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1. 发明申请

WO0242295A3 PEPTIDES AS MET-AP2 INHIBITORS 审中-公开
标题翻译：作为MET-AP2抑制剂的肽
公开(公告)号：WO0242295A3
公开(公告)日：2003-02-20
申请号：PCT/US0146086
申请日：2001-11-01
申请人： PRAECIS PHARM INC , OLSON GARY L , SELF CHRISTOPHER , LEE LILY , COOK CHARLES MICHAEL , BIRKTOFT JENS , MORGAN BARRY , ARICO-MUENDEL CHRISTOPHER C
发明人： OLSON GARY L , SELF CHRISTOPHER , LEE LILY , COOK CHARLES MICHAEL , BIRKTOFT JENS , MORGAN BARRY , ARICO-MUENDEL CHRISTOPHER C
IPC分类号： C07D303/22 , A61K31/336 , A61K38/00 , A61K38/48 , A61K47/48 , A61P9/00 , A61P19/02 , A61P35/00 , A61P37/00 , A61P37/02 , C07D405/14 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/09 , C07K5/103 , C07K14/00 , C07K14/81 , C07D303/16 , A61K31/335
CPC分类号： A61K38/4886 , A61K47/64 , C07D405/14 , C07K5/0202 , C07K5/0606 , C07K5/0806 , C07K5/081 , C07K5/0817 , C07K5/1008 , C07K14/8146
摘要： The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis of the invention.
摘要翻译：本发明提供包含与肽偶联的MetAP-2抑制性核心的血管生成抑制剂化合物，以及包含血管生成抑制剂化合物和药学上可接受的载体的药物组合物。本发明还提供了通过向受试者施用治疗有效量的本发明血管生成中的一种或多种来治疗受试者中血管生成疾病例如癌症的方法。

2. 发明申请

WO2008011114A3 METHIONINE AMINOPEPTIDASE-2 INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：蛋氨酸氨肽酶-2抑制剂及其使用方法
公开(公告)号：WO2008011114A3
公开(公告)日：2008-11-27
申请号：PCT/US2007016392
申请日：2007-07-19
申请人： PRAECIS PHARM INC , OLSON GARY L , SELF CHRISTOPHER , LEE LILY , COOK CHARLES M , BIRKTOFT JENS , MORGAN BARRY , ARICO-MUENDEL CHRISTOPHER C , LORUSSO JEANINE
发明人： OLSON GARY L , SELF CHRISTOPHER , LEE LILY , COOK CHARLES M , BIRKTOFT JENS , MORGAN BARRY , ARICO-MUENDEL CHRISTOPHER C , LORUSSO JEANINE
IPC分类号： A61K47/48 , A61P37/06
CPC分类号： A61K38/05 , A61K38/07 , A61K38/08 , A61K47/542 , A61K47/65 , C07K5/06078 , C07K5/1008 , C07K5/1024 , C07K7/06
摘要： The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of inducing an immunosupressed condition and/or treating chronic allograft vasculopathy in a subject undergoing or who has undergone a transplant, by administering to the subject a therapeutically effective amount of one or more of the compounds of the invention.
摘要翻译：本发明提供了包含与肽偶联的MetAP-2抑制性核心的血管生成抑制剂化合物，以及包含血管生成抑制剂化合物和药学上可接受的载体的药物组合物。本发明还提供了通过给受试者施用治疗有效量的一种或多种本发明化合物来诱导接受移植或已接受移植的受试者的免疫抑制状态和/或治疗慢性同种异体移植血管病的方法。

3. 发明申请

WO03092608A3 METHIONINE AMINOPEPTIDASE-2 INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：甲氨酸氨基转移酶-2抑制剂及其使用方法
公开(公告)号：WO03092608A3
公开(公告)日：2004-01-15
申请号：PCT/US0313623
申请日：2003-05-02
申请人： PRAECIS PHARM INC , OLSON GARY L , SELF CHRISTOPHER , LEE LILY , COOK CHARLES MICHAEL , BIRKTOPF JENS , MORGAN BARRY , ARICO-MUENDEL CHRISTOPHER C
发明人： OLSON GARY L , SELF CHRISTOPHER , LEE LILY , COOK CHARLES MICHAEL , BIRKTOPF JENS , MORGAN BARRY , ARICO-MUENDEL CHRISTOPHER C
IPC分类号： C12N9/99 , A61K31/336 , A61K38/00 , A61K38/48 , A61K47/48 , A61P1/04 , A61P3/10 , A61P9/10 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/04 , A61P33/06 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P37/06 , A61P43/00 , C07D303/16 , C07D303/24 , C07D405/14 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/09 , C07K5/10 , C07K5/103 , C07K7/06 , C07K14/81 , A61K38/02 , A61K38/07 , A61K38/08 , C07D303/02 , C07K2/00
CPC分类号： C07D405/14 , A61K38/4886 , A61K47/64 , C07D303/16 , C07K5/0202 , C07K5/0606 , C07K5/0806 , C07K5/081 , C07K5/0817 , C07K5/1008 , C07K5/1024 , C07K7/06 , C07K14/8146
摘要： The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.
摘要翻译：本发明提供包含与肽偶联的MetAP-2抑制性核心的血管生成抑制剂化合物，以及包含血管生成抑制剂化合物和药学上可接受的载体的药物组合物。本发明还提供了通过向受试者施用治疗有效量的一种或多种本发明的血管发生抑制剂化合物来治疗受试者中血管生成疾病例如癌症的方法。

4. 发明申请

WO0052048A9 MODULATORS OF BETA-AMYLOID PEPTIDE AGGREGATION COMPRISING D-AMINO ACIDS 审中-公开
标题翻译：包含D-氨基酸的β-淀粉样蛋白聚集的调节剂
公开(公告)号：WO0052048A9
公开(公告)日：2002-04-11
申请号：PCT/US0005574
申请日：2000-03-03
申请人： PRAECIS PHARM INC
发明人： FINDEIS MARK A , PHILLIPS KATHRYN , OLSON GARY L , SELF CHRISTOPHER
IPC分类号： G01N33/68 , A61K38/00 , A61K38/17 , A61P25/28 , A61P43/00 , C07K5/083 , C07K7/06 , C07K14/47
CPC分类号： C07K14/4711 , A61K38/00
摘要： Compounds that modulate natural beta amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a beta amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a beta amyloid peptide, preferably a retro-inverso isomer of A beta 17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an acetate group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
摘要翻译：提供调节天然β淀粉样肽聚集的化合物。本发明的调节剂包含优选基于β-淀粉样肽的肽，其完全由D-氨基酸组成。优选地，肽包含3-5个D-氨基酸残基，并且包括独立地选自D-亮氨酸，D-苯丙氨酸和D-缬氨酸的至少两个D-氨基酸残基。在特别优选的实施方案中，肽是β淀粉样蛋白肽的逆反异构体，优选Aβ17-21的逆反式异构体。在某些实施方案中，肽在氨基末端，羧基末端或两者都被修饰。优选的氨基末端修饰基团是烷基。优选的羧基末端修饰基团包括酰胺基，乙酸基，烷基酰胺基，芳基酰胺基或羟基。还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。

5. 发明公开

EP1503749A4 METHIONINE AMINOPEPTIDASE-2 INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：蛋氨酸氨基肽酶2抑制剂及其使用DERENY方法
公开(公告)号：EP1503749A4
公开(公告)日：2008-04-09
申请号：EP03724378
申请日：2003-05-02
申请人： PRAECIS PHARM INC
发明人： OLSON GARY L , SELF CHRISTOPHER , LEE LILY , COOK CHARLES MICHAEL , BIRKTOPF JENS , MORGAN BARRY , ARICO-MUENDEL CHRISTOPHER C
IPC分类号： C07D303/02 , C12N9/99 , A61K31/336 , A61K38/00 , A61K38/02 , A61K38/07 , A61K38/08 , A61K38/48 , A61K47/48 , A61P1/04 , A61P3/10 , A61P9/10 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/04 , A61P25/00 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/04 , A61P33/06 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P37/06 , A61P43/00 , C07D303/16 , C07D303/24 , C07D405/14 , C07K2/00 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/09 , C07K5/10 , C07K5/103 , C07K7/06 , C07K14/81
CPC分类号： C07D405/14 , A61K38/4886 , A61K47/64 , C07D303/16 , C07K5/0202 , C07K5/0606 , C07K5/0806 , C07K5/081 , C07K5/0817 , C07K5/1008 , C07K5/1024 , C07K7/06 , C07K14/8146
摘要： The present invention provides methods of treating a parasitic infection, a lymphoid malignancy or an autoimmune disorder in a subject by administering to the subject a therapeutically effective amount of an angiogenesis inhibitor compound comprising a MetAP-2 inhibitory core coupled to a peptide.

6. 发明专利

BR0115109A 未知
公开(公告)号：BR0115109A
公开(公告)日：2005-10-18
申请号：BR0115109
申请日：2001-11-01
申请人： PRAECIS PHARM INC
发明人： OLSON GARY L , SELF CHRISTOPHER , LEE LILY , COOK CHARLES MICHAEL , BIRKTOFT JENS , MORGAN BARRY , ARICO-MUENDEL CHRISTOPHER C
IPC分类号： C07D303/22 , A61K31/336 , A61K38/00 , A61K38/48 , A61K47/48 , A61P9/00 , A61P19/02 , A61P35/00 , A61P37/00 , A61P37/02 , C07D405/14 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/09 , C07K5/103 , C07K14/00 , C07K14/81 , C07D303/16 , A61K31/335
摘要： The present invention provides angiogenesis inhibitor compounds comprising a MetAP-2 inhibitory core coupled to a peptide, as well as pharmaceutical compositions comprising the angiogenesis inhibitor compounds and a pharmaceutically acceptable carrier. The present invention also provides methods of treating an angiogenic disease, e.g., cancer, in a subject by administering to the subject a therapeutically effective amount of one or more of the angiogenesis inhibitor compounds of the invention.

7. 发明专利

NO20031978A 未知
公开(公告)号：NO20031978A
公开(公告)日：2003-06-11
申请号：NO20031978
申请日：2003-04-30
申请人： PRAECIS PHARM INC
发明人： OLSON GARY L , SELF CHRISTOPHER , LEE LILY , COOK CHARLES MICHAEL , BIRKTOFT JENS , MORGAN BARRY A , ARICO-MUENDEL C CHRISTOPHER
IPC分类号： C07D303/22 , A61K31/336 , A61K38/00 , A61K38/48 , A61K47/48 , A61P9/00 , A61P19/02 , A61P35/00 , A61P37/00 , A61P37/02 , C07D405/14 , C07K5/02 , C07K5/06 , C07K5/083 , C07K5/09 , C07K5/103 , C07K14/00 , C07K14/81 , C07K5/00
CPC分类号： A61K38/4886 , A61K47/64 , C07D405/14 , C07K5/0202 , C07K5/0606 , C07K5/0806 , C07K5/081 , C07K5/0817 , C07K5/1008 , C07K14/8146

8. 发明专利

CA2362834A1 MODULATORS OF BETA-AMYLOID PEPTIDE AGGREGATION COMPRISING D-AMINO ACIDS 未知
公开(公告)号：CA2362834A1
公开(公告)日：2000-09-08
申请号：CA2362834
申请日：2000-03-03
申请人： PRAECIS PHARM INC
发明人： PHILLIPS KATHRYN , OLSON GARY L , SELF CHRISTOPHER , FINDEIS MARK A
IPC分类号： G01N33/68 , A61K38/00 , A61K38/17 , A61P25/28 , A61P43/00 , C07K5/083 , C07K7/06 , C07K14/47 , A61K38/08
摘要： Compounds that modulate natural .beta. amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably bas ed on a .beta. amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a .beta. amyloid peptide, preferably a retro-inverso isomer of A.beta.17-21. In certa in embodiments, the peptide is modified at the amino-terminus, the carboxy- terminus, or both. Preferred amino-terminal modifying groups alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an aceta te group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.

9. 发明专利

DE60035412T2 未知
公开(公告)号：DE60035412T2
公开(公告)日：2008-02-14
申请号：DE60035412
申请日：2000-03-03
申请人： PRAECIS PHARM INC
发明人： FINDEIS MARK A , PHILLIPS KATHRYN , OLSON GARY L , SELF CHRISTOPHER
IPC分类号： C07K14/47 , A61K38/00 , G01N33/68 , A61K38/17 , A61P25/28 , A61P43/00 , C07K5/083 , C07K7/06
摘要： Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an acetate group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.

10. 发明专利

DK1161449T3 未知
公开(公告)号：DK1161449T3
公开(公告)日：2007-11-05
申请号：DK00916028
申请日：2000-03-03
申请人： PRAECIS PHARM INC
发明人： FINDEIS MARK A , PHILLIPS KATHRYN , OLSON GARY L , SELF CHRISTOPHER
IPC分类号： C07K14/47 , A61K38/00 , G01N33/68 , A61K38/17 , A61P25/28 , A61P43/00 , C07K5/083 , C07K7/06
摘要： Compounds that modulate natural &bgr; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &bgr; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &bgr; amyloid peptide, preferably a retro-inverso isomer of A&bgr;17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an acetate group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.

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