMYX TECHNOLOGIES INC , KLAERNER GERRIT , PETRO MIROSLAV , BENOIT DIDIER , CHARMOT DOMINIQUE
发明人： KLAERNER GERRIT , PETRO MIROSLAV , BENOIT DIDIER , CHARMOT DOMINIQUE
IPC分类号： C08F2/38 , C08F220/54 , C08F220/58 , G01N27/447 , G01N33/543 , C08F220/56 , C08F293/00
CPC分类号： C08F220/58 , C08F220/54 , G01N27/44747 , G01N33/54353
摘要： Controlled architecture polymers made preferably with acrylamide type monomers are prepared in living-type or semi-living-type free radical polymerizations, with the architecture preferably being other than linear, such as star, branched, grafted or hyper-branched. The controlled architecture polymers have high weight average molecular weights and low viscosities, which make them particularly useful in replaceable capillary electrophoresis separation media for biological molecules, such as DNA fragments.
摘要翻译：用活性型或半活性型自由基聚合制备优选用丙烯酰胺型单体制备的受控结构聚合物，其结构优选不是线性的，如星形，支化，接枝或超支化。受控结构聚合物具有高重均分子量和低粘度，这使得它们在用于生物分子如DNA片段的可置换毛细管电泳分离介质中特别有用。

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