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1. 发明申请

WO2006135786A3 METHODS FOR SYNTHESIS OF ENCODED LIBRARIES 审中-公开
标题翻译：编码图书馆的合成方法
公开(公告)号：WO2006135786A3
公开(公告)日：2007-06-21
申请号：PCT/US2006022555
申请日：2006-06-09
申请人： PRAECIS PHARM INC , MORGAN BARRY , HALE STEPHEN , ARICO-MUENDEL CHRISTOPHER C , CLARK MATTHEW , WAGNER RICHARD , KAVARANA MALCOLM J , CREASER STEFFEN PHILLIP , FRANKLIN GEORGE J , CENTRELLA PAOLO A , ISRAEL DAVID I , GEFTER MALCOLM L , BENJAMIN DENNIS , HANSEN NILS JAKOB VEST , ACHARYA RAKSHA A
发明人： MORGAN BARRY , HALE STEPHEN , ARICO-MUENDEL CHRISTOPHER C , CLARK MATTHEW , WAGNER RICHARD , KAVARANA MALCOLM J , CREASER STEFFEN PHILLIP , FRANKLIN GEORGE J , CENTRELLA PAOLO A , ISRAEL DAVID I , GEFTER MALCOLM L , BENJAMIN DENNIS , HANSEN NILS JAKOB VEST , ACHARYA RAKSHA A
IPC分类号： C12N15/10 , C07B61/00 , C07H21/00
CPC分类号： C07H21/00 , C12N15/1068
摘要： The present invention provides a method of synthesizing libraries of molecules which include an encoding oligonucleotide tag.
摘要翻译：本发明提供合成包含编码寡核苷酸标签的分子文库的方法。

2. 发明申请

WO2007053358A3 METHODS FOR IDENTIFYING COMPOUNDS OF INTEREST USING ENCODED LIBRARIES 审中-公开
标题翻译：使用编码的图书馆识别兴趣化合物的方法
公开(公告)号：WO2007053358A3
公开(公告)日：2007-11-01
申请号：PCT/US2006041356
申请日：2006-10-23
申请人： PRAECIS PHARM INC , MORGAN BARRY , HALE STEPHEN , ARICO-MUENDEL CHRISTOPHER C , CLARK MATTHEW , WAGNER RICHARD , ISRAEL DAVID I , GEFTER MALCOLM L , KAVARANA MALCOLM J , CREASER STEFFEN PHILLIP , FRANKLIN GEORGE J , CENTRELLA PAULO A , ACHARYA RAKSHA A , BENJAMIN DENNIS , HANSEN NILS JAKOB VEST
发明人： MORGAN BARRY , HALE STEPHEN , ARICO-MUENDEL CHRISTOPHER C , CLARK MATTHEW , WAGNER RICHARD , ISRAEL DAVID I , GEFTER MALCOLM L , KAVARANA MALCOLM J , CREASER STEFFEN PHILLIP , FRANKLIN GEORGE J , CENTRELLA PAULO A , ACHARYA RAKSHA A , BENJAMIN DENNIS , HANSEN NILS JAKOB VEST
IPC分类号： C07B61/00 , C12N15/10
CPC分类号： C12N15/1068 , C07H21/00
摘要： The present invention provides a method for identifying a compound of interest by screening libraries of molecules which include an encoding oligonucleotide tag.
摘要翻译：本发明提供了通过筛选包括编码寡核苷酸标签的分子文库来鉴定感兴趣的化合物的方法。

3. 发明申请

WO2005058479A3 METHODS FOR SYNTHESIS OF ENCODED LIBRARIES 审中-公开
标题翻译：编码图书馆的合成方法
公开(公告)号：WO2005058479A3
公开(公告)日：2005-10-13
申请号：PCT/US2004042964
申请日：2004-12-17
申请人： PRAECIS PHARM 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： C07B61/00 , C07H21/00 , C07H21/04 , C07K1/00 , C12N15/10 , C12P19/34 , C12Q1/68 , A61K38/00
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：本发明提供合成包含编码寡核苷酸标签的分子文库的方法。

4. 发明申请

WO2004092728A3 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：WO2004092728A3
公开(公告)日：2005-06-02
申请号：PCT/US2004010941
申请日：2004-04-07
申请人： PRAECIS PHARM INC , BENJAMIN DENNIS , THOMPSON CHARLES , WANG BRYAN , WAKEFIELD JAMES , GEFTER MALCOLM L , ARICO-MUENDEL CHRISTOPHER C
发明人： BENJAMIN DENNIS , THOMPSON CHARLES , WANG BRYAN , WAKEFIELD JAMES , GEFTER MALCOLM L , ARICO-MUENDEL CHRISTOPHER C
IPC分类号： C12Q1/37 , G01N33/50 , G01N33/53 , G01N33/567 , G01N33/573 , G01N33/574
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。

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

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。

8. 发明申请

WO0222154A3 PHARMACEUTICAL COMPOSITIONS FOR SUSTAINED DRUG DELIVERY 审中-公开
标题翻译：用于持续输送药物的药物组合物
公开(公告)号：WO0222154A3
公开(公告)日：2003-03-13
申请号：PCT/US0128691
申请日：2001-09-13
申请人： PRAECIS PHARM INC
发明人： GEFTER MALCOLM L
IPC分类号： A61K47/48 , A61K38/00 , A61K38/04 , A61K38/09 , A61K38/11 , A61K38/18 , A61K38/22 , A61K38/26 , A61K38/27 , A61K38/28 , A61K38/29 , A61K38/31 , A61K38/33 , A61K47/30 , A61K47/32 , A61K47/34 , A61K47/38 , A61P5/00 , A61P5/02
CPC分类号： A61K38/27 , A61K38/09 , A61K47/58 , A61K47/59 , A61K47/61 , A61K47/64 , A61K47/645
摘要： Sustained delivery formulations comprisinmg a water-insoluble complex of a peptide and a plurality of ligands are disclosed. The formulations of the invention allow for loading of high concentrations of peptide in a small volume and for delivery of a pharmaceutically active peptide 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. Methods of making the complexes of the invention, and methods of these complexes are also disclosed.
摘要翻译：公开了含有肽和多种配体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以较小的体积装载高浓度的肽并延长药物活性肽的递送时间，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。还公开了制备本发明配合物的方法，以及这些络合物的方法。

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. 发明公开

EP1373496A4 METHODS FOR IDENTIFYING PEPTIDES WHICH MODULATE A BIOLOGICAL PROCESS 审中-公开
标题翻译：一种用于识别的生物过程控制调节肽
公开(公告)号：EP1373496A4
公开(公告)日：2004-10-27
申请号：EP02719077
申请日：2002-02-22
申请人： PRAECIS PHARM INC
发明人： GEFTER MALCOLM L
IPC分类号： G01N33/50 , A61K38/00 , A61P31/18 , A61P35/00 , C07K14/47 , C12N1/21 , C12N15/00 , C12N15/10 , C12Q1/02 , G01N33/15 , G01N33/68 , C07K5/00 , C07K14/00 , C12N15/85 , C12N15/86 , C12P21/06 , C12Q1/68
CPC分类号： C12N15/1086 , A61K38/00 , C12N15/1079

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