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1. 发明申请

WO2008016547A2 AURORA KINASE INHIBITORS FROM AN ENCODED SMALL MOLECULE LIBRARY 审中-公开
标题翻译： AURORA激酶抑制剂从一个编码的小分子库
公开(公告)号：WO2008016547A2
公开(公告)日：2008-02-07
申请号：PCT/US2007016894
申请日：2007-07-27
申请人： PRAECIS PHARM INC , CLARK MATTHEW
发明人： CLARK MATTHEW
IPC分类号： C07D251/54 , A61K31/53 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , C07D251/54 , C07D401/12
摘要： The present invention provides, at least in part, compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein Z 1, Z 2 , Z 3 , R 1 , x, y, R 2 , R 3 , R 4a , R 4b , R 5 , R 6 and R 7 are described herein, as well as methods for their identification, their preparation, pharmaceutical compositions containing them, and their use as Aurora A kinase inhibitors in treatment, e.g., of cancer and other proliferative disorders.
摘要翻译：本发明至少部分提供式I化合物或其药学上可接受的盐，其中Z 1，Z 2，Z 3， R 1，R 1，R 2，R 3，R 4，R 4，R 4，R 4，R 4，本文描述了本发明的化合物以及它们的鉴定方法，其制备方法，，含有它们的药物组合物，以及它们在治疗（例如癌症和其他增殖性疾病）中作为Aurora A激酶抑制剂的用途。

2. 发明申请

WO02074247A8 PHARMACEUTICAL FORMULATIONS FOR SUSTAINED RELEASE 审中-公开
标题翻译：用于持续发布的药物制剂
公开(公告)号：WO02074247A8
公开(公告)日：2003-01-03
申请号：PCT/US0208453
申请日：2002-03-19
申请人： PRAECIS PHARM INC , BARKER NICHOLAS , WOLFE JANET L
发明人： BARKER NICHOLAS , WOLFE JANET L
IPC分类号： A61K47/48 , A61K9/08 , A61K38/00 , A61K38/02 , A61K47/36 , A61K47/38 , A61K47/42 , A01N25/00 , A61K9/14 , A61K47/00 , A61K47/30 , A61K47/32 , A61K47/34
CPC分类号： A61K38/02 , A61K47/61
摘要： Sustained delivery pharmaceutical compositions comprising a solid ionic complex of a pharmaceutically active compound and an ionic macromolecule are provided by the present invention. The pharmaceutical compositions of the invention allow for loading of high concentrations of pharmaceutically active compounds and for delivery of a pharmaceutically active compound for prolonged periods of time, e.g. , one month, after administration. Methods for preparing these pharmaceutical compositions, as well as methods of using them to treat a subject are also provided.
摘要翻译：包含药物活性化合物和离子高分子的固体离子络合物的持续递送药物组合物由本发明提供。本发明的药物组合物允许加载高浓度的药学活性化合物和用于递送药物活性化合物延长的时间，例如在给药后一个月。还提供了制备这些药物组合物的方法，以及使用它们治疗受试者的方法。

3. 发明申请

WO02074247A2 PHARMACEUTICAL FORMULATIONS FOR SUSTAINED RELEASE 审中-公开
标题翻译：用于持续发布的药物制剂
公开(公告)号：WO02074247A2
公开(公告)日：2002-09-26
申请号：PCT/US0208453
申请日：2002-03-19
申请人： PRAECIS PHARM INC , BARKER NICHOLAS , WOLFE JANET L
发明人： BARKER NICHOLAS , WOLFE JANET L
IPC分类号： A61K47/48 , A61K9/08 , A61K38/00 , A61K38/02 , A61K47/36 , A61K47/38 , A61K47/42 , A61K
CPC分类号： A61K38/02 , A61K47/61
摘要： Sustained delivery pharmaceutical compositions comprising a solid ionic complex of a pharmaceutically active compound and an ionic macromolecule are provided by the present invention. The pharmaceutical compositions of the invention allow for loading of high concentrations of pharmaceutically active compounds and for delivery of a pharmaceutically active compound for prolonged periods of time, e.g. , one month, after administration. Methods for preparing these pharmaceutical compositions, as well as methods of using them to treat a subject are also provided.
摘要翻译：包含药物活性化合物和离子高分子的固体离子络合物的持续递送药物组合物由本发明提供。本发明的药物组合物允许加载高浓度的药学活性化合物和用于递送药物活性化合物延长的时间，例如在给药后一个月。还提供了制备这些药物组合物的方法，以及使用它们治疗受试者的方法。

4. 发明申请

WO9825642A2 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：WO9825642A2
公开(公告)日：1998-06-18
申请号：PCT/US9722881
申请日：1997-12-11
申请人： PRAECIS PHARM INC , GEFTER MALCOLM L , BARKER NICHOLAS , MUSSO GARY , MOLINEAUX CHRISTOPHER J
发明人： GEFTER MALCOLM L , BARKER NICHOLAS , MUSSO GARY , MOLINEAUX CHRISTOPHER J
IPC分类号： A61K47/30 , A61K9/22 , A61K38/04 , A61K38/09 , A61K38/22 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/48 , A61P15/00 , A61P15/18 , A61P35/00 , A61K38/00
CPC分类号： B82Y5/00 , A61K38/09 , A61K47/61 , A61K47/6949 , Y10S514/80
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。本发明的制剂允许在施用复合物之后将较高体积的肽化合物加载至少量的药物活性肽化合物延长的时期，例如一个月。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。

5. 发明申请

WO9821237A2 PEPTIDE COMPOUNDS USEFUL FOR MODULATING FGF RECEPTOR ACTIVITY 审中-公开
标题翻译：用于调节FGF受体活性的肽类化合物
公开(公告)号：WO9821237A2
公开(公告)日：1998-05-22
申请号：PCT/US9721070
申请日：1997-11-12
申请人： PRAECIS PHARM INC , BENJAMIN HOWARD , CHAI LING , FINDEIS MARK A , GOODWIN WILLIAM , HUNDAL ARVIND , ISRAEL DAVID I , KELLEY MICHAEL , KEOUGH MARTIN P , LU KUANGHUI , NATOLI FARAH , PETICOLAS ALICIA , SIGNER ETHAN R , GEFTER MALCOLM L
发明人： BENJAMIN HOWARD , CHAI LING , FINDEIS MARK A , GOODWIN WILLIAM , HUNDAL ARVIND , ISRAEL DAVID I , KELLEY MICHAEL , KEOUGH MARTIN P , LU KUANGHUI , NATOLI FARAH , PETICOLAS ALICIA , SIGNER ETHAN R , GEFTER MALCOLM L
IPC分类号： A61K38/00 , A61P1/18 , A61P3/10 , A61P9/00 , A61P13/08 , A61P15/08 , A61P17/02 , A61P17/06 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07K7/06 , C07K14/50 , A61K38/18
CPC分类号： C07K7/06 , A61K38/00 , C07K14/50
摘要： This invention provides peptide compounds that bind to either of fibroblast growth factor (FGF) or a fibroblast growth factor receptor (FGFR) and, accordingly, are useful for modulating FGFR activity. Preferably, the FGFR is FGFR2-IIIC. Preferably, the FGF is basic FGF. Preferably the peptide compound comprises an amino acid sequence (Y/F)-(L/F/I)-(R/D/E/S/Y/G)-(Q/L/Y)-Y-(M/L/K/R)-(L/M/D/E/N/S)-(R/L/S/T)-(L/F/M/V) (SEQ ID NO:1). The invention further comprises pharmaceutical compositions comprising the peptide compounds of the invention and a pharmaceutically acceptable carrier. The invention still further provides methods of modulating FGFR activity using the peptide compounds of the invention.
摘要翻译：本发明提供了结合成纤维细胞生长因子（FGF）或成纤维细胞生长因子受体（FGFR）之一的肽化合物，因此可用于调节FGFR活性。优选地，FGFR是FGFR2-IIIC。优选地，FGF是碱性FGF。优选地，肽化合物包含氨基酸序列（Y / F） - （L / F / I） - （R / D / E / S / Y / G） - （Q / L / Y）-Y-（M / （L / K / R） - （L / M / D / E / N / S） - （R / L / S / T） - （L / F / M / V）（SEQ ID NO：1）。本发明还包括包含本发明的肽化合物和药学上可接受的载体的药物组合物。本发明还提供使用本发明的肽化合物调节FGFR活性的方法。

6. 发明申请

WO2007022254A3 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：WO2007022254A3
公开(公告)日：2008-10-23
申请号：PCT/US2006031967
申请日：2006-08-15
申请人： PRAECIS PHARM 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。

7. 发明申请

WO2008016692A3 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO2008016692A3
公开(公告)日：2008-03-20
申请号：PCT/US2007017282
申请日：2007-08-01
申请人： PRAECIS PHARM INC , EVINDAR GHOTAS , DENG HONGFENG , BERNIER SYLVIE , YAO GANG , COFFIN AARON , YANG HONGFANG
发明人： EVINDAR GHOTAS , DENG HONGFENG , BERNIER SYLVIE , YAO GANG , COFFIN AARON , YANG HONGFANG
IPC分类号： C07D213/38 , A61K31/425 , A61K31/433 , A61K31/44 , A61K31/505 , A61P37/00 , C07D261/08 , C07D271/10 , C07D277/28 , C07D285/12 , C07D417/12 , C07F9/6539
CPC分类号： C07D277/28 , C07D213/38 , C07D261/08 , C07D271/10 , C07D285/12 , C07D417/12 , C07F9/582 , C07F9/65033 , C07F9/65122 , C07F9/653 , C07F9/65312 , C07F9/65318 , C07F9/6539 , C07F9/65395
摘要： The invention provides compounds formula I, their preparation, and their use as pharmaceutically active immunosuppressive agents for the treatment of autoimmune disorders, organ transplant rejection, disorders associated with an activated immune system, as well as other disorders modulated by lymphopenia or SlP receptors.
摘要翻译：本发明提供式I化合物及其制备方法及其作为药物活性免疫抑制剂用于治疗自身免疫疾病，器官移植排斥，与活化的免疫系统相关的病症以及由淋巴细胞减少或S1P受体调节的其它病症的用途。

8. 发明申请

WO2007124005A3 METHODS FOR TREATING BONE ASSOCIATED DISEASES BY THE USE OF METHIONINE AMINOPEPTIDASE-2 INHIBITORS 审中-公开
标题翻译：通过使用甲氨酸氨基转移酶-2抑制剂治疗骨相关疾病的方法
公开(公告)号：WO2007124005A3
公开(公告)日：2008-01-03
申请号：PCT/US2007009582
申请日：2007-04-18
申请人： PRAECIS PHARM INC , HANNING GERHARD , WESTLIN WILLIAM F
发明人： HANNING GERHARD , WESTLIN WILLIAM F
IPC分类号： A61K31/336 , A61P3/14
CPC分类号： A61K31/336
摘要： The instant invention provides the use of METAP-2 inhibitors to manufacture pharmaceutical compositions for treating a subject suffering from bone associated diseases, such as osteoporosis.
摘要翻译：本发明提供了使用METAP-2抑制剂来制备用于治疗患有骨相关疾病如骨质疏松症的受试者的药物组合物。

9. 发明申请

WO0242462A3 THERAPEUTIC AGENTS AND METHODS OF USE THEREOF FOR TREATING AN AMYLOIDOGENIC DISEASE 审中-公开
标题翻译：治疗药物及其用于治疗淀粉样变性疾病的方法
公开(公告)号：WO0242462A3
公开(公告)日：2003-06-19
申请号：PCT/US0144581
申请日：2001-11-27
申请人： PRAECIS PHARM INC
发明人： GEFTER MALCOLM L , ISRAEL DAVID I , JOYAL JOHN L , GOSSELIN MICHAEL
IPC分类号： C12N15/09 , A61K38/00 , A61K45/00 , A61K47/48 , A61P25/28 , C07K5/103 , C07K7/06 , C07K14/47 , C07K16/00 , C07K16/18 , C07K19/00 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/12 , C12N15/13 , C12P21/02 , A61K38/17 , C07K14/00 , C12N15/62 , C12N15/85
CPC分类号： C07K14/4711 , A61K38/00 , A61K47/6811 , A61K47/6835 , C07K16/00 , C07K2319/00 , C07K2319/30
摘要： The present invention provides therapeutic agents suitable for treating an amyloidogenic disorder, as well as pharmaceutical compositions comprising the therapeutic agents and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an amyloidogenic disorder, e.g., Alzheimer's disease, in a subject by administering to the subject a therapeutically effective amount of one or more of the compounds of the invention.
摘要翻译：本发明提供了适合于治疗淀粉样变性疾病的治疗剂，以及包含治疗剂和药学上可接受的载体的药物组合物。本发明还提供了通过向受试者施用治疗有效量的一种或多种本发明化合物来治疗受试者中淀粉样变性疾病例如阿尔茨海默氏病的方法。

10. 发明申请

WO0183554A3 ANTI-INFLAMMATORY COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：抗炎化合物及其用途
公开(公告)号：WO0183554A3
公开(公告)日：2002-08-01
申请号：PCT/US0114346
申请日：2001-05-02
申请人： PRAECIS PHARM INC , UNIV YALE , MAY MICHAEL J , GHOSH SANKAR , FINDEIS MARK A , PHILLIPS KATHRYN
发明人： MAY MICHAEL J , GHOSH SANKAR , FINDEIS MARK A , PHILLIPS KATHRYN
IPC分类号： A61K38/00 , A61P1/04 , A61P7/02 , A61P9/10 , A61P9/14 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/06 , A61P31/08 , A61P31/12 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07K7/06 , C07K7/08 , C07K14/47 , C12N9/12 , C12N15/09 , C12Q1/02 , C07K14/08 , A61K38/10 , A61K38/43
CPC分类号： C07K14/4703 , A61K38/00 , C07K14/4747 , C12N9/1205
摘要： The present invention provides anti-inflammatory compounds, pharmaceutical compositions thereof, and methods of use thereof for treating inflammatory disorders. The present invention also provides methods of identifying anti-inflammatory compounds and methods of inhibiting NF- kappa B-dependent target gene expression in a cell.
摘要翻译：本发明提供抗炎化合物，其药物组合物及其用于治疗炎症性疾病的方法。本发明还提供鉴定抗炎化合物的方法和抑制细胞中NF-κB依赖性靶基因表达的方法。

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