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11. 发明申请

WO2010085246A1 2,4-DIAMINO-1,3,5-TRIAZINE AND 4, 6-DIAMINO-PYRIMIDINE DERIVATIVES AND THEIR USE AS AGGRECANASE INHIBITORS 审中-公开
标题翻译： 2,4-二氨基-1,3,5-三嗪和4,6-二氨基 - 吡啶衍生物及其作为AGGRECANASE抑制剂的用途
公开(公告)号：WO2010085246A1
公开(公告)日：2010-07-29
申请号：PCT/US2009/031575
申请日：2009-01-21
申请人： PRAECIS PHARMACEUTICALS INC , DING, Yun
发明人： DING, Yun
IPC分类号： C07D251/18 , C07D251/54 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/12 , C07D417/12 , A61P29/00 , A61K31/53
CPC分类号： C07D401/04 , C07D251/18 , C07D251/54 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The invention is directed to compounds of formula (I): that modulate, e.g., inhibit, aggrecanase proteolytic activity, which is implicated in joint diseases including osteoarthritis, joint injury, reactive arthritis, acute pyrophosphate arthritis, psoriatic arthritis, and rheumatoid arthritis. The current invention also relates to processes for making the compounds of the invention and to pharmaceutical compositions containing these compounds. The present invention further provides methods of treating diseases associated with aggrecanase activity, e.g., osteoarthritis and other joint diseases, using the compounds of the invention.
摘要翻译：本发明涉及式（I）化合物：调节，例如抑制聚集蛋白聚糖蛋白酶解蛋白水解活性，其涉及关节疾病，包括骨关节炎，关节损伤，反应性关节炎，急性焦磷酸关节炎，牛皮癣关节炎和类风湿性关节炎。本发明还涉及制备本发明化合物的方法和含有这些化合物的药物组合物。本发明还提供使用本发明化合物治疗与聚集蛋白聚糖酶活性相关的疾病，例如骨关节炎和其它关节疾病的方法。

12. 发明申请

WO2007022239A2 PHARMACEUTICAL FORMULATIONS FOR SUSTAINED DRUG DELIVERY 审中-公开
标题翻译：用于持续输送药物的药物制剂
公开(公告)号：WO2007022239A2
公开(公告)日：2007-02-22
申请号：PCT/US2006/031938
申请日：2006-08-15
申请人： PRAECIS PHARMACEUTICALS, INC. , MUSSO, Gary, F. , BARKER, Nicholas , WOLFE, Janet, L. , YE, Ming
发明人： MUSSO, Gary, F. , BARKER, Nicholas , WOLFE, Janet, L. , YE, Ming
IPC分类号： A61K47/48
CPC分类号： A61K31/717 , A61K9/0019 , A61K38/17 , A61K47/38 , A61K47/61
摘要： The present invention provides pharmaceutical formulations comprising a solid ionic complex of a polypeptide having an isoelectric point lower than physiological pH and an anionic carrier molecule. The formulations of the invention are suitable as depot formulations for the sustained release of therapeutic polypeptides.
摘要翻译：本发明提供了包含具有低于生理pH的等电点的多肽的固体离子络合物和阴离子载体分子的药物制剂。本发明的制剂适合用作持续释放治疗性多肽的贮库制剂。

13. 发明申请

WO2007022254A2 PHARMACEUTICAL FORMULATIONS FOR SUSTAINED DRUG DELIVERY 审中-公开
标题翻译：用于持续输送药物的药物制剂
公开(公告)号：WO2007022254A2
公开(公告)日：2007-02-22
申请号：PCT/US2006/031967
申请日：2006-08-15
申请人： PRAECIS PHARMACEUTICALS, INC. , GEFTER, Malcolm, L. , BARKER, Nicholas , MUSSO, Gary, F. , MOLINEAUX, Christopher, J.
发明人： GEFTER, Malcolm, L. , BARKER, Nicholas , MUSSO, Gary, F. , MOLINEAUX, Christopher, J.
IPC分类号： A61K47/48
CPC分类号： A61K38/09 , A61K47/61
摘要： Sustained delivery formulations comprising a water-insoluble complex of a peptidic compound (e.g., a peptide, polypeptide, protein, peptidomimetic or the like) and a carrier macromolecule are disclosed. The formulations of the invention allow for loading of high concentrations of peptidic compound in a small volume and for delivery of a pharmaceutically active peptidic compound for prolonged periods, e.g. , one month, after administration of the complex. The complexes of the invention can be milled or crushed to a fine powder. In powdered form, the complexes form stable aqueous suspensions and dispersions, suitable for injection. In a preferred embodiment, the peptidic compound of the complex is an LHRH analogue, preferably an LHRH antagonist, and the carrier macromolecule is an anionic polymer, preferably carboxymethylcellulose. Methods of making the complexes of the invention, and methods of using LHRH-analogue-containing complexes to treat conditions treatable with an LHRH analogue, are also disclosed.
摘要翻译：公开了包含肽化合物（例如肽，多肽，蛋白质，拟肽等）和载体大分子的水不溶性络合物的持续递送制剂。本发明的制剂允许以小体积装载高浓度的肽化合物并延长药物活性的肽化合物，例如用于递送。，一个月后，复杂的管理。本发明的络合物可以研磨或粉碎成细粉末。以粉末形式，络合物形成稳定的水性悬浮液和分散体，适于注射。在优选的实施方案中，复合物的肽化合物是LHRH类似物，优选LHRH拮抗剂，载体大分子是阴离子聚合物，优选羧甲基纤维素。还公开了制备本发明复合物的方法，以及使用含LHRH类似物的复合物治疗可用LHRH类似物治疗的病症的方法。

14. 发明申请

WO2007021970A2 STABLE PHARMACEUTICAL FORMULATIONS AND METHODS OF USE THEREOF 审中-公开
标题翻译：稳定的药物制剂及其使用方法
公开(公告)号：WO2007021970A2
公开(公告)日：2007-02-22
申请号：PCT/US2006/031439
申请日：2006-08-14
申请人： PRAECIS PHARMACEUTICALS, INC. , TAN, Heow, Meng , YE, Ming , MCGRATH, Thomas, F. , JOHNSTON, Kevin, A. , MICALIZZI, Maria , MCKENNA, Patrick , REDMON, Martin, Patrick , VUPPALA, Murali, K. , MUSSO, Gary, F.
发明人： TAN, Heow, Meng , YE, Ming , MCGRATH, Thomas, F. , JOHNSTON, Kevin, A. , MICALIZZI, Maria , MCKENNA, Patrick , REDMON, Martin, Patrick , VUPPALA, Murali, K. , MUSSO, Gary, F.
IPC分类号： A61K47/48
CPC分类号： A61K31/485 , A61K45/06 , A61K47/61 , A61K2300/00
摘要： The present invention provides pharmaceutical formulations characterized by improved stability of the pharmaceutically active compounds contained therein, methods for preparing the same, and methods of use thereof. The pharmaceutical compositions of the present invention comprise a stable water-insoluble complex of a pharmaceutically active compound and a carrier macromolecule. The advantages of the pharmaceutical compositions of the invention include, for example, the increased stability of a pharmaceutically active compound contained therein.
摘要翻译：本发明提供药物制剂，其特征在于其中所含的药物活性化合物的稳定性提高，其制备方法及其使用方法。本发明的药物组合物包含药物活性化合物和载体大分子的稳定的水不溶性复合物。本发明的药物组合物的优点包括例如其中所含的药物活性化合物的稳定性增加。

15. 发明申请

WO2006020951A1 METHODS AND COMPOSITIONS FOR MODULATING SPHINGOSINE-1-PHOSPHATE (S1P) RECEPTOR ACTIVITY 审中-公开
标题翻译：调节磷脂酸1-磷酸（S1P）受体活性的方法和组合物
公开(公告)号：WO2006020951A1
公开(公告)日：2006-02-23
申请号：PCT/US2005/028914
申请日：2005-08-12
申请人： PRAECIS PHARMACEUTICALS, INC. , SAHA, Ashis, K. , KAVARANA, Malcolm, J. , EVINDAR, Ghotas , SATZ, Alexander, L. , MORGAN, Barry
发明人： SAHA, Ashis, K. , KAVARANA, Malcolm, J. , EVINDAR, Ghotas , SATZ, Alexander, L. , MORGAN, Barry
IPC分类号： C07C237/04
CPC分类号： C07D213/30 , C07C237/04 , C07C237/06 , C07C237/08 , C07C237/16 , C07C237/42 , C07C317/40 , C07C323/41 , C07C2601/14 , C07D207/12 , C07D209/82 , C07D209/88 , C07D231/10 , C07D231/12 , C07D233/54 , C07D233/64 , C07D277/20 , C07D277/28 , C07D317/58 , C07D317/64 , C07D333/06 , C07D333/16 , C07D417/10 , C07D493/04 , C07F9/091 , C07F9/3808 , C07F9/5728 , C07F9/65033 , C07F9/65037 , C07F9/65062 , C07F9/6539 , C07F9/65517 , C07F9/655345 , C07F9/65586 , C07F9/65742
摘要： The present invention relates to compounds which modulate the activity of the SI P1 receptor, the use of these compounds for treating conditions associated with signaling through the S1 P1 receptor, and pharmaceutical compositions comprising these compounds.
摘要翻译：本发明涉及调节SI P1受体活性的化合物，这些化合物用于治疗通过S1P1受体与信号传导相关的病症的用途，以及包含这些化合物的药物组合物。

16. 发明申请

WO2005058479A2 METHODS FOR SYNTHESIS OF ENCODED LIBRARIES 审中-公开
标题翻译：合成编码文库的方法
公开(公告)号：WO2005058479A2
公开(公告)日：2005-06-30
申请号：PCT/US2004/042964
申请日：2004-12-17
申请人： PRAECIS PHARMACEUTICALS, INC. , MORGAN, Barry , HALE, Stephen , ARICO-MUENDEL, Christopher, C. , CLARK, Mathew , WAGNER, Richard , ISRAEL, Davide, I. , GEFTER, Malcolm, L. , BENJAMIN, Dennis , HANSEN, Nils, Jacob, Vest , KAVARNA, Malcolm, J. , CREASER, Steffan, Phillip , FRANKLIN, George, J. , CLARK, Mathew, A. , CENTRELLA, Paolo, A. , ACHARYA, Raksha, A.
发明人： MORGAN, Barry , HALE, Stephen , ARICO-MUENDEL, Christopher, C. , CLARK, Mathew , WAGNER, Richard , ISRAEL, Davide, I. , GEFTER, Malcolm, L. , BENJAMIN, Dennis , HANSEN, Nils, Jacob, Vest , KAVARNA, Malcolm, J. , CREASER, Steffan, Phillip , FRANKLIN, George, J. , CLARK, Mathew, A. , CENTRELLA, Paolo, A. , ACHARYA, Raksha, A.
IPC分类号： B01J19/00
CPC分类号： C07H21/00 , C12N15/1068 , C40B50/10
摘要： The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.
摘要翻译：本发明提供了合成包含编码寡核苷酸标签的分子文库的方法。

17. 发明申请

WO2004092728A2 METHODS OF MEASURING THE ABILITY OF A TEST COMPOUND TO INACTIVATE A BIOLOGICAL TARGET IN CELLS OF A SUBJECT 审中-公开
标题翻译：测试化合物能够使主体细胞中的生物学目标失活的方法
公开(公告)号：WO2004092728A2
公开(公告)日：2004-10-28
申请号：PCT/US2004/010941
申请日：2004-04-07
申请人： PRAECIS PHARMACEUTICALS, INC. , BENJAMIN, Dennis , THOMPSON, Charles , WANG, Bryan , WAKEFIELD, James , GEFTER, Malcolm, L.
发明人： BENJAMIN, Dennis , THOMPSON, Charles , WANG, Bryan , WAKEFIELD, James , GEFTER, Malcolm, L. , ARICO-MUENDEL, Christopher, C.
IPC分类号： G01N33/53
CPC分类号： G01N33/573 , G01N33/5032 , G01N33/57496
摘要： The present invention provides a method of assessing the ability of a compound (the "test compound") which is an inhibitor of a biological target to inhibit the biological target in a biological compartment of interest when administered to a subject in vivo .
摘要翻译：本发明提供了当在体内施用于受试者时，评估作为生物靶标抑制剂的化合物（“测试化合物”）在感兴趣的生物区室中抑制生物靶标的能力的方法。

18. 发明申请

WO2003105677A3 METHODS FOR TREATING VIRAL DISEASES USING MODULATORS OF AMYLOIDOGENIC PEPTIDE AGGREGATION 审中-公开
公开(公告)号：WO2003105677A3
公开(公告)日：2003-12-24
申请号：PCT/US2003/019365
申请日：2003-06-18
申请人： PRAECIS PHARMACEUTICALS, INC. , ISRAEL, David, I. , MIRZABEKOV, Tajib , WOJTOWICZ, Woj, M. , SODROSKI, Joseph
发明人： ISRAEL, David, I. , MIRZABEKOV, Tajib , WOJTOWICZ, Woj, M. , SODROSKI, Joseph
IPC分类号： C12Q1/00
摘要： The present invention provides methods and compositions for modulating infection of a cell by a virus and methods and compositions for treating a viral disease, e.g., a viral disease of the brain, in a subject. Figure (1) is a graph demonstrating that AB stimulates infection by recombinant HIV-1 viruses.

19. 发明申请

WO2003077931A1 TRANSCRIPTION FACTOR MODULATORS AND USES THEREOF 审中-公开
标题翻译：转录因子调节器及其用途
公开(公告)号：WO2003077931A1
公开(公告)日：2003-09-25
申请号：PCT/US2003/008196
申请日：2003-03-17
申请人： PRAECIS PHARMACEUTICALS, INC. , JOYAL, John, L. , FINDEIS, Mark, A. , KAVARANA, Malcolm , MORGAN, Barry , GEFTER, Malcolm, L.
发明人： JOYAL, John, L. , FINDEIS, Mark, A. , KAVARANA, Malcolm , MORGAN, Barry , GEFTER, Malcolm, L.
IPC分类号： A61K31/70
CPC分类号： C07K14/4702
摘要： The present invention provides transcription factor modulators useful for modulating gene expression in a cell, as well as pharmaceutical compositions containing these transcription factor modulators. The present invention also provides methods for modulating gene transcription in a cell and methods of treating a subject suffering from a transcription factor-associated disorder, such as cancer, inflammatory disorders or autoimmune disorders.
摘要翻译：本发明提供了可用于调节细胞中基因表达的转录因子调节剂，以及含有这些转录因子调节剂的药物组合物。本发明还提供了调节细胞中基因转录的方法以及治疗患有转录因子相关疾病如癌症，炎症性疾病或自身免疫性疾病的受试者的方法。

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